WorldWideScience

Sample records for bioactive compound libraries

  1. Natural products as an inspiration in the diversity-oriented synthesis of bioactive compound libraries

    OpenAIRE

    Cordier, Christopher; Morton, Daniel; Murrison, Sarah; Nelson, Adam; O'Leary-Steele, Catherine

    2008-01-01

    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 describ...

  2. An FDA-Drug Library Screen for Compounds with Bioactivities against Meticillin-Resistant Staphylococcus aureus (MRSA

    Directory of Open Access Journals (Sweden)

    Qiu Ying Lau

    2015-10-01

    Full Text Available The lack of new antibacterial drugs entering the market and their misuse have resulted in the emergence of drug-resistant bacteria, posing a major health crisis worldwide. In particular, meticillin-resistant Staphylococcus aureus (MRSA, a pathogen responsible for numerous human infections, has become endemic in hospitals worldwide. Drug repurposing, the finding of new therapeutic indications for approved drugs, is deemed a plausible solution to accelerate drug discovery and development in this area. Towards this end, we screened 1163 drugs approved by the Food and Drug Administration (FDA for bioactivities against MRSA in a 10 μM single-point assay. After excluding known antibiotics and antiseptics, six compounds were identified and their MICs were determined against a panel of clinical MRSA strains. A toxicity assay using human keratinocytes was also conducted to gauge their potential for repurposing as topical agents for treating MRSA skin infections.

  3. Five new bioactive compounds from Chenopodium ambrosioides.

    Science.gov (United States)

    Song, Kun; Zhang, Jian; Zhang, Peng; Wang, Hong-Qing; Liu, Chao; Li, Bao-Ming; Kang, Jie; Chen, Ruo-Yun

    2015-05-01

    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. PMID:26001043

  4. Chemically engineered extracts: source of bioactive compounds.

    Science.gov (United States)

    Ramallo, I Ayelen; Salazar, Mario O; Mendez, Luciana; Furlan, Ricardo L E

    2011-04-19

    Biological research and drug discovery critically depend on access to libraries of small molecules that have an affinity for biomacromolecules. By virtue of their sustained success as sources of lead compounds, natural products are recognized as "privileged" starting points in structural space for library development. Compared with synthetic compounds, natural products have distinguishing structural properties; indeed, researchers have begun to quantify and catalog the differences between the two classes of molecules. Measurable differences in the number of chiral centers, the degree of saturation, the presence of aromatic rings, and the number of the various heteroatoms are among the chief distinctions between natural and synthetic compounds. Natural products also include a significant proportion of recurring molecular scaffolds that are not present in currently marketed drugs: the bioactivity of these natural substructures has been refined over the long process of evolution. In this Account, we present our research aimed at preparing libraries of semisynthetic compounds, or chemically engineered extracts (CEEs), through chemical diversification of natural products mixtures. The approach relies on the power of numbers, that is, in the chemical alteration of a sizable fraction of the starting complex mixture. Major changes in composition can be achieved through the chemical transformation of reactive molecular fragments that are found in most natural products. If such fragments are common enough, their transformation represents an entry point for chemically altering a high proportion of the components of crude natural extracts. We have searched for common reactive fragments in the Dictionary of Natural Products (CRC Press) and identified several functional groups that are expected to be present in a large fraction of the components of an average natural crude extract. To date, we have used reactions that incorporate (i) nitrogen atoms through carbonyl groups, (ii

  5. Bioactive compounds in whole grain wheat

    OpenAIRE

    Mateo Anson, N.

    2010-01-01

    Bread can be healthier! Consuming whole-grain foods can prevent cardiovascular diseases, type-2 diabetes and metabolic syndrome. This is due to bioactive compounds in whole grain, such as antioxidants and anti-inflammatory compounds. We found that the different fractions of a wheat grain vary much in their content. The external fractions of the grain, the bran and specially the aleurone, are the richest. We observed that processing the bran in whole-grain breads increased three times the leve...

  6. Bioactive compounds from Carissa spinarum.

    Science.gov (United States)

    Wangteeraprasert, Ruchira; Lipipun, Vimolmas; Gunaratnam, Mekala; Neidle, Stephen; Gibbons, Simon; Likhitwitayawuid, Kittisak

    2012-10-01

    In our continuing efforts to find new antiherpetic agents from plants, an extract prepared from the stems of Carissa spinarum L. was found to possess appreciable activity against herpes simplex viruses (HSV I and II). A chemical study of this plant was then initiated, and this led to the isolation of 12 compounds, including a coumarin, two cardiac glycosides and nine lignans. These isolated compounds were evaluated for several biological activities, including antiherpetic, cytotoxic, antioxidant and antibacterial effects. The cardiac glycoside evomonoside was found to be the only antiherpetic principle, showing moderate activity against herpes simplex virus types I and II in the inactivation method. The lignans (-)-carinol, (-)-carissanol and (-)-nortrachelogenin exhibited cytotoxicity against breast (MCF7) and lung (A549) cancer cells. Moderate anti-DPPH free radical activity was observed for all the lignans. None of the isolates showed antibacterial activity. PMID:22308099

  7. Bioactive compounds from northern plants.

    Science.gov (United States)

    Hohtola, Anja

    2010-01-01

    Northern conditions are characterised by long days with much light and low temperatures during the growing season. It has been chimed that herbs and berries grown in the north are stronger tasting compared to those of southern origin. The compounds imparting aroma and color to berries and herbs are secondary metabolites which in plants mostly act as chemical means of defense. Recently, the production of secondary metabolites using plant cells has been the subject of expanding research. Light intensity, photoperiod and temperature have been reported to influence the biosynthesis of many secondary metabolites. Native wild aromatic and medicinal plant species of different families are being studied to meet the needs of raw material for the expanding industry of e.g., health-promoting food products known as nutraceutics. There are already a large number of known secondary compounds produced by plants, but the recent advances in modern extraction and analysis should enable many more as yet unknown compounds to be found, characterised and utilised. Rose root (Rhodiola rosea) is a perennial herbaceous plant which inhabits mountain regions throughout Europe, Asia and east coastal regions of North America. The extract made from the rhizomes acts as a stimulant like the Ginseng root. Roseroot has been categorized as an adaptogen and is reported to have many pharmacological properties. The biologically active components of the extract are salitroside tyrosol and cinnamic acid glycosides (rosavin, rosarin, rosin). Round-leaved sundew (Drosera rotundifolia L.) has circumboreal distribution. It inhabits nutrient-poor, moist and sunny areas such as peat bogs and wetlands. Sundew leaves are collected from the wild-type for various medicinal preparations and can be utilized in treating e.g., as an important "cough-medicine" for different respiratory diseases. The antimicrobial activity of extracts of aerial parts against various bacteria has been investigated. Drosera produces

  8. Structural Library of Natural Compounds

    Directory of Open Access Journals (Sweden)

    Subhash Chandra Bose Kotte

    2011-07-01

    Full Text Available Natural products with biological activity are of considerable interest to drug discovery community and a structural library of such compounds serves as data set for insilico experiments to predict the target specific activity before screening them in in-vitro experiments. This work leverages open source scientific tools to create a database of such compounds library in Structure Data Format with 3D coordinates which in turn may be used as an input file for various applications.

  9. NOVEL BIOACTIVE COMPOUNDS FROM MANGROVE DERIVED ACTINOMYCETES

    OpenAIRE

    Kumari Amrita; Jain Nitin; Subathra Devi, C.

    2012-01-01

    Mangrove is most productive and unexplored ecosystem that approximately covers one fourth of world coastline with high diversity of thriving organism. Recently the rate of isolation of novel bioactive compounds from microorganism living in mangrove forest has tremendously increased which is reflected in significant hasten for exploration of mangrove actinomycetes. Actinomycetes are group of bacteria which are extremely interesting as active producers of many primary and secondary metabolites....

  10. Nanoencapsulation of bioactive compounds for food applications

    OpenAIRE

    Sessa, Mariarenata

    2012-01-01

    2010 - 2011 The increase in dietary-intake-related illnesses, such as obesity, cardiovascular diseases, hypertension, diabetes and cancer, have made in recent years the development of health-and-wellness promoting foods a priority of the food industry. Clinical studies have demonstrated tangible health benefits that may be derived from the intake of bioactive compounds. However many difficulties are associated with their inclusion in food matrices, due to a very low solubility in water and...

  11. Bioactive Compounds Found in Brazilian Cerrado Fruits

    OpenAIRE

    Elisa Flávia Luiz Cardoso Bailão; Ivano Alessandro Devilla; Edemilson Cardoso da Conceição; Leonardo Luiz Borges

    2015-01-01

    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 provi...

  12. Bioactive Compounds Found in Brazilian Cerrado Fruits

    Directory of Open Access Journals (Sweden)

    Elisa Flávia Luiz Cardoso Bailão

    2015-10-01

    Full Text Available 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.

  13. Bioactive Compounds Found in Brazilian Cerrado Fruits.

    Science.gov (United States)

    Bailão, Elisa Flávia Luiz Cardoso; Devilla, Ivano Alessandro; da Conceição, Edemilson Cardoso; Borges, Leonardo Luiz

    2015-01-01

    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

  14. Isolation and characterization of regulatory peptides and bioactive compounds

    OpenAIRE

    Norberg, Åke

    2004-01-01

    Isolation of peptides and other bioactive compounds is an important and often necessary step to get the total information about their structures. This is demonstrated by a number of different characterizations in this thesis. Bioactive peptides and small organic molecules can act as signaling substances and messengers in multicellular organisms and are fundamental to higher forms of life. The following bioactive peptides and compounds were studied. 1) Different assays ca...

  15. Bioactive compounds: Safety and efficacy (Consensus Meeting - Part II)

    NARCIS (Netherlands)

    Biesalski, H.K.; Dragsted, L.O.; Elmadfa, I.; Grossklaus, R.; Müller, M.R.; Schrenk, D.; Walter, P.; Weber, P.

    2009-01-01

    The efficacy and safety of bioactive compounds depend on a few known and unknown parameters. What is a physiologic dose and how can that dose be defined in cases of bioactive compounds with a poor knowledge of supply and distribution? What safety sets are needed? How can individual aspects such as p

  16. Radiation Parameters of Some Potential Bioactive Compounds

    Institute of Scientific and Technical Information of China (English)

    Zeynep Gedik; Mehtap Tugrak; Aysenur Dastan; Haliseinci Gul; Demet YIlmaz

    2015-01-01

    In this study ,we aimed to determine the radiation parameters of some potential bioactive com‐pounds .1‐Aryl‐3‐dibenzylamino‐propane‐1‐on hydrochloride type Mannich bases were synthesized via classical conventional heating method .Aryl part was changed as phenyl (C6 H5 ) ,4‐methylphenyl (4‐CH3 C6 H4 ) ,4‐flu‐orophenyl (4‐FC6 H4 ) , 4‐nitrophenyl (4‐NO2 C6 H4 ) , 4‐chlorophenyl (4‐ClC6 H4 ) , 4‐bromophenyl (4‐BrC6 H4 ) ,and 2‐thienyl (C4 H3 S‐2‐yl) .Mass attenuation coefficient (μm ) ,effective atomic number (Zef ) and effective electron density (Nel ) of compounds were determined experimentally and theoretically for at 8.040 , 8.910 ,13.40 ,14.96 ,17.48 ,19.61 ,22.16 ,24.94 ,32.19 ,36.38 ,44.48 ,50.38 and 59.54 keV photon en‐ergies by using an HPGe detector with a resolution of 182 eV at 5.9 keV .Radiation parameters of these com‐pounds which can be anti‐cancer drug candidate were given in the tables .The results show that phenyl ring be‐have like thiophene ring in terms of radiation absorption .It is thought that the results of study may drive allow the development of drug candidate new compounds in medical oncology .

  17. Bioactive Compounds and Antioxidant Activity in Different Types of Berries

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    Sona Skrovankova

    2015-10-01

    Full Text Available 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.

  18. Bioactive Compounds and Antioxidant Activity in Different Types of Berries.

    Science.gov (United States)

    Skrovankova, Sona; Sumczynski, Daniela; Mlcek, Jiri; Jurikova, Tunde; Sochor, Jiri

    2015-01-01

    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

  19. Phenolic waste valorization through bioenergy and bioactive compounds production [Resumo

    OpenAIRE

    Marques, Isabel Paula Ramos; Morana, A; La Cara, F.

    2014-01-01

    The agricultural and industrial processing activities produce large amounts of waste that are only partially valorised at different value-added levels (spread on land, animal feed, composting), whereas the main volumes are managed as waste of environmental worry. These by-products are rich sources of bioactive compounds, including phenolic compounds with high antioxidant activity.

  20. Bioactive Compounds from Marine Bacteria and Fungi

    OpenAIRE

    Debbab, Abdessamad; Aly, Amal H.; Lin, Wen H.; Proksch, Peter

    2010-01-01

    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 me...

  1. Jellyfish Bioactive Compounds: Methods for Wet-Lab Work.

    Science.gov (United States)

    Frazão, Bárbara; Antunes, Agostinho

    2016-04-01

    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

  2. Mass spectrometry for determination of bioactive compounds

    Digital Repository Service at National Institute of Oceanography (India)

    Tilvi, S.; Majik, M.S.; Singh, K.S.

    cell. This type of experiment is particularly useful for monitoring groups of compounds contained within a mixture which fragment to produce common fragment ions, e.g. glycosylated peptides in a tryptic digest mixture, aliphatic hydrocarbons in an oil... in a matrix e.g. drug testing with blood or urine samples. It is not only a highly specific method but also has very high sensitivity. For known compounds, mass spectra can be used much like fingerprints. A match is extremely strong evidence...

  3. Immense Essence of Excellence: Marine Microbial Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Ira Bhatnagar

    2010-10-01

    Full Text Available 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.

  4. Bioactive compounds in baby spinach (Spinacia oleracea L.)

    OpenAIRE

    Bergquist, Sara

    2006-01-01

    A high intake of fruit and vegetables is well known to have positive effects on human health, and has been correlated to a decreased risk of most degenerative diseases of ageing, such as cardiovascular disease, cataracts and several forms of cancer. These protective effects have been attributed to high concentrations of bioactive compounds (ascorbic acid, flavonoids, carotenoids) in fruit and vegetables, partly due to the antioxidative action of some of these compounds. Maintaining a high lev...

  5. Nocardiopsis species: a potential source of bioactive compounds.

    Science.gov (United States)

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

    2016-01-01

    Members of the genus Nocardiopsis are an ecologically versatile and biotechnologically important group of Actinomycetes. Most of the isolates are halotolerant or halophilic and they prevail in soils, marine environments or hypersaline locations. To aid their survival under these conditions, they mainly produce extremozymes, compatible solutes, surfactants and bioactive compounds. The current review details the bioactive compounds obtained for this genus. Important antimicrobial agents obtained from this genus include polyketides, phenzines, quinoline alkaloids, terphenyls, proteins, thiopeptides and amines. Polyketides and peptides displaying potent anticancer activities are also significant. Tumour promoting agents, P-glycoprotein (P-gp) inhibitors, immunomodulators and protein kinase inhibitors are other relevant products obtained from Nocardiopsis species. Structurally, polyketides (synthesized by polyketide synthases) and peptides (made by nonribosomal peptide synthetases or cyclodipeptide synthases) are important compounds. Considered here are also toxins, anti photoaging and adipogenic agents produced by this genus. The gene clusters mediating the synthesis of bioactive compounds have been described. Commercially available products (Apoptolidins and K-252a) derived from this genus have also been described. This review highlights the significance of a single genus in producing an assortment of compounds with varied biological activities. On account of these features, the members of this genus have established a place for themselves and are of considerable value in producing compounds with profound bio-medical applications. PMID:26369300

  6. Bioactive compounds from Iostephane heterophylla (Asteraceae).

    Science.gov (United States)

    Aguilar, M I; Delgado, G; Hernández, M L; Villarreal, M L

    2001-01-01

    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. PMID:11561451

  7. Isolation and identification of bioactive compounds in Andrographis paniculata (Chuanxinlian)

    OpenAIRE

    Lin Bi-Fong; Chao Wen-Wan

    2010-01-01

    Abstract Andrographis paniculata (Burm. f.) Nees (Acanthaceae) is a medicinal plant used in many countries. Its major constituents are diterpenoids, flavonoids and polyphenols. Among the single compounds extracted from A. paniculata, andrographolide is the major one in terms of bioactive properties and abundance. Among the andrographolide analogues, 14-deoxy-11,12-didehydroandrographolide is immunostimulatory, anti-infective and anti-atherosclerotic; neoandrographolide is anti-inflammatory, a...

  8. Compressed fluids for the extraction of bioactive compounds

    OpenAIRE

    Herrero, Miguel; Castro-Puyana, M.; Mendiola, J. A.; Ibáñez, Elena

    2013-01-01

    The improvement of sample-preparation and extraction techniques for determinations of natural bioactive compounds is very important. New concepts relate to not only enhancement of extraction efficiencies but also environmental impact. This evolution towards Green Analytical Chemistry is to new extraction and sample-preparation processes that should be faster, more reproducible and more environmentally friendly.Compressed fluid-based sample-preparation techniques (e.g., supercritical fluid ext...

  9. Echinoderms: their culture and bioactive compounds.

    Science.gov (United States)

    Kelly, M S

    2005-01-01

    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. PMID:17152697

  10. Bioactive compounds and antioxidant activity analysis of Malaysian pineapple cultivars

    Science.gov (United States)

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

    2014-03-01

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

  11. Bioactive compounds of sea cucumbers and their therapeutic effects

    Science.gov (United States)

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

    2015-11-01

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

  12. Variation of bioactive compounds content of 14 oriental strawberry cultivars.

    Science.gov (United States)

    Kim, Sung Kyeom; Kim, Dong Sub; Kim, Dae Young; Chun, Changhoo

    2015-10-01

    Variation in bioactive compounds content was assessed in antioxidant rich June-bearing strawberry cultivars. Ascorbic acid, anthocyanin, and ellagic acid content were analyzed in ripe fruits of 14 cultivars. The bioactive content in strawberry fruit was found to vary significantly among cultivars and from year to year. The highest ascorbic acid content was found in 'Sugyeong'. The 'Red Pearl' and 'Sachinoka' had three to fourfold higher amounts of pelargonidin 3-glucoside than other cultivars. For cyanidin 3-glucoide and pelargonidin 3-rutinoside, two other characterized anthocyanins, 'Dahong' and 'Keumhyang' had the highest contents among all the tested cultivars. The ellagic acid content of 'Dahong' was generally all within the upper ranges. These results can be used for the validation of fruit antioxidant capacity and in addition, provide useful information for breeding programs looking to enhance the antioxidant capacity in strawberry fruit. PMID:25872444

  13. Bioactive compounds of sea cucumbers and their therapeutic effects

    Science.gov (United States)

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

    2016-05-01

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

  14. Fruits Bioactive Compounds Characterization from a New Food Product

    Directory of Open Access Journals (Sweden)

    Valentina Mariana RUS

    2014-12-01

    Full Text Available The aim of this study was (I to create a new product, smart bar type which can be consumed as protective food by adults and children (II to characterize the bioactive compounds from the designed food. The bioactive compounds were identified from nuts, raw seeds of almonds, dry cranberries, dry plums and flax seeds. Secoisolariciresinol (683 ppm has been identified as a major compound in flax seeds.  The vitamin C was quantified by HPLC in a concentration of 35.02 mg% in cranberries extract. The total phenolic content varied from 7.1 mg/g for walnut to 71.8 mg/g for cranberries. In addition, the antioxidative capability of phenolic compounds was monitored and evaluated using a colored free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH. Almond showed better results than walnut in the antioxidant capacity test. The results obtained in this study collect information that enables the use of nuts, raw seeds of almonds, dry cranberries, dry plums and flax seeds as raw material for the production of smart bar which may serve as a new product for food market.

  15. Accurate Dereplication of Bioactive Secondary Metabolites from Marine-Derived Fungi by UHPLC-DAD-QTOFMS and a MS/HRMS Library

    DEFF Research Database (Denmark)

    Kildgaard, Sara; Mansson, Maria; Dosen, Ina;

    2014-01-01

    -DAD-QTOFMS) providing both accurate mass full-scan mass spectrometry (MS) and tandem high resolution MS (MS/HRMS) data. The methodology was demonstrated on compounds from bioactive marine-derived strains of Aspergillus, Penicillium, and Emericellopsis, including small polyketides, non-ribosomal peptides, terpenes, and......In drug discovery, reliable and fast dereplication of known compounds is essential for identification of novel bioactive compounds. Here, we show an integrated approach using ultra-high performance liquid chromatography-diode array detection-quadrupole time of flight mass spectrometry (UHPLC...... meroterpenoids. The MS/HRMS data were then searched against an in-house MS/HRMS library of ~1300 compounds for unambiguous identification. The full scan MS data was used for dereplication of compounds not in the MS/HRMS library, combined with ultraviolet/visual (UV/Vis) and MS/HRMS data for faster exclusion of...

  16. Bioactive compounds in seaweed; functional food applications and legislation

    DEFF Research Database (Denmark)

    Holdt, Susan Løvstad; Kraan, Stefan

    2011-01-01

    Seaweed is more than the wrap that keeps rice together in sushi. Seaweed biomass is already used for a wide range of other products in food, including stabilising agents. Biorefineries with seaweed as feedstock are attracting worldwide interest and include low-volume, high value-added products an...... of uses to enhance comparisons. In addition, scientific experiments performed on seaweed used as animal feed are presented, and EU, US and Japanese legislation on functional foods is reviewed.......Seaweed is more than the wrap that keeps rice together in sushi. Seaweed biomass is already used for a wide range of other products in food, including stabilising agents. Biorefineries with seaweed as feedstock are attracting worldwide interest and include low-volume, high value-added products...... and vice versa. Scientific research on bioactive compounds in seaweed usually takes place on just a few species and compounds. This paper reviews worldwide research on bioactive compounds, mainly of nine genera or species of seaweed, which are also available in European temperate Atlantic waters, i...

  17. Metabolites identification of bioactive licorice compounds in rats.

    Science.gov (United States)

    Wang, Qi; Qian, Yi; Wang, Qing; Yang, Yan-Fang; Ji, Shuai; Song, Wei; Qiao, Xue; Guo, De-An; Liang, Hong; Ye, Min

    2015-11-10

    Licorice (Glycyrrhiza uralensis Fisch.) is one of the most popular herbal medicines worldwide. This study aims to identify the metabolites of seven representative bioactive licorice compounds in rats. These compounds include 22β-acetoxyl glycyrrhizin (1), licoflavonol (2), licoricidin (3), licoisoflavanone (4), isoglycycoumarin (5), semilicoisoflavone B (6), and 3-methoxy-9-hydroxy-pterocarpan (7). After oral administration of 250mg/kg of 1 or 40mg/kg of 2-7 to rats, a total of 16, 43 and 31 metabolites were detected in the plasma, urine and fecal samples, respectively. The metabolites were characterized by HPLC/DAD/ESI-MS(n) and LC/IT-TOF-MS analyses. Particularly, two metabolites of 1 were unambiguously identified by comparing with reference standards, and 22β-acetoxyl glycyrrhizin-6″-methyl ester (1-M2) is a new compound. Compound 1 could be readily hydrolyzed to eliminate the glucuronic acid residue. The phenolic compounds (4-7) mainly undertook phase II metabolism (glucuronidation or sulfation). Most phenolic compounds with an isoprenyl group (chain or cyclized, 2-5) could also undertake hydroxylation reaction. This is the first study on in vivo metabolism of these licorice compounds. PMID:26311472

  18. Effect of Dietary Bioactive Compounds on Mitochondrial and Metabolic Flexibility

    Directory of Open Access Journals (Sweden)

    Jose C. E. Serrano

    2016-03-01

    Full Text Available Metabolic flexibility is the capacity of an organism to adequately respond to changes in the environment, such as nutritional input, energetic demand, etc. An important player in the capacity of adaptation through different stages of metabolic demands is the mitochondrion. In this context, mitochondrial dysfunction has been attributed to be the onset and center of many chronic diseases, which are denoted by an inability to adapt fuel preferences and induce mitochondrial morphological changes to respond to metabolic demands, such as mitochondrial number, structure and function. Several nutritional interventions have shown the capacity to induce changes in mitochondrial biogenesis/degradation, oxidative phosphorylation efficiency, mitochondrial membrane composition, electron transfer chain capacity, etc., in metabolic inflexibility states that may open new target options and mechanisms of action of bioactive compounds for the treatment of metabolic diseases. This review is focused in three well-recognized food bioactive compounds that modulate insulin sensitivity, polyphenols, ω-3 fatty acids and dietary fiber, by several mechanism of action, like caloric restriction properties and inflammatory environment modulation, both closely related to mitochondrial function and dynamics.

  19. Isolation and identification of bioactive compounds in Andrographis paniculata (Chuanxinlian

    Directory of Open Access Journals (Sweden)

    Lin Bi-Fong

    2010-05-01

    Full Text Available Abstract Andrographis paniculata (Burm. f. Nees (Acanthaceae is a medicinal plant used in many countries. Its major constituents are diterpenoids, flavonoids and polyphenols. Among the single compounds extracted from A. paniculata, andrographolide is the major one in terms of bioactive properties and abundance. Among the andrographolide analogues, 14-deoxy-11,12-didehydroandrographolide is immunostimulatory, anti-infective and anti-atherosclerotic; neoandrographolide is anti-inflammatory, anti-infective and anti-hepatotoxic; 14-deoxyandrographolide is immunomodulatory and anti-atherosclerotic. Among the less abundant compounds from A. paniculata, andrograpanin is both anti-inflammatory and anti-infective; 14-deoxy-14,15-dehydroandrographolide is anti-inflammatory; isoandrographolide, 3,19-isopropylideneandrographolide and 14-acetylandrographolide are tumor suppressive; arabinogalactan proteins are anti-hepatotoxic. The four flavonoids from A. paniculata, namely 7-O-methylwogonin, apigenin, onysilin and 3,4-dicaffeoylquinic acid are anti-atherosclerotic.

  20. Encapsulating fatty acid esters of bioactive compounds in starch

    Science.gov (United States)

    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

  1. Amazonian Native Palm Fruits as Sources of Antioxidant Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Mary de Fátima Guedes dos Santos

    2015-09-01

    Full Text Available 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.

  2. Production of Bioactive Compounds by Bacillus subtilis against Sclerotium rolfsii

    Directory of Open Access Journals (Sweden)

    Nalisha, I.

    2006-01-01

    Full Text Available This study aims to investigate the characteristic of bioactive compound produced by Bacillus subtilis against Sclerotium rolfsii and the influence of additive supplements on the antagonistic activity of B. subtilis. The fact that B. subtilis produced an antifungal substance which has inhibitory effect on wide range of fungi, including S. rolfsii, is well known. To learn the effect of pH, temperature and light condition on the production of antifungal compound, B. subtilis was inoculated in Potato Dextrose Broth at various initial pH, temperatures and light conditions, respectively. This antagonist was found to produce antifungal compound that stable at 80C with 58.3 % inhibition on S. rolfsii. The activity was constant within a wide range of pH (3–11. However, treatment with pH11 lead to higher antifungal activity (31.57 % inhibition and it was also found to produce substance that can endure dark condition (46.24 % inhibition with fungicidal effect on S. rolfsii. A series of experiments also been carried out to enhance the antifungal production by supplementing different carbon source preparation into bacterial liquid culture. B. subtilis were grown in minimal medium containing 1 % of oil palm root, Ganoderma lucidum or chitin, respectively prior to bioassay. Crude culture from oil palm root supplemented culture shown significantly reduction in S. rolfsii growth compared to other carbon source crude culture or the antagonism alone, suggesting that this approach may provide improved biocontrol efficiency.

  3. Rosmarinus Officinalis Leaves as a Natural Source of Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Isabel Borrás-Linares

    2014-11-01

    Full Text Available 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.

  4. Carrier system for a plant extract or bioactive compound from a plant

    DEFF Research Database (Denmark)

    2016-01-01

    This invention relates to a carrier system for use in producing a beverage with a metered amount of plant extract or bioactive compound.......This invention relates to a carrier system for use in producing a beverage with a metered amount of plant extract or bioactive compound....

  5. Determination of bioactive and potentially toxic compounds in food: raw material analysis and shelf life evaluation

    OpenAIRE

    Verardo, Vito

    2009-01-01

    "Bioactive compounds" are extranutritional constituents that typically occur in small quantities in food. They are being intensively studied to evaluate their effects on health. Bioactive compounds include both water soluble compounds, such as phenolics, and lipidic substances such as n-3 fatty acids, tocopherols and sterols. Phenolic compounds, tocopherols and sterols are present in all plants and have been studied extensively in cereals, nuts and oil. n-3 fatty acids are pres...

  6. Antioxidant capacity and bioactive compounds of four Brazilian native fruits

    Directory of Open Access Journals (Sweden)

    Cristiane C. Denardin

    2015-09-01

    Full Text Available The purpose of this study was to evaluate the bioactive compounds and antioxidant activity of extracts from araçá (Psidium cattleianum, butiá (Butia eriospatha, and pitanga (Eugenia uniflora fruits with different flesh colors (i.e., purple, red, and orange, and blackberries (Rubus sp.; cv. Xavante and Cherokee collected in the southern region of Brazil. The content of ascorbic acid, total carotenoids, and phenolics were determined. The profile of the phenolic compounds was assessed by high-performance liquid chromatography combined with diode array detection (HPLC-DAD. The antioxidant activity was determined using the ferric-reducing antioxidant power (FRAP assay, 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH assay, total reactive antioxidant potential (TRAP assay, and total antioxidant reactivity (TAR assay. The Xavante blackberry and purple-fleshed pitanga showed the highest total phenolic content [816.50 mg gallic acid equivalents (GAE/100g and 799.80 mg GAE/100g, respectively]. The araçá and red-fleshed pitanga showed the highest carotenoid content (6.27 ug β-carotene/g and 5.86 ug β-carotene/g, respectively. The fruits contained several phenolic compounds such as quercetin derivatives, quercitrin, isoquercitrin, and cyanidin derivatives, which may contribute differentially to the antioxidant capacity. The highest scavenging activity in the DPPH assay was found for purple-fleshed pitanga (IC50 36.78 mg/L, blackberries [IC50 44.70 (Xavante and IC50 78.25 mg/L (Cherokee], and araçá (IC50 48.05 mg/L, which also showed the highest FRAP, followed by orange- and red-fleshed pitanga. Our results revealed that some fruits grown in southern Brazil such as purple-fleshed pitanga, blackberries, and araçá are rich sources of phenolic compounds and have great antioxidant activity.

  7. Potential Bioactive Compounds from Seaweed for Diabetes Management

    Directory of Open Access Journals (Sweden)

    Yusrizam Sharifuddin

    2015-08-01

    Full Text Available 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.

  8. The effects of bioactive compounds on biomarkers of obesity

    Directory of Open Access Journals (Sweden)

    Rebecca Coats

    2015-11-01

    Full Text Available Background: The world is presently facing a prolonged struggle without a predictable cure. Obesity causes hundreds of thousands of fatalities each year, along with holding a position as a primary contributor to several other virulent chronic diseases. This review of scientific literature will examine the current state of obesity along with the mechanisms and biomarkers that lay the foundation for the development of the disease. Furthermore, this article will assess several functional foods and the bioactive compounds they contain that play an influential role in the prevention and treatment of obesity as a chronic disease. By presenting many relevant functional food research studies, this review aims to offer auxiliary support to traditional obesity treatments. The topic of functional foods and their relation to obesity is an extremely important topic to explore due to the severe expansion of obesity in the past few decades. Overall, the purpose of this review is to supply a comprehensive description of obesity and examine results of functional foods in clinical trials that may offer innovative benefits.

  9. Evaluating the potential bioactivity of a novel compound ER1626.

    Directory of Open Access Journals (Sweden)

    Lijun Wang

    Full Text Available BACKGROUND: ER1626, a novel compound, is a derivate of indeno-isoquinoline ketone. This study was designed to evaluate the biological activity and potential anti-tumor mechanism of ER1626. METHOD: MTT assay, scratch assay and flow cytometry were used to determine cell proliferation, cell migration and cell cycle distribution as well as cell apoptosis on human breast cancer MCF-7 cells and endometrial cancer Ishikawa cells. We also explored the antiangiogenic effect of ER1626 on HUVEC cells and chicken embryos. The expression of estrogen receptor protein was investigated with western-blot analysis. RESULTS: ER1626 down-regulated the expression of estrogen receptor α protein and up-regulated β protein in MCF-7 and Ishikawa cells. The value of IC50 of ER1626 on MCF-7 and Ishikawa cells were respectively 8.52 and 3.08 µmol/L. Meanwhile, ER1626 decreased VEGF secretion of MCF-7 and Ishikawa cells, disturbed the formation of VEGF-stimulated tubular structure in HUVEC cells, and inhibited the angiogenesis on the chicken chorioallantoic membrane. Scratch assay revealed that ER1626 suppressed the migration of MCF-7, Ishikawa and HUVEC cells. In addition to induction tumor cell apoptosis, ER1626 arrested cell cycle in G1/G0 phase in MCF-7 cells and G2/M phase in Ishikawa cells. CONCLUSION: In conclusion, our results demonstrated that ER1626 has favorable bioactivities to be a potential candidate against breast cancer and angiogenesis.

  10. BIOACTIVE COMPOUNDS IN COMMONLY UTILIZED LEGUME CULTIVARS FROM IRAQ

    Directory of Open Access Journals (Sweden)

    Dalaram S. Ismael

    2013-02-01

    Full Text Available Total polyphenol content as well as total antioxidant capacity in three chickpea, four fababean and four lentil cultivars from regions of Iraq with different environmental growth conditions were investigated in the work. The total polyphenol content (TP was estimated using Folin-Ciocalteau assay and the total antioxidant capacity (TAC of legume extracts was measured using the DPPH spectrophotometrically. The obtained results confirmed that the polyphenols content in the tested legume cultivars was influenced by locality. From tested legumes the highest polyphenol content was measured in fababean (1220 – 6286 mg GAE.kg-1. In lentil (2351 – 3011 mgGAE.kg-1 the average TP value was slightly lower (by 1,6%, while in chickpea (549 – 978 mg GAE.kg-1 it was dramatically (by 71,5% lower in comparison to fababean. The similar trend was observed at values of TAC. The highest average TAC value was determined in fababean (15.2 – 25.6% DPPH, in lentil (14.2 – 28.9% DPPH the TAC value was by 2% and in chickpea (1.9 – 4.5% DPPH by 83,6% lower in comparison to fababean. Only in lentil a statistically strong correlation (P-value 2.391E-06; R = 0.802 was found. Our results confirmed that legumes can be a good source of bioactive compounds in the human nutrition.

  11. Bioactive Compounds of Aristotelia chilensis Stuntz and their Pharmacological Effects.

    Science.gov (United States)

    Romanucci, Valeria; D'Alonzo, Daniele; Guaragna, Annalisa; Di Marino, Cinzia; Davinelli, Sergio; Scapagnini, Giovanni; Di Fabio, Giovanni; Zarrelli, Armando

    2016-01-01

    Aristotelia chilensis ([Molina], Stuntz) a member of the family Eleocarpaceae, is a plant native to Chile that is distributed in tropical and temperate Asia, Australia, the Pacific Area, and South America. The juice of its berries has important medicinal properties, as an astringent, tonic, and antidiarrhoeal. Its many qualities make the maqui berry the undisputed sovereign of the family of so-called "superfruits", as well as a valuable tool to combat cellular inflammation of bones and joints. Recently, it is discovered that the leaves of the maqui berry have important antibacterial and antitumour activities. This review provides a comprehensive overview of the traditional use, phytochemistry, and biological activity of A. chilensis using information collected from scientific journals, books, and electronic searches. Anthocyanins, other flavonoids, alkaloids, cinnamic acid derivatives, benzoic acid derivatives, other bioactive molecules, and mineral elements are summarized. A broad range of activities of plant extracts and fractions are presented, including antioxidant activity, inhibition of visible light-induced damage of photoreceptor cells, inhibition of α-glucosidase, inhibition of pancreatic lipase, anti-diabetic effects, anti-inflammatory effects, analgesic effects, anti-diabetes, effective prevention of atherosclerosis, promotion of hair growth, anti-photo ageing of the skin, and inhibition of lipid peroxidation. Although some ethnobotanical uses have been supported in in vitro experiments, further studies of the individual compounds or chemical classes of compounds responsible for the pharmacological effects and the mechanisms of action are necessary. In addition, the toxicity and the side effects from the use of A. chilensis, as well as clinical trials, require attention. PMID:26778456

  12. Bioactive compounds in potatoes: Accumulation under drought stress conditions

    Directory of Open Access Journals (Sweden)

    Christina B. Wegener

    2015-03-01

    Full Text Available Background: Potato (Solanum tuberosum is a valuable source of bioactive compounds. Besides starch, crude fibre, amino acids (AAS, vitamins and minerals, the tubers contain diverse phenolic compounds. These phenolics and AAS confer anti-oxidant protection against reactiveoxygen species, tissue damage, and diseases like atherosclerosis, renal failure, diabetes mellitus,and cancer. Climate change and drought stress may become a major risk for crop production worldwide, resulting in reduced access for those who depend on the nutritional value of this staple crop. Objective: The aim of this study is to determine the effect of drought stress on water, lipid soluble antioxidants, anthocyanins (Ac, soluble phenols, proteins, free AAS, peroxidase (POD and lipid acyl hydrolase activity (LAH in tuber tissue. Methods: The study was carried out on three potato genotypes comprising one yellow-fleshed cultivar and two purple breeding clones. The plants were grown in pots (from April to September in a glasshouse with sufficient water supply and under drought stress conditions. After harvest, the tubers of both variants were analysed for antioxidants measured as ascorbic acid (ACE and Trolox equivalent (TXE using a photo-chemiluminescent method. Amounts of anthocyanins (Ac, soluble phenols, proteins, as well as POD and LAH activities were analysed using a UV photometer. Finally, free AAS were measured by HPLC. Results: The results revealed that drought stress significantly reduces tuber yield, but has no significant effect on antioxidants, Ac, soluble phenols and POD. Drought stress significantly increased the levels of soluble protein (P < 0.0001 and LAH (P < 0.001. Also, total amounts of free AAS were higher in the drought stressed tubers (+34.2%, on average than in the tubers grown with a sufficient water supply. Above all, proline was elevated due to drought stress.

  13. Cheminformatics approaches to analyze diversity in compound screening libraries.

    Science.gov (United States)

    Akella, Lakshmi B; DeCaprio, David

    2010-06-01

    As high-throughput screening matures as a discipline, cheminformatics is playing an increasingly important role in selecting new compounds for diverse screening libraries. New visualization techniques such as multi-fusion similarity maps, scaffold trees, and principal moments of inertia plots provide complementary information on compound libraries and enable identification of unexplored regions of chemical space with potential biological relevance. Quantitative metrics have been developed to analyze libraries for properties such as natural product-likeness and shape complexity. Analysis of high-throughput screening results and drug discovery programs identify compounds problematic for screening. Taken together these approaches allow us to increase the diversity of biological outcomes available in compound screening libraries and improve the success rates of high-throughput screening against new targets without making significant increases in the size of compound libraries. PMID:20457001

  14. Identification of Novel Hexapeptides Bioactive against Phytopathogenic Fungi through Screening of a Synthetic Peptide Combinatorial Library

    OpenAIRE

    López-García, Belén; Pérez-Payá, Enrique; Marcos, Jose F.

    2002-01-01

    The purpose of the present study was to improve the antifungal activity against selected phytopathogenic fungi of the previously identified hexapeptide PAF19. We describe some properties of a set of novel synthetic hexapeptides whose d-amino acid sequences were obtained through screening of a synthetic peptide combinatorial library in a positional scanning format. As a result of the screening, 12 putative bioactive peptides were identified, synthesized, and assayed. The peptides PAF26 (Ac-rkk...

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

    OpenAIRE

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

    2012-01-01

    This work evaluated the effect of carnauba and mineral oil coatings on the bioactive compounds and antioxidant capacity of tomato fruits (cv. “Grandela”). Carnauba and mineral oil coatings were applied on fresh tomatoes at two maturity stages (breaker and pink) over 28 day of storage at 10 °C was evaluated. Bioactive compound and antioxidant activity assays included total phenols, total flavonoids, ascorbic acid (ASA), lycopene, DPPH radical scavenging activity (%RSA), trolox equivalent antio...

  16. Silica-Gelatin Composite Materials for Prolonged Desorption of Bioactive Compounds

    OpenAIRE

    Oksana STAVINSKAYA; Iryna LAGUTA; Inna OREL

    2014-01-01

    The set of gelatin and silica-gelatin films with incorporated bioactive compounds of different chemical nature was prepared. The swelling behavior of the films and desorption of active ingredients into aqueous media were studied. For all the silica-gelatin films we observed considerable improvement of the materials water stability and retardation of the release of bioactive compounds as compared to gelatin samples. The results obtained make it possible to consider silica-gelatin composite mat...

  17. Minor bioactive compounds in milk and their determination

    OpenAIRE

    Kocmanová, Adéla

    2012-01-01

    Milk is an essential part of human nutrition at every stage of life, due to the balanced content of all necessary nutrients, valuable protein, lactose, fat and easily digestible bioactive minor components, especially vitamins and minerals. Milk is used as so - called ‘functional food’ due to its composition and positive effects on human health. Through the use of literature search it was possible to dispose compendium of minor bioactive substances found in milk and their effect on human he...

  18. Bioactive compounds of goat milk and their determination

    OpenAIRE

    Petránková, Barbora

    2013-01-01

    Summary Milk is for centuries the basic natural food of man. It is more than a source of nutrients. Due to its nutritional composition, specific effects on physiological and biochemical functions of the organism and the content of a wide range of bioactive substances, milk is ranked into the group of so-called functional foods. In this literature review was drawn sketch effect, particularly goat's milk, and it's bioactive substances on the human organism. At the end of this work are a...

  19. Design of a general-purpose European compound screening library for EU-OPENSCREEN.

    Science.gov (United States)

    Horvath, Dragos; Lisurek, Michael; Rupp, Bernd; Kühne, Ronald; Specker, Edgar; von Kries, Jens; Rognan, Didier; Andersson, C David; Almqvist, Fredrik; Elofsson, Mikael; Enqvist, Per-Anders; Gustavsson, Anna-Lena; Remez, Nikita; Mestres, Jordi; Marcou, Gilles; Varnek, Alexander; Hibert, Marcel; Quintana, Jordi; Frank, Ronald

    2014-10-01

    This work describes a collaborative effort to define and apply a protocol for the rational selection of a general-purpose screening library, to be used by the screening platforms affiliated with the EU-OPENSCREEN initiative. It is designed as a standard source of compounds for primary screening against novel biological targets, at the request of research partners. Given the general nature of the potential applications of this compound collection, the focus of the selection strategy lies on ensuring chemical stability, absence of reactive compounds, screening-compliant physicochemical properties, loose compliance to drug-likeness criteria (as drug design is a major, but not exclusive application), and maximal diversity/coverage of chemical space, aimed at providing hits for a wide spectrum of drugable targets. Finally, practical availability/cost issues cannot be avoided. The main goal of this publication is to inform potential future users of this library about its conception, sources, and characteristics. The outline of the selection procedure, notably of the filtering rules designed by a large committee of European medicinal chemists and chemoinformaticians, may be of general methodological interest for the screening/medicinal chemistry community. The selection task of 200K molecules out of a pre-filtered set of 1.4M candidates was shared by five independent European research groups, each picking a subset of 40K compounds according to their own in-house methodology and expertise. An in-depth analysis of chemical space coverage of the library serves not only to characterize the collection, but also to compare the various chemoinformatics-driven selection procedures of maximal diversity sets. Compound selections contributed by various participating groups were mapped onto general-purpose self-organizing maps (SOMs) built on the basis of marketed drugs and bioactive reference molecules. In this way, the occupancy of chemical space by the EU-OPENSCREEN library could

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

    Science.gov (United States)

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

    2016-01-01

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

  1. Bioactive Compounds Isolated from Lignin of Empty Bunch Palm Fiber and Their Effects on in Vitro Rumen Fermentation

    OpenAIRE

    M. Prayuwidayati; T. C. Sunarti; Sumardi; Subeki; K. G. Wiryawan

    2015-01-01

    The objective of this experiment was to study the effects of bioactive compounds isolated from purified lignin formacell (PLF) of empty bunch palm fiber as natural antimicrobes and their effects on in vitro rumen fermentation. The first experiment was inhibition test of 11 bioactive compounds isolated from PLF, using disc diffusion method against the growth of Escherichia coli, Salmonella typhimurium, and Staphylococcus aureus. Four of the most potential bioactive compounds were then used in ...

  2. Bioactive compounds of the main milk constituents and their determination

    OpenAIRE

    Malecký, Lukáš

    2012-01-01

    Diet is a blend of nutrients that the body needs to obtain energy and building materials needed for growth and repair of cells, tissues and organs. The nutrients or bioactive subtances are divided into two main groups: basic nutrients (macronutritients) and additional nutrients (micronutritients). Essential nutrients are divided into proteins, fats, carbohydrates and the body needs in large doses. The first part of this work with the available literature focuses on the milk, its general d...

  3. Public Domain HTS Fingerprints: Design and Evaluation of Compound Bioactivity Profiles from PubChem's Bioassay Repository.

    Science.gov (United States)

    Helal, Kazi Yasin; Maciejewski, Mateusz; Gregori-Puigjané, Elisabet; Glick, Meir; Wassermann, Anne Mai

    2016-02-22

    Molecular profiling efforts aim at characterizing the biological actions of small molecules by screening them in hundreds of different biochemical and/or cell-based assays. Together, these assays yield a rich data landscape of target-based and phenotypic effects of the tested compounds. However, submitting an entire compound library to a molecular profiling panel can easily become cost-prohibitive. Here, we make use of historical screening assays to create comprehensive bioactivity profiles for more than 300 000 small molecules. These bioactivity profiles, termed PubChem high-throughput screening fingerprints (PubChem HTSFPs), report small molecule activities in 243 different PubChem bioassays. Although the assays originate from originally independently pursued drug or probe discovery projects, we demonstrate their value as molecular signatures when used in combination. We use these PubChem HTSFPs as molecular descriptors in hit expansion experiments for 33 different targets and phenotypes, showing that, on average, they lead to 27 times as many hits in a set of 1000 chosen molecules as a random screening subset of the same size (average ROC score: 0.82). Moreover, we demonstrate that PubChem HTSFPs retrieve hits that are structurally diverse and distinct from active compounds retrieved by chemical similarity-based hit expansion methods. PubChem HTSFPs are made freely available for the chemical biology research community. PMID:26898267

  4. Phytochemical analysis and estimation of major bioactive compounds from Triticum aestivum L. grass with antimicrobial potential.

    Science.gov (United States)

    Rajoria, Anand; Mehta, Archana; Mehta, Pradeep; Ahirwal, Laxmi; Shukla, Shruti

    2015-11-01

    The aim of the present study was to investigate phytochemical analysis, and qualitative and quantitative determination of major bioactive compound present in various organic extracts of T. aestivum L. grass. Soxhlet apparatus was used for the extraction purpose using hexane, chloroform, methanol and distilled water as a solvent system. All the extracts derived from T. aestivum showed qualitative presence of major phytochemicals including alkaloids, steroids and cardiac glycosides tannins, flavonoids carbohydrates. Further, HPLC analysis revealed the presence of major bioactive compounds such as rutin, chlorogenic acid, tocopherol, chlorogenic acid, and gallic acid in various organic extracts responsible for the reported maximum antimicrobial activity of T. aestivum grass against pathogenic bacteria including Salmonella typhi, Staphylococcus aureus and Vibrio cholerae. These findings confirm that T. aestivum grass containing medicinally important bioactive compounds may have significant potential to be used in traditional medicine system for the treatment of various diseases caused by pathogenic microorganisms. PMID:26687741

  5. Seasonal Effects on Bioactive Compounds and Antioxidant Capacity of Six Economically Important Brassica Vegetables

    Directory of Open Access Journals (Sweden)

    Eduardo A.S. Rosa

    2011-08-01

    Full Text Available Research on natural and bioactive compounds is increasingly focused on their effects on human health, but there are unexpectedly few studies evaluating the relationship between climate and natural antioxidants. The aim of this study was analyze the biological role of six different Brassica vegetables (Brassica oleracea L. and Brassica rapa L. as a natural source of antioxidant compounds. The antioxidant activity may be assigned to high levels of L-ascorbic acid, total phenolics and total flavonoids of each sample. The climate seasons affected directly the concentration of bioactive components and the antioxidant activity. Broccoli inflorescences and Portuguese kale showed high antioxidant activity in Spring-Summer whilst turnip leaves did so in Summer-Winter. The Brassica vegetables can provide considerable amounts of bioactive compounds and thus may constitute an important natural source of dietary antioxidants.

  6. Phenolic compounds and bioactive properties of wild German and Roman chamomiles

    OpenAIRE

    Guimarães, Rafaela; Barros, Lillian; Dueñas, Montserrat; Ricardo C. Calhelha; Carvalho, Ana Maria; Santos-Buelga, Celestino; Queiroz, Maria João R. P.; Ferreira, Isabel C. F. R.

    2012-01-01

    Natural products represent a rich source of biologically active compounds and are an example of molecular diversity, with recognized potential in drug discovery. In the present work, methanolic extracts of Matricaria recutita L. (German chamomile) and Chamaemelum nobile L. (Roman chamomile) and their decoction and infusion (the most consumed preparations of these herbs) were submitted to an analysis of phenolic compounds and bioactivity evaluation. Phenolic compounds were characterized by HPL...

  7. Bioactive phenolic compounds : production and extraction by solid-state fermentation. A review

    OpenAIRE

    Martins, Silvia; Solange I. Mussatto; Martínez-Avila, G.; Montañez-Saenz, J.; Aguilar Gonzalez, Cristobal Noé; Teixeira, J.A.

    2011-01-01

    Interest in the development of bioprocesses for the production or extraction of bioactive compounds from natural sources has increased in recent years due to the potential applications of these compounds in food, chemical, and pharmaceutical industries. In this context, solid-state fermentation (SSF) has received great attention because this bioprocess has potential to successfully convert inexpensive agro-industrial residues, as well as plants, in a great variety of valuable compounds, inclu...

  8. Isolation, partial purification and evaluation of bioactive compounds from leaves of Ageratum houstonianum

    OpenAIRE

    M. S. Khan; Kumar, A; Rizvi, S.M.D.; M. Zeeshan

    2012-01-01

    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 ...

  9. Structure-Based Virtual Screening of Commercially Available Compound Libraries.

    Science.gov (United States)

    Kireev, Dmitri

    2016-01-01

    Virtual screening (VS) is an efficient hit-finding tool. Its distinctive strength is that it allows one to screen compound libraries that are not available in the lab. Moreover, structure-based (SB) VS also enables an understanding of how the hit compounds bind the protein target, thus laying ground work for the rational hit-to-lead progression. SBVS requires a very limited experimental effort and is particularly well suited for academic labs and small biotech companies that, unlike pharmaceutical companies, do not have physical access to quality small-molecule libraries. Here, we describe SBVS of commercial compound libraries for Mer kinase inhibitors. The screening protocol relies on the docking algorithm Glide complemented by a post-docking filter based on structural protein-ligand interaction fingerprints (SPLIF). PMID:27316988

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

    Institute of Scientific and Technical Information of China (English)

    Maghdu Nainamohamed Abubacker; Palaniyappan Kamala Devi

    2014-01-01

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

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

    Science.gov (United States)

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

    2012-09-01

    In recent years, ionic liquids (ILs), as green and designer solvents, have accelerated research in analytical chemistry. This review highlights some of the unique properties of ILs and provides an overview of the preparation and application of IL or IL-based materials to extract bioactive compounds in plants. IL or IL-based materials in conjunction with liquid-liquid extraction (LLE), ultrasonic-assisted extraction (UAE), microwave-assisted extraction (MAE), high performance liquid chromatography (HPLC) and solid-phase extraction (SPE) analytical technologies etc., have been applied successfully to the extraction or separation of bioactive compounds from plants. This paper reviews the available data and references to examine the advantages of IL and IL-based materials in these applications. In addition, the main target compounds reviewed in this paper are bioactive compounds with multiple therapeutic effects and pharmacological activities. Based on the importance of the targets, this paper reviews the applications of ILs, IL-based materials or co-working with analytical technologies. The exploitation of new applications of ILs on the extraction of bioactive compounds from plant samples is expected to increase. PMID:22877739

  12. In Vitro Wound Healing Potential and Identification of Bioactive Compounds from Moringa oleifera Lam

    Directory of Open Access Journals (Sweden)

    Abubakar Amali Muhammad

    2013-01-01

    Full Text Available 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.

  13. Phenolic compounds among the bioactive molecules in Ginkgo biloba L.

    OpenAIRE

    Pereira, Eliana; Barros, Lillian; Santos-Buelga, Celestino; Ferreira, Isabel C.F.R.

    2015-01-01

    The interest for natural antioxidants has been increasing over the years. Phenolic compounds comprise a very large group of biologically active molecules, being appreciated for their beneficial effects on health (physiologically active compounds with anti-allergic, antiatherogenic, antimicrobial, antithrombotic, anti-inflammatory, antioxidant, cardioprotective and vasodilatory effects) [1-3]. The aim of the present study was to evaluate the phenolic compounds of Ginkgo biloba L...

  14. Characterization of phenolic compounds using separation techniques coupled to mass spectrometry of plant extracts with demonstrated bioactivity

    OpenAIRE

    Iswaldi, Ihsan

    2012-01-01

    This doctoral thesis, entitled "Characterization of phenolic compounds using separation techniques coupled to mass spectrometry of plant extracts with demonstrated bioactivity", consists of two main sections: the Introduction and the Experimental Section. The first section describes an overview of traditional medicine and functional food, plant foods as natural source of bioactive compounds, polyphenols and bioactivity and the analytical tools used to identify polyphenols such as high-pe...

  15. OrgTrace – No difference found in bioactive compounds of organic and conventional crops

    DEFF Research Database (Denmark)

    Knuthsen, Pia; Søltoft, Malene; Laursen, Kristian Holst;

    years as well as soil types. The results showed that contents of neither polyacetylenes and carotenoids in carrots, flavonoids in onions, nor phenolic acids in carrots and potatoes were significantly influenced by growth system. Thus it could not be concluded that the organically grown crops had higher......The objective of the present study was to compare the content of selected bioactive compounds in organically and conventionally grown crops, and to evaluate if the ability of the crops to synthesize selected secondary metabolites was systematically affected by growth systems across different growth...... contents of bioactive compounds than the conventionally grown. This indicates that giving preference to organic products because they contain more bioactive components is doubtfull. However, there are many other reasons for the consumer to choose organic food products, including: no pesticide residues in...

  16. A Systematic Review of the Efficacy of Bioactive Compounds in Cardiovascular Disease: Phenolic Compounds

    Science.gov (United States)

    Rangel-Huerta, Oscar D.; Pastor-Villaescusa, Belen; Aguilera, Concepcion M.; Gil, Angel

    2015-01-01

    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

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

    Science.gov (United States)

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

    2016-06-01

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

  18. Bioactive compounds in dairy products and their relation to neurodegenerative disease

    Science.gov (United States)

    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...

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

    Science.gov (United States)

    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...

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

    Directory of Open Access Journals (Sweden)

    Ana Teixeira

    2014-09-01

    Full Text Available 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.

  1. Solvent-free microwave extraction of bioactive compounds provides a tool for green analytical chemistry

    OpenAIRE

    Ying LI; Fabiano-Tixier, Anne-Sylvie; Vian, Maryline; Chemat, Farid

    2013-01-01

    We present an overview on solvent-free microwave-extraction techniques of bioactive compounds from natural products. This new technique is based on the concept of green analytical chemistry. It has proved to be an alternative to other techniques with the advantages of reducing extraction times, energy consumption, solvent use and CO2 emissions.

  2. Quantification of six bioactive compounds in Zhenqi Fuzheng preparation by high-performance liquid chromatography couple

    Institute of Scientific and Technical Information of China (English)

    Yi-Kai Shi; Fang Cui; Fang-Di Hu; Ying-Yan Bi; Yu-Feng Ma; Shi-Lan Feng

    2011-01-01

    A simple and accurate high-performance liquid chromatography(HPLC)coupled with diode array detector(DAD)and evaporative light scattering detector(ELSD)was established for the determination of six bioactive compounds in Zhenqi Fuzheng preparation(ZFP).The

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

    Science.gov (United States)

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

  4. Natural bioactive compounds from winery by-products as health promoters: a review.

    Science.gov (United States)

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

    2014-01-01

    The relevance of food composition for human health has increased consumers' interest in the consumption of fruits and vegetables, as well as foods enriched in bioactive compounds and nutraceuticals. This fact has led to a growing attention of suppliers on reuse of agro-industrial wastes rich in healthy plant ingredients. On this matter, grape has been pointed out as a rich source of bioactive compounds. Currently, up to 210 million tons of grapes (Vitis vinifera L.) are produced annually, being the 15% of the produced grapes addressed to the wine-making industry. This socio-economic activity generates a large amount of solid waste (up to 30%, w/w of the material used). Winery wastes include biodegradable solids namely stems, skins, and seeds. Bioactive compounds from winery by-products have disclosed interesting health promoting activities both in vitro and in vivo. This is a comprehensive review on the phytochemicals present in winery by-products, extraction techniques, industrial uses, and biological activities demonstrated by their bioactive compounds concerning potential for human health. PMID:25192288

  5. Health promoting effects of bioactive compounds in plants: Targeting Type 2 diabetes

    DEFF Research Database (Denmark)

    Bhattacharya, Sumangala

    While type 2 diabetes is an increasing problem worldwide, there is still no cure and therefore search for the new insulin sensitizer continues. Plants are a natural source of bioactive compounds and have been used to improve human health and wellbeing for centuries. Today, several studies...

  6. Draft Genome Sequence of Hoeflea sp. Strain BAL378, a Potential Producer of Bioactive Compounds

    DEFF Research Database (Denmark)

    Bentzon-Tilia, Mikkel; Riemann, Lasse; Gram, Lone

    2014-01-01

    Some phytoplankton-associated marine bacteria produce bioactive compounds. Members of the genus Hoeflea may be examples of such bacteria; however, data describing their metabolisms are scarce. Here, we report the draft genome sequence of Hoeflea sp. strain BAL378, a putative producer of bacterioc...... of bacteriocins, polyketides, and auxins, as demonstrated by genome mining....

  7. EPlantLIBRA: A composition and biological activity database for bioactive compounds in plant food supplements

    DEFF Research Database (Denmark)

    Plumb, J.; Lyons, J.; Nørby, Karin Kristiane;

    2015-01-01

    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...

  8. Seasonal effects on bioactive compounds and antioxidant capacity of six economically important brassica vegetables

    OpenAIRE

    Rosa, Eduardo A.S.; Saavedra, Maria J; Alfredo Aires; Rosa Carvalho; Conceição Fernandes; Bennett, Richard N

    2011-01-01

    Research on natural and bioactive compounds is increasingly focused on their effects on human health, but there are unexpectedly few studies evaluating the relationship between climate and natural antioxidants. The aim of this study was analyze the biological role of six different Brassica vegetables (Brassica oleracea L. and Brassica rapa L.) as a natural source of antioxidant compounds. The antioxidant activity may be assigned to high levels of L-ascorbic acid, total phenolics and total fla...

  9. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata

    OpenAIRE

    Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Edmar CLEMENTE

    2012-01-01

    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 anamorph...

  10. Chemically engineered extracts as an alternative source of bioactive natural product-like compounds

    OpenAIRE

    Silvia N. López; Ramallo, I. Ayelen; Sierra, Manuel Gonzalez; SUSANA A ZACCHINO; Furlan, Ricardo L. E.

    2006-01-01

    The access to libraries of molecules with interesting biomolecular properties is a limiting step in the drug discovery process. By virtue of a long molecular evolution process, natural products are recognized as biologically validated starting points in structural space for library development. We introduce here a strategy to generate natural product-like libraries. A semisynthetic mixture of compounds was produced by diversification of a natural product extract through the chemical transform...

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

    Directory of Open Access Journals (Sweden)

    Franco Van De Velde

    2013-03-01

    Full Text Available 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.

  12. Bioactive compounds, antioxidant and binding activities and spear yield of Asparagus officinalis L.

    Science.gov (United States)

    Lee, Jong Won; Lee, Jeong Hyun; Yu, In Ho; Gorinstein, Shela; Bae, Jong Hyang; Ku, Yang Gyu

    2014-06-01

    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 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. PMID:24793354

  13. Bioactive compounds in edible flowers processed by radiation

    International Nuclear Information System (INIS)

    Edible flowers are increasingly being used in culinary preparations, being also recognized for their potential valuable effects in human health, which require new approaches to improve their conservation and safety. These highly perishable products should be grown without using any pesticide. Irradiation treatment might be the answer to these problems, ensuring food quality, increasing shelf-life and disinfestation of foods. Irradiation treatment might be the answer to these problems, to ensure food quality, to increase shelf-life and disinfestation of foods. Tropaeolum majus L. (nasturtium) and Viola tricolor L. (johnny-jump-up) flowers are widely used in culinary preparations, being also acknowledged for their antioxidant properties and high content of phenolics. The purpose of this study was to evaluate the dose-dependent effects of gamma and electron beam irradiation (doses of 0, 0.5, 0.8 and 1 kGy) on the antioxidant activity, phenolic compounds, physical aspects and antiproliferative potential of edible flowers. Kaempferol-O-hexoside-O-hexoside was the most abundant compound in all samples of Tropaeolum majus flower while pelargonidin-3-O-sophoroside was the major anthocyanin. In general, irradiated samples gave higher antioxidant activity, probably due to their higher amounts of phenolic compounds, which were also favored by the 1.0 kGy dose, regardless of the source . The Viola tricolor samples displayed flavonols as the most abundant phenolic compounds, particularly those derived from quercetin. In general, gamma-irradiated samples, independently of the applied dose, showed higher amounts in phenolic compounds, which were also favored by the 1.0 kGy dose, regardless of the source. The antioxidant activity was also higher among irradiated samples. The two species of edible flowers have not provided the samples did not show potential antiproliferative and cytotoxicity. Accordingly, the applied irradiation treatments seemed to represent a feasible technology

  14. Accurate Dereplication of Bioactive Secondary Metabolites from Marine-Derived Fungi by UHPLC-DAD-QTOFMS and a MS/HRMS Library

    Directory of Open Access Journals (Sweden)

    Sara Kildgaard

    2014-06-01

    Full Text Available In drug discovery, reliable and fast dereplication of known compounds is essential for identification of novel bioactive compounds. Here, we show an integrated approach using ultra-high performance liquid chromatography-diode array detection-quadrupole time of flight mass spectrometry (UHPLC-DAD-QTOFMS providing both accurate mass full-scan mass spectrometry (MS and tandem high resolution MS (MS/HRMS data. The methodology was demonstrated on compounds from bioactive marine-derived strains of Aspergillus, Penicillium, and Emericellopsis, including small polyketides, non-ribosomal peptides, terpenes, and meroterpenoids. The MS/HRMS data were then searched against an in-house MS/HRMS library of ~1300 compounds for unambiguous identification. The full scan MS data was used for dereplication of compounds not in the MS/HRMS library, combined with ultraviolet/visual (UV/Vis and MS/HRMS data for faster exclusion of database search results. This led to the identification of four novel isomers of the known anticancer compound, asperphenamate. Except for very low intensity peaks, no false negatives were found using the MS/HRMS approach, which proved to be robust against poor data quality caused by system overload or loss of lock-mass. Only for small polyketides, like patulin, were both retention time and UV/Vis spectra necessary for unambiguous identification. For the ophiobolin family with many structurally similar analogues partly co-eluting, the peaks could be assigned correctly by combining MS/HRMS data and m/z of the [M + Na]+ ions.

  15. HPLC ANALYSIS OF BIOACTIVE COMPOUNDS IN TEN DIFFERENT WILD TYPE UNDER-UTILIZED LEGUME GRAINS

    Directory of Open Access Journals (Sweden)

    Vellingiri Vadivel and Hans Konrad Biesalski

    2010-05-01

    Full Text Available In recent years, many food industries have been initiated the formulation of nutraceutical/functional foods by incorporating the bioactive ingredients for the prevention/treatment of certain chronic diseases. In this connection, certain promising wild type under-utilized legume grains received more attention, since they are naturally a rich source of L-Dopa (precursor of dopamine and certain bioactive compounds including phenolics, tannins and phytic acid. In the present study, seed materials of certain promising wild type under-utilized food legume grains such as Abrus precatorius L., Acacia leucopholea Willd, Bauhinia varigata L., Canavalia gladiata (Jacq. DC., Cassia floribunda Cav., Entada scandens Benth., Indigofera linifolia (L.f. Retz., Mucuna monosperma DC. Ex Wight., Sesbania bispinosa (Jacq. Wight. and Tamarindus indica L., collected from Eastern and Western Ghats of South India, were investigated for certain bioactive compounds through HPLC technique. All the analysed samples were found to constitute a viable source of total free phenolics (4.23 – 8.75 g/100 g DM, tannins (1.04 – 5.41 g /100 g DM, L-Dopa (1.17 – 5.34 g/100 g DM and phytic acid (0.96 – 2.74 g/100 g DM and also the newly developed HPLC procedures were proven to be sensitive enough to detect these bioactive compounds even at tracer level. Further, such wild type legume grains could be recommended as a natural source of bioactive compounds in the dietary management of certain chronic diseases such as Parkinsonism, diabetes, obesity, cardiovascular diseases, cancer etc.

  16. Evaluation of Mycelial Nutrients, Bioactive Compounds, and Antioxidants of Five Himalayan Entomopathogenic Ascomyceteous Fungi from India.

    Science.gov (United States)

    Sharma, Sapan Kumar; Gautam, Nandini; Atri, Narender Singh

    2015-01-01

    In this study, using standard methods, mycelial nutrients, bioactive compounds, and antioxidants were analyzed for the first time for five fungal species: Isaria sinclairii (Berk.) Lloyd, I. tenuipes Peck, I. japonica Yasuda, I. farinosa (Holmsk) Fr. and Cordyceps tuberculata (Lebert) Maire. All of these species were low in fat content and rich in protein, fiber, ash, and carbohydrates. Mineral elements (Fe, Mg, Cu, Mn, and Ca) were detected in appreciable amounts. All three types of fatty acids (saturated, monounsaturated, and polyunsaturated) as well as bioactive compounds (ascorbic acid, β-carotene, lycopene, phenolic compounds, and polysaccharides) were detected for each species. The investigated species showed high ferric-reducing antioxidant power as well as 2,2-diphenyl-1-picryl-hydrazyl radical scavenging activity. Although differences were observed in the values of each species, each species showed richness in one or more components. PMID:26559700

  17. Aromatic Plants as a Source of Bioactive Compounds

    OpenAIRE

    Panagiota Florou-Paneri; Ilias Giannenas; Eleftherios Bonos; Efterpi Christaki

    2012-01-01

    Aromatic plants, also known as herbs and spices, have been used since antiquity as folk medicine and as preservatives in foods. The best known aromatic plants, such as oregano, rosemary, sage, anise, basil, etc., originate from the Mediterranean area. They contain many biologically active compounds, mainly polyphenolics, which have been found to possess antimicrobial, antioxidant, antiparasitic, antiprotozoal, antifungal, and anti-inflammatory properties. Currently, the demand for these plant...

  18. Separation and determination of bioactive compounds in food

    OpenAIRE

    Dvořáčková, Eva

    2014-01-01

    Herbs are widely known for their numerous applications in the food industry; however, there is increasing interest in their pharmaceutical properties. In recent years, major research has been focused on the biologically active derivatives of medicinal plants, mainly because of their potential anti-tumor activity and protective effects with respect to the cardiovascular system. This thesis summarizes the biosynthesis of phenolic compounds mainly responsible for such positive health impacts, th...

  19. Nanoencapsulation of pomegranate bioactive compounds for breast cancer chemoprevention

    Directory of Open Access Journals (Sweden)

    Shirode AB

    2015-01-01

    Full Text Available Amit B Shirode,1,2,* Dhruba J Bharali,3,* Sameera Nallanthighal,1,2 Justin K Coon,1,2 Shaker A Mousa,3 Ramune Reliene1,2 1Department of Environmental Health Sciences, University at Albany, State University of New York, Albany, NY, USA; 2Cancer Research Center, University at Albany, Rensselaer, NY, USA; 3Pharmaceutical Research Institute, Albany College of Pharmacy and Health Sciences, Albany, NY, USA *These authors contributed equally to this work Abstract: Pomegranate polyphenols are potent antioxidants and chemopreventive agents but have low bioavailability and a short half-life. For example, punicalagin (PU, the major polyphenol in pomegranates, is not absorbed in its intact form but is hydrolyzed to ellagic acid (EA moieties and rapidly metabolized into short-lived metabolites of EA. We hypothesized that encapsulation of pomegranate polyphenols into biodegradable sustained release nanoparticles (NPs may circumvent these limitations. We describe here the development, characterization, and bioactivity assessment of novel formulations of poly(D,L-lactic-co-glycolic acid–poly(ethylene glycol (PLGA–PEG NPs loaded with pomegranate extract (PE or individual polyphenols such as PU or EA. Monodispersed, spherical 150–200 nm average diameter NPs were prepared by the double emulsion–solvent evaporation method. Uptake of Alexa Fluor-488-labeled NPs was evaluated in MCF-7 breast cancer cells over a 24-hour time course. Confocal fluorescent microscopy revealed that PLGA–PEG NPs were efficiently taken up, and the uptake reached the maximum at 24 hours. In addition, we examined the antiproliferative effects of PE-, PU-, and/or EA-loaded NPs in MCF-7 and Hs578T breast cancer cells. We found that PE, PU, and EA nanoprototypes had a 2- to 12-fold enhanced effect on cell growth inhibition compared to their free counterparts, while void NPs did not affect cell growth. PU-NPs were the most potent nanoprototype of pomegranates. Thus, PU may be the

  20. Effect of Mobile Phase Additives on the Resolution of Four Bioactive Compounds by RP-HPLC

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    Shengnan Li

    2010-05-01

    Full Text Available The use of mobile phase additives enhances the separation and resolution of the bioactive compounds on the C18 column. Chlorogenic acid, caffeic acid, rutin, and scoparone from Herba Artemisiae Scopariae were investigated as the target compounds. Acetic acid, triethylamine, inorganic salts, and several ionic liquids were added as mobile phase additives into methanol/water (40:60, v/v. The result revealed that a mobile phase with 0.01 mol/L of ionic liquid [BMIM][BF4] enabled the optimum separation of the four target compounds.

  1. Antioxidant-Prooxidant Properties of a New Organoselenium Compound Library

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    Carmen Sanmartín

    2010-10-01

    Full Text Available The present study describes the biological evaluation of a library of 59 organo-selenium compounds as superoxide (O2─ generators and cytotoxic agents in human prostate cancer cells (PC-3 and in breast adenocarcinoma (MCF-7. In order to corroborate that the biological activity for selenium compounds depends on the chemical form, a broad structural variety is presented. These structures include selenocyanates, diselenides, selenoalkyl functional moieties and eight newly synthesized symmetrically substituted dithioselenites and selenylureas. Eleven of the derivatives tested showed high levels of superoxide generation in vitro via oxidation of reduced glutathione (GSH and nine of them were more catalytic than the reference compound, diselenodipropionic acid. Eighteen of the library compounds inhibited cell growth more than or similar to reference chemotherapeutic drugs in PC-3 and eleven were more potent cytotoxic agents than etoposide in the MCF-7 cell line. Considering both parameters (superoxide generation and cell cytotoxicity compounds B1, C6 and C9 displayed the best therapeutic profiles. Considering that many diselenide compounds can generate superoxide (O2─ in vitro via oxidation of GSH and other thiols, the analogue B1, that contains a diselenide moiety, was selected for a preliminary mechanistic investigation, which . revealed that B1 has apoptogenic effects similar to camptothecin mediated by reactive oxygen species (ROS in lymphocytic leukemia cells (CCRF-CEM and affected the MCF-7 cell-cycle in G2/M and S-phases.

  2. Bovine and soybean milk bioactive compounds: Effects on inflammatory response of human intestinal Caco-2 cells.

    Science.gov (United States)

    Calvello, Rosa; Aresta, Antonella; Trapani, Adriana; Zambonin, Carlo; Cianciulli, Antonia; Salvatore, Rosaria; Clodoveo, Maria Lisa; Corbo, Filomena; Franchini, Carlo; Panaro, Maria Antonietta

    2016-11-01

    In this study the effects of commercial bovine and soybean milks and their bioactive compounds, namely genistein, daidzein and equol, on the inflammatory responses induced by lipopolysaccharide (LPS) treatment of human intestinal Caco-2 cells were examined, in terms of nitric oxide (NO) release and inducible nitric oxide synthetase (iNOS) expression. Both milks and their bioactive compounds significantly inhibited, dose-dependently, the expression of iNOS mRNA and protein, resulting in a decreased NO production. The NF-κB activation in LPS-stimulated intestinal cells was also examined. In all cases we observed that cell pre-treatment before LPS activation inhibited the IkB phosphorylation. Accordingly, quantification of bioactive compounds by solid phase microextraction coupled with liquid chromatography has shown that they were absorbed, metabolized and released by Caco-2 cells in culture media. In conclusion, we demonstrated that milks and compounds tested are able to reduce LPS-induced inflammatory responses from intestinal cells, interfering with NF-kB dependent molecular mechanisms. PMID:27211648

  3. Germination Time Dependence of Bioactive Compounds and Antioxidant Activity in Germinated Rough Rice (Oryza sativa L.

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    Anuchita Moongngarm

    2011-01-01

    Full Text Available Problem statement: Germinated rice has been recognized as a functional food and its health benefits. However, most related studies were on germinated brown rice but our previous study indicated that germination of rough rice was an effective method to obtain high concentrations of bioactive compounds. Germination time is one of the most important factors affecting the level of biochemical compositions and antioxidant activity. Approach: Rough rice seeds were soaked in water for 2 days and germinated for four different days (1- 4 days. Total phenolic compounds, phytic acid, á-tocopherol, á- tocopherol, á-tocotrienol and á-oryzanol were investigated compared with those of ungerminated brown rice. The antioxidant activity of germinated rice was evaluated through four different methods, the 1, 1- Diphenyl-2-Picrylhydrazyl (DPPH free radical scavenging assay, hydroxyl radical scavenging activity, lipid peroxidation assay and linoleic acid emulsion system-thiocyanate method. Results: The results showed that the germination for 2 days or longer, after soaking, yielded significantly higher level of total phenolic, á-tocopherol, á-tocopherol, á-tocotrienol and á-oryzanol than those of ungerminated brown rice and soaked rice, whilst the concentration of phytic acid was reduced significantly when germination time was increased. The samples germinated for one day or longer also revealed greater antioxidant activity than those of ungerminated rice. Conclusion: The level of bioactive compounds and antioxidant activity of germinated rough rice were affected by germination time. Germination for 2 and 3 days was the optimum time for germination rough rice to obtain high concentration of bioactive compounds and high antioxidant activity. The germination process of rough rice could be a potential method to obtain functional germinated rice flour with high bioactive compounds and health beneficial properties and could be applied to produce

  4. Zebrafish dives into food research: effectiveness assessment of bioactive compounds.

    Science.gov (United States)

    Caro, M; Iturria, I; Martinez-Santos, M; Pardo, M A; Rainieri, S; Tueros, I; Navarro, V

    2016-06-15

    Zebrafish have been traditionally used in ecotoxicology and developmental biology. However, due to the advances in available methodologies and the similitude with mammals, it has been increasingly used in other fields. One of the most recent fields using zebrafish is food research, being the focus of this review. Most relevant and recent publications including food component toxicity and key metabolic effects together with effectiveness on some zebrafish disease models have been reviewed. This model is a good intermediate tool between in vitro and rodent models, because it provides information from a complete organism in a fast and cost-effective manner. Definitely, in the near future, we will see this model being used by the ingredient suppliers and scientists in order to show the potential impact on health of several compounds. PMID:27109696

  5. Aromatic Plants as a Source of Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Panagiota Florou-Paneri

    2012-09-01

    Full Text Available Aromatic plants, also known as herbs and spices, have been used since antiquity as folk medicine and as preservatives in foods. The best known aromatic plants, such as oregano, rosemary, sage, anise, basil, etc., originate from the Mediterranean area. They contain many biologically active compounds, mainly polyphenolics, which have been found to possess antimicrobial, antioxidant, antiparasitic, antiprotozoal, antifungal, and anti-inflammatory properties. Currently, the demand for these plants and their derivatives has increased because they are natural, eco-friendly and generally recognized as safe products. Therefore, aromatic plants and their extracts have the potential to become new generation substances for human and animal nutrition and health. The purpose of this review is to provide an overview of the literature surrounding the in vivo and in vitro use of aromatic plants.

  6. Bioactive compounds and the antioxidant capacity in new kiwi fruit cultivars.

    Science.gov (United States)

    Park, Yong-Seo; Namiesnik, Jacek; Vearasilp, Kann; Leontowicz, Hanna; Leontowicz, Maria; Barasch, Dinorah; Nemirovski, Alina; Trakhtenberg, Simon; Gorinstein, Shela

    2014-12-15

    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 (Pkiwi 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. PMID:25038687

  7. Enzymatic synthesis of bioactive compounds with high potential for cosmeceutical application.

    Science.gov (United States)

    Antonopoulou, Io; Varriale, Simona; Topakas, Evangelos; Rova, Ulrika; Christakopoulos, Paul; Faraco, Vincenza

    2016-08-01

    Cosmeceuticals are cosmetic products containing biologically active ingredients purporting to offer a pharmaceutical therapeutic benefit. The active ingredients can be extracted and purified from natural sources (botanicals, herbal extracts, or animals) but can also be obtained biotechnologically by fermentation and cell cultures or by enzymatic synthesis and modification of natural compounds. A cosmeceutical ingredient should possess an attractive property such as anti-oxidant, anti-inflammatory, skin whitening, anti-aging, anti-wrinkling, or photoprotective activity, among others. During the past years, there has been an increased interest on the enzymatic synthesis of bioactive esters and glycosides based on (trans)esterification, (trans)glycosylation, or oxidation reactions. Natural bioactive compounds with exceptional theurapeutic properties and low toxicity may offer a new insight into the design and development of potent and beneficial cosmetics. This review gives an overview of the enzymatic modifications which are performed currently for the synthesis of products with attractive properties for the cosmeceutical industry. PMID:27276911

  8. Chemical quality parameters and bioactive compound content of brazilian berries

    Directory of Open Access Journals (Sweden)

    Daniela Mota Segantini

    2015-09-01

    Full Text Available There is a growing consumer demand for higher healthy foods such as berries which are a rich source of phenolic compounds. The current work evaluated blackberry cultivars: Cherokee, Tupy and Xavante; raspberry cultivars: Heritage, Fallgold and Black; and the hybrid Boysenberry. All berries were grown under homogenous subtropical conditions in Brazil. Black raspberry, Cherokee and Tupy blackberry cultivars showed the highest ratio between soluble solid contents and titratable acidity, and Fallgold and Heritage raspberry showed the highest titratable acidity. Total phenolic content ranged from 2.03 to 5.33 g kg–1 fresh weight and total anthocyanin content registered values from 0.41 to 1.81 g kg–1 fresh weight. The most common phenolic acids were gallic, p-coumaric and ellagic, and for anthocyanins: cyanidin-3-glucoside and malvinidin-3-glucoside. Antioxidant capacity ranged from 14.13 to 21.51 mol equivalent trolox kg–1 fresh weight. Black raspberry, all blackberry cultivars and the Boysenberry hybrid are appropriate to be consumed fresh, while Fallgold and Heritage raspberries are recommended to the food industry. Due to their phenolic richness and antioxidant properties, these fruits are of great interest to the fresh fruit market and to pharmaceutical industries. These results could help breeders and growers when planning the cultivar selection according to their foreseeable destination.

  9. Bioactivity of volatile organic compounds produced by Pseudomonas tolaasii

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    Pietro eLo Cantore

    2015-10-01

    Full Text Available 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, 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 dimethyl disulfide toxicity was assessed till a quantity of 1.25 µg, below which it caused, together with 1-undecene ( 10 µg, broccoli growth increase.

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

    OpenAIRE

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

    2014-01-01

    Metabolites resulting from nitrogen metabolism in yeast are currently found in some fermented beverages such as wine and beer. Their study has recently attracted the attention of researchers. Some metabolites derived from aromatic amino acids are bioactive compounds that can behave as hormones or even mimic their role in humans and may also act as regulators in yeast. Although the metabolic pathways for their formation are well known, the physiological significance is still far from being und...

  11. Fermentation of Plant Material - Effect on Sugar Content and Stability of Bioactive Compounds

    OpenAIRE

    Reis Bruno A. dos; Kosińska-Cagnazzo Agnieszka; Schmitt Rudolf; Andlauer Wilfried

    2014-01-01

    Extraction is a method often used to obtain products rich in bioactive compounds from plant material. Most of the solvents used for the poly-phenols extraction simultaneously extract also sugars, undesirable as a component of health-promoting food. Fermentation might be a simple, cheap and efficient way of sugar elimination. In our study, black tea and goji berries, both known for their health benefits, were used and alcoholic fermentation by Saccharomyces cerevisiae was carried out to elimin...

  12. Ultraviolet Irradiation Effect on Apple Juice Bioactive Compounds during Shelf Storage

    OpenAIRE

    Edmundo Juarez-Enriquez; Ivan Salmerón; Nestor Gutierrez-Mendez; Enrique Ortega-Rivas

    2016-01-01

    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 descri...

  13. The investigation of some bioactive compounds and antioxidant properties of hawthorn (Crataegus monogyna subsp. monogyna Jacq)

    OpenAIRE

    Serhat KESER; Celik, Sait; Turkoglu, Semra; Yilmaz, Okkes; Turkoglu, Ismail

    2014-01-01

    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 c...

  14. Isolation and Characterization of Potential Bioactive Compounds from Landolphia owariensis P. Beauv Stringy Seed Pulp

    OpenAIRE

    T JN Okonkwo; P O Osadebe

    2013-01-01

    Summary. Landolphia owariensis P. Beauv, a tropical climber, is economically important for latex/rubber and folklore medicine. Among other uses, it is utilized in the management of malaria and inflammatory related diseases in ethno medicine. Thus its stringy seed pulp (LOSSP) was subjected to isolation and characterization of bioactive compounds. A fresh portion of LOSSP was air-dried, pulverized, defatted with petroleum ether and subsequently extracted with acetone and distilled water succes...

  15. GOAT SPERM SURFACE ALTERATION DURING EPIDIDYMAL MATURATION: AN EVALUATION BY MARINE BIOACTIVE COMPOUND FROM TELESCOPIUM TELESCOPIUM

    OpenAIRE

    HEMBRAM, Manik Lai; Datta, Uttam; Dasgupta, Raju

    2012-01-01

    ABSTRACT Bio-active compounds from marine flora and fauna contain various types of pharmacologically active novel biomolecules enriched with different types of lectins. Lectins, with high saccharide binding specificities have been considered important probe to monitor the changes in plasmamembrance during physiological maturation of spermatozoa. Cytosol fraction, isolated from the spermatheca and / or ovotestis gland of a marine mollusc Telescopium telescopium, specific for sialic acid, has b...

  16. Recovering Bioactive Compounds from Olive Oil Filter Cake by Advanced Extraction Techniques

    OpenAIRE

    Jesús Lozano-Sánchez; María Castro-Puyana; Mendiola, Jose A.; Antonio Segura-Carretero; Alejandro Cifuentes; Elena Ibáez

    2014-01-01

    The potential of by-products generated during extra-virgin olive oil (EVOO) filtration as a natural source of phenolic compounds (with demonstrated bioactivity) has been evaluated using pressurized liquid extraction (PLE) and considering mixtures of two GRAS (generally recognized as safe) solvents (ethanol and water) at temperatures ranging from 40 to 175 °C. The extracts were characterized by high-performance liquid chromatography (HPLC) coupled to diode array detection (DAD) and electrospra...

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

    OpenAIRE

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

    2011-01-01

    Supercritical carbon dioxide (SC-CO2) extraction of bioactive compounds including flavonoids and phenolics from Ampelopsis grossedentata stems was carried out. Extraction parameters such as pressure, temperature, dynamic time and modifier, were optimized using an orthogonal array design of L9 (34), and antioxidant activities of the extracts were evaluated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and ferrous ion chelating (FIC) assay. The best conditions obtained f...

  18. Bioactive compounds in soluble cocoa products; polyphenols, dietary fibre and methylxanthines

    OpenAIRE

    Gómez Juaristi, Miren; Martínez López, Sara; Sarriá, Beatriz; Permanyer, J.; Mateos, Raquel; Bravo, Laura

    2013-01-01

    Cocoa powder is a highly consumed food product that may confer health benefits such as cardiovascular protection [1], antitumor and antioxidant effects [2]. These health benefits have been widely attributed to its phenolic composition and dietary fibre content [3]. Other bioactive compounds naturally present in cocoa are methylxanthines, alkaloids that induce modulation of the central nervous system. In response to cocoa consumers' demands, the food industry produces new cocoa products aimed ...

  19. Production of Nanofibers Containing the Bioactive Compound C-Phycocyanin.

    Science.gov (United States)

    Figueira, Felipe da Silva; Gettens, Juliana Garcia; Costa, Jorge Alberto Vieira; de Morais, Michele Greque; Moraes, Caroline Costa; Kalil, Susana Juliano

    2016-01-01

    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. PMID:27398551

  20. Study on endophytic bacteria for bioactive compound production use as plant protection agent

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    RUTH MELLIAWATI

    2006-07-01

    Full Text Available Endophytic microbes are microbes which live symbiotically inside the plant tissue. The potential of those microbes were studied for many purposes such as industrial and agriculture. The purpose of this research was to study the potential of endophytic microbes for bioactive compound production as plants protection agent. From 238 bacteria isolates tested, it were identified that 44 bacteria were against the Xanthomonas campestris, 49 isolates against Pseudomonas solanacearum, 28 isolates against Colletotricum gloeosporioides, 18 isolates against Fusarium oxysporum, 19 isolates against Xanthomonas campestris and Pseudomonas solanacearum, 6 isolates against X. campestris and C. gloeosporioides, four isolates against X. campestris and F. oxysporum, two isolates against P. solanacearum and F. oxysporum, seven isolates against C. gloeosporioides and F. oxysporum, five isolates againt X. campestris, P. solanacearum and C. gloeosporioides. Fermentation process was conducted to collect the bioactive compound against pathogen. Isolates HL.50B.106 could produce bioactive compound against C. gloeosporioides, and F. oxysporum, isolates HL.13B.21 against X. campestris and P. solanacearum, isolates Hl.12B.19 against X. campestris, P. solanacearum and C. gloeosporioides. Thin layer chromatography analysis showed specific spot, different from standard (media. Spot was purple in color after sprayed with CeSO4. Rf value of HL.50B.106 extract were 0.51 and 0.53 (fraction 1 and 2, 0.62 and 0.64 (fraction 3 and 4.

  1. Effects of orange winemaking variables on antioxidant activity and bioactive compounds

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    María del Carmen Schvab

    2015-09-01

    Full Text Available AbstractAscorbic acid, carotenoids and polyphenols stand out among the orange juice natural antioxidants. The winemaking process affects their bioavailability and bioactivity. Antioxidant activities (AA were estimated in different process conditions to asses those properties. The AA and their correlation with ascorbic acid, total phenolics and carotenoids content were calculated. The variables and levels analyzed were: pasteurized and natural must (PJ and NJ, pH 3.5 and 4.0 and fermentation temperatures at 10°C and 20°C. Statistically significant differences (α=0.05 were found among bioactive compounds concentrations. Antioxidant compounds concentration was higher in raw material than in orange wine. Juice pasteurization caused the major losses while subsequent vinification affects them to a lesser extent. Highest antioxidants retention was measured in wines from JN fermented at pH 3.5 and 10 °C (JN-3.5-10 followed by wines from JP and fermented at the same conditions (JP-3.5-10. AA determined by DPPH showed a positive and close correlation with FRAP, while ABTS showed a low correlation with former assays. Juice pasteurization process and fermentation temperature influenced bioactive compound reduction which correlates with the AA variation.

  2. Bioactive Compounds and Antioxidant Activity in Different Grafted Varieties of Bell Pepper

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    Celia Chávez-Mendoza

    2015-06-01

    Full Text Available 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.

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

    Science.gov (United States)

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

    2014-10-01

    This work evaluated the effect of carnauba and mineral oil coatings on the bioactive compounds and antioxidant capacity of tomato fruits (cv. "Grandela"). Carnauba and mineral oil coatings were applied on fresh tomatoes at two maturity stages (breaker and pink) over 28 day of storage at 10 °C was evaluated. Bioactive compound and antioxidant activity assays included total phenols, total flavonoids, ascorbic acid (ASA), lycopene, DPPH radical scavenging activity (%RSA), trolox equivalent antioxidant capacity (TEAC) and oxygen radical absorbance capacity assay (ORAC). The total phenolic, flavonoid and lycopene contents were significantly lower for coated fruit than control fruits. However, ascorbic acid content was highest in fruits treated with carnauba, followed by mineral oil coating and control fruits. The ORAC values were highest in breaker tomatoes coated with carnauba wax, followed by mineral oil-coated fruits and controls. No significant differences in ORAC values were observed in pink tomatoes. % RSA and TEAC values were higher for controls than for coated fruit. Edible coatings preserve the overall quality of tomatoes during storage without affecting the nutritional quality of fruit. We found that the physiological response to the coatings is in function of the maturity stage of tomatoes. The information obtained in this study support to use of edible coating as a safe and good alternative to preserve tomato quality, and that the changes of bioactive compounds and antioxidant activity of tomato fruits, was not negatively affected. This approach can be used by producers to preserve tomato quality. PMID:25328215

  4. Effects of Processing Treatments on the Bioactive Compounds of Campbell Grape Juice

    Directory of Open Access Journals (Sweden)

    Shirley G. Cabrera

    2015-11-01

    Full Text Available It is well known that phenolic compounds and flavonoids have a lot of health benefits. Most current heat treatments especially those that are using too high temperature and longer period of processing produce juice with unacceptable analytical and sensory properties. Thus, microwave heating, ultrasonication and blanching before grape juice processing were employed in this study. Each juice sample was subjected to total phenolics, total flavonoid, total anthocyanin and % radical scavenging activity analysis. Analysis of Variance and Duncan’s multiple range tests were performed using the SAS program. The concentration of total phenolics, total flavonoids, total anthocyanin and % radical scavenging activity of the grape juices treated with microwave heating and ultrasonication increased significantly with increasing treatment time notably at 5 min treatment. It can be noted that all the bioactive contents and % radical scavenging activity were higher in noncold stabilized grape juice than in cold stabilized juices. However, blanching whole grapes for longer period of time before processing resulted in the decrease of all bioactive compounds and % radical scavenging activity both in non-cold stabilized and cold stabilized juice especially at 5 min blanching period. It was also showed that 1 min blanching is more effective in increasing the bioactive compounds of the grape juice as compared to other treatment time.

  5. Synthesis of potentially bioactive compounds and tools for biological studies

    International Nuclear Information System (INIS)

    NMR spectroscopy is one of the most versatile tools for studying structural parameters of organic and bioorganic compounds. It became a highly suitable method to achieve spectra simplification of macromolecules in combination with isotope labeling techniques. This technique is used to study protein structures, folding properties and mechanisms of chemical and biochemical reactions. Proteins typically feature a high molecular mass showing a high number of spin systems, being responsible for increasingly difficult to interpret NMR spectra, which is why it is essential to introduce 13C- and 15N- isotopes to obtain reasonable signal intensities. The development of a new synthetic route towards 13C-isotope labeled Phenylalanine or precursors thereof, starting from inexpensive and easily accessible labeled starting materials, is the main purpose of this work. Label sources such as [13C]-acetic acid, [13C]-formaldehyde, [13C]-allyl alcohol and [13C]-glycine will be used. The synthetic pathway will be carried out in a way where the position-selective incorporation of labeled isotopes can be performed. This important feature of the synthesis may open access towards newly designed NMR-experiments. Key steps for the tested route are ring closing metatheses as well as indium mediated reactions. The second part of this work focuses on the field of sugar chemistry, in particular on the family of deoxy sugars, components of many natural products, found in different plants, fungi and bacteria. Deoxy sugars also participate in a wide range of biological processes. Special focus is given to 3-deoxy sugars and the research of a versatile and flexible synthetic route for their preparation starting from the easily accessible D-glyceraldehyde. These sugars are found on Gram-negative bacteria where they are a key component of the lipopolysaccharides, or where they can take place in the biosynthesis of aromatic amino acids in bacteria and plants. Being able to perform this synthesis on a

  6. Synthesis and evaluation of some bioactive compounds having oxygen and nitrogen heteroatom

    Indian Academy of Sciences (India)

    Poonam Yadav; Nalini V Purohit

    2013-01-01

    Some new 3,4-disubstituted isocoumarins were synthesized having bioactive pyrazole molecule at 3rd position of isocoumarin moiety (5a,b), from isocoumarin -3- carboxylic acid hydrazide (4a,b) followed by cyclization with acetyl acetone. A series of isocoumarin derivative having Schiff base as lateral side chain at 3rd position of isocoumarin moiety were also synthesized (7a,b), by condensing isocoumarin acid hydrazide and benzaldehyde derivative followed by dehydration. The chemical structures of all the compounds were determined by analytical and spectral method. The lead compounds were screened for antimicrobial and analgesic activities.

  7. Extraction Techniques for Bioactive Compounds and Antioxidant Capacity Determination of Chilean Papaya (Vasconcellea pubescens) Fruit

    OpenAIRE

    Elsa Uribe; Alvaro Delgadillo; Claudia Giovagnoli-Vicuña; Issis Quispe-Fuentes; Liliana Zura-Bravo

    2015-01-01

    The aim of this work was to assess and compare different extraction methods by using high hydrostatic pressure (HHPE), ultrasound (UE), agitation (AE), and their combinations for the extraction of bioactive compounds of Chilean papaya. Extract antioxidant capacity was evaluated by three methods (i.e., DPPH, FRAP, and Voltammetry) and phenolic compounds and vitamin C were determined by HPLC. Papaya sample extraction was performed by HHPE at 500 MPa for 10 min and UE and AE for 30 min, respecti...

  8. Fermentation of Plant Material - Effect on Sugar Content and Stability of Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Reis Bruno A. dos

    2014-12-01

    Full Text Available Extraction is a method often used to obtain products rich in bioactive compounds from plant material. Most of the solvents used for the poly-phenols extraction simultaneously extract also sugars, undesirable as a component of health-promoting food. Fermentation might be a simple, cheap and efficient way of sugar elimination. In our study, black tea and goji berries, both known for their health benefits, were used and alcoholic fermentation by Saccharomyces cerevisiae was carried out to eliminate sugars. In the course of fermentation the concentration of polyphenols, L-theanine and carotenoids was evaluated in order to verify the preservation of selected bioactive compounds. Decreases in sugar content, formation of ethanol and yeasts growth were monitored during fermentation. The fermentation of black tea decreased the sugar concentration by 84% within 6 h without decreasing total polyphenols and L-theanine contents. Goji berry fermentation yielded a sugars decrease of 87% within 24 h, without decrease in poly-phenol content. However, carotenoid content was reduced by 17%. The study showed that fermentation was an effective way to decrease sugar content in plant extracts, and therefore it might be a pertinent step to concentrate bioactives.

  9. Green algae Chlorococcum humicola- a new source of bioactive compounds with antimicrobial activity

    Institute of Scientific and Technical Information of China (English)

    Bhagavathy S; Sumathi P; Jancy Sherene Bell I

    2011-01-01

    Objective: To analyse the existence of bioactive phytochemicals and their antimicrobial role of green algae Chlorococcum humicola (C. humicola). Methods: The various organic solvents such as acetone, benzene, chloroform, diethyl ether, ethyl acetate, ethanol, hexane and methanol were used for the preparation of the algal extracts then subjected to chemical analysis and further used for the screening of antimicrobial assay. The purified carotenoid pigments and chlorophylls were used for the antimicrobial studies against the harmful pathogens Escherichia coli, Pseudomonasaeruginosa, Salmonella typhimurium, Klebsiella pneumoniae, Vibreo cholerae, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Aspergillus niger and Aspergillus flavus. Results: The chemical analysis showed the existence of bioactive compounds such as carotenoids, alkaloids, favanoids, fattyacids, saponins, aminoacids and carbohydrates. In vitro screening of organic solvent extracts of green algae C. humicola shows activity in inhibiting the growth of virulent strains of bacteria and fungi pathogenic to human. Eight different extracts showed effective inhibitory action against the selected pathogens. Depends upon their existence of the bioactive compounds the different organic algal extracts shows difference in their inhibitory zone against the microbes. Out of all the organic extracts benzene and ethyl acetate extracts showed excellent effect nearly 80% microbial growth inhibition. The separated carotenoid and chlorophyll fractions of C. humicola, also results in the microbial growth inhibition. Conclusions: The present study concludes that green algae C. humicola are a rich and varied source of pharmacologically active natural products and nutraceuticals. While nutraceutical and pharmaceutical content in the baseline algae strain is very small, they showed excellent effect against the microbial pathogens.

  10. Extraction and characterization of candidate bioactive compounds in different tissues from salmon (Salmo salar)

    DEFF Research Database (Denmark)

    Falkenberg, Susan Skanderup; Mikalsen, S. O.; Joensen, H.;

    2014-01-01

    and for their ability to inhibit activity of the proteases angiotensin I-converting enzyme (ACE) and dipeptidyl peptidase 4 (DPP-4). In vitro assays were used to detect these activities and the corresponding candidate bioactive compounds were characterized by LC-MS/MS.Radical scavenging activity was...... detected in <10kDa extracts of gills, belly flap muscle and skin with EC50 values of 39, 82 and 100 µg/mL, respectively. No ACE or DPP-4 inhibiting activity could be detected. LC-MS/MS analysis of dominating compounds in active fractions from size exclusion chromatography showed that families of related...... compounds were found in several fractions from different tissues but most pronounced in gills. One family was defined according to content of a specific amino acid sequence (PW). Three families were defined by the m/z value of the smallest compound reported in each family (219, 434 and 403). The three...

  11. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata

    Science.gov (United States)

    Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Clemente, Edmar

    2012-01-01

    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

  12. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata.

    Science.gov (United States)

    Specian, Vânia; Sarragiotto, Maria Helena; Pamphile, João Alencar; Clemente, Edmar

    2012-07-01

    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 (1)H and (13)C 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

  13. Chemical characterization of bioactive compounds from the endophytic fungus Diaporthe helianthi isolated from Luehea divaricata

    Directory of Open Access Journals (Sweden)

    Vânia Specian

    2012-09-01

    Full Text Available 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.

  14. Minimally processed mixed salad submitted to gamma radiation: effects on bioactive compounds

    International Nuclear Information System (INIS)

    High consumption of fruits and vegetables has been associated with a lowered incidence of oxidative stress-related diseases due to the presence of bioactive structures. Minimally processed products are a growing segment in food retail establishments because it is associated with practicality and convenience without significantly altering fresh-like characteristics. Low-dose of gamma radiation in combination with minimal processes has shown to be a promising strategy for extending shelf life and maintaining the organoleptic quality of fruits and vegetables. The objective of this study was to evaluate the levels of phenolic compounds, flavonoids, proanthocyanidins and antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH•) free radical scavenging and Oxygen Radical Absorbance Capacity (ORAC) method in minimally processed mixed salad before and after different radiation doses. Samples of minimally processed mixed salad (with green and red cabbage and carrot) were purchased at local supermarket and irradiated with doses of 0.5, 1.0, 2.0 and 3.0 kGy. Phenolic compounds, flavonoids, proanthocyanidins and antioxidant activity by DPPH• and ORAC were analyzed on the same extract prepared with MeOH. The results showed that bioactive compounds levels and antioxidant activity decreased significantly (p<0.05) with an increasing on radiation dose. Gamma-rays may affect these compounds and can cause degradation or oxidation, which can explain the drop on levels. Although the radiation has affected the bioactive contents, the process seems to be interesting to maintaining organoleptic characteristics and provide microbiological security at doses up to 2.0 kGy, according to studies conducted by our research group. (author)

  15. Minimally processed mixed salad submitted to gamma radiation: effects on bioactive compounds

    Energy Technology Data Exchange (ETDEWEB)

    Hirashima, Fabiana K.; Sabato, Susy F., E-mail: fmayumi@usp.br [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil); Lanfer-Marquez, Ursula M., E-mail: lanferum@usp.br [Universidade de Sao Paulo (FCF/USP), Sao Paulo, SP (Brazil). Faculdade de Ciencias Farmaceuticas. Dept. de Alimentos e Nutricao Experimental

    2015-07-01

    High consumption of fruits and vegetables has been associated with a lowered incidence of oxidative stress-related diseases due to the presence of bioactive structures. Minimally processed products are a growing segment in food retail establishments because it is associated with practicality and convenience without significantly altering fresh-like characteristics. Low-dose of gamma radiation in combination with minimal processes has shown to be a promising strategy for extending shelf life and maintaining the organoleptic quality of fruits and vegetables. The objective of this study was to evaluate the levels of phenolic compounds, flavonoids, proanthocyanidins and antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl (DPPH•) free radical scavenging and Oxygen Radical Absorbance Capacity (ORAC) method in minimally processed mixed salad before and after different radiation doses. Samples of minimally processed mixed salad (with green and red cabbage and carrot) were purchased at local supermarket and irradiated with doses of 0.5, 1.0, 2.0 and 3.0 kGy. Phenolic compounds, flavonoids, proanthocyanidins and antioxidant activity by DPPH• and ORAC were analyzed on the same extract prepared with MeOH. The results showed that bioactive compounds levels and antioxidant activity decreased significantly (p<0.05) with an increasing on radiation dose. Gamma-rays may affect these compounds and can cause degradation or oxidation, which can explain the drop on levels. Although the radiation has affected the bioactive contents, the process seems to be interesting to maintaining organoleptic characteristics and provide microbiological security at doses up to 2.0 kGy, according to studies conducted by our research group. (author)

  16. Infusion and decoction of wild German chamomile: bioactivity and characterization of organic acids and phenolic compounds.

    Science.gov (United States)

    Guimarães, Rafaela; Barros, Lillian; Dueñas, Montserrat; Calhelha, Ricardo C; Carvalho, Ana Maria; Santos-Buelga, Celestino; Queiroz, Maria João R P; Ferreira, Isabel C F R

    2013-01-15

    Natural products represent a rich source of biologically active compounds and are an example of molecular diversity, with recognised potential in drug discovery. Herein, the methanol extract of Matricaria recutita L. (German chamomile) and its decoction and infusion (the most consumed preparations of this herb) were submitted to an analysis of phytochemicals and bioactivity evaluation. The antioxidant activity was determined by free radicals scavenging activity, reducing power and inhibition of lipid peroxidation; the antitumour potential was tested in human tumour cell lines (breast, lung, colon, cervical and hepatocellular carcinomas), and the hepatotoxicity was evaluated using a porcine liver primary cell culture (non-tumour cells). All the samples revealed antioxidant properties. The decoction exhibited no antitumour activity (GI(50)>400 μg/mL) which could indicate that this bioactivity might be related to compounds (including phenolic compounds) that were not extracted or that were affected by the decoction procedure. Both plant methanol extract and infusion showed inhibitory activity to the growth of HCT-15 (GI(50) 250.24 and 298.23 μg/mL, respectively) and HeLa (GI(50) 259.36 and 277.67 μg/mL, respectively) cell lines, without hepatotoxicity (GI(50)>400 μg/mL). Infusion and decoction gave higher contents of organic acids (24.42 and 23.35 g/100g dw). Otherwise, the plant methanol extract contained the highest amounts of both phenolic acids (3.99 g/100g dw) and flavonoids (2.59 g/100g dw). The major compound found in all the preparations was luteolin O-acylhexoside. Overall, German chamomile contains important phytochemicals with bioactive properties (mainly antitumour potential selective to colon and cervical carcinoma cell lines) to be explored in the pharmaceutical, food and cosmetics industries. PMID:23122148

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

    Directory of Open Access Journals (Sweden)

    Albert Mas

    2014-01-01

    Full Text Available 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.

  18. GC-MS analysis of bioactive compounds in the methanol extract of Clerodendrum viscosum leaves

    Directory of Open Access Journals (Sweden)

    Pritipadma Panda

    2015-01-01

    Full Text Available 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(1HPyrimidinone,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.

  19. Experimental protocol for the recovery and evaluation of bioactive compounds of tarbush against postharvest fruit fungi.

    Science.gov (United States)

    De León-Zapata, Miguel A; Pastrana-Castro, Lorenzo; Rua-Rodríguez, María Luisa; Alvarez-Pérez, Olga Berenice; Rodríguez-Herrera, Raul; Aguilar, Cristóbal N

    2016-05-01

    The aim of this study was to recover and evaluate in vitro the antifungal activity of bioactive compounds of tarbush Flourensia cernua against fruit postharvest fungi and their antioxidant capacity. A yield of 15% of bioactive compounds of tarbush was obtained by infusion method and heating using water as solvent. A concentration of 4000 mg/L showed a higher antioxidant activity against the ABTS radical (3.21 μMol/g) in comparison with the DPPH radical (7.62 μMol/g); however the DPPH radical showed a better correlation with the content of tannins. The BCT showed values of IC50 between 1519 and 3310 mg/L against Rhizopus stolonifer, Botrytis cinerea, Fusarium oxysporum and Colletotrichum gloeosporioides. Antifungal activity is attributable mainly to gallic acid and flavonoids identified by infrared and HPLC analysis. In this study, the BCT have shown to be a possible natural alternative of antioxidant and antifungal compounds for use against postharvest fruit fungi. PMID:26769505

  20. GC-MS analysis of bio-active compounds in methanolic extract of Lactuca runcinata DC

    Directory of Open Access Journals (Sweden)

    Lakshmi Kanta Kanthal

    2014-01-01

    Full Text Available 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.

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

    Science.gov (United States)

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

    2014-01-15

    This study aimed to quantify the levels of resveratrol, coumarin, and other bioactives in pulps and by-products of twelve tropical fruits from Brazil obtained during pulp production process. Pineapple, acerola, monbin, cashew apple, guava, soursop, papaya, mango, passion fruit, surinam cherry, sapodilla, and tamarind pulps were evaluated as well as their by-products (peel, pulp's leftovers, and seed). Total phenolic, anthocyanins, yellow flavonoids, β-carotene and lycopene levels were also determined. Resveratrol was identified in guava and surinam cherry by-products and coumarin in passion fruit, guava and surinam cherry by-products and mango pulp. These fruit pulp and by-products could be considered a new natural source of both compounds. Overall, fruit by-products presented higher (P<0.05) bioactive content than their respective fruit pulps. This study provides novel information about tropical fruits and their by-products bioactive composition, which is essential for the understanding of their nutraceutical potential and future application in the food industry. PMID:24054258

  2. Identification and Characterization of Bioactive Compounds Targeting Uropathogenic Escherichia coli from Sanjin Tablets

    Directory of Open Access Journals (Sweden)

    Jie Meng

    2015-01-01

    Full Text Available Sanjin Tablets are completely natural preparation with significant efficacy in treating urinary tract infection. To identify the bioactive compounds from Sanjin Tablets, we separated components capable of binding to the soluble proteins of uropathogenic Escherichia coli (UPEC by affinity binding and characterized their identities using liquid chromatography-mass spectrometry (LC-MS analysis. Our study discovered eight compounds with E. coli protein-binding capabilities, and all these compounds were tracked back to the original natural ingredients of Sanjin Tablets. These compounds presented essentially no antibacteria activity, indicating that they affect UPEC by means other than directly killing the cells. Further molecular modeling analysis predicted molecular targets for these compounds and mapped the residues potentially involved in compound-target interactions. All the predicted targets turned out to be critical proteins regulating the metabolisms of E. coli, suggesting that these compounds may affect metabolic pathways in UPEC and inhibit pathogenesis. These data will benefit future design of drugs with higher efficacy and specificity on targeting pathogenic bacteria.

  3. Bioactive Compounds of Palm Fatty Acid Distillate (PFAD) from Several Palm Oil Refineries

    OpenAIRE

    Teti Estiasih1)*; Kgs. Ahmadi2); Tri Dewanti Widyaningsih; Jaya Mahar Maligan; Ahmad Zaki Mubarok; Elok Zubaidah; Jhauharotul Mukhlisiyyah; Risma Puspitasari

    2013-01-01

    This research studied the characteristics of Palm Fatty Acids Distillates (PFADs) from several palm oil refineries. It was aimed to know the potency of PFAD as bioactive compounds source, including vitamin E (mainly tocotrienols), phytosterols, squalene and possibly co-enzyme Q10 and polycosanol. Sampling was conducted at 6 palm oil refineries. The results showed that PFAD was dominated by free fatty acids of 85-95% with low oxidation level indicated by peroxide value of 1-10 meq/kg and anisi...

  4. The powerful in vitro bioactivity of Euterpe oleracea Mart. seeds and related phenolic compounds

    OpenAIRE

    Barros, Lillian; Ricardo C. Calhelha; Queiroz, Maria João R. P.; Santos-Buelga, Celestino; Santos, Elândia A.; Regis, Wiliam C. B.; Ferreira, Isabel C.F.R.

    2015-01-01

    The Euterpe oleracea Mart. (açaí) is a plant from the Amazon region, classified as "super fruit" because of its various functional properties. However, limited investigation has been performed on açaí by-products, such as seeds. Therefore, the aim of this work was to characterized the phenolic compounds of the aqueous extract of açaí seeds and further evaluate its bioactivity (antioxidant and cytotoxic activities. Only proanthocyanidins were detected, being a B-type (epi)catech...

  5. Studying a Drug-like, RNA-Focused Small Molecule Library Identifies Compounds That Inhibit RNA Toxicity in Myotonic Dystrophy.

    Science.gov (United States)

    Rzuczek, Suzanne G; Southern, Mark R; Disney, Matthew D

    2015-12-18

    There are many RNA targets in the transcriptome to which small molecule chemical probes and lead therapeutics are desired. However, identifying compounds that bind and modulate RNA function in cellulo is difficult. Although rational design approaches have been developed, they are still in their infancies and leave many RNAs "undruggable". In an effort to develop a small molecule library that is biased for binding RNA, we computationally identified "drug-like" compounds from screening collections that have favorable properties for binding RNA and for suitability as lead drugs. As proof-of-concept, this collection was screened for binding to and modulating the cellular dysfunction of the expanded repeating RNA (r(CUG)(exp)) that causes myotonic dystrophy type 1. Hit compounds bind the target in cellulo, as determined by the target identification approach Competitive Chemical Cross-Linking and Isolation by Pull-down (C-ChemCLIP), and selectively improve several disease-associated defects. The best compounds identified from our 320-member library are more potent in cellulo than compounds identified by high-throughput screening (HTS) campaigns against this RNA. Furthermore, the compound collection has a higher hit rate (9% compared to 0.01-3%), and the bioactive compounds identified are not charged; thus, RNA can be "drugged" with compounds that have favorable pharmacological properties. Finally, this RNA-focused small molecule library may serve as a useful starting point to identify lead "drug-like" chemical probes that affect the biological (dys)function of other RNA targets by direct target engagement. PMID:26414664

  6. EuroFIR-BASIS - a combined composition and biological activity database for bioactive compounds in plant-based foods

    DEFF Research Database (Denmark)

    Gry, Jørn; Black, Lucinda; Eriksen, Folmer Damsted; Pilegaard, Kirsten; Plumb, Jenny; Rhodes, Mike; Sheehan, Darina; Kiely, Mairéad; Kroon, Poul A.

    2007-01-01

    Mounting evidence suggests that certain non-nutrient bioactive compounds promote optimal human health and reduce the risk of chronic disease. An Internet-deployed database, EuroFIR-BASIS, which uniquely combines food composition and biological effects data for plant-based bioactive compounds, is...... being developed. The database covers multiple compound classes and 330 major food plants and their edible parts with data sourced from quality-assessed, peer-reviewed literature. The database will be a valuable resource for food regulatory and advisory bodies, risk authorities, epidemiologists and...... researchers interested in diet and health relationships, and product developers within the food industry....

  7. Bioactive compounds in different cocoa (Theobroma cacao, L cultivars during fermentation

    Directory of Open Access Journals (Sweden)

    Jaqueline Fontes Moreau Cruz

    2015-06-01

    Full Text Available One component that contribute to the flavor and aroma of chocolate are the polyphenols, which have received much attention due to their beneficial implications to human health. Besides bioactive action, polyphenols and methylxantines are responsible for astringency and bitterness in cocoa beans. Another important point is its drastic reduction during cocoa processing for chocolate production and the difference between cultivars. Thus, the present study aimed to evaluate the modifications in monomeric phenolic compounds and methylxanthines during fermentation of three cocoa cultivars grown in southern Bahia. Cocoa beans from three cultivars were fermented and sun dried and monomeric phenolic compounds and methylxantines were determinated. The results showed that each cultivar have different amounts of phenolic compounds and the behaviour of them is different during fermentation. The amount of methylxantines varied but there was not a pattern for methylxantines behavior during process. In addition a huge reduction in phenolic compounds could be observed after drying. Differently of phenolic compounds, methylxantines did not have great modification after sun drying. So, the differences observed in this study between cultivars, take to the conclusion that the compounds studied in those cocoa cultivars have different behavior during fermentation and drying, which consequently, give to these cultivars differences in sensory characteristics.

  8. The effect of probiotic microorganisms and bioactive compounds on chemically induced carcinogenesis in rats.

    Science.gov (United States)

    Bertkova, I; Hijova, E; Chmelarova, A; Mojzisova, G; Petrasova, D; Strojny, L; Bomba, A; Zitnan, R

    2010-01-01

    Diet interventions and natural bioactive supplements have now been extensively studied to reduce risks of colon cancer, which is one of the major public health problem throughout the world. The objective of our investigation was to study the effects of probiotic, prebiotic, nutritional plant extract, and plant oil on selected biochemical and immunological parameters in rats with colon cancer induced by N,N dimethylhydrazine (DMH). Male and female Wistar albino rats were were fed by a high-fat (HF) diet (10% fat in the diet) and were divided into 9 groups: Control group; PRO group - HF diet supplemented with probiotic Lactobacillus plantarum to provide 3 x 109 c.f.u. of strain/1 ml of medium; PRE group - HF diet supplemented with inulin enriched with oligofructose (2% of HF diet); HES group - HF diet supplemented with plant extract of Aesculus hippocastanum L. (1% of HF diet); OIL group - HF diet comprised Linioleum virginale (2% of HF diet); and combination of probiotic microorganisms and bioactive compounds in the groups - PRO-PRE, PRO-HES, PRO-OIL, PRE-OIL. Carcinogenesis was initiated with subcutaneous injection of DMH (20 mg/kg) two times at week interval and dietary treatments were continued for the six weeks. Application of probiotic microorganisms and bioactive compounds in all treated groups significantly decreased the activities of bacterial enzymes (p<0.001), the fecal bile acids concentration (p<0.01; p<0.001) and significantly increased serum TNFalpha level (p<0.001) in comparison to the control rats. The number of coliforms was reduced in PRO, PRO-PRE, PRO-OIL and PRE-OIL groups and significantly higher count of lactobacilli (p<0.05) was observed in PRO-PRE, PRO-OIL and PRE-OIL groups in compare with the controls. In conclusion, the results of this study indicate that probiotic microorganisms and bioactive compounds could exert a preventive effect on colon carcinogenesis induced by DMH. PMID:20568896

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

    Science.gov (United States)

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

    2015-03-25

    A method for the rapid in situ identification of bioactive compounds in fresh plants has been developed using in vivo nanospray coupled to high-resolution mass spectrometry (HR-MS). Using a homemade in vivo nanospray ion source, the plant liquid was drawn out from a target region and ionized in situ. The ionized bioactive compounds were then identified using Q-Orbitrap HR-MS. The accurate mass measurements of these bioactive compounds were performed by full-scan or selected ion monitoring (SIM), and tandem mass spectrometry (MS/MS) was used in the structural elucidation. Without sample pretreatment, 12 bioactive compounds in 7 different plant species were identified, namely, isoalliin in onion; butylphthalide in celery; N-methylpelletierine, pelletierine, and pseudopelletierine in pomegranate; chlorogenic acid in crabapple; solamargine, solasonine, and solasodine in nightshade; aloin and aloe-emodin in aloe; and menthone in mint. This work demonstrates that in vivo nanospray HR-MS is a good method for rapid in situ identification of bioactive compounds in plants. PMID:25749134

  10. Optimization of the extraction process for the seven bioactive compounds in Yukmijihwang-tang, an herbal formula, using response surface methodology

    OpenAIRE

    Jung-Hoon Kim; Hyeun-Kyoo Shin; Chang-Seob Seo

    2014-01-01

    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 numb...

  11. Determination of some physicochemical characteristics, bioactive compounds and antioxidant activity of tropical fruits from Yucatan, Mexico.

    Science.gov (United States)

    Moo-Huchin, Víctor M; Estrada-Mota, Iván; Estrada-León, Raciel; Cuevas-Glory, Luis; Ortiz-Vázquez, Elizabeth; Vargas y Vargas, María de Lourdes; Betancur-Ancona, David; Sauri-Duch, Enrique

    2014-01-01

    The aim to the study was to determine the physicochemical composition, bioactive compounds and antioxidant activity of fruits from Yucatan, Mexico such as star apple, cashew, mombin, mamey sapote, white sapote, sugar apple, sapodilla, dragon fruit, nance, ilama, custard apple, mamoncillo and black sapote. The physicochemical characteristics were different between fruits and were good sources of bioactive compounds. The edible part with the highest values of antioxidant activity were mamoncillo, star apple, mombin, cashew, white sapote, ilama, custard apple, sugar apple, and nance. Total soluble phenols content showed a correlation with antioxidant activity by ABTS (R=0.52, P⩽0.05) and DPPH (R=0.43, P⩽0.05). A high correlation was obtained between the two assays (ABTS and DPPH) used to measure antioxidant activity in the tropical fruit species under study (R=0.82, P⩽0.05). The results show promising perspectives for the exploitation and use of tropical fruits studied with significant levels of nutrients and antioxidant activity. PMID:24444968

  12. Recovering bioactive compounds from olive oil filter cake by advanced extraction techniques.

    Science.gov (United States)

    Lozano-Sánchez, Jesús; Castro-Puyana, María; Mendiola, Jose A; Segura-Carretero, Antonio; Cifuentes, Alejandro; Ibáñez, Elena

    2014-01-01

    The potential of by-products generated during extra-virgin olive oil (EVOO) filtration as a natural source of phenolic compounds (with demonstrated bioactivity) has been evaluated using pressurized liquid extraction (PLE) and considering mixtures of two GRAS (generally recognized as safe) solvents (ethanol and water) at temperatures ranging from 40 to 175 °C. The extracts were characterized by high-performance liquid chromatography (HPLC) coupled to diode array detection (DAD) and electrospray time-of-flight mass spectrometry (HPLC-DAD-ESI-TOF/MS) to determine the phenolic-composition of the filter cake. The best isolation procedure to extract the phenolic fraction from the filter cake was accomplished using ethanol and water (50:50, v/v) at 120 °C. The main phenolic compounds identified in the samples were characterized as phenolic alcohols or derivatives (hydroxytyrosol and its oxidation product), secoiridoids (decarboxymethylated and hydroxylated forms of oleuropein and ligstroside aglycones), flavones (luteolin and apigenin) and elenolic acid derivatives. The PLE extraction process can be applied to produce enriched extracts with applications as bioactive food ingredients, as well as nutraceuticals. PMID:25226536

  13. Chemical composition, fatty acid profile and bioactive compounds of guava seeds (Psidium guajava L.

    Directory of Open Access Journals (Sweden)

    Ana Maria Athayde Uchôa-thomaz

    2014-09-01

    Full Text Available This study aimed to characterize the chemical composition, determine the fatty acid profile, and quantify the bioactive compounds present in guava seed powder (Psidium guajava L.. The powder resulted from seeds obtained from guava pulp processing. The agro-industrial seeds from red guava cv. paluma were used, and they were donated by a frozen pulp fruit manufacturer. They contain varying amounts of macronutrients and micronutrients, with a high content of total dietary fiber (63.94 g/100g, protein (11.19 g/100g, iron (13.8 mg/100g, zinc (3.31 mg/100g, and reduced calorie content (182 kcal/100g. Their lipid profile showed a predominance of unsaturated fatty acids (87.06%, especially linoleic acid (n6 and oleic acid (n9. The powder obtained contained significant amounts of bioactive compounds such as ascorbic acid (87.44 mg/100g, total carotenoids (1.25 mg/100 g and insoluble dietary fiber (63.55 g/100g. With regard to their microbiological quality, the samples were found suitable for consumption. Based on these results, it can be concluded that the powder produced has favorable attributes for industrial use, and that use of these seeds would be a viable alternative to prevent various diseases and malnutrition in our country and to reduce the environmental impact of agricultural waste.

  14. Isolation of Bioactive Compounds from Sunflower Leaves (Helianthus annuus L.) Extracted with Supercritical Carbon Dioxide.

    Science.gov (United States)

    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

    2015-07-22

    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. PMID:26151222

  15. Separation and identification of bioactive compounds in Anabasis articulata (Forsk) Moq. roots.

    Science.gov (United States)

    Ghembaza, Nacéra; Belyagoubi-Benhammou, Nabila; Atik Bekkara, Fawzia

    2016-01-01

    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. PMID:26263238

  16. Citrus fruits by-products as sources of bioactive compounds with antioxidant potential

    International Nuclear Information System (INIS)

    Peel and pulp from Orlando orange, Kinnow mandarin and Eureka lemon fruits were evaluated for phenolic compounds, ascorbic acid contents and free radical scavenging activities. Pulp from orange, mandarin and lemon contained 123.02, 104.98 and 98.38 mg GAE/100 g total phenolics; 61.38, 38.52 and 57.63 mg/100g ascorbic acid and 69.31, 62.82 and 59.60 % DPPH radical scavenging activities, respectively. Peel from orange, mandarin and lemon contained 178.90, 169.54 and 61.22 mg GAE/100 g total phenolics; 62.45, 54.87 and 25.68 mg/100g ascorbic acid and 67.58, 68.57 and 46.98% DPPH radical scavenging activities, respectively. The data reveals that these citrus by-products are good sources of bioactive compounds and be considered as antioxidant constituents for developing functional foods. (author)

  17. Effects of elevated CO2 and temperature on Gynostemma pentaphyllum physiology and bioactive compounds.

    Science.gov (United States)

    Chang, Jia-Dong; Mantri, Nitin; Sun, Bin; Jiang, Li; Chen, Ping; Jiang, Bo; Jiang, Zhengdong; Zhang, Jialei; Shen, Jiahao; Lu, Hongfei; Liang, Zongsuo

    2016-06-01

    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. PMID:27054772

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

    Science.gov (United States)

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

    2009-10-01

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

  19. Nutrients and bioactive compounds in popular and indigenous durian (Durio zibethinus murr.).

    Science.gov (United States)

    Charoenkiatkul, Somsri; Thiyajai, Parunya; Judprasong, Kunchit

    2016-02-15

    This study identified nutrients, fatty acids, bioactive compounds and antioxidant activities of two popular varieties (Mon-thong, Cha-ni) and two indigenous varieties (Kra-dum and Kob-ta-kam) of durian. Each of variety was collected from 3 gardens in Nonthaburi province, Thailand. At optimal ripeness, the edible part was separated, homogenised or freeze dried, as fresh or dry samples for further analysis using standard methods. All durian varieties contained a considerable amount of dietary fibre (7.5-9.1g/100g dry matter, DM) and high amounts of carbohydrate and sugar (62.9-70.7g and 47.9-56.4g/100g DM respectively). Cha-ni, Kra-dum and Kob-ta-kam varieties had monounsaturated (MUFA) (6.1-7.8g/100g DM)>saturated (SFA) (4.2-5.7g/100g DM)>polyunsaturated fatty acid (PUFA) (0.8-1.5g/100g DM), whereas the Mon-thong variety had SFA>MUFA>PUFA (5.1, 4.0, 1.1g/100g DM, respectively). The Kob-ta-kam variety showed greater potential for health benefits in terms of carotenoids and β-carotene (2248μg and 1202μg/100g DM respectively). Phenolic compounds and antioxidant capacity were not significantly different among each variety, though the Cha-ni variety had the lowest. This study provides data on nutrients, bioactive compounds and antioxidant activities of indigenous and popular durian varieties that could be used for consumer education as well as for incorporation into the food composition databases. PMID:26433306

  20. Bioactive Compounds Screening from Zingiberaceae Family as Influenza A/Swine Flu Virus Neuraminidase Inhibitor through Docking Approach

    Directory of Open Access Journals (Sweden)

    Usman S.F. Tambunan

    2010-01-01

    Full Text Available Problem statement: Influenza A/H1N1 is a disease caused by infection of influenza a virus subtype H1N1. It is a major health problem in tropical and subtropical countries. This virus constantly mutates and consequently will be developed into new drug-resistant strains. Approach: In this research, we have conducted docking study to screen bioactive compounds from Zingiberaceae family, which has a role as neuraminidase inhibitor of influenza a virus. Results: The docking result identified that 1, 2-di-O- β-D-glucopyranosyl-4-allylbenzene (BGA compound has the affinity and ability to inhibit neuraminidase. There are fourteen residues contact of BGA compound to neuraminidase and eight residues contact of enzyme that formed hydrogen bond with catalytic site. Conclusion/recommendation: The docking result showed that BGA has better binding energy and affinity compared with other bioactive compounds and the standard compounds.

  1. The Investigation of Some Bioactive Compounds and Antioxidant Properties of Hawthorn (Crataegus monogyna subsp. monogyna jacq.

    Directory of Open Access Journals (Sweden)

    Serhat KESER

    2014-04-01

    Full Text Available 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. For this purpose, antioxidant activities of extracts were assessed on DPPH and #8226;, ABTS and #8226;+, superoxide scavenging, reducing power and ferrous metal chelating activity assays and phenolic content of extracts was determined by Folin-Cioacalteu and #8217;s reagent. The flavonoids including rutin, apigenin, myricetin, quercetin, naringenin and kaempferol, were identified by HPLC in the hawthorn extract. It was observed the aqueous and ethanol extracts of Crataegus monogyna subsp. monogyna fruits showed highest activity in reducing power and metal chelating activity assays. Additionally, it was determined that the aqueous flower extract showed higher flavonoid content than aqueous leaves extract. [J Intercult Ethnopharmacol 2014; 3(2.000: 51-55

  2. Induction of bioactive compound composition from marine microalgae (Lyngbya sp.) by using different stress condition

    Institute of Scientific and Technical Information of China (English)

    Nurul Farhana Rosly; Rabeah Adawiyah Abdul Razak; Palaniselvam Kuppusamy; Mashitah M. Yusoff; Natanamurugaraj Govindan

    2013-01-01

    Objective: To the effect of salinity stress on the production of microalgae (Lyngbya sp.) and chlorophyll pigments in the growth medium.Methods:Stress was investigated by using green algae strains Lyngbya sp. in response to change bioactive compounds without any modification of cell growth and biomass production rate. The different stress conditions like 10%-40% were analyzed.Results:During the stress condition, various biochemical and microbiological assays were monitored. The photochemical composition was evaluated by GC-MS studies. The studies expressed that 30% higher salinity stress was suitable for high phytochemical production rate including chlorophyll content.Conclusions:Our study indicates the wide range of salinity stress to enhance the growth on microalgae culture and enhance the production of major secondary metabolites.

  3. Simultaneous extraction and biotransformation process to obtain high bioactivity phenolic compounds from Brazilian citrus residues.

    Science.gov (United States)

    Madeira, Jose Valdo; Macedo, Gabriela Alves

    2015-01-01

    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. PMID:26081498

  4. Strawberry Achenes Are an Important Source of Bioactive Compounds for Human Health

    Directory of Open Access Journals (Sweden)

    María Teresa Ariza

    2016-07-01

    Full Text Available 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.

  5. Use of Time-Resolved Fluorescence to Monitor Bioactive Compounds in Plant Based Foodstuffs.

    Science.gov (United States)

    Lemos, M Adília; Sárniková, Katarína; Bot, Francesca; Anese, Monica; Hungerford, Graham

    2015-01-01

    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

  6. Use of Time-Resolved Fluorescence to Monitor Bioactive Compounds in Plant Based Foodstuffs

    Directory of Open Access Journals (Sweden)

    M. Adília Lemos

    2015-06-01

    Full Text Available 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.

  7. Strawberry Achenes Are an Important Source of Bioactive Compounds for Human Health

    Science.gov (United States)

    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

    2016-01-01

    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

  8. Strawberry Achenes Are an Important Source of Bioactive Compounds for Human Health.

    Science.gov (United States)

    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

    2016-01-01

    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

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

    Directory of Open Access Journals (Sweden)

    Dario Donno

    2016-02-01

    Full Text Available 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

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

    Science.gov (United States)

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

    2016-01-01

    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

  11. Variation of Bioactive Compounds in Hypericum perforatum Growing in Turkey During Its Phenological Cycle

    Institute of Scientific and Technical Information of China (English)

    Cüneyt Cirak; Jolita Radusiěnё; Birsen (Sa(g)lam) Karabük; Valdimaras Janulis; Liudas Ivanauskas

    2007-01-01

    The present study was conducted to determine phenologic and morphogenetic variation of hypericin, chlorogenic acid and flavonoids, as rutin, hyperoside, apigenin-7-O-glucoside, quercltrin, quercetin content of Hypericum perforatum L. growing in Turkey. Wild growing plants were harvested at vegetative, floral budding, full flowering,fresh fruiting and mature fruiting stages and dissected into stem, leaf and reproductive tissues and assayed for bioactive compounds by the High performance liquid chromatography (HPLC) method. Hyperlcin concentration ranged between 0 and 2.73 mg/g DW, chlorogenic acid 0.00-3.64 mg/g DW, rutin 0.00-3.36 mg/g DW, hyperoside 0.04-22.42 mg/g DW, quercitrin 0.03-3.45 mg/g DW and quercetin 0.04-1.02 mg/g DW depending on ontogenetic and morphogenetic sampling. Leaves were found to be superior to stems and reproductive parts with regard to phenolic accumulation for all compounds tested while flowers accumulated the highest levels of hypericin. Quercitrin,quercetin and hypericin content in all tissues increased with advancing of developmental stages and reached their highest level during flower ontogenesis. Similarly, chlorogenic acid, hyperoside and apigenin-7-O-glucoside content in different plant parts increased during plant development, however, the highest level was observed at different stages of plant phenology for each tissue. Chlorogenic acid was not detected in stems, leaves and reproductive parts in several stages of plant phenology and its variation during plant growth showed inconsistent manner. In contrast to the other compounds examined, rutin content of stems and leaves decreased with advancing of plant development and the highest level for both tissues was observed at the vegetative stage. However,content of the same compound in reproductive parts was the highest at mature fruiting. The present findings might be useful to obtain increased concentration of these natural compounds.

  12. Comparison of the contents of bioactive compounds and the level of antioxidant activity in different kiwifruit cultivars

    Czech Academy of Sciences Publication Activity Database

    Park, Y.S.; Leontowicz, H.; Leontowicz, M.; Namiesnik, J.; Suhaj, M.; Cvikrová, Milena; Martincová, Olga; Weisz, M.; Gorinstein, S.

    2011-01-01

    Roč. 24, č. 7 (2011), s. 963-970. ISSN 0889-1575 Institutional research plan: CEZ:AV0Z50380511 Keywords : Kiwifruits cultivars * Actinidia sp. * Bioactive compounds Subject RIV: EF - Botanics Impact factor: 2.079, year: 2011

  13. Physico-chemical characterization of chitosan-based edible films incorporating bioactive compounds of different molecular weight

    OpenAIRE

    Bourbon, A. I.; A.C. Pinheiro; Cerqueira, M. A.; Rocha, Cristina M. R.; Avides, Maria do Carmo; Quintas, Mafalda A. C.; Vicente, A.A.

    2011-01-01

    Chitosan packaging films containing different bioactive compounds (a peptide fraction from whey protein concentrate (WPC) hydrolysate, glycomacropeptide (GMP) and lactoferrin) were produced and their mechanical and barrier properties were evaluated. The molecular weight of protein-based compounds was determined using SDS–PAGE. The addition of GMP and lactoferrin to chitosan film caused a significant reduction of tensile strength and the elongation-at-break significantly increased ...

  14. Cooking techniques improve the levels of bioactive compounds and antioxidant activity in kale and red cabbage.

    Science.gov (United States)

    Murador, Daniella Carisa; Mercadante, Adriana Zerlotti; de Rosso, Veridiana Vera

    2016-04-01

    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. PMID:26593594

  15. Bioactive compounds and sensory quality of black and white mulberries grown in Spain.

    Science.gov (United States)

    Calín-Sánchez, Angel; Martínez-Nicolás, Juan José; Munera-Picazo, Sandra; Carbonell-Barrachina, Angel A; Legua, Pilar; Hernández, Francisca

    2013-12-01

    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. PMID:23979495

  16. Could gestational diabetes mellitus be managed through dietary bioactive compounds? Current knowledge and future perspectives.

    Science.gov (United States)

    Santangelo, Carmela; Zicari, Alessandra; Mandosi, Elisabetta; Scazzocchio, Beatrice; Mari, Emanuela; Morano, Susanna; Masella, Roberta

    2016-04-14

    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. PMID:26879600

  17. Use of ultrasound radiation for extraction of bioactive compounds from natural sources. Current events and perspectives

    International Nuclear Information System (INIS)

    In recent years, clean technologies have been developed for high efficiency extracting of isolation of biologically active compounds from natural sources, without the loss of biological activity, with good yield and high purity. Ultrasound-assisted extraction has low instrumental requirements and their implementation is very appropriate where the stability of the active component to be removed is affected by the high temperatures of conventional processes. In this paper it is evaluated the state of the art of ultrasound-assisted extraction of bioactive compounds from various natural sources, its mechanism, the parameters governing its use and research perspectives in this field. Ultrasonic cavitation phenomenon promotes cell wall rupture, reduction of particle size and tissue permeability, which facilitates the diffusion of the solvent into the inert part of the plant material and increasing the mass transferred through membranes. This mechanism explains the high efficiency of ultrasound-assisted extraction as it allows to reduce the time, temperature and amounts of solvent extraction process with high yields and high purity of the extracted product. Currently there is a great demand for the use of ultrasound to industrial and current research lead to the development of larger scale reactors and the theoretical modeling of the parameters that determine efficient extraction

  18. Assessment of by-products from fresh-cut products for reuse as bioactive compounds.

    Science.gov (United States)

    Tarazona-Díaz, M P; Aguayo, E

    2013-10-01

    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 (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. PMID:23733809

  19. Salinity effect on nutritional value, chemical composition and bioactive compounds content of Cichorium spinosum L.

    Science.gov (United States)

    Petropoulos, Spyridon A; Levizou, Efi; Ntatsi, Georgia; Fernandes, Ângela; Petrotos, Konstantinos; Akoumianakis, Konstantinos; Barros, Lillian; Ferreira, Isabel C F R

    2017-01-01

    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). PMID:27507457

  20. Bioactive compounds in Bidens pilosa L. populations: a key step in the standardization of phytopharmaceutical preparations

    Directory of Open Access Journals (Sweden)

    Diego F. Cortés-Rojas

    2013-02-01

    Full Text Available The total flavonoid content (TFC, total polyphenols content (TPC, and in vitro antioxidant activity (AA of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL. The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL. A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.

  1. Bioactive compounds in Bidens pilosa L. populations: a key step in the standardization of phytopharmaceutical preparations

    Directory of Open Access Journals (Sweden)

    Diego F. Cortés-Rojas

    2012-01-01

    Full Text Available The total flavonoid content (TFC, total polyphenols content (TPC, and in vitro antioxidant activity (AA of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL. The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL. A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.

  2. Bioactive compounds in banana and their associated health benefits - A review.

    Science.gov (United States)

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

    2016-09-01

    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. PMID:27041291

  3. Microbial Transformation of Bioactive Compounds and Production of ortho-Dihydroxyisoflavones and Glycitein from Natural Fermented Soybean Paste

    Directory of Open Access Journals (Sweden)

    Changhyun Roh

    2014-12-01

    Full Text Available 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.

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

    Science.gov (United States)

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

    2016-05-20

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

  5. Rapid screening and quantitative determination of bioactive compounds from fruit extracts of Myristica species and their in vitro antiproliferative activity.

    Science.gov (United States)

    Pandey, Renu; Mahar, Rohit; Hasanain, Mohammad; Shukla, Sanjeev K; Sarkar, Jayanta; Rameshkumar, K B; Kumar, Brijesh

    2016-11-15

    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. PMID:27283658

  6. Cell Survival and Apoptosis Signaling as Therapeutic Target for Cancer: Marine Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Kim Se-Kwon

    2013-01-01

    Full Text Available 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.

  7. Green alga Ulva pertusa--a new source of bioactive compounds with antialgal activity.

    Science.gov (United States)

    Ying-ying, Sun; Hui, Wang; Gan-lin, Guo; Yin-fang, Pu; Bin-lun, Yan; Chang-hai, Wang

    2015-07-01

    We tested the effects of solvent fractions (FA, FB, FC, and FD), which partitioned by liquid-liquid extraction from the methanol extract of Ulva pertusa, on the growth of red tide microalgae (Karenia mikimitoi, Skeletonema costatum, Alexandrium tamarense, Heterosigma akashiwo, Prorocentrum donghaiense), and FA, FB, and FC exhibited significantly antialgal activity. The chemical constituent analysis showed the existence of bioactive compounds such as phenols and alkaloids. Further, four solvent fractions were applied to silica gel column and repeated preparative TLC to produce 13 samples and their purity qualified as thin-layer chromatographic grade. Among these purified samples, FA111, FB411, FC411, FD111, and FD211 exhibited stronger antialgal activity. Furthermore, their functional groups were analyzed by colorimetric methods and UV spectra data. FD111 and FD211 were temptatively identified as alkaloids; the others were initially identified as phenolic acids. This is a preliminary study and the structure identification of these purified samples requires further investigation. While concentration of these purified samples in this algae was very small, they showed excellent effects against red tide microalgae. PMID:25724801

  8. Bioactive compounds and antioxidative activity of colored rice bran

    Directory of Open Access Journals (Sweden)

    Yu-Ping Huang

    2016-07-01

    Full Text Available The profiles of bioactive compounds (including phenolics and flavonoids in free and bound fractions, anthocyanins, proanthocyanidins, vitamin E, and γ-oryzanol of outer and inner rice bran from six colored rice samples collected from local markets were investigated. Proanthocyanidins could only be detected in red rice bran but not in black rice bran. The free fraction of the extracts dominated the total phenolics (72–92% and the total flavonoids (72–96% of colored rice bran. Most of the phenolic acids (83–97% in colored rice bran were present in the bound form. Protocatechualdehyde was identified for the first time in the bound fraction of red rice bran by high performance liquid chromatography-photodiode array/electrospray ionization tandem mass spectrometry. The antioxidative activities of the free fraction of the colored rice bran were attributed to the proanthocyanidins in red colored rice and anthocyanins in black rice, while that of the bound fraction was mainly due to the phenolic acids.

  9. Isolation of Bioactive Compounds That Relate to the Anti-Platelet Activity of Cymbopogon ambiguus

    Directory of Open Access Journals (Sweden)

    I. Darren Grice

    2011-01-01

    Full Text Available Infusions and decoctions of Cymbopogon ambiguus have been used traditionally in Australia for the treatment of headache, chest infections and muscle cramps. The aim of the present study was to screen and identify bioactive compounds from C. ambiguus that could explain this plant’s anti-headache activity. A dichloromethane extract of C. ambiguus was identified as having activity in adenosine-diphosphate-induced human platelet aggregation and serotonin-release inhibition bioassays. Subsequent fractionation of this extract led to the isolation of four phenylpropenoids, eugenol, elemicin, eugenol methylether and trans-isoelemicin. While both eugenol and elemicin exhibited dose-dependent inhibition of ADP-induced human platelet serotonin release, only eugenol displayed potent inhibitory activity with an IC50 value of 46.6 μM, in comparison to aspirin, with an IC50 value of 46.1 μM. These findings provide evidence to support the therapeutic efficacy of C. ambiguus in the non-conventional treatment of headache and inflammatory conditions.

  10. Fractionation and Purification of Bioactive Compounds Obtained from a Brewery Waste Stream

    Directory of Open Access Journals (Sweden)

    Letricia Barbosa-Pereira

    2013-01-01

    Full Text Available 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.

  11. Identification of a Bioactive Compound against Adult T-cell Leukaemia from Bitter Gourd Seeds

    Science.gov (United States)

    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

    2013-01-01

    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.

  12. Effect of extrusion cooking on bioactive compounds in encapsulated red cactus pear powder.

    Science.gov (United States)

    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

    2015-01-01

    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. PMID:25993418

  13. Effect of Extrusion Cooking on Bioactive Compounds in Encapsulated Red Cactus Pear Powder

    Directory of Open Access Journals (Sweden)

    Martha G. Ruiz-Gutiérrez

    2015-05-01

    Full Text Available 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.

  14. Ultraviolet Irradiation Effect on Apple Juice Bioactive Compounds during Shelf Storage

    Directory of Open Access Journals (Sweden)

    Edmundo Juarez-Enriquez

    2016-02-01

    Full Text Available 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.

  15. Modulation of Banana Polyphenol Oxidase (Ppo Activity by Naturally Occurring Bioactive Compounds From Plant Extracts

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    Alamelumangai. M

    2015-01-01

    Full Text Available Polyphenol Oxidase (PPO (E.C number 1.14.18.1 was extracted from banana (Musa paradisiaca and partially purified by acetone precipitation. The enzyme was found to have high affinity towards its substrate, catechol. In this study, various plant extracts like Glycyrrhiza glabra, Rubia cordifolia, Hesperethusa crenulata and oil from the seeds of Hydnocarpus laurifolia were observed to modulate the activity of banana PPO. Method In this study, various plant extracts were observed to modulate the activity of banana PPO at two different concentrations (0.4 and 40 μg/ml concentrations Result Among these 4 plant extracts, Glycyrrhiza glabra and Rubia cordifolia were found to increase the activity of PPO up to 1.35- 2.7 fold at two different concentrations (4 and 40 μg/ml. Few other two samples like Chaulmogra oil (2 and 4 μl/ml and the Hesperethusa crenulata plant extract (0.4 and 40 μg/ml concentrations, when used at low concentrations decreased the enzyme activity (38 %. Conclusion The novelty of this study is to screen their naturally occurring bioactive compounds from the plant extracts and their inhibitory activity against PPO.

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

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    Da Sun

    2011-10-01

    Full Text Available 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.

  17. Microencapsulation of lipophilic bioactive compounds using prebiotic carbohydrates: Effect of the degree of inulin polymerization.

    Science.gov (United States)

    Silva, Eric Keven; Zabot, Giovani L; Bargas, Matheus A; Meireles, M Angela A

    2016-11-01

    This paper presents novel outcomes about the effect of degree of inulin polymerization (DP) on the technological properties of annatto seed oil powder obtained by freeze-drying. Inulins with two DP's were evaluated: GR-inulin (DP≥10) and HP-inulin (DP≥23). Micrographs obtained by confocal microscopy were analyzed to confirm the encapsulation of bioactive compounds using both inulins, especially the encapsulation of the natural fluorescent substance δ-tocotrienol. Microparticles formed with both inulins presented the same capacity for geranylgeraniol retention (77%). Glass transitions of microparticles formed with GR-inulin and HP-inulin succeeded at 144°C and 169°C, respectively. Regarding water adsorption isotherms, microparticles formed with HP-inulin and GR-inulin presented behaviors of Types II (sigmoidal) and III (non-sigmoidal), respectively. Reduction of water adsorption capacity in the matrix at high relative moistures (>70%) was presented when HP-inulin was used. At low relative moistures (<30%), the opposite behavior was observed. PMID:27516329

  18. Microbial Communities and Bioactive Compounds in Marine Sponges of the Family Irciniidae—A Review

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    Cristiane C. P. Hardoim

    2014-09-01

    Full Text Available 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.

  19. Bioactive Compounds in Potato Tubers: Effects of Farming System, Cooking Method, and Flesh Color.

    Science.gov (United States)

    Grudzińska, Magdalena; Czerko, Zbigniew; Zarzyńska, Krystyna; Borowska-Komenda, Monika

    2016-01-01

    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

  20. Bioactive Compounds in Potato Tubers: Effects of Farming System, Cooking Method, and Flesh Color

    Science.gov (United States)

    Czerko, Zbigniew; Zarzyńska, Krystyna; Borowska-Komenda, Monika

    2016-01-01

    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

  1. Bioactive compounds in blood oranges (Citrus sinensis (L.) Osbeck): Level and intake.

    Science.gov (United States)

    Fallico, Biagio; Ballistreri, Gabriele; Arena, Elena; Brighina, Selina; Rapisarda, Paolo

    2017-01-15

    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. PMID:27542451

  2. Effects on Animal Models of Depression of Bioactive Compounds from Entomogenous Fungi, A Novel Antioxidant

    Institute of Scientific and Technical Information of China (English)

    周兰兰; 明亮; 马传庚; 樊美珍; 程燕; 江勤

    2004-01-01

    Objective: To study the antidepressant effects and its mechanism of bioactive compounds (metabolite extract) from entomogenous fungi (BCEF) on experimental animal models of depression. Methods: The antidepressant effect of BCEF was examined on the acquired models of depression (rats and mice in forced swimming test) and unpredictable chronic stress mouse models. The behavior alterations were assayed by detecting the duration of immobility in forced swimming test. UV spectrophotometer analysis technique was used to detect the activity of superoxide dismutase (SOD), glutathione peroxidase (GSH-PX) and catalase (CAT) in mice brain mitochondria; and colorimetric method was used to detect the content of malondealdehyde (MDA), nitrogen oxide (NO) in rat brain cytoplasm and mitochondria. Results: BCEF (25, 50,100 mg/kg) could obviously shorten the immobility time in forced swimming mice and BCEF (50,100 mg/kg)could obviously shorten the immobility time in forced swimming rats. Both of them showed some extent of dose-effect relationship. BCEF (50, 100 mg/kg) could significantly inhibit the increase of MDA and NO content in brain mitochondria and cytoplasm in chronic unpredictable stress models. BCEF (25,50,100 mg/kg)could obviously enhance the activities of SOD and GSH-PX. BCEF (50 mg/kg) also enhances the activities of CAT. Conclusion: BCEF has antidepressant effects in depressed animal models. The anti-oxidation may be one of the important mechanisms.

  3. Bioactive Compounds in Potato Tubers: Effects of Farming System, Cooking Method, and Flesh Color.

    Directory of Open Access Journals (Sweden)

    Magdalena Grudzińska

    Full Text Available 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.

  4. Antidepressant effect of bioactive compounds from Paecilomyces tenuipes in mice and rats

    Institute of Scientific and Technical Information of China (English)

    Hongwei Kan; Liang Ming; Chunru Li; Hongxing Kan; Bei Sun; Yan Liang

    2010-01-01

    A bioactive compound from Paecilomyces tenuipes(BCPT)has an inhibitory effect on monoamine oxidase A(MAO-A)in vitro.Researchers have thought that BCPT may be a potential antidepressant.The MAO-A suppressor moclobemide served as a control,and this study investigated the mechanisms of BCPT as an antidepressant.Results demonstrated that BCPT induced significantly increased sucrose intake in chronic unpredictable stressed rats,shortened immobility time in forced swimming mice,improved the scores of blepharoptosis and akinesia in reserpine-treated mice,increased the number of 5-hydroxy tryptophan-induced head-twitches,remarkably enhanced the expression of hippocampus mineralcorticoid receptor and glucocorticoid receptor mRNA,decreased the ratio of mineralcorticoid receptor to glucocorticoid receptor and raised the levels of dopamine,norepinephrine and 5-hydroxytryptamine,while decreasing hydroxyindole acetic acid levels or dihydroxy-phenyl acetic acid in chronic unpredictable stressed rats.Behavioral test results suggested that BCPT potentially had antidepressant-like activity.Meanwhile,BCPT increased the levels of neurotransmitters,and mineralcorticoid receptor and glucocorticoid receptor mRNA in the hippocampus,which may be an important mechanism of its antidepressant effect.

  5. Optimization of ultrasound-assisted extraction of bioactive compounds from wild garlic (Allium ursinum L.).

    Science.gov (United States)

    Tomšik, Alena; Pavlić, Branimir; Vladić, Jelena; Ramić, Milica; Brindza, Ján; Vidović, Senka

    2016-03-01

    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. PMID:26563916

  6. Physicochemical Parameters and Bioactive Compounds of Strawberry Tree (Arbutus unedo L. Honey

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    Pablo A. Ulloa

    2015-01-01

    Full Text Available Botanical origin, physicochemical properties (ash, colour, diastase activity, electrical conductivity (EC, hydroxymethylfurfural (HMF, moisture, optical rotation (OP, pH, reducing sugars, total acidity, total soluble solids, and water activity, bioactive compounds (BC, and antioxidant activity obtained from strawberry tree honey from South Portugal were investigated. Results showed that the pollen analysis and physicochemical parameters were found within to meet international honey specifications. Significant differences (P<0.05 in results of ash content, EC, HMF, OP and colour when were compared with analogous famous Italian honey (Sardinia island. For BC, total phenolic and total flavonoid content were 94.47 mg gallic acid/100 g and 5.33 mg quercetin/100 g, respectively. Concerning Portuguese honey, it was also found that radical scavenging activity (DPPH assay was 43.46% and antioxidant activity was 18.85 mg ascorbic acid equivalent/100 g and 9.92 mg quercetin equivalent/100 g. These results confirmed that Portuguese strawberry tree honey has the highest antioxidant activity, when compared with other kinds of honey. This complete report demonstrates advantages and can help to promote consumption and shown their benefical properties (e.g., antioxidant; which will may increase the commercial value.

  7. Electrostatic extrusion as a dispersion technique for encapsulation of cells and bioactive compounds

    Directory of Open Access Journals (Sweden)

    Kostić Ivana T.

    2012-01-01

    Full Text Available Significant development of cells and bioactive compound encapsulation technologies is taking place due to an exceptional possibility of their application in various scientific disciplines, including biomedicine, pharmacy, cosmetology, food and agricultural sciences, beverage production, industrial waste treatment. Despite the broad application of microencapsulation, the literature reviews on dispersion techniques for microcapsule/microbead production, their advantages, restrictions and drawbacks are scarce. The purpose of this paper is to assess the possibilities of electrostatic extrusion for encapsulation of biological material, including living cells in hydrogel microbeads. The paper presents an overview of the mechanisms of droplet formation and controlling experimental parameters for producing microbeads by means of electrostatic extrusion. Electrostatic droplet formation utilizes a special type of physical process taking advantage of electrostatic effects occurring in flowing conductive liquids after introduction of an electric field.When an electrostatic field is applied to the metal needle and an electric charge is induced in the liquid flowing out of the needle, the size of droplet detaching from the needle tip decreases as a funcion of applied electrostatic field. It has been shown that few parameters affect microbead size: applied voltage, electrode geometry, needle size, polarity arrangement and polymer concentration. The electrostatic droplet formation is one of the most precise methods, which enables one to produce spherical and uniform particles ranging from 100 μm up to 1000 μm. Most of the authors report that the encapsulated compounds (drugs, enzymes and living cells remain unaltered after electrostatic extrusion. This technique seems to be particularly promising in biotechnology, pharmaceutical and cosmetics industries, where a low-temperature process, preserving heat-sensitive material is a prerequisite. Future efforts in

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

    Science.gov (United States)

    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...

  9. Bioactive Compounds Isolated from Lignin of Empty Bunch Palm Fiber and Their Effects on in Vitro Rumen Fermentation

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    M. Prayuwidayati

    2015-12-01

    Full Text Available The objective of this experiment was to study the effects of bioactive compounds isolated from purified lignin formacell (PLF of empty bunch palm fiber as natural antimicrobes and their effects on in vitro rumen fermentation. The first experiment was inhibition test of 11 bioactive compounds isolated from PLF, using disc diffusion method against the growth of Escherichia coli, Salmonella typhimurium, and Staphylococcus aureus. Four of the most potential bioactive compounds were then used in the second experiment, which was an in vitro test using fresh rumen liquid of Ongole grade beef cattle, to study their effects on rumen fermentation. Six treatments with 3 replications were applied in a completely randomized block (CRB design. The treatments were R0= 0.5 g basal diet; R1= R0 + 0.3 mg Rumensin®; R2= R0 + 0.3 mg syringaldehyde; R3= R0 + 0.3 mg p-hydroxybenzoic acid; R4= R0 + 0.3 mg m-hydroxybenzoic acid; and R5= R0 + 0.3 mg oxybenzene. Isolate fraction of CC-2 (syringaldehyde, CC-3 (m-hydroxybenzoic acid, VLC-5 (oxybenzene, and VLC-9 (p-hydroxybenzoic acid exhibited antimicrobes activity against all tested bacteria. Other isolated fractions exhibited antimicrobes activity only against 1 or 2 tested bacteria. The use of syringaldehyde, p-hydroxybenzoic acid, m-hydroxybenzoic acid, and oxybenzene improved ammonia concentration, microbial protein synthesis, and nutrients digestibility. Bioactive compounds had no effect on rumen pH but reduced total VFA concentration as well as the estimate of methane production.

  10. Exploiting natural factors in greenhouses to stimulate plants’ defences and the concentration in bioactive compounds of fruits and vegetables

    OpenAIRE

    Urban, Laurent; Aarrouf, Jawad; Nicot, Philippe

    2012-01-01

    Many secondary metabolites, such as carotenoids, flavonoids, glucosinolates, contribute to the health benefits of fruits and vegetables. It has been repeatedly observed that environmental factors can be used as a powerful lever, besides genetic factors, to increase the concentrations in bioactive compounds of fruits and vegetables. More specifically, it has been observed in a large range of vegetables, including lettuce, pepper, tomato, and strawberry, that high light intensity, red and UV li...

  11. Bioactive Compounds Screening from Zingiberaceae Family as Influenza A/Swine Flu Virus Neuraminidase Inhibitor through Docking Approach

    OpenAIRE

    Tambunan, Usman S. F.; Fadilah; Parikesit, Arli A.

    2010-01-01

    Problem statement: Influenza A/H1N1 is a disease caused by infection of influenza a virus subtype H1N1. It is a major health problem in tropical and subtropical countries. This virus constantly mutates and consequently will be developed into new drug-resistant strains. Approach: In this research, we have conducted docking study to screen bioactive compounds from Zingiberaceae family, which has a role as neuraminidase inhibitor of influenza a virus. Results: The docking res...

  12. Traceability of Functional Bioactive Compounds in Fresh and Pasteurized Milk Obtained from Goats Fed with Orange Pulp

    Directory of Open Access Journals (Sweden)

    Maria Simona Chiş

    2015-11-01

    Full Text Available Traceability is the ability to identify and trace the history, distribution, location, and application of products, parts, and materials. A traceability system records and follows the trail as products, parts, and materials come from suppliers and are processed and ultimately distributed as end products (Prache et al, 2002. In this work, were studied the bioactive compounds (total vitamin C, ascorbic acid, total phenols, flavonoids, carotenoids, vitamin A and vitamin E and antioxidant activity of goat fresh milk and pasteurized one. The goats were fed with a standard diet (control diet and then with a diet that incorporates orange pulp. The control diet (CD corresponded with a standard ration (a ration wich provide the energetic and proteic values, daily food for milking animals. From that ration, the Department of Animal Science, from Politechnic University of Valencia replaced the different proportions of the ingredients for incorporating orange pulp diet (OPD. The results of the present study show that the citrus pulp silage mixture used can be fed to goats without any negative effects on the performance of the animals. Results of this study indicate that citrus pulp silage can replace part of the conventional ration of goats, thus lowering the cost of production. The first aim of this study was to compare the two types of goat diets: a standard diet and a diet with orange pulp, by analyzing the bioactive compounds in fresh and pasteurized milk. The results demonstrate that all the bioactive compounds are bigger in the orange pulp diet than in the control diet. The second objective of this study was to analyze the bioavailability and traceability of bioactive compounds in fresh milk. 

  13. Influence of extraction techniques on antioxidant properties and bioactive compounds of loquat fruit (Eriobotrya japonica Lindl.) skin and pulp extracts

    OpenAIRE

    Delfanian, Mojtaba; Esmaeilzadeh Kenari, Reza; Sahari, Mohammad Ali

    2015-01-01

    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 ass...

  14. Traceability of Functional Bioactive Compounds in Fresh and Pasteurized Milk Obtained from Goats Fed with Orange Pulp

    OpenAIRE

    Maria Simona Chiş; Sevastiţa Muste; Maria Del Mar Camacho Vidal

    2015-01-01

    Traceability is the ability to identify and trace the history, distribution, location, and application of products, parts, and materials. A traceability system records and follows the trail as products, parts, and materials come from suppliers and are processed and ultimately distributed as end products (Prache et al, 2002). In this work, were studied the bioactive compounds (total vitamin C, ascorbic acid, total phenols, flavonoids, carotenoids, vitamin A and vitamin E) and antioxidant activ...

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

    Science.gov (United States)

    Meighani, Hossein; Ghasemnezhad, Mahmood; Bakhshi, Davood

    2015-07-01

    The effect of three different coatings; resin wax (Britex Ti), carnauba wax (Xedasol M14), and chitosan (1 and 2 % w/v) on postharvest quality of pomegranate fruits were investigated. Fruits quality characteristics and bioactive compounds were evaluated during 40, 80 and 120 days storage at 4.5 °C and 3 additional days at 20 °C. The results showed that uncoated fruits showed higher respiration rate, weight loss, L* and b* values of arils, total soluble solids (TSS)/titratable acidity (TA), and pH than coated fruits during storage. Coating treatments could delay declining TSS and TA percent, a* value of arils, as well as bioactive compounds such as total phenolics, flavonoids and anthocyanins content and antioxidant activity. The coated fruits with commercial resin and carnauba waxes showed significantly lower respiration rate and weight loss than other treatments, however carnauba wax could maintain considerably higher fruits quality and bioactive compounds than other coating treatments. The results suggested that postharvest application of carnauba wax have a potential to extend storage life of pomegranate fruits by reducing respiration rate, water loss and maintaining fruit quality. PMID:26139918

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

    Science.gov (United States)

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

    2015-01-01

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

  17. Polyhydroxyalkanoate-based 3-hydroxyoctanoic acid and its derivatives as a platform of bioactive compounds.

    Science.gov (United States)

    Radivojevic, Jelena; Skaro, Sanja; Senerovic, Lidija; Vasiljevic, Branka; Guzik, Maciej; Kenny, Shane T; Maslak, Veselin; Nikodinovic-Runic, Jasmina; O'Connor, Kevin E

    2016-01-01

    A library of 18 different compounds was synthesized starting from (R)-3-hydroxyoctanoic acid which is derived from the bacterial polymer polyhydroxyalkanoate (PHA). Ten derivatives, including halo and unsaturated methyl and benzyl esters, were synthesized and characterized for the first time. Given that (R)-3-hydroxyalkanoic acids are known to have biological activity, the new compounds were evaluated for antimicrobial activity and in vitro antiproliferative effect with mammalian cell lines. The presence of the carboxylic group was essential for the antimicrobial activity, with minimal inhibitory concentrations against a panel of bacteria (Gram-positive and Gram-negative) and fungi (Candida albicans and Microsporum gypseum) in the range 2.8-7.0 mM and 0.1-6.3 mM, respectively. 3-Halogenated octanoic acids exhibited the ability to inhibit C. albicans hyphae formation. In addition, (R)-3-hydroxyoctanoic and (E)-oct-2-enoic acids inhibited quorum sensing-regulated pyocyanin production in the opportunistic pathogen Pseudomonas aeruginosa PAO1. Generally, derivatives did not inhibit mammalian cell proliferation even at 3-mM concentrations, while only (E)-oct-2-enoic and 3-oxooctanoic acid had IC50 values of 1.7 and 1.6 mM with the human lung fibroblast cell line. PMID:26399414

  18. Biochemometrics for Natural Products Research: Comparison of Data Analysis Approaches and Application to Identification of Bioactive Compounds.

    Science.gov (United States)

    Kellogg, Joshua J; Todd, Daniel A; Egan, Joseph M; Raja, Huzefa A; Oberlies, Nicholas H; Kvalheim, Olav M; Cech, Nadja B

    2016-02-26

    A central challenge of natural products research is assigning bioactive compounds from complex mixtures. The gold standard approach to address this challenge, bioassay-guided fractionation, is often biased toward abundant, rather than bioactive, mixture components. This study evaluated the combination of bioassay-guided fractionation with untargeted metabolite profiling to improve active component identification early in the fractionation process. Key to this methodology was statistical modeling of the integrated biological and chemical data sets (biochemometric analysis). Three data analysis approaches for biochemometric analysis were compared, namely, partial least-squares loading vectors, S-plots, and the selectivity ratio. Extracts from the endophytic fungi Alternaria sp. and Pyrenochaeta sp. with antimicrobial activity against Staphylococcus aureus served as test cases. Biochemometric analysis incorporating the selectivity ratio performed best in identifying bioactive ions from these extracts early in the fractionation process, yielding altersetin (3, MIC 0.23 μg/mL) and macrosphelide A (4, MIC 75 μg/mL) as antibacterial constituents from Alternaria sp. and Pyrenochaeta sp., respectively. This study demonstrates the potential of biochemometrics coupled with bioassay-guided fractionation to identify bioactive mixture components. A benefit of this approach is the ability to integrate multiple stages of fractionation and bioassay data into a single analysis. PMID:26841051

  19. Isolation and Characterization of Potential Bioactive Compounds from Landolphia owariensis P. Beauv Stringy Seed Pulp

    Directory of Open Access Journals (Sweden)

    T JN Okonkwo

    2013-06-01

    Full Text Available Summary. Landolphia owariensis P. Beauv, a tropical climber, is economically important for latex/rubber and folklore medicine. Among other uses, it is utilized in the management of malaria and inflammatory related diseases in ethno medicine. Thus its stringy seed pulp (LOSSP was subjected to isolation and characterization of bioactive compounds. A fresh portion of LOSSP was air-dried, pulverized, defatted with petroleum ether and subsequently extracted with acetone and distilled water successively. The acetone extract was fractionated serially into chloroform, ethylacetate and acetone to obtain the respective solvent fractions. LOSSP/CF-1 was obtained by re-crystallization of the chloroform fraction. Phytochemical analysis of the extracts and fractions was performed using standard methods. The chemical structure of LOSSP/CF-1 was elucidated by ultraviolet/visible light, infrared, H-NMR, C-NMR and mass spectroscopic techniques. While the flavonoid concentrate (FC and LOSSP/CF-1 tested positive to 2, 2-diphenylpicryl hydrazyl radical and KMnO4 assays, indicating strong antioxidant properties. In addition, LOSSP/CF-1 expressed a 50% radical inhibition concentration (IC50 of 238.24 ± 3.12 µg/ml against gallic acid (37.63 ± 0.47 µg/ml. Ultraviolet/visible light, infrared, H-NMR, C-NMR spectroscopy and gas chromatography-mass spectrometry of LOSSP/CF-1 indicated it to be ascorbic acid. This is novel for the herb, and the first ever compound isolated and characterized from L. owariensis. Flavonoids and LOSSP/CF-1 (ascorbic acid are potent bioactive principles of L. owariensis, acting via antioxidant mechanism. Thus the herb is recommended for use as an adjuvant in the management of diseases involving pro-oxidative state.   Industrial relevance. Pro-oxidative state-induced disorders like hepatitis, cardiovascular disorders, arthritis, cancer, et c., have been identified as major course of morbidity and mortality throughout the world, especially in

  20. The polyphasic description of a Desmodesmus spp. isolate with the potential of bioactive compounds production

    Directory of Open Access Journals (Sweden)

    El Semary, NA.

    2011-01-01

    Full Text Available A polyphasic approach was applied to describe a colony-forming Desmodesmus species collected from the Nile River, Maadi area, Helwan district, Egypt. The isolate grows best at moderate temperature and relatively high light intensity. The phenotypic features revealed the presence of both unicellular and colonial forms of the isolate and the latter form was either 2-4 celled. Cells were 4-6 mm ± 0.5 at their widest point and 11-15 mm ± 0.48 in their length with spiny projections that encircled the cells. Cells were heavily-granulated and enclosed within common mucilaginous sheath. Colonial forms were developed through production of daughter cells within mother cell. Molecular analysis using 18S rRNA gene showed some similarity to its nearest relative (Desmodesmus communis whereas the phylogenetic analyses clustered it together with other Desmodesmus spp. and away from Scenedesmus spp. from the database. However, the use of ITS-2 as a phylotaxonomic marker proved to be more resolving and confirmed the generic identity of the isolate as Desmodesmus spp. The fatty acid composition revealed the presence of saturated palmitic fatty acid as the most abundant component followed by monounsaturated palmitoleic acid whereas the polyunsaturated fatty acids were in relatively low abundance. The palmitoleic acid in particular is suggested to be involved in active defense mechanism. The phytochemical screening revealed the presence of alkaloids and saponins and absence of tannins. Fractions of methanolic extracts showed antimicrobial activities against pathogenic bacterial strains including multi-drug resistant ones. This study documents the presence of this strain in the River Nile and highlights its biotechnological potential as a source of bioactive compounds.

  1. Design, synthesis, and biological evaluation of a biyouyanagin compound library

    OpenAIRE

    Nicolaou, K. C.; Sanchini, Silvano; Sarlah, David; Lu, Gang; Wu, T. Robert; Nomura, Daniel K.; Cravatt, Benjamin F.; Cubitt, Beatrice; de la Torre, Juan C.; Hessell, Ann J.; Burton, Dennis R.

    2011-01-01

    Modern drug discovery efforts rely, to a large extent, on lead compounds from two classes of small organic molecules; namely, natural products (i.e., secondary metabolites) and designed compounds (i.e., synthetic molecules). In this article, we demonstrate how these two domains of lead compounds can be merged through total synthesis and molecular design of analogs patterned after the targeted natural products, whose promising biological properties provide the motivation. Specifically, the pre...

  2. Bioactive Compounds, Antioxidant, Xanthine Oxidase Inhibitory, Tyrosinase Inhibitory and Anti-Inflammatory Activities of Selected Agro-Industrial By-products

    OpenAIRE

    Ehsan Karimi; Ehsan Oskoueian; Rudi Hendra; Norhani Abdullah

    2011-01-01

    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 f...

  3. Solanum diploconos fruits: profile of bioactive compounds and in vitro antioxidant capacity of different parts of the fruit.

    Science.gov (United States)

    Ribeiro, Alessandra Braga; Chisté, Renan Campos; Lima, José L F C; Fernandes, Eduarda

    2016-05-18

    Solanum diploconos is an unexploited Brazilian native fruit that belongs to the same genus of important food crops, such as tomato (Solanum lycorpersicum) and potato (Solanum tuberosum). In this study, we determined, for the first time, the profile of bioactive compounds (phenolic compounds, carotenoids, ascorbic acid and tocopherols) of the freeze-dried pulp and peel of Solanum diploconos fruits, as well as of an extract obtained from the whole fruit. Additionally, the antioxidant potential of the whole fruit extract was evaluated in vitro, against reactive oxygen species (ROS) and reactive nitrogen species (RNS). Eighteen phenolic compounds were identified in the peel and pulp and 6 compounds were found in the whole fruit extract. Coumaric, ferulic and caffeic acid derivatives were revealed to be the major phenolic constituents. All-trans-β-carotene was the major carotenoid (17-38 μg g(-1), dry basis), but all-trans-lutein and 9-cis-β-carotene were also identified. The peel and pulp presented extract exhibited scavenging capacity against all tested ROS and RNS (IC50 = 14-461 μg mL(-1)) with high antioxidant efficiency against HOCl. Thus, Solanum diploconos fruits may be seen as a promising source of bioactive compounds with high antioxidant potential against the most physiologically relevant ROS and RNS. PMID:27142444

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

    Science.gov (United States)

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

    2015-12-15

    The aim of this study was to characterize grape pomace (GP) from winemaking byproducts of different grape samples (Cabernet Sauvignon-CS; Merlot-ME; Mix composed of 65% Bordeaux, 25% Isabel and 10% BRS Violet-MI and Terci-TE) with a view to exploiting its potential as a source of bioactive compounds and an alternative to the reuse of waste. Bioactive compounds such as individual phenolic compounds and polyunsaturated fatty acids (PUFA) were identified and quantified by spectrophotometric, chromatographic and spectral analyses. The sample of MI had the highest concentrations for total phenolic compounds and total flavonoids, while TE had the highest content for total monomeric anthocyanins. For all samples it was possible to identify 13 different anthocyanins by high performance liquid chromatography (HPLC) and mass spectrometry (MS). Moreover, the GP samples showed phenolic acids; flavan-3-ols such as catechin; flavonols such as quercetin, rutin and kaempferol; and stilbenes such as trans-resveratrol. Therefore, grape pomace can be considered a source for the recovery of phenolic compounds having antioxidant activity as well as a rich source of PUFA. Thus it can be used as an ingredient in the development of new food products, since it is suitable for human consumption, and a viable alternative both to adding nutritional value to food and to reduce environmental contamination. PMID:26590878

  5. The Use of Plant Bioactive Compounds to Mitigate Enteric Methane in Ruminants and its Application in Indonesia

    Directory of Open Access Journals (Sweden)

    Elizabeth Wina

    2012-03-01

    Full Text Available Worldwide, increasing greenhouse gas (GHG emissions have become a major concern as they are now considered to be the cause of global warming. Several strategies have been planned and taken by different countries including Indonesia to mitigate this situation. Agriculture is considered to be one of major contributors to GHG, especially methane coming from ruminant digestive processes. More than 85% of the methane produced by ruminants comes from enteric fermentation. Several options have been proposed to lower this enteric methane production. This paper describes a review on diet manipulation using feed additives, especially plant bioactive compounds, to mitigate the GHG emission from ruminant livestock. Plant bioactive compounds have been found with various chemical structures. Some of them such as saponin, tannin, essential oils, organosulphur compounds, have been reported to have ability to reduce enteric methane production. Indonesia has many plant resources that have potential as methane reducing agents. Sapindus rarak fruit especially its methanol extract contain saponins which reduce the activity of methanogens in the rumen in vitro, hence reduce methane production (11%. Feeding S. rarak to sheep increased daily weight gain but not that of local cattle. Shrub legumes such as Calliandra calothyrsus and Leucaena leucocephala contain tannins which can reduce methanogenesis (3 – 21% methane reduction. Besides tannin, these shrub legumes are a good source of protein. Feeding shrub legumes can be beneficial as a protein source and a methane reducer. Other sources of methane reducing agents have been tested in other countries and some can be applied for Indonesian situation. The strategy to reduce methane by plant bioactive compounds should be developed to be simple and relatively cheap so it will benefit the local farmers. Extraction of these compounds may be expensive, therefore, costs should be considered carefully when proposing to use the

  6. Investigation of the incidence of "undesirable" molecular moieties for high-throughput screening compound libraries in marketed drug compounds.

    Science.gov (United States)

    Axerio-Cilies, Peter; Castañeda, Ivan P; Mirza, Amin; Reynisson, Jóhannes

    2009-03-01

    A database of 1070 marketed drug compounds was compiled and analyzed in order to assess the occurrence of moieties described in the literature as "undesirable" for high-throughput screening compound libraries due to their ability to perturb assay formats. The study revealed a total of 277 compounds, 26% of the database, contained at least one of the moieties. As some of the drug compounds contained more than one "undesirable" moiety, the total number was 352. Electrophilic reactive groups, particularly aliphatic esters, were the most abundant type with 55% of the total. Half of the drug compounds incorporating the "undesirable" moieties were synthetic organic molecules. These findings suggest that "undesirable" moieties do not pose a major hindrance during clinical trials, the most expensive phase of drug development. In addition, their early elimination in the preclinical stage excludes large regions of known drug space due to the reliance on biochemical and cell-based assays. In general, it can be concluded that compounds with "undesirable" moieties should not simply be eliminated from compound screening libraries but rather be flagged as potentially problematic. A possible solution is to segregate the compounds containing suspect moieties and screen them when deemed appropriate. PMID:18692938

  7. Prediction of solubilities for ginger bioactive compounds in hot water by the COSMO-RS method

    International Nuclear Information System (INIS)

    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.

  8. Direct Comparison of Linear and Macrocyclic Compound Libraries as a Source of Protein Ligands

    Science.gov (United States)

    2015-01-01

    There has been much discussion of the potential desirability of macrocyclic molecules for the development of tool compounds and drug leads. But there is little experimental data comparing otherwise equivalent macrocyclic and linear compound libraries as a source of protein ligands. In this Letter, we probe this point in the context of peptoid libraries. Bead-displayed libraries of macrocyclic and linear peptoids containing four variable positions and 0–2 fixed residues, to vary the ring size, were screened against streptavidin and the affinity of every hit for the target was measured. The data show that macrocyclization is advantageous, but only when the ring contains 17 atoms, not 20 or 23 atoms. This technology will be useful for conducting direct comparisons between many different types of chemical libraries to determine their relative utility as a source of protein ligands. PMID:25623285

  9. Bioactive Compounds of Cold-pressed Thyme (Thymus vulgaris) Oil with Antioxidant and Antimicrobial Properties.

    Science.gov (United States)

    Assiri, Adel M A; Elbanna, Khaled; Abulreesh, Hussein H; Ramadan, Mohamed Fawzy

    2016-01-01

    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

  10. Evaluation of Bioactive Compounds, Pharmaceutical Quality, and Anticancer Activity of Curry Leaf (Murraya koenigii L.

    Directory of Open Access Journals (Sweden)

    Ali Ghasemzadeh

    2014-01-01

    Full Text Available 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.

  11. GC-MS and NMR analysis of the bioactive compounds from the crude extracts of Waltheria indica and the histopathological changes induced in albino rats challenged with Naja nigricollis venom

    Directory of Open Access Journals (Sweden)

    Philip Ilani

    2016-05-01

    Full Text Available Objective: To develop a characteristic fingerprint of the different chemical compounds of plant by gas chromatography-mass spectrometer (GC-MS and nuclear magnetic resonance (NMR analysis and assess the effect of the crude extract on histological changes induced in Naja nigricollis (N. nigricollis envenomed albino rats. Methods: The coarsely powdered Waltheria indica (W. indica whole plant material was extracted using 70% methanol. GC-MS analysis was carried out using a Shimadzu GC-MS QP 2010 plus system of gas chromatography interfaced to a mass spectrometer. The identification of components was based on National Institute of Standard and Technology-08 and Willey-8 libraries. Hydrogen-NMR spectra of the extracts was performed using Bruker Biospin Avance 400-MHz NMR spectrophotometer with a 5 mm broad inverse probe head, equipped with shielded z-gradient accessories and C-13 NMR hetero-nuclear single quantum correction was carried out using the Brucker’s standard pulse library. The efficacy of the crude extract of W. indica whole plant was tested and the lesions induced in the liver, brain and kidney of albino rats challenged with N. nigricollis were analyzed by light microscopy. Results: The identification of the bioactive compounds from W. indica by GC-MS analysis revealed 41 peaks. A total of 38 compounds were identified with majority having important pharmacological activities that included anti-microbial, anti-cancer, anti-oxidant antiinflammatory, anti-allergenic, anti-ageing, anti-arthritic, larvicidal, anti-convulsant and herbicidal activities. C-13 and hydrogen-NMR analysis of W. indica elucidated key bioactive compounds in the whole plant that were consistent with the classes of bioactive compounds detected by GC-MS analysis. The efficacy of the crude extract of W. indica whole plant in ameliorating histopathological lesions induced in the liver, brain and kidney of albino rats challenged with N. nigricollis venom revealed the

  12. GC-MS and NMR analysis of the bioactive compounds from the crude extracts ofWaltheria indica and the histopathological changes induced in albino rats challenged withNaja nigricollis venom

    Institute of Scientific and Technical Information of China (English)

    Philip Ilani; Nicholas Ajodo; Folashade Adewusi; Samirat Yakubu; Victor Yakubu Cosmos; Ache Eunice; Atonila Kayode Ezekiel; Oshiedu Sarah; Emmanuel Amlabu

    2016-01-01

    Objective:To develop a characteristic fingerprint of the different chemical compounds of plant by gas chromatography-mass spectrometer (GC-MS) and nuclear magnetic resonance (NMR) analysis and assess the effect of the crude extract on histological changes induced inNaja nigricollis(N. nigricollis)envenomed albino rats. Methods: The coarsely powderedWaltheria indica (W. indica) whole plant material was extracted using 70% methanol.GC-MS analysis was carried out using a ShimadzuGC-MS QP 2010 plus system of gas chromatography interfaced to a mass spectrometer. The identification of components was based on National Institute of Standard and Technology-08 and Willey-8 libraries. Hydrogen-NMR spectra of the extracts was performed using Bruker Biospin Avance 400-MHzNMR spectrophotometer with a 5 mm broad inverse probe head, equipped with shielded z-gradient accessories andC-13 NMR hetero-nuclear single quantum correction was carried out using the Brucker’s standard pulse library. The efficacy of the crude extract ofW. indica whole plant was tested and the lesions induced in the liver, brain and kidney of albino rats challenged withN. nigricollis were analyzed by light microscopy. Results:The identification of the bioactive compounds fromW. indica byGC-MS analysis revealed 41 peaks. A total of 38 compounds were identified with majority having important pharmacological activities that included anti-microbial, anti-cancer, anti-oxidant anti-inflammatory, anti-allergenic, anti-ageing, anti-arthritic, larvicidal, anti-convulsant and herbicidal activities.C-13 and hydrogen-NMR analysis ofW. indica elucidated key bioactive compounds in the whole plant that were consistent with the classes of bioactive compounds detected byGC-MS analysis. The efficacy of the crude extract ofW. indica whole plant in ameliorating histopathological lesions induced in the liver, brain and kidney of albino rats challenged withN. nigricollis venom revealed the abrogation of tissue degeneration when

  13. UVA I-protection effectiveness of bioactive compound and organic UV filters: an in vitro assessment

    Directory of Open Access Journals (Sweden)

    André Rolim Baby

    2009-01-01

    Full Text Available This research work aimed at determining the UVA effectiveness (UVA I/UV ratio, by diffuse transmittance analysis, of sunscreens developed with a bioactive substance, the rutin, associating or not with organic UVB-UVA filters incorporated at a phosphate-base O/W emulsion. Sunscreens provided conflicting and unpredictable results concerning the anti-UVA protection, specially, at the UVA I region. Possible interactions among the organic UV filters and the polyphenolic bioactive substance may have accounted with improvement or reduction of UV protection by a complex and not yet elucidated mechanism, probably regarding wavelength delocalization to superior or inferior values, by resonant molecule stabilization or destabilization.

  14. Discovery Strategies of Bioactive Compounds Synthesized by Nonribosomal Peptide Synthetases and Type-I Polyketide Synthases Derived from Marine Microbiomes

    Science.gov (United States)

    Amoutzias, Grigoris D.; Chaliotis, Anargyros; Mossialos, Dimitris

    2016-01-01

    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

  15. Discovery Strategies of Bioactive Compounds Synthesized by Nonribosomal Peptide Synthetases and Type-I Polyketide Synthases Derived from Marine Microbiomes

    Directory of Open Access Journals (Sweden)

    Grigoris D. Amoutzias

    2016-04-01

    Full Text Available 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.

  16. Discovery Strategies of Bioactive Compounds Synthesized by Nonribosomal Peptide Synthetases and Type-I Polyketide Synthases Derived from Marine Microbiomes.

    Science.gov (United States)

    Amoutzias, Grigoris D; Chaliotis, Anargyros; Mossialos, Dimitris

    2016-04-01

    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

  17. Laser alloying of Ti–Si compound coating on Ti–6Al–4V alloy for the improvement of bioactivity

    Energy Technology Data Exchange (ETDEWEB)

    Wu, Y. [State Key Laboratory of Material Processing and Die and Mould Technology, School of Materials Science and Engineering, Huazhong University of Science and Technology, Wuhan 430074 (China); The State Key Laboratory Breeding Base of Basic Science of Stomatology (Hubei-MOST) and Key Laboratory of Oral Biomedicine Ministry of Education, Wuhan University, Wuhan 430079 (China); Wang, A.H., E-mail: ahwang@mail.hust.edu.cn [State Key Laboratory of Material Processing and Die and Mould Technology, School of Materials Science and Engineering, Huazhong University of Science and Technology, Wuhan 430074 (China); Zhang, Z.; Zheng, R.R. [State Key Laboratory of Material Processing and Die and Mould Technology, School of Materials Science and Engineering, Huazhong University of Science and Technology, Wuhan 430074 (China); Xia, H.B.; Wang, Y.N. [The State Key Laboratory Breeding Base of Basic Science of Stomatology (Hubei-MOST) and Key Laboratory of Oral Biomedicine Ministry of Education, Wuhan University, Wuhan 430079 (China)

    2014-06-01

    Laser alloying of Ti–Si compound coating on Ti–6Al–4V alloy is carried out by a pulsed Nd:YAG laser. The corresponding microstructure, phase structure, microhardness profiles, corrosion properties and bioactivity of the laser-alloyed coatings are investigated to optimize the atomic ratio of Ti–Si. The laser alloyed Ti–Si compound coatings are free of cracks, and primarily present block-like crystals, lath-like crystals and dendrite crystals. The phase structures of both laser-alloyed Ti + Si and 5Ti + 3Si coatings are mainly consisted of α-Ti and Ti{sub 5}Si{sub 3}, while the laser-alloyed Si coating is mainly consisted of TiSi{sub 2} and Ti{sub 5}Si{sub 3}. Microhardness test indicates that the laser-alloyed Si coating has the highest microhardness. Also, corrosion resistance measurement reveals that the corrosion resistance of the laser-alloyed Si coating is much better than that of the Ti–6Al–4V alloy. Evaluation of bioactivity shows that cell growth on the laser-alloyed Si coating with high volume fraction of Ti–Si compounds is faster than that of the Ti–6Al–4V alloy.

  18. Screening of minor bioactive compounds from herbal medicines by in silico docking and the trace peak exposure methods.

    Science.gov (United States)

    Wu, Bin; Song, Hui-Peng; Zhou, Xu; Liu, Xin-Guang; Gao, Wen; Dong, Xin; Li, Hui-Jun; Li, Ping; Yang, Hua

    2016-03-01

    Screening of high potent enzyme inhibitors from herbal medicines is always lacking of efficiency due to the complexity of chemicals. The constituents responsible for the holistic effect may be trace-level chemicals, but these chemicals were covered by highly abundant compositions. To challenge this bottleneck, a strategy for screening minor bioactive compounds was proposed. It generally included four steps, (1) preliminarily find the enzyme binders by ultrafiltration; (2) optimise and predict the potential inhibitors by docking analysis; (3) selectively identify and prepare trace compounds by segment and exposure approach; (4) validate the activity and summarize the structure-activity relationship. As a case study, α-glucosidase (AGH) and Ginkgo biloba extract were used as the experimental materials. By comprehensive screening, 11 trace flavones were screened out and identified as strong AGH inhibitors. Among them, AGH inhibitory activities of syringetin and sciadopitysin were reported for the first time. Their IC50 values were 36.80 and 8.29μM, respectively, which were lower than that of a positive control acarbose. In addition, the AGH inhibitory activities of the flavonoids could be ranked, based on a decreased order, as biflavone, flavone, flavone glycoside, flavone biglycoside. The strategy is expected to be practical and useful for screening bioactive molecules from herbal medicines, especially for the minor compounds, which will definitely accelerate the discovery of new drug candidates. PMID:26852619

  19. Laser alloying of Ti–Si compound coating on Ti–6Al–4V alloy for the improvement of bioactivity

    International Nuclear Information System (INIS)

    Laser alloying of Ti–Si compound coating on Ti–6Al–4V alloy is carried out by a pulsed Nd:YAG laser. The corresponding microstructure, phase structure, microhardness profiles, corrosion properties and bioactivity of the laser-alloyed coatings are investigated to optimize the atomic ratio of Ti–Si. The laser alloyed Ti–Si compound coatings are free of cracks, and primarily present block-like crystals, lath-like crystals and dendrite crystals. The phase structures of both laser-alloyed Ti + Si and 5Ti + 3Si coatings are mainly consisted of α-Ti and Ti5Si3, while the laser-alloyed Si coating is mainly consisted of TiSi2 and Ti5Si3. Microhardness test indicates that the laser-alloyed Si coating has the highest microhardness. Also, corrosion resistance measurement reveals that the corrosion resistance of the laser-alloyed Si coating is much better than that of the Ti–6Al–4V alloy. Evaluation of bioactivity shows that cell growth on the laser-alloyed Si coating with high volume fraction of Ti–Si compounds is faster than that of the Ti–6Al–4V alloy.

  20. Optimized Solid Phase-Assisted Synthesis of Dendrons Applicable as Scaffolds for Radiolabeled Bioactive Multivalent Compounds Intended for Molecular Imaging

    Directory of Open Access Journals (Sweden)

    Gabriel Fischer

    2014-05-01

    Full Text Available Dendritic structures, being highly homogeneous and symmetric, represent ideal scaffolds for the multimerization of bioactive molecules and thus enable the synthesis of compounds of high valency which are e.g., applicable in radiolabeled form as multivalent radiotracers for in vivo imaging. As the commonly applied solution phase synthesis of dendritic scaffolds is cumbersome and time-consuming, a synthesis strategy was developed that allows for the efficient assembly of acid amide bond-based highly modular dendrons on solid support via standard Fmoc solid phase peptide synthesis protocols. The obtained dendritic structures comprised up to 16 maleimide functionalities and were derivatized on solid support with the chelating agent DOTA. The functionalized dendrons furthermore could be efficiently reacted with structurally variable model thiol-bearing bioactive molecules via click chemistry and finally radiolabeled with 68Ga. Thus, this solid phase-assisted dendron synthesis approach enables the fast and straightforward assembly of bioactive multivalent constructs for example applicable as radiotracers for in vivo imaging with Positron Emission Tomography (PET.

  1. Detection of Bioactive Compounds in the Mucus Nets of Dendropoma maxima, Sowerby 1825 (Prosobranch Gastropod Vermetidae, Mollusca

    Directory of Open Access Journals (Sweden)

    Anne Klöppel

    2013-01-01

    Full Text Available The sessile suspension-feeding wormsnail Dendropoma maxima, Sowerby 1825 (Vermetidae secretes a mucus net to capture planktonic prey. The nets are spread out over the corals and often have remarkable deleterious effects on them like changes in growth form and pigmentation shifts not uncommonly resulting in tissue necrosis. Until now, there is no explanation for this phenomenon although the indication as well as theories about its genesis is mentioned in several publications. Vermetids are well studied concerning the intraspecific competition with neighboring individuals but not in their interaction with other taxa like corals or fish. We did extensive in situ video recording and observed that fish avoided the plankton-load nets although several specialized taxa are known to be molluscivores, mucivores, and/or feed on plankton. As many molluscs use chemical weapons to combat feeding pressure and to defend themselves against predators, we screened empty and plankton-load mucus nets for potential bioactive metabolites. Bioactivity testing was performed with a recently developed system based on a chromatographic separation (high-performance thin-layer chromatography (HPTLC and a bioassay with luminescent bacteria Vibrio fischeri. Thus, we found at least two active compounds exclusively accumulated by the wormsnails themselves. This is the first record of bioactive properties in the whole family of Vermetidae.

  2. Rescuing compound bioactivity in a secondary cell-based screening by using γ-cyclodextrin as a molecular carrier

    Science.gov (United States)

    Claveria-Gimeno, Rafael; Vega, Sonia; Grazu, Valeria; de la Fuente, Jesús M; Lanas, Angel; Velazquez-Campoy, Adrian; Abian, Olga

    2015-01-01

    In vitro primary screening for identifying bioactive compounds (inhibitors, activators or pharmacological chaperones) against a protein target results in the discovery of lead compounds that must be tested in cell-based efficacy secondary screenings. Very often lead compounds do not succeed because of an apparent low potency in cell assays, despite an excellent performance in primary screening. Primary and secondary screenings differ significantly according to the conditions and challenges the compounds must overcome in order to interact with their intended target. Cellular internalization and intracellular metabolism are some of the difficulties the compounds must confront and different strategies can be envisaged for minimizing that problem. Using a novel screening procedure we have identified 15 compounds inhibiting the hepatitis C NS3 protease in an allosteric fashion. After characterizing biophysically the interaction with the target, some of the compounds were not able to inhibit viral replication in cell assays. In order to overcome this obstacle and potentially improve cellular internalization three of these compounds were complexed with γ-cyclodextrin. Two of them showed a five- and 16-fold activity increase, compared to their activity when delivered as free compounds in solution (while γ-cyclodextrin did not show antiviral activity by itself). The most remarkable result came from a third compound that showed no antiviral activity in cell assays when delivered free in solution, but its γ-cyclodextrin complex exhibited a 50% effective concentration of 5 μM. Thus, the antiviral activity of these compounds can be significantly improved, even completely rescued, using γ-cyclodextrin as carrier molecule. PMID:25834436

  3. Effects of selected bioactive food compounds on human white adipocyte function

    DEFF Research Database (Denmark)

    Björk, Christel; Wilhelm, Uta; Mandrup, Susanne;

    2016-01-01

    bioactive nutrients on fat metabolism, we investigated their role on human white adipocyte function. METHODS: The influence of the omega-3-fatty acid docosahexaenoic acid (DHA), the anthocyanin (AC) cyanidin-3-glucoside and its metabolite protocatechuic acid, and the beta-glucan metabolite propionic acid...

  4. Study of bioactive compounds in spices (Syzygium aromaticum L, Cinnamomum zeylanicum Blume and Myristica fragrans Houtt) processed by ionizing radiation

    International Nuclear Information System (INIS)

    Spices and aromatic herbs are divided into leaves, flowers, bud, seeds bark or dry roots from different plants and it is possible to define them as products of highly flavored vegetal origin that volatize easily when incorporated in small quantities to food products and contribute to its aroma, flavor, color or even to its preservation. Nowadays, people look for its functional properties, bioactive compounds and sensory qualities. A big problem is the reduction of the quantity of these compounds throughout the production chain from the harvest process, storage and distribution. For a long time researchers and industries have concentrated on perfecting the processes of the production chain seeking to guarantee the sanitary and food safety, preserving foodstuffs for a long period and an increase in its lifespan without drastically altering its properties. Due to homemade products and the lack of compliance with good practices in its production chain, the spices can contain a high amount of microbiology causing serious complications to the health of the consumer and the radiation processing is often used for reduce these problems. With this finding, the objectives of this work were: Analyze the oil antifungal properties of spices irradiated with average doses (2.5; 5; 7.5 and 10 kGy); Study the average doses (5 and 10 kGy) and high dose (20 and 30 kGy) effects of gamma radiation 60Co in the bioactive compounds of the spices - cloves, cinnamon and nutmeg; Identify the oils compounds; Identify the volatile compounds in the headspace of the oils and the in natura spices. Identify the compounds of the nonvolatile part of the nutmeg; Identify the chiral compounds of the cinnamon. Comparing the control samples (not irradiated) with the processed at the described doses, regarding the oil antifungal properties it was possible to verify the efficiency and later that the irradiation did not interfered in its efficiency; Regarding to the others tests in this work, the compounds

  5. Effective properties of a sturgeon-based bioactive compound on stress-induced hippocampal degeneration and on in vitro neurogenesis.

    Science.gov (United States)

    Marotta, F; Chui, D H; Yadav, H; Lorenzetti, A; Celep, G; Jain, S; Bomba, A; Polimeni, A; Zhong, K; Allegri, F

    2012-01-01

    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. PMID:23034252

  6. Evaluation of the potential of squash pumpkin by-products (seeds and shell) as sources of antioxidant and bioactive compounds.

    Science.gov (United States)

    Saavedra, M J; Aires, A; Dias, C; Almeida, J A; De Vasconcelos, M C B M; Santos, P; Rosa, E A

    2015-02-01

    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. PMID:25694712

  7. Antifouling effect of bioactive compounds from selected marine organisms in the Obhur Creek, Red Sea

    Science.gov (United States)

    Al-Sofyani, Abdulmohsin; Marimuthu, N.; Wilson, J. Jerald; Pugazhendi, Arulazhagan; Dhavamani, Jeyakumar

    2016-06-01

    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.

  8. Using immobilized G-protein coupled receptors to screen bioactive traditional Chinese medicine compounds with multiple targets.

    Science.gov (United States)

    Zhao, Xinfeng; Li, Qian; Bian, Liujiao; Zheng, Xiaohui; Zheng, Jianbin; Zhang, Youyi; Li, Zijian

    2012-11-01

    Demand on high-throughput methods for multi-target compounds screening continues to increase nowadays due to the decline of new drugs on the market. Two kinds of G-protein-coupled receptors, alpha1-adrenoceptor (α(1A)-AR) and beta2-adrenoceptor (β(2)-AR), were purified and immobilized on the surface of macroporous silica gel to prepare new chromatographic stationary phases. Control drugs (e.g., prazosin, terazosin, salbutamol, and terbutaline) were used to characterize the retention behavior of the obtained α(1A)-AR and β(2)-AR columns. This study also coupled both columns with a six-way switching valve to construct an automatic two-dimensional system for multi-target compounds screening in complex mixtures. Adrenaline hydrochloride was used as a representative drug to evaluate the chromatographic performance of the two dimensional system. The aqueous extracts from Salvia miltiorrhiza and Coptis chinensis were also analyzed by the automatic system. The compounds in S. miltiorrhiza had no binding to both α(1A)-AR and β(2)-AR columns. But berberine, palmatine and jatrorrhizine were screened as the bioactive compounds in C. chinensis, targeting both the receptors. The proposed method is an alternative for recognizing and separating the compounds targeting different proteins from a complex matrix. PMID:22651959

  9. Synthesis and bioactive evaluations of novel benzotriazole compounds as potential antimicrobial agents and the interaction with calf thymus DNA

    Indian Academy of Sciences (India)

    Yu Ren; Hui Zhen Zhang; Shao Lin Zhang; Yun Lei Luo; Ling Zhang; Cheng He Zhou; Rong Xia Geng

    2015-12-01

    A novel series of benzotriazole derivatives were synthesized and characterized by NMR, IR and MS spectra. The bioactive assay manifested that most of the new compounds exhibited moderate to good antibacterial and antifungal activities against the tested strains in comparison to reference drugs chloromycin, norfloxacin and fluconazole. Especially, 2,4-dichlorophenyl substituted benzotriazole derivative 6f displayed good antibacterial activity against MRSA with MIC value of 4 g/mL, which was 2-fold more potent than Chloromycin, and it also displayed 3-fold stronger antifungal activity (MIC = 4 g/mL) than fluconazole (MIC = 16 g/mL) against Beer yeast. The preliminary interactive investigations of compound 6f with calf thymus DNA revealed that compound 6f could effectively intercalate into DNA to form compound 6f–DNA complex which might block DNA replication to exert antimicrobial activities. Molecular docking experiments suggested that compound 6f projected into base-pairs of DNA hexamer duplex forming two hydrogen bonds with guanine of DNA. The theoretical calculations were in accordance with the experimental results.

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

    Science.gov (United States)

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

    2016-11-15

    Garlic (Allium sativum L.) is considered one of the twenty most important vegetables, with various uses throughout the world, either as a raw vegetable for culinary purposes, or as an ingredient of traditional and modern medicine. Furthermore, it has also been proposed as one of the richest sources of total phenolic compounds, among the usually consumed vegetables, and has been highly ranked regarding its contribution of phenolic compounds to human diet. This review aims to examine all the aspects related with garlic chemical composition and quality, focusing on its bioactive properties. A particular emphasis is given on the organosulfur compounds content, since they highly contribute to the effective bioactive properties of garlic, including its derived products. The important effects of pre-harvest (genotype and various cultivation practices) and post-harvest conditions (storage conditions and processing treatments) on chemical composition and, consequently, bioactive potency of garlic are also discussed. PMID:27283605

  11. Nonlinear dimensionality reduction and mapping of compound libraries for drug discovery.

    Science.gov (United States)

    Reutlinger, Michael; Schneider, Gisbert

    2012-04-01

    Visualization of 'chemical space' and compound distributions has received much attraction by medicinal chemists as it may help to intuitively comprehend pharmaceutically relevant molecular features. It has been realized that for meaningful feature extraction from complex multivariate chemical data, such as compound libraries represented by many molecular descriptors, nonlinear projection techniques are required. Recent advances in machine-learning and artificial intelligence have resulted in a transfer of such methods to chemistry. We provide an overview of prominent visualization methods based on nonlinear dimensionality reduction, and highlight applications in drug discovery. Emphasis is on neural network techniques, kernel methods and stochastic embedding approaches, which have been successfully used for ligand-based virtual screening, SAR landscape analysis, combinatorial library design, and screening compound selection. PMID:22326864

  12. Bioactivity of essential oil of Artemisia argyi Lévl. et Van. and its main compounds against Lasioderma serricorne.

    Science.gov (United States)

    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

    2014-01-01

    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. PMID:25017866

  13. Isolation of bioactive biphenyl compounds from the twigs of Chaenomeles sinensis.

    Science.gov (United States)

    Kim, Chung Sub; Subedi, Lalita; Kwon, Oh Kil; Kim, Sun Yeou; Yeo, Eui-Ju; Choi, Sang Un; Lee, Kang Ro

    2016-01-15

    Investigation of the MeOH extract of Chaenomeles sinensis twigs resulted in the isolation of seven biphenyl compounds (1-7) including a new compound, chaenomin (1). The chemical structures of the isolated compounds were elucidated by extensive NMR data ((1)H and (13)C NMR, (1)H-(1)H COSY, HSQC and HMBC), specific optical rotation, and chemical reaction. Compounds 2 and 6 showed potent cytotoxic activities against four cancer cell lines (A549, SK-OV-3, SK-MEL-2, and HCT15), and compound 7 exhibited potent anti-neuroinflammatory and NGF-potentiating activity. PMID:26706168

  14. In Vitro evaluation of antifungal activity of Bioactive Compound 2H-FURO [2,3-H]-1-Benzopyran-2-one against seed borne fungi of maize

    Directory of Open Access Journals (Sweden)

    B. Kiran

    2012-03-01

    Full Text Available Antifungal activity of bioactive compound 2HFuro[ 2,3-H]-1-benzopyran-2-one recorded a significant activity at 100-1000 ppm concentration against all the ten Aspergillus species tested. A. flavus recorded complete inhibition at 100 ppm concentration, A. niger at 500 ppm, A. fumigates at 600 ppm, A. flavus oryzae and A. flavus columnaris at 700 ppm respectively. A. ochraceous and A. flavipes recorded complete inhibition at 900 ppm concentration. Compared to synthetic fungicide Captan and Thiram at 2000ppm concentration. Minimum Inhibitory Concentration (MIC of bioactive compound was in the range of 100- 900ppm concentration against all the test fungi.

  15. Stability and metabolism of Arbutus unedo bioactive compounds (phenolics and antioxidants) under in vitro digestion and colonic fermentation.

    Science.gov (United States)

    Mosele, Juana I; Macià, Alba; Romero, Mari-Paz; Motilva, María-José

    2016-06-15

    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. PMID:26868556

  16. Fruit quality and bioactive compounds relevant to human health of sweet cherry (Prunus avium L.) cultivars grown in Italy.

    Science.gov (United States)

    Ballistreri, Gabriele; Continella, Alberto; Gentile, Alessandra; Amenta, Margherita; Fabroni, Simona; Rapisarda, Paolo

    2013-10-15

    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. PMID:23692746

  17. Impact of molecular weight on the formation of electrosprayed chitosan microcapsules as delivery vehicles for bioactive compounds.

    Science.gov (United States)

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

    2016-10-01

    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. PMID:27312621

  18. Screening of marine seaweeds for bioactive compound against fish pathogenic bacteria and active fraction analysed by gas chromatography– mass spectrometry

    Directory of Open Access Journals (Sweden)

    Rajasekar Thirunavukkarasu

    2014-05-01

    Full Text Available Objective: To isolate bioactive molecules from marine seaweeds and check the antimicrobial activity against the fish pathogenic bacteria. Methods: Fresh marine seaweeds Gracilaria edulis, Kappaphycus spicifera, Sargassum wightii (S. wightii were collected. Each seaweed was extracted with different solvents. In the study, test pathogens were collected from microbial type culture collection. Antibacterial activity was carried out by using disc diffusion method and minimum inhibition concentration (MIC was calculated. Best seaweed was analysed by fourier transform infrared spectroscopy. The cured extract was separated by thin layer chromatography (TLC. Fraction was collected from TLC to check the antimicrobial activity. Best fraction was analysed by gas chromatography mass spectrometer (GCMS. Results: Based on the disc diffusion method, S. wightii showed a better antimicrobial activity than other seaweed extracts. Based on the MIC, methanol extract of S. wightii showed lower MIC than other solvents. S. wightii were separated by TLC. In this TLC, plate showed a two fraction. These two fractions were separated in preparative TLC and checked for their antimicrobial activity. Fraction 2 showed best MIC value against the tested pathogen. Fraction 2 was analysed by GCMS. Based on the GCMS, fraction 2 contains n-hexadecanoic acid (59.44%. Conclusions: From this present study, it can be concluded that S. wightii was potential sources of bioactive compounds.

  19. Juglans regia L. leaves as a source of bioactive phenolic compounds

    OpenAIRE

    André SANTOS; Barros, Lillian; Dueñas, Montserrat; Carvalho, Ana Maria; Santos-Buelga, Celestino; Ferreira, Isabel C. F. R.

    2013-01-01

    Walnut (Juglans regia L.) leaves are considered a source of healthcare compounds, and have been widely used in traditional medicine for treatment of skin inflammations, hyperhidrosis and ulcers and for its antidiarrheic, anti-helmintic, antiseptic and astringent properties [1]. Furthermore, they have been reported as a source of phenolic compounds [2,3].The beneficial effects derived from those compounds with interesting properties, such as anticarcinogenic, antimutagenic and c...

  20. Evaluation of antibacterial activity of bioactive compounds obtained from the seaweed Chondrococcus hornemanni on ichthyopathogenic bacteria affecting marine ornamental fish

    Institute of Scientific and Technical Information of China (English)

    Raghunathan Ganeshamurthy; Kapila Tissera

    2013-01-01

    Objective: To investigate antibacterial effects of extracts from the seaweed Chondrococcushornemanni (C. hornemanni) on bacterial pathogens of marine ornamental fish. Method: Methanol extract obtained from C. hornemanni showed a broad and high antibacterial activity against four fish pathogens including Providencia rettgeri, Aeromonas hydrophila, Vibrioalginoticus and Vibrio parahaemolyticus. The crude extract obtained from the dried seaweeds was fractionated and purified using column chromatography. Purified extracts were analyzed with Fourier transform infrared spectroscopy (FTIR) for identifying the functional groups. Phytoconstituents of the active fraction were further identified by means of gas chromatography and mass spectrometric (GC-MS) analysis. Result: The first fraction of the extracts showed effective inhibitory activity against Aeromonashydrophila and Vibrio parahaemolyticus at a concentration of 100 µL. However, Vibrio alginolyticus and Providencia rettgeri had shown a moderately lesser inhibitory response to the extract.Conclusion:Hence, it is concluded that extracts of seaweed C. hornemanni, contain potential bioactive compounds with a considerable antibiotic activity.

  1. Evaluation of antibacterial activity of bioactive compounds obtained from the seaweed Chondrococcus hornemanni on ichthyopathogenic bacteria affecting marine ornamental fish

    Directory of Open Access Journals (Sweden)

    Raghunathan Ganeshamurthy

    2013-08-01

    Full Text Available Objective: To investigate antibacterial effects of extracts from the seaweed Chondrococcus hornemanni (C. hornemanni on bacterial pathogens of marine ornamental fish. Method: Methanol extract obtained from C. hornemanni showed a broad and high antibacterial activity against four fish pathogens including Providencia rettgeri, Aeromonas hydrophila, Vibrio alginoticus and Vibrio parahaemolyticus. The crude extract obtained from the dried seaweeds was fractionated and purified using column chromatography. Purified extracts were analyzed with Fourier transform infrared spectroscopy (FTIR for identifying the functional groups. Phytoconstituents of the active fraction were further identified by means of gas chromatography and mass spectrometric (GC-MS analysis. Result: The first fraction of the extracts showed effective inhibitory activity against Aeromonas hydrophila and Vibrio parahaemolyticus at a concentration of 100 µL. However, Vibrio alginolyticus and Providencia rettgeri had shown a moderately lesser inhibitory response to the extract. Conclusion: Hence, it is concluded that extracts of seaweed C. hornemanni, contain potential bioactive compounds with a considerable antibiotic activity.

  2. An Alternative Use of Horticultural Crops: Stressed Plants as Biofactories of Bioactive Phenolic Compounds

    OpenAIRE

    Luis Cisneros-Zevallos; Daniel A. Jacobo-Velázquez

    2012-01-01

    Plants subjected to abiotic stresses synthesize secondary metabolites with potential application in the functional foods, dietary supplements, pharmaceutical, cosmetics and agrochemical markets. This approach can be extended to horticultural crops. This review describes previous reports regarding the effect of different postharvest abiotic stresses on the accumulation of phenolic compounds. Likewise, the physiological basis for the biosynthesis of phenolic compounds as an abiotic stress respo...

  3. Effect of germination time on proximate analysis, bioactive compounds and antioxidant activity of lentil (Lens culinaris Medik. sprouts

    Directory of Open Access Journals (Sweden)

    A. Ahmed Fouad

    2015-09-01

    Full Text Available Background. The lentil plant, Lens culinaris L., is a member of the Leguminoceae family and constitutes one of the most important traditional dietary components. The purpose of the current study was to investigate the effects of sprouting for 3, 4, 5 and 6 days on proximate, bioactive compounds and antioxidative characteristics of lentil (Lens culinaris sprouts. Material and methods. Lentil seeds were soaked in distilled water (1:10, w/v for 12 h at room temperature (~25°C, then kept between thick layers of cotton cloth and allowed to germinate in the dark for 3, 4, 5 and 6 days. The nutritional composition, protein solubility, free amino acids, antinutritional factors, bioactive compounds and antioxidant activity of raw and germinated samples were determined using standard official procedures. Results. Sprouting process caused significant (P ≤ 0.05 increases in moisture, protein, ash, crude fiber, protein solubility, free amino acids, total, reducing and nonreducing sugars. However, oil content, antinutritional factors (tannins and phytic acid significantly (P ≤ 0.05 decreased. Results indicated that total essential amino acids of lentil seeds protein formed 38.10% of the total amino acid content. Sulfur-containing amino acids were the first limiting amino acid, while threonine was the second limiting amino acid in raw and germinated lentil seeds. Sprouting process has a positive effect on the essential amino acid contents and protein efficiency ratio (PER of lentil sprouts. Phenolics content increased from 1341.13 mg/100 g DW in raw lentil seeds to 1411.50, 1463.00, 1630.20 and 1510.10 in those samples germinated for 3, 4, 5 and 6 days, respectively. Sprouted seeds had higher DPPH radical scavenging and reducing power activities. Conclusions. Based on these results, sprouting process is recommended to increase nutritive value, and antioxidant activity of lentil seeds.

  4. Binding, Antioxidant and Anti-proliferative Properties of Bioactive Compounds of Sweet Paprika (Capsicum annuum L.).

    Science.gov (United States)

    Kim, Hong-Gi; Bae, Jong-Hyang; Jastrzebski, Zenon; Cherkas, Andriy; Heo, Buk-Gu; Gorinstein, Shela; Ku, Yang-Gyu

    2016-06-01

    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. PMID:27184000

  5. Bioactive Foamed Emulsion Reactor: A New Technology for Biotreatment of Airborne Volatile Organic Compound

    Directory of Open Access Journals (Sweden)

    F. Ghorbani Shahna

    2010-04-01

    Full Text Available Introduction & Objective: Biological treatment is a new established technology for the air pollutants. This technology can be an alternative for physical and chemical treatment methods. Among bioreators, the Bioactive Foamed Emulsion Reactor (BFER is a new alternative that has not the problems of the conventional ones. In this reactor bed clogging in the conventional bioreactor was resolved by bioactive foam as a substitute of packing bed. The pollutant absorption has been increased using biocompatible organic phase in liquid .This reactor can be used for higher inlet toluene concentration. The objective of this study was designing and optimizing the operational parameters of BFER for toluene treatment.Materials & Methods: In the first step of this experimental-analytic study, the toluene degradation microorganisms were identified, extracted and concentrated for injection to bioreactor. Then the effect of several parameters such as Kind and concentration of organic phase,and residence time oxygen content on bioreactor performance were studied and the optimum conditions were selected for continuous operation. The continuous operation of bioreactor was monitored at the optimum conditions.Results: Experimental results showed that the residence time of 15s, oxygen content of 40%, and the 4 % (v/v n-hexadecane as organic phase were the optimum conditions. The average elimination capacity (EC and removal efficiency of bioreactor were 231.68 g/m3h and 88.44% respectively for the inlet concentration about of 1 g/m3. The statistical developed model predicted that the maximum EC of this reactor could reach to 426.21 g/m3h.Conclusion: Since the elimination capacity of this reactor is several times more than the other bioreactors, it has the potential to be applied instead of biofilters and biotrickling filters.

  6. Simultaneous analysis of eight bioactive compounds in Danning tablet by HPLC-ESI-MS and HPLC-UV.

    Science.gov (United States)

    Liu, Runhui; Zhang, Jiye; Liang, Mingjin; Zhang, Weidong; Yan, Shikai; Lin, Min

    2007-02-19

    A high performance liquid chromatography (HPLC) coupled with electrospray tandem mass spectrometry (ESI-MS) and ultraviolet detector (UV) has been developed for the simultaneous analysis of eight bioactive compounds in Danning tablet (including hyperin, hesperidin, resveratrol, nobiletin, curcumine, emodin, chrysophanol, and physcion), a widely used prescription of traditional Chinese medicine (TCM). The chromatographic separation was performed on a ZORBAX Extend C(18) analytical column by gradient elution with acetonitrile and formate buffer (containing 0.05% formic acid, adjusted with triethylamine to pH 5.0) at a flow rate of 0.8 ml/min. The eight compounds in Danning tablet were identified and their MS(n) fractions were elucidated by using HPLC-ESI-MS, and the contents of these compounds were determined by using HPLC-UV method. The standard calibration curves were linear between 5.0 and 100 microg/ml for hyperin, 10-200 microg/ml for hesperidin, 1.0-150 microg/ml for resveratrol, 2.0-120 microg/ml for nobiletin, 2.0-225 microg/ml for curcumine, 20-300 microg/ml for emodin, 2.0-200 microg/ml for chrysophanol, and 20-250 microg/ml for physcion with regression coefficient r(2)>0.9995. The intra-day and inter-day precisions of this method were evaluated with the R.S.D. values less than 0.7% and 1.3%, respectively. The recoveries of the eight investigated compounds were ranged from 99.3% to 100.2% with R.S.D. values less than 1.5%. This method was successfully used to determine the 8 target compounds in 10 batches of Danning tablet. PMID:17079108

  7. Stereoselective synthesis of a natural product inspired tetrahydroindolo[2,3-a]-quinolizine compound library.

    Science.gov (United States)

    Sankar, Muthukumar G; Mantilli, Luca; Bull, James; Giordanetto, Fabrizio; Bauer, Jonathan O; Strohmann, Carsten; Waldmann, Herbert; Kumar, Kamal

    2015-06-01

    A natural product-inspired synthesis of a compound collection embodying the tetrahydroindolo[2,3-a]quinolizine scaffold was established with a five step synthesis route. An imino-Diels-Alder reaction between Danishefsky's diene and the iminoesters derived from tryptamines was used as a key reaction. Reductive amination of the ketone function and amide synthesis with the carboxylic acid derived from the ethyl ester, were used to decorate the core scaffold. Thus a compound library of 530 tetrahydroindolo[2,3-a]quinolizines was generated and submitted to European lead factory consortium for various biological screenings. PMID:25648684

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

    Science.gov (United States)

    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...

  9. Bioactive compounds and antifungal activity of three different seaweed species Ulva lactuca, Sargassum tenerrimum and Laurencia obtusa collected from Okha coast, Western India

    OpenAIRE

    Megha Barot; Nirmal Kumar JI; Rita N. Kumar

    2016-01-01

    Objective: To evaluate bioactive compounds responsible for antifungal activity from seaweeds of Okha coast, Western India. Methods: Each species were extracted with different solvents with increasing polarity: hexane, ethyl acetate, chloroform and methanol using Soxhlet apparatus. The antifungal activity was determined by agar diffusion plate method by using fluconazole, ketoconazole and amphotericin B as standards. Gas chromatography-mass spectrometer analysis was done for ...

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

    Directory of Open Access Journals (Sweden)

    Giulio Cerullo

    2008-10-01

    Full Text Available 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.

  11. Green chemistry approach to the synthesis of potentially bioactive aminobenzylated Mannich bases through active hydrogen compounds

    OpenAIRE

    S. L. VASOYA; P. T. CHOVATIA; D. H. PUROHIT; H. S. JOSHI

    2005-01-01

    An efficient and high yield method for the synthesis of aminobenzylated Mannich bases is described. The synthesis occurs in aqueous medium at 0 ºC. The compounds show moderate antitubercular and antimicrobial activities.

  12. Green chemistry approach to the synthesis of potentially bioactive aminobenzylated Mannich bases through active hydrogen compounds

    Directory of Open Access Journals (Sweden)

    S. L. VASOYA

    2005-10-01

    Full Text Available An efficient and high yield method for the synthesis of aminobenzylated Mannich bases is described. The synthesis occurs in aqueous medium at 0 ºC. The compounds show moderate antitubercular and antimicrobial activities.

  13. Use of Time-Resolved Fluorescence to Monitor Bioactive Compounds in Plant Based Foodstuffs

    OpenAIRE

    Lemos, M. Adília; Sárniková, Katarína; Bot, Francesca; Anese, Monica; Hungerford, Graham

    2015-01-01

    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...

  14. Effect of solid-state fermentation with Rhizopus oligosporus on bioactive compounds and antioxidant capacity of raw and roasted buckwheat groats

    OpenAIRE

    Wronkowska Małgorzata; Honke Joanna; Piskuła Mariusz Konrad

    2015-01-01

    The effect of solid-state fermentation with Rhizopus oligosporus on the changes in the total phenolic compounds, rutin, vitamin B and C, tocopherol, phytic acid and antioxidant capacity of raw and roasted buckwheat groats was studied. The roasted groats contained reduced level of studied bioactive compounds as compared to raw groats. In this study was evidenced that the solidstate fermentation with Rhizopus oligosporus enhanced water soluble vitamins (thiamine, pyridoxine and L-ascorbic acid)...

  15. A Wide-Field Fluorescence Microscope Extension for Ultrafast Screening of One-Bead One-Compound Libraries Using a Spectral Image Subtraction Approach.

    Science.gov (United States)

    Heusermann, Wolf; Ludin, Beat; Pham, Nhan T; Auer, Manfred; Weidemann, Thomas; Hintersteiner, Martin

    2016-05-01

    The increasing involvement of academic institutions and biotech companies in drug discovery calls for cost-effective methods to identify new bioactive molecules. Affinity-based on-bead screening of combinatorial one-bead one-compound libraries combines a split-mix synthesis design with a simple protein binding assay operating directly at the bead matrix. However, one bottleneck for academic scale on-bead screening is the unavailability of a cheap, automated, and robust screening platform that still provides a quantitative signal related to the amount of target protein binding to individual beads for hit bead ranking. Wide-field fluorescence microscopy has long been considered unsuitable due to significant broad spectrum autofluorescence of the library beads in conjunction with low detection sensitivity. Herein, we demonstrate how such a standard microscope equipped with LED-based excitation and a modern CMOS camera can be successfully used for selecting hit beads. We show that the autofluorescence issue can be overcome by an optical image subtraction approach that yields excellent signal-to-noise ratios for the detection of bead-associated target proteins. A polymer capillary attached to a semiautomated bead-picking device allows the operator to efficiently isolate individual hit beads in less than 20 s. The system can be used for ultrafast screening of >200,000 bead-bound compounds in 1.5 h, thereby making high-throughput screening accessible to a wider group within the scientific community. PMID:27057765

  16. Identification and Bioactivity of Compounds from the Mangrove Endophytic Fungus Alternaria sp.

    Directory of Open Access Journals (Sweden)

    Jinhua Wang

    2015-07-01

    Full Text Available Racemic new cyclohexenone and cyclopentenone derivatives, (±-(4R*,5S*,6S*-3-amino-4,5,6-trihydroxy-2-methoxy-5-methyl-2-cyclohexen-1-one (1 and (±-(4S*,5S*-2,4,5-trihydroxy-3-methoxy-4-methoxycarbonyl-5-methyl-2-cyclopenten-1-one (2, and two new xanthone derivatives 4-chloro-1,5-dihydroxy-3-hydroxymethyl-6-methoxycarbonyl-xanthen-9-one (3 and 2,8-dimethoxy-1,6-dimethoxycarbonyl-xanthen-9-one (4, along with one known compound, fischexanthone (5, were isolated from the culture of the mangrove endophytic fungus Alternaria sp. R6. The structures of these compounds were elucidated by analysis of their MS (Mass, one and two dimensional NMR (nuclear magnetic resonance spectroscopic data. Compounds 1 and 2 exhibited potent ABTS [2,2′-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid] scavenging activities with EC50 values of 8.19 ± 0.15 and 16.09 ± 0.01 μM, respectively. In comparison to Triadimefon, compounds 2 and 3 exhibited inhibitory activities against Fusarium graminearum with minimal inhibitory concentration (MIC values of 215.52 and 107.14 μM, respectively, and compound 3 exhibited antifungal activity against Calletotrichum musae with MIC value of 214.29 μM.

  17. Bioactive compounds, RP-HPLC analysis of phenolics, and antioxidant activity of some Portuguese shrub species extracts.

    Science.gov (United States)

    Luís, Angelo; Domingues, Fernanda; Duarte, Ana Paula

    2011-12-01

    In the ecosystem of Serra Da Estrela, some plant species have the potential to be used as raw material for extraction of bioactive products. The goal of this work was to determine the phenolic, flavonoid, tannin and alkaloid contents of the methanolic extracts of some shrubs (Echinospartum ibericum, Pterospartum tridentatum, Juniperus communis, Ruscus aculeatus, Rubus ulmifolius, Hakea sericea, Cytisus multiflorus, Crataegus monogyna, Erica arborea and Ipomoea acuminata), and then to correlate the phenolic compounds and flavonoids with the antioxidant activity of each extract. The Folin-Ciocalteu's method was used for the determination of total phenols, and tannins were then precipitated with polyvinylpolypyrrolidone (PVPP); a colorimetric method with aluminum chloride was used for the determination of flavonoids, and a Dragendorff's reagent method was used for total alkaloid estimation. The 2,2-diphenyl-1-picrylhydrazyl (DPPH) and beta-carotene bleaching tests were used to assess the antioxidant activity of extracts. The identification of phenolic compounds present in extracts was performed using RP-HPLC. A positive linear correlation between antioxidant activity index and total phenolic content of methanolic extracts was observed. The RP-HPLC procedure showed that the most common compounds were ferulic and ellagic acids and quercetin. Most of the studied shrubs have significant antioxidant properties that are probably due to the existence of phenolic compounds in the extracts. It is noteworthy to emphasize that for Echinospartum ibericum, Hakea sericea and Ipomoea acuminata, to the best of our knowledge, no phytochemical studies have been undertaken nor their use in traditional medicine been described. PMID:22312726

  18. Library+

    Science.gov (United States)

    Merrill, Alex

    2011-01-01

    This article discusses possible future directions for academic libraries in the post Web/Library 2.0 world. These possible directions include areas such as data literacy, linked data sets, and opportunities for libraries in support of digital humanities. The author provides a brief sketch of the background information regarding the topics and…

  19. An Alternative Use of Horticultural Crops: Stressed Plants as Biofactories of Bioactive Phenolic Compounds

    Directory of Open Access Journals (Sweden)

    Luis Cisneros-Zevallos

    2012-09-01

    Full Text Available Plants subjected to abiotic stresses synthesize secondary metabolites with potential application in the functional foods, dietary supplements, pharmaceutical, cosmetics and agrochemical markets. This approach can be extended to horticultural crops. This review describes previous reports regarding the effect of different postharvest abiotic stresses on the accumulation of phenolic compounds. Likewise, the physiological basis for the biosynthesis of phenolic compounds as an abiotic stress response is described. The information presented herein would be useful for growers and the fresh produce market which are interested in finding alternative uses for their crops, especially for those not meeting quality standards and thus are considered as waste.

  20. Physico-Chemical Characterization, Bioactive Compounds and Antioxidant Activity of Malay Apple [Syzygium malaccense (L.) Merr. & L.M. Perry

    Science.gov (United States)

    Nunes, Polyana Campos; Aquino, Jailane de Souza; Rockenbach, Ismael Ivan; Stamford, Tânia Lúcia Montenegro

    2016-01-01

    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

  1. Biopolymer-prebiotic carbohydrate blends and their effects on the retention of bioactive compounds and maintenance of antioxidant activity.

    Science.gov (United States)

    Silva, Eric Keven; Zabot, Giovani L; Cazarin, Cinthia B B; Maróstica, Mário R; Meireles, M Angela A

    2016-06-25

    The objective of this study was to evaluate the use of inulin (IN), a prebiotic carbohydrate without superficial activity, as an encapsulating matrix of lipophilic bioactive compounds. For achieving the encapsulation, IN was associated with biopolymers that present superficial activity: modified starch (HiCap), whey protein isolate (WPI) and gum acacia (GA). Encapsulation was performed through emulsification assisted by ultrasound followed by freeze-drying (FD) process to dry the emulsions. All blends retained geranylgeraniol. GA-IN blend yielded the highest geranylgeraniol retention (96±2wt.%) and entrapment efficiency (94±3wt.%), whilst WPI-IN blend yielded the highest encapsulation efficiency (88±2wt.%). After encapsulation, composition of geranylgeraniol in the annatto seed oil was maintained (23.0±0.5g/100g of oil). Such findings indicate that the method of encapsulation preserved the active compound. All blends were also effective for maintaining the antioxidant activity of the oil through ORAC and DPPH analyses. PMID:27083804

  2. Physico-Chemical Characterization, Bioactive Compounds and Antioxidant Activity of Malay Apple [Syzygium malaccense (L.) Merr. & L.M. Perry].

    Science.gov (United States)

    Nunes, Polyana Campos; Aquino, Jailane de Souza; Rockenbach, Ismael Ivan; Stamford, Tânia Lúcia Montenegro

    2016-01-01

    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

  3. Physico-Chemical Characterization, Bioactive Compounds and Antioxidant Activity of Malay Apple [Syzygium malaccense (L. Merr. & L.M. Perry].

    Directory of Open Access Journals (Sweden)

    Polyana Campos Nunes

    Full Text Available 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.

  4. Influence of extraction techniques on antioxidant properties and bioactive compounds of loquat fruit (Eriobotrya japonica Lindl.) skin and pulp extracts

    Science.gov (United States)

    Delfanian, Mojtaba; Esmaeilzadeh Kenari, Reza; Sahari, Mohammad Ali

    2015-01-01

    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

  5. Bioactive compounds and nutritional significance of virgin argan oil--an edible oil with potential as a functional food.

    Science.gov (United States)

    Cabrera-Vique, Carmen; Marfil, Rocío; Giménez, Rafael; Martínez-Augustin, Olga

    2012-05-01

    This review compiles recently published scientific reports on the bioactive compounds present in virgin argan oil along with their possible beneficial effects on human health, which could justify consideration of this oil as a new functional food. Virgin argan oil is characterized by high levels of linoleic and oleic acids, tocopherols (especially γ-tocopherol), and minor compounds such as sterols, carotenoids, and squalene. The total antioxidant capacity of virgin argan oil is higher than that of other vegetable oils. Recent studies suggest that this edible oil, as a functional food, may play a role in disease prevention. For example, some authors have found it to have hypolipidemic, hypocholesterolemic, hypoglycemic, and antihypertensive effects as well as a possible role in cancer prevention. This review demonstrates the need for further studies in order to fully characterize argan oil from bromatological, nutritional, culinary, and technological perspectives. In particular, the scarcity of clinical data hampers relevant conclusions from being drawn regarding the therapeutic effects of virgin argan oil. PMID:22537213

  6. A comparison of bioactive compounds of strawberry fruit from Europe affected by genotype and latitude

    DEFF Research Database (Denmark)

    Josuttis, M.; Carlen, C.; Nestby, R.;

    2012-01-01

    compounds and this effect was stronger than local variations by temporary weather changes or even year-to-year effects. As a result, the northern samples had principally lower anthocyanin amounts than the southern ones and, moreover, distribution of individual anthocyanins was different. In contrast, the...

  7. Two new naphthalene glucosides and other bioactive compounds from the carnivorous plant Nepenthes mirabilis.

    Science.gov (United States)

    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

    2015-10-01

    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. PMID:25724283

  8. Hyphenated GC-FTIR and GC-MS techniques applied in the analysis of bioactive compounds

    Science.gov (United States)

    Gosav, Steluta; Paduraru, Nicoleta; Praisler, Mirela

    2014-08-01

    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.

  9. In vitro Antioxidant Activity between Bioactive Compounds from Nine Species of Passiflora

    Directory of Open Access Journals (Sweden)

    DAV Montero

    2015-06-01

    Full Text Available Main bioactive substances identified from the genus Passiflora include polyphenols, flavonoids, carotenoids, anthocyanins and other natural antioxidants that are critical factors for maintaining optimum health. Polyphenols mainly C-glycosides are present in well studied species such as P. edulis, P. incarnata and P. alata. However, most Passiflora species remains little explored and it’s for this reason that we address our work at the comparison between species. Three experiments with completely randomized designs were performed in order to compare the total amount of flavonoids, phenols and in vitro free radical DPPH scavenger activity (%DPPH of nine species of Passiflora (P. edulis, P. alata, P. incarnata, P. ligularis, P. tripartite, P. coccinea, P. gardneri, P. laurifólia and P. mucronata. Non parametric Kruskal-Wallis and Friedman tests (for flavonoids, parametric analyses of variances (Anova and the last significant differences (LSD tests (for phenols and free radical scavenger activity were performed to compare the studied species and then a correlation analysis was carried out to assess the interaction between the variables using RStudio statistical software. Results showed significant differences between the studied passionflowers for the total amount of flavonoids (p=4.4e-5, total amount of phenols (p=2.2e-16 and scavenger activity of the free radical DPPH (p=2.2e-16. Also, we found a positive correlation between %DPPH scavenging activity and the total content of polyphenols (Pearson’s coefficient=0.706 and a negative one between flavonoid (Pearson’s coefficient=-0.485. The results suggest that in passionflower leaf samples the scavenging activity of the free radical DPPH is more related with polyphenols rather than flavonoids.

  10. Bioactive compounds in edible flowers processed by radiation; Compostos bioativos em flores comestiveis processadas por radiacao

    Energy Technology Data Exchange (ETDEWEB)

    Koike, Amanda Cristina Ramos

    2015-07-01

    Edible flowers are increasingly being used in culinary preparations, being also recognized for their potential valuable effects in human health, which require new approaches to improve their conservation and safety. These highly perishable products should be grown without using any pesticide. Irradiation treatment might be the answer to these problems, ensuring food quality, increasing shelf-life and disinfestation of foods. Irradiation treatment might be the answer to these problems, to ensure food quality, to increase shelf-life and disinfestation of foods. Tropaeolum majus L. (nasturtium) and Viola tricolor L. (johnny-jump-up) flowers are widely used in culinary preparations, being also acknowledged for their antioxidant properties and high content of phenolics. The purpose of this study was to evaluate the dose-dependent effects of gamma and electron beam irradiation (doses of 0, 0.5, 0.8 and 1 kGy) on the antioxidant activity, phenolic compounds, physical aspects and antiproliferative potential of edible flowers. Kaempferol-O-hexoside-O-hexoside was the most abundant compound in all samples of Tropaeolum majus flower while pelargonidin-3-O-sophoroside was the major anthocyanin. In general, irradiated samples gave higher antioxidant activity, probably due to their higher amounts of phenolic compounds, which were also favored by the 1.0 kGy dose, regardless of the source . The Viola tricolor samples displayed flavonols as the most abundant phenolic compounds, particularly those derived from quercetin. In general, gamma-irradiated samples, independently of the applied dose, showed higher amounts in phenolic compounds, which were also favored by the 1.0 kGy dose, regardless of the source. The antioxidant activity was also higher among irradiated samples. The two species of edible flowers have not provided the samples did not show potential antiproliferative and cytotoxicity. Accordingly, the applied irradiation treatments seemed to represent a feasible technology

  11. Antileishmanial activity of compounds produced by endophytic fungi derived from medicinal plant Vernonia polyanthes and their potential as source of bioactive substances.

    Science.gov (United States)

    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

    2015-11-01

    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. PMID:26318306

  12. Optimization of the extraction process for the seven bioactive compounds in Yukmijihwang-tang, an herbal formula, using response surface methodology

    Directory of Open Access Journals (Sweden)

    Jung-Hoon Kim

    2014-01-01

    Full Text Available 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.

  13. Bioactivity-guided isolation of new antiproliferative compounds from Juniperus foetidissima Willd.

    Science.gov (United States)

    Rafieian-Kopaei, Mahmood; Suleimani Dehkordi, Ibrahim; Ghanadian, Mustafa; Shokrollahi, Ardeshir; Aghaei, Mahmoud; Syed Majid, Ayatollahi; Choudhary, M Iqbal

    2016-09-01

    Based on a literature survey on cytotoxic medicinal plants, Juniper species were identified as interesting source of antitumor compounds. Using bioassay-guided fractionation against Caov-4 cancer cells on acetone extract of leaves and branchlets of Juniperus foetidissima led to the isolation of a new 3H-benzofuaran-2-one: 4-methyl-3-methoxy-3H-benzofuaran-2-one (1), a new sesquiterpene: 4,9(α)-dihydroxy-nardosin-6-en (2) and an already known labdane-type diterpene: 15-hydroxy-8(17),13(E)-labdadiene-19-carboxilic acid (3). Compounds 1-3 exhibited cytotoxic effects, with moderate cytotoxicity against the EJ-138 bladder and CAOV-4 ovary cancer cell lines. PMID:26506268

  14. Inflorescences of Brassicacea species as source of bioactive compounds: a comparative study

    OpenAIRE

    C. Sousa; Taveira, M.; Valentão, P.; Fernandes, F; Pereira, J.A.; Leticia M. Estevinho; Bento, Albino; Ferreres, F.; Seabra, R.M.; P. B. Andrade

    2008-01-01

    Two Brassica oleracea varieties (B. oleracea L. var. costata DC and B. oleracea L. var. acephala) and Brassica rapa L. var. rapa inflorescences were studied for their chemical composition and antioxidant capacity. Phenolic compounds and organic acids profiles were determined by HPLC–DAD and HPLC–UV, respectively. B. oleracea var. costata and B. oleracea L. var. acephala inflorescences presented a similar qualitative phenolic composition, exhibiting several complex kaempferol deriv...

  15. Effects of Processing Treatments on the Bioactive Compounds of Campbell Grape Juice

    OpenAIRE

    Shirley G. Cabrera; Kwang-Deog Moon

    2015-01-01

    It is well known that phenolic compounds and flavonoids have a lot of health benefits. Most current heat treatments especially those that are using too high temperature and longer period of processing produce juice with unacceptable analytical and sensory properties. Thus, microwave heating, ultrasonication and blanching before grape juice processing were employed in this study. Each juice sample was subjected to total phenolics, total flavonoid, total anthocyanin and % radical sc...

  16. Innovative minimal processing of mini broccoli for keeping quality and safety and enhancing bioactive compounds

    OpenAIRE

    Martínez Hernández, Ginés Benito

    2012-01-01

    [ENG] Broccoli has been described as the ‘super–vegetable’ in the media after a great number of epidemiological and laboratory studies on this Brassica specie. These studies have shown numerous health–promoting properties of broccoli such as chemopreventive, antioxidant, antitumor, antimutagenicity, anti–inflammatory, antimicrobial, antiviral and reduction of coronary heart disease risk. These properties are related to the high content of broccoli in phenolic compounds, glucosinolates (isothi...

  17. In Vitro Wound Healing Potential and Identification of Bioactive Compounds from Moringa oleifera Lam

    OpenAIRE

    Abubakar Amali Muhammad; Nur Aimi Syarina Pauzi; Palanisamy Arulselvan; Faridah Abas; Sharida Fakurazi

    2013-01-01

    Moringa oleifera Lam. (M. oleifera) from the monogeneric family Moringaceae is found in tropical and subtropical countries. The present study was aimed at exploring the in vitro wound healing potential of M. oleifera and identification of active compounds that may be responsible for its wound healing action. The study included cell viability, proliferation, and wound scratch test assays. Different solvent crude extracts were screened, and the most active crude extract was further subjected to...

  18. Evaluation of bioactive properties and phenolic compounds in different extracts prepared from Salvia officinalis L.

    OpenAIRE

    Martins, Natália; Barros, Lillian; Santos-Buelga, Celestino; Henriques, Mariana; Silva, Sónia; Ferreira, Isabel C. F. R.

    2015-01-01

    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 characterized in terms of phenolic compounds. Decoction and methanol/water extract gave the most...

  19. Tocopherols as bioactive compounds in different cultivars of Gomphrena globosa L.

    OpenAIRE

    Liberal, Ângela; Pereira, Carla; Adega, Filomena; Barros, Lillian; Ferreira, Isabel C. F. R.

    2015-01-01

    Tocopherols are lipid-soluble molecules that belong to the group of the Vitamin E compounds, playing an essential role on human nutrition and health [1]. The term "Vitamin E" was first introduced as an important dietary factor for animal reproduction and, more than 40 years later, it was associated to antioxidant properties. Nowadays, most of the researches focus on the fundamental chemistry that explains their antioxidant properties, specific location, role in biological membr...

  20. Variation in the Bioactive Compound Content at Three Ripening Stages of Strawberry Fruit

    OpenAIRE

    Sandra Voća; Jana Šic Žlabur; Nadica Dobričević; Lidija Jakobek; Marijan Šeruga; Ante Galić; Stjepan Pliestić

    2014-01-01

    During the harvest season of two consecutive years, five strawberry cultivars (‘Arosa’, ‘Elsanta’, ‘Marmolada’, ‘Miss’ and ‘Raurica’), grown in the continental part of the Republic of Croatia, were examined. Strawberry fruits quality was evaluated by individual phenol compounds, individual anthocyanins and fruit color. Fruits were harvested in three different periods. Analyzed strawberry cultivars show very good average values of the studied phenolic acids and flavonoids with predominant caff...

  1. Targeted analysis of bioactive phenolic compounds and antioxidant activity of Macedonian red wines

    OpenAIRE

    Ivanova, Violeta; Ricci, Arianna; Nedelkovski, Dusko; Dimovska, Violeta; Parpinello, Giuseppina P.; Versari, Andrea

    2015-01-01

    Phenolic composition of twenty-two Macedonian red wines, including ten autochthonous monovarietal Vranec wines produced with different yeasts for fermentation, and twelve wines from international varieties (Syrah, Merlot and Cabernet Sauvignon) from different wine regions was studied. All wines presented relatively high value of total phenols and antioxidant activity. A total of 19 phenolic compounds were identified and quantified using HPLC-DAD and among them, malvidin-3-glucoside and its de...

  2. Optimization of extraction and microencapsulation of bioactive compounds from red grape (Vitis vinifera L.) pomace

    OpenAIRE

    Boonchu, Thapakorn; Utama-ang, Niramon

    2013-01-01

    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 resu...

  3. Bioactive compounds and antioxidant activity of Rosa canina L. biotypes from spontaneous flora of Transylvania

    OpenAIRE

    Roman, Ioana; Stănilă, Andreea; Sorin STĂNILĂ

    2013-01-01

    Background The theoretical, but especially the practical values of identifying the biochemical compounds from the Rosa canina L. fruits are of present interest, this aspect being illustrated by the numerous researches. It was reported that the Rosa canina L. fruit, with its high ascorbic acid, phenolics and flavonoids contents, have antioxidant, antimutagenic and anticarcinogenic effects. This study was performed on order to evaluate the amount of the main phytochemicals (vitamin C, total pol...

  4. Phytochemical characterization of bioactive compounds on methanolic and ethanolic leaf extracts of Myrciaria sp.

    Directory of Open Access Journals (Sweden)

    Nathalia F. Naspolini

    2016-06-01

    Full Text Available Among the native species of importance in Brazil, jabuticabeira (Myrciaria sp. is a native fruit tree from several Brazilian regions. Few studies report the chemical constituents of the leaves and its pharmacological and nutraceutical properties. The aim of this study was to identify the phenolic compounds of the methanolic (MeOH and ethanolic (EtOH leaf extracts of Myrciaria sp. Phytochemical profile of the extracts was carried-out using High Performance Liquid Chromatography (HPLC analysis. Antioxidant potential was evaluated by radical scavenging capacity with 2,2-diphenyl-1-picryl-hydrazyl (DPPH and total phenolics were determined with Folin-Ciocalteau reagent. A total of nine different compounds were identified in the free and bound phenolics extractions: 2,4 dihydroxybenzoic, vanillin, p-coumaric, ferulic, sinapinic, rutin, epicatechin, trans-caffeic and myricetin. The extracts demonstrated high radical scavenging capacity (MeOH: 1.83 and EtOH: 8.05 mg/mL and high phenolic content (MeOH: 1.15; and EtOH: 1.04 mg/g dry matter. The wide variability of compounds revealed and the amount of peaks not identified, gives us a background of a potential plant matrix for further investigations in order to develop a nutraceutical agent.

  5. Optimization of extraction and microencapsulation of bioactive compounds from red grape (Vitis vinifera L.) pomace.

    Science.gov (United States)

    Boonchu, Thapakorn; Utama-Ang, Niramon

    2015-02-01

    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. PMID:25694686

  6. FAF-Drugs3: a web server for compound property calculation and chemical library design.

    Science.gov (United States)

    Lagorce, David; Sperandio, Olivier; Baell, Jonathan B; Miteva, Maria A; Villoutreix, Bruno O

    2015-07-01

    Drug attrition late in preclinical or clinical development is a serious economic problem in the field of drug discovery. These problems can be linked, in part, to the quality of the compound collections used during the hit generation stage and to the selection of compounds undergoing optimization. Here, we present FAF-Drugs3, a web server that can be used for drug discovery and chemical biology projects to help in preparing compound libraries and to assist decision-making during the hit selection/lead optimization phase. Since it was first described in 2006, FAF-Drugs has been significantly modified. The tool now applies an enhanced structure curation procedure, can filter or analyze molecules with user-defined or eight predefined physicochemical filters as well as with several simple ADMET (absorption, distribution, metabolism, excretion and toxicity) rules. In addition, compounds can be filtered using an updated list of 154 hand-curated structural alerts while Pan Assay Interference compounds (PAINS) and other, generally unwanted groups are also investigated. FAF-Drugs3 offers access to user-friendly html result pages and the possibility to download all computed data. The server requires as input an SDF file of the compounds; it is open to all users and can be accessed without registration at http://fafdrugs3.mti.univ-paris-diderot.fr. PMID:25883137

  7. Bioactivity Screening of Fermentation Crude Extracts from Deep Sea Metagenomic Library Clones%深海宏基因组文库克隆子发酵产物的生物活性筛选

    Institute of Scientific and Technical Information of China (English)

    汤熙翔; 易志伟; 李宁; 马群; 李慧; 秦丹; 肖湘

    2011-01-01

    目的:对前期构建的深海宏基因组文库克隆子发酵产物进行生物活性筛选.方法:利用CCK8法及琼脂扩散法和双层琼脂法进行了细胞毒活性及抗菌活性筛选,利用荧光定量PCR法进行了抗乙肝病毒活性筛选.结果:筛选发现3个具有细胞毒活性的混合克隆子.HPLC指纹图谱分析表明这3个混合克隆子具有与大肠杆菌宿主对照不同的指纹图谱,其活性与出现的指纹峰成分可能相关.结论:研究结果提示对深海宏基因组文库克隆子发酵产物进行化学筛选为常规的生物活性功能筛选之外的有意义途径.%Objective: Detect bioactivities of fermentation crude extracts originated from previously constructed deep sea metagenomic libraries. Methods : Functional screening of antitumor( cytotoxic ) ,antibacterial and anti HBV activity from fermentation crude extracts was performed by CCK-8 method, agar diffusion method,double agar method and real time PCR method. Results: No antibacterial and anti HBV clones were identified and three mixed clones showed good cytotoxic activity. HPLC analysis of these three mixed clones fingerprints indicated they possess obviously different fingerprints with E. coli host which could be useful to next isolation of cytotoxic compounds from deep sea metagenomic library. Conclusion: These results indicated that chemical screening could be potential way for screening bioactivity substance from deep sea metagenomic libraries besides functional screening and homology screening.

  8. Cdc25B Dual-Specificity Phosphatase Inhibitors Identified in a High-Throughput Screen of the NIH Compound Library

    OpenAIRE

    Johnston, Paul A.; Foster, Caleb A.; Tierno, Marni Brisson; Shun, Tong Ying; Shinde, Sunita N.; Paquette, William D.; Brummond, Kay M.; Wipf, Peter; Lazo, John S.

    2009-01-01

    The University of Pittsburgh Molecular Library Screening Center (Pittsburgh, PA) conducted a screen with the National Institutes of Health compound library for inhibitors of in vitro cell division cycle 25 protein (Cdc25) B activity during the pilot phase of the Molecular Library Screening Center Network. Seventy-nine (0.12%) of the 65,239 compounds screened at 10 μM met the active criterion of ≥50% inhibition of Cdc25B activity, and 25 (31.6%) of these were confirmed as Cdc25B inhibitors wit...

  9. Effect of solid-state fermentation with Rhizopus oligosporus on bioactive compounds and antioxidant capacity of raw and roasted buckwheat groats

    Directory of Open Access Journals (Sweden)

    Wronkowska Małgorzata

    2015-12-01

    Full Text Available The effect of solid-state fermentation with Rhizopus oligosporus on the changes in the total phenolic compounds, rutin, vitamin B and C, tocopherol, phytic acid and antioxidant capacity of raw and roasted buckwheat groats was studied. The roasted groats contained reduced level of studied bioactive compounds as compared to raw groats. In this study was evidenced that the solidstate fermentation with Rhizopus oligosporus enhanced water soluble vitamins (thiamine, pyridoxine and L-ascorbic acid as well as tocopherols contents. In contrast the decrease of the inositol hexaphosphate, phenolic compounds, the rutin content and antioxidant capacity determined by ACL and ABTS methods was noticed.

  10. Use of Biotechnology to increase the content of bioactive compounds in fermented foods of plant origin

    OpenAIRE

    Taneyo Saa, Danielle Laure

    2014-01-01

    The objectives of this PhD research were: i) to evaluate the use of bread making process to increase the content of β-glucans, resistant starch, fructans, dietary fibers and phenolic compounds of kamut khorasan and wheat breads made with flours obtained from kernels at different maturation stage (at milky stage and fully ripe) and ii) to study the impact of whole grains consumption in the human gut. The fermentation and the stages of kernel development or maturation had a great impact on t...

  11. Assessment of wild mint from Tunceli as source of bioactive compounds, and its antioxidant Activity.

    Science.gov (United States)

    Turkoglu, S

    2015-01-01

    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. PMID:26718431

  12. Wild Prunus Fruit Species as a Rich Source of Bioactive Compounds.

    Science.gov (United States)

    Mikulic-Petkovsek, Maja; Stampar, Franci; Veberic, Robert; Sircelj, Helena

    2016-08-01

    Sugars, organic acids, carotenoids, tocopherols, chlorophylls, and phenolic compounds were quantified in fruit of 4 wild growing Prunus species (wild cherry, bird cherry, blackthorn, and mahaleb cherry) using HPLC-DAD-MSn. In wild Prunus, the major sugars were glucose and fructose, whereas malic and citric acids dominated among organic acids. The most abundant classes of phenolic compounds in the analyzed fruit species were anthocyanins, flavonols, derivatives of cinnamic acids, and flavanols. Two major groups of anthocyanins measured in Prunus fruits were cyanidin-3-rutinoside and cyanidin-3-glucoside. Flavonols were represented by 19 derivatives of quercetin, 10 derivatives of kaempferol, and 2 derivatives of isorhamnetin. The highest total flavonol content was measured in mahaleb cherry and bird cherry, followed by blackthorn and wild cherry fruit. Total phenolic content varied from 2373 (wild cherry) to 11053 mg GAE per kg (bird cherry) and ferric reducing antioxidant power antioxidant activity from 7.26 to 31.54 mM trolox equivalents per kg fruits. PMID:27464261

  13. Construction and screening of marine metagenomic libraries

    DEFF Research Database (Denmark)

    Weiland, Nancy; Löscher, Carolin; Metzger, Rebekka;

    2010-01-01

    microbial consortia on marine tissues of multicellular organisms are rich sources for isolating novel bioactive compounds and genes. Here we describe the sampling, construction of large-insert metagenomic libraries from marine habitats and exemplarily one function based screen of metagenomic clones....

  14. Characterization of physiochemical and microbiological properties, and bioactive compounds, of flour made from the skin and bagasse of kiwi fruit (Actinidia deliciosa).

    Science.gov (United States)

    Soquetta, Marcela Bromberger; Stefanello, Flávia Santi; Huerta, Katira da Mota; Monteiro, Sabrina Sauthier; da Rosa, Claudia Severo; Terra, Nelcindo Nascimento

    2016-05-15

    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. PMID:26775997

  15. Simultaneous determination of four bioactive compounds in Verbena officinalis L. by using high-performance liquid chromatography

    Directory of Open Access Journals (Sweden)

    Zhen Liu

    2012-01-01

    Full Text Available Background: Verbena officinalis L., called mabiancao in Chinese, is derived from the aerial part of Herba Verbanae. It is a traditional Chinese medicine commonly used in China and northern Europe, which is widely used for clearing away heat and detoxicating, promoting blood circulation, and removing blood stasis. This paper describes a sensitive and specific assay for the determination of four bioactive compounds in V. officinalis L. Materials and Methods: In this paper, the four components were separated on an Agilent Zorbax Extend C 18 column (250 mm × 4.6 mm × 5 μm and detected by a diode array detector. The mobile phase was composed of (a aqueous phosphoric acid (0.1%, v/v and (b acetonitrile using a gradient elution. Analytes were performed at 30°C with a flow rate of 1.0 ml/min and UV detection at 203, 238, and 331 nm. Results: All calibration curves showed good linear regression (r2 ≥ 0.9999 within tested ranges. Overall intra- and interday variations were less than 1.84%, and the average recoveries were 97.32-102.81% for analytes. Discussion and Conclusion: The proposed method would be sensitive enough and reliable for comprehensive quality control for clinical use and modernization of V. officinalis L.

  16. Preharvest application of oxalic acid increased fruit size, bioactive compounds, and antioxidant capacity in sweet cherry cultivars (Prunus avium L.).

    Science.gov (United States)

    Martínez-Esplá, Alejandra; Zapata, Pedro Javier; Valero, Daniel; García-Viguera, Cristina; Castillo, Salvador; Serrano, María

    2014-04-16

    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. PMID:24684635

  17. Molecular docking of the anticancer bioactive compound proceraside with macromolecules involved in the cell cycle and DNA replication.

    Science.gov (United States)

    Gurung, A B; Ali, M A; Bhattacharjee, A; AbulFarah, M; Al-Hemaid, F; Abou-Tarboush, F M; Al-Anazi, K M; Al-Anazi, F S M; Lee, J

    2016-01-01

    The bioactive compounds proceraside A, frugoside and calotropin, which were extracted from the root bark of Calotropis procera (Aiton) W.T. Aiton (family Asclepiadaceae), were recently reported to inhibit the growth of inhibition against various human cancer cell lines in vitro. However, their modes of action have not been clearly defined. Therefore, we attempted an in silico approach to gain insights into their binding modes against the following selected molecular targets: CDK-2, CDK-6, topoisomerase I, BCL-2, VEGFR-2, telomere: G-quadruplex, and topoisomerase II. These targets were selected based on their key roles in cancer progression via the regulation of the cell cycle and DNA replication. Molecular-docking analyses revealed that proceraside A was the best docked ligand against all the targets, with the exception of telomere-G: quadruplex. Furthermore, it displayed the lowest binding energies and inhibition constants, and critical hydrogen bonds and hydrophobic interactions with the targets were also revealed. The present study may aid in the identification of possible targets for proceraside A, and might provide a plausible explanation for its proven anti-tumor activities. Moreover, the result of this study may further guide structure-activity relationship studies used to generate more potent target-specific inhibitors. PMID:27173346

  18. Novel fiber-rich lentil flours as snack-type functional foods: an extrusion cooking effect on bioactive compounds.

    Science.gov (United States)

    Morales, P; Berrios, J De J; Varela, A; Burbano, C; Cuadrado, C; Muzquiz, M; Pedrosa, M M

    2015-09-01

    Novel snack-type functional foods based on extruded lentil flours could convey the related health benefit of their bioactive compounds, provide a gluten-free alternative to consumers, and potentially increase the consumption of pulses. Extrusion treatment promoted an increase in galactopinitol, ciceritol, raffinose, stachyose and total α-galactoside content, in most lentil flours. As α-galactosides may act as prebiotics, they could convey beneficial effects to human and monogastric animals. Conversely, extrusion significantly (p < 0.05) reduced the inositol hexaphosphate content to less phosphorylated phytates (inositol pentaphosphate and inositol tetraphosphate), which provide health effects. The gluten-free formulation (control formulation #3) presented the highest significant (p < 0.05) drop in the inositol hexaphosphate of 14.7-fold decrease, but had a large increase in inositol pentaphosphate, due to extrusion processing. These two results are desirable in the finished product. Extrusion also caused a significant (p < 0.05) reduction in the trypsin content and completely inactivated lectin, in all processed samples. PMID:26221783

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

    Science.gov (United States)

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

    2015-06-01

    The objective of this work was investigate the synergistic, additive and antagonistic effects of fruit mixtures on total antioxidant capacities and bioactive compounds in tropical fruit juices, and optimize its formulation by the response surface methodology based on the responses: total polyphenols (TP), total antioxidant capacity (TAC), ascorbic acid content and sensorial acceptance. Camu-camu, acerola and acai were the major factors that influenced the antioxidant potential of the juice; and the yellow mombin showed a positive effect on the acceptance of the tropical juice. It was observed an/antagonistic effect between acerola and camu-camu for the TAC response. The optimum formulation obtained was 20% acerola, 10% camu-camu, 10% yellow mombin, 10% cashew apple and 10% acai, which was responsible for a response of 155.46 mg.100 g(-1) of ascorbic acid, 103.01 mg of GAE.100 g-1 of TP, 10.27 µM Trolox g(-1) of TAC and approximately 6.1 of acceptance. PMID:26817384

  20. Review of clinical studies of Polygonum multiflorum Thunb. and its isolated bioactive compounds

    Directory of Open Access Journals (Sweden)

    Guy-Armel Bounda

    2015-01-01

    Full Text Available 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.

  1. Immunomodulatory Effects of a Bioactive Compound Isolated from Dryopteris crassirhizoma on the Grass Carp Ctenopharyngodon idella

    Directory of Open Access Journals (Sweden)

    Cheng Chi

    2016-01-01

    Full Text Available In the present study, we investigated effects of compound kaempferol 3-a-L-(4-O-acetylrhamnopyranoside-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.

  2. ANALYSIS OF BIOACTIVE COMPOUNDS BY GC-MS FROM THE YOUNG LEAVES OF TECTONA GRANDISL.F.

    Directory of Open Access Journals (Sweden)

    Greeshma Murukan

    2015-07-01

    Full Text Available The timber value of Tectona grandis has been established from decades. Teak is an exotic species cultivated along most parts of tropical regions. Anthocyanins are natural colourants which have raised a growing demand due to their extensive range of colours, innocuous and beneficial health effects. Anthocyanins belong to large group of polyphenolics - flavonoids, which are secondary metabolites synthesized by higher plants. Despite the remarkable application of anthocyanins in food, pharmaceutical and cosmetic industries, still it is not properly exploited. In the present study, the bioactive components of Tectona grandis young leaves have been evaluated using Perkin-Elmer Gas chromatography-Mass spectrometry. GC-MS analysis revealed the existence of eleven compounds. 5,9-Methanobenzocycloocten-1(2H-one,3,4,5,6,7,8,9,10-octahydro-5,10-dihydroxy-3,3,7,7,9- pentamethyl (76.02% and 1-naphthalenecarboxylic acid,5-[2-(3-furanylethyl]decahydro-1,4a-dimethyl-6- methylene-[1R-(1.alpha.,4a.] (13.95%. Other compounds present in minor quantities were ledol(0.92%, 3- Buten-2-one,4-(2,6,6-trimethyl-1-cyclohexen-1-ylorionone(0.49%,9,12,15 Octadecatrienoic acid, methyl ester, (Z,Z,Z- or Linolenic acid methyl ester (0.82%, Phytol (0.69%, Cedran-diol, 8S,14- (0.60%, Lupeol (0.71%, 3- Methoxymethyl-2,5,5,8a-tetramethyl-6,7,8a-tetrahydro-5H-chromene (3.45% and Retinol(1.27%. This is the first report of identification of active constituents from the young leaves of Tectona grandis.

  3. Metabonomics classifies pathways affected by bioactive compounds. Artificial neural network classification of NMR spectra of plant extracts.

    Science.gov (United States)

    Ott, Karl-Heinz; Araníbar, Nelly; Singh, Bijay; Stockton, Gerald W

    2003-03-01

    The biochemical mode-of-action (MOA) for herbicides and other bioactive compounds can be rapidly and simultaneously classified by automated pattern recognition of the metabonome that is embodied in the 1H NMR spectrum of a crude plant extract. The ca. 300 herbicides that are used in agriculture today affect less than 30 different biochemical pathways. In this report, 19 of the most interesting MOAs were automatically classified. Corn (Zea mays) plants were treated with various herbicides such as imazethapyr, glyphosate, sethoxydim, and diuron, which represent various biochemical modes-of-action such as inhibition of specific enzymes (acetohydroxy acid synthase [AHAS], protoporphyrin IX oxidase [PROTOX], 5-enolpyruvylshikimate-3-phosphate synthase [EPSPS], acetyl CoA carboxylase [ACC-ase], etc.), or protein complexes (photosystems I and II), or major biological process such as oxidative phosphorylation, auxin transport, microtubule growth, and mitosis. Crude isolates from the treated plants were subjected to 1H NMR spectroscopy, and the spectra were classified by artificial neural network analysis to discriminate the herbicide modes-of-action. We demonstrate the use and refinement of the method, and present cross-validated assignments for the metabolite NMR profiles of over 400 plant isolates. The MOA screen also recognizes when a new mode-of-action is present, which is considered extremely important for the herbicide discovery process, and can be used to study deviations in the metabolism of compounds from a chemical synthesis program. The combination of NMR metabolite profiling and neural network classification is expected to be similarly relevant to other metabonomic profiling applications, such as in drug discovery. PMID:12590124

  4. Identification of entry inhibitors of Ebola virus pseudotyped vectors from a myxobacterial compound library.

    Science.gov (United States)

    Beck, Simon; Henß, Lisa; Weidner, Tatjana; Herrmann, Jennifer; Müller, Rolf; Chao, Yu-Kai; Grimm, Christian; Weber, Christopher; Sliva, Katja; Schnierle, Barbara S

    2016-08-01

    Myxobacteria produce secondary metabolites many of which were described to have various biological effects including anti-fungal, anti-bacterial and anti-viral activity. The majority of these metabolites are novel scaffolds with unique modes-of-action and hence might be potential leads for drug discovery. Here, we tested a myxobacterial natural product library for compounds with inhibitory activity against Ebola virus (EBOV). The assay was performed with a surrogate system using Ebola envelope glycoprotein (GP) pseudotyped lentiviral vectors. EBOV specificity was proven by counter-screening with vesicular stomatitis virus G protein pseudotyped vectors. Two compounds were identified that preferentially inhibited EBOV GP mediated cell entry: Chondramides that act on the actin skeleton but might be too toxic and noricumazole A, a potassium channel inhibitor, which might constitute a novel pathway to inhibit Ebola virus cell entry. PMID:27241689

  5. Rapid screening and distribution of bioactive compounds in different parts of Berberis petiolaris using direct analysis in real time mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    Awantika Singh; Vikas Bajpai; Mukesh Srivastava; Kamal Ram Arya; Brijesh Kumar

    2015-01-01

    Berberis petiolaris Wall. ex G. Don, an unexplored medicinal plant belonging to the family Berberidaceae, is a large deciduous shrub found in Western Himalaya between 1800-3000 m. Chemical profiling of fruit, leaf, root and stem was done by direct analysis in real time mass spectrometry followed by multivariate analysis for discrimination among the plant parts. The bioactive compounds, including magnoflorine, berberine, jatrorrhizine, thalifendine/berberrubine, demethyleneberberine, reticuline, 8-oxoberberine, N-methyltetrahydroberberine, tetrahydropalmatine, tetrahydroberberine and palmatine, were identified by their exact mass measurement and the corresponding molecular formula of each compound. A comparative study of distribution pattern for all these bioactive alkaloids showed qualitative and quantitative variations in different parts of B. petiolaris. Principal component analysis clearly dis-criminated each part of B. petiolaris plant.

  6. Some bioactive compounds and antioxidant activities of the bitter almond kernel (prunus dulcis var. amara)

    International Nuclear Information System (INIS)

    in this study, it was determined antioxidant activities and phenolic, flavonoid, phytosterol, lipid soluble vitamin and fatty acid contents of bitter almond kernel extract (bae). antioxidant activities of bae was investigated by dppho, abtso+, oho radical scavenging, metal chelating activity and determination of lipid peroxidation levels (tbars). bae was scavenged 83.49% of the abts radical, 68.34% of the hydroxyl radical, and 68.65% of the dpph radical. this extract was shown 49.36% of the metal chelating activity myricetin (1831.52 mu g/g), kaempferol (104.52 mu g/g), naringenin (2.51 mu g/g), vanillic acid (91.70 mu g/g), caffeic acid (85.92 mu g/g), ferulic acid (27.11 mu g/g) rosmarinic acid (0.95 mu g/g), hydroxycinnamic acid (1.35 mu g/g), delta-tocopherol (4.95 mg/kg), mu-tocopherol (104.15 mg/kg), vitamin k (42.25 mg/kg), beta-sitosterol (366.95 mg/kg) and stigmasterol (242.65 mg/kg) were determined in the bae. the major fatty acids were oleic acid (70.61%) and linoleic acid (20.68%) in the bae. these results indicate that bitter almond can be a good natural source of fatty acids, lipid soluble vitamins, phytosterols, flavonoid, phenolic compounds. (author)

  7. Nutritional composition, bioactive compounds and volatile profile of cocoa beans from different regions of Cameroon.

    Science.gov (United States)

    Caprioli, Giovanni; Fiorini, Dennis; Maggi, Filippo; Nicoletti, Marcello; Ricciutelli, Massimo; Toniolo, Chiara; Prosper, Biapa; Vittori, Sauro; Sagratini, Gianni

    2016-06-01

    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. PMID:27055484

  8. Spectrophotometric determination of bio-active compounds with chloramine-T and gallocyanine.

    Science.gov (United States)

    Sastry, C S; Srinivas, K R; Prasad, K M

    1996-10-01

    A simple, sensitive and selective method for the spectrophotometric determination of drugs, viz., sulphamethoxazole, tetracycline HCl, amidopyrine, nifurtimox and isoniazid and biologically important amino acids, cysteine, aspartic acid and arginine based on their reactivity with chloramine-T (CAT) is proposed. The method involves the addition of excess CAT of a known concentration in the presence of 0.25 M HCl and the determination of the unreacted CAT by measurement of the decrease in the absorbance of the dye, gallocyanine (lambda(max): 540 nm), the most suitable of several dyes that were tested. This method was applied to the determination of drug contents in pharmaceutical formulations and to the measurement of the aspartic acid content of some protein hydrolysates. The method is useful for the determination of the target compounds in microgram quantities from 0.4-5.6 microg mL(-1) with the exceptions of arginine (1.0-8.0 microg mL(-1)) and nifurtimox (0.8-5.6 microg mL(-1)). Standard deviations were typically 0.5 mg per dose (RSD 0.5-1.2%). No interferences were observed from common excipients in formulations, and detailed interference studies of other amino acids in the determination of cysteine, aspartic acid and arginine are reported. The validity of the method was tested against spectrophotometric and titrimetric reference methods. Recoveries were 99.8-102.1%. PMID:18966644

  9. AILANTHUS ALTISSIMA (MILLER SWINGLE: A SOURCE OF BIOACTIVE COMPOUNDS WITH ANTIOXIDANT ACTIVITY

    Directory of Open Access Journals (Sweden)

    Ângelo Luís,

    2012-02-01

    Full Text Available Ailanthus altissima (Miller Swingle is a tree used in Chinese traditional medicine as a bitter aromatic drug and in the treatment of colds and gastric diseases. Previous phytochemical studies have demonstrated the presence of quassinoids in the plant, as well as indole alkaloids. The purpose of this work was to determine the phenolic, flavonoid, and total alkaloid contents of the ethanolic, methanolic, acetone, and hydroalcoholic crude extracts of A. altissima and then try to correlate them with antioxidant activity of corresponding extracts. Moreover, the phenolic compounds present in the extracts were analyzed by RP-HPLC. Extracts from leaves have greater phenolic content than the other parts of this tree. Concerning the extraction process, it is possible to conclude that the mixture of water and ethanol is the best solvent to extract substances with antioxidant activity. Analysis by RP-HPLC showed that ferulic acid was the most dominant hydroxycinnamic acid, with an occurrence percentage of 25.59%. These results presented a positive linear correlation between antioxidant activity index and total phenolic content of all the extracts.

  10. Diversity of Micromonospora strains from the deep Mediterranean Sea and their potential to produce bioactive compounds

    Directory of Open Access Journals (Sweden)

    Andrea Gärtner

    2016-06-01

    Full Text Available During studies on bacteria from the Eastern Mediterranean deep-sea, incubation under in situ conditions (salinity, temperature and pressure and heat treatment were used to selectively enrich representatives of Micromonospora. From sediments of the Ierapetra Basin (4400 m depth and the Herodotos Plain (2800 m depth, 21 isolates were identified as members of the genus Micromonospora. According to phylogenetic analysis of 16S rRNA gene sequences, the Micromonospora isolates could be assigned to 14 different phylotypes with an exclusion limit of ≥ 99.5% sequence similarity. They formed 7 phylogenetic clusters. Two of these clusters, which contain isolates obtained after enrichment under pressure incubation and phylogenetically are distinct from representative reference organism, could represent bacteria specifically adapted to the conditions in situ and to life in these deep-sea sediments. The majority of the Micromonospora isolates (90% contained at least one gene cluster for biosynthesis of secondary metabolites for non-ribosomal polypeptides and polyketides (polyketide synthases type I and type II. The determination of biological activities of culture extracts revealed that almost half of the strains produced substances inhibitory to the growth of Gram-positive bacteria. Chemical analyses of culture extracts demonstrated the presence of different metabolite profiles also in closely related strains. Therefore, deep-sea Micromonospora isolates are considered to have a large potential for the production of new antibiotic compounds.

  11. Moringa oleifera: bioactive compounds and nutritional potential Moringa oleifera: compostos bioativos e potencialidade nutricional

    Directory of Open Access Journals (Sweden)

    Paulo Michel Pinheiro Ferreira

    2008-08-01

    Full Text Available This work aims to review the nutritional properties of the Moringa oleifera tree, emphasizing its main constituents and nutritional applications for humans and animals. Moringa oleifera (Moringaceae is a cosmopolitan tree that grows in many tropical countries showing uncountable folk uses due to its various nutritional and pharmacological applications. The young leaves, flowers and pods are common vegetables in the Asian diet. All parts of this plant are renewable sources of tocopherols (γ and α, phenolic compounds, β-carotene, vitamin C and total proteins, including the essential sulfur amino acids, methionine and cysteine. The seed protein and fat contents are higher than those reported for important grain legumes and soybean varieties, respectively. Unsaturated fatty acids, especially oleic acid, carbohydrates and minerals are present in the seed in reasonable amounts. In general, there are low concentrations of antinutritional factors in the plant, although the seeds possess glucosinolates (65.5µmol/g dry matter, phytates (41g/kg and hemagglutination activity while the leaves have appreciable amounts of saponins (80g/kg, besides low quantity of phytates (21g/kg and tannins (12g/kg. Taking into consideration the excellent nutritional properties, the low toxicity of the seeds and the excellent ability of the plant to adapt to poor soils and dry climates, Moringa oleifera can be an alternative to some leguminous seeds as a source of high-quality protein, oil and antioxidant compounds and a way to treat water in rural areas where appropriate water resources are not available.O objetivo deste trabalho é fazer uma revisão sobre as propriedades nutricionais da planta Moringa oleifera, enfatizando seus principais constituintes e suas aplicações nutricionais para o homem e os animais. Moringa oleifera é uma planta que cresce em muitos países tropicais, possuindo inúmeros usos populares devido às suas aplicações nutricionais e farmacol

  12. Bioactive Compounds, Antioxidant, Xanthine Oxidase Inhibitory, Tyrosinase Inhibitory and Anti-Inflammatory Activities of Selected Agro-Industrial By-products

    Directory of Open Access Journals (Sweden)

    Ehsan Karimi

    2011-11-01

    Full Text Available 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  IC50 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.

  13. Impact of Cultivar on Profile and Concentration of Lipophilic Bioactive Compounds in Kernel Oils Recovered from Sweet Cherry (Prunus avium L.) by-Products.

    Science.gov (United States)

    Górnaś, Paweł; Rudzińska, Magdalena; Raczyk, Marianna; Mišina, Inga; Segliņa, Dalija

    2016-06-01

    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. PMID:26984340

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

    Science.gov (United States)

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

    2012-10-15

    Peppers (Capsicum spp.) are a rich source of diverse bioactive compounds with potential health-promoting properties. This study investigated the extraction efficiency of five solvents on antioxidant activities from cayenne (CA408 and Mesilla), jalapeño (Ixtapa) and serrano (Tuxtlas) pepper cultivars. Freeze-dried peppers were extracted using a Soxhlet extractor with five solvents: hexane, ethyl acetate, acetone, methanol, and methanol:water (80:20). The levels of specific bioactive compounds (phenolics, capsaicinoids, carotenoids and flavonoids) were determined by HPLC and antioxidant activities were assayed by three methods. For all pepper cultivars tested, hexane extracts had the highest levels of capsaicinoids and carotenoids, but methanol extracts had the maximum levels of flavonoids. Hexane extracts showed higher 2,2-diphenyl-1-pricrylhydrozyl (DPPH) radical-scavenging activity and higher reducing power, and acetone extracts (from Mesilla pepper) had a high reducing power. All pepper extracts, except hexane, were effective in preventing deoxyribose degradation, and the inhibition was increased by high concentrations of extracts. The results of the present study indicated that, among the different measures of antioxidant activity, DPPH radical-scavenging activity was strongly correlated with total bioactive compounds (capsaicinoids, carotenoids, flavonoids and total phenolics) in pepper cultivars. PMID:23442638

  15. Volatile compounds from leaves of the African spider plant (Gynandropsis gynandra) with bioactivity against spider mite (Tetranychus urticae)

    DEFF Research Database (Denmark)

    Nyalala, Samuel Odeyo; Petersen, Mikael Agerlin; Grout, Brian William Wilson

    2013-01-01

    volatile compounds were emitted by G. gynandra at significantly higher levels than mite-susceptible pot roses, including isothiocyanates, aldehydes, esters, alcohols and terpenes. Six representative compounds were selected to assess bioactivity. Spider mite populations were completely inactive after a 2¿h......Previous studies have demonstrated that Gynandropsis gynandra emits acetonitrile as a foliar volatile from intact plants and isolated leaves, and that this compound is an effective spider mite repellent. This study has used gas chromatography–mass spectrometry to investigate volatile compounds...... emitted from homogenised G. gynandra leaves to evaluate their tissue acetonitrile content and to look for other compounds that might be exploited for the management of spider mites. Acetonitrile was absent from the homogenised tissues of five lines of G. gynandra, studied over two seasons. Thirteen...

  16. Screening of antitubercular compound library identifies novel shikimate kinase inhibitors of Mycobacterium tuberculosis.

    Science.gov (United States)

    Rajput, Vikrant S; Mehra, Rukmankesh; Kumar, Sanjay; Nargotra, Amit; Singh, Parvinder Pal; Khan, Inshad Ali

    2016-06-01

    Shikimate kinase of Mycobacterium tuberculosis is involved in the biosynthesis of aromatic amino acids through shikimate pathway. The enzyme is essential for the survival of M. tuberculosis and is absent from mammals, thus providing an excellent opportunity for identifying new chemical entities to combat tuberculosis with a novel mechanism of action. In this study, an antitubercular library of 1000 compounds was screened against M. tuberculosis shikimate kinase (MtSK). This effort led to the identification of 20 inhibitors, among which five promising leads exhibited half maximal inhibitory concentration (IC50) values below 10 μM. The most potent inhibitor ("5631296") showed an IC50 value of 5.10 μM ± 0.6. The leads were further evaluated for the activity against multidrug-resistant (MDR)-TB, Gram-positive and Gram-negative bacterial strains, mode of action, docking simulations, and combinatorial study with three frontline anti-TB drugs. Compound "5491210" displayed a nearly synergistic activity with rifampicin, isoniazid, and ethambutol while compound "5631296" was synergistic with rifampicin. In vitro cytotoxicity against HepG2 cell line was evaluated and barring one compound; all were found to be non-toxic (SI > 10). In order to rule out mitochondrial toxicity, the promising inhibitors were also evaluated for cell cytotoxicity using galactose medium where compounds "5631296" and "5122752" appeared non-toxic. Upon comprehensive analysis, compound "5631296" was found to be the most promising MtSK inhibitor that was safe, synergistic with rifampicin, and bactericidal against M. tuberculosis. PMID:26887318

  17. Essential oil of Mitracarpus frigidus as a potent source of bioactive compounds

    Directory of Open Access Journals (Sweden)

    Rodrigo L. Fabri

    2012-12-01

    Full Text Available In our previous work (Fabri et al. 2009, we showed that different extracts of Mitracarpus frigidus had significant antibacterial, antifungal and leishmanicidal activities. In order to increase our knowledge about this species, this work assesses the chemical composition and the in vitro biological activity of its essential oil. Thus, the essential oil obtained by hydrodistillation of the aerial parts of M. frigidus was analyzed by GC/MS. Among several compounds detected, 11 were identified, being linalool and eugenol acetate the major components. The essential oil exhibited a moderate antibacterial effect against Staphyloccocus aureus, Bacillus cereus, Pseudomonas aeruginosa and Enterobacter cloacae (MIC 250 µg/mL. On the other hand, it showed a strong antifungal effect against Cryptoccocus neoformans (MIC 8 µg/mL and Candida albicans (MIC 63 µg/mL. Expressive activity against L. major and L. amazonensis promastigote forms with IC50 values of 47.2 and 89.7 µg/mL, respectively, were also observed. In addition, the antioxidant activity was investigated through DPPH radical-scavenging and showed a significative activity with IC50 of 38 µg/mL. The cytotoxicity against Artemia salina was moderate with LC50 of 88 µg/mL. The results presented here are the first report on the chemical composition and biological properties of M. frigidus essential oil.Em nosso trabalho anterior (Fabri et al. 2009, mostramos que diferentes extratos de Mitracarpus frigidus apresentaram atividades antibacteriana, antifúngica e leishmanicida significativas. Com o objetivo de aprofundar o conhecimento sobre essa espécie, esse trabalho objetiva identificar os constituintes químicos e avaliar as atividades biológicas in vitro de seu óleo essencial. Dessa forma, o óleo essencial das partes aéreas de M.frigidus foi obtido por hidrodestilação e analisado por CG/EM. Entre os compostos detectados, 11 foram identificados, sendo linalol e o acetato de eugenol os

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

    Science.gov (United States)

    Bower, Allyson M; Real Hernandez, Luis M; Berhow, Mark A; de Mejia, Elvira Gonzalez

    2014-07-01

    Greek oregano (Origanum vulgare), marjoram (Origanum majorana), rosemary (Rosmarinus officinalis), and Mexican oregano (Lippia graveolens) are concentrated sources of bioactive compounds. The aims were to characterize and examine extracts from greenhouse-grown or commercially purchased herbs for their ability to inhibit dipeptidyl peptidase IV (DPP-IV) and protein tyrosine phosphatase 1B (PTP1B), enzymes that play a role in insulin secretion and insulin signaling, respectively. Greenhouse herbs contained more polyphenols (302.7-430.1 μg of gallic acid equivalents/mg of dry weight of extract (DWE)) and flavonoids (370.1-661.4 μg of rutin equivalents/mg of DWE) compared to the equivalent commercial herbs. Greenhouse rosemary, Mexican oregano, and marjoram extracts were the best inhibitors of DPP-IV (IC₅₀=16, 29, and 59 μM, respectively). Commercial rosemary, Mexican oregano, and marjoram were the best inhibitors of PTP1B (32.4-40.9% at 500 μM). The phytochemicals eriodictyol, naringenin, hispidulin, cirsimaritin, and carnosol were identified by LC-ESI-MS as being present in greenhouse-grown Mexican oregano and rosemary. Computational modeling indicated that hispidulin, carnosol, and eriodictyol would have the best binding affinities for DPP-IV. Biochemically, the best inhibitors of DPP-IV were cirsimaritin (IC₅₀=0.43±0.07 μM), hispidulin (IC₅₀=0.49±0.06 μM), and naringenin (IC₅₀=2.5±0.29 μM). Overall, herbs contain several flavonoids that inhibit DPP-IV and should be investigated further regarding their potential in diabetes management. PMID:24881464

  19. Bioactive compounds from Paecilomyces tenuipes regulating the function of the hypothalamo-hypophyseal system axis in chronic unpredictable stress rats

    Institute of Scientific and Technical Information of China (English)

    YIN Yan-yan; MING Liang; ZHENG Li-fang; KAN Hong-wei; LI Chun-ru; LI Wei-ping

    2007-01-01

    Background A bioactive compound from Paecilomyces tenuipes (BGPT) has an inhibitory effect on monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) in vitro and in vivo, which indicates BCPT may be a potential antidepressant. In this study we aimed to study the antidepressant effects of BCPT in the chronic unpredictable stress(CUS) model in rats and explore underlying mechanisms in the hypothalamic-pituitary-adrenal (HPA) axis.Methods The antidepressant effects of BCPT were studied in the chronic unpredictable stress model in rats. Animals were housed isolated, except the control group. Rats were exposed daily to different random stressors from day 1 to 21.Awarding response was detected by calculating the 24-hour consumption of sucrose water. Cortisol (CORT) and adrenocorticotropic hormone (ATCH) contents in serum and arginine vasopressin (AVP) contents in the pituitary body were detected by radio immunoassays. Total RNA of hippocampus or hypothalamus was extracted and subjected to reverse transcription-polymerase chain reaction (RT-PCR) for the measurement of corticotrophin releasing hormone(CRH) mRNA or mineralocorticoid receptor (MR) mRNA and glucocorticoid receptor (GR) mRNA levels. Statistical analyses were performed using one way analysis of variance (ANOVA) followed by Student-Newman-Keuls (SNK) test.Results Chronic unpredictable stress resulted in reduction of sensitivity to reward and abnormality in the HPA axis in the animal model. BCPT improved the reward reaction as measured by increasing sucrose consumption, remarkably reduced serum CORT and ACTH levels and the AVP content in the pituitary body in the CUS-treated rats, decreased the expression of CRH mRNA, enhanced the expression of hippocampus MR mRNA, GR mRNA and decreased the ratio of MR/GR.Conclusions BCPT has potentially antidepressant-like activity and normalized the HPA axis hyperactivity in a CUS model of depression in rats. This may be an important mechanism of its antidepressant effect.

  20. Bioactivation of particles

    Science.gov (United States)

    Pinaud, Fabien; King, David; Weiss, Shimon

    2011-08-16

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

  1. The utilization of some coordination compounds of V(IV and Co(III as regulators of the content of bioactive substances with antioxidant properties at Spirulina platensis

    Directory of Open Access Journals (Sweden)

    Valentina BULIMAGA

    2011-05-01

    Full Text Available Investigation of non-traditional sources of bioactive substances is one of the current directions of biotechnology development in many countries worldwide. This paper reports on the study of possibility of utilization of some coordination compounds of V(IV and Co(III as regulators of the content of bioactive substances with antioxidant properties: superoxiddismutase (SOD, phycobiliproteins, carotenoids and lipids in the biomass of cyanobacterium Spirulina platensis. Natural antioxidants possess a broad spectrum of biological activity due to the ability to neutralize the negative effects of free radicals in living organisms. The obtained experimental results demonstrate that utilization of some coordination compounds of V(IV at the spirulina cultivation contribute to the accumulation of β-carotene and lipids in spirulina biomass, as well as metallocomplexes of Co(III have the beneficial effect on the content of phycobiliproteins, lipids and activity of SOD. The present study reveals that obtained biomass of cyanobacterium Spirulina platensis with high content of bioactive substances with antioxidant properties can be used for the elaboration of medical remedies for prophylaxis and treatment of diseases, caused by the negative effect of oxidative stress on live organisms and, also, for the elaboration of cosmetic preparations for the prevention of premature skin aging, protection against solar radiation and treatment of skin diseases.

  2. Effect of Stevia rebaudiana addition on bioaccessibility of bioactive compounds and antioxidant activity of beverages based on exotic fruits mixed with oat following simulated human digestion.

    Science.gov (United States)

    Carbonell-Capella, Juana M; Buniowska, Magdalena; Esteve, María J; Frígola, Ana

    2015-10-01

    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. PMID:25872434

  3. Relationship between the elemental composition of grapeyards and bioactive compounds in the Cabernet Sauvignon grapes Vitis vinífera harvested in Mexico.

    Science.gov (United States)

    Acuña-Avila, Pedro Estanislao; Vásquez-Murrieta, María Soledad; Franco Hernández, Marina Olivia; López-Cortéz, Ma del Socorro

    2016-07-15

    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. PMID:26948592

  4. Molecular descriptor data explain market prices of a large commercial chemical compound library

    Science.gov (United States)

    Polanski, Jaroslaw; Kucia, Urszula; Duszkiewicz, Roksana; Kurczyk, Agata; Magdziarz, Tomasz; Gasteiger, Johann

    2016-06-01

    The relationship between the structure and a property of a chemical compound is an essential concept in chemistry guiding, for example, drug design. Actually, however, we need economic considerations to fully understand the fate of drugs on the market. We are performing here for the first time the exploration of quantitative structure-economy relationships (QSER) for a large dataset of a commercial building block library of over 2.2 million chemicals. This investigation provided molecular statistics that shows that on average what we are paying for is the quantity of matter. On the other side, the influence of synthetic availability scores is also revealed. Finally, we are buying substances by looking at the molecular graphs or molecular formulas. Thus, those molecules that have a higher number of atoms look more attractive and are, on average, also more expensive. Our study shows how data binning could be used as an informative method when analyzing big data in chemistry.

  5. Bioactive Compounds in Meat

    Science.gov (United States)

    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.

  6. Panel docking of small-molecule libraries - Prospects to improve efficiency of lead compound discovery.

    Science.gov (United States)

    Sarnpitak, Pakornwit; Mujumdar, Prashant; Taylor, Paul; Cross, Megan; Coster, Mark J; Gorse, Alain-Dominique; Krasavin, Mikhail; Hofmann, Andreas

    2015-11-01

    Computational docking as a means to prioritise small molecules in drug discovery projects remains a highly popular in silico screening approach. Contemporary docking approaches without experimental parametrisation can reliably differentiate active and inactive chemotypes in a protein binding site, but the absence of a correlation between the score of a predicted binding pose and the biological activity of the molecule presents a clear limitation. Several novel or improved computational approaches have been developed in the recent past to aid in screening and profiling of small-molecule ligands for drug discovery, but also more broadly in developing conceptual relationships between different protein targets by chemical probing. Among those new methodologies is a strategy known as inverse virtual screening, which involves the docking of a compound into different protein structures. In the present article, we review the different computational screening methodologies that employ docking of atomic models, and, by means of a case study, present an approach that expands the inverse virtual screening concept. By computationally screening a reasonably sized library of 1235 compounds against a panel of 48 mostly human kinases, we have been able to identify five groups of putative lead compounds with substantial diversity when compared to each other. One representative of each of the five groups was synthesised, and tested in kinase inhibition assays, yielding two compounds with micro-molar inhibition in five human kinases. This highly economic and cost-effective methodology holds great promise for drug discovery projects, especially in cases where a group of target proteins share high structural similarity in their binding sites. PMID:26025037

  7. Bioactive compounds and antifungal activity of three different seaweed species Ulva lactuca, Sargassum tenerrimum and Laurencia obtusa collected from Okha coast, Western India

    Directory of Open Access Journals (Sweden)

    Megha Barot

    2016-04-01

    Full Text Available Objective: To evaluate bioactive compounds responsible for antifungal activity from seaweeds of Okha coast, Western India. Methods: Each species were extracted with different solvents with increasing polarity: hexane, ethyl acetate, chloroform and methanol using Soxhlet apparatus. The antifungal activity was determined by agar diffusion plate method by using fluconazole, ketoconazole and amphotericin B as standards. Gas chromatography-mass spectrometer analysis was done for identification of bioactive compounds present in crude extract. Results: The gas chromatography-mass spectrometer analysis of all the extracts revealed the presence of steroids, fatty acids and esters compounds. Among the three species, the maximum crude extract yield (53.46% and the largest inhibition zone (36 mm were recorded in methanol extract of Ulva lactuca, whereas the minimum crude extract yield and inhibition zone were recorded in chloroform extract of the same species as 0.5% and 10 mm, respectively. Methanol and ethyl acetate extract showed the maximum antifungal activity and the major important compounds like steroids, fatty acids and esters were detected with higher amount in all the extracts. Conclusions: The present study revealed that the different seaweed extracts showed moderate to significant antifungal activity against the strains tested as compared with the standard fungicides, and polar solvents methanol and ethyl acetate were comparatively efficient for extraction of different metabolites that are responsible for antifungal activity.

  8. Bio-active Compounds of Bitter Melon Genotypes (Momordica charantia L. in Relation to Their Physiological Functions

    Directory of Open Access Journals (Sweden)

    Navam S. Hettiarachchy

    2011-02-01

    protein, most of the essential amino acid contents of Bitter Melon were similar as in soy proteins. Some amino acids such as Alanine, Glycine, and Valanine were relatively higher in Bitter Melon flesh than in soy protein. Phenolics contents of the flesh, seed, and seed coat tissue [SCT] were significantly different [p<0.05] among the four varieties. The four varieties were similar in their antioxidant activities of the flesh tissues; however, they were significantly different in their antioxidant activities in the seed and seed coat tissues [SCT]. Bitter melon varieties IW and CG, tested for antimutagenic effects, both flesh and seed had considerably high activities against benzo[a]pyrene with Salmonella TA98 [92-100% inhibition] and Salmonella TA100 [79-86% inhibition].Conclusion: Based on these studies, Bitter Melon is a good source of phenolic compounds. All four varieties tested showed considerably high antioxidant and antimutagenic activities. Therefore, these natural plant phenolics can be a good source of biologically active compounds that may be applied in many food systems to enhance food values and special nutritional qualities. Further studies will be needed using more genetically diverse varieties to pin point the bioactive and functional compounds and their physiological properties.

  9. Compostos bioativos presentes em amora-preta (Rubus spp. Bioactive compounds of blackberry fruits (Rubus spp. grown in Brazil

    Directory of Open Access Journals (Sweden)

    Daniela Souza Ferreira

    2010-09-01

    and, or, inhibitors of degenerative disorders; however, data regarding the bioactive compounds in blackberry cultivated in Brazil are rare. Thus, the objectives of the present study were to identify the anthocyanins and carotenoids in blackberry (Rubus spp., to determine the total contents of phenolic compounds, flavonoids, carotenoids, and total, monomeric, polimeric and co-pigmented anthocyanins, and the antioxidant capacity against the free radicals ABTS and DPPH. The total carotenoids level was low (86.5 ± 0.2 µg/100 g, with all-trans-β-carotene (39.6 % and all-trans-lutein (28.2 % as the major ones. The blackberries showed high antioxidant status mainly due to the high level of monomeric anthocyanins (104.1 ± 1.8 mg/100 g de fruta, presence of polimeric anthocyanins (22.9 ± 0.4 %, low percentage of co-pigmented anthocyanins (1.6 ± 0.1 % and high contents of phenolic compounds (241.7 ± 0.8 mg gallic acid equivalent/100 g and total flavonoids (173.7 ± 0.7 mg catechin equivalent/100 g. Cyanidin 3-glucoside was the major anthocyanin (92.9 %. These results indicate that the blackberry cultivated in Brazil can be considered a rich natural source of antioxidants and pigments.

  10. Inhibition of Listeria monocytogenes ATCC 19115 on ham steak by tea bioactive compounds incorporated into chitosan-coated plastic films

    Directory of Open Access Journals (Sweden)

    Vodnar Dan C

    2012-07-01

    Full Text Available Abstract Background The consumer demands for better quality and safety of food products have given rise to the development and implementation of edible films. The use of antimicrobial films can be a promising tool for controlling L. monocytogenes on ready to eat products. The aim of this study was to develop effective antimicrobial films incorporating bioactive compounds from green and black teas into chitosan, for controlling L. monocytogenes ATCC 19115 on vacuum-packaged ham steak. The effectiveness of these antimicrobial films was evaluated at room temperature (20°C for 10 days and at refrigerated temperature (4°C for 8 weeks. Results The HPLC results clearly show that relative concentrations of catechins and caffeine in green tea ranked EGCG>EGC>CAF>ECG>EC>C while in black tea extracts ranked CAF>EGCG>ECG>EGC>EC>C. The chitosan-coated plastic films incorporating green tea and black tea extracts shows specific markers identified by FTIR. Incorporating natural extracts into chitosan showed that the growth of L monocytogenes ATCC 19115 was inhibited. The efficacy of antimicrobial effect of tea extracts incorporated into chitosan-coated plastic film was dose dependent. However, chitosan-coated films without addition of tea extracts did not inhibit the growth of L. monocytogenes ATCC 19115. Chitosan-coated plastic films incorporating 4% Green tea extract was the most effective antimicrobial, reducing the initial counts from 3.2 to 2.65 log CFU/cm2 during room temperature storage and from 3.2 to 1–1.5 log CFU/cm2 during refrigerated storage. Conclusions Incorporation of tea extracts into the chitosan-coated films considerably enhanced their effectiveness against L. monocytogenes ATCC 19115. 4% Green tea incorporated into chitosan-coated plastic film had a better antilisterial effect than 2% green tea or 2% and 4% black tea. Data from this study would provide new formulation options for developing antimicrobial packaging films using tea

  11. An Automated Microwave-Assisted Synthesis Purification System for Rapid Generation of Compound Libraries.

    Science.gov (United States)

    Tu, Noah P; Searle, Philip A; Sarris, Kathy

    2016-06-01

    A novel methodology for the synthesis and purification of drug-like compound libraries has been developed through the use of a microwave reactor with an integrated high-performance liquid chromatography-mass spectrometry (HPLC-MS) system. The strategy uses a fully automated synthesizer with a microwave as energy source and robotic components for weighing and dispensing of solid reagents, handling liquid reagents, capper/crimper of microwave reaction tube assemblies, and transportation. Crude reaction products were filtered through solid-phase extraction cartridges and injected directly onto a reverse-phase chromatography column via an injection valve. For multistep synthesis, crude products were passed through scavenger resins and reintroduced for subsequent reactions. All synthetic and purification steps were conducted under full automation with no handling or isolation of intermediates, to afford the desired purified products. This approach opens the way to highly efficient generation of drug-like compounds as part of a lead discovery strategy or within a lead optimization program. PMID:26085482

  12. Comparison of the levels of bioactive benzoxazinoids in different wheat and rye fractions and the transformation of these compounds in homemade foods

    DEFF Research Database (Denmark)

    Tanwir, Fariha; Fredholm, Maria; Gregersen, Per L.;

    2013-01-01

    Benzoxazinoids are important phytochemicals found in wheat and rye that are associated with plant resistance against pathogens, and recent studies have emphasized the potential health-promoting role of these compounds i.e. anti-cancer, anti-allergy and anti-inflammation. Accordingly, an understan......Benzoxazinoids are important phytochemicals found in wheat and rye that are associated with plant resistance against pathogens, and recent studies have emphasized the potential health-promoting role of these compounds i.e. anti-cancer, anti-allergy and anti-inflammation. Accordingly, an...... analysis of seed fractions obtained from the milling of wheat and rye showed significantly higher concentrations of these bioactive compounds in the germ than in the other fractions, i.e. the bran and endosperm. Di-hexoses of 2,4-dihydroxy-1, 4-benzoxazin-3-one (DIBOA-glc-hexose) and 2-hydroxy-1, 4...

  13. Effect of the Production of Dried Fruits and Juice from Chokeberry (Aronia melanocarpa L.) on the Content and Antioxidative Activity of Bioactive Compounds.

    Science.gov (United States)

    Oszmiański, Jan; Lachowicz, Sabina

    2016-01-01

    The aim of this study was to evaluate the production of dried fruits and juices from chokeberry as potential sources of bioactive compounds with beneficial effects on human health. Dry powders and juices from chokeberry were analyzed for the contents of sugars with high-performance liquid chromatography coupled with an evaporative light scattering detector (HPLC-ELSD method), and the antioxidant capacity was analyzed by the FRAP (ferric-reducing ability of plasma) and ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid)) tests. Polyphenols were identified by high performance liquid chromatography (HPLC) coupled with a tandem mass spectrometer and a photodiode-array detector (LC-PDA-ESI-MS/MS), and their quantitative analysis was carried out by UPLC-MS/MS (using a Q/TOF detector and a PDA detector). A total of 27 polyphenolic compounds was identified in chokeberry products, including 7 anthocyanins, 11 flavonols, 5 phenolic acids, 3 flavan-3-ols and 1 flavanone. Three anthocyanin derivatives were reported for the first time from chokeberry fruit. A higher activity of the bioactive compounds was determined in dried fruit pomace and in juice obtained from crushed fruits than in those from the whole fruits. In addition, the pomace was found to be a better material for the production of dry powders, compared to chokeberry fruits. PMID:27556441

  14. Synthesis of hexahydropyrrolo[2,1-a]isoquinoline compound libraries through a Pictet–Spengler cyclization/metal-catalyzed cross coupling/amidation sequence

    DEFF Research Database (Denmark)

    Petersen, Rico; Cohrt, A. Emil; Petersen, Michael Åxman;

    2015-01-01

    Molecular libraries of natural product-like and structurally diverse compounds are attractive in early drug discovery campaigns. In here, we present synthetic methodology for library production of hexahydropyrrolo[2,1-a]isoquinoline (HPIQ) compounds. Two advanced HPIQ intermediates, both incorpor...

  15. Antiaggregation Potential of Padina gymnospora against the Toxic Alzheimer's Beta-Amyloid Peptide 25-35 and Cholinesterase Inhibitory Property of Its Bioactive Compounds.

    Directory of Open Access Journals (Sweden)

    Balakrishnan Shanmuganathan

    Full Text Available 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.

  16. Bioactive compounds contents, antioxidant and antimicrobial activities during ripening of Prunus persica L. varieties from the North West of Tunisia.

    Science.gov (United States)

    Belhadj, Feten; Somrani, Imen; Aissaoui, Neyssene; Messaoud, Chokri; Boussaid, Mohamed; Marzouki, M Nejib

    2016-08-01

    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. PMID:26988472

  17. Metabolomic-Based Study of the Leafy Gall, the Ecological Niche of the Phytopathogen Rhodococcus fascians, as a Potential Source of Bioactive Compounds

    Directory of Open Access Journals (Sweden)

    Pierre Duez

    2013-06-01

    Full Text Available 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.

  18. Pre-harvest treatments of pepper plants with nitrophenolates increase crop yield and enhance nutritive and bioactive compounds in fruits at harvest and during storage.

    Science.gov (United States)

    Valero, D; Zapata, P J; Martínez-Romero, D; Guillén, F; Castillo, S; Serrano, M

    2014-06-01

    Pepper plants (Capsicum annuum L. cv Lamuyo) were treated with a mix of nitrophenolates either by foliar spray or in the irrigation system, and its effect on crop yield and the content of nutritive and bioactive compounds in fruit were analysed at harvest and after post-harvest storage. Treatments were applied at 2-week intervals from the development of first floral bunch (1 March) to end of August. Pepper fruits were harvested at commercial ripening stage (red surface colour) along the growth cycle (from May to September). Total yield (cumulative kilogram per plant) was increased ( 4.5% more) by nitrophenolate treatments due to significant increases in fruit mass, although the number of fruits per plant was unaffected. Pepper fruit quality (weight, firmness and pericarp thickness), its content in nutritive (sugars and organic acids) and bioactive compounds (vitamin C and total phenolics) and antioxidant activity were also enhanced by nitrophenolate treatments at the three harvested dates assayed (end May, mid July and end August). In addition, all these parameters were maintained at higher levels in treated peppers during storage, while diminutions in these parameters occurred generally in control fruit. Thus, nitrophenolate treatments were able to improve crop yield as well as the nutritional value and antioxidant properties of peppers at harvest and after fruit storage. PMID:23751541

  19. Antiproliferative activity and apoptosis induction of Eucalyptus Citriodora resin and its major bioactive compound in melanoma B16F10 cells.

    Science.gov (United States)

    Duh, Pin-Der; Chen, Zong-Tsi; Lee, Shwu-Woan; Lin, Tsuey-Pin; Wang, Ya-Ting; Yen, Wen-Jye; Kuo, Ling-Feng; Chu, Heuy-Ling

    2012-08-15

    Antiproliferative activity and apoptosis induction of ethyl acetate of Eucalyptus citriodora resin (EAEER), and its major bioactive compound in melanoma B16F10 cells were investigated. 6-[1-(p-Hydroxy-phenyl)ethyl]-7-O-methyl aromadendrin (HEMA), a flavanol derivative, was isolated from EAEER and identified on the basis of its mass and NMR spectra. The results from MTT assay showed high antiproliferative effects of EAEER and HEMA on B16F10 cells. Moreover, EAEER- and HEMA-induced cell apoptosis was association with the decrease in the mitochondrial transmembrane potentials (Δψ(m)), increase in Bax/Bcl-2 ratio, and activation of caspase-3. Cells treated with EAEER and HEMA generated intracellular reactive oxygen species (ROS) and nitric oxide (NO), indicating that ROS and RNS play important roles in the induction of apoptosis in B16F10 cells. Taken together, EAEER and its major bioactive compound, HEMA, inhibited the proliferation of B16F10 cells via apoptosis and may be a potential antimelanoma agent. PMID:22838509

  20. Impact of high pressure processing on color, bioactive compounds, polyphenol oxidase activity, and microbiological attributes of pumpkin purée.

    Science.gov (United States)

    González-Cebrino, Francisco; Durán, Rocío; Delgado-Adámez, Jonathan; Contador, Rebeca; Bernabé, Rosario Ramírez

    2016-04-01

    Physicochemical parameters, bioactive compounds' content (carotenoids and total phenols), total antioxidant activity, and enzymatic activity of polyphenol oxidase (PPO) were evaluated after high pressure processing (HPP) on a pumpkin purée (cv. 'Butternut'). Three pressure levels (400, 500, and 600 MPa) were combined with three holding times (200, 400, and 600 s). The applied treatments reduced the levels of total aerobic mesophilic (TAM), total psychrophilic and psychrotrophic bacteria (TPP), and molds and yeasts (M&Y). All applied treatments did not affect enzymatic activity of PPO. Pressure level increased CIE L* values, which could enhance the lightness perception of high pressure (HP)-treated purées. No differences were found between the untreated and HP-treated purées regarding total phenols and carotenoids content (lutein, α-carotene, and β-carotene) and total antioxidant activity. HPP did not affect most quality parameters and maintained the levels of bioactive compounds. However, it did not achieve the complete inhibition of PPO, which could reduce the shelf-life of the pumpkin purée. PMID:26123635

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

    Science.gov (United States)

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

    2016-05-13

    In the current study, response surface methodology (RSM) was used to assess the effects of extraction time and temperature on the content of bioactive compounds and antioxidant activity of purple basil leaf (Ocimum basilicum L.) extracts. The stability of anthocyanins in relation to temperature, light and copigmentation was also studied. The highest anthocyanin content was 67.40 mg/100 g extracted at 30 °C and 60 min. The degradation of anthocyanins with varying temperatures and in the presence of light followed a first-order kinetics and the activation energy was 44.95 kJ/mol. All the extracts exposed to light showed similar half-lives. The extracts protected from light, in the presence of copigments, showed an increase in half-life from 152.67 h for the control to 856.49 and 923.17 h for extract in the presence of gallic acid and phytic acid, respectively. These results clearly indicate that purple basil is a potential source of stable bioactive compounds. PMID:27192193

  2. The Cooking Effect on Two Edible Mushrooms in Anatolia: Fatty Acid Composition, Total Bioactive Compounds, Antioxidant and Anticholinesterase Activities

    Directory of Open Access Journals (Sweden)

    Mehmet Öztürk

    2014-03-01

    Full Text Available The effects of baking practices on the fatty acid and bioactivity of edible mushrooms; namely, Lactarius delicious and Ramaria flava, naturally growing in Anatolia were investigated. Each mushroom species was divided into two parts and one of the parts was baked. Both baked and unbaked materials were extracted with hexane and methanol, successively. The fatty acid contents of baked and unbaked extracts of both species were carried out by GC and GC-MS analytical techniques. In the unbaked extracts palmitic acid (9.7-14.43%, stearic acid (41.41-6.68%, oleic acid (25.94-47.12% and linoleic acid (22.85-9.78% were identified as major fatty acids, respectively. In the baked extracts, however, palmitic acid (7.92-19.12%, stearic acid (49.94-6.23%, oleic acid (18.07-45.13% and linoleic acid (23.36-9.25% were identified as major fatty acids, as well. The antioxidative effect of the extracts of baked and unbaked mushroom species was also determined by using four complimentary assays. In addition, the extracts and the major fatty acids were also evaluated for anticholinesterase activity against acetylcholinesterase (AChE and butyrylcholinesterase (BChE which are the chief enzymes of Alzheimer’s disease. The baked methanol extract of R. flava showed the highest activity in DPPH scavenging, ABTS scavenging and BChE assays, while the unbaked hexane extract of R. flava exhibited the best lipid peroxidation inhibition activity. In conclusion, baking proved to have influence in nutritional values and bioactivity properties of L. delicious and R. flava. The nutrient concentration and bioactivities of L. delicious were decreased when baked; however, baked R. flava proved to have higher nutrient concentrations and higher bioactivities than unbaked samples.

  3. Bioactive compounds in green tea leaves attenuate the injury of retinal ganglion RGC-5 cells induced by H2O2 and ultraviolet radiation.

    Science.gov (United States)

    Jin, Jianchang; Ying, Hao; Huang, Meirong; Du, Qizhen

    2015-11-01

    The Chinese commonly believe that tea helps maintain clear vision. This viewpoint has been recorded in Chinese medical books also. The key bioactive compounds in green tea leaves, (-)-epigallocatechin gallate (EGCG), L-theanine (theanine) and caffeine, were investigated for their abilities to attenuate the injury of retinal ganglion cells (RGC-5) induced by H2O2 and ultraviolet radiation. Theanine and caffeine promoted cell growth while concentrations of EGCG greater than 10μg/ml inhibited cell growth. The nine and caffeine both protected RGC-5 cells from injury as well as enhanced their recovery, while EGCG only protected the cells from injury and did not help them to recover. Tea is a unique drink, which is simultaneously enriched with EGCG, theanine and caffeine. The role of these compounds in optic nerve protection may partially explain why some tea drinkers feel enhanced vision. PMID:26687755

  4. Technological characteristics and selected bioactive compounds of Opuntia dillenii cactus fruit juice following the impact of pulsed electric field pre-treatment.

    Science.gov (United States)

    Moussa-Ayoub, Tamer E; Jaeger, Henry; Youssef, Khaled; Knorr, Dietrich; El-Samahy, Salah; Kroh, Lothar W; Rohn, Sascha

    2016-11-01

    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. PMID:27211645

  5. Correlation, by multivariate statistical analysis, between the scavenging capacity against reactive oxygen species and the bioactive compounds from frozen fruit pulps

    Directory of Open Access Journals (Sweden)

    Lizziane Cynara Vissotto

    2013-02-01

    Full Text Available The contents of total phenolic compounds (TPC, total flavonoids (TF, and ascorbic acid (AA of 18 frozen fruit pulps and their scavenging capacities against peroxyl radical (ROO•, hydrogen peroxide (H2O2, and hydroxyl radical (•OH were determined. Principal Component Analysis (PCA showed that TPC (total phenolic compounds and AA (ascorbic acid presented positive correlation with the scavenging capacity against ROO•, and TF (total flavonoids showed positive correlation with the scavenging capacity against •OH and ROO• However, the scavenging capacity against H2O2 presented low correlation with TF (total flavonoids, TPC (total phenolic compounds, and AA (ascorbic acid. The Hierarchical Cluster Analysis (HCA allowed the classification of the fruit pulps into three groups: one group was formed by the açai pulp with high TF, total flavonoids, content (134.02 mg CE/100 g pulp and the highest scavenging capacity against ROO•, •OH and H2O2; the second group was formed by the acerola pulp with high TPC, total phenolic compounds, (658.40 mg GAE/100 g pulp and AA , ascorbic acid, (506.27 mg/100 g pulp contents; and the third group was formed by pineapple, cacao, caja, cashew-apple, coconut, cupuaçu, guava, orange, lemon, mango, passion fruit, watermelon, pitanga, tamarind, tangerine, and umbu pulps, which could not be separated considering only the contents of bioactive compounds and the scavenging properties.

  6. Bioactive berry phenolics

    OpenAIRE

    Heinonen, Marina

    2007-01-01

    Compositional data on phenolic compounds in berries has been rapidly accumulating and readily included in the national food composition data base. Among the different bioactive substances in berries, phenolic compounds including flavonoids, tannins, and phenolic acids have received considerable interest due to their effects in food and health.

  7. A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen

    OpenAIRE

    2009-01-01

    Background Regulators of G protein signaling (RGSs) accelerate GTP hydrolysis by Gα subunits and profoundly inhibit signaling by G protein-coupled receptors (GPCRs). The distinct expression patterns and pathophysiologic regulation of RGS proteins suggest that inhibitors may have therapeutic potential. We recently described a focused one-bead, one-compound (OBOC) library screen to identify peptide inhibitors of RGS4. Here we extend our observations to include another peptide with a different m...

  8. Bioactive substances

    Digital Repository Service at National Institute of Oceanography (India)

    Wahidullah, S.

    Chemistry related to certain bioactive molecules, from Indian Ocean Region, developed into drugs or which served as models for the synthesis of more effective bioactive substances or in use in fundamental studies of physiological and biochemical...

  9. Identification of bioactive candidate compounds responsible for oxidative challenge from hydro-ethanolic extract of Moringa oleifera leaves.

    Science.gov (United States)

    Karthivashan, Govindarajan; Tangestani Fard, Masoumeh; Arulselvan, Palanisamy; Abas, Faridah; Fakurazi, Sharida

    2013-09-01

    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. PMID:24024688

  10. Characterization of Bioactive Compounds in Tunisian Bitter Orange (Citrus aurantium L.) Peel and Juice and Determination of Their Antioxidant Activities

    OpenAIRE

    Brahim Marzouk; Iness Jabri karoui

    2013-01-01

    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 representin...

  11. Simultaneous quantification of 50 bioactive compounds of the traditional Chinese medicine formula Gegen-Qinlian decoction using ultra-high performance liquid chromatography coupled with tandem mass spectrometry.

    Science.gov (United States)

    Wang, Qi; Song, Wei; Qiao, Xue; Ji, Shuai; Kuang, Yi; Zhang, Zheng-Xiang; Bo, Tao; Guo, De-An; Ye, Min

    2016-07-01

    The quality evaluation of patent drugs derived from traditional Chinese medicine (TCM) compound formulas has been challenging due to their complex chemical composition. In this study, we developed a solution to evaluate the quality of Gegen-Qinlian Decoction (GQD), an ancient four-herb TCM formula for the treatment of diarrhea and diabetes, together with its derived patent drugs by simultaneously quantifying 50 bioactive compounds. The samples were extracted by 100% methanol (for hydrophobic compounds) and 50% methanol in water (for hydrophilic compounds), respectively, and were separated on a Waters Acquity charged surface hybrid C18 column (2.1×100mm, 1.7μm) eluted with gradients of acetonitrile and water containing 0.1% formic acid at a flow rate of 400μL/min. The analytes were determined by ultra-high performance liquid chromatography coupled with tandem mass spectrometry in the selected reaction monitoring mode. The 50 compounds (including acidic and alkaline, hydrophilic and hydrophobic) were well resolved within 14min, and were determined using an internal standard method. The method was fully validated for precision, repeatability, and recovery. The limits of detection were 0.3-10.0ng/mL. Finally, this method was used to analyze 24 batches of GQD samples, including water decoction, pills, tablets, and oral solutions. Principal component analysis indicated significantly varied chemical compositions among these formulations. The tablets and pills contained higher concentrations of Scutellaria and Coptis compounds than the oral solutions, and the water decoction contained abundant glycosides and saponins. Moreover, the contents of flavanones and flavone O-glucuronides varied remarkably. This study provides a feasible solution for the comprehensive quality control of TCM patent drugs. PMID:27262372

  12. Use of ethyl lactate to extract bioactive compounds from Cytisus scoparius: Comparison of pressurized liquid extraction and medium scale ambient temperature systems.

    Science.gov (United States)

    Lores, Marta; Pájaro, Marta; Álvarez-Casas, Marta; Domínguez, Jorge; García-Jares, Carmen

    2015-08-01

    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

  13. Comparison of Major Bioactive Compounds of the Caterpillar Medicinal Mushroom, Cordyceps militaris (Ascomycetes), Fruiting Bodies Cultured on Wheat Substrate and Pupae.

    Science.gov (United States)

    Guo, Mingmin; Guo, Suping; Huaijun, Yang; Bu, Ning; Dong, Cai-Hong

    2016-01-01

    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. PMID:27481299

  14. Pilot-scale culture of Hypericum perforatum L. adventitious roots in airlift bioreactors for the production of bioactive compounds.

    Science.gov (United States)

    Cui, Xi-Hua; Murthy, Hosakatte Niranjana; Paek, Kee-Yoeup

    2014-09-01

    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. PMID:25096393

  15. Measurement of volatile organic compounds emitted in libraries and archives: an inferential indicator of paper decay?

    Directory of Open Access Journals (Sweden)

    Gibson Lorraine T

    2012-05-01

    Full Text Available Abstract Background A sampling campaign of indoor air was conducted to assess the typical concentration of indoor air pollutants in 8 National Libraries and Archives across the U.K. and Ireland. At each site, two locations were chosen that contained various objects in the collection (paper, parchment, microfilm, photographic material etc. and one location was chosen to act as a sampling reference location (placed in a corridor or entrance hallway. Results Of the locations surveyed, no measurable levels of sulfur dioxide were detected and low formaldehyde vapour (-3 was measured throughout. Acetic and formic acids were measured in all locations with, for the most part, higher acetic acid levels in areas with objects compared to reference locations. A large variety of volatile organic compounds (VOCs was measured in all locations, in variable concentrations, however furfural was the only VOC to be identified consistently at higher concentration in locations with paper-based collections, compared to those locations without objects. To cross-reference the sampling data with VOCs emitted directly from books, further studies were conducted to assess emissions from paper using solid phase microextraction (SPME fibres and a newly developed method of analysis; collection of VOCs onto a polydimethylsiloxane (PDMS elastomer strip. Conclusions In this study acetic acid and furfural levels were consistently higher in concentration when measured in locations which contained paper-based items. It is therefore suggested that both acetic acid and furfural (possibly also trimethylbenzenes, ethyltoluene, decane and camphor may be present in the indoor atmosphere as a result of cellulose degradation and together may act as an inferential non-invasive marker for the deterioration of paper. Direct VOC sampling was successfully achieved using SPME fibres and analytes found in the indoor air were also identified as emissive by-products from paper. Finally a new non

  16. Novel Anti-Campylobacter Compounds Identified Using High Throughput Screening of a Pre-selected Enriched Small Molecules Library

    Science.gov (United States)

    Kumar, Anand; Drozd, Mary; Pina-Mimbela, Ruby; Xu, Xiulan; Helmy, Yosra A.; Antwi, Janet; Fuchs, James R.; Nislow, Corey; Templeton, Jillian; Blackall, Patrick J.; Rajashekara, Gireesh

    2016-01-01

    Campylobacter is a leading cause of foodborne bacterial gastroenteritis worldwide and infections can be fatal. The emergence of antibiotic-resistant Campylobacter spp. necessitates the development of new antimicrobials. We identified novel anti-Campylobacter small molecule inhibitors using a high throughput growth inhibition assay. To expedite screening, we made use of a “bioactive” library of 4182 compounds that we have previously shown to be active against diverse microbes. Screening for growth inhibition of Campylobacter jejuni, identified 781 compounds that were either bactericidal or bacteriostatic at a concentration of 200 μM. Seventy nine of the bactericidal compounds were prioritized for secondary screening based on their physico-chemical properties. Based on the minimum inhibitory concentration against a diverse range of C. jejuni and a lack of effect on gut microbes, we selected 12 compounds. No resistance was observed to any of these 12 lead compounds when C. jejuni was cultured with lethal or sub-lethal concentrations suggesting that C. jejuni is less likely to develop resistance to these compounds. Top 12 compounds also possessed low cytotoxicity to human intestinal epithelial cells (Caco-2 cells) and no hemolytic activity against sheep red blood cells. Next, these 12 compounds were evaluated for ability to clear C. jejuni in vitro. A total of 10 compounds had an anti-C. jejuni effect in Caco-2 cells with some effective even at 25 μM concentrations. These novel 12 compounds belong to five established antimicrobial chemical classes; piperazines, aryl amines, piperidines, sulfonamide, and pyridazinone. Exploitation of analogs of these chemical classes may provide Campylobacter specific drugs that can be applied in both human and animal medicine. PMID:27092106

  17. Anti-nociceptive Activity of Ethnomedicinally Important Analgesic Plant Isodon rugosus Wall. ex Benth: Mechanistic Study and Identifications of Bioactive Compounds.

    Science.gov (United States)

    Zeb, Anwar; Ahmad, Sajjad; Ullah, Farhat; Ayaz, Muhammad; Sadiq, Abdul

    2016-01-01

    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

  18. Transformation of Rhodiola rosea with rol-genes from Agrobacterium rhizogenes to enhance the production of bioactive compounds and analyses of key genes in their pathways

    DEFF Research Database (Denmark)

    Stofberg, Jimmi; Antypa, Natalia-Meropi; Müller, Renate;

    Abstract Rhodiola rosea known as roseroot contains the secondary metabolites salidroside and rosavinoids. These composites are bioactive and plant products containing these compounds have been used for centuries to alleviate depression and stimulate the memory. Exploitation of the plant has led t...... auxins and cytokinins to stimulate further root growth and nodule formation for regeneration....

  19. Evaluation of antioxidant activities of bioactive compounds and various extracts obtained from saffron (Crocus sativus L.): a review

    OpenAIRE

    Rahaiee, Somayeh; Moini, Sohrab; Hashemi, Maryam; Shojaosadati, Seyed Abbas

    2014-01-01

    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 a...

  20. LAS ANTOCIANINAS COMO COLORANTES NATURALES Y COMPUESTOS BIOACTIVOS: REVISIÓN Anthocyanins As Natural Colorants And Bioactive Compounds: A Review

    Directory of Open Access Journals (Sweden)

    GLORIA ASTRID GARZÓN

    Full Text Available En la actualidad existe una demanda considerable de colorantes naturales alternativos a los colorantes sintéticos, como el rojo No. 40, debido a su toxicidad en alimentos, cosméticos y productos farmacéuticos. Las antocianinas son pigmentos vegetales con gran potencial para el reemplazo competitivo de colorantes sintéticos; por tanto es de gran importancia conocer los aspectos bioquímicos que enmarcan estos pigmentos. El objetivo de esta revisión es ofrecer un esquema actualizado sobre el potencial de las antocianinas como colorantes de origen natural, y de sus propiedades químicas y bioactivas. Las antocianinas son pigmentos responsables de la gama de colores que abarcan desde el rojo hasta el azul de muchas frutas, vegetales y cereales. El interés en estos pigmentos se ha intensificado gracias a sus posibles efectos terapéuticos y benéficos, dentro de los cuales se encuentran la reducción de la enfermedad coronaria, los efectos anticancerígenos, antitumorales, antiinflamatorios y antidiabéticos; además del mejoramiento de la agudeza visual y del comportamiento cognitivo. Las propiedades bioactivas de las antocianinas abren una nueva perspectiva para la obtención de productos coloreados con valor agregado para el consumo humano.At present there is a considerable demand for natural colorants to replace synthetic ones such red No. 40 due to their toxicity when added to food products, pharmaceuticals or cosmetics. Anthocyanins are vegetable pigments with high potential for replacement of synthetic dyes. Consequently, it is important to know the biochemical aspects that characterize these pigments. The objective of this review is to offer an updated overview of the potential of anthocyanins as natural colorants and their chemical and bioactive properties. Anthocyanins are pigments responsible for colors varying between red and purple in many fruits, vegetables and cereals. Interest in these pigments has intensified due not only to

  1. Comparison of the levels of bioactive benzoxazinoids in different wheat and rye fractions and the transformation of these compounds in homemade foods.

    Science.gov (United States)

    Tanwir, Fariha; Fredholm, Maria; Gregersen, Per L; Fomsgaard, Inge S

    2013-11-01

    Benzoxazinoids are important phytochemicals found in wheat and rye that are associated with plant resistance against pathogens, and recent studies have emphasized the potential health-promoting role of these compounds i.e. anti-cancer, anti-allergy and anti-inflammation. Accordingly, an understanding of their distribution in seeds and the effect of different processing techniques on their transformation will be helpful in identifying the mechanisms of their production and distribution and will support the on-going efforts to utilize these compounds in health-promoting food products. The analysis of seed fractions obtained from the milling of wheat and rye showed significantly higher concentrations of these bioactive compounds in the germ than in the other fractions, i.e. the bran and endosperm. Di-hexoses of 2,4-dihydroxy-1, 4-benzoxazin-3-one (DIBOA-glc-hexose) and 2-hydroxy-1, 4-benzoxazin-3-one (HBOA-glc-hexose) were the predominant compounds found in the different wheat and rye seed fractions followed by DIBOA-glc and DIBOA. The soaking and boiling of three rye-based breakfast cereals resulted in considerable changes in the benzoxazinoid contents. The soaking of pearled rye promoted the conversion of DIBOA-glc-hexose into DIBOA-glc. When these cereals were boiled, the increase in the DIBOA-glc content was much lower than that observed for soaking. For rye flakes, the pattern of these benzoxazinoids was different from that in pearled rye seeds. A considerable amount of the benzoxazinoids was also leached into the water during soaking or boiling. This study contributes to the understanding of the underlying processes involved in the biochemical changes of benzoxazinoids and will be the basis for future studies on other food-processing techniques. PMID:23768378

  2. Bioassay-Guided Isolation and HPLC Determination of Bioactive Compound That Relate to the Antiplatelet Activity (Adhesion, Secretion, and Aggregation from Solanum lycopersicum

    Directory of Open Access Journals (Sweden)

    Eduardo Fuentes

    2012-01-01

    Full Text Available 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.

  3. Antifungal activity of extracts from Atacama Desert fungi againstParacoccidioides brasiliensis and identification ofAspergillus felis as a promising source of natural bioactive compounds

    Directory of Open Access Journals (Sweden)

    Graziele Mendes

    2016-03-01

    Full Text Available 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.

  4. Antifungal activity of extracts from Atacama Desert fungi against Paracoccidioides brasiliensis and identification of Aspergillus felis as a promising source of natural bioactive compounds.

    Science.gov (United States)

    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

    2016-03-01

    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

  5. Preparative separation of bioactive compounds from essential oil of Flaveria bidentis (L.) Kuntze using steam distillation extraction and one step high-speed counter-current chromatography.

    Science.gov (United States)

    Wei, Yun; Du, Jilin; Lu, Yuanyuan

    2012-10-01

    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. PMID:22907873

  6. Ultrasound processing to enhance drying of cashew apple bagasse puree: Influence on antioxidant properties and in vitro bioaccessibility of bioactive compounds.

    Science.gov (United States)

    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

    2016-07-01

    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. PMID:26964946

  7. Characterization of Bioactive Compounds in Tunisian Bitter Orange (Citrus aurantium L. Peel and Juice and Determination of Their Antioxidant Activities

    Directory of Open Access Journals (Sweden)

    Iness Jabri karoui

    2013-01-01

    Full Text Available 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.

  8. Rescuing compound bioactivity in a secondary cell-based screening by using γ-cyclodextrin as a molecular carrier

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    Claveria-Gimeno R

    2015-03-01

    Full Text Available Rafael Claveria-Gimeno,1–3 Sonia Vega,3 Valeria Grazu,4 Jesús M de la Fuente,4–6 Angel Lanas,2,8–10 Adrian Velazquez-Campoy,2,3,7 Olga Abian1–3,8 1Instituto Aragonés de Ciencias de la Salud (IACS, Zaragoza, Spain; 2IIS Aragón, Zaragoza, Spain; 3Institute of Biocomputation and Physics of Complex Systems (BIFI, Joint Unit IQFR-CSIC-BIFI, Universidad de Zaragoza, Zaragoza, Spain; 4Instituto de Nanociencia de Aragon (INA, Universidad de Zaragoza, Zaragoza, Spain; 5Instituto de Ciencia de Materiales de Aragón (ICMA, CSIC-Universidad de Zaragoza, Zaragoza, Spain; 6Institute NanoBiomedicine and Engineering, Shanghai Jiao Tong University, Shanghai, People’s Republic of China; 7Fundacion ARAID, Government of Aragon, Spain; 8Centro de Investigación Biomédica en Red en el Área Temática de Enfermedades Hepáticas y Digestivas (CIBERehd, Barcelona, Spain; 9Servicio de Aparato Digestivo, Hospital Clínico Universitario Lozano Blesa, Zaragoza, Spain; 10Department of Medicine, University of Zaragoza, Zaragoza, Spain Abstract: In vitro primary screening for identifying bioactive compounds (inhibitors, activators or pharmacological chaperones against a protein target results in the discovery of lead compounds that must be tested in cell-based efficacy secondary screenings. Very often lead compounds do not succeed because of an apparent low potency in cell assays, despite an excellent performance in primary screening. Primary and secondary screenings differ significantly according to the conditions and challenges the compounds must overcome in order to interact with their intended target. Cellular internalization and intracellular metabolism are some of the difficulties the compounds must confront and different strategies can be envisaged for minimizing that problem. Using a novel screening procedure we have identified 15 compounds inhibiting the hepatitis C NS3 protease in an allosteric fashion. After characterizing biophysically the interaction

  9. Compostos bioativos em café integral e descafeinado e qualidade sensorial da bebida Bioactive compounds in whole and decaffeinated coffee and sensorial quality of the beverage

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    Sheila Andrade Abrahão

    2008-12-01

    Full Text Available O objetivo deste estudo foi determinar a qualidade sensorial de café (Coffea arabica descafeinado e integral, os níveis de compostos bioativos, antes e após a torração, e a estabilidade destes após a extração da bebida. A análise sensorial foi realizada por meio do método oficial brasileiro de classificação do café. As análises de cafeína, trigonelina e ácido clorogênico foram realizadas por cromatografia líquida de alta eficiência. O delineamento experimental foi o inteiramente ao acaso, em parcelas subdivididas com quatro tipos de café, cinco tempos de análise e três repetições. Na análise sensorial, foi observado que as características sensoriais, presentes na amostra integral, foram perdidas após o processo de descafeinação. Na variável concentração de trigonelina, não houve diferença significativa entre as amostras integrais e descafeinadas. As concentrações para as amostras de café descafeinado verde e integral torrado não foram alteradas após 4 horas de extração. Houve redução significativa na concentração do ácido clorogênico após a torração, após o processo de descafeinação, e com o decorrer do tempo de extração. Quanto à cafeína, não houve diferença significativa após a torração e nem com o passar do tempo após a extração. A descafeinação e a torração afetaram a qualidade sensorial do café e alteraram a concentração dos compostos bioativos.The aims of this study were to determine the sensorial quality of both decaffeinated and whole coffee (Coffea arabica, the levels of bioactive compounds, before and after toasting, and bioactive compound stability after beverage extraction. The sensorial analysis was accomplished according to the official Brazilian method for coffee classification. The analyses of caffeine, trigonelline and chlorogenic acid were performed by high performance liquid chromatography. The experimental design was completely randomized with split plot

  10. Optimization of the Extraction of Total Phenolic Compounds from Sunflower Meal and Evaluation of the Bioactivities of Chosen Extracts

    OpenAIRE

    M.M. Kamil; Mohamed, S.S.; Mohamed, S. H.; G.F. Mohamed; Taha, F. S.

    2011-01-01

    Sunflower seed defatted meal (SM) is an underutilized source of protein due to the presence of chlorogenic acid (CGA) which imparts a greenish color to sunflower meal protein products. The aim of the present study was to prepare a (CGA) extract from SM and evaluate its biological activity. The study included extraction of phenolic compounds from SM, using 80% methanol, 80% ethanol and 80% acetone. The methods of extraction used included conventional extraction (CE), microwave assisted extract...

  11. Bioactive compounds of red grapes from Dão region (Portugal): Evaluation of phenolic and organic profile

    OpenAIRE

    Luís Rodrigues Silva; Mafalda Queiroz

    2016-01-01

    Objective: To improve the knowledge on the metabolite profile of five red grapes from Dão region (Portugal), concerning to the phenolic characteristics (coloured and non-coloured phenolics) and organic acid composition. Methods: Five red grapes collected from Dão region were studied. The profiles of phenolic compounds and organic acids were estimated by high-performance liquid chromatography with diode-array detection and high-performance liquid chromatography with UV detector, respectivel...

  12. Three statistical experimental designs for enhancing yield of active compounds from herbal medicines and anti motion sickness bioactivity

    Directory of Open Access Journals (Sweden)

    Yan Chen

    2015-01-01

    Full Text Available Background: Since antiquity, Zingiber officinale (ginger, pogostemonis herba, and radix aucklandiae have been used as traditional Chinese medicines to remit gastrointestinal discomfort. Recent evidences also show the efficacy of the three herbal medicines against nausea and vomiting. Objective: To optimize the CO2 supercritical fluid extraction (SFE CO2 conditions for ginger and the ethanol reflux extraction conditions for radix aucklandiae, control the quality of pogostemonis herba essential oil, and evaluate anti motion sickness activity of the compound recipes composed of the three herbal medicine extracts. Materials and Methods: Two orthogonal array designs L9 (34 were employed to optimize the SFE CO2 conditions for enhancing yield of 6 gingerol from ginger and the ethanol reflux extraction conditions for enhancing yield of costunolide and dehydrocostus lactone from radix aucklandiae; a uniform design U5(53 was applied for evaluation of anti motion sickness activity of the compound recipes. Results: Extraction pressure (P < 0.01, extraction temperature and extraction time (P < 0.05 have significant effects on the yield of 6 gingerol from ginger by SFE CO2; ethanol concentration (P < 0.01 and times of repeating extraction (P < 0.05 have significant effects on the total yield of costunolide and dehydrocostus lactone from radix aucklandiae by ethanol reflux extraction; the anti motion sickness effects of the optimized compound recipe composed of the three herbal medicine extracts were markedly better than those of dimenhydrinate. Conclusion: The compound recipe composed of ginger, pogostemonis herba, and radix aucklandiae could be developed as a promising anti motion sickness medicine.

  13. Simultaneous determination of 11 bioactive compounds in Jaeumganghwa-tang by high performance liquid chromatography-diode array detection

    OpenAIRE

    Bo-Ra Yun; Jin Bae Weon; Jiwoo Lee; Min Rye Eom; Choong Je Ma

    2014-01-01

    Background: Jaeumganghwa-tang (JEGH) is a traditional Korean herbal medicine for the treatment of chronic bronchitis, nephritis and diabetes mellitus. Objective: A high performance liquid chromatography-diode array detector (HPLC-DAD) method was developed for simultaneous determination of 11 major compounds such as 5- hydroxymethylfurfural, mangiferin, paeoniflorin, nodakenin, naringin, hesperidin, decursinol, berberine, glycyrrhizin, atractylenolide III and decursin, in JEGH. Materials and M...

  14. Isolation of bioactive compound from marine seaweeds against fish pathogenic bacteria Vibrio alginolyticus (VA09) and characterisation by FTIR

    Institute of Scientific and Technical Information of China (English)

    Rajasekar Thirunavukkarasu; Priyadharshini Pandiyan; Deivasigamani Balaraman; Kumaran Subaramaniyan; George Edward Gnana Jothi; Sakthivel Manikkam; Balamurugan Sadaiyappan

    2013-01-01

    Objective: Fresh marine seaweeds Gracilaria edulis, Gracillaria verrcosa, Acanthospora spicifera,Ulva facita, Ulva lacta (U. lacta), Kappaphycus spicifera, Sargassum ilicifolium, Sargassum wightii (S. wightii), Padina tetramatica and Padina gymonospora were collected from Mandapam (Rameshwaram, Tamil Nadu) of South East coast of India and were screened for antibacterial activity.Methods:All the collected seaweeds were extracted by using five different solvent (methanol, isopropanol, acetone, chloroform, diethyl ether) to study their extracts against fish pathogenic bacteria V. alginolyticus (VA09) purchased from MTCC. And minimum inhibition carried out by using Resazurin micro-titre assay. Crude extract of S. wightii analysied by FTIR.Results:The methanolic extract of S. wightii produced a maximum zone of inhibition (1.95±0.11) cm, isopropanol extract maximum inhibition was produced by S. wightii (1.93±0.78) cm, Acetone extract of Gracilaria verrcosa showed maximum zone of inhibition (1.36±0.05) cm, chloroform extract of S. wightii produced a maximum zone (1.56±0.25) cm and diethyl ether extract of S.wightii produced maximum zone of inhibition(1.86±0.11) cm. Based on the antibacterial activity S. wightii, U. lacta and Padina tetramatica showed best antibacterial activity against Vibrio harveyi. In this three seaweeds were taken for MIC study. The S. wightii methanolic extract, U. lacta diethyl ether extract and Padina tetramatica methanolic extract showed a higher MIC values, and despectively were 25 mg/mL, 50 mg/mL and 50 mg/mL. FTIR result showed that mostly phenolic compounds were present in the S. wightii.Conclusions:Based on the FTIR result S. wightii have high amount of phenolic compound. Phenolic compound have the good antimicrobial activity. The results clearly show that seaweedS. wightii is an interesting source for biologically active compounds that may be applied for prophylaxis and therapy of bacterial fish diseases and it should be used for

  15. COMPARISON OF SIMCA PATTERN RECOGNITION & LIBRARY SEARCH IDENTIFICATION OF HAZARDOUS COMPOUNDS FROM MASS SPECTRA

    Science.gov (United States)

    SIMCA pattern recognition methods have been applied to mass spectral data from a target list of hazardous chemicals. cheme has been proposed for classification and identification of five classes of compounds including aromatics, chlorocarbons, bromocarbons, hydrocarbons, and poly...

  16. COMPARISON OF SIMCA PATTERN RECOGNITION AND LIBRARY SEARCH IDENTIFICATION OF HAZARDOUS COMPOUNDS FROM MASS SPECTRA

    Science.gov (United States)

    SIMCA pattern recognition methods have been applied to mass spectral data from a target list of hazardous chemicals. cheme has been proposed for classification and identification of five classes of compounds including aromatics, chlorocarbons, bromocarbons, hydrocarbons, and poly...

  17. Probing the bioactivity-relevant chemical space of robust reactions and common molecular building blocks.

    Science.gov (United States)

    Hartenfeller, Markus; Eberle, Martin; Meier, Peter; Nieto-Oberhuber, Cristina; Altmann, Karl-Heinz; Schneider, Gisbert; Jacoby, Edgar; Renner, Steffen

    2012-05-25

    In the search for new bioactive compounds, there is a trend toward increasingly complex compound libraries aiming to target the demanding targets of the future. In contrast, medicinal chemistry and traditional library design rely mainly on a small set of highly established and robust reactions. Here, we probe a set of 58 such reactions for their ability to sample the chemical space of known bioactive molecules, and the potential to create new scaffolds. Combined with ~26,000 common available building blocks, the reactions retrieve around 9% of a scaffold-diverse set of compounds active on human target proteins covering all major pharmaceutical target classes. Almost 80% of generated scaffolds from virtual one-step synthesis products are not present in a large set of known bioactive molecules for human targets, indicating potential for new discoveries. The results suggest that established synthesis resources are well suited to cover the known bioactivity-relevant chemical space and that there are plenty of unexplored regions accessible by these reactions, possibly providing valuable "low-hanging fruit" for hit discovery. PMID:22512717

  18. Elicitation, an Effective Strategy for the Biotechnological Production of Bioactive High-Added Value Compounds in Plant Cell Factories

    Directory of Open Access Journals (Sweden)

    Karla Ramirez-Estrada

    2016-02-01

    Full Text Available Plant in vitro cultures represent an attractive and cost-effective alternative to classical approaches to plant secondary metabolite (PSM production (the “Plant Cell Factory” concept. Among other advantages, they constitute the only sustainable and eco-friendly system to obtain complex chemical structures biosynthesized by rare or endangered plant species that resist domestication. For successful results, the biotechnological production of PSM requires an optimized system, for which elicitation has proved one of the most effective strategies. In plant cell cultures, an elicitor can be defined as a compound introduced in small concentrations to a living system to promote the biosynthesis of the target metabolite. Traditionally, elicitors have been classified in two types, abiotic or biotic, according to their chemical nature and exogenous or endogenous origin, and notably include yeast extract, methyl jasmonate, salicylic acid, vanadyl sulphate and chitosan. In this review, we summarize the enhancing effects of elicitors on the production of high-added value plant compounds such as taxanes, ginsenosides, aryltetralin lignans and other types of polyphenols, focusing particularly on the use of a new generation of elicitors such as coronatine and cyclodextrins.

  19. The Herbal Drug Melampyrum pratense L. (Koch: Isolation and Identification of Its Bioactive Compounds Targeting Mediators of Inflammation

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    S. Vogl

    2013-01-01

    Full Text Available Melampyrum pratense L. (Koch is used in traditional Austrian medicine for the treatment of different inflammation-related conditions. In this work, we show that the extracts of M. pratense stimulated peroxisome proliferator-activated receptors- (PPARs-α and -γ that are well recognized for their anti-inflammatory activities. Furthermore, the extract inhibited the activation of the proinflammatory transcription factor NF-κB and induction of its target genes interleukin-8 (IL-8 and E-selectin in vitro. Bioassay-guided fractionation identified several active flavonoids and iridoids including melampyroside and mussaenoside and the phenolic compound lunularin that were identified in this species for the first time. The flavonoids apigenin and luteolin were distinguished as the main components accountable for the anti-inflammatory properties. Apigenin and luteolin effectively inhibited tumor necrosis factor α (TNF-α-induced NF-κB-mediated transactivation of a luciferase reporter gene. Furthermore, the two compounds dose-dependently reduced IL-8 and E-selectin protein expression after stimulation with lipopolysaccharide (LPS or TNF-α in endothelial cells (ECs. The iridoids melampyroside and mussaenoside prevented the elevation of E-selectin in LPS-stimulated ECs. Lunularin was found to reduce the protein levels of the proinflammatory mediators E-selectin and IL-8 in ECs in response to LPS. These data validate the ethnomedical use of M. pratense for the treatment of inflammatory conditions and point to the constituents accountable for its anti-inflammatory activity.

  20. HPLC-DAD-ESI/MS(n) analysis of phenolic compounds for quality control of Grindelia robusta Nutt. and bioactivities.

    Science.gov (United States)

    Ferreres, Federico; Grosso, Clara; Gil-Izquierdo, Angel; Valentão, Patrícia; Azevedo, Carolina; Andrade, Paula B

    2014-06-01

    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. PMID:24603350

  1. Simultaneous determination of 11 bioactive compounds in Jaeumganghwa-tang by high performance liquid chromatography-diode array detection

    Directory of Open Access Journals (Sweden)

    Bo-Ra Yun

    2014-01-01

    Full Text Available Background: Jaeumganghwa-tang (JEGH is a traditional Korean herbal medicine for the treatment of chronic bronchitis, nephritis and diabetes mellitus. Objective: A high performance liquid chromatography-diode array detector (HPLC-DAD method was developed for simultaneous determination of 11 major compounds such as 5- hydroxymethylfurfural, mangiferin, paeoniflorin, nodakenin, naringin, hesperidin, decursinol, berberine, glycyrrhizin, atractylenolide III and decursin, in JEGH. Materials and Methods: The separation was conducted on Shishedo C 18 column with gradient elution of 0.1% trifluoroacetic acid-acetonitrile. Detection of wavelength was set at 205, 250, 280 and 330 nm. Results: The developed analysis showed a good linearity (R2 >0.9997. The range of limit of detection and limit of quantification were observed from 0.04 to 0.43 and from 0.11 to 1.30, respectively. The intra- and inter-day test relative standard deviations (RSD were less than 3% and the accuracy was 95.98-108.44%. The recoveries were between 92.75% and 109.19% and RSD range of recoveries was measured from 0.52% to 2.78%. Conclusion: This HPLC-DAD method can be successfully applied for simultaneous determination of 11 major compounds in JEGH samples.

  2. Effect of ultrasound on the supercritical CO2 extraction of bioactive compounds from dedo de moça pepper (Capsicum baccatum L. var. pendulum).

    Science.gov (United States)

    Dias, Arthur Luiz Baião; Arroio Sergio, Camilla Scarelli; Santos, Philipe; Barbero, Gerardo Fernandéz; Rezende, Camila Alves; Martínez, Julian

    2016-07-01

    Extracts with bioactive compounds were obtained from the red pepper variety "dedo de moça" (Capsicum baccatum L. var. pendulum) through supercritical fluid extraction with carbon dioxide assisted by ultrasound (SFE-US). The process was tested at pressures of 15, 20 and 25 MPa; temperatures of 40, 50 and 60 °C, and ultrasonic powers of 200, 400 and 600 W applied during 40, 60 and 80 min of extraction. The CO2 mass flow rate was fixed at 1.7569 × 10(-4) kg/s. Global yield, phenolic content, antioxidant capacity and capsaicinoid concentration were evaluated in the extracts. The application of ultrasound raised the global extraction yield of SFE up to 45%. The phenolic content of the extract increased with the application of higher ultrasound power and radiation time. The capsaicinoid yield was also enhanced with ultrasound up to 12%. However, the antioxidant capacity did not increase with the ultrasound application. The BET-based model and the broken and intact cell model fitted well to the kinetic SFE curves. The BET-based model with three adjustable parameters resulted in the best fits to the experimental data. Field emission scanning electron microscopy (FESEM) images showed that SFE disturbed the vegetable matrix, releasing particles from the inner region of the plant cells to their surface. When the ultrasound was applied this effect was more pronounced. On the other hand, cracks, fissures or any sign of rupture were not identified on the sample surface. PMID:26964951

  3. Colour Evaluation, Bioactive Compound Content, Phenolic Acid Profiles and in Vitro Biological Activity of Passerina del Frusinate White Wines: Influence of Pre-Fermentative Skin Contact Times.

    Science.gov (United States)

    Carbone, Katya; Fiordiponti, Luciano

    2016-01-01

    Passerina del Frusinate is an autochthonous wine grape variety, which grows in the Lazio region that is currently being evaluated by local wine producers. In this study, colour properties (CIELab coordinates), bioactive compounds (total polyphenols and flavan-3-ols), HPLC-DAD phenolic acid profiles and in vitro biological activity of monovarietal Passerina del Frusinate white wines and the effect of different maceration times (0, 18 and 24 h) were evaluated based on these parameters. Results highlighted statistically significant differences for almost all analysed parameters due to a strong influence of the pre-fermentative skin contact time. The flavan content of macerated wines was six times higher than that of the control, while total polyphenols were 1.5 times higher. According to their phytochemical content, macerated wines showed the highest antiradical capacity tested by means of DPPH(•) and ABTS(+•) assays. Besides, prolonged maceration resulted in a reduction of CIELab coordinates as well as of the content of phenolic substances and antiradical capacity. Among the phenolic acids analysed, the most abundant were vanillic acid and caffeic acid; the latter proved to be the most susceptible to degradation as a result of prolonged maceration. Passerina del Frusinate appears as a phenol-rich white wine with a strong antioxidant potential similar to that of red wines. PMID:27455227

  4. Antiprotozoal Activity against Entamoeba histolytica of Plants Used in Northeast Mexican Traditional Medicine. Bioactive Compounds from Lippia graveolens and Ruta chalepensis

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    Ramiro Quintanilla-Licea

    2014-12-01

    Full Text Available Amoebiasis caused by Entamoeba histolytica is associated with high morbidity and mortality is becoming a major public health problem worldwide, especially in developing countries. Because of the side-effects and the resistance that pathogenic protozoa build against the standard antiparasitic drugs, e.g., metronidazole, much recent attention has been paid to plants used in traditional medicine around the world in order to find new antiprotozoal agents. We collected 32 plants used in Northeast Mexican traditional medicine and the methanolic extracts of these species were screened for antiprotozoal activity against E. histolytica trophozoites using in vitro tests. Only 18 extracts showed a significant inhibiting activity and among them six plant extracts showed more than 80% growth inhibition against E. histolytica at a concentration of 150 µg/mL and the IC50 values of these extracts were determined. Lippia graveolens Kunth and Ruta chalepensis Pers. showed the more significant antiprotozoal activity (91.54% and 90.50% growth inhibition at a concentration of 150 µg/mL with IC50 values of 59.14 and 60.07 µg/mL, respectively. Bioassay-guided fractionation of the methanolic extracts from these two plants afforded carvacrol (1 and chalepensin (2, respectively, as bioactive compounds with antiprotozoal activity.

  5. Colour Evaluation, Bioactive Compound Content, Phenolic Acid Profiles and in Vitro Biological Activity of Passerina del Frusinate White Wines: Influence of Pre-Fermentative Skin Contact Times

    Directory of Open Access Journals (Sweden)

    Katya Carbone

    2016-07-01

    Full Text Available Passerina del Frusinate is an autochthonous wine grape variety, which grows in the Lazio region that is currently being evaluated by local wine producers. In this study, colour properties (CIELab coordinates, bioactive compounds (total polyphenols and flavan-3-ols, HPLC-DAD phenolic acid profiles and in vitro biological activity of monovarietal Passerina del Frusinate white wines and the effect of different maceration times (0, 18 and 24 h were evaluated based on these parameters. Results highlighted statistically significant differences for almost all analysed parameters due to a strong influence of the pre-fermentative skin contact time. The flavan content of macerated wines was six times higher than that of the control, while total polyphenols were 1.5 times higher. According to their phytochemical content, macerated wines showed the highest antiradical capacity tested by means of DPPH• and ABTS+• assays. Besides, prolonged maceration resulted in a reduction of CIELab coordinates as well as of the content of phenolic substances and antiradical capacity. Among the phenolic acids analysed, the most abundant were vanillic acid and caffeic acid; the latter proved to be the most susceptible to degradation as a result of prolonged maceration. Passerina del Frusinate appears as a phenol-rich white wine with a strong antioxidant potential similar to that of red wines.

  6. Dehydrated olive-waste cake as a source of high value-added bioproduct: Drying kinetics, physicochemical properties, and bioactive compounds

    Directory of Open Access Journals (Sweden)

    Elsa Uribe

    2014-09-01

    Full Text Available Olive (Olea europaea L. oil processing produces significant amount of waste that can be utilized for the production of high value-added ingredients for various industrial applications. In this work, the effects of temperature on drying kinetics and quality indexes of the olive-waste cake during convective dehydration (40-90 °C were investigated. Results on effective moisture diffusivity, physicochemical parameters, fatty acid profile, total phenolic, flavonoid, and flavanol contents as well as antioxidant capacity are also reported. Most of the fatty acids increased their content with respect to control sample with a temperature increase, i.e. oleic and linoleic acids increased 48% and 43% at 70 and 40 °C, respectively. Total flavanol content increased with temperature (48-62 mg catechin equivalents [CTE] 100 g-1 DM except for 80 °C. Total phenolic and total flavonoid contents were highly correlated to antioxidant capacity (0.923 < r < 0.992, except for 70 and 80 °C, the rest of the samples maintained their initial antioxidant capacity by ORAC analysis. Thus, these parameters show that dried olive-waste cake has a high bioactive compounds with potential use as additives for the food or other industries.

  7. Nopal cactus (Opuntia ficus-indica) as a source of bioactive compounds for nutrition, health and disease.

    Science.gov (United States)

    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

    2014-01-01

    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. PMID:25232708

  8. Nopal Cactus (Opuntia ficus-indica as a Source of Bioactive Compounds for Nutrition, Health and Disease

    Directory of Open Access Journals (Sweden)

    Karym El-Mostafa

    2014-09-01

    Full Text Available 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.

  9. Characterization and stability studies of bioactive compounds and food matrices as evidence in support of health claims.

    Science.gov (United States)

    González-Ferrero, Carolina; Sáiz-Abajo, María-José

    2015-07-01

    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. PMID:26241010

  10. Activity Profile of an FDA-Approved Compound Library against Schistosoma mansoni.

    Directory of Open Access Journals (Sweden)

    Gordana Panic

    Full Text Available As plans to expand mass drug treatment campaigns to fight schistosomiasis form, worries about reliance on praziquantel as the sole available treatment motivate the investigation for novel antischistosomal compounds. Drug repurposing might be an inexpensive and effective source of novel antischistosomal leads.1600 FDA approved compounds were first assayed against Schistosoma mansoni schistosomula at a concentration of 10 µM. Active compounds identified from this screen were advanced to the adult worm screen at 33.33 µM, followed by hit characterization. Leads with complementary pharmacokinetic and toxicity profiles were then selected for in vivo studies.The in vitro screen identified 121 and 36 compounds active against the schistosomula and adult stage, respectively. Further, in vitro characterization and comparison with already available pharmacokinetic and toxicity data identified 11 in vivo candidates. Doramectin (10 mg/kg and clofazimine (400 mg/kg were found to be active in vivo with worm burden reductions of 60.1% and 82.7%, respectively.The work presented here expands the knowledge of antischistosomal properties of already approved compounds and underscores variations observed between target-based and phenotypic approaches and among laboratories. The two in vivo-active drugs identified in this study, doramectin and clofazimine are widely available and present as novel drug classes as starting points for further investigation.

  11. Beneficial effect of a sturgeon-based bioactive compound on gene expression of tumor necrosis factor-alpha, matrix metalloproteinases and type-10 collagen in human chondrocytes.

    Science.gov (United States)

    Catanzaro, R; Marotta, F; Jain, S; Rastmanesh, R; Allegri, F; Celep, G; Lorenzetti, A; Polimeni, A; Yadav, H

    2012-01-01

    In the present study, we examined the effect of a marine bioactive compound containing high-purity caviar-derived DNA, collagen elastin and protein extracts from sturgeon (LD-1227, Caviarlieri, Laboratoires Dom, Switzerland) on IL-1beta-induced activation and production of TNFalpha and MMP-13 in human osteo-arthritis (OA) chondrocytes and intracellular signaling factors. Human chondrocytes were derived from OA cartilage and stimulated with IL-1beta. Gene expression of TNFalpha, MMP-13, MMP-1 and Col10A1 was measured by quantitative RT-PCR. TNFalpha protein in culture medium was determined using cytokine-specific ELISA. Western immunoblotting was used to analyze the MMP-13 production in the culture medium and the activation of NF-kB. DNA binding activity of NF-kB p65 was determined using a highly sensitive and specific ELISA. MMP-13 activity in the culture medium was assayed by gelatine zymography. LD-1227 significantly decreased IL-1beta-stimulated gene expression and production of TNFalpha, MMP-1, MMP-13 and Col10A1 in human chondrocytes. The inhibitory effect of LD-1227 on the IL-1beta-induced expression of these genes was mediated at least in part via suppression of NF-kB p65. These data show that LD-1227 can inhibit IL-1beta-induced proliferation and inflammatory reactions via inhibited activation of the transcription factor NF-kB pathway in human chondrocytes derived from OA patients. These novel pharmacological actions of LD-1227 on IL-1beta-stimulated human OA chondrocytes provide suggestions that this marine biology compound may inhibit cartilage degradation by suppressing IL-1beta-mediated activation and the catabolic response in human chondrocytes. PMID:23034253

  12. Gene-Set Local Hierarchical Clustering (GSLHC--A Gene Set-Based Approach for Characterizing Bioactive Compounds in Terms of Biological Functional Groups.

    Directory of Open Access Journals (Sweden)

    Feng-Hsiang Chung

    Full Text Available Gene-set-based analysis (GSA, which uses the relative importance of functional gene-sets, or molecular signatures, as units for analysis of genome-wide gene expression data, has exhibited major advantages with respect to greater accuracy, robustness, and biological relevance, over individual gene analysis (IGA, which uses log-ratios of individual genes for analysis. Yet IGA remains the dominant mode of analysis of gene expression data. The Connectivity Map (CMap, an extensive database on genomic profiles of effects of drugs and small molecules and widely used for studies related to repurposed drug discovery, has been mostly employed in IGA mode. Here, we constructed a GSA-based version of CMap, Gene-Set Connectivity Map (GSCMap, in which all the genomic profiles in CMap are converted, using gene-sets from the Molecular Signatures Database, to functional profiles. We showed that GSCMap essentially eliminated cell-type dependence, a weakness of CMap in IGA mode, and yielded significantly better performance on sample clustering and drug-target association. As a first application of GSCMap we constructed the platform Gene-Set Local Hierarchical Clustering (GSLHC for discovering insights on coordinated actions of biological functions and facilitating classification of heterogeneous subtypes on drug-driven responses. GSLHC was shown to tightly clustered drugs of known similar properties. We used GSLHC to identify the therapeutic properties and putative targets of 18 compounds of previously unknown characteristics listed in CMap, eight of which suggest anti-cancer activities. The GSLHC website http://cloudr.ncu.edu.tw/gslhc/ contains 1,857 local hierarchical clusters accessible by querying 555 of the 1,309 drugs and small molecules listed in CMap. We expect GSCMap and GSLHC to be widely useful in providing new insights in the biological effect of bioactive compounds, in drug repurposing, and in function-based classification of complex diseases.

  13. Bioactive compounds of Eriocaulon sieboldianum blocking proliferation and inducing apoptosis of HepG2 cells might be involved in Aurora kinase inhibition.

    Science.gov (United States)

    Fan, Yanhua; Lu, Hongyuan; Ma, Hongda; Feng, Fan; Hu, Xiaolong; Zhang, Qiao; Wang, Jian; Xu, Yongnan; Zhao, Qingchun

    2015-12-01

    Eriocaulon sieboldianum (Sieb. & Zucc. ex Steud.) is an edible and medicinal plant used in traditional Chinese medicine. Often in combination with other herbs, it is processed into healthcare beverages for expelling wind-heat, protecting eyes, and reducing blood lipids. Besides, its water decoction together with other herbs has been utilized to treat cancer in China. However, the active ingredients and the precise cellular mechanisms of E. sieboldianum remain to be elucidated. The Aurora kinase family plays critical roles in the regulation of cell division and has attracted great attention to the identification of small-molecule Aurora kinase inhibitors for potential treatment of cancer. A molecular docking study was employed for docking of the most bioactive compounds. Hispidulin (HPDL) and quercetin-3-O-(6''-O-galloyl)-β-D-galactopyranoside (QGGP) were singled out as potent inhibitors of Aurora kinase. Their inhibitory activity towards Aurora kinase was further confirmed by the obvious decrease in autophosphorylation of Aurora-A (Thr288) and Aurora-B (Thr232). Moreover, the induction of cell cycle arrest in HepG2 cells and the suppressed phosphorylation of histone H3 were also consistent with the inhibition of Aurora kinase. The data indicate that the E. sieboldianum extract and its two active compounds, HPDL and QGGP, could effectively induce apoptosis via p53, MAPKs and the mitochondrial apoptotic pathways. These findings could improve the understanding and enhance the development of drugs based on E. sieboldianum and raise its application value in anticancer therapy or prevention. In addition, our results indicated that Aurora kinase might be a novel target of HPDL and QGGP. PMID:26369427

  14. Gene-Set Local Hierarchical Clustering (GSLHC)--A Gene Set-Based Approach for Characterizing Bioactive Compounds in Terms of Biological Functional Groups.

    Science.gov (United States)

    Chung, Feng-Hsiang; Jin, Zhen-Hua; Hsu, Tzu-Ting; Hsu, Chueh-Lin; Liu, Hsueh-Chuan; Lee, Hoong-Chien

    2015-01-01

    Gene-set-based analysis (GSA), which uses the relative importance of functional gene-sets, or molecular signatures, as units for analysis of genome-wide gene expression data, has exhibited major advantages with respect to greater accuracy, robustness, and biological relevance, over individual gene analysis (IGA), which uses log-ratios of individual genes for analysis. Yet IGA remains the dominant mode of analysis of gene expression data. The Connectivity Map (CMap), an extensive database on genomic profiles of effects of drugs and small molecules and widely used for studies related to repurposed drug discovery, has been mostly employed in IGA mode. Here, we constructed a GSA-based version of CMap, Gene-Set Connectivity Map (GSCMap), in which all the genomic profiles in CMap are converted, using gene-sets from the Molecular Signatures Database, to functional profiles. We showed that GSCMap essentially eliminated cell-type dependence, a weakness of CMap in IGA mode, and yielded significantly better performance on sample clustering and drug-target association. As a first application of GSCMap we constructed the platform Gene-Set Local Hierarchical Clustering (GSLHC) for discovering insights on coordinated actions of biological functions and facilitating classification of heterogeneous subtypes on drug-driven responses. GSLHC was shown to tightly clustered drugs of known similar properties. We used GSLHC to identify the therapeutic properties and putative targets of 18 compounds of previously unknown characteristics listed in CMap, eight of which suggest anti-cancer activities. The GSLHC website http://cloudr.ncu.edu.tw/gslhc/ contains 1,857 local hierarchical clusters accessible by querying 555 of the 1,309 drugs and small molecules listed in CMap. We expect GSCMap and GSLHC to be widely useful in providing new insights in the biological effect of bioactive compounds, in drug repurposing, and in function-based classification of complex diseases. PMID:26473729

  15. Direct Phenotypic Screening in Mice: Identification of Individual, Novel Antinociceptive Compounds from a Library of 734,821 Pyrrolidine Bis-piperazines.

    Science.gov (United States)

    Houghten, Richard A; Ganno, Michelle L; McLaughlin, Jay P; Dooley, Colette T; Eans, Shainnel O; Santos, Radleigh G; LaVoi, Travis; Nefzi, Adel; Welmaker, Greg; Giulianotti, Marc A; Toll, Lawrence

    2016-01-11

    The hypothesis in the current study is that the simultaneous direct in vivo testing of thousands to millions of systematically arranged mixture-based libraries will facilitate the identification of enhanced individual compounds. Individual compounds identified from such libraries may have increased specificity and decreased side effects early in the discovery phase. Testing began by screening ten diverse scaffolds as single mixtures (ranging from 17,340 to 4,879,681 compounds) for analgesia directly in the mouse tail withdrawal model. The "all X" mixture representing the library TPI-1954 was found to produce significant antinociception and lacked respiratory depression and hyperlocomotor effects using the Comprehensive Laboratory Animal Monitoring System (CLAMS). The TPI-1954 library is a pyrrolidine bis-piperazine and totals 738,192 compounds. This library has 26 functionalities at the first three positions of diversity made up of 28,392 compounds each (26 × 26 × 42) and 42 functionalities at the fourth made up of 19,915 compounds each (26 × 26 × 26). The 120 resulting mixtures representing each of the variable four positions were screened directly in vivo in the mouse 55 °C warm-water tail-withdrawal assay (ip administration). The 120 samples were then ranked in terms of their antinociceptive activity. The synthesis of 54 individual compounds was then carried out. Nine of the individual compounds produced dose-dependent antinociception equivalent to morphine. In practical terms what this means is that one would not expect multiexponential increases in activity as we move from the all-X mixture, to the positional scanning libraries, to the individual compounds. Actually because of the systematic formatting one would typically anticipate steady increases in activity as the complexity of the mixtures is reduced. This is in fact what we see in the current study. One of the final individual compounds identified, TPI 2213-17, lacked significant respiratory

  16. Ozone-induced changes in the content of bioactive compounds and enzyme activity during storage of pepper fruits.

    Science.gov (United States)

    Sachadyn-Król, Monika; Materska, Małgorzata; Chilczuk, Barbara; Karaś, Monika; Jakubczyk, Anna; Perucka, Irena; Jackowska, Izabella

    2016-11-15

    This paper presents for the first time the results of investigations concerning the effect of treatment of whole pepper fruits with gaseous ozone and the refrigeration storage period conditions on pepper quality. The effects are reflected in changes in the flavonoid contents, the antioxidant activity of the phenolic compound fraction and the enzymes involved in phenylpropanoid metabolism. The investigations were carried out on a hot pepper fruit cultivar, Cyklon. It was found that the levels of a majority of flavonoids, in particular those of quercetin 3-O-rhamnoside and quercetin 3-O-rhamnoside-7-O-glucoside increased in the pericarp of fruits treated with ozone for 3h and stored for 20days (by 25% relative to the control). Simultaneously, reduced phenylalanine ammonia-lyase and tyrosine ammonia-lyase activity were noted, which implies slight degradation of enzymes caused by the ozone treatment and enhancement of the polyphenol oxidase and guaiacol oxidase activity involved in response to increased oxidative stress. PMID:27283607

  17. Fungi associated with rocks of the Atacama Desert: taxonomy, distribution, diversity, ecology and bioprospection for bioactive compounds.

    Science.gov (United States)

    Gonçalves, Vívian N; Cantrell, Charles L; Wedge, David E; Ferreira, Mariana C; Soares, Marco Aurélio; Jacob, Melissa R; Oliveira, Fabio S; Galante, Douglas; Rodrigues, Fabio; Alves, Tânia M A; Zani, Carlos L; Junior, Policarpo A S; Murta, Silvane; Romanha, Alvaro J; Barbosa, Emerson C; Kroon, Erna G; Oliveira, Jaquelline G; Gomez-Silva, Benito; Galetovic, Alexandra; Rosa, Carlos A; Rosa, Luiz H

    2016-01-01

    This study assessed the diversity of cultivable rock-associated fungi from Atacama Desert. A total of 81 fungal isolates obtained were identified as 29 Ascomycota taxa by sequencing different regions of DNA. Cladosporium halotolerans, Penicillium chrysogenum and Penicillium cf. citrinum were the most frequent species, which occur at least in four different altitudes. The diversity and similarity indices ranged in the fungal communities across the latitudinal gradient. The Fisher-α index displayed the higher values for the fungal communities obtained from the siltstone and fine matrix of pyroclastic rocks with finer grain size, which are more degraded. A total of 23 fungal extracts displayed activity against the different targets screened. The extract of P. chrysogenum afforded the compounds α-linolenic acid and ergosterol endoperoxide, which were active against Cryptococcus neoformans and methicillin-resistance Staphylococcus aureus respectively. Our study represents the first report of a new habitat of fungi associated with rocks of the Atacama Desert and indicated the presence of interesting fungal community, including species related with saprobes, parasite/pathogen and mycotoxigenic taxa. The geological characteristics of the rocks, associated with the presence of rich resident/resilient fungal communities suggests that the rocks may provide a favourable microenvironment fungal colonization, survival and dispersal in extreme conditions. PMID:26235221

  18. Enhanced Production of Bioactive Isoprenoid Compounds from Cell Suspension Cultures of Artemisia annua L. Using β-Cyclodextrins

    Directory of Open Access Journals (Sweden)

    Francesca Rizzello

    2014-10-01

    Full Text Available Plant cell cultures as valuable tools for the production of specific metabolites can be greatly improved by the application of elicitors including cyclodextrins (CDs for enhancing the yields of the desired plant compounds. Here the effects of 2,6-dimethyl-β-cyclodextrins (DIMEB on the production of carotenoids and quinones from Artemisia annua L. cell suspension cultures were investigated. The addition of 50 mM DIMEB induced an early increase of intracellular carotenoid and quinone contents, which could be observed to a higher extent for lutein (10-fold, Q9 (3-fold and Q10 (2.5-fold. Real Time PCR analysis revealed that the expression of 1-deoxy-d-xylulose-5-phosphate reductoisomerase (DXR gene in DIMEB treated cell cultures after three days was 2.5-fold higher than in untreated samples, thus suggesting that the DIMEB induced increase of carotenoids and quinones could be due to the induction of the plastidial isoprenoid biosynthetic route. In addition, the DIMEB treatment induced an enhanced release of carotenoids and quinones into the culture medium of A. annua cell suspension cultures possibly due to the ability of CDs to form inclusion complexes with hydrophobic molecules.

  19. Enhanced production of bioactive isoprenoid compounds from cell suspension cultures of Artemisia annua L. using β-cyclodextrins.

    Science.gov (United States)

    Rizzello, Francesca; De Paolis, Angelo; Durante, Miriana; Blando, Federica; Mita, Giovanni; Caretto, Sofia

    2014-01-01

    Plant cell cultures as valuable tools for the production of specific metabolites can be greatly improved by the application of elicitors including cyclodextrins (CDs) for enhancing the yields of the desired plant compounds. Here the effects of 2,6-dimethyl-β-cyclodextrins (DIMEB) on the production of carotenoids and quinones from Artemisia annua L. cell suspension cultures were investigated. The addition of 50 mM DIMEB induced an early increase of intracellular carotenoid and quinone contents, which could be observed to a higher extent for lutein (10-fold), Q9 (3-fold) and Q10 (2.5-fold). Real Time PCR analysis revealed that the expression of 1-deoxy-d-xylulose-5-phosphate reductoisomerase (DXR) gene in DIMEB treated cell cultures after three days was 2.5-fold higher than in untreated samples, thus suggesting that the DIMEB induced increase of carotenoids and quinones could be due to the induction of the plastidial isoprenoid biosynthetic route. In addition, the DIMEB treatment induced an enhanced release of carotenoids and quinones into the culture medium of A. annua cell suspension cultures possibly due to the ability of CDs to form inclusion complexes with hydrophobic molecules. PMID:25338048

  20. Enhanced Production of Bioactive Isoprenoid Compounds from Cell Suspension Cultures of Artemisia annua L. Using β-Cyclodextrins

    Science.gov (United States)

    Rizzello, Francesca; De Paolis, Angelo; Durante, Miriana; Blando, Federica; Mita, Giovanni; Caretto, Sofia

    2014-01-01

    Plant cell cultures as valuable tools for the production of specific metabolites can be greatly improved by the application of elicitors including cyclodextrins (CDs) for enhancing the yields of the desired plant compounds. Here the effects of 2,6-dimethyl-β-cyclodextrins (DIMEB) on the production of carotenoids and quinones from Artemisia annua L. cell suspension cultures were investigated. The addition of 50 mM DIMEB induced an early increase of intracellular carotenoid and quinone contents, which could be observed to a higher extent for lutein (10-fold), Q9 (3-fold) and Q10 (2.5-fold). Real Time PCR analysis revealed that the expression of 1-deoxy-d-xylulose-5-phosphate reductoisomerase (DXR) gene in DIMEB treated cell cultures after three days was 2.5-fold higher than in untreated samples, thus suggesting that the DIMEB induced increase of carotenoids and quinones could be due to the induction of the plastidial isoprenoid biosynthetic route. In addition, the DIMEB treatment induced an enhanced release of carotenoids and quinones into the culture medium of A. annua cell suspension cultures possibly due to the ability of CDs to form inclusion complexes with hydrophobic molecules. PMID:25338048

  1. HPLC and GC-MS determination of bioactive compounds in microwave obtained extracts of three varieties of Labisia pumila Benth.

    Science.gov (United States)

    Karimi, Ehsan; Jaafar, Hawa Z E

    2011-01-01

    Microwave extraction of phytochemicals from medicinal plant materials has generated tremendous research interest and shown great potential. This research highlights the importance of microwave extraction in the analysis of flavonoids, isoflavonoid and phenolics and the antioxidant properties of extracts from three varieties of the Malaysian medicinal herb, Labisia pumila Benth. High and fast extraction performance ability, equal or higher extraction efficiencies than other methods, and the need for small samples and reagent volumes are some of the attractive features of this new promising microwave assisted extraction (MAE) technique. The aims of the present research were to determine the foliar phenolics and flavonoids contents of extracts of three varieties of L. pumila obtained by a microwave extraction method while flavonoid, isoflavonoid and phenolic compounds were analyzed using RP-HPLC. Furthermore, the antioxidant activities were measured by the DPPH and FRAP methods and finally, the chemical composition of the crude methanolic extracts of the leaves of all three varieties were analyzed by GS-MS. PMID:21829154

  2. Ruta montana L. leaf essential oil and extracts: characterization of bioactive compounds and suppression of crown gall disease.

    Science.gov (United States)

    Hammami, Inés; Smaoui, Slim; Hsouna, Anis Ben; Hamdi, Naceur; Triki, Mohamed Ali

    2015-01-01

    The aims of this study were to assess the antimicrobial efficacy of the leaf essential oil and the leaf extracts of R. montana against Botrytis cinerea, Fusarium oxysporum, Verticillium dahliae, Aspergillus oryzae and Fusarium solani. The oil (1.000 µg/disk) and the extracts (1.500 µg/disk) revealed a remarkable antifungal effect against the tested plant pathogenic fungi with a radial growth inhibition percentage of 40.0-80.0 % and 5.0-58.0 %, respectively along with their respective MIC values ranging from 100 to 1100 µg/mL and 250 to 3000 µg/mL. The oil had a strong detrimental effect on spore germination of all the tested plant pathogens along with the concentration as well as time-dependent kinetic inhibition of Fusarium oxysporum. Also, the oil exhibited a potent in vivo antifungal effect against Botrytis cinerea on tomato plants. Experiments carried out in plant revealed that the essential oil was slightly effective in suppression of gall formation induced by Agrobacterium tumefaciens on bitter almond. The results of this study indicate that the oil and extracts of R. montana leaves could become natural alternatives to synthetic fungicides to control certain important plant microbial diseases. The GC-MS analysis determined that 28 compounds, which represented 89.03 % of total oil, were present in the oil containing mainly 1-butene, methylcyclopropane, 2-butene and caryophyllene oxide. PMID:26417353

  3. HPLC and GC-MS Determination of Bioactive Compounds in Microwave Obtained Extracts of Three Varieties of Labisia pumila Benth.

    Directory of Open Access Journals (Sweden)

    Hawa Z.E. Jaafar

    2011-08-01

    Full Text Available Microwave extraction of phytochemicals from medicinal plant materials has generated tremendous research interest and shown great potential. This research highlights the importance of microwave extraction in the analysis of flavonoids, isoflavonoid and phenolics and the antioxidant properties of extracts from three varieties of the Malaysian medicinal herb, Labisia pumila Benth. High and fast extraction performance ability, equal or higher extraction efficiencies than other methods, and the need for small samples and reagent volumes are some of the attractive features of this new promising microwave assisted extraction (MAE technique. The aims of the present research were to determine the foliar phenolics and flavonoids contents of extracts of three varieties of L. pumila obtained by a microwave extraction method while flavonoid, isoflavonoid and phenolic compounds were analyzed using RP-HPLC. Furthermore, the antioxidant activities were measured by the DPPH and FRAP methods and finally, the chemical composition of the crude methanolic extracts of the leaves of all three varieties were analyzed by GS-MS.

  4. Molecular modeling methods in the study and design of bioactive compounds: An introduction [Métodos de Modelagem Molecular para estudo e planejamento de compostos bioativos: Uma introdução

    OpenAIRE

    Carlos Mauricio R. Sant´Anna

    2009-01-01

    This paper presents an introduction to the main methods used in molecular modeling calculations applied in the design of bioactive compounds. An introductory description of the two approaches methods predominantly used in molecular modeling studies is presented: the classical approach, which includes molecular mechanics and molecular dynamics; and the quantum mechanical approach, which includes ab initio and semi-empirical methods. We discuss how these methods can be applied to determine the ...

  5. Bioactivity of Essential Oil of Zingiber purpureum Rhizomes and Its Main Compounds against Two Stored Product Insects.

    Science.gov (United States)

    Wang, Y; You, C X; Yang, K; Wu, Y; Chen, R; Zhang, W J; Liu, Z L; Du, S S; Deng, Z W; Geng, Z F; Han, J

    2015-06-01

    The insecticidal and repellent activities of the essential oil extracted from Zingiber purpureum Roscoe rhizomes were evaluated against Tribolium castaneum (Herbst) and Lasioderma serricorne (L.) adults. During our screening program for agrochemicals from Chinese medicinal herbs and wild plants, the essential oil of Z. purpureum rhizomes was found to possess strong contact toxicity against T. castaneum and L. serricorne adults, with LD50 values of 39.0 and 16.3 µg per adult, respectively, and also showed strong fumigant toxicity against the two grain storage insects with LC50 values of 13.6 and 9.3 mg/liter of air, respectively. The essential oil obtained by hydrodistillation was investigated by gas chromatography-mass spectrometry. The main components of the essential oil were identified to be sabinene (48.1%), terpinen-4-ol (25.1%), and γ-terpinene (6.7%), followed by α-terpinene (4.3%), β-thujene (3.4%), and α-phellandrene (2.7%). Sabinene, terpinen-4-ol, and γ-terpinene were separated and purified by silica gel column chromatography and preparative thin-layer chromatography. Terpinen-4-ol showed the strongest contact toxicity against T. castaneum and L. serricorne (LD50=19.7 and 5.4 µg per adult, respectively) and also the strongest fumigant toxicity against T. castaneum and L. serricorne (LC50=3.7 and 1.3 mg/liter of air, respectively). Otherwise, sabinene and terpinen-4-ol were strongly repellent against T. castaneum as well as the essential oil, while γ-terpinene exhibited weaker repellency against T. castaneum compared with the positive control, DEET (N, N-diethyl-3-methylbenzamide). Moreover, only the essential oil exhibited strong repellency against L. serricorne, the three compounds exhibited weaker repellency against L. serricorne relative to DEET. PMID:26470212

  6. Phenolic Compounds and Bioactivity of Healthy and Infected Grapevine Leaf Extracts from Red Varieties Merlot and Vranac (Vitis vinifera L.).

    Science.gov (United States)

    Anđelković, Marko; Radovanović, Blaga; Anđelković, Ana Milenkovic; Radovanović, Vladimir

    2015-09-01

    We investigated the phenolic composition, radical scavenging activity, and antimicrobial activity of grapevine leaf extracts from two red grape varieties, Vranac and Merlot (Vitis vinifera L.). The extracts were prepared from healthy grapevine leaves and those infected by Plasmopara viticola (downy mildew). The phenolic composition of the grapevine leaf extracts was determined using spectrophotometric assays and reverse-phase high performance liquid chromatography (RP-HPLC). The radical scavenging activity of grapevine leaf extracts was determined by the 2,2-diphenyl-1-picrylhydrazyl assay, and their antimicrobial activity was determined by microwell dilution tests. The total phenolic content was higher in healthy grapevine leaf extracts than in infected grapevine leaf extracts. The RP-HPLC analysis detected significant amounts of flavonols, phenolic acids, and flavan-3-ols, and small amounts of stilbenes in the grapevine leaf extracts. Compared with the infected grapevine leaf extracts, the healthy grapevine leaf extracts were richer in flavonols, phenolic acids, and flavan-3-ols, but had lower stilbenes contents. All extracts showed strong free radical scavenging activity, which was strongly correlated with the total phenolic content (R(2) = 0.978). The extracts showed a stronger antimicrobial activity towards Gram-positive bacterial strains than towards Gram-negative bacterial strains and yeast. The phenolic compounds in grapevine leaves were responsible for their strong radical scavenging and antimicrobial activities. Together, these results demonstrate that grapevine leaves have high nutritional value and can be used as a fresh food and to prepare extracts that can be used as additives in food and medicines. PMID:26174183

  7. Molecular modeling methods in the study and design of bioactive compounds: An introduction [Métodos de Modelagem Molecular para estudo e planejamento de compostos bioativos: Uma introdução

    Directory of Open Access Journals (Sweden)

    Carlos Mauricio R. Sant´Anna

    2009-01-01

    Full Text Available This paper presents an introduction to the main methods used in molecular modeling calculations applied in the design of bioactive compounds. An introductory description of the two approaches methods predominantly used in molecular modeling studies is presented: the classical approach, which includes molecular mechanics and molecular dynamics; and the quantum mechanical approach, which includes ab initio and semi-empirical methods. We discuss how these methods can be applied to determine the molecular structure and properties from these compounds and how to make the best choice according to the problem being addressed.

  8. In vitro activity of natural honey alone and in combination with curcuma starch against Rhodotorula mucilaginosa in correlation with bioactive compounds and diastase activity

    Institute of Scientific and Technical Information of China (English)

    Moussa Ahmed; Noureddine Djebli; Saad Aissat; Baghdad Khiati; Abdelmalek Meslem; Salima Bacha

    2013-01-01

    Objective:To evaluate the in vitro activity and synergism of the combinations of natural honey and curcuma starch against Rhodotorula mucilaginosa in correlation with total phenolic, flavonoid contents, and diastase activity. Methods:The Folin-Ciocalteu test was used to determine the total polyphenols content and the flavonoid content was analyzed using by the aluminum chloride method. The antifungal activity of the natural honey, determined by an agar well diffusion assay and agar incorporation method. Results:Total phenolic content varied from (63.93±0.11) to (95.36±6.08) mg GAE/100 g honey as gallic acid equivalent. Total flavonoids content varied from (5.41±0.04) to (9.94±0.54) mg CE/100 g. Diastase activity values were between (7.3±2.8) and (26±2.8). The zone inhibition diameter for the six honey samples without starch ranged between 6 and 20 mm. When starch was mixed with honey and then added to well, a zone inhibition increase diameter 7 and 21 mm. The percentage increase was noticed with each variety and it ranged between 5% and 62.5%. The minimal inhibitory concentrations for the six varieties of honey without starch against Rhodotorula mucilaginosa ranged between 28%and 36%(v/v). When starch was incubated with honey and then added to media, a minimal inhibitory concentration drop has been noticed with each variety. It ranged between 6.66%and 20%(w/v). No significant correlation was established between diastase activity and bioactive compounds. Conclusions:The mixture of curcuma starch and honey could lead to the development of new combination antibiotics against Rhodotorula infections.

  9. Antioxidant activity and identification of bioactive compounds from leaves of Anthocephalus cadamba by ultra-performance liquid chromatography/electrospray ionization quadrupole time of flight mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    Madhu Chandel; Upendra Sharma; Neeraj Kumar; Bikram Singh; Satwinderjeet Kaur

    2012-01-01

    Objective: To evaluate the antioxidant potential of different extract/fractions of Anthocephalus cadamba (A. cadamba) (Roxb.) Miq. (Rubiaceae) and study the tentative identification of their active constituents. Methods: The extract/fractions were screened for antioxidant activity using various in vitro assays viz. DPPH assay, ABTS assay, superoxide anion radical scavenging assay, reducing power assay and plasmid DNA nicking assay. Total phenolic content of extract/fractions was determined by colorimetric method. An ultra-performance LC-electrospray-quadrupole-time of flight mass spectrometry method was used to analyse the active constituents of extract/fractions of A. cadamba. Results: The ethyl acetate fraction was found to be most active fraction in all the assays as compared to other extract/fractions. The IC50 value of ethyl acetate fraction (ETAC fraction) was 21.24 μg/mL, 1.12 μg/mL, 9.68 μg/mL and 57.81 μg/mL in DPPH assay, ABTS assay, reducing power assay and superoxide scavenging assay respectively. All the extract/fractions also showed the potential to protect the plasmid DNA (pBR322) against the attack of hydroxyl radicals generated by Fenton’s reagent. The bioactive compounds were identified by UPLC-ESI-QTOF-MS, by comparing the mass and λmax with literature values. Conclusions: The potential of the extract/fractions to scavenge different free radicals in different systems indicated that they may be useful therapeutic agents for treating radical-related pathologic damage.

  10. Bioactive phytochemicals in flaxseed

    OpenAIRE

    Johnsson, Pernilla

    2009-01-01

    Flaxseed (Linum usitatissimum L.) is rich in health-promoting bioactive compounds. Among plant foods, flaxseed has the highest content of lignans, mainly in the form of secoisolariciresinol diglucoside (SDG). Flaxseed oil also has a very high concentration of the essential omega-3 fatty acid alpha-linolenic acid (ALA). This thesis presents studies on both SDG and ALA. An HPLC method for quantification of SDG in hydrolysed flaxseed extracts was developed and used to compare the SDG content in ...

  11. Bioactive compounds from Carissa opaca roots and xanthine oxidase and alpha-amylase inhibitory activities of their methanolic extract and its fractions in different solvents

    Directory of Open Access Journals (Sweden)

    Ramsha Saeed

    2015-01-01

    Full Text Available Background: Carissa opaca is known for its many ethnomedicinal uses. There was a need to study its bioactivities and identify its phytochemicals. Objective: The objective was to isolate and identify phytochemicals from roots of C. opaca and to evaluate xanthine oxidase (XO and alpha-amylase inhibitory activities of their methanolic extract and its fractions. Materials and Methods: Methanolic extract of finely divided powder of roots of C. opaca was obtained by cold maceration, followed by its fractionation to obtain hexane, chloroform, ethyl acetate, n-butanolic, and aqueous fractions. Phytochemicals screening was done by standard protocols. XO and alpha-amylase inhibitory activities of the methanolic extract and its fractions were studied. The most active ethyl acetate fraction was subjected to the column and thin layer chromatography to isolate its compounds, which were identified by gas chromatography-mass spectrometry and high-performance liquid chromatography comparison. Results: Methanolic extract displayed significant activity against both the enzymes with IC 50 of 156.0 mg/mL and 5.6 mg/mL for XO and alpha-amylase, respectively. Ethyl acetate fraction showed highest activity against both the enzymes with IC 50 of 129 mg/mL and 4.9 mg/mL for XO and alpha-amylase, respectively. Chloroform fraction had IC 50 of 154.2 mg/mL and 5.5 mg/mL for XO and alpha-amylase, respectively. Aqueous fraction exhibited significant efficacy against alpha-amylase (IC 50 5.0 mg/mL. Hexane fraction showed good activity against alpha-amylase in a dose-dependent manner but exhibited opposite trend against XO. The compounds isolated from ethyl acetate fraction included limonene, vanillin, lupeol, rutin, quercetin, b-sitosterol, Vitamin E, 2-hydroxyacetophenone, naphthalenone, 2,3,3-trimethyl-2-(3-methylbuta-1,3-dienyl-6-methylenecyclohexanone, and 2-benzenedicarboxylic acid, mono(2-ethylhexyl ester. Conclusions: Moderately polar phytochemicals of C. opaca roots

  12. Bioactive compounds from marine actinomycetes

    OpenAIRE

    Solanki, Renu; Khanna, Monisha; Lal, Rup

    2008-01-01

    Actinomycetes are one of the most efficient groups of secondary metabolite producers and are very important from an industrial point of view. Among its various genera, Streptomyces, Saccharopolyspora, Amycolatopsis, Micromonospora and Actinoplanes are the major producers of commercially important biomolecules. Several species have been isolated and screened from the soil in the past decades. Consequently the chance of isolating a novel actinomycete strain from a terrestrial habitat, which wou...

  13. Technologies for the Synthesis of mRNA-Encoding Libraries and Discovery of Bioactive Natural Product-Inspired Non-Traditional Macrocyclic Peptides

    Directory of Open Access Journals (Sweden)

    Hiroaki Suga

    2013-03-01

    Full Text Available In this review, we discuss emerging technologies for drug discovery, which yields novel molecular scaffolds based on natural product-inspired non-traditional peptides expressed using the translation machinery. Unlike natural products, these technologies allow for constructing mRNA-encoding libraries of macrocyclic peptides containing non-canonical sidechains and N-methyl-modified backbones. The complexity of sequence space in such libraries reaches as high as a trillion (>1012, affording initial hits of high affinity ligands against protein targets. Although this article comprehensively covers several related technologies, we discuss in greater detail the technical development and advantages of the Random non-standard Peptide Integration Discovery (RaPID system, including the recent identification of inhibitors against various therapeutic targets.

  14. COMBINATORIAL LIBRARIES

    DEFF Research Database (Denmark)

    1997-01-01

    The invention provides a method for the production of a combinatorial library of compound of general formula (I) using solid phase methodologies. The cleavage of the array of immobilised compounds of the phthalimido type from the solid support matrix is accomplished by using an array of dinucleop......The invention provides a method for the production of a combinatorial library of compound of general formula (I) using solid phase methodologies. The cleavage of the array of immobilised compounds of the phthalimido type from the solid support matrix is accomplished by using an array of...... dinucleophiles, e.g. hydrazines (hydrazinolysis) or N-hydroxylamines, whereby a combinatorial dimension is introduced in the cleavage step. The invention also provides a compound library....

  15. SENYAWA BIOAKTIF RIMPANG JAHE (Zingiber officinale Roscue MENINGKATKAN RESPON SITOLITIK SEL NK TERHADAP SEL KANKER DARAH K-562 IN VITRO [Ginger Root Bioactive Compounds Increased Cytolitic Response of Natural Killer (NK Cells Against Leucemic Cell Line K-562 In Vitro

    Directory of Open Access Journals (Sweden)

    Fransiska Rungkat Zakaria 2

    2006-08-01

    Full Text Available Natural killer (NK cell, a kind of lymphocyte cells, plays an important role in attacking infectious, immature, and cancer cell. Its function could be modulated by food bioactive compounds. This experiment was conducted to investigate the effects of ginger root bioactive compounds such as oleoresin, gingerol, and shogaol on cytolitic response of NK cell in vitro. Lymphocyte cells were isolated by centrifugation on ficoll-hypaque density (1,77 ?0,001 g/ml method. Leukemic cells line K-562 as target cells(TC labelled by [3H]-timidin, together with lymphocyte as effector cell (EC were cultured in two ratio levels of EC : TC equal to 1:50 and 1:100, and two culture conditions, for 4 hours, respectively. Paraquate dichloride (1,1-dimethyl-4,4-bipyridilium dichloride 3 mM was used to induce stress oxidative circumstance. Cytolytic capacity of NK cells was determined by percentage of TC lysed by NK cells, in normal and oxidative stress conditions. Statistical analysis showed that the effects of ginger bioactive compounds on cytolytic response of NK cell depended on the culture conditions, as shown by cultures in the presence of oleoresin, and gingerol, but not shogaol. In the lymphocyte culture without stress oxidative, oleoresin, gingerol and shogaol compounds increased significantly cytolytic response of NK cells cultured at a ratio of TC : EC equal to 1:50, with the highest increament of 65 % at oleoresin concentration of 50 ?g/ml. However, in culture at a ratio of TC : EC equals to 1:100, only oleoresin at a concentration of 50 ?g/ml increased significantly cytolytic response of NK cells with the highest increament of 8 %. Shogaol did not affect significantly NK cells cytolytic response. Under stress oxidative conditions, shogaol increased significantly cytolytic response of NK cells cultured at a ratio of TC:EC equal to 1:50, but the highest increament of 56 % , was by oleoresin at concentration of 50 ?g/ml. Meanwhile, oleoresin and gingerol did

  16. Acoustic Sample Deposition MALDI-MS (ASD-MALDI-MS): A Novel Process Flow for Quality Control Screening of Compound Libraries.

    Science.gov (United States)

    Chin, Jefferson; Wood, Elizabeth; Peters, Grace S; Drexler, Dieter M

    2016-02-01

    In the early stages of drug discovery, high-throughput screening (HTS) of compound libraries against pharmaceutical targets is a common method to identify potential lead molecules. For these HTS campaigns to be efficient and successful, continuous quality control of the compound collection is necessary and crucial. However, the large number of compound samples and the limited sample amount pose unique challenges. Presented here is a proof-of-concept study for a novel process flow for the quality control screening of small-molecule compound libraries that consumes only minimal amounts of samples and affords compound-specific molecular data. This process employs an acoustic sample deposition (ASD) technique for the offline sample preparation by depositing nanoliter volumes in an array format onto microscope glass slides followed by matrix-assisted laser desorption/ionization mass spectrometric (MALDI-MS) analysis. An initial study of a 384-compound array employing the ASD-MALDI-MS workflow resulted in a 75% first-pass positive identification rate with an analysis time of <1 s per sample. PMID:26203056

  17. Novel selection methods for DNA-encoded chemical libraries

    Science.gov (United States)

    Chan, Alix I.; McGregor, Lynn M.; Liu, David R.

    2015-01-01

    Driven by the need for new compounds to serve as biological probes and leads for therapeutic development and the growing accessibility of DNA technologies including high-throughput sequencing, many academic and industrial groups have begun to use DNA-encoded chemical libraries as a source of bioactive small molecules. In this review, we describe the technologies that have enabled the selection of compounds with desired activities from these libraries. These methods exploit the sensitivity of in vitro selection coupled with DNA amplification to overcome some of the limitations and costs associated with conventional screening methods. In addition, we highlight newer techniques with the potential to be applied to the high-throughput evaluation of DNA-encoded chemical libraries. PMID:25723146

  18. Study of bioactive compounds in spices (Syzygium aromaticum L, Cinnamomum zeylanicum Blume and Myristica fragrans Houtt) processed by ionizing radiation; Estudo dos compostos bioativos em especiarias (Syzygium aromaticum L, Cinnamomum zeylanicum Blume e Myristica fragans Houtt) processadas por radiacao ionizante

    Energy Technology Data Exchange (ETDEWEB)

    Duarte, Renato Cesar

    2014-07-01

    Spices and aromatic herbs are divided into leaves, flowers, bud, seeds bark or dry roots from different plants and it is possible to define them as products of highly flavored vegetal origin that volatize easily when incorporated in small quantities to food products and contribute to its aroma, flavor, color or even to its preservation. Nowadays, people look for its functional properties, bioactive compounds and sensory qualities. A big problem is the reduction of the quantity of these compounds throughout the production chain from the harvest process, storage and distribution. For a long time researchers and industries have concentrated on perfecting the processes of the production chain seeking to guarantee the sanitary and food safety, preserving foodstuffs for a long period and an increase in its lifespan without drastically altering its properties. Due to homemade products and the lack of compliance with good practices in its production chain, the spices can contain a high amount of microbiology causing serious complications to the health of the consumer and the radiation processing is often used for reduce these problems. With this finding, the objectives of this work were: Analyze the oil antifungal properties of spices irradiated with average doses (2.5; 5; 7.5 and 10 kGy); Study the average doses (5 and 10 kGy) and high dose (20 and 30 kGy) effects of gamma radiation {sup 60}Co in the bioactive compounds of the spices - cloves, cinnamon and nutmeg; Identify the oils compounds; Identify the volatile compounds in the headspace of the oils and the in natura spices. Identify the compounds of the nonvolatile part of the nutmeg; Identify the chiral compounds of the cinnamon. Comparing the control samples (not irradiated) with the processed at the described doses, regarding the oil antifungal properties it was possible to verify the efficiency and later that the irradiation did not interfered in its efficiency; Regarding to the others tests in this work, the

  19. Effect of the perforation level of recycled-LDPE bags on the modification of the atmosphere development, bioactive compounds content, and other qualities of Jalapeño peppers during storage.

    Science.gov (United States)

    de Jesús Ornelas-Paz, José; Castañeda-Jiménez, Andrés C; Estrada-Alvarado, María I; Ramos-Aguilar, Olivia P; Ibarra-Junquera, Vrani; Pérez-Martínez, Jaime D; Escalante-Minakata, Pilar; Guevara-Arauza, Juan C; Ruiz-Cruz, Saúl

    2015-10-01

    The impact of modified atmosphere packaging on the content of selected bioactive compounds and other quality attributes of Jalapeño peppers has not been well studied. In this study, Jalapeño peppers were packed in low-cost bags (composed of recycled-LDPE) that had been perforated at several levels (0-4 holes). Packages were stored at 7 °C for 6 weeks. Samples of unpacked peppers were stored at 23 and 7 °C and were used as control groups. The quality of the peppers and the gas composition inside of the packages were evaluated during storage. The best modified atmosphere was obtained with unperforated bags. Significant loss of weight and firmness were prevented by packaging. The loss of weight and firmness were 20.2-82.6 and 32-100 % in unpacked peppers. Low levels of fermentative metabolites accumulated in packed peppers in unperforated bags and in bags with 1 perforation. The tristimulus color and the bioactive compounds content (phenols, ascorbic acid, β-carotene, and capsaicinoids) remained unchanged in packed peppers. These quality attributes changed gradually in peppers that were stored at 23 °C. The tested bags represent a cost-effective alternative to preserve the quality of intact Jalapeño peppers. PMID:26396386

  20. Active compounds from a diverse library of triazolothiadiazole and triazolothiadiazine scaffolds: synthesis, crystal structure determination, cytotoxicity, cholinesterase inhibitory activity, and binding mode analysis.

    Science.gov (United States)

    Khan, Imtiaz; Ibrar, Aliya; Zaib, Sumera; Ahmad, Sarfraz; Furtmann, Norbert; Hameed, Shahid; Simpson, Jim; Bajorath, Jürgen; Iqbal, Jamshed

    2014-11-01

    In an effort to identify novel cholinesterase candidates for the treatment of Alzheimer's disease (AD), a diverse array of potentially bioactive compounds including triazolothiadiazoles (4a-h and 5a-f) and triazolothiadiazines (6a-h) was obtained in good yields through the cyclocondensation reaction of 4-amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol (3) with various substituted aryl/heteroaryl/aryloxy acids and phenacyl bromides, respectively. The structures of newly prepared compounds were confirmed by IR, (1)H and (13)C NMR spectroscopy and, in case of 4a, by single crystal X-ray diffraction analysis. The purity of the synthesized compounds was ascertained by elemental analysis. The newly synthesized conjugated heterocycles were screened for cholinesterase inhibitory activity against electric eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinesterase (hBChE). Among the evaluated hybrids, several compounds were identified as potent inhibitors. Compounds 5b and 5d were most active with an IC50 value of 3.09 ± 0.154 and 11.3 ± 0.267 μM, respectively, against acetylcholinesterase, whereas 5b, 6a and 6g were most potent against butyrylcholinesterase, with an IC50 of 0.585 ± 0.154, 0.781 ± 0.213, and 1.09 ± 0.156 μM, respectively, compared to neostigmine and donepezil as standard drugs. The synthesized heteroaromatic compounds were also tested for their cytotoxic potential against lung carcinoma (H157) and vero cell lines. Among them, compound 6h exhibited highest antiproliferative activity against H157 cell lines, with IC50 value of 0.96 ± 0.43 μM at 1mM concentration as compared to vincristine (IC50=1.03 ± 0.04 μM), standard drug used in this study. PMID:25257911

  1. Bioactive saponins from Dioscorea futschauensis.

    Science.gov (United States)

    Liu, H W; Hu, K; Zhao, Q C; Cui, C B; Kobayashi, H; Yao, X S

    2002-08-01

    A new anti-neoplastic spirostanol saponin, (25S)-spirost-5-en-3 beta, 27-diol-3O-[alpha-L-rhamnopyranosyl(1-->2)-beta-D-glucopyranosyl (1-->3)]-beta-D-glucopyranoside and three known compounds viz. prosapogenin A of dioscin, dioscin and gracilin were isolated from Dioscorea futschauensis by bioactivity-guided fractionation. Their structures were elucidated mainly by means of spectroscopic analysis. Their bioactivity against Pyricularia oryzae and cytotoxic activity on ts-FT210 cell line was evaluated. PMID:12227201

  2. Excipient Nanoemulsions for Improving Oral Bioavailability of Bioactives

    OpenAIRE

    Laura Salvia-Trujillo; Olga Martín-Belloso; David Julian McClements

    2016-01-01

    The oral bioavailability of many hydrophobic bioactive compounds found in natural food products (such as vitamins and nutraceuticals in fruits and vegetables) is relatively low due to their low bioaccessibility, chemical instability, or poor absorption. Most previous research has therefore focused on the design of delivery systems to incorporate isolated bioactive compounds into food products. However, a more sustainable and cost-effect approach to enhancing the functionality of bioactive com...

  3. Planctomycetes as Novel Source of Bioactive Molecules

    Science.gov (United States)

    Graça, Ana P.; Calisto, Rita; Lage, Olga M.

    2016-01-01

    Marine environments are a fruitful source of bioactive compounds some of which are the newest leading drugs in medicinal therapeutics. Of particular importance are organisms like sponges and macroalgae and their associated microbiome. Planctomycetes, abundant in macroalgae biofilms, are promising producers of bioactive compounds since they share characteristics, like large genomes and complex life cycles, with the most bioactive bacteria, the Actinobacteria. Furthermore, genome mining revealed the presence of secondary metabolite pathway genes or clusters in 13 analyzed Planctomycetes genomes. In order to assess the antimicrobial production of a large and diverse collection of Planctomycetes isolated from macroalgae from the Portuguese coast, molecular, and bioactivity assays were performed in 40 bacteria from several taxa. Two genes commonly associated with the production of bioactive compounds, nonribosomal peptide synthetases (NRPS), and polyketide synthases (PKS) genes were screened. Molecular analysis revealed that 95% of the planctomycetes potentially have one or both secondary bioactive genes; 85% amplified with PKS-I primers and 55% with NRPS primers. Some of the amplified genes were confirmed to be involved in secondary metabolite pathways. Using bioinformatic tools their biosynthetic pathways were predicted. The secondary metabolite genomic potential of strains LF1, UC8, and FC18 was assessed using in silico analysis of their genomes. Aqueous and organic extracts of the Planctomycetes were evaluated for their antimicrobial activity against an environmental Escherichia coli, E. coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, Bacillus subtilis ATCC 6633, and a clinical isolate of Candida albicans. The screening assays showed a high number of planctomycetes with bioactive extracts revealing antifungal (43%) and antibacterial (54%) activity against C. albicans and B. subtilis, respectively. Bioactivity was observed in

  4. Novel ingredients from brewers' spent grain - bioactivity in cell culture model systems and bioactivity retention in fortified food products

    OpenAIRE

    McCarthy, Aoife Louise

    2013-01-01

    Functional food ingredients, with scientifically proven and validated bioactive effects, present an effective means of inferring physiological health benefits to consumers to reduce the risk of certain diseases. The search for novel bioactive compounds for incorporation into functional foods is particularly active, with brewers’ spent grain (BSG, a brewing industry co-product) representing a unique source of potentially bioactive compounds. The DNA protective, antioxidant and immunomodulatory...

  5. Ligand-free Suzuki-Miyaura coupling with sulfur-modified gold-supported palladium in the synthesis of a conformationally-restricted cyclopropane compound library with three-dimensional diversity.

    Science.gov (United States)

    Arisawa, Mitsuhiro; Sato, Takatoshi; Hoshiya, Naoyuki; Al-Amin, Mohammad; Kogami, Yuji; Shuto, Satoshi

    2014-05-12

    A conformationally restricted privileged structure library with stereochemical diversity for a "fragment growth" methodology comprising 90 compounds was designed and systematically and efficiently synthesized using sulfur-modified Au-supported Pd (SAPd)-catalyzed ligand-free Suzuki-Miyaura coupling of vinyl iodide promoted by microwave and subsequent amidation in liquid-phase combinatorial chemistry as key reactions. Evaluation of the compounds with a 20-kinase panel indicated the usefulness of this "fragment growth" methodology for finding hit library compounds for fragment-based drug discovery. PMID:24697302

  6. Bioactivities and Health Benefits of Wild Fruits.

    Science.gov (United States)

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

    2016-01-01

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

  7. Bioactivities and Health Benefits of Wild Fruits

    Directory of Open Access Journals (Sweden)

    Ya Li

    2016-08-01

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

  8. Flavonoid-mediated inhibition of intestinal ABC transporters may affect the oral bioavailability of drugs, food-borne toxic compounds and bioactive ingredients

    NARCIS (Netherlands)

    Brand, W.; Schutte, M.E.; Bladeren, van P.J.; Rietjens, I.M.C.M.

    2006-01-01

    The transcellular transport of ingested food ingredients across the intestinal epithelial barrier is an important factor determining bioavailability upon oral intake. This transcellular transport of many chemicals, food ingredients, drugs or toxic compounds over the intestinal epithelium can be high

  9. Correlation, by multivariate statistical analysis, between the scavenging capacity against reactive oxygen species and the bioactive compounds from frozen fruit pulps

    OpenAIRE

    Lizziane Cynara Vissotto; Eliseu Rodrigues; Renan Campos Chisté; Marta de Toledo Benassi; Adriana Zerlotti Mercadante

    2013-01-01

    The contents of total phenolic compounds (TPC), total flavonoids (TF), and ascorbic acid (AA) of 18 frozen fruit pulps and their scavenging capacities against peroxyl radical (ROO•), hydrogen peroxide (H2O2), and hydroxyl radical (•OH) were determined. Principal Component Analysis (PCA) showed that TPC (total phenolic compounds) and AA (ascorbic acid) presented positive correlation with the scavenging capacity against ROO•, and TF (total flavonoids) showed positive correlation with the scaven...

  10. Free radical scavenging capacity, anticandicidal effect of bioactive compounds from Sida Cordifolia L., in combination with nystatin and clotrimazole and their effect on specific immune response in rats

    Directory of Open Access Journals (Sweden)

    Ouédraogo Maurice

    2012-12-01

    Full Text Available Abstract Background Infectious diseases caused by fungi are still a major threat to public health, despite numerous efforts by researchers. Use of ethnopharmacological knowledge is one attractive way to reduce empiricism and enhance the probability of success in new drug-finding efforts. In this work, the total alkaloid compounds (AC from Sida cordifolia L. (Malvaceae have been investigated for their free radical scavenging capacity, antifungal and immunostimulatory properties. Method The antifungal activity was investigated against five candida strains using the microplate dilution method and the Fractional Inhibitory Concentration Index (FICI of compounds was evaluated. The antioxidant activity of the samples was evaluate using three separate methods, at last, the immunostimulatory effect on immunosuppressed wistar rats was performed. Results As for the antifungal activity, result varied according to microorganism. The results obtained in this antifungal activity were interesting and indicated a synergistic effect between alkaloid compounds and the antifungal references such as Nystatin and Clotrimazole. Antioxidant capacity noticed that the reduction capacity of DPPH radicals obtained the best result comparatively to the others methods of free radical scavenging. Our results showed a low immunostimulatory effect and this result could be explained by the lack of biologically active antioxidants such as polyphenol compounds lowly contained in the alkaloid compounds. Conclusion The results of this study showed that alkaloid compounds in combination with antifungal references (Nystatin and Clotrimazole exhibited antimicrobial effects against candida strains tested. The results supported the utilization of these plants in infectious diseases particularly in treatment of candida infections.

  11. Virtual Screening Approaches in Identification of Bioactive Compounds Akin to Delphinidin as Potential HER2 Inhibitors for the Treatment of Breast Cancer.

    Science.gov (United States)

    Patidar, Kavisha; Deshmukh, Aruna; Bandaru, Srinivas; Lakkaraju, Chandana; Girdhar, Amandeep; Vr, Gutlapalli; Banerjee, Tushar; Nayarisseri, Anuraj; Singh, Sanjeev Kumar

    2016-01-01

    Small molecule tyrosine kinase inhibitors targeting HER 2 receptors have emerged as an important therapeutic approach in inhibition of downstream proliferation and survival signals for the treatment of breast cancers. Recent drug discovery efforts have demonstrated that naturally occurring polyphenolic compounds like delphinidin have potential to inhibit proliferation and promote apoptosis of breast cancer cells by targeting HER2 receptors. While delphinidin may thus reduce tumour size, it is associated with serious side effects like dysphonia. Owing to the narrow therapeutic window of delphinidin, the present study aimed to identify high affinity compounds targeting HER2 with safer pharmacological profiles than delphinidin through virtual screening approaches. Delphinidin served as the query parent for identification of structurally similar compounds by Tanimoto-based similarity searching with a threshold of 95% against the PubChem database. The compounds retrieved were further subjected to Lipinski and Verber's filters to obtain drug like agents, then further filtered by diversity based screens with a cut off of 0.6. The compound with Pubchem ID: 91596862 was identified to have higher affinity than its parent. In addition it also proved to be non-toxic with a better ADMET profile and higher kinase activity. The compound identified in the study can be put to further in vitro drug testing to complement the present study. PMID:27221932

  12. Bacillus subtilis subsp. subtilis CBMDC3f with antimicrobial activity against Gram-positive foodborne pathogenic bacteria: UV-MALDI-TOF MS analysis of its bioactive compounds.

    Science.gov (United States)

    Torres, M J; Petroselli, G; Daz, M; Erra-Balsells, R; Audisio, M C

    2015-06-01

    In this work a new Bacillus sp. strain, isolated from honey, was characterized phylogenetically. Its antibacterial activity against three relevant foodborne pathogenic bacteria was studied; the main bioactive metabolites were analyzed using ultraviolet matrix assisted laser desorption-ionization mass spectrometry (UV-MALDI MS). Bacillus CBMDC3f was phylogenetically characterized as Bacillus subtilis subsp. subtilis after rRNA analysis of the 16S subunit and the gyrA gene (access codes Genbank JX120508 and JX120516, respectively). Its antibacterial potential was evaluated against Listeria monocytogenes (9 strains), B. cereus (3 strains) and Staphylococcus aureus ATCC29213. Its cell suspension and cell-free supernatant (CFS) exerted significant anti-Listeria and anti-S. aureus activities, while the lipopeptides fraction (LF) also showed anti-B. cereus effect. The UV-MALDI-MS analysis revealed surfactin, iturin and fengycin in the CFS, whereas surfactin predominated in the LF. The CFS from CBMDC3f contained surfactin, iturin and fengycin with four, two and four homologues per family, respectively, whereas four surfactin, one iturin and one fengycin homologues were identified in the LF. For some surfactin homologues, their UV-MALDI-TOF/TOF (MS/MS; Laser Induced Decomposition method, LID) spectra were also obtained. Mass spectrometry analysis contributed with relevant information about the type of lipopeptides that Bacillus strains can synthesize. From our results, surfactin would be the main metabolite responsible for the antibacterial effect. PMID:25820813

  13. 香榧坚果生物活性成分与抗氧化研究进展%Recent Advances in Research on Bioactive Compounds and Anfioxidant Activity of Torreya grandis

    Institute of Scientific and Technical Information of China (English)

    李兴飞; 郜海燕; 陈杭君; 房祥军; 葛林梅

    2012-01-01

    香榧为浙江著名的坚果,其富含多种生物活性成分,诸如油脂、二萜类、多酚类等都具有一定的药用及生物活性。本文综述了香榧的生物活性成分,并探讨其与氧化劣变之间的关系,可为更好的贮存坚果提供借鉴,也为进一步发展利用香榧资源提供参考。%Torreya grandis is a conifer of the Cephalotaxaceae family. It is found only in China, mostly in Zhejiang Province. The seed of Torreya grandis, known as 'Xiangfei', is edible and has been recognized as a valuable tree nut for their high content of various medical and biological active compounds, such as essential fatty acids, polyphenols and diterpenoids. Here we review bioactive compounds in the seeds and discuss their association with oxidative deteriorations during storage with the purpose to provide some reference for better storage and utilization of Torreya grandis seeds.

  14. Chemical Library Screens Targeting an HIV-1 Accessory Factor/Host Cell Kinase Complex Identify Novel Anti-retroviral Compounds

    OpenAIRE

    Emert-Sedlak, Lori; Kodama, Toshiaki; Lerner, Edwina C.; Dai, Weixiang; Foster, Caleb; Day, Billy W.; Lazo, John S.; Smithgall, Thomas E

    2009-01-01

    Nef is an HIV-1 accessory protein essential for AIDS progression and an attractive target for drug discovery. Lack of a catalytic function makes Nef difficult to assay in chemical library screens. We developed a high-throughput screening assay for inhibitors of Nef function by coupling it to one of its host cell binding partners, the Src-family kinase Hck. Hck activation is dependent upon Nef in this assay, providing a direct readout of Nef activity in vitro. Using this screen, a unique diphe...

  15. Quantitative Analysis of Bioactive Compounds from Aromatic Plants by Means of Dynamic Headspace Extraction and Multiple Headspace Extraction-Gas Chromatography-Mass Spectrometry.

    Science.gov (United States)

    Omar, Jone; Olivares, Maitane; Alonso, Ibone; Vallejo, Asier; Aizpurua-Olaizola, Oier; Etxebarria, Nestor

    2016-04-01

    Seven monoterpenes in 4 aromatic plants (sage, cardamom, lavender, and rosemary) were quantified in liquid extracts and directly in solid samples by means of dynamic headspace-gas chromatography-mass spectrometry (DHS-GC-MS) and multiple headspace extraction-gas chromatography-mass spectrometry (MHSE), respectively. The monoterpenes were 1st extracted by means of supercritical fluid extraction (SFE) and analyzed by an optimized DHS-GC-MS. The optimization of the dynamic extraction step and the desorption/cryo-focusing step were tackled independently by experimental design assays. The best working conditions were set at 30 °C for the incubation temperature, 5 min of incubation time, and 40 mL of purge volume for the dynamic extraction step of these bioactive molecules. The conditions of the desorption/cryo-trapping step from the Tenax TA trap were set at follows: the temperature was increased from 30 to 300 °C at 150 °C/min, although the cryo-trapping was maintained at -70 °C. In order to estimate the efficiency of the SFE process, the analysis of monoterpenes in the 4 aromatic plants was directly carried out by means of MHSE because it did not require any sample preparation. Good linearity (r2) > 0.99) and reproducibility (relative standard deviation % <12) was obtained for solid and liquid quantification approaches, in the ranges of 0.5 to 200 ng and 10 to 500 ng/mL, respectively. The developed methods were applied to analyze the concentration of 7 monoterpenes in aromatic plants obtaining concentrations in the range of 2 to 6000 ng/g and 0.25 to 110 μg/mg, respectively. PMID:26925555

  16. Bioactive compounds content of chimarrão infusions related to the moisture of yerba maté (Ilex Paraguariensis leaves

    Directory of Open Access Journals (Sweden)

    Deborah H. M. Bastos

    2006-05-01

    Full Text Available The aim of this study was to evaluate the effects of the processing stages of yerba maté (Ilex paraguariensis on the moisture content of the leaves and the efficiency of the aqueous extraction of some bioactive substances. Samples of yerba maté were analyzed for caffeine, phenolic acids (caffeic acid, 5-caffeoilquinic acid and flavonoids (quercetin, kaempferol and myricetin by HPLC equipped with a diode array detector. Processing widely influenced the caffeine and 5-caffeoilquinic acid content of the aqueous extract (p A erva mate (Ilex paraguariensis é a matéria prima para três tipos de bebidas largamente consumidas na América do Sul. Substâncias bioativas presentes neste produto como a cafeína e os ácidos clorogênicos têm recebido especial atenção da comunidade científica. O objetivo deste trabalho é avaliar o efeito do processamento da erva mate no teor de umidade das folhas e a eficiência da extração aquosa de algumas substâncias bioativas. Amostras de erva mate coletadas no Paraná, Brasil foram objeto deste estudo. Cafeína, ácidos fenólicos (ácido cafeico e ácido 5-cafeoilquinico e flavonóides (quercitina, miricetina e caempferol foram analisados por HPLC equipado com detector de arranjo de diodos. Os teores de ácido 5-cafeoilquinico e cafeína do extrato aquoso variam em função da etapa do processamento (p0,9. O ácido cafeico foi determinado em 45% das infusões obtidas das folhas secas e quercitina, miricetina e caempferol não foram detectados nesses extratos.

  17. Identification of Selective Inhibitors of the Plasmodium falciparum Hexose Transporter PfHT by Screening Focused Libraries of Anti-Malarial Compounds

    Science.gov (United States)

    Johnson, Alex; Elya, Carolyn; Anderson, Johanna; Clark, Julie; Connelly, Michele; Yang, Lei; Min, Jaeki; Sato, Yuko; Guy, R. Kiplin; Landfear, Scott M.

    2015-01-01

    Development of resistance against current antimalarial drugs necessitates the search for novel drugs that interact with different targets and have distinct mechanisms of action. Malaria parasites depend upon high levels of glucose uptake followed by inefficient metabolic utilization via the glycolytic pathway, and the Plasmodium falciparum hexose transporter PfHT, which mediates uptake of glucose, has thus been recognized as a promising drug target. This transporter is highly divergent from mammalian hexose transporters, and it appears to be a permease that is essential for parasite viability in intra-erythrocytic, mosquito, and liver stages of the parasite life cycle. An assay was developed that is appropriate for high throughput screening against PfHT based upon heterologous expression of PfHT in Leishmania mexicana parasites that are null mutants for their endogenous hexose transporters. Screening of two focused libraries of antimalarial compounds identified two such compounds that are high potency selective inhibitors of PfHT compared to human GLUT1. Additionally, 7 other compounds were identified that are lower potency and lower specificity PfHT inhibitors but might nonetheless serve as starting points for identification of analogs with more selective properties. These results further support the potential of PfHT as a novel drug target. PMID:25894322

  18. Controle biológico da mancha-aquosa do melão por compostos bioativos produzidos por Bacillus spp. Biocontrol of bacterial fruit blotch of melon by bioactive compounds produced by Bacillus spp.

    Directory of Open Access Journals (Sweden)

    Elizama Roza Santos

    2006-09-01

    Full Text Available A mancha-aquosa, causada por Acidovorax avenae subsp. citrulli (Aac causa grandes prejuízos à cultura do melão. O controle dessa doença foi estudado in vivo, com microbiolização de sementes de melão Amarelo infectadas, com líquidos fermentados de Bacillus subtilis R14, B. megaterium pv. cerealis RAB7, B. pumilus C116 e Bacillus sp. MEN2, com e sem células bacterianas. O mecanismo de ação dos isolados foi estudado in vitro pelo método de difusão em ágar e os compostos bioativos parcialmente caracterizados por testes de hemólise e atividade surfactante. Nos testes in vivo, não houve diferença significativa entre os tratamentos com e sem células, indicando que o controle ocorreu devido à presença de compostos bioativos produzidos durante as fermentações. Todos os tratamentos diferiram da testemunha sem diferir entre si (P=0,05%. B. megaterium pv. cerealis RAB7 proporcionou redução da incidência (89,1% e do índice de doença (92,7%, elevou o período de incubação da mancha-aquosa de 9,8 para 11,9 dias e reduziu a AACPD de 3,36 para 0,17. In vitro, todos isolados apresentaram antibiose contra Aac e os compostos bioativos foram parcialmente caracterizados como lipopeptídeos.The bacterial fruit blotch, caused by the bacterium Acidovorax avenae subsp. citrulli (Aac, is responsible for great losses in melon production. The control of this disease was investigated in vivo by treating infected yellow melon seeds with fermented broths of B. subtilis R14, B. megaterium pv. cerealis RAB7, B. pumilus C116 and Bacillus sp. MEN2, with and without bacterial cells. The mechanism of action of the strains was studied in vitro by the agar diffusion technique. The bioactive compounds produced were partially characterized by hemolysis test and surfactant activity. Regarding the tests conducted in vivo there was no statistical difference between the treatments with and without bacterial cells, which indicated that the control was due to the

  19. Thymoquinone, the Nigella sativa Bioactive Compound, Prevents Circulatory Oxidative Stress Caused by 1,2-Dimethylhydrazine in Erythrocyte during Colon Postinitiation Carcinogenesis

    OpenAIRE

    Hanene Jrah Harzallah; Rahma Grayaa; Wafa Kharoubi; Aya Maaloul; Mohamed Hammami; Touhami Mahjoub

    2012-01-01

    We have performed this study to investigate the modulatory effect of thymoquinone (TQ), the Nigella sativa active compound, on erythrocyte lipid peroxidation and antioxidant status during 1,2-dimethylhydrazine- (DMH-) induced colon carcinogenesis after initiation in male Wistar rats. Rats exposed to DMH showed an increase of malondialdehyde and conjugated diene levels, and an augmentation of enzyme activities like catalase, glutathione peroxidase, and superoxide dismutase activities was also ...

  20. Characterization of Fatty Acid, Amino Acid and Volatile Compound Compositions and Bioactive Components of Seven Coffee (Coffea robusta) Cultivars Grown in Hainan Province, China

    OpenAIRE

    Wenjiang Dong; Lehe Tan; Jianping Zhao; Rongsuo Hu; Minquan Lu

    2015-01-01

    Compositions of fatty acid, amino acids, and volatile compound were investigated in green coffee beans of seven cultivars of Coffea robusta grown in Hainan Province, China. The chlorogenic acids, trigonelline, caffeine, total lipid, and total protein contents as well as color parameters were measured. Chemometric techniques, principal component analysis (PCA), hierarchical cluster analysis (HCA), and analysis of one-way variance (ANOVA) were performed on the complete data set to reveal chemic...

  1. Effects of energy drink major bioactive compounds on the performance of young adults in fitness and cognitive tests: a randomized controlled trial

    OpenAIRE

    Kammerer, Maximiliano; Jaramillo, Jaime A; García, Adriana; Juan C. Calderón; Valbuena, Luis H

    2014-01-01

    Background The consumption of beverages containing caffeine and taurine before exercising has been associated with increased physical and psychological performances and has been promoted to support the emotional state and provide vitality to consumers. However, there are contradictory results on these issues, it is not clear the effect of every major compound in relation to the whole effect of the beverages and there is a lack in knowledge about their degree of safety for consumption. Methods...

  2. Agronomic Management under Organic Farming May Affect the Bioactive Compounds of Lentil (Lens culinaris L. and Grass Pea (Lathyrus communis L.?

    Directory of Open Access Journals (Sweden)

    Valeria Menga

    2014-02-01

    Full Text Available A two year field experiment was carried out to evaluate the effects of three row and eight row seeding on the total phenolic compound (TPC, total flavonoid content (TFC, hydrolyzed (HTC and condensed tannin (CTC, antioxidant activity (ABTS assay, protein content and soluble dietary fiber (SDF and insoluble dietary fiber (IDF in the extracts of lentil (Lens culinaris L. and grass pea (Lathyrus communis L. cultivated under organic farming. The aim of this study was to determine whether row spacing used for seeding in organic farming systems for lentil and grass pea is a suitable method to increase the accumulation of antioxidant compounds in these crops. Grass pea showed the highest mean SDF and protein while lentil varieties showed the greatest and significant content of all of the antioxidant compounds. In lentil, there were increases in TPC (52%, HTC (73%, TFC (85% and CTC (41%, passing from three rows to eight rows, while in grass pea, the increases were lower, and only significant for TFC and CTC (37%, 13% respectively. In both lentils and grass pea, the highest correlation coefficient was between TPC and HTC, which indicates that the HTC includes the predominant phenolic compounds in lentil as well as in grass pea (r = 0.98, 0.71 p < 0.001, respectively. Regardless of legume species, TPC, HTC, TFC and CTC showed significant (p < 0.001 and linear correlations with the ABTS assay. These data confirm the key role of row spacing for the improvement of the antioxidant properties of lentil in organic farming; moreover, they hint at the major responsiveness and adaptation of lentil to environmental stimulus with respect to grass pea.

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

    Science.gov (United States)

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

    2017-01-15

    Organosulphur compounds (OSCs) present in garlic (Allium sativum L.) are responsible of several biological properties. Functional foods researches indicate the importance of quantifying these compounds in food matrices and biological fluids. For this purpose, this paper introduces a novel methodology based on dispersive liquid-liquid microextraction (DLLME) coupled to high performance liquid chromatography with ultraviolet detector (HPLC-UV) for the extraction and determination of organosulphur compounds in different matrices. The target analytes were allicin, (E)- and (Z)-ajoene, 2-vinyl-4H-1,2-dithiin (2-VD), diallyl sulphide (DAS) and diallyl disulphide (DADS). The microextraction technique was optimized using an experimental design, and the analytical performance was evaluated under optimum conditions. The desirability function presented an optimal value for 600μL of chloroform as extraction solvent using acetonitrile as dispersant. The method proved to be reliable, precise and accurate. It was successfully applied to determine OSCs in cooked garlic samples as well as blood plasma and digestive fluids. PMID:27542503

  4. Pine Bark and Green Tea Concentrated Extracts: Antioxidant Activity and Comprehensive Characterization of Bioactive Compounds by HPLC–ESI-QTOF-MS

    Directory of Open Access Journals (Sweden)

    María de la Luz Cádiz-Gurrea

    2014-11-01

    Full Text Available The consumption of polyphenols has frequently been associated with low incidence of degenerative diseases. Most of these natural antioxidants come from fruits, vegetables, spices, grains and herbs. For this reason, there has been increasing interest in identifying plant extract compounds. Polymeric tannins and monomeric flavonoids, such as catechin and epicatechin, in pine bark and green tea extracts could be responsible for the higher antioxidant activities of these extracts. The aim of the present study was to characterize the phenolic compounds in pine bark and green tea concentrated extracts using high-performance liquid chromatography coupled to electrospray ionization mass spectrometry (HPLC–ESI-QTOF-MS. A total of 37 and 35 compounds from pine bark and green tea extracts, respectively, were identified as belonging to various structural classes, mainly flavan-3-ol and its derivatives (including procyanidins. The antioxidant capacity of both extracts was evaluated by three complementary antioxidant activity methods: Trolox equivalent antioxidant capacity (TEAC, ferric reducing antioxidant power (FRAP and oxygen radical absorbance capacity (ORAC. Higher antioxidant activity values by each method were obtained. In addition, total polyphenol and flavan-3-ol contents, which were determined by Folin–Ciocalteu and vanillin assays, respectively, exhibited higher amounts of gallic acid and (+-catechin equivalents.

  5. Physico-chemical characterization and bioactive compounds of blackberry fruits (Rubus sp. grown in Brazil Caracterização físico-química e de compostos bioativos em amora-preta (Rubus sp. cultivada no Brasil

    Directory of Open Access Journals (Sweden)

    Neuza Mariko Aymoto Hassimotto

    2008-09-01

    Full Text Available Five blackberry cultivars (Rubus sp. were evaluated for antioxidant capacity, bioactive compounds and composition. Ascorbic acid levels, consisting of dehydro-ascorbic acid, ranged from 9.8 to 21.4 mg.100 g-1 fresh weight. Cyanidin (66 to 80% of total flavonoids, epicatechin, quercetin and traces of kaempferol were the main flavonoids found in all cultivars. The five cultivars presented high antioxidant capacity in the β-carotene/linoleic acid system, with inhibition similar to the synthetic antioxidant BHT, at a 50 µM concentration. Caingangue cultivar presented high vitamin C and total phenolics content, while Guarani had the highest cyanidin, total anthocyanin and total flavonoids levels and also the highest antioxidant capacity. These cultivars also presented good TSS/TA ratios. From the data, at a quantitative level, blackberry can be considered a good source of bioactive compounds, as well as potentially beneficial to human health.Cinco cultivares de amora-preta (Rubus sp. foram avaliadas quanto a sua capacidade antioxidante, perfil de compostos bioativos e composição físico-química. Os níveis de ácido ascórbico total, presentes na forma de ácido desidroascórbico, variaram entre 9,8 a 21,4 mg.100 g-1 (b.u.. Os principais flavonóides presentes nas cinco cultivares foram: a antocianina cianidina (66 a 80% do total de flavonóides; o flavan-3-ol epicatequina; e os flavonóis quercetina e traços de caenferol. As cinco cultivares apresentaram alta capacidade antioxidante quando avaliadas pelo sistema de co-oxidação β-caroteno/ácido linoléico, similar ao antioxidante sintético BHT, na concentração de 50 µM. A cultivar Guarani apresentou os maiores teores de flavonóides totais, antocianina total, cianidina e de capacidade antioxidante, enquanto que a cultivar Caigangue apresentou alto conteúdo de vitamina C e de fenólicos totais. Estas duas cultivares também apresentaram uma boa correlação TSS/TA. Assim, a amora

  6. 对复合图书馆编目工作重心的思考%Thought on Cataloging Work Core in the Compound Library

    Institute of Scientific and Technical Information of China (English)

    朱晓燕

    2012-01-01

    In the compound library era,the library cataloging work core will turn to deepen the connotation of the traditional cataloging work,broaden the extension of the digital resource cataloging,enhance the OPAC function and strengthen the construction of the authority file of the online bibliography database.Catalogers should foot on the practice,innovate the cataloging work,pay attention to the international cataloging development,and guide the daily cataloging work,in order to improve the professional competitiveness.%在复合图书馆时代,图书馆编目工作的重心将转向深化传统编目工作内涵、拓宽数字化资源编目的外延、增强OPAC功能、加强联机书目数据库的规范文档建设工作4个方面。编目员应立足实践,创新编目工作,关注国际编目新动态,指导日常编目工作,以提升职业竞争力。

  7. TRENDS ON ANALYTICAL METHODS FOR RESVERATROL, A MAJOR BIOACTIVE

    OpenAIRE

    Cabrita, Maria João; Martins, Nuno; Soares, Bruno; Costa Freitas, Ana Maria; Garcia, Raquel

    2014-01-01

    Resveratrol (3,5,4-trans-trihydroxystilbene) is a member of the stilbene group of phenolic compounds, comprising two aromatic rings linked by an ethylene bridge and is considered one of the most promising bioactive compounds due to its bioactivity. Wine is one of the main source of this bioactive compound in Mediterranean diet. Several authors have dedicated their research to the relationship between diet and health, and concerning wine and health studies, ‘‘French Paradox’’ was the starting ...

  8. Screen of FDA-approved drug library reveals compounds that protect hair cells from aminoglycosides and cisplatin

    OpenAIRE

    Vlasits, Anna L.; Simon, Julian A.; Raible, David W.; Rubel, Edwin W; Owens, Kelly N.

    2012-01-01

    Loss of mechanosensory hair cells in the inner ear accounts for many hearing loss and balance disorders. Several beneficial pharmaceutical drugs cause hair cell death as a side effect. These include aminoglycoside antibiotics, such as neomycin, kanamycin and gentamicin, and several cancer chemotherapy drugs, such as cisplatin. Discovering new compounds that protect mammalian hair cells from toxic insults is experimentally difficult because of the inaccessibility of the inner ear. We used the ...

  9. Application of parallel liquid chromatography/mass spectrometry for high throughput microsomal stability screening of compound libraries.

    Science.gov (United States)

    Xu, Rongda; Nemes, Csaba; Jenkins, Kelly M; Rourick, Robyn A; Kassel, Daniel B; Liu, Charles Z C

    2002-02-01

    Solution-phase and solid-phase parallel synthesis and high throughput screening have enabled biologically active and selective compounds to be identified at an unprecedented rate. The challenge has been to convert these hits into viable development candidates. To accelerate the conversion of these hits into lead development candidates, early assessment of the physicochemical and pharmacological properties of these compounds is being made. In particular, in vitro absorption, distribution, metabolism, and elimination (ADME) assays are being conducted at earlier and earlier stages of discovery with the goal of reducing the attrition rate of these potential drug candidates as they progress through development. In this report, we present an eight-channel parallel liquid chromatography/mass spectrometry (LC/MS) system in combination with custom Visual Basic and Applescript automated data processing applications for high throughput early ADME. The parallel LC/MS system was configured with one set of gradient LC pumps and an eight-channel multiple probe autosampler. The flow was split equivalently into eight streams before the multiple probe autosampler and recombined after the eight columns and just prior to the mass spectrometer ion source. The system was tested for column-to-column variation and for reproducibility over a 17 h period (approximately 500 injections per column). The variations in retention time and peak area were determined to be less than 2 and 10%, respectively, in both tests. The parallel LC/MS system described permits time-course microsomal incubations (t(o), t5, t15, t30) to be measured in triplicate and enables estimations of t 1/2 microsomal stability. The parallel LC/MS system is capable of analyzing up to 240 samples per hour and permits the complete profiling up to two microtiter plates of compounds per day (i.e., 176 test substrate compounds + sixteen controls). PMID:11841071

  10. Anti-inflammatory activity of cinnamon (C. zeylanicum and C. cassia) extracts - identification of E-cinnamaldehyde and o-methoxy cinnamaldehyde as the most potent bioactive compounds.

    Science.gov (United States)

    Gunawardena, Dhanushka; Karunaweera, Niloo; Lee, Samiuela; van Der Kooy, Frank; Harman, David G; Raju, Ritesh; Bennett, Louise; Gyengesi, Erika; Sucher, Nikolaus J; Münch, Gerald

    2015-03-01

    Chronic inflammation is a contributing factor in many age-related diseases. In a previous study, we have shown that Sri Lankan cinnamon (C. zeylanicum) was one of the most potent anti-inflammatory foods out of 115 foods tested. However, knowledge about the exact nature of the anti-inflammatory compounds and their distribution in the two major cinnamon species used for human consumption is limited. The aim of this investigation was to determine the anti-inflammatory activity of C. zeylanicum and C. cassia and elucidate their main phytochemical compounds. When extracts were tested in LPS and IFN-γ activated RAW 264.7 macrophages, most of the anti-inflammatory activity, measured by down-regulation of nitric oxide and TNF-α production, was observed in the organic extracts. The most abundant compounds in these extracts were E-cinnamaldehyde and o-methoxycinnamaldehyde. The highest concentration of E-cinnamaldehyde was found in the DCM extract of C. zeylanicum or C. cassia (31 and 34 mg g(-1) of cinnamon, respectively). When these and other constituents were tested for their anti-inflammatory activity in RAW 264.7 and J774A.1 macrophages, the most potent compounds were E-cinnamaldehyde and o-methoxycinnamaldehyde, which exhibited IC₅₀ values for NO with RAW 264.7 cells of 55 ± 9 μM (7.3 ± 1.2 μg mL(-1)) and 35 ± 9 μM (5.7 ± 1.5 μg mL(-1)), respectively; and IC₅₀ values for TNF-α of 63 ± 9 μM (8.3 ± 1.2 μg mL(-1)) and 78 ± 16 μM (12.6 ± 2.6 μg mL(-1)), respectively. If therapeutic concentrations can be achieved in target tissues, cinnamon and its components may be useful in the treatment of age-related inflammatory conditions. PMID:25629927

  11. Chemical composition and bioactive compounds of grape pomace (Vitis vinifera L., Benitaka variety, grown in the semiarid region of Northeast Brazil

    Directory of Open Access Journals (Sweden)

    Eldina Castro Sousa

    2014-03-01

    Full Text Available Grape pomace (Vitis vinifera L., Benitaka variety, grown in the semiarid region of Northeast Brazil was evaluated in relation to chemical composition, and content of minerals and functional properties. Its microbiological quality and toxic potential, using Artemia salina sp, were also investigated. The results showed that the flour obtained from these residues had below neutral pH (3.82, moisture (3.33g/100g, acidity of (0.64g of citric acid/100g, and ash (4.65 g/100g. The amount of total dietary fiber (46.17g/100g stood out quantitatively compared to the content of carbohydrate (29.2g/100 g, protein (8.49g/100g, and lipids (8.16g/100g. The total energy was 224Kcal/100g. With regard to the compounds with functional properties, higher values of insoluble fiber 79% (36.4 g/100 g; vitamin C (26.25 mg of acid ascorbic/100g, and anthocyanins (131mg/100g were found. The minerals iron, potassium, zinc, manganese, and calcium were present in higher concentrations. There were no significant copper values. The results showed that the grape residues are an important source of nutrients and compounds with functional properties suggesting that they can be incorporated as an ingredient in the diet and/or used as a dietary supplement aiming at health benefits. The residues did not show microbiological contamination and were considered nontoxic.

  12. Characterization of Fatty Acid, Amino Acid and Volatile Compound Compositions and Bioactive Components of Seven Coffee (Coffea robusta Cultivars Grown in Hainan Province, China

    Directory of Open Access Journals (Sweden)

    Wenjiang Dong

    2015-09-01

    Full Text Available Compositions of fatty acid, amino acids, and volatile compound were investigated in green coffee beans of seven cultivars of Coffea robusta grown in Hainan Province, China. The chlorogenic acids, trigonelline, caffeine, total lipid, and total protein contents as well as color parameters were measured. Chemometric techniques, principal component analysis (PCA, hierarchical cluster analysis (HCA, and analysis of one-way variance (ANOVA were performed on the complete data set to reveal chemical differences among all cultivars and identify markers characteristic of a particular botanical origin of the coffee. The major fatty acids of coffee were linoleic acid, palmitic acid, oleic acid, and arachic acid. Leucine (0.84 g/100 g DW, lysine (0.63 g/100 g DW, and arginine (0.61 g/100 g DW were the predominant essential amino acids (EAAs in the coffee samples. Seventy-nine volatile compounds were identified and semi-quantified by HS-SPME/GC-MS. PCA of the complete data matrix demonstrated that there were significant differences among all cultivars, HCA supported the results of PCA and achieved a satisfactory classification performance.

  13. Food Byproducts as a New and Cheap Source of Bioactive Compounds: Lignans with Antioxidant and Anti-inflammatory Properties from Crataegus pinnatifida Seeds.

    Science.gov (United States)

    Huang, Xiao-Xiao; Bai, Ming; Zhou, Le; Lou, Li-Li; Liu, Qing-Bo; Zhang, Yan; Li, Ling-Zhi; Song, Shao-Jiang

    2015-08-19

    During the process of manufacturing hawthorn (Crataegus pinnatifida) juice and jam, a significant quantity of byproducts (leaves, seeds) is generated. The antioxidant and anti-inflammatory bioassay-guided fractionation of the extract of hawthorn seeds has led to the isolation of eight new lignans, hawthornnins A-H (1-8), and seven known analogues (9-15). Their structures were elucidated by spectroscopic techniques, including 1D and 2D NMR and CD spectra. The radical-scavenging effects of all isolated compounds were investigated. 1-6 and 8 showed moderate activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH), whereas 1-6 and 14 displayed good 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical-scavenging activities that were even more potent than that of trolox. In addition, all isolates were evaluated for their anti-inflammatory activities by detecting the nitric oxide (NO) and tumor necrosis factor α (TNF-α) production by the LPS-induced murine macrophage cell line RAW264.7, and compounds 1-7, 13, and 14 exhibited potent inhibition of NO and TNF-α production. The structure-activity relationships of isolated lignans were also examined, and the results obtained show that C. pinnatifida seeds can be regarded as a potential new and cheap source of antioxidants and inflammation inhibitors. PMID:26237121

  14. Characterization of Fatty Acid, Amino Acid and Volatile Compound Compositions and Bioactive Components of Seven Coffee (Coffea robusta) Cultivars Grown in Hainan Province, China.

    Science.gov (United States)

    Dong, Wenjiang; Tan, Lehe; Zhao, Jianping; Hu, Rongsuo; Lu, Minquan

    2015-01-01

    Compositions of fatty acid, amino acids, and volatile compound were investigated in green coffee beans of seven cultivars of Coffea robusta grown in Hainan Province, China. The chlorogenic acids, trigonelline, caffeine, total lipid, and total protein contents as well as color parameters were measured. Chemometric techniques, principal component analysis (PCA), hierarchical cluster analysis (HCA), and analysis of one-way variance (ANOVA) were performed on the complete data set to reveal chemical differences among all cultivars and identify markers characteristic of a particular botanical origin of the coffee. The major fatty acids of coffee were linoleic acid, palmitic acid, oleic acid, and arachic acid. Leucine (0.84 g/100 g DW), lysine (0.63 g/100 g DW), and arginine (0.61 g/100 g DW) were the predominant essential amino acids (EAAs) in the coffee samples. Seventy-nine volatile compounds were identified and semi-quantified by HS-SPME/GC-MS. PCA of the complete data matrix demonstrated that there were significant differences among all cultivars, HCA supported the results of PCA and achieved a satisfactory classification performance. PMID:26389867

  15. Quantum efficiency and bandgap analysis for combinatorial photovoltaics: sorting activity of Cu-O compounds in all-oxide device libraries.

    Science.gov (United States)

    Anderson, Assaf Y; Bouhadana, Yaniv; Barad, Hannah-Noa; Kupfer, Benjamin; Rosh-Hodesh, Eli; Aviv, Hagit; Tischler, Yaakov R; Rühle, Sven; Zaban, Arie

    2014-02-10

    All-oxide-based photovoltaics (PVs) encompass the potential for extremely low cost solar cells, provided they can obtain an order of magnitude improvement in their power conversion efficiencies. To achieve this goal, we perform a combinatorial materials study of metal oxide based light absorbers, charge transporters, junctions between them, and PV devices. Here we report the development of a combinatorial internal quantum efficiency (IQE) method. IQE measures the efficiency associated with the charge separation and collection processes, and thus is a proxy for PV activity of materials once placed into devices, discarding optical properties that cause uncontrolled light harvesting. The IQE is supported by high-throughput techniques for bandgap fitting, composition analysis, and thickness mapping, which are also crucial parameters for the combinatorial investigation cycle of photovoltaics. As a model system we use a library of 169 solar cells with a varying thickness of sprayed titanium dioxide (TiO2) as the window layer, and covarying thickness and composition of binary compounds of copper oxides (Cu-O) as the light absorber, fabricated by Pulsed Laser Deposition (PLD). The analysis on the combinatorial devices shows the correlation between compositions and bandgap, and their effect on PV activity within several device configurations. The analysis suggests that the presence of Cu4O3 plays a significant role in the PV activity of binary Cu-O compounds. PMID:24410367

  16. High-Throughput Sorting and Placement of One-Bead-One-Compound (OBOC) Libraries from Bulk to Single Wells in Organic Solvent

    Science.gov (United States)

    Bordo, Mark W.; Oketokoun, Rafiou; Cross, Conor J.; Bao, Kai; Lee, Jeong Heon; Feygin, Ilya; Chang, Alex B.; Frangioni, John V.; Choi, Hak Soo

    2015-01-01

    One-bead-one-compound (OBOC) solid-phase combinatorial chemistry has been used extensively in drug discovery. However, a major bottleneck has been the sorting of individual beads, while still swollen in organic solvent, into individual wells of a microwell plate. To solve this problem we have constructed an automated bead sorting system with integrated quality control that is capable of sorting and placing large numbers of beads in bulk to single wells of a 384-well plate, all in organic solvent. The bead sorter employs a unique, reciprocating fluidic design capable of depositing 1 bead per 1.5 s with an average accuracy of 97%. We quantified the performance of this instrument by sorting over 8,500 beads followed by cleaving the conjugated compound and confirming the chemical identity of each by LC/MS. This instrument should enable more efficient screening of combinatorial small molecule libraries without the need to dry beads or otherwise change chemical environment. PMID:25879633

  17. Effect of drying methods with the application of vacuum microwaves on the bioactive compounds, color, and antioxidant activity of strawberry fruits.

    Science.gov (United States)

    Wojdyło, Aneta; Figiel, Adam; Oszmiański, Jan

    2009-02-25

    The objective of this study was to evaluate the application of vacuum-microwave drying (240, 360, and 480 W) in the production process of dehydrated strawberry and to compare and contrast the quality of these dehydrated strawberries in terms of their polyphenol compounds, concentration of some heat liable components, and color to that of freeze-dried, convective, and vacuum-dried strawberry. Thus, the effect of vacuum-microwave drying and other drying methods on the antioxidant activity of berries was evaluated. Whole fresh and dried fruits were assessed for phenolics (anthocyanins, flavanols, hydroxycinnamic acids, and flavonols), ascorbic acid, and antioxidant activity (all parameters were calculated on a dry matter basis). Analysis of data shows that ellagic acid and flavanol changes were affected by drying techniques and cultivar. Drying destroyed anthocyanins, flavanols, and ascorbic acid, and there was a significant decrease in antioxidant activity. The most striking result was that conventional and vacuum drying decreased antioxidant activity in both cultivars, whereas contradictory results were found for vacuum-microwave processed strawberry. This study has demonstrated that vacuum-microwave drying, especially at 240 W, can produce high-quality products, with the additional advantage of reduced processing times, compared to other processes such as freeze-drying. PMID:19170638

  18. Bioactive furanonaphthoquinones from Crescentia cujete.

    Science.gov (United States)

    Hetzel, C E; Gunatilaka, A A; Glass, T E; Kingston, D G; Hoffmann, G; Johnson, R K

    1993-09-01

    Bioassay-directed fractionation of the MeCOEt extract of Crescentia cujete (Bignonaceae) resulted in the isolation of (2S,3S)-3-hydroxy-5,6-dimethoxydehydroiso-alpha-lapachone [1], (2R)-5,6-dimethoxydehydroiso-alpha-lapachone [2], (2R)-5-methoxydehydroiso-alpha-lapachone [3], 2-(1-hydroxyethyl)naphtho[2,3-b]furan-4,9-dione [4], 5-hydroxy-2-(1-hydroxyethyl)naphtho[2,3-b]furan-4,9-dione [5], 2-isopropenylnaphtho[2,3-b]furan-4,9-dione [6], and 5-hydroxydehydroiso-alpha-lapachone [7]. Compounds 1-3 are new, and all compounds are bioactive, showing selective activity towards DNA-repair-deficient yeast mutants. The isolation, structure elucidation, and biological activities of these compounds are reported. PMID:8254347

  19. Integration of high-content screening and untargeted metabolomics for comprehensive functional annotation of natural product libraries

    Science.gov (United States)

    Kurita, Kenji L.; Glassey, Emerson; Linington, Roger G.

    2015-01-01

    Traditional natural products discovery using a combination of live/dead screening followed by iterative bioassay-guided fractionation affords no information about compound structure or mode of action until late in the discovery process. This leads to high rates of rediscovery and low probabilities of finding compounds with unique biological and/or chemical properties. By integrating image-based phenotypic screening in HeLa cells with high-resolution untargeted metabolomics analysis, we have developed a new platform, termed Compound Activity Mapping, that is capable of directly predicting the identities and modes of action of bioactive constituents for any complex natural product extract library. This new tool can be used to rapidly identify novel bioactive constituents and provide predictions of compound modes of action directly from primary screening data. This approach inverts the natural products discovery process from the existing ‟grind and find” model to a targeted, hypothesis-driven discovery model where the chemical features and biological function of bioactive metabolites are known early in the screening workflow, and lead compounds can be rationally selected based on biological and/or chemical novelty. We demonstrate the utility of the Compound Activity Mapping platform by combining 10,977 mass spectral features and 58,032 biological measurements from a library of 234 natural products extracts and integrating these two datasets to identify 13 clusters of fractions containing 11 known compound families and four new compounds. Using Compound Activity Mapping we discovered the quinocinnolinomycins, a new family of natural products with a unique carbon skeleton that cause endoplasmic reticulum stress. PMID:26371303

  20. Glutathione conjugation as a bioactivation reaction

    NARCIS (Netherlands)

    Bladeren, P.J. van

    2000-01-01

    In general, glutathione conjugation is regarded as a detoxication reaction. However, depending on the properties of the substrate, bioactivation is also possible. Four types of activation reaction have been recognized: direct-acting compounds, conjugates that are activated through cysteine conjugate

  1. Bioactive Terpenes from Marine-Derived Fungi

    Directory of Open Access Journals (Sweden)

    Ahmed M. Elissawy

    2015-04-01

    Full Text Available Marine-derived fungi continue to be a prolific source of secondary metabolites showing diverse bioactivities. Terpenoids from marine-derived fungi exhibit wide structural diversity including numerous compounds with pronounced biological activities. In this review, we survey the last five years’ reports on terpenoidal metabolites from marine-derived fungi with particular attention on those showing marked biological activities.

  2. Bioactive Terpenes from Marine-Derived Fungi

    OpenAIRE

    Ahmed M. Elissawy; Mohamed El-Shazly; Ebada, Sherif S.; AbdelNasser B. Singab; Peter Proksch

    2015-01-01

    Marine-derived fungi continue to be a prolific source of secondary metabolites showing diverse bioactivities. Terpenoids from marine-derived fungi exhibit wide structural diversity including numerous compounds with pronounced biological activities. In this review, we survey the last five years’ reports on terpenoidal metabolites from marine-derived fungi with particular attention on those showing marked biological activities.

  3. Fluorescence studies by quenching and protein unfolding on the interaction of bioactive compounds in water extracts of kiwi fruit cultivars with human serum albumin

    International Nuclear Information System (INIS)

    The main aim of this investigation was to characterize new kiwi fruit cultivars after cold storage treatment and to determine the similarities and differences between them, using spectroscopic methods. The chemometric comparison of kiwi fruit cultivars based on physicochemical indices during cold storage was carried out. All kiwi fruit cultivars showed a high level of correlation between the contents of phenolic compounds (polyphenols, tannins and flavonoids) and their antioxidant capacities. The interactions of soluble polyphenols of different kiwi fruit cultivars with human serum albumin (HSA) were investigated by fluorescence. The obtained statistical and fluorescence results allow to classify the investigated kiwi fruit cultivars according to their properties. The antioxidant properties of different cultivars monitored by β-carotene assay showed that the highest percentage of antioxidant activity (%AA) at the end of the cold storage was detected for ‘SKK-12’ (27.61±2.44) %AA with the lowest shelf life (8 weeks) and the lowest was found for ‘Hayward’ variety (8.33±0.74) %AA with the highest shelf life (24 weeks). The averaged amount of polyphenols in ‘Bidan’ and ‘SKK-12’ 13.97±1.95 mg GAE/g was much higher than in other cultivars 3.93±3.26 mg GAE/g, without respect on time of cold storage. The HSA-binding capacities of these cultivars were the highest and correlated with their antioxidant capacities. To our knowledge this is the first report showing differences and similarities in new kiwi fruit cultivars, using spectroscopic techniques. The fact that fluorescence spectral methods are applied as a powerful tool to show the photophysical properties of intrinsic fluorophores in protein molecules in the presence of fruit extracts is important in this study. In conclusion, the obtained knowledge would contribute to the pharmaceutical development and clinical application of kiwi fruit extracts. - Highlights: • Different kiwi fruit cultivars

  4. Fluorescence studies by quenching and protein unfolding on the interaction of bioactive compounds in water extracts of kiwi fruit cultivars with human serum albumin

    Energy Technology Data Exchange (ETDEWEB)

    Seo Park, Yong, E-mail: ypark@mokpo.ac.kr [Department of Horticultural Science, Mokpo National University, Muan, Jeonnam (Korea, Republic of); Polovka, Martin [National Agricultural and Food Centre VUP, Food Research Institute, SK-824 75 Bratislava (Slovakia); Leticia Martinez-Ayala, Alma [Centro de Desarrollo de Productos Bioticos, Instituto Politécnico Nacional, Carretera Yautepec-Jojutla, Km. 6, calle CEPROBI No. 8, Col. San Isidro, Yautepec, Morelos 62731 (Mexico); González-Aguilar, Gustavo A. [Research Center for Food & Development, A.C. (CIAD), Carretera a Ejido La Victoria, Km 0.6, Hermosillo, Sonora 83304 (Mexico); Ham, Kyung-Sik; Kang, Seong-Gook; Park, Yang-Kyun [Department of Food Engineering, Mokpo National University, Muan, Jeonnam (Korea, Republic of); Heo, Buk-Gu [Naju Foundation of Natural Dyeing Culture, Naju 520-931 (Korea, Republic of); Namiesnik, Jacek [Department of Analytical Chemistry, Chemical Faculty, Gdańsk University of Technology, 80 952 Gdańsk (Poland); Gorinstein, Shela, E-mail: shela.gorin@mail.huji.ac.il [The Institute for Drug Research, School of Pharmacy, The Hebrew University, Hadassah Medical School, Jerusalem 91120 (Israel)

    2015-04-15

    The main aim of this investigation was to characterize new kiwi fruit cultivars after cold storage treatment and to determine the similarities and differences between them, using spectroscopic methods. The chemometric comparison of kiwi fruit cultivars based on physicochemical indices during cold storage was carried out. All kiwi fruit cultivars showed a high level of correlation between the contents of phenolic compounds (polyphenols, tannins and flavonoids) and their antioxidant capacities. The interactions of soluble polyphenols of different kiwi fruit cultivars with human serum albumin (HSA) were investigated by fluorescence. The obtained statistical and fluorescence results allow to classify the investigated kiwi fruit cultivars according to their properties. The antioxidant properties of different cultivars monitored by β-carotene assay showed that the highest percentage of antioxidant activity (%AA) at the end of the cold storage was detected for ‘SKK-12’ (27.61±2.44) %AA with the lowest shelf life (8 weeks) and the lowest was found for ‘Hayward’ variety (8.33±0.74) %AA with the highest shelf life (24 weeks). The averaged amount of polyphenols in ‘Bidan’ and ‘SKK-12’ 13.97±1.95 mg GAE/g was much higher than in other cultivars 3.93±3.26 mg GAE/g, without respect on time of cold storage. The HSA-binding capacities of these cultivars were the highest and correlated with their antioxidant capacities. To our knowledge this is the first report showing differences and similarities in new kiwi fruit cultivars, using spectroscopic techniques. The fact that fluorescence spectral methods are applied as a powerful tool to show the photophysical properties of intrinsic fluorophores in protein molecules in the presence of fruit extracts is important in this study. In conclusion, the obtained knowledge would contribute to the pharmaceutical development and clinical application of kiwi fruit extracts. - Highlights: • Different kiwi fruit cultivars

  5. Bioactive proteins from pipefishes

    Institute of Scientific and Technical Information of China (English)

    E. Rethna Priya; S. Ravichandran; R. Ezhilmathi

    2013-01-01

    Objective: To screen antimicrobial potence of some pipefish species collected from Tuticorin coastal environment.Methods:Antimicrobial activity of pipefishes in methanol extract was investigated against 10 bacterial and 10 fungal human pathogenic strains.Results:Among the tested strains, in Centriscus scutatus, pipefish showed maximum zone of inhibition against Vibrio cholerae (8 mm) and minimum in the sample of Hippichthys cyanospilos against Klebseilla pneumoniae (2 mm). In positive control, maximum zone of inhibition was recorded in Vibrio cholerae (9 mm) and minimum in Klebseilla pneumoniae, and Salmonella paratyphi (5 mm). Chemical investigation indicated the presence of peptides as evidenced by ninhydrin positive spots on thin layer chromatography and presence of peptide. In SDS PAGE, in Centriscus scutatus, four bands were detected in the gel that represented the presence of proteins in the range nearly 25.8-75 kDa. In Hippichthys cyanospilos, five bands were detected in the gel that represented the presence of proteins in the range nearly 20.5-78 kDa. The result of FT-IR spectrum revealed that the pipe fishes extracts compriseed to have peptide derivatives as their predominant chemical groups.Conclusions:It can be conclude that this present investigation suggests the tested pipe fishes will be a potential source of natural bioactive compounds.

  6. Compostos bioativos e atividade antioxidante do café (Coffea arabica L. Coffee (Coffea arabica L. bioactive compounds and antioxidant activity

    Directory of Open Access Journals (Sweden)

    Sheila Andrade Abrahão

    2010-04-01

    Full Text Available Conduziu-se este trabalho, com a proposta de avaliar o potencial antioxidante de dois padrões da bebida do café (rio e mole, verdes e torrados, utilizando modelos in vitro. Foram determinados o teor de fenólicos totais, ácido clorogênico (ácido 5-cafeoilquínico e cafeína das bebidas. A avaliação in vitro do potencial antioxidante foi investigada pelos métodos de captação do radical DPPH e pelo poder redutor de metais. Os dois padrões de bebida do café analisados não apresentaram diferenças quanto aos parâmetros cor, ácido clorogênico e cafeína. Observou-se que houve redução nos valores de ácido clorogênico à medida que os grãos foram torrados. O café verde bebida rio apresentou maior teor de fenólicos totais que o café bebida mole. Nos grãos torrados não foi observada diferença. A bebida do café independente da qualidade sensorial apresentou alto poder redutor e importante atividade sequestrante de radicais livres. A atividade sequestrante de radicais livres foi significativamente superior nas amostras obtidas a partir dos grãos torrados, quando comparados aos extratos dos grãos verdes. A torração, porém, reduziu o poder redutor das bebidas do café. Os dados obtidos permitem sugerir que, independente da classificação sensorial da bebida, o café apresenta expressiva capacidade sequestrante de radicais livres e poder redutor de metais.The present work intended to evaluate the antioxidant potential of two coffee sorts (soft and river, green and roasted, in vitro. Phenolic compounds content, chlorogenic acid (5-cafeoyolquinic and caffeine of the beverages were evaluated. In vitro evaluation of the antioxidant potential was investigated by DPPH radical scavenging assay and by reducing the power of metals. Both sorts of coffee did not present statistical differences for color, chlorogenic acid and caffeine. After roasting, 5-cafeoyolquinic acid levels decreased. River coffee beverage presented greater content

  7. Magnitude Differences in Bioactive Compounds, Chemical Functional Groups, Fatty Acid Profiles, Nutrient Degradation and Digestion, Molecular Structure, and Metabolic Characteristics of Protein in Newly Developed Yellow-Seeded and Black-Seeded Canola Lines.

    Science.gov (United States)

    Theodoridou, Katerina; Zhang, Xuewei; Vail, Sally; Yu, Peiqiang

    2015-06-10

    Recently, new lines of yellow-seeded (CS-Y) and black-seeded canola (CS-B) have been developed with chemical and structural alteration through modern breeding technology. However, no systematic study was found on the bioactive compounds, chemical functional groups, fatty acid profiles, inherent structure, nutrient degradation and absorption, or metabolic characteristics between the newly developed yellow- and black-seeded canola lines. This study aimed to systematically characterize chemical, structural, and nutritional features in these canola lines. The parameters accessed include bioactive compounds and antinutrition factors, chemical functional groups, detailed chemical and nutrient profiles, energy value, nutrient fractions, protein structure, degradation kinetics, intestinal digestion, true intestinal protein supply, and feed milk value. The results showed that the CS-Y line was lower (P ≤ 0.05) in neutral detergent fiber (122 vs 154 g/kg DM), acid detergent fiber (61 vs 99 g/kg DM), lignin (58 vs 77 g/kg DM), nonprotein nitrogen (56 vs 68 g/kg DM), and acid detergent insoluble protein (11 vs 35 g/kg DM) than the CS-B line. There was no difference in fatty acid profiles except C20:1 eicosenoic acid content (omega-9) which was in lower in the CS-Y line (P condensed tannins with averages of 0.3 and 3.1 g/kg DM, respectively. When protein was portioned into five subfractions, significant differences were found in PA, PB1 (65 vs 79 g/kg CP), PB2, and PC fractions (10 vs 33 g/kg CP), indicating protein degradation and supply to small intestine differed between two new lines. In terms of protein structure spectral profile, there were no significant differences in functional groups of amides I and II, α helix, and β-sheet structure as well as their ratio between the two new lines, indicating no difference in protein structure makeup and conformation between the two lines. In terms of energy values, there were significant differences in total digestible nutrient

  8. 豆类种子及萌发过程中功效性成分研究概述%Research Advancement of Bioactive Compounds in Legumes Seeds and Their Germinated Products

    Institute of Scientific and Technical Information of China (English)

    陈振; 康玉凡

    2012-01-01

    豆类种子及其萌发后形成的芽苗菜富含多种生物活性成分,本文综述近几年有关大豆、绿豆、红小豆、蚕豆、豌豆等多种豆类种子及其萌发过程中酚类、大豆异黄酮、γ-氨基丁酸和左旋多巴等功能性成分的研究,分别从结构与种类、植物体内合成途径、保健功能和代谢过程中的变化规律等方面对这些功能成分进行了综述,为豆类芽苗菜功能保健产品开发提供理论借鉴与技术参考。%Legumes seeds and their germinated products are rich in various bioactive compounds. This article summaried the research on functional components of phenolics, isoflavones, γ-aminobutyric acid and levodopa in legumes seeds including soybeans, mung beans, red beans, broad beans, peas, etc and their germinated products in recent years. Furthermore, structure and species, biosynthesis pathway, health functions and variation in the metabolic processes of the functional components of legumes and their germinated products were reviewed respectively, which provided agronomic traits and transgenic technology for the development of health products of bean sprouts.

  9. 青霉菌固体发酵对三七药材活性成分的影响%Chemical changes of bioactive compounds in panax notoginseng fermented by penicillium sp.

    Institute of Scientific and Technical Information of China (English)

    许文迪; 闫炳雄; 邱智东; 王伟楠

    2015-01-01

    目的:对三七药材经青霉菌发酵之后的主要活性成分变化进行研究。方法利用青霉菌对三七药材进行固体发酵,根据 HPLC-Q-TOF-MS 的检测结果,对三七发酵产物的主要活性成分进行分析和指认,同时考察黄曲霉素和赭曲霉素等微生物毒素的含量。结果三七药材经青霉菌发酵之后稀有皂苷含量显著提高,未见黄曲霉素和赭曲霉素产生。结论青霉菌可以对三七药材中皂苷类成分进行转化,提高稀有皂苷含量,改变药性,且未见明显的微生物毒素产生,具有一定的使用安全性。%objective The chemical changes of bioactive compounds in Panax notoginseng fermented by Penicillium sp. were studied in this paper. Method The major components together with aflatoxins and ochratoxins of the fer-mented panax notoginseng were analyzed and determined by HPLC-Q-TOF-MS. Result The content of rare ginsen-osides in the fermented panax notoginseng significantly increased while neither aflatoxins nor ochratoxins was detected. Conclusion The accumulation of rare ginsenosides and enhancement in efficacy of panax notoginseng could be a-chieved by fermenting with Penicillium sp. without any obvious biotoxins. Hence this fermentation product was either beneficial or harmless.

  10. Cypriot libraries

    OpenAIRE

    John F. Harvey

    1982-01-01

    Describes the current state of librarianship and bibliography in Cyprus, with separate sections for the Greek and Turkish sectors. Although there is no national library in the Greek sector there are 5 types of public library: Nicosia public library; Limassol, Larnaca and Paphos public libraries; community libraries; mobile libraries; and foreign cultural centre libraries. Schools and colleges in the Greek centre are well provided with libraries and most government departments sponsor special ...

  11. Combined Use of Oligopeptides, Fragment Libraries, and Natural Compounds: A Comprehensive Approach To Sample the Druggability of Vascular Endothelial Growth Factor.

    Science.gov (United States)

    Bayó-Puxan, Núria; Rodríguez-Mias, Ricard; Goldflam, Michael; Kotev, Martin; Ciudad, Sonia; Hipolito, Christopher J; Varese, Monica; Suga, Hiroaki; Campos-Olivas, Ramón; Barril, Xavier; Guallar, Víctor; Teixidó, Meritxell; García, Jesús; Giralt, Ernest

    2016-04-19

    The modulation of protein-protein interactions (PPIs) is emerging as a highly promising tool to fight diseases. However, whereas an increasing number of compounds are able to disrupt peptide-mediated PPIs efficiently, the inhibition of domain-domain PPIs appears to be much more challenging. Herein, we report our results related to the interaction between vascular endothelial growth factor (VEGF) and its receptor (VEGFR). The VEGF-VEGFR interaction is a typical domain-domain PPI that is highly relevant for the treatment of cancer and some retinopathies. Our final goal was to identify ligands able to bind VEGF at the region used by the growth factor to interact with its receptor. We undertook an extensive study, combining a variety of experimental approaches, including NMR-spectroscopy-based screening of small organic fragments, peptide libraries, and medicinal plant extracts. The key feature of the successful ligands that emerged from this study was their capacity to expose hydrophobic functional groups able to interact with the hydrophobic hot spots at the interacting VEGF surface patch. PMID:26553526

  12. Agricultural by-products with bioactive effects: A multivariate approach to evaluate microbial and physicochemical changes in a fresh pork sausage enriched with phenolic compounds from olive vegetation water.

    Science.gov (United States)

    Fasolato, Luca; Carraro, Lisa; Facco, Pierantonio; Cardazzo, Barbara; Balzan, Stefania; Taticchi, Agnese; Andreani, Nadia Andrea; Montemurro, Filomena; Martino, Maria Elena; Di Lecce, Giuseppe; Toschi, Tullia Gallina; Novelli, Enrico

    2016-07-01

    The use of phenolic compounds derived from agricultural by-products could be considered as an eco-friendly strategy for food preservation. In this study a purified phenol extract from olive vegetation water (PEOVW) was explored as a potential bioactive ingredient for meat products using Italian fresh sausage as food model. The research was developed in two steps: first, an in vitro delineation of the extract antimicrobial activities was performed, then, the PEOVW was tested in the food model to investigate the possible application in food manufacturing. The in vitro tests showed that PEOVW clearly inhibits the growth of food-borne pathogens such as Listeria monocytogenes and Staphylococcus aureus. The major part of Gram-positive strains was inhibited at the low concentrations (0.375-3mg/mL). In the production of raw sausages, two concentrates of PEOVW (L1: 0.075% and L2: 0.15%) were used taking into account both organoleptic traits and the bactericidal effects. A multivariate statistical approach allowed the definition of the microbial and physicochemical changes of sausages during the shelf life (14days). In general, the inclusion of the L2 concentration reduced the growth of several microbial targets, especially Staphylococcus spp. and LABs (2log10CFU/g reduction), while the increasing the growth of yeasts was observed. The reduction of microbial growth could be involved in the reduced lipolysis of raw sausages supplemented with PEOVW as highlighted by the lower amount of diacylglycerols. Moisture and aw had a significant effect on the variability of microbiological features, while food matrix (the sausages' environment) can mask the effects of PEOVW on other targets (e.g. Pseudomonas). Moreover, the molecular identification of the main representative taxa collected during the experimentation allowed the evaluation of the effects of phenols on the selection of bacteria. Genetic data suggested a possible strain selection based on storage time and the addition of

  13. A comprehensive LC/MS analysis of novel cyclopentenedione library.

    Science.gov (United States)

    Papouskova, Barbora; Bernard, Martin; Ottenschlager, Jakub; Karban, Jindrich; Velisek, Petr; Hrbac, Jan; Sykora, Jan; Storch, Jan; Vacek, Jan

    2016-09-01

    Cyclopentenediones (CPDs) are compounds with a variety of applications ranging from the preparation of functional polymers to the development of antimicrobial agents, suggesting the potential use of CPDs as novel bioactive compounds or drugs. For this reason, a detailed characterization of CPDs and the development of robust analytical methods for their trace analysis are being sought. Here we focused on the design and synthesis of a library of novelized benzylidene CPD derivatives that were consequently characterized by ultra-high performance liquid chromatography (UHPLC) on-line connected with tandem mass spectrometry (MS/MS). The library design was based on a 2-benzylidene-4-cyclopentene-1,3-dione skeleton substituted with a variety of hydroxy, methoxy, halogen, linear aliphatic, heterocyclic and saccharide moieties, primarily modulating the skeleton's hydrophobicity. The prepared CPDs were effectively ionized by positive/negative atmospheric pressure photoionization (APPI) and atmospheric pressure chemical ionization (APCI). After careful optimization of the dopant composition and flow rate, positive-mode APPI proved to be more sensitive than APCI. In negative mode, both ionization techniques gave similar results. Further, a detailed MS fragmentation study was performed, confirming the structure of the compounds and enabling positional isomers of CPDs to be differentiated on the basis of their collision spectra analysis. Finally, an optimization of the composition of the mobile phase and reversed-phased separation mode were done, followed by a selection of the most suitable UHPLC stationary phases, i.e. C18, C8 and phenyl. The applicability of the method was evaluated by the inclusion of the other two substances in the study, i.e. monomeric and dimeric bioactive CPDs, compound TX-1123 and nostotrebin 6 with cytostatic and antimicrobial activities, respectively. The results presented here could be used in further investigations of the chromatographic retention

  14. Electrochemistry of organic, bioactive compounds and biopolymers

    Czech Academy of Sciences Publication Activity Database

    Fojta, Miroslav; Navrátil, Tomáš

    2015-01-01

    Roč. 146, č. 5 (2015), s. 721-721. ISSN 0026-9247 Institutional support: RVO:68081707 ; RVO:61388955 Keywords : electrochemistry * biopolymers Subject RIV: CG - Electrochemistry Impact factor: 1.222, year: 2014

  15. Bioactive compounds of the genus nostoc (cyanobacteria)

    Czech Academy of Sciences Publication Activity Database

    Kopecký, Jiří

    Lublin, 2004, s. 58. [International Symposium on Chromatography of Natural Products /4./. Lublin (PL), 14.06.2004-17.06.2004] Institutional research plan: CEZ:AV0Z5020903 Keywords : cp * nostoc taxa Subject RIV: EI - Biotechnology ; Bionics

  16. Bioactive compounds: Definition and assessment of activity

    NARCIS (Netherlands)

    Biesalski, H.K.; Dragsted, L.O.; Elmadfa, I.; Grossklaus, R.; Müller, M.R.; Schrenk, D.; Walter, P.; Weber, P.

    2009-01-01

    Biomarkers and their role in evaluating efficacy and safety were the topic of the 23rd Hohenheim Consensus Meeting at the University of Hohenheim in Stuttgart. Scientists who had published and reviewed scientific and regulatory papers on the topic were invited, among them basic researchers, toxicolo

  17. Bioactive compounds and antioxidant activity in fruits of clone and ungrafted genotypes of yellow mombin tree Compostos bioativos e capacidade antioxidante de frutos de genótipos clones e pés-franco de cajazeira

    Directory of Open Access Journals (Sweden)

    Fernanda Vanessa Gomes da Silva

    2012-12-01

    Full Text Available Yellow mombin is a fruit tree that grows spontaneously in the Semi-Arid Northeastern Brazil. Its fruits are still extractively exploited. The pulp of yellow mombin fruit stands out regarding the commercial aspect due to the characteristic flavor and aroma felt when consumed in diverse ways. This study aimed to evaluate the presence of bioactive compounds, total extractable polyphenols, and antioxidant activity of yellow mombin fruits (Spondias mombin, L., from clone and ungrafted genotypes. The fruits were harvested at commercial maturity from twelve yellow mombin tree genotypes from an experimental orchard located at the municipality of Joao Pessoa, Paraíba, Brazil, and evaluated for chlorophyll, carotenoids, yellow flavonoids, total extractable polyphenols, and antioxidant activity, which was measured by the β-carotene/linoleic acid method. The antioxidant activity showed a percentage of inhibition of oxidation higher than 75% for all genotypes evaluated at the time of 120 minutes. The fruits from clone genotypes showed a higher percentage of antioxidant activity.A cajazeira é uma árvore frutífera de ocorrência espontânea no Semiárido Nordestino e seus frutos são ainda explorados de forma extrativista. A polpa do fruto da cajazeira assume posição de destaque no que tange ao aspecto comercial, em função do aroma e do sabor característicos que oferece quando degustada nas mais variadas formas. Este trabalho teve como objetivo avaliar a presença de compostos bioativos e polifenóis extraíveis, e a atividade antioxidante de frutos da cajazeira (Spondias mombin, L, provenientes de genótipos clones e pés-franco. Os frutos foram colhidos na maturidade comercial de doze genótipos de cajazeiras provenientes de pomar experimental localizado no Município de João Pessoa-PB, Brazil, e avaliados quanto ao teor de clorofila, carotenoides, flavonoides amarelos e polifenóis extraíveis totais, sendo a atividade antioxidante avaliada pelo

  18. Real-Time Biological Annotation of Synthetic Compounds.

    Science.gov (United States)

    Gerry, Christopher J; Hua, Bruce K; Wawer, Mathias J; Knowles, Jonathan P; Nelson, Shawn D; Verho, Oscar; Dandapani, Sivaraman; Wagner, Bridget K; Clemons, Paul A; Booker-Milburn, Kevin I; Boskovic, Zarko V; Schreiber, Stuart L

    2016-07-20

    Organic chemists are able to synthesize molecules in greater number and chemical complexity than ever before. Yet, a majority of these compounds go untested in biological systems, and those that do are often tested long after the chemist can incorporate the results into synthetic planning. We propose the use of high-dimensional "multiplex" assays, which are capable of measuring thousands of cellular features in one experiment, to annotate rapidly and inexpensively the biological activities of newly synthesized compounds. This readily accessible and inexpensive "real-time" profiling method can be used in a prospective manner to facilitate, for example, the efficient construction of performance-diverse small-molecule libraries that are enriched in bioactives. Here, we demonstrate this concept by synthesizing ten triads of constitutionally isomeric compounds via complexity-generating photochemical and thermal rearrangements and measuring compound-induced changes in cellular morphology via an imaging-based "cell painting" assay. Our results indicate that real-time biological annotation can inform optimization efforts and library syntheses by illuminating trends relating to biological activity that would be difficult to predict if only chemical structure were considered. We anticipate that probe and drug discovery will benefit from the use of optimization efforts and libraries that implement this approach. PMID:27398798

  19. Bioactive Cembrane Derivatives from the Indian Ocean Soft Coral, Sinularia kavarattiensis

    Directory of Open Access Journals (Sweden)

    Katja-Emilia Lillsunde

    2014-07-01

    Full Text Available Marine organisms and their metabolites represent a unique source of potential pharmaceutical substances. In this study, we examined marine-derived substances for their bioactive properties in a cell-based Chikungunya virus (CHIKV replicon model and for in vitro anti-inflammatory activity. In the screening of a marine sample library, crude extracts from the Indian soft coral, Sinularia kavarattiensis, showed promising activity against the CHIKV replicon. Bioassay-guided chemical fractionation of S. kavarattiensis resulted in the isolation of six known norcembranoids (1–6 and one new compound, named kavaranolide (7. The structures were elucidated on the basis of NMR and MS spectroscopic data. Compounds 1–3 and 5–7 were evaluated for their replicon-inhibiting potential in the CHIKV model by using a luminescence-based detection technique and live cell imaging. Compounds 1 and 2 showed moderate inhibition of the CHIKV replicon, but imaging studies also revealed cytotoxic properties. Moreover, the effects of the isolated compounds on primary microglial cells, an experimental model for neuroinflammation, were evaluated. Compound 2 was shown to modulate the immune response in microglial cells and to possess potential anti-inflammatory properties by dose-dependently reducing the release of pro- and anti-inflammatory cytokines.

  20. PIPERIDINE OLIGOMERS AND COMBINATORIAL LIBRARIES THEREOF

    DEFF Research Database (Denmark)

    1999-01-01

    The present invention relates to piperidine oligomers, methods for the preparation of piperidine oligomers and compound libraries thereof, and the use of piperidine oligomers as drug substances. The present invention also relates to the use of combinatorial libraries of piperidine oligomers for...... libraries (arrays) of compounds especially suitable for screening purposes....