The Physiological Effects of Dandelion (Taraxacum Officinale) in Type 2 Diabetes.

PubMed

Wirngo, Fonyuy E; Lambert, Max N; Jeppesen, Per B

2016-01-01

The tremendous rise in the economic burden of type 2 diabetes (T2D) has prompted a search for alternative and less expensive medicines. Dandelion offers a compelling profile of bioactive components with potential anti-diabetic properties. The Taraxacum genus from the Asteraceae family is found in the temperate zone of the Northern hemisphere. It is available in several areas around the world. In many countries, it is used as food and in some countries as therapeutics for the control and treatment of T2D. The anti-diabetic properties of dandelion are attributed to bioactive chemical components; these include chicoric acid, taraxasterol (TS), chlorogenic acid, and sesquiterpene lactones. Studies have outlined the useful pharmacological profile of dandelion for the treatment of an array of diseases, although little attention has been paid to the effects of its bioactive components on T2D to date. This review recapitulates previous work on dandelion and its potential for the treatment and prevention of T2D, highlighting its anti-diabetic properties, the structures of its chemical components, and their potential mechanisms of action in T2D. Although initial research appears promising, data on the cellular impact of dandelion are limited, necessitating further work on clonal β-cell lines (INS-1E), α-cell lines, and human skeletal cell lines for better identification of the active components that could be of use in the control and treatment of T2D. In fact, extensive in-vitro, in-vivo, and clinical research is required to investigate further the pharmacological, physiological, and biochemical mechanisms underlying the effects of dandelion-derived compounds on T2D.

The Physiological Effects of Dandelion (Taraxacum Officinale) in Type 2 Diabetes

PubMed Central

Wirngo, Fonyuy E.; Lambert, Max N.; Jeppesen, Per B.

2016-01-01

The tremendous rise in the economic burden of type 2 diabetes (T2D) has prompted a search for alternative and less expensive medicines. Dandelion offers a compelling profile of bioactive components with potential anti-diabetic properties. The Taraxacum genus from the Asteraceae family is found in the temperate zone of the Northern hemisphere. It is available in several areas around the world. In many countries, it is used as food and in some countries as therapeutics for the control and treatment of T2D. The anti-diabetic properties of dandelion are attributed to bioactive chemical components; these include chicoric acid, taraxasterol (TS), chlorogenic acid, and sesquiterpene lactones. Studies have outlined the useful pharmacological profile of dandelion for the treatment of an array of diseases, although little attention has been paid to the effects of its bioactive components on T2D to date. This review recapitulates previous work on dandelion and its potential for the treatment and prevention of T2D, highlighting its anti-diabetic properties, the structures of its chemical components, and their potential mechanisms of action in T2D. Although initial research appears promising, data on the cellular impact of dandelion are limited, necessitating further work on clonal β-cell lines (INS-1E), α-cell lines, and human skeletal cell lines for better identification of the active components that could be of use in the control and treatment of T2D. In fact, extensive in-vitro, in-vivo, and clinical research is required to investigate further the pharmacological, physiological, and biochemical mechanisms underlying the effects of dandelion-derived compounds on T2D. PMID:28012278

ITPI: Initial Transcription Process-Based Identification Method of Bioactive Components in Traditional Chinese Medicine Formula

PubMed Central

Zhang, Baixia; Li, Yanwen; Zhang, Yanling; Li, Zhiyong; Bi, Tian; He, Yusu; Song, Kuokui; Wang, Yun

2016-01-01

Identification of bioactive components is an important area of research in traditional Chinese medicine (TCM) formula. The reported identification methods only consider the interaction between the components and the target proteins, which is not sufficient to explain the influence of TCM on the gene expression. Here, we propose the Initial Transcription Process-based Identification (ITPI) method for the discovery of bioactive components that influence transcription factors (TFs). In this method, genome-wide chip detection technology was used to identify differentially expressed genes (DEGs). The TFs of DEGs were derived from GeneCards. The components influencing the TFs were derived from STITCH. The bioactive components in the formula were identified by evaluating the molecular similarity between the components in formula and the components that influence the TF of DEGs. Using the formula of Tian-Zhu-San (TZS) as an example, the reliability and limitation of ITPI were examined and 16 bioactive components that influence TFs were identified. PMID:27034696

Lactic Acid Bacteria and Bifidobacteria with Potential to Design Natural Biofunctional Health-Promoting Dairy Foods.

PubMed

Linares, Daniel M; Gómez, Carolina; Renes, Erica; Fresno, José M; Tornadijo, María E; Ross, R P; Stanton, Catherine

2017-01-01

Consumer interest in healthy lifestyle and health-promoting natural products is a major driving force for the increasing global demand of biofunctional dairy foods. A number of commercial sources sell synthetic formulations of bioactive substances for use as dietary supplements. However, the bioactive-enrichment of health-oriented foods by naturally occurring microorganisms during dairy fermentation is in increased demand. While participating in milk fermentation, lactic acid bacteria can be exploited in situ as microbial sources for naturally enriching dairy products with a broad range of bioactive components that may cover different health aspects. Several of these bioactive metabolites are industrially and economically important, as they are claimed to exert diverse health-promoting activities on the consumer, such as anti-hypertensive, anti-inflammatory, and anti-diabetic, anti-oxidative, immune-modulatory, anti-cholesterolemic, or microbiome modulation. This review aims at discussing the potential of these health-supporting bacteria as starter or adjunct cultures for the elaboration of dairy foods with a broad spectrum of new functional properties and added value.

Microgreens: Production, shelf life, and bioactive components.

PubMed

Mir, Shabir Ahmad; Shah, Manzoor Ahmad; Mir, Mohammad Maqbool

2017-08-13

Microgreens are emerging specialty food products which are gaining popularity and increased attention nowadays. They are young and tender cotyledonary leafy greens that are found in a pleasing palette of colors, textures, and flavors. Microgreens are a new class of edible vegetables harvested when first leaves have fully expanded and before true leaves have emerged. They are gaining popularity as a new culinary ingredient. They are used to enhance salads or as edible garnishes to embellish a wide variety of other dishes. Common microgreens are grown mainly from mustard, cabbage, radish, buckwheat, lettuce, spinach, etc. The consumption of microgreens has nowadays increased due to higher concentrations of bioactive components such as vitamins, minerals, and antioxidants than mature greens, which are important for human health. However, they typically have a short shelf life due to rapid product deterioration. This review aimed to evaluate the postharvest quality, potential bioactive compounds, and shelf life of microgreens for proper management of this specialty produce.

The role of seaweed bioactives in the control of digestion: implications for obesity treatments.

PubMed

Chater, Peter I; Wilcox, Matthew D; Houghton, David; Pearson, Jeffrey P

2015-11-01

Seaweeds are an underutilised nutritional resource that could not only compliment the current western diet but potentially bring additional health benefits over and above their nutritional value. There are four groups of seaweed algae; green algae (Chlorophyceae), red algae (Rhodophycae), blue-green algae (Cyanophyceae) and brown algae (Phaeophyceae). Seaweeds are rich in bioactive components including polysaccharides and polyphenols. Polysaccharides content, such as fucoidan, laminarin, as well as alginate is generally high in brown seaweeds which are also a source of polyphenols such as phenolic acids, flavonoids, phlorotannin, stilbenes and lignans. These components have been shown to reduce the activity of digestive enzymes, modulating enzymes such as α-amylase, α-glucosidase, pepsin and lipase. This review discusses the effect of several of these components on the digestive processes within the gastrointestinal tract; focusing on the effect of alginate on pancreatic lipase activity and its potential health benefits. Concluding that there is evidence to suggest alginate has the potential to be used as an obesity treatment, however, further in vivo research is required and an effective delivery method for alginate must be designed.

Complementary effects of cereal and pulse polyphenols and dietary fiber on chronic inflammation and gut health.

PubMed

Awika, Joseph M; Rose, Devin J; Simsek, Senay

2018-03-01

Cereal grains and grain pulses are primary staples often consumed together, and contribute a major portion of daily human calorie and protein intake globally. Protective effects of consuming whole grain cereals and grain pulses against various inflammation-related chronic diseases are well documented. However, potential benefits of combined intake of whole cereals and pulses beyond their complementary amino acid nutrition is rarely considered in literature. There is ample evidence that key bioactive components of whole grain cereals and pulses are structurally different and thus may be optimized to provide synergistic/complementary health benefits. Among the most important whole grain bioactive components are polyphenols and dietary fiber, not only because of their demonstrated biological function, but also their major impact on consumer choice of whole grain/pulse products. This review highlights the distinct structural differences between key cereal grain and pulse polyphenols and non-starch polysaccharides (dietary fiber), and the evidence on specific synergistic/complementary benefits of combining the bioactive components from the two commodities. Interactive effects of the polyphenols and fiber on gut microbiota and associated benefits to colon health, and against systemic inflammation, are discussed. Processing technologies that can be used to further enhance the interactive benefits of combined cereal-pulse bioactive compounds are highlighted.

Red Raspberries and Their Bioactive Polyphenols: Cardiometabolic and Neuronal Health Links12

PubMed Central

Burton-Freeman, Britt M; Sandhu, Amandeep K; Edirisinghe, Indika

2016-01-01

Diet is an essential factor that affects the risk of modern-day metabolic diseases, including cardiovascular disease, diabetes mellitus, obesity, and Alzheimer disease. The potential ability of certain foods and their bioactive compounds to reverse or prevent the progression of the pathogenic processes that underlie these diseases has attracted research attention. Red raspberries (Rubus idaeus L.) are unique berries with a rich history and nutrient and bioactive composition. They possess several essential micronutrients, dietary fibers, and polyphenolic components, especially ellagitannins and anthocyanins, the latter of which give them their distinctive red coloring. In vitro and in vivo studies have revealed various mechanisms through which anthocyanins and ellagitannins (via ellagic acid or their urolithin metabolites) and red raspberry extracts (or the entire fruit) could reduce the risk of or reverse metabolically associated pathophysiologies. To our knowledge, few studies in humans are available for evaluation. We review and summarize the available literature that assesses the health-promoting potential of red raspberries and select components in modulating metabolic disease risk, especially cardiovascular disease, diabetes mellitus, obesity, and Alzheimer disease—all of which share critical metabolic, oxidative, and inflammatory links. The body of research is growing and supports a potential role for red raspberries in reducing the risk of metabolically based chronic diseases. PMID:26773014

The major bioactive components of seaweeds and their mosquitocidal potential.

PubMed

Yu, Ke-Xin; Jantan, Ibrahim; Ahmad, Rohani; Wong, Ching-Lee

2014-09-01

Seaweeds are one of the most widely studied natural resources for their biological activities. Novel seaweed compounds with unique chemical structures have been reported for their pharmacological properties. The urge to search for novel insecticidal compound with a new mode of action for development of botanical insecticides supports the relevant scientific research on discovering the bioactive compounds in seaweeds. The mosquitocidal potential of seaweed extracts and their isolated compounds are documented in this review paper, along with the discussion on bioactivities of the major components of seaweeds such as polysaccharides, phenolics, proteins, terpenes, lipids, and halogenated compounds. The effects of seaweed extracts and compounds toward different life stages of mosquito (egg, larva, pupa, and adult), its growth, development, and reproduction are elaborated. The structure-activity relationships of mosquitocidal compounds are discussed to extrapolate the possible chemical characteristics of seaweed compounds responsible for insecticidal properties. Furthermore, the possible target sites and mode of actions of the mosquitocidal seaweed compounds are included in this paper. The potential synergistic effects between seaweeds and commercial insecticides as well as the toxic effects of seaweed extracts and compounds toward other insects and non-target organisms in the same habitat are also described. On top of that, various factors that influence the mosquitocidal potential of seaweeds, such as abiotic and biotic variables, sample preparation, test procedures, and considerations for a precise experimental design are discussed. The potential of active seaweed extracts and compounds in the development of effective bioinsecticide are also discussed.

Exposing Differences in Monomer Exchange Rates of Multicomponent Supramolecular Polymers in Water.

PubMed

Baker, Matthew B; Gosens, Ronald P J; Albertazzi, Lorenzo; Matsumoto, Nicholas M; Palmans, Anja R A; Meijer, E W

2016-02-02

The formation of multicomponent and bioactive supramolecular polymers is a promising strategy for the formation of biomaterials that match the dynamic and responsive nature of biological systems. In order to fully realize the potential of this strategy, knowledge of the location and behavior of bioactive components within the system is crucial. By employing synthetic strategies to create multifunctional monomers, coupled with FRET and STORM techniques, we have investigated the formation and behavior of a bioactive and multicomponent supramolecular polymer. By creating a peptide-dye-monomer conjugate, we were able to measure high degrees of monomer incorporation and to visualize the equal distribution of monomers within the supramolecular polymer. Furthermore, by tracking the movement of monomers, we uncovered small differences in the dynamics of the bioactive monomers. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chondrogenic potential of physically treated bovine cartilage matrix derived porous scaffolds on human dermal fibroblast cells.

PubMed

Moradi, Ali; Ataollahi, Forough; Sayar, Katayoun; Pramanik, Sumit; Chong, Pan-Pan; Khalil, Alizan Abdul; Kamarul, Tunku; Pingguan-Murphy, Belinda

2016-01-01

Extracellular matrices have drawn attention in tissue engineering as potential biomaterials for scaffold fabrication because of their bioactive components. Noninvasive techniques of scaffold fabrication and cross-linking treatments are believed to maintain the integrity of bioactive molecules while providing proper architectural and mechanical properties. Cartilage matrix derived scaffolds are designed to support the maintenance of chondrocytes and provide proper signals for differentiation of chondroinducible cells. Chondroinductive potential of bovine articular cartilage matrix derived porous scaffolds on human dermal fibroblasts and the effect of scaffold shrinkage on chondrogenesis were investigated. An increase in sulfated glycosaminoglycans production along with upregulation of chondrogenic genes confirmed that physically treated cartilage matrix derived scaffolds have chondrogenic potential on human dermal fibroblasts. © 2015 Wiley Periodicals, Inc.

Lactic Acid Bacteria and Bifidobacteria with Potential to Design Natural Biofunctional Health-Promoting Dairy Foods

PubMed Central

Linares, Daniel M.; Gómez, Carolina; Renes, Erica; Fresno, José M.; Tornadijo, María E.; Ross, R. P.; Stanton, Catherine

2017-01-01

Consumer interest in healthy lifestyle and health-promoting natural products is a major driving force for the increasing global demand of biofunctional dairy foods. A number of commercial sources sell synthetic formulations of bioactive substances for use as dietary supplements. However, the bioactive-enrichment of health-oriented foods by naturally occurring microorganisms during dairy fermentation is in increased demand. While participating in milk fermentation, lactic acid bacteria can be exploited in situ as microbial sources for naturally enriching dairy products with a broad range of bioactive components that may cover different health aspects. Several of these bioactive metabolites are industrially and economically important, as they are claimed to exert diverse health-promoting activities on the consumer, such as anti-hypertensive, anti-inflammatory, and anti-diabetic, anti-oxidative, immune-modulatory, anti-cholesterolemic, or microbiome modulation. This review aims at discussing the potential of these health-supporting bacteria as starter or adjunct cultures for the elaboration of dairy foods with a broad spectrum of new functional properties and added value. PMID:28572792

Dietary bioactives: establishing a scientific framework for recommended intakes

USDA-ARS?s Scientific Manuscript database

Research has shown that numerous dietary bioactive components that are not considered essential may still be beneficial to health. The dietary reference intake (DRI) process has been applied to nonessential nutrients, such as fiber, yet the majority of bioactive components await a recommended intake...

Suppression of tumor growth by Pleurotus ferulae ethanol extract through induction of cell apoptosis, and inhibition of cell proliferation and migration.

PubMed

Wang, Weilan; Chen, Kaixu; Liu, Qing; Johnston, Nathan; Ma, Zhenghai; Zhang, Fuchun; Zheng, Xiufen

2014-01-01

Cancer is the second leading cause of death worldwide. Edible medicinal mushrooms have been used in traditional medicine as regimes for cancer patients. Recently anti-cancer bioactive components from some mushrooms have been isolated and their anti-cancer effects have been tested. Pleurotus ferulae, a typical edible medicinal mushroom in Xinjiang China, has also been used to treat cancer patients in folk medicine. However, little studies have been reported on the anti-cancer components of Pleurotus ferulae. This study aims to extract bioactive components from Pleurotus ferulae and to investigate the anti-cancer effects of the extracts. We used ethanol to extract anti-cancer bioactive components enriched with terpenoids from Pleurotus ferulae. We tested the anti-tumour effects of ethanol extracts on the melanoma cell line B16F10, the human gastric cancer cell line BGC 823 and the immortalized human gastric epithelial mucosa cell line GES-1 in vitro and a murine melanoma model in vivo. Cell toxicity and cell proliferation were measured by MTT assays. Cell cycle progression, apoptosis, caspase 3 activity, mitochondrial membrane potential (MMP), migration and gene expression were studied in vitro. PFEC suppressed tumor cell growth, inhibited cell proliferation, arrested cells at G0/G1 phases and was not toxic to non-cancer cells. PFEC also induced cell apoptosis and necrosis, increased caspase 3 activity, reduced the MMP, prevented cell invasion and changed the expression of genes associated with apoptosis and the cell cycle. PFEC delayed tumor formation and reduced tumor growth in vivo. In conclusion, ethanol extracted components from Pleurotus ferulae exert anti-cancer effects through direct suppression of tumor cell growth and invasion, demonstrating its therapeutic potential in cancer treatment.

A Non-Biological Method for Screening Active Components against Influenza Virus from Traditional Chinese Medicine by Coupling a LC Column with Oseltamivir Molecularly Imprinted Polymers

PubMed Central

Yang, Ya-Jun; Li, Jian-Yong; Liu, Xi-Wang; Zhang, Ji-Yu; Liu, Yu-Rong; Li, Bing

2013-01-01

To develop a non-biological method for screening active components against influenza virus from traditional Chinese medicine (TCM) extraction, a liquid chromatography (LC) column prepared with oseltamivir molecularly imprinted polymer (OSMIP) was employed with LC-mass spectrometry (LC-MS). From chloroform extracts of compound TCM liquid preparation, we observed an affinitive component m/z 249, which was identified to be matrine following analysis of phytochemical literatures, OSMIP-LC column on-line of control compounds and MS/MS off-line. The results showed that matrine had similar bioactivities with OS against avian influenza virus H9N2 in vitro for both alleviating cytopathic effect and hemagglutination inhibition and that the stereostructures of these two compounds are similar while their two-dimensional structures were different. In addition, our results suggested that the bioactivities of those affinitive compounds were correlated with their chromatographic behaviors, in which less difference of the chromatographic behaviors might have more similar bioactivities. This indicates that matrine is a potential candidate drug to prevent or cure influenza for human or animal. In conclusion, the present study showed that molecularly imprinted polymers can be used as a non-biological method for screening active components against influenza virus from TCM. PMID:24386385

Multi-component identification and target cell-based screening of potential bioactive compounds in toad venom by UPLC coupled with high-resolution LTQ-Orbitrap MS and high-sensitivity Qtrap MS.

PubMed

Ren, Wei; Han, Lingyu; Luo, Mengyi; Bian, Baolin; Guan, Ming; Yang, Hui; Han, Chao; Li, Na; Li, Tuo; Li, Shilei; Zhang, Yangyang; Zhao, Zhenwen; Zhao, Haiyu

2018-04-28

Traditional Chinese medicines (TCMs) are undoubtedly treasured natural resources for discovering effective medicines in treating and preventing various diseases. However, it is still extremely difficult for screening the bioactive compounds due to the tremendous constituents in TCMs. In this work, the chemical composition of toad venom was comprehensively analyzed using ultra-high performance liquid chromatography (UPLC) coupled with high-resolution LTQ-Orbitrap mass spectrometry and 93 compounds were detected. Among them, 17 constituents were confirmed by standard substances and 8 constituents were detected in toad venom for the first time. Further, a compound database of toad venom containing the fullest compounds was further constructed using UPLC coupled with high-sensitivity Qtrap MS. Then a target cell-based approach for screening potential bioactive compounds from toad venom was developed by analyzing the target cell extracts. The reliability of this method was validated by negative controls and positive controls. In total, 17 components in toad venom were discovered to interact with the target cancer cells. Further, in vitro pharmacological trials were performed to confirm the anti-cancer activity of four of them. The results showed that the six bufogenins and seven bufotoxins detected in our research represented a promising resource to explore bufogenins/bufotoxins-based anticancer agents with low cardiotoxic effect. The target cell-based screening method coupled with the compound database of toad venom constructed by UPLC-Qtrap-MS with high sensitivity provide us a new strategy to rapidly screen and identify the potential bioactive constituents with low content in natural products, which was beneficial for drug discovery from other TCMs. ᅟ Graphical abstract.

Epigenetics of breast cancer: modifying role of environmental and bioactive food compounds

PubMed Central

Romagnolo, Donato F.; Daniels, Kevin D.; Grunwald, Jonathan T.; Ramos, Stephan A.; Propper, Catherine R.; Selmin, Ornella I.

2017-01-01

Scope Reduced expression of tumor suppressor genes (TSG) increases the susceptibility to breast cancer. However, only a small percentage of breast tumors is related to family history and mutational inactivation of TSG. Epigenetics refers to non-mutational events that alter gene expression. Endocrine disruptors found in foods and drinking water may disrupt epigenetically hormonal regulation and increase breast cancer risk. This review centers on the working hypothesis that agonists of the aromatic hydrocarbon receptor (AHR); bisphenol A (BPA); and arsenic compounds, induce in TSG epigenetic signatures that mirror those often seen in sporadic breast tumors. Conversely, it is hypothesized that bioactive food components that target epigenetic mechanisms protect against sporadic breast cancer induced by these disruptors. Methods and results This review highlights 1) overlaps between epigenetic signatures placed in TSG by AHR-ligands, BPA, and arsenic with epigenetic alterations associated with sporadic breast tumorigenesis; and 2) potential opportunities for prevention of sporadic breast cancer with food components that target the epigenetic machinery. Conclusions Characterizing the overlap between epigenetic signatures elicited in TSG by endocrine disruptors with those observed in sporadic breast tumors may afford new strategies for breast cancer prevention with specific bioactive food components or diet. PMID:27144894

Bioactive Components in Fish Venoms

PubMed Central

Ziegman, Rebekah; Alewood, Paul

2015-01-01

Animal venoms are widely recognized excellent resources for the discovery of novel drug leads and physiological tools. Most are comprised of a large number of components, of which the enzymes, small peptides, and proteins are studied for their important bioactivities. However, in spite of there being over 2000 venomous fish species, piscine venoms have been relatively underrepresented in the literature thus far. Most studies have explored whole or partially fractioned venom, revealing broad pharmacology, which includes cardiovascular, neuromuscular, cytotoxic, inflammatory, and nociceptive activities. Several large proteinaceous toxins, such as stonustoxin, verrucotoxin, and Sp-CTx, have been isolated from scorpaenoid fish. These form pores in cell membranes, resulting in cell death and creating a cascade of reactions that result in many, but not all, of the physiological symptoms observed from envenomation. Additionally, Natterins, a novel family of toxins possessing kininogenase activity have been found in toadfish venom. A variety of smaller protein toxins, as well as a small number of peptides, enzymes, and non-proteinaceous molecules have also been isolated from a range of fish venoms, but most remain poorly characterized. Many other bioactive fish venom components remain to be discovered and investigated. These represent an untapped treasure of potentially useful molecules. PMID:25941767

High-pressure processing as emergent technology for the extraction of bioactive ingredients from plant materials.

PubMed

Jun, Xi

2013-01-01

High-pressure processing is a food processing technique that has shown great potentials in the food industry. Recently, it was developed to extract bioactive ingredients from plant materials, known as ultrahigh pressure extraction (UPE), taking advantages of time saving, higher extraction yields, fewer impurities in the extraction solution, minimal heat and can avoid thermal degradation on the activity and structure of bioactive components, and so on. This review provides an overview of the developments in the UPE of bioactive ingredients from plant material. Apart from a brief presentation of the theories of UPE and extraction equipment systems, the principal parameters that influence the extraction efficiency to be optimized in the UPE (e.g., solvent, pressure, temperature, extraction time, and the number of cycle) were discussed in detail, and finally the more recent applications of UPE for the extraction of active compounds from plant materials were summarized.

Chemopreventive Properties of Dietary Rice Bran: Current Status and Future Prospects12

PubMed Central

Henderson, Angela J.; Ollila, Cadie A.; Kumar, Ajay; Borresen, Erica C.; Raina, Komal; Agarwal, Rajesh; Ryan, Elizabeth P.

2012-01-01

Emerging evidence suggests that dietary rice bran may exert beneficial effects against several types of cancer, such as breast, lung, liver, and colorectal cancer. The chemopreventive potential has been related to the bioactive phytochemicals present in the bran portion of the rice such as ferulic acid, tricin, β-sitosterol, γ-oryzanol, tocotrienols/tocopherols, and phytic acid. Studies have shown that the anticancer effects of the rice bran–derived bioactive components are mediated through their ability to induce apoptosis, inhibit cell proliferation, and alter cell cycle progression in malignant cells. Rice bran bioactive components protect against tissue damage through the scavenging of free radicals and the blocking of chronic inflammatory responses. Rice bran phytochemicals have also been shown to activate anticancer immune responses as well as affecting the colonic tumor microenvironment in favor of enhanced colorectal cancer chemoprevention. This is accomplished through the modulation of gut microflora communities and the regulation of carcinogen-metabolizing enzymes. In addition, the low cost of rice production and the accessibility of rice bran make it an appealing candidate for global dietary chemoprevention. Therefore, the establishment of dietary rice bran as a practical food-derived chemopreventive agent has the potential to have a significant impact on cancer prevention for the global population. PMID:22983843

Infant formula and infant nutrition: bioactive proteins of human milk and implications for composition of infant formulas.

PubMed

Lönnerdal, Bo

2014-03-01

Human milk contains an abundance of biologically active components that are highly likely to contribute to the short- and long-term benefits of breastfeeding. Many of these components are proteins; this article describes some of these proteins, such as α-lactalbumin, lactoferrin, osteopontin, and milk fat globule membrane proteins. The possibility of adding their bovine counterparts to infant formula is discussed as well as the implications for infant health and development. An important consideration when adding bioactive proteins to infant formula is that the total protein content of formula needs to be reduced, because formula-fed infants have significantly higher concentrations of serum amino acids, insulin, and blood urea nitrogen than do breastfed infants. When reducing the protein content of formula, the amino acid composition of the formula protein becomes important because serum concentrations of the essential amino acids should not be lower than those in breastfed infants. Both the supply of essential amino acids and the bioactivities of milk proteins are dependent on their digestibility: some proteins act only in intact form, others act in the form of larger or small peptides formed during digestion, and some are completely digested and serve as a source of amino acids. The purity of the proteins or protein fractions, potential contaminants of the proteins (such as lipopolysaccharide), as well as the degree of heat processing used during their isolation also need to be considered. It is likely that there will be more bioactive components added to infant formulas in the near future, but guidelines on how to assess their bioactivities in vitro, in animal models, and in clinical studies need to be established. The extent of testing needed is likely going to depend on the degree of complexity of the components and their bioequivalence with the human compounds whose effects they are intended to mimic.

Crystals and crystallization in oil-in-water emulsions: implications for emulsion-based delivery systems.

PubMed

McClements, David Julian

2012-06-15

Many bioactive components intended for oral ingestion (pharmaceuticals and nutraceuticals) are hydrophobic molecules with low water-solubilities and high melting points, which poses considerable challenges to the formulation of oral delivery systems. Oil-in-water emulsions are often suitable vehicles for the encapsulation and delivery of this type of bioactive component. The bioactive component is usually dissolved in a carrier lipid phase by either dilution and/or heating prior to homogenization, and then the carrier lipid and water phases are homogenized to form an emulsion consisting of small oil droplets dispersed in water. The successful development of this kind of emulsion-based delivery system depends on a good understanding of the influence of crystals on the formation, stability, and properties of emulsions. This review article addresses the physicochemical phenomena associated with the encapsulation, retention, crystallization, release, and absorption of hydrophobic bioactive components within emulsions. This knowledge will be useful for the rational formulation of effective emulsion-based delivery systems for oral delivery of crystalline hydrophobic bioactive components in the food, health care, and pharmaceutical industries. Copyright © 2012 Elsevier B.V. All rights reserved.

Fast Centrifugal Partition Chromatography Fractionation of Concentrated Agave (Agave salmiana) Sap to Obtain Saponins with Apoptotic Effect on Colon Cancer Cells.

PubMed

Santos-Zea, Liliana; Fajardo-Ramírez, Oscar R; Romo-López, Irasema; Gutiérrez-Uribe, Janet A

2016-03-01

Separation of potentially bioactive components from foods and plant extracts is one of the main challenges for their study. Centrifugal partition chromatography has been a successful technique for the screening and identification of molecules with bioactive potential, such as steroidal saponins. Agave is a source of steroidal saponins with anticancer potential, though the activity of these compounds in concentrated agave sap has not been yet explored. In this study, fast centrifugal partition chromatography (FCPC) was used coupled with in vitro tests on HT-29 cells as a screening procedure to identify apoptotic saponins from an acetonic extract of concentrated agave sap. The three most bioactive fractions obtained by FCPC at partition coefficients between 0.23 and 0.4 contained steroidal saponins, predominantly magueyoside b. Flow cytometry analysis determined that the fraction rich in kammogenin and manogenin glycosides induced apoptosis, but when gentrogenin and hecogenin glycosides were also found in the fraction, a necrotic effect was observed. In conclusion, this study provides the evidence that steroidal saponins in concentrated agave sap were potential inductors of apoptosis and that it was possible to separate them using fast centrifugal partition chromatography.

Cocoa Bioactive Compounds: Significance and Potential for the Maintenance of Skin Health

PubMed Central

Scapagnini, Giovanni; Davinelli, Sergio; Di Renzo, Laura; De Lorenzo, Antonino; Olarte, Hector Hugo; Micali, Giuseppe; Cicero, Arrigo F.; Gonzalez, Salvador

2014-01-01

Cocoa has a rich history in human use. Skin is prone to the development of several diseases, and the mechanisms in the pathogenesis of aged skin are still poorly understood. However, a growing body of evidence from clinical and bench research has begun to provide scientific validation for the use of cocoa-derived phytochemicals as an effective approach for skin protection. Although the specific molecular and cellular mechanisms of the beneficial actions of cocoa phytochemicals remain to be elucidated, this review will provide an overview of the current literature emphasizing potential cytoprotective pathways modulated by cocoa and its polyphenolic components. Moreover, we will summarize in vivo studies showing that bioactive compounds of cocoa may have a positive impact on skin health. PMID:25116848

Citrus medica: nutritional, phytochemical composition and health benefits - a review.

PubMed

Chhikara, Navnidhi; Kour, Ragni; Jaglan, Sundeep; Gupta, Pawan; Gat, Yogesh; Panghal, Anil

2018-04-25

Citrus medica (Citron) is an underutilized fruit plant having various bioactive components in all parts of the plant. The major bioactive compounds present are iso-limonene, citral, limonene, phenolics, flavonones, vitamin C, pectin, linalool, decanal, and nonanal, accounting for several health benefits. Pectin and heteropolysachharides also play a major role as dietary fibers. The potential impact of citron and its bioactive components to prevent or reverse destructive deregulated processes responsible for certain diseases has attracted different researchers' attention. The fruit has numerous nutraceutical benefits, proven by pharmacological studies; for example, anti-catarrhal, capillary protector, anti-hypertensive, diuretic, antibacterial, antifungal, anthelmintic, antimicrobial, analgesic, strong antioxidant, anticancerous, antidiabetic, estrogenic, antiulcer, cardioprotective, and antihyperglycemic. The present review explores new insights into the benefits of citron in various body parts. Throughout the world, citron has been used in making carbonated drinks, alcoholic beverages, syrup, candied peels, jams, marmalade, cordials, and many other value added products, which suggests it is an appropriate raw material to develop healthy processed food. In the present review, the fruit taxonomical classification, beneficial phytochemicals, antioxidant activities, and health benefits are discussed.

Modulation of the multidrug efflux pump EmrD-3 from Vibrio cholerae by Allium sativum extract and the bioactive agent allyl sulfide plus synergistic enhancement of antimicrobial susceptibility by A. sativum extract.

PubMed

Bruns, Merissa M; Kakarla, Prathusha; Floyd, Jared T; Mukherjee, Mun Mun; Ponce, Robert C; Garcia, John A; Ranaweera, Indrika; Sanford, Leslie M; Hernandez, Alberto J; Willmon, T Mark; Tolson, Grace L; Varela, Manuel F

2017-10-01

The causative agent of cholera, Vibrio cholerae, is a public health concern. Multidrug-resistant V. cholerae variants may reduce chemotherapeutic efficacies of severe cholera. We previously reported that the multidrug efflux pump EmrD-3 from V. cholerae confers resistance to multiple structurally distinct antimicrobials. Medicinal plant compounds are potential candidates for EmrD-3 efflux pump modulation. The antibacterial activities of garlic Allium sativum, although poorly understood, predicts that a main bioactive component, allyl sulfide, modulates EmrD-3 efflux. Thus, we tested whether A. sativum extract acts in synergy with antimicrobials and that a main bioactive component allyl sulfide inhibits EmrD-3 efflux. We found that A. sativum extract and allyl sulfide inhibited ethidium bromide efflux in cells harboring EmrD-3 and that A. sativum lowered the MICs of multiple antibacterials. We conclude that A. sativum and allyl sulfide inhibit EmrD-3 and that A. sativum extract synergistically enhances antibacterial agents.

Designing biopolymer microgels to encapsulate, protect and deliver bioactive components: Physicochemical aspects.

PubMed

McClements, David Julian

2017-02-01

Biopolymer microgels have considerable potential for their ability to encapsulate, protect, and release bioactive components. Biopolymer microgels are small particles (typically 100nm to 1000μm) whose interior consists of a three-dimensional network of cross-linked biopolymer molecules that traps a considerable amount of solvent. This type of particle is also sometimes referred to as a nanogel, hydrogel bead, biopolymer particles, or microsphere. Biopolymer microgels are typically prepared using a two-step process involving particle formation and particle gelation. This article reviews the major constituents and fabrication methods that can be used to prepare microgels, highlighting their advantages and disadvantages. It then provides an overview of the most important characteristics of microgel particles (such as size, shape, structure, composition, and electrical properties), and describes how these parameters can be manipulated to control the physicochemical properties and functional attributes of microgel suspensions (such as appearance, stability, rheology, and release profiles). Finally, recent examples of the utilization of biopolymer microgels to encapsulate, protect, or release bioactive agents, such as pharmaceuticals, nutraceuticals, enzymes, flavors, and probiotics is given. Copyright © 2016 Elsevier B.V. All rights reserved.

Bioactive components and mechanisms of Chinese poplar propolis alleviates oxidized low-density lipoprotein-induced endothelial cells injury.

PubMed

Chang, Huasong; Yuan, Wenwen; Wu, Haizhu; Yin, Xusheng; Xuan, Hongzhuan

2018-05-03

Propolis, a polyphenol-rich natural product, has been used as a functional food in anti-inflammation. However, its bioactive components and mechanisms have not been fully elucidated. To discover the bioactive components and anti-inflammatory mechanism, we prepared and separated 8 subfractions from ethyl acetate extract of Chinese propolis (EACP) and investigated the mechanism in oxidized low density lipoprotein (ox-LDL) induced human umbilical vein endothelial cells (HUVECs) damage. Eight subfractions were prepared and separated from ethyl acetate extract of Chinese propolis (EACP) with different concentrations of methanol-water solution, and analysed its chemical constituents by HPLC-DAD/Q-TOF-MS. Then 80% confluent HUVECs were stimulated with 40 μg/mL ox-LDL. Cell viability and apoptosis were evaluated by Sulforhodamine B (SRB) assay and Hoechst 33,258 staining, respectively. Levels of caspase 3, PARP, LC3B, p62, p-mTOR, p-p70S6K, p-PI3K, p-Akt, LOX-1 and p-p38 MAPK were assessed by western blotting and immunofluorescence assay, respectively. Reactive oxygen species (ROS) and mitochondrial membrane potential (MMP) were measured with fluorescent probes. Each subfraction exhibited similar protective effect although the contents of chemical constituents were different. EACP attenuated ox-LDL induced HUVECs apoptosis, depressed the ratio of LC3-II/LC3-I and enhanced the p62 level. In addition, treatment with EACP also activated the phosphorylation of PI3K/Akt/mTOR, and deactivated the level of LOX-1 and phosphorylation of p38 MAPK. The overproduction of ROS and the damage of MMP were also ameliorated after ECAP treatment. These findings indicated that the bioactive component of propolis on anti-inflammatory activity was not determined by a single constituent, but a complex interaction including flavonoids, esters and phenolic acids. EACP attenuated ox-LDL induced HUVECs injury by inhibiting LOX-1 level and depressed ROS production against oxidative stress in ox-LDL induced HUVECs, further to activate PI3K/Akt/mTOR pathway and deactivate p38 MAPK to inhibit apoptosis and autophagy, which provide novel insights into the potential application of propolis on modulating chronic inflammation.

Clinical applications of bioactive milk components

PubMed Central

Newburg, David S.

2015-01-01

Milk represents a unique resource for translational medicine: It contains a rich pool of biologically active molecules with demonstrated clinical benefits. The ongoing characterization of the mechanistic process through which milk components promote development and immunity has revealed numerous milk-derived compounds with potential applications as clinical therapies in infectious and inflammatory disease, cancer, and other conditions. Lactoferrin is an effective antimicrobial and antiviral agent in high-risk patient populations and a potentially potent adjuvant to chemotherapy in lung cancer. Enteric nutrition formulas supplemented with transforming growth factor β, a milk cytokine, have been shown to promote remission in pediatric Crohn's disease. A number of milk glycans, including human milk oligosaccharides, show promise in preclinical studies as antimicrobial and anti-inflammatory agents. While active preclinical investigations of human milk may soon result in large-scale production of human milk molecules, bovine milk components in many instances represent a practical source of bioactive milk compounds for use in clinical trials. This review summarizes current efforts to translate the compounds derived from human and bovine milk into effective clinical therapies. These efforts suggest a common pathway for the translation of milk-derived compounds into clinical applications. PMID:26011900

Targeting the Epigenome with Bioactive Food Components for Cancer Prevention

PubMed Central

Ong, Thomas Prates; Moreno, Fernando Salvador; Ross, Sharon Ann

2012-01-01

Epigenetic processes participate in cancer development and likely influence cancer prevention. Global DNA hypomethylation, gene promoter hypermethylation and aberrant histone post-translational modifications are hallmarks of neoplastic cells which have been associated with genomic instability and altered gene expression. Because epigenetic deregulation occurs early in carcinogenesis and is potentially reversible, intervention strategies targeting the epigenome have been proposed for cancer prevention. Bioactive food components (BFCs) with anticancer potential, including folate, polyphenols, selenium, retinoids, fatty acids, isothiocyanates and allyl compounds, influence DNA methylation and histone modification processes. Such activities have been shown to affect the expression of genes involved in cell proliferation, death and differentiation that are frequently altered in cancer. Although the epigenome represents a promising target for cancer prevention with BFCs, few studies have addressed the influence of dietary components on these mechanisms in vivo, particularly on the phenotype of humans, and thus the exact mechanisms whereby diet mediates an effect on cancer prevention remains unclear. Primary factors that should be elucidated include the effective doses and dose timing of BFCs to attain epigenetic effects. Because diet-epigenome interactions are likely to occur in utero, the impact of early-life nutrition on cancer risk programming should be further investigated. PMID:22353664

Clinical applications of bioactive milk components.

PubMed

Hill, David R; Newburg, David S

2015-07-01

Milk represents a unique resource for translational medicine: It contains a rich pool of biologically active molecules with demonstrated clinical benefits. The ongoing characterization of the mechanistic process through which milk components promote development and immunity has revealed numerous milk-derived compounds with potential applications as clinical therapies in infectious and inflammatory disease, cancer, and other conditions. Lactoferrin is an effective antimicrobial and antiviral agent in high-risk patient populations and a potentially potent adjuvant to chemotherapy in lung cancer. Enteric nutrition formulas supplemented with transforming growth factor β, a milk cytokine, have been shown to promote remission in pediatric Crohn's disease. A number of milk glycans, including human milk oligosaccharides, show promise in preclinical studies as antimicrobial and anti-inflammatory agents. While active preclinical investigations of human milk may soon result in large-scale production of human milk molecules, bovine milk components in many instances represent a practical source of bioactive milk compounds for use in clinical trials. This review summarizes current efforts to translate the compounds derived from human and bovine milk into effective clinical therapies. These efforts suggest a common pathway for the translation of milk-derived compounds into clinical applications.

A monoclonal antibody targeting amyloid β (Aβ) restores complement factor I bioactivity: Potential implications in age-related macular degeneration and Alzheimer's disease.

PubMed

Lashkari, Kameran; Teague, Gianna; Chen, Hong; Lin, Yong-Qing; Kumar, Sanjay; McLaughlin, Megan M; López, Francisco J

2018-01-01

Activation of the alternative complement cascade has been implicated in the pathogenesis of age related macular degeneration (AMD) and Alzheimer's disease (AD). Amyloid β (Aβ), a component of drusen, may promote complement activation by inhibiting CFI bioactivity. We determined whether Aβ reduced CFI bioactivity and whether antibodies against Aβ including a monoclonal antibody, GSK933776 could restore CFI bioactivity. We also measured CFI bioactivity in plasma of subjects with AMD and AD. In support of the GSK933776 development program in AMD (geographic atrophy), we developed a quantitative assay to measure CFI bioactivity based on its ability to cleave C3b to iC3b, and repeated it in presence or absence of Aβ and anti-Aβ antibodies. Using this assay, we measured CFI bioactivity in plasma of 194 subjects with AMD, and in samples from subjects with AD that had been treated with GSK933776 as part of the GSK933776 development program in AD. Aβ reduced the CFI bioactivity by 5-fold and pre-incubation with GSK933776 restored CFI bioactivity. In subjects with AMD, plasma CFI levels and bioactivity were not significantly different from non-AMD controls. However, we detected a positive linear trend, suggesting increasing activity with disease severity. In subjects with AD, we observed a 10% and 27% increase in overall CFI bioactivity after treatment with GSK933776 during the second and third dose. Our studies indicate that CFI enzymatic activity can be inhibited by Aβ and be altered in proinflammatory diseases such as AMD and AD, in which deposition of Aβ and activation of the alternative complement cascade are believed to play a key role in the disease process.

Soy and gut microbiota: interaction and implication for human health

USDA-ARS?s Scientific Manuscript database

Soy (Glycine max) is a major commodity in the U.S. and soy foods are gaining popularity due to its reported health promoting effects. In the past two decades, soy and soy bioactive components have been studied for their health promoting/disease preventing activities and potential mechanism of action...

AMPK activation by pterostilbene contributes to suppression of hepatic gluconeogenic gene expression and glucose production in H4IIE cells

USDA-ARS?s Scientific Manuscript database

Pterostilbene, a bioactive component of blueberries and grapes, shows structural similarity to resveratrol, and exhibits antioxidant, anti-inflammatory, anti-cancer, hypoglycemic, and cholesterol lowering effects. This study examined potential mechanisms that may contribute to its lipid- and glucose...

Component analysis and target cell-based neuroactivity screening of Panax ginseng by ultra-performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry.

PubMed

Yuan, Jinbin; Chen, Yang; Liang, Jian; Wang, Chong-Zhi; Liu, Xiaofei; Yan, Zhihong; Tang, Yi; Li, Jiankang; Yuan, Chun-Su

2016-12-01

Ginseng is one of the most widely used natural medicines in the world. Recent studies have suggested Panax ginseng has a wide range of beneficial effects on aging, central nervous system disorders, and neurodegenerative diseases. However, knowledge about the specific bioactive components of ginseng is still limited. This work aimed to screen for the bioactive components in Panax ginseng that act against neurodegenerative diseases, using the target cell-based bioactivity screening method. Firstly, component analysis of Panax ginseng extracts was performed by UPLC-QTOF-MS, and a total of 54 compounds in white ginseng were characterized and identified according to the retention behaviors, accurate MW, MS characteristics, parent nucleus, aglycones, side chains, and literature data. Then target cell-based bioactivity screening method was developed to predict the candidate compounds in ginseng with SH-SY5Y cells. Four ginsenosides, Rg 2 , Rh 1 , Ro, and Rd, were observed to be active. The target cell-based bioactivity screening method coupled with UPLC-QTOF-MS technique has suitable sensitivity and it can be used as a screening tool for low content bioactive constituents in natural products. Copyright © 2016 Elsevier B.V. All rights reserved.

Effect of different drying techniques on bioactive components, fatty acid composition, and volatile profile of robusta coffee beans.

PubMed

Dong, Wenjiang; Hu, Rongsuo; Chu, Zhong; Zhao, Jianping; Tan, Lehe

2017-11-01

This study investigated the effect of different drying techniques, namely, room-temperature drying (RTD), solar drying (SD), heat-pump drying (HPD), hot-air drying (HAD), and freeze drying (FD), on bioactive components, fatty acid composition, and the volatile compound profile of robusta coffee beans. The data showed that FD was an effective method to preserve fat, organic acids, and monounsaturated fatty acids. In contrast, HAD was ideal for retaining polyunsaturated fatty acids and amino acids. Sixty-two volatile compounds were identified in the differently dried coffee beans, representing 90% of the volatile compounds. HPD of the coffee beans produced the largest number of volatiles, whereas FD resulted in the highest volatile content. A principal component analysis demonstrated a close relationship between the HPD, SD, and RTD methods whereas the FD and HAD methods were significantly different. Overall, the results provide a basis for potential application to other similar thermal sensitive materials. Copyright © 2017 Elsevier Ltd. All rights reserved.

Prospects in the use of aptamers for characterizing the structure and stability of bioactive proteins and peptides in food.

PubMed

Agyei, Dominic; Acquah, Caleb; Tan, Kei Xian; Hii, Hieng Kok; Rajendran, Subin R C K; Udenigwe, Chibuike C; Danquah, Michael K

2018-01-01

Food-derived bioactive proteins and peptides have gained acceptance among researchers, food manufacturers and consumers as health-enhancing functional food components that also serve as natural alternatives for disease prevention and/or management. Bioactivity in food proteins and peptides is determined by their conformations and binding characteristics, which in turn depend on their primary and secondary structures. To maintain their bioactivities, the molecular integrity of bioactive peptides must remain intact, and this warrants the study of peptide form and structure, ideally with robust, highly specific and sensitive techniques. Short single-stranded nucleic acids (i.e. aptamers) are known to have high affinity for cognate targets such as proteins and peptides. Aptamers can be produced cost-effectively and chemically derivatized to increase their stability and shelf life. Their improved binding characteristics and minimal modification of the target molecular signature suggests their suitability for real-time detection of conformational changes in both proteins and peptides. This review discusses the developmental progress of systematic evolution of ligands by exponential enrichment (SELEX), an iterative technology for generating cost-effective aptamers with low dissociation constants (K d ) for monitoring the form and structure of bioactive proteins and peptides. The review also presents case studies of this technique in monitoring the structural stability of bioactive peptide formulations to encourage applications in functional foods. The challenges and potential of aptamers in this research field are also discussed. Graphical abstract Advancing bioactive proteins and peptide functionality via aptameric ligands.

Biomarkers for diet and cancer prevention research: potentials and challenges.

PubMed

Davis, Cindy D; Milner, John A

2007-09-01

As cancer incidence is projected to increase for decades there is a need for effective preventive strategies. Fortunately, evidence continues to mount that altering dietary habits is an effective and cost-efficient approach for reducing cancer risk and for modifying the biological behavior of tumors. Predictive, validated and sensitive biomarkers, including those that reliably evaluate "intake" or exposure to a specific food or bioactive component, that assess one or more specific biological "effects" that are linked to cancer, and that effectively predict individual "susceptibility" as a function of nutrient-nutrient interactions and genetics, are fundamental to evaluating who will benefit most from dietary interventions. These biomarkers must be readily accessible, easily and reliably assayed, and predictive of a key process(es) involved in cancer. The response to a food is determined not only by the effective concentration of the bioactive food component(s) reaching the target tissue, but also by the amount of the target requiring modification. Thus, this threshold response to foods and their components will vary from individual to individual. The key to understanding a personalized response is a greater knowledge of nutrigenomics, proteomics and metabolomics.

Molecular Mechanisms and Pathways as Targets for Cancer Prevention and Progression with Dietary Compounds.

PubMed

Nosrati, Nagisa; Bakovic, Marica; Paliyath, Gopinadhan

2017-09-25

A unique feature of bioactive food ingredients is their broad antioxidant function. Antioxidants having a wide spectrum of chemical structure and activity beyond basic nutrition; display different health benefits by the prevention and progression of chronic diseases. Functional food components are capable of enhancing the natural antioxidant defense system by scavenging reactive oxygen and nitrogen species, protecting and repairing DNA damage, as well as modulating the signal transduction pathways and gene expression. Major pathways affected by bioactive food ingredients include the pro-inflammatory pathways regulated by nuclear factor kappa B (NF-κB), as well as those associated with cytokines and chemokines. The present review summarizes the importance of plant bioactives and their roles in the regulation of inflammatory pathways. Bioactives influence several physiological processes such as gene expression, cell cycle regulation, cell proliferation, cell migration, etc., resulting in cancer prevention. Cancer initiation is associated with changes in metabolic pathways such as glucose metabolism, and the effect of bioactives in normalizing this process has been provided. Initiation and progression of inflammatory bowel diseases (IBD) which increase the chances of developing of colorectal cancers can be downregulated by plant bioactives. Several aspects of the potential roles of microRNAs and epigenetic modifications in the development of cancers have also been presented.

Effect of green tea extract microencapsulation on hypertriglyceridemia and cardiovascular tissues in high fructose-fed rats

PubMed Central

Jung, Moon Hee; Seong, Pil Nam; Kim, Myung Hwan; Myong, Na-Hye

2013-01-01

The application of polyphenols has attracted great interest in the field of functional foods and nutraceuticals due to their potential health benefits in humans. However, the effectiveness of polyphenols depends on their bioactivity and bioavailability. In the present study, the bioactive component from green tea extract (GTE) was administrated orally (50 mg/kg body weight/day) as free or in a microencapsulated form with maltodextrin in rats fed a high fructose diet. High fructose diet induced features of metabolic syndrome including hypertriglyceridemia, hyperuricemia, increased serum total cholesterol, and retroperitoneal obesity. In addition, myocardial fibrosis was increased. In rats receiving high fructose diet, the lowering of blood triglycerides, total cholesterol, non esterified fatty acid (NEFA) and uric acid, as well as the reduction in final body weight and retroperitoneal fat weight associated with the administration of GTE, led to a reversal of the features of metabolic syndrome (P < 0.05). In particular, the administration of microencapsulated GTE decreased myocardial fibrosis and increased liver catalase activity consistent with a further alleviation of serum NEFA, and hyperuricemia compared to administration of GTE. Taken together, our results suggest that microencapsulation of the bioactive components of GTE might have a protective effect on cardiovasucular system by attenuating the adverse features of myocardial fibrosis, decreasing uric acid levels and increasing hepatic catalase activity effectively by protecting their bioactivities. PMID:24133615

Comparative analysis of the main bioactive components of Xin-Sheng-Hua granule and its single herbs by ultrahigh performance liquid chromatography with tandem mass spectrometry.

PubMed

Pang, Hanqing; Wang, Jun; Tang, Yuping; Xu, Huiqin; Wu, Liang; Jin, Yi; Zhu, Zhenhua; Guo, Sheng; Shi, Xuqin; Huang, Shengliang; Sun, Dazheng; Duan, Jin-Ao

2016-11-01

Xin-Sheng-Hua granule, a representative formula for postpartum hemorrhage, has been used clinically to treat postpartum diseases. Its main bioactive components comprise aromatic acids, phthalides, alkaloids, flavonoids, and gingerols among others. To investigate the changes in main bioactive constituents in its seven single herbs before and after compatibility, a rapid, simple, and sensitive method was developed for comparative analysis of 27 main bioactive components by using ultrahigh-performance liquid chromatography with triple quadrupole electrospray tandem mass spectrometry for the first time. The sufficient separation of 27 target constituents was achieved on a Thermo Scientific Hypersil GOLD column (100 mm × 3 mm, 1.9 μm) within 20 min under the optimized chromatographic conditions. Compared with the theoretical content, the observed content of each analyte showed remarkable differences in Xin-Sheng-Hua granule except thymine, p-coumaric acid, senkyunolide I, senkyunolide H, and ligustilide; the total contents of 27 components increased significantly, and the content variation degrees for the different components were gingerols > flavonoids > aromatic acids > alkaloids > phthalides. The results could provide a good reference for the quality control of Xin-Sheng-Hua granule and might be helpful to interpret the drug interactions based on variation of bioactive components in formulae. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Non-targeted metabolite profiling highlights the potential of strawberry leaves as a resource for specific bioactive compounds.

PubMed

Kårlund, Anna; Hanhineva, Kati; Lehtonen, Marko; McDougall, Gordon J; Stewart, Derek; Karjalainen, Reijo O

2017-05-01

The non-edible parts of horticultural crops, such as leaves, contain substantial amounts of valuable bioactive compounds which are currently only little exploited. For example, strawberry (Fragaria × ananassa) leaves may be a promising bioresource for diverse health-related applications. However, product standardization sets a real challenge, especially when the leaf material comes from varying cultivars. The first step towards better quality control of berry fruit leaf-based ingredients and supplements is to understand metabolites present and their stability in different plant cultivars, so this study surveyed the distribution of potentially bioactive strawberry leaf metabolites in six different strawberry cultivars. Non-targeted metabolite profiling analysis using LC/qTOF-ESI-MS with data processing via principal component analysis and k-means clustering analysis was utilized to examine differences and commonalities between the leaf metabolite profiles. Quercetin and kaempferol derivatives were the dominant flavonol groups in strawberry leaves. Previously described and novel caffeic and chlorogenic acid derivatives were among the major phenolic acids. In addition, ellagitannins were one of the distinguishing compound classes in strawberry leaves. In general, strawberry leaves also contained high levels of octadecatrienoic acid derivatives, precursors of valuable odour compounds. The specific bioactive compounds found in the leaves of different strawberry cultivars offer the potential for the selection of optimized leaf materials for added-value food and non-food applications. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

Comparative analyses of seeds of wild fruits of Rubus and Sambucus species from Southern Italy: fatty acid composition of the oil, total phenolic content, antioxidant and anti-inflammatory properties of the methanolic extracts.

PubMed

Fazio, Alessia; Plastina, Pierluigi; Meijerink, Jocelijn; Witkamp, Renger F; Gabriele, Bartolo

2013-10-15

Fruit seeds are byproducts from fruit processing. Characterisation of the bioactive compounds present in seeds and evaluation of their potential biological properties is therefore of particular importance in view of a possible valorisation of seeds as a source of health beneficial components. In this work, we have analysed the seeds of Sambucus and Rubus species in order to identify their bioactive components and to determine the antioxidant and anti-inflammatory activities of the extracts. We first analysed their oil content, in order to assess the fatty acid profile and tocopherol content. Moreover, the methanolic extracts of the seeds were analysed for their total phenolic contents and antioxidant capacities. Polyphenols were identified by HPLC-ESI-MS/MS analysis. Furthermore, extracts were evaluated for their inhibitory effects on the production of LPS-induced inflammatory mediators (NO, CCL-20) in RAW 264.7 cells. Our findings show that the methanolic extracts from Rubus seeds have strong antioxidant and anti-inflammatory properties and could therefore represent an attractive source of bioactive compounds for food, cosmetic, or pharmaceutical applications. Copyright © 2012 Elsevier Ltd. All rights reserved.

Therapeutic polymers for dental adhesives: Loading resins with bio-active components

PubMed Central

Imazato, Satoshi; Ma, Sai; Chen, Ji-hua; Xu, Hockin H.K.

2014-01-01

Objectives Many recent adhesives on the market exhibit reasonable clinical performance. Future innovations in adhesive materials should therefore seek out novel properties rather than simply modifying existing technologies. It is proposed that adhesive materials that are “bio-active” could contribute to better prognosis of restorative treatments. Methods This review examines the recent approaches used to achieve therapeutic polymers for dental adhesives by incorporating bio-active components. A strategy to maintain adhesive restorations is the focus of this paper. Results Major trials on therapeutic dental adhesives have looked at adding antibacterial activities or remineralization effects. Applications of antibacterial resin monomers based on quaternary ammonium compounds have received much research attention, and the loading of nano-sized bioactive particles or multiple ion-releasing glass fillers have been perceived as advantageous since they are not expected to influence the mechanical properties of the carrier polymer. Significance The therapeutic polymer approaches described here have the potential to provide clinical benefits. However, not many technological applications in this category have been successfully commercialized. Clinical evidence as well as further advancement of these technologies can be a driving force to make these new types of materials clinically available. PMID:23899387

Preventive and Prophylactic Mechanisms of Action of Pomegranate Bioactive Constituents

PubMed Central

Viladomiu, Monica; Hontecillas, Raquel; Lu, Pinyi; Bassaganya-Riera, Josep

2013-01-01

Pomegranate fruit presents strong anti-inflammatory, antioxidant, antiobesity, and antitumoral properties, thus leading to an increased popularity as a functional food and nutraceutical source since ancient times. It can be divided into three parts: seeds, peel, and juice, all of which seem to have medicinal benefits. Several studies investigate its bioactive components as a means to associate them with a specific beneficial effect and develop future products and therapeutic applications. Many beneficial effects are related to the presence of ellagic acid, ellagitannins (including punicalagins), punicic acid and other fatty acids, flavonoids, anthocyanidins, anthocyanins, estrogenic flavonols, and flavones, which seem to be its most therapeutically beneficial components. However, the synergistic action of the pomegranate constituents appears to be superior when compared to individual constituents. Promising results have been obtained for the treatment of certain diseases including obesity, insulin resistance, intestinal inflammation, and cancer. Although moderate consumption of pomegranate does not result in adverse effects, future studies are needed to assess safety and potential interactions with drugs that may alter the bioavailability of bioactive constituents of pomegranate as well as drugs. The aim of this review is to summarize the health effects and mechanisms of action of pomegranate extracts in chronic inflammatory diseases. PMID:23737845

Isolation of bioactive allelochemicals from sunflower (variety Suncross-42) through fractionation-guided bioassays.

PubMed

Anjum, Tehmina; Bajwa, Rukhsana

2010-11-01

Plants are rich source of biologically active allelochemicals. However, natural product discovery is not an easy task. Many problems encountered during this laborious practice can be overcome through the modification of preliminary trials. Bioassay-directed isolation of active plant compounds can increase efficiency by eliminating many of the problems encountered. This strategy avoids unnecessary compounds, concentrating on potential components and thus reducing the cost and time required. In this study, a crude aqueous extract of sunflower leaves was fractionated through high performance liquid chromatography. The isolated fractions were checked against Chenopodium album and Rumex dentatus. The fraction found active against two selected weeds was re-fractionated, and the active components were checked for their composition. Thin layer chromatography isolated a range of phenolics, whereas the presence of bioactive terpenoids was confirmed through mass spectroscopy and nuclear magnetic resonance spectroscopy.

Sodium Is Not Essential for High Bioactivity of Glasses

PubMed Central

Chen, Xiaojing; Chen, Xiaohui; Brauer, Delia S.; Wilson, Rory M.; Law, Robert V.; Hill, Robert G.; Karpukhina, Natalia

2017-01-01

This study aims to demonstrate that excellent bioactivity of glass can be achieved without the presence of an alkali metal component in glass composition. In vitro bioactivity of two sodium-free glasses based on the quaternary system SiO2-P2O5-CaO-CaF2 with 0 and 4.5 mol% CaF2 content was investigated and compared with the sodium containing glasses with equivalent amount of CaF2. The formation of apatite after immersion in Tris buffer was followed by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), 31P and 19F solid state MAS-NMR. The dissolution study was completed by ion release measurements in Tris buffer. The results show that sodium free bioactive glasses formed apatite at 3 hours of immersion in Tris buffer, which is as fast as the corresponding sodium containing composition. This signifies that sodium is not an essential component in bioactive glasses and it is possible to make equally degradable bioactive glasses with or without sodium. The results presented here also emphasize the central role of the glass compositions design which is based on understanding of structural role of components and/or predicting the network connectivity of glasses. PMID:29271977

Sodium Is Not Essential for High Bioactivity of Glasses.

PubMed

Chen, Xiaojing; Chen, Xiaohui; Brauer, Delia S; Wilson, Rory M; Law, Robert V; Hill, Robert G; Karpukhina, Natalia

2017-12-01

This study aims to demonstrate that excellent bioactivity of glass can be achieved without the presence of an alkali metal component in glass composition. In vitro bioactivity of two sodium-free glasses based on the quaternary system SiO 2 -P 2 O 5 -CaO-CaF 2 with 0 and 4.5 mol% CaF 2 content was investigated and compared with the sodium containing glasses with equivalent amount of CaF 2 . The formation of apatite after immersion in Tris buffer was followed by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), 31 P and 19 F solid state MAS-NMR. The dissolution study was completed by ion release measurements in Tris buffer. The results show that sodium free bioactive glasses formed apatite at 3 hours of immersion in Tris buffer, which is as fast as the corresponding sodium containing composition. This signifies that sodium is not an essential component in bioactive glasses and it is possible to make equally degradable bioactive glasses with or without sodium. The results presented here also emphasize the central role of the glass compositions design which is based on understanding of structural role of components and/or predicting the network connectivity of glasses.

Bioactive compounds of sea cucumbers and their therapeutic effects

NASA Astrophysics Data System (ADS)

Shi, Shujuan; Feng, Wenjing; Hu, Song; Liang, Shixiu; An, Nina; Mao, Yongjun

2016-05-01

Sea cucumbers belong to the Class Holothuroidea of marine invertebrates. They are commercially valuable and prized as a food and folk medicine in Asia. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as vitamins, minerals and amino acids. A number of unique biological and pharmacological activities/properties, including anticancer, anticoagulant/antithrombotic, antimicrobial, antioxidant, antihyperlipidemic, antihyperglycemic, anti-inflammatory, antihypertension and radioprotective, have been ascribed to various compounds isolated from sea cucumbers. The therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array of bioactives, especially triterpene glycosides, acid mucopolysaccharide, sphingoid bases, glycolipids, fucosylated chondroitin sulfate, polysaccharides, phospholipids, cerebrosides, phosphatidylcholines, and other extracts and hydrolysates. This review highlights the valuable bioactive components as well as the multiple therapeutic properties of sea cucumbers with a view to exploring their potential uses as functional foods and a natural source of new multifunctional drugs.

Neem components as potential agents for cancer prevention and treatment

PubMed Central

Hao, Fang; Kumar, Sandeep; Yadav, Neelu; Chandra, Dhyan

2016-01-01

Azadirachta indica, also known as neem, is commonly found in many semi-tropical and tropical countries including India, Pakistan, and Bangladesh. The components extracted from neem plant have been used in traditional medicine for the cure of multiple diseases including cancer for centuries. The extracts of seeds, leaves, flowers, and fruits of neem have consistently shown chemopreventive and antitumor effects in different types of cancer. Azadirachtin and nimbolide are among the few bioactive components in neem that have been studied extensively, but research on a great number of additional bioactive components is warranted. The key anticancer effects of neem components on malignant cells include inhibition of cell proliferation, induction of cell death, suppression of cancer angiogenesis, restoration of cellular reduction/oxidation (redox) balance, and enhancement of the host immune responses against tumor cells. While the underlying mechanisms of these effects are mostly unclear, the suppression of NF-κB signaling pathway is, at least partially, involved in the anticancer functions of neem components. Importantly, the anti-proliferative and apoptosis-inducing effects of neem components are tumor selective as the effects on normal cells are significantly weaker. In addition, neem extracts sensitize cancer cells to immunotherapy and radiotherapy, and enhance the efficacy of certain cancer chemotherapeutic agents. This review summarizes the current updates on the anticancer effects of neem components and their possible impact on managing cancer incidence and treatment. PMID:25016141

Mushrooms: A Potential Natural Source of Anti-Inflammatory Compounds for Medical Applications

PubMed Central

Elsayed, Elsayed A.; El Enshasy, Hesham; Wadaan, Mohammad A. M.; Aziz, Ramlan

2014-01-01

For centuries, macrofungi have been used as food and medicine in different parts of the world. This is mainly attributed to their nutritional value as a potential source of carbohydrates, proteins, amino acids, and minerals. In addition, they also include many bioactive metabolites which make mushrooms and truffles common components in folk medicine, especially in Africa, the Middle East, China, and Japan. The reported medicinal effects of mushrooms include anti-inflammatory effects, with anti-inflammatory compounds of mushrooms comprising a highly diversified group in terms of their chemical structure. They include polysaccharides, terpenoids, phenolic compounds, and many other low molecular weight molecules. The aims of this review are to report the different types of bioactive metabolites and their relevant producers, as well as the different mechanisms of action of mushroom compounds as potent anti-inflammatory agents. PMID:25505823

[Multiple emulsions; bioactive compounds and functional foods].

PubMed

Jiménez-Colmenero, Francisco

2013-01-01

The continued appearance of scientific evidence about the role of diet and/or its components in health and wellness, has favored the emergence of functional foods which currently constitute one of the chief factors driving the development of new products. The application of multiple emulsions opens new possibilities in the design and development of functional foods. Multiple emulsions can be used as an intermediate product (food ingredient) into technological strategies normally used in the optimization of the presence of bioactive compounds in healthy and functional foods. This paper presents a summary of the types, characteristics and formation of multiple emulsions, possible location of bioactive compounds and their potential application in the design and preparation of healthy and functional foods. Such applications are manifested particularly relevant in relation to quantitative and qualitative aspects of lipid material (reduced fat/calories and optimization of fatty acid profile), encapsulation of bioactive compounds mainly hydrophilic and sodium reduction. This strategy offers interesting possibilities regarding masking flavours and improving sensory characteristics of foods. Copyright © AULA MEDICA EDICIONES 2013. Published by AULA MEDICA. All rights reserved.

Multi-layer porous fiber-reinforced composites for implants: in vitro calcium phosphate formation in the presence of bioactive glass.

PubMed

Nganga, Sara; Zhang, Di; Moritz, Niko; Vallittu, Pekka K; Hupa, Leena

2012-11-01

Glass-fiber-reinforced composites (FRCs), based on bifunctional methacrylate resin, have recently shown their potential for use as durable cranioplasty, orthopedic and oral implants. In this study we suggest a multi-component sandwich implant structure with (i) outer layers out of porous FRC, which interface the cortical bone, and (ii) inner layers encompassing bioactive glass granules, which interface with the cancellous bone. The capability of Bioglass(®) 45S5 granules (100-250μm) to induce calcium phosphate formation on the surface of the FRC was explored by immersing the porous FRC-Bioglass laminates in simulated body fluid (SBF) for up to 28d. In both static (agitated) and dynamic conditions, bioactive glass granules induced precipitation of calcium phosphate at the laminate surfaces as confirmed by scanning electron microscopy. The proposed dynamic flow system is useful for the in vitro simulation of bone-like apatite formation on various new porous implant designs containing bioactive glass and implant material degradation. Copyright © 2012 Academy of Dental Materials. Published by Elsevier Ltd. All rights reserved.

Establishing health benefits of bioactive food components: a basic research scientist's perspective

USDA-ARS?s Scientific Manuscript database

Bioactive food components or functional foods have recently received significant attention because of their widely touted positive effects beyond basic nutrition. However, a question continues to lurk: are these 'super foods' backed by sound science or simply an exaggerated portrayal of very small '...

Large-scale randomized clinical trials of bioactives and nutrients in relation to human health and disease prevention - Lessons from the VITAL and COSMOS trials.

PubMed

Rautiainen, Susanne; Sesso, Howard D; Manson, JoAnn E

2017-12-29

Several bioactive compounds and nutrients in foods have physiological properties that are beneficial for human health. While nutrients typically have clear definitions with established levels of recommended intakes, bioactive compounds often lack such a definition. Although a food-based approach is often the optimal approach to ensure adequate intake of bioactives and nutrients, these components are also often produced as dietary supplements. However, many of these supplements are not sufficiently studied and have an unclear role in chronic disease prevention. Randomized trials are considered the gold standard of study designs, but have not been fully applied to understand the effects of bioactives and nutrients. We review the specific role of large-scale trials to test whether bioactives and nutrients have an effect on health outcomes through several crucial components of trial design, including selection of intervention, recruitment, compliance, outcome selection, and interpretation and generalizability of study findings. We will discuss these components in the context of two randomized clinical trials, the VITamin D and OmegA-3 TriaL (VITAL) and the COcoa Supplement and Multivitamin Outcomes Study (COSMOS). We will mainly focus on dietary supplements of bioactives and nutrients while also emphasizing the need for translation and integration with food-based trials that are of vital importance within nutritional research. Copyright © 2017. Published by Elsevier Ltd.

[Screening of anti-lung cancer bioactive compounds from Curcuma longa by target cell extraction and UHPLC/LTQ Orbitrap MS].

PubMed

Zhou, Jian-Liang; Wu, Ye-Qing; Tan, Chun-Mei; Zhu, Ming; Ma, Lin-Ke

2016-10-01

A target cell extraction-chemical profiling method based on human alveolar adenocarcinoma cell line (A549 cells) and UHPLC/LTQ Orbitrap MS for screening the anti-lung cancer bioactive compounds from Curcuma longa has been developed in this paper. According to the hypothesis that when cells are incubated together with the extract of Curcuma longa, the potential bioactive compounds in the extract should selectively combine with the cells, then the cell-binding compounds could be separated and analyzed by LC-MS. The bioactive compounds in C. longa are lipophilic components. They intend to be absorbed on the inner wall of cell culture flask when they were incubated with A549 cells, which will produce interference in the blank solution. In this paper, by using cells digestion and multi-step centrifugation and transfer strategy, the interference problem has been solved. Finally, using the developed method, three cell-binding compounds were screened out and were identified as bisdemethoxycurcumin, demethoxycurcumin, and curcumin. These compounds are the main bioactive compounds with anti-lung cancer bioactivity in C. longa. The improved method developed in this paper could avoid the false positive results due to the absorption of lipophilic compounds on the inner wall of cell culture flask, which will to be an effective complementary method for current target cell extraction-chemical profiling technology. Copyright© by the Chinese Pharmaceutical Association.

[Nutrigenomics--bioactive dietary components].

PubMed

Gętek, Monika; Czech, Natalia; Fizia, Katarzyna; Białek-Dratwa, Agnieszka; Muc-Wierzgoń, Małgorzata; Kokot, Teresa; Nowakowska-Zajdel, Ewa

2013-04-05

Nutrigenomics analyzes relations between diet and genes, and identifies mechanisms in which food and nutrition affect health and lifestyles and noncommunicable diseases (R. Chadwick, 2004). Bioactive dietary components are signal molecules that carry information from the external environment and affect in terms of quantity and quality in the process of gene expression. The biological effect of bioactive dietary components depends on various of physiological processes that can occur within a few genes. Polymorphism of genes can change their function and physiological response of the body for nutrients. Bioactive dietary components work on at least two levels of the expression of genes as factors regulating chromatin structure and as factors directly regulate the activity of nuclear receptors. The processes of synthesis and DNA repair are regulated by some of vitamins, macro-and micro-elements. They provide, among others, cofactors of enzymes that catalyze the replication of DNA methylation and its repair. DNA methylation profile may change under the influence of diet, single nucleotide polymorphisms and environmental factors. Bioactive dietary components may directly affect the process of gene expression by acting as ligands for nuclear receptors. Sensitive to dietary group of nuclear receptors are sensory receptors. This group includes, among others receptor PPAR (peroxisome proliferator activated), responsible for energy metabolism and receptors LXR (liver X receptor), FXR (farnesoid X receptor) and RXR, which is responsible for the metabolism of cholesterol.

Relationship of Mycotoxins Accumulation and Bioactive Components Variation in Ginger after Fungal Inoculation.

PubMed

Yang, Zhixin; Wang, Haiwei; Ying, Guangyao; Yang, Meihua; Nian, Yujiao; Liu, Jiajia; Kong, Weijun

2017-01-01

Ginger has got increasing worldwide interests due to its extensive biological activities, along with high medical and edible values. But fungal contamination and mycotoxin residues have brought challenges to its quality and safety. In the present study, the relationship of content of mycotoxins accumulation and bioactive components variation in ginger after infection by toxigenic fungi were investigated for the first time to elucidate the influence of fungal contamination on the inherent quality of ginger. After being infected by Aspergillus flavus and Aspergillus carbonarius for different periods, the produced mycotoxins was determined by an immunoaffinity column clean-up based ultra-fast liquid chromatography coupled with tandem mass spectrometry, and the main bioactive components in ginger were analyzed by ultra performance liquid chromatography-photodiode array detection. The results showed that consecutive incubation of ginger with A. flavus and A. carbonarius within 20 days resulted in the production and accumulation of aflatoxins (especially AFB 1 ) and ochratoxin A, as well as the constant content reduction of four bioactive components, which were confirmed through the scanning electron microscope images. Significantly negative correlation was expressed between the mycotoxins accumulation and bioactive components variation in ginger, which might influence the quality and safety of it. Furthermore, a new compound was detected after inoculation for 6 days, which was found in our study for the first time.

Correlations between chromatographic parameters and bioactivity predictors of potential herbicides.

PubMed

Janicka, Małgorzata

2014-08-01

Different liquid chromatography techniques, including reversed-phase liquid chromatography on Purosphere RP-18e, IAM.PC.DD2 and Cosmosil Cholester columns and micellar liqud chromatography with a Purosphere RP-8e column and using buffered sodium dodecyl sulfate-acetonitrile as the mobile phase, were applied to study the lipophilic properties of 15 newly synthesized phenoxyacetic and carbamic acid derivatives, which are potential herbicides. Chromatographic lipophilicity descriptors were used to extrapolate log k parameters (log kw and log km) and log k values. Partitioning lipophilicity descriptors, i.e., log P coefficients in an n-octanol-water system, were computed from the molecular structures of the tested compounds. Bioactivity descriptors, including partition coefficients in a water-plant cuticle system and water-human serum albumin and coefficients for human skin partition and permeation were calculated in silico by ACD/ADME software using the linear solvation energy relationship of Abraham. Principal component analysis was applied to describe similarities between various chromatographic and partitioning lipophilicities. Highly significant, predictive linear relationships were found between chromatographic parameters and bioactivity descriptors. © The Author [2013]. Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Antioxidant activity of raw, cooked and Rhizopus oligosporus fermented beans of Canavalia of coastal sand dunes of Southwest India.

PubMed

Niveditha, Vedavyas R; Sridhar, Kandikere R

2014-11-01

The raw and processed (cooked and cooked + solid-state fermented with Rhizopus oligosporus) split beans of two landraces of coastal sand dune wild legumes (Canavalia cathartica and Canavalia maritima) of the southwest coast of India were examined for bioactive compounds (total phenolics, tannins and vitamin C) and antioxidant potential (total antioxidant activity, ferrous-ion chelating capacity, DPPH free radical-scavenging activity and reducing activity). One-way ANOVA revealed significant elevation of bioactive compounds as well as antioxidant activities in fermented beans compared to raw and cooked beans in both legumes (p < 0.001). The EC50 values in fermented beans of both legumes were significantly lowest compared to raw and cooked beans (p < 0.001). In principal component analysis, total phenolics along with antioxidant activities (total antioxidant, ferrous-ion chelating and free radical-scavenging activities) of fermented beans of C. cathartica, while total antioxidant and free radical-scavenging activities of fermented beans of C. maritima were clustered. The present study demonstrated that split beans of coastal sand dune Canavalia fermented by R. oligosporus endowed with high bioactive principles as well as antioxidant potential and thus serve as future nutraceutical source.

Garlic and onions: Their cancer prevention properties

PubMed Central

Nicastro, Holly L.; Ross, Sharon A.; Milner, John A.

2015-01-01

The Allium genus includes garlic, onions, shallots, leeks, and chives. These vegetables are popular in cuisines worldwide and are valued for their potential medicinal properties. Epidemiological studies, while limited in their abilities to assess Allium consumption, indicate some associations of Allium vegetable consumption with decreased risk of cancer, particularly cancers of the gastrointestinal tract. Limited intervention studies have been conducted to support these associations. The majority of supportive evidence on Allium vegetables cancer preventive effects comes from mechanistic studies. These studies highlight potential mechanisms of individual sulfur-containing compounds and of various preparations and extracts of these vegetables, including decreased bioactivation of carcinogens, antimicrobial activities, and redox modification. Allium vegetables and their components have effects at each stage of carcinogenesis and affect many biological processes that modify cancer risk. This review discusses the cancer preventive effects of Allium vegetables, particularly garlic and onions, and their bioactive sulfur compounds and highlights research gaps. PMID:25586902

Implications of bioactive solute transfer from hosts to parasitic plants.

PubMed

Smith, Jason D; Mescher, Mark C; De Moraes, Consuelo M

2013-08-01

Parasitic plants--which make their living by extracting nutrients and other resources from other plants--are important components of many natural ecosystems; and some parasitic species are also devastating agricultural pests. To date, most research on plant parasitism has focused on nutrient transfer from host to parasite and the impacts of parasites on host plants. Far less work has addressed potential effects of the translocation of bioactive non-nutrient solutes-such as phytohormones, secondary metabolites, RNAs, and proteins-on the development and physiology of parasitic plants and on their subsequent interactions with other organisms such as insect herbivores. A growing number of recent studies document the transfer of such molecules from hosts to parasites and suggest that they may have significant impacts on parasite physiology and ecology. We review this literature and discuss potential implications for management and priorities for future research. Copyright © 2013 Elsevier Ltd. All rights reserved.

Cancer control and prevention: nutrition and epigenetics.

PubMed

Verma, Mukesh

2013-07-01

To evaluate recent developments in nutritional epigenomics and related challenges, opportunities, and implications for cancer control and prevention. Cancer is one of the leading causes of death worldwide, and understanding the factors that contribute to cancer development may facilitate the development of strategies for cancer prevention and control. Cancer development involves genetic and epigenetic alterations. Genetic marks are permanent, whereas epigenetic marks are dynamic, change with age, and are influenced by the external environment. Thus, epigenetics provides a link between the environment, diet, and cancer development. Proper food selection is imperative for better health and to avoid cancer and other diseases. Nutrients either contribute directly to cancer prevention or support the repair of genomic and epigenomic damage caused by exposure to cancer-causing agents such as toxins, free radicals, radiation, and infectious agents. Nutritional epigenomics provides an opportunity for cancer prevention because selected nutrients have the potential to reverse cancer-associated epigenetic marks in different tumor types. A number of natural foods and their bioactive components have been shown to have methylation-inhibitory and deacetylation-inhibitory properties. Natural foods and bioactive food components have characteristics and functions that are similar to epigenetic inhibitors and therefore have potential in cancer control and prevention.

High-value components and bioactives from sea cucumbers for functional foods--a review.

PubMed

Bordbar, Sara; Anwar, Farooq; Saari, Nazamid

2011-01-01

Sea cucumbers, belonging to the class Holothuroidea, are marine invertebrates, habitually found in the benthic areas and deep seas across the world. They have high commercial value coupled with increasing global production and trade. Sea cucumbers, informally named as bêche-de-mer, or gamat, have long been used for food and folk medicine in the communities of Asia and Middle East. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as Vitamin A, Vitamin B1 (thiamine), Vitamin B2 (riboflavin), Vitamin B3 (niacin), and minerals, especially calcium, magnesium, iron and zinc. A number of unique biological and pharmacological activities including anti-angiogenic, anticancer, anticoagulant, anti-hypertension, anti-inflammatory, antimicrobial, antioxidant, antithrombotic, antitumor and wound healing have been ascribed to various species of sea cucumbers. Therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array of bioactives especially triterpene glycosides (saponins), chondroitin sulfates, glycosaminoglycan (GAGs), sulfated polysaccharides, sterols (glycosides and sulfates), phenolics, cerberosides, lectins, peptides, glycoprotein, glycosphingolipids and essential fatty acids. This review is mainly designed to cover the high-value components and bioactives as well as the multiple biological and therapeutic properties of sea cucumbers with regard to exploring their potential uses for functional foods and nutraceuticals.

High-Value Components and Bioactives from Sea Cucumbers for Functional Foods—A Review

PubMed Central

Bordbar, Sara; Anwar, Farooq; Saari, Nazamid

2011-01-01

Sea cucumbers, belonging to the class Holothuroidea, are marine invertebrates, habitually found in the benthic areas and deep seas across the world. They have high commercial value coupled with increasing global production and trade. Sea cucumbers, informally named as bêche-de-mer, or gamat, have long been used for food and folk medicine in the communities of Asia and Middle East. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as Vitamin A, Vitamin B1 (thiamine), Vitamin B2 (riboflavin), Vitamin B3 (niacin), and minerals, especially calcium, magnesium, iron and zinc. A number of unique biological and pharmacological activities including anti-angiogenic, anticancer, anticoagulant, anti-hypertension, anti-inflammatory, antimicrobial, antioxidant, antithrombotic, antitumor and wound healing have been ascribed to various species of sea cucumbers. Therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array of bioactives especially triterpene glycosides (saponins), chondroitin sulfates, glycosaminoglycan (GAGs), sulfated polysaccharides, sterols (glycosides and sulfates), phenolics, cerberosides, lectins, peptides, glycoprotein, glycosphingolipids and essential fatty acids. This review is mainly designed to cover the high-value components and bioactives as well as the multiple biological and therapeutic properties of sea cucumbers with regard to exploring their potential uses for functional foods and nutraceuticals. PMID:22072996

Overview of the anti-inflammatory effects, pharmacokinetic properties and clinical efficacies of arctigenin and arctiin from Arctium lappa L.

PubMed

Gao, Qiong; Yang, Mengbi; Zuo, Zhong

2018-05-01

Arctigenin (AR) and its glycoside, arctiin, are two major active ingredients of Arctium lappa L (A lappa), a popular medicinal herb and health supplement frequently used in Asia. In the past several decades, bioactive components from A lappa have attracted the attention of researchers due to their promising therapeutic effects. In the current article, we aimed to provide an overview of the pharmacology of AR and arctiin, focusing on their anti-inflammatory effects, pharmacokinetics properties and clinical efficacies. Compared to acrtiin, AR was reported as the most potent bioactive component of A lappa in the majority of studies. AR exhibits potent anti-inflammatory activities by inhibiting inducible nitric oxide synthase (iNOS) via modulation of several cytokines. Due to its potent anti-inflammatory effects, AR may serve as a potential therapeutic compound against both acute inflammation and various chronic diseases. However, pharmacokinetic studies demonstrated the extensive glucuronidation and hydrolysis of AR in liver, intestine and plasma, which might hinder its in vivo and clinical efficacy after oral administration. Based on the reviewed pharmacological and pharmacokinetic characteristics of AR, further pharmacokinetic and pharmacodynamic studies of AR via alternative administration routes are suggested to promote its ability to serve as a therapeutic agent as well as an ideal bioactive marker for A lappa.

Bioactive Food Components, Inflammatory Targets, and Cancer Prevention

PubMed Central

Kim, Young S.; Young, Matthew R.; Bobe, Gerd; Colburn, Nancy H.; Milner, John A.

2012-01-01

Various dietary components may modify chronic inflammatory processes at the stage of cytokine production, amplification of nuclear factor-κB–mediated inflammatory gene expression, and the release of anti-inflammatory cytokine, transforming growth factor-β. This review provides a synopsis of the strengths and weaknesses of the evidence that specific bioactive food components influence inflammation-related targets linked to cancer. A target repeatedly surfacing as a site of action for several dietary components is transforming growth factor β. Whereas the use of dietary intervention strategies offers intriguing possibilities for maintaining normal cell function by modifying a process that is essential for cancer development and progression, more information is needed to characterize the minimum quantity of the bioactive food components required to bring about a change in inflammation-mediated cancer, the ideal time for intervention, and the importance of genetics in determining the response. Unquestionably, the societal benefits of using foods and their components to prevent chronic inflammation and associated complications, including cancer, are enormous. PMID:19258539

Evaluation of Ginger (Zingiber officinale Roscoe) Bioactive Compounds in Increasing the Ratio of T-cell Surface Molecules of CD3+CD4+:CD3+CD8+ In-Vitro.

PubMed

Tejasari, Dr

2007-09-01

The potential ability of ginger bioactive compounds in increasing the ratio of T-cell surface molecules of CD3+CD4+:CD3+CD8+ was investigated using dual tagging FITC and PE of monoclonal antibody anti-human with its fluorescence measured by flow cytometer. Oleoresin was extracted using sinkhole distillation technique. Its components namely, gingerol in fraction-1, shogaol in fraction 2 and zingeron in fraction-3 were separated by column vacuum chromatography method. The doses of oleoresin, gingerol, shogaol, and zingeron tested were 50, 100,150, 200, and 250 μg/ml. Lymphocytes (2x106 cell/ml) from human peripheral blood were isolated using ficoll density gradient technique, and cultured in the presence of the compounds in RPMI-1640 medium and phytohemaglutinin (PHA) mitogen for 96 h under normal conditions. Percentages of T-cell surface molecules (CD4+ and CD8+) were determined using dual-tagging FITC and PE fluorescents labeled on monoclonal antibody anti human. The fluorescence-labeled bands on the T-cell surface molecules were counted using flow cytometer. The experiment revealed that oleoresin and its three fractions increased the percentage of CD3+CD4+. The compound in fraction 3 of oleoresin at 200 μg/ml increased by the highest percentage of CD3+CD4+ of 9%, but slightly decreased the percentage of CD3+CD8+. These ginger bioactive compounds increased the ratio of CD3+CD4:CD3+CD8+ T-cells with the highest increment of 30% from effects of 200 μg/ml fraction 3 of oleoresin. This in vitro finding revealed that ginger bioactive compounds potentially increased cellular and humoral immune response. Further clinical studies are needed to confirm the benefits of these ginger bioactive compounds as a potential functional food for testing on HIV infected patients.

Natural products and biological activity of the pharmacologically active cauliflower mushroom Sparassis crispa.

PubMed

Kimura, Takashi

2013-01-01

Sparassis crispa, also known as cauliflower mushroom, is an edible mushroom with medicinal properties. Its cultivation became popular in Japan about 10 years ago, a phenomenon that has been attributed not only to the quality of its taste, but also to its potential for therapeutic applications. Herein, I present a comprehensive summary of the pharmacological activities and mechanisms of action of its bioactive components, such as beta-glucan, and other physiologically active substances. In particular, the immunomodulatory mechanisms of the beta-glucan components are presented herein in detail.

An effective vacuum assisted extraction method for the optimization of labdane diterpenoids from Andrographis paniculata by response surface methodology.

PubMed

Wang, Ya-Qi; Wu, Zhen-Feng; Ke, Gang; Yang, Ming

2014-12-31

An effective vacuum assisted extraction (VAE) technique was proposed for the first time and applied to extract bioactive components from Andrographis paniculata. The process was carefully optimized by response surface methodology (RSM). Under the optimized experimental conditions, the best results were obtained using a boiling temperature of 65 °C, 50% ethanol concentration, 16 min of extraction time, one extraction cycles and a 12:1 liquid-solid ratio. Compared with conventional ultrasonic assisted extraction and heat reflux extraction, the VAE technique gave shorter extraction times and remarkable higher extraction efficiency, which indicated that a certain degree of vacuum gave the solvent a better penetration of the solvent into the pores and between the matrix particles, and enhanced the process of mass transfer. The present results demonstrated that VAE is an efficient, simple and fast method for extracting bioactive components from A. paniculata, which shows great potential for becoming an alternative technique for industrial scale-up applications.

Effects of Vegetables on Cardiovascular Diseases and Related Mechanisms

PubMed Central

Tang, Guo-Yi; Meng, Xiao; Li, Ya; Zhao, Cai-Ning; Liu, Qing

2017-01-01

Epidemiological studies have shown that vegetable consumption is inversely related to the risk of cardiovascular diseases. Moreover, research has indicated that many vegetables like potatoes, soybeans, sesame, tomatoes, dioscorea, onions, celery, broccoli, lettuce and asparagus showed great potential in preventing and treating cardiovascular diseases, and vitamins, essential elements, dietary fibers, botanic proteins and phytochemicals were bioactive components. The cardioprotective effects of vegetables might involve antioxidation; anti-inflammation; anti-platelet; regulating blood pressure, blood glucose, and lipid profile; attenuating myocardial damage; and modulating relevant enzyme activities, gene expression, and signaling pathways as well as some other biomarkers associated to cardiovascular diseases. In addition, several vegetables and their bioactive components have been proven to protect against cardiovascular diseases in clinical trials. In this review, we analyze and summarize the effects of vegetables on cardiovascular diseases based on epidemiological studies, experimental research, and clinical trials, which are significant to the application of vegetables in prevention and treatment of cardiovascular diseases. PMID:28796173

Adhesive Bioactive Coatings Inspired by Sea Life.

PubMed

Rego, Sónia J; Vale, Ana C; Luz, Gisela M; Mano, João F; Alves, Natália M

2016-01-19

Inspired by nature, in particular by the marine mussels adhesive proteins (MAPs) and by the tough brick-and-mortar nacre-like structure, novel multilayered films are prepared in the present work. Organic-inorganic multilayered films, with an architecture similar to nacre based on bioactive glass nanoparticles (BG), chitosan, and hyaluronic acid modified with catechol groups, which are the main components responsible for the outstanding adhesion in MAPs, are developed for the first time. The biomimetic conjugate is prepared by carbodiimide chemistry and analyzed by ultraviolet-visible spectrophotometry. The buildup of the multilayered films is monitored with a quartz crystal microbalance with dissipation monitoring, and their topography is characterized by atomic force microscopy. The mechanical properties reveal that the films containing catechol groups and BG present an enhanced adhesion. Moreover, the bioactivity of the films upon immersion in a simulated body fluid solution is evaluated by scanning electron microscopy coupled with energy dispersive X-ray spectroscopy, Fourier transform infrared spectroscopy, and X-ray diffraction. It was found that the constructed films promote the formation of bonelike apatite in vitro. Such multifunctional mussel inspired LbL films, which combine enhanced adhesion and bioactivity, could be potentially used as coatings of a variety of implants for orthopedic applications.

Discovery of Bioactive Metabolites in Biofuel Microalgae That Offer Protection against Predatory Bacteria

PubMed Central

Bagwell, Christopher E.; Abernathy, Amanda; Barnwell, Remy; Milliken, Charles E.; Noble, Peter A.; Dale, Taraka; Beauchesne, Kevin R.; Moeller, Peter D. R.

2016-01-01

Microalgae could become an important resource for addressing increasing global demand for food, energy, and commodities while helping to reduce atmospheric greenhouse gasses. Even though Chlorophytes are generally regarded safe for human consumption, there is still much we do not understand about the metabolic and biochemical potential of microscopic algae. The aim of this study was to evaluate biofuel candidate strains of Chlorella and Scenedesmus for the potential to produce bioactive metabolites when grown under nutrient depletion regimes intended to stimulate production of triacylglycerides. Strain specific combinations of macro- and micro-nutrient restricted growth media did stimulate neutral lipid accumulation by microalgal cultures. However, cultures that were restricted for iron consistently and reliably tested positive for cytotoxicity by in vivo bioassays. The addition of iron back to these cultures resulted in the disappearance of the bioactive components by LC/MS fingerprinting and loss of cytotoxicity by in vivo bioassay. Incomplete NMR characterization of the most abundant cytotoxic fractions suggested that small molecular weight peptides and glycosides could be responsible for Chlorella cytotoxicity. Experiments were conducted to determine if the bioactive metabolites induced by Fe-limitation in Chlorella sp. cultures would elicit protection against Vampirovibrio chlorellavorus, an obligate predator of Chlorella. Introduction of V. chlorellavorus resulted in a 72% decrease in algal biomass in the experimental controls after 7 days. Conversely, only slight losses of algal biomass were measured for the iron limited Chlorella cultures (0–9%). This study demonstrates a causal linkage between iron bioavailability and bioactive metabolite production in strains of Chlorella and Scenedesmus. Further study of this phenomenon could contribute to the development of new strategies to extend algal production cycles in open, outdoor systems while ensuring the protection of biomass from predatory losses. PMID:27148205

Metabolomic-Guided Isolation of Bioactive Natural Products from Curvularia sp., an Endophytic Fungus of Terminalia laxiflora.

PubMed

Tawfike, Ahmed F; Abbott, Grainne; Young, Louise; Edrada-Ebel, RuAngelie

2018-02-01

Endophytic fungi associated with medicinal plants are a potential source of novel chemistry and biology. Metabolomic tools were successfully employed to compare the metabolite fingerprints of solid and liquid culture extracts of endophyte Curvularia sp. isolated from the leaves of Terminalia laxiflora . Natural product databases were used to dereplicate metabolites in order to determine known compounds and the presence of new natural products. Multivariate analysis highlighted the putative metabolites responsible for the bioactivity of the fungal extract and its fractions on NF- κ B and the myelogenous leukemia cell line K562. Metabolomic tools and dereplication studies using high-resolution electrospray ionization mass spectrometry directed the fractionation and isolation of the bioactive components from the fungal extracts. This resulted in the isolation of N -acetylphenylalanine (1: ) and two linear peptide congeners of 1: : dipeptide N -acetylphenylalanyl-L-phenylalanine (2: ) and tripeptide N -acetylphenylalanyl-L-phenylalanyl-L-leucine (3: ). Georg Thieme Verlag KG Stuttgart · New York.

D-Optimal mixture experimental design for stealth biodegradable crosslinked docetaxel-loaded poly-ε-caprolactone nanoparticles manufactured by dispersion polymerization.

PubMed

Ogunwuyi, O; Adesina, S; Akala, E O

2015-03-01

We report here our efforts on the development of stealth biodegradable crosslinked poly-ε-caprolactone nanoparticles by free radical dispersion polymerization suitable for the delivery of bioactive agents. The uniqueness of the dispersion polymerization technique is that it is surfactant free, thereby obviating the problems known to be associated with the use of surfactants in the fabrication of nanoparticles for biomedical applications. Aided by a statistical software for experimental design and analysis, we used D-optimal mixture statistical experimental design to generate thirty batches of nanoparticles prepared by varying the proportion of the components (poly-ε-caprolactone macromonomer, crosslinker, initiators and stabilizer) in acetone/water system. Morphology of the nanoparticles was examined using scanning electron microscopy (SEM). Particle size and zeta potential were measured by dynamic light scattering (DLS). Scheffe polynomial models were generated to predict particle size (nm) and particle surface zeta potential (mV) as functions of the proportion of the components. Solutions were returned from simultaneous optimization of the response variables for component combinations to (a) minimize nanoparticle size (small nanoparticles are internalized into disease organs easily, avoid reticuloendothelial clearance and lung filtration) and (b) maximization of the negative zeta potential values, as it is known that, following injection into the blood stream, nanoparticles with a positive zeta potential pose a threat of causing transient embolism and rapid clearance compared to negatively charged particles. In vitro availability isotherms show that the nanoparticles sustained the release of docetaxel for 72 to 120 hours depending on the formulation. The data show that nanotechnology platforms for controlled delivery of bioactive agents can be developed based on the nanoparticles.

Screening and analysis of the multiple absorbed bioactive components and metabolites in rat plasma after oral administration of Jitai tablets by high-performance liquid chromatography/diode-array detection coupled with electrospray ionization tandem mass spectrometry.

PubMed

Wang, Shu-Ping; Liu, Lei; Wang, Ling-Ling; Jiang, Peng; Zhang, Ji-Quan; Zhang, Wei-Dong; Liu, Run-Hui

2010-06-15

Based on the serum pharmacochemistry technique and high-performance liquid chromatography/diode-array detection (HPLC/DAD) coupled with electrospray tandem mass spectrometry (HPLC/ESI-MS/MS), a method for screening and analysis of the multiple absorbed bioactive components and metabolites of Jitai tablets (JTT) in orally dosed rat plasma was developed. Plasma was treated by methanol precipitation prior to liquid chromatography, and the separation was carried out on a Symmetry C(18) column, with a linear gradient (0.1% formic acid/water/acetonitrile). Mass spectra were acquired in negative and positive ion modes, respectively. As a result, 26 bioactive components originated from JTT and 5 metabolites were tentatively identified in orally dosed rat plasma by comparing their retention times and MS spectra with those of authentic standards and literature data. It is concluded that an effective and reliable analytical method was set up for screening the bioactive components of Chinese herbal medicine, which provided a meaningful basis for further pharmacology and active mechanism research of JTT. Copyright (c) 2010 John Wiley & Sons, Ltd.

Suitability of Different Food Grade Materials for the Encapsulation of Some Functional Foods Well Reported for Their Advantages and Susceptibility.

PubMed

Wani, Touseef Ahmed; Shah, Adil Gani; Wani, Sajad Mohd; Wani, Idrees Ahmed; Masoodi, Farooq Ahmad; Nissar, Nazia; Shagoo, Mudasir Ahmad

2016-11-17

Functional foods find a very important place in the modern era, where different types of cancer, diabetes, cardiovascular diseases, etc. are on a high. Irrespective of the abundance of bioactive components in different fruits and vegetables, their low solubility in aqueous solution, vulnerability to destruction in different environmental and gastrointestinal conditions and a low intestinal absorption becomes a concern. Because it is quite difficult to commercialize non food materials for the food encapsulation purposes due to their safety concerns in the human body, scientists in the recent times have come up with the idea of encapsulating the different bioactive components in different food grade materials that are able to safeguard these bioactive components against the different environmental and gastrointestinal conditions and ensure their safe and targeted delivery at their absorption sites. Different food grade encapsulation materials including various oligosaccharides, polysaccharides (starch, cyclodextrins, alginates, chitosan, gum arabic, and carboxymethyl cellulose) and proteins and their suitability for encapsulating various bioactive components like flavonoids (catechins, rutin, curcumin, hesperetin, and vanillin), nonflavonoids (resveratrol), carotenoids (β-carotene, lycopene, and lutein), and fatty acids (fish oil, flaxseed oil, and olive oil) of high medical and nutritional value are reviewed here.

Edible lipid nanoparticles: digestion, absorption, and potential toxicity.

PubMed

McClements, David Julian

2013-10-01

Food-grade nanoemulsions are being increasingly used in the food and beverage industry to encapsulate, protect, and deliver hydrophobic functional components, such as oil-soluble flavors, colors, preservatives, vitamins, and nutraceuticals. These nanoemulsions contain lipid nanoparticles (radius <100 nm) whose physicochemical characteristics (e.g., composition, dimensions, structure, charge, and physical state) can be controlled by selection of appropriate ingredients and fabrication techniques. Nanoemulsions have a number of potential advantages over conventional emulsions for applications within the food industry: higher stability to particle aggregation and gravitational separation; higher optical transparency; and, increased bioavailability of encapsulated components. On the other hand, there are also some risks associated with consumption of lipid nanoparticles that should be considered before they are widely utilized, such as their ability to alter the fate of bioactive components within the gastrointestinal tract and the potential toxicity of some of the components used in their fabrication (e.g., surfactants and organic solvents). This article provides an overview of the current status of the biological fate and potential toxicity of food-grade lipid nanoparticles suitable for utilization within the food and beverage industry. Copyright © 2013 Elsevier Ltd. All rights reserved.

Skin bioavailability of dietary vitamin E, carotenoids, polyphenols, vitamin C, zinc and selenium.

PubMed

Richelle, Myriam; Sabatier, Magalie; Steiling, Heike; Williamson, Gary

2006-08-01

Dietary bioactive compounds (vitamin E, carotenoids, polyphenols, vitamin C, Se and Zn) have beneficial effects on skin health. The classical route of administration of active compounds is by topical application direct to the skin, and manufacturers have substantial experience of formulating ingredients in this field. However, the use of functional foods and oral supplements for improving skin condition is increasing. For oral consumption, some dietary components could have an indirect effect on the skin via, for example, secondary messengers. However, in the case of the dietary bioactive compounds considered here, we assume that they must pass down the gastrointestinal tract, cross the intestinal barrier, reach the blood circulation, and then be distributed to the different tissues of the body including the skin. The advantages of this route of administration are that the dietary bioactive compounds are metabolized and then presented to the entire tissue, potentially in an active form. Also, the blood continuously replenishes the skin with these bioactive compounds, which can then be distributed to all skin compartments (i.e. epidermis, dermis, subcutaneous fat and also to sebum). Where known, the distribution and mechanisms of transport of dietary bioactive compounds in skin are presented. Even for compounds that have been studied well in other organs, information on skin is relatively sparse. Gaps in knowledge are identified and suggestions made for future research.

Eucommia ulmoides Oliver: A Potential Feedstock for Bioactive Products.

PubMed

Zhu, Ming-Qiang; Sun, Run-Cang

2018-06-06

Eucommia ulmoides Oliver (EUO), a traditional Chinese herb, contains a variety of bioactive chemicals, including lignans, iridoids, phenolics, steroids, terpenoids, flavonoids, etc. These bioactive chemicals possess the effective function in nourishing the liver and kidneys and regulating blood pressure. The composition of bioactive chemicals extracted from EUO vary in the different functional parts (leaves, seeds, bark, and staminate flower) and planting models. The bioactive parts of EUO are widely used as raw materials for medicine and food, powdery extracts, herbal formulations, and tinctures. These capabilities hold potential for future development and commercial exploitation of the bioactive products from EUO.

Bioactive Carbohydrates and Peptides in Foods: An Overview of Sources, Downstream Processing Steps and Associated Bioactivities.

PubMed

Hayes, Maria; Tiwari, Brijesh K

2015-09-17

Bioactive peptides and carbohydrates are sourced from a myriad of plant, animal and insects and have huge potential for use as food ingredients and pharmaceuticals. However, downstream processing bottlenecks hinder the potential use of these natural bioactive compounds and add cost to production processes. This review discusses the health benefits and bioactivities associated with peptides and carbohydrates of natural origin and downstream processing methodologies and novel processes which may be used to overcome these.

Bioactive Carbohydrates and Peptides in Foods: An Overview of Sources, Downstream Processing Steps and Associated Bioactivities

PubMed Central

Hayes, Maria; Tiwari, Brijesh K.

2015-01-01

Bioactive peptides and carbohydrates are sourced from a myriad of plant, animal and insects and have huge potential for use as food ingredients and pharmaceuticals. However, downstream processing bottlenecks hinder the potential use of these natural bioactive compounds and add cost to production processes. This review discusses the health benefits and bioactivities associated with peptides and carbohydrates of natural origin and downstream processing methodologies and novel processes which may be used to overcome these. PMID:26393573

Combinations of Ashwagandha Leaf Extracts Protect Brain-Derived Cells against Oxidative Stress and Induce Differentiation

PubMed Central

Shah, Navjot; Singh, Rumani; Sarangi, Upasana; Saxena, Nishant; Chaudhary, Anupama; Kaur, Gurcharan; Kaul, Sunil C.; Wadhwa, Renu

2015-01-01

Background Ashwagandha, a traditional Indian herb, has been known for its variety of therapeutic activities. We earlier demonstrated anticancer activities in the alcoholic and water extracts of the leaves that were mediated by activation of tumor suppressor functions and oxidative stress in cancer cells. Low doses of these extracts were shown to possess neuroprotective activities in vitro and in vivo assays. Methodology/Principal Findings We used cultured glioblastoma and neuroblastoma cells to examine the effect of extracts (alcoholic and water) as well as their bioactive components for neuroprotective activities against oxidative stress. Various biochemical and imaging assays on the marker proteins of glial and neuronal cells were performed along with their survival profiles in control, stressed and recovered conditions. We found that the extracts and one of the purified components, withanone, when used at a low dose, protected the glial and neuronal cells from oxidative as well as glutamate insult, and induced their differentiation per se. Furthermore, the combinations of extracts and active component were highly potent endorsing the therapeutic merit of the combinational approach. Conclusion Ashwagandha leaf derived bioactive compounds have neuroprotective potential and may serve as supplement for brain health. PMID:25789768

Screening and analysis of potential anti-tumor components from the stipe of Ganoderma sinense using high-performance liquid chromatography/time-of-flight mass spectrometry with multivariate statistical tool.

PubMed

Chan, Kar-Man; Yue, Grace Gar-Lee; Li, Ping; Wong, Eric Chun-Wai; Lee, Julia Kin-Ming; Kennelly, Edward J; Lau, Clara Bik-San

2017-03-03

According to Chinese Pharmacopoeia 2015 edition, Ganoderma (Lingzhi) is a species complex that comprise of Ganoderma lucidum and Ganoderma sinense. The bioactivity and chemical composition of G. lucidium had been studied extensively, and it was shown to possess antitumor activities in pharmacological studies. In contrast, G. sinense has not been studied in great detail. Our previous studies found that the stipe of G. sinense exhibited more potent antitumor activity than the pileus. To identify the antitumor compounds in the stipe of G. sinense, we studied its chemical components by merging the bioactivity results with liquid chromatography-mass spectrometry-based chemometrics. The stipe of G. sinense was extracted with water, followed by ethanol precipitation and liquid-liquid partition. The resulting residue was fractionated using column chromatography. The antitumor activity of these fractions were analysed using MTT assay in murine breast tumor 4T1 cells, and their chemical components were studied using the LC-QTOF-MS with multivariate statistical tools. The chemometric and MS/MS analysis correlated bioactivity with five known cytotoxic compounds, 4-hyroxyphenylacetate, 9-oxo-(10E,12E)-octadecadienoic acid, 3-phenyl-2-propenoic acid, 13-oxo-(9E,11E)-octadecadienoic acid and lingzhine C, from the stipe of G. sinense. To the best of our knowledge, 4-hyroxyphenylacetate, 3-phenyl-2-propenoic acid and lingzhine C are firstly reported to be found in G. sinense. These five compounds will be investigated for their antitumor activities in the future. Copyright © 2017 Elsevier B.V. All rights reserved.

Evaluation of quality of kefir from milk obtained from goats supplemented with a diet rich in bioactive compounds.

PubMed

Cais-Sokolińska, Dorota; Pikul, Jan; Wójtowski, Jacek; Danków, Romualda; Teichert, Joanna; Czyżak-Runowska, Grażyna; Bagnicka, Emilia

2015-04-01

The composition of bioactive components in dairy products depends on their content in raw milk and the processing conditions. The experimental material consisted of the milk of dairy goats supplemented with 120 g d(-1) per head of false flax cake. The aim of the study was to evaluate the quality of kefir produced from goat's milk with a higher content of bioactive components resulting from supplementation of the goats' diet with false flax cake. The administration of false flax cake to goats had a positive effect on the fatty acid profile of the raw milk, causing an increase in the proportion of polyunsaturated fatty acids (PUFA), including conjugated linoleic acid (CLA) and n-3 fatty acids. Their increased percentage was detected in the kefir after production as well as after storage. The processing value of the harvested milk did not differ from the qualitative characteristics of milk from goats of the control group. Increasing the proportion of bioactive components in goat's milk did not result in changes in the acidity, texture, colour, flavour, aroma or consistency of the kefir obtained. Milk and kefir obtained after the administration of false flax cake to goats contain bioactive components (PUFA including CLA, n-3 and monoenic trans fatty acids) in significant amounts. Kefir from experimental goat's milk did not differ in quality from kefir made from the milk of the control group. © 2014 Society of Chemical Industry.

Preparation, process optimization and characterization of core-shell polyurethane/chitosan nanofibers as a potential platform for bioactive scaffolds.

PubMed

Maleknia, Laleh; Dilamian, Mandana; Pilehrood, Mohammad Kazemi; Sadeghi-Aliabadi, Hojjat; Hekmati, Amir Houshang

2018-06-01

In this paper, polyurethane (PU), chitosan (Cs)/polyethylene oxide (PEO), and core-shell PU/Cs nanofibers were produced at the optimal processing conditions using electrospinning technique. Several methods including SEM, TEM, FTIR, XRD, DSC, TGA and image analysis were utilized to characterize these nanofibrous structures. SEM images exhibited that the core-shell PU/Cs nanofibers were spun without any structural imperfections at the optimized processing conditions. TEM image confirmed the PU/Cs core-shell nanofibers were formed apparently. It that seems the inclusion of Cs/PEO to the shell, did not induce the significant variations in the crystallinity in the core-shell nanofibers. DSC analysis showed that the inclusion of Cs/PEO led to the glass temperature of the composition increased significantly compared to those of neat PU nanofibers. The thermal degradation of core-shell PU/Cs was similar to PU nanofibers degradation due to the higher PU concentration compared to other components. It was hypothesized that the core-shell PU/Cs nanofibers can be used as a potential platform for the bioactive scaffolds in tissue engineering. Further biological tests should be conducted to evaluate this platform as a three dimensional scaffold with the capabilities of releasing the bioactive molecules in a sustained manner.

The molecular mechanism of the cholesterol-lowering effect of dill and kale: The influence of the food matrix components.

PubMed

Danesi, Francesca; Govoni, Marco; D'Antuono, Luigi Filippo; Bordoni, Alessandra

2016-07-01

Foods are complex matrices containing many different compounds, all of which contribute to the overall effect of the food itself, although they have different mechanisms of action. While evaluating the effect of bioactive compounds, it is important to consider that the use of a single compound can hide the effects of the other molecules that can act synergistically or antagonistically in the same food. The aim of the present study was to evaluate the influence of food matrix components by comparing two edible plants (dill and kale) with cholesterol-lowering potential and similar contents of their most representative bioactive, quercetin. The molecular effects of the extracts were evaluated in HepG2 cells by measuring the expression of sterol-regulatory element-binding proteins (SREBPs), 3-hydroxy-3-methylglutaryl-CoA reductase (HMGCR) and low density lipoprotein receptor (LDLR) at the mRNA and protein level. The results reported here show that both extracts reduced the cellular cholesterol level with a similar trend and magnitude. It is conceivable that the slightly different results are due to the diverse composition of minor bioactive compounds, indicating that only by considering food as a whole is it possible to understand the complex relationship between food, nutrition, and health in a foodomics vision. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Dentin Biomodification: Strategies, Renewable Resources and Clinical Applications

PubMed Central

Bedran-Russo, Ana K.; Pauli, Guido F.; Chen, Shao-Nong; McAlpine, James; Castellan, Carina S.; Phansalkar, Rasika S; Aguiar, Thaiane R.; Vidal, Cristina M.P.; Napotilano, José; Nam, Joo-Won; Leme, Ariene A.

2014-01-01

Objectives The biomodification of dentin is a biomimetic approach, mediated by bioactive agents, to enhance and reinforce the dentin by locally altering the biochemistry and biomechanical properties. This review provides an overview of key dentin matrix components, targeting effects of biomodification strategies, the chemistry of renewable natural sources, and current research on their potential clinical applications. Methods The PubMed database and collected literature were used as a resource for peer-reviewed articles to highlight the topics of dentin hierarchical structure, biomodification agents, and laboratorial investigations of their clinical applications. In addition, new data is presented on laboratorial methods for the standardization of proanthocyanidin-rich preparations as a renewable source of plant-derived biomodification agents. Results Biomodification agents can be categorized as physical methods and chemical agents. Synthetic and naturally occurring chemical strategies present distinctive mechanism of interaction with the tissue. Initially thought to be driven only by inter- or intra-molecular collagen induced non-enzymatic collagen cross-linking, multiple interactions with other dentin components are fundamental for the long-term biomechanics and biostability of the tissue. Oligomeric proanthocyanidins show promising bioactivity, and their chemical complexity requires systematic evaluation of the active compounds to produce a fully standardized intervention material from renewable resource, prior to their detailed clinical evaluation. Significance Understanding the hierarchical structure of dentin and the targeting effect of the bioactive compounds will establish their use in both dentin-biomaterials interface and caries management. PMID:24309436

Comparative study on major bioactive components in natural, artificial and in-vitro cultured Calculus Bovis.

PubMed

Yan, Shi-Kai; Wu, Yan-Wen; Liu, Run-Hui; Zhang, Wei-Dong

2007-01-01

Major bioactive components in various Calculus Bovis, including natural, artificial and in-vitro cultured Calculus Bovis, were comparatively studied. An approach of high-performance liquid chromatography coupled with ultraviolet and evaporative light scattering detections (HPLC/UV/ELSD) was established to simultaneously determinate six bioactive components thereof, including five bile acids (cholic acid, deoxycholic acid, ursodeoxycholic, chenodeoxycholic acid, hyodeoxycholic acid) and bilirubin. ELSD and UV detector were applied to detect bile acids and bilirubin respectively. The assay was performed on a C(18) column with water-acetonitrile gradient elution and the investigated constituents were authenticated by comparing retention times and mass spectra with those of reference compounds. The proposed method was applied to analyze twenty-one Calculus Bovis extraction samples, and produced data with acceptable linearity, precision, repeatability and accuracy. The result indicated the variations among Calculus Bovis samples under different developmental conditions. Artificial and in-vitro cultured Calculus Bovis, especially in-vitro cultured ones, which contain total bioactive constituents no less than natural products and have the best batch-to-batch uniformity, suffice to be used as substitutes of natural Calculus Bovis.

Hypolipidemic activity of Taraxacum mongolicum associated with the activation of AMP-activated protein kinase in human HepG2 cells.

PubMed

Liu, Yan-Jin; Shieh, Po-Chuen; Lee, Jang-Chang; Chen, Fu-An; Lee, Chih-Hung; Kuo, Sheng-Chu; Ho, Chi-Tang; Kuo, Daih-Huang; Huang, Li-Jiau; Way, Tzong-Der

2014-08-01

This study investigated the hypolipidemic effect and potential mechanisms of T. mongolicum extracts. T. mongolicum was extracted by refluxing three times with water (TM-1), 50% ethanol (TM-2) and 95% ethanol (TM-3). TM-2 contained components with the most effective hypolipidemic potentials in HepG2 cells. Extended administration of TM-2 stimulated a significant reduction in body weight and levels of serum triglyceride LDL-C and total cholesterol in rats. To evaluate the bioactive compounds, we successively fractionated TM-2 with n-hexane (TM-4), dichloromethane (TM-5), ethyl acetate (TM-6), and water (TM-7). TM-4 fraction had the most effective hypolipidemic potential in HepG2 cells, and it decreased the expression of fatty acid synthase (FASN) and inhibited the activity of acetyl-coenzyme A carboxylase (ACC) through the phosphorylation of AMP-activated protein kinase (AMPK). Linoleic acid, phytol and tetracosanol are bioactive compounds identified from TM-4. These results suggest that T. mongolicum is expected to be useful for hypolipidemic effects.

Bioactive components on immuno-enhancement effects in the traditional Chinese medicine Shenqi Fuzheng Injection based on relevance analysis between chemical HPLC fingerprints and in vivo biological effects.

PubMed

Wang, Jinxu; Tong, Xin; Li, Peibo; Liu, Menghua; Peng, Wei; Cao, Hui; Su, Weiwei

2014-08-08

Shenqi Fuzheng Injection (SFI) is an injectable traditional Chinese herbal formula comprised of two Chinese herbs, Radix codonopsis and Radix astragali, which were commonly used to improve immune functions against chronic diseases in an integrative and holistic way in China and other East Asian countries for thousands of years. This present study was designed to explore the bioactive components on immuno-enhancement effects in SFI using the relevance analysis between chemical fingerprints and biological effects in vivo. According to a four-factor, nine-level uniform design, SFI samples were prepared with different proportions of the four portions separated from SFI via high speed counter current chromatography (HSCCC). SFI samples were assessed with high performance liquid chromatography (HPLC) for 23 identified components. For the immunosuppressed murine experiments, biological effects in vivo were evaluated on spleen index (E1), peripheral white blood cell counts (E2), bone marrow cell counts (E3), splenic lymphocyte proliferation (E4), splenic natural killer cell activity (E5), peritoneal macrophage phagocytosis (E6) and the amount of interleukin-2 (E7). Based on the hypothesis that biological effects in vivo varied with differences in components, multivariate relevance analysis, including gray relational analysis (GRA), multi-linear regression analysis (MLRA) and principal component analysis (PCA), were performed to evaluate the contribution of each identified component. The results indicated that the bioactive components of SFI on immuno-enhancement activities were calycosin-7-O-β-d-glucopyranoside (P9), isomucronulatol-7,2'-di-O-glucoside (P11), biochanin-7-glucoside (P12), 9,10-dimethoxypterocarpan-3-O-xylosylglucoside (P15) and astragaloside IV (P20), which might have positive effects on spleen index (E1), splenic lymphocyte proliferation (E4), splenic natural killer cell activity (E5), peritoneal macrophage phagocytosis (E6) and the amount of interleukin-2 (E7), while 5-hydroxymethyl-furaldehyde (P5) and lobetyolin (P13) might have negative effects on E1, E4, E5, E6 and E7. Finally, the bioactive HPLC fingerprint of SFI based on its bioactive components on immuno-enhancement effects was established for quality control of SFI. In summary, this study provided a perspective to explore the bioactive components in a traditional Chinese herbal formula with a series of HPLC and animal experiments, which would be helpful to improve quality control and inspire further clinical studies of traditional Chinese medicines. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

In vitro antifungal potentials of bioactive compound oleic acid, 3-(octadecyloxy) propyl ester isolated from Lepidagathis cristata Willd. (Acanthaceae) inflorescence.

PubMed

Abubacker, Maghdu Nainamohamed; Devi, Palaniyappan Kamala

2014-09-01

To identify bioactive compound oleic acid, 3-(octadecyloxy) propyl ester from Lepidagathis cristata Willd. (L. cristata) and to assess antifungal potentials of the isolated compound. Aqueous extracts of L. cristata inflorescence were used for this study. The major bioactive compound isolated was tested for antifungal activities. The major bioactive compound oleic acid, 3-(octadecyloxy) propyl ester was isolated from the inflorescence of L. cristata. The bioactive compound was tested for antifungal potentials and found to be highly effective to plant pathogenic fungi Colletotrichum fulcatum NCBT 146, Fusarium oxysporum NCBT 156 and Rhizoctonia solani NCBT 196 as well as for the human pathogenic fungi Curvularia lunata MTCC 2030 and Microsporum canis MTCC 2820. The results justify the antifungal potentials of both plant and human pathogenic fungi. The plant bioactive compound will be helpful in herbal antifungal formulations. Copyright © 2014 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

Simultaneous Quantification of Seven Bioactive Flavonoids in Citri Reticulatae Pericarpium by Ultra-Fast Liquid Chromatography Coupled with Tandem Mass Spectrometry.

PubMed

Zhao, Lian-Hua; Zhao, Hong-Zheng; Zhao, Xue; Kong, Wei-Jun; Hu, Yi-Chen; Yang, Shi-Hai; Yang, Mei-Hua

2016-05-01

Citri Reticulatae Pericarpium (CRP) is a commonly-used traditional Chinese medicine with flavonoids as the major bioactive components. Nevertheless, the contents of the flavonoids in CRP of different sources may significantly vary affecting their therapeutic effects. Thus, the setting up of a reliable and comprehensive quality assessment method for flavonoids in CRP is necessary. To set up a rapid and sensitive ultra-fast liquid chromatography coupled with tandem mass spectrometry (UFLC-MS/MS) method for simultaneous quantification of seven bioactive flavonoids in CRP. A UFLC-MS/MS method coupled to ultrasound-assisted extraction was developed for simultaneous separation and quantification of seven flavonoids including hesperidin, neohesperidin, naringin, narirutin, tangeretin, nobiletin and sinensetin in 16 batches of CRP samples from different sources in China. The established method showed good linearity for all analytes with correlation coefficient (R) over 0.9980, together with satisfactory accuracy, precision and reproducibility. Furthermore, the recoveries at the three spiked levels were higher than 89.71% with relative standard deviations (RSDs) lower than 5.19%. The results indicated that the contents of seven bioactive flavonoids in CRP varied significantly among different sources. Among the samples under study, hesperidin showed the highest contents in 16 samples ranged from 27.50 to 86.30 mg/g, the contents of hesperidin in CRP-15 and CRP-9 were 27.50 and 86.30 mg/g, respectively, while, the amount of narirutin was too low to be measured in some samples. This study revealed that the developed UFLC-MS/MS method was simple, sensitive and reliable for simultaneous quantification of multi-components in CRP with potential perspective for quality control of complex matrices. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

Use of Raman microscopy and multivariate data analysis to observe the biomimetic growth of carbonated hydroxyapatite on bioactive glass.

PubMed

Seah, Regina K H; Garland, Marc; Loo, Joachim S C; Widjaja, Effendi

2009-02-15

In the present contribution, the biomimetic growth of carbonated hydroxyapatite (HA) on bioactive glass were investigated by Raman microscopy. Bioactive glass samples were immersed in simulated body fluid (SBF) buffered solution at pH 7.40 up to 17 days at 37 degrees C. Raman microscopy mapping was performed on the bioglass samples immersed in SBF solution for different periods of time. The collected data was then analyzed using the band-target entropy minimization technique to extract the observable pure component Raman spectral information. In this study, the pure component Raman spectra of the precursor amorphous calcium phosphate, transient octacalcium phosphate, and matured HA were all recovered. In addition, pure component Raman spectra of calcite, silica glass, and some organic impurities were also recovered. The resolved pure component spectra were fit to the normalized measured Raman data to provide the spatial distribution of these species on the sample surfaces. The current results show that Raman microscopy and multivariate data analysis provide a sensitive and accurate tool to characterize the surface morphology, as well as to give more specific information on the chemical species present and the phase transformation of phosphate species during the formation of HA on bioactive glass.

Bioaccessible nutrients and bioactive components from fortified products prepared using finger millet (Eleusine coracana).

PubMed

Oghbaei, Morteza; Prakash, Jamuna

2012-08-30

Finger millet (Eleusine coracana), a staple food in semi-arid parts of the world, is a rich source of nutrients and bioactive components comparable to rice and wheat but with higher fibre content. Unprocessed and processed finger millet (whole flour (WFM), sieved flour (SFM), wafers and vermicelli with altered matrices (added Fe or Zn or reduced fibre)) were analysed for chemical composition, bioaccessible Fe, Zn and Ca, in vitro digestible starch (IVSD) and protein (IVPD) and bioactive components (polyphenols and flavonoids). WFM and SFM flours differed significantly in their composition. Sieving decreased the content of both nutrients and antinutrients in WFM but increased their digestibility/bioaccessibility. WFM products with Zn and Fe showed highest IVPD, whereas SFM products with Fe showed highest IVSD. Products with externally added Fe and Zn showed maximum bioaccessibility of Fe and Zn respectively. WFM had the highest levels of total polyphenols and flavonoids, 4.18 and 15.85 g kg⁻¹ respectively; however, bioaccessibility was highest in SFM vermicelli. The availability of nutrients and bioactive components was influenced by both processing methods and compositional alterations of the food matrix in finger millet products, and bioaccessibility of all constituents was higher in vermicelli (wet matrix) than in wafers (dry matrix). Copyright © 2012 Society of Chemical Industry.

Characterisation of metabolic profile of banana genotypes, aiming at biofortified Musa spp. cultivars.

PubMed

Borges, Cristine Vanz; Amorim, Vanusia Batista de Oliveira; Ramlov, Fernanda; Ledo, Carlos Alberto da Silva; Donato, Marcela; Maraschin, Marcelo; Amorim, Edson Perito

2014-02-15

The banana is an important, widely consumed fruit, especially in areas of rampant undernutrition. Twenty-nine samples were analysed, including 9 diploids, 13 triploids and 7 tetraploids, in the Active Germplasm Bank, at Embrapa Cassava & Fruits, to evaluate the bioactive compounds. The results of this study reveal the presence of a diversity of bioactive compounds, e.g., catechins; they are phenolic compounds with high antioxidant potential and antitumour activity. In addition, accessions with appreciable amounts of pVACs were identified, especially compared with the main cultivars that are currently marketed. The ATR-FTIR, combined with principal components analysis, identified accessions with distinct metabolic profiles in the fingerprint regions of compounds important for human health. Likewise, starch fraction characterisation allowed discrimination of accessions according to their physical, chemical, and functional properties. The results of this study demonstrate that the banana has functional characteristics endowing it with the potential to promote human health. Copyright © 2013 Elsevier Ltd. All rights reserved.

Bioactive Mushroom Polysaccharides: A Review on Monosaccharide Composition, Biosynthesis and Regulation.

PubMed

Wang, Qiong; Wang, Feng; Xu, Zhenghong; Ding, Zhongyang

2017-06-13

Mushrooms are widely distributed around the world and are heavily consumed because of their nutritional value and medicinal properties. Polysaccharides (PSs) are an important component of mushrooms, a major factor in their bioactive properties, and have been intensively studied during the past two decades. Monosaccharide composition/combinations are important determinants of PS bioactivities. This review summarizes: (i) monosaccharide composition/combinations in various mushroom PSs, and their relationships with PS bioactivities; (ii) possible biosynthetic pathways of mushroom PSs and effects of key enzymes on monosaccharide composition; (iii) regulation strategies in PS biosynthesis, and prospects for controllable biosynthesis of PSs with enhanced bioactivities.

Comparison of bioactive components in pressurized and pasteurized longan juices fortified with encapsulated Lactobacillus casei 01

NASA Astrophysics Data System (ADS)

Chaikham, Pittaya; Apichartsrangkoon, Arunee

2012-06-01

In this study, longan juice was subjected to a high pressure of 500 MPa for 30 min and compared with a juice pasteurized at 90°C/2 min. Probiotic Lactobacillus casei 01 was fortified into both juices and the shelf life of these products was studied. Their bioactive components such as ascorbic acid, gallic acid and ellagic acid were analyzed by High Performance Liquid Chromatography (HPLC). Total phenolic compounds and 2,2-Diphenyl-1-picrythydrazyl radical-scavenging activity were determined by colorimetric and spectrophotometric methods. It was found that the pressurized longan juice retained higher amounts of bioactive compounds than the pasteurized juice. In terms of storage stability, bioactive compounds in both processed juices decreased according to the increase in storage time. The survivability of probiotic L. casei 01 in both processed juices declined from 9 to 6 log CFU/mL after 4 weeks of storage.

In vitro studies on the relationship between the antioxidant activities of some berry extracts and their binding properties to serum albumin.

PubMed

Namiesnik, Jacek; Vearasilp, Kann; Nemirovski, Alina; Leontowicz, Hanna; Leontowicz, Maria; Pasko, Pawel; Martinez-Ayala, Alma Leticia; González-Aguilar, Gustavo A; Suhaj, Milan; Gorinstein, Shela

2014-03-01

The aim of this study was to investigate the possibility to use the bioactive components from cape gooseberry (Physalis peruviana), blueberry (Vaccinium corymbosum), and cranberry (Vaccinium macrocarpon) extracts as a novel source against oxidation in food supplementation. The quantitative analysis of bioactive compounds (polyphenols, flavonoids, flavanols, carotenoids, and chlorophyll) was based on radical scavenging spectrophometric assays and mass spectrometry. The total phenolic content was the highest (P < 0.05) in water extract of blueberries (46.6 ± 4.2 mg GAE/g DW). The highest antioxidant activities by 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay and Cupric reducing antioxidant capacity were in water extracts of blueberries, showing 108.1 ± 7.2 and 131.1 ± 9.6 μMTE/g DW with correlation coefficients of 0.9918 and 0.9925, and by β-carotene linoleate assay at 80.1 ± 6.6 % with correlation coefficient of 0.9909, respectively. The water extracts of berries exhibited high binding properties with human serum albumin in comparison with quercetin. In conclusion, the bioactive compounds from a relatively new source of gooseberries in comparison with blueberries and cranberries have the potential as food supplementation for human health. The antioxidant and binding activities of berries depend on their bioactive compounds.

Reduced graphene oxide-coated hydroxyapatite composites stimulate spontaneous osteogenic differentiation of human mesenchymal stem cells

NASA Astrophysics Data System (ADS)

Lee, Jong Ho; Shin, Yong Cheol; Jin, Oh Seong; Kang, Seok Hee; Hwang, Yu-Shik; Park, Jong-Chul; Hong, Suck Won; Han, Dong-Wook

2015-07-01

Human mesenchymal stem cells (hMSCs) have great potential as cell sources for bone tissue engineering and regeneration, but the control and induction of their specific differentiation into bone cells remain challenging. Graphene-based nanomaterials are considered attractive candidates for biomedical applications such as scaffolds in tissue engineering, substrates for SC differentiation and components of implantable devices, due to their biocompatible and bioactive properties. Despite the potential biomedical applications of graphene and its derivatives, only limited information is available regarding their osteogenic activity. This study concentrates upon the effects of reduced graphene oxide (rGO)-coated hydroxyapatite (HAp) composites on osteogenic differentiation of hMSCs. The average particle sizes of HAp and rGO were 1270 +/- 476 nm and 438 +/- 180 nm, respectively. When coated on HAp particulates, rGO synergistically enhanced spontaneous osteogenic differentiation of hMSCs, without hampering their proliferation. This result was confirmed by determining alkaline phosphatase activity and mineralization of calcium and phosphate as early and late stage markers of osteogenic differentiation. It is suggested that rGO-coated HAp composites can be effectively utilized as dental and orthopedic bone fillers since these graphene-based particulate materials have potent effects on stimulating the spontaneous differentiation of MSCs and show superior bioactivity and osteoinductive potential.Human mesenchymal stem cells (hMSCs) have great potential as cell sources for bone tissue engineering and regeneration, but the control and induction of their specific differentiation into bone cells remain challenging. Graphene-based nanomaterials are considered attractive candidates for biomedical applications such as scaffolds in tissue engineering, substrates for SC differentiation and components of implantable devices, due to their biocompatible and bioactive properties. Despite the potential biomedical applications of graphene and its derivatives, only limited information is available regarding their osteogenic activity. This study concentrates upon the effects of reduced graphene oxide (rGO)-coated hydroxyapatite (HAp) composites on osteogenic differentiation of hMSCs. The average particle sizes of HAp and rGO were 1270 +/- 476 nm and 438 +/- 180 nm, respectively. When coated on HAp particulates, rGO synergistically enhanced spontaneous osteogenic differentiation of hMSCs, without hampering their proliferation. This result was confirmed by determining alkaline phosphatase activity and mineralization of calcium and phosphate as early and late stage markers of osteogenic differentiation. It is suggested that rGO-coated HAp composites can be effectively utilized as dental and orthopedic bone fillers since these graphene-based particulate materials have potent effects on stimulating the spontaneous differentiation of MSCs and show superior bioactivity and osteoinductive potential. Electronic supplementary information (ESI) available: Additional figures. See DOI: 10.1039/c5nr01580d

Effects of Ultrasound Assistance on Dehydration Processes and Bioactive Component Retention of Osmo-Dried Sour Cherries.

PubMed

Siucińska, Karolina; Mieszczakowska-Frąc, Monika; Połubok, Aleksandra; Konopacka, Dorota

2016-07-01

Despite having numerous health benefits, dried sour cherries have proven to be more acceptable to consumers when infused with sugar or other sweeteners to enhance their flavor, which, in turn, leads to serious anthocyanin losses. For this reason, a consideration was made for the application of ultrasound to accelerate solid gain and shorten drying time, thus favoring bioactive component retention. To determine the usefulness of ultrasound as a tool for sour cherry osmotic infusion enhancement, the effect of sonication time on dehydration effectiveness, as well as the stability of bioactive components during osmotic treatment and consecutive convective drying, was investigated. Fruits were osmo-dehydrated using a 60% sucrose solution for 120 min (40 °C), during which, ultrasound of 25 kHz (0.4 W/cm(2) ), was applied for 0, 30, 60, 90, and 120 min, after which, the fruits were convectively dried. In the range of the applied ultrasound energy no significant effect of sonication on mass transfer intensification was observed; moreover, longer acoustic treatment seemed to retard moisture removal during subsequent convective drying, which can be related to the breakdown of the parenchyma cell walls caused by the prolonged ultrasound (US) action. It was concluded that although US assistance could be considered neutral for bioactive component retention, excessive sonication time can lead to some anthocyanin deterioration. According to high-performance liquid chromatography analysis, the particular anthocyanin alterations, both during dehydration and final drying, occurred in a similar way. Sonication time prolongation caused approximately 10% more bioactive compound deterioration, than earlier, shorter trials. © 2016 Institute of Food Technologists®

Integrating Dynamic Positron Emission Tomography and Conventional Pharmacokinetic Studies to Delineate Plasma and Tumor Pharmacokinetics of FAU, a Prodrug Bioactivated by Thymidylate Synthase.

PubMed

Li, Jing; Kim, Seongho; Shields, Anthony F; Douglas, Kirk A; McHugh, Christopher I; Lawhorn-Crews, Jawana M; Wu, Jianmei; Mangner, Thomas J; LoRusso, Patricia M

2016-11-01

FAU, a pyrimidine nucleotide analogue, is a prodrug bioactivated by intracellular thymidylate synthase to form FMAU, which is incorporated into DNA, causing cell death. This study presents a model-based approach to integrating dynamic positron emission tomography (PET) and conventional plasma pharmacokinetic studies to characterize the plasma and tissue pharmacokinetics of FAU and FMAU. Twelve cancer patients were enrolled into a phase 1 study, where conventional plasma pharmacokinetic evaluation of therapeutic FAU (50-1600 mg/m 2 ) and dynamic PET assessment of 18 F-FAU were performed. A parent-metabolite population pharmacokinetic model was developed to simultaneously fit PET-derived tissue data and conventional plasma pharmacokinetic data. The developed model enabled separation of PET-derived total tissue concentrations into the parent drug and metabolite components. The model provides quantitative, mechanistic insights into the bioactivation of FAU and retention of FMAU in normal and tumor tissues and has potential utility to predict tumor responsiveness to FAU treatment. © 2016, The American College of Clinical Pharmacology.

Meat and fermented meat products as a source of bioactive peptides.

PubMed

Stadnik, Joanna; Kęska, Paulina

2015-01-01

Bioactive peptides are short amino acid sequences, that upon release from the parent protein may play different physiological roles, including antioxidant, antihypertensive, antimicrobial, and other bioactivities. They have been identified from a range of foods, including those of animal origin, e.g., milk and muscle sources (with pork, beef, or chicken and various species of fish and marine organism). Bioactive peptides are encrypted within the sequence of the parent protein molecule and latent until released and activated by enzymatic proteolysis, e.g. during gastrointestinal digestion or food processing. Bioactive peptides derived from food sources have the potential for incorporation into functional foods and nutraceuticals. The aim of this paper is to present an overview of the muscle-derived bioactive peptides, especially those of fermented meats and the potential benefits of these bioactive compounds to human health.

Antioxidant activity of Sicilian pistachio (Pistacia vera L. var. Bronte) nut extract and its bioactive components.

PubMed

Gentile, Carla; Tesoriere, Luisa; Butera, Daniela; Fazzari, Marco; Monastero, Massimo; Allegra, Mario; Livrea, Maria A

2007-02-07

Pistacia vera L. is the only species of Pistacia genus producing edible nuts. This paper investigates the antioxidant potential of a Sicilian variety of pistachio nut by chemical as well as biological assays and measured antioxidant vitamins and a number of antioxidant polyphenols in either the hydrophilic and/or the lipophilic nut extract. In accordance with the majority of foods, the total antioxidant activity, measured as a TAA test, was much higher (50-fold) in the hydrophilic than in the lipophilic extract. Substantial amounts of total phenols were measured. The hydrophilic extract inhibited dose-dependently both the metal-dependent and -independent lipid oxidation of bovine liver microsomes, and the Cu+2-induced oxidation of human low-density lipoprotein (LDL). Peroxyl radical-scavenging as well as chelating activity of nut components may be suggested to explain the observed inhibition patterns. Among tocopherols, gamma-tocopherol was the only vitamin E isomer found in the lipophilic extract that did not contain any carotenoid. Vitamin C was found only in a modest amount. The hydrophilic extract was a source of polyphenol compounds among which trans-resveratrol, proanthocyanidins, and a remarkable amount of the isoflavones daidzein and genistein, 3.68 and 3.40 mg per 100 g of edible nut, respectively, were evaluated. With the exception of isoflavones that appeared unmodified, the amounts of other bioactive molecules were remarkably reduced in the pistachio nut after roasting, and the total antioxidant activity decreased by about 60%. Collectively, our findings provide evidence that the Sicilian pistachio nut may be considered for its bioactive components and can effectively contribute to a healthy status.

Curing potential of experimental resin composites with systematically varying amount of bioactive glass: Degree of conversion, light transmittance and depth of cure.

PubMed

Par, Matej; Spanovic, Nika; Bjelovucic, Ruza; Skenderovic, Hrvoje; Gamulin, Ozren; Tarle, Zrinka

2018-06-17

The aim of this work was to investigate the curing potential of an experimental resin composite series with the systematically varying amount of bioactive glass 45S5 by evaluating the degree of conversion, light transmittance and depth of cure. Resin composites based on a Bis-GMA/TEGDMA resin with a total filler load of 70 wt% and a variable amount of bioactive glass (0-40 wt%) were prepared. The photoinitiator system was camphorquinone and ethyl-4-(dimethylamino) benzoate. The degree of conversion and light transmittance were measured by Raman spectroscopy and UV-vis spectroscopy, respectively. The depth of cure was evaluated according to the classical ISO 4049 test. The initial introduction of bioactive glass into the experimental series diminished the light transmittance while the further increase in the bioactive glass amount up to 40 wt% caused minor variations with no clear trend. The curing potential of the experimental composites was similar to or better than that of commercial resin composites. However, unsilanized bioactive glass fillers demonstrated the tendency to diminish both the maximum attainable conversion and the curing efficiency at depth. Experimental composite materials containing bioactive glass showed a clinically acceptable degree of conversion and depth of cure. The degree of conversion and depth of cure were diminished by bioactive glass fillers in a dose-dependent manner, although light transmittance was similar among all of the experimental composites containing 5-40 wt% of bioactive glass. Reduced curing potential caused by the bioactive glass has possible consequences on mechanical properties and biocompatibility. Copyright © 2018 Elsevier Ltd. All rights reserved.

[Beneficial effects of chocolate on cardiovascular health].

PubMed

Gómez-Juaristi, M; González-Torres, L; Bravo, L; Vaquero, M P; Bastida, S; Sánchez-Muniz, F J

2011-01-01

Since ancient times, numerous health beneficial effects have been attributed to chocolate, closing up its consumption to a therapeutic use. The present study reviews some relevant studies about chocolate (and its bioactive compounds) on some cardiovascular risk factors and stresses the need of future studies. The consumption of cocoa/ chocolate (i) increases plasma antioxidant capacity, (ii) diminishes platelet function and inflammation, and (iii) decreases diastolic and systolic arterial pressures. Data currently available indicate that daily consumption of cocoa-rich chocolate (rich in polyphenols) may at least partially lower cardiovascular disease risk. Further studies are required in order to establish the bioavailability and mechanisms of action of bioactive compounds in chocolate. The study of the interaction of chocolate and its components with candidate genes will also supply necessary information regarding the individuals best suited to benefit from a potential cardiovascular disease treatment with chocolate.

Development of polymethacrylate nanospheres as targeted delivery systems for catechin within the gastrointestinal tract

NASA Astrophysics Data System (ADS)

Pool, Hector; Luna-Barcenas, Gabriel; McClements, David Julian; Mendoza, Sandra

2017-09-01

In this study, pH-sensitive nanospheres were fabricated using a polymethacrylate-based copolymer to encapsulate, protect, and release catechin, and thereby overcome its poor water solubility and low oral bioaccessibility. The polymer used was a polymethacrylic acid-co-ethyl acrylate 1:1 copolymer that dissolves above pH 5.5, and so can be used to retain and protect bioactives within the stomach but releases them in the small intestine. Catechin-loaded nanospheres were fabricated using the solvent displacement method. Physicochemical characterization of the nanospheres indicated that they were relatively small ( d = 160 nm) and had a high negative charge ( ζ = - 36 mV), which meant that they had good stability to aggregation under physiological conditions (pH 7.2). Catechin was trapped within the nanospheres at an encapsulation efficiency of about 51% in an amorphous state. A simulated gastrointestinal study showed that catechin was slowly released under gastric conditions (pH 2.5), but rapidly released under small intestine conditions (pH 7.2). The observed improvement in the antioxidant activity and bioaccessibility of catechin after encapsulation was attributed to the fact that it was in an amorphous state and had good water dispersibility. This study provides useful information for the formulation of novel delivery systems to improve the dispersibility, bioaccessibility, and bioactivity of catechin and potentially other active components. These delivery systems could be used to improve the efficacy of bioactive components in foods, supplements, and pharmaceutical products.

The improvement of M1 polarization in macrophages by glycopeptide derived from Ganoderma lucidum.

PubMed

Sun, Li-Xin; Lin, Zhi-Bin; Lu, Jie; Li, Wei-Dong; Niu, Yan-Dong; Sun, Yu; Hu, Chen-Yang; Zhang, Guo-Qiang; Duan, Xin-Suo

2017-06-01

Ganoderma lucidum (Fr.) Karst (Ganodermataceae) is a medicinal mushroom that has been extensively used in China for centuries to promote longevity and improve vigor without significant adverse effects. There is continuous interest in the bioactive properties of G. lucidum in view of its newly developed popularity in other regions besides Asia, such as Europe. Glycopeptide derived from G. lucidum (Gl-PS) is one of the main effective components isolated from this mushroom. The Gl-PS has been demonstrated pleiotropic with many bioactivities including immunomodulatory and antitumor effects. Macrophages are important cells involved in innate and adaptive immunity. Classically activated macrophages (M1) and alternatively activated macrophages (M2), with their different roles, display distinct cytokine profiles: M1 preferentially produces TNF-α, IL-6, and IL-12; conversely, M2 generates more IL-10 and arginase. Gl-PS might have the potential to promote macrophage M1 polarization by lipopolysaccharide (LPS). In this study, LPS was used to induce the M1 polarization. It was shown that the level of the TNF-α, IL-6, and IL-12 were increased and the IL-10 and arginase I were decreased in the polarized M1 macrophages after application of Gl-PS compared to the control. The results indicated the potential of Gl-PS to promote M1 polarization vs M2, with the health beneficial understanding of the bioactivities of Gl-PS.

Bioactive natural constituents from food sources-potential use in hypertension prevention and treatment.

PubMed

Huang, Wu-Yang; Davidge, Sandra T; Wu, Jianping

2013-01-01

Prevention and management of hypertension are the major public health challenges worldwide. Uncontrolled high blood pressure may lead to a shortened life expectancy and a higher morbidity due to a high risk of cardiovascular complications such as coronary heart disease (which leads to heart attack) and stroke, congestive heart failure, heart rhythm irregularities, and kidney failure etc. In recent years, it has been recognized that many dietary constituents may contribute to human cardiovascular health. There has been an increased focus on identifying these natural components of foods, describing their physiological activities and mechanisms of actions. Grain, vegetables, fruits, milk, cheese, meat, chicken, egg, fish, soybean, tea, wine, mushrooms, and lactic acid bacteria are various food sources with potential antihypertensive effects. Their main bioactive constituents include angiotensin I-converting enzyme (ACE) inhibitory peptides, vitamins C and E, flavonoids, flavanols, cathecins, anthocyanins, phenolic acids, polyphenols, tannins, resveratrol, polysaccharides, fiber, saponin, sterols, as well as K, Ca, and P. They may reduce blood pressure by different mechanisms, such as ACE inhibition effect, antioxidant, vasodilatory, opiate-like, Ca(2+) channel blocking, and chymase inhibitory activities. These functional foods may provide new therapeutic applications for hypertension prevention and treatment, and contribute to a healthy cardiovascular population. The present review summarizes the antihypertensive food sources and their bioactive constituents, as well as physiological mechanisms of dietary products, especially focusing on ACE inhibitory activity.

An oral colon-targeting controlled release system based on resistant starch acetate: synthetization, characterization, and preparation of film-coating pellets.

PubMed

Pu, Huayin; Chen, Ling; Li, Xiaoxi; Xie, Fengwei; Yu, Long; Li, Lin

2011-05-25

An oral colon-targeting controlled release system based on resistant starch acetate (RSA) as a film-coating material was developed. The RSA was successfully synthesized, and its digestion resistibility could be improved by increasing the degree of substitution (DS), which was favorable for the colon-targeting purpose. As a delivery carrier material, the characteristics of RSA were investigated by polarized light microscopy, FTIR spectroscopy, and X-ray diffraction. The results revealed a decrease of the crystallinity of RSA and a change of its crystalline structure from B + V hydrid type to V type. To evaluate the colon-targeting release performance, the RSA film-coated pellets loaded with different bioactive components were prepared by extrusion-spheronization and then by fluid bed coating. The effects of the DS, plasticizer content, and coating thickness of the RSA film and those of the content and molecular weight of the loaded bioactive component on the colon-targeting release performance of the resulting delivery system were investigated. By adjusting the DS, the coating thickness, and the plasticizer content of the RSA film, either the pellets loaded with a small molecular bioactive component such as 5-aminosalicylic acid or those with a macromolecular bioactive peptide or protein such as bovine serum albumin, hepatocyte growth-promoting factor, or insulin showed a desirable colon-targeting release performance. The release percentage was less than 12% in simulated upper gastrointestinal tract and went up to 70% over a period of 40 h in simulated colonic fluid. This suggests that the delivery system based on RSA film has an excellent colon-targeting release performance and the universality for a wide range of bioactive components.

Metabolomics-Driven Nutraceutical Evaluation of Diverse Green Tea Cultivars

PubMed Central

Ida, Megumi; Kosaka, Reia; Miura, Daisuke; Wariishi, Hiroyuki; Maeda-Yamamoto, Mari; Nesumi, Atsushi; Saito, Takeshi; Kanda, Tomomasa; Yamada, Koji; Tachibana, Hirofumi

2011-01-01

Background Green tea has various health promotion effects. Although there are numerous tea cultivars, little is known about the differences in their nutraceutical properties. Metabolic profiling techniques can provide information on the relationship between the metabolome and factors such as phenotype or quality. Here, we performed metabolomic analyses to explore the relationship between the metabolome and health-promoting attributes (bioactivity) of diverse Japanese green tea cultivars. Methodology/Principal Findings We investigated the ability of leaf extracts from 43 Japanese green tea cultivars to inhibit thrombin-induced phosphorylation of myosin regulatory light chain (MRLC) in human umbilical vein endothelial cells (HUVECs). This thrombin-induced phosphorylation is a potential hallmark of vascular endothelial dysfunction. Among the tested cultivars, Cha Chuukanbohon Nou-6 (Nou-6) and Sunrouge (SR) strongly inhibited MRLC phosphorylation. To evaluate the bioactivity of green tea cultivars using a metabolomics approach, the metabolite profiles of all tea extracts were determined by high-performance liquid chromatography-mass spectrometry (LC-MS). Multivariate statistical analyses, principal component analysis (PCA) and orthogonal partial least-squares-discriminant analysis (OPLS-DA), revealed differences among green tea cultivars with respect to their ability to inhibit MRLC phosphorylation. In the SR cultivar, polyphenols were associated with its unique metabolic profile and its bioactivity. In addition, using partial least-squares (PLS) regression analysis, we succeeded in constructing a reliable bioactivity-prediction model to predict the inhibitory effect of tea cultivars based on their metabolome. This model was based on certain identified metabolites that were associated with bioactivity. When added to an extract from the non-bioactive cultivar Yabukita, several metabolites enriched in SR were able to transform the extract into a bioactive extract. Conclusions/Significance Our findings suggest that metabolic profiling is a useful approach for nutraceutical evaluation of the health promotion effects of diverse tea cultivars. This may propose a novel strategy for functional food design. PMID:21853132

At-line nanofractionation with parallel mass spectrometry and bioactivity assessment for the rapid screening of thrombin and factor Xa inhibitors in snake venoms.

PubMed

Mladic, Marija; Zietek, Barbara M; Iyer, Janaki Krishnamoorthy; Hermarij, Philip; Niessen, Wilfried M A; Somsen, Govert W; Kini, R Manjunatha; Kool, Jeroen

2016-02-01

Snake venoms comprise complex mixtures of peptides and proteins causing modulation of diverse physiological functions upon envenomation of the prey organism. The components of snake venoms are studied as research tools and as potential drug candidates. However, the bioactivity determination with subsequent identification and purification of the bioactive compounds is a demanding and often laborious effort involving different analytical and pharmacological techniques. This study describes the development and optimization of an integrated analytical approach for activity profiling and identification of venom constituents targeting the cardiovascular system, thrombin and factor Xa enzymes in particular. The approach developed encompasses reversed-phase liquid chromatography (RPLC) analysis of a crude snake venom with parallel mass spectrometry (MS) and bioactivity analysis. The analytical and pharmacological part in this approach are linked using at-line nanofractionation. This implies that the bioactivity is assessed after high-resolution nanofractionation (6 s/well) onto high-density 384-well microtiter plates and subsequent freeze drying of the plates. The nanofractionation and bioassay conditions were optimized for maintaining LC resolution and achieving good bioassay sensitivity. The developed integrated analytical approach was successfully applied for the fast screening of snake venoms for compounds affecting thrombin and factor Xa activity. Parallel accurate MS measurements provided correlation of observed bioactivity to peptide/protein masses. This resulted in identification of a few interesting peptides with activity towards the drug target factor Xa from a screening campaign involving venoms of 39 snake species. Besides this, many positive protease activity peaks were observed in most venoms analysed. These protease fingerprint chromatograms were found to be similar for evolutionary closely related species and as such might serve as generic snake protease bioactivity fingerprints in biological studies on venoms. Copyright © 2015 Elsevier Ltd. All rights reserved.

Large Soluble Oligomers of Amyloid β-Protein from Alzheimer Brain Are Far Less Neuroactive Than the Smaller Oligomers to Which They Dissociate

PubMed Central

Yang, Ting; Li, Shaomin; Xu, Huixin

2017-01-01

Soluble oligomers of amyloid β-protein (oAβ) isolated from the brains of Alzheimer's disease (AD) patients have been shown experimentally (in the absence of amyloid plaques) to impair hippocampal synaptic plasticity, decrease synapses, induce tau hyperphosphorylation and neuritic dystrophy, activate microglial inflammation, and impair memory in normal adult rodents. Nevertheless, there has been controversy about what types of oligomers actually confer these AD-like phenotypes. Here, we show that the vast majority of soluble Aβ species obtained from brains of humans who died with confirmed AD elute at high molecular weight (HMW) on nondenaturing size-exclusion chromatography. These species have little or no cytotoxic activity in several bioassays. However, incubation of HMW oAβ in mildly alkaline buffer led to their quantitative dissociation into low molecular weight oligomers (∼8–70 kDa), and these were now far more bioactive: they impaired hippocampal LTP, decreased neuronal levels of β2-adrenergic receptors, and activated microglia in wt mice in vivo. Thus, most soluble Aβ assemblies in AD cortex are large and inactive but under certain circumstances can dissociate into smaller, highly bioactive species. Insoluble amyloid plaques likely sequester soluble HMW oligomers, limiting their potential to dissociate. We conclude that conditions that destabilize HMW oligomers or retard the sequestration of their smaller, more bioactive components are important drivers of Aβ toxicity. Selectively targeting these small, cytotoxic forms should be therapeutically beneficial. SIGNIFICANCE STATEMENT Oligomers of amyloid β-protein (oAβ) are tought to play an important role in Alzheimer's disease (AD), but there is confusion and controversy about what types and sizes of oligomers have disease-relevant activity. Using size-exclusion chromatography and three distinct measures of bioactivity, we show that the predominant forms of Aβ in aqueous extracts of AD brain are high molecular weight (HMW) and relatively inactive. Importantly, under certain conditions, the abundant HMW oAβ can dissociate into low molecular weight species, and these low molecular weight oligomers are significantly more bioactive on synapses and microglia than the HMW species from which they are derived. We conclude that conditions that destabilize HMW oAβ or retard the sequestration of smaller, more bioactive components are important drivers of Aβ toxicity. PMID:28053038

Epigenetic diet: impact on the epigenome and cancer

PubMed Central

Hardy, Tabitha M; Tollefsbol, Trygve O

2011-01-01

A number of bioactive dietary components are of particular interest in the field of epigenetics. Many of these compounds display anticancer properties and may play a role in cancer prevention. Numerous studies suggest that a number of nutritional compounds have epigenetic targets in cancer cells. Importantly, emerging evidence strongly suggests that consumption of dietary agents can alter normal epigenetic states as well as reverse abnormal gene activation or silencing. Epigenetic modifications induced by bioactive dietary compounds are thought to be beneficial. Substantial evidence is mounting proclaiming that commonly consumed bioactive dietary factors act to modify the epigenome and may be incorporated into an ‘epigenetic diet’. Bioactive nutritional components of an epigenetic diet may be incorporated into one’s regular dietary regimen and used therapeutically for medicinal or chemopreventive purposes. This article will primarily focus on dietary factors that have been demonstrated to influence the epigenome and that may be used in conjunction with other cancer prevention and chemotherapeutic therapies. PMID:22022340

Organic-inorganic composites designed for biomedical applications.

PubMed

Miyazaki, Toshiki; Ishikawa, Kunio; Shirosaki, Yuki; Ohtsuki, Chikara

2013-01-01

Several varieties of ceramics, such as Bioglass-type glasses, sintered hydroxyapatite and glass-ceramic A-W, exhibit specific biological affinity, i.e., direct bonding to surrounding bone, when implanted in bony defects. These bone-bonding ceramics are called bioactive ceramics and are utilized as important bone substitutes in the medical field. However, there is a limitation to their clinical applications because of their inappropriate mechanical properties. Natural bone takes a kind of organic-inorganic composite, where apatite nanocrystals are precipitated on collagen fibers. Therefore, problems with the bioactive ceramics can be solved by material design based on the composites. In this paper, current research topics on the development of bioactive organic-inorganic composites inspired by actual bone microstructure have been reviewed in correlation with preparation methods and various properties. Several kinds of inorganic components have been found to exhibit bioactivity in the body environment. Combination of the inorganic components with various organic polymers enables the development of bioactive organic-inorganic composites. In addition, novel biomedical applications of the composites to drug delivery systems, scaffolds for tissue regeneration and injectable biomaterials are available by combining drugs or biological molecules with appropriate control of its microstructure.

Bioactive peptides derived from traditional Chinese medicine and traditional Chinese food: A review.

PubMed

Liu, Ming; Wang, Yunpu; Liu, Yuhuan; Ruan, Roger

2016-11-01

There is an urgent treat of numerous chronic diseases including heart disease, stroke, cancer, chronic respiratory diseases and diabetes, which have a significant influence on the health of people worldwide. In addition to numerous preventive and therapeutic drug treatments, important advances have been achieved in the identification of bioactive peptides that may contribute to long-term health. Although bioactive peptides with various biological activities received unprecedented attention, as a new source of bioactive peptides, the significant role of bioactive peptides from traditional Chinese medicine and traditional Chinese food has not fully appreciated compared to other bioactive components. Hence, identification and bioactivity assessment of these peptides could benefit the pharmaceutical and food industry. Furthermore, the functional properties of bioactive peptides help to demystify drug properties and health benefits of traditional Chinese medicine and traditional Chinese food. This paper reviews the generation and biofunctional properties of various bioactive peptides derived from traditional Chinese medicine and traditional Chinese food. Mechanisms of digestion, bioavailability of bioactive peptides and interactions between traditional Chinese medicine and traditional Chinese food are also summarized in this review. Copyright © 2016 Elsevier Ltd. All rights reserved.

Emerging concepts promising new horizons for marine biodiscovery and synthetic biology.

PubMed

Reen, F Jerry; Gutiérrez-Barranquero, José A; Dobson, Alan D W; Adams, Claire; O'Gara, Fergal

2015-05-13

The vast oceans of the world, which comprise a huge variety of unique ecosystems, are emerging as a rich and relatively untapped source of novel bioactive compounds with invaluable biotechnological and pharmaceutical potential. Evidence accumulated over the last decade has revealed that the diversity of marine microorganisms is enormous with many thousands of bacterial species detected that were previously unknown. Associated with this diversity is the production of diverse repertoires of bioactive compounds ranging from peptides and enzymes to more complex secondary metabolites that have significant bioactivity and thus the potential to be exploited for innovative biotechnology. Here we review the discovery and functional potential of marine bioactive peptides such as lantibiotics, nanoantibiotics and peptidomimetics, which have received particular attention in recent years in light of their broad spectrum of bioactivity. The significance of marine peptides in cell-to-cell communication and how this may be exploited in the discovery of novel bioactivity is also explored. Finally, with the recent advances in bioinformatics and synthetic biology, it is becoming clear that the integration of these disciplines with genetic and biochemical characterization of the novel marine peptides, offers the most potential in the development of the next generation of societal solutions.

Emerging Concepts Promising New Horizons for Marine Biodiscovery and Synthetic Biology

PubMed Central

Reen, F. Jerry; Gutiérrez-Barranquero, José A.; Dobson, Alan D. W.; Adams, Claire; O’Gara, Fergal

2015-01-01

The vast oceans of the world, which comprise a huge variety of unique ecosystems, are emerging as a rich and relatively untapped source of novel bioactive compounds with invaluable biotechnological and pharmaceutical potential. Evidence accumulated over the last decade has revealed that the diversity of marine microorganisms is enormous with many thousands of bacterial species detected that were previously unknown. Associated with this diversity is the production of diverse repertoires of bioactive compounds ranging from peptides and enzymes to more complex secondary metabolites that have significant bioactivity and thus the potential to be exploited for innovative biotechnology. Here we review the discovery and functional potential of marine bioactive peptides such as lantibiotics, nanoantibiotics and peptidomimetics, which have received particular attention in recent years in light of their broad spectrum of bioactivity. The significance of marine peptides in cell-to-cell communication and how this may be exploited in the discovery of novel bioactivity is also explored. Finally, with the recent advances in bioinformatics and synthetic biology, it is becoming clear that the integration of these disciplines with genetic and biochemical characterization of the novel marine peptides, offers the most potential in the development of the next generation of societal solutions. PMID:25984990

Littoral lichens as a novel source of potentially bioactive Actinobacteria.

PubMed

Parrot, Delphine; Antony-Babu, Sanjay; Intertaglia, Laurent; Grube, Martin; Tomasi, Sophie; Suzuki, Marcelino T

2015-10-30

Cultivable Actinobacteria are the largest source of microbially derived bioactive molecules. The high demand for novel antibiotics highlights the need for exploring novel sources of these bacteria. Microbial symbioses with sessile macro-organisms, known to contain bioactive compounds likely of bacterial origin, represent an interesting and underexplored source of Actinobacteria. We studied the diversity and potential for bioactive-metabolite production of Actinobacteria associated with two marine lichens (Lichina confinis and L. pygmaea; from intertidal and subtidal zones) and one littoral lichen (Roccella fuciformis; from supratidal zone) from the Brittany coast (France), as well as the terrestrial lichen Collema auriforme (from a riparian zone, Austria). A total of 247 bacterial strains were isolated using two selective media. Isolates were identified and clustered into 101 OTUs (98% identity) including 51 actinobacterial OTUs. The actinobacterial families observed were: Brevibacteriaceae, Cellulomonadaceae, Gordoniaceae, Micrococcaceae, Mycobacteriaceae, Nocardioidaceae, Promicromonosporaceae, Pseudonocardiaceae, Sanguibacteraceae and Streptomycetaceae. Interestingly, the diversity was most influenced by the selective media rather than lichen species or the level of lichen thallus association. The potential for bioactive-metabolite biosynthesis of the isolates was confirmed by screening genes coding for polyketide synthases types I and II. These results show that littoral lichens are a source of diverse potentially bioactive Actinobacteria.

Littoral lichens as a novel source of potentially bioactive Actinobacteria

PubMed Central

Parrot, Delphine; Antony-Babu, Sanjay; Intertaglia, Laurent; Grube, Martin; Tomasi, Sophie; Suzuki, Marcelino T.

2015-01-01

Cultivable Actinobacteria are the largest source of microbially derived bioactive molecules. The high demand for novel antibiotics highlights the need for exploring novel sources of these bacteria. Microbial symbioses with sessile macro-organisms, known to contain bioactive compounds likely of bacterial origin, represent an interesting and underexplored source of Actinobacteria. We studied the diversity and potential for bioactive-metabolite production of Actinobacteria associated with two marine lichens (Lichina confinis and L. pygmaea; from intertidal and subtidal zones) and one littoral lichen (Roccella fuciformis; from supratidal zone) from the Brittany coast (France), as well as the terrestrial lichen Collema auriforme (from a riparian zone, Austria). A total of 247 bacterial strains were isolated using two selective media. Isolates were identified and clustered into 101 OTUs (98% identity) including 51 actinobacterial OTUs. The actinobacterial families observed were: Brevibacteriaceae, Cellulomonadaceae, Gordoniaceae, Micrococcaceae, Mycobacteriaceae, Nocardioidaceae, Promicromonosporaceae, Pseudonocardiaceae, Sanguibacteraceae and Streptomycetaceae. Interestingly, the diversity was most influenced by the selective media rather than lichen species or the level of lichen thallus association. The potential for bioactive-metabolite biosynthesis of the isolates was confirmed by screening genes coding for polyketide synthases types I and II. These results show that littoral lichens are a source of diverse potentially bioactive Actinobacteria. PMID:26514347

Comparative analysis of main bio-active components in the herb pair Danshen-Honghua and its single herbs by ultra-high performance liquid chromatography coupled to triple quadrupole tandem mass spectrometry.

PubMed

Qu, Cheng; Pu, Zong-Jin; Zhou, Gui-Sheng; Wang, Jun; Zhu, Zhen-Hua; Yue, Shi-Jun; Li, Jian-Ping; Shang, Li-Li; Tang, Yu-Ping; Shi, Xu-Qin; Liu, Pei; Guo, Jian-Ming; Sun, Jing; Tang, Zhi-Shu; Zhao, Jing; Zhao, Bu-Chang; Duan, Jin-Ao

2017-09-01

A sensitive, reliable, and powerful ultra-high performance liquid chromatography coupled to triple quadrupole tandem mass spectrometry method was developed for simultaneous quantification of the 15 main bio-active components including phenolic acids and flavonoids within 13 min for the first time. The proposed method was first reported and validated by good linearity (r 2  > 0.9975), limit of detection (1.12-7.01 ng/mL), limit of quantification (3.73-23.37 ng/mL), intra- and inter-day precisions (RSD ≤ 1.92%, RSD ≤ 2.45%), stability (RSD ≤ 5.63%), repeatability (RSD ≤ 4.34%), recovery (96.84-102.12%), and matrix effects (0.92-1.02). The established analytical methodology was successfully applied to comparative analysis of main bio-active components in the herb pair Danshen-Honghua and its single herbs. Compared to the single herb, the content of most flavonoid glycosides was remarkably increased in their herb pair, and main phenolic acids were decreased, conversely. The content changes of the main components in the herb pair supported the synergistic effects on promoting blood circulation and removing blood stasis. The results provide a scientific basis and reference for the quality control of Danshen-Honghua herb pair and the drug interactions based on variation of bio-active components in herb pairs. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Revelation and cloning of valinomycin synthetase genes in Streptomyces lavendulae ACR-DA1 and their expression analysis under different fermentation and elicitation conditions.

PubMed

Sharma, Richa; Jamwal, Vijaylakshmi; Singh, Varun P; Wazir, Priya; Awasthi, Praveen; Singh, Deepika; Vishwakarma, Ram A; Gandhi, Sumit G; Chaubey, Asha

2017-07-10

Streptomyces species are amongst the most exploited microorganisms due to their ability to produce a plethora of secondary metabolites with bioactive potential, including several well known drugs. They are endowed with immense unexplored potential and substantial efforts are required for their isolation as well as characterization for their bioactive potential. Unexplored niches and extreme environments are host to diverse microbial species. In this study, we report Streptomyces lavendulae ACR-DA1, isolated from extreme cold deserts of the North Western Himalayas, which produces a macrolactone antibiotic, valinomycin. Valinomycin is a K + ionophoric non-ribosomal cyclodepsipeptide with a broad range of bioactivities including antibacterial, antifungal, antiviral and cytotoxic/anticancer activities. Production of valinomycin by the strain S. lavendulae ACR-DA1 was studied under different fermentation conditions like fermentation medium, temperature and addition of biosynthetic precursors. Synthetic medium at 10°C in the presence of precursors i.e. valine and pyruvate showed enhanced valinomycin production. In order to assess the impact of various elicitors, expression of the two genes viz. vlm1 and vlm2 that encode components of heterodimeric valinomycin synthetase, was analyzed using RT-PCR and correlated with quantity of valinomycin using LC-MS/MS. Annelid, bacterial and yeast elicitors increased valinomycin production whereas addition of fungal and plant elicitors down regulated the biosynthetic genes and reduced valinomycin production. This study is also the first report of valinomycin biosynthesis by Streptomyces lavendulae. Copyright © 2017 Elsevier B.V. All rights reserved.

Nutrients and certain lipid soluble bioactive components in dehusked whole grains (gota) and dehusked splits (dhal) from pigeon pea (Cajanus cajan) and their cooking characteristics.

PubMed

Jayadeep, Padmanabhan A; Sashikala, Vadakkoot B; Pratape, Vishwas M

2009-01-01

The nutritional quality of dehusked whole grains (gota) and dehusked splits (dhal) in red and white varieties of pigeon pea regarding proximate composition and certain lipid-soluble bioactive components was investigated. A decrease in fat and crude fiber was noticed when gota was converted to dhal. The lipid profile of gota and dhal from red and white husk pigeon pea types indicated that essential fatty acids were greater in gota than in their respective dhals. Gota from white husk variety contained more tocopherols than the red variety. Dhal contained less tocopherols than gota. A decrease in the content of gamma and alpha tocopherols, vitamin E activity and total antioxidant activity also indicates loss of bioactive components on splitting gota into dhal. Cooking time and dispersed solids on cooking indicated good cooking quality of gotta. The results indicated the nutritional superiority of gota over dhal and its similarity with dhal in cooking characteristics.

Electrophoretic co-deposition of cellulose nanocrystals-45S5 bioactive glass nanocomposite coatings on stainless steel

NASA Astrophysics Data System (ADS)

Chen, Qiang; Yang, Yuyun; Pérez de Larraya, Uxua; Garmendia, Nere; Virtanen, Sannakaisa; Boccaccini, Aldo R.

2016-01-01

An organic-inorganic nanocomposite coating consisting of fibrous cellulose nanocrystals and 45S5 bioactive glass, intended as a bioactive surface for bone implants, was developed by a one-step electrophoretic deposition. The composition, surface roughness and wettability of the deposited coatings, influenced by the concentration of each component in the suspension, were controllable as a result of the simplicity of the coating technique. Bioactive glass particles were individually wrapped with porous cellulose layers, forming a porous coating with uniform thickness. Bioactivity test in simulated body fluid revealed a rapid hydroxyapatite formation on the deposited nanocomposite coating. Furthermore, electrochemical test was carried out to understand the corrosion behavior of the deposited coatings during incubation in simulated body fluid. According to the results of this study, the obtained cellulose-bioactive glass coatings with tunable properties represent a promising approach for biofunctionalization of metallic orthopedic implants.

Chromatogram-Bioactivity Correlation-Based Discovery and Identification of Three Bioactive Compounds Affecting Endothelial Function in Ginkgo Biloba Extract.

PubMed

Liu, Hong; Tan, Li-Ping; Huang, Xin; Liao, Yi-Qiu; Zhang, Wei-Jian; Li, Pei-Bo; Wang, Yong-Gang; Peng, Wei; Wu, Zhong; Su, Wei-Wei; Yao, Hong-Liang

2018-05-03

Discovery and identification of three bioactive compounds affecting endothelial function in Ginkgo biloba Extract (GBE) based on chromatogram-bioactivity correlation analysis. Three portions were separated from GBE via D101 macroporous resin and then re-combined to prepare nine GBE samples. 21 compounds in GBE samples were identified through UFLC-DAD-Q-TOF-MS/MS. Correlation analysis between compounds differences and endothelin-1 (ET-1) in vivo in nine GBE samples was conducted. The analysis results indicated that three bioactive compounds had close relevance to ET-1: Kaempferol-3- O -α-l-glucoside, 3- O -{2- O -{6- O -[P-OH-trans-cinnamoyl]-β-d-glucosyl}-α-rhamnosyl} Quercetin isomers, and 3- O -{2- O -{6- O -[P-OH-trans-cinnamoyl]-β-d-glucosyl}-α-rhamnosyl} Kaempferide. The discovery of bioactive compounds could provide references for the quality control and novel pharmaceuticals development of GRE. The present work proposes a feasible chromatogram-bioactivity correlation based approach to discover the compounds and define their bioactivities for the complex multi-component systems.

Identification and Analysis of Bioactive Components of Fruit and Vegetable Products

ERIC Educational Resources Information Center

Mann, Francis M.

2015-01-01

Many small-molecule antioxidants found in whole fruits and vegetables are analyzed and identified in this laboratory module for upper-division biochemistry courses. During this experiment, students develop their knowledge of the bioactivity of fruit and vegetable products while learning techniques to identify vitamins and nutritionally derived…

Rice varietal differences in bioactive bran components for inhibition of colorectal cancer cell growth

USDA-ARS?s Scientific Manuscript database

Studies support that the bran fraction of rice contains bioactive compounds capable of inhibiting the formation of colonic tumors. Screening bran extracts from diverse rice varieties represents a novel approach to assessing the colon cancer chemopreventive properties of rice bran. We analyzed a pane...

Bio Prospecting of Marine-derived Streptomyces spectabilis VITJS10 and Exploring its Cytotoxicity Against Human Liver Cancer Cell Lines.

PubMed

Selvakumar, Jemimah Naine; Chandrasekaran, Subathra Devi; Vaithilingam, Mohanasrinivasan

2015-10-01

Recently, numerous pathogens have developed resistance due to the indiscriminate use of commercial therapeutic drugs. The main aim of the study was to evaluate the bioactive potential of the Streptomyces spectabilis VITJS10 crude extract. The S. spectabilis VITJS10 ethyl acetate extract was tested for antibacterial, antioxidant, and cytotoxic properties. Genotypic characterization was done using 16S r-DNA partial gene amplification and sequencing. The authenticity of the crude chemical constitutes were determined by gas chromatography-mass spectrometry (GC-MS). The antibacterial potential revealed the effective activity against Shigellaflexneri (MTCC No: 1457) (22 mm), Salmonella typhi (MTCC No: 1167) (23 mm), Escherichia coli (MTCC No: 1588) (22 mm), Pseudomonas aeruginosa (MTCC No: 4676) (22 mm) at 20 mg/mL concentration. Scavenging ability of the extract was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay revealing its 95% inhibition at 5 mg/mL concentration. Hepatocellular cancer cells (HepG2) cell line was used to evaluate the cytotoxicity by 3-(4, 5-dimethyl thiazol-2yl)-2, 5-diphenyl tetrazolium bromide assay. The extract showed maximum inhibition at IC50 of 250 μg/mL with 53.6% cell viability. The highest 16S rRNA gene sequence homogeneity was observed 99% similar with the novel strain S. spectabilis S3-1. The chemical components of the crude extract of VITJS10 were detected with 37 chemical constituents. However three major compounds were identified, namely Sulfurous acid, 2-ethylhexyl tridecyl ester, Phenol, 2,4-bis (1,1-dimethylethyl), and Trans-2-methyl-4-n-pentylthiane, S, S-Dioxide. Hence the present study justifies the overwhelming circumstantial evidence as the most bioactive metabolites from the marine origin, which has potential utilization in pharmaceutical industry. The aim of this study was to explore the bioactive potential of marine Streptomyces sp. isolated from marine soil and understand the bioactive properties of the crude extracts. It is clearly evident from the study that the bioactive metabolites produced by Streptomyces sp. exhibited good antibacterial, antioxidant and anticancer activity. Our results indicated that Starch casein medium was the good base for bioactive metabolite production. The taxonomic position of Streptomyces sp. isolated revealed unique pattern of phenotypic properties that distinguished it from representatives. The molecular characterization results provided valuable data for establishing the internal taxonomic structure of the genus. Hence high mortality rates, serious side effects, deficiencies of the available chemotherapeutics, and high costs during treatment clearly underscore the need to develop new anticancer agents, With the above significant features the strain could be recommended for its use in medicinal and agricultural sectors, an extensive knowledge on the behavior of natural compounds can be gained for the benefit of health.

Spices for Prevention and Treatment of Cancers

PubMed Central

Zheng, Jie; Zhou, Yue; Li, Ya; Xu, Dong-Ping; Li, Sha; Li, Hua-Bin

2016-01-01

Spices have been widely used as food flavorings and folk medicines for thousands of years. Numerous studies have documented the antioxidant, anti-inflammatory and immunomodulatory effects of spices, which might be related to prevention and treatment of several cancers, including lung, liver, breast, stomach, colorectum, cervix, and prostate cancers. Several spices are potential sources for prevention and treatment of cancers, such as Curcuma longa (tumeric), Nigella sativa (black cumin), Zingiber officinale (ginger), Allium sativum (garlic), Crocus sativus (saffron), Piper nigrum (black pepper) and Capsicum annum (chili pepper), which contained several important bioactive compounds, such as curcumin, thymoquinone, piperine and capsaicin. The main mechanisms of action include inducing apoptosis, inhibiting proliferation, migration and invasion of tumors, and sensitizing tumors to radiotherapy and chemotherapy. This review summarized recent studies on some spices for prevention and treatment of cancers, and special attention was paid to bioactive components and mechanisms of action. PMID:27529277

Spices for Prevention and Treatment of Cancers.

PubMed

Zheng, Jie; Zhou, Yue; Li, Ya; Xu, Dong-Ping; Li, Sha; Li, Hua-Bin

2016-08-12

Spices have been widely used as food flavorings and folk medicines for thousands of years. Numerous studies have documented the antioxidant, anti-inflammatory and immunomodulatory effects of spices, which might be related to prevention and treatment of several cancers, including lung, liver, breast, stomach, colorectum, cervix, and prostate cancers. Several spices are potential sources for prevention and treatment of cancers, such as Curcuma longa (tumeric), Nigella sativa (black cumin), Zingiber officinale (ginger), Allium sativum (garlic), Crocus sativus (saffron), Piper nigrum (black pepper) and Capsicum annum (chili pepper), which contained several important bioactive compounds, such as curcumin, thymoquinone, piperine and capsaicin. The main mechanisms of action include inducing apoptosis, inhibiting proliferation, migration and invasion of tumors, and sensitizing tumors to radiotherapy and chemotherapy. This review summarized recent studies on some spices for prevention and treatment of cancers, and special attention was paid to bioactive components and mechanisms of action.

Bioactivity, proximate, mineral and volatile profiles along the flowering stages of Opuntia microdasys (Lehm.): defining potential applications.

PubMed

Chahdoura, Hassiba; Barreira, João C M; Fernández-Ruiz, Virginia; Morales, Patricia; Calhelha, Ricardo C; Flamini, Guido; Soković, Marina; Ferreira, Isabel C F R; Achour, Lotfi

2016-03-01

Opuntia spp. flowers have been traditionally used for medical purposes, mostly because of their diversity in bioactive molecules with health promoting properties. The proximate, mineral and volatile compound profiles, together with the cytotoxic and antimicrobial properties were characterized in O. microdasys flowers at different maturity stages, revealing several statistically significant differences. O. microdasys stood out mainly for its high contents of dietary fiber, potassium and camphor, and its high activities against HCT15 cells, Staphylococcus aureus, Aspergillus versicolor and Penicillium funiculosum. The vegetative stage showed the highest cytotoxic and antifungal activities, whilst the full flowering stage was particularly active against bacterial species. The complete dataset has been classified by principal component analysis, achieving clearly identifiable groups for each flowering stage, elucidating also the most distinctive features, and comprehensively profiling each of the assayed stages. The results might be useful to define the best flowering stage considering practical application purposes.

Determination of bioactivity of chemical fractions of liquid wastes using freshwater and saltwater algae and crustaceans

DOE Office of Scientific and Technical Information (OSTI.GOV)

Walsh, G.E.; Garnas, R.L.

1983-03-01

Complex wastes from industrial and municipal outfalls were fractionated chemically and tested for toxicity with freshwater and saltwater algae and crustaceans. The organic fraction of each waste was subfractionated into acid-, base-, and neutral-extractable portions, and the inorganic fraction was subfractionated into its anion and cation components. All wastes affected growth of the algae Skeletonema costatum (saltwater) and Monoraphidium capricornutum (freshwater) or survival of Mysidopsis bahia (saltwater) and Daphnia magna (freshwater). Usually, bioactivity was limited to one or two subfractions. In some cases, algal growth was stimulated by a fraction or subfraction, whereas stimulation was not detected in whole waste.more » It is suggested that fractionation must be done in order to estimate the full potential impact of complex wastes on aquatic systems. The method can also be used to identify toxic factors before application of cost-effective control technology.« less

Applications of the Phytomedicine Echinacea purpurea (Purple Coneflower) in Infectious Diseases

PubMed Central

Hudson, James B.

2012-01-01

Extracts of Echinacea purpurea (EP, purple coneflower) have been used traditionally in North America for the treatment of various types of infections and wounds, and they have become very popular herbal medicines globally. Recent studies have revealed that certain standardized preparations contain potent and selective antiviral and antimicrobial activities. In addition, they display multiple immune-modulatory activities, comprising stimulation of certain immune functions such as phagocytic activity of macrophages and suppression of the proinflammatory responses of epithelial cells to viruses and bacteria, which are manifested as alterations in secretion of various cytokines and chemokines. These immune modulations result from upregulation or downregulation of the relevant genes and their transcription factors. All these bioactivities can be demonstrated at noncytotoxic concentrations of extract and appear to be due to multiple components rather than the individual chemical compounds that characterize Echinacea extracts. Potential applications of the bioactive extracts may go beyond their traditional uses. PMID:22131823

A chemical family-based strategy for uncovering hidden bioactive molecules and multicomponent interactions in herbal medicines.

PubMed

Song, Hui-Peng; Wu, Si-Qi; Hao, Haiping; Chen, Jun; Lu, Jun; Xu, Xiaojun; Li, Ping; Yang, Hua

2016-03-30

Two concepts involving natural products were proposed and demonstrated in this paper. (1) Natural product libraries (e.g. herbal extract) are not perfect for bioactivity screening because of the vast complexity of compound compositions, and thus a library reconstruction procedure is necessary before screening. (2) The traditional mode of "screening single compound" could be improved to "screening single compound, drug combination and multicomponent interaction" due to the fact that herbal medicines work by integrative effects of multi-components rather than single effective constituents. Based on the two concepts, we established a novel strategy aiming to make screening easier and deeper. Using thrombin as the model enzyme, we firstly uncovered the minor lead compounds, potential drug combinations and multicomponent interactions in an herbal medicine of Dan-Qi pair, showing a significant advantage over previous methods. This strategy was expected to be a new and promising mode for investigation of herbal medicines.

Expanding the biomass derived chemical space

PubMed Central

Brun, Nicolas; Hesemann, Peter

2017-01-01

Biorefinery aims at the conversion of biomass and renewable feedstocks into fuels and platform chemicals, in analogy to conventional oil refinery. In the past years, the scientific community has defined a number of primary building blocks that can be obtained by direct biomass decomposition. However, the large potential of this “renewable chemical space” to contribute to the generation of value added bio-active compounds and materials still remains unexplored. In general, biomass derived building blocks feature a diverse range of chemical functionalities. In order to be integrated into value-added compounds, they require additional functionalization and/or covalent modification thereby generating secondary building blocks. The latter can be thus regarded as functional components of bio-active molecules or materials and represent an expansion of the renewable chemical space. This perspective highlights the most recent developments and opportunities for the synthesis of secondary biomass derived building blocks and their application to the preparation of value added products. PMID:28959397

Promise of bitter melon (Momordica charantia) bioactives in cancer prevention and therapy

PubMed Central

Raina, Komal; Kumar, Dileep; Agarwal, Rajesh

2016-01-01

Recently, there is a paradigm shift that the whole food-derived components are not ‘idle bystanders’ but actively participate in modulating aberrant metabolic and signaling pathways in both healthy and diseased individuals. One such whole food from Cucurbitaceae family is ‘bitter melon’ (Momordica charantia, also called bitter gourd, balsam apple, etc.), which has gained an enormous attention in recent years as an alternative medicine in developed countries. The increased focus on bitter melon consumption could in part be due to several recent pre-clinical efficacy studies demonstrating bitter melon potential to target obesity/type II diabetes-associated metabolic aberrations as well as its pre-clinical anti-cancer efficacy against various malignancies. The bioassay-guided fractionations have also classified the bitter melon chemical constituents based on their anti-diabetic or cytotoxic effects. Thus, by definition, these bitter melon constituents are at cross roads on the bioactivity parameters; they either have selective efficacy for correcting metabolic aberrations or targeting cancer cells, or have beneficial effects in both conditions. However, given the vast, though dispersed, literature reports on the bioactivity and beneficial attributes of bitter melon constituents, a comprehensive review on the bitter melon components and the overlapping beneficial attributes is lacking; our review attempts to fulfill these unmet needs. Importantly, the recent realization that there are common risk factors associated with obesity/type II diabetes-associated metabolic aberrations and cancer, this timely review focuses on the dual efficacy of bitter melon against the risk factors associated with both diseases that could potentially impact the course of malignancy to advanced stages. Furthermore, this review also addresses a significant gap in our knowledge regarding the bitter melon drug-drug interactions which can be predicted from the available reports on bitter melon effects on metabolism enzymes and drug transporters. This has important implications, given that a large proportion of individuals, taking bitter melon based supplements/phytochemical extracts/food based home-remedies, are also likely to be taking conventional therapeutic drugs at the same time. Accordingly, the comprehensively reviewed information here could be prudently translated to the clinical implications associated with any potential concerns regarding bitter melon consumption by cancer patients. PMID:27452666

Promise of bitter melon (Momordica charantia) bioactives in cancer prevention and therapy.

PubMed

Raina, Komal; Kumar, Dileep; Agarwal, Rajesh

2016-10-01

Recently, there is a paradigm shift that the whole food-derived components are not 'idle bystanders' but actively participate in modulating aberrant metabolic and signaling pathways in both healthy and diseased individuals. One such whole food from Cucurbitaceae family is 'bitter melon' (Momordica charantia, also called bitter gourd, balsam apple, etc.), which has gained an enormous attention in recent years as an alternative medicine in developed countries. The increased focus on bitter melon consumption could in part be due to several recent pre-clinical efficacy studies demonstrating bitter melon potential to target obesity/type II diabetes-associated metabolic aberrations as well as its pre-clinical anti-cancer efficacy against various malignancies. The bioassay-guided fractionations have also classified the bitter melon chemical constituents based on their anti-diabetic or cytotoxic effects. Thus, by definition, these bitter melon constituents are at cross roads on the bioactivity parameters; they either have selective efficacy for correcting metabolic aberrations or targeting cancer cells, or have beneficial effects in both conditions. However, given the vast, though dispersed, literature reports on the bioactivity and beneficial attributes of bitter melon constituents, a comprehensive review on the bitter melon components and the overlapping beneficial attributes is lacking; our review attempts to fulfill these unmet needs. Importantly, the recent realization that there are common risk factors associated with obesity/type II diabetes-associated metabolic aberrations and cancer, this timely review focuses on the dual efficacy of bitter melon against the risk factors associated with both diseases that could potentially impact the course of malignancy to advanced stages. Furthermore, this review also addresses a significant gap in our knowledge regarding the bitter melon drug-drug interactions which can be predicted from the available reports on bitter melon effects on metabolism enzymes and drug transporters. This has important implications, given that a large proportion of individuals, taking bitter melon based supplements/phytochemical extracts/food based home-remedies, are also likely to be taking conventional therapeutic drugs at the same time. Accordingly, the comprehensively reviewed information here could be prudently translated to the clinical implications associated with any potential concerns regarding bitter melon consumption by cancer patients. Copyright © 2016 Elsevier Ltd. All rights reserved.

Bioactive Phytochemicals from Wild Arbutus unedo L. Berries from Different Locations in Portugal: Quantification of Lipophilic Components

PubMed Central

Fonseca, Daniela F. S.; Salvador, Ângelo C.; Santos, Sónia A. O.; Vilela, Carla; Freire, Carmen S. R.; Silvestre, Armando J. D.; Rocha, Sílvia M.

2015-01-01

The lipophilic composition of wild Arbutus unedo L. berries, collected from six locations in Penacova (center of Portugal), as well as some general chemical parameters, namely total soluble solids, pH, titratable acidity, total phenolic content and antioxidant activity was studied in detail to better understand its potential as a source of bioactive compounds. The chemical composition of the lipophilic extracts, focused on the fatty acids, triterpenoids, sterols, long chain aliphatic alcohols and tocopherols, was investigated by gas chromatography–mass spectrometry (GC–MS) analysis of the dichloromethane extracts. The lipophilic extractives of the ripe A. unedo berries ranged from 0.72% to 1.66% (w/w of dry weight), and consisted mainly of triterpenoids, fatty acids and sterols. Minor amounts of long chain aliphatic alcohols and tocopherols were also identified. Forty-one compounds were identified and among these, ursolic acid, lupeol, α-amyrin, linoleic and α-linolenic acids, and β-sitosterol were highlighted as the major components. To the best of our knowledge the current research study provides the most detailed phytochemical repository for the lipophilic composition of A. unedo, and offers valuable information for future valuation and exploitation of these berries. PMID:26110390

Human Milk Composition and Preservation: Evaluation of High-pressure Processing as a Nonthermal Pasteurization Technology.

PubMed

Sousa, Sílvia G; Delgadillo, Ivonne; Saraiva, Jorge A

2016-01-01

Human milk is seen not only as a food, but as a functional and dynamic biologic system. It provides nutrients, bioactive components, and immune factors, promoting adequate and healthy growth of newborn infants. When mothers cannot supply their children, donated breast milk is the nutrition recommended by the World Health Organization, as it is a better alternative than infant formula. However, because of the manner in which donor milk is handled in human milk banks (HMB) many of the properties ascribed to mother's own milk are diminished or destroyed. The major process responsible for these losses is Holder pasteurization. High-pressure processing (HPP) is a novel nonthermal pasteurization technology that is being increasingly applied in food industries worldwide, primarily as an alternative to thermal treatment. This is due to its capacity to inactivate microorganisms while preserving both nutritional and bioactive components of foods. This review describes human milk composition and preservation, and critically discusses HMB importance and practices, highlighting HPP as a potential nonthermal pasteurization technology for human milk preservation. HPP technology is described and the few currently existing studies of its effects in human milk are presented.

Essential Oil of Aristolochia trilobata: Synthesis, Routes of Exposure, Acute Toxicity, Binary Mixtures and Behavioral Effects on Leaf-Cutting Ants.

PubMed

de Oliveira, Bruna Maria S; Melo, Carlisson R; Alves, Péricles B; Santos, Abraão A; Santos, Ane Caroline C; Santana, Alisson da S; Araújo, Ana Paula A; Nascimento, Pedro E S; Blank, Arie F; Bacci, Leandro

2017-02-25

Plants of the genus Aristolochia have been frequently reported as important medicinal plants. Despite their high bioactive potential, to date, there are no reports of their effects on leaf-cutting ants. Therefore, the present study aimed to evaluate the insecticidal activity of the essential oil of Aristolochia trilobata and its major components on Atta sexdens and Acromyrmex balzani , two species of leaf-cutting ants. The bioassays were performed regarding routes of exposure, acute toxicity, binary mixtures of the major components and behavioral effects. Twenty-five components were identified in the essential oil of A. trilobata using a gas chromatographic system equipped with a mass spectrometer and a flame ionization detector. The components found in higher proportions were sulcatyl acetate, limonene, p -cymene and linalool. The essential oil of A. trilobata and its individual major components were efficient against A. balzani and A. sexdens workers when applied by fumigation. These components showed fast and efficient insecticidal activity on ants. The components acted synergistically and additively on A. balzani and A. sexdens , respectively, and caused a strong repellency/irritability in the ants. Thus, our results demonstrate the great potential of the essential oil of A. trilobata and its major components for the development of new insecticides.

Method and product for phosphosilicate slurry for use in dentistry and related bone cements

DOEpatents

Wagh, Arun S.; Primus, Carolyn

2006-08-01

The present invention is directed to magnesium phosphate ceramics and their methods of manufacture. The composition of the invention is produced by combining a mixture of a substantially dry powder component with a liquid component. The substantially dry powder component comprises a sparsely soluble oxide powder, an alkali metal phosphate powder, a sparsely soluble silicate powder, with the balance of the substantially dry powder component comprising at least one powder selected from the group consisting of bioactive powders, biocompatible powders, fluorescent powders, fluoride releasing powders, and radiopaque powders. The liquid component comprises a pH modifying agent, a monovalent alkali metal phosphate in aqueous solution, the balance of the liquid component being water. The use of calcined magnesium oxide as the oxide powder and hydroxylapatite as the bioactive powder produces a self-setting ceramic that is particularly suited for use in dental and orthopedic applications.

Effects of medium components and culture conditions on mycelial biomass and the production of bioactive ingredients in submerged culture of Xylaria nigripes (Ascomycetes), a Chinese medicinal fungus.

PubMed

Chen, Jian-Zhi; Lo, Hui-Chen; Lin, Fang-Yi; Chang, Shih-Liang; Hsieh, Changwei; Liang, Zeng-Chin; Ho, Wai-Jane; Hsu, Tai-Hao

2014-01-01

The optimal culture conditions were investigated to maximize the production of mycelial biomass and bioactive ingredients in submerged cultivation of Xylaria nigripes, a Chinese medicinal fungus. The one-factor-at-a-time method was used to explore the effects of medium components, including carbon, nitrogen, mineral sources, and initial pH of the medium and environmental factors, such as culture temperature and rotation speed, on mycelial growth and production of bioactive ingredients. The results indicated that the optimal culture temperature and rotation speed were 25°C and 100 rpm in a medium with 20 g fructose, 6 g yeast extract, and 2 g magnesiun sulfate heptahydrate as carbon, nitrogen, and mineral sources, respectively, in 1 L distilled water with an initial medium pH of 5.5. With optimal medium components and conditions of cultivation, the maximal production of mycelial biomass was 6.64 ± 0.88 g/L, with maximal production of bioactive ingredients such as extracellular polysaccharides (2.36 ± 0.18 mg/mL), intracellular polysaccharides (2.38 ± 0.07 mg/g), adenosine (43.27 ± 2.37 mg/g), total polyphenols (36.57 ± 1.36 mg/g), and triterpenoids (31.29 ± 1.17 mg/g) in a shake flask culture. These results suggest that different bioactive ingredients including intracellular polysaccharides, adenosine, total polyphenols and triterpenoids in mycelia and extracellular polysaccharides in broth can be obtained from one simple medium for submerged cultivation of X. nigripes.

BIOPEP database and other programs for processing bioactive peptide sequences.

PubMed

Minkiewicz, Piotr; Dziuba, Jerzy; Iwaniak, Anna; Dziuba, Marta; Darewicz, Małgorzata

2008-01-01

This review presents the potential for application of computational tools in peptide science based on a sample BIOPEP database and program as well as other programs and databases available via the World Wide Web. The BIOPEP application contains a database of biologically active peptide sequences and a program enabling construction of profiles of the potential biological activity of protein fragments, calculation of quantitative descriptors as measures of the value of proteins as potential precursors of bioactive peptides, and prediction of bonds susceptible to hydrolysis by endopeptidases in a protein chain. Other bioactive and allergenic peptide sequence databases are also presented. Programs enabling the construction of binary and multiple alignments between peptide sequences, the construction of sequence motifs attributed to a given type of bioactivity, searching for potential precursors of bioactive peptides, and the prediction of sites susceptible to proteolytic cleavage in protein chains are available via the Internet as are other approaches concerning secondary structure prediction and calculation of physicochemical features based on amino acid sequence. Programs for prediction of allergenic and toxic properties have also been developed. This review explores the possibilities of cooperation between various programs.

Sphingosine 1-phosphate, present in serum-derived lipoproteins, activates matriptase.

PubMed

Benaud, Christelle; Oberst, Michael; Hobson, John P; Spiegel, Sarah; Dickson, Robert B; Lin, Chen-Yong

2002-03-22

We describe here a novel biological function of sphingosine 1-phosphate (S1P): the activation of a serine protease, matriptase. Matriptase is a type II integral membrane serine protease, expressed on the surface of a variety of epithelial cells; it may play an important role in tissue remodeling. We have previously reported that the activation of matriptase is regulated by serum. We have now identified the bioactive component from serum. First, the activity was observed to co-purify with lipoproteins by conventional liquid chromatography and immunoaffinity chromatography. The ability of lipoproteins to induce the activation of matriptase was further confirmed with commercial preparations of low density lipoprotein (LDL) and very low density lipoprotein (VLDL). Next, we observed that the bioactive component of LDL is associated with the phospholipid components of LDL. Fractionation of lipid components of LDL by thin layer chromatography (TLC) revealed that the bioactive component of LDL comigrates with S1P. Nanomolar concentrations of commercially obtained S1P were then observed to induce the rapid activation of matriptase on the surfaces of nontransformed human mammary epithelial cells. Other structurally related sphingolipids, including dihydro-S1P, ceramide 1-phosphates, and sphingosine phosphocholine as well as lysophosphatidic acid, can also induce the activation of matriptase, but at significantly higher concentrations than S1P. Furthermore, S1P-dependent matriptase activation is dependent on Ca(2+) but not via G(i) protein-coupled receptors. Our results demonstrate that bioactive phospholipids can function as nonprotein activators of a cell surface protease, suggesting a possible mechanistic link between S1P and normal and possibly pathologic tissue remodeling.

Bioactive Compounds in Some Culinary Aromatic Herbs and Their Effects on Human Health.

PubMed

Guiné, Raquel P F; Gonçalves, Fernando J

2016-01-01

Culinary herbs are herbaceous (leafy) plants that add flavour and colour to all types of meals. There is a wide variety of herbs that are used for culinary purposes worldwide, which are also recognized for their beneficial health effects, and thus have also been used in folk medicine. Besides their nutritional value herbs are rich in many phytochemical components with bioactive effects, thus improving human health. The aim of the present work was to make a general overview of some of these herbs, including their gastronomic usage, their chemical composition in bioactive components and their reported health effects. This work showed that the health effects are very diverse and differ according to the herb in question. However, some of the most frequently citted biological activities include antioxidant, antimicrobial, and antiviral effects.

In vitro antiproliferative/cytotoxic activity on cancer cell lines of a cardanol and a cardol enriched from Thai Apis mellifera propolis.

PubMed

Teerasripreecha, Dungporn; Phuwapraisirisan, Preecha; Puthong, Songchan; Kimura, Kiyoshi; Okuyama, Masayuki; Mori, Haruhide; Kimura, Atsuo; Chanchao, Chanpen

2012-03-30

Propolis is a complex resinous honeybee product. It is reported to display diverse bioactivities, such as antimicrobial, anti-inflammatory and anti-tumor properties, which are mainly due to phenolic compounds, and especially flavonoids. The diversity of bioactive compounds depends on the geography and climate, since these factors affect the floral diversity. Here, Apis mellifera propolis from Nan province, Thailand, was evaluated for potential anti-cancer activity. Propolis was sequentially extracted with methanol, dichloromethane and hexane and the cytotoxic activity of each crude extract was assayed for antiproliferative/cytotoxic activity in vitro against five human cell lines derived from duet carcinoma (BT474), undifferentiated lung (Chaco), liver hepatoblastoma (Hep-G(2)), gastric carcinoma (KATO-III) and colon adenocarcinoma (SW620) cancers. The human foreskin fibroblast cell line (Hs27) was used as a non-transformed control. Those crude extracts that displayed antiproliferative/cytotoxic activity were then further fractionated by column chromatography using TLC-pattern and MTT-cytotoxicity bioassay guided selection of the fractions. The chemical structure of each enriched bioactive compound was analyzed by nuclear magnetic resonance and mass spectroscopy. The crude hexane and dichloromethane extracts of propolis displayed antiproliferative/cytotoxic activities with IC(50) values across the five cancer cell lines ranging from 41.3 to 52.4 μg/ml and from 43.8 to 53.5 μg/ml, respectively. Two main bioactive components were isolated, one cardanol and one cardol, with broadly similar in vitro antiproliferation/cytotoxicity IC(50) values across the five cancer cell lines and the control Hs27 cell line, ranging from 10.8 to 29.3 μg/ml for the cardanol and < 3.13 to 5.97 μg/ml (6.82 - 13.0 μM) for the cardol. Moreover, both compounds induced cytotoxicity and cell death without DNA fragmentation in the cancer cells, but only an antiproliferation response in the control Hs27 cells However, these two compounds did not account for the net antiproliferation/cytotoxic activity of the crude extracts suggesting the existence of other potent compounds or synergistic interactions in the propolis extracts. This is the first report that Thai A. mellifera propolis contains at least two potentially new compounds (a cardanol and a cardol) with potential anti-cancer bioactivity. Both could be alternative antiproliferative agents for future development as anti-cancer drugs.

Enhanced bioactivity, biocompatibility and mechanical behavior of strontium substituted bioactive glasses.

PubMed

Arepalli, Sampath Kumar; Tripathi, Himanshu; Hira, Sumit Kumar; Manna, Partha Pratim; Pyare, Ram; S P Singh

2016-12-01

Strontium contained biomaterials have been reported as a potential bioactive material for bone regeneration, as it reduces bone resorption and stimulates bone formation. In the present investigation, the bioactive glasses were designed to partially substitute SrO for SiO2 in Na2O-CaO-SrO-P2O5-SiO2 system. This work demonstrates that the substitution of SrO for SiO2 has got significant benefit than substitution for CaO in the bioactive glass. Bioactivity was assessed by the immersion of the samples in simulated body fluid for different intervals. The formation of hydroxy carbonate apatite layer was identified by X-ray diffractometry, scanning electron microscopy (SEM) and energy dispersive spectroscopy. The elastic modulus of the bioactive glasses was measured and found to increase with increasing SrO for SiO2. The blood compatibility of the samples was evaluated. In vitro cell culture studies of the samples were performed using human osteosarcoma U2-OS cell lines and found a significant improvement in cell viability and proliferation. The investigation showed enhancement in bioactivity, mechanical and biological properties of the strontia substituted for silica in glasses. Thus, these bioactive glasses would be highly potential for bone regeneration. Copyright © 2016 Elsevier B.V. All rights reserved.

Investigating the protective properties of milk phospholipids against ultraviolet light exposure in a skin equivalent model

NASA Astrophysics Data System (ADS)

Russell, Ashley; Laubscher, Andrea; Jimenez-Flores, Rafael; Laiho, Lily H.

2010-02-01

Current research on bioactive molecules in milk has documented health advantages of bovine milk and its components. Milk Phospholipids, selected for this study, represent molecules with great potential benefit in human health and nutrition. In this study we used confocal reflectance and multiphoton microscopy to monitor changes in skin morphology upon skin exposure to ultraviolet light and evaluate the potential of milk phospholipids in preventing photodamage to skin equivalent models. The results suggest that milk phospholipids act upon skin cells in a protective manner against the effect of ultraviolet (UV) radiation. Similar results were obtained from MTT tissue viability assay and histology.

Bioactive focus in conformational ensembles: a pluralistic approach

NASA Astrophysics Data System (ADS)

Habgood, Matthew

2017-12-01

Computational generation of conformational ensembles is key to contemporary drug design. Selecting the members of the ensemble that will approximate the conformation most likely to bind to a desired target (the bioactive conformation) is difficult, given that the potential energy usually used to generate and rank the ensemble is a notoriously poor discriminator between bioactive and non-bioactive conformations. In this study an approach to generating a focused ensemble is proposed in which each conformation is assigned multiple rankings based not just on potential energy but also on solvation energy, hydrophobic or hydrophilic interaction energy, radius of gyration, and on a statistical potential derived from Cambridge Structural Database data. The best ranked structures derived from each system are then assembled into a new ensemble that is shown to be better focused on bioactive conformations. This pluralistic approach is tested on ensembles generated by the Molecular Operating Environment's Low Mode Molecular Dynamics module, and by the Cambridge Crystallographic Data Centre's conformation generator software.

Comparative Developmental Toxicity of Flavonoids Using an Integrative Zebrafish System

PubMed Central

Bugel, Sean M.; Bonventre, Josephine A.; Tanguay, Robert L.

2016-01-01

Flavonoids are a large, structurally diverse class of bioactive naturally occurring chemicals commonly detected in breast milk, soy based infant formulas, amniotic fluid, and fetal cord blood. The potential for pervasive early life stage exposures raises concerns for perturbation of embryogenesis, though developmental toxicity and bioactivity information is limited for many flavonoids. Therefore, we evaluated a suite of 24 flavonoid and flavonoid-like chemicals using a zebrafish embryo-larval toxicity bioassay—an alternative model for investigating developmental toxicity of environmentally relevant chemicals. Embryos were exposed to 1–50 µM of each chemical from 6 to 120 h postfertilization (hpf), and assessed for 26 adverse developmental endpoints at 24, 72, and 120 hpf. Behavioral changes were evaluated in morphologically normal animals at 24 and 72 hpf, at 120 hpf using a larval photomotor response (LPR) assay. Gene expression was comparatively evaluated for all compounds for effects on biomarker transcripts indicative of AHR (cyp1a) and ER (cyp19a1b, esr1, lhb, vtg) pathway bioactivity. Overall, 15 of 24 flavonoids elicited adverse effects on one or more of the developmental or behavioral endpoints. Hierarchical clustering and principle component analyses compared toxicity profiles and identified 3 distinct groups of bioactive flavonoids. Despite robust induction of multiple estrogen-responsive biomarkers, co-exposure with ER and GPER antagonists did not ameliorate toxicity, suggesting ER-independence and alternative modes of action. Taken together, these studies demonstrate that development is sensitive to perturbation by bioactive flavonoids in zebrafish that are not related to traditional estrogen receptor mode of action pathways. This integrative zebrafish platform provides a useful framework for evaluating flavonoid developmental toxicity and hazard prioritization. PMID:27492224

Lippia origanoides chemotype differentiation based on essential oil GC-MS and principal component analysis.

PubMed

Stashenko, Elena E; Martínez, Jairo R; Ruíz, Carlos A; Arias, Ginna; Durán, Camilo; Salgar, William; Cala, Mónica

2010-01-01

Chromatographic (GC/flame ionization detection, GC/MS) and statistical analyses were applied to the study of essential oils and extracts obtained from flowers, leaves, and stems of Lippia origanoides plants, growing wild in different Colombian regions. Retention indices, mass spectra, and standard substances were used in the identification of 139 substances detected in these essential oils and extracts. Principal component analysis allowed L. origanoides classification into three chemotypes, characterized according to their essential oil major components. Alpha- and beta-phellandrenes, p-cymene, and limonene distinguished chemotype A; carvacrol and thymol were the distinctive major components of chemotypes B and C, respectively. Pinocembrin (5,7-dihydroxyflavanone) was found in L. origanoides chemotype A supercritical fluid (CO(2)) extract at a concentration of 0.83+/-0.03 mg/g of dry plant material, which makes this plant an interesting source of an important bioactive flavanone with diverse potential applications in cosmetic, food, and pharmaceutical products.

Current Strategies to Improve the Bioactivity of PEEK

PubMed Central

Ma, Rui; Tang, Tingting

2014-01-01

The synthetic thermoplastic polymer polyetheretherketone (PEEK) is becoming a popular component of clinical orthopedic and spinal applications, but its practical use suffers from several limitations. Although PEEK is biocompatible, chemically stable, radiolucent and has an elastic modulus similar to that of normal human bone, it is biologically inert, preventing good integration with adjacent bone tissues upon implantation. Recent efforts have focused on increasing the bioactivity of PEEK to improve the bone-implant interface. Two main strategies have been used to overcome the inert character of PEEK. One approach is surface modification to activate PEEK through surface treatment alone or in combination with a surface coating. Another strategy is to prepare bioactive PEEK composites by impregnating bioactive materials into PEEK substrate. Researchers believe that modified bioactive PEEK will have a wide range of orthopedic applications. PMID:24686515

Bioactives from microalgal dinoflagellates.

PubMed

Gallardo-Rodríguez, J; Sánchez-Mirón, A; García-Camacho, F; López-Rosales, L; Chisti, Y; Molina-Grima, E

2012-01-01

Dinoflagellate microalgae are an important source of marine biotoxins. Bioactives from dinoflagellates are attracting increasing attention because of their impact on the safety of seafood and potential uses in biomedical, toxicological and pharmacological research. Here we review the potential applications of dinoflagellate toxins and the methods for producing them. Only sparing quantities of dinoflagellate toxins are generally available and this hinders bioactivity characterization and evaluation in possible applications. Approaches to production of increased quantities of dinoflagellate bioactives are discussed. Although many dinoflagellates are fragile and grow slowly, controlled culture in bioreactors appears to be generally suitable for producing many of the metabolites of interest. Copyright © 2012 Elsevier Inc. All rights reserved.

Isolation and characterization of bioactive fungi from shark Carcharodon carcharias' gill with biopharmaceutical prospects

NASA Astrophysics Data System (ADS)

Zhang, Yi; Han, Jinyuan; Feng, Yan; Mu, Jun; Bao, Haiyan; Kulik, Andreas; Grond, Stephanie

2016-01-01

Until recently, little was known about the fungi found in shark gills and their biomedicinal potential. In this article, we described the isolation, bioactivity, diversity, and secondary metabolites of bioactive fungi from the gill of a shark ( Carcharodon carcharias). A total of 115 isolates were obtained and grown in 12 culture media. Fifty-eight of these isolates demonstrated significant activity in four antimicrobial, pesticidal, and cytotoxic bioassay models. Four randomly selected bioactive isolates inhibited human cancer cell proliferation during re-screening. These active isolates were segregated into 6 genera using the internal transcribed spacer-large subunit (ITS-LSU) rDNA-sequence BLAST comparison. Four genera, Penicillium, Aspergillus, Mucor, and Chaetomium were the dominant taxa. A phylogenic tree illustrated their intergenera and intragenera genetic diversity. HPLC-DAD-HRMS analysis and subsequent database searching revealed that nine representative strains produced diverse bioactive compound profiles. These results detail the broad range of bioactive fungi found in a shark's gills, revealing their biopharmaceutical potential. To the best of our knowledge, this is the first study characterizing shark gill fungi and their bioactivity.

Garcinia morella fruit, a promising source of antioxidant and anti-inflammatory agents induces breast cancer cell death via triggering apoptotic pathway.

PubMed

Choudhury, Bhaswati; Kandimalla, Raghuram; Elancheran, R; Bharali, Rupjyoti; Kotoky, Jibon

2018-04-17

A rapid rise in cancer cases worldwide, especially breast cancer in females, instigates the need for more effective and less side effect causing drugs from natural origin. Thereby, in the present study, Garcinia morella fruit was investigated for antioxidant, anti-inflammatory and anti-breast cancer activity. Preliminary antioxidant and anticancer evaluation of different fractions and crude methanol extract of G. morella fruit suggested chloroform fraction as the bioactive fraction. Time course analysis (by 24 h, 48 h and 72 h) of the bioactive fraction (1.56-25) μg/ml treatment on breast cancer cell lines (MCF7, MDAMB231 and SKBR3) showed dose and time dependent antiproliferative responses. Further, mechanistic studies involving morphological observation and western blotting analysis, revealed its apoptosis inducing effect on breast cancer. P53 dependent up-regulation of Bax and down-regulation of Bcl X L is suggested as the possible pathway of apoptosis followed by MCF7 cells on exposure to the bioactive fraction. The anti-inflammatory assays revealed that it significantly lowered the release of nitrite and TNF-α level of LPS induced RAW 264.7 cells (p < 0.05). Moreover, pre treatment of Carrageenan induced paw edema animals with 20 mg/kg of the bioactive fraction significantly (p < 0.05) inhibited paw inflammation and controlled the cytokine and nitrite levels of the edema induced rat. Its main bioactive component was identified to be Garcinol by UHPLC and ESI-MS/MS. Thereby, this study clearly reflects that G. morella fruit is a valuable antioxidant and anti-inflammatory gift of nature with the potential to be used against breast cancer. This is also the first report of isolation of bioactive compound Garcinol from G. morella fruit. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Drug target identification using network analysis: Taking active components in Sini decoction as an example

NASA Astrophysics Data System (ADS)

Chen, Si; Jiang, Hailong; Cao, Yan; Wang, Yun; Hu, Ziheng; Zhu, Zhenyu; Chai, Yifeng

2016-04-01

Identifying the molecular targets for the beneficial effects of active small-molecule compounds simultaneously is an important and currently unmet challenge. In this study, we firstly proposed network analysis by integrating data from network pharmacology and metabolomics to identify targets of active components in sini decoction (SND) simultaneously against heart failure. To begin with, 48 potential active components in SND against heart failure were predicted by serum pharmacochemistry, text mining and similarity match. Then, we employed network pharmacology including text mining and molecular docking to identify the potential targets of these components. The key enriched processes, pathways and related diseases of these target proteins were analyzed by STRING database. At last, network analysis was conducted to identify most possible targets of components in SND. Among the 25 targets predicted by network analysis, tumor necrosis factor α (TNF-α) was firstly experimentally validated in molecular and cellular level. Results indicated that hypaconitine, mesaconitine, higenamine and quercetin in SND can directly bind to TNF-α, reduce the TNF-α-mediated cytotoxicity on L929 cells and exert anti-myocardial cell apoptosis effects. We envisage that network analysis will also be useful in target identification of a bioactive compound.

Drug target identification using network analysis: Taking active components in Sini decoction as an example

PubMed Central

Chen, Si; Jiang, Hailong; Cao, Yan; Wang, Yun; Hu, Ziheng; Zhu, Zhenyu; Chai, Yifeng

2016-01-01

Identifying the molecular targets for the beneficial effects of active small-molecule compounds simultaneously is an important and currently unmet challenge. In this study, we firstly proposed network analysis by integrating data from network pharmacology and metabolomics to identify targets of active components in sini decoction (SND) simultaneously against heart failure. To begin with, 48 potential active components in SND against heart failure were predicted by serum pharmacochemistry, text mining and similarity match. Then, we employed network pharmacology including text mining and molecular docking to identify the potential targets of these components. The key enriched processes, pathways and related diseases of these target proteins were analyzed by STRING database. At last, network analysis was conducted to identify most possible targets of components in SND. Among the 25 targets predicted by network analysis, tumor necrosis factor α (TNF-α) was firstly experimentally validated in molecular and cellular level. Results indicated that hypaconitine, mesaconitine, higenamine and quercetin in SND can directly bind to TNF-α, reduce the TNF-α-mediated cytotoxicity on L929 cells and exert anti-myocardial cell apoptosis effects. We envisage that network analysis will also be useful in target identification of a bioactive compound. PMID:27095146

A review on the ethnomedicinal uses, phytochemistry and pharmacology of Alpinia officinarum Hance.

PubMed

Abubakar, Ibrahim Babangida; Malami, Ibrahim; Yahaya, Yakubu; Sule, Sahabi Manga

2018-05-25

Alpinia officinarum Hance is a perennial plant that has been traditionally used for many decades to treat several ailments including inflammation, pain, stomach-ache, cold, amongst others. Pharmacological studies over the years have demonstrated remarkable bioactivities that could be further explored for development of new therapeutic agents against various ailments. The paper critically reviewed the ethno-medicinal uses, pharmacology, and phytochemistry of A. officinarum. Keywords including A. officinarum and its synonyms were searched using electronic databases including ISI web of knowledge, Science direct, Scopus, PubMed, Google scholar and relevant database for Masters and Doctoral theses. A. officinarum is prepared in Asia, Turkey, Morocco and Iran as a decoction, infusion or juice as a single preparation or in combination with other herbs, food or drinks for the treatment of general health problems including cold, inflammation, digestive disorders, etc. Pharmacological studies revealed the potent in vitro and in vivo bioactivities of various parts of A. officinarum that include anti-inflammatory, cytotoxicity, homeostasis, lipid regulation, antioxidant, antiviral, antimicrobial, antiosteoporosis, etc. Over 90 phytochemical constituents have been identified and isolated from A. officinarum comprising vastly of phenolic compounds especially diarylheptanoids isolated from the rhizome and considered the most active bioactive components. In vitro and in vivo studies have confirmed the potency of A. officinarum. However, further studies are required to establish the mechanisms mediating its bioactivities in relation to the medicinal uses as well as investigating any potential toxicity for future clinical studies. Copyright © 2018 Elsevier B.V. All rights reserved.

Bitter gourd (Momordica charantia) as a rich source of bioactive components to combat cancer naturally: Are we on the right track to fully unlock its potential as inhibitor of deregulated signaling pathways.

PubMed

Farooqi, Ammad Ahmad; Khalid, Sumbul; Tahir, Fatima; Sabitaliyevich, Uteuliev Yerzhan; Yaylim, Ilhan; Attar, Rukset; Xu, Baojun

2018-05-10

Research over decades has progressively explored pharmacological actions of bitter gourd (Momordica charantia). Biologically and pharmacologically active molecules isolated from M. charantia have shown significant anti-cancer activity in cancer cell lines and xenografted mice. In this review spotlight was set on the bioactive compounds isolated from M. charantia that effectively inhibited cancer development and progression via regulation of protein network in cancer cells. We summarize most recent high-quality research work in cancer cell lines and xenografted mice related to tumor suppressive role-play of M. charantia and its bioactive compounds. Although M. charantia mediated health promoting, anti-diabetic, hepatoprotective, anti-inflammatory effects have been extensively investigated, there is insufficient information related to regulation of signaling networks by bioactive molecules obtained from M. charantia in different cancers. M. charantia has been shown to modulate AKT/mTOR/p70S6K signaling, p38MAPK-MAPKAPK-2/HSP-27 pathway, cell cycle regulatory proteins and apoptosis-associated proteins in different cancers. However, still there are visible knowledge gaps related to the drug targets in different cancers because we have not yet developed comprehensive understanding of the M. charantia mediated regulation of signal transduction pathways. To explore these questions, experimental platforms are needed that can prove to be helpful in getting a step closer to personalized medicine. Copyright © 2018 Elsevier Ltd. All rights reserved.

Integrative Approach to Analyze Biodiversity and Anti-Inflammatory Bioactivity of Wedelia Medicinal Plants

PubMed Central

Chen, Yung-Hsiang; Hsiao, Pei-Wen; Liao, Jiunn-Wang; Peng, Ching-I; Yang, Ning-Sun

2015-01-01

For the development of “medical foods” and/or botanical drugs as defined USA FDA, clear and systemic characterizations of the taxonomy, index phytochemical components, and the functional or medicinal bioactivities of the reputed or candidate medicinal plant are needed. In this study, we used an integrative approach, including macroscopic and microscopic examination, marker gene analysis, and chemical fingerprinting, to authenticate and validate various species/varieties of Wedelia, a reputed medicinal plant that grows naturally and commonly used in Asian countries. The anti-inflammatory bioactivities of Wedelia extracts were then evaluated in a DSS-induced murine colitis model. Different species/varieties of Wedelia exhibited distinguishable morphology and histological structures. Analysis of the ribosomal DNA internal transcribed spacer (ITS) region revealed significant differences among these plants. Chemical profiling of test Wedelia species demonstrated candidate index compounds and distinguishable secondary metabolites, such as caffeic acid derivatives, which may serve as phytochemical markers or index for quality control and identification of specific Wedelia species. In assessing their effect on treating DSS induced-murine colitis, we observed that only the phytoextract from W. chinensis species exhibited significant anti-inflammatory bioactivity on DSS-induced murine colitis among the various Wedelia species commonly found in Taiwan. Our results provide a translational research approach that may serve as a useful reference platform for biotechnological applications of traditional phytomedicines. Our findings indicate that specific Wedelia species warrant further investigation for potential treatment of human inflammatory bowel disease. PMID:26042672

Integrative approach to analyze biodiversity and anti-inflammatory bioactivity of Wedelia medicinal plants.

PubMed

Lin, Wen-Ching; Wen, Chih-Chun; Chen, Yung-Hsiang; Hsiao, Pei-Wen; Liao, Jiunn-Wang; Peng, Ching-I; Yang, Ning-Sun

2015-01-01

For the development of "medical foods" and/or botanical drugs as defined USA FDA, clear and systemic characterizations of the taxonomy, index phytochemical components, and the functional or medicinal bioactivities of the reputed or candidate medicinal plant are needed. In this study, we used an integrative approach, including macroscopic and microscopic examination, marker gene analysis, and chemical fingerprinting, to authenticate and validate various species/varieties of Wedelia, a reputed medicinal plant that grows naturally and commonly used in Asian countries. The anti-inflammatory bioactivities of Wedelia extracts were then evaluated in a DSS-induced murine colitis model. Different species/varieties of Wedelia exhibited distinguishable morphology and histological structures. Analysis of the ribosomal DNA internal transcribed spacer (ITS) region revealed significant differences among these plants. Chemical profiling of test Wedelia species demonstrated candidate index compounds and distinguishable secondary metabolites, such as caffeic acid derivatives, which may serve as phytochemical markers or index for quality control and identification of specific Wedelia species. In assessing their effect on treating DSS induced-murine colitis, we observed that only the phytoextract from W. chinensis species exhibited significant anti-inflammatory bioactivity on DSS-induced murine colitis among the various Wedelia species commonly found in Taiwan. Our results provide a translational research approach that may serve as a useful reference platform for biotechnological applications of traditional phytomedicines. Our findings indicate that specific Wedelia species warrant further investigation for potential treatment of human inflammatory bowel disease.

Design of bone-integrating organic-inorganic composite suitable for bone repair.

PubMed

Miyazaki, Toshiki

2013-01-01

Several ceramics exhibit specific biological affinity, i.e. direct bone integration, when implanted in bony defects. They are called bioactive ceramics and utilized as important bone substitutes. However, there is limitation on clinical application, because of their inappropriate mechanical properties such as high Young's modulus and low fracture toughness. Novel bioactive materials exhibiting high machinability and flexibility have been desired in medical fields. Mixing bioactive ceramic powders and organic polymers have developed various organic-inorganic composites. Their mechanical property and bioactivity are mainly governed by the ceramics content. It is known that bioactive ceramics integrate with the bone through bone-like hydroxyapatite layer formed on their surfaces by chemical reaction with body fluid. This is triggered by a catalytic effect of various functional groups. On the basis of these facts, novel bioactive organic-inorganic nanocomposites have been developed. In these composites, inorganic components effective for triggering the hydroxyapatite nucleation are dispersed in polymer matrix at molecular level. Concept of the organic-inorganic composite is also applicable for providing polymethyl methacrylate (PMMA) bone cement with the bioactivity.

A validated high performance liquid chromatograph-photodiode array method for simultaneous determination of 10 bioactive components in compound hongdoushan capsule

PubMed Central

Zhu, Liancai; Yang, Xian; Tan, Jun; Wang, Bochu; Zhang, Xue

2014-01-01

Background: The compound Hongdoushan capsule (CHC) is widely known as compound herbal preparation and is often used to treat ovarian cancer and breast cancer, and to enhance the body immunity, etc., in clinical practice. Objective: To determine simultaneously 10 bioactive components from CHC, namely glycyrrhetinic acid, liquiritin, glycyrrhizin, baccatin III, 10-deacetylbaccatin III, cephalomannine, taxol, ginsenoside Rg1, ginsenoside Re, and ginsenoside Rb1. Materials and Methods: A high performance liquid chromatograph method coupled with photodiode array detector was developed and validated for the 1st time. Chromatographic analysis was performed on a SHIMADZU C18 by utilizing a gradient elution program. The mobile phase was acetonitrile (A)-water (B) at a flow rate of 0.8 mL/min. Results: The calibration curve was linear over the investigated concentration ranges with the values of r2 higher than 0.9993 for all the 10 bioactive components. The average recovery rates range from 98.4% to 100.5% with relative standard deviations ≤2.9%. The developed method was successfully applied to analyze 10 compounds in six CHC samples from different batches. In addition, the herbal sources of 32 chromatographic peaks were identified through comparative studying on chromatograms of standard, the respective extracts of Hongdoushan, RenShen, GanCao, and CHC. Conclusion: All the results imply that the accurate and reproducible method developed has high separation rate and enables the determination of 10 bioactive components in a single run for the quality control of CHC. PMID:24696551

Bioactive factors in milk across lactation: maternal effects and influence on infant growth in rhesus macaques (Macaca mulatta)

PubMed Central

Bernstein, Robin; Hinde, Katie

2017-01-01

Among mammals, numerous bioactive factors in milk vary across mothers and influence offspring outcomes. This emerging area of research has primarily investigated such dynamics within rodent biomedical models, domesticated dairy breeds, and among humans in clinical contexts. Less understood are signaling factors in the milk of non-human primates. Here, we report on multiple bioactive components in rhesus macaque (Macaca mulatta) milk and their associations with maternal and infant characteristics. Milk samples were collected from 59 macaques at multiple time points across lactation in conjunction with maternal and infant morphometrics and life-history animal records. Milk was assayed for adiponectin (APN), epidermal growth factor (EGF) and its receptor (EGF-R), and transforming growth factor beta 2 (TGF-β2). Regression models were constructed to assess the contributions of maternal factors on variation in milk bioactives, and on the relationship of this variation to infant body mass and growth. Maternal body mass, parity, social rank and infant sex were all predictive of concentrations of milk bioactives. Primiparous mothers produced milk with higher adiponectin, but lower EGF, than multiparous mothers. Heavier mothers produced milk with lower EGF and EGF-R, but higher TGF-β2. Mothers of daughters produced milk with higher TGF-β2. Mid-ranking mothers produced milk with higher mean EGF and adiponectin concentrations than low-ranking mothers. Milk EGF and EGF-R were positively associated with infant body mass and growth rate. Importantly, these signaling bioactives (APN, EGF, EGF-R, TGF-β2) were significantly correlated with nutritional values of milk. The effects of milk signals remained after controlling for the available energy in milk revealing the added physiological role of non-nutritive milk bioactives in the developing infant. Integrating analyses of energetic and other bioactive components of milk yields an important perspective for interpreting the magnitude, sources, and consequences of inter-individual variation in milk synthesis. PMID:27029025

Differential release of manure-borne bioactive P Forms to runoff and leachate under simulated rain

USDA-ARS?s Scientific Manuscript database

Limited information exist on the release of bioactive forms of P to runoff from a distinct manure layer, without the confounding effects of properties of the underlying soil in manure-amended fields to predict and model P partitioning and environmental behavior of the component P species. A study o...

Composition and biological activities of hydrolyzable tannins of fruits of Phyllanthus emblica.

PubMed

Yang, Baoru; Liu, Pengzhan

2014-01-22

Fruits of emblic leafflower have been used as food and traditional medicine in Asia. A wide range of biological activities have been shown in modern research suggesting potential of the fruits as healthy food and raw material for bioactive ingredients of food. Hydrolyzable tannins are among the major bioactive components of the fruits. Mucic acid gallate, mucic acid lactone gallate, monogalloylglucose, gallic acid, digalloylglucose, putranjivain A, galloyl-HHDP-glucose, elaeocarpusin, and chebulagic acid are the most abundant hydrolyzable tannins. The compositional profiles of tannins in the fruits vary depending on the cultivars as well as ripening stages. Fruits and tannin-rich extracts of fruits have shown antidiabetic, antimicrobial, anti-inflammatory, and immune-regulating activities in vitro and in animal studies. The fruits and fruit extracts have manifested protective effects on organs/tissues from damages induced by chemicals, stresses, and aging in animal models. The fruits and fruit extracts have potential in inhibiting the growth of cancer cells and reducing DNA damage induced by chemicals and radiation. Antioxidative activities are likely among the mechanisms of the biological activities and physiological effects. Human intervention/clinical studies are needed to investigate the bioavailability and metabolism of the tannins and to substantiate the health benefits in humans. Emblic leafflower may be a potential raw material for natural food preservatives.

Applications for α-lactalbumin in human nutrition.

PubMed

Layman, Donald K; Lönnerdal, Bo; Fernstrom, John D

2018-06-01

α-Lactalbumin is a whey protein that constitutes approximately 22% of the proteins in human milk and approximately 3.5% of those in bovine milk. Within the mammary gland, α-lactalbumin plays a central role in milk production as part of the lactose synthase complex required for lactose formation, which drives milk volume. It is an important source of bioactive peptides and essential amino acids, including tryptophan, lysine, branched-chain amino acids, and sulfur-containing amino acids, all of which are crucial for infant nutrition. α-Lactalbumin contributes to infant development, and the commercial availability of α-lactalbumin allows infant formulas to be reformulated to have a reduced protein content. Likewise, because of its physical characteristics, which include water solubility and heat stability, α-lactalbumin has the potential to be added to food products as a supplemental protein. It also has potential as a nutritional supplement to support neurological function and sleep in adults, owing to its unique tryptophan content. Other components of α-lactalbumin that may have usefulness in nutritional supplements include the branched-chain amino acid leucine, which promotes protein accretion in skeletal muscle, and bioactive peptides, which possess prebiotic and antibacterial properties. This review describes the characteristics of α-lactalbumin and examines the potential applications of α-lactalbumin for human health.

Applications for α-lactalbumin in human nutrition

PubMed Central

Lönnerdal, Bo; Fernstrom, John D

2018-01-01

Abstract α-Lactalbumin is a whey protein that constitutes approximately 22% of the proteins in human milk and approximately 3.5% of those in bovine milk. Within the mammary gland, α-lactalbumin plays a central role in milk production as part of the lactose synthase complex required for lactose formation, which drives milk volume. It is an important source of bioactive peptides and essential amino acids, including tryptophan, lysine, branched-chain amino acids, and sulfur-containing amino acids, all of which are crucial for infant nutrition. α-Lactalbumin contributes to infant development, and the commercial availability of α-lactalbumin allows infant formulas to be reformulated to have a reduced protein content. Likewise, because of its physical characteristics, which include water solubility and heat stability, α-lactalbumin has the potential to be added to food products as a supplemental protein. It also has potential as a nutritional supplement to support neurological function and sleep in adults, owing to its unique tryptophan content. Other components of α-lactalbumin that may have usefulness in nutritional supplements include the branched-chain amino acid leucine, which promotes protein accretion in skeletal muscle, and bioactive peptides, which possess prebiotic and antibacterial properties. This review describes the characteristics of α-lactalbumin and examines the potential applications of α-lactalbumin for human health. PMID:29617841

Marine bioactives and potential application in sports.

PubMed

Gammone, Maria Alessandra; Gemello, Eugenio; Riccioni, Graziano; D'Orazio, Nicolantonio

2014-04-30

An enriched diet with antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic compounds, has always been suggested to improve oxidative stress, preventing related diseases. In this respect, marine natural product (MNP), such as COX inhibitors, marine steroids, molecules interfering with factors involved in the modulation of gene expression (such as NF-κB), macrolides, many antioxidant agents, thermogenic substances and even substances that could help the immune system and that result in the protection of cartilage, have been recently gaining attention. The marine world represents a reserve of bioactive ingredients, with considerable potential as functional food. Substances, such as chitin, chitosan, n-3 oils, carotenoids, vitamins, minerals and bioactive peptides, can provide several health benefits, such as the reduction of cardiovascular diseases, anti-inflammatory and anticarcinogenic activities. In addition, new marine bioactive substances with potential anti-inflammatory, antioxidant and thermogenic capacity may provide health benefits and performance improvement, especially in those who practice physical activity, because of their increased free radical and Reacting Oxygen Species (ROS) production during exercise, and, particularly, in athletes. The aim of this review is to examine the potential pharmacological properties and application of many marine bioactive substances in sports.

Marine Bioactives and Potential Application in Sports

PubMed Central

Gammone, Maria Alessandra; Gemello, Eugenio; Riccioni, Graziano; D’Orazio, Nicolantonio

2014-01-01

An enriched diet with antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic compounds, has always been suggested to improve oxidative stress, preventing related diseases. In this respect, marine natural product (MNP), such as COX inhibitors, marine steroids, molecules interfering with factors involved in the modulation of gene expression (such as NF-κB), macrolides, many antioxidant agents, thermogenic substances and even substances that could help the immune system and that result in the protection of cartilage, have been recently gaining attention. The marine world represents a reserve of bioactive ingredients, with considerable potential as functional food. Substances, such as chitin, chitosan, n-3 oils, carotenoids, vitamins, minerals and bioactive peptides, can provide several health benefits, such as the reduction of cardiovascular diseases, anti-inflammatory and anticarcinogenic activities. In addition, new marine bioactive substances with potential anti-inflammatory, antioxidant and thermogenic capacity may provide health benefits and performance improvement, especially in those who practice physical activity, because of their increased free radical and Reacting Oxygen Species (ROS) production during exercise, and, particularly, in athletes. The aim of this review is to examine the potential pharmacological properties and application of many marine bioactive substances in sports. PMID:24796298

Piper betle leaf extract affects the quorum sensing and hence virulence of Pseudomonas aeruginosa PAO1.

PubMed

Datta, Siraj; Jana, Debanjan; Maity, Tilak Raj; Samanta, Aveek; Banerjee, Rajarshi

2016-06-01

Quorum sensing (QS) plays an important role in virulence of Pseudomonas aeruginosa, blocking of QS ability are viewed as viable antimicrobial chemotherapy and which may prove to be a safe anti-virulent drug. Bioactive components from Piper betle have been reported to possess antimicrobial ability. This study envisages on the anti-QS properties of ethanolic extract of P. betle leaf (PbLE) using P. aeruginosa PAO1 as a model organism. A marked reduction in swarming, swimming, and twitching ability of the bacteria is demonstrated in presence of PbLE. The biofilm and pyocyanin production also shows a marked reduction in presence of PbLE, though it does not affect the bacterial growth. Thus, the studies hint on the possible effect of the bioactive components of PbLE on reducing the virulent ability of the bacteria; identification of bioactive compounds should be investigated further.

Isolation and bioactivities of a non-sericin component from cocoon shell silk sericin of the silkworm Bombyx mori.

PubMed

Wang, Hai-Yan; Wang, Yuan-Jing; Zhou, Li-Xia; Zhu, Lin; Zhang, Yu-Qing

2012-02-01

The cocoon shell of the silkworm Bombyx mori consists of silk fibroin fiber (70%) surrounded by a sericin layer made up of sericin (25%) and non-sericin (5%) components. The non-sericin component which consists of carbohydrate, salt, wax, flavonoids and derivatives is often overlooked in applied research into sericin and its hydrolysate. Here, sericin and non-sericin compounds were obtained from the sericin layer of five types of cocoon shell by means of degumming in water followed by extraction and separation in ethanol. These ethanol extracts were found to mainly contain flavonoids and free amino acids possessing scavenging activities of the 2,2-diphenyl -1-picrylhydrazyl (DPPH) free radical and inhibiting activities of tyrosinase, which were much greater than the corresponding activities of the purified sericin proteins. The extracts also strongly inhibited α-glucosidase while the sericins had no such activity. In particular, the inhibitory activities of the ethanol extract of Daizo cocoons were much greater than those of the other cocoons. The IC(50) values of the Daizo cocoons for DPPH free radicals, tyrosinase, and α-glucosidase were 170, 27, and 110 μg mL(-1), respectively. The bioactivities of the non-sericin component were much higher than the activity of sericin alone. In addition, the in vivo test showed preliminarily that the administration of the non-sericin component had effectively resistant activity against streptozocin (STZ) oxidation and that of the purified sericin could also evidently decrease the induction ratio of diabetic mice induced by STZ. Therefore, ethanol extract protocols of the sericin layer of cocoon shells provide a novel stock which, together with sericin protein, has potential uses in functional food, biotechnological and medical applications.

A one-step method to fabricate PLLA scaffolds with deposition of bioactive hydroxyapatite and collagen using ice-based microporogens

PubMed Central

Li, Jiashen; Chen, Yun; Mak, Arthur F.T.; Tuan, Rocky S.; Li, Lin; Li, Yi

2010-01-01

Porous poly(L-lactic acid) (PLLA) scaffolds with bioactive coatings were prepared by a novel one-step method. In this process, ice-based microporogens containing bioactive molecules, such as hydroxyapatite (HA) and collagen, served as both porogens to form the porous structure and vehicles to transfer the bioactive molecules to the inside of PLLA scaffolds in a single step. Based on scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) analysis, the bioactive components were found to be transferred successfully from the porogens to PLLA scaffolds evenly. Osteoblast cells were used to evaluate the cellular behaviors of the composite scaffolds. After 8 days culturing, MTT assay and alkaline phosphatase (ALP) activity results suggested that HA/collagen could improve the interactions between osteoblast cells and the polymeric scaffold. PMID:20004261

Three-dimensional, bioactive, biodegradable, polymer-bioactive glass composite scaffolds with improved mechanical properties support collagen synthesis and mineralization of human osteoblast-like cells in vitro.

PubMed

Lu, Helen H; El-Amin, Saadiq F; Scott, Kimberli D; Laurencin, Cato T

2003-03-01

In the past decade, tissue engineering-based bone grafting has emerged as a viable alternative to biological and synthetic grafts. The biomaterial component is a critical determinant of the ultimate success of the tissue-engineered graft. Because no single existing material possesses all the necessary properties required in an ideal bone graft, our approach has been to develop a three dimensional (3-D), porous composite of polylactide-co-glycolide (PLAGA) and 45S5 bioactive glass (BG) that is biodegradable, bioactive, and suitable as a scaffold for bone tissue engineering (PLAGA-BG composite). The objectives of this study were to examine the mechanical properties of a PLAGA-BG matrix, to evaluate the response of human osteoblast-like cells to the PLAGA-BG composite, and to evaluate the ability of the composite to form a surface calcium phosphate layer in vitro. Structural and mechanical properties of PLAGA-BG were measured, and the formation of a surface calcium phosphate layer was evaluated by surface analysis methods. The growth and differentiation of human osteoblast-like cells on PLAGA-BG were also examined. A hypothesis was that the combination of PLAGA with BG would result in a biocompatible and bioactive composite, capable of supporting osteoblast adhesion, growth and differentiation, with mechanical properties superior to PLAGA alone. The addition of bioactive glass granules to the PLAGA matrix resulted in a structure with higher compressive modulus than PLAGA alone. Moreover, the PLAGA-BA composite was found to be a bioactive material, as it formed surface calcium phosphate deposits in a simulated body fluid (SBF), and in the presence of cells and serum proteins. The composite supported osteoblast-like morphology, stained positively for alkaline phosphatase, and supported higher levels of Type I collagen synthesis than tissue culture polystyrene controls. We have successfully developed a degradable, porous, polymer bioactive glass composite possessing improved mechanical properties and osteointegrative potential compared to degradable polymers of poly(lactic acid-glycolic acid) alone. Future work will focus on the optimization of the composite scaffold for bone tissue-engineering applications and the evaluation of the 3-D composite in an in vivo model. Copyright 2003 Wiley Periodicals, Inc.

Sources and Bioactive Properties of Conjugated Dietary Fatty Acids.

PubMed

Hennessy, Alan A; Ross, Paul R; Fitzgerald, Gerald F; Stanton, Catherine

2016-04-01

The group of conjugated fatty acids known as conjugated linoleic acid (CLA) isomers have been extensively studied with regard to their bioactive potential in treating some of the most prominent human health malignancies. However, CLA isomers are not the only group of potentially bioactive conjugated fatty acids currently undergoing study. In this regard, isomers of conjugated α-linolenic acid, conjugated nonadecadienoic acid and conjugated eicosapentaenoic acid, to name but a few, have undergone experimental assessment. These studies have indicated many of these conjugated fatty acid isomers commonly possess anti-carcinogenic, anti-adipogenic, anti-inflammatory and immune modulating properties, a number of which will be discussed in this review. The mechanisms through which these bioactivities are mediated have not yet been fully elucidated. However, existing evidence indicates that these fatty acids may play a role in modulating the expression of several oncogenes, cell cycle regulators, and genes associated with energy metabolism. Despite such bioactive potential, interest in these conjugated fatty acids has remained low relative to the CLA isomers. This may be partly attributed to the relatively recent emergence of these fatty acids as bioactives, but also due to a lack of awareness regarding sources from which they can be produced. In this review, we will also highlight the common sources of these conjugated fatty acids, including plants, algae, microbes and chemosynthesis.

Therapeutic Potential of Pterocarpus santalinus L.: An Update

PubMed Central

Bulle, Saradamma; Reddyvari, Hymavathi; Nallanchakravarthula, Varadacharyulu; Vaddi, Damodara Reddy

2016-01-01

Recently there has been increasing interest in plants and plant-derived compounds as raw food and medicinal agents. In Ayurveda, an Indian system of traditional medicine, a wide spectrum of medicinal properties of Pterocarpus santalinus is described. Many important bioactive phytocompounds have been extracted and identified from the heartwood of P. santalinus. Bioactive compounds typically occur in small amounts and have more subtle effects than nutrients. These bioactive compounds influence cellular activities that modify the risk of disease rather than prevent deficiency diseases. A wide array of biological activities and potential health benefits of P. santalinus have been reported, including antioxidative, antidiabetic, antimicrobial, anticancer, and anti-inflammatory properties, and protective effects on the liver, gastric mucosa, and nervous system. All these protective effects were attributed to bioactive compounds present in P. santalinus. The major bioactive compounds present in the heartwood of P. santalinus are santalin A and B, savinin, calocedrin, pterolinus K and L, and pterostilbenes. The bioactive compounds have potentially important health benefits: These compounds can act as antioxidants, enzyme inhibitors and inducers, inhibitors of receptor activities, and inducers and inhibitors of gene expression, among other actions. The present review aims to understand the pharmacological effects of P. santalinus on health and disease with “up-to-date” discussion. PMID:27041873

Therapeutic Potential of Pterocarpus santalinus L.: An Update.

PubMed

Bulle, Saradamma; Reddyvari, Hymavathi; Nallanchakravarthula, Varadacharyulu; Vaddi, Damodara Reddy

2016-01-01

Recently there has been increasing interest in plants and plant-derived compounds as raw food and medicinal agents. In Ayurveda, an Indian system of traditional medicine, a wide spectrum of medicinal properties of Pterocarpus santalinus is described. Many important bioactive phytocompounds have been extracted and identified from the heartwood of P. santalinus. Bioactive compounds typically occur in small amounts and have more subtle effects than nutrients. These bioactive compounds influence cellular activities that modify the risk of disease rather than prevent deficiency diseases. A wide array of biological activities and potential health benefits of P. santalinus have been reported, including antioxidative, antidiabetic, antimicrobial, anticancer, and anti-inflammatory properties, and protective effects on the liver, gastric mucosa, and nervous system. All these protective effects were attributed to bioactive compounds present in P. santalinus. The major bioactive compounds present in the heartwood of P. santalinus are santalin A and B, savinin, calocedrin, pterolinus K and L, and pterostilbenes. The bioactive compounds have potentially important health benefits: These compounds can act as antioxidants, enzyme inhibitors and inducers, inhibitors of receptor activities, and inducers and inhibitors of gene expression, among other actions. The present review aims to understand the pharmacological effects of P. santalinus on health and disease with "up-to-date" discussion.

Facial Regioselective Synthesis of Novel Bioactive Spiropyrrolidine/Pyrrolizine-Oxindole Derivatives via a Three Components Reaction as Potential Antimicrobial Agents.

PubMed

Hassaneen, Huwaida M E; Eid, Elshimaa M; Eid, Hamid A; Farghaly, Thoraya A; Mabkhot, Yahia Nasser

2017-02-26

This article presents the synthesis of new derivatives of spirooxindole-spiropiperidinone- pyrrolidines 6a - j and spirooxindole-spiropiperidinone-pyrrolizines 8a - j, through a 1,3-dipolar cycloaddition reaction of azomethineylides generated from isatin, sarcosine, and l-proline, through a decarboxylative route with dipolarophile 4a - j . All of the newly synthesized compounds were evaluated for their antimicrobial activities and their minimum inhibitory concentration (MIC) against most of the test organisms. The tested compounds displayed excellent activity against all of the tested microorganisms.

Novel Methods to Generate Active Ingredients-Enriched Ashwagandha Leaves and Extracts.

PubMed

Kaul, Sunil C; Ishida, Yoshiyuki; Tamura, Kazuya; Wada, Teruo; Iitsuka, Tomoko; Garg, Sukant; Kim, Mijung; Gao, Ran; Nakai, Shoichi; Okamoto, Youji; Terao, Keiji; Wadhwa, Renu

2016-01-01

Ashwagandha (Withania somnifera) is an Ayurvedic herb commonly used in world-renowned traditional Indian home medicine system. Roots of Ashwagandha have been traditionally known to possess a variety of therapeutic and health promoting potentials that have not been sufficiently supported by laboratory studies. Nevertheless, most, if not all, of the preventive and therapeutic potentials have been assigned to its bioactive components, steroidal alkaloids and lactones. In contrast to the traditional use of roots, we have been exploring bioactivities in leaves of Ashwagandha. Here, we report that the leaves possess higher content of active Withanolides, Withaferin-A (Wi-A) and Withanone (Wi-N), as compared to the roots. We also established, for the first time, hydroponic cultivation of Ashwagandha and investigated the effect of various cultivation conditions on the content of Wi-A and Wi-N by chemical analysis and bioassays. We report that the Withanone/Withaferin A-rich leaves could be obtained by manipulating light condition during hydroponic cultivation. Furthermore, we recruited cyclodextrins to prepare extracts with desired ratio of Wi-N and Wi-A. Hydroponically grown Ashwagandha and its extracts with high ratio of withanolides are valuable for cancer treatment.

Chemopreventive role of food-derived proteins and peptides: A review.

PubMed

Hernández-Ledesma, Blanca; Hsieh, Chia-Chien

2017-07-24

Cancer is one of the leading causes of mortality and disability worldwide. Although great advances in cancer treatments such as chemotherapy, surgery, and radiation are currently being achieved, their application is associated with numerous and expensive adverse side effects. Epidemiological evidence has demonstrated that the consumption of certain foods potentially prevents up to 35% of cancer cases. Bioactive components are ubiquitous in nature, also in dietary food, providing an essential link in health maintenance, promotion, and prevention of chronic diseases, such as cancer. Development of bioactive proteins and peptides is a current and innovative strategy for cancer prevention/cure. A growing body of anticancer protein and peptides from natural sources has shown the ability to reduce tumor progression through multiple mechanisms including apoptotic, antiproliferative, antiangiogenic, and immunomodulatory activities. This review is focused on proteins and peptides from different food sources including plants, milk, egg, and marine organisms in which chemopreventive properties have been demonstrated. Other aspects such as mechanism of action, bioavailability, and identification and characterization of food-derived peptides by advance separated technologies are also included. This review highlights the potential application of food-derived peptides as functional food ingredients and pharmaceutical candidates in the auxiliary therapy of cancer.

Novel Methods to Generate Active Ingredients-Enriched Ashwagandha Leaves and Extracts

PubMed Central

Kaul, Sunil C.; Ishida, Yoshiyuki; Tamura, Kazuya; Wada, Teruo; Iitsuka, Tomoko; Garg, Sukant; Kim, Mijung; Gao, Ran; Nakai, Shoichi; Okamoto, Youji; Terao, Keiji; Wadhwa, Renu

2016-01-01

Ashwagandha (Withania somnifera) is an Ayurvedic herb commonly used in world-renowned traditional Indian home medicine system. Roots of Ashwagandha have been traditionally known to possess a variety of therapeutic and health promoting potentials that have not been sufficiently supported by laboratory studies. Nevertheless, most, if not all, of the preventive and therapeutic potentials have been assigned to its bioactive components, steroidal alkaloids and lactones. In contrast to the traditional use of roots, we have been exploring bioactivities in leaves of Ashwagandha. Here, we report that the leaves possess higher content of active Withanolides, Withaferin-A (Wi-A) and Withanone (Wi-N), as compared to the roots. We also established, for the first time, hydroponic cultivation of Ashwagandha and investigated the effect of various cultivation conditions on the content of Wi-A and Wi-N by chemical analysis and bioassays. We report that the Withanone/Withaferin A-rich leaves could be obtained by manipulating light condition during hydroponic cultivation. Furthermore, we recruited cyclodextrins to prepare extracts with desired ratio of Wi-N and Wi-A. Hydroponically grown Ashwagandha and its extracts with high ratio of withanolides are valuable for cancer treatment. PMID:27936030

Bioactivity tests of calcium phosphates with variant molar ratios of main components.

PubMed

Pluta, Klaudia; Sobczak-Kupiec, Agnieszka; Półtorak, Olga; Malina, Dagmara; Tyliszczak, Bożena

2018-03-09

Calcium phosphates constitute attractive materials of biomedical applications. Among them particular attention is devoted to bioactive hydroxyapatite (HAp) and bioresorbable tricalcium phosphate (TCP) that possess ability to bind to living bones and can be used clinically as important bone substitutes. Notably, in vivo bone bioactivity can be predicted from apatite formation of bone immersed in SBF fluids. Thus, analyses of behavior of calcium phosphates immersed in various bio fluids are of great importance. Recently, stoichiometric HAp and TCP structures have been widely studied, whereas only limited number of publications have been devoted to analyses of nonstoichiometric calcium phosphates. Here, we report physicochemical analysis of natural and synthetic phosphates with variable Ca/P molar ratios. Subsequently attained structures were subjected to incubation in either artificial saliva or Ringer's fluids. Both pH and conductivity of such fluids were determined before and after incubation. Furthermore, the influence of the Ca/P values on such parameters was exemplified. Physicochemical analysis of received materials was performed by XRD and FT-IR characterization techniques. Their potential antibacterial activity and behavior in the presence of infectious microorganisms as Escherichia coli and Staphylococcus aureus was also evaluated. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2018. © 2018 Wiley Periodicals, Inc.

A Review of Extraction and Analysis of Bioactives in Oat and Barley and Scope for Use of Novel Food Processing Technologies.

PubMed

Gangopadhyay, Nirupama; Hossain, Mohammad B; Rai, Dilip K; Brunton, Nigel P

2015-06-12

Oat and barely are cereal crops mainly used as animal feed and for the purposes of malting and brewing, respectively. Some studies have indicated that consumption of oat and barley rich foods may reduce the risk of some chronic diseases such as coronary heart disease, type II diabetes and cancer. Whilst there is no absolute consensus, some of these benefits may be linked to presence of compounds such as phenolics, vitamin E and β-glucan in these cereals. A number of benefits have also been linked to the lipid component (sterols, fatty acids) and the proteins and bioactive peptides in oats and barley. Since the available evidence is pointing toward the possible health benefits of oat and barley components, a number of authors have examined techniques for recovering them from their native sources. In the present review, we summarise and examine the range of conventional techniques that have been used for the purpose of extraction and detection of these bioactives. In addition, the recent advances in use of novel food processing technologies as a substitute to conventional processes for extraction of bioactives from oats and barley, has been discussed.

Anti-Inflammatory and Anti-Obesity Properties of Food Bioactive Components: Effects on Adipose Tissue

PubMed Central

Jayarathne, Shasika; Koboziev, Iurii; Park, Oak-Hee; Oldewage-Theron, Wilna; Shen, Chwan-Li; Moustaid-Moussa, Naima

2017-01-01

Obesity is an epidemic and costly disease affecting 13% of the adult population worldwide. Obesity is associated with adipose tissue hypertrophy and hyperplasia, as well as pathologic endocrine alterations of adipose tissue including local and chronic systemic low-grade inflammation. Moreover, this inflammation is a risk factor for both metabolic syndrome (MetS) and insulin resistance. Basic and clinical studies demonstrate that foods containing bioactive compounds are capable of preventing both obesity and adipose tissue inflammation, improving obesity-associated MetS in human subjects and animal models of obesity. In this review, we discuss the anti-obesity and anti-inflammatory protective effects of some bioactive polyphenols of plant origin and omega-3 polyunsaturated fatty acids, available for the customers worldwide from commonly used foods and/or as components of commercial food supplements. We review how these bioactive compounds modulate cell signaling including through the nuclear factor-κB, adenosine monophosphate-activated protein kinase, mitogen-activated protein kinase, toll-like receptors, and G-protein coupled receptor 120 intracellular signaling pathways and improve the balance of pro- and anti-inflammatory mediators secreted by adipose tissue and subsequently lower systemic inflammation and risk for metabolic diseases. PMID:29333376

Should bioactive trace elements not recognized as essential, but with beneficial health effects, have intake recommendations.

PubMed

Nielsen, Forrest H

2014-10-01

Today, most nutritionists do not consider a trace element essential unless it has a defined biochemical function in higher animals or humans. As a result, even though it has been found that trace elements such as boron and silicon have beneficial bioactivity in higher animals and humans, they generally receive limited attention or mention when dietary guidelines or intake recommendations are formulated. Recently, the possibility of providing dietary intake recommendations such as an adequate intake (AI) for some bioactive food components (e.g., flavonoids) has been discussed. Boron, chromium, nickel, and silicon are bioactive food components that provide beneficial health effects by plausible mechanisms of action in nutritional and supra nutritional amounts, and thus should be included in the discussions. Although the science base may not be considered adequate for establishing AIs, a significant number of findings suggest that statements about these trace elements should be included when dietary intake guidance is formulated. An appropriate recommendation may be that diets should include foods that would provide trace elements not currently recognized as essential in amounts shown to reduce the risk of chronic disease and/or promote health and well-being. Published by Elsevier GmbH.

A narrative review of the associations between six bioactive components in breast milk and infant adiposity.

PubMed

Fields, David A; Schneider, Camille R; Pavela, Gregory

2016-06-01

This narrative review examines six important non-nutritive substances in breast milk, many of which were thought to have little to no biological significance. The overall objective is to provide background on key bioactive factors in breast milk believed to have an effect on infant outcomes (growth and body composition). The evidence for the effects of the following six bioactive compounds in breast milk on infant growth outcomes are reviewed: insulin, leptin, adiponectin, ghrelin, interleukin-6, and tumor necrosis factor-α. The existing literature on the effects of breast milk insulin, ghrelin, interleukin-6, and tumor necrosis factor-α and their associations with infant growth and adiposity is sparse. Of the bioactive compounds reviewed, leptin and adiponectin are the most researched. Data reveal that breast milk adiponectin has negative associations with growth in infancy. There is a need for innovative, well-designed studies to improve causal inference and advance our understanding in the effects of breast milk and its components on offspring growth and body composition. The recommendations provided, along with careful consideration of both known and unknown factors that affect breast milk composition, will help improve, standardize, and ultimately advance this emergent field. © 2016 The Obesity Society.

Thermal analysis and in vitro bioactivity of bioactive glass-alumina composites

DOE Office of Scientific and Technical Information (OSTI.GOV)

Chatzistavrou, Xanthippi, E-mail: x.chatzistavrou@imperial.ac.uk; Kantiranis, Nikolaos, E-mail: kantira@geo.auth.gr; Kontonasaki, Eleana, E-mail: kont@dent.auth.gr

2011-01-15

Bioactive glass-alumina composite (BA) pellets were fabricated in the range 95/5-60/40 wt.% respectively and were heat-treated under a specific thermal treatment up to 950 {sup o}C. Control (unheated) and heat-treated pellets were immersed in Simulated Body Fluid (SBF) for bioactivity testing. All pellets before and after immersion in SBF were studied by Fourier Transform Infrared spectroscopy (FTIR), Scanning Electron Microscopy (SEM-EDS) and X-ray Diffraction (XRD) analysis. All composite pellets presented bioactive response. On the surface of the heat-treated pellets the development of a rich biological hydroxyapatite (HAp) layer was delayed for one day, compared to the respective control pellets. Independentmore » of the proportion of the two components, all composites of each group (control and heat-treated) presented the same bioactive response as a function of immersion time in SBF. It was found that by the applied methodology, Al{sub 2}O{sub 3} can be successfully applied in bioactive glass composites without obstructing their bioactive response. - Research Highlights: {yields} Isostatically pressed glass-alumina composites presented apatite-forming ability. {yields} The interaction with SBF resulted in an aluminium phosphate phase formation. {yields} The formation of an aluminium phosphate phase enhanced the in vitro apatite growth.« less

The Sea Urchin Arbacia lixula: A Novel Natural Source of Astaxanthin

PubMed Central

Cirino, Paola; Brunet, Christophe; Ciaravolo, Martina; Galasso, Christian; Musco, Luigi; Vega Fernández, Tomás; Sansone, Clementina; Toscano, Alfonso

2017-01-01

Several echinoderms, including sea urchins, are valuable sources of bioactive compounds but their nutraceutical potential is largely unexplored. In fact, the gonads of some sea urchin species contain antioxidants including carotenoids and polyhydroxylated naphthoquinones (PHNQ’s), such as echinochrome A. Astaxanthin is known to have particular bioactivity for the prevention of neurodegenerative diseases. This carotenoid is produced by microalgae, while several marine invertebrates can bioaccumulate or synthetize it from metabolic precursors. We determined the carotenoid content and analyzed the bioactivity potential of non-harvested Atlantic-Mediterranean sea urchin Arbacia lixula. The comparison of methanol crude extracts obtained from eggs of farmed and wild specimens revealed a higher bioactivity in farmed individuals fed with a customized fodder. HPLC-analysis revealed a high concentration of astaxanthin (27.0 μg/mg), which was the only pigment observed. This study highlights the potential of farmed A. lixula as a new source of the active stereoisomer of astaxanthin. PMID:28635649

Therapeutic potential of abalone and status of bioactive molecules: A comprehensive review.

PubMed

Suleria, H A R; Masci, P P; Gobe, G C; Osborne, S A

2017-05-24

Marine organisms are increasingly being investigated as sources of bioactive molecules with therapeutic applications as nutraceuticals and pharmaceuticals. In particular, nutraceuticals are gaining popularity worldwide owing to their therapeutic potential and incorporation in functional foods and dietary supplements. Abalone, a marine gastropod, contains a variety of bioactive compounds with anti-oxidant, anti-thrombotic, anti-inflammatory, anti-microbial, and anti-cancer activities. For thousands of years different cultures have used abalone as a traditional functional food believing consumption provides health benefits. Abalone meat is one of the most precious commodities in Asian markets where it is considered a culinary delicacy. Recent research has revealed that abalone is composed of many vital moieties like polysaccharides, proteins, and fatty acids that provide health benefits beyond basic nutrition. A review of past and present research is presented with relevance to the therapeutic potential of bioactive molecules from abalone.

Isolation, structure, and bioactivities of polysaccharides from Cyclocarya paliurus (Batal.) Iljinskaja.

PubMed

Li, Qiqiong; Hu, Jielun; Xie, Jianhua; Nie, Shaoping; Xie, Ming-Yong

2017-06-01

Cyclocarya paliurus (Batal.) Iljinskaja, a well-known edible and medicinal plant, has been widely used in China as a traditional medicine for treating hypertension and diabetes. C. paliurus possesses various bioactivities, such as antihyperglycemic, antihyperlipidemic, antihypertensive, anticancer, antifatigue, antioxidation, antimicrobial, colon health-promoting, and immunological activities. Polysaccharides, as natural macromolecules with various biological activities, are considered to be the main effective components in C. paliurus. Here, we summarize studies of polysaccharides from C. paliurus over the past 20 years, including extraction and purification processes, structure, and bioactivities. © 2017 New York Academy of Sciences.

Increasing the Coverage of Medicinal Chemistry-Relevant Space in Commercial Fragments Screening

PubMed Central

2014-01-01

Analyzing the chemical space coverage in commercial fragment screening collections revealed the overlap between bioactive medicinal chemistry substructures and rule-of-three compliant fragments is only ∼25%. We recommend including these fragments in fragment screening libraries to maximize confidence in discovering hit matter within known bioactive chemical space, while incorporation of nonoverlapping substructures could offer novel hits in screening libraries. Using principal component analysis, polar and three-dimensional substructures display a higher-than-average enrichment of bioactive compounds, indicating increasing representation of these substructures may be beneficial in fragment screening. PMID:24405118

Yogurt and Cardiometabolic Diseases: A Critical Review of Potential Mechanisms.

PubMed

Fernandez, Melissa Anne; Panahi, Shirin; Daniel, Noémie; Tremblay, Angelo; Marette, André

2017-11-01

Associations between yogurt intake and risk of diet-related cardiometabolic diseases (CMDs) have been the subject of recent research in epidemiologic nutrition. A healthy dietary pattern has been identified as a pillar for the prevention of weight gain and CMDs. Epidemiologic studies suggest that yogurt consumption is linked to healthy dietary patterns, lifestyles, and reduced risk of CMDs, particularly type 2 diabetes. However, to our knowledge, few to no randomized controlled trials have investigated yogurt intake in relation to cardiometabolic clinical outcomes. Furthermore, there has been little attempt to clarify the mechanisms that underlie the potential beneficial effects of yogurt consumption on CMDs. Yogurt is a nutrient-dense dairy food and has been suggested to reduce weight gain and prevent CMDs by contributing to intakes of protein, calcium, bioactive lipids, and several other micronutrients. In addition, fermentation with bacterial strains generates bioactive peptides, resulting in a potentially greater beneficial effect of yogurt on metabolic health than nonfermented dairy products such as milk. To date, there is little concrete evidence that the mechanisms proposed in observational studies to explain positive results of yogurt on CMDs or parameters are valid. Many proposed mechanisms are based on assumptions that commercial yogurts contain strain-specific probiotics, that viable yogurt cultures are present in adequate quantities, and that yogurt provides a minimum threshold dose of nutrients or bioactive components capable of exerting a physiologic effect. Therefore, the primary objective of this review is to investigate the plausibility of potential mechanisms commonly cited in the literature in order to shed light on the inverse associations reported between yogurt intake and various cardiometabolic health parameters that are related to its nutrient profile, bacterial constituents, and food matrix. This article reviews current gaps and challenges in identifying such mechanisms and provides a perspective on the research agenda to validate the proposed role of yogurt in protecting against CMDs. © 2017 American Society for Nutrition.

Cannabidiol in medicine: a review of its therapeutic potential in CNS disorders.

PubMed

Scuderi, Caterina; Filippis, Daniele De; Iuvone, Teresa; Blasio, Angelo; Steardo, Antonio; Esposito, Giuseppe

2009-05-01

Cannabidiol (CBD) is the main non-psychotropic component of the glandular hairs of Cannabis sativa. It displays a plethora of actions including anticonvulsive, sedative, hypnotic, antipsychotic, antiinflammatory and neuroprotective properties. However, it is well established that CBD produces its biological effects without exerting significant intrinsic activity upon cannabinoid receptors. For this reason, CBD lacks the unwanted psychotropic effects characteristic of marijuana derivatives, so representing one of the bioactive constituents of Cannabis sativa with the highest potential for therapeutic use.The present review reports the pharmacological profile of CBD and summarizes results from preclinical and clinical studies utilizing CBD, alone or in combination with other phytocannabinoids, for the treatment of a number of CNS disorders.

The impact of multi-walled carbon nanotubes (MWCNTs) on macrophages: contribution of MWCNT characteristics.

PubMed

Li, Yinghe; Cao, Jimin

2018-05-22

Multi-walled carbon nanotubes (MWCNTs) have wide application prospects but also exhibit notable biotoxicity that is tightly associated with macrophages. Macrophages simultaneously act as initiators and defenders in MWCNT-induced organ lesions, and targeting macrophages with MWCNTs may be a potential immunotherapy and oncotherapy approach. This review focuses on the impacts of MWCNTs on macrophages and further discusses the influence of MWCNT characteristics on their bioactivity. Based on existing studies, MWCNTs stimulate macrophage migration, induce secretion of various cytokines and activate inflammatory pathways in macrophages, especially NLRP3-mediated IL-1β production. This inflammatory state, together with the oxidative stress and cell membrane lesions induced by MWCNTs, contributes to decreased phagocytic ability and cell viability, which finally results in cell apoptosis and necrosis. A series of intracellular and systemic components, such as toll-like receptor, high-mobility group box 1, Rho-associated kinases, scavenger receptor and complement components, may be involved in the above-mentioned cell-MWCNT interactions. The characteristics of MWCNTs can influence their bioactivity in macrophages both mechanically and chemically. The size (length and/or diameter), functionalization, purification and even the experimental method can affect the influence of MWCNTs on macrophages, and a better understanding of these MWCNT characteristics may benefit utilization of this nanomaterial in associated nanomedical applications.

Nutraceutical and functional scenario of wheat straw.

PubMed

Pasha, Imran; Saeed, Farhan; Waqas, Khalid; Anjum, Faqir Muhammad; Arshad, Muhammad Umair

2013-01-01

In the era of nutrition, much focus has been remunerated to functional and nutraceutical foodstuffs. The health endorsing potential of such provisions is attributed to affluent phytochemistry. These dynamic constituents have functional possessions that are imperative for cereal industry. The functional and nutraceutical significance of variety of foods is often accredited to their bioactive molecules. Numerous components have been considered but wheat straw and its diverse components are of prime consideration. In this comprehensive dissertation, efforts are directed to elaborate the functional and nutraceutical importance of wheat straw. Wheat straw is lignocellulosic materials including cellulose, hemicellulose and lignin. It hold various bioactive compounds such as policosanols, phytosterols, phenolics, and triterpenoids, having enormous nutraceutical properties like anti-allergenic, anti-artherogenic, anti-inflammatory, anti-microbial, antioxidant, anti-thrombotic, cardioprotective and vasodilatory effects, antiviral, and anticancer. These compounds are protecting against various ailments like hypercholesterolemia, intermittent claudication, benign prostatic hyperplasia and cardiovascular diseases. Additionally, wheat straw has demonstrated successfully, low cost, renewable, versatile, widely distributed, easily available source for the production of biogas, bioethanol, and biohydrogen in biorefineries to enhance the overall effectiveness of biomass consumption in protected and eco-friendly environment. Furthermore, its role in enhancing the quality and extending the shelf life of bakery products through reducing the progression of staling and retrogradation is limelight of the article.

Novel non-cytotoxic, bioactive and biodegradable hybrid materials based on polyurethanes/TiO2 for biomedical applications.

PubMed

González-García, Dulce M; Téllez Jurado, L; Jiménez-Gallegos, R; Rodríguez-Lorenzo, Luis M

2017-06-01

Titanium compounds have demonstrated great interfacial properties with biological tissues whereas a wide variety of polyurethanes have also been successfully probed in medical applications. However, studies about hybrids based on polyurethanes/TiO 2 for medical applications are scarce. The aim of this work is to design novel biodegradable hybrid materials based on polyurethanes/TiO 2 (80% organic-20% inorganic) and to perform a preliminary study of the potential applications in bone regeneration. The hybrids have been prepared by a sol-gel reaction using titanium isopropoxide as precursor of the inorganic component and polyurethane as the organic one. A series of polyurethanes has been prepared using different polyesters glycol succinate as soft segment, and 1,6-diisocyanatohexane (HDI) and butanediol (BD) as linear hard segment. The spectroscopy techniques used allow to confirm the formation of the required polyurethanes by the identification of bands related to carboxylic groups (COOH), and the amine groups (NH), and also the TiOH bonds and the bonds related to the interconnected network between the inorganic and the organic components from hybrids. The results from SEM/EDS show a homogeneous distribution of the inorganic component into the organic matrix. The nontoxic character of the hybrid (H400) was probed using MG-63 cell line with over 90% of cell viability. Finally, the formation of a hydroxyapatite layer in the material surface after 21days of soaking in SBF shows the bioactive character. Copyright © 2017 Elsevier B.V. All rights reserved.

Assessing similarity analysis of chromatographic fingerprints of Cyclopia subternata extracts as potential screening tool for in vitro glucose utilisation.

PubMed

Schulze, Alexandra E; De Beer, Dalene; Mazibuko, Sithandiwe E; Muller, Christo J F; Roux, Candice; Willenburg, Elize L; Nyunaï, Nyemb; Louw, Johan; Manley, Marena; Joubert, Elizabeth

2016-01-01

Similarity analysis of the phenolic fingerprints of a large number of aqueous extracts of Cyclopia subternata, obtained by high-performance liquid chromatography (HPLC), was evaluated as a potential tool to screen extracts for relative bioactivity. The assessment was based on the (dis)similarity of their fingerprints to that of a reference active extract of C. subternata, proven to enhance glucose uptake in vitro and in vivo. In vitro testing of extracts, selected as being most similar (n = 5; r ≥ 0.962) and most dissimilar (n = 5; r ≤ 0.688) to the reference active extract, showed that no clear pattern in terms of relative glucose uptake efficacy in C2C12 myocytes emerged, irrespective of the dose. Some of the most dissimilar extracts had higher glucose-lowering activity than the reference active extract. Principal component analysis revealed the major compounds responsible for the most variation within the chromatographic fingerprints, as mangiferin, isomangiferin, iriflophenone-3-C-β-D-glucoside-4-O-β-D-glucoside, iriflophenone-3-C-β-D-glucoside, scolymoside, and phloretin-3',5'-di-C-β-D-glucoside. Quantitative analysis of the selected extracts showed that the most dissimilar extracts contained the highest mangiferin and isomangiferin levels, whilst the most similar extracts had the highest scolymoside content. These compounds demonstrated similar glucose uptake efficacy in C2C12 myocytes. It can be concluded that (dis)similarity of chromatographic fingerprints of extracts of unknown activity to that of a proven bioactive extract does not necessarily translate to lower or higher bioactivity.

Bioactive Natural Products Prioritization Using Massive Multi-informational Molecular Networks.

PubMed

Olivon, Florent; Allard, Pierre-Marie; Koval, Alexey; Righi, Davide; Genta-Jouve, Gregory; Neyts, Johan; Apel, Cécile; Pannecouque, Christophe; Nothias, Louis-Félix; Cachet, Xavier; Marcourt, Laurence; Roussi, Fanny; Katanaev, Vladimir L; Touboul, David; Wolfender, Jean-Luc; Litaudon, Marc

2017-10-20

Natural products represent an inexhaustible source of novel therapeutic agents. Their complex and constrained three-dimensional structures endow these molecules with exceptional biological properties, thereby giving them a major role in drug discovery programs. However, the search for new bioactive metabolites is hampered by the chemical complexity of the biological matrices in which they are found. The purification of single constituents from such matrices requires such a significant amount of work that it should be ideally performed only on molecules of high potential value (i.e., chemical novelty and biological activity). Recent bioinformatics approaches based on mass spectrometry metabolite profiling methods are beginning to address the complex task of compound identification within complex mixtures. However, in parallel to these developments, methods providing information on the bioactivity potential of natural products prior to their isolation are still lacking and are of key interest to target the isolation of valuable natural products only. In the present investigation, we propose an integrated analysis strategy for bioactive natural products prioritization. Our approach uses massive molecular networks embedding various informational layers (bioactivity and taxonomical data) to highlight potentially bioactive scaffolds within the chemical diversity of crude extracts collections. We exemplify this workflow by targeting the isolation of predicted active and nonactive metabolites from two botanical sources (Bocquillonia nervosa and Neoguillauminia cleopatra) against two biological targets (Wnt signaling pathway and chikungunya virus replication). Eventually, the detection and isolation processes of a daphnane diterpene orthoester and four 12-deoxyphorbols inhibiting the Wnt signaling pathway and exhibiting potent antiviral activities against the CHIKV virus are detailed. Combined with efficient metabolite annotation tools, this bioactive natural products prioritization pipeline proves to be efficient. Implementation of this approach in drug discovery programs based on natural extract screening should speed up and rationalize the isolation of bioactive natural products.

Marine-Derived Bioactive Peptides for Biomedical Sectors: A Review.

PubMed

Ruiz-Ruiz, Federico; Mancera-Andrade, Elena I; Iqbal, Hafiz M N

2017-01-01

Marine-based resources such as algae and other marine by-products have been recognized as rich sources of structurally diverse bioactive peptides. Evidently, their structural characteristics including unique amino acid residues are responsible for their biological activity. Several of the above-mentioned marine-origin species show multi-functional bioactivities that are useful for a new discovery and/or reinvention of biologically active ingredients, nutraceuticals and/or pharmaceuticals. Therefore, in recent years, marine-derived bioactive peptides have gained a considerable attention with high-value biomedical and/or pharmaceutical potentials. Furthermore, a wider spectrum of bioactive peptides can be produced through proteolytic-assisted hydrolysis of various marine resources under controlled physicochemical (pH and temperature of the reaction media) environment. Owing to their numerous health-related beneficial effects and therapeutic potential in the treatment and/or prevention of many diseases, such marine-derived bioactive peptides exhibit a wider spectrum of biological activities such as anti-cancerous, anti-proliferative, anti-coagulant, antibacterial, antifungal, and anti-tumor activities among many others. Based on emerging evidence of marine-derived peptide mining, the above-mentioned marine resources contain noteworthy levels of high-value protein. The present review article mainly summarizes the marine-derived bioactive peptides and emphasizing their potential applications in biomedical and/or pharmaceutical sectors of the modern world. In conclusion, recent literature has provided evidence that marine-derived bioactive peptides play a critical role in human health along with many possibilities of designing new functional nutraceuticals and/or pharmaceuticals to clarify potent mechanisms of action for a wider spectrum of diseases. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Water-based polyurethane 3D printed scaffolds with controlled release function for customized cartilage tissue engineering.

PubMed

Hung, Kun-Che; Tseng, Ching-Shiow; Dai, Lien-Guo; Hsu, Shan-hui

2016-03-01

Conventional 3D printing may not readily incorporate bioactive ingredients for controlled release because the process often involves the use of heat, organic solvent, or crosslinkers that reduce the bioactivity of the ingredients. Water-based 3D printing materials with controlled bioactivity for customized cartilage tissue engineering is developed in this study. The printing ink contains the water dispersion of synthetic biodegradable polyurethane (PU) elastic nanoparticles, hyaluronan, and bioactive ingredients TGFβ3 or a small molecule drug Y27632 to replace TGFβ3. Compliant scaffolds are printed from the ink at low temperature. These scaffolds promote the self-aggregation of mesenchymal stem cells (MSCs) and, with timely release of the bioactive ingredients, induce the chondrogenic differentiation of MSCs and produce matrix for cartilage repair. Moreover, the growth factor-free controlled release design may prevent cartilage hypertrophy. Rabbit knee implantation supports the potential of the novel 3D printing scaffolds in cartilage regeneration. We consider that the 3D printing composite scaffolds with controlled release bioactivity may have potential in customized tissue engineering. Copyright © 2016 Elsevier Ltd. All rights reserved.

Molecular mechanisms of the anti-obesity effect of bioactive compounds in tea and coffee.

PubMed

Pan, Min-Hsiung; Tung, Yen-Chen; Yang, Guliang; Li, Shiming; Ho, Chi-Tang

2016-11-09

Obesity is a serious health problem in adults and children worldwide. However, the basic strategies for the management of obesity (diet, exercise, drugs and surgery) have limitations and side effects. Therefore, many researchers have sought to identify bioactive components in food. Tea and coffee are the most frequently consumed beverages in the whole world. Their health benefits have been studied for decades, especially those of green tea. The anti-obesity effect of tea and coffee has been studied for at least ten years. The results have shown decreased lipid accumulation in cells via the regulation of the cell cycle during adipogenesis, changes in transcription factors and lipogenesis-related proteins in the adipose tissue of animal models, and decreased body weight and visceral fat in humans. Tea and coffee also influence the gut microbiota in obese animals and humans. Although the anti-obesity mechanism of tea and coffee still needs further clarification, they may have potential as a new strategy to prevent or treat obesity.

Milk Proteins, Peptides, and Oligosaccharides: Effects against the 21st Century Disorders

PubMed Central

Hsieh, Chia-Chien; Hernández-Ledesma, Blanca; Fernández-Tomé, Samuel; Weinborn, Valerie; Barile, Daniela; de Moura Bell, Juliana María Leite Nobrega

2015-01-01

Milk is the most complete food for mammals, as it supplies all the energy and nutrients needed for the proper growth and development of the neonate. Milk is a source of many bioactive components, which not only help meeting the nutritional requirements of the consumers, but also play a relevant role in preventing various disorders. Milk-derived proteins and peptides have the potential to act as coadjuvants in conventional therapies, addressing cardiovascular diseases, metabolic disorders, intestinal health, and chemopreventive properties. In addition to being a source of proteins and peptides, milk contains complex oligosaccharides that possess important functions related to the newborn's development and health. Some of the health benefits attributed to milk oligosaccharides include prebiotic probifidogenic effects, antiadherence of pathogenic bacteria, and immunomodulation. This review focuses on recent findings demonstrating the biological activities of milk peptides, proteins, and oligosaccharides towards the prevention of diseases of the 21st century. Processing challenges hindering large-scale production and commercialization of those bioactive compounds have been also addressed. PMID:25789308

Espresso coffee residues: a valuable source of unextracted compounds.

PubMed

Cruz, Rebeca; Cardoso, Maria M; Fernandes, Luana; Oliveira, Marta; Mendes, Eulália; Baptista, Paula; Morais, Simone; Casal, Susana

2012-08-15

Espresso spent coffee grounds were chemically characterized to predict their potential, as a source of bioactive compounds, by comparison with the ones from the soluble coffee industry. Sampling included a total of 50 samples from 14 trademarks, collected in several coffee shops and prepared with distinct coffee machines. A high compositional variability was verified, particularly with regard to such water-soluble components as caffeine, total chlorogenic acids (CGA), and minerals, supported by strong positive correlations with total soluble solids retained. This is a direct consequence of the reduced extraction efficiency during espresso coffee preparation, leaving a significant pool of bioactivity retained in the extracted grounds. Besides the lipid (12.5%) and nitrogen (2.3%) contents, similar to those of industrial coffee residues, the CGA content (478.9 mg/100 g), for its antioxidant capacity, and its caffeine content (452.6 mg/100 g), due to its extensive use in the food and pharmaceutical industries, justify the selective assembly of this residue for subsequent use.

Milk proteins, peptides, and oligosaccharides: effects against the 21st century disorders.

PubMed

Hsieh, Chia-Chien; Hernández-Ledesma, Blanca; Fernández-Tomé, Samuel; Weinborn, Valerie; Barile, Daniela; de Moura Bell, Juliana María Leite Nobrega

2015-01-01

Milk is the most complete food for mammals, as it supplies all the energy and nutrients needed for the proper growth and development of the neonate. Milk is a source of many bioactive components, which not only help meeting the nutritional requirements of the consumers, but also play a relevant role in preventing various disorders. Milk-derived proteins and peptides have the potential to act as coadjuvants in conventional therapies, addressing cardiovascular diseases, metabolic disorders, intestinal health, and chemopreventive properties. In addition to being a source of proteins and peptides, milk contains complex oligosaccharides that possess important functions related to the newborn's development and health. Some of the health benefits attributed to milk oligosaccharides include prebiotic probifidogenic effects, antiadherence of pathogenic bacteria, and immunomodulation. This review focuses on recent findings demonstrating the biological activities of milk peptides, proteins, and oligosaccharides towards the prevention of diseases of the 21st century. Processing challenges hindering large-scale production and commercialization of those bioactive compounds have been also addressed.

Composition and properties of virgin pistachio oils and their by-products from different cultivars.

PubMed

Ojeda-Amador, Rosa M; Fregapane, Giuseppe; Salvador, María Desamparados

2018-02-01

Pistachios (Pistacia vera) exhibit an interesting nutritional value, due to the high content of oleic acid and minor components with antioxidant and bioactive properties. This work aimed to characterize pistachio virgin oils and their partially defatted residual cakes, obtained from eight cultivars (Aegina, Avdat, Kastel, Kerman, Larnaka, Mateur, Napoletana, and Sirora). Interesting results on phenolics, tocopherols and antioxidant activity were observed, which were greatly affected by variety. Pistachio virgin oils are rich in healthy oleic acid (55-74%), phytosterols (3200-7600mg/kg) and γ-tocopherol (550-720mg/kg). A high content of phenolic compounds (8600-15000mg/kg gallic acid equivalents) and the corresponding antioxidant activities (12-46 and 155-496mmol/kg for DPPH and ORAC) of the residual cakes demonstrate their potential applications as functional ingredients and as rich sources of bioactive compounds. Moreover, virgin pistachio oils possess peculiar and pleasant sensory characteristics, contributing greater added value to the consumers compared to refined vegetable oils. Copyright © 2017 Elsevier Ltd. All rights reserved.

Characterization of polysaccharides with marked inhibitory effect on lipid accumulation in Pleurotus eryngii.

PubMed

Chen, Jingjing; Yong, Yangyang; Xing, Meichun; Gu, Yifan; Zhang, Zhao; Zhang, Shizhu; Lu, Ling

2013-09-12

Mushrooms have a great potential for the production of useful bioactive metabolites. To explore the bioactive compounds from edible mushrooms for interfering with the development of macrophage-derived foam cells, which is recognized as the hallmark of early atherosclerosis, eight types of mushrooms polysaccharides had been selected to be tested. Consequently, different mushrooms polysaccharides displayed diverse component profiles. Of polysaccharides that we tested, the Pleurotus eryngii polysaccharide had the strongest inhibitory effect on lipid accumulation. Furthermore, through fractionation of DEAE-52 and Sephadex G-100, the polysaccharide from P. eryngii had been successfully purified and identified. By the analysis of IR, GC, and HPLC, the purified polysaccharide was estimated to be 30-38 kDa for the average molecular weight with the monosaccharide composition mainly composed of D-types of mannose, glucose and galactose. Findings presented in this report firstly provide direct evidence, which links the purified polysaccharide moiety with the biological function in foam-cell model. Copyright © 2013 Elsevier Ltd. All rights reserved.

Enzymatic hybridization of α-lipoic acid with bioactive compounds in ionic solvents.

PubMed

Papadopoulou, Athena A; Katsoura, Maria H; Chatzikonstantinou, Alexandra; Kyriakou, Eleni; Polydera, Angeliki C; Tzakos, Andreas G; Stamatis, Haralambos

2013-05-01

The lipase-catalyzed molecular hybridization of α-lipoic acid (LA) with bioactive compounds pyridoxine, tyrosol and tyramine was performed in ionic solvents and deep eutectic solvents. The biocatalytic reactions were catalyzed by Candida antarctica lipase B immobilized onto various functionalized multi-walled carbon nanotubes (f-CNTs-CaLB), as well as by commercial Novozym 435. The use of f-CNTs-CaLB leads, in most cases, to higher conversion yields as compared to Novozym 435. The nature and ion composition of ionic solvents affect the performance of the biocatalytic process. The highest conversion yield was observed in (mtoa)NTf2. The high enzyme stability and the relatively low solubility of substrates in specific media account for the improved biocatalytic synthesis of molecular hybrids of LA. Principal component analysis was used to screen for potential lipoxygenase inhibitors. In vitro studies showed that the synthesized compounds exhibit up to 10-fold increased inhibitory activity on lipoxygenase mediated lipid peroxidation as compared to parent molecules. Copyright © 2013 Elsevier Ltd. All rights reserved.

Effect of postharvest handling practices on phytochemical concentrations and bioactive potential in wild blueberry fruit

USDA-ARS?s Scientific Manuscript database

In this study, we quantified anthocyanin (ANC), proanthocyanidin (PAC), and chlorogenic acid (CA) concentrations in wild blueberry fruit (WBB) exposed to a variety of postharvest handling practices relevant to consumers and to industry. Additionally, we analyzed the bioactive potential of WBB subjec...

Antimycobacterial and antimalarial activities of endophytic fungi associated with the ancient and narrowly endemic neotropical plant Vellozia gigantea from Brazil.

PubMed

Ferreira, Mariana C; Cantrell, Charles L; Wedge, David E; Gonçalves, Vívian N; Jacob, Melissa R; Khan, Shabana; Rosa, Carlos A; Rosa, Luiz H

2017-10-01

Endophytic fungi, present mainly in the Ascomycota and Basidiomycota phyla, are associated with different plants and represent important producers of bioactive natural products. Brazil has a rich biodiversity of plant species, including those reported as being endemic. Among the endemic Brazilian plant species, Vellozia gigantea (Velloziaceae) is threatened by extinction and is a promising target to recover endophytic fungi. The present study focused on bioprospecting of bioactive compounds of the endophytic fungi associated with V. gigantea, an endemic, ancient, and endangered plant species that occurs only in the rupestrian grasslands of Brazil. The capability of 285 fungal isolates to produce antimicrobial and antimalarial activities was examined. Fungi were grown at solid-state fermentation to recover their crude extracts in dichloromethane. Bioactive extracts were analysed by chromatographic fractionation and NMR and displayed compounds with antimicrobial, antimycobacterial, and antimalarial activities. Five fungi produced antimicrobial and antimalarial compounds. Extracts of Diaporthe miriciae showed antifungal, antibacterial, and antimalarial activities; Trichoderma effusum displayed selective antibacterial activity against methicillin-resistant Staphylococcus aureus and Mycobacterium intracellulare; and three Penicillium species showed antibacterial activity. D. miriciae extract contained highly functionalised secondary metabolites, yielding the compound epoxycytochalasin H with high antimalarial activity against the chloroquine-resistant strain of Plasmodium falciparum, with an IC50 approximately 3.5-fold lower than that with chloroquine. Our results indicate that V. gigantea may represent a microhabitat repository hotspot of potential fungi producers of bioactive compounds and suggest that endophytic fungal communities might be an important biological component contributing to the fitness of the plants living in the rupestrian grassland.

Applied modern biotechnology for cultivation of Ganoderma and development of their products.

PubMed

Zhou, Xuan-Wei; Su, Kai-Qi; Zhang, Yong-Ming

2012-02-01

A white-rot basidiomycete Ganoderma spp. has long been used as a medicinal mushroom in Asia, and it has an array of pharmacological properties for immunomodulatory activity. There have been many reports about the bioactive components and their pharmacological properties. In order to analyze the current status of Ganoderma products, the detailed process of cultivation of Ganoderma spp. and development of their products are restated in this review article. These include the breeding, cultivating, extracting bioactive component, and processing Ganoderma products, etc. This article will expand people's common knowledge on Ganoderma, and provide a beneficial reference for research and industrial production.

Vegetable Oils as Alternative Solvents for Green Oleo-Extraction, Purification and Formulation of Food and Natural Products.

PubMed

Yara-Varón, Edinson; Li, Ying; Balcells, Mercè; Canela-Garayoa, Ramon; Fabiano-Tixier, Anne-Sylvie; Chemat, Farid

2017-09-05

Since solvents of petroleum origin are now strictly regulated worldwide, there is a growing demand for using greener, bio-based and renewable solvents for extraction, purification and formulation of natural and food products. The ideal alternative solvents are non-volatile organic compounds (VOCs) that have high dissolving power and flash point, together with low toxicity and less environmental impact. They should be obtained from renewable resources at a reasonable price and be easy to recycle. Based on the principles of Green Chemistry and Green Engineering, vegetable oils could become an ideal alternative solvent to extract compounds for purification, enrichment, or even pollution remediation. This review presents an overview of vegetable oils as solvents enriched with various bioactive compounds from natural resources, as well as the relationship between dissolving power of non-polar and polar bioactive components with the function of fatty acids and/or lipid classes in vegetable oils, and other minor components. A focus on simulation of solvent-solute interactions and a discussion of polar paradox theory propose a mechanism explaining the phenomena of dissolving polar and non-polar bioactive components in vegetable oils as green solvents with variable polarity.

Mesoporous bioactive glass nanolayer-functionalized 3D-printed scaffolds for accelerating osteogenesis and angiogenesis

NASA Astrophysics Data System (ADS)

Zhang, Yali; Xia, Lunguo; Zhai, Dong; Shi, Mengchao; Luo, Yongxiang; Feng, Chun; Fang, Bing; Yin, Jingbo; Chang, Jiang; Wu, Chengtie

2015-11-01

The hierarchical microstructure, surface and interface of biomaterials are important factors influencing their bioactivity. Porous bioceramic scaffolds have been widely used for bone tissue engineering by optimizing their chemical composition and large-pore structure. However, the surface and interface of struts in bioceramic scaffolds are often ignored. The aim of this study is to incorporate hierarchical pores and bioactive components into the bioceramic scaffolds by constructing nanopores and bioactive elements on the struts of scaffolds and further improve their bone-forming activity. Mesoporous bioactive glass (MBG) modified β-tricalcium phosphate (MBG-β-TCP) scaffolds with a hierarchical pore structure and a functional strut surface (~100 nm of MBG nanolayer) were successfully prepared via 3D printing and spin coating. The compressive strength and apatite-mineralization ability of MBG-β-TCP scaffolds were significantly enhanced as compared to β-TCP scaffolds without the MBG nanolayer. The attachment, viability, alkaline phosphatase (ALP) activity, osteogenic gene expression (Runx2, BMP2, OPN and Col I) and protein expression (OPN, Col I, VEGF, HIF-1α) of rabbit bone marrow stromal cells (rBMSCs) as well as the attachment, viability and angiogenic gene expression (VEGF and HIF-1α) of human umbilical vein endothelial cells (HUVECs) in MBG-β-TCP scaffolds were significantly upregulated compared with conventional bioactive glass (BG)-modified β-TCP (BG-β-TCP) and pure β-TCP scaffolds. Furthermore, MBG-β-TCP scaffolds significantly enhanced the formation of new bone in vivo as compared to BG-β-TCP and β-TCP scaffolds. The results suggest that application of the MBG nanolayer to modify 3D-printed bioceramic scaffolds offers a new strategy to construct hierarchically porous scaffolds with significantly improved physicochemical and biological properties, such as mechanical properties, osteogenesis, angiogenesis and protein expression for bone tissue engineering applications, in which the incorporation of nanostructures and bioactive components into the scaffold struts synergistically play a key role in the improved bone formation.

Isolation and characterization of bioactive components from Mirabilis jalapa L. radix

PubMed Central

Gogoi, Jyotchna; Nakhuru, Khonamai Sewa; Policegoudra, Rudragoud S.; Chattopadhyay, Pronobesh; Rai, Ashok Kumar; Veer, Vijay

2015-01-01

The present investigation was carried out to isolate and characterize bioactive components from Mirabilis jalapa L. radix (紫茉莉根 zǐ mò lì gēn). Thin-layer chromatography was used for the separation of spots from fractions of the crude extract. Separated spots were collected for identification of their activities. Free-radical scavenging activity was evaluated by spraying thin-layer chromatography plates (spotted with fractions) with 0.2% of 2,2-diphenyl-1-picrylhydrazyl solution. Activity against human pathogens such as Staphylococcus aureus and Candida albicans were determined using the agar diffusion method. Potential spots were subjected to infrared (IR) analysis and gas chromatography for characterization. Two spots (5F1 and 1F3) showed free-radical scavenging activity. The 1F3 spot was active against both S. aureus and C. albicans, whereas the 5F1 spot was active against S. aureus only. IR spectral analysis indicated that 5F1 spot to be a triterpenoid. Using IR spectral analysis and an IR library search, the 1F3 spot was identified to be a flavone, which may have a hydroxyl group in ring “A” of the flavone nucleus. Our results indicated that the 1F3 and 5F1 spots are potential free-radical scavengers. Both 1F3 and 5F1 exhibited antimicrobial activity. IR spectral analysis coupled with an IR library search indicated 1F3 and 5F1 to be a flavone and a triterpenoid, respectively. PMID:26870679

In vitro antiproliferative/cytotoxic activity on cancer cell lines of a cardanol and a cardol enriched from Thai Apis mellifera propolis

PubMed Central

2012-01-01

Background Propolis is a complex resinous honeybee product. It is reported to display diverse bioactivities, such as antimicrobial, anti-inflammatory and anti-tumor properties, which are mainly due to phenolic compounds, and especially flavonoids. The diversity of bioactive compounds depends on the geography and climate, since these factors affect the floral diversity. Here, Apis mellifera propolis from Nan province, Thailand, was evaluated for potential anti-cancer activity. Methods Propolis was sequentially extracted with methanol, dichloromethane and hexane and the cytotoxic activity of each crude extract was assayed for antiproliferative/cytotoxic activity in vitro against five human cell lines derived from duet carcinoma (BT474), undifferentiated lung (Chaco), liver hepatoblastoma (Hep-G2), gastric carcinoma (KATO-III) and colon adenocarcinoma (SW620) cancers. The human foreskin fibroblast cell line (Hs27) was used as a non-transformed control. Those crude extracts that displayed antiproliferative/cytotoxic activity were then further fractionated by column chromatography using TLC-pattern and MTT-cytotoxicity bioassay guided selection of the fractions. The chemical structure of each enriched bioactive compound was analyzed by nuclear magnetic resonance and mass spectroscopy. Results The crude hexane and dichloromethane extracts of propolis displayed antiproliferative/cytotoxic activities with IC50 values across the five cancer cell lines ranging from 41.3 to 52.4 μg/ml and from 43.8 to 53.5 μg/ml, respectively. Two main bioactive components were isolated, one cardanol and one cardol, with broadly similar in vitro antiproliferation/cytotoxicity IC50 values across the five cancer cell lines and the control Hs27 cell line, ranging from 10.8 to 29.3 μg/ml for the cardanol and < 3.13 to 5.97 μg/ml (6.82 - 13.0 μM) for the cardol. Moreover, both compounds induced cytotoxicity and cell death without DNA fragmentation in the cancer cells, but only an antiproliferation response in the control Hs27 cells However, these two compounds did not account for the net antiproliferation/cytotoxic activity of the crude extracts suggesting the existence of other potent compounds or synergistic interactions in the propolis extracts. Conclusion This is the first report that Thai A. mellifera propolis contains at least two potentially new compounds (a cardanol and a cardol) with potential anti-cancer bioactivity. Both could be alternative antiproliferative agents for future development as anti-cancer drugs. PMID:22458642

Impact of Nutrients and Food Components on Dyslipidemias: What Is the Evidence?12

PubMed Central

Rosa, Carla de Oliveira Barbosa; dos Santos, Carolina Araújo; Leite, Jacqueline Isaura Alvarez; Caldas, Ana Paula Silva; Bressan, Josefina

2015-01-01

Dyslipidemias have been shown to bear a close association with an increased risk of cardiovascular diseases, atherosclerosis in particular. As efforts are being made to find alternative therapies and ways to prevent disease, there is a corresponding rise in public interest in food and/or active food components that contribute to an improved lipid profile and, thus, to better health. Besides supplying the basic nutrients necessary for well-being, some foods add further physiologic benefits. In fact, specific foods and bioactive components could be beneficial in controlling dyslipidemias. From a review of the literature on foods and bioactive compounds, their recommended quantities, and expected effects, we found that the following nutrients and food components could positively impact the lipid profile: monounsaturated and polyunsaturated fatty acids, soluble fiber, vegetable proteins, phytosterols, and polyphenols. Therefore, incorporating these components into the regular diets of individuals is justified, because they contribute additional positive effects. This suggests that they also be recommended in clinical practice. PMID:26567195

Bioactive factors in milk across lactation: Maternal effects and influence on infant growth in rhesus macaques (Macaca mulatta).

PubMed

Bernstein, Robin M; Hinde, Katie

2016-08-01

Among mammals, numerous bioactive factors in milk vary across mothers and influence offspring outcomes. This emerging area of research has primarily investigated such dynamics within rodent biomedical models, domesticated dairy breeds, and among humans in clinical contexts. Less understood are signaling factors in the milk of non-human primates. Here, we report on multiple bioactive components in rhesus macaque (Macaca mulatta) milk and their associations with maternal and infant characteristics. Milk samples were collected from 59 macaques at multiple time points across lactation in conjunction with maternal and infant morphometrics and life-history animal records. Milk was assayed for adiponectin (APN), epidermal growth factor (EGF) and its receptor (EGF-R), and transforming growth factor beta 2 (TGF-β2 ). Regression models were constructed to assess the contributions of maternal factors on variation in milk bioactives, and on the relationship of this variation to infant body mass and growth. Maternal body mass, parity, social rank, and infant sex were all predictive of concentrations of milk bioactives. Primiparous mothers produced milk with higher adiponectin, but lower EGF, than multiparous mothers. Heavier mothers produced milk with lower EGF and EGF-R, but higher TGF-β2 . Mothers of daughters produced milk with higher TGF-β2 . Mid-ranking mothers produced milk with higher mean EGF and adiponectin concentrations than low-ranking mothers. Milk EGF and EGF-R were positively associated with infant body mass and growth rate. Importantly, these signaling bioactives (APN, EGF, EGF-R, and TGF-β2 ) were significantly correlated with nutritional values of milk. The effects of milk signals remained after controlling for the available energy in milk revealing the added physiological role of non-nutritive milk bioactives in the developing infant. Integrating analyses of energetic and other bioactive components of milk yields an important perspective for interpreting the magnitude, sources, and consequences of inter-individual variation in milk synthesis. Am. J. Primatol. 78:838-850, 2016. © 2016 Wiley Periodicals, Inc. © 2016 Wiley Periodicals, Inc.

Bioavailability of bioactive food compounds: a challenging journey to bioefficacy

PubMed Central

Rein, Maarit J.; Renouf, Mathieu; Cruz‐Hernandez, Cristina; Actis‐Goretta, Lucas; Thakkar, Sagar K.; da Silva Pinto, Marcia

2013-01-01

Bioavailability is a key step in ensuring bioefficacy of bioactive food compounds or oral drugs. Bioavailability is a complex process involving several different stages: liberation, absorption, distribution, metabolism and elimination phases (LADME). Bioactive food compounds, whether derived from various plant or animal sources, need to be bioavailable in order to exert any beneficial effects. Through a better understanding of the digestive fate of bioactive food compounds we can impact the promotion of health and improvement of performance. Many varying factors affect bioavailability, such as bioaccessibility, food matrix effect, transporters, molecular structures and metabolizing enzymes. Bioefficacy may be improved through enhanced bioavailability. Therefore, several technologies have been developed to improve the bioavailability of xenobiotics, including structural modifications, nanotechnology and colloidal systems. Due to the complex nature of food bioactive compounds and also to the different mechanisms of absorption of hydrophilic and lipophilic bioactive compounds, unravelling the bioavailability of food constituents is challenging. Among the food sources discussed during this review, coffee, tea, citrus fruit and fish oil were included as sources of food bioactive compounds (e.g. (poly)phenols and polyunsaturated fatty acids (PUFAs)) since they are examples of important ingredients for the food industry. Although there are many studies reporting on bioavailability and bioefficacy of these bioactive food components, understanding their interactions, metabolism and mechanism of action still requires extensive work. This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds. PMID:22897361

Bioactive Egg Components and Inflammation

PubMed Central

Andersen, Catherine J.

2015-01-01

Inflammation is a normal acute response of the immune system to pathogens and tissue injury. However, chronic inflammation is known to play a significant role in the pathophysiology of numerous chronic diseases, such as cardiovascular disease, type 2 diabetes mellitus, and cancer. Thus, the impact of dietary factors on inflammation may provide key insight into mitigating chronic disease risk. Eggs are recognized as a functional food that contain a variety of bioactive compounds that can influence pro- and anti-inflammatory pathways. Interestingly, the effects of egg consumption on inflammation varies across different populations, including those that are classified as healthy, overweight, metabolic syndrome, and type 2 diabetic. The following review will discuss the pro- and anti-inflammatory properties of egg components, with a focus on egg phospholipids, cholesterol, the carotenoids lutein and zeaxanthin, and bioactive proteins. The effects of egg consumption of inflammation across human populations will additionally be presented. Together, these findings have implications for population-specific dietary recommendations and chronic disease risk. PMID:26389951

Rice Varietal Differences in Bioactive Bran Components for Inhibition of Colorectal Cancer Cell Growth

PubMed Central

Forster, Genevieve M.; Raina, Komal; Kumar, Ajay; Kumar, Sushil; Agarwal, Rajesh; Chen, Ming-Hsuan; Bauer, John E.; McClung, Anna M.; Ryan, Elizabeth P.

2013-01-01

Rice bran chemical profiles differ across rice varieties and have not yet been analyzed for differential chemopreventive bioactivity. A diverse panel of 7 rice bran varieties was analyzed for growth inhibition of human colorectal cancer (CRC) cells. Inhibition varied from 0–99%, depending on the variety of bran used. Across varieties, total lipid content ranged 5–16%, individual fatty acids had 1.4 to 1.9 fold differences, vitamin E isoforms (α-, γ-, δ- tocotrienols and tocopherols) showed 1.3 to 15.2 fold differences, and differences in γ- oryzanol and total phenolics ranged between 100–275 ng/mg and 57–146 ng GAE/mg, respectively. Spearman correlation analysis was used to identify bioactive compounds implicated in CRC cell growth inhibitory activity. Total phenolics and γ- tocotrienol were positively correlated with reduced CRC cell growth (p < 0.05). Stoichiometric variation in rice bran components and differential effects on CRC viability merit further evaluation elucidate their role in dietary CRC chemoprevention. PMID:23790950

Rice varietal differences in bioactive bran components for inhibition of colorectal cancer cell growth.

PubMed

Forster, Genevieve M; Raina, Komal; Kumar, Ajay; Kumar, Sushil; Agarwal, Rajesh; Chen, Ming-Hsuan; Bauer, John E; McClung, Anna M; Ryan, Elizabeth P

2013-11-15

Rice bran chemical profiles differ across rice varieties and have not yet been analysed for differential chemopreventive bioactivity. A diverse panel of seven rice bran varieties was analysed for growth inhibition of human colorectal cancer (CRC) cells. Inhibition varied from 0% to 99%, depending on the variety of bran used. Across varieties, total lipid content ranged 5-16%, individual fatty acids had 1.4- to 1.9-fold differences, vitamin E isoforms (α-, γ-, δ-tocotrienols, and tocopherols) showed 1.3- to 15.2-fold differences, and differences in γ-oryzanol and total phenolics ranged between 100-275ng/mg and 57-146ngGAE/mg, respectively. Spearman correlation analysis was used to identify bioactive compounds implicated in CRC cell growth inhibitory activity. Total phenolics and γ-tocotrienol were positively correlated with reduced CRC cell growth (p<0.05). Stoichiometric variation in rice bran components and differential effects on CRC viability merit further evaluation elucidate their role in dietary CRC chemoprevention. Copyright © 2013 Elsevier Ltd. All rights reserved.

Biomimetic and bioactive nanofibrous scaffolds from electrospun composite nanofibers

PubMed Central

Zhang, YZ; Su, B; Venugopal, J; Ramakrishna, S; Lim, CT

2007-01-01

Electrospinning is an enabling technology that can architecturally (in terms of geometry, morphology or topography) and biochemically fabricate engineered cellular scaffolds that mimic the native extracellular matrix (ECM). This is especially important and forms one of the essential paradigms in the area of tissue engineering. While biomimesis of the physical dimensions of native ECM’s major constituents (eg, collagen) is no longer a fabrication-related challenge in tissue engineering research, conveying bioactivity to electrospun nanofibrous structures will determine the efficiency of utilizing electrospun nanofibers for regenerating biologically functional tissues. This can certainly be achieved through developing composite nanofibers. This article gives a brief overview on the current development and application status of employing electrospun composite nanofibers for constructing biomimetic and bioactive tissue scaffolds. Considering that composites consist of at least two material components and phases, this review details three different configurations of nanofibrous composite structures by using hybridizing basic binary material systems as example. These are components blended composite nanofiber, core-shell structured composite nanofiber, and nanofibrous mingled structure. PMID:18203429

Enzyme-assisted extraction of bioactives from plants.

PubMed

Puri, Munish; Sharma, Deepika; Barrow, Colin J

2012-01-01

Demand for new and novel natural compounds has intensified the development of plant-derived compounds known as bioactives that either promote health or are toxic when ingested. Enhanced release of these bioactives from plant cells by cell disruption and extraction through the cell wall can be optimized using enzyme preparations either alone or in mixtures. However, the biotechnological application of enzymes is not currently exploited to its maximum potential within the food industry. Here, we discuss the use of environmentally friendly enzyme-assisted extraction of bioactive compounds from plant sources, particularly for food and nutraceutical purposes. In particular, we discuss an enzyme-assisted extraction of stevioside from Stevia rebaudiana, as an example of a process of potential value to the food industry. Copyright © 2011 Elsevier Ltd. All rights reserved.

Bioactive Compounds and Their Neuroprotective Effects in Diabetic Complications

PubMed Central

Oh, Yoon Sin

2016-01-01

Hyperglycemia, hyperlipidemia and impaired insulin signaling during the development of diabetes can cause diabetic complications, such as diabetic neuropathy, resulting in significant morbidity and mortality. Although various therapeutics are available for the treatment of diabetic neuropathy, no absolute cure exists, and additional research is necessary to comprehensively understand the underlying pathophysiological pathways. A number of studies have demonstrated the potential health benefits of bioactive compounds, i.e., flavonoids and vitamins, which may be effective as supplementary treatments for diabetes and its complications. In this review, we highlight the most recent reports about the mechanisms of action of bioactive compounds (flavonoids and vitamins) possessing potential neuroprotective properties in diabetic conditions. Additional clinical studies are required to determine the appropriate dose and duration of bioactive compound supplementation for neuroprotection in diabetic patients. PMID:27483315

Isolation, Bioactivity, and Production of ortho-Hydroxydaidzein and ortho-Hydroxygenistein

PubMed Central

Chang, Te-Sheng

2014-01-01

Daidzein and genistein are two major components of soy isoflavones. They exist abundantly in plants and possess multiple bioactivities. In contrast, ortho-hydroxydaidzein (OHD) and ortho-hydroxygenistein (OHG), including 6-hydroxydaidzein (6-OHD), 8-hydroxydaidzein (8-OHD), 3′-hydroxydaidzein (3′-OHD), 6-hydroxygenistein (6-OHG), 8-hydroxygenistein (8-OHG), and 3′-hydroxygenistein (3′-OHG), are rarely found in plants. Instead, they are usually isolated from fermented soybean foods or microbial fermentation broth feeding with soybean meal. Accordingly, the bioactivity of OHD and OHG has been investigated less compared to that of soy isoflavones. Recently, OHD and OHG were produced by genetically engineering microorganisms through gene cloning of cytochrome P450 (CYP) enzyme systems. This success opens up bioactivity investigation and industrial applications of OHD and OHG in the future. This article reviews isolation of OHD and OHG from non-synthetic sources and production of the compounds by genetically modified microorganisms. Several bioactivities, such as anticancer and antimelanogenesis-related activities, of OHD and OHG, are also discussed. PMID:24705463

Effect of Low Temperature Cultivation on the Phytochemical Profile and Bioactivity of Arctic Plants: A Case of Dracocephalum palmatum.

PubMed

Olennikov, Daniil N; Chirikova, Nadezhda K; Kashchenko, Nina I; Gornostai, Tat'yana G; Selyutina, Inessa Yu; Zilfikarov, Ifrat N

2017-11-30

The influence of climatic factors, e.g., low temperature, on the phytochemical composition and bioactivity of the arctic plant Dracocephalum palmatum Steph. ax Willd. (palmate dragonhead), a traditional food and medical herb of Northern Siberia, was investigated. D. palmatum seedlings were grown in a greenhouse experiment at normal (20 °C, NT) and low (1 °C, LT) temperature levels and five groups of components that were lipophilic and hydrophilic in nature were characterized. The analyses indicated that D. palmatum under NT demonstrates high content of photosynthetic pigments, specific fatty acid (FA) profile with domination of saturated FA (53.3%) and the essential oil with trans-pinocamphone as a main component (37.9%). Phenolic compounds were identified using a combination of high performance liquid chromatography with diode array detection and electrospray ionization mass-spectrometric detection (HPLC-DAD-ESI-MS) techniques, as well as free carbohydrates and water soluble polysaccharides. For the first time, it was established that the cold acclimation of D. palmatum seedlings resulted in various changes in physiological and biochemical parameters such as membrane permeability, photosynthetic potential, membrane fluidity, leaf surface secretory function, reactive oxygen species-antioxidant balance, osmoregulator content and cell wall polymers. In brief, results showed that the adaptive strategy of D. palmatum under LT was realized on the accumulation of membrane or surface components with more fluid properties (unsaturated FA and essential oils), antioxidants (phenolic compounds and enzymes), osmoprotectants (free sugars) and cell wall components (polysaccharides). In addition, the occurrence of unusual flavonoids including two new isomeric malonyl esters of eriodictyol-7- O -glucoside was found in LT samples. Data thus obtained allow improving our understanding of ecophysiological mechanisms of cold adaptation of arctic plants.

Polymeric proanthocyanidins from Sicilian pistachio (Pistacia vera L.) nut extract inhibit lipopolysaccharide-induced inflammatory response in RAW 264.7 cells.

PubMed

Gentile, C; Allegra, M; Angileri, F; Pintaudi, A M; Livrea, M A; Tesoriere, L

2012-04-01

Positive effects of pistachio nut consumption on plasma inflammatory biomarkers have been described; however, little is known about molecular events associated with these effects. We studied the anti-inflammatory activity of a hydrophilic extract from Sicilian Pistacia L. (HPE) in a macrophage model and investigated bioactive components relevant to the observed effects. HPE oligomer/polymer proanthocyanidin fractions were isolated by adsorbance chromatography, and components quantified as anthocyanidins after acidic hydrolysis. Isoflavones were measured by gradient elution HPLC analysis. RAW 264.7 murine macrophages were pre-incubated with either HPE (1- to 20-mg fresh nut equivalents) or its isolated components for 1 h, then washed before stimulating with lipopolysaccharide (LPS) for 24 h. Cell viability and parameters associated with Nuclear Factor-κB (NF-κB) activation were assayed according to established methods including ELISA, Western blot, or cytofluorimetric analysis. HPE suppressed nitric oxide (NO) and tumor necrosis factor-α (TNF-α) production and inducible NO-synthase levels dose dependently, whereas inhibited prostaglandin E2 (PGE2) release and decreased cyclo-oxygenase-2 content, the lower the HPE amount the higher the effect. Cytotoxic effects were not observed. HPE also caused a dose-dependent decrease in intracellular reactive oxygen species and interfered with the NF-κB activation. Polymeric proanthocyanidins, but not isoflavones, at a concentration comparable with their content in HPE, inhibited NO, PGE2, and TNF-α formation, as well as activation of IκB-α. Oligomeric proanthocyanidins showed only minor effects. Our results provide molecular evidence of anti-inflammatory activity of pistachio nut and indicate polymeric proanthocyanidins as the bioactive components. The mechanism may involve the redox-sensitive transcription factor NF-κB. Potential effects associated with pistachio nut consumption are discussed in terms of the proanthocyanidin bioavailability.

Effect of Low Temperature Cultivation on the Phytochemical Profile and Bioactivity of Arctic Plants: A Case of Dracocephalum palmatum

PubMed Central

Chirikova, Nadezhda K.; Gornostai, Tat’yana G.; Selyutina, Inessa Yu.; Zilfikarov, Ifrat N.

2017-01-01

The influence of climatic factors, e.g., low temperature, on the phytochemical composition and bioactivity of the arctic plant Dracocephalum palmatum Steph. ax Willd. (palmate dragonhead), a traditional food and medical herb of Northern Siberia, was investigated. D. palmatum seedlings were grown in a greenhouse experiment at normal (20 °C, NT) and low (1 °C, LT) temperature levels and five groups of components that were lipophilic and hydrophilic in nature were characterized. The analyses indicated that D. palmatum under NT demonstrates high content of photosynthetic pigments, specific fatty acid (FA) profile with domination of saturated FA (53.3%) and the essential oil with trans-pinocamphone as a main component (37.9%). Phenolic compounds were identified using a combination of high performance liquid chromatography with diode array detection and electrospray ionization mass-spectrometric detection (HPLC-DAD-ESI-MS) techniques, as well as free carbohydrates and water soluble polysaccharides. For the first time, it was established that the cold acclimation of D. palmatum seedlings resulted in various changes in physiological and biochemical parameters such as membrane permeability, photosynthetic potential, membrane fluidity, leaf surface secretory function, reactive oxygen species–antioxidant balance, osmoregulator content and cell wall polymers. In brief, results showed that the adaptive strategy of D. palmatum under LT was realized on the accumulation of membrane or surface components with more fluid properties (unsaturated FA and essential oils), antioxidants (phenolic compounds and enzymes), osmoprotectants (free sugars) and cell wall components (polysaccharides). In addition, the occurrence of unusual flavonoids including two new isomeric malonyl esters of eriodictyol-7-O-glucoside was found in LT samples. Data thus obtained allow improving our understanding of ecophysiological mechanisms of cold adaptation of arctic plants. PMID:29189749

Electrospun Polyhydroxybutyrate/Poly(ε-caprolactone)/58S Sol-Gel Bioactive Glass Hybrid Scaffolds with Highly Improved Osteogenic Potential for Bone Tissue Engineering.

PubMed

Ding, Yaping; Li, Wei; Müller, Teresa; Schubert, Dirk W; Boccaccini, Aldo R; Yao, Qingqing; Roether, Judith A

2016-07-13

Electrospinning of biopolymer and inorganic substances is one of the efficient ways to combine various advantageous properties in one single fibrous structure with potential for tissue engineering applications. In the present study, to integrate the high stiffness of polyhydroxybutyrate (PHB), the flexibility of poly(ε-caprolactone) (PCL) and the bioactivity of 58S bioactive glass, PHB/PCL/58S sol-gel bioactive glass hybrid scaffolds were fabricated using combined electrospinning and sol-gel method. Physical features such as fiber diameter distribution, mechanical strength and Young's modulus were characterized thoroughly. FTIR analysis demonstrated the successful incorporation of 58S bioactive glass into the blend polymers, which greatly improved the hydrophilicity of PHB/PCL fibermats. The primary biological response of MG-63 osteoblast-like cells on the prepared fibrous scaffolds was evaluated, proving that the 58S glass sol containing hybrid scaffold were not only favorable to MG-63 cell adhesion but also slightly enhanced cell viability and significantly increased alkaline phosphate activity .

Milk derived bioactive peptides and their impact on human health - A review.

PubMed

Mohanty, D P; Mohapatra, S; Misra, S; Sahu, P S

2016-09-01

Milk-derived bioactive peptides have been identified as potential ingredients of health-promoting functional foods. These bioactive peptides are targeted at diet-related chronic diseases especially the non-communicable diseases viz., obesity, cardiovascular diseases and diabetes. Peptides derived from the milk of cow, goat, sheep, buffalo and camel exert multifunctional properties, including anti-microbial, immune modulatory, anti-oxidant, inhibitory effect on enzymes, anti-thrombotic, and antagonistic activities against various toxic agents. Majority of those regulate immunological, gastrointestinal, hormonal and neurological responses, thereby playing a vital role in the prevention of cancer, osteoporosis, hypertension and other disorders as discussed in this review. For the commercial production of such novel bioactive peptides large scale technologies based on membrane separation and ion exchange chromatography methods have been developed. Separation and identification of those peptides and their pharmacodynamic parameters are necessary to transfer their potent functional properties into food applications. The present review summarizes the preliminary classes of bioactive milk-derived peptides along with their physiological functions, general characteristics and potential applications in health-care.

The potential of Ganoderma lucidum extracts as bioactive ingredients in topical formulations, beyond its nutritional benefits.

PubMed

Taofiq, Oludemi; Heleno, Sandrina A; Calhelha, Ricardo C; Alves, Maria José; Barros, Lillian; González-Paramás, Ana M; Barreiro, Maria F; Ferreira, Isabel C F R

2017-10-01

Ganoderma lucidum was characterized in terms of nutritional value and chemical composition. Thereafter, ethanolic Soxhlet extracts were evaluated for antioxidant, anti-inflammatory, antityrosinase, antimicrobial and cytotoxic effects, and further characterized in terms of phenolic acids, polysaccharides and triterpenoids. Finally, the obtained extracts were tested as cosmeceutical ingredients. G. lucidum proved to be a source of macronutrients and important bioactive compounds such as terpenoids, specially triterpenoids, and polysaccharides. In the extracts, ganoderic acids C2, A and H were the most abundant triterpenic acids and protocatechuic, p-hydroxibenzoic and syringic acids the identified phenolics. The developed cosmeceutical formulation preserved the extract bioactivities, presented a light-yellow colour and a pH of 4.6, which is considered appropriate for cosmeceutical's design. Behind the important nutritional/bioactive composition of G. lucidum, a potential towards its valorisation in the field of cosmeceuticals is foreseeable, as deduced from the bioactivities of its ethanolic extract and preservation in the tested formulation. Copyright © 2017 Elsevier Ltd. All rights reserved.

Marine actinobacteria: an important source of bioactive natural products.

PubMed

Manivasagan, Panchanathan; Kang, Kyong-Hwa; Sivakumar, Kannan; Li-Chan, Eunice C Y; Oh, Hyun-Myung; Kim, Se-Kwon

2014-07-01

Marine environment is largely an untapped source for deriving actinobacteria, having potential to produce novel, bioactive natural products. Actinobacteria are the prolific producers of pharmaceutically active secondary metabolites, accounting for about 70% of the naturally derived compounds that are currently in clinical use. Among the various actinobacterial genera, Actinomadura, Actinoplanes, Amycolatopsis, Marinispora, Micromonospora, Nocardiopsis, Saccharopolyspora, Salinispora, Streptomyces and Verrucosispora are the major potential producers of commercially important bioactive natural products. In this respect, Streptomyces ranks first with a large number of bioactive natural products. Marine actinobacteria are unique enhancing quite different biological properties including antimicrobial, anticancer, antiviral, insecticidal and enzyme inhibitory activities. They have attracted global in the last ten years for their ability to produce pharmaceutically active compounds. In this review, we have focused attention on the bioactive natural products isolated from marine actinobacteria, possessing unique chemical structures that may form the basis for synthesis of novel drugs that could be used to combat resistant pathogenic microorganisms. Copyright © 2014 Elsevier B.V. All rights reserved.

Principal component analysis of phenolic acid spectra

USDA-ARS?s Scientific Manuscript database

Phenolic acids are common plant metabolites that exhibit bioactive properties and have applications in functional food and animal feed formulations. The ultraviolet (UV) and infrared (IR) spectra of four closely related phenolic acid structures were evaluated by principal component analysis (PCA) to...

Bioactive formulations prepared from fruiting bodies and submerged culture mycelia of the Brazilian edible mushroom Pleurotus ostreatoroseus Singer.

PubMed

Corrêa, Rúbia Carvalho Gomes; de Souza, Aloisio Henrique Pereira; Calhelha, Ricardo C; Barros, Lillian; Glamoclija, Jasmina; Sokovic, Marina; Peralta, Rosane Marina; Bracht, Adelar; Ferreira, Isabel C F R

2015-07-01

Pleurotus ostreatoroseus is a Brazilian edible mushroom whose chemical characterization and bioactivity still remain underexplored. In this study, the hydrophilic and lipophilic compounds as well as the antioxidant, anti-inflammatory and antimicrobial activities of formulations (ethanol extracts) prepared with its fruiting bodies and submerged culture mycelia were compared. The bioactive formulations contain at least five free sugars, four organic acids, four phenolic compounds and two tocopherols. The fruiting body-based formulation revealed higher reducing power, DPPH scavenging activity, β-carotene bleaching inhibition and lipid peroxidation inhibition in brain homogenates than the mycelium-based preparation, as well as higher anti-inflammatory and antimicrobial activities. The absence of hepatotoxicity was confirmed in porcine liver primary cells. These functional responses can be related to the levels of bioactive components including phenolic acids, organic acids and tocopherols.

Bioactive Properties of Maillard Reaction Products Generated From Food Protein-derived Peptides.

PubMed

Arihara, K; Zhou, L; Ohata, M

Food protein-derived peptides are promising food ingredients for developing functional foods, since various bioactive peptides are released from food proteins. The Maillard reaction, which plays an important role in most processed foods, generates various chemical components during processing. Although changes of amino acids or proteins and reduced sugars by the Maillard reaction have been studied extensively, such changes of peptides by the Maillard reaction are still not resolved enough. Since food protein-derived peptides are widely utilized in many processed foods, it deserves concern and research on the changes of peptides by the Maillard reaction in foods during processing or storage. This chapter initially overviewed food protein-derived bioactive peptides. Then, Maillard reaction products generated from peptides are discussed. We focused particularly on their bioactivities. © 2017 Elsevier Inc. All rights reserved.

Multilayer bioactive glass/zirconium titanate thin films in bone tissue engineering and regenerative dentistry

PubMed Central

Mozafari, Masoud; Salahinejad, Erfan; Shabafrooz, Vahid; Yazdimamaghani, Mostafa; Vashaee, Daryoosh; Tayebi, Lobat

2013-01-01

Surface modification, particularly coatings deposition, is beneficial to tissue-engineering applications. In this work, bioactive glass/zirconium titanate composite thin films were prepared by a sol-gel spin-coating method. The surface features of the coatings were studied by scanning electron microscopy, atomic force microscopy, and spectroscopic reflection analyses. The results show that uniform and sound multilayer thin films were successfully prepared through the optimization of the process variables and the application of carboxymethyl cellulose as a dispersing agent. Also, it was found that the thickness and roughness of the multilayer coatings increase nonlinearly with increasing the number of the layers. This new class of nanocomposite coatings, comprising the bioactive and inert components, is expected not only to enhance bioactivity and biocompatibility, but also to protect the surface of metallic implants against wear and corrosion. PMID:23641155

[ANTIOXIDANT POTENTIAL OF MELIPONA BEECHEII HONEY AND ITS RELATIONSHIP TO HEALTH: A REVIEW].

PubMed

Cauich Kumul, Roger; Ruiz Ruiz, Jorge Carlos; Ortíz Vázquez, Elizabeth; Segura Campos, Maira Rubi

2015-10-01

The present article provides a literature review about the biological potential of Melipona beecheii. The objective is to project some tendecies in research about nutraceutical aspects related to the bioactive compounds presents in the honey of this stingless bee species, known for its medicinal properties traditional, in the Yucatan Peninsula. Currently, there is strong evidence that M. beecheii honey has bioactive compounds such as proteins, flavonoids and polyphenols with high antioxidant activity. The scientific evidence allows to propose to the honey of stingless bee species as a potential alternative for the obtention of bioactive compounds with antioxidant activity in the Yucatan Peninsula and natural food being proposed to reduce some diseases associated with stress oxidative physiological human cells. However, there is still information that explains such antioxidant activity, therefore, according to the literature reviewed, sees the need to address nutraceuticals and functional aspects correlated with the bioactive compounds present in this honey bee. Copyright AULA MEDICA EDICIONES 2014. Published by AULA MEDICA. All rights reserved.

Bitter gourd (Momordica Charantia): A dietary approach to hyperglycemia.

PubMed

Krawinkel, Michael B; Keding, Gudrun B

2006-07-01

Bitter gourd (Momordica charantia) is a vegetable with pantropical distribution. It contains substances with antidiabetic properties such as charantin, vicine, and polypeptide-p, as well as other unspecific bioactive components such as antioxidants. Metabolic and hypoglycemic effects of bitter gourd extracts have been demonstrated in cell culture, animal, and human studies. The mechanism of action, whether it is via regulation of insulin release or altered glucose metabolism and its insulin-like effect, is still under debate. Adverse effects are also known. Nevertheless, bitter gourd has the potential to become a component of the diet or a dietary supplement for diabetic and prediabetic patients. Well-designed interdisciplinary research by nutritionists, medical doctors, and agronomists is needed before a dietary recommendation can be given and a product brought to the market.

Comparative Analysis of the Effects of Hydroxysafflor Yellow A and Anhydrosafflor Yellow B in Safflower Series of Herb Pairs Using Prep-HPLC and a Selective Knock-Out Approach.

PubMed

Qu, Cheng; Wang, Lin-Yan; Jin, Wen-Tao; Tang, Yu-Ping; Jin, Yi; Shi, Xu-Qin; Shang, Li-Li; Shang, Er-Xin; Duan, Jin-Ao

2016-11-06

The flower of Carthamus tinctorius L. (Carthami Flos, safflower), important in traditional Chinese medicine (TCM), is known for treating blood stasis, coronary heart disease, hypertension, and cerebrovascular disease in clinical and experimental studies. It is widely accepted that hydroxysafflor yellow A (HSYA) and anhydrosafflor yellow B (ASYB) are the major bioactive components of many formulae comprised of safflower. In this study, selective knock-out of target components such as HSYA and ASYB by using preparative high performance liquid chromatography (prep-HPLC) followed by antiplatelet and anticoagulation activities evaluation was used to investigate the roles of bioactive ingredients in safflower series of herb pairs. The results showed that both HSYA and ASYB not only played a direct role in activating blood circulation, but also indirectly made a contribution to the total bioactivity of safflower series of herb pairs. The degree of contribution of HSYA in the safflower and its series herb pairs was as follows: Carthami Flos-Ginseng Radix et Rhizoma Rubra (CF-GR) > Carthami Flos-Sappan Lignum (CF-SL) > Carthami Flos-Angelicae Sinensis Radix (CF-AS) > Carthami Flos-Astragali Radix (CF-AR) > Carthami Flos-Angelicae Sinensis Radix (CF-AS) > Carthami Flos-Glycyrrhizae Radix et Rhizoma (CF-GL) > Carthami Flos-Salviae Miltiorrhizae Radix et Rhizoma (CF-SM) > Carthami Flos (CF), and the contribution degree of ASYB in the safflower and its series herb pairs: CF-GL > CF-PS > CF-AS > CF-SL > CF-SM > CF-AR > CF-GR > CF. So, this study provided a significant and effective approach to elucidate the contribution of different herbal components to the bioactivity of the herb pair, and clarification of the variation of herb-pair compatibilities. In addition, this study provides guidance for investigating the relationship between herbal compounds and the bioactivities of herb pairs. It also provides a scientific basis for reasonable clinical applications and new drug development on the basis of the safflower series of herb pairs.

Bioactive Oligosaccharide Natural Products

PubMed Central

McCranie, Emilianne K.; Bachmann, Brian O.

2016-01-01

Oligosaccharide natural products target a wide spectrum of biological processes including disruption of cell wall biosynthesis, interference of bacterial translation, and inhibition of human α-amylase. Correspondingly, oligosaccharides possess potential for development as treatments of such diverse diseases as bacterial infections and type II diabetes. Despite their potent and selective activities and potential clinical relevance, isolated bioactive secondary metabolic oligosaccharides are less prevalent than other classes of natural products and their biosynthesis has received comparatively less attention. This review highlights the unique modes of action and biosynthesis of four classes of bioactive oligosaccharides: the orthosomycins, moenomycins, saccharomicins, and acarviostatins. PMID:24883430

Facilitated Visual Interpretation of Scores in Principal Component Analysis by Bioactivity-Labeling of 1H-NMR Spectra-Metabolomics Investigation and Identification of a New α-Glucosidase Inhibitor in Radix Astragali.

PubMed

Liu, Yueqiu; Nyberg, Nils T; Jäger, Anna K; Staerk, Dan

2017-03-06

Radix Astragali is a component of several traditional medicines used for the treatment of type 2 diabetes in China. Radix Astragali is known to contain isoflavones, which inhibit α-glucosidase in the small intestines, and thus lowers the blood glucose levels. In this study, 21 samples obtained from different regions of China were extracted with ethyl acetate, then the IC50-values were determined, and the crude extracts were analyzed by 1H-NMR spectroscopy. A principal component analysis of the 1H-NMR spectra labeled with their IC50-values, that is, bioactivity-labeled 1H-NMR spectra, showed a clear correlation between spectral profiles and the α-glucosidase inhibitory activity. The loading plot and LC-HRMS/NMR of microfractions indicated that previously unknown long chain ferulates could be partly responsible for the observed antidiabetic activity of Radix Astragali. Subsequent preparative scale isolation revealed a compound not previously reported, linoleyl ferulate (1), showing α-glucosidase inhibitory activity (IC50 0.5 mM) at a level comparable to the previously studied isoflavones. A closely related analogue, hexadecyl ferulate (2), did not show significant inhibitory activity, and the double bonds in the alcohol part of 1 seem to be important structural features for the α-glucosidase inhibitory activity. This proof of concept study demonstrates that bioactivity-labeling of the 1H-NMR spectral data of crude extracts allows global and nonselective identification of individual constituents contributing to the crude extract's bioactivity.

Plant proteases for bioactive peptides release: A review.

PubMed

Mazorra-Manzano, M A; Ramírez-Suarez, J C; Yada, R Y

2017-04-10

Proteins are a potential source of health-promoting biomolecules with medical, nutraceutical, and food applications. Nowadays, bioactive peptides production, its isolation, characterization, and strategies for its delivery to target sites are a matter of intensive research. In vitro and in vivo studies regarding the bioactivity of peptides has generated strong evidence of their health benefits. Dairy proteins are considered the richest source of bioactive peptides, however proteins from animal and vegetable origin also have been shown to be important sources. Enzymatic hydrolysis has been the process most commonly used for bioactive peptide production. Most commercial enzymatic preparations frequently used are from animal (e.g., trypsin and pepsin) and microbial (e.g., Alcalase® and Neutrase®) sources. Although the use of plant proteases is still relatively limited to papain and bromelain from papaya and pineapple, respectively, the application of new plant proteases is increasing. This review presents the latest knowledge in the use and diversity of plant proteases for bioactive peptides release from food proteins including both available commercial plant proteases as well as new potential plant sources. Furthermore, the properties of peptides released by plant proteases and health benefits associated in the control of disorders such as hypertension, diabetes, obesity, and cancer are reviewed.

Aloe Vera for Tissue Engineering Applications

PubMed Central

Rahman, Shekh; Carter, Princeton; Bhattarai, Narayan

2017-01-01

Aloe vera, also referred as Aloe barbadensis Miller, is a succulent plant widely used for biomedical, pharmaceutical and cosmetic applications. Aloe vera has been used for thousands of years. However, recent significant advances have been made in the development of aloe vera for tissue engineering applications. Aloe vera has received considerable attention in tissue engineering due to its biodegradability, biocompatibility, and low toxicity properties. Aloe vera has been reported to have many biologically active components. The bioactive components of aloe vera have effective antibacterial, anti-inflammatory, antioxidant, and immune-modulatory effects that promote both tissue regeneration and growth. The aloe vera plant, its bioactive components, extraction and processing, and tissue engineering prospects are reviewed in this article. The use of aloe vera as tissue engineering scaffolds, gels, and films is discussed, with a special focus on electrospun nanofibers. PMID:28216559

Aloe Vera for Tissue Engineering Applications.

PubMed

Rahman, Shekh; Carter, Princeton; Bhattarai, Narayan

2017-02-14

Aloe vera, also referred as Aloe barbadensis Miller, is a succulent plant widely used for biomedical, pharmaceutical and cosmetic applications. Aloe vera has been used for thousands of years. However, recent significant advances have been made in the development of aloe vera for tissue engineering applications. Aloe vera has received considerable attention in tissue engineering due to its biodegradability, biocompatibility, and low toxicity properties. Aloe vera has been reported to have many biologically active components. The bioactive components of aloe vera have effective antibacterial, anti-inflammatory, antioxidant, and immune-modulatory effects that promote both tissue regeneration and growth. The aloe vera plant, its bioactive components, extraction and processing, and tissue engineering prospects are reviewed in this article. The use of aloe vera as tissue engineering scaffolds, gels, and films is discussed, with a special focus on electrospun nanofibers.

Green Tea Extracts Epigallocatechin-3-gallate for Different Treatments

PubMed Central

Chu, Chenyu; Deng, Jia

2017-01-01

Epigallocatechin-3-gallate (EGCG), a component extracted from green tea, has been proved to have multiple effects on human pathological and physiological processes, and its mechanisms are discrepant in cancer, vascularity, bone regeneration, and nervous system. Although there are multiple benefits associated with EGCG, more and more challenges are still needed to get through. For example, EGCG shows low bioactivity via oral administration. This review focuses on effects of EGCG, including anti-cancer, antioxidant, anti-inflammatory, anticollagenase, and antifibrosis effects, to express the potential of EGCG and necessity of further studies in this field. PMID:28884125

Dietary Natural Products for Prevention and Treatment of Liver Cancer

PubMed Central

Zhou, Yue; Li, Ya; Zhou, Tong; Zheng, Jie; Li, Sha; Li, Hua-Bin

2016-01-01

Liver cancer is the most common malignancy of the digestive system with high death rate. Accumulating evidences suggests that many dietary natural products are potential sources for prevention and treatment of liver cancer, such as grapes, black currant, plum, pomegranate, cruciferous vegetables, French beans, tomatoes, asparagus, garlic, turmeric, ginger, soy, rice bran, and some edible macro-fungi. These dietary natural products and their active components could affect the development and progression of liver cancer in various ways, such as inhibiting tumor cell growth and metastasis, protecting against liver carcinogens, immunomodulating and enhancing effects of chemotherapeutic drugs. This review summarizes the potential prevention and treatment activities of dietary natural products and their major bioactive constituents on liver cancer, and discusses possible mechanisms of action. PMID:26978396

Hericium erinaceus: an edible mushroom with medicinal values.

PubMed

Khan, Md Asaduzzaman; Tania, Mousumi; Liu, Rui; Rahman, Mohammad Mijanur

2013-05-24

Mushrooms are considered as nutritionally functional foods and source of physiologically beneficial medicines. Hericium erinaceus, also known as Lion's Mane Mushroom or Hedgehog Mushroom, is an edible fungus, which has a long history of usage in traditional Chinese medicine. This mushroom is rich in some physiologically important components, especially β-glucan polysaccharides, which are responsible for anti-cancer, immuno-modulating, hypolipidemic, antioxidant and neuro-protective activities of this mushroom. H. erinaceus has also been reported to have anti-microbial, anti-hypertensive, anti-diabetic, wound healing properties among other therapeutic potentials. This review article has overviewed the recent advances in the research and study on H. erinaceus and discussed the potential health beneficial activities of this mushroom, with the recognition of bioactive compounds responsible for these medicinal properties.

Valuable Nutrients and Functional Bioactives in Different Parts of Olive (Olea europaea L.)—A Review

PubMed Central

Ghanbari, Rahele; Anwar, Farooq; Alkharfy, Khalid M.; Gilani, Anwarul-Hassan; Saari, Nazamid

2012-01-01

The Olive tree (Olea europaea L.), a native of the Mediterranean basin and parts of Asia, is now widely cultivated in many other parts of the world for production of olive oil and table olives. Olive is a rich source of valuable nutrients and bioactives of medicinal and therapeutic interest. Olive fruit contains appreciable concentration, 1–3% of fresh pulp weight, of hydrophilic (phenolic acids, phenolic alchohols, flavonoids and secoiridoids) and lipophilic (cresols) phenolic compounds that are known to possess multiple biological activities such as antioxidant, anticarcinogenic, antiinflammatory, antimicrobial, antihypertensive, antidyslipidemic, cardiotonic, laxative, and antiplatelet. Other important compounds present in olive fruit are pectin, organic acids, and pigments. Virgin olive oil (VOO), extracted mechanically from the fruit, is also very popular for its nutritive and health-promoting potential, especially against cardiovascular disorders due to the presence of high levels of monounsaturates and other valuable minor components such as phenolics, phytosterols, tocopherols, carotenoids, chlorophyll and squalene. The cultivar, area of production, harvest time, and the processing techniques employed are some of the factors shown to influence the composition of olive fruit and olive oil. This review focuses comprehensively on the nutrients and high-value bioactives profile as well as medicinal and functional aspects of different parts of olives and its byproducts. Various factors affecting the composition of this food commodity of medicinal value are also discussed. PMID:22489153

Bioactivities and Health Benefits of Wild Fruits

PubMed Central

Li, Ya; Zhang, Jiao-Jiao; Xu, Dong-Ping; Zhou, Tong; Zhou, Yue; Li, Sha; Li, Hua-Bin

2016-01-01

Wild fruits are exotic or underutilized. Wild fruits contain many bioactive compounds, such as anthocyanins and flavonoids. Many studies have shown that wild fruits possess various bioactivities and health benefits, such as free radical scavenging, antioxidant, anti-inflammatory, antimicrobial, and anticancer activity. Therefore, wild fruits have the potential to be developed into functional foods or pharmaceuticals to prevent and treat several chronic diseases. In the present article, we review current knowledge about the bioactivities and health benefits of wild fruits, which is valuable for the exploitation and utilization of wild fruits. PMID:27527154

Polyethylene glycol grafted polyethylene: a versatile platform for nonmigratory active packaging applications.

PubMed

Barish, Jeffrey A; Goddard, Julie M

2011-01-01

Nonmigratory active packaging, in which bioactive components are tethered to the package, offers the potential to reduce the need for additives in food products while maintaining safety and quality. A challenge in developing nonmigratory active packaging materials is the loss of biomolecular activity that can occur when biomolecules are immobilized. In this work, we describe a method in which a biocompatible polymer (polyethylene glycol, PEG) is grafted from the surface of ozone-treated low-density polyethylene (LDPE) resulting in a surface functionalized polyethylene to which a range of amine-terminated bioactive molecules can be immobilized. Free radical graft polymerization is used to graft PEG onto the LDPE surface, followed by immobilization of ethylenediamine onto the PEG tether. Ethylenediamine was used to demonstrate that amine-terminated molecules could be covalently attached to the PEG-grafted film. Changes in surface chemistry and topography were measured by attenuated total reflectance Fourier transform infrared spectroscopy, contact angle, atomic force microscopy, scanning electron microscopy, and X-ray photoelectron spectroscopy. We demonstrate the ability to graft PEG onto the surface of polymer packaging films by free radical graft polymerization, and to covalently link an amine-terminated molecule to the PEG tether, demonstrating that amine-terminated bioactive compounds (such as peptides, enzymes, and some antimicrobials) can be immobilized onto PEG-grafted LDPE in the development of nonmigratory active packaging.   Nonmigratory active packaging offers the potential for improving food safety and quality while minimizing the migration of the active agent into food. In this paper, we describe a technique to modify polyethylene packaging films such that active agents can be covalently immobilized by a biocompatible tether. Such a technique can be adapted to a number of applications such as antimicrobial, antioxidant, or immobilized enzyme active packaging. © 2011 Institute of Food Technologists®

Mixed Network Former Effect on Structure, Physical Properties, and Bioactivity of 45S5 Bioactive Glasses: An Integrated Experimental and Molecular Dynamics Simulation Study.

PubMed

Lu, Xiaonan; Deng, Lu; Huntley, Caitlin; Ren, Mengguo; Kuo, Po-Hsuen; Thomas, Ty; Chen, Jonathan; Du, Jincheng

2018-03-08

Boron-containing bioactive glasses display a strong potential in various biomedical applications lately due to their controllable dissolution rates. In this paper, we prepared a series of B 2 O 3 /SiO 2 -substituded 45S5 bioactive glasses and performed in vitro biomineralization tests with both simulated body fluid and K 2 HPO 4 solutions to evaluate the bioactivities of these glasses as a function of boron oxide to silica substitution. The samples were examined with scanning electron microscopy, X-ray diffraction, and Fourier transform infrared spectrometry after immersing them in the two solutions (simulated body fluid and K 2 HPO 4 ) up to 3 weeks. It was found that introduction of boron oxide delayed the formation of hydroxyapatite, but all the glasses were shown to be bioactive. Molecular dynamics (MD) simulations were used to complement the experimental efforts to understand the structural changes due to boron oxide to silica substitution by using newly developed partial charge composition-dependent potentials. Local structures around the glass network formers, medium-range structural information, network connectivity, and self-diffusion coefficients of ions were elucidated from MD simulation. Relationships between boron content and glass properties such as structure, density, glass transition temperature, and in vitro bioactivity were discussed in light of both experimental and simulation results.

Enhancing the Bioactivity of Yttria-Stabilized Tetragonal Zirconia Ceramics via Grain-Boundary Activation.

PubMed

Ke, Jinhuan; He, Fupo; Ye, Jiandong

2017-05-17

Yttria-stabilized tetragonal zirconia (Y-TZP) has been proposed as a potential dental implant because of its good biocompatibility, excellent mechanical properties, and distinctive aesthetic effect. However, Y-TZP cannot form chemical bonds with bone tissue because of its biological inertness, which affects the reliability and long-term efficacy of Y-TZP implants. In this study, to improve the bioactivity of Y-TZP ceramics while maintaining their good mechanical performance, Y-TZP was modified by grain-boundary activation via the infiltration of a bioactive glass (BG) sol into the surface layers of Y-TZP ceramics under different negative pressures (atmospheric pressure, -0.05 kPa, and -0.1 kPa), followed by gelling and sintering. The in vitro bioactivity, mechanical properties, and cell behavior of the Y-TZP with improved bioactivity were systematically investigated using X-ray diffraction (XRD), scanning electron microscopy (SEM), energy-dispersive spectrometry (EDS), electron probe microanalysis (EPMA), and Raman spectroscopy. The results of the bioactivity test conducted by immersing Y-TZP in simulated body fluid (SBF) showed that a bonelike apatite layer was produced on the entire surface. The mechanical properties of the modified Y-TZP decreased as the negative pressure in the BG-infiltration process increased relative to those of the Y-TZP blank group. However, the samples infiltrated with the BG sol under -0.05 kPa and atmospheric pressure still retained good mechanical performance. The cell-culture results revealed that the bioactive surface modification of Y-TZP could promote cell adhesion and differentiation. The present work demonstrates that the bioactivity of Y-TZP can be enhanced by grain-boundary activation, and the bioactive Y-TZP is expected to be a potential candidate for use as a dental implant material.

Food formats for effective delivery of probiotics.

PubMed

Sanders, Mary Ellen; Marco, Maria L

2010-01-01

Probiotic bacteria are increasingly incorporated into food products intended to confer health benefits in the human gut and beyond. Little is known about how the food matrix and product formulation impacts probiotic functionality, even though such information is essential to scientific understanding and regulatory substantiation of health benefits. The food format has the potential to affect probiotic survival, physiology, and potentially efficacy, but few comparative studies in humans have been conducted. Human studies should account for the effects of the food base on human health and the bioactive components present in the foods that may augment or diminish interactions of the probiotic with the human host. Some studies show that food ingredients such as prebiotics and milk components can improve probiotic survival during the shelf life of foods, which may enhance probiotic efficacy through increased dose effects. Furthermore, there are indications that synbiotic products are more effective than either probiotics or prebiotics alone. Identification of probiotic adaptations to the food and gut environments holds promise for determining the specific cell components and potential bacterial-food interactions necessary for health benefits and determining how these factors are affected by changes in food formulation and host diet. These studies, combined with controlled human studies, are important future research activities for advancing this field.

Bioavailability of bioactive food compounds: a challenging journey to bioefficacy.

PubMed

Rein, Maarit J; Renouf, Mathieu; Cruz-Hernandez, Cristina; Actis-Goretta, Lucas; Thakkar, Sagar K; da Silva Pinto, Marcia

2013-03-01

Bioavailability is a key step in ensuring bioefficacy of bioactive food compounds or oral drugs. Bioavailability is a complex process involving several different stages: liberation, absorption, distribution, metabolism and elimination phases (LADME). Bioactive food compounds, whether derived from various plant or animal sources, need to be bioavailable in order to exert any beneficial effects. Through a better understanding of the digestive fate of bioactive food compounds we can impact the promotion of health and improvement of performance. Many varying factors affect bioavailability, such as bioaccessibility, food matrix effect, transporters, molecular structures and metabolizing enzymes. Bioefficacy may be improved through enhanced bioavailability. Therefore, several technologies have been developed to improve the bioavailability of xenobiotics, including structural modifications, nanotechnology and colloidal systems. Due to the complex nature of food bioactive compounds and also to the different mechanisms of absorption of hydrophilic and lipophilic bioactive compounds, unravelling the bioavailability of food constituents is challenging. Among the food sources discussed during this review, coffee, tea, citrus fruit and fish oil were included as sources of food bioactive compounds (e.g. (poly)phenols and polyunsaturated fatty acids (PUFAs)) since they are examples of important ingredients for the food industry. Although there are many studies reporting on bioavailability and bioefficacy of these bioactive food components, understanding their interactions, metabolism and mechanism of action still requires extensive work. This review focuses on some of the major factors affecting the bioavailability of the aforementioned bioactive food compounds. © 2012 Nestec S. A.. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.

Analysing the bioactive makeup of demineralised dentine matrix on bone marrow mesenchymal stem cells for enhanced bone repair.

PubMed

Avery, S J; Sadaghiani, L; Sloan, A J; Waddington, R J

2017-07-10

Dentine matrix has proposed roles for directing mineralised tissue repair in dentine and bone; however, the range of bioactive components in dentine and specific biological effects on bone-derived mesenchymal stem cells (MSCs) in humans are less well understood. The aims of this study were to further elucidate the biological response of MSCs to demineralised dentine matrix (DDM) in enhancing wound repair responses and ascertain key contributing components. Dentine was obtained from human teeth and DDM proteins solubilised with ethylenediaminetetraacetic acid (EDTA). Bone marrow derived MSCs were commercially obtained. Cells with a more immature phenotype were then selected by preferential fibronectin adhesion (FN-BMMSCs) for use in subsequent in vitro assays. DDM at 10 µg/mL reduced cell expansion, attenuated apoptosis and was the minimal concentration capable of inducing osteoblastic differentiation. Enzyme-linked immunosorbent assay (ELISA) quantification of growth factors indicated physiological levels produced the above responses; transforming growth factor β (TGF-β1) was predominant (15.6 ng/mg DDM), with relatively lower concentrations of BMP-2, FGF, VEGF and PDGF (6.2-4.7 ng/mg DDM). Fractionation of growth factors from other DDM components by heparin affinity chromatography diminished osteogenic responses. Depletion of biglycan from DDM also attenuated osteogenic potency, which was partially rescued by the isolated biglycan. Decorin depletion from DDM had no influence on osteogenic potency. Collectively, these results demonstrate the potential of DDM for the delivery of physiological levels of growth factors for bone repair processes, and substantiate a role for biglycan as an additional adjuvant for driving osteogenic pathways.

Spark Plasma Sintering of Load-Bearing Iron-Carbon Nanotube-Tricalcium Phosphate CerMets for Orthopaedic Applications

NASA Astrophysics Data System (ADS)

Montufar, Edgar B.; Horynová, Miroslava; Casas-Luna, Mariano; Diaz-de-la-Torre, Sebastián; Celko, Ladislav; Klakurková, Lenka; Spotz, Zdenek; Diéguez-Trejo, Guillermo; Fohlerová, Zdenka; Dvorak, Karel; Zikmund, Tomáš; Kaiser, Jozef

2016-04-01

Recently, ceramic-metallic composite materials (CerMets) have been investigated for orthopaedic applications with promising results. This first generation of bio-CerMets combine the bioactivity of hydroxyapatite with the mechanical stability of titanium to fabricate bioactive, tough and biomechanically more biocompatible osteosynthetic devices. Nonetheless, these first CerMets are not biodegradable materials and a second surgery is required to remove the implant after bone healing. The present work aims to develop the next generation bio-CerMets, which are potential biodegradable materials. The process to produce the new biodegradable CerMet consisted of mixing powder of soluble and osteoconductive alpha tricalcium phosphate with biocompatible and biodegradable iron with consolidation through spark plasma sintering (SPS). The microstructure, composition and mechanical strength of the new CerMet were studied by metallography, x-ray diffraction and diametral tensile strength tests, respectively. The results show that SPS produces CerMet with higher mechanical performance (120 MPa) than the ceramic component alone (29 MPa) and similar mechanical strength to the pure metallic component (129 MPa). Nonetheless, although a short sintering time (10 min) was used, partial transformation of the alpha tricalcium phosphate into its allotropic and slightly less soluble beta phase was observed. Cell adhesion tests show that osteoblasts are able to attach to the CerMet surface, presenting spread morphology regardless of the component of the material with which they are in contact. However, the degradation process restricted to the small volume of the cell culture well quickly reduces the osteoblast viability.

Persimmon (Diospyros kaki) fruit: hidden phytochemicals and health claims

PubMed Central

Butt, Masood Sadiq; Sultan, M. Tauseef; Aziz, Mahwish; Naz, Ambreen; Ahmed, Waqas; Kumar, Naresh; Imran, Muhammad

2015-01-01

Currently, nutrition and health linkages focused on emerging strategy of diet based regimen to combat various physiological threats including cardiovascular disorders, oxidative stress, diabetes mellitus, etc. In this context, consumption of fruits and vegetables is gaining considerable importance as safeguard to maintain human health. Likewise, their phytochemicals and bioactive molecules are also becoming popular as promising demulcent against various ailments. The current review is an effort to sum up information regarding persimmon fruit with special reference to its phytochemistry and associated health claims. Accordingly, the role of its certain bioactive molecules like proanthocyanidin, carotenoids, tannins, flavonoids, anthocyanidin, catechin, etc. is highlighted. Owing to rich phytochemistry, persimmon and its products are considered effective in mitigating oxidative damage induced by reactive oxygen species (ROS). The antioxidant potential is too responsible for anti-malignant and anti-melanogenic perspectives of persimmon functional ingredients. Additionally, they are effectual in soothing lifestyle related disparities e.g. cardiovascular disorders and diabetes mellitus. There are proven facts that pharmacological application of persimmon or its functional ingredients like proanthocyanidin may helps against hyperlipidemia and hyperglycemia. Nevertheless, astringent taste and diospyrobezoars formation are creating lacuna to prop up its vitality. In toto, persimmon and its components hold potential as one of effective modules in diet based therapy; however, integrated research and meta-analysis are still required to enhance meticulousness. PMID:27047315

Gelatin/nano-hydroxyapatite hydrogel scaffold prepared by sol-gel technology as filler to repair bone defects.

PubMed

Raucci, Maria Grazia; Demitri, Christian; Soriente, Alessandra; Fasolino, Ines; Sannino, Alessandro; Ambrosio, Luigi

2018-03-25

This study reports on the development of a scaffold with a gradient of bioactive solid signal embedded in the biodegradable polymer matrix by combining a sol-gel approach and freeze-drying technology. The chemical approach based on the sol-gel transition of calcium phosphates ensures the particles dispersion into the gelatin matrix and a direct control of interaction among COOH gelatin /Ca 2+ ions. Morphological analysis demonstrated that on the basis of the amount of inorganic component and by using specific process conditions, it is possible to control the spatial distribution of nanoparticles around the gelatin helix. In fact, methodology and formulations were able to discriminate between the different hydroxyapatite concentrations and their respective morphology. The good biological response represented by good cell attachment, proliferation and increased levels of alkaline phosphatase as an indicator of osteoblastic differentiation of human mesenchymal stem cells toward the osteogenic lineage, demonstrating the effect of bioactive solid signals on cellular behavior. Furthermore, the inhibition of reactive oxygen species production by composite materials predicted potential anti-inflammatory properties of scaffolds thus confirming their biocompatibility. Indeed, these interesting biological results suggest good potential application of this scaffold as filler to repair bone defects. © 2018 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2018. © 2018 Wiley Periodicals, Inc.

New beverages of lemon juice enriched with the exotic berries maqui, açaı́, and blackthorn: bioactive components and in vitro biological properties.

PubMed

Gironés-Vilaplana, Amadeo; Valentão, Patrícia; Moreno, Diego A; Ferreres, Federico; García-Viguera, Cristina; Andrade, Paula B

2012-07-04

Following previous research on lemon juice enriched with berries, the aim of this work was to design new blends based on lemon juice mixed with different edible berries of exotic and national origin: maqui ( Aristotelia chilensis (Molina) Stuntz), açaı́ ( Euterpe oleracea Mart.), and blackthorn ( Prunus spinosa L.). The phytochemical characterization of controls and blends was performed by HPLC-DAD-ESI/MS(n). Their antioxidant capacity against DPPH, superoxide, and hydroxyl radicals and hypochlorous acid and their potential to inhibit cholinesterases were also assessed. The profiling of the red fruits and lemon revealed a wide range of bioactive phenolics. The novel beverage based on lemon juice and maqui berry (LM) was the most interesting blend in terms of antioxidant capacity. Berry control samples displayed reduced effects on acetylcholinesterase and butyrylcholinesterase, the lemon juice control being always the most active. This activity was also remarkable for lemon-blackthorn (LB) and lemon-açaı́ (LA) blends, the last being the most effective inhibitor of cholinesterases among all samples. The results suggested that lemon juice enriched with berries could be of potential interest in the design of new drinks with a nutritive related function on health for chronic diseases.

Absorption Profile of (Poly)Phenolic Compounds after Consumption of Three Food Supplements Containing 36 Different Fruits, Vegetables, and Berries

PubMed Central

Bresciani, Letizia; Martini, Daniela; Mena, Pedro; Tassotti, Michele; Calani, Luca; Brigati, Giacomo; Brighenti, Furio; Holasek, Sandra; Malliga, Daniela-Eugenia; Lamprecht, Manfred; Del Rio, Daniele

2017-01-01

The market of plant-based nutraceuticals and food supplements is continuously growing due to the increased consumer demand. The introduction of new products with relevant nutritional characteristics represents a new way of providing bioactive compounds and (poly)phenols to consumers, becoming a strategy to ideally guarantee the health benefits attributed to plant foodstuffs and allowing the increase of daily bioactive compound intake. A paramount step in the study of nutraceuticals is the evaluation of the bioavailability and metabolism of their putatively active components. Therefore, the aim of the present study was to investigate the absorption profile of the (poly)phenolic compounds contained in three different plant-based food supplements, made of 36 different plant matrices, which were consumed by 20 subjects in an open one-arm study design. Blood samples were collected at baseline and 1, 2, 5, and 10 h after capsule intake. Twenty quantifiable metabolites deriving from different (poly)phenolic compounds were identified. Results showed that the consumption of the three capsules allowed the effective absorption of several (poly)phenolic compounds and metabolites appearing at different times in plasma, thereby indicating different absorption profiles. The capsules thus ensured potential health-promoting molecules to be potentially available to target tissues and organs. PMID:28245627

Isolation, Characterization, and Antibacterial Activity of Hard-to-Culture Actinobacteria from Cave Moonmilk Deposits.

PubMed

Adam, Delphine; Maciejewska, Marta; Naômé, Aymeric; Martinet, Loïc; Coppieters, Wouter; Karim, Latifa; Baurain, Denis; Rigali, Sébastien

2018-03-22

Cave moonmilk deposits host an abundant and diverse actinobacterial population that has a great potential for producing novel natural bioactive compounds. In our previous attempt to isolate culturable moonmilk-dwelling Actinobacteria, only Streptomyces species were recovered, whereas a metagenetic study of the same deposits revealed a complex actinobacterial community including 46 actinobacterial genera in addition to streptomycetes. In this work, we applied the rehydration-centrifugation method to lessen the occurrence of filamentous species and tested a series of strategies to achieve the isolation of hard-to-culture and rare Actinobacteria from the moonmilk deposits of the cave "Grotte des Collemboles". From the "tips and tricks" that were tested, separate autoclaving of the components of the International Streptomyces Project (ISP) medium number 5 (ISP5) medium, prolonged incubation time, and dilution of the moonmilk suspension were found to most effectively improve colony forming units. Taxonomic analyses of the 40 isolates revealed new representatives of the Agromyces , Amycolatopsis , Kocuria , Micrococcus , Micromonospora , Nocardia , and Rhodococcus species, as well as additional new streptomycetes. The applied methodologies allowed the isolation of strains associated with both the least and most abundant moonmilk-dwelling actinobacterial operational taxonomic units. Finally, bioactivity screenings revealed that some isolates displayed high antibacterial activities, and genome mining uncovered a strong potential for the production of natural compounds.

Absorption Profile of (Poly)Phenolic Compounds after Consumption of Three Food Supplements Containing 36 Different Fruits, Vegetables, and Berries.

PubMed

Bresciani, Letizia; Martini, Daniela; Mena, Pedro; Tassotti, Michele; Calani, Luca; Brigati, Giacomo; Brighenti, Furio; Holasek, Sandra; Malliga, Daniela-Eugenia; Lamprecht, Manfred; Del Rio, Daniele

2017-02-26

The market of plant-based nutraceuticals and food supplements is continuously growing due to the increased consumer demand. The introduction of new products with relevant nutritional characteristics represents a new way of providing bioactive compounds and (poly)phenols to consumers, becoming a strategy to ideally guarantee the health benefits attributed to plant foodstuffs and allowing the increase of daily bioactive compound intake. A paramount step in the study of nutraceuticals is the evaluation of the bioavailability and metabolism of their putatively active components. Therefore, the aim of the present study was to investigate the absorption profile of the (poly)phenolic compounds contained in three different plant-based food supplements, made of 36 different plant matrices, which were consumed by 20 subjects in an open one-arm study design. Blood samples were collected at baseline and 1, 2, 5, and 10 h after capsule intake. Twenty quantifiable metabolites deriving from different (poly)phenolic compounds were identified. Results showed that the consumption of the three capsules allowed the effective absorption of several (poly)phenolic compounds and metabolites appearing at different times in plasma, thereby indicating different absorption profiles. The capsules thus ensured potential health-promoting molecules to be potentially available to target tissues and organs.

Vortex-ultrasound-assisted dispersive liquid-liquid microextraction coupled with gas chromatography-mass spectrometry for the analysis of volatile bioactive components and comparative pharmacokinetic study of the herb-herb interactions in Guanxin Shutong Capsule.

PubMed

Mu, Jingqing; Gao, Xun; Li, Qing; Yang, Xiaomei; Yang, Wenling; Sun, Xu; Bi, Kaishun; Zhang, Huifen

2017-08-01

Guanxin Shutong Capsule, an effective traditional Chinese medicine, is widely used for coronary heart disease clinically. Volatile components are one of its important bioactive constituents. To better understand the material basis for the therapeutic effects, the components of Guanxin Shutong Capsule absorbed into the blood and their metabolites were identified based on gas chromatography with mass spectrometry coupled with vortex-ultrasound-assisted dispersive liquid-liquid microextraction. As a result, three prototypes and 15 metabolites were identified or tentatively characterized in rat plasma. Subsequently, a pharmacokinetic study was carried out to monitor the concentrations of the main bioactive constituents and metabolites (isoborneol, borneol, eugenol, and camphor) by gas chromatography with mass spectrometry in rat plasma following oral administration of single herb extract and different combinations of herbs in this prescription. Compared to other groups, a statistically significant difference of the pharmacokinetic properties was obtained when the total complex prescription was administered, indicating possible drug-drug interactions among the complex ingredients of Guanxin Shutong Capsule. These findings provided an experimental basis concerning the clinical application and medicinal efficacy of Guanxin Shutong Capsule in the treatment of coronary heart disease. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Enzyme-assistant extraction (EAE) of bioactive components: a useful approach for recovery of industrially important metabolites from seaweeds: a review.

PubMed

Wijesinghe, W A J P; Jeon, You-Jin

2012-01-01

Over the years, the biological activities of seaweeds could have gained a considerable research interest because of their specific functional compounds, which may not be available in land plants. Thus, efforts at discovery of novel metabolites from seaweeds over the past years have yielded a considerable amount of new active compounds. In addition, studies about the extraction of active compounds from natural products have attracted special attention in the last recent years. Potent biologically active compounds of seaweeds have been demonstrated to play a significant role in prevention of certain degenerative diseases such as cancer, inflammation, arthritis, diabetes and hypertension. Therefore, seaweed derived active components, whose immense biochemical diversity looks like to become a rich source of novel chemical entities for the use as functional ingredients in many industrial applications such as functional foods, pharmaceuticals and cosmeceuticals. Thus, the interest in the extraction of active compounds from seaweeds is obvious. However, the physical and chemical barriers of the plant material become the key drawbacks of such extraction process. Therefore, enhanced release and recovery of active compounds attached to the cells have been addressed. Taken together, the aim of this communication is to discuss the potential use of enzyme treatment as a tool to improve the extraction efficiency of bioactive compounds from seaweeds. Copyright © 2011 Elsevier B.V. All rights reserved.

Bioactivity of gel-glass powders in the CaO-SiO2 system: a comparison with ternary (CaO-P2O5-SiO2) and quaternary glasses (SiO2-CaO-P2O5-Na2O).

PubMed

Saravanapavan, Priya; Jones, Julian R; Pryce, Russell S; Hench, Larry L

2003-07-01

Bioactive glasses react chemically with body fluids in a manner that is compatible with the repair processes of the tissues. This results in the formation of an interfacial bond between the glasses and living tissue. Bioactive glasses also stimulate bone-cell proliferation. This behavior is dependent on the chemical composition as well as the surface texture of the glasses. It has been recently reported that gel-derived monolith specimens in the binary SiO2 - CaO are bioactive over a similar molar range of SiO2 content as the previously studied ternary CaO-P2O5-SiO2 system. In this report, the preparation and bioactivity of the binary gel-glass powder with 70 mol % SiO2 is discussed and its bioactivity is compared with the melt-derived 45S5 (quaternary) Bioglass and sol-gel-derived 58S (ternary) bioactive gel-glass compositions. Dissolution kinetic parameters K(1) and K(2) were also computed based on the silicon release for all glass powders. It was shown that the simple two-component SiO2-CaO gel-glass powder is bioactive with comparable dissolution rates as the clinically used melt-derived 45S5 Bioglass powder and extensively studied sol-gel-derived 58S gel-glass powder. Copyright 2003 Wiley Periodicals, Inc.

In vitro fermentation patterns of rice bran components by human gut microbiota

USDA-ARS?s Scientific Manuscript database

Rice bran is a rich source of bioactive components that can promote gastrointestinal health. However, bran is removed during polishing. Among those, feruloylated arabinoxylan oligosaccharides (FAXO) and rice bran polyphenolics (RBPP) are hypothesized to have positive impacts on human gut microbiota ...

Black garlic: A critical review of its production, bioactivity, and application.

PubMed

Kimura, Shunsuke; Tung, Yen-Chen; Pan, Min-Hsiung; Su, Nan-Wei; Lai, Ying-Jang; Cheng, Kuan-Chen

2017-01-01

Black garlic is obtained from fresh garlic (Allium sativum L.) that has been fermented for a period of time at a controlled high temperature (60-90°C) under controlled high humidity (80-90%). When compared with fresh garlic, black garlic does not release a strong offensive flavor owing to the reduced content of allicin. Enhanced bioactivity of black garlic compared with that of fresh garlic is attributed to its changes in physicochemical properties. Studies concerning the fundamental findings of black garlic, such as its production, bioactivity, and applications, have thus been conducted. Several types of black garlic products are also available in the market with a fair selling volume. In this article, we summarize the current knowledge of changes in the components, bioactivity, production, and applications of black garlic, as well as the proposed future prospects on their possible applications as a functional food product. Copyright © 2016. Published by Elsevier B.V.

Effects of drying processes on starch-related physicochemical properties, bioactive components and antioxidant properties of yam flours.

PubMed

Chen, Xuetao; Li, Xia; Mao, Xinhui; Huang, Hanhan; Wang, Tingting; Qu, Zhuo; Miao, Jing; Gao, Wenyuan

2017-06-01

The effects of five different drying processes, air drying (AD), sulphur fumigation drying (SFD), hot air drying (HAD), freeze drying (FD) and microwave drying (MWD) for yams in terms of starch-related properties and antioxidant activity were studied. From the results of scanning electron microscopy (SEM), polarized optical microscopy (POM), X-ray diffraction (XRD), and Fourier transform infrared (FT-IR), the MWD sample was found to contain gelatinized starch granules. The FD yam had more slow digestible (SDS) and resistant starches (RS) compared with those processed with other modern drying methods. The bioactive components and the reducing power of the dried yams, were lower than those of fresh yam. When five dried samples were compared by principal component analysis, the HAD and SFD samples were observed to have the highest comprehensive principal component values. Based on our results, HAD would be a better method for yam drying than the more traditional SFD. Copyright © 2016 Elsevier Ltd. All rights reserved.

Bioactive Materials in Endodontics: An Evolving Component of Clinical Dentistry.

PubMed

Mohapatra, Satyajit; Patro, Swadheena; Mishra, Sumita

2016-06-01

Achieving biocompatibility in a material requires an interdisciplinary approach that involves a sound knowledge of materials science, bioengineering, and biotechnology. The host microbial-material response is also critical. Endodontic treatment is a delicate procedure that must be planned and executed properly. Despite major advances in endodontic therapy in recent decades, clinicians are confronted with a complex root canal anatomy and a wide selection of endodontic filling materials that, in turn, may not be well tolerated by the periapical tissues and may evoke an immune reaction. This article discusses published reports of various bioactive materials that are used in endodontic therapy, including calcium hydroxide, mineral trioxide aggregate, a bioactive dentin substrate, calcium phosphate ceramics, and calcium phosphate cements.

Albiziahexoside: a potential source of bioactive saponin from the leaves of Albizzia lebbeck.

PubMed

Ueda, Minoru; Tokunaga, Takashi; Okazaki, Masayuki; Sata, Noriko U; Ueda, Katsuhiro; Yamamura, Shosuke

2003-10-01

Albiziahexoside (1), a new hexaglycosylated saponin, was isolated from leaves of Albizzia lebbeck. Saponin 1, which is an analog of cytotoxic albiziatrioside A (2), did not show cytotoxicity. However, 1 is a potential source of 2 and related bioactive saponins for medicinal use because leaves, which can be regenerated after collection, contain 1 in substantial quantity.

Coating of VEGF-releasing scaffolds with bioactive glass for angiogenesis and bone regeneration.

PubMed

Leach, J Kent; Kaigler, Darnell; Wang, Zhuo; Krebsbach, Paul H; Mooney, David J

2006-06-01

Bioactive glasses are potentially useful as bone defect fillers, and vascular endothelial growth factor (VEGF) has demonstrated benefit in bone regeneration as well. We hypothesized that the specific combination of prolonged localized VEGF presentation from a matrix coated with a bioactive glass may enhance bone regeneration. To test this hypothesis, the capacity of VEGF-releasing polymeric scaffolds with a bioactive glass coating was examined in vitro and in vivo using a rat critical-sized defect model. In the presence of a bioactive glass coating, we did not detect pronounced differences in the differentiation of human mesenchymal stem cells in vitro. However, we observed significantly enhanced mitogenic stimulation of endothelial cells in the presence of the bioactive glass coating, with an additive effect with VEGF release. This trend was maintained in vivo, where coated VEGF-releasing scaffolds demonstrated significant improvements in blood vessel density at 2 weeks versus coated control scaffolds. At 12 weeks, bone mineral density was significantly increased in coated VEGF-releasing scaffolds versus coated controls, while only a slight increase in bone volume fraction was observed. The results of this study suggest that a bioactive glass coating on a polymeric substrate participates in bone healing through indirect processes which enhance angiogenesis and bone maturation and not directly on osteoprogenitor differentiation and bone formation. The mass of bioactive glass used in this study provides a comparable and potentially additive, response to localized VEGF delivery over early time points. These studies demonstrate a materials approach to achieve an angiogenic response formerly limited to the delivery of inductive growth factors.

Structure, bioactivity, and synthesis of methylated flavonoids.

PubMed

Wen, Lingrong; Jiang, Yueming; Yang, Jiali; Zhao, Yupeng; Tian, Miaomiao; Yang, Bao

2017-06-01

Methylated flavonoids are an important type of natural flavonoid derivative with potentially multiple health benefits; among other things, they have improved bioavailability compared with flavonoid precursors. Flavonoids have been documented to have broad bioactivities, such as anticancer, immunomodulation, and antioxidant activities, that can be elevated, to a certain extent, by methylation. Understanding the structure, bioactivity, and bioavailability of methylated flavonoids, therefore, is an interesting topic with broad potential applications. Though methylated flavonoids are widely present in plants, their levels are usually low. Because developing efficient techniques to produce these chemicals would likely be beneficial, we provide an overview of their chemical and biological synthesis. © 2017 New York Academy of Sciences.

The agar diffusion scratch assay - A novel method to assess the bioactive and cytotoxic potential of new materials and compounds

PubMed Central

Pusnik, Mascha; Imeri, Minire; Deppierraz, Grégoire; Bruinink, Arie; Zinn, Manfred

2016-01-01

A profound in vitro evaluation not only of the cytotoxic but also of bioactive potential of a given compound or material is crucial for predicting potential effects in the in vivo situation. However, most of the current methods have weaknesses in either the quantitative or qualitative assessment of cytotoxicity and/or bioactivity of the test compound. Here we describe a novel assay combining the ISO 10993-5 agar diffusion test and the scratch also termed wound healing assay. In contrast to these original tests this assay is able to detect and distinguish between cytotoxic, cell migration modifying and cytotoxic plus cell migration modifying compounds, and this at higher sensitivity and in a quantitative way. PMID:26861591

Phenotypic Screening Identifies Synergistically Acting Natural Product Enhancing the Performance of Biomaterial Based Wound Healing.

PubMed

Sivasubramanian, Srinivasan; Chandrasekar, Gayathri; Svensson Akusjärvi, Sara; Thangam, Ramar; Sathuvan, Malairaj; Kumar, R B S; Hussein, Hawraa; Vincent, Savariar; Madhan, Balaraman; Gunasekaran, Palani; Kitambi, Satish S

2017-01-01

The potential of multifunctional wound heal biomaterial relies on the optimal content of therapeutic constituents as well as the desirable physical, chemical, and biological properties to accelerate the healing process. Formulating biomaterials such as amnion or collagen based scaffolds with natural products offer an affordable strategy to develop dressing material with high efficiency in healing wounds. Using image based phenotyping and quantification, we screened natural product derived bioactive compounds for modulators of types I and III collagen production from human foreskin derived fibroblast cells. The identified hit was then formulated with amnion to develop a biomaterial, and its biophysical properties, in vitro and in vivo effects were characterized. In addition, we performed functional profiling analyses by PCR array to understand the effect of individual components of these materials on various genes such as inflammatory mediators including chemokines and cytokines, growth factors, fibroblast stimulating markers for collagen secretion, matrix metalloproteinases, etc., associated with wound healing. FACS based cell cycle analyses were carried out to evaluate the potential of biomaterials for induction of proliferation of fibroblasts. Western blot analyses was done to examine the effect of biomaterial on collagen synthesis by cells and compared to cells grown in the presence of growth factors. This work demonstrated an uncomplicated way of identifying components that synergistically promote healing. Besides, we demonstrated that modulating local wound environment using biomaterials with bioactive compounds could enhance healing. This study finds that the developed biomaterials offer immense scope for healing wounds by means of their skin regenerative features such as anti-inflammatory, fibroblast stimulation for collagen secretion as well as inhibition of enzymes and markers impeding the healing, hydrodynamic properties complemented with other features including non-toxicity, biocompatibility, and safety.

An integrated approach to uncover quality marker underlying the effects of Alisma orientale on lipid metabolism, using chemical analysis and network pharmacology.

PubMed

Liao, Maoliang; Shang, Haihua; Li, Yazhuo; Li, Tian; Wang, Miao; Zheng, Yanan; Hou, Wenbin; Liu, Changxiao

2018-06-01

Quality control of traditional Chinese medicines is currently a great concern, due to the correlation between the quality control indicators and clinic effect is often questionable. According to the "multi-components and multi-targets" property of TCMs, a new special quality and bioactivity evaluation system is urgently needed. Present study adopted an integrated approach to provide new insights relating to uncover quality marker underlying the effects of Alisma orientale (AO) on lipid metabolism. In this paper, guided by the concept of the quality marker (Q-marker), an integrated strategies "effect-compound-target-fingerprint" was established to discovery and screen the potential quality marker of AO based on network pharmacology and chemical analysis. Firstly, a bioactivity evaluation was performed to screen the main active fractions. Then the chemical compositions were rapidly identified by chemical analysis. Next, networks were constructed to illuminate the interactions between these component and their targets for lipid metabolism, and the potential Q-marker of AO was initially screened. Finally, the activity of the Q-markers was validated in vitro. 50% ethanol extract fraction was found to have the strongest lipid-lowering activity. Then, the network pharmacology was used to clarify the unique relationship between the Q-markers and their integral pharmacological action. Combined with the results obtained, five active ingredients in the 50% ethanol extract fraction were given special considerations to be representative Q-markers: Alisol A, Alisol B, Alisol A 23-acetate, Alisol B 23-acetate and Alisol A 24-acetate, respectively. The chromatographic fingerprints based Q-marker was establishment. The integrated Q-marker screen may offer an alternative quality assessment of herbal medicines. Copyright © 2018. Published by Elsevier GmbH.

Phenotypic Screening Identifies Synergistically Acting Natural Product Enhancing the Performance of Biomaterial Based Wound Healing

PubMed Central

Sivasubramanian, Srinivasan; Chandrasekar, Gayathri; Svensson Akusjärvi, Sara; Thangam, Ramar; Sathuvan, Malairaj; Kumar, R. B. S.; Hussein, Hawraa; Vincent, Savariar; Madhan, Balaraman; Gunasekaran, Palani; Kitambi, Satish S.

2017-01-01

The potential of multifunctional wound heal biomaterial relies on the optimal content of therapeutic constituents as well as the desirable physical, chemical, and biological properties to accelerate the healing process. Formulating biomaterials such as amnion or collagen based scaffolds with natural products offer an affordable strategy to develop dressing material with high efficiency in healing wounds. Using image based phenotyping and quantification, we screened natural product derived bioactive compounds for modulators of types I and III collagen production from human foreskin derived fibroblast cells. The identified hit was then formulated with amnion to develop a biomaterial, and its biophysical properties, in vitro and in vivo effects were characterized. In addition, we performed functional profiling analyses by PCR array to understand the effect of individual components of these materials on various genes such as inflammatory mediators including chemokines and cytokines, growth factors, fibroblast stimulating markers for collagen secretion, matrix metalloproteinases, etc., associated with wound healing. FACS based cell cycle analyses were carried out to evaluate the potential of biomaterials for induction of proliferation of fibroblasts. Western blot analyses was done to examine the effect of biomaterial on collagen synthesis by cells and compared to cells grown in the presence of growth factors. This work demonstrated an uncomplicated way of identifying components that synergistically promote healing. Besides, we demonstrated that modulating local wound environment using biomaterials with bioactive compounds could enhance healing. This study finds that the developed biomaterials offer immense scope for healing wounds by means of their skin regenerative features such as anti-inflammatory, fibroblast stimulation for collagen secretion as well as inhibition of enzymes and markers impeding the healing, hydrodynamic properties complemented with other features including non-toxicity, biocompatibility, and safety. PMID:28769790

Targeted profiling of hydrophilic constituents of royal jelly by hydrophilic interaction liquid chromatography-tandem mass spectrometry.

PubMed

Pina, Athanasia; Begou, Olga; Kanelis, Dimitris; Gika, Helen; Kalogiannis, Stavros; Tananaki, Chrysoula; Theodoridis, Georgios; Zotou, Anastasia

2018-01-05

In the present work a Hydrophilic Interaction Liquid Chromatography-tandem Mass Spectrometry (HILIC-MS/MS) method was developed for the efficient separation and quantification of a large number of small polar bioactive molecules in Royal Jelly. The method was validated and provided satisfactory detection sensitivity for 88 components. Quantification was proven to be precise for 64 components exhibiting good linearity, recoveries R% >90% for the majority of analytes and intra- and inter-day precision from 0.14 to 20% RSD. Analysis of 125 fresh royal jelly samples of Greek origin provided useful information on royal jelly's hydrophilic bioactive components revealing lysine, ribose, proline, melezitose and glutamic acid to be in high abundance. In addition the occurrence of 18 hydrophilic nutrients which have not been reported previously as royal jelly constituents is shown. Copyright © 2017 Elsevier B.V. All rights reserved.

Marine Peptides as Potential Agents for the Management of Type 2 Diabetes Mellitus-A Prospect.

PubMed

Xia, En-Qin; Zhu, Shan-Shan; He, Min-Jing; Luo, Fei; Fu, Cheng-Zhan; Zou, Tang-Bin

2017-03-23

An increasing prevalence of diabetes is known as a main risk for human health in the last future worldwide. There is limited evidence on the potential management of type 2 diabetes mellitus using bioactive peptides from marine organisms, besides from milk and beans. We summarized here recent advances in our understanding of the regulation of glucose metabolism using bioactive peptides from natural proteins, including regulation of insulin-regulated glucose metabolism, such as protection and reparation of pancreatic β-cells, enhancing glucose-stimulated insulin secretion and influencing the sensitivity of insulin and the signaling pathways, and inhibition of bioactive peptides to dipeptidyl peptidase IV, α-amylase and α-glucosidase activities. The present paper tried to understand the underlying mechanism involved and the structure characteristics of bioactive peptides responsible for its antidiabetic activities to prospect the utilization of rich marine organism proteins.

Bioactive Proteins and Peptides from Soybeans.

PubMed

Agyei, Dominic

2015-01-01

Dietary proteins from soybeans have been shown to offer health benefits in vivo and/or in vitro either as intact proteins or in partially digested forms also called bioactive peptides. Upon oral administration and absorption, soy-derived bioactive peptides may induce several physiological responses such as antioxidative, antimicrobial, antihypertensive, anticancer and immunomodulatory effects. There has therefore been a mounting research interest in the therapeutic potential of soy protein hydrolysates and their subsequent incorporation in functional foods and 'Food for Specified Health Uses' (FOSHU) related products where their biological activities may assist in the promotion of good health or in the control and prevention of diseases. This mini review discusses relevant patents and gives an overview on bioactive proteins and peptides obtainable from soybeans. Processes for the production and formulation of these peptides are given, together with specific examples of their therapeutic potential and possible areas of application.

Anti-angiogenic activity and phytochemical screening of fruit fractions from Vitex agnus castus.

PubMed

Certo, Giovanna; Costa, Rosaria; D'Angelo, Valeria; Russo, Marina; Albergamo, Ambrogina; Dugo, Giacomo; Germanò, Maria Paola

2017-12-01

Although the antitumour activity of Vitex agnus castus fruits has been already addressed, no work has yet assessed their anti-angiogenic potential. To this purpose, several extractive fractions of such fruits were tested on zebrafish embrios by EAP assay, so that only the bioactive fractions could be subsequently tested on the chick chorioallantoic membrane by CAM assay. Bioactive fractions were also phytochemically screened to identify those bioactive compounds responsible for anti-angiogenic activity. A marked inhibition of vessel formation was detected only in zebrafish embryos treated with chloroform or ethyl acetate fractions. Considering CAM assay, chloroform fraction induced a strong reduction of microvasculature and haemoglobin content; while lower anti-angiogenic effects of the ethyl acetate fraction were determined. Phytochemical analyses confirmed the presence of several bioactive anti-angiogenic compounds. Overall, obtained preliminary results highlighted a potential anti-angiogenic activity of V. agnus castus fruits.

Bioactive secondary metabolites from marine microbes for drug discovery.

PubMed

Nikapitiya, Chamilani

2012-01-01

The isolation and extraction of novel bioactive secondary metabolites from marine microorganisms have a biomedical potential for future drug discovery as the oceans cover 70% of the planet's surface and life on earth originates from sea. Wide range of novel bioactive secondary metabolites exhibiting pharmacodynamic properties has been isolated from marine microorganisms and many to be discovered. The compounds isolated from marine organisms (macro and micro) are important in their natural form and also as templates for synthetic modifications for the treatments for variety of deadly to minor diseases. Many technical issues are yet to overcome before wide-scale bioprospecting of marine microorganisms becomes a reality. This chapter focuses on some novel secondary metabolites having antitumor, antivirus, enzyme inhibitor, and other bioactive properties identified and isolated from marine microorganisms including bacteria, actinomycetes, fungi, and cyanobacteria, which could serve as potentials for drug discovery after their clinical trials. Copyright © 2012 Elsevier Inc. All rights reserved.

Marine Peptides as Potential Agents for the Management of Type 2 Diabetes Mellitus—A Prospect

PubMed Central

Xia, En-Qin; Zhu, Shan-Shan; He, Min-Jing; Luo, Fei; Fu, Cheng-Zhan; Zou, Tang-Bin

2017-01-01

An increasing prevalence of diabetes is known as a main risk for human health in the last future worldwide. There is limited evidence on the potential management of type 2 diabetes mellitus using bioactive peptides from marine organisms, besides from milk and beans. We summarized here recent advances in our understanding of the regulation of glucose metabolism using bioactive peptides from natural proteins, including regulation of insulin-regulated glucose metabolism, such as protection and reparation of pancreatic β-cells, enhancing glucose-stimulated insulin secretion and influencing the sensitivity of insulin and the signaling pathways, and inhibition of bioactive peptides to dipeptidyl peptidase IV, α-amylase and α-glucosidase activities. The present paper tried to understand the underlying mechanism involved and the structure characteristics of bioactive peptides responsible for its antidiabetic activities to prospect the utilization of rich marine organism proteins. PMID:28333091

Electrospun F18 Bioactive Glass/PCL—Poly (ε-caprolactone)—Membrane for Guided Tissue Regeneration

PubMed Central

Hidalgo Pitaluga, Lucas; Trevelin Souza, Marina; Santocildes Romero, Martin Eduardo; Hatton, Paul V.

2018-01-01

Barrier membranes that are used for guided tissue regeneration (GTR) therapy usually lack bioactivity and the capability to promote new bone tissue formation. However, the incorporation of an osteogenic agent into polymeric membranes seems to be the most assertive strategy to enhance their regenerative potential. Here, the manufacturing of composite electrospun membranes made of poly (ε-caprolactone) (PCL) and particles of a novel bioactive glass composition (F18) is described. The membranes were mechanically and biologically tested with tensile strength tests and tissue culture with MG-63 osteoblast-like cell line, respectively. The PCL-F18 composite membranes demonstrated no increased cytotoxicity and an enhanced osteogenic potential when compared to pure PCL membranes. Moreover, the addition of the bioactive phase increased the membrane tensile strength. These preliminary results suggested that these new membranes can be a strong candidate for small bone injuries treatment by GTR technique. PMID:29517988

Chemical, Bioactive, and Antioxidant Potential of Twenty Wild Culinary Mushroom Species.

PubMed

Sharma, S K; Gautam, N

2015-01-01

The chemical, bioactive, and antioxidant potential of twenty wild culinary mushroom species being consumed by the people of northern Himalayan regions has been evaluated for the first time in the present study. Nutrients analyzed include protein, crude fat, fibres, carbohydrates, and monosaccharides. Besides, preliminary study on the detection of toxic compounds was done on these species. Bioactive compounds evaluated are fatty acids, amino acids, tocopherol content, carotenoids (β-carotene, lycopene), flavonoids, ascorbic acid, and anthocyanidins. Fruitbodies extract of all the species was tested for different types of antioxidant assays. Although differences were observed in the net values of individual species all the species were found to be rich in protein, and carbohydrates and low in fat. Glucose was found to be the major monosaccharide. Predominance of UFA (65-70%) over SFA (30-35%) was observed in all the species with considerable amounts of other bioactive compounds. All the species showed higher effectiveness for antioxidant capacities.

Bioactive glass coupling with natural polyphenols: Surface modification, bioactivity and anti-oxidant ability

NASA Astrophysics Data System (ADS)

Cazzola, Martina; Corazzari, Ingrid; Prenesti, Enrico; Bertone, Elisa; Vernè, Enrica; Ferraris, Sara

2016-03-01

Polyphenols are actually achieving an increasing interest due to their potential health benefits, such as antioxidant, anticancer, antibacterial and bone stimulation abilities. However their poor bioavailability and stability hamper an effective clinical application as therapeutic principles. The opportunity to couple these biomolecules with synthetic biomaterials, in order to obtain local delivery at the site of interest, improve their bioavailability and stability and combine their properties with the ones of the substrate, is a challenging opportunity for the biomedical research. A silica based bioactive glass, CEL2, has been successfully coupled with gallic acid and natural polyphenols extracted from red grape skins and green tea leaves. The effectiveness of grafting has been verified by means of XPS analyses and the Folin&Ciocalteu tests. In vitro bioactivity has been investigated by soaking in simulated body fluid (SBF). Surface modification after functionalization and early stage reactivity in SBF have been studied by means of zeta potential electrokinetic measurements in KCl and SBF. Finally the antioxidant properties of bare and modified bioactive glasses has been investigated by means of the evaluation of free radical scavenging activity by Electron Paramagnetic Resonance (EPR)/spin trapping technique after UV photolysis of H2O2 highlighting scavenging activity of the bioactive glass.

Current and potential uses of bioactive molecules from marine processing waste.

PubMed

Suleria, Hafiz Ansar Rasul; Masci, Paul; Gobe, Glenda; Osborne, Simone

2016-03-15

Food industries produce huge amounts of processing waste that are often disposed of incurring expenses and impacting upon the environment. For these and other reasons, food processing waste streams, in particular marine processing waste streams, are gaining popularity amongst pharmaceutical, cosmetic and nutraceutical industries as sources of bioactive molecules. In the last 30 years, there has been a gradual increase in processed marine products with a concomitant increase in waste streams that include viscera, heads, skins, fins, bones, trimmings and shellfish waste. In 2010, these waste streams equated to approximately 24 million tonnes of mostly unused resources. Marine processing waste streams not only represent an abundant resource, they are also enriched with structurally diverse molecules that possess a broad panel of bioactivities including anti-oxidant, anti-coagulant, anti-thrombotic, anti-cancer and immune-stimulatory activities. Retrieval and characterisation of bioactive molecules from marine processing waste also contributes valuable information to the vast field of marine natural product discovery. This review summarises the current use of bioactive molecules from marine processing waste in different products and industries. Moreover, this review summarises new research into processing waste streams and the potential for adoption by industries in the creation of new products containing marine processing waste bioactives. © 2015 Society of Chemical Industry.

Antimicrobial properties, antioxidant activity and bioactive compounds from six wild edible mushrooms of western ghats of Karnataka, India

PubMed Central

Ramesh, Ch.; Pattar, Manohar G.

2010-01-01

Methanolic extracts of 6 wild edible mushrooms isolated from the Western Ghats of Karnataka were used in this study. Among the isolates (Lycoperdon perlatum, Cantharellus cibarius, Clavaria vermiculris, Ramaria formosa, Marasmius oreades, Pleurotus pulmonarius), only 4 showed satisfactory results. Quantitative analysis of bioactive components revealed that total phenols are the major bioactive component found in extracts of isolates expressed as mg of GAE per gram of fruit body, which ranged from 3.20 ± 0.05 mg/mL to 6.25 ± 0.08 mg/mL. Average concentration of flavonoid ranged from 0.40 ± 0.052 mg/mL to 2.54 ± 0.08 mg/mL; followed by very small concentration of ascorbic acid (range, 0.06 ± 0.01 mg/mL to 0.16 ± 0.01 mg/mL) in all the isolates. All the isolates showed high phenol and flavonoid content, but ascorbic acid content was found in traces. Antioxidant efficiency by inhibitory concentration on 1,1-Diphenly-2-picrylhydrazyl (DPPH) was found significant when compared to standard antioxidant like Buthylated hydroxyanisol (BHA). The concentration (IC50) ranged from 0.94 ± 0.27 mg/mL to 7.57 ± 0.21 mg/mL. Determination of antimicrobial activity profile of all the isolates tested against a panel of standard pathogenic bacteria and fungi indicated that the concentrations of bioactive components directly influence the antimicrobial capability of the isolates. Agar diffusion assay showed considerable activity against all bacteria. Minimum inhibitory concentration values of the extracts of 4 isolates showed that they are also active even in least concentrations. These results are discussed in relation to therapeutic value of the studied mushrooms. PMID:21808550

Bioactivity characterization of 45S5 bioglass using TL, OSL and EPR: Comparison with the case of 58S sol-gel bioactive glass.

PubMed

Polymeris, G S; Giannoulatou, V; Kyriakidou, A; Sfampa, I K; Theodorou, G S; Şahiner, E; Meriç, N; Kitis, G; Paraskevopoulos, K M

2017-01-01

The current work exploits the effective application of thermoluminescence (TL), optically stimulated luminescence (OSL) and the possibility of applying Electron Paramagnetic Resonance (EPR) for the discrimination between different bioactive responses in the case of the 45S5 bioactive glass (SiO 2 45, Na 2 O 24.5, CaO 24.5, P 2 O 5 6 in wt%), which was synthesized through melting process. These techniques are suggested mainly due to their low spectroscopic detection thresholds. The original 45S5 in grain size range of 20-40μm was immersed in the Simulated Body Fluid (SBF) for various different immersion times ranging over one week. In this work the 110°C TL peak, a specific OSL component and the EPR signal at g=2.013 ascribed to oxygen hole center (OHC) are used due to their sensitivity to the different bioactive responses. For all luminescence and EPR components, the intensity plot versus immersion time yields sharp discontinuities, resulting in effective probes regarding the timescale for both the beginning as well as the end of the procedure of the crystalline HCAp formation respectively. On the contrary to the smooth decreasing pattern of both luminescence entities, the peak to peak amplitude of the EPR signal indicates an initial increase for the initial 16min of immersion, followed by a further decrease throughout the immersion time duration. The discontinuities monitored for both sensitivity of TL, OSL and EPR, in conjunction with the discontinuities monitored for the sensitization of TL and OSL, when plotted versus immersion time, provide an individual time scale for each one of the chemical reactions involved in the five steps of the aforementioned procedure. According to the authors' best knowledge, scarce characterization techniques could provide this time scale frame, while it is the first time that such an application of OSL and EPR is attempted. Finally, the bioactive response of the 45S5 bioglass was compared with that of the 58S sol-gel bioactive glass, in terms of the timescale of these five stages required for the final formation of the HCAp. The techniques of luminescence and EPR which take advantage of trapped charges are proposed as alternative cheap and prompt effective techniques towards discrimination between different bioactive responses in bioactive glasses. Copyright © 2016. Published by Elsevier B.V.

Dietary bioactives: establishing a scientific framework for recommended intakes.

PubMed

Wallace, Taylor C; Blumberg, Jeffrey B; Johnson, Elizabeth J; Shao, Andrew

2015-01-01

In the United States, dietary reference intakes describe the relations between nutrient intakes and indicators of adequacy, prevention of disease, and avoidance of excessive intakes among healthy populations for essential nutrients but not dietary bioactive components (DBCs), whose absence from the diet is presumably not deleterious to health (i.e., does not cause a deficiency syndrome). An appropriate framework is needed for establishing recommended intakes for which public health messages and food labeling for DBCs can be derived, because their putative health benefits may not be readily defined in the context of nutritional essentiality. In addition, a myriad of factors make determining their intake and status and investigating their discrete contributions to health particularly challenging. Therefore, the ASN Dietary Bioactive Components Research Interest Section felt it worthwhile to convene a special "hot topic" session at the 2014 Experimental Biology meeting to discuss this issue and serve as a call for future scientific dialogue on establishing a framework for recommended intakes of DBCs. This session summary captures the discussions and presentations that transpired during this session. © 2015 American Society for Nutrition.

Dietary Bioactives: Establishing a Scientific Framework for Recommended Intakes12

PubMed Central

Wallace, Taylor C; Blumberg, Jeffrey B; Johnson, Elizabeth J; Shao, Andrew

2015-01-01

In the United States, dietary reference intakes describe the relations between nutrient intakes and indicators of adequacy, prevention of disease, and avoidance of excessive intakes among healthy populations for essential nutrients but not dietary bioactive components (DBCs), whose absence from the diet is presumably not deleterious to health (i.e., does not cause a deficiency syndrome). An appropriate framework is needed for establishing recommended intakes for which public health messages and food labeling for DBCs can be derived, because their putative health benefits may not be readily defined in the context of nutritional essentiality. In addition, a myriad of factors make determining their intake and status and investigating their discrete contributions to health particularly challenging. Therefore, the ASN Dietary Bioactive Components Research Interest Section felt it worthwhile to convene a special “hot topic” session at the 2014 Experimental Biology meeting to discuss this issue and serve as a call for future scientific dialogue on establishing a framework for recommended intakes of DBCs. This session summary captures the discussions and presentations that transpired during this session. PMID:25593139

Simultaneous quantification of eight bioactive components of Houttuynia cordata and related Saururaceae medicinal plants by on-line high performance liquid chromatography-diode array detector-electrospray mass spectrometry.

PubMed

Meng, Jiang; Leung, Kelvin Sze-Yin; Dong, Xiao-Ping; Zhou, Yi-Sheng; Jiang, Zhi-Hong; Zhao, Zhong-Zhen

2009-12-01

An on-line high performance liquid chromatography (HPLC)-diode array detector (DAD)-electrospray ionization mass spectrometry (ESI-MS) method has been developed to quantify simultaneously eight bioactive chemical components in Houttuynia cordata Thunb and related Saururaceae medicinal plants. Simultaneous separation of these eight compounds was achieved on a C(18) analytical column with gradient elution of acetonitrile and 0.2% acetic acid (v/v) at a flow rate of 0.6 mL/min and being detected at 280 nm. These eight compounds were completely separated within 90 min. Good linear regression relationship (r(2)>0.9978) within test ranges was shown in all calibration curves. Good repeatabilty for the quantification of these eight compounds in H.cordata was also demonstrated in this method, with intra- and inter-day variations less than 3.0%. The method established was successfully applied to quantify eight bioactive compounds in closely related species of H.cordata, which provides a new basis for quality assessment of H.cordata.

Reciprocal regulation of adipocyte and osteoblast differentiation of mesenchymal stem cells by Eupatorium japonicum prevents bone loss and adiposity increase in osteoporotic rats.

PubMed

Kim, Min-Ji; Jang, Woo-Seok; Lee, In-Kyoung; Kim, Jong-Keun; Seong, Ki-Seung; Seo, Cho-Rong; Song, No-Joon; Bang, Min-Hyuk; Lee, Young Min; Kim, Haeng Ran; Park, Ki-Moon; Park, Kye Won

2014-07-01

Pathological increases in adipogenic potential with decreases in osteogenic differentiation occur in osteoporotic bone marrow cells. Previous studies have shown that bioactive materials isolated from natural products can reciprocally regulate adipogenic and osteogenic fates of bone marrow cells. In this study, we showed that Eupatorium japonicum stem extracts (EJE) suppressed lipid accumulation and inhibited the expression of adipocyte markers in multipotent C3H10T1/2 and primary bone marrow cells. Conversely, EJE stimulated alkaline phosphatase activity and induced the expression of osteoblast markers in C3H10T1/2 and primary bone marrow cells. Daily oral administration of 50 mg/kg of EJE for 6 weeks to ovariectomized rats prevented body weight increase and bone mineral density decrease. Finally, activity-guided fractionation led to the identification of coumaric acid and coumaric acid methyl ester as bioactive anti-adipogenic and pro-osteogenic components in EJE. Taken together, our data indicate a promising possibility of E. japonicum as a functional food and as a therapeutic intervention for preventing osteoporosis and bone fractures.

Tracking flow of leukocytes in blood for drug analysis

NASA Astrophysics Data System (ADS)

Basharat, Arslan; Turner, Wesley; Stephens, Gillian; Badillo, Benjamin; Lumpkin, Rick; Andre, Patrick; Perera, Amitha

2011-03-01

Modern microscopy techniques allow imaging of circulating blood components under vascular flow conditions. The resulting video sequences provide unique insights into the behavior of blood cells within the vasculature and can be used as a method to monitor and quantitate the recruitment of inflammatory cells at sites of vascular injury/ inflammation and potentially serve as a pharmacodynamic biomarker, helping screen new therapies and individualize dose and combinations of drugs. However, manual analysis of these video sequences is intractable, requiring hours per 400 second video clip. In this paper, we present an automated technique to analyze the behavior and recruitment of human leukocytes in whole blood under physiological conditions of shear through a simple multi-channel fluorescence microscope in real-time. This technique detects and tracks the recruitment of leukocytes to a bioactive surface coated on a flow chamber. Rolling cells (cells which partially bind to the bioactive matrix) are detected counted, and have their velocity measured and graphed. The challenges here include: high cell density, appearance similarity, and low (1Hz) frame rate. Our approach performs frame differencing based motion segmentation, track initialization and online tracking of individual leukocytes.

Bioactive components from flowers of Sambucus nigra L. increase glucose uptake in primary porcine myotube cultures and reduce fat accumulation in Caenorhabditis elegans.

PubMed

Bhattacharya, Sumangala; Christensen, Kathrine B; Olsen, Louise C B; Christensen, Lars P; Grevsen, Kai; Færgeman, Nils J; Kristiansen, Karsten; Young, Jette F; Oksbjerg, Niels

2013-11-20

Obesity and insulin resistance in skeletal muscles are major features of type 2 diabetes. In the present study, we examined the potential of Sambucus nigra flower (elderflowers) extracts to stimulate glucose uptake (GU) in primary porcine myotubes and reduce fat accumulation (FAc) in Caenorhabditis elegans. Bioassay guided chromatographic fractionations of extracts and fractions resulted in the identification of naringenin and 5-O- caffeoylquinic acid exhibiting a significant increase in GU. In addition, phenolic compounds related to those found in elderflowers were also tested, and among these, kaempferol, ferulic acid, p-coumaric acid, and caffeic acid increased GU significantly. FAc was significantly reduced in C. elegans, when treated with elderflower extracts, their fractions and the metabolites naringenin, quercetin-3-O-rutinoside, quercetin-3-O-glucoside, quercetin-3-O-5″-acetylglycoside, kaempferol-3-O-rutinoside, isorhamnetin-3-O-rutinoside, and isorhamnetin-3-O-glucoside and the related phenolic compounds kaempferol and ferulic acid. The study indicates that elderflower extracts contain bioactive compounds capable of modulating glucose and lipid metabolism, suitable for nutraceutical and pharmaceutical applications.

Endophytic Streptomyces sp. AC35, a producer of bioactive isoflavone aglycones and antimycins.

PubMed

Ondrejíčková, P; Šturdíková, M; Hushegyi, A; Švajdlenka, E; Markošová, K; Čertík, M

2016-09-01

In this research, a microbial endophytic strain obtained from the rhizosphere of the conifer Taxus baccata and designated as Streptomyces sp. AC35 (FJ001754.1 Streptomyces, GenBank) was investigated. High 16S rDNA gene sequence similarity suggests that this strain is closely related to S. odorifer. The major fatty acid profile of intracellular lipids was also carried out to further identify this strain. Atomic force microscopy and scanning acoustic microscopy were used to image our strain. Its major excreted substances were extracted, evaluated for antimicrobial activity, purified, and identified by ultraviolet-visible spectroscopy (UV-vis), liquid chromatography-mass spectrometry (LC-MS/MS) and nuclear magnetic resonance as the bioactive isoflavone aglycones-daidzein, glycitein and genistein. Batch cultivation, performed under different pH conditions, revealed enhanced production of antimycin components when the pH was stable at 7.0. Antimycins were detected by HPLC and identified by UV-vis and LC-MS/MS combined with the multiple reaction monitoring. Our results demonstrate that Streptomyces sp. AC35 might be used as a potential source of effective, pharmaceutically active compounds.

Nutrigenomics of essential oils and their potential domestic use for improving health.

PubMed

Cayuela Sánchez, José Antonio; Elamrani, Abdelaziz

2014-11-01

The use of essential oils as industrial food additives is notorious, like their medicinal properties. However, their use in household food spicing is for now limited. In this work, we have made a review to reveal the nutrigenomic actions exerted by their bioactive components, to promote awareness of their modulating gene expression ability and the potential that this implies. Also considered is how essential oils can be used as flavoring and seasoning after cooking and before consumption, such as diet components which can improve human health. Genetic mechanisms involved in the medicinal properties of essential oils for food use are identified from literature. These genetic mechanisms reveal nutrigenomic actions. Reviews on the medicinal properties of essential oils have been particularly considered. A wide diversity of nutrigenomic effects from essential oils useful potentially for food spicing is reviewed. General ideas are discussed about essential oils and their properties, such as anti-inflammatory, analgesic, immunomodulatory, anticancer, hepatoprotective, hypolipidemic, anti-diabetic, antioxidant, bone-reparation, anti-depressant and mitigatory for Alzheimer's disease. The essential oils for food use are potentially promoting health agents, and, therefore, worth using as flavoring and condiments. Becoming aware of the modulating gene expression actions from essential oils is important for understanding their potential for use in household dishes as spices to improve health.

Patents on Therapeutic and Cosmetic Applications of Bioactives of Crocus Sativus L. and their Production through Synthetic Biology Methods: A Review.

PubMed

Dawalbhakta, Mitali; Telang, Manasi

2017-01-01

Saffron (Crocus sativus L.) has a long history of use as a food additive and a traditional medicine for treating a number of disorders. Prominent bioactives of saffron are crocin, crocetin and safranal. The aim of this study was to carry out an extensive patent search to collect information on saffron bioactives and their derivatives as therapeutic and cosmeceutical agents. All patents related to the area of interest published globally till date have been reviewed. Moreover, a recent synthetic biology approach to cost effective and consistent production of saffron bioactives has been highlighted. A patent search strategy was designed based on keywords and concepts related to Crocus sativus L. and its bioactives- safranal, crocin and crocetin in combination with different patent classification codes relevant to the technology areas. This search strategy was employed to retrieve patents from various patent databases. The patents which focused on therapeutic or cosmetic applications and claimed compositions comprising crocin, crocetin or safranal as the main active component were selected and analysed. Maximum patenting activity was noticed towards the use of these bioactives in the treatment of neurological disorders followed by multiple uses of the same compound, use in treatment of metabolic disorders and use as cosmeceuticals. Interestingly, there were no patent records related to use of these bioactives in treating infectious disorders. Our patent analysis points out the populous and less explored uses of saffron bioactives and areas where there is further scope for research and growth. Recently developed synthetic biology approach is contributory in improving availability, consistency and cost effectiveness of saffron bioactives. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Bioinformatics and peptidomics approaches to the discovery and analysis of food-derived bioactive peptides.

PubMed

Agyei, Dominic; Tsopmo, Apollinaire; Udenigwe, Chibuike C

2018-06-01

There are emerging advancements in the strategies used for the discovery and development of food-derived bioactive peptides because of their multiple food and health applications. Bioinformatics and peptidomics are two computational and analytical techniques that have the potential to speed up the development of bioactive peptides from bench to market. Structure-activity relationships observed in peptides form the basis for bioinformatics and in silico prediction of bioactive sequences encrypted in food proteins. Peptidomics, on the other hand, relies on "hyphenated" (liquid chromatography-mass spectrometry-based) techniques for the detection, profiling, and quantitation of peptides. Together, bioinformatics and peptidomics approaches provide a low-cost and effective means of predicting, profiling, and screening bioactive protein hydrolysates and peptides from food. This article discuses the basis, strengths, and limitations of bioinformatics and peptidomics approaches currently used for the discovery and analysis of food-derived bioactive peptides.

Smart Dressings Based on Nanostructured Fibers Containing Natural Origin Antimicrobial, Anti-Inflammatory, and Regenerative Compounds

PubMed Central

Andreu, Vanesa; Mendoza, Gracia; Arruebo, Manuel; Irusta, Silvia

2015-01-01

A fast and effective wound healing process would substantially decrease medical costs, wound care supplies, and hospitalization significantly improving the patients’ quality of life. The search for effective therapeutic approaches seems to be imperative in order to avoid the aggravation of chronic wounds. In spite of all the efforts that have been made during the recent years towards the development of artificial wound dressings, none of the currently available options combine all the requirements necessary for quick and optimal cutaneous regeneration. Therefore, technological advances in the area of temporary and permanent smart dressings for wound care are required. The development of nanoscience and nanotechnology can improve the materials and designs used in topical wound care in order to efficiently release antimicrobial, anti-inflammatory and regenerative compounds speeding up the endogenous healing process. Nanostructured dressings can overcome the limitations of the current coverings and, separately, natural origin components can also overcome the drawbacks of current antibiotics and antiseptics (mainly cytotoxicity, antibiotic resistance, and allergies). The combination of natural origin components with demonstrated antibiotic, regenerative, or anti-inflammatory properties together with nanostructured materials is a promising approach to fulfil all the requirements needed for the next generation of bioactive wound dressings. Microbially compromised wounds have been treated with different essential oils, honey, cationic peptides, aloe vera, plant extracts, and other natural origin occurring antimicrobial, anti-inflammatory, and regenerative components but the available evidence is limited and insufficient to be able to draw reliable conclusions and to extrapolate those findings to the clinical practice. The evidence and some promising preliminary results indicate that future comparative studies are justified but instead of talking about the beneficial or inert effects of those natural origin occurring materials, the scientific community leads towards the identification of the main active components involved and their mechanism of action during the corresponding healing, antimicrobial, or regenerative processes and in carrying out systematic and comparative controlled tests. Once those natural origin components have been identified and their efficacy validated through solid clinical trials, their combination within nanostructured dressings can open up new avenues in the fabrication of bioactive dressings with outstanding characteristics for wound care. The motivation of this work is to analyze the state of the art in the use of different essential oils, honey, cationic peptides, aloe vera, plant extracts, and other natural origin occurring materials as antimicrobial, anti-inflammatory and regenerative components with the aim of clarifying their potential clinical use in bioactive dressings. We conclude that, for those natural occurring materials, more clinical trials are needed to reach a sufficient level of evidence as therapeutic agents for wound healing management. PMID:28793497

Long-term antibiotic delivery by chitosan-based composite coatings with bone regenerative potential

NASA Astrophysics Data System (ADS)

Ordikhani, F.; Simchi, A.

2014-10-01

Composite coatings with bone-bioactivity and drug-eluting capacity are considered as promising materials for titanium bone implants. In this work, drug-eluting chitosan-bioactive glass coatings were fabricated by a single-step electrophoretic deposition technique. Drug-loading and -releasing capacity of the composite coatings were carried out using the vancomycin antibiotic. Uniform coatings with a thickness of ∼55 μm containing 23.7 wt% bioactive glass particles and various amounts of the antibiotic (380-630 μg/cm2) were produced. The coatings were bioactive in terms of apatite-forming ability in simulated body fluid and showed favorable cell adhesion and growth. In vitro biological tests also indicated that the composite coatings had better cellular affinity than pristine chitosan coatings. The in vitro elution kinetics of the composite coating revealed an initial burst release of around 40% of the drug within the first elution step of 1 h and following by a continuous eluting over 4 weeks, revealing long-term drug-delivering potential. Antibacterial tests using survival assay against Gram-positive Staphylococcus aureus bacteria determined the effect of vancomycin release on reduction of infection risk. Almost no bacteria were survived on the coatings prepared from the EPD suspension containing ≥0.5 g/l vancomycin. The developed chitosan-based composite coatings with bone bioactivity and long-term drug-delivery ability may be potentially useful for metallic implants to reduce infection risk.

Improving In Vivo Efficacy of Bioactive Molecules: An Overview of Potentially Antitumor Phytochemicals and Currently Available Lipid-Based Delivery Systems

PubMed Central

Torres, Carlos; Vázquez, Luis; Reglero, Guillermo; Fornari, Tiziana

2017-01-01

Cancer is among the leading causes of morbidity and mortality worldwide. Many of the chemotherapeutic agents used in cancer treatment exhibit cell toxicity and display teratogenic effect on nontumor cells. Therefore, the search for alternative compounds which are effective against tumor cells but reduce toxicity against nontumor ones is of great importance in the progress or development of cancer treatments. In this sense, scientific knowledge about relevant aspects of nutrition intimately involved in the development and progression of cancer progresses rapidly. Phytochemicals, considered as bioactive ingredients present in plant products, have shown promising effects as potential therapeutic/preventive agents on cancer in several in vitro and in vivo assays. However, despite their bioactive properties, phytochemicals are still not commonly used in clinical practice due to several reasons, mainly attributed to their poor bioavailability. In this sense, new formulation strategies are proposed as carriers to improve their bioefficacy, highlighting the use of lipid-based delivery systems. Here, we review the potential antitumoral activity of the bioactive compounds derived from plants and the current studies carried out in animal and human models. Furthermore, their association with lipids as a formulation strategy to enhance their efficacy in vivo is also reported. The development of high effective bioactive supplements for cancer treatment based on the improvement of their bioavailability goes through this association. PMID:28555156

Stereospermum fimbriatum as a Potential Source of Phytochemicals: A Review of Stereospermum Genus.

PubMed

Awang, Anis F I; Ferdosh, Sahena; Sarker, Md Zaidul I; Sheikh, Hassan I; Ghafoor, Kashif; Yunus, Kamaruzzaman

Stereospermum fimbriatum is one of the medicinal plants that has been claimed to be used traditionally to treat several illnesses such as stomachache, earache, skin irritation and postpartum illness. The genus of this plant is known to possess medicinal properties in every part of the plant. Therapeutic potential of S. fimbriatum is anticipated based on numerous previous studies that documented variety of phytochemical contents and bioactivity of the genus. The most reported bioactivities of its genus are antimicrobial, antioxidant, anti-diabetic, anti-inflammatory, anti-diarrheal and analgesic activities. S. fimbriatum is a rare species that has not been discovered yet. Thus, this review aims at highlighting the potentials of S. fimbriatum by collecting available data on the bioactivities of its genus and set the directions for future research on this plant.

Diet versus jaw bones: Lessons from experimental models and potential clinical implications.

PubMed

Montalvany-Antonucci, Carina Cristina; Zicker, Marina C; Oliveira, Marina C; Macari, Soraia; Madeira, Mila Fernandes M; Andrade, Ildeu; Ferreira, Adaliene Versiani M; Silva, Tarcilia A

2018-01-01

The consumption of different types of diets influences not only body health but the bone remodeling process as well. Nutritional components can directly affect maxillary and mandibular alveolar bone microarchitecture. In this review, we focus on the current knowledge regarding the influence of diets and dietary supplementation on alveolar bone. Accumulating evidence from experimental models suggests that carbohydrate- and fat-rich diets are detrimental for alveolar bone, whereas protective effects are associated with consumption of calcium, ω-3, and bioactive compounds. Little is known about the effects of protein-free and protein-rich diets, boron, vitamin C, vitamin E, zinc, and caffeine on alveolar bone remodeling. Adipokines and direct effects of nutritional components on bone cells are proposed mechanisms linking diet and bone. Results from animal models substantiate the role of nutritional components on alveolar bone. It is a well-built starting point for clinical studies on nutritional monitoring and intervention for patients with alveolar bone disorders, especially those who are treatment refractory. Copyright © 2017 Elsevier Inc. All rights reserved.

Cocoa Polyphenols and Inflammatory Markers of Cardiovascular Disease

PubMed Central

Khan, Nasiruddin; Khymenets, Olha; Urpí-Sardà, Mireia; Tulipani, Sara; Garcia-Aloy, Mar; Monagas, María; Mora-Cubillos, Ximena; Llorach, Rafael; Andres-Lacueva, Cristina

2014-01-01

Epidemiological studies have demonstrated the beneficial effect of plant-derived food intake in reducing the risk of cardiovascular disease (CVD). The potential bioactivity of cocoa and its polyphenolic components in modulating cardiovascular health is now being studied worldwide and continues to grow at a rapid pace. In fact, the high polyphenol content of cocoa is of particular interest from the nutritional and pharmacological viewpoints. Cocoa polyphenols are shown to possess a range of cardiovascular-protective properties, and can play a meaningful role through modulating different inflammatory markers involved in atherosclerosis. Accumulated evidence on related anti-inflammatory effects of cocoa polyphenols is summarized in the present review. PMID:24566441

New bioactive and biobased product applications of pectin

USDA-ARS?s Scientific Manuscript database

Pectin is well known for its bioactive health-promoting properties and use in biobased products. Recent reports have demonstrated that pectin and pectic fractions have potential as prebiotics, prevent pathogenic bacterial adhesion, increase prostate specific antigen doubling time in patients with re...

Protein-based emulsion electrosprayed micro- and submicroparticles for the encapsulation and stabilization of thermosensitive hydrophobic bioactives.

PubMed

Gómez-Mascaraque, Laura G; López-Rubio, Amparo

2016-03-01

This work shows the potential of emulsion electrospraying of proteins using food-grade emulsions for the microencapsulation and enhanced protection of a model thermosensitive hydrophobic bioactive. Specifically, gelatin, a whey protein concentrate (WPC) and a soy protein isolate (SPI) were compared as emulsion stabilizers and wall matrices for encapsulation of α-linolenic acid. In a preliminary stage, soy bean oil was used as the hydrophobic component for the implementation of the emulsion electrospraying process, investigating the effect of protein type and emulsion protocol used (i.e. with or without ultrasound treatment) on colloidal stability. This oil was then substituted by the ω-3 fatty acid and the emulsions were processed by electrospraying and spray-drying, comparing both techniques. While the latter resulted in massive bioactive degradation, electrospraying proved to be a suitable alternative, achieving microencapsulation efficiencies (MEE) of up to ∼70%. Although gelatin yielded low MEEs due to the need of employing acetic acid for its processing by electrospraying, SPI and WPC achieved MEEs over 60% for the non-sonicated emulsions. Moreover, the degradation of α-linolenic acid at 80°C was significantly delayed when encapsulated within both matrices. Whilst less than an 8% of its alkene groups were detected after 27h of thermal treatment for free α-linolenic acid, up to 43% and 67% still remained intact within the electrosprayed SPI and WPC capsules, respectively. Copyright © 2015 Elsevier Inc. All rights reserved.

Using combined optimization, GC-MS and analytical technique to analyze the germination effect on phenolics, dietary fibers, minerals and GABA contents of Kodo millet (Paspalum scrobiculatum).

PubMed

Sharma, Seema; Saxena, Dharmesh C; Riar, Charanjit S

2017-10-15

A central composite rotatable design was applied to study the effects of soaking time, germination time and temperature on the responses; total phenolics, total flavonoids and antioxidant activity for the biochemical enhancement of bioactive components of Kodo millet. The optimum conditions for producing germinated Kodo millet flour of highest TPC (83.01mgGAE/100g), TFC (87.53mgRUE/g) and AoxA (91.34%), were soaking time (13.81h), germination temperature (38.75°C) and germination time (35.82h). Protein increased significantly form, 6.7 to 7.9%, dietary fibers from 35.30 to 38.34g/100g, minerals from 232.82 to 251.73mg/100g, GABA contents from 9.36 to 47.43mg/100g, whereas phytates and tannins decreased from 1.344 to 0.997mol/kg and 1.603 to 0.234mg/100g respectively, in optimized germinated Kodo millet sample. Six new bioactive compounds [n-propyl-9,12,15-octadecatrienoate (0.86%), pregan,20-one-2hydroxy,5,6,epox-15-methyl (3.45%), hexa-decanoicacid (8.19%), 9,O-ctadecenoicacid (5.00%), butyl-6,9,12,15-octadecatetraenoate (4.03%), hexadecanoicacid-methylester (1.43%)], synthesized as a result of germination under optimum conditions in the Kodo millet depicted the germination potential of millets as a source of valuable bioactive compounds. Copyright © 2017 Elsevier Ltd. All rights reserved.

Cigarette smoke increases Staphylococcus aureus biofilm formation via oxidative stress.

PubMed

Kulkarni, Ritwij; Antala, Swati; Wang, Alice; Amaral, Fábio E; Rampersaud, Ryan; Larussa, Samuel J; Planet, Paul J; Ratner, Adam J

2012-11-01

The strong epidemiological association between cigarette smoke (CS) exposure and respiratory tract infections is conventionally attributed to immunosuppressive and irritant effects of CS on human cells. Since pathogenic bacteria such as Staphylococcus aureus are members of the normal microbiota and reside in close proximity to human nasopharyngeal cells, we hypothesized that bioactive components of CS might affect these organisms and potentiate their virulence. Using Staphylococcus aureus as a model organism, we observed that the presence of CS increased both biofilm formation and host cell adherence. Analysis of putative molecular pathways revealed that CS exposure decreased expression of the quorum-sensing agr system, which is involved in biofilm dispersal, and increased transcription of biofilm inducers such as sarA and rbf. CS contains bioactive compounds, including free radicals and reactive oxygen species, and we observed transcriptional induction of bacterial oxidoreductases, including superoxide dismutase, following exposure. Moreover, pretreatment of CS with an antioxidant abrogated CS-mediated enhancement of biofilms. Exposure of bacteria to hydrogen peroxide alone increased biofilm formation. These observations are consistent with the hypothesis that CS induces staphylococcal biofilm formation in an oxidant-dependent manner. CS treatment induced transcription of fnbA (encoding fibronectin binding protein A), leading to increased binding of CS-treated staphylococci to immobilized fibronectin and increased adherence to human cells. These observations indicate that the bioactive effects of CS may extend to the resident microbiota of the nasopharynx, with implications for the pathogenesis of respiratory infection in CS-exposed humans.

Preparation of Microkernel-Based Mesoporous (SiO2-CdTe-SiO2)@SiO2 Fluorescent Nanoparticles for Imaging Screening and Enrichment of Heat Shock Protein 90 Inhibitors from Tripterygium Wilfordii.

PubMed

Hu, Yue; Miao, Zhao-Yi; Zhang, Xiao-Jing; Yang, Xiao-Tong; Tang, Ying-Ying; Yu, Sheng; Shan, Chen-Xiao; Wen, Hong-Mei; Zhu, Dong

2018-05-01

The currently utilized ligand fishing for bioactive molecular screening from complex matrixes cannot perform imaging screening. Here, we developed a new solid-phase ligand fishing coupled with an in situ imaging protocol for the specific enrichment and identification of heat shock protein 90 (Hsp 90) inhibitors from Tripterygium wilfordii, utilizing a multiple-layer and microkernel-based mesoporous nanostructure composed of a protective silica coating CdTe quantum dot (QD) core and a mesoporous silica shell, i.e., microkernel-based mesoporous (SiO 2 -CdTe-SiO 2 )@SiO 2 fluorescent nanoparticles (MMFNPs) as extracting carries and fluorescent probes. The prepared MMFNPs showed a highly uniform spherical morphology, retention of fluorescence emission, and great chemical stability. The fished ligands by Hsp 90α-MMFNPs were evaluated via the preliminary bioactivity based on real-time cellular morphology imaging by confocal laser scanning microscopy (CLSM) and then identified by mass spectrometry (MS). Celastrol was successfully isolated as an Hsp 90 inhibitor, and two other specific components screened by Hsp 90α-MMFNPs, i.e., demecolcine and wilforine, were preliminarily identified as potential Hsp 90 inhibitors through the verification of strong affinity to Hsp 90 and antitumor bioactivity. The approach based on the MMFNPs provides a strong platform for imaging screening and discovery of plant-derived biologically active molecules with high efficiency and selectivity.

Immense essence of excellence: marine microbial bioactive compounds.

PubMed

Bhatnagar, Ira; Kim, Se-Kwon

2010-10-15

Oceans have borne most of the biological activities on our planet. A number of biologically active compounds with varying degrees of action, such as anti-tumor, anti-cancer, anti-microtubule, anti-proliferative, cytotoxic, photo protective, as well as antibiotic and antifouling properties, have been isolated to date from marine sources. The marine environment also represents a largely unexplored source for isolation of new microbes (bacteria, fungi, actinomycetes, microalgae-cyanobacteria and diatoms) that are potent producers of bioactive secondary metabolites. Extensive research has been done to unveil the bioactive potential of marine microbes (free living and symbiotic) and the results are amazingly diverse and productive. Some of these bioactive secondary metabolites of microbial origin with strong antibacterial and antifungal activities are being intensely used as antibiotics and may be effective against infectious diseases such as HIV, conditions of multiple bacterial infections (penicillin, cephalosporines, streptomycin, and vancomycin) or neuropsychiatric sequelae. Research is also being conducted on the general aspects of biophysical and biochemical properties, chemical structures and biotechnological applications of the bioactive substances derived from marine microorganisms, and their potential use as cosmeceuticals and nutraceuticals. This review is an attempt to consolidate the latest studies and critical research in this field, and to showcase the immense competence of marine microbial flora as bioactive metabolite producers. In addition, the present review addresses some effective and novel approaches of procuring marine microbial compounds utilizing the latest screening strategies of drug discovery.

Immense Essence of Excellence: Marine Microbial Bioactive Compounds

PubMed Central

Bhatnagar, Ira; Kim, Se-Kwon

2010-01-01

Oceans have borne most of the biological activities on our planet. A number of biologically active compounds with varying degrees of action, such as anti-tumor, anti-cancer, anti-microtubule, anti-proliferative, cytotoxic, photo protective, as well as antibiotic and antifouling properties, have been isolated to date from marine sources. The marine environment also represents a largely unexplored source for isolation of new microbes (bacteria, fungi, actinomycetes, microalgae-cyanobacteria and diatoms) that are potent producers of bioactive secondary metabolites. Extensive research has been done to unveil the bioactive potential of marine microbes (free living and symbiotic) and the results are amazingly diverse and productive. Some of these bioactive secondary metabolites of microbial origin with strong antibacterial and antifungal activities are being intensely used as antibiotics and may be effective against infectious diseases such as HIV, conditions of multiple bacterial infections (penicillin, cephalosporines, streptomycin, and vancomycin) or neuropsychiatric sequelae. Research is also being conducted on the general aspects of biophysical and biochemical properties, chemical structures and biotechnological applications of the bioactive substances derived from marine microorganisms, and their potential use as cosmeceuticals and nutraceuticals. This review is an attempt to consolidate the latest studies and critical research in this field, and to showcase the immense competence of marine microbial flora as bioactive metabolite producers. In addition, the present review addresses some effective and novel approaches of procuring marine microbial compounds utilizing the latest screening strategies of drug discovery. PMID:21116414

Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity

PubMed Central

Godoy, Luis D.; Lucas, Julianna E.; Bender, Abigail J.; Romanick, Samantha S.; Ferguson, Bradley S.

2017-01-01

Scope Nutrigenomics is a rapidly expanding field that elucidates the link between diet-genome interactions. Recent evidence demonstrates that regulation of the epigenome, and in particular inhibition of HDACs, impact pathogenetic mechanisms involved in chronic disease. Few studies, to date, have screened libraries of bioactive compounds that act as epigenetic modifiers. This study screened a library of 131 natural compounds to determine bioactive compounds that inhibit Zn-dependent HDAC activity. Methods and results Using class-specific HDAC substrates, we screened 131 natural compounds for HDAC activity in bovine cardiac tissue. From this screen, we identified 18 bioactive compound HDAC inhibitors. Using our class-specific HDAC substrates, we next screened these 18 bioactive compounds against recombinant HDAC proteins. Consistent with inhibition of HDAC activity, these compounds were capable of inhibiting activity of individual HDAC isoforms. Lastly, we report that treatment of H9c2 cardiac myoblasts with bioactive HDAC inhibitors was sufficient to increase lysine acetylation as assessed via immunoblot. Conclusion This study provided the first step in identifying multiple bioactive compound HDAC inhibitors. Taken together, this report sets the stage for future exploration of these bioactive compounds as epigenetic regulators to potentially ameliorate chronic disease. PMID:27981795

A new synthesis route to high surface area sol gel bioactive glass through alcohol washing

PubMed Central

M. Mukundan, Lakshmi; Nirmal, Remya; Vaikkath, Dhanesh; Nair, Prabha D.

2013-01-01

Bioactive glass is one of the widely used bone repair material due to its unique properties like osteoconductivity, osteoinductivity and biodegradability. In this study bioactive glass is prepared by the sol gel process and stabilized by a novel method that involves a solvent instead of the conventional calcinations process. This study represents the first attempt to use this method for the stabilization of bioactive glass. The bioactive glass stabilized by this ethanol washing process was characterized for its physicochemical and biomimetic property in comparison with similar composition of calcined bioactive glass. The compositional similarity of the two stabilized glass powders was confirmed by spectroscopic and thermogravimetric analysis. Other physicochemical characterizations together with the cell culture studies with L929 fibroblast cells and bone marrow mesenchymal stem cells proved that the stabilization was achieved with the retention of its inherent bioactive potential. However an increase in the surface area of the glass powder was obtained as a result of this ethanol washing process and this add up to the success of the study. Hence the present study exhibits a promising route for high surface area bioactive glass for increasing biomimicity. PMID:23512012

Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity.

PubMed

Godoy, Luis D; Lucas, Julianna E; Bender, Abigail J; Romanick, Samantha S; Ferguson, Bradley S

2017-04-01

Nutrigenomics is a rapidly expanding field that elucidates the link between diet-genome interactions. Recent evidence demonstrates that regulation of the epigenome, and in particular inhibition of histone deacetylases (HDACs), impact pathogenetic mechanisms involved in chronic disease. Few studies, to date, have screened libraries of bioactive compounds that act as epigenetic modifiers. This study screened a library of 131 natural compounds to determine bioactive compounds that inhibit Zn-dependent HDAC activity. Using class-specific HDAC substrates, we screened 131 natural compounds for HDAC activity in bovine cardiac tissue. From this screen, we identified 18 bioactive compound HDAC inhibitors. Using our class-specific HDAC substrates, we next screened these 18 bioactive compounds against recombinant HDAC proteins. Consistent with inhibition of HDAC activity, these compounds were capable of inhibiting activity of individual HDAC isoforms. Lastly, we report that treatment of H9c2 cardiac myoblasts with bioactive HDAC inhibitors was sufficient to increase lysine acetylation as assessed via immunoblot. This study provided the first step in identifying multiple bioactive compound HDAC inhibitors. Taken together, this report sets the stage for future exploration of these bioactive compounds as epigenetic regulators to potentially ameliorate chronic disease. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Screening and identification of three typical phenylethanoid glycosides metabolites from Cistanches Herba by human intestinal bacteria using UPLC/Q-TOF-MS.

PubMed

Li, Yang; Zhou, Guisheng; Peng, Ying; Tu, Pengfei; Li, Xiaobo

2016-01-25

Acteoside, isoacteoside, and 2'-acetylacteoside are three representative phenylethanoid glycosides (PhGs), which are widely distributed in many plants and also known as the active components of Cistanches Herba. However, the extremely low oral bioavailability of acteoside in rats implies that these structural similar components may go through multiple sequential routes of hydrolysis in gastrointestinal tract before they are absorbed into blood. Therefore, the metabolites of these three components and other PhGs from gastrointestinal tract such as echinacoside, are supposed to be the bioactive elements. In this study, we established an approach combining ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) with MS(E) technology and MetaboLynx™ software for the rapid metabolic profiling of acteoside, isoacteoside, and 2'-acetylacteoside by human intestinal bacteria. As a result, 11 metabolites of acteoside, 7 metabolites of isoacteoside, and 11 metabolites of 2'-acetylacteoside were identified respectively. 8 metabolic pathways including deglycosylation, de-rhamnose, de-hydroxytyrosol, de-caffeoyl, deacetylation, reduction, acetylation, and sulfate conjugation were proposed to involve in the generation of these metabolites. Furthermore, we found that the degraded metabolites hydroxytyrosol (HT) and 3-hydroxyphenylpropionic (3-HPP) were transformed from acteoside, isoacteoside, and 2'-acetylacteoside by human intestinal bacteria and demonstrated similar bioactivities to their precursors. These findings are significant for our understanding of the metabolism of PhGs and the proposed metabolic pathways of bioactive components might be crucial for further pharmacokinetic evaluations of Cistanches Herba. Copyright © 2015 Elsevier B.V. All rights reserved.

A modeling approach to evaluate the balance between bioactivation and detoxification of MeIQx in human hepatocytes

PubMed Central

Delannée, Victorien; Théret, Nathalie; Siegel, Anne

2017-01-01

Background Heterocyclic aromatic amines (HAA) are environmental and food contaminants that are potentially carcinogenic for humans. 2-Amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) is one of the most abundant HAA formed in cooked meat. MeIQx is metabolized by cytochrome P450 1A2 in the human liver into detoxificated and bioactivated products. Once bioactivated, MeIQx metabolites can lead to DNA adduct formation responsible for further genome instability. Methods Using a computational approach, we developed a numerical model for MeIQx metabolism in the liver that predicts the MeIQx biotransformation into detoxification or bioactivation pathways according to the concentration of MeIQx. Results Our results demonstrate that (1) the detoxification pathway predominates, (2) the ratio between detoxification and bioactivation pathways is not linear and shows a maximum at 10 µM of MeIQx in hepatocyte cell models, and (3) CYP1A2 is a key enzyme in the system that regulates the balance between bioactivation and detoxification. Our analysis suggests that such a ratio could be considered as an indicator of MeIQx genotoxicity at a low concentration of MeIQx. Conclusions Our model permits the investigation of the balance between bioactivation (i.e., DNA adduct formation pathway through the prediction of potential genotoxic compounds) and detoxification of MeIQx in order to predict the behaviour of this environmental contaminant in the human liver. It highlights the importance of complex regulations of enzyme competitions that should be taken into account in any further multi-organ models. PMID:28879062

Seaweed as a source of novel nutraceuticals: sulfated polysaccharides and peptides.

PubMed

Jiménez-Escrig, A; Gómez-Ordóñez, E; Rupérez, P

2011-01-01

Seaweeds and seaweed-derived products are underexploited marine bioresources and a source of natural ingredients for functional foods. Nutritional studies on seaweeds indicate that brown and red seaweeds possess a good nutritional quality and could be used as an alternative source of dietary fiber, protein, and minerals. Moreover, bioactive sulfated polysaccharides are the main components of soluble fiber in seaweeds and also bioactive peptides can be prepared from seaweed protein. This chapter gives an overview of the main biological properties of sulfated polysaccharides and peptides from brown and red seaweeds. Recent studies have provided evidence that sulfated polysaccharides from seaweeds can play a vital role in human health and nutrition. Besides, peptides derived from algal protein are most promising as antihypertensive agents. Further research work, especially in vivo studies, are needed in order to gain a better knowledge of the relation structure-function by which bioactive compounds from seaweeds exert their bioactivity. Copyright © 2011 Elsevier Inc. All rights reserved.

78 FR 36786 - Linking Marketplace Heparin Product Attributes and Manufacturing Processes to Bioactivity and...

Federal Register 2010, 2011, 2012, 2013, 2014

2013-06-19

... heparin. The condition leads to formation of abnormal blood clots and concomitant complications associated... antibody formation although these smaller chain length heparins are much less likely to lead to clinical... components of heparin that lead to the pathogenesis of HIT is the lack of pure component heparin standards...

Hydroxyapatite and bioactive glass surfaces for fiber reinforced composite implants via surface ablation by Excimer laser.

PubMed

Kulkova, Julia; Moritz, Niko; Huhtinen, Hannu; Mattila, Riina; Donati, Ivan; Marsich, Eleonora; Paoletti, Sergio; Vallittu, Pekka K

2017-11-01

In skeletal reconstructions, composites, such as bisphenol-A-glycidyldimethacrylate resin reinforced with glass fibers, are potentially useful alternatives to metallic implants. Recently, we reported a novel method to prepare bioactive surfaces for these composites. Surface etching by Excimer laser was used to expose bioactive glass granules embedded in the resin. The purpose of this study was to analyze two types of bioactive surfaces created by this technique. The surfaces contained bioactive glass and hydroxyapatite granules. The selected processing parameters were adequate for the creation of the surfaces. However, the use of porous hydroxyapatite prevented the complete exposure the granules. In cell culture, for bioactive glass coatings, the pattern of proliferation of MG63 cells was comparable to that in the positive control group (Ti6Al4V) while inferior cell proliferation was observed on the surfaces containing hydroxyapatite granules. Scanning electron microscopy revealed osteointegration of implants with both types of surfaces. The technique is suitable for the exposure of solid bioactive glass granules. However, the long-term performance of the surfaces needs further assessment. Copyright © 2017 Elsevier Ltd. All rights reserved.

Rapid Screening for α-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration–HPLC-MS

PubMed Central

Chen, Guilin; Guo, Mingquan

2017-01-01

Gymnema sylvestre R. Br. (Asclepiadaceae) has been known to posses potential anti-diabetic activity, and the gymnemic acids were reported as the main bioactive components in this plant species. However, the specific components responsible for the hypoglycemic effect still remain unknown. In the present study, the in vitro study revealed that the extract of G. sylvestre exhibited significant inhibitory activity against α-glucosidase with IC50 at 68.70 ± 1.22 μg/mL compared to acarbose (positive control) at 59.03 ± 2.30 μg/mL, which further indicated the potential anti-diabetic activity. To this end, a method based on affinity ultrafiltration coupled with liquid chromatography mass spectrometry (UF-HPLC-MS) was established to rapidly screen and identify the α-glucosidase inhibitors from G. sylvestre. In this way, 9 compounds with higher enrichment factors (EFs) were identified according to their MS/MS spectra. Finally, the structure-activity relationships revealed that glycosylation could decrease the potential antisweet activity of sapogenins, and other components except gymnemic acids in G. sylvestre could also be good α-glucosidase inhibitors due to their synergistic effects. Taken together, the proposed method combing α-glucosidase and UF-HPLC-MS presents high efficiency for rapidly screening and identifying potential inhibitors of α-glucosidase from complex natural products, and could be further explored as a valuable high-throughput screening (HTS) platform in the early anti-diabetic drug discovery stage. PMID:28496409

Rapid Screening for α-Glucosidase Inhibitors from Gymnema sylvestre by Affinity Ultrafiltration-HPLC-MS.

PubMed

Chen, Guilin; Guo, Mingquan

2017-01-01

Gymnema sylvestre R. Br. (Asclepiadaceae) has been known to posses potential anti-diabetic activity, and the gymnemic acids were reported as the main bioactive components in this plant species. However, the specific components responsible for the hypoglycemic effect still remain unknown. In the present study, the in vitro study revealed that the extract of G. sylvestre exhibited significant inhibitory activity against α-glucosidase with IC 50 at 68.70 ± 1.22 μg/mL compared to acarbose (positive control) at 59.03 ± 2.30 μg/mL, which further indicated the potential anti-diabetic activity. To this end, a method based on affinity ultrafiltration coupled with liquid chromatography mass spectrometry (UF-HPLC-MS) was established to rapidly screen and identify the α-glucosidase inhibitors from G. sylvestre . In this way, 9 compounds with higher enrichment factors (EFs) were identified according to their MS/MS spectra. Finally, the structure-activity relationships revealed that glycosylation could decrease the potential antisweet activity of sapogenins, and other components except gymnemic acids in G. sylvestre could also be good α-glucosidase inhibitors due to their synergistic effects. Taken together, the proposed method combing α-glucosidase and UF-HPLC-MS presents high efficiency for rapidly screening and identifying potential inhibitors of α-glucosidase from complex natural products, and could be further explored as a valuable high-throughput screening (HTS) platform in the early anti-diabetic drug discovery stage.

Antimicrobial potential of macro and microalgae against pathogenic and spoilage microorganisms in food.

PubMed

Pina-Pérez, M C; Rivas, A; Martínez, A; Rodrigo, D

2017-11-15

Algae are a valuable and never-failing source of bioactive compounds. The increasing efforts to use ingredients that are as natural as possible in the formulation of innovative products has given rise to the introduction of macro and microalgae in food industry. To date, scarce information has been published about algae ingredients as antimicrobials in food. The antimicrobial potential of algae is highly dependent on: (i) type, brown algae being the most effective against foodborne bacteria; (ii) the solvent used in the extraction of bioactive compounds, ethanolic and methanolic extracts being highly effective against Gram-positive and Gram-negative bacteria; and (iii) the concentration of the extract. The present paper reviews the main antimicrobial potential of algal species and their bioactive compounds in reference and real food matrices. The validation of the algae antimicrobial potential in real food matrices is still a research niche, being meat and bakery products the most studied substrates. Copyright © 2017 Elsevier Ltd. All rights reserved.

Zirconia toughened alumina ceramic foams for potential bone graft applications: fabrication, bioactivation, and cellular responses.

PubMed

He, X; Zhang, Y Z; Mansell, J P; Su, B

2008-07-01

Zirconia toughened alumina (ZTA) has been regarded as the next generation orthopedic graft material due to its excellent mechanical properties and biocompatibility. Porous ZTA ceramics with good interconnectivity can potentially be used as bone grafts for load-bearing applications. In this work, three-dimensional (3D) interconnected porous ZTA ceramics were fabricated using a direct foaming method with egg white protein as binder and foaming agent. The results showed that the porous ZTA ceramics possessed a bimodal pore size distribution. Their mechanical properties were comparable to those of cancellous bone. Due to the bio-inertness of alumina and zirconia ceramics, surface bioactivation of the ZTA foams was carried out in order to improve their bioactivity. A simple NaOH soaking method was employed to change the surface chemistry of ZTA through hydroxylation. Treated samples were tested by conducting osteoblast-like cell culture in vitro. Improvement on cells response was observed and the strength of porous ZTA has not been deteriorated after the NaOH treatment. The porous 'bioactivated' ZTA ceramics produced here could be potentially used as non-degradable bone grafts for load-bearing applications.

Investigation of the Biosynthetic Potential of Endophytes in Traditional Chinese Anticancer Herbs

PubMed Central

Miller, Kristin I.; Qing, Chen; Sze, Daniel Man Yuen; Neilan, Brett A.

2012-01-01

Traditional Chinese medicine encompasses a rich empirical knowledge of the use of plants for the treatment of disease. In addition, the microorganisms associated with medicinal plants are also of interest as the producers of the compounds responsible for the observed plant bioactivity. The present study has pioneered the use of genetic screening to assess the potential of endophytes to synthesize bioactive compounds, as indicated by the presence of non-ribosomal peptide synthetase (NRPS) and polyketide synthase (PKS) genes. The total DNA extracts of 30 traditional Chinese herbs, were screened for functional genes involved in the biosynthesis of bioactive compounds. The four PCR screens were successful in targeting four bacterial PKS, six bacterial NRPS, ten fungal PKS and three fungal NRPS gene fragments. Analysis of the detected endophyte gene fragments afforded consideration of the possible bioactivity of the natural products produced by endophytes in medicinal herbs. This investigation describes a rapid method for the initial screening of medicinal herbs and has highlighted a subset of those plants that host endophytes with biosynthetic potential. These selected plants can be the focus of more comprehensive endophyte isolation and natural product studies. PMID:22629306

Formulation, evaluation and bioactive potential of Xylaria primorskensis terpenoid nanoparticles from its major compound xylaranic acid.

PubMed

Adnan, Mohd; Patel, Mitesh; Reddy, Mandadi Narsimha; Alshammari, Eyad

2018-01-29

In recent years, fungi have been shown to produce a plethora of new bioactive secondary metabolites of interest, as new lead structures for medicinal and other pharmacological applications. The present investigation was carried out to study the pharmacological properties of a potent and major bioactive compound: xylaranic acid, which was obtained from Xylaria primorskensis (X. primorskensis) terpenoids in terms of antibacterial activity, antioxidant potential against DPPH & H 2 O 2 radicals and anticancer activity against human lung cancer cells. Due to terpenoid nature, low water solubility and wretched bioavailability, its pharmacological use is limited. To overcome these drawbacks, a novel xylaranic acid silver nanoparticle system (AgNPs) is developed. In addition to improving its solubility and bioavailability, other advantageous pharmacological properties has been evaluated. Furthermore, enhanced anticancer activity of xylaranic acid and its AgNPs due to induced apoptosis were also confirmed by determining the expression levels of apoptosis regulatory genes p53, bcl-2 and caspase-3 via qRT PCR method. This is the first study developing the novel xylaranic acid silver nanoparticle system and enlightening its therapeutic significance with its improved physico-chemical properties and augmented bioactive potential.

ToxCast: Developing Predictive Signatures of Chemically Induced Toxicity (Developing Predictive Bioactivity Signatures from ToxCasts HTS Data)

EPA Science Inventory

ToxCast, the United States Environmental Protection Agency’s chemical prioritization research program, is developing methods for utilizing computational chemistry, bioactivity profiling and toxicogenomic data to predict potential for toxicity and prioritize limited testing resour...

EPAs ToxCast Research Program: Developing Predictive Bioactivity Signatures for Chemicals

EPA Science Inventory

The international community needs better predictive tools for assessing the hazards and risks of chemicals. It is technically feasible to collect bioactivity data on virtually all chemicals of potential concern ToxCast is providing a proof of concept for obtaining predictive, b...

Cranberries and their bioactive constituents in human health

USDA-ARS?s Scientific Manuscript database

Recent observational and clinical studies have raised interest in the potential health effects of cranberry consumption, an association that appears due to the phytochemical content of this fruit. The profile of cranberry bioactives is distinct from other berry fruit, being rich in A-type proanthocy...

Stability of bioactive compounds in butiá (Butia odorata) fruit pulp and nectar.

PubMed

Hoffmann, Jessica Fernanda; Zandoná, Giovana Paula; Dos Santos, Priscila Silveira; Dallmann, Camila Müller; Madruga, Francine Bonemann; Rombaldi, Cesar Valmor; Chaves, Fábio Clasen

2017-12-15

Butia odorata is a palm tree native to southern Brazil whose fruit (known as butiá) and leaves are used to make many food products and crafts. Butiá contain several biologically active compounds with potential health benefits. However, processing conditions can alter quality attributes including bioactive compound content. This study evaluated the stability of bioactive compounds in butiá pulp upon pasteurization, during 12months of frozen storage, and in butiá nectar after a 3-month storage period. Pulp pasteurization resulted in a reduction in phenolic, flavonoid, carotenoid, and ascorbic acid contents. After a 12-month frozen storage period, flavonoid, phenolic, and ascorbic acid contents decreased while carotenoid content remained unaltered. Carotenoid, ascorbic acid, and phenolic contents were unaffected by the 3-month storage of butiá nectar; however, flavonoid content and antioxidant potential were reduced. Despite bioactive compound degradation upon heat treatment and storage, butiá nectar remained rich in phenolics, especially (-)-epicatechin, rutin, and (+)-catechin. Copyright © 2017 Elsevier Ltd. All rights reserved.

Chemical, Bioactive, and Antioxidant Potential of Twenty Wild Culinary Mushroom Species

PubMed Central

Sharma, S. K.; Gautam, N.

2015-01-01

The chemical, bioactive, and antioxidant potential of twenty wild culinary mushroom species being consumed by the people of northern Himalayan regions has been evaluated for the first time in the present study. Nutrients analyzed include protein, crude fat, fibres, carbohydrates, and monosaccharides. Besides, preliminary study on the detection of toxic compounds was done on these species. Bioactive compounds evaluated are fatty acids, amino acids, tocopherol content, carotenoids (β-carotene, lycopene), flavonoids, ascorbic acid, and anthocyanidins. Fruitbodies extract of all the species was tested for different types of antioxidant assays. Although differences were observed in the net values of individual species all the species were found to be rich in protein, and carbohydrates and low in fat. Glucose was found to be the major monosaccharide. Predominance of UFA (65–70%) over SFA (30–35%) was observed in all the species with considerable amounts of other bioactive compounds. All the species showed higher effectiveness for antioxidant capacities. PMID:26199938

Nanocellulose-based composites and bioactive agents for food packaging.

PubMed

Khan, Avik; Huq, Tanzina; Khan, Ruhul A; Riedl, Bernard; Lacroix, Monique

2014-01-01

Global environmental concern, regarding the use of petroleum-based packaging materials, is encouraging researchers and industries in the search for packaging materials from natural biopolymers. Bioactive packaging is gaining more and more interest not only due to its environment friendly nature but also due to its potential to improve food quality and safety during packaging. Some of the shortcomings of biopolymers, such as weak mechanical and barrier properties can be significantly enhanced by the use of nanomaterials such as nanocellulose (NC). The use of NC can extend the food shelf life and can also improve the food quality as they can serve as carriers of some active substances, such as antioxidants and antimicrobials. The NC fiber-based composites have great potential in the preparation of cheap, lightweight, and very strong nanocomposites for food packaging. This review highlights the potential use and application of NC fiber-based nanocomposites and also the incorporation of bioactive agents in food packaging.

Bioactives in Chinese Proprietary Medicine Modulates 5α-Reductase Activity and Gene Expression Associated with Androgenetic Alopecia

PubMed Central

Tan, Justin J. Y.; Pan, Jing; Sun, Lihan; Zhang, Junying; Wu, Chunyong; Kang, Lifeng

2017-01-01

Androgenetic alopecia (AGA) is characterized by a progressive and patterned transformation of thick, pigmented terminal scalp hairs into short, hypo-pigmented vellus-like hairs. The use of Minoxidil and Finasteride to treat AGA are often associated with complications in safety and efficacy. However, herbal remedies are deemed to have lesser side effects in many societies. This study aims to identify potential hair growth properties of individual compounds from a Chinese proprietary medicine known as Yangxue Shengfa capsule (YSC), used in China for many years for improving AGA. Six marker compounds, including 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside (TSG), Chlorogenic acid, Emodin, Ferulic acid, Isoimperatorin, and Paeoniflorin were used for simultaneous HPLC quantification and anti-AGA in-vitro screening. Simultaneous quantification of these components was performed on 75% (v/v) methanol extracts of YSC, using a Welch Ultimate XB-C18 column and gradient elution. Five compounds significantly promoted cell proliferation in cultured immortalized human Dermal Papilla Cells (DPC). Multiple genes associated with the progression of AGA, including IGF-1, DKK-1, and TGF-β1, were found to be regulated by some of these compounds. Interestingly, Ferulic acid and Emodin demonstrated good pharmacological properties against AGA, thereby concluding the potential of these bioactives to be used in the treatment against AGA. PMID:28450835

Phyllanthus wightianus Müll. Arg.: A Potential Source for Natural Antimicrobial Agents

PubMed Central

Natarajan, D.; Srinivasan, R.; Shivakumar, M. S.

2014-01-01

Phyllanthus wightianus belongs to Euphorbiaceae family having ethnobotanical importance. The present study deals with validating the antimicrobial potential of solvent leaf extracts of P. wightianus. 11 human bacterial pathogens (Bacillus subtilis, Streptococcus pneumoniae, Staphylococcus epidermidis, Proteus vulgaris, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhimurium, Escherichia coli, Shigella flexneri, Proteus vulgaris, and Serratia marcescens) and 4 fungal pathogens (Candida albicans, Cryptococcus neoformans, Mucor racemosus, and Aspergillus niger) were also challenged with solvent leaf extracts usingagar well and disc diffusion methods. Further, identification of the active component present in the bioactive extract was done using GC-MS analysis. Results show that all extracts exhibited broad spectrum (6–29 mm) of antibacterial activity on most of the tested organisms. The results highlight the fact that the well in agar method was more effective than disc diffusion method. Significant antimicrobial activity was detected in methanol extract against S. pneumoniae (29 mm) with MIC and MBC values of 15.62 μg/mL. GC-MS analysis revealed that 29 bioactive constituents were present in methanolic extract of P. wightianus, of which 9,12-octadecaenioic acid (peak area 22.82%; RT-23.97) and N-hexadecanoic acid (peak area 21.55% RT-21.796) are the major compounds. The findings of this study show that P. wightianus extracts may be used as an anti-infective agent in folklore medicine. PMID:24883301

A Python Analytical Pipeline to Identify Prohormone Precursors and Predict Prohormone Cleavage Sites

PubMed Central

Southey, Bruce R.; Sweedler, Jonathan V.; Rodriguez-Zas, Sandra L.

2008-01-01

Neuropeptides and hormones are signaling molecules that support cell–cell communication in the central nervous system. Experimentally characterizing neuropeptides requires significant efforts because of the complex and variable processing of prohormone precursor proteins into neuropeptides and hormones. We demonstrate the power and flexibility of the Python language to develop components of an bioinformatic analytical pipeline to identify precursors from genomic data and to predict cleavage as these precursors are en route to the final bioactive peptides. We identified 75 precursors in the rhesus genome, predicted cleavage sites using support vector machines and compared the rhesus predictions to putative assignments based on homology to human sequences. The correct classification rate of cleavage using the support vector machines was over 97% for both human and rhesus data sets. The functionality of Python has been important to develop and maintain NeuroPred (http://neuroproteomics.scs.uiuc.edu/neuropred.html), a user-centered web application for the neuroscience community that provides cleavage site prediction from a wide range of models, precision and accuracy statistics, post-translational modifications, and the molecular mass of potential peptides. The combined results illustrate the suitability of the Python language to implement an all-inclusive bioinformatics approach to predict neuropeptides that encompasses a large number of interdependent steps, from scanning genomes for precursor genes to identification of potential bioactive neuropeptides. PMID:19169350

Bioactive sterols from marine resources and their potential benefits for human health.

PubMed

Kim, Se-Kwon; Van Ta, Quang

2012-01-01

Bioactive agents from marine resources have shown their valuable health beneficial effects. Therefore, increase knowledge on novel functional ingredients with biological activities from marine animal and microbe has gained much attention. Sterols are recognized as potential in development functional food ingredients and pharmaceutical agents. Marine resources, with a great diversity, can be a very interesting natural resource of sterols. This chapter focuses on biological activities of marine animal and microbe sterols with potential health beneficial applications in functional foods and pharmaceuticals. Copyright © 2012 Elsevier Inc. All rights reserved.

High therapeutic potential of Spilanthes acmella: A review

PubMed Central

Prachayasittikul, Veda; Prachayasittikul, Supaluk; Ruchirawat, Somsak; Prachayasittikul, Virapong

2013-01-01

Spilanthes acmella, a well known antitoothache plant with high medicinal usages, has been recognized as an important medicinal plant and has an increasingly high demand worldwide. From its traditional uses in health care and food, extensive phytochemical studies have been reported. This review provides an overview and general description of the plant species, bioactive metabolites and important pharmacological activities including the preparation, purification and in vitro large-scale production. Structure-activity relationships of the bioactive compounds have been discussed. Considering data from the literature, it could be demonstrated that S. acmella possesses diverse bioactive properties and immense utilization in medicine, health care, cosmetics and as health supplements. As a health food, it is enriched with high therapeutic value with high potential for further development. PMID:27092032

Antibacterial activity of kecombrang flower extract (Nicolaia speciosa) microencapsulation with food additive materials formulation

NASA Astrophysics Data System (ADS)

Naufalin, R.; Rukmini, H. S.

2018-01-01

Kecombrang flower (Nicolaia speciosa) contains bioactive components of alkaloids, flavonoids, polyphenols, steroids, saponins, and essential oils as potential antimicrobials. The use of antibacterials in the form of essential oils has constraints; therefore microencapsulation needs to be done to prevent damage to the bioactive components. Microencapsulation can prevent degradation due to radiation or oxygen, easy-mix with foodstuffs and also slow the occurrence of evaporation. This study aimed to determine the effect of types of kecombrang extract, the concentration of microcapsules in food additives (NaCl and sucrose), and concentration of flower extract in the microcapsules. This study used Randomized Block Design (RBD) with 18 treatment combinations and two replications. Factors studied were types of kecombrang flower extract of (semi polar and polar extract), Food Additive types (sucrose and NaCl), the concentration of microcapsules in food additive (0%; 15%; 30% w /v). The results showed that polar and non-polar extract microcapsules produced antibacterial activity of 7.178 mm and 7.145 respectively of Bacillus cereus bacteria, while Escherichia coli was 7.272 mm and 7.289 mm respectively. A 30 percent microcapsule concentration provides antibacterial activity with inhibiting zone of 7, 818 mm for B. cereus and 8,045 for E.coli. Food Additive of sucrose concentrations showed that microcapsules produced tend to be more effective in inhibiting the growth of E.coli and B. cereus bacteria than that of NaCl, with each inhibition zone of 7.499 mm and 7.357 mm

Extraction and identification of bioactive components in Sida cordata (Burm.f.) using gas chromatography-mass spectrometry.

PubMed

Ganesh, Mani; Mohankumar, Murugan

2017-09-01

Sida cordata (Burm.f.) is a pineal tropical plant in the family Malvaceae that is found throughout India and used to treat various diseases and ailments in many complementary and alternative medicine systems. This study identified the bioactive components present in whole-plant ethanol extracts of S . cordata using gas chromatography-mass spectrometry (GC-MS). Based on their retention times (RT) and mass-to-charge ratios (m/z), 29 bioactive compounds were identified: nonanoic acid, vitamin D 3 , 3-trifluroacetoxypentadecane, α-d-glucopyranoside, O-α-d-glucopyranosyl-(1.fwdarw.3)-α-d-fructofuranosyl,3,7,11,15-tetramethyl-2-hexadecan-1-ol, octadecanoic acid, ethyl ester, phytol, 9,12-octadecadienoic acid, methyl ester (E,E), 9,12,15-octadecadienoic acid, methyl ester (Z,Z,Z), oleic acid, 1,2-15,16-diepoxyhexadecane, 3-hexadecyloxycarbonyl-5-(2-hydroxyethyl)-4-methylimidazolium ion, methoxyacetic acid, 4-tetradecyl ester, 1,2-benzenedicarboxylic acid, mono (2-ethylhexyl) ester, 1-iodo-2-methylundecane, dodecane, 2,6,10-trimethyl-, 2-piperidinone-N-[4-bromo-n-butyl]-, squalene, octadecane-1-(ethenyloxy)-, Z,Z-2,5-pentadecadien-1-ol, 1-hexadecanol, 2-methyl-, spiro[androst-5ene-17,1'-cyclobutan]-2'-one-3-hydroxy-, (3a,17a)-, diethylene glycol monododecyl ether, vitamin E, cholestan-3-ol, 2-methylene-, (3a,5a)-, 2H-pyran, 2-(7-heptadecynyloxy)tetrahydro-, and cis -Z-α-bisabolene epoxide. The presence of various bioactive compounds justifies the use of this plant for treating various ailments by traditional practitioners.

Design strategies and applications of nacre-based biomaterials.

PubMed

Gerhard, Ethan Michael; Wang, Wei; Li, Caiyan; Guo, Jinshan; Ozbolat, Ibrahim Tarik; Rahn, Kevin Michael; Armstrong, April Dawn; Xia, Jingfen; Qian, Guoying; Yang, Jian

2017-05-01

The field of tissue engineering and regenerative medicine relies heavily on materials capable of implantation without significant foreign body reactions and with the ability to promote tissue differentiation and regeneration. The field of bone tissue engineering in particular requires materials capable of providing enhanced mechanical properties and promoting osteogenic cell lineage commitment. While bone repair has long relied almost exclusively on inorganic, calcium phosphate ceramics such as hydroxyapatite and their composites or on non-degradable metals, the organically derived shell and pearl nacre generated by mollusks has emerged as a promising alternative. Nacre is a naturally occurring composite material composed of inorganic, calcium carbonate plates connected by a framework of organic molecules. Similar to mammalian bone, the highly organized microstructure of nacre endows the composite with superior mechanical properties while the organic phase contributes to significant bioactivity. Studies, both in vitro and in vivo, have demonstrated nacre's biocompatibility, biodegradability, and osteogenic potential, which are superior to pure inorganic minerals such as hydroxyapatite or non-degradable metals. Nacre can be used directly as a bulk implant or as part of a composite material when combined with polymers or other ceramics. While nacre has demonstrated its effectiveness in multiple cell culture and animal models, it remains a relatively underexplored biomaterial. This review introduces the formation, structure, and characteristics of nacre, and discusses the present and future uses of this biologically-derived material as a novel biomaterial for orthopedic and other tissue engineering applications. Mussel derived nacre, a biological composite composed of mineralized calcium carbonate platelets and interplatelet protein components, has recently gained interest as a potential alternative ceramic material in orthopedic biomaterials, combining the integration and mechanical capabilities of calcium phosphates with increased bioactivity derived from proteins and biomolecules; however, there is limited awareness of this material's potential. Herein, we present, to our knowledge, the first comprehensive review of nacre as a biomaterial. Nacre is a highly promising yet overlooked biomaterial for orthopedic tissue engineering with great potential in a wide variety of material systems. It is our hope that publication of this article will lead to increased community awareness of the potential of nacre as a versatile, bioactive ceramic capable of improving bone tissue regeneration and will elicit increased research effort and innovation utilizing nacre. Copyright © 2017 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

The flavonoid fisetin as an anticancer agent targeting the growth signaling pathways.

PubMed

Rengarajan, Thamaraiselvan; Yaacob, Nik Soriani

2016-10-15

Epidemiological studies show that consumption of diets rich in fruits and vegetables is associated with lower risks of cancer. This evidence has kindled interest into research on bioactive food components and has till date resulted in the identification of many compounds with cancer preventive and therapeutic potential. Among such compounds is fisetin (3,7,3,4-tetrahydroxyflavone), a flavonol that is commonly found in many fruits and vegetables such as apples, persimmons, grapes, kiwis, strawberries, onions and cucumbers. Fisetin has been shown to inhibit or retard the growth of various cancer cells in culture and implanted tumors in vivo. Fisetin targets many components of intracellular signaling pathways including regulators of cell survival and apoptosis, tumor angiogenic and metastatic switches by modulating a distinct set of upstream kinases, transcription factors and their regulators. Current evidence supports the idea that fisetin is a promising agent for cancer treatment. This review summarizes reported anticancer effects of fisetin, and re-emphasizes its potential therapeutic role in the treatment of cancer. Copyright © 2016 Elsevier B.V. All rights reserved.

Food-derived bioactive peptides on inflammation and oxidative stress.

PubMed

Chakrabarti, Subhadeep; Jahandideh, Forough; Wu, Jianping

2014-01-01

Chronic diseases such as atherosclerosis and cancer are now the leading causes of morbidity and mortality worldwide. Inflammatory processes and oxidative stress underlie the pathogenesis of these pathological conditions. Bioactive peptides derived from food proteins have been evaluated for various beneficial effects, including anti-inflammatory and antioxidant properties. In this review, we summarize the roles of various food-derived bioactive peptides in inflammation and oxidative stress and discuss the potential benefits and limitations of using these compounds against the burden of chronic diseases.

Recent Advances in Phospholipids from Colostrum, Milk and Dairy By-Products.

PubMed

Verardo, Vito; Gómez-Caravaca, Ana Maria; Arráez-Román, David; Hettinga, Kasper

2017-01-17

Milk is one of the most important foods for mammals, because it is the first form of feed providing energy, nutrients and immunological factors. In the last few years, milk lipids have attracted the attention of researchers due to the presence of several bioactive components in the lipid fraction. The lipid fraction of milk and dairy products contains several components of nutritional significance, such as ω-3 and ω-6 polyunsaturated fatty acids, CLA, short chain fatty acids, gangliosides and phospholipids. Prospective cohort evidence has shown that phospholipids play an important role in the human diet and reinforce the possible relationship between their consumption and prevention of several chronic diseases. Because of these potential benefits of phospholipids in the human diet, this review is focused on the recent advances in phospholipids from colostrum, milk and dairy by-products. Phospholipid composition, its main determination methods and the health activities of these compounds will be addressed.

Recent Advances in Phospholipids from Colostrum, Milk and Dairy By-Products

PubMed Central

Verardo, Vito; Gómez-Caravaca, Ana Maria; Arráez-Román, David; Hettinga, Kasper

2017-01-01

Milk is one of the most important foods for mammals, because it is the first form of feed providing energy, nutrients and immunological factors. In the last few years, milk lipids have attracted the attention of researchers due to the presence of several bioactive components in the lipid fraction. The lipid fraction of milk and dairy products contains several components of nutritional significance, such as ω-3 and ω-6 polyunsaturated fatty acids, CLA, short chain fatty acids, gangliosides and phospholipids. Prospective cohort evidence has shown that phospholipids play an important role in the human diet and reinforce the possible relationship between their consumption and prevention of several chronic diseases. Because of these potential benefits of phospholipids in the human diet, this review is focused on the recent advances in phospholipids from colostrum, milk and dairy by-products. Phospholipid composition, its main determination methods and the health activities of these compounds will be addressed. PMID:28106745

Neuroprotective and Cognitive Enhancement Potentials of Angelica gigas Nakai Root: A Review

PubMed Central

Sowndhararajan, Kandhasamy; Kim, Songmun

2017-01-01

Angelica gigas Nakai is an important medicinal plant with health promoting properties that is used to treat many disorders. In traditional herbal medicine, the root of this plant is used to promote blood flow, to treat anemia, and is used as sedative or tonic agent. The root contains various bioactive metabolites; in particular, decursin and decursinol (pyranocoumarin type components) have been reported to possess various pharmacological properties. Recently, several in vitro and in vivo studies have reported that the crude extracts and isolated components from the root of A. gigas exhibited neuroprotective and cognitive enhancement effects. Neuronal damage or death is the most important factor for many neurodegenerative diseases. In addition, recent studies have clearly demonstrated the possible mechanisms behind the neuroprotective action of extracts/compounds from the root of A. gigas. In the present review, we summarized the neuroprotective and cognitive enhancement effects of extracts and individual compounds from A. gigas root. PMID:28452965

Neuroprotective and Cognitive Enhancement Potentials of Angelica gigas Nakai Root: A Review.

PubMed

Sowndhararajan, Kandhasamy; Kim, Songmun

2017-04-28

Angelica gigas Nakai is an important medicinal plant with health promoting properties that is used to treat many disorders. In traditional herbal medicine, the root of this plant is used to promote blood flow, to treat anemia, and is used as sedative or tonic agent. The root contains various bioactive metabolites; in particular, decursin and decursinol (pyranocoumarin type components) have been reported to possess various pharmacological properties. Recently, several in vitro and in vivo studies have reported that the crude extracts and isolated components from the root of A. gigas exhibited neuroprotective and cognitive enhancement effects. Neuronal damage or death is the most important factor for many neurodegenerative diseases. In addition, recent studies have clearly demonstrated the possible mechanisms behind the neuroprotective action of extracts/compounds from the root of A. gigas . In the present review, we summarized the neuroprotective and cognitive enhancement effects of extracts and individual compounds from A. gigas root.

Marine snail venoms: use and trends in receptor and channel neuropharmacology.

PubMed

Favreau, Philippe; Stöcklin, Reto

2009-10-01

Venoms are rich mixtures of mainly peptides and proteins evolved by nature to catch and digest preys or for protection against predators. They represent extensive sources of potent and selective bioactive compounds that can lead to original active ingredients, for use as drugs, as pharmacological tools in research and for the biotechnology industry. Among the most fascinating venomous animals, marine snails offer a unique set of pharmacologically active components, targeting a wide diversity of receptors and ion channels. Recent advances still continue to demonstrate their huge neuropharmacological potential. In the quest for interesting pharmacological profiles, researchers face a vast number of venom components to investigate within time and technological constraints. A brief perspective on marine snail venom's complexity and features is given followed by the different discovery strategies and pharmacological approaches, exemplified with some recent developments. These advances will hopefully help further uncovering new pharmacologically important venom molecules.

Stability of Polyphenols Epigallocatechin Gallate and Pentagalloyl Glucose in a Simulated Digestive System

PubMed Central

Krook, Melanie A.; Hagerman, Ann E.

2012-01-01

Polyphenols found in foods and beverages are under intense scrutiny for their potential beneficial effects on human health. We examined the stability of two bioactive polyphenols, epigallocatechin-O-gallate (EGCg) and 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (PGG), in a model digestive system at low oxygen tension with and without added digestive components and foods. Both compounds were stable at pH values of 5–6 and below, indicating gastric stability. Both compounds decomposed at pH 7.0. PGG was stabilized in a model system containing pepsin, pancreatin, bile and lipase, and/or baby food, but was not stabilized by dry cereal. EGCg was not stabilized by the addition of any biomolecule. The effects of polyphenols on human health should be evaluated in the context of their stability in the digestive tract with and without added digestive components and/or food. PMID:23028206

Peptide profiling and the bioactivity character of yogurt in the simulated gastrointestinal digestion.

PubMed

Jin, Yan; Yu, Yang; Qi, Yanxia; Wang, Fangjun; Yan, Jiaze; Zou, Hanfa

2016-06-01

This study investigated the relationship between peptide profiles and the bioactivity character of yogurt in simulated gastrointestinal trials. A total of 250, 434 and 466 peptides were identified by LC-MS/MS analyses of yogurt, gastric digest and pancreatic digest. Forty peptides of yogurt survived in gastrointestinal digestion. κ-CN and β-CN contributed the diversity of peptides during the fermentation process and gastrointestinal digestion, respectively. The favorite of κ-CN by lactic acid bacteria complemented gut digestion by hydrolyzing κ-CN, the low abundance milk proteins. The potential bioactivities were evaluated by in vitro ACE and DPP-IV inhibition assays. The ACE inhibition rate of the pancreatic digests was ~4 - and ~2 - fold greater than that of yogurt and the gastric digests. The ACE inhibitory peptides generated during gastrointestinal digestion improved the ACE inhibitory activity of the gastric and pancreatic digests. The DPP-IV inhibition rate of the pancreatic digest was ~6 - and ~3 - fold greater than that of yogurt and the gastric digest. The numbers of potential DPP-IV inhibitory peptides were positively correlated to the DPP-IV inhibitory activity of the gastric and pancreatic digests. The present study describes the characters and bioactivities of peptides from yogurt in a simulated gastrointestinal digestion. The number of peptides identified from yogurt and gastrointestinal digests by LC-MS/MS increased in the simulated gastrointestinal trials. The in vitro ACE and DPP-IV inhibition bioactivities revealed that the bioactivity of yogurt was enhanced during gastrointestinal digestion. The correlation between peptides and bioactivity in vitro indicated that not only the peptides amount but also the proportion of peptides with high bioactivities contributed to increased bioactivity during gastrointestinal digestion. The study of peptides identified from yogurt and digests revealed that the number of released peptides was not determined by the abundance of the parent proteins but by whether the enzymes favored the protein. In summary, peptide profiling and bioactivities of yogurt in simulated gastrointestinal digestion helped to elucidate the health benefits of yogurt peptides. The results further revealed that pre-digestion of milk by lactic acid bacteria are complementary to generate bioactive peptides and to provide particular yogurt functions. Copyright © 2016 Elsevier B.V. All rights reserved.

Bioactive components and functional properties of biologically activated cereal grains: A bibliographic review.

PubMed

Singh, Arashdeep; Sharma, Savita

2017-09-22

Whole grains provide energy, nutrients, fibers, and bioactive compounds that may synergistically contribute to their protective effects. A wide range of these compounds is affected by germination. While some compounds, such as β-glucans are degraded, others, like antioxidants and total phenolics are increased by means of biological activation of grains. The water and oil absorption capacity as well as emulsion and foaming capacity of biologically activated grains are also improved. Application of biological activation of grains is of emerging interest, which may significantly enhance the nutritional, functional, and bioactive content of grains, as well as improve palatability of grain foods in a natural way. Therefore, biological activation of cereals can be a way to produce food grains enriched with health-promoting compounds and enhanced functional attributes.

It’s a lipid’s world: Bioactive lipid metabolism and signaling in neural stem cell differentiation

PubMed Central

Bieberich, Erhard

2012-01-01

Lipids are often considered membrane components whose function is to embed proteins into cell membranes. In the last two decades, studies on brain lipids have unequivocally demonstrated that many lipids have critical cell signaling functions; they are called “bioactive lipids”. Pioneering work in Dr. Robert Ledeen’s laboratory has shown that two bioactive brain sphingolipids, sphingomyelin and the ganglioside GM1 are major signaling lipids in the nuclear envelope. In addition to derivatives of the sphingolipid ceramide, the bioactive lipids discussed here belong to the classes of terpenoids and steroids, eicosanoids, and lysophospholipids. These lipids act mainly through two mechanisms: 1) direct interaction between the bioactive lipid and a specific protein binding partner such as a lipid receptor, protein kinase or phosphatase, ion exchanger, or other cell signaling protein; and 2) formation of lipid microdomains or rafts that regulate the activity of a group of raft-associated cell signaling proteins. In recent years, a third mechanism has emerged, which invokes lipid second messengers as a regulator for the energy and redox balance of differentiating neural stem cells (NSCs). Interestingly, developmental niches such as the stem cell niche for adult NSC differentiation may also be metabolic compartments that respond to a distinct combination of bioactive lipids. The biological function of these lipids as regulators of NSC differentiation will be reviewed and their application in stem cell therapy discussed. PMID:22246226

An Enzyme-Coated Metal-Organic Framework Shell for Synthetically Adaptive Cell Survival.

PubMed

Liang, Kang; Richardson, Joseph J; Doonan, Christian J; Mulet, Xavier; Ju, Yi; Cui, Jiwei; Caruso, Frank; Falcaro, Paolo

2017-07-10

A bioactive synthetic porous shell was engineered to enable cells to survive in an oligotrophic environment. Eukaryotic cells (yeast) were firstly coated with a β-galactosidase (β-gal), before crystallization of a metal-organic framework (MOF) film on the enzyme coating; thereby producing a bioactive porous synthetic shell. The β-gal was an essential component of the bioactive shell as it generated nutrients (that is, glucose and galactose) required for cell viability in nutrient-deficient media (lactose-based). Additionally, the porous MOF coating carried out other vital functions, such as 1) shielding the cells from cytotoxic compounds and radiation, 2) protecting the non-native enzymes (β-gal in this instance) from degradation and internalization, and 3) allowing for the diffusion of molecules essential for the survival of the cells. Indeed, this bioactive porous shell enabled the survival of cells in simulated extreme oligotrophic environments for more than 7 days, leading to a decrease in cell viability less than 30 %, versus a 99 % decrease for naked yeast. When returned to optimal growth conditions the bioactive porous exoskeleton could be removed and the cells regained full growth immediately. The construction of bioactive coatings represents a conceptually new and promising approach for the next-generation of cell-based research and application, and is an alternative to synthetic biology or genetic modification. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Bioactive peptides from meat muscle and by-products: generation, functionality and application as functional ingredients.

PubMed

Lafarga, Tomas; Hayes, Maria

2014-10-01

Bioactive peptides are sequences of between 2-30 amino acids in length that impart a positive health effect to the consumer when ingested. They have been identified from a range of foods, including milk and muscle sources including beef, chicken, pork and marine muscles. The myriad of peptides identified from these sources have known antihypertensive, opioid, antioxidant, antithrombotic and other bioactivities. Indeed, bioactive peptides could play a role in the prevention of diseases associated with the development of metabolic syndrome and mental health diseases. The aim of this work is to present an overview of the bioactive peptides identified in muscle proteins and by-products generated during the processing of meat. The paper looks at the isolation, enrichment and characterisation strategies that have been employed to date to generate bioactive peptides and the potential future applications of these peptides in functional foods for the prevention of heart and mental health problems and obesity. Copyright © 2014 Elsevier Ltd. All rights reserved.

Nanomaterial (NM) bioactivity profiling by ToxCast high-throughput screening (HTS)

EPA Science Inventory

Rapidly increasing numbers of new NMs and their uses demand efficient tests of NM bioactivity for safety assessment. The EPA’s ToxCast program uses HTS assays to prioritize for targeted testing, identify biological pathways affected, and aid in linking NM properties and potential...

Enzymatic Hydrolysis of Peanut Flour Produces Bioactive Peptides with Reduced Allergenicity

USDA-ARS?s Scientific Manuscript database

Peanut allergy is one of the most severe food allergies due to its life-threatening nature and persistency. Current immunotherapy methods, though effective, are often accompanied by allergic side-effects. Enzymatic hydrolysis of peanut flour has the potential to produce bioactive peptides with impro...

Production and bioactivity of pectic oligosaccharides from fruit and vegetable biomass

USDA-ARS?s Scientific Manuscript database

Pectin is abundant in various agro-industrial bio-resources such as citrus peel, apple pomace, cranberry pulp and sugar beet pulp. These materials can therefore be considered as a source of potential bioactive pectic oligosaccharides. This chapter reviews the various extraction and purification meth...

Functional food productions: release the potential of bioactive compounds through food processing

USDA-ARS?s Scientific Manuscript database

Epidemiological studies of bioactive compounds from plant-based foods have consistently pointed to undisputed benefits of consumption of plant-based foods on human health particularly regarding cardiovascular diseases and cancers. However, in order to attain the dosage required from these studies, p...

Bioactive Components in Moringa Oleifera Leaves Protect against Chronic Disease

PubMed Central

Vergara-Jimenez, Marcela; Almatrafi, Manal Mused

2017-01-01

Moringa Oleifera (MO), a plant from the family Moringacea is a major crop in Asia and Africa. MO has been studied for its health properties, attributed to the numerous bioactive components, including vitamins, phenolic acids, flavonoids, isothiocyanates, tannins and saponins, which are present in significant amounts in various components of the plant. Moringa Oleifera leaves are the most widely studied and they have shown to be beneficial in several chronic conditions, including hypercholesterolemia, high blood pressure, diabetes, insulin resistance, non-alcoholic liver disease, cancer and overall inflammation. In this review, we present information on the beneficial results that have been reported on the prevention and alleviation of these chronic conditions in various animal models and in cell studies. The existing limited information on human studies and Moringa Oleifera leaves is also presented. Overall, it has been well documented that Moringa Oleifera leaves are a good strategic for various conditions associated with heart disease, diabetes, cancer and fatty liver. PMID:29144438

The secret to a successful relationship: lasting chemistry between ascidians and their symbiotic bacteria

PubMed Central

Schmidt, Eric W.

2014-01-01

Bioactive secondary metabolites are common components of marine animals. In many cases, symbiotic bacteria, and not the animals themselves, synthesize the compounds. Among marine animals, ascidians are good models for understanding these symbioses. Ascidians often contain potently bioactive secondary metabolites as their major extractable components. Strong evidence shows that ~8% of the known secondary metabolites from ascidians are made by symbiotic bacteria, and indirect evidence implicates bacteria in the synthesis of many more. Far from being “secondary” to the animals, secondary metabolites are essential components of the interaction between host animals and their symbiotic bacteria. These interactions have complex underlying biology, but the chemistry is clearly ascidian-species specific. The chemical interactions are ancient in at least some cases, and they are widespread among ascidians. Ascidians maintain secondary metabolic symbioses with bacteria that are phylogenetically diverse, indicating a convergent solution to obtaining secondary metabolites and reinforcing the importance of secondary metabolism in animal survival. PMID:25937788

Current progress in isolation and characterization of toxins isolated from Pfiesteria piscicida.

PubMed Central

Moeller, P D; Morton, S L; Mitchell, B A; Sivertsen, S K; Fairey, E R; Mikulski, T M; Glasgow, H; Deamer-Melia, N J; Burkholder, J M; Ramsdell, J S

2001-01-01

The isolation and partial purification of toxic substances derived from Pfiesteria piscicida Steidinger & Burkholder extracts is described. Four distinct bioassay systems were used to monitor bioactivity of the P. piscicida extracts, including a high throughput cell cytotoxicity assay and a reporter gene assay as well as assays using brine shrimp and fish. Using these bioassays to guide fractionation, we have isolated two distinct, active fractions from Pfiesteria culture medium and cell mass extracts on the basis of their solubility characteristics. We have identified and characterized a bioactive lipophilic substance from Pfiesteria-derived extracts as di(2-ethylhexyl)phthalate, a commonly used plasticizer. The source of this typically man-made substance has been identified as originating from Instant Ocean (Aquarium Systems, Mentor, OH, USA), a commercially available seawater salt mixture used to prepare our mass culture growth medium. We have developed chromatographic methodology to isolate a bioactive polar compound isolated from extracts of Pfiesteria culture and presently report the characterization of the activity of this substance. The molecular structural analysis of the polar active component(s) using mass spectrometry and nuclear magnetic resonance spectroscopy is currently under way. PMID:11677183

GC-MS analysis of bio-active compounds in methanolic extract of Lactuca runcinata DC

PubMed Central

Kanthal, Lakshmi Kanta; Dey, Akalanka; Satyavathi, K.; Bhojaraju, P.

2014-01-01

Background: The presence of phytochemical constitutes has been reported from species of the Compositae (Asteraceae). Hitherto no reports exist on the phytochemical components and biological activity of Lactuca runcinata DC. Objective: The present study was designed to determine the bioactive compounds in the whole plant methanol extract of Lactuca runcinata. Materials and Methods: Phytochemical screening of the entire herb of Lactuca runcinata DC revealed the presence of some bio-active components. Gas chromatography-mass spectrometry (GC-MS) analysis of the whole plant methanol extract of Lactuca runcinata was performed on a GC-MS equipment (Thermo Scientific Co.) Thermo GC-TRACE ultra ver.: 5.0, Thermo MS DSQ II. Results: The phytochemical tests showed the presence of alkaloids, cardiac glycosides, flavonoids, phenols, phlobatannin, reducing sugars, saponins, steroids, tannins, terpenoids, volatile oils, carbohydrates, and protein/amino acids in methanolic extract of L. runcinata. The GC-MS analysis has shown the presence of different phytochemical compounds in the methanolic extract of Lactuca runcinata. A total of 21 compounds were identified representing 84.49% of total methanolic extract composition. Conclusion: From the results, it is evident that Lactuca runcinata contains various phytocomponents and is recommended as a plant of phytopharmaceutical importance. PMID:24497744

eBASIS (Bioactive Substances in Food Information Systems) and Bioactive Intakes: Major Updates of the Bioactive Compound Composition and Beneficial Bioeffects Database and the Development of a Probabilistic Model to Assess Intakes in Europe.

PubMed

Plumb, Jenny; Pigat, Sandrine; Bompola, Foteini; Cushen, Maeve; Pinchen, Hannah; Nørby, Eric; Astley, Siân; Lyons, Jacqueline; Kiely, Mairead; Finglas, Paul

2017-03-23

eBASIS (Bioactive Substances in Food Information Systems), a web-based database that contains compositional and biological effects data for bioactive compounds of plant origin, has been updated with new data on fruits and vegetables, wheat and, due to some evidence of potential beneficial effects, extended to include meat bioactives. eBASIS remains one of only a handful of comprehensive and searchable databases, with up-to-date coherent and validated scientific information on the composition of food bioactives and their putative health benefits. The database has a user-friendly, efficient, and flexible interface facilitating use by both the scientific community and food industry. Overall, eBASIS contains data for 267 foods, covering the composition of 794 bioactive compounds, from 1147 quality-evaluated peer-reviewed publications, together with information from 567 publications describing beneficial bioeffect studies carried out in humans. This paper highlights recent updates and expansion of eBASIS and the newly-developed link to a probabilistic intake model, allowing exposure assessment of dietary bioactive compounds to be estimated and modelled in human populations when used in conjunction with national food consumption data. This new tool could assist small- and medium-sized enterprises (SMEs) in the development of food product health claim dossiers for submission to the European Food Safety Authority (EFSA).

Pomegranate extracts and cancer prevention: molecular and cellular activities.

PubMed

Syed, Deeba N; Chamcheu, Jean-Christopher; Adhami, Vaqar M; Mukhtar, Hasan

2013-10-01

There is increased appreciation by the scientific community that dietary phytochemicals can be potential weapons in the fight against cancer. Emerging data has provided new insights into the molecular and cellular framework needed to establish novel mechanism-based strategies for cancer prevention by selective bioactive food components. The unique chemical composition of the pomegranate fruit, rich in antioxidant tannins and flavonoids has drawn the attention of many investigators. Polyphenol rich fractions derived from the pomegranate fruit have been studied for their potential chemopreventive and/or cancer therapeutic effects in several animal models. Although data from in vitro and in vivo studies look convincing, well designed clinical trials in humans are needed to ascertain whether pomegranate can become part of our armamentarium against cancer. This review summarizes the available literature on the effects of pomegranate against various cancers.

Pomegranate Extracts and Cancer Prevention: Molecular and Cellular Activities

PubMed Central

Syed, Deeba N.; Chamcheu, Jean-Christopher; Adhami, Vaqar M.; Mukhtar, Hasan

2014-01-01

There is increased appreciation by the scientific community that dietary phytochemicals can be potential weapons in the fight against cancer. Emerging data has provided new insights into the molecular and cellular framework needed to establish novel mechanism-based strategies for cancer prevention by selective bioactive food components. The unique chemical composition of the pomegranate fruit, rich in antioxidant tannins and flavonoids has drawn the attention of many investigators. Polyphenol rich fractions derived from the pomegranate fruit have been studied for their potential chemopreventive and/or cancer therapeutic effects in several animal models. Although data from in vitro and in vivo studies look convincing, well designed clinical trials in humans are needed to ascertain whether pomegranate can become part of our armamentarium against cancer. This review summarizes the available literature on the effects of pomegranate against various cancers. PMID:23094914

Bioassays for Evaluating Water Quality: Screening for total bioactivity to assess water safety

EPA Science Inventory

Bioassays are a potential solution for assessing complex samples since they screen for total bioactivity for a given pathway or mode of action (MOA), such as estrogen receptor activation, in the samples. Overall, they can account for the three challenges listed above, and can sim...

Optimization of liquid culture conditions of Philippine wild edible mushrooms as potential source of bioactive lipids

USDA-ARS?s Scientific Manuscript database

With remarkable bioactivities and delightful taste, mushrooms have been a commercial nutraceutical around the world. Mushrooms are cultivated on solid materials. Here we report the successful cultivation of four Philippine edible mushrooms in liquid medium. This work highlights the optimal liquid cu...

Potential anticancer properties of bioactive compounds of Gymnema sylvestre and its biofunctionalized silver nanoparticles.

PubMed

Arunachalam, Kantha Deivi; Arun, Lilly Baptista; Annamalai, Sathesh Kumar; Arunachalam, Aarrthy M

2015-01-01

Gymnema sylvestre is an ethno-pharmacologically important medicinal plant used in many polyherbal formulations for its potential health benefits. Silver nanoparticles (SNPs) were biofunctionalized using aqueous leaf extracts of G. sylvestre. The anticancer properties of the bioactive compounds and the biofunctionalized SNPs were compared using the HT29 human adenoma colon cancer cell line. The preliminary phytochemical screening for bioactive compounds from aqueous extracts revealed the presence of alkaloids, triterpenes, flavonoids, steroids, and saponins. Biofunctionalized SNPs were synthesized using silver nitrate and characterized by ultraviolet-visible spectroscopy, scanning electron microscopy, energy-dispersive X-ray analysis, Fourier transform infrared spectroscopy, and X-ray diffraction for size and shape. The characterized biofunctionalized G. sylvestre were tested for its in vitro anticancer activity against HT29 human colon adenocarcinoma cells. The biofunctionlized G. sylvestre SNPs showed the surface plasmon resonance band at 430 nm. The scanning electron microscopy images showed the presence of spherical nanoparticles of various sizes, which were further determined using the Scherrer equation. In vitro cytotoxic activity of the biofunctionalized green-synthesized SNPs (GSNPs) indicated that the sensitivity of HT29 human colon adenocarcinoma cells for cytotoxic drugs is higher than that of Vero cell line for the same cytotoxic agents and also higher than the bioactive compound of the aqueous extract. Our results show that the anticancer properties of the bioactive compounds of G. sylvestre can be enhanced through biofunctionalizing the SNPs using the bioactive compounds present in the plant extract without compromising their medicinal properties.

Osteogenic differentiation of 3D cultured mesenchymal stem cells induced by bioactive peptides.

PubMed

Lukasova, Vera; Buzgo, Matej; Sovkova, Vera; Dankova, Jana; Rampichova, Michala; Amler, Evzen

2017-08-01

Bioactive peptides derived from receptor binding motifs of native proteins are a potent source of bioactive molecules that can induce signalling pathways. These peptides could substitute for osteogenesis promoting supplements. The work presented here compares three kinds of bioactive peptides derived from collagen III, bone morphogenetic protein 7 (BMP-7) and BMP-2 with their potential osteogenic activity on the model of porcine mesenchymal stem cells (pMSCs). pMSCs were cultured on electrospun polycaprolactone nanofibrous scaffolds with different concentrations of the bioactive peptides without addition of any osteogenic supplement. Analysis of pMSCs cultures included measurement of the metabolic activity and proliferation, immunofluorescence staining and also qPCR. Results showed no detrimental effect of the bioactive peptides to cultured pMSCs. Based on qPCR analysis, the bioactive peptides are specific for osteogenic differentiation with no detectable expression of collagen II. Our results further indicate that peptide derived from BMP-2 protein promoted the expression of mRNA for osteocalcin (OCN) and collagen I significantly compared to control groups and also supported deposition of OCN as observed by immunostaining method. The data suggest that bioactive peptide with an amino acid sequence of KIPKASSVPTELSAISTLYL derived from BMP-2 protein was the most potent for triggering osteogenic differentiation of pMSCs. © 2017 John Wiley & Sons Ltd.

Sloth hair as a novel source of fungi with potent anti-parasitic, anti-cancer and anti-bacterial bioactivity.

PubMed

Higginbotham, Sarah; Wong, Weng Ruh; Linington, Roger G; Spadafora, Carmenza; Iturrado, Liliana; Arnold, A Elizabeth

2014-01-01

The extraordinary biological diversity of tropical forests harbors a rich chemical diversity with enormous potential as a source of novel bioactive compounds. Of particular interest are new environments for microbial discovery. Sloths--arboreal mammals commonly found in the lowland forests of Panama--carry a wide variety of micro- and macro-organisms on their coarse outer hair. Here we report for the first time the isolation of diverse and bioactive strains of fungi from sloth hair, and their taxonomic placement. Eighty-four isolates of fungi were obtained in culture from the surface of hair that was collected from living three-toed sloths (Bradypus variegatus, Bradypodidae) in Soberanía National Park, Republic of Panama. Phylogenetic analyses revealed a diverse group of Ascomycota belonging to 28 distinct operational taxonomic units (OTUs), several of which are divergent from previously known taxa. Seventy-four isolates were cultivated in liquid broth and crude extracts were tested for bioactivity in vitro. We found a broad range of activities against strains of the parasites that cause malaria (Plasmodium falciparum) and Chagas disease (Trypanosoma cruzi), and against the human breast cancer cell line MCF-7. Fifty fungal extracts were tested for antibacterial activity in a new antibiotic profile screen called BioMAP; of these, 20 were active against at least one bacterial strain, and one had an unusual pattern of bioactivity against Gram-negative bacteria that suggests a potentially new mode of action. Together our results reveal the importance of exploring novel environments for bioactive fungi, and demonstrate for the first time the taxonomic composition and bioactivity of fungi from sloth hair.

Sloth Hair as a Novel Source of Fungi with Potent Anti-Parasitic, Anti-Cancer and Anti-Bacterial Bioactivity

PubMed Central

Higginbotham, Sarah; Wong, Weng Ruh; Linington, Roger G.; Spadafora, Carmenza; Iturrado, Liliana; Arnold, A. Elizabeth

2014-01-01

The extraordinary biological diversity of tropical forests harbors a rich chemical diversity with enormous potential as a source of novel bioactive compounds. Of particular interest are new environments for microbial discovery. Sloths – arboreal mammals commonly found in the lowland forests of Panama – carry a wide variety of micro- and macro-organisms on their coarse outer hair. Here we report for the first time the isolation of diverse and bioactive strains of fungi from sloth hair, and their taxonomic placement. Eighty-four isolates of fungi were obtained in culture from the surface of hair that was collected from living three-toed sloths (Bradypus variegatus, Bradypodidae) in Soberanía National Park, Republic of Panama. Phylogenetic analyses revealed a diverse group of Ascomycota belonging to 28 distinct operational taxonomic units (OTUs), several of which are divergent from previously known taxa. Seventy-four isolates were cultivated in liquid broth and crude extracts were tested for bioactivity in vitro. We found a broad range of activities against strains of the parasites that cause malaria (Plasmodium falciparum) and Chagas disease (Trypanosoma cruzi), and against the human breast cancer cell line MCF-7. Fifty fungal extracts were tested for antibacterial activity in a new antibiotic profile screen called BioMAP; of these, 20 were active against at least one bacterial strain, and one had an unusual pattern of bioactivity against Gram-negative bacteria that suggests a potentially new mode of action. Together our results reveal the importance of exploring novel environments for bioactive fungi, and demonstrate for the first time the taxonomic composition and bioactivity of fungi from sloth hair. PMID:24454729

The action of neutrophil serine proteases on elastin and its precursor.

PubMed

Heinz, Andrea; Jung, Michael C; Jahreis, Günther; Rusciani, Anthony; Duca, Laurent; Debelle, Laurent; Weiss, Anthony S; Neubert, Reinhard H H; Schmelzer, Christian E H

2012-01-01

This study aimed to investigate the degradation of the natural substrates tropoelastin and elastin by the neutrophil-derived serine proteases human leukocyte elastase (HLE), proteinase 3 (PR3) and cathepsin G (CG). Focus was placed on determining their cleavage site specificities using mass spectrometric techniques. Moreover, the release of bioactive peptides from elastin by the three proteases was studied. Tropoelastin was comprehensively degraded by all three proteases, whereas less cleavage occurred in mature cross-linked elastin. An analysis of the cleavage site specificities of the three proteases in tropoelastin and elastin revealed that HLE and PR3 similarly tolerate hydrophobic and/or aliphatic amino acids such as Ala, Gly and Val at P(1), which are also preferred by CG. In addition, CG prefers the bulky hydrophobic amino acid Leu and accepts the bulky aromatic amino acids Phe and Tyr. CG shows a strong preference for the charged amino acid Lys at P(1) in tropoelastin, whereas Lys was not identified at P(1) in CG digests of elastin due to extensive cross-linking at Lys residues in mature elastin. All three serine proteases showed a clear preference for Pro at P(2) and P(4)'. With respect to the liberation of potentially bioactive peptides from elastin, the study revealed that all three serine proteases have a similar ability to release bioactive sequences, with CG producing the highest number of these peptides. In bioactivity studies, potentially bioactive peptides that have not been investigated on their bioactivity to date, were tested. Three new bioactive GxxPG motifs were identified; GVYPG, GFGPG and GVLPG. Copyright © 2011 Elsevier Masson SAS. All rights reserved.

Present and future potential of plant-derived products to control arthropods of veterinary and medical significance

PubMed Central

2014-01-01

The use of synthetic pesticides and repellents to target pests of veterinary and medical significance is becoming increasingly problematic. One alternative approach employs the bioactive attributes of plant-derived products (PDPs). These are particularly attractive on the grounds of low mammalian toxicity, short environmental persistence and complex chemistries that should limit development of pest resistance against them. Several pesticides and repellents based on PDPs are already available, and in some cases widely utilised, in modern pest management. Many more have a long history of traditional use in poorer areas of the globe where access to synthetic pesticides is often limited. Preliminary studies support that PDPs could be more widely used to target numerous medical and veterinary pests, with modes of action often specific to invertebrates. Though their current and future potential appears significant, development and deployment of PDPs to target veterinary and medical pests is not without issue. Variable efficacy is widely recognised as a restraint to PDPs for pest control. Identifying and developing natural bioactive PDP components in place of chemically less-stable raw or 'whole’ products seems to be the most popular solution to this problem. A limited residual activity, often due to photosensitivity or high volatility, is a further drawback in some cases (though potentially advantageous in others). Nevertheless, encapsulation technologies and other slow-release mechanisms offer strong potential to improve residual activity where needed. The current review provides a summary of existing use and future potential of PDPs against ectoparasites of veterinary and medical significance. Four main types of PDP are considered (pyrethrum, neem, essential oils and plant extracts) for their pesticidal, growth regulating and repellent or deterrent properties. An overview of existing use and research for each is provided, with direction to more extensive reviews given in many sections. Sections to highlight potential issues, modes of action and emerging and future potential are also included. PMID:24428899

Bioactive Secondary Metabolites Produced by the Fungal Endophytes of Conifers.

PubMed

Stierle, Andrea A; Stierle, Donald B

2015-10-01

This is a review of bioactive secondary metabolites isolated from conifer-associated endophytic fungi from 1990-2014. This includes compounds with antimicrobial, anti-inflammatory, anti-proliferative and cytotoxic activity towards human cancer cell lines, and activity against either plant pathogens or plant insect pests. Compounds that were originally reported without associated activity were included if other studies ascribed activity to these compounds. Compounds were not included if they were exclusively phytotoxic or if they were isolated from active extracts but were not determined to be the active component of that extract.

Grapes (Vitis vinifera) as a Potential Candidate for the Therapy of the Metabolic Syndrome.

PubMed

Akaberi, Maryam; Hosseinzadeh, Hosein

2016-04-01

Metabolic syndrome is associated with several disorders, including hypertension, diabetes, hyperlipidemia as well as cardiovascular diseases and stroke. Plant-derived polyphenols, compounds found in numerous plant species, play an important role as potential treatments for components of metabolic syndrome. Studies have provided evidence for protective effects of various polyphenol-rich foods against metabolic syndrome. Fruits, vegetables, cereals, nuts, and berries are rich in polyphenolic compounds. Grapes (Vitis vinifera), especially grape seeds, stand out as rich sources of polyphenol potent antioxidants and have been reported helpful for inhibiting the risk factors involved in the metabolic syndrome such as hyperlipidemia, hyperglycemia, and hypertension. There are also many studies about gastroprotective, hepatoprotective, and anti-obesity effects of grape polyphenolic compounds especially proanthocyanidins in the literature. The present study investigates the protective effects of grape seeds in metabolic syndrome. The results of this study show that grape polyphenols have significant effects on the level of blood glucose, lipid profile, blood pressure, as well as beneficial activities in liver and heart with various mechanisms. In addition, the pharmacokinetics of grape polyphenols is discussed. More detailed mechanistic investigations and phytochemical studies for finding the exact bioactive component(s) and molecular signaling pathways are suggested. Copyright © 2016 John Wiley & Sons, Ltd.

In Vitro Wound Healing Potential and Identification of Bioactive Compounds from Moringa oleifera Lam

PubMed Central

Muhammad, Abubakar Amali; Pauzi, Nur Aimi Syarina; Arulselvan, Palanisamy; Abas, Faridah; Fakurazi, Sharida

2013-01-01

Moringa oleifera Lam. (M. oleifera) from the monogeneric family Moringaceae is found in tropical and subtropical countries. The present study was aimed at exploring the in vitro wound healing potential of M. oleifera and identification of active compounds that may be responsible for its wound healing action. The study included cell viability, proliferation, and wound scratch test assays. Different solvent crude extracts were screened, and the most active crude extract was further subjected to differential bioguided fractionation. Fractions were also screened and most active aqueous fraction was finally obtained for further investigation. HPLC and LC-MS/MS analysis were used for identification and confirmation of bioactive compounds. The results of our study demonstrated that aqueous fraction of M. oleifera significantly enhanced proliferation and viability as well as migration of human dermal fibroblast (HDF) cells compared to the untreated control and other fractions. The HPLC and LC-MS/MS studies revealed kaempferol and quercetin compounds in the crude methanolic extract and a major bioactive compound Vicenin-2 was identified in the bioactive aqueous fraction which was confirmed with standard Vicenin-2 using HPLC and UV spectroscopic methods. These findings suggest that bioactive fraction of M. oleifera containing Vicenin-2 compound may enhance faster wound healing in vitro. PMID:24490175

Tomato as a Source of Carotenoids and Polyphenols Targeted to Cancer Prevention

PubMed Central

Martí, Raúl; Roselló, Salvador; Cebolla-Cornejo, Jaime

2016-01-01

A diet rich in vegetables has been associated with a reduced risk of many diseases related to aging and modern lifestyle. Over the past several decades, many researches have pointed out the direct relation between the intake of bioactive compounds present in tomato and a reduced risk of suffering different types of cancer. These bioactive constituents comprise phytochemicals such as carotenoids and polyphenols. The direct intake of these chemoprotective molecules seems to show higher efficiencies when they are ingested in its natural biological matrix than when they are ingested isolated or in dietary supplements. Consequently, there is a growing trend for improvement of the contents of these bioactive compounds in foods. The control of growing environment and processing conditions can ensure the maximum potential accumulation or moderate the loss of bioactive compounds, but the best results are obtained developing new varieties via plant breeding. The modification of single steps of metabolic pathways or their regulation via conventional breeding or genetic engineering has offered excellent results in crops such as tomato. In this review, we analyse the potential of tomato as source of the bioactive constituents with cancer-preventive properties and the result of modern breeding programs as a strategy to increase the levels of these compounds in the diet. PMID:27331820

Cinnamaldehyde, Cinnamic Acid, and Cinnamyl Alcohol, the Bioactives of Cinnamomum cassia Exhibit HDAC8 Inhibitory Activity: An In vitro and In silico Study

PubMed Central

Patil, Mangesh; Choudhari, Amit S.; Pandita, Savita; Islam, Md Ataul; Raina, Prerna; Kaul-Ghanekar, Ruchika

2017-01-01

Background: The altered expression of histone deacetylase family member 8 (HDAC8) has been found to be linked with various cancers, thereby making its selective inhibition a potential strategy in cancer therapy. Recently, plant secondary metabolites, particularly phenolic compounds, have been shown to possess HDAC inhibitory activity. Objective: In the present work, we have evaluated the potential of cinnamaldehyde (CAL), cinnamic acid (CA), and cinnamyl alcohol (CALC) (bioactives of Cinnamomum) as well as aqueous cinnamon extract (ACE), to inhibit HDAC8 activity in vitro and in silico. Materials and Methods: HDAC8 inhibitory activity of ACE and cinnamon bioactives was determined in vitro using HDAC8 inhibitor screening kit. Trichostatin A (TSA), a well-known anti-cancer agent and HDAC inhibitor, was used as a positive control. In silico studies included molecular descriptor Analysis molecular docking absorption, distribution, metabolism, excretion, and toxicity prediction, density function theory calculation and synthetic accessibility program. Results: Pharmacoinformatics studies implicated that ACE and its Bioactives (CAL, CA, and CALC) exhibited comparable activity with that of TSA. The highest occupied molecular orbitals and lowest unoccupied molecular orbitals along with binding energy of cinnamon bioactives were comparable with that of TSA. Molecular docking results suggested that all the ligands maintained two hydrogen bond interactions within the active site of HDAC8. Finally, the synthetic accessibility values showed that cinnamon bioactives were easy to synthesize compared to TSA. Conclusion: It was evident from both the experimental and computational data that cinnamon bioactives exhibited significant HDAC8 inhibitory activity, thereby suggesting their potential therapeutic implications against cancer. SUMMARY Pharmacoinformatics studies revealed that cinnamon bioactives bound to the active site of HDAC8 enzyme in a way similar to that of TSAThe molecular descriptors of cinnamon compounds successfully correlated with TSA values. The binding interactions and energies were also found to be close to TSASynthetic accessibility values showed that cinnamon bioactives were easy to synthesize compared to TSA. Abbreviations used: ACE: Aqueous Cinnamon Extract; DFT: Density Function Theory; CAL: Cinnamaldehyde; CA: Cinnamic Acid; CALC: Cinnamyl Alcohol; MW: Molecular Weight; ROTBs: Rotatable Bonds; ROF: Lipinski's Rule of Five; TSA: Trichostatin A; PDB: Protein Data Bank; RMSD: Root Mean Square Deviation; HBA: Hydrogen Bond Acceptor; HBD: Hydrogen Bond Donor; ADMET: Absorption, Distribution, Metabolism, Excretion and Toxicity; FO: Frontier Orbital; HOMOs: Highest Occupied Molecular Orbitals; LUMOs: Lowest Unoccupied Molecular Orbitals; BE: Binding Energy. PMID:29142427

Comparative and quantitative analysis of antioxidant and scavenging potential of Indigofera tinctoria Linn. extracts.

PubMed

Singh, Rashmi; Sharma, Shatruhan; Sharma, Veena

2015-07-01

To compare and elucidate the antioxidant efficacy of ethanolic and hydroethanolic extracts of Indigofera tinctoria Linn. (Fabaceae family). Various in-vitro antioxidant assays and free radical-scavenging assays were done. Quantitative measurements of various phytoconstituents, reductive abilities and chelating potential were carried out along with standard compounds. Half inhibitory concentration (IC50) values for ethanol and hydroethanol extracts were analyzed and compared with respective standards. Hydroethanolic extracts showed considerably more potent antioxidant activity in comparison to ethanol extracts. Hydroethanolic extracts had lower IC50 values than ethanol extracts in the case of DPPH, metal chelation and hydroxyl radical-scavenging capacity (829, 659 and 26.7 μg/mL) but had slightly higher values than ethanol in case of SO2- and NO2-scavenging activity (P<0.001 vs standard). Quantitative measurements also showed that the abundance of phenolic and flavonoid bioactive phytoconstituents were significantly (P<0.001) greater in hydroethanol extracts (212.920 and 149.770 mg GAE and rutin/g of plant extract respectively) than in ethanol extracts (211.691 and 132.603 mg GAE and rutin/g of plant extract respectively). Karl Pearson's correlation analysis (r2) between various antioxidant parameters and bioactive components also associated the antioxidant potential of I. tinctoria with various phytoconstituents, especially phenolics, flavonoids, saponins and tannins. This study may be helpful to draw the attention of researchers towards the hydroethanol extracts of I. tinctoria, which has a high yield, and great prospects in herbal industries to produce inexpensive and powerful herbal products.

Cyanobactins from Cyanobacteria: Current Genetic and Chemical State of Knowledge.

PubMed

Martins, Joana; Vasconcelos, Vitor

2015-11-13

Cyanobacteria are considered to be one of the most promising sources of new, natural products. Apart from non-ribosomal peptides and polyketides, ribosomally synthesized and post-translationally modified peptides (RiPPs) are one of the leading groups of bioactive compounds produced by cyanobacteria. Among these, cyanobactins have sparked attention due to their interesting bioactivities and for their potential to be prospective candidates in the development of drugs. It is assumed that the primary source of cyanobactins is cyanobacteria, although these compounds have also been isolated from marine animals such as ascidians, sponges and mollusks. The aim of this review is to update the current knowledge of cyanobactins, recognized as being produced by cyanobacteria, and to emphasize their genetic clusters and chemical structures as well as their bioactivities, ecological roles and biotechnological potential.

Marine-Based Nutraceuticals: An Innovative Trend in the Food and Supplement Industries.

PubMed

Suleria, Hafiz Ansar Rasul; Osborne, Simone; Masci, Paul; Gobe, Glenda

2015-10-14

Recent trends in functional foods and supplements have demonstrated that bioactive molecules play a major therapeutic role in human disease. Nutritionists and biomedical and food scientists are working together to discover new bioactive molecules that have increased potency and therapeutic benefits. Marine life constitutes almost 80% of the world biota with thousands of bioactive compounds and secondary metabolites derived from marine invertebrates such as tunicates, sponges, molluscs, bryozoans, sea slugs and many other marine organisms. These bioactive molecules and secondary metabolites possess antibiotic, antiparasitic, antiviral, anti-inflammatory, antifibrotic and anticancer activities. They are also inhibitors or activators of critical enzymes and transcription factors, competitors of transporters and sequestrants that modulate various physiological pathways. The current review summaries the widely available marine-based nutraceuticals and recent research carried out for the purposes of isolation, identification and characterization of marine-derived bioactive compounds with various therapeutic potentials.

Marine-Based Nutraceuticals: An Innovative Trend in the Food and Supplement Industries

PubMed Central

Suleria, Hafiz Ansar Rasul; Osborne, Simone; Masci, Paul; Gobe, Glenda

2015-01-01

Recent trends in functional foods and supplements have demonstrated that bioactive molecules play a major therapeutic role in human disease. Nutritionists and biomedical and food scientists are working together to discover new bioactive molecules that have increased potency and therapeutic benefits. Marine life constitutes almost 80% of the world biota with thousands of bioactive compounds and secondary metabolites derived from marine invertebrates such as tunicates, sponges, molluscs, bryozoans, sea slugs and many other marine organisms. These bioactive molecules and secondary metabolites possess antibiotic, antiparasitic, antiviral, anti-inflammatory, antifibrotic and anticancer activities. They are also inhibitors or activators of critical enzymes and transcription factors, competitors of transporters and sequestrants that modulate various physiological pathways. The current review summaries the widely available marine-based nutraceuticals and recent research carried out for the purposes of isolation, identification and characterization of marine-derived bioactive compounds with various therapeutic potentials. PMID:26473889

Cnidarians as a Source of New Marine Bioactive Compounds—An Overview of the Last Decade and Future Steps for Bioprospecting

PubMed Central

Rocha, Joana; Peixe, Luisa; Gomes, Newton C.M.; Calado, Ricardo

2011-01-01

Marine invertebrates are rich sources of bioactive compounds and their biotechnological potential attracts scientific and economic interest worldwide. Although sponges are the foremost providers of marine bioactive compounds, cnidarians are also being studied with promising results. This diverse group of marine invertebrates includes over 11,000 species, 7500 of them belonging to the class Anthozoa. We present an overview of some of the most promising marine bioactive compounds from a therapeutic point of view isolated from cnidarians in the first decade of the 21st century. Anthozoan orders Alcyonacea and Gorgonacea exhibit by far the highest number of species yielding promising compounds. Antitumor activity has been the major area of interest in the screening of cnidarian compounds, the most promising ones being terpenoids (monoterpenoids, diterpenoids, sesquiterpenoids). We also discuss the future of bioprospecting for new marine bioactive compounds produced by cnidarians. PMID:22073000

Layered titanates with fibrous nanotopographic features as reservoir for bioactive ions to enhance osteogenesis

NASA Astrophysics Data System (ADS)

Song, Xiaoxia; Tang, Wei; Gregurec, Danijela; Yate, Luis; Moya, Sergio Enrique; Wang, Guocheng

2018-04-01

In this study, an osteogenic environment was constructed on Ti alloy implants by in-situ formation of nanosized fibrous titanate, Na2Ti6O13, loaded with bioactive ions, i.e. Sr, Mg and Zn, to enhance surface bioactivity. The bioactive ions were loaded by ion exchange with sodium located at inter-layer positions between the TiO6 slabs, and their release was not associated with the degradation of the structural unit of the titanate. In-vitro cell culture experiments using MC3T3-E1 cells proved that both bioactive ions and nanotopographic features are critical in promoting osteogenic differentiation of the cells. It was found that the osteogenic functions of the titanate can be modulated by the type and amount of ions incorporated. This study points out that nanosized fibrous titanate formed on the Ti alloy can be a promising reservoir for bioactive ions. The major advantage of this approach over other alternatives for bioactive ion delivery using degradable bioceramic coatings is its capacity of maintaining the structural integrity of the coating and thus avoiding structural deterioration and potential mechanical failure.

Biomaterial compounds and bioactivity of horseshoe crab Carsinoscorpius rotundicauda biomass harvested from the Madura Strait

NASA Astrophysics Data System (ADS)

Asih, Eka Nurrahema Ning; Kawaroe, Mujizat; Bengen, Dietriech G.

2018-03-01

Carsinoscorpius rotundicauda or horseshoe crab biomass has great potential in pharmaceutical aspects, one of them as an antibacterial substance. Information related to the benefits of Carsinoscorpius rotundicauda biomass such as meat and blood is essential because in fact, this species is considered a pest by fishermen, a low market value and has no legal protection in Indonesia. The purpose of this study was to determine the content of biomaterial compounds of meat and bioactivity of Carsinoscorpius rotundicauda plasma on bacterial inhibition from three different stations harvested from the waters in Madura Strait. The observation of the utilization of the potential from horseshoe crab biomass ie meat and plasma was performed by measuring the content of biomaterial compound in horseshoe crab meat by HPLC method and zone of inhibition test for gram-positive and gram-negative bacteria in horseshoe crab plasma. Analysis of the relationship between the two parameters used the Principal Component Analysis. The highest content of biomaterial compounds of monoterpenoid and zoosterol is found in horseshoe crab from Bangkalan waters, namely monoterpenoid (18.33 ppm) and zoosterol (22.67 ppm), while the smallest compound content obtained in horseshoe crab from Probolinggo waters, namely monoterpenoid (13.67) ppm and zoosterol (17.33 ppm). The bioactivity of Dark Blue Plasma (BDP) and Light Blue Plasma (LBP) samples of horseshoe crab obtained around the Madura Strait has the ability to inhibit gram-positive bacteria higher than gram-negative bacteria. The total average of DBP plasma inhibitory power on Staphylococcus aureus was 10.00 mm and 10.07 mm on Bacillus, while that in LBP sample, Staphylococcus aureus was 9.11 mm and Bacillus was 9.67 mm. The high biomaterial compound content of horseshoe crab is in line with the ability of horseshoe crab plasma to inhibit Bacillus and Staphylococcus aureus.

Curcumin conjugated silica nanoparticles for improving bioavailability and its anticancer applications.

PubMed

Gangwar, Rajesh K; Tomar, Geetanjali B; Dhumale, Vinayak A; Zinjarde, Smita; Sharma, Rishi B; Datar, Suwarna

2013-10-09

Curcumin, a yellow bioactive component of Indian spice turmeric, is known to have a wide spectrum of biological applications. In spite of various astounding therapeutic properties, it lacks in bioavailability mainly due to its poor solubility in water. In this work, we have conjugated curcumin with silica nanoparticles to improve its aqueous solubility and hence to make it more bioavailable. Conjugation and loading of curcumin with silica nanoparticles was further examined with transmission electron microscope (TEM) and thermogravimetric analyzer. Cytotoxicity analysis of synthesized silica:curcumin conjugate was studied against HeLa cell lines as well as normal fibroblast cell lines. This study shows that silica:curcumin conjugate has great potential for anticancer application.

Ganoderma lucidum Polysaccharides as An Anti-cancer Agent.

PubMed

Sohretoglu, Didem; Huang, Shile

2017-11-13

The mushroom Ganoderma lucidum (G. lucidum) has been used for centuries in Asian countries to treat various diseases and to promote health and longevity. Clinical studies have shown beneficial effects of G. lucidum as an alternative adjuvant therapy in cancer patients without obvious toxicity. G. lucidum polysaccharides (GLP) is the main bioactive component in the water soluble extracts of this mushroom. Evidence from in vitro and in vivo studies has demonstrated that GLP possesses potential anticancer activity through immunomodulatory, anti-proliferative, pro-apoptotic, anti-metastatic and anti-angiogenic effects. Here, we briefly summarize these anticancer effects of GLP and the underlying mechanisms. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Cyclotides Insert into Lipid Bilayers to Form Membrane Pores and Destabilize the Membrane through Hydrophobic and Phosphoethanolamine-specific Interactions*

PubMed Central

Wang, Conan K.; Wacklin, Hanna P.; Craik, David J.

2012-01-01

Cyclotides are a family of plant-derived circular proteins with potential therapeutic applications arising from their remarkable stability, broad sequence diversity, and range of bioactivities. Their membrane-binding activity is believed to be a critical component of their mechanism of action. Using isothermal titration calorimetry, we studied the binding of the prototypical cyclotides kalata B1 and kalata B2 (and various mutants) to dodecylphosphocholine micelles and phosphoethanolamine-containing lipid bilayers. Although binding is predominantly an entropy-driven process, suggesting that hydrophobic forces contribute significantly to cyclotide-lipid complex formation, specific binding to the phosphoethanolamine-lipid headgroup is also required, which is evident from the enthalpic changes in the free energy of binding. In addition, using a combination of dissipative quartz crystal microbalance measurements and neutron reflectometry, we elucidated the process by which cyclotides interact with bilayer membranes. Initially, a small number of cyclotides bind to the membrane surface and then insert first into the outer membrane leaflet followed by penetration through the membrane and pore formation. At higher concentrations of cyclotides, destabilization of membranes occurs. Our results provide significant mechanistic insight into how cyclotides exert their bioactivities. PMID:23129773

Effect of Curcumin Supplementation on Physiological Fatigue and Physical Performance in Mice

PubMed Central

Huang, Wen-Ching; Chiu, Wan-Chun; Chuang, Hsiao-Li; Tang, Deh-Wei; Lee, Zon-Min; Wei, Li; Chen, Fu-An; Huang, Chi-Chang

2015-01-01

Curcumin (CCM) is a well-known phytocompound and food component found in the spice turmeric and has multifunctional bioactivities. However, few studies have examined its effects on exercise performance and physical fatigue. We aimed to evaluate the potential beneficial effects of CCM supplementation on fatigue and ergogenic function following physical challenge in mice. Male ICR mice were divided into four groups to receive vehicle or CCM (180 μg/mL) by oral gavage at 0, 12.3, 24.6, or 61.5 mL/kg/day for four weeks. Exercise performance and anti-fatigue function were evaluated after physical challenge by forelimb grip strength, exhaustive swimming time, and levels of physical fatigue-associated biomarkers serum lactate, ammonia, blood urea nitrogen (BUN), and glucose and tissue damage markers such as aspartate transaminase (AST), alanine transaminase (ALT), and creatine kinase (CK). CCM supplementation dose-dependently increased grip strength and endurance performance and significantly decreased lactate, ammonia, BUN, AST, ALT, and CK levels after physical challenge. Muscular glycogen content, an important energy source for exercise, was significantly increased. CCM supplementation had few subchronic toxic effects. CCM supplementation may have a wide spectrum of bioactivities for promoting health, improving exercise performance and preventing fatigue. PMID:25647661

Electrospun nanofibers-mediated on-demand drug release.

PubMed

Chen, Menglin; Li, Yan-Fang; Besenbacher, Flemming

2014-11-01

A living system has a complex and accurate regulation system with intelligent sensor-processor-effector components to enable the release of vital bioactive substances on demand at a specific site and time. Stimuli-responsive polymers mimic biological systems in a crude way where an external stimulus results in a change in conformation, solubility, or alternation of the hydrophilic/hydrophobic balance, and consequently release of a bioactive substance. Electrospinning is a straightforward and robust method to produce nanofibers with the potential to incorporate drugs in a simple, rapid, and reproducible process. This feature article emphasizes an emerging area using an electrospinning technique to generate biomimetic nanofibers as drug delivery devices that are responsive to different stimuli, such as temperature, pH, light, and electric/magnetic field for controlled release of therapeutic substances. Although at its infancy, the mimicry of these stimuli-responsive nanofibers to the function of the living systems includes both the fibrous structural feature and bio-regulation function as an on demand drug release depot. The electrospun nanofibers with extracellular matrix morphology intrinsically guide cellular drug uptake, which will be highly desired to translate the promise of drug delivery for the clinical success. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Effect of solvents extraction on phytochemical components and biological activities of Tunisian date seeds (var. Korkobbi and Arechti).

PubMed

Thouri, Amira; Chahdoura, Hassiba; El Arem, Amira; Omri Hichri, Amel; Ben Hassin, Rihab; Achour, Lotfi

2017-05-04

The interest in natural antioxidants, especially polyphenols, is growing more and more thanks to their positive contribution to human health. Thus, the prevention from the harmful action of oxidative stress which has been involved in many diseases such as cancer, inflammation diabetes, and cardiovascular illness. Recent research proved the bioactive compounds richness of date seeds which could be a good biological matrix of natural antioxidants. Unfortunately, an important quantity of Tunisian dates seed is discarded yearly. In this study, different solvents extraction (water, methanol, absolute acetone and aqueous acetone 80%) were used and the evaluation of its effect on phytochemical level, in vitro antioxidant activities, in vitro hyperglycemia key enzymes inhibition and in vivo anti-inflammatory proprieties were established for Tunisian date seeds. The result revealed that the polar solvent exhibited the highest amount of bioactive compounds. The correlation between polyphenol compounds and the antioxidant potentiality explains the powerful effect of used polar solvents on inflammation, TBARS and hyperglycemia inhibition. Furthermore, it showed its higher capacity to scavenge radicals. Therefore, this big waste of Tunisian seeds could be used as cheap source of natural antioxidant compounds which are considered as a health challenge for the poor countries.

Bioprospecting of Marine Macrophytes Using MS-Based Lipidomics as a New Approach

PubMed Central

Maciel, Elisabete; Leal, Miguel Costa; Lillebø, Ana Isabel; Domingues, Pedro; Domingues, Maria Rosário; Calado, Ricardo

2016-01-01

The marine environment supports a remarkable diversity of organisms which are a potential source of natural products with biological activities. These organisms include a wide variety of marine plants (from micro- to macrophytes), which have been used in the food and pharmaceutical industry. However, the biochemistry and biological activities of many of these macrophytes (namely macroalgae and halophytes, including seagrasses) are still far from being fully explored. Most popular bioactive components include polysaccharides, peptides, phenolics and fatty acids (FAs). Polar lipids (glycolipids, phospholipids and betaine lipids) are emerging as novel value-added bioactive phytochemicals, rich in n-3 FA, with high nutritional value and health beneficial effects for the prevention of chronic diseases. Polar lipids account various combinations of polar groups, fatty acyl chains and backbone structures. The polar lipidome of macrophytes is remarkably diverse, and its screening represents a significant analytical challenge. Modern research platforms, particularly mass spectrometry (MS)-based lipidomic approaches, have been recently used to address this challenge and are here reviewed. The application of lipidomics to address lipid composition of marine macrophytes will contribute to the stimulation of further research on this group and foster the exploration of novel applications. PMID:27005634

The use of marine-derived bioactive compounds as potential hepatoprotective agents

PubMed Central

Nair, Dileep G; Weiskirchen, Ralf; Al-Musharafi, Salma K

2015-01-01

The marine environment may be explored as a rich source for novel drugs. A number of marine-derived compounds have been isolated and identified, and their therapeutic effects and pharmacological profiles are characterized. In the present review, we highlight the recent studies using marine compounds as potential hepatoprotective agents for the treatment of liver fibrotic diseases and discuss the proposed mechanisms of their activities. In addition, we discuss the significance of similar studies in Oman, where the rich marine life provides a potential for the isolation of novel natural, bioactive products that display therapeutic effects on liver diseases. PMID:25500871

Thermophilic and alkaliphilic Actinobacteria: biology and potential applications

PubMed Central

Shivlata, L.; Satyanarayana, Tulasi

2015-01-01

Microbes belonging to the phylum Actinobacteria are prolific sources of antibiotics, clinically useful bioactive compounds and industrially important enzymes. The focus of the current review is on the diversity and potential applications of thermophilic and alkaliphilic actinobacteria, which are highly diverse in their taxonomy and morphology with a variety of adaptations for surviving and thriving in hostile environments. The specific metabolic pathways in these actinobacteria are activated for elaborating pharmaceutically, agriculturally, and biotechnologically relevant biomolecules/bioactive compounds, which find multifarious applications. PMID:26441937

In Vitro Assessment of Bioactivities of Lactobacillus Strains as Potential Probiotics for Humans and Chickens.

PubMed

Shokryazdan, P; Jahromi, M F; Liang, J B; Sieo, C C; Kalavathy, R; Idrus, Z; Ho, Y W

2017-11-01

Twelve previously isolated Lactobacillus strains were investigated for their in vitro bioactivities, including bile salt hydrolase (BSH), cholesterol-reducing and antioxidant activities, cytotoxic effects against cancer cells, enzyme activity, and biogenic amine production. Among them, only 4 strains showed relatively high BSH activity, whereas the rest exhibited low BSH activity. All 12 strains showed cholesterol-reducing and antioxidant activities, especially in their intact cells, which in most of the cases, the isolated strains were stronger in these activities than the tested commercial reference strains. None of the tested strains produced harmful enzymes (β-glucosidase and β-glucuronidase) or biogenic amines. Among the 12 strains, 3 strains were tested for their cytotoxic effects against 3 cancer cell lines, which exhibited strong cytotoxic effects, and they also showed selectivity in killing cancer cells when compared to normal cells. Hence, all 12 Lactobacillus strains could be considered good potential probiotic candidates because of their beneficial functional bioactivities. The Lactobacillus strains tested in this study could be considered good potential probiotic candidates for food/feed industry because of their beneficial functional bioactivities such as good cholesterol-reducing ability, high antioxidant activity, and good and selective cytotoxic effect against cancer cells. © 2017 Institute of Food Technologists®.

Bioactive Proteins in Human Milk-Potential Benefits for Preterm Infants.

PubMed

Lönnerdal, Bo

2017-03-01

Human milk contains many bioactive proteins that are likely to be involved in the better outcomes of breast-fed infants compared with those fed infant formula. Bovine milk proteins or protein fractions may be able to provide some of these benefits and may, therefore, be used for preterm infants. Recombinant human milk proteins are likely to exert bioactivities similar to those of the native human milk proteins, but considerable research is needed before they can be used in routine care of preterm infants. Copyright © 2016 Elsevier Inc. All rights reserved.

Biologically active chitosan systems for tissue engineering and regenerative medicine.

PubMed

Jiang, Tao; Kumbar, Sangamesh G; Nair, Lakshmi S; Laurencin, Cato T

2008-01-01

Biodegradable polymeric scaffolds are widely used as a temporary extracellular matrix in tissue engineering and regenerative medicine. By physical adsorption of biomolecules on scaffold surface, physical entrapment of biomolecules in polymer microspheres or hydrogels, and chemical immobilization of oligopeptides or proteins on biomaterials, biologically active biomaterials and scaffolds can be derived. These bioactive systems show great potential in tissue engineering in rendering bioactivity and/or specificity to scaffolds. This review highlights some of the biologically active chitosan systems for tissue engineering application and the associated strategies to develop such bioactive chitosan systems.

Dietary fibre: The scientific search for an ideal definition and methodology of analysis, and its physiological importance as a carrier of bioactive compounds.

PubMed

Macagnan, Fernanda Teixeira; da Silva, Leila Picolli; Hecktheuer, Luisa Helena

2016-07-01

There is a growing need for a global consensus on the definition of dietary fibre and the use of appropriate methodologies for its determination in different food matrices. Oligosaccharides (prebiotic effect) and bioactive compounds (antioxidant effect) are important constituents of dietary fibre, which enhance its beneficial effects in the body, such as those related to maintaining intestinal health. These dietary components need to be quantified and addressed in conjunction with fibre in nutritional studies due to the close relationship between them and their common destiny in the human body. This review discusses updates to the concept of dietary fibre, with an emphasis on biological and methodological aspects, and highlights the physiological importance of fibre as a carrier of bioactive compounds. Copyright © 2016 Elsevier Ltd. All rights reserved.

Bioactive factors for tissue regeneration: state of the art.

PubMed

Ohba, Shinsuke; Hojo, Hironori; Chung, Ung-Il

2012-07-01

THERE ARE THREE COMPONENTS FOR THE CREATION OF NEW TISSUES: cell sources, scaffolds, and bioactive factors. Unlike conventional medical strategies, regenerative medicine requires not only analytical approaches but also integrative ones. Basic research has identified a number of bioactive factors that are necessary, but not sufficient, for organogenesis. In skeletal development, these factors include bone morphogenetic proteins (BMPs), transforming growth factor β TGF-β, Wnts, hedgehogs (Hh), fibroblast growth factors (FGFs), insulin-like growth factors (IGFs), SRY box-containing gene (Sox) 9, Sp7, and runt-related transcription factors (Runx). Clinical and preclinical studies have been extensively performed to apply the knowledge to bone and cartilage regeneration. Given the large number of findings obtained so far, it would be a good time for a multi-disciplinary, collaborative effort to optimize these known factors and develop appropriate drug delivery systems for delivering them.

Cytotoxic effects of Mangifera indica L. kernel extract on human breast cancer (MCF-7 and MDA-MB-231 cell lines) and bioactive constituents in the crude extract.

PubMed

Abdullah, Al-Shwyeh Hussah; Mohammed, Abdulkarim Sabo; Abdullah, Rasedee; Mirghani, Mohamed Elwathig Saeed; Al-Qubaisi, Mothanna

2014-06-25

Waterlily Mango (Mangifera indica L.) is thought to be antioxidant-rich, conferred by its functional phytochemicals. The potential anticancer effects of the ethanolic kernel extract on breast cancer cells (MDA-MB-231 and MCF-7) using MTT, anti-proliferation, neutral red (NR) uptake and lactate dehydrogenase (LDH) release assays were evaluated. Cytological studies on the breast cancer cells were also conducted, and phytochemical analyses of the extract were carried out to determine the likely bioactive compounds responsible for such effects. Results showed the extract induced cytotoxicity in MDA-MB-231 cells and MCF-7 cells with IC50 values of 30 and 15 μg/mL, respectively. The extract showed significant toxicity towards both cell lines, with low toxicity to normal breast cells (MCF-10A). The cytotoxic effects on the cells were further confirmed by the NR uptake, antiproliferative and LDH release assays. Bioactive analyses revealed that many bioactives were present in the extract although butylated hydroxytoluene, a potent antioxidant, was the most abundant with 44.65%. M. indica extract appears to be more cytoxic to both estrogen positive and negative breast cancer cell lines than to normal breast cells. Synergistic effects of its antioxidant bioactives could have contributed to the cytotoxic effects of the extract. The extract of M. indica, therefore, has potential anticancer activity against breast cancer cells. This potential is worth studying further, and could have implications on future studies and eventually management of human breast cancers.

Cytotoxic effects of Mangifera indica L. kernel extract on human breast cancer (MCF-7 and MDA-MB-231 cell lines) and bioactive constituents in the crude extract

PubMed Central

2014-01-01

Background Waterlily Mango (Mangifera indica L.) is thought to be antioxidant-rich, conferred by its functional phytochemicals. Methods The potential anticancer effects of the ethanolic kernel extract on breast cancer cells (MDA-MB-231 and MCF-7) using MTT, anti-proliferation, neutral red (NR) uptake and lactate dehydrogenase (LDH) release assays were evaluated. Cytological studies on the breast cancer cells were also conducted, and phytochemical analyses of the extract were carried out to determine the likely bioactive compounds responsible for such effects. Results Results showed the extract induced cytotoxicity in MDA-MB-231 cells and MCF-7 cells with IC50 values of 30 and 15 μg/mL, respectively. The extract showed significant toxicity towards both cell lines, with low toxicity to normal breast cells (MCF-10A). The cytotoxic effects on the cells were further confirmed by the NR uptake, antiproliferative and LDH release assays. Bioactive analyses revealed that many bioactives were present in the extract although butylated hydroxytoluene, a potent antioxidant, was the most abundant with 44.65%. Conclusions M. indica extract appears to be more cytoxic to both estrogen positive and negative breast cancer cell lines than to normal breast cells. Synergistic effects of its antioxidant bioactives could have contributed to the cytotoxic effects of the extract. The extract of M. indica, therefore, has potential anticancer activity against breast cancer cells. This potential is worth studying further, and could have implications on future studies and eventually management of human breast cancers. PMID:24962691

Studies on influence of aluminium ions on the bioactivity of B2O3-SiO2-P2O5-Na2O-CaO glass system by means of spectroscopic studies

NASA Astrophysics Data System (ADS)

Mohini, G. Jagan; Krishnamacharyulu, N.; Sahaya Baskaran, G.; Rao, P. Venkateswara; Veeraiah, N.

2013-12-01

Bioactive multi component glasses of the composition of 27.4 B2O3-6.4 SiO2-2.5 P2O5-25.5 Na2O-(38.2 - x) CaO: x Al2O3 (x between 0 and 3.2) were synthesized, by melt quenching technique and their bioactivity was investigated as a function of Al2O3 concentration. Initially, optical absorption and infrared spectra were recorded and analyzed in order to have some pre-understanding over structural aspects of the glasses. For understanding the bioactivity, the samples were immersed in simulated body fluid (SBF) solution for prolonged times (∼30 days) and the weight loss measurements were carried out. The spectroscopic studies were repeated on the post immersed samples. From the comparison of the analysis of the spectroscopic data of both pre-immersed and post-immersed samples together with the information on variation of pH value of residual solution as a function of immersion time, it is concluded that the participation of aluminium ions in tetrahedral positions is hindrance for the formation of HA layer and for the bioactivity of the samples.

[Microbial secondary metabolites as potential reserve of pharmaceuticals].

PubMed

Orlova, T I; Bulgakova, V G; Polin, A N

2014-01-01

The major characteristics of new bioactive microbial secondary metabolites are summarized in the review. A wide range of new molecular targets are implicated in discovery of new nonantibiotic compounds with some other pharmacological activities (noninfectious diseases). Microorganisms represent fascinating resources due to their production of novel products with broad spectra of bioactivities.

Sulfated polysaccharides with antioxidant and anticoagulant activity from the sea cucumber Holothuria fuscogliva

NASA Astrophysics Data System (ADS)

Li, Rongfeng; Yu, Huahua; Yue, Yang; Liu, Song; Xing, Rong'e.; Chen, Xiaolin; Li, Pengcheng

2017-07-01

Sea cucumber is a traditional nutritional food and medicinal resource with many bioactive components in China. Holothuria fuscogliva is a big sea cucumber with a rich of bioactive polysaccharides. To investigate the bioactivities of the polysaccharides from sea cucumber H. fuscogliva, we prepared the sulfated polysaccharides (HfP) from sea cucumber H. fuscogliva using a protease hydrolysis method. Antioxidant activities of HfP were investigated, including hydroxyl radical scavenging activity and superoxide radical scavenging activity. And, the anticoagulant activities of HfP were studied, including the activated partial thromboplastin time (APTT), prothrombin time (PT) and thrombin time (TT). The average molecular weight was 1 867.1 Da, with a sulfate content of 20.7%. In addition, the molar ratio of monosaccharide composition of HfP was Man: Rha: Glc A: Glc: Gal: Xyl: Fuc=0.083 6: 0.437: 0.134: 0:1.182: 0.748: 1. It had a strong antioxidant activity, the hydroxyl and superoxide radical scavenging activity EC50 of HfP was 3.74 and 0.037 mg/mL, respectively. It also showed a good anticoagulant activity in our study. The APTT of HfP was much higher than that of heparin sodium, and the PT and TT of HfP was close to that of heparin sodium at a low concentration. Therefore, HfP shows a good antioxidant and anticoagulant activity and it may become a potential candidate of the natural antioxidant and anticoagulant and will have a good application future in health product or medicine industry.

Implications of the Maillard reaction on bovine alpha-lactalbumin and its proteolysis during in vitro infant digestion.

PubMed

Joubran, Yousef; Moscovici, Alice; Portmann, Reto; Lesmes, Uri

2017-06-21

This study investigated the functionality and digestibility of Maillard reaction products (MRPs) of alpha-lactalbumin (α-la), a major whey protein and component of infant formulas. The impact of different carbohydrates (glucose, galactose or galacto-oligosaccharides (GOS)) and heating duration was studied. SDS-PAGE, UV and color measurements monitored reaction extent, which varied between carbohydrates whereby galactose reacted more readily than glucose. Surface hydrophobicity and antioxidant capacity were found to be significantly (p < 0.05) higher following Maillard conjugation, with GOS-based MRPs elevating antioxidant capacity ∼50-fold compared to α-la. In addition, the digestive proteolysis of MRPs was evaluated using an infant in vitro gastro-duodenal model. SDS-PAGE analyses of digesta revealed Maillard conjugation generally increased α-la's susceptibility to proteolysis. Interestingly, GOS-based MRPs presented an optimization challenge, since heating for 12 h delayed proteolysis, while extended heating resulted in the highest susceptibility to proteolysis. Proteomic analyses further demonstrated the differences in enzymatic cleavage patterns and helped identify bioactive peptides rendered bioaccessible during the digestion of α-la or its MRPs. Bioinformatic mining of the proteomic data using PeptideRanker also gave rise to two potentially novel bioactive peptides, FQINNKIW and GINYWLAHKALCS. Finally, antioxidant capacity of luminal contents, measured by DPPH, revealed Maillard conjugation increased the antioxidant capacity of both gastric and duodenal digesta. Overall, this work draws a link between the Maillard reaction, digestive proteolysis and the bioaccessibility of bioactive peptides and antioxidant species in the infant alimentary canal. This could help rationally process infant formulas towards improved nutritional and extra-nutritional benefits.

eBASIS (Bioactive Substances in Food Information Systems) and Bioactive Intakes: Major Updates of the Bioactive Compound Composition and Beneficial Bioeffects Database and the Development of a Probabilistic Model to Assess Intakes in Europe

PubMed Central

Plumb, Jenny; Pigat, Sandrine; Bompola, Foteini; Cushen, Maeve; Pinchen, Hannah; Nørby, Eric; Astley, Siân; Lyons, Jacqueline; Kiely, Mairead; Finglas, Paul

2017-01-01

eBASIS (Bioactive Substances in Food Information Systems), a web-based database that contains compositional and biological effects data for bioactive compounds of plant origin, has been updated with new data on fruits and vegetables, wheat and, due to some evidence of potential beneficial effects, extended to include meat bioactives. eBASIS remains one of only a handful of comprehensive and searchable databases, with up-to-date coherent and validated scientific information on the composition of food bioactives and their putative health benefits. The database has a user-friendly, efficient, and flexible interface facilitating use by both the scientific community and food industry. Overall, eBASIS contains data for 267 foods, covering the composition of 794 bioactive compounds, from 1147 quality-evaluated peer-reviewed publications, together with information from 567 publications describing beneficial bioeffect studies carried out in humans. This paper highlights recent updates and expansion of eBASIS and the newly-developed link to a probabilistic intake model, allowing exposure assessment of dietary bioactive compounds to be estimated and modelled in human populations when used in conjunction with national food consumption data. This new tool could assist small- and medium-sized enterprises (SMEs) in the development of food product health claim dossiers for submission to the European Food Safety Authority (EFSA). PMID:28333085

Species classification and bioactive ingredients accumulation of BaiJiangCao based on characteristic inorganic elements analysis by inductively coupled plasma-mass spectrometry and multivariate analysis

PubMed Central

Wen-Lan, Li; Xue, Zhang; Xin-Xin, Yang; Shuai, Wang; Lin, Zhao; Huan-Jun, Zhao; Yong-Rui, Bao; Chen-Feng, Ji; Ning, Chen; Zheng, Xiang

2015-01-01

Background: Patrinia scabiosaefolia Fisch and Patrinia villosa (Thunb.) Juss., two species herbs with the same Chinese name “BaiJiangCao”, are important ancient herbal medicines widely used for more than 2000 years. The clinical application of two species herb is confused due to the difficult identification. Objective: The objective was to authenticate the species of BaiJiangCao and analyze the accumulation of bioactive ingredients based on characteristic inorganic elements analysis. Materials and Methods: Content of 32 inorganic elements in BaiJiangCao from different habitats were determined by inductively coupled plasma-mass spectrometry (ICP-MS), and the characteristic inorganic elements were picked to distinguish the species of the herb by principal component analysis and cluster analysis. Contents of two bioactive ingredients, luteoloside, and oleanolic acid, in the samples, were also analyzed by high-performance liquid chromatography method. Relationship between accumulation of bioactive ingredients and content of macroelements in BaiJiangCao was established by statistics. Results: A 4 macroelements (Na, Mg, K, Fe) in 32 determined inorganic elements were picked for characteristic inorganic elements. Content of Na, Mg, K and Fe showed positive correlations with that of luteoloside, content of Na, Mg showed positive correlations with that of oleanolic acid, but content of K and Fe showed negative correlations with that of oleanolic acid. Conclusion: It is for the first time to utilize the characteristic inorganic elements as an index to classify the herb species by the method of ICP-MS and multivariate analysis. And it is also the first report to investigate the influence of inorganic elements in herb on the accumulation of bioactive components which could affect the pharmacological efficacy of the herb medicine. And this method could also be utilized in research of corresponding aspects. PMID:26600721

Binding of bile acids by pastry products containing bioactive substances during in vitro digestion.

PubMed

Dziedzic, Krzysztof; Górecka, Danuta; Szwengiel, Artur; Smoczyńska, Paulina; Czaczyk, Katarzyna; Komolka, Patrycja

2015-03-01

The modern day consumer tends to choose products with health enhancing properties, enriched in bioactive substances. One such bioactive food component is dietary fibre, which shows a number of physiological properties including the binding of bile acids. Dietary fibre should be contained in everyday, easily accessible food products. Therefore, the aim of this study was to determine sorption capacities of primary bile acid (cholic acid - CA) and secondary bile acids (deoxycholic - DCA and lithocholic acids - LCA) by muffins (BM) and cookies (BC) with bioactive substances and control muffins (CM) and cookies (CC) in two sections of the in vitro gastrointestinal tract. Variations in gut flora were also analysed in the process of in vitro digestion of pastry products in a bioreactor. Enzymes: pepsin, pancreatin and bile salts: cholic acid, deoxycholic acid and lithocholic acid were added to the culture. Faecal bacteria, isolated from human large intestine, were added in the section of large intestine. The influence of dietary fibre content in cookies and concentration of bile acids in two stages of digestion were analysed. Generally, pastry goods with bioactive substances were characterized by a higher content of total fibre compared with the control samples. These products also differ in the profile of dietary fibre fractions. Principal Component Analysis (PCA) showed that the bile acid profile after two stages of digestion depends on the quality and quantity of fibre. The bile acid profile after digestion of BM and BC forms one cluster, and with the CM and CC forms a separate cluster. High concentration of H (hemicellulose) is positively correlated with LCA (low binding effect) and negatively correlated with CA and DCA contents. The relative content of bile acids in the second stage of digestion was in some cases above the content in the control sample, particularly LCA. This means that the bacteria introduced in the 2nd stage of digestion synthesize the LCA.

Optimization of ultrasound assisted extraction of bioactive components from brown seaweed Ascophyllum nodosum using response surface methodology.

PubMed

Kadam, Shekhar U; Tiwari, Brijesh K; Smyth, Thomas J; O'Donnell, Colm P

2015-03-01

The objective of this study was to investigate the effect of key extraction parameters of extraction time (5-25 min), acid concentration (0-0.06 M HCl) and ultrasound amplitude (22.8-114 μm) on yields of bioactive compounds (total phenolics, fucose and uronic acid) from Ascophyllumnodosum. Response surface methodology was employed to optimize the extraction variables for bioactive compounds' yield. A second order polynomial model was fitted well to the extraction experimental data with (R(2)>0.79). Extraction yields of 143.12 mgGAE/gdb, 87.06 mg/gdb and 128.54 mg/gdb were obtained for total phenolics, fucose and uronic acid respectively at optimized extraction conditions of extraction time (25 min), acid concentration (0.03 M HCl) and ultrasonic amplitude (114 μm). Mass spectroscopy analysis of extracts show that ultrasound enhances the extraction of high molecular weight phenolic compounds from A. nodosum. This study demonstrates that ultrasound assisted extraction (UAE) can be employed to enhance extraction of bioactive compounds from seaweed. Copyright © 2014 Elsevier B.V. All rights reserved.

Chemical composition and bioactivity of different oregano (Origanum vulgare) extracts and essential oil.

PubMed

Teixeira, Bárbara; Marques, António; Ramos, Cristina; Serrano, Carmo; Matos, Olívia; Neng, Nuno R; Nogueira, José M F; Saraiva, Jorge Alexandre; Nunes, Maria Leonor

2013-08-30

There is a growing interest in industry to replace synthetic chemicals by natural products with bioactive properties. Aromatic plants are excellent sources of bioactive compounds that can be extracted using several processes. As far as oregano is concerned, studies are lacking addressing the effect of extraction processes in bioactivity of extracts. This study aimed to characterise the in vitro antioxidant and antibacterial properties of oregano (Origanum vulgare) essential oil and extracts (in hot and cold water, and ethanol), and the chemical composition of its essential oil. The major components of oregano essential oil were carvacrol, β-fenchyl alcohol, thymol, and γ-terpinene. Hot water extract had the strongest antioxidant properties and the highest phenolic content. All extracts were ineffective in inhibiting the growth of the seven tested bacteria. In contrast, the essential oil inhibited the growth of all bacteria, causing greater reductions on both Listeria strains (L. monocytogenes and L. innocua). O. vulgare extracts and essential oil from Portuguese origin are strong candidates to replace synthetic chemicals used by the industry. © 2013 Society of Chemical Industry.

Emerging Strategies and Integrated Systems Microbiology Technologies for Biodiscovery of Marine Bioactive Compounds

PubMed Central

Rocha-Martin, Javier; Harrington, Catriona; Dobson, Alan D.W.; O’Gara, Fergal

2014-01-01

Marine microorganisms continue to be a source of structurally and biologically novel compounds with potential use in the biotechnology industry. The unique physiochemical properties of the marine environment (such as pH, pressure, temperature, osmolarity) and uncommon functional groups (such as isonitrile, dichloroimine, isocyanate, and halogenated functional groups) are frequently found in marine metabolites. These facts have resulted in the production of bioactive substances with different properties than those found in terrestrial habitats. In fact, the marine environment contains a relatively untapped reservoir of bioactivity. Recent advances in genomics, metagenomics, proteomics, combinatorial biosynthesis, synthetic biology, screening methods, expression systems, bioinformatics, and the ever increasing availability of sequenced genomes provides us with more opportunities than ever in the discovery of novel bioactive compounds and biocatalysts. The combination of these advanced techniques with traditional techniques, together with the use of dereplication strategies to eliminate known compounds, provides a powerful tool in the discovery of novel marine bioactive compounds. This review outlines and discusses the emerging strategies for the biodiscovery of these bioactive compounds. PMID:24918453

Antifungal, Anticancer and Aminopeptidase Inhibitory Potential of a Phenazine Compound Produced by Lactococcus BSN307.

PubMed

Varsha, Kontham Kulangara; Nishant, Gopalan; Sneha, Srambikal Mohandas; Shilpa, Ganesan; Devendra, Leena; Priya, Sulochana; Nampoothiri, Kesavan Madhavan

2016-12-01

A bioactive compound was purified from the culture medium of a new strain of Lactococcus BSN307 by solvent extraction followed by chromatographic techniques. This bioactive compound was identified to belong to phenazine class of compounds by MS, NMR and FTIR. The phenazine compound showed antifungal activity against Aspergillus niger , Penicillium chrysogenum as well as Fusarium oxysporum by disc diffusion assay in addition to antioxidant potential as demonstrated by DPPH scavenging assay. The compound demonstrated selective cytotoxicity against cancer cell lines HeLa and MCF-7 where IC 50 was achieved with 20 and 24 µg/mL respectively. At the same time no cytotoxicity was occurred in normal H9c2 cells. The bioactive found to be inhibitory to both leucine and proline aminopeptidases and thus revealed its potential as metalloenzyme inhibitor. This study, for the first time reports the production of phenazine class of compounds by lactic acid bacteria.

Nutrigenomics and nutrigenetics.

PubMed

Farhud, Dd; Zarif Yeganeh, M; Zarif Yeganeh, M

2010-01-01

The nutrients are able to interact with molecular mechanisms and modulate the physiological functions in the body. The Nutritional Genomics focuses on the interaction between bioactive food components and the genome, which includes Nutrigenetics and Nutrigenomics. The influence of nutrients on f genes expression is called Nutrigenomics, while the heterogeneous response of gene variants to nutrients, dietary components and developing nutraceticals is called Nutrigenetics. Genetic variation is known to affect food tolerances among human subpopulations and may also influence dietary requirements and raising the possibility of individualizing nutritional intake for optimal health and disease prevention on the basis of an individual's genome. Nutrigenomics provides a genetic understanding for how common dietary components affect the balance between health and disease by altering the expression and/or structure of an individual's genetic makeup. Nutrigenetics describes that the genetic profile have impact on the response of body to bioactive food components by influencing their absorption, metabolism, and site of action.In this way, considering different aspects of gene-nutrient interaction and designing appropriate diet for every specific genotype that optimize individual health, diagnosis and nutritional treatment of genome instability, we could prevent and control conversion of healthy phenotype to diseases.

Nutrigenomics and Nutrigenetics

PubMed Central

Farhud, DD; Zarif Yeganeh, M; Zarif Yeganeh, M

2010-01-01

The nutrients are able to interact with molecular mechanisms and modulate the physiological functions in the body. The Nutritional Genomics focuses on the interaction between bioactive food components and the genome, which includes Nutrigenetics and Nutrigenomics. The influence of nutrients on f genes expression is called Nutrigenomics, while the heterogeneous response of gene variants to nutrients, dietary components and developing nutraceticals is called Nutrigenetics. Genetic variation is known to affect food tolerances among human subpopulations and may also influence dietary requirements and raising the possibility of individualizing nutritional intake for optimal health and disease prevention on the basis of an individual’s genome. Nutrigenomics provides a genetic understanding for how common dietary components affect the balance between health and disease by altering the expression and/or structure of an individual’s genetic makeup. Nutrigenetics describes that the genetic profile have impact on the response of body to bioactive food components by influencing their absorption, metabolism, and site of action. In this way, considering different aspects of gene–nutrient interaction and designing appropriate diet for every specific genotype that optimize individual health, diagnosis and nutritional treatment of genome instability, we could prevent and control conversion of healthy phenotype to diseases. PMID:23113033

Therapeutic and nutraceutical potential of bioactive compounds extracted from fruit residues.

PubMed

Babbar, Neha; Oberoi, Harinder Singh; Sandhu, Simranjeet Kaur

2015-01-01

The growing interest in the substitution of synthetic food antioxidants by natural ones has fostered research in identifying new low-cost antioxidants having commercial potential. Fruits such as mango, banana, and those belonging to the citrus family leave behind a substantial amount of residues in the form of peels, pulp, seeds, and stones. Due to lack of infrastructure to handle a huge quantity of available biomass, lack of processing facilities, and high processing cost, these residues represent a major disposal problem, especially in developing countries. Because of the presence of phenolic compounds, which impart nutraceutical properties to fruit residues, such residues hold tremendous potential in food, pharmaceutical, and cosmetic industries. The biological properties such as anticarcinogenicity, antimutagenicity, antiallergenicity, and antiageing activity have been reported for both natural as well as synthetic antioxidants. Special attention is focused on extraction of bioactive compounds from inexpensive or residual sources. The purpose of this review is to characterize different phenolics present in the fruit residues, discuss the antioxidant potential of such residues and the assays used in determination of antioxidant properties, discuss various methods for efficient extraction of the bioactive compounds, and highlight the importance of fruit residues as potential nutraceutical resources and biopreservatives.

Piperine production by endophytic fungus Colletotrichum gloeosporioides isolated from Piper nigrum.

PubMed

Chithra, S; Jasim, B; Sachidanandan, P; Jyothis, M; Radhakrishnan, E K

2014-03-15

Many endophytic fungi have been reported with the biosynthetic potential to produce same or similar metabolites present in host plants. The adaptations that might have acquired by these fungi as a result of the long-term association with their host plants can be the possible basis of their biosynthetic potential. The bioactive compounds originated from endophytes are currently explored for their potential applications in pharmaceutical, agriculture and food industries. Piper nigrum, a plant of the Piperaceae is very remarkable because of the presence of the alkaloid piperine. Piperine has been reported to have broad bioactive properties ranging from antimicrobial, antidepressant, anti-inflammatory, antioxidative to anticancer activities. Interestingly, piperine also plays a vital role in increasing the bioavailability of many drugs which again is a promising property. The current study was carried out to identify piperine producing endophytic fungus from Piper nigrum L. By screening various endophytic fungi, the isolate which was identified as member of Colletotrichum gloeosporioides was found to have the ability to form piperine and was confirmed by HPLC and LCMS. Considering the broad bioactive potential of piperine, the piperine producing fungi identified in the study can expect to have much industrial potential. Copyright © 2013 Elsevier GmbH. All rights reserved.

Soy and Gut Microbiota: Interaction and Implication for Human Health.

PubMed

Huang, Haiqiu; Krishnan, Hari B; Pham, Quynhchi; Yu, Liangli Lucy; Wang, Thomas T Y

2016-11-23

Soy (Glycine max) is a major commodity in the United States, and soy foods are gaining popularity due to their reported health-promoting effects. In the past two decades, soy and soy bioactive components have been studied for their health-promoting/disease-preventing activities and potential mechanisms of action. Recent studies have identified gut microbiota as an important component in the human body ecosystem and possibly a critical modulator of human health. Soy foods' interaction with the gut microbiota may critically influence many aspects of human development, physiology, immunity, and nutrition at different stages of life. This review summarizes current knowledge on the effects of soy foods and soy components on gut microbiota population and composition. It was found, although results vary in different studies, in general, both animal and human studies have shown that consumption of soy foods can increase the levels of bifidobacteria and lactobacilli and alter the ratio between Firmicutes and Bacteroidetes. These changes in microbiota are consistent with reported reductions in pathogenic bacteria populations in the gut, thereby lowering the risk of diseases and leading to beneficial effects on human health.

Boosting the bioavailability of hydrophobic nutrients, vitamins, and nutraceuticals in natural products using excipient emulsions.

PubMed

McClements, David Julian; Saliva-Trujillo, Laura; Zhang, Ruojie; Zhang, Zipei; Zou, Liqiang; Yao, Mingfei; Xiao, Hang

2016-10-01

Many highly hydrophobic bioactives, such as non-polar nutrients, nutraceuticals, and vitamins, have a relatively low or variable oral bioavailability. The poor bioavailability profile of these bioactives may be due to limited bioaccessibility, poor absorption, and/or chemical transformation within the gastrointestinal tract (GIT). The bioavailability of hydrophobic bioactives can be improved using specially designed oil-in-water emulsions consisting of lipid droplets dispersed within an aqueous phase. The bioactives may be isolated from their natural environment and then incorporated into the lipid phase of emulsion-based delivery systems. Alternatively, the bioactives may be left in their natural environment (e.g., fruits or vegetables), and then ingested with emulsion-based excipient systems. An excipient emulsion may have no inherent health benefits itself, but it boosts the biological activity of bioactive ingredients co-ingested with it by altering their bioaccessibility, absorption, and/or chemical transformation. This review discusses the design and fabrication of excipient emulsions, and gives some examples of recent research that demonstrates their potential efficacy for improving the bioavailability of hydrophobic bioactives. The concept of excipient emulsions could be used to formulate emulsion-based food products (such as excipient sauces, dressings, dips, creams, or yogurts) specifically designed to increase the bioavailability of bioactive agents in natural foods, such as fruits and vegetables. Copyright © 2015 Elsevier Ltd. All rights reserved.

Mouse Models for Unraveling the Importance of Diet in Colon Cancer Prevention

PubMed Central

Tammariello, Alexandra E.; Milner, John A.

2010-01-01

Diet and genetics are both considered important risk determinants for colorectal cancer, a leading cause of death worldwide. Several genetically engineered mouse models have been created, including the ApcMin mouse, to aid in the identification of key cancer related processes and to assist with the characterization of environmental factors, including the diet, which influence risk. Current research using these models provides evidence that several bioactive food components can inhibit genetically predisposed colorectal cancer, while others increase risk. Specifically, calorie restriction or increased exposure to n-3 fatty acids, sulforaphane, chafuroside, curcumin, and dibenzoylmethane were reported protective. Total fat, calories and all-trans retinoic acid are associated with an increased risk. Unraveling the importance of specific dietary components in these models is complicated by the basal diet used, the quantity of test components provided, and interactions among food components. Newer models are increasingly available to evaluate fundamental cellular processes, including DNA mismatch repair, immune function and inflammation as markers for colon cancer risk. Unfortunately, these models have been used infrequently to examine the influence of specific dietary components. The enhanced use of these models can shed mechanistic insights about the involvement of specific bioactive food and components and energy as determinants of colon cancer risk. However, the use of available mouse models to exactly represent processes important to human gastrointestinal cancers will remain a continued scientific challenge. PMID:20122631

Potential anticancer properties of bioactive compounds of Gymnema sylvestre and its biofunctionalized silver nanoparticles

PubMed Central

Arunachalam, Kantha Deivi; Arun, Lilly Baptista; Annamalai, Sathesh Kumar; Arunachalam, Aarrthy M

2015-01-01

Background Gymnema sylvestre is an ethno-pharmacologically important medicinal plant used in many polyherbal formulations for its potential health benefits. Silver nanoparticles (SNPs) were biofunctionalized using aqueous leaf extracts of G. sylvestre. The anticancer properties of the bioactive compounds and the biofunctionalized SNPs were compared using the HT29 human adenoma colon cancer cell line. Methods The preliminary phytochemical screening for bioactive compounds from aqueous extracts revealed the presence of alkaloids, triterpenes, flavonoids, steroids, and saponins. Biofunctionalized SNPs were synthesized using silver nitrate and characterized by ultraviolet–visible spectroscopy, scanning electron microscopy, energy-dispersive X-ray analysis, Fourier transform infrared spectroscopy, and X-ray diffraction for size and shape. The characterized biofunctionalized G. sylvestre were tested for its in vitro anticancer activity against HT29 human colon adenocarcinoma cells. Results The biofunctionlized G. sylvestre SNPs showed the surface plasmon resonance band at 430 nm. The scanning electron microscopy images showed the presence of spherical nanoparticles of various sizes, which were further determined using the Scherrer equation. In vitro cytotoxic activity of the biofunctionalized green-synthesized SNPs (GSNPs) indicated that the sensitivity of HT29 human colon adenocarcinoma cells for cytotoxic drugs is higher than that of Vero cell line for the same cytotoxic agents and also higher than the bioactive compound of the aqueous extract. Conclusion Our results show that the anticancer properties of the bioactive compounds of G. sylvestre can be enhanced through biofunctionalizing the SNPs using the bioactive compounds present in the plant extract without compromising their medicinal properties. PMID:25565802

Cyanobactins from Cyanobacteria: Current Genetic and Chemical State of Knowledge

PubMed Central

Martins, Joana; Vasconcelos, Vitor

2015-01-01

Cyanobacteria are considered to be one of the most promising sources of new, natural products. Apart from non-ribosomal peptides and polyketides, ribosomally synthesized and post-translationally modified peptides (RiPPs) are one of the leading groups of bioactive compounds produced by cyanobacteria. Among these, cyanobactins have sparked attention due to their interesting bioactivities and for their potential to be prospective candidates in the development of drugs. It is assumed that the primary source of cyanobactins is cyanobacteria, although these compounds have also been isolated from marine animals such as ascidians, sponges and mollusks. The aim of this review is to update the current knowledge of cyanobactins, recognized as being produced by cyanobacteria, and to emphasize their genetic clusters and chemical structures as well as their bioactivities, ecological roles and biotechnological potential. PMID:26580631

Marine bioactives as functional food ingredients: potential to reduce the incidence of chronic diseases.

PubMed

Lordan, Sinéad; Ross, R Paul; Stanton, Catherine

2011-01-01

The marine environment represents a relatively untapped source of functional ingredients that can be applied to various aspects of food processing, storage, and fortification. Moreover, numerous marine-based compounds have been identified as having diverse biological activities, with some reported to interfere with the pathogenesis of diseases. Bioactive peptides isolated from fish protein hydrolysates as well as algal fucans, galactans and alginates have been shown to possess anticoagulant, anticancer and hypocholesterolemic activities. Additionally, fish oils and marine bacteria are excellent sources of omega-3 fatty acids, while crustaceans and seaweeds contain powerful antioxidants such as carotenoids and phenolic compounds. On the basis of their bioactive properties, this review focuses on the potential use of marine-derived compounds as functional food ingredients for health maintenance and the prevention of chronic diseases.

Marine Bioactives as Functional Food Ingredients: Potential to Reduce the Incidence of Chronic Diseases

PubMed Central

Lordan, Sinéad; Ross, R. Paul; Stanton, Catherine

2011-01-01

The marine environment represents a relatively untapped source of functional ingredients that can be applied to various aspects of food processing, storage, and fortification. Moreover, numerous marine-based compounds have been identified as having diverse biological activities, with some reported to interfere with the pathogenesis of diseases. Bioactive peptides isolated from fish protein hydrolysates as well as algal fucans, galactans and alginates have been shown to possess anticoagulant, anticancer and hypocholesterolemic activities. Additionally, fish oils and marine bacteria are excellent sources of omega-3 fatty acids, while crustaceans and seaweeds contain powerful antioxidants such as carotenoids and phenolic compounds. On the basis of their bioactive properties, this review focuses on the potential use of marine-derived compounds as functional food ingredients for health maintenance and the prevention of chronic diseases. PMID:21747748

Nutritional Genomics, Polyphenols, Diets, and Their Impact on Dietetics

PubMed Central

Barnes, Stephen

2009-01-01

Nutritional genomics offers a way to optimize human health and the quality of life. It is an attractive endeavor, but one with substantial challenges. It encompasses almost all known aspects of science, ranging from the genomes of humans, plants and microorganisms, to the highest levels of food science, analytical science, computing and statistics of large systems, as well as human behavior. The underlying biochemistry that is targeted by the principal issues in nutritional genomics is described and entails genomics, transcriptomics, proteomics and metabolomics. A major feature relevant to nutritional genomics is the single nucleotide polymorphisms in genes that interact with nutrients and other bioactive food components. These genetic changes may lead to alterations in absorption, metabolism and functional responses to bioactive nutritional factors. Bioactive food components may also regulate gene expression at the transcriptome, protein abundance and/or protein turnover levels. Even if all of these variables are known, additional variables to be taken into account include the nutritional variability of the food (unprocessed and processed), the amount that is actually eaten, and the eating-related behaviors of those consuming the food. These challenges are explored within the context of soy intake. Finally, the importance of international co-operation in nutritional genomics research is presented. PMID:18954579

Designing polymers with sugar-based advantages for bioactive delivery applications.

PubMed

Zhang, Yingyue; Chan, Jennifer W; Moretti, Alysha; Uhrich, Kathryn E

2015-12-10

Sugar-based polymers have been extensively explored as a means to increase drug delivery systems' biocompatibility and biodegradation. Here,we review he use of sugar-based polymers for drug delivery applications, with a particular focus on the utility of the sugar component(s) to provide benefits for drug targeting and stimuli responsive systems. Specifically, numerous synthetic methods have been developed to reliably modify naturally-occurring polysaccharides, conjugate sugar moieties to synthetic polymer scaffolds to generate glycopolymers, and utilize sugars as a multifunctional building block to develop sugar-linked polymers. The design of sugar-based polymer systems has tremendous implications on both the physiological and biological properties imparted by the saccharide units and are unique from synthetic polymers. These features include the ability of glycopolymers to preferentially target various cell types and tissues through receptor interactions, exhibit bioadhesion for prolonged residence time, and be rapidly recognized and internalized by cancer cells. Also discussed are the distinct stimuli-sensitive properties of saccharide-modified polymers to mediate drug release under desired conditions. Saccharide-based systems with inherent pH- and temperature-sensitive properties, as well as enzyme-cleavable polysaccharides for targeted bioactive delivery, are covered. Overall, this work emphasizes inherent benefits of sugar-containing polymer systems for bioactive delivery.

Influence of silica matrix composition and functional component additives on the bioactivity and viability of encapsulated living cells

DOE Office of Scientific and Technical Information (OSTI.GOV)

Savage, Travis J.; Dunphy, Darren R.; Harbaugh, Svetlana

The remarkable impact encapsulation matrix chemistry can have on the bioactivity and viability of integrated living cells is reported. Two silica chemistries (aqueous silicate and alkoxysilane), and a functional component additive (glycerol), are employed to generate three distinct silica matrices. These matrices are used to encapsulate living E. coli cells engineered with a synthetic riboswitch for cell-based biosensing. Following encapsulation, membrane integrity, reproductive capability, and riboswitch-based protein expression levels and rates are measured over a 5 week period. Striking differences in E. coli bioactivity, viability, and biosensing performance are observed for cells encapsulated within the different matrices. E. coli cellsmore » encapsulated for 35 days in aqueous silicate-based (AqS) matrices showed relatively low membrane integrity, but high reproductive capability in comparison to cells encapsulated in glycerol containing sodium silicate-based (AqS + g) and alkoxysilane-based (PGS) gels. Further, cells in sodium silicate-based matrices showed increasing fluorescence output over time, resulting in a 1.8-fold higher fluorescence level, and a faster expression rate, over cells free in solution. Furthermore, this unusual and unique combination of biological properties demonstrates that careful design of the encapsulation matrix chemistry can improve functionality of the biocomposite material, and result in new and unexpected physiological states.« less

Influence of silica matrix composition and functional component additives on the bioactivity and viability of encapsulated living cells

DOE PAGES

Savage, Travis J.; Dunphy, Darren R.; Harbaugh, Svetlana; ...

2015-11-06

The remarkable impact encapsulation matrix chemistry can have on the bioactivity and viability of integrated living cells is reported. Two silica chemistries (aqueous silicate and alkoxysilane), and a functional component additive (glycerol), are employed to generate three distinct silica matrices. These matrices are used to encapsulate living E. coli cells engineered with a synthetic riboswitch for cell-based biosensing. Following encapsulation, membrane integrity, reproductive capability, and riboswitch-based protein expression levels and rates are measured over a 5 week period. Striking differences in E. coli bioactivity, viability, and biosensing performance are observed for cells encapsulated within the different matrices. E. coli cellsmore » encapsulated for 35 days in aqueous silicate-based (AqS) matrices showed relatively low membrane integrity, but high reproductive capability in comparison to cells encapsulated in glycerol containing sodium silicate-based (AqS + g) and alkoxysilane-based (PGS) gels. Further, cells in sodium silicate-based matrices showed increasing fluorescence output over time, resulting in a 1.8-fold higher fluorescence level, and a faster expression rate, over cells free in solution. Furthermore, this unusual and unique combination of biological properties demonstrates that careful design of the encapsulation matrix chemistry can improve functionality of the biocomposite material, and result in new and unexpected physiological states.« less

An Extensive Description of the Peptidomic Repertoire of the Hen Egg Yolk Plasma.

PubMed

Arena, Simona; Scaloni, Andrea

2018-03-28

Hen egg is a raw material widely used for the preparation of food,  pharmaceutical and cosmetoceutical products. Dedicated proteomic studies were accomplished on eggshell membrane, egg white, and yolk, identifying the most abundant proteins. No similar peptidomic studies have been performed so far. Only preliminary investigations on bioactive peptides in egg fractions and digestates were accomplished through functional screening assays, characterizing antioxidant, antibacterial, antiviral, immunomodulatory, and antihypertensive preparations and isolated components. This study fills this gap and provides a comprehensive picture of the peptides present in the yolk plasma of different hen egg types after 24 and 264 h of laying, taking advantage of a procedure based on a two-step fractionation followed by combined MALDI-TOF-TOF-MS- and nanoLC-ESI-Q-Orbitrap-MS/MS-based analysis. Six hundred and twenty-eight peptides were characterized as deriving from the proteolytic processing of larger protein components after the physiological action of chicken chymotrypsin-like and pepsin-like enzymes. Structural details on their post-translational modifications were also provided. Identified peptides were subjected to bioinformatic analysis and further compared with available data from the literature, ascertaining 198 peptides associable with putative antihypertensive, antimicrobial, anticancer, antiviral, antibiofilm, anorectic, calcium-binding, and anti-inflammatory activities. This analysis was often confirmative of previous experimental evidence on functional properties of unfractionated preparations or isolated molecules. These results further emphasize the bioactive action of yolk-derived peptides as related to egg consumption, and the potential use of these molecules as additive ingredients in the preparation of functional foods and cosmetics.

Epigenetic mechanisms in anti-cancer actions of bioactive food components – the implications in cancer prevention

PubMed Central

Stefanska, B; Karlic, H; Varga, F; Fabianowska-Majewska, K; Haslberger, AG

2012-01-01

The hallmarks of carcinogenesis are aberrations in gene expression and protein function caused by both genetic and epigenetic modifications. Epigenetics refers to the changes in gene expression programming that alter the phenotype in the absence of a change in DNA sequence. Epigenetic modifications, which include amongst others DNA methylation, covalent modifications of histone tails and regulation by non-coding RNAs, play a significant role in normal development and genome stability. The changes are dynamic and serve as an adaptation mechanism to a wide variety of environmental and social factors including diet. A number of studies have provided evidence that some natural bioactive compounds found in food and herbs can modulate gene expression by targeting different elements of the epigenetic machinery. Nutrients that are components of one-carbon metabolism, such as folate, riboflavin, pyridoxine, cobalamin, choline, betaine and methionine, affect DNA methylation by regulating the levels of S-adenosyl-L-methionine, a methyl group donor, and S-adenosyl-L-homocysteine, which is an inhibitor of enzymes catalyzing the DNA methylation reaction. Other natural compounds target histone modifications and levels of non-coding RNAs such as vitamin D, which recruits histone acetylases, or resveratrol, which activates the deacetylase sirtuin and regulates oncogenic and tumour suppressor micro-RNAs. As epigenetic abnormalities have been shown to be both causative and contributing factors in different health conditions including cancer, natural compounds that are direct or indirect regulators of the epigenome constitute an excellent approach in cancer prevention and potentially in anti-cancer therapy. PMID:22536923

Inhibitory Effects of Polyacetylene Compounds from Panax ginseng on Neurotrophin Receptor-Mediated Hair Growth.

PubMed

Suzuki, Aoi; Matsuura, Daisuke; Kanatani, Hirotoshi; Yano, Shingo; Tsunakawa, Mitsuo; Matsuyama, Shigeru; Shigemori, Hideyuki

2017-01-01

Neurotrophins play an important role in the control of the hair growth cycle. Therefore, neurotrophin receptor antagonists have therapeutic potential for the treatment of hair growth disorders. In this study, we investigated the inhibitory effect of Panax ginseng, a medicinal plant commonly used to treat alopecia, on the binding of neurotrophins to their receptors. In addition, we isolated and characterized the bioactive compounds of P. ginseng extracts. P. ginseng hexane extracts strongly inhibited brain-derived neurotrophic factor (BDNF)-TrkB and β-nerve growth factor (β-NGF)-p75 neurotrophin receptor (p75NTR) binding. Furthermore, we identified the following 6 polyacetylene compounds as the bioactive components in P. ginseng hexane extract: panaxynol (1), panaxydol (2), panaxydol chlorohydrin (3), 1,8-heptadecadiene-4,6-diyne-3,10-diol (4), panaxytriol (5), and dihydropanaxacol (6). In particular, compounds 4, 5, and 6 significantly inhibited BDNF-TrkB binding in a dose-dependent manner. To identify the structural component mediating the inhibitory effect, we investigated the effects of the hydroxyl moiety in these compounds. We found that the inhibitory effect of panaxytriol (5) was strong, whereas the inhibitory effect of Ac-panaxytriol (7) was relatively weak. Our findings suggest that P. ginseng-derived polyacetylenes with a hydroxyl moiety might provide therapeutic benefits to patients with hair growth disorders such as alopecia by inhibiting the binding of neurotrophins to their receptors. Although saponins have been proposed to be the primary mediators of the effects of P. ginseng on hair growth, this study revealed that polyacetylene compounds exert similar effects.

Synthesis, bioactivity and zeta potential investigations of chlorine and fluorine substituted hydroxyapatite.

PubMed

Fahami, Abbas; Beall, Gary W; Betancourt, Tania

2016-02-01

Chlorine and fluorine substituted hydroxyapatites (HA-Cl-F) with different degrees of ion replacement were successfully prepared by the one step mechanochemical activation method. X-ray diffraction (XRD) and FT-IR spectra indicated that substitution of these anions in milled powders resulted in the formation of pure hydroxyapatite phase except for the small observed change in the lattice parameters and unit cell volumes of the resultant hydroxyapatite. Microscopic observations showed that the milled product had a cluster-like structure made up of polygonal and spherical particles with an average particle size of approximately ranged from 20±5 to 70±5nm. The zeta potential of milled samples was performed at three different pH (5, 7.4, and 9). The obtained zeta potential values were negative for all three pH values. Negative zeta potential was described to favor osseointegration, apatite nucleation, and bone regeneration. The bioactivity of samples was investigated on sintered pellets soaked in simulated body fluid (SBF) solution and apatite crystals formed on the surface of the pellets after being incubated for 14days. Zeta potential analysis and bioactivity experiment suggested that HA-Cl-F will lead to the formation of new apatite particles and therefore be a potential implant material. Copyright © 2015 Elsevier B.V. All rights reserved.

Preparation, characterization and bioavailability by oral administration of O/W curcumin nanoemulsions stabilized with lysophosphatidylcholine.

PubMed

Chávez-Zamudio, Rubi; Ochoa-Flores, Angélica A; Soto-Rodríguez, Ida; Garcia-Varela, Rebeca; García, Hugo Sergio

2017-09-20

Curcumin is the main and most abundant bioactive component in Curcuma longa L. with documented properties in the prevention and treatment of chronic degenerative and infectious diseases. However, curcumin has low solubility in aqueous media, hence low bioavailability when administered orally. The use of nanoemulsions as carriers can provide a partial solution to bioavailability restrictions. In our study, O/W nanoemulsions of curcumin were prepared using lysophosphatidylcholine, a phospholipid with proven emulsification capacity; nevertheless, such qualities have not been previously reported in the preparation of nanoemulsions. Lysophosphatidylcholine was obtained by enzymatic removal of one fatty acid residue from phosphatidylcholine. The objective of our work was to formulate stable curcumin nanoemulsions and evaluate their bioavailability in BALB/c mice plasma after oral administration. Formulated nanoemulsions had a droplet size mean of 154.32 ± 3.10 nm, a polydispersity index of 0.34 ± 0.07 and zeta potential of -10.43 ± 1.10 mV; stability was monitored for 12 weeks. Lastly, in vivo pharmacokinetic parameters, using BALB/c mice, were obtained; namely, C max of 610 ± 65.0 μg mL -1 and T max of 2 h. Pharmacokinetic data revealed a higher bioavailability of emulsified as opposed to free curcumin. Research regarding other potential emulsifiers that may provide better health benefits and carry nano-encapsulated bioactive compounds more effectively, is necessary. This study provides important data on the preparation and design of nanoencapsulated Curcumin using lysophosphatidylcholine as an emulsifier.

Application of multi-target phytotherapeutic concept in malaria drug discovery: a systems biology approach in biomarker identification.

PubMed

Tarkang, Protus Arrey; Appiah-Opong, Regina; Ofori, Michael F; Ayong, Lawrence S; Nyarko, Alexander K

2016-01-01

There is an urgent need for new anti-malaria drugs with broad therapeutic potential and novel mode of action, for effective treatment and to overcome emerging drug resistance. Plant-derived anti-malarials remain a significant source of bioactive molecules in this regard. The multicomponent formulation forms the basis of phytotherapy. Mechanistic reasons for the poly-pharmacological effects of plants constitute increased bioavailability, interference with cellular transport processes, activation of pro-drugs/deactivation of active compounds to inactive metabolites and action of synergistic partners at different points of the same signaling cascade. These effects are known as the multi-target concept. However, due to the intrinsic complexity of natural products-based drug discovery, there is need to rethink the approaches toward understanding their therapeutic effect. This review discusses the multi-target phytotherapeutic concept and its application in biomarker identification using the modified reverse pharmacology - systems biology approach. Considerations include the generation of a product library, high throughput screening (HTS) techniques for efficacy and interaction assessment, High Performance Liquid Chromatography (HPLC)-based anti-malarial profiling and animal pharmacology. This approach is an integrated interdisciplinary implementation of tailored technology platforms coupled to miniaturized biological assays, to track and characterize the multi-target bioactive components of botanicals as well as identify potential biomarkers. While preserving biodiversity, this will serve as a primary step towards the development of standardized phytomedicines, as well as facilitate lead discovery for chemical prioritization and downstream clinical development.

Iron depletion strategy for targeted cancer therapy: utilizing the dual roles of neutrophil gelatinase-associated lipocalin protein.

PubMed

Tang, Hsin-Chieh; Chang, Pei-Chun; Chen, Yu-Chian

2016-01-01

Decreasing iron uptake and increasing iron efflux may result in cell death by oxidative inactivation of vital enzymes. Applying the dual function of neutrophil gelatinase-associated lipocalin (NGAL) could achieve the goal of iron depletion in the cancer cells. Tyr106, Lys125 or Lys134 was the key binding site for NGAL protein to sequester iron-chelating siderophores. In this study, we employed all bioactive peptides in peptide databank to dock with the siderophore-binding sites of NGAL protein by virtual screening. In addition, we performed molecular dynamics (MD) simulation to observe the molecular character and structural variation of ligand-protein interaction. Glu-Glu-Lys-Glu (EEKE), Glu-Glu-Asp-Cys-Lys (EEDCK), and Gly-Glu-Glu-Cys-Asp (GEECD) were selected preliminarily by rigorous scoring functions for further investigation. GEECD was excluded due to higher binding total energy than the others. Moreover, we also excluded EEKE due to larger influence to the stability of binding residues by the information of root mean square fluctuation (RMSF) and principal component analysis (PCA). Thus, we suggested that EEDCK was the potential bioactive peptide which had been proved to inhibit malignant cells for targeted cancer therapy. Graphical Abstract Perspective drug design of occupying the siderophore-binding sites of NGAL outside the cell temporarily by a potential short peptide until NGAL enters into the cell, and releasing the siderophore-binding sites inside the cell.

Identification of multifunctional peptides from human milk.

PubMed

Mandal, Santi M; Bharti, Rashmi; Porto, William F; Gauri, Samiran S; Mandal, Mahitosh; Franco, Octavio L; Ghosh, Ananta K

2014-06-01

Pharmaceutical industries have renewed interest in screening multifunctional bioactive peptides as a marketable product in health care applications. In this context, several animal and plant peptides with potential bioactivity have been reported. Milk proteins and peptides have received much attention as a source of health-enhancing components to be incorporated into nutraceuticals and functional foods. By using this source, 24 peptides have been fractionated and purified from human milk using RP-HPLC. Multifunctional roles including antimicrobial, antioxidant and growth stimulating activity have been evaluated in all 24 fractions. Nevertheless, only four fractions show multiple combined activities among them. Using a proteomic approach, two of these four peptides have been identified as lactoferrin derived peptide and kappa casein short chain peptide. Lactoferrin derived peptide (f8) is arginine-rich and kappa casein derived (f12) peptide is proline-rich. Both peptides (f8 and f12) showed antimicrobial activities against both Gram-positive and Gram-negative bacteria. Fraction 8 (f8) exhibits growth stimulating activity in 3T3 cell line and f12 shows higher free radical scavenging activity in comparison to other fractions. Finally, both peptides were in silico evaluated and some insights into their mechanism of action were provided. Thus, results indicate that these identified peptides have multiple biological activities which are valuable for the quick development of the neonate and may be considered as potential biotechnological products for nutraceutical industry. Copyright © 2014 Elsevier Inc. All rights reserved.

Oral administration of Nitraria retusa ethanolic extract enhances hepatic lipid metabolism in db/db mice model 'BKS.Cg-Dock7(m)+/+ Lepr(db/)J' through the modulation of lipogenesis-lipolysis balance.

PubMed

Zar Kalai, Feten; Han, Junkyu; Ksouri, Riadh; Abdelly, Chedly; Isoda, Hiroko

2014-10-01

The medicinal plants can be used in the prevention or treatment of many diseases. Several studies concerning the potential of bioactive components in plants and food products and their link to obesity and related metabolic disorders, have been gaining big interest. Diabetes is a serious metabolic syndrome. Searching for alternative natural bioactive molecules is considered main strategy to manage diabetes through weight management. In the present study, an edible halophyte Nitraria retusa was selected and in vivo experiment was conducted using db/db model mice. We orally administrated its ethanol extract (NRE) to BKS.Cg-Dock7(m)+/+ Lepr(db/)J mice model for a period of 4 weeks. The effect was evaluated on the body weight and adiposity changes and on the biochemical parameters of db/db NRE-treated mice. The molecular mechanism underlying the anti-obesity effect was investigated by testing the gene expression related to hepatic lipid metabolism. NRE was found to significantly supress increases in body and fat mass weight, decreases triglycerides and LDL-cholesterol levels and enhances gene expression related to lipid homeostasis in liver showing anti-obesity actions. Our findings, indicate that NRE possesses potential anti-obesity effects in BKS.Cg-Dock7(m)+/+ Lepr(db/)J model mice and may relieve obesity-related symptoms including hyperlipidemia through modulating the lipolysis-lipogenesis balance. Copyright © 2014 Elsevier Ltd. All rights reserved.

Development of novel techniques to extract phenolic compounds from Romanian cultivars of Prunus domestica L. and their biological properties.

PubMed

Mocan, Andrei; Diuzheva, Alina; Carradori, Simone; Andruch, Vasil; Massafra, Chiara; Moldovan, Cadmiel; Sisea, Cristian; Petzer, Jacobus P; Petzer, Anél; Zara, Susi; Marconi, Guya Diletta; Zengin, Gokhan; Crișan, Gianina; Locatelli, Marcello

2018-04-21

In the present work, fourteen cultivars of Prunus domestica were analysed to investigate their phenolic pattern with the purpose of using the leaves as potential resources of bioactive compounds in the pharmaceutical and food industry. Microwave-assisted extraction (MAE), dispersive liquid-liquid microextraction and sugaring-out liquid-liquid extraction techniques were optimized in order to obtain an exhaustive multi-component panel of phenolic compounds. The best phenolic-enriched recovery was achieved using MAE in water:methanol (30:70), and this procedure was further applied for quantitative analysis of phenolic compounds in real samples. In order to prove the safeness of these extracts, the biological potential of the Prunus cultivars was tested by several in vitro antioxidant and enzyme inhibitory assays. Moreover, their cytotoxicity was evaluated on human gingival fibroblasts (HGFs), and in most of the cases the treatment with different concentrations of extracts didn't show cytotoxicity up to 500 μg/mL. Only 'Carpatin' and 'Minerva' cultivars, at 250 and 500 μg/mL, reduced partially cell viability of HGFs population. Noteworthy, Centenar cultivar was the most active for the α-glucosidase inhibition (6.77 mmolACAE/g extract), whereas Ialomița cultivar showed the best antityrosinase activity (23.07 mgKAE/g extract). Overall, leaves of P. domestica represent a rich alternative source of bioactive compounds. Copyright © 2018. Published by Elsevier Ltd.

Pharmacological Potential of Phylogenetically Diverse Actinobacteria Isolated from Deep-Sea Coral Ecosystems of the Submarine Avilés Canyon in the Cantabrian Sea.

PubMed

Sarmiento-Vizcaíno, Aida; González, Verónica; Braña, Alfredo F; Palacios, Juan J; Otero, Luis; Fernández, Jonathan; Molina, Axayacatl; Kulik, Andreas; Vázquez, Fernando; Acuña, José L; García, Luis A; Blanco, Gloria

2017-02-01

Marine Actinobacteria are emerging as an unexplored source for natural product discovery. Eighty-seven deep-sea coral reef invertebrates were collected during an oceanographic expedition at the submarine Avilés Canyon (Asturias, Spain) in a range of 1500 to 4700 m depth. From these, 18 cultivable bioactive Actinobacteria were isolated, mainly from corals, phylum Cnidaria, and some specimens of phyla Echinodermata, Porifera, Annelida, Arthropoda, Mollusca and Sipuncula. As determined by 16S rRNA sequencing and phylogenetic analyses, all isolates belong to the phylum Actinobacteria, mainly to the Streptomyces genus and also to Micromonospora, Pseudonocardia and Myceligenerans. Production of bioactive compounds of pharmacological interest was investigated by high-performance liquid chromatography (HPLC) and gas chromatography-mass spectrometry (GC-MS) techniques and subsequent database comparison. Results reveal that deep-sea isolated Actinobacteria display a wide repertoire of secondary metabolite production with a high chemical diversity. Most identified products (both diffusible and volatiles) are known by their contrasted antibiotic or antitumor activities. Bioassays with ethyl acetate extracts from isolates displayed strong antibiotic activities against a panel of important resistant clinical pathogens, including Gram-positive and Gram-negative bacteria, as well as fungi, all of them isolated at two main hospitals (HUCA and Cabueñes) from the same geographical region. The identity of the active extracts components of these producing Actinobacteria is currently being investigated, given its potential for the discovery of pharmaceuticals and other products of biotechnological interest.

Termitarium-Inhabiting Bacillus spp. Enhanced Plant Growth and Bioactive Component in Turmeric (Curcuma longa L.).

PubMed

Chauhan, Ankit Kumar; Maheshwari, Dinesh Kumar; Dheeman, Shrivardhan; Bajpai, Vivek K

2017-02-01

Curcumin (diferuloyl methane) is the main bioactive component of turmeric (Curcuma longa L.) having remarkable multipotent medicinal and therapeutic applications. Two Bacilli isolated from termitarium soil and identified as Bacillus endophyticus TSH42 and Bacillus cereus TSH77 were used for bacterization of rhizome for raising C. longa ver. suguna for growth and enhancement. Both the strains showed remarkable PGP activities and also chemotactic in nature with high chemotactic index. Turmeric plants bacterized with strains B. endophyticus TSH42 and B. cereus TSH77 individually and in combination increased plant growth and turmeric production up to 18% in field trial in comparison to non-bacterized plants. High-performance liquid chromatography analysis was performed to determine the content of curcumin, which showed concentration of curcumin in un-inoculated turmeric as 3.66 g which increased by 13.6% (4.16 g) when combination of TSH42 and TSH77 was used.

Antialgal and antilarval activities of bioactive compounds extracted from the marine dinoflagellate Amphidinium carterae

NASA Astrophysics Data System (ADS)

Kong, Xianyu; Han, Xiurong; Gao, Min; Su, Rongguo; Wang, Ke; Li, Xuzhao; Lu, Wei

2016-12-01

With the global ban on the application of organotin-based marine coatings by the International Maritime Organization, the development of environmentally friendly, low-toxic and nontoxic antifouling compounds for marine industries has become an urgent need. Marine microorganisms have been considered as a potential source of natural antifoulants. In this study, the antifouling potential of marine dinoflagellate Amphidinium carterae, the toxic and red-tide microalgae, was investigated. We performed a series of operations to extract the bioactive substances from Amphidinium carterae and tested their antialgal and antilarval activities. The crude extract of Amphidinium carterae showed significant antialgal activity and the EC50 value against Skeletonema costatum was 55.4 μg mL-1. After purification, the isolated bioactive substances (the organic extract C) exhibited much higher antialgal and antilarval activities with EC50 of 12.9 μg mL-1 against Skeletonema costatum and LC50 of 15.1 μg mL-1 against Amphibalanus amphitrite larvae. Subsequently, IR, Q-TOFMS, and GC-MS were utilized for the structural elucidation of the bioactive compounds, and a series of unsaturated and saturated 16- to 22-carbon fatty acids were detected. The data suggested the bioactive compounds isolated from Amphidinium carterae exhibited a significant inhibiting effect against the diatom Skeletonema costatum and Amphibalanus amphitrite larvae, and could be substitutes for persistent, toxic antifouling compounds.

Bead-based screening in chemical biology and drug discovery.

PubMed

Komnatnyy, Vitaly V; Nielsen, Thomas E; Qvortrup, Katrine

2018-06-11

High-throughput screening is an important component of the drug discovery process. The screening of libraries containing hundreds of thousands of compounds requires assays amenable to miniaturisation and automization. Combinatorial chemistry holds a unique promise to deliver structurally diverse libraries for early drug discovery. Among the various library forms, the one-bead-one-compound (OBOC) library, where each bead carries many copies of a single compound, holds the greatest potential for the rapid identification of novel hits against emerging drug targets. However, this potential has not yet been fully realized due to a number of technical obstacles. In this feature article, we review the progress that has been made in bead-based library screening and its application to the discovery of bioactive compounds. We identify the key challenges of this approach and highlight key steps needed for making a greater impact in the field.

Mangiferin in cancer chemoprevention and treatment: pharmacokinetics and molecular targets.

PubMed

Rajendran, Peramaiyan; Rengarajan, Thamaraiselvan; Nandakumar, Natarajan; Divya, H; Nishigaki, Ikuo

2015-02-01

A variety of bioactive food components have been shown to modulate inflammatory responses and to attenuate carcinogenesis. Polyphenols isolated several years ago from various medicinal plants now seem to have a prominent role in the prevention and therapy of a variety of ailments. Mangiferin, a unique, important, and highly investigated polyphenol, has attracted much attention of late for its potential as a chemopreventive and chemotherapeutic agent against various types of cancer. Mangiferin has been shown to target multiple proinflammatory transcription factors, cell- cycle proteins, growth factors, kinases, cytokines, chemokines, adhesion molecules, and inflammatory enzymes. These targets can potentially mediate the chemopreventive and therapeutic effects of mangiferin by inhibiting the initiation, promotion, and metastasis of cancer. This review not only summarizes the diverse molecular targets of mangiferin, but also gives the results of various preclinical studies that have been performed in the last decade with this promising polyphenol.

Helleborus purpurascens-Amino Acid and Peptide Analysis Linked to the Chemical and Antiproliferative Properties of the Extracted Compounds.

PubMed

Segneanu, Adina-Elena; Grozescu, Ioan; Cziple, Florentina; Berki, Daniel; Damian, Daniel; Niculite, Cristina Mariana; Florea, Alexandru; Leabu, Mircea

2015-12-11

There is a strong drive worldwide to discover and exploit the therapeutic potential of a large variety of plants. In this work, an alcoholic extract of Helleborus purpurascens (family Ranunculaceae) was investigated for the identification of amino acids and peptides with putative antiproliferative effects. In our work, a separation strategy was developed using solvents of different polarity in order to obtain active compounds. Biochemical components were characterized through spectroscopic (mass spectroscopy) and chromatographic techniques (RP-HPLC and GC-MS). The biological activity of the obtained fractions was investigated in terms of their antiproliferative effects on HeLa cells. Through this study, we report an efficient separation of bioactive compounds (amino acids and peptides) from a plant extract dependent on solvent polarity, affording fractions with unaffected antiproliferative activities. Moreover, the two biologically tested fractions exerted a major antiproliferative effect, thereby suggesting potential anticancer therapeutic activity.

Bioactive phytochemicals in barley.

PubMed

Idehen, Emmanuel; Tang, Yao; Sang, Shengmin

2017-01-01

Epidemiological studies have consistently shown that regular consumption of whole grain barley reduces the risk of developing chronic diseases. The presence of barley fiber, especially β-glucan in whole grain barley, has been largely credited for these health benefits. However, it is now widely believed that the actions of the fiber component alone do not explain the observed health benefits associated with the consumption of whole grain barley. Whole grain barley also contains phytochemicals including phenolic acids, flavonoids, lignans, tocols, phytosterols, and folate. These phytochemicals exhibit strong antioxidant, antiproliferative, and cholesterol lowering abilities, which are potentially useful in lowering the risk of certain diseases. Therefore, the high concentration of phytochemicals in barley may be largely responsible for its health benefits. This paper reviews available information regarding barley phytochemicals and their potential to combat common nutrition-related diseases including cancer, cardiovascular disease, diabetes, and obesity. Copyright © 2016. Published by Elsevier B.V.

Digestibility of sulfated polysaccharide from the brown seaweed Ascophyllum nodosum and its effect on the human gut microbiota in vitro.

PubMed

Chen, Ligen; Xu, Wei; Chen, Dan; Chen, Guijie; Liu, Junwei; Zeng, Xiaoxiong; Shao, Rong; Zhu, Hongjun

2018-06-01

Sulfated polysaccharides from marine algae exhibit various bioactivities with potential benefits for human health and well-being. In this study, the in vitro digestibility and fermentability of polysaccharides from the brown seaweed Ascophyllum nodosum (AnPs) were examined, and the effects of AnPs on gut microbiota were determined using high-throughput sequencing technology. Salivary amylase, artificial gastric juice, and intestinal juice had no effect on AnPs, but the molecular weight of AnPs and reducing sugar decreased significantly after fermentation by gut microbiota. AnPs significantly modulated the composition of the gut microbiota; in particular, they increased the relative abundance of Bacteroidetes and Firmicutes, suggesting the potential for AnPs to decrease the risk of obesity. Furthermore, the total SCFA content after fermentation increased significantly. These results suggest that AnPs have potential uses as functional food components to improve human gut health. Copyright © 2018. Published by Elsevier B.V.

Polysaccharides from the Marine Environment with Pharmacological, Cosmeceutical and Nutraceutical Potential.

PubMed

Ruocco, Nadia; Costantini, Susan; Guariniello, Stefano; Costantini, Maria

2016-04-27

Carbohydrates, also called saccharides, are molecules composed of carbon, hydrogen, and oxygen. They are the most abundant biomolecules and essential components of many natural products and have attracted the attention of researchers because of their numerous human health benefits. Among carbohydrates the polysaccharides represent some of the most abundant bioactive substances in marine organisms. In fact, many marine macro- and microorganisms are good resources of carbohydrates with diverse applications due to their biofunctional properties. By acting on cell proliferation and cycle, and by modulating different metabolic pathways, marine polysaccharides (including mainly chitin, chitosan, fucoidan, carrageenan and alginate) also have numerous pharmaceutical activities, such as antioxidative, antibacterial, antiviral, immuno-stimulatory, anticoagulant and anticancer effects. Moreover, these polysaccharides have many general beneficial effects for human health, and have therefore been developed into potential cosmeceuticals and nutraceuticals. In this review we describe current advances in the development of marine polysaccharides for nutraceutical, cosmeceutical and pharmacological applications. Research in this field is opening new doors for harnessing the potential of marine natural products.

Impact of sampling parameters on the radical scavenging potential of olive (Olea europaea L.) leaves.

PubMed

Papoti, Vassiliki T; Tsimidou, Maria Z

2009-05-13

The impact of sampling parameters, that is, cultivar, leaf age, and sampling date, on the radical scavenging potential of olive leaf extracts was examined via the DPPH(*) and other assays. Total phenol content was estimated colorimetrically and by fluorometry, whereas phenol composition was assessed by RP-HPLC coupled with diode array, fluorometric, and MS detection systems. Oleuropein was not always the major leaf constituent. Considerable differences noted in individual phenol levels (hydroxytyrosol, oleuropein and other secoiridoids, verbascoside, and flavonoids) among samples were not reflected either in the total phenol content or in the radical scavenging potential of the extracts. It can be suggested that olive leaf is a robust source of radical scavengers throughout the year and that differentiation in the levels of individual components depends rather on sampling period than on cultivar or age. The latter does not present predictable regularity. Exploitation of all types of leaves expected in an olive tree shoot for the extraction of bioactive compounds is feasible.

Red algal extracts from Plocamium lyngbyanum and Ceramium secundatum stimulate osteogenic activities in vitro and bone growth in zebrafish larvae.

PubMed

Carson, Matthew A; Nelson, John; Cancela, M Leonor; Laizé, Vincent; Gavaia, Paulo J; Rae, Margaret; Heesch, Svenja; Verzin, Eugene; Maggs, Christine; Gilmore, Brendan F; Clarke, Susan A

2018-05-16

Through the current trend for bioprospecting, marine organisms - particularly algae - are becoming increasingly known for their osteogenic potential. Such organisms may provide novel treatment options for osteoporosis and other musculoskeletal conditions, helping to address their large healthcare burden and the limitations of current therapies. In this study, extracts from two red algae - Plocamium lyngbyanum and Ceramium secundatum - were tested in vitro and in vivo for their osteogenic potential. In vitro, the growth of human bone marrow stromal cells (hBMSCs) was significantly greater in the presence of the extracts, particularly with P. lyngbyanum treatment. Osteogenic differentiation was promoted more by C. secundatum (70 µg/ml), though P. lyngbyanum had greater in vitro mineralisation potential. Both species caused a marked and dose-dependent increase in the opercular bone area of zebrafish larvae. Our findings therefore indicate the presence of bioactive components in P. lyngbyanum and C. secundatum extracts, which can promote both in vitro and in vivo osteogenic activity.

Bioactive Glasses: Where Are We and Where Are We Going?

PubMed

Baino, Francesco; Hamzehlou, Sepideh; Kargozar, Saeid

2018-03-19

Bioactive glasses caused a revolution in healthcare and paved the way for modern biomaterial-driven regenerative medicine. The first 45S5 glass composition, invented by Larry Hench fifty years ago, was able to bond to living bone and to stimulate osteogenesis through the release of biologically-active ions. 45S5-based glass products have been successfully implanted in millions of patients worldwide, mainly to repair bone and dental defects and, over the years, many other bioactive glass compositions have been proposed for innovative biomedical applications, such as soft tissue repair and drug delivery. The full potential of bioactive glasses seems still yet to be fulfilled, and many of today's achievements were unthinkable when research began. As a result, the research involving bioactive glasses is highly stimulating and requires a cross-disciplinary collaboration among glass chemists, bioengineers, and clinicians. The present article provides a picture of the current clinical applications of bioactive glasses, and depicts six relevant challenges deserving to be tackled in the near future. We hope that this work can be useful to both early-stage researchers, who are moving with their first steps in the world of bioactive glasses, and experienced scientists, to stimulate discussion about future research and discover new applications for glass in medicine.

Bioactive Glasses: Where Are We and Where Are We Going?

PubMed Central

Hamzehlou, Sepideh

2018-01-01

Bioactive glasses caused a revolution in healthcare and paved the way for modern biomaterial-driven regenerative medicine. The first 45S5 glass composition, invented by Larry Hench fifty years ago, was able to bond to living bone and to stimulate osteogenesis through the release of biologically-active ions. 45S5-based glass products have been successfully implanted in millions of patients worldwide, mainly to repair bone and dental defects and, over the years, many other bioactive glass compositions have been proposed for innovative biomedical applications, such as soft tissue repair and drug delivery. The full potential of bioactive glasses seems still yet to be fulfilled, and many of today’s achievements were unthinkable when research began. As a result, the research involving bioactive glasses is highly stimulating and requires a cross-disciplinary collaboration among glass chemists, bioengineers, and clinicians. The present article provides a picture of the current clinical applications of bioactive glasses, and depicts six relevant challenges deserving to be tackled in the near future. We hope that this work can be useful to both early-stage researchers, who are moving with their first steps in the world of bioactive glasses, and experienced scientists, to stimulate discussion about future research and discover new applications for glass in medicine. PMID:29562680

Effects of borate-based bioactive glass on neuron viability and neurite extension.

PubMed

Marquardt, Laura M; Day, Delbert; Sakiyama-Elbert, Shelly E; Harkins, Amy B

2014-08-01

Bioactive glasses have recently been shown to promote regeneration of soft tissues by positively influencing tissue remodeling during wound healing. We were interested to determine whether bioactive glasses have the potential for use in the treatment of peripheral nerve injury. In these experiments, degradable bioactive borate glass was fabricated into rods and microfibers. To study the compatibility with neurons, embryonic chick dorsal root ganglia (DRG) were cultured with different forms of bioactive borate glass. Cell viability was measured with no media exchange (static condition) or routine media exchange (transient condition). Neurite extension was measured within fibrin scaffolds with embedded glass microfibers or aligned rod sheets. Mixed cultures of neurons, glia, and fibroblasts growing in static conditions with glass rods and microfibers resulted in decreased cell viability. However, the percentage of neurons compared with all cell types increased by the end of the culture protocol compared with culture without glass. Furthermore, bioactive glass and fibrin composite scaffolds promoted neurite extension similar to that of control fibrin scaffolds, suggesting that glass does not have a significant detrimental effect on neuronal health. Aligned glass scaffolds guided neurite extension in an oriented manner. Together these findings suggest that bioactive glass can provide alignment to support directed axon growth. © 2013 Wiley Periodicals, Inc.

Biologically Active and Antimicrobial Peptides from Plants

PubMed Central

Salas, Carlos E.; Badillo-Corona, Jesus A.; Ramírez-Sotelo, Guadalupe; Oliver-Salvador, Carmen

2015-01-01

Bioactive peptides are part of an innate response elicited by most living forms. In plants, they are produced ubiquitously in roots, seeds, flowers, stems, and leaves, highlighting their physiological importance. While most of the bioactive peptides produced in plants possess microbicide properties, there is evidence that they are also involved in cellular signaling. Structurally, there is an overall similarity when comparing them with those derived from animal or insect sources. The biological action of bioactive peptides initiates with the binding to the target membrane followed in most cases by membrane permeabilization and rupture. Here we present an overview of what is currently known about bioactive peptides from plants, focusing on their antimicrobial activity and their role in the plant signaling network and offering perspectives on their potential application. PMID:25815307

Sequentially-crosslinked biomimetic bioactive glass/gelatin methacryloyl composites hydrogels for bone regeneration.

PubMed

Zheng, Jiafu; Zhao, Fujian; Zhang, Wen; Mo, Yunfei; Zeng, Lei; Li, Xian; Chen, Xiaofeng

2018-08-01

In recent years, gelatin-based composites hydrogels have been intensively investigated because of their inherent bioactivity, biocompatibility and biodegradability. Herein, we fabricated photocrosslinkable biomimetic composites hydrogels from bioactive glass (BG) and gelatin methacryloyl (GelMA) by a sequential physical and chemical crosslinking (gelation + UV) approach. The results showed that the compressive modulus of composites hydrogels increased significantly through the sequential crosslinking approach. The addition of BG resulted in a significant increase in physiological stability and apatite-forming ability. In vitro data indicated that BG/GelMA composites hydrogels promoted cell attachment, proliferation and differentiation. Overall, the BG/GelMA composites hydrogels combined the advantages of good biocompatibility and bioactivity, and had potential applications in bone regeneration. Copyright © 2018. Published by Elsevier B.V.

Design of Bioactive Organic-inorganic Hybrid Materials with Self-setting Ability

NASA Astrophysics Data System (ADS)

Miyazaki, T.; Machida, S.; Morita, Y.; Ishida, E.

2011-10-01

Paste-like materials with ability of self-setting are attractive for bone substitutes, since they can be injected from the small hole with minimized invasion to the patient. Although bone cements which set as apatite are clinically used, there is limitation on clinical applications due to their mechanical properties such as high brittleness and low fracture toughness. To overcome this problem, organic-inorganic hybrids based on a flexible polymer are attractive. We have obtained an idea for design of self-setting hybrids using polyion complex fabricated by ionic interaction of anionic and cationic polymers. We aimed at preparation of organic-inorganic hybrids exhibiting self-setting ability and bioactivity. The liquid component was prepared from cationic chitosan aqueous solution. The powder component was prepared by mixing various carrageenans with α-tricalcium phosphate (α-TCP). The obtained cements set within 1 day. Compressive strength showed tendency to increase with increase in α-TCP content in the powder component. The prepared cements formed the apatite in simulated body fluid within 3 days. Novel self-setting materials based on organic-inorganic hybrid can be designed utilizing ionic interaction of polysaccharide.

Food components with antifibrotic activity and implications in prevention of liver disease.

PubMed

Bae, Minkyung; Park, Young-Ki; Lee, Ji-Young

2018-05-01

Increasing prevalence of nonalcoholic fatty liver disease (NAFLD) in parallel with the obesity epidemic has been a major public health concern. NAFLD is the most common chronic liver disease in the United States, ranging from fatty liver to steatohepatitis, fibrosis and cirrhosis in the liver. In response to chronic liver injury, fibrogenesis in the liver occurs as a protective response; however, prolonged and dysregulated fibrogenesis can lead to liver fibrosis, which can further progress to cirrhosis and eventually hepatocellular carcinoma. Interplay of hepatocytes, macrophages and hepatic stellate cells (HSCs) in the hepatic inflammatory and oxidative milieu is critical for the development of NAFLD. In particular, HSCs play a major role in the production of extracellular matrix proteins. Studies have demonstrated that bioactive food components and natural products, including astaxanthin, curcumin, blueberry, silymarin, coffee, vitamin C, vitamin E, vitamin D, resveratrol, quercetin and epigallocatechin-3-gallate, have antifibrotic effects in the liver. This review summarizes current knowledge of the mechanistic insight into the antifibrotic actions of the aforementioned bioactive food components. Copyright © 2017 Elsevier Inc. All rights reserved.

Wine, resveratrol and health: a review.

PubMed

Guerrero, Raúl F; García-Parrilla, Maria C; Puertas, Belén; Cantos-Villar, Emma

2009-05-01

Several studies have cited the Mediterranean diet as an example of healthy eating. In fact, the Mediterranean diet has become the reference diet for the prevention of cardiovascular disease. Red wine seems to be an essential component of the diet, since moderate consumption of wine is associated with lower risk and mortality from cardiovascular disease. Evidence is also accumulating that wine helps prevent the development of certain cancers. Of all the many components of wine, resveratrol, which is a natural component specifically present in wine, has been identified as being mainly responsible for these health-promoting properties. Many valuable properties such as cardioprotective and anticarcinogenic activity have been attributed to resveratrol; however, its bioavailability is quite low. The bioactivity of metabolites derived from resveratrol, and the accumulation of resveratrol in vital organs are still under study, but there are high expectations of positive results. Other stilbene compounds are also considered in this review, despite being present in undetectable or very small quantities in wine. The present paper reviews all aspects of the health properties of wine, bioactive compounds found in wine, and their concentrations, bioavailability and possible synergistic effects.

Predicting the glass transition temperature of bioactive glasses from their molecular chemical composition.

PubMed

Hill, Robert G; Brauer, Delia S

2011-10-01

A recently published paper (M.D. O'Donnell, Acta Biomaterialia 7 (2011) 2264-2269) suggests that it is possible to correlate the glass transition temperature (T(g)) of bioactive glasses with their molar composition, based on iterative least-squares fitting of published T(g) data. However, we show that the glass structure is an important parameter in determining T(g). Phase separation, local structural effects and components (intermediate oxides) which can switch their structural role in the glass network need to be taken into consideration, as they are likely to influence the glass transition temperature of bioactive glasses. Although the model suggested by O'Donnell works reasonably well for glasses within the composition range presented, it is oversimplified and fails for glasses outside certain compositional boundaries. Copyright © 2011 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.

Identification of an Epoxide Metabolite of Lycopene in Human Plasma Using 13C-Labeling and QTOF-MS.

PubMed

Cichon, Morgan J; Moran, Nancy E; Riedl, Ken M; Schwartz, Steven J; Clinton, Steven K

2018-03-20

The carotenoid lycopene is a bioactive component of tomatoes and is hypothesized to reduce risk of several chronic diseases, such as prostate cancer. The metabolism of lycopene is only beginning to be understood and some studies suggest that metabolites of lycopene may be partially responsible for bioactivity associated with the parent compound. The detection and characterization of these compounds in vivo is an important step in understanding lycopene bioactivity. The metabolism of lycopene likely involves both chemical and enzymatic oxidation. While numerous lycopene metabolites have been proposed, few have actually been identified in vivo following lycopene intake. Here, LC-QTOF-MS was used along with 13 C-labeling to investigate the post-prandial oxidative metabolism of lycopene in human plasma. Previously reported aldehyde cleavage products were not detected, but a lycopene 1,2-epoxide was identified as a new candidate oxidative metabolite.

Nanostructured bioactive glass-ceramic coatings deposited by the liquid precursor plasma spraying process

NASA Astrophysics Data System (ADS)

Xiao, Yanfeng; Song, Lei; Liu, Xiaoguang; Huang, Yi; Huang, Tao; Wu, Yao; Chen, Jiyong; Wu, Fang

2011-01-01

Bioactive glass-ceramic coatings have great potential in dental and orthopedic medical implant applications, due to its excellent bioactivity, biocompatibility and osteoinductivity. However, most of the coating preparation techniques either produce only thin thickness coatings or require tedious preparation steps. In this study, a new attempt was made to deposit bioactive glass-ceramic coatings on titanium substrates by the liquid precursor plasma spraying (LPPS) process. Tetraethyl orthosilicate, triethyl phosphate, calcium nitrate and sodium nitrate solutions were mixed together to form a suspension after hydrolysis, and the liquid suspension was used as the feedstock for plasma spraying of P 2O 5-Na 2O-CaO-SiO 2 bioactive glass-ceramic coatings. The in vitro bioactivities of the as-deposited coatings were evaluated by soaking the samples in simulated body fluid (SBF) for 4 h, 1, 2, 4, 7, 14, and 21 days, respectively. The as-deposited coating and its microstructure evolution behavior under SBF soaking were systematically analyzed by scanning electron microscopy (SEM), X-ray diffraction (XRD), inductively coupled plasma (ICP), and Fourier transform infrared (FTIR) spectroscopy. The results showed that P 2O 5-Na 2O-CaO-SiO 2 bioactive glass-ceramic coatings with nanostructure had been successfully synthesized by the LPPS technique and the synthesized coatings showed quick formation of a nanostructured HCA layer after being soaked in SBF. Overall, our results indicate that the LPPS process is an effective and simple method to synthesize nanostructured bioactive glass-ceramic coatings with good in vitro bioactivity.

Marine Bioactives: Pharmacological Properties and Potential Applications against Inflammatory Diseases

PubMed Central

D’Orazio, Nicolantonio; Gammone, Maria Alessandra; Gemello, Eugenio; De Girolamo, Massimo; Cusenza, Salvatore; Riccioni, Graziano

2012-01-01

Inflammation is a hot topic in medical research, because it plays a key role in inflammatory diseases: rheumatoid arthritis (RA) and other forms of arthritis, diabetes, heart diseases, irritable bowel syndrome, Alzheimer’s disease, Parkinson’s disease, allergies, asthma, even cancer and many others. Over the past few decades, it was realized that the process of inflammation is virtually the same in different disorders, and a better understanding of inflammation may lead to better treatments for numerous diseases. Inflammation is the activation of the immune system in response to infection, irritation, or injury, with an influx of white blood cells, redness, heat, swelling, pain, and dysfunction of the organs involved. Although the pathophysiological basis of these conditions is not yet fully understood, reactive oxygen species (ROS) have often been implicated in their pathogenesis. In fact, in inflammatory diseases the antioxidant defense system is compromised, as evidenced by increased markers of oxidative stress, and decreased levels of protective antioxidant enzymes in patients with rheumatoid arthritis (RA). An enriched diet containing antioxidants, such as vitamin E, vitamin C, β-carotene and phenolic substances, has been suggested to improve symptoms by reducing disease-related oxidative stress. In this respect, the marine world represents a largely untapped reserve of bioactive ingredients, and considerable potential exists for exploitation of these bioactives as functional food ingredients. Substances such as n-3 oils, carotenoids, vitamins, minerals and peptides provide a myriad of health benefits, including reduction of cardiovascular diseases, anticarcinogenic and anti-inflammatory activities. New marine bioactives are recently gaining attention, since they could be helpful in combating chronic inflammatory degenerative conditions. The aim of this review is to examine the published studies concerning the potential pharmacological properties and application of many marine bioactives against inflammatory diseases. PMID:22690145

The antimicrobial activity of heterotrophic bacteria isolated from the marine sponge Erylus deficiens (Astrophorida, Geodiidae)

PubMed Central

Graça, Ana Patrícia; Viana, Flávia; Bondoso, Joana; Correia, Maria Inês; Gomes, Luis; Humanes, Madalena; Reis, Alberto; Xavier, Joana R.; Gaspar, Helena; Lage, Olga M.

2015-01-01

Interest in the study of marine sponges and their associated microbiome has increased both for ecological reasons and for their great biotechnological potential. In this work, heterotrophic bacteria associated with three specimens of the marine sponge Erylus deficiens, were isolated in pure culture, phylogenetically identified and screened for antimicrobial activity. The isolation of bacteria after an enrichment treatment in heterotrophic medium revealed diversity in bacterial composition with only Pseudoalteromonas being shared by two specimens. Of the 83 selected isolates, 58% belong to Proteobacteria, 23% to Actinobacteria and 19% to Firmicutes. Diffusion agar assays for bioactivity screening against four bacterial strains and one yeast, revealed that a high number of the isolated bacteria (68.7%) were active, particularly against Candida albicans and Vibrio anguillarum. Pseudoalteromonas, Microbacterium, and Proteus were the most bioactive genera. After this preliminary screening, the bioactive strains were further evaluated in liquid assays against C. albicans, Bacillus subtilis and Escherichia coli. Filtered culture medium and acetone extracts from three and 5 days-old cultures were assayed. High antifungal activity against C. albicans in both aqueous and acetone extracts as well as absence of activity against B. subtilis were confirmed. Higher levels of activity were obtained with the aqueous extracts when compared to the acetone extracts and differences were also observed between the 3 and 5 day-old extracts. Furthermore, a low number of active strains was observed against E. coli. Potential presence of type-I polyketide synthases (PKS-I) and non-ribosomal peptide synthetases (NRPSs) genes were detected in 17 and 30 isolates, respectively. The high levels of bioactivity and the likely presence of associated genes suggest that Erylus deficiens bacteria are potential sources of novel marine bioactive compounds. PMID:25999928

One-step synthesis of bioactive glass by spray pyrolysis

NASA Astrophysics Data System (ADS)

Shih, Shao-Ju; Chou, Yu-Jen; Chien, I.-Chen

2012-12-01

Bioactive glasses (BGs) have recently received more attention from biologists and engineers because of their potential applications in bone implants. The sol-gel process is one of the most popular methods for fabricating BGs, and has been used to produce BGs for years. However, the sol-gel process has the disadvantages of discontinuous processing and a long processing time. This study presented a one-step spray pyrolysis (SP) synthesis method to overcome these disadvantages. This SP method has synthesized spherical bioactive glass (SBG) and mesoporous bioactive glass (MBG) particles using Si-, Ca- and P-based precursors. This study used transmission electron microscopy, selected area electron diffraction and X-ray dispersive spectroscopy to characterize the microstructure, crystallographic structure, and chemical composition for the BG particles. In addition, in vitro bioactive tests showed the formation of hydroxyl apatite layers on SBG and MBG particles after immersion in simulated body fluid for 5 h. Experimental results show the SP formation mechanisms of SBG and MBG particles.

Therapeutic potential of dairy bioactive peptides: A contemporary perspective.

PubMed

Sultan, Saira; Huma, Nuzhat; Butt, Masood Sadiq; Aleem, Muhammad; Abbas, Munawar

2018-01-02

Dairy products are associated with numerous health benefits. These are a good source of nutrients such as carbohydrates, protein (bioactive peptides), lipids, minerals, and vitamins, which are essential for growth, development, and maintenance of the human body. Accordingly, dairy bioactive peptides are one of the targeted compounds present in different dairy products. Dairy bioactive compounds can be classified as antihypertensive, anti-oxidative, immmunomodulant, anti-mutagenic, antimicrobial, opoid, anti-thrombotic, anti-obesity, and mineral-binding agents, depending upon biological functions. These bioactive peptides can easily be produced by enzymatic hydrolysis, and during fermentation and gastrointestinal digestion. For this reason, fermented dairy products, such as yogurt, cheese, and sour milk, are gaining popularity worldwide, and are considered excellent source of dairy peptides. Furthermore, fermented and non-fermented dairy products are associated with lower risks of hypertension, coagulopathy, stroke, and cancer insurgences. The current review article is an attempt to disseminate general information about dairy peptides and their health claims to scientists, allied stakeholders, and, certainly, readers.

Simultaneous Delivery of Highly Diverse Bioactive Compounds from Blend Electrospun Fibers for Skin Wound Healing.

PubMed

Peh, Priscilla; Lim, Natalie Sheng Jie; Blocki, Anna; Chee, Stella Min Ling; Park, Heyjin Chris; Liao, Susan; Chan, Casey; Raghunath, Michael

2015-07-15

Blend emulsion electrospinning is widely perceived to destroy the bioactivity of proteins, and a blend emulsion of water-soluble and nonsoluble molecules is believed to be thermodynamically unstable to electrospin smoothly. Here we demonstrate a method to retain the bioactivity of disparate fragile biomolecules when electrospun. Using bovine serum albumin as a carrier protein; water-soluble vitamin C, fat soluble vitamin D3, steroid hormone hydrocortisone, peptide hormone insulin, thyroid hormone triiodothyronine (T3), and peptide epidermal growth factor (EGF) were simultaneously blend-spun into PLGA-collagen nanofibers. Upon release, vitamin C maintained the ability to facilitate Type I collagen secretion by fibroblasts, EGF stimulated skin fibroblast proliferation, and insulin potentiated adipogenic differentiation. Transgenic cell reporter assays confirmed the bioactivity of vitamin D3, T3, and hydrocortisone. These factors concertedly increased keratinocyte and fibroblast proliferation while maintaining keratinocyte basal state. This method presents an elegant solution to simultaneously deliver disparate bioactive biomolecules for wound healing applications.

Toughening and functionalization of bioactive ceramic and glass bone scaffolds by biopolymer coatings and infiltration: a review of the last 5 years.

PubMed

Philippart, Anahí; Boccaccini, Aldo R; Fleck, Claudia; Schubert, Dirk W; Roether, Judith A

2015-01-01

Inorganic scaffolds with high interconnected porosity based on bioactive glasses and ceramics are prime candidates for applications in bone tissue engineering. These materials however exhibit relatively low fracture strength and high brittleness. A simple and effective approach to improve the toughness is to combine the basic scaffold structure with polymer coatings or through the formation of interpenetrating polymer-bioactive ceramic microstructures. The polymeric phase can additionally serve as a carrier for growth factors and therapeutic drugs, thus adding biological functionalities. The present paper reviews the state-of-the art in the field of polymer coated and infiltrated bioactive inorganic scaffolds. Based on the notable combination of bioactivity, improved mechanical properties and drug or growth factor delivery capability, this scaffold type is a candidate for bone and osteochondral regeneration strategies. Remaining challenges for the improvement of the materials are discussed and opportunities to broaden the application potential of this scaffold type are also highlighted.

In situ regeneration of bioactive coatings enabled by an evolved Staphylococcus aureus sortase A

NASA Astrophysics Data System (ADS)

Ham, Hyun Ok; Qu, Zheng; Haller, Carolyn A.; Dorr, Brent M.; Dai, Erbin; Kim, Wookhyun; Liu, David R.; Chaikof, Elliot L.

2016-04-01

Surface immobilization of bioactive molecules is a central paradigm in the design of implantable devices and biosensors with improved clinical performance capabilities. However, in vivo degradation or denaturation of surface constituents often limits the long-term performance of bioactive films. Here we demonstrate the capacity to repeatedly regenerate a covalently immobilized monomolecular thin film of bioactive molecules through a two-step stripping and recharging cycle. Reversible transpeptidation by a laboratory evolved Staphylococcus aureus sortase A (eSrtA) enabled the rapid immobilization of an anti-thrombogenic film in the presence of whole blood and permitted multiple cycles of film regeneration in vitro that preserved its biological activity. Moreover, eSrtA transpeptidation facilitated surface re-engineering of medical devices in situ after in vivo implantation through removal and restoration film constituents. These studies establish a rapid, orthogonal and reversible biochemical scheme to regenerate selective molecular constituents with the potential to extend the lifetime of bioactive films.

Natural bioactive compounds from winery by-products as health promoters: a review.

PubMed

Teixeira, Ana; Baenas, Nieves; Dominguez-Perles, Raul; Barros, Ana; Rosa, Eduardo; Moreno, Diego A; Garcia-Viguera, Cristina

2014-09-04

The relevance of food composition for human health has increased consumers' interest in the consumption of fruits and vegetables, as well as foods enriched in bioactive compounds and nutraceuticals. This fact has led to a growing attention of suppliers on reuse of agro-industrial wastes rich in healthy plant ingredients. On this matter, grape has been pointed out as a rich source of bioactive compounds. Currently, up to 210 million tons of grapes (Vitis vinifera L.) are produced annually, being the 15% of the produced grapes addressed to the wine-making industry. This socio-economic activity generates a large amount of solid waste (up to 30%, w/w of the material used). Winery wastes include biodegradable solids namely stems, skins, and seeds. Bioactive compounds from winery by-products have disclosed interesting health promoting activities both in vitro and in vivo. This is a comprehensive review on the phytochemicals present in winery by-products, extraction techniques, industrial uses, and biological activities demonstrated by their bioactive compounds concerning potential for human health.

A Comprehensive Strategy to Evaluate Compatible Stability of Chinese Medicine Injection and Infusion Solutions Based on Chemical Analysis and Bioactivity Assay.

PubMed

Li, Jian-Ping; Liu, Yang; Guo, Jian-Ming; Shang, Er-Xin; Zhu, Zhen-Hua; Zhu, Kevin Y; Tang, Yu-Ping; Zhao, Bu-Chang; Tang, Zhi-Shu; Duan, Jin-Ao

2017-01-01

Stability of traditional Chinese medicine injection (TCMI) is an important issue related with its clinical application. TCMI is composed of multi-components, therefore, when evaluating TCMI stability, several marker compounds cannot represent global components or biological activities of TCMI. Till now, when evaluating TCMI stability, method involving the global components or biological activities has not been reported. In this paper, we established a comprehensive strategy composed of three different methods to evaluate the chemical and biological stability of a typical TCMI, Danhong injection (DHI). UHPLC-TQ/MS was used to analyze the stability of marker compounds (SaA, SaB, RA, DSS, PA, CA, and SG) in DHI, UHPLC-QTOF/MS was used to analyze the stability of global components (MW 80-1000 Da) in DHI, and cell based antioxidant capability assay was used to evaluate the bioactivity of DHI. We applied this strategy to assess the compatible stability of DHI and six infusion solutions (GS, NS, GNS, FI, XI, and DGI), which were commonly used in combination with DHI in clinic. GS was the best infusion solution for DHI, and DGI was the worst one based on marker compounds analysis. Based on global components analysis, XI and DGI were the worst infusion solutions for DHI. And based on bioactivity assay, GS was the best infusion solution for DHI, and XI was the worst one. In conclusion, as evaluated by the established comprehensive strategy, GS was the best infusion solution, however, XI and DGI were the worst infusion solutions for DHI. In the compatibility of DHI and XI or DGI, salvianolic acids in DHI would be degraded, resulting in the reduction of original composition and generation of new components, and leading to the changes of biological activities. This is the essence of instability compatibility of DHI and some infusion solutions. Our study provided references for choosing the reasonable infusion solutions for DHI, which could contribute the improvement of safety and efficacy of DHI. Moreover, the established strategy may be applied for the compatible stability evaluation of other TCMIs.

Phylogenetic diversity of culturable endophytic fungi in Dongxiang wild rice (Oryza rufipogon Griff), detection of polyketide synthase gene and their antagonistic activity analysis.

PubMed

Wang, Ya; Gao, Bo Liang; Li, Xi Xi; Zhang, Zhi Bin; Yan, Ri Ming; Yang, Hui Lin; Zhu, Du

2015-11-01

The biodiversity of plant endophytic fungi is enormous, numerous competent endophytic fungi are capable of providing different forms of fitness benefits to host plants and also could produce a wide array of bioactive natural products, which make them a largely unexplored source of novel compounds with potential bioactivity. In this study, we provided a first insights into revealing the diversity of culturable endophytic fungi in Dongxiang wild rice (Oryza rufipogon Griff.) from China using rDNA-ITS phylogenetic analysis. Here, the potential of fungi in producing bioactive natural products was estimated based on the beta-ketosynthase detected in the polyketide synthase (PKS) gene cluster and on the bioassay of antagonistic activity against two rice phytopathogens Thanatephorus cucumeris and Xanthomonas oryzae. A total of 229 endophytic fungal strains were validated in 19 genera. Among the 24 representative strains, 13 strains displayedantagonistic activity against the phytopathogens. Furthermore, PKS genes were detected in 9 strains, indicating their potential for synthesising PKS compounds. Our study confirms the phylogenetic diversity of endophytic fungi in O. rufipogon G. and highlights that endophytic fungi are not only promising resources of biocontrol agents against phytopathogens of rice plants, but also of bioactive natural products and defensive secondary metabolites. Copyright © 2015 The British Mycological Society. Published by Elsevier Ltd. All rights reserved.

Membrane mimetic surface functionalization of nanoparticles: Methods and applications

PubMed Central

Weingart, Jacob; Vabbilisetty, Pratima; Sun, Xue-Long

2013-01-01

Nanoparticles (NPs), due to their size-dependent physical and chemical properties, have shown remarkable potential for a wide range of applications over the past decades. Particularly, the biological compatibilities and functions of NPs have been extensively studied for expanding their potential in areas of biomedical application such as bioimaging, biosensing, and drug delivery. In doing so, surface functionalization of NPs by introducing synthetic ligands and/or natural biomolecules has become a critical component in regards to the overall performance of the NP system for its intended use. Among known examples of surface functionalization, the construction of an artificial cell membrane structure, based on phospholipids, has proven effective in enhancing biocompatibility and has become a viable alternative to more traditional modifications, such as direct polymer conjugation. Furthermore, certain bioactive molecules can be immobilized onto the surface of phospholipid platforms to generate displays more reminiscent of cellular surface components. Thus, NPs with membrane-mimetic displays have found use in a range of bioimaging, biosensing, and drug delivery applications. This review herein describes recent advances in the preparations and characterization of integrated functional NPs covered by artificial cell membrane structures and their use in various biomedical applications. PMID:23688632

Phenolics from Garcinia mangostana alleviate exaggerated vasoconstriction in metabolic syndrome through direct vasodilatation and nitric oxide generation.

PubMed

Abdallah, Hossam M; El-Bassossy, Hany M; Mohamed, Gamal A; El-Halawany, Ali M; Alshali, Khalid Z; Banjar, Zainy M

2016-09-13

Exaggerated vasoconstriction plays a very important role in the hypertension, a major component of metabolic syndrome (MetS). In the current work, the potential protective effect of methanol extract of fruit hulls of Garcinia mangostana L. on the exaggerated vasoconstriction in MetS has been investigated. In addition, the bioactive fraction and compounds as well as the possible mechanism of action have been illustrated. The effect of methanol extract of G. mangostana (GMT) fruit hulls on the vascular reactivity of aorta isolated from animals with MetS was investigated through bioassay-guided fractionation procedures. GMT was partitioned with chloroform (I) and the remaining mother liquor was fractionated on a Diaion HP-20 with H2O, 50 and 100 % methanol to give fractions II, III, and IV, respectively. The effect of total extract (GMT), bioactive fraction and the bioactive compounds on the vasoconstriction were examined in aortae isolated from animals with MetS by incubation for 30 min before exposing aortae to cumulative concentrations of phenylephrine (PE). The direct relaxant effect was also examined by adding cumulative concentrations of the bioactive fraction and its bioactive compounds to PE precontracted vessels. In addition, aortic nitric oxide (NO) and reactive oxygen species (ROS) production was investigated. Bioassay-guided fractionation of GMT revealed isolation of garcimangosone D (1), aromadendrin-8-C-β-D-glucopyranoside (2), 2,4,3'-trihydroxy benzophenone-6-O-β-D-glucopyranoside (3), maclurin-6-O-β-D-glucopyranoside (rhodanthenone) (4), epicatechin (5), and 2,3',4,5',6-pentahydroxy benzophenone (6). Only compounds 2, 4, and 5 significantly alleviated the exaggerated vasoconstriction of MetS aortae and in the same time showed significant vasodilation of PE pre-contracted aortae. To further illustrate the mechanism of action, the observed vasodilation was completely blocked by the nitric oxide (NO) synthase inhibitor, Nω-nitro-L-arginine methyl ester hydrochloride and inhibited by guanylate cyclase inhibitor, methylene blue. However, vasodilation was not affected by the potassium channel blocker, tetraethylammonium or the cyclooxygenase inhibitor, indomethacin. In addition, compounds 2, 4, and 5 stimulated NO generation from isolated aortae to levels comparable with acetylcholine. Furthermore, 4 and 5 inhibited reactive oxygen species generation in MetS aortae. The phenolic compounds 2, 4, and 5 ameliorated the exaggerated vasoconstriction in MetS aortae through vasodilatation-NO generation mechanism.

Sulfur and sulfur nanoparticles as potential antimicrobials: from traditional medicine to nanomedicine.

PubMed

Rai, Mahendra; Ingle, Avinash P; Paralikar, Priti

2016-10-01

The alarming rate of infections caused by various pathogens and development of their resistance towards a large number of antimicrobial agents has generated an essential need to search for novel and effective antimicrobial agents. Metal nanoparticles such as silver have been widely used and accepted as strong antimicrobial agents, but considering the cost effectiveness and significant bioactivities, researchers are looking to utilize sulfur nanoparticles as an effective alternative to silver nanoparticles. This review has been focused on different approaches for the synthesis of sulfur nanoparticles, their broad spectrum bioactivities and possible mechanisms involved in their bioactivities. Expert commentary: Sulfur nanoparticles are reported to possess broad spectrum antimicrobial activity, and hence can be used to treat microbial infections and potentially tackle the problem of antibiotic resistance. Thus, in the future, sulfur nanoparticles can be used as an effective, non-toxic and economically viable alternative to other precious metal nanoparticles.

Potential of Bioactive Glasses for Cardiac and Pulmonary Tissue Engineering

PubMed Central

Hamzehlou, Sepideh

2017-01-01

Repair and regeneration of disorders affecting cardiac and pulmonary tissues through tissue-engineering-based approaches is currently of particular interest. On this matter, different families of bioactive glasses (BGs) have recently been given much consideration with respect to treating refractory diseases of these tissues, such as myocardial infarction. The inherent properties of BGs, including their ability to bond to hard and soft tissues, to stimulate angiogenesis, and to elicit antimicrobial effects, along with their excellent biocompatibility, support these newly proposed strategies. Moreover, BGs can also act as a bioactive reinforcing phase to finely tune the mechanical properties of polymer-based constructs used to repair the damaged cardiac and pulmonary tissues. In the present study, we evaluated the potential of different forms of BGs, alone or in combination with other materials (e.g., polymers), in regards to repair and regenerate injured tissues of cardiac and pulmonary systems. PMID:29244726

Bioactive compounds and encapsulation of Yanang (Tiliacora triandra) leaves.

PubMed

Singthong, Jittra; Oonsivilai, Ratchadaporn; Oonmetta-Aree, Jirawan; Ningsanond, Suwayd

2014-01-01

Yanang (Tiliacora triandra) has been known as vegetable and herbal in northeast Thailand and Lao People's Democratic Republic. Extracts from Yanang leaves contain high amounts of polyphenol constituents possessing antioxidant activity. This work investigated bioactive compounds of Yanang extracts prepared by infusion with water, ethanol and acetone. Furthermore, this paper reports the design of the experimental method for optimization of Yanang encapsulation using three independent variables: the ratio of core material (Yanang), to wall material (gum Arabic), gum Arabic concentration and inlet temperature of spray drying on bioactive compounds stability. The stability of bioactive compounds was evaluated using phenolic compounds, total antioxidant, carotenoids and chlorophyll. The study of the bioactivity of Yanang extracts found that extraction with water was the appropriate application. The study of Yanang encapsulation demonstrated that gum Arabic, as coating agents, protected bioactive compounds of Yanang. Optimized condition for the encapsulation was at the ratio of core to wall {1:4}, in gum Arabic concentration 10% (w/v), and inlet temperature at 160▯C. The results show that the bioactive compounds were mainly affected by the ratio of core to wall material. Besides, moisture content and particle size of encapsulation depend on inlet temperature of spray drying, and gum Arabic concentration, respectively. This optimization reveals that the encapsulation process did not lose the bioactive compounds. Yanang extract with water was the main phenolic compound and showed high antioxidant activities. This study demonstrates the potentials of using spray drying process and optimization for the encapsulation of herbal products.

Genome analysis of Daldinia eschscholtzii strains UM 1400 and UM 1020, wood-decaying fungi isolated from human hosts

DOE Office of Scientific and Technical Information (OSTI.GOV)

Chan, Chai Ling; Yew, Su Mei; Ngeow, Yun Fong

Background: Daldinia eschscholtzii is a wood-inhabiting fungus that causes wood decay under certain conditions. It has a broad host range and produces a large repertoire of potentially bioactive compounds. However, there is no extensive genome analysis on this fungal species. Results: Two fungal isolates (UM 1400 and UM 1020) from human specimens were identified as Daldinia eschscholtzii by morphological features and ITS-based phylogenetic analysis. Both genomes were similar in size with 10,822 predicted genes in UM 1400 (35.8 Mb) and 11,120 predicted genes in UM 1020 (35.5 Mb). A total of 751 gene families were shared among both UM isolates,more » including gene families associated with fungus-host interactions. In the CAZyme comparative analysis, both genomes were found to contain arrays of CAZyme related to plant cell wall degradation. Genes encoding secreted peptidases were found in the genomes, which encode for the peptidases involved in the degradation of structural proteins in plant cell wall. In addition, arrays of secondary metabolite backbone genes were identified in both genomes, indicating of their potential to produce bioactive secondary metabolites. Both genomes also contained an abundance of gene encoding signaling components, with three proposed MAPK cascades involved in cell wall integrity, osmoregulation, and mating/filamentation. Besides genomic evidence for degrading capability, both isolates also harbored an array of genes encoding stress response proteins that are potentially significant for adaptation to living in the hostile environments. In conclusion: Our genomic studies provide further information for the biological understanding of the D. eschscholtzii and suggest that these wood-decaying fungi are also equipped for adaptation to adverse environments in the human host.« less

Antioxidant and antifungal potential of methanol extracts of Phellinus spp. from Sonora, Mexico.

PubMed

Ayala-Zavala, Jesús Fernando; Silva-Espinoza, Brenda Adriana; Cruz-Valenzuela, Manuel Reynaldo; Villegas-Ochoa, Mónica Alejandra; Esqueda, Martín; González-Aguilar, Gustavo Adolfo; Calderón-López, Yazaric

2012-01-01

Among the potential natural sources of bioactive compounds, those of the macroscopic fungi Phellinus spp. have been identified by previous researches. Phenolic compounds are among the major antioxidant and antimicrobial contributors due to their bioactive properties. The goal of this study was to determine the total phenolic and flavonoid contents, and its relation with the antioxidant and antifungal activity of methanolic extracts of Phellinus gilvus, Phellinus rimosus and Phellinus badius, respectively. The collected and identified organisms of Phellinus spp. were treated with methanol and the generated aqueous extract was analyzed to quantified total phenolic compounds, total flavonoids, radical scavenging activity against DPPH, trolox equivalent antioxidant capacity, and oxygen absorbance capacity. The antifungal property of the extracts was evaluated against Alternaria alternata. The content of phenolic compounds was of 49.31, 46.51 and 44.7 mg of gallic acid equivalents/g, for P. gilvus, P. rimosus and P. badius, respectively. The total flavonoid content followed the same pattern with values of 30.58, 28, and 26.48 mg of quercetin equivalents/g for P. gilvus, P. rimosus and P. badius, respectively. The variation on the content of phenolic components was reflected on the antioxidant activity of every organism. The antioxidant activity ranked as follows: P. gilvus>P. rimosus>P. badius. The antifungal effect of the different extracts against A. alternata showed a significant effect, all of them, inhibiting the growth of this pathogen. P. gilvus showed the best potential to inactivate free radicals, being all the tested fungi effective to inhibit A. alternata growth. Copyright © 2011 Revista Iberoamericana de Micología. Published by Elsevier Espana. All rights reserved.

Genome analysis of Daldinia eschscholtzii strains UM 1400 and UM 1020, wood-decaying fungi isolated from human hosts

DOE PAGES

Chan, Chai Ling; Yew, Su Mei; Ngeow, Yun Fong; ...

2015-11-18

Background: Daldinia eschscholtzii is a wood-inhabiting fungus that causes wood decay under certain conditions. It has a broad host range and produces a large repertoire of potentially bioactive compounds. However, there is no extensive genome analysis on this fungal species. Results: Two fungal isolates (UM 1400 and UM 1020) from human specimens were identified as Daldinia eschscholtzii by morphological features and ITS-based phylogenetic analysis. Both genomes were similar in size with 10,822 predicted genes in UM 1400 (35.8 Mb) and 11,120 predicted genes in UM 1020 (35.5 Mb). A total of 751 gene families were shared among both UM isolates,more » including gene families associated with fungus-host interactions. In the CAZyme comparative analysis, both genomes were found to contain arrays of CAZyme related to plant cell wall degradation. Genes encoding secreted peptidases were found in the genomes, which encode for the peptidases involved in the degradation of structural proteins in plant cell wall. In addition, arrays of secondary metabolite backbone genes were identified in both genomes, indicating of their potential to produce bioactive secondary metabolites. Both genomes also contained an abundance of gene encoding signaling components, with three proposed MAPK cascades involved in cell wall integrity, osmoregulation, and mating/filamentation. Besides genomic evidence for degrading capability, both isolates also harbored an array of genes encoding stress response proteins that are potentially significant for adaptation to living in the hostile environments. In conclusion: Our genomic studies provide further information for the biological understanding of the D. eschscholtzii and suggest that these wood-decaying fungi are also equipped for adaptation to adverse environments in the human host.« less

TBC2health: a database of experimentally validated health-beneficial effects of tea bioactive compounds.

PubMed

Zhang, Shihua; Xuan, Hongdong; Zhang, Liang; Fu, Sicong; Wang, Yijun; Yang, Hua; Tai, Yuling; Song, Youhong; Zhang, Jinsong; Ho, Chi-Tang; Li, Shaowen; Wan, Xiaochun

2017-09-01

Tea is one of the most consumed beverages in the world. Considerable studies show the exceptional health benefits (e.g. antioxidation, cancer prevention) of tea owing to its various bioactive components. However, data from these extensively published papers had not been made available in a central database. To lay a foundation in improving the understanding of healthy tea functions, we established a TBC2health database that currently documents 1338 relationships between 497 tea bioactive compounds and 206 diseases (or phenotypes) manually culled from over 300 published articles. Each entry in TBC2health contains comprehensive information about a bioactive relationship that can be accessed in three aspects: (i) compound information, (ii) disease (or phenotype) information and (iii) evidence and reference. Using the curated bioactive relationships, a bipartite network was reconstructed and the corresponding network (or sub-network) visualization and topological analyses are provided for users. This database has a user-friendly interface for entry browse, search and download. In addition, TBC2health provides a submission page and several useful tools (e.g. BLAST, molecular docking) to facilitate use of the database. Consequently, TBC2health can serve as a valuable bioinformatics platform for the exploration of beneficial effects of tea on human health. TBC2health is freely available at http://camellia.ahau.edu.cn/TBC2health. © The Author 2016. Published by Oxford University Press.

Beneficial Effects of Cinnamon on the Metabolic Syndrome, Inflammation, and Pain, and Mechanisms Underlying These Effects – A Review

PubMed Central

Shen, Yan; Jia, Liu-Nan; Honma, Natsumi; Hosono, Takashi; Ariga, Toyohiko; Seki, Taiichiro

2012-01-01

Cinnamon is one of the most important herbal drugs and has been widely used in Asia for more than 4000 years. As a folk medicine, cinnamon has been traditionally applied to the treatment of inflammatory disorders and gastric diseases. After chemical profiling of cinnamon's components, their biological activities including antimicrobial, antiviral, antioxidant, antitumor, antihypertension, antilipemic, antidiabetes, gastroprotective and immunomodulatory were reported by many investigators. As a result, current studies have been performed mostly focusing on the bioactivity of cinnamon toward the recently generalized metabolic syndrome involving diabetes. In this review article, we provide an overview of the recent literature describing cinnamon's potential for preventing the metabolic syndrome. PMID:24716111

Functional components and medicinal properties of food: a review.

PubMed

Abuajah, Christian Izuchukwu; Ogbonna, Augustine Chima; Osuji, Chijioke Maduka

2015-05-01

Research has proved a relationship between functional components of food, health and well-being. Thus, functional components of food can be effectively applied in the treatment and prevention of diseases. They act simultaneously at different or identical target sites with the potential to impart physiological benefits and promotion of wellbeing including reducing the risk of cancer, cardiovascular disease, osteoporosis, inflammation, type II diabetes, and other chronic degenerative diseases, lowering of blood cholesterol, neutralization of reactive oxygen species and charged radicals, anticarcinogenic effect, low-glycaemic response, etc. Previously, it was thought that functional ingredients such as non-starchy carbohydrates including soluble and insoluble dietary fibres, fucoidan; antioxidants including polyphenols, carotenoids, tocopherols, tocotrienols, phytosterols, isoflavones, organosulphur compounds; plant sterols and soy phytoestrogens occur only in plant foods (whole grains, fruits, and vegetables) as phytochemicals. However, probiotics, prebiotics, conjugated linolenic acid, long-chain omega-3, -6 and -9-polyunsaturated fatty acids, and bioactive peptides have proved that functional components are equally available in animal products such as milk, fermented milk products and cold-water fish. The way a food is processed affects its functional components. Many processing techniques have been found to lower the concentration of functional components in food. Conversely, other techniques were found to increase them. Hence, in a time when the role of a healthy diet in preventing non-communicable diseases is well accepted, the borderline between food and medicine is becoming very thin.

High-throughput in Vitro Data To Inform Prioritization of Ambient Water Monitoring and Testing for Endocrine Active Chemicals.

PubMed

Heiger-Bernays, Wendy J; Wegner, Susanna; Dix, David J

2018-01-16

The presence of industrial chemicals, consumer product chemicals, and pharmaceuticals is well documented in waters in the U.S. and globally. Most of these chemicals lack health-protective guidelines and many have been shown to have endocrine bioactivity. There is currently no systematic or national prioritization for monitoring waters for chemicals with endocrine disrupting activity. We propose ambient water bioactivity concentrations (AWBCs) generated from high throughput data as a health-based screen for endocrine bioactivity of chemicals in water. The U.S. EPA ToxCast program has screened over 1800 chemicals for estrogen receptor (ER) and androgen receptor (AR) pathway bioactivity. AWBCs are calculated for 110 ER and 212 AR bioactive chemicals using high throughput ToxCast data from in vitro screening assays and predictive pathway models, high-throughput toxicokinetic data, and data-driven assumptions about consumption of water. Chemical-specific AWBCs are compared with measured water concentrations in data sets from the greater Denver area, Minnesota lakes, and Oregon waters, demonstrating a framework for identifying endocrine bioactive chemicals. This approach can be used to screen potential cumulative endocrine activity in drinking water and to inform prioritization of future monitoring, chemical testing and pollution prevention efforts.

Sphingoid esters from the molecular distillation of squid oil: A preliminary bioactivity determination.

PubMed

Saliu, Francesco; Longhin, Eleonora; Salanti, Anika; Degano, Ilaria; Della Pergola, Roberto

2016-06-15

A mixture of sphingoid esters was isolated (1.4% w/w) from the molecular distillation of crude squid visceral oil. A preliminary investigation on the bioactivity profile and toxic potential of this residue was carried out by in vitro experiments. No cytotoxicity and a moderate lipase inhibition activity were highlighted. Copyright © 2016 Elsevier Ltd. All rights reserved.

Design of cinnamaldehyde amino acid Schiff base compounds based on the quantitative structure–activity relationship

Treesearch

Hui Wang; Mingyue Jiang; Shujun Li; Chung-Yun Hse; Chunde Jin; Fangli Sun; Zhuo Li

2017-01-01

Cinnamaldehyde amino acid Schiff base (CAAS) is a new class of safe, bioactive compounds which could be developed as potential antifungal agents for fungal infections. To design new cinnamaldehyde amino acid Schiff base compounds with high bioactivity, the quantitative structure–activity relationships (QSARs) for CAAS compounds against Aspergillus niger (A. niger) and...