Muhammad, Abubakar Amali; Pauzi, Nur Aimi Syarina; Arulselvan, Palanisamy; Abas, Faridah; Fakurazi, Sharida
Moringa oleifera Lam. (M. oleifera) from the monogeneric family Moringaceae is found in tropical and subtropical countries. The present study was aimed at exploring the in vitro wound healing potential of M. oleifera and identification of active compounds that may be responsible for its wound healing action. The study included cell viability, proliferation, and wound scratch test assays. Different solvent crude extracts were screened, and the most active crude extract was further subjected to differential bioguided fractionation. Fractions were also screened and most active aqueous fraction was finally obtained for further investigation. HPLC and LC-MS/MS analysis were used for identification and confirmation of bioactive compounds. The results of our study demonstrated that aqueous fraction of M. oleifera significantly enhanced proliferation and viability as well as migration of human dermal fibroblast (HDF) cells compared to the untreated control and other fractions. The HPLC and LC-MS/MS studies revealed kaempferol and quercetin compounds in the crude methanolic extract and a major bioactive compound Vicenin-2 was identified in the bioactive aqueous fraction which was confirmed with standard Vicenin-2 using HPLC and UV spectroscopic methods. These findings suggest that bioactive fraction of M. oleifera containing Vicenin-2 compound may enhance faster wound healing in vitro. PMID:24490175
Lee, Chia-Pu; Yen, Gow-Chin
The oil of tea seed (Camellia oleifera Abel.) is used extensively in China as cooking oil. The objectives of this study were to investigate the antioxidant activity of tea seed oil and its active compounds. Of the five solvent extracts, methanol extract of tea seed oil exhibited the highest yield and the strongest antioxidant activity as determined by DPPH scavenging activity and Trolox equivalent antioxidant capacity (TEAC). Two peaks separated from the methanol extract by HPLC contributed the most significant antioxidant activity. These two peaks were further identified as sesamin and a novel compound: 2,5-bis-benzo[1,3]dioxol-5-yl-tetrahydro-furo [3,4-d][1,3]dioxine (named compound B) by UV absorption and characterized by MS, IR, 1H NMR, and 13C NMR techniques. Sesamin and compound B decreased H2O2-mediated formation of reactive oxygen species in red blood cells (RBCs), inhibited RBCs hemolysis induced by AAPH, and increased the lag time of conjugated dienes formation in human low-density lipoprotein. The results indicate that both compounds isolated from tea seed oil exhibit remarkable antioxidant activity. Apart from the traditional pharmacological effects of Camellia oleifera, the oil of tea seed may also act as a prophylactic agent to prevent free radical related diseases.
Karthivashan, Govindarajan; Tangestani Fard, Masoumeh; Arulselvan, Palanisamy; Abas, Faridah; Fakurazi, Sharida
Free radicals trigger chain reaction and inflict damage to the cells and its components, which in turn ultimately interrupts their biological activities. To prevent free radical damage, together with an endogenous antioxidant system, an exogenous supply of antioxidant components to the body in the form of functional food or nutritional diet helps undeniably. Research conducted by the Natl. Inst. of Health claimed that Moringa oleifera Lam possess the highest antioxidant content among various natural food sources based on an oxygen radical absorbent capacity assay. In this study, a 90% (ethanol:distilled water--90:10) gradient solvent was identified as one of the best gradient solvents for the effectual extraction of bioactive components from M. oleifera leaves. This finding was confirmed by various antioxidant assays, including radical scavenging activity (that is, 1, 1-diphenyl-2-picrylhydrazyl, H(2)O(2), and NO radical scavenging assay) and total antioxidant capacity (that is, ferric reducing antioxidant power and molybdenum assay). High-performance liquid chromatography (HPLC) fingerprints of the 90% gradient extract visually showed few specific peaks, which on further analysis, using HPLC-DAD-ESI-MS, were identified as flavonoids and their derivatives. Despite commonly reported flavonoids, that is, kaempferol and quercetin, we report here for the 1st time the presence of multiflorin-B and apigenin in M. oleifera leaves. These findings might help researchers to further scrutinize this high activity exhibiting gradient extract and its bio-active candidates for fruitful clinical/translational investigations.
Fard, Masoumeh Tangestani; Arulselvan, Palanisamy; Karthivashan, Govindarajan; Adam, Siti Khadijah; Fakurazi, Sharida
Introduction: Inflammation is a well-known physiological response to protect the body against infection and restore tissue injury. Nevertheless, the chronic inflammation can trigger various inflammatory associated diseases/disorder. Moringa oleifera is a widely grown plant in most tropical countries and it has been recognized traditionally for several medicinal benefits. Objectives: The objective of this study was to investigate the anti-inflammatory properties of M. oleifera extract on lipopolysaccharide (LPS) - stimulated macrophages. Materials and Methods: The anti-inflammatory effect of M. oleifera hydroethanolic bioactive leaves extracts was evaluated by assessing the inhibition of nitric oxide (NO) production during Griess reaction and the expression of pro-inflammatory mediators in macrophages. Results: Interestingly, we found that M. oleifera hydroethanolic bioactive leaves extract significantly inhibited the secretion of NO production and other inflammatory markers such as prostaglandin E2, tumor necrosis factor alpha, interleukin (IL)-6, and IL-1β. Meanwhile, the bioactive extract has induced the production of IL-10 in a dose-dependent manner. In addition, M. oleifera hydroethanolic bioactive leaves extract effectively suppressed the protein expression of inflammatory markers inducible NO synthase, cyclooxygenase-2, and nuclear factor kappa-light-chain-enhancer of activated B-cells p65 in LPS-induced RAW264.7 macrophages in a dose-dependent manner. Conclusion: These findings support the traditional use of M. oleifera plant as an effective treatment for inflammation associated diseases/disorders. SUMMARY Hydroethanolic extracts of Moringa oleifera effectively inhibit the NO production in LPS induced inflammatory model.M. oleifera crude extracts successfully modulate the production of pro-inflammatory mediators in LPS stimulated macrophages.M. oleifera extracts suppressed the expression of inflammatory mediators in LPS stimulated macrophages. PMID:27013794
Moringa oleifera (MO) is used for a number of therapeutic purposes. This raises the question of safety and possible toxicity. The objective of the study was to ascertain the safety and possible metabolic toxicity in comparison with metformin, a known drug associated with acidosis. Animals confirmed with diabetes were grouped into 2 groups. The control group only received oral dose of PBS while the test group was treated with ethanolic extract of MO orally twice daily for 5-6 days. Data showed that the extract significantly lowered glucose level to normal values and did not cause any significant cytotoxicity compared to the control group (P = 0.0698); there was no gain in weight between the MO treated and the control groups (P > 0.8115). However, data showed that treatment with an ethanolic extract of MO caused a decrease in bicarbonate (P < 0.0001), and more than twofold increase in anion gap (P < 0.0001); metformin treatment also decreased bicarbonate (P < 0.0001) and resulted in a threefold increase in anion gap (P < 0.0001). Conclusively, these data show that while MO appears to have antidiabetic and noncytotoxic properties, it is associated with statistically significant anion gap acidosis in alloxan induced type 2 diabetic rats. PMID:25548560
Omabe, Maxwell; Nwudele, Chibueze; Omabe, Kenneth Nwobini; Okorocha, Albert Egwu
Moringa oleifera (MO) is used for a number of therapeutic purposes. This raises the question of safety and possible toxicity. The objective of the study was to ascertain the safety and possible metabolic toxicity in comparison with metformin, a known drug associated with acidosis. Animals confirmed with diabetes were grouped into 2 groups. The control group only received oral dose of PBS while the test group was treated with ethanolic extract of MO orally twice daily for 5-6 days. Data showed that the extract significantly lowered glucose level to normal values and did not cause any significant cytotoxicity compared to the control group (P = 0.0698); there was no gain in weight between the MO treated and the control groups (P > 0.8115). However, data showed that treatment with an ethanolic extract of MO caused a decrease in bicarbonate (P < 0.0001), and more than twofold increase in anion gap (P < 0.0001); metformin treatment also decreased bicarbonate (P < 0.0001) and resulted in a threefold increase in anion gap (P < 0.0001). Conclusively, these data show that while MO appears to have antidiabetic and noncytotoxic properties, it is associated with statistically significant anion gap acidosis in alloxan induced type 2 diabetic rats.
Pierson, Jean T; Dietzgen, Ralf G; Shaw, Paul N; Roberts-Thomson, Sarah J; Monteith, Gregory R; Gidley, Michael J
The plant kingdom harbours many diverse bioactive molecules of pharmacological relevance. Temperate fruits and vegetables have been highly studied in this regard, but there have been fewer studies of fruits and vegetables from the tropics. As global consumers demand and are prepared to pay for new appealing and exotic foods, tropical fruits are now being more intensively investigated. Polyphenols and major classes of compounds like flavonoids or carotenoids are ubiquitously present in these fruits, as they are in the temperate ones, but particular classes of compounds are unique to tropical fruits and other plant parts. Bioactivity studies of compounds specific to tropical fruit plants may lead to new drug discoveries, while the synergistic action of the wide range of diverse compounds contained in plant extracts underlies nutritional and health properties of tropical fruits and vegetables. The evidence for in vitro and animal bioactivities is a strong indicator of the pharmacological promise shown in tropical fruit plant biodiversity. In this review, we will discuss both the occurrence of potential bioactive compounds isolated and identified from a selection of tropical fruit plants of importance in Australia, as well as recent studies of bioactivity associated with such fruits and other fruit plant parts.
Song, Kun; Zhang, Jian; Zhang, Peng; Wang, Hong-Qing; Liu, Chao; Li, Bao-Ming; Kang, Jie; Chen, Ruo-Yun
Five new bioactive compounds, chenopodiumamines A-D (1-4) and chenopodiumoside A (5), were isolated from the ethanol extract of Chenopodium ambrosioides. The structures of these compounds were elucidated by various spectroscopic means (UV, IR, HR-ESI-MS, 1D and 2D NMR). Compounds 1-3 had moderate antioxidant and anti-inflammatory activities.
Sanglier, J J; Wellington, E M; Behal, V; Fiedler, H P; Ellouz Ghorbel, R; Finance, C; Hacene, M; Kamoun, A; Kelly, C; Mercer, D K
Actinomycetes form an enormous reservoir of secondary metabolites and enzymes. The potential for exploiting rare actinomycetes is highlighted by the discovery of novel compounds from strains of Spirillospora and Nocardioides. Novel compounds of well known classes of antibiotics, such as polyenes, continue to be discovered. For compounds containing a chromophore, the analysis by high-performance liquid chromatography coupled with a diode-array detector enables the elimination of producers of known compounds and facilitates the discovery of novel compounds or derivatives. The complexity of the regulatory mechanisms is illustrated by glutamine synthetase. The characterization of thermostable amylolytic, lignolytic, peroxidase and neuramidase activities, and the isolation of novel cellulolytic actinomycetes clearly demonstrate the potential of Actinomycetes as producers of enzymes.
Jaiganesh, R; Sampath Kumar, N S
Thousands of novel compounds have been isolated from various marine bacteria and tested for pharmacological properties, many of which are commercially available. Many more are being tested as potential bioactive compound at the preclinical and clinical stages. The growing interest in marine-derived antiviral compounds, along with the development of new technology in marine cultures and extraction, will significantly expedite the current exploration of the marine environment for compounds with significant pharmacological applications, which will continue to be a promising strategy and new trend for modern medicine. Marine actinomycetes and cyanobacteria are a prolific but underexploited source for the discovery of novel secondary metabolites.
Kiuru, Paula; DʼAuria, M Valeria; Muller, Christian D; Tammela, Päivi; Vuorela, Heikki; Yli-Kauhaluoma, Jari
Biodiversity in the seas is only partly explored, although marine organisms are excellent sources for many industrial products. Through close co-operation between industrial and academic partners, it is possible to successfully collect, isolate and classify marine organisms, such as bacteria, fungi, micro- and macroalgae, cyanobacteria, and marine invertebrates from the oceans and seas globally. Extracts and purified compounds of these organisms can be studied for several therapeutically and industrially significant biological activities, including anticancer, anti-inflammatory, antiviral, antibacterial, and anticoagulant activities by applying a wide variety of screening tools, as well as for ion channel/receptor modulation and plant growth regulation. Chromatographic isolation of bioactive compounds will be followed by structural determination. Sustainable cultivation methods for promising organisms and biotechnological processes for selected compounds can be developed, as well as biosensors for monitoring the target compounds. The (semi)synthetic modification of marine-based bioactive compounds produces their new derivatives, structural analogs and mimetics that could serve as hit or lead compounds and be used to expand compound libraries based on marine natural products. The research innovations can be targeted for industrial product development in order to improve the growth and productivity of marine biotechnology. Marine research aims at a better understanding of environmentally conscious sourcing of marine biotechnology products and increased public awareness of marine biodiversity. Marine research is expected to offer novel marine-based lead compounds for industries and strengthen their product portfolios related to pharmaceutical, nutraceutical, cosmetic, agrochemical, food processing, material and biosensor applications.
Pan, Wenhui; Liu, Kanglun; Guan, Yifu; Tan, Ghee Teng; Hung, Nguyen Van; Cuong, Nguyen Manh; Soejarto, D. Doel; Pezzuto, John M.; Fong, Harry H.S.; Zhang, Hongjie
A new lignan, vitexkarinol (1), as well as a known lignan, neopaulownin (2), a known chalcone, 3-(4-hydroxyphenyl)-1-(2,4,6-trimethoxyphenyl)-2-propen-1-one (3), two known dehydroflavones, tsugafolin (4) and alpinetin (5), two known dipeptides, aurantiamide and aurantiamide acetate, a known sesquiterpene, vemopolyanthofuran, and five known carotenoid metabolites, vomifoliol, dihydrovomifoliol, dehydrovomifoliol, loliolide and isololiolide, were isolated from the leaves and twigs of Vitex leptobotrys through bioassay-guided fractionation. The chalcone (3) was found to inhibit HIV-1 replication by 77% at 15.9 µM, and the two dehydroflavones (4 and 5) showed weak anti-HIV activity with IC50 values of 118 and 130 µM, respectively, while being devoid of cytotoxicity at 150 µM. A chlorophyll-enriched fraction of V. leptobotrys, containing pheophorbide a, was found to inhibit the replication of HIV-1 by 80% at a concentration of 10 µg/mL. Compounds 1 and 3 were further selected to be evaluated against 21 viral targets available at NIAID (National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, MD). PMID:24404757
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.
Bailão, Elisa Flávia Luiz Cardoso; Devilla, Ivano Alessandro; da Conceição, Edemilson Cardoso; Borges, Leonardo Luiz
Functional foods include any natural product that presents health-promoting effects, thereby reducing the risk of chronic diseases. Cerrado fruits are considered a source of bioactive substances, mainly phenolic compounds, making them important functional foods. Despite this, the losses of natural vegetation in the Cerrado are progressive. Hence, the knowledge propagation about the importance of the species found in Cerrado could contribute to the preservation of this biome. This review provides information about Cerrado fruits and highlights the structures and pharmacologic potential of functional compounds found in these fruits. Compounds detected in Caryocar brasiliense Camb. (pequi), Dipteryx alata Vog. (baru), Eugenia dysenterica DC. (cagaita), Eugenia uniflora L. (pitanga), Genipa americana L. (jenipapo), Hancornia speciosa Gomes (mangaba), Mauritia flexuosa L.f. (buriti), Myrciaria cauliflora (DC) Berg (jabuticaba), Psidium guajava L. (goiaba), Psidium spp. (araçá), Solanum lycocarpum St. Hill (lobeira), Spondias mombin L. (cajá), Annona crassiflora Mart. (araticum), among others are reported here. PMID:26473827
Muhammad, Abubakar Amali; Arulselvan, Palanisamy; Cheah, Pike See; Abas, Farida; Fakurazi, Sharida
Diabetic foot ulcer is a serious complication of diabetes, which affects a significant percentage (15%) of diabetics and up to 15%–24% of those affected may require amputation. Therefore, the economic burden of diabetic foot ulcers is enormous and is associated with high cost of treatment and prolongs hospitalization. The present study was conducted to evaluate antibacterial and in vivo wound healing activities of an aqueous fraction of Moringa oleifera on a diabetic condition. Antibacterial activity testing was carried out using agar well and tube dilution techniques. The in vivo study was conducted using six groups of animals that comprise of one normal and diabetic control group each, three treatment groups of 0.5%, 1%, and 2% w/w aqueous fraction, and a positive control group (1% w/w silver sulfadiazine). Rats were induced with diabetes using a combination of streptozotocin 65 and 150 mg/kg nicotinamide daily for 2 days, and excision wounds were created and treated with various doses (0.5%, 1%, and 2% w/w aqueous fraction) daily for 21 days. Biophysical, histological, and biochemical parameters were investigated. The results of the study revealed that aqueous fraction possessed antibacterial activity through inhibition of growth of Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli organisms. The topical application of aqueous fraction revealed enhancement of wound healing under sustained hyperglycemic condition for the duration of the experiment. This enhancement was achieved through decreased wound size, improved wound contraction, and tissue regeneration, as well as downregulation of inflammatory mediators, such as tumor necrosis factor-α, interleukin-1β, interleukin-6, inducible nitric oxide synthase, and cyclooxygenase-2, and upregulation of an angiogenic marker vascular endothelial growth factor in wound tissue treated with various doses of aqueous fraction of M. oleifera. The findings suggest that aqueous fraction of M. oleifera
Mao, Xiangzhao; Liu, Zhen; Sun, Jianan; Lee, Sang Yup
Many marine bioactive compounds have medicinal and nutritional values. These bioactive compounds have been prepared using solvent-based extraction from marine bio-resources or chemical synthesis, which are costly, inefficient with low yields, and environmentally unfriendly. Recent advances in metabolic engineering allowed to some extent more efficient production of these compounds, showing promises to meet the increasing demand of marine natural bioactive compounds. In this paper, we review the strategies and statuses of metabolic engineering applied to microbial production of marine natural bioactive compounds including terpenoids and their derivatives, omega-3 polyunsaturated fatty acids, and marine natural drugs, and provide perspectives.
Plaza, M; Santoyo, S; Jaime, L; García-Blairsy Reina, G; Herrero, M; Señoráns, F J; Ibáñez, E
In the present work, a comprehensive methodology to carry out the screening for novel natural functional compounds is presented. To do that, a new strategy has been developed including the use of unexplored natural sources (i.e., algae and microalgae) together with environmentally clean extraction techniques and advanced analytical tools. The developed procedure allows also estimating the functional activities of the different extracts obtained and even more important, to correlate these activities with their particular chemical composition. By applying this methodology it has been possible to carry out the screening for bioactive compounds in the algae Himanthalia elongata and the microalgae Synechocystis sp. Both algae produced active extracts in terms of both antioxidant and antimicrobial activity. The obtained pressurized liquid extracts were chemically characterized by GC-MS and HPLC-DAD. Different fatty acids and volatile compounds with antimicrobial activity were identified, such as phytol, fucosterol, neophytadiene or palmitic, palmitoleic and oleic acids. Based on the results obtained, ethanol was selected as the most appropriate solvent to extract this kind of compounds from the natural sources studied.
Kim, Seong-Eun; Hwang, Byung Soon; Song, Ja-Gyeong; Lee, Seung Woong; Lee, In-Kyoung
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
Rein, Maarit J.; Renouf, Mathieu; Cruz‐Hernandez, Cristina; Actis‐Goretta, Lucas; Thakkar, Sagar K.; da Silva Pinto, Marcia
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
Rein, Maarit J; Renouf, Mathieu; Cruz-Hernandez, Cristina; Actis-Goretta, Lucas; Thakkar, Sagar K; da Silva Pinto, Marcia
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.
Champagne, Claude P; Fustier, Patrick
The development of functional foods through the addition of bioactive compounds holds many technological challenges. Microencapsulation is a useful tool to improve the delivery of bioactive compounds into foods, particularly probiotics, minerals, vitamins, phytosterols, lutein, fatty acids, lycopene and antioxidants. Several microencapsulation technologies have been developed for use in the food industry and show promise for the production of functional foods. Moreover, these technologies could promote the successful delivery of bioactive ingredients to the gastrointestinal tract. Future research is likely to focus on aspects of delivery and the potential use of co-encapsulation methodologies, where two or more bioactive ingredients can be combined to have a synergistic effect.
Samy, Ramar Perumal; Pushparaj, Peter Natesan; Gopalakrishnakone, Ponnampalam
This review deals with the key bioactive compounds and the role of medicinal plants in Ayurvedic systems of medicine in India and their earlier investigation. There has been an increase in demand for the Phytopharmaceutical products of Ayurvĕda in Western countries, because of the fact that the allopathic drugs have more side effects. Many pharmaceutical companies are now concentrating on manufacturing of Ayurvĕdic Phytopharmaceutical products. Ayurvĕda is the Indian traditional system of medicine, which also deals about pharmaceutical science. Different type of plant parts used for the Ayurvedic formulation; overall out line of those herbal scenario and its future prospects for the scientific evaluation of medicinal plants used by traditional healers are also discussed. In India most of them, where Ayurvedic treatment is frequently used, for their ailments and provides instructions to local people how to prepare medicine from the herbs. As much as possible importance is also given for the taxonomic literature. PMID:19238245
Rivera, Melissa C; Pinheiro, Ana C; Bourbon, Ana I; Cerqueira, Miguel A; Vicente, António A
This work aimed at the development of biodegradable nanocapsules as carriers of two bioactive compounds, 5-aminosalycilic acid and glycomacropeptide. Nanocapsules were produced through layer-by-layer (LbL) deposition of chitosan (CH) and alginate (ALG) layers on polystyrene nanoparticles. The bioactive compounds were incorporated on the third layer of the nanocapsules being its encapsulation efficiency and release behaviour evaluated. The LbL deposition process, stability, morphology and size of the multilayer nanocapsules were monitored by means of zeta potential and transmission electron microscopy (TEM). The bioactive compounds release from the CH/ALG nanocapsules was successfully described by a mathematical model (linear superimposition model - LSM), which allowed concluding that bioactive compounds release is due to both Brownian motion and the polymer relaxation of the CH/ALG layers. Final results demonstrated that the synthesized LbL hollow nanocapsules presented spherical morphology and a good capacity to encapsulate different bioactive compounds, being the best results obtained for the system containing 5-aminosalycilic acid (with an encapsulation efficiency of approximately 70%). CH/ALG multilayer nanocapsules could be a promising carrier of bioactive compounds for applications in food and pharmaceutical industries.
Karthivashan, Govindarajan; Arulselvan, Palanisamy; Alimon, Abd. Razak; Safinar Ismail, Intan; Fakurazi, Sharida
The influence of Moringa oleifera (MO) leaf extract as a dietary supplement on the growth performance and antioxidant parameters was evaluated on broiler meat and the compounds responsible for the corresponding antioxidant activity were identified. 0.5%, 1.0%, and 1.5% w/v of MO leaf aqueous extracts (MOLE) were prepared, and nutritional feed supplemented with 0%, 0.5%, 1.0%, and 1.5% w/w of MO leaf meal (MOLM) extracts were also prepared and analysed for their in vitro antioxidant potential. Furthermore, the treated broiler groups (control (T1) and treatment (T2, T3, and T4)) were evaluated for performance, meat quality, and antioxidant status. The results of this study revealed that, among the broilers fed MOLM, the broilers fed 0.5% w/w MOLM (T2) exhibited enhanced meat quality and antioxidant status (P < 0.05). However, the antioxidant activity of the MOLE is greater than that of the MOLM. The LC-MS/MS analysis of MOLM showed high expression of isoflavones and fatty acids from soy and corn source, which antagonistically inhibit the expression of the flavonoids/phenols in the MO leaves thereby masking its antioxidant effects. Thus, altering the soy and corn gradients in conventional nutrition feed with 0.5% w/w MO leaves supplement would provide an efficient and cost-effective feed supplement. PMID:25793214
Skrovankova, Sona; Sumczynski, Daniela; Mlcek, Jiri; Jurikova, Tunde; Sochor, Jiri
Berries, especially members of several families, such as Rosaceae (strawberry, raspberry, blackberry), and Ericaceae (blueberry, cranberry), belong to the best dietary sources of bioactive compounds (BAC). They have delicious taste and flavor, have economic importance, and because of the antioxidant properties of BAC, they are of great interest also for nutritionists and food technologists due to the opportunity to use BAC as functional foods ingredients. The bioactive compounds in berries contain mainly phenolic compounds (phenolic acids, flavonoids, such as anthocyanins and flavonols, and tannins) and ascorbic acid. These compounds, either individually or combined, are responsible for various health benefits of berries, such as prevention of inflammation disorders, cardiovascular diseases, or protective effects to lower the risk of various cancers. In this review bioactive compounds of commonly consumed berries are described, as well as the factors influencing their antioxidant capacity and their health benefits. PMID:26501271
Skrovankova, Sona; Sumczynski, Daniela; Mlcek, Jiri; Jurikova, Tunde; Sochor, Jiri
Berries, especially members of several families, such as Rosaceae (strawberry, raspberry, blackberry), and Ericaceae (blueberry, cranberry), belong to the best dietary sources of bioactive compounds (BAC). They have delicious taste and flavor, have economic importance, and because of the antioxidant properties of BAC, they are of great interest also for nutritionists and food technologists due to the opportunity to use BAC as functional foods ingredients. The bioactive compounds in berries contain mainly phenolic compounds (phenolic acids, flavonoids, such as anthocyanins and flavonols, and tannins) and ascorbic acid. These compounds, either individually or combined, are responsible for various health benefits of berries, such as prevention of inflammation disorders, cardiovascular diseases, or protective effects to lower the risk of various cancers. In this review bioactive compounds of commonly consumed berries are described, as well as the factors influencing their antioxidant capacity and their health benefits.
Pinho, Eva; Grootveld, Martin; Soares, Graça; Henriques, Mariana
Plants possess a wide range of molecules capable of improve healing: fibre, vitamins, phytosterols, and further sulphur-containing compounds, carotenoids, organic acid anions and polyphenolics. However, they require an adequate level of protection from the environmental conditions to prevent losing their structural integrity and bioactivity. Cyclodextrins are cyclic oligosaccharides arising from the degradation of starch, which can be a viable option as encapsulation technique. Cyclodextrins are inexpensive, friendly to humans, and also capable of improving the biological, chemical and physical properties of bioactive molecules. Therefore, the aim of this review is to highlight the use of cyclodextrins as encapsulating agents for bioactive plant molecules in the pharmaceutical field.
Debbab, Abdessamad; Aly, Amal H.; Lin, Wen H.; Proksch, Peter
Summary Marine bacteria and fungi are of considerable importance as new promising sources of a huge number of biologically active products. Some of these marine species live in a stressful habitat, under cold, lightless and high pressure conditions. Surprisingly, a large number of species with high diversity survive under such conditions and produce fascinating and structurally complex natural products. Up till now, only a small number of microorganisms have been investigated for bioactive metabolites, yet a huge number of active substances with some of them featuring unique structural skeletons have been isolated. This review covers new biologically active natural products published recently (2007–09) and highlights the chemical potential of marine microorganisms, with focus on bioactive products as well as on their mechanisms of action. PMID:21255352
Oh, Yoon Sin
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
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
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.
Oh, Yoon Sin
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.
Kudanga, Tukayi; Nemadziva, Blessing; Le Roes-Hill, Marilize
The demand for compounds of therapeutic value is increasing mainly because of new applications of bioactive compounds in medicine, pharmaceutical, agricultural, and food industries. This has necessitated the search for cost-effective methods for producing bioactive compounds and therefore the intensification of the search for enzymatic approaches in organic synthesis. Laccase is one of the enzymes that have shown encouraging potential as biocatalysts in the synthesis of bioactive compounds. Laccases are multicopper oxidases with a diverse range of catalytic activities revolving around synthesis and degradative reactions. They have attracted much attention as potential industrial catalysts in organic synthesis mainly because they are essentially green catalysts with a diverse substrate range. Their reaction only requires molecular oxygen and releases water as the only by-product. Laccase catalysis involves the abstraction of a single electron from their substrates to produce reactive radicals. The free radicals subsequently undergo homo- and hetero-coupling to form dimeric, oligomeric, polymeric, or cross-coupling products which have practical implications in organic synthesis. Consequently, there is a growing body of research focused on the synthetic applications of laccases such as organic synthesis, hair and textile dyeing, polymer synthesis, and grafting processes. This paper reviews the major advances in laccase-mediated synthesis of bioactive compounds, the mechanisms of enzymatic coupling, structure-activity relationships of synthesized compounds, and the challenges that might guide future research directions.
Bhatnagar, Ira; Kim, Se-Kwon
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.
Yang, Jian-Hong; Kondratyuk, Tamara P.; Jermihov, Katherine C.; Marler, Laura E.; Qiu, Xi; Choi, Yongsoo; Cao, Hongmei; Yu, Rui; Sturdy, Megan; Huang, Rong; Liu, Ying; Wang, Li-Qin; Mesecar, Andrew D.; van Breemen, Richard B.; Pezzuto, John M.; Fong, Harry H. S.; Chen, Ye-Gao; Zhang, Hong-Jie
Phytochemical investigation of the whole plant of Lepisorus contortus (Christ) Ching led to the isolation of five new phenylethanoid glycosides (1–5), each containing a caffeoyl group, a new flavonoid glycoside (10), as well as 14 known compounds (6–9 and 11–15, syringic acid, vanillic acid, phloretic acid, diplopterol, and β-sitosterol). This is the first report of phenylethanoid glycosides from the family Polypodiaceae. Compounds 1–15 were evaluated for their cancer chemopreventive potential based on their ability to inhibit tumor necrosis factor alpha (TNF-α)-induced NF-κB activity, nitric oxide (NO) production, aromatase, quinone reductase 2 (QR-2), and COX-1/-2 activities. Quercetin-3-O-β-D-glucoside (15) demonstrated inhibition against QR2 with an IC50 value of 6.7 µM, which confirmed kaempferol/quercetin glycosides as the active compounds to inhibit QR2. The compound also demonstrated NF-κB activity with an IC50 value of 33.6 µM. In addition, compounds 1, 2, 4 and 6 showed aromatase activity with IC50 values of 30.7, 32.3, 26.8, and 35.3 µM, respectively. PMID:21261296
Aguilar, M I; Delgado, G; Hernández, M L; Villarreal, M L
The novel bisabolene sesquiterpenes 3-6, were isolated from Iostephane heterophylla, using bioguided fractionation. The new compounds were determined to be (12R/12S)-12,13-epoxy-xanthorrhizols (3,4) and (12R/12S)-12,13-dihydro-12,13-dihydroxy-xanthorrizols (5,6) and their structures were characterized by analysis of spectroscopic data and by chemical correlation from xanthorrhizol (2). The stereochemistry at C-12 of 5 was deduced using the modified Mosher experiment. Some of the isolated compounds elicited activity against gram positive and gram negative bacteria, levadura and dermatophytes.
Cooper, M. R.; Douglas, G. L.
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
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
Narayana, Kolla J P; Prabhakar, Peddikotla; Vijayalakshmi, Muvva; Venkateswarlu, Yenamandra; Krishna, Palakodety S J
An attempt was made to study the bioactive compounds from a terrestrial Streptomyces sp. ANU 6277 isolated from laterite soil. Four active fractions were recovered from the solvent extracts obtained from the culture broth of five day-old strain. Three bioactive compounds were purified and identified as 3-phenylpropionic acid, anthracene-9,10-quinone and 8-hydroxyquinoline. The components of the partially purified fourth active fraction were analyzed by gas chromatography-mass spectrometry and identified as benzyl alcohol, phenylethyl alcohol and 2H-1, 4-benzoxazin-3 (4H)-one. Four active fractions were screened for antimicrobial activity against Gram-positive and Gram-negative bacteria, and fungi including phytopathogenic, toxigenic and dermatophytic genera. Among these metabolites, 8-hydroxyquinoline exhibited strong antibacterial and antifungal activity as compared to 3-phenylpropionic acid and anthracene-9,10-quinone.
Kelly, M S
biologically active compounds with biomedical applications. Sea cucumber has been valued in Chinese medicine for hundreds of years as a cure for a wide variety of ailments. Some more recently isolated compounds, mainly from sea cucumbers and starfish, and including those with antitumour, antiviral, anticoagulant and antimicrobial activity are summarised below. When wild stocks decline, the demand created in the market place raises to the price of the product and, consequently, culturing is more likely to become viable economically. As this review shows, there have been dramatic advances in the culture methods of sea urchins and sea cucumbers in the last 10-15 years, to the extent that one can conclude that currently the major obstacles to successful cultivation are indeed economic rather than biological. Hence the future of the echinoculture industry is closely linked to that of the fisheries, whose fate will ultimately determine the market forces that will shape this growing industry.
Azman, Adzzie-Shazleen; Othman, Iekhsan; Velu, Saraswati S; Chan, Kok-Gan; Lee, Learn-Han
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.
Azman, Adzzie-Shazleen; Othman, Iekhsan; Velu, Saraswati S.; Chan, Kok-Gan; Lee, Learn-Han
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
Chiet, Chong Hang; Zulkifli, Razauden Mohamed; Hidayat, Topik; Yaakob, Harisun
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.
Sun, Yujing; Rukeya, Japaer; Tao, Wenyang; Sun, Peilong; Ye, Xingqian
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
Sun, Yujing; Rukeya, Japaer; Tao, Wenyang; Sun, Peilong; Ye, Xingqian
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.
Shi, Shujuan; Feng, Wenjing; Hu, Song; Liang, Shixiu; An, Nina; Mao, Yongjun
Sea cucumbers belong to the Class Holothuroidea of marine invertebrates. They are commercially valuable and prized as a food and folk medicine in Asia. Nutritionally, sea cucumbers have an impressive profile of valuable nutrients such as vitamins, minerals and amino acids. A number of unique biological and pharmacological activities/properties, including anticancer, anticoagulant/antithrombotic, antimicrobial, antioxidant, antihyperlipidemic, antihyperglycemic, anti-inflammatory, antihypertension and radioprotective, have been ascribed to various compounds isolated from sea cucumbers. The therapeutic properties and medicinal benefits of sea cucumbers can be linked to the presence of a wide array of bioactives, especially triterpene glycosides, acid mucopolysaccharide, sphingoid bases, glycolipids, fucosylated chondroitin sulfate, polysaccharides, phospholipids, cerebrosides, phosphatidylcholines, and other extracts and hydrolysates. This review highlights the valuable bioactive components as well as the multiple therapeutic properties of sea cucumbers with a view to exploring their potential uses as functional foods and a natural source of new multifunctional drugs.
Borrás-Linares, Isabel; Stojanović, Zorica; Quirantes-Piné, Rosa; Arráez-Román, David; Švarc-Gajić, Jaroslava; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio
In an extensive search for bioactive compounds from plant sources, the composition of different extracts of rosemary leaves collected from different geographical zones of Serbia was studied. The qualitative and quantitative characterization of 20 rosemary (Rosmarinus officinalis) samples, obtained by microwave-assisted extraction (MAE), was determined by high performance liquid chromatography coupled to electrospray quadrupole-time of flight mass spectrometry (HPLC-ESI-QTOF-MS). The high mass accuracy and true isotopic pattern in both MS and MS/MS spectra provided by the QTOF-MS analyzer enabled the characterization of a wide range of phenolic compounds in the extracts, including flavonoids, phenolic diterpenes and abietan-type triterpenoids, among others. According to the data compiled, rosemary samples from Sokobanja presented the highest levels in flavonoids and other compounds such as carnosol, rosmaridiphenol, rosmadial, rosmarinic acid, and carnosic acid. On the other hand, higher contents in triterpenes were found in the extracts of rosemary from Gložan (Vojvodina).
Panda, Siva S
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.
Vasundhara, M.; Kumar, Anil; Reddy, M. Sudhakara
Endophytic fungi are capable of producing plant associated metabolites and their analogs with therapeutic value. In order to identify the potential endophytic isolates producing bioactive compounds, one need to screen all isolated endophytes, which may run into hundreds. Isolation of endophytic fungi is relatively a simple process; but screening of the isolated fungi for required metabolite production is a cumbersome process. Endophytic fungi producing plant associated metabolites may contain genes involved in the entire biosynthetic pathway(s). Therefore, ascertaining the presence of key enzymes of a particular biosynthetic pathway could serve as a molecular marker for screening of these endophytes to produce that metabolite. In absence of entire biosynthetic pathways in endophytic fungi, plant genes associated with that metabolic pathway could serve as markers. This review focuses on the impact of molecular approaches to screen the endophytic fungi for the production of bioactive compounds. An attempt has been made on screening of anticancer compounds like taxol (paclitaxel), podophyllotoxin, and camptothecin using molecular markers. The advantages of molecular approaches over conventional methods to screen endophytic fungi and also identification of endophytic fungi are discussed. PMID:27895623
Sasidharan, S; Chen, Y; Saravanan, D; Sundram, K M; Yoga Latha, L
Natural products from medicinal plants, either as pure compounds or as standardized extracts, provide unlimited opportunities for new drug leads because of the unmatched availability of chemical diversity. Due to an increasing demand for chemical diversity in screening programs, seeking therapeutic drugs from natural products, interest particularly in edible plants has grown throughout the world. Botanicals and herbal preparations for medicinal usage contain various types of bioactive compounds. The focus of this paper is on the analytical methodologies, which include the extraction, isolation and characterization of active ingredients in botanicals and herbal preparations. The common problems and key challenges in the extraction, isolation and characterization of active ingredients in botanicals and herbal preparations are discussed. As extraction is the most important step in the analysis of constituents present in botanicals and herbal preparations, the strengths and weaknesses of different extraction techniques are discussed. The analysis of bioactive compounds present in the plant extracts involving the applications of common phytochemical screening assays, chromatographic techniques such as HPLC and, TLC as well as non-chromatographic techniques such as immunoassay and Fourier Transform Infra Red (FTIR) are discussed.
Asnin, L; Park, S W
An overview of the state of the art in the extraction, isolation, and analytical determination of bioactive compounds in peppers of the genus Capsicum is presented. The review is structured by classes of phytochemicals. Both major and minor constituents of peppers are considered. Modern trends in analytical chemistry of nutrients in regard to pepper analysis with particular focus on chromatographic and related methods are discussed. Attention was paid to controversial questions of pepper analysis, including but not limited to problems of sample degradation and the completeness of extraction of target analytes. The rationale for choosing an optimal strategy of analysis is given.
Maldini, Mariateresa; Maksoud, Salwa A; Natella, Fausta; Montoro, Paola; Petretto, Giacomo Luigi; Foddai, Marzia; De Nicola, Gina Rosalinda; Chessa, Mario; Pintore, Giorgio
Moringa oleifera is a medicinal plant and an excellent dietary source of micronutrients (vitamins and minerals) and health-promoting phytochemicals (phenolic compounds, glucosinolates and isothiocyanates). Glucosinolates and isothiocyanates are known to possess anti-carcinogenic and antioxidant effects and have attracted great interest from both toxicological and pharmacological points of view, as they are able to induce phase 2 detoxification enzymes and to inhibit phase 1 activation enzymes. Phenolic compounds possess antioxidant properties and may exert a preventative effect in regards to the development of chronic degenerative diseases. The aim of this work was to assess the profile and the level of bioactive compounds in all parts of M. oleifera seedlings, by using different MS approaches. First, flow injection electrospray ionization mass spectrometry (FI-ESI-MS) fingerprinting techniques and chemometrics (PCA) were used to achieve the characterization of the different plant's organs in terms of profile of phenolic compounds and glucosinolates. Second, LC-MS and LC-MS/MS qualitative and quantitative methods were used for the identification and/or determination of phenolics and glucosinolates in M. oleifera.
Matshediso, Phatsimo G; Cukrowska, Ewa; Chimuka, Luke
Pressurised hot water extraction (PHWE) is a "green" technology which can be used for the extraction of essential components in Moringa oleifera leaf extracts. The behaviour of three flavonols (myricetin, quercetin and kaempferol) and total phenolic content (TPC) in Moringa leaf powder were investigated at various temperatures using PHWE. The TPC of extracts from PHWE were investigated using two indicators. These are reducing activity and the radical scavenging activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH). Flavonols content in the PHWE extracts were analysed on high performance liquid chromatography with ultra violet (HPLC-UV) detection. The concentration of kaempferol and myricetin started decreasing at 150 °C while that of quercetin remained steady with extraction temperature. Optimum extraction temperature for flavonols and DPPH radical scavenging activity was found to be 100 °C. The TPC increased with temperature until 150 °C and then decreased while the reducing activity increased.
Li, Kai; Ji, Shuai; Song, Wei; Kuang, Yi; Lin, Yan; Tang, Shunan; Cui, Zexu; Qiao, Xue; Yu, Siwang; Ye, Min
In an attempt to discover bioactive agents from the herbal medicine Glycyrrhiza glabra (widely known as licorice), 11 new phenolic compounds, glycybridins A-K (1-11), along with 47 known phenolics (12-58) were isolated. Their structures were elucidated on the basis of extensive NMR and MS analyses as well as experimental and computed ECD data. According to the clinical therapeutic effects of licorice, enzyme or cell-based bioactivity screenings of 1-58 were conducted. A number of compounds significantly activate Nrf2, inhibit tyrosinase or PTP1B, inhibit LPS-induced NO production and NF-κB transcription, and inhibit the proliferation of human cancer cells (HepG2, SW480, A549, MCF7). Glycybridin D (4) showed moderate cytotoxic activities against the four cancer cell lines, with IC50 values ranging from 4.6 to 6.6 μM. Further studies indicated that 4 (10 mg/kg, ip) decreased tumor mass by 39.7% on an A549 human lung carcinoma xenograft mice model, but showed little toxicity.
Côté, J; Caillet, S; Doyon, G; Sylvain, J-F; Lacroix, M
Cranberries are healthy fruit that contribute color, flavor, nutritional value, and functionality. They are one of only three fruits native to America. Over the past decade, public interest for the North American cranberry (Vaccinium macrocarpon) has been rising with reports of their potential health benefits linked to the numerous phytochemicals present in the fruit--the anthocyanins, the flavonols, the flavan-3-ols, the proanthocyanidins, and the phenolic acid derivatives. The presence of these phytochemicals appears to be responsible for the cranberry property of preventing many diseases and infections, including cardiovascular diseases, various cancers, and infections involving the urinary tract, dental health, and Helicobacter pylori-induced stomach ulcers and cancers. Recent years have seen important breakthroughs in our understanding of the mechanisms through which these compounds exert their beneficial biological effects, yet these remain to be scientifically substantiated. In this paper these characteristics, as well as the antioxidant, radical scavenging, antibacterial, antimutagen, and anticarcinogen properties of cranberry major bioactive compounds are explained.
Bermejo, A; Llosá, M J; Cano, A
Chemical content in peels of fruits belonging to cultivars of Clementine mandarin (Fino, Loretina and Marisol), Satsume mandarin (Owari), Navel orange (Navelate and Navelina) and Common orange (Valencia Late) groups have been analyzed. The influence of the variety on the content of bioactive constituents at the varietal level is discussed. Rind contents showed similar tendencies for the majority of compounds although Satsume group presented the highest amounts on the flavanone glycosides hesperidin and narirutin, as well as the highest amounts of the carotenoid and β-cryptoxanthin, comparing with the remaining varieties studied. Both mandarin and orange varieties studied showed similar tendencies concerning to other phenolic compounds and total ascorbic acid concentrations. Limonene was the most abundant peel essential oil in all cultivars studied, followed by myrcene. Calcium and potassium were the dominant macronutrients for each cultivar studied, although the proportion of the individual nutrients ranged among different cultivars.
Puupponen-Pimiä, Riitta; Nohynek, Liisa; Alakomi, Hanna-Leena; Oksman-Caldentey, Kirsi-Marja
Berry fruits are rich sources of bioactive compounds, such as phenolics and organic acids, which have antimicrobial activities against human pathogens. Among different berries and berry phenolics, cranberry, cloudberry, raspberry, strawberry and bilberry especially possess clear antimicrobial effects against, e.g. Salmonella and Staphylococcus. Complex phenolic polymers, like ellagitannins, are strong antibacterial agents present in cloudberry and raspberry. Several mechanisms of action in the growth inhibition of bacteria are involved, such as destabilisation of cytoplasmic membrane, permeabilisation of plasma membrane, inhibition of extracellular microbial enzymes, direct actions on microbial metabolism and deprivation of the substrates required for microbial growth. Antimicrobial activity of berries may also be related to antiadherence of bacteria to epithelial cells, which is a prerequisite for colonisation and infection of many pathogens. Antimicrobial berry compounds may have important applications in the future as natural antimicrobial agents for food industry as well as for medicine. Some of the novel approaches are discussed.
Taveira, Marcos; Ferreres, Federico; Gil-Izquierdo, Angel; Oliveira, Luísa; Valentão, Patrícia; Andrade, Paula B
Lycopersicon esculentum leaves, usually considered as a by-product of tomato production, present several bioactive compounds of interest for industries like food, pharmaceutical and cosmetics. Nevertheless, before industrial application, suitable methods to identify and quantify those metabolites should be developed. In this study agitation with aqueous methanol was used for phenolic compounds extraction. Solid-phase extraction (SPE) was performed as the purification step before alkaloids analysis. Among the SPE sorbents tested, sulphonic acid bonded silica with H(+) counterion (SCX) proved to be the most efficient one for removing interfering components. Fifteen phenolics and four steroidic alkaloids were identified in 35 and 20 min analysis, respectively. The optimised methods were validated, revealing to be accurate, fast, simple and sensitive. Thus, these methods represent an easy and fast analytical approach, using equipment available in almost laboratory, which render them to be appropriate for routine analysis.
Sugumaran, Manickam; Robinson, William E.
The amino acid, tyrosine, and its hydroxylated product, 3,4-dihydroxyphenylalanine (dopa), plays an important role in the biogenesis of a number of potentially important bioactive molecules in marine organisms. Interestingly, several of these tyrosyl and dopa-containing compounds possess dehydro groups in their side chains. Examples span the range from simple dehydrotyrosine and dehydrodopamines to complex metabolic products, including peptides and polycyclic alkaloids. Based on structural information, these compounds can be subdivided into five categories: (a) Simple dehydrotyrosine and dehydrotyramine containing molecules; (b) simple dehydrodopa derivatives; (c) peptidyl dehydrotyrosine and dehydrodopa derivatives; (d) multiple dehydrodopa containing compounds; and (e) polycyclic condensed dehydrodopa derivatives. These molecules possess a wide range of biological activities that include (but are not limited to) antitumor activity, antibiotic activity, cytotoxicity, antioxidant activity, multidrug resistance reversal, cell division inhibition, immunomodulatory activity, HIV-integrase inhibition, anti-viral, and anti-feeding (or feeding deterrent) activity. This review summarizes the structure, distribution, possible biosynthetic origin, and biological activity, of the five categories of dehydrotyrosine and dehydrodopa containing compounds. PMID:21339956
Lay Ma, Ursula Vanesa
Interest in the use of many bioactive compounds in foods is growing in large part because of the apparent health benefits of these molecules. However, many of these compounds can be easily degraded during processing, storage, or their passage through the gastrointestinal tract before reaching the target site. In addition, they can be bitter, acrid, or astringent, which may negatively affect the sensory properties of the product. Encapsulation of these molecules may increase their stability during processing, storage, and in the gastrointestinal tract, while providing controlled release properties. The ability of amylose to form inclusion complexes and spherulites while entrapping certain compounds has been suggested as a potential method for encapsulation of certain molecules. However, complex formation and spherulitic crystallization are greatly affected by the type of inclusion molecules, type of starch, and processing conditions. The objectives of the present investigation were to: (a) study the effect of amylose, amylopectin, and intermediate material on spherulite formation and its microstructure; (b) investigate the formation of amylose and high amylose starch inclusion complexes with ascorbyl palmitate, retinyl palmitate, and phytosterol esters; (c) evaluate the ability of spherulites to form in the presence of fatty acid esters and to entrap ascorbyl palmitate, retinyl palmitate, and phytosterol esters; and (d) evaluate the effect of processing conditions on spherulite formation and fatty acid ester entrapment. Higher ratios of linear to branched molecules resulted in the formation of more and rounder spherulites with higher heat stability. In addition to the presence of branches, it appears that spherulitic crystallization is also affected by other factors, such as degree of branching, chain length, and chain length distribution. Amylose and Hylon VII starch formed inclusion complexes with fatty acid esters of ascorbic acid, retinol, or phytosterols
Karim, Nurul Ashikin Abd; Ibrahim, Muhammad Din; Kntayya, Saie Brindha; Rukayadi, Yaya; Hamid, Hazrulizawati Abd; Razis, Ahmad Faizal Abdull
Moringa oleifera Lam, family Moringaceae, is a perennial plant which is called various names, but is locally known in Malaysia as "murungai" or "kelor". Glucomoringin, a glucosinolate with from M. oleifera is a major secondary metabolite compound. The seeds and leaves of the plant are reported to have the highest amount of glucosinolates. M. oleifera is well known for its many uses health and benefits. It is claimed to have nutritional, medicinal and chemopreventive potentials. Chemopreventive effects of M. oleifera are expected due to the existence of glucosinolate which it is reported to have the ability to induce apoptosis in anticancer studies. Furthermore, chemopreventive value of M. oleifera has been demonstrated in studies utilizing its leaf extract to inhibit the growth of human cancer cell lines. This review highlights the advantages of M. oleifera targeting chemoprevention where glucosinolates could help to slow the process of carcinogenesis through several molecular targets. It is also includes inhibition of carcinogen activation and induction of carcinogen detoxification, anti-inflammatory, anti-tumor cell proliferation, induction of apoptosis and inhibition of tumor angiogenesis. Finally, for synergistic effects of M. oleifera with other drugs and safety, essential for chemoprevention, it is important that it safe to be consumed by human body and works well. Although there is promising evidence about M. oleifera in chemoprevention, extensive research needs to be done due to the expected rise of cancer in coming years and to gain more information about the mechanisms involved in M. oleifera influence, which could be a good source to inhibit several major mechanisms involved in cancer development.
Leone, Alessandro; Fiorillo, Giovanni; Criscuoli, Franca; Ravasenghi, Stefano; Santagostini, Laura; Fico, Gelsomina; Spadafranca, Angela; Battezzati, Alberto; Schiraldi, Alberto; Pozzi, Federica; di Lello, Sara; Filippini, Sandro; Bertoli, Simona
Moringa oleifera is a plant that grows in tropical and subtropical areas of the world. Its leaves are rich of nutrients and bioactive compounds. However, several differences are reported in the literature. In this article we performed a nutritional characterization and a phenolic profiling of M. oleifera leaves grown in Chad, Sahrawi refugee camps, and Haiti. In addition, we investigated the presence of salicylic and ferulic acids, two phenolic acids with pharmacological activity, whose presence in M. oleifera leaves has been scarcely investigated so far. Several differences were observed among the samples. Nevertheless, the leaves were rich in protein, minerals, and β-carotene. Quercetin and kaempferol glycosides were the main phenolic compounds identified in the methanolic extracts. Finally, salicylic and ferulic acids were found in a concentration range of 0.14–0.33 and 6.61–9.69 mg/100 g, respectively. In conclusion, we observed some differences in terms of nutrients and phenolic compounds in M. oleifera leaves grown in different countries. Nevertheless, these leaves are a good and economical source of nutrients for tropical and sub-tropical countries. Furthermore, M. oleifera leaves are a source of flavonoids and phenolic acids, among which salicylic and ferulic acids, and therefore they could be used as nutraceutical and functional ingredients. PMID:26274956
Leone, Alessandro; Fiorillo, Giovanni; Criscuoli, Franca; Ravasenghi, Stefano; Santagostini, Laura; Fico, Gelsomina; Spadafranca, Angela; Battezzati, Alberto; Schiraldi, Alberto; Pozzi, Federica; di Lello, Sara; Filippini, Sandro; Bertoli, Simona
Moringa oleifera is a plant that grows in tropical and subtropical areas of the world. Its leaves are rich of nutrients and bioactive compounds. However, several differences are reported in the literature. In this article we performed a nutritional characterization and a phenolic profiling of M. oleifera leaves grown in Chad, Sahrawi refugee camps, and Haiti. In addition, we investigated the presence of salicylic and ferulic acids, two phenolic acids with pharmacological activity, whose presence in M. oleifera leaves has been scarcely investigated so far. Several differences were observed among the samples. Nevertheless, the leaves were rich in protein, minerals, and β-carotene. Quercetin and kaempferol glycosides were the main phenolic compounds identified in the methanolic extracts. Finally, salicylic and ferulic acids were found in a concentration range of 0.14-0.33 and 6.61-9.69 mg/100 g, respectively. In conclusion, we observed some differences in terms of nutrients and phenolic compounds in M. oleifera leaves grown in different countries. Nevertheless, these leaves are a good and economical source of nutrients for tropical and sub-tropical countries. Furthermore, M. oleifera leaves are a source of flavonoids and phenolic acids, among which salicylic and ferulic acids, and therefore they could be used as nutraceutical and functional ingredients.
dos Santos, Mary de Fátima Guedes; Mamede, Rosa Virginia Soares; Rufino, Maria do Socorro Moura; de Brito, Edy Sousa; Alves, Ricardo Elesbão
The Amazon region has many sources of fruits, especially native ones not yet explored, but which have some potential for use, as is the case with certain palms. The objective of this study was to evaluate the content of bioactive compounds and total antioxidant capacities of fruits from native palms from the Brazilian Amazon. The fruits of five palm species (bacaba, buriti, inajá, pupunha, and tucumã) were evaluated for levels of ascorbic acid, anthocyanins, yellow flavonoids, total carotenoids, and total extractable polyphenols, as well as the total antioxidant capacities. The fruits had high contents of extractable total polyphenols, especially bacaba and tucumã (941.56 and 158.98 mg of galic acid·100g−1), total carotenoids in the case of tucumã and buriti (7.24 and 4.67 mg·100g−1), and anthocyanins in bacaba (80.76 mg·100g−1). As for the antioxidant capacity, bacaba had the highest total antioxidant activity by the Oxygen Radical Antioxidant Capacity (ORAC) (194.67 µM·Trolox·g−1), 2,2-diphenyl-1-picrylhydrazyl (DPPH) (47.46 g·pulp·g−1 DPPH), and β-carotene/linoleic acid (92.17% Oxidation Inhibition (O.I) methods. Bacaba phenolic profile revealed the presence of cyanidin-3-O-rutinoside and other flavonoids. The palm fruits studied can be considered good sources of bioactive compounds, some containing higher amounts than that of commonly consumed fruits. Total extractable polyphenols and anthocyanins were directly correlated to antioxidant activity in these fruits. PMID:26783846
Dos Santos, Mary de Fátima Guedes; Mamede, Rosa Virginia Soares; Rufino, Maria do Socorro Moura; de Brito, Edy Sousa; Alves, Ricardo Elesbão
The Amazon region has many sources of fruits, especially native ones not yet explored, but which have some potential for use, as is the case with certain palms. The objective of this study was to evaluate the content of bioactive compounds and total antioxidant capacities of fruits from native palms from the Brazilian Amazon. The fruits of five palm species (bacaba, buriti, inajá, pupunha, and tucumã) were evaluated for levels of ascorbic acid, anthocyanins, yellow flavonoids, total carotenoids, and total extractable polyphenols, as well as the total antioxidant capacities. The fruits had high contents of extractable total polyphenols, especially bacaba and tucumã (941.56 and 158.98 mg of galic acid·100g(-1)), total carotenoids in the case of tucumã and buriti (7.24 and 4.67 mg·100g(-1)), and anthocyanins in bacaba (80.76 mg·100g(-1)). As for the antioxidant capacity, bacaba had the highest total antioxidant activity by the Oxygen Radical Antioxidant Capacity (ORAC) (194.67 µM·Trolox·g(-1)), 2,2-diphenyl-1-picrylhydrazyl (DPPH) (47.46 g·pulp·g(-1) DPPH), and β-carotene/linoleic acid (92.17% Oxidation Inhibition (O.I) methods. Bacaba phenolic profile revealed the presence of cyanidin-3-O-rutinoside and other flavonoids. The palm fruits studied can be considered good sources of bioactive compounds, some containing higher amounts than that of commonly consumed fruits. Total extractable polyphenols and anthocyanins were directly correlated to antioxidant activity in these fruits.
Cipolla, L; Peri, F
In this article we review our work over the years on carbohydrates and carbohydrate mimetics and their applications in medicinal chemistry. In the first part of the review innovative synthetic methods, such as the chemoselective glycosylation method originally developed by our group and its applications to the synthesis of neoglycoconjugates (neoglycopeptides, oligosaccharide mimetics, neoglycolipids, etc…) will be presented. The high density of functional groups (hydroxyls) on the monosaccharides and the structural role of sugars forming the core of complex glycans in scaffolding and orienting the external sugar units for the interaction with receptors, inspired us and others to use sugars as scaffolds for the construction of pharmacologically active compounds. In the second part of this review, we will present some examples of bioactive and pharmacologically active compounds obtained by decorating monosaccharide scaffolds with pharmacophore groups. Sugar-derived protein ligands were also used as chemical probes to study the interaction of their target with other proteins in the cell. In this context, sugar mimetics and sugar-derived compounds have been employed as tools for exploring biology according to the "chemical genetic" approach.
Borrás-Linares, Isabel; Stojanović, Zorica; Quirantes-Piné, Rosa; Arráez-Román, David; Švarc-Gajić, Jaroslava; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio
In an extensive search for bioactive compounds from plant sources, the composition of different extracts of rosemary leaves collected from different geographical zones of Serbia was studied. The qualitative and quantitative characterization of 20 rosemary (Rosmarinus officinalis) samples, obtained by microwave-assisted extraction (MAE), was determined by high performance liquid chromatography coupled to electrospray quadrupole-time of flight mass spectrometry (HPLC–ESI-QTOF-MS). The high mass accuracy and true isotopic pattern in both MS and MS/MS spectra provided by the QTOF-MS analyzer enabled the characterization of a wide range of phenolic compounds in the extracts, including flavonoids, phenolic diterpenes and abietan-type triterpenoids, among others. According to the data compiled, rosemary samples from Sokobanja presented the highest levels in flavonoids and other compounds such as carnosol, rosmaridiphenol, rosmadial, rosmarinic acid, and carnosic acid. On the other hand, higher contents in triterpenes were found in the extracts of rosemary from Gložan (Vojvodina). PMID:25391044
Lee, N. Y.; Yunus, M. A. C.; Idham, Z.; Ruslan, M. S. H.; Aziz, A. H. A.; Irwansyah, N.
Agarwood commonly known as gaharu, aloeswood or eaglewood have been used as traditional medicine for centuries and its essential oil also being used as perfumery ingredients and aroma enhancers in food products. However, there is least study on the agarwood leaves though it contains large number of biomolecules component that show diverse pharmacological activity. Previous study showed that the extracted compounds from the leaves possess activities like anti-mutagenic, anti-tumor and anti-helminthic. The main objectives of this research were to determine bioactive compounds in agarwood leaves; leaves extract and oil yield obtained from maceration and soxhlet extraction methods respectively. The maceration process was performed at different operating temperature of 25°C, 50°C and 75°C and different retention time at 30, 60, 90 and 120 minutes. Meanwhile, various solvents were used to extract the oil from agarwood leaves using soxhlet method which are hexane, water, isopropanol and ethanol. The extracted oil from agarwood leaves by soxhlet extraction was analyzed using gas chromatography mass spectrometry. The results showed that the highest extract of 1.53% was obtained when increase the temperature to 75 °C and longest retention time of 120 minutes gave the highest oil yield of 2.10 % by using maceration. This is because at higher temperature enhances the solubility solute and diffusivity coefficient, thus increase the extract yield while longer retention time allow the reaction between solvent and solute occurred more rapidly giving higher extract. Furthermore, the soxhlet extraction using n-hexane as the solvent gave the highest oil yield as compared to other solvent due to the non-polar properties of n-hexane increase the efficiency of oil which is also non-polar to soluble in the solvent. In addition, the results also reported that the oil extracted from agarwood leaves contains bioactive compounds which are phytol, squalene, n-hexadecanoic acid and
Malaguti, Marco; Angeloni, Cristina; Hrelia, Silvana
Cardiovascular diseases (CVDs) are the leading cause of mortality in the Western world. Multiple factors are involved in CVD, including genetic factors and modifiable factors such as diet, physical activity, and smoking. CVD incidence and prevalence increase progressively with age, and it is estimated that over 80% of men and women older than 75 years have clinically manifest CVD. To reduce the gap between life expectancy (LE) and healthy life expectancy is one of the main challenges of the 21st century. Lifestyle improvement appears to be the only sustainable approach to face the dramatic chronic-degenerative disease burden of an aging population. A healthy lifestyle, represented by avoiding smoking, following a healthy diet, and practicing physical activity, protects from chronic-degenerative disease onset and progression. A healthy dietetic approach specifically formulated for elderly people, with a defined pattern of nutraceutical bioactive compounds, may represent a key strategy to improve the aging process and increase the life span. This short review summarizes the biochemical mechanisms underpinning the cardiovascular protective effects of some nutraceutical compounds such as quercetin and sulforaphane.
Sharifuddin, Yusrizam; Chin, Yao-Xian; Lim, Phaik-Eem; Phang, Siew-Moi
Diabetes mellitus is a group of metabolic disorders of the endocrine system characterised by hyperglycaemia. Type II diabetes mellitus (T2DM) constitutes the majority of diabetes cases around the world and are due to unhealthy diet, sedentary lifestyle, as well as rise of obesity in the population, which warrants the search for new preventive and treatment strategies. Improved comprehension of T2DM pathophysiology provided various new agents and approaches against T2DM including via nutritional and lifestyle interventions. Seaweeds are rich in dietary fibres, unsaturated fatty acids, and polyphenolic compounds. Many of these seaweed compositions have been reported to be beneficial to human health including in managing diabetes. In this review, we discussed the diversity of seaweed composition and bioactive compounds which are potentially useful in preventing or managing T2DM by targeting various pharmacologically relevant routes including inhibition of enzymes such as α-glucosidase, α-amylase, lipase, aldose reductase, protein tyrosine phosphatase 1B (PTP1B) and dipeptidyl-peptidase-4 (DPP-4). Other mechanisms of action identified, such as anti-inflammatory, induction of hepatic antioxidant enzymes’ activities, stimulation of glucose transport and incretin hormones release, as well as β-cell cytoprotection, were also discussed by taking into consideration numerous in vitro, in vivo, and human studies involving seaweed and seaweed-derived agents. PMID:26308010
Sharifuddin, Yusrizam; Chin, Yao-Xian; Lim, Phaik-Eem; Phang, Siew-Moi
Diabetes mellitus is a group of metabolic disorders of the endocrine system characterised by hyperglycaemia. Type II diabetes mellitus (T2DM) constitutes the majority of diabetes cases around the world and are due to unhealthy diet, sedentary lifestyle, as well as rise of obesity in the population, which warrants the search for new preventive and treatment strategies. Improved comprehension of T2DM pathophysiology provided various new agents and approaches against T2DM including via nutritional and lifestyle interventions. Seaweeds are rich in dietary fibres, unsaturated fatty acids, and polyphenolic compounds. Many of these seaweed compositions have been reported to be beneficial to human health including in managing diabetes. In this review, we discussed the diversity of seaweed composition and bioactive compounds which are potentially useful in preventing or managing T2DM by targeting various pharmacologically relevant routes including inhibition of enzymes such as α-glucosidase, α-amylase, lipase, aldose reductase, protein tyrosine phosphatase 1B (PTP1B) and dipeptidyl-peptidase-4 (DPP-4). Other mechanisms of action identified, such as anti-inflammatory, induction of hepatic antioxidant enzymes' activities, stimulation of glucose transport and incretin hormones release, as well as β-cell cytoprotection, were also discussed by taking into consideration numerous in vitro, in vivo, and human studies involving seaweed and seaweed-derived agents.
Frazão, Bárbara; Antunes, Agostinho
The study of bioactive compounds from marine animals has provided, over time, an endless source of interesting molecules. Jellyfish are commonly targets of study due to their toxic proteins. However, there is a gap in reviewing successful wet-lab methods employed in these animals, which compromises the fast progress in the detection of related biomolecules. Here, we provide a compilation of the most effective wet-lab methodologies for jellyfish venom extraction prior to proteomic analysis—separation, identification and toxicity assays. This includes SDS-PAGE, 2DE, gel chromatography, HPLC, DEAE, LC-MS, MALDI, Western blot, hemolytic assay, antimicrobial assay and protease activity assay. For a more comprehensive approach, jellyfish toxicity studies should further consider transcriptome sequencing. We reviewed such methodologies and other genomic techniques used prior to the deep sequencing of transcripts, including RNA extraction, construction of cDNA libraries and RACE. Overall, we provide an overview of the most promising methods and their successful implementation for optimizing time and effort when studying jellyfish. PMID:27077869
Frazão, Bárbara; Antunes, Agostinho
The study of bioactive compounds from marine animals has provided, over time, an endless source of interesting molecules. Jellyfish are commonly targets of study due to their toxic proteins. However, there is a gap in reviewing successful wet-lab methods employed in these animals, which compromises the fast progress in the detection of related biomolecules. Here, we provide a compilation of the most effective wet-lab methodologies for jellyfish venom extraction prior to proteomic analysis-separation, identification and toxicity assays. This includes SDS-PAGE, 2DE, gel chromatography, HPLC, DEAE, LC-MS, MALDI, Western blot, hemolytic assay, antimicrobial assay and protease activity assay. For a more comprehensive approach, jellyfish toxicity studies should further consider transcriptome sequencing. We reviewed such methodologies and other genomic techniques used prior to the deep sequencing of transcripts, including RNA extraction, construction of cDNA libraries and RACE. Overall, we provide an overview of the most promising methods and their successful implementation for optimizing time and effort when studying jellyfish.
Papaleo, Maria Cristiana; Romoli, Riccardo; Bartolucci, Gianluca; Maida, Isabel; Perrin, Elena; Fondi, Marco; Orlandini, Valerio; Mengoni, Alessio; Emiliani, Giovanni; Tutino, Maria Luisa; Parrilli, Ermenegilda; de Pascale, Donatella; Michaud, Luigi; Lo Giudice, Angelina; Fani, Renato
Antarctic bacteria represent a reservoir of unexplored biodiversity, which, in turn, might be correlated to the synthesis of still undescribed bioactive molecules, such as antibiotics. In this work we have further characterized a panel of four marine Antarctic bacteria able to inhibit the growth of human opportunistic multiresistant pathogenic bacteria belonging to the Burkholderia cepacia complex (responsible for the 'cepacia' syndrome in Cystic Fibrosis patients) through the production of a set of microbial Volatile Organic Compounds (mVOCs). A list of 30 different mVOCs synthesized under aerobic conditions by Antarctic bacteria was identified by GC-SPME analysis. Cross-streaking experiments suggested that Antarctic bacteria might also synthesize non-volatile molecules able to enhance the anti-Burkholderia activity. The biosynthesis of such a mixture of mVOCs was very probably influenced by both the presence/absence of oxygen and the composition of media used to grow the Antarctic strains. The antimicrobial activity exhibited by Antarctic strains also appeared to be more related to their taxonomical position rather than to the sampling site. Different Bcc bacteria were differently sensitive to the 'Antarctic' mVOCs and this was apparently related neither to the taxonomical position of the different strains nor to their source. The genome sequence of three new Antarctic strains was determined revealing that only P. atlantica TB41 possesses some genes belonging to the nrps-pks cluster. The comparative genomic analysis performed on the genome of the four strains also revealed the presence of a few genes belonging to the core genome and involved in the secondary metabolites biosynthesis. Data obtained suggest that the antimicrobial activity exhibited by Antarctic bacteria might rely on a (complex) mixture of mVOCs whose relative concentration may vary depending on the growth conditions. Besides, it is also possible that the biosynthesis of these compounds might occur
Kim, Se-Kwon; Dewapriya, Pradeep
Sponges are considered as the chemical factory in marine environment because of its immense production of chemically diverse compounds. Other than the chemical diversity, these compounds possess remarkable bioactivities. This great potential has aroused applications of sponge-derived compounds as therapeutics and at present, a number of promising compounds are in clinical and preclinical trials. Recently, nutraceuticals have received considerable interest among the health conscious community because of its multiple therapeutic effects. Natural health-promoting substances gain continuous popularity as nutraceuticals due to its reduced risk of side effects. This overview discusses the potentials of marine sponge-derived bioactivities as natural health-promoting compounds.
Martinez-Mayorga, Karina; Peppard, Terry L; López-Vallejo, Fabian; Yongye, Austin B; Medina-Franco, José L
Bioactive food compounds can be both therapeutically and nutritionally relevant. Screening strategies are widely employed to identify bioactive compounds from edible plants. Flavor additives contained in the so-called FEMA GRAS (generally recognized as safe) list of approved flavoring ingredients is an additional source of potentially bioactive compounds. This work used the principles of molecular similarity to identify compounds with potential mood-modulating properties. The ability of certain GRAS molecules to inhibit histone deacetylase-1 (HDAC1), proposed as an important player in mood modulation, was assayed. Two GRAS chemicals were identified as HDAC1 inhibitors in the micromolar range, results similar to what was observed for the structurally related mood prescription drug valproic acid. Additional studies on bioavailability, toxicity at higher concentrations, and off-target effects are warranted. The methodology described in this work could be employed to identify potentially bioactive flavor chemicals present in the FEMA GRAS list.
de Morais Cardoso, Leandro; Pinheiro, Soraia Silva; Martino, Hércia Stampini Duarte; Pinheiro-Sant'Ana, Helena Maria
Sorghum is the fifth most produced cereal in the world and is a source of nutrients and bioactive compounds for the human diet. We summarize the recent findings concerning the nutrients and bioactive compounds of sorghum and its potential impact on human health, analyzing the limitations and positive points of the studies and proposing directions for future research. Sorghum is basically composed of starch, which is more slowly digested than that of other cereals, has low digestibility proteins and unsaturated lipids, and is a source of some minerals and vitamins. Furthermore, most sorghum varieties are rich in phenolic compounds, especially 3-deoxyanthocyanidins and tannins. The results obtained in vitro and in animals have shown that phenolics compounds and fat soluble compounds (polycosanols) isolated from sorghum benefit the gut microbiota and parameters related to obesity, oxidative stress, inflammation, diabetes, dyslipidemia, cancer, and hypertension. The effects of whole sorghum and its fractions on human health need to be evaluated. In conclusion, sorghum is a source of nutrients and bioactive compounds, especially 3-deoxyanthocyanidins, tannins, and polycosanols, which beneficially modulate, in vitro and in animals, parameters related to noncommunicable diseases. Studies should be conducted to evaluate the effects of different processing on protein and starch digestibility of sorghum as well as on the profile and bioavailability of its bioactive compounds, especially 3-deoxyanthocyanidins and tannins. Furthermore, the benefits resulting from the interaction of bioactive compounds in sorghum and human microbiota should be studied.
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.
Albuquerque, Priscilla B S; Cerqueira, Miguel A; Vicente, António A; Teixeira, José A; Carneiro-da-Cunha, Maria G
Galactomannan extracted from Cassia grandis seeds was used for the production of films containing different concentrations of the bioactive compounds lactoferrin (LF), bioactive peptides (BAPs), and phytosterols. SEM, FTIR, mechanical and thermal properties, colour, moisture content (MC), solubility, water vapour permeability (WVP), and contact angle (CA) were performed evaluating the effect of increasing concentrations of bioactive compounds on the films' physicochemical properties. The immobilization of bioactive compounds leads to films with roughness on their surface, as observed by SEM. The thermal events demonstrated that bioactive compounds avoided the establishment of more hydrogen bonds when compared to galactomannan control film; this behaviour was also confirmed by FTIR. All the studied films had a strong whiteness tendency as well as a yellowish appearance. The addition of Lf reduced MC and solubility values and leads to an increase of WVP and CA values, while the addition of BAPs and phytosterols did not changed the filmś solubility. The mechanical properties were affected by the addition of bioactive compounds, which improved the stiffness of the films. Galactomannan-based films from C. grandis showed to be a promising structure for the immobilization of biomolecules, pointing at a significant number of possible applications in food and pharmaceutical industries.
Šic Žlabur, Jana; Voća, Sandra; Dobričević, Nadica; Pliestić, Stjepan; Galić, Ante; Boričević, Ana; Borić, Nataša
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.
Rocha-Martin, Javier; Harrington, Catriona; Dobson, Alan D.W.; O’Gara, Fergal
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
Vallverdú-Queralt, Anna; Oms-Oliu, Gemma; Odriozola-Serrano, Isabel; Lamuela-Raventos, Rosa María; Martín-Belloso, Olga; Elez-Martínez, Pedro
The effect of moderate intensity pulsed electric fields (MIPEF) on the bioactive compounds (total polyphenol, lycopene, and vitamin C content) as well as on the antioxidant capacity of tomato fruit was studied. The MIPEF treatment conditions were optimized to obtain tomato fruit with a high content of bioactive compounds. Tomato fruits were subjected to different electric field strengths (from 0.4 to 2.0 kV/cm) and number of pulses (from 5 to 30) and then immediately refrigerated at 4 °C for 24 h. A concentration of bioactive compounds higher than that of untreated tomatoes was obtained in MIPEF-treated tomatoes. A 44% increase in total polyphenol content was achieved under 30 pulses at 1.2 kV/cm. The hydrophilic antioxidant capacity was also enhanced by 44% applying 18 pulses at 1.2 kV/cm, and the lipophilic antioxidant capacity was increased by 37% under 5 pulses at 1.2 kV/cm. The maximum overall level of bioactive compounds and antioxidant capacity in the treated tomatoes was obtained under 16 pulses at 1 kV/cm. Therefore, MIPEF treatments could be considered an effective method to enhance the bioactive compound content and antioxidant potential of tomatoes.
Tan, Wen-Jie; Xu, Jia-Cheng; Li, Li; Chen, Ke-Li
Four flavone compounds were isolated from the effective fractions inhibiting xanthine oxidase (XOD) of the medicinal plant Selaginella labordei with anti-virus activity, and the structures were elucidated as 4'-methylether robustaflavone (1), robustaflavone (2), eriodictyol (3) and amentoflavone (4). The 50% inhibitory concentration (IC(50)) of the three compounds of inhibiting XOD were 61.0, 0.199, 16.0 and 32.0 mg L(-1), respectively. All of these compounds were isolated from the species for the first time, and eriodictyol was found from Selaginellaceae for the first time. Among these compounds, robustaflavone has been reported as an effective compound against the hepatitis B virus.
Redondo-Blanco, Saúl; Fernández, Javier; Gutiérrez-del-Río, Ignacio; Villar, Claudio J.; Lombó, Felipe
Combination therapy consists in the simultaneous administration of a conventional chemotherapy drug (or sometimes, a radiotherapy protocol) together with one or more natural bioactives (usually from plant or fungal origin) of small molecular weight. This combination of anticancer drugs may be applied to cell cultures of tumor cells, or to an animal model for a cancer type (or its xenograft), or to a clinical trial in patients. In this review, we summarize current knowledge describing diverse synergistic effects on colorectal cancer cell cultures, animal models, and clinical trials of various natural bioactives (stilbenes, flavonoids, terpenes, curcumin, and other structural families), which may be important with respect to diminish final doses of the chemotherapy drug, although maintaining its biological effect. This is important as these approaches may help reduce side effects in patients under conventional chemotherapy. Also, these molecules may exerts their synergistic effects via different cell cycle pathways, including different ones to those responsible of resistance phenotypes: transcription factors, membrane receptors, adhesion and structural molecules, cell cycle regulatory components, and apoptosis pathways. PMID:28352231
Galarraga-Vinueza, M E; Mesquita-Guimarães, J; Magini, R S; Souza, J C M; Fredel, M C; Boccaccini, A R
Bioactive glasses (BGs) are promising materials for bone repair due to their desirable properties such as osteoconductivity, biodegradability, angiogenic potential, and antibacterial activity. Ionic dissolution products from bioactive glasses increase the medium pH inhibiting surrounding bacteria proliferation. The activity of BGs against biofilm formation has been enhanced by incorporating organic antibacterial compounds. The aim of this review was to summarize evidence in literature which assesses the efficacy of antibacterial and anti-biofilm compounds embedded in bioactive glasses to prevent peri-implant infection during bone healing. A PubMed bibliographical research was carried out including articles published in the last 20 years. Most previous studies evaluated antibacterial efficiency in planktonic cultures but did not investigate biofilm inhibition, underestimating biofilm clinical relevance. Multifactorial features such as biocompatibility of embedded compounds, receptor site characteristics, and drug delivery efficiency have been found to influence the bioactive glass capability of acting both as an anti-biofilm agent and as a bone repairing biomaterial. Accordingly, further in vitro and in vivo studies are required to select the most promising anti-biofilm agents which should be incorporated into bioactive glasses to counteract biofilm proliferation, without inducing toxic effects on human cells, and with the added functionality of promoting bone regeneration. © 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part A: 105A: 672-679, 2017.
Tang, Baokun; Bi, Wentao; Tian, Minglei; Row, Kyung Ho
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.
Gao, Jiayu; Yin, Weiping; Gao, Ting; Deng, Ruixue; Li, Xin
Two compounds, 3β-acetoxyl,2,14,22-trihydroxy,19-hydroxymethyl,9α,5β,14β-card-20(22)enolide (1) and 1,2,3,4-tetrahydro-6-hydroxy1-5-pyrimidinecarbox-aldehyde (2), were isolated from arthropods in scorpion, Buthus martensii Karsch, by medium pressure liquid chromatography with silica gel as stationary phase and RP-HPLC analysis technology. The structures were elucidated on the basis of NMR spectroscopic analysis and HR-ESI-MS determination. It was found that (1) is a novel compound and both compounds showed inhibitory activities against the Gram-positive bacteria Bacillus subtilis (minimum inhibitory concentrations = 15 μg/mL), with diameter of inhibition zone at ϕ = 6.0 mm (compound 1) and ϕ = 9.0 mm (compound 2), respectively.
Gouda, Sushanto; Das, Gitishree; Sen, Sandeep K.; Shin, Han-Seung; Patra, Jayanta Kumar
Endophytes are an endosymbiotic group of microorganisms that colonize in plants and microbes that can be readily isolated from any microbial or plant growth medium. They act as reservoirs of novel bioactive secondary metabolites, such as alkaloids, phenolic acids, quinones, steroids, saponins, tannins, and terpenoids that serve as a potential candidate for antimicrobial, anti-insect, anticancer and many more properties. While plant sources are being extensively explored for new chemical entities for therapeutic purposes, endophytic microbes also constitute an important source for drug discovery. This review aims to comprehend the contribution and uses of endophytes as an impending source of drugs against various forms of diseases and other possible medicinal use. PMID:27746767
Rangel-Huerta, Oscar D.; Pastor-Villaescusa, Belen; Aguilera, Concepcion M.; Gil, Angel
The prevalence of cardiovascular diseases (CVD) is rising and is the prime cause of death in all developed countries. Bioactive compounds (BAC) can have a role in CVD prevention and treatment. The aim of this work was to examine the scientific evidence supporting phenolic BAC efficacy in CVD prevention and treatment by a systematic review. Databases utilized were Medline, LILACS and EMBASE, and all randomized controlled trials (RCTs) with prospective, parallel or crossover designs in humans in which the effects of BAC were compared with that of placebo/control were included. Vascular homeostasis, blood pressure, endothelial function, oxidative stress and inflammatory biomarkers were considered as primary outcomes. Cohort, ecological or case-control studies were not included. We selected 72 articles and verified their quality based on the Scottish Intercollegiate Guidelines Network, establishing diverse quality levels of scientific evidence according to two features: the design and bias risk of a study. Moreover, a grade of recommendation was included, depending on evidence strength of antecedents. Evidence shows that certain polyphenols, such as flavonols can be helpful in decreasing CVD risk factors. However, further rigorous evidence is necessary to support the BAC effect on CVD prevention and treatment. PMID:26132993
Rangel-Huerta, Oscar D; Pastor-Villaescusa, Belen; Aguilera, Concepcion M; Gil, Angel
The prevalence of cardiovascular diseases (CVD) is rising and is the prime cause of death in all developed countries. Bioactive compounds (BAC) can have a role in CVD prevention and treatment. The aim of this work was to examine the scientific evidence supporting phenolic BAC efficacy in CVD prevention and treatment by a systematic review. Databases utilized were Medline, LILACS and EMBASE, and all randomized controlled trials (RCTs) with prospective, parallel or crossover designs in humans in which the effects of BAC were compared with that of placebo/control were included. Vascular homeostasis, blood pressure, endothelial function, oxidative stress and inflammatory biomarkers were considered as primary outcomes. Cohort, ecological or case-control studies were not included. We selected 72 articles and verified their quality based on the Scottish Intercollegiate Guidelines Network, establishing diverse quality levels of scientific evidence according to two features: the design and bias risk of a study. Moreover, a grade of recommendation was included, depending on evidence strength of antecedents. Evidence shows that certain polyphenols, such as flavonols can be helpful in decreasing CVD risk factors. However, further rigorous evidence is necessary to support the BAC effect on CVD prevention and treatment.
Mahajan, Girish; Balachandran, Lakshmi
Microbes continue to play a highly considerable role in the drug discovery and development process. Nevertheless, the number of new chemical entities (NCEs) of microbial origin that has been approved by the Food and Drug Administration (FDA) has been reduced in the past decade. This scarcity can be partly attributed to the redundancy in the discovered molecules from microbial isolates, which are isolated from common terrestrial ecological units. However, this situation can be partly overcome by exploring rarely exploited ecological niches as the source of microbes, which reduces the chances of isolating compounds similar to existing ones. The use of modern and advanced isolation techniques, modification of the existing fermentation methods, genetic modifications to induce expression of silent genes, analytical tools for the detection and identification of new chemical entities, use of polymers in fermentation to enhance yield of fermented compounds, and so on, have all aided in enhancing the frequency of acquiring novel compounds. These compounds are representative of numerous classes of diverse compounds. Thus, compounds of microbial origin and their analogues undergoing clinical trials continue to demonstrate the importance of compounds from microbial sources in modern drug discovery.
Gull, Iram; Javed, Attia; Aslam, Muhammad Shahbaz; Mushtaq, Roohi; Athar, Muhammad Amin
The use of Moringa oleifera as natural food preservative has been evaluated in the present study. In addition, for quality assurance, the study has also been focused on the shelf life of product to authenticate the identification of plant by development of DNA based marker. Among the different extracts prepared from flower pods of Moringa oleifera, methanol and aqueous extract exhibited high antibacterial and antioxidant activity, respectively. The high phenolic contents (53.5 ± 0.169 mg GAE/g) and flavonoid contents (10.9 ± 0.094 mg QE/g) were also recorded in methanol and aqueous extract, respectively. Due to instability of bioactive compounds in aqueous extract, methanol extract is considered as potent natural preservative. The shelf life of methanol extract was observed for two months at 4°C under dark conditions. The developed SCAR primers (MOF217/317/MOR317) specifically amplified a fragment of 317 bp from DNA of Moringa oleifera samples collected from different regions of Punjab province of Pakistan. The methanol extract of Moringa oleifera flower pods has great potential to be used as natural preservative and nutraceutical in food industry. PMID:27471732
Gull, Iram; Javed, Attia; Aslam, Muhammad Shahbaz; Mushtaq, Roohi; Athar, Muhammad Amin
The use of Moringa oleifera as natural food preservative has been evaluated in the present study. In addition, for quality assurance, the study has also been focused on the shelf life of product to authenticate the identification of plant by development of DNA based marker. Among the different extracts prepared from flower pods of Moringa oleifera, methanol and aqueous extract exhibited high antibacterial and antioxidant activity, respectively. The high phenolic contents (53.5 ± 0.169 mg GAE/g) and flavonoid contents (10.9 ± 0.094 mg QE/g) were also recorded in methanol and aqueous extract, respectively. Due to instability of bioactive compounds in aqueous extract, methanol extract is considered as potent natural preservative. The shelf life of methanol extract was observed for two months at 4°C under dark conditions. The developed SCAR primers (MOF217/317/MOR317) specifically amplified a fragment of 317 bp from DNA of Moringa oleifera samples collected from different regions of Punjab province of Pakistan. The methanol extract of Moringa oleifera flower pods has great potential to be used as natural preservative and nutraceutical in food industry.
Rahmam., S.; Naim., M. N.; Ng., E.; Mokhtar, M. Nn; Abu Bakar, N. F.
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.
Teixeira, Ana; Baenas, Nieves; Dominguez-Perles, Raul; Barros, Ana; Rosa, Eduardo; Moreno, Diego A.; Garcia-Viguera, Cristina
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
Kong, Xianyu; Han, Xiurong; Gao, Min; Su, Rongguo; Wang, Ke; Li, Xuzhao; Lu, Wei
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.
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...
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...
Müller, Werner E G; Grebenjuk, Vladislav A; Le Pennec, Gaël; Schröder, Heinz- C; Brümmer, Franz; Hentschel, Ute; Müller, Isabel M; Breter, Hans- J
Sponges (phylum Porifera) are sessile marine filter feeders that have developed efficient defense mechanisms against foreign attackers such as viruses, bacteria, or eukaryotic organisms. Protected by a highly complex immune system, as well as by the capacity to produce efficient antiviral compounds (e.g., nucleoside analogues), antimicrobial compounds (e.g., polyketides), and cytostatic compounds (e.g., avarol), they have not become extinct during the last 600 million years. It can be assumed that during this long period of time, bacteria and microorganisms coevolved with sponges, and thus acquired a complex common metabolism. It is suggested that (at least) some of the bioactive secondary metabolites isolated from sponges are produced by functional enzyme clusters, which originated from the sponges and their associated microorganisms. As a consequence, both the host cells and the microorganisms lost the ability to grow independently from each other. Therefore, it was--until recently--impossible to culture sponge cells in vitro. Also the predominant number of "symbiotic bacteria" proved to be nonculturable. In order to exploit the bioactive potential of both the sponge and the "symbionts," a 3D-aggregate primmorph culture system was established; also it was proved that one bioactive compound, avarol/avarone, is produced by the sponge Dysidea avara. Another promising way to utilize the bioactive potential of the microorganisms is the cloning and heterologous expression of enzymes involved in secondary metabolism, such as the polyketide synthases.
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...
Chen, Zong-Tsi; Chu, Heuy-Ling; Chyau, Charng-Cherng; Chu, Chin-Chen; Duh, Pin-Der
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.
Nakashima, Takuji; Mayuzumi, Shinzo; Inaba, Shigeki; Park, Ju-Young; Anzai, Kozue; Suzuki, Rieko; Kuwahara, Natsumi; Utsumi, Noriko; Yokoyama, Fumie; Sato, Hajime; Okane, Izumi; Tsurumi, Yasuhisa; Ando, Katsuhiko
Penicillium strains (n=394) preserved at NBRC (the NITE Biological Resource Center) were compared as to groupings (11 species-clusters) based on phylogeny and the production of bioactive compounds. The strains in two clusters, of which P. chrysogenum and P. citrinum are representative, showed higher rates of positive strains with multi-biological activities.
do Carmo Brito, Brenda de Nazaré; Campos Chisté, Renan; da Silva Pena, Rosinelson; Abreu Gloria, Maria Beatriz; Santos Lopes, Alessandra
Cocoa is the target of increased scientific research as it is one of the richest source of bioactive compounds. The formation of bioactive amines and their changes in cocoa beans during seven days of traditional fermentation was investigated for the first time. In addition, total phenolic compounds, anthocyanins contents and the scavenging capacity against ABTS radical were determined to monitor the fermentation process. Only two biogenic amines (tryptamine and tyramine) and two polyamines (spermidine and spermine) were detected in cocoa beans during fermentation. Fermentation was characterized by three stages: i) high levels of tryptamine, phenolics, and scavenging capacity; ii) high contents of spermine, total biogenic amines and total polyamines; and iii) the highest spermidine levels and total acidity, but the lowest total phenolic compounds and anthocyanins contents. The scavenging capacity of cocoa beans during fermentation correlated with total phenolic compounds and anthocyanins contents.
Youssef, Diaa T. A.; Shaala, Lamiaa A.; Asfour, Hani Z.
In continuation of our search for drug leads from Red Sea sponges we have investigated the ethyl acetate fraction of the organic extract of the Red Sea sponge Hyrtios species. Bioassay-directed fractionation of the active fraction resulted into the identification of three new alkaloids, hyrtioerectines D–F (1–3). Hyrtioerectines D–F belong to the rare marine alkaloids in which the indole and β-carboline fragments of the molecule are linked through C-3/C-3 of both moieties. The structures of the isolated compounds were established based on different spectroscopic data including UV, IR, 1D and 2D NMR (COSY, HSQC, and HMBC) and high-resolution mass spectral studies. The antimicrobial activity against several pathogens and the free radical scavenging activity of the compounds using DPPH reagent were evaluated. In addition, the growth inhibitory activity of the compounds against three cancer cell lines was also evaluated. Hyrtioerectines D–F (1–3) displayed variable antimicrobial, free radical scavenging and cancer growth inhibition activities. Generally, compounds 1 and 3 were more active than compound 2. PMID:23538870
Kayastha, Shilva; Dimova, Dilyana; Iyer, Preeti; Vogt, Martin; Bajorath, Jürgen
Activity landscape representations integrate pairwise compound similarity and potency relationships and provide direct access to characteristic structure-activity relationship features in compound data sets. Because pairwise compound comparisons provide the foundation of activity landscape design, the assessment of specific landscape features such as activity cliffs has generally been confined to the level of compound pairs. A conditional probability-based approach has been applied herein to assign most probable activity landscape features to individual compounds. For example, for a given data set compound, it was determined if it would preferentially engage in the formation of activity cliffs or other landscape features. In a large-scale effort, we have determined conditional activity landscape feature probabilities for more than 160,000 compounds with well-defined activity annotations contained in 427 different target-based data sets. These landscape feature probabilities provide a detailed view of how different activity landscape features are distributed over currently available bioactive compounds.
Arunachalam, Kantha Deivi; Arun, Lilly Baptista; Annamalai, Sathesh Kumar; Arunachalam, Aarrthy M
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
Van De Velde, Franco; Tarola, Anna M.; Güemes, Daniel; Pirovani, María E.
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. PMID:28239102
Van De Velde, Franco; Tarola, Anna M; Güemes, Daniel; Pirovani, María E
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.
Lee, Jong Won; Lee, Jeong Hyun; Yu, In Ho; Gorinstein, Shela; Bae, Jong Hyang; Ku, Yang Gyu
The aim of this investigation was to find a proper harvesting period and establishing fern number, which effects the spear yield, bioactive compounds and antioxidant activities of Asparagus officinalis L. Spears were harvested at 2, 4, and 6 weeks after sprouting. Control for comparison was used without harvest. Spears and total yield increased with prolonged spear harvest period. In harvest of 6 weeks long optimum spear yield was the highest and fern numbers were 5 ~ 8. Bioactive compounds (polyphenols, flavonoids, flavanols, tannins and ascorbic acid) and the levels of antioxidant activities by ferric-reducing/antioxidant power (FRAP) and cupric reducing antioxidant capacity (CUPRAC) assays in asparagus ethanol extracts significantly differed in the investigated samples and were the highest at 6 weeks harvest period (P < 0.05). The first and the second segments from the tip significantly increased with the increase of catalase (CAT). It was interesting to investigate in vitro how human serum albumin (HSA) interacts with polyphenols extracted from investigated vegetables. Therefore the functional properties of asparagus were studied by the interaction of polyphenol ethanol extracts with HSA, using 3D- FL. In conclusion, antioxidant status (bioactive compounds, binding and antioxidant activities) improved with the harvesting period and the first segment from spear tip. Appropriate harvesting is effective for higher asparagus yield and its bioactivity.
Bray, Walter; Lokey, R Scott
When a disk of filter paper is impregnated with a cytotoxic or cytostatic drug and added to solid medium seeded with yeast, a visible clear zone forms around the disk whose size depends on the concentration and potency of the drug. This is the traditional "halo" assay and provides a convenient, if low-throughput, read-out of biological activity that has been the mainstay of antifungal and antibiotic testing for decades. Here, we describe a protocol for a high-throughput version of the halo assay, which uses an array of 384 pins to deliver ∼200 nL of stock solutions from compound plates onto single-well plates seeded with yeast. Using a plate reader in the absorbance mode, the resulting halos can be quantified and the data archived in the form of flat files that can be connected to compound databases with standard software. This assay has the convenience associated with the visual readout of the traditional halo assay but uses far less material and can be automated to screen thousands of compounds per day.
Bruno Bonnet, Christelle; Hubert, Olivier; Mbeguie-A-Mbeguie, Didier; Pallet, Dominique; Hiol, Abel; Reynes, Max; Poucheret, Patrick
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.
Bruno Bonnet, Christelle; Hubert, Olivier; Mbeguie-A-Mbeguie, Didier; Pallet, Dominique; Hiol, Abel; Reynes, Max; Poucheret, Patrick
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
Serrano, Jose C E; Jove, Mariona; Gonzalo, Hugo; Pamplona, Reinald; Portero-Otin, Manuel
Mechanism of action of bioactive compounds may be multiple, especially in the food matrix. Therefore, the interplay between these compounds and hosts' physiology, and the consequences of its continuous intake should be considered. In analogy with pharmacodynamics, the bioactive compounds should have both defined targets and mechanisms of action. However, several essential differences arise when considering the heterogeneous nature of the food matrix, the multiplicity of mechanisms and the variety of responses. In order to ascertain a potential mechanism of activity, one should consider both the intended use of the food, the biomarker that will support this claim and previous evidences, examined from current information sources. Once these have been examined, several experimental strategies should be considered, ranging from the choice of preclinical or experimental model, the use of samples from pilot interventional studies and the application of system's biology derived techniques, such as transcriptomics or metabolomics.
Cornejo, Fabiola; Caceres, Patricio J; Martínez-Villaluenga, Cristina; Rosell, Cristina M; Frias, Juana
The effect of germination conditions on the nutritional benefits of germinated brown rice flour (GBR) bread has been determined. The proximate composition, phytic acid, in vitro protein digestibility and in vitro enzymatic hydrolysis of starch, glucose and starch content, as well as the most relevant bioactive compounds (GABA, γ-oryzanol and total phenolic compounds) and antioxidant activity of breads prepared with GBR at different germination conditions was determined. When comparing different germination times (0 h, 12 h, 24 h and 48 h), germination for 48 h provides GBR bread with nutritionally superior quality on the basis of its higher content of protein, lipids and bioactive compounds (GABA and polyphenols), increased antioxidant activity and reduced phytic acid content and glycaemic index, although a slight decrease in in vitro protein digestibility was detected. Overall, germination seems to be a natural and sustainable way to improving the nutritional quality of gluten-free rice breads.
Turcu, Ioana; Zarafu, Irina; Popa, Marcela; Chifiriuc, Mariana Carmen; Bleotu, Coralia; Culita, Daniela; Ghica, Corneliu; Ionita, Petre
Water soluble gold nanoparticles protected by lipoic acid were obtained and further functionalized by standard coupling reaction with 1-naphtylamine, 4-aminoantipyrine, and 4′-aminobenzo-15-crown-5 ether. Derivatives of lipoic acid with 1-naphtylamine, 4-aminoantipyrine, and 4′-aminobenzo-15-crown-5 ether were also obtained and characterized. All these were tested for their antimicrobial activity, as well as for their influence on mammalian cell viability and cellular cycle. In all cases a decreased antimicrobial activity of the obtained bioactive nanoparticles was observed as compared with the organic compounds, proving that a possible inactivation of the bioactive groups could occur during functionalization. However, both the gold nanoparticles as well as the functionalized bioactive nanosystems proved to be biocompatible at concentrations lower than 50 µg/mL, as revealed by the cellular viability and cell cycle assay, demonstrating their potential for the development of novel antimicrobial agents. PMID:28336877
Tree tomato (Cyphomandra betacea) is appreciated for its excellent nutritional qualities, being considered a good source of antioxidants compounds, calcium, phosphorus, potassium and iron, sugars, organic acids, pectins and flavonoids. In this study, were evaluated physical parameters (weight, size, compression strength and humidity) and chemical (degrees Brix, titratable acidity, pH, protein, dietary fiber, ash, minerals and their bioaccesibility, pectin, antioxidants compounds) of the fruit from the Aragua State, Venezuela, as a contribution to stimulate and diversify the consumption of the tree tomato. The characterization showed that the fruits were at the ripening stage for consumption (degrees Brix 10.51, pH 3.5, acidity 0.02 g/100ml and 4.32 Kgf/cm2 compression strength) gave a yield of 74% pulp. The analytical results of the ripped pulp showed a content of 30 Kcal/100 g, dietary fiber (4.10 g/100 g), and minerals such as phosphorous, calcium, magnesium, potassium and iron (331.32, 21.25, 21.18, 17.03 and 7.44 mg/100 g, respectively). Bioaccesibility values of 6.71 and 1.86% were reported for calcium and iron. The extracted pectin (1.00 g/100 g) was classified as high methoxyl with high degree of esterification. The antioxidant capacity of the ripped pulp (EC50 of 165.00 g/g DPPH and reducing power of 0.07 mmol Fe +2/100 g), could be attributed to the presence of ascorbic acid (23.32 mg/100 g), lycopene (1.22 mg/100 g), and phenolic compounds (1.39 mg GAE/g), anthocyanins (0.29 mg cyanidin/g) and tannins (0.40 mg catechin/100 g).The results obtained encourage the nutritional benefits and suggest applications as a functional ingredient in food product development.
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
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.
Greque de Morais, Michele; Greque de Morais, Etiele; Vaz, Bruna da Silva; Gonçalves, Carolina Ferrer; Lisboa, Cristiane; Costa, Jorge Alberto Vieira
Microalgae have been studied in biotechnological processes due to the various biocompounds that can be obtained from their biomasses, including pigments, proteins, antioxidants, biopeptides, fatty acids and biopolymers. Microalgae biopolymers are biodegradable materials that present similar characteristics to traditional polymers, with the advantage of being rapidly degraded when discarded. In addition, nanoencapsulation is capable of increasing the availability of bioactive compounds by allowing the release of these biocompounds to occur slowly over time. The use of polymers in the nanoencapsulation of active ingredients can mask the undesired physicochemical properties of the compounds to be encapsulated, thereby enhancing consumer acceptability. This covering also acts as a barrier against several foreign substances that can react with bioactive compounds and reduce their activity. Studies of the development of poly-3-hydroxybutyrate (PHB) nanocapsules from microbial sources are little explored; this review addresses the use of nanotechnology to obtain bioactive compounds coated with biopolymer nanocapsules, both obtained from Spirulina biomasses. These microalgae are Generally Recognized as Safe (GRAS) certified, which guarantees that the biomass can be used to obtain high added value biocompounds, which can be used in human and animal supplementation.
Scolaro, Bianca; Soo Jin Kim, Hellen; Castro, Inar Alves de
Different pharmacological interventions have been applied with success to reduce the progression of atherosclerosis. However, many patients are not good responders or must interrupt treatment due to adverse effects. Bioactive compounds such as omega-3 fatty acids (n-3 FA), plant sterol esters (PSE) and phenolic compounds (PHC) are natural molecules with great potential to reduce the atherosclerosis burden by reducing inflammation, LDL cholesterol (LDL-C) and oxidative stress, respectively. Although their physiological effects on biomarkers are much lower than those expected by drugs used for the same purpose, bioactive compounds can easily be incorporated into the daily diet and present no adverse effects. However, little is known about the combination of n-3 FA, PSE, PHC and drugs in atherosclerosis progression. This review article summarizes potential effects of co-therapies involving n-3 FA, PSE and PHC combined with major hypolipidemic drugs on atherosclerosis biomarkers and clinical outcomes. Evidence of additive and/or complementary effects regarding drugs action reveals possible roles for bioactive compounds in disease management. Pharmaceutical companies, physicians and food scientists should be prepared to better understand this type of interaction and its consequences in terms of efficacy and life quality.
Arcan, Iskender; Yemenicioğlu, Ahmet
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.
Barbosa, Mariana; Valentão, Patrícia; Andrade, Paula B.
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
Talero, Elena; García-Mauriño, Sofía; Ávila-Román, Javier; Rodríguez-Luna, Azahara; Alcaide, Antonio; Motilva, Virginia
The risk of onset of cancer is influenced by poorly controlled chronic inflammatory processes. Inflammatory diseases related to cancer development include inflammatory bowel disease, which can lead to colon cancer, or actinic keratosis, associated with chronic exposure to ultraviolet light, which can progress to squamous cell carcinoma. Chronic inflammatory states expose these patients to a number of signals with tumorigenic effects, including nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) activation, pro-inflammatory cytokines and prostaglandins release and ROS production. In addition, the participation of inflammasomes, autophagy and sirtuins has been demonstrated in pathological processes such as inflammation and cancer. Chemoprevention consists in the use of drugs, vitamins, or nutritional supplements to reduce the risk of developing or having a recurrence of cancer. Numerous in vitro and animal studies have established the potential colon and skin cancer chemopreventive properties of substances from marine environment, including microalgae species and their products (carotenoids, fatty acids, glycolipids, polysaccharides and proteins). This review summarizes the main mechanisms of actions of these compounds in the chemoprevention of these cancers. These actions include suppression of cell proliferation, induction of apoptosis, stimulation of antimetastatic and antiangiogenic responses and increased antioxidant and anti-inflammatory activity. PMID:26437418
Guimaraes, Cesar L S; Moreira-Dill, Leandro S; Fernandes, Renata S; Costa, Tassia R; Hage-Melim, Lorane I S; Marcussi, Silvana; Carvalho, Bruna M A; da Silva, Saulo L; Zuliani, Juliana P; Fernandes, Carla F C; Calderon, Leonardo A; Soares, Andreimar M; Stabeli, Rodrigo G
Snakebites are a frequently neglected public health issue in tropical and subtropical countries. According to the World Health Organization, 5 million people are bitten annually including up to 2.5 million envenomations. Treatment with antivenom serum remains the only specific therapy for snakebite envenomation. However, it is heterologous and therefore liable to cause adverse reactions, such as early anaphylactic, pyrogenic and delayed reactions. In order to develop alternatives to the current therapy, researchers have been looking for natural products and plant extracts with antimyotoxic, anti-hemorrhagic and anti-inflammatory properties. Especially due to the role the physiopathological processes triggered by snake toxins, play in paralysis, bleeding disorders, kidney failure and tissue damage. Considering the fact that studies involving snake toxins and specific inhibitors, particularly on a molecular level, are the main key to understand neutralization mechanisms and to propose models or prototypes for an alternative therapy, this article presents efforts made by the scientific community in order to produce validated data regarding 87 compounds and plant extracts obtained from 79 species. These plants, which belong to 63 genera and 40 families, have been used by traditional medicine as alternatives or complements to the current serum therapy.
Lo Cantore, Pietro; Giorgio, Annalisa; Iacobellis, Nicola S.
Pseudomonas tolaasii is the main bacterial pathogen of several mushroom species. In this paper we report that strains of P. tolaasii produce volatile substances inducing in vitro mycelia growth inhibition of Pleurotus ostreatus and P. eryngii, and Agaricus bisporus and P. ostreatus basidiome tissue blocks brown discoloration. P. tolaasii strains produced the volatile ammonia but not hydrogen cyanide. Among the volatiles detected by GC–MS, methanethiol, dimethyl disulfide (DMDS), and 1-undecene were identified. The latter, when assayed individually as pure compounds, led to similar effects noticed when P. tolaasii volatiles natural blend was used on mushrooms mycelia and basidiome tissue blocks. Furthermore, the natural volatile mixture resulted toxic toward lettuce and broccoli seedling growth. In contrast, pure volatiles showed different activity according to their nature and/or doses applied. Indeed, methanethiol resulted toxic at all the doses used, while DMDS toxicity was assessed till a quantity of 1.25 μg, below which it caused, together with 1-undecene (≥10 μg), broccoli growth increase. PMID:26500627
Cruz, Rebeca; Gomes, Teresa; Ferreira, Anabela; Mendes, Eulália; Baptista, Paula; Cunha, Sara; Pereira, José Alberto; Ramalhosa, Elsa; Casal, Susana
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.
Figueira, Felipe da Silva; Gettens, Juliana Garcia; Costa, Jorge Alberto Vieira; de Morais, Michele Greque; Moraes, Caroline Costa; Kalil, Susana Juliano
C-phycocyanin (C-PC) is a water-soluble phycobiliprotein present in light-harvesting antenna system of cyanobacteria. The nanostructures have not been widely evaluated, precluding improvements in stability and application of the C-PC. Electrospun nanofibers have an extremely high specific surface area due to their small diameter, they can be produced from a wide variety of polymers, and they are successfully evaluated to increase the efficacy of antitumor drugs. The incorporation of C-PC into nanofibers would allow investigations of potential uses in alternative cancer treatments and tissue engineering scaffolds. In this paper, C-phycocyanin were incorporated into the polymer polyethylene oxide (PEO) in various concentrations for nanofiber production via an electrospinning process. Nanofibers structures were analyzed using digital optical microscopy and scanning electron microscopy (SEM). Thermogravimetric analysis was performed on the pure starting compounds and the produced nanofibers. At a concentration of 2% (w/w) of PEO, nanofibers were not produced, and concentrations of 4% (w/w) of PEO failed to produce nanofibers of good quality. Solutions with 6% (w/w) PEO, 6% (w/w) PEO plus 1% (w/w) NaCI, and 8% (w/w) PEO promote the formation of bluish, homogeneous and bead-free nanofibers with average diameters varying between 542.1 and 759.9 nm, as evaluated by optical microscopy. SEM analysis showed that nanofibers produced from polymer solutions containing 6% (w/w) PEO, 1% (w/w) NaCl and 3% (w/w) C-PC have an average diameter of 295 nm. Thermogravimetric analysis detected an increase in thermal resistance with the incorporation of C-phycocyanin into nanofibers.
Leone, Alessandro; Spada, Alberto; Battezzati, Alberto; Schiraldi, Alberto; Aristil, Junior; Bertoli, Simona
Moringa oleifera is an interesting plant for its use in bioactive compounds. In this manuscript, we review studies concerning the cultivation and production of moringa along with genetic diversity among different accessions and populations. Different methods of propagation, establishment and cultivation are discussed. Moringa oleifera shows diversity in many characters and extensive morphological variability, which may provide a resource for its improvement. Great genetic variability is present in the natural and cultivated accessions, but no collection of cultivated and wild accessions currently exists. A germplasm bank encompassing the genetic variability present in Moringa is needed to perform breeding programmes and develop elite varieties adapted to local conditions. Alimentary and medicinal uses of moringa are reviewed, alongside the production of biodiesel. Finally, being that the leaves are the most used part of the plant, their contents in terms of bioactive compounds and their pharmacological properties are discussed. Many studies conducted on cell lines and animals seem concordant in their support for these properties. However, there are still too few studies on humans to recommend Moringa leaves as medication in the prevention or treatment of diseases. Therefore, further studies on humans are recommended. PMID:26057747
Leone, Alessandro; Spada, Alberto; Battezzati, Alberto; Schiraldi, Alberto; Aristil, Junior; Bertoli, Simona
Moringa oleifera is an interesting plant for its use in bioactive compounds. In this manuscript, we review studies concerning the cultivation and production of moringa along with genetic diversity among different accessions and populations. Different methods of propagation, establishment and cultivation are discussed. Moringa oleifera shows diversity in many characters and extensive morphological variability, which may provide a resource for its improvement. Great genetic variability is present in the natural and cultivated accessions, but no collection of cultivated and wild accessions currently exists. A germplasm bank encompassing the genetic variability present in Moringa is needed to perform breeding programmes and develop elite varieties adapted to local conditions. Alimentary and medicinal uses of moringa are reviewed, alongside the production of biodiesel. Finally, being that the leaves are the most used part of the plant, their contents in terms of bioactive compounds and their pharmacological properties are discussed. Many studies conducted on cell lines and animals seem concordant in their support for these properties. However, there are still too few studies on humans to recommend Moringa leaves as medication in the prevention or treatment of diseases. Therefore, further studies on humans are recommended.
Chávez-Mendoza, Celia; Sanchez, Esteban; Muñoz-Marquez, Ezequiel; Sida-Arreola, Juan Pedro; Flores-Cordova, Maria Antonia
Grafting favors the presence of bioactive compounds in the bell pepper, but many species and varieties have not yet been analyzed in this sense, including commonly grafted varieties. The aim of the present study is to characterize the content in β-carotenes, vitamin C, lycopene, total phenols, and the antioxidant activity of bell pepper (Capsicum annum L) using the cultivar/rootstock combinations: Jeanette/Terrano (yellow), Sweet/Robusto (green), Fascinato/Robusto (red), Orangela/Terrano (orange), and Fascinato/Terrano (red). The plants were grown in a net-shading system and harvested on three sampling dates of the same crop cycle. The results show statistical differences (p ≤ 0.05) between cultivar/rootstock combinations and sampling dates for the content in bioactive compounds and antioxidant activity. Fascinato/Robusto presented the highest concentration of lycopene and total phenols as well as the greatest antioxidant activity of all cultivar/rootstock combinations evaluated. In addition, it was found that the best sampling time for the peppers to have the highest concentrations of bioactive compounds and antioxidant activity was September. PMID:26783714
Park, Yong-Seo; Namiesnik, Jacek; Vearasilp, Kann; Leontowicz, Hanna; Leontowicz, Maria; Barasch, Dinorah; Nemirovski, Alina; Trakhtenberg, Simon; Gorinstein, Shela
The aim of this investigation was to find the best among seven different kiwi fruit cultivars ('Hayward', 'Daheung', 'Haenam', 'Bidan', 'Hort16A', 'Hwamei' and 'SKK12') for human consumption and to classify them as groups. Therefore, the contents of bioactive compounds and the level of antioxidant capacities of these cultivars were determined in four different extracts and compared. It was found that the contents of the bioactive compounds and the level of antioxidant capacities in different extracts differ significantly (P<0.05). Bioactive compounds and the antioxidant capacities were significantly higher in 'Bidan' and 'SKK12' cultivars than in other studied samples. The ethanol and water extracts of these cultivars exhibited high binding properties with human serum albumin (HSA) in comparison with catechin. In conclusion, based on fluorescence profiles the seven new kiwi fruit cultivars can be classified for three groups: 'Hayward' (including 'Daheung', 'Haenam', Hwamei' and 'SKK12'), 'Bidan' and 'Hort 16A'. In MS - profiles some differences in the peaks were found between the cultivar groups. All studied fruits could be a valuable addition to known disease preventing diets.
Koriyama, Takuya; Asoh, Taka-Aki; Kikuchi, Akihiko
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.
Chávez-Mendoza, Celia; Sanchez, Esteban; Muñoz-Marquez, Ezequiel; Sida-Arreola, Juan Pedro; Flores-Cordova, Maria Antonia
Grafting favors the presence of bioactive compounds in the bell pepper, but many species and varieties have not yet been analyzed in this sense, including commonly grafted varieties. The aim of the present study is to characterize the content in β-carotenes, vitamin C, lycopene, total phenols, and the antioxidant activity of bell pepper (Capsicum annum L.) using the cultivar/rootstock combinations: Jeanette/Terrano (yellow), Sweet/Robusto (green), Fascinato/Robusto (red), Orangela/Terrano (orange), and Fascinato/Terrano (red). The plants were grown in a net-shading system and harvested on three sampling dates of the same crop cycle. The results show statistical differences (p ≤ 0.05) between cultivar/rootstock combinations and sampling dates for the content in bioactive compounds and antioxidant activity. Fascinato/Robusto presented the highest concentration of lycopene and total phenols as well as the greatest antioxidant activity of all cultivar/rootstock combinations evaluated. In addition, it was found that the best sampling time for the peppers to have the highest concentrations of bioactive compounds and antioxidant activity was September.
Rodríguez-Neira, Lidia; Lage-Yusty, María Asunción; López-Hernández, Julia
Saffron, the dried stigmas of Crocus sativus L., is used as a condiment spice. The major bioactive compounds are crocins, picrocrocin and safranal, which are responsible for the sensory profile of saffron (color, flavor and aroma, respectively), and also health-promoting properties. In this paper, the effect on the bioactive compounds of different cooking times in boiling water at 100 °C in samples of Saffron from La Mancha (safranal, picrocrocin, trans-crocin 4, cis-crocin 4 and trans-crocin 3) was investigated. Performance characteristics of High Performance Liquid Chromatography with Variable Wavelength Detector method, parameters of linearity, limits of detection and quantification are reported. High Performance Liquid Chromatography-Photo Diode Array-Mass Spectrometry was used as a confirmatory technique in crocins identification. When the samples are subjected to different cooking times, they present different behaviors, depending on the bioactive compound. In this way, no changes were observed in the concentration of picrocrocin, while heat culinary treatment adversely affects the concentrations of crocins and safranal.
Ruiz, Guillermo G.; Nelson, Erik O.; Kozin, Adam F.; Turner, Tiffany C.; Waters, Robert F.; Langland, Jeffrey O.
The use of botanical medicine by practitioners and the general public has dramatically increased in recent years. Most of these botanical therapeutics are obtained through commercial manufacturers or nutraceutical companies. The current standard of practice that manufacturers typically use to standardize botanicals is done based on the level of a well-known, abundant marker compound present in the botanical. This study evaluated the putative correlation between the level of a marker compound and the biological activity of eight common botanicals. Overall, the standardization of a botanical based on a marker compound was found not to be a reliable method when compared to in vitro bioactivity. A marker compound is often not the biologically active component of a plant and therefore the level of such a marker compound does not necessarily correlate with biological activity or therapeutic efficacy. PMID:27458926
Nair, Dileep G; Weiskirchen, Ralf; Al-Musharafi, Salma K
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
Jin, Liming; Quan, Chunshan; Hou, Xiyan; Fan, Shengdi
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
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...
Stumpfe, Dagmar; Dimova, Dilyana; Bajorath, Jürgen
The assessment of activity cliffs has thus far mostly focused on compound pairs, although the majority of activity cliffs are not formed in isolation but in a coordinated manner involving multiple active compounds and cliffs. However, the composition of coordinated activity cliff configurations and their topologies are unknown. Therefore, we have identified all activity cliff configurations formed by currently available bioactive compounds and analyzed them in network representations where activity cliff configurations occur as clusters. The composition, topology, frequency of occurrence, and target distribution of activity cliff clusters have been determined. A limited number of large cliff clusters with unique topologies were identified that were centers of activity cliff formation. These clusters originated from a small number of target sets. However, most clusters were of small to moderate size. Three basic topologies were sufficient to describe recurrent activity cliff cluster motifs/topologies. For example, frequently occurring clusters with star topology determined the scale-free character of the global activity cliff network and represented a characteristic activity cliff configuration. Large clusters with complex topology were often found to contain different combinations of basic topologies. Our study provides a first view of activity cliff configurations formed by currently available bioactive compounds and of the recurrent topologies of activity cliff clusters. Activity cliff clusters of defined topology can be selected, and from compounds forming the clusters, SAR information can be obtained. The SAR information of activity cliff clusters sharing a/one specific activity and topology can be compared.
Liu, Changhong; Liu, Wei; Chen, Wei; Yang, Jianbo; Zheng, Lei
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.
Geethangili, Madamanchi; Tzeng, Yew-Min
Antrodia camphorata is a unique mushroom of Taiwan, which has been used as a traditional medicine for protection of diverse health-related conditions. In an effort to translate this Eastern medicine into Western-accepted therapy, a great deal of work has been carried out on A. camphorata. This review discusses the biological activities of the crude extracts and the main bioactive compounds of A. camphorata. The list of bioactivities of crude extracts is huge, ranging from anti-cancer to vasorelaxation and others. Over 78 compounds consisting of terpenoids, benzenoids, lignans, benzoquinone derivatives, succinic and maleic derivatives, in addition to polysaccharides have been identified. Many of these compounds were evaluated for biological activity. Many activities of crude extracts and pure compounds of A. camphorata against some major diseases of our time, and thus, a current review is of great importance. It is concluded that A. camphorata can be considered as an efficient alternative phytotherapeutic agent or a synergizer in the treatment of cancer and other immune-related diseases. However, clinical trails of human on A. camphorata extracts are limited and those of pure compounds are absent. The next step is to produce some medicines from A. camphorata, however, the production may be hampered by problems related to mass production. PMID:19687189
Thi, Nhuan Do; Hwang, Eun-Sun
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
Geethangili, Madamanchi; Tzeng, Yew-Min
Antrodia camphorata is a unique mushroom of Taiwan, which has been used as a traditional medicine for protection of diverse health-related conditions. In an effort to translate this Eastern medicine into Western-accepted therapy, a great deal of work has been carried out on A. camphorata. This review discusses the biological activities of the crude extracts and the main bioactive compounds of A. camphorata. The list of bioactivities of crude extracts is huge, ranging from anti-cancer to vasorelaxation and others. Over 78 compounds consisting of terpenoids, benzenoids, lignans, benzoquinone derivatives, succinic and maleic derivatives, in addition to polysaccharides have been identified. Many of these compounds were evaluated for biological activity. Many activities of crude extracts and pure compounds of A. camphorata against some major diseases of our time, and thus, a current review is of great importance. It is concluded that A. camphorata can be considered as an efficient alternative phytotherapeutic agent or a synergizer in the treatment of cancer and other immune-related diseases. However, clinical trails of human on A. camphorata extracts are limited and those of pure compounds are absent. The next step is to produce some medicines from A. camphorata, however, the production may be hampered by problems related to mass production.
Thi, Nhuan Do; Hwang, Eun-Sun
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.
Moradi, Samira; Koushesh Saba, Mahmoud; Mozafari, Ali Akbar; Abdollahi, Hamid
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.
Khemawoot, Phisit; Hunsakunachai, Natthaphon; Anukunwithaya, Tosapol; Bangphumi, Kunan; Ongpipattanakul, Boonsri; Jiratchariyakul, Weena; Soawakontha, Ruedee; Inthachart, Thanakorn; Dechatiwongse Na Ayudhya, Thaweephol; Koontongkaew, Sittichai; Poachanukoon, Orapan
Rhizomes of Zingiber cassumunar have been used for many years in traditional Thai medicine as an anti-inflammatory agent. The major bioactive component of this plant is Compound D [E-4-(3', 4'-dimethoxyphenyl)but-3-en-1-ol], which is a strong smooth muscle relaxant, and has antihistamine and anti-inflammatory actions. There is, however, incomplete information available for the pharmacokinetics of Compound D in mammals. In this study, we examined the pharmacokinetic profiles of Compound D in male Wistar rats. A standardized extract of Z. cassumunar containing 4 % w/w Compound D was administered intravenously at 25 mg/kg or by oral gavage at 25, 75, or 250 mg/kg to Wistar rats. Blood, tissues, urine, and feces were collected from 0 to 48 h after dosing and the level of Compound D was determined by liquid chromatography-tandem mass spectrometry. The concentration of Compound D ranged from 10-100 µg/L, reached a maximum approximately 0.15 h after oral dosing. Compound D exhibited an excellent tissue to plasma ratio, ranging from 1- to 1000 in several organs at 1-4 h after oral dosing. Less than 1 % of unchanged Compound D was excreted in the urine and feces. Further studies on tissue uptake and metabolite identification are required to obtain complete pharmacokinetic information and to develop appropriate dosing strategies of Compound D and the standardized extract of Z. cassumunar.
Gothai, Sivapragasam; Ganesan, Palanivel; Park, Shin-Young; Fakurazi, Sharida; Choi, Dong-Kug; Arulselvan, Palanisamy
Diabetes is a metabolic, endocrine disorder which is characterized by hyperglycemia and glucose intolerance due to insulin resistance. Extensive research has confirmed that inflammation is closely involved in the pathogenesis of diabetes and its complications. Patients with diabetes display typical features of an inflammatory process characterized by the presence of cytokines, immune cell infiltration, impaired function and tissue destruction. Numerous anti-diabetic drugs are often prescribed to diabetic patients, to reduce the risk of diabetes through modulation of inflammation. However, those anti-diabetic drugs are often not successful as a result of side effects; therefore, researchers are searching for efficient natural therapeutic targets with less or no side effects. Natural products’ derived bioactive molecules have been proven to improve insulin resistance and associated complications through suppression of inflammatory signaling pathways. In this review article, we described the extraction, isolation and identification of bioactive compounds and its molecular mechanisms in the prevention of diabetes associated complications. PMID:27527213
Gothai, Sivapragasam; Ganesan, Palanivel; Park, Shin-Young; Fakurazi, Sharida; Choi, Dong-Kug; Arulselvan, Palanisamy
Diabetes is a metabolic, endocrine disorder which is characterized by hyperglycemia and glucose intolerance due to insulin resistance. Extensive research has confirmed that inflammation is closely involved in the pathogenesis of diabetes and its complications. Patients with diabetes display typical features of an inflammatory process characterized by the presence of cytokines, immune cell infiltration, impaired function and tissue destruction. Numerous anti-diabetic drugs are often prescribed to diabetic patients, to reduce the risk of diabetes through modulation of inflammation. However, those anti-diabetic drugs are often not successful as a result of side effects; therefore, researchers are searching for efficient natural therapeutic targets with less or no side effects. Natural products' derived bioactive molecules have been proven to improve insulin resistance and associated complications through suppression of inflammatory signaling pathways. In this review article, we described the extraction, isolation and identification of bioactive compounds and its molecular mechanisms in the prevention of diabetes associated complications.
Daletos, Georgios; Ebrahim, Weaam; Ancheeva, Elena; El-Neketi, Mona; Proksch, Peter
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 will summarize the new and/or bioactive compounds reported from deep-sea-derived fungi in the last six years (2010 - present) and will critically evaluate whether the data published so far really support the notion that these fungi are a promising source of new bioactive chemical entities.
Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Clemente, Edmar
Endophytic microorganisms, defined as fungi or bacteria that colonize the interior of plants without causing any immediate negative effects or damages, have reciprocal relationships with host plants. In some cases their presence is beneficial to the host due to the synthesis of bioactive compounds, among which several alcohols, esters, ketones and others that may react with other compounds and may be lethal to pathogenic microorganisms. Diaporthe helianthi (Phomopsis helianthi in its anamorphic phase) is available worldwide, especially in Europe, Asia and America. Isolated in Europe as an agent of the sunflower stem cancer, it has also been endophytically isolated from tropical and temperate plants. A D. helianthi strain isolated from Luehea divaricata has been employed in current research. An investigation of the secondary metabolite from D. helianthi by CC and NMR of 1H and 13C yielded the separation of 10 fractions and the identification of the phenolic compound 2(-4 hydroxyphenyl)-ethanol (Tyrosol). Its antimicrobial reaction was tested and the ensuing antagonistic effects on the human pathogenic bacteria Enterococcus hirae, Escherichia coli, Micrococcus luteus, Salmonella typhi, Staphylococcus aureus, phytopathogenic Xanthomonas asc. phaseoli and phytopathogenic fungi were demonstrated. Results show that bioactive compounds and Tyrosol produced by D. helianthi have a biotechnological potential. PMID:24031942
Ventura, Sónia P M; E Silva, Francisca A; Quental, Maria V; Mondal, Dibyendu; Freire, Mara G; Coutinho, João A P
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.
Zeeshan, M.; Rizvi, S.M.D.; Khan, M.S.; Kumar, A.
The present study deals with the isolation and partial purification of bioactive compounds from the crude methanol extracts of the leaves of Ageratum houstonianum (Asteraceae). The quantification and the identification of compounds in the crude extract and active bands isolated by preparative TLC were accomplished using GC-MS analysis. The most important compounds identified in the crude extract and active bands (AB-1 and AB-2) were 6-acetyl-7-methoxy-2, 2-dimethylchromene, hexadecanoic acid and squalene, respectively. Crude extract and active bands (AB-1 and AB-2) were investigated for their antibacterial activity against Staphylococcus epidermidis, Staphylococcus aureus, Bacillus subtilis, Bacillus cereus, Escherichia coli, Enterobacter aerogenes, Klebsiella pneumoniae, and Pseudomonas aeruginosa. The crude extract, AB-1 and AB-2 showed maximum zone of inhibition (10-13 mm) against Staphylococcus epidermidis, however, the antibacterial potential of active bands was slightly higher as compared to the crude extract. Dose-dependant increase in antioxidant potential was noticed in crude extract as well as with both active bands measured by DPPH free radicals, ion chelation and total antioxidants capacity. Our study reports various bioactive compounds in the leaves of the A. houstonianum with significant antioxidant and antibacterial potential. PMID:27350770
Vahid, F; Zand, H; Nosrat-Mirshekarlou, E; Najafi, R; Hekmatdoost, A
Nutrigenomics is an area of epigenomics that explores and defines the rapidly evolving field of diet-genome interactions. Lifestyle and diet can significantly influence epigenetic mechanisms, which cause heritable changes in gene expression without changes in DNA sequence. Nutrient-dependent epigenetic variations can significantly affect genome stability, mRNA and protein expression, and metabolic changes, which in turn influence food absorption and the activity of its constituents. Dietary bioactive compounds can affect epigenetic alterations, which are accumulated over time and are shown to be involved in the pathogenesis of age-related diseases such as diabetes, cancer, and cardiovascular disease. Histone acetylation is an epigenetic modification mediated by histone acetyl transferases (HATs) and histone deacetylases (HDACs) critically involved in regulating affinity binding between the histones and DNA backbone. The HDAC-mediated increase in histone affinity to DNA causes DNA condensation, preventing transcription, whereas HAT-acetylated chromatin is transcriptionally active. HDAC and HAT activities are reported to be associated with signal transduction, cell growth and death, as well as with the pathogenesis of various diseases. The aim of this review was to evaluate the role of diet and dietary bioactive compounds on the regulation of HATs and HDACs in epigenetic diseases. Dietary bioactive compounds such as genistein, phenylisothiocyanate, curcumin, resveratrol, indole-3-carbinol, and epigallocatechin-3-gallate can regulate HDAC and HAT activities and acetylation of histones and non-histone chromatin proteins, and their health benefits are thought to be attributed to these epigenetic mechanisms. The intake of dietary compounds that regulate epigenetic modifications can provide significant health effects and may prevent various pathological processes involved in the development of cancer and other life-threatening diseases.
Nagarajan, M; Maruthanayagam, V; Sundararaman, M
Freshwater and terrestrial cyanobacteria resemble the marine forms in producing divergent chemicals such as linear, cyclic and azole containing peptides, alkaloids, cyclophanes, terpenes, lactones, etc. These metabolites have wider biomedical potentials in targeting proteases, cancers, parasites, pathogens and other cyanobacteria and algae (allelopathy). Among the various families of non-marine cyanobacterial peptides reported, many of them are acting as serine protease inhibitors. While the micropeptin family has a preference for chymotrypsin inhibition rather than other serine proteases, the aeruginosin family targets trypsin and thrombin. In addition, cyanobacterial compounds such as scytonemide A, lyngbyazothrins C and D and cylindrocyclophanes were found to inhibit 20S proteosome. Apart from proteases, metabolites blocking the other targets of cancer pathways may exhibit cytotoxic effect. Colon and rectum, breast, lung and prostate are the worst affecting cancers in humans and are deduced to be inhibited by both peptidic and non-peptidic compounds. Moreover, the growth of infections causing parasites such as Plasmodium, Leishmania and Trypanosoma are well controlled by peptides: aerucyclamides A-D, tychonamides and alkaloids: nostocarboline and calothrixins. Likewise, varieties of cyanobacterial compounds tend to inhibit serious infectious disease causing bacterial, fungal and viral agents. Interestingly, portoamides, spiroidesin, nostocyclamide and kasumigamide are the allelopathic peptides determined to suppress the growth of toxic cyanobacteria and nuisance algae. Thus cyanobacterial compounds have a broad bioactive spectrum; the analysis of SAR studies will not only assist to find out the mode of action but also reveal bioactive key components. Thereby, developing the drugs bearing these bioactive skeletons to treat various illnesses is wide open.
Fungo, Robert; Muyonga, John; Kaaya, Archileo; Okia, Clement; Tieguhong, Juius C; Baidu-Forson, Jojo J
Baillonella toxisperma, Pentaclethra macrophylla and Trichoscypha abut are important foods for communities living around forests in Cameroon. Information on the nutritional value and bioactive content of these foods is required to establish their contribution to the nutrition and health of the communities. Samples of the three foods were obtained from four villages in east and three villages in south Cameroon. The foods were analyzed for proximate composition, minerals and bioactive content using standard chemical analysis methods. T. abut was found to be an excellent source of bioactive compounds; flavonoids (306 mg/100 g), polyphenols (947 mg/100 g), proanthocyanins (61.2 mg/100 g), vitamin C (80.05 mg/100 g), and total oxalates (0.6 mg/100 g). P. macrophylla was found to be a rich source of total fat (38.71%), protein (15.82%) and total fiber (17.10%) and some bioactive compounds; vitamin E (19.4 mg/100 g) and proanthocyanins (65.0 mg/100 g). B. toxisperma, was found to have high content of carbohydrates (89.6%), potassium (27.5 mg/100 g) and calcium (37.5 mg/100 g). Flavonoids, polyphenols, vitamins C and E are the main bioactive compounds in these forest foods. The daily consumption of some of these fruits may coffer protection against some ailments and oxidative stress. Approximately 200 g of either B. toxisperma or P. macrophylla, can supply 100% iron and zinc RDAs for children aged 1–3 years, while 300 g of the two forest foods can supply about 85% iron and zinc RDAs for non-pregnant non-lactating women. The three foods provide 100% daily vitamins C and E requirements for both adults and children. The results of this study show that Baillonella toxisperma, Pentaclethra macrophylla and Trichoscypha abut can considerably contribute towards the human nutrient requirements. These forest foods also contain substantial levels of health promoting phytochemicals notably flavonoids, polyphenols, vitamins C and E. These foods therefore have
Ajila, C M; Rao, L Jaganmohan; Rao, U J S Prasada
Mango is one of the important tropical fruits in the world. As it is a seasonal fruit, it is processed for various products. During its processing, peel is one of the major byproducts, which is being wasted. Bioactive conserves were extracted using 80% acetone from peels of raw and ripe mango fruits and subjected to acid hydrolysis. The prominent phenolic compounds identified by HPLC were protocatechuic acid, gentisic acid and gallic acid. The phenolic acid derivatives present in acetone extracts of raw and ripe peels were tentatively identified by LC-MS. Gallic acid, syringic acid, mangiferin, ellagic acid, gentisyl-protocatechuic acid, quercetin were the phenolic compounds identified in both raw and ripe peels, while raw peel showed the presence of glycosylated iriflophenone and maclurin derivatives also. β-Carotene was the major carotenoid followed by violaxanthin and lutein. Thus, both raw and ripe mango peel extracts have different phenolic compounds and carotenoids, which will have various pharmaceutical applications.
Mas, Albert; Guillamon, Jose Manuel; Torija, Maria Jesus; Beltran, Gemma; Cerezo, Ana B; Troncoso, Ana M; Garcia-Parrilla, M Carmen
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.
Abugri, D A; Tiimob, B J; Apalangya, V A; Pritchett, G; McElhenney, W H
Sorghum bicolor L. Moench (Naga Red) red leaves is an ingredient used in rice and beans that is known as "waakye" in the Hausa language in some African countries. Little is known about its benefits aside from its colourant properties. We studied its bioactive, nutritive compounds and the effectiveness of four organic solvents (methanol, ethanol, acetone and diethyl ether) in isolation of these compounds to gain information regarding its health benefits to consumers. Of the compounds evaluated, the leaves consisted primarily of carotenoids, flavonoids and phenolic acids with small amounts of chlorophyll (a and b), lycopene and β-carotene. The fatty acid profiles of the leaves revealed palmitic, stearic, oleic and linoleic acid as predominant with each having greater than 5% of the total fatty acid identified. The nutritional implication of these findings is that the consumption of diets prepared with the leaves provides natural antioxidant and essential fatty acids that could fight cardiovascular related diseases.
Pimentel, Mariana Recco; Molina, Gustavo; Dionísio, Ana Paula; Maróstica Junior, Mário Roberto; Pastore, Gláucia Maria
Endophytes are microorganisms that reside asymptomatically in the tissues of higher plants and are a promising source of novel organic natural metabolites exhibiting a variety of biological activities. The laboratory of Bioaromas (Unicamp, Brazil) develops research in biotransformation processes and functional evaluation of natural products. With the intent to provide subsidies for studies on endophytic microbes related to areas cited before, this paper focuses particularly on the role of endophytes on the production of anticancer, antimicrobial, and antioxidant compounds and includes examples that illustrate their potential for human use. It also describes biotransformation as an auspicious method to obtain novel bioactive compounds from microbes. Biotransformation allows the production of regio- and stereoselective compounds under mild conditions that can be labeled as “natural,” as discussed in this paper. PMID:21350663
Guillamon, Jose Manuel; Torija, Maria Jesus; Beltran, Gemma; Troncoso, Ana M.; Garcia-Parrilla, M. Carmen
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
Martins, Natália; Barros, Lillian; Santos-Buelga, Celestino; Henriques, Mariana; Silva, Sónia; Ferreira, Isabel C F R
Bioactivity of oregano methanolic extracts and essential oils is well known. Nonetheless, reports using aqueous extracts are scarce, mainly decoction or infusion preparations used for therapeutic applications. Herein, the antioxidant and antibacterial activities, and phenolic compounds of the infusion, decoction and hydroalcoholic extract of oregano were evaluated and compared. The antioxidant activity is related with phenolic compounds, mostly flavonoids, since decoction presented the highest concentration of flavonoids and total phenolic compounds, followed by infusion and hydroalcoholic extract. The samples were effective against gram-negative and gram-positive bacteria. It is important to address that the hydroalcoholic extract showed the highest efficacy against Escherichia coli. This study demonstrates that the decoction could be used for antioxidant purposes, while the hydroalcoholic extract could be incorporated in formulations for antimicrobial features. Moreover, the use of infusion/decoction can avoid the toxic effects showed by oregano essential oil, widely reported for its antioxidant and antimicrobial properties.
Anunciação, Pamella Cristine; Cardoso, Leandro de Morais; Gomes, Jaqueline Vieira Piovesana; Della Lucia, Ceres Mattos; Carvalho, Carlos Wanderlei Piler; Galdeano, Melicia Cintia; Queiroz, Valéria Aparecida Vieira; Alfenas, Rita de Cássia Gonçalves; Martino, Hércia Stampini Duarte; Pinheiro-Sant'Ana, Helena Maria
The sensory acceptance and the content of bioactive compounds of whole-sorghum and whole-wheat breakfast cereals were compared. Sensory acceptance was assessed using the Food Action RatingScale. 3-Deoxyanthocyanidins, flavones and flavanones were determined by high-performance liquid chromatography (HPLC) with diode array detection, and vitamin E by HPLC with fluorescence detection. Total phenolics and antioxidant activity were determined by spectrophotometry. The sorghum breakfast cereal had better sensory acceptance (70.6%) than wheat breakfast cereal (41.18%). Sorghum had higher 3-deoxyanthocyanidin content (100% higher), total phenolic compounds (98.2% higher) and antioxidant activity (87.9% higher) than wheat breakfast cereal. Flavones and flavanones were not detected in both breakfast cereals. Total vitamin E content was 78.6% higher in wheat than in sorghum breakfast cereal. Thus, consumption of whole sorghum breakfast cereal should be encouraged, since it had good sensory acceptance and is a source of bioactive compounds that can promote benefits to human health.
Babbar, Neha; Oberoi, Harinder Singh; Sandhu, Simranjeet Kaur
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.
Ghosh, Goutam; Panda, Pritipadma; Rath, Meera; Pal, Abhisek; Sharma, Tripti; Das, Debajyoti
Background: Clerodendrum viscosum is commonly found in India and Bangladesh. Previously, various parts of this plant were reported for treatment of different types of diseases and there was no report on GC-Ms analysis. Objective: To analyze and characterize the phytochemical compounds of methanol extract of Clerodendrum viscosum using GC-MS. Materials and Methods: The preliminary phytochemical screening of methanol extract was carried out according to standard procedures described in WHO guidelines. Various bioactive compounds of the extract were determined by GC-MS technique. Results: The presence of steroids, triterpenoids, alkaloids, saponins, flavonoids, tannins and carbohydrate was found on phytochemical screening of methanol extract of the leaves. The GC-MS analysis showed 16 peaks of different phytoconstituents namely acetamide, N, N-carbonylbis-, 4-Pyranone,2,3-dihydro-, alpha-D-Galactofuranoside, methyl 2,3,5,6-tetra-O-methyl-, Glycerin, Xylitol, N, N-Dimethylglycine, 4H-Pyran-4-one,2,3-dihydro-3, 5-dihydroxy-6-methyl-, Benzofuran,2,3-dihydro-, 5-Hydroxymethylfurfural, 2(1H)Pyrimidinone,1-methyl-, 2,4-Dihydroxy-5,6-dimethylpyrimidine, 3-Deoxy-d-mannoic lactone, 1,3-Methylene-d-arabitol, Orcinol, n-Hexadecanoic acid and Phenol,4,4’-(1-methyl ethylidene) bis etc. Conclusion: The bioactive compounds present in the methanol extract of Clerodendrum viscosum suggest the application of this extract for the treatment of various diseases by the aborigine tribes. PMID:25598644
Kanthal, Lakshmi Kanta; Dey, Akalanka; Satyavathi, K.; Bhojaraju, P.
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
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
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.
Hippophae rhamnoides (sea buckthorn) offers many health benefits. It has significant cardioprotective activity and exerts many positive healing effects on the cardiovascular system, including inhibiting blood platelet activation (especially platelet aggregation), lowering cholesterol concentration and blood pressure, and providing antioxidant activity. In addition, sea buckthorn has antibacterial and antiviral properties. The leaves and fruits of the plant, and its oils, are sources of many bioactive substances including vitamins (A, C and E), unsaturated fatty acids, phenolic compounds, especially flavonoids, and phytosterols, which bestow positive effects on the cardiovascular system. This review article summarizes the current knowledge of the biological roles of sea buckthorn in cardiovascular diseases.
Rzuczek, Suzanne G.; Gao, Yu; Tang, Zhen-Zhi; Thornton, Charles A.; Kodadek, Thomas; Disney, Matthew D.
Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of a general program to study RNA function using small molecules, we designed bioactive, modularly assembled small molecules that target the non-coding expanded RNA repeat that causes myotonic dystrophy type 1 (DM1), r(CUG)exp. Herein, we present a rigorous study to elucidate features in modularly assembled compounds that afford bioactivity. Different modular assembly scaffolds were investigated including polyamines, α-peptides, β-peptides, and peptide tertiary amides (PTAs). Based on activity as assessed by improvement of DM1-associated defects, stability against proteases, cellular permeability, and toxicity, we discovered that constrained backbones, namely PTAs, are optimal. Notably, we determined that r(CUG)exp is the target of the optimal PTA in cellular models and that the optimal PTA improves DM1-associated defects in a mouse model. Biophysical analyses were employed to investigate potential sources of bioactivity. These investigations show that modularly assembled compounds have increased residence times on their targets and faster on rates than the RNA-binding modules from which they were derived and faster on rates than the protein that binds r(CUG)exp, the inactivation of which gives rise to DM1-associated defects. These studies provide information about features of small molecules that are programmable for targeting RNA, allowing for the facile optimization of therapeutics or chemical probes against other cellular RNA targets. PMID:24032410
Rzuczek, Suzanne G; Gao, Yu; Tang, Zhen-Zhi; Thornton, Charles A; Kodadek, Thomas; Disney, Matthew D
Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell-permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of a general program to study RNA function using small molecules, we designed bioactive, modularly assembled small molecules that target the noncoding expanded RNA repeat that causes myotonic dystrophy type 1 (DM1), r(CUG)(exp). Herein, we present a rigorous study to elucidate features in modularly assembled compounds that afford bioactivity. Different modular assembly scaffolds were investigated, including polyamines, α-peptides, β-peptides, and peptide tertiary amides (PTAs). On the basis of activity as assessed by improvement of DM1-associated defects, stability against proteases, cellular permeability, and toxicity, we discovered that constrained backbones, namely, PTAs, are optimal. Notably, we determined that r(CUG)(exp) is the target of the optimal PTA in cellular models and that the optimal PTA improves DM1-associated defects in a mouse model. Biophysical analyses were employed to investigate potential sources of bioactivity. These investigations show that modularly assembled compounds have increased residence times on their targets and faster on rates than the RNA-binding modules from which they were derived. Moreover, they have faster on rates than the protein that binds r(CUG)(exp), the inactivation of which gives rise to DM1-associated defects. These studies provide information about features of small molecules that are programmable for targeting RNA, allowing for the facile optimization of therapeutics or chemical probes against other cellular RNA targets.
Chang, Qing; Peng, Yue'e; Dan, Conghui; Shuai, Qin; Hu, Shenghong
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.
Hervert-Hernández, Deisy; Sáyago-Ayerdi, Sonia G; Goñi, Isabel
Pepper fruits (Capsicum annuum) contain a wide array of phytochemicals with well-known antioxidant properties. Since bioactive compounds depend on their bioavailability to exert beneficial effects, it was crucial to estimate the extent of release from the food matrix and thus their bioaccessibility. Accordingly, we determined the individual carotenoid and phenolic content as well as the antioxidant properties of four red hot dried cultivars (Capsicum annuum L.) of high consumption in Mexico and estimated the extent of intestinal bioaccessibility of carotenoids with significance in human health, beta-carotene, beta-cryptoxanthin, and zeaxanthin, using an in vitro gastrointestinal model. Hot dried peppers at ripe stage had a high content of bioactive compounds that exhibited significant antioxidant properties (26-80 micromol trolox equivalents/g of dry matter), such as polyphenols (>2000 mg/100 g of dry matter) and carotenoids (95-437 mg/100 g of dry matter), which were partially bioaccessible. The amount released from the food matrix by the action of digestive enzymes was about 75% for total polyphenols, up to 49% for both beta-carotene and zeaxanthin, and up to 41% for beta-cryptoxanthin. The results suggest that from 50 to 80% of these carotenoids could reach the colon to be potentially fermented or could remain unavailable.
Palmeri, Agostino; Mammana, Leonardo; Tropea, Maria Rosaria; Gulisano, Walter; Puzzo, Daniela
Rhodiola Rosea (R. Rosea) is a plant used in traditional popular medicine to enhance cognition and physical performance. R. Rosea medicinal properties have been related to its capability to act as an adaptogen, i.e., a substance able to increase the organism's resistance to a variety of chemical, biological, and physical stressors in a non-specific way. These adaptogen properties have been mainly attributed to the glycoside salidroside, one of the bioactive compounds present in the standardized extracts of R. Rosea. Here, we aimed to investigate whether a single dose of salidroside is able to affect memory and emotional behavior in wild type adult mice. We performed fear conditioning to assess cued and contextual memory, elevated plus maze and open field to evaluate anxiety, and tail suspension test to evaluate depression. Our results showed that a single i.p. administration of salidroside was able to enhance fear memory and exerted an anxiolytic and antidepressant effect. These data confirmed the adaptogenic effect of R. Rosea bioactive compounds in animal models and suggest that salidroside might represent an interesting pharmacological tool to ameliorate cognition and counteract mood disorders.
Lozano-Sánchez, Jesús; Castro-Puyana, María; Mendiola, Jose A.; Segura-Carretero, Antonio; Cifuentes, Alejandro; Ibáñez, Elena
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
Reboredo-Rodríguez, Patricia; Figueiredo-González, María; González-Barreiro, Carmen; Simal-Gándara, Jesús; Salvador, María Desamparados; Cancho-Grande, Beatriz; Fregapane, Giuseppe
Virgin olive oil, the main fat of the Mediterranean diet, is per se considered as a functional food—as stated by the European Food Safety Authority (EFSA)—due to its content in healthy compounds. The daily intake of endogenous bioactive phenolics from virgin olive oil is variable due to the influence of multiple agronomic and technological factors. Thus, a good strategy to ensure an optimal intake of polyphenols through habitual diet would be to produce enriched virgin olive oil with well-known bioactive polyphenols. Different sources of natural biological active substances can be potentially used to enrich virgin olive oil (e.g., raw materials derived from the same olive tree, mainly olive leaves and pomaces, and/or other compounds from plants and vegetables, mainly herbs and spices). The development of these functional olive oils may help in prevention of chronic diseases (such as cardiovascular diseases, immune frailty, ageing disorders and degenerative diseases) and improving the quality of life for many consumers reducing health care costs. In the present review, the most relevant scientific information related to the development of enriched virgin olive oil and their positive human health effects has been collected and discussed. PMID:28335517
Manosroi, Aranya; Chutoprapat, Romchat; Sato, Yuji; Miyamoto, Kukizo; Hsueh, Kesyin; Abe, Masahiko; Manosroi, Worapaka; Manosroi, Jiradej
Bioactive compounds [ferulic acid (F), gamma-oryzanol (O) and phytic acid (P)] in rice bran have been widely used as antioxidants in skin care products. However, one of the major problems of antioxidants is the deterioration of their activities during long exposure to air and light. Niosomes have been used to entrap many degradable active agents not only for stability improvement, but also for increasing skin hydration. The objective of this study was to determine antioxidant activities [by in vitro ORAC (oxygen radical absorbance capacity) and ex vivo lipid peroxidation inhibition assay] and in vivo human skin hydration effects of gel and cream containing the rice bran extracts entrapped in niosomes. Gel and cream containing the rice bran extracts entrapped in niosomes showed higher antioxidant activity (ORAC value) at 20-28 micromol of Trolox equivalents (TE) per gram of the sample than the placebo gel and cream which gave 16-18 micromolTE/g. Human sebum treated with these formulations showed more lipid peroxidation inhibition activity than with no treatment of about 1.5 times. The three different independent techniques including corneometer, vapometer and confocal Raman microspectroscopy (CRM) indicated the same trend in human skin hydration enhancement of the gel or cream formulations containing the rice bran extracts entrapped in niosomes of about 20, 3 and 30%, respectively. This study has demonstrated the antioxidant activities and skin hydration enhancement of the rice bran bioactive compounds when entrapped in niosomes and incorporated in cream formulations.
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
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.
Trox, Jennifer; Vadivel, Vellingiri; Vetter, Walter; Stuetz, Wolfgang; Scherbaum, Veronika; Gola, Ute; Nohr, Donatus; Biesalski, Hans Konrad
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.
Chaudhary, Priyanka; Jayaprakasha, G K; Porat, Ron; Patil, Bhimanagouda S
Ethylene is commercially used for artificial degreening of early season grapefruits. The present study investigated the effect of degreening and storage period on Star Ruby grapefruit (Citrus paradisi Macf.) bioactive compounds. Freshly harvested grapefruits were degreened in commercial packing shed for 60h using 2ppm of ethylene at a constant temperature of 20°C. Both degreened and non-degreened (control) fruits were stored at 10°C for 21days and later transferred to 20°C for a period of 14days to simulate shipment and retail store market conditions. Bioactive compounds including carotenoids, limonoids, flavonoids and furocoumarins were analyzed using high performance liquid chromatography. Nomilin was significantly higher (P<0.05) in degreened fruits at 35days after storage. In contrast, flavonoids such as narirutin, naringin and poncirin were significantly (P<0.05) lower in degreened fruits at 35days after storage. Degreening treatment reduced the levels of deacetyl nomilinic acid glucoside and bergamottin after 35days of storage; however, it had no significant effect on total soluble solids, decay, fruit softening, taste, odour, ascorbic acid, β-carotene, lycopene, limonin, neohesperidin, didymin, 6,7-dihydroxybergamottin, 5-geranyloxy-7-methoxycoumarin and radical scavenging activity. Therefore, degreening could be utilized to enhance the grapefruit aesthetic quality, with minimal effect on nutritional quality.
Encarnação, Telma; Pais, Alberto A C C; Campos, Maria G; Burrows, Hugh D
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.
El Marsni, Zouhir; Torres, Ascension; Varela, Rosa M; Molinillo, José M G; Casas, Lourdes; Mantell, Casimiro; Martinez de la Ossa, Enrique J; Macias, Francisco A
The work described herein is a continuation of our initial studies on the supercritical fluid extraction (SFE) with CO2 of bioactive substances from Helianthus annuus L. var. Arianna. The selected SFE extract showed high activity in the wheat coleoptile bioassay, in Petri dish phytotoxicity bioassays, and in the hydroponic culture of tomato seeds. Chromatographic fractionations of the extracts and a spectroscopic analysis of the isolated compounds showed 52 substances belonging to 10 different chemical classes, which were mainly sesquiterpene lactones, diterpenes, and flavonoids. Heliannuol M (31), helivypolides K and L (36, 37), and helieudesmanolide B (38) are described for the first time in the literature. Metabolites have been tested in the etiolated wheat coleoptile bioassay with good results in a noteworthy effect on germination. The most active compounds were also tested on tomato seeds, heliannuol A (30) and leptocarpin (45) being the most active, with values similar to those of the commercial herbicide.
Ferracane, Rosalia; Graziani, Giulia; Gallo, Monica; Fogliano, Vincenzo; Ritieni, Alberto
In this work the bioactive metabolic profile, the antioxidant activity and total phenolic content of burdock (Arctium lappa) seeds, leaves and roots were obtained. TEAC values and total phenolic content for hydro-alcoholic extracts of burdock ranged from 67.39 to 1.63 micromol Trolox equivalent/100g dry weight (DW), and from 2.87 to 45 g of gallic acid equivalent/100g DW, respectively. Phytochemical compounds were analyzed by liquid chromatography coupled to electrospray tandem mass spectrometry (LC/MS/MS) in negative mode. The main compounds of burdock extracts were caffeoylquinic acid derivatives, lignans (mainly arctiin) and various flavonoids. The occurrence of some phenolic acids (caffeic acid, chlorogenic acid and cynarin) in burdock seeds; arctiin, luteolin and quercetin rhamnoside in burdock roots; phenolic acids, quercetin, quercitrin and luteolin in burdock leaves was reported for the first time.
Zizyphus lotus, belonging to the Rhamnaceae family, is a deciduous shrub which generally grows in arid and semiarid regions of the globe. In traditional medicine, Z. lotus is used as antidiabetes, sedative, bronchitis, and antidiarrhea by local populations. Recently, several scientific reports for health benefit and nutritional potential of bioactive compounds from this jujube have been reported. This plant is rich in polyphenols, cyclopeptide alkaloids, dammarane saponins, vitamins, minerals, amino acids, and polyunsaturated fatty acids. These identified compounds were supposed to be responsible for most of Z. lotus biologically relevant activities including antimicrobial, anti-inflammatory, hypoglycemic, antioxidant, and immunomodulatory effects. The aim of the present review was to give particular emphasis on the most recent findings on biological effects of the major groups of Zizyphus lotus components and their medical interest, notably for human nutrition, health benefit, and therapeutic impacts. PMID:28053781
Ghembaza, Nacéra; Belyagoubi-Benhammou, Nabila; Atik Bekkara, Fawzia
In the present paper, for the first time, we are interested to separate and identify some bioactive fractions isolated from the roots of a Saharan plant Anabasis articulata, which is widely used in traditional medicine against cancer. The crude methanolic extract of the roots was fractionated on column chromatography, and eluted with dichloromethane/methanol each time with increasing polarity of methanol; 17 fractions were separated. One of these fractions named F12 showed more antioxidant activity to scavenge DPPH free radical with percentage inhibition of 95.29%. F12 was separated by thin-layer chromatography (TLC) to give 12 compounds. A second preparative TLC of compound 2, which has antioxidative activity of 74.92%, provided the three phenolic acids M1, M2 and M3, analysed by high-performance liquid chromatography and UV-visible spectrophotometry.
Singh, Balwinder; Singh, Jatinder Pal; Kaur, Amritpal; Singh, Narpinder
Banana is a very popular fruit in the world market and is consumed as staple food in many countries. It is grown worldwide and constitutes the fifth most important agricultural food crop in terms of world trade. It has been classified into the dessert or sweet bananas and the cooking bananas or plantains. It is either eaten raw or processed, and also as a functional ingredient in various food products. Banana contains several bioactive compounds, such as phenolics, carotenoids, biogenic amines and phytosterols, which are highly desirable in the diet as they exert many positive effects on human health and well-being. Many of these compounds have antioxidant activities and are effective in protecting the body against various oxidative stresses. In the past, bananas were effectively used in the treatment of various diseases, including reducing the risk of many chronic degenerative disorders. In the present review, historical background, cultivar classification, beneficial phytochemicals, antioxidant activity and health benefits of bananas are discussed.
Froissard, Didier; Rapior, Sylvie; Bessière, Jean-Marie; Fruchier, Alain; Buatois, Bruno; Fons, Françoise
Aerial parts of six Dryopteris species collected in France were investigated for volatile organic compounds (VOC) for the first time. Fifty-three biosynthesized VOC from the shikimic, lipidic and terpenic pathways were identified using gas chromatography/mass spectrometry. Many bioactive polyketide compounds as filicinic derivatives (from 8.5 to 23.5%) and phloroglucinol derivatives (from 8.2 to 53.8%) with various pharmacological activities were detected in high amount from five analysed Dryopteris species, in particular D. oreades and D. borreri, i.e., propionylfilicinic acid (> 10% in D. affinis and D. ardechensis) and 2,6-dihydroxy-4-methoxy-3-methylbutyrophenone (aspidinol) (19.1% and 14.6% in D. oreades and D. borreri, respectively). Several terpenic derivatives with a low odor threshold were identified, i.e., carota-5,8-diene (from 2.5 to 18.4%: floral, woody or fresh bark note), (E)-nerolidol (> 10% for D. borreri and D. cambrensis; floral or woody odor), alpha-selinene (> 7% for D. ardechensis; woody-spicy odor), and aristolene (12.8% in D. affinis; flower, sweet odor). The main isoprenoid derivatives were 4-hydroxy-5,6-epoxyionol, 3-oxo-alpha-ionol and 4-oxo-7,8-dihydro-beta-ionone (essentially in D. remota), whereas the main aromatic compound was 4-hydroxy-3-methoxyacetophenone (20.6% and 12.6% in D. cambrensis and D. borreri, respectively) and the main lipid derivative was 1-octen-3-ol with a mushroom-like odor (from 0.4 to 8.3%). Dryopteris species resources are of great interest as a reservoir of odorous and bioactive compounds.
Chang, Jia-Dong; Mantri, Nitin; Sun, Bin; Jiang, Li; Chen, Ping; Jiang, Bo; Jiang, Zhengdong; Zhang, Jialei; Shen, Jiahao; Lu, Hongfei; Liang, Zongsuo
Recently, an important topic of research has been how climate change is seriously threatening the sustainability of agricultural production. However, there is surprisingly little experimental data regarding how elevated temperature and CO2 will affect the growth of medicinal plants and production of bioactive compounds. Here, we comprehensively analyzed the effects of elevated CO2 and temperature on the photosynthetic process, biomass, total sugars, antioxidant compounds, antioxidant capacity, and bioactive compounds of Gynostemma pentaphyllum. Two different CO2 concentrations [360 and 720μmolmol(-1)] were imposed on plants grown at two different temperature regimes of 23/18 and 28/23°C (day/night) for 60days. Results show that elevated CO2 and temperature significantly increase the biomass, particularly in proportion to inflorescence total dry weight. The chlorophyll content in leaves increased under the elevated temperature and CO2. Further, electron transport rate (ETR), photochemical quenching (qP), actual photochemical quantum yield (Yield), instantaneous photosynthetic rate (Photo), transpiration rate (Trmmol) and stomatal conductance (Cond) also increased to different degrees under elevated CO2 and temperature. Moreover, elevated CO2 increased the level of total sugars and gypenoside A, but decreased the total antioxidant capacity and main antioxidant compounds in different organs of G. pentaphyllum. Accumulation of total phenolics and flavonoids also decreased in leaves, stems, and inflorescences under elevated CO2 and temperature. Overall, our data indicate that the predicted increase in atmospheric temperature and CO2 could improve the biomass of G. pentaphyllum, but they would reduce its health-promoting properties.
To understand the material basis and underlying molecular machinery of antiosteoporosis activity of the Flos Chrysanthemi Indici (FCI), the consequences of ethanol extract on the bone loss in mice induced due to ovariectomy (OVX) was evaluated. Also, the antiosteoporosis fraction obtained from the FCI ethanol extract was isolated and purified using a preparative high-speed countercurrent chromatography (HSCCC). The in vitro impact of the compounds was investigated on osteoblast proliferation and differentiation. The results revealed that ethyl acetate fraction with robust in vivo antiosteoporosis activity was obtained. The important compounds purified by HSCCC using gradient elution system included acacetin, apigenin, luteolin, and linarin. The four compounds enhanced the differentiation and proliferation of osteoblasts in MC3T3-E1 cells. They also augmented the mRNA levels of runt-related transcription factor 2 (Runx2), osteocalcin (OCN), osteopontin (OPN), and type I collagen (COL I). The AKT signaling pathway was also activated in MC3T3-E1 cells by the four compounds. The present study demonstrated that the antiosteoporosis effects of FCI did not depend on a single component, and HSCCC efficiently isolated and purified the antiosteoporosis bioactive compounds from FCI. PMID:27885328
Tan, Woan Sean; Arulselvan, Palanisamy; Karthivashan, Govindarajan; Fakurazi, Sharida
Aim of Study. Moringa oleifera Lam. (M. oleifera) possess highest concentration of antioxidant bioactive compounds and is anticipated to be used as an alternative medicine for inflammation. In the present study, we investigated the anti-inflammatory activity of 80% hydroethanolic extract of M. oleifera flower on proinflammatory mediators and cytokines produced in lipopolysaccharide- (LPS-) induced RAW 264.7 macrophages. Materials and Methods. Cell cytotoxicity was conducted by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Nitric oxide (NO) production was quantified through Griess reaction while proinflammatory cytokines and other key inflammatory markers were assessed through enzyme-linked immunosorbent assay (ELISA) and immunoblotting. Results. Hydroethanolic extract of M. oleifera flower significantly suppressed the secretion and expression of NO, prostaglandin E2 (PGE2), interleukin- (IL-) 6, IL-1β, tumor necrosis factor-alpha (TNF-α), nuclear factor-kappa B (NF-κB), inducible NO synthase (iNOS), and cyclooxygenase-2 (COX-2). However, it significantly increased the production of IL-10 and IκB-α (inhibitor of κB) in a concentration dependent manner (100 μg/mL and 200 μg/mL). Conclusion. These results suggest that 80% hydroethanolic extract of M. oleifera flower has anti-inflammatory action related to its inhibition of NO, PGE2, proinflammatory cytokines, and inflammatory mediator's production in LPS-stimulated macrophages through preventing degradation of IκB-α in NF-κB signaling pathway. PMID:26609199
Fernandez, Sulmer; Pedrow, Patrick; Powers, Joseph; Pitts, Marvin
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.
Michalska, Anna; Łysiak, Grzegorz
Blueberries, besides having commonly-recognized taste properties, are also a valuable source of health-promoting bioactive compounds. For several decades, blueberries have gained in popularity all over the world, and recent years have seen not only an increase in fresh consumption, but also in the importance of blueberries for the processing industry. Blueberry processing mostly consists of freezing and juicing. Recently, more attention has been drawn to dewatering and drying, which are promising areas for developing novel blueberry products. Processing affects each biologically-active compound in a different way, and it is still unknown what changes those compounds undergo at the molecular level after the application of different processing technologies. This work presents the most recent state of knowledge about the pre-treatment and processing methods applied to blueberries and their influence on the content of biologically-active compounds. The presentation of methods is preceded by a brief overview of the characteristics of the blueberry species, a description of the chemical composition of the fruit and a short note about the main growing areas, production volumes and the management of fruit crops.
Shashirekha, M N; Mallikarjuna, S E; Rajarathnam, S
Components of cereals, legumes, pulses, proteins, sea food, milk, carbohydrates and lipids are being evaluated for their influence on human health, as biofunctional compounds. However, references dealing with fruits and vegetables exceed any other food group and accordingly their focus. Fruits and vegetables abound in a spectacular range of such health influencing compounds and thus, study of their bioactivity, in lieu of their consumption in fresh or processed form. Anti-cancerous phenolics from Phyllanthus, radioprotective Litchi phenolics/flavonoids, hypoglycemic Sygium, quercitin and hydroxyl cinnamates of Sweet cherries, xanthones of Mangosteen, ellagitannins of Pomegranate, ursolic acid of Sea buckthorn, muscle relaxative watermelon, anti-cholesterolemic soluble fibre and sterols, cardioprotective saponins, ACE-inhibitory potato hydrolysates, anti-pancreatic cancerous ascorbic acid, carotenoids including pro-vitamin A are few examples unraveled. Thus, the imminent scope to obviate their structural chemistry, influence on storage and processing conditions, factors favoring their bio-accessibility/bio-availability in the food formulations, influencing human health. It is the meticulous combination of these compounds in daily consumption that determines their usefulness to human body. What is of paramount importance is the actual health benefits accrued from consumption of such functional- compound based fresh/processed fruits,vegetables or other foods.
Michalska, Anna; Łysiak, Grzegorz
Blueberries, besides having commonly-recognized taste properties, are also a valuable source of health-promoting bioactive compounds. For several decades, blueberries have gained in popularity all over the world, and recent years have seen not only an increase in fresh consumption, but also in the importance of blueberries for the processing industry. Blueberry processing mostly consists of freezing and juicing. Recently, more attention has been drawn to dewatering and drying, which are promising areas for developing novel blueberry products. Processing affects each biologically-active compound in a different way, and it is still unknown what changes those compounds undergo at the molecular level after the application of different processing technologies. This work presents the most recent state of knowledge about the pre-treatment and processing methods applied to blueberries and their influence on the content of biologically-active compounds. The presentation of methods is preceded by a brief overview of the characteristics of the blueberry species, a description of the chemical composition of the fruit and a short note about the main growing areas, production volumes and the management of fruit crops. PMID:26266408
Sinha, S; Chand, S; Tripathi, P
Ecological samples rich in microbial diversity like cow dung, legume rhizosphere, fish waste and garden soil were used for isolation of chitosan-degrading microorganisms. Selected isolates were used for production of chitosanase and food related bioactive compounds by conversion of biowaste. Production of glucosamine (Gln), N-acetylglucosamine (NAG), chitooligosaccharides (COS), antioxidants, antibacterial compounds and prebiotics was carried out by microbial fermentation of biowaste. The highest chitosanase activity (8 U/mL) was observed in Aspergillus sp. isolated from fish market waste and it could produce Gln and NAG while Streptomyces sp. isolated from garden soil was able to produce COS along with Gln and NAG. Radical scavenging activity was observed in culture supernatants of 35% of studied isolates, and 20% isolates secreted compounds which showed positive effect on growth of Bifidobacterium. Antibacterial compounds were produced by 40% of selected isolates and culture supernatants of two microbial isolates, Streptomyces zaomyceticus C6 and one of garden soil isolates, were effective against both gram positive and negative bacteria.
Benkendorff, Kirsten; Rudd, David; Devi Nongmaithem, Bijayalakshmi; Liu, Lei; Young, Fiona; Edwards, Vicki; Avila, Cathy; Abbott, Catherine A.
Marine molluscs from the family Muricidae hold great potential for development as a source of therapeutically useful compounds. Traditionally known for the production of the ancient dye Tyrian purple, these molluscs also form the basis of some rare traditional medicines that have been used for thousands of years. Whilst these traditional and alternative medicines have not been chemically analysed or tested for efficacy in controlled clinical trials, a significant amount of independent research has documented the biological activity of extracts and compounds from these snails. In particular, Muricidae produce a suite of brominated indoles with anti-inflammatory, anti-cancer and steroidogenic activity, as well as choline esters with muscle-relaxing and pain relieving properties. These compounds could explain some of the traditional uses in wound healing, stomach pain and menstrual problems. However, the principle source of bioactive compounds is from the hypobranchial gland, whilst the shell and operculum are the main source used in most traditional remedies. Thus further research is required to understand this discrepancy and to optimise a quality controlled natural medicine from Muricidae. PMID:26295242
Grienke, Ulrike; Silke, Joe; Tasdemir, Deniz
The consumption of marine mussels as popular seafood has increased steadily over the past decades. Awareness of mussel derived molecules, that promote health, has contributed to extensive research efforts in that field. This review highlights the bioactive potential of mussel components from species of the genus Mytilus (e.g. M. edulis) and Perna (e.g. P. canaliculus). In particular, the bioactivity related to three major chemical classes of mussel primary metabolites, i.e. proteins, lipids, and carbohydrates, is evaluated. Within the group of proteins the focus is mainly on mussel peptides e.g. those obtained by bio-transformation processes, such as fermentation. In addition, mussel lipids, comprising polyunsaturated fatty acids (PUFAs), are discussed as compounds that are well known for prevention and treatment of rheumatoid arthritis (RA). Within the third group of carbohydrates, mussel polysaccharides are investigated. Furthermore, the importance of monitoring the mussel as food material in respect to contaminations with natural toxins produced by microalgae is discussed.
Rodríguez Arce, Esteban; Machado, Ignacio; Rodríguez, Belén; Lapier, Michel; Zúñiga, María Carolina; Maya, Juan Diego; Olea Azar, Claudio; Otero, Lucía; Gambino, Dinorah
American Trypanosomiasis is a chronic infection discovered and described in 1909 by the Brazilian scientist Carlos Chagas. It is caused by the protozoan parasite Trypanosoma cruzi. Although it affects about 10million people in Latin America, the current chemotherapy is still inadequate. The discovery of new drugs is urgently needed. Our group is focused on the development of prospective metal-based drugs mainly based on bioactive ligands and pharmacologically interesting metal ions. In this work three new rhenium(I) tricarbonyl compounds fac-[Re(I)(CO)3Br(HL)] where HL=5-nitrofuryl containing thiosemicarbazones were synthesized and fully characterized in solution and in the solid state. The in vitro evaluation of the compounds on T. cruzi trypomastigotes (Dm28c strain) showed that the Re(I) compounds are 8 to 15 times more active than the reference drug Nifurtimox and show a 4 to 17 fold increase in activity in respect to the free (HL) ligands. Obtained compounds also show good selectivity indexes (IC50 endothelial cells Ea.hy926/IC50 T. cruzi (Dm28c tripomastigotes)). (1)H NMR and MS studies, performed with time, showed that the fac-[Re(CO)3Br(HL)] species convert into the dimers [Re2(CO)6(L)2] in solution. Crystal structure of [Re(I)2(CO)6(L2)2], the product of complexes' dimerization, was solved. Related to the mechanism of action, the studied compounds do not generate radical oxygen species in the parasite (as 5-nitrofuryl derived thiosemicarbazones do) probably due to the unfavorable nitro reduction potential of the generated dimeric species. On the contrary, the compounds produce a decrease of the oxygen consumption rate of the parasites, maybe inhibiting their mitochondrial respiration.
Vardanega, Renata; Santos, Diego T.; Meireles, M. Angela A.
Extraction processes are largely used in many chemical, biotechnological and pharmaceutical industries for recovery of bioactive compounds from medicinal plants. To replace the conventional extraction techniques, new techniques as high-pressure extraction processes that use environment friendly solvents have been developed. However, these techniques, sometimes, are associated with low extraction rate. The ultrasound can be effectively used to improve the extraction rate by the increasing the mass transfer and possible rupture of cell wall due the formation of microcavities leading to higher product yields with reduced processing time and solvent consumption. This review presents a brief survey about the mechanism and aspects that affecting the ultrasound assisted extraction focusing on the use of ultrasound irradiation for high-pressure extraction processes intensification. PMID:25125880
Toro-Funes, N; Bosch-Fusté, J; Veciana-Nogués, M T; Vidal-Carou, M C
Ultra high pressure homogenization (UHPH) is a useful novel technology to obtain safe and high-quality liquid foods. The effect of UHPH at 200 and 300 MPa in combination with different inlet temperatures (Tin) (55, 65 and 75 °C) on the bioactive compounds of soya milk was studied. Total phytosterols increased with the higher combination of pressure and temperature. The main phytosterol was β-sitosterol, followed by stigmasterol and campesterol. Total tocopherols in UHPH-treated soya milks decreased as the temperature and pressure increased. UHPH treatment also affected the different chemical forms of tocopherols. No biogenic amines were detected in any of the analyzed soya milks. Meanwhile, the polyamines SPD and SPM were found in all soya milks, being stable to the UHPH treatment. Total isoflavones increased with the higher combination of pressure and temperature. No differences in the isoflavone profile were found, with β-glucoside conjugates being the predominant form.
Limón, Rocio I; Peñas, Elena; Torino, M Inés; Martínez-Villaluenga, Cristina; Dueñas, Montserrat; Frias, Juana
The influence of solid (SSF) or liquid state fermentation (LSF) for 48 and 96 h on the production of water soluble extracts from kidney beans was investigated. SSF was carried out by Bacillus subtilis, whilst LSF was performed either by natural fermentation (NF) or by Lactobacillus plantarum strain (LPF). SSF extracts showed high soluble phenolic compound content (31-36 mg/g) and antioxidant activity (508-541 μg trolox equivalents/g), whilst LSF extracts exhibited potential antihypertensive activity due to their large γ-aminobutyric acid (GABA) content (6.8-10.6 mg/g) and angiotensin converting enzyme inhibitory (ACEI) activity (>90%). Therefore, fermentation can be considered as a valuable process to obtain bioactive ingredients from kidney beans, which could encourage their utilisation in the formulation of added-value functional foods.
Nicoletti, Rosario; Trincone, Antonio
In recent years, the search for novel natural compounds with bioactive properties has received a remarkable boost in view of their possible pharmaceutical exploitation. In this respect the sea is entitled to hold a prominent place, considering the potential of the manifold animals and plants interacting in this ecological context, which becomes even greater when their associated microbes are considered for bioprospecting. This is the case particularly of fungi, which have only recently started to be considered for their fundamental contribution to the biosynthetic potential of other more valued marine organisms. Also in this regard, strains of species which were previously considered typical terrestrial fungi, such as Penicillium and Talaromyces, disclose foreground relevance. This paper offers an overview of data published over the past 25 years concerning the production and biological activities of secondary metabolites of marine strains belonging to these genera, and their relevance as prospective drugs. PMID:26901206
Scapagnini, Giovanni; Davinelli, Sergio; Di Renzo, Laura; De Lorenzo, Antonino; Olarte, Hector Hugo; Micali, Giuseppe; Cicero, Arrigo F.; Gonzalez, Salvador
Cocoa has a rich history in human use. Skin is prone to the development of several diseases, and the mechanisms in the pathogenesis of aged skin are still poorly understood. However, a growing body of evidence from clinical and bench research has begun to provide scientific validation for the use of cocoa-derived phytochemicals as an effective approach for skin protection. Although the specific molecular and cellular mechanisms of the beneficial actions of cocoa phytochemicals remain to be elucidated, this review will provide an overview of the current literature emphasizing potential cytoprotective pathways modulated by cocoa and its polyphenolic components. Moreover, we will summarize in vivo studies showing that bioactive compounds of cocoa may have a positive impact on skin health. PMID:25116848
Bartłomiej, Siurek; Justyna, Rosicka-Kaczmarek; Ewa, Nebesny
This review presents current information about principal, biologically active compounds contained in grains of cereals that are most popular in Europe (wheat, rye, barley and oat). The tendency to provide consumers with safe foods, which promote their health and are based on cereal grains and/or their components with the high nutritive value, has been recently observed. The intake of protective substances contained in whole grains and their fractions contributes to a decreased risk of food-dependent diseases like the coronary heart disease and insulin-dependent diabetes. This study describes the structure, occurrence in cereal grains, technological importance and beneficial influence on human health of bioactive substances such as arabinoxylans, β-glucans, alkylresorcinols, tocols and phytosterols.
Madeira, Jose Valdo; Macedo, Gabriela Alves
Recent studies have pointed to a reduction in the incidence of some cancers, diabetes, and neuro-degenerative diseases as a result of human health benefits from flavanones. Currently, flavanones are obtained by chemical synthesis or extraction from plants, and these processes are only produced in the glycosylated form. An interesting environmentally friendly alternative that deserves attention regarding phenolic compound production is the simultaneous extraction and biotransformation of these molecules. Orange juice consumption has become a worldwide dietary habit and Brazil is the largest producer of orange juice in the world. Approximately half of the citrus fruit is discarded after the juice is processed, thus generating large amounts of residues (peel and pectinolytic material). Hence, finding an environmentally clean technique to extract natural products and bioactive compounds from different plant materials has presented a challenging task over the last decades. The aim of this study was to obtain phenolics from Brazilian citrus residues with high bioactivity, using simultaneous extraction (cellulase and pectinase) and biotransformation (tannase) by enzymatic process. The highest hesperetin, naringenin and ellagic acid production in the experiment were 120, 80, and 11,250 µg g(-1), respectively, at 5.0 U mL(-1) of cellulase and 7.0 U mL(-1) of tannase at 40°C and 200 rpm. Also, the development of this process generated an increase of 77% in the total antioxidant capacity. These results suggest that the bioprocess obtained innovative results where the simultaneous enzymatic and biotransformatic extracted flavanones from agro-industrial residues was achieved without the use of organic solvents. The methodology can therefore be considered a green technology.
Tarazona-Díaz, M P; Aguayo, E
The fresh-cut industry is constantly growing and generating wastes. The major challenge for this industry consists in an environmentally sustainable production through re-utilization of by-products, for instance, in extraction of bioactive compounds. In this paper, the nutritional and functional compounds of apple, potato, cucumber, melon and watermelon by-products were investigated. The amount of by-product produced was of 10.10 to 30.80% of initial fresh weight depending on the product. By-products were characterized by low protein (<20 g/kg fresh weight) and fatty acid content (<5 g/kg fresh weight) and high levels of minerals. Carbohydrates content ranged from 43.7 to 235 g/kg fresh weight, while total dietary fibre was between 20 and 150 g/kg fresh weight The content of antioxidants (53.6 to 3453.2 mg/kg fresh weight) and total polyphenols (124.5 to 4250.2 mg/kg fresh weight) depended strongly on the type of by-product. In most cases, the nutritional and bioactive content was higher in the peel than in whole product. Apple peel was rich in carbohydrates, total dietary fibre, antioxidants and total polyphenols. Potato peel was high in iron. Melon was rich in magnesium. Watermelon peel was characterized by the level of potassium, and cucumber peel was rich in manganese, zinc, phosphorous, calcium and sodium. All these data demonstrate than natural by-product from fresh-cut industry could potentially be utilized as ingredients to design new functional foods with a future market.
Tsogoeva, Svetlana B
The present mini-review highlights the recent developments on different classes of synthetic hybrids of natural and/or unnatural bioactive compounds, the utilization of which is very promising, as distinct features of each component can be hybridized and their properties leveraged. Particular stress is put on the respective mode of action and the corresponding rationale behind covalent combinations of various bioactive agents to increase their therapeutic potential, facilitate their administration, to reduce harmful side effects and/or to overcome the problem of multi-drug resistance. This rather recent approach has already found applications in the development of new anti-cancer, anti-Alzheimer, anti-malaria, anti-microbial therapeutics and other novel compounds with unprecedented bioactivity.
de Oliveira, Admilton G.; Spago, Flavia R.; Simionato, Ane S.; Navarro, Miguel O. P.; da Silva, Caroline S.; Barazetti, André R.; Cely, Martha V. T.; Tischer, Cesar A.; San Martin, Juca A. B.; de Jesus Andrade, Célia G. T.; Novello, Cláudio R.; Mello, João C. P.; Andrade, Galdino
Citrus canker is a very destructive disease of citrus species. The challenge is to find new compounds that show strong antibiotic activity and low toxicity to plants and the environment. The objectives of the present study were (1) to extract, purify and evaluate the secondary metabolites with antibiotic activity produced by Pseudomonas aeruginosa LV strain in vitro against Xanthomonas citri subsp. citri (strain 306), (2) to determine the potential of semi-purified secondary metabolites in foliar application to control citrus canker under greenhouse conditions, and (3) to identify antibiotic activity in orange leaf mesophyll infected with strain 306, by electron microscopy. Two pure bioactive compounds were isolated, an organocopper antibiotic compound (OAC) and phenazine-1-carboxamide. Phenazine-1-carboxamide did not show any antibiotic activity under the experimental conditions used in this study. The OAC showed a high level of antibiotic activity with a minimum inhibitory concentration of 0.12 μg mL-1. In greenhouse tests for control of citrus canker in orange trees, the semi-purified fraction F3d reduced lesion formation by about 97%. The concentration used was 500 times lower than that for the recommended commercial copper-based product. Electron microscopy showed that F3d altered the exopolysaccharide matrix and caused cell lysis of the pathogen inside the citrus canker lesions. These results suggest that secondary metabolites produced by inducing P. aeruginosa LV strain have a high potential to be used as a bioproduct to control citrus canker. PMID:26903992
Lemos, M Adília; Sárniková, Katarína; Bot, Francesca; Anese, Monica; Hungerford, Graham
The study of compounds that exhibit antioxidant activity has recently received much interest in the food industry because of their potential health benefits. Most of these compounds are plant based, such as polyphenolics and carotenoids, and there is a need to monitor them from the field through processing and into the body. Ideally, a monitoring technique should be non-invasive with the potential for remote capabilities. The application of the phenomenon of fluorescence has proved to be well suited, as many plant associated compounds exhibit fluorescence. The photophysical behaviour of fluorescent molecules is also highly dependent on their microenvironment, making them suitable probes to monitor changes in pH, viscosity and polarity, for example. Time-resolved fluorescence techniques have recently come to the fore, as they offer the ability to obtain more information, coupled with the fact that the fluorescence lifetime is an absolute measure, while steady state just provides relative and average information. In this work, we will present illustrative time-resolved measurements, rather than a comprehensive review, to show the potential of time-resolved fluorescence applied to the study of bioactive substances. The aim is to help assess if any changes occur in their form, going from extraction via storage and cooking to the interaction with serum albumin, a principal blood transport protein.
de Oliveira, Admilton G; Spago, Flavia R; Simionato, Ane S; Navarro, Miguel O P; da Silva, Caroline S; Barazetti, André R; Cely, Martha V T; Tischer, Cesar A; San Martin, Juca A B; de Jesus Andrade, Célia G T; Novello, Cláudio R; Mello, João C P; Andrade, Galdino
Citrus canker is a very destructive disease of citrus species. The challenge is to find new compounds that show strong antibiotic activity and low toxicity to plants and the environment. The objectives of the present study were (1) to extract, purify and evaluate the secondary metabolites with antibiotic activity produced by Pseudomonas aeruginosa LV strain in vitro against Xanthomonas citri subsp. citri (strain 306), (2) to determine the potential of semi-purified secondary metabolites in foliar application to control citrus canker under greenhouse conditions, and (3) to identify antibiotic activity in orange leaf mesophyll infected with strain 306, by electron microscopy. Two pure bioactive compounds were isolated, an organocopper antibiotic compound (OAC) and phenazine-1-carboxamide. Phenazine-1-carboxamide did not show any antibiotic activity under the experimental conditions used in this study. The OAC showed a high level of antibiotic activity with a minimum inhibitory concentration of 0.12 μg mL(-1). In greenhouse tests for control of citrus canker in orange trees, the semi-purified fraction F3d reduced lesion formation by about 97%. The concentration used was 500 times lower than that for the recommended commercial copper-based product. Electron microscopy showed that F3d altered the exopolysaccharide matrix and caused cell lysis of the pathogen inside the citrus canker lesions. These results suggest that secondary metabolites produced by inducing P. aeruginosa LV strain have a high potential to be used as a bioproduct to control citrus canker.
Ariza, María Teresa; Reboredo-Rodríguez, Patricia; Mazzoni, Luca; Forbes-Hernández, Tamara Yuliett; Giampieri, Francesca; Afrin, Sadia; Gasparrini, Massimiliano; Soria, Carmen; Martínez-Ferri, Elsa; Battino, Maurizio; Mezzetti, Bruno
Strawberries are highly appreciated for their taste, nutritional value and antioxidant compounds, mainly phenolics. Fruit antioxidants derive from achenes and flesh, but achene contribution to the total fruit antioxidant capacity and to the bioaccessibility after intake is still unknown. In this work, the content of total phenolic compounds, flavonoids, anthocyanins and antioxidant capacity (TEAC, FRAP and DPPH) of achenes and flesh were compared in non-digested as well as in gastric and intestinal extracts after in vitro digestion. Results showed that, despite strawberry achenes represent a small fraction of the fruit, their contribution to total fruit antioxidant content was more than 41% and accounted for 81% of antioxidant capacity (TEAC). Achenes have higher quantity and different quality of antioxidants in non-digested and digested extracts. Antioxidant release was higher in the in vitro gastric digested extracts, but digestion conditions did not only affect quantity but quality, resulting in differences in antioxidant capacity and highlighting the importance of simulating physiological-like extraction conditions for assessing fruit antioxidant properties on human health. These results give new insights into the use of strawberry achenes as a source of bioactive compounds to be considered in strawberry breeding programs for improving human health.
Ariza, María Teresa; Reboredo-Rodríguez, Patricia; Mazzoni, Luca; Forbes-Hernández, Tamara Yuliett; Giampieri, Francesca; Afrin, Sadia; Gasparrini, Massimiliano; Soria, Carmen; Martínez-Ferri, Elsa; Battino, Maurizio; Mezzetti, Bruno
Strawberries are highly appreciated for their taste, nutritional value and antioxidant compounds, mainly phenolics. Fruit antioxidants derive from achenes and flesh, but achene contribution to the total fruit antioxidant capacity and to the bioaccessibility after intake is still unknown. In this work, the content of total phenolic compounds, flavonoids, anthocyanins and antioxidant capacity (TEAC, FRAP and DPPH) of achenes and flesh were compared in non-digested as well as in gastric and intestinal extracts after in vitro digestion. Results showed that, despite strawberry achenes represent a small fraction of the fruit, their contribution to total fruit antioxidant content was more than 41% and accounted for 81% of antioxidant capacity (TEAC). Achenes have higher quantity and different quality of antioxidants in non-digested and digested extracts. Antioxidant release was higher in the in vitro gastric digested extracts, but digestion conditions did not only affect quantity but quality, resulting in differences in antioxidant capacity and highlighting the importance of simulating physiological-like extraction conditions for assessing fruit antioxidant properties on human health. These results give new insights into the use of strawberry achenes as a source of bioactive compounds to be considered in strawberry breeding programs for improving human health. PMID:27409612
Lemos, M. Adília; Sárniková, Katarína; Bot, Francesca; Anese, Monica; Hungerford, Graham
The study of compounds that exhibit antioxidant activity has recently received much interest in the food industry because of their potential health benefits. Most of these compounds are plant based, such as polyphenolics and carotenoids, and there is a need to monitor them from the field through processing and into the body. Ideally, a monitoring technique should be non-invasive with the potential for remote capabilities. The application of the phenomenon of fluorescence has proved to be well suited, as many plant associated compounds exhibit fluorescence. The photophysical behaviour of fluorescent molecules is also highly dependent on their microenvironment, making them suitable probes to monitor changes in pH, viscosity and polarity, for example. Time-resolved fluorescence techniques have recently come to the fore, as they offer the ability to obtain more information, coupled with the fact that the fluorescence lifetime is an absolute measure, while steady state just provides relative and average information. In this work, we will present illustrative time-resolved measurements, rather than a comprehensive review, to show the potential of time-resolved fluorescence applied to the study of bioactive substances. The aim is to help assess if any changes occur in their form, going from extraction via storage and cooking to the interaction with serum albumin, a principal blood transport protein. PMID:26132136
Donno, Dario; Mellano, Maria Gabriella; Cerutti, Alessandro Kim; Beccaro, Gabriele Loris
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
Lee, Eun-Jung; Paek, Kee-Yoeup
Ammonium to nitrate ratios of 0:30, 5:25, 10:20, 15:15, 20:10, 25:5, and 30:0 mM were tested to determine the optimal NH(4)(+) :NO(3)(-) ratio for improving biomass and bioactive compound production in Eleutherococcus koreanum Nakai adventitious roots using 3-L bulb-type bubble bioreactors. A high ammonium nitrogen ratio had a negative effect on root growth, and the highest fresh and dry weights were obtained when NH(4)(+):NO(3)(-) ratios were 5:25 and 10:20 (mM) after 5 weeks of culture. Although the total production of eleutherosides B and E was slightly higher at the 10:20 ratio than at the 5:25 ratio (NH(4)(+):NO(3)(-)), we proposed that the optimal NH(4)(+):NO(3)(-) ratio was 5:25 mM. This ratio achieved both the highest total production of five target bioactive compounds (eleutherosides B and E, chlorogenic acid, total phenolics, and flavonoids) and the highest root biomass. Furthermore, increasing NH(4)(+):NO(3)(-) ratios to 10:20 decreased pH in the medium, interrupted the absorption of essential minerals from the culture medium, and resulted in low biomass and increased relative oxidative stress levels, which were evaluated by determining 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity. Therefore, nitrate rather than ammonium nitrogen was more essential not for only biomass production but also for bioactive compound production in E. koreanum adventitious root cultures. The optimal nitrogen source ratio produced 5.63 g L(-1) of biomass and 24.41 mg of the five total bioactive compounds per gram of biomass (dry weight basis). The development of such in vitro culture technology will benefit the pilot-scale production of E. koreanum-based bioactive compounds for commercialization.
Calín-Sánchez, Angel; Martínez-Nicolás, Juan José; Munera-Picazo, Sandra; Carbonell-Barrachina, Angel A; Legua, Pilar; Hernández, Francisca
The objective of this study was to evaluate and compare, for the first time, white and black mulberry species in terms of main phytochemical, volatile composition and sensory profile characteristics in eight Spanish clones. The results showed that black and white mulberry species displayed significant different characteristics. PLS analysis has allowed grouping of the clones into four groups (i) MA1, MA2 and MN2, (ii) MN3 and MN4, (iii) MA3 and MA4, and (iv) MN1. Experimental results proved that Spanish mulberries have potential for fresh consumption due to their high antioxidant capacity (10.7-86.1 mg Trolox 100 g(-1)), polyphenol (76.7-180 mg gallic acid 100 g(-1)) and ellagic acid content (8.7-15.5 mg 100 g(-1)) as well as considerable amount of volatile compounds (35) with desirable attributes, which were scored high by a trained panel. Cultivars from the Morus nigra species seem to provide fruits with higher content of bioactive compounds and better aptitude for fresh consumption than Morus alba. Differences among the species should be attributed to genetics because they were cultivated under same conditions.
Murador, Daniella Carisa; Mercadante, Adriana Zerlotti; de Rosso, Veridiana Vera
The aim of this study is to investigate the effects of different home cooking techniques (boiling, steaming, and stir-frying) in kale and red cabbage, on the levels of bioactive compounds (carotenoids, anthocyanins and phenolic compounds) determined by high-performance liquid chromatography coupled with photodiode array and mass spectrometry detectors (HPLC-DAD-MS(n)), and on the antioxidant activity evaluated by ABTS, ORAC and cellular antioxidant activity (CAA) assays. The steaming technique resulted in a significant increase in phenolic content in kale (86.1%; p<0.001) whereas in red cabbage it was significantly reduced (34.6%; p<0.001). In the kale, steaming resulted in significant increases in antioxidant activity levels in all of the evaluation methods. In the red cabbage, boiling resulted in a significant increase in antioxidant activity using the ABTS assay but resulted in a significant decrease using the ORAC assay. According to the CAA assay, the stir-fried sample displayed the highest levels of antioxidant activity.
Santangelo, Carmela; Zicari, Alessandra; Mandosi, Elisabetta; Scazzocchio, Beatrice; Mari, Emanuela; Morano, Susanna; Masella, Roberta
Gestational diabetes mellitus (GDM) is a serious problem growing worldwide that needs to be addressed with urgency in consideration of the resulting severe complications for both mother and fetus. Growing evidence indicates that a healthy diet rich in fruit, vegetables, nuts, extra-virgin olive oil and fish has beneficial effects in both the prevention and management of several human diseases and metabolic disorders. In this review, we discuss the latest data concerning the effects of dietary bioactive compounds such as polyphenols and PUFA on the molecular mechanisms regulating glucose homoeostasis. Several studies, mostly based on in vitro and animal models, indicate that dietary polyphenols, mainly flavonoids, positively modulate the insulin signalling pathway by attenuating hyperglycaemia and insulin resistance, reducing inflammatory adipokines, and modifying microRNA (miRNA) profiles. Very few data about the influence of dietary exposure on GDM outcomes are available, although this approach deserves careful consideration. Further investigation, which includes exploring the 'omics' world, is needed to better understand the complex interaction between dietary compounds and GDM.
Papadopoulou, Athena A; Katsoura, Maria H; Chatzikonstantinou, Alexandra; Kyriakou, Eleni; Polydera, Angeliki C; Tzakos, Andreas G; Stamatis, Haralambos
The lipase-catalyzed molecular hybridization of α-lipoic acid (LA) with bioactive compounds pyridoxine, tyrosol and tyramine was performed in ionic solvents and deep eutectic solvents. The biocatalytic reactions were catalyzed by Candida antarctica lipase B immobilized onto various functionalized multi-walled carbon nanotubes (f-CNTs-CaLB), as well as by commercial Novozym 435. The use of f-CNTs-CaLB leads, in most cases, to higher conversion yields as compared to Novozym 435. The nature and ion composition of ionic solvents affect the performance of the biocatalytic process. The highest conversion yield was observed in (mtoa)NTf2. The high enzyme stability and the relatively low solubility of substrates in specific media account for the improved biocatalytic synthesis of molecular hybrids of LA. Principal component analysis was used to screen for potential lipoxygenase inhibitors. In vitro studies showed that the synthesized compounds exhibit up to 10-fold increased inhibitory activity on lipoxygenase mediated lipid peroxidation as compared to parent molecules.
Petropoulos, Spyridon A; Levizou, Efi; Ntatsi, Georgia; Fernandes, Ângela; Petrotos, Konstantinos; Akoumianakis, Konstantinos; Barros, Lillian; Ferreira, Isabel C F R
Soil salinization is an increasing problem for many areas throughout the world that renders prohibitive vegetables and crop production in general. In the present study, Cichorium spinosum L. plants were grown under saline conditions in order to evaluate chemical composition and bioactive compounds content of their leaves. Salinity increase resulted in significant changes of macro and micro-nutrients content (nutritional value, sugars, fatty acids, minerals, ascorbic acid and tocopherols), whereas the concentration of phenolic compounds was not significantly affected. Chicoric and 5-O-caffeoylquinic acid were the most abundant phenolic acids. In contrast, antioxidant activity and mineral composition were beneficially affected by mid-to-high and high salinity levels. In conclusion, C. spinosum can be cultivated under saline conditions without compromising the quality of the final product, especially in semi-arid areas where irrigation water is scarce and/or of low quality due to high content of NaCl (coastal areas or areas where underground water is saline).
Reversible covalent bond formation under thermodynamic control adds reactivity to self-assembled supramolecular systems, and is therefore an ideal tool to assess complexity of chemical and biological systems. Dynamic combinatorial/covalent chemistry (DCC) has been used to read structural information by selectively assembling receptors with the optimum molecular fit around a given template from a mixture of reversibly reacting building blocks. This technique allows access to efficient sensing devices and the generation of new biomolecules, such as small molecule receptor binders for drug discovery, but also larger biomimetic polymers and macromolecules with particular three-dimensional structural architectures. Adding a kinetic factor to a thermodynamically controlled equilibrium results in dynamic resolution and in self-sorting and self-replicating systems, all of which are of major importance in biological systems. Furthermore, the temporary modification of bioactive compounds by reversible combinatorial/covalent derivatisation allows control of their release and facilitates their transport across amphiphilic self-assembled systems such as artificial membranes or cell walls. The goal of this review is to give a conceptual overview of how the impact of DCC on supramolecular assemblies at different levels can allow us to understand, predict and modulate the complexity of biological systems.
Linthorne, Jamie S; Chang, Barbara J; Flematti, Gavin R; Ghisalberti, Emilio L; Sutton, David C
A promising new strategy in antibacterial research is inhibition of the bacterial communication system termed quorum sensing. In this study, a novel and rapid pre-screening method was developed to detect the production of chemical inhibitors of this system (quorum-quenching compounds) by bacteria isolated from marine and estuarine waters. This method involves direct screening of mixed populations on an agar plate, facilitating specific isolation of bioactive colonies. The assay showed that between 4 and 46 % of culturable bacteria from various samples were bioactive, and of the 95 selectively isolated bacteria, 93.7 % inhibited Vibrio harveyi bioluminescence without inhibiting growth, indicating potential production of quorum-quenching compounds. Of the active isolates, 21 % showed further activity against quorum-sensing-regulated pigment production by Serratia marcescens. The majority of bioactive isolates were identified by 16S ribosomal DNA (rDNA) amplification and sequencing as belonging to the genera Vibrio and Pseudoalteromonas. Extracts of two strongly bioactive Pseudoalteromonas isolates (K1 and B2) were quantitatively assessed for inhibition of growth and quorum-sensing-regulated processes in V. harveyi, S. marcescens and Chromobacterium violaceum. Extracts of the isolates reduced V. harveyi bioluminescence by as much as 98 % and C. violaceum pigment production by 36 % at concentrations which had no adverse effect on growth. The activity found in the extracts indicated that the isolates may produce quorum-quenching compounds. This study further supports the suggestion that quorum quenching may be a common attribute among culturable planktonic marine and estuarine bacteria.
Pusnik, Mascha; Imeri, Minire; Deppierraz, Grégoire; Bruinink, Arie; Zinn, Manfred
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
Rahaiee, Somayeh; Moini, Sohrab; Hashemi, Maryam; Shojaosadati, Seyed Abbas
Saffron (Crocus sativus L. stigma), the most valuable medicinal food product, belongs to the Iridaceae family which has been widely used as a coloring and flavoring agent. These properties are basically related to its crocins, picrocrocin and safranal contents which have all demonstrated health promoting properties. The present review article highlights the phytochemical constituents (phenolic and flavonoid compounds, degraded carotenoid compounds crocins and crocetin) that are important in antioxidant activity of saffron extracts. However, the synergistic effect of all the bioactive components presence in saffron gave a significant antioxidant activity similar to vegetables rich in carotenoids. Our study provides an updated overview focused on the antioxidant activity of saffron related to its bioactive compounds to design the different functional products in food, medicine and cosmetic industries.
Recently, there has been a great deal of remarkable interest in finding bioactive compounds from nutritional foods to replace synthetic compounds. In particular, ortho-dihydroxyisoflavones and glycitein are of growing scientific interest owing to their attractive biological properties. In this study, 7,8-ortho-dihydroxyisoflavone, 6,7-ortho-dihydroxyisoflavone, 3',4'-ortho-dihydroxyisoflavone and 7,4'-dihydroxy-6-methoxyisoflavone were characterized using microorganism screened from soybean Doenjang. Three ortho-dihydroxyisoflavones and glycitein were structurally elucidated by 1H-NMR and GC-MS analysis. Furthermore, bacterial strains from soybean Doenjang with the capacity of biotransformation were screened. The bacterial strain, identified as Bacillus subtilis Roh-1, was shown to convert daidzein into ortho-dihydroxyisoflavones and glycitein. Thus, this study has, for the first time, demonstrated that a bacterial strain had a substrate specificity for multiple modifications of the bioactive compounds.
Peñas, Elena; Frias, Juana; Martínez-Villaluenga, Cristina; Vidal-Valverde, Concepción
The influence of two Spanish growing locations with well-differentiated climatic conditions (northern and eastern areas) on the main bioactive compounds, glucosinolates (GLS), total phenolic compounds (TPC), and vitamin C, as well as myrosinase activity and antioxidant capacity in five white cabbage ( Brassica oleracea L. var. capitata) cultivars was investigated. Cabbages with the highest concentration of total GLS presented the highest vitamin C level (r = 0.75, P ≤ 0.05) and the lowest antioxidant capacity (r = -0.76, P ≤ 0.05). The cultivars with the highest vitamin C content had the lowest myrosinase activity (r = -0.89, P ≤ 0.05) and antioxidant capacity (r = -0.86, P ≤ 0.05), whereas those with the largest TPC amount showed the highest antioxidant capacity (r = 0.71, P ≤ 0.05). Cabbage cultivars grown in the northern area of Spain with low temperatures and radiation led to higher mean values of myrosinase activity (29.25 U/g dm), TPC (10.0 GAE mg/g dm), and antioxidant capacity (81.6 μmol Trolox/g dm), whereas cultivars grown in the eastern area with high temperature and radiation led to larger mean values of GLS (14.3 μmol/g dm) and vitamin C (5.3 mg/g dm). The results of this investigation provide information regarding the most suitable Spanish growing location to produce white cabbage with an optimized content of health-promoting compounds.
Duval, Johanna; Destandau, Emilie; Pecher, Virginie; Poujol, Marion; Tranchant, Jean-François; Lesellier, Eric
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
Rocha, Joana; Peixe, Luisa; Gomes, Newton C M; Calado, Ricardo
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.
Tan, Xiao-jie; Li, Qing; Chen, Xiao-hui; Wang, Zhi-wei; Shi, Zheng-yuan; Bi, Kai-shun; Jia, Ying
Herba Artemisiae Scopariae is a Chinese herbal medicine widely used for the remedy of liver diseases. A high performance liquid chromatography method coupled with diode array detection was developed to simultaneously determine 13 different bioactive compounds in Herba Artemisiae Scopariae (Yin Chen) including chlorogenic acid (1), 6,7-dihydroxycoumarin (2), caffeic acid (3), 4-hydroxyacetophenone (4), scopoletin (5), rutin (6), hyperoside (7), isoquercitrin (8), scoparone (11), 7-methoxycoumarine (12) and quercetin (13). By using four different wavelengths in the HPLC analysis, the developed method was able to determine the bioactive compounds with excellent resolution, precision and recovery. The method was applied to determine the amounts of the bioactive compounds in nine samples from different cultivated regions and harvest seasons in China, and significant variations were revealed. Chlorogenic acid was the most abundant among the analyzed compounds. The samples harvested in the spring contained higher contents of chlorogenic acid than those collected in other seasons. Other phenolic acids as caffeic acid, 3,5-dicaffeoylquinic acid, 4,5-dicaffeoylquinic acid and 4-hydroxyacetophenone accumulated at much higher amounts in about May to July. The samples analyzed contained a much lower level of the amount of other flavonoids and coumarins as rutin, hyperoside, isoquercitrin and scoparone.
Pandey, Renu; Mahar, Rohit; Hasanain, Mohammad; Shukla, Sanjeev K; Sarkar, Jayanta; Rameshkumar, K B; Kumar, Brijesh
Efficient and sensitive LC-MS/MS methods have been developed for the rapid screening and determination of bioactive compounds in different fruit parts of four Myristica species, viz., Myristica beddomeii, Myristica fragrans, Myristica fatua and Myristica malabarica. Twenty-one compounds were identified and characterized on the basis of their accurate mass and MS/MS fragmentation pattern using HPLC-QTOF-MS/MS and NMR analysis. Quantitative determination of five major bioactive compounds was performed using multiple-reaction monitoring mode with continuous polarity switching by UHPLC-QqQLIT-MS/MS. Moreover, in vitro antiproliferative activity of these Myristica species was evaluated against five human cancer cell lines A549, DLD-1, DU145, FaDu and MCF-7 using SRB assay. Seventeen phytoconstituents were identified and reported for the first time from M. beddomeii and sixteen from M. fatua. Quantification result showed highest total content of five major bioactive compounds in mace of M. fragrans. Evaluation of in vitro antiproliferative activity revealed potent activity in all investigated species except M. fragrans.
Jacobi, Jennifer L; Yang, Bo; Li, Xu; Menze, Anna K; Laurentz, Sara M; Janle, Elsa M; Ferruzzi, Mario G; McCabe, George P; Chapple, Clint; Kirchmaier, Ann L
The plant secondary metabolite and common food additive dihydrocoumarin (DHC) is an inhibitor of the Sirtuin family of NAD+-dependent deacetylases. Sirtuins are key regulators of epigenetic processes that maintain silent chromatin in yeast and have been linked to gene expression, metabolism, apoptosis, tumorogenesis and age-related processes in multiple organisms, including humans. Here we report that exposure to the polyphenol DHC led to defects in several Sirtuin-regulated processes in budding yeast including the establishment and maintenance of Sir2p-dependent silencing by causing disassembly of silent chromatin, Hst1p-dependent repression of meiotic-specific genes during the mitotic cell cycle. As both transient and prolonged exposure to environmental and dietary factors have the potential to lead to heritable alterations in epigenetic states and to modulate additional Sirtuin-dependent phenotypes, we examined the bioavailability and digestive stability of DHC using an in vivo rat model and in vitro digestive simulator. Our analyses revealed that DHC was unstable during digestion and could be converted to melilotic acid (MA), which also caused epigenetic defects, albeit less efficiently. Upon ingestion, DHC was observed primarily in intestinal tissues, but did not accumulate over time and was readily cleared from the animals. MA displayed a wider tissue distribution and, in contrast to DHC, was also detected in the blood plasma, interstitial fluid, and urine, implying that the conversion of DHC to the less bioactive compound, MA, occurred efficiently in vivo.
Wang, Yuefei; Ying, Le; Sun, Da; Zhang, Shikang; Zhu, Yuejin; Xu, Ping
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
Tomšik, Alena; Pavlić, Branimir; Vladić, Jelena; Ramić, Milica; Brindza, Ján; Vidović, Senka
Ultrasound-assisted extraction was used for extraction of bioactive compounds and for production of Allium ursinum liquid extract. The experiments were carried out according to tree level, four variables, face-centered cubic experimental design (FDC) combined with response surface methodology (RSM). Temperature (from 40 to 80 °C), ethanol concentration (from 30% to 70%), extraction time (from 40 to 80 min) and ultrasonic power (from 19.2 to 38.4 W/L) were investigated as independent variables in order to obtain the optimal conditions for extraction and to maximize the yield of total phenols (TP), flavonoids (TF) and antioxidant activity of obtained extracts. Experimental results were fitted to the second order polynomial model where multiple regression and analysis of variance were used to determine the fitness of the model and optimal condition for investigated responses. The predicted values of the TP (1.60 g GAE/100 g DW), TF (0.35 g CE/100 g DW), antioxidant activity, IC50 (0.71 mg/ml) and EY (38.1%) were determined at the optimal conditions for ultrasound assisted extraction: 80 °C temperature, 70% ethanol, 79.8 min and 20.06 W/L ultrasonic power. The predicted results matched well with the experimental results obtained using optimal extraction conditions which validated the RSM model with a good correlation.
Wan, Tien-Chun; Cheng, Fu-Yuan; Liu, Yu-Tse; Lin, Liang-Chuan; Sakata, Ryoichi
The purpose of the study was to investigate bioactive compounds of in vitro cultured Calculus Suis and natural Calculus Bovis obtained as valuable by-products from animals used for meat production. The results showed that the components of natural Calculus Bovis were rich in bilirubin and biliverdin and had higher content of essential amino acids. The major amino acids of in vitro cultured Calculus Suis were identified as glycine, alanine, glutamic acid and aspartic acid, and those for natural Calculus Bovis were found to be glutamic acid, aspartic acid, proline, and arginine. The methionine and cysteine contents of precursors for glutathione in natural Calculus Bovis were significantly higher than those of in vitro cultured Calculus Suis. The mineral contents of zinc, iron and manganese of natural Calculus Bovis were significantly higher than those of in vitro cultured Calculus Suis. The major bile acids in both products were cholic acid and dehydrocholic acid, respectively. The chenodeoxycholic and ursodeoxycholic acid content of in vitro cultured Calculus Suis was significantly higher than that of natural Calculus Bovis.
Juarez-Enriquez, Edmundo; Salmerón, Ivan; Gutierrez-Mendez, Nestor; Ortega-Rivas, Enrique
Clarified and standardized apple juice was ultraviolet-irradiated to inactivate polyphenol oxidase enzyme and microbiota, and its effect on bioactive compounds and stability during storage was also evaluated. Apple juice was irradiated with 345.6 J/cm² and treatment effect was evaluated in terms of color, antioxidant capacity, polyphenol content, pH, titratable acidity and total soluble solids. Using a linear regression design, inactivation kinetic of polyphenol oxidase enzyme was also described. In addition, a repeated measures design was carried out to evaluate apple juice during 24 days of storage at 4 °C and 20 °C. After irradiation, reduction of antioxidant capacity was observed while during storage, ascorbic acid content decreased up to 40% and total polyphenol content remain stable. Ultraviolet irradiation achieved a complete inactivation of polyphenol oxidase enzyme and microbiota, keeping apple juice antioxidants during ultraviolet treatment and storage available until juice consumption. UV-treated apple juice can be used as a regular beverage, ensuring antioxidant intake.
Keser, Serhat; Celik, Sait; Turkoglu, Semra; Yilmaz, Ökkes; Turkoglu, Ismail
Aim: The antioxidant and pharmacological effects of hawthorn have mainly been attributed to the polyphenolic contents. The aim of this research is to determine some bioactive compounds and antioxidant properties of hawthorn aqueous and ethanol extracts of leaves, flowers, and ripened fruits. Materials and Methods: For this purpose, antioxidant activities of extracts were assessed on DPPH•, ABTS•+, superoxide scavenging, reducing power and ferrous metal chelating activity assays and phenolic content of extracts was determined by Folin—Cioacalteu’s reagent. Results: The flavonoids including rutin, apigenin, myricetin, quercetin, naringenin and kaempferol, were identified by high-performance liquid chromatography in the hawthorn extract. Conclusion: It was observed the aqueous and ethanol extracts of Crataegus monogyna subsp. monogyna fruits showed the highest activity in reducing power and metal chelating activity assays. In addition, it was determined that the aqueous flower extract showed higher flavonoid content than aqueous leaves extract. The antioxidant and pharmacological effects of hawthorn have mainly been attributed to the polyphenolic contents. PMID:26401347
Kalimuthu, Senthilkumar; Se-Kwon, Kim
Inhibition of apoptosis leads to activation of cell survival factors (e.g., AKT) causes continuous cell proliferation in cancer. Apoptosis, the major form of cellular suicide, is central to various physiological processes and the maintenance of homeostasis in multicellular organisms. A number of discoveries have clarified the molecular mechanism of apoptosis, thus clarifying the link between apoptosis and cell survival factors, which has a therapeutic outcome. Induction of apoptosis and inhibition of cell survival by anticancer agents has been shown to correlate with tumor response. Cellular damage induces growth arrest and tumor suppression by inducing apoptosis, necrosis and senescence; the mechanism of cell death depends on the magnitude of DNA damage following exposure to various anticancer agents. Apoptosis is mainly regulated by cell survival and proliferating signaling molecules. As a new therapeutic strategy, alternative types of cell death might be exploited to control and eradicate cancer cells. This review discusses the signaling of apoptosis and cell survival, as well as the potential contribution of marine bioactive compounds, suggesting that new therapeutic strategies might follow. PMID:23348928
Barbosa-Pereira, Letricia; Pocheville, Ainara; Angulo, Inmaculada; Paseiro-Losada, Perfecto; Cruz, Jose M.
The brewery industry generates waste that could be used to yield a natural extract containing bioactive phenolic compounds. We compared two methods of purifying the crude extract—solid-phase extraction (SPE) and supercritical fluid extraction (SFE)—with the aim of improving the quality of the final extract for potential use as safe food additive, functional food ingredient, or nutraceutical. The predominant fractions yielded by SPE were the most active, and the fraction eluted with 30% (v/v) of methanol displayed the highest antioxidant activity (0.20 g L−1), similar to that of BHA. The most active fraction yielded by SFE (EC50 of 0.23 g L−1) was obtained under the following conditions: temperature 40°C, pressure 140 bar, extraction time 30 minutes, ethanol (6%) as a modifier, and modifier flow 0.2 mL min−1. Finally, we found that SFE is the most suitable procedure for purifying the crude extracts and improves the organoleptic characteristics of the product: the final extract was odourless, did not contain solvent residues, and was not strongly coloured. Therefore, natural extracts obtained from the residual stream and purified by SFE can be used as natural antioxidants with potential applications in the food, cosmetic, and pharmaceutical industries. PMID:23762844
Kai, Hisahiro; Akamatsu, Ena; Torii, Eri; Kodama, Hiroko; Yukizaki, Chizuko; Akagi, Isao; Ino, Hisatoshi; Sakakibara, Yoichi; Suiko, Masahito; Yamamoto, Ikuo; Okayama, Akihiko; Morishita, Kazuhiro; Kataoka, Hiroaki; Matsuno, Koji
In our previous report, an 80% ethanol bitter gourd seed extract (BGSE) was found to suppress proliferation of adult T-cell leukemia (ATL) cell lines. The present study aimed to identify the bioactive compounds from BGSE specific against ATL. From the result of an HPLC-MS analysis, α-eleostearic acid (α-ESA) was present in BGSE at 0.68% ± 0.0022% (±SD, n = 5). In the cell proliferation test, α-ESA potently suppressed proliferation of two ATL cell lines (ED and Su9T01; IC50 = 8.9 and 29.3 µM, respectively) more than several other octadecanoic acids. However, α-ESA moderately inhibited phytohemagglutinin-activated human peripheral blood mononuclear cells (PBMC; IC50 = 31.0 µM). These results suggest that BGSE-derived α-ESA has potential as a functional food constituent because of its activity against ATL, particularly against ED cells. Moreover, α-ESA might be effective for the prevention of moderate adverse effects of ATL on normal T cells.
Ruiz-Gutiérrez, Martha G; Amaya-Guerra, Carlos A; Quintero-Ramos, Armando; Pérez-Carrillo, Esther; Ruiz-Anchondo, Teresita de J; Báez-González, Juan G; Meléndez-Pizarro, Carmen O
Red cactus pear has significant antioxidant activity and potential as a colorant in food, due to the presence of betalains. However, the betalains are highly thermolabile, and their application in thermal process, as extrusion cooking, should be evaluated. The aim of this study was to evaluate the effect of extrusion conditions on the chemical components of red cactus pear encapsulated powder. Cornstarch and encapsulated powder (2.5% w/w) were mixed and processed by extrusion at different barrel temperatures (80, 100, 120, 140 °C) and screw speeds (225, 275, 325 rpm) using a twin-screw extruder. Mean residence time (trm), color (L*, a*, b*), antioxidant activity, total polyphenol, betacyanin, and betaxanthin contents were determined on extrudates, and pigment degradation reaction rate constants (k) and activation energies (Ea) were calculated. Increases in barrel temperature and screw speed decreased the trm, and this was associated with better retentions of antioxidant activity, total polyphenol, betalain contents. The betacyanins k values ranged the -0.0188 to -0.0206/s and for betaxanthins ranged of -0.0122 to -0.0167/s, while Ea values were 1.5888 to 6.1815 kJ/mol, respectively. The bioactive compounds retention suggests that encapsulated powder can be used as pigments and to provide antioxidant properties to extruded products.
Uusitalo, Liisa; Salmenhaara, Maija; Isoniemi, Merja; Garcia-Alvarez, Alicia; Serra-Majem, Lluís; Ribas-Barba, Lourdes; Finglas, Paul; Plumb, Jenny; Tuominen, Pirkko; Savela, Kirsti
The purpose of this study was to estimate the intake of selected bioactive compounds from fennel-containing plant food supplements (PFS) among Finnish consumers. The estimated average intake of estragole was 0.20mg/d, of trans-anethole 1.15mg/d, of rosmarinic acid 0.09mg/d, of p-coumaric acid 0.0068mg/d, of kaempferol 0.0034mg/d, of luteolin 0.0525μg/d, of quercetin 0.0246mg/d, of matairesinol 0.0066μg/d and of lignans 0.0412μg/d. The intakes of kaempferol, quercetin, luteolin, matairesinol and lignans from PFS were low in comparison with their dietary supply. The intake of estragole was usually moderate, but a heavy consumption of PFS may lead to a high intake of estragole. The intake of trans-anethole did not exceed the acceptable daily intake, but PFS should be taken into account when assessing the total exposure. To our knowledge, this study provided the first intake estimates of trans-anethole, p-coumaric acid and rosmarinic acid in human populations.
Czerko, Zbigniew; Zarzyńska, Krystyna; Borowska-Komenda, Monika
We investigated the effect of cultivation system (conventional or organic), cooking method, and flesh color on the contents of ascorbic acid (AA) and total phenolics (TPs), and on total antioxidant activity (Trolox equivalents, TE) in Solanum tuberosum (potato) tubers. The research material, consisting of 4 potato cultivars, was grown in experimental fields, using organic and conventional systems, at the experimental station in 2012 and 2013. The analysis showed that organically grown potatoes with creamy, light yellow, and yellow flesh had significantly higher TPs than did potatoes grown conventionally. Flesh color and cooking method also affected AA. The greatest losses of AA occurred in yellow-fleshed potatoes grown conventionally and cooked in the microwave; such losses were not observed in potatoes grown organically. A dry cooking method (baking in a microwave) increased the TP contents in potatoes by about 30%, regardless of the flesh color and the production system. TE was significantly higher in organically grown potatoes (raw and cooked in a steamer) than in conventionally grown potatoes. TE and AA contents showed a significant positive correlation, but only in potatoes from the organic system [R2 = 0.686]. By contrast, the positive correlation between TE and TPs was observed regardless of the production system. Therefore, we have identified the effects of farming system, cooking method, and flesh color on the contents of bioactive compounds in potato tubers. PMID:27139188
Hardoim, Cristiane C. P.; Costa, Rodrigo
Marine sponges harbour complex microbial communities of ecological and biotechnological importance. Here, we propose the application of the widespread sponge family Irciniidae as an appropriate model in microbiology and biochemistry research. Half a gram of one Irciniidae specimen hosts hundreds of bacterial species—the vast majority of which are difficult to cultivate—and dozens of fungal and archaeal species. The structure of these symbiont assemblages is shaped by the sponge host and is highly stable over space and time. Two types of quorum-sensing molecules have been detected in these animals, hinting at microbe-microbe and host-microbe signalling being important processes governing the dynamics of the Irciniidae holobiont. Irciniids are vulnerable to disease outbreaks, and concerns have emerged about their conservation in a changing climate. They are nevertheless amenable to mariculture and laboratory maintenance, being attractive targets for metabolite harvesting and experimental biology endeavours. Several bioactive terpenoids and polyketides have been retrieved from Irciniidae sponges, but the actual producer (host or symbiont) of these compounds has rarely been clarified. To tackle this, and further pertinent questions concerning the functioning, resilience and physiology of these organisms, truly multi-layered approaches integrating cutting-edge microbiology, biochemistry, genetics and zoology research are needed. PMID:25272328
Jacobi, Jennifer L.; Yang, Bo; Li, Xu; Menze, Anna K.; Laurentz, Sara M.; Janle, Elsa M.; Ferruzzi, Mario G.; McCabe, George P.; Chapple, Clint; Kirchmaier, Ann L.
The plant secondary metabolite and common food additive dihydrocoumarin (DHC) is an inhibitor of the Sirtuin family of NAD+-dependent deacetylases. Sirtuins are key regulators of epigenetic processes that maintain silent chromatin in yeast and have been linked to gene expression, metabolism, apoptosis, tumorogenesis and age-related processes in multiple organisms, including humans. Here we report that exposure to the polyphenol DHC led to defects in several Sirtuin-regulated processes in budding yeast including the establishment and maintenance of Sir2p-dependent silencing by causing disassembly of silent chromatin, Hst1p-dependent repression of meiotic-specific genes during the mitotic cell cycle. As both transient and prolonged exposure to environmental and dietary factors have the potential to lead to heritable alterations in epigenetic states and to modulate additional Sirtuin-dependent phenotypes, we examined the bioavailability and digestive stability of DHC using an in vivo rat model and in vitro digestive simulator. Our analyses revealed that DHC was unstable during digestion and could be converted to melilotic acid (MA), which also caused epigenetic defects, albeit less efficiently. Upon ingestion, DHC was observed primarily in intestinal tissues, but did not accumulate over time and was readily cleared from the animals. MA displayed a wider tissue distribution and, in contrast to DHC, was also detected in the blood plasma, interstitial fluid, and urine, implying that the conversion of DHC to the less bioactive compound, MA, occurred efficiently in vivo. PMID:26882112
Juarez-Enriquez, Edmundo; Salmerón, Ivan; Gutierrez-Mendez, Nestor; Ortega-Rivas, Enrique
Clarified and standardized apple juice was ultraviolet-irradiated to inactivate polyphenol oxidase enzyme and microbiota, and its effect on bioactive compounds and stability during storage was also evaluated. Apple juice was irradiated with 345.6 J/cm2 and treatment effect was evaluated in terms of color, antioxidant capacity, polyphenol content, pH, titratable acidity and total soluble solids. Using a linear regression design, inactivation kinetic of polyphenol oxidase enzyme was also described. In addition, a repeated measures design was carried out to evaluate apple juice during 24 days of storage at 4 °C and 20 °C. After irradiation, reduction of antioxidant capacity was observed while during storage, ascorbic acid content decreased up to 40% and total polyphenol content remain stable. Ultraviolet irradiation achieved a complete inactivation of polyphenol oxidase enzyme and microbiota, keeping apple juice antioxidants during ultraviolet treatment and storage available until juice consumption. UV-treated apple juice can be used as a regular beverage, ensuring antioxidant intake. PMID:28231106
López de Felipe, Félix; de Las Rivas, Blanca; Muñoz, Rosario
The microorganisms in the human gastrointestinal tract have a profound influence on the transformation of food into metabolites which can impact human health. Gallic acid (GA) and pyrogallol (PG) are bioactive compounds displaying diverse biological properties, including carcinogenic inhibiting activities. However, its concentration in fruits and vegetables is generally low. These metabolites can be also generated as final products of tannin metabolism by microbes endowed with tannase, which opens up the possibility of their anti-cancer potential being increased. Patients with colorectal cancer (CRC) display an imbalanced gut microbiota respect to healthy population. The recent use of next generation sequencing technologies has greatly improved knowledge of the identity of bacterial species that colonize non-tumorous and tumorous tissues of CRC patients. This information provides a unique opportunity to shed light on the role played by gut microorganisms in the different stages of this disease. We here review the recently published gut microbiome associated to CRC patients and highlight tannase as an underlying gene function of bacterial species that selectively colonize tumorous tissues, but not adjacent non-malignant tissues. Given the anti-carcinogenic roles of GA and PG produced by gut tannin-degrading bacteria, we provide an overview of the possible consequences of this intriguing coincidence for CRC development.
de Moraes Filho, Marsilvio Lima; Hirozawa, Sabrina Satie; Prudencio, Sandra Helena; Ida, Elza Iouko; Garcia, Sandra
This study aimed to evaluate the antioxidant properties, bioactive compounds and other physico-chemical parameters from black soybean and its derivatives over 30 days under refrigeration at 4 °C and develop a probiotic petit suisse produced from black soybean. The soymilk showed the highest levels of isoflavones (109 mg/100 g), total phenolics (600 mg/100 g) and total anthocyanins (388 mg/100 g) with the highest response in the tests with DPPH• and ABTS+• on a dry basis. There was a significant increase (p ≤ 0.05) in antioxidant activity during storage due to the hydrolysis of isoflavone glycosides to aglycones in soymilk sample, having a strong linear correlation between the concentration of isoflavone aglycones and the antioxidant activity for ABTS+• (R = 0.9437, 0.9624 and 0.9992) and DPPH• (R = 0.9865, 0.9978 and 0.9911), respectively, for soymilk, quark and petit suisse. The conversion of isoflavone was influenced directly by the characteristics of each sample, inhibiting or promoting the action of the enzyme. The petit suisse developed is an alternative for consumers, providing isoflavones and anthocyanins, possessing probiotic average counts (10⁸ CFU g⁻¹) during storage.
Fallico, Biagio; Ballistreri, Gabriele; Arena, Elena; Brighina, Selina; Rapisarda, Paolo
Both the composition and the intake of antioxidants (anthocyanins, ascorbic acid and hydroxycinnamic acids) were reported for all blood oranges including the single cultivars (Moro, Tarocco and Sanguinello) and industrially produced juices. The mean values of the studied bioactive compounds in the edible part oranges were: 9.6mg/100g of orange edible part for the anthocyanins; 8.1, 0.7, 1.3, 3.8, 2.5mg/100g for total hydroxycinnamic acids, caffeic, sinapic, ferulic and coumaric acids, respectively and 59.1mg/100g for ascorbic acid. The consumption of blood oranges contributes to a daily intake of: 9.4mg/d (up to 55mg/d) of anthocyanins and 58.5mg/d (up to 340mg/d) of vitamin C, respectively. Data suggest that the 50% of consumers, males and females, receive more than the 70% and 90% of EAR value of vitamin C, respectively. The 25% of males and the 40% of females has an intake higher than the EAR.
Baraya, Yusha U Shu Aibu; Wong, Kah Keng; Yaacob, Nik Soriani
Breast cancer has continued to cause high cancer death rates among women worldwide. The use of plants' natural products in breast cancer treatment has received more attention in recent years due to their potentially wider safety margin and the potential to complement conventional chemotherapeutic drugs. Plant-based products have demonstrated anticancer potential through different biological pathways including modulation of the immune system. Immunomodulatory properties of medicinal plants have been shown to mitigate breast cancer cell growth. Different immune cell types participate in this process especially cytotoxic T cells and natural killer cells, and cytokines including chemokines and tumor necrosis factor-α. Medicinal plants such as Glycyrrhiza glabra, Uncaria tomentosa, Camellia sinensis, Panax ginseng, Prunus armenaica (apricot), Allium sativum, Arctium lappa and Curcuma longa were reported to hold strong potential in breast cancer treatment in various parts of the world. Interestingly, research findings have shown that these plants possess bioactive immunomodulators as their main constituents producing the anticancer effects. These immunomodulatory compounds include ajoene, arctigenin, β-carotene, curcumin, epigallocatechin-3-gallate, ginsan, glabridin and quinic acid. In this review, we discussed the ability of these eight immunomodulators in regulating the immune system potentially applicable in breast cancer treatment via anti-inflammatory (curcumin, arctigenin, glabridin and ajoene) and lymphocytes activation (β-carotene, epigallocatechin-3-gallate, quinic acid and ginsan) properties, as well as future research direction in their use for breast cancer treatment.
Prado-Prado, Francisco; Garcia-Mera, Xerardo; Rodriguez-Borges, Jose Enrique; Concu, Riccardo; Perez-Montoto, Lazaro Guillermo; Gonzalez-Diaz, Humberto; Duardo-Sanchez, Aliuska
In recent times, there has been an increased use of Computer-Aided Drug Discovery (CADD) techniques in Medicinal Chemistry as auxiliary tools in drug discovery. Whilst the ultimate goal of Medicinal Chemistry research is for the discovery of new drug candidates, a secondary yet important outcome that results is in the creation of new computational tools. This process is often accompanied by a lack of understanding of the legal aspects related to software and model use, that is, the copyright protection of new medicinal chemistry software and software-mediated discovered products. In the center of picture, which lies in the frontiers of legal, chemistry, and biosciences, we found computational modeling-based drug discovery patents. This article aims to review prominent cases of patents of bio-active organic compounds that involved/protect also computational techniques. We put special emphasis on patents based on Quantitative Structure-Activity Relationships (QSAR) models but we include other techniques too. An overview of relevant international issues on drug patenting is also presented.
Jiang, Bo; Mantri, Nitin; Hu, Ya; Lu, Jiayin; Jiang, Wu; Lu, Hongfei
The effect of different sterilization methods (thermal, microwave, and ultrasonic processing) on the main bioactive compounds and antioxidant activity of black mulberry juice during selected storage time (8 days) and temperatures (5, 15, and 25 ℃) was investigated. The antioxidant activity of thermal-treated juice depleted with storage time, whilst both ultrasound- and microwave-treated juices showed transient increase in antioxidant activity during the first 2 days that later decreased with storage time. Lower temperature storage preserved more bioactive compounds and antioxidant activity, especially in ultrasound sterilized samples. The activation energy values were 15.99, 13.07, and 12.81 kJ/mol for ultrasonic, microwave, and thermal pasteurization processes, respectively. In general, ultrasound-sterilized samples showed higher total phenolics, anthocyanin, and antioxidant activity compared to the microwave- and thermal-processed juice during the storage time especially at lower temperatures.
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...
Kim, Sun Hyo; Heo, Kang Nyung
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
Meighani, Hossein; Ghasemnezhad, Mahmood; Bakhshi, Davood
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.
Sun, Hanwen; Ge, Xusheng; Lv, Yunkai; Wang, Anbang
Accelerated solvent extraction (ASE) has become a popular green extraction technology for different classes of organic contaminants present in numerous kinds of food and feed for food safety. The parameters affecting ASE efficiency and application advancement of ASE in the analysis of organic contaminants, natural toxins compounds as well as bioactive and nutritional compounds in animal origin food, plant origin food and animal feed are reviewed in detail. ASE is a fully automated and reliable extraction technique with many advantages over traditional extraction techniques, so it could be especially useful for routine analyses of pollutants in food and feed.
Kellogg, Joshua J.; Todd, Daniel A.; Egan, Joseph M.; Raja, Huzefa A.; Oberlies, Nicholas H.; Kvalheim, Olav M.; Cech, Nadja B.
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 towards 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 datasets (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. PMID:26841051
Kou, Xiaohong; Wu, Ji Yun; Wang, Yong; Chen, Qiong; Xue, Zhaohui; Bai, Yang; Zhou, Fengjuan
Hypobaric treatment is becoming a potential technology to protect fruits from postharvest decay. The objective of this study was to investigate the effects of hypobaric treatments on storage quality, bioactive compounds, and antioxidant activity of tomato fruit. In this study, green tomatoes (cv. "Fen guan") were treated with hypobaric pressures (0.04 and 0.07 MPa) at ambient temperature (20 ℃) for 28 d. The results showed that under hypobaric storage, the respiration rates significantly declined and the respiratory peaks postponed 12 and 8 d by 0.04 and 0.07 MPa treatments, respectively, compared to control. Total soluble solid, titratable acidity, ascorbic acid, and lycopene were retained by hypobaric treatment. Moreover, ascorbic acid contents treated with 0.04 and 0.07 MPa were, respectively, 37% and 26% higher than control at day 24 and the contents of total polyphenols were, respectively, 1.28 and 1.11 times higher than control. Production and accumulation of toxic substances were significantly restrained. The ethanol content decreased, respectively, by 53% and 84% than control. At later storage period, the superoxide dismutase activity in treated fruits was about 0.58 U/(g·FW·min), whereas only 0.29 U/(g·FW·min) in control. Hypobaric treatment not only maintained a high activity of superoxide dismutase and peroxidase (POD), but also improved antioxidant capacity. All the results indicated that hypobaric treatment was a potential helpful method to protect the quality and nutrition of tomato and prolong ripening of tomato. Furthermore, the effect of 0.04 MPa hypobaric treatment was found better than 0.07 MPa.
Okada, Mio; Imai, Toshio; Yaegaki, Ken; Ishkitiev, Nikolay; Tanaka, Tomoko
Transplantation of insulin (INS)-secreting cells differentiated in vitro from stem cells promises a safer and easier treatment of severe diabetes mellitus. A volatile bioactive compound, hydrogen sulfide (H2S), promotes cell differentiation; human tooth-pulp stem cells undergo hepatic differentiation. The aim of this study is to develop a novel protocol using H2S to enhance pancreatic differentiation from the CD117(+) cell fraction of human tooth pulp. During the differentiation, the cells were exposed to 0.1 ng ml(-1) H2S. Immunocytochemistry, RT-PCR, determination of INS c-peptide content and flow cytometry of pancreatically related markers were carried out. Expression of WNT and the PI3K/AKT signaling pathway were also determined by PCR array. After differentiation, INS, glucagon (GCG), somatostatin (SST) and pancreatic polypeptide (PPY) were positive when examined by immunofluorescence. INS and GCG were also determined flow-cytometrically. Only the cells expressing INS increased after H2S exposure. The number of cells expressing GCG was significantly decreased. Genes involved in canonical WNT and the WNT/calcium pathways were highly expressed after H2S exposure. H2S accelerated INS synthesis and secretion by regenerated INS-producing cells from human teeth. All signaling pathway functions of the PI3K-AKT pathway were extremely activated by H2S exposure. The matured INS-producing cells originating in human teeth were increased by H2S in order to control blood-glucose level.
Ribeiro, L F; Ribani, R H; Francisco, T M G; Soares, A A; Pontarolo, R; Haminiuk, C W I
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.
Gómez-Mascaraque, Laura G; Sanchez, Gloria; López-Rubio, Amparo
The molecular weight of chitosan is one of its most determinant characteristics, which affects its processability and its performance as a biomaterial. However, information about the effect of this parameter on the formation of electrosprayed chitosan microcapsules is scarce. In this work, the impact of chitosan molecular weight on its electrosprayability was studied and correlated with its effect on the viscosity, surface tension and electrical conductivity of solutions. A Discriminant Function Analysis revealed that the morphology of the electrosprayed chitosan materials could be correctly predicted using these three parameters for almost 85% of the samples. The suitability of using electrosprayed chitosan capsules as carriers for bioactive agents was also assessed by loading them with a model active compound, (-)-epigallocatechin gallate (EGCG). This encapsulation, with an estimated efficiency of around 80% in terms of preserved antioxidant activity, showed the potential to prolong the antiviral activity of EGCG against murine norovirus via gradual bioactive release combined with its protection against degradation in simulated physiological conditions.
Shah, Salma Gul; Shier, W Thomas; Jamaluddin; Tahir, Nawaz; Hameed, Abdul; Ahmad, Safia; Ali, Naeem
A newly isolated fungus Penicillium verruculosum SG was evaluated for the production and characterization of bioactive colored secondary metabolites using solid-state fermentation along with their cytotoxic activities against normal and cancer cell lines. Logical fragmentation pattern following column chromatography, thin layer chromatography and liquid chromatography and mass spectrometry of crude culture filtrate of fungus revealed the presence of different polyketide pigments and other bioactive compounds. Cytotoxicity of the selected colored fractions of fungal filtrate containing different compounds revealed IC50 (μg/ml) values ranging from 5 to 100. It was significantly higher in case of orevactaene (5 + 0.44) and monascorubrine followed by pyripyropene (8 + 0.63) against cancer cell line KA3IT. Overall, these compounds considerably showed less toxicity toward normal cell lines NIH3T3, HSCT6, HEK293 and MDCK. XRD of a yellow crystalline compound (224.21 m/z) confirmed its 3-dimensional structure as phenazine 1 carboxylic acid (C13H8N2O2) (broad spectrum antibiotic), and it is first time reported in fungi.
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.
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
Zaimah Syed Jaapar, Syaripah; Azian Morad, Noor; Iwai, Yoshio
The solubilities in water of four main ginger bioactives, 6-gingerol, 6-shogaol, 8-gingerol and 10-gingerol, were predicted using a conductor-like screening model for real solvent (COSMO-RS) calculations. This study was conducted since no experimental data are available for ginger bioactive solubilities in hot water. The σ-profiles of these selected molecules were calculated using Gaussian software and the solubilities were calculated using the COSMO-RS method. The solubilities of these ginger bioactives were calculated at 50 to 200 °C. In order to validate the accuracy of the COSMO-RS method, the solubilities of five hydrocarbon molecules were calculated using the COSMO-RS method and compared with the experimental data in the literature. The selected hydrocarbon molecules were 3-pentanone, 1-hexanol, benzene, 3-methylphenol and 2-hydroxy-5-methylbenzaldehyde. The calculated results of the hydrocarbon molecules are in good agreement with the data in the literature. These results confirm that the solubilities of ginger bioactives can be predicted using the COSMO-RS method. The solubilities of the ginger bioactives are lower than 0.0001 at temperatures lower than 130 °C. At 130 to 200 °C, the solubilities increase dramatically with the highest being 6-shogaol, which is 0.00037 mole fraction, and the lowest is 10-gingerol, which is 0.000039 mole fraction at 200 °C.
Ghasemzadeh, Ali; Jaafar, Hawa Z. E.; Rahmat, Asmah; Devarajan, Thiyagu
In this study, we investigated some bioactive compounds and pharmaceutical qualities of curry leaf (Murraya koenigii L.) extracts from three different locations in Malaysia. The highest TF and total phenolic (TP) contents were observed in the extracts from Kelantan (3.771 and 14.371 mg/g DW), followed by Selangor (3.146 and 12.272 mg/g DW) and Johor (2.801 and 12.02 mg/g DW), respectively. High quercetin (0.350 mg/g DW), catechin (0.325 mg/g DW), epicatechin (0.678 mg/g DW), naringin (0.203 mg/g DW), and myricetin (0.703 mg/g DW) levels were observed in the extracts from Kelantan, while the highest rutin content (0.082 mg/g DW) was detected in the leaves from Selangor. The curry leaf extract from Kelantan exhibited higher concentration of gallic acid (0.933 mg/g DW) than that from Selangor (0.904 mg/g DW) and Johor (0.813 mg/g DW). Among the studied samples, the ones from Kelantan exhibited the highest radical scavenging activity (DPPH, 66.41%) and ferric reduction activity potential (FRAP, 644.25 μm of Fe(II)/g) followed by those from Selangor (60.237% and 598.37 μm of Fe(II)/g) and Johor (50.76% and 563.42 μm of Fe(II)/g), respectively. A preliminary screening showed that the curry leaf extracts from all the locations exhibited significant anticarcinogenic effects inhibiting the growth of breast cancer cell line (MDA-MB-231) and maximum inhibition of MDA-MB-231 cell was observed with the curry leaf extract from Kelantan. Based on these results, it is concluded that Malaysian curry leaf collected from the North (Kelantan) might be potential source of potent natural antioxidant and beneficial chemopreventive agents. PMID:24693327
Assiri, Adel M A; Elbanna, Khaled; Abulreesh, Hussein H; Ramadan, Mohamed Fawzy
Herbs rich in bioactive phytochemicals were recognized to have biological activities and possess many health-promoting effects. In this work, cold-pressed thyme (Thymus vulgaris L.) oil (TO) was studied for its lipid classes, fatty acid profile, tocols and phenolics contents. Antioxidant activity and radical scavenging potential of TO against free radicals (DPPH(・) and galvinoxyl) was determined. Antimicrobial activity (AA) of TO against food borne bacteria, food spoilage fungi and dermatophyte fungi were also evaluated. Neutral lipids accounted for the main lipid fraction in TO, followed by glycolipids and phospholipids. The major fatty acids in TO were linoleic, oleic, stearic, and palmitic. γ-Tocopherol (60.2% of total tocols) followed by α-tocotrienol (26.9%) and α-tocopherol (9.01% of total tocols) were the main tocols. TO contained high amounts of phenolic compounds (7.3 mg/g as GAE). TO had strong antiradical action wherein 65% of DPPH(・) radicals and 55% of galvinoxyl radical were quenched after 60 min of incubation. Rancimat assay showed that induction time (IT) for TO: sunflower oil blend (1:9, w/w) was 6.5 h, while TO: sunflower oil blend (2:8, w/w) recorded higher IT (9 h). TO inhibited the growth of all tested microorganisms. TO exhibited various degrees of AA against different food borne bacteria, food spoilage fungi and dermatophyte fungi, wherein the highest AA was recorded against dermatophyte fungi and yeasts including T. mentagrophytes (62 mm), T. rubrum (40 mm), and C. albicans (20 mm) followed by food spoilage fungi including A. flavus (32 mm) with minimal lethal concentrations (MLC) ranging between 80 to 320 μg/mL. Furthermore, TO exhibited broad-spectra activity against food borne bacteria including S. aureus (30 mm), E. coli (25 mm) and L. Monocytogenes (20 mm) with MLC ranging between 160 to 320 μg/mL. The results suggest that TO could be used economically as a valuable natural product with novel functional properties in food
Parra, Andres; Lopez, Pilar E; Garcia-Granados, Andres
Starting from solid wastes from two-phase olive-oil extraction, the pentacyclic triterpenes oleanolic acid and maslinic acid were isolated. These natural compounds were transformed into methyl olean-12-en-28-oate (5), which then was transformed into several seco-C-ring triterpene compounds by chemical and photolytic modifications. The triene seco-products were fragmented through several oxidative procedures to produce, simultaneously, cis- and trans-decalin derivatives, both potential synthons for bioactive compounds. The chemical behavior of the isolated fragments was investigated, and a suitable approach to several low-molecular-weight terpenes was performed. These are interesting processes for the value-addition to solid waste from the olive-oil industry.
Silva, Luís R; Azevedo, Jessica; Pereira, Maria J; Carro, Lorena; Velazquez, Encarna; Peix, Alvaro; Valentão, Patrícia; Andrade, Paula B
Pepper (Capsicum annuum L.) is an economically important agricultural crop and an excellent dietary source of natural colors and antioxidant compounds. The levels of these compounds can vary according to agricultural practices, like inoculation with plant growth-promoting rhizobacteria. In this work we evaluated for the first time the effect of the inoculation of two Rhizobium strains on C. annuum metabolites and bioactivity. The results revealed a decrease of organic acids and no effect on phenolics and capsaicinoids of leaves from inoculated plants. In the fruits from inoculated plants organic acids and phenolic compounds decreased, showing that fruits from inoculated plants present a higher ripeness stage than those from uninoculated ones. In general, the inoculation with Rhizobium did not improve the antioxidant activity of pepper fruits and leaves. Considering the positive effect on fruit ripening, the inoculation of C. annuum with Rhizobium is a beneficious agricultural practice for this nonlegume.
Amoutzias, Grigoris D; Chaliotis, Anargyros; Mossialos, Dimitris
Considering that 70% of our planet's surface is covered by oceans, it is likely that undiscovered biodiversity is still enormous. A large portion of marine biodiversity consists of microbiomes. They are very attractive targets of bioprospecting because they are able to produce a vast repertoire of secondary metabolites in order to adapt in diverse environments. In many cases secondary metabolites of pharmaceutical and biotechnological interest such as nonribosomal peptides (NRPs) and polyketides (PKs) are synthesized by multimodular enzymes named nonribosomal peptide synthetases (NRPSes) and type-I polyketide synthases (PKSes-I), respectively. Novel findings regarding the mechanisms underlying NRPS and PKS evolution demonstrate how microorganisms could leverage their metabolic potential. Moreover, these findings could facilitate synthetic biology approaches leading to novel bioactive compounds. Ongoing advances in bioinformatics and next-generation sequencing (NGS) technologies are driving the discovery of NRPs and PKs derived from marine microbiomes mainly through two strategies: genome-mining and metagenomics. Microbial genomes are now sequenced at an unprecedented rate and this vast quantity of biological information can be analyzed through genome mining in order to identify gene clusters encoding NRPSes and PKSes of interest. On the other hand, metagenomics is a fast-growing research field which directly studies microbial genomes and their products present in marine environments using culture-independent approaches. The aim of this review is to examine recent developments regarding discovery strategies of bioactive compounds synthesized by NRPS and type-I PKS derived from marine microbiomes and to highlight the vast diversity of NRPSes and PKSes present in marine environments by giving examples of recently discovered bioactive compounds.
Amoutzias, Grigoris D.; Chaliotis, Anargyros; Mossialos, Dimitris
Considering that 70% of our planet’s surface is covered by oceans, it is likely that undiscovered biodiversity is still enormous. A large portion of marine biodiversity consists of microbiomes. They are very attractive targets of bioprospecting because they are able to produce a vast repertoire of secondary metabolites in order to adapt in diverse environments. In many cases secondary metabolites of pharmaceutical and biotechnological interest such as nonribosomal peptides (NRPs) and polyketides (PKs) are synthesized by multimodular enzymes named nonribosomal peptide synthetases (NRPSes) and type-I polyketide synthases (PKSes-I), respectively. Novel findings regarding the mechanisms underlying NRPS and PKS evolution demonstrate how microorganisms could leverage their metabolic potential. Moreover, these findings could facilitate synthetic biology approaches leading to novel bioactive compounds. Ongoing advances in bioinformatics and next-generation sequencing (NGS) technologies are driving the discovery of NRPs and PKs derived from marine microbiomes mainly through two strategies: genome-mining and metagenomics. Microbial genomes are now sequenced at an unprecedented rate and this vast quantity of biological information can be analyzed through genome mining in order to identify gene clusters encoding NRPSes and PKSes of interest. On the other hand, metagenomics is a fast-growing research field which directly studies microbial genomes and their products present in marine environments using culture-independent approaches. The aim of this review is to examine recent developments regarding discovery strategies of bioactive compounds synthesized by NRPS and type-I PKS derived from marine microbiomes and to highlight the vast diversity of NRPSes and PKSes present in marine environments by giving examples of recently discovered bioactive compounds. PMID:27092515
Kim, Sun-A; Kim, Seung Hyun; Kim, In Sook; Lee, Dongho; Dong, Mi-Sook; Na, Chun-Soo; Nhiem, Nguyen Xuan; Yoo, Hye Hyun
A simple, sensitive, and precise reversed-phase liquid chromatographic method was developed for the quantitative determination of 4 bioactive phenolic compounds (gallic acid, fustin, fisetin, and sulfuretin) from the stem extract of Rhus verniciflua stokes. Chromatographic analysis was performed on a Capcell Pak C18 column (150 × 4.6 mm, 3 μm) with a mobile phase consisting of 0.1% formic acid and 90% acetonitrile at a flow rate of 1 mL/min. Quantitation was performed using a UV-vis detector at 260 nm. The method was validated in terms of selectivity, linearity, accuracy, precision, and recovery. Excellent linear behavior was observed over the investigated concentration range (10-500 μg/mL for gallic acid, fustin, and fisetin; 0.5-100 μg/mL for sulfuretin) with correlation coefficient (r(2)) values >0.99. The intra- and inter-day precision over the concentration range of compounds was less than 6.65% (relative standard deviation) and the accuracy was between 92.42% and 103.62%. The mean recoveries for all the analytes were more than 92.18%. This method was successfully applied for the analysis of bioactive phenolic compounds in the R. verniciflua extracts.
Escudero-López, Blanca; Cerrillo, Isabel; Gil-Izquierdo, Ángel; Hornero-Méndez, Dámaso; Herrero-Martín, Griselda; Berná, Genoveva; Medina, Sonia; Ferreres, Federico; Martín, Franz; Fernández-Pachón, María-Soledad
Previously, we reported that alcoholic fermentation enhanced flavanones and carotenoids content of orange juice. The aim of this work was to evaluate the influence of pasteurization on the qualitative and quantitative profile of bioactive compounds and the antioxidant capacity of fermented orange juice. Ascorbic acid (203 mg/L), total flavanones (647 mg/L), total carotenoids (7.07 mg/L) and provitamin A (90.06 RAEs/L) values of pasteurized orange beverage were lower than those of fermented juice. Total phenolic remained unchanged (585 mg/L) and was similar to that of original juice. The flavanones naringenin-7-O-glucoside, naringenin-7-O-rutinoside, hesperetin-7-O-rutinoside, hesperetin-7-O-glucoside and isosakuranetin-7-O-rutinoside, and the carotenoids karpoxanthin and isomer, neochrome, lutein, ζ-carotene, zeaxanthin, mutatoxanthin epimers, β-cryptoxanthin and auroxanthin epimers were the major compounds. Pasteurization produced a decrease in antioxidant capacity of fermented juice. However, TEAC (5.45 mM) and ORAC (6353 μM) values of orange beverage were similar to those of original orange juice. The novel orange beverage could be a valuable source of bioactive compounds with antioxidant capacity and exert potential beneficial effects.
Martínez-Flores, Héctor E; Garnica-Romo, Ma Guadalupe; Bermúdez-Aguirre, Daniela; Pokhrel, Prashant Raj; Barbosa-Cánovas, Gustavo V
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.
Identification of phenolic compounds by liquid chromatography-mass spectrometry in seventeen species of wild mushrooms in Central Mexico and determination of their antioxidant activity and bioactive compounds.
Yahia, Elhadi M; Gutiérrez-Orozco, Fabiola; Moreno-Pérez, Marco A
Wild mushrooms are important for the diet of some communities in Mexico. However, limited information exists on their chemical composition, contribution to the diet, and health effects. We characterized seventeen wild mushroom species growing in the state of Queretaro in Central Mexico. Most species analyzed were edible, but also included nonedible, medicinal, poisonous and toxic specimens. Whole mushrooms (caps and stipes) were characterized for water content, color, and total content of phenolic compounds, flavonoids and anthocyanins. In vitro antioxidant capacity was measured by FRAP and DPPH assays. Phenolic compounds were identified and quantified by HPLC-mass spectrometry. All species analyzed were found to possess antioxidant activity in vitro and a wide range of phenolic and organic compounds were identified. Our results add to the limited information available on the composition and potential nutritional and health value of wild mushrooms. Further analyses of their bioactivities are warranted.
Plumb, J; Lyons, J; Nørby, K; Thomas, M; Nørby, E; Poms, R; Bucchini, L; Restani, P; Kiely, M; Finglas, P
The newly developed ePlantLIBRA database is a comprehensive and searchable database, with up-to-date coherent and validated scientific information on plant food supplement (PFS) bioactive compounds, with putative health benefits as well as adverse effects, and contaminants and residues. It is the only web-based database available compiling peer reviewed publications and case studies on PFS. A user-friendly, efficient and flexible interface has been developed for searching, extracting, and exporting the data, including links to the original references. Data from over 570 publications have been quality evaluated and entered covering 70 PFS or their botanical ingredients.
Ainslie-Waldman, Cheryl E; Simpkins, Scott W; Upadhyaya, Pramod; Carmella, Steven G; Hecht, Stephen S; Trudo, Sabrina P
Bioactive compounds from plant foods are intensely investigated for effects on disease prevention. β-Glucuronidase/arylsulfatase from Helix pomatia (snail) is commonly used when quantifying exposure to metabolized dietary components. However, we describe here the contamination of multiple formulations of this enzyme preparation with 3,3'-diindolylmethane (DIM), 8-methoxypsoralen (8-MOP), and 5-methoxypsoralen (5-MOP), bioactives from cruciferous and apiaceous vegetables under investigation as putative cancer chemopreventive agents. We identified an Escherichia coli preparation of β-glucuronidase as free from contamination with any of the compounds tested. These results demonstrate the importance of selecting appropriate enzyme preparations when quantifying naturally occurring, trace level compounds in biological fluids.
Shaala, Lamiaa A; Youssef, Diaa T A
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.
Siqueira, Egle Machado de Almeida; Rosa, Fernanda Ribeiro; Fustinoni, Adriana Medeiros; de Sant'Ana, Lívia Pimentel; Arruda, Sandra Fernandes
The bioactive compounds content and the antioxidant activity (AA) of twelve fruits native to the Cerrado were compared with the Red Delicious apple by means of the antiradical efficiency (using the 2,2-diphenyl-1-picrylhydrazil assay/DPPH), ferric reducing antioxidant power (FRAP) and the β-carotene/linoleic system. The antiradical efficiency (AE) and the kinetic parameters (Efficient concentration/EC50 and time needed to reach the steady state to EC50 concentration/TEC50) of the DPPH curve were also evaluated for comparison with the Trolox equivalent (TE) values. A strong, significant and positive correlation was observed between the TE and AE values, whereas a weak and negative correlation was observed between TE and EC50, suggesting that the values of AE and TE are more useful for the determination of antiradical activity in fruits than the widely used EC50. The total phenolic content found in the fruits corresponded positively to their antioxidant activity. The high content of bioactive compounds (flavanols, anthocyanins or vitamin C) relative to the apple values found in araticum, cagaita, cajuzinho, jurubeba, lobeira, magaba and tucum corresponded to the high antioxidant activity of these fruits. Flavanols and anthocyanins may be the main bioactive components in these Cerrado fruits. The daily consumption of at least seven of the twelve Cerrado fruits studied, particularly, araticum, cagaita, lobeira and tucum, may confer protection against oxidative stress, and thus, they may prevent chronic diseases and premature aging. The findings of this study should stimulate demand, consumption and cultivation of Cerrado fruits and result in sustainable development of the region where this biome dominates. PMID:23991156
Zaini, Rana G; Brandt, Kirsten; Clench, Malcolm R; Le Maitre, Christine L
New therapies for leukaemia are urgently needed. Carrots have been suggested as a potential treatment for leukaemia in traditional medicine and have previously been studied in other contexts as potential sources of anticancer agents. Indicating that carrots may contain bioactive compounds, which may show potential in leukaemia therapies. This study investigated the effects of five fractions from carrot juice extract (CJE) on human lymphoid leukaemia cell lines, together with five purified bioactive compounds found in Daucus carota L, including: three polyacetylenes (falcarinol, falcarindiol and falcarindiol-3-acetate) and two carotenoids (beta-carotene and lutein). Their effects on induction of apoptosis using Annexin V/PI and Caspase 3 activity assays analysed via flow cytometry and inhibition of cellular proliferation using Cell Titer Glo assay and cell cycle analysis were investigated. Treatment of all three lymphoid leukaemia cell lines with the fraction from carrot extracts which contained polyacetylenes and carotenoids was significantly more cytotoxic than the 4 other fractions. Treatments with purified polyacetylenes also induced apoptosis in a dose and time responsive manner. Moreover, falcarinol and falcarindiol-3-acetate isolated from Daucus carota L were more cytotoxic than falcarindiol. In contrast, the carotenoids showed no significant effect on either apoptosis or cell proliferation in any of the cells investigated. This suggests that polyacetylenes rather than beta-carotene or lutein are the bioactive components found in Daucus carota L and could be useful in the development of new leukemic therapies. Here, for the first time, the cytotoxic effects of polyacetylenes have been shown to be exerted via induction of apoptosis and arrest of cell cycle.
Siqueira, Egle Machado de Almeida; Rosa, Fernanda Ribeiro; Fustinoni, Adriana Medeiros; de Sant'Ana, Lívia Pimentel; Arruda, Sandra Fernandes
The bioactive compounds content and the antioxidant activity (AA) of twelve fruits native to the Cerrado were compared with the Red Delicious apple by means of the antiradical efficiency (using the 2,2-diphenyl-1-picrylhydrazil assay/DPPH), ferric reducing antioxidant power (FRAP) and the β-carotene/linoleic system. The antiradical efficiency (AE) and the kinetic parameters (Efficient concentration/EC50 and time needed to reach the steady state to EC50 concentration/TEC50) of the DPPH curve were also evaluated for comparison with the Trolox equivalent (TE) values. A strong, significant and positive correlation was observed between the TE and AE values, whereas a weak and negative correlation was observed between TE and EC50, suggesting that the values of AE and TE are more useful for the determination of antiradical activity in fruits than the widely used EC50. The total phenolic content found in the fruits corresponded positively to their antioxidant activity. The high content of bioactive compounds (flavanols, anthocyanins or vitamin C) relative to the apple values found in araticum, cagaita, cajuzinho, jurubeba, lobeira, magaba and tucum corresponded to the high antioxidant activity of these fruits. Flavanols and anthocyanins may be the main bioactive components in these Cerrado fruits. The daily consumption of at least seven of the twelve Cerrado fruits studied, particularly, araticum, cagaita, lobeira and tucum, may confer protection against oxidative stress, and thus, they may prevent chronic diseases and premature aging. The findings of this study should stimulate demand, consumption and cultivation of Cerrado fruits and result in sustainable development of the region where this biome dominates.
Guiné, Raquel P F; Gonçalves, Fernando J
Culinary herbs are herbaceous (leafy) plants that add flavour and colour to all types of meals. There is a wide variety of herbs that are used for culinary purposes worldwide, which are also recognized for their beneficial health effects, and thus have also been used in folk medicine. Besides their nutritional value herbs are rich in many phytochemical components with bioactive effects, thus improving human health. The aim of the present work was to make a general overview of some of these herbs, including their gastronomic usage, their chemical composition in bioactive components and their reported health effects. This work showed that the health effects are very diverse and differ according to the herb in question. However, some of the most frequently citted biological activities include antioxidant, antimicrobial, and antiviral effects.
Marotta, F; Chui, D H; Yadav, H; Lorenzetti, A; Celep, G; Jain, S; Bomba, A; Polimeni, A; Zhong, K; Allegri, F
The aim of this study is to test the activity of a marine bioactive compound containing high-purity caviar-derived DNA, collagen elastin and protein extracts from sturgeon (LD-1227, Caviarlieri, Laboratoires Dom, Switzerland) to exert neuroprotective properties in an experimental setting while also being potential triggers of neurogenesis in a separate in vitro study. Supplementation with high-DHA mixture of LD-1227 was applied for 30 days to stress model rats. Both supplementations significantly mitigated the histological brain damage when analyzing hippocampal subregions and corticosterone level. However, LD-1227 was most significantly efficient in preventing SOD, Catalase and ascorbic acid decrease in brain tissue. Both supplementations stimulated neurogenesis in vitro and neuron markers in particular but og olygodendrocyte markers and glia increased only in LD-1227-enriched medium. Taken together, these data suggest that LD-1227 is able to significantly protect the brain structure redox system to higher degree than DHA. Moreover, from in vitro study it appears that marine bioactive compound, through it wide array of small unsaturated fatty acids, phospholipids and neurotransmitter precursors, is likely to influence neuronal and glial lineage to act differently from a DHA-rich mixture.
Lee, Jisoo; Kim, Yoo-Sun; Lee, JaeHwan; Heo, Seung Chul; Lee, Kook Lae; Choi, Sang-Woon; Kim, Yuri
Walnut has been known for its health benefits, including anti-cardiovascular disease and anti-oxidative properties. However, there is limited evidence elucidating its effects on cancer stem cells (CSCs) which represent a small subset of cancer cells that provide resistance against chemotherapy. This study aimed to evaluate the anti-CSCs potential of walnut phenolic extract (WPE) and its bioactive compounds, including (+)-catechin, chlorogenic acid, ellagic acid, and gallic acid. In the present study, CD133+CD44+ cells were isolated from HCT116 cells using fluorescence-activated cell sorting (FACS) and then treated with WPE. As a result, survival of the CD133+CD44+ HCT116 cells was inhibited and cell differentiation was induced by WPE. In addition, WPE down-regulated the CSC markers, CD133, CD44, DLK1, and Notch1, as well as the β-catenin/p-GSK3β signaling pathway. WPE suppressed the self-renewal capacity of CSCs. Furthermore, the WPE exhibited stronger anti-CSC effects than its individual bioactive compounds. Finally, the WPE inhibited specific CSC markers in primary colon cancer cells isolated from primary colon tumor. These results suggest that WPE can suppress colon cancer by regulating the characteristics of colon CSCs. PMID:27455311
Saavedra, M J; Aires, A; Dias, C; Almeida, J A; De Vasconcelos, M C B M; Santos, P; Rosa, E A
The transformation of byproducts and wastes generated by agro-food companies is of high importance since only a small portion of plant material is utilized directly for human consumption. Squash pumpkin is greatly used in Portugal and as by-products of its processing are generated tons of shell and seeds. In this study we aim to evaluate the potential of these wastes as sources of beneficial and bioactive compounds (antioxidants and antimicrobials), studying the effect of different extraction solvents and drying methods. The samples (fresh and cooked) were freeze-dried and oven-dried followed by extraction with different solvents that revealed the following decreasing order of efficiency: 70 % ethanol, 70 % methanol, 70 % acetone, ultra-pure water and 100 % dichloromethane. The oven-dried samples showed higher values of antioxidant activity and phenolic content, with exception of the values of phenolics for the seeds material. The shell samples presented higher values (1.47 - 70.96 % inhibition) of antioxidant activity and total phenolic content (2.00 - 10.69 mg GAE/g DW). A positive correlation was found between these two parameters on the shell samples, however the squash seeds revealed a negative correlation between the phenolic content and the antioxidant activity. The results show that these industrial agro-food residues are potentially good sources of bioactive compounds with health benefits.
Kwiecień, Iwona; Radecka, Iza; Kowalczuk, Marek; Adamus, Grażyna
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. PMID:25781908
Lee, Jisoo; Kim, Yoo-Sun; Lee, JaeHwan; Heo, Seung Chul; Lee, Kook Lae; Choi, Sang-Woon; Kim, Yuri
Walnut has been known for its health benefits, including anti-cardiovascular disease and anti-oxidative properties. However, there is limited evidence elucidating its effects on cancer stem cells (CSCs) which represent a small subset of cancer cells that provide resistance against chemotherapy. This study aimed to evaluate the anti-CSCs potential of walnut phenolic extract (WPE) and its bioactive compounds, including (+)-catechin, chlorogenic acid, ellagic acid, and gallic acid. In the present study, CD133⁺CD44⁺ cells were isolated from HCT116 cells using fluorescence-activated cell sorting (FACS) and then treated with WPE. As a result, survival of the CD133⁺CD44⁺ HCT116 cells was inhibited and cell differentiation was induced by WPE. In addition, WPE down-regulated the CSC markers, CD133, CD44, DLK1, and Notch1, as well as the β-catenin/p-GSK3β signaling pathway. WPE suppressed the self-renewal capacity of CSCs. Furthermore, the WPE exhibited stronger anti-CSC effects than its individual bioactive compounds. Finally, the WPE inhibited specific CSC markers in primary colon cancer cells isolated from primary colon tumor. These results suggest that WPE can suppress colon cancer by regulating the characteristics of colon CSCs.
Al-Sofyani, Abdulmohsin; Marimuthu, N.; Wilson, J. Jerald; Pugazhendi, Arulazhagan; Dhavamani, Jeyakumar
Three species of sponges and a tunicate were collected from Obhur creek of Jeddah coast for this bioactivity study. In order to assess the antifouling efficacy of selected marine organisms, methanolic extracts of these organisms were tested against different fouling bacterial forms and II-instar stage of the barnacle, Balanus amphitrite. Antibiosis, bioactivity and followed by multivariate analyses were carried out to check the efficacy of antifouling effect of the selected marine organisms. Principal component analysis revealed the exemplary antifouling efficacy of the sponge extracts of Stylissa sp. observed followed by Hyrtios sp. against bacterial forms in the laboratory study. De-trended correspondence analysis confirmed that the contribution of antifouling efficacy of the selected sponge extracts was observed to be more towards Bacillus sp., Vibrio sp. and Alteromonas sp. Moreover, the efficacy of Hyrtios sp. extract (20.430 μg mL-1) followed by Stylissa sp. (30.945 μg mL-1) showed higher against barnacle instar compared with other extracts in the bioactivity assay. Bray-Curtis cluster analysis under paired linkage categorized all the sponge extracts into one major cluster with 75% similarity, and one outlier tunicate. More than 80% similarity observed between Hyrtios sp. and Stylissa sp. Fourier transform infrared spectroscopy (FTIR) showed that the contribution of major peaks found in the marine organisms were towards sulfones, sulfoxides, cyanates and ketones.
Lassen, Lærke Münter; Nielsen, Agnieszka Zygadlo; Ziersen, Bibi; Gnanasekaran, Thiyagarajan; Møller, Birger Lindberg; Jensen, Poul Erik
Photosynthesis in plants, green algae, and cyanobacteria converts solar energy into chemical energy in the form of ATP and NADPH, both of which are used in primary metabolism. However, often more reducing power is generated by the photosystems than what is needed for primary metabolism. In this review, we discuss the development in the research field, focusing on how the photosystems can be used as synthetic biology building blocks to channel excess reducing power into light-driven production of alternative products. Plants synthesize a large number of high-value bioactive natural compounds. Some of the key enzymes catalyzing their biosynthesis are the cytochrome P450s situated in the endoplasmic reticulum. However, bioactive compounds are often synthesized in low quantities in the plants and are difficult to produce by chemical synthesis due to their often complex structures. Through a synthetic biology approach, enzymes with a requirement for reducing equivalents as cofactors, such as the cytochrome P450s, can be coupled directly to the photosynthetic energy output to obtain environmentally friendly production of complex chemical compounds. By relocating cytochrome P450s to the chloroplasts, reducing power can be diverted toward the reactions catalyzed by the cytochrome P450s. This provides a sustainable production method for high-value compounds that potentially can solve the problem of NADPH regeneration, which currently limits the biotechnological uses of cytochrome P450s. We describe the approaches that have been taken to couple enzymes to photosynthesis in vivo and to photosystem I in vitro and the challenges associated with this approach to develop new green production platforms.
Slatnar, Ana; Jakopic, Jerneja; Stampar, Franci; Veberic, Robert; Jamnik, Polona
Background Berry fruit is known for its high contents of various bioactive compounds. The latter constitute of anthocyanins, flavonols and flavanols and posses high antioxidative activity. The highly dynamic antioxidant system can be evaluated in vitro and in vivo in several model organisms. These measurements represent a good approximation of the real potential of bioactive compounds in the cells of higher eucarions. The aim of the study was thus to determine in vitro and in vivo antioxidant activity of different berry juices, which reportedly contain high amounts of phenolics. Methodology/Principal Findings Five different berry species were collected from several locations in central Slovenia and juice was extracted from each species separately. Juice was assessed for their in vitro and in vivo antioxidant activity. Phenolic profiles of berries were determined with the use of a HPLC/MS system, in vitro antioxidant activity with the DPPH radical scavenging method and in vivo antioxidative activity using Saccharomyces cerevisiae. The highest diversity of individual phenols was detected for bilberry juice. The highest in vitro antioxidant capacity was determined for blackcurrant juice. A decrease in intracellular oxidation compared to control was observed in the following order: blackcurrant < chokeberry = blueberry < bilberry. The results indicate important differences in antioxidant activity of berry juices between in vitro and in vivo studies. Conclusion/Significance In addition to the total content of phenolic compounds entering the cells, a key factor determining antioxidative activity of berry juices is also the ratio between the compounds. Where high content levels of anthocyanins and very low content levels of flavonols and hydroxycinnamic acids were measured a lower intracellular oxidation has been detected. Specifically, intracellular oxidation increased with higher consumption of hydroxycinnamic acids and lower consumption of anthocyanins in the cells
Ribnicky, David M; Kuhn, Peter; Poulev, Alexander; Logendra, Sithes; Zuberi, Aamir; Cefalu, William T; Raskin, Ilya
An ethanolic extract of Artemisia dracunculus L. (PMI-5011) was shown to be hypoglycemic in animal models for Type 2 diabetes and contain at least 6 bioactive compounds responsible for its anti-diabetic properties. To evaluate the bioavailability of the active compounds, high fat dietary induced obese C57BL/6J male mice were gavaged with PMI-5011 at 500 mg/kg body weight, after 4 h of food restriction. Blood plasma samples (200 uL) were obtained after ingestion, and the concentrations of the active compound in the blood sera were measured by electrospray LC-MS and determined to be maximal 4–6 h after gavage. Formulations of the extract with bioenhancers/solubilizers were evaluated in vivo for hypoglycemic activity and their effect on the abundance of active compounds in blood sera. At doses of 50–500 mg/kg/day, the hypoglycemic activity of the extract was enhanced 3–5 fold with the bioenhancer Labrasol, making it comparable to the activity of the anti-diabetic drug metformin. When combined with Labrasol, one of the active compounds, 2′, 4′-dihydroxy-4-methoxydihydrochalcone, was at least as effective as metformin at doses of 200–300 mg/kg/day. Therefore, bioenhancing agents like Labrasol can be used with multi-component botanical therapeutics such as PMI-5011 to increase their efficacy and/or to reduce the effective dose. PMID:19084584
Martins, Natália; Petropoulos, Spyridon; Ferreira, Isabel C F R
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.
Howell, Amy B
Cranberry (Vaccinium macrocarpon Ait.) ingestion has long been associated with prevention of urinary tract infections. The beneficial mechanism was historically thought to be due to the fruit acids causing a bacteriostatic effect in the urine. However, recently, a group of proanthocyanidins (PACs) with A-type linkages were isolated from cranberry which exhibit bacterial antiadhesion activity against both antibiotic susceptible and resistant strains of uropathogenic P-fimbriated Escherichia coli bacteria. The link between cranberry ingestion and maintenance of urinary tract health as well as the structural diversity, pharmacokinetics, quantification, and bacterial antiadhesion bioactivity of the A-linked cranberry PACs are reviewed.
Wang, Chen; Wang, Gang; Liu, Hong; Hou, Yun-long
Objective(s): Pharmacological studies showed that the extracts of Jin Yin Hua and its active constituents have lipid lowering, antipyretic, hepatoprotective, cytoprotective, antimicrobial, antibiotic, antioxidative, antiviral, and anti-inflammatory effects. The purpose of the present study was to investigate the protective effects of caffeoylquinic acids (CQAs) from Jin Yin Hua against hydrogen peroxide (H2O2)-induced and hypoxia-induced cytotoxicity using neonatal rat cardiomyocytes. Materials and Methods: Seven CQAs (C1 to C7) isolated and identified from Jin Yin Hua were used to examine the effects of H2O2-induced and hypoxia-induced cytotoxicity. We studied C4 and C6 as preventative bioactive compounds of the reactive oxygen species (ROS) production, apoptotic pathway, and apoptosis-related gene expression. Results: C4 and C6 were screened as bioactive compounds to exert a cytoprotective effect against oxidative injury. Pretreatment with C4 and C6, dose-dependently attenuated hypoxia-induced ROS production and reduced the ratio of GSSG/GStotal. Western blot data revealed that the inhibitory effect of C4 on H2O2-induced up and down-regulation of Bcl-2, Bax, caspase-3, and cleaved caspase-3. Apoptosis was evaluated by detection of DNA fragmentation using TUNEL assay, and quantified with Annexin V/PI staining. Conclusion: In vitro experiments revealed that both C4 and C6 protect cardiomyocytes from necrosis and apoptosis during H2O2-induced injury, via inhibiting the generation of ROS and activation of caspase-3 apoptotic pathway. These results demonstrated that CQAs might be a class of compounds which possess potent myocardial protective activity against the ischemic heart diseases related to oxidative stress. PMID:27096070
Zhang, Wen-Juan; You, Chun-Xue; Yang, Kai; Chen, Ran; Wang, Ying; Wu, Yan; Geng, Zhu-Feng; Chen, Hai-Ping; Jiang, Hai-Yan; Su, Yang; Lei, Ning; Ma, Ping; Du, Shu-Shan; Deng, Zhi-Wei
Artemisia argyi Lévl. et Van., a perennial herb with a strong volatile odor, is widely distrbuted in the world. Essential oil obtained from Artemisia argyi was analyzed by gas chromatography-mass spectrometry (GC-MS). A total of 32 components representing 91.74% of the total oil were identified and the main compounds in the oil were found to be eucalyptol (22.03%), β-pinene (14.53%), β-caryophyllene (9.24%) and (-)-camphor (5.45%). With a further isolation, four active constituents were obtained from the essential oil and identified as eucalyptol, β-pinene, β-caryophyllene and camphor. The essential oil and the four isolated compounds exhibited potential bioactivity against Lasioderma serricorne adults. In the progress of assay, it showed that the essential oil, camphor, eucalyptol, β-caryophyllene and β-pinene exhibited strong contact toxicity against L. serricorne adults with LD50 values of 6.42, 11.30, 15.58, 35.52, and 65.55 μg/adult, respectively. During the fumigant toxicity test, the essential oil, eucalyptol and camphor showed stronger fumigant toxicity against L. serricorne adults than β-pinene (LC50 = 29.03 mg/L air) with LC50 values of 8.04, 5.18 and 2.91 mg/L air. Moreover, the essential oil, eucalyptol, β-pinene and camphor also exhibited the strong repellency against L. serricorne adults, while, β-caryophyllene exhibited attracting activity relative to the positive control, DEET. The study revealed that the bioactivity properties of the essential oil can be attributed to the synergistic effects of its diverse major and minor components. The results indicate that the essential oil of A. argyi and the isolated compounds have potential to be developed into natural insecticides, fumigants or repellents in controlling insects in stored grains and traditional Chinese medicinal materials.
Hernández Suárez, Marcos; Molina Pérez, Daniel; Rodríguez-Rodríguez, Elena M; Díaz Romero, Carlos; Espinosa Borreguero, Francisco; Galindo-Villardón, Purificación
Tomatoes have been described as a functional food because of their particular composition of different bioactive compounds. In this study, the proximate composition, minerals and trace elements, and antioxidant compounds were determined in two tomato cultivars (Mariana and Dunkan) that were grown in Gran Canaria (Spain) either conventionally or hydroponically. Although compositional data of this type require being subjected to the specific statistical techniques of compositional analysis, this approach has not usually been considered in this context. In the present case, a compositional Mann-Whitney U test of the data showed significant differences for each factor (cultivar and cultivation system) in several of the compositional variables studied. For the differences between cultivars, these parameters were the protein, Mg, lycopene, ascorbic acid, citric acid, and fumaric acid contents. For the differences between cultivation systems, they were mainly those of the mineral and trace elements group. Although one-year data are insufficient to make clear relationship among compounds because more repetitions in several localities and years are necessary, the compositional HJ-biplot (in which the links provide estimates of the linear relationship among variables) results agreed with other scientific results about linear relationship among some compounds analyzed.
Mosele, Juana I; Macià, Alba; Romero, Mari-Paz; Motilva, María-José
The natural antioxidants of Arbutus unedo highlight the importance of this fruit as natural source of bioactive compounds. In the present study, to evaluate the stability of phenolic compounds, ascorbic acid and fat-soluble antioxidants (α-tocopherol, β-carotene and lutein), in vitro gastrointestinal digestion was applied to A. unedo fruit. After that, the non-absorbable fraction was anaerobically incubated with human faeces and the metabolic pathway for gallotannins, ellagitannins, flavan-3-ols and anthocyanins from A. unedo fruit was proposed. The results showed that the presence of pectin from the fruit hampered the solubilization of the phenolic compounds (with exception of gallic and ellagic acids) and fat-soluble vitamins during gastric digestion. Degradation of pectin-gel during the duodenal digestion favored the release of the phenolic compounds and fat-soluble antioxidants to the media. The catabolic activity of human microbiota led to the generation of a wide range of simple phenols, such as p-hydroxybenzoic acid and catechol, derived from the catabolism of gallotannins, ellagitannins, flavan-3-ols and anthocyanins.
Hernández Suárez, Marcos; Molina Pérez, Daniel; Rodríguez-Rodríguez, Elena M.; Díaz Romero, Carlos; Espinosa Borreguero, Francisco; Galindo-Villardón, Purificación
Tomatoes have been described as a functional food because of their particular composition of different bioactive compounds. In this study, the proximate composition, minerals and trace elements, and antioxidant compounds were determined in two tomato cultivars (Mariana and Dunkan) that were grown in Gran Canaria (Spain) either conventionally or hydroponically. Although compositional data of this type require being subjected to the specific statistical techniques of compositional analysis, this approach has not usually been considered in this context. In the present case, a compositional Mann–Whitney U test of the data showed significant differences for each factor (cultivar and cultivation system) in several of the compositional variables studied. For the differences between cultivars, these parameters were the protein, Mg, lycopene, ascorbic acid, citric acid, and fumaric acid contents. For the differences between cultivation systems, they were mainly those of the mineral and trace elements group. Although one-year data are insufficient to make clear relationship among compounds because more repetitions in several localities and years are necessary, the compositional HJ-biplot (in which the links provide estimates of the linear relationship among variables) results agreed with other scientific results about linear relationship among some compounds analyzed. PMID:27827839
Ballistreri, Gabriele; Continella, Alberto; Gentile, Alessandra; Amenta, Margherita; Fabroni, Simona; Rapisarda, Paolo
The fruit quality characteristics, phenolic compounds and antioxidant capacities of 24 sweet cherry (Prunus avium L.) cultivars grown on the mountainsides of the Etna volcano (Sicily, Italy) were evaluated. High-performance liquid chromatographic methods were used to identify and quantify sugars, organic acids and phenolics. A total of seven phenolic compounds were characterised as hydroxycinnamic acid derivatives (neochlorogenic acid, p-coumaroylquinic acid and chlorogenic acid) and anthocyanins (cyanidin 3-glucoside, cyanidin 3-rutinoside, pelargonidin 3-rutinoside and peonidin 3-rutinoside). The total anthocyanin content ranged from 6.21 to 94.20mg cyanidin 3-glucoside equivalents/100g fresh weight (FW), while the total phenol content ranged from 84.96 to 162.21mg gallic acid equivalents/100g FW. The oxygen radical absorbance capacity (ORAC) assay indicated that fruit of all genotypes possessed considerable antioxidant activity. The high level of phenolic compounds and antioxidant capacity of some sweet cherry fruits implied that they might be sources of bioactive compounds that are relevant to human health.
Nagendra chari, K L; Manasa, D; Srinivas, P; Sowbhagya, H B
Ginger (Zingiber officinale R.) is a popular spice used in various foods and beverages. 6-Gingerol is the major bioactive constituent responsible for the antiinflammatory, antitumour and antioxidant activities of ginger. The effect of application of α-amylase, viscozyme, cellulase, protease and pectinase enzymes to ginger on the oleoresin yield and 6-gingerol content has been investigated. Pre-treatment of ginger with α-amylase or viscozyme followed by extraction with acetone afforded higher yield of oleoresin (20%±0.5) and gingerol (12.2%±0.4) compared to control (15%±0.6 oleoresin, 6.4%±0.4 gingerol). Extraction of ginger pre-treated with enzymes followed by extraction with ethanol provided higher yield of gingerol (6.2-6.3%) than the control (5.5%) with comparable yields of the oleoresin (31-32%). Also, ethanol extract of cellulase pre-treated ginger had the maximum polyphenol content (37.5 mg/g). Apart from 6-gingerol, 6-paradol along with 6- and 8-methyl shogaols were the other important bio-active constituents in the oleoresin from cellulase-treated ginger.
Najafabadi, Najmeh Shams; Sahari, Mohammad Ali; Barzegar, Mohsen; Esfahani, Zohreh Hamidi
Interest in the protection of bioactive compounds and a safe alternative method for preservation of processed fruits and fruit juices has recently increased significantly throughout the world. There is a distinct lack of information on the profile of bioactive compounds in jujube fruit (e.g. organic acids, anthocyanins, and water-soluble vitamins) and their changes during processing (e.g. gamma irradiation). Therefore, in this study, the effect of gamma irradiation at different doses (0.0, 0.5, 1.0, 2.5 and 5.0 kGy) on some physicochemical properties and the bioactive compounds of jujube fruit was investigated. The total soluble solids (TSSs) values remained unaffected at various doses, while the level of total acidity (TA) showed a slight increase at doses ≥ 2.5 kGy (p ≤ 0.05). Irradiation up to 2.5 kGy caused a significant increase in the total monomeric anthocyanin and the total phenolic content (about 12% and 6%, respectively), but a significant decrease was observed in both parameters immediately after irradiation at 5 kGy. Moreover, irradiation treatment caused a significant decrease in L* value and a significant increase in a* and b* values (P ≤ 0.05); however, changes of color were slight until the dose of 5 kGy. Gamma irradiation up to 2.5 kGy had no significant effect on the concentration of malic, citric and succinic acids, while the level of ascorbic acid decreased significantly at all irradiation doses (0-5 kGy). Cyanidin-3, 5-diglucoside was determined as the major anthocyanin in the jujube fruit studied (about 68%), which was reduced significantly when 5 kGy of irradiation was applied (degradation percentage: 27%). The results demonstrated that vitamins C, B2 and B1 are the most water-soluble vitamins in jujube fruit, respectively. Vitamins C and B1 content significantly decreased at all applied doses (0-5 kGy), whereas B2 content at doses ≤ 2.5 kGy was not significantly affected. The results of this study indicate that gamma irradiation at
Richter, Ingrid; Fidler, Andrew E.
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
Richter, Ingrid; Fidler, Andrew E
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.
Rękas, Agnieszka; Wroniak, Małgorzata; Siger, Aleksander; Ścibisz, Iwona; Derewiaka, Dorota; Anders, Andrzej
In this study, the effect of rapeseed mechanical hulling and thermal pre-treatment by microwaves (from 2 to 10 min with 2-min intervals, 800 W) and roasting (from 20 to 100 min with 20-min intervals, 165 °C) on the content of phytochemicals in the oil was investigated. Results showed that both pre-treatments applied differentiated the oils in terms of the content of bioactive compounds. In general, oils pressed from hulled and thermally pre-treated seeds contained higher content of tocopherols, PC-8 and phytosterols, while oils pressed from non-hulled and pre-processed seeds had significantly higher concentration of polyphenols. Both microwaving and roasting contributed to an increase of antioxidant capacity of studied oils. The increase of radical scavenging activity of oils was seen mainly in hydrophilic fraction of oil, which was highly positively correlated with the amount of canolol formed during seeds heating.
Sikora, Małgorzata; Hallmann, Ewelina; Rembiałkowska, Ewa
Carrot roots are good source of diet fiber phenolic acids and also carotenoids, in that beta-carotene and lutein. Therefore carrot is an important in a preventive nutrition. According to many researchers vegetables from organic production and their products contain more beneficial nutrients than conventional vegetables. However the results in this field are not fully consistent. The research has been established to solve the rising doubts. The aim of work was to evaluate the level of bioactive compounds in organic and conventional carrot roots. Two varieties of carrots from organic and conventional system have been chosen to study: Flacoro and Perfekcja. The samples of the roots have been selected in the same time and passed on to the chemical analyzis. The results obtained showed that organic carrots contained significantly more dry matter, vitamin C, phenolic acids and carotenoids in comparison to the conventional ones.
Ducruet, Julien; Rébénaque, Pierrick; Diserens, Serge; Kosińska-Cagnazzo, Agnieszka; Héritier, Isabelle; Andlauer, Wilfried
Goji berries, traditionally used in Chinese medicine, are nowadays gaining popularity in the Western world. Efforts are made to enlarge the offer of goji containing foods. In this study, goji berries were added to ale type beer at different stages of the production process in order to develop a beverage with desirable sensory characteristic and high antioxidant capacity. The obtained beers differed significantly in terms of appearance, taste and antioxidant activity. Consumers preferred beers to which goji berries were added at the beginning of the brewing process. These beers were also characterized by lower turbidity, high color intensity, caramel- and coffee-like taste, high antioxidant activity and high content of bioactives such as rutin and 2-O-β-d-glucopyranosyl-l-ascorbic acid. To conclude, an addition of goji berries to traditional brewing process creates a perspective to enlarge the range of goji containing foods.
Osińska-Jaroszuk, Monika; Błachowicz, Adriana; Wydrych, Jerzy; Polak, Jolanta; Jarosz-Wilkołazka, Anna; Kandefer-Szerszeń, Martyna
A new exopolysaccharide preparation isolated from stationary cultures of the white rot fungus Ganoderma applanatum (GpEPS) was tested in terms of its bioactive properties including its cytotoxic and immunostimulatory effect. The results indicate that the tested GpEPS (at concentrations above 22.85 µg/mL and 228.5 µg/mL) may exhibit selective activity against tumor cells (cell lines SiHa) and stimulate production of TNF-α THP-1-derived macrophages at the level of 752.17 pg/mL. The GpEPS showed antibacterial properties against Staphyloccoccus aureus and a toxic effect against Vibrio fischeri cells (82.8% cell damage). High cholesterol-binding capacity and triglycerides-binding capacity (57.9% and 41.6% after 24 h of incubation with the tested substances, resp.) were also detected for the investigated samples of GpEPS. PMID:25114920
Kim, Hong-Gi; Bae, Jong-Hyang; Jastrzebski, Zenon; Cherkas, Andriy; Heo, Buk-Gu; Gorinstein, Shela; Ku, Yang-Gyu
The scope of this research was to determine the bioactive composition, antioxidant, binding, and anti-proliferative properties of red sweet paprika growing under artificial light. The amounts of carotenoids, chlorophyll, polyphenols, tannins, and flavonoids in red paprika (RP), cultivated in Korea, before and after light treatments under high pressure sodium (HPS) and lighting emitting plasma (LEP) lamps (RPControl, RPHPS, RPLEP), were analyzed in water (W) and ethanolic extracts (Et). Spectroscopic, radical scavenging assays, fluorescence and cytotoxicity measurements were applied. The results of this study showed that total chlorophyll and carotenes were the highest in RPHPS (10.50 ± 1.02 and 33.90 ± 3.26 μg/g dry weight (DW)). The strongest antioxidant capacity (μM TE/g DW) in a 2, 2'-azino-bis (3-ethyl-benzothiazoline-6-sulfonic acid) diammonium salt (ABTS(•+)) assay was in RPControlEt (24.34 ± 2.36), in a ferric-reducing/antioxidant power (FRAP) assay in RPHPSW (27.08 ± 2.4) and in a cupric reducing antioxidant (CUPRAC) in RPLEPW (70.99 ± 7.11). The paprika ethanolic extracts showed lower values in their bioactivity than the water ones. The binding and cytotoxicity abilities of extracted polyphenols correlated with their amounts. LEP treatment is better for plant growth characteristics than other conventional treatments. The investigated paprika samples can be used as a source of antioxidants.
Delgado-Adámez, Jonathan; Baltasar, M Nieves Franco; Yuste, María Concepción Ayuso; Martín-Vertedor, Daniel
The aim of this research was to evaluate strategies for the development of a virgin olive oil (VOO) enriched with aqueous extracts of olive leaf and cake to increase the necessary dose in the diet of phenolic compounds with a natural product, as phenolic compounds are involved on the healthy properties of olive oil. Different extraction procedures were evaluated with the aim of increasing the phenol content and antioxidant potential of extracts of olive leaf and cake. As leaves extract presented a higher total phenolic content, it was characterized in order to determine its phenolic profile, and was employed to enrich VOO. Diverse procedures were used to prepare enriched VOO with the leaves extract, and finally the effects of phenol enrichment were evaluated based on the antioxidant potential and oxidative stability of the prepared phenol-enriched virgin olive oils. These enriched VOOs increased significantly the content in phenolic compounds, antioxidant potential and oxidative stability 40, 4 and 1.5 fold more, respectively, than the Control oil. Furthermore, the addition of lecithin had a positive effect both on the phenolic compounds content, and on the antioxidant potential of the oils. Besides, the use of the olive leaves extract, with and without lecithin respectively, supposes a strategy potential for reducing the harmful effects that inflicts long-term preservation of VOOs and its possible deterioration.
Buniowska, Magdalena; Carbonell-Capella, Juana M; Frigola, Ana; Esteve, Maria J
A comparative study of the bioaccessibility of bioactive compounds and antioxidant capacity in a fruit juice-Stevia rebaudiana mixture processed by pulsed electric fields (PEF), high voltage electrical discharges (HVED) and ultrasound (USN) technology at two equivalent energy inputs (32-256kJ/kg) was made using an in vitro model. Ascorbic acid was not detected following intestinal digestion, while HVED, PEF and USN treatments increased total carotenoid bioaccessibility. HVED at an energy input of 32kJ/kg improved bioaccessibility of phenolic compounds (34.2%), anthocyanins (31.0%) and antioxidant capacity (35.8%, 29.1%, 31.9%, for TEAC, ORAC and DPPH assay, respectively) compared to untreated sample. This was also observed for PEF treated samples at an energy input of 256kJ/kg (37.0%, 15.6%, 29.4%, 26.5%, 23.5% for phenolics, anthocyanins, and antioxidant capacity using TEAC, ORAC and DPPH method, respectively). Consequently, pulsed electric technologies (HVED and PEF) show good prospects for enhanced bioaccessibility of compounds with putative health benefit.
Thuaytong, W; Anprung, P
This research involves the comparison of bioactive compounds, volatile compounds and prebiotic activity of white guava (Psidium guajava L.) cv. Pansithong and red guava cv. Samsi. The antioxidant activity values determined by 2-diphenyl-1-picryhydrazyl (DPPH) free radical scavenging and ferric reducing antioxidant power (FRAP) assays were 10.28 µg fresh weight (fw)/µg DPPH and 78.56 µg Trolox equivalent (TE)/g fw for white guava and 7.82 µg/µg DPPH, fw and 111.06 µM TE/g fw for red guava. Ascorbic acid contents were 130 and 112mg/100g fw total phenolics contents 145.52 and 163.36 mg gallic acid equivalents (GAE)/100 g fw and total flavonoids contents 19.06 and 35.85 mg catechin equivalents (CE)/100 g fw, in white and red guava, respectively. Volatile compounds in guava were analyzed by the solid-phase microextraction (SPME)/gas chromatography (GC)/mass spectrometry (MS) method. The major constituents identified in white and red guavas were cinnamyl alcohol, ethyl benzoate, ß-caryophyllene, (E)-3-hexenyl acetate and α-bisabolene. Prebiotic activity scores for Lactobacillus acidophilus LA-5 and Bifidobacterium lactis BB-12 were 0.12 and 0.28 in white guava, respectively, and 0.13 and 0.29 in red guava, respectively.
Costa, Margarida; Garcia, Mónica; Costa-Rodrigues, João; Costa, Maria Sofia; Ribeiro, Maria João; Fernandes, Maria Helena; Barros, Piedade; Barreiro, Aldo; Vasconcelos, Vitor; Martins, Rosário
The oceans remain a major source of natural compounds with potential in pharmacology. In particular, during the last few decades, marine cyanobacteria have been in focus as producers of interesting bioactive compounds, especially for the treatment of cancer. In this study, the anticancer potential of extracts from twenty eight marine cyanobacteria strains, belonging to the underexplored picoplanktonic genera, Cyanobium, Synechocystis and Synechococcus, and the filamentous genera, Nodosilinea, Leptolyngbya, Pseudanabaena and Romeria, were assessed in eight human tumor cell lines. First, a crude extract was obtained by dichloromethane:methanol extraction, and from it, three fractions were separated in a Si column chromatography. The crude extract and fractions were tested in eight human cancer cell lines for cell viability/toxicity, accessed with the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and lactic dehydrogenase release (LDH) assays. Eight point nine percent of the strains revealed strong cytotoxicity; 17.8% showed moderate cytotoxicity, and 14.3% assays showed low toxicity. The results obtained revealed that the studied genera of marine cyanobacteria are a promising source of novel compounds with potential anticancer activity and highlight the interest in also exploring the smaller filamentous and picoplanktonic genera of cyanobacteria. PMID:24384871
Fernandes, Ana; Fernandes, Iva; Cruz, Luís; Mateus, Nuno; Cabral, Miguel; de Freitas, Victor
Phenolic compounds, namely, hydrolyzable tannins and low molecular weight phenolic compounds, were isolated and purified from Portuguese cork from Quercus suber L. Some of these compounds were studied to evaluate their antioxidant activity, including free-radical scavenging capacity (DPPH method) and reducing capacity (FRAP method). All compounds tested showed significant antioxidant activity, namely, antiradical and reducing properties. The antiradical capacity seemed to increase with the presence of galloyl groups. Regarding the reducing capacity, this structure-activity relationship was not so clear. These compounds were also studied to evaluate the growth inhibitory effect on the estrogen responsive human breast cancer cell line (ER+) MCF-7 and two other colon cancer cell lines (Caco-2 and HT-29). Generally, all the compounds tested exhibited, after a continuous exposure during a 48 h period, a dose-dependent growth inhibitory effect. Relative inhibitory activity was primarily related to the number of phenolic hydroxyl groups (galloyl and HHDP moieties) found in the active structures, with more groups generally conferring increased effects, except for HHDP-di-galloyl-glucose. Mongolicain B showed a greater potential to inhibit the growth of the three cell lines tested, identical to the effect observed with castalagin. Since these compounds are structurally related with each other, this activity might be based within the C-glycosidic ellagitannin moiety.
Abdull Razis, Ahmad Faizal; Ibrahim, Muhammad Din; Kntayya, Saie Brindha
Phytomedicines are believed to have benefits over conventional drugs and are regaining interest in current research. Moringa oleifera is a multi-purpose herbal plant used as human food and an alternative for medicinal purposes worldwide. It has been identified by researchers as a plant with numerous health benefits including nutritional and medicinal advantages. Moringa oleifera contains essential amino acids, carotenoids in leaves, and components with nutraceutical properties, supporting the idea of using this plant as a nutritional supplement or constituent in food preparation. Some nutritional evaluation has been carried out in leaves and stem. An important factor that accounts for the medicinal uses of Moringa oleifera is its very wide range of vital antioxidants, antibiotics and nutrients including vitamins and minerals. Almost all parts from Moringa can be used as a source for nutrition with other useful values. This mini-review elaborate on details its health benefits.
Ghezzi, Diego; Vazquez, Rebeca Martinez; Osellame, Roberto; Valtorta, Flavia; Pedrocchi, Alessandra; Valle, Giuseppe Della; Ramponi, Roberta; Ferrigno, Giancarlo; Cerullo, Giulio
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
Cordier, Christopher; Morton, Daniel; Murrison, Sarah; Nelson, Adam; O'Leary-Steele, Catherine
The purpose of diversity-oriented synthesis is to drive the discovery of small molecules with previously unknown biological functions. Natural products necessarily populate biologically relevant chemical space, since they bind both their biosynthetic enzymes and their target macromolecules. Natural product families are, therefore, libraries of pre-validated, functionally diverse structures in which individual compounds selectively modulate unrelated macromolecular targets. This review describes examples of diversity-oriented syntheses which have, to some extent, been inspired by the structures of natural products. Particular emphasis is placed on innovations that allow the synthesis of compound libraries that, like natural products, are skeletally diverse. Mimicking the broad structural features of natural products may allow the discovery of compounds that modulate the functions of macromolecules for which ligands are not known. The ability of innovations in diversity-oriented synthesis to deliver such compounds is critically assessed.
Pazhanimurugan, Raasaiyah; Radhakrishnan, Manikkam; Shanmugasundaram, Thangavel; Gopikrishnan, Venugopal; Balagurunathan, Ramasamy
The present study emphasized the production of biologically active terpenoid compound from Streptomyces rochei M32, which was isolated from Western Ghats ecosystem, South India. The presence of resistant genes like mecA, vanA of Staphylococcus aureus and bla SHV, bla TEM of Pseudomonas aeruginosa was confirmed by molecular studies. The isolated compound from Streptomyces rochei M32 inhibited wide range of standard and clinical drug resistant pathogens and enteric pathogens. The rice bran supplemented basal medium influenced the active compound production on 8th day of fermentation and yielded 1875 mg of crude extract from 10 g of rice bran substrate. Purification and characterization of crude ethyl acetate extract was achieved by preparative thin layer chromatography. The active fraction was identified as terpenoid class compound by chemical screening. Based on the results of spectral studies (NMR, LC-MS, FTIR, etc.), the active compound was tentatively identified as 1, 19-bis (3-hydroxyazetidin-1-yl) nonadeca-5, 14-diene-1, 8, 12, 19-tetraone with molecular weight 462.41 g/mol. Minimum inhibitory concentration value ranges between 7.6 and 31.2 µg/mL against test organisms was observed. The cytotoxicity results on cervical cancer (HeLa) cell line showed IC50 value of 2.034 µg/mL. The corresponding compound is not previously reported from any microbial resources.
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...
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 ...
Lee, Eun-Jung; Moh, Sang-Hyun; Paek, Kee-Yoeup
This study deals with the effects of initial inoculum density and aeration volume on biomass and bioactive compound production in adventitious roots of Eleutherococcus koreanum Nakai in bulb-type bubble bioreactors (3-L capacity). While the fresh and dry weights of the roots increased with increasing inoculum density, the highest percentage dry weight and accumulation of total target compounds (eleutheroside B and E, chlorogenic acid, total phenolics, and flavonoids) were noted at an inoculum density of 5.0 g L(-1). Poor aeration volume (0.05 vvm) stunted root growth, and high aeration volume (0.4 vvm) caused physiological disorders. Moreover, an inoculum density of 5.0 g L(-1) and an aeration volume of 0.1 vvm resulted in the highest concentration of total target compounds and least root death. Such optimization of culture conditions will be beneficial for the large-scale production of E. koreanum biomass and bioactive compounds.
Zhang, Lanyue; Yang, Zhiwen; Huang, Zebin; Zhao, Mincong; Li, Penghui; Zhou, Wei; Zhang, Kun; Zheng, Xi; Lin, Li; Tang, Jian; Fang, Yanxiong; Du, Zhiyun
The chemical compositions of essential oils (EOs) extracted from Curcuma kwangsiensis rhizomes collected from six natural habitats in China were evaluated using gas chromatography-mass spectrometry (GC-MS). Fifty-seven components were identified from the six Eos; their main constituents were 8,9-dehydro-9-formyl-cycloisolongifolene (2.37-42.59%), germacrone (6.53-22.20%), and L-camphor (0.19-6.12%). The six EOs exhibited different DPPH radical-scavenging activities (IC50 , 2.24-31.03 μg/mL), with the activity of most of the EOs being much higher than that of Trolox C (IC50 , 10.49 μg/mL) and BHT (IC50 , 54.13 μg/mL). Most EOs had potent antimicrobial effects against the tested bacteria and fungus. They also exhibited cytotoxicity in B16 (IC50 , 4.44-147.4 μg/mL) and LNCaP cells (IC50 , 73.94-429.25 μg/mL). The EOs showed excellent anti-inflammatory action by significantly downregulating the expression of pro-inflammatory cytokines, cyclooxygenase-2 and tumor necrosis factor-α. This study provides insight into relationship among growth location, phytoconstituents, and bioactivities; the results indicate the potential of C. kwangsiensis as natural nutrients, medicines, and others additives. This article is protected by copyright. All rights reserved.
Varin, Thibault; Schuffenhauer, Ansgar; Ertl, Peter; Renner, Steffen
Identification of meaningful chemical patterns in the increasing amounts of high-throughput-generated bioactivity data available today is an increasingly important challenge for successful drug discovery. Herein, we present the scaffold network as a novel approach for mapping and navigation of chemical and biological space. A scaffold network represents the chemical space of a library of molecules consisting of all molecular scaffolds and smaller "parent" scaffolds generated therefrom by the pruning of rings, effectively leading to a network of common scaffold substructure relationships. This algorithm provides an extension of the scaffold tree algorithm that, instead of a network, generates a tree relationship between a heuristically rule-based selected subset of parent scaffolds. The approach was evaluated for the identification of statistically significantly active scaffolds from primary screening data for which the scaffold tree approach has already been shown to be successful. Because of the exhaustive enumeration of smaller scaffolds and the full enumeration of relationships between them, about twice as many statistically significantly active scaffolds were identified compared to the scaffold-tree-based approach. We suggest visualizing scaffold networks as islands of active scaffolds.
Teiten, Marie-Hélène; Gaascht, François; Dicato, Mario; Diederich, Marc
Since centuries, natural compounds from plants, animals and microorganisms were used in medicinal traditions to treat various diseases without a solid scientific basis. Recent studies have shown that plants that were used or are still used in the medieval European medicine are able to provide relieve for many diseases including cancer. Here we summarize impact and effect of selected purified active natural compounds from plants used in European medieval medicinal traditions on cancer hallmarks and enabling characteristics identified by Hanahan and Weinberg. The aim of this commentary is to discuss the pharmacological effect of pure compounds originally discovered in plants with therapeutic medieval use. Whereas many reviews deal with Ayurvedic traditions and traditional Chinese medicine, to our knowledge, the molecular basis of European medieval medicinal approaches are much less documented.
Van Cleemput, Marjan; Cattoor, Ko; De Bosscher, Karolien; Haegeman, Guy; De Keukeleire, Denis; Heyerick, Arne
Hop acids, a family of bitter compounds derived from the hop plant (Humulus lupulus), have been reported to exert a wide range of effects, both in vitro and in vivo. They exhibit potential anticancer activity by inhibiting cell proliferation and angiogenesis, by inducing apoptosis, and by increasing the expression of cytochrome P450 detoxification enzymes. Furthermore, hop bitter acids are effective against inflammatory and metabolic disorders, which makes them challenging candidates for the treatment of diabetes mellitus, cardiovascular diseases, and metabolic syndrome. This review summarizes the current knowledge on hop bitter acids, including both phytochemical aspects, as well as the biological and pharmacological properties of these compounds.
Hanif, Muhammad Asif; Al-Maskari, Ahmed Yahya; Al-Sabahi, Jamal Nasser; Al-Hdhrami, Ibtisam; Khan, Muhammad Mumtaz; Al-Azkawi, Ahlam; Hussain, Abdullah Ijaz
Medicago sativa Linn growing in Omani desert were chemically characterised using flame photometry, inductively coupled plasma, gas chromatography-mass spectrometry and high performance liquid chromatographic (HPLC) analysis. HPLC analyses were performed to determine the phenolics and flavonoids present in M. sativa. The major compounds detected in M. sativa leaves were protchaechenic acid (3.22%), hydroxyl benzoic acid (1.05%), β-Phenyl caffate (0.97%) and kaempherol (0.89%). Pterostilbene, a cholesterol-lowering compound, was detected in M. sativa.
Andrés, Víctor; Villanueva, María J; Tenorio, María D
The effects of high-pressure processing--HPP--(450 and 600 MPa/3 min/20 °C) on the colour, carotenoids, ascorbic acid, polyphenols and antioxidant activity (FRAP and DPPH) of a smoothie were compared to thermal processing (80 °C/3 min). Stability during 45 days at 4 °C was also evaluated. HPP samples showed slight differences (p < 0.05) in colour compared to untreated smoothies. Both HPP significantly increased the extractability of lycopene, β-carotene and polyphenols compared to untreated samples. After HPP, ascorbic acid was retained by more than 92% of the initial content. The best results for antioxidant activity were obtained when HPP was applied at 600 MPa. FRAP and DPPH showed a high correlation with ascorbic acid (R(2) = 0.7135 and 0.8107, respectively) and polyphenolic compounds (R(2) = 0.6819 and 0.6935, respectively), but not with total carotenoids. Changes in bioactive compounds during the storage period were lower in the HPP smoothie than in the thermal-treated sample.
Rao, Vidadala Rama Subba; Raju, Sagi Satyanarayana; Sarma, Vanka Umamaheswara; Sabine, Fouriner; Babu, Kothapalli Hari; Babu, Katragadda Suresh; Rao, Janaswamy Madhusudana
Piper nigrum L. is a traditional medicine widely used in India for illnesses such as constipation, diarrhoea, earache, gangrene, heart disease, hernia, hoarseness, indigestion, insect bites, insomnia, joint pain, liver problems, lung disease, oral abscesses, sunburn, tooth decay and toothaches. In this study, six bioactive compounds, namely piperine (1), pellitorine (2), guineensine (3), pipnoohine (4), trichostachine (5) and piperonal (6) were quantified in different extracts of P. nigrum L. and compared with those of P. longum L. and P. chaba Hunter. To evaluate the quality of P. nigrum, a simple, accurate and precise HPLC-PDA method was developed for the simultaneous determination of the above-mentioned six compounds. The separation was achieved by Phenomenex Luna RP C(18) column (150 × 4.6 mm, 5 µm, Phenomenex Inc, CA, USA) with a binary gradient solvent system of water-acetonitrile, at a flow rate of 1.0 mL min(-1) and detected at 210, 232, 262 and 343 nm. All six calibration curves showed good linearity (R (2) > 0.9966). The method was reproducible with intra- and inter-day variations of less than 2% and 5%, respectively. The results demonstrated that this method is simple, reliable and suitable for the quality control of these plants.
Delfanian, Mojtaba; Esmaeilzadeh Kenari, Reza; Sahari, Mohammad Ali
In this study, the bioactive compounds of loquat fruit (Eriobotrya japonica Lindl.) skin and pulp extracted by two extraction methods (solvent and ultrasound-assisted) with three solvents (ethanol, water and ethanol–water) were compared to supercritical fluid extraction. The antioxidant activities of skin and pulp extracts were evaluated and compared to tertiary butylhydroquinone (TBHQ) using 2, 2-diphenyl-1-picrylhydrazyl (DPPH˙) radical scavenging, β-carotene bleaching, and the Rancimat assays. In DPPH assay solvent extracts of skin by ethanol (SSE) and ethanol–water (SSEW) showed strong inhibitory activity. The SSEW also showed the highest inhibition percentage of 85.58% by the β-carotene bleaching assay and longest induction time of 4.78 h by the Rancimat method. The large amount of tocopherols and phenolics contained in the skin extract may cause its strong antioxidant ability. The results indicated that the solvent extraction with ethanol–water produced the maximum extraction yield of phenolic and tocopherol compounds from loquat fruit skin and pulp. Furthermore, solvent extraction was the most effective in antioxidant activity of the extracts compared to other extraction techniques. PMID:25987992
Górnaś, Paweł; Rudzińska, Magdalena; Raczyk, Marianna; Mišina, Inga; Soliven, Arianne; Lācis, Gunārs; Segliņa, Dalija
The profile of bioactive compounds (carotenoids, tocopherols, tocotrienols, phytosterols, and squalene) in oils recovered from the kernels of 28 plum varieties of hexaploid species Prunus domestica L. and diploid plums Prunus cerasifera Ehrh. and their crossbreeds were studied. Oil yields in plum kernels of both P. cerasifera and P. domestica was in wide ranges of 22.6-53.1 and 24.2-46.9% (w/w) dw, respectively. The contents of total tocochromanols, carotenoids, phytosterols, and squalene was significantly affected by the variety and ranged between 70.7 and 208.7 mg/100 g of oil, between 0.41 and 3.07 mg/100 g of oil, between 297.2 and 1569.6 mg/100 g of oil, and between 25.7 and 80.4 mg/100 g of oil, respectively. Regardless of the cultivar, β-sitosterol and γ-tocopherol were the main minor lipophilic compounds in plum kernel oils and constituted between 208.5 and 1258.7 mg/100 g of oil and between 60.5 and 182.0 mg/100 g of oil, respectively. Between the studied plum species, significant differences were recorded for δ-tocopherol (p = 0.007), 24-methylenecycloartanol (p = 0.038), and citrostadienol (p = 0.003), but they were insufficient for discrimination by PCA.
Carbonell-Capella, Juana M; Barba, Francisco J; Esteve, María J; Frígola, Ana
Comprehensive research is required to achieve the optimization of the antioxidant protection through baby foods, in particular, the commercially available fruit-based baby foods. This study investigated the physicochemical properties, ascorbic acid (AA), total carotenoids (TC), total phenolic content (TPC), trolox equivalent antioxidant capacity (TEAC) and oxygen radical absorbance capacity (ORAC) of 23 different commercially available fruit-based baby foods. The main contribution to the total antioxidant capacity (trolox equivalent antioxidant capacity and oxygen radical absorbance capacity) was provided by ascorbic acid, followed by phenolic compounds, in accordance with a mathematical equation obtained from the data: TEAC = 245.906 + 7.727 × (AA) + 1.988 × (TPC) - 0.008 × (TC) and ORAC = 318.662 + 2.775 × (AA) - 0.531 × (TPC) - 0.073 × (TC). Moreover, a positive correlation (r = 0.346, p < 0.05) was found for oxygen radical absorbance capacity and trolox equivalent antioxidant capacity methods. Baby foods with different kind of fruits used as ingredients showed higher antioxidant capacity. Among the commercial baby foods analysed in this work, that treated by gentle steam cooking process had high levels of bioactive compounds and antioxidant capacity.
Rubió, Laura; Serra, Aida; Macià, Alba; Borràs, Xenia; Romero, Maria-Paz; Motilva, Maria-José
In the present study, a selective and sensitive method, based on microelution solid-phase extraction (μSPE) plate and ultra-performance liquid chromatography coupled to tandem mass spectrometry (UPLC-MS/MS) was validated and applied to determine the plasma metabolites of the bioactive compounds of thyme. For validation process, standards of the more representative components of the phenolic and monoterpene fractions of thyme were spiked in plasma samples and then the quality parameters of the method were studied. Extraction recoveries (%R) of the studied compounds were higher than 75%, and the matrix effect (%ME) was lower than 18%. The LODs ranged from 1 to 65 μg/L, except for the thymol sulfate metabolite, which was 240 μg/L. This method was then applied for the analysis of rat plasma obtained at different times, from 0 to 6h, after an acute intake of thyme extract (5 g/kg body weight). Different thyme metabolites were identified and were mainly derived from rosmarinic acid (coumaric acid sulfate, caffeic acid sulfate, ferulic acid sulfate, hydroxyphenylpropionic acid sulfate, dihydroxyphenylpropionic acid sulfate and hydroxybenzoic acid) and thymol (thymol sulfate and thymol glucuronide). The most abundant thyme metabolites generated were hydroxyphenylpropionic acid sulfate and thymol sulfate, their respective concentrations in plasma being 446 and 8464 μM 1h after the intake of the thyme extract.
Nunes, Polyana Campos; Aquino, Jailane de Souza; Rockenbach, Ismael Ivan; Stamford, Tânia Lúcia Montenegro
The purpose of this study was to evaluate the physico-chemical characteristics, bioactive compounds and antioxidant activity of Malay apple fruit (Syzygium malaccense) grown in Brazil with regard to the geographical origin and its peel fractions and edible portion analyzed independently. Fruit diameter, weight, yield, and centesimal composition, ascorbic acid, reductive sugars, total soluble solids, pH and fiber content were determined. Total phenolics (1293 mg gallic acid equivalent/100 g) and total anthocyanins (1045 mg/100 g) contents were higher in the peel, with the major anthocyanin identified using HPLC-DAD-MS/MS as cyanidin 3-glucoside. Higher values for DPPH antiradical scavenging activity (47.52 μMol trolox equivalent antioxidant capacity/g) and Ferric Reducing Antioxidant Potential (FRAP, 0.19 mM ferreous sulfate/g) were also observed in the peel fraction. All extracts tested showed the ability to inhibit oxidation in the β-carotene/linoleic acid system. This study highlights the potential of Malay apple fruit as a good source of antioxidant compounds with potential benefits to human health. PMID:27352306
Thanh, Nguyen Van; Thao, Nguyen Phuong; Dat, Le Duc; Huong, Phan Thi Thanh; Lee, Sang Hyun; Jang, Hae Dong; Cuong, Nguyen Xuan; Nam, Nguyen Hoai; Kiem, Phan Van; Minh, Chau Van; Kim, Young Ho
Two new naphthalene diglucosides named nepenthosides A (1) and B (2), together with eleven known compounds (3-13), were isolated from the carnivorous plant Nepenthes mirabilis. The structures of these compounds were elucidated based on extensive spectroscopic analysis, including 1D- and 2D-NMR, and MS. The antioxidant activities of compounds 1-13 were evaluated in terms of their peroxyl radical-scavenging (trolox equivalent, TE) and reducing capacities. All isolates showed peroxyl radical-scavenging and reducing activities at concentrations of 1.0 and 10.0 μM. Anti-osteoporotic activities were investigated using murine osteoclastic RAW 264.7 cells. Compounds 1-7 and 9-12 significantly suppressed tartrate-resistant acid phosphatase activity down to 91.13 ± 1.18 to 42.39 ± 1.11%, relative to the control (100%) in nuclear factor-κB ligand (RANκL)-induced osteoclastic RAW 264.7 macrophage cells.
Wang, Yi; Liang, Xinying; Chen, Yaqi; Zhao, Xiaoping
Sirtuin type 1 (SIRT1) belongs to the family of NAD+ dependent histone deacetylases and plays a critical role in cellular metabolism and response to oxidative stress. Traditional Chinese medicines (TCMs), as an important part of natural products, have been reported to exert protective effect against oxidative stress in mitochondria. In this study, we screened SIRT1 activators from TCMs and investigated their activities against mitochondrial damage. 19 activators were found in total by in vitro SIRT1 activity assay. Among those active compounds, four compounds, ginsenoside Rb2, ginsenoside F1, ginsenoside Rc, and schisandrin A, were further studied to validate the SIRT1-activation effects by liquid chromatography-mass spectrometry and confirm their activities against oxidative damage in H9c2 cardiomyocytes exposed to tert-butyl hydroperoxide (t-BHP). The results showed that those compounds enhanced the deacetylated activity of SIRT1, increased ATP content, and inhibited intracellular ROS formation as well as regulating the activity of Mn-SOD. These SIRT1 activators also showed moderate protective effects on mitochondrial function in t-BHP cells by recovering oxygen consumption and increasing mitochondrial DNA content. Our results suggested that those compounds from TCMs attenuated oxidative stress-induced mitochondrial damage in cardiomyocytes through activation of SIRT1. PMID:26981165
Ghribi, Lotfi; Waffo-Téguo, Pierre; Cluzet, Stéphanie; Marchal, Axel; Marques, Jessica; Mérillon, Jean-Michel; Ben Jannet, Hichem
A phytochemical investigation of the roots of Ononis angustissima L. (Fabaceae) offered to the bio-guided isolation of new isoflavone 3-(4-(glucopyranosyloxy)-5-hydroxy-2-methoxyphenyl)-7-hydroxy-4H-chromen-4-one 1, together with nine known compounds, ononin 2, formononetin 3, (+)-puerol A-2'-O-β-D-glucose 4, (-)-puerol B-2'-O-β-D-glucopyranose ((-)-sophoraside A) 5, (+)-puerol A 6, (-)-trifolirhizin 7, (-)-trifolirhizin-6'-O-malonate 8, (-)-maackiain 9 and (-)-medicarpin 10. Compounds 2-10 were isolated and identified for the first time in Ononis angustissima. We investigated antioxidant capacities of isolated molecules and results showed that compound 6 exhibited the highest antioxidant activity with IC50 values of 19.53 μg/mL, 28.29 μg/mL and 38.53 μg/mL by DPPH radical, ABTS radical cation and reducing power assay, respectively, and an interesting IC50 (20.45 μg/mL) of 1 against DPPH. In addition, the neuroprotective activity of six isolated molecules (4-7, 9, 10) were evaluated. Following the exposure of PC12 cells to Aβ25-35, compounds 9 and 10 triggered a significant increase of cell viability and in a dose dependent manner.
Gosav, Steluta; Paduraru, Nicoleta; Praisler, Mirela
The drugs of abuse, which affect human nature and cause numerous crimes, have become a serious problem throughout the world. There are hundreds of amphetamine analogues on the black market. They consist of various alterations of the basic amphetamine molecular structure, which are yet not yet included in the lists of forbidden compounds although they retain or slightly modify the hallucinogenic effects of their parent compound. It is their important variety that makes their identification quite a challenge. A number of analytical procedures for the identification of amphetamines and their analogues have recently been reported. We are presenting the profile of the main hallucinogenic amphetamines obtained with the hyphenated techniques that are recommended for the identification of illicit amphetamines, i. e. gas chromatography combined with mass spectrometry (GC-MS) and gas chromatography coupled with Fourier transform infrared spectrometry (GC-FTIR). The infrared spectra of the analyzed hallucinogenic amphetamines present some absorption bands (1490 cm-1, 1440 cm-1, 1245 cm-1, 1050 cm-1 and 940 cm-1) that are very stable as position and shape, while their intensity depends of the side-chain substitution. The specific ionic fragment of the studied hallucinogenic compounds is the 3,4-methylenedioxybenzyl cation (m/e = 135) which has a small relative abundance (lesser than 20%). The complementarity of the above mentioned techniques for the identification of hallucinogenic compounds is discussed.
The jujube fruit is widely cultivated from China to Southwest Europe, India and the Middle East. Fresh, processed, and dried jujube fruit is used as a medical food, mostly in fresh form or as dried dates and confectionary recipes. Jujube fruit and seed extracts and pure compounds are reported to exh...
Kelebek, Hasim; Selli, Serkan; Kadiroğlu, Pınar; Kola, Osman; Kesen, Songul; Uçar, Burçak; Çetiner, Başak
The effects of hot and cold break industrial tomato paste production steps on phenolic compounds, carotenoids, organic acids, hydroxy methyl furfural (HMF) and other quality parameters of tomato pastes were investigated in this study. Phenolic compounds, carotenoids, organic acids, and HMF analyses were performed with LC-DAD-ESI-MS/MS and LC-DAD-RID was used for the sugar analyses. Furthermore, the antioxidant capacities of tomato pastes were assessed via the DPPH and ABTS methods. The increase of phenol acids at the processing steps of cold break production method was higher than the hot break production method. According to PCA analyses, phenolic acids characterized cold break tomato pastes while hot break tomato pastes were characterized by flavanols and flavanones. The total amount of organic acids decreased with processing and the loss of organic acids was lower in cold break pastes. Heating and evaporation were determined as the most important processing steps in which the amount of different quality parameters change.
Martins, Natália; Barros, Lillian; Santos-Buelga, Celestino; Henriques, Mariana; Silva, Sónia; Ferreira, Isabel C F R
The therapeutic benefits of medicinal plants are well known. Nevertheless, essential oils have been the main focus of antioxidant and antimicrobial studies, remaining scarce the reports with hydrophilic extracts. Thus, the antioxidant and antifungal activities of aqueous (prepared by infusion and decoction) and methanol/water (80:20, v/v) extracts of sage (Salvia officinalis L.) were evaluated and characterised in terms of phenolic compounds. Decoction and methanol/water extract gave the most pronounced antioxidant and antifungal properties, being positively related with their phenolic composition. The highest concentration of phenolic compounds was observed in the decoction, followed by methanol/water extract and infusion. Fungicidal and/or fungi static effects proved to be dependent on the extracts concentration. Overall, the incorporation of sage decoction in the daily diet or its use as a complement for antifungal therapies, could provide considerable benefits, also being an alternative to sage essential oils that can display some toxic effects.
Basta, Altaf H; El-Saied, Houssni; El-Deftar, Mervat M; El-Henawy, Ahmed A; El-Sheikh, Hussein H; Abdel-Shakour, Essam H; Hasanin, Mohamed S
The present study deals with synthesizing novel cellulose derivative, from modifying the carboxymethyl cellulose with amino phenylpropanoic acid (CMC-APP). The synthesized CMC-APP was evaluated as biological and anti-cancer active compound. The molecular structures of this active compound were built using the HyperChem program 7.5, together with conventional analysis (nitrogen content, FT-IR, and non-isothermal TGA analysis). Optimizing the CMC/APPA ratio was carried out as preliminary assessment step, via undetected antimicrobial activity measurement. The TEM study showed that, the synthesized cellulose CMC-APP derivative in the nano-scale particle size (range from 12.5 to 89.3nm). Among all the tested microorganisms and MCF-7 breast cancer cells, the synthesized nano-cellulose derivative is possible used as safety medicine for microbial infections and cancers. The minimal inhibitory concentration (MIC) for Gram-positive bacteria, and gram-negative bacteria are 48.82μg/mL and 97μg/mL, respectively. While, the unicellular fungi and filamentous fungi are 12.2μg/mL and 97.65μg/mL, respectively. The cytotoxic index (IC50) for MCF-7 breast cancers is 50μg/mL. Moreover, the computational study of ADMET (absorption, distribution, metabolism, elimination and toxic) properties, of the molecules showed that, this investigated nano-compound is good oral bioavailability.
Benítez, Vanesa; Mollá, Esperanza; Martín-Cabrejas, María A; Aguilera, Yolanda; López-Andréu, Francisco J; Cools, Katherine; Terry, Leon A; Esteban, Rosa M
The food industry produces a large amount of onion wastes, making it necessary to search for possible ways for their utilization. One way could be to use these onion wastes as a natural source of high-value functional ingredients, since onion are rich in several groups of compounds, which have perceived benefits to human health. The objective of this work is to gain knowledge of any differences between the different onion wastes obtained from industry and non-commercial bulbs to use them as food ingredients rich in specific compounds. The results showed that brown skin and top-bottom could be potentially used as functional ingredient rich in dietary fibre, mainly in insoluble fraction, and in total phenolics and flavonoids, with high antioxidant activity. Moreover, brown skin showed a high concentration of quercetin aglycone and calcium, and top-bottom showed high concentration of minerals. Outer scales could be used as source of flavonols, with good antioxidant activity and content of dietary fibre. However, inner scales could be an interesting source of fructans and alk(en)yl cystein sulphoxides. In addition, discarded onions (cvs Recas and Figueres) could be used as a good source of dietary fibre, and cv Recas also as a source of phenolics compounds.
More, Sandeep Vasant; Koppula, Sushruta; Kim, In-Su; Kumar, Hemant; Kim, Byung-Wook; Choi, Dong-Kug
Neurite loss is one of the cardinal features of neuronal injury. Apart from neuroprotection, reorganization of the lost neuronal network in the injured brain is necessary for the restoration of normal physiological functions. Neuritogenic activity of endogenous molecules in the brain such as nerve growth factor is well documented and supported by scientific studies which show innumerable compounds having neurite outgrowth activity from natural sources. Since the damaged brain lacks the reconstructive capacity, more efforts in research are focused on the identification of compounds that promote the reformation of neuronal networks. An abundancy of natural resources along with the corresponding activity profiles have shown promising results in the field of neuroscience. Recently, importance has also been placed on understanding neurite formation by natural products in relation to neuronal injury. Arrays of natural herbal products having plentiful active constituents have been found to enhance neurite outgrowth. They act synergistically with neurotrophic factors to promote neuritogenesis in the diseased brain. Therefore use of natural products for neuroregeneration provides new insights in drug development for treating neuronal injury. In this study, various compounds from natural sources with potential neurite outgrowth activity are reviewed in experimental models.
Boonchu, Thapakorn; Utama-Ang, Niramon
Grape (Vitis vinifera L.) pomace constitutes a promising source of phenolic compounds, gallic acid, flavan-3-ols, flavonoids, stilbene and anthocyanins that are beneficial for human health. The objectives of this study were to optimize the extraction and microencapsulation of red grape pomace. Central composite designs with two factors were conducted for optimization using response surface methodology. The temperature (45-85 °C), and the time (2-8 h) were designed for the extraction. The results indicated that the extraction temperature and time introduced the increasing the extraction yield, total phenolic content, anthocyanin and resveratrol, but the long extraction time reduced the tannin content. The results showed that the optimize condition was the extraction at 80 ± 1 °C for 2 h 53 min. This provided the highest content of polyphenolic compounds. The next experiment was microencapsulation of the extract which studied the amounts of maltodextrin (7-28 % w/v) and carboxymethylcellulose (CMC) (0-1.4 % w/v). The results showed that the optimized microencapsulation used 10.21 % w/v maltodextrin and 0.21 % w/v CMC to maximize all polyphenolic compounds, and also to minimize bitterness and astringency. This study illustrated that the optimal conditions for extraction and microencapsulation of the red grape extract have a high potential to produce functional ingredients.
Bowman, John P
The genus Pseudoalteromonas is a marine group of bacteria belonging to the class Gammaproteobacteria that has come to attention in the natural product and microbial ecology science fields in the last decade. Pigmented species of the genus have been shown to produce an array of low and high molecular weight compounds with antimicrobial, anti-fouling, algicidal and various pharmaceutically-relevant activities. Compounds formed include toxic proteins, polyanionic exopolymers, substituted phenolic and pyrolle-containing alkaloids, cyclic peptides and a range of bromine-substituted compounds. Ecologically, Pseudoalteromonas appears significant and to date has been shown to influence biofilm formation in various marine econiches; involved in predator-like interactions within the microbial loop; influence settlement, germination and metamorphosis of various invertebrate and algal species; and may also be adopted by marine flora and fauna as defensive agents. Studies have been so far limited to a relatively small subset of strains compared to the known diversity of the genus suggesting that many more discoveries of novel natural products as well as ecological connections these may have in the marine ecosystem remain to be made.
do Nascimento, Adriana M; Soares, Mateus Gonçalves; da Silva Torchelsen, Fernanda K V; de Araujo, Jorge A Viana; Lage, Paula S; Duarte, Mariana C; Andrade, Pedro H R; Ribeiro, Tatiana G; Coelho, Eduardo A F; do Nascimento, Andréa M
The purpose of this work was to evaluate the antileishmanial activity of endophytic fungi isolated from leaves of Vernonia polyanthes plant and their prospective use in the discovery of bioactive compounds. Sixteen endophytes were isolated by using potato dextrose agar medium and submitted to cultivation in rice medium. The fungal cultures were extracted with ethanol and used as crude extracts for testing their antileishmanial activity. The most active ethanol extract was obtained from P2-F3 strain, which was identified as Cochliobolus sativus by ITS rRNA gene sequence data. Followed by a bioassay-guided fractionation, the cochlioquinone A, isocochlioquinone A and anhydrocochlioquinone A compounds were isolated from the crude extracts and demonstrated to inhibit the parasites. From the present work, it is possible to conclude that endophytic fungi derived from medicinal plant V. polyanthes may be considered promising source for the discovery of bioactive compounds.
Kim, Jung-Hoon; Shin, Hyeun-Kyoo; Seo, Chang-Seob
Background: Yukmijihwang-tang (YJT) contains multiple bioactive compounds. Heat-reflux extraction was employed and optimized for the extraction of the bioactive compounds in YJT. Objective: The determination of optimal conditions with maximum yields of bioactive compounds, gallic acid, 5-hydroxymethylfurfural, morroniside, loganin, paeoniflorin, benzoic acid and paeonol, in YJT. Materials and Methods: The extraction ratio (ratio of water to herbal formula), extraction time and extraction number were set as individual values and the yields of the seven compounds were the response values that were optimized with a Box–Behnken design. Results: The optimal conditions obtained from response surface methodology (RSM) were 1:11.99 for the extraction ratio, 94.53 min for the extraction time and 2.21 for the extraction number. Under the optimal conditions, the response value of the experiment closely agreed with the predicted response value. Conclusions: The result suggests that RSM is successfully applied for optimizing the extraction of the marker compounds in YJT. PMID:25298681
Yun, Bo-Ra; Yang, Hye Jin; Weon, Jin Bae; Lee, Jiwoo; Eom, Min Rye; Ma, Choong Je
Background: Dianthus superbus, one of traditional herbal medicine, is widely used to treat urethritis, carbuncles and carcinoma. Objective: A simultaneous determination method was established for controlling the quality of D. superbus using the eight compounds, (E)-methyl-4-hydroxy-4-(8a-methyl-3-oxodecahydronaphthalen-4a-yl) (1), diosmetin-7-O(2'',6''-di-O-α-L-rhamnopyranosyl)-β-D-glucopyranoside (2), vanillic acid (3), 4-hydroxyphenyl acetic acid (4), 4-methoxyphenyl acetic acid (5), (E)-4-methoxycinnamic acid (6), 3-methoxy-4-hydroxyphenylethanol (7), and methyl hydroferulate (8) isolated from D. superbus. Materials and Methods: This analysis method was developed using high performance liquid chromatography coupled with diode array detector with a Shishedo C18 column at a column temperature of 3°C. The mobile phase was composed of 0.1% trifluoroacetic acid in water and acetonitrile. The flow rate was 1 ml/min and detection wavelength was set at 205 nm and 280 nm. Validation was performed in order to demonstrate selectivity, accuracy and precision of the method. Results: The calibration curves showed good linearity (R2 > 0.99). The limits of detection and limits of quantification were within the ranges 0.0159–0.6205 μg/ml and 0.3210–1.8802 μg/ml, respectively. Moreover, the relative standard deviations of intra- and inter-day precision were both <2.98%. The overall recoveries were in the range of 96.23–109.87%. Quantitative analysis of eight compounds in 12 D. superbus samples (D-1–D-12) from various regions were analyzed and compared by developed method. Conclusion: As a result, this established method was accurate and sensitive for the quality evaluation of eight compounds isolated from D. superbus and may provide a new basis for quality control of D. superbus. SUMMARY A simultaneous determination method of eight compounds in Dianthus superbus was established by high performance liquid chromatography-diode array detectorDeveloped analysis method is
Gomathi, Duraisamy; Kalaiselvi, Manokaran; Ravikumar, Ganesan; Devaki, Kanakasabapathi; Uma, Chandrasekar
Medicinal plants are at great interest to the researcher in the field of biotechnology, as most of the drug industries depend in medicinal plants for the production of pharmaceutical compounds. Plants are the traditional sources for many chemicals used as pharmaceutical biochemicals, fragrances, food colours and flavours in different countries especially in India. Most herbal medicines and their derivative products were often prepared from crude plant extracts, which comprise a complex mixture of different phytochemical constituents (plant secondary metabolites). The chemical features of these constituents differ considerably among different species. GC-MS method used for the analysis of the obtained extracts can be an interesting tool for testing the amount of some active principles in herbs used in cosmetic, drugs, pharmaceutical or food industry. The aim of this study was to carry out for identification of bioactive compounds from the whole plant ethanolic extract of Evolvulus alsinoides by Gas chromatography and Mass spectroscopy (GC-MS). GCMS analysis of ethanolic extract was done by standard protocol using the equipment Thermo GC-Trace Ultra Version: 5.0, Thermo MS DSQ II. The GC-MS analysis revealed the presence of various compounds like piperine, octodeconoic acids, hexadecanoic acid and squalene in the ethanolic extract of Evolvulus alsinoides. Hence, the Evolvulus alsinoides may have chemopreventive, anticancer, anti-microbial activity, antioxidant and antidiabetic activity due to the presence of secondary metabolites in the ethanolic extract. Due to the presence of esters which can be used as a flavoring agent in food industries. These findings support the traditional use of Evolvulus alsinoides in various disorders. Further studies are needed to isolate active principle of the extract as well as to elucidate their exact mechanism of action in various disorders.
Li, Jing; Wang, Juan; Li, Jinxin; Liu, Dahui; Li, Hongfa; Gao, Wenyuan; Li, Jianli; Liu, Shujie
In the present study, the culture conditions for the accumulation of Glycyrrhiza uralensis adventitious root metabolites in balloon-type bubble bioreactors (BTBBs) have been optimized. The results of the culture showed that the best culture conditions were a cone angle of 90° bioreactor and 0.4-0.6-0.4-vvm aeration volume. Aspergillus niger can be used as a fungal elicitor to enhance the production of defense compounds in plants. With the addition of a fungal elicitor (derived from Aspergillus niger), the maximum accumulation of total flavonoids (16.12 mg g(-1)) and glycyrrhetinic acid (0.18 mg g(-1)) occurred at a dose of 400 mg L(-1) of Aspergillus niger resulting in a 3.47-fold and 1.8-fold increase over control roots. However, the highest concentration of polysaccharide (106.06 mg g(-1)) was achieved with a mixture of elicitors (Aspergillus niger and salicylic acid) added to the medium, resulting in a 1.09-fold increase over Aspergillus niger treatment alone. Electrospray ionization tandem mass spectrometry (ESI-MS(n)) analysis was performed, showing that seven compounds were present after treatment with the elicitors, including uralsaponin B, licorice saponin B2, liquiritin, and (3R)-vestitol, only identified in the mixed elicitor treatment group. It has also been found that elicitors (Aspergillus niger and salicylic acid) significantly upregulated the expression of the cinnamate 4-hydroxylase (C4H), β-amyrin synthase (β-AS), squalene epoxidase (SE) and a cytochrome P450 monooxygenase (CYP72A154) genes, which are involved in the biosynthesis of bioactive compounds, and increased superoxide dismutase (SOD), catalase (CAT), and peroxidase (POD) activity.
Conley, Justin M.; Evans, Nicola; Cardon, Mary C.; Rosenblum, Laura; Iwanowicz, Luke; Hartig, Phillip C.; Schenck, Kathleen M.; Bradley, Paul M.; Wilson, Vickie S.
In vitro bioassays are sensitive, effect-based tools used to quantitatively screen for chemicals with nuclear receptor activity in environmental samples. We measured in vitro estrogen (ER), androgen (AR), and glucocorticoid receptor (GR) activity, along with a broad suite of chemical analytes, in streamwater from 35 well-characterized sites (3 reference and 32 impacted) across 24 states and Puerto Rico. ER agonism was the most frequently detected with nearly all sites (34/35) displaying activity (range, 0.054–116 ng E2Eq L–1). There was a strong linear relationship (r2 = 0.917) between in vitro ER activity and concentrations of steroidal estrogens after correcting for the in vitro potency of each compound. AR agonism was detected in 5/35 samples (range, 1.6–4.8 ng DHTEq L–1) but concentrations of androgenic compounds were largely unable to account for the in vitro activity. Similarly, GR agonism was detected in 9/35 samples (range, 6.0–43 ng DexEq L–1); however, none of the recognized GR-active compounds on the target-chemical analyte list were detected. The utility of in vitro assays in water quality monitoring was evident from both the quantitative agreement between ER activity and estrogen concentrations, as well as the detection of AR and GR activity for which there were limited or no corresponding target-chemical detections to explain the bioactivity. Incorporation of in vitro bioassays as complements to chemical analyses in standard water quality monitoring efforts would allow for more complete assessment of the chemical mixtures present in many surface waters.
Santos, Tássia R T; Silva, Marcela F; Nishi, Leticia; Vieira, Angélica M S; Klein, Márcia R F; Andrade, Murilo B; Vieira, Marcelo F; Bergamasco, Rosângela
In this work, to evaluate the effectiveness of the coagulation/flocculation using a natural coagulant, using Moringa oleifera Lam functionalized with magnetic iron oxide nanoparticles, producing flakes that are attracted by an external magnetic field, thereby allowing a fast settling and separation of the clarified liquid, is proposed. The removal efficiency of the parameters, apparent color, turbidity, and compounds with UV254nm absorption, was evaluated. The magnetic functionalized M. oleifera Lam coagulant could effectively remove 90 % of turbidity, 85 % of apparent color, and 50 % for the compounds with absorption at UV254nm, in surface waters under the influence of an external magnetic field within 30 min. It was found that the coagulation/flocculation treatment using magnetic functionalized M. oleifera Lam coagulant was able to reduce the values of the physico-chemical parameters evaluated with reduced settling time.
Mejia, Monica; Heghinian, Mari D.; Busch, Alexandra; Marí, Frank; Godenschwege, Tanja A.
Screening compounds for in vivo activity can be used as a first step to identify candidates that may be developed into pharmacological agents1,2. We developed a novel nanoinjection/electrophysiology assay that allows the detection of bioactive modulatory effects of compounds on the function of a neuronal circuit that mediates the escape response in Drosophila melanogaster3,4. Our in vivo assay, which uses the Drosophila Giant Fiber System (GFS, Figure 1) allows screening of different types of compounds, such as small molecules or peptides, and requires only minimal quantities to elicit an effect. In addition, the Drosophila GFS offers a large variety of potential molecular targets on neurons or muscles. The Giant Fibers (GFs) synapse electrically (Gap Junctions) as well as chemically (cholinergic) onto a Peripheral Synapsing Interneuron (PSI) and the Tergo Trochanteral Muscle neuron (TTMn)5. The PSI to DLMn (Dorsal Longitudinal Muscle neuron) connection is dependent on Dα7 nicotinic acetylcholine receptors (nAChRs)6. Finally, the neuromuscular junctions (NMJ) of the TTMn and the DLMn with the jump (TTM) and flight muscles (DLM) are glutamatergic7-12. Here, we demonstrate how to inject nanoliter quantities of a compound, while obtaining electrophysiological intracellular recordings from the Giant Fiber System13 and how to monitor the effects of the compound on the function of this circuit. We show specificity of the assay with methyllycaconitine citrate (MLA), a nAChR antagonist, which disrupts the PSI to DLMn connection but not the GF to TTMn connection or the function of the NMJ at the jump or flight muscles. Before beginning this video it is critical that you carefully watch and become familiar with the JoVE video titled "Electrophysiological Recordings from the Giant Fiber Pathway of D. melanogaster " from Augustin et al7, as the video presented here is intended as an expansion to this existing technique. Here we use the electrophysiological recordings method
The types of wild mint (Mentha spicata L.) were sampled from different geographical regions in Tunceli (Turkey) in order to find out their vitamin, mineral, phenolic contents and their antioxidant properties. The total phenol varied from 77.7±0.242 to 52.34±0.351 mg of GAEs/g of dry mint. The highest radical effect of scavenging was observed in Mazgirt parting of the ways 7.5 km with 6.17±0.245 mg/mL. The highest reducing power and metal chelating were observed in the mint from Cicekli parting of the ways 6.5 km Demirkapı. Among the various macronutrients which were estimated in the plant samples, potassium was presented in the highest quantity followed by calcium and phosphate. Although rutin and resveratrol were not determined in any samples, kaempferol and catechin levels were found out in almost all samples. The concentrations of vitamin A ranged between 42,14±5.70 and 13.61±3.00 (mg/kg dry weight). These results show that plants of mint are quite rich in phenolic compounds, and these have been appeared to have antioxidant activity, which agrees with this work, since the extract showed a higher content of phenolic compounds and higher antioxidant activity and mint may be considered as a natural alternative source for food, pharmacology and medicine sectors.
Lou-Bonafonte, José M; Arnal, Carmen; Navarro, María A; Osada, Jesús
As olive oil is the main source of calories in the Mediterranean diet, a great deal of research has been devoted to characterizing its role in atherosclerosis. Virgin olive oil is an oily matrix that contains hydrocarbons, mainly squalene; triterpenes such as uvaol, erythrodiol, oleanolic, and maslinic acid; phytosterols; and a wide range of phenolic compounds comprising simple phenols, flavonoids, secoiridoids, and lignans. In this review, we analyze the studies dealing with atherosclerosis and olive oil in several species. A protective role of virgin olive oil against atherosclerosis has been shown in ApoE-deficient mice and hamsters. In the former animal, sex, dose, and dietary cholesterol are modulators of the outcome. Contradictory findings have been reported for rabbits, a circumstance that could be due to the profusion of experimental designs, differing in terms of doses and animal strains, as well as sources of olive oils. This role has yet to be fully validated in humans. Minor components of olive oil have been shown to be involved in atherosclerosis protection. Nevertheless, evidence of the potential of isolated compounds or the right combination of them to achieve the antiatherosclerotic effect of virgin olive oil is inconclusive and will undoubtedly require further experimental support.
Amjad, Muhammad; Sumrra, Sajjad H; Akram, Muhammad Safwan; Chohan, Zahid H
Metal-based ethanolamines, (L(1))-(L(4)) coordinated with Co(II), Cu(II), Ni(II) and Zn(II) metals in 1:2 (metal:ligand) molar ratio to produce new compounds have been reported. These compounds were screened for their bactericidal/fungicidal activity against a number of bacterial (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa, Salmonella typhi, Staphylococcus aureus and Bacillus subtilis) and fungal strains (Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glabrata) alongside against a shrimp species known as Artemia salina. The screening results indicated that metal complexes have significantly higher activity than uncomplexed ligands against one or more bacterial/fungal species due to chelation. The ligand (L(4)) displayed good bacterial and fungal activity as compared to other ligands. The antibacterial results revealed that the Zn(II) complex (16) of (L(4)) was found to be the most active complex and Co(II) complex (14) of the same ligand (L(4)), demonstrated the highest antifungal activity.
Bounda, Guy-Armel; Feng, YU
Polygonum multiflorum Thunb. (PMT), officially listed in the Chinese Pharmacopoeia, is one of the most popular perennial Chinese traditional medicines known as He shou wu in China and East Asia, and as Fo-ti in North America. Mounting pharmacological studies have stressed out its key benefice for the treatment of various diseases and medical conditions such as liver injury, cancer, diabetes, alopecia, atherosclerosis, and neurodegenerative diseases as well. International databases such as PubMed/Medline, Science citation Index and Google Scholar were searched for clinical studies recently published on P. multiflorum. Various clinical studies published articles were retrieved, providing information relevant to pharmacokinetics-pharmacodynamics analysis, sleep disorders, dyslipidemia treatment, and neurodegenerative diseases. This review is an effort to update the clinical picture of investigations ever carried on PMT and/or its isolated bio-compounds and to enlighten its therapeutic assessment. PMID:26130933
Jara-Palacios, M José; Hernanz, Dolores; Cifuentes-Gomez, Tania; Escudero-Gilete, M Luisa; Heredia, Francisco J; Spencer, Jeremy P E
The antiproliferative effects of a purified white grape pomace extract (PWGPE), as well as of some phenolic standards on colon cancer cells were examined. The phenolic composition of the PWGPE was determined by rapid resolution liquid chromatography/mass spectrometry (RRLC/MS). The PWGPE had 92.6, 43.3 and 6.01mg/g of flavanols, flavonols and phenolic acids, respectively and, along with pure catechin, epicatechin, quercetin and gallic acid, they were all found capable of inhibiting cellular proliferation. PWGPE (100μg/ml) inhibited the proliferation of cells by 52.1% at 48h, whilst catechin, epicatechin, quercetin and gallic acid (60μg/ml) inhibited growth by 65.2%, 62.2%, 81.0% and 71.0%, respectively, at 72h. The PWGPE is an interesting source of phenolic compounds with antiproliferative properties, that could be of interest in the food and pharmaceutical industries.
The UbiA superfamily of intramembrane prenyltransferases catalyzes a key biosynthetic step in the production of ubiquinones, menaquinones, plastoquinones, hemes, chlorophylls, vitamin E, and structural lipids. These lipophilic compounds serve as electron and proton carriers for cellular respiration and photosynthesis, as antioxidants to reduce cell damage, and as structural components of microbial cell walls and membranes. This article reviews the biological functions and enzymatic activities of representative members of the superfamily, focusing on the remarkable recent research progress revealing that the UbiA superfamily is centrally implicated in several important physiological processes and human diseases. Because prenyltransferases in this superfamily have distinctive substrate preferences, two recent crystal structures are compared to illuminate the general mechanism for substrate recognition. PMID:26922674
Chi, Cheng; Giri, Sib Sankar; Jun, Jin Woo; Kim, Hyoun Joong; Yun, Saekil; Kim, Sang Guen
In the present study, we investigated effects of compound kaempferol 3-a-L-(4-O-acetyl)rhamnopyranoside-7-a-L-rhamnopyranoside (SA) isolated from Dryopteris crassirhizoma during immune-related gene expression in Ctenopharyngodon idella head kidney macrophages (CIHKM). The expression of immune-related genes (IL-1β, TNF-α, MyD88, and Mx1) were investigated using real-time PCR at 2 h, 8 h, 12 h, and 24 h after incubation with 1, 10, and 50 μg mL−1 of SA. Furthermore, fish were injected intraperitoneally with 100 μL of SA, and immune parameters such as lysozyme activity, complement C3, SOD, phagocytic activity, and IgM level were examined at 1, 2, and 3 weeks after injection. The differential expression of cytokines was observed after exposure to SA. IL-1β genes displayed significant expression at 2 and 8 h after exposure to 1–10 μg mL−1 of SA. SA also induced gene expression of cytokines such as MyD88, Mx1, and TNF-α. Furthermore, enhanced immune parameters in grass carp confirmed the immunomodulatory activity of SA. Interestingly, this compound has no toxic effect on CIHKM cells as tested by MTT assay. In addition, fish immunised with 10 μg mL−1 of SA exhibited maximum resistance against Aeromonas hydrophila infection. These results suggest that SA has the potential to stimulate immune responses in grass carp. PMID:27294155
Karaman, Kevser; Polat, Busra; Ozturk, Ismet; Sagdic, Osman; Ozdemir, Cihat
Eremurus spectabilis grows in the spring as a wild vegetable and for many years has been used both as a food or food additive and for therapeutic purposes. This study investigated the total phenolic content and the antimicrobial, antioxidant, and antiradical activities of methanol, ethanol, and aqueous extracts of E. spectabilis (obtained from the Antalya region of Turkey). In addition, volatile compounds of E. spectabilis were characterized by using gas chromatography/mass spectrometry. Major components of E. spectabilis volatile compounds were carvone (44.64%), carvacrol (14.45%), pentane, 2-methyl- (7.34%), (E)-caryophyllene (5.57%), valencene (5.11%), cis-calamenene (2.01%), cadalene (1.10%), and acetic acid (1.12%). The highest total phenolic content was seen with methanol extract (mean±standard deviation, 31.92 ± 0.48 mg gallic acid equivalents/g dry extract). The ethanol extract showed the highest antiradical activity, with a 50% inhibitory concentration of 35.14 μg/L in the 1,1-diphenyl-2- picrylhydrazyl assay. The strongest antioxidant activity was detected in methanol extract (81.72 ± 0.62 mg ascorbic acid equivalents/g). Twelve bacteria species were used to analyze the antimicrobial activity of extracts. The 1% concentrations of all extracts showed no inhibitive effect on any bacterium. The most resistant bacterium was Yersinia enterocolitica, and the most sensitive bacterium was Pseudomonas aeruginosa. A positive correlation was seen between concentrations and inhibition zones, and some differences occurred between antimicrobial activity of other concentrations.
Christensen, Lars P; Jensen, Martin
Fifty selected roots from a 7-year-old American ginseng (Panax quinquefolium L.) plant population grown in Denmark, with root weights varying from 191 to 490 g fresh weight (FW), were investigated for bioactive ginsenosides and polyacetylenes (PAs) in order to determine the correlation between the content of ginsenosides and PAs and root FW. PAs (falcarinol, panaxydol) and ginsenosides (Rb(1), Rb(2), Rb(3), Rc, Rd, Re, Rg(1)) were extracted from roots by sequential extraction with ethyl acetate and 80% methanol, respectively, and quantified in extracts by reverse-phase high-performance liquid chromatography (HPLC) using photodiode array detection. Total concentrations of PAs and ginsenosides varied between 150 and 780 mg/kg FW and 5,920 and 15,660 mg/kg FW, respectively. No correlation existed between the content of ginsenosides and PAs and root FW or between the total concentration of ginsenosides and PAs. Strong significant correlation was found between total content of ginsenosides and ginsenoside Rb(1) (r = 0.8190, P < 0.0001) and between total content of PAs and falcarinol (r = 0.9904, P < 0.0001). Based on the results of this study, it was concluded that it is possible to select large American ginseng roots for increased biomass production and concentration of bioactive ginsenosides and PAs without affecting the profile of bioactive compounds. Ginsenoside Rb(1) and falcarinol were found to be important selection parameters for identifying superior genotypes with the highest content of bioactive compounds.
Soquetta, Marcela Bromberger; Stefanello, Flávia Santi; Huerta, Katira da Mota; Monteiro, Sabrina Sauthier; da Rosa, Claudia Severo; Terra, Nelcindo Nascimento
The objective of this study was to analyze the physicochemical and microbiological properties, as well as the bioactive compounds, of flour made from the skin and bagasse of two varieties (Bruno and Monty) of kiwi fruit (Actinidia deliciosa) at two stages of maturation. The flour made with kiwi fruit peel from both varieties showed higher levels of bioactive compounds and antioxidant activity that the flour made with bagasse from both varieties. The flour made with green kiwi fruit skin from the Bruno variety had higher DPPH values and levels of phenolic compounds (1262.34 mg GAE/100g flour), while the Monty variety showed higher FRAP values, vitamin C (189.06 mg/100g flour), flavonoids (486.47 mg/100g flour), chlorophylls (12.13 mg/100g flour) and carotenoids (246.91 μg/100g flour). Flour made from kiwi fruit bagasse can be used to reduce agro-industrial waste. This flour is a promising ingredient which can be used to enrich products providing dietary fiber and bioactive compounds, as well as antioxidant action.
Sedaghat, Reza; Roghani, Mehrdad; Khalili, Mohsen
Parkinson disease (PD) is the most common movement disorder with progressive degeneration of midbrain dopaminergic neurons for which current treatments afford symptomatic relief with no-prevention of disease progression. Due to the neuroprotective property of the Nigella sativa bioactive compound thymoquinone (TQ), this study was undertaken to evaluate whether TQ could improve behavioral and cellular abnormalities and markers of oxidative stress in an experimental model of early PD in rat. Unilateral intrastriatal 6-hydroxydopamine (6-OHDA)-lesioned rats were daily pretreated p.o. with TQ at doses of 5 and/or 10 mg/Kg three times at an interval of 24 h. After 1 week, apomorphine caused contralateral rotations, a reduction in the number of neurons on the left side of the substantia nigra pars compacta (SNC) was observed, malondialdehyde (MDA) and nitrite level in midbrain homogenate increased and activity of superoxide dismutase (SOD) reduced in the 6-OHDA lesion group. TQ pretreatment significantly improved turning behavior, prevented loss of SNC neurons, and lowered level of MDA. These results suggest that TQ could afford neuroprotection against 6-OHDA neurotoxicity that is partly due to the attenuation of lipid peroxidation and this may provide benefits, along with other therapies, in neurodegenerative disorders including PD. PMID:24734075
Hwang, Eun-Sun; Thi, Nhuan Do
The objective of this study was to determine the effects of different growing regions on quality characteristics, total bioactive compound contents, and in vitro antioxidant activity in aronia. Aronia grown in 3 different regions (Sangjoo, Ulju, and Youngcheon) in Korea was obtained and used fresh or as a freeze-dried powder. No statistically significant differences were observed for moisture, ash, crude lipid, and crude protein contents in aronia sampled from the 3 different regions. Aronia grown in Sangjoo had the highest total acid content and the lowest sugar content and pH value. Conversely, aronia grown in Youngcheon possessed the lowest total acid content and the highest sugar content and pH value. Aronia grown in Sangjoo possessed relatively high levels of polyphenols, flavonoids, and anthocyanins, as well as high antioxidant activity in comparison with aronia produced in other regions. Aronia grown in Youngcheon scored the highest for taste and overall acceptability in sensory evaluations, which may be related to the high sugar content and pH, and the low total acidity of the fruits. It is possible that higher sugar contents and pH, and lower total acidity in the aronia grown in Youngcheon result in more preferable sensory characteristics. However, they also contain relatively low levels of total polyphenols, flavonoids, and anthocyanins, and have low antioxidant activity as measured by 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging assays. PMID:27752502
Hwang, Eun-Sun; Thi, Nhuan Do
The objective of this study was to determine the effects of different growing regions on quality characteristics, total bioactive compound contents, and in vitro antioxidant activity in aronia. Aronia grown in 3 different regions (Sangjoo, Ulju, and Youngcheon) in Korea was obtained and used fresh or as a freeze-dried powder. No statistically significant differences were observed for moisture, ash, crude lipid, and crude protein contents in aronia sampled from the 3 different regions. Aronia grown in Sangjoo had the highest total acid content and the lowest sugar content and pH value. Conversely, aronia grown in Youngcheon possessed the lowest total acid content and the highest sugar content and pH value. Aronia grown in Sangjoo possessed relatively high levels of polyphenols, flavonoids, and anthocyanins, as well as high antioxidant activity in comparison with aronia produced in other regions. Aronia grown in Youngcheon scored the highest for taste and overall acceptability in sensory evaluations, which may be related to the high sugar content and pH, and the low total acidity of the fruits. It is possible that higher sugar contents and pH, and lower total acidity in the aronia grown in Youngcheon result in more preferable sensory characteristics. However, they also contain relatively low levels of total polyphenols, flavonoids, and anthocyanins, and have low antioxidant activity as measured by 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging assays.
Lomarat, Pattamapan; Chancharunee, Sirirat; Anantachoke, Natthinee; Kitphati, Worawan; Sripha, Kittisak; Bunyapraphatsara, Nuntavan
The objective of this study was to evaluate the health benefits of plants used in Thai food, specifically Acacia pennata Willd., in Alzheimer's prevention. A. pennata twigs strongly inhibited β-amyloid aggregation. Bioactivity-guided separation of the active fractions yielded six known compounds, tetracosane (1), 1-(heptyloxy)-octadecane (2), methyl tridecanoate (3), arborinone (4), confertamide A (5) and 4-hydroxy-1-methyl-pyrrolidin-2-carboxylic acid (6). The structures were determined by spectroscopic analysis. Biological testing revealed that tetracosane (1) was the most potent inhibitor of β-amyloid aggregation, followed by 1-(heptyloxy)-octadecane (2) with IC50 values of 0.4 and 12.3 μM. Methyl tridecanoate (3), arborinone (4) and 4-hydroxy-1-methyl-pyrrolidin-2-carboxylic acid (6) moderately inhibited β-amyloid aggregation. In addition, tetracosane (1) and methyl tridecanoate (3) weakly inhibited acetylcholinesterase (AChE). These results suggested that the effect of A. pennata on Alzheimer's disease was likely due to the inhibition of β-amyloid aggregation. Thus A. pennata may be beneficial for Alzheimer's prevention.
Martínez-Esplá, Alejandra; Zapata, Pedro Javier; Valero, Daniel; García-Viguera, Cristina; Castillo, Salvador; Serrano, María
Trees of 'Sweet Heart' and 'Sweet Late' sweet cherry cultivars (Prunus avium L.) were treated with oxalic acid (OA) at 0.5, 1.0, and 2.0 mM at 98, 112, and 126 days after full blossom. Results showed that all treatments increased fruit size at harvest, manifested by higher fruit volume and weight in cherries from treated trees than from controls, the higher effect being found with 2.0 mM OA (18 and 30% higher weight for 'Sweet Heart' and 'Sweet Late', respectively). Other quality parameters, such as color and firmness, were also increased by OA treatments, although no significant differences were found in total soluble solids or total acidity, showing that OA treatments did not affect the on-tree ripening process of sweet cherry. However, the increases in total anthocyanins, total phenolics, and antioxidant activity associated with the ripening process were higher in treated than in control cherries, leading to fruit with high bioactive compounds and antioxidant potential at commercial harvest (≅45% more anthocyanins and ≅20% more total phenolics). In addition, individual anthocyanins, flavonols, and chlorogenic acid derivatives were also increased by OA treatment. Thus, OA preharvest treatments could be an efficient and natural way to increase the quality and functional properties of sweet cherries.
Akanni, E O; Adedeji, A L; Adedosu, O T; Olaniran, O I; Oloke, J K
Pharmacological exploitation of natural compounds has continued to lead to development of non-synthetic and non-toxic anticancer agents that are promising at ameliorating the menace of neoplastic diseases such as leukemia. This study is an attempt to determine the chemopreventive and antileukemic activities of ethanol extracts of Moringa oleifera leaves on benzene induced leukemia bearing rats. Leukemia was induced by intravenous injection of 0.2 mL benzene solution 48 hourly for 4 weeks in appropriate rat groups. Ethanol extract of Moringa oleifera (EMO) leaves was administered at 0.2 mL of 100 mg/mL to respective treatment rat groups. A standard antileukemic drug (cyclophosphamide) was also used to treat appropriate rat groups. Clinical examination of liver and spleen with hematological parameters were employed to assess the leukemia burden following analysis of the rat blood samples on Sysmex KX-21N automated instrument. Leukemia induction reflected in severe anemia and a marked leukocytosis over the control/baseline group. Liver and spleen enlargements were also observed in group exposed to benzene carcinogen. The in vivo antioxidative potential of EMO was evaluated using Malondialdehyde (MDA) and reduced glutathione (GSH) levels. The liver MDA and GSH levels obtained in benzene induced leukemic rats treated with EMO compared favorably with those obtained in similar treatments with the standard drug (p< 0.05). The extract demonstrated chemopreventive and anti-leukemic activities as much as the standard anti-leukemic drug (p>0.05) by ameliorating the induced leukemic condition in the affected rat groups owing to its bioactive constituents. This study reveals that the extract might be an active, natural and non-toxic anticancer drug lead.
Mace, Thomas A.; King, Samantha A.; Ameen, Zeenath; Elnaggar, Omar; Young, Gregory; Riedl, Kenneth M.; Schwartz, Steven J.; Clinton, Steven K.; Knobloch, Thomas J.; Weghorst, Christopher M.; Lesinski, Gregory B.
Bioactive phyotochemicals from natural products, such as black raspberries (BRB; Rubus occidentalis) have direct anti-cancer properties on malignant cells in culture and in xenograft models. BRB components inhibit cancer progression in more complex rodent carcinogenesis models. Although mechanistic targets for BRB phytochemicals in cancer cells are beginning to emerge, the potential role in modulating host immune processes impacting cancer have not been systematically examined. We hypothesized that BRB contain compounds capable of eliciting potent immunomodulatory properties that impact cellular mediators relevant to chronic inflammation and tumor progression. We studied both an ethanol extract from black raspberries (BRB-E) containing a diverse mixture of phytochemicals and two abundant phytochemical metabolites of BRB produced upon ingestion (Cyanidin-3-Rutinoside, C3R; Quercitin-3-Rutinoside, Q3R). BRB-E inhibited proliferation and viability of CD3/CD28 activated human CD4+ and CD8+ T lymphocytes. BRB-E also limited in vitro expansion of myeloid-derived suppressor cells (MDSC) and their suppressive capacity. Pre-treatment of immune cells with BRB-E attenuated IL-6-mediated phosphorylation of signal transducer and activator of transcription-3 (STAT3) and IL-2 induced STAT5 phosphorylation. In contrast, pre-treatment of immune cells with the C3R and Q3R metabolites inhibited MDSC expansion, IL-6-mediated STAT3 signaling, but not IL-2 induced STAT5 phosphorylation and were less potent inhibitors of T cell viability. Together these data indicate that BRB extracts and their physiologically-relevant metabolites contain phytochemicals that affect immune processes relevant to carcinogenesis and immunotherapy. Furthermore, specific BRB components and their metabolites may be a source of lead compounds for drug development that exhibit targeted immunological outcomes or inhibition of specific STAT-regulated signaling pathways. PMID:24893859
Mace, Thomas A; King, Samantha A; Ameen, Zeenath; Elnaggar, Omar; Young, Gregory; Riedl, Kenneth M; Schwartz, Steven J; Clinton, Steven K; Knobloch, Thomas J; Weghorst, Christopher M; Lesinski, Gregory B
Bioactive phytochemicals from natural products, such as black raspberries (BRB; Rubus occidentalis), have direct anticancer properties on malignant cells in culture and in xenograft models. BRB components inhibit cancer progression in more complex rodent carcinogenesis models. Although mechanistic targets for BRB phytochemicals in cancer cells are beginning to emerge, the potential role in modulating host immune processes impacting cancer have not been systematically examined. We hypothesized that BRB contain compounds capable of eliciting potent immunomodulatory properties that impact cellular mediators relevant to chronic inflammation and tumor progression. We studied both an ethanol extract from black raspberries (BRB-E) containing a diverse mixture of phytochemicals and two abundant phytochemical metabolites of BRB produced upon ingestion (Cyanidin-3-Rutinoside, C3R; Quercitin-3-Rutinoside, Q3R). BRB-E inhibited proliferation, and viability of CD3/CD28 activated human CD4(+) and CD8(+) T lymphocytes. BRB-E also limited in vitro expansion of myeloid-derived suppressor cells (MDSC) and their suppressive capacity. Pre-treatment of immune cells with BRB-E attenuated IL-6-mediated phosphorylation of signal transducer and activator of transcription-3 (STAT3) and IL-2-induced STAT5 phosphorylation. In contrast, pre-treatment of immune cells with the C3R and Q3R metabolites inhibited MDSC expansion, IL-6-mediated STAT3 signaling, but not IL-2-induced STAT5 phosphorylation and were less potent inhibitors of T cell viability. Together these data indicate that BRB extracts and their physiologically relevant metabolites contain phytochemicals that affect immune processes relevant to carcinogenesis and immunotherapy. Furthermore, specific BRB components and their metabolites may be a source of lead compounds for drug development that exhibits targeted immunological outcomes or inhibition of specific STAT-regulated signaling pathways.
dos Santos Ferreira, Rosângela; de Cássia Avellaneda Guimarães, Rita; Jardim Cury Pontes, Elenir Rose; Aragão do Nascimento, Valter; Aiko Hiane, Priscila
Cardiovascular events due to decompensated lipid metabolism are commonly found in Human Immunodeficiency Virus/Acquired Immunodeficiency Syndrome (HIV/AIDS) patients using anti-retroviral therapy (HAART). Thus, the aim of this study was to identify the effect of a bioactive food compound (BFC) containing functional foods on individuals with HIV undergoing HAART. Particularly, this study aims to verify the clinical outcome in the change of the lipid profile due to the use of this compound. This study includes 115 individuals with HIV on HAART. All patients received dietary guidelines; however, sixty-one consumed BFC while fifty-one did not (NO BFC). Biochemical examinations and socio-demographic and clinical profiles were evaluated. As result, in patients using hypolipidemic and/or hypoglycemic drugs, there was 28.6% decrease in triglyceride levels (p < 0.001) in the NO BFC group, and 18.3% reduction in low density lipoprotein cholesterol (LDL-C) (p < 0.001) in the BFC group. In patients who did not use hypolipidemic and/or hypoglycemic drugs in the NO BFC group, there was 30.6% increase in triglycerides, 11.3% total cholesterol and 15.3% LDL-C levels (p < 0.001) while for the BFC group there was 4.5% reduction in total cholesterol (p < 0.001). In conclusion, this study evidenced that the dietary intervention containing BFC positively affected in lipid control, since these HIV/AIDS patients using HAART are more vulnerable to lipid disorders. PMID:27740592
Caprioli, Giovanni; Fiorini, Dennis; Maggi, Filippo; Nicoletti, Marcello; Ricciutelli, Massimo; Toniolo, Chiara; Prosper, Biapa; Vittori, Sauro; Sagratini, Gianni
Analysis of the complex composition of cocoa beans provides fundamental information for evaluating the quality and nutritional aspects of cocoa-based food products, nutraceuticals and supplements. Cameroon, the world's fourth largest producer of cocoa, has been defined as "Africa in miniature" because of the variety it habitats. In order to evaluate the nutritional characteristics of cocoa beans from five different regions of Cameroon, we studied their polyphenolic content, volatile compounds and fatty acids composition. The High Performance Thin Layer Chromatography (HPTLC) analysis showed that the Mbalmayo sample had the highest content of theobromine (11.6 mg/g) and caffeic acid (2.1 mg/g), while the Sanchou sample had the highest level of (-)-epicatechin (142.9 mg/g). Concerning fatty acids, the lowest level of stearic acid was found in the Mbalmayo sample while the Bertoua sample showed the highest content of oleic acid. Thus, we confirmed that geographical origin influences the quality and nutritional characteristics of cocoa from these regions of Cameroon.
Gaínza, Yousmel Alemán; Fantatto, Rafaela Regina; Chaves, Francisco Celio Maia; Bizzo, Humberto Ribeiro; Esteves, Sérgio Novita; Chagas, Ana Carolina de Souza
The anthelminthic activity of the essential oil (EO) of Piper aduncum L. was tested in vitro on eggs and larvae of resistant (Embrapa2010) and susceptible (McMaster) isolates of Haemonchus contortus. The EO was obtained by steam distillation and its components identified by chromatography. EO concentrations of 12.5 to 0.02 mg/mL were used in the egg hatch test (EHT) and concentrations of 3.12 to 0.01 mg/mL in the larval development test (LDT). Inhibition concentrations (IC) were determined by the SAS Probit procedure, and significant differences assessed by ANOVA followed by Tukey's test. In the EHT, the IC50 for the susceptible isolate was 5.72 mg/mL. In the LDT, the IC50 and IC90 were, respectively, 0.10 mg/mL and 0.34 mg/mL for the susceptible isolate, and 0.22 mg/mL and 0.51 mg/mL for the resistant isolate. The EO (dillapiole 76.2%) was highly efficacious on phase L1. Due to the higher ICs obtained for the resistant isolate, it was raised the hypothesis that dillapiole may have a mechanism of action that resembles those of other anthelmintic compounds. We further review and discuss studies, especially those conducted in Brazil, that quantified the major constituents of P. aduncum-derived EO.
Srinivas, K; King, J W; Monrad, J K; Howard, L R; Hansen, C M
Process engineering operations in food and nutraceutical industries pertaining to the design of extraction of value-added products from biomass using pressurized liquids involve a careful selection of the solvent and optimal temperature conditions to achieve maximum yield. Complex molecular structure and limited physical property data in the literature of biological solutes extracted from biomass compounds have necessitated the process modeling of such operations. In this study, we have applied the Hansen 3-dimensional solubility parameter concept to optimize the extraction of molecularly complex solutes using subcritical fluid solvents. Hansen solubility spheres characterized by the relative energy differences (RED) have been used to characterize and quantify the solute-subcritical solvent interactions as a function of temperature. The solvent power of subcritical water and compressed hydroethanolic mixtures above their boiling points has been characterized using the above-mentioned method. The use of group contribution methods in collaboration with computerized algorithms to plot the Hansen spheres provides a quantitative prediction tool for optimizing the design of extraction conditions. The method can be used to estimate conditions for solute-solvent miscibility, an optimum temperature range for conducting extractions under pressurized conditions, and approximate extraction conditions of solutes from natural matrices.
Ahmed, Fouad A; Ali, Rehab F M
Brassica species are very rich in health-promoting phytochemicals, including phenolic compounds, vitamin C, and minerals. The objective of this study was to investigate the effect of different blanching (i.e., water and steam) and cooking (i.e., water boiling, steam boiling, microwaving, and stir-frying) methods on the nutrient components, phytochemical contents (i.e., polyphenols, carotenoids, flavonoid, and ascorbic acid), antioxidant activity measured by DPPH assay, and phenolic profiles of white cauliflower. Results showed that water boiling and water blanching processes had a great effect on the nutrient components and caused significant losses of dry matter, protein, and mineral and phytochemical contents. However, steam treatments (blanching and cooking), stir-frying, and microwaving presented the lowest reductions. Methanolic extract of fresh cauliflower had significantly the highest antioxidant activity (68.91%) followed by the extracts of steam-blanched, steam-boiled, stir-fried, and microwaved cauliflower 61.83%, 59.15%, 58.93%, and 58.24%, respectively. HPLC analysis revealed that the predominant phenolics of raw cauliflower were protocatechuic acid (192.45), quercetin (202.4), pyrogallol (18.9), vanillic acid (11.90), coumaric acid (6.94), and kaempferol (25.91) mg/100 g DW, respectively.
Twelve questions concerning tannin selected from questions raised by other workers on the author's research were picked up. The answers of each question are as follows. 1. What is tannin?--the differences between the old concept and the new definition of tannin. 2. Is tannic acid the same as tannin? 3. How could each tannin be analyzed as a pure compound? 4. Which tannin found in recent years is implicated with the change of the concept of tannin in medicinal plants? 5. Is it possible that one to several chemical structures represent tannins contained in each plant species? 6. Which tannin-containing plants met in the human life are rich in tannins? 7. Is tannin produced by all species of plants?--a correlation between the occurrence of hydrolyzable tannins and the plant evolution system. 8. When and where are the hydrolyzable tannin oligomers produced, in the plant or after extraction? 9. Are tannins bound to other substances in the plants? 10. Is it appropriate to call tannins "plant polyphenols"? 11. Is it true that tannins are inhibitors of enzymes? 12. What kind of biological activities have been found for tannins.
Ahmed, Fouad A.; Ali, Rehab F. M.
Brassica species are very rich in health-promoting phytochemicals, including phenolic compounds, vitamin C, and minerals. The objective of this study was to investigate the effect of different blanching (i.e., water and steam) and cooking (i.e., water boiling, steam boiling, microwaving, and stir-frying) methods on the nutrient components, phytochemical contents (i.e., polyphenols, carotenoids, flavonoid, and ascorbic acid), antioxidant activity measured by DPPH assay, and phenolic profiles of white cauliflower. Results showed that water boiling and water blanching processes had a great effect on the nutrient components and caused significant losses of dry matter, protein, and mineral and phytochemical contents. However, steam treatments (blanching and cooking), stir-frying, and microwaving presented the lowest reductions. Methanolic extract of fresh cauliflower had significantly the highest antioxidant activity (68.91%) followed by the extracts of steam-blanched, steam-boiled, stir-fried, and microwaved cauliflower 61.83%, 59.15%, 58.93%, and 58.24%, respectively. HPLC analysis revealed that the predominant phenolics of raw cauliflower were protocatechuic acid (192.45), quercetin (202.4), pyrogallol (18.9), vanillic acid (11.90), coumaric acid (6.94), and kaempferol (25.91) mg/100 g DW, respectively. PMID:24171164
Rodríguez-Meizoso, I; Jaime, L; Santoyo, S; Señoráns, F J; Cifuentes, A; Ibáñez, E
In this work, extraction and characterization of compounds with antioxidant and antimicrobial activity from Haematococcus pluvialis microalga in red phase have been carried out. To do this, subcritical water extraction (SWE) has been combined with analytical techniques such as HPLC-DAD, HPLC-QqQ-MS and GC-MS and in vitro assays (i.e., for antioxidant and antimicrobial activity). The effect of the extraction temperature (50, 100, 150 and 200 degrees C) and solvent polarity has been studied in terms of yield and activity of the extracts. Results demonstrate that the extraction temperature has a positive influence in the extraction yield and antioxidant activity. Thus, the extraction yield achieved with this process was higher than 30% of dry weight at 200 degrees C as extraction temperature. Moreover, the extract obtained at 200 degrees C presented the highest antioxidant activity by far, while temperature does not seem to significatively affect the antimicrobial activity. Chemical composition was determined by HPLC-DAD, HPLC-QqQ-MS and GC-MS. Short chain fatty acids turned out to be responsible of the antimicrobial activity, whereas the antioxidant activity was correlated to vitamin E (present exclusively in the 200 degrees C extract), together with simple phenols, caramelization products and possible Maillard reaction products obtained during the extraction at high temperatures.
Meillisa, Aviannie; Woo, Hee-Chul; Chun, Byung-Soo
Polysaccharides are the major components of brown seaweed, accounting for approximately 40-65% of the total mass. The majority of the brown seaweed polysaccharides consists of alginate (40% of dry matter), a linear hetero-polysaccharides commonly developed in fields. However, depolymerisation of alginate is required to recover high-value compounds. In this report, depolymerisation was performed using subcritical water hydrolysis (SWH) at 180-260°C, with a ratio of material to water of 1:25 (w/v) and 1% formic acid as a catalyst. Sugar recovery was higher at low temperatures in the presence of catalyst. The antioxidant properties of Saccharina japonica showed the best activity at 180°C in the presence of a catalyst. The mass spectra produced using MALDI-TOF showed that polysaccharides and oligosaccharides were produced during hydrothermal treatment. Hydrolysis treatment at 180°C in the presence of a catalyst may be useful for modifying the structure of S. japonica and purified alginate.
Troina, A A; Figueiredo, M S; Passos, M C F; Reis, A M; Oliveira, E; Lisboa, P C; Moura, E G
We evaluated maternal intake of SDG (secoisolariciresinol diglucoside), a compound from flaxseed, and flaxseed oil+SDG on biochemical and hormonal parameters of dams and male and female offspring during lactation. Dams were fed a standard diet (C); diet added 40 mg of SDG/100g diet (SDG) or diet added 40 mg of SDG/100g diet and 7% of flaxseed oil (OLSDG). SDG and OLSDG dams showed hyperprolactinemia. The OLSDG milk had lower lactose and protein, while the SDG milk had lower protein on the 14th day of lactation. At 14 days, OLSDG male and female pups showed lower body mass, SDG and OLSDG male pups had hypoprolactinemia and lower body fat mass, but higher visceral fat mass (VFM) and hypertriglyceridemia. At 21 days, male SDG and OLSDG presented hypotriglyceridemia. At 14 days, SDG and OLSDG female offspring showed higher serum 17-β estradiol (E2); OLSDG presented hypercholesterolemia and SDG presented hypertriglyceridemia. At 21 days, SDG and OLSDG female pups showed hypotriglyceridemia and OLSDG shower lower E2. Both maternal treatments changes maternal metabolism as well as hormonal and biochemical parameters of the offspring, which are gender-dependent. Maternal hyperprolactinemia may act as an imprint factor responsible for the hormonal and metabolic changes observed in the pups.
Kazumura, Kimiko; Sato, Yukiko; Satozono, Hiroshi; Koike, Takashi; Tsuchiya, Hiroshi; Hiramatsu, Mitsuo; Katsumata, Masakazu; Okazaki, Shigetoshi
We have developed a measuring system for simultaneous monitoring of chemiluminescence and fluorescence, which indicate respectively, (i) generation of superoxide anion radicals (O2(-•)) and (ii) change in the intracellular calcium ion concentration ([Ca(2+)]i) of neutrophils triggered by the mechanism of innate immune response. We applied this measuring system for establishing a method to distinguish between anti-inflammatory actions and antioxidant actions caused by bioactive compounds. We evaluated anti-inflammatory agents (zinc ion [Zn(2+)] and ibuprofen) and antioxidants (superoxide dismutase [SOD] and ascorbic acid). It was shown that ibuprofen and Zn(2+) were anti-inflammatory while SOD and ascorbic acid were anti-oxidative. We conclude that it is possible to determine the mechanism of action of bioactive compounds using this method.
Enman, Josefine; Hodge, David; Berglund, Kris A; Rova, Ulrika
Fruit bodies and mycelia of shiitake mushroom ( Lentinus edodes) have been shown to contain the cholesterol-reducing compound eritadenine, 2( R),3( R)-dihydroxy-4-(9-adenyl)butyric acid. In the search for a production method for eritadenine, shiitake mycelia were investigated in the present study. The mycelia were cultivated both in shake flasks and in bioreactors, to investigate the effects of pH, stirring rate, and reactor type on the production and distribution of eritadenine. Both the biomass and the culture broth were examined for their eritadenine content. In the shake flasks, the final concentration of eritadenine was 1.76 mg/L and eritadenine was equally distributed between the mycelia and the growth media. In the bioreactors, the shiitake mycelia were found to contain eritadenine in relatively low levels, whereas the majority, 90.6-98.9%, was detected in the growth media. Applying a stirring rate of 250 rpm during bioreactor cultivation resulted in the highest eritadenine concentrations: 10.23 mg/L when the pH was uncontrolled and 9.59 mg/L when the pH was controlled at 5.7. Reducing the stirring rate to 50 rpm resulted in a decreased eritadenine concentration, both at pH 5.7 (5.25 mg/L) and when pH was not controlled (5.50 mg/L). The mycelia in the shake flask cultures appeared as macroscopic aggregates, whereas mycelia cultivated in bioreactors grew more as freely dispersed filaments. This study demonstrates for the first time the extra- and intracellular distribution of eritadenine produced by shiitake mycelial culture and the influence of reactor conditions on the mycelial morphology and eritadenine concentrations.
Milaneze, Bárbara A.; Oliveira, Jairo P.; Augusto, Ingrid; Keijok, Wanderson J.; Côrrea, Andressa S.; Ferreira, Débora M.; Nunes, Otalíbio C.; Gonçalves, Rita de Cássia R.; Kitagawa, Rodrigo R.; Celante, Vinícius G.; da Silva, André Romero; Pereira, Ana Claudia H.; Endringer, Denise C.; Schuenck, Ricardo P.; Guimarães, Marco C. C.
The development of new routes and strategies for nanotechnology applications that only employ green synthesis has inspired investigators to devise natural systems. Among these systems, the synthesis of gold nanoparticles using plant extracts has been actively developed as an alternative, efficient, cost-effective, and environmentally safe method for producing nanoparticles, and this approach is also suitable for large-scale synthesis. This study reports reproducible and completely natural gold nanocrystals that were synthesized using Virola oleifera extract. V. oleifera resin is rich in epicatechin, ferulic acid, gallic acid, and flavonoids (i.e., quercetin and eriodictyol). These gold nanoparticles play three roles. First, these nanoparticles exhibit remarkable stability based on their zeta potential. Second, these nanoparticles are functionalized with flavonoids, and third, an efficient, economical, and environmentally friendly mechanism can be employed to produce green nanoparticles with organic compounds on the surface. Our model is capable of reducing the resin of V. oleifera, which creates stability and opens a new avenue for biological applications. This method does not require painstaking conditions or hazardous agents and is a rapid, efficient, and green approach for the fabrication of monodisperse gold nanoparticles.
Al-Asmari, Abdulrahman Khazim; Albalawi, Sulaiman Mansour; Athar, Md Tanwir; Khan, Abdul Quaiyoom; Al-Shahrani, Hamoud; Islam, Mozaffarul
In this study we investigated the anti-cancer effect of Moringa oleifera leaves, bark and seed extracts. When tested against MDA-MB-231 and HCT-8 cancer cell lines, the extracts of leaves and bark showed remarkable anti-cancer properties while surprisingly, seed extracts exhibited hardly any such properties. Cell survival was significantly low in both cells lines when treated with leaves and bark extracts. Furthermore, a striking reduction (about 70–90%) in colony formation as well as cell motility was observed upon treatment with leaves and bark. Additionally, apoptosis assay performed on these treated breast and colorectal cancer lines showed a remarkable increase in the number of apoptotic cells; with a 7 fold increase in MD-MB-231 to an increase of several fold in colorectal cancer cell lines. However, no significant apoptotic cells were detected upon seeds extract treatment. Moreover, the cell cycle distribution showed a G2/M enrichment (about 2–3 fold) indicating that these extracts effectively arrest the cell progression at the G2/M phase. The GC-MS analyses of these extracts revealed numerous known anti-cancer compounds, namely eugenol, isopropyl isothiocynate, D-allose, and hexadeconoic acid ethyl ester, all of which possess long chain hydrocarbons, sugar moiety and an aromatic ring. This suggests that the anti-cancer properties of Moringa oleifera could be attributed to the bioactive compounds present in the extracts from this plant. This is a novel study because no report has yet been cited on the effectiveness of Moringa extracts obtained in the locally grown environment as an anti-cancer agent against breast and colorectal cancers. Our study is the first of its kind to evaluate the anti-malignant properties of Moringa not only in leaves but also in bark. These findings suggest that both the leaf and bark extracts of Moringa collected from the Saudi Arabian region possess anti-cancer activity that can be used to develop new drugs for treatment of
Al-Asmari, Abdulrahman Khazim; Albalawi, Sulaiman Mansour; Athar, Md Tanwir; Khan, Abdul Quaiyoom; Al-Shahrani, Hamoud; Islam, Mozaffarul
In this study we investigated the anti-cancer effect of Moringa oleifera leaves, bark and seed extracts. When tested against MDA-MB-231 and HCT-8 cancer cell lines, the extracts of leaves and bark showed remarkable anti-cancer properties while surprisingly, seed extracts exhibited hardly any such properties. Cell survival was significantly low in both cells lines when treated with leaves and bark extracts. Furthermore, a striking reduction (about 70-90%) in colony formation as well as cell motility was observed upon treatment with leaves and bark. Additionally, apoptosis assay performed on these treated breast and colorectal cancer lines showed a remarkable increase in the number of apoptotic cells; with a 7 fold increase in MD-MB-231 to an increase of several fold in colorectal cancer cell lines. However, no significant apoptotic cells were detected upon seeds extract treatment. Moreover, the cell cycle distribution showed a G2/M enrichment (about 2-3 fold) indicating that these extracts effectively arrest the cell progression at the G2/M phase. The GC-MS analyses of these extracts revealed numerous known anti-cancer compounds, namely eugenol, isopropyl isothiocynate, D-allose, and hexadeconoic acid ethyl ester, all of which possess long chain hydrocarbons, sugar moiety and an aromatic ring. This suggests that the anti-cancer properties of Moringa oleifera could be attributed to the bioactive compounds present in the extracts from this plant. This is a novel study because no report has yet been cited on the effectiveness of Moringa extracts obtained in the locally grown environment as an anti-cancer agent against breast and colorectal cancers. Our study is the first of its kind to evaluate the anti-malignant properties of Moringa not only in leaves but also in bark. These findings suggest that both the leaf and bark extracts of Moringa collected from the Saudi Arabian region possess anti-cancer activity that can be used to develop new drugs for treatment of breast
Chen, B; Greenside, P; Paik, H; Sirota, M; Hadley, D; Butte, A J
A central premise in systems pharmacology is that structurally similar compounds have similar cellular responses; however, this principle often does not hold. One of the most widely used measures of cellular response is gene expression. By integrating gene expression data from Library of Integrated Network-based Cellular Signatures (LINCS) with chemical structure and bioactivity data from PubChem, we performed a large-scale correlation analysis of chemical structures and gene expression profiles of over 11,000 compounds taking into account confounding factors such as biological conditions (e.g., cell line, dose) and bioactivities. We found that structurally similar compounds do indeed yield similar gene expression profiles. There is an ∼20% chance that two structurally similar compounds (Tanimoto Coefficient ≥ 0.85) share significantly similar gene expression profiles. Regardless of structural similarity, two compounds tend to share similar gene expression profiles in a cell line when they are administrated at a higher dose or when the cell line is sensitive to both compounds.
Oskoueian, Ehsan; Abdullah, Norhani; Hendra, Rudi; Karimi, Ehsan
Evaluation of abundantly available agro-industrial by-products for their bioactive compounds and biological activities is beneficial in particular for the food and pharmaceutical industries. In this study, rapeseed meal, cottonseed meal and soybean meal were investigated for the presence of bioactive compounds and antioxidant, anti-inflammatory, xanthine oxidase and tyrosinase inhibitory activities. Methanolic extracts of rapeseed meal showed significantly (P < 0.01) higher phenolics and flavonoids contents; and significantly (P < 0.01) higher DPPH and nitric oxide free radical scavenging activities when compared to that of cottonseed meal and soybean meal extracts. Ferric thiocyanate and thiobarbituric acid tests results showed rapeseed meal with the highest antioxidant activity (P < 0.01) followed by BHT, cotton seed meal and soybean meal. Rapeseed meal extract in xanthine oxidase and tyrosinase inhibitory assays showed the lowest IC(50) values followed by cottonseed and soybean meals. Anti-inflammatory assay using IFN-γ/LPS stimulated RAW 264.7 cells indicated rapeseed meal is a potent source of anti-inflammatory agent. Correlation analysis showed that phenolics and flavonoids were highly correlated to both antioxidant and anti-inflammatory activities. Rapeseed meal was found to be promising as a natural source of bioactive compounds with high antioxidant, anti-inflammatory, xanthine oxidase and tyrosinase inhibitory activities in contrast to cotton and soybean meals.
Bae, Haejin; Jayaprakasha, G K; Jifon, John; Patil, Bhimanagouda S
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.
Górnaś, Paweł; Rudzińska, Magdalena; Raczyk, Marianna; Mišina, Inga; Segliņa, Dalija
Lipophilic bioactive compounds in oils recovered from the kernels of seven sweet cherry (Prunus avium L.) cultivars, harvested at single location in 2013, were studied. Oil yield in sweet cherry ranged between 30.3-40.3 % (w/w) dw. The main fatty acids were oleic acid (39.62-49.92 %), linoleic acid (31.13-38.81 %), α-eleostearic acid (7.23-10.73 %) and palmitic acid (5.59-7.10 %), all four represented approximately 95 % of the total detected fatty acids. The ranges of total tocochromanols and sterols were between 83.1-111.1 and 233.6-419.4 mg/100 g of oil, respectively. Regardless of the cultivar, the γ-tocopherol and β-sitosterol were the main lipophilic minor bioactive compounds. The content of the carotenoids and squalene were between 0.38-0.62 and 60.9-127.7 mg/100 g of oil, respectively. Three significant correlations were found between oil yield and total contents of sterols (r = -0.852), tocochromanols (r = -0.880) and carotenoids (r = -0.698) in sweet cherry kernel oils. The oil yield, as well as the content of lipophilic bioactive compounds in oil was significantly affected by the cultivar.
Liang, Zeng-Chin; Liang, Chih-Hung; Wu, Chiu-Yeh
In this study, several grains such as brown rice (Br), plumule rice (Pr), wheat (W) and pearl barley (Pb) supplemented with 1% (w/w) peptone (P), yeast extract (Ye), ammonia sulfate (As), and monosodium glutamate (Mg) as a nitrogen source, respectively, were used to produce fruiting bodies and bioactive compounds of two strains of Cordyceps militaris. Among these grain substrates, the substrate most suitable to mycelial growth was Pb+Ye for C. militaris H and L. The mushroom strains colonized this substrate in 12.8 and 12.6 days, respectively. For C. militaris L, the fewest days were required for primordial initiation on Br+Ye and Pr+P substrates. The highest yield and biological efficiency was observed with Pb substrate (25.16 g/bottle and 87.36%) and Br+P substrate (21.84 g/bottle and 75.83%) for C. militaris H and L, respectively. In the fruiting bodies of C. militaris H, the highest cordycepin content was cultivated on W+Mg substrate (25.07 mg/g), the highest mannitol content was cultivated with Pr+Mg (153.21 mg/g) and Pr (151.65 mg/g) substrates, and the highest adenosine content was cultivated with Pr+Ye (0.94 mg/g) and Pb+Ye (0.90 mg/g) substrates. In the fruiting bodies of C. militaris L, the highest cordycepin content was cultivated with W+Mg substrate (22.14 mg/g); the highest mannitol content was cultivated with Pb substrate (189.33 mg/g); and the highest adenosine content was cultivated with Pb+Ye substrate (0.71 mg/g).
Trendafilova, Antoaneta; Jadranin, Milka; Gorgorov, Rossen; Stanilova, Marina
In vitro cultures were initiated from a single seed of Centaurea davidovii. Whole plantlets were regenerated and cultivated for several months on agar-solidified nutrient media differing by their composition: basal MS medium, MS medium supplemented with plant growth regulators, and liquid MS medium. Plantlets were ex vitro adapted and successfully acclimated to open-air conditions; flowering was observed in some individuals in the first summer, and mass flowering during the second summer. The contents of the total flavonoids and the total phenolic compounds were determined spectrophotometrically in the leaves of the in vitro plantlets cultured on different media, and then compared with those in the leaves of the wild plants and in the leaves of the acclimated plants of the field plot. The sesquiterpene lactone 8α-(5'-hydroxyangeloyl)-salonitenolide was determined by HPLC in leaf samples of C. davidovii wild plants, in vitro obtained plantlets and ex vitro acclimated plants in the greenhouse and on the experimental field plot. The composition of the nutrient medium influenced the contents of all studied bioactive substances. The highest concentrations of all tested secondary metabolites were detected in the leaves of the acclimated plants during mass flowering, the content of the lactone reaching 56.2 mg/g DW, which was several times more than in the other leaf samples. The obtained results revealed both the effectiveness of biotechnological methods for propagation and conservation of rare and endangered plant species, and the possibility to use C. davidovii plants ex vitro acclimated to field conditions as a source of secondary metabolites with potential biological activity.
El Anany, Ayman Mohammed
The purpose of this study was to explore the influences of roasting process on the nutritional composition and nutritive value, antinutritional factors, bioactive compounds and antioxidant activity of guava seeds. Roasting process caused significant (P ≤ 0.05) decreases in moisture content, crude protein, crude fiber, ash and mineral contents, isoleucine, arginine, glutamic and total aromatic and sulfur amino acids, antinutritional factors (tannins and phytic acid) and flavonoids, while oil content increased. Subjecting guava seeds to 150 °C for 10, 15 and 20 min increased the total essential amino acids from 35.19 g/100 g protein in the raw sample to 36.96, 37.30 and 37.47 g/100 g protein in roasted samples, respectively. Protein efficiency ratio (PER) of guava seeds roasted at 150 °C for 10, 15 and 20 min were about 1.08, 1.14 and 1.18 times as high as that in unroasted seeds. Lysine was the first limiting amino acid, while leucine was the second limiting amino acid in raw and roasted guava seeds. Total phenolic contents was significantly (P ≤ 0.05) increased by roasting at 150 °C for 10 min. However, roasting at 150 °C for 15 and 20 min caused significant decrease in the phenolic content of guava seeds. Guava seeds subjected to roasting process showed higher DPPH radical scavenging and reducing power activities.
Castillejo, Noelia; Martínez-Hernández, Ginés Benito; Monaco, Kamila; Gómez, Perla A; Aguayo, Encarna; Artés, Francisco; Artés-Hernández, Francisco
) showed better quality and bioactive compounds retention in a green fresh vegetable smoothie during low temperature storage.
Acuña-Avila, Pedro Estanislao; Vásquez-Murrieta, María Soledad; Franco Hernández, Marina Olivia; López-Cortéz, Ma del Socorro
The red grape Vitis vinífera is an important source of phenolic compounds, which can prevent disease if included as a part of a diet. The levels of these compounds in grapes have been associated with various environmental factors, such as climate, soil composition, and biotic stress. The purpose of this study was to determine the relationship between the elemental compositions of the soil and the grapes and the presence of bioactive compounds, such as catechin, epicatechin, piceid and resveratrol. Ethanol-based extracts of red grapes were used to quantify total and individual phenolic compounds by HPLC. It was observed that the elemental compositions of the soil and the grapes were related to their locations within different wine-producing regions. A principal component analysis showed a relationship between high metal content (Sr, Mn, Si and Pb) and higher concentrations of antioxidants in the grapes.
Carbonell-Capella, Juana M; Buniowska, Magdalena; Esteve, María J; Frígola, Ana
In order to determine the impact of Stevia rebaudiana (SR) addition on bioactive compounds bioaccessibility of a new developed functional beverage based on exotic fruits (mango juice, papaya juice and açaí) mixed with orange juice and oat, an in vitro gastrointestinal digestion was performed. Ascorbic acid, total carotenoids, total phenolics, total anthocyanins, total antioxidant capacity and steviol glycosides were evaluated before and after a simulated gastrointestinal digestion. Salivary and gastric digestion had no substantial effect on any of the major phenolic compounds, ascorbic acid, total antioxidant capacity and steviol glycosides, whereas carotenoids and anthocyanins diminished significantly during the gastric step. All analysed compounds were significantly altered during the pancreatic-bile digestion and this effect was more marked for carotenoids and total anthocyanins. However, phenolic compounds, anthocyanins, total antioxidant capacity and steviol glycosides bioaccessibility increased as did SR concentration. Ascorbic acid bioaccessibility was negatively affected by the SR addition.
Zengin, Gokhan; Bulut, Gizem; Mollica, Adriano; Haznedaroglu, Mehmet Zeki; Dogan, Ahmet; Aktumsek, Abdurrahman
This study presents the effects of the Achillea phrygia Boiss. et Bal. and Bupleurum croceum Fenzl. extracts obtained by different solvents (ethyl acetate, methanol and water) on selected enzyme inhibitory effects and antioxidant ability with screening bioactive compounds. Total and individual bioactive compounds were detected by spectrophotometric and HPLC-DAD techniques. Antioxidant abilities were evaluated by different methods including free radical scavenging (ABTS and DPPH), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating. Enzyme inhibitory effects were tested against cholinesterases, tyrosinase, amylase, glucosidase and lipase. Total phenolic contents were ranged from 20.52 mgGAE/g extract (B. croceum methanol extract) to 41.13 mgGAE/g extract (A. phrygia methanol extract). Generally, methanol and water extracts showed the strongest antioxidant abilities, while the ethyl acetate extracts had the most promising enzyme inhibitory effects. HPLC analysis revealed the abundance of some phenolics including rutin, quercetin, sinapic acid and chlorogenic acid, respectively. These components were also assessed using molecular modelling with the aim to study their docking properties on a set of six enzymes used in this study. Overall, these species could be suggested as valuable sources of natural-bioactive agents for developing new functional, pharmacological and health-promoting ingredients.
Hernández-Carrión, M; Vázquez-Gutiérrez, J L; Hernando, I; Quiles, A
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.
Arihara, Keizo; Ohata, Motoko
Since health-conscious consumers have made functional foods the leading trends in the food industry, efforts have been taken in many countries to develop new functional foods and to establish regulations for functional foods (Arihara, 2004; Dentali, 2002; Eve, 2000; Hutt, 2000). For example, in 1991, the concept of foods for specified health use (FOSHU) was established by the Japanese Ministry of Health and Welfare (Arihara, 2004, 2006b). FOSHU are foods that, based on the knowledge of the relationship between foods or food components and health, are expected to have certain health benefits and have been licensed to bear the label claiming that a person using them may expect to obtain that health use through the consumption of these foods. As of June 2008, 786 FOSHU products have been approved in Japan.
Pinaud, Fabien; King, David; Weiss, Shimon
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.
Iwata, Michio; Sawada, Ryusuke; Iwata, Hiroaki; Kotera, Masaaki; Yamanishi, Yoshihiro
The identification of the modes of action of bioactive compounds is a major challenge in chemical systems biology of diseases. Genome-wide expression profiling of transcriptional responses to compound treatment for human cell lines is a promising unbiased approach for the mode-of-action analysis. Here we developed a novel approach to elucidate the modes of action of bioactive compounds in a cell-specific manner using large-scale chemically-induced transcriptome data acquired from the Library of Integrated Network-based Cellular Signatures (LINCS), and analyzed 16,268 compounds and 68 human cell lines. First, we performed pathway enrichment analyses of regulated genes to reveal active pathways among 163 biological pathways. Next, we explored potential target proteins (including primary targets and off-targets) with cell-specific transcriptional similarity using chemical–protein interactome. Finally, we predicted new therapeutic indications for 461 diseases based on the target proteins. We showed the usefulness of the proposed approach in terms of prediction coverage, interpretation, and large-scale applicability, and validated the new prediction results experimentally by an in vitro cellular assay. The approach has a high potential for advancing drug discovery and repositioning. PMID:28071740
Vanajothi, Ramar; Srinivasan, Pappu
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.
Patathananone, Supawadee; Thammasirirak, Sompong; Daduang, Jureerut; Gung Chung, Jing; Temsiripong, Yosapong; Daduang, Sakda
Matrix metalloproteinases (MMPs) play a key role in cancer progression, including cell invasion, metastasis, cell growth, apoptosis, angiogenesis, and cell adhesion. Thus, suppression of the MMPs activities is crucial for inhibiting cancer cells metastasis. Herein, bioactive agents from crocodile (Crocodylus siamensis) leukocyte extracts (WBCex) showed the anticancer activity with HeLa cells and inhibited the migration and invasion process by reducing gelatinases (MMP-2, MMP-9) activity and their protein levels. This mechanism is regulated via interfering Ras and p38 signal transduction. Moreover, disrupting VEGF and integrin-signaling cascade by bioactive agents are the predictable mechanisms that cause the decreasing of MMP-2 and MMP-9 activity. Hence, bioactive substances in WBCex may play the mode of action similar with MMPs inhibitor due to HeLa cell metastasis being suppressed in vitro. © 2015 Wiley Periodicals, Inc. Environ Toxicol 31: 1329-1336, 2016.
Krishnan, Kannabiran; Mani, Abirami; Jasmine, Subashini
Marine Streptomyces are prolific producers of majority of bioactive secondary metabolites which are used in pharmaceutical industry as effective drugs against life threatening diseases. The cytotoxic activity of the pure compound 1, 2- benzene dicarboxylic acid, mono 2- ethylhexyl ester (DMEHE) from marine derived actinomycete Streptomyces sp. VITSJK8 was investigated against mouse embryonic fibroblast (NIH 3T3) and human keratinocyte (HaCaT) normal cell lines, human hepatocellular liver carcinoma (HepG 2) and human breast adenocarcinoma (MCF-7) cell lines by using MTT assay. The compound DMEHE exhibited IC 50 values of 42, 100, 250 and 500 µg/ ml against HepG2, MCF-7, HaCaT and NIH 3T3 cell lines, respectively. The effect of DMEHE on the growth of cancer cell lines was expressed as the % of viability. Cell viability was recorded as 67.7%, 78.14%, 82.23% and 96. 11% in HepG2, MCF-7, HaCaT and NIH 3T3 cells, respectively. The results of the study conclude that the bioactive compound isolated from the potential isolate Streptomyces sp. VITSJK8 exhibited cytotoxic activity against HepG2 and MCF- 7 cancer cell lines and low toxicity against normal HaCaT and NIH 3T3 cell lines.
Robles-Sánchez, R M; Islas-Osuna, M A; Astiazarán-García, H; Vázquez-Ortiz, F A; Martín-Belloso, O; Gorinstein, S; González-Aguilar, G A
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.
Krishnan, Kannabiran; Mani, Abirami; Jasmine, Subashini
Marine Streptomyces are prolific producers of majority of bioactive secondary metabolites which are used in pharmaceutical industry as effective drugs against life threatening diseases. The cytotoxic activity of the pure compound 1, 2- benzene dicarboxylic acid, mono 2- ethylhexyl ester (DMEHE) from marine derived actinomycete Streptomyces sp. VITSJK8 was investigated against mouse embryonic fibroblast (NIH 3T3) and human keratinocyte (HaCaT) normal cell lines, human hepatocellular liver carcinoma (HepG 2) and human breast adenocarcinoma (MCF-7) cell lines by using MTT assay. The compound DMEHE exhibited IC 50 values of 42, 100, 250 and 500 µg/ ml against HepG2, MCF-7, HaCaT and NIH 3T3 cell lines, respectively. The effect of DMEHE on the growth of cancer cell lines was expressed as the % of viability. Cell viability was recorded as 67.7%, 78.14%, 82.23% and 96. 11% in HepG2, MCF-7, HaCaT and NIH 3T3 cells, respectively. The results of the study conclude that the bioactive compound isolated from the potential isolate Streptomyces sp. VITSJK8 exhibited cytotoxic activity against HepG2 and MCF- 7 cancer cell lines and low toxicity against normal HaCaT and NIH 3T3 cell lines. PMID:25635251
Zhu, Hao; Liang, Qing-Hua; Xiong, Xin-Gui; Chen, Jiang; Wu, Dan; Yang, Bo; Zhang, Yang; Zhang, Yong; Huang, Xi
Objectives. This study aimed to identify the active compounds in Oldenlandia diffusa (OD) decoction and the compounds absorbed into plasma, and to determine whether the absorbed compounds derived from OD exerted any anti-inflammatory effects in rats with collagen induced arthritis (CIA). Methods. The UPLC-PDA (Ultra Performance Liquid Chromatography Photo-Diode Array) method was applied to identify the active compounds both in the decoction and rat plasma. The absorbable compound was administered to the CIA rats, and the effects were dynamically observed. X-ray films of the joints and HE stain of synovial tissues were analyzed. The levels of IL-1β and TNF-α in the rats from each group were measured by means of ELISA. The absorbed compound in the plasma of CIA rats was identified as ferulic acid (FA), following OD decoction administration. Two weeks after the administration of FA solution or OD decoction, the general conditions improved compared to the model group. The anti-inflammatory effect of FA was inferior to that of the OD decoction (P < 0.05), based on a comparison of IL-1β TNF-α levels. FA from the OD decoction was absorbed into the body of CIA rats, where it elicited anti-inflammatory responses in rats with CIA. Conclusions. These results suggest that FA is the bioactive compound in OD decoction, and FA exerts its effects through anti-inflammatory pathways. PMID:24883069
Biodiesel was prepared from the unconventional crude oil of Moringa oleifera by transesterification with methanol and alkali catalyst. Moringa oleifera oil is reported for the first time as potential feedstock for biodiesel. Moringa oleifera oil contains a high amount of oleic acid (>70%) with sat...
Shanmuganathan, Balakrishnan; Sheeja Malar, Dicson; Sathya, Sethuraman; Pandima Devi, Kasi
Inhibition of β-amyloid (Aβ) aggregation in the cerebral cortex of the brain is a promising therapeutic and defensive strategy in identification of disease modifying agents for Alzheimer’s disease (AD). Since natural products are considered as the current alternative trend for the discovery of AD drugs, the present study aims at the evaluation of anti-amyloidogenic potential of the marine seaweed Padina gymnospora. Prevention of aggregation and disaggregation of the mature fibril formation of Aβ 25–35 by acetone extracts of P. gymnospora (ACTPG) was evaluated in two phases by Thioflavin T assay. The results were further confirmed by confocal laser scanning microscopy (CLSM) analysis and Fourier transform infrared (FTIR) spectroscopic analysis. The results of antiaggregation and disaggregation assay showed that the increase in fluorescence intensity of aggregated Aβ and the co-treatment of ACTPG (250 μg/ml) with Aβ 25–35, an extensive decrease in the fluorescence intensity was observed in both phases, which suggests that ACTPG prevents the oligomers formation and disaggregation of mature fibrils. In addition, ACTPG was subjected to column chromatography and the bioactivity was screened based on the cholinesterase inhibitory activity. Finally, the active fraction was subjected to LC-MS/MS analysis for the identification of bioactive compounds. Overall, the results suggest that the bioactive compound alpha bisabolol present in the alga might be responsible for the observed cholinesterase inhibition with the IC50 value < 10 μg/ml for both AChE and BuChE when compared to standard drug donepezil (IC50 value < 6 μg/ml) and support its use for the treatment of neurological disorders. PMID:26536106
Belhadj, Feten; Somrani, Imen; Aissaoui, Neyssene; Messaoud, Chokri; Boussaid, Mohamed; Marzouki, M Nejib
Bioactive molecules from fruits of four varieties of Prunus persica at different stages of ripening (green, small orange, red) were studied. For example, contents on polyphenols (20.36mg GAE/g FW) and flavonoids (0.764mg RE/g FW) were high and varied according variety. The antioxidant activity, using four different tests (DPPH radical scavenging activity, reducing power, β carotene bleaching system and TBARS assay) showed that the variety Chatos exhibited the highest antioxidant activity comparing with others varieties. The antibacterial activity of Prunus persica varieties studied seems to be more sensitive against Staphylococcus aureus and Listeria monocytogenes. The capacity of peach DMSO extracts to inhibit Candida albicans growth was more pronounced, especially, in the presence of Chatos DMSO extract. Enzymes inhibition gives results which correlate with polyphenols, flavonoids and condensed tannins contents, and so, confirm the fascinating bioactivity of this fruit.
Wu, Chiu-Yeh; Liang, Zeng-Chin; Tseng, Chin-Yin; Hu, Shu-Hui
We investigated the effects of light intensity in the 3 cultivation stages separately-the mycelium colonization stage, the primordial initiation stage, and the fruiting stage (in order)-on fruiting body and bioactive compound production by Cordyceps militaris. In the mycelium colonization stage, rice substrates were incubated in a spawn running room at 23°C. During the primordial initiation stage, C. militaris was grown at 18°C and illuminated 12 hours/day. In the fruiting stage the temperature was 23°C, with illumination provided 12 hours/day. The highest fruiting body yield and biological efficiency were 4.06 g dry weight/bottle and 86.83%, respectively, under 1750 ± 250 lux during the second and third stages. The cordycepin content was highest during the second and third stages under 1250 ± 250 lux. The mannitol and polysaccharide contents were highest under 1250 ± 250 and 1750 ± 250 lux during the primordial initiation stage and the fruiting stage, respectively. Thus, with controlled lighting, C. militaris can be cultivated in rice-water medium to increase fruiting body yield and bioactive compound production.
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.
Pedro, Alessandra C; Moreira, Fernanda; Granato, Daniel; Rosso, Neiva D
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.
Nacoulma, Aminata P.; Vandeputte, Olivier M.; De Lorenzi, Manuella; El Jaziri, Mondher; Duez, Pierre
Leafy gall is a plant hyperplasia induced upon Rhodococcus fascians infection. Previously, by genomic and transcriptomic analysis, it has been reported that, at the early stage of symptom development, both primary and secondary metabolisms are modified. The present study is based on the hypothesis that fully developed leafy gall, could represent a potential source of new bioactive compounds. Therefore, non-targeted metabolomic analysis of aqueous and chloroform extracts of leafy gall and non-infected tobacco was carried out by 1H-NMR coupled to principal component analysis (PCA) and orthogonal projections to latent structures-discriminant analysis (OPLS-DA). Polar metabolite profiling reflects modifications mainly in the primary metabolites and in some polyphenolics. In contrast, main modifications occurring in non-polar metabolites concern secondary metabolites, and gas chromatography and mass spectrometry (GC-MS) evidenced alterations in diterpenoids family. Analysis of crude extracts of leafy galls and non-infected tobacco leaves exhibited a distinct antiproliferative activity against all four tested human cancer cell lines. A bio-guided fractionation of chloroformic crude extract yield to semi-purified fractions, which inhibited proliferation of glioblastoma U373 cells with IC50 between 14.0 and 2.4 μg/mL. Discussion is focused on the consequence of these metabolic changes, with respect to plant defense mechanisms following infection. Considering the promising role of diterpenoid family as bioactive compounds, leafy gall may rather be a propitious source for drug discovery. PMID:23771021
Kasapis, Stefan; Shrinivas, Preeti
An investigation of the diffusional mobility of a bioactive compound (caffeine) within a carbohydrate matrix (glucose syrup) at a glassy consistency is reported. The experimental temperature range was from 30 to - 70 degrees C, and the techniques of modulated differential scanning calorimetry, small-deformation dynamic oscillation on shear, and UV spectrometry were employed. It is not a straightforward matter to identify the relaxation dynamics of such a glassy matrix. This makes suggestions of the relationship between the structural properties of the matrix and the diffusional mobility of bioactive compounds reported earlier in the literature rather tenuous. To address this issue, we recorded mechanical spectra over the aforementioned temperature range and utilized the combined framework of the Williams, Landel, and Ferry (WLF) equation with the time-temperature superposition principle to rationalize results. The protocol produced a fundamental definition of the glass transition temperature and free volume parameters of the glucose syrup sample within the glass transition region. Results were related to the kinetic rates of caffeine diffusion derived by UV spectroscopy leading to the conclusion that the diffusional mobility of the chemical substance is independent of the carbohydrate matrix. This conclusion was further supported by the high level of fractional free volume of caffeine, which is congruent with the predictions of the reaction rate theory (modified Arrhenius equation), as compared to the collapsing levels of free volume in the glucose-syrup matrix that make appropriate WLF considerations.
Nacoulma, Aminata P; Vandeputte, Olivier M; De Lorenzi, Manuella; Jaziri, Mondher El; Duez, Pierre
Leafy gall is a plant hyperplasia induced upon Rhodococcus fascians infection. Previously, by genomic and transcriptomic analysis, it has been reported that, at the early stage of symptom development, both primary and secondary metabolisms are modified. The present study is based on the hypothesis that fully developed leafy gall, could represent a potential source of new bioactive compounds. Therefore, non-targeted metabolomic analysis of aqueous and chloroform extracts of leafy gall and non-infected tobacco was carried out by 1H-NMR coupled to principal component analysis (PCA) and orthogonal projections to latent structures-discriminant analysis (OPLS-DA). Polar metabolite profiling reflects modifications mainly in the primary metabolites and in some polyphenolics. In contrast, main modifications occurring in non-polar metabolites concern secondary metabolites, and gas chromatography and mass spectrometry (GC-MS) evidenced alterations in diterpenoids family. Analysis of crude extracts of leafy galls and non-infected tobacco leaves exhibited a distinct antiproliferative activity against all four tested human cancer cell lines. A bio-guided fractionation of chloroformic crude extract yield to semi-purified fractions, which inhibited proliferation of glioblastoma U373 cells with IC50 between 14.0 and 2.4 µg/mL. Discussion is focused on the consequence of these metabolic changes, with respect to plant defense mechanisms following infection. Considering the promising role of diterpenoid family as bioactive compounds, leafy gall may rather be a propitious source for drug discovery.
Ziegler, Valmor; Vanier, Nathan Levien; Ferreira, Cristiano Dietrich; Paraginski, Ricardo Tadeu; Monks, Jander Luis Fernandes; Elias, Moacir Cardoso
Soybean is a rich source of bioactive compounds, such as phenolic acids, flavonoids, isoflavones, carotenoids, and tocopherols. The amount of bioactive compounds in freshly harvested soybeans and their derived products has been determined; however, when they are used in the food industry, soybeans are generally stored prior to being processed. This study aimed to evaluate the effects of soybean moisture content (12%, 15%, and 18%) and storage temperature (11, 18, 25, and 32 °C) on the free phenolic, total flavonoid, vanillic acid, total carotenoid, and δ- and γ-tocopherol content of soybeans stored for 12 mo. Moreover, the ABTS and DPPH radical scavenging activities of phenolic extracts were determined. There was an increase in free phenolics and total flavonoids in the stored grains compared with the grains on the 1st d of storage. Vanillic acid showed a decrease in soybeans stored at 15% and 18% moisture content and 25 or 32 °C, which indicated some degradation into other metabolites. Total carotenoid content decreased as a function of storage temperature and showed some temperature-dependent degradation. The δ- and γ-tocopherol content also tended to decrease in grains stored at 15% or 18% moisture content or 25 or 32 °C, regardless of the moisture content studied.
González-Cebrino, Francisco; Durán, Rocío; Delgado-Adámez, Jonathan; Contador, Rebeca; Bernabé, Rosario Ramírez
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.
Moussa-Ayoub, Tamer E; Jaeger, Henry; Youssef, Khaled; Knorr, Dietrich; El-Samahy, Salah; Kroh, Lothar W; Rohn, Sascha
Selected technological characteristics and bioactive compounds of juice pressed directly from the mash of whole Opuntia dillenii cactus fruits have been investigated. The impact of pulsed electric fields (PEF) for a non-thermal disintegration on the important juice characteristics has been evaluated in comparison to microwave heating and use of pectinases. Results showed that the cactus juice exhibited desirable technological characteristics. Besides, it also contained a high amount of phenolic compounds being the major contributors to the overall antioxidant activity of juice. HPLC-DAD/ESI-MS(n) measurements in the fruits' peel and pulp showed that isorhamnetin 3-O-rutinoside was determined as the single flavonol found only in the fruit's peel. Treating fruit mash with a moderate electric field strength increased juice yield and improved juice characteristics. Promisingly, the highest release of isorhamnetin 3-O-rutinoside from fruit's peel into juice was maximally achieved by PEF.
Frankel, Edwin; Bakhouche, Abdelhakim; Lozano-Sánchez, Jesús; Segura-Carretero, Antonio; Fernández-Gutiérrez, Alberto
This review describes the olive oil production process to obtain extra virgin olive oil (EVOO) enriched in polyphenol and byproducts generated as sources of antioxidants. EVOO is obtained exclusively by mechanical and physical processes including collecting, washing, and crushing of olives, malaxation of olive paste, centrifugation, storage, and filtration. The effect of each step is discussed to minimize losses of polyphenols from large quantities of wastes. Phenolic compounds including phenolic acids, alcohols, secoiridoids, lignans, and flavonoids are characterized in olive oil mill wastewater, olive pomace, storage byproducts, and filter cake. Different industrial pilot plant processes are developed to recover phenolic compounds from olive oil byproducts with antioxidant and bioactive properties. The technological information compiled in this review will help olive oil producers to improve EVOO quality and establish new processes to obtain valuable extracts enriched in polyphenols from byproducts with food ingredient applications.
Ye, Yong; Xing, Haiting; Li, Yue
Sasanquasaponin, a bioactive compound isolated from seeds of Camellia oleifera, shows central effects in our previous research. In order to investigate its neuroprotective effects, a new kind of nanocapsule with photo responsiveness was designed to deliver sasanquasaponin into the brain and adjusted by red light. The nanocapsule was prepared using sasanquasaponin emulsified with soybean lecithin and cholesterol solution. The natural phaeophorbide from silkworm excrement as a photosensitizer was added in the lipid phase to make the nanocapsules photo responsive. The physicochemical properties of encapsulation efficiency, size distribution, morphology and stability were measured using high-performance liquid chromatography, particle size analyzer, transmission electron microscope, differential scanning calorimetry and thermogravimetry. Photo responsiveness was determined by the sasanquasaponin release in pH 7.5 phosphate buffer under the laser at 670 nm. The neuroprotective effects were evaluated by the expression of tyrosine hydroxylase (TH), decrease of inflammatory cytokines TNF-α and IL-1β in the brain, and amelioration of kainic acid-induced behavioral disorder in mice. The nanocapsules had higher encapsulation efficiency and stability when the phaeophorbide content was 2% of lecithin weight. The average size was 172.2 nm, distributed in the range of 142–220 nm. The phaeophorbide was scattered sufficiently in the outer lecithin layer of the nanocapsules and increased the drug release after irradiation. TH expression in brain tissues and locomotive activities in mice were reduced by kainic acid, but could be improved by the sasanquasaponin nanocapsules after tail vein injection with 15 minutes of irradiation at the nasal cavity. The sasanquasaponin took effect through inflammatory alleviation in central tissues. The sasanquasaponin nanocapsules with phaeophorbide have photo responsiveness and neuroprotective effects under the irradiation of red light. This
Ye, Yong; Xing, Haiting; Li, Yue
Sasanquasaponin, a bioactive compound isolated from seeds of Camellia oleifera, shows central effects in our previous research. In order to investigate its neuroprotective effects, a new kind of nanocapsule with photo responsiveness was designed to deliver sasanquasaponin into the brain and adjusted by red light. The nanocapsule was prepared using sasanquasaponin emulsified with soybean lecithin and cholesterol solution. The natural phaeophorbide from silkworm excrement as a photosensitizer was added in the lipid phase to make the nanocapsules photo responsive. The physicochemical properties of encapsulation efficiency, size distribution, morphology and stability were measured using high-performance liquid chromatography, particle size analyzer, transmission electron microscope, differential scanning calorimetry and thermogravimetry. Photo responsiveness was determined by the sasanquasaponin release in pH 7.5 phosphate buffer under the laser at 670 nm. The neuroprotective effects were evaluated by the expression of tyrosine hydroxylase (TH), decrease of inflammatory cytokines TNF-α and IL-1β in the brain, and amelioration of kainic acid-induced behavioral disorder in mice. The nanocapsules had higher encapsulation efficiency and stability when the phaeophorbide content was 2% of lecithin weight. The average size was 172.2 nm, distributed in the range of 142-220 nm. The phaeophorbide was scattered sufficiently in the outer lecithin layer of the nanocapsules and increased the drug release after irradiation. TH expression in brain tissues and locomotive activities in mice were reduced by kainic acid, but could be improved by the sasanquasaponin nanocapsules after tail vein injection with 15 minutes of irradiation at the nasal cavity. The sasanquasaponin took effect through inflammatory alleviation in central tissues. The sasanquasaponin nanocapsules with phaeophorbide have photo responsiveness and neuroprotective effects under the irradiation of red light. This
Cui, Yulei; Shen, Na; Yuan, Xiang; Dang, Jun; Shao, Yun; Mei, Lijuan; Tao, Yanduo; Wang, Qilan; Liu, Zenggen
Traditional Tibetan medicine is important for discovery of drug precursors. However, information about the chemical composition of traditional Tibetan medicine is very limited due to the lack of appropriate chromatographic purification methods. In the present work, A. kansuensis was taken as an example and a novel two-dimensional reversed-phase/hydrophilic interaction liquid chromatography(HILIC) method based on on-line HPLC-DPPH bioactivity-guided assay was developed for the purification of analogue antioxidant compounds with high purity from the extract of A. kansuensis. Based on the separation results of many different chromatographic stationary phases, the first-dimensional (1D) preparation was carried on a RP-C18HCE prep column, and 2 antioxidant fractions were obtained from the 800mg crude sample with a recovery of 56.7%. A HILIC-XAmide prep column was selected for the second-dimensional (2D) preparation. Finally, a novel antioxidant β-carboline Alkaloids (Glusodichotomine AK) and 4 known compounds (Tricin, Homoeriodictyol, Luteolin, Glucodichotomine B) were purified from A. kansuensis. The purity of the compounds isolated from the crude extract was >98%, which indicated that the method built in this work was efficient to manufacture single analogue antioxidant compounds of high purity from the extract of A. kansuensis. Additionally, this method showed great potential in the preparation of analogue structure antioxidant compounds and can serve as a good example for the purification of analogue structure antioxidant carboline alkaloids and flavonoids from other plant materials.
Barrado-Moreno, M M; Beltran-Heredia, J; Martín-Gallardo, J
Moringa oleifera seed extract was tested for algae (Chlorella, Microcystis, Oocystis and Scenedesmus) removal by Jar-test technique. This coagulant can be used in drinking water treatment. Jar-test has been carried out in order to evaluate the efficiency of this natural coagulant agent inside real surface water matrix. The influence of variables has been studied in this process, including operating parameters such as coagulant dosage, initial algae concentration, pH, agitation time and water matrix. Removal capacity is verified for water with high contamination of algae while the process is not affected by the pH and water matrix. Coagulation process may be modelling through Langmuir and Freundlich adsorption hypothesis, so acceptable r2 coefficients are obtained.
Singh, Dharmendra; Arya, Priya Vrat; Aggarwal, Ved Prakash; Gupta, Radhey Shyam
The antioxidant and hepatoprotective activities of the extract of Moringa oleifera leaves were investigated against CCl4-induced hepatotoxicity in rats. Hepatotoxic rats were treated with ethanol extract of Moringa oleifera for a period of 60 days at the following three dose levels; 100, 200 and 400 mg/kg body weight/day, orally. The activities were studied by assaying the serum marker enzymes like SGOT, SGPT, GGT, LDH, ALP, ACP, as well as total bilirubin, total protein and albumin in serum concomitantly with the activities of LPO, SOD, CAT, GSH, GR and GPx in liver. The activities of all parameters registered a significant (p ≤ 0.001) alteration in CCl4 treated rats, which were significantly recovered towards an almost normal level in rats co-administered with M. oleifera extract in a dose-dependent manner. All the biochemical investigations were confirmed by the histopathological observations and compared with the standard drug. silymarin. Results suggest that the antioxidant and hepatoprotective activities of M. oleifera leaves are possibly related to the free radical scavenging activity which might be due to the presence of total phenolics and flavonoids in the extract and/or the purified compounds β-sitosterol, quercetin and kaempferol, which were isolated from the ethanol extract of M. oleifera leaves. PMID:26785072
Many oxygenated fatty acids are bioactive compounds. Nocardia cholesterolicum and Flavobacterium DS5 convert oleic acid to 10 hydroxy stearic acid and linoleic acid to 10-hydroxy-12(Z)-octadecanoic acid. Pseudomonas aeruginosa PR3 converts oleic acid to the new compounds, 7,10-dihydroxy-8(E)-octad...
Many oxygenated fatty acids are bioactive compounds. Nocardia cholesterolicum and Flavobacterium DS5 convert oleic acid to 10 hydroxy stearic acid and linoleic acid to 10-hydroxy-12(Z)-octadecanoic acid. Pseudomonas aeruginosa PR3 converts oleic acid to new compounds, 7,10-dihydroxy-8(E)-octadecen...
Many oxygenated fatty acids are bioactive compounds. Nocardia cholesterolicum and Flavobacterium DS5 convert oleic acid to 10 hydroxy stearic acid and linoleic acid to 10-hydroxy-12(Z)-octadecanoic acid. Pseudomonas aeruginosa PR3 converts oleic acid to the new compounds, 7,10-dihydroxy-8(E)-octad...
Ramesh, Ch.; Pattar, Manohar G.
Methanolic extracts of 6 wild edible mushrooms isolated from the Western Ghats of Karnataka were used in this study. Among the isolates (Lycoperdon perlatum, Cantharellus cibarius, Clavaria vermiculris, Ramaria formosa, Marasmius oreades, Pleurotus pulmonarius), only 4 showed satisfactory results. Quantitative analysis of bioactive components revealed that total phenols are the major bioactive component found in extracts of isolates expressed as mg of GAE per gram of fruit body, which ranged from 3.20 ± 0.05 mg/mL to 6.25 ± 0.08 mg/mL. Average concentration of flavonoid ranged from 0.40 ± 0.052 mg/mL to 2.54 ± 0.08 mg/mL; followed by very small concentration of ascorbic acid (range, 0.06 ± 0.01 mg/mL to 0.16 ± 0.01 mg/mL) in all the isolates. All the isolates showed high phenol and flavonoid content, but ascorbic acid content was found in traces. Antioxidant efficiency by inhibitory concentration on 1,1-Diphenly-2-picrylhydrazyl (DPPH) was found significant when compared to standard antioxidant like Buthylated hydroxyanisol (BHA). The concentration (IC50) ranged from 0.94 ± 0.27 mg/mL to 7.57 ± 0.21 mg/mL. Determination of antimicrobial activity profile of all the isolates tested against a panel of standard pathogenic bacteria and fungi indicated that the concentrations of bioactive components directly influence the antimicrobial capability of the isolates. Agar diffusion assay showed considerable activity against all bacteria. Minimum inhibitory concentration values of the extracts of 4 isolates showed that they are also active even in least concentrations. These results are discussed in relation to therapeutic value of the studied mushrooms. PMID:21808550
Teo, Chin Chye; Tan, Swee Ngin; Yong, Jean Wan Hong; Hew, Choy Sin; Ong, Eng Shi
Our earlier work showed that the stability of the bioactive compounds gastrodin (GA) and vanillyl alcohol (VA) in Gastrodia elata Blume behaved differently with varying compositions of water-ethanol using pressurized liquid extraction (PLE) at room temperature. To have a better understanding of the extraction process of these thermally labile compounds under elevated temperature conditions, pressurized hot water extraction (PHWE) and microwave-assisted extraction (MAE) methods were proposed. PHWE and MAE showed that GA and VA could be extracted using pure water under optimized conditions of temperature and extraction time. The extraction efficiency of GA and VA by the proposed methods was found to be higher or comparable to heating under reflux using water. The marker compounds present in the plant extracts were determined by RP-HPLC. The optimized conditions were found to be different for the two proposed methods on extraction of GA and VA. The method precision (RSD, n=6) was found to vary from 0.92% to 3.36% for the two proposed methods on different days. Hence, PHWE and MAE methods were shown to be feasible alternatives for the extraction of thermally labile marker compounds present in medicinal plants.
Llorent-Martínez, E J; Ortega-Barrales, P; Zengin, G; Mocan, A; Simirgiotis, M J; Ceylan, R; Uysal, S; Aktumsek, A
The genus Lathyrus has great importance in terms of food and agricultural areas. In this study, the in vitro antioxidant activity (phosphomolybdenum, DPPH, ABTS, FRAP, CUPRAC and metal chelating) and enzyme inhibitory activity evaluation (acetyl cholinesterase, butyryl cholinesterase, α-amylase and α-glucosidase) of L. cicera and L. digitatus were investigated, as well as their phytochemical profiles. The screening of the main phytochemical compounds in aerial parts of L. cicera and L. digitatus was carried out by high-performance liquid chromatography with electrospray ionization mass spectrometric detection (HPLC-ESI-MS(n)), observing that flavonoids represent the highest percentage of identified compounds, with abundance of tri- and tetra-glycosilated flavonoids, including acylated ones, especially in L. cicera. Generally, L. digitatus exhibited stronger antioxidant and enzyme inhibitory activities in correlation with its higher level of phenolics. The high number of phenolic compounds and the results of the antioxidant and enzyme assays suggest that these plants may be further used as sources of bioactive compounds, and for the preparation of new nutraceuticals.
Förster, Nadja; Mewis, Inga; Glatt, Hansruedi; Haack, Michael; Brigelius-Flohé, Regina; Schreiner, Monika; Ulrichs, Christian
Leaves of Moringa oleifera are used by tribes as biological cancer medicine. Scientific investigations with M. oleifera conducted so far have almost exclusively used total plant extracts. Studies on the activity of single compounds are missing. Therefore, the biological effects of the two main aromatic multi-glycosylated glucosinolates of M. oleifera were investigated in the present study. The cytotoxic effects of M. oleifera glucosinolates were identified for HepG2 cells (NRU assay), for V79-MZ cells (HPRT assay, SCE assay), and for two Salmonella typhimurium strains (Ames test). Genotoxic effects of these glucosinolates were not observed (Ames test, HPRT assay, and SCE assay). Reporter gene assays revealed a significant increase in the ARE-dependent promoter activity of NQO1 and GPx2 indicating an activation of the Nrf2 pathway by M. oleifera glucosinolates. Since both enzymes can also be induced via activation of the AhR, plasmids containing promoters of both enzymes mutated in the respective binding sites (pGL3enh-hNQO1-ARE, pGL3enh-hNQO1-XRE, pGL3bas-hGPX2-mutARE, pGL3bas-hGPX2-mutXRE) were transfected. Analyses revealed that the majority of the stimulating effects was mediated by the ARE motif, whereas the XRE motif played only a minor role. The stimulating effects of M. oleifera glucosinolates could be demonstrated both at the transcriptional (reporter gene assay, real time-PCR) and translational levels (enzyme activity) making them interesting compounds for further investigation.
Li, Weiwei; Yuan, Guoqi; Pan, Yuxiang; Wang, Cong; Chen, Haixia
Diabetes mellitus (DM) is a kind of chronic and metabolic disease, which can cause a number of diseases and severe complications. Network pharmacology approach is introduced to study DM, which can combine the drugs, target proteins and disease and form drug-target-disease networks. Network pharmacology has been widely used in the studies of the bioactive compounds and action mechanisms of natural products for the treatment of DM due to the multi-components, multi-targets, and lower side effects. This review provides a balanced and comprehensive summary on network pharmacology from current studies, highlighting different bioactive constituents, related databases and applications in the investigations on the treatment of DM especially type 2. The mechanisms related to type 2 DM, including α-amylase and α-glucosidase inhibitory, targeting β cell dysfunction, AMPK signal pathway and PI3K/Akt signal pathway are summarized and critiqued. It suggests that the network pharmacology approach cannot only provide a new research paradigm for natural products, but also improve the current antidiabetic drug discovery strategies. Furthermore, we put forward the perspectives on the reasonable applications of network pharmacology for the therapy of DM and related drug discovery. PMID:28280467
Li, Weiwei; Yuan, Guoqi; Pan, Yuxiang; Wang, Cong; Chen, Haixia
Diabetes mellitus (DM) is a kind of chronic and metabolic disease, which can cause a number of diseases and severe complications. Network pharmacology approach is introduced to study DM, which can combine the drugs, target proteins and disease and form drug-target-disease networks. Network pharmacology has been widely used in the studies of the bioactive compounds and action mechanisms of natural products for the treatment of DM due to the multi-components, multi-targets, and lower side effects. This review provides a balanced and comprehensive summary on network pharmacology from current studies, highlighting different bioactive constituents, related databases and applications in the investigations on the treatment of DM especially type 2. The mechanisms related to type 2 DM, including α-amylase and α-glucosidase inhibitory, targeting β cell dysfunction, AMPK signal pathway and PI3K/Akt signal pathway are summarized and critiqued. It suggests that the network pharmacology approach cannot only provide a new research paradigm for natural products, but also improve the current antidiabetic drug discovery strategies. Furthermore, we put forward the perspectives on the reasonable applications of network pharmacology for the therapy of DM and related drug discovery.
Thøgersen, Mariane S.; Delpin, Marina W.; Melchiorsen, Jette; Kilstrup, Mogens; Månsson, Maria; Bunk, Boyke; Spröer, Cathrin; Overmann, Jörg; Nielsen, Kristian F.; Gram, Lone
It has previously been reported that some strains of the marine bacterium Pseudoalteromonas luteoviolacea produce the purple bioactive pigment violacein as well as the antibiotic compound indolmycin, hitherto only found in Streptomyces. The purpose of the present study was to determine the relative role of each of these two compounds as antibacterial compounds in P. luteoviolacea S4054. Using Tn10 transposon mutagenesis, a mutant strain that was significantly reduced in violacein production in mannose-containing substrates was created. Full genome analyses revealed that the vio-biosynthetic gene cluster was not interrupted by the transposon; instead the insertion was located to the maeA gene encoding the malic enzyme. Supernatant of the mutant strain inhibited Vibrio anguillarum and Staphylococcus aureus in well diffusion assays and in MIC assays at the same level as the wild type strain. The mutant strain killed V. anguillarum in co-culture experiments as efficiently as the wild type. Using UHPLC-UV/Vis analyses, we quantified violacein and indolmycin, and the mutant strain only produced 7–10% the amount of violacein compared to the wild type strain. In contrast, the amount of indolmycin produced by the mutant strain was about 300% that of the wild type. Since inhibition of V. anguillarum and S. aureus by the mutant strain was similar to that of the wild type, it is concluded that violacein is not the major antibacterial compound in P. luteoviolacea. We furthermore propose that production of violacein and indolmycin may be metabolically linked and that yet unidentified antibacterial compound(s) may be play a role in the antibacterial activity of P. luteoviolacea. PMID:27695447
Lores, Marta; Pájaro, Marta; Álvarez-Casas, Marta; Domínguez, Jorge; García-Jares, Carmen
An important trend in the extraction of chemical compounds is the application of new environmentally friendly, food grade solvents. Ethyl lactate (ethyl 2-hydroxypropanoate), produced by fermentation of carbohydrates, is miscible with both hydrophilic and hydrophobic compounds being a potentially good solvent for bioactive compounds. Despite its relatively wide use as a general solvent, the utilization of ethyl lactate as an extraction solvent has only recently been considered. Here, we evaluate the possible use of ethyl lactate to extract phenolic compounds from wild plants belonging to Cytisus scoparius, and we compare the characteristics of the extracts obtained by Pressurized Solvent Extraction (the total phenolics content, the antioxidant activity and the concentration of the major polyphenols) with those of other extracts obtained with methanol. In order to explore the industrial production of the ethyl lactate Cytisus extract, we also evaluate medium scale ambient temperature setups. The whole plant and the different parts (flowers, branches, and seed pods) were evaluated separately as potential sources of polyphenols. All extracts were analyzed by LC-MS/MS for accurate identification of the major polyphenols. Similar phenolic profiles were obtained when using ethyl lactate or methanol. The main bioactives found in the Cytisus extract were the non-flavonoid phenolic compounds caffeic and protocatechuic acids and 3,4-dihydroxybenzaldehyde; the flavonoids rutin, kaempferol and quercetin; the flavones chrysin, orientin and apigenin; and the alkaloid lupanine. Regarding the comparison of the extraction systems, although the performance of the PLE was much better than that of the ambient-temperature columns, the energy consumption was also much higher. Ethyl lactate has resulted an efficient extraction solvent for polyphenols from C. scoparius, yielding extracts with high levels of plant phenolics and antioxidant activity. The antimicrobial activity of these
Rangel-Huerta, Oscar Daniel; Gil, Angel
Metabolomics is the study of low-weight molecules present in biological samples such as biofluids, tissue/cellular extracts, and culture media. Metabolomics research is increasing, and at the moment, it has several applications in the food science and nutrition fields. In the present review, we provide an update about the most frequently used methodologies and metabolomic platforms in these areas. Also, we discuss different metabolomic strategies regarding the discovery of new bioactive compounds (BACs) in plant-based foods. Furthermore, we review the existing literature related to the use of metabolomics to investigate the potential protective role of BACs in the prevention and treatment of non-communicable chronic diseases, namely cardiovascular disease, diabetes, and cancer. PMID:27941699
De Monte, Celeste; Bizzarri, Bruna; Gidaro, Maria Concetta; Carradori, Simone; Mollica, Adriano; Luisi, Grazia; Granese, Arianna; Alcaro, Stefano; Costa, Giosuè; Basilico, Nicoletta; Parapini, Silvia; Scaltrito, Maria Maddalena; Masia, Carla; Sisto, Francesca
Crocus sativus L. is known in herbal medicine for the various pharmacological effects of its components, but no data are found in literature about its biological properties toward Helicobacter pylori, Plasmodium spp. and Leishmania spp. In this work, the potential anti-bacterial and anti-parasitic effects of crocin and safranal, two important bioactive components in C. sativus, were explored, and also some semi-synthetic derivatives of safranal were tested in order to establish which modifications in the chemical structure could improve the biological activity. According to our promising results, we virtually screened our compounds by means of molecular modeling studies against the main H. pylori enzymes in order to unravel their putative mechanism of action.
Rangel-Huerta, Oscar Daniel; Gil, Angel
Metabolomics is the study of low-weight molecules present in biological samples such as biofluids, tissue/cellular extracts, and culture media. Metabolomics research is increasing, and at the moment, it has several applications in the food science and nutrition fields. In the present review, we provide an update about the most frequently used methodologies and metabolomic platforms in these areas. Also, we discuss different metabolomic strategies regarding the discovery of new bioactive compounds (BACs) in plant-based foods. Furthermore, we review the existing literature related to the use of metabolomics to investigate the potential protective role of BACs in the prevention and treatment of non-communicable chronic diseases, namely cardiovascular disease, diabetes, and cancer.
Kivrak, Ibrahim; Kivrak, Seyda; Harmandar, Mansur
In this study, the compositions of Calvatia gigantea were first analyzed in order to elucidate its chemical basis for development as a health-enhancing food or medicine. This study investigates the chemical composition (nutritional value; phenolic, sugar and fatty acid content; aroma compounds) and antioxidant properties (radical scavenging activity, reducing power, and inhibition of lipid peroxidation) of C. gigantea. The results showed that C. gigantea contains phenolic compounds and sugars and is rich in polyunsaturated fatty acids (67.93%), proteins (34.37%), and carbohydrates (51.97%). The most abundant compounds were gentisic acid (23.26 µg/g; as a phenolic compound), trehalose (9.78 g/100g; as a sugar), and hexanal (34.71%; as an aroma compound). These findings suggest that C. gigantea might be a promising source of medicine and has the potential to be a health food and food supplementary product.
Cui, Xi-Hua; Murthy, Hosakatte Niranjana; Paek, Kee-Yoeup
Hypericum perforatum L. (St. John's Wort) is an important medicinal plant which is widely used in the treatment for depression and irritable bowel syndrome. It is also used as a dietary supplement. Major bioactive phytochemicals of H. perforatum are phenolics and flavonoids. Quality of these phytochemicals is dramatically influenced by environmental and biological factors in the field grown plants. As an alternative, we have developed adventitious root cultures in large-scale bioreactors for the production of useful phytochemicals. Adventitious roots of H. perforatum were cultured in 500 l pilot-scale airlift bioreactors using half-strength Murashige and Skoog medium with an ammonium and nitrate ratio of 5:25 mM and supplemented with 1.0 mg l(-1) indole butyric acid, 0.1 mg l(-1) kinetin, and 3 % sucrose for the production of bioactive phenolics and flavonoids. Then 4.6 and 6.3 kg dry biomass were realized in the 500 l each of drum-type and balloon-type bioreactors, respectively. Accumulation of 66.9 mg g(-1) DW of total phenolics, 48.6 mg g(-1) DW of total flavonoids, 1.3 mg g(-1) DW of chlorogenic acid, 0.01 mg g(-1) DW of hyperin, 0.04 mg g(-1) DW of hypericin, and 0.01 mg g(-1) DW of quercetin could be achieved with adventitious roots cultured in 500 l balloon-type airlift bioreactors. Our findings demonstrate the possibilities of using H. perforatum adventitious root cultures for the production of useful phytochemicals to meet the demand of pharmaceutical and food industry.
Lewis, Mark A; Williams, Katie M; Fang, Ya-Yin; Schultz, Franklin A; Long, Eric C
Amino terminal peptides of the general form Gly-Gly-His have been used to introduce single sites of metal binding and redox activity into a wide range of biomolecules to create bioactive compounds and conjugates capable of substrate oxidation. We report here that Gly-Gly-His-like peptides linked in a tandem fashion can also be generated leading to multi-metal binding arrays. While metal binding by the native Gly-Gly-His motif (typically to Cu(2+), Ni(2+), or Co(2+)) requires a terminal peptide amine ligand, previous work has demonstrated that an ornithine (Orn) residue can be substituted for the terminal Gly residue to allow solid-phase peptide synthesis to continue via the side chain N-δ. This strategy thus frees the Orn residue N-α for metal binding and permits placement of a Gly-Gly-His-like metal binding domain at any location within a linear, synthetic peptide chain. As we show here, this strategy also permits the assembly of tandem arrays of metal binding units in linear peptides of the form: NH2-Gly-Gly-His-[(δ)-Orn-Gly-His]n-(δ)-Orn-Gly-His-CONH2 (where n = 0, 1, and 2). Metal binding titrations of these tandem arrays monitored by UV-vis and ESI-MS indicated that they bind Cu(2+), Ni(2+), or Co(2+) at each available metal binding site. Further, it was found that these systems retained their ability to modify DNA oxidatively and to an extent greater than their parent M(II)•Gly-Gly-His. These findings suggest that the tandem array metallopeptides described here may function with increased efficiency as "next generation" appendages in the design of bioactive compounds and conjugates.
Guo, Mingmin; Guo, Suping; Huaijun, Yang; Bu, Ning; Dong, Cai-Hong
In this study, the main bioactive compounds of the fruit bodies of Cordyceps militaris-such as adenosine, cordycepin, polysaccharides, mannitol, superoxide dismutase (SOD), and carotenoids-were cultivated on wheat and pupae, as well as sclerotium (the pupae portion) and sclerotium with fruiting bodies. The amounts of adenosine and polysaccharide in all the tested samples (except for the polysaccharides of sclerotium) are higher than the quality standards (adenosine ≥0.055% and polysaccharide ≥2.5%) determined by the Ministry of Health of the People's Republic of China. As the most important bioactive compound in C. militaris, cordycepin is the highest in the fruiting bodies on pupae than in other samples, whereas it is the lowest in the sclerotium. The amounts of cordycepin, carotenoids, and SOD were higher in the fruiting bodies on pupae than that in the fruiting bodies on wheat, whereas the amounts of adenosine, polysaccharides, and mannitol were higher in the fruiting bodies on wheat than in the fruiting bodies on pupae. There was no significant difference in the amounts of cordycepin, carotenoids, and SOD in the sclerotium with fruiting bodies and the fruiting bodies on wheat. The adenosine, polysaccharide, and mannitol contents in the sclerotium with fruiting bodies were significantly lower than those of the fruiting bodies on wheat. Overall, the results of this evaluation could not distinguish which is better: the fruiting bodies on pupae or those on wheat; each has its own merits. The fruiting bodies of C. militaris cultivated on both wheat and pupae are important candidates for medicinal and tonic use for the welfare of humankind.
Ramar, Vanajothi; Pappu, Srinivasan
Nuclear factor kappa B (NF-κB) is a transcription factor, plays a crucial role in the regulation of various physiological processes such as differentiation, cell proliferation and apoptosis. It also coordinates the expression of various soluble proinflammatory mediators like cytokines and chemokines. The 1, 8-dihydroxy-4-methylanthracene-9, 10-dione (DHMA) was isolated from Luffa acutangala and its in vitro cytotoxic activity against NCI-H460 cells was reported earlier. It also effectively induces apoptosis through suppressing the expression NF-κB protein. Based on experimental evidence, the binding affinity of compound 1 with NF-κB p50 (monomer) and NF-κB-DNA was investigated using molecular docking and its stability was confirmed through molecular dynamic simulation. The reactivity of the compound was evaluated using density functional theory (DFT) calculation. From the docking results, we noticed that the hydroxyl group of DHMA forms hydrogen bond interactions with polar and negatively charged amino acid Tyr57 and Asp239 and the protein-ligand complex was stabilized through pi-pi stacking with the help of polar amino acid His114, which plays a key role in binding of NF-κB to DNA at a site of DNA-binding region (DBR). The result indicates that the isolated bioactive compound DHMA might have altered the binding affinity between DNA and NF-κB. These findings suggest that potential use of DHMA in cancer chemoprevention and therapeutics.
Sianipar, N. F.; Purnamaningsih, R.; Rosaria
Rodent tuber (Typhonium flagelliforme Lodd.) is an Indonesian anticancer medicinal plant. The natural genetic diversity of rodent tuber is low due to vegetative propagation. Plant's genetic diversity has to be increased for obtaining clones which contain a high amount of anticancer compounds. In vitro calli were irradiated with 6 Gy of gamma ray to produce in vitro mutant plantlets. Mutant plantlets were acclimated and propagated in a greenhouse. This research was aimed to identify the chemical compounds in the leaves and tubers ofthe fourth generation of rodent tuber's vegetative mutant clones (MV4) and control plantsby using GC- MS method. Leaves and tubers of MV4 each contained 2 and 5 anticancer compounds which quantities were higher compared to control plants. MV4 leaves contained 5 new anticancer compounds while its tubers contained 3 new anticancer compounds which were not found in control. The new anticancer compounds in leaves were hexadecanoic acid, stigmast-5-en-3-ol, ergost-5-en-3-ol, farnesol isomer a, and oleic acid while the new anticancer compounds in tubers were alpha tocopherol, ergost-5-en-3-ol, and beta-elemene. Rodent tuber mutant clones are very potential to be developed into anticancer drugs.
Zeb, Anwar; Ahmad, Sajjad; Ullah, Farhat; Ayaz, Muhammad; Sadiq, Abdul
Isodon rugosus Wall. ex Benth. is extensively used as traditional medicine for the management of various types of pain including tooth ache, gastric pain, abdominal pain, ear ache, and generalized body pain. The current study is designed to scientifically verify the purported uses of I. rugosus as analgesic agent and to figure out its possible mechanism of action. Bioactive compounds responsible for analgesic activity were identified using GC and GC-MS analysis. Analgesic potentials were evaluated using acetic acid induced writhing, hot plate test, and formalin induced paw licking test. In acetic acid induced writhing chloroform fraction (Ir.Chf) exhibited 53% analgesia while formalin test displayed 61% inhibition at phase-I and 45% at phase-II respectively at a dose of 100 mg/kg. Similarly, in hot plate test Ir.Chf displayed average reaction time of 7 min at 15, 30, 45, and 60 min intervals. The possible mechanism of action was found to be the central pathway via opioidergic receptors as the mice showed morphine like analgesic activity at pre-administration of naloxone (opioid antagonist) in hot plate and formalin tests. In GC-MS analysis, 83 compounds were identified among which eight compounds including benzyl alcohol, sebacic acid, myristic acid, phytol, sugiol, Tocopherol, α-Amyrin, and stigmasterol were sorted out as previously reported analgesic compounds. Current study revealed that analgesic potential of I. rugosus can attributed to the presence of analgesic compounds. It may also be concluded that opioids receptors are involved in the analgesic mechanism of I. rugosus due to effective antagonism of nalaxone. PMID:27458379
Sirajuddin, Muhammad; Uddin, Noor; Ali, Saqib; Tahir, Muhammad Nawaz
Three Schiff base compounds ofN‧-substituted benzohydrazide and sulfonohydrazide derivatives: N‧-(2-hydroxy-3-methoxybenzylidene)-4-tert-butyl- benzohydrazide (1), N‧-(5-bromo-2-hydroxybenzylidene)-4-tert-butylbenzohydrazide (2) and N‧-(2-hydroxy-3-methoxybenzylidene)-4-methylbenzenesulfonohydrazide (3) were synthesized and characterized by elemental analysis, FT-IR, 1H, 13C NMR spectroscopy and single crystal analysis. The title compounds have been screened for their biological activities including, antibacterial, antifungal, antioxidant, cytotoxic, enzymatic activities as well as interaction with SS-DNA which showed remarkable activities in each area of research. The DNA binding of the compounds 1-3 with SS-DNA has been carried out with absorption spectroscopy, which reveals the binding propensity towards SS-DNA via intercalation mode of interaction. The intercalative mode of interaction is also supported by viscometric results. The synthesized compounds were also found to be effective against alkaline phosphatase enzyme. They also show significant to good antimicrobial activity against six bacterial and five fungal strains. The MIC (minimum inhibitory concentration) for antibacterial activity ranges from 1.95-500 μg/mL. Compounds 1-3 show cytotoxic activity comparable to the control. At higher conc. (100 μg/L) compound 3 shows 100% activity means that it has killed all brine shrimps. They were also found to be effective antioxidant of 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and show almost comparable antioxidant activity to that of the standard and known antioxidant, ascorbic acid.
Moyo, B; Oyedemi, S; Masika, P J; Muchenje, V
The study investigated antioxidant potency of Moringa oleifera leaves in different in vitro systems using standard phytochemical methods. The antioxidative effect on the activities of superoxide dismutase (SOD), catalase (CAT), lipid peroxidation (LPO) and reduced glutathione (GSH) were investigated in goats supplemented with M. oleifera (MOL) or sunflower seed cake (SC). The acetone extract had higher concentrations of total flavonoids (295.01 ± 1.89 QE/g) followed by flavonols (132.74 ± 0.83 QE/g), phenolics (120.33 ± 0.76 TE/g) and then proanthocyanidins (32.59 ± 0.50 CE/g) than the aqueous extract. The reducing power of both solvent extracts showed strong antioxidant activity in a concentration dependent manner. The acetone extract depicted higher percentage inhibition against DPPH, ABTS and nitric oxide radicals which were comparable with reference standard antioxidants (vitamin C and BHT). MOL increased the antioxidant activity of GSH (186%), SOD (97.8%) and catalase (0.177%). Lipid peroxidation was significantly reduced by MOL. The present study suggests that M. oleifera could be a potential source of compounds with strong antioxidant potential.
Teleszko, Mirosława; Wojdyło, Aneta; Rudzińska, Magdalena; Oszmiański, Jan; Golis, Tomasz
The aim of this study was to determine selected phytochemicals in berries of eight sea buckthorn (Hippophaë rhamnoides subsp. mongolica) cultivars, including lipophilic and hydrophilic compounds. In the experiment chromatographic analyses, GC (phytosterols and fatty acids), UPLC-PDA-FL, LC-MS (polyphenols), and HPLC (L-ascorbic acid), as well spectrophotometric method (total carotenoids) were used. The lipid fraction isolated from whole fruit contained 14 phytosterols (major compounds β-sitosterol > 24-methylenecykloartanol > squalene) and 11 fatty acids in the order MUFAs > SFAs > PUFAs. Carotenoids occurred in concentrations between 6.19 and 23.91 mg/100 g fresh weight (fw) (p < 0.05). The major polyphenol group identified in berries was flavonols (mean content of 311.55 mg/100 g fw), with the structures of isorhamnetin (six compounds), quercetin (four compounds), and kaempferol (one compound) glycosides. Examined sea buckthorn cultivars were characterized also by a high content of L-ascorbic acid in a range from 52.86 to 130.97 mg/100 g fw (p < 0.05).
Li, Yan; Zheng, Jinkai; Xiao, Hang; McClements, David Julian
Polymethoxyflavones (PMFs) extracted from citrus peel exhibit potent anti-cancer activity, but are highly hydrophobic molecules with poor solubility in both water and oil at ambient and body temperature, which limits their bioavailability. The possibility of encapsulating PMFs within nanoemulsion-based delivery systems to facilitate their application in nutraceutical and pharmaceutical products was investigated. The influence of oil type (corn oil, MCT, orange oil), emulsifier type (β-lactoglobulin, lyso-lecithin, Tween, and DTAB), and neutral cosolvents (glycerol and ethanol) on the formation and stability of PMF-loaded nanoemulsions was examined. Nanoemulsions (r < 100 nm) could be formed using high pressure homogenization for all emulsifier types, except DTAB. Lipid droplet charge could be altered from highly cationic (DTAB), to near neutral (Tween), to highly anionic (β-lactoglobulin, lyso-lecithin) by varying emulsifier type. PMF crystals formed in all nanoemulsions after preparation, which had a tendency to sediment during storage. The size, morphology, and aggregation of PMF crystals depended on preparation method, emulsifier type, oil type, and cosolvent addition. These results have important implications for the development of delivery systems for bioactive components that have poor oil and water solubility at application temperatures. PMID:22685367
Acevedo, Francisca; Torres, Paulina; Oomah, B Dave; de Alencar, Severino Matias; Massarioli, Adna Prado; Martín-Venegas, Raquel; Albarral-Ávila, Vicenta; Burgos-Díaz, César; Ferrer, Ruth; Rubilar, Mónica
Ulmo honey originating from Eucryphia cordifolia tree, known locally in the Araucania region as the Ulmo tree is a natural product with valuable nutritional and medicinal qualities. It has been used in the Mapuche culture to treat infections. This study aimed to identify the volatile and non-volatile/semi-volatile compounds of Ulmo honey and elucidate its in vitro biological properties by evaluating its antioxidant, antibacterial, antiproliferative and hemolytic properties and cytotoxicity in Caco-2 cells. Headspace volatiles of Ulmo honey were isolated by solid-phase microextraction (SPME); non-volatiles/semi-volatiles were obtained by removing all saccharides with acidified water and the compounds were identified by GC/MS analysis. Ulmo honey volatiles consisted of 50 compounds predominated by 20 flavor components. Two of the volatile compounds, lyrame and anethol have never been reported before as honey compounds. The non-volatile/semi-volatile components of Ulmo honey comprised 27 compounds including 13 benzene derivatives accounting 75% of the total peak area. Ulmo honey exhibited weak antioxidant activity but strong antibacterial activity particularly against gram-negative bacteria and methicillin-resistant Staphylococcus aureus (MRSA), the main strain involved in wounds and skin infections. At concentrations >0.5%, Ulmo honey reduced Caco-2 cell viability, released lactate dehydrogenase (LDH) and increased reactive oxygen species (ROS) production in a dose dependent manner in the presence of foetal bovine serum (FBS). The wide array of volatile and non-volatile/semi-volatile constituents of Ulmo honey rich in benzene derivatives may partly account for its strong antibacterial and antiproliferative properties important for its therapeutic use. Our results indicate that Ulmo honey can potentially inhibit cancer growth at least partly by modulating oxidative stress.
Mendes, Graziele; Gonçalves, Vívian N; Souza-Fagundes, Elaine M; Kohlhoff, Markus; Rosa, Carlos A; Zani, Carlos L; Cota, Betania B; Rosa, Luiz H; Johann, Susana
Fungi of the genus Paracoccidioides are responsible for paracoccidioidomycosis. The occurrence of drug toxicity and relapse in this disease justify the development of new antifungal agents. Compounds extracted from fungal extract have showing antifungal activity. Extracts of 78 fungi isolated from rocks of the Atacama Desert were tested in a microdilution assay against Paracoccidioides brasiliensis Pb18. Approximately 18% (5) of the extracts showed minimum inhibitory concentration (MIC) values ≤ 125.0 µg/mL. Among these, extract from the fungus UFMGCB 8030 demonstrated the best results, with an MIC of 15.6 µg/mL. This isolate was identified as Aspergillus felis (by macro and micromorphologies, and internal transcribed spacer, β-tubulin, and ribosomal polymerase II gene analyses) and was grown in five different culture media and extracted with various solvents to optimise its antifungal activity. Potato dextrose agar culture and dichloromethane extraction resulted in an MIC of 1.9 µg/mL against P. brasiliensis and did not show cytotoxicity at the concentrations tested in normal mammalian cell (Vero). This extract was subjected to bioassay-guided fractionation using analytical C18RP-high-performance liquid chromatography (HPLC) and an antifungal assay using P. brasiliensis. Analysis of the active fractions by HPLC-high resolution mass spectrometry allowed us to identify the antifungal agents present in the A. felis extracts cytochalasins. These results reveal the potential of A. felis as a producer of bioactive compounds with antifungal activity.
Fonteles, Thatyane Vidal; Leite, Ana Karoline Ferreira; Silva, Ana Raquel Araújo; Carneiro, Alessandra Pinheiro Góes; Miguel, Emilio de Castro; Cavada, Benildo Sousa; Fernandes, Fabiano André Narciso; Rodrigues, Sueli
The present study has evaluated the effects of power ultrasound pre-treatment on air-drying and bioactive compounds of cashew apple bagasse. The sonication induced the disruption of cashew bagasse parenchyma, which resulted in lower resistance to water diffusion, less hysteresis, and increased rehydration rate. The processing did not affect the lignocellulose fibers or the sclerenchyma cells. For sonicated samples, water activity reached values below 0.4, after 2h of drying, which is appropriate to prevent bacterial and fungi growth. The sorption isotherms of cashew apple bagasse presented sigmoid-shape for all samples and followed the type II according to BET classification. Sonicated cashew apple bagasse showed higher antioxidant activity, higher total phenolic compounds (TPC) and higher vitamin C content when compared to the non-sonicated sample. The increase in TPC and vitamin C contributed to the product antioxidant activity. A slight reduction on Vitamin C bioaccessibility was observed, but the TPC bioaccessibility has increased. Sonication reduced the quality loss of conventional drying treatments improving the quality of the dried product.
Mendes, Graziele; Gonçalves, Vívian N; Souza-Fagundes, Elaine M; Kohlhoff, Markus; Rosa, Carlos A; Zani, Carlos L; Cota, Betania B; Rosa, Luiz H; Johann, Susana
Fungi of the genus Paracoccidioides are responsible for paracoccidioidomycosis. The occurrence of drug toxicity and relapse in this disease justify the development of new antifungal agents. Compounds extracted from fungal extract have showing antifungal activity. Extracts of 78 fungi isolated from rocks of the Atacama Desert were tested in a microdilution assay against Paracoccidioides brasiliensis Pb18. Approximately 18% (5) of the extracts showed minimum inhibitory concentration (MIC) values≤ 125.0 µg/mL. Among these, extract from the fungus UFMGCB 8030 demonstrated the best results, with an MIC of 15.6 µg/mL. This isolate was identified as Aspergillus felis (by macro and micromorphologies, and internal transcribed spacer, β-tubulin, and ribosomal polymerase II gene analyses) and was grown in five different culture media and extracted with various solvents to optimise its antifungal activity. Potato dextrose agar culture and dichloromethane extraction resulted in an MIC of 1.9 µg/mL against P. brasiliensis and did not show cytotoxicity at the concentrations tested in normal mammalian cell (Vero). This extract was subjected to bioassay-guided fractionation using analytical C18RP-high-performance liquid chromatography (HPLC) and an antifungal assay using P. brasiliensis. Analysis of the active fractions by HPLC-high resolution mass spectrometry allowed us to identify the antifungal agents present in the A. felis extracts cytochalasins. These results reveal the potential of A. felis as a producer of bioactive compounds with antifungal activity. PMID:27008375
Fuentes, Eduardo; Castro, Ricardo; Astudillo, Luis; Carrasco, Gilda; Alarcón, Marcelo; Gutiérrez, Margarita; Palomo, Iván
In seeking the functionality of foodstuff applicable to medicine, ripe tomato fruits were found to show an antiplatelet activity. Therefore, the bioactive compound was isolated, structurally identified, and studied for an inhibitory effects on platelet adhesion, secretion, and aggregation. The concentration of adenosine in ripe tomato fruits (pulp and skin extracts) and its processing by-products (paste and pomace) was determined by reversed-phase high-performance liquid chromatography (HPLC). According to platelet aggregation inhibition induced by ADP, the total extract residual was fractionated by liquid-liquid separation, obtaining aqueous, ethyl acetate and petroleum ether extracts. The aqueous extract was subjected to repeated permeation over sephadex LH-20 and semipreparative TLC. The isolate finally obtained was identified as adenosine on the basis of ESI-MS, (1)H NMR, HPLC, and UV spectra. Adenosine concentration dependently (2.3-457 μM) platelet aggregation inhibited induced by ADP. Also, adenosine present inhibition of platelet secretion and thrombus formation under flow conditions. The quantitative HPLC analysis revealed significant amounts of adenosine in ripe tomato fruits and its processing by-products. From these results, extracts/fractions of ripe tomato fruits and their processing by-products may be referred to as functional food and functional ingredients containing a compound that inhibits platelet function with a potent preventive effect on thrombus formation, as those that occur in stroke.
Fuentes, Eduardo; Castro, Ricardo; Astudillo, Luis; Carrasco, Gilda; Alarcón, Marcelo; Gutiérrez, Margarita; Palomo, Iván
In seeking the functionality of foodstuff applicable to medicine, ripe tomato fruits were found to show an antiplatelet activity. Therefore, the bioactive compound was isolated, structurally identified, and studied for an inhibitory effects on platelet adhesion, secretion, and aggregation. The concentration of adenosine in ripe tomato fruits (pulp and skin extracts) and its processing by-products (paste and pomace) was determined by reversed-phase high-performance liquid chromatography (HPLC). According to platelet aggregation inhibition induced by ADP, the total extract residual was fractionated by liquid-liquid separation, obtaining aqueous, ethyl acetate and petroleum ether extracts. The aqueous extract was subjected to repeated permeation over sephadex LH-20 and semipreparative TLC. The isolate finally obtained was identified as adenosine on the basis of ESI-MS, 1H NMR, HPLC, and UV spectra. Adenosine concentration dependently (2.3–457 μM) platelet aggregation inhibited induced by ADP. Also, adenosine present inhibition of platelet secretion and thrombus formation under flow conditions. The quantitative HPLC analysis revealed significant amounts of adenosine in ripe tomato fruits and its processing by-products. From these results, extracts/fractions of ripe tomato fruits and their processing by-products may be referred to as functional food and functional ingredients containing a compound that inhibits platelet function with a potent preventive effect on thrombus formation, as those that occur in stroke. PMID:23227097
Photosynthetically active radiation (PAR) and Ultraviolet B (UV-B) radiation are among the main environmental factors acting on herbal yield and biosynthesis of bioactive compounds in medicinal plants. The objective of this study was to evaluate the influence of biologically effective UV-B light (280-315 nm) and PAR (400-700 nm) on herbal yield, content and composition, as well as antioxidant capacity of essential oils and polyphenols of lemon catmint (Nepeta cataria L. f. citriodora), lemon balm (Melissa officinalis L.) and sage (Salvia officinalis L.) under controlled greenhouse cultivation. Intensive UV-B radiation (2.5 kJ m(-2) d(-1) ) influenced positively the herbal yield. The essential oil content and composition of studied herbs were mainly affected by PAR and UV-B radiation. In general, additional low-dose UV-B radiation (1 kJ m(-2) d(-1) ) was most effective for biosynthesis of polyphenols in herbs. Analysis of major polyphenolic compounds provided differences in sensitivity of main polyphenols to PAR and UV-B radiation. Essential oils and polyphenol-rich extracts of radiated herbs showed essential differences in antioxidant capacity by the ABTS system. Information from this study can be useful for herbal biomass and secondary metabolite production with superior quality under controlled environment conditions.
Analgesic, Anti- inflammatory, Anti- lipoxygenase Activity and Characterization of Three Bioactive Compounds in the Most Active Fraction of Leptadenia reticulata (Retz.)Wight & Arn. - A Valuable Medicinal Plant.
Mohanty, Sudipta Kumar; Swamy, Mallappa Kumara; Middha, Sushil Kumar; Prakash, Lokesh; Subbanarashiman, Balasubramanya; Maniyam, Anuradha
Leptadenia reticulata was reported to be used for several medicinal purposes. The present study was undertaken to evaluate anti-inflammatory, analgesic and lipid peroxidation inhibition activities of L. reticulata. The anti-inflammatory assay was performed by λ-carrageenan and formalin induced paw edema test. Pro inflammatory mediators (IL2, IL6, TNF-α) in serum of treated and control organism were analyzed by quantitative ELISA. Lipid peroxidation inhibition was measured by thiobarbituric acid reactive substances (TBARS) assay. Analysis of the most active fraction revealed the presence of one phenolic compound (p-coumaric acid), two flavonoids (rutin and quercetin) which also determined quantitatively. The ethyl acetate fraction at 600 mg/Kg significantly inhibited λ-carrageenan and formalin induced paw edema by 60.59% and 59.24% respectively. Notable reduction in percentage of writhing (76.25%), induced by acetic acid signifies the potent analgesic activity. Lower level of pro-inflammatory cytokines (IL-2, IL-6, TNF-α) in serum at the 4(th) hour of λ-Carrageenan injection indicated the inhibition of cyclooxigenase-2 (Cox-2), Nitric oxide (NO) and release of prostaglandin to prevent inflammation. The study also demonstrated the decrease in malonaldehyde (MDA) concentration which revealed the lipid peroxidation inhibition potential of the plant. Our finding provides evidence for potent biological activities in tested model which is supported by its characterized bioactive compounds and ethnomedicinal relevance.
Jonker, Willem; Ballesteros-Gómez, Ana; Hamers, Timo; Somsen, Govert W; Lamoree, Marja H; Kool, Jeroen
The chemical safety of consumer products is an issue of emerging concern. Plastics are widely used, e.g. as casings of consumer electronics (TVs, computers, routers, etc.), which are present in houses and offices in continuously increasing numbers. In this study, we investigate the estrogenic activity of components of plastics coming from electronics' casings. A recently developed fractionation platform for effect-directed analysis (EDA) was used. This platform combines reversed-phase liquid chromatography in parallel with bioassay detection via nanofractionation and with online high-resolution time-of-flight mass spectrometry (TOFMS) for the identification of bioactives. Four out of eight of the analyzed plastics samples showed the presence of estrogenic compounds. Based on the MS results these were assigned to bisphenol A (BPA), 2,4-di-tert-butylphenol, and a possible bisphenol A analog. All samples contained flame retardants, but these did not show any estrogenicity. The observed BPA, however, could be an impurity of tetrabromo-BPA (TBBPA) or TBBPA-based flame retardants. Due to the plausible migration of additives from plastics into the environment, plastics from consumer electronics likely constitute a source of estrogenic compound contamination in the indoor environment.
Wei, Yun; Du, Jilin; Lu, Yuanyuan
In order to utilize and control the invasive weed, bioactive compounds from essential oil of Flaveria bidentis (L.) Kuntze were studied. Steam distillation extraction and one step high-speed counter-current chromatography were applied to separate and purify the caryophyllene oxide, 7,11-dimethyl-3-methylene-1,6,10-dodecatriene, and caryophyllene from essential oil of Flaveria bidentis (L.) Kuntze. The two-phase solvent system containing n-hexane/acetonitrile/ethanol (5:4:3, v/v/v) was selected for the one step separation mode according to the partition coefficient values (K) of the target compounds and the separation factor (α). The purity of each isolated fraction after a single high-speed counter-current chromatography run was determined by high performance liquid chromatography. A 3.2 mg of caryophyllene oxide at a purity of 92.6%, 10.4 mg of 7,11-dimethyl-3-methylene-1,6,10-dodecatriene at a purity of 99.1% and 5.7 mg of caryophyllene at a purity of 98.8% were obtained from 200 mg essential oil of Flaveria bidentis (L.) Kuntze. The chemical structures of these components were identified by GC-MS, (1) H-NMR, and (13) C-NMR.
Bioactive compound loaded stable silver nanoparticle synthesis from microwave irradiated aqueous extracellular leaf extracts of Naringi crenulata and its wound healing activity in experimental rat model.
Bhuvaneswari, T; Thiyagarajan, M; Geetha, N; Venkatachalam, P
An efficient and eco-friendly protocol for the synthesis of bioactive silver nanoparticles was developed using Naringi crenulata leaf extracts via microwave irradiation method. Silver nanoparticles were synthesized by treating N. crenulata leaf extracts with 1mM of aqueous silver nitrate solution. An effective bioactive compound such as alkaloids, phenols, saponins and quinines present in the N. crenulata reduces the Ag(+) into Ag(0). The synthesized silver nanoparticles were monitored by UV-vis spectrophotometer and further characterized by X-ray diffraction (XRD), Fourier Transform Infra Red (FTIR), Energy-dispersive X-ray spectroscopy (EDX) and field emission scanning electron microscopy (FESEM). UV-vis spectroscopy showed maximum absorbance at 390nm due to surface plasmon resonance of AgNPs. From FESEM results, an average crystal size of the synthesized nanoparticle was 72-98nm. FT-IR results showed sharp absorption peaks and they were assigned to phosphine, alkyl halides and sulfonate groups. Silver nanoparticles synthesized were generally found to be spherical and cubic shape. Topical application of ointment prepared from silver nanoparticles of N. crenulata were formulated and evaluated in vivo using the excision wound healing model on Wistar albino rats. The measurement of the wound areas was performed on 3rd, 6th, 9th, 12th and 15th days and the percentage of wound closures was calculated accordingly. By the 15th day, the ointment base containing 5% (w/w) of silver nanoparticles showed 100% wound healing activity compared with that of the reference as well as control bases. The results strongly suggested that the batch C ointment containing silver nanaoparticles synthesized from the leaf extracts of N. crenulata was found to be very effective in wound repair and encourages harnessing the potentials of the plant biomolecules loaded silver nanoparticle in the treatment of tropical diseases including wound healing.
Jabri Karoui, Iness; Marzouk, Brahim
Citrus aurantium peel and juice aroma compounds were investigated by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS), whereas phenolic compounds analysis was performed by reversed-phase high-performance liquid chromatography (RP-HPLC). Limonene was the major volatile compound of bitter orange peel (90.25%) and juice (91.61%). HPLC analysis of bitter orange peel and juice methanolic extracts indicated that phenolic acids constitute their main phenolic class representing 73.80% and 71.25%, respectively, followed by flavonoids (23.02% and 23.13%, resp.). p-Coumaric and ferulic acids were the most abundant phenolic compounds representing 24.68% and 23.79%, respectively, in the peel, while the juice contained 18.02% and 19.04%, respectively. The antioxidant activities of bitter orange peel and juice methanolic extracts have been evaluated using four in vitro assays, and the results were compared with the standard antioxidants (BHT, BHA, and ascorbic acid). Our findings demonstrated that Citrus aurantium peel and juice possess antioxidant activities which were less effective than those of antioxidant standards. Both extracts may be suggested as a new potential source of natural antioxidant.
Jabri karoui, Iness; Marzouk, Brahim
Citrus aurantium peel and juice aroma compounds were investigated by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS), whereas phenolic compounds analysis was performed by reversed-phase high-performance liquid chromatography (RP-HPLC). Limonene was the major volatile compound of bitter orange peel (90.25%) and juice (91.61%). HPLC analysis of bitter orange peel and juice methanolic extracts indicated that phenolic acids constitute their main phenolic class representing 73.80% and 71.25%, respectively, followed by flavonoids (23.02% and 23.13%, resp.). p-Coumaric and ferulic acids were the most abundant phenolic compounds representing 24.68% and 23.79%, respectively, in the peel, while the juice contained 18.02% and 19.04%, respectively. The antioxidant activities of bitter orange peel and juice methanolic extracts have been evaluated using four in vitro assays, and the results were compared with the standard antioxidants (BHT, BHA, and ascorbic acid). Our findings demonstrated that Citrus aurantium peel and juice possess antioxidant activities which were less effective than those of antioxidant standards. Both extracts may be suggested as a new potential source of natural antioxidant. PMID:23841062
Ajaghaku, Daniel Lotanna; Obasi, Okechukwu; Umeokoli, Blessing Ogechukwu; Ogbuatu, Peter; Nworu, Chukwuemeka Sylvester; Ilodigwe, Emmanuel Emeka; Okoye, Festus Basden Chiedu
Objective: Alchornea floribunda leaves are widely used in ethnomedicine for the management of immuno-inflammatory disorders. We investigated the in vivo and in vitro antioxidant activity of the leaf extract, fractions and isolated compounds of A. floribunda. Materials and Methods: The ethyl acetate fraction of the methanol leaf extract was subjected to several chromatographic separations to isolate compounds 1-4. The structures of the isolated compounds were elucidated by a combination of 1D and 2D NMR and mass spectrometry. Oxidative stress was induced with carbon tetrachloride (CCl4). Further analysis on the isolated phenolic compounds were done using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and hydrogen peroxide scavenging activity tests. Results: The ethyl acetate fraction at 200 mg/kg produced significant (p<0.05) elevations of catalase enzyme activity and a significant (p<0.05) reduction in serum malondialdehyde. The chemical investigation of the ethyl acetate fraction led to the isolation of three flavans, (-) cathechin (1), (-) epicathechin (2), (+) epicathechin (3) and a flavanone, 2R, 3R dihydroquercitin (4). In hydrogen peroxide scavenging assay, (-) epicathechin exhibited an EC50 value of 8 μg/ml, similar to the standard ascorbic acid (EC50 = 8 μg/ml). (-) epicathechin showed scavenging of DPPH radical with EC50 value of 19 μg/ml while in the FRAP assay, it had EC50 value of 46 μg/ml which was lower than that of the standard, ascobic acid (EC50 = 66 μg/ml). Conclusion: The medicinal uses of A. floribunda may be due to the antioxidant activities of its phenolic compounds. PMID:28265550
Borland, Kayla M.; AbdulSalam, Safnas F.; Solivio, Morwena J.; Burke, Matthew P.; Wolfkiel, Patrick R.; Lawson, Sean M.; Stockman, Courtney A.; Andersen, Joel M.; Smith, Skyler; Tolstolutskaya, Julia N.; Gurjar, Purujit N.; Bercz, Aron P.; Merino, Edward J.; Litosh, Vladislav A.
Current FDA-approved chemotherapeutic antimetabolites elicit severe side effects that warrant their improvement; therefore, we designed compounds with mechanisms of action focusing on inhibiting DNA replication rather than targeting multiple pathways. We previously discovered that 5-(α-substituted-2-nitrobenzyloxy)methyluridine-5′-triphosphates were exquisite DNA synthesis terminators; therefore, we synthesized a library of 35 thymidine analogs and evaluated their activity using an MTT cell viability assay of MCF7 breast cancer cells chosen for their vulnerability to these nucleoside derivatives. Compound 3a, having an α-tert-butyl-2-nitro-4-(phenyl)alkynylbenzyloxy group, showed an IC50 of 9 ± 1 μM. The compound is more selective for cancer cells than for fibroblast cells compared with 5-fluorouracil. Treatment of MCF7 cells with 3a elicits the DNA damage response as indicated by phosphorylation of γ-H2A. A primer extension assay of the 5′-triphosphate of 3a revealed that 3aTP is more likely to inhibit DNA polymerase than to lead to termination events upon incorporation into the DNA replication fork. PMID:25778768
Tseng, Angela; Zhao, Yanyun
The effects of different drying methods (40 °C conventional and vacuum oven, 25 °C ambient air and freeze dry) on the stability of two red wine grape (Pinot Noir, PN and Merlot, M) byproducts, pomace containing skins and seeds (P) and pomace containing skins only (S) were investigated. Freeze dried samples retained the highest bioactive compounds with total phenolic content (TPC) of 21.19-67.74 mg GAE/g d.m., anthocyanin content (ACY) of 0.35-0.76 mg Mal-3-glu/g d.m., DPPH antiradical scavenge activity (ARS) of 22.01-37.46 mg AAE/g d.m., and total flavanol content (TFC) of 30.16-106.61 mg CE/g d.m., followed with ambient air dried samples. All samples lost significant amount of bioactive compounds during 16 wk of storage at 15 ± 2 °C, in which ambient air and freeze dried samples had TPC reduction of 32-56% and 35-58%, respectively, but ARS in PN-P and M-P still remained more than 50 mg TE/g d.m. Overall, TPC, ARS, and TFC were higher in PN than in M, and higher in pomace than in skins, while reverse results were observed in ACY. Pomace extracts showed higher antibacterial efficiency against Listeria innocua ATCC 51142 than Escherichia coli ATCC 25922 with minimal inhibition concentration (MIC) of 3%, 6%, 4%, and 9% against E. coli, and 2%, 7%, 3%, and 8% against L. innocua for PN-P, PN-S, M-P, and M-S samples, respectively. Dietary fiber content of samples was 57-63% of total dry matter. This study demonstrated that Pinot Noir and Merlot pomace are good sources of antioxidant dietary fibers and may be incorporated into various food products as a functional ingredient. Practical Application: Wine grape pomace (WGP), the byproduct of wine making, is a good source of polyphenols and dietary fibers and may be incorporated into various food products as a functional ingredient. This study reported the effect of four drying methods and storage at 15 ± 2 °C up to 4 months on the retention of polyphenols and antioxidant activity in two types of red WGP (with and
Orbán-Gyapai, Orsolya; Liktor-Busa, Erika; Kúsz, Norbert; Stefkó, Dóra; Urbán, Edit; Hohmann, Judit; Vasas, Andrea
Plants belonging to the genus Rumex (family Polygonaceae) are used worldwide in traditional medicine for the treatment of various diseases caused by different microorganisms (e.g. bacteria-related dermatologic conditions, dysentery and enteritis). The present study focused on the antibacterial screening of Rumex species native to the Carpathian Basin, and isolation of compounds from one of the most efficient species, Rumex aquaticus. The antibacterial effects of n-hexane, chloroform and aqueous fractions of methanol extracts prepared from different parts of 14 Rumex species (R. acetosella, R. acetosa, R. alpinus, R. aquaticus, R. conglomeratus, R. crispus, R. hydrolapathum, R. obtusifolius subsp. obtusifolius, R. obtusifolius subsp. subalpinus, R. patientia, R. pulcher, R. scutatus, R. stenophyllus and R. thyrsiflorus) were investigated against Staphylococcus epidermidis, S. aureus, MRSA, Bacillus subtilis, Moraxella catarrhalis, Streptococcus pyogenes, S. pneumoniae, S. agalactiae, Pseudomonas aeruginosa, Escherichia coli and Klebsiella pneumoniae using the disc diffusion method. Mainly the n-hexane and chloroform extracts prepared from the roots of the plants displayed high antibacterial activity (inhibition zones>15mm) against one or more bacterial strains. The highly active extracts of the aerial part and root of R. aquaticus were subjected to a multistep separation procedure. 19 Compounds, among them naphthalenes (musizin, and its glucoside, torachrysone-glucoside, 2-methoxystypandrone), anthraquinones (emodin, chrysophanol, physcion, citreorosein, chrysophanol-8-O-glucoside), flavonoids (quercetin, quercetin-3,3'-dimethylether, isokaempferide, quercetin 3-O-arabinoside, quercetin 3-O-galactoside, catechin), stilbenes (resveratrol, piceid), and 1-stearoylglycerol were isolated from the plant. The antibacterial activities of isolated compounds were determined, and it was observed that especially naphthalenes exerted remarkable antibacterial effects against
Ferreres, Federico; Grosso, Clara; Gil-Izquierdo, Angel; Valentão, Patrícia; Azevedo, Carolina; Andrade, Paula B
The phenolic composition of herbal tea (HT) and hydromethanolic extract (HME) obtained from Grindelia robusta Nutt. was studied by HPLC-DAD-ESI/MS(n). Thirty six flavonoids and hydroxycinnamic acids were detected, from which thirty are described for the first time in this species. Quantification by HPLC-DAD showed that diosmetin-7-O-glucuronide-3'-O-pentoside+apigenin-7-O-glucuronide-4'-O-pentoside, apigenin-7-O-glucuronide+diosmetin-7-O-glucuronide and 3,5-dicaffeoylquinic acid+3,4-dicaffeoylquinic acid were the major compounds. Since the health-promoting effects of natural phenolic compounds against brain disorders is of increasing interest, HT and HME were also tested against oxygen and nitrogen reactive species and against enzymes related with Alzheimer's disease and depression. Extracts displayed strong in vitro scavenging activity and monoamine oxidase-A (MAO-A) inhibitory activity. The anti-MAO-A capacity was observed at non-toxic concentrations for SH-SY5Y human neuroblastoma cell line, reinforcing the benefits of G. robusta HT. However, no protection against hydrogen peroxide treatment was observed.
Betancur, Luz A.; Naranjo-Gaybor, Sandra J.; Vinchira-Villarraga, Diana M.; Moreno-Sarmiento, Nubia C.; Maldonado, Luis A.; Suarez-Moreno, Zulma R.; Acosta-González, Alejandro; Padilla-Gonzalez, Gillermo F.; Puyana, Mónica; Castellanos, Leonardo; Ramos, Freddy A.
Marine bacteria are considered as promising sources for the discovery of novel biologically active compounds. In this study, samples of sediment, invertebrate and algae were collected from the Providencia and Santa Catalina coral reef (Colombian Caribbean Sea) with the aim of isolating Actinobateria-like strain able to produce antimicrobial and quorum quenching compounds against pathogens. Several approaches were used to select actinobacterial isolates, obtaining 203 strains from all samples. According to their 16S rRNA gene sequencing, a total of 24 strains was classified within Actinobacteria represented by three genera: Streptomyces, Micromonospora, and Gordonia. In order to assess their metabolic profiles, the actinobacterial strains were grown in liquid cultures, and LC-MS-based analyses from ethyl acetate fractions were performed. Based on taxonomical classification, screening information of activity against phytopathogenic strains and quorum quenching activity, as well as metabolic profiling, six out of the 24 isolates were selected for follow-up with chemical isolation and structure identification analyses of putative metabolites involved in antimicrobial activities. PMID:28225766
Betancur, Luz A; Naranjo-Gaybor, Sandra J; Vinchira-Villarraga, Diana M; Moreno-Sarmiento, Nubia C; Maldonado, Luis A; Suarez-Moreno, Zulma R; Acosta-González, Alejandro; Padilla-Gonzalez, Gillermo F; Puyana, Mónica; Castellanos, Leonardo; Ramos, Freddy A
Marine bacteria are considered as promising sources for the discovery of novel biologically active compounds. In this study, samples of sediment, invertebrate and algae were collected from the Providencia and Santa Catalina coral reef (Colombian Caribbean Sea) with the aim of isolating Actinobateria-like strain able to produce antimicrobial and quorum quenching compounds against pathogens. Several approaches were used to select actinobacterial isolates, obtaining 203 strains from all samples. According to their 16S rRNA gene sequencing, a total of 24 strains was classified within Actinobacteria represented by three genera: Streptomyces, Micromonospora, and Gordonia. In order to assess their metabolic profiles, the actinobacterial strains were grown in liquid cultures, and LC-MS-based analyses from ethyl acetate fractions were performed. Based on taxonomical classification, screening information of activity against phytopathogenic strains and quorum quenching activity, as well as metabolic profiling, six out of the 24 isolates were selected for follow-up with chemical isolation and structure identification analyses of putative metabolites involved in antimicrobial activities.
Badejo, Adebanjo A.; Damilare, Akintoroye; Ojuade, Temitope D.
The discovery of bioactive compounds in foods has changed the dietary lifestyle of many people. Cyperus esculentus (tigernut) is highly underutilized in Africa, yet tigernut extract is highly profitable in Europe. This study aims to add value to tigernut extract by revealing its health benefits and food value. In this study, tigernut tubers were germinated or roasted and the extracts were combined with Moringa oleifera extract (MOE) or Hibiscus sabdariffa extract (HSE) and spiced with ginger to produce functional drinks. The drinks were evaluated for physicochemical characteristics, sensory parameters, and antioxidant potentials. The total phenolic content of each beverage was measured by the Folin-Ciocalteu method, and the antioxidant activity of each beverage was determined by the 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid assays. The beverages from the germinated tigernut extracts had the highest titratable acidity and the lowest pH, while beverages containing the roasted tigernut extract had the highest ∘Brix. Germination and roasting significantly enhanced the total phenolic content of the drinks. The beverage containing HSE and germinated tigernut extract had a total phenolic content of 45.67 mg/100 mL gallic acid equivalents, which was significantly higher than the total phenolic content of all other samples. The DPPH inhibition activity of the beverages prepared with germinated tigernut extracts was significantly higher than the DPPH inhibition activity of the beverages prepared with fresh tigernut extract. The taste and overall acceptability of drinks containing the roasted tigernut extract were preferred, while the color and appearance of drinks with the germinated samples were preferred. Roasting or germinating tigernuts before extraction and addition of MOE or HSE extracts is another way to add value and enhance the utilization of tigernuts. PMID:25320721
Yu, Jin-Gao; Liu, Pei; Duan, Jin-Ao; Tang, Zong-Xiang; Yang, Yan
Colocasia esculenta (L.) Schoot (taro) is one of the most common crops in the world. Its rhizome was a tonic medicine and accustomed to treat some gastrointestinal disorders in traditional Chinese medicine. Today, the taro was further developed as anticancer prescription in herbal therapy. However, the mucilage of the fresh taro has irritation, and causes itchy feeling. The components in the mucilage were not evident up to now. Two active compounds, uracil and glycol-protein taro lectin (Accession number: A5HMM7), were purified and identified from the fresh taro. The glycol-protein taro lectin showed nerve stimulation activity on dorsal root ganglion (DRG) neurons from GCaMP transgenic mice at the concentration of 1mg/mL.
González-Ferrero, Carolina; Sáiz-Abajo, María-José
The characterization and stability evaluation of food and food constituents (chemical active ingredient/microorganism) for which nutrition or health claims want to be requested are essential for the success of an application to EFSA. This work reviews the requirements that must be fulfilled for a full characterization of the active substance, comprising origin, elaboration, or extraction method, and chemical/microbiological composition, using validated analytical methods. The review focuses not only on establishing the specifications of the final active ingredient or food but also on ensuring homogeneity between batches. In addition, the article discusses the methodologies and conditions of the stability studies that need to be performed on food and food constituents to verify that the relevant compounds--chemical and microbiological active ingredients--will get to the consumer in the intended state and concentration to accomplish the claimed health effect over shelf life.
El-Mostafa, Karym; El Kharrassi, Youssef; Badreddine, Asmaa; Andreoletti, Pierre; Vamecq, Joseph; El Kebbaj, M'Hammed Saïd; Latruffe, Norbert; Lizard, Gérard; Nasser, Boubker; Cherkaoui-Malki, Mustapha
Opuntia ficus-indica, commonly referred to as prickly pear or nopal cactus, is a dicotyledonous angiosperm plant. It belongs to the Cactaceae family and is characterized by its remarkable adaptation to arid and semi-arid climates in tropical and subtropical regions of the globe. In the last decade, compelling evidence for the nutritional and health benefit potential of this cactus has been provided by academic scientists and private companies. Notably, its rich composition in polyphenols, vitamins, polyunsaturated fatty acids and amino acids has been highlighted through the use of a large panel of extraction methods. The identified natural cactus compounds and derivatives were shown to be endowed with biologically relevant activities including anti-inflammatory, antioxidant, hypoglycemic, antimicrobial and neuroprotective properties. The present review is aimed at stressing the major classes of cactus components and their medical interest through emphasis on some of their biological effects, particularly those having the most promising expected health benefit and therapeutic impacts.
Custódio, Luísa; Laukaityte, Simona; Engelen, Aschwin H; Rodrigues, Maria João; Pereira, Hugo; Vizetto-Duarte, Catarina; Barreira, Luísa; Rodríguez, Hortensia; Alberício, Fernando; Varela, João
This work assessed the antioxidant potential, acetylcholinesterase (AChE) inhibition and the in vitro cytotoxic activity of extracts of the seagrasses Zostera marina and Zostera noltei collected from southern Portugal. The total phenolic contents (TPCs), the rosmarinic acid (RA) concentration (HPLC/DAD) and the fatty acid (FA) profile (GC/MS) are also described. Z. marina had the highest TPC, radical scavenging activity against DPPH radicals and copper chelating activity. Z. noltei had metal chelation capacity to copper and iron ions. None of the species was able to inhibit AChE. Both seagrasses had high levels of polyunsaturated FAs. Z. marina significantly and selectively reduced the viability of tumorous neuronal cells. Z. noltei was highly toxic for the three cell lines tested and was selective against hepatocarcinoma cells at the concentration of 100 μg/mL. RA was the main compound identified in Z. marina, but not in Z. noltei.
Geng, Haifeng; Tran-Gyamfi, Mary B.; Lane, Todd W.; Sale, Kenneth L.; Yu, Eizadora T.
Open microalgae cultures host a myriad of bacteria, creating a complex system of interacting species that influence algal growth and health. Many algal microbiota studies have been conducted to determine the relative importance of bacterial taxa to algal culture health and physiological states, but these studies have not characterized the interspecies relationships in the microbial communities. We subjected Nanochroloropsis salina cultures to multiple chemical treatments (antibiotics and quorum sensing compounds) and obtained dense time-series data on changes to the microbial community using 16S gene amplicon metagenomic sequencing (21,029,577 reads for 23 samples) to measure microbial taxa-taxa abundance correlations. Short-term treatment with antibiotics resulted in substantially larger shifts in the microbiota structure compared to changes observed following treatment with signaling compounds and glucose. We also calculated operational taxonomic unit (OTU) associations and generated OTU correlation networks to provide an overview of possible bacterial OTU interactions. This analysis identified five major cohesive modules of microbiota with similar co-abundance profiles across different chemical treatments. The Eigengenes of OTU modules were examined for correlation with different external treatment factors. This correlation-based analysis revealed that culture age (time) and treatment types have primary effects on forming network modules and shaping the community structure. Additional network analysis detected Alteromonadeles and Alphaproteobacteria as having the highest centrality, suggesting these species are “keystone” OTUs in the microbial community. Furthermore, we illustrated that the chemical tropodithietic acid, which is secreted by several species in the Alphaproteobacteria taxon, is able to drastically change the structure of the microbiota within 3 h. Taken together, these results provide valuable insights into the structure of the microbiota
Cerezo, Ana B.; Hornedo-Ortega, Ruth; Álvarez-Fernández, M. Antonia; Troncoso, Ana M.; García-Parrilla, M. Carmen
Excessive concentrations of vascular endothelial growth factor (VEGF) trigger angiogenesis, which causes complications such as the destabilization of atherosclerotic plaques and increased growth of tumors. This work focuses on the determination of the inhibitory activity of melatonin and other indolic related compounds on VEGF-induced VEGF receptor-2 (VEGFR-2) activation and an approximation to the molecular mechanism underlying the inhibition. Quantification of phosphorylated VEGFR-2 was measured by ELISA. Migration wound-healing assay was used to determine cell migration of human umbilical vein endothelial cells (HUVECs). This is the first time that melatonin, 3-indolacetic acid, 5-hydroxytryptophol, and serotonin are proved to significantly inhibit VEGF-induced VEGFR-2 activation in human umbilical vein endothelial cells and subsequent angiogenesis. 3-Indolacetic acid showed the highest inhibitory effect (IC50 value of 0.9704 mM), followed by 5-hydroxytryptophol (35% of inhibition at 0.1 mM), melatonin (30% of inhibition at 1 mM), and serotonin (24% of inhibition at 1 mM). An approximation to the molecular mechanism of the inhibition has been proposed, suggesting that indolic compounds might interact with the cell surface components of the endothelial membrane in a way that prevents VEGF from activating the receptor. Additionally, wound-healing assay revealed that exposure of HUVECs to melatonin and 3-indolacetic acid in the presence of VEGF significantly inhibited cell migration by 87% and 99%, respectively, after 24 h. These data demonstrate that melatonin, 3-indolacetic acid, 5-hydroxytryptophol, and serotonin would be good molecules for future exploitation as anti-VEGF signaling agents. PMID:28282869
Geng, Haifeng; Tran-Gyamfi, Mary B.; Lane, Todd W.; Sale, Kenneth L.; Yu, Eizadora T.
Open microalgae cultures host a myriad of bacteria, creating a complex system of interacting species that influence algal growth and health. Many algal microbiota studies have been conducted to determine the relative importance of bacterial taxa to algal culture health and physiological states, but these studies have not characterized the interspecies relationships in the microbial communities. Here we subjected Nanochroloropsis salina cultures to multiple chemical treatments (antibiotics and quorum sensing compounds) and obtained dense time-series data on changes to the microbial community using 16S gene amplicon metagenomic sequencing (21,029,577 reads for 23 samples) to measure microbial taxa-taxa abundance correlations. Short-term treatment with antibiotics resulted in substantially larger shifts in the microbiota structure compared to changes observed following treatment with signaling compounds and glucose. We also calculated operational taxonomic unit (OTU) associations and generated OTU correlation networks to provide an overview of possible bacterial OTU interactions. This analysis identified five major cohesive modules of microbiota with similar co-abundance profiles across different chemical treatments. The Eigengenes of OTU modules were examined for correlation with different external treatment factors. This correlation-based analysis revealed that culture age (time) and treatment types have primary effects on forming network modules and shaping the community structure. Additional network analysis detected Alteromonadeles and Alphaproteobacteria as having the highest centrality, suggesting these species are “keystone” OTUs in the microbial community. Furthermore, we illustrated that the chemical tropodithietic acid, which is secreted by several species in the Alphaproteobacteria taxon, is able to drastically change the structure of the microbiota within 3 h. Lastly, taken together, these results provide valuable insights into the structure of the