The protective effect of some Thai plants and their bioactive compounds in UV light-induced skin carcinogenesis.

PubMed

de Silva, Madhura B; Tencomnao, Tewin

2018-05-02

Skin cancer, represents a major public health concern. While the vast majority is non-melanoma skin cancers, melanomas are mostly responsible for mortality. Solar UVB radiation is mutagenic and carcinogenic. It is primarily responsible for both non-melanoma and melanoma skin cancers via excessive production of reactive oxygen species (ROS), which mediate changes in inflammation and immunity, and have been implicated in all three stages of skin cancer development. Due to their regulatory role in numerous functions of cells, signaling pathways are targets for chemoprevention. The current standards in melanoma therapy are targeted and combination therapies, which, albeit prolong survival responses, are still prone to development of drug resistance. To this extent, drugs of natural origin continue to spark great interest. Thailand has a rich biodiversity of indigenous flora, which have traditionally been used to treat a variety of pathologies. The active components in plant extracts that have medicinal properties, termed 'bioactive compounds,' are efficient chemopreventive agents due to their antioxidant, antimutagenic, anticarcinogenic, and carcinogen detoxification properties. Thai plants and their bioactive compounds have shown protective effects on UV light-induced skin cancer in different experimental models. This warrants further in vivo investigations and translation to clinical studies to determine efficacy and safety, for use as lead compounds in targeted/combination therapy or adjuvant therapy with existing regimes. Coupled with a strategy for prevention, this offers a promising outlook for protection against photocarcinogenesis. Copyright © 2018 Elsevier B.V. All rights reserved.

Profiling the Oxylipin and Endocannabinoid Metabolome by UPLC-ESI-MS/MS in Human Plasma to Monitor Postprandial Inflammation.

PubMed

Gouveia-Figueira, Sandra; Späth, Jana; Zivkovic, Angela M; Nording, Malin L

2015-01-01

Bioactive lipids, including oxylipins, endocannabinoids, and related compounds may function as specific biochemical markers of certain aspects of inflammation. However, the postprandial responsiveness of these compounds is largely unknown; therefore, changes in the circulating oxylipin and endocannabinoid metabolome in response to a challenge meal were investigated at six occasions in a subject who freely modified her usual diet. The dietary change, and especially the challenge meal itself, represented a modification of precursor fatty acid status, with expectedly subtle effects on bioactive lipid levels. To detect even the slightest alteration, highly sensitive ultra-performance liquid chromatography (UPLC) coupled to electrospray ionization (ESI) tandem mass spectrometry (MS/MS) methods for bioactive lipid profiling was employed. A previously validated UPLC-ESI-MS/MS method for profiling the endocannabinoid metabolome was used, while validation of an UPLC-ESI-MS/MS method for oxylipin analysis was performed with acceptable outcomes for a majority of the parameters according to the US Food and Drug Administration guidelines for linearity (0.9938 < R2 < 0.9996), limit of detection (0.0005-2.1 pg on column), limit of quantification (0.0005-4.2 pg on column), inter- and intraday accuracy (85-115%) and precision (< 5%), recovery (40-109%) and stability (40-105%). Forty-seven of fifty-two bioactive lipids were detected in plasma samples at fasting and in the postprandial state (0.5, 1, and 3 hours after the meal). Multivariate analysis showed a significant shift of bioactive lipid profiles in the postprandial state due to inclusion of dairy products in the diet, which was in line with univariate analysis revealing seven compounds (NAGly, 9-HODE, 13-oxo-ODE, 9(10)-EpOME, 12(13)-EpOME, 20-HETE, and 11,12-DHET) that were significantly different between background diets in the postprandial state (but not at fasting). The only change in baseline levels at fasting was displayed by TXB2. Furthermore, postprandial responsiveness was detected for seven compounds (POEA, SEA, 9(10)-DiHOME, 12(13)-DiHOME, 13-oxo-ODE, 9-HODE, and 13-HODE). Hence, the data confirm that the UPLC-ESI-MS/MS method performance was sufficient to detect i) a shift, in the current case most notably in the postprandial bioactive lipid metabolome, caused by changes in diet and ii) responsiveness to a challenge meal for a subset of the oxylipin and endocannabinoid metabolome. To summarize, we have shown proof-of-concept of our UPLC-ESI-MS/MS bioactive lipid protocols for the purpose of monitoring subtle shifts, and thereby useful to address lipid-mediated postprandial inflammation.

Profiling the Oxylipin and Endocannabinoid Metabolome by UPLC-ESI-MS/MS in Human Plasma to Monitor Postprandial Inflammation

PubMed Central

Gouveia-Figueira, Sandra; Späth, Jana; Zivkovic, Angela M.; Nording, Malin L.

2015-01-01

Bioactive lipids, including oxylipins, endocannabinoids, and related compounds may function as specific biochemical markers of certain aspects of inflammation. However, the postprandial responsiveness of these compounds is largely unknown; therefore, changes in the circulating oxylipin and endocannabinoid metabolome in response to a challenge meal were investigated at six occasions in a subject who freely modified her usual diet. The dietary change, and especially the challenge meal itself, represented a modification of precursor fatty acid status, with expectedly subtle effects on bioactive lipid levels. To detect even the slightest alteration, highly sensitive ultra-performance liquid chromatography (UPLC) coupled to electrospray ionization (ESI) tandem mass spectrometry (MS/MS) methods for bioactive lipid profiling was employed. A previously validated UPLC-ESI-MS/MS method for profiling the endocannabinoid metabolome was used, while validation of an UPLC-ESI-MS/MS method for oxylipin analysis was performed with acceptable outcomes for a majority of the parameters according to the US Food and Drug Administration guidelines for linearity (0.9938 < R2 < 0.9996), limit of detection (0.0005–2.1 pg on column), limit of quantification (0.0005–4.2 pg on column), inter- and intraday accuracy (85–115%) and precision (< 5%), recovery (40–109%) and stability (40–105%). Forty-seven of fifty-two bioactive lipids were detected in plasma samples at fasting and in the postprandial state (0.5, 1, and 3 hours after the meal). Multivariate analysis showed a significant shift of bioactive lipid profiles in the postprandial state due to inclusion of dairy products in the diet, which was in line with univariate analysis revealing seven compounds (NAGly, 9-HODE, 13-oxo-ODE, 9(10)-EpOME, 12(13)-EpOME, 20-HETE, and 11,12-DHET) that were significantly different between background diets in the postprandial state (but not at fasting). The only change in baseline levels at fasting was displayed by TXB2. Furthermore, postprandial responsiveness was detected for seven compounds (POEA, SEA, 9(10)-DiHOME, 12(13)-DiHOME, 13-oxo-ODE, 9-HODE, and 13-HODE). Hence, the data confirm that the UPLC-ESI-MS/MS method performance was sufficient to detect i) a shift, in the current case most notably in the postprandial bioactive lipid metabolome, caused by changes in diet and ii) responsiveness to a challenge meal for a subset of the oxylipin and endocannabinoid metabolome. To summarize, we have shown proof-of-concept of our UPLC-ESI-MS/MS bioactive lipid protocols for the purpose of monitoring subtle shifts, and thereby useful to address lipid-mediated postprandial inflammation. PMID:26186333

Phenolic Compounds in the Potato and Its Byproducts: An Overview

PubMed Central

Akyol, Hazal; Riciputi, Ylenia; Capanoglu, Esra; Caboni, Maria Fiorenza; Verardo, Vito

2016-01-01

The potato (Solanum tuberosum L.) is a tuber that is largely used for food and is a source of different bioactive compounds such as starch, dietary fiber, amino acids, minerals, vitamins, and phenolic compounds. Phenolic compounds are synthetized by the potato plant as a protection response from bacteria, fungi, viruses, and insects. Several works showed that these potato compounds exhibited health-promoting effects in humans. However, the use of the potato in the food industry submits this vegetable to different processes that can alter the phenolic content. Moreover, many of these compounds with high bioactivity are located in the potato’s skin, and so are eliminated as waste. In this review the most recent articles dealing with phenolic compounds in the potato and potato byproducts, along with the effects of harvesting, post-harvest, and technological processes, have been reviewed. Briefly, the phenolic composition, main extraction, and determination methods have been described. In addition, the “alternative” food uses and healthy properties of potato phenolic compounds have been addressed. PMID:27240356

Recent developments in solid lipid nanoparticle and surface-modified solid lipid nanoparticle delivery systems for oral delivery of phyto-bioactive compounds in various chronic diseases

PubMed Central

Ko, Young Tag; Choi, Dong-Kug

2018-01-01

Solid lipid nanoparticle (SLN) delivery systems have a wide applicability in the delivery of phyto-bioactive compounds to treat various chronic diseases, including diabetes, cancer, obesity and neurodegenerative diseases. The multiple benefits of SLN delivery include improved stability, smaller particle size, leaching prevention and enhanced lymphatic uptake of the bioactive compounds through oral delivery. However, the burst release makes the SLN delivery systems inadequate for the oral delivery of various phyto-bioactive compounds that can treat such chronic diseases. Recently, the surface-modified SLN (SMSLN) was observed to overcome this limitation for oral delivery of phyto-bioactive compounds, and there is growing evidence of an enhanced uptake of curcumin delivered orally via SMSLNs in the brain. This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases. PMID:29588585

Xenohormesis: health benefits from an eon of plant stress response evolution

PubMed Central

Hooper, Paul L.; Tytell, Michael; Vígh, Lászlo

2010-01-01

Xenohormesis is a biological principle that explains how environmentally stressed plants produce bioactive compounds that can confer stress resistance and survival benefits to animals that consume them. Animals can piggyback off products of plants' sophisticated stress response which has evolved as a result of their stationary lifestyle. Factors eliciting the plant stress response can judiciously be employed to maximize yield of health-promoting plant compounds. The xenohormetic plant compounds can, when ingested, improve longevity and fitness by activating the animal's cellular stress response and can be applied in drug discovery, drug production, and nutritional enhancement of diet. PMID:20524162

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

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.

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.

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

Impact of high hydrostatic pressure and pasteurization on the structure and the extractability of bioactive compounds of persimmon “Rojo Brillante”.

PubMed

Hernández-Carrión, M; Vázquez-Gutiérrez, J L; Hernando, I; Quiles, A

2014-01-01

Rojo Brillante is an astringent oriental persimmon variety with high levels of bioactive compounds such as soluble tannins, carotenoids, phenolic acids, and dietary fiber. The purpose of this study was to investigate the effects of high hydrostatic pressure (HHP) and pasteurization on the structure of the fruit and on the extractability of certain bioactive compounds. The microstructure was studied using light microscopy, transmission electron microscopy, and low temperature scanning electron microscopy, and certain physicochemical properties (carotenoid and total soluble tannin content, antioxidant activity, fiber content, color, and texture properties) were measured. The structural changes induced by HHP caused a rise in solute circulation in the tissues that could be responsible for the increased carotenoid level and the unchanged antioxidant activity in comparison with the untreated persimmon. In contrast, the changes that took place during pasteurization lowered the tannin content and antioxidant activity. Consequently, HHP treatment could improve the extraction of potentially bioactive compoundsxsts from persimmons. A high nutritional value ingredient to be used when formulating new functional foods could be obtained using HHP. © 2013 Institute of Food Technologists®

Organically grown tomato (Lycopersicon esculentum Mill.): bioactive compounds in the fruit and infection with Phytophthora infestans.

PubMed

Mohammed, Afrah E; Smit, Inga; Pawelzik, Elke; Keutgen, Anna J; Horneburg, Bernd

2012-05-01

Tomato fruits are characterized by a good nutritional profile, including different bioactive compounds such as carotenoids, phenolic compounds and ascorbic acid. The objective of this study was to analyze the content of bioactive compounds in the fruit and the infection by Phytophthora infestans of 28 tomato genotypes from organic outdoor production. The relationship between bioactive compounds in the fruit and infection with P. infestans was estimated. Field experiments were carried out in 2004 and 2005 at two locations in central Germany. Significant variation among genotypes, locations and years was observed for the content of lycopene, ascorbic acid, total phenolic compounds, antioxidant capacity and the infection level of P. infestans. Antioxidant capacity seemed to be influenced mainly by the phenolics and was highest in small fruits, which were less infected with P. infestans. The large genetic variation among tomato genotypes for the content of bioactive compounds in their fruit allows for selection gains. None of the investigated bioactive compounds can be recommended for the indirect selection for increased field resistance against P. infestans. Copyright © 2011 Society of Chemical Industry.

Addressing Facts and Gaps in the Phenolics Chemistry of Winery By-Products.

PubMed

Machado, Nelson F L; Domínguez-Perles, Raúl

2017-02-14

Grape and wine phenolics display a noticeable structural diversity, encompassing distinct compounds ranging from simple molecules to oligomers, as well as polymers usually designated as tannins. Since these compounds contribute critically to the organoleptic properties of wines, their analysis and quantification are of primordial importance for winery industry operators. Besides, the occurrence of these compounds has been also extensively described in winery residues, which have been pointed as a valuable source of bioactive phytochemicals presenting potential for the development of new added value products that could fit the current market demands. Therefore, the cumulative knowledge generated during the last decades has allowed the identification of the most promising compounds displaying interesting biological functions, as well as the chemical features responsible for the observed bioactivities. In this regard, the present review explores the scope of the existing knowledge, concerning the compounds found in these winery by-products, as well as the chemical features presumably responsible for the biological functions already identified. Moreover, the present work will hopefully pave the way for further actions to develop new powerful applications to these materials, thus, contributing to more sustainable valorization procedures and the development of newly obtained compounds with enhanced biological properties.

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.

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.

Separation of Biologically Active Compounds by Membrane Operations.

PubMed

Zhu, Xiaoying; Bai, Renbi

2017-01-01

Bioactive compounds from various natural sources have been attracting more and more attention, owing to their broad diversity of functionalities and availabilities. However, many of the bioactive compounds often exist at an extremely low concentration in a mixture so that massive harvesting is needed to obtain sufficient amounts for their practical usage. Thus, effective fractionation or separation technologies are essential for the screening and production of the bioactive compound products. The applicatons of conventional processes such as extraction, distillation and lyophilisation, etc. may be tedious, have high energy consumption or cause denature or degradation of the bioactive compounds. Membrane separation processes operate at ambient temperature, without the need for heating and therefore with less energy consumption. The "cold" separation technology also prevents the possible degradation of the bioactive compounds. The separation process is mainly physical and both fractions (permeate and retentate) of the membrane processes may be recovered. Thus, using membrane separation technology is a promising approach to concentrate and separate bioactive compounds. A comprehensive survey of membrane operations used for the separation of bioactive compounds is conducted. The available and established membrane separation processes are introduced and reviewed. The most frequently used membrane processes are the pressure driven ones, including microfiltration (MF), ultrafiltration (UF) and nanofiltration (NF). They are applied either individually as a single sieve or in combination as an integrated membrane array to meet the different requirements in the separation of bioactive compounds. Other new membrane processes with multiple functions have also been developed and employed for the separation or fractionation of bioactive compounds. The hybrid electrodialysis (ED)-UF membrane process, for example has been used to provide a solution for the separation of biomolecules with similar molecular weights but different surface electrical properties. In contrast, the affinity membrane technology is shown to have the advantages of increasing the separation efficiency at low operational pressures through selectively adsorbing bioactive compounds during the filtration process. Individual membranes or membrane arrays are effectively used to separate bioactive compounds or achieve multiple fractionation of them with different molecule weights or sizes. Pressure driven membrane processes are highly efficient and widely used. Membrane fouling, especially irreversible organic and biological fouling, is the inevitable problem. Multifunctional membranes and affinity membranes provide the possibility of effectively separating bioactive compounds that are similar in sizes but different in other physical and chemical properties. Surface modification methods are of great potential to increase membrane separation efficiency as well as reduce the problem of membrane fouling. Developing membranes and optimizing the operational parameters specifically for the applications of separation of various bioactive compounds should be taken as an important part of ongoing or future membrane research in this field. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Synergistic, additive and antagonistic effects of fruit mixtures on total antioxidant capacities and bioactive compounds in tropical fruit juices.

PubMed

Pereira, Ana Carolina da Silva; Wurlitzer, Nedio Jair; Dionisio, Ana Paula; Lacerda Soares, Marcia Valéria; Rocha Bastos, Maria do Socorro; Elesbão Alves, Ricardo; Montenegro Brasil, Isabella

2015-06-01

The objective of this work was investigate the synergistic, additive and antagonistic effects of fruit mixtures on total antioxidant capacities and bioactive compounds in tropical fruit juices, and optimize its formulation by the response surface methodology based on the responses: total polyphenols (TP), total antioxidant capacity (TAC), ascorbic acid content and sensorial acceptance. Camu-camu, acerola and acai were the major factors that influenced the antioxidant potential of the juice; and the yellow mombin showed a positive effect on the acceptance of the tropical juice. It was observed an/antagonistic effect between acerola and camu-camu for the TAC response. The optimum formulation obtained was 20% acerola, 10% camu-camu, 10% yellow mombin, 10% cashew apple and 10% acai, which was responsible for a response of 155.46 mg.100 g(-1) of ascorbic acid, 103.01 mg of GAE.100 g-1 of TP, 10.27 µM Trolox g(-1) of TAC and approximately 6.1 of acceptance.

A novel bioactive osteogenesis scaffold delivers ascorbic acid, β-glycerophosphate, and dexamethasone in vivo to promote bone regeneration.

PubMed

Wang, Chao; Cao, Xuecheng; Zhang, Yongxian

2017-05-09

Ascorbic acid, β-glycerophosphate, and dexamethasone have been used in osteogenesis differentiation medium for in vitro cell culture, nothing is known for delivering these three bioactive compounds in vivo. In this study, we synthesized a novel bioactive scaffold by combining these three compounds with a lysine diisocyanate-based polyurethane. These bioactive compounds were released from the scaffold during the degradation process. The cell culture showed that the sponge-like structure in the scaffold was critical in providing a large surface area to support cell growth and all degradation products of the polymer were non-toxic. This bioactive scaffold enhanced the bone regeneration as evidenced by increasing the expression of three bone-related genes including collagen type I, Runx-2 and osteocalcin in rabbit bone marrow stem cells (BMSCs) in vitro and in vivo. The osteogenesis differentiation of BMSCs cultured in this bioactive scaffold was similar to that in osteogenesis differentiation medium and more extensive in this bioactive scaffold compared to the scaffold without these three bioactive compounds. These results indicated that the scaffold containing three bioactive compounds was a good osteogenesis differentiation promoter to enhance the osteogenesis differentiation and new bone formation in vivo.

A novel bioactive osteogenesis scaffold delivers ascorbic acid, β-glycerophosphate, and dexamethasone in vivo to promote bone regeneration

PubMed Central

Wang, Chao; Cao, Xuecheng; Zhang, Yongxian

2017-01-01

Ascorbic acid, β-glycerophosphate, and dexamethasone have been used in osteogenesis differentiation medium for in vitro cell culture, nothing is known for delivering these three bioactive compounds in vivo. In this study, we synthesized a novel bioactive scaffold by combining these three compounds with a lysine diisocyanate-based polyurethane. These bioactive compounds were released from the scaffold during the degradation process. The cell culture showed that the sponge-like structure in the scaffold was critical in providing a large surface area to support cell growth and all degradation products of the polymer were non-toxic. This bioactive scaffold enhanced the bone regeneration as evidenced by increasing the expression of three bone-related genes including collagen type I, Runx-2 and osteocalcin in rabbit bone marrow stem cells (BMSCs) in vitro and in vivo. The osteogenesis differentiation of BMSCs cultured in this bioactive scaffold was similar to that in osteogenesis differentiation medium and more extensive in this bioactive scaffold compared to the scaffold without these three bioactive compounds. These results indicated that the scaffold containing three bioactive compounds was a good osteogenesis differentiation promoter to enhance the osteogenesis differentiation and new bone formation in vivo. PMID:28404942

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.

Rapid in situ identification of bioactive compounds in plants by in vivo nanospray high-resolution mass spectrometry.

PubMed

Chang, Qing; Peng, Yue'e; Dan, Conghui; Shuai, Qin; Hu, Shenghong

2015-03-25

A method for the rapid in situ identification of bioactive compounds in fresh plants has been developed using in vivo nanospray coupled to high-resolution mass spectrometry (HR-MS). Using a homemade in vivo nanospray ion source, the plant liquid was drawn out from a target region and ionized in situ. The ionized bioactive compounds were then identified using Q-Orbitrap HR-MS. The accurate mass measurements of these bioactive compounds were performed by full-scan or selected ion monitoring (SIM), and tandem mass spectrometry (MS/MS) was used in the structural elucidation. Without sample pretreatment, 12 bioactive compounds in 7 different plant species were identified, namely, isoalliin in onion; butylphthalide in celery; N-methylpelletierine, pelletierine, and pseudopelletierine in pomegranate; chlorogenic acid in crabapple; solamargine, solasonine, and solasodine in nightshade; aloin and aloe-emodin in aloe; and menthone in mint. This work demonstrates that in vivo nanospray HR-MS is a good method for rapid in situ identification of bioactive compounds in plants.

Increase of content and bioactivity of total phenolic compounds from spent coffee grounds through solid state fermentation by Bacillus clausii.

PubMed

Rochín-Medina, Jesús J; Ramírez, Karina; Rangel-Peraza, Jesús G; Bustos-Terrones, Yaneth A

2018-03-01

Spent coffee grounds are waste material generated during coffee beverage preparation. This by-product disposal causes a negative environmental impact, in addition to the loss of a rich source of nutrients and bioactive compounds. A rotating central composition design was used to determine the optimal conditions for the bioactivity of phenolic compounds obtained after the solid state fermentation of spent coffee grounds by Bacillus clausii . To achieve this, temperature and fermentation time were varied according to the experimental design and the total phenolic and flavonoid content, antioxidant activity and antimicrobial activity were determined. Surface response methodology showed that optimum bioprocessing conditions were a temperature of 37 °C and a fermentation time of 39 h. Under these conditions, total phenolic and flavonoid contents increased by 36 and 13%, respectively, in fermented extracts as compared to non-fermented. In addition, the antioxidant activity was increased by 15% and higher antimicrobial activity was observed against Gram positive and negative bacteria. These data demonstrated that bioprocessing optimization of spent coffee grounds using the surface response methodology was an important tool to improve phenolic extraction, which could be used as an antioxidant and antimicrobial agents incorporated into different types of food products.

Mediterranean Diet and Multi-Ingredient-Based Interventions for the Management of Non-Alcoholic Fatty Liver Disease

PubMed Central

Suárez, Manuel; Boqué, Noemí; del Bas, Josep M.; Arola, Lluís; Caimari, Antoni

2017-01-01

Non-alcoholic fatty liver disease (NAFLD) comprises a wide spectrum of hepatic disorders, from simple steatosis to hepatic necro-inflammation leading to non-alcoholic steatohepatitis (NASH). Although the prevalence of these multifactorial pathologies is continuously increasing in the population, there is still not an established methodology for their treatment other than weight loss and a change in lifestyle habits, such as a hypocaloric diet and physical exercise. In this framework, there is increasing evidence that several food bioactives and dietary patterns are effective for reversing and preventing the onset of these pathologies. Some studies have claimed that better responses are obtained when treatments are performed under a multifaceted approach, using different bioactive compounds that act against complementary targets. Thus, in this work, current strategies for treating NAFLD and NASH based on multi-ingredient-based supplements or the Mediterranean diet, a dietary pattern rich in bioactive compounds, are reviewed. Furthermore, the usefulness of omics techniques to design effective multi-ingredient nutritional interventions and to predict and monitor their response against these disorders is also discussed. PMID:28937599

High-throughput microfluidic mixing and multiparametric cell sorting for bioactive compound screening.

PubMed

Young, Susan M; Curry, Mark S; Ransom, John T; Ballesteros, Juan A; Prossnitz, Eric R; Sklar, Larry A; Edwards, Bruce S

2004-03-01

HyperCyt, an automated sample handling system for flow cytometry that uses air bubbles to separate samples sequentially introduced from multiwell plates by an autosampler. In a previously documented HyperCyt configuration, air bubble separated compounds in one sample line and a continuous stream of cells in another are mixed in-line for serial flow cytometric cell response analysis. To expand capabilities for high-throughput bioactive compound screening, the authors investigated using this system configuration in combination with automated cell sorting. Peptide ligands were sampled from a 96-well plate, mixed in-line with fluo-4-loaded, formyl peptide receptor-transfected U937 cells, and screened at a rate of 3 peptide reactions per minute with approximately 10,000 cells analyzed per reaction. Cell Ca(2+) responses were detected to as little as 10(-11) M peptide with no detectable carryover between samples at up to 10(-7) M peptide. After expansion in culture, cells sort-purified from the 10% highest responders exhibited enhanced sensitivity and more sustained responses to peptide. Thus, a highly responsive cell subset was isolated under high-throughput mixing and sorting conditions in which response detection capability spanned a 1000-fold range of peptide concentration. With single-cell readout systems for protein expression libraries, this technology offers the promise of screening millions of discrete compound interactions per day.

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

[Exploring New Drug Targets through the Identification of Target Molecules of Bioactive Natural Products].

PubMed

Arai, Masayoshi

2016-01-01

With the development of cell biology and microbiology, it has become easy to culture many types of animal cells and microbes, and they are frequently used for phenotypic screening to explore medicinal seeds. On the other hand, it is recognized that cells and pathogenic microbes present in pathologic sites and infected regions of the human body display unique properties different from those under general culture conditions. We isolated several bioactive compounds from marine medicinal resources using constructed bioassay-guided separation focusing on the unique changes in the characteristics of cells and pathogenic microbes (Mycobacterium spp.) in the human body under disease conditions. In addition, we also carried out identification studies of target molecules of the bioactive compounds by methods utilizing the gene expression profile, transformants of cells or microbes, synthetic probe molecules of the isolated compounds, etc., since bioactive compounds isolated from the phenotypic screening system often target new molecules. This review presents our phenotypic screening systems, isolation of bioactive compounds from marine medicinal resources, and target identification of bioactive compounds.

Bioactive compounds from palm fatty acid distillate and crude palm oil

NASA Astrophysics Data System (ADS)

Estiasih, T.; Ahmadi, K.

2018-03-01

Crude palm oil (CPO) and palm fatty acid distillate (PFAD) are rich sources of bioactive compounds. PFAD is a by-product of palm oil refinery that produce palm frying oil. Physical refining of palm oil by deodorization produces palm fatty acid distillate. CPO and PFAD contain some bioactive compounds such as vitamin E (tocopherol and tocotrienols), phytosterol, and squalene. Bioactive compounds of CPO and PFAD are vitamin E, phytosterols, and squalene. Vitamin E of CPO and PFAD mainly comprised of tocotrienols and the remaining is tocopherol. Phytosterols of CPO and PFAD contained beta sitosterol, stigmasterol, and campesterol. Tocotrienols and phytosterols of CPO and PFAD, each can be separated to produce tocotrienol rich fraction and phytosterol rich fraction. Tocotrienol rich fraction from PFAD has both antioxidant and cholesterol lowering properties. Bioactive compounds of PFAD silmultaneously have been proven to improve lipid profile, and have hepatoprotector effect, imunomodulator, antioxidant properties, and lactogenic effect in animal test experiment. It is possible to develop separation of bioactive compounds of CPO and PFAD integratively with the other process that utilizes fatty acid.

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

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.

Integrated HPTLC-based Methodology for the Tracing of Bioactive Compounds in Herbal Extracts Employing Multivariate Chemometrics. A Case Study on Morus alba.

PubMed

Chaita, Eliza; Gikas, Evagelos; Aligiannis, Nektarios

2017-03-01

In drug discovery, bioassay-guided isolation is a well-established procedure, and still the basic approach for the discovery of natural products with desired biological properties. However, in these procedures, the most laborious and time-consuming step is the isolation of the bioactive constituents. A prior identification of the compounds that contribute to the demonstrated activity of the fractions would enable the selection of proper chromatographic techniques and lead to targeted isolation. The development of an integrated HPTLC-based methodology for the rapid tracing of the bioactive compounds during bioassay-guided processes, using multivariate statistics. Materials and Methods - The methanol extract of Morus alba was fractionated employing CPC. Subsequently, fractions were assayed for tyrosinase inhibition and analyzed with HPTLC. PLS-R algorithm was performed in order to correlate the analytical data with the biological response of the fractions and identify the compounds with the highest contribution. Two methodologies were developed for the generation of the dataset; one based on manual peak picking and the second based on chromatogram binning. Results and Discussion - Both methodologies afforded comparable results and were able to trace the bioactive constituents (e.g. oxyresveratrol, trans-dihydromorin, 2,4,3'-trihydroxydihydrostilbene). The suggested compounds were compared in terms of R f values and UV spectra with compounds isolated from M. alba using typical bioassay-guided process. Chemometric tools supported the development of a novel HPTLC-based methodology for the tracing of tyrosinase inhibitors in M. alba extract. All steps of the experimental procedure implemented techniques that afford essential key elements for application in high-throughput screening procedures for drug discovery purposes. Copyright © 2017 John Wiley & Sons, Ltd. Copyright © 2017 John Wiley & Sons, Ltd.

Statistical research on the bioactivity of new marine natural products discovered during the 28 years from 1985 to 2012.

PubMed

Hu, Yiwen; Chen, Jiahui; Hu, Guping; Yu, Jianchen; Zhu, Xun; Lin, Yongcheng; Chen, Shengping; Yuan, Jie

2015-01-07

Every year, hundreds of new compounds are discovered from the metabolites of marine organisms. Finding new and useful compounds is one of the crucial drivers for this field of research. Here we describe the statistics of bioactive compounds discovered from marine organisms from 1985 to 2012. This work is based on our database, which contains information on more than 15,000 chemical substances including 4196 bioactive marine natural products. We performed a comprehensive statistical analysis to understand the characteristics of the novel bioactive compounds and detail temporal trends, chemical structures, species distribution, and research progress. We hope this meta-analysis will provide useful information for research into the bioactivity of marine natural products and drug development.

Extraction of bioactive compounds and free radical scavenging activity of purple basil (Ocimum basilicum L.) leaf extracts as affected by temperature and time.

PubMed

Pedro, Alessandra C; Moreira, Fernanda; Granato, Daniel; Rosso, Neiva D

2016-05-13

In the current study, response surface methodology (RSM) was used to assess the effects of extraction time and temperature on the content of bioactive compounds and antioxidant activity of purple basil leaf (Ocimum basilicum L.) extracts. The stability of anthocyanins in relation to temperature, light and copigmentation was also studied. The highest anthocyanin content was 67.40 mg/100 g extracted at 30 °C and 60 min. The degradation of anthocyanins with varying temperatures and in the presence of light followed a first-order kinetics and the activation energy was 44.95 kJ/mol. All the extracts exposed to light showed similar half-lives. The extracts protected from light, in the presence of copigments, showed an increase in half-life from 152.67 h for the control to 856.49 and 923.17 h for extract in the presence of gallic acid and phytic acid, respectively. These results clearly indicate that purple basil is a potential source of stable bioactive compounds.

[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.

Lauric acid and myristic acid from Allium sativum inhibit the growth of Mycobacterium tuberculosis H37Ra: in silico analysis reveals possible binding to protein kinase B.

PubMed

Muniyan, Rajiniraja; Gurunathan, Jayaraman

2016-12-01

The bulb of Allium sativum Linn (Alliaceae) has numerous medicinal values. Though the petroleum ether extract of the bulb has shown to exhibit antimycobacterial activity, the phytochemical(s) responsible for this inhibitory activity is not known. To characterize the bioactive compounds in the petroleum ether extract of Allium sativum (garlic) that inhibit the growth of Mycobacterium tuberculosis H37Ra. Bioactivity-guided fractionation was employed to isolate the bioactive compounds. Antimycobacterial activity was evaluated by well-diffusion method and microplate alamar blue assay (MABA). Infrared spectroscopy, mass spectrometry and nuclear magnetic resonance spectroscopy were used to characterize the bioactive compounds. Autodock was used to obtain information on molecular recognition, and molecular dynamics simulation was performed using GROMACS. The bioactive compounds that inhibited the growth of M. tuberculosis H37Ra were found to be lauric acid (LA) and myristic acid (MA). The minimal inhibitory concentration of LA and MA was found to be 22.2 and 66.7 μg/mL, respectively. In silico analysis revealed that these fatty acids could bind at the cleft between the N-terminal and C-terminal lobes of the cytosolic domain of serine/threonine protein kinase B (PknB). The inhibition activity was dependent on the alkyl chain length of the fatty acid, and the amino acid residues involved in binding to fatty acid was found to be conserved across the Pkn family of proteins. The study indicates the possibility of using fatty acid derivatives, involving Pkn family of proteins, to inhibit the signal transduction processes in M. tuberculosis.

Bis-Acridines as Lead Antiparasitic Agents: Structure-Activity Analysis of a Discrete Compound Library In Vitro▿

PubMed Central

Caffrey, Conor R.; Steverding, Dietmar; Swenerton, Ryan K.; Kelly, Ben; Walshe, Deirdre; Debnath, Anjan; Zhou, Yuan-Min; Doyle, Patricia S.; Fafarman, Aaron T.; Zorn, Julie A.; Land, Kirkwood M.; Beauchene, Jessica; Schreiber, Kimberly; Moll, Heidrun; Ponte-Sucre, Alicia; Schirmeister, Tanja; Saravanamuthu, Ahilan; Fairlamb, Alan H.; Cohen, Fred E.; McKerrow, James H.; Weisman, Jennifer L.; May, Barnaby C. H.

2007-01-01

Parasitic diseases are of enormous public health significance in developing countries—a situation compounded by the toxicity of and resistance to many current chemotherapeutics. We investigated a focused library of 18 structurally diverse bis-acridine compounds for in vitro bioactivity against seven protozoan and one helminth parasite species and compared the bioactivities and the cytotoxicities of these compounds toward various mammalian cell lines. Structure-activity relationships demonstrated the influence of both the bis-acridine linker structure and the terminal acridine heterocycle on potency and cytotoxicity. The bioactivity of polyamine-linked acridines required a minimum linker length of approximately 10 Å. Increasing linker length resulted in bioactivity against most parasites but also cytotoxicity toward mammalian cells. N alkylation, but less so N acylation, of the polyamine linker ameliorated cytotoxicity while retaining bioactivity with 50% effective concentration (EC50) values similar to or better than those measured for standard drugs. Substitution of the polyamine for either an alkyl or a polyether linker maintained bioactivity and further alleviated cytotoxicity. Polyamine-linked compounds in which the terminal acridine heterocycle had been replaced with an aza-acridine also maintained acceptable therapeutic indices. The most potent compounds recorded low- to mid-nanomolar EC50 values against Plasmodium falciparum and Trypanosoma brucei; otherwise, low-micromolar potencies were measured. Importantly, the bioactivity of the library was independent of P. falciparum resistance to chloroquine. Compound bioactivity was a function of neither the potential to bis-intercalate DNA nor the inhibition of trypanothione reductase, an important drug target in trypanosomatid parasites. Our approach illustrates the usefulness of screening focused compound libraries against multiple parasite targets. Some of the bis-acridines identified here may represent useful starting points for further lead optimization. PMID:17371810

Statistical Research on the Bioactivity of New Marine Natural Products Discovered during the 28 Years from 1985 to 2012

PubMed Central

Hu, Yiwen; Chen, Jiahui; Hu, Guping; Yu, Jianchen; Zhu, Xun; Lin, Yongcheng; Chen, Shengping; Yuan, Jie

2015-01-01

Every year, hundreds of new compounds are discovered from the metabolites of marine organisms. Finding new and useful compounds is one of the crucial drivers for this field of research. Here we describe the statistics of bioactive compounds discovered from marine organisms from 1985 to 2012. This work is based on our database, which contains information on more than 15,000 chemical substances including 4196 bioactive marine natural products. We performed a comprehensive statistical analysis to understand the characteristics of the novel bioactive compounds and detail temporal trends, chemical structures, species distribution, and research progress. We hope this meta-analysis will provide useful information for research into the bioactivity of marine natural products and drug development. PMID:25574736

Improving the estimation of flavonoid intake for study of health outcomes

PubMed Central

Dwyer, Johanna T.; Jacques, Paul F.; McCullough, Marjorie L.

2015-01-01

Imprecision in estimating intakes of non-nutrient bioactive compounds such as flavonoids is a challenge in epidemiologic studies of health outcomes. The sources of this imprecision, using flavonoids as an example, include the variability of bioactive compounds in foods due to differences in growing conditions and processing, the challenges in laboratory quantification of flavonoids in foods, the incompleteness of flavonoid food composition tables, and the lack of adequate dietary assessment instruments. Steps to improve databases of bioactive compounds and to increase the accuracy and precision of the estimation of bioactive compound intakes in studies of health benefits and outcomes are suggested. PMID:26084477

Effect of Different Germination Conditions on Antioxidative Properties and Bioactive Compounds of Germinated Brown Rice

PubMed Central

Lin, You-Tung; Pao, Cheng-Cheng; Wu, Shwu-Tzy; Chang, Chi-Yue

2015-01-01

This study investigates antioxidative activity and bioactive compounds of ungerminated brown rice (UBR) and germinated brown rice (GBR). We used two rice cultivars (Oryza sativa L.), Taiwan Japonica 9 (TJ-9) and Taichung Indica 10 (TCI-10), as the materials in our experiments. The conditions for inducing germination are soaking time in water 24, 48, or 72 h; temperature 26 or 36°C; incubation in light or darkness; and open or closed vessels, in which the antioxidative activities and bioactive compounds of GBR were determined. We found that, in order to maximize antioxidative activity and bioactive compounds, germination should be under higher temperature (36°C), long soaking time (72 h), darkness, and closed vessel. GBR contains much higher levels of antioxidative activity and bioactive compounds than ungerminated brown rice (UBR). We found a strong correlation between antioxidative activities (DPPH radical scavenging ability, reducing power, and Trolox equivalent antioxidant capacity) and bioactive compounds (γ-oryzanols, tocopherol, and tocotrienol). Higher temperature (36°C) is also conducive to the production of GABA in GBR. These results are considered very useful research references for the development of future functional foods and additives. PMID:25861637

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.

Biosynthetic approaches to creating bioactive fungal metabolites: Pathway engineering and activation of secondary metabolism.

PubMed

Motoyama, Takayuki; Osada, Hiroyuki

2016-12-15

The diversity of natural products is greater than that of combinatorial chemistry compounds and is similar to that of drugs. Compounds rich in sp 3 carbons, such as natural products, typically exhibit high structural complexity and high specificity to molecular targets. Microorganisms can synthesize such sp 3 carbon-rich compounds and can be used as excellent factories for making bioactive compounds. Here, we mainly focus on pathway engineering of two sp 3 carbon-rich bioactive indole alkaloids, fumitremorgin C and terpendole E. We also demonstrate the importance of activation of secondary metabolism by focusing on tenuazonic acid, a bioactive tetramic acid compound, as an example. Copyright © 2016 Elsevier Ltd. All rights reserved.

Transcriptome analysis reveals the genetic basis underlying the biosynthesis of volatile oil, gingerols, and diarylheptanoids in ginger (Zingiber officinale Rosc.).

PubMed

Jiang, Yusong; Liao, Qinhong; Zou, Yong; Liu, Yiqing; Lan, Jianbin

2017-10-23

Ginger (Zingiber officinale Rosc.) is a popular flavoring that widely used in Asian, and the volatile oil in ginger rhizomes adds a special fragrance and taste to foods. The bioactive compounds in ginger, such as gingerols, diarylheptanoids, and flavonoids, are of significant value to human health because of their anticancer, anti-oxidant, and anti-inflammatory properties. However, as a non-model plant, knowledge about the genome sequences of ginger is extremely limited, and this limits molecular studies on this plant. In this study, de novo transcriptome sequencing was performed to investigate the expression of genes associated with the biosynthesis of major bioactive compounds in matured ginger rhizome (MG), young ginger rhizome (YG), and fibrous roots of ginger (FR). A total of 361,876 unigenes were generated by de novo assembly. The expression of genes involved in the pathways responsible for the biosynthesis of major bioactive compounds differed between tissues (MG, YG, and FR). Two pathways that give rise to volatile oil, gingerols, and diarylheptanoids, the "terpenoid backbone biosynthesis" and "stilbenoid, diarylheptanoid and gingerol biosynthesis" pathways, were significantly enriched (adjusted P value < 0.05) for differentially expressed genes (DEGs) (FDR < 0.005) both between the FR and YG libraries, and the FR and MG libraries. Most of the unigenes mapped in these two pathways, including curcumin synthase, phenylpropanoylacetyl-CoA synthase, trans-cinnamate 4-monooxygenase, and 4-hydroxy-3-methylbut-2-en-1-yl diphosphate synthase, were expressed to a significantly higher level (log 2 (fold-change) ≥ 1) in FR than in YG or MG. This study provides the first insight into the biosynthesis of bioactive compounds in ginger at a molecular level and provides valuable genome resources for future molecular studies on ginger. Moreover, our results establish that bioactive compounds in ginger may predominantly synthesized in the root and then transported to rhizomes, where they accumulate.

Cyanobacteria as a Source for Novel Anti-Leukemic Compounds.

PubMed

Humisto, Anu; Herfindal, Lars; Jokela, Jouni; Karkman, Antti; Bjørnstad, Ronja; Choudhury, Romi R; Sivonen, Kaarina

2016-01-01

Cyanobacteria are an inspiring source of bioactive secondary metabolites. These bioactive agents are a diverse group of compounds which are varying in their bioactive targets, the mechanisms of action, and chemical structures. Cyanobacteria from various environments, especially marine benthic cyanobacteria, are found to be rich sources for the search for novel bioactive compounds. Several compounds with anticancer activities have been discovered from cyanobacteria and some of these have succeeded to enter the clinical trials. Varying anticancer agents are needed to overcome increasing challenges in cancer treatments. Different search methods are used to reveal anticancer compounds from natural products, but cell based methods are the most common. Cyanobacterial bioactive compounds as agents against acute myeloid leukemia are not well studied. Here we examined our new results combined with previous studies of anti-leukemic compounds from cyanobacteria with emphasis to reveal common features in strains producing such activity. We report that cyanobacteria harbor specific anti-leukemic compounds since several studied strains induced apoptosis against AML cells but were inactive against non-malignant cells like hepatocytes. We noted that particularly benthic strains from the Baltic Sea, such as Anabaena sp., were especially potential AML apoptosis inducers. Taken together, this review and re-analysis of data demonstrates the power of maintaining large culture collections for the search for novel bioactivities, and also how anti-AML activity in cyanobacteria can be revealed by relatively simple and low-cost assays.

Antioxidant capacity, insecticidal ability and heat-oxidation stability of Tagetes lemmonii leaf extract.

PubMed

Ma, Chih-Ming; Cheng, Chih-Lun; Lee, Shang-Chieh; Hong, Gui-Bing

2018-04-30

The aim of this study was to examine the effect of process factors such as ethanol concentration, extraction time and temperature on the extraction yield and the bioactive contents of Tagetes lemmonii leaf extracts using response surface methodology (RSM). ANOVA results showed that the response variables were affected by the ethanol concentration to a very significant degree and by extraction temperature to a lesser degree. GC/MS characterization showed that the extract is rich in bioactive compounds and those present exhibited important biological activities such as antioxidant, insect repellence and insecticidal activities. The results from the toxicity assay demonstrate that the extract obtained from the leaves of Tagetes lemmonii was an effective insect toxin against Tribolium castaneum. The radical scavenging activity and p-anisidine test results of olive oil spiked with different concentrations of leaf extract showed that the phenolic compounds can retard lipid oxidation. Copyright © 2018 Elsevier Inc. All rights reserved.

Elicitation: a tool for enriching the bioactive composition of foods.

PubMed

Baenas, Nieves; García-Viguera, Cristina; Moreno, Diego A

2014-09-01

Elicitation is a good strategy to induce physiological changes and stimulate defense or stress-induced responses in plants. The elicitor treatments trigger the synthesis of phytochemical compounds in fruits, vegetables and herbs. These metabolites have been widely investigated as bioactive compounds responsible of plant cell adaptation to the environment, specific organoleptic properties of foods, and protective effects in human cells against oxidative processes in the development of neurodegenerative and cardiovascular diseases and certain types of cancer. Biotic (biological origin), abiotic (chemical or physical origin) elicitors and phytohormones have been applied alone or in combinations, in hydroponic solutions or sprays, and in different selected time points of the plant growth or during post-harvest. Understanding how plant tissues and their specific secondary metabolic pathways respond to specific treatments with elicitors would be the basis for designing protocols to enhance the production of secondary metabolites, in order to produce quality and healthy fresh foods.

Phenethyl ester and amide of Ferulic Acids: Synthesis and bioactivity against P388 Leukemia Murine Cells

NASA Astrophysics Data System (ADS)

Firdaus; Soekamto, N. H.; Seniwati; Islam, M. F.; Sultan

2018-03-01

Bioactivity of a compound is closely related to the molecular structure of the compound concerned, its strength being the quantitative relation of the strength of the activity of the group it possesses. The combining of moieties of the active compounds will produce more active compounds. Most phenolic compounds as well as compounds containing moiety phenethyl groups have potential activity as anticancer. Combining phenolic groups and phenethyl groups in a compound will result in compounds having strong anticancer bioactivity. This study aims to combine the feruloyl and phenethyl groups to form esters and amides by synthesize of phenethyl trans-3-(4-hydroxy-3-methoxyphenyl)acrylate (5) and trans-3-(4- hydroxy-3-methoxyphenyl)-N-phenethylacrylamide (6) from ferulic acid with phenethyl alcohol and phenethylamine, and to study their bioactivity as anticancer. The synthesis of both compounds was conducted via indirect reaction, including acetylation, chlorination, esterfication/amidation, and deacetylation. Structures of products were characterized by FTIR and NMR data, and their bioactivity assay of the compounds against P388 Leukemia Murine Cells was conducted by an MTT method. Results showed that the compound 5 was obtained as a yellow gel with the IC50 of 10.79 μg/mL (36.21 μΜ), and the compound 6 was a yellowish solid with a melting point of 118-120°C and the IC50 of 29.14 μg/mL (97.79 μΜ). These compounds were more active than the analog compounds.

A nitrous acid biosynthetic pathway for diazo group formation in bacteria.

PubMed

Sugai, Yoshinori; Katsuyama, Yohei; Ohnishi, Yasuo

2016-02-01

Although some diazo compounds have bioactivities of medicinal interest, little is known about diazo group formation in nature. Here we describe an unprecedented nitrous acid biosynthetic pathway responsible for the formation of a diazo group in the biosynthesis of the ortho-diazoquinone secondary metabolite cremeomycin in Streptomyces cremeus. This finding provides important insights into the biosynthetic pathways not only for diazo compounds but also for other naturally occurring compounds containing nitrogen-nitrogen bonds.

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.

VIT-CMJ2: Endophyte of Agaricus bisporus in Production of Bioactive Compounds.

PubMed

Gautam, Chandan Kumar; Madhav, Mukund; Sinha, Astha; Jabez Osborne, William

2016-06-01

Agaricus bisporus is an edible basidiomycete fungus. Both the body and the mycelium contain compounds comprising a wide range of antimicrobial molecules, contributing in improvement of immunity and tumor-retardation. The presence of endophytes capable of producing bioactive compounds was investigated in Agaricus bisporus . Endophytes from Agaricus bisporus was isolated on LB agar. The obtained isolates were characterized morphologically and biochemically. Further 16S rRNA sequencing was implemented for molecular analysis of isolates. The isolate was mass produced and the bioactive compounds were extracted using ethyl acetate, chloroform and hexane. Agar well diffusion method was carried out to seek the potential of any antimicrobial activity of the crude bioactive compounds against known pathogens. GC-MS and FT-IR analysis were performed for the identification of bioactive compounds. VIT-CMJ2 was identified as Enterobacter sp. as revealed by 16S rRNA sequencing. Chloroform extract of VIT-CMJ2 showed a maximum zone of inhibition of 19 mm against Salmonella typhi followed by hexane and ethyl acetate extracts. The GC-MS analysis revealed the presence of several bioactive compounds having effective antimicrobial activity like butyl ester, Behenicalcohol, S , S-dioxide derivatives and some others which were later confirmed by FT-IR spectral stretches. The present study shows the insight on the way endophytes interact with Agaricus bisporus ; thereby improving the nutritional profile.

VIT-CMJ2: Endophyte of Agaricus bisporus in Production of Bioactive Compounds

PubMed Central

Gautam, Chandan Kumar; Madhav, Mukund; Sinha, Astha; Jabez Osborne, William

2016-01-01

Background Agaricus bisporus is an edible basidiomycete fungus. Both the body and the mycelium contain compounds comprising a wide range of antimicrobial molecules, contributing in improvement of immunity and tumor-retardation. Objectives The presence of endophytes capable of producing bioactive compounds was investigated in Agaricus bisporus. Materials and Methods Endophytes from Agaricus bisporus was isolated on LB agar. The obtained isolates were characterized morphologically and biochemically. Further 16S rRNA sequencing was implemented for molecular analysis of isolates. The isolate was mass produced and the bioactive compounds were extracted using ethyl acetate, chloroform and hexane. Agar well diffusion method was carried out to seek the potential of any antimicrobial activity of the crude bioactive compounds against known pathogens. GC-MS and FT-IR analysis were performed for the identification of bioactive compounds. Results VIT-CMJ2 was identified as Enterobacter sp. as revealed by 16S rRNA sequencing. Chloroform extract of VIT-CMJ2 showed a maximum zone of inhibition of 19 mm against Salmonella typhi followed by hexane and ethyl acetate extracts. The GC-MS analysis revealed the presence of several bioactive compounds having effective antimicrobial activity like butyl ester, Behenicalcohol, S , S-dioxide derivatives and some others which were later confirmed by FT-IR spectral stretches. Conclusions The present study shows the insight on the way endophytes interact with Agaricus bisporus; thereby improving the nutritional profile. PMID:28959322

Computational Analysis of Gynura bicolor Bioactive Compounds as Dipeptidyl Peptidase-IV Inhibitor

PubMed Central

Abdullah Zawawi, Muhammad Redha; Ahmad, Muhamad Aizuddin; Jaganath, Indu Bala

2017-01-01

The inhibition of dipeptidyl peptidase-IV (DPPIV) is a popular route for the treatment of type-2 diabetes. Commercially available gliptin-based drugs such as sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin were specifically developed as DPPIV inhibitors for diabetic patients. The use of Gynura bicolor in treating diabetes had been reported in various in vitro experiments. However, an understanding of the inhibitory actions of G. bicolor bioactive compounds on DPPIV is still lacking and this may provide crucial information for the development of more potent and natural sources of DPPIV inhibitors. Evaluation of G. bicolor bioactive compounds for potent DPPIV inhibitors was computationally conducted using Lead IT and iGEMDOCK software, and the best free-binding energy scores for G. bicolor bioactive compounds were evaluated in comparison with the commercial DPPIV inhibitors, sitagliptin, anagliptin, linagliptin, saxagliptin, and alogliptin. Drug-likeness and absorption, distribution, metabolism, and excretion (ADME) analysis were also performed. Based on molecular docking analysis, four of the identified bioactive compounds in G. bicolor, 3-caffeoylquinic acid, 5-O-caffeoylquinic acid, 3,4-dicaffeoylquinic acid, and trans-5-p-coumaroylquinic acid, resulted in lower free-binding energy scores when compared with two of the commercially available gliptin inhibitors. The results revealed that bioactive compounds in G. bicolor are potential natural inhibitors of DPPIV. PMID:28932239

Effect of edible coatings on bioactive compounds and antioxidant capacity of tomatoes at different maturity stages.

PubMed

Dávila-Aviña, Jorge E; Villa-Rodríguez, José A; Villegas-Ochoa, Mónica A; Tortoledo-Ortiz, Orlando; Olivas, Guadalupe I; Ayala-Zavala, J Fernando; González-Aguilar, Gustavo A

2014-10-01

This work evaluated the effect of carnauba and mineral oil coatings on the bioactive compounds and antioxidant capacity of tomato fruits (cv. "Grandela"). Carnauba and mineral oil coatings were applied on fresh tomatoes at two maturity stages (breaker and pink) over 28 day of storage at 10 °C was evaluated. Bioactive compound and antioxidant activity assays included total phenols, total flavonoids, ascorbic acid (ASA), lycopene, DPPH radical scavenging activity (%RSA), trolox equivalent antioxidant capacity (TEAC) and oxygen radical absorbance capacity assay (ORAC). The total phenolic, flavonoid and lycopene contents were significantly lower for coated fruit than control fruits. However, ascorbic acid content was highest in fruits treated with carnauba, followed by mineral oil coating and control fruits. The ORAC values were highest in breaker tomatoes coated with carnauba wax, followed by mineral oil-coated fruits and controls. No significant differences in ORAC values were observed in pink tomatoes. % RSA and TEAC values were higher for controls than for coated fruit. Edible coatings preserve the overall quality of tomatoes during storage without affecting the nutritional quality of fruit. We found that the physiological response to the coatings is in function of the maturity stage of tomatoes. The information obtained in this study support to use of edible coating as a safe and good alternative to preserve tomato quality, and that the changes of bioactive compounds and antioxidant activity of tomato fruits, was not negatively affected. This approach can be used by producers to preserve tomato quality.

Three phase partitioning and spectroscopic characterization of bioactive constituent from halophilic Bacillus subtilis EMB M15.

PubMed

Yadav, Neerja; Gupta, Munishwar Nath; Khare, Sunil K

2017-10-01

In the present study, a halophilic Bacillus subtilis subsp. spizizenii (NCBI GenBank accession number KX109607) was isolated from the Sambhar Salt Lake, Rajasthan India. This organism exhibited significance antibacterial and antifungal activity against Proteus vulgaris, Bacillus subtilis, Aspergillus niger, Rhizopus oligosporus and Penicillium chrysogenum respectively. The bioactive constituent responsible for it was extracted by three phase partitioning and purified by column chromatography. The purified compound was further characterized by FTIR-ATR, NMR and Mass spectrometry. The mass spectra show a molecular ion of m/z 301.14. The compound has very high antimicrobial activity showing 35mm zone of inhibition against Bacillus subtilis. Copyright © 2017 Elsevier Ltd. All rights reserved.

Current Advances in the Antimicrobial Potential of Species of Genus Ganoderma (Higher Basidiomycetes) against Human Pathogenic Microorganisms (Review).

PubMed

Rai, Mahendra K; Gaikwad, Swapnil; Nagaonkar, Dipali; dos Santos, Carolina Alves

2015-01-01

Ganoderma spp. are very important therapeutic mushrooms and have been used traditionally for 4000 years in the treatment of various human disorders. Different species of Ganoderma possess bioactive compounds, which have already demonstrated antiviral, antibacterial, and antifungal activities. Various bioactive compounds such as triterpenoids, colossolactones, and polysaccharides, which are responsible for the antimicrobial potential of the genus, are discussed here in detail. Some Ganoderma spp. have been reported to be potential agents for the synthesis of metal nanoparticles. These nanoparticles have demonstrated antimicrobial activity and also are reviewed herein. The main aim of this review is to discuss the possible use of Ganoderma extracts and their active principles in antimicrobial therapy.

New Bioactive Compounds from Korean Native Mushrooms

PubMed Central

Kim, Seong-Eun; Hwang, Byung Soon; Song, Ja-Gyeong; Lee, Seung Woong; Lee, In-Kyoung

2013-01-01

Mushrooms are ubiquitous in nature and have high nutritional attributes. They have demonstrated diverse biological effects and therefore have been used in treatments of various diseases, including cancer, diabetes, bacterial and viral infections, and ulcer. In particular, polysaccharides, including β-glucan, are considered as the major constituents responsible for the biological activity of mushrooms. Although an overwhelming number of reports have been published on the importance of polysaccharides as immunomodulating agents, not all of the healing properties found in these mushrooms could be fully accounted for. Recently, many research groups have begun investigations on biologically active small-molecular weight compounds in wild mushrooms. In this mini-review, both structural diversity and biological activities of novel bioactive substances from Korean native mushrooms are described. PMID:24493936

Antimicrobial compounds from seaweeds-associated bacteria and fungi.

PubMed

Singh, Ravindra Pal; Kumari, Puja; Reddy, C R K

2015-02-01

In recent decade, seaweeds-associated microbial communities have been significantly evaluated for functional and chemical analyses. Such analyses let to conclude that seaweeds-associated microbial communities are highly diverse and rich sources of bioactive compounds of exceptional molecular structure. Extracting bioactive compounds from seaweed-associated microbial communities have been recently increased due to their broad-spectrum antimicrobial activities including antibacterial, antifungal, antiviral, anti-settlement, antiprotozoan, antiparasitic, and antitumor. These allelochemicals not only provide protection to host from other surrounding pelagic microorganisms, but also ensure their association with the host. Antimicrobial compounds from marine sources are promising and priority targets of biotechnological and pharmaceutical applications. This review describes the bioactive metabolites reported from seaweed-associated bacterial and fungal communities and illustrates their bioactivities. Biotechnological application of metagenomic approach for identifying novel bioactive metabolites is also dealt, in view of their future development as a strong tool to discover novel drug targets from seaweed-associated microbial communities.

Ultrahigh pressure extraction of bioactive compounds from plants-A review.

PubMed

Xi, Jun

2017-04-13

Extraction of bioactive compounds from plants is one of the most important research areas for pharmaceutical and food industries. Conventional extraction techniques are usually associated with longer extraction times, lower yields, more organic solvent consumption, and poor extraction efficiency. A novel extraction technique, ultrahigh pressure extraction, has been developed for the extraction of bioactive compounds from plants, in order to shorten the extraction time, decrease the solvent consumption, increase the extraction yields, and enhance the quality of extracts. The mild processing temperature of ultrahigh pressure extraction may lead to an enhanced extraction of thermolabile bioactive ingredients. A critical review is conducted to introduce the different aspects of ultrahigh pressure extraction of plants bioactive compounds, including principles and mechanisms, the important parameters influencing its performance, comparison of ultrahigh pressure extraction with other extraction techniques, advantages, and disadvantages. The future opportunities of ultrahigh pressure extraction are also discussed.

Can Invalid Bioactives Undermine Natural Product-Based Drug Discovery?

PubMed Central

2015-01-01

High-throughput biology has contributed a wealth of data on chemicals, including natural products (NPs). Recently, attention was drawn to certain, predominantly synthetic, compounds that are responsible for disproportionate percentages of hits but are false actives. Spurious bioassay interference led to their designation as pan-assay interference compounds (PAINS). NPs lack comparable scrutiny, which this study aims to rectify. Systematic mining of 80+ years of the phytochemistry and biology literature, using the NAPRALERT database, revealed that only 39 compounds represent the NPs most reported by occurrence, activity, and distinct activity. Over 50% are not explained by phenomena known for synthetic libraries, and all had manifold ascribed bioactivities, designating them as invalid metabolic panaceas (IMPs). Cumulative distributions of ∼200,000 NPs uncovered that NP research follows power-law characteristics typical for behavioral phenomena. Projection into occurrence–bioactivity–effort space produces the hyperbolic black hole of NPs, where IMPs populate the high-effort base. PMID:26505758

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).

Comprehensive identification of bioactive compounds of avocado peel by liquid chromatography coupled to ultra-high-definition accurate-mass Q-TOF.

PubMed

Figueroa, Jorge G; Borrás-Linares, Isabel; Lozano-Sánchez, Jesús; Segura-Carretero, Antonio

2018-04-15

Industrially the avocado pulp is exploited principally as oil and paste, generating a huge quantity of peel and seed as by-products. Avocado peel is a promising inexpensive candidate for recovery phenolic compounds. The aim of this work was to identify the bioactive compounds present in an extract of avocado peel obtained by a green extraction technique. Accelerated solvent extraction was performed using water and ethanol as extraction solvents. Liquid chromatography coupled to ultra-high-definition accurate-mass spectrometry was used in order to identify the bioactive compounds. A total of sixty-one compounds belonging to eleven families were identified. Procyanidins, flavonols, hydroxybenzoic and hydroxycinnamic acids were the most common compounds. A sum of thirty-five compounds has been identified here for the first time in avocado peel. These results confirm the potential of avocado peel as a source of bioactive ingredients for its use in the food, cosmetic or pharmaceutical sector. Copyright © 2017 Elsevier Ltd. All rights reserved.

Ultrasound-assisted extraction of bioactive compounds from lemon balm and peppermint leaves

NASA Astrophysics Data System (ADS)

Šic Žlabur, Jana; Voća, Sandra; Dobričević, Nadica; Pliestić, Stjepan; Galić, Ante; Boričević, Ana; Borić, Nataša

2016-01-01

The aim of this study was to investigate the influence of conventional and ultrasound-assisted extraction (frequency, time, temperature) on the content of bioactive compounds as well as on the antioxidant activity of aqueous extracts from fresh lemon balm and peppermint leaves. Total phenols, flavonoids, non-flavonoids, total chlorophylls, total carotenoids, and radical scavenging capacity were determined. Moreover, the relationship between bioactive compounds and antioxidant capacity was studied by linear regression. A significant increase in all studied bioactive compounds during ultrasonic extraction for 5 to 20 min was found. With the classical extraction method, the highest amounts of total phenols, flavonoids, and antioxidant activity were determined, and the maximum amounts of total chlorophylls and carotenoids were determined during 20 min ultrasonic extraction. The correlation analysis revealed a strong, positive relationship between antioxidant activity and total phenolic compounds.

Effect-directed analysis of cold-pressed hemp, flax and canola seed oils by planar chromatography linked with (bio)assays and mass spectrometry.

PubMed

Teh, Sue-Siang; Morlock, Gertrud E

2015-11-15

Cold-pressed hemp, flax and canola seed oils are healthy oils for human consumption as these are rich in polyunsaturated fatty acids and bioactive phytochemicals. However, bioactive information on the food intake side is mainly focused on target analysis. For more comprehensive information with regard to effects, single bioactive compounds present in the seed oil extracts were detected by effect-directed assays, like bioassays or an enzymatic assay, directly linked with chromatography and further characterized by mass spectrometry. This effect-directed analysis is a streamlined method for the analysis of bioactive compounds in the seed oil extracts. All effective compounds with regard to the five assays or bioassays applied were detected in the samples, meaning also bioactive breakdown products caused during oil processing, residues or contaminants, aside the naturally present bioactive phytochemicals. The investigated cold-pressed oils contained compounds that exert antioxidative, antimicrobial, acetylcholinesterase inhibitory and estrogenic activities. This effect-directed analysis can be recommended for bioactivity profiling of food to obtain profound effect-directed information on the food intake side. Copyright © 2015 Elsevier Ltd. All rights reserved.

Effect of barrier properties of zein colloidal particles and oil-in-water emulsions on oxidative stability of encapsulated bioactive compounds

USDA-ARS?s Scientific Manuscript database

Oxidation of encapsulated bioactive compounds is a key challenge that limits shelf-life of bioactive containing products. The objectives of this study were to compare differences between the oxidative barrier properties of biopolymer particle based encapsulation system (zein colloidal particles) and...

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.

Toward automated biochemotype annotation for large compound libraries.

PubMed

Chen, Xian; Liang, Yizeng; Xu, Jun

2006-08-01

Combinatorial chemistry allows scientists to probe large synthetically accessible chemical space. However, identifying the sub-space which is selectively associated with an interested biological target, is crucial to drug discovery and life sciences. This paper describes a process to automatically annotate biochemotypes of compounds in a library and thus to identify bioactivity related chemotypes (biochemotypes) from a large library of compounds. The process consists of two steps: (1) predicting all possible bioactivities for each compound in a library, and (2) deriving possible biochemotypes based on predictions. The Prediction of Activity Spectra for Substances program (PASS) was used in the first step. In second step, structural similarity and scaffold-hopping technologies are employed. These technologies are used to derive biochemotypes from bioactivity predictions and the corresponding annotated biochemotypes from MDL Drug Data Report (MDDR) database. About a one million (982,889) commercially available compound library (CACL) has been tested using this process. This paper demonstrates the feasibility of automatically annotating biochemotypes for large libraries of compounds. Nevertheless, some issues need to be considered in order to improve the process. First, the prediction accuracy of PASS program has no significant correlation with the number of compounds in a training set. Larger training sets do not necessarily increase the maximal error of prediction (MEP), nor do they increase the hit structural diversity. Smaller training sets do not necessarily decrease MEP, nor do they decrease the hit structural diversity. Second, the success of systematic bioactivity prediction relies on modeling, training data, and the definition of bioactivities (biochemotype ontology). Unfortunately, the biochemotype ontology was not well developed in the PASS program. Consequently, "ill-defined" bioactivities can reduce the quality of predictions. This paper suggests the ways in which the systematic bioactivities prediction program should be improved.

Application of ionic liquid for extraction and separation of bioactive compounds from plants.

PubMed

Tang, Baokun; Bi, Wentao; Tian, Minglei; Row, Kyung Ho

2012-09-01

In recent years, ionic liquids (ILs), as green and designer solvents, have accelerated research in analytical chemistry. This review highlights some of the unique properties of ILs and provides an overview of the preparation and application of IL or IL-based materials to extract bioactive compounds in plants. IL or IL-based materials in conjunction with liquid-liquid extraction (LLE), ultrasonic-assisted extraction (UAE), microwave-assisted extraction (MAE), high performance liquid chromatography (HPLC) and solid-phase extraction (SPE) analytical technologies etc., have been applied successfully to the extraction or separation of bioactive compounds from plants. This paper reviews the available data and references to examine the advantages of IL and IL-based materials in these applications. In addition, the main target compounds reviewed in this paper are bioactive compounds with multiple therapeutic effects and pharmacological activities. Based on the importance of the targets, this paper reviews the applications of ILs, IL-based materials or co-working with analytical technologies. The exploitation of new applications of ILs on the extraction of bioactive compounds from plant samples is expected to increase. Copyright © 2012 Elsevier B.V. All rights reserved.

Natural Bioactive Compounds from Winery By-Products as Health Promoters: A Review

PubMed Central

Teixeira, Ana; Baenas, Nieves; Dominguez-Perles, Raul; Barros, Ana; Rosa, Eduardo; Moreno, Diego A.; Garcia-Viguera, Cristina

2014-01-01

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. PMID:25192288

Protective effects of sweet orange (Citrus sinensis) peel and their bioactive compounds on oxidative stress.

PubMed

Chen, Zong-Tsi; Chu, Heuy-Ling; Chyau, Charng-Cherng; Chu, Chin-Chen; Duh, Pin-Der

2012-12-15

Protective effects of sweet orange (Citrus sinensis) peel and their bioactive compounds on oxidative stress were investigated. According to HPLC-DAD and HPLC-MS/MS analysis, hesperidin (HD), hesperetin (HT), nobiletin (NT), and tangeretin (TT) were present in water extracts of sweet orange peel (WESP). The cytotoxic effect in 0.2mM t-BHP-induced HepG2 cells was inhibited by WESP and their bioactive compounds. The protective effect of WESP and their bioactive compounds in 0.2mM t-BHP-induced HepG2 cells may be associated with positive regulation of GSH levels and antioxidant enzymes, decrease in ROS formation and TBARS generation, increase in the mitochondria membrane potential and Bcl-2/Bax ratio, as well as decrease in caspase-3 activation. Overall, WESP displayed a significant cytoprotective effect against oxidative stress, which may be most likely because of the phenolics-related bioactive compounds in WESP, leading to maintenance of the normal redox status of cells. Copyright © 2012 Elsevier Ltd. All rights reserved.

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

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

Purification and identification of 4-allylbenzene-1,2-diol: an antilisterial and biofilm preventing compound from the leaves of Piper betle L. var Pachaikodi.

PubMed

Kavitha, Sekar; HariKrishnan, Adhikesavan; Jeevaratnam, Kadirvelu

2017-12-22

Antibiotic-resistant food-borne Listeriosis has been rising with up to 30% mortality threat in humans since several decades. Hence, discovering antilisterial from the extracts of ethnomedicinal plants may be of value as a novel antidote. In our preceding study, we reported that ethanolic extract of Piper betle L. var Pachaikodi leaves exhibited antibacterial activity towards Listeria monocytogenes MTCC 657. Consequently in the present study, the bioactive molecule responsible for anti-Listeria activity was purified and identified as 4-allylbenzene-1,2-diol. This identified bioactive compound may have significance while used as antimicrobials and/or food additives in food processing sector as evidenced by dual action: biofilm inhibition and pore formation on cell membrane.

Identification of Ideal Multi-targeting Bioactive Compounds Against Mur Ligases of Enterobacter aerogenes and Its Binding Mechanism in Comparison with Chemical Inhibitors.

PubMed

Chakkyarath, Vijina; Natarajan, Jeyakumar

2017-10-31

Enterobacter aerogenes have been reported as important opportunistic and multi-resistant bacterial pathogens for humans during the last three decades in hospital wards. The emergence of drug-resistant E. aerogenes demands the need for developing new drugs. Peptidoglycan is an important component of the cell wall of bacteria and the peptidoglycan biochemical pathway is considered as the best source of antibacterial targets. Within this pathway, four Mur ligases MurC, MurD, MurE, and MurF are responsible for the successive additions of L-alanine and suitable targets for developing novel antibacterial drugs. As an inference from this fact, we modeled the three-dimensional structure of above Mur ligases using best template structures available in PDB and analyzed its common binding features. Structural refinement and energy minimization of the predicted Mur ligases models is also being done using molecular dynamics studies. The models of Mur ligases were further investigated for in silico docking studies using bioactive plant compounds from the literature. Interestingly, these results indicate that four plant compounds Isojuripidine, Atroviolacegenin, Porrigenin B, and Nummularogenin showing better docking results in terms of binding energy and number of hydrogen bonds. All these four compounds are spirostan-based compounds with differences in side chains and the amino acid such as ASN, LYS, THR, HIS, ARG (polar) and PHE, GLY, VAL, ALA, MET (non-polar) playing active role in binding site of all four Mur ligases. Overall, in the predicted model, the four plant compounds with its binding features could pave way to design novel multi-targeted antibacterial plant-based bioactive compounds specific to Mur ligases for the treatment of Enterobacter infections.

Self-selection of plant bioactive compounds by sheep in response to challenge infection with Haemonchus contortus.

PubMed

Poli, Cesar H E C; Thornton-Kurth, Kara J; Legako, Jerrad F; Bremm, Carolina; Hampel, Viviane S; Hall, Jeffery; Ipharraguerre, Ignacio R; Villalba, Juan J

2018-06-12

Plant bioactives can potentially benefit herbivores through their effects on health and nutrition. The objective of this study was to determine the importance of polyphenols and terpenes on the ability of lambs to self-select these compounds when challenged by a parasitic infection and the subsequent impact on their health and productivity. Thirty-five lambs were housed in individual pens and assigned to five treatment groups (7 animals/group), where they received: 1) A basal diet of beet pulp:soybean meal (90:10) (CONTROL); 2) The same diet, but containing 0.3% of bioactive natural plant compounds extracted from grape, olive and pomegranate (BNP); 3) A simultaneous offer of the diets offered to the Control and BNP groups (Choice-Parasitized; CHP-1); 4) The Control diet, and when lambs developed a parasitic infection, the choice described for CHP-1 (CHP-2); and 5) The same choice as CHP-1, but animals did not experience a parasitic burden (Choice-Non-Parasitized; CHNP). Lambs, except CHNP, were dosed with 10,000 L 3 stage larvae of Haemonchus contortus. Infected lambs under choice treatments (CHP-1 and CHP-2) modified their feeding behavior in relation to the CHNP group as they increased their preference for the feed containing polyphenols and terpenes, interpreted as a behavior aimed at increasing the likelihood of encountering medicinal compounds and nutrients in the environment that restore health. This change in behavior corresponded with an improvement in feed conversion efficiency. However, an increased preference for the diet with added plant bioactives did not have an effect on parasitic burdens, hematological parameters, blood oxidation, or serum concentration of IgE. Copyright © 2018. Published by Elsevier Inc.

Diversity, Novelty, and Antimicrobial Activity of Endophytic Actinobacteria From Mangrove Plants in Beilun Estuary National Nature Reserve of Guangxi, China.

PubMed

Jiang, Zhong-Ke; Tuo, Li; Huang, Da-Lin; Osterman, Ilya A; Tyurin, Anton P; Liu, Shao-Wei; Lukyanov, Dmitry A; Sergiev, Petr V; Dontsova, Olga A; Korshun, Vladimir A; Li, Fei-Na; Sun, Cheng-Hang

2018-01-01

Endophytic actinobacteria are one of the important pharmaceutical resources and well known for producing different types of bioactive substances. Nevertheless, detection of the novelty, diversity, and bioactivity on endophytic actinobacteria isolated from mangrove plants are scarce. In this study, five different mangrove plants, Avicennia marina, Aegiceras corniculatum, Kandelia obovota, Bruguiera gymnorrhiza , and Thespesia populnea , were collected from Beilun Estuary National Nature Reserve in Guangxi Zhuang Autonomous Region, China. A total of 101 endophytic actinobacteria strains were recovered by culture-based approaches. They distributed in 7 orders, 15 families, and 28 genera including Streptomyces, Curtobacterium, Mycobacterium, Micrococcus, Brevibacterium, Kocuria, Nocardioides, Kineococcus, Kytococcus, Marmoricola, Microbacterium, Micromonospora, Actinoplanes, Agrococcus, Amnibacterium, Brachybacterium, Citricoccus, Dermacoccus, Glutamicibacter, Gordonia, Isoptericola, Janibacter, Leucobacter, Nocardia, Nocardiopsis, Pseudokineococcus, Sanguibacter , and Verrucosispora . Among them, seven strains were potentially new species of genera Nocardioides, Streptomyces, Amnibacterium, Marmoricola , and Mycobacterium . Above all, strain 8BXZ-J1 has already been characterized as a new species of the genus Marmoricola . A total of 63 out of 101 strains were chosen to screen antibacterial activities by paper-disk diffusion method and inhibitors of ribosome and DNA biosynthesis by means of a double fluorescent protein reporter. A total of 31 strains exhibited positive results in at least one antibacterial assay. Notably, strain 8BXZ-J1 and three other potential novel species, 7BMP-1, 5BQP-J3, and 1BXZ-J1, all showed antibacterial bioactivity. In addition, 21 strains showed inhibitory activities against at least one "ESKAPE" resistant pathogens. We also found that Streptomyces strains 2BBP-J2 and 1BBP-1 produce bioactive compound with inhibitory activity on protein biosynthesis as result of translation stalling. Meanwhile, Streptomyces strain 3BQP-1 produces bioactive compound inducing SOS-response due to DNA damage. In conclusion, this study proved mangrove plants harbored a high diversity of cultivable endophytic actinobacteria, which can be a promising source for discovery of novel species and bioactive compounds.

Diversity, Novelty, and Antimicrobial Activity of Endophytic Actinobacteria From Mangrove Plants in Beilun Estuary National Nature Reserve of Guangxi, China

PubMed Central

Jiang, Zhong-ke; Tuo, Li; Huang, Da-lin; Osterman, Ilya A.; Tyurin, Anton P.; Liu, Shao-wei; Lukyanov, Dmitry A.; Sergiev, Petr V.; Dontsova, Olga A.; Korshun, Vladimir A.; Li, Fei-na; Sun, Cheng-hang

2018-01-01

Endophytic actinobacteria are one of the important pharmaceutical resources and well known for producing different types of bioactive substances. Nevertheless, detection of the novelty, diversity, and bioactivity on endophytic actinobacteria isolated from mangrove plants are scarce. In this study, five different mangrove plants, Avicennia marina, Aegiceras corniculatum, Kandelia obovota, Bruguiera gymnorrhiza, and Thespesia populnea, were collected from Beilun Estuary National Nature Reserve in Guangxi Zhuang Autonomous Region, China. A total of 101 endophytic actinobacteria strains were recovered by culture-based approaches. They distributed in 7 orders, 15 families, and 28 genera including Streptomyces, Curtobacterium, Mycobacterium, Micrococcus, Brevibacterium, Kocuria, Nocardioides, Kineococcus, Kytococcus, Marmoricola, Microbacterium, Micromonospora, Actinoplanes, Agrococcus, Amnibacterium, Brachybacterium, Citricoccus, Dermacoccus, Glutamicibacter, Gordonia, Isoptericola, Janibacter, Leucobacter, Nocardia, Nocardiopsis, Pseudokineococcus, Sanguibacter, and Verrucosispora. Among them, seven strains were potentially new species of genera Nocardioides, Streptomyces, Amnibacterium, Marmoricola, and Mycobacterium. Above all, strain 8BXZ-J1 has already been characterized as a new species of the genus Marmoricola. A total of 63 out of 101 strains were chosen to screen antibacterial activities by paper-disk diffusion method and inhibitors of ribosome and DNA biosynthesis by means of a double fluorescent protein reporter. A total of 31 strains exhibited positive results in at least one antibacterial assay. Notably, strain 8BXZ-J1 and three other potential novel species, 7BMP-1, 5BQP-J3, and 1BXZ-J1, all showed antibacterial bioactivity. In addition, 21 strains showed inhibitory activities against at least one “ESKAPE” resistant pathogens. We also found that Streptomyces strains 2BBP-J2 and 1BBP-1 produce bioactive compound with inhibitory activity on protein biosynthesis as result of translation stalling. Meanwhile, Streptomyces strain 3BQP-1 produces bioactive compound inducing SOS-response due to DNA damage. In conclusion, this study proved mangrove plants harbored a high diversity of cultivable endophytic actinobacteria, which can be a promising source for discovery of novel species and bioactive compounds. PMID:29780376

Exploring the Mode of Action of Bioactive Compounds by Microfluidic Transcriptional Profiling in Mycobacteria

PubMed Central

Lim, Vivian; Naim, Ahmad Nazri Mohamed; Bifani, Pablo; Boshoff, Helena I. M.; Sambandamurthy, Vasan K.; Dick, Thomas; Hibberd, Martin L.; Schreiber, Mark; Rao, Srinivasa P. S.

2013-01-01

Most candidate anti-bacterials are identified on the basis of their whole cell anti-bacterial activity. A critical bottleneck in the early discovery of novel anti-bacterials is tracking the structure activity relationship (SAR) of the novel compounds synthesized during the hit to lead and lead optimization stage. It is often very difficult for medicinal chemists to visualize if the novel compounds synthesized for understanding SAR of a particular scaffold have similar molecular mechanism of action (MoA) as that of the initial hit. The elucidation of the molecular MoA of bioactive inhibitors is critical. Here, a new strategy and routine assay for MoA de-convolution, using a microfluidic platform for transcriptional profiling of bacterial response to inhibitors with whole cell activity has been presented. First a reference transcriptome compendium of Mycobacterial response to various clinical and investigational drugs was built. Using feature reduction, it was demonstrated that subsets of biomarker genes representative of the whole genome are sufficient for MoA classification and deconvolution in a medium-throughput microfluidic format ultimately leading to a cost effective and rapid tool for routine antibacterial drug-discovery programs. PMID:23935951

Gibberellins in Penicillium strains: Challenges for endophyte-plant host interactions under salinity stress.

PubMed

Leitão, Ana Lúcia; Enguita, Francisco J

2016-02-01

The genus Penicillium is one of the most versatile "mycofactories", comprising some species able to produce gibberellins, bioactive compounds that can modulate plant growth and development. Although plants have the ability to synthesize gibberellins, their levels are lower when plants are under salinity stress. It has been recognized that detrimental abiotic conditions, such as saline stress, have negative effects on plants, being the availability of bioactive gibberellins a critical factor for their growth under this conditions. This review summarizes the interplay existing between endophytic Penicillium strains and plant host interactions, with focus on bioactive gibberellins production as a fungal response that allows plants to overcome salinity stress. Copyright © 2015 Elsevier GmbH. All rights reserved.

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.

Relationship between fresh-packaged spinach leaves exposed to continuous light or dark and bioactive contents: Effects of cultivar, leaf size, and storage duration

USDA-ARS?s Scientific Manuscript database

Human-health benefits derived from consumption of fruits and vegetables are due to the many bioactive compounds found in produce. The concentrations of these bioactive compounds are heavily influenced by genetics (i.e. cultivar) and environment, especially the many pigments and vitamins that can ch...

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...

Marine Invertebrate Xenobiotic-Activated Nuclear Receptors: Their Application as Sensor Elements in High-Throughput Bioassays for Marine Bioactive Compounds

PubMed Central

Richter, Ingrid; Fidler, Andrew E.

2014-01-01

Developing high-throughput assays to screen marine extracts for bioactive compounds presents both conceptual and technical challenges. One major challenge is to develop assays that have well-grounded ecological and evolutionary rationales. In this review we propose that a specific group of ligand-activated transcription factors are particularly well-suited to act as sensors in such bioassays. More specifically, xenobiotic-activated nuclear receptors (XANRs) regulate transcription of genes involved in xenobiotic detoxification. XANR ligand-binding domains (LBDs) may adaptively evolve to bind those bioactive, and potentially toxic, compounds to which organisms are normally exposed to through their specific diets. A brief overview of the function and taxonomic distribution of both vertebrate and invertebrate XANRs is first provided. Proof-of-concept experiments are then described which confirm that a filter-feeding marine invertebrate XANR LBD is activated by marine bioactive compounds. We speculate that increasing access to marine invertebrate genome sequence data, in combination with the expression of functional recombinant marine invertebrate XANR LBDs, will facilitate the generation of high-throughput bioassays/biosensors of widely differing specificities, but all based on activation of XANR LBDs. Such assays may find application in screening marine extracts for bioactive compounds that could act as drug lead compounds. PMID:25421319

Deep Subseafloor Fungi as an Untapped Reservoir of Amphipathic Antimicrobial Compounds.

PubMed

Navarri, Marion; Jégou, Camille; Meslet-Cladière, Laurence; Brillet, Benjamin; Barbier, Georges; Burgaud, Gaëtan; Fleury, Yannick

2016-03-10

The evolving global threat of antimicrobial resistance requires a deep renewal of the antibiotic arsenal including the isolation and characterization of new drugs. Underexplored marine ecosystems may represent an untapped reservoir of novel bioactive molecules. Deep-sea fungi isolated from a record-depth sediment core of almost 2000 m below the seafloor were investigated for antimicrobial activities. This antimicrobial screening, using 16 microbial targets, revealed 33% of filamentous fungi synthesizing bioactive compounds with activities against pathogenic bacteria and fungi. Interestingly, occurrence of antimicrobial producing isolates was well correlated with the complexity of the habitat (in term of microbial richness), as higher antimicrobial activities were obtained at specific layers of the sediment core. It clearly highlights complex deep-sea habitats as chemical battlefields where synthesis of numerous bioactive compounds appears critical for microbial competition. The six most promising deep subseafloor fungal isolates were selected for the production and extraction of bioactive compounds. Depending on the fungal isolates, antimicrobial compounds were only biosynthesized in semi-liquid or solid-state conditions as no antimicrobial activities were ever detected using liquid fermentation. An exception was made for one fungal isolate, and the extraction procedure designed to extract amphipathic compounds was successful and highlighted the amphiphilic profile of the bioactive metabolites.

Curcuma longa L. leaves: Characterization (bioactive and antinutritional compounds) for use in human food in Brazil.

PubMed

Braga, Monick Cristina; Vieira, Ellen Caroline Silvério; de Oliveira, Tatianne Ferreira

2018-11-01

This study evaluated the physicochemical characterization of Curcuma longa L. leaves with respect to proximate composition, mineral content, the presence of antinutritional factors, content of bioactive compounds and antioxidant capacity, and color measurements of leaves in natura and leaves subjected to microwave drying, oven drying, and freeze-drying methods. The proximate composition showed appreciable levels of protein (39.5 g.100 g -1 ), carbohydrates (44.74 g.100 g -1 ), total fiber (34.47 g.100 g -1 ), soluble fiber (22.65 g.100 g -1 ), insoluble fiber (11.81 g.100 g -1 ), ash (13.81 g.100 g -1 ), and low lipid contents (2.47 g.100 g -1 ). No cyanogenic compounds were detected in both samples. Freeze-drying stood out as the method that led to the greatest reductions of the bioactive compounds (33.12-73.86%, dry basis) and antioxidant capacity when compared to the leaves in natura. Microwave drying was the preservation method that produced dry leaves with higher content of bioactive compounds and antioxidant capacity. Therefore, microwave drying produced dehydrated Curcuma longa L. leaves with the highest bioactive compounds and antioxidant activity. Copyright © 2018 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.

Isolation, purification, and characterization of antimicrobial compound 6-[1,2-dimethyl-6-(2-methyl-allyloxy)-hexyl]-3-(2-methoxy-phenyl)-chromen-4-one from Penicillium sp. HT-28.

PubMed

Kaur, Harpreet; Arora, Daljit Singh; Sharma, Vishal

2014-08-01

A fungal culture (Penicillium sp., HT-28), isolated from soil has been evaluated for its bioactivity, which showed broad spectrum antimicrobial activity and was effective against methicillin-resistant Staphylococcus aureus (MRSA) also. Statistical optimization of the medium by response surface methodology (RSM) enhanced the antimicrobial activity up to 1.8-fold. Column chromatography was used to isolate the active compound (A), which was characterized to be 6-[1,2-dimethyl-6-(2-methyl-allyloxy)-hexyl]-3-(2-methoxy-phenyl)-chromen-4-one by various spectroscopic techniques such as infrared (IR), (1)H and (13)C nuclear magnetic resonance (NMR) spectra, and mass spectroscopy. Minimum inhibitory concentration (MIC) of the active compound (A) ranged from 0.5 to 15 μg/mL. Viable cell count studies of the active compound (A) showed S. aureus, Escherichia coli, Staphylococcus epidermidis, and Salmonella typhimurium 1 to be the most sensitive. The compound retained its bioactivity after treating it at 100 °C for 1 h. Furthermore, the compound (A) when tested for its biosafety was found neither to be cytotoxic nor mutagenic. The study demonstrated that an apparently novel compound isolated from Penicillium sp. (HT-28) seems to be a stable and potent antimicrobial.

Chemistry, Nutrition, and Health-Promoting Properties of Hericium erinaceus (Lion's Mane) Mushroom Fruiting Bodies and Mycelia and Their Bioactive Compounds.

PubMed

Friedman, Mendel

2015-08-19

The culinary and medicinal mushroom Hericium erinaceus is widely consumed in Asian countries, but apparently not in the United States, for its nutritional and health benefits. To stimulate broader interest in the reported beneficial properties, this overview surveys and consolidates the widely scattered literature on the chemistry (isolation and structural characterization) of polysaccharides and secondary metabolites such as erinacines, hericerins, hericenones, resorcinols, steroids, mono- and diterpenes, and volatile aroma compounds, nutritional composition, food and industrial uses, and exceptional nutritional and health-promoting aspects of H. erinaceus. The reported health-promoting properties of the mushroom fruit bodies, mycelia, and bioactive pure compounds include antibiotic, anticarcinogenic, antidiabetic, antifatigue, antihypertensive, antihyperlipodemic, antisenescence, cardioprotective, hepatoprotective, nephroprotective, and neuroprotective properties and improvement of anxiety, cognitive function, and depression. The described anti-inflammatory, antioxidative, and immunostimulating properties in cells, animals, and humans seem to be responsible for the multiple health-promoting properties. A wide range of research advances and techniques are described and evaluated. The collated information and suggestion for further research might facilitate and guide further studies to optimize the use of the whole mushrooms and about 70 characterized actual and potential bioactive secondary metabolites to help prevent or treat human chronic, cognitive, and neurological diseases.

Nanoparticles and Controlled Delivery for Bioactive Compounds: Outlining Challenges for New “Smart-Foods” for Health

PubMed Central

Martínez-Ballesta, MCarment; García-Viguera, Cristina

2018-01-01

Nanotechnology is a field of research that has been stressed as a very valuable approach for the prevention and treatment of different human health disorders. This has been stressed as a delivery system for the therapeutic fight against an array of pathophysiological situations. Actually, industry has applied this technology in the search for new oral delivery alternatives obtained upon the modification of the solubility properties of bioactive compounds. Significant works have been made in the last years for testing the input that nanomaterials and nanoparticles provide for an array of pathophysiological situations. In this frame, this review addresses general questions concerning the extent to which nanoparticles offer alternatives that improve therapeutic value, while avoid toxicity, by releasing bioactive compounds specifically to target tissues affected by specific chemical and pathophysiological settings. In this regard, to date, the contribution of nanoparticles to protect encapsulated bioactive compounds from degradation as a result of gastrointestinal digestion and cellular metabolism, to enable their release in a controlled manner, enhancing biodistribution of bioactive compounds, and to allow them to target those tissues affected by biological disturbances has been demonstrated. PMID:29735897

An emerging strategy for evaluating the grades of Keemun black tea by combinatory liquid chromatography-Orbitrap mass spectrometry-based untargeted metabolomics and inhibition effects on α-glucosidase and α-amylase.

PubMed

Guo, Xuemei; Long, Piaopiao; Meng, Qilu; Ho, Chi-Tang; Zhang, Liang

2018-04-25

Quantitative analysis and untargeted liquid chromatography mass spectrum (LC-MS) based metabolomics of different grades of Keemun black tea (KBT) were conducted. Quantitative analysis did not show tight correlation between tea grades and contents of polyphenols, but untargeted metabolomics analysis revealed that high-grades KBT were distinguished from the low-grades. S-plot and Variable Importance (VIP) analysis gave 28 marker compounds responsible for the discrimination of different grades of KBT. The inhibitory effects of KBT on α-amylase and α-glucosidase were positively correlated to tea grades, and the correlation coefficient between each marker compound and inhibitory rate were calculated. Thirteen compounds were positively related to the anti-glycemic activity, and theasinensin A, afzelechin gallate and kaempferol-glucoside were confirmed as grade-related bioactive marker compounds by chemical and bioassay in effective fractions. This study suggested that combinatory metabolomics and bioactivities assay provided a new strategy for the classification of tea grades. Copyright © 2017 Elsevier Ltd. All rights reserved.

The Stability of Bioactive Compounds in Spaceflight Foods

NASA Technical Reports Server (NTRS)

Cooper, M. R.; Douglas, G. L.

2017-01-01

The status and stability of bioactive compounds in the processed and shelf-stable spaceflight food system have not previously been investigated though the presence of such compounds in aged space foods could have health significance for crews on long duration exploration missions. Over forty foods - either existing International Space Station (ISS) food provisioning items, newly developed foods for spaceflight, or commercially-available ready-to-eat foods - that were predicted to have a relatively high concentrations of one or more bioactive compounds (lycopene, lutein, omega-3 fatty acids, phenolics, sterols, and/or flavonoids) were selected for the study. Food samples were sent overnight to the Food Composition Laboratory of the Linus Pauling Institute at Oregon State University (Corvallis, OR) for bioactive compound analysis. Three packages of each product were blended together for the analysis to reduce package-to-package variability. All ISS food items and commercial foods were analyzed initially and after 12 and 24 months of 21degC storage. Food development occurred in a staggered fashion, so data collection for the newly developed foods continues. Lastly, sensory evaluation and additional temperature storage data (4degC, 35degC) for select foods were collected to establish additional stability parameters. Efficacious concentrations of lycopene, lutein, and omega-3 fatty acids were measured in limited spaceflight foods; two grams of sterols a day may be difficult to achieve with the current space diet. Total polyphenol delivery appears stable and adequate, but individual phenolic compounds vary in stability and were not specifically evaluated in this study. The data suggests that some bioactive compounds, like lycopene and lutein, degrade and then plateau at some equilibrium concentration. The anthocyanin stability appears to be related to storage temperature and food matrix, and lutein stability in leafy vegetables may be impacted by storage temperature. Because of the limited number of foods with high concentrations of the bioactive compounds, additional menu variety, formulation optimization, and reduced temperature storage will be required to ensure delivery of several bioactive compounds in the space food system. Validation of stability to five years will enable provisioning of these functional foods within the space food system for a mission to Mars.

Optimization of drying process and pressurized liquid extraction for recovery of bioactive compounds from avocado peel by-product.

PubMed

Figueroa, Jorge G; Borrás-Linares, Isabel; Lozano-Sánchez, Jesús; Quirantes-Piné, Rosa; Segura-Carretero, Antonio

2018-04-16

The aim of the present study was to optimize the extraction of phenolic compounds in avocado peel using pressurized liquid extraction (PLE) with GRAS solvents. Response surface methodology (RSM) based on Central Composite Design 2 2 model was used in order to optimize PLE conditions. Moreover, the effect of air drying temperature on the total polyphenol content (TPC) and individual phenolic compounds concentration were evaluated. The quantification of individual compounds was performed by HPLC-DAD-ESI-TOF-MS. The optimized extraction conditions were 200°C as extraction temperature and 1:1 v/v as ethanol/water ratio. Regarding to the effect of drying, the highest TPC was obtained with a drying temperature of 85°C. Forty seven phenolic compounds were quantified in the obtained extracts, showing that phenolic acids found to be the more stables compounds to drying process, while procyanidins were the more thermolabiles analytes. To our knowledge, this is the first available study in which phenolic compounds extraction was optimized using PLE and such amount of phenolic compounds was quantified in avocado peel. These results confirm that PLE represents a powerful tool to obtain avocado peel extracts with high concentration in bioactive compounds suitable for its use in the food, cosmetic or pharmaceutical sector. © 2018 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

An Investigation into Spent Coffee Waste as a Renewable Source of Bioactive Compounds and Industrially Important Sugars.

PubMed

Scully, Damhan S; Jaiswal, Amit K; Abu-Ghannam, Nissreen

2016-11-21

Conventional coffee brewing techniques generate vast quantities of spent espresso grounds (SEGs) rich in lignocellulose and valuable bioactives. These bioactive compounds can be exploited as a nutraceutical or used in a range of food products, while breakdown of lignocellulose generates metabolizable sugars that can be used for the production of various high-value products such as biofuels, amino acids and enzymes. Response surface methodology (RSM) was used to optimize the enzymatic saccharification of lignocellulose in SEGs following a hydrothermal pretreatment. A maximum reducing sugar yield was obtained at the following optimized hydrolysis conditions: 4.97 g of pretreated SEGs, 120 h reaction time, and 1246 and 250 µL of cellulase and hemicellulase, respectively. Industrially important sugars (glucose, galactose and mannose) were identified as the principal hydrolysis products under the studied conditions. Total flavonoids ( p = 0.0002), total polyphenols ( p = 0.03) and DPPH free-radical scavenging activity ( p = 0.004) increased significantly after processing. A 14-fold increase in caffeine levels was also observed. This study provides insight into SEGs as a promising source of industrially important sugars and polyphenols.

Microwave-assisted extraction for Hibiscus sabdariffa bioactive compounds.

PubMed

Pimentel-Moral, Sandra; Borrás-Linares, Isabel; Lozano-Sánchez, Jesús; Arráez-Román, David; Martínez-Férez, Antonio; Segura-Carretero, Antonio

2018-07-15

H. sabdariffa has demonstrated positive results against chronic diseases due to the presence of phytochemicals, mainly phenolic compounds. The extraction process of bioactive compounds increases the efficient collection of extracts with high bioactivity. Microwave-Assisted Extraction (MAE) constituted a "green technology" widely employed for plant matrix. In this work, the impact of temperature (50-150 °C), composition of extraction solvent (15-75% EtOH) and extraction time (5-20 min) on the extraction yield and individual compounds concentrations were evaluated. Furthermore, the characterization of 16 extracts obtained was performed by HPLC-ESI-TOF-MS. The results showed that 164 °C, 12.5 min, 45% ethanol was the best extraction condition, although glycoside flavonoids were degraded. Besides that, the optimal conditions for extraction yield were 164 °C, 60% ethanol and 22 min. Thus, temperature and solvent concentration have demonstrated to be potential factors in MAE for obtaining bioactive compounds from H. sabdariffa. Copyright © 2018 Elsevier B.V. All rights reserved.

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.

Encapsulation of bioactive compound from extracted jasmine flower using β-Cyclodextrin via electrospray

NASA Astrophysics Data System (ADS)

Rahmam., S.; Naim., M. N.; Ng., E.; Mokhtar, M. Nn; Abu Bakar, N. F.

2016-06-01

The ability of electrospray to encapsulate the bioactive compound extracted from Jasmine flower with β-Cyclodextrion (β-CD) without any thermal-assisted processing was demonstrated in this study. The extraction of Jasmine compound were conducted using sonicator at 70 000 Hz, for 10 minutes and followed by mixing of the filtered compound with β-CD. Then, the mixture was electrosprayed under a stable Taylor cone jet mode at the voltage of 4 - 5 kV, with flow rate of 0.2 ml/hour. The aluminum substrate that used for collecting the deposit was placed at 30 cm from the needle's tip to allow the occurrence of evaporation and droplet fission until the droplet transform to solid particles. Characteristics of solidified bioactive compound from Jasmine flower (non-encapsulated compound) and solidified bioactive compound with β-CD (encapsulated compound) were studied in this work. From SEM images, it can be observed that the particles size distribution of encapsulated compound deposits have better deposition array and did not aggregate with each other compared to the non-encapsulated compound. FE-SEM images of encapsulated compound deposits indicate more solid crystal looks while non-encapsulated compound was obtained in the porous form. The electrospray process in this work has successfully encapsulated the Jasmine compound with β-CD without any thermal-assisted process. The encapsulation occurrence was determined using FTIR analysis. Identical peaks that referred to the β-CD were found on the encapsulated compound demonstrated that most deposits were encapsulated with β-CD.

A Dereplication and Bioguided Discovery Approach to Reveal New Compounds from a Marine-Derived Fungus Stilbella fimetaria

PubMed Central

Kildgaard, Sara; Subko, Karolina; Phillips, Emma; Goidts, Violaine; de la Cruz, Mercedes; Díaz, Caridad; Gotfredsen, Charlotte H.; Frisvad, Jens C.; Nielsen, Kristian F.; Larsen, Thomas O.

2017-01-01

A marine-derived Stilbella fimetaria fungal strain was screened for new bioactive compounds based on two different approaches: (i) bio-guided approach using cytotoxicity and antimicrobial bioassays; and (ii) dereplication based approach using liquid chromatography with both diode array detection and high resolution mass spectrometry. This led to the discovery of several bioactive compound families with different biosynthetic origins, including pimarane-type diterpenoids and hybrid polyketide-non ribosomal peptide derived compounds. Prefractionation before bioassay screening proved to be a great aid in the dereplication process, since separate fractions displaying different bioactivities allowed a quick tentative identification of known antimicrobial compounds and of potential new analogues. A new pimarane-type diterpene, myrocin F, was discovered in trace amounts and displayed cytotoxicity towards various cancer cell lines. Further media optimization led to increased production followed by the purification and bioactivity screening of several new and known pimarane-type diterpenoids. A known broad-spectrum antifungal compound, ilicicolin H, was purified along with two new analogues, hydroxyl-ilicicolin H and ilicicolin I, and their antifungal activity was evaluated. PMID:28805711

Preparation of S-Allylcysteine-Enriched Black Garlic Juice and Its Antidiabetic Effects in Streptozotocin-Induced Insulin-Deficient Mice.

PubMed

Kim, Jun Ho; Yu, Su Hyun; Cho, Yun Jeong; Pan, Jeong Hoon; Cho, Hyung Taek; Kim, Jeong Ho; Bong, Hyejin; Lee, Yeojin; Chang, Moon Han; Jeong, Ye Jin; Choi, Garam; Kim, Young Jun

2017-01-18

S-Allylcysteine (SAC), produced in large amounts during the aging process of garlic via enzymatic hydrolysis, is known as a key compound responsible for the multiple pharmacological activities of aged black garlic. This study investigated the effects of enzyme- and high hydrostatic pressure (HHP)-assisted extraction on the content of the bioactive compounds, including SAC, in black garlic juice (BGJ) and evaluated the antidiabetic effects of SAC-enriched BGJ in streptozotocin (STZ)-treated mice. The aging process increased the contents of SAC, total polyphenols, and total flavonoids in garlic juice. More importantly, pretreatment of pectinase cocktail with HHP resulted in a greater increase in those compounds during aging. Enzyme-treated BGJ reduced hyperglycemia and improved islet architecture and β-cell function in STZ-treated mice. Moreover, these effects were more potent than those of BGJ prepared by the conventional aging process. These findings provide useful information for the production of black garlic with improved bioactivities.

Potential of Fruit Wastes as Natural Resources of Bioactive Compounds

PubMed Central

Deng, Gui-Fang; Shen, Chen; Xu, Xiang-Rong; Kuang, Ru-Dan; Guo, Ya-Jun; Zeng, Li-Shan; Gao, Li-Li; Lin, Xi; Xie, Jie-Feng; Xia, En-Qin; Li, Sha; Wu, Shan; Chen, Feng; Ling, Wen-Hua; Li, Hua-Bin

2012-01-01

Fruit wastes are one of the main sources of municipal waste. In order to explore the potential of fruit wastes as natural resources of bioactive compounds, the antioxidant potency and total phenolic contents (TPC) of lipophilic and hydrophilic components in wastes (peel and seed) of 50 fruits were systematically evaluated. The results showed that different fruit residues had diverse antioxidant potency and the variation was very large. Furthermore, the main bioactive compounds were identified and quantified, and catechin, cyanidin 3-glucoside, epicatechin, galangin, gallic acid, homogentisic acid, kaempferol, and chlorogenic acid were widely found in these residues. Especially, the values of ferric-reducing antioxidant power (FRAP), trolox equivalent antioxidant capacity (TEAC) and TPC in the residues were higher than in pulps. The results showed that fruit residues could be inexpensive and readily available resources of bioactive compounds for use in the food and pharmaceutical industries. PMID:22942704

Potential of fruit wastes as natural resources of bioactive compounds.

PubMed

Deng, Gui-Fang; Shen, Chen; Xu, Xiang-Rong; Kuang, Ru-Dan; Guo, Ya-Jun; Zeng, Li-Shan; Gao, Li-Li; Lin, Xi; Xie, Jie-Feng; Xia, En-Qin; Li, Sha; Wu, Shan; Chen, Feng; Ling, Wen-Hua; Li, Hua-Bin

2012-01-01

Fruit wastes are one of the main sources of municipal waste. In order to explore the potential of fruit wastes as natural resources of bioactive compounds, the antioxidant potency and total phenolic contents (TPC) of lipophilic and hydrophilic components in wastes (peel and seed) of 50 fruits were systematically evaluated. The results showed that different fruit residues had diverse antioxidant potency and the variation was very large. Furthermore, the main bioactive compounds were identified and quantified, and catechin, cyanidin 3-glucoside, epicatechin, galangin, gallic acid, homogentisic acid, kaempferol, and chlorogenic acid were widely found in these residues. Especially, the values of ferric-reducing antioxidant power (FRAP), trolox equivalent antioxidant capacity (TEAC) and TPC in the residues were higher than in pulps. The results showed that fruit residues could be inexpensive and readily available resources of bioactive compounds for use in the food and pharmaceutical industries.

Atmospheric-Pressure Cold Plasmas Used to Embed Bioactive Compounds in Matrix Material for Active Packaging of Fruits and Vegetables

NASA Astrophysics Data System (ADS)

Fernandez, Sulmer; Pedrow, Patrick; Powers, Joseph; Pitts, Marvin

2009-10-01

Active thin film packaging is a technology with the potential to provide consumers with new fruit and vegetable products-if the film can be applied without deactivating bioactive compounds.Atmospheric pressure cold plasma (APCP) processing can be used to activate monomer with concomitant deposition of an organic plasma polymerized matrix material and to immobilize a bioactive compound all at or below room temperature.Aims of this work include: 1) immobilize an antimicrobial in the matrix; 2) determine if the antimicrobial retains its functionality and 3) optimize the reactor design.The plasma zone will be obtained by increasing the voltage on an electrode structure until the electric field in the feed material (argon + monomer) yields electron avalanches. Results will be described using Red Delicious apples.Prospective matrix precursors are vanillin and cinnamic acid.A prospective bioactive compound is benzoic acid.

Bioactive Lignans from Zanthoxylum alatum Roxb. stem bark with cytotoxic potential.

PubMed

Mukhija, Minky; Lal Dhar, Kanaya; Nath Kalia, Ajudhia

2014-02-27

Zanthoxylum alatum is used in traditional medicinal systems for number of disorders like cholera, diabetes, cough, diarrhea, fever, headache, microbial infections, toothache, inflammation and cancer. The aim of the present study was to evaluate Zanthoxylum alatum stem bark for its cytotoxic potential and to isolate the bioactive constituents. Cytotoxicity of the different extracts and isolated compounds was studied on lung carcinoma cell line (A549) and pancreatic carcinoma cell line (MIA-PaCa) using MTT assay. Isolation of compounds from most active extract (petroleum ether) was done on silica gel column. Structure elucidation was done by using various spectrophotometric techniques like UV, IR, (1)H NMR, (13)C NMR and mass spectroscopy. The type of cell death caused by most active compound C was explored by fluorescence microscopy using the acridine orange/ethidium bromide method. Petroleum ether extract of plant has shown significant cytotoxic potential. Three lignans sesamin (A), kobusin (B), and 4'O demethyl magnolin (C) has been isolated. All lignans showed cytotoxic activities in different ranges. Compound C was the novel bioactive compound from a plant source and found to be most active. In apoptosis study, treatment caused typical apoptotic morphological changes. It enhances the apoptosis at IC50 dose (21.72 µg/mL) however showing necrotic cell death at higher dose after 24h on MIA-PaCa cell lines. Petroleum ether extract (60-80 °C) of Zanthoxylum alatum has cytotoxic potential. The lignans isolated from the petroleum ether extract were responsible for the cytotoxic potential of the extract. 4'O demethyl magnolin was novel compound from Zanthoxylum alatum. Hence the Zanthoxylum alatum can be further explored for the development of anticancer drug. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

Metabolomic and functional genomic analyses reveal varietal differences in bioactive compounds of cooked rice

USDA-ARS?s Scientific Manuscript database

Emerging evidence supports that cooked brown rice (Oryza sativa L.) contains metabolites with biomedical activities, yet little is known about the genetic diversity that is responsible for metabolite variation and differences in health beneficial traits. Metabolites from cooked brown rice of ten div...

Activation of ERK signaling and induction of colon cancer cell death by piperlongumine

USDA-ARS?s Scientific Manuscript database

Piperlongumine (PPLGM) is a bioactive compound isolated from long peppers that shows selective toxicity towards a variety of cancer cell types including colon cancer. The signaling pathways that lead to cancer cell death in response to PPLGM exposure have not been previously identified. Our objectiv...

Bioactive Compounds and Antioxidant Capacity of Camarosa and Selva Strawberries (Fragaria x ananassa Duch.).

PubMed

Van De Velde, Franco; Tarola, Anna M; Güemes, Daniel; Pirovani, María E

2013-03-25

Strawberries represent an important source of bioactive compounds due to their vitamin C and phenolic compound levels, which present high antioxidant effects, beneficial for the maintenance of consumer's health. Argentina is the second largest strawberry producer in The Common Market of the Southern Cone (MERCOSUR), covering the main export destinations of Argentinian strawberries, i.e. , Canada, United States, and European Union. Information about the bioactive compound occurrence and antioxidant capacity of these fruits is scarce or not available. Health related compounds of strawberry cultivars ( Camarosa and Selva ) from different zones of Argentina were investigated. Vitamin C content was in the same range for both studied cultivars. However, Camarosa strawberries, which are the most cultivated, consumed, and exported berries in Argentina, presented higher total phenolic and anthocyanins content, and consequently better in vitro antioxidant capacity. Moreover, there were differences in the occurrence and concentration in the phenolic compound profiles for both cultivars. Camarosa cultivar presented higher content of anthocyanidins, and Selva showed higher total ellagic acid content. The research shows that Argentina's strawberries are an interesting source of bioactive compounds comparable to those in other parts of the world.

Determining whether curcumin degradation/condensation is actually bioactivation (Review).

PubMed

Jankun, Jerzy; Wyganowska-Świątkowska, Marzena; Dettlaff, Katarzyna; Jelińska, Anna; Surdacka, Anna; Wątróbska-Świetlikowska, Dorota; Skrzypczak-Jankun, Ewa

2016-05-01

Curcumin has been shown to exert therapeutic or protective effects against a variety of diseases, such as cancer, pulmonary diseases, neurological, liver, metabolic, autoimmune, cardiovascular diseases and numerous other chronic ailments. Over 116 clinical studies on curcumin in humans were registered with the US National Institutes of Health in 2015. However, it is mystifying how curcumin can be so effective in the treatment of many diseases since it has very low water solubility and bioavailability. Furthermore, curcumin is not stable under various conditions; its degradation or condensation into different bioactive compounds may be responsible for its biological activities rather than curcumin itself. In this review, we provide evidence of curcumin degradation and condensation into different compounds which have or may have health benefits themselves. Literature reviews strongly suggest that these molecules contribute to the observed health benefits, rather than curcumin itself.

Laucysteinamide A, a Hybrid PKS/NRPS Metabolite from a Saipan Cyanobacterium, cf. Caldora penicillata.

PubMed

Zhang, Chen; Naman, C Benjamin; Engene, Niclas; Gerwick, William H

2017-04-14

A bioactivity guided study of a cf. Caldora penicillata species, collected during a 2013 expedition to the Pacific island of Saipan, Northern Mariana Islands (a commonwealth of the USA), led to the isolation of a new thiazoline-containing alkaloid, laucysteinamide A ( 1 ). Laucysteinamide A is a new monomeric analogue of the marine cyanobacterial metabolite, somocystinamide A ( 2 ), a disulfide-bonded dimeric compound that was isolated previously from a Fijian marine cyanobacterium. The structure and absolute configuration of laucysteinamide A ( 1 ) was determined by a detailed analysis of its NMR, MS, and CD spectra. In addition, the highly bioactive lipid, curacin D ( 3 ), was also found to be present in this cyanobacterial extract. The latter compound was responsible for the potent cytotoxicity of this extract to H-460 human non-small cell lung cancer cells in vitro.

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

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

Medicinal halophytes: potent source of health promoting biomolecules with medical, nutraceutical and food applications.

PubMed

Ksouri, Riadh; Ksouri, Wided Megdiche; Jallali, Inès; Debez, Ahmed; Magné, Christian; Hiroko, Isoda; Abdelly, Chedly

2012-12-01

Salt-tolerant plants grow in a wide variety of saline habitats, from coastal regions, salt marshes and mudflats to inland deserts, salt flats and steppes. Halophytes living in these extreme environments have to deal with frequent changes in salinity level. This can be done by developing adaptive responses including the synthesis of several bioactive molecules. Consequently, several salt marsh plants have traditionally been used for medical, nutritional, and even artisanal purposes. Currently, an increasing interest is granted to these species because of their high content in bioactive compounds (primary and secondary metabolites) such as polyunsaturated fatty acids, carotenoids, vitamins, sterols, essential oils (terpenes), polysaccharides, glycosides, and phenolic compounds. These bioactive substances display potent antioxidant, antimicrobial, anti-inflammatory, and anti-tumoral activities, and therefore represent key-compounds in preventing various diseases (e.g. cancer, chronic inflammation, atherosclerosis and cardiovascular disorder) and ageing processes. The ongoing research will lead to the utilisation of halophytes as a new source of healthy products as functional foods, nutraceuticals or active principles in several industries. This contribution focuses on the ethnopharmacological uses of halophytes in traditional medicine and reviews recent investigations on their biological activities and nutraceuticals. The work is distributed according to the different families of nutraceuticals (lipids, vitamins, proteins, glycosides, phenolic compounds, etc.) discussing the analytical techniques employed for their determination. Information about the claimed health promoting effects of the different families of nutraceuticals is also provided together with data on their application.

A Review of Nanoliposomal Delivery System for Stabilization of Bioactive Omega-3 Fatty Acids

PubMed Central

Hadian, Zahra

2016-01-01

Currently, bioactive compounds are required in the design and production of functional foods, with the aim of improving the health status of consumers all around the world. Various epidemiological and clinical studies have demonstrated the salutary role of eicosapentaenoic acid (EPA, 22:6 n−3) and docosahexaenoic acid (DHA, 22:5 n−3) in preventing diseases and reducing mortality from cardiovascular diseases. The unsaturated nature of bioactive lipids leads to susceptibility to oxidation under environmental conditions. Oxidative deterioration of omega-3 fatty acids can cause the reduction in their nutritional quality and sensory properties. Encapsulation of these fatty acids could create a barrier against reaction with harmful environmental factors. Currently, fortification of foods containing bioactive omega-3 fatty acids has found great application in the food industries of different countries. Previous studies have suggested that nano-encapsulation has significant effects on the stability of physical and chemical properties of bioactive compounds. Considering the functional role of omega-3 fatty acids, this study has provided a literature review on applications of nanoliposomal delivery systems for encapsulation of these bioactive compounds. PMID:26955449

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 benzopyrone derivatives from new recombinant fusant of marine Streptomyces.

PubMed

El-Gendy, Mervat M A; Shaaban, M; El-Bondkly, A M; Shaaban, K A

2008-07-01

In our searching program for bioactive secondary metabolites from marine Streptomycetes, three microbial benzopyrone derivatives (1-3), 7-methylcoumarin (1) and two flavonoides, rhamnazin (2) and cirsimaritin (3), were obtained during the working up of the ethyl acetate fraction of a marine Streptomyces fusant obtained from protoplast fusion between Streptomyces strains Merv 1996 and Merv 7409. The structures of the three compounds (1-3) were established by nuclear magnetic resonance, mass, UV spectra, and by comparison with literature data. Marine Streptomyces strains were identified based on their phenotypic and chemotypic characteristics as two different bioactive strains of the genus Streptomyces. We described here the fermentation, isolation, as well as the biological activity of these bioactive compounds. The isolated compounds (1-3) are reported here as microbial products for the first time.

Biomolecules and Natural Medicine Preparations: Analysis of New Sources of Bioactive Compounds from Ribes and Rubus spp. Buds.

PubMed

Donno, Dario; Mellano, Maria Gabriella; Cerutti, Alessandro Kim; Beccaro, Gabriele Loris

2016-02-05

It is well known that plants are important sources for the preparation of natural remedies as they contain many biologically active compounds. In particular, polyphenols, terpenic compounds, organic acids, and vitamins are the most widely occurring groups of phytochemicals. Some endemic species may be used for the production of herbal preparations containing phytochemicals with significant bioactivity, as antioxidant activity and anti-inflammatory capacities, and health benefits. Blackberry sprouts and blackcurrant buds are known to contain appreciable levels of bioactive compounds, including flavonols, phenolic acids, monoterpenes, vitamin C, and catechins, with several clinical effects. The aim of this research was to perform an analytical study of blackcurrant and blackberry bud-preparations, in order to identify and quantify the main biomarkers, obtaining a specific phytochemical fingerprint to evaluate the single botanical class contribution to total phytocomplex and relative bioactivity, using a High Performance Liquid Chromatograph-Diode Array Detector; the same analyses were performed both on the University laboratory and commercial preparations. Different chromatographic methods were used to determine concentrations of biomolecules in the preparations, allowing for quantification of statistically significant differences in their bioactive compound content both in the case of Ribes nigrum and Rubus cultivated varieties at different harvest stages. In blackcurrant bud-extracts the most important class was organic acids (50.98%) followed by monoterpenes (14.05%), while in blackberry preparations the main bioactive classes were catechins (50.06%) and organic acids (27.34%). Chemical, pharmaceutical and agronomic-environmental knowledge could be important for obtaining label certifications for the valorization of specific genotypes, with high clinical and pharmaceutical value: this study allowed to develop an effective tool for the natural preparation quality control and bioactivity evaluation through the chemical fingerprinting of bud preparations.

Potency of Purple Sweet Potato’s Anthocyanin as Biosensor for Detection of Chemicals in Food Products

NASA Astrophysics Data System (ADS)

Wulandari, A.; Sunarti, TC; Fahma, F.; Noor, E.

2018-05-01

Bioactive compounds such as anthocyanin are a natural ingredient that produces color with typical specificity. Anthocyanin from Ayamurasaki purple sweet potato (Ipomoea batatas L.) was extracted in ethanol and used as crude anthocyanin extracts. The color of bioactive anthocyanin can be used as a biosensor to detect chemical of food products because it provides a unique color change. However, the each bioactive has a particular sensitivity and selectivity to a specific chemical, so it is necessary to select and test the selectivity. Six chemicals, which were sodium nitrite, sodium benzoate, sodium cyclamate (food additives), formalin, borax (illegal food preservatives), and residue fertilizer (urea) were tested and observed for its color change. The results showed that the bioactive anthocyanin of purple sweet potato with the concentration of ± 42.65 ppm had better selectivity and sensitivity to sodium nitrite with a detection limit of 100 ppm, where the color change response time ranged from 15-20 minutes. The selectivity and sensitivity of this bioactive can be used as the basic information for the development of biosensor.

Bioactive compounds in dairy products and their relation to neurodegenerative disease

USDA-ARS?s Scientific Manuscript database

Enhancement of nervous system function and cognitive ability may be aided by bioactive compounds found in dairy products, including calcium-binding phosphopeptides and peptides derived from casein and beta-lactoglobulin. These peptides inhibit angiotensin converting enzyme I, scavenge radicals, red...

Phytochemical-rich foods inhibit the growth of pathogenic trichomonads

USDA-ARS?s Scientific Manuscript database

Plants produce bioactive organic compounds known as secondary metabolites that possess numerous health benefits, including antimicrobial properties. One mechanism of action of these plant bioactive compounds targets the disruption of cell membranes. The main of objective of the present study was t...

Extraction and determination of bioactive compounds from bee pollen.

PubMed

Ares, Ana M; Valverde, Silvia; Bernal, José L; Nozal, María J; Bernal, José

2018-01-05

Since ancient times bee pollen has been considered a good source of bioactive substances and energy. Taking into account the current demand for healthy and natural foods, it is not surprising that bee pollen has been attracting commercial interest in recent years, making it one of the most widely consumed food supplements. It has been extensively reported that bee pollen contains several health-promoting compounds, such as proteins, amino acids, lipids, phenolic compounds, vitamins or minerals. Thus, this study aims to give an overview of the extraction and determination techniques of several of the above-mentioned compounds which have been published in the last few years (2011-2017). The design of the study is in accordance with the different families of bioactive compounds, and the extraction procedures together with the analytical techniques employed and their determination are discussed. A list of some of the most relevant applications is provided for each category, including a brief summary of the experimental conditions. The references included will provide the reader with a comprehensive overview of and insight into the analysis of bioactive compounds from bee pollen. Copyright © 2017 Elsevier B.V. All rights reserved.

Toxins and bioactive compounds from cyanobacteria and their implications on human health.

PubMed

Rao, P V Lakshmana; Gupta, Nidhi; Bhaskar, A S B; Jayaraj, R

2002-07-01

Many species of cyanobacteria (blue-green algae) produce secondary metabolites with potent biotoxic or cytotoxic properties. These metabolites differ from the intermediates and cofactor compounds that are essential for cell structural synthesis and energy transduction. The mass growth of cyanobacteria which develop in fresh, brackish and, marine waters commonly contain potent toxins. Cyanobacterial toxins or cyanotoxins are responsible for or implicated in animal poisoning, human gastroenteritis, dermal contact irritations and primary liver cancer in humans. These toxins (microcystins, nodularins, saxitoxins, anatoxin-a, anatoxin-a(s), cylindrospermopsin) are structurally diverse and their effects range from liver damage, including liver cancer to neurotoxicity. Several incidents of human illness and more recently, the death of 60 haemodialysis patients in Caruaru, Brazil, have been linked to the presence of microcystins in water. In response to the growing concern about the non-lethal acute and chronic effects of microcystins, World Health Organization has recently set a new provisional guideline value for microcystin-LR of 1.0 microg/L in drinking water. Cyanobacteria including microcystin-producing strains produce a large number of peptide compounds, e.g. micropeptins, cyanopeptolins, microviridin, circinamide, aeruginosin, with varying bioactivities and potential pharmacological application. This article discusses briefly cyanobacterial toxins and their implications on human health.

Advancement into the Arctic Region for Bioactive Sponge Secondary Metabolites

PubMed Central

Abbas, Samuel; Kelly, Michelle; Bowling, John; Sims, James; Waters, Amanda; Hamann, Mark

2011-01-01

Porifera have long been a reservoir for the discovery of bioactive compounds and drug discovery. Most research in the area has focused on sponges from tropical and temperate waters, but more recently the focus has shifted to the less accessible colder waters of the Antarctic and, to a lesser extent, the Arctic. The Antarctic region in particular has been a more popular location for natural products discovery and has provided promising candidates for drug development. This article reviews groups of bioactive compounds that have been isolated and reported from the southern reaches of the Arctic Circle, surveys the known sponge diversity present in the Arctic waters, and details a recent sponge collection by our group in the Aleutian Islands, Alaska. The collection has yielded previously undescribed sponge species along with primary activity against opportunistic infectious diseases, malaria, and HCV. The discovery of new sponge species and bioactive crude extracts gives optimism for the isolation of new bioactive compounds from a relatively unexplored source. PMID:22163194

Plastids of Marine Phytoplankton Produce Bioactive Pigments and Lipids

PubMed Central

Heydarizadeh, Parisa; Poirier, Isabelle; Loizeau, Damien; Ulmann, Lionel; Mimouni, Virginie; Schoefs, Benoît; Bertrand, Martine

2013-01-01

Phytoplankton is acknowledged to be a very diverse source of bioactive molecules. These compounds play physiological roles that allow cells to deal with changes of the environmental constrains. For example, the diversity of light harvesting pigments allows efficient photosynthesis at different depths in the seawater column. Identically, lipid composition of cell membranes can vary according to environmental factors. This, together with the heterogenous evolutionary origin of taxa, makes the chemical diversity of phytoplankton compounds much larger than in terrestrial plants. This contribution is dedicated to pigments and lipids synthesized within or from plastids/photosynthetic membranes. It starts with a short review of cyanobacteria and microalgae phylogeny. Then the bioactivity of pigments and lipids (anti-oxidant, anti-inflammatory, anti-mutagenic, anti-cancer, anti-obesity, anti-allergic activities, and cardio- neuro-, hepato- and photoprotective effects), alone or in combination, is detailed. To increase the cellular production of bioactive compounds, specific culture conditions may be applied (e.g., high light intensity, nitrogen starvation). Regardless of the progress made in blue biotechnologies, the production of bioactive compounds is still limited. However, some examples of large scale production are given, and perspectives are suggested in the final section. PMID:24022731

Design of cinnamaldehyde amino acid Schiff base compounds based on the quantitative structure-activity relationship.

PubMed

Wang, Hui; Jiang, Mingyue; Li, Shujun; Hse, Chung-Yun; Jin, Chunde; Sun, Fangli; Li, Zhuo

2017-09-01

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 Penicillium citrinum (P. citrinum) were analysed. The QSAR models ( R 2  = 0.9346 for A. niger , R 2  = 0.9590 for P. citrinum, ) were constructed and validated. The models indicated that the molecular polarity and the Max atomic orbital electronic population had a significant effect on antifungal activity. Based on the best QSAR models, two new compounds were designed and synthesized. Antifungal activity tests proved that both of them have great bioactivity against the selected fungi.

Design of cinnamaldehyde amino acid Schiff base compounds based on the quantitative structure–activity relationship

PubMed Central

Wang, Hui; Jiang, Mingyue; Hse, Chung-Yun; Jin, Chunde; Sun, Fangli; Li, Zhuo

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 Penicillium citrinum (P. citrinum) were analysed. The QSAR models (R2 = 0.9346 for A. niger, R2 = 0.9590 for P. citrinum,) were constructed and validated. The models indicated that the molecular polarity and the Max atomic orbital electronic population had a significant effect on antifungal activity. Based on the best QSAR models, two new compounds were designed and synthesized. Antifungal activity tests proved that both of them have great bioactivity against the selected fungi. PMID:28989758

Chemical composition and bioactive compounds of garlic (Allium sativum L.) as affected by pre- and post-harvest conditions: A review.

PubMed

Martins, Natália; Petropoulos, Spyridon; Ferreira, Isabel C F R

2016-11-15

Garlic (Allium sativum L.) is considered one of the twenty most important vegetables, with various uses throughout the world, either as a raw vegetable for culinary purposes, or as an ingredient of traditional and modern medicine. Furthermore, it has also been proposed as one of the richest sources of total phenolic compounds, among the usually consumed vegetables, and has been highly ranked regarding its contribution of phenolic compounds to human diet. This review aims to examine all the aspects related with garlic chemical composition and quality, focusing on its bioactive properties. A particular emphasis is given on the organosulfur compounds content, since they highly contribute to the effective bioactive properties of garlic, including its derived products. The important effects of pre-harvest (genotype and various cultivation practices) and post-harvest conditions (storage conditions and processing treatments) on chemical composition and, consequently, bioactive potency of garlic are also discussed. Copyright © 2016 Elsevier Ltd. All rights reserved.

[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.

The addition of rosehip oil to Aloe gels improves their properties as postharvest coatings for maintaining quality in plum.

PubMed

Martínez-Romero, Domingo; Zapata, Pedro J; Guillén, Fabián; Paladines, Diego; Castillo, Salvador; Valero, Daniel; Serrano, María

2017-02-15

The effect of Aloe vera gel (AV) and Aloe arborescens gel (AA) alone or in combination with rosehip oil (RO) at 2% on ethylene production, respiration rate, quality parameters, bioactive compounds and antioxidant activity during plum postharvest storage was studied. Coated plums showed a delay in ethylene production and respiration rate at 20°C and during cold storage and subsequent shelf life, the main effect being observed for those fruits coated with AA+RO. Quality parameters such as softening, colour and maturity index was also delayed during storage by the use of the coatings, which led to a 2-fold increase in plum storability. Accumulation of bioactive compounds was also delayed although at the end of the experiment the content of bioactive compounds was higher than those found for control fruits at the estimated shelf life. The most effective coating for maintaining plum quality and bioactive compounds was AA+RO. Copyright © 2016 Elsevier Ltd. All rights reserved.

Identification of 3-hydroxy-3-methylglutaric acid (HMG) as a hypoglycemic principle of Spanish moss (Tillandsia usneoides).

PubMed

Witherup, K M; McLaughlin, J L; Judd, R L; Ziegler, M H; Medon, P J; Keller, W J

1995-08-01

Bioactivity-directed fractionation, using brine shrimp lethality and murine hypoglycemia, of an ethanol extract prepared from Tillandsia usneoides, led to the isolation of four apparently bioactive compounds from the water-soluble fraction. The compounds were identified as citric acid, succinic acid, 3-hydroxy-3-methylglutaric acid (HMG), and 3,6,3',5'-tetramethoxy-5,7,4'-trihydroxyflavone-7-O-beta-D-g lucoside. The brine shrimp lethality of the acids was simply due to acidity; however, HMG elicited significant hypoglycemic responses in fasting normal mice. Ethyl and methyl esters of citric acid were prepared and tested in the murine hypoglycemic assay. Five of the predominant sugars were identified by tlc. Free thymidine was also isolated. Further evaluation of HMG and other potential inhibitors of HMG CoA lyase, in the treatment of symptoms of diabetes mellitus, is suggested.

Bioactive compounds and antioxidant potential for polyphenol-rich cocoa extract obtained by agroindustrial residue.

PubMed

Gabbay Alves, Taís Vanessa; Silva da Costa, Russany; Aliakbarian, Bahar; Casazza, Alessandro Alberto; Perego, Patrizia; Pinheiro Arruda, Mara Silvia; Carréra Silva Júnior, José Otávio; Converti, Attilio; Ribeiro Costa, Roseane Maria

2017-11-10

Processing of cocoa (Theobroma cacao L.) beans responsible for agricultural exports leads to large amounts of solid waste that were discarded, however, this one presents high contents of metabolites with biological activities. The major objective of this study was to valorise cocoa agroindustrial residue obtained by hydraulic pressing for extract rich in antioxidants. For it, the centesimal composition of residue was investigated, the green extraction was carried out from the residue after, the bioactive compounds, sugar contents and screaming by HPTLC were quantified for extract. The extract has a total polyphenol content of 229.64 mg/g and high antioxidant activity according to ABTS 225.0 μM/g. HTPLC analysis confirmed the presence in the extract, residue of terpenes, sesquiterpenes, flavonoids and antioxidant activity. These results, as a whole, suggest that the extract from the cocoa residue has interesting characteristics to alternative crops with potential industrial uses.

Laucysteinamide A, a Hybrid PKS/NRPS Metabolite from a Saipan Cyanobacterium, cf. Caldora penicillata

PubMed Central

Zhang, Chen; Naman, C. Benjamin; Engene, Niclas; Gerwick, William H.

2017-01-01

A bioactivity guided study of a cf. Caldora penicillata species, collected during a 2013 expedition to the Pacific island of Saipan, Northern Mariana Islands (a commonwealth of the USA), led to the isolation of a new thiazoline-containing alkaloid, laucysteinamide A (1). Laucysteinamide A is a new monomeric analogue of the marine cyanobacterial metabolite, somocystinamide A (2), a disulfide-bonded dimeric compound that was isolated previously from a Fijian marine cyanobacterium. The structure and absolute configuration of laucysteinamide A (1) was determined by a detailed analysis of its NMR, MS, and CD spectra. In addition, the highly bioactive lipid, curacin D (3), was also found to be present in this cyanobacterial extract. The latter compound was responsible for the potent cytotoxicity of this extract to H-460 human non-small cell lung cancer cells in vitro. PMID:28420100

Anti-Cancer Phytometabolites Targeting Cancer Stem Cells

PubMed Central

Torquato, Heron F.V.; Goettert, Márcia I.; Justo, Giselle Z.; Paredes-Gamero, Edgar J.

2017-01-01

Medicinal plants are a plentiful source of bioactive molecules with much structural diversity. In cancer treatment, molecules obtained from plants represent an attractive alternative to other treatments because several plant-derived compounds have exhibited lower toxicity and higher selectivity against cancer cells. In this review, we focus on the possible application of bioactive molecules obtained from plants against more primitive cell populations in cancers, cancer stem cells. Cancer stem cells are present in several kinds of tumors and are responsible for recurrences and metastases. Common anti-cancer drugs exhibit lower effectiveness against cancer stem cells because of their biological features. However, recently discovered natural phytometabolites exert cytotoxic effects on this rare population of cells in cancers. Therefore, this review presents the latest research on promising compounds from plants that can act as antitumor drugs and that mainly affect stem cell populations in cancers. PMID:28367074

Bioactive compounds isolated from apple, tea, and ginger protect against dicarbonyl induced stress in cultured human retinal epithelial cells.

PubMed

Sampath, Chethan; Zhu, Yingdong; Sang, Shengmin; Ahmedna, Mohamed

2016-02-15

Methylglyoxal (MGO) is known to be a major precursor of advanced glycation end products (AGEs) which are linked to diabetes and its related complications. Naturally occurring bioactive compounds could play an important role in countering AGEs thereby minimizing the risk associated with their formation. In this study, eight specific bioactive compounds isolated from apple, tea and ginger were evaluated for their AGEs scavenging activity using Human Retinal Pigment Epithelial (H-RPE) cells treated with MGO. Among the eight specific compounds evaluated, (-)-epigallocatechin 3-gallate (EGCG) from tea, phloretin in apple, and [6]-shogaol and [6]-gingerol from ginger were found to be most effective in preventing MGO-induced cytotoxicity in the epithelial cells. Investigation of possible underlying mechanisms suggests that that these compounds could act by modulating key regulative detoxifying enzymes via modifying nuclear factor-erythroid 2-related factor 2 (Nrf2) function. MGO-induced cytotoxicity led to increased levels of AGEs causing increase in Nε-(Carboxymethyl) lysine (CML) and glutathione (GSH) levels and over expression of receptor for advanced glycation end products (RAGE). Data also showed that translocation of Nrf2 from cytosol to nucleus was inhibited, which decreased the expression of detoxifying enzyme like heme oxygenase-1 (HO-1). The most potent bioactive compounds scavenged dicarbonyl compounds, inhibited AGEs formation and significantly reduced carbonyl stress by Nrf2 related pathway and restoration of HO-1 expression. These findings demonstrated the protective effect of bioactive compounds derived from food sources against MGO-induced carbonyl stress through activation of the Nrf2 related defense pathway, which is of significant importance for therapeutic interventions in complementary treatment/management of diabetes-related complications. Copyright © 2016. Published by Elsevier GmbH.

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.

Improving the estimation of flavonoid intake for study of health outcomes

USDA-ARS?s Scientific Manuscript database

Imprecision in estimating intakes of non-nutrient bioactive compounds such as flavonoids is a challenge in epidemiologic studies of health outcomes. The sources of this imprecision, using flavonoids as an example, include the variability of bioactive compounds in foods due to differences in growing ...

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...

Microanalysis characterization of bioactive protein-bound polysaccharides produced by Amanita ponderosa cultures.

PubMed

Salvador, Cátia; Martins, M Rosário; Caldeira, A Teresa

2015-02-01

Different compounds of edible mushrooms are responsible for their bioactivity. The ability to synthesize polysaccharides, namely protein-polysaccharide (PPS) complexes, is related to the antioxidant capacity of these compounds and present great interest in preventing a number of diseases, including cancer, cardiovascular and auto-immune diseases, and accelerated aging. Amanita ponderosa are wild edible mushrooms that grow in Mediterranean "montado" areas [Portuguese name given to cork oak (Quercus suber) and holm oak (Quercus ilex) forests]. The aim of this study was to evaluate the production of PPS complexes obtained from A. ponderosa cultures using a new microanalytical approach to quickly and easily monitor the production process. Microanalysis using Fourier-transform infrared using attenuated total reflection and Raman spectroscopy of PPS samples showed spectra compatible with identification of this type of compound in culture extracts. PPS separated by size-exclusion chromatography showed seven main complexes. Molecular weights of the main PPS complexes isolated from cultures ranged between 1.5 and 20 kDa and did not present toxicity against Artemia salina, demonstrating the potential of A. ponderosa as a source of biologically active compounds with nutraceutical value. Application of this microanalytical approach to monitoring the production of PPS compounds can be successfully applied in biotechnological processes.

Mosquito adulticidal activity of the leaf extracts of Spondias mombin L. against Aedes aegypti L. and isolation of active principles.

PubMed

Ajaegbu, Elijah Eze; Danga, Simon Pierre Yinyang; Chijoke, Ikemefuna Uzochukwu; Okoye, Festus Basden Chiedu

2016-03-01

Aedes aegypti is a domestic mosquito and one of the primary vectors for dengue and yellow fever. Since, it is a vector of deadly diseases, its control becomes essential. Medicinal plants may be an alternative to adulticidal agents since they contain rich source of bioactive compounds. This study was designed to determine the adulticidal activity of Spondias mombin leaf methanol crude extract, n-hexane, dichloromethane and ethyl acetate fractions against female adults of Ae. aegypti mosquitoes and isolate active compound(s) responsible for the bioactivity. All leaf extract and fractions were evaluated for adulticidal activity against Ae. aegypti mosquitoes. Adult mortality was observed after 24 h of exposure. The dichloromethane fraction was further purified being the most active fraction using silica gel column chromatography and the active compounds were identified with the aid of HPLC and LC-ESI-MS/MS. The LC50 and LC90 were determined by Probit analysis. Dichloromethane fraction was the most effective fraction with LC50 value of 2172.815 μg/ml. Compounds identified were mainly ellagic acid and 1-O-Galloyl-6-O-luteoyl-α-D-glucose. The S. mombin leaf extracts and fractions proved to be a strong candidate for a natural, safe and stable adulticide, alternative to synthetic adulticide.

Bioturbo similarity searching: combining chemical and biological similarity to discover structurally diverse bioactive molecules.

PubMed

Wassermann, Anne Mai; Lounkine, Eugen; Glick, Meir

2013-03-25

Virtual screening using bioactivity profiles has become an integral part of currently applied hit finding methods in pharmaceutical industry. However, a significant drawback of this approach is that it is only applicable to compounds that have been biologically tested in the past and have sufficient activity annotations for meaningful profile comparisons. Although bioactivity data generated in pharmaceutical institutions are growing on an unprecedented scale, the number of biologically annotated compounds still covers only a minuscule fraction of chemical space. For a newly synthesized compound or an isolated natural product to be biologically characterized across multiple assays, it may take a considerable amount of time. Consequently, this chemical matter will not be included in virtual screening campaigns based on bioactivity profiles. To overcome this problem, we herein introduce bioturbo similarity searching that uses chemical similarity to map molecules without biological annotations into bioactivity space and then searches for biologically similar compounds in this reference system. In benchmark calculations on primary screening data, we demonstrate that our approach generally achieves higher hit rates and identifies structurally more diverse compounds than approaches using chemical information only. Furthermore, our method is able to discover hits with novel modes of inhibition that traditional 2D and 3D similarity approaches are unlikely to discover. Test calculations on a set of natural products reveal the practical utility of the approach for identifying novel and synthetically more accessible chemical matter.

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.

An Investigation into Spent Coffee Waste as a Renewable Source of Bioactive Compounds and Industrially Important Sugars

PubMed Central

Scully, Damhan S.; Jaiswal, Amit K.; Abu-Ghannam, Nissreen

2016-01-01

Conventional coffee brewing techniques generate vast quantities of spent espresso grounds (SEGs) rich in lignocellulose and valuable bioactives. These bioactive compounds can be exploited as a nutraceutical or used in a range of food products, while breakdown of lignocellulose generates metabolizable sugars that can be used for the production of various high-value products such as biofuels, amino acids and enzymes. Response surface methodology (RSM) was used to optimize the enzymatic saccharification of lignocellulose in SEGs following a hydrothermal pretreatment. A maximum reducing sugar yield was obtained at the following optimized hydrolysis conditions: 4.97 g of pretreated SEGs, 120 h reaction time, and 1246 and 250 µL of cellulase and hemicellulase, respectively. Industrially important sugars (glucose, galactose and mannose) were identified as the principal hydrolysis products under the studied conditions. Total flavonoids (p = 0.0002), total polyphenols (p = 0.03) and DPPH free-radical scavenging activity (p = 0.004) increased significantly after processing. A 14-fold increase in caffeine levels was also observed. This study provides insight into SEGs as a promising source of industrially important sugars and polyphenols. PMID:28952594

Anti-inflammatory activity of aqueous extract and bioactive compounds identified from the fruits of Hancornia speciosa Gomes (Apocynaceae).

PubMed

Torres-Rêgo, Manoela; Furtado, Allanny Alves; Bitencourt, Mariana Angélica Oliveira; Lima, Maira Conceição Jerônimo de Souza; Andrade, Rafael Caetano Lisbôa Castro de; Azevedo, Eduardo Pereira de; Soares, Thaciane da Cunha; Tomaz, José Carlos; Lopes, Norberto Peporine; da Silva-Júnior, Arnóbio Antônio; Zucolotto, Silvana Maria; Fernandes-Pedrosa, Matheus de Freitas

2016-08-05

Hancornia speciosa Gomes (Apocynaceae), popularly known as "mangabeira," has been used in folk medicine to treat inflammatory disorders, hypertension, dermatitis, diabetes, liver diseases and gastric disorders. Although the ethnobotany indicates that its fruits can be used for the treatment of ulcers and inflammatory disorders, only few studies have been conducted to prove such biological activities. This study investigated the anti-inflammatory properties of the aqueous extract of the fruits of H. speciosa Gomes as well as its bioactive compounds using in vivo experimental models. The bioactive compounds were identified by High Performance Liquid Chromatography coupled with diode array detector (HPLC-DAD) and Liquid Chromatography coupled with Mass Spectrometry (LC-MS). The anti-inflammatory properties were investigated through in vivo tests, which comprised xylene-induced ear edema, carrageenan-induced peritonitis and zymosan-induced air pouch. The levels of IL-1β, IL-6, IL-12 and TNF-α were determined using ELISA. Rutin and chlorogenic acid were identified in the extract as the main secondary metabolites. In addition, the extract as well as rutin and chlorogenic acid significantly inhibited the xilol-induced ear edema and also reduced the cell migration in both carrageenan-induced peritonitis and zymosan-induced air pouch models. Reduced levels of cytokines were also observed. This is the first study that demonstrated the anti-inflammatory activity of the extract of H. speciosa fruits against different inflammatory agents in animal models, suggesting that its bioactive molecules, especially rutin and chlorogenic acid are, at least in part, responsible for such activity. These findings support the widespread use of Hancornia speciosa in popular medicine and demonstrate that its aqueous extract has therapeutical potential for the development of herbal drugs with anti-inflammatory properties.

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

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.

Bioactive compounds from culinary herbs inhibit a molecular target for type 2 diabetes management, dipeptidyl peptidase IV

USDA-ARS?s Scientific Manuscript database

Greek oregano (Origanum vulgare), marjoram (Origanum majorana), rosemary (Rosmarinus officinalis) and Mexican oregano (Lippia graveolens) are concentrated sources of bioactive compounds. The aims of this study were to characterize extracts from greenhouse grown or commercially purchased herbs for th...

Enhancement of nutritional and bioactive compounds by in vitro culture of wild Fragaria vesca L. vegetative parts.

PubMed

Dias, Maria Inês; Barros, Lillian; Sousa, Maria João; Oliveira, M Beatriz P P; Santos-Buelga, Celestino; Ferreira, Isabel C F R

2017-11-15

In vitro culture emerges as a sustainable way to produce bioactives for further applicability in the food industry. Herein, vegetative parts of Fragaria vesca L. (wild strawberry) obtained by in vitro culture were analyzed regarding nutritional and phytochemical compounds, as well as antioxidant activity. These samples proved to have higher content of protein, polyunsaturated fatty acids, soluble sugars, organic acids (including ascorbic acid) and tocopherols (mainly α-tocopherol) than wild grown F. vesca, as well as containing additional phenolic compounds. The antioxidant activity of hydromethanolic extracts could be correlated with the content of different phenolic groups and other compounds (sugars and organic acids). It was demonstrated that in vitro culture could enhance nutritional and bioactive compounds of Fragaria vesca L. plants, providing a very interesting biotechnological tool for potential food applications. Copyright © 2017 Elsevier Ltd. All rights reserved.

Exploring sets of molecules from patents and relationships to other active compounds in chemical space networks

NASA Astrophysics Data System (ADS)

Kunimoto, Ryo; Bajorath, Jürgen

2017-09-01

Patents from medicinal chemistry represent a rich source of novel compounds and activity data that appear only infrequently in the scientific literature. Moreover, patent information provides a primary focal point for drug discovery. Accordingly, text mining and image extraction approaches have become hot topics in patent analysis and repositories of patent data are being established. In this work, we have generated network representations using alternative similarity measures to systematically compare molecules from patents with other bioactive compounds, visualize similarity relationships, explore the chemical neighbourhood of patent molecules, and identify closely related compounds with different activities. The design of network representations that combine patent molecules and other bioactive compounds and view patent information in the context of current bioactive chemical space aids in the analysis of patents and further extends the use of molecular networks to explore structure-activity relationships.

Large-Scale Metabolomics Reveals A Complex Response of Aspergillus nidulans to Epigenetic Perturbation

PubMed Central

Albright, Jessica C.; Henke, Matthew T.; Soukup, Alexandra A.; McClure, Ryan A.; Thomson, Regan J.; Keller, Nancy P.; Kelleher, Neil L.

2015-01-01

The microbial world offers a rich source of bioactive compounds for those able to sift through it. Technologies capable of quantitatively detecting natural products while simultaneously identifying known compounds would expedite the search for new pharmaceutical leads. Prior efforts have targeted histone deacetylases in fungi to globally activate the production of new secondary metabolites, yet no study has directly assessed its effects with minimal bias at the metabolomic level. Using untargeted metabolomics, we monitored changes in >1000 small molecules secreted from the model fungus, Aspergillus nidulans, following genetic or chemical reductions in histone deacetylase activity (HDACi). Through quantitative, differential analyses, we found nearly equal numbers of compounds were up- and down-regulated by >100 fold. We detected products from both known and unknown biosynthetic pathways and discovered that A. nidulans is capable of producing fellutamides, proteasome inhibitors whose expression was induced by ~100 fold or greater upon HDACi. This work adds momentum to an ‘omics’-driven resurgence in natural products research, where direct detection replaces bioactivity as the primary screen for new pharmacophores. PMID:25815712

Purification and identification of bioactive angucyclinones from Streptomyces matensis BG5, isolated from the rhizosphere of Rosa indica L.

PubMed

Sajid, Imran; Shaaban, Khaled A; Hasnain, Shahida

2013-01-01

A newly isolated strain Streptomyces sp. BG5 was investigated for the production of bioactive compounds. The strain exhibited broad-spectrum activity against an array of nine test organisms including gram-positive bacteria, gram-negative bacteria, and fungal and microalgal pathogens, along with a moderate cytotoxic response (28.9% mortality) in a microwell cytotoxicity assay against the brine shrimp Artimia salina. The morphological, physiological, and biochemical characterization of the Streptomyces sp. BG5 strongly suggested it to be a member of the genus Streptomyces. The nucleotide sequence of 16S rRNA gene (1433 pb) of the Streptomyces sp. BG5 (Gene bank accession number EU301836) exhibited high similarity (98%) with Streptomyces matensis. The large-scale fermentation of Streptomyces sp. BG5 and subsequent extraction, isolation, and purification of the crude extract afforded three pure compounds. The structures of these compounds were identified as ochromycinone (1a), emycin D (2), and 1-acetyl-β-carbolin (3), based on nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry, and by comparison with reference data from the literature.

Molecular Dynamics Simulation of Mahkota Dewa (Phaleria Macrocarpa) Extract in Subcritical Water Extraction Process

NASA Astrophysics Data System (ADS)

Hashim, N. A.; Mudalip, S. K. Abdul; Harun, N.; Che Man, R.; Sulaiman, S. Z.; Arshad, Z. I. M.; Shaarani, S. M.

2018-05-01

Mahkota Dewa (Phaleria Macrocarpa), a good source of saponin, flavanoid, polyphenol, alkaloid, and mangiferin has an extensive range of medicinal effects. The intermolecular interactions between solute and solvents such as hydrogen bonding considered as an important factor that affect the extraction of bioactive compounds. In this work, molecular dynamics simulation was performed to elucidate the hydrogen bonding exists between Mahkota Dewa extracts and water during subcritical extraction process. A bioactive compound in the Mahkota Dewa extract, namely mangiferin was selected as a model compound. The simulation was performed at 373 K and 4.0 MPa using COMPASS force field and Ewald summation method available in Material Studio 7.0 simulation package. The radial distribution functions (RDF) between mangiferin and water signify the presence of hydrogen bonding in the extraction process. The simulation of the binary mixture of mangiferin:water shows that strong hydrogen bonding was formed. It is suggested that, the intermolecular interaction between OH2O••HMR4(OH1) has been identified to be responsible for the mangiferin extraction process.

Tapping the Bioactivity Potential of Residual Stream from Its Pretreatments May Be a Green Strategy for Low-Cost Bioconversion of Rice Straw.

PubMed

Chen, Xingxuan; Wang, Xiahui; Xue, Yiyun; Zhang, Tian-Ao; Hu, Jiajun; Tsang, Yiu Fai; Gao, Min-Tian

2018-04-16

In this study, it was found that the residual stream from pretreatments of rice straw exhibited high antioxidant activity. Assays based on the Folin-Ciocalteu colorimetric method confirmed that the residual stream contained large amounts of phenolic compounds. Three antioxidant assays were employed to evaluate the bioactivity of the residual stream. Strong linear correlations existed among the release of phenolic compounds, saccharification efficiency, and antioxidant activity. The alkaline pretreatment provided a much greater release of phenolic compounds, especially phenolic acids, compared to the acid pretreatment, and consequently, it had stronger linear correlations than the acid pretreatment. Antibacterial experiments demonstrated the ability of the phenolic compounds in the residual stream to inhibit the growth of microorganisms, indicating the potential of these compounds as antimicrobial agents. To discuss the possibility of the co-production of antimicrobial agents and biofuels/biochemicals, both acid and alkaline pretreatments were optimized using response surface methodology. Under the optimal conditions, 285.7 g glucose could be produced from 1 kg rice straw with the co-production of 3.84 g FA and 6.98 g p-CA after alkaline pretreatment. These results show that the recovery of phenolic compounds from the residual stream could be a green strategy for the low-cost bioconversion of rice straw.

DNA-encoded libraries - an efficient small molecule discovery technology for the biomedical sciences.

PubMed

Kunig, Verena; Potowski, Marco; Gohla, Anne; Brunschweiger, Andreas

2018-06-27

DNA-encoded compound libraries are a highly attractive technology for the discovery of small molecule protein ligands. These compound collections consist of small molecules covalently connected to individual DNA sequences carrying readable information about the compound structure. DNA-tagging allows for efficient synthesis, handling and interrogation of vast numbers of chemically synthesized, drug-like compounds. They are screened on proteins by an efficient, generic assay based on Darwinian principles of selection. To date, selection of DNA-encoded libraries allowed for the identification of numerous bioactive compounds. Some of these compounds uncovered hitherto unknown allosteric binding sites on target proteins; several compounds proved their value as chemical biology probes unraveling complex biology; and the first examples of clinical candidates that trace their ancestry to a DNA-encoded library were reported. Thus, DNA-encoded libraries proved their value for the biomedical sciences as a generic technology for the identification of bioactive drug-like molecules numerous times. However, large scale experiments showed that even the selection of billions of compounds failed to deliver bioactive compounds for the majority of proteins in an unbiased panel of target proteins. This raises the question of compound library design.

Optimisation of Germination Time and Temperature on the Concentration of Bioactive Compounds in Brazilian Soybean Cultivar BRS 133 using Response Surface Methodology

USDA-ARS?s Scientific Manuscript database

The objective was to optimize the effect of germination time and temperature on the concentration of soluble protein, lunasin, BBI, lectin, saponins and isoflavones in soybean seeds from cultivar BRS 133. Isoflavone and saponin concentrations were analysed by HPLC. Lunasin, Bowman-Birk inhibitor a...

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.

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.

Controlled release properties of zein-fatty acid blend films for multiple bioactive compounds.

PubMed

Arcan, Iskender; Yemenicioğlu, Ahmet

2014-08-13

To develop edible films having controlled release properties for multiple bioactive compounds, hydrophobicity and morphology of zein films were modified by blending zein with oleic (C18:1)Δ⁹, linoleic (C18:2)Δ(9,12), or lauric (C₁₂) acids in the presence of lecithin. The blend zein films showed 2-8.5- and 1.6-2.9-fold lower initial release rates for the model active compounds, lysozyme (LYS) and (+)-catechin (CAT), than the zein control films, respectively. The change of fatty acid chain length affected both CAT and LYS release rates while the change of fatty acid double bond number affected only the CAT release rate. The film morphologies suggested that the blend films owe their controlled release properties mainly to the microspheres formed within their matrix and encapsulation of active compounds. The blend films showed antilisterial activity and antioxidant activity up to 81 μmol Trolox/cm². The controlled release of multiple bioactive compounds from a single film showed the possibility of combining application of active and bioactive packaging technologies and improving not only safety and quality but also health benefits of packed food.

Nocardiopsis species: a potential source of bioactive compounds.

PubMed

Bennur, T; Ravi Kumar, A; Zinjarde, S S; Javdekar, V

2016-01-01

Members of the genus Nocardiopsis are an ecologically versatile and biotechnologically important group of Actinomycetes. Most of the isolates are halotolerant or halophilic and they prevail in soils, marine environments or hypersaline locations. To aid their survival under these conditions, they mainly produce extremozymes, compatible solutes, surfactants and bioactive compounds. The current review details the bioactive compounds obtained for this genus. Important antimicrobial agents obtained from this genus include polyketides, phenzines, quinoline alkaloids, terphenyls, proteins, thiopeptides and amines. Polyketides and peptides displaying potent anticancer activities are also significant. Tumour promoting agents, P-glycoprotein (P-gp) inhibitors, immunomodulators and protein kinase inhibitors are other relevant products obtained from Nocardiopsis species. Structurally, polyketides (synthesized by polyketide synthases) and peptides (made by nonribosomal peptide synthetases or cyclodipeptide synthases) are important compounds. Considered here are also toxins, anti photoaging and adipogenic agents produced by this genus. The gene clusters mediating the synthesis of bioactive compounds have been described. Commercially available products (Apoptolidins and K-252a) derived from this genus have also been described. This review highlights the significance of a single genus in producing an assortment of compounds with varied biological activities. On account of these features, the members of this genus have established a place for themselves and are of considerable value in producing compounds with profound bio-medical applications. © 2015 The Society for Applied Microbiology.

Challenges in Analyzing the Biological Effects of Resveratrol

PubMed Central

Erdogan, Cihan Suleyman; Vang, Ole

2016-01-01

The suggested health effects (e.g., disease prevention) of dietary bioactive compounds such as resveratrol are challenging to prove in comparison to man-made drugs developed for therapeutic purposes. Dietary bioactive compounds have multiple cellular targets and therefore have a variety of biological effects. Extrapolating the biological effects of dietary compounds from in vitro and in vivo animal experiments to humans may lead to over- or under-estimation of the effect and role of these compounds. The present paper will discuss a few of these challenges and suggest directions for future research. Questions we address include: (1) Is the combinatorial effect of resveratrol and other compounds real? (2) What are the real and relevant doses of resveratrol after administration? and (3) Is it possible to estimate the preventive effect of resveratrol by clinical trials using standard experimental designs? The examples concerning resveratrol taken from the scientific literature are mainly from 2010 and later. The challenges pointed out in this review are similar to most naturally occurring bioactive compounds. PMID:27294953

Feasibility in multispectral imaging for predicting the content of bioactive compounds in intact tomato fruit.

PubMed

Liu, Changhong; Liu, Wei; Chen, Wei; Yang, Jianbo; Zheng, Lei

2015-04-15

Tomato is an important health-stimulating fruit because of the antioxidant properties of its main bioactive compounds, dominantly lycopene and phenolic compounds. Nowadays, product differentiation in the fruit market requires an accurate evaluation of these value-added compounds. An experiment was conducted to simultaneously and non-destructively measure lycopene and phenolic compounds content in intact tomatoes using multispectral imaging combined with chemometric methods. Partial least squares (PLS), least squares-support vector machines (LS-SVM) and back propagation neural network (BPNN) were applied to develop quantitative models. Compared with PLS and LS-SVM, BPNN model considerably improved the performance with coefficient of determination in prediction (RP(2))=0.938 and 0.965, residual predictive deviation (RPD)=4.590 and 9.335 for lycopene and total phenolics content prediction, respectively. It is concluded that multispectral imaging is an attractive alternative to the standard methods for determination of bioactive compounds content in intact tomatoes, providing a useful platform for infield fruit sorting/grading. Copyright © 2014 Elsevier Ltd. All rights reserved.

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

Bioactive capacity of some Romanian wild edible mushrooms consumed mainly by local communities.

PubMed

Vamanu, Emanuel

2018-02-01

Wild edible mushrooms are considered as a cheap food source, but rich in bioactive compounds, especially in phenolic compounds. The purpose of the study was to determine the antioxidant and antimicrobial activity and the content of polyphenolcarboxylic acids in 10 species of mushrooms commonly used (consumed) in Romania and two controls. The effect against free radicals, lipid peroxidation and reducing power were determined. The antimicrobial effect was revealed on some strains with pathogenic effect by disk diffusion assay. The antioxidant capacity expressed in vitro was correlated both with the presence of the main polyphenolcarboxylic acids, and also with the presence of other bioactive molecules (flavonoids, carotenoid compounds, etc.).

Bioactive annonaceous acetogenins from the bark of Xylopia aromatica.

PubMed

Colman-Saizarbitoria, T; Zambrano, J; Ferrigni, N R; Gu, Z M; Ng, J H; Smith, D L; McLaughlin, J L

1994-04-01

Bioactive Annonaceous acetogenins have been isolated from the EtOH extract of the bark of Xylopia aromatica by bioactivity-directed fractionation using lethality to brine shrimp. These acetogenins include xylopianin [1 , xylopiacin [2], and xylomaticin [3], which are three new mono-tetrahydrofuran ring type acetogenins, in addition to the known compounds, annomontacin, gigantetronenin, gigantetrocin A, and annonacin. Compounds 1 and 2 are unusual in having hydroxylation at C-8; 3 has the same functionalities as annonacin but with 37 carbons instead of 35 carbons. The structures were elucidated by spectral analysis of the parent compounds and/or simple chemical derivatives. These acetogenins showed cytotoxicities, comparable to adriamycin, against three human solid tumor cell lines.

The Evaluation and Utilization of Marine-derived Bioactive Compounds with Anti-obesity Effect.

PubMed

Jin, Qiu; Yu, Huahua; Li, Pengcheng

2018-01-01

Obesity is a global epidemic throughout the world. There is thus increasing interest in searching for natural bioactive compounds with anti-obesity effect. A number of marine compounds have been regarded as potential sources of bioactive compounds and are associated with an anti-obesity effect. Marine-derived compounds with anti-obesity effect and their current applications, methods and indicators for the evaluation of anti-obesity activity are summarized in this review. in order to make contributions to the development of marine-derived functional food against obesity. In this review, an overview of marine-derived compounds with anti-obesity effect, including marine polysaccharides, marine lipid, marine peptides, marine carotenoids is intensively made with an emphasis on their efficacy and mechanism of action. Meanwhile, methods and indicators for the evaluation of anti-obesity activity are discussed. We summarize these methods into three categories: in vitro assay (including adsorption experiments and enzyme inhibitory assay), cell line study, animal experiments and clinical experiments. In addition, a brief introduction of the current applications of marine bioactive compounds with anti-obesity activity is discussed. Marine environment is a rich source of both biological and chemical diversity. In the past decades, numerous novel compounds with anti-obesity activity have been obtained from marine organisms, and many of them have been applied to industrial production such as functional foods and pharmaceuticals. Further studies are needed to explore the above-mentioned facts. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Effect of light exposure on sensorial quality, concentrations of bioactive compounds and antioxidant capacity of radish microgreens during low temperature storage

USDA-ARS?s Scientific Manuscript database

Daikon radish microgreens constitute a good source of bioactive compounds. However, the quality deteriorates rapidly during postharvest storage. In this study, we investigated the effects of light exposure and modified atmosphere packaging conditions on changes in sensorial quality and retention of ...

Effect of time and temperature on bioactive compounds in germinated Brazilian soybean cultivar BRS 258

USDA-ARS?s Scientific Manuscript database

The consumption of soybeans and soybean products has increased in the last few years due to the functional properties of bioactive compounds such as lunasin, Bowman Birk Inhibitor (BBI), lectin, saponins, and isoflavones. The objective of this study was to determine the effect of germination of soy...

Distribution, diversity and bioprospecting of bioactive compounds from cryptic fungal communities associated with endemic and cold-adapted macroalgae in Antarctica

USDA-ARS?s Scientific Manuscript database

We surveyed the distribution and diversity of fungi associated with eight macroalgae from Antarctica and their capability to produce bioactive compounds. The collections yielded 148 fungal isolates identified using molecular methods into 21 genera and 43 species. The most frequent taxa were Geomyces...

Chondriotin sulfate disaccharides as a bioactive compound modified the murine gut microbiome under healthy and stressed conditions

USDA-ARS?s Scientific Manuscript database

Chondriotin sulfate (CS) has been widely used for medical and nutraceutical purposes due to its roles in maintaining tissue structural integrity. We investigated if CS disaccharides may act as a bioactive compound and modulate gut microbial composition in mice. Our data show that CS disaccharides su...

Nutritional value, bioactive compounds, and health benefits of lettuce (Lactuca sativa L.)

USDA-ARS?s Scientific Manuscript database

Lettuce is one of the most popularly consumed vegetables worldwide but its nutritional value has been underestimated. Lettuce is low in calories and fat but high in fiber. Moreover, lettuce is high in potassium but low in sodium. Lettuce is also a good source of health-beneficial bioactive compounds...

Preparation of a thermoresponsive polymer grafted polystyrene monolithic capillary for the separation of bioactive compounds.

PubMed

Koriyama, Takuya; Asoh, Taka-Aki; Kikuchi, Akihiko

2016-11-01

To develop aqueous microseparation columns for bioactive compounds, a thermoresponsive polymer grafted polymer monolith was prepared inside silica capillaries having an I.D. of 100μm by polymerization of styrene (St) with m/p-divinylbenzene (DVB) in the presence of polydimethylsiloxane as porogen, followed by surface-initiated atom transfer radical polymerization (SI-ATRP) of N-isopropylacrylamide (NIPAAm). SEM analysis indicated that the resulting poly(N-isopropylacrylamide) (PNIPAAm) grafted polystyrene monolith had a consecutive three-dimensionally interconnected structure and through-pores, similar to the base polystyrene (PSt) monolith. The elution behavior of steroids with different hydrophobicity was evaluated using micro-high-performance liquid chromatography in sole aqueous mobile phase. Temperature dependent interaction changes were observed between steroids and the PNIPAAm modified surfaces. Furthermore, the interaction between bioactive compounds and the PNIPAAm grafted PSt surfaces was controlled and eventually separate these molecules with different hydrophobicities by simple temperature modulation in aqueous environment. The PNIPAAm grafted PSt monolithic capillary showed improved separation properties of bioactive compounds, compared with a PNIPAAm grafted hollow capillary in aqueous environment. Copyright © 2016 Elsevier B.V. All rights reserved.

Comparison of Bioactive Compounds and Quality Traits of Breast Meat from Korean Native Ducks and Commercial Ducks.

PubMed

Lee, Hyun Jung; Jayasena, Dinesh D; Kim, Sun Hyo; Kim, Hyun Joo; Heo, Kang Nyung; Song, Ji Eun; Jo, Cheorun

2015-01-01

The aim of this research was to compare the bioactive compound content and quality traits of breast meat from male and female Korean native ducks (KND) and commercial ducks (CD, Cherry Valley). Meat from three 6-wk old birds of each sex from KND and CD were evaluated for carcass and breast weights, pH, color, cooking loss, shear force, and bioactive compound (creatine, carnosine, anserine, betaine, and L-carnitine) content. KND showed significantly higher carcass weights than CD whereas no such difference (p>0.05) was found between male and female ducks. The breed and sex had no significant effects on the breast weight, pH value, and shear force. However, KND had significantly lower cooking loss values than did CD. Creatine, anserine, and L-carnitine contents were significantly higher in KND than in CD and were predominant in female ducks compared to males. The results of this study provide rare information regarding the amounts and the determinants of several bioactive compounds in duck meat, which can be useful for selection and breeding programs, and for popularizing indigenous duck meat.

[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.

Bioactive compounds and antioxidant activity analysis of Malaysian pineapple cultivars

NASA Astrophysics Data System (ADS)

Chiet, Chong Hang; Zulkifli, Razauden Mohamed; Hidayat, Topik; Yaakob, Harisun

2014-03-01

Pineapple industry is one of the important agricultural sectors in Malaysia with 76 cultivars planted throughout the country. This study aims to generate useful nutritional information as well as evaluating antioxidant properties of different pineapple commercial cultivars in Malaysia. The bioactive compound content and antioxidant capacity of `Josapine', `Morris' and `Sarawak' pineapple (Ananas comosus) were studied. The pineapple varieties were collected at commercial maturity stage (20-40% yellowish of fruit peel) and the edible portion of the fruit was used as sample for evaluation. The bioactive compound of the fruit extracts were evaluated by total phenolic and tannin content assay while the antioxidant capacity was determined by ferric reducing antioxidant power (FRAP). From the results obtained, total phenolic and tannin content was highest for `Josapine' followed by `Morris' and `Sarawak'. With respect to FRAP, `Josapine' showed highest reducing capacity, followed by `Morris' and then `Sarawak' having the least value. The bioactive compounds content are positively correlated with the antioxidant capacities of the pineapple extracts. This result indicates that the total phenolics and tannin content present in the pineapples may contribute to the antioxidant capacity of the pineapples.

Non-targeted workflow for identification of antimicrobial compounds in animal feed using bioassay-directed screening in combination with liquid chromatography-high resolution mass spectrometry.

PubMed

Wegh, Robin S; Berendsen, Bjorn J A; Driessen-Van Lankveld, Wilma D M; Pikkemaat, Mariël G; Zuidema, Tina; Van Ginkel, Leen A

2017-11-01

A non-targeted workflow is reported for the isolation and identification of antimicrobial active compounds using bioassay-directed screening and LC coupled to high-resolution MS. Suspect samples are extracted using a generic protocol and fractionated using two different LC conditions (A and B). The behaviour of the bioactive compound under these different conditions yields information about the physicochemical properties of the compound and introduces variations in co-eluting compounds in the fractions, which is essential for peak picking and identification. The fractions containing the active compound(s) obtained with conditions A and B are selected using a microbiological effect-based bioassay. The selected bioactive fractions from A and B are analysed using LC combined with high-resolution MS. Selection of relevant signals is automatically carried out by selecting all signals present in both bioactive fractions A and B, yielding tremendous data reduction. The method was assessed using two spiked feed samples and subsequently applied to two feed samples containing an unidentified compound showing microbial growth inhibition. In all cases, the identity of the compound causing microbiological inhibition was successfully confirmed.

Effect of physiological harvest stages on the composition of bioactive compounds in Cavendish bananas.

PubMed

Bruno Bonnet, Christelle; Hubert, Olivier; Mbeguie-A-Mbeguie, Didier; Pallet, Dominique; Hiol, Abel; Reynes, Max; Poucheret, Patrick

2013-04-01

The combined influence of maturation, ripening, and climate on the profile of bioactive compounds was studied in banana (Musa acuminata, AAA, Cavendish, cv. Grande Naine). Their bioactive compounds were determined by the Folin-Ciocalteu assay and high-performance thin layer chromatographic (HPTLC) method. The polyphenol content of bananas harvested after 400 degree days remained unchanged during ripening, while bananas harvested after 600 and 900 degree days exhibited a significant polyphenol increase. Although dopamine was the polyphenol with the highest concentration in banana peels during the green developmental stage and ripening, its kinetics differed from the total polyphenol profile. Our results showed that this matrix of choice (maturation, ripening, and climate) may allow selection of the banana (M. acuminata, AAA, Cavendish, cv. Grande Naine) status that will produce optimal concentrations of identified compounds with human health relevance.

Impact of high-intensity pulsed electric fields on bioactive compounds in Mediterranean plant-based foods.

PubMed

Elez-Martínez, Pedro; Soliva-Fortuny, Robert; Martín-Belloso, Olga

2009-05-01

Novel non-thermal processing technologies such as high-intensity pulsed electric field (HIPEF) treatments may be applied to pasteurize plant-based liquid foods as an alternative to conventional heat treatments. In recent years, there has been an increasing interest in HIPEF as a way of preserving and extending the shelf-life of liquid products without the quality damage caused by heat treatments. However, less attention has been paid to the effects of HIPEF on minor constituents of these products, namely bioactive compounds. This review is a state-of-the-art update on the effects of HIPEF treatments on health-related compounds in plants of the Mediterranean diet such as fruit juices, and Spanish gazpacho. The relevance of HIPEF-processing parameters on retaining plant-based bioactive compounds will be discussed.

Mangrove rare actinobacteria: taxonomy, natural compound, and discovery of bioactivity

PubMed Central

Azman, Adzzie-Shazleen; Othman, Iekhsan; Velu, Saraswati S.; Chan, Kok-Gan; Lee, Learn-Han

2015-01-01

Actinobacteria are one of the most important and efficient groups of natural metabolite producers. The genus Streptomyces have been recognized as prolific producers of useful natural compounds as they produced more than half of the naturally-occurring antibiotics isolated to-date and continue as the primary source of new bioactive compounds. Lately, Streptomyces groups isolated from different environments produced the same types of compound, possibly due to frequent genetic exchanges between species. As a result, there is a dramatic increase in demand to look for new compounds which have pharmacological properties from another group of Actinobacteria, known as rare actinobacteria; which is isolated from special environments such as mangrove. Recently, mangrove ecosystem is becoming a hot spot for studies of bioactivities and the discovery of natural products. Many novel compounds discovered from the novel rare actinobacteria have been proven as potential new drugs in medical and pharmaceutical industries such as antibiotics, antimicrobials, antibacterials, anticancer, and antifungals. This review article highlights the latest studies on the discovery of natural compounds from the novel mangrove rare actinobacteria and provides insight on the impact of these findings. PMID:26347734

Mangrove rare actinobacteria: taxonomy, natural compound, and discovery of bioactivity.

PubMed

Azman, Adzzie-Shazleen; Othman, Iekhsan; Velu, Saraswati S; Chan, Kok-Gan; Lee, Learn-Han

2015-01-01

Actinobacteria are one of the most important and efficient groups of natural metabolite producers. The genus Streptomyces have been recognized as prolific producers of useful natural compounds as they produced more than half of the naturally-occurring antibiotics isolated to-date and continue as the primary source of new bioactive compounds. Lately, Streptomyces groups isolated from different environments produced the same types of compound, possibly due to frequent genetic exchanges between species. As a result, there is a dramatic increase in demand to look for new compounds which have pharmacological properties from another group of Actinobacteria, known as rare actinobacteria; which is isolated from special environments such as mangrove. Recently, mangrove ecosystem is becoming a hot spot for studies of bioactivities and the discovery of natural products. Many novel compounds discovered from the novel rare actinobacteria have been proven as potential new drugs in medical and pharmaceutical industries such as antibiotics, antimicrobials, antibacterials, anticancer, and antifungals. This review article highlights the latest studies on the discovery of natural compounds from the novel mangrove rare actinobacteria and provides insight on the impact of these findings.

Changes in endogenous bioactive compounds of Korean native chicken meat at different ages and during cooking.

PubMed

Jayasena, Dinesh D; Jung, Samooel; Bae, Young Sik; Kim, Sun Hyo; Lee, Soo Kee; Lee, Jun Heon; Jo, Cheorun

2014-07-01

This study aimed to examine the effect of bird age on the contents of endogenous bioactive compounds, including carnosine, anserine, creatine, betaine, and carnitine, in meat from a certified meat-type commercial Korean native chicken strain (KNC; Woorimatdag). Additionally, the effects of the meat type (breast or leg meat) and the state of the meat (raw or cooked) were examined. Cocks of KNC were raised under similar standard commercial conditions at a commercial chicken farm. At various ages (10, 11, 12, 13, and 14 wk), breast and leg meats from a total of 10 birds from each age group were obtained. Raw and cooked meat samples were then prepared separately and analyzed for bioactive compounds. The age of the KNC had a significant effect only on the betaine content. The breast meat of KNC had higher amounts of carnosine and anserine but had lower amounts of betaine and carnitine than the leg meat (P < 0.05). The KNC meat lost significant amounts of all bioactive compounds during cooking (P < 0.05). Leg meat had high retention percentages of carnosine and anserine after cooking, whereas breast meat showed almost complete retention of betaine and carnitine. The results of this study provide useful and rare information regarding the presence, amounts, and determinants of endogenous bioactive compounds in KNC meat, which can be useful for selection and breeding programs, and also for popularizing indigenous chicken meat. © 2014 Poultry Science Association Inc.

Anaerobes as Sources of Bioactive Compounds and Health Promoting Tools.

PubMed

Mamo, Gashaw

Aerobic microorganisms have been sources of medicinal agents for several decades and an impressive variety of drugs have been isolated from their cultures, studied and formulated to treat or prevent diseases. On the other hand, anaerobes, which are believed to be the oldest life forms on earth and evolved remarkably diverse physiological functions, have largely been neglected as sources of bioactive compounds. However, results obtained from the limited research done so far show that anaerobes are capable of producing a range of interesting bioactive compounds that can promote human health. In fact, some of these bioactive compounds are found to be novel in their structure and/or mode of action.Anaerobes play health-promoting roles through their bioactive products as well as application of whole cells. The bioactive compounds produced by these microorganisms include antimicrobial agents and substances such as immunomodulators and vitamins. Bacteriocins produced by anaerobes have been in use as preservatives for about 40 years. Because these substances are effective at low concentrations, encounter relatively less resistance from bacteria and are safe to use, there is a growing interest in these antimicrobial agents. Moreover, several antibiotics have been reported from the cultures of anaerobes. Closthioamide and andrimid produced by Clostridium cellulolyticum and Pantoea agglomerans, respectively, are examples of novel antibiotics of anaerobe origin. The discovery of such novel bioactive compounds is expected to encourage further studies which can potentially lead to tapping of the antibiotic production potential of this fascinating group of microorganisms.Anaerobes are widely used in preparation of fermented foods and beverages. During the fermentation processes, these organisms produce a number of bioactive compounds including anticancer, antihypertensive and antioxidant substances. The well-known health promoting effect of fermented food is mostly due to these bioactive compounds. In addition to their products, whole cell anaerobes have very interesting applications for enhancing the quality of life. Probiotic anaerobes have been on the market for many years and are receiving growing acceptance as health promoters. Gut anaerobes have been used to treat patients suffering from severe Clostridium difficile infection syndromes including diarrhoea and colitis which cannot be treated by other means. Whole cell anaerobes are also studied to detect and cure cancer. In recent years, evidence is emerging that anaerobes constituting the microbiome are linked to our overall health. A dysfunctional microbiome is believed to be the cause of many diseases including cancer, allergy, infection, obesity, diabetes and several other disorders. Maintaining normal microflora is believed to alleviate some of these serious health problems. Indeed, the use of probiotics and prebiotics which favourably change the number and composition of the gut microflora is known to render a health promoting effect. Our interaction with the microbiome anaerobes is complex. In fact, not only our lives but also our identities are more closely linked to the anaerobic microbial world than we may possibly imagine. We are just at the beginning of unravelling the secret of association between the microbiome and human body, and a clear understanding of the association may bring a paradigm shift in the way we diagnose and treat diseases and disorders. This chapter highlights some of the work done on bioactive compounds and whole cell applications of the anaerobes that foster human health and improve the quality of life.

[Chemical constituents of Carya cathayensis and their antitumor bioactivity].

PubMed

Wu, De-lin; Chen, Shi-yun; Liu, Jing-song; Jin, Chuan-shan; Xu, Feng-qing

2011-07-01

To investigate the chemical constituents of Carya cathayensis and their antitumor bioactivity. The compounds were isolated by Sephadex LH-20 and silica gel column chromatography. Their structures were identified by physicochemical properties and spectroscopic analysis. Then their cytotoxic activity was studied. Five compounds were elucidated as chrysophanol (1), physcion (2), beta-sitosterol (3), pinostrobin(4), 4,8-dihydroxy-1-tetralone (5). Compounds 2 and 5 are isolated from Carya cathayensis for the first time. In the MTT antitumor experiments, the compounds 1,4 and 5 have the cytotoxic activity to KB cell.

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.

Metabolomic and Functional Genomic Analyses Reveal Varietal Differences in Bioactive Compounds of Cooked Rice

PubMed Central

Heuberger, Adam L.; Lewis, Matthew R.; Chen, Ming-Hsuan; Brick, Mark A.; Leach, Jan E.; Ryan, Elizabeth P.

2010-01-01

Emerging evidence supports that cooked rice (Oryza sativa L.) contains metabolites with biomedical activities, yet little is known about the genetic diversity that is responsible for metabolite variation and differences in health traits. Metabolites from ten diverse varieties of cooked rice were detected using ultra performance liquid chromatography coupled to mass spectrometry. A total of 3,097 compounds were detected, of which 25% differed among the ten varieties. Multivariate analyses of the metabolite profiles showed that the chemical diversity among the varieties cluster according to their defined subspecies classifications: indica, japonica, and aus. Metabolite-specific genetic diversity in rice was investigated by analyzing a collection of single nucleotide polymorphisms (SNPs) in genes from biochemical pathways of nutritional importance. Two classes of bioactive compounds, phenolics and vitamin E, contained nonsynonymous SNPs and SNPs in the 5′ and 3′ untranslated regions for genes in their biosynthesis pathways. Total phenolics and tocopherol concentrations were determined to examine the effect of the genetic diversity among the ten varieties. Per gram of cooked rice, total phenolics ranged from 113.7 to 392.6 µg (gallic acid equivalents), and total tocopherols ranged between 7.2 and 20.9 µg. The variation in the cooked rice metabolome and quantities of bioactive components supports that the SNP-based genetic diversity influenced nutritional components in rice, and that this approach may guide rice improvement strategies for plant and human health. PMID:20886119

In vitro screening techniques for reactive metabolites for minimizing bioactivation potential in drug discovery.

PubMed

Prakash, Chandra; Sharma, Raman; Gleave, Michelle; Nedderman, Angus

2008-11-01

Drug induced toxicity remains one of the major reasons for failures of new pharmaceuticals, and for the withdrawal of approved drugs from the market. Efforts are being made to reduce attrition of drug candidates, and to minimize their bioactivation potential in the early stages of drug discovery in order to bring safer compounds to the market. Therefore, in addition to potency and selectivity; drug candidates are now selected on the basis of acceptable metabolism/toxicology profiles in preclinical species. To support this, new approaches have been developed, which include extensive in vitro methods using human and animal hepatic cellular and subcellular systems, recombinant human drug metabolizing enzymes, increased automation for higher-throughput screens, sensitive analytical technologies and in silico computational models to assess the metabolism aspects of the new chemical entities. By using these approaches many compounds that might have serious adverse reactions associated with them are effectively eliminated before reaching clinical trials, however some toxicities such as those caused by idiosyncratic responses, are not detected until a drug is in late stages of clinical trials or has become available to the market. One of the proposed mechanisms for the development of idiosyncratic drug toxicity is the bioactivation of drugs to form reactive metabolites by drug metabolizing enzymes. This review discusses the different approaches to, and benefits of using existing in vitro techniques, for the detection of reactive intermediates in order to minimize bioactivation potential in drug discovery.

A database of natural products and chemical entities from marine habitat

PubMed Central

Babu, Padavala Ajay; Puppala, Suma Sree; Aswini, Satyavarapu Lakshmi; Vani, Metta Ramya; Kumar, Chinta Narasimha; Prasanna, Tallapragada

2008-01-01

Marine compound database consists of marine natural products and chemical entities, collected from various literature sources, which are known to possess bioactivity against human diseases. The database is constructed using html code. The 12 categories of 182 compounds are provided with the source, compound name, 2-dimensional structure, bioactivity and clinical trial information. The database is freely available online and can be accessed at http://www.progenebio.in/mcdb/index.htm PMID:19238254

Unique antimicrobial spectrum of ophiobolin K produced by Aspergillus ustus.

PubMed

Sohsomboon, Natthapat; Kanzaki, Hiroshi; Nitoda, Teruhiko

2018-03-01

A co-cultivation study of two fungal strains showed that Aspergillus ustus could inhibit Aspergillus repens growth. The bioactive compound responsible for the observed activity was purified and identified as a sesterterpene, ophiobolin K. Ophiobolin K exhibited marked inhibition against both fungi and bacteria, especially A. repens, A. glaucus and gram-positive bacteria including Bacillus subtilis, Staphylococcus aureus, and Micrococcus luteus.

Nutrient Optimization Using Response Surface Methodology for Simultaneous Biomass and Bioactive Compound Production by Lion's Mane Medicinal Mushroom, Hericium erinaceus (Agaricomycetes).

PubMed

Ofosu, Fred K; Yu, Xiaobin; Wang, Qiang; Li, Hanguang

2016-01-01

Due to the unpleasant side effects of long-term use of commercially available drugs, the discovery and development of natural therapeutic agents to prevent life-debilitating diseases is urgently needed. In the present study, the optimization of medium composition for maximum mycelial biomass and bioactive compounds production by Hericium erinaceus was studied using response surface methodology based on a central composite design. Under the optimal conditions and at a pH of 5.41 ± 0.28, the maximum mycelial biomass and exopolysaccharide production reached 25.0 ± 1.38 g/L and 1.73 ± 0.06 g/L, respectively, compared with 22.65 ± 0.10 g/L and 1.56 ± 0.23 g/L in the basal medium, after 7 days of cultivation. Furthermore, we report for the first time the production of adenosine, both intra- and extracellularly in submerged cultures of H. erinaceus. Although most of the adenosine detected existed in the culture medium, the highest intracellular and extracellular adenosine concentrations of 150.84 ± 1.87 mg/L and 142.48 ± 3.78 mg/L were achieved after 7 and 6 days of cultivation, respectively.

Spirolactones: Recent Advances in Natural Products, Bioactive Compounds and Synthetic Strategies.

PubMed

Quintavalla, Arianna

2018-01-01

The spirocyclic compounds have always aroused a great interest because this motif is present as structural core in a number of natural products and bioactive compounds. In particular, the spirolactone moiety has been recognized in a wide array of natural and non-natural scaffolds showing a variety of useful pharmacological properties. Extensive literature search using SciFinder (Databases: CA Plus, CAS Registry, CAS React, Chemlist, Chemcat and Medline) and Web of Science (Database: Web of Science Core Collection) was conducted. Nowadays, many efforts are being devoted to the discovery of new natural products containing the promising spirolactone framework and to the disclosure of the potential bioactivities of these chemical entities. Moreover, the medicinal relevance of many spirolactones makes these scaffolds attractive targets for the design and development of innovative and efficient synthetic strategies, enabling the construction of complex and variably substituted products. This review gives an overview on the recent advances in the spirolactones field, in terms of new compounds isolated from natural sources, recently determined bioactivity profiles and innovative synthetic approaches. The collected data demonstrate the key role played by spirolactones in medicinal chemistry and the great attention still devoted by the scientific community to these compounds. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Quantitative and fingerprint analyses of Chinese sweet tea plant (Rubus Suavissimus S. Lee)

PubMed Central

Chou, Guixin; Xu, Shun-Jun; Liu, Dong; Koh, Gar Yee; Zhang, Jian; Liu, Zhijun

2009-01-01

Quality of botanical food is increasingly assessed by the content of multiple bioactive compounds. In this study we report, for the first time, an HPLC fingerprinting method for the quality evaluation of Rubus suavissimus leaves possessing multiple bioactivities. Five constituents, gallic acid, rutin, ellagic acid, rubusoside, and steviol monoside were quantified and used in developing qualitative chromatographic fingerprints. The limits of detection and quantification ranged from 0.29 μg/mL to 37.86 μg/mL. The relative standard deviations (RSDs) of intra- and inter-day precisions were no more than 3.14% and 3.01%, respectively. The average recoveries were between 93.1% and 97.5%. The developed method was validated in analyzing fourteen leaf samples with satisfactory results. The contents of the five marker compounds accounted for an average of about 6% w/w with a variability of 16% among the fourteen samples collected from a single site and year. Gallic acid was the least whereas steviol monoside the most variable compounds among the fourteen leaf samples. The characteristic compound rubusoside that is responsible for the sweet taste accounted for 5% of leaf weight. The validated method can now be used to quantitatively and qualitatively assess the quality of Rubus suavissimus leaves as traditional beverage or potential medicines. PMID:19138116

Italian Opuntia ficus-indica Cladodes as Rich Source of Bioactive Compounds with Health-Promoting Properties

PubMed Central

Pellizzoni, Marco; Lucini, Luigi

2018-01-01

Natural by-products, especially phenolic compounds, are in great demand by the nutra-pharmaceutical and biomedical industries. An analytical study was performed to investigate, for the first time, the presence of antioxidant constituents and the corresponding in vitro antioxidant activity in the extract of cladodes from Ficodindia di San Cono (Opuntia ficus-indica) protected designation of origin (PDO). The cladode extracts were analysed for target determination of selected constituents, i.e., β-polysaccharides and total phenolic content. Moreover, the antioxidant activity of hydro-alcoholic extracts was assessed by means of two different methods: α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method and ferric reducing antioxidant power (FRAP) assay. An untargeted UHPLC-ESI-QTOF-MS profiling approach was used to depict the phenolic profile of hydro-alcoholic cladode extracts. Interestingly, over 2 g/kg of polyphenols were detected in this matrix, and these compounds were mainly responsible for the antioxidant properties, as shown by the strong correlation between phenolic classes and antioxidant scores. Finally, this study provides basic information on the presence of bioactive compounds and in vitro antioxidant activities in cladode extracts from cactus that might recommend their novel applications at the industrial level in the field of nutraceutical products. PMID:29463028

Italian Opuntia ficus-indica Cladodes as Rich Source of Bioactive Compounds with Health-Promoting Properties.

PubMed

Rocchetti, Gabriele; Pellizzoni, Marco; Montesano, Domenico; Lucini, Luigi

2018-02-18

Natural by-products, especially phenolic compounds, are in great demand by the nutra-pharmaceutical and biomedical industries. An analytical study was performed to investigate, for the first time, the presence of antioxidant constituents and the corresponding in vitro antioxidant activity in the extract of cladodes from Ficodindia di San Cono ( Opuntia ficus-indica ) protected designation of origin (PDO). The cladode extracts were analysed for target determination of selected constituents, i.e. β-polysaccharides and total phenolic content. Moreover, the antioxidant activity of hydro-alcoholic extracts was assessed by means of two different methods: α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method and ferric reducing antioxidant power (FRAP) assay. An untargeted UHPLC-ESI-QTOF-MS profiling approach was used to depict the phenolic profile of hydro-alcoholic cladode extracts. Interestingly, over 2 g/kg of polyphenols were detected in this matrix, and these compounds were mainly responsible for the antioxidant properties, as shown by the strong correlation between phenolic classes and antioxidant scores. Finally, this study provides basic information on the presence of bioactive compounds and in vitro antioxidant activities in cladode extracts from cactus that might recommend their novel applications at the industrial level in the field of nutraceutical products.

Effect of physiological harvest stages on the composition of bioactive compounds in Cavendish bananas*

PubMed Central

Bruno Bonnet, Christelle; Hubert, Olivier; Mbeguie-A-Mbeguie, Didier; Pallet, Dominique; Hiol, Abel; Reynes, Max; Poucheret, Patrick

2013-01-01

The combined influence of maturation, ripening, and climate on the profile of bioactive compounds was studied in banana (Musa acuminata, AAA, Cavendish, cv. Grande Naine). Their bioactive compounds were determined by the Folin-Ciocalteu assay and high-performance thin layer chromatographic (HPTLC) method. The polyphenol content of bananas harvested after 400 degree days remained unchanged during ripening, while bananas harvested after 600 and 900 degree days exhibited a significant polyphenol increase. Although dopamine was the polyphenol with the highest concentration in banana peels during the green developmental stage and ripening, its kinetics differed from the total polyphenol profile. Our results showed that this matrix of choice (maturation, ripening, and climate) may allow selection of the banana (M. acuminata, AAA, Cavendish, cv. Grande Naine) status that will produce optimal concentrations of identified compounds with human health relevance. PMID:23549844

Peanuts as functional food: a review.

PubMed

Arya, Shalini S; Salve, Akshata R; Chauhan, S

2016-01-01

Peanut is an important crop grown worldwide. Commercially it is used mainly for oil production but apart from oil, the by-products of peanut contains many other functional compounds like proteins, fibers, polyphenols, antioxidants, vitamins and minerals which can be added as a functional ingredient into many processed foods. Recently it has also revealed that peanuts are excellent source of compounds like resveratrol, phenolic acids, flavonoids and phytosterols that block the absorption of cholesterol from diet. It is also a good source of Co-enzyme Q10 and contains all the 20 amino acids with highest amount of arginine. These bioactive compounds have been recognized for having disease preventive properties and are thought to promote longevity. The processing methods like roasting and boiling have shown increase in the concentration of these bioactive compounds. In the present paper an overview on peanut bioactive constituents and their health benefits are presented.

Change of Bioactive Constituent in Clinacanthus nutans Leaves under Sun Drying

NASA Astrophysics Data System (ADS)

Abdullah, Sriyana; Aziz, Muhamad Faris Abdul

2018-03-01

Clinacanthus nutans (C. nutans) or locally known as belalai gajah is a folk medicine since ancient time. This research project was established to investigate the effects of under sun drying on the C. nutans bioactive constituent. The drying experiments were conducted using different drying surfaces i.e. perforated, black polythene and white polythene. The fresh and dried leaves were then extracted using a sonicator to evaluate its bioactive constituent. The total phenolic content (TPC) in the C. nutans extracts were determined using Follin Ciocalteu reagent method to represent the bioactive constituent. Drying over the white polythene surface showed the slowest reduction of moisture content as compared to the perforated polythene and black surfaces. Results also showed no significant effect of the drying surfaces on the TPC. However, the TPC in the dried leaves was significantly higher than in the fresh leaves. This may be due to the plant cells response to abiotic stress and the inhibition of oxidation enzymes. Therefore, drying C. nutanc leaves under sun light could be considered in order to preserve the concentration of phenolic compounds and for minimizing energy consumption.

Identifying relationships between unrelated pharmaceutical target proteins on the basis of shared active compounds.

PubMed

Miljković, Filip; Kunimoto, Ryo; Bajorath, Jürgen

2017-08-01

Computational exploration of small-molecule-based relationships between target proteins from different families. Target annotations of drugs and other bioactive compounds were systematically analyzed on the basis of high-confidence activity data. A total of 286 novel chemical links were established between distantly related or unrelated target proteins. These relationships involved a total of 1859 bioactive compounds including 147 drugs and 141 targets. Computational analysis of large amounts of compounds and activity data has revealed unexpected relationships between diverse target proteins on the basis of compounds they share. These relationships are relevant for drug discovery efforts. Target pairs that we have identified and associated compound information are made freely available.

Ultrasound-Assisted Extraction of Cannabinoids from Cannabis Sativa L. Optimized by Response Surface Methodology.

PubMed

Agarwal, Charu; Máthé, Katalin; Hofmann, Tamás; Csóka, Levente

2018-03-01

Ultrasonication was used to extract bioactive compounds from Cannabis sativa L. such as polyphenols, flavonoids, and cannabinoids. The influence of 3 independent factors (time, input power, and methanol concentration) was evaluated on the extraction of total phenols (TPC), flavonoids (TF), ferric reducing ability of plasma (FRAP) and the overall yield. A face-centered central composite design was used for statistical modelling of the response data, followed by regression and analysis of variance in order to determine the significance of the model and factors. Both the solvent composition and the time significantly affected the extraction while the sonication power had no significant impact on the responses. The response predictions obtained at optimum extraction conditions of 15 min time, 130 W power, and 80% methanol were 314.822 mg GAE/g DW of TPC, 28.173 mg QE/g DW of TF, 18.79 mM AAE/g DW of FRAP, and 10.86% of yield. A good correlation was observed between the predicted and experimental values of the responses, which validated the mathematical model. On comparing the ultrasonic process with the control extraction, noticeably higher values were obtained for each of the responses. Additionally, ultrasound considerably improved the extraction of cannabinoids present in Cannabis. Low frequency ultrasound was employed to extract bioactive compounds from the inflorescence part of Cannabis. The responses evaluated were-total phenols, flavonoids, ferric reducing assay and yield. The solvent composition and time significantly influenced the extraction process. Appreciably higher extraction of cannabinoids was achieved on sonication against control. © 2018 Institute of Food Technologists®.

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

Immobilized magnetic beads-based multi-target affinity selection coupled with HPLC-MS for screening active compounds from traditional Chinese medicine and natural products.

PubMed

Chen, Yaqi; Chen, Zhui; Wang, Yi

2015-01-01

Screening and identifying active compounds from traditional Chinese medicine (TCM) and other natural products plays an important role in drug discovery. Here, we describe a magnetic beads-based multi-target affinity selection-mass spectrometry approach for screening bioactive compounds from natural products. Key steps and parameters including activation of magnetic beads, enzyme/protein immobilization, characterization of functional magnetic beads, screening and identifying active compounds from a complex mixture by LC/MS, are illustrated. The proposed approach is rapid and efficient in screening and identification of bioactive compounds from complex natural products.

Bioactivity-Guided Metabolite Profiling of Feijoa ( Acca sellowiana) Cultivars Identifies 4-Cyclopentene-1,3-dione as a Potent Antifungal Inhibitor of Chitin Synthesis.

PubMed

Mokhtari, Mona; Jackson, Michael D; Brown, Alistair S; Ackerley, David F; Ritson, Nigel J; Keyzers, Robert A; Munkacsi, Andrew B

2018-06-06

Pathogenic fungi continue to develop resistance against current antifungal drugs. To explore the potential of agricultural waste products as a source of novel antifungal compounds, we obtained an unbiased GC-MS profile of 151 compounds from 16 commercial and experimental cultivars of feijoa peels. Multivariate analysis correlated 93% of the compound profiles with antifungal bioactivities. Of the 18 compounds that significantly correlated with antifungal activity, 5 had not previously been described from feijoa. Two novel cultivars were the most bioactive, and the compound 4-cyclopentene-1,3-dione, detected in these cultivars, was potently antifungal (IC 50 = 1-2 μM) against human-pathogenic Candida species. Haploinsufficiency and fluorescence microscopy analyses determined that the synthesis of chitin, a fungal-cell-wall polysaccharide, was the target of 4-cyclopentene-1,3-dione. This fungal-specific mechanism was consistent with a 22-70-fold reduction in antibacterial activity. Overall, we identified the agricultural waste product of specific cultivars of feijoa peels as a source of potential high-value antifungal compounds.

Whey acerola-flavoured drink submitted Ohmic Heating: Bioactive compounds, antioxidant capacity, thermal behavior, water mobility, fatty acid profile and volatile compounds.

PubMed

Cappato, Leandro P; Ferreira, Marcus Vinicius S; Moraes, Jeremias; Pires, Roberto P S; Rocha, Ramon S; Silva, Ramon; Neto, Roberto P C; Tavares, Maria Inês B; Freitas, Mônica Q; Rodrigues, Flavio N; Calado, Veronica M A; Raices, Renata S L; Silva, Marcia C; Cruz, Adriano G

2018-10-15

Whey acerola-flavoured drink was subjected to Ohmic Heating (OH) under different operational conditions (45, 60, 80 V at 60 Hz and 10, 100, 1000 Hz with 25 V, 65 °C/30 min) and conventional pasteurization (65 °C/30 min). Bioactive compounds (total phenolics, DPPH, FRAP, ACE levels), fatty acid profile, volatile compounds (CG-MS), thermal behaviors (DSC) and water mobility (TD-NMR) were performed. Reduction of frequency (1000-10 Hz) resulted in a lower bioactive compounds and antioxidant capacity of the samples, except for the DPPH values. Concerning the thermal behaviors, fatty acids profile and volatile compounds, different findings were observed as a function of the parameters used (voltage and frequency). In respect of TD-NMR parameters, OH led to a slightly reduction of the relaxation time when compared to the conventional treatment, suggesting more viscous beverages. Overall, OH may be interesting option to whey acerola-flavoured drink processing. Copyright © 2018 Elsevier Ltd. All rights reserved.

Marine Rare Actinobacteria: Isolation, Characterization, and Strategies for Harnessing Bioactive Compounds

PubMed Central

Dhakal, Dipesh; Pokhrel, Anaya Raj; Shrestha, Biplav; Sohng, Jae Kyung

2017-01-01

Actinobacteria are prolific producers of thousands of biologically active natural compounds with diverse activities. More than half of these bioactive compounds have been isolated from members belonging to actinobacteria. Recently, rare actinobacteria existing at different environmental settings such as high altitudes, volcanic areas, and marine environment have attracted attention. It has been speculated that physiological or biochemical pressures under such harsh environmental conditions can lead to the production of diversified natural compounds. Hence, marine environment has been focused for the discovery of novel natural products with biological potency. Many novel and promising bioactive compounds with versatile medicinal, industrial, or agricultural uses have been isolated and characterized. The natural compounds cannot be directly used as drug or other purposes, so they are structurally modified and diversified to ameliorate their biological or chemical properties. Versatile synthetic biological tools, metabolic engineering techniques, and chemical synthesis platform can be used to assist such structural modification. This review summarizes the latest studies on marine rare actinobacteria and their natural products with focus on recent approaches for structural and functional diversification of such microbial chemicals for attaining better applications. PMID:28663748

Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages.

PubMed

Thi, Nhuan Do; Hwang, Eun-Sun

2014-09-01

The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols.

Bioactive Compound Contents and Antioxidant Activity in Aronia (Aronia melanocarpa) Leaves Collected at Different Growth Stages

PubMed Central

Thi, Nhuan Do; Hwang, Eun-Sun

2014-01-01

The bioactive compounds and antioxidant activity of aronia leaves at different stages of maturity were identified and evaluated. Young and old leaves were approximately 2 months of age and 4 months of age, respectively. The young leaves contained more polyphenols and flavonoids than the old leaves. Three phenolic compounds (i.e., chlorogenic acid, p-coumaric acid, and rutin) were detected by HPLC. Antioxidant activity was measured using 2,2-di-phenyl-1-picrylhydrazyl (DPPH) radical, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical, and superoxide anion radical scavenging assays. The reducing power of aronia leaf extracts increased in a concentration-dependent manner (0~100 μg/mL). The antioxidant activity of the 80% ethanol extract was greater than that of distilled water extract. The high phenolic compound content indicated that these compounds contribute to antioxidant activity. The overall results indicate that aronia leaves contain bioactive compounds, and that younger aronia leaves may be more favorable for extracting antioxidative ingredients because they contain more polyphenols. PMID:25320718

Characteristics, chemical compositions and biological activities of propolis from Al-Bahah, Saudi Arabia

PubMed Central

Elnakady, Yasser A.; Rushdi, Ahmed I.; Franke, Raimo; Abutaha, Nael; Ebaid, Hossam; Baabbad, Mohannad; Omar, Mohamed O. M.; Al Ghamdi, Ahmad A.

2017-01-01

Propolis has been used to treat several diseases since ancient times, and is an important source of bioactive natural compounds and drug derivatives. These properties have kept the interest of investigators around the world, leading to the investigation of the chemical and biological properties and application of propolis. In this report, the chemical constituents that are responsible for the anticancer activities of propolis were analyzed. The propolis was sourced from Al-Baha in the southern part of the Kingdom of Saudi Arabia. Standard protocols for chemical fractionation and bioactivity-guided chemical analysis were used to identify the bio-active ethyl acetate fraction. The extraction was performed in methanol and then analyzed by gas chromatography-mass spectrometry (GC-MS). The major compounds are triterpenoids, with a relative concentration of 74.0%; steroids, with a relative concentration of 9.8%; and diterpenoids, with a relative concentration of 7.9%. The biological activity was characterized using different approaches and cell-based assays. Propolis was found to inhibit the proliferation of cancer cells in a concentration-dependent manner through apoptosis. Immunofluorescence staining with anti-α-tubulin antibodies and cell cycle analysis indicated that tubulin and/or microtubules are the cellular targets of the L-acetate fraction. This study demonstrates the importance of Saudi propolis as anti-cancer drug candidates. PMID:28165013

Characteristics, chemical compositions and biological activities of propolis from Al-Bahah, Saudi Arabia

NASA Astrophysics Data System (ADS)

Elnakady, Yasser A.; Rushdi, Ahmed I.; Franke, Raimo; Abutaha, Nael; Ebaid, Hossam; Baabbad, Mohannad; Omar, Mohamed O. M.; Al Ghamdi, Ahmad A.

2017-02-01

Propolis has been used to treat several diseases since ancient times, and is an important source of bioactive natural compounds and drug derivatives. These properties have kept the interest of investigators around the world, leading to the investigation of the chemical and biological properties and application of propolis. In this report, the chemical constituents that are responsible for the anticancer activities of propolis were analyzed. The propolis was sourced from Al-Baha in the southern part of the Kingdom of Saudi Arabia. Standard protocols for chemical fractionation and bioactivity-guided chemical analysis were used to identify the bio-active ethyl acetate fraction. The extraction was performed in methanol and then analyzed by gas chromatography-mass spectrometry (GC-MS). The major compounds are triterpenoids, with a relative concentration of 74.0%; steroids, with a relative concentration of 9.8%; and diterpenoids, with a relative concentration of 7.9%. The biological activity was characterized using different approaches and cell-based assays. Propolis was found to inhibit the proliferation of cancer cells in a concentration-dependent manner through apoptosis. Immunofluorescence staining with anti-α-tubulin antibodies and cell cycle analysis indicated that tubulin and/or microtubules are the cellular targets of the L-acetate fraction. This study demonstrates the importance of Saudi propolis as anti-cancer drug candidates.

Innovative natural functional ingredients from microalgae.

PubMed

Plaza, Merichel; Herrero, Miguel; Cifuentes, Alejandro; Ibáñez, Elena

2009-08-26

Nowadays, a wide variety of compounds such as polyphenols, polyunsaturated fatty acids (PUFA), or phytosterols obtained, for example, from wine, fish byproducts, or plants are employed to prepare new functional foods. However, unexplored natural sources of bioactive ingredients are gaining much attention since they can lead to the discovery of new compounds or bioactivities. Microalgae have been proposed as an interesting, almost unlimited, natural source in the search for novel natural functional ingredients, and several works have shown the possibility to find bioactive compounds in these organisms. Some advantages can be associated with the study of microalgae such as their huge diversity, the possibility of being used as natural reactors at controlled conditions, and their ability to produce active secondary metabolites to defend themselves from adverse or extreme conditions. In this contribution, an exhaustive revision is presented involving the research for innovative functional food ingredients from microalgae. The most interesting results in this promising field are discussed including new species composition and bioactivity and new processing and extraction methods. Moreover, the future research trends are critically commented.

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

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

Electric-field triggered controlled release of bioactive volatiles from imine-based liquid crystalline phases.

PubMed

Herrmann, Andreas; Giuseppone, Nicolas; Lehn, Jean-Marie

2009-01-01

Application of an electric field to liquid crystalline film forming imines with negative dielectric anisotropy, such as N-(4-methoxybenzylidene)-4-butylaniline (MBBA, 1), results in the expulsion of compounds that do not participate in the formation of the liquid crystalline phase. Furthermore, amines and aromatic aldehydes undergo component exchange with the imine by generating constitutional dynamic libraries. The strength of the electric field and the duration of its application to the liquid crystalline film influence the release rate of the expelled compounds and, at the same time, modulate the equilibration of the dynamic libraries. The controlled release of volatile organic molecules with different chemical functionalities from the film was quantified by dynamic headspace analysis. In all cases, higher headspace concentrations were detected in the presence of an electric field. These results point to the possibility of using imine-based liquid crystalline films to build devices for the controlled release of a broad variety of bioactive volatiles as a direct response to an external electric signal.

Potential Pharmacological Resources: Natural Bioactive Compounds from Marine-Derived Fungi

PubMed Central

Jin, Liming; Quan, Chunshan; Hou, Xiyan; Fan, Shengdi

2016-01-01

In recent years, a considerable number of structurally unique metabolites with biological and pharmacological activities have been isolated from the marine-derived fungi, such as polyketides, alkaloids, peptides, lactones, terpenoids and steroids. Some of these compounds have anticancer, antibacterial, antifungal, antiviral, anti-inflammatory, antioxidant, antibiotic and cytotoxic properties. This review partially summarizes the new bioactive compounds from marine-derived fungi with classification according to the sources of fungi and their biological activities. Those fungi found from 2014 to the present are discussed. PMID:27110799

Effect of different coatings on post-harvest quality and bioactive compounds of pomegranate (Punica granatum L.) fruits.

PubMed

Meighani, Hossein; Ghasemnezhad, Mahmood; Bakhshi, Davood

2015-07-01

The effect of three different coatings; resin wax (Britex Ti), carnauba wax (Xedasol M14), and chitosan (1 and 2 % w/v) on postharvest quality of pomegranate fruits were investigated. Fruits quality characteristics and bioactive compounds were evaluated during 40, 80 and 120 days storage at 4.5 °C and 3 additional days at 20 °C. The results showed that uncoated fruits showed higher respiration rate, weight loss, L* and b* values of arils, total soluble solids (TSS)/titratable acidity (TA), and pH than coated fruits during storage. Coating treatments could delay declining TSS and TA percent, a* value of arils, as well as bioactive compounds such as total phenolics, flavonoids and anthocyanins content and antioxidant activity. The coated fruits with commercial resin and carnauba waxes showed significantly lower respiration rate and weight loss than other treatments, however carnauba wax could maintain considerably higher fruits quality and bioactive compounds than other coating treatments. The results suggested that postharvest application of carnauba wax have a potential to extend storage life of pomegranate fruits by reducing respiration rate, water loss and maintaining fruit quality.

Comparison of Bioactive Compounds and Quality Traits of Breast Meat from Korean Native Ducks and Commercial Ducks

PubMed Central

Kim, Sun Hyo; Heo, Kang Nyung

2015-01-01

The aim of this research was to compare the bioactive compound content and quality traits of breast meat from male and female Korean native ducks (KND) and commercial ducks (CD, Cherry Valley). Meat from three 6-wk old birds of each sex from KND and CD were evaluated for carcass and breast weights, pH, color, cooking loss, shear force, and bioactive compound (creatine, carnosine, anserine, betaine, and L-carnitine) content. KND showed significantly higher carcass weights than CD whereas no such difference (p>0.05) was found between male and female ducks. The breed and sex had no significant effects on the breast weight, pH value, and shear force. However, KND had significantly lower cooking loss values than did CD. Creatine, anserine, and L-carnitine contents were significantly higher in KND than in CD and were predominant in female ducks compared to males. The results of this study provide rare information regarding the amounts and the determinants of several bioactive compounds in duck meat, which can be useful for selection and breeding programs, and for popularizing indigenous duck meat. PMID:26761808

Bioactive Compounds and Fruit Quality of Green Sweet Pepper Grown under Different Colored Shade Netting during Postharvest Storage.

PubMed

Mashabela, Madonna N; Selahle, Kamogelo M; Soundy, Puffy; Crosby, Kevin M; Sivakumar, Dharini

2015-11-01

In this study, influence of 3 types of photo-selective nets (pearl, red and yellow) and a standard black net on marketable yield, fruit quality and bioactive compounds after postharvest storage was investigated. Percentage marketable fruits were higher in green sweet peppers produced under the pearl nets. Fruits produced under the pearl nets showed higher fruit mass, firmness, chlorophyll content, ascorbic acid content, antioxidant scavenging activity after postharvest storage. Red/far red photon ratio under the pearl net could have improved the ascorbic acid content and the antioxidant scavenging activity in green peppers. Green sweet peppers grown under the pearl nets had higher hue values and maintained green color longer. Our results showed the impact of modified light quality on the bioactive compounds of green sweet pepper during postharvest storage. Green sweet peppers are rich in phytochemicals. Marketability of green sweet peppers is affected partially due to ripening after postharvest storage and decay. Maintenance of green color, fruit mass, firmness, and nutritional composition are important parameters that attract consumers. This research shows the influence of light quality during production on the fruit quality parameters and bioactive compounds after postharvest storage. © 2015 Institute of Food Technologists®

Preparation of stimulus responsive multiple emulsions by membrane emulsification using con a as biochemical sensor.

PubMed

Piacentini, Emma; Drioli, Enrico; Giorno, Lidietta

2011-04-01

In this work, a novel strategy for the controlled fabrication of biomolecular stimulus responsive water-in-oil-in-water (W/O/W) multiple emulsion using the membrane emulsification process was investigated. The emulsions interface was functionalized with a biomolecule able to function as a receptor for a target compound. The interaction between the biomolecular receptor and target stimulus activated the release of bioactive molecules contained within the structured emulsion. A glucose sensitive emulsion was investigated as a model study case. Concanavalin A (Con A) was used as the biomolecular glucose sensor. Various physicochemical strategies for stimulus responsive materials formulation are available in literature, but the preparation of biomolecule-responsive emulsions has been explored for the first time in this paper. The development of novel drug delivery systems requires advanced and highly precise techniques to obtain their particular properties and targeting requirements. The present study has proven the flexibility and suitability of membrane emulsification for the preparation of stable and functional multiple emulsions containing Con A as interfacial biomolecular receptor able to activate the release of a bioactive molecule as a consequence of interaction with the glucose target molecule. The influence of emulsion interfacial composition and membrane emulsification operating conditions on droplets stability and functional properties have been investigated. The release of the bioactive molecule as a function of glucose stimulus and its concentration has been demonstrated. Copyright © 2010 Wiley Periodicals, Inc.

Screening plant derived dietary phenolic compounds for bioactivity related to cardiovascular disease.

PubMed

Croft, Kevin D; Yamashita, Yoko; O'Donoghue, Helen; Shirasaya, Daishi; Ward, Natalie C; Ashida, Hitoshi

2018-04-01

The potential health benefits of phenolic acids found in food and beverages has been suggested from a number of large population studies. However, the mechanism of how these compounds may exert biological effects is less well established. It is also now recognised that many complex polyphenols in the diet are metabolised to simple phenolic acids which can be taken up in the circulation. In this paper a number of selected phenolic compounds have been tested for their bioactivity in two cell culture models. The expression and activity of endothelial nitric oxide synthase (eNOS) in human aortic endothelial cells and the uptake of glucose in muscle cells. Our data indicate that while none of the compounds tested had a significant effect on eNOS expression or activation in endothelial cells, several of the compounds increased glucose uptake in muscle cells. These compounds also enhanced the translocation of the glucose transporter GLUT4 to the plasma membrane, which may explain the observed increase in cellular glucose uptake. These results indicate that simple cell culture models may be useful to help understand the bioactivity of phenolic compounds in relation to cardiovascular protection. Copyright © 2017 Elsevier B.V. All rights reserved.

Metabolic profiling of sourdough fermented wheat and rye bread.

PubMed

Koistinen, Ville M; Mattila, Outi; Katina, Kati; Poutanen, Kaisa; Aura, Anna-Marja; Hanhineva, Kati

2018-04-09

Sourdough fermentation by lactic acid bacteria is commonly used in bread baking, affecting several attributes of the final product. We analyzed whole-grain wheat and rye breads and doughs prepared with baker's yeast or a sourdough starter including Candida milleri, Lactobacillus brevis and Lactobacillus plantarum using non-targeted metabolic profiling utilizing LC-QTOF-MS. The aim was to determine the fermentation-induced changes in metabolites potentially contributing to the health-promoting properties of whole-grain wheat and rye. Overall, we identified 118 compounds with significantly increased levels in sourdough, including branched-chain amino acids (BCAAs) and their metabolites, small peptides with high proportion of BCAAs, microbial metabolites of phenolic acids and several other potentially bioactive compounds. We also identified 69 compounds with significantly decreased levels, including phenolic acid precursors, nucleosides, and nucleobases. Intensive sourdough fermentation had a higher impact on the metabolite profile of whole-grain rye compared to milder whole-grain wheat sourdough fermentation. We hypothesize that the increased amount of BCAAs and potentially bioactive small peptides may contribute to the insulin response of rye bread, and in more general, the overall protective effect against T2DM and CVD.

Selective enrichment in bioactive compound from Kniphofia uvaria by super/subcritical fluid extraction and centrifugal partition chromatography.

PubMed

Duval, Johanna; Destandau, Emilie; Pecher, Virginie; Poujol, Marion; Tranchant, Jean-François; Lesellier, Eric

2016-05-20

Nowadays, a large portion of synthetic products (active cosmetic and therapeutic ingredients) have their origin in natural products. Kniphofia uvaria is a plant from Africa which has proved in the past by in-vivo tests an antioxidant activity due to compounds present in roots. Recently, we have observed anthraquinones in K. uvaria seeds extracts. These derivatives are natural colorants which could have interesting bioactive potential. The aim of this study was to obtain an extract enriched in anthraquinones from K. uvaria seeds which mainly contains glycerides. First, the separation of the seed compounds was studied by using supercritical fluid chromatography (SFC) in the goal to provide a rapid quantification method of these bioactive compounds. A screening of numerous polar stationary phases was achieved for selecting the most suited phase to the separation of the four anthraquinones founded in the seeds. A gradient elution was optimized for improving the separation of the bioactive compounds from the numerous other families of major compounds of the extracts (fatty acids, di- and triglycerides). Besides, a non-selective and green Supercritical Fluid Extraction (SFE) with pure CO2 was applied to seeds followed by a Centrifugal Partition Chromatography (CPC). The CPC system was optimized by using the Arizona phase system, to enrich the extract in anthraquinones. Two systems were selected to isolate the bioactive compounds from the oily extract with varied purity target. The effect of the injection mode for these very viscous samples was also studied. Finally, in order to directly apply a selective process of extraction to the seeds, the super/subcritical fluid extraction was optimized to increase the anthraquinone yield in the final extract, by studying varied modifier compositions and nature, as well as different temperatures and backpressures. Conditions suited to favour an enrichment factor bases on the ratio of anthraquinone and trilycerides extracted are described. Copyright © 2016 Elsevier B.V. All rights reserved.

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

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

Human liver microsomal cytochrome P-450 enzymes involved in the bioactivation of procarcinogens detected by umu gene response in Salmonella typhimurium TA 1535/pSK1002.

PubMed

Shimada, T; Iwasaki, M; Martin, M V; Guengerich, F P

1989-06-15

A total of 57 procarcinogens was examined for induction of umu gene response in the chimeric plasmid pSK1002, carried in Salmonella typhimurium TA 1535, after incubation with a series of human liver microsomal preparations which had been selected on the basis of characteristic levels of individual cytochrome P-450 (P-450) enzymes. The 18 most active compounds were selected and further analyzed using the umu gene response and correlative studies with a larger number of microsomal preparations, enzyme reconstitution studies involving purified enzymes, immunochemical inhibition, and patterns of stimulation and inhibition of catalytic activity by 7,8-benzoflavone. The results collectively indicate that 16 of these 18 most potent genotoxins examined are activated primarily either by P-450NF (the nifedipine oxidase) or P-450PA (the phenacetin O-deethylase). P-450NF appears to be the major enzyme involved in the bioactivation of aflatoxin B1, aflatoxin G1, sterigmatocystin, trans-7,8-dihydroxy-7,8-dihydrobenzo(a)pyrene, 6-aminochrysene, and tris-(2,3-dibromopropyl)phosphate in human liver. P-450PA appears to be the major enzyme involved in the bioactivation of 2-amino-3-methylimidazo[4,5-f]quinoline, 2-amino-3,5-dimethylimidazo[4, 5-f]quinoline, 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline, 2-aminoanthracene, 2-amino-6-methyldipyrido[1,2-a:3',2'-d]imidazole, 2-aminofluorene, 2-acetylaminofluorene, 4-aminobiphenyl, 3-amino-1-methyl-5H-pyrido[4,3-b] indole, and 2-aminodipyrido[1,2-a:3',2'-d]imidazole. More than one enzyme appears to contribute significantly to the bioactivation of the other two compounds examined, 3-amino-1,4-dimethyl-5H-pyrido[4,3-b] indole and 6-nitrochrysene. The literature suggests that the two human liver P-450s involved in activation of these 16 procarcinogens are highly inducible by barbiturates, macrolide antibodies, and certain steroids (P-450NF) and by smoking and ingestion of charcoal-containing food (P-450PA); noninvasive assays are available to monitor the function of both P-450NF and P-450PA.

Extraction of triterpenoids and phenolic compounds from Ganoderma lucidum: optimization study using the response surface methodology.

PubMed

Oludemi, Taofiq; Barros, Lillian; Prieto, M A; Heleno, Sandrina A; Barreiro, Maria F; Ferreira, Isabel C F R

2018-01-24

The extraction of triterpenoids and phenolic compounds from Ganoderma lucidum was optimized by using the response surface methodology (RSM), using heat and ultrasound assisted extraction techniques (HAE and UAE). The obtained results were compared with that of the standard Soxhlet procedure. RSM was applied using a circumscribed central composite design with three variables (time, ethanol content, and temperature or ultrasonic power) and five levels. The conditions that maximize the responses (extraction yield, triterpenoids and total phenolics) were: 78.9 min, 90.0 °C and 62.5% ethanol and 40 min, 100.0 W and 89.5% ethanol for HAE and UAE, respectively. The latter was the most effective, resulting in an extraction yield of 4.9 ± 0.6% comprising a content of 435.6 ± 21.1 mg g -1 of triterpenes and 106.6 ± 16.2 mg g -1 of total phenolics. The optimized extracts were fully characterized in terms of individual phenolic compounds and triterpenoids by HPLC-DAD-ESI/MS. The recovery of the above-mentioned bioactive compounds was markedly enhanced using the UAE technique.

Integration of Microfractionation, qNMR and Zebrafish Screening for the In Vivo Bioassay-Guided Isolation and Quantitative Bioactivity Analysis of Natural Products

PubMed Central

Maes, Jan; Siverio-Mota, Dany; Marcourt, Laurence; Munck, Sebastian; Kamuhabwa, Appolinary R.; Moshi, Mainen J.; Esguerra, Camila V.; de Witte, Peter A. M.; Crawford, Alexander D.; Wolfender, Jean-Luc

2013-01-01

Natural products (NPs) are an attractive source of chemical diversity for small-molecule drug discovery. Several challenges nevertheless persist with respect to NP discovery, including the time and effort required for bioassay-guided isolation of bioactive NPs, and the limited biomedical relevance to date of in vitro bioassays used in this context. With regard to bioassays, zebrafish have recently emerged as an effective model system for chemical biology, allowing in vivo high-content screens that are compatible with microgram amounts of compound. For the deconvolution of the complex extracts into their individual constituents, recent progress has been achieved on several fronts as analytical techniques now enable the rapid microfractionation of extracts, and microflow NMR methods have developed to the point of allowing the identification of microgram amounts of NPs. Here we combine advanced analytical methods with high-content screening in zebrafish to create an integrated platform for microgram-scale, in vivo NP discovery. We use this platform for the bioassay-guided fractionation of an East African medicinal plant, Rhynchosia viscosa, resulting in the identification of both known and novel isoflavone derivatives with anti-angiogenic and anti-inflammatory activity. Quantitative microflow NMR is used both to determine the structure of bioactive compounds and to quantify them for direct dose-response experiments at the microgram scale. The key advantages of this approach are (1) the microgram scale at which both biological and analytical experiments can be performed, (2) the speed and the rationality of the bioassay-guided fractionation – generic for NP extracts of diverse origin – that requires only limited sample-specific optimization and (3) the use of microflow NMR for quantification, enabling the identification and dose-response experiments with only tens of micrograms of each compound. This study demonstrates that a complete in vivo bioassay-guided fractionation can be performed with only 20 mg of NP extract within a few days. PMID:23700445

[Studies on bioactive constituents of whole herbs of Vernonia cinerea].

PubMed

Zhu, Hua-xu; Tang, Yu-ping; Pan, Lin-mei; Min, Zhi-da

2008-08-01

To study the constituents of the whole herbs of Vernonia cinerea. by bio-activity guided isolation with PC-12 model. The constituents were separated by column chromatography and the structures were elucidated by spectroscopic methods. Four compounds were identified to be (+)-lirioresinol B (1), stigmasterol (2), stigmasterol-3-O-beta-D-glucoside (3), 4-sulfo-benzocyclobutene (4), and their NGF inducing activity were also investigated. Compounds 1, 3, 4 were isolated from this genus for the first time, and compound 4 was identified as a new natural product. Compounds 1, 3, 4 showed cytotoxicity on PC-12, and compounds 2, 3, 4 showed inhibition activity. Compound 4 showed a specific effect on the survival of TrkA fibroblasts, and resulted in the inducing NGF activity.

[Study on alkaloids of Corydalis ochotensis and their antitumor bioactivity].

PubMed

Yu, Jia-jia; Cong, Deng-li; Jiang, Ying; Zhou, Yuan; Wang, Yan; Zhao, Chun-fang

2014-10-01

To investigate the chemical constituents of Corydalis ochotensis and their antitumor bioactivity. The compounds were isolated by silica gel column chromatography and recrystallization. Their structures were identified by spectroscopic analysis (NMR) and physicochemical properties. Their cytotoxic activity was studied by MTT. Six compounds were elucidated as protopine (1), ochotensimine (2), fumariline (3), sanguinarine (4), tetrahydroberberine (5) and berberine (6). Compound 1 had excellent inhibitory activity on HepG2, SW480 and A549 cells, and compound 4 had excellent inhibitory activity on Hep2, HepG2, SW480 and A549 cells. Compounds 3, 4 and 5 are isolated from this plant for the first time; In the MTT antitumor experiments,compounds 1 and 4 show an antitumor activity.

Rat health status affects bioavailability, target tissue levels, and bioactivity of grape seed flavanols.

PubMed

Margalef, Maria; Pons, Zara; Iglesias-Carres, Lisard; Quiñones, Mar; Bravo, Francisca Isabel; Arola-Arnal, Anna; Muguerza, Begoña

2017-02-01

Studying the flavanol metabolism is essential to identify bioactive compounds, as beneficial effects of flavanols have been attributed to their metabolic products. However, host-related factors, including pathological conditions, may affect flavanol metabolism and, thus, their bioactivity. This study aims to elucidate whether hypertension affects grape seed flavanol metabolism, influencing their bioactivity in relation to hypertension. Grape seed flavanols' effect on blood pressure (BP) was studied in spontaneously hypertensive rats (SHR) and healthy Wistar rats 6 h after grape seed extract administration (375 mg/kg). Animals were then sacrificed, and plasma bioavailability and aorta distribution of flavanol metabolites were studied by HPLC-MS/MS in both the groups. Grape seed flavanols were only able to decrease BP in SHR. Plasma total flavanol metabolites showed similar levels, being the difference noticed in specific metabolites' concentrations. Specifically, microbial metabolites showed quantitative and qualitative differences between both health states. Moreover, aorta total concentrations were found decreased in SHR. Interestingly, flavanol microbial metabolites were specifically increased SHR aortas, showing qualitative differences in small phenolic forms. This study demonstrates important differences in bioactivity and target tissue metabolite levels between healthy and diseased rats, indicating potential metabolites responsible of the anti-hypertensive effect. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Investigations of vibrational spectra and bioactivity of novel anticancer drug N-(6-ferrocenyl-2-naphthoyl)-gamma-amino butyric acid ethyl ester

NASA Astrophysics Data System (ADS)

Sudhi, Geethu; Rajina, S. R.; Praveen, S. G.; Xavier, T. S.; Kenny, Peter T. M.; Jaiswal-Nagar, D.; Binoy, J.

2017-10-01

The bioactivity of compounds is mainly dependent on molecular structure and the present work aims to explore the bonding features responsible for biological activity of novel anticancer drug N-(6-ferrocenyl-2-naphthoyl)-gamma-amino butyric acid ethyl ester (FNGABEE). In the present study, we investigate the molecular structural properties of newly synthesized title compound through experimental and quantum chemical studies. The detailed vibrational analysis has been performed using FT IR and FT Raman spectrum, aided by DFT computed geometry, vibrational spectrum, Eigen vector distribution and PED, at B3LYP/6-311 ++G(d,p) level. The resonance structure of naphthalene, different from that of benzene, revealed by molecular structure has been investigated using Csbnd C and Cdbnd C stretching modes. The proton transfer in amide has been analyzed to obtain spectral distinction between different carbonyl and Csbnd N groups which point to the reactive sites responsible for binding with DNA and bovine serum albumin (BSA). The spectral distinction between eclipsed and staggered form of ferrocene has been analyzed. The molecular docking of FNGABEE with BSA and DNA has been performed to find the strength of binding and the moieties responsible for the interactions. The experimental binding studies of FNGABEE with BSA and DNA has been performed using UV absorption spectroscopy and fluorometric assay, to find the nature and strength of binding.

Isolation and characterization of bioactive polyacetylenes Panax ginseng Meyer roots.

PubMed

Yeo, Chia-Rou; Yong, Jin-Jie; Popovich, David G

2017-05-30

Panax ginseng has been studied for its chemo-preventive properties and pharmaceutical potential. Polyacetylenic compounds isolated from Panax ginseng root typically comprised of non-polar C 17 compound have been reported to exhibit bioactive properties. The objective of this project is to extract, isolate, and characterize bioactive polyacetylenes from Panax ginseng root using various extraction and separation methods Ginseng was extracted by reflux using methanol, ethanol, hexane, ethyl acetate, methanolic ultrasonication. The extracts were partitioned with hexane to obtain water-soluble portion and hexane-soluble portion. Hexane was subsequently removed under vacuum, and formed a crude polyacetylenes extract (crude PA). Silica gel chromatography and semi-preparative HPLC were utilized to prepare 5 fractions and the polyacetylenes were measure by HPLC and molecular weights confirm my APCI-MS and MNR. The bioactive effect was measured by MTT viability assay using murine 3T3-L1 cells. Extraction with methanol under reflux produced significantly larger amount of polyacetylenes (p<0.05). Liquid-liquid extraction and column chromatography were used to separate polyacetylenic compounds into five different fractions. Major polyacetylenes, panaxynol and panaxydol were found in fraction 1 and 2 respectively. Dose-response relationships were observed in 3T3-L1 cells and LC50 were 13.52±3.05μg/mL (fraction 1), 3.69±1.09μg/mL (fraction 2), 52.88±11.16μg/mL (fraction 3), 85.91±27.37μg/mL (fraction 4) and 135.52±32.91μg/mL (fraction 5). Fraction 2 containing panaxydol was found to have exhibited the greatest anti-proliferative effects on 3T3-L1 preadipocytes. Extraction with methanol under reflux produced significantly more polyacetylenes. Fractions that contain panaxydol was the most cytotoxic. Copyright © 2017 Elsevier B.V. All rights reserved.

The Dual Edema-Preventing Molecular Mechanism of the Crataegus Extract WS 1442 Can Be Assigned to Distinct Phytochemical Fractions.

PubMed

Fuchs, Simone; Bischoff, Iris; Willer, Elisabeth A; Bräutigam, Jacqueline; Bubik, Martin F; Erdelmeier, Clemens A J; Koch, Egon; Faleschini, Maria T; De Mieri, Maria; Bauhart, Milena; Zahler, Stefan; Hensel, Andreas; Hamburger, Matthias; Potterat, Olivier; Fürst, Robert

2017-05-01

The hawthorn ( Crataegus spp.) extract WS 1442 is used against mild forms of chronic heart failure. This disease is associated with endothelial barrier dysfunction and edema formation. We have recently shown that WS 1442 protects against this dysfunction by a dual mechanism: it both promotes endothelial barrier integrity by activation of a barrier-enhancing pathway (cortactin activation) and inhibits endothelial hyperpermeability by blocking a barrier disruptive pathway (calcium signaling). In this study, we aimed to identify the bioactive compounds responsible for these actions by using a bioactivity-guided fractionation approach. From the four fractions generated from WS 1442 by successive elution with water, 95 % ethanol, methanol, and 70 % acetone, only the water fraction was inactive, whereas the other three triggered a reduction of endothelial hyperpermeability. Analyses of intracellular calcium levels and cortactin phosphorylation were used as readouts to estimate the bioactivity of subfractions and isolated compounds. Interestingly, only the ethanolic fraction interfered with the calcium signaling, whereas only the methanolic fraction led to an activation of cortactin. Thus, the dual mode of action of WS 1442 could be clearly assigned to two distinct fractions. Although the identification of the calcium-active substance(s) was not successful, we could exclude an involvement of phenolic compounds. Cortactin activation, however, could be clearly attributed to oligomeric procyanidins with a distinct degree of polymerization. Taken together, our study provides the first approach to identify the active constituents of WS 1442 that address different cellular pathways leading to the inhibition of endothelial barrier dysfunction. Georg Thieme Verlag KG Stuttgart · New York.

Effect of photo-selective nettings on post-harvest quality and bioactive compounds in selected tomato cultivars.

PubMed

Selahle, Maphoko Kamogelo; Sivakumar, Dharini; Soundy, Puffy

2014-08-01

Photo-selective coloured netting is referred to as a 'new agro-technological' concept adopted to manipulate light quality changes that can induce favourable responses in plants. Tomato (Solanum lycopersicum L.) cultivars AlvaV, Irit and SCX 248 grown under the black net (commercial net, 25% shading) showed higher weight loss, loss of firmness, ascorbic acid content and decline in the ratio of soluble solids content/titrable acidity during post-harvest storage (low-temperature storage at 10°C and 90% relative humidity for 21 days followed by market shelf conditions at 25°C for 2 days). During post-harvest storage, lycopene, β-carotene, total phenolic content and antioxidant scavenging activity were higher in cvs AlfaV and Irit grown under the black or pearl nets. However, the β-carotene, total phenolic content and antioxidant scavenging activity were higher in SCX 248 grown under the red net during post-harvest storage. Cultivar AlfaV grown under the red and pearl nets had a higher number of odour active aroma compounds during post-harvest storage. Panellists preferred cv. AlfaV grown under the pearl nets after storage based on taste, overall appearance and firm textured fruits. Pearl photo-selective nets retained the overall fruit quality and bioactive components in cvs AlfaV and Irit during post-harvest storage. Red photo-selective nets, however, showed greater influence on retention of overall fruit quality and bioactive compounds in cv. SCX 248 during post-harvest storage. © 2013 Society of Chemical Industry.

Anti-dengue efficacy of bioactive andrographolide from Andrographis paniculata (Lamiales: Acanthaceae) against the primary dengue vector Aedes aegypti (Diptera: Culicidae).

PubMed

Edwin, Edward-Sam; Vasantha-Srinivasan, Prabhakaran; Senthil-Nathan, Sengottayan; Thanigaivel, Annamalai; Ponsankar, Athirstam; Pradeepa, Venkatraman; Selin-Rani, Selvaraj; Kalaivani, Kandaswamy; Hunter, Wayne B; Abdel-Megeed, Ahmed; Duraipandiyan, Veeramuthu; Al-Dhabi, Naif Abdullah

2016-11-01

The current study investigated the toxic effect of the leaf extract compound andrographolide from Andrographis paniculata (Burm.f) against the dengue vector Ae. aegypti. GC-MS analysis revealed that andrographolide was recognized as the major chemical constituent with the prominent peak area compared with other compounds. All isolated toxic compounds were purified and confirmed through RP-HPLC against chemical standards. The larvicidal assays established at 25ppm of bioactive compound against the treated instars of Ae. Aegypti showed prominent mortality compared to other treated concentrations. The percent mortality of larvae was directly proportional to concentration. The lethal concentration (LC50) was observed at 12ppm treatment concentration. The bioactive andrographolide considerably reduced the detoxifying enzyme regulations of α- and β- carboxylesterases. In contrast, the levels of GST and CYP450 significantly increase in a dose dependent manner. The andrographolide also showed strong oviposition deterrence effects at the sub-lethal dose of 12ppm. Similarly, the mean number of eggs were also significantly reduced in a dose dependent manner. At the concentration of 12ppm the effective percentage of repellency was greater than 90% with a protection time of 15-210min, compared with control. The histopathology study displayed that larvae treated with bioactive andrographolide had cytopathic effects in the midgut epithelium compared with the control. The present study established that bioactive andrographolide served as a potential useful for dengue vector management. Copyright © 2016 Elsevier B.V. All rights reserved.

Juncaceae species as sources of innovative bioactive compounds for the food industry: In vitro antioxidant activity, neuroprotective properties and in silico studies.

PubMed

Rodrigues, Maria João; Gangadhar, Katkam N; Zengin, Gokhan; Mollica, Adriano; Varela, João; Barreira, Luísa; Custódio, Luísa

2017-09-01

Several Juncus species are traditionally used as sedative and to treat health problems like insomnia. This work was based on the hypothesis that Juncus acutus, J. maritimus and J. inflexus may have molecules with bioactivities relevant for the improvement of cognitive functions and thus with potential use as food additives and/or nutraceuticals. Therefore leaves and roots extracts of those species were evaluated for radical scavenging (RSA) and metal chelating activities, and for in vitro inhibition of acetyl-(AChE) and butyrylcholinesterase (BuChE). The bioactive compound was isolated and identified by HPLC-DAD, and its anticholinesterase capacity was determined by different assays. Docking studies were performed to elucidate its inhibitory mechanism. The dichloromethane root extract of J. acutus had the highest RSA against DPPH and ABTS radicals, and the dichloromethane extract of J. maritimus leaves had the uppermost FRAP. The dichloromethane extract from J. acutus leaves had the strongest BuChE inhibition. Juncunol was the bioactive compound, exhibiting dual anticholinesterase capacity on enzyme-based assays and AChE inhibition in neuronal and glial cells in vitro. Molecular docking studies indicate juncunol as a competitive reversible inhibitor. Our results suggest that Juncus spp. can be sources of bioactive compounds with application in the food industry as cognitive-enhancer nutraceuticals. Copyright © 2017 Elsevier Ltd. All rights reserved.

Identification of early target genes of aflatoxin B1 in human hepatocytes, inter-individual variability and comparison with other genotoxic compounds

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

Josse, Rozenn; Dumont, Julie; Fautrel, Alain

Gene expression profiling has recently emerged as a promising approach to identify early target genes and discriminate genotoxic carcinogens from non-genotoxic carcinogens and non-carcinogens. However, early gene changes induced by genotoxic compounds in human liver remain largely unknown. Primary human hepatocytes and differentiated HepaRG cells were exposed to aflatoxin B1 (AFB1) that induces DNA damage following enzyme-mediated bioactivation. Gene expression profile changes induced by a 24 h exposure of these hepatocyte models to 0.05 and 0.25 μM AFB1 were analyzed by using oligonucleotide pangenomic microarrays. The main altered signaling pathway was the p53 pathway and related functions such as cellmore » cycle, apoptosis and DNA repair. Direct involvement of the p53 protein in response to AFB1 was verified by using siRNA directed against p53. Among the 83 well-annotated genes commonly modulated in two pools of three human hepatocyte populations and HepaRG cells, several genes were identified as altered by AFB1 for the first time. In addition, a subset of 10 AFB1-altered genes, selected upon basis of their function or tumor suppressor role, was tested in four human hepatocyte populations and in response to other chemicals. Although they exhibited large variable inter-donor fold-changes, several of these genes, particularly FHIT, BCAS3 and SMYD3, were found to be altered by various direct and other indirect genotoxic compounds and unaffected by non-genotoxic compounds. Overall, this comprehensive analysis of early gene expression changes induced by AFB1 in human hepatocytes identified a gene subset that included several genes representing potential biomarkers of genotoxic compounds. -- Highlights: ► Gene expression profile changes induced by aflatoxin B1 in human hepatocytes. ► AFB1 modulates various genes including tumor suppressor genes and proto-oncogenes. ► Important inter-individual variations in the response to AFB1. ► Some genes also altered by other genotoxic compounds requiring or not bioactivation.« less

Ionic-Liquid-Mediated Extraction and Separation Processes for Bioactive Compounds: Past, Present, and Future Trends.

PubMed

Ventura, Sónia P M; E Silva, Francisca A; Quental, Maria V; Mondal, Dibyendu; Freire, Mara G; Coutinho, João A P

2017-05-24

Ionic liquids (ILs) have been proposed as promising media for the extraction and separation of bioactive compounds from the most diverse origins. This critical review offers a compilation on the main results achieved by the use of ionic-liquid-based processes in the extraction and separation/purification of a large range of bioactive compounds (including small organic extractable compounds from biomass, lipids, and other hydrophobic compounds, proteins, amino acids, nucleic acids, and pharmaceuticals). ILs have been studied as solvents, cosolvents, cosurfactants, electrolytes, and adjuvants, as well as used in the creation of IL-supported materials for separation purposes. The IL-based processes hitherto reported, such as IL-based solid-liquid extractions, IL-based liquid-liquid extractions, IL-modified materials, and IL-based crystallization approaches, are here reviewed and compared in terms of extraction and separation performance. The key accomplishments and future challenges to the field are discussed, with particular emphasis on the major lacunas found within the IL community dedicated to separation processes and by suggesting some steps to overcome the current limitations.

Production of Bioactive Secondary Metabolites by Marine Vibrionaceae

PubMed Central

Mansson, Maria; Gram, Lone; Larsen, Thomas O.

2011-01-01

Bacteria belonging to the Vibrionaceae family are widespread in the marine environment. Today, 128 species of vibrios are known. Several of them are infamous for their pathogenicity or symbiotic relationships. Despite their ability to interact with eukaryotes, the vibrios are greatly underexplored for their ability to produce bioactive secondary metabolites and studies have been limited to only a few species. Most of the compounds isolated from vibrios so far are non-ribosomal peptides or hybrids thereof, with examples of N-containing compounds produced independent of nonribosomal peptide synthetases (NRPS). Though covering a limited chemical space, vibrios produce compounds with attractive biological activities, including antibacterial, anticancer, and antivirulence activities. This review highlights some of the most interesting structures from this group of bacteria. Many compounds found in vibrios have also been isolated from other distantly related bacteria. This cosmopolitan occurrence of metabolites indicates a high incidence of horizontal gene transfer, which raises interesting questions concerning the ecological function of some of these molecules. This account underlines the pending potential for exploring new bacterial sources of bioactive compounds and the challenges related to their investigation. PMID:22131950

Ionic-Liquid-Mediated Extraction and Separation Processes for Bioactive Compounds: Past, Present, and Future Trends

PubMed Central

2017-01-01

Ionic liquids (ILs) have been proposed as promising media for the extraction and separation of bioactive compounds from the most diverse origins. This critical review offers a compilation on the main results achieved by the use of ionic-liquid-based processes in the extraction and separation/purification of a large range of bioactive compounds (including small organic extractable compounds from biomass, lipids, and other hydrophobic compounds, proteins, amino acids, nucleic acids, and pharmaceuticals). ILs have been studied as solvents, cosolvents, cosurfactants, electrolytes, and adjuvants, as well as used in the creation of IL-supported materials for separation purposes. The IL-based processes hitherto reported, such as IL-based solid–liquid extractions, IL-based liquid–liquid extractions, IL-modified materials, and IL-based crystallization approaches, are here reviewed and compared in terms of extraction and separation performance. The key accomplishments and future challenges to the field are discussed, with particular emphasis on the major lacunas found within the IL community dedicated to separation processes and by suggesting some steps to overcome the current limitations. PMID:28151648

Targeting activator protein 1 signaling pathway by bioactive natural agents: Possible therapeutic strategy for cancer prevention and intervention.

PubMed

Tewari, Devesh; Nabavi, Seyed Fazel; Nabavi, Seyed Mohammad; Sureda, Antoni; Farooqi, Ammad Ahmad; Atanasov, Atanas G; Vacca, Rosa Anna; Sethi, Gautam; Bishayee, Anupam

2018-02-01

Activator protein 1 (AP-1) is a key transcription factor in the control of several cellular processes responsible for cell survival proliferation and differentiation. Dysfunctional AP-1 expression and activity are involved in several severe diseases, especially inflammatory disorders and cancer. Therefore, targeting AP-1 has recently emerged as an attractive therapeutic strategy for cancer prevention and therapy. This review summarizes our current understanding of AP-1 biology and function as well as explores and discusses several natural bioactive compounds modulating AP-1-associated signaling pathways for cancer prevention and intervention. Current limitations, challenges, and future directions of research are also critically discussed. Copyright © 2017 Elsevier Ltd. All rights reserved.

Bioactive compounds in pindo palm (Butia capitata) juice and in pomace resulting of the extraction process.

PubMed

Jachna, Tiphaine J; Hermes, Vanessa S; Flôres, Simone H; Rios, Alessandro O

2016-03-15

Pindo palm (Butia capitata, Becc. 1916) is a tropical fruit native to South America and is relatively rich in bioactive compounds. It is often consumed as juice. The aim of this study was, first, to identify the degradation of these compounds by pasteurization and by cold storage (4 °C) of pindo palm juice. Physicochemical properties and concentrations of phenolic compounds, carotenoids and vitamin C have been evaluated on fresh and pasteurized juices. Moreover, another objective was to characterize the nutritional composition and the bioactive compounds of pindo palm pomace, the by-product of juice processing. The results demonstrated a degradation of carotenoids with pasteurization and a degradation of vitamin C with both pasteurization and cold storage of juices. Furthermore, the evaluation of pindo palm pomace showed that it is relatively rich in total phenols (20.06 g gallic acid equivalents kg(-1) dry matter) and in β-carotene (0.22 g kg(-1) dry matter). Thus, from the nutrition viewpoint, it does not seem interesting to pasteurize juice. On the other hand, extraction of carotenoids and phenolic compounds from the pomace appears to be a relevant process. © 2015 Society of Chemical Industry.

Synthesis and Biological Evaluation of Thiosemicarbazide Derivatives Endowed with High Activity toward Mycobacterium Bovis.

PubMed

Sardari, Soroush; Feizi, Samaneh; Rezayan, Ali Hossein; Azerang, Parisa; Shahcheragh, Seyyed Mohammad; Ghavami, Ghazaleh; Habibi, Azizollah

2017-01-01

Thiosemicarbazides are potent intermediates for the synthesis of pharmaceutical and bioactive materials and thus, they are used extensively in the field of medicinal chemistry. The imine bond (-N=CH-) in this compounds are useful in organic synthesis, in particular for the preparation of heterocycles and non-natural β-aminoacids. In this paper the synthesis of some new thiosemicarbazide derivatives by condensation reaction of various aldehydes or ketones with 4-phenylthiosemicarbazide or thiosemicarbazide is reported. This synthesis method has the advantages of high yields and good bioactivity. The structures of these compounds were confirmed by IR, mass, 1 H NMR, 13 C NMR, and single-crystal X-ray diffraction studies. All of these compounds were tested for their in-vitro anti-mycobacterial activity. The influence of the functional group and position of substituent on anti-bacterial activity of compounds is investigated too. The preliminary results indicated that all of the tested compounds showed good activity against the test organism. The compounds 11 and 30 showed the highest anti-tubercular activity (0.39 μg/mL). This synthesis method has the advantages of high yields and good bioactivity.

Chemical genomics: characterizing target pathways for bioactive compounds using the endomembrane trafficking network.

PubMed

Rodriguez-Furlán, Cecilia; Hicks, Glenn R; Norambuena, Lorena

2014-01-01

The plant endomembrane trafficking system is a highly complex set of processes. This complexity presents a challenge for its study. Classical plant genetics often struggles with loss-of-function lethality and gene redundancy. Chemical genomics allows overcoming many of these issues by using small molecules of natural or synthetic origin to inhibit specific trafficking proteins thereby affecting the processes in a tunable and reversible manner. Bioactive chemicals identified by high-throughput phenotype screens must be characterized in detail starting with understanding of the specific trafficking pathways affected. Here, we describe approaches to characterize bioactive compounds that perturb vesicle trafficking. This should equip researchers with practical knowledge on how to identify endomembrane-specific trafficking pathways that may be perturbed by specific compounds and will help to eventually identify molecular targets for these small molecules.

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.

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

Seaweed Bioactive Compounds against Pathogens and Microalgae: Potential Uses on Pharmacology and Harmful Algae Bloom Control.

PubMed

Zerrifi, Soukaina El Amrani; El Khalloufi, Fatima; Oudra, Brahim; Vasconcelos, Vitor

2018-02-09

Cyanobacteria are found globally due to their adaptation to various environments. The occurrence of cyanobacterial blooms is not a new phenomenon. The bloom-forming and toxin-producing species have been a persistent nuisance all over the world over the last decades. Evidence suggests that this trend might be attributed to a complex interplay of direct and indirect anthropogenic influences. To control cyanobacterial blooms, various strategies, including physical, chemical, and biological methods have been proposed. Nevertheless, the use of those strategies is usually not effective. The isolation of natural compounds from many aquatic and terrestrial plants and seaweeds has become an alternative approach for controlling harmful algae in aquatic systems. Seaweeds have received attention from scientists because of their bioactive compounds with antibacterial, antifungal, anti-microalgae, and antioxidant properties. The undesirable effects of cyanobacteria proliferations and potential control methods are here reviewed, focusing on the use of potent bioactive compounds, isolated from seaweeds, against microalgae and cyanobacteria growth.

Antioxidant activity, total phenolics and flavonoids contents: Should we ban in vitro screening methods?

PubMed

Granato, Daniel; Shahidi, Fereidoon; Wrolstad, Ronald; Kilmartin, Paul; Melton, Laurence D; Hidalgo, Francisco J; Miyashita, Kazuo; Camp, John van; Alasalvar, Cesarettin; Ismail, Amin B; Elmore, Stephen; Birch, Gordon G; Charalampopoulos, Dimitris; Astley, Sian B; Pegg, Ronald; Zhou, Peng; Finglas, Paul

2018-10-30

As many studies are exploring the association between ingestion of bioactive compounds and decreased risk of non-communicable diseases, the scientific community continues to show considerable interest in these compounds. In addition, as many non-nutrients with putative health benefits are reducing agents, hydrogen donors, singlet oxygen quenchers or metal chelators, measurement of antioxidant activity using in vitro assays has become very popular over recent decades. Measuring concentrations of total phenolics, flavonoids, and other compound (sub)classes using UV/Vis spectrophotometry offers a rapid chemical index, but chromatographic techniques are necessary to establish structure-activity. For bioactive purposes, in vivo models are required or, at the very least, methods that employ distinct mechanisms of action (i.e., single electron transfer, transition metal chelating ability, and hydrogen atom transfer). In this regard, better understanding and application of in vitro screening methods should help design of future research studies on 'bioactive compounds'. Copyright © 2018 Elsevier Ltd. All rights reserved.

Seaweed Bioactive Compounds against Pathogens and Microalgae: Potential Uses on Pharmacology and Harmful Algae Bloom Control

PubMed Central

Zerrifi, Soukaina El Amrani; El Khalloufi, Fatima; Oudra, Brahim; Vasconcelos, Vitor

2018-01-01

Cyanobacteria are found globally due to their adaptation to various environments. The occurrence of cyanobacterial blooms is not a new phenomenon. The bloom-forming and toxin-producing species have been a persistent nuisance all over the world over the last decades. Evidence suggests that this trend might be attributed to a complex interplay of direct and indirect anthropogenic influences. To control cyanobacterial blooms, various strategies, including physical, chemical, and biological methods have been proposed. Nevertheless, the use of those strategies is usually not effective. The isolation of natural compounds from many aquatic and terrestrial plants and seaweeds has become an alternative approach for controlling harmful algae in aquatic systems. Seaweeds have received attention from scientists because of their bioactive compounds with antibacterial, antifungal, anti-microalgae, and antioxidant properties. The undesirable effects of cyanobacteria proliferations and potential control methods are here reviewed, focusing on the use of potent bioactive compounds, isolated from seaweeds, against microalgae and cyanobacteria growth. PMID:29425153

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.

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.

Characterization of bioactive peptides obtained from marine invertebrates.

PubMed

Lee, Jung Kwon; Jeon, Joong-Kyun; Kim, Se-Kwon; Byun, Hee-Guk

2012-01-01

Bioactive peptides as products of hydrolysis of diverse marine invertebrate (shellfish, crustacean, rotifer, etc.) proteins are the focus of current research. After much research on these muscles and by-products, some biologically active peptides were identified and applied to useful compounds for human utilization. This chapter reviews bioactive peptides from marine invertebrates in regarding to their bioactivities. Additionally, specific characteristics of antihypertensive, anti-Alzheimer, antioxidant, antimicrobial peptide enzymatic production, methods to evaluate bioactivity capacity, bioavailability, and safety concerns of peptides are reviewed. Copyright © 2012 Elsevier Inc. All rights reserved.

Bioactivation of particles

DOEpatents

Pinaud, Fabien [Berkeley, CA; King, David [San Francisco, CA; Weiss, Shimon [Los Angeles, CA

2011-08-16

Particles are bioactivated by attaching bioactivation peptides to the particle surface. The bioactivation peptides are peptide-based compounds that impart one or more biologically important functions to the particles. Each bioactivation peptide includes a molecular or surface recognition part that binds with the surface of the particle and one or more functional parts. The surface recognition part includes an amino-end and a carboxy-end and is composed of one or more hydrophobic spacers and one or more binding clusters. The functional part(s) is attached to the surface recognition part at the amino-end and/or said carboxy-end.

Hybrid gels by conjugation of hyaluronic acid with poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro (5.5)undecane) copolymers.

PubMed

Chiriac, Aurica P; Nita, Loredana Elena; Diaconu, Alina; Bercea, Maria; Tudorachi, Nita; Pamfil, Daniela; Mititelu-Tartau, Liliana

2017-05-01

The approach of covalent conjugation for coupling synthetic polymers with biomolecules represents an appealing strategy to produce new compounds with distinctive properties for biomedical applications. In the present study we generated hybrid gels with tunable characteristics by using hyaluronic acid (HA) and four variants of poly(itaconic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro[5.5] undecane) (PITAU) copolymers, differing through the molar ratios between comonomers. The new bioconjugate compounds were realized by using a ″grafting to″ strategy, for further ensuring new ways for coupling of various bioactive compounds, taking into account that the grafted copolymers are dual sensitive to pH and temperature. The procedure of chemical crosslinking, by opening the anhydride cycle of the copolymer with the hydroxyl groups of hyaluronic acid, was used to prepare the bioconjugates. The chemical conjugation between HA and PITAU copolymers, as well as the structure of the new compounds, was confirmed by FTIR and NMR techniques. The physical properties of the new gels as thermal stability, swelling capacity, and rheological properties were investigated. The bioconjugate networks were also investigated as drug delivery carriers by using indomethacin as a model drug. In vitro and in vivo tests attested the homogeneity of the bioactive compounds as well as a good biochemical response, showing good biocompatibility for the new structures. Copyright © 2017 Elsevier B.V. All rights reserved.

Enhanced and green extraction polyphenols and furanocoumarins from Fig (Ficus carica L.) leaves using deep eutectic solvents.

PubMed

Wang, Tong; Jiao, Jiao; Gai, Qing-Yan; Wang, Peng; Guo, Na; Niu, Li-Li; Fu, Yu-Jie

2017-10-25

Nowadays, green extraction of bioactive compounds from medicinal plants has gained increasing attention. As green solvent, deep eutectic solvent (DES) have been highly rated to replace toxic organic solvents in extraction process. In present study, to simultaneous extraction five main bioactive compounds from fig leaves, DES was tailor-made. The tailor-made DES composed of a 3:3:3 molar ratio of glycerol, xylitol and D-(-)-Fructose showed enhanced extraction yields for five target compounds simultaneously compared with traditional methanol and non-tailor DESs. Then, the tailor-made DES based extraction methods have compared and microwave-assisted extraction was selected and optimized due to its high extraction yields with lower time consumption. The influencing parameters including extraction temperature, liquid-solid ratio, and extraction time were optimized using response surface methodology (RSM). Under optimal conditions the extraction yield of caffeoylmalic acid, psoralic acid-glucoside, rutin, psoralen and bergapten was 6.482mg/g, 16.34mg/g, 5.207mg/g, 15.22mg/g and 2.475mg/g, respectively. Macroporous resin D101 has been used to recovery target compounds with recovery yields of 79.2%, 83.4%, 85.5%, 81.2% and 75.3% for caffeoylmalic acid, psoralic acid-glucoside, rutin, psoralen and bergapten, respectively. The present study suggests that DESs are truly designer and efficient solvents and the method we developed was efficient and sustainable for extraction main compounds from Fig leaves.mg/g. Copyright © 2017 Elsevier B.V. All rights reserved.

Physiological role of phenolic biostimulants isolated from brown seaweed Ecklonia maxima on plant growth and development.

PubMed

Aremu, Adeyemi O; Masondo, Nqobile A; Rengasamy, Kannan R R; Amoo, Stephen O; Gruz, Jiří; Bíba, Ondřej; Šubrtová, Michaela; Pěnčík, Aleš; Novák, Ondřej; Doležal, Karel; Van Staden, Johannes

2015-06-01

Eckol, a major phenolic compound isolated from brown seaweed significantly enhanced the bulb size and bioactive compounds in greenhouse-grown Eucomis autumnalis. We investigated the effect of eckol and phloroglucinol (PG) (phenolic compounds) isolated from the brown seaweed, Ecklonia maxima (Osbeck) Papenfuss on the growth, phytochemical and auxin content in Eucomis autumnalis (Mill.) Chitt. The model plant is a popular medicinal species with increasing conservation concern. Eckol and PG were tested at 10(-5), 10(-6) and 10(-7) M using soil drench applications. After 4 months, growth parameters, phytochemical and auxin content were recorded. When compared to the control, eckol (10(-6) M) significantly improved bulb size, fresh weight and root production while the application of PG (10(-6) M) significantly increased the bulb numbers. However, both compounds had no significant stimulatory effect on aerial organs. Bioactive phytochemicals such as p-hydroxybenzoic and ferulic acids were significantly increased in eckol (10(-5) M) and PG (10(-6) M) treatments, compared to the control. Aerial (1,357 pmol/g DW) and underground (1,474 pmol/g DW) parts of eckol-treated (10(-5) M) plants yielded the highest concentration of indole-3-acetic acid. Overall, eckol and PG elicited a significant influence on the growth and physiological response in E. autumnalis. Considering the medicinal importance of E. autumnalis and the increasing strains on its wild populations, these compounds are potential tools to enhance their cultivation and growth.

Bioactive Compounds of Kimchi Inhibit Apoptosis by Attenuating Endoplasmic Reticulum Stress in the Brain of Amyloid β-Injected Mice.

PubMed

Woo, Minji; Noh, Jeong Sook; Cho, Eun Ju; Song, Yeong Ok

2018-05-16

This study investigated the inhibitory effects of kimchi bioactive compounds against endoplasmic reticulum (ER) stress-induced apoptosis in amyloid beta (Aβ)-injected mice. Mice received a single intracerebroventricular injection of Aβ 25-35 , except for the normal group. Mice were subjected to oral administration of 10 mg of capsaicin, 50 mg of 3-(4'-hydroxyl-3',5'-dimethoxyphenyl)propionic acid (HDMPPA), 50 mg of quercetin, 50 mg of ascorbic acid, or 200 mg of kimchi methanol extract (KME) per kilogram of body weight for 2 weeks ( n = 7 per group). In the in vitro blood-brain barrier (BBB) permeability test, all bioactive compounds penetrated the BBB except ascorbic acid. The protein expression level of APP, BACE, and p-Tau elevated by Aβ injection was decreased by kimchi bioactive compounds ( P < 0.05). Quercetin, HDMPPA, and KME decreased oxidative stress, as indicated by ROS and TBARS levels ( P < 0.05). The protein expression level of ER stress markers GRP78, p-PERK, p-eIF2α, XBP1, and CHOP and the proapoptotic molecules Bax, p-JNK, and cleaved caspases-3 and -9 decreased ( P < 0.05). In contrast, the protein expression level of antiapoptotic molecules Bcl2 and cIAP increased ( P < 0.05). These results were supported by histological analysis.

Bioactive properties and potentials cosmeceutical applications of phlorotannins isolated from brown seaweeds: A review.

PubMed

Sanjeewa, Kalu Kapuge Asanka; Kim, Eun-A; Son, Kwang-Tae; Jeon, You-Jin

2016-09-01

Currently, natural ingredients are becoming more attractive for the industries such as functional food, nutraceuticals, cosmeceutical and pharmaceutical industries as people starting to believe naturally occurring compounds are safer to humans than artificial compounds. Seaweeds are one of the most interesting organisms found in oceans around the earth, which are carrying great ecological importance and contribute to increase the biodiversity of ecosystems where they were originated and habitat. Within last few decades, discovery of secondary metabolites with biological activities from seaweeds has been significantly increased. Further, the unique secondary metabolites isolated from seaweeds including polysaccharides, carotenoids and polyphenols possess range of bioactive properties that make them potential ingredient for many industrial applications. Among those groups of compounds phlorotannins isolated from brown seaweeds have shown interesting bioactive properties including anti-cancer, anti-inflammation, anti-oxidant, anti-allergic, anti-wrinkling and hair growth promotion properties. Moreover, these properties associated with phlorotannins make them an ideal compounds to use as a functional ingredient in cosmeceutical products. Up to now no report has been reviewed about discuss properties of phlorotannins related to the cosmeceutical application. In the present review primary attention is given to the collect scientific data published about bioactive properties of brown algal phlorotannins related to the cosmeceutical industry. Copyright © 2016 Elsevier B.V. All rights reserved.

Variation of antioxidant activity and the levels of bioactive compounds in lipophilic and hydrophilic extracts from hot pepper (Capsicum spp.) cultivars.

PubMed

Bae, Haejin; Jayaprakasha, G K; Jifon, John; Patil, Bhimanagouda S

2012-10-15

Peppers (Capsicum spp.) are a rich source of diverse bioactive compounds with potential health-promoting properties. This study investigated the extraction efficiency of five solvents on antioxidant activities from cayenne (CA408 and Mesilla), jalapeño (Ixtapa) and serrano (Tuxtlas) pepper cultivars. Freeze-dried peppers were extracted using a Soxhlet extractor with five solvents: hexane, ethyl acetate, acetone, methanol, and methanol:water (80:20). The levels of specific bioactive compounds (phenolics, capsaicinoids, carotenoids and flavonoids) were determined by HPLC and antioxidant activities were assayed by three methods. For all pepper cultivars tested, hexane extracts had the highest levels of capsaicinoids and carotenoids, but methanol extracts had the maximum levels of flavonoids. Hexane extracts showed higher 2,2-diphenyl-1-pricrylhydrozyl (DPPH) radical-scavenging activity and higher reducing power, and acetone extracts (from Mesilla pepper) had a high reducing power. All pepper extracts, except hexane, were effective in preventing deoxyribose degradation, and the inhibition was increased by high concentrations of extracts. The results of the present study indicated that, among the different measures of antioxidant activity, DPPH radical-scavenging activity was strongly correlated with total bioactive compounds (capsaicinoids, carotenoids, flavonoids and total phenolics) in pepper cultivars. Copyright © 2012 Elsevier Ltd. All rights reserved.

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

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.

Bioprospecting Red Sea Coastal Ecosystems for Culturable Microorganisms and Their Antimicrobial Potential.

PubMed

Al-Amoudi, Soha; Essack, Magbubah; Simões, Marta F; Bougouffa, Salim; Soloviev, Irina; Archer, John A C; Lafi, Feras F; Bajic, Vladimir B

2016-09-10

Microorganisms that inhabit unchartered unique soil such as in the highly saline and hot Red Sea lagoons on the Saudi Arabian coastline, represent untapped sources of potentially new bioactive compounds. In this study, a culture-dependent approach was applied to three types of sediments: mangrove mud (MN), microbial mat (MM), and barren soil (BS), collected from Rabigh harbor lagoon (RHL) and Al-Kharrar lagoon (AKL). The isolated bacteria were evaluated for their potential to produce bioactive compounds. The phylogenetic characterization of 251 bacterial isolates based on the 16S rRNA gene sequencing, supported their assignment to five different phyla: Proteobacteria, Firmicutes, Actinobacteria, Bacteroidetes, and Planctomycetes. Fifteen putative novel species were identified based on a 16S rRNA gene sequence similarity to other strain sequences in the NCBI database, being ≤98%. We demonstrate that 49 of the 251 isolates exhibit the potential to produce antimicrobial compounds. Additionally, at least one type of biosynthetic gene sequence, responsible for the synthesis of secondary metabolites, was recovered from 25 of the 49 isolates. Moreover, 10 of the isolates had a growth inhibition effect towards Staphylococcus aureus, Salmonella typhimurium and Pseudomonas syringae. We report the previously unknown antimicrobial activity of B. borstelensis, P. dendritiformis and M. salipaludis against all three indicator pathogens. Our study demonstrates the evidence of diverse cultured microbes associated with the Red Sea harbor/lagoon environments and their potential to produce antimicrobial compounds.

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.

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

Bioalerts: a python library for the derivation of structural alerts from bioactivity and toxicity data sets.

PubMed

Cortes-Ciriano, Isidro

2016-01-01

Assessing compound toxicity at early stages of the drug discovery process is a crucial task to dismiss drug candidates likely to fail in clinical trials. Screening drug candidates against structural alerts, i.e. chemical fragments associated to a toxicological response prior or after being metabolized (bioactivation), has proved a valuable approach for this task. During the last decades, diverse algorithms have been proposed for the automatic derivation of structural alerts from categorical toxicity data sets. Here, the python library bioalerts is presented, which comprises functionalities for the automatic derivation of structural alerts from categorical (dichotomous), e.g. toxic/non-toxic, and continuous bioactivity data sets, e.g. [Formula: see text] or [Formula: see text] values. The library bioalerts relies on the RDKit implementation of the circular Morgan fingerprint algorithm to compute chemical substructures, which are derived by considering radial atom neighbourhoods of increasing bond radius. In addition to the derivation of structural alerts, bioalerts provides functionalities for the calculation of unhashed (keyed) Morgan fingerprints, which can be used in predictive bioactivity modelling with the advantage of allowing for a chemically meaningful deconvolution of the chemical space. Finally, bioalerts provides functionalities for the easy visualization of the derived structural alerts.

Endophytic Paraconiothyrium sp. from Zingiber officinale Rosc. Displays Broad-Spectrum Antimicrobial Activity by Production of Danthron.

PubMed

Anisha, C; Sachidanandan, P; Radhakrishnan, E K

2018-03-01

The bioactivity spectrum of fungal endophytes isolated from Zingiber officinale was analyzed against clinical pathogens and against the phytopathogen Pythium myriotylum, which causes Pythium rot in ginger. One of the isolates GFM13 showed broad bioactivity against various pathogens tested including P. myriotylum. The spore suspension as well as the culture filtrate of the endophytic fungal isolate was found to effectively protect ginger rhizomes from Pythium rot. By molecular identification, the fungal endophyte was identified as Paraconiothyrium sp. The bioactive compound produced by the isolate was separated by bioactivity-guided fractionation and was identified by GC-MS as danthron, an anthraquinone derivative. PCR amplification showed the presence of non-reducing polyketide synthase gene (NR-PKS) in the endophyte GFM13, which is reported to be responsible for the synthesis of anthraquinones in fungi. This is the first report of danthron being produced as the biologically active component of Paraconiothyrium sp. Danthron is reported to have wide pharmaceutical and agronomic applications which include its use as a fungicide in agriculture. The broad-spectrum antimicrobial activity of danthron and the endophytic origin of Paraconiothyrium sp. offer immense applications of the study.

Bioactive components from the heartwood of Pterocarpus santalinus.

PubMed

Wu, Shou-Fang; Hwang, Tsong-Long; Chen, Shu-Li; Wu, Chin-Chung; Ohkoshi, Emika; Lee, Kuo-Hsiung; Chang, Fang-Rong; Wu, Yang-Chang

2011-09-15

One new phenanthrenedione, pterolinus K (1), and one new chalcone, pterolinus L (2) were isolated from the heartwood extract of Pterocarpus santalinus. The structures were elucidated by spectroscopic methods. Both 1 and 2 showed inhibitory effect on elastase release by human neutrophils in response to fMLP with an IC(50) value of 4.24 and 0.95 μM, and compound 1 also inhibited superoxide anion generation with IC(50) value of 0.99 μM. In addition, compound 1 showed selective cytotoxicity against HepG2 with IC(50) value of 10.86 μM, while compound 2 showed a moderate cytotoxicity against KB with IC(50) values of 17.18 μM. Copyright © 2011 Elsevier Ltd. All rights reserved.

Identification and evaluation of magnolol and chrysophanol as the principle protein tyrosine phosphatase-1B inhibitory compounds in a Kampo medicine, Masiningan.

PubMed

Onoda, Toshihisa; Li, Wei; Sasaki, Tatsunori; Miyake, Megumi; Higai, Koji; Koike, Kazuo

2016-06-20

Masiningan is a traditional medicine consisting of six crude drugs that have been used for treating constipation and diabetes mellitus in both Japan and China. Masiningan has been reported to have significant PTP1B inhibitory activity and to affect cells in the insulin-signaling pathway. The aim of the present study is to identify the PTP1B inhibitory compounds in Masiningan. Bioactivity peaks were identified by analytical HPLC profiling and PTP1B inhibitory activity profiling of sub-fractions from Masiningan extract. The bioactive compounds were isolated by tracking two identified bioactive peaks, and the chemical structures were determined by spectroscopic analyses. The bioactive compounds were further investigated for their inhibitory effect against PTP1B by enzymatic kinetic analysis, molecular docking simulation, inhibitory selectivity against other PTPs, and cellular activity in the insulin signal transduction pathway. From Masiningan, magnolol (1) and chrysophanol (2) were isolated as compounds that exhibited significant dose-dependent inhibitory activities against PTP1B, with IC50 values of 24.6 and 12.3μM, respectively. Kinetic analysis revealed that 1 is a non-competitive and that 2 is a competitive PTP1B inhibitor. In the molecular docking simulation, compound 2 was stably positioned in the active pocket of PTP1B, and the CDOCKER energy was calculated to be 24.3411kcal/mol. Both compounds demonstrated remarkably high selectivity against four PTPs and revealed cellular activity against the insulin signal transduction pathway. Magnolol (1) and chrysophanol (2) were identified as the principle PTP1B inhibitory active compounds in Masiningan, and their actions were investigated in detail. These findings demonstrated the effectiveness of Masiningan on diabetes mellitus through the inhibition of PTP1B at a molecular level as well as the potential of magnolol (1) and chrysophanol (2) as lead compounds in future anti-diabetes drug development. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

Femtosecond Laser Microfabrication of an Integrated Device for Optical Release and Sensing of Bioactive Compounds.

PubMed

Ghezzi, Diego; Vazquez, Rebeca Martinez; Osellame, Roberto; Valtorta, Flavia; Pedrocchi, Alessandra; Valle, Giuseppe Della; Ramponi, Roberta; Ferrigno, Giancarlo; Cerullo, Giulio

2008-10-23

Flash photolysis of caged compounds is one of the most powerful approaches to investigate the dynamic response of living cells. Monolithically integrated devices suitable for optical uncaging are in great demand since they greatly simplify the experiments and allow their automation. Here we demonstrate the fabrication of an integrated bio-photonic device for the optical release of caged compounds. Such a device is fabricated using femtosecond laser micromachining of a glass substrate. More in detail, femtosecond lasers are used both to cut the substrate in order to create a pit for cell growth and to inscribe optical waveguides for spatially selective uncaging of the compounds present in the culture medium. The operation of this monolithic bio-photonic device is tested using both free and caged fluorescent compounds to probe its capability of multipoint release and optical sensing. Application of this device to the study of neuronal network activity can be envisaged.

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.

Isolation, Purification, and Characterization of Five Active Diketopiperazine Derivatives from Endophytic Streptomyces SUK 25 with Antimicrobial and Cytotoxic Activities.

PubMed

Alshaibani, Muhanna; Zin, Noraziah; Jalil, Juriyati; Sidik, Nik; Ahmad, Siti Junaidah; Kamal, Nurkhalida; Edrada-Ebel, Ruangelie

2017-07-28

In our search for new sources of bioactive secondary metabolites from Streptomyces sp., the ethyl acetate extracts from endophytic Streptomyces SUK 25 afforded five active diketopiperazine (DKP) compounds. The aim of this study was to characterize the bioactive compounds isolated from endophytic Streptomyces SUK 25 and evaluate their bioactivity against multiple drug resistance (MDR) bacteria such as Enterococcus raffinosus, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanii, Pseudomonas aeruginosa, and Enterobacter spp., and their cytotoxic activities against the human hepatoma (HepaRG) cell line. The production of secondary metabolites by this strain was optimized through Thornton's medium. Isolation, purification, and identification of the bioactive compounds were carried out using high-performance liquid chromatography, high-resolution mass liquid chromatography-mass spectrometry, Fourier transform infrared spectroscopy, and nuclear magnetic resonance, and cryopreserved HepaRG cells were selected to test the cytotoxicity. The results showed that endophytic Streptomyces SUK 25 produces four active DKP compounds and an acetamide derivative, which were elucidated as cyclo -( L -Val- L -Pro), cyclo -( L -Leu- L -Pro), cyclo -( L -Phe- L -Pro), cyclo -( L -Val- L -Phe), and N -(7-hydroxy-6-methyl-octyl)-acetamide. These active compounds exhibited activity against methicillin-resistant S. aureus ATCC 43300 and Enterococcus raffinosus , with low toxicity against human hepatoma HepaRG cells. Endophytic Streptomyces SUK 25 has the ability to produce DKP derivatives biologically active against some MDR bacteria with relatively low toxicity against HepaRG cells line.

Conventional and unconventional extraction methods applied to the plant, Thymus serpyllum L

NASA Astrophysics Data System (ADS)

Đukić, D.; Mašković, P.; Vesković Moračanin, S.; Kurćubić, V.; Milijašević, M.; Babić, J.

2017-09-01

This study deals with the application of two conventional and three non-conventional extraction approaches for isolation of bioactive compounds from the plant Thymus serpyllum L. The extracts obtained were tested regarding their chemical profile (content of phenolics, flavonoids, condensed tannins, gallotannins and anthocyanins) and antioxidant activities. Subcritical water extract of Thymus serpyllum L. generally had the highest concentrations of the chemical bioactive compounds examined and the best antioxidant properties.

Chiral Alkyl Halides: Underexplored Motifs in Medicine

PubMed Central

Gál, Bálint; Bucher, Cyril; Burns, Noah Z.

2016-01-01

While alkyl halides are valuable intermediates in synthetic organic chemistry, their use as bioactive motifs in drug discovery and medicinal chemistry is rare in comparison. This is likely attributable to the common misconception that these compounds are merely non-specific alkylators in biological systems. A number of chlorinated compounds in the pharmaceutical and food industries, as well as a growing number of halogenated marine natural products showing unique bioactivity, illustrate the role that chiral alkyl halides can play in drug discovery. Through a series of case studies, we demonstrate in this review that these motifs can indeed be stable under physiological conditions, and that halogenation can enhance bioactivity through both steric and electronic effects. Our hope is that, by placing such compounds in the minds of the chemical community, they may gain more traction in drug discovery and inspire more synthetic chemists to develop methods for selective halogenation. PMID:27827902

Effect of post-harvest treatment on bioactive phytochemicals of Thai black rice.

PubMed

Norkaew, Orranuch; Boontakham, Pittayaporn; Dumri, Kanchana; Noenplab, Acharaporn Na Lampang; Sookwong, Phumon; Mahatheeranont, Sugunya

2017-02-15

Because black rice is rich in antioxidants, appropriate methods of post-harvest treatment are necessary for maintaining these bioactive phytochemicals. Drying methods, storage temperatures, storage duration, and packaging methods affected the contents of some bioactive compounds in the two varieties of Thai black rice used in this research. Sun drying reduces the loss of anthocyanins and γ-oryzanols more than does hot air drying. Glutinous black rice stored as paddy at cool room temperature retains more anthocyanins, γ-oryzanols, and vitamin E than does paddy stored at room temperature. Nylon/LLDPE pouches containing N2 are the most suitable packaging for preserving the key aroma compound 2-acetyl-1-pyrroline (2AP), total phenolic, and anthocyanin contents of unpolished aromatic black rice. These pouches also retard the formation of some common off-flavor compounds. Copyright © 2016 Elsevier Ltd. All rights reserved.

Bioactive compounds synthesized by non-ribosomal peptide synthetases and type-I polyketide synthases discovered through genome-mining and metagenomics.

PubMed

Nikolouli, Katerina; Mossialos, Dimitris

2012-08-01

Non-ribosomal peptide synthetases (NRPS) and type-I polyketide synthases (PKS-I) are multimodular enzymes involved in biosynthesis of oligopeptide and polyketide secondary metabolites produced by microorganisms such as bacteria and fungi. New findings regarding the mechanisms underlying NRPS and PKS-I evolution illustrate how microorganisms expand their metabolic potential. During the last decade rapid development of bioinformatics tools as well as improved sequencing and annotation of microbial genomes led to discovery of novel bioactive compounds synthesized by NRPS and PKS-I through genome-mining. Taking advantage of these technological developments metagenomics is a fast growing research field which directly studies microbial genomes or specific gene groups and their products. Discovery of novel bioactive compounds synthesized by NRPS and PKS-I will certainly be accelerated through metagenomics, allowing the exploitation of so far untapped microbial resources in biotechnology and medicine.

Nano-encapsulations liberated from barley protein microparticles for oral delivery of bioactive compounds.

PubMed

Wang, Ruoxi; Tian, Zhigang; Chen, Lingyun

2011-03-15

Novel microparticles (3-5 μm) were created by pre-emulsifying barley proteins with a homogenizer followed a microfluidizer system. These microparticles exhibited a high oil carrying capacity (encapsulation efficiency, 93-97%; loading efficiency, 46-49%). Microparticle degradation and bioactive compound release behaviours were studied in the simulated gastro-intestinal (GI) tract. The data revealed that nano-encapsulations (20-30 nm) were formed as a result of enzymatic degradation of barley protein microparticle bulk matrix in the simulated gastric tract. These nano-encapsulations delivered β-carotene to a simulated human intestinal tract intact, where they were degraded by pancreatic enzymes and steadily released the β-carotene. These uniquely structured microparticles may provide a new strategy for the nutraceutical and pharmaceutical industries to develop targeted delivery systems for lipophilic bioactive compounds. Copyright © 2011 Elsevier B.V. All rights reserved.

Cocoa Shell: A By-Product with Great Potential for Wide Application.

PubMed

Panak Balentić, Jelena; Ačkar, Đurđica; Jokić, Stela; Jozinović, Antun; Babić, Jurislav; Miličević, Borislav; Šubarić, Drago; Pavlović, Nika

2018-06-09

Solving the problem of large quantities of organic waste, which represents an enormous ecological and financial burden for all aspects of the process industry, is a necessity. Therefore, there is an emerged need to find specific solutions to utilize raw materials as efficiently as possible in the production process. The cocoa shell is a valuable by-product obtained from the chocolate industry. It is rich in protein, dietary fiber, and ash, as well as in some other valuable bioactive compounds, such as methylxanthines and phenolics. This paper gives an overview of published results related to the cocoa shell, mostly on important bioactive compounds and possible applications of the cocoa shell in different areas. The cocoa shell, due to its nutritional value and high-value bioactive compounds, could become a desirable raw material in a large spectrum of functional, pharmaceutical, or cosmetic products, as well as in the production of energy or biofuels in the near future.

Improvement of Nutritional and Bioactive Compound Production by Lion's Mane Medicinal Mushroom, Hericium erinaceus (Agaricomycetes), by Spraying Growth Regulators.

PubMed

Vi, Minhthuan; Yang, Xueqin; Zeng, Xianlu; Chen, Rui'an; Guo, Liqiong; Lin, Junfang; He, Qianyun; Zheng, Qianwang; Wei, Tao

2018-01-01

Hericium erinaceus is a popular culinary and medicinal mushroom in China because of its broad beneficial effects. In this study we evaluated the effects of stimulation with 7 growth regulators at 5 different concentrations on improving the production of nutritional and bioactive compounds by H. erinaceus. Results showed that among all the tested regulators, gibberellic acid (GA) increased protein content (165%), free amino acids (100%), polysaccharides (108%), and polyphenols (26%). Spraying nephthyl acetic acid increased polysaccharides and triterpenoids to 4.37 and 17.27 g/100 g, respectively. Spraying chitosan significantly increased polyphenols by 42%. The addition of triacontanol, indole acetic acid, and 2,4-dichlorophenoxyacetic acid improved the production of proteins, free amino acids, polysaccharides, and polyphenols, but not to the extent that GA did. These results indicate that adding certain growth regulators can effectively improve the production of nutritional and bioactive compounds in H. erinaceus.

Anti-inflammatory and bronchodilatory constituents of leaf extracts of Anacardium occidentale L. in animal models.

PubMed

Awakan, Oluwakemi Josephine; Malomo, Sylvia Omonirume; Adejare, Abdullahi Adeyinka; Igunnu, Adedoyin; Atolani, Olubunmi; Adebayo, Abiodun Humphrey; Owoyele, Bamidele Victor

2018-01-01

Anacardium occidentale L. leaf is useful in the treatment of inflammation and asthma, but the bioactive constituents responsible for these activities have not been characterized. Therefore, this study was aimed at identifying the bioactive constituent(s) of A. occidentale ethanolic leaf extract (AOEL) and its solvent-soluble portions, and evaluating their effects on histamine-induced paw edema and bronchoconstriction. The bronchodilatory effect was determined by measuring the percentage protection provided by plant extracts in the histamine-induced bronchoconstriction model in guinea pigs. The anti-inflammatory effect of the extracts on histamine-induced paw edema in rats was determined by measuring the increase in paw diameter, after which the percent edema inhibition was calculated. The extracts were analyzed using gas chromatography-mass spectrometry to identify the bioactive constituents. Column chromatography and Fourier transform infrared spectroscopy were used respectively to isolate and characterize the constituents. The bronchodilatory and anti-inflammatory activities of the isolated bioactive constituent were evaluated. Histamine induced bronchoconstriction in the guinea pigs and edema in the rat paw. AOEL, hexane-soluble portion of AOEL, ethyl acetate-soluble portion of AOEL, and chloroform-soluble portion of AOEL significantly increased bronchodilatory and anti-inflammatory activities (P < 0.05). Oleamide (9-octadecenamide) was identified as the most abundant compound in the extracts and was isolated. Oleamide significantly increased bronchodilatory and anti-inflammatory activities by 32.97% and 98.41%, respectively (P < 0.05). These results indicate that oleamide is one of the bioactive constituents responsible for the bronchodilatory and anti-inflammatory activity of A. occidentale leaf, and can therefore be employed in the management of bronchoconstriction and inflammation. Copyright © 2017 Shanghai Changhai Hospital. Published by Elsevier B.V. All rights reserved.

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

Enriching screening libraries with bioactive fragment space.

PubMed

Zhang, Na; Zhao, Hongtao

2016-08-01

By deconvoluting 238,073 bioactive molecules in the ChEMBL library into extended Murcko ring systems, we identified a set of 2245 ring systems present in at least 10 molecules. These ring systems belong to 2221 clusters by ECFP4 fingerprints with a minimum intracluster similarity of 0.8. Their overlap with ring systems in commercial libraries was further quantified. Our findings suggest that success of a small fragment library is driven by the convergence of effective coverage of bioactive ring systems (e.g., 10% coverage by 1000 fragments vs. 40% by 2million HTS compounds), high enrichment of bioactive ring systems, and low molecular complexity enhancing the probability of a match with the protein targets. Reconciling with the previous studies, bioactive ring systems are underrepresented in screening libraries. As such, we propose a library of virtual fragments with key functionalities via fragmentation of bioactive molecules. Its utility is exemplified by a prospective application on protein kinase CK2, resulting in the discovery of a series of novel inhibitors with the most potent compound having an IC50 of 0.5μM and a ligand efficiency of 0.41kcal/mol per heavy atom. 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

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

Bioactive Compounds in Functional Meat Products.

PubMed

Pogorzelska-Nowicka, Ewelina; Atanasov, Atanas G; Horbańczuk, Jarosław; Wierzbicka, Agnieszka

2018-01-31

Meat and meat products are a good source of bioactive compounds with positive effect on human health such as vitamins, minerals, peptides or fatty acids. Growing food consumer awareness and intensified global meat producers competition puts pressure on creating new healthier meat products. In order to meet these expectations, producers use supplements with functional properties for animal diet and as direct additives for meat products. In the presented work seven groups of key functional constituents were chosen: (i) fatty acids; (ii) minerals; (iii) vitamins; (iv) plant antioxidants; (v) dietary fibers; (vi) probiotics and (vii) bioactive peptides. Each of them is discussed in term of their impact on human health as well as some quality attributes of the final products.

Two new bioactive monotetrahydrofuran Annonaceous acetogenins from the bark of Xylopia aromatica.

PubMed

Colman-Saizarbitoria, T; Gu, Z M; McLaughlin, J L

1994-12-01

Xylopien [1] and xylomatenin [2], two new bioactive monotetrahydrofuran Annonaceous acetogenins, have been isolated from an EtOH extract of the bark of Xylopia aromatica, using bioactivity-directed fractionation employing lethality to brine shrimp. These new compounds each have a double bond in the hydrocarbon chain and have been identified as C-23, C-24 dehydro analogs of xylopiacin and xylomaticin. Their structures were elucidated by spectral analyses of the parent compounds and/or simple chemical derivatives. Their absolute stereochemistries have been established by 1H- and 2D nmr experiments utilizing the production of Mosher esters. These acetogenins showed cytotoxic potencies superior to adriamycin against three human solid tumor cell lines.

Anticancer Natural Compounds as Epigenetic Modulators of Gene Expression

PubMed Central

Ratovitski, Edward A.

2017-01-01

Abstract: Accumulating evidence shows that hallmarks of cancer include: “genetic and epigenetic alterations leading to inactivation of cancer suppressors, overexpression of oncogenes, deregulation of intracellular signaling cascades, alterations of cancer cell metabolism, failure to undergo cancer cell death, induction of epithelial to mesenchymal transition, invasiveness, metastasis, deregulation of immune response and changes in cancer microenvironment, which underpin cancer development”. Natural compounds as bioactive ingredients isolated from natural sources (plants, fungi, marine life forms) have revolutionized the field of anticancer therapeutics and rapid developments in preclinical studies are encouraging. Natural compounds could affect the epigenetic molecular mechanisms that modulate gene expression, as well as DNA damage and repair mechanisms. The current review will describe the latest achievements in using naturally produced compounds targeting epigenetic regulators and modulators of gene transcription in vitro and in vivo to generate novel anticancer therapeutics. PMID:28367075

Supercritical Carbon Dioxide Extraction of Bioactive Compounds from Ampelopsis grossedentata Stems: Process Optimization and Antioxidant Activity

PubMed Central

Wang, Yuefei; Ying, Le; Sun, Da; Zhang, Shikang; Zhu, Yuejin; Xu, Ping

2011-01-01

Supercritical carbon dioxide (SC-CO2) extraction of bioactive compounds including flavonoids and phenolics from Ampelopsis grossedentata stems was carried out. Extraction parameters such as pressure, temperature, dynamic time and modifier, were optimized using an orthogonal array design of L9 (34), and antioxidant activities of the extracts were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and ferrous ion chelating (FIC) assay. The best conditions obtained for SC-CO2 extraction of flavonoids was 250 bar, 40 °C, 50 min, and with a modifier of methanol/ethanol (1:3, v/v), and that for phenolics extraction was 250 bar, 40 °C, 50 min, and with a modifier of methanol/ethanol (1:1, v/v). Meantime, flavonoids and phenolics were found to be mainly responsible for the DPPH scavenging activity of the extracts, but not for the chelating activity on ferrous ion according to Pearson correlation analysis. Furthermore, several unreported flavonoids such as apigenin, vitexin, luteolin, etc., have been detected in the extracts from A. grossedentata stems. PMID:22072923

Photosynthetic Pigments in Diatoms

PubMed Central

Kuczynska, Paulina; Jemiola-Rzeminska, Malgorzata; Strzalka, Kazimierz

2015-01-01

Photosynthetic pigments are bioactive compounds of great importance for the food, cosmetic, and pharmaceutical industries. They are not only responsible for capturing solar energy to carry out photosynthesis, but also play a role in photoprotective processes and display antioxidant activity, all of which contribute to effective biomass and oxygen production. Diatoms are organisms of a distinct pigment composition, substantially different from that present in plants. Apart from light-harvesting pigments such as chlorophyll a, chlorophyll c, and fucoxanthin, there is a group of photoprotective carotenoids which includes β-carotene and the xanthophylls, diatoxanthin, diadinoxanthin, violaxanthin, antheraxanthin, and zeaxanthin, which are engaged in the xanthophyll cycle. Additionally, some intermediate products of biosynthetic pathways have been identified in diatoms as well as unusual pigments, e.g., marennine. Marine algae have become widely recognized as a source of unique bioactive compounds for potential industrial, pharmaceutical, and medical applications. In this review, we summarize current knowledge on diatom photosynthetic pigments complemented by some new insights regarding their physico-chemical properties, biological role, and biosynthetic pathways, as well as the regulation of pigment level in the cell, methods of purification, and significance in industries. PMID:26389924

Bioactive constituents in pulses and their health benefits.

PubMed

Singh, Balwinder; Singh, Jatinder Pal; Shevkani, Khetan; Singh, Narpinder; Kaur, Amritpal

2017-03-01

Pulses are good sources of bioactive compounds such as polyphenols, phytosterols and non-digestible carbohydrates that play important physiological as well as metabolic roles. These compounds vary in concentration amongst different pulse species and varieties. Pulse seed coats are rich in water-insoluble fibres and polyphenols (having high antioxidant activities), while cotyledons contain higher soluble fibres, oligosaccharides, slowly digestible and resistant starch content. Ferulic acid is the most abundant phenolic acid present in pulses, while flavonol glycosides, anthocyanins and tannins are responsible for the seed coat colour. Sitosterol (most abundant), stigmasterol, and campesterol are the major phytosterols present in pulses. Pulse fibres, resistant starch and oligosaccharides function as probiotics and possess several other health benefits such as anti-inflammatory, anti-tumour, and reduce glucose as well as lipid levels. Beans and peas contain higher amounts of oligosaccharides than other pulses. Processing methods affect resistant starch, polyphenol composition and generally increase antioxidant activities of different pulses. In this review, the current information on pulse polyphenols, phytosterols, resistant starch, dietary fibre, oligosaccharides, antioxidant and associated health benefits are discussed.

Tramesan, a novel polysaccharide from Trametes versicolor. Structural characterization and biological effects

PubMed Central

Sveronis, Aris; Cescutti, Paola; Rizzo, Roberto

2017-01-01

Mushrooms represent a formidable source of bioactive compounds. Some of these may be considered as biological response modifiers; these include compounds with a specific biological function: antibiotics (e.g. plectasin), immune system stimulator (e,g, lentinan), antitumor agents (e.g. krestin, PSK) and hypolipidemic agents (e.g. lovastatin) inter alia. In this study, we focused on the Chinese medicinal mushroom “yun zhi”, Trametes versicolor, traditionally used for (cit.) “replenish essence and qi (vital energy)”. Previous studies indicated the potential activity of extracts from culture filtrate of asexual mycelia of T. versicolor in controlling the growth and secondary metabolism (e.g. mycotoxins) of plant pathogenic fungi. The quest of active principles produced by T. versicolor, allowed us characterising an exo-polysaccharide released in its culture filtrate and naming it Tramesan. Herein we evaluate the biological activity of Tramesan in different organisms: plants, mammals and plant pathogenic fungi. We suggest that the bioactivity of Tramesan relies mostly on its ability to act as pro antioxidant molecule regardless the biological system on which it was applied. PMID:28829786

Tramesan, a novel polysaccharide from Trametes versicolor. Structural characterization and biological effects.

PubMed

Scarpari, Marzia; Reverberi, Massimo; Parroni, Alessia; Scala, Valeria; Fanelli, Corrado; Pietricola, Chiara; Zjalic, Slaven; Maresca, Vittoria; Tafuri, Agostino; Ricciardi, Maria R; Licchetta, Roberto; Mirabilii, Simone; Sveronis, Aris; Cescutti, Paola; Rizzo, Roberto

2017-01-01

Mushrooms represent a formidable source of bioactive compounds. Some of these may be considered as biological response modifiers; these include compounds with a specific biological function: antibiotics (e.g. plectasin), immune system stimulator (e,g, lentinan), antitumor agents (e.g. krestin, PSK) and hypolipidemic agents (e.g. lovastatin) inter alia. In this study, we focused on the Chinese medicinal mushroom "yun zhi", Trametes versicolor, traditionally used for (cit.) "replenish essence and qi (vital energy)". Previous studies indicated the potential activity of extracts from culture filtrate of asexual mycelia of T. versicolor in controlling the growth and secondary metabolism (e.g. mycotoxins) of plant pathogenic fungi. The quest of active principles produced by T. versicolor, allowed us characterising an exo-polysaccharide released in its culture filtrate and naming it Tramesan. Herein we evaluate the biological activity of Tramesan in different organisms: plants, mammals and plant pathogenic fungi. We suggest that the bioactivity of Tramesan relies mostly on its ability to act as pro antioxidant molecule regardless the biological system on which it was applied.

Profiling of red pigment produced by Streptomyces sp. JAR6 and its bioactivity.

PubMed

Abraham, Jayanthi; Chauhan, Ritika

2018-01-01

Actinomycetes strain was isolated from leaf litter soil sample and was identified as Streptomyces sp. by conventional and molecular approaches. The biologically active compound responsible for antimicrobial and anticancer activity of the strain JAR6 was elucidated by solid state fermentation followed by subsequent chromatographic and spectroscopic analysis. Extraction, purification and structural confirmation of red pigment metabolite viz undecylprodigiosin were established on the basis of spectroscopic studies and comparing the data from the literature. The biologically active compound was tested against Gram-positive and Gram-negative clinical isolates and its minimum inhibitory concentration was recorded. The antimicrobial activity of undecylprodigiosin is more prominent against Salmonella sp., Proteus mirabilis , Shigella sp. and Enterococcus sp. whereas, it was less effective against Staphylococcus aureus , Klebsiella pneumonia and Escherichia coli . The anticancer activity of undecylprodigiosin was tested against HeLa cell lines and it exhibited commendable cytotoxicity effect with IC 50 value of 145 µg/ml. The present investigation reveals that undecylprodigiosin produced by Streptomyces strain JAR6 is a potent bioactive metabolite with effective pharmaceutical properties.

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.

Anthocyanin Absorption and Metabolism by Human Intestinal Caco-2 Cells—A Review

PubMed Central

Kamiloglu, Senem; Capanoglu, Esra; Grootaert, Charlotte; Van Camp, John

2015-01-01

Anthocyanins from different plant sources have been shown to possess health beneficial effects against a number of chronic diseases. To obtain any influence in a specific tissue or organ, these bioactive compounds must be bioavailable, i.e., effectively absorbed from the gut into the circulation and transferred to the appropriate location within the body while still maintaining their bioactivity. One of the key factors affecting the bioavailability of anthocyanins is their transport through the gut epithelium. The Caco-2 cell line, a human intestinal epithelial cell model derived from a colon carcinoma, has been proven to be a good alternative to animal studies for predicting intestinal absorption of anthocyanins. Studies investigating anthocyanin absorption by Caco-2 cells report very low absorption of these compounds. However, the bioavailability of anthocyanins may be underestimated since the metabolites formed in the course of digestion could be responsible for the health benefits associated with anthocyanins. In this review, we critically discuss recent findings reported on the anthocyanin absorption and metabolism by human intestinal Caco-2 cells. PMID:26370977

High-performance thin-layer chromatography linked with (bio)assays and mass spectrometry - a suited method for discovery and quantification of bioactive components? Exemplarily shown for turmeric and milk thistle extracts.

PubMed

Taha, Mahmoud N; Krawinkel, Michael B; Morlock, Gertrud E

2015-05-15

Extraction parameters, chemical fingerprint, and the single compounds' activity levels were considered for the selection of active botanicals. For an initial survey, the total bioactivity (i.e., total reducing capacity, total flavonoids contents and free radical scavenging capacity) of 21 aqueous and 21 ethanolic plant extracts was investigated. Ethanolic extracts showed a higher yield and were further analyzed by HPTLC in detail to obtain fingerprints of single flavonoids and further bioactive components. Exemplarily shown for turmeric (Curcuma longa) and milk thistle (Silybum marianum), effect-directed analysis (EDA) was performed using three selected (bio)assays, the Aliivibrio fischeri bioassay, the Bacillus subtilis bioassay and the 2,2-diphenyl-1-picrylhydrazyl (DPPH*) assay. As a proof of principle, the bioactive components found in the extracts were confirmed by HPTLC-MS. Bioassays in combination with planar chromatography directly linked to the known, single effective compounds like curcumin and silibinin. However, also some unknown bioactive components were discovered and exemplarily characterized, which demonstrated the strength of this kind of EDA. HPTLC-UV/Vis/FLD-EDA-MS could become a useful tool for selection of active botanicals and for the activity profiling of the active ingredients therein. The flexibility in effect-directed detections allows a comprehensive survey of effective ingredients in samples. This streamlined methodology comprised a non-targeted, effect-directed screening first, followed by a highly targeted characterization of the discovered bioactive compounds. HPTLC-EDA-MS can also be recommended for bioactivity profiling of food on the food intake side, as not only effective phytochemicals, but also unknown bioactive degradation products during food processing or contamination products or residues or metabolites can be detected. Thus, an efficient survey on potential food intake effects on wellness could be obtained. Having performed both, sum parameter assays and HPTLC analysis, a comparison of both approaches was made and discussed. Copyright © 2015 Elsevier B.V. All rights reserved.

Mutagenic, cytotoxic, and teratogenic effects of 2-acetylaminofluorene and reactive metabolites in vitro.

PubMed

Faustman-Watts, E M; Yang, H Y; Namkung, M J; Greenaway, J C; Fantel, A G; Juchau, M R

1984-01-01

The embryotoxic, mutagenic, and cytotoxic properties of 2-acetylaminofluorene (AAF) and two of its reactive metabolites, N-acetoxy-2-acetylaminofluorene (AAAF) and 2-nitrosofluorene (NF) were assessed in vitro. A combined embryo culture/biotransformation system was used to determine the ability of these compounds to produce embryonic malformations, growth retardation, and/or embryolethality. Salmonella typhimurium auxotrophs (his-) were utilized to measure the mutagenic and cytotoxic potentials of these compounds. The parent compound, AAF, did not produce embryonic malformations or mutagenicity in the absence of an added cytochrome P-450-dependent monooxygenase system. Both metabolites produced each of the measured toxic effects without supplementation of a bioactivation system. However, the three chemicals each elicited a different spectrum of malformations. Bioactivated AAF produced neural tube abnormalities, whereas embryos treated with AAAF primarily exhibited prosencephalic malformations, and NF produced abnormalities of axial rotation or flexure. NF was approximately ten times more potent than AAAF as a direct-acting mutagen but only slightly more active in producing embryonic malformations in vitro. The results indicated that differential effects on the various measured parameters could be produced by these chemicals. The results indicated further that neither NF nor AAAF appeared to be individually responsible for the neural tube abnormalities generated by biotransformed AAF.

Effects of Spray-Drying Parameters on In Vitro Functional Properties of Camu-Camu (Myrciaria dubia Mc. Vaugh): A Typical Amazonian Fruit.

PubMed

Fujita, Alice; Souza, Volnei Brito; Daza, Luis Daniel; Fávaro-Trindade, Carmen Silvia; Granato, Daniel; Genovese, Maria Inés

2017-05-01

Camu-camu (Myrciaria dubia) fruit is a rich source of bioactive compounds but its shelf life is rather short. Therefore, this study was aimed to evaluate the effect of inlet air temperature (T) and concentration (C) of maltodextrin and arabic gum on the spray-drying process of commercial camu-camu pulps (São Paulo and Manaus). Moisture, solubility, total phenolics (TP), ascorbic acid (AA), and proanthocyanidins (PAC) contents, and in vitro antioxidant capacity of the powders (FRAP, DPPH, Folin-Ciocalteu's reducing capacity were measured). Arabic gum resulted in better yields (22% to 30%), powder solubility (84% to 90%), and lower losses of analyzed compounds than the powders manufactured with maltodextrin. Overall, inlet air temperature had a lower impact on the responses studied than the concentration of carrier agents. Polynomial equations were generated for AA (R 2 = 0.993), TP (R 2 = 0.735), PAC (R 2 = 0.946), and for the antioxidant capacity assays (0.867 ≤ R 2  ≤ 0.963). In addition, principal component analysis showed that the lowest concentration of carrier agents (6%) in spray drying resulted in the lowest losses of bioactive compounds and, consequently, the highest antioxidant capacity. © 2017 Institute of Food Technologists®.

Rutin increases critical wavelength of systems containing a single UV filter and with good skin compatibility.

PubMed

Peres, D A; de Oliveira, C A; da Costa, M S; Tokunaga, V K; Mota, J P; Rosado, C; Consiglieri, V O; Kaneko, T M; Velasco, M V R; Baby, A R

2016-08-01

Ultraviolet (UV) radiation is responsible for sunburns, skin cancer, photoaging, and the production of reactive oxygen species (ROS). The awareness on preventing these deleterious effects made the use of anti-UVB formulations an important part of population habits; however, despite the availability of several antioxidants capable of ROS scavenging, the pharmaceutical market lacks products associating UV filters with natural compounds of proven efficacy. Here, we investigated the effect of rutin, a flavonoid with antioxidant activity, associated with UVB filters in dermocosmetic preparations. Formulations were assessed through its antioxidant activity, in vitro photoprotective effectiveness, photostability, and in vivo skin tolerance (hydration, transepidermal water loss, and erythema). Samples containing rutin were compatible with the human skin and presented a pronounced antioxidant potential, with scavenging activity values 75% higher than the ones containing only UVB filters. Although rutin could not prevent the sunscreens photodegradation post-irradiation, the bioactive compound significantly increased the formulations critical wavelengths, showing a photoprotective gain, especially in the UVA range. In conclusion, the absorption in the UVA range, coupled with ROS scavenging potential, proved the positive effect of rutin applied to anti-UVB formulations, making this bioactive compound a promising candidate for photoprotection improvement. © 2015 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

In Vitro Antifungal Activity of Burkholderia gladioli pv. agaricicola against Some Phytopathogenic Fungi

PubMed Central

Elshafie, Hazem S.; Camele, Ippolito; Racioppi, Rocco; Scrano, Laura; Iacobellis, Nicola S.; Bufo, Sabino A.

2012-01-01

The trend to search novel microbial natural biocides has recently been increasing in order to avoid the environmental pollution from use of synthetic pesticides. Among these novel natural biocides are the bioactive secondary metabolites of Burkholderia gladioli pv. agaricicola (Bga). The aim of this study is to determine antifungal activity of Bga strains against some phytopathogenic fungi. The fungicidal tests were carried out using cultures and cell-free culture filtrates against Botrytis cinerea, Aspergillus flavus, Aspergillus niger, Penicillium digitatum, Penicillium expansum, Sclerotinia sclerotiorum and Phytophthora cactorum. Results demonstrated that all tested strains exert antifungal activity against all studied fungi by producing diffusible metabolites which are correlated with their ability to produce extracellular hydrolytic enzymes. All strains significantly reduced the growth of studied fungi and the bacterial cells were more bioactive than bacterial filtrates. All tested Bulkholderia strains produced volatile organic compounds (VOCs), which inhibited the fungal growth and reduced the growth rate of Fusarium oxysporum and Rhizoctonia solani. GC/MS analysis of VOCs emitted by strain Bga 11096 indicated the presence of a compound that was identified as 1-methyl-4-(1-methylethenyl)-cyclohexene, a liquid hydrocarbon classified as cyclic terpene. This compound could be responsible for the antifungal activity, which is also in agreement with the work of other authors. PMID:23208371

Bioactive Compounds from Macroalgae in the New Millennium: Implications for Neurodegenerative Diseases

PubMed Central

Barbosa, Mariana; Valentão, Patrícia; Andrade, Paula B.

2014-01-01

Marine environment has proven to be a rich source of structurally diverse and complex compounds exhibiting numerous interesting biological effects. Macroalgae are currently being explored as novel and sustainable sources of bioactive compounds for both pharmaceutical and nutraceutical applications. Given the increasing prevalence of different forms of dementia, researchers have been focusing their attention on the discovery and development of new compounds from macroalgae for potential application in neuroprotection. Neuroprotection involves multiple and complex mechanisms, which are deeply related. Therefore, compounds exerting neuroprotective effects through different pathways could present viable approaches in the management of neurodegenerative diseases, such as Alzheimer’s and Parkinson’s. In fact, several studies had already provided promising insights into the neuroprotective effects of a series of compounds isolated from different macroalgae species. This review will focus on compounds from macroalgae that exhibit neuroprotective effects and their potential application to treat and/or prevent neurodegenerative diseases. PMID:25257784

Bioactive compounds from macroalgae in the new millennium: implications for neurodegenerative diseases.

PubMed

Barbosa, Mariana; Valentão, Patrícia; Andrade, Paula B

2014-09-25

Marine environment has proven to be a rich source of structurally diverse and complex compounds exhibiting numerous interesting biological effects. Macroalgae are currently being explored as novel and sustainable sources of bioactive compounds for both pharmaceutical and nutraceutical applications. Given the increasing prevalence of different forms of dementia, researchers have been focusing their attention on the discovery and development of new compounds from macroalgae for potential application in neuroprotection. Neuroprotection involves multiple and complex mechanisms, which are deeply related. Therefore, compounds exerting neuroprotective effects through different pathways could present viable approaches in the management of neurodegenerative diseases, such as Alzheimer's and Parkinson's. In fact, several studies had already provided promising insights into the neuroprotective effects of a series of compounds isolated from different macroalgae species. This review will focus on compounds from macroalgae that exhibit neuroprotective effects and their potential application to treat and/or prevent neurodegenerative diseases.

Bioactive compounds isolated from submerged fermentations of the Chilean fungus Stereum rameale.

PubMed

Aqueveque, Pedro; Céspedes, Carlos Leonardo; Becerra, José; Dávila, Marcelo; Sterner, Olov

2015-01-01

Liquid fermentations of the fungus Stereum rameale (N° 2511) yielded extracts with antibacterial activity. The antibacterial activity reached its peak after 216 h of stirring. Bioassay-guided fractionation methods were employed for the isolation of the bioactive metabolites. Three known compounds were identified: MS-3 (1), vibralactone (2) and vibralactone B (3). The three compounds showed antibacterial activity as a function of their concentration. Minimal bactericidal concentrations (MBC) of compound 1 against Gram-positive bacteria were as follows: Bacillus cereus (50 μg/mL), Bacillus subtilis (10 μg/mL) and Staphylococcus aureus (100 μg/mL). Compounds 2 and 3 were active only against Gram-negative bacteria. The MBC of compound 2 against Escherichia coli was 200 μg/mL. Compound 3 inhibited significantly the growth of E. coli and Pseudomonas aeruginosa, with MBC values of 50 and 100 μg/mL, respectively.

Resources and biological activities of natural polyphenols.

PubMed

Li, An-Na; Li, Sha; Zhang, Yu-Jie; Xu, Xiang-Rong; Chen, Yu-Ming; Li, Hua-Bin

2014-12-22

The oxidative stress imposed by reactive oxygen species (ROS) plays an important role in many chronic and degenerative diseases. As an important category of phytochemicals, phenolic compounds universally exist in plants, and have been considered to have high antioxidant ability and free radical scavenging capacity, with the mechanism of inhibiting the enzymes responsible for ROS production and reducing highly oxidized ROS. Therefore, phenolic compounds have attracted increasing attention as potential agents for preventing and treating many oxidative stress-related diseases, such as cardiovascular diseases, cancer, ageing, diabetes mellitus and neurodegenerative diseases. This review summarizes current knowledge of natural polyphenols, including resource, bioactivities, bioavailability and potential toxicity.

Resources and Biological Activities of Natural Polyphenols

PubMed Central

Li, An-Na; Li, Sha; Zhang, Yu-Jie; Xu, Xiang-Rong; Chen, Yu-Ming; Li, Hua-Bin

2014-01-01

The oxidative stress imposed by reactive oxygen species (ROS) plays an important role in many chronic and degenerative diseases. As an important category of phytochemicals, phenolic compounds universally exist in plants, and have been considered to have high antioxidant ability and free radical scavenging capacity, with the mechanism of inhibiting the enzymes responsible for ROS production and reducing highly oxidized ROS. Therefore, phenolic compounds have attracted increasing attention as potential agents for preventing and treating many oxidative stress-related diseases, such as cardiovascular diseases, cancer, ageing, diabetes mellitus and neurodegenerative diseases. This review summarizes current knowledge of natural polyphenols, including resource, bioactivities, bioavailability and potential toxicity. PMID:25533011

Bioassay-guided isolation and identification of bioactive compound from aerial parts of Luffa acutangula against lung cancer cell line NCI-H460.

PubMed

Vanajothi, Ramar; Srinivasan, Pappu

2015-01-01

Luffa acutangula (Cucurbitaceae) is widely used as a traditional medicine in India and was reported to possess various pharmacological activities including its anti-proliferative effects. In this study, the bioactive compound of ethanolic extract of L. acutangula (LA) was isolated using bioassay-guided approach. Five major fractions were collected and evaluated for their anti-proliferative activity against non-small cell lung cancer cells (NCI-H460). Among the test fractions, the fraction LA/FII effectively decreased the growth of cancer cells with IC50 values of 10 µg/ml concentration. Furthermore, it significantly increased intracellular reactive oxygen species and decreased the mitochondrial membrane potential. The apoptogenic activity of fraction LA/FII was confirmed by cell shrinkage, membrane blebbing and formation of apoptotic bodies. A single bioactive compound was isolated from the active faction, LA/FII and subsequently identified as 1,8 dihydroxy-4-methylanthracene 9,10-dione (compound 1) by comparing its spectral data [Ultraviolet (UV), Infrared (IR), Nuclear magnetic resonance (NMR) and Electrospray Ionization-Mass Spectroscopy (ESI-MS)] with literature values. This is the first report on the isolation of compound 1 from this plant.

Oxidative Stress Modulation and ROS-Mediated Toxicity in Cancer: A Review on In Vitro Models for Plant-Derived Compounds.

PubMed

Vallejo, María José; Salazar, Lizeth; Grijalva, Marcelo

2017-01-01

Medicinal and aromatic plants (MAPs) are known and have been long in use for a variety of health and cosmetics applications. Potential pharmacological usages that take advantage of bioactive plant-derived compounds' antimicrobial, antifungal, anti-inflammatory, and antioxidant properties are being developed and many new ones explored. Some phytochemicals could trigger ROS-mediated cytotoxicity and apoptosis in cancer cells. A lot of effort has been put into investigating novel active constituents for cancer therapeutics. While other plant-derived compounds might enhance antioxidant defenses by either radical scavenging or stimulation of intracellular antioxidant enzymes, the generation of reactive oxygen species (ROS) leading to oxidative stress is one of the strategies that may show effective in damaging cancer cells. The biochemical pathways involved in plant-derived bioactive compounds' properties are complex, and in vitro platforms have been useful for a comprehensive understanding of the mechanism of action of these potential anticancer drugs. The present review aims at compiling the findings of particularly interesting studies that use cancer cell line models for assessment of antioxidant and oxidative stress modulation properties of plant-derived bioactive compounds.

An in vitro study of the antimicrobial effects of indigo naturalis prepared from Strobilanthes formosanus Moore.

PubMed

Chiang, Yin-Ru; Li, Ann; Leu, Yann-Lii; Fang, Jia-You; Lin, Yin-Ku

2013-11-21

Indigo naturalis is effective in treating nail psoriasis coexisting with microorganism infections. This study examines the antimicrobial effects of indigo naturalis prepared from Strobilanthes formosanus Moore. Eight bacterial and seven fungal strains were assayed using the agar diffusion method to examine the effects of indigo naturalis and its bioactive compounds. The bioactive compounds of indigo naturalis were purified sequentially using GFC, TLC, and HPLC. Their structures were identified using mass spectrometry and NMR spectroscopy. UPLC-MS/MS was applied to compare the metabolome profiles of indigo naturalis ethyl-acetate (EA) extract and its source plant, Strobilanthes formosanus Moore. The results of in vitro antimicrobial assays showed that indigo naturalis EA-extract significantly (≥1 mg/disc) inhibits Gram-positive bacteria (Staphylococcus aureus, S. epidermis and methicillin-resistant S. aureus (MRSA)) and mildly inhibits non-dermatophytic onychomycosis pathogens (Aspergillus fumigates and Candida albicans), but has little effect on dermatophyes. Isatin and tryptanthrin were identified as the bioactive compounds of indigo naturalis using S. aureus and S. epidermis as the bioassay model. Both bioactive ingredients had no effect on all tested fungi. In summary, indigo naturalis prepared from Strobilanthes formosanus Moore exhibits antimicrobial effects on Staphylococcus and non-dermatophytic onychomycosis pathogens. Tryptanthrin and isatin may be its major bioactive ingredients against Staphylococcus and the inhibitory effect on MRSA may be due to other unidentified ingredients.

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.

Biological Targets and Mechanisms of Action of Natural Products from Marine Cyanobacteria

PubMed Central

Salvador-Reyes, Lilibeth A.

2015-01-01

Marine cyanobacteria are an ancient group of organisms and prolific producers of bioactive secondary metabolites. These compounds are presumably optimized by evolution over billions of years to exert high affinity for their intended biological target in the ecologically relevant organism but likely also possess activity in different biological contexts such as human cells. Screening of marine cyanobacterial extracts for bioactive natural products has largely focused on cancer cell viability; however, diversification of the screening platform led to the characterization of many new bioactive compounds. Targets of compounds have oftentimes been elusive if the compounds were discovered through phenotypic assays. Over the past few years, technology has advanced to determine mechanism of action (MOA) and targets through reverse chemical genetic and proteomic approaches, which has been applied to certain cyanobacterial compounds and will be discussed in this review. Some cyanobacterial molecules are the most-potent-in-class inhibitors and therefore may become valuable tools for chemical biology to probe protein function but also be templates for novel drugs, assuming in vitro potency translates into cellular and in vivo activity. Our review will focus on compounds for which the direct targets have been deciphered or which were found to target a novel pathway, and link them to disease states where target modulation may be beneficial. PMID:25571978

Characterization, Preparation, and Purification of Marine Bioactive Peptides

PubMed Central

Wang, Xueqin; Yu, Huahua; Xing, Ronge

2017-01-01

Marine bioactive peptides, as a source of unique bioactive compounds, are the focus of current research. They exert various biological roles, some of the most crucial of which are antioxidant activity, antimicrobial activity, anticancer activity, antihypertensive activity, anti-inflammatory activity, and so forth, and specific characteristics of the bioactivities are described. This review also describes various manufacturing techniques for marine bioactive peptides using organic synthesis, microwave assisted extraction, chemical hydrolysis, and enzymes hydrolysis. Finally, purification of marine bioactive peptides is described, including gel or size exclusion chromatography, ion-exchange column chromatography, and reversed-phase high-performance liquid chromatography, which are aimed at finding a fast, simple, and effective method to obtain the target peptides. PMID:28761878

Piper betel leaf: a reservoir of potential xenohormetic nutraceuticals with cancer-fighting properties.

PubMed

Gundala, Sushma R; Aneja, Ritu

2014-05-01

Plants contain a much greater diversity of bioactive compounds than any man-made chemical library. Heart-shaped Piper betel leaves are magnificent reservoirs of phenolic compounds with antiproliferative, antimutagenic, antibacterial, and antioxidant properties. Widely consumed in South Asian countries, the glossy leaf contains a multitude of biophenolics such as hydroxychavicol, eugenol, chavibetol, and piperols. Convincing data underscore the remarkable chemotherapeutic and chemopreventive potential of betel leaves against a variety of cancer types. The leaf constituents modulate an extensive array of signaling molecules such as transcription factors as well as reactive oxygen species (ROS) to control multiple nodes of various cellular proliferation and death pathways. Herein, we provide an overall perspective on the cancer-fighting benefits of the phenolic phytochemicals in betel leaves and a comprehensive overview of the mechanisms responsive to dose-driven ROS-mediated signaling cascades conscripted by bioactive phenolics to confer chemotherapeutic and chemopreventive advantages. Intriguingly, these ROS-triggered responses are contextual and may either elicit a protective xenohormetic antioxidant response to premalignant cells to constitute a chemopreventive effect or generate a curative chemotherapeutic response by pro-oxidatively augmenting the constitutively elevated ROS levels in cancer cells to tip the balance in favor of selective apoptosis induction in cancer cells while sparing normal ones. In conclusion, this review provides an update on how distinct ROS levels exist in normal versus cancer cells and how these levels can be strategically modulated and exploited for therapeutic gains. We emphasize the yet untapped potential of the evergreen vine, betel leaf, for chemopreventive and chemotherapeutic management of cancer.

Delivery of Flavonoids and Saponins from Black Bean (Phaseolus vulgaris) Seed Coats Incorporated into Whole Wheat Bread

PubMed Central

Chávez-Santoscoy, Rocio A.; Lazo-Vélez, Marco A.; Serna-Sáldivar, Sergio O.; Gutiérrez-Uribe, Janet A.

2016-01-01

Cereal-based products can be used as vehicles for the delivery of relevant bioactive compounds since they are staple foods for most cultures throughout the world. The health promoting benefits of flavonoids and saponins contained in black bean seed coats have been previously described. In the present work, the effect of adding flavonoids and saponins from black bean seed coat to the typical yeast-leavened whole wheat bread formulation in terms of bread features, organoleptic properties and phytochemical profile was studied. The retention of bioactive compounds was determined and the inhibitory effects of in vitro enzyme digested samples on two colon cancer cell lines (Caco-2 and HT29) was evaluated. The addition of bioactive compounds did not significantly affect baking properties or texture parameters. Among organoleptic properties of enriched breads, only crumb color was affected by the addition of bioactive compounds. However, the use of whole wheat flour partially masked the effect on color. More than 90% of added flavonoids and saponins and 80% of anthocyanins were retained in bread after baking. However, saponins were reduced more than 50% after the in vitro enzyme digestion. The black bean seed coat phytochemicals recovered after in vitro enzyme digestion of enriched breads significantly reduced by 20% the viability of colon cancer cells without affecting standard fibroblast cells (p < 0.05). PMID:26901186

Delivery of Flavonoids and Saponins from Black Bean (Phaseolus vulgaris) Seed Coats Incorporated into Whole Wheat Bread.

PubMed

Chávez-Santoscoy, Rocio A; Lazo-Vélez, Marco A; Serna-Sáldivar, Sergio O; Gutiérrez-Uribe, Janet A

2016-02-17

Cereal-based products can be used as vehicles for the delivery of relevant bioactive compounds since they are staple foods for most cultures throughout the world. The health promoting benefits of flavonoids and saponins contained in black bean seed coats have been previously described. In the present work, the effect of adding flavonoids and saponins from black bean seed coat to the typical yeast-leavened whole wheat bread formulation in terms of bread features, organoleptic properties and phytochemical profile was studied. The retention of bioactive compounds was determined and the inhibitory effects of in vitro enzyme digested samples on two colon cancer cell lines (Caco-2 and HT29) was evaluated. The addition of bioactive compounds did not significantly affect baking properties or texture parameters. Among organoleptic properties of enriched breads, only crumb color was affected by the addition of bioactive compounds. However, the use of whole wheat flour partially masked the effect on color. More than 90% of added flavonoids and saponins and 80% of anthocyanins were retained in bread after baking. However, saponins were reduced more than 50% after the in vitro enzyme digestion. The black bean seed coat phytochemicals recovered after in vitro enzyme digestion of enriched breads significantly reduced by 20% the viability of colon cancer cells without affecting standard fibroblast cells (p < 0.05).

Rebelling against the (Insulin) Resistance: A Review of the Proposed Insulin-Sensitizing Actions of Soybeans, Chickpeas, and Their Bioactive Compounds

PubMed Central

Zahradka, Peter

2018-01-01

Insulin resistance is a major risk factor for diseases such as type 2 diabetes and metabolic syndrome. Current methods for management of insulin resistance include pharmacological therapies and lifestyle modifications. Several clinical studies have shown that leguminous plants such as soybeans and pulses (dried beans, dried peas, chickpeas, lentils) are able to reduce insulin resistance and related type 2 diabetes parameters. However, to date, no one has summarized the evidence supporting a mechanism of action for soybeans and pulses that explains their ability to lower insulin resistance. While it is commonly assumed that the biological activities of soybeans and pulses are due to their antioxidant activities, these bioactive compounds may operate independent of their antioxidant properties and, thus, their ability to potentially improve insulin sensitivity via alternative mechanisms needs to be acknowledged. Based on published studies using in vivo and in vitro models representing insulin resistant states, the proposed mechanisms of action for insulin-sensitizing actions of soybeans, chickpeas, and their bioactive compounds include increasing glucose transporter-4 levels, inhibiting adipogenesis by down-regulating peroxisome proliferator-activated receptor-γ, reducing adiposity, positively affecting adipokines, and increasing short-chain fatty acid-producing bacteria in the gut. Therefore, this review will discuss the current evidence surrounding the proposed mechanisms of action for soybeans and certain pulses, and their bioactive compounds, to effectively reduce insulin resistance. PMID:29601521

Combined genetic and bioactivity-based prioritization leads to the isolation of an endophyte-derived antimycobacterial compound.

PubMed

Alvin, A; Kalaitzis, J A; Sasia, B; Neilan, B A

2016-05-01

To initiate a genetic and bioactivity-based screening programme of culturable endophytes to identify micro-organisms capable of producing bioactive polyketides and peptides. Fungal endophytes were isolated from flowers, leaves and roots of Rhoeo spathacea, revealing a community consisting of Colletotrichum sp., Fusarium sp., Guignardia sp., Phomopsis sp., Phoma sp. and Microdochium sp. Genetic screening showed that all isolates had polyketide synthase (PKS) genes and most had nonribosomal peptide synthetase (NRPS) genes. Ethyl acetate extracts of the fungal isolates exhibited antiproliferative activity against at least one of the seven bacterial and mycobacterial test strains. Nuclear Magnetic Resonance -guided fractionation of the crude extract from a Fusarium sp. strain which exhibited strong antiproliferative activity against Mycobacterium tuberculosis resulted in the isolation of the polyketide javanicin. This compound was active against Myco. tuberculosis (MIC = 25 μg ml(-1)) and Mycobacterium phlei (MIC = 50 μg ml(-1)). The medicinal plant R. spathacea hosts a variety of fungal endophytes capable of producing antibacterial and antimycobacterial compounds. There is a positive correlation between the presence of PKS and/or NRPS encoding genes in endophytes and the bioactivity of their respective organic extracts. This is the first report on the fungal endophytic diversity of R. spathacea, and the isolation of an antimycobacterial compound from the plant which has been traditionally used for the treatment of tuberculosis symptoms. © 2016 The Society for Applied Microbiology.

Antioxidant activity and bioactive compound contents before and after in vitro digestion of new tomato hybrids.

PubMed

Tommonaro, Giuseppina; Speranza, Giovanna; De Prisco, Rocco; Iodice, Carmine; Crudele, Egle; Abbamondi, Gennaro Roberto; Nicolaus, Barbara

2017-12-01

The antioxidant properties and bioactive compound contents of fresh new tomato hybrids before and after in vitro digestion were investigated. To this aim, the antioxidant activities of lipophilic, hydrophilic and polyphenolic extracts of tomato hybrids were determined by ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)), DMPD (N,N-dimethyl-p-phenylenediamine dihydrochloride) and DPPH (2,2-diphenyl-1-picrylhydrazyl) methods respectively, while the bioactive compound contents were estimated via Folin-Ciocalteu (polyphenols), pH differential (anthocyanins) and high-performance liquid chromatography (lycopene and β-carotene) methods. After the digestion process, a marked loss (ranging from 37 to 77%) of antioxidant capacity linked to the hydrophilic fraction was observed. In contrast, the lipophilic and methanolic fractions showed an increase in antioxidant activity (ranging from 9 to 40%) after gastric digestion, and a rapid decrease was observed after total digestion. Moreover, the presence of anthocyanins and carotenoids after simulated digestion was a notable result. The bioavailability of bioactive metabolites from nutraceutical food and their healthful properties in humans are strictly dependent on the digestion process. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Hibiscus sabdariffa L. as a source of nutrients, bioactive compounds and colouring agents.

PubMed

Jabeur, Inès; Pereira, Eliana; Barros, Lillian; Calhelha, Ricardo C; Soković, Marina; Oliveira, M Beatriz P P; Ferreira, Isabel C F R

2017-10-01

The nutritional and bioactive composition of plants have aroused much interest not only among scientists, but also in people's daily lives. Apart from the health benefits, plants are a source of pigments that can be used as natural food colorants. In this work, the nutritional composition of Hibiscus sabdariffa L. was analysed, as well as its bioactive compounds and natural pigments. Glucose (sugar), malic acid (organic acid), α-tocopherol (tocopherol) and linoleic acid (fatty acid) were the major constituents in the corresponding classes. 5-(Hydroxymethyl) furfural was the most abundant non-anthocyanin compound, while delphinidin-3-O-sambubioside was the major anthocyanin both in its hydroethanolic extract and infusion. H. sabdariffa extracts showed antioxidant and antimicrobial activities, highlighting that the hydroethanol extract presents not only lipid peroxidation inhibition capacity, but also bactericidal/fungicidal inhibition ability for all the bacteria and fungi tested. Furthermore, both extracts revealed the absence of toxicity using porcine primary liver cells. The studied plant species was thus not only interesting for nutritional purposes but also for bioactive and colouring applications in food, cosmetic and pharmaceutical industries. Copyright © 2017 Elsevier Ltd. All rights reserved.

Antioxidant Activity of Hawaiian Marine Algae

PubMed Central

Kelman, Dovi; Posner, Ellen Kromkowski; McDermid, Karla J.; Tabandera, Nicole K.; Wright, Patrick R.; Wright, Anthony D.

2012-01-01

Marine algae are known to contain a wide variety of bioactive compounds, many of which have commercial applications in pharmaceutical, medical, cosmetic, nutraceutical, food and agricultural industries. Natural antioxidants, found in many algae, are important bioactive compounds that play an important role against various diseases and ageing processes through protection of cells from oxidative damage. In this respect, relatively little is known about the bioactivity of Hawaiian algae that could be a potential natural source of such antioxidants. The total antioxidant activity of organic extracts of 37 algal samples, comprising of 30 species of Hawaiian algae from 27 different genera was determined. The activity was determined by employing the FRAP (Ferric Reducing Antioxidant Power) assays. Of the algae tested, the extract of Turbinaria ornata was found to be the most active. Bioassay-guided fractionation of this extract led to the isolation of a variety of different carotenoids as the active principles. The major bioactive antioxidant compound was identified as the carotenoid fucoxanthin. These results show, for the first time, that numerous Hawaiian algae exhibit significant antioxidant activity, a property that could lead to their application in one of many useful healthcare or related products as well as in chemoprevention of a variety of diseases including cancer. PMID:22412808

Targeted isolation and identification of bioactive compounds lowering cholesterol in the crude extracts of crabapples using UPLC-DAD-MS-SPE/NMR based on pharmacology-guided PLS-DA.

PubMed

Wen, Chao; Wang, Dongshan; Li, Xing; Huang, Tao; Huang, Cheng; Hu, Kaifeng

2018-02-20

The anti-hyperlipidemic effects of crude crabapple extracts derived from Malus 'Red jade', Malus hupehensis (Pamp.) Rehd. and Malus prunifolia (Willd.) Borkh. were evaluated on high-fat diet induced obese (HF DIO) mice. The results revealed that some of these extracts could lower serum cholesterol levels in HF DIO mice. The same extracts were also parallelly analyzed by LC-MS in both positive and negative ionization modes. Based on the pharmacological results, 22 LC-MS variables were identified to be correlated with the anti-hyperlipidemic effects using partial least square discriminant analysis (PLS-DA) and independent samples t-test. Further, under the guidance of the bioactivity-correlated LC-MS signals, 10 compounds were targetedly isolated and enriched using UPLC-DAD-MS-SPE and identified/elucidated by NMR together with MS/MS as citric acid(1), p-coumaric acid(2), hyperoside(3), myricetin(4), naringenin(5), quercetin(6), kaempferol(7), gentiopicroside(8), ursolic acid(9) and 8-epiloganic acid(10). Among these 10 compounds, 6 compounds, hyperoside(3), myricetin(4), naringenin(5), quercetin(6), kaempferol(7) and ursolic acid(9), were individually studied and reported to indeed have effects on lowering the serum lipid levels. These results demonstrated the efficiency of this strategy for drug discovery. In contrast to traditional routes to discover bioactive compounds in the plant extracts, targeted isolation and identification of bioactive compounds in the crude plant extracts using UPLC-DAD-MS-SPE/NMR based on pharmacology-guided PLS-DA of LC-MS data brings forward a new efficient dereplicated approach to natural products research for drug discovery. Copyright © 2017 Elsevier B.V. All rights reserved.

Marine Algicolous Endophytic Fungi - A Promising Drug Resource of the Era.

PubMed

Sarasan, Manomi; Puthumana, Jayesh; Job, Neema; Han, Jeonghoon; Lee, Jae-Seong; Philip, Rosamma

2017-06-28

Endophytic fungi have currently been acknowledged as the most promising source of bioactive compounds for drug discovery, and considerable progress has been made in exploring their diversity, species richness, and bioprospecting. Fungal endophytes from unique environmental settings offer a pool of potentially useful medicinal entities. Owing to the constant stresses imposed on macroalgae by marine environments, it is believed that algae and their associated endophytic symbionts represent a good source of structurally diverse bioactive secondary metabolites. Despite the proven significance of active metabolites of algal endophytes, little have been exploited. This review highlights the latest discoveries in algicolous endophytic research, with particular focus on the bioactive metabolites from algal endophytes. Compounds are classified according to their reported biological activities, like anticancer, antibacterial, antifungal, and antioxidant properties. Present experimental evidence suggests that a majority of the bioactive metabolites were reported from Phaeophyceae followed by Rhodophyceae and Chlorophyceae. An intensive search for newer and more effective bioactive metabolites has generated a treasure trove of publications, and this review partially covers the literature published up to 2016.

Direct growth inhibition assay of total airborne fungi with application of biocide-treated malt extract agar.

PubMed

Er, Chin Ming; Sunar, N M; Leman, A M; Othman, N

2015-01-01

Indoor air pollution by airborne fungi has risen to become a common issue all over the world and it is hazardous to indoor occupants' health as it is associated with a series of respiratory-related and skin-related diseases. Selected bioactive compounds from the food industry have been suggested to be effective against individual fungus isolated from indoor environment. However, the techniques used to evaluate these compounds were lengthy and unsuitable against total airborne fungi. Therefore, this paper describes an assay to assess the effectiveness of a bioactive compound to inhibit growth of total airborne fungi.•A combination and modification of previous methods and the NIOSH Manual Analytical Standard Method (NMAM 0800) is proposed.•This method concurrently samples the total airborne fungi and evaluates the ability of bioactive compounds (potassium sorbate in this paper), as a biocide, to treat these indoor airborne fungi.•The current method shortens the time of evaluation from 30 days to only 5 days and employs the counting of colony forming units (CFUs) to ease the measurement of the growth of fungi.

Electro-activation of sweet defatted whey: Impact on the induced Maillard reaction products and bioactive peptides.

PubMed

Kareb, Ourdia; Gomaa, Ahmed; Champagne, Claude P; Jean, Julie; Aïder, Mohammed

2017-04-15

Electro-activation was used to add value to sweet defatted whey. This study aimed to investigate and to characterize the bioactive compounds formed under different electro-activation conditions by molecular and proteomic approaches. The effects of electric current intensity (400, 500 or 600mA) and whey concentration (7, 14 or 21% (w/v)) as a function of the electro-activation time (0, 15, 30 or 45min) were evaluated. The targeted dependent variables were the formation of Maillard reaction products (MRPs), protein hydrolysates and glycated compounds. It was shown that the MRPs derived from electro-activated whey at a concentration of 14% had the highest potential of biological activity. SDS-PAGE analyses indicated the formation of hydrolysates and glycated compounds with different molecular weight distributions. FTIR indicated the predominance of intermediate MRPs, such as the Schiff base compounds. LC-MS/MS and proteomics analysis showed the production of multi-functional bioactive peptides due to the hydrolysis of whey proteins. Crown Copyright © 2016. Published by Elsevier Ltd. All rights reserved.

Bioactive compounds from orange epicarp to enrich fish burgers.

PubMed

Spinelli, Sara; Lecce, Lucia; Likyova, Desislava; Del Nobile, Matteo Alessandro; Conte, Amalia

2018-05-01

The orange industry produces considerable amounts of by-products, traditionally used for animal feed or fuel production. Most of these by-products could be used as functional ingredients. To assess the potential food application of orange epicarp, different percentages of micro-encapsulated orange extract were added to fresh fish burgers. Then, an in vitro digestion was also carried out, before and after micro-encapsulation, to measure the bio-accessibility of the active compounds. A significant increase of bio-accessibility of bioactive compounds has been observed in the orange epicarp extract after micro-encapsulation by spray-drying. From the sensory point of view, the fish sample enriched with 50 g kg -1 micro-encapsulated extract was the most comparable to the control burger, even if it showed a higher phenolic, flavonoid and carotenoid bio-accessibility. Orange epicarp may be used as a food additive to enhance the health content of food products. The micro-encapsulation is a valid technique to protect the bioactive compounds and increase their bio-accessibility. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Quality index, consumer acceptability, bioactive compounds, and antioxidant activity of fresh-cut "ataulfo" mangoes (mangifera indica L.) as affected by low-temperature storage.

PubMed

Robles-Sánchez, R M; Islas-Osuna, M A; Astiazarán-García, H; Vázquez-Ortiz, F A; Martín-Belloso, O; Gorinstein, S; González-Aguilar, G A

2009-04-01

To measure bioactive compound losses due to minimal processing, mature green fresh-cut mangoes (Mangifera indica L.) cv. "Ataulfo" were subjected to an antioxidant treatment and stored at 5 degrees C during 15 d. Quality index, total phenols, flavonoids, beta-carotene, ascorbic acid, vitamin E, and antioxidant activity were measured during the storage period of fruits. Antioxidant capacity was estimated using ORAC(FL), TEAC, and DPPH assays. The dipping treatments with ascorbic acid (AA) + citric acid (CA) + CaCl2 affected positively quality delaying deterioration of fresh-cut mango as compared with whole fruit. However, dipping treatment affected the consumer preferences of fresh-cut mangoes. The highest vitamin C, beta-carotene, and vitamin E losses were observed after 10 d, being similar in whole and fresh-cut mangoes. The antioxidant activity was not significantly affected by storage time. We conclude that fresh-cut mangoes retained their bioactive compound content during storage and their antioxidant and nutritional properties make them a good source of these compounds.

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.

Comparison of nutritional properties of Stinging nettle (Urtica dioica) flour with wheat and barley flours.

PubMed

Adhikari, Bhaskar Mani; Bajracharya, Alina; Shrestha, Ashok K

2016-01-01

Stinging nettle (Urtica dioica. L) is a wild, unique herbaceous perennial flowering plant with Stinging hairs. It has a long history of use as a food sources as a soup or curries, and also used as a fiber as well as a medicinal herb. The current aim was to analyze the composition and bioactive compounds in Nepalese Stinging nettle. Chemical analysis showed the relatively higher level of crude protein (33.8%), crude fiber (9.1%), crude fat (3.6%), total ash (16.2%), carbohydrate (37.4%), and relatively lower energy value (307 kcal/100 g) as compared to wheat and barley flours. Analysis of nettle powder showed significantly higher level of bioactive compounds: phenolic compounds as 129 mg Gallic acid equivalent/g; carotenoid level 3497 μg/g; tannin 0.93 mg/100 g; anti-oxidant activity 66.3 DPPH inhibition (%), as compared to wheat and barley. This study further established that nettle plants as very good source of energy, proteins, high fiber, and a range of health benefitting bioactive compounds.

Health Effects of Psidium guajava L. Leaves: An Overview of the Last Decade.

PubMed

Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

2017-04-24

Today, there is increasing interest in discovering new bioactive compounds derived from ethnomedicine. Preparations of guava ( Psidium guajava L.) leaves have traditionally been used to manage several diseases. The pharmacological research in vitro as well as in vivo has been widely used to demonstrate the potential of the extracts from the leaves for the co-treatment of different ailments with high prevalence worldwide, upholding the traditional medicine in cases such as diabetes mellitus, cardiovascular diseases, cancer, and parasitic infections. Moreover, the biological activity has been attributed to the bioactive composition of the leaves, to some specific phytochemical subclasses, or even to individual compounds. Phenolic compounds in guava leaves have been credited with regulating blood-glucose levels. Thus, the aim of the present review was to compile results from in vitro and in vivo studies carried out with guava leaves over the last decade, relating the effects to their clinical applications in order to focus further research for finding individual bioactive compounds. Some food applications (guava tea and supplementary feed for aquaculture) and some clinical, in vitro, and in vivo outcomes are also included.

Health Effects of Psidium guajava L. Leaves: An Overview of the Last Decade

PubMed Central

Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

2017-01-01

Today, there is increasing interest in discovering new bioactive compounds derived from ethnomedicine. Preparations of guava (Psidium guajava L.) leaves have traditionally been used to manage several diseases. The pharmacological research in vitro as well as in vivo has been widely used to demonstrate the potential of the extracts from the leaves for the co-treatment of different ailments with high prevalence worldwide, upholding the traditional medicine in cases such as diabetes mellitus, cardiovascular diseases, cancer, and parasitic infections. Moreover, the biological activity has been attributed to the bioactive composition of the leaves, to some specific phytochemical subclasses, or even to individual compounds. Phenolic compounds in guava leaves have been credited with regulating blood-glucose levels. Thus, the aim of the present review was to compile results from in vitro and in vivo studies carried out with guava leaves over the last decade, relating the effects to their clinical applications in order to focus further research for finding individual bioactive compounds. Some food applications (guava tea and supplementary feed for aquaculture) and some clinical, in vitro, and in vivo outcomes are also included. PMID:28441777

Phytochemical characterization of different prickly pear (Opuntia ficus-indica (L.) Mill.) cultivars and botanical parts: UHPLC-ESI-MSn metabolomics profiles and their chemometric analysis.

PubMed

Mena, Pedro; Tassotti, Michele; Andreu, Lucía; Nuncio-Jáuregui, Nallely; Legua, Pilar; Del Rio, Daniele; Hernández, Francisca

2018-06-01

Prickly pear is an important source of bioactive compounds. However, a comprehensive characterization of the phytochemical profile of its aerial botanical parts, considering genotypic differences, has not been conducted. This study evaluated the phytochemical composition of four botanical parts (fruit pulp and skin, and young and adult cladodes) of six cultivars. Analysis was carried out by using two non-targeted UHPLC-ESI-MS n experimental conditions and assisted with multivariate analysis to facilitate data interpretation. Up to 41 compounds, mainly (poly)phenolic molecules, were identified and quantified, 23 compounds being reported for the first time in Opuntia ficus-indica. Phenolic composition varied significantly depending on the part of the plant. Betalains were detected only in the fruit of a red cultivar. This study provided novel insights in terms of identification of bioactives and thorough characterization of botanical parts of prickly pears. This information may be used for the development of prickly pear-derived products with high levels of bioactive compounds. Copyright © 2018 Elsevier Ltd. All rights reserved.

Analysis of Pfizer compounds in EPA's ToxCast chemicals-assay space.

PubMed

Shah, Falgun; Greene, Nigel

2014-01-21

The U.S. Environmental Protection Agency (EPA) launched the ToxCast program in 2007 with the goal of evaluating high-throughput in vitro assays to prioritize chemicals that need toxicity testing. Their goal was to develop predictive bioactivity signatures for toxic compounds using a set of in vitro assays and/or in silico properties. In 2009, Pfizer joined the ToxCast initiative by contributing 52 compounds with preclinical and clinical data for profiling across the multiple assay platforms available. Here, we describe the initial analysis of the Pfizer subset of compounds within the ToxCast chemical (n = 1814) and in vitro assay (n = 486) space. An analysis of the hit rate of Pfizer compounds in the ToxCast assay panel allowed us to focus our mining of assays potentially most relevant to the attrition of our compounds. We compared the bioactivity profile of Pfizer compounds to other compounds in the ToxCast chemical space to gain insights into common toxicity pathways. Additionally, we explored the similarity in the chemical and biological spaces between drug-like compounds and environmental chemicals in ToxCast and compared the in vivo profiles of a subset of failed pharmaceuticals having high similarity in both spaces. We found differences in the chemical and biological spaces of pharmaceuticals compared to environmental chemicals, which may question the applicability of bioactivity signatures developed exclusively based on the latter to drug-like compounds if used without prior validation with the ToxCast Phase-II chemicals. Finally, our analysis has allowed us to identify novel interactions for our compounds in particular with multiple nuclear receptors that were previously not known. This insight may help us to identify potential liabilities with future novel compounds.

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.

Optimization of pressurized liquid extraction by response surface methodology of Goji berry (Lycium barbarum L.) phenolic bioactive compounds.

PubMed

Tripodo, Giusy; Ibáñez, Elena; Cifuentes, Alejandro; Gilbert-López, Bienvenida; Fanali, Chiara

2018-01-03

Pressurized liquid extraction (PLE) has been used for the first time in this work to extract phenolic compounds from Goji berries according to a multilevel factorial design using response surface methodology. The global yield (% w/dw, weight/dry-weight), total phenolic content (TPC), total flavonoid (TF) and antioxidant activity (determined via ABTS assay, expressed as TEAC value) were used as response variables to study the effects of temperature (50-180°C) and green solvent composition (mixtures of ethanol/water). Phenolic compounds characterization was performed by high performance liquid chromatography-diode array detector-tandem mass spectrometry (HPLC-DAD-MS/MS). The optimum PLE conditions predicted by the model were as follows: 180°C and 86% ethanol in water with a good desirability value of 0.815. The predicted conditions were confirmed experimentally and once the experimental design was validated for commercial fruit samples, the PLE extraction of phenolic compounds from three different varieties of fruit samples (Selvatico mongolo, Bigol, and Polonia) was performed. Nine phenolic compounds were tentatively identified in these extracts, including phenolic acids and their derivatives, and flavonols. The optimized PLE conditions were compared to a conventional solid-liquid extraction, demonstrating that PLE is a useful alternative to extract phenolic compounds from Goji berry. © 2018 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Development of garlic bioactive compounds analytical methodology based on liquid phase microextraction using response surface design. Implications for dual analysis: Cooked and biological fluids samples.

PubMed

Ramirez, Daniela Andrea; Locatelli, Daniela Ana; Torres-Palazzolo, Carolina Andrea; Altamirano, Jorgelina Cecilia; Camargo, Alejandra Beatriz

2017-01-15

Organosulphur compounds (OSCs) present in garlic (Allium sativum L.) are responsible of several biological properties. Functional foods researches indicate the importance of quantifying these compounds in food matrices and biological fluids. For this purpose, this paper introduces a novel methodology based on dispersive liquid-liquid microextraction (DLLME) coupled to high performance liquid chromatography with ultraviolet detector (HPLC-UV) for the extraction and determination of organosulphur compounds in different matrices. The target analytes were allicin, (E)- and (Z)-ajoene, 2-vinyl-4H-1,2-dithiin (2-VD), diallyl sulphide (DAS) and diallyl disulphide (DADS). The microextraction technique was optimized using an experimental design, and the analytical performance was evaluated under optimum conditions. The desirability function presented an optimal value for 600μL of chloroform as extraction solvent using acetonitrile as dispersant. The method proved to be reliable, precise and accurate. It was successfully applied to determine OSCs in cooked garlic samples as well as blood plasma and digestive fluids. Copyright © 2016 Elsevier Ltd. All rights reserved.

Aqua mediated synthesis of bio-active compounds.

PubMed

Panda, Siva S

2013-05-01

Recently the aqueous medium has attracted the interest of organic chemists, and many. Moreover, in the past 20 years, the drug-discovery process has undergone extraordinary changes, and high-throughput biological screening of potential drug candidates has led to an ever-increasing demand for novel drug-like compounds. Noteworthy advantages were observed during the course of study on aqua mediated synthesis of compounds of medicinal importance. The established advantages of water as a solvent for reactions are, water is the most abundant and available resource on the planet and many biochemical processes occur in aqueous medium. This review will focus on describing new developments in the application of water in medicinal chemistry for the synthesis of bio-active compounds possessing various biological properties.

Bioactive Compounds Derived from the Yeast Metabolism of Aromatic Amino Acids during Alcoholic Fermentation

PubMed Central

Guillamon, Jose Manuel; Torija, Maria Jesus; Beltran, Gemma; Troncoso, Ana M.; Garcia-Parrilla, M. Carmen

2014-01-01

Metabolites resulting from nitrogen metabolism in yeast are currently found in some fermented beverages such as wine and beer. Their study has recently attracted the attention of researchers. Some metabolites derived from aromatic amino acids are bioactive compounds that can behave as hormones or even mimic their role in humans and may also act as regulators in yeast. Although the metabolic pathways for their formation are well known, the physiological significance is still far from being understood. The understanding of this relevance will be a key element in managing the production of these compounds under controlled conditions, to offer fermented food with specific enrichment in these compounds or even to use the yeast as nutritional complements. PMID:24895623

Dihydroresveratrol Type Dihydrostilbenoids: Chemical Diversity, Chemosystematics, and Bioactivity.

PubMed

Vitalini, Sara; Cicek, Serhat S; Granica, Sebastian; Zidorn, Christian

2018-01-01

Dihydrostilbenoids, a diverse class of natural products differing from stilbenoids by the missing double bond in the ethylene chain linking the aromatic moieties, have been reported from fungi, mosses, ferns, and flowering plants. Occurrence, structure, and bioactivity of naturally occurring dihydroresveratrol type dihydrostilbenoids are discussed in this review. A Reaxys database search for dihydroresveratrol derivatives with possible substitutions on all atoms, but excluding non-natural products and compounds featuring additional rings involving the ethyl connecting chain, was performed. Structures include simple dihydroresveratrol derivatives, compounds substituted with complex side chains composed of acyl moieties and sugars, and compounds containing polycyclic cores attached to dihydrostilbenoid units. Dihydrostilbenoids have a wide spectrum of bioactivities ranging from expectable antioxidant and anti-inflammatory activities to interesting neuroprotective and anticancer activity. The anticancer activity in particular is very pronounced for some plant-derived dihydrostilbenoids and makes them interesting lead compounds for drug development. Apart from some reports on dihydroresveratrol derivatives as phytoalexins against plant-pathogenic fungi, only very limited information is available on the ecological role of these compounds for the organisms producing them. Dihydrostilbenoids are a class of natural products possessing significant biological activities; their scattered but not ubiquitous occurrence throughout the kingdoms of plants and fungi is not easily explained. We are convinced that future studies will identify new sources of dihydrostilbenoids, and we hope that the present review will inspire such studies and will help in directing such efforts to suitable source organisms and towards promising bioactivities. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

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.

Exploring Marine Cyanobacteria for Lead Compounds of Pharmaceutical Importance

PubMed Central

Uzair, Bushra; Tabassum, Sobia; Rasheed, Madiha; Rehman, Saima Firdous

2012-01-01

The Ocean, which is called the “mother of origin of life,” is also the source of structurally unique natural products that are mainly accumulated in living organisms. Cyanobacteria are photosynthetic prokaryotes used as food by humans. They are excellent source of vitamins and proteins vital for life. Several of these compounds show pharmacological activities and are helpful for the invention and discovery of bioactive compounds, primarily for deadly diseases like cancer, acquired immunodeficiency syndrome (AIDS), arthritis, and so forth, while other compounds have been developed as analgesics or to treat inflammation, and so forth. They produce a large variety of bioactive compounds, including substances with anticancer and antiviral activity, UV protectants, specific inhibitors of enzymes, and potent hepatotoxins and neurotoxins. Many cyanobacteria produce compounds with potent biological activities. This paper aims to showcase the structural diversity of marine cyanobacterial secondary metabolites with a comprehensive coverage of alkaloids and other applications of cyanobacteria. PMID:22545008

A Review on Ethnopharmacological Applications, Pharmacological Activities, and Bioactive Compounds of Mangifera indica (Mango)

PubMed Central

2017-01-01

Mangifera indica (family Anacardiaceae), commonly known as mango, is a pharmacologically, ethnomedically, and phytochemically diverse plant. Various parts of M. indica tree have been used in traditional medicine for the treatment of different ailments, and a number of bioactive phytochemical constituents of M. indica have been reported, namely, polyphenols, terpenes, sterols, carotenoids, vitamins, and amino acids, and so forth. Several studies have proven the pharmacological potential of different parts of mango trees such as leaves, bark, fruit peel and flesh, roots, and flowers as anticancer, anti-inflammatory, antidiabetic, antioxidant, antibacterial, antifungal, anthelmintic, gastroprotective, hepatoprotective, immunomodulatory, antiplasmodial, and antihyperlipemic. In the present review, a comprehensive study on ethnopharmacological applications, pharmacological activities, and bioactive compounds of M. indica has been described. PMID:29456572

Chemical Biology Probes from Advanced DNA-encoded Libraries.

PubMed

Salamon, Hazem; Klika Škopić, Mateja; Jung, Kathrin; Bugain, Olivia; Brunschweiger, Andreas

2016-02-19

The identification of bioactive compounds is a crucial step toward development of probes for chemical biology studies. Screening of DNA-encoded small molecule libraries (DELs) has emerged as a validated technology to interrogate vast chemical space. DELs consist of chimeric molecules composed of a low-molecular weight compound that is conjugated to a DNA identifier tag. They are screened as pooled libraries using selection to identify "hits." Screening of DELs has identified numerous bioactive compounds. Some of these molecules were instrumental in gaining a deeper understanding of biological systems. One of the main challenges in the field is the development of synthesis methodology for DELs.

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

Postharvest responses of red and yellow sweet peppers grown under photo-selective nets.

PubMed

Selahle, Kamogelo M; Sivakumar, Dharini; Jifon, John; Soundy, Puffy

2015-04-15

Postharvest responses of red ('HTSP-3') and yellow ('Celaya') sweet pepper fruit yield, quality parameters and bioactive compounds (to three types of photo-selective nets and a standard black net) were investigated in this study. Red and yellow peppers produced under the black net retained higher β-carotene, lower total phenolic contents and showed deep red and orange colour after storage. Both peppers produced under the pearl net retained a higher ascorbic content, antioxidant scavenging activity, fruit firmness and also reduced weight loss after storage. Red and yellow peppers grown under pearl and yellow nets resulted in a higher percentage of marketable fruit, after storage. Red pepper grown under the yellow net showed a higher number of odour active aroma compounds in the fruit, while black nets significantly affected the synthesis of odour active aroma compounds during storage. Sensory analysis indicated a preference for red pepper fruits after storage from plants grown under pearl nets. Copyright © 2014 Elsevier Ltd. All rights reserved.

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

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.

Extensive characterisation of bioactive phenolic constituents from globe artichoke (Cynara scolymus L.) by HPLC-DAD-ESI-QTOF-MS.

PubMed

Abu-Reidah, Ibrahim M; Arráez-Román, David; Segura-Carretero, Antonio; Fernández-Gutiérrez, Alberto

2013-12-01

The aim of this work was to characterise the phenolic compounds in artichoke (hearts) by using HPLC coupled to DAD-ESI-QTOF-MS, which proved useful in characterising 61 phenolic and other polar compounds. Notably, of the 61 compounds characterised, 34 new phenolic compounds with their isomers have been tentatively characterised in artichoke for the first time, namely: 3 hydroxybenzoic acids, 17 hydroxycinnamic acids, 4 lignans, 7 flavones, 2 flavonols, and 1 phenol derivative. Moreover, a total of 28 isomers of previously described phenolics have also been detected. The data compiled from the qualitative polyphenol characterisation indicate that the artichoke extract analysed (Blanca de Tudela variety) could be regarded as a bioactive functional food and also as a promising source of antioxidant phenolic compounds. Copyright © 2013 Elsevier Ltd. All rights reserved.

The Role of the Gut Microbiota in the Metabolism of Polyphenols as Characterized by Gnotobiotic Mice

PubMed Central

Pasinetti, Giulio Maria; Singh, Risham; Westfall, Susan; Herman, Francis; Faith, Jeremiah; Ho, Lap

2018-01-01

A growing body of experimental data suggests that microbes in the gut influence behavior and can alter brain physiology and neurochemistry. Although promising, researchers are only starting to understand the potential of the gut microbiota for use in neurological disease. Recent evidence demonstrated that gastrointestinal activities are linked to mood disorders such as anxiety, depression, and most recently, cognitive functions in age-related neurodegenerative disorders. Studies from our group and others are uncovering new evidence suggesting that the gut microbiota plays a crucial role in the metabolism and bioavailability of certain dietary compounds and synthetic drugs. Based on this evidence, this review article will discuss the implications of the gut microbiota in mechanisms of bioavailability and biotransformation with an emphasis on dietary polyphenol compounds. This will be followed by a survey of ongoing innovative research identifying the ability of individual gut bacteria to enhance the bioavailability of gut-derived, brain-penetrating, bioactive polyphenol metabolites that ultimately influence mechanisms associated with the promotion of resilience against psychological and cognitive impairment in response to stress. Lastly, current research initiatives aimed at promoting the generation of brain bioactive polyphenol metabolites by specialized gut microbes will be discussed, specifically the use of gnotobiotic mice to develop bioengineered second generation probiotics. We propose that leveraging the gut microbial ecosystem to generate brain targeted bioactive metabolites from dietary polyphenols can attenuate lifestyle risk factors and promote resilience against age-related cognitive decline. PMID:29660942

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.

Bioactive Potential of Marine Macroalgae from the Central Red Sea (Saudi Arabia) Assessed by High-Throughput Imaging-Based Phenotypic Profiling

PubMed Central

Kremb, Stephan; Müller, Constanze; Schmitt-Kopplin, Philippe; Voolstra, Christian R.

2017-01-01

Marine algae represent an important source of novel natural products. While their bioactive potential has been studied to some extent, limited information is available on marine algae from the Red Sea. This study aimed at the broad discovery of new bioactivities from a collection of twelve macroalgal species from the Central Red Sea. We used imaging-based High-Content Screening (HCS) with a diverse spectrum of cellular markers for detailed cytological profiling of fractionated algal extracts. The cytological profiles for 3 out of 60 algal fractions clustered closely to reference inhibitors and showed strong inhibitory activities on the HIV-1 reverse transcriptase in a single-enzyme biochemical assay, validating the suggested biological target. Subsequent chemical profiling of the active fractions of two brown algal species by ultra-high resolution mass spectrometry (FT-ICR-MS) revealed possible candidate molecules. A database query of these molecules led us to groups of compounds with structural similarities, which are suggested to be responsible for the observed activity. Our work demonstrates the versatility and power of cytological profiling for the bioprospecting of unknown biological resources and highlights Red Sea algae as a source of bioactives that may serve as a starting point for further studies. PMID:28335513

Bioactive Potential of Marine Macroalgae from the Central Red Sea (Saudi Arabia) Assessed by High-Throughput Imaging-Based Phenotypic Profiling.

PubMed

Kremb, Stephan; Müller, Constanze; Schmitt-Kopplin, Philippe; Voolstra, Christian R

2017-03-20

Marine algae represent an important source of novel natural products. While their bioactive potential has been studied to some extent, limited information is available on marine algae from the Red Sea. This study aimed at the broad discovery of new bioactivities from a collection of twelve macroalgal species from the Central Red Sea. We used imaging-based High-Content Screening (HCS) with a diverse spectrum of cellular markers for detailed cytological profiling of fractionated algal extracts. The cytological profiles for 3 out of 60 algal fractions clustered closely to reference inhibitors and showed strong inhibitory activities on the HIV-1 reverse transcriptase in a single-enzyme biochemical assay, validating the suggested biological target. Subsequent chemical profiling of the active fractions of two brown algal species by ultra-high resolution mass spectrometry (FT-ICR-MS) revealed possible candidate molecules. A database query of these molecules led us to groups of compounds with structural similarities, which are suggested to be responsible for the observed activity. Our work demonstrates the versatility and power of cytological profiling for the bioprospecting of unknown biological resources and highlights Red Sea algae as a source of bioactives that may serve as a starting point for further studies.

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.

Traversing the fungal terpenome

PubMed Central

Quin, Maureen B.; Flynn, Christopher M.; Schmidt-Dannert, Claudia

2014-01-01

Fungi (Ascomycota and Basidiomycota) are prolific producers of structurally diverse terpenoid compounds. Classes of terpenoids identified in fungi include the sesqui-, di- and triterpenoids. Biosynthetic pathways and enzymes to terpenoids from each of these classes have been described. These typically involve the scaffold generating terpene synthases and cyclases, and scaffold tailoring enzymes such as e.g. cytochrome P450 monoxygenases, NAD(P)+ and flavin dependent oxidoreductases, and various group transferases that generate the final bioactive structures. The biosynthesis of several sesquiterpenoid mycotoxins and bioactive diterpenoids has been well-studied in Ascomycota (e.g. filamentous fungi). Little is known about the terpenoid biosynthetic pathways in Basidiomycota (e.g. mushroom forming fungi), although they produce a huge diversity of terpenoid natural products. Specifically, many trans-humulyl cation derived sesquiterpenoid natural products with potent bioactivities have been isolated. Biosynthetic gene clusters responsible for the production of trans-humulyl cation derived protoilludanes, and other sesquiterpenoids, can be rapidly identified by genome sequencing and bioinformatic methods. Genome mining combined with heterologous biosynthetic pathway refactoring has the potential to facilitate discovery and production of pharmaceutically relevant fungal terpenoids. PMID:25171145

Antioxidant activity and bioactive compounds of lettuce improved by espresso coffee residues.

PubMed

Cruz, Rebeca; Gomes, Teresa; Ferreira, Anabela; Mendes, Eulália; Baptista, Paula; Cunha, Sara; Pereira, José Alberto; Ramalhosa, Elsa; Casal, Susana

2014-02-15

The antioxidant activity and individual bioactive compounds of lettuce, cultivated with 2.5-30% (v/v) of fresh or composted espresso spent coffee grounds, were assessed. A progressive enhancement of lettuce's antioxidant capacity, evaluated by radical scavenging effect and reducing power, was exhibited with the increment of fresh spent coffee amounts, while this pattern was not so clear with composted treatments. Total reducing capacity also improved, particularly for low spent coffee concentrations. Additionally, very significant positive correlations were observed for all carotenoids in plants from fresh spent coffee treatments, particularly for violaxanthin, evaluated by HPLC. Furthermore, chlorophyll a was a good discriminating factor between control group and all spent coffee treated samples, while vitamin E was not significantly affected. Espresso spent coffee grounds are a recognised and valuable source of bioactive compounds, proving herein, for the first time, to potentiate the antioxidant pool and quality of the vegetables produced. Copyright © 2013 Elsevier Ltd. All rights reserved.

Efficient use of shrimp waste: present and future trends.

PubMed

Kandra, Prameela; Challa, Murali Mohan; Jyothi, Hemalatha Kalangi Padma

2012-01-01

The production of shrimp waste from shrimp processing industries has undergone a dramatic increase in recent years. Continued production of this biomaterial without corresponding development of utilizing technology has resulted in waste collection, disposal, and pollution problems. Currently used chemical process releases toxic chemicals such as HCl, acetic acid, and NaOH into aquatic ecosystem as byproducts which will spoil the aquatic flora and fauna. Environmental protection regulations have become stricter. Now, there is a need to treat and utilize the waste in most efficient manner. The shrimp waste contains several bioactive compounds such as chitin, pigments, amino acids, and fatty acids. These bioactive compounds have a wide range of applications including medical, therapies, cosmetics, paper, pulp and textile industries, biotechnology, and food applications. This current review article present the utilization of shrimp waste as well as an alternative technology to replace hazardous chemical method that address the future trends in total utilization of shrimp waste for recovery of bioactive compounds.

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.

Direct isolation of flavonoids from plants using ultra-small anatase TiO2 nanoparticles

PubMed Central

Kurepa, Jasmina; Nakabayashi, Ryo; Paunesku, Tatjana; Suzuki, Makoto; Saito, Kazuki; Woloschak, Gayle E.; Smalle, Jan A.

2013-01-01

Summary Surface functionalization of nanoparticles has become an important tool for the in vivo delivery of bioactive agents to their target sites. Here we describe the reverse strategy, nanoharvesting, in which nanoparticles are used as a tool to isolate and enrich bioactive compounds from living cells. Anatase TiO2 nanoparticles smaller than 20 nm form strong bonds with molecules carrying enediol and especially catechol groups. We show that these nanoparticles can enter plant cells, conjugate enediol and catechol group-rich flavonoids in situ, and exit plant cells as flavonoid-nanoparticle conjugates. The source plant tissues remain viable after treatment. As predicted by the surface chemistry of anatase TiO2 nanoparticles, the quercetin-based flavonoids were enriched amongst the nanoharvested flavonoid species. Nanoharvesting eliminates the use of organic solvents, allows spectral identification of the isolated compounds, and offers a new avenue for the use of nanomaterials for the coupled isolation and testing of bioactive properties of plant-made compounds. PMID:24147867

Influence of Cooking Methods on Bioactive Compound Content and Antioxidant Activity of Brussels Sprouts.

PubMed

Hwang, Eun-Sun

2017-12-01

The effects of different cooking methods on total bioactive compound content were determined, and in vitro antioxidant activity in 80% ethanolic extracts of Brussels sprouts was evaluated by spectrophotometric methods. Compared to uncooked, steamed, and microwaved Brussels sprouts extracted with 80% ethanol contained higher amounts of total polyphenols. Uncooked Brussels sprouts contained the highest amounts of total flavonoids. Microwaved Brussels sprouts contained the highest amounts of total carotenoids (0.35 mg/g) and chlorophylls (3.01 mg/g), followed by steamed and uncooked samples. Uncooked fresh Brussels sprouts showed the highest antioxidant activity followed by microwaved and steamed sprouts. Antioxidant activity was measured with the 2,2-diphenyl-1-picrylhydrazyl, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and hydroxyl racial scavenging assays as well as the reducing power activity assay, and antioxidant activity was found to increase in a concentration-dependent manner. Based on these results, cooking or heat treatment may decrease antioxidant activities, although their effect on bioactive compound content remains controversial.

Transesterification of PHA to oligomers covalently bonded with (bio)active compounds containing either carboxyl or hydroxyl functionalities.

PubMed

Kwiecień, Iwona; Radecka, Iza; Kowalczuk, Marek; Adamus, Grażyna

2015-01-01

This manuscript presents the synthesis and structural characterisation of novel biodegradable polymeric controlled-release systems of pesticides with potentially higher resistance to weather conditions in comparison to conventional forms of pesticides. Two methods for the preparation of pesticide-oligomer conjugates using the transesterification reaction were developed. The first method of obtaining conjugates, which consist of bioactive compounds with the carboxyl group and polyhydroxyalkanoates (PHAs) oligomers, is "one-pot" transesterification. In the second method, conjugates of bioactive compounds with hydroxyl group and polyhydroxyalkanoates oligomers were obtained in two-step method, through cyclic poly(3-hydroxybutyrate) oligomers. The obtained pesticide-PHA conjugates were comprehensively characterised using GPC, 1H NMR and mass spectrometry techniques. The structural characterisation of the obtained products at the molecular level with the aid of mass spectrometry confirmed that both of the synthetic strategies employed led to the formation of conjugates in which selected pesticides were covalently bonded to PHA oligomers via a hydrolysable ester bond.

Profile of bioactive compounds from grape pomace (Vitis vinifera and Vitis labrusca) by spectrophotometric, chromatographic and spectral analyses.

PubMed

Ribeiro, L F; Ribani, R H; Francisco, T M G; Soares, A A; Pontarolo, R; Haminiuk, C W I

2015-12-15

The aim of this study was to characterize grape pomace (GP) from winemaking byproducts of different grape samples (Cabernet Sauvignon-CS; Merlot-ME; Mix composed of 65% Bordeaux, 25% Isabel and 10% BRS Violet-MI and Terci-TE) with a view to exploiting its potential as a source of bioactive compounds and an alternative to the reuse of waste. Bioactive compounds such as individual phenolic compounds and polyunsaturated fatty acids (PUFA) were identified and quantified by spectrophotometric, chromatographic and spectral analyses. The sample of MI had the highest concentrations for total phenolic compounds and total flavonoids, while TE had the highest content for total monomeric anthocyanins. For all samples it was possible to identify 13 different anthocyanins by high performance liquid chromatography (HPLC) and mass spectrometry (MS). Moreover, the GP samples showed phenolic acids; flavan-3-ols such as catechin; flavonols such as quercetin, rutin and kaempferol; and stilbenes such as trans-resveratrol. Therefore, grape pomace can be considered a source for the recovery of phenolic compounds having antioxidant activity as well as a rich source of PUFA. Thus it can be used as an ingredient in the development of new food products, since it is suitable for human consumption, and a viable alternative both to adding nutritional value to food and to reduce environmental contamination. Copyright © 2015. Published by Elsevier B.V.

Identification of Secondary Metabolite Gene Clusters in the Pseudovibrio Genus Reveals Encouraging Biosynthetic Potential toward the Production of Novel Bioactive Compounds.

PubMed

Naughton, Lynn M; Romano, Stefano; O'Gara, Fergal; Dobson, Alan D W

2017-01-01

Increased incidences of antimicrobial resistance and the emergence of pan-resistant 'superbugs' have provoked an extreme sense of urgency amongst researchers focusing on the discovery of potentially novel antimicrobial compounds. A strategic shift in focus from the terrestrial to the marine environment has resulted in the discovery of a wide variety of structurally and functionally diverse bioactive compounds from numerous marine sources, including sponges. Bacteria found in close association with sponges and other marine invertebrates have recently gained much attention as potential sources of many of these novel bioactive compounds. Members of the genus Pseudovibrio are one such group of organisms. In this study, we interrogate the genomes of 21 Pseudovibrio strains isolated from a variety of marine sources, for the presence, diversity and distribution of biosynthetic gene clusters (BGCs). We expand on results obtained from antiSMASH analysis to demonstrate the similarity between the Pseudovibrio -related BGCs and those characterized in other bacteria and corroborate our findings with phylogenetic analysis. We assess how domain organization of the most abundant type of BGCs present among the isolates (Non-ribosomal peptide synthetases and Polyketide synthases) may influence the diversity of compounds produced by these organisms and highlight for the first time the potential for novel compound production from this genus of bacteria, using a genome guided approach.

Rapid screening of bioactive compounds from natural products by integrating 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays.

PubMed

Zhang, Yufeng; Xiao, Shun; Sun, Lijuan; Ge, Zhiwei; Fang, Fengkai; Zhang, Wen; Wang, Yi; Cheng, Yiyu

2013-05-13

A high throughput method was developed for rapid screening and identification of bioactive compounds from traditional Chinese medicine, marine products and other natural products. The system, integrated with five-channel chromatographic separation and dual UV-MS detection, is compatible with in vitro 96-well microplate based bioassays. The stability and applicability of the proposed method was validated by testing radical scavenging capability of a mixture of seven known compounds (rutin, dihydroquercetin, salvianolic acid A, salvianolic acid B, glycyrrhizic acid, rubescensin A and tangeretin). Moreover, the proposed method was successfully applied to the crude extracts of traditional Chinese medicine and a marine sponge from which 12 bioactive compounds were screened and characterized based on their anti-oxidative or anti-tumor activities. In particular, two diterpenoid derivatives, agelasine B and (-)-agelasine D, were identified for the first time as anti-tumor compounds from the sponge Agelas mauritiana, showing a considerable activity toward MCF-7 cells (IC50 values of 7.84±0.65 and 10.48±0.84 μM, respectively). Our findings suggested that the integrated system of 5-channel parallel chromatography coupled with on-line mass spectrometry and microplate based assays can be a versatile and high efficient approach for the discovery of active compounds from natural products. Copyright © 2013 Elsevier B.V. All rights reserved.

Antifouling potential of Nature-inspired sulfated compounds

NASA Astrophysics Data System (ADS)

Almeida, Joana R.; Correia-da-Silva, Marta; Sousa, Emília; Antunes, Jorge; Pinto, Madalena; Vasconcelos, Vitor; Cunha, Isabel

2017-02-01

Natural products with a sulfated scaffold have emerged as antifouling agents with low or nontoxic effects to the environment. In this study 13 sulfated polyphenols were synthesized and tested for antifouling potential using the anti-settlement activity of mussel (Mytilus galloprovincialis) plantigrade post-larvae and bacterial growth inhibition towards four biofilm-forming bacterial strains. Results show that some of these Nature-inspired compounds were bioactive, particularly rutin persulfate (2), 3,6-bis(β-D-glucopyranosyl) xanthone persulfate (6), and gallic acid persulfate (12) against the settlement of plantigrades. The chemical precursors of sulfated compounds 2 and 12 were also tested for anti-settlement activity and it was possible to conclude that bioactivity is associated with sulfation. While compound 12 showed the most promising anti-settlement activity (EC50 = 8.95 μg.mL-1), compound 2 also caused the higher level of growth inhibition in bacteria Vibrio harveyi (EC20 = 12.5 μg.mL-1). All the three bioactive compounds 2, 6, and 12 were also found to be nontoxic to the non target species Artemia salina (<10% mortality at 250 μM) and Vibrio fischeri (LC50 > 1000 μg.mL-1). This study put forward the relevance of synthesizing non-natural sulfated small molecules to generate new nontoxic antifouling agents.

Antifouling potential of Nature-inspired sulfated compounds

PubMed Central

Almeida, Joana R.; Correia-da-Silva, Marta; Sousa, Emília; Antunes, Jorge; Pinto, Madalena; Vasconcelos, Vitor; Cunha, Isabel

2017-01-01

Natural products with a sulfated scaffold have emerged as antifouling agents with low or nontoxic effects to the environment. In this study 13 sulfated polyphenols were synthesized and tested for antifouling potential using the anti-settlement activity of mussel (Mytilus galloprovincialis) plantigrade post-larvae and bacterial growth inhibition towards four biofilm-forming bacterial strains. Results show that some of these Nature-inspired compounds were bioactive, particularly rutin persulfate (2), 3,6-bis(β-D-glucopyranosyl) xanthone persulfate (6), and gallic acid persulfate (12) against the settlement of plantigrades. The chemical precursors of sulfated compounds 2 and 12 were also tested for anti-settlement activity and it was possible to conclude that bioactivity is associated with sulfation. While compound 12 showed the most promising anti-settlement activity (EC50 = 8.95 μg.mL−1), compound 2 also caused the higher level of growth inhibition in bacteria Vibrio harveyi (EC20 = 12.5 μg.mL−1). All the three bioactive compounds 2, 6, and 12 were also found to be nontoxic to the non target species Artemia salina (<10% mortality at 250 μM) and Vibrio fischeri (LC50 > 1000 μg.mL−1). This study put forward the relevance of synthesizing non-natural sulfated small molecules to generate new nontoxic antifouling agents. PMID:28205590

Comparative proteomics and protein profile related to phenolic compounds and antioxidant activity in germinated Oryza sativa 'KDML105' and Thai brown rice 'Mali Daeng' for better nutritional value.

PubMed

Maksup, Sarunyaporn; Pongpakpian, Sarintip; Roytrakul, Sittiruk; Cha-Um, Suriyan; Supaibulwatana, Kanyaratt

2018-01-01

Brown rice (BR) and germinated brown rice (GBR) are considered as prime sources of carbohydrate and bioactive compounds for more than half of the populations worldwide. Several studies have reported on the proteomics of BR and GBR; however, the proteomic profiles related to the synthesis of bioactive compounds are less well documented. In the present study, BR and GBR were used in a comparative analysis of the proteomic and bioactive compound profiles for two famous Thai rice varieties: Khao Dawk Mali 105 (KDML) and Mali Daeng (MD). The proteomes of KDML and MD revealed differences in the expression patterns of proteins after germination. Total phenolic compound content, anthocyanin contents and antioxidant activity of red rice MD was approximately 2.6-, 2.2- and 9.2-fold higher, respectively, compared to that of the white rice KDML. Moreover, GBR of MD showed higher total anthocyanin content and greater antioxidant activity, which is consistent with the increase expression of several proteins involved in the biosynthesis of phenolic compounds and protection against oxidative stress. Red rice MD exhibits higher nutrient values compared to white rice KDML and the appropriate germination of brown rice could represent a method for improving health-related benefits. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

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.

Naturally occurring bioactive compounds from four repellent essential oils against Bemisia tabaci whiteflies.

PubMed

Deletre, Emilie; Chandre, Fabrice; Barkman, Barbara; Menut, Chantal; Martin, Thibaud

2016-01-01

In tropical countries, netting is an effective sustainable tool for protecting horticultural crops against Lepidoptera, although not against small pests such as Bemisia tabaci, while smaller mesh netting can be used in temperate regions. A solution is to combine a net with a repellent. Previously we identified repellent essential oils: lemongrass (Cymbopogon citratus), cinnamon (Cinnamomum zeylanicum), cumin (Cuminum cyminum) and citronella (Cymbopogon winternarius). The present study was designed to identify the active compounds of these essential oils, characterise their biological activity and examine their potential for coating nets. We investigated the efficiency and toxicity of nets dipped in different solutions. We then studied the repellent effect with an olfactometer and the irritant effect by videotracking. Geraniol and citronellol were the most promising net coatings owing to their repellent effect. The repellency, irritancy or toxicity varied with the product and concentration, and these features were independent, indicating that the repellent and the irritant/toxic mechanisms were not the same. The combined effects of these different compounds account for the bioactivity of the mixture, suggesting interactions between the compounds. This new sustainable strategy for protecting vegetable crops against whiteflies is discussed, in addition to the use of companion plants that could produce such bioactive compounds. © 2015 Society of Chemical Industry.

Germinated brown rice and its bio-functional compounds.

PubMed

Cho, Dong-Hwa; Lim, Seung-Taik

2016-04-01

Brown rice (BR) contains bran layers and embryo, where a variety of nutritional and biofunctional components, such as dietary fibers, γ-oryzanol, vitamins, and minerals, exist. However, BR is consumed less than white rice because it has an inferior eating texture when cooked. Germination is one of the techniques used to improve the texture of the cooked BR. In addition, it induces numerous changes in the composition and chemical structure of the bioactive components. Moreover, many studies reported that the germination could induce the formation of new bioactive compounds, such as gamma-aminobutyric acid (GABA). The consumption of germinated brown rice (GBR) is increasing in many Asian countries because of its improved eating quality and potential health-promoting functions. However, there is still a lack of studies on the compositional and functional changes of the bioactive components during germination. This review contains recent research findings, especially on the bioactive components in GBR. Copyright © 2015 Elsevier Ltd. All rights reserved.

Quantification of bioactive compounds in pulps and by-products of tropical fruits from Brazil.

PubMed

Ribeiro da Silva, Larissa Morais; Teixeira de Figueiredo, Evania Altina; Silva Ricardo, Nagila Maria Pontes; Pinto Vieira, Icaro Gusmao; Wilane de Figueiredo, Raimundo; Brasil, Isabella Montenegro; Gomes, Carmen L

2014-01-15

This study aimed to quantify the levels of resveratrol, coumarin, and other bioactives in pulps and by-products of twelve tropical fruits from Brazil obtained during pulp production process. Pineapple, acerola, monbin, cashew apple, guava, soursop, papaya, mango, passion fruit, surinam cherry, sapodilla, and tamarind pulps were evaluated as well as their by-products (peel, pulp's leftovers, and seed). Total phenolic, anthocyanins, yellow flavonoids, β-carotene and lycopene levels were also determined. Resveratrol was identified in guava and surinam cherry by-products and coumarin in passion fruit, guava and surinam cherry by-products and mango pulp. These fruit pulp and by-products could be considered a new natural source of both compounds. Overall, fruit by-products presented higher (P<0.05) bioactive content than their respective fruit pulps. This study provides novel information about tropical fruits and their by-products bioactive composition, which is essential for the understanding of their nutraceutical potential and future application in the food industry. Published by Elsevier Ltd.

Chemical features of Ganoderma polysaccharides with antioxidant, antitumor and antimicrobial activities.

PubMed

Ferreira, Isabel C F R; Heleno, Sandrina A; Reis, Filipa S; Stojkovic, Dejan; Queiroz, Maria João R P; Vasconcelos, M Helena; Sokovic, Marina

2015-06-01

Ganoderma genus comprises one of the most commonly studied species worldwide, Ganoderma lucidum. However, other Ganoderma species have been also reported as important sources of bioactive compounds. Polysaccharides are important contributors to the medicinal properties reported for Ganoderma species, as demonstrated by the numerous publications, including reviews, on this matter. Yet, what are the chemical features of Ganoderma polysaccharides that have bioactivity? In the present manuscript, the chemical features of Ganoderma polysaccharides with reported antioxidant, antitumor and antimicrobial activities (the most studied worldwide) are analyzed in detail. The composition of sugars (homo- versus hetero-glucans and other polysaccharides), type of glycosidic linkages, branching patterns, and linkage to proteins are discussed. Methods for extraction, isolation and identification are evaluated and, finally, the bioactivity of polysaccharidic extracts and purified compounds are discussed. The integration of data allows deduction of structure-activity relationships and gives clues to the chemical aspects involved in Ganoderma bioactivity. Copyright © 2014 Elsevier Ltd. All rights reserved.

Structural Elucidation and Molecular Docking of a Novel Antibiotic Compound from Cyanobacterium Nostoc sp. MGL001

PubMed Central

Niveshika; Verma, Ekta; Mishra, Arun K.; Singh, Angad K.; Singh, Vinay K.

2016-01-01

Cyanobacteria are rich source of array of bioactive compounds. The present study reports a novel antibacterial bioactive compound purified from cyanobacterium Nostoc sp. MGL001 using various chromatographic techniques viz. thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Further characterization was done using electrospray ionization mass spectroscopy (ESIMS) and nuclear magnetic resonance (NMR) and predicted structure of bioactive compound was 9-Ethyliminomethyl-12-(morpholin - 4 - ylmethoxy) -5, 8, 13, 16–tetraaza–hexacene - 2, 3 dicarboxylic acid (EMTAHDCA). Structure of EMTAHDCA clearly indicated that it is a novel compound that was not reported in literature or natural product database. The compound exhibited growth inhibiting effects mainly against the gram negative bacterial strains and produced maximum zone of inhibition at 150 μg/mL concentration. The compound was evaluated through in silico studies for its ability to bind 30S ribosomal fragment (PDB ID: 1YRJ, 1MWL, 1J7T, and 1LC4) and OmpF porin protein (4GCP, 4GCQ, and 4GCS) which are the common targets of various antibiotic drugs. Comparative molecular docking study revealed that EMTAHDCA has strong binding affinity for these selected targets in comparison to a number of most commonly used antibiotics. The ability of EMTAHDCA to bind the active sites on the proteins and 30S ribosomal fragments where the antibiotic drugs generally bind indicated that it is functionally similar to the commercially available drugs. PMID:27965634

Comparison and Analysis of Toxcast Data with In Vivo Data for ...

EPA Pesticide Factsheets

The ToxCast program has generated a great wealth of in vitro high throughput screening (HTS) data on a large number of compounds, providing a unique resource of information on the bioactivity of these compounds. However, analysis of these data are ongoing, and interpretation and use of the ToxCast data such as for safety assessment of food related compounds remains undetermined. To fill this gap, we conducted a case study of 2 food-related compounds to better understand the ToxCast data and its potential use in chemical safety assessment by comparison between ToxCast and traditional, in vivo toxicology data using the Risk21 approach. Risk21 is an exposure driven flexible risk assessment framework developed by ILSI HESI. Prior work (Karmaus et. al., 2016) looking at all food-relevant compounds in ToxCast showed that food contact substances had high bioactivity in ToxCast assays. To better understand these chemicals based on their indirect food use, exposure and availability of traditional toxicology data, two compounds, dibutyltin dichloride and sodium pyrithione, were selected from a list of the food contact substances with the greatest activity in ToxCast. Exposure and hazard data were compiled and analyzed for both compounds. Comparison between in vitro HTS and in vivo data for sodium pyrithione showed that concentrations that elicited bioactivity in ToxCast assays corresponded to low- and no- observed adverse effect doses in animals. For dibutyltin dichlori

Bioactive compounds and quality parameters of natural cloudy lemon juices.

PubMed

Uçan, Filiz; Ağçam, Erdal; Akyildiz, Asiye

2016-03-01

In this study, bioactive compounds (phenolic and carotenoid) and some quality parameters (color, browning index and hydroxymethylfurfural (HMF)) of natural cloudy lemon juice, pasteurized (90 °C/15 s) and storage stability of concentrated lemon juice (-25 °C/180 days) were carried out. Fifteen phenolic compounds were determined in the lemon juice and the most abounded phenolic compounds were hesperidin, eriocitrin, chlorogenic acid and neoeriocitrin. In generally, phenolic compound concentrations of lemon juice samples increased after the pasteurization treatment. Four carotenoid compounds (β-carotene, β-cryptoxanthin, lutein and zeaxanthin) were detected in natural cloudy lemon juice. Lutein and β-cryptoxanthin were the most abounded carotenoid compounds in the lemon juice. Color values of the lemon juices were not affected by processing and storage periods. HMF and browning index of the lemon juices increased with concentration and storage. According to the results, storing at -25 °C was considered as sufficient for acceptable quality limits of natural cloudy lemon juice.

The bioactive compounds and antioxidant activity of ethanol and ethyl ecetate extracts of Candi Banana (Musa paradisiaca)

NASA Astrophysics Data System (ADS)

Laeliocattleya, R. A.; Estiasih, T.; Griselda, G.; Muchlisyiyah, J.

2018-03-01

Banana has various benefits for health. One local variety of banana is candi banana (Musa paradisiaca). The aim of this research was to study the content of the bioactive compounds of phenolics, flavonoids, tannin, carotenoids and the antioxidant activity of extract ethanol and ethyl acetate of candi banana. Powdered candi banana was extracted using ethanol and ethyl acetate in an ultrasonic bath. The results showed that the content of phenolics, flavonoids, tannin and carotenoids in ethanol extract were 58.76 ± 3.19 mg/kg, 416.08 ± 18.79 mg/kg, 209.83 ± 15.87 mg/kg and 74.55 ± 4.31 mg/kg, respectively. The content of phenolics, flavonoids, tannin and carotenoids in ethyl acetate extract were 0.83 ± 0.12 mg/kg, 4.31 ± 0.66 mg/kg, 49.97 ± 2.43 mg/kg and 304.40 ± 16.62 mg/kg. While the antioxidant activity (IC50) of ethanol extract and ethyl acetate were 3374.13 ± 123.46 ppm and 40318.19 ± 1014.90 ppm. This research showed that type of solvents of ethanol and ethyl acetate affected the content of bioactive compounds and antioxidant activity of candi banana. The antioxidant activity of ethanol extract was higher than that of ethyl acetate extract. It showed that ethanol was a better solvent than ethyl acetate to extract bioactive compounds in candi banana.

Effect of high-hydrostatic pressure and moderate-intensity pulsed electric field on plum.

PubMed

García-Parra, J; González-Cebrino, F; Delgado-Adámez, J; Cava, R; Martín-Belloso, O; Élez-Martínez, P; Ramírez, R

2018-03-01

Moderate intensity pulse electric fields were applied in plum with the aim to increase bioactive compounds content of the fruit, while high-hydrostatic pressure was applied to preserve the purées. High-hydrostatic pressure treatment was compared with an equivalent thermal treatment. The addition of ascorbic acid during purée manufacture was also evaluated. The main objective of this study was to assess the effects on microorganisms, polyphenoloxidase, color and bioactive compounds of high-hydrostatic pressure, or thermal-processed plum purées made of moderate intensity pulse electric field-treated or no-moderate intensity pulse electric field-treated plums, after processing during storage. The application of moderate intensity pulse electric field to plums slightly increased the levels of anthocyanins and the antioxidant activity of purées. The application of Hydrostatic-high pressure (HHP) increased the levels of bioactive compounds in purées, while the thermal treatment preserved better the color during storage. The addition of ascorbic acid during the manufacture of plum purée was an important factor for the final quality of purées. The color and the bioactive compounds content were better preserved in purées with ascorbic acid. The no inactivation of polyphenoloxidase enzyme with treatments applied in this study affected the stability purées. Probably more intense treatments conditions (high-hydrostatic pressure and thermal treatment) would be necessary to reach better quality and shelf life during storage.

Bioactive compounds: historical perspectives, opportunities, and challenges.

PubMed

Patil, Bhimanagouda S; Jayaprakasha, G K; Chidambara Murthy, K N; Vikram, Amit

2009-09-23

Mom's conventional wisdom of eating fruits and vegetables to lead a healthy life has evolved with scientific, fact-finding research during the past four decades due to advances in science of "Foods for Health". Epidemiological and prospective studies have demonstrated the vital role of fruits, vegetables, and nuts in reducing the risk of cancer and cardiovascular diseases. In recent years, several meta-analyses strongly suggested that by adding one serving of fruits and vegetables to daily diet, the risk of cardiovascular diseases will be decreased up to 7%. The multidisciplinary and partnership efforts of agriculture and medical scientists across the globe stimulated interest in establishing certain interdisciplinary centers and institutes focusing on "Foods for Health". While the consumption of various healthy foods continues, several questions about toxicity, bioavailability, and food-drug interactions of bioactive compounds are yet to be fully understood on the basis of scientific evidence. Recent research on elucidation of the molecular mechanisms to understand the "proof of the concept" will provide the perfect answer when consumers are ready for a "consumer-to-farm" rather than the current "farm-to-consumer" approach. The multidisciplinary research and educational efforts will address the role of healthy foods to improve eye, brain, and heart health while reducing the risk of cancer. Through this connection, this review is an attempt to provide insight and historical perspectives on some of the bioactive compounds from the day of discovery to their current status. The bioactive compounds discussed in this review are flavonoids, carotenoids, curcumin, ascorbic acid, and citrus limonoids.

The influence of different types of preparation (espresso and brew) on coffee aroma and main bioactive constituents.

PubMed

Caprioli, Giovanni; Cortese, Manuela; Sagratini, Gianni; Vittori, Sauro

2015-01-01

Coffee is one of the most popular hot drinks in the world; it may be prepared by several methods, but the most common forms are boiled (brew) and pressurized (espresso). Analytical studies on the substances responsible for the pleasant aroma of roasted coffee have been carried out for more than 100 years. Brew coffee and espresso coffee (EC) have a different and peculiar aroma profile, demonstrating the importance of the brewing process on the final product sensorial quality. Concerning bioactive compounds, the extraction mechanism plays a crucial role. The differences in the composition of coffee brew in chlorogenic acids and caffeine content is the result of the different procedures of coffee preparation. The aim of the present review is to detail how the brewing process affects coffee aroma and composition.

Early interactions between leukocytes and three different potentially bioactive titanium surface modifications.

PubMed

Arvidsson, Anna; Malmberg, Per; Kjellin, Per; Currie, Fredrik; Arvidsson, Martin; Franke Stenport, Victoria

2011-05-01

The aim of the present study was to compare the early interactions between leukocytes and three different surface modifications, suggested as bioactive. Blasted titanium discs were modified by alkali and heat treatment, sodium fluoride treatment, or hydroxyapatite coating. A number of these discs were also immersed in simulated body fluid (SBF) for a week, a treatment which yielded high levels of calcium and phosphate on each surface type. The specimens were exposed for human venous blood for 32 minutes and the respiratory burst response was measured in terms of reactive oxygen species with a luminometer, and coverage of viable cells with a fluorescence microscope after staining steps. The topography, morphology, and chemistry of the surfaces were evaluated with optical interferometry and scanning electron microscopy/energy dispersive X-ray analysis (SEM/EDX). A high respiratory burst response was found for HA coated titanium in comparison with the other surface groups (p < 0.0005). The SBF immersion resulted in an increased respiratory burst response (p < 0.0005) and removed statistically significant differences between the surface groups. Thus, the results in the present study indicate that different titanium surface modifications influence the early inflammatory response differently, and that calcium phosphate compounds increase the inflammatory response. Copyright © 2011 Wiley Periodicals, Inc.

Opuntia ficus-indica (L.) Miller as a source of bioactivity compounds for health and nutrition.

PubMed

Aragona, M; Lauriano, E R; Pergolizzi, S; Faggio, C

2017-08-14

Plants with beneficial properties are known in traditional medicine. Nowadays, in spite of widespread availability of synthetic compounds, the search goes towards natural compounds to lower cost and few side effects. The increasing interest in preventive medicine encourages use of nutraceuticals, bioactive compounds of vegetable origin with important nutritional values. Among the medicinal plants, Opuntia ficus-indica (L.) Miller (Family Cactaceae, subfamily Opuntiodeae, Genus Opuntia, subgenus Platyopuntia, species Opuntia ficus-indica (L.) Miller) is widely known for its beneficial properties. The aim of the present review is to stress the major classes of Opuntia components and their medical interest through emphasis on some of their biological effects, particularly those having the most promising expected health benefits and therapeutic impacts on fish and mammals.

Effect of antioxidant properties of lecithin emulsifier on oxidative stability of encapsulated bioactive compounds.

PubMed

Pan, Yuanjie; Tikekar, Rohan V; Nitin, N

2013-06-25

Oxidation of encapsulated bioactive compounds in emulsions is one of the key challenges that limit shelf life of emulsion containing products. Oxidation in these emulsions is triggered by permeation of free radicals generated at the emulsion interface. The objective of this study was to evaluate the role of antioxidant properties of common emulsifiers (lecithin and Tween 20) in reducing permeation of free radicals across the emulsion interface. Radical permeation rates were correlated with oxidative stability of a model bioactive compound (curcumin) encapsulated in these emulsions. Rate of permeation of peroxyl radicals from the aqueous phase to the oil phase of emulsion was inversely proportional to the antioxidant properties of emulsifiers. The rate of radical permeation was significantly higher (p<0.05) for emulsions stabilized using Tween 20 and oxidized lecithin compared to native lecithin that showed higher antioxidant activity. Free radical permeation rate correlated with stability of curcumin in emulsions and was significantly higher (p<0.05) in lecithin stabilized emulsions as compared to Tween 20 emulsions. Overall, this study demonstrates that antioxidant activity of emulsifiers significantly influences permeation of free radicals across the emulsion interface and the rate of oxidation of bioactive encapsulant. Copyright © 2013 Elsevier B.V. All rights reserved.

Antioxidant Bioactive Compounds Changes in Fruit of Quince Genotypes Over Cold Storage.

PubMed

Moradi, Samira; Koushesh Saba, Mahmoud; Mozafari, Ali Akbar; Abdollahi, Hamid

2016-07-01

Quince fruit has many benefits to human health and is excellent source of bioactive compounds. The fruit of 15 quince genotypes stored at 2 °C for 5 mo to study fruit quality changes during cold storage. Fruit were sampled monthly and stored at 20 °C for 24 h. Fruit ascorbic acid (AA), total phenol (TP), and total flavonoid (TF) concentrations, total antioxidant activity (TAA), flesh browning (FB) incidence, polyphenol oxidase (PPO), peroxidase (POX), and superoxide dismutase (SOD) activities were measured during storage. A high variation in bioactive compounds was observed across genotypes. The range of 26.8 to 44.4 mg/100 g FW for AA, 86.7% to 98.2% for TAA, 157.7 to 380.7 mg GAE 100(-1) g FW for TP, and 5.3 to 10.7 mg/100 g FW for TF were observed across genotypes at harvest time. The overall AA, TAA, TP, TF, and SOD decreased while PPO and POX increased during storage. FB was first observed after 4 mo and increased thereafter while the FB index was different across genotypes. Higher bioactive content may prevent or reduce FB index so that a negative correlation was found between FB and AA, TAA, TP, TF, and SOD. © 2016 Institute of Food Technologists®

Integration of magnetic solid phase fishing and off-line two-dimensional high-performance liquid chromatography-diode array detector-mass spectrometry for screening and identification of human serum albumin binders from Radix Astragali.

PubMed

Zhang, Yuping; Nie, Mingkun; Shi, Shuyun; You, Qingping; Guo, Junfang; Liu, Liangliang

2014-03-01

Radix Astragali is one of the most popular traditional medicinal herb and healthy dietary supplement. Isoflavonoids and astragalosides are the main bioactive ingredients. However, the systematic bioactive component analysis is inadequate so far. Then a facile method based on Fe3O4@SiO2-human serum albumin (Fe3O4@SiO2-HSA) magnetic solid phase fishing integrated with two-dimensional high-performance liquid chromatography-diode array detector-mass spectrometry (2D HPLC-DAD-MS(n)) was developed to fish out and identify HSA binders from Radix Astragali. The immobilized HSA displayed a high stability with 96.2% retained after ten consecutive cycles. 2D HPLC system (size exclusion chromatography×reversed phase chromatography, SEC×RP) were developed and optimised. Forty-seven bioactive compounds including thirty-four isoflavonoids and thirteen astragalosides were screened and identified or tentatively deduced based on their retention time, ultraviolet (UV), accurate molecular weight and diagnostic fragment ions. The results indicated that the integrated method could be widely applied for systematical fishing and identification of bioactive compounds, especially for low-abundance and overlapped compounds, from complex mixtures. Copyright © 2013 Elsevier Ltd. All rights reserved.

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.

Influence of cultivar and ripening time on bioactive compounds and antioxidant properties in Cape gooseberry (Physalis peruviana L.).

PubMed

Bravo, Karent; Sepulveda-Ortega, Stella; Lara-Guzman, Oscar; Navas-Arboleda, Alejandro A; Osorio, Edison

2015-05-01

Cape gooseberry (Physalis peruviana) is an exotic fruit highly valued for its organoleptic properties and bioactive compounds. Considering that the presence of phenolics and ascorbic acid could contribute to its functional capacity, it is important to investigate the quality parameters, bioactive contents and functional properties with respect to genotype and ripening time. In this study the genotype effect was evaluated in 15 cultivars for two different harvest times. Changes during maturation were recorded in two commercial cultivars within seven levels of maturity. Multivariate statistical analysis suggested that phenolic content and ORAC value were mainly affected by harvest time and that ascorbic acid content and DPPH level were mainly affected by genotype. In addition, acidity, phenolic content, ORAC value and inhibition of LDL oxidation decreased with maturity, but soluble solids content, ascorbic acid content, β-carotene content and DPPH-scavenging activity were higher in mature fruits. The phenolic content, ascorbic acid content and antioxidant properties of Cape gooseberry fruit were strongly affected by cultivar, harvest time and maturity state. Consequently, the harvest time must be scheduled carefully to gain the highest proportion of bioactive compounds according to the specific cultivar and the environment where it is grown. © 2014 Society of Chemical Industry.

Bioactive compounds and antioxidant activity of wolfberry infusion

PubMed Central

Sun, Yujing; Rukeya, Japaer; Tao, Wenyang; Sun, Peilong; Ye, Xingqian

2017-01-01

An infusion of the wolfberry (Lycium barbarum L.) is a traditional Asian herbal tea. This is the most commonly consumed form of dried wolfberry worldwide, yet little scientific information on wolfberry infusions is available. We investigated the effects of making infusions with hot water on the color, the content of bioactive compounds (polysaccharides, polyphenols, flavonoids and carotenoids) and the antioxidant ability of wolfberry infusions. The contents of bioactive compounds and the antioxidant activity of a wolfberry infusion increased with increased infusion temperature and time. Total polysaccharides content (TPOC), total polyphenols (TPC), total flavonoids (TFC) and total carotenoids contents (TCC) were important for determining the antioxidant capacity of wolfberry infusions with the contribution to antioxidant activity in the order TPC > TFC > TCC > TPOC. Hierarchical cluster analysis indicated preparation conditions of 100 °C for 1~3 h, 90 °C for 2~3 h and 80 °C for 2.5~3 h were equivalent as regards the value of TPC, TPOC, TFC, TCC, FRAP, DPPH and ABTS. The results of this study suggest the length of time of making a wolfberry infusion in actual real life practice is too short and different dietary habits associated with the intake of wolfberry infusion might provide the same bioactive nutrients. PMID:28102295

Natural products from filamentous fungi and production by heterologous expression.

PubMed

Alberti, Fabrizio; Foster, Gary D; Bailey, Andy M

2017-01-01

Filamentous fungi represent an incredibly rich and rather overlooked reservoir of natural products, which often show potent bioactivity and find applications in different fields. Increasing the naturally low yields of bioactive metabolites within their host producers can be problematic, and yield improvement is further hampered by such fungi often being genetic intractable or having demanding culturing conditions. Additionally, total synthesis does not always represent a cost-effective approach for producing bioactive fungal-inspired metabolites, especially when pursuing assembly of compounds with complex chemistry. This review aims at providing insights into heterologous production of secondary metabolites from filamentous fungi, which has been established as a potent system for the biosynthesis of bioactive compounds. Numerous advantages are associated with this technique, such as the availability of tools that allow enhanced production yields and directing biosynthesis towards analogues of the naturally occurring metabolite. Furthermore, a choice of hosts is available for heterologous expression, going from model unicellular organisms to well-characterised filamentous fungi, which has also been shown to allow the study of biosynthesis of complex secondary metabolites. Looking to the future, fungi are likely to continue to play a substantial role as sources of new pharmaceuticals and agrochemicals-either as producers of novel natural products or indeed as platforms to generate new compounds through synthetic biology.

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.

A Brief Review of Bioactive Metabolites Derived from Deep-Sea Fungi.

PubMed

Wang, Yan-Ting; Xue, Ya-Rong; Liu, Chang-Hong

2015-07-23

Deep-sea fungi, the fungi that inhabit the sea and the sediment at depths of over 1000 m below the surface, have become an important source of industrial, agricultural, and nutraceutical compounds based on their diversities in both structure and function. Since the first study of deep-sea fungi in the Atlantic Ocean at a depth of 4450 m was conducted approximately 50 years ago, hundreds of isolates of deep-sea fungi have been reported based on culture-dependent methods. To date more than 180 bioactive secondary metabolites derived from deep-sea fungi have been documented in the literature. These include compounds with anticancer, antimicrobial, antifungal, antiprotozoal, and antiviral activities. In this review, we summarize the structures and bioactivities of these metabolites to provide help for novel drug development.

A Brief Review of Bioactive Metabolites Derived from Deep-Sea Fungi

PubMed Central

Wang, Yan-Ting; Xue, Ya-Rong; Liu, Chang-Hong

2015-01-01

Deep-sea fungi, the fungi that inhabit the sea and the sediment at depths of over 1000 m below the surface, have become an important source of industrial, agricultural, and nutraceutical compounds based on their diversities in both structure and function. Since the first study of deep-sea fungi in the Atlantic Ocean at a depth of 4450 m was conducted approximately 50 years ago, hundreds of isolates of deep-sea fungi have been reported based on culture-dependent methods. To date more than 180 bioactive secondary metabolites derived from deep-sea fungi have been documented in the literature. These include compounds with anticancer, antimicrobial, antifungal, antiprotozoal, and antiviral activities. In this review, we summarize the structures and bioactivities of these metabolites to provide help for novel drug development. PMID:26213949

In vitro antioxidant activity of phenolic-enriched extracts from Zhangping Narcissus tea cake and their inhibition on growth and metastatic capacity of 4T1 murine breast cancer cells* #

PubMed Central

Ying, Le; Kong, De-dong; Gao, Yuan-yuan; Yan, Feng; Wang, Yue-fei; Xu, Ping

2018-01-01

Phenolics, as the main bioactive compounds in tea, have been suggested to have potential in the prevention of various human diseases. However, little is known about phenolics and their bioactivity in Zhangping Narcissue tea cake which is considered the most special kind of oolong tea. To unveil its bioactivity, three phenolic-enriched extracts were obtained from Zhangping Narcissue tea cake using ethyl acetate, n-butanol, and water. Their main chemical compositions and in vitro bioactivity were analyzed by high-performance liquid chromatography (HPLC) and ultra-performance liquid chromatography-mass spectrometry (UPLC-MS). The ethyl acetate fraction (ZEF) consisted of higher content of phenolics, flavonoids, procyanidins, and catechin monomers (including epigallocatechin gallate (EGCG), epicatechin gallate (ECG), and gallocatechin gallate (GCG)) than n-butanol fraction (ZBF) and water fraction (ZWF). ZEF exhibited the strongest antioxidant capacity in vitro due to its abundant bioactive compounds. This was validated by Pearson correlation and hierarchical clustering analyses. ZEF also showed a remarkable inhibition on the growth, migration, and invasion of 4T1 murine breast cancer cells. PMID:29504313

The reducibility of heLa cell viability by Sargassum polycystum extracts

NASA Astrophysics Data System (ADS)

Firdaus, M.; Setijawati, D.; Islam, I.; Nursyam, H.; Kartikaningsih, H.; Yufidasari, H. S.; Prihanto, A. A.; Nurdiani, R.; Jaziri, A. A.

2018-04-01

Cervical cancer is the second largest cause of death-related cancer in women. The efficacy of cancer drugs is still low. Bioactive of brown seaweed has been studied by in vitro and in vivo as anticancer. The aim of this study was to evaluate the cytotoxicity of Sargassum polycystum extracts on HeLa cell, to recognize bioactive on extract and estimate the interaction between the bioactive and target protein. S. polycystum was found from Talango Island waters and HeLa cell was obtained from Indonesian Science Institute. Sample was extracted by ethanol, ethyl acetate and hexane, concentrated and finally, extracts were assayed on HeLa cell. The viability of this cell was quantified on ELISA-Reader. The bioactive compounds of the extract were elucidated by GC-MS. The interaction between bioactive and target protein was evaluated by using in silico method. The result showed that the lowest viability of HeLa cell on n-hexane extracts treatment. The n-hexane extract of this seaweed contained benzenepropanoic acid. This compound reduced HeLa cell viability by reducing of thrombin concentration. In conclusion, the benzene propanoic acid of S. polycystum was the cytotoxic agent and it is potential agent for anti-cervical cancer.

The Pocket-4-Life project, bioavailability and beneficial properties of the bioactive compounds of espresso coffee and cocoa-based confectionery containing coffee: study protocol for a randomized cross-over trial.

PubMed

Mena, Pedro; Tassotti, Michele; Martini, Daniela; Rosi, Alice; Brighenti, Furio; Del Rio, Daniele

2017-11-09

Coffee is an important source of bioactive compounds, including caffeine, phenolic compounds (mainly chlorogenic acids), trigonelline, and diterpenes. Several studies have highlighted the preventive effects of coffee consumption on major cardiometabolic diseases, but the impact of coffee dosage on markers of cardiometabolic risk is not well understood. Moreover, the pool of coffee-derived circulating metabolites and the contribution of each metabolite to disease prevention still need to be evaluated in real-life settings. The aim of this study will be to define the bioavailability and beneficial properties of coffee bioactive compounds on the basis of different levels of consumption, by using an innovative experimental design. The contribution of cocoa-based products containing coffee to the pool of circulating metabolites and their putative bioactivity will also be investigated. A three-arm, crossover, randomized trial will be conducted. Twenty-one volunteers will be randomly assigned to consume three treatments in a random order for 1 month: 1 cup of espresso coffee/day, 3 cups of espresso coffee/day, and 1 cup of espresso coffee plus 2 cocoa-based products containing coffee twice per day. The last day of each treatment, blood and urine samples will be collected at specific time points, up to 24 hours following the consumption of the first product. At the end of each treatment the same protocol will be repeated, switching the allocation group. Besides the bioavailability of the coffee/cocoa bioactive compounds, the effect of the coffee/cocoa consumption on several cardiometabolic risk factors (anthropometric measures, blood pressure, inflammatory markers, trimethylamine N-oxide, nitric oxide, blood lipids, fasting indices of glucose/insulin metabolism, DNA damage, eicosanoids, and nutri-metabolomics) will be investigated. Results will provide information on the bioavailability of the main groups of phytochemicals in coffee and on their modulation by the level of consumption. Findings will also show the circulating metabolites and their bioactivity when coffee consumption is substituted with the intake of cocoa-based products containing coffee. Finally, the effect of different levels of 1-month coffee consumption on cardiometabolic risk factors will be elucidated, likely providing additional insights on the role of coffee in the protection against chronic diseases. ClinicalTrials.gov, NCT03166540 . Registered on May 21, 2017.

Analysis of Antibacterial Activity and Bioactive Compounds of the Giant Mushroom, Macrocybe gigantea (Agaricomycetes), from India.

PubMed

Gaur, Tanvi; Rao, P B

2017-01-01

The antibacterial activity, phenolic profile, and bioactive compounds of fruiting bodies from 2 strains (MA1 and MA2) of the giant mushroom Macrocybe gigantea were evaluated to access their nutraceutical efficacy. The antibacterial activity was higher in MA2 against all selected pathogenic bacteria. Selected phenolics were analyzed by high-performance liquid chromatography coupled with ultraviolet-visible detection. Gallic acid, ferulic acid, quercetin, p-hydroxy benzoic acid, cinnamic acid, and rutin contents (micrograms per gram dry weight) were quantified. Quercetin and rutin were absent in both strains of M. gigantea. M. gigantea MA2 showed relatively higher phenolic content (915.8 μg/g dry weight) than M. gigantea MA1 (854.4 μg/g dry weight). Among the phenolics, gallic acid is found in the largest amount; in M. gigantea MA2, it was 847.9 ± 2.67 μg/g dry weight. Gas chromatography-mass spectrometry analysis showed the presence of bioactive compounds in both strains; most compounds were antibacterial. Thus, the selected strains of M. gigantea can combat oxidative damage and can be used in foods, pharmaceuticals, and cosmetics because of their antioxidant potential.

Recent Research Progress on Garlic (大蒜 dà suàn) as a Potential Anticarcinogenic Agent Against Major Digestive Cancers

PubMed Central

Raghu, Rajasekaran; Lu, Kuan-Hung; Sheen, Lee-Yan

2012-01-01

Garlic (大蒜 dà suàn; the bulb of Allium sativum), bestowed with an array of organosulfur compounds finds its application in treating many ailments including cardiovascular problems, common cold, bacterial and fungal infections and cancer. Numerous epidemiological evidences document the beneficial effects of various bioactive organosulfur compounds of garlic against different types of cancer. Studies involving the animal and cell models indicate garlic bioactive compounds could be effective in treating all the stages of cancer. This review gives an update on the recent pre-clinical and clinical trials, carried out to evaluate the efficacy of various garlic bioactive compounds along with the mechanism of action pertaining to major digestive cancers including liver, gastric and colorectal cancers. The major anti-carcinogenic mechanisms are caspase dependent and/or independent induction of apoptosis, anti-proliferative, anti-metastasis, anti-oxidant and immunomodulative properties. Form the clinical trials an increase in the garlic consumption of 20 g/day reduced the risk of gastric and colorectal cancer. In summary, increased uptake of garlic in diet may prevent the incidence of digestive cancers. PMID:24716132

Evaluation of fruit quality, bioactive compounds and total antioxidant activity of flat peach cultivars.

PubMed

Di Vaio, Claudio; Marallo, Nadia; Graziani, Giulia; Ritieni, Alberto; Di Matteo, Antonio

2015-08-15

Fruit quality traits (fresh weight, dry weight, soluble solids content, titratable acidity and firmness) as well as the content of bioactive compounds (phenolic compounds) and total antioxidant activity were evaluated in four commercial cultivars of peach (Greta, Ufo 4, Rome Star and Ufo 6) and four of nectarine (Neve, Planet 1, Maria Carla and Mesembrina) differing in fruit shape (standard or flat) and flesh colour (white or yellow), important cultivars of the Italian and foreign market. The higher fruit organoleptic quality and nutritional profile of flat peach and nectarine cultivars make them candidates for exploiting new market opportunities and the chance to improve profits of farmers. The results showed that assayed quality parameters differed greatly among cultivars. In particular, flesh color and fruit shape accounted for most of the variation in traits underlying organoleptic and nutritional quality. Overall data suggested that the flat white-fleshed nectarine Planet 1, the yellow-fleshed nectarine Mesembrina and the yellow-fleshed peach Ufo 6, because of their profiles in terms of soluble solids content, titratable acidity and bioactive compounds, have the greatest potential to meet current consumer requirements. © 2014 Society of Chemical Industry.

Microwave-Assisted Drying for the Conservation of Honeybee Pollen.

PubMed

Canale, Angelo; Benelli, Giovanni; Castagna, Antonella; Sgherri, Cristina; Poli, Piera; Serra, Andrea; Mele, Marcello; Ranieri, Annamaria; Signorini, Francesca; Bientinesi, Matteo; Nicolella, Cristiano

2016-05-12

Bee pollen is becoming an important product thanks to its nutritional properties, including a high content of bioactive compounds such as essential amino acids, antioxidants, and vitamins. Fresh bee pollen has a high water content (15%-30% wt %), thus it is a good substrate for microorganisms. Traditional conservation methods include drying in a hot air chamber and/or freezing. These techniques may significantly affect the pollen organoleptic properties and its content of bioactive compounds. Here, a new conservation method, microwave drying, is introduced and investigated. The method implies irradiating the fresh pollen with microwaves under vacuum, in order to reduce the water content without reaching temperatures capable of thermally deteriorating important bioactive compounds. The method was evaluated by taking into account the nutritional properties after the treatment. The analyzed parameters were phenols, flavonoids, with special reference to rutin content, and amino acids. Results showed that microwave drying offers important advantages for the conservation of bee pollen. Irrespective of microwave power and treatment time, phenol and flavonoid content did not vary over untreated fresh pollen. Similarly, rutin content was unaffected by the microwave drying, suggesting that the microwave-assisted drying could be a powerful technology to preserve bioprotective compounds in fresh pollen.

Mulberry (桑葚子 Sang Shèn Zǐ) and its Bioactive Compounds, the Chemoprevention Effects and Molecular Mechanisms In Vitro and In Vivo

PubMed Central

Huang, Hui-Pei; Ou, Ting-Tsz; Wang, Chau-Jong

2013-01-01

Mulberry (桑葚子 sāng shèn zǐ), a traditional Chinese medicine (TCM) in Taiwan, has many bioactive substances, including polyphenol and anthocyanins compounds. Over the past decade, many scientific and medical studies have examined mulberry fruit for its antioxidation and antiinflammation effects both in vitro and in vivo. This review thus focuses on the recent advances of mulberry extracts (MEs) and their applications in the prevention and treatment of human cancer, liver disease, obesity, diabetes, and cardiovascular disease. The ME modulates several apoptotic pathways and matrix metalloproteinases (MMPs) to block cancer progression. Mulberry can increase detoxicated and antioxidant enzyme activities and regulate the lipid metabolism to treat hepatic disease resulting from alcohol consumption, high fat diet, lipopolysaccharides (LPS) and CCl4 exposure. Of the various compounds in ME, cyanidin 3-glucoside (C3G) is the most abundant, and the active compound studied in mulberry research. Herein, the antioxidant and antiinflammatory actions of C3G to improve diabetes and cardiovascular disease are also discussed. These studies provide strong evidence ME may possess the bioactivity to affect the pathogenesis of several chronic diseases. PMID:24716151

Mulberry ( sang shèn zǐ) and its bioactive compounds, the chemoprevention effects and molecular mechanisms in vitro and in vivo.

PubMed

Huang, Hui-Pei; Ou, Ting-Tsz; Wang, Chau-Jong

2013-01-01

Mulberry ( sāng shèn zǐ), a traditional Chinese medicine (TCM) in Taiwan, has many bioactive substances, including polyphenol and anthocyanins compounds. Over the past decade, many scientific and medical studies have examined mulberry fruit for its antioxidation and antiinflammation effects both in vitro and in vivo. This review thus focuses on the recent advances of mulberry extracts (MEs) and their applications in the prevention and treatment of human cancer, liver disease, obesity, diabetes, and cardiovascular disease. The ME modulates several apoptotic pathways and matrix metalloproteinases (MMPs) to block cancer progression. Mulberry can increase detoxicated and antioxidant enzyme activities and regulate the lipid metabolism to treat hepatic disease resulting from alcohol consumption, high fat diet, lipopolysaccharides (LPS) and CCl4 exposure. Of the various compounds in ME, cyanidin 3-glucoside (C3G) is the most abundant, and the active compound studied in mulberry research. Herein, the antioxidant and antiinflammatory actions of C3G to improve diabetes and cardiovascular disease are also discussed. These studies provide strong evidence ME may possess the bioactivity to affect the pathogenesis of several chronic diseases.

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.

Phytotoxicity of triterpenes and limonoids from the Rutaceae and Meliaceae. 5α,6β,8α,12α-Tetrahydro-28-norisotoonafolin--a potent phytotoxin from Toona ciliata.

PubMed

Nebo, Liliane; Varela, Rosa M; Molinillo, José M G; Severino, Vanessa G P; Sarria, André L F; Cazal, Cristiane M; Fernandes, Maria Fátima das Graças; Fernandes, João B; Macías, Francisco A

2015-01-01

Limonoids and triterpenes are the largest groups of secondary metabolites and have notable biological activities. Meliaceae and Rutaceae are known for their high diversity of metabolites, including limonoids, and are distinguished from other families due to the frequent occurrence of such compounds. The increased interest in crop protection associated with the diverse bioactivity of these compounds has made these families attractive in the search for new allelopathic compounds. In the study reported here we evaluated the bioactivity profiles of four triterpenes (1-4) and six limonoids (5-10) from Meliaceae and Rutaceae. The compounds were assessed in a wheat coleoptile bioassay and those that had the highest activities were tested on the standard target species Lepidinum sativum (cress), Lactuca sativa (lettuce), Lycopersicon esculentum (tomato) and Allium cepa (onion). Limonoids showed phytotoxic activity and 5α,6β,8α, 12α- tetrahydro-28-norisotoonafolin (10) and gedunin (5) were the most active, with bioactivity levels similar to, and in some cases better than, those of the commercial herbicide Logran. The results indicate that these products could also be allelochemicals involved in the ecological interactions of these plant species.

Comparative study on gamma irradiation and cold plasma pretreatment for a cellulosic substrate modification with phenolic compounds

NASA Astrophysics Data System (ADS)

Irimia, Anamaria; Ioanid, Ghiocel Emil; Zaharescu, Traian; Coroabă, Adina; Doroftei, Florica; Safrany, Agnes; Vasile, Cornelia

2017-01-01

The efficiency of the activation of the cellulose/chitin mix substrate by cold plasma or γ-radiation exposure in order to modify it with bioactive compounds was studied. The eugenol or vegetable oils such as grape seed oil and rosehip seed oil have been grafted onto activated substrate. The examination of modified cellulose/chitin mix substrate by ATR-FTIR spectroscopy, X-ray photoelectron spectroscopy and scanning electron microscopy confirms that the structural and morphological changes took place in both cases. The grafting degrees of the surface layer estimated from XPS data varied from 31.1% to 58.7% for air cold plasma activation and from 9.7% to 22.8% for γ-irradiation treatment. They depend both on bioactive compound used and procedure of substrate activation. Higher grafting degree are obtain by using vegetable oils than in the case of modification with eugenol and the air cold plasma activation seems to be much efficient than γ-irradiation. By grafting the polymeric substrate with bioactive compounds, antimicrobial and antioxidant properties have been conferred. Such materials can be considered promising for food packaging applications and medical textiles and also the applied procedures are environmental friendly ones.

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

Ginger Phytochemicals Inhibit Cell Growth and Modulate Drug Resistance Factors in Docetaxel Resistant Prostate Cancer Cell.

PubMed

Liu, Chi-Ming; Kao, Chiu-Li; Tseng, Yu-Ting; Lo, Yi-Ching; Chen, Chung-Yi

2017-09-05

Ginger has many bioactive compounds with pharmacological activities. However, few studies are known about these bioactive compounds activity in chemoresistant cells. The aim of the present study was to investigate the anticancer properties of ginger phytochemicals in docetaxel-resistant human prostate cancer cells in vitro. In this study, we isolated 6-gingerol, 10-gingerol, 4-shogaol, 6-shogaol, 10-shogaol, and 6-dehydrogingerdione from ginger. Further, the antiproliferation activity of these compounds was examined in docetaxel-resistant (PC3R) and sensitive (PC3) human prostate cancer cell lines. 6-gingerol, 10-gingerol, 6-shogaol, and 10-shogaol at the concentration of 100 μM significantly inhibited the proliferation in PC3R but 6-gingerol, 6-shogaol, and 10-shogaol displayed similar activity in PC3. The protein expression of multidrug resistance associated protein 1 (MRP1) and glutathione-S-transferase (GSTπ) is higher in PC3R than in PC3. In summary, we isolated the bioactive compounds from ginger. Our results showed that 6-gingerol, 10-gingerol, 6-shogaol, and 10-shogaol inhibit the proliferation of PC3R cells through the downregulation of MRP1 and GSTπ protein expression.

Femtosecond Laser Microfabrication of an Integrated Device for Optical Release and Sensing of Bioactive Compounds

PubMed Central

Ghezzi, Diego; Vazquez, Rebeca Martinez; Osellame, Roberto; Valtorta, Flavia; Pedrocchi, Alessandra; Valle, Giuseppe Della; Ramponi, Roberta; Ferrigno, Giancarlo; Cerullo, Giulio

2008-01-01

Flash photolysis of caged compounds is one of the most powerful approaches to investigate the dynamic response of living cells. Monolithically integrated devices suitable for optical uncaging are in great demand since they greatly simplify the experiments and allow their automation. Here we demonstrate the fabrication of an integrated bio-photonic device for the optical release of caged compounds. Such a device is fabricated using femtosecond laser micromachining of a glass substrate. More in detail, femtosecond lasers are used both to cut the substrate in order to create a pit for cell growth and to inscribe optical waveguides for spatially selective uncaging of the compounds present in the culture medium. The operation of this monolithic bio-photonic device is tested using both free and caged fluorescent compounds to probe its capability of multipoint release and optical sensing. Application of this device to the study of neuronal network activity can be envisaged. PMID:27873888

An ethnobotanical survey of medicinal plants of Laos toward the discovery of bioactive compounds as potential candidates for pharmaceutical development

PubMed Central

Soejarto, D.D.; Gyllenhaal, C.; Kadushin, M.R.; Southavong, B.; Sydara, K.; Bouamanivong, S.; Xaiveu, M.; Zhang, H.-J.; Franzblau, S.G.; Tan, Ghee T.; Pezzuto, J.M.; Riley, M.C.; Elkington, B.G.; Waller, D.P.

2012-01-01

Context An ethnobotany-based approach in the selection of raw plant materials to study was implemented. Objective To acquire raw plant materials using ethnobotanical field interviews as starting point to discover new bioactive compounds from medicinal plants of the Lao People’s Democratic Republic. Methods Using semi-structured field interviews with healers in the Lao PDR, plant samples were collected, extracted, and bio-assayed to detect bioactivity against cancer, HIV/AIDS, TB, malaria. Plant species demonstrating activity were recollected and the extracts subjected to a bioassay-guided isolation protocol to isolate and identify the active compounds. Results Field interviews with 118 healers in 15 of 17 provinces of Lao PDR yielded 753 collections (573 species) with 955 plant samples. Of these 955, 50 extracts demonstrated activity in the anticancer, 10 in the anti-HIV, 30 in the anti-TB, and 52 in the antimalarial assay. Recollection of actives followed by bioassay-guided isolation processes yielded a series of new and known in vitro-active anticancer and antimalarial compounds from 5 species. Discussion Laos has a rich biodiversity, harboring an estimated 8000–11,000 species of plants. In a country highly dependent on traditional medicine for its primary health care, this rich plant diversity serves as a major source of their medication. Conclusions Ethnobotanical survey has demonstrated the richness of plant-based traditional medicine of Lao PDR, taxonomically and therapeutically. Biological assays of extracts of half of the 955 samples followed by in-depth studies of a number of actives have yielded a series of new bioactive compounds against the diseases of cancer and malaria. PMID:22136442

Ilex kaushue and Its Bioactive Component 3,5-Dicaffeoylquinic Acid Protected Mice from Lipopolysaccharide-Induced Acute Lung Injury

PubMed Central

Chen, Yu-Li; Hwang, Tsong-Long; Yu, Huang-Ping; Fang, Jia-You; Chong, Kowit Yu; Chang, Yao-Wen; Chen, Chun-Yu; Yang, Hsuan-Wu; Chang, Wen-Yi; Hsieh, Pei-Wen

2016-01-01

Acute lung injury (ALI) is a severe respiratory disease with high mortality rates worldwide. Recent reports suggest that human neutrophil elastase (HNE) plays a key role in the inflammatory response that is characteristic of ALI, which indicates that the development of HNE inhibitors could be an efficient treatment strategy. In the current study, an enzyme-based screening assay was used to identify effective HNE inhibitors from a number of traditional Chinese medicines (TCMs). Among them, a water extract of Ilex kaushue (IKWE) effectively inhibited HNE activity (IC50, 11.37 ± 1.59 μg/mL). Using bioactivity-guided fractionation, one new compound and 23 known compounds were identified. Compound 6 (identified as 3,5-dicaffeoylquinic acid; 3,5-DCQA) exerted the most potent and selective inhibitory effect on HNE activity (IC50, 1.86 ± 0.06 μM). In a cell-based assay, 3,5-DCQA not only directly reduced superoxide generation and elastase activity but also attenuated the Src family kinase (SRKs)/Vav signaling pathway in N-formyl-L-Met-L-Leu-L-Phe (fMLF)-stimulated human neutrophils. In an animal disease model, both 3,5-DCQA and standardized IKWE protected against lipopolysaccharide-induced ALI in mice, which provides support for their potential as candidates in the development of new therapeutic agents for neutrophilic inflammatory diseases. PMID:27681838

Antioxidant activity from encapsulated Cinnamaldehyde-Chitosan

NASA Astrophysics Data System (ADS)

Ariestiani, Bonita; Purbowatingrum; Ngadiwiyana; Ismiyarto; Fachriyah, Enny; Nurani, Khikmah

2018-05-01

Cinnamaldehyde compound is a powerful antioxidant agent that can effectively combat the free radicals referred to superoxide anions and hydroxy radicals, as well as other free radicals in in vitro testing. An antioxidant is an electron donor or reductant. antioxidants are also compounds that can inhibit oxidation reactions by binding to free radicals and highly reactive molecules. As a result, cell damage will be inhibited. However, the use of this compound still provides unsatisfactory results due to its degradation during the absorption process. The solution offered to solve the problem is by encapsulated it within chitosan nanoparticles that serve to protect the bioactive compound from degradation, increases of solubility and delivery of a bioactive compound to the target site by using freeze-drying technique. The value of encapsulation efficiency (EE) of cinnamaldyhde which encapsulated within chitosan nanoparticles is about 74,389% also antioxidant activity test showed that cinnamaldehyde encapsulated by nanochitosan could inhibit free radicals of 223.44 in IC50.

Whey-grape juice drink processed by supercritical carbon dioxide technology: Physicochemical characteristics, bioactive compounds and volatile profile.

PubMed

Amaral, Gabriela V; Silva, Eric Keven; Cavalcanti, Rodrigo N; Martins, Carolina P C; Andrade, Luiz Guilherme Z S; Moraes, Jeremias; Alvarenga, Verônica O; Guimarães, Jonas T; Esmerino, Erick A; Freitas, Mônica Q; Silva, Márcia C; Raices, Renata S L; Sant' Ana, Anderson S; Meireles, M Angela A; Cruz, Adriano G

2018-01-15

The effect of supercritical carbon dioxide technology (SCCD, 14, 16, and 18MPa at 35±2°C for 10min) on whey-grape juice drink characteristics was investigated. Physicochemical characterization (pH, titratable acidity, total soluble solids), bioactive compounds (phenolic compounds, anthocyanin, DPPH and ACE activity) and the volatile compounds were performed. Absence of differences were found among treatments for pH, titratable acidity, soluble solids, total anthocyanin and DPPH activity (p-value>0.05). A direct relationship between SCCD pressure and ACE inhibitory activity was observed, with 34.63, 38.75, and 44.31% (14, 16, and 18MPa, respectively). Regards the volatile compounds, it was noted few differences except by the presence of ketones. The findings confirm the SCCD processing as a potential promising technology to the conventional thermal treatment. Copyright © 2017 Elsevier Ltd. All rights reserved.

Benzoquinones and terphenyl compounds as phosphodiesterase-4B inhibitors from a fungus of the order Chaetothyriales (MSX 47445).

PubMed

El-Elimat, Tamam; Figueroa, Mario; Raja, Huzefa A; Graf, Tyler N; Adcock, Audrey F; Kroll, David J; Day, Cynthia S; Wani, Mansukh C; Pearce, Cedric J; Oberlies, Nicholas H

2013-03-22

Three bioactive compounds were isolated from an organic extract of an ascomycete fungus of the order Chaetothyriales (MSX 47445) using bioactivity-directed fractionation as part of a search for anticancer leads from filamentous fungi. Of these, two were benzoquinones [betulinan A (1) and betulinan C (3)], and the third was a terphenyl compound, BTH-II0204-207:A (2). The structures were elucidated using a set of spectroscopic and spectrometric techniques; the structure of the new compound (3) was confirmed via single-crystal X-ray diffraction. Compounds 1-3 were evaluated for cytotoxicity against a human cancer cell panel, for antimicrobial activity against Staphylococcus aureus and Candida albicans, and for phosphodiesterase (PDE4B2) inhibitory activities. The putative binding mode of 1-3 with PDE4B2 was examined using a validated docking protocol, and the binding and enzyme inhibitory activities were correlated.

Bioactivity-guided isolation of anticancer agents from Bauhinia kockiana Korth.

PubMed

Chew, Yik Ling; Lim, Yau Yan; Stanslas, Johnson; Ee, Gwendoline Cheng Lian; Goh, Joo Kheng

2014-01-01

Flowers of Bauhinia kockiana were investigated for their anticancer properties. Gallic acid (1), and methyl gallate (2), were isolated via bioassay-directed isolation, and they exhibited anticancer properties towards several cancer cell lines, examined using MTT cell viability assay. Pyrogallol (3) was examined against the same cancer cell lines to deduce the bioactive functional group of the phenolic compounds. The results showed that the phenolic compounds could exhibit moderate to weak cytotoxicity towards certain cell lines (GI50 30 - 86 µM), but were inactive towards DU145 prostate cancer cell (GI50 > 100 µM). It was observed that pyrogallol moiety was one of the essential functional structures of the phenolic compounds in exhibiting anticancer activity. Also, the carboxyl group of compound 1 was also important in anticancer activity. Examination of the PC-3 cells treated with compound 1 using fluorescence microscopy showed that PC-3 cells were killed by apoptosis.

Stability of lipid encapsulated phenolic acid particles

USDA-ARS?s Scientific Manuscript database

Phenolic compounds such as ferulic acid and p-coumaric acids are potential bioactive additives for use in animal feeds to replace current antioxidants and antimicrobial compounds. These compounds are ubiquitous in plants and may be obtained from commodity grain crops and waste biomass. Encapsulation...

Spectroscopic analysis of phenolic compounds for food and feed formulations

USDA-ARS?s Scientific Manuscript database

Phenolic compounds exhibit several bioactive properties including anti-oxidant, anti-microbial, and anti-fungal characteristics with potential applications as additives in functional food and feed formulations. Phenolic compounds occur in plants as secondary metabolites and may be recovered as a co-...

Fumigant activity of the Psidium guajava var. pomifera (Myrtaceae) essential oil in Drosophila melanogaster by means of oxidative stress.

PubMed

Pinho, Antonio Ivanildo; Wallau, Gabriel Luz; Nunes, Mauro Eugenio Medina; Leite, Nadghia Figueiredo; Tintino, Saulo Relison; da Cruz, Litiele Cezar; da Cunha, Francisco Assis Bezerra; da Costa, José Galberto Martins; Douglas Melo Coutinho, Henrique; Posser, Thais; Franco, Jeferson Luis

2014-01-01

The guava fruit, Psidium guajava var. pomifera (Myrtaceae family), is a native plant from South America. Its leaves and fruits are widely used in popular medicine in tropical and subtropical countries. Drosophila melanogaster has been used as one of the main model organisms in genetic studies since the 1900s. The extensive knowledge about this species makes it one of the most suitable organisms to study many aspects of toxic compound effects. Due to the lack of studies on the effects of the bioactive compounds present in the P. guajava var. pomifera essential oil, we performed a phytochemical characterization by CG-MS and evaluated the toxicity induced by the essential oil in the D. melanogaster insect model. In order to understand the biochemical mechanisms of toxicity, changes on the Nrf2 signaling as well as hallmarks of oxidative stress response were followed in the exposed flies. Our results showed that exposure of insects to the P. guajava oil increased mortality and locomotor deficits in parallel with an oxidative stress response signaling. Therefore, it suggested a bioinsecticidal activity for P. guajava volatile compounds by means of oxidative stress. Further studies are ongoing to identify which oil compounds are responsible for such effect.

Fumigant Activity of the Psidium guajava Var. Pomifera (Myrtaceae) Essential Oil in Drosophila melanogaster by Means of Oxidative Stress

PubMed Central

Pinho, Antonio Ivanildo; Wallau, Gabriel Luz; Nunes, Mauro Eugenio Medina; Leite, Nadghia Figueiredo; Tintino, Saulo Relison; da Cruz, Litiele Cezar; da Cunha, Francisco Assis Bezerra; da Costa, José Galberto Martins; Douglas Melo Coutinho, Henrique; Posser, Thais

2014-01-01

The guava fruit, Psidium guajava var. pomifera (Myrtaceae family), is a native plant from South America. Its leaves and fruits are widely used in popular medicine in tropical and subtropical countries. Drosophila melanogaster has been used as one of the main model organisms in genetic studies since the 1900s. The extensive knowledge about this species makes it one of the most suitable organisms to study many aspects of toxic compound effects. Due to the lack of studies on the effects of the bioactive compounds present in the P. guajava var. pomifera essential oil, we performed a phytochemical characterization by CG-MS and evaluated the toxicity induced by the essential oil in the D. melanogaster insect model. In order to understand the biochemical mechanisms of toxicity, changes on the Nrf2 signaling as well as hallmarks of oxidative stress response were followed in the exposed flies. Our results showed that exposure of insects to the P. guajava oil increased mortality and locomotor deficits in parallel with an oxidative stress response signaling. Therefore, it suggested a bioinsecticidal activity for P. guajava volatile compounds by means of oxidative stress. Further studies are ongoing to identify which oil compounds are responsible for such effect. PMID:25478063

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...

In Silico and In Vitro Anticancer Activity of Isolated Novel Marker Compound from Chemically Modified Bioactive Fraction from Curcuma longa (NCCL).

PubMed

Naqvi, Arshi; Malasoni, Richa; Gupta, Swati; Srivastava, Akansha; Pandey, Rishi R; Dwivedi, Anil Kumar

2017-10-01

Turmeric ( Curcuma longa ) is reported to possess wide array of biological activities. Herbal Medicament (HM) is a standardized hexane-soluble fraction of C. longa and is well known for its neuroprotective effect. In this study, we attempted to synthesize a novel chemically modified bioactive fraction from HM (NCCL) along with isolation and characterization of a novel marker compound (I). NCCL was prepared from HM. The chemical structure of the marker compound isolated from NCCL was determined from 1D/2D nuclear magnetic resonance, mass spectroscopy, and Fourier transform infrared. The compound so isolated was subjected to in silico and in vitro screenings to test its inhibitory effect on estrogen receptors. Molecular docking studies revealed that the binding poses of the compound I was energetically favorable. Among NCCL and compound I taken for in vitro studies, NCCL had exhibited good anti-cancer activity over compound I against MCF-7, MDA-MB-231, DU-145, and PC-3 cells. This is the first study about the synthesis of a chemically modified bioactive fraction which used a standardized extract since the preparation of the HM. It may be concluded that NCCL fraction having residual components induce more cell death than compound I alone. Thus, NCCL may be used as a potent therapeutic drug. In the present paper, a standardized hexane soluble fraction of Curcuma longa (HM) was chemically modified to give a novel bioactive fraction (NCCL). A novel marker compound was isolated from NCCL and was characerized using various spectral techniques. The compound so isolated was investigated for in-silico screenings. NCCL and isolated compound was subjected to in-vitro anti-cancer screenings against MCF 7, MDA MB 231 (breast adenocarcinoma) and DU 145 and PC 3 cell lines (androgen independent human prostate cancer cells). The virtual screenings reveals that isolated compound has shown favourable drug like properties. NCCL fraction having residual components induces more cell death in these four cancer cell lines than isolated compound alone. Abbreviations used: HM: Herbal Medicament; NCCL: Chemically modified HM; FT-IR: Fourier transform-infrared spectroscopy; NMR: Nuclear magnetic resonance spectroscopy; MS: Mass spectroscopy; HPLC: High-performance liquid chromatography; ER: Estrogen receptor; MTT: 3-(4,5 dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide; MIC: Minimum inhibitory concentration; TAM: Tamoxifen KBr: Potassium bromide; DMSO: Dimethyl sulfoxide; ACN: Acetonitrile; PDB: Protein Data Bank; PDA: Photodiode array detector.

Bioactive compounds and antioxidant activity in scalded Jalapeño pepper industrial byproduct (Capsicum annuum).

PubMed

Sandoval-Castro, Claudia Jaqueline; Valdez-Morales, Maribel; Oomah, B Dave; Gutiérrez-Dorado, Roberto; Medina-Godoy, Sergio; Espinosa-Alonso, L Gabriela

2017-06-01

Bioactive compounds and antioxidant activity were evaluated from industrial Jalapeño pepper byproducts and simulated non processed byproducts from two Mexican states (Chihuahua and Sinaloa) to determine their value added potential as commercial food ingredients. Aqueous 80% ethanol produced about 13% of dry extract of polar compounds. Total phenolic content increased and capsaicin and dihydrocapsaicin decreased on scalding samples (80 °C, 2 min) without affecting ascorbic acid. The major phenolic compounds, rutin, epicatechin and catechin comprised 90% of the total compounds detected by HPLC of each Jalapeño pepper byproducts. ORAC analysis showed that the origin and scalding process affected the antioxidant activity which correlated strongly with capsaicin content. Although scalding decreased capsaicinoids (up to 42%), phenolic content by (up to 16%), and the antioxidant activity (variable). Jalapeño pepper byproduct is a good source of compounds with antioxidant activity, and still an attractive ingredient to develop useful innovative products with potential food/non-food applications simultaneously reducing food loss and waste.

Crossfit analysis: a novel method to characterize the dynamics of induced plant responses.

PubMed

Jansen, Jeroen J; van Dam, Nicole M; Hoefsloot, Huub C J; Smilde, Age K

2009-12-16

Many plant species show induced responses that protect them against exogenous attacks. These responses involve the production of many different bioactive compounds. Plant species belonging to the Brassicaceae family produce defensive glucosinolates, which may greatly influence their favorable nutritional properties for humans. Each responding compound may have its own dynamic profile and metabolic relationships with other compounds. The chemical background of the induced response is therefore highly complex and may therefore not reveal all the properties of the response in any single model. This study therefore aims to describe the dynamics of the glucosinolate response, measured at three time points after induction in a feral Brassica, by a three-faceted approach, based on Principal Component Analysis. First the large-scale aspects of the response are described in a 'global model' and then each time-point in the experiment is individually described in 'local models' that focus on phenomena that occur at specific moments in time. Although each local model describes the variation among the plants at one time-point as well as possible, the response dynamics are lost. Therefore a novel method called the 'Crossfit' is described that links the local models of different time-points to each other. Each element of the described analysis approach reveals different aspects of the response. The crossfit shows that smaller dynamic changes may occur in the response that are overlooked by global models, as illustrated by the analysis of a metabolic profiling dataset of the same samples.

Crossfit analysis: a novel method to characterize the dynamics of induced plant responses

PubMed Central

2009-01-01

Background Many plant species show induced responses that protect them against exogenous attacks. These responses involve the production of many different bioactive compounds. Plant species belonging to the Brassicaceae family produce defensive glucosinolates, which may greatly influence their favorable nutritional properties for humans. Each responding compound may have its own dynamic profile and metabolic relationships with other compounds. The chemical background of the induced response is therefore highly complex and may therefore not reveal all the properties of the response in any single model. Results This study therefore aims to describe the dynamics of the glucosinolate response, measured at three time points after induction in a feral Brassica, by a three-faceted approach, based on Principal Component Analysis. First the large-scale aspects of the response are described in a 'global model' and then each time-point in the experiment is individually described in 'local models' that focus on phenomena that occur at specific moments in time. Although each local model describes the variation among the plants at one time-point as well as possible, the response dynamics are lost. Therefore a novel method called the 'Crossfit' is described that links the local models of different time-points to each other. Conclusions Each element of the described analysis approach reveals different aspects of the response. The crossfit shows that smaller dynamic changes may occur in the response that are overlooked by global models, as illustrated by the analysis of a metabolic profiling dataset of the same samples. PMID:20015363

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

Aqueous Extract Composition of Spent Ginger (Zingiber officinale var. Amarum) from Essential Oil Distillation

NASA Astrophysics Data System (ADS)

Manuhara, G. J.; Mentari, G. P.; Khasanah, L. U.; Utami, R.

2018-03-01

Ginger (Zingiber officinale var Amarum) is widely used as raw material for essential oil production in Indonesia and contain high functional compounds. After producing essential oil, distillation leave less valuable spent ginger. This research was conducted to determine the bioactive compounds remained in aqueous extract of the spent ginger. The extracts were produced at various combination of temperature (55, 75, 95°C) and duration (15, 30, 45 minutes). The extract composition was observed using Gas Chromatography - Mass Spectrometry analysis. The temperature and time of maceration extraction affected the content of compounds in spent ginger aqueous extracts. The extracts contained four largest components of α-curcumene, α-zingiberene, β-sesquiphellandrene and β-bisabolene. The aqueous extracts from spent ginger contained the compounds which may contribute to distinctive flavor of ginger and also bioactive function.

Current technologies and new insights for the recovery of high valuable compounds from fruits by-products.

PubMed

Ferrentino, Giovanna; Asaduzzaman, Md; Scampicchio, Matteo Mario

2018-02-11

The recovery of high valuable compounds from food waste is becoming a tighten issue in food processing. The large amount of non-edible residues produced by food industries causes pollution, difficulties in the management, and economic loss. The waste produced during the transformation of fruits includes a huge amount of materials such as peels, seeds, and bagasse, whose disposal usually represents a problem. Research over the past 20 years revealed that many food wastes could serve as a source of potentially valuable bioactive compounds, such as antioxidants and vitamins with increasing scientific interest thanks to their beneficial effects on human health. The challenge for the recovery of these compounds is to find the most appropriate and environment friendly extraction technique able to achieve the maximum extraction yield without compromising the stability of the extracted products. Based on this scenario, the aim of the current review is twofold. The first is to give a brief overview of the most important bioactive compounds occurring in fruit wastes. The second is to describe the pro and cons of the most up-to-dated innovative and environment friendly extraction technologies that can be an alternative to the classical solvent extraction procedures for the recovery of valuable compounds from fruit processing. Furthermore, a final section will take into account published findings on the combination of some of these technologies to increase the extracts yields of bioactives.

Phenolics from Garcinia mangostana Inhibit Advanced Glycation Endproducts Formation: Effect on Amadori Products, Cross-Linked Structures and Protein Thiols.

PubMed

Abdallah, Hossam M; El-Bassossy, Hany; Mohamed, Gamal A; El-Halawany, Ali M; Alshali, Khalid Z; Banjar, Zainy M

2016-02-22

Accumulation of Advanced Glycation Endproducts (AGEs) in body tissues plays a major role in the development of diabetic complications. Here, the inhibitory effect of bioactive metabolites isolated from fruit hulls of Garcinia mangostana on AGE formation was investigated through bio-guided approach using aminoguanidine (AG) as a positive control. Including G. mangostana total methanol extract (GMT) in the reaction mixture of bovine serum albumin (BSA) and glucose or ribose inhibited the fluorescent and non-fluorescent AGEs formation in a dose dependent manner. The bioassay guided fractionation of GMT revealed isolation of four bioactive constituents from the bioactive fraction; which were identified as: garcimangosone D (1), aromadendrin-8-C-glucopyranoside (2), epicatechin (3), and 2,3',4,5',6-pentahydroxybenzophenone (4). All the tested compounds significantly inhibited fluorescent and non-fluorescent AGEs formation in a dose dependent manner whereas compound 3 (epicatechin) was found to be the most potent. In search for the level of action, addition of GMT, and compounds 2-4 inhibited fructosamine (Amadori product) and protein aggregation formation in both glucose and ribose. To explore the mechanism of action, it was found that addition of GMT and only compound (3) to reaction mixture increased protein thiol in both glucose and ribose while compounds 1, 2 and 4 only increased thiol in case of ribose. In conclusion, phenolic compounds 1-4 inhibited AGEs formation at the levels of Amadori product and protein aggregation formation through saving protein thiol.

Reversed Phase HPLC-DAD Profiling of Carotenoids, Chlorophylls and Phenolic Compounds in Adiantum capillus-veneris Leaves

NASA Astrophysics Data System (ADS)

Zeb, Alam; Ullah, Fareed

2017-04-01

Adiantum capillus-veneris is important endangered fern species with several medicinal properties. In this study, the leaves samples were extracted and separated using reversed phase HPLC with DAD for carotenoids, chlorophylls and phenolic compounds. Separation of carotenoids and chlorophylls were carried out using a tertiary gradient system of water, MTBE and methanol-water, while a binary gradient system of methanol-water-acetic acid was used for phenolic profiling. Results revealed eight carotenoids, four pheophytins and two chlorophylls. Lutein (806.0 µg/g), chlorophyll b' (410.0 µg/g), chlorophyll a (162.4 µg/g), 9'-Z-neoxanthin (142.8 µg/g) and all-E-violaxanthin (82.2 µg/g)) were present in higher amounts. The relatively high amounts of lutein may be one of the key indicator of beneficial antioxidant properties. The phenolic profile revealed a total of thirteen compounds, namely p-hydroxybenzoic acid, chlorogenic acid, caftaric acid, kaempferol glycosides, p-coumaric acid, rosmarinic acid, 5-caffeoylquinic acid, and quercetin glycosides. Kaempferol-3-sophorotrioside (58.7 mg/g), chlorogenic acid (28.5 mg/g), 5-O-caffeoylquinic acid (18.7 mg/g), coumaric acid (11.2 mg/g) and its derivative (33.1 mg/g) were present in high amounts. These results suggest that the reversed phase HPLC profiling of adiantum leaves provides a better understanding in to the actual composition of bioactive compounds, which may be responsible for possible medicinal properties. Adiantum leaves rich in important bioactive phytochemicals can be used as a potential source of nutraceuticals or as a functional food ingredient.

Reversed Phase HPLC-DAD Profiling of Carotenoids, Chlorophylls and Phenolic Compounds in Adiantum capillus-veneris Leaves

PubMed Central

Zeb, Alam; Ullah, Fareed

2017-01-01

Adiantum capillus-veneris is important endangered fern species with several medicinal properties. In this study, the leaves samples were extracted and separated using reversed phase HPLC with DAD for carotenoids, chlorophylls and phenolic compounds. Separation of carotenoids and chlorophylls were carried out using a tertiary gradient system of water, MTBE and methanol-water, while a binary gradient system of methanol-water-acetic acid was used for phenolic profiling. Results revealed eight carotenoids, four pheophytins, and two chlorophylls. Lutein (806.0 μg/g), chlorophyll b′ (410.0 μg/g), chlorophyll a (162.4 μg/g), 9′-Z-neoxanthin (142.8 μg/g) and all-E-violaxanthin (82.2 μg/g) were present in higher amounts. The relatively high amounts of lutein may be one of the key indicator of beneficial antioxidant properties. The phenolic profile revealed a total of 13 compounds, namely 4-hydroxybenzoic acid, chlorogenic acid, caftaric acid, kaempferol glycosides, p-coumaric acid, rosmarinic acid, 5-caffeoylquinic acid, and quercetin glycosides. Kaempferol-3-sophorotrioside (58.7 mg/g), chlorogenic acid (28.5 mg/g), 5-O-caffeoylquinic acid (18.7 mg/g), coumaric acid (11.2 mg/g), and its derivative (33.1 mg/g) were present in high amounts. These results suggest that the reversed phase HPLC profiling of Adiantum leaves provides a better understanding in to the actual composition of bioactive compounds, which may be responsible for the potential medicinal properties. Adiantum leaves rich in important bioactive phytochemicals can be used as a possible source of nutraceuticals or as a functional food ingredient. PMID:28497036

Reversed Phase HPLC-DAD Profiling of Carotenoids, Chlorophylls and Phenolic Compounds in Adiantum capillus-veneris Leaves.

PubMed

Zeb, Alam; Ullah, Fareed

2017-01-01

Adiantum capillus-veneris is important endangered fern species with several medicinal properties. In this study, the leaves samples were extracted and separated using reversed phase HPLC with DAD for carotenoids, chlorophylls and phenolic compounds. Separation of carotenoids and chlorophylls were carried out using a tertiary gradient system of water, MTBE and methanol-water, while a binary gradient system of methanol-water-acetic acid was used for phenolic profiling. Results revealed eight carotenoids, four pheophytins, and two chlorophylls. Lutein (806.0 μg/g), chlorophyll b ' (410.0 μg/g), chlorophyll a (162.4 μg/g), 9'- Z -neoxanthin (142.8 μg/g) and all- E -violaxanthin (82.2 μg/g) were present in higher amounts. The relatively high amounts of lutein may be one of the key indicator of beneficial antioxidant properties. The phenolic profile revealed a total of 13 compounds, namely 4-hydroxybenzoic acid, chlorogenic acid, caftaric acid, kaempferol glycosides, p-coumaric acid, rosmarinic acid, 5-caffeoylquinic acid, and quercetin glycosides. Kaempferol-3-sophorotrioside (58.7 mg/g), chlorogenic acid (28.5 mg/g), 5- O -caffeoylquinic acid (18.7 mg/g), coumaric acid (11.2 mg/g), and its derivative (33.1 mg/g) were present in high amounts. These results suggest that the reversed phase HPLC profiling of Adiantum leaves provides a better understanding in to the actual composition of bioactive compounds, which may be responsible for the potential medicinal properties. Adiantum leaves rich in important bioactive phytochemicals can be used as a possible source of nutraceuticals or as a functional food ingredient.

Polymethoxyflavones Isolated from the Peel of Miaray Mandarin (Citrus miaray) Have Biofilm Inhibitory Activity in Vibrio harveyi.

PubMed

Uckoo, Ram M; Jayaprakasha, G K; Vikram, Amit; Patil, Bhimanagouda S

2015-08-19

Citrus fruits are a good source of bioactive compounds with numerous beneficial biological activities. In the present study, fruits of the unexplored Miaray mandarin were used for the isolation of 10 bioactive compounds. Dried peels were sequentially extracted with hexane and chloroform in a Soxhlet-type apparatus for 8 h. The extracts were concentrated under vacuum and separated by flash chromatography to obtain nine polymethoxyflavones and a limonoid. The purity of each compound was analyzed by high-performance liquid chromatography (HPLC), and the compounds were identified by spectral analysis using MALDI-TOF-MS and NMR. The isolated compounds were identified as 5-hydroxy-3,7,3',4'-tetramethoxyflavone, 5,6,7,8,4'-pentamethoxyflavone (tangeretin), 3,5,6,7,8,3',4'-heptamethoxyflavone, 5,6,7,8,3',4'-hexamethoxyflavone (nobiletin), 3,5,7,8,3',4'-hexamethoxyflavone, 3,5,7,3',4'-pentamethoxyflavone (pentamethylquercetin), 5,7,4'-trimethoxyflavone, 5,7,8,4'-tetramethoxyflavone, 5,7,8,3',4'-pentamethoxyflavone, and limonin. These compounds were further tested for their ability to inhibit cell-cell signaling and biofilm formation in Vibrio harveyi. Among the evaluated polymethoxyflavones, 3,5,6,7,8,3',4'-heptamethoxyflavone and 3,5,7,8,3',4'-hexamethoxyflavone inhibited autoinducer-mediated cell-cell signaling and biofilm formation. These results suggest that Miaray mandarin fruits are a good source of polymethoxyflavones. This is the first report on the isolation of bioactive compounds from Miaray mandarin and evaluation of their biofilm inhibitory activity as well as isolation of pentamethylquercetin from the Citrus genus.

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

Natural Products from Deep-Sea-Derived Fungi ̶ A New Source of Novel Bioactive Compounds?

PubMed

Daletos, Georgios; Ebrahim, Weaam; Ancheeva, Elena; El-Neketi, Mona; Song, Weiguo; Lin, Wenhan; Proksch, Peter

2018-01-01

Over the last two decades, deep-sea-derived fungi are considered to be a new source of pharmacologically active secondary metabolites for drug discovery mainly based on the underlying assumption that the uniqueness of the deep sea will give rise to equally unprecedented natural products. Indeed, up to now over 200 new metabolites have been identified from deep-sea fungi, which is in support of the statement made above. This review summarizes the new and/or bioactive compounds reported from deepsea- derived fungi in the last six years (2010 - October 2016) and critically evaluates whether the data published so far really support the notion that these fungi are a promising source of new bioactive chemical entities. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Kinetics of a bioactive compound (caffeine) mobility at the vicinity of the mechanical glass transition temperature induced by gelling polysaccharide.

PubMed

Jiang, Bin; Kasapis, Stefan

2011-11-09

An investigation of the diffusional mobility of a bioactive compound (caffeine) within the high-solid (80.0% w/w) matrices of glucose syrup and κ-carrageenan plus glucose syrup exhibiting distinct mechanical glass transition properties is reported. The experimental temperature range was from 20 to -60 °C, and the techniques of modulated differential scanning calorimetry, small deformation dynamic oscillation in shear, and UV spectrometry were employed. Calorimetric and mechanical measurements were complementary in recording the relaxation dynamics of high-solid matrices upon controlled heating. Predictions of the reaction rate theory and the combined WLF/free volume framework were further utilized to pinpoint the glass transition temperature (T(g)) of the two matrices in the softening dispersion. Independent of composition, calorimetry yielded similar T(g) predictions for both matrices at this level of solids. Mechanical experimentation, however, was able to detect the effect of adding gelling polysaccharide to glucose syrup as an accelerated pattern of vitrification leading to a higher value of T(g). Kinetic rates of caffeine diffusion within the experimental temperature range were taken with UV spectroscopy. These demonstrated the pronounced effect of the gelling κ-carrageenan/glucose syrup mixture to retard diffusion of the bioactive compound near the mechanical T(g). Modeling of the diffusional mobility of caffeine produced activation energy and fractional free-volume estimates, which were distinct from those of the carbohydrate matrix within the glass transition region. This result emphasizes the importance of molecular interactions between macromolecular matrix and small bioactive compound in glass-related relaxation phenomena.

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

Relationship between fresh-packaged spinach leaves exposed to continuous light or dark and bioactive contents: effects of cultivar, leaf size, and storage duration.

PubMed

Lester, Gene E; Makus, Donald J; Hodges, D Mark

2010-03-10

Current retail marketing conditions allow produce to receive artificial light 24 h per day during its displayed shelf life. Essential human-health vitamins [ascorbic acid (vit C), folate (vit B(9)), phylloquinone (vit K(1)), alpha-tocopherol (vit E), and the carotenoids lutein, violaxanthin, zeaxanthin, and beta-carotene (provit A)] also are essential for photosynthesis and are biosynthesized in plants by light conditions even under chilling temperatures. Spinach leaves, notably abundant in the aforementioned human-health compounds, were harvested from flat-leaf 'Lazio' and crinkle-leafed 'Samish' cultivars at peak whole-plant maturity as baby (top- and midcanopy) and larger (lower-canopy) leaves. Leaves were placed as a single layer in commercial, clear-polymer retail boxes and stored at 4 degrees C for up to 9 days under continuous light (26.9 micromol.m(2 ).s) or dark. Top-canopy, baby-leaf spinach generally had higher concentrations of all bioactive compounds, on a dry weight basis, with the exception of carotenoids, than bottom-canopy leaves. All leaves stored under continuous light generally had higher levels of all bioactive compounds, except beta-carotene and violaxanthin, and were more prone to wilting, especially the flat-leafed cultivar. All leaves stored under continuous darkness had declining or unchanged levels of the aforementioned bioactive compounds. Findings from this study revealed that spinach leaves exposed to simulated retail continuous light at 4 degrees C, in clear plastic containers, were overall more nutritionally dense (enriched) than leaves exposed to continuous darkness.

The first structure of a bacterial diterpene cyclase: CotB2.

PubMed

Janke, Ronja; Görner, Christian; Hirte, Max; Brück, Thomas; Loll, Bernhard

2014-06-01

Sesquiterpenes and diterpenes are a diverse class of secondary metabolites that are predominantly derived from plants and some prokaryotes. The properties of these natural products encompass antitumor, antibiotic and even insecticidal activities. Therefore, they are interesting commercial targets for the chemical and pharmaceutical industries. Owing to their structural complexity, these compounds are more efficiently accessed by metabolic engineering of microbial systems than by chemical synthesis. This work presents the first crystal structure of a bacterial diterpene cyclase, CotB2 from the soil bacterium Streptomyces melanosporofaciens, at 1.64 Å resolution. CotB2 is a diterpene cyclase that catalyzes the cyclization of the linear geranylgeranyl diphosphate to the tricyclic cyclooctat-9-en-7-ol. The subsequent oxidation of cyclooctat-9-en-7-ol by two cytochrome P450 monooxygenases leads to bioactive cyclooctatin. Plasticity residues that decorate the active site of CotB2 have been mutated, resulting in alternative monocyclic, dicyclic and tricyclic compounds that show bioactivity. These new compounds shed new light on diterpene cyclase reaction mechanisms. Furthermore, the product of mutant CotB2(W288G) produced the new antibiotic compound (1R,3E,7E,11S,12S)-3,7,18-dolabellatriene, which acts specifically against multidrug-resistant Staphylococcus aureus. This opens a sustainable route for the industrial-scale production of this bioactive compound.

Can we conserve trans-resveratrol content and antioxidant activity during industrial production of chocolate?

PubMed

Salvador, Izabela; Massarioli, Adna P; Silva, Anna Paula S; Malaguetta, Heloísa; Melo, Priscilla S; Alencar, Severino M

2018-05-23

Cocoa exhibits high content of phenolic compounds, among which trans-resveratrol stands out, associated with several bioactive activities such as antioxidant properties. Chocolate contains reduced amounts of these bioactive compounds due to losses during the production process. Therefore, this study aimed to assess changes in total phenolic content and specifically trans-resveratrol, as well as in the antioxidant activity of cocoa and its products during industrial production of chocolate. A total of ten different cocoa products were analyzed. The processes of fermentation and roasting caused significant loss of total phenolic compounds and antioxidant activity. However, due to high temperature, roasting had a major influence on this loss (71% for total phenolic compounds and 53% to 77% for antioxidant activity), except for trans-resveratrol. The content of trans-resveratrol formed after fermentation (9.8 μg kg -1 ) showed little variation during the processes, and it was detected in higher concentrations both in natural (11.4 μg kg -1 ) and in alkalized cocoa powder (13.5 μg kg -1 ). Alkalization of cocoa products led to loss of capacity of deactivating superoxide radical. These findings contribute to the optimization of the production process of chocolate and other food products containing cocoa and its derivatives aiming to better preserve their bioactive compounds. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

Bioactive compounds and antioxidant activities of some cereal milling by-products.

PubMed

Smuda, Sayed Saad; Mohsen, Sobhy Mohamed; Olsen, Karsten; Aly, Mohamed Hassan

2018-03-01

The present study was performed to evaluate the phytochemicals profiles of some cereal milling by-products such as wheat (bran, germ and shorts), rice (bran, germ and husk) and corn (bran, germ and germ meal) to assess their potentiality as bioactive compounds sources. Distilled water, ethanol, methanol, and acetone separately were used as solvents for the extraction of phytochemicals compounds. The antioxidant activity (AOA), total phenolics content (TPC), and total flavonoids content (TFC) of the extracts were investigated using various in vitro assays. The results showed that tannins content was ranged from 113.4 to 389.5 (mg/100 g sample).The study revealed that TPC and TFC of cereal by-products extracts were significantly different for various solvents. TPC content varied from 366.1 to 1924.9 mg/100 g and TFC content varied from 139.3 to 681.6 mg/100 g. High carotenoids content was observed for corn germ meal and minimum for wheat bran. Distilled water, ethanol and methanol extracts showed significantly different antioxidant activity. Significant variations were observed with regard to AOA of different cereal by-products by using various solvents. The ethanol and methanol were observed to be the best solvents to extract phenolic compounds and antioxidant activity, while acetone extract showed less efficiency. Also, the cereal milling by-products were rich in bioactive compounds and could be used as a value added products.

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.

Metabolomics and Ionomics of Potato Tuber Reveals an Influence of Cultivar and Market Class on Human Nutrients and Bioactive Compounds

PubMed Central

Chaparro, Jacqueline M.; Holm, David G.; Broeckling, Corey D.; Prenni, Jessica E.; Heuberger, Adam L.

2018-01-01

Potato (Solanum tuberosum L.) is an important global food crop that contains phytochemicals with demonstrated effects on human health. Understanding sources of chemical variation of potato tuber can inform breeding for improved health attributes of the cooked food. Here, a comprehensive metabolomics (UPLC- and GC-MS) and ionomics (ICP-MS) analysis of raw and cooked potato tuber was performed on 60 unique potato genotypes that span 5 market classes including russet, red, yellow, chip, and specialty potatoes. The analyses detected 2,656 compounds that included known bioactives (43 compounds), nutrients (42), lipids (76), and 23 metals. Most nutrients and bioactives were partially degraded during cooking (44 out of 85; 52%), however genotypes with high quantities of bioactives remained highest in the cooked tuber. Chemical variation was influenced by genotype and market class. Specifically, ~53% of all detected compounds from cooked potato varied among market class and 40% varied by genotype. The most notable metabolite profiles were observed in yellow-flesh potato which had higher levels of carotenoids and specialty potatoes which had the higher levels of chlorogenic acid as compared to the other market classes. Variation in several molecules with known association to health was observed among market classes and included vitamins (e.g., pyridoxal, ~2-fold variation), bioactives (e.g., chlorogenic acid, ~40-fold variation), medicinals (e.g., kukoamines, ~6-fold variation), and minerals (e.g., calcium, iron, molybdenum, ~2-fold variation). Furthermore, more metabolite variation was observed within market class than among market class (e.g., α-tocopherol, ~1-fold variation among market class vs. ~3-fold variation within market class). Taken together, the analysis characterized significant metabolite and mineral variation in raw and cooked potato tuber, and support the potential to breed new cultivars for improved health traits. PMID:29876353

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.

Diet Bioactive Compounds: Implications for Oxidative Stress and Inflammation in the Vascular System.

PubMed

Gabriele, Morena; Pucci, Laura

2017-11-16

Increasing evidence has demonstrated that dietary products and their active components are independently or jointly responsible for the apparent reduction of the cardiovascular diseases (CVDs) risk. Nowadays, there is a growing attention in the use of nutraceuticals as a new approach for the prevention and management of many diseases, as well as for controlling rising of chronic illnesses with minimal side effects. Food-derived peptides, as well as peptide-rich protein hydrolysates, represent new and valuable tools for the prevention of metabolic and cardiovascular diseases, acting as modulators of oxidative stress, inflammation, and overactivity of the renin-angiotensin system (RAS). This review summarizes the recently published data on antioxidant, anti-inflammatory, and vascular protective properties of nutraceuticals, notably on the effects of food-derived bioactive peptides and protein hydrolysates, paying particular attention to those derived from fermented foods. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Potential Anti-Atherosclerotic Properties of Astaxanthin.

PubMed

Kishimoto, Yoshimi; Yoshida, Hiroshi; Kondo, Kazuo

2016-02-05

Astaxanthin is a naturally occurring red carotenoid pigment classified as a xanthophyll, found in microalgae and seafood such as salmon, trout, and shrimp. This review focuses on astaxanthin as a bioactive compound and outlines the evidence associated with its potential role in the prevention of atherosclerosis. Astaxanthin has a unique molecular structure that is responsible for its powerful antioxidant activities by quenching singlet oxygen and scavenging free radicals. Astaxanthin has been reported to inhibit low-density lipoprotein (LDL) oxidation and to increase high-density lipoprotein (HDL)-cholesterol and adiponectin levels in clinical studies. Accumulating evidence suggests that astaxanthin could exert preventive actions against atherosclerotic cardiovascular disease (CVD) via its potential to improve oxidative stress, inflammation, lipid metabolism, and glucose metabolism. In addition to identifying mechanisms of astaxanthin bioactivity by basic research, much more epidemiological and clinical evidence linking reduced CVD risk with dietary astaxanthin intake is needed.

Potential Anti-Atherosclerotic Properties of Astaxanthin

PubMed Central

Kishimoto, Yoshimi; Yoshida, Hiroshi; Kondo, Kazuo

2016-01-01

Astaxanthin is a naturally occurring red carotenoid pigment classified as a xanthophyll, found in microalgae and seafood such as salmon, trout, and shrimp. This review focuses on astaxanthin as a bioactive compound and outlines the evidence associated with its potential role in the prevention of atherosclerosis. Astaxanthin has a unique molecular structure that is responsible for its powerful antioxidant activities by quenching singlet oxygen and scavenging free radicals. Astaxanthin has been reported to inhibit low-density lipoprotein (LDL) oxidation and to increase high-density lipoprotein (HDL)-cholesterol and adiponectin levels in clinical studies. Accumulating evidence suggests that astaxanthin could exert preventive actions against atherosclerotic cardiovascular disease (CVD) via its potential to improve oxidative stress, inflammation, lipid metabolism, and glucose metabolism. In addition to identifying mechanisms of astaxanthin bioactivity by basic research, much more epidemiological and clinical evidence linking reduced CVD risk with dietary astaxanthin intake is needed. PMID:26861359

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

Bioactive alkaloids from the aerial parts of Houttuynia cordata.

PubMed

Ma, Qinge; Wei, Rongrui; Wang, Zhiqiang; Liu, Wenmin; Sang, Zhipei; Li, Yaping; Huang, Hongchun

2017-01-04

Houttuynia cordata is an important traditional Chinese medicine used in heat-clearing and detoxifying, swelling and discharging pus, promoting diuresis and relieving stranguria which recorded in Pharmacopoeia of the people's Republic of China (2015 Edition). H. cordata has been recorded in the book Bencaogangmu which was written by Shizhen Li for the treatment of pyretic toxicity, carbuncle swelling, haemorrhoids, and rectocele diseases. Phytochemical investigation of the aerial parts of H. cordata and evaluation of their PTP1B inhibitory activities and hepatoprotective activities. The dried aerial parts of H. cordata were fractionated by liquid-liquid extraction to obtain CHCl 3 , ethyl acetate, and n-butanolic fractions. The CHCl 3 fraction was confirmed active fraction by the bioactivity-guided investigation, which was isolated and purified by chromatographing over silica gel, Sephadex LH-20, MPLC, and preparative HPLC. The chemical structures of the purified compounds were identified by their spectroscopic data and references. Eight new compounds (1-8), together with fourteen known compounds (9-22) were isolated from the aerial parts of H. cordata. The known compounds (9-22) were obtained from this plant for the first time. Among them, some compounds exhibited moderate bioactivities. Compounds (1-8) were identified as new alkaloids, and the known alkaloids (9-22) were isolated from this plant for the first time. Compounds 1, 4, 14, and 19 showed significant PTP1B inhibitory activities with IC 50 values of 1.254, 2.016, 2.672, and 1.862µm, respectively. Compounds 1, 3, 6, 11, 17, and 20 (10µm) exhibited moderate hepatoprotective activities against D-galactosamine-induced WB-F344 cells damage. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

Hard cap espresso extraction and liquid chromatography determination of bioactive compounds in vegetables and spices.

PubMed

Martinez-Sena, María Teresa; de la Guardia, Miguel; Esteve-Turrillas, Francesc A; Armenta, Sergio

2017-12-15

A new analytical procedure, based on liquid chromatography with diode array and fluorescence detection, has been proposed for the determination of bioactive compounds in vegetables and spices after hard cap espresso extraction. This novel extraction system has been tested for the determination of capsaicin and dihydrocapsaicin from fresh chilli and sweet pepper, piperine from ground pepper, curcumin from turmeric and curry, and myristicin from nutmeg. Extraction efficiency was evaluated by using acetonitrile:water and ethanol:water mixtures. The proposed method allows the extraction of samples with 100mL of 60% (v/v) ethanol in water. The obtained limits of quantification for the proposed procedure ranged from 0.07 to 0.30mgg -1 and results were statistically comparable with those obtained by ultrasound assisted extraction. Hard cap espresso machines offer a fast, effective and quantitative tool for the extraction of bioactive compounds from food samples with an extraction time lower than 30s, using a global available and low cost equipment. Copyright © 2017 Elsevier Ltd. All rights reserved.

Impact of high pressure processing on color, bioactive compounds, polyphenol oxidase activity, and microbiological attributes of pumpkin purée.

PubMed

González-Cebrino, Francisco; Durán, Rocío; Delgado-Adámez, Jonathan; Contador, Rebeca; Bernabé, Rosario Ramírez

2016-04-01

Physicochemical parameters, bioactive compounds' content (carotenoids and total phenols), total antioxidant activity, and enzymatic activity of polyphenol oxidase (PPO) were evaluated after high pressure processing (HPP) on a pumpkin purée (cv. 'Butternut'). Three pressure levels (400, 500, and 600 MPa) were combined with three holding times (200, 400, and 600 s). The applied treatments reduced the levels of total aerobic mesophilic (TAM), total psychrophilic and psychrotrophic bacteria (TPP), and molds and yeasts (M&Y). All applied treatments did not affect enzymatic activity of PPO. Pressure level increased CIE L* values, which could enhance the lightness perception of high pressure (HP)-treated purées. No differences were found between the untreated and HP-treated purées regarding total phenols and carotenoids content (lutein, α-carotene, and β-carotene) and total antioxidant activity. HPP did not affect most quality parameters and maintained the levels of bioactive compounds. However, it did not achieve the complete inhibition of PPO, which could reduce the shelf-life of the pumpkin purée. © The Author(s) 2015.

Bioactive compounds in cashew nut (Anacardium occidentale L.) kernels: effect of different shelling methods.

PubMed

Trox, Jennifer; Vadivel, Vellingiri; Vetter, Walter; Stuetz, Wolfgang; Scherbaum, Veronika; Gola, Ute; Nohr, Donatus; Biesalski, Hans Konrad

2010-05-12

In the present study, the effects of various conventional shelling methods (oil-bath roasting, direct steam roasting, drying, and open pan roasting) as well as a novel "Flores" hand-cracking method on the levels of bioactive compounds of cashew nut kernels were investigated. The raw cashew nut kernels were found to possess appreciable levels of certain bioactive compounds such as beta-carotene (9.57 microg/100 g of DM), lutein (30.29 microg/100 g of DM), zeaxanthin (0.56 microg/100 g of DM), alpha-tocopherol (0.29 mg/100 g of DM), gamma-tocopherol (1.10 mg/100 g of DM), thiamin (1.08 mg/100 g of DM), stearic acid (4.96 g/100 g of DM), oleic acid (21.87 g/100 g of DM), and linoleic acid (5.55 g/100 g of DM). All of the conventional shelling methods including oil-bath roasting, steam roasting, drying, and open pan roasting revealed a significant reduction, whereas the Flores hand-cracking method exhibited similar levels of carotenoids, thiamin, and unsaturated fatty acids in cashew nuts when compared to raw unprocessed samples.

Pressurized hot water extraction (PHWE) for the green recovery of bioactive compounds and steviol glycosides from Stevia rebaudiana Bertoni leaves.

PubMed

Bursać Kovačević, Danijela; Barba, Francisco J; Granato, Daniel; Galanakis, Charis M; Herceg, Zoran; Dragović-Uzelac, Verica; Putnik, Predrag

2018-07-15

Stevia rebaudiana Bertoni leaves are a natural source of diterpenic glycosides, and various bioactive compounds. The objectives were to characterize antioxidants and steviol glycosides in the extracts obtained from Stevia after "green" pressurized hot water extraction (PHWE). PHWE extracts were obtained at different temperatures (100, 130, 160 °C); static extraction times (5 and 10 min), and cycle numbers (1, 2, 3) using a constant pressure of 10.34 MPa. Temperature was the most important parameter for extraction, where the highest recoveries of all bioactive compounds (except for carotenoids) were at 160 °C. Extracts obtained at longer static times had more steviol glycosides, condensed tannins, and chlorophyll A. Higher amounts of total phenols, condensed tannins, and steviol glycosides were obtained under higher cycle numbers. This study indicated that PHWE is useful for recovering polar and nonpolar antioxidants and steviol glycosides. PHWE may be a suitable technique for scale-up to industrial applications. Copyright © 2018 Elsevier Ltd. All rights reserved.

Recovering Bioactive Compounds from Olive Oil Filter Cake by Advanced Extraction Techniques

PubMed Central

Lozano-Sánchez, Jesús; Castro-Puyana, María; Mendiola, Jose A.; Segura-Carretero, Antonio; Cifuentes, Alejandro; Ibáñez, Elena

2014-01-01

The potential of by-products generated during extra-virgin olive oil (EVOO) filtration as a natural source of phenolic compounds (with demonstrated bioactivity) has been evaluated using pressurized liquid extraction (PLE) and considering mixtures of two GRAS (generally recognized as safe) solvents (ethanol and water) at temperatures ranging from 40 to 175 °C. The extracts were characterized by high-performance liquid chromatography (HPLC) coupled to diode array detection (DAD) and electrospray time-of-flight mass spectrometry (HPLC-DAD-ESI-TOF/MS) to determine the phenolic-composition of the filter cake. The best isolation procedure to extract the phenolic fraction from the filter cake was accomplished using ethanol and water (50:50, v/v) at 120 °C. The main phenolic compounds identified in the samples were characterized as phenolic alcohols or derivatives (hydroxytyrosol and its oxidation product), secoiridoids (decarboxymethylated and hydroxylated forms of oleuropein and ligstroside aglycones), flavones (luteolin and apigenin) and elenolic acid derivatives. The PLE extraction process can be applied to produce enriched extracts with applications as bioactive food ingredients, as well as nutraceuticals. PMID:25226536

Determination of some physicochemical characteristics, bioactive compounds and antioxidant activity of tropical fruits from Yucatan, Mexico.

PubMed

Moo-Huchin, Víctor M; Estrada-Mota, Iván; Estrada-León, Raciel; Cuevas-Glory, Luis; Ortiz-Vázquez, Elizabeth; Vargas y Vargas, María de Lourdes; Betancur-Ancona, David; Sauri-Duch, Enrique

2014-01-01

The aim to the study was to determine the physicochemical composition, bioactive compounds and antioxidant activity of fruits from Yucatan, Mexico such as star apple, cashew, mombin, mamey sapote, white sapote, sugar apple, sapodilla, dragon fruit, nance, ilama, custard apple, mamoncillo and black sapote. The physicochemical characteristics were different between fruits and were good sources of bioactive compounds. The edible part with the highest values of antioxidant activity were mamoncillo, star apple, mombin, cashew, white sapote, ilama, custard apple, sugar apple, and nance. Total soluble phenols content showed a correlation with antioxidant activity by ABTS (R=0.52, P⩽0.05) and DPPH (R=0.43, P⩽0.05). A high correlation was obtained between the two assays (ABTS and DPPH) used to measure antioxidant activity in the tropical fruit species under study (R=0.82, P⩽0.05). The results show promising perspectives for the exploitation and use of tropical fruits studied with significant levels of nutrients and antioxidant activity. Copyright © 2013 Elsevier Ltd. All rights reserved.

An enantiomer-based virtual screening approach: Discovery of chiral organophosphates as acetyl cholinesterase inhibitors.

PubMed

Zhang, Aiqian; Mu, Yunsong; Wu, Fengchang

2017-04-01

Chiral organophosphates (OPs) have been used widely around the world, very little is known about binding mechanisms with biological macromolecules. An in-depth understanding of the stereo selectivity of human AChE and discovering bioactive enantiomers of OPs can decrease health risks of these chiral chemicals. In the present study, a flexible molecular docking approach was conducted to investigate different binding modes of twelve phosphorus enantiomers. A pharmacophore model was then developed on basis of the bioactive conformations of these compounds. After virtual screening, twenty-four potential bioactive compounds were found, of which three compounds (Ethyl p-nitrophenyl phenylphosphonate (EPN), 1-naphthaleneacetic anhydride and N,4-dimethyl-N-phenyl-benzenesulfonamide) were tested by use of different in vitro assays. S-isomer of EPN was also found to exhibit greater inhibitory activity towards human AChE than the corresponding R-isomer. These findings affirm that stereochemistry plays a crucial role in virtual screening, and provide a new insight into designing safer organ phosphorus pesticides on human health. Copyright © 2017 Elsevier Inc. All rights reserved.

Biotechnological and Pharmacological Applications of Biotoxins and Other Bioactive Molecules from Dinoflagellates

PubMed Central

Guedes, A. Catarina; Malcata, F. Xavier

2017-01-01

The long-lasting interest in bioactive molecules (namely toxins) produced by (microalga) dinoflagellates has risen in recent years. Exhibiting wide diversity and complexity, said compounds are well-recognized for their biological features, with great potential for use as pharmaceutical therapies and biological research probes. Unfortunately, provision of those compounds is still far from sufficient, especially in view of an increasing demand for preclinical testing. Despite the difficulties to establish dinoflagellate cultures and obtain reasonable productivities of such compounds, intensive research has permitted a number of advances in the field. This paper accordingly reviews the characteristics of some of the most important biotoxins (and other bioactive substances) produced by dinoflagellates. It also presents and discusses (to some length) the main advances pertaining to dinoflagellate production, from bench to large scale—with an emphasis on material published since the latest review available on the subject. Such advances encompass improvements in nutrient formulation and light supply as major operational conditions; they have permitted adaptation of classical designs, and aided the development of novel configurations for dinoflagellate growth—even though shearing-related issues remain a major challenge. PMID:29261163

Evaluation of polyphenolic content and antioxidant activity in two onion varieties grown under organic and conventional production systems.

PubMed

Ren, Feiyue; Reilly, Kim; Gaffney, Michael; Kerry, Joseph P; Hossain, Mohammad; Rai, Dilip K

2017-07-01

Onions contain a number of bioactive compounds, in particular polyphenols. They are rich sources of such compounds in the human diet and offer significant health benefits to the consumer. Demand for organic crops is steadily increasing partly based on the expected health benefits of organic food consumption. The current study examines the influence of organic and conventional crop management practices on bioactive polyphenolic content of onion. We examined the effect of conventional, organic, and mixed cultivation practices on the content of total phenolics, total flavonoids and antioxidant activity in two varieties of onion grown over 4 years in a split-plot factorial systems comparison trial. Levels of total phenolics and total flavonoids showed a significant year-on-year variation and were significantly different between organic and conventional production systems. The levels of total phenolics, total flavonoids and antioxidant activity in general were significantly higher (P < 0.05) under fully organic compared to fully conventional management. Organic cultivation practices resulted in significantly higher levels of potential bioactive compounds in onion. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

Cyanobacteria and microalgae: a renewable source of bioactive compounds and other chemicals.

PubMed

Encarnação, Telma; Pais, Alberto A C C; Campos, Maria G; Burrows, Hugh D

2015-01-01

Microalgae and cyanobacteria are rich sources of many valuable compounds, including important bioactive and biotechnologically relevant chemicals. Their enormous biodiversity, and the consequent variability in the respective biochemical composition, make microalgae cultivations a promising resource for many novel chemically and biologically active molecules and compounds of high commercial value such as lipids and dyes. The nature of the chemicals produced can be manipulated by changing the cultivation media and conditions. Algae are extremely versatile because they can be adapted to a variety of cell culture conditions. They do not require arable land, can be cultivated on saline water and wastewaters, and require much less water than plants. They possess an extremely high growth rate making these microorganisms very attractive for use in biofuel production--some species of algae can achieve around 100 times more oil than oil seeds. In addition, microalgae and cyanobacteria can accumulate various biotoxins and can contribute to mitigate greenhouse gases since they produce biomass through carbon dioxide fixation. In this review, we provide an overview of the application of microalgae in the production of bioactive and other chemicals.

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.

Discovery, Synthesis, and Functional Characterization of a Novel Neuroprotective Natural Product from the Fruit of Alpinia oxyphylla for use in Parkinson's Disease Through LC/MS-Based Multivariate Data Analysis-Guided Fractionation.

PubMed

Li, Guohui; Zhang, Zaijun; Quan, Quan; Jiang, Renwang; Szeto, Samuel S W; Yuan, Shuai; Wong, Wing-Tak; Lam, Herman H C; Lee, Simon Ming-Yuen; Chu, Ivan K

2016-08-05

Herein we report the discovery of a novel lead compound, oxyphylla A [(R)-4-(2-hydroxy-5-methylphenyl)-5-methylhexanoic acid] (from the fruit of Alpinia oxyphylla), which functions as a neuroprotective agent against Parkinson's disease. To identify a shortlist of candidates from the extract of A. oxyphylla, we employed an integrated strategy combining liquid chromatography/mass spectrometry, bioactivity-guided fractionation, and chemometric analysis. The neuroprotective effects of the shortlisted candidates were validated prior to scaling up the finalized list of potential neuroprotective constituents for more detailed chemical and biological characterization. Oxyphylla A has promising neuroprotective effects: (i) it ameliorates in vitro chemical-induced primary neuronal cell damage and (ii) alleviates chemical-induced dopaminergic neuron loss and behavioral impairment in both zebrafish and mice in vivo. Quantitative proteomics analyses of oxyphylla A-treated primary cerebellar granule neurons that had been intoxicated with 1-methyl-4-phenylpyridinium revealed that oxyphylla A activates nuclear factor-erythroid 2-related factor 2 (NRF2)-a master redox switch-and triggers a cascade of antioxidative responses. These observations were verified independently through western blot analyses. Our integrated metabolomics, chemometrics, and pharmacological strategy led to the efficient discovery of novel bioactive ingredients from A. oxyphylla while avoiding the nontargeting, labor-intensive steps usually required for identification of bioactive compounds. Our successful development of a synthetic route toward oxyphylla A should lead to its availability on a large scale for further functional development and pathological studies.

Chemical characterization and bioactive properties of Geranium molle L.: from the plant to the most active extract and its phytochemicals.

PubMed

Graça, V C; Barros, Lillian; Calhelha, Ricardo C; Dias, Maria Inês; Carvalho, Ana Maria; Santos-Buelga, Celestino; Ferreira, Isabel C F R; Santos, P F

2016-05-18

After a period of indifference, in which synthetic compounds were favored, there is an increasing interest in the study of the biological properties of plants and the active principles responsible for their therapeutic properties. Geranium molle L. has been used in the Portuguese folk medicine for the treatment of various ailments including cancer but, unlike many of the species from the Geranium genus, its phytochemical characterization and biological activity are virtually unexplored. In this study a G. molle sample from Trás-os-Montes, north-eastern Portugal, was chemically characterized regarding nutritional value, free sugars, organic acids, fatty acids and tocopherols, and several aqueous (decoction, infusion) and organic (n-hexane, dichloromethane, ethyl acetate, acetone, methanol) extracts of the plant were assessed for their bioactive properties. The antioxidant activity was evaluated by means of the free radicals scavenging activity, reducing power and inhibition of lipid peroxidation. The cytotoxicity of the different extracts was assessed in vitro against several human cancer cell lines (breast, lung, cervical and hepatocellular carcinomas) and, additionally, their hepatotoxicity was evaluated using a porcine liver primary cell culture. G. molle was shown to be rich in carbohydrates and proteins, providing tocopherols and essential fatty acids. Amongst the various extracts, the acetone extract was found to have the highest content of phenolic compounds (mainly ellagitannins, but also some flavone and flavonol glycosides) as well as the highest antioxidant and cytotoxic activities. To the best of our knowledge, this is the first report on the chemical composition and bioactive properties of G. molle.

Fruit wastes fermentation for phenolic antioxidants production and their application in manufacture of edible coatings and films.

PubMed

Martinez-Avila, G C G; Aguilera, A F; Saucedo, S; Rojas, R; Rodriguez, R; Aguilar, C N

2014-01-01

Agro-industrial by-products are important sources of potent bioactive phenolic compounds. These compounds are of extreme relevance for food and pharmacological industries due to their great variety of biological activities. Fermentation represents an environmentally clean technology for production and extraction of these bioactive compounds, providing high quality and high activity extracts, which can be incorporated in foods using coatings/films wax-based in order to avoid alterations in their quality. In this document is presented an overview about importance and benefits of solid-state fermentation, pointing out this bioprocess as an alternative technology for use agro-industrial by-products as substrates to produce valuable secondary metabolites and their applications as food quality conservatives.

Phytochemicals: Extraction, Isolation, and Identification of Bioactive Compounds from Plant Extracts

PubMed Central

Altemimi, Ammar; Lakhssassi, Naoufal; Baharlouei, Azam; Watson, Dennis G.; Lightfoot, David A.

2017-01-01

There are concerns about using synthetic phenolic antioxidants such as butylated hydroxytoluene (BHT) and butylated hydroxyanisole (BHA) as food additives because of the reported negative effects on human health. Thus, a replacement of these synthetics by antioxidant extractions from various foods has been proposed. More than 8000 different phenolic compounds have been characterized; fruits and vegetables are the prime sources of natural antioxidants. In order to extract, measure, and identify bioactive compounds from a wide variety of fruits and vegetables, researchers use multiple techniques and methods. This review includes a brief description of a wide range of different assays. The antioxidant, antimicrobial, and anticancer properties of phenolic natural products from fruits and vegetables are also discussed. PMID:28937585

NO inhibitory constituents as potential anti-neuroinflammatory agents for AD from Blumea balsamifera.

PubMed

Ma, Jun; Ren, Quanhui; Dong, Bangjian; Shi, Zhaoyu; Zhang, Jie; Jin, Da-Qing; Xu, Jing; Ohizumi, Yasushi; Lee, Dongho; Guo, Yuanqiang

2018-02-01

Our continuous search for new nitric oxide (NO) inhibitory substances as anti-neuroinflammatory agents for AD resulted in the isolation of one new labdane diterpenoid and three new guaiane sesquiterpenoids, as well as ten known compounds from Blumea balsamifera. Their structures were elucidated by NMR spectroscopic data analysis and the time-dependent density functional theory (TDDFT) electronic circular dichroism (ECD) calculations. The anti-neuroinflammatory effects were examined by inhibiting NO release in LPS-induced murine microglial BV-2 cells. The possible mechanism of NO inhibition of some bioactive compounds was also investigated using molecular docking, which revealed the interactions of bioactive compounds with the iNOS protein. Copyright © 2017 Elsevier Inc. All rights reserved.

The development of microalgal biotechnology in the Czech Republic.

PubMed

Masojídek, Jiří; Prášil, Ondřej

2010-12-01

Microscopic algae and cyanobacteria are excellent sources of numerous compounds, from raw biomass rich in proteins, oils, and antioxidants to valuable secondary metabolites with potential medical use. In the former Czechoslovakia, microalgal biotechnology developed rapidly in the 1960s with the main aim of providing industrial, high-yield sources of algal biomass. Unique cultivation techniques that are still in use were successfully developed and tested. Gradually, the focus changed from bulk production to more sophisticated use of microalgae, including production of bioactive compounds. Along the way, better understanding of the physiology and cell biology of productive microalgal strains was achieved. Currently, microalgae are in the focus again, mostly as possible sources of bioactive compounds and next-generation biofuels for the 21st century.

Mushroom immunomodulators: unique molecules with unlimited applications.

PubMed

El Enshasy, Hesham A; Hatti-Kaul, Rajni

2013-12-01

For centuries, mushrooms have been used as food and medicine in different cultures. More recently, many bioactive compounds have been isolated from different types of mushrooms. Among these, immunomodulators have gained much interest based on the increasing growth of the immunotherapy sector. Mushroom immunomodulators are classified under four categories based on their chemical nature as: lectins, terpenoids, proteins, and polysaccharides. These compounds are produced naturally in mushrooms cultivated in greenhouses. For effective industrial production, cultivation is carried out in submerged culture to increase the bioactive compound yield, decrease the production time, and reduce the cost of downstream processing. This review provides a comprehensive overview on mushroom immunomodulators in terms of chemistry, industrial production, and applications in medical and nonmedical sectors. Copyright © 2013 Elsevier Ltd. All rights reserved.

Identification and bioactivity of compounds from the fungus Penicillium sp. CYE-87 isolated from a marine tunicate.

PubMed

Shaala, Lamiaa A; Youssef, Diaa T A

2015-03-25

In the course of our continuous interest in identifying bioactive compounds from marine microbes, we have investigated a tunicate-derived fungus, Penicillium sp. CYE-87. A new compound with the 1,4-diazepane skeleton, terretrione D (2), together with the known compounds, methyl-2-([2-(1H-indol-3-yl)ethyl]carbamoyl)acetate (1), tryptamine (3), indole-3-carbaldehyde (4), 3,6-diisobutylpyrazin-2(1H)-one (5) and terretrione C (6), were isolated from Penicillium sp. CYE-87. The structures of the isolated compounds were established by spectral analysis, including 1D (1H, 13C) and 2D (COSY, multiplicity edited-HSQC and HMBC) NMR and HRESIMS, as well as comparison of their NMR data with those in the literature. The compounds were evaluated for their antimigratory activity against the human breast cancer cell line (MDA-MB-231) and their antiproliferation activity against HeLa cells. Compounds 2 and 6 showed significant antimigratory activity against MDA-MB-231, as well as antifungal activity against C. albicans.

Identification and Bioactivity of Compounds from the Fungus Penicillium sp. CYE-87 Isolated from a Marine Tunicate

PubMed Central

Shaala, Lamiaa A.; Youssef, Diaa T. A.

2015-01-01

In the course of our continuous interest in identifying bioactive compounds from marine microbes, we have investigated a tunicate-derived fungus, Penicillium sp. CYE-87. A new compound with the 1,4-diazepane skeleton, terretrione D (2), together with the known compounds, methyl-2-([2-(1H-indol-3-yl)ethyl]carbamoyl)acetate (1), tryptamine (3), indole-3-carbaldehyde (4), 3,6-diisobutylpyrazin-2(1H)-one (5) and terretrione C (6), were isolated from Penicillium sp. CYE-87. The structures of the isolated compounds were established by spectral analysis, including 1D (1H, 13C) and 2D (COSY, multiplicity edited-HSQC and HMBC) NMR and HRESIMS, as well as comparison of their NMR data with those in the literature. The compounds were evaluated for their antimigratory activity against the human breast cancer cell line (MDA-MB-231) and their antiproliferation activity against HeLa cells. Compounds 2 and 6 showed significant antimigratory activity against MDA-MB-231, as well as antifungal activity against C. albicans. PMID:25815893

Characterization of Neem (Azadirachta indica A. Juss) seed volatile compounds obtained by supercritical carbon dioxide process.

PubMed

Swapna Sonale, R; Ramalakshmi, K; Udaya Sankar, K

2018-04-01

Extraction process employing Supercritical fluid carbon dioxide (SCF) yields bioactive compounds near natural forms without any artifact formation. Neem seed was subjected to SCF at different temperatures and pressure conditions. These extracts were partitioned to separate volatile fraction and were analyzed by Gas Chromatography-Mass spectroscopy along with the volatiles extracted by the hydro-distillation method. Experimental results show that there is a significant effect of pressure and temperature on isolation of a number of volatile compounds as well as retention of biologically active compounds. Twenty-five volatile compounds were isolated in the Hydro-distillate compare to the SCF extract of 100 bar, 40 °C which showed forty volatile compounds corresponds to 76.38 and 92.39% of total volatiles respectively. The majority of bioactive compounds such as Terpinen-4-ol, 1,2,4-Trithiolane, 3,5-diethyl, allyl isopropyl sulphide, Cycloisolongifolene, á-Bisabolene, (-)-α-Panasinsen, Isocaryophyllene, trans-Sesquisabinene hydrate, 1-Naphthalenol, were identified in the extract when isolated at 100 bar and 40 °C.

Wetspun poly-L-(lactic acid)-borosilicate bioactive glass scaffolds for guided bone regeneration.

PubMed

Fernandes, João S; Reis, Rui L; Pires, Ricardo A

2017-02-01

We developed a porous poly-L-lactic acid (PLLA) scaffold compounded with borosilicate bioactive glasses (BBGs) endowing it with bioactive properties. Porous PLLA-BBG fibre mesh scaffolds were successfully prepared by the combination of wet spinning and fibre bonding techniques. Micro-computed tomography (μCT) confirmed that the PLLA-BBG scaffolds containing ≈25% of BBGs (w/w) exhibited randomly interconnected porous (58 to 62% of interconnectivity and 53 to 67% of porosity) with mean pore diameters higher that 100μm. Bioactivity and degradation studies were performed by immersing the scaffolds in simulated body fluid (SBF) and ultrapure water, respectively. The PLLA-BBG scaffolds presented a faster degradation rate with a constant release of inorganic species, which are capable to produce calcium phosphate structures at the surface of the material after 7days of immersion in SBF (Ca/P ratio of ~1.7). Cellular in vitro studies with human osteosarcoma cell line (Saos-2) and human adipose-derived stem cells (hASCs) showed that PLLA-BBGs are not cytotoxic to cells, while demonstrating their capacity to promote cell adhesion and proliferation. Overall, we showed that the proposed scaffolds present a tailored kinetics on the release of inorganic species and controlled biological response under conditions that mimic the bone physiological environment. Copyright © 2016 Elsevier B.V. All rights reserved.

[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.

Bioactive terpenes from marine-derived fungi.

PubMed

Elissawy, Ahmed M; El-Shazly, Mohamed; Ebada, Sherif S; Singab, AbdelNasser B; Proksch, Peter

2015-04-03

Marine-derived fungi continue to be a prolific source of secondary metabolites showing diverse bioactivities. Terpenoids from marine-derived fungi exhibit wide structural diversity including numerous compounds with pronounced biological activities. In this review, we survey the last five years' reports on terpenoidal metabolites from marine-derived fungi with particular attention on those showing marked biological activities.

Strategies for designing novel functional meat products.

PubMed

Arihara, Keizo

2006-09-01

In recent years, much attention has been paid to physiological functions of foods due to increasing concerns for health. Although there has been limited information of physiological functions of meat until recently, several attractive meat-based bioactive compounds, such as carnosine, anserine, l-carnitine, conjugated linoleic acid, have been studied. Emphasizing these activities is one possible approach for improving the health image of meat and developing functional meat products. This article provides potential benefits of representative meat-based bioactive compounds on human health and an overview of meat-based functional products. Strategies for designing novel functional meat products utilizing bioactive peptides and/or probiotic bacteria, is also discussed. This article focuses particularly on the possibility of meat protein-derived bioactive peptides, such as antihypertensive peptides. There are still some hurdles in developing and marketing novel functional meat products since such products are unconventional and consumers in many countries recognize meat and meat products to be bad for health. Along with accumulation of scientific data, there is an urgent need to inform consumers of the exact functional value of meat and meat products including novel functional foods.

Development of Mushroom-Based Cosmeceutical Formulations with Anti-Inflammatory, Anti-Tyrosinase, Antioxidant, and Antibacterial Properties.

PubMed

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

2016-10-14

The cosmetic industry is in a constant search for natural compounds or extracts with relevant bioactive properties, which became valuable ingredients to design cosmeceutical formulations. Mushrooms have been markedly studied in terms of nutritional value and medicinal properties. However, there is still slow progress in the biotechnological application of mushroom extracts in cosmetic formulations, either as antioxidants, anti-aging, antimicrobial, and anti-inflammatory agents or as hyperpigmentation correctors. In the present work, the cosmeceutical potential of ethanolic extracts prepared from Agaricus bisporus , Pleurotus ostreatus , and Lentinula edodes was analyzed in terms of anti-inflammatory, anti-tyrosinase, antioxidant, and antibacterial activities. The extracts were characterized in terms of phenolic acids and ergosterol composition, and further incorporated in a base cosmetic cream to achieve the same bioactive purposes. From the results obtained, the final cosmeceutical formulations presented 85%-100% of the phenolic acids and ergosterol levels found in the mushroom extracts, suggesting that there was no significant loss of bioactive compounds. The final cosmeceutical formulation also displayed all the ascribed bioactivities and as such, mushrooms can further be exploited as natural cosmeceutical ingredients.

Biochemometrics for Natural Products Research: Comparison of Data Analysis Approaches and Application to Identification of Bioactive Compounds.

PubMed

Kellogg, Joshua J; Todd, Daniel A; Egan, Joseph M; Raja, Huzefa A; Oberlies, Nicholas H; Kvalheim, Olav M; Cech, Nadja B

2016-02-26

A central challenge of natural products research is assigning bioactive compounds from complex mixtures. The gold standard approach to address this challenge, bioassay-guided fractionation, is often biased toward abundant, rather than bioactive, mixture components. This study evaluated the combination of bioassay-guided fractionation with untargeted metabolite profiling to improve active component identification early in the fractionation process. Key to this methodology was statistical modeling of the integrated biological and chemical data sets (biochemometric analysis). Three data analysis approaches for biochemometric analysis were compared, namely, partial least-squares loading vectors, S-plots, and the selectivity ratio. Extracts from the endophytic fungi Alternaria sp. and Pyrenochaeta sp. with antimicrobial activity against Staphylococcus aureus served as test cases. Biochemometric analysis incorporating the selectivity ratio performed best in identifying bioactive ions from these extracts early in the fractionation process, yielding altersetin (3, MIC 0.23 μg/mL) and macrosphelide A (4, MIC 75 μg/mL) as antibacterial constituents from Alternaria sp. and Pyrenochaeta sp., respectively. This study demonstrates the potential of biochemometrics coupled with bioassay-guided fractionation to identify bioactive mixture components. A benefit of this approach is the ability to integrate multiple stages of fractionation and bioassay data into a single analysis.

A Critical Review of Bioactive Food Components, and of their Functional Mechanisms, Biological Effects and Health Outcomes.

PubMed

Perez-Gregorio, Rosa; Simal-Gandara, Jesus

2017-01-01

Eating behaviours are closely related to some medical conditions potentially leading to death such as cancer, cardiovascular disease and diabetes. Healthy eating practices, maintaining a normal weight, and regular physical activity could prevent up to 80% of coronary heart disease, 90% of type-2 diabetes and onethird of all cancers [1]. Over the last two decades, the food industry has invested much effort in research and development of healthier, more nutritious foods. These foods are frequently designated "functional" when they contain nutritional components required for healthy living or "nutraceuticals" when intended to treat or prevent disease or disorders through a variety of bioactive (e.g., antioxidant, antimicrobial, immunomodulatory, hypocholesterolaemic) functions that are performed by functional enzymes, probiotics, prebiotics, fibres, phytosterols, peptides, proteins, isoflavones, saponins or phytic acid, among other substances. Some agricultural and industrial residues have proven to be excellent choices as raw materials for producing bioactive compounds and have been proposed as potentially safe natural sources of antimicrobials and/or antioxidants for the food industry. Functional food ingredients containing bioactive compounds could be used as plant extracts by pharmaceutical and food industries. Bioactive food components influence health outcomes. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Investigation of bioactivity and cell effects of nano-porous sol-gel derived bioactive glass film

NASA Astrophysics Data System (ADS)

Ma, Zhijun; Ji, Huijiao; Hu, Xiaomeng; Teng, Yu; Zhao, Guiyun; Mo, Lijuan; Zhao, Xiaoli; Chen, Weibo; Qiu, Jianrong; Zhang, Ming

2013-11-01

In orthopedic surgery, bioactive glass film coating is extensively studied to improve the synthetic performance of orthopedic implants. A lot of investigations have confirmed that nano-porous structure in bioactive glasses can remarkably improve their bioactivity. Nevertheless, researches on preparation of nano-porous bioactive glasses in the form of film coating and their cell response activities are scarce. Herein, we report the preparation of nano-porous bioactive glass film on commercial glass slide based on a sol-gel technique, together with the evaluation of its in vitro bioactivity through immersion in simulated body fluid and monitoring the precipitation of apatite-like layer. Cell responses of the samples, including attachment, proliferation and osteogenic differentiation, were also investigated using BMSCS (bone marrow derived mesenchymal stem cells) as a model. The results presented here provide some basic information on structural influence of bioactive glass film on the improvement of bioactivity and cellular effects.

Melatonin and hydroxytyrosol protect against oxidative stress related to the central nervous system after the ingestion of three types of wine by healthy volunteers.

PubMed

Marhuenda, Javier; Medina, Sonia; Martínez-Hernández, Pedro; Arina, Simón; Zafrilla, Pilar; Mulero, Juana; Oger, Camille; Galano, Jean-Marie; Durand, Thierry; Ferreres, Federico; Gil-Izquierdo, Angel

2017-01-25

Adrenic acid (AdA) and docosahexaenoic acid (DHA) peroxidation produces F 2 -dihomo-IsoPs and neuroprostanes, which have been related to oxidative damage in the central nervous system. Besides polyphenols, melatonin (MEL) and hydroxytyrosol (OHTyr) could be partly responsible for the antioxidant benefits of red wine (excluding colon derivatives). In order to elucidate whether these compounds are responsible for the protective antioxidant effects of red wine, a double-blind, crossover, placebo-controlled in vivo study - involving the intake of red wines and their native musts by healthy volunteers - was performed. The urinary metabolites decreased after the administration of red wines, to a greater extent than after the intake of their corresponding musts or ethanol. Melatonin is the most effective compound that protects adrenic acid from oxidative attack, judged by the reduction in the formation of F 2 -dihomo-isoprostanes. Similarly, hydroxytyrosol, being the most effective bioactive compound in reducing the formation of F 3 -neuroprostanes n-6 DPA and F 4 -neuroprostanes, protected docosahexaenoic and eicosapentaenoic acids from oxidative attack.

Solubilization of poorly water-soluble compounds using amphiphilic phospholipid polymers with different molecular architectures.

PubMed

Mu, Mingwei; Konno, Tomohiro; Inoue, Yuuki; Ishihara, Kazuhiko

2017-10-01

To achieve stable and effective solubilization of poorly water-soluble bioactive compounds, water-soluble and amphiphilic polymers composed of hydrophilic 2-methacryloyloxyethyl phosphorylcholine (MPC) units and hydrophobic n-butyl methacrylate (BMA) units were prepared. MPC polymers having different molecular architectures, such as random-type monomer unit sequences and block-type sequences, formed polymer aggregates when they were dissolved in aqueous media. The structure of the random-type polymer aggregate was loose and flexible. On the other hand, the block-type polymer formed polymeric micelles, which were composed of very stable hydrophobic poly(BMA) cores and hydrophilic poly(MPC) shells. The solubilization of a poorly water-soluble bioactive compound, paclitaxel (PTX), in the polymer aggregates was observed, however, solubilizing efficiency and stability were strongly depended on the polymer architecture; in other words, PTX stayed in the poly(BMA) core of the polymer micelle formed by the block-type polymer even when plasma protein was present in the aqueous medium. On the other hand, when the random-type polymer was used, PTX was transferred from the polymer aggregate to the protein. We conclude that water-soluble and amphiphilic MPC polymers are good candidates as solubilizers for poorly water-soluble bioactive compounds. Copyright © 2017 Elsevier B.V. All rights reserved.

Bioprospecting of Novel and Bioactive Compounds from Marine Actinomycetes Isolated from South China Sea Sediments.

PubMed

Yang, Na; Song, Fuhang

2018-02-01

Marine actinomycetes are less investigated compared to terrestrial strains as potential sources of natural products. To date, few investigations have been performed on culturable actinomycetes associated with South China Sea sediments. In the present study, twenty-eight actinomycetes were recovered from South China Sea sediments after dereplication by traditional culture-dependent method. The 16S rRNA gene sequences analyses revealed that these strains related to five families and seven genera. Twelve representative strains possessed at least one of the biosynthetic genes coding for polyketide synthase I, II, and nonribosomal peptide synthetase. Four strains had anti-Mycobacterium phlei activities and five strains had activities against methicillin-resistant Staphylococcus aureus. 10 L-scale fermentation of strains Salinispora sp. NHF45, Nocardiopsis sp. NHF48, and Streptomyces sp. NHF86 were carried out for novel and bioactive compounds discovery. Finally, we obtained a novel α-pyrone compound from marine Nocardiopsis sp. NHF48, an analogue of paulomenol from marine Streptomyces sp. NHF86 and a new source of rifamycin B, produced by Salinispora sp. NHF45. The present study concluded that marine actinomycetes, which we isolated from South China Sea sediments, will be a suitable source for the development of novel and bioactive compounds.

Effects of dehydration methods on quality characteristics of yellow passion fruit co-products.

PubMed

Silva, Neiton C; Duarte, Claudio R; Barrozo, Marcos As

2017-11-01

The production and processing of fruits generate a large amount of residues, which are usually disposed of or under-used, representing losses of raw material and energy. The present paper investigates the effect of four dehydration techniques (convective, infrared, microwave and freeze-drying) on yellow passion fruit (Passiflora edulis f. flavicarpa) co-products and the influence of the main variables on moisture removal and bioactive compounds. The compounds analyzed were total phenolics, total flavonoids, ascorbic acid and pectin. The content of phenolics and flavonoids increased after dehydration in all techniques investigated and the process temperatures directly affected the ascorbic acid content. Microwave dehydration showed the best results for most bioactive compounds analyzed, if performed in suitable process conditions. However, the highest levels of pectin content were obtained by freeze-drying and convective dehydration. This study reinforces the importance of the adequate use of passion fruit co-products due to the high levels of bioactive compounds in this material. Microwave dehydration presented the best results, which indicates the potential use of this technique for a better exploitation of fruit co-products. Larger quantities of pectin were extracted from samples dehydrated through methodologies with long-time process and low temperatures, such as convective drying and freeze-drying. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Physico-chemical parameters, bioactive compounds and microbial quality of thermo-sonicated carrot juice during storage.

PubMed

Martínez-Flores, Héctor E; Garnica-Romo, Ma Guadalupe; Bermúdez-Aguirre, Daniela; Pokhrel, Prashant Raj; Barbosa-Cánovas, Gustavo V

2015-04-01

Thermosonication has been successfully tested in food for microbial inactivation; however, changes in bioactive compounds and shelf-life of treated products have not been thoroughly investigated. Carrot juice was thermo-sonicated (24 kHz, 120 μm amplitude) at 50 °C, 54 °C and 58 °C for 10 min (acoustic power 2204.40, 2155.72, 2181.68 mW/mL, respectively). Quality parameters and microbial growth were evaluated after processing and during storage at 4 °C. Control and sonicated treatments at 50 °C and 54 °C had 10, 12 and 14 d of shelf-life, respectively. Samples sonicated at 58 °C had the best quality; microbial growth remained low at around 3-log for mesophiles, 4.5-log for yeasts and molds and 2-log for enterobacteria after 20 d of storage. Furthermore, thermo-sonicated juice at 58 °C retained >98% of carotenoids and 100% of ascorbic acid. Phenolic compounds increased in all stored, treated juices. Thermo-sonication is therefore a promising technology for preserving the quality of carrot juice by minimising the physicochemical changes during storage, retarding microbial growth and retaining the bioactive compounds. Copyright © 2014 Elsevier Ltd. All rights reserved.

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

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.

Teratogenicity in vitro of two deacetylated metabolites of N-hydroxy-2-acetylaminofluorene.

PubMed

Faustman-Watts, E M; Greenaway, J C; Namkung, M J; Fantel, A G; Juchau, M R

1984-10-01

In previous studies [E. Faustman-Watts, J. C. Greenaway, M. J. Namkung, A. G. Fantel, and M. R. Juchau (1983) Teratology 27, 19-28] an embryo culture system was utilized to investigate the role of biotransformation in the embryotoxicity of 2-acetylaminofluorene. For this investigation, the capacity of two deacetylated metabolites of N-hydroxy-2-acetylaminofluorene (N-OH-AAF) to produce malformations in cultured whole rat embryos is reported. The relative capacities of N-hydroxy-2-aminofluorene (N-OH-AF) and 2-nitrosofluorene (NF) to elicit embryotoxic effects, including embryolethality, malformations, growth retardation, and alterations in macromolecular content, were assessed and compared with effects produced by N-OH-AAF and bioactivated 2-acetylaminofluorene (AAF). Qualitatively similar patterns of malformations were produced by NF and N-OH-AF. At initial concentrations greater than 60 microM, both deacetylated compounds caused abnormalities in axial rotation (flexure), decreased viability, and decreases in embryonic DNA and protein content. Both chemicals were active in the absence of a bioactivating system. AAF produced a different spectrum of defects, and was active only in the presence of a complete monooxygenase system. The malformations produced by bioactivated AAF included abnormally open neural tubes; flexure abnormalities were rarely observed. The primary defect elicited by N-OH-AAF was prosencephalic hypoplasia. This chemical was active without an added bioactivating system. Temporal studies demonstrated that exposure of embryos to NF (128 microM) for as little as 2 hr was sufficient to elicit embryotoxic effects. None of the individual metabolites appeared to be solely responsible for the interruptions of neural tube closure produced by bioactivated AAF.

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

The effects of marine carbohydrates and glycosylated compounds on human health.

PubMed

Kang, Hee-Kyoung; Seo, Chang Ho; Park, Yoonkyung

2015-03-16

Marine organisms have been recognized as a valuable source of bioactive compounds with industrial and nutraceutical potential. Recently, marine-derived carbohydrates, including polysaccharides and low molecular weight glycosylated oligosaccharides, have attracted much attention because of their numerous health benefits. Moreover, several studies have reported that marine carbohydrates exhibit various biological activities, including antioxidant, anti-infection, anticoagulant, anti-inflammatory, and anti-diabetic effects. The present review discusses the potential industrial applications of bioactive marine carbohydrates for health maintenance and disease prevention. Furthermore, the use of marine carbohydrates in food, cosmetics, agriculture, and environmental protection is discussed.

[Bioactive constituents from whole herbs of Vernonia cinerea (II)].

PubMed

Zhu, Huaxu; Tang, Yuping; Min, Zhida; Gong, Zhunan

2009-11-01

To study the constituents of the whole herbs of Vernonia cinerea by bio-activity guided isolation with PC-12 model. The constituents were separated by column chromatography and the structures were elucidated by spectroscopic methods. Ten compounds were identified to be (-)-clovane-2,9-diol (1), caryolane-1,9beta-diol (2), apigenin (3), chrysoeriol (4), luteolin (5), thermopsoside (6), luteolin-7-O-beta-D-glucoside (7), quercetin(8), apigenin-4'-O-beta-D-glucoside (9), hyperin (10), beta-amyrin aceate (11), lupeol acetate (12). Compounds 1, 2, 6 and 10 were isolated from this genus for the first time.

The Effects of Marine Carbohydrates and Glycosylated Compounds on Human Health

PubMed Central

Kang, Hee-Kyoung; Seo, Chang Ho; Park, Yoonkyung

2015-01-01

Marine organisms have been recognized as a valuable source of bioactive compounds with industrial and nutraceutical potential. Recently, marine-derived carbohydrates, including polysaccharides and low molecular weight glycosylated oligosaccharides, have attracted much attention because of their numerous health benefits. Moreover, several studies have reported that marine carbohydrates exhibit various biological activities, including antioxidant, anti-infection, anticoagulant, anti-inflammatory, and anti-diabetic effects. The present review discusses the potential industrial applications of bioactive marine carbohydrates for health maintenance and disease prevention. Furthermore, the use of marine carbohydrates in food, cosmetics, agriculture, and environmental protection is discussed. PMID:25785562

New Therapeutic Drugs from Bioactive Natural Molecules: the Role of Gut Microbiota Metabolism in Neurodegenerative Diseases.

PubMed

Di Meo, Francesco; Donato, Stella; Di Pardo, Alba; Maglione, Vittorio; Filosa, Stefania; Crispi, Stefania

2018-04-03

The gut-brain axis is considered a neuroendocrine system, which connects brain and gastrointestinal tract and plays an important role in stress response. The homeostasis of gut-brain axis is important for healthy conditions and its alterations are associated to neurological disorders and neurodegenerative diseases. Gut microbiota is a dynamic ecosystem that can be altered by external factors such as diet composition, antibiotics or xenobiotics. Recent advances in gut microbiota analyses indicate that the gut bacterial community plays a key role in maintaining normal brain functions. Recent metagenomic analyses have elucidated that the relationship between gut and brain, either in normal or in pathological conditions, reflects the existence of a "microbiota-gut-brain" axis. Gut microbiota composition can be influenced by dietary ingestion of probiotics or natural bioactive molecules such as prebiotics and polyphenols. Their derivatives coming from microbiota metabolism can affect both gut bacterial composition and brain biochemistry. Modifications of microbiota composition by natural bioactive molecules could be used to restore the altered brain functions, which characterize neurodegenerative diseases, leading to consider these compounds as novel therapeutic strategies for the treatment of neuropathologies. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

Vibrational spectra and natural bond orbital analysis of organic crystal L-prolinium picrate

NASA Astrophysics Data System (ADS)

Edwin, Bismi; Amalanathan, M.; Hubert Joe, I.

2012-10-01

Vibrational spectral analysis and quantum chemical computations based on density functional theory (DFT) have been performed on the organic crystal L-prolinium picrate (LPP). The equilibrium geometry, various bonding features and harmonic vibrational wavenumbers of LPP have been investigated using B3LYP method. The calculated molecular geometry has been compared with the experimental data. The detailed interpretation of the vibrational spectra has been carried out with the aid of VEDA 4 program. The various intramolecular interactions confirming the biological activity of the compound have been exposed by natural bond orbital analysis. The distribution of Mulliken atomic charges and bending of natural hybrid orbitals associated with hydrogen bonding also reflects the presence of intramolecular hydrogen bonding thereby enhancing bioactivity. The analysis of the electron density of HOMO and LUMO gives an idea of the delocalization and low value of energy gap indicates electron transport in the molecule and thereby bioactivity. Vibrational analysis reveals the presence of strong O-H⋯O and N-H⋯O interaction between L-prolinium and picrate ions providing evidence for the charge transfer interaction between the donor and acceptor groups and is responsible for its bioactivity.

Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis.

PubMed

Pamunuwa, Geethi; Karunaratne, D Nedra; Waisundara, Viduranga Y

2016-01-01

This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means.