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Sample records for biologically active compounds

  1. Biological activity of acetylated phenolic compounds.

    Science.gov (United States)

    Fragopoulou, Elizabeth; Nomikos, Tzortzis; Karantonis, Haralabos C; Apostolakis, Constantinos; Pliakis, Emmanuel; Samiotaki, Martina; Panayotou, George; Antonopoulou, Smaragdi

    2007-01-10

    In recent years an effort has been made to isolate and identify biologically active compounds that are included in the Mediterranean diet. The existence of naturally occurring acetylated phenolics, as well as studies with synthetic ones, provide evidence that acetyl groups could be correlated with their biological activity. Platelet activating factor (PAF) is implicated in atherosclerosis, whereas its inhibitors seem to play a protective role against cardiovascular disease. The aim of this study was to examine the biological activity of resveratrol and tyrosol and their acetylated derivatives as inhibitors of PAF-induced washed rabbit platelet aggregation. Acetylation of resveratrol and tyrosol was performed, and separation was achieved by HPLC. Acetylated derivatives were identified by negative mass spectrometry. The data showed that tyrosol and its monoacetylated derivatives act as PAF inhibitors, whereas diacetylated derivatives induce platelet aggregation. Resveratrol and its mono- and triacetylated derivatives exert similar inhibitory activity, whereas the diacetylated ones are more potent inhibitors. In conclusion, acetylated phenolics exert the same or even higher antithrombotic activity compared to the biological activity of the initial one.

  2. High Resolution Screening of biologically active compounds and metabolites

    NARCIS (Netherlands)

    Kool, J.

    2007-01-01

    High Resolution Screening of biologically active compounds and metabolites Jeroen Kool Biotransformation enzymes play a crucial role in the metabolism of both endogenous compounds and xenobiotics. Usually, the detoxication of these compounds by biotransformation enzymes results in harmless metab

  3. Targeting Platinum Compounds: synthesis and biological activity

    OpenAIRE

    VAN ZUTPHEN, Steven

    2005-01-01

    Inspired by cisplatin, the inorganic drug discovered by Barnett Rosenberg in 1965, the research described in this thesis uses targeting ligands, or ligands varied in a combinatorial fashion, to find platinum complexes with more specific modes of action. These studies have lead to the development of novel (solid-phase) synthetic methods and to the discovery of several compounds with promising biological properties.

  4. Biological active compounds from Georgian Galanthus shaoricus.

    Science.gov (United States)

    Jokhadze, M; Kuchukhidze, J; Chincharadze, D; Murtazashvili, T

    2011-10-01

    Amaryllidaceae alkaloids exhibit antitumour, antiviral and anticholinergic activities. Some of them have been used in the treatment of myasthenia gravis, myopathy and diseases of the nervous system. In this study, the characterization of these compounds from Amaryllidaceae plants along with some biological activities and some regulations to conserve the native flora will be reviewed. Plants materials: Galanthus shaoricus Kem.-Nath., were collected in 2007-2008 during the flowering period in Georgia. The preparation of extracts and fractions were obtained using methanolic maceration. Crude alkaloidal extracts were typically purified by liquid-liquid partitioning of their basic forms in chloroform. Lycorine, galantamine and tazettine has been found as one of the major alkaloid from Amaryllidaceae plants. Galanthus shaoricus have shown good antimalarial and cytotoxic activity in a dose-dependent manner. Methanolic extracts from bulbs demonstrated significant growth inhibition on human Hela and HCT-116 cells lines with IC50 (μg/mL) 16.3±1.8; 22.1±2.9 (aerial parts) and 12.8±1.7; 16.5±1.9 (Bulbs), respectively. Concerning the Amaryllidaceae alkaloids, lycorine with IC50 (μM) 0.8±0.5 and 2.6±0.2, haemantaimene (IC50=1.1±0.7 and 2.7±0.8 μM), hamaine (IC50=3.4±1.0 and 6.2 ±1.4 μM), homolycorine (IC50=1.4±0.9 and 3.3±1.0 μM), hipeastrine (IC50=2.8±1.0 and 7.5±1.8 μM) were found to be responsible for the cytotoxic activity on HCT-116 and Hela cell lines, respectively.

  5. Synthesis,Characterization and Biological Activities of Novel Acrylamide Compounds

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; XU Zhong-jie; ZHANG Gong-sheng; ZHOU Kai; ZHAI Zhi-wei

    2008-01-01

    With dimethomorph and flumorph as the leading compounds,four novel acrylamide compounds with two types of structure were designed and synthesized by means of the method of"me too chemistry".The target compounds were characterized by 1H NMR,IR,MS,and elemental analysis.The influences of solvent and raw material on the yield were investigated and optimum processing conditions were determined.The results of preliminary biological tests show that all those compounds exhibit certain antifungal activities.

  6. Aspartate and glutamate mimetic structures in biologically active compounds.

    Science.gov (United States)

    Stefanic, Peter; Dolenc, Marija Sollner

    2004-04-01

    Glutamate and aspartate are frequently recognized as key structural elements for the biological activity of natural peptides and synthetic compounds. The acidic side-chain functionality of both the amino acids provides the basis for the ionic interaction and subsequent molecular recognition by specific receptor sites that results in the regulation of physiological or pathophysiological processes in the organism. In the development of new biologically active compounds that possess the ability to modulate these processes, compounds offering the same type of interactions are being designed. Thus, using a peptidomimetic design approach, glutamate and aspartate mimetics are incorporated into the structure of final biologically active compounds. This review covers different bioisosteric replacements of carboxylic acid alone, as well as mimetics of the whole amino acid structure. Amino acid analogs presented include those with different distances between anionic moieties, and analogs with additional functional groups that result in conformational restriction or alternative interaction sites. The article also provides an overview of different cyclic structures, including various cycloalkane, bicyclic and heterocyclic analogs, that lead to conformational restriction. Higher di- and tripeptide mimetics in which carboxylic acid functionality is incorporated into larger molecules are also reviewed. In addition to the mimetic structures presented, emphasis in this article is placed on their steric and electronic properties. These mimetics constitute a useful pool of fragments in the design of new biologically active compounds, particularly in the field of RGD mimetics and excitatory amino acid agonists and antagonists.

  7. Synthesis, Characterization and Biological Activities of Organotin (IV Methylcyclohexyldithiocarbamate Compounds

    Directory of Open Access Journals (Sweden)

    Normah Awang

    2011-01-01

    Full Text Available Problem statement: The growing interest in the chemistry of sulphur donor ligands are due to their encouraging anticancer, antibacterial and antifungal activities as well as their widespread industrial application. Dithiocarbamates belong to this class and much attention has been paid to them. Approach: Novel organotin compounds with the molecular formula RmSn[S2CN(CH3(C6H11]4-m (where m = 2, R = CH3, C2H5; m = 3, R = C6H5 have been synthesized using in situ method. These compounds were characterized by elemental analysis, IR, 1H and 13C NMR spectroscopy. Results: Elemental analysis revealed that all compounds were of good purity. Infrared spectra of the compounds showed that the thioureide ν(C-N band was in the region 1450-1500 cm−1. The unsplitting band of ν(C-S in the region 974-979 cm−1 indicated the bidentate nature of the chelated dithiocarbamato legends. The 13C NMR chemical shift of the carbon atom in the N-CS2 group appeared in the range of 196.29-199.82 ppm. Single crystal analysis from one of these compounds showed that the chelating mode of the dithiocarbamate groups was isobidentate. These compounds have been screened for antibacterial activity against four bacteria; Staphylococcus aureus, Salmonella typhimurium, Pseudomonas aeruginosa and Bacillus subtilis. Only one of these compounds shows promising results against S. aureus and S. typhi. Cytotoxicity screening on human leukemic promyelocyte HL-60 cells found that two of these compounds were very active with CD50 values of 0.87 and 0.18 µg mL−1. Conclusion: The studied compounds were found to have the potential in biological activity especially in cytotoxicity where this possibly can be used for clinical trials after further research.

  8. Biological Activities of Phenolic Compounds Present in Virgin Olive Oil

    OpenAIRE

    2010-01-01

    The Mediterranean diet is associated with a lower incidence of atherosclerosis, cardiovascular disease, neurodegenerative diseases and certain types of cancer. The apparent health benefits have been partially ascribed to the dietary consumption of virgin olive oil by Mediterranean populations. Much research has focused on the biologically active phenolic compounds naturally present in virgin olive oils to aid in explaining reduced mortality and morbidity experienced by people consuming a trad...

  9. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil.

    Science.gov (United States)

    Servili, Maurizio; Sordini, Beatrice; Esposto, Sonia; Urbani, Stefania; Veneziani, Gianluca; Di Maio, Ilona; Selvaggini, Roberto; Taticchi, Agnese

    2013-12-20

    Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO) phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  10. Biological Activities of Phenolic Compounds of Extra Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Maurizio Servili

    2013-12-01

    Full Text Available Over the last few decades, multiple biological properties, providing antioxidant, anti-inflammatory, chemopreventive and anti-cancer benefits, as well as the characteristic pungent and bitter taste, have been attributed to Extra Virgin Olive Oil (EVOO phenols. In particular, growing efforts have been devoted to the study of the antioxidants of EVOO, due to their importance from health, biological and sensory points of view. Hydrophilic and lipophilic phenols represent the main antioxidants of EVOO, and they include a large variety of compounds. Among them, the most concentrated phenols are lignans and secoiridoids, with the latter found exclusively in the Oleaceae family, of which the drupe is the only edible fruit. In recent years, therefore, we have tackled the study of the main properties of phenols, including the relationships between their biological activity and the related chemical structure. This review, in fact, focuses on the phenolic compounds of EVOO, and, in particular, on their biological properties, sensory aspects and antioxidant capacity, with a particular emphasis on the extension of the product shelf-life.

  11. Phenolic Compounds Characterization and Biological Activities of Citrus aurantium Bloom

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    Armin Oskoueian

    2012-01-01

    Full Text Available Citrus plants are known to possess beneficial biological activities for human health. In addition, ethnopharmacological application of plants is a good tool to explore their bioactivities and active compounds. This research was carried out to evaluate the phenolic and flavonoid analysis, antioxidant properties, anti inflammatory and anti cancer activity of Citrus aurantium bloom. The total phenolics and flavonoids results revealed that methanolic extract contained high total phenolics and flavonoids compared to ethanolic and boiling water extracts. The obtained total phenolics value for methanolic Citrus aurantium bloom extract was 4.55 ± 0.05 mg gallic acid equivalent (GAE/g dry weight (DW, and for total flavonoids it was 3.83 ± 0.05 mg rutin equivalent/g DW. In addition, the RP-HPLC analyses of phenolics and flavonoids indicated the presence of gallic acid, pyrogallol, syringic acid, caffeic acid, rutin, quercetin and naringin as bioactive compounds. The antioxidant activity of Citrus aurantium bloom were examined by the 1,1-diphenyl-2-picryl-hydrazyl (DPPH assay and the ferric reducing/antioxidant potential (FRAP. The free radical scavenging and ferric reducing power activities were higher for the methanolic extract of Citrus aurantium bloom at a concentration of 300 μg/mL, with values of 55.3% and 51.7%, respectively, as compared to the corresponding boiling water and ethanolic extracts, but the activities were lower than those of antioxidant standards such as BHT and α-tocopherol. Furthermore, the anti-inflammatory result of methanolic extract showed appreciable reduction in nitric oxide production of stimulated RAW 264.7 cells at the presence of plant extract. Apart from that, the anticancer activity of the methanolic extract was investigated in vitro against human cancer cell lines (MCF-7; MDA-MB-231, human colon adenocarcinoma (HT-29 and Chang cell as a normal human hepatocyte. The obtained result demonstrated the moderate to

  12. Studies on Synthesis and Biological Activities of Novel Triazole Compounds Containing 1,3-Dioxolane

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Nine title compounds were synthesized. Their strucures were identified by means of IR, EA, 1H NMR and MS. The results from the primary biological test show that all the compounds have some activitiies of fungicide and plant growth regulator. When R group is 2,4-Cl2C6H3, compound 2 or compound 4 shows better biological activities.

  13. [Biological activity of selenorganic compounds at heavy metal salts intoxication].

    Science.gov (United States)

    Rusetskaya, N Y; Borodulin, V B

    2015-01-01

    Possible mechanisms of the antitoxic action of organoselenium compounds in heavy metal poisoning have been considered. Heavy metal toxicity associated with intensification of free radical oxidation, suppression of the antioxidant system, damage to macromolecules, mitochondria and the genetic material can cause apoptotic cell death or the development of carcinogenesis. Organic selenium compounds are effective antioxidants during heavy metal poisoning; they exhibit higher bioavailability in mammals than inorganic ones and they are able to activate antioxidant defense, bind heavy metal ions and reactive oxygen species formed during metal-induced oxidative stress. One of promising organoselenium compounds is diacetophenonyl selenide (DAPS-25), which is characterized by antioxidant and antitoxic activity, under conditions including heavy metal intoxication.

  14. Biological activities of lignin hydrolysate-related compounds

    Directory of Open Access Journals (Sweden)

    Siseon Lee

    2012-05-01

    Full Text Available Lignin hydrolysates contain many different chemical species,including ferulic acid, coumaric acid, vanillic acid, vanillin,syringaldehyde and furfural. From the perspective of biofuels,these compounds are problematic and can cause downstreamloss of product if not removed prior to beginning the fermentativeprocess. In contrast, a search for these compounds withinthe literature turns up many papers where the same compoundshave beneficial properties pertaining to human health,including as antioxidants and in cancer prevention, or are involvedin bacterial cell-to-cell signaling. Consequently, this articlereviews the dual nature of these and other compoundsfound in lignin hydrolysates, highlighting both their detrimentaland beneficial activities. [BMB Reports 2012; 45(5:265-274

  15. Synthesis, Characterization and Biological Activities of Organotin (IV) Methylcyclohexyldithiocarbamate Compounds

    OpenAIRE

    Normah Awang; Ibrahim Baba; Yamin, Bohari M.; Mohd S. Othman; Nurul F. Kamaludin

    2011-01-01

    Problem statement: The growing interest in the chemistry of sulphur donor ligands are due to their encouraging anticancer, antibacterial and antifungal activities as well as their widespread industrial application. Dithiocarbamates belong to this class and much attention has been paid to them. Approach: Novel organotin compounds with the molecular formula RmSn[S2CN(CH3)(C6H11)]4-m (where m = 2, R = CH3, C2H5; m = 3, R = C6H5) have been synthesized using in situ method. The...

  16. Therapeutic Uses and Pharmacological Properties of Garlic, Shallot, and Their Biologically Active Compounds

    Directory of Open Access Journals (Sweden)

    Peyman Mikaili

    2013-10-01

    Garlic and shallots are safe and rich sources of biologically active compounds with low toxicity. Further studies are needed to confirm the safety and quality of the plants to be used by clinicians as therapeutic agents.

  17. Studies on Syntheses and Biological Activities of Novel Triazole Compounds Containing Phosphorodithioate Groups

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; ZHANG Shu-sheng; CHEN Xiao; JIAO Kui

    2003-01-01

    Sixteen new triazole organic phosphorus compounds were synthesized. Their structures were confirmed with IR, 1H NMR, elemental analysis and MS. The primary biological tests show that the titled compounds have the fungicidal activities, which are influenced by R groups and the substituents attached to the P atom.

  18. Studies on Synthesis and Biological Activities of Novel Triazole compounds Containing Thiophene Groups

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; ZHANG Shu-sheng; HU Zhi-qiang; JIAO Kui

    2003-01-01

    Fifteen new triazole compounds containing thiophene groups were synthesized and their structures were confirmed by means of 1H NMR, IR, MS spectroscopies and elemental analyses. The preliminary biological tests show that the titled compounds exhibit some activities of fungicides and plant growth regulators.

  19. Case study: Comparison of biological active compounds in milk from organic and conventional dairy herds

    Science.gov (United States)

    Conflicting reports of the quantities of biologically active compounds present in milk from organic grass-fed and conventional herds show that more research is required, especially as these compounds are linked to human health benefits and can improve the health value consumers place on dairy produc...

  20. Biologically Active Macrocyclic Compounds – from Natural Products to Diversity‐Oriented Synthesis

    DEFF Research Database (Denmark)

    Madsen, Charlotte Marie; Clausen, Mads Hartvig

    2011-01-01

    Macrocyclic compounds are attractive targets when searching for molecules with biological activity. The interest in this compound class is increasing, which has led to a variety of methods for tackling the difficult macrocyclization step in their synthesis. This microreview highlights some recent...

  1. Structure and Biological Activities of Novel Triazole Compounds Containing 1,3,4-Oxadiazole Ring

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; BI Wen-zhao; SHANG Yu-qing; ZHAI Zhi-wei; YI Xu

    2008-01-01

    Eighteen novel triazole compounds containing 1,3,4-oxadiazole groups were synthesized from 2-(1H-1,2,4-triazol-1-y1)acetohydrazide and carbon disulfide by several step reactions. The target compounds were characterized by elemental analysis, 1H NMR, 13C NMR, IR, MS, and X-ray crystallography. The results of preliminary biological tests show that all the compounds exhibit certain fungicidal activities.

  2. Baltic cyanobacteria- A source of biologically active compounds

    Digital Repository Service at National Institute of Oceanography (India)

    Mazur-Marzec, H.; Błaszczyk, A; Felczykowska, A; Hohlfeld, N; Kobos, J.; Toruńska-Sitarz, A; PrabhaDevi; Montalva`o, S.; DeSouza, L.; Tammela, P.; Mikosik, A; Bloch, S.; Nejman-Faleńczyk, B.; Węgrzyn, G.

    and chemotypes were tested in a wide variety of assays. The cyanobacteria showed strain-specific differences in the induced effects. The extracts from Nodularia spumigena CCNP1401 were active in the highest number of tests, including protease and phosphatase...

  3. Synthesis and Antiplatelet Activity of Antithrombotic Thiourea Compounds: Biological and Structure-Activity Relationship Studies

    Directory of Open Access Journals (Sweden)

    André Luiz Lourenço

    2015-04-01

    Full Text Available The incidence of hematological disorders has increased steadily in Western countries despite the advances in drug development. The high expression of the multi-resistance protein 4 in patients with transitory aspirin resistance, points to the importance of finding new molecules, including those that are not affected by these proteins. In this work, we describe the synthesis and biological evaluation of a series of N,N'-disubstituted thioureas derivatives using in vitro and in silico approaches. New designed compounds inhibit the arachidonic acid pathway in human platelets. The most active thioureas (compounds 3d, 3i, 3m and 3p displayed IC50 values ranging from 29 to 84 µM with direct influence over in vitro PGE2 and TXA2 formation. In silico evaluation of these compounds suggests that direct blockage of the tyrosyl-radical at the COX-1 active site is achieved by strong hydrophobic contacts as well as electrostatic interactions. A low toxicity profile of this series was observed through hemolytic, genotoxic and mutagenic assays. The most active thioureas were able to reduce both PGE2 and TXB2 production in human platelets, suggesting a direct inhibition of COX-1. These results reinforce their promising profile as lead antiplatelet agents for further in vivo experimental investigations.

  4. [Progress in study of flavonoids from Annonaceae and biological activities of these compounds].

    Science.gov (United States)

    Hu, Chun-Mei; Wu, Jiu-Hong

    2007-05-01

    More than 50 new flavonoids derived from Annonaceae are reported in the last two decades. Many genuses in Annonaceae contain flavonoids having structural novelty and broad pharmacological activities. Due to the pharmacological interest of some of these compounds, chemical investigations on this topic have grown considerably in the decades. Here the biological activities of some of these flavonoids are also briefly discussed.

  5. Supercritical Algal Extracts: A Source of Biologically Active Compounds from Nature

    Directory of Open Access Journals (Sweden)

    Izabela Michalak

    2015-01-01

    Full Text Available The paper discusses the potential applicability of the process of supercritical fluid extraction (SFE in the production of algal extracts with the consideration of the process conditions and yields. State of the art in the research on solvent-free isolation of biologically active compounds from the biomass of algae was presented. Various aspects related with the properties of useful compounds found in cells of microalgae and macroalgae were discussed, including their potential applications as the natural components of plant protection products (biostimulants and bioregulators, dietary feed and food supplements, and pharmaceuticals. Analytical methods of determination of the natural compounds derived from algae were discussed. Algal extracts produced by SFE process enable obtaining a solvent-free concentrate of biologically active compounds; however, detailed economic analysis, as well as elaboration of products standardization procedures, is required in order to implement the products in the market.

  6. [Biosynthesis of biologically active low-molecular weight compounds by fungi of the genus Penicillium (review)].

    Science.gov (United States)

    Kozlovskii, A G; Antipova, T V; Zhelifonova, V P

    2015-01-01

    The recent data on exometabolite biosynthesis in fungi of the genus Penicillium is summarized. The study of creative species, as well as those isolated from extreme ecotopes, resulted in the identification of a number of novel, biologically active compounds. Alkaloid biosynthesis has been shown to begin on.the first day of fungus cultivation and to proceed throughout the cultivation period. Idiophase kinetics was observed for the biosynthesis of polyketide metabolites. The mechanisms of regulation of biosynthesis of promising bioactive compounds are discussed.

  7. The phenolic compounds of olive oil: structure, biological activity and beneficial effects on human health.

    Science.gov (United States)

    Tripoli, Elisa; Giammanco, Marco; Tabacchi, Garden; Di Majo, Danila; Giammanco, Santo; La Guardia, Maurizio

    2005-06-01

    The Mediterranean diet is rich in vegetables, cereals, fruit, fish, milk, wine and olive oil and has salutary biological functions. Epidemiological studies have shown a lower incidence of atherosclerosis, cardiovascular diseases and certain kinds of cancer in the Mediterranean area. Olive oil is the main source of fat, and the Mediterranean diet's healthy effects can in particular be attributed not only to the high relationship between unsaturated and saturated fatty acids in olive oil but also to the antioxidant property of its phenolic compounds. The main phenolic compounds, hydroxytyrosol and oleuropein, which give extra-virgin olive oil its bitter, pungent taste, have powerful antioxidant activity both in vivo and in vitro. The present review focuses on recent works analysing the relationship between the structure of olive oil polyphenolic compounds and their antioxidant activity. These compounds' possible beneficial effects are due to their antioxidant activity, which is related to the development of atherosclerosis and cancer, and to anti-inflammatory and antimicrobial activity.

  8. BASIC SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME PHOSPHORCONTATNING ORGANIC COMPOUNDS CONTAINING FRAGMENTS OF UREA AND TRYHLORETILAMID

    Directory of Open Access Journals (Sweden)

    Gushylyk B.

    2013-10-01

    Full Text Available Data about directions of synthesis and use of the phosphororganic compounds in technics, biology and medicine is presented in the paper. Antimicrobial activity of 51 phosphororganic salts and ilides containing urine and threechlor ethylenamide has been studied. Perspective of the development of effective antimicrobial substances has been determined

  9. Moooving forward on determining biologically active compounds in milk and their impact on health

    Science.gov (United States)

    Recent studies have demonstrated that some of the lesser studied components in milk, known as biologically active compounds (BACs), may provide potential benefits to human health. The added health-value of raw milk and milk from organic and grass-fed herds is strongly debated because of limited, an...

  10. Emergy Evaluations of the Global Biogeochemical Cycles of Six Biologically Active Elements and Two Compounds

    Science.gov (United States)

    Estimates of the emergy carried by the flows of biologically active elements (BAE) and compounds are needed to accurately evaluate the near and far field effects of anthropogenic wastes. The transformities and specific emergies of these elements and of their different chemical sp...

  11. Spectral Response and Diagnostics of Biological Activity of Hydroxyl-Containing Aromatic Compounds

    Science.gov (United States)

    Tolstorozhev, G. B.; Mayer, G. V.; Bel'kov, M. V.; Shadyro, O. I.

    2016-08-01

    Using IR Fourier spectra and employing quantum-chemical calculations of electronic structure, spectra, and proton-acceptor properties, synthetic derivatives of aminophenol exhibiting biological activity in the suppression of herpes, influenza, and HIV viruses have been investigated from a new perspective, with the aim of establishing the spectral response of biological activity of the molecules. It has been experimentally established that the participation of the aminophenol hydroxyl group in intramolecular hydrogen bonds is characteristic of structures with antiviral properties. A quantum-chemical calculation of the proton-acceptor ability of the investigated aminophenol derivatives has shown that biologically active structures are characterized by a high proton-acceptor ability of oxygen of the hydroxyl group. A correlation that has been obtained among the formation of an intramolecular hydrogen bond, high proton-acceptor ability, and antiviral activity of substituted aminophenols enables us to predict the pharmacological properties of new medical preparations of the given class of compounds.

  12. Composition of thermodestruction products of biologically active compounds polluting the atmosphere

    Energy Technology Data Exchange (ETDEWEB)

    Dmitriyev, M.T.; Rastyannikov, Y.G.; Sotnikov, Y.Y.; Volkov, S.A.

    1981-01-01

    The most promising method of removal of biologically active compounds such as microorganisms, antibiotics, food and other household waste from industrial waste gases is to destroy them by thermal destruction including burning. In this case, products of thermodestruction enter into the atmosphere along with carbon dioxide and steam and can unfavorably affect the population. Thus, mass spectrometric analyses have determined in the waste gases of antibiotics production aldehydes and ketones (croton- and adipalaldehydes, acetone), alcohols (propanol and butanol), amines, unsaturated and aromatic hydrocarbons. The composition of thermodestruction products of biologically active compounds was identified by their pyrolysis at 700/sup 0/C for 2 min. in the presence of air. The main components were proteins and amino acids. The products of pyrolysis were analyzed by chromato-mass-spectrometric and gas-chromatographic methods by means of a two-flame thermionic detector. No significant difference between the thermodestruction products of proteins and amino acids was found. Many of detected substances can be not only toxic but also emit strong unpleasant odors. The studies revealed toxic substances that pollute the atmospheric air during removal of biologically-active compounds from waste gases.

  13. The importance of extremophile cyanobacteria in the production of biologically active compounds

    Directory of Open Access Journals (Sweden)

    Drobac-Čik Aleksandra V.

    2007-01-01

    Full Text Available Due to their ability to endure extreme conditions, terrestrial cyanobacteria belong to a group of organisms known as "extremophiles". Research so far has shown that these organisms posses a great capacity for producing biologically active compounds (BAC. The antibacterial and antifungal activities of methanol extracts of 21 cyanobacterial strains belonging to Anabaena and Nostoc genera, previously isolated from different soil types and water resources in Serbia, were evaluated. In general, larger number of cyanobacterial strains showed antifungal activity. In contrast to Nostoc, Anabaena strains showed greater diversity of antibacterial activity (mean value of percentages of sensitive targeted bacterial strains 3% and 25.9% respectively. Larger number of targeted fungi was sensitive to cultural liquid extract (CL, while crude cell extract (CE affected more bacterial strains. According to this investigation, the higher biological activity of terrestrial strains as representatives of extremophiles may present them as significant BAC producers. This kind of investigation creates very general view of cyanobacterial possibility to produce biologically active compounds but it points out the necessity of exploring terrestrial cyanobacterial extremophiles as potentially excellent sources of these substances and reveals the most prospective strains for further investigations.

  14. A concise review of applications of micellar liquid chromatography to study biologically active compounds.

    Science.gov (United States)

    Stępnik, Katarzyna E

    2017-01-01

    The features of micellar systems are outstanding compared with conventional RP-LC ones. Therefore, the unique properties of micellar chromatography (MLC) are widely recognized. In this short review the applicability of MLC as an in vitro method for the determination of biological activity is discussed. For this purpose many specific examples of MLC applications supported by the theoretical backgrounds of the cited biological activity areas as well as the factors affecting them are presented. This study collects and organizes the most important references of bioactivity determination which were created both recently and in the past, using the MLC method. Although there are many papers on the MLC there is no literature review focused particularly on its applicability in the study of biological activity of various compounds. This work can be treated as a significant review of so far published papers which particularly emphasizes the importance of MLC as in vitro method for determination of bioactivity of different compounds. Copyright © 2016 John Wiley & Sons, Ltd.

  15. Compounds Released from Biomass Deconstruction: Understanding Their Effect on Cellulose Enzyme Hydrolysis and Their Biological Activity

    Science.gov (United States)

    Djioleu, Angele Mezindjou

    The effect of compounds produced during biomass pretreatment on cellulolytic enzyme was investigated. Liquid prehydrolyzates were prepared by pretreating switchgrass using 24 combinations of temperature, time, and sulfuric acid concentration based on a full factorial design. Temperature was varied from 140°C to 180°C; time ranged from 10 to 40 min; and the sulfuric acid concentrations were 0.5% or 1% (v/v). Identified products in the prehydrolyzates included xylose, glucose, hydroxymethylfurfural (HMF), furfural, acetic acid, formic acid, and phenolic compounds at concentration ranging from 0 to 21.4 g/L. Pretreatment conditions significantly affected the concentrations of compounds detected in prehydrolyzates. When assayed in the presence of switchgrass prehydrolyzates against model substrates, activities of cellulase, betaglucosidase, and exoglucanase, were significantly reduced by at least 16%, 31.8%, and 57.8%, respectively, as compared to the control. A strong positive correlation between inhibition of betaglucosidase and concentration of glucose, acetic acid, and furans in prehydrolyzate was established. Exoglucanase inhibition correlated with the presence of phenolic compounds and acetic acid. The prehydrolyzate, prepared at 160°C, 30 min, and 1% acid, was fractionated by centrifugal partition chromatography (CPC) into six fractions; the inhibition effect of these fractions on betaglucosidase and exoglucanase was determined. The initial hydrolysis rate of cellobiose by betaglucosidase was significantly reduced by the CPC sugar-rich fraction; however, exoglucanase was deactivated by the CPC phenolic-rich fraction. Finally, biological activities of water-extracted compounds from sweetgum bark and their effect on cellulase was investigated. It was determined that 12% of solid content of the bark extract could be accounted by phenolic compounds with gallic acid identified as the most concentrated phytochemical. Sweetgum bark extract inhibited Staphylococcus

  16. Ab initio computational study of vincristine as a biological active compound: NMR and NBO analyses

    Directory of Open Access Journals (Sweden)

    Shiva Joohari

    2015-06-01

    Full Text Available Vincristine is a biological active alkaloid that has been used clinically against a variety of neoplasms. In the current study we have theoretically investigated the magnetic properties of titled compound to predict physical and chemical properties of vincristine as a biological inhibitor. Ab initio computation using HF and B3LYP with 3-21G(d and 6-31G(d level of theory have been performed and then magnetic shielding tensor (, ppm, shielding asymmetry (, magnetic shielding anisotropy (aniso, ppm, the skew of a tensor (K, chemical shift anisotropy ( and chemical shift ( were calculated to indicate the details of the interaction mechanism between microtubules and vincristine. Moreover, EHOMO, ELUMO and Ebg were evaluated. The maximum and minimum values of Ebg were found in HF/3-21g and B3LYP/3-21g respectively. It was also uggested that O24, O37, O49 and O55 with minimum values of iso, are active sites of titled compound. Furthermore the calculated chemical shifts were compared with experimental data in DMSO and CDCl3 solvents.

  17. Chemical reactivity and biological activity of chalcones and other α,β-unsaturated carbonyl compounds.

    Science.gov (United States)

    Maydt, Daniela; De Spirt, Silke; Muschelknautz, Christian; Stahl, Wilhelm; Müller, Thomas J J

    2013-08-01

    Abstract 1. Chalcones are structural analogues of benzalacetophenone (BAP). Several derivatives have been identified in plants and anticarcinogenic and anti-inflammatory properties were attributed to the compounds, probably related to their direct antioxidant activity or stimulatory effects on the expression of endogenous defence enzymes like hemeoxygenase-1 (HO-1). HO-1 expression is triggered by the Nrf2-Keap1 signalling pathway, initiated by the addition of chalcones to thiol groups of Keap1 via Michael-type reaction. 2. The present study used a model system estimating the reactivity of different synthetic chalcones and other α,β-unsaturated carbonyl compounds with thiols and compared the chemical reactivity with the biological activity, measured by HO-1 expression in human dermal fibroblasts. 3. Chemical reactivity with the thiol group of N-acetylcysteine was determined with 5,5'-dithiobis-(2-nitrobenzoic acid) and followed chemical principles of structure-reactivity relationship. Most reactive were sulforaphane, dimethylfumarate, chalcone 3 ((2E)-1-phenyl-3-pyrimidin-2-ylprop-2-en-1-one) and chalcone 7 (1,3-diphenylprop-2-yn-1-one). This result demonstrates that α,β-unsaturated carbonyl derivatives react with thiols differently. All compounds were also biologically active; however, expression of HO-1 was not only related to the chemical reactivity but also to the lipophilicity of the molecules which likely affected transmembrane uptake. Most efficient inducers of HO-1 expression were BAP, 4-hydroxynonenal and chalcone 1 (4-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]benzonitrile), chalcone 5 ((2E)-1-phenyl-3-[4-(trifluoromethyl)-phenyl]prop-2-en-1-one) and chalcone 7.

  18. Microwave-Mediated Hetero Diels-Alder reaction: Synthesis of biologically active compounds

    OpenAIRE

    D’Aurizio, Antonio

    2009-01-01

    Heterocyclic compounds represent almost two-thirds of all the known organic compounds: they are widely distributed in nature and play a key role in a huge number of biologically important molecules including some of the most significant for human beings. A powerful tool for the synthesis of such compounds is the hetero Diels-Alder reaction (HDA), that involve a [4+2] cycloaddition reaction between heterodienes and suitable dienophiles. Among heterodienes to be used in such six-membered ...

  19. Synthesis, Structure and Biological Activities of Novel Triazole Compounds Containing Thioamide Group

    Institute of Scientific and Technical Information of China (English)

    刘法谦; 秦永其; 许良忠; 陆路德; 杨绪杰; 汪信

    2005-01-01

    Two compounds 2-benzoyl-N-phenyl-2-( 1,2,4-triazol- 1-yl)thioacetamide (1) and 2-(4-chlorobenzoyl)-N-phenyl-2-(1,2,4-triazol-1-yl)thioacetamide (2) were synthesized from substituted acetophenone, triazole and phenyl isothiocyanate by several step reactions. The structure of compound 1 was determined by single-crystal X-ray diffraction analysis. It crystallizes in monoclinic system with space group P21/c, a =0.8806(2) nm, b= 1.2097(2) nm, c= 1.4809(3) nm, β=105.88°, Z=4, V=1.5173(6) nm3, Dc= 1.411 Mg/m3, μ=0.22 mm-1, F(000)=672, final R1=0.040 and Rw=0.103. There is obvious potentially weak C—H…N intermolecular interaction in the crystal, which stabilizes the structure. The results of biological test show that the two compounds have antifungal and plant growth regulating activities.

  20. Review of the Inhibition of Biological Activities of Food-Related Selected Toxins by Natural Compounds

    Directory of Open Access Journals (Sweden)

    Reuven Rasooly

    2013-04-01

    Full Text Available There is a need to develop food-compatible conditions to alter the structures of fungal, bacterial, and plant toxins, thus transforming toxins to nontoxic molecules. The term ‘chemical genetics’ has been used to describe this approach. This overview attempts to survey and consolidate the widely scattered literature on the inhibition by natural compounds and plant extracts of the biological (toxicological activity of the following food-related toxins: aflatoxin B1, fumonisins, and ochratoxin A produced by fungi; cholera toxin produced by Vibrio cholerae bacteria; Shiga toxins produced by E. coli bacteria; staphylococcal enterotoxins produced by Staphylococcus aureus bacteria; ricin produced by seeds of the castor plant Ricinus communis; and the glycoalkaloid α-chaconine synthesized in potato tubers and leaves. The reduction of biological activity has been achieved by one or more of the following approaches: inhibition of the release of the toxin into the environment, especially food; an alteration of the structural integrity of the toxin molecules; changes in the optimum microenvironment, especially pH, for toxin activity; and protection against adverse effects of the toxins in cells, animals, and humans (chemoprevention. The results show that food-compatible and safe compounds with anti-toxin properties can be used to reduce the toxic potential of these toxins. Practical applications and research needs are suggested that may further facilitate reducing the toxic burden of the diet. Researchers are challenged to (a apply the available methods without adversely affecting the nutritional quality, safety, and sensory attributes of animal feed and human food and (b educate food producers and processors and the public about available approaches to mitigating the undesirable effects of natural toxins that may present in the diet.

  1. Bioreactor Cultivation of Zeltnera beyrichii (Torr. & A. Gray Mans.: A Novel Source of Biologically Active Compounds

    Directory of Open Access Journals (Sweden)

    Miloš Radović

    2013-08-01

    Full Text Available With regard to world’s increasing demand for biologically active compounds, a novel source of xanthones and secoiridoid glycosides has been studied . Zeltnera beyrichii (Torr. & A. Gray Mans., an insufficiently acknowledged North American medicinal plant species, may be considered a pharmacological substitute for commercial C. erythraea Rafn, since it accumulates in aerial parts nearly the same amount of secoiridoid glycosides: swertiamarin, gentiopicrin, and sweroside (13.76, 7.56, and 0.17 mmol per 100 g dry weight, respectively in plants grown under greenhouse condition, and a considerable amount of xanthones: decussatin and eustomin. Additionally, Z. beyrichii produced as much biomass during cultivation in RITA ® temporary immersion bioreactors as greenhouse-grown plants, in a third of the time. Plants grown in bioreactors contained moderate levels of total phenolics and total flavonoids, and possessed modest antioxidant activity and antimicrobial potential against eight bacterial and eight fungal species. Therefore, this species may be highly recommended for cultivation either in natural environment, or in bioreactors under in vitro conditions, for producing compounds of interest of modern pharmacology and food industry.

  2. Biologically active vitamin B12 compounds in foods for preventing deficiency among vegetarians and elderly subjects.

    Science.gov (United States)

    Watanabe, Fumio; Yabuta, Yukinori; Tanioka, Yuri; Bito, Tomohiro

    2013-07-17

    The usual dietary sources of vitamin B12 are animal-source based foods, including meat, milk, eggs, fish, and shellfish, although a few plant-based foods such as certain types of dried lavers (nori) and mushrooms contain substantial and considerable amounts of vitamin B12, respectively. Unexpectedly, detailed characterization of vitamin B12 compounds in foods reveals the presence of various corrinoids that are inactive in humans. The majority of edible blue-green algae (cyanobacteria) and certain edible shellfish predominately contain an inactive corrinoid known as pseudovitamin B12. Various factors affect the bioactivity of vitamin B12 in foods. For example, vitamin B12 is partially degraded and loses its biological activity during cooking and storage of foods. The intrinsic factor-mediated gastrointestinal absorption system in humans has evolved to selectively absorb active vitamin B12 from naturally occurring vitamin B12 compounds, including its degradation products and inactive corrinoids that are present in daily meal foods. The objective of this review is to present up-to-date information on various factors that can affect the bioactivity of vitamin B12 in foods. To prevent vitamin B12 deficiency in high-risk populations such as vegetarians and elderly subjects, it is necessary to identify plant-source foods that contain high levels of bioactive vitamin B12 and, in conjunction, to prepare the use of crystalline vitamin B12-fortified foods.

  3. Thermodynamic and transport properties of some biologically active compounds in aqueous solutions at different temperatures

    Energy Technology Data Exchange (ETDEWEB)

    Dhondge, Sudhakar S., E-mail: s_dhondge@hotmail.co [P.G. Department of Chemistry, S.K. Porwal College, Kamptee, Nagpur 441 002 (India); Zodape, Sangesh P.; Parwate, Dilip V. [Department of Chemistry, R.T.M. Nagpur University, Nagpur 440 033 (India)

    2011-01-15

    The experimental data of density and viscosity have been obtained for aqueous solutions of biologically active compounds like salbutamol sulphate (SS), diethylcarbamazine citrate (DEC), and chlorpheniramine maleate (CPM) in the concentration range (0 to 0.15) mol . kg{sup -1} at three different temperatures. The derived parameters, such as apparent molar volume of solute ({phi}{sub V})), limiting apparent molar volume of solute ({phi}{sub V}{sup 0}), limiting apparent molar expansivity ({phi}{sub E}{sup 0}), thermal expansion coefficient ({alpha}*) and Jones-Dole equation viscosity A and B coefficients, were obtained using the density and viscosity results. It has been observed that the electrolyte-salt (SS) as well as adducts exhibit a positive viscosity B coefficient having negative ((dB)/(dT)). These results are interpreted in the light of possible solute-solute and solute-solvent interactions.

  4. Synthesis, Structure and Biological Activities of Novel Triazole Compounds Containing N,N-Dialkyldithiocarbamate Moiety

    Institute of Scientific and Technical Information of China (English)

    XU,Liang-Zhong(许良忠); JIAN,Fang-Fang(建方方); SHI,Jian-Gang(时建刚); SUN,Ping-Ping(孙萍萍); JIAO,Kui(焦奎)

    2004-01-01

    The two compounds, 2,2-dimethyl-4-S-(N,N-dimethyldithiocarbamato)-5-(1,2,4-triazol-1-yl)-propione (1) and 2,2-dimethyl-4-S-(N,N-diethyldithiocarbamato)-5-(1,2,4-triazol-1-yl)-3-propione (2), were prepared by reacting N,N-dialkyldithiocarbamate sodium with 2,2-dimethyl-4-bromo-5-(1,2,4-triazol-1-yl)-propione. Their structures were identified by elemental analysis, IR and 1H NMR spectroscopy. The structure of 1 has been determined by X-ray single crystal structure analysis. It crystallizes in monoclinic system with space group P21/c, a= 1.2315(3)nm, b =1.2057(2) nm, c=1.2532(3) nm, β=118.55(3)° Z=4, V= 1.6345(6) nm3, Dc= 1.221 g/cm3, μ=0.324 mm -1, F(000)=640, final R1 =0.0449. There is obvious potentially weak C-H…N intermolecular interaction in the crystal, which stabilizes the crystal structure. The result of the biological test showed that the two compounds have fungistasis and plant growth regulating activities.

  5. Synthesis and biological activity of some heterocyclic compounds containing benzimidazole and beta-lactam moiety

    Indian Academy of Sciences (India)

    K F Ansari; C Lal

    2009-11-01

    A number of 1-substituted-2-methyl benzimidazole derivatives have been synthesized and tested for their antibacterial activities. The chemical structures of the newly synthesized compounds were verified on the basis of spectral and elemental methods of analyses. Investigation of antimicrobial activity of the compounds was done by disc diffusion method using Gram-positive (S. aureus, S. mutans and B. subtilis), Gram-negative (E. coli, S. typhi and P. aeruginosa) bacteria and fungi (C. albicans, A. flavus and A. niger). Among the compounds tested 5a, 5b, 5d, 5i, 5j and 5k exhibited good antibacterial activities against Gram positive bacteria, while 5d and 5i also showed notable antifungal activity. Specially compounds 5a and 5b exhibited appreciable activity against S. aureus and B. subtilis comparable to reference drugs.

  6. Proline catalyzed α-aminoxylation reaction in the synthesis of biologically active compounds.

    Science.gov (United States)

    Kumar, Pradeep; Dwivedi, Namrata

    2013-02-19

    The search for new and efficient ways to synthesize optically pure compounds is an active area of research in organic synthesis. Asymmetric catalysis provides a practical, cost-effective, and efficient method to create a variety of complex natural products containing multiple stereocenters. In recent years, chemists have become more interested in using small organic molecules to catalyze organic reactions. As a result, organocatalysis has emerged both as a promising strategy and as an alternative to catalysis with expensive proteins or toxic metals. One of the most successful and widely studied secondary amine-based organocatalysts is proline. This small molecule can catalyze numerous reactions such as the aldol, Mannich, Michael addition, Robinson annulation, Diels-Alder, α-functionalization, α-amination, and α-aminoxylation reactions. Catalytic and enantioselective α-oxygenation of carbonyl compounds is an important reaction to access a variety of useful building blocks for bioactive molecules. Proline catalyzed α-aminoxylation using nitrosobenzene as oxygen source, followed by in situ reduction, gives enantiomerically pure 1,2-diol. This molecule can then undergo a variety of organic reactions. In addition, proline organocatalysis provides access to an assortment of biologically active natural products including mevinoline (a cholesterol lowering drug), tetrahydrolipstatin (an antiobesity drug), R(+)-α-lipoic acid, and bovidic acid. In this Account, we present an iterative organocatalytic approach to synthesize both syn- and anti-1,3-polyols, both enantio- and stereoselectively. This method is primarily based on proline-catalyzed sequential α-aminoxylation and Horner-Wadsworth-Emmons (HWE) olefination of aldehyde to give a γ-hydroxy ester. In addition, we briefly illustrate the broad application of our recently developed strategy for 1,3-polyols, which serve as valuable, enantiopure building blocks for polyketides and other structurally diverse and

  7. Synthesis and biological activity of sulfur compounds showing structural analogy with combretastatin A-4

    Energy Technology Data Exchange (ETDEWEB)

    Santos, Edson dos A. dos; Prado, Paulo C.; Carvalho, Wanderley R. de; Lima, Ricardo V. de; Beatriz, Adilson; Lima, Denis P. de, E-mail: denis.lima@ufms.br [Universidade Federal de Mato Grosso do Sul (UFMS), Campo Grande, MS (Brazil). Departamento de Quimica; Hamel, Ernest [Screening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute at Frederick, National Institutes of Health, Frederick, MD (United States); Dyba, Marzena A. [Basic Science Program , SAIC-Frederick, Inc., Structural Biophysics Laboratory National Cancer Institute, Frederick, MD (United States); Albuquerque, Sergio [Universidade de Sao Paulo (USP), Ribeirao Preto, SP (Brazil). Faculdade de Ciencias Farmaceuticas

    2013-09-01

    We extended our previous exploration of sulfur bridges as bioisosteric replacements for atoms forming the bridge between the aromatic rings of combretastatin A-4. Employing coupling reactions between 5-iodo-1,2,3-trimethoxybenzene and substituted thiols, followed by oxidation to sulfones with m-CPBA, different locations for attaching the sulfur atom to ring A through the synthesis of nine compounds were examined. Antitubulin activity was performed with electrophoretically homogenous bovine brain tubulin, and activity occurred with the 1,2,3-trimethoxy-4-[(4-methoxyphenyl)thio]benzene (12), while the other compounds were inactive. The compounds were also tested for leishmanicidal activity using promastigote forms of Leishmania braziliensis (MHOM/BR175/M2904),and the greatest activity was observed with 1,2,3-trimethoxy-4-(phenylthio)benzene (10) and 1,2,3-trimethoxy-4-[(4-methoxyphenyl) sulfinyl]benzene (15). (author)

  8. New approaches to estimation of peat deposits for production of biologically active compounds

    Science.gov (United States)

    Stepchenko, L. M.; Yurchenko, V. I.; Krasnik, V. G.; Syedykh, N. J.

    2009-04-01

    It is known, that biologically active preparations from peat increase animals productivity as well as resistance against stress-factors and have adaptogeneous, antioxidant, immunomodulative properties. Optymal choice of peat deposits for the production of biologically active preparations supposes the detailed comparative analysis of peat properties from different deposits. For this the cadastre of peat of Ukraine is developed in the humic substances laboratory named after prof. Khristeva L.A. (Dnipropetrovsk Agrarian University, Ukraine). It based on the research of its physical and chemical properties, toxicity and biological activity, and called Biocadastre. The Biocadastre is based on the set of parameters, including the descriptions of physical and chemical properties (active acidity, degree of decomposition, botanical composition etc.), toxicity estimation (by parabyotyc, infusorial, inhibitor and other tests), biological activity indexes (growth-promoting, antioxidative, adaptogeneous, immunomodulative antistress and other actions). The blocks of Biocadastre indexes are differentiated, taking into account their use for creation the preparations for vegetable, animals and microorganisms. The Biocadastre will allow to choose the peat deposits, most suitable for the production of different biologically active preparations, both wide directed and narrow spectrum of action, depending on application fields (medicine, agriculture, veterinary medicine, microbiological industry, balneology, cosmetology).

  9. Insights from the docking analysis of biologically active compounds from plant Litsea Genus as potential COX-2 inhibitors.

    Science.gov (United States)

    Gogoi, Dhrubajyoti; Bezbaruah, Rajib Lochan; Bordoloi, Manabjyoti; Sarmah, Rajeev; Bora, Tarun Chandra

    2012-01-01

    Litsea spp of Laural family are traditionally used as herbal medicine for treating inflammation including gastroenterologia, oedema and rheumatic arthritis. Therefore, it is of interest to investigate and understand the molecular principles for such actions. Here, we have illustrated the binding of thirteen Litsea derived biologically active compounds against the inflammation associated target COX (cyclo-oxygenase) -2 enzymes. We compared the binding information of these compounds with a selected number of already known COX-2 inhibitors. The comparison reflected that some of these compounds such as linderol, catechin, 6'-hydroxy-2',3',4' - trimethoxy-chalcone and litseaone have better or equivalent binding features compared to already known inhibitory compounds namely celecoxib, acetylsalicylic acid, rofecoxib. Therefore, all these small compounds reported from plant Litsea spp were found to possess potential medicinal values with anti-inflammatory properties.

  10. Insights from the docking analysis of biologically active compounds from plant Litsea Genus as potential COX-2 inhibitors

    Science.gov (United States)

    Gogoi, Dhrubajyoti; Bezbaruah, Rajib Lochan; Bordoloi, Manabjyoti; Sarmah, Rajeev; Bora, Tarun Chandra

    2012-01-01

    Litsea spp of Laural family are traditionally used as herbal medicine for treating inflammation including gastroenterologia, oedema and rheumatic arthritis. Therefore, it is of interest to investigate and understand the molecular principles for such actions. Here, we have illustrated the binding of thirteen Litsea derived biologically active compounds against the inflammation associated target COX (cyclo-oxygenase) -2 enzymes. We compared the binding information of these compounds with a selected number of already known COX-2 inhibitors. The comparison reflected that some of these compounds such as linderol, catechin, 6'-hydroxy-2',3',4' - trimethoxy-chalcone and litseaone have better or equivalent binding features compared to already known inhibitory compounds namely celecoxib, acetylsalicylic acid, rofecoxib. Therefore, all these small compounds reported from plant Litsea spp were found to possess potential medicinal values with anti-inflammatory properties. PMID:23139590

  11. Synthesis, characterization, investigation of biological activity and theoretical studies of hydrazone compounds containing choloroacetyl group

    Science.gov (United States)

    Cukurovali, Alaaddin; Yilmaz, Engin

    2014-10-01

    In this study, three new hydrazide-hydrazone derivative compounds which contain choloroacetyl group have been synthesized and characterized. In the characterization, spectral techniques such as IR, 1H NMR, 13C NMR and UV-Vis spectroscopy techniques were used. Antibacterial effects of the synthesized compounds were investigated against Staphylococcus aureus ATCC 29213, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853. In the theoretical calculations Gaussian 09 software was used with the DFT/6-311+(d,p) basis set. Experimental X-ray analysis of compounds has not been studied. Theoretical bond lengths of synthesized compounds were compared with experimental bond lengths of a similar compound. Theoretical and experimental bond lengths are in good agreement with R2: 0.896, 0.899 and 0.900 for compounds 1, 2, and 3, respectively. For antibacterial activity, the most effective one was found to be N‧-(4-bromobenzylidene)-2-chloro-N-(4-(3-methyl-3-phenylcyclobutyl)-thiazol-2-yl) acetohydrazide against P.aeroginaosa ATTC 27853, among the studied compounds.

  12. Study of the Biological Activity of Novel Synthetic Compounds with Antiviral Properties against Human Rhinoviruses

    Directory of Open Access Journals (Sweden)

    Raffaello Pompei

    2011-04-01

    Full Text Available Picornaviridae represent a very large family of small RNA viruses, some of which are the cause of important human and animal diseases. Since no specific therapy against any of these viruses currently exists, palliative symptomatic treatments are employed. The early steps of the picornavirus replicative cycle seem to be privileged targets for some antiviral compounds like disoxaril and pirodavir. Pirodavir’s main weakness is its cytotoxicity on cell cultures at relatively low doses. In this work some original synthetic compounds were tested, in order to find less toxic compounds with an improved protection index (PI on infected cells. Using an amino group to substitute the oxygen atom in the central chain, such as that in the control molecule pirodavir, resulted in decreased activity against Rhinoviruses and Polioviruses. The presence of an -ethoxy-propoxy- group in the central chain (as in compound I-6602 resulted in decreased cell toxicity and in improved anti-Rhinovirus activity. This compound actually showed a PI >700 on HRV14, while pirodavir had a PI of 250. These results demonstrate that modification of pirodavir’s central hydrocarbon chain can lead to the production of novel derivatives with low cytotoxicity and improved PI against some strains of Rhinoviruses.

  13. Facile Synthesis and Antimicrobial Evaluation of Some New Heterocyclic Compounds Incorporating a Biologically Active Sulfamoyl Moiety

    Directory of Open Access Journals (Sweden)

    Elham S. Darwish

    2014-01-01

    Full Text Available A facile and convenient synthesis of new heterocyclic compounds containing a sulfamoyl moiety suitable for use as antimicrobial agents was reported. The precursor 3-oxo-3-phenyl-N-(4-sulfamoylphenylpropionamide was coupled smoothly with arenediazonium salt producing hydrazones which reacted with malononitrile or triethylorthoformate affording pyridazine and triazine derivatives, respectively. Also, the reactivity of the same precursor with DMF-DMA was followed by aminotriazole; aromatic aldehydes was followed by hydrazine hydrate, triethylorthoformate, or thiourea affording triazolo[1,5-a]pyrimidine, pyrazole, acrylamide, and dihydropyrimidine derivatives, respectively. On the other hand, treatment of the precursor propionamide with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt which was treated with dilute HCl followed by 2-bromo-1-phenylethanone affording carboxamide derivative. While the same intermediate salt reacted in situ with chloroacetone, ethyl 2-chloroacetate, 3-(2-bromoacetyl-2H-chromen-2-one, methyl iodide, or 2-oxo-N-phenylpropane hydrazonoyl chloride afforded the thiophene, ketene N,S-acetal, and thiadiazole derivatives, respectively. The structure of the new products was established based on elemental and spectral analysis. Antimicrobial evaluation of some selected examples from the synthesized products was carried out whereby four compounds were found to have moderate activities and one compound showed the highest activity.

  14. Three new triterpenes from Nerium oleander and biological activity of the isolated compounds.

    Science.gov (United States)

    Fu, Liwei; Zhang, Shujun; Li, Na; Wang, Jinlan; Zhao, Ming; Sakai, Junichi; Hasegawa, Toshiaki; Mitsui, Tomokazu; Kataoka, Takao; Oka, Seiko; Kiuchi, Miwa; Hirose, Katutoshi; Ando, Masayoshi

    2005-02-01

    New ursane-type triterpene 1, oleanane-type triterpene 2, and dammarane-type triterpene 15 were isolated from the leaves of Nerium oleander together with 12 known triterpenes, 3beta-hydroxy-12-ursen-28-oic acid (ursolic acid, 3), 3beta,27-dihydroxy-12-ursen-28-oic acid (4), 3beta,13beta-dihydroxyurs-11-en-28-oic acid (5), 3beta-hydroxyurs-12-en-28-aldehyde (6), 28-norurs-12-en-3beta-ol (7), urs-12-en-3beta-ol (8), urs-12-ene-3beta,28-diol (9), 3beta-hydroxy-12-oleanen-28-oic acid (oleanolic acid, 10), 3beta,27-dihydroxy-12-oleanen-28-oic acid (11), 3beta-hydroxy-20(29)-lupen-28-oic acid (betulinic acid, 12), 20(29)-lupene-3beta,28-diol (betulin, 13), and (20S,24R)-epoxydammarane-3beta,25-diol (14). On the basis of their spectroscopic data, the structures of the new compounds 1, 2, and 15 were established as 3beta,20alpha-dihydroxyurs-21-en-28-oic acid, 3beta,12alpha-dihydroxyoleanan-28,13beta-olide, and (20S,24S)-epoxydammarane-3beta,25-diol, respectively. The anti-inflammatory activity of the seven isolated compounds and methyl esters of ursolic acid and oleanoic acid in vitro was examined on the basis of inhibitory activity against the induction of the intercellular adhesion molecule-1 (ICAM-1). The anticancer activity of the 14 isolated compounds, including 1, 2, 15, and methyl esters of ursolic acid and oleanolic acid in vitro was examined on the basis of the cell growth inhibitory activities toward three kinds of human cell lines.

  15. Cu(II AND Zn(II COMPLEX COMPOUNDS WITH BIGUANIDES AROMATIC DERIVATIVES. SYNTHESIS, CHARACTERIZATION, BIOLOGICAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    Ticuţa Negreanu-Pîrjol

    2011-05-01

    Full Text Available In this paper we report the synthesis, physical-chemical characterization and antimicrobial activity of some new complex compounds of hetero-aromatic biguanides ligands, chlorhexidine base (CHX and chlorhexidine diacetate (CHXac2 with metallic ions Cu(II and Zn(II, in different molar ratio. The synthesized complexes were characterized by elemental chemical analysis and differential thermal analysis. The stereochemistry of the metallic ions was determined by infrared spectra, UV-Vis, EPR spectroscopy and magnetic susceptibility in the aim to establish the complexes structures. The biological activity of the new complex compounds was identified in solid technique by measuring minimum inhibition diameter of bacterial and fungal culture, against three standard pathogen strains, Escherichia coli ATCC 25922, Staphilococcus aureus ATCC 25923 and Candida albicans ATCC 10231. The results show an increased specific antimicrobial activity for the complexes chlorhexidine:Cu(II 1:1 and 1:2 compared with the one of the Zn(II complexes.

  16. Elevated temperature altered photosynthetic products in wheat seedlings and organic compounds and biological activity in rhizopshere soil under cadmium stress

    Science.gov (United States)

    Jia, Xia; Zhao, Yonghua; Wang, Wenke; He, Yunhua

    2015-09-01

    The objective of this study was to investigate the effects of slightly elevated atmospheric temperature in the spring on photosynthetic products in wheat seedlings and on organic compounds and biological activity in rhizosphere soil under cadmium (Cd) stress. Elevated temperature was associated with increased soluble sugars, reducing sugars, starch, and total sugars, and with decreased amino acids in wheat seedlings under Cd stress. Elevated temperature improved total soluble sugars, free amino acids, soluble phenolic acids, and organic acids in rhizosphere soil under Cd stress. The activity of amylase, phenol oxidase, invertase, β-glucosidase, and L-asparaginase in rhizosphere soil was significantly improved by elevated temperature under Cd stress; while cellulase, neutral phosphatase, and urease activity significantly decreased. Elevated temperature significantly improved bacteria, fungi, actinomycetes, and total microorganisms abundance and fluorescein diacetate activity under Cd stress. In conclusion, slightly elevated atmospheric temperature in the spring improved the carbohydrate levels in wheat seedlings and organic compounds and biological activity in rhizosphere soil under Cd stress in the short term. In addition, elevated atmospheric temperature in the spring stimulated available Cd by affecting pH, DOC, phenolic acids, and organic acids in rhizosphere soil, which resulted in the improvement of the Cd uptake by wheat seedlings.

  17. Correlation between the structure and biological activity studies of supramolecular coordination azodye compounds

    Directory of Open Access Journals (Sweden)

    M.I. Abou-Dobara

    2017-02-01

    Full Text Available A series of novel bidentate azodye quinoline ligands were synthesized with various p-aromatic amines like p-(OCH3, CH3, H, Cl and NO2. Novel azodye (HLn and complexes [Cu(II/Ni(II] of these ligands have been characterized on the basis of elemental analysis, molar conductance and magnetic measurements, infrared and electronic spectral studies. Suitable structures have been proposed for these complexes. The synthesized ligands and their metal complexes were screened for their antimicrobial activity against four local bacterial species, two Gram positive bacteria (Bacillus cereus and Staphylococcus aureus and two Gram negative bacteria (Escherichia coli and Klebsiella pneumoniae as well as against four local fungal species; namely Aspergillus niger, Alternaria alternata, Penicillium italicum and Fusarium oxysporium. The tested compounds have good antibacterial activity against B. cereus, E. coli and K. pneumoniae. Very low effect was detected against S. aureus and F. oxysporium. We found that the results of antifungal activity of HLn revealed that the complexes are more toxic than ligands against fungi due to the transition metal involved in the coordination. Also Cu2+ complexes are more active than Ni2+ complexes against B. cereus, E. coli and K. pneumoniae. The size of the clear zone was in the following order p-(OCH3 < CH3 < H < Cl < NO2 as expected from Hammett’s constants σR.

  18. The doping effect of fluorinated aromatic hydrocarbon solvents on the performance of common olefin metathesis catalysts: application in the preparation of biologically active compounds.

    Science.gov (United States)

    Samojłowicz, Cezary; Bieniek, Michał; Zarecki, Andrzej; Kadyrov, Renat; Grela, Karol

    2008-12-21

    Aromatic fluorinated hydrocarbons, used as solvents for olefin metathesis reactions, catalysed by standard commercially available Ru precatalysts, allow substantially higher yields to be obtained, especially of challenging substrates, including natural and biologically active compounds.

  19. Occurrence of Endocrine Active Compounds and Biological Responses in the Mississippi River - Study Design and Data, June through August 2006

    Science.gov (United States)

    Lee, Kathy E.; Yaeger, Christine S.; Jahns, Nathan D.; Schoenfuss, Heiko L.

    2008-01-01

    Concern that selected chemicals in the environment may act as endocrine active compounds in aquatic ecosystems is widespread; however, few studies have examined the occurrence of endocrine active compounds and identified biological markers of endocrine disruption such as intersex occurrence in fish longitudinally in a river system. This report presents environmental data collected and analyzed by the U.S. Geological Survey, Minnesota Pollution Control Agency and St. Cloud State University as part of an integrated biological and chemical study of endocrine disruption in fish in the Mississippi River. Data were collected from water, bed sediment, and fish at 43 sites along the river from the headwaters at Lake Itasca to 14 miles downstream from Brownsville, Minnesota during June through August 2006. Twenty-four individual compounds were detected in water samples, with cholesterol, atrazine, N,N-diethyl-meta-toluamide, metolachlor, and hexahydrohexamethylcyclopentabenzopyran detected most frequently (in at least 10 percent of the samples). The number of compounds detected in water per site ranged from 0 to 8. Forty individual compounds were detected in bed-sediment samples. The most commonly detected compounds (in at least 50 percent of the samples) were indole, beta-sitosterol, cholesterol, beta-stigmastanol, 3-methyl-1H-indole, p-cresol, pyrene, phenol, fluoranthene, 3-beta coprostanol, benzo[a]pyrene, acetophenone, and 2,6-dimethylnaphthalene. The total number of detections in bed sediment (at a site) ranged from 3 to 31. The compounds NP1EO, NP2EO, and 4-nonylphenol were detected in greater than 10 percent of the samples. Most (80 percent) female fish collected had measurable concentrations of vitellogenin. Vitellogenin also was detected in 62, 63, and 33 percent of male carp, smallmouth bass, and redhorse, respectively. The one male walleye sample plasma sample analyzed had a vitellogenin detection. Vitellogenin concentrations were lower in male fish (not

  20. Palladium- and copper-mediated N-aryl bond formation reactions for the synthesis of biological active compounds

    Directory of Open Access Journals (Sweden)

    Burkhard Koenig

    2011-01-01

    Full Text Available N-Arylated aliphatic and aromatic amines are important substituents in many biologically active compounds. In the last few years, transition-metal-mediated N-aryl bond formation has become a standard procedure for the introduction of amines into aromatic systems. While N-arylation of simple aromatic halides by simple amines works with many of the described methods in high yield, the reactions may require detailed optimization if applied to the synthesis of complex molecules with additional functional groups, such as natural products or drugs. We discuss and compare in this review the three main N-arylation methods in their application to the synthesis of biologically active compounds: Palladium-catalysed Buchwald–Hartwig-type reactions, copper-mediated Ullmann-type and Chan–Lam-type N-arylation reactions. The discussed examples show that palladium-catalysed reactions are favoured for large-scale applications and tolerate sterically demanding substituents on the coupling partners better than Chan–Lam reactions. Chan–Lam N-arylations are particularly mild and do not require additional ligands, which facilitates the work-up. However, reaction times can be very long. Ullmann- and Buchwald–Hartwig-type methods have been used in intramolecular reactions, giving access to complex ring structures. All three N-arylation methods have specific advantages and disadvantages that should be considered when selecting the reaction conditions for a desired C–N bond formation in the course of a total synthesis or drug synthesis.

  1. Chemical characterization and evaluation of biological activity of Cynara cardunculus extractable compounds

    OpenAIRE

    Ramos, Patrícia Alexandra Bogango

    2015-01-01

    The Mediterranean species Cynara cardunculus L. is recognized in the traditional medicine, for their hepatoprotective and choleretic effects. Biomass of C. cardunculus L. var. altilis (DC), or cultivated cardoon, may be explored not only for the production of energy and pulp fibers, but also for the extraction of bioactive compounds. The chemical characterization of extractable components, namely terpenic and phenolic compounds, may valorize the cultivated cardoon plantation, due to their ant...

  2. 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......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...

  3. 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;

    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...... and researchers interested in diet and health relationships, and product developers within the food industry....

  4. Monotherapy and combined therapy of new potential antitumor compounds: antiproliferative activities and biological targets

    OpenAIRE

    Marques, Mara Lisa Miranda

    2014-01-01

    Review article Martins, P., Marques, M., Coito, L., Pombeiro, A.J.L., Baptista, P.V., Fernandes, A.R. 2014. Organometallic Compounds in Cancer Therapy: Past Lessons and Future Directions. Anti-cancer Agents in Medicinal Chemistry 14. PMID: 25173559

  5. Novel Data Mining Methods for Virtual Screening of Biological Active Chemical Compounds

    KAUST Repository

    Soufan, Othman M.

    2016-11-23

    Drug discovery is a process that takes many years and hundreds of millions of dollars to reveal a confident conclusion about a specific treatment. Part of this sophisticated process is based on preliminary investigations to suggest a set of chemical compounds as candidate drugs for the treatment. Computational resources have been playing a significant role in this part through a step known as virtual screening. From a data mining perspective, availability of rich data resources is key in training prediction models. Yet, the difficulties imposed by big expansion in data and its dimensionality are inevitable. In this thesis, I address the main challenges that come when data mining techniques are used for virtual screening. In order to achieve an efficient virtual screening using data mining, I start by addressing the problem of feature selection and provide analysis of best ways to describe a chemical compound for an enhanced screening performance. High-throughput screening (HTS) assays data used for virtual screening are characterized by a great class imbalance. To handle this problem of class imbalance, I suggest using a novel algorithm called DRAMOTE to narrow down promising candidate chemicals aimed at interaction with specific molecular targets before they are experimentally evaluated. Existing works are mostly proposed for small-scale virtual screening based on making use of few thousands of interactions. Thus, I propose enabling large-scale (or big) virtual screening through learning millions of interaction while exploiting any relevant dependency for a better accuracy. A novel solution called DRABAL that incorporates structure learning of a Bayesian Network as a step to model dependency between the HTS assays, is showed to achieve significant improvements over existing state-of-the-art approaches.

  6. Biological Activities of Hydrazone Derivatives

    Directory of Open Access Journals (Sweden)

    S. Güniz Küçükgüzel

    2007-08-01

    Full Text Available There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, vasodilator, antiviral and antischistosomiasis activities. Hydrazones possessing an azometine -NHN=CH- proton constitute an important class of compounds for new drug development. Therefore, many researchers have synthesized these compounds as target structures and evaluated their biological activities. These observations have been guiding for the development of new hydrazones that possess varied biological activities.

  7. Synthesis, Structure and Biological Activities of Novel Triazole Compounds Containing 4,6-Dimethyl-pyrimidin-2-ylthio Group

    Institute of Scientific and Technical Information of China (English)

    XU, Liang-Zhong(许良忠); JIAN, Fang-Fang(建方方); SHI, Jian-Gang(时建刚); LI, Lin(李琳)

    2004-01-01

    Four compounds were prepared by reacting 4,6-dimethyl-2-mercaptopyrimidine with α-bromo-α-(1,2,4-triazol-1-yl)-substituted acetylbenzene. Their structures were identified by means of elemental analysis, IR, and 1H NMR spectra. The single crystal structure of 2- [ 1 -(1,2,4-triazol- 1-yl)- 1-p-methoxyphenylcarbonylmethylthio] -4,6-dimethyl-pyrimidine was also determined. It crystallizes in monoclinic system, space group P21/c, a=0.8016(2) nm, b=1.2462(3) nm, c= 1.7824(4) nm,β=99.89(3)°, Z=4, V=1.7540(7) nm3, Dc=1.346 g/cm3, μ=0.205 mm-1, F(000)=744, final R1=0.0452. There is obviously potentially weak C-H…N intermolecular interaction between the molecules in the crystal lattice, which stabilizes the crystal structure. The result of the biological test showed that the four compounds all have some fungicidal and plant growth regulating activities.

  8. Synthesis and biological activities of 2,6-dihydroxy-4-isopentenyloxychalcone as an antimicrobial and anti-inflammatory compound.

    Science.gov (United States)

    Bonifait, Laetitia; Zhao, Lei; Azelmat, Jabrane; Genovese, Salvatore; Epifano, Francesco; Grenier, Daniel

    2014-05-01

    Chalcones are a group of plant-derived polyphenolic compounds possessing a wide variety of biological activities. The aim of this study was to synthesize 2,6-dihydroxy-4-isopentenyloxychalcone (1), a chalcone found in plants belonging to the genera Helichrysum, Pleiotaxix and Metalasia, and evaluate its antimicrobial effects against major oral pathogens as well as its anti-inflammatory properties. Compound 1 was synthesized using a simple two-step procedure. Among the seven pathogens tested, Porphyromonas gingivalis and Prevotella intermedia were the most susceptible to inhibition by 1. This chalcone also attenuated the secretion of interleukin-8 and chemokine (C-C motif) ligand 5 (CCL5) by lipopolysaccharide (LPS)-stimulated oral epithelial cells as well as the secretion of matrix metalloproteinase 2 (MMP-2) by LPS-stimulated gingival fibroblasts. In conclusion, our study showed that 1 exerts a dual effect by acting on both oral pathogens and the host inflammatory response and thus represents a molecule of interest for periodontal infections.

  9. New bimetallic dicyanidoargentate(I)-based coordination compounds: Synthesis, characterization, biological activities and DNA-BSA binding affinities

    Science.gov (United States)

    Korkmaz, Nesrin; Aydın, Ali; Karadağ, Ahmet; Yanar, Yusuf; Maaşoğlu, Yelis; Şahin, Ertan; Tekin, Şaban

    2017-02-01

    Four compounds -two (2 and 3) completely new- of composition [Ni(edbea)Ag3(CN)5] (1), [Cu(edbea)Ag2(CN)4]·H2O (2), [Cd(edbea)Ag3(CN)5]·H2O (3) and [Cd(edbea)2] [Ag(CN)2]2·H2O (4) {edbea; 2,2‧-(ethylenedioxy)bis (ethylamine)}, were synthesized and characterized using elemental, FT-IR, X-Ray (4), thermal, variable temperature magnetic measurement (1 and 2) and biological techniques. The DNA/BSA binding affinities of 2 and 3 were evaluated by UV-Vis spectrophotometric titrations, ethidium bromide exchange experiments and electrophoretic mobility measurements. Compounds 1 and 4 have previously been characterized and shown to reduce the proliferation and migration of tumor cells. For the sake of clarity, 1 precise mechanism of action on microbial organisms and temperature magnetic measurement were determined. The crystallographic analyses showed that 4 was built up of [Cd(edbea)2]II cations and [Ag2(CN)4]II anions. Complexes demonstrated a remarkable antibacterial (1-4), antifungal (1-4) and antiproliferative activities (2 and 3) to ten human bacterial pathogens, four plant pathogenic fungi or three tumor cells (HeLa, HT29, and C6), respectively. Therefore, our results strongly confirm that cell proliferation, cell morphology, Bcl-2, P53 changes and apoptosis can be related to the pharmacological effects of the complexes as suitable candidate for clinical trials.

  10. Chemical composition, biological and cytotoxic activities of plant extracts and compounds isolated from Ferula lutea.

    Science.gov (United States)

    Znati, Mansour; Hichem, Ben Jannet; Cazaux, Sylvie; Bouajila, Jalloul

    2014-02-26

    The present work describes the phytochemical study on Ferula lutea flowers. Total phenolics and flavonoids of the n-butanol and ethyl acetate extracts were quantified (phenolics [40.68-52.29 mg gallic acid equivalent/g of dry weight], flavonoids [12.38-14.72 mg quercitin/g dry weight]). Two diastereoisomers were isolated and identified using spectroscopic techniques (1D, 2D NMR and GC-MS). The extracts and diastereoisomers were tested for antioxidant, antiacetylcholinesterase, antimicrobial, antidiabectic, cytotoxic (leukemia cell line) activities and allelopathic potentialities. The strongest antioxidant activity was obtained for the ethyl acetate extract (IC₅₀ = 12.8 ± 1.29 µg/mL). The two extracts exhibited high antidiabetic activity (54.1 and 52.1% at 40 µg/mL).

  11. Chemical Composition, Biological and Cytotoxic Activities of Plant Extracts and Compounds Isolated from Ferula lutea

    Directory of Open Access Journals (Sweden)

    Mansour Znati

    2014-02-01

    Full Text Available The present work describes the phytochemical study on Ferula lutea flowers. Total phenolics and flavonoids of the n-butanol and ethyl acetate extracts were quantified (phenolics [40.68–52.29 mg gallic acid equivalent/g of dry weight], flavonoids [12.38–14.72 mg quercitin/g dry weight]. Two diastereoisomers were isolated and identified using spectroscopic techniques (1D, 2D NMR and GC-MS. The extracts and diastereoisomers were tested for antioxidant, antiacetylcholinesterase, antimicrobial, antidiabectic, cytotoxic (leukemia cell line activities and allelopathic potentialities. The strongest antioxidant activity was obtained for the ethyl acetate extract (IC50 = 12.8 ± 1.29 µg/mL. The two extracts exhibited high antidiabetic activity (54.1 and 52.1% at 40 µg/mL.

  12. Effect of storage conditions on the biological activity of phenolic compounds of blueberry extract packed in glass bottles.

    Science.gov (United States)

    Srivastava, Anita; Akoh, Casimir C; Yi, Weiguang; Fischer, Joan; Krewer, Gerard

    2007-04-04

    Recent research suggests that blueberries are rich in total polyphenols and total anthocyanins. Phenolic compounds are highly unstable and may be lost during processing, particularly when heat treatment is involved. There is no systematic study available providing information on the fate of phenolic compounds during storage and how that affects their biological activity. We provide a systematic evaluation of the changes observed in total polyphenols (TPP), total anthocyanins (TACY), Trolox equivalent antioxidant capacity (TEAC), phenolic acids, and individual anthocyanins of blueberry extract stored in glass bottles and the ability of blueberry extract to inhibit cell proliferation. The extract was stored at different temperatures (-20 +/- 1, 6 +/- 1, 23 +/- 1, and 35 +/- 1 degrees C). Two cultivars, Tifblue and Powderblue, were chosen for the study. The recoveries of TPP, TACY, and TEAC in blueberry extract after pressing and heating were approximately 25, approximately 29, and approximately 69%, respectively, for both cultivars. The recovery of gallic acid, catechin, and quercetin was approximately 25%. Ferulic acid was not detected in the final extract in both Tifblue and Powderblue cultivars. The recovery of peonidin, malvidin, and cyanidin glycosides was approximately 20% in the final extract in both cultivars. Losses due to storage were less when compared with initial losses due to processing. At -20 degrees C, no statistically significant loss of TPP, TACY, and TEAC was observed up to 30 days (P glass bottles for Tifblue and Powderblue, respectively, when compared with other individual anthocyanins. A linear relationship was observed between TEAC values and total polyphenols or total anthocyanins. A cell viability assay was performed using HT-29 cancer cell lines and anthocyanins extracted from 30, 60, and 90 days of stored extract at 6 +/- 1 and 23 +/- 1 degrees C. A significant cell proliferation inhibition percentage was observed in 30 days, although this

  13. Pinocembrin: a novel natural compound with versatile pharmacological and biological activities.

    Science.gov (United States)

    Rasul, Azhar; Millimouno, Faya Martin; Ali Eltayb, Wafa; Ali, Muhammad; Li, Jiang; Li, Xiaomeng

    2013-01-01

    Pinocembrin (5,7-dihydroxyflavanone) is one of the primary flavonoids isolated from the variety of plants, mainly from Pinus heartwood, Eucalyptus, Populus, Euphorbia, and Sparattosperma leucanthum, in the diverse flora and purified by various chromatographic techniques. Pinocembrin is a major flavonoid molecule incorporated as multifunctional in the pharmaceutical industry. Its vast range of pharmacological activities has been well researched including antimicrobial, anti-inflammatory, antioxidant, and anticancer activities. In addition, pinocembrin can be used as neuroprotective against cerebral ischemic injury with a wide therapeutic time window, which may be attributed to its antiexcitotoxic effects. Pinocembrin exhibits pharmacological effects on almost all systems, and our aim is to review the pharmacological and therapeutic applications of pinocembrin with specific emphasis on mechanisms of actions. The design of new drugs based on the pharmacological effects of pinocembrin could be beneficial. This review suggests that pinocembrin is a potentially promising pharmacological candidate, but additional studies and clinical trials are required to determine its specific intracellular sites of action and derivative targets in order to fully understand the mechanism of its anti-inflammatory, anticancer, and apoptotic effects to further validate its medical applications.

  14. Pinocembrin: A Novel Natural Compound with Versatile Pharmacological and Biological Activities

    Directory of Open Access Journals (Sweden)

    Azhar Rasul

    2013-01-01

    Full Text Available Pinocembrin (5,7-dihydroxyflavanone is one of the primary flavonoids isolated from the variety of plants, mainly from Pinus heartwood, Eucalyptus, Populus, Euphorbia, and Sparattosperma leucanthum, in the diverse flora and purified by various chromatographic techniques. Pinocembrin is a major flavonoid molecule incorporated as multifunctional in the pharmaceutical industry. Its vast range of pharmacological activities has been well researched including antimicrobial, anti-inflammatory, antioxidant, and anticancer activities. In addition, pinocembrin can be used as neuroprotective against cerebral ischemic injury with a wide therapeutic time window, which may be attributed to its antiexcitotoxic effects. Pinocembrin exhibits pharmacological effects on almost all systems, and our aim is to review the pharmacological and therapeutic applications of pinocembrin with specific emphasis on mechanisms of actions. The design of new drugs based on the pharmacological effects of pinocembrin could be beneficial. This review suggests that pinocembrin is a potentially promising pharmacological candidate, but additional studies and clinical trials are required to determine its specific intracellular sites of action and derivative targets in order to fully understand the mechanism of its anti-inflammatory, anticancer, and apoptotic effects to further validate its medical applications.

  15. Exploring the DNA binding mode of transition metal based biologically active compounds

    Science.gov (United States)

    Raman, N.; Sobha, S.

    2012-01-01

    Few novel 4-aminoantipyrine derived Schiff bases and their metal complexes were synthesized and characterized. Their structural features and other properties were deduced from the elemental analysis, magnetic susceptibility and molar conductivity as well as from mass, IR, UV-vis, 1H NMR and EPR spectral studies. The binding of the complexes with CT-DNA was analyzed by electronic absorption spectroscopy, viscosity measurement, and cyclic voltammetry. The interaction of the metal complexes with DNA was also studied by molecular modeling with special reference to docking. The experimental and docking results revealed that the complexes have the ability of interaction with DNA of minor groove binding mode. The intrinsic binding constants ( Kb) of the complexes with CT-DNA were found out which show that they are minor groove binders. Gel electrophoresis assay demonstrated the ability of the complexes to cleave the pUC19 DNA in the presence of AH 2 (ascorbic acid). Moreover, the oxidative cleavage studies using distamycin revealed the minor groove binding for the newly synthesized 4-aminoantipyrine derived Schiff bases and their metal complexes. Evaluation of antibacterial activity of the complexes against Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus epidermidis, and Klebsiella pneumoniae exhibited that the complexes have potent biocidal activity than the free ligands.

  16. Biological and Pharmacological Activities of Squalene and Related Compounds: Potential Uses in Cosmetic Dermatology

    Directory of Open Access Journals (Sweden)

    Jia-You Fang

    2009-01-01

    Full Text Available Squalene is a triterpene that is an intermediate in the cholesterol biosynthesis pathway. It was so named because of its occurrence in shark liver oil, which contains large quantities and is considered its richest source. However, it is widely distributed in nature, with reasonable amounts found in olive oil, palm oil, wheat-germ oil, amaranth oil, and rice bran oil. Squalene, the main component of skin surface polyunsaturated lipids, shows some advantages for the skin as an emollient and antioxidant, and for hydration and its antitumor activities. It is also used as a material in topically applied vehicles such as lipid emulsions and nanostructured lipid carriers (NLCs. Substances related to squalene, including β-carotene, coenzyme Q10 (ubiquinone and vitamins A, E, and K, are also included in this review article to introduce their benefits to skin physiology. We summarize investigations performed in previous reports from both in vitro and in vivo models.

  17. Bioactive Compounds and Biological Activities of Jatropha curcas L. Kernel Meal Extract

    Directory of Open Access Journals (Sweden)

    Abdul Rahman Omar

    2011-09-01

    Full Text Available Defatted Jatropha curcas L. (J. curcas seed kernels contained a high percentage of crude protein (61.8% and relatively little acid detergent fiber (4.8% and neutral detergent fiber (9.7%. Spectrophotometric analysis of the methanolic extract showed the presence of phenolics, flavonoids and saponins with values of 3.9, 0.4 and 19.0 mg/g DM, respectively. High performance liquid chromatography (HPLC analyses showed the presence of gallic acid and pyrogallol (phenolics, rutin and myricetin (flavonoids and daidzein (isoflavonoid. The amount of phorbol esters in the methanolic extract estimated by HPLC was 3.0 ± 0.1 mg/g DM. Other metabolites detected by GC-MS include: 2-(hydroxymethyl-2 nitro-1,3-propanediol, β-sitosterol, 2-furancarboxaldehyde, 5-(hydroxymethy and acetic acid in the methanolic extract; 2-furancarboxaldehyde, 5-(hydroxymethy, acetic acid and furfural (2-furancarboxaldehyde in the hot water extract. Methanolic and hot water extracts of kernel meal showed antimicrobial activity against both Gram positive and Gram negative pathogenic bacteria (inhibition range: 0–1.63 cm at the concentrations of 1 and 1.5 mg/disc. Methanolic extract exhibited antioxidant activities that are higher than hot water extract and comparable to β-carotene. The extracts tended to scavenge the free radicals in the reduction of ferric ion (Fe3+ to ferrous ion (Fe2+. Cytotoxicity assay results indicated the potential of methanolic extract as a source of anticancer therapeutic agents toward breast cancer cells.

  18. Syntheses of biologically active natural products and leading compounds for new pharmaceuticals employing effective construction of a polycyclic skeleton.

    Science.gov (United States)

    Ihara, Masataka

    2006-06-01

    Cascade reactions are useful methods for the construction of polycyclic skeletons, which are important cores for biological activities. A variety of cascade reactions carried out under multiple reaction conditions, such as pericyclic, polar, radical, and transition metal-catalyzed reaction conditions, have been investigated. Culmorin, pentalenene, pentalenic acid, deoxypentalenic acid, longiborneol, cedrandiol, 8,14-cedranoxide, atisirene, atisine, and estrane-type steroids were synthesized via the intramolecular double Michael reaction. Aza double Michael reaction was applied to the syntheses of tylophorine, epilupinine, tacamonine, and paroxetine. Furthermore, sequential Michael and aldol reactions were performed in both intramolecular and intermolecular manners, leading to the formation of polycyclic compounds fused to a four-membered ring. Synthesis of paesslerin A utilizing a multicomponent cascade reaction revealed an error in the proposed structure. Unique cascade reactions carried out under radical and transition metal-catalyzed reaction conditions were also investigated. With the combination of several cascade reactions, serofendic acids and methyl 7beta-hydroxykaurenoate, both of which have neuroprotective activity, were synthesized in a selective manner.

  19. Polyketide and benzopyran compounds of an endophytic fungus isolated from Cinnamomum mollissimum:biological activity and structure

    Institute of Scientific and Technical Information of China (English)

    Carolina Santiago; Lin Sun; Murray Herbert Gibson Munro; Jacinta Santhanam

    2014-01-01

    Objective:To study bioactivity and compounds produced by an endophytic Phoma sp. fungus isolated from the medicinal plant Cinnamomum mollissimum. Methods: Compounds produced by the fungus were extracted from fungal broth culture with ethyl acetate. This was followed by bioactivity profiling of the crude extract fractions obtained via high performance liquid chromatography. The fractions were tested for cytotoxicity to P388 murine leukemic cells and antimicrobial activity against bacteria and pathogenic fungi. Compounds purified from active fractions which showed antibacterial, antifungal and cytotoxic activities were identified using capillary nuclear magnetic resonance analysis, mass spectrometry and admission to AntiMarin database. Results: Three known compounds, namely 4-hydroxymellein, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one and 1-(2,6-dihydroxyphenyl) ethanone, were isolated from the fungus. The polyketide compound 4-hydroxymellein showed high inhibitory activity against P388 murine leukemic cells (94.6%) and the bacteria Bacillus subtilis (97.3%). Meanwhile, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one, a benzopyran compound, demonstrated moderate inhibitory activity against P388 murine leukemic cells (48.8%) and the fungus Aspergillus niger (56.1%). The second polyketide compound, 1 (2,6-dihydroxyphenyl) ethanone was inactive against the tested targets. Conclusions: These findings demonstrate the potential of endophytes as producers of pharmacologically important compounds, including polyketides which are major secondary metabolites in fungi.

  20. polyketide and benzopyran compounds of an endophytic fungus isolated from Cinnamomum mollissimum:biological activity and structure

    Institute of Scientific and Technical Information of China (English)

    Carolina; Santiago; Lin; Sun; Murray; Herbert; Gibson; Munro; Jacinta; Santhanam

    2014-01-01

    Objective:To study bioactivity and compounds produced by an endophytic Phoma sp.fungus isolated from the medicinal plant Cinnamomum mollissimum.Methods:Compounds produced by the fungus were extracted from fungal broth culture with ethyl acetate.This was followed by hioaclivity profiling of the crude extract fractions obtained via high performance liquid chromatography.The fractions were tested for cytotoxicity to P388 murine leukemic cells and antimicrobial activity against bacteria and pathogenic fungi.Compounds purified from active fractions which showed antibacterial,antifungal and cytotoxic activities were identified using capillary nuclear magnetic resonance analysis,mass spectrometry and admission to AntiMarin database.Results:Three known compounds,namely 4—hydroxymellein,4,8—dihydroxy—6—melhoxy—3—methyl—3,4-dihydro—1H-isochromen-1—one and 1—(2,6-dihydroxyphenyl) ethanone,were isolated from the fungus.The polyketide compound 4—hydroxymellein showed high inhibitory activity against P388 murine leukemic cells(94.6%) and the bacteria Bacillus sublilis(97.3%).Meanwhile.4,8—dihydroxy-6—melhoxy—3—meth) 1—3,4-dihydro—1H—isochromen—1-one,a benzopyran compound,demonstrated moderate inhibitory activity against P388 murine leukemic cells(48.8%)and the fungus Aspergillus niger(56.1%).The second polyketide compound.1(2,6—dihydroxyphenyl)ethanone was inactive against the tested targets.Conclusions:These findings demonstrate the potential of endophytes as producers ol pharmacologically important compounds,including polyketides which are major secondary metabolites in fungi.

  1. Studies on Synthesis and Biological Activities of Novel Triazole Compounds Containing Pyrimidine or N,N-Dialkyldithiocarbamate Ring

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; ZHANG Shu-sheng; GAO Hong-rong; JIAO Kui

    2003-01-01

    Twelve of the title compounds were synthesized. Their structures were identified by means of IR, EA, 1H NMR and MS. The IR spectra clearly show that the absorptions in the regions of 1716-1666 cm-1 and 1505-1499 cm-1 are the characteristic absorption bands for νC=O and νC=N. In the 1H NMR spectra of target compounds(10a-10g), three protons of a CH-CH2- group present three sets of quartet peaks of the protons. The preliminary bioassays showed that the synthesized compounds exhibited some activities of fungicides and plant growth regulators.

  2. [Preparations and biological properties of chiral compounds].

    Science.gov (United States)

    Sinko, Goran

    2005-12-01

    Enantiomers of chiral compounds may express various biological activities and also different toxicities. Examples of different pharmacological effects of some chiral drugs such as fluoxetine, penicillamine, ibuprofen and albuterol are provided in this paper. Due to possible differences in activity, the chiral drugs are required to be pure enantiomeric compounds in order to be more effective and safer to use. In the laboratory, enantiomers are mainly synthesized as racemates (an equimolar mixture of enantiomers) while in biological pathways only one enantiomeric form is produced, such as amino acids, sugars and lipids. This paper presents the principles of chirality, general information about enantiomers and their biological aspects. It gives an outline of stereoselective methods for chromatographic resolution of enantiomers with stereoselective protein stationary phases, i.e. capillary electrochromatography (CEC) and high performance liquid chromatography (HPLC). The use of enzyme biotransformations (hydrolysis, oxidation and reduction) in chiral syntheses of carboxyl-, phosphoryl- or beta-hydroxy esters, alcohols, epoxides and cis-carboxyl sulphoxide is described. This article also includes an example of lipase stereoselectivity improvement by amino acid mutations within the enzyme active site.

  3. Potential antifertility agents. 6. Synthesis and biological activities of optical isomers of 4 beta-(p-methozyphenyl)-2 beta-methylcyclohexane-alpha-carboxylic acid and related compounds.

    Science.gov (United States)

    Crenshaw, R R; Jenks, T A; Luke, G M; Bialy, G

    1974-12-01

    The optical isomers of the title compound were synthesized and the biological potencies of the two enantiomers were compared. There was essentially no difference in their hypocholesterolemic activities, as had been predicted, and little or no difference between their uterotropic potencies. The approximately equal uterotropic activities seen with the enantiomers is explained in terms of stereochemical requirements at the receptor level for an estrogenic response. A working model of an estrogenic receptor is proposed. An accompanying paper provides support for the proposed model.

  4. A REVIEW: BIOLOGICAL SIGNIFICANCES OF HETEROCYCLIC COMPOUNDS.

    Directory of Open Access Journals (Sweden)

    Mukhtyar. S. Saini

    2013-03-01

    Full Text Available Heterocyclic chemistry offers an example for the lack of distinct demarcations; in fact, it pervades the plurality of the other chemical disciplines. Heterocycles are inextricably woven into the life processes. The vital interest of the pharmaceutical and agrochemical industries in heterocycles is often connected with their natural occurrence. Synthetic chemistry provides cornucopia of heterocyclic systems. More than 90% of new drugs contain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery and application is taking place is crossed by heterocyclic compounds. This review article covers the most active heterocycles that have shown considerable biological actions as antifungal, anti-inflammatory, antibacterial, anticonvulsant, antiallergic, herbicidal, anticancer activity

  5. Extracts of Agrimonia eupatoria L. as sources of biologically active compounds and evaluation of their antioxidant, antimicrobial, and antibiofilm activities

    Directory of Open Access Journals (Sweden)

    Mirjana Ž. Muruzović

    2016-07-01

    Full Text Available In this study, we determined the concentration of total phenols, flavonoids, tannins, and proanthocyanidins in the water, diethyl ether, acetone, and ethanol extracts of Agrimonia eupatoria L. We also investigated the antioxidant activity of these extracts using two methods [2,2-diphenyl-1-picrylhydrazyl (DPPH and reducing power] and their in vitro antimicrobial (antibacterial and antifungal activity on some selected species of bacteria and fungi. In addition, the effects of the acetone and water extracts on the inhibition of biofilm formation of Proteus mirabilis and Pseudomonas aeruginosa were investigated using the crystal violet method. The concentration of total phenols was measured according to the Folin–Ciocalteu method and the values obtained ranged from 19.61 mgGA/g to 220.31 mgGA/g. The concentration of flavonoids was examined by the aluminum chloride method and the values obtained ranged from 20.58 mgRU/g to 97.06 mgRU/g. The total tannins concentration was measured by the polyvinylpolypyrrolidone method and the values obtained ranged from 3.06 mgGA/g to 207.27 mgGA/g. The concentration of proanthocyanidins was determined by the butanol–HCl method and the values obtained ranged from 4.15 CChE/g to 103.72 CChE/g. Among the various extracts studied, the acetone extract exhibited good antioxidant activity (97.13%, as determined by the DPPH method. The acetone extract was active in the absorbance value range from 2.2665 to 0.2495 (as determined by the reducing power method. The strongest antimicrobial activity was detected on G+ bacteria, especially on probiotic species, and the acetone extract demonstrated the highest activity. Biofilm inhibitory concentration required to reduce biofilm coverage by 50% values for acetone extract was 4315 μg/mL for P. mirabilis and 4469.5 μg/mL for P. aeruginosa. The results provide a basis for further research of this plant species.

  6. Synthesis and study on biological activity of nitrogen-containing heterocyclic compounds – regulators of enzymes of nucleic acid biosynthesis

    Directory of Open Access Journals (Sweden)

    Alexeeva I. V.

    2013-07-01

    Full Text Available Results of investigations on the development of new regulators of functional activity of nucleic acid biosynthesis enzymes based on polycyclic nitrogen-containing heterosystems are summarized. Computer design and molecular docking in the catalytic site of target enzyme (T7pol allowed to perform the directed optimization of basic structures. Several series of compounds were obtained and efficient inhibitors of herpes family (simple herpes virus type 2, Epstein-Barr virus, influenza A and hepatitis C viruses were identified, as well as compounds with potent antitumor, antibacterial and antifungal activity. It was established that the use of model test systems based on enzymes participating in nucleic acids synthesis is a promising approach to the primary screening of potential inhibitors in vitro.

  7. An endophytic/pathogenic Phoma sp. from creosote bush producing biologically active volatile compounds having fuel potential.

    Science.gov (United States)

    Strobel, Gary; Singh, Sanjay K; Riyaz-Ul-Hassan, Syed; Mitchell, Angela M; Geary, Brad; Sears, Joe

    2011-07-01

    A Phoma sp. was isolated and characterized as endophytic and as a pathogen of Larrea tridentata (creosote bush) growing in the desert region of southern Utah, USA. This fungus produces a unique mixture of volatile organic compounds (VOCs), including a series of sesquiterpenoids, some alcohols and several reduced naphthalene derivatives. Trans-caryophyllene, a product in the fungal VOCs, was also noted in the VOCs of this pungent plant. The gases of Phoma sp. possess antifungal properties and is markedly similar to that of a methanolic extract of the host plant. Some of the test organisms with the greatest sensitivity to the Phoma sp. VOCs were Verticillium, Ceratocystis, Cercospora and Sclerotinia while those being the least sensitive were Trichoderma, Colletotrichum and Aspergillus. We discuss the possible involvement of VOC production by the fungus and its role in the biology/ecology of the fungus/plant/environmental relationship with implications for utilization as an energy source.

  8. A comparative evaluation of biological activities and bioactive compounds of the seagrasses Zostera marina and Zostera noltei from southern Portugal.

    Science.gov (United States)

    Custódio, Luísa; Laukaityte, Simona; Engelen, Aschwin H; Rodrigues, Maria João; Pereira, Hugo; Vizetto-Duarte, Catarina; Barreira, Luísa; Rodríguez, Hortensia; Alberício, Fernando; Varela, João

    2016-01-01

    This work assessed the antioxidant potential, acetylcholinesterase (AChE) inhibition and the in vitro cytotoxic activity of extracts of the seagrasses Zostera marina and Zostera noltei collected from southern Portugal. The total phenolic contents (TPCs), the rosmarinic acid (RA) concentration (HPLC/DAD) and the fatty acid (FA) profile (GC/MS) are also described. Z. marina had the highest TPC, radical scavenging activity against DPPH radicals and copper chelating activity. Z. noltei had metal chelation capacity to copper and iron ions. None of the species was able to inhibit AChE. Both seagrasses had high levels of polyunsaturated FAs. Z. marina significantly and selectively reduced the viability of tumorous neuronal cells. Z. noltei was highly toxic for the three cell lines tested and was selective against hepatocarcinoma cells at the concentration of 100 μg/mL. RA was the main compound identified in Z. marina, but not in Z. noltei.

  9. Chemical composition and biological activity of four salvia essential oils and individual compounds against two species of mosquitoes.

    Science.gov (United States)

    Ali, Abbas; Tabanca, Nurhayat; Demirci, Betul; Blythe, Eugene K; Ali, Zulfiqar; Baser, K Husnu Can; Khan, Ikhlas A

    2015-01-21

    The chemical compositions of essential oils obtained from four species of genus Salvia were analyzed by gas chromatography with a flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The main compounds identified from Salvia species essential oils were as follows: 1,8-cineole (71.7%), α-pinene (5.1%), camphor (4.4%), and β-pinene (3.8%) in Salvia apiana; borneol (17.4%), β-eudesmol (10.4%), bornyl acetate (5%), and guaiol (4.8%) in Salvia elegans; bornyl acetate (11.4%), β-caryophyllene (6.5%), caryophyllene oxide (13.5%), and spathulenol (7.0%) in Salvia leucantha; α-thujene (25.8%), viridiflorol (20.4%), β-thujene (5.7%), and camphor (6.4%) in Salvia officinalis. In biting-deterrent bioassays, essential oils of S. leucantha and S. elegans at 10 μg/cm(2) showed activity similar to that of DEET (97%, N, N-diethyl-m-toluamide) in two species of mosquitoes, whereas the activities of S. officinalis and S. apiana essential oils were lower than those of the other oils or DEET. Pure compounds β-eudesmol and guaiol showed biting-deterrent activity similar to DEET at 25 nmol/cm(2), whereas the activity of 13-epi-manool, caryophyllene oxide, borneol, bornyl acetate, and β-caryophyllene was significantly lower than that of β-eudesmol, guaiol, or DEET. All essential oils showed larvicidal activity except that of S. apiana, which was inactive at the highest dose of 125 ppm against both mosquito species. On the basis of 95% CIs, all of the essential oils showed higher toxicity in Anopheles quadrimaculatus than in Aedes aegypti. The essential oil of S. leucantha with an LC50 value of 6.2 ppm showed highest toxicity in An. quadrimaculatus.

  10. A review exploring biological activities of hydrazones

    Directory of Open Access Journals (Sweden)

    Garima Verma

    2014-01-01

    Full Text Available The development of novel compounds, hydrazones has shown that they possess a wide variety of biological activities viz. antimicrobial, anticonvulsant, antidepressant, anti-inflammatory, analgesic, antiplatelet, antimalarial, anticancer, antifungal, antitubercular, antiviral, cardio protective etc., Hydrazones/azomethines/imines possess-NHN = CH- and constitute an important class of compounds for new drug development. A number of researchers have synthesized and evaluated the biological activities of hydrazones. This review aims at highlighting the diverse biological activities of hydrazones.

  11. Use of an in vitro flat-bed biofilm model to measure biologically active anti-odour compounds.

    Science.gov (United States)

    Saad, S; Hewett, K; Greenman, J

    2013-09-01

    The objective of this study was to demonstrate the utility of a modified flat-bed perfusion biofilm matrix system for testing toothpaste formulations directly, without dilution, as a layer in direct contact with the biofilm matrix surface. Final biofilm yields and volatile sulphur compounds (VSC) biogenesis were measured to show the relative efficacy of toothpaste formulations. Diffusion characteristics of the flat-bed system to exposure with Meridol® tooth and tongue gel (TTG; 1,400 ppm F(-) from amine fluoride/stannous fluoride, 0.5 % zinc lactate, oral malodour counteractives) was assessed using a bioluminescent target species Escherichia coli Nissle 1917/pGLITE coupled with a low-light photon camera to visualise the kill kinetics. Tongue-flora derived, mixed culture biofilms (n = 4) received 5, 15 and 30 min treatment with TTG, respectively, to determine the optimum time of exposure. VSC biogenesis was measured from headspace samples by gas chromatography prior to and following treatment of two daily applications for 4 days of treatment (TTG), positive control (CHX gel) and negative controls (placebo and sham treatment). Viable counts were performed at the end of experiments by destructive sampling of the biofilms and plating onto selective and non-selective agar. Following a single treatment with TTG, the E. coli biofilm with lux target gave >50 % reduction of luminescence within 2 to 3 h before recovering to a steady state over 10 h, suggesting biofilm cidal activity rather biostasis. For mixed culture biofilms, 15- and 30-min treatment exposure with TTG gave almost identical reductions in final biofilm yields. For comparing efficacy of treatments, biofilms treated with TTG gave greatest reductions in both pre-post levels of H2S (P biofilm microflora within a real mouth, including VSC biogenesis and its inhibition by exposure to active agents as components of toothpastes and gels applied in direct contact with the biofilm.

  12. ePlantLIBRA: A composition and biological activity database for bioactive compounds in plant food supplements.

    Science.gov (United States)

    Plumb, J; Lyons, J; Nørby, K; Thomas, M; Nørby, E; Poms, R; Bucchini, L; Restani, P; Kiely, M; Finglas, P

    2016-02-15

    The newly developed ePlantLIBRA database is a comprehensive and searchable database, with up-to-date coherent and validated scientific information on plant food supplement (PFS) bioactive compounds, with putative health benefits as well as adverse effects, and contaminants and residues. It is the only web-based database available compiling peer reviewed publications and case studies on PFS. A user-friendly, efficient and flexible interface has been developed for searching, extracting, and exporting the data, including links to the original references. Data from over 570 publications have been quality evaluated and entered covering 70 PFS or their botanical ingredients.

  13. Biological activity of Pinus nigra terpenes--evaluation of FtsZ inhibition by selected compounds as contribution to their antimicrobial activity.

    Science.gov (United States)

    Sarac, Zorica; Matejić, Jelena S; Stojanović-Radić, Zorica Z; Veselinović, Jovana B; Džamić, Ana M; Bojović, Srdjan; Marin, Petar D

    2014-11-01

    In the current work, in vitro antioxidant, antibacterial, and antifungal activites of the needle terpenes of three taxa of Pinus nigra from Serbia (ssp. nigra, ssp. pallasiana, and var. banatica) were analyzed. The black pine essential oils showed generally weak antioxidative properties tested by two methods (DPPH and ABTS scavenging assays), where the highest activity was identified in P. nigra var. banatica (IC50=25.08 mg/mL and VitC=0.67 mg (vitamin C)/g when tested with the DPPH and ABTS reagents, respectively). In the antimicrobial assays, one fungal (Aspergilus niger) and two bacterial strains (Staphylococcus aureus and Bacillus cereus) showed sensitivity against essential oils of all three P. nigra taxa. The tested oils have been shown to possess inhibitory action in the range from 20.00 to 0.62 mg/mL, where var. banatica exhibited the highest and ssp. nigra the lowest antimicrobial action. In order to determine potential compounds that are responsible for alternative mode of action, molecular docking simulations inside FtsZ (a prokaryotic homolog of tubulin) were performed. Tested compounds were the most abundant terpenoid (germacrene D-4-ol) and its structurally similar terpene (germacrene D), both present in all three essential oils. It was determined that the oxygenated form of the molecule creates stable bonds with investigated enzyme FtsZ, and that this compound, through this mechanism of action participates in the antimicrobial activity.

  14. Quantitative determination of biological activity of botulinum toxins utilizing compound muscle action potentials (CMAP), and comparison of neuromuscular transmission blockage and muscle flaccidity among toxins.

    Science.gov (United States)

    Torii, Yasushi; Goto, Yoshitaka; Takahashi, Motohide; Ishida, Setsuji; Harakawa, Tetsuhiro; Sakamoto, Takashi; Kaji, Ryuji; Kozaki, Shunji; Ginnaga, Akihiro

    2010-01-01

    The biological activity of various types of botulinum toxin has been evaluated using the mouse intraperitoneal LD(50) test (ip LD(50)). This method requires a large number of mice to precisely determine toxin activity, and so has posed a problem with regard to animal welfare. We have used a direct measure of neuromuscular transmission, the compound muscle action potential (CMAP), to evaluate the effect of different types of botulinum neurotoxin (NTX), and we compared the effects of these toxins to evaluate muscle relaxation by employing the digit abduction scoring (DAS) assay. This method can be used to measure a broad range of toxin activities the day after administration. Types A, C, C/D, and E NTX reduced the CMAP amplitude one day after administration at below 1 ip LD(50), an effect that cannot be detected using the mouse ip LD(50) assay. The method is useful not only for measuring toxin activity, but also for evaluating the characteristics of different types of NTX. The rat CMAP test is straightforward, highly reproducible, and can directly determine the efficacy of toxin preparations through their inhibition of neuromuscular transmission. Thus, this method may be suitable for pharmacology studies and the quality control of toxin preparations.

  15. 2-(Substituted phenyl-3,4-dihydroisoquinolin-2-iums as Novel Antifungal Lead Compounds: Biological Evaluation and Structure-Activity Relationships

    Directory of Open Access Journals (Sweden)

    Xin-Juan Yang

    2013-08-01

    Full Text Available The title compounds are a class of structurally simple analogues of quaternary benzo[c]phenanthridine alkaloids (QBAs. In order to develop novel QBA-like antifungal drugs, in this study, 24 of the title compounds with various substituents on the N-phenyl ring were evaluated for bioactivity against seven phytopathogenic fungi using the mycelial growth rate method and their SAR discussed. Almost all the compounds showed definite activities in vitro against each of the test fungi at 50 μg/mL and a broad antifungal spectrum. In most cases, the mono-halogenated compounds 2–12 exhibited excellent activities superior to the QBAs sanguinarine and chelerythrine. Compound 8 possessed the strongest activities on each of the fungi with EC50 values of 8.88–19.88 µg/mL and a significant concentration-dependent relationship. The SAR is as follows: the N-phenyl group is a high sensitive structural moiety for the activity and the characteristics and position of substituents intensively influence the activity. Generally, electron-withdrawing substituents remarkably enhance the activity while electron-donating substituents cause a decrease of the activity. In most cases, ortha- and para-halogenated isomers were more active than the corresponding m-halogenated isomers. Thus, the title compounds emerged as promising lead compounds for the development of novel biomimetic antifungal agrochemicals. Compounds 8 and 2 should have great potential as new broad spectrum antifungal agents for plant protection.

  16. Imidazole: Having Versatile Biological Activities

    Directory of Open Access Journals (Sweden)

    Amita Verma

    2013-01-01

    Full Text Available Imidazoles have occupied a unique position in heterocyclic chemistry, and its derivatives have attracted considerable interests in recent years for their versatile properties in chemistry and pharmacology. Imidazole is nitrogen-containing heterocyclic ring which possesses biological and pharmaceutical importance. Thus, imidazole compounds have been an interesting source for researchers for more than a century. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, and nucleic acid. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus is used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. There are several methods used for the synthesis of imidazole-containing compounds, and also their various structure reactions offer enormous scope in the field of medicinal chemistry. The imidazole derivatives possess extensive spectrum of biological activities such as antibacterial, anticancer, antitubercular, antifungal, analgesic, and anti-HIV activities. This paper aims to review the biological activities of imidazole during the past years.

  17. Biological activities of organic compounds adsorbed onto ambient air particles: comparison between the cities of Teplice and Prague during the summer and winter seasons 2000-2001

    Energy Technology Data Exchange (ETDEWEB)

    Binkova, Blanka; Cerna, Milena; Pastorkova, Anna; Jelinek, Richard; Benes, Ivan; Novak, Jiri; Sram, Radim J

    2003-04-09

    The capital of the Czech Republic, Prague, appears today to be one of the most polluted residential areas in the country, whereas air pollution in the Northern Bohemia region (the former 'Black Triangle Region') has substantially decreased during the last decade, especially with respect to the gaseous pollutant SO{sub 2}. This study evaluated the biological activities of complex mixtures of organic compounds adsorbed onto ambient air particles (PM10) collected during the summer and winter seasons of 2000-2001 at three monitoring sites - Teplice (TP), Prague-Smichov (PRG-SM) (city centre) and Prague-Libus (PRG-LB) (suburban area). The following short-term in vitro assays with strikingly different endpoints were used: a bacterial mutagenicity test using the Salmonella typhimurium tester strain TA98 and YG1041, an acellular assay (CT DNA) combined with {sup 32}P-postlabelling to evaluate DNA adduct-forming potency and the chick embryotoxicity screening test (CHEST). The results of the mutagenicity test with the YG1041 strain, the acellular genotoxicity (DNA adducts) and the embryotoxicity tests responded to the amount of eight carcinogenic polycyclic aromatic hydrocarbons (PAHs) analysed in the EOM (dichloromethane extractable organic matter) samples tested. Nevertheless, the biological effects of the EOM did not differ between locations. The highest biological activity of the ambient air in terms of organic compounds associated with particles (per unit volume of air) was seen in the Prague city centre during both summer and winter seasons. At this location, B[a]P concentration ranged from 0.1 to 8.9 ng/m{sup 3} (mean 0.3 and 3.6 ng/m{sup 3} for summer and winter seasons, respectively), 13 PAHs ranged from 11 to 343 ng/m{sup 3} (mean 52 and 160 ng/m{sup 3} for summer and winter seasons, respectively). Generally, using in vitro tests, higher ambient air activity was found in the winter season as compared with the summer season at all three monitoring sites

  18. Human biological monitoring of suspected endocrine-disrupting compounds

    OpenAIRE

    Moosa Faniband; Lindh, Christian H; Bo AG Jönsson

    2014-01-01

    Endocrine-disrupting compounds are exogenous agents that interfere with the natural hormones of the body. Human biological monitoring is a powerful method for monitoring exposure to endocrine disrupting compounds. In this review, we describe human biological monitoring systems for different groups of endocrine disrupting compounds, polychlorinated biphenyls, brominated flame retardants, phthalates, alkylphenols, pesticides, metals, perfluronated compounds, parabens, ultraviolet filters, and o...

  19. Natural compounds with herbicidal activity

    Directory of Open Access Journals (Sweden)

    Pasquale Montemurro

    2011-02-01

    Full Text Available Research about phytotoxic activity of natural compounds could lead both to find new herbicidal active ingredients and to plan environmental friendly weed control strategies. Particularly, living organisms could be a source of compounds that are impossible, for their complexity, to synthesize artificially. More over, they could have alternative sites of action respect to the known chemical herbicides and, due to their origin, they should be more environmental safe. Many living organism, such as bacteria, fungi, insects, lichens and plants, are able to produce bioactive compounds. They generally are secondary metabolites or simply waste molecules. In this paper we make a review about these compounds, highlighting potential and constraints.

  20. Síntesis y Actividad Biológica de Nuevos Compuestos Gemini Peptídicos Synthesis and Biological Activity of New Peptide-Based Gemini Compounds

    Directory of Open Access Journals (Sweden)

    Diana M Müller

    2011-01-01

    Full Text Available Se ha sintetizado y evaluado la actividad antimicrobiana de nuevos compuestos gemini derivados de un tetrapéptido. La síntesis se realizó utilizando química en fase sólida y N-d -alquilación directa e indirecta de los residuos peptídicos de ornitina . La actividad antimicrobiana se ensayó frente a cepas ATCC (American Type Culture Collection mediante difusión en agar y determinación de la concentración inhibitoria mínima. El método directo de N- alquilación con carbonato de potasio fue el más adecuado con rendimientos del 40 % permitiendo obtener compuestos mono y di alquilados biológicamente activos. La baja masa molecular de estos compuestos, su forma simple de obtención y su actividad hacia bacterias causantes de enfermedades de transmisión alimentaria los hace tecnológicamente atractivos para ser utilizados como preservadores alimentarios. La presencia de ornitina en las moléculas les otorga resistencia enzimática y vida media biológica mayor, por que podrían ser utilizados para el desarrollo de drogas con fines terapéuticos.The antimicrobial activity of new gemini derived from a tetrapeptide has been evaluated. The synthesis was carried out using solid phase chemistry and N - d - direct and indirect alkylation of the ornithine peptide residue . The antimicrobial activity was tested against ATCC strains (American Type Culture Collection by well-diffusion assay and determination of minimal inhibitory concentration. The method of N- alkylation with potassium carbonate was the best with yields of 40% allows achieving biologically active mono and dialkylate surfactants. The low molecular weight of these compounds, their simple way of preparation and their activity towards bacteria causing food-borne diseases makes them technologycally attractive for use as food preservatives. The presence in the molecules of ornithine gives them enzymatic resistance and a longer biological half-life and thus may be used to develop drugs

  1. 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

    2016-07-22

    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.

  2. Some biological compounds, radical scavenging capacities and antimicrobial activities in the seeds of Nepeta italica L. and Sideritis montana L. subsp. montana from Turkey

    Energy Technology Data Exchange (ETDEWEB)

    Emre, I.; Kursat, M.; Yilmaz, O.; Erecevit, P.

    2011-07-01

    This study determined some biological compounds (fatty acid compositions, lipid-soluble vitamins, sterols, flavonoids), radical scavenging capacities and antimicrobial activities in the seeds of Nepeta italica L. and Sideritis montana L. subsp. montana. It was found that palmitic acid (C16:0; 8.54+-0.13-3.05+-0.04%), oleic acid (C18:1 n9, 22.41+-0.8-18.83+-0.1%) and a-inolenic acid were the dominant fatty acids in both Nepeta italica L. and Sideritis montana L. subsp. montana. It was concluded that both Nepeta italica L. and Sideritis montana L. subsp. montana contained stigmasterol and ergosterol as well as beta-sitosterol. The present findings show that Nepeta italica L. contains morin, catechin, naringin and Sideritis montana L. subsp. montana contains morin, naringenin as major flavonoids. It was also determined that methanol extracts of Nepeta italica L. and Sideritis montana L. subsp. montana were most effective against DPPH radicals. The results of the present study show that the vitamins, flavonoids and fatty acid extracts in the seeds of N. italica L. and S. montana L. subsp. montana prevented the growth of the microorganisms used in the tests at different ratios. (Author).

  3. Some biological compounds, radical scavenging capacities and antimicrobial activities in the seeds of Nepeta italica L. and Sideritis montana L. sub sp. montana from Turkey

    Energy Technology Data Exchange (ETDEWEB)

    Emre, I.; Kursat, M.; Yilmaz, O.; Erecevit, P.

    2011-07-01

    This study determined some biological compounds (fatty acid compositions, lipid-soluble vitamins, sterols, flavonoids), radical scavenging capacities and antimicrobial activities in the seeds of Nepeta italica L. and Sideritis montana L. subsp. montana. It was found that palmitic acid (C16:0; 8.54+-0.13-3.05+-0.04%), oleic acid (C18:1 n9, 22.41+-0.8-18.83+-0.1%) and a-inolenic acid were the dominant fatty acids in both Nepeta italica L. and Sideritis montana L. subsp. montana. It was concluded that both Nepeta italica L. and Sideritis montana L. subsp. montana contained stigmasterol and ergosterol as well as beta-sitosterol. The present findings show that Nepeta italica L. contains morin, catechin, naringin and Sideritis montana L. subsp. montana contains morin, naringenin as major flavonoids. It was also determined that methanol extracts of Nepeta italica L. and Sideritis montana L. subsp. montana were most effective against DPPH radicals. The results of the present study show that the vitamins, flavonoids and fatty acid extracts in the seeds of N. italica L. and S. montana L. subsp. montana prevented the growth of the microorganisms used in the tests at different ratios. (Author).

  4. 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.

  5. Shapeshifting photoswitchable azobenzene compounds and their biological applications

    Science.gov (United States)

    Peddie, Victoria; Heng, Sabrina; Mustafa, Sanam; Thomas, Jacob; Hutchinson, Mark R.; Abell, Andrew D.

    2016-11-01

    The photoisomerisation of azobenzenes between trans and cis results in well-defined changes in geometry and a considerable change of polarity. Thus, incorporating an azobenezene into a bioactive compound provides an opportunity to control biological activity, with ideally one configuration being active and the other inactive. This can allow the role of a specific biomolecule to be probed in its native environment by controlling activity both spatially and temporally using light. Incorporating such a photoswitchable moiety into the structure of a known GRK2 inhibitor can generate photoswitchable inhibitors, which can be used to reversibly regulate the activity of GRK2, and hence GPRCs.

  6. Molecular characteristics versus biological activity

    Science.gov (United States)

    Applegate, Vernon C.; Smith, Manning A.; Willeford, Bennett R.

    1967-01-01

    The molecular characteristics of mononitrophenols containing halogens not only play a key role in their biological activity but provide a novel example of selective toxicity among vertebrate animals. It has been reported that efforts to control the parasitic sea lamprey in the Great Lakes are directed at present to the applications of a selective toxicant to streams inhabited by lamprey larvae. Since 1961, the larvicide that has been used almost exclusively in the control program has been 3-trifluoromethyl-4-nitrophenol (TFM). However, this is only one of about 15 closely related compounds, all halogen-containing mononitrophenols, that display a selectively toxic action upon lampreys. Although not all of the halogenated mononitrophenols are selectively toxic to lampreys (in fact, fewer than half of those tested), no other group of related compounds has displayed any useful larvicidal activity except for the substituted nitrosalicylanilides.

  7. 微藻的生物活性物质及其功能%Biologically active compounds from microalgae and its health function

    Institute of Scientific and Technical Information of China (English)

    卢仡; 林红华; 柯群

    2011-01-01

    Microalgae are a biochemically diverse assemblage of microorganisms amenable to fermentation and mass culture.Most of these microalgae species produce unique products like carotenoids,antioxidants,fatty acids, enzymes,polymers,peptides,toxins and sterols.Microalgae might become economic sources of new drugs,other specialty chemicals and functional foods because production can be optimized in controlled culture. This paper introduced the biologically active compounds from microalgae and its health function, studies of microalgae in human nutrition and new trends in microalgae food,researched on microalgal health food,and the development of information was provided.%微藻是适于发酵和生物培养的一种微生物生化组合.大多数微藻产生特有的生物活性物质,如类胡萝卜素、抗氧化剂、脂肪酸、酶类、聚合物、肽类、毒素和甾醇.由于微藻可以控制、优化培养条件,将能成为新的药品、特种化学品和功能食品的经济资源.本文对微藻的生物活性物质及其保健功能、微藻与人类营养方面的研究以及微藻食品的新发展做了较全面的介绍,以期时微藻保健食品的研究、开发提供有益的参考.

  8. Human biological monitoring of suspected endocrine-disrupting compounds.

    Science.gov (United States)

    Faniband, Moosa; Lindh, Christian H; Jönsson, Bo A G

    2014-01-01

    Endocrine-disrupting compounds are exogenous agents that interfere with the natural hormones of the body. Human biological monitoring is a powerful method for monitoring exposure to endocrine disrupting compounds. In this review, we describe human biological monitoring systems for different groups of endocrine disrupting compounds, polychlorinated biphenyls, brominated flame retardants, phthalates, alkylphenols, pesticides, metals, perfluronated compounds, parabens, ultraviolet filters, and organic solvents. The aspects discussed are origin to exposure, metabolism, matrices to analyse, analytical determination methods, determinants, and time trends.

  9. [Biological activity of Spirulina].

    Science.gov (United States)

    Blinkova, L P; Gorobets, O B; Baturo, A P

    2001-01-01

    In this review information of Spirulina platensis (SP), a blue-green alga (photosynthesizing cyanobacterium) having diverse biological activity is presented. Due to high content of highly valuable proteins, indispensable amino acids, vitamins, beta-carotene and other pigments, mineral substances, indispensable fatty acids and polysaccharides, PS has been found suitable for use as bioactive additive. SP produces an immunostimulating effect by enhancing the resistance of humans, mammals, chickens and fish to infections, the capacity of influencing hemopoiesis, stimulating the production of antibodies and cytokines. Under the influence of SP macrophages, T and B cells are activated. SP sulfolipids have proved to be effective against HIV. Preparations obtained from SP biomass have also been found active against herpesvirus, cytomegalovirus, influenza virus, etc. SP extracts are capable in inhibiting cancerogenesis. SP preparations are regarded as functional products contributing to the preservation of the resident intestinal microflora, especially lactic acid bacilli and bifidobacteria, and to a decrease in the level of Candida albicans. The biological activity of SP with respect to microorganisms holds good promise for using these microalgae as components of culture media.

  10. Activity-guided isolation, identification and quantification of biologically active isomeric compounds from folk medicinal plant Desmodium adscendens using high performance liquid chromatography with diode array detector, mass spectrometry and multidimentional nuclear magnetic resonance spectroscopy.

    Science.gov (United States)

    Zielińska-Pisklak, Monika A; Kaliszewska, Dorota; Stolarczyk, Magdalena; Kiss, Anna K

    2015-01-01

    The antioxidant activity of the crude extract (60% ethanol) from the leaves of Desmodium adscendens (Sw.) DC. (Fabaceae) was observed in DPPH, xanthine/xanthine oxidase, lipid peroxydation and neutrophils burst tests. Further activity-guided fractionation on C18 column (water, 20% methanol, 50% methanol and 100% methanol) resulted in the separation of the fraction (50% methanol) with the highest antioxidant capacity. HPLC-DAD analysis of biologically active fraction revealed the presence of two pairs of flavonoid isomers as the dominant constituents. Those compounds were isolated and purified by multi-step liquid column chromatography (Sephadex LH20). Their structures were elucidated by various spectroscopic techniques, including NMR, UV and MS. Based on 1D and 2D NMR spectra as well as ion fragmentation, flavonoids were identified as: isovitexin 2''-O-xyloside (1), vitexin 2''-O-xyloside (2), vitexin (3) and isovitexin (4). The hybrid HSQC-DEPT technique provided very fast determination of the glycosylation positions in aglycone and the type of glycosidic bond in the flavonoid isomers. This study provides novel information concerning identity of the major compounds present in the leaves of D. adscendens cultivated in Ghana, which broadens the knowledge about anti-inflammatory, antiallergic and antioxidant properties of their extracts.

  11. Biologically active sesquiterpene coumarins from Ferula species.

    Science.gov (United States)

    Nazari, Zeinab Esmail; Iranshahi, Mehrdad

    2011-03-01

    Extracts from different species of the genus Ferula (Apiaceae) have had various biomedical applications for many centuries. Many biological features of this genus such as cytotoxicity, antibacterial, antiviral, P-glycoprotein (P-gp) inhibitory and antiinflammatory activity have been attributed to sesquiterpene coumarins; structures containing a common coumarin group and a sesquiterpene moiety. This both highlights the importance of sesquiterpene coumarins as biologically active natural products and necessitates further studies on these compounds. Taking into account the versatile biological properties of compounds isolated from Ferula and the unprecedented interest in the application of natural products as a new generation of therapeutics, the present review will discuss reports on biological activities of sesquiterpene coumarins of the genus Ferula, from 1990 onwards.

  12. Impact of bioaccessibility and bioavailability of phenolic compounds in biological systems upon the antioxidant activity of the ethanolic extract of Triplaris gardneriana seeds.

    Science.gov (United States)

    Neto, José Joaquim Lopes; de Almeida, Thiago Silva; de Medeiros, Jackeline Lima; Vieira, Leonardo Rogério; Moreira, Thaís Borges; Maia, Ana Isabel Vitorino; Ribeiro, Paulo Riceli Vasconcelos; de Brito, Edy Sousa; Farias, Davi Felipe; Carvalho, Ana Fontenele Urano

    2017-04-01

    The most studied bioactive potential of phenolic compounds corresponds to antioxidant activity, which in turn, is associated with a reduction in the incidence of various human diseases. However, the total quantity of these bioactive substances in foods and medicinal preparations does not reflect the amount absorbed and metabolized by the body. The present study aimed to investigate the bioaccessibility of Triplaris gardneriana seeds ethanolic extract (EETg) by determination of phenolic composition and antioxidant activities before and after in vitro digestion as well as to estimate its bioavailability by chemical analysis of plasma and urine in animal models after oral administration. The bioaccessibility indexes of phenolic compounds in EETg were 48.65 and 69.28% in the presence and absence of enzymes, respectively. Among the identified phenolics classes, flavonoids, represented by galloylated procyanidins type B, proved to be more bioaccessible, 81.48 and 96.29% in the post-intestinal phase with and without enzymes, respectively. The oral administration in Wistar rats resulted in a significant decrease in plasma of the total antioxidant capacity, TAC, by FRAP assay 4h after beginning the experiment. For urine samples, an increase in TAC by DPPH and FRAP was observed from 1 and 4h after administration, respectively. UPLC-QTOF analysis of urine detected 2 metabolites originated from the degradation of phenolic compounds, i.e. hippuric acid and phenylacetil glycine. These results suggest that phenolic compounds in T. gardneriana are unstable under gastrointestinal conditions, being flavonoids the components with higher bioaccessibility; besides that, they showed limited bioavailability due to their rapid biotransformation and urinary elimination.

  13. A novel approach for identification of biologically active phenolic compounds in complex matrices using hybrid quadrupole-orbitrap mass spectrometer: A promising tool for testing antimicrobial activity of hops.

    Science.gov (United States)

    Dušek, Martin; Jandovská, Vladimíra; Čermák, Pavel; Mikyška, Alexandr; Olšovská, Jana

    2016-08-15

    The phenolic compounds, secondary metabolites of hops represent a large family of compounds that could be subsequently divided into smaller groups based on the similarities between their chemical structures. The antibacterial, antifungal and antiviral properties of hops are well known, but there is a lack of information about antimicrobial activities of individual hop compounds. This study was carried out with an objective to identify compounds present in hops that have potential antibacterial activity. In the first stage of experiment, the active compounds with potential anti-microbial activity had to be extracted from hop cones. Therefore, minced hop cones were applied on solid growth medium inoculated with Staphylococcus aureus. The active substances that migrated into the medium created an inhibition zone. In the second stage of experiment, the inhibition zones were cut out from Petri dishes, active compounds were extracted from these zones and consequently analyzed using LC-HRMS. These complex assays were developed and optimized. The data were acquired by using a quadrupole-orbitrap hybrid mass spectrometer by targeted-MS2 experiment in both ionization modes. The MS method has been developed as a screening method with a subsequent fragmentation of compound of interest on the base of inclusion mass list. The unknown compounds extracted from inhibition zones have been identified either by searching against a database or their structure has been elucidated on the basis of their fragmentation spectra. On the basis of this experiment the list of active compounds with potential anti-microbial activities was enhanced.

  14. Human biological monitoring of suspected endocrine-disrupting compounds

    Directory of Open Access Journals (Sweden)

    Moosa Faniband

    2014-02-01

    Full Text Available Endocrine-disrupting compounds are exogenous agents that interfere with the natural hormones of the body. Human biological monitoring is a powerful method for monitoring exposure to endocrine disrupting compounds. In this review, we describe human biological monitoring systems for different groups of endocrine disrupting compounds, polychlorinated biphenyls, brominated flame retardants, phthalates, alkylphenols, pesticides, metals, perfluronated compounds, parabens, ultraviolet filters, and organic solvents. The aspects discussed are origin to exposure, metabolism, matrices to analyse, analytical determination methods, determinants, and time trends.

  15. Structural optimization and evaluation of butenolides as potent antifouling agents: modification of the side chain affects the biological activities of compounds

    KAUST Repository

    Li, Yongxin

    2012-09-01

    A recent global ban on the use of organotin compounds as antifouling agents has increased the need for safe and effective antifouling compounds. In this study, a series of new butenolide derivatives with various amine side chains was synthesized and evaluated for their anti-larval settlement activities in the barnacle, Balanus amphitrite. Side chain modification of butenolide resulted in butenolides 3c-3d, which possessed desirable physico-chemical properties and demonstrated highly effective non-toxic anti-larval settlement efficacy. A structure-activity relationship analysis revealed that varying the alkyl side chain had a notable effect on anti-larval settlement activity and that seven to eight carbon alkyl side chains with a tert-butyloxycarbonyl (Boc) substituent on an amine terminal were optimal in terms of bioactivity. Analysis of the physico-chemical profile of butenolide analogues indicated that lipophilicity is a very important physico-chemical parameter contributing to bioactivity. © 2012 Copyright Taylor and Francis Group, LLC.

  16. Biologically Active Substances from Higher Fungi

    Institute of Scientific and Technical Information of China (English)

    Liu Jikai

    2007-01-01

    As a part of our search for naturally occurring bioactive metabolites of mushrooms, we have investigated the chemical constituents of more than 100 Basidiomycetes and Ascomycetes fungi, and isolated over 300 including 150 new terpenoids,phenolics and nitrogen-containing compounds. The isolation, structural elucidation and biologically activity of the natural products from the higher fungi are briefly discussed.

  17. Metal based biologically active compounds: design, synthesis, and antibacterial/antifungal/cytotoxic properties of triazole-derived Schiff bases and their oxovanadium(IV) complexes.

    Science.gov (United States)

    Chohan, Zahid H; Sumrra, Sajjad H; Youssoufi, Moulay H; Hadda, Taibi B

    2010-07-01

    A new series of oxovanadium(IV) complexes have been designed and synthesized with a new class of triazole Schiff bases derived from the reaction of 3,5-diamino-1,2,4-triazole with 2-hydroxy-1-naphthaldehyde, pyrrole-2-carboxaldehyde, pyridine-2-carboxaldehyde and acetyl pyridine-2-carboxaldehyde, respectively. Physical (magnetic susceptibility, molar conductance), spectral (IR, (1)H NMR, (13)C NMR, mass and electronic) and analytical data have established the structures of these synthesized Schiff bases and their oxovanadium(IV) complexes. The Schiff bases, predominantly act as bidentate and coordinate with the vanadium(IV) metal to give a stoichiometric ratio of 1:2 [M:L], forming a general formulae, [M(L-H)(2)] and [M(L)(2)]SO(4) where L = (L(1))-(L(4)) and M = VO(IV) of these complexes in a square-pyramidal geometry. In order to evaluate the biological activity of Schiff bases and to assess the role of vanadium(IV) metal on biological activity, the triazole Schiff bases and their oxovanadium(IV) complexes have been studied for in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexenari, Pseudomonas aeruginosa, Salmonella typhi) and two Gram-positive (Staphylococcus aureus, Bacillus subtilis) bacterial strains, in vitro antifungal activity against Trichophyton longifucus, Candida albican, Aspergillus flavus, Microscopum canis, Fusarium solani and Candida glaberata. The simple Schiff bases showed weaker to significant activity against one or more bacterial and fungal strains. In most of the cases higher activity was exhibited upon coordination with vanadium(IV) metal. Brine shrimp bioassay was also carried out for in vitro cytotoxic properties against Artemia salina.

  18. Centrifugal partition extraction in the pH-zone-refining displacement mode: an efficient strategy for the screening and isolation of biologically active phenolic compounds.

    Science.gov (United States)

    Hamzaoui, Mahmoud; Renault, Jean-Hugues; Reynaud, Romain; Hubert, Jane

    2013-10-15

    Centrifugal partition extraction (CPE) was developed for the first time in the pH-zone-refining mode to fractionate a crude bark extract of the African tree Anogeissus leiocarpus Guill. & Perr. (Combretaceae). The fractionation process was performed at a flow rate of 20mL/min using a biphasic solvent system composed of methyl tert-butyl ether/acetonitrile/water (4:1:5, v/v/v) in the ascending mode. Sodium hydroxide (40mM) and trifluoroacetic acid (30mM) were used as retainer and displacer agents, respectively. In a single run of 67min, 3g of the initial crude extract were successfully separated into fractions selectively enriched in ionizable triterpenes, ellagic acid derivatives and flavonoids. The antioxidant potential of the initial crude extract, isolated compounds and fraction pools was also evaluated by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) stable free radical scavenging assay, providing an interesting view about the effect of the degree of substitution of ellagic acid derivatives on their radical scavenging activity. This study will demonstrate that centrifugal partition extraction used in the pH-zone-refining mode can be proposed as an efficient strategy for the rapid screening of natural phenolic compounds.

  19. Some Biological Compounds, Radical Scavenging Capacities and Antimicrobial Activities in the seeds of Nepeta italica L. and Sideritis montana L. subsp. montana from Turkey

    Directory of Open Access Journals (Sweden)

    Erecevit, Pınar

    2011-03-01

    Full Text Available This study determined some biological compounds (fatty acid compositions, lipid-soluble vitamins, sterols, flavonoids, radical scavenging capacities and antimicrobial activities in the seeds of Nepeta italica L. and Sideritis montana L. subsp. montana. It was found that palmitic acid (C16:0; 8.54±0.13- 3.05±0.04%, oleic acid (C18:1 n9, 22.41±0.8-18.83±0.1% and α-linolenic acid (C18:3 n3;39.56±0.67-77.04±2.07% were the dominant fatty acids in both Nepeta italica L. and Sideritis montana L. subsp. montana. It was concluded that both Nepeta italica L. and Sideritis montana L. subsp. montana contained stigmasterol (630.07±1.81µg/g, 80.74±0.71µg/g, respectively and ergosterol (1.11±0.14µg/g, 161.32±0.63µg/g respectively as well as beta-sitosterol (2.93±0.03 µg/g. The present findings show that Nepeta italica L. contains morin (37.79±1.09μg/g, catechin (124.39±2.23µg/g, naringin (475.96±3.57µg/g and Sideritis montana L. subsp. montana contains morin (188.41±2.53µg/g, catechin (64.14±1.86μg/g, naringenin (38.34±1.78μg/g as major flavonoids. It was also determined that methanol extracts of Nepeta italica L. and Sideritis montana L. subsp. montana were most effective against DPPH radicals. The results of the present study show that the vitamins, flavonoids and fatty acid extracts in the seeds of N. italica L. and S. montana L. subsp. montana prevented the growth of the microorganisms used in the tests at different ratios.Este estudio ha determinado algunos compuestos biológicos (ácidos grasos, vitaminas liposolubles, esteroles y flavonoides, capacidad atrapadora de radicales libres, y actividades antimicrobianas de las semillas de Nepeta italica L. y Sideritis montana L. subsp. montana. Se encontró que el ácido palmítico (C16:0; 8.54±0.13-3.05±0.04%, ácido oleico (C18:1 n9, 22.41±0.8-18.83±0.1% y α-linolénico (C18:3 n 3;39.56±0.67-77.04±2.07% eran mayoritarios en ambas semillas de Nepeta italica L. y Sideritis

  20. Original Inventions based on Chemical scaffolds and electro-physical activity-derived biosimilars interacting with specialties in biology yielding platforms for analysis in virology and antiviral compounds

    Directory of Open Access Journals (Sweden)

    Yamaji N

    2014-11-01

    effective anti viral agents. A biosimilar-based compound having been proven against Chickungunya virus, the same could be tried against life threatening viruses in appropriate and safe environments. Clinister being a food additive-based material, is considered to be safe to human beings [4] and hence its inclusion as an additive to cell culture medium could be studied further in order to check whether the use of common antibiotics and anti-fungals which may be detrimental to cell growth can be avoided yielding safer anti-bacterial and anti-viral agents for cell culture. Conclusion: Multidisciplinary interaction within and across various domains of science has several potentials in bringing out novel solutions and this has been proven by this study of interaction among physicists, chemists and biologists. The authors recommend that establishment of barrier-free interaction platforms within and among institutes and various specialties at varied stages of research activities as portrayed here like the IIDIAS session to bring about novel solutions such as the ones described in this article. References Sumathipala A, Siribaddana S, Patel V. Under-representation of developing countries in the research literature: ethical issues arising from a survey of five leading medical journals. BMC Med Ethics. 2004;5: E5. The World Bank (2008. Global Economic Prospects 2008: Technology Diffusion in the Developing World. Washington, DC: The World Bank. Retrieved February 18, 2008 from http://siteresources.worldbank.org/INTGEP2008/Resources/complete-report.pdf Abraham S. The "Electric Biology" Duo. Trade Secrets- Nature Biotechnology Blog 2011. Full text can be accessed at http://blogs.nature.com/tradesecrets/2011/12/06/the-electric-biology-duo. Kubota S, Matsuzawa K, Wada M, Yamaji N. Bactericidal Effect of a Disinfectant (Bio Io Nurse Prepared by Adding Citric Acid and Low Concentration Alcohol to Strongly Acidic Electrolyzed Water. New Food Industry 2008; 50:9. Dedeepiya VD, William JB

  1. Biological activities of alginate.

    Science.gov (United States)

    Ueno, Mikinori; Oda, Tatsuya

    2014-01-01

    To gain insight into the structure-activity relationship of alginate, we examined the effect of alginates with varying molecular weights and M/G ratio on murine macrophage cell line, RAW264.7 cells in terms of induction of tumor necrosis factor-α (TNF-α) secretion. Among the alginates tested, alginate with the highest molecular weight (MW 38,000, M/G 2.24) showed the most potent TNF-α-inducing activity. Alginates having higher M/G ratio tended to show higher activity. These results suggest that molecular size and M/G ratio are important structural parameters influencing the TNF-α-inducing activity. Interestingly, enzymatic depolymerization of alginate with bacterial alginate lyase resulted in dramatic increase in the TNF-α-inducing activity. The higher activity of enzymatically digested alginate oligomers to induce nitric oxide production from RAW264.7 cells than alginate polymer was also observed. On the other hand, alginate polymer and oligomer showed nearly equal hydroxyl radical scavenging activities.

  2. Biologic activities of molecular chaperones and pharmacologic chaperone imidazole-containing dipeptide-based compounds: natural skin care help and the ultimate challenge: implication for adaptive responses in the skin.

    Science.gov (United States)

    Babizhayev, Mark A; Nikolayev, Gennady M; Nikolayeva, Juliana G; Yegorov, Yegor E

    2012-03-01

    Accumulation of molecular damage and increased molecular heterogeneity are hallmarks of photoaged skin and pathogenesis of human cutaneous disease. Growing evidence demonstrates the ability of molecular chaperone proteins and of pharmacologic chaperones to decrease the environmental stress and ameliorate the oxidation stress-related and glycation disease phenotypes, suggesting that the field of chaperone therapy might hold novel treatments for skin diseases and aging. In this review, we examine the evidence suggesting a role for molecular chaperone proteins in the skin and their inducer and protecting agents: pharmacologic chaperone imidazole dipeptide-based agents (carcinine and related compounds) in cosmetics and dermatology. Furthermore, we discuss the use of chaperone therapy for the treatment of skin photoaging diseases and other skin pathologies that have a component of increased glycation and/or free radical-induced oxidation in their genesis. We examine biologic activities of molecular and pharmacologic chaperones, including strategies for identifying potential chaperone compounds and for experimentally demonstrating chaperone activity in in vitro and in vivo models of human skin disease. This allows the protein to function and traffic to the appropriate location in the skin, thereby increasing protein activity and cellular function and reducing stress on skin cells. The benefits of imidazole dipeptide antioxidants with transglycating activity (such as carcinine) in skin care are that they help protect and repair cell membrane damage and help retain youthful, younger-looking skin. All skin types will benefit from daily, topical application of pharmacologic chaperone antioxidants, anti-irritants, in combination with water-binding protein agents that work to mimic the structure and function of healthy skin. General strategies are presented addressing ground techniques to improve absorption of usually active chaperone proteins and dipeptide compounds, include

  3. Biological Activities of Polyphenols from Grapes

    OpenAIRE

    Hua-Bin Li; Ya-Jun Guo; Gui-Fang Deng; En-Qin Xia

    2010-01-01

    The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial proper...

  4. Measurement and biological significance of the volatile sulfur compounds hydrogen sulfide, methanethiol and dimethyl sulfide in various biological matrices.

    NARCIS (Netherlands)

    Tangerman, A.

    2009-01-01

    This review deals with the measurement of the volatile sulfur compounds hydrogen sulfide, methanethiol and dimethyl sulfide in various biological matrices of rats and humans (blood, serum, tissues, urine, breath, feces and flatus). Hydrogen sulfide and methanethiol both contain the active thiol (-SH

  5. Measurement and biological significance of the volatile sulfur compounds hydrogen sulfide, methanethiol and dimethyl sulfide in various biological matrices

    NARCIS (Netherlands)

    Tangerman, Albert

    2009-01-01

    This review deals with the measurement of the volatile Sulfur compounds hydrogen sulfide, methanethiol and dimethyl sulfide in various biological matrices of rats and humans (blood, serum, tissues, urine, breath, feces and flatus). Hydrogen sulfide and methanethiol both contain the active thiol (-SH

  6. Estrogenic flavonoids: structural requirements for biological activity.

    Science.gov (United States)

    Miksicek, R J

    1995-01-01

    A systematic survey of polycyclic phenols has been performed to identify members of this chemical group with estrogenic activity. Twelve compounds were found to be able to stimulate the transcriptional activity of the human estrogen receptor expressed in cultured cells by transient transfection. These natural estrogens belong to several distinct, but chemically related classes including chalcones, flavanones, flavones, flavonols, and isoflavones. Selected examples of estrogenic flavonoids were further analyzed to determine their biological potencies and their relative affinities for binding to the estrogen receptor. These data are interpreted with respect to the molecular structure of polycyclic phenols required for hormonal activity as nonsteroidal estrogens.

  7. Biologically active substances of stone crop fruits

    Directory of Open Access Journals (Sweden)

    Margarita Makarkina

    2014-04-01

    Full Text Available Stone fruit crops are successfully cultivated in many regions of Russia. Their fruits contain a great diversity of biologically active and mineral substances. The stone fruit varietal collection of the All Russia Research Institute of Fruit Crop Breeding has been estimated on the content of biologically active substances (ascorbic acid and phenolic compounds in fruits: 80 sour cherry varieties, 28 sweet cherry varieties, 29 plum varieties and 24 apricot varieties. High cultivar variability of the content of ascorbic acid and P-active sub-stances in fruits has been determined in each crop. The best genotypes have been singled out according to each biochemical component and a complex of characters.

  8. Isoflavones: estrogenic activity, biological effect and bioavailability.

    Science.gov (United States)

    Vitale, Daniela Cristina; Piazza, Cateno; Melilli, Barbara; Drago, Filippo; Salomone, Salvatore

    2013-03-01

    Isoflavones are phytoestrogens with potent estrogenic activity; genistein, daidzein and glycitein are the most active isoflavones found in soy beans. Phytoestrogens have similarity in structure with the human female hormone 17-β-estradiol, which can bind to both alpha and beta estrogen receptors, and mimic the action of estrogens on target organs, thereby exerting many health benefits when used in some hormone-dependent diseases. Numerous clinical studies claim benefits of genistein and daidzein in chemoprevention of breast and prostate cancer, cardiovascular disease and osteoporosis as well as in relieving postmenopausal symptoms. The ability of isoflavones to prevent cancer and other chronic diseases largely depends on pharmacokinetic properties of these compounds, in particular absorption and distribution to the target tissue. The chemical form in which isoflavones occur is important because it influences their bioavailability and, therefore, their biological activity. Glucose-conjugated isoflavones are highly polar, water-soluble compounds. They are hardly absorbed by the intestinal epithelium and have weaker biological activities than the corresponding aglycone. Different microbial families of colon can transform glycosylated isoflavones into aglycones. Clinical studies show important differences between the aglycone and conjugated forms of genistein and daidzein. The evaluation of isoflavone metabolism and bioavailability is crucial to understanding their biological effects. Lipid-based formulations such as drug incorporation into oils, emulsions and self-microemulsifying formulations have been introduced to increase bioavailability. Complexation with cyclodextrin also represent a valid method to improve the physicochemical characteristics of these substances in order to be absorbed and distributed to target tissues. We review and discuss pharmacokinetic issues that critically influence the biological activity of isoflavones.

  9. Biologically Active Metabolites Synthesized by Microalgae

    Directory of Open Access Journals (Sweden)

    Michele Greque de Morais

    2015-01-01

    Full Text Available Microalgae are microorganisms that have different morphological, physiological, and genetic traits that confer the ability to produce different biologically active metabolites. Microalgal biotechnology has become a subject of study for various fields, due to the varied bioproducts that can be obtained from these microorganisms. When microalgal cultivation processes are better understood, microalgae can become an environmentally friendly and economically viable source of compounds of interest, because production can be optimized in a controlled culture. The bioactive compounds derived from microalgae have anti-inflammatory, antimicrobial, and antioxidant activities, among others. Furthermore, these microorganisms have the ability to promote health and reduce the risk of the development of degenerative diseases. In this context, the aim of this review is to discuss bioactive metabolites produced by microalgae for possible applications in the life sciences.

  10. Spilanthol: occurrence, extraction, chemistry and biological activities

    Directory of Open Access Journals (Sweden)

    Alan F. Barbosa

    2016-02-01

    Full Text Available Abstract Spilanthol (C14H23NO, 221.339 g/mol is a bioactive compound that is found in many different plants that are used as traditional remedies throughout the world. It is present in Heliopsis longipes and several species in the genus Acmella, including A. oleracea L., also known as paracress and jambu. Its leaves and flowers have sensory properties (pungency, tingling, numbing, mouth-watering that make it a popular spice and ingredient in several Brazilian dishes. Spilanthol can exert a variety of biological and pharmacological effects including analgesic, neuroprotective, antioxidant, antimutagenic, anti-cancer, anti-inflammatory, antimicrobial, antilarvicidal and insecticidal activities. So, the aim of this review is to present a literature review on the spilanthol that describes its occurrence, chemistry, extraction and biological activities.

  11. Exploration of Cyanine Compounds as Selective Inhibitors of Protein Arginine Methyltransferases: Synthesis and Biological Evaluation

    Science.gov (United States)

    2016-01-01

    Protein arginine methyltransferase 1 (PRMT1) is involved in many biological activities, such as gene transcription, signal transduction, and RNA processing. Overexpression of PRMT1 is related to cardiovascular diseases, kidney diseases, and cancers; therefore, selective PRMT1 inhibitors serve as chemical probes to investigate the biological function of PRMT1 and drug candidates for disease treatment. Our previous work found trimethine cyanine compounds that effectively inhibit PRMT1 activity. In our present study, we systematically investigated the structure–activity relationship of cyanine structures. A pentamethine compound, E-84 (compound 50), showed inhibition on PRMT1 at the micromolar level and 6- to 25-fold selectivity over CARM1, PRMT5, and PRMT8. The cellular activity suggests that compound 50 permeated the cellular membrane, inhibited cellular PRMT1 activity, and blocked leukemia cell proliferation. Additionally, our molecular docking study suggested compound 50 might act by occupying the cofactor binding site, which provided a roadmap to guide further optimization of this lead compound. PMID:25559100

  12. Metal-Based Biologically Active Compounds: Synthesis, Spectral, and Antimicrobial Studies of Cobalt, Nickel, Copper, and Zinc Complexes of Triazole-Derived Schiff Bases

    Directory of Open Access Journals (Sweden)

    Kiran Singh

    2011-01-01

    Full Text Available A series of cobalt, nickel, copper, and zinc complexes of bidentate Schiff bases derived from the condensation reaction of 4-amino-5-mercapto-3-methyl/ethyl-1,2,4-triazole with 2,4-dichlorobenzaldehyde were synthesized and tested as antimicrobial agents. The synthesized Schiff bases and their metal complexes were characterized with the aid of elemental analyses, magnetic moment measurements, spectroscopic and thermogravimetric techniques. The presence of coordinated water in metal complexes was supported by infrared and thermal gravimetric studies. A square planar geometry was suggested for Cu(II and octahedral geometry proposed for Co(II, Ni(II, and Zn(II complexes. The Schiff bases and their metal complexes have been screened for antibacterial (Pseudomonas aeruginosa, Bacillus subtilis and antifungal activities (Aspergillus niger, A. flavus. The metal complexes exhibited significantly enhanced antibacterial and antifungal activity as compared to their simple Schiff bases.

  13. Biological Activities of Polyphenols from Grapes

    Directory of Open Access Journals (Sweden)

    Hua-Bin Li

    2010-02-01

    Full Text Available The dietary consumption of grape and its products is associated with a lower incidence of degenerative diseases such as cardiovascular disease and certain types of cancers. Most recent interest has focused on the bioactive phenolic compounds in grape. Anthocyanins, flavanols, flavonols and resveratrol are the most important grape polyphenols because they possess many biological activities, such as antioxidant, cardioprotective, anticancer, anti-inflammation, antiaging and antimicrobial properties. This review summarizes current knowledge on the bioactivities of grape phenolics. The extraction, isolation and identification methods of polyphenols from grape as well as their bioavailability and potential toxicity also are included.

  14. Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.

    Science.gov (United States)

    Décor, Anne; Grand-Maître, Chantal; Hucke, Oliver; O'Meara, Jeff; Kuhn, Cyrille; Constantineau-Forget, Léa; Brochu, Christian; Malenfant, Eric; Bertrand-Laperle, Mégan; Bordeleau, Josée; Ghiro, Elise; Pesant, Marc; Fazal, Gulrez; Gorys, Vida; Little, Michael; Boucher, Colette; Bordeleau, Sylvain; Turcotte, Pascal; Guo, Tim; Garneau, Michel; Spickler, Catherine; Gauthier, Annick

    2013-07-01

    We describe here the design, synthesis and biological evaluation of antiviral compounds acting against human rhinovirus (HRV). A series of aminothiazoles demonstrated pan-activity against the HRV genotypes screened and productive structure-activity relationships. A comprehensive investigational library was designed and performed allowing the identification of potent compounds with lower molecular weight and improved ADME profile. 31d-1, 31d-2, 31f showed good exposures in CD-1 mice. The mechanism of action was discovered to be a host target: the lipid kinase phosphatidylinositol 4-kinase III beta (PI4KIIIß). The identification of the pan-HRV active compound 31f combined with a structurally distinct literature compound T-00127-HEV1 allowed the assessment of target related tolerability of inhibiting this kinase for a short period of time in order to prevent HRV replication.

  15. Insecticidal Activity of Cyanohydrin and Monoterpenoid Compounds

    Directory of Open Access Journals (Sweden)

    Joel R. Coats

    2000-04-01

    Full Text Available The insecticidal activities of several cyanohydrins, cyanohydrin esters and monoterpenoid esters (including three monoterpenoid esters of a cyanohydrin were evaluated. Topical toxicity to Musca domestica L. adults was examined, and testing of many compounds at 100 mg/fly resulted in 100% mortality. Topical LD50 values of four compounds for M. domestica were calculated. Testing of many of the reported compounds to brine shrimp (Artemia franciscana Kellog resulted in 100% mortality at 10 ppm, and two compounds caused 100% mortality at 1 ppm. Aquatic LC50 values were calculated for five compounds for larvae of the yellow fever mosquito (Aedes aegypti (L.. Monoterpenoid esters were among the most toxic compounds tested in topical and aquatic bioassays.

  16. Ficus carica L. (Moraceae: Phytochemistry, Traditional Uses and Biological Activities

    Directory of Open Access Journals (Sweden)

    Shukranul Mawa

    2013-01-01

    Full Text Available This paper describes the botanical features of Ficus carica L. (Moraceae, its wide variety of chemical constituents, its use in traditional medicine as remedies for many health problems, and its biological activities. The plant has been used traditionally to treat various ailments such as gastric problems, inflammation, and cancer. Phytochemical studies on the leaves and fruits of the plant have shown that they are rich in phenolics, organic acids, and volatile compounds. However, there is little information on the phytochemicals present in the stem and root. Reports on the biological activities of the plant are mainly on its crude extracts which have been proven to possess many biological activities. Some of the most interesting therapeutic effects include anticancer, hepatoprotective, hypoglycemic, hypolipidemic, and antimicrobial activities. Thus, studies related to identification of the bioactive compounds and correlating them to their biological activities are very useful for further research to explore the potential of F. carica as a source of therapeutic agents.

  17. Chemistry and biology of the compounds that modulate cell migration.

    Science.gov (United States)

    Tashiro, Etsu; Imoto, Masaya

    2016-03-01

    Cell migration is a fundamental step for embryonic development, wound repair, immune responses, and tumor cell invasion and metastasis. Extensive studies have attempted to reveal the molecular mechanisms behind cell migration; however, they remain largely unclear. Bioactive compounds that modulate cell migration show promise as not only extremely powerful tools for studying the mechanisms behind cell migration but also as drug seeds for chemotherapy against tumor metastasis. Therefore, we have screened cell migration inhibitors and analyzed their mechanisms for the inhibition of cell migration. In this mini-review, we introduce our chemical and biological studies of three cell migration inhibitors: moverastin, UTKO1, and BU-4664L.

  18. Targeting Platinum Compounds : synthesis and biological activity

    NARCIS (Netherlands)

    Zutphen, Steven van

    2005-01-01

    Inspired by cisplatin, the inorganic drug discovered by Barnett Rosenberg in 1965, the research described in this thesis uses targeting ligands, or ligands varied in a combinatorial fashion, to find platinum complexes with more specific modes of action. These studies have lead to the development of

  19. Vanadium compounds biological actions and potential as pharmacological agents.

    Science.gov (United States)

    Tsiani, E; Fantus, I G

    1997-03-01

    Vanadium is an element found in low concentrations in mammals, for which a function remains to be discovered. Over the past century, vanadium compounds have been suggested anecdotally as therapeutic agents for a variety of diseases. The discovery that vanadate inhibits various enzymes, in particular protein tyrosine phosphatases, and mimics many of the biological actions of insulin suggested a potential role in the therapy of diabetes mellitus. Successful use and an enhancement of insulin sensitivity in rodents and human diabetic subjects, as well as the finding that these agents are capable of stimulating metabolic effects while bypassing the insulin receptor and the early steps in insulin action, target these agents preferentially toward type II diabetes mellitus. Long-term safety remains a major concern, as tissue accumulation and relative nonspecificity of enzyme inhibition may result in adverse effects. Continued research into mechanism of action, consequences of chronic administration, and improvement of specificity is warranted. Regardless of their ultimate success or failure as therapeutic agents, vanadium compounds continue to be useful probes of enzyme structure and function in various biological processes. (Trends Endocrinol Metab 1997;8:51-58). (c) 1997, Elsevier Science Inc.

  20. Biological properties of garlic and garlic-derived organosulfur compounds.

    Science.gov (United States)

    Iciek, Małgorzata; Kwiecień, Inga; Włodek, Lidia

    2009-04-01

    Medicinal properties of garlic (Allium sativum) have been widely known and used since ancient times till the present. Garlic enhances immune functions and has antibacterial, antifungal and antivirus activities. It is known to prevent platelet aggregation, and to have hypotensive and cholesterol- and triglyceride-lowering properties, although the latter features have been questioned. This review is focused on anticancer efficacy of Allium sativum, and attempts to explain the mechanisms of this action. Medicinal properties of garlic rely upon organosulfur compounds mostly derived from alliin. Organosulfur compounds originating from garlic inhibit carcinogen activation, boost phase 2 detoxifying processes, cause cell cycle arrest mostly in G2/M phase, stimulate the mitochondrial apoptotic pathway, increase acetylation of histones. Garlic-derived sulfur compounds influence also gap-junctional intercellular communication and participate in the development of multidrug resistance. This review presents also other little known aspects of molecular action of garlic-derived compounds, like modulation of cellular redox state, involvement in signal transduction and post-translational modification of proteins by sulfane sulfur or by formation of mixed disulfides (S-thiolation reactions).

  1. Gemini ester quat surfactants and their biological activity.

    Science.gov (United States)

    Łuczyński, Jacek; Frąckowiak, Renata; Włoch, Aleksandra; Kleszczyńska, Halina; Witek, Stanisław

    2013-03-01

    Cationic gemini surfactants are an important class of surface-active compounds that exhibit much higher surface activity than their monomeric counterparts. This type of compound architecture lends itself to the compound being easily adsorbed at interfaces and interacting with the cellular membranes of microorganisms. Conventional cationic surfactants have high chemical stability but poor chemical and biological degradability. One of the main approaches to the design of readily biodegradable and environmentally friendly surfactants involves inserting a bond with limited stability into the surfactant molecule to give a cleavable surfactant. The best-known example of such a compound is the family of ester quats, which are cationic surfactants with a labile ester bond inserted into the molecule. As part of this study, a series of gemini ester quat surfactants were synthesized and assayed for their biological activity. Their hemolytic activity and changes in the fluidity and packing order of the lipid polar heads were used as the measures of their biological activity. A clear correlation between the hemolytic activity of the tested compounds and their alkyl chain length was established. It was found that the compounds with a long hydrocarbon chain showed higher activity. Moreover, the compounds with greater spacing between their alkyl chains were more active. This proves that they incorporate more easily into the lipid bilayer of the erythrocyte membrane and affect its properties to a greater extent. A better understanding of the process of cell lysis by surfactants and of their biological activity may assist in developing surfactants with enhanced selectivity and in widening their range of application.

  2. Biological Activity of Aminophosphonic Acids and Their Short Peptides

    Science.gov (United States)

    Lejczak, Barbara; Kafarski, Pawel

    The biological activity and natural occurrence of the aminophosphonic acids were described half a century ago. Since then the chemistry and biology of this class of compounds have developed into the separate field of phosphorus chemistry. Today it is well acknowledged that these compounds possess a wide variety of promising, and in some cases commercially useful, physiological activities. Thus, they have found applications ranging from agrochemical (with the herbicides glyphosate and bialaphos being the most prominent examples) to medicinal (with the potent antihypertensive fosinopril and antiosteoporetic bisphosphonates being examples).

  3. Applications of SFC-MS to toxins and compounds of biological interest

    Energy Technology Data Exchange (ETDEWEB)

    Udseth, H.R.; Kalinoski, H.T.; Smith, R.D.

    1988-06-01

    The principal applications of supercritical fluid chromatography (SFC) are for compounds that are thermally labile, of low volatility, and of low to moderate polarity. Many compounds of biological and pharmaceutical interest are defined by these criteria. We have examined selected compounds of moderate to high molecular weight with biological activity. We have used the HFR interface with CO/sub 2/ as the mobile phase with from 2 to 5% modifier. One class of compounds potentially addressable by SFC-MS are cyclic peptides. These polar compounds require the use of polar fluid modifiers with CO/sub 2/ as the mobile phase. The ionic nature of the more hydrophilic portions of such polypeptides can sometimes be shielded, allowing solvation in supercritical fluid solvents. Cyclosporin A was successfully separated by SFC-MS using a microbore column using a 2% methanol modifier. The compound was also successfully separated with a capillary column. With the capillary column 2% 2-propanol was adequate, whereas with the microbore column more polar methanol was needed. The mass spectra were identical in both cases. We also analyzed the sodium salt of two ionic polyethers, digitoxigenin, digoxigenin, and cymarin. Results are briefly discussed. 5 refs.

  4. Monascus secondary metabolites: production and biological activity.

    Science.gov (United States)

    Patakova, Petra

    2013-02-01

    The genus Monascus, comprising nine species, can reproduce either vegetatively with filaments and conidia or sexually by the formation of ascospores. The most well-known species of genus Monascus, namely, M. purpureus, M. ruber and M. pilosus, are often used for rice fermentation to produce red yeast rice, a special product used either for food coloring or as a food supplement with positive effects on human health. The colored appearance (red, orange or yellow) of Monascus-fermented substrates is produced by a mixture of oligoketide pigments that are synthesized by a combination of polyketide and fatty acid synthases. The major pigments consist of pairs of yellow (ankaflavin and monascin), orange (rubropunctatin and monascorubrin) and red (rubropunctamine and monascorubramine) compounds; however, more than 20 other colored products have recently been isolated from fermented rice or culture media. In addition to pigments, a group of monacolin substances and the mycotoxin citrinin can be produced by Monascus. Various non-specific biological activities (antimicrobial, antitumor, immunomodulative and others) of these pigmented compounds are, at least partly, ascribed to their reaction with amino group-containing compounds, i.e. amino acids, proteins or nucleic acids. Monacolins, in the form of β-hydroxy acids, inhibit hydroxymethylglutaryl-coenzyme A reductase, a key enzyme in cholesterol biosynthesis in animals and humans.

  5. Synthesis and Biological Activity of Philanthotoxin Analogs

    Institute of Scientific and Technical Information of China (English)

    Yong An ZHANG; Ke Zhong LIU; Deng Yuan WANG; Yu Zhu WANG; Liang Jian QU; Chang Jin ZHU

    2006-01-01

    The synthesis of four analogs of philanthotoxin is described. The preliminary bioassay showed that these compounds all had good insecticidal activities, and the compound 6a had the best killing effect.

  6. Design, Synthesis and Biological Activities of Novel Benzoyl Hydrazines Containing Pyrazole

    Institute of Scientific and Technical Information of China (English)

    闫涛; 于淑晶; 刘鹏飞; 刘卓; 王宝雷; 熊丽霞; 李正名

    2012-01-01

    In search of environmentally benign compounds with high biological activity, low toxicity and low resistance, 8 novel benzoyl hydrazines containing pyrazole were designed and synthesized. All compounds were characterized by I H NMR spectra and HRMS. The preliminary results of biological activity assessment indicated that most of title compounds exhibited certain insecticidal activities against M),thimna separata Walker at 200 mg L-1 but excellent fungicidal activities against six fungus at 50 mg L-1, which were better than the control.

  7. Synthesis, crystal structure and biological activity of novel diester cyclophanes

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Pengfei; Yang, Bingqin; Fang, Xianwen; Cheng, Zhao; Yang, Meipan, E-mail: yangbq@nwu.edu.cn [Department of Chemistry, Key Laboratory of Synthetic and Natural Functional Molecule Chemistry, Northwest University, Shaanxi (China)

    2012-10-15

    A series of novel diester cyclophanes was synthesized by esterification of 1,2-benzenedicarbonyl chloride with eight different diols under high dilution conditions. The structures of the compounds were verified by elemental analysis, {sup 1}H nuclear magnetic resonance (NMR), IR spectroscopy and high resolution mass spectrometry (HRMS). The crystal structures of two compounds were characterized by single crystal X-ray diffractometry (XRD). All the new cyclophanes were evaluated for biological activities and the results showed that some of these compounds have low antibacterial or antifungal activities (author)

  8. Activity of Polyphenolic Compounds against Candida glabrata

    Directory of Open Access Journals (Sweden)

    Ricardo Salazar-Aranda

    2015-09-01

    Full Text Available Opportunistic mycoses increase the morbidity and mortality of immuno-compromised patients. Five Candida species have been shown to be responsible for 97% of worldwide cases of invasive candidiasis. Resistance of C. glabrata and C. krusei to azoles has been reported, and new, improved antifungal agents are needed. The current study was designed to evaluatethe activity of various polyphenolic compounds against Candida species. Antifungal activity was evaluated following the M27-A3 protocol of the Clinical and Laboratory Standards Institute, and antioxidant activity was determined using the DPPH assay. Myricetin and baicalein inhibited the growth of all species tested. This effect was strongest against C. glabrata, for which the minimum inhibitory concentration (MIC value was lower than that of fluconazole. The MIC values against C. glabrata for myricitrin, luteolin, quercetin, 3-hydroxyflavone, and fisetin were similar to that of fluconazole. The antioxidant activity of all compounds was confirmed, and polyphenolic compounds with antioxidant activity had the greatest activity against C. glabrata. The structure and position of their hydroxyl groups appear to influence their activity against C. glabrata.

  9. Biological Activity of Masked Endotoxin

    Science.gov (United States)

    Schwarz, Harald; Gornicec, Jan; Neuper, Theresa; Parigiani, Maria Alejandra; Wallner, Michael; Duschl, Albert; Horejs-Hoeck, Jutta

    2017-01-01

    Low endotoxin recovery (LER) is a recently discovered phenomenon describing the inability of limulus amebocyte lysate (LAL)-based assays to detect lipopolysaccharide (LPS) because of a “masking effect” caused by chelators or detergents commonly used in buffer formulations for medical products and recombinant proteins. This study investigates the masking capacities of different buffer formulations and whether masked endotoxin is biologically active. We show that both naturally occurring endotoxin as well as control standard endotoxin can be affected by LER. Furthermore, whereas masked endotoxin cannot be detected in Factor C based assays, it is still detectable in a cell-based TLR4-NF-κB-luciferase reporter gene assay. Moreover, in primary human monocytes, masked LPS induces the expression of pro-inflammatory cytokines and surface activation markers even at very low concentrations. We therefore conclude that masked LPS is a potent trigger of immune responses, which emphasizes the potential danger of masked LPS, as it may pose a health threat in pharmaceutical products or compromise experimental results. PMID:28317862

  10. Synthesis, Mass Spectrometric Studies, and Biological Evaluation of 3,5-Dimethoxyhomophthalic Acid and Related Compounds

    Institute of Scientific and Technical Information of China (English)

    GHULAM Qadeer; NASIM Hasan-rama; FAN Zhi-jin

    2007-01-01

    3,5-Dimethoxyhomophthalic acid was synthesized in four steps from 3,5-dimethoxycinnamic acid via a series of reactions including cyclization of 3-(3' ,5'-dimethoxyphenyl) propionic acid to 5,7-dimethoxy-1-indanone and oxidative decomposition of methyl-2-hydroxy-2-[ 5,7-dimethyoxy-1-oxo-1H-inden-2 (3H) -ylidene ] acetate to 3,5-dimethoxyhomophthalic acid. The synthesized compounds were characterized by elemental analysis, IR, 1H NMR, and MS. The biological evaluation experiments of 3,5-dimthoxyhomophthalic acid and the related synthesized compounds were also carried out. Naturally occurring biologically active isocoumarins were prepared in a single step by the condensation of the homophthalic acid with appropriate acid chlorides.

  11. TRIAZOLE: A POTENTIAL BIOACTIVE AGENT (SYNTHESIS AND BIOLOGICAL ACTIVITY)

    OpenAIRE

    Pandeya Surendra Nath; Pathak Ashish; Mishra Rupesh

    2011-01-01

    Azoles belong to very important class of Antimicrobial drugs. Triazole is very important Azole which exists in two isomeric forms namely 1, 2, 3-Triazole and 1, 2, 4-Triazole. This Review Article covers the Different approaches to synthesize Triazoles having different substitution and their different biological activity. This Review article can be useful to synthesize new compounds having Triazole nucleolus.

  12. ANTIMICROBIAL ACTIVITY OF DIFFERENT THIOSEMICARBAZONE COMPOUNDS AGAINST MICROBIAL PATHOGENS

    Directory of Open Access Journals (Sweden)

    Negi Parul

    2012-05-01

    Full Text Available Thiosemicarbazone belongs to a large group of thiourea derivatives, whose biological activities are a function of parent aldehyde or ketone moiety. They have been evaluated over the last 50 year as antiviral, antibacterial, antifungal, antimalarial, anticancer, leprosy, rheumatism, trypanosomiasis and coccidiodis. Thiosemicarbazones were prepared by simple process in which N4-thiosemicarbazone moiety was replaced by aliphatic, arylic and cyclic amines. Present study reported the anti-microbial activity of different thiosemicarbazone compounds against certain bacterial and fungal pathogens viz. Bacillus cereus, Staphylococcus epidermis, Moraxella cattarhalis, Staph. Saprophyticus, Candida albicans and Aspergillus flavans.

  13. Physicochemical Mechanisms of Synergistic Biological Action of Combinations of Aromatic Heterocyclic Compounds

    Directory of Open Access Journals (Sweden)

    Maxim P. Evstigneev

    2013-01-01

    Full Text Available The mechanisms of synergistic biological effects observed in the simultaneous use of aromatic heterocyclic compounds in combination are reviewed, and the specific biological role of heteroassociation of aromatic molecules is discussed.

  14. Biological technologies for the removal of sulfur containing compounds from waste streams: bioreactors and microbial characteristics.

    Science.gov (United States)

    Li, Lin; Zhang, Jingying; Lin, Jian; Liu, Junxin

    2015-10-01

    Waste gases containing sulfur compounds, such as hydrogen sulfide, sulfur dioxide, thioethers, and mercaptan, produced and emitted from industrial processes, wastewater treatment, and landfill waste may cause undesirable issues in adjacent areas and contribute to atmospheric pollution. Their control has been an area of concern and research for many years. As alternative to conventional physicochemical air pollution control technologies, biological treatment processes which can transform sulfur compounds to harmless products by microbial activity, have gained in popularity due to their efficiency, cost-effectiveness and environmental acceptability. This paper provides an overview of the current biological techniques used for the treatment of air streams contaminated with sulfur compounds as well as the advances made in the past year. The discussion focuses on bioreactor configuration and design, mechanism of operation, insights into the overall biological treatment process, and the characterization of the microbial species present in bioreactors, their populations and their interactions with the environment. Some bioreactor case studies are also introduced. Finally, the perspectives on future research and development needs in this research area were also highlighted.

  15. Antitumor activity of chemical modified natural compounds

    Directory of Open Access Journals (Sweden)

    Marilda Meirelles de Oliveira

    1991-01-01

    Full Text Available Search of new activity substances starting from chemotherapeutic agents, continously appears in international literature. Perhaps this search has been done more frequently in the field of anti-tumor chemotherapy on account of the unsuccess in saving advanced stage patients. The new point in this matter during the last decade was computer aid in planning more rational drugs. In near future "the accessibility of supercomputers and emergence of computer net systems, willopen new avenues to rational drug design" (Portoghese, P. S. J. Med. Chem. 1989, 32, 1. Unknown pharmacological active compounds synthetized by plants can be found even without this eletronic devices, as tradicional medicine has pointed out in many contries, and give rise to a new drug. These compounds used as found in nature or after chemical modifications have produced successful experimental medicaments as FAA, "flavone acetic acid" with good results as inibitors of slow growing animal tumors currently in preclinical evaluation for human treatment. In this lecture some international contributions in the field of chemical modified compounds as antineoplasic drugs will be examined, particularly those done by Brazilian researches.

  16. Secondary Metabolites from Inula britannica L. and Their Biological Activities

    Directory of Open Access Journals (Sweden)

    Yoon-Ha Kim

    2010-03-01

    Full Text Available Inula britannica L., family Asteraceae, is used in traditional Chinese and Kampo Medicines for various diseases. Flowers or the aerial parts are a rich source of secondary metabolites. These consist mainly of terpenoids (sesquiterpene lactones and dimmers, diterpenes and triterpenoids and flavonoids. The isolated compounds have shown diverse biological activities: anticancer, antioxidant, anti-inflammatory, neuroprotective and hepatoprotective activities. This review provides information on isolated bioactive phytochemicals and pharmacological potentials of I. britannica.

  17. Synthesis Characterization and Biological Activities of Coordination Compounds of 4-Hydroxy-3-nitro-2H-chromen-2-one and Its Aminoethanoic Acid and Pyrrolidine-2-carboxylic Acid Mixed Ligand Complexes

    Science.gov (United States)

    Akinkunmi, Ezekiel; Obuotor, Efere; Olawuni, Idowu; Isabirye, David; Jordaan, Johan

    2017-01-01

    Coordination compounds of 4-hydroxy-3-nitro-2H-chromen-2-one and their mixed ligand complexes with aminoethanoic acid and pyrrolidine-2-carboxylic acid were synthesized by the reaction of Cu(II) and Zn(II) salts in molar ratio 1 : 2 for the coumarin complexes and 1 : 1 : 1 for the mixed ligand complexes, in basic media. The compounds formed were characterized using infrared, Uv-vis spectrophotometric analyses, mass spectrometry, magnetic susceptibility measurements, and EDX analyses. It was concluded that 4-hydroxy-3-nitro-2H-chromen-2-one coordinated as a monobasic ligand for all the complexes; it also coordinated via the carbonyl moiety in the case of the Cu(II) mixed ligand complexes. Similarly it was proposed that the amino acids also coordinated in a bidentate fashion via their amino nitrogen and carboxylate oxygen atoms. The synthesized compounds were screened for their antimicrobial and cytotoxic activities. The complexes exhibited marginal antimicrobial activity but good cytotoxic activity. PMID:28270743

  18. Synthesis, structure and biological properties of active spirohydantoin derivatives

    Directory of Open Access Journals (Sweden)

    Lazić Anita M.

    2016-01-01

    Full Text Available Spirohidantoins represent an pharmacologically important class of heterocycles since many derivatives have been recognized that display interesting activities against a wide range of biological targets. First synthesis of cycloalkanespiro-5-hydantoins was performed by Bucherer and Lieb 1934 by the reaction of cycloalkanone, potassium cyanide and ammonium-carbonate at reflux in a mixture of ethanol and water. QSAR (Quantitative Structure-Activity Relationship studies showed that a wide range of biological activities of spirohydantoin derivatives strongly depend upon their structure. This paper describes different methods of synthesis of spirohydantoin derivatives, their physico-chemical properties and biological activity. It emphasizes the importance of cycloalkanespiro-5-hydantoins with anticonvulsant, antiproliferative, antipsychotic, antimicrobial and antiinflammatory properties as well as their importance in the treatment of diabetes. Numerous spirohydantoin compounds exhibit physiological activity such as serotonin and fibrinogen antagonist, inhibitors of the glycine binding site of the NMDA receptor also, antagonist of leukocyte cell adhesion, acting as allosteric inhibitors of the protein-protein interactions. Some spirohydantoin derivatives have been identified as antitumor agents. Their activity depends on the substituent presented at position N-3 of the hydantoin ring and increases in order alkene > ester > ether. Besides that, compounds that contain two electron withdrawing groups (e.g. fluorine or chlorine on the third and fourth position of the phenyl ring are better antitumor agents than compounds with a single electron withdrawing group. [Projekat Ministarstva nauke Republike Srbije, br. 172013

  19. Anti-allergic activity of compounds from Boesenbergia thorelii

    Directory of Open Access Journals (Sweden)

    Supinya Tewtrakul

    2013-04-01

    Full Text Available Boesenbergia thorelii extract of rhizomes and its compounds were investigated for anti-allergic activities usingantigen-induced -hexosaminidase release in RBL-2H3 cells. From bioassay-guided fractionation, the chloroform fraction wasseparated to afford four compounds: asaronaldehyde (1, -sitosterol-D-glucoside (2, protocatechuic acid methyl ester (3and 2-hydroxy-1-(3, 4-dimethoxyphenyl ethanols (4. Their structures were elucidated on the basis of UV, IR and NMRspectroscopic data. Of these, compound 1 (asaronaldehyde was the most active with an IC50 value of 24.3 µM, followed by2 (IC50 = 63.3 µM and 4 (IC50 = 72.6 µM; whereas compound 3 was inactive (IC50 > 100µM. Anti-allergic effect of 1 (IC50 =24.3 µM was higher than that of ketotifen fumarate (IC50 = 41.1 µM, the positive control. This study may support the useof B. thorelii for treatment of allergy-related diseases. Moreover, this is the first report on biological study and chemicalconstituents of B. thorelii.

  20. Distribution and biological turnover of dissolved organic compounds in the water column of the Black Sea

    Science.gov (United States)

    Mopper, Kenneth; Kieber, David J.

    Water column concentrations and turnover rates were determined for a suite of low molecular weight organic compounds in the Black Sea. The classes of compounds studied included amino acids, simple sugars, α-keto acids, aldehydes, ketones, carboxylic acids, flavins and thiols. Our study yielded some new insights, as well as a few surprising discoveries, regarding the composition and cycling of organic matter in the Black Sea. (1) Uptake rates of organic compounds were from 2 to 4640 times faster in oxic surface waters than in anoxic waters. (2) Sharp maxima or minima in concentrations of organic compounds coincided with zones of enhanced microbial activities, especially in the vicinity of the oxic-suboxic and suboxic-anoxic interfaces. (3) The benthic boundary layer, 300-400 m thick, had a markedly different organic composition and substantially higher concentrations of organic acids, and to a lesser extent sugars and thiols, than the overlying water. (4) A dramatic change in the composition and concentration of dissolved free amino acids occurred in the water column during the cruise and appeared to be related to biological patchiness. (5) Organic thiols constituted a significant portion (e.g. 10-20%) of the total reduced sulfur near the top of the sulfidic zone, and may contribute to the origin of hydrogen sulfide in this zone. (6) Major unknown amine and carbonyl compounds were discovered in the anoxic zone, providing evidence that the Black Sea contains unique anaerobic bacteria with possibly new biochemical pathways.

  1. Pharmacologically active compounds in the environment and their chirality.

    Science.gov (United States)

    Kasprzyk-Hordern, Barbara

    2010-11-01

    Pharmacologically active compounds including both legally used pharmaceuticals and illicit drugs are potent environmental contaminants. Extensive research has been undertaken over the recent years to understand their environmental fate and toxicity. The one very important phenomenon that has been overlooked by environmental researchers studying the fate of pharmacologically active compounds in the environment is their chirality. Chiral drugs can exist in the form of enantiomers, which have similar physicochemical properties but differ in their biological properties such as distribution, metabolism and excretion, as these processes (due to stereospecific interactions of enantiomers with biological systems) usually favour one enantiomer over the other. Additionally, due to different pharmacological activity, enantiomers of chiral drugs can differ in toxicity. Furthermore, degradation of chiral drugs during wastewater treatment and in the environment can be stereoselective and can lead to chiral products of varied toxicity. The distribution of different enantiomers of the same chiral drug in the aquatic environment and biota can also be stereoselective. Biological processes can lead to stereoselective enrichment or depletion of the enantiomeric composition of chiral drugs. As a result the very same drug might reveal different activity and toxicity and this will depend on its origin and exposure to several factors governing its fate in the environment. In this critical review a discussion of the importance of chirality of pharmacologically active compounds in the environmental context is undertaken and suggestions for directions in further research are made. Several groups of chiral drugs of major environmental relevance are discussed and their pharmacological action and disposition in the body is also outlined as it is a key factor in developing a full understanding of their environmental occurrence, fate and toxicity. This review will be of interest to environmental

  2. BIOLOGICAL ACTIVITIES OF OXAZINE AND ITS DERIVATIVES: A REVIEW

    Directory of Open Access Journals (Sweden)

    SINDHU T J

    2014-12-01

    Full Text Available Oxazine derivatives are an important class of heterocycles, which has attracted much synthetic interest due to their wide range of biological activities. Oxazine is a heterocyclic compound can be formally derived from benzene, and its reduction products, by suitable substitution of carbon (and hydrogen atoms by nitrogen and oxygen. In the last few years oxazine derivatives have proved to be valuable synthetic intermediates and also possess important biological activities like sedative, analgesic, antipyretic, anticonvulsant, antitubercular, antitumour, antimalarial and antimicrobial. In these days, development of drug resistance is a major problem and to overcome this situation, it is necessary to synthesize new classes of compounds. The aim of the article is to review the generalization of the collected data about the synthesis of oxazine derivatives and their activities. We hope that this work will be a definite interest for researchers concerned with azines in generally and oxazines in particular.

  3. Sulfation and biological activities of konjac glucomannan.

    Science.gov (United States)

    Bo, Surina; Muschin, Tegshi; Kanamoto, Taisei; Nakashima, Hideki; Yoshida, Takashi

    2013-05-15

    The sulfation of konjac glucomannan and its anti-HIV and blood anticoagulant activities were investigated. Konjac glucomannan is a polysaccharide occurring naturally in konjac plant tubers and has high molecular weights. Solubility in water is very low, and the aqueous solutions at low concentrations have high viscosity. Before sulfation, hydrolysis by diluted sulfuric acid was carried out to decrease the molecular weights of M¯n=19.2 × 10(4)-0.2 × 10(4). Sulfation with piperidine-N-sulfonic acid or SO3-pyridine complex gave sulfated konjac glucomannans with molecular weights of M¯n=1.0 × 10(4)-0.4 × 10(4) and degrees of sulfation (DS) of 1.3-1.4. It was found that the sulfated konjac glucomannans had potent anti-HIV activity at a 50% effective concentration, (EC50) of 1.2-1.3 μg/ml, which was almost as high as that of an AIDS drug, ddC, whose EC50=3.2 μg/ml, and moderate blood anticoagulant activity, AA=0.8-22.7 units/mg, compared to those of standard sulfated polysaccharides, curdlan (10 units/mg) and dextran (22.7 units/mg) sulfates. Structural analysis of sulfated konjac glucomannans with negatively charged sulfated groups was performed by high resolution NMR, and the interaction between poly-l-lysine with positively charged amino groups as a model compound of proteins and peptides was measured by surface plasmon resonance measurement, suggesting that the sulfated konjac glucomannans had a high binding stability on immobilized poly-l-lysine. The binding of sulfated konjac glucomannan was concentration-dependent, and the biological activity of the sulfated konjac glucomannans may be due to electrostatic interaction between the sulfate and amino groups.

  4. Sulfur-centered reactive intermediates derived from the oxidation of sulfur compounds of biological interest

    Energy Technology Data Exchange (ETDEWEB)

    Abedinzadeh, Z. [Lab. de Chimie Physique, UMR, Univ. Rene Descartes, Paris (France)

    2001-02-01

    Sulphur compounds play a central role in the structure and activity of many vital systems. In the living cell, sulfur constitutes an essential part of the defense against oxidative damage and is transformed into a variety of sulfur free radical species. Many studies of the chemistry of sulfur-centered radicals using pulse radiolysis and photolysis techniques to detect and measure the kinetics of these radicals have been published and reviewed. This paper discusses the present state of research on the formation and reactivity of certain sulfur-centered radicals [RS{sup .}, RSS{sup .}, RS{sup .+}, (RSSR){sup .+}] and their implications for biological systems. (author)

  5. Syntheses, Characterization, Resolution, and Biological Studies of Coordination Compounds of Aspartic Acid and Glycine.

    Science.gov (United States)

    Aiyelabola, Temitayo; Akinkunmi, Ezekiel; Ojo, Isaac; Obuotor, Efere; Adebajo, Clement; Isabirye, David

    2017-01-01

    Enantiomerically enriched coordination compounds of aspartic acid and racemic mixtures of coordination compounds of glycine metal-ligand ratio 1 : 3 were synthesized and characterized using infrared and UV-Vis spectrophotometric techniques and magnetic susceptibility measurements. Five of the complexes were resolved using (+)-cis-dichlorobis(ethylenediamine)cobalt(III) chloride, (+)-bis(glycinato)(1,10-phenanthroline)cobalt(III) chloride, and (+)-tris(1,10-phenanthroline)nickel(II) chloride as resolving agents. The antimicrobial and cytotoxic activities of these complexes were then determined. The results obtained indicated that aspartic acid and glycine coordinated in a bidentate fashion. The enantiomeric purity of the compounds was in the range of 22.10-32.10%, with (+)-cis-dichlorobis(ethylenediamine)cobalt(III) complex as the more efficient resolving agent. The resolved complexes exhibited better activity in some cases compared to the parent complexes for both biological activities. It was therefore inferred that although the increase in the lipophilicity of the complexes may assist in the permeability of the complexes through the cell membrane of the pathogens, the enantiomeric purity of the complexes is also of importance in their activity as antimicrobial and cytotoxic agents.

  6. Syntheses, Characterization, Resolution, and Biological Studies of Coordination Compounds of Aspartic Acid and Glycine

    Science.gov (United States)

    Akinkunmi, Ezekiel; Ojo, Isaac; Adebajo, Clement; Isabirye, David

    2017-01-01

    Enantiomerically enriched coordination compounds of aspartic acid and racemic mixtures of coordination compounds of glycine metal-ligand ratio 1 : 3 were synthesized and characterized using infrared and UV-Vis spectrophotometric techniques and magnetic susceptibility measurements. Five of the complexes were resolved using (+)-cis-dichlorobis(ethylenediamine)cobalt(III) chloride, (+)-bis(glycinato)(1,10-phenanthroline)cobalt(III) chloride, and (+)-tris(1,10-phenanthroline)nickel(II) chloride as resolving agents. The antimicrobial and cytotoxic activities of these complexes were then determined. The results obtained indicated that aspartic acid and glycine coordinated in a bidentate fashion. The enantiomeric purity of the compounds was in the range of 22.10–32.10%, with (+)-cis-dichlorobis(ethylenediamine)cobalt(III) complex as the more efficient resolving agent. The resolved complexes exhibited better activity in some cases compared to the parent complexes for both biological activities. It was therefore inferred that although the increase in the lipophilicity of the complexes may assist in the permeability of the complexes through the cell membrane of the pathogens, the enantiomeric purity of the complexes is also of importance in their activity as antimicrobial and cytotoxic agents. PMID:28293149

  7. EVALUATION OF BIOLOGICALLY ACTIVE MOLECULES ISOLATED FROM OBLIGATE MARINE FUNGI

    Directory of Open Access Journals (Sweden)

    A. KRISHNA SATYA

    2013-01-01

    Full Text Available The marine environment is a tremendous source of natural products. Marine microorganisms have become an important source of pharmacologically active metabolites Fungi are well known for their vast diversity of secondary metabolites that include many life-saving drugs and highly toxic mycotoxins. In general, fungal cultures producing such metabolites are immune to their toxic effects. However, some are known to produce self-toxic compounds that can pose production optimization challenges if the metabolites are needed in large amounts for chemical modification. Objective: The main objective of the present study was the isolation of new and preferably biologically active secondary metabolites from marine microorganisms, especially marine-derived fungi. Method: Marine fungi had isolated from marine soil by serial dilution method from Rose Bengal medium. Single colony was isolated by microscopic and macroscopic observation. Secondary metabolites are produced by marine fungi. Biological evaluation was performed by microbial studies. TLC is performed to identify the number of sub compounds in the crude extract. Further species level identification and structure elucidation of the compound are to be done. Results: The isolated marine fungi Aspergillus sp, showed maximum activity against the Candida rugosa with a zone diameter of 16mm at a concentration of 200μg and for bacterial strains it showed maximum activity against the E.coli with a diameter of 24mm at a concentration of 200μg. From the thin layer chromatography it has nearly 2-3 compounds to be purified. Conclusion: The selected organism which produces the compounds contains the biological activities which include anti-bacterial and anti fungal activities.

  8. Carbon Nanomaterials Based Electrochemical Sensors/Biosensors for the Sensitive Detection of Pharmaceutical and Biological Compounds

    Directory of Open Access Journals (Sweden)

    Bal-Ram Adhikari

    2015-09-01

    Full Text Available Electrochemical sensors and biosensors have attracted considerable attention for the sensitive detection of a variety of biological and pharmaceutical compounds. Since the discovery of carbon-based nanomaterials, including carbon nanotubes, C60 and graphene, they have garnered tremendous interest for their potential in the design of high-performance electrochemical sensor platforms due to their exceptional thermal, mechanical, electronic, and catalytic properties. Carbon nanomaterial-based electrochemical sensors have been employed for the detection of various analytes with rapid electron transfer kinetics. This feature article focuses on the recent design and use of carbon nanomaterials, primarily single-walled carbon nanotubes (SWCNTs, reduced graphene oxide (rGO, SWCNTs-rGO, Au nanoparticle-rGO nanocomposites, and buckypaper as sensing materials for the electrochemical detection of some representative biological and pharmaceutical compounds such as methylglyoxal, acetaminophen, valacyclovir, β-nicotinamide adenine dinucleotide hydrate (NADH, and glucose. Furthermore, the electrochemical performance of SWCNTs, rGO, and SWCNT-rGO for the detection of acetaminophen and valacyclovir was comparatively studied, revealing that SWCNT-rGO nanocomposites possess excellent electrocatalytic activity in comparison to individual SWCNT and rGO platforms. The sensitive, reliable and rapid analysis of critical disease biomarkers and globally emerging pharmaceutical compounds at carbon nanomaterials based electrochemical sensor platforms may enable an extensive range of applications in preemptive medical diagnostics.

  9. Biologically active secondary metabolites from Asphodelus microcarpus.

    Science.gov (United States)

    Ghoneim, Mohammed M; Ma, Guoyi; El-Hela, Atef A; Mohammad, Abd-Elsalam I; Kottob, Saeid; El-Ghaly, Sayed; Cutler, Stephen J; Ross, Samir A

    2013-08-01

    Bioassay guided fractionation of the ethanolic extract of Asphodelus microcarpus Salzm.et Vivi (Asphodelaceae) resulted in the isolation of one new metabolite, 1,6-dimethoxy-3-methyl-2-naphthoic acid (1) as well as nine known compounds: asphodelin (2), chrysophanol (3), 8-methoxychrysophanol (4), emodin (5), 2-acetyl-1,8-dimethoxy-3-methylnaphthalene (6), 10-(chrysophanol-7'-yl)-10-hydroxychrysophanol-9-anthrone (7), aloesaponol-III-8-methyl ether (8), ramosin (9) and aestivin (10). The compounds were identified by 1D and 2D NMR and HRESIMS. Compounds 3, 6 and 10 were isolated for the first time from this species. Compounds 3 and 4 showed moderate to weak antileishmanial activity with IC50 values of 14.3 and 35.1 microg/mL, respectively. Compound 4 exhibited moderate antifungal activity against Cryptococcus neoformans with an IC50 value of 15.0 microg/mL, while compounds 5, 7 and 10 showed good to potent activity against methicillin resistant Staphylococcus aureus (MRSA) with IC50 values of 6.6, 9.4 microg/mL and 1.4 microg/mL respectively. Compounds 5, 8 and 9 displayed good activity against S. aureus with IC50 values of 3.2, 7.3 and 8.5 microg/mL, respectively. Compounds 7 and 9 exhibited a potent cytotoxic activity against leukemia LH60 and K562 cell lines. Compound 10 showed potent antimalarial activities against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with IC50 values in the range of 0.8-0.7 microg/mL without showing any cytotoxicity to mammalian cells.

  10. Biological and chemical investigation of Allium cepa L. response to selenium inorganic compounds.

    Science.gov (United States)

    Michalska-Kacymirow, M; Kurek, E; Smolis, A; Wierzbicka, M; Bulska, E

    2014-06-01

    The aim of this study was to evaluate the biological and chemical response of Allium cepa L. exposed to inorganic selenium compounds. Besides the investigation of the total content of selenium as well as its chemical speciation, the Allium test was used to evaluate the growth of onion roots and mitotic activity in the roots' meristem. The total content of selenium was determined by inductively coupled plasma mass spectrometry (ICP MS). High-performance liquid chromatography (HPLC), coupled to ICP MS, was used for the selenium chemical speciation. Results indicated that A. cepa plants are able to biotransform inorganic selenium compounds into their organic derivatives, e.g., Se-methylselenocysteine from the Se(IV) inorganic precursor. Although the differences in the biotransformation of selenium are due mainly to the oxidation state of selenium, the experiment has also shown a fine effect of counter ions (H(+), Na(+), NH4 (+)) on the response of plants and on the specific metabolism of selenium.

  11. Biological Activities of Oleanolic Acid Derivatives from Calendula officinalis Seeds.

    Science.gov (United States)

    Zaki, Ahmed; Ashour, Ahmed; Mira, Amira; Kishikawa, Asuka; Nakagawa, Toshinori; Zhu, Qinchang; Shimizu, Kuniyoshi

    2016-05-01

    Phytochemical examination of butanol fraction of Calendula officinalis seeds led to the isolation of two compounds identified as 28-O-β-D-glucopyranosyl-oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS1) and oleanolic acid 3-O-β-D-glucopyranosyl (1→3)-β-D-glucopyranosiduronic acid (CS2). Biological evaluation was carried out for these two compounds such as melanin biosynthesis inhibitory, hyaluronic acid production activities, anti obesity using lipase inhibition and adipocyte differentiation as well as evaluation of the protective effect against hydrogen peroxide induced neurotoxicity in neuro-2A cells. The results showed that, compound CS2 has a melanin biosynthesis stimulatory activity; however, compound CS1 has a potent stimulatory effect for the production of hyaluronic acid on normal human dermal fibroblast from adult (NHDF-Ad). Both compounds did not show any inhibitory effect on both lipase and adipocyte differentiation. Compound CS2 could protect neuro-2A cells and increased cell viability against H2 O2 . These activities (melanin biosynthesis stimulatory and protective effect against H2 O2 of CS2 and hyaluronic acid productive activities of these triterpene derivatives) have been reported for the first time. Copyright © 2016 John Wiley & Sons, Ltd.

  12. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF SOME NOVEL ARYL AND HETROARYL CHALCONE ANALOGUES

    Directory of Open Access Journals (Sweden)

    Tribhuvan Singh

    2012-07-01

    Full Text Available A new series of Heterocyclic chalcones showed diversified biological activities. In view of potential biological activities of Heterocyclic chalcones derivative were prepared by claisen-Schmidt condensation technique. The compound were screened for anti-inflammatory and antibacterial activity.

  13. BIOLOGICALLY ACTIVE SUBSTANCES OF SPIRIT PRODUCTION WASTE

    Directory of Open Access Journals (Sweden)

    A. S. Kayshev

    2014-01-01

    Full Text Available A content of biologically active compounds (BAC with signified pharmacological activity in distillers grains was proved. It is prospective for applications of these grains as a raw material resource of pharmaceuticals. A composition of BAC distillers grains received from wheat, corn, barley, millet at different spirit enterprises which use hydro fermentative grain processing. Considering polydispersity of distillers grains they were separated on solid and liquid phases preliminary. Physical and chemical characteristics of distillers grains' liquid base were identified. Elementary composition of distillers grains is signified by active accumulation of biogenic elements (phosphorus, potassium, magnesium, calcium, sodium, iron and low content of heavy metals. The solid phase of distillers grains accumulates carbon, hydrogen and nitrogen in high concentration. The liquid phase of distillers grains contains: proteins and amino acids (20-46%, reducing sugars (5,6%-17,5%, galacturonides (0,8-1,4%, ascorbic acid (6,2-11,4 mg%. The solid base of distillers grains contains: galacturonides (3,4-5,3%, fatty oil (8,4-11,1% with predomination of essential fatty acids, proteins and amino acids (2,1-2,5%, flavonoids (0,4-0,9%, tocopherols (3,4-7,7 mg%. A method of complex processing of distillers grains based on application of membrane filtering of liquid phase and liquid extraction by inorganic and organic solvents of solid phase, which allows almost full extraction of the sum of biologically active compounds (BAC from liquid phase (Biobardin BM and solid phase (Biobardin UL. Biobardin BM comprises the following elements: proteins and amino acids (41-69%, reducing sugars (3,5-15,6%, fatty oil (0,2-0,3%, flavonoids (0,2-0,7%, ascorbic acid (17-37 mg%. Biobardin UL includes: oligouronids (16,4-19,5%, proteins and amino acids (11-21%, fatty oil (3,2-4,9% which includes essential acids; flavonoids (0,6-1,5%, tocopherols (6,6-10,2 mg%, carotinoids (0,13-0,21 mg

  14. Biological activities and medicinal properties of Gokhru (Pedalium murex L.)

    Institute of Scientific and Technical Information of China (English)

    V Rajashekar; E Upender Rao; Srinivas P

    2012-01-01

    Bada Gokhru (Pedalium murex L.) is perhaps the most useful traditional medicinal plant in India. Each part of the neem tree has some medicinal property and is thus commercially exploitable. During the last five decades, apart from the chemistry of the Pedalium murex compounds, considerable progress has been achieved regarding the biological activity and medicinal applications of this plant. It is now considered as a valuable source of unique natural products for development of medicines against various diseases and also for the development of industrial products. This review gives a bird’s eye view mainly on the biological activities of some of this compounds isolated, pharmacological actions of the extracts, clinical studies and plausible medicinal applications of gokharu along with their safety evaluation.

  15. Synthesis and biological evaluation of biaryl analogs of antitubulin compounds

    Directory of Open Access Journals (Sweden)

    Camila Santos Suniga Tozatti

    2012-01-01

    Full Text Available This paper reports the synthesis of methanones and esters bearing different substitution patterns as spacer groups between aromatic rings. This series of compounds can be considered phenstatin analogs. Two of the newly synthesized compounds, 5a and 5c, strongly inhibited tubulin polymerization and the binding of [³H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site.

  16. Synthesis and biological evaluation of biaryl analogs of antitubulin compounds

    Energy Technology Data Exchange (ETDEWEB)

    Tozatti, Camila Santos Suniga; Khodyuk, Rejane Goncalves Diniz; Silva, Adriano Olimpio da; Santos, Edson dos Anjos dos; Amaral, Marcos Serrou do; Lima, Denis Pires de, E-mail: denis.lima@ufms.br [Centro de Ciencias Exatas e Tecnologia, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Hamel, Ernest [Screening Technologies Branch, Division of Cancer Treatment and Diagnosis, National Cancer Institute at Frederick, MD (United States)

    2012-07-01

    This paper reports the synthesis of methanones and esters bearing different substitution patterns as spacer groups between aromatic rings. This series of compounds can be considered phenstatin analogs. Two of the newly synthesized compounds, 5a and 5c, strongly inhibited tubulin polymerization and the binding of [{sup 3}H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site. (author)

  17. Creatinyl amino acids: new hybrid compounds with neuroprotective activity.

    Science.gov (United States)

    Burov, Sergey; Leko, Maria; Dorosh, Marina; Dobrodumov, Anatoliy; Veselkina, Olga

    2011-09-01

    Prolonged oral creatine administration resulted in remarkable neuroprotection in experimental models of brain stroke. However, because of its polar nature creatine has poor ability to penetrate the blood-brain barrier (BBB) without specific creatine transporter (CRT). Thus, synthesis of hydrophobic derivatives capable of crossing the BBB by alternative pathway is of great importance for the treatment of acute and chronic neurological diseases including stroke, traumatic brain injury and hereditary CRT deficiency. Here we describe synthesis of new hybrid compounds-creatinyl amino acids, their neuroprotective activity in vivo and stability to degradation in different media. The title compounds were synthesized by guanidinylation of corresponding sarcosyl peptides or direct creatine attachment using isobutyl chloroformate method. Addition of lipophilic counterion (p-toluenesulfonate) ensures efficient creatine dissolution in DMF with simultaneous protection of guanidino group towards intramolecular cyclization. It excludes the application of expensive guanidinylating reagents, permits to simplify synthetic procedure and adapt it to large-scale production. The biological activity of creatinyl amino acids was tested in vivo on ischemic stroke and NaNO(2) -induced hypoxia models. One of the most effective compounds-creatinyl-glycine ethyl ester increases life span of experimental animals more than two times in hypoxia model and has neuroprotective action in brain stroke model when applied both before and after ischemia. These data evidenced that creatinyl amino acids can represent promising candidates for the development of new drugs useful in stroke treatment.

  18. Recent progress in biological activities of synthesized phenothiazines.

    Science.gov (United States)

    Pluta, Krystian; Morak-Młodawska, Beata; Jeleń, Małgorzata

    2011-08-01

    This review summarizes recent medicinal chemistry investigations in vitro and in vivo in search for new phenothiazines of promising biological activities. New phenothiazine derivatives (over 50 main structures) contain dialkylaminoalkyl, cycloaminoalkyl and aminoalkyl substituents and their acyl and sulfonyl derivatives, and other substituents with varied the monocyclic (pyrazole, thiazole, oxadiazole, thiadiazole, tetrazole) and bicyclic (quinolizine, pyrazolopyrimidine, thiazolopyridine, azabicyclononane and spiro[chromanpyrimidine] heterocycles linked directly or via the alkyl chain with the thiazine nitrogen atom or with the benzene ring. The modifications of the tricyclic ring system with the bicyclic homoaromatic ring (naphthalene) and monocyclic and bicyclic azine rings (pyridine, pyrimidine, pyrazine and quinoline) led to compounds of significant biological activities. Recently obtained phenothiazines exhibit promising antibacterial, antifungal, anticancer, antiviral, anti-inflammatory, antimalarial, antifilarial, trypanocidal, anticonvulsant, analgesic, immunosuppressive and multidrug resistance reversal properties. These activities were the results of the actions of phenothiazines on biological systems via the interaction of the pharmacophoric substituent (in some cases of strict length), via the interaction of the multicyclic ring system (π-π interaction, intercalation in DNA) and via the lipophilic character allowing the penetration through the biological membranes. The activities were examined by using various biological systems such as cell lines, bacteria, viruses, parasites, laboratory mice, rats and rabbits, and monolayer and bilayer membranes. Some mechanisms of the actions are discussed. This review shows current tendency in the phenothiazine synthesis (without synthetic routes) and reveals the phenothiazine core to be very potent pharmacophoric moiety which can be a rich source of new compounds having desirable biological activities.

  19. Biological activity of liposomal vanillin.

    Science.gov (United States)

    Castan, Leniher; Del Toro, Grisel; Fernández, Adolfo A; González, Manuel; Ortíz, Emilia; Lobo, Daliana

    2013-06-01

    This article presents a study of vanillin encapsulation inside multilamellar liposomes, with emphasis on the evaluation of antioxidant activity, the hemolytic effect, and the antisickling properties of these products. Egg phosphatidylcholine-cholesterol and egg phosphatidylcholine-cholesterol-1-O-decylglycerol liposomes were prepared by mechanical dispersion, all with vanillin included. Vesicles were characterized by determination of encapsulation efficiency and vanillin retention capacity. Antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The hemolytic effect of liposomes was also evaluated by spectrophotometry, as well as the antisickling activity by the Huck test using optical microscopy. Results showed that the lipid composition of liposomes did not significantly affect the encapsulation efficiency. Stable vesicles were obtained with a high retention percentage of vanillin. Liposomes exhibited a high capture of the DPPH radical compared to free vanillin and 1-O-decylglycerol (C10) in solution. Vesicles caused no significant hemolisys in normal erythrocytes, nor in those coming from patients with sickle cell anemia. Vanillin encapsulated in liposomes retained its antisickling activity, with a greater effect for C10-containing vesicles. Our results show that vanillin encapsulation in liposomes is a way to enhance the pharmacologic properties of this molecule using a suitable vehicle.

  20. Relationship between Zingiberaceae Leaves Compounds and its Tyrosinase Activity

    Directory of Open Access Journals (Sweden)

    Irmanida Batubara

    2016-11-01

    Full Text Available The leaves of Zingiberaceae family has not been much explored its potential, especially as a skin lightening. The relationship between total anthocyanins, chlorophyll, carotenoids and tannins contents of Zingiberaceae leaves and tyrosinase activity were determined. Ten species of Zingiberaceae were separated by n-hexane and the residues were extracted with ethyl acetate. The total anthocyanins, chlorophyll, carotenoids, tannins contents and the activities of ethyl acetate extracts were determined by spectrometric method. The tyrosinase inhibition was determined by using L-tyrosine (monophenolase and L-DOPA (diphenolase substrates. The most active extract was the leaves extract of Zingiber purpureum which exhibited 82.86% for monophenolase inhibition and the leaves extract of Curcuma zedoaria which exhibited 90.20% for diphenolase inhibition. The correlation between carotenoids content and monophenolase inhibition was 52%, while between tannin content and diphenolase inhibition was only 15%. Therefore, among 10 leaves species of Zingiberaceae, Zingiber purpureum Roscoe and Curcuma zedoaria leaves are the most potential for tyrosinase inhibitors and can be developed as whitening agent.How to CiteBatubara, I., Kartika, Y. & Darusman, L. K. (2016. Relationship between Zingiberaceae Leaves Compounds and its Tyrosinase Activity. Biosaintifika: Journal of Biology & Biology Education, 8(3, 371-377. 

  1. Production of Some Biologically Active Secondary Metabolites From Marine-derived Fungus Varicosporina ramulosa

    Directory of Open Access Journals (Sweden)

    Atalla, M. M.

    2008-01-01

    Full Text Available In a screening of fungal isolates associated with marine algae collected from Abou-keer, Alexanderia during the four seasons of 2004, to obtain new biologically active compounds. Varicosporina ramulosa isolate was identified and selected as a producer of 13 compounds. Out of 13 pure compounds produced, compounds 3 and 10 were considered as antibacterial and antifungal compounds, respectively as they were active against gram positive, gram negative bacteria and a fungus. Optimization of conditions (fermentation media, incubation period, temperature, initial pH, aeration levels which activate compounds 3 and 10 production were studied. Also the spectral properties (UV, MS, GC/MS, IR and 1H-NMR of the purified compounds were determined. Compound 3 suggested to be dibutyl phthalate and compound 10 may be ergosterol or one of its isomers. Biological evaluation of the two compounds towards 6 different types of tumor cell lines showed weak effect of compound 3 at different concentrations on the viable cell count of the different tumor cell lines. While compound 10 showed different activities against the viable cell count of the 6 different tumor cell lines. It kills 50% of the viable infected liver and lung cells at concentrations equal to 99.7 µg/mL, 74.9µg/mL, respectively. Compound 10 can be recommended as new anticancer compounds.

  2. Bioactive Components and Functional Properties of Biologically Activated Cereal Grains: A Bibliographic Review.

    Science.gov (United States)

    Singh, Arashdeep; Sharma, Savita

    2015-10-14

    Whole grains provide energy, nutrients, fibres and bioactive compounds that may synergistically contribute to their protective effects. A wide range of these compounds is affected by germination. While some compounds, such as β-glucans are degraded, others, like antioxidants and total phenolics are increased by means of biological activation of grains. The water and oil absorption capacity as well as emulsion and foaming capacity of biologically activated grains are also improved. Application of biological activation of grains is of emerging interest, which may significantly enhance the nutritional, functional and bioactive content of grains, as well as improve palatability of grain foods in a natural way. Therefore, biological activation of cereals can be a way to produce food grains enriched with health promoting compounds and enhanced functional attributes.

  3. Systems Biology based studies on anti-inflammatory compounds

    NARCIS (Netherlands)

    Verhoeckx, Kitty Catharina Maria

    2005-01-01

    The introduction of the ‘omics’ techniques (transcriptomics, proteomics, and metabolomics) and systems biology, has caused fundamental changes in the drug discovery process and many other fields in the life science area. In this thesis we explored the possibilities to apply these holistic technologi

  4. Marine Pyridoacridine Alkaloids: Biosynthesis and Biological Activities.

    Science.gov (United States)

    Ibrahim, Sabrin R M; Mohamed, Gamal A

    2016-01-01

    Pyridoacridines are a class of strictly marine-derived alkaloids that constitute one of the largest chemical families of marine alkaloids. During the last few years, both natural pyridoacridines and their analogues have constituted excellent targets for synthetic works. They have been the subject of intense study due to their significant biological activities; cytotoxic, antibacterial, antifungal, antiviral, insecticidal, anti-HIV, and anti-parasitic activities. In the present review, 95 pyridoacridine alkaloids isolated from marine organisms are discussed in term of their occurrence, biosynthesis, biological activities, and structural assignment.

  5. Grape Seed Oil Compounds: Biological and Chemical Actions for Health

    Science.gov (United States)

    Garavaglia, Juliano; Markoski, Melissa M.; Oliveira, Aline; Marcadenti, Aline

    2016-01-01

    Grape seed oil is rich in phenolic compounds, fatty acids, and vitamins, with economic importance to pharmaceutical, cosmetic, and food industry. Its use as an edible oil has also been suggested, especially due to its pleasant sensory characteristics. Grape seed oil has beneficial properties for health that are mainly detected by in vitro studies, such as anti-inflammatory, cardioprotective, antimicrobial, and anticancer properties, and may interact with cellular and molecular pathways. These effects have been related to grape seed oil constituents, mainly tocopherol, linolenic acid, resveratrol, quercetin, procyanidins, carotenoids, and phytosterols. The aim of this article was to briefly review the composition and nutritional aspects of grape seed oil, the interactions of its compounds with molecular and cellular pathways, and its possible beneficial effects on health. PMID:27559299

  6. Marine Biology Activities. Ocean Related Curriculum Activities.

    Science.gov (United States)

    Pauls, John

    The ocean affects all of our lives. Therefore, awareness of and information about the interconnections between humans and oceans are prerequisites to making sound decisions for the future. Project ORCA (Ocean Related Curriculum Activities) has developed interdisciplinary curriculum materials designed to meet the needs of students and teachers…

  7. Data-Driven Derivation of an "Informer Compound Set" for Improved Selection of Active Compounds in High-Throughput Screening.

    Science.gov (United States)

    Paricharak, Shardul; IJzerman, Adriaan P; Jenkins, Jeremy L; Bender, Andreas; Nigsch, Florian

    2016-09-26

    Despite the usefulness of high-throughput screening (HTS) in drug discovery, for some systems, low assay throughput or high screening cost can prohibit the screening of large numbers of compounds. In such cases, iterative cycles of screening involving active learning (AL) are employed, creating the need for smaller "informer sets" that can be routinely screened to build predictive models for selecting compounds from the screening collection for follow-up screens. Here, we present a data-driven derivation of an informer compound set with improved predictivity of active compounds in HTS, and we validate its benefit over randomly selected training sets on 46 PubChem assays comprising at least 300,000 compounds and covering a wide range of assay biology. The informer compound set showed improvement in BEDROC(α = 100), PRAUC, and ROCAUC values averaged over all assays of 0.024, 0.014, and 0.016, respectively, compared to randomly selected training sets, all with paired t-test p-values <10(-15). A per-assay assessment showed that the BEDROC(α = 100), which is of particular relevance for early retrieval of actives, improved for 38 out of 46 assays, increasing the success rate of smaller follow-up screens. Overall, we showed that an informer set derived from historical HTS activity data can be employed for routine small-scale exploratory screening in an assay-agnostic fashion. This approach led to a consistent improvement in hit rates in follow-up screens without compromising scaffold retrieval. The informer set is adjustable in size depending on the number of compounds one intends to screen, as performance gains are realized for sets with more than 3,000 compounds, and this set is therefore applicable to a variety of situations. Finally, our results indicate that random sampling may not adequately cover descriptor space, drawing attention to the importance of the composition of the training set for predicting actives.

  8. Biological activity of trisporoids and trisporoid analogues in Mucor mucedo (-).

    Science.gov (United States)

    Schachtschabel, Doreen; Schimek, Christine; Wöstemeyer, Johannes; Boland, Wilhelm

    2005-06-01

    In the course of their sexual interactions, zygomycete fungi communicate via an elaborate series of carotene-derived compounds, namely trisporic acid and its biosynthetic progenitors. A novel building-block strategy allowed the systematic generation of structurally modified trisporoids along with putative early biosynthetic precursors for physiological tests. The impact of discrete structural elements was documented by the ability of individual compounds to induce sexually committed hyphae in Mucor mucedo. The activity screening contributed to establish general structure-function relationships for trisporoid action. Most crucial for activity were the dimension of the longer side chain, the polarity of functional groups at C(4) and C(13), and the number of conjugated double bonds in the side chain. The presence of an oxygen substituent at the cyclohexene ring is not essential for function. The overall biological activity apparently results from the combination of the various structural elements.

  9. Chemical Analysis and Biological Activity of Jordanian Chamomile Extracts

    Directory of Open Access Journals (Sweden)

    Nawal Hassan Al Bahtiti

    2012-02-01

    Full Text Available The Jordanian chamomile (Matricaria chamomilla has been researched more thoroughly to evaluate its useful properties. It is investigated and found that Jordanian chamomile is rich in phenolic compounds, with beneficial biological activities. By applying the most promising HPLC method, the content of total phenolics in methanolic extract was determined according to the Folin-Clocalteu procedure, and was found (GAE>20 mg/g. The flavonoid types were found as flavones and flavonolos.The minimum inhibitory concentration values for methanolic extracts of Jordanian chamomile were determined for different kinds of bacteria. The extracts have activity against Staphylococcus aurous, candida albicans, Esherichia Coli, Betula pubescens and Pinus sylvestris. The activity has been observed to be due to the tannins and a pigenin present in the extract. To utilize these significant sources of natural compounds, further characterization of phenolic composition is needed.

  10. Antioxidant activity relationship of phenolic compounds in Hypericum perforatum L.

    Directory of Open Access Journals (Sweden)

    Petrović Slobodan S

    2011-06-01

    Full Text Available Abstract Background The St John's Wort (Hypericum perforatum; Clusiaceae has been used in traditional and modern medicine for a long time due to its high content of biologically active phenolics. The purpose of this work was to develop a method for their fractionation and identification, and to determine the most active antioxidant compounds in plant extract. Results An LC-MS method which enables fast qualitative and semiquantitative analysis was developed. The composition determined is in agreement with the previous results, where 6 flavonoids, 4 naphthodianthrones and 4 phloroglucinols have been identified. Significant antioxidant activity was determined for most of the fractions by DPPH assay (the lowest IC50 of 0.52 μg/ml, NO scavenging (6.11 μg/ml, superoxide scavenging (1.86 μg/ml, lipid peroxidation (0.0079 μg/ml and FRAP (the highest reduction capacity of 104 mg Fe equivalents/g assays. Conclusion LC-MS technique has been successfully applied for a quick separation and identification of the major components of H. perforatum fractions. Majority of the fractions analyzed have expressed a very high antioxidative activity when compared to synthetic antioxidants. The antioxidant activity could be attributed to flavonoids and phenolic acids, while phloroglucinols and naphthodianthrones showed no significant activity. It is demonstrated that it is possible to obtain, by fractionation, H. perforatum preparations with significantly increased phloroglucinols-to-naphthodianthrones ratio (up to 95:5.

  11. Synthesis and Biological Investigation of Δ(12)-Prostaglandin J3 (Δ(12)-PGJ3) Analogues and Related Compounds.

    Science.gov (United States)

    Nicolaou, K C; Pulukuri, Kiran Kumar; Rigol, Stephan; Heretsch, Philipp; Yu, Ruocheng; Grove, Charles I; Hale, Christopher R H; ElMarrouni, Abdelatif; Fetz, Verena; Brönstrup, Mark; Aujay, Monette; Sandoval, Joseph; Gavrilyuk, Julia

    2016-05-25

    A series of Δ(12)-prostaglandin J3 (Δ(12)-PGJ3) analogues and derivatives were synthesized employing an array of synthetic strategies developed specifically to render them readily available for biological investigations. The synthesized compounds were evaluated for their cytotoxicity against a number of cancer cell lines, revealing nanomolar potencies for a number of them against certain cancer cell lines. Four analogues (2, 11, 21, and 27) demonstrated inhibition of nuclear export through a covalent addition at Cys528 of the export receptor Crm1. One of these compounds (i.e., 11) is currently under evaluation as a potential drug candidate for the treatment of certain types of cancer. These studies culminated in useful and path-pointing structure-activity relationships (SARs) that provide guidance for further improvements in the biological/pharmacological profiles of compounds within this class.

  12. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Cédric Charrier; Joëlle Roche; Jean-Pierre Gesson; Philippe Bertrand

    2009-07-01

    New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide derivatives. The first fluorinated derivatives of trichostatic acid are described, such as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity.

  13. 生物土壤添加剂对连作黄瓜防御酶系及酚类物质含量的影响%Effects of biological soil amendment on defense enzyme activity and phenolic compound of cucumber continuous cropping

    Institute of Scientific and Technical Information of China (English)

    郝永娟; 魏军; 刘春艳; 王勇; 王万立

    2009-01-01

    The changes of several defense enzyme activities and phenolic compound in cucumber roots were examined after biological soil amendment(BSA) was applied to the cucumber continuous cropping through pot trials. It could promote seedling growth and reduce disease incidence. The results showed that the activities of defense enzymes such as peroxidase (POD), polyphenol oxidase (PPO) and TTC in treated cucumber roots were measured significantly higher than that of control. The activities of POD and PPO in BSA-treated roots were significantly higher than that of control after inoculation with Fusarium oxysporum(Schl.)f. sp. Cucumerinum. Phenolic compound content of roots decreased in the initial period of inoculation, increased after disease incidence, but it was higher in BSA-treated than that of control. These indicated that BSA could induce the defense enzyme activities and increased phenolic compound in cucumber roots.%@@ 连作障碍是设施蔬菜发展的瓶颈问题,表现为根系生长受到抑制,土传病害严重发生.目前解决方法以嫁接栽培和药剂处理土壤为主,国内外也有利用有机物、生物肥和生防菌剂防治土传病害,缓解连作障碍的报道~([1]).

  14. Synthesis and Biological Activity of Arylspiroborate Salts Derived from Caffeic Acid Phenethyl Ester

    Directory of Open Access Journals (Sweden)

    Martin J. G. Hébert

    2015-01-01

    Full Text Available Two novel boron compounds containing caffeic acid phenethyl ester (CAPE derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes. These results clearly show the effectiveness of the synthesized salts as transporter of CAPE.

  15. Organolead compounds shown to be genetically active

    Energy Technology Data Exchange (ETDEWEB)

    Ahlberg, J.; Ramel, C.; Wachtmeister, C.A.

    1972-01-01

    The purpose of the present investigation was to determine whether alkyllead compounds would cause a genetic effect similar to that caused by alkyl mercury compounds. Experiments were conducted on Allium cepa (onion) in order to determine the effect of lead compounds on the spindle fiber mechanism. Results indicate that disturbances of the spindle fiber mechanism occur even at very low concentrations. The lowest concentration at which such effects are observed seems to be between 10/sup -6/ and 10/sup -7/ M for the organic compounds. Although no effect can be observed on the spindle fibers at lower dosages, the mitotic index is changed even at a dose of 10/sup -7/ M with dimethyllead. A preliminary experiment was made on Drosophila with triethyllead in order to investigate whether the effects which were observed on mitoses in Allium would also be observed in a meiotic cell system in an animal.

  16. Active compounds from cyanobacteria and microalgae: properties and potential applications in biomedicine

    Directory of Open Access Journals (Sweden)

    Alexey Llopiz

    2016-05-01

    Full Text Available Cyanobacteria and microalgae are source of many chemicals substances with potential applications on biopharmaceutical industry. Many structures have been characterized in these organism, such as: peptides, proteins, carbohydrates, terpenoids, polyinsatured fatty acids, flavonoids, phenolic compounds, vitamins, porfirins and other organic substances. Chemicals structures of isolated compounds are diverse and it depends of microalgae habitats. Pharmacological activities located in microalgae are bactericides, immunomodulatory, antioxidants, cytoprotective, fungicides and antivirals. These properties may possible the potential treatment of many diseases including autoimmunes disorders, tumoral, and infectious process. In this review are presented and discussed some elements associated to chemical structure and biological activities around of compounds with potential uses as biopharmaceuticals.

  17. Oxovanadium(IV) Compounds of cis-[VOCl(N-N){sub 2}]{sup +} (N-N = 4,4'- and 5,5'-dimethyl-2,2'-bipyridine); Crystal Structure and Biological Activity

    Energy Technology Data Exchange (ETDEWEB)

    Nasser Ostad, S.; Tavajohi, Shohreh [Univ. of Medical Sciences, Tehran (Iran, Islamic Republic of); Masoomeh Emadi, S.; Amani, Vahid; Abedi, Anita [Islamic Azad Univ., Tehran (Iran, Islamic Republic of)

    2012-11-15

    Vanadium(IV) complexes in a general formula of cis-[VOX(N-N){sub 2}]{sup 0/+1}, (X=Cl., OH., SO{sub 4}{sup -2} and N-N = phen, bipy) have been reported. We considered the methyl-substituted bipyridine analogues, 4,4'-dimethyl-2,2'-bipyridine (4dmbpy) and 5,5'-dimethyl-2,2'-bipyridine (5dmbpy) as ligands since our last studies on cytotoxicity of oxovanadium(IV) exhibited that introduction of a methyl group into N-N ligands causes further enhanced cytotoxicity of the related complex. Totally, two new oxovanadium(IV), [VOCl(4dmbpy){sub 2}]·Cl·H{sub 2}O·C{sub 2}H{sub 5}OH (1) and [VOCl(5dmbpy){sub 2}]·Cl·H{sub 2}O·CH{sub 3}OH (2) were synthesized, proposing anticancer activity of the cationic part of the complexes, as ionic vanadium compounds show to increase membrane permeability with a potential for dose reduction.4 Both complexes were fully characterized by means of elemental analysis, IR and UV-Vis. spectroscopy as well as the X-ray diffraction method. Furthermore their cytotoxicity were assayed in three cell cultures, colorectal adenocarcinoma (Caco-2), colon carcinoma (HT-29) and breast ductal carcinoma (T47D) by means of MTT assay (MTT=3-(4,5-dimethylthiazol-2-yl) 2,5-diphenyl tetrazolium bromide) and the results were compared with cisplatin, an anticancer drugs which shows limited activity on colon and breast cancers.

  18. A New Natural Compound with Cytotoxic Activity from Tripterygium hypoglaucum

    Institute of Scientific and Technical Information of China (English)

    LI Wei; WANG Fang; ZHAO Yu-qing

    2011-01-01

    Objective To find antitumor cOnstituents from Tripterygium hypoglaucum.Methods The chloroform extract of T.hypoglaucum was separated by silica gel column chromatography and preparative HPLC.The structures of compounds isolated were identified by spectral analysis and chemical evidence.Results Seven compounds were isolated and identified as rhein ethyl ester(1),chrysophenol(2),physcion(3),emodin(4),wilfordine(5),wilforgine(6),and wilforine(7).The cytotoxic activities of the compounds against cancer cell lines were assayed.Conclusion Compound 1 is a new natural compound with strong activities against human cancer cell lines (A2780 and OVCAR-3).Compounds 2-4 are isolated from this genus plants for the first time.The possible structure-activity relationship among compounds 1-4 shows that the methoxy group or oxyethyl moiety might be responsible for the cytotoxity.

  19. Biological activities of Curcuma longa L.

    OpenAIRE

    Araújo CAC; LL Leon

    2001-01-01

    There are several data in the literature indicating a great variety of pharmacological activities of Curcuma longa L. (Zingiberaceae), which exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacteria, antioxidant effects and nematocidal activities. Curcumin is a major component in Curcuma longa L., being responsible for its biological actions. Other extracts of this plant has been showing potency too. In vitro, curcumin exhibits anti-parasitic, antispasmodic, anti-inflammator...

  20. Flavonoid-membrane interactions: possible consequences for biological effects of some polyphenolic compounds

    Institute of Scientific and Technical Information of China (English)

    Andrzej B HENDRICH

    2006-01-01

    Flavonoids are found ubiquitously in higher plants and constitute an important component of the majority of peoples' daily diets. The biological activities of flavonoids cover a very broad spectrum, from anticancer and antibacterial activities through to inhibition of bone resorption. In the present paper, the interactions between flavonoids and lipid bilayers as well as biological membranes and their components are reviewed, with special emphasis on the structure-activity relationships and mechanisms underlying the biological activity of flavonoids.

  1. Preparation and characterization of new biologically active polyurethane foams.

    Science.gov (United States)

    Savelyev, Yuri; Veselov, Vitali; Markovskaya, Ludmila; Savelyeva, Olga; Akhranovich, Elena; Galatenko, Natalya; Robota, Ludmila; Travinskaya, Tamara

    2014-12-01

    Biologically active polyurethane foams are the fast-developed alternative to many applications of biomedical materials. Due to the polyurethane structure features and foam technology it is possible to incorporate into their structure the biologically active compounds of target purpose via structural-chemical modification of macromolecule. A series of new biologically active polyurethane foams (PUFs) was synthesized with polyethers (MM 2500-5000), polyesters MM (500-2200), 2,4(2,6) toluene diisocyanate, water as a foaming agent, catalysts, foam stabilizers and functional compounds. Different functional compounds: 1,4-di-N-oxy-2,3-bis-(oxymethyl)-quinoxaline (DOMQ), partial sodium salt of poly(acrylic acid) and 2,6-dimethyl-N,N-diethyl aminoacetatanilide hydrochloride were incorporated into the polymer structure/composition due to the chemical and/or physical bonding. Structural peculiarities of PUFs were studied by FTIR spectroscopy and X-ray scattering. Self-adhesion properties of PUFs were estimated by measuring of tensile strength at break of adhesive junction. The optical microscopy method was performed for the PUF morphology studies. Toxicological estimation of the PUFs was carried out in vitro and in vivo. The antibacterial action towards the Gram-positive and Gram-negative bacteria (Escherichia coli ATC 25922, E. coli ATC 2150, Klebsiella pneumoniae 6447, Staphylococcus aureus 180, Pseudomonas aeruginosa 8180, Proteus mirabilis F 403, P. mirabilis 6054, and Proteus vulgaris 8718) was studied by the disc method on the solid nutrient. Physic-chemical properties of the PUFs (density, tensile strength and elongation at break, water absorption and vapor permeability) showed that all studied PUFs are within the operational requirements for such materials and represent fine-cellular foams. Spectral studies confirmed the incorporation of DOMQ into the PUF's macrochain. PUFs are characterized by microheterogeneous structure. They are antibacterially active, non

  2. Biological activities of secondary metabolites of the order Zoanthids

    Directory of Open Access Journals (Sweden)

    Zahra Aminikhoei

    2015-11-01

    Full Text Available The phylum Cnidaria is a large, diverse and ecologically important group of marine invertebrates, which produce powerful toxins and venoms. The number of marine natural product from cnidarians isolated from class Anthozoa. Among the Anthozoa, the order of zoanthids are sessile, clonal and mostly brightly colored invertebrate which produce high biodiversity of cytolitic, neurotoxic and cardiotoxic compounds. Zoanthids containing palytoxins are reportedly among the most toxic marine organisms known. In addition, a high concentration of zoanthamine alkaloids extracted from this group.The zoanthamine alkaloids were isolated over 20 years ago, exhibit a broad range of biological activities.The best studied and most well-known biological activity of zoanthamine derivative significantly suppressed bone resorption and enhanced bone formation.

  3. Visual Analysis of Biological Activity Data with Scaffold Hunter.

    Science.gov (United States)

    Klein, Karsten; Koch, Oliver; Kriege, Nils; Mutzel, Petra; Schäfer, Till

    2013-12-01

    The growing interest in chemogenomics approaches over the last years has led to an increasing amount of data regarding chemical and the corresponding biological activity space. The resulting data, collected in either in-house or public databases, need to be analyzed efficiently to speed-up the increasingly difficult task of drug discovery. Unfortunately, the discovery of new chemical entities or new targets for known drugs ('drug repurposing') is not suitable to a fully automated analysis or a simple drill down process. Visual interactive interfaces that allow to explore chemical space in a systematic manner and facilitate analytical reasoning can help to overcome these problems. Scaffold Hunter is a tool for the visual analysis of chemical compound databases that provides integrated visualization and analysis of biological activity data and fosters the interactive exploration of data imported from a variety of sources. We describe the features and illustrate the use by means of an exemplary analysis workflow.

  4. Biological activities and medicinal properties of Cajanus cajan (L Millsp.

    Directory of Open Access Journals (Sweden)

    Dilipkumar Pal

    2011-01-01

    Full Text Available Cajanus cajan (L Millsp. (Sanskrit: Adhaki, Hindi: Arhar, English: Pigeon pea, Bengali: Tur (family: Fabaceae is the most important grain legume crop of rain-fed agriculture in semi-arid tropics. It is both a food crop and a cover/forage crop with high levels of proteins and important amino acids like methionine, lysine and tryptophan. During the last few decades extensive studies have been carried out regarding the chemistry of C. cajan and considerable progress has been achieved regarding its biological activities and medicinal applications. This review article gives an overview on the biological activities of the compounds isolated, pharmacological actions and clinical studies of C. cajan extracts apart from its general details.

  5. Loranthus micranthus Linn.: Biological Activities and Phytochemistry

    Directory of Open Access Journals (Sweden)

    Soheil Zorofchian Moghadamtousi

    2013-01-01

    Full Text Available Loranthus micranthus Linn. is a medicinal plant from the Loranthaceae family commonly known as an eastern Nigeria species of the African mistletoe and is widely used in folkloric medicine to cure various ailments and diseases. It is semiparasitic plant because of growing on various host trees and shrubs and absorbing mineral nutrition and water from respective host. Hence, the phytochemicals and biological activities of L. micranthus demonstrated strong host and harvesting period dependency. The leaves have been proved to possess immunomodulatory, antidiabetic, antimicrobial, antihypertensive, antioxidant, antidiarrhoeal, and hypolipidemic activities. This review summarizes the information and findings concerning the current knowledge on the biological activities, pharmacological properties, toxicity, and chemical constituents of Loranthus micranthus.

  6. Seasonal variations of phenolic compounds and biological properties in sage (Salvia officinalis L.).

    Science.gov (United States)

    Generalić, Ivana; Skroza, Danijela; Surjak, Jana; Možina, Sonja Smole; Ljubenkov, Ivica; Katalinić, Ana; Simat, Vida; Katalinić, Višnja

    2012-02-01

    The aim was to investigate the phenolic content, antioxidant capacity, and antibacterial activity of Dalmatian sage (Salvia officinalis L.) leaves collected during different vegetation periods. Separation and quantification of the individual phenols were performed by reversed-phase (RP)-HPLC coupled with a PDA (photodiode array) detector and using an internal standard, while the contents of total phenols, flavonoids, flavones, and flavonols were determined spectrophotometrically. The antioxidant properties of the sage leaf extracts were evaluated using five different antioxidant assays (FRAP, DPPH, ABTS, Briggs-Rauscher reaction, and β-carotene bleaching). The antimicrobial activity of the extracts was tested against two Gram-positive (Bacillus cereus and Staphylococcus aureus) and two Gram-negative (Salmonella Infantis and Escherichia coli) bacterial reference strains. All extracts were extremely rich in phenolic compounds, and provided good antioxidant and antibacterial properties, but the phenophase in which the leaves were collected affected the phenolic composition of the sage extracts and consequently their biological activity. The May Extract, the richest in total flavonoids, showed the best antioxidant properties and the highest antimicrobial activity. Thus, collection of the plants during May seems the best choice for further use of them in the pharmaceutical and food industry.

  7. Glycosides from Marine Sponges (Porifera, Demospongiae: Structures, Taxonomical Distribution, Biological Activities and Biological Roles

    Directory of Open Access Journals (Sweden)

    Valentin A. Stonik

    2012-08-01

    Full Text Available Literature data about glycosides from sponges (Porifera, Demospongiae are reviewed. Structural diversity, biological activities, taxonomic distribution and biological functions of these natural products are discussed.

  8. Glycosides from marine sponges (Porifera, Demospongiae): structures, taxonomical distribution, biological activities and biological roles.

    Science.gov (United States)

    Kalinin, Vladimir I; Ivanchina, Natalia V; Krasokhin, Vladimir B; Makarieva, Tatyana N; Stonik, Valentin A

    2012-08-01

    Literature data about glycosides from sponges (Porifera, Demospongiae) are reviewed. Structural diversity, biological activities, taxonomic distribution and biological functions of these natural products are discussed.

  9. Using synthetic biology to increase nitrogenase activity

    OpenAIRE

    Li, Xin-Xin; Liu, Qi; Liu, Xiao-Meng; Shi, Hao-Wen; Chen, San-feng

    2016-01-01

    Background Nitrogen fixation has been established in protokaryotic model Escherichia coli by transferring a minimal nif gene cluster composed of 9 genes (nifB, nifH, nifD, nifK, nifE, nifN, nifX, hesA and nifV) from Paenibacillus sp. WLY78. However, the nitrogenase activity in the recombinant E. coli 78-7 is only 10 % of that observed in wild-type Paenibacillus. Thus, it is necessary to increase nitrogenase activity through synthetic biology. Results In order to increase nitrogenase activity ...

  10. Synthesis and Antibacterial Activity of New Cephalosporin Compounds

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Five new cephalosporin compounds were designed and synthesized, and the antibacterial activities were evaluated by the standard serial 2-fold agar dilution method in vitro.The results showed that the activities of the compounds Ⅰa and Ⅰb against ESBL E. coli and K.pneumoniae are comparable to those of Cefepime.

  11. The ice nucleation activity of biological aerosols

    Science.gov (United States)

    Grothe, H.; Pummer, B.; Bauer, H.; Bernardi, J.

    2012-04-01

    Primary Biological Aerosol Particles (PBAPs), including bacteria, spores and pollen may be important for several atmospheric processes. Particularly, the ice nucleation caused by PBAPs is a topic of growing interest, since their impact on ice cloud formation and thus on radiative forcing, an important parameter in global climate is not yet fully understood. In laboratory model studies we investigated the ice nucleation activity of selected PBAPs. We studied the immersion mode freezing using water-oil emulsion, which we observed by optical microscopy. We particularly focused on pollen. We show that pollen of different species strongly differ in their ice nucleation behavior. The average freezing temperatures in laboratory experiments range from 240 K to 255 K. As the most efficient nuclei (silver birch, Scots pine and common juniper pollen) have a distribution area up to the Northern timberline, their ice nucleation activity might be a cryoprotective mechanism. For comparison the ice nucleation activity of Snomax, fungal spores, and mushrooms will be discussed as well. In the past, pollen have been rejected as important atmospheric IN, as they are not as abundant in the atmosphere as bacteria or mineral dust and are too heavy to reach higher altitudes. However, in our experiments (Pummer et al. 2011) it turned out that water, which had been in contact with pollen and then been separated from the bodies, nucleates as good as the pollen grains themselves. So the ice nuclei have to be easily-suspendable macromolecules (100-300 kDa) located on the pollen. Once extracted, they can be distributed further through the atmosphere than the heavy pollen grains and so augment the impact of pollen on ice cloud formation even in the upper troposphere. It is widely known, that material from the pollen, like allergens and sugars, can indeed leave the pollen body and be distributed independently. The most probable mechanism is the pollen grain bursting by rain, which releases

  12. Inactivation of the antibacterial and cytotoxic properties of silver ions by biologically relevant compounds.

    Directory of Open Access Journals (Sweden)

    Geraldine Mulley

    Full Text Available There has been a recent surge in the use of silver as an antimicrobial agent in a wide range of domestic and clinical products, intended to prevent or treat bacterial infections and reduce bacterial colonization of surfaces. It has been reported that the antibacterial and cytotoxic properties of silver are affected by the assay conditions, particularly the type of growth media used in vitro. The toxicity of Ag+ to bacterial cells is comparable to that of human cells. We demonstrate that biologically relevant compounds such as glutathione, cysteine and human blood components significantly reduce the toxicity of silver ions to clinically relevant pathogenic bacteria and primary human dermal fibroblasts (skin cells. Bacteria are able to grow normally in the presence of silver nitrate at >20-fold the minimum inhibitory concentration (MIC if Ag+ and thiols are added in a 1:1 ratio because the reaction of Ag+ with extracellular thiols prevents silver ions from interacting with cells. Extracellular thiols and human serum also significantly reduce the antimicrobial activity of silver wound dressings Aquacel-Ag (Convatec and Acticoat (Smith & Nephew to Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli in vitro. These results have important implications for the deployment of silver as an antimicrobial agent in environments exposed to biological tissue or secretions. Significant amounts of money and effort have been directed at the development of silver-coated medical devices (e.g. dressings, catheters, implants. We believe our findings are essential for the effective design and testing of antimicrobial silver coatings.

  13. Synthesis and biological activity of hydroxycinnamoyl containing antiviral drugs

    Directory of Open Access Journals (Sweden)

    Chochkova Maya G.

    2014-01-01

    Full Text Available Seven N-hydroxycinnamoyl amides were synthesized by EDC/HOBt coupling of the corresponding substituted cinnamic acids (p-coumaric-, ferulic-, sinapic- and caffeic acids with influenza antivirals (amantadine, rimantadine and oseltamivir. DPPH (1,1-diphenyl-2-picrylhydrazyl scavenging abilities and the inhibitory effect on mushroom tyrosinase activity (using L-tyrosine as the substrate were investigated in vitro. Amongst the synthesized compounds, N-[(E-3-(3’,4’-dihydroxyphenyl-2-propenoyl]oseltamivir (1 and N-[(E-3-(3’,4’-dihydroxyphenyl-2-propenoyl]rimantadine (4, containing catechol moiety, exhibited the most potent DPPH radical-scavenging activity. Amide (1 displayed also tyrosinase inhibitory effect toward L-tyrosine as the substrate (~50%. Due to its biological activities revealed so far compound (1 can be considered as a promising candidate for a cosmetic ingredient. The synthesized compounds were also investigated for their in vitro inhibitory activity against the replication of influenza virus A (H3N2.

  14. Biological activities of water-soluble fullerene derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Nakamura, S; Mashino, T [Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shiba-koen, Minato-ku, Tokyo 105-8512 (Japan)], E-mail: mashino-td@pha.keio.ac.jp

    2009-04-01

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C{sub 60}-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C{sub 60}-bis(7V,7V-dimethylpyrrolidinium iodide), a cationic fullerene derivative, has antibacterial activity and antiproliferative effect on cancer cell lines. The mechanism is suggested to be respiratory chain inhibition by reactive oxygen species produced by the cationic fullerene derivative. Proline-type fullerene derivatives showed strong inhibition activities on HIV-reverse transcriptase. The IC{sub 50} values were remarkably lower than nevirapine, a clinically used anti-HIV drug. Fullerene derivatives have a big potential for a new type of lead compound to be used as medicine.

  15. Monitoring Biological Activity at Geothermal Power Plants

    Energy Technology Data Exchange (ETDEWEB)

    Peter Pryfogle

    2005-09-01

    The economic impact of microbial growth in geothermal power plants has been estimated to be as high as $500,000 annually for a 100 MWe plant. Many methods are available to monitor biological activity at these facilities; however, very few plants have any on-line monitoring program in place. Metal coupon, selective culturing (MPN), total organic carbon (TOC), adenosine triphosphate (ATP), respirometry, phospholipid fatty acid (PLFA), and denaturing gradient gel electrophoresis (DGGE) characterizations have been conducted using water samples collected from geothermal plants located in California and Utah. In addition, the on-line performance of a commercial electrochemical monitor, the BIoGEORGE?, has been evaluated during extended deployments at geothermal facilities. This report provides a review of these techniques, presents data on their application from laboratory and field studies, and discusses their value in characterizing and monitoring biological activities at geothermal power plants.

  16. Novel triple reuptake inhibitors with low risk of CAD associated liabilities: design, synthesis and biological activities of 4-[(1S)-1-(3,4-dichlorophenyl)-2-methoxyethyl]piperidine and related compounds.

    Science.gov (United States)

    Ishichi, Yuji; Kimura, Eiji; Honda, Eiji; Yoshikawa, Masato; Nakahata, Takashi; Terao, Yasuko; Suzuki, Atsuko; Kawai, Takayuki; Arakawa, Yuuichi; Ohta, Hiroyuki; Kanzaki, Naoyuki; Nakagawa, Hideyuki; Terauchi, Jun

    2013-08-01

    A novel triple reuptake inhibitor with low potential of liabilities associated with cationic amphiphilic drug (CAD) was identified following an analysis of existing drugs. Low molecular weight (MW liabilities (CYP2D6 inhibition, hERG inhibition and phospholipidosis). Based on the hypothesis, a series of piperidine compounds was designed with consideration of the common characteristic features of CNS drugs. Optimization of the side chain by adjusting overall lipophilicity suggested that incorporation of a methoxymethyl group could provide compounds with a balance of both potent reuptake inhibition and low liability potential. Compound (S)-3a showed a potent antidepressant-like effect in the mice tail suspension test (MED = 10 mg/kg, p.o.), proportional monoamine transporter occupancies and enhancement of monoamine concentrations in mouse prefrontal cortex.

  17. Biologically active extracts with kidney affections applications

    Science.gov (United States)

    Pascu (Neagu), Mihaela; Pascu, Daniela-Elena; Cozea, Andreea; Bunaciu, Andrei A.; Miron, Alexandra Raluca; Nechifor, Cristina Aurelia

    2015-12-01

    This paper is aimed to select plant materials rich in bioflavonoid compounds, made from herbs known for their application performances in the prevention and therapy of renal diseases, namely kidney stones and urinary infections (renal lithiasis, nephritis, urethritis, cystitis, etc.). This paper presents a comparative study of the medicinal plant extracts composition belonging to Ericaceae-Cranberry (fruit and leaves) - Vaccinium vitis-idaea L. and Bilberry (fruit) - Vaccinium myrtillus L. Concentrated extracts obtained from medicinal plants used in this work were analyzed from structural, morphological and compositional points of view using different techniques: chromatographic methods (HPLC), scanning electronic microscopy, infrared, and UV spectrophotometry, also by using kinetic model. Liquid chromatography was able to identify the specific compounds of the Ericaceae family, present in all three extracts, arbutosid, as well as specific components of each species, mostly from the class of polyphenols. The identification and quantitative determination of the active ingredients from these extracts can give information related to their therapeutic effects.

  18. Optimization of hypocrellin B derivative amphiphilicity and biological activity

    Institute of Scientific and Technical Information of China (English)

    LIU Xin; XIE Jie; ZHANG LuYong; CHEN HongXia; GU Ying; ZHAO JingQuan

    2009-01-01

    To satisfy the dual requirements of the fluent transportation in blood and the affinity to the target tissues of vascular diseases, hypocrellin derivatives with optimized amphiphilicity are expected. In this work, 3-amino-1-propanesulfonic acid and 4-amino-1-butanesulfonic acid substituted hypocrellin B,named compounds 1 and 2, were designed, synthesized in high yields and characterized. Besides greatly strengthened red absorption, the maximum solubility of compound 2 in phosphate buffered saline (PBS) is 4.2 mg/mL which is just enough to prepare an aqueous solution for intravenous injection in clinically acceptable concentration, while the partition coefficient between n-octanol and PBS,5.6, benefits the cell-uptake and biological activity as well. Furthermore, EPR measurements reveal that the photosensitization activities of the two compounds to generate semiquinone anion radicals, superoxide anion radicals and singlet oxygen are a little bit higher than those of taurine substituted hypocrellin B (THB), but the photodynamic activities to human lung cancer A549 cells are several times that of THB, mainly due to increases in lipophilicity and cell-uptake.

  19. Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach

    Directory of Open Access Journals (Sweden)

    Yasmeen Gull

    2016-02-01

    Full Text Available A new series of N-(6-arylbenzo[d]thiazol-2-ylacetamides were synthesized by C-C coupling methodology in the presence of Pd(0 using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolylbenzo[d]thiazol-2-ylacetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

  20. Potential therapeutic applications of microbial surface-active compounds

    Directory of Open Access Journals (Sweden)

    Letizia Fracchia

    2015-08-01

    Full Text Available Numerous investigations of microbial surface-active compounds or biosurfactants over the past two decades have led to the discovery of many interesting physicochemical and biological properties including antimicrobial, anti-biofilm and therapeutic among many other pharmaceutical and medical applications. Microbial control and inhibition strategies involving the use of antibiotics are becoming continually challenged due to the emergence of resistant strains mostly embedded within biofilm formations that are difficult to eradicate. Different aspects of antimicrobial and anti-biofilm control are becoming issues of increasing importance in clinical, hygiene, therapeutic and other applications. Biosurfactants research has resulted in increasing interest into their ability to inhibit microbial activity and disperse microbial biofilms in addition to being mostly nontoxic and stable at extremes conditions. Some biosurfactants are now in use in clinical, food and environmental fields, whilst others remain under investigation and development. The dispersal properties of biosurfactants have been shown to rival that of conventional inhibitory agents against bacterial, fungal and yeast biofilms as well as viral membrane structures. This presents them as potential candidates for future uses in new generations of antimicrobial agents or as adjuvants to other antibiotics and use as preservatives for microbial suppression and eradication strategies.

  1. Structure-Activity Relationships in Nitro-Aromatic Compounds

    Science.gov (United States)

    Vogt, R. A.; Rahman, S.; Crespo-Hernández, C. E.

    Many nitro-aromatic compounds show mutagenic and carcinogenic properties, posing a potential human health risk. Despite this potential health hazard, nitro-aromatic compounds continue to be emitted into ambient air from municipal incinerators, motor vehicles, and industrial power plants. As a result, understanding the structural and electronic factors that influence mutagenicity in nitro-aromatic compounds has been a long standing objective. Progress toward this goal has accelerated over the years, in large part due to the synergistic efforts among toxicology, computational chemistry, and statistical modeling of toxicological data. The concerted influence of several structural and electronic factors in nitro-aromatic compounds makes the development of structure-activity relationships (SARs) a paramount challenge. Mathematical models that include a regression analysis show promise in predicting the mutagenic activity of nitro-aromatic compounds as well as in prioritizing compounds for which experimental data should be pursued. A major challenge of the structure-activity models developed thus far is their failure to apply beyond a subset of nitro-aromatic compounds. Most quantitative structure-activity relationship papers point to statistics as the most important confirmation of the validity of a model. However, the experimental evidence shows the importance of the chemical knowledge in the process of generating models with reasonable applicability. This chapter will concisely summarize the structural and electronic factors that influence the mutagenicity in nitro-aromatic compounds and the recent efforts to use quantitative structure-activity relationships to predict those physicochemical properties.

  2. Molecular simulation of receptors of physiologically active compounds for purposes of medical chemistry

    Science.gov (United States)

    Baskin, Igor I.; Palyulin, Vladimir A.; Zefirov, Nikolai S.

    2009-06-01

    The general strategy of the molecular simulation of biological receptors and their interaction with ligands is considered. The procedures for construction of 3D protein models, molecular docking, evaluation of model quality, determination of the free energy of protein binding with ligands are discussed. The methods of molecular design of new medicaments based on molecular models of biological targets: virtual screening and de novo design, are presented. Examples of the above-listed approaches for the simulation of a number of pharmacologically significant receptors, analysis of receptor-ligand interactions and design of new biologically active organic compounds are given.

  3. Molecular simulation of receptors of physiologically active compounds for purposes of medical chemistry

    Energy Technology Data Exchange (ETDEWEB)

    Baskin, Igor I; Palyulin, Vladimir A; Zefirov, Nikolai S [Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow (Russian Federation)

    2009-06-30

    The general strategy of the molecular simulation of biological receptors and their interaction with ligands is considered. The procedures for construction of 3D protein models, molecular docking, evaluation of model quality, determination of the free energy of protein binding with ligands are discussed. The methods of molecular design of new medicaments based on molecular models of biological targets: virtual screening and de novo design, are presented. Examples of the above-listed approaches for the simulation of a number of pharmacologically significant receptors, analysis of receptor-ligand interactions and design of new biologically active organic compounds are given.

  4. Biologic activity of digoxin-specific antisera.

    Science.gov (United States)

    Watson, J F; Butler, V P

    1972-03-01

    Digoxin-specific antibodies are capable of removing essentially all intracellular digoxin from rat renal cortical slices or from human erythrocytes. In removing digoxin from erythrocytes, these antibodies are capable of reversing an effect of the drug on cellular potassium transport. This study provides direct evidence that antibodies are capable of removing, and thereby reversing the biological effect of, physiologically active low molecular weight substances after they have been taken up by mammalian cells. This biologic property of digoxin-specific antibodies suggests that autidigoxin sera may prove useful in the reversal of digoxin toxicity. Rapid and essentially quantitative removal of digoxin from red cells by antibody is not accompanied by an immediate restoration of patassium influx to normal levels. Identification of the mechanism of this phenomenon may provide useful information concerning the mode of action not only of digoxin, but also of the cation transport system of human erythrocytes.

  5. Biological Activities of Royal Jelly - Review

    Directory of Open Access Journals (Sweden)

    Crenguţa I. Pavel

    2011-10-01

    Full Text Available Royal jelly is a secretion product of the cephalic glands of nurse bees that has been used for centuries for itsextraordinary properties and health effects. This bibliographic study aims to review many of the scientific findingsand research that prove many of the remarkable various actions, effects and some uses of royal jelly. There are takeninto consideration numerous biological properties and effects of royal jelly: antioxidant, neurotrophic, hipoglicemiant, hipocholesterolemiant and hepatoprotective, hypotensive and blood pressure regulatory, antitumor, antibiotic, anti-inflammatory, immunomodulatory and anti-allergic, general tonic and antiaging. Royal jelly is one ofthe most studied bee products, but there still remains much to reveal about its biochemistry and biological activity infuture research for our health and life benefit.

  6. Feasibility of Active Machine Learning for Multiclass Compound Classification.

    Science.gov (United States)

    Lang, Tobias; Flachsenberg, Florian; von Luxburg, Ulrike; Rarey, Matthias

    2016-01-25

    A common task in the hit-to-lead process is classifying sets of compounds into multiple, usually structural classes, which build the groundwork for subsequent SAR studies. Machine learning techniques can be used to automate this process by learning classification models from training compounds of each class. Gathering class information for compounds can be cost-intensive as the required data needs to be provided by human experts or experiments. This paper studies whether active machine learning can be used to reduce the required number of training compounds. Active learning is a machine learning method which processes class label data in an iterative fashion. It has gained much attention in a broad range of application areas. In this paper, an active learning method for multiclass compound classification is proposed. This method selects informative training compounds so as to optimally support the learning progress. The combination with human feedback leads to a semiautomated interactive multiclass classification procedure. This method was investigated empirically on 15 compound classification tasks containing 86-2870 compounds in 3-38 classes. The empirical results show that active learning can solve these classification tasks using 10-80% of the data which would be necessary for standard learning techniques.

  7. Rhodiola plants: Chemistry and biological activity

    Directory of Open Access Journals (Sweden)

    Hsiu-Mei Chiang

    2015-09-01

    Full Text Available Rhodiola is a genus of medicinal plants that originated in Asia and Europe and are used traditionally as adaptogens, antidepressants, and anti-inflammatory remedies. Rhodiola plants are rich in polyphenols, and salidroside and tyrosol are the primary bioactive marker compounds in the standardized extracts of Rhodiola rosea. This review article summarizes the bioactivities, including adaptogenic, antifatigue, antidepressant, antioxidant, anti-inflammatory, antinoception, and anticancer activities, and the modulation of immune function of Rhodiola plants and its two constituents, as well as their potential to prevent cardiovascular, neuronal, liver, and skin disorders.

  8. Compounds from Polyphaga plancyi and their inhibitory activities against JAK3 and DDR1 kinases.

    Science.gov (United States)

    Zhu, Hong-Jie; Yan, Yong-Ming; Tu, Zheng-Chao; Luo, Jin-Feng; Liang, Rui; Yang, Tong-Hua; Cheng, Yong-Xian; Wang, Shu-Mei

    2016-10-01

    Plancyamides A (1) and B (3), plancypyrazine A (2), and plancyols A (4) and B (5), five new compounds (1-5), and three known ones (6-8), were isolated from the whole bodies of Polyphaga plancyi Bolivar. Their structures were elucidated by a combination of spectroscopic analyses including 1D and 2D NMR, and HRESIMS. Among them, compound 3 is racemic, chiral HPLC separation afforded its respective enantiomers. The absolute configuration of 1 was assigned by computational methods. Biological evaluation of all the compounds with exception of 7 and 8 discloses that compounds 2 and 4 could inhibit JAK3 kinase with IC50 values of 12.6 and 5.0μM, respectively. In addition, compound 4 exhibit inhibitory activity towards DDR1 kinase with IC50 value of 4.87μM.

  9. Biological activities of Curcuma longa L.

    Directory of Open Access Journals (Sweden)

    CAC Araújo

    2001-07-01

    Full Text Available There are several data in the literature indicating a great variety of pharmacological activities of Curcuma longa L. (Zingiberaceae, which exhibit anti-inflammatory, anti-human immunodeficiency virus, anti-bacteria, antioxidant effects and nematocidal activities. Curcumin is a major component in Curcuma longa L., being responsible for its biological actions. Other extracts of this plant has been showing potency too. In vitro, curcumin exhibits anti-parasitic, antispasmodic, anti-inflammatory and gastrointestinal effects; and also inhibits carcinogenesis and cancer growth. In vivo, there are experiments showing the anti-parasitic, anti-inflammatory potency of curcumin and extracts of C. longa L. by parenteral and oral application in animal models. In this present work we make an overview of the pharmacological activities of C. longa L., showing its importance.

  10. The Chemistry and Biological Activities of Mimosine: A Review.

    Science.gov (United States)

    Nguyen, Binh Cao Quan; Tawata, Shinkichi

    2016-08-01

    Mimosine [β-[N-(3-hydroxy-4-oxypyridyl)]-α-aminopropionic acid] is a non-protein amino acid found in the members of Mimosoideae family. There are a considerable number of reports available on the chemistry, methods for estimation, biosynthesis, regulation, and degradation of this secondary metabolite. On the other hand, over the past years of active research, mimosine has been found to have various biological activities such as anti-cancer, antiinflammation, anti-fibrosis, anti-influenza, anti-virus, herbicidal and insecticidal activities, and others. Mimosine is a leading compound of interest for use in the development of RAC/CDC42-activated kinase 1 (PAK1)-specific inhibitors for the treatment of various diseases/disorders, because PAK1 is not essential for the growth of normal cells. Interestingly, the new roles of mimosine in malignant glioma treatment, regenerative dentistry, and phytoremediation are being emerged. These identified properties indicate an exciting future for this amino acid. The present review is focused on the chemistry and recognized biological activities of mimosine in an attempt to draw a link between these two characteristics. Copyright © 2016 John Wiley & Sons, Ltd.

  11. Antioxidant and biological properties of bioactive phenolic compounds from Quercus suber L.

    Science.gov (United States)

    Fernandes, Ana; Fernandes, Iva; Cruz, Luís; Mateus, Nuno; Cabral, Miguel; de Freitas, Victor

    2009-12-09

    Phenolic compounds, namely, hydrolyzable tannins and low molecular weight phenolic compounds, were isolated and purified from Portuguese cork from Quercus suber L. Some of these compounds were studied to evaluate their antioxidant activity, including free-radical scavenging capacity (DPPH method) and reducing capacity (FRAP method). All compounds tested showed significant antioxidant activity, namely, antiradical and reducing properties. The antiradical capacity seemed to increase with the presence of galloyl groups. Regarding the reducing capacity, this structure-activity relationship was not so clear. These compounds were also studied to evaluate the growth inhibitory effect on the estrogen responsive human breast cancer cell line (ER+) MCF-7 and two other colon cancer cell lines (Caco-2 and HT-29). Generally, all the compounds tested exhibited, after a continuous exposure during a 48 h period, a dose-dependent growth inhibitory effect. Relative inhibitory activity was primarily related to the number of phenolic hydroxyl groups (galloyl and HHDP moieties) found in the active structures, with more groups generally conferring increased effects, except for HHDP-di-galloyl-glucose. Mongolicain B showed a greater potential to inhibit the growth of the three cell lines tested, identical to the effect observed with castalagin. Since these compounds are structurally related with each other, this activity might be based within the C-glycosidic ellagitannin moiety.

  12. Prediction of bioactive compounds activity against wood contaminant fungi using artificial neural networks

    OpenAIRE

    Vicente, Henrique; Roseiro, José C.; Arteiro, José M.; Neves, José; Caldeira, A. Teresa

    2013-01-01

    Biopesticides based on natural endophytic bacteria to control plant diseases are an ecological alternative to the chemical treatments. Bacillus species produce a wide variety of metabolites with biological activity like iturinic lipopeptides. This work addresses the production of biopesticides based on natural endophytic bacteria, isolated from Quercus suber. Artificial Neural Networks were used to maximize the percentage of inhibition triggered by antifungal activity of bioactive compounds p...

  13. Reconstructing Causal Biological Networks through Active Learning.

    Directory of Open Access Journals (Sweden)

    Hyunghoon Cho

    Full Text Available Reverse-engineering of biological networks is a central problem in systems biology. The use of intervention data, such as gene knockouts or knockdowns, is typically used for teasing apart causal relationships among genes. Under time or resource constraints, one needs to carefully choose which intervention experiments to carry out. Previous approaches for selecting most informative interventions have largely been focused on discrete Bayesian networks. However, continuous Bayesian networks are of great practical interest, especially in the study of complex biological systems and their quantitative properties. In this work, we present an efficient, information-theoretic active learning algorithm for Gaussian Bayesian networks (GBNs, which serve as important models for gene regulatory networks. In addition to providing linear-algebraic insights unique to GBNs, leading to significant runtime improvements, we demonstrate the effectiveness of our method on data simulated with GBNs and the DREAM4 network inference challenge data sets. Our method generally leads to faster recovery of underlying network structure and faster convergence to final distribution of confidence scores over candidate graph structures using the full data, in comparison to random selection of intervention experiments.

  14. [Antibacterial activity of natural compounds - essential oils].

    Science.gov (United States)

    Hassan, Sherif T S; Majerová, Michaela; Šudomová, Miroslava; Berchová, Kateřina

    2015-12-01

    Since the problem of bacterial resistance has become a serious problem worldwide, it was necessary to search for new active substances that can overcome the problem and enhance the treatment efficacy of bacterial infections. Numerous plant-derived essential oils exhibited significant antibacterial activities. This review aimed to summarize the most promising essential oils that exhibited remarkable antibacterial activities against various bacterial infections, including staphylococcal infections, Helicobacter pylori infections, skin infections, tuberculosis infection and dental bacterial infection. The synergy effect of essential oils in combination with antibiotics, as well as their role in the treatment of bacterial infections have been discussed. Essential oils can be used as models for further studies in vivo and clinical trials.

  15. TRYPANOCIDAL ACTIVE COMPOUNDS FROM SCOTTISH ABIES NOBILIS AND PINUS SYLVESTRIS

    Directory of Open Access Journals (Sweden)

    Veronique Seidel

    2013-02-01

    Full Text Available Three active compounds obtained from the aerial parts of Abies nobilis and Pinus sylvestris isolated by different chromatographic techniques. Their structures were identified by NMR (1H, 13C, COSY, HMBC spectroscopic and mass spectrometric data and established as catechin, dehydroabietic acid and Dihydroconiferyl alcohol. The isolated compounds were exhibited activity against blood stream form of parasite Trypanosoma brucei brucei (S 427.

  16. Relationship between electronic properties and drug activity of seven quinoxaline compounds: A DFT study

    Science.gov (United States)

    Behzadi, Hadi; Roonasi, Payman; Assle taghipour, Khatoon; van der Spoel, David; Manzetti, Sergio

    2015-07-01

    The quantum chemical calculations at the DFT/B3LYP level of theory were carried out on seven quinoxaline compounds, which have been synthesized as anti-Mycobacterium tuberculosis agents. Three conformers were optimized for each compound and the lowest energy structure was found and used in further calculations. The electronic properties including EHOMO, ELUMO and related parameters as well as electron density around oxygen and nitrogen atoms were calculated for each compound. The relationship between the calculated electronic parameters and biological activity of the studied compounds were investigated. Six similar quinoxaline derivatives with possible more drug activity were suggested based on the calculated electronic descriptors. A mechanism was proposed and discussed based on the calculated electronic parameters and bond dissociation energies.

  17. Biological Activities of a Thai Luminescent Mushroom

    Directory of Open Access Journals (Sweden)

    Jiraporn BURAKORN

    2015-06-01

    Full Text Available Wild fruit bodies of luminescent mushrooms were collected from wood stumps over a period covering August to October 2011 in the Kosumpisai forest, Mahasarakham province, in the Northeast of Thailand. A study of the morphological and genetic characteristics of the luminescent mushroom suggested that it was Neonothopanus nimbi KS. The fruiting bodies and mycelium of Neonothopanus nimbi KS were assayed for their antimicrobial activities, antifungal activity, inhibitory activity against avian influenza H5N1 neuraminidase (NA, and anticancer activity, using organic solvent extracts. The results showed that only the methanol extract of mycelia was effective against Bacillus sphaericus, with the widest inhibition zone of 11.66±2.71 mm, but this was not effective against the other 3 bacteria (Pseudomonas aeruginosa, Serratia marcescens, and Escherichia coli. On the other hand, all of the fruit body extracts were inactive against all four bacteria. The ethylacetate extract of mycelia inhibited the NCI-H187 small lung cancer cell line, KB oral cavity cancer cell line, and the MCF7 breast cancer cell line, including Magnaporthe grisea and Curvularia lunata. The methanol extract of mycelia inhibited the KB oral cavity cell cancer cell line, Magnaporthe grisea, and Curvularia lunata at 96.66, 95.32 and 95.41 %, respectively. The results imply that polar extracts of mycelia are a resource of bioactive compounds, whereas extracts of fruit bodies have less inhibitory activity against cancer, phytopathogenic-fungi and H5N1 neuraminidase.

  18. [Advances in studies on chemical constituents and biological activities of Desmodium species].

    Science.gov (United States)

    Liu, Chao; Wu, Ying; Zhang, Qian-Jun; Kang, Wen-Yi; Zhang, Long; Zhou, Qing-Di

    2013-12-01

    The chemical constituents isolated from Desmodium species (Leguminosae) included terpenoids, flavonoids, steroids, alkaloids compounds. Modem pharmacological studies have showed that the Desmodium species have antioxidant, antibacterial, anti-inflammatory, hepatoprotective, diuretic, antipyretic, analgesic and choleretic activity. This article mainly has reviewed the research advances of chemical constituents and biological activities of Desmodium species since 2003.

  19. Transport and biological activities of bile acids.

    Science.gov (United States)

    Zwicker, Brittnee L; Agellon, Luis B

    2013-07-01

    Bile acids have emerged as important biological molecules that support the solubilization of various lipids and lipid-soluble compounds in the gut, and the regulation of gene expression and cellular function. Bile acids are synthesized from cholesterol in the liver and eventually released into the small intestine. The majority of bile acids are recovered in the distal end of the small intestine and then returned to the liver for reuse. The components of the mechanism responsible for the recycling of bile acids within the enterohepatic circulation have been identified whereas the mechanism for intracellular transport is less understood. Recently, the ileal lipid binding protein (ILBP; human gene symbol FABP6) was shown to be needed for the efficient transport of bile acids from the apical side to the basolateral side of enterocytes in the distal intestine. This review presents an overview of the transport of bile acids between the liver and the gut as well as within hepatocytes and enterocytes. A variety of pathologies is associated with the malfunction of the bile acid transport system.

  20. [Antioxidant and antibacterial activities of dimeric phenol compounds].

    Science.gov (United States)

    Ogata, Masahiro

    2008-08-01

    We studied the antioxidant and antibacterial activities of monomeric and dimeric phenol compounds. Dimeric compounds had higher antioxidant activities than monomeric compounds. Electron spin resonance spin-trapping experiments showed that phenol compounds with an allyl substituent on their aromatic rings directly scavenged superoxide, and that only eugenol trapped hydroxyl radicals. We developed a generation system of the hydroxyl radical without using any metals by adding L-DOPA and DMPO to PBS or MiliQ water in vitro. We found that eugenol trapped hydroxyl radicals directly and is metabolized to a dimer. On the other hand, dipropofol, a dimer of propofol, has strong antibacterial activity against Gram-positive bacteria. However, it lacks solubility in water and this property is assumed to limit its efficacy. We tried to improve the solubility and found a new solubilization method of dipropofol in water with the addition of a monosaccharide or ascorbic acid.

  1. Investigating the spectrum of biological activity of ring-substituted salicylanilides and carbamoylphenylcarbamates.

    Science.gov (United States)

    Otevrel, Jan; Mandelova, Zuzana; Pesko, Matus; Guo, Jiahui; Kralova, Katarina; Sersen, Frantisek; Vejsova, Marcela; Kalinowski, Danuta S; Kovacevic, Zaklina; Coffey, Aidan; Csollei, Jozef; Richardson, Des R; Jampilek, Josef

    2010-11-10

    In this study, a series of twelve ring-substituted salicylanilides and carbamoylphenylcarbamates were prepared and characterized. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Moreover, their site of action in the photosynthetic apparatus was determined. Primary in vitro screening of the synthesized compounds was also performed against mycobacterial, bacterial and fungal strains. Several compounds showed biological activity comparable with or higher than the standards 3-(3,4-dichlorophenyl)-1,1-dimethylurea, isoniazid, penicillin G, ciprofloxacin or fluconazole. The most active compounds showed minimal anti-proliferative activity against human cells in culture, indicating they would have low cytotoxicity. For all compounds, the relationships between lipophilicity and the chemical structure are discussed.

  2. Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates

    Directory of Open Access Journals (Sweden)

    Josef Jampilek

    2010-11-01

    Full Text Available In this study, a series of twelve ring-substituted salicylanilides and carbamoylphenylcarbamates were prepared and characterized. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET in spinach (Spinacia oleracea L. chloroplasts. Moreover, their site of action in the photosynthetic apparatus was determined. Primary in vitro screening of the synthesized compounds was also performed against mycobacterial, bacterial and fungal strains. Several compounds showed biological activity comparable with or higher than the standards 3-(3,4-dichlorophenyl-1,1-dimethylurea, isoniazid, penicillin G, ciprofloxacin or fluconazole. The most active compounds showed minimal anti-proliferative activity against human cells in culture, indicating they would have low cytotoxicity. For all compounds, the relationships between lipophilicity and the chemical structure are discussed.

  3. Biological activities of radiation-degraded carrageenan

    Energy Technology Data Exchange (ETDEWEB)

    Relleve, Lorna; Dela Rosa, Alumanda; ABAD, Lucille; Aranilla, Charito; Aliganga, Anne Kathrina [Philippine Nuclear Research Institute, Quezon City (Philippines); Yoshii, Fumio; Kume, Tamikazu; Nagasawa, Naotsugu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment

    2001-03-01

    Carrageenans were irradiated in solid state to doses 50-1000 kGy in air at ambient temperature. Changes in their molecular weight and functional properties with respect to their FT-IR and UV spectra were evaluated. Irradiation of carrageenans resulted in a rapid decrease of molecular weight indicating main chain scission in their polymeric structures. Formations of some compounds were evident by new absorption peaks in their UV and FT-IR spectra and quantitative analyses of the FT-IR spectra which, in addition, support that there is a breakdown in the carrageenan structure. Irradiated carrageenans were investigated for their plant growth-promoting activity. Carrageenans were added to the nutrient solutions for rice seedlings under non-circulating hydroponics cultivation. Irradiated carrageenan induced weight gain in treated rice seedlings. Maximum weight gain was obtained with KC irradiated at 100 kGy while treatment with IC at 500 kGy. IC exhibited less growth promoting properties than KC. The growth of fungi on the roots disappeared with treatment of IC and KC irradiated at 500 kGy. Growth promotion of some leafy vegetables was also observed with application of degraded KC. The carrageenan molecule has been broken down to smaller molecule (s) or compound (s) that can be absorbed effectively as nourishment factors and anti-microbial agents by plants. (author)

  4. Synthesis, Characterization and Biological Activities of Novel Water-soluble Metalloporphyrins

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    The synthesis, characterization, and biological activities of a series of metal porphyrins were described. The complexes 3a~3e were prepared from the reaction of compound 2 with M(OAc)2 in CHCl3, and the treatment of 3a~3f with pyridine gave corresponding complexes 4a~4f. These new compounds were identified by absorption spectroscopies, 1H NMR and elemental analysis. The results of biological activity testing revealed that 4a and 4c had stronger inhibiting action for Escherichia coli (CCTCC AB91115).

  5. Synthesis and Assay of SIRT1-Activating Compounds.

    Science.gov (United States)

    Dai, H; Ellis, J L; Sinclair, D A; Hubbard, B P

    2016-01-01

    The NAD(+)-dependent deacetylase SIRT1 plays key roles in numerous cellular processes including DNA repair, gene transcription, cell differentiation, and metabolism. Overexpression of SIRT1 protects against a number of age-related diseases including diabetes, cancer, and Alzheimer's disease. Moreover, overexpression of SIRT1 in the murine brain extends lifespan. A number of small-molecule sirtuin-activating compounds (STACs) that increase SIRT1 activity in vitro and in cells have been developed. While the mechanism for how these compounds act on SIRT1 was once controversial, it is becoming increasingly clear that they directly interact with SIRT1 and enhance its activity through an allosteric mechanism. Here, we present detailed chemical syntheses for four STACs, each from a distinct structural class. Also, we provide a general protocol for purifying active SIRT1 enzyme and outline two complementary enzymatic assays for characterizing the effects of STACs and similar compounds on SIRT1 activity.

  6. Litchi Flavonoids: Isolation, Identification and Biological Activity

    Directory of Open Access Journals (Sweden)

    Yueming Jiang

    2007-04-01

    Full Text Available The current status of the isolation, identification, biological activity, utilization and development prospects of flavonoids found in litchi fruit pericarp (LFP tissues is reviewed. LFP tissues account for approximately 15% by weight of the whole fresh fruit and are comprised of significant amount of flavonoids. The major flavonoids in ripe LFP include flavonols and anthocyanins. The major flavanols in the LFP are reported to be procyanidin B4, procyanidin B2 and epicatechin, while cyanindin-3-rutinside, cyanidin-3-glucoside, quercetin-3-rutinosde and quercetin-3-glucoside are identified as the important anthocyanins. Litchi flavanols and anthocyanins exhibit good potential antioxidant activity. The hydroxyl radical and superoxide anion scavenging activities of procyanidin B2 are greater than those of procyanidin B4 and epicatechin, while epicatechin has the highest α,α-diphenyl-β-picrylhydrazyl radical (DPPH· scavenging activity. In addition to the antioxidant activity, LFP extract displays a dose- and time-dependent inhibitory effect on human breast cancer, which could be attributed, in part, to its inhibition of proliferation and induction of apoptosis in cancer cells through upregulation and down-regulation of multiple genes. Furthermore, various anticancer activities are observed for epicatechin, procyanidin B2, procyanidin B4 and the ethyl acetate fraction of LFP tissue extracts. Procyanidin B4 and the ethyl acetate fraction show a stronger inhibitory effect on HELF than MCF-7 proliferation, while epicatechin and procyanidin B2 have lower cytotoxicities towards MCF-7 and HELF than paclitaxel. It is therefore suggested that flavonoids from LFP might be potentially useful components for functional foods and/or anti-breast cancer drugs.

  7. Isolation and anticomplement activity of compounds from Dendropanax morbifera.

    Science.gov (United States)

    Park, Bo-Young; Min, Byung-Sun; Oh, Sei-Ryang; Kim, Jung-Hee; Kim, Tae-Jin; Kim, Dong-Hee; Bae, Ki-Hwan; Lee, Hyeong-Kyu

    2004-02-01

    Dendropanax morbifera Leveille (Araliaceae) is used in Korea for a variety of disease, such as migraine headache and dysmenorrhea. A new polyacetylene (1) and six known compounds (2-7) were isolated from the leaves of this plant by conventional chromatographic techniques. The structure of the new polyacetylene (1) was determined as (9Z,16S)-16-hydroxy-9,17-octadecadiene-12,14-diynoic acid by spectroscopic means including 2D NMR, which comprised the determination of a chiral by modified Mosher's ester method. Compounds 1-7 were investigated in vitro for their anticomplement activity against the classical pathway of the complement system. Of these, compound 1 showed significant anticomplement activity with 50% inhibitory concentration (IC50) value of 56.98 microM, whereas compounds 2-7 were inactive.

  8. Potential therapeutic effects of functionally active compounds isolated from garlic.

    Science.gov (United States)

    Yun, Hyung-Mun; Ban, Jung Ok; Park, Kyung-Ran; Lee, Chong Kil; Jeong, Heon-Sang; Han, Sang Bae; Hong, Jin Tae

    2014-05-01

    The medicinal properties of functionally active organosulfur compounds such as allin, diallyl disulfide, S-allylmercaptocysteine, and S-trityl-L-cysteine isolated from garlic have received great attention from a large number of investigators who have studied their pharmacological effects for the treatment of various diseases. These organosulfur compounds are able to prevent for development of cancer, cardiovascular, neurological, and liver diseases as well as allergy and arthritis. There have been also many reports on toxicities and pharmacokinetics of these compounds. The aim of this study is to review a variety of experimental and clinical reports, and describe the effectiveness, toxicities and pharmacokinetics, and possible mechanisms of pharmaceutical actions of functionally active compounds isolated from garlic.

  9. Endophytic fungi with antitumor activities: Their occurrence and anticancer compounds.

    Science.gov (United States)

    Chen, Ling; Zhang, Qiao-Yan; Jia, Min; Ming, Qian-Liang; Yue, Wei; Rahman, Khalid; Qin, Lu-Ping; Han, Ting

    2016-05-01

    Plant endophytic fungi have been recognized as an important and novel resource of natural bioactive products, especially in anticancer application. This review mainly deals with the research progress on the production of anticancer compounds by endophytic fungi between 1990 and 2013. Anticancer activity is generally associated with the cytotoxicity of the compounds present in the endophytic fungi. All strains of endophytes producing antitumor chemicals were classified taxonomically and the genera of Pestalotiopsis and Aspergillus as well as the taxol producing endophytes were focused on. Classification of endophytic fungi producing antitumor compounds has received more attention from mycologists, and it can also lead to the discovery of novel compounds with antitumor activity due to phylogenetic relationships. In this review, the structures of the anticancer compounds isolated from the newly reported endophytes between 2010 and 2013 are discussed including strategies for the efficient production of the desired compounds. The purpose of this review is to provide new directions in endophytic fungi research including integrated information relating to its anticancer compounds.

  10. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: MODELING

    Directory of Open Access Journals (Sweden)

    Brînduşa-Antonela SBÎRCEA

    2011-01-01

    Full Text Available By using active and participatory methods it is hoped that pupils will not only come to a deeper understanding of the issues involved, but also that their motivation will be heightened. Pupil involvement in their learning is essential. Moreover, by using a variety of teaching techniques, we can help students make sense of the world in different ways, increasing the likelihood that they will develop a conceptual understanding. The teacher must be a good facilitator, monitoring and supporting group dynamics. Modeling is an instructional strategy in which the teacher demonstrates a new concept or approach to learning and pupils learn by observing. In the teaching of biology the didactic materials are fundamental tools in the teaching-learning process. Reading about scientific concepts or having a teacher explain them is not enough. Research has shown that modeling can be used across disciplines and in all grade and ability level classrooms. Using this type of instruction, teachers encourage learning.

  11. Biologically Active and Antimicrobial Peptides from Plants

    Directory of Open Access Journals (Sweden)

    Carlos E. Salas

    2015-01-01

    Full Text Available Bioactive peptides are part of an innate response elicited by most living forms. In plants, they are produced ubiquitously in roots, seeds, flowers, stems, and leaves, highlighting their physiological importance. While most of the bioactive peptides produced in plants possess microbicide properties, there is evidence that they are also involved in cellular signaling. Structurally, there is an overall similarity when comparing them with those derived from animal or insect sources. The biological action of bioactive peptides initiates with the binding to the target membrane followed in most cases by membrane permeabilization and rupture. Here we present an overview of what is currently known about bioactive peptides from plants, focusing on their antimicrobial activity and their role in the plant signaling network and offering perspectives on their potential application.

  12. Barbiturate bearing aroylhydrazine derivatives: Synthesis, NMR investigations, single crystal X-ray studies and biological activity

    Science.gov (United States)

    Giziroglu, Emrah; Sarikurkcu, Cengiz; Aygün, Muhittin; Basbulbul, Gamze; Soyleyici, H. Can; Firinci, Erkan; Kirkan, Bulent; Alkis, Ayse; Saylica, Tayfur; Biyik, Halil

    2016-03-01

    A series of barbituric acid aroylhydrazine derivatives have been prepared from their corresponding 1,3-dimethyl-5-acetyl barbituric acid and aroylhydrazines. All compounds have been fully characterized by using FT-IR, multinuclear NMR (1H, 13C) and Mass (MS) spectrometry. We also describe the X-ray crystal structure of 3a, which crystallizes in the monoclinic P21/n space group. The crystal structure is stabilized with infinite linear chains of dimeric units. Furthermore, all compounds were investigated for their tyrosinase inhibition, antioxidative and antimicrobial activies. The results from biological activity assays have shown that all of compounds have excellent antioxidant, significant tyrosinase inhibition and moderate antimicrobial activity.

  13. Inorganic sulfur-nitrogen compounds: from gunpowder chemistry to the forefront of biological signaling.

    Science.gov (United States)

    Cortese-Krott, Miriam M; Butler, Anthony R; Woollins, J Derek; Feelisch, Martin

    2016-04-14

    The reactions between inorganic sulfur and nitrogen-bearing compounds to form S-N containing species have a long history and, besides assuming importance in industrial synthetic processes, are of relevance to microbial metabolism; waste water treatment; aquatic, soil and atmospheric chemistry; and combustion processes. The recent discovery that hydrogen sulfide and nitric oxide exert often similar, sometimes mutually dependent effects in a variety of biological systems, and that the chemical interaction of these two species leads to formation of S-N compounds brought this chemistry to the attention of physiologists, biochemists and physicians. We here provide a perspective about the potential role of S-N compounds in biological signaling and briefly review their chemical properties and bioactivities in the context of the chronology of their discovery. Studies of the biological role of NO revealed why its chemistry is ideally suited for the tasks Nature has chosen for it; realising how the distinctive properties of sulfur can enrich this bioactivity does much to revive 'die Freude am experimentellen Spiel' of the pioneers in this field.

  14. Designing, syntheses, characterization, computational study and biological activities of silver-phenothiazine metal complex

    Science.gov (United States)

    Kumar, Vijay; Upadhyay, Niraj; Manhas, Anu

    2015-11-01

    A noble biologically active compound Ag(I)-PTZ metal complex (1) with spherical morphology was synthesized first time. Entire characterization tool (spectral, elemental, mass and thermal analysis) was supported a distorted tetrahedral structure, where two water compounds were coordinated with Ag(I) including one phenothiazine and one nitrate group. For the better insight, obtained spectral/structural results were supported by 3D molecular modeling. Compound 1 had shown excellent activities against the Salmonella typhimurium and Aspergillus fumigatus with minimum inhibitory concentration (MIC) value 20 mg/L and 25 mg/L. The observed antioxidant radical scavenging activity (in %) of compound 1 (62.74%) was more than control ascorbic acid (28.58%). The observed protein (BSA) binding constant of 1 was 8.86 × 104 M-1, which is similar to binding constant of salicylic acid with BSA protein. Initial studies have revealed that synthesized compound 1 may act as multipurpose drug analogue in future.

  15. Synthesis and anticonvulsant activity of certain chalcone based pyrazoline compounds

    Directory of Open Access Journals (Sweden)

    Sudhakara Rao Gerapati

    2015-09-01

    Full Text Available Convulsions are involuntary, violent, spasmodic and prolonged contractions of skeletal muscles. That means a patient may have epilepsy without convulsions and vice versa. Epilepsy is a common neurological abnormality affecting about 1% of the world population. The primary objectives of these synthesized compounds are to suppress seizures and provide neuroprotection by minimizing the effects from seizure attacks. Here some of the chalcones and chalcone based various pyrazolines were evaluated for anticonvulsant activity. Their structures have been elucidated on the basis of elemental analyses and spectroscopic studies (IR, 1H-NMR & Mass spectroscopy. A preliminary evaluation of the prepared compounds has indicated that some of them exhibit moderate to significant anticonvulsant activity compared to a diazepam standard1-3.  All compounds were tested for their anticonvulsant activity using maximal electroshock induced convulsions (MES in mice at a dose level of 4 mg/kg.b.w. The compounds  Ph1, Ph2 , Py2 ,Py3 and Py4 have shown  to  good anticonvulsant activity when doses are administered as 25mg/ kg.b.w  , reduced the phases of seizures severity and  found to be active and also  increased survival rate. Remaining compounds are less efficacious.

  16. Study of Biological Activity of Some New Heterocyclic Compounds Synthesized on Base of Furfural%基于糠醛合成的几种新杂环化合物的生物学活性研究

    Institute of Scientific and Technical Information of China (English)

    Nori.,MV; Susl.,TA

    2000-01-01

    本研究以醛和酮进行缩合反应并进而转化成3种新的呋喃基取代尿素:丁基-呋喃基-尿素(BFC)、二丁基-呋喃基尿素(DIBFC)、二氯苯基-丁基-尿素;分别在播前浸种处理禾本科类和蔬菜种子,结果表明它们具有促进作物生长及提高免疫力的作用.进一步的研究证实这3种杂环化合物可以提高植物叶片中过氧化物酶的活性,从而使作物的产量和抗病性得以提高,作物过氧化物酶的活性与其抗病性及产量之间存在一种正相关关系(r=0.7).%The article examines methods of furfural production as a result of its condensation with aldehydes and ketones and further transformations to new fury lsubstituted carbamides. Their growth generating and immunization activity is sh own in pre-sowing treatment of seeds of vegetables and cereals. The role of per o xidase in protective functions of plants is confirmed. The activity of peroxidaz e in the plant leaves shows the immunization impact of the preparations. Positiv e correlation between peroxidaze activity, resistance to pathogens and yield cap acity was discovered (r=0.7).

  17. Synthesis and biological evaluation of glyco-GA compounds as anticancer agents

    Institute of Scientific and Technical Information of China (English)

    Li Qin He; Zhong Hu; La Mei Yuan; Xiao Shan Wang; Yi Hua Zhang

    2012-01-01

    A series of novel glyco-gambogic acid (GA) compounds were synthesized and evaluated for their in vitro anti-proliferative activity against human hepatocellular carcinoma (HCC) cells.All compounds showed much better aqueous solubility (0.92-1.89 mg/mL) than GA (0.013 mg/mL),and displayed potent inhibition on HCC cells (IC50:0.21-12.23 μmol/L) and little affects on non-tumor liver cells (IC50:42.56-86.43 μmol/L),suggesting that glyco-GA compounds selectively inhibit HCC proliferation,and may be promising candidates for further intensive study.

  18. Production and biological activities of yellow pigments from Monascus fungi.

    Science.gov (United States)

    Chen, Gong; Wu, Zhenqiang

    2016-08-01

    Monascus yellow pigments (MYPs), are azaphilone compounds and one of the three main components of total Monascus pigments (MPs). Thirty-five hydrophilic or hydrophobic MYPs have been identified, with the majority being hydrophobic. Apart from screening special Monascus strains, some advanced approaches, such as extractive and high-cell-density fermentations, have been applied for developing or producing new MYPs, especially extracellular hydrophilic MYPs. The outstanding performance of MYPs in terms of resistance to photodegradation, as well as tolerance for temperature and pH, give natural MYPs reasonable prospects, compared with the orange and red MPs, for practical use in the present and future. Meanwhile, MYPs have shown promising potential for applications in the food and pharmaceutical industries based on their described bioactivities. This review briefly summarizes the reports to date on chemical structures, biological activities, biosynthetic pathways, production technologies, and physicochemical performances of MYPs. The existing problems for MYPs are discussed and research prospects proposed.

  19. Current parallel chemistry principles and practice: application to the discovery of biologically active molecules.

    Science.gov (United States)

    Edwards, Paul J

    2009-11-01

    This article describes the use of parallel chemistry techniques for drug discovery, based on publications from January 2006 to December 2008. Chemical libraries that yielded active compounds across a range of biological targets are presented, together with synthetic details when appropriate. Background information for the biological targets involved and any SAR that could be discerned within members of a library series also is discussed. New technological developments, as applied to library design and synthesis and, more generally, in the discovery of biologically active entities, are highlighted. In addition, the likely future directions for parallel chemistry in its ability to impact upon drug discovery are also presented.

  20. Bactericidal activity of glutaraldehyde-like compounds from olive products.

    Science.gov (United States)

    Medina, Eduardo; Brenes, Manuel; García, Aranzazu; Romero, Concepción; de Castro, Antonio

    2009-12-01

    The bactericidal effects of several olive compounds (nonenal, oleuropein, tyrosol, the dialdehydic form of decarboxymethyl elenolic acid either free [EDA] or linked to tyrosol [TyEDA] or to hydroxytyrosol [HyEDA]), other food phenolic compounds (catechin, epicatechin, eugenol, thymol, carvacrol, and carnosic acid), and commercial disinfectants (glutaraldehyde [GTA] and ortho-phthalaldehyde [OPA]), were tested against strains of Pseudomonas fluorescens, Staphylococcus aureus, Enterococcus faecalis, and Escherichia coli. It was found that the bactericidal activities of olive GTA-like compounds (EDA, HyEDA, and TyEDA) were greater than those exerted by several food phenolic substances. Surprisingly, these olive antimicrobials were as active as the synthetic biocides GTA and OPA against the four bacteria studied. Thus, it has been proposed that the bactericidal activity of the main olive antimicrobials is primarily due to their dialdehydic structure, which is similar to that of the commercial biocides GTA and OPA. Our results clearly reveal that olive GTA-like compounds possess a strong bactericidal activity even greater than that of other food phenolic compounds or synthetic biocides.

  1. Synthesis, Crystal Structure and Biological Activities of Novel Anthranilic(Isophthalic) Acid Esters

    Institute of Scientific and Technical Information of China (English)

    YAN Tao; YU Guan-ping; LIU Peng-fei; XIONG Li-xia; YU Shu-jing; LI Zheng-ming

    2012-01-01

    In search of environmentally benign insecticides with high activity,low toxicity and low resistance,a series of novel anthranilic(isophthalic) acid esters was designed and synthesized based on the structure of ryanodine modulating agent.All the compounds were characterized by 1H NMR spectra,elemental analysis or high resolution mass spectrometry(HRMS).The preliminary results of biological activity assessment indicate that some of the title compounds exhibit certain but unremarkable insecticidal activity against Mythimna separata Walker at 200 mg/L and fungicidal activities against five funguses at 50 mg/L.

  2. Cryptic antifungal compounds active by synergism with polyene antibiotics.

    Science.gov (United States)

    Kinoshita, Hiroshi; Yoshioka, Mariko; Ihara, Fumio; Nihira, Takuya

    2016-04-01

    The majority of antifungal compounds reported so far target the cell wall or cell membrane of fungi, suggesting that other types of antibiotics cannot exert their activity because they cannot penetrate into the cells. Therefore, if the permeability of the cell membrane could be enhanced, many antibiotics might be found to have antifungal activity. We here used the polyene antibiotic nystatin, which binds to ergosterol and forms pores at the cell membrane, to enhance the cellular permeability. In the presence of nystatin, many culture extracts from entomopathogenic fungi displayed antifungal activity. Among all the active extracts, two active components were purified and identified as helvolic acid and terramide A. Because the minimum inhibitory concentration of either compound was reduced four-fold in the presence of nystatin, it can be concluded that this screening method is useful for detecting novel antifungal activity.

  3. Fruit cuticular waxes as a source of biologically active triterpenoids.

    Science.gov (United States)

    Szakiel, Anna; Pączkowski, Cezary; Pensec, Flora; Bertsch, Christophe

    2012-06-01

    The health benefits associated with a diet rich in fruit and vegetables include reduction of the risk of chronic diseases such as cardiovascular disease, diabetes and cancer, that are becoming prevalent in the aging human population. Triterpenoids, polycyclic compounds derived from the linear hydrocarbon squalene, are widely distributed in edible and medicinal plants and are an integral part of the human diet. As an important group of phytochemicals that exert numerous biological effects and display various pharmacological activities, triterpenoids are being evaluated for use in new functional foods, drugs, cosmetics and healthcare products. Screening plant material in the search for triterpenoid-rich plant tissues has identified fruit peel and especially fruit cuticular waxes as promising and highly available sources. The chemical composition, abundance and biological activities of triterpenoids occurring in cuticular waxes of some economically important fruits, like apple, grape berry, olive, tomato and others, are described in this review. The need for environmentally valuable and potentially profitable technologies for the recovery, recycling and upgrading of residues from fruit processing is also discussed.

  4. Composition for the controlled release of active compounds

    NARCIS (Netherlands)

    Hovens, I.A.P.; Jongboom, R.O.J.; Stuut, P.I.

    1999-01-01

    The invention provides a composition for the controlled release of one or more biologically active substances encapsulated in a degradable biopolymer matrix, consisting of a thermoplastic and/or partly crystalline inulin. A plasticiser such as glycerol, and an emulsifier may be present. The active s

  5. Xanthine oxidase inhibitory activity of compounds from Chythrantus claneianus

    Directory of Open Access Journals (Sweden)

    Anar Sahib Gojayev

    2013-03-01

    Full Text Available Phytochemical investigation of the stem bark and the trunk of Chythrantus claneianus led to the isolation of six known compounds named β-sitosterol (1, umbelliferone (2, scopoletin (3, benjaminamide (4, β-sitosterol-3-O-β-D-glucopyranoside (5 and Panconoside B (6. All these compounds were isolated for the first time from this plant species. The chemical structures of isolates were elucidated on the basis of 1 and 2 D-NMR spectra and other spectroscopic techniques including UV–vis, FT-IR, HR-ESIMS and HR-FABMS. The isolates were tested in vitro for their inhibitory properties towards xanthine oxidase enzyme. Compounds 2, 3 and 6 showed weak inhibi-tory activities on the enzyme with IC50 values ranging from 307 µM for com-pound 6 to 475 µM for compound 3, while the extract and compounds 1, 4 and 5 showed extremely weak activities with inhibition percentage less than 50%.

  6. Occurrence, biological activities and {sup 13}C NMR data of amides from Piper (Piperaceae)

    Energy Technology Data Exchange (ETDEWEB)

    Nascimento, Jeferson C. do; Paula, Vanderlucia F. de [Universidade Estadual do Sudoeste da Bahia, Jequie, BA (Brazil). Dept. de Quimica e Exatas; David, Jorge M. [Universidade Federal da Bahia (UFBA), Salvador, BA (Brazil). Inst. de Quimica; David, Juceni P., E-mail: jmdavid@ufba.br [Universidade Federal da Bahia (UFBA), Salvador, BA (Brazil). Fac. de Farmacia

    2012-07-01

    This manuscript describes an update review with up to 285 references concerning the occurrence of amides from a variety of species of the genus Piper (Piperaceae). Besides addressing occurrence, this review also describes the biological activities attributed to extracts and pure compounds, a compiled {sup 13}C NMR data set, the main correlations between structural and NMR spectroscopic data of these compounds, and employment of hyphened techniques such as LC-MS, GC-MS and NMR for analysis of amides from biological samples and crude Piper extracts. (author)

  7. Occurrence, biological activities and 13C NMR data of amides from Piper (Piperaceae

    Directory of Open Access Journals (Sweden)

    Jeferson C. do Nascimento

    2012-01-01

    Full Text Available This manuscript describes an update review with up to 285 references concerning the occurrence of amides from a variety of species of the genus Piper (Piperaceae. Besides addressing occurrence, this review also describes the biological activities attributed to extracts and pure compounds, a compiled 13C NMR data set, the main correlations between structural and NMR spectroscopic data of these compounds, and employment of hyphened techniques such as LC-MS, GC-MS and NMR for analysis of amides from biological samples and crude Piper extracts.

  8. New materials and biologically active preparations on the basis of (organilthio) chloroacetylene

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    @@ (Organylthio)chloroacetylenes [RSC≡CCl, 1], the object of our systematic research, provide a promising source of new classes of polyfunctional compounds of acetylenic and polyheterocyclic seriesamong which biologically active substances, monomers and precursors for the preparation of new materials possessing a whole complex of valuable properties have been recognized.

  9. New materials and biologically active preparations on the basis of (organilthio) chloroacetylene

    Institute of Scientific and Technical Information of China (English)

    D'yachkova; S.; G.

    2005-01-01

    (Organylthio)chloroacetylenes [RSC≡CCl, 1], the object of our systematic research, provide a promising source of new classes of polyfunctional compounds of acetylenic and polyheterocyclic seriesamong which biologically active substances, monomers and precursors for the preparation of new materials possessing a whole complex of valuable properties have been recognized.……

  10. Byrsonima fagifolia Niedenzu Apolar Compounds with Antitubercular Activity

    Directory of Open Access Journals (Sweden)

    C. T. Higuchi

    2011-01-01

    Full Text Available Bioassay-guided fractionation of the chloroform extract of Byrsonima fagifolia leaves led to the isolation of active antitubercular compounds alkane dotriacontane (Minimal Inhibitory Concentration—MIC, 62.5 μg mL−1, triterpenoids as bassic acid (MIC = 2.5 μg mL−1, α-amyrin acetate (MIC = 62.5 μg mL−1, a mixture of lupeol, α- and β-amyrin (MIC = 31.5 μg mL−1 and a mixture of lupeol, and acetates of α- and β-amyrin (MIC = 31.5 μg mL−1. The antimycobacterial activity was determined by the Microplate Alamar Blue Assay (MABA and the structures of promising compounds were determined by spectroscopic analysis. This investigation constitutes the first report of a chemical and antitubercular study of apolar compounds from B. fagifolia Niedenzu (IK.

  11. Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds

    Directory of Open Access Journals (Sweden)

    Da-Jun Zhang

    2014-01-01

    Full Text Available A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC50 = 3.21–5.06 μM and 3g (IC50 = 0.71–34.87 μM showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus and a DNA virus (HBV at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses.

  12. Phytochemical profile and biological activity of Juglans regia.

    Science.gov (United States)

    Panth, Nisha; Paudel, Keshav Raj; Karki, Rajendra

    2016-09-01

    Juglans regia Linn. (Juglandaceae), popularly known as English or Persian walnut, is a valuable medicinal plant with a potency to cure various diseases in traditional medicine. Since ancient time, different local ethnic groups have used various part of J. regia for a wide array of ailments including helminthiasis, diarrhea, sinusitis, stomach ache, arthritis, asthma, eczema, scrofula, skin disorders, diabetes mellitus, anorexia, thyroid dysfunction, cancer and infectious diseases. Biological activities of J. regia have been reported in several peer review journals and scientific attention is increasing. The present review attempts to provide comprehensive information on plant description, ethnobotanical use, toxicity, phytochemical profile, pharmacology, clinical studies and current research prospective of the J. regia. Currently, there is an immense interest on isolation/identification of active constituents from walnut and screening those active compounds for pharmacological activities. In addition, researchers are performing clinical trials as well as screening various solvent extracts or fractions of J. regia in several animal diseases models to identify promising therapeutic benefits. In the present work, we review the latest information based on published scientific investigations of J. regia.

  13. Phytochemical profi le and biological activity of Juglans regia

    Institute of Scientific and Technical Information of China (English)

    Nisha Panth; Keshav Raj Paudel; Rajendra Karki

    2016-01-01

    Juglans regia Linn. (Juglandaceae), popularly known as English or Persian walnut, is a valuable medicinal plant with a potency to cure various diseases in traditional medicine. Since ancient time, different local ethnic groups have used various part ofJ. regia for a wide array of ailments including helminthiasis, diarrhea, sinusitis, stomach ache, arthritis, asthma, eczema, scrofula, skin disorders, diabetes melitus, anorexia, thyroid dysfunction, cancer and infectious diseases. Biological activities of J. regia have been reported in several peer review journals and scientifi c attention is increasing. The present review attempts to provide comprehensive information on plant description, ethnobotanical use, toxicity, phytochemical profi le, pharmacology, clinical studies and current research prospective of theJ. regia. Currently, there is an immense interest on isolation/identifi cation of active constituents from walnut and screening those active compounds for pharmacological activities. In addition, researchers are performing clinical trials as wel as screening various solvent extracts or fractions ofJ. regiain several animal diseases models to identify promising therapeutic benefi ts. In the present work, we review the latest information based on published scientifi c investigations ofJ. regia.

  14. Biological activity of Serratia marcescens cytotoxin

    Directory of Open Access Journals (Sweden)

    G.V. Carbonell

    2003-03-01

    Full Text Available Serratia marcescens cytotoxin was purified to homogeneity by ion-exchange chromatography on a DEAE Sepharose Fast Flow column, followed by gel filtration chromatography on a Sephadex G100 column. The molecular mass of the cytotoxin was estimated to be about 50 kDa. Some biological properties of the cytotoxin were analyzed and compared with well-characterized toxins, such as VT1, VT2 and CNF from Escherichia coli and hemolysin produced by S. marcescens. The sensitivity of the cell lines CHO, HeLa, HEp-2, Vero, BHK-21, MA 104 and J774 to the cytotoxin was determined by the cell viability assay using neutral red. CHO and HEp-2 were highly sensitive, with massive cellular death after 1 h of treatment, followed by BHK-21, HeLa, Vero and J774 cells, while MA 104 was insensitive to the toxin. Cytotoxin induced morphological changes such as cell rounding with cytoplasmic retraction and nuclear compactation which were evident 15 min after the addition of cytotoxin. The cytotoxic assays show that 15 min of treatment with the cytotoxin induced irreversible intoxication of the cells, determined by loss of cell viability. Concentrations of 2 CD50 (0.56 µg/ml of purified cytotoxin did not present any hemolytic activity, showing that the cytotoxin is distinct from S. marcescens hemolysin. Antisera prepared against S. marcescens cytotoxin did not neutralize the cytotoxic activity of VT1, VT2 or CNF toxin, indicating that these toxins do not share antigenic determinants with cytotoxin. Moreover, we did not detect gene sequences for any of these toxins in S. marcescens by PCR assay. These results suggest that S. marcescens cytotoxin is not related to any of these toxins from E. coli.

  15. Biological activity of Serratia marcescens cytotoxin.

    Science.gov (United States)

    Carbonell, G V; Amorim, C R N; Furumura, M T; Darini, A L C; Fonseca, B A L; Yano, T

    2003-03-01

    Serratia marcescens cytotoxin was purified to homogeneity by ion-exchange chromatography on a DEAE Sepharose Fast Flow column, followed by gel filtration chromatography on a Sephadex G100 column. The molecular mass of the cytotoxin was estimated to be about 50 kDa. Some biological properties of the cytotoxin were analyzed and compared with well-characterized toxins, such as VT1, VT2 and CNF from Escherichia coli and hemolysin produced by S. marcescens. The sensitivity of the cell lines CHO, HeLa, HEp-2, Vero, BHK-21, MA 104 and J774 to the cytotoxin was determined by the cell viability assay using neutral red. CHO and HEp-2 were highly sensitive, with massive cellular death after 1 h of treatment, followed by BHK-21, HeLa, Vero and J774 cells, while MA 104 was insensitive to the toxin. Cytotoxin induced morphological changes such as cell rounding with cytoplasmic retraction and nuclear compactation which were evident 15 min after the addition of cytotoxin. The cytotoxic assays show that 15 min of treatment with the cytotoxin induced irreversible intoxication of the cells, determined by loss of cell viability. Concentrations of 2 CD50 (0.56 g/ml) of purified cytotoxin did not present any hemolytic activity, showing that the cytotoxin is distinct from S. marcescens hemolysin. Antisera prepared against S. marcescens cytotoxin did not neutralize the cytotoxic activity of VT1, VT2 or CNF toxin, indicating that these toxins do not share antigenic determinants with cytotoxin. Moreover, we did not detect gene sequences for any of these toxins in S. marcescens by PCR assay. These results suggest that S. marcescens cytotoxin is not related to any of these toxins from E. coli.

  16. Anti-Salmonella Activity of Volatile Compounds of Vietnam Coriander.

    Science.gov (United States)

    Fujita, Ken-Ichi; Chavasiri, Warinthorn; Kubo, Isao

    2015-07-01

    Essential oil derived from the fresh leaves of Polygonum odoratum Lour was tested for their effects on a foodborne bacterium Salmonella choleraesuis subsp. choleraesuis ATCC 35640 using a broth dilution method. This essential oil showed a significant antibacterial activity against S. choleraesuis at the concentration of 200 µg/mL. Twenty-five volatile compounds were characterized from this essential oil by GC-MS, and aldehyde compounds were found abundant and accounted for more than three-fourths of the essential oil. Among the compounds characterized, dodecanal (C12 ) was the most abundant (55.5%), followed by decanal (C10 ) (11.6%). Both alkanals were effective against S. choleraesuis with the minimum growth inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 100 µg/mL. The most potent antibacterial activity against this bacterium was found with two minor compounds, dodecanol (lauryl alcohol) and 2E-dodecenal, both with each MBC of 6.25 µg/mL. Their primary antibacterial action against S. choleraesuis provably comes from their ability to function as nonionic surface-active agents (surfactants), disrupting the native function of integral membrane proteins nonspecifically. Thus, the antibacterial activity is mediated by biophysical processes. In the case of 2E-alkenals, a biochemical mechanism is also somewhat involved, depending on their alkyl chain length.

  17. Anti-Inflammatory Activity of Compounds Isolated from Plants

    Directory of Open Access Journals (Sweden)

    R.M. Perez G.

    2001-01-01

    Full Text Available This review shows over 300 compounds isolated and identified from plants that previously demonstrated anti-inflammatory activity. They have been classified in appropriate chemical groups and data are reported on their pharmacological effects, mechanisms of action, and other properties.

  18. Biological and enzymatic treatment of bisphenol A and other endocrine disrupting compounds: a review.

    Science.gov (United States)

    Husain, Qayyum; Qayyum, Shariq

    2013-09-01

    Bisphenol A is predominantly used as an intermediate in the production of polycarbonate plastics and epoxy resins. Traces of bisphenol A released into the environment can reach into the wastewater and soil via application of sewage sludge from wastewater treatment systems that receive water containing bisphenol A, or from leachate from uncontrolled landfills. In this study we have made an effort to review the work on the presence of bisphenol A and other related endocrine disrupting compounds in the environment and their impact on the life of living organisms including human beings. Bisphenol A has several implications on the health of human beings as well it can also affect the growth of plants and animals. Number of physicochemical methods such as adsorption, membrane based filtration, ozonation, fenton, electrochemical and photochemical degradation has been used for the removal of bisphenol A. However, these methods have some inherent limitations and therefore cannot be used for large scale treatment of such pollutants. The alternative procedures have attracted the attention of environmental scientists. Biological methods are looking quite promising and these procedures are helpful in the complete degradation of bisphenol A and related compounds. Several bacterial, fungal, and algal strains and mixed cultures have successfully been employed for the degradation of bisphenol A. Recently, enzymatic methods have attracted the attention of the environmentalists for the treatment of bisphenol A and other endocrine disrupting compounds. Numerous types of oxidoreductases; laccases, tyrosinases, manganese peroxidase, lignin peroxidase, polyphenol oxidases, horseradish peroxidase and bitter gourd peroxidase have exhibited their potential for the remediation of such types of compounds. The cytochrome P 450 monooxygenases and hemoglobin have also participated in the degradation of bisphenol A and other related endocrine disrupting compounds. Various redox mediators

  19. Synthesis and biological screening by novel hybrid fluorocarbon hydrocarbon compounds for use as artificial blood substitutes

    Science.gov (United States)

    Moacanin, J.; Scherer, K.; Toronto, A.; Lawson, D.; Terranova, T.; Yavrouian, A.; Astle, L.; Harvey, S.; Kaaelble, D. H.

    1979-01-01

    A series of hybrid fluorochemicals of general structure R(1)R(2)R(3)CR(4) was prepared where the R(i)'s (i=1,2,3) is a saturated fluoroalkyl group of formula C sub N F sub 2n+1, and R(4) is an alkyl group C sub n H sub 2n+1 or a related moiety containing amino, ether, or ester functions but no CF bonds. Compounds of this class containing approximately eight to twenty carbons total have physical properties suitable for use as the oxygen carrying phase of fluorochemical emulsion artificial blood. The chemical synthesis, and physical and biological testing of pure single isomers of the proposed artificial blood candidate compounds are included. Significant results are given.

  20. A novel membrane distillation-thermophilic bioreactor system: biological stability and trace organic compound removal.

    Science.gov (United States)

    Wijekoon, Kaushalya C; Hai, Faisal I; Kang, Jinguo; Price, William E; Guo, Wenshan; Ngo, Hao H; Cath, Tzahi Y; Nghiem, Long D

    2014-05-01

    The removal of trace organic compounds (TrOCs) by a novel membrane distillation-thermophilic bioreactor (MDBR) system was examined. Salinity build-up and the thermophilic conditions to some extent adversely impacted the performance of the bioreactor, particularly the removal of total nitrogen and recalcitrant TrOCs. While most TrOCs were well removed by the thermophilic bioreactor, compounds containing electron withdrawing functional groups in their molecular structure were recalcitrant to biological treatment and their removal efficiency by the thermophilic bioreactor was low (0-53%). However, the overall performance of the novel MDBR system with respect to the removal of total organic carbon, total nitrogen, and TrOCs was high and was not significantly affected by the conditions of the bioreactor. All TrOCs investigated here were highly removed (>95%) by the MDBR system. Biodegradation, sludge adsorption, and rejection by MD contribute to the removal of TrOCs by MDBR treatment.

  1. Analytical Methodologies for the Determination of Endocrine Disrupting Compounds in Biological and Environmental Samples

    Science.gov (United States)

    Sosa-Ferrera, Zoraida; Mahugo-Santana, Cristina; Santana-Rodríguez, José Juan

    2013-01-01

    Endocrine-disruptor compounds (EDCs) can mimic natural hormones and produce adverse effects in the endocrine functions by interacting with estrogen receptors. EDCs include both natural and synthetic chemicals, such as hormones, personal care products, surfactants, and flame retardants, among others. EDCs are characterised by their ubiquitous presence at trace-level concentrations and their wide diversity. Since the discovery of the adverse effects of these pollutants on wildlife and human health, analytical methods have been developed for their qualitative and quantitative determination. In particular, mass-based analytical methods show excellent sensitivity and precision for their quantification. This paper reviews recently published analytical methodologies for the sample preparation and for the determination of these compounds in different environmental and biological matrices by liquid chromatography coupled with mass spectrometry. The various sample preparation techniques are compared and discussed. In addition, recent developments and advances in this field are presented. PMID:23738329

  2. Analytical methodologies for the determination of endocrine disrupting compounds in biological and environmental samples.

    Science.gov (United States)

    Sosa-Ferrera, Zoraida; Mahugo-Santana, Cristina; Santana-Rodríguez, José Juan

    2013-01-01

    Endocrine-disruptor compounds (EDCs) can mimic natural hormones and produce adverse effects in the endocrine functions by interacting with estrogen receptors. EDCs include both natural and synthetic chemicals, such as hormones, personal care products, surfactants, and flame retardants, among others. EDCs are characterised by their ubiquitous presence at trace-level concentrations and their wide diversity. Since the discovery of the adverse effects of these pollutants on wildlife and human health, analytical methods have been developed for their qualitative and quantitative determination. In particular, mass-based analytical methods show excellent sensitivity and precision for their quantification. This paper reviews recently published analytical methodologies for the sample preparation and for the determination of these compounds in different environmental and biological matrices by liquid chromatography coupled with mass spectrometry. The various sample preparation techniques are compared and discussed. In addition, recent developments and advances in this field are presented.

  3. Diversity of Secondary Metabolites from Marine Bacillus Species: Chemistry and Biological Activity

    Directory of Open Access Journals (Sweden)

    Hee Jae Shin

    2013-08-01

    Full Text Available Marine Bacillus species produce versatile secondary metabolites including lipopeptides, polypeptides, macrolactones, fatty acids, polyketides, and isocoumarins. These structurally diverse compounds exhibit a wide range of biological activities, such as antimicrobial, anticancer, and antialgal activities. Some marine Bacillus strains can detoxify heavy metals through reduction processes and have the ability to produce carotenoids. The present article reviews the chemistry and biological activities of secondary metabolites from marine isolates. Side by side, the potential for application of these novel natural products from marine Bacillus strains as drugs, pesticides, carotenoids, and tools for the bioremediation of heavy metal toxicity are also discussed.

  4. Low intensity ultrasound stimulates biological activity of aerobic activated sludge

    Institute of Scientific and Technical Information of China (English)

    LIU Hong; YAN Yixin; WANG Wenyan; YU Yongyong

    2007-01-01

    This work aims to explore a procedure to improve biological wastewater treatment efficiency using low intensity ultrasound.The aerobic activated sludge from a municipal wastewater treatment plant was used as the experimental material.Oxygen uptake rate(OUR)of the activated sludge (AS)was determined to indicate the changes of AS activity stimulated by ultrasound at 35 kHZ for 0-40 min with ultrasonic intensities of 0-1.2 W/cm2.The highest OUR was observed at the ultrasonic intensity of 0.3 W/cm2 and an irradiation period of 10 min;more than 15% increase was achieved immediately after sonication.More significantly,the AS activity stimulated by ultrasound could last 24 h after sonication,and the AS activity achieved its peak value within 8 h after sonication.or nearly 100% higher than the initial level after sonication.Therefore,to improve the wastewater treatment efficiency of bioreactors,ultrasound with an intensity of 0.3 W/cm2 could be employed to irradiate a part of the AS in the bioreactor for 10 min every 8 h.

  5. Biological Activities of 2, 5-Disubstituted – 1, 3, 4-Oxadiazoles

    Directory of Open Access Journals (Sweden)

    ARVIND K. SINGH

    2011-06-01

    Full Text Available The heterocyclic compound has been known for several years and investigations in field have been indentified due to the large no. of uses & application in most diverse area. Heterocyclic compounds has been an interesting area for the study of synthesis and biological activity of novel oxadiazole derivatives for a long time.Oxadiazole are the major compound of heterocyclic nucleus for the development of new drugs and the drugs of oxadiazole were the first effective chemotherapeutic agent to be employed systemically for the prevention & cure of bacterial infection. Oxadiazole have accelerated interest in various field like medicinal chemistry, polymer industry, etc. Literature survey reveals that the compound are well known to have a no. of broad spectrum biological activities like as antibacterial, anti-inflammatory, anticonvulsant, anticancer, antitubercular,anti-diabetic, antihelmintic, analgesic etc.Therefore, the synthesis of new 2,5-di-substituted 1,3,4-oxadiazole derivatives that possess a promising biological activity for the future development to get a safer & effective compounds

  6. Taste-active compounds in a traditional Italian food: 'lampascioni'.

    Science.gov (United States)

    Borgonovo, Gigliola; Caimi, Sara; Morini, Gabriella; Scaglioni, Leonardo; Bassoli, Angela

    2008-06-01

    Nature is a rich source of taste-active compounds, in particular of plant origin, many of which have unusual tastes. Many of these are found in traditional food, where spontaneous plants are used as ingredients. Some taste-active compounds were identified in the bulbs of Muscari comosum, a spontaneous plant belonging to the family of the Liliaceae, very common in the Mediterranean area, and used in traditional gastronomy (called 'lampascioni' in South Italy). The bulbs were extracted with a series of solvents of different polarity. The different fractions were submitted to a preliminary sensory evaluation, and the most interesting ones, characterized by a strong bitter taste and some chemestetic properties, were submitted to further purification and structural analysis. From the ethereal extract, several 3-benzyl-4-chromanones and one stilbene derivative were isolated. Pure compounds were examined for their taste activity by means of sensory evaluation, and proved to be responsible for the characteristic taste of this food. Some of these compounds have been synthesized de novo to confirm their structure.

  7. Representation of multi-target activity landscapes through target pair-based compound encoding in self-organizing maps.

    Science.gov (United States)

    Iyer, Preeti; Bajorath, Jürgen

    2011-11-01

    Activity landscape representations provide access to structure-activity relationships information in compound data sets. In general, activity landscape models integrate molecular similarity relationships with biological activity data. Typically, activity against a single target is monitored. However, for steadily increasing numbers of compounds, activity against multiple targets is reported, resulting in an opportunity, and often a need, to explore multi-target structure-activity relationships. It would be attractive to utilize activity landscape representations to aid in this process, but the design of activity landscapes for multiple targets is a complicated task. Only recently has a first multi-target landscape model been introduced, consisting of an annotated compound network focused on the systematic detection of activity cliffs. Herein, we report a conceptually different multi-target activity landscape design that is based on a 2D projection of chemical reference space using self-organizing maps and encodes compounds as arrays of pair-wise target activity relationships. In this context, we introduce the concept of discontinuity in multi-target activity space. The well-ordered activity landscape model highlights centers of discontinuity in activity space and is straightforward to interpret. It has been applied to analyze compound data sets with three, four, and five target annotations and identify multi-target structure-activity relationships determinants in analog series.

  8. Plant compounds insecticide activity against Coleoptera pests of stored products

    Energy Technology Data Exchange (ETDEWEB)

    Moreira, Marcio Dionizio; Picanco, Marcelo Coutinho; Guedes, Raul Narciso Carvalho; Campos, Mateus Ribeiro de; Silva, Gerson Adriano; Martins, Julio Claudio [Universidade Federal de Vicosa (UFV), MG (Brazil). Dept. de Biologia Animal]. E-mail: marcio.dionizio@gmail.com; picanco@ufv.br; guedes@ufv.br; mateusc3@yahoo.com.br; agronomiasilva@yahoo.com.br

    2007-07-15

    The objective of this work was to screen plants with insecticide activity, in order to isolate, identify and assess the bioactivity of insecticide compounds present in these plants, against Coleoptera pests of stored products: Oryzaephilus surinamensis L. (Silvanidae), Rhyzopertha dominica F. (Bostrichidae) and Sitophilus zeamais Mots. (Curculionidae). The plant species used were: basil (Ocimum selloi Benth.), rue (Ruta graveolens L.), lion's ear (Leonotis nepetifolia (L.) R.Br.), jimson weed (Datura stramonium L.), baleeira herb (Cordia verbenacea L.), mint (Mentha piperita L.), wild balsam apple (Mormodica charantia L.), and billy goat weed or mentrasto (Ageratum conyzoides L.). The insecticide activity of hexane and ethanol extracts from those plants on R. dominica was evaluated. Among them, only hexane extract of A. conyzoides showed insecticide activity; the hexane extract of this species was successively fractionated by silica gel column chromatography, for isolation and purification of the active compounds. Compounds 5,6,7,8,3',4',5'-heptamethoxyflavone; 5,6,7,8,3'-pentamethoxy-4',5'-methilenedioxyflavone and coumarin were identified. However, only coumarin showed insecticide activity against three insect pests (LD{sub 50} from 2.72 to 39.71 mg g{sup -1} a.i.). The increasing order of insects susceptibility to coumarin was R. dominica, S. zeamais and O. surinamensis. (author)

  9. Antimicrobial active herbal compounds against Acinetobacter baumannii and other pathogens.

    Science.gov (United States)

    Tiwari, Vishvanath; Roy, Ranita; Tiwari, Monalisa

    2015-01-01

    Bacterial pathogens cause a number of lethal diseases. Opportunistic bacterial pathogens grouped into ESKAPE pathogens that are linked to the high degree of morbidity, mortality and increased costs as described by Infectious Disease Society of America. Acinetobacter baumannii is one of the ESKAPE pathogens which cause respiratory infection, pneumonia and urinary tract infections. The prevalence of this pathogen increases gradually in the clinical setup where it can grow on artificial surfaces, utilize ethanol as a carbon source and resists desiccation. Carbapenems, a β-lactam, are the most commonly prescribed drugs against A. baumannii. The high level of acquired and intrinsic carbapenem resistance mechanisms acquired by these bacteria makes their eradication difficult. The pharmaceutical industry has no solution to this problem. Hence, it is an urgent requirement to find a suitable alternative to carbapenem, a commonly prescribed drug for Acinetobacter infection. In order to do this, here we have made an effort to review the active compounds of plants that have potent antibacterial activity against many bacteria including carbapenem resistant strain of A. baumannii. We have also briefly highlighted the separation and identification methods used for these active compounds. This review will help researchers involved in the screening of herbal active compounds that might act as a replacement for carbapenem.

  10. Antimicrobial active herbal compounds against Acinetobacter baumannii and other pathogens

    Directory of Open Access Journals (Sweden)

    Vishvanath eTiwari

    2015-06-01

    Full Text Available Bacterial pathogens cause a number of lethal diseases. Opportunistic bacterial pathogens grouped into ESKAPE pathogens that are linked to the high degree of morbidity, mortality and increased costs as described by Infectious Disease Society of America. Acinetobacter baumannii is one of the ESKAPE pathogens which cause respiratory infection, pneumonia and urinary tract infections. The prevalence of this pathogen increases gradually in the clinical setup where it can grow on artificial surfaces, utilize ethanol as a carbon source and resists desiccation. Carbapenems, a β-lactam, are the most commonly prescribed drugs against A. baumannii. The high level of acquired and intrinsic carbapenem resistance mechanisms acquired by these bacteria makes their eradication difficult. The pharmaceutical industry has no solution to this problem. Hence, it is an urgent requirement to find a suitable alternative to carbapenem, a commonly prescribed drug for Acinetobacter infection. In order to do this, here we have made an effort to review the active compounds of plants that have potent antibacterial activity against many bacteria including carbapenem resistant strain of A. baumannii. We have also briefly highlighted the separation and identification methods used for these active compounds. This review will help researchers involved in the screening of herbal active compounds that might act as a replacement for carbapenem.

  11. Hydraphiles: A Rigorously Studied Class of Synthetic Channel Compounds with In Vivo Activity

    Directory of Open Access Journals (Sweden)

    Saeedeh Negin

    2013-01-01

    Full Text Available Hydraphiles are a class of synthetic ion channels that now have a twenty-year history of analysis and success. In early studies, these compounds were rigorously validated in a wide range of in vitro assays including liposomal ion flow detected by NMR or ion-selective electrodes, as well as biophysical experiments in planar bilayers. During the past decade, biological activity was observed for these compounds including toxicity to bacteria, yeast, and mammalian cells due to stress caused by the disruption of ion homeostasis. The channel mechanism was verified in cells using membrane polarity sensitive dyes, as well as patch clamping studies. This body of work has provided a solid foundation with which hydraphiles have recently demonstrated acute biological toxicity in the muscle tissue of living mice, as measured by whole animal fluorescence imaging and histological studies. Here we review the critical structure-activity relationships in the hydraphile family of compounds and the in vitro and in cellulo experiments that have validated their channel behavior. This report culminates with a description of recently reported efforts in which these molecules have demonstrated activity in living mice.

  12. Resources and biological activities of natural polyphenols.

    Science.gov (United States)

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

    2014-12-22

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

  13. Automated Structure-Activity Relationship Mining: Connecting Chemical Structure to Biological Profiles.

    Science.gov (United States)

    Wawer, Mathias J; Jaramillo, David E; Dančík, Vlado; Fass, Daniel M; Haggarty, Stephen J; Shamji, Alykhan F; Wagner, Bridget K; Schreiber, Stuart L; Clemons, Paul A

    2014-06-01

    Understanding the structure-activity relationships (SARs) of small molecules is important for developing probes and novel therapeutic agents in chemical biology and drug discovery. Increasingly, multiplexed small-molecule profiling assays allow simultaneous measurement of many biological response parameters for the same compound (e.g., expression levels for many genes or binding constants against many proteins). Although such methods promise to capture SARs with high granularity, few computational methods are available to support SAR analyses of high-dimensional compound activity profiles. Many of these methods are not generally applicable or reduce the activity space to scalar summary statistics before establishing SARs. In this article, we present a versatile computational method that automatically extracts interpretable SAR rules from high-dimensional profiling data. The rules connect chemical structural features of compounds to patterns in their biological activity profiles. We applied our method to data from novel cell-based gene-expression and imaging assays collected on more than 30,000 small molecules. Based on the rules identified for this data set, we prioritized groups of compounds for further study, including a novel set of putative histone deacetylase inhibitors.

  14. Multifunctional and biologically active matrices from multicomponent polymeric solutions

    Science.gov (United States)

    Kiick, Kristi L. (Inventor); Yamaguchi, Nori (Inventor); Rabolt, John (Inventor); Casper, Cheryl (Inventor)

    2012-01-01

    A functionalized electrospun matrix for the controlled-release of biologically active agents, such as growth factors, is presented. The functionalized matrix comprises a matrix polymer, a compatibilizing polymer and a biomolecule or other small functioning molecule. In certain aspects the electrospun polymer fibers comprise at least one biologically active molecule functionalized with low molecular weight heparin.

  15. Determination of phenolic compounds derived from hydrolysable tannins in biological matrices by RP-HPLC.

    Science.gov (United States)

    Díez, María Teresa; García del Moral, Pilar; Resines, José Antonio; Arín, María Jesús

    2008-08-01

    An RP-HPLC method for the determination of four phenolic compounds: gallic acid (GA), pyrogallol (PY), resorcinol (RE) and ellagic acid (EA), derived from hydrolysable tannins is reported. Separation was achieved on a SunFire C18 (250 x 4.6 mm id, 5 microm) column at 40 degrees C with gradient elution. UV detection at 280 nm was applied. The developed method was validated in terms of linearity, accuracy and precision. Satisfactory repeatability and between day precision were noticed with RSD values lower than 3%. Recoveries from different biological samples ranged from 91.50 to 105.25%. The LODs were estimated as 1.70 mg/L for PY, 1.68 mg/L for GA, 1.52 mg/L for RE and 0.98 mg/L for EA with a 20 microL injection volume. The method was applied for the determination of these compounds in oak leaves and in ruminal fluid and urine samples taken from beef cattle fed with oak leaves. The proposed method could be used in ruminant nutrition studies to verify the effect that a diet rich in tannins have on ruminal fermentation and to determine the toxicity of these compounds.

  16. Anticancer activity of botanical compounds in ancient fermented beverages (review).

    Science.gov (United States)

    McGovern, P E; Christofidou-Solomidou, M; Wang, W; Dukes, F; Davidson, T; El-Deiry, W S

    2010-07-01

    Humans around the globe probably discovered natural remedies against disease and cancer by trial and error over the millennia. Biomolecular archaeological analyses of ancient organics, especially plants dissolved or decocted as fermented beverages, have begun to reveal the preliterate histories of traditional pharmacopeias, which often date back thousands of years earlier than ancient textual, ethnohistorical, and ethnological evidence. In this new approach to drug discovery, two case studies from ancient Egypt and China illustrate how ancient medicines can be reconstructed from chemical and archaeological data and their active compounds delimited for testing their anticancer and other medicinal effects. Specifically, isoscopoletin from Artemisia argyi, artemisinin from Artemisia annua, and the latter's more easily assimilated semi-synthetic derivative, artesunate, showed the greatest activity in vitro against lung and colon cancers. In vivo tests of these compounds previously unscreened against lung and pancreatic cancers are planned for the future.

  17. Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity.

    Science.gov (United States)

    Yanagita, Ryo C; Kamachi, Hiroaki; Tanaka, Keisuke; Murakami, Akira; Nakagawa, Yu; Tokuda, Harukuni; Nagai, Hiroshi; Irie, Kazuhiro

    2010-10-15

    The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1. Compound 3 as well as 1 showed significant affinity for protein kinase Cδ (PKCδ), and the antiproliferative activity of 3 was slightly higher than that of 1. However, the anti-tumor-promoting activity of 3 was less than that of 1 in vitro, suggesting that the phenolic hydroxyl group of 1 is necessary for the anti-tumor-promoting activity but not for the binding of PKCδ and antiproliferative activity. Moreover, PKC isozyme selectivity of 3 was similar to that of 1, suggesting non-PKC receptors for these compounds to play some roles in the anti-tumor-promoting activity of 1.

  18. Crystal Structures and Antimicrobial Activity of Two Phosphorus Compounds

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    One phosphorus heterocycle compound 1, C13H13N2OPS, was synthesized by the reaction of Lawesson's reagent (LR) with o-phenylene diamine. The crystal belongs to the orthorhombic system, space group P212121 with a = 5.5274(11), b = 8.1603(16), c = 28.830(6) (A), V =1300.4(4) (A)3, Z = 4, Mr= 276.28, Dc = 1.411 g/cm3, F(000) = 576,μ = 0.360 mm-1, R = 0.0259 and wR = 0.0652 for 1414 observed reflections with I > 2σ(I). While compound 2, C14H17N2O2PS, was obtained as a ring-cleavage product of compound 1. This crystal is of monoclinic system, space group P21/c with a = 9.5619(19), b = 21.879(4), c = 7.3618(15) (A), β= 103.03(3)°, V=1500.4(5) (A)3,Z = 4, Mr= 308.33, Dc = 1.365 g/cm3, F(000) = 648, μ = 0.325 mm-1, R = 0.0383 and wR =0.0742for 2283 observed reflections with I > 2σ(I). Phosphorus atom in each compound bonds with sulfur and carbon atoms using sp3 hybrid orbitals, and crystals of these two compounds are formed and stabilized by intermolecular hydrogen bonds and Van der Waals' forces. The special structure of compound 1 leads to its good antimicrobial activity against staphylococcus aureus.

  19. Monobromination of Activated Aromatic Compounds withPolyvinylbenzyltriphenylphosphonium Supported Tribromide

    Institute of Scientific and Technical Information of China (English)

    WU Ming-Hu; YANG Gui-Chun; CHEN Zu-Xing

    2001-01-01

    Chloromethylated crosslinked co-polyvinylbenzene-divinylber-zene (2% DVB) was treated with triphenylphospbhie and then with sodium bromate and hydrobromic acid to afford red col-ored insoluble polyvinylbenzyltriphenylphosphon supportedtribromide.This reagent could be used as a mild and efficient monobrominating reagent for activated aromatic compounds such as phenols,aromatic,aromatic amines and acety-lanilines with good yields and high para-selectivity.

  20. Insilico studies of organosulfur-functional active compounds in garlic.

    Science.gov (United States)

    Singh, Yogendra P; Singh, Ram A

    2010-01-01

    Garlic has been used medicinally since antiquity because of its antimicrobial activity, anticancer activity, antioxidant activity, ability to reduce cardiovascular diseases, improving immune functions, and antidiabetic activities and also in reducing cardiovascular diseases and improving immune functions. Recent studies identify that the wide variety of medicinal functions are attributed to the sulfur compounds present in garlic. Epidemiological observations and laboratory studies in animal models have also showed anticarcinogenic potential of organosulfur compounds of garlic. In this study, in silico analysis of organosulfur compounds is reported using the methods of theoretical chemistry to elucidate the molecular properties of garlic as it is more time and cost efficient, reduces the number of wet experiments, and offers the possibility of replacing some animal tests with suitable in silico models. The analysis of molecular descriptors defined by Lipinski has been done. The solubility of drug in water has been determined as it is of useful importance in the process of drug discovery from molecular design to pharmaceutical formulation and biopharmacy. All toxicities associated with candidate drug have been calculated. P-Glycoprotein expressed in normal tissues as a cause of drug pharmacokinetics and pharmacodynamics has been examined. Drug-plasma protein binding and volume of distribution have also been calculated. To avoid rejection of drugs, it is becoming more important to determine pK(a), absorption, polar surface area, and other physiochemical properties associated with a drug, before synthetic work is undertaken. The present in silico study is aimed at examining these compounds of garlic to evaluate its possible efficacy and toxicity under conditions of actual use in humans.

  1. Synthesis and biological activity of benzamide DNA minor groove binders.

    Science.gov (United States)

    Khan, Gul Shahzada; Pilkington, Lisa I; Barker, David

    2016-02-01

    A range of di- and triaryl benzamides were synthesised to investigate the effect of the presence and nature of a polar sidechain, bonding and substitution patterns and functionalisation of benzylic substituents. These compounds were tested for their antiproliferative activity as well as their DNA binding activity. The most active compounds in all assays were unsymmetrical triaryl benzamides with a bulky or alkylating benzylic substituent and a polar amino sidechain.

  2. A novel aphrodisiac compound from an orchid that activates nitric oxide synthases.

    Science.gov (United States)

    Subramoniam, A; Gangaprasad, A; Sureshkumar, P K; Radhika, J; Arun, K B; Arun, B K

    2013-01-01

    Nitric oxide (NO) is known to have roles in several crucial biological functions including vasodilation and penile erection. There are neuronal, endothelial and inducible NO synthases that influence the levels of NO in tissues and blood. NO activates guanylate cyclase and thereby increases the levels of cyclic GMP (cGMP). Viagra (sildenafil), a top selling drug in the world for erectile dysfunction, inhibits phosphodiesterase-5, which hydrolyses cGMP to GMP. Thus, it fosters an NO-mediated increase in the levels of cGMP, which mediates erectile function. Here, we show the aphrodisiac activity of a novel chemical isolate from the flowers of an epiphytic orchid, Vanda tessellata (Roxb.) ex Don, which activates neuronal and endothelial, but not inducible, NO synthases. The aphrodisiac activity is caused by an increase in the level of NO in corpus cavernosum. The drug increases blood levels of NO as early as 30 min after oral administration. The active compound was isolated by column chromatography. Based on the spectral data, the active compound is found to be a new compound, 2,7,7-tri methyl bicyclo [2.2.1] heptane. We anticipate that our findings could lead to the development of a commercially viable and valuable drug for erectile dysfunction.

  3. Anticancer activity of new compounds using benzimidazole as a scaffold.

    Science.gov (United States)

    Rashid, Mohd; Husain, Asif; Shaharyar, Mohammad; Sarafroz, Mohd

    2014-01-01

    The design and synthesis of substituted 1-(1-ethy-1H-benzimidazol-2-yl) ethanone (3a-f) and substituted 1-(2-bromoethyl)-2- (1-hydrazinylidene or ethylidene)-1H-benzimidazole (3g-j) have been successfully achieved under microwave irradiation with an aim for finding promising anticancer agents. Among the synthetic compounds, those with potential activity were selected and evaluated in-vitro for anticancer activity at the National Cancer Institute (NCI), USA, against 60 cancer cell lines from nine types of human cancer. The title compound 3e (NSC: 765733/1) exhibited notable growth inhibition that satisfies threshold criteria at single dose (10 µM) on all human cell lines of NCI. This compound was considered for further study at five dose levels (0.01, 0.1, 1, 10 and 100 µM) with GI50 values ranging from 0.19 to 92.7 µM. Compound 3e was found superior for Non-small cell lung cancer cell lines (HOP-92) and calculated end points (GI50 0.19, TGI 1.45, LC50 >100 and Log10GI50 -6.70, Log10TGI -5.84, Log10LC50 >-4.00). Docking study was performed using Maestro 9.0 to provide binding mode into binding sites of topoisomerase enzyme (PDB ID: 1SC7). Hopefully in the future, compound 3e could be used as novel template for the development of potential anticancer agents.

  4. Cooked garlic and antioxidant activity: Correlation with organosulfur compound composition.

    Science.gov (United States)

    Locatelli, D A; Nazareno, M A; Fusari, C M; Camargo, A B

    2017-04-01

    The antioxidant properties and the main beneficial organosulphur compounds of home-cooked garlic samples were studied in order to establish relationships between them. Antioxidant activity was tested by free radical scavenging against 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and 2,2'-azino-bis-(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS(+)), Fe(III) reducing ability (FRAP) and linoleic acid co-oxidation initiated by soybean lipoxygenase in a micelle system. DPPH, ABTS and FRAP assays showed the highest activity for raw garlic samples, while β-carotene bleaching assay yielded the highest activity for stir-fried garlic. Pure organosulphur compounds tested by DPPH, FRAP and β-carotene bleaching assays showed that allicin had an antiradical action mechanism, as well as iron reducing capacity; while antioxidant activity was the main mechanism for ajoenes and 2-VD. To our knowledge, this study is the first demonstration that home-cooked garlic retains its antioxidant activity, and, at the same time, elucidates the mechanisms involved in this activity.

  5. Milk inhibits the biological activity of ricin

    Science.gov (United States)

    Ricin is a highly toxic protein produced by the castor plant Ricinus communis. The toxin is relatively easy to isolate and can be used as a biological weapon. There is great interest in identifying effective inhibitors for ricin. In this study, we demonstrated by three independent assays that compon...

  6. Evaluation of toxicity to the biological treatment and removal of recalcitrant organic compounds from oil refineries wastewaters; Avaliacao da toxicidade ao tratamento biologico e remocao de compostos organicos recalcitrantes existentes em efluentes de refinarias de petroleo

    Energy Technology Data Exchange (ETDEWEB)

    Barros Junior, Laerte M.; Macedo, Gorete R.; Bezerra, Marcio S.; Pereira, Franklin M.S. [Universidade Federal do Rio Grande do Norte (UFRN), Natal, RN (Brazil). Dept. de Engenharia Quimica; Schmidell, Willibaldo [Universidade Federal de Santa Catarina (UFSC), Florianopolis, SC (Brazil)

    2004-07-01

    Oil industry waste water usually contains recalcitrant chemical compounds, like phenol, benzene, toluene, xylene, naphthalene and acenaphthene. The respirometry, determination of respiration rate of an active biomass, is an adequate methodology for quantification of aerobic activity biological. This study aims evaluate the inhibition effect of phenol in the oxidation capacity of an industrial sludge. This work also intends to study the phenol removal through biological and photochemical-biological processes. The respirometry was carried out with synthetic solution, using sludge from an oil processing industry. The phenol degradation experiments were carried out in an activated sludge unit and in a photochemical reactor. This work suggests the potential of photochemical-biological treatment use, in relation to the biological process with a no-acclimated sludge, in the removal of refractory organic compounds from oil industry wastewaters. The characterization of biomass using the respirometry methodology showed which is a useful tool in evaluation of phenol toxicity to biological treatment. (author)

  7. Synthesis and Biological Activities of Substituted Triazolethione Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN, Xiao-Hong; TAO, Yan; LIU, Yuan-Fa; CHEN, Bang

    2007-01-01

    Six novel Schiff bases have been synthesized by the condensation reaction of 4-amino-5-(4-pyridyl)-2,4-dihydro-1,2,4-triazole-3-thione with various benzaldehydes. The structures of the compounds have been confirmed by 1H NMR, IR and elemental analysis. The preliminary bioassay indicated that the title compounds possessed good fungicidal activities to several vegetable pathogens.

  8. Active machine learning-driven experimentation to determine compound effects on protein patterns.

    Science.gov (United States)

    Naik, Armaghan W; Kangas, Joshua D; Sullivan, Devin P; Murphy, Robert F

    2016-02-03

    High throughput screening determines the effects of many conditions on a given biological target. Currently, to estimate the effects of those conditions on other targets requires either strong modeling assumptions (e.g. similarities among targets) or separate screens. Ideally, data-driven experimentation could be used to learn accurate models for many conditions and targets without doing all possible experiments. We have previously described an active machine learning algorithm that can iteratively choose small sets of experiments to learn models of multiple effects. We now show that, with no prior knowledge and with liquid handling robotics and automated microscopy under its control, this learner accurately learned the effects of 48 chemical compounds on the subcellular localization of 48 proteins while performing only 29% of all possible experiments. The results represent the first practical demonstration of the utility of active learning-driven biological experimentation in which the set of possible phenotypes is unknown in advance.

  9. Relationship structure-antioxidant activity of hindered phenolic compounds

    Directory of Open Access Journals (Sweden)

    Weng, X. C.

    2014-12-01

    Full Text Available The relationship between the structure and the antioxidant activity of 21 hindered phenolic compounds was investigated by Rancimat and DPPH· tests. 3-tert-butyl-5-methylbenzene-1,2-diol is the strongest antioxidant in the Rancimat test but not in the DPPH· test because its two hydroxyl groups have very strong steric synergy. 2,6-Ditert-butyl-4-hydroxy-methylphenol exhibits a strong antioxidant activity as 2,6-ditertbutyl- 4-methoxyphenol does in lard. 2,6-Ditert-butyl-4- hydroxy-methylphenol also exhibits stronger activity than 2-tert-butyl-4- methoxyphenol. The methylene of 2,6-ditert-butyl-4-hydroxy-methylphenol can provide a hydrogen atom to active free radicals like a phenolic hydroxyl group does because it is greatly activated by both the aromatic ring and hydroxyl group. Five factors affect the antioxidant activities of the phenolic compounds: how stable the phenolic compound free radicals are after providing hydrogen atoms; how many hy drogen atoms each of the phenolic compounds can provide; how fast the phenolic compounds provide hydrogen atoms; how easily the phenolic compound free radicals can combine with more active free radicals, and whether or not a new antioxidant can form after the phenolic compound provides hydrogen atoms.La relación entre estructura y la actividad antioxidante de 21 compuestos fenólicos con impedimentos estéricos fue investigado mediante ensayos con Rancimat y DPPH·. El 3-terc-butil-5-metilbenceno-1,2-diol es el antioxidante más potente en los ensayos mediante Rancimat pero no mediante ensayos con DPPH·, porque sus dos grupos hidroxilo tienen una fuerte sinergia estérica. El 2,6-Di-terc-butil-4-hidroxi-metil-fenol mostró una actividad antioxidante tan fuerte como el 2,6-di-ter-butil-4-metoxifenol en ensayos con manteca de cerdo. El 2,6-di-terc-butil-4-hidroxi-metilfenol también mostró una actividad más fuerte que el 2-terc-butil-4-metoxifenol. El grupo metileno del 2,6-di-ter-butil-4-hidroxi

  10. Electrochemical screening of biomembrane-active compounds in water

    Energy Technology Data Exchange (ETDEWEB)

    Mohamadi, Shahrzad, E-mail: cmsm@leeds.ac.uk; Tate, Daniel J.; Vakurov, Alexander; Nelson, Andrew

    2014-02-01

    Graphical abstract: - Highlights: • Analytical technology application with improvement allowing for on-line high-throughput water toxin screening is presented. • Compound classes of related structure and shape interact with DOPC coated Pt/Hg with a class specific response. • Predecessor membrane system proved as fragile, complex and for environmental application incompatible. - Abstract: Interactions of biomembrane-active compounds with phospholipid monolayers on microfabricated Pt/Hg electrodes in an on-line high throughput flow system are demonstrated by recording capacitance current peak changes as rapid cyclic voltammograms (RCV). Detection limits of the compounds’ effects on the layer have been estimated from the data. Compounds studied include steroids, polycyclic aromatic hydrocarbons, tricyclic antidepressants and tricyclic phenothiazines. The results show that the extent and type of interaction depends on the—(a) presence and number of aromatic rings and substituents, (b) presence and composition of side chains and, (c) molecular shape. Interaction is only indirectly related to compound hydrophobicity. For a selection of tricyclic antidepressants and tricyclic phenothiazines the detection limit in water is related to their therapeutic normal threshold. The sensing assay has been tested in the presence of humic acid as a potential interferent and in a tap water matrix. The system can be applied to the screening of putative hazardous substances and pharmaceuticals allowing for early detection thereof in the water supply. The measurements are made in real time which means that potentially toxic compounds are detected rapidly within <10 min per assay. This technology will contribute greatly to environment safety and health.

  11. SOURCE, PRODUCTION AND BIOLOGICAL ACTIVITIES OF PICEATANNOL: A REVIEW

    Directory of Open Access Journals (Sweden)

    A. Kukreja*, A. Mishra and A. Tiwari

    2013-10-01

    Full Text Available Phenolic compounds are group of molecules which contain different families of secondary metabolites. Phenolic compounds, secondary metabolites, are abundantly found in plants and are mostly categorized into two major groups: non-soluble compounds and soluble compounds. Stilbenes which come under the category of soluble compounds of phenolics are small molecules, ranges in their weight from ~200 to 300 g/mol and are found in diverse plants. These compounds are produced in plants via phenylpropanoid pathway. Under unfavourable conditions such as microbial or viral attack, ultraviolet light exposure and disease in plants, stilbenes are synthesized and act as natural agents to protect plants. Piceatannol, a natural stilbene, is found in different plant species and is beneficial for human health. It possesses various pharmacological properties such as antioxidant, antitumor, anti-inflammatory and anti-carcinogenic activities. This review paper focuses on piceatannol, its sources, chemical synthesis mechanism, production and its useful applications in various diseases.

  12. Antimycobacterial and cytotoxicity activity of synthetic and natural compounds

    Energy Technology Data Exchange (ETDEWEB)

    Souza, Ana O. de [Instituto Butantan, Sao Paulo, SP (Brazil). Lab. de Bioquimica e Biofisica]. E-mail: olivia@butantan.gov.br; Galetti, Fabio C.S.; Silva, Celio L. [Universidade de Sao Paulo (USP), Ribeirao Preto, SP (Brazil). Faculdade de Medicina. Dept. de Bioquimica e Imunologia] (and others)

    2007-07-01

    Antimycobacterial and cytotoxicity activity of synthetic and natural compounds. Secondary metabolites from Curvularia eragrostidis and Drechslera dematioidea, Clusia sp. floral resin, alkaloids from Pilocarpus alatus, salicylideneanilines, piperidine amides, the amine 1-cinnamylpiperazine and chiral pyridinium salts were assayed on Mycobacterium tuberculosis H37Rv. N-(salicylidene)-2-hydroxyaniline was the most effective compound with a minimal inhibitory concentration (MIC) of 8 {mu}mol/L. Dihydrocurvularin was moderately effective with a MIC of 40 {mu}mol/L. Clusia sp. floral resin and a gallocatechin-epigallocatechin mixture showed MIC of 0.02 g/L and 38 {mu}mol/L, respectively. The cytotoxicity was evaluated for N-(salicylidene)-2-hydroxyaniline, curvularin, dihydrocurvularin and Clusia sp. floral resin, and the selectivity indexes were > 125, 0.47, 0.75 and 5, respectively. (author)

  13. SYNTHESIS AND BIOLOGICAL ACTIVITY OF AMIDE DERIVATIVES OF GINKGOLIDE A

    Institute of Scientific and Technical Information of China (English)

    LI-HONG HU; ZHONG-LIANG CHEN; YU-YUAN XIE

    2001-01-01

    Amide derivatives of ginkgolide A were prepared and evaluated for their in vitro ability to inhibit the PAF-induced aggregation of rabbit platelets. They showed less activities than their parent compound ginkgolide A.

  14. Screening for Antiviral Activities of Isolated Compounds from Essential Oils

    Directory of Open Access Journals (Sweden)

    Akram Astani

    2011-01-01

    Full Text Available Essential oil of star anise as well as phenylpropanoids and sesquiterpenes, for example, trans-anethole, eugenol, β-eudesmol, farnesol, β-caryophyllene and β-caryophyllene oxide, which are present in many essential oils, were examined for their antiviral activity against herpes simplex virus type 1 (HSV-1 in vitro. Antiviral activity was analyzed by plaque reduction assays and mode of antiviral action was determined by addition of the drugs to uninfected cells, to the virus prior to infection or to herpesvirus-infected cells. Star anise oil reduced viral infectivity by >99%, phenylpropanoids inhibited HSV infectivity by about 60–80% and sesquiterpenes suppressed herpes virus infection by 40–98%. Both, star anise essential oil and all isolated compounds exhibited anti-HSV-1 activity by direct inactivation of free virus particles in viral suspension assays. All tested drugs interacted in a dose-dependent manner with herpesvirus particles, thereby inactivating viral infectivity. Star anise oil, rich in trans-anethole, revealed a high selectivity index of 160 against HSV, whereas among the isolated compounds only β-caryophyllene displayed a high selectivity index of 140. The presence of β-caryophyllene in many essential oils might contribute strongly to their antiviral ability. These results indicate that phenylpropanoids and sesquiterpenes present in essential oils contribute to their antiviral activity against HSV.

  15. Microwave assisted synthesis and biological activity of novel coumarinyltriazolothiadiazoles

    Directory of Open Access Journals (Sweden)

    Kumar P

    2010-01-01

    Full Text Available A series of new 3-(4-methylcoumarinyl-7-oxymethyl-6-substitutedphenyl-5,6-dihydro-s-triazolo (3,4-b(1,3,4-thiadiazoles 2(a-j have been synthesized by reacting 5-(4-methyl coumarinyl-7-oxymethyl-4-amino-3-mercapto(4H-1,2,4-triazole with various aromatic aldehydes by microwave assisted organic synthesis. The structure of the compounds 2 (a-j has been confirmed by IR, 1 H NMR and mass spectral data. All the compounds were screened for antimicrobial and antioxidant activity. Among the compounds tested, compounds 2d (4-dimethyl amino phenyl derivative and 2h (3,4-dimethoxy phenyl derivative showed better antimicrobial and antioxidant activity than rest of the compounds in the series.

  16. Biological Role of Anions (Sulfate, Nitrate , Oxalate and Acetate) on the Antibacterial Properties of Cobalt (II) and Nickel(II) Complexes With Pyrazinedicarboxaimide Derived, Furanyl and Thienyl Compounds

    OpenAIRE

    Chohan, Zahid H.; Praveen, M.

    1999-01-01

    A number of biologically active complexes of cobalt(II) and nickel(II) with pyrazinedicarboxaimido derived thienyl and furanyl compounds having the same metal ion but different anions such as sulphate, nitrate, oxalate and acetate have been synthesized and characterized on the basis of their physical, spectral and analytical data. In order to evaluate the role of anions on their antibacterial properties, these ligands and their synthesized metal complexes with various anions have been screene...

  17. Matricryptins and matrikines: biologically active fragments of the extracellular matrix.

    Science.gov (United States)

    Ricard-Blum, Sylvie; Salza, Romain

    2014-07-01

    Numerous extracellular proteins and glycosaminoglycans (GAGs) undergo limited enzymatic cleavage resulting in the release of fragments exerting biological activities, which are usually different from those of the full-length molecules. In this review, we define matrikines and matricryptins, which are bioactive fragments released from the extracellular matrix proteins, proteoglycans and GAGs and report their major biological activities. These fragments regulate a number of physiopathological processes including angiogenesis, cancer, fibrosis, inflammation, neurodegenerative diseases and wound healing. The challenges to translate these fragments from molecules biologically active in vitro and in experimental models to potential drugs are discussed in the last part of the review.

  18. Analytical applications of oscillatory chemical reactions: determination of some pharmaceuticaly and biologically important compounds

    Directory of Open Access Journals (Sweden)

    Pejić Nataša D.

    2012-01-01

    Full Text Available Novel analytical methods for quantitive determination of analytes based on perturbations of oscillatory chemical reactions realized under open reactor conditions (continuosly fed well stirred tank reactor, CSTR, have been developed in the past twenty years. The proposed kinetic methods are generally based on the ability of the analyzed substances to change the kinetics of the chemical reactions matrix. The unambiguous correlation of quantitative characteristics of perturbations, and the amount (concentration of analyte expressed as a regression equation, or its graphics (calibration curve, enable the determination of the unknown analyte concentration. Attention is given to the development of these methods because of their simple experimental procedures, broad range of linear regression ( 10-7 10-4 mol L-1 and low limits of detection of analytes ( 10-6 10-8 mol L1, in some cases even lower than 10-12 mol L-1. Therefore, their application is very convenient for routine analysis of various inorganic and organic compounds as well as gases. This review summarizes progress made in the past 5 years on quantitative determination of pharmaceutically and biologically important compounds.

  19. Actinobacteria from arid and desert habitats: diversity and biological activity

    Directory of Open Access Journals (Sweden)

    Joachim eWink

    2016-01-01

    Full Text Available Abstract The lack of new antibiotics in the pharmaceutical pipeline guides more and more researchers to leave the classical isolation procedures and to look in special niches and ecosystems. Bioprospecting of extremophilic Actinobacteria through mining untapped strains and avoiding resiolation of known biomolecules is among the most promising strategies for this purpose. With this approach, members of acidtolerant, alkalitolerant, psychrotolerant, thermotolerant, halotolerant and xerotolerant Actinobacteria have been obtained from respective habitats. Among these, little survey exists on the diversity of Actinobacteria in arid areas, which are often adapted to relatively high temperatures, salt concentrations, and radiation. Therefore, arid and desert habitats are special ecosystems which can be recruited for the isolation of uncommon Actinobacteria with new metabolic capability.At the time of this writing, members of Streptomyces, Micromonospora, Saccharothrix, Streptosporangium, Cellulomonas, Amycolatopsis, Geodermatophilus, Lechevalieria, Nocardia and Actinomadura are reported from arid habitats. However, metagenomic data present dominant members of the communities in desiccating condition of areas with limited water availability that are not yet isolated. Furthermore, significant diverse types of polyketide synthase (PKS and nonribosomal peptide synthetase (NRPS genes are detected in xerophilic and xerotolerant Actinobacteria and some bioactive compounds are reported from them. Rather than pharmaceutically active metabolites, molecules with protection activity against drying such as Ectoin and Hydroxyectoin with potential application in industry and agriculture have also been identified from xerophilic Actinobacteria. In addition, numerous biologically active small molecules are expected to be discovered from arid adapted Actinobacteria in the future. In the current survey, the diversity and biotechnological potential of Actinobacteria

  20. Biological activities of Juglans regia flowers

    Directory of Open Access Journals (Sweden)

    Seyed Fazel Nabavi

    2011-06-01

    Full Text Available Antidepressant, anti-inflammatory, antihypoxic and antioxidant activities of methanol extract of Juglans regia L., Juglandaceae, flower were investigated. Antidepressant activity was examined by forced swimming test and tail suspension test in mice. Antihypoxic activity was investigated in haemic and circulatory models. The effects were pronounced in both models. It produced statistically significant anti-inflammatory activity in carrageenan induced edema at nearly all doses, compared to control groups. IC50 for DPPH radical-scavenging activity was 674±27.6 µg mL-1. Extract showed good Fe2+ chelating ability (IC50 43±1.5 µg mL-1. It exhibited low antioxidant activity in linoleic acid peroxidation test. Its pharmacological effects may be attributed, in part, to the presence of phenols and ISSN 0102-695X flavonoids in the extract.

  1. Anti-inflammatory activity of different agave plants and the compound cantalasaponin-1.

    Science.gov (United States)

    Monterrosas-Brisson, Nayeli; Ocampo, Martha L Arenas; Jiménez-Ferrer, Enrique; Jiménez-Aparicio, Antonio R; Zamilpa, Alejandro; Gonzalez-Cortazar, Manases; Tortoriello, Jaime; Herrera-Ruiz, Maribel

    2013-07-10

    Species of the agave genus, such as Agave tequilana, Agave angustifolia and Agave americana are used in Mexican traditional medicine to treat inflammation-associated conditions. These plants' leaves contain saponin compounds which show anti-inflammatory properties in different models. The goal of this investigation was to evaluate the anti-inflammatory capacity of these plants, identify which is the most active, and isolate the active compound by a bio-directed fractionation using the ear edema induced in mice with 12-O-tetradecanoylphorbol-13-acetate (TPA) technique. A dose of 6 mg/ear of acetone extract from the three agave species induced anti-inflammatory effects, however, the one from A. americana proved to be the most active. Different fractions of this species showed biological activity. Finally the F5 fraction at 2.0 mg/ear induced an inhibition of 85.6%. We identified one compound in this fraction as (25R)-5α-spirostan-3β,6α,23α-triol-3,6-di-O-β-D-glucopyranoside (cantalasaponin-1) through 1H- and 13C-NMR spectral analysis and two dimensional experiments like DEPT NMR, COSY, HSQC and HMBC. This steroidal glycoside showed a dose dependent effect of up to 90% of ear edema inhibition at the highest dose of 1.5 mg/ear.

  2. Anti-Inflammatory Activity of Different Agave Plants and the Compound Cantalasaponin-1

    Directory of Open Access Journals (Sweden)

    Jaime Tortoriello

    2013-07-01

    Full Text Available Species of the agave genus, such as Agave tequilana, Agave angustifolia and Agave americana are used in Mexican traditional medicine to treat inflammation-associated conditions. These plants’ leaves contain saponin compounds which show anti-inflammatory properties in different models. The goal of this investigation was to evaluate the anti-inflammatory capacity of these plants, identify which is the most active, and isolate the active compound by a bio-directed fractionation using the ear edema induced in mice with 12-O-tetradecanoylphorbol-13-acetate (TPA technique. A dose of 6 mg/ear of acetone extract from the three agave species induced anti-inflammatory effects, however, the one from A. americana proved to be the most active. Different fractions of this species showed biological activity. Finally the F5 fraction at 2.0 mg/ear induced an inhibition of 85.6%. We identified one compound in this fraction as (25R-5α-spirostan-3β,6α,23α-triol-3,6-di-O-β-D-glucopyranoside (cantalasaponin-1 through 1H- and 13C-NMR spectral analysis and two dimensional experiments like DEPT NMR, COSY, HSQC and HMBC. This steroidal glycoside showed a dose dependent effect of up to 90% of ear edema inhibition at the highest dose of 1.5 mg/ear.

  3. Synthesis, algal inhibition activities and QSAR studies of novel gramine compounds containing ester functional groups

    Institute of Scientific and Technical Information of China (English)

    LI Xia; YU Liangmin; JIANG Xiaohui; XIA Shuwei; ZHAO Haizhou

    2009-01-01

    2,5,6-Tribromo-l-methylgramine (TBG), isolated from bryozoan Zoobotryon pellucidum was shown to be very efficient in preventing recruitment of larval settlement. In order to improve the compatibility of TBG and its analogues with other ingredients in antifouling paints, structural modification of TBG was focused mainly on halogen substitution and N-substitution. Two halogen-substitute gramines and their derivatives which contain ester functional groups at N-position of gramines were synthesized. Algal inhibition activities of the synthesized compounds against algae Nitzschia closterium were evaluated and the Median Effective Concentration (EC50) range was 1.06-6.74 μg ml-1. Compounds that had a long chain ester group exhibited extremely high antifouling activity. Quantitive Structure Activity Relationship (QSAR) studies with multiple linear regression analysis were applied to find correlation between different calculated molecular descriptors and biological activity of the synthesized compounds. The results show that the toxicity (log (1/EC50)) is correlated well with the partition coefficient log P. Thus, these products have potential function as antifouling agents.

  4. Biologically active dibenzofurans from Pilidiostigma glabrum, an endemic Australian Myrtaceae.

    Science.gov (United States)

    Shou, Qingyao; Banbury, Linda K; Renshaw, Dane E; Lambley, Eleanore H; Mon, Htwe; Macfarlane, Graham A; Griesser, Hans J; Heinrich, Michael M; Wohlmuth, Hans

    2012-09-28

    In an effort to identify new anti-inflammatory and antibacterial agents with potential application in wound healing, five new dibenzofurans, 1,3,7,9-tetrahydroxy-2,8-dimethyl-4,6-di(2-methylbutanoyl)dibenzofuran (1), 1,3,7,9-tetrahydroxy-2,8-dimethyl-4-(2-methylbutanoyl)-6-(2-methylpropionyl)dibenzofuran (2), 1,3,7,9-tetrahydroxy-2,8-dimethyl-4,6-di(2-methylpropionyl)dibenzofuran (3), 1,3,7,9-tetrahydroxy-4,6-dimethyl-2-(2-methylbutanoyl)-8-(2-methylpropionyl)dibenzofuran (4), and 1,3,7,9-tetrahydroxy-4,6-dimethyl-2,8-di(2-methylpropionyl)dibenzofuran (5), were isolated from the leaves of Pilidiostigma glabrum together with one previously described dibenzofuran. Structure elucidation was achieved by way of spectroscopic measurements including 2D-NMR spectroscopy. Compounds with 2,8-acyl substitutions had potent antibacterial activity against several Gram-positive strains (MIC in the low micromolar range), while compounds with 4,6-acyl substitutions were less active. All compounds except 3 inhibited the synthesis of nitric oxide in RAW264 macrophages with IC(50) values in the low micromolar range. Compounds with 2,8-acyl substitutions also inhibited the synthesis of PGE(2) in 3T3 cells, whereas 4,6-acyl-substituted compounds were inactive. None of the compounds inhibited the synthesis of TNF-α in RAW264 cells. The compounds showed variable but modest antioxidant activity in the oxygen radical absorbance capacity assay. These findings highlight that much of the Australian flora remains unexplored and may yet yield many new compounds of interest. Initial clues are provided on structure/activity relationships for this class of bioactives, which may enable the design and synthesis of compounds with higher activity and/or selectivity.

  5. Production of N-13 labeled compounds with high specific activity

    Energy Technology Data Exchange (ETDEWEB)

    Suzuki, Kazutoshi; Sasaki, Motoji; Yoshida, Yuichiro; Haradahira, Terushi; Inoue, Osamu [National Inst. of Radiological Sciences, Chiba (Japan)

    1997-03-01

    Nitrogen-13 was produced by irradiating ultra pure water saturated with a pure gas (N2, O2, He, H2) with 18 MeV protons. Ion species generated by irradiation were analyzed with radio ion chromatography systems. An automated equipment was developed to synthesize anhydrous (13N)NH3 as a synthetic precursor and (13N)p-nitrophenyl carbamate ((13N)NPC) as a model compound, using the (13N)NH3. The radiochemical yield and specific activity of (13N)NPC was high enough to carry out the receptor study with PET. (author)

  6. Acetylated Triterpene Glycosides and Their Biological Activity from Holothuroidea Reported in the Past Six Decades

    Science.gov (United States)

    Bahrami, Yadollah; Franco, Christopher M. M.

    2016-01-01

    Sea cucumbers have been valued for many centuries as a tonic and functional food, dietary delicacies and important ingredients of traditional medicine in many Asian countries. An assortment of bioactive compounds has been described in sea cucumbers. The most important and abundant secondary metabolites from sea cucumbers are triterpene glycosides (saponins). Due to the wide range of their potential biological activities, these natural compounds have gained attention and this has led to their emergence as high value compounds with extended application in nutraceutical, cosmeceutical, medicinal and pharmaceutical products. They are characterized by bearing a wide spectrum of structures, such as sulfated, non-sulfated and acetylated glycosides. Over 700 triterpene glycosides have been reported from the Holothuroidea in which more than 145 are decorated with an acetoxy group having 38 different aglycones. The majority of sea cucumber triterpene glycosides are of the holostane type containing a C18 (20) lactone group and either Δ7(8) or Δ9(11) double bond in their genins. The acetoxy group is mainly connected to the C-16, C-22, C-23 and/or C-25 of their aglycone. Apparently, the presence of an acetoxy group, particularly at C-16 of the aglycone, plays a significant role in the bioactivity; including induction of caspase, apoptosis, cytotoxicity, anticancer, antifungal and antibacterial activities of these compounds. This manuscript highlights the structure of acetylated saponins, their biological activity, and their structure-activity relationships. PMID:27527190

  7. [Effects of biological organic fertilizer on microbial community's metabolic activity in a soil planted with chestnut (Castanea mollissima)].

    Science.gov (United States)

    Chen, Lin; Gu, Jie; Hu, Ting; Gao, Hua; Chen, Zhi-Xue; Qin, Qing-Jun; Wang, Xiao-Juan

    2013-06-01

    A field experiment was conducted in Zhashui County of Shaanxi Province, Northwest China in 2011 to study the effects of biological organic fertilizer on the microbial community's metabolic activity in a soil planted with chestnut (Castanea mollissima). Three treatments were installed, i. e., control, compound fertilizer, and biological organic fertilizer. Soil samples were collected at harvest, and the metabolic activity was tested by Biolog method. In the treatment of biological organic fertilizer, the average well color development, Shannon evenness, richness, and McIntosh indices of microbial community were all significantly higher than the other two treatments. As compared with the control, applying biological organic fertilizer improved the ability of soil microbes in utilizing the carbon sources of carbohydrates and polymers, while applying compound fertilizer was in opposite. The principal component analysis demonstrated that there was an obvious difference in the soil microbial community among different treatments, mainly depending on the species of carbohydrates and amino acids.

  8. Biological activities of Croton palanostigma Klotzsch

    Directory of Open Access Journals (Sweden)

    Eduardo Ferreira Mota

    2015-01-01

    Full Text Available Background: Different species of Croton are used in traditional Amazonian medicine. Among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers. Objective: This study evaluated the antileishmanial, antiplasmodial and antimicrobial activities of the extracts and diterpenes of Croton palanostigma Klotzsch (Euphorbiaceae. Materials and Methods: Leaves and bark were extracted with dichloromethane and methanol. The bark dichloromethane extract (BDE was chromatographed on a column, obtaining cordatin and aparisthman. The extracts and diterpenes were assayed thought agar disk diffusion method and their bactericidal or fungicidal effects were evaluated by minimum bactericidal or fungicidal concentration. The antiplasmodial activity was evaluated after 24 and 72 h of exposition. The antileishmanial activity was performed on promastigotes forms of Leishmania amazonensis. Results: The bark methanol extract (BME and cordatin were not active against any microbial strains tested; BDE and leaves methanol extract (LME were positive for Pseudomonas aeruginosa and aparisthman was positive for Candida albicans. In the determination of the minimum bactericidal concentration, neither of them were active in the highest concentration tested. The extracts and diterpenes were inactive in Plasmodium falciparum, except the LME in 72 h. Any extract was shown to be active in promastigote forms of L. amazonensis. Conclusion: These results indicate that the BDE and LME did not inhibit the bacterial growth, then they probably had bacteriostatic effect. LME presented activity in P. falciparum.

  9. [Ajoene the main active compound of garlic (Allium sativum): a new antifungal agent].

    Science.gov (United States)

    Ledezma, Eliades; Apitz-Castro, Rafael

    2006-06-01

    The curative properties of garlic in medicine have been known for a long time. But, it was only in the last three decades when garlic properties were seriously investigated confirming its potential as therapeutic agent. Allicin, ajoene, thiosulfinates and a wide range of other organosulphurate compounds, are known to be the constituents linked to the garlic properties. Regarding the biochemical properties of these compounds, ajoene [(E,Z)-4,5,9 Trithiadodeca 1,6,11 Triene 9-oxide] is stable in water, and it can be obtained by chemical synthesis. There is evidence that some of the garlic constituents exert a wide variety of effects on different biological systems. However, ajoene is the garlic compound related to more biological activities, as showed in in vitro and in vivo systems. Those studies found that ajoene has antithrombotic, anti-tumoral,antifungal, and antiparasitic effects. This study deals with a recently described antifungal property of ajoene, and its potential use in clinical trails to treat several fungal infections.

  10. Design, synthesis, and biological properties of triazole derived compounds and their transition metal complexes.

    Science.gov (United States)

    Chohan, Zahid H; Hanif, Muhammad

    2010-10-01

    Triazole derived Schiff bases and their metal complexes (cobalt(II), copper(II), nickel(II), and zinc(II)) have been prepared and characterized using IR, (1)H and (13)C NMR, mass spectrometry, magnetic susceptibility and conductivity measurements, and CHN analysis data. The structure of L(2), N-[(5-methylthiophen-2-yl)methylidene]-1H-1,2,4-triazol-3-amine, has also been determined by the X-ray diffraction method. All the metal(II) complexes showed octahedral geometry except the copper(II) complexes, which showed distorted octahedral geometry. The triazole ligands and their metal complexes have been screened for their in vitro antibacterial, antifungal, and cytotoxic activity. All the synthesized compounds showed moderate to significant antibacterial activity against one or more bacterial strains. It is revealed that all the synthesized complexes showed better activity than the ligands, due to coordination.

  11. Astaxanthin: Sources, Extraction, Stability, Biological Activities and Its Commercial Applications—A Review

    Directory of Open Access Journals (Sweden)

    Ranga Rao Ambati

    2014-01-01

    Full Text Available There is currently much interest in biological active compounds derived from natural resources, especially compounds that can efficiently act on molecular targets, which are involved in various diseases. Astaxanthin (3,3′-dihydroxy-β, β′-carotene-4,4′-dione is a xanthophyll carotenoid, contained in Haematococcus pluvialis, Chlorella zofingiensis, Chlorococcum, and Phaffia rhodozyma. It accumulates up to 3.8% on the dry weight basis in H. pluvialis. Our recent published data on astaxanthin extraction, analysis, stability studies, and its biological activities results were added to this review paper. Based on our results and current literature, astaxanthin showed potential biological activity in in vitro and in vivo models. These studies emphasize the influence of astaxanthin and its beneficial effects on the metabolism in animals and humans. Bioavailability of astaxanthin in animals was enhanced after feeding Haematococcus biomass as a source of astaxanthin. Astaxanthin, used as a nutritional supplement, antioxidant and anticancer agent, prevents diabetes, cardiovascular diseases, and neurodegenerative disorders, and also stimulates immunization. Astaxanthin products are used for commercial applications in the dosage forms as tablets, capsules, syrups, oils, soft gels, creams, biomass and granulated powders. Astaxanthin patent applications are available in food, feed and nutraceutical applications. The current review provides up-to-date information on astaxanthin sources, extraction, analysis, stability, biological activities, health benefits and special attention paid to its commercial applications.

  12. Astaxanthin: sources, extraction, stability, biological activities and its commercial applications--a review.

    Science.gov (United States)

    Ambati, Ranga Rao; Phang, Siew Moi; Ravi, Sarada; Aswathanarayana, Ravishankar Gokare

    2014-01-07

    There is currently much interest in biological active compounds derived from natural resources, especially compounds that can efficiently act on molecular targets, which are involved in various diseases. Astaxanthin (3,3'-dihydroxy-β, β'-carotene-4,4'-dione) is a xanthophyll carotenoid, contained in Haematococcus pluvialis, Chlorella zofingiensis, Chlorococcum, and Phaffia rhodozyma. It accumulates up to 3.8% on the dry weight basis in H. pluvialis. Our recent published data on astaxanthin extraction, analysis, stability studies, and its biological activities results were added to this review paper. Based on our results and current literature, astaxanthin showed potential biological activity in in vitro and in vivo models. These studies emphasize the influence of astaxanthin and its beneficial effects on the metabolism in animals and humans. Bioavailability of astaxanthin in animals was enhanced after feeding Haematococcus biomass as a source of astaxanthin. Astaxanthin, used as a nutritional supplement, antioxidant and anticancer agent, prevents diabetes, cardiovascular diseases, and neurodegenerative disorders, and also stimulates immunization. Astaxanthin products are used for commercial applications in the dosage forms as tablets, capsules, syrups, oils, soft gels, creams, biomass and granulated powders. Astaxanthin patent applications are available in food, feed and nutraceutical applications. The current review provides up-to-date information on astaxanthin sources, extraction, analysis, stability, biological activities, health benefits and special attention paid to its commercial applications.

  13. Total synthesis and biological activity of natural product Urukthapelstatin A.

    Science.gov (United States)

    Lin, Chun-Chieh; Tantisantisom, Worawan; McAlpine, Shelli R

    2013-07-19

    Herein we report the first total synthesis of the natural product Urkuthaplestatin A (Ustat A) utilizing a convergent synthetic strategy. The characterization and biological activity match those of the previously published natural product. Interestingly, several intermediates, including the linear and serine cyclized precursors, show a 100-fold decrease in cytotoxicity, with IC50's in the low micromolar range. These data indicate that the rigidity and the consecutive aromatic heterocyclic system are responsible for the biological activity.

  14. Phytochemicals and Their Biological Activities of Plants in Tagetes L.

    Institute of Scientific and Technical Information of China (English)

    XU Li-wei; CHEN Juan; QI Huan-yang; SHI Yan-ping

    2012-01-01

    Tagetes L.,the genus in the family Asteraceae,consists of about 30 species spread in South and Middle America as well as Mexico.More than one hundred secondary metabolites have been obtained in phytochemical investigation on the species,some of which have potent biological activities.The advances in phytochemical studies and biological activities of the plants in Tagetes L.from 1925 to 2011 are summarized in this paper.

  15. Quantitative structure-activity relationship of phenoxyphenyl-methanamine compounds with 5HT2A, SERT, and hERG activities.

    Science.gov (United States)

    Mente, Scot; Gallaschun, Randall; Schmidt, Anne; Lebel, Lorrie; Vanase-Frawley, Michelle; Fliri, Anton

    2008-12-01

    QSAR models have been used to evaluate activities for compounds in the phenoxyphenyl-methanamine (PPMA) class of compounds. These models utilize Hammett-type donating-withdrawing substituent values as well as simple parameters to describe substituent size and elucidate the SAR of the 'A' and 'B' rings. Using this methodology, intuitive QSAR relationships were found for the three biological activities with R(2) values of 0.73, 0.45, and 0.58 for 5HT(2A), SerT, and hERG activities.

  16. Isolation of biologically active constituents from Moringa peregrina (Forssk.) Fiori. (family: Moringaceae) growing in Egypt

    OpenAIRE

    El-Alfy, Taha S.; Shahira M. Ezzat; Hegazy, Ahmed K.; Amer, Aziza M. M.; Kamel, Gehan M.

    2011-01-01

    Background: Moringa peregrina is a wild plant that grown in the eastern desert mountains in Egypt. Although, this plant is native to Egypt, no details studies were traced on its chemical composition and biological activity. Materials and Methods: The different fractions of the ethanolic extract of the dried aerial parts of the plants were subjected to fractionation and purification on various silica and sephadex columns for the isolation of the major compounds which were tested for there anti...

  17. Catalytic activities of zeolite compounds for decomposing aqueous ozone.

    Science.gov (United States)

    Kusuda, Ai; Kitayama, Mikito; Ohta, Yoshio

    2013-12-01

    The advanced oxidation process (AOP), chemical oxidation using aqueous ozone in the presence of appropriate catalysts to generate highly reactive oxygen species, offers an attractive option for removing poorly biodegradable pollutants. Using the commercial zeolite powders with various Si/Al ratios and crystal structures, their catalytic activities for decomposing aqueous ozone were evaluated by continuously flowing ozone to water containing the zeolite powders. The hydrophilic zeolites (low Si/Al ratio) with alkali cations in the crystal structures were found to possess high catalytic activity for decomposing aqueous ozone. The hydrophobic zeolite compounds (high Si/Al ratio) were found to absorb ozone very well, but to have no catalytic activity for decomposing aqueous ozone. Their catalytic activities were also evaluated by using the fixed bed column method. When alkali cations were removed by acid rinsing or substituted by alkali-earth cations, the catalytic activities was significantly deteriorated. These results suggest that the metal cations on the crystal surface of the hydrophilic zeolite would play a key role for catalytic activity for decomposing aqueous ozone.

  18. Synthesis, biological evaluation and SAR of sulfonamide 4-methoxychalcone derivatives with potential antileishmanial activity.

    Science.gov (United States)

    Andrighetti-Fröhner, Carla R; de Oliveira, Kely N; Gaspar-Silva, Daniela; Pacheco, Letícia K; Joussef, Antônio C; Steindel, Mário; Simões, Cláudia M O; de Souza, Alessandra M T; Magalhaes, Uiaran O; Afonso, Ilídio F; Rodrigues, Carlos R; Nunes, Ricardo J; Castro, Helena C

    2009-02-01

    Despite clinical importance of leishmaniasis, an infectious disease that affects 12 thousand million people in 88 countries, the treatment is still unsatisfactory due to its limited efficacy, cost expensive and undesirable side effects. Aiming to develop new antileishmanial lead compounds, we used a rational approach to synthesize a new set of sulfonamide 4-methoxychalcone derivatives (3a-3i) and evaluate the sulfonamide and methoxy moieties as promising adding-groups to chalcones. For that purpose we tested this new set against Leishmania braziliensis promastigotes and intracellular amastigotes and determined its cell toxicity profile. Interestingly all compounds presented a concentration-dependent antileishmanial profile and the benzylamino derivative (3i) showed a biological activity better than pentamidine. None of these compounds affected Trypanosoma cruzi epimastigotes, which suggests a specific antileishmanial profile. The structure-activity analysis of these sulfonamide 4-methoxychalcone derivatives pointed the molecular volume, the HOMO density concentrated in the chalcone moiety and the conformational structure of the compounds as important structural and stereoelectronic features for the antileishmanial activity. In addition, these compounds also fulfilled Lipinski rule of 5 and presented druglikeness similar to antileishmanial drugs. Altogether these results point the sulfonamide 4-methoxychalcone derivatives as potential lead compounds for designing new candidates for leishmaniasis treatment.

  19. The biological activities and chemical composition of Pereskia species (Cactaceae)--a review.

    Science.gov (United States)

    Pinto, Nícolas de Castro Campos; Scio, Elita

    2014-09-01

    The exploration of nature as a source of sustainable, novel bioactive substances continues to grow as natural products play a significant role in the search for new therapeutic and agricultural agents. In this context, plants of the genus Pereskia (Cactaceae) have been studied for their biological activities, and are evolving as an interesting subject in the search for new, bioactive compounds. These species are commonly used as human foodstuffs and in traditional medicine to treat a variety of diseases. This review focuses on the bioactivity and chemical composition of the genus Pereskia, and aims to stimulate further studies on the chemistry and biological potential of the genus.

  20. Intramolecular Hydrogen Bond in Biologically Active o-Carbonyl Hydroquinones

    Directory of Open Access Journals (Sweden)

    Maximiliano Martínez-Cifuentes

    2014-07-01

    Full Text Available Intramolecular hydrogen bonds (IHBs play a central role in the molecular structure, chemical reactivity and interactions of biologically active molecules. Here, we study the IHBs of seven related o-carbonyl hydroquinones and one structurally-related aromatic lactone, some of which have shown anticancer and antioxidant activity. Experimental NMR data were correlated with theoretical calculations at the DFT and ab initio levels. Natural bond orbital (NBO and molecular electrostatic potential (MEP calculations were used to study the electronic characteristics of these IHB. As expected, our results show that NBO calculations are better than MEP to describe the strength of the IHBs. NBO energies (∆Eij(2 show that the main contributions to energy stabilization correspond to LPàσ* interactions for IHBs, O1…O2-H2 and the delocalization LPàπ* for O2-C2 = Cα(β. For the O1…O2-H2 interaction, the values of ∆Eij(2 can be attributed to the difference in the overlap ability between orbitals i and j (Fij, instead of the energy difference between them. The large energy for the LP O2àπ* C2 = Cα(β interaction in the compounds 9-Hydroxy-5-oxo-4,8, 8-trimethyl-l,9(8H-anthracenecarbolactone (VIII and 9,10-dihydroxy-4,4-dimethylanthracen-1(4H-one (VII (55.49 and 60.70 kcal/mol, respectively when compared with the remaining molecules (all less than 50 kcal/mol, suggests that the IHBs in VIII and VII are strongly resonance assisted.

  1. Polyphenols from Bee Pollen: Structure, Absorption, Metabolism and Biological Activity

    Directory of Open Access Journals (Sweden)

    Anna Rzepecka-Stojko

    2015-12-01

    Full Text Available Bee pollen constitutes a natural source of antioxidants such as phenolic acids and flavonoids, which are responsible for its biological activity. Research has indicated the correlation between dietary polyphenols and cardioprotective, hepatoprotective, anti-inflammatory, antibacterial, anticancerogenic, immunostimulating, antianaemic effects, as well as their beneficial influence on osseous tissue. The beneficial effects of bee pollen on health result from the presence of phenolic acids and flavonoids which possess anti-inflammatory properties, phytosterol and linolenic acid which play an anticancerogenic role, and polysaccharides which stimulate immunological activity. Polyphenols are absorbed in the alimentary tract, metabolised by CYP450 enzymes, and excreted with urine and faeces. Flavonoids and phenolic acids are characterised by high antioxidative potential, which is closely related to their chemical structure. The high antioxidant potential of phenolic acids is due to the presence and location of hydroxyl groups, a carboxyl group in the immediate vicinity of ortho-diphenolic substituents, and the ethylene group between the phenyl ring and the carboxyl group. As regards flavonoids, essential structural elements are hydroxyl groups at the C5 and C7 positions in the A ring, and at the C3′ and C4′ positions in the B ring, and a hydroxyl group at the C3 position in the C ring. Furthermore, both, the double bond between C2 and C3, and a ketone group at the C4 position in the C ring enhance the antioxidative potential of these compounds. Polyphenols have an ideal chemical structure for scavenging free radicals and for creating chelates with metal ions, which makes them effective antioxidants in vivo.

  2. Polyphenols from Bee Pollen: Structure, Absorption, Metabolism and Biological Activity.

    Science.gov (United States)

    Rzepecka-Stojko, Anna; Stojko, Jerzy; Kurek-Górecka, Anna; Górecki, Michał; Kabała-Dzik, Agata; Kubina, Robert; Moździerz, Aleksandra; Buszman, Ewa

    2015-12-04

    Bee pollen constitutes a natural source of antioxidants such as phenolic acids and flavonoids, which are responsible for its biological activity. Research has indicated the correlation between dietary polyphenols and cardioprotective, hepatoprotective, anti-inflammatory, antibacterial, anticancerogenic, immunostimulating, antianaemic effects, as well as their beneficial influence on osseous tissue. The beneficial effects of bee pollen on health result from the presence of phenolic acids and flavonoids which possess anti-inflammatory properties, phytosterol and linolenic acid which play an anticancerogenic role, and polysaccharides which stimulate immunological activity. Polyphenols are absorbed in the alimentary tract, metabolised by CYP450 enzymes, and excreted with urine and faeces. Flavonoids and phenolic acids are characterised by high antioxidative potential, which is closely related to their chemical structure. The high antioxidant potential of phenolic acids is due to the presence and location of hydroxyl groups, a carboxyl group in the immediate vicinity of ortho-diphenolic substituents, and the ethylene group between the phenyl ring and the carboxyl group. As regards flavonoids, essential structural elements are hydroxyl groups at the C5 and C7 positions in the A ring, and at the C3' and C4' positions in the B ring, and a hydroxyl group at the C3 position in the C ring. Furthermore, both, the double bond between C2 and C3, and a ketone group at the C4 position in the C ring enhance the antioxidative potential of these compounds. Polyphenols have an ideal chemical structure for scavenging free radicals and for creating chelates with metal ions, which makes them effective antioxidants in vivo.

  3. Bioactive compounds and antioxidant activity of wolfberry infusion

    Science.gov (United States)

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

    2017-01-01

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

  4. A SAR and QSAR Study of New Artemisinin Compounds with Antimalarial Activity

    Directory of Open Access Journals (Sweden)

    Cleydson Breno R. Santos

    2013-12-01

    Full Text Available The Hartree-Fock method and the 6-31G** basis set were employed to calculate the molecular properties of artemisinin and 20 derivatives with antimalarial activity. Maps of molecular electrostatic potential (MEPs and molecular docking were used to investigate the interaction between ligands and the receptor (heme. Principal component analysis and hierarchical cluster analysis were employed to select the most important descriptors related to activity. The correlation between biological activity and molecular properties was obtained using the partial least squares and principal component regression methods. The regression PLS and PCR models built in this study were also used to predict the antimalarial activity of 30 new artemisinin compounds with unknown activity. The models obtained showed not only statistical significance but also predictive ability. The significant molecular descriptors related to the compounds with antimalarial activity were the hydration energy (HE, the charge on the O11 oxygen atom (QO11, the torsion angle O1-O2-Fe-N2 (D2 and the maximum rate of R/Sanderson Electronegativity (RTe+. These variables led to a physical and structural explanation of the molecular properties that should be selected for when designing new ligands to be used as antimalarial agents.

  5. Chemical constituents from Cornus officinalis and their biological activity 1

    Directory of Open Access Journals (Sweden)

    Zhan-Ying Ma

    2012-01-01

    Full Text Available Objective: To study the chemical constituents from Cornus officinalis Sieb., Et Zucc, and their peroxisome proliferator-activated receptors (PPARs agonist activity. Materials and Methods: The leaves of C. officinalis were extracted three times with 90% EtOH at room temperature. The ethanol extracts were combined and concentrated under reduced pressure to yield residue, which was isolated and purified by silica gel and reverse-phase C 18 column chromatography. The structures were elucidated on the basis of spectroscopic evidence and their physiochemical characteristics. Cell-based luciferase reporter gene assays were used to evaluate PPARα/γ agonistic activities. Results: Five compounds were isolated and elucidated as 10-hydroxyhastatoside (1, β-dihydrocornin (2, isoquercitrin (3, loganin (4 and oleanolic acid (5. Conclusion: Compounds 1 and 2 were obtained from C. officinalis for the first time. Compound 3 exhibited moderate agonistic activities for PPARα, with EC 50 values of 29.5 μM.

  6. Synthesis and biological activity of novel tiliroside derivants.

    Science.gov (United States)

    Qin, Nan; Li, Chun-Bao; Jin, Mei-Na; Shi, Li-Huan; Duan, Hong-Quan; Niu, Wen-Yan

    2011-10-01

    A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i-l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5'-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes.

  7. Synthesis and Biological Activities of Camphor Hydrazone and Imine Derivatives

    Science.gov (United States)

    da Silva, Emerson T.; da Silva Araújo, Adriele; Moraes, Adriana M.; de Souza, Leidiane A.; Silva Lourenço, Maria Cristina; de Souza, Marcus V. N.; Wardell, James L.; Wardell, Solange M. S. V.

    2015-01-01

    Both sonochemical and classical methodologies have been employed to convert camphor, 1,7,7-trimethylbicyclo[2.2.1]heptan-2-one, C9H16C=O, into a number of derivatives including hydrazones, C9H16C=N-NHAr 3, imines, C9H16C=N-R 7, and the key intermediate nitroimine, C9H16C=N-NO2 6. Reactions of nitroamine 6 with nucleophiles by classical methods provided the desired compounds in a range of yields. In evaluations of activity against Mycobacterium tuberculosis, compound 7j exhibited the best activity (minimal inhibitory concentration (MIC) = 3.12 µg/mL), comparable to that of the antitubercular drug ethambutol. The other derivatives displayed modest antimycobacterial activities at 25–50 µg/mL. In in vitro tests against cancer cell lines, none of the synthesized camphor compounds exhibited cytotoxic activities.

  8. Synthesis of N-(6-Arylbenzo[d]thiazole-2-acetamide Derivatives and Their Biological Activities: An Experimental and Computational Approach.

    Science.gov (United States)

    Gull, Yasmeen; Rasool, Nasir; Noreen, Mnaza; Altaf, Ataf Ali; Musharraf, Syed Ghulam; Zubair, Muhammad; Nasim, Faiz-Ul-Hassan; Yaqoob, Asma; DeFeo, Vincenzo; Zia-Ul-Haq, Muhammad

    2016-02-25

    A new series of N-(6-arylbenzo[d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.

  9. New Conjugated Benzothiazole-N-oxides: Synthesis and Biological Activity

    Directory of Open Access Journals (Sweden)

    Pavlína Foltínová

    2009-12-01

    Full Text Available Eleven new 2-styrylbenzothiazole-N-oxides have been prepared by aldol – type condensation reactions between 2-methylbenzothiazole–N-oxide and para-substituted benzaldehydes. Compounds with cyclic amino substituents showed typical push-pull molecule properties. Four compounds were tested against various bacterial strains as well as the protozoan Euglena gracilis as model microorganisms. Unlike previously prepared analogous benzothiazolium salts, only weak activity was recorded.

  10. Physical aspects of biological activity and cancer

    Science.gov (United States)

    Pokorný, Jiří

    2012-03-01

    Mitochondria are organelles at the boundary between chemical-genetic and physical processes in living cells. Mitochondria supply energy and provide conditions for physical mechanisms. Protons transferred across the inner mitochondrial membrane diffuse into cytosol and form a zone of a strong static electric field changing water into quasi-elastic medium that loses viscosity damping properties. Mitochondria and microtubules form a unique cooperating system in the cell. Microtubules are electrical polar structures that make possible non-linear transformation of random excitations into coherent oscillations and generation of coherent electrodynamic field. Mitochondria supply energy, may condition non-linear properties and low damping of oscillations. Electrodynamic activity might have essential significance for material transport, organization, intra- and inter-cellular interactions, and information transfer. Physical processes in cancer cell are disturbed due to suppression of oxidative metabolism in mitochodria (Warburg effect). Water ordering level in the cell is decreased, excitation of microtubule electric polar oscilations diminished, damping increased, and non-linear energy transformation shifted towards the linear region. Power and coherence of the generated electrodynamic field are reduced. Electromagnetic activity of healthy and cancer cells may display essential differences. Local invasion and metastastatic growth may strongly depend on disturbed electrodynamic activity. Nanotechnological measurements may disclose yet unknown properties and parameters of electrodynamic oscillations and other physical processes in healthy and cancer cells.

  11. The Biological Activities of Troponoids and Their Use in Agriculture A Review

    Directory of Open Access Journals (Sweden)

    Saniewski Marian

    2014-09-01

    Full Text Available Chemical compounds containing the tropone structure (2,4,6-cycloheptatrien-1-one, in their molecule, called troponoids, characterized by a seven-membered ring, are distributed in some plants, bacteria and fungi, although they are relatively rare. ß-Thujaplicin (2-hydroxy-4-isopropyl-2,4,6-cycloheptatrien-1-one, also known as hinokitiol, is a natural compound found in several plants of the Cupressaceae family. Besides hinokitiol, related compounds were identified in Cupressaceae trees. It has been demonstrated that hinokitiol and its derivatives have various biological effects, such as antibacterial, antifungal, insecticidal, antimalarial, antitumor, anti-ischemic, iron chelating and the inhibitory activity against polyphenol oxidase activity. Activity similar to ß-thujaplicin has tropolone and its derivatives, which are not present nature. Due to the high scientific and practical interest, synthetic ß-thujaplicin and other troponoids have been produced for many years. In this review, the major biological effects of troponoids, mostly ß-thujaplicin and tropolone, on tyrosinase and polyphenol oxidase activity, ethylene production, antibacterial, antifungal and insecticidal activities, and biotransformation of ß-thujaplicin by cultured plant cells are presented. Accumulation of ß-thujaplicin and related troponoids has been shown in cell cultures of Cupressus lusitanica and other species of Cupressaceae. The biosynthetic pathway of the troponoids in plants, bacteria and fungi has been also briefly described.

  12. Golden Needle Mushroom: A Culinary Medicine with Evidenced-Based Biological Activities and Health Promoting Properties

    Science.gov (United States)

    Tang, Calyn; Hoo, Pearl Ching-Xin; Tan, Loh Teng-Hern; Pusparajah, Priyia; Khan, Tahir Mehmood; Lee, Learn-Han; Goh, Bey-Hing; Chan, Kok-Gan

    2016-01-01

    Flammulina velutipes (enoki, velvet shank, golden needle mushroom or winter mushroom), one of the main edible mushrooms on the market, has long been recognized for its nutritional value and delicious taste. In recent decades, research has expanded beyond detailing its nutritional composition and delved into the biological activities and potential health benefits of its constituents. Many bioactive constituents from a range of families have been isolated from different parts of the mushroom, including carbohydrates, protein, lipids, glycoproteins, phenols, and sesquiterpenes. These compounds have been demonstrated to exhibit various biological activities, such as antitumour and anticancer activities, anti-atherosclerotic and thrombosis inhibition activity, antihypertensive and cholesterol lowering effects, anti-aging and antioxidant properties, ability to aid with restoring memory and overcoming learning deficits, anti-inflammatory, immunomodulatory, anti-bacterial, ribosome inactivation and melanosis inhibition. This review aims to consolidate the information concerning the phytochemistry and biological activities of various compounds isolated from F. velutipes to demonstrate that this mushroom is not only a great source of nutrients but also possesses tremendous potential in pharmaceutical drug development. PMID:28003804

  13. Saponins from Swartzia langsdorffii: biological activities

    Directory of Open Access Journals (Sweden)

    Magalhães Aderbal Farias

    2003-01-01

    Full Text Available The presence of saponins and the molluscicidal activity of the roots, leaves, seeds and fruits of Swartzia langsdorffii Raddi (Leguminosae against Biomphalaria glabrata adults and eggs were investigated. The roots, seeds and fruits were macerated in 95% ethanol. These extracts exerted a significant molluscicidal activity against B. glabrata, up to a dilution of 100 mg/l. Four mixtures (A2, B2, C and D of triterpenoid oleanane type saponins were chromatographically isolated from the seed and fruit extracts. Two known saponins (1 and 2 were identified as beta-D-glucopyranosyl-[alpha-L-rhamnopyranosyl-(1->3- beta-D-glucuronopyranosyl-(1->3]-3beta-hydroxyolean-12-ene-28 -oate, and beta-D-glucopyranosyl-(1->3-beta-D-glucuronopyranosyl-(1 ->3]-3beta-hydroxyolean-12-ene-28-oate, respectively. These two saponins were present in all the mixtures, together with other triterpenoid oleane type saponins, which were shown to be less polar, by reversed-phase HPLC. The saponin identifications were based on spectral evidence, including ¹H-¹H two-dimensional correlation spectroscopy, nuclear Overhauser and exchange spectroscopy, heteronuclear multiple quantum coherence, and heteronuclear multiple-bond connectivity experiments. The toxicity of S. langsdorffii saponins to non-target organisms was prescreened by the brine shrimp lethality test.

  14. Syntheses, characterization, and anti-cancer activities of pyridine-amide based compounds containing appended phenol or catechol groups

    Indian Academy of Sciences (India)

    Afsar Ali; Deepak Bansal; Nagendra K Kaushik; Neha Kaushik; Neha Kaushik; Eun Ha Choi; Rajeev Gupta

    2014-07-01

    Several pyridine-amide compounds appended with phenol/catechol groups are synthesized. These compounds consist of protected or deprotected phenol/catechol groups and offer pyridine, amide, and phenol/catechol functional groups. All compounds have been well-characterized by various spectroscopic methods, elemental analysis, thermal studies, and crystallography. The biological activities of all compounds were investigated while a few compounds significantly decreased the metabolic viability, growth and clonogenicity of T98G cells in dose dependent manner. Accumulation of ROS was observed in T98G cells, which displayed a compromised redox status as evident from increased cellular Caspase 3/7 activity and formation of micronuclei. The in silico pharmacokinetic studies suggest that all compounds have good bioavailability, water solubility and other drug-like parameters. A few compounds were identified as the lead molecules for future investigation due to their: (a) high activity against T98G brain, H-460 lung, and SNU-80 thyroid cancer cells; (b) low cytotoxicity in non-malignant HEK and MRC-5 cells; (c) low toxic risks based on in silico evaluation; (d) good theoretical oral bioavailability according to Lipinski ‘rule of five’ pharmacokinetic parameters; and (e) better drug-likeness and drug-score values.

  15. The traditional uses, chemical constituents and biological activities of Plantago major L. A review.

    Science.gov (United States)

    Samuelsen, A B

    2000-07-01

    Plantago major L. leaves have been used as a wound healing remedy for centuries in almost all parts of the world and in the treatment of a number of diseases apart from wound healing. These include diseases related to the skin, respiratory organs, digestive organs, reproduction, the circulation, against cancer, for pain relief and against infections. P. major contains biologically active compounds such as polysaccharides, lipids, caffeic acid derivatives, flavonoids, iridoid glycosides and terpenoids. Alkaloids and some organic acids have also been detected. A range of biological activities has been found from plant extracts including wound healing activity, anti-inflammatory, analgesic, antioxidant, weak antibiotic, immuno modulating and antiulcerogenic activity. Some of these effects may attribute to the use of this plant in folk medicine.

  16. Generation of structurally novel short carotenoids and study of their biological activity

    DEFF Research Database (Denmark)

    Kim, Se Hyeuk; Kim, Moon S.; Lee, Bun Y.

    2016-01-01

    Recent research interest in phytochemicals has consistently driven the efforts in the metabolic engineering field toward microbial production of various carotenoids. In spite of systematic studies, the possibility of using C30 carotenoids as biologically functional compounds has not been explored...... thus far. Here, we generated 13 novel structures of C30 carotenoids and one C35 carotenoid, including acyclic, monocyclic, and bicyclic structures, through directed evolution and combinatorial biosynthesis, in Escherichia coli. Measurement of radical scavenging activity of various C30 carotenoid...... structures revealed that acyclic C30 carotenoids showed higher radical scavenging activity than did DL-atocopherol. We could assume high potential biological activity of the novel structures of C30 carotenoids as well, based on the neuronal differentiation activity observed for the monocyclic C30 carotenoid...

  17. Effects of 5-FU combined compound Ginseng and Astragalus on biological behavior of human gastric cancer MGC-803 cells

    Institute of Scientific and Technical Information of China (English)

    韦尉元

    2013-01-01

    Objective To observe the in vitro effects of 5-fluorouracil(5-FU) combined Compound Ginseng and Astragalus(CGA) on the biological behaviors such as the proliferation,the cloning,apoptosis and migration of human gastric cancer MGC-803 cells. Methods The cell proliferation inhibition rate was detected by MTT assay,

  18. A two-dimensional coordination compound as a zinc ion selective luminescent probe for biological applications.

    Science.gov (United States)

    Dhara, Koushik; Karan, Santanu; Ratha, Jagnyeswar; Roy, Partha; Chandra, Goutam; Manassero, Mario; Mallik, Biswanath; Banerjee, Pradyot

    2007-09-01

    A 2D coordination compound {[Cu2(HL)(N3)]ClO4}infinity (1; H3L = 2,6-bis(hydroxyethyliminoethyl)-4-methyl phenol) was synthesized and characterized by single-crystal X-ray diffraction to be a polymer in the crystalline state. Each [Cu2(HL)(N3)]+ species is connected to its adjacent unit by a bridging alkoxide oxygen atom of the ligand to form a helical propagation along the crystallographic a axis. The adjacent helical frameworks are connected by a ligand alcoholic oxygen atom along the crystallographic b axis to produce pleated 2D sheets. In solution, 1 dissociates into [Cu2(HL)2(H3L)]2H2O (2); the monomer displays high selectivity for Zn2+ and can be used in HEPES buffer (pH 7.4) as a zinc ion selective luminescent probe for biological application. The system shows a nearly 19-fold Zn2+-selective chelation-enhanced fluorescence response in the working buffer. Application of 2 to cultured living cells (B16F10 mouse melanoma and A375 human melanoma) and rat hippocampal slices was also studied by fluorescence microscopy.

  19. SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF POLYKETONES

    Institute of Scientific and Technical Information of China (English)

    Ismail A.Alkskas; Altaher M.Alhubge; Faizul Azam

    2013-01-01

    Polyketone resins have been prepared by the Friedel-Crafts polymerization of dithiophenylidenecyclopentanone (Ⅰ),dithiophenylidenecyclohexanone (Ⅱ) and dithiophenylideneacetone (Ⅲ) with adipoyl,sebacoyl and terephthaloyl dichlorides using boron trifluoride as catalyst and carbon disulphide as solvent.Polymers were characterized with IR,1H-NMR,and the results showed the presence of carbonyl of ketonic groups in the main chain.The polyketones have inherent viscosities of 0.40-0.70 dL/g.All the polymers are semicrystalline and most of them are partially soluble in most common organic solvents but freely soluble in aprotic solvents.The temperatures of 50% weight loss are as high as 185℃ to 280℃ in air,indicating that these aromatic polyketones have excellent thermal stability.All the polyketones were tested for their antimicrobial activity against bacteria and fungi.

  20. Analysis of Heat Transfer in Actively Cooled Compound Gun Barrel

    Institute of Scientific and Technical Information of China (English)

    WU Bin; XIA Wei

    2005-01-01

    when a gun fires, a large amount of heat is brought in the barrel. Erosion/wear and security problems(self ignition of the propellant) associated with this high thermal energy have to be solved owing to the use of higher combustion gas temperature for improved cannon performance and firing at the sustained high rates. Barrel cooling technologies are the effective measures for addressing this issue. In view of the importance of having knowledge of the heat flux, an approach to calculate heat flux based on measurements was presented and validated. The calculated heat flux is used as the inner boundary condition for modeling heat transfer in a 155 mm mid-wall cooled compound gun barrel. Theoretical analysis and simulated results show that natural air cooling is dramatically slower than the forced liquid mid-wall cooling, accordingly wear life of actively cooled barrel is increased and barrel overheating is prevented.

  1. Photo-activated biological processes as quantum measurements

    CERN Document Server

    Imamoglu, Atac

    2014-01-01

    We outline a framework for describing photo-activated biological reactions as generalized quantum measurements of external fields, for which the biological system takes on the role of a quantum meter. By using general arguments regarding the Hamiltonian that describes the measurement interaction, we identify the cases where it is essential for a complex chemical or biological system to exhibit non-equilibrium quantum coherent dynamics in order to achieve the requisite functionality. We illustrate the analysis by considering measurement of the solar radiation field in photosynthesis and measurement of the earth's magnetic field in avian magnetoreception.

  2. Structure and antibacterial activity of new layered perovskite compounds

    Institute of Scientific and Technical Information of China (English)

    TAN Shao-zao; ZHANG Li-ling; XIA Liao-yuan; LIU Ying-liang; LI Du-xin

    2007-01-01

    New layered perovskite compounds, AgxNa2-xLa2Ti3O10 (x=0.2, 0.3 and 0.5) were synthesized by an ion-exchange reaction of Na2La2Ti3O10 with AgNO3 solution and characterized by energy dispersive X-ray analysis(EDX), X-ray diffractometry(XRD), scanning electron microscopy(SEM) and X-ray photoelectron spectroscopy(XPS). The ion-exchange processes were optimized, and the antibacterial activity, light permanency and water-resistance were evaluated. Surprisedly, no significant changes in crystal structure of Na2La2Ti3O10 are found by the exchange of silver ions. The Ag0.3Na1.7La2Ti3O10 particles conglomerate obviously with irregular shape and size. Ag0.3Na1.7La2Ti3O10, possessing the minimum inhibitory concentrations(MICs) against Escherichia coli (E. coli), Staphylococcus aureus (S. aureus) of 180 mg/L and 240 mg/L, has high antibacterial activity, good light permanency and water-resistance. The ionic state silver in AgxNa2-xLa2Ti3O10 is the antibacterial active component.

  3. Amphibian skin secretions as a new source of antibiotics and biologically active substances

    Directory of Open Access Journals (Sweden)

    Ireneusz Całkosiński

    2009-11-01

    Full Text Available So far, the main sources of biologically active substances used in medicine have been plants, molds, and propolis. The obtained compounds have either therapeutic features or require additional modification. They are sometimes combined with other pharmacological substances to intensify their therapeutic effect. However, the effectiveness of many drugs has been rapidly decreasing. The overuse of antibiotics in the treatment and prophylaxis of human infections (especially in hospitals as well as their widespread and often unjustified use in the treatment and prophylaxis of farm animal illnesses contribute to the development of a variety of resistance mechanisms by microorganisms. Because of the increasing ineffectiveness of antibiotics used so far and difficulties in obtaining new drugs, it is necessary to find new sources of these compounds, for example in animal organisms. Research has demonstrated that amphibian skin secretions are rich in a variety of active substances which have strong pharmacological properties. In these compounds we can distinguish, for example, toxins, antimicrobial peptides, opioid peptides, steroids, and alkaloids. These compounds show cytotoxic, antimicrobial, analgesic, anti-inflammatory, and even antiviral activities (including anti-HIV. These substances can be used in cell receptor studies and in transmembrane ion transport analysis. Because these compounds are secreted by skin glands, they can be easy obtained without injuring these animals. It is probable that amphibian skin constitutes a potential source of modern drugs.

  4. [Amphibian skin secretions as a new source of antibiotics and biologically active substances].

    Science.gov (United States)

    Całkosiński, Ireneusz; Zasadowski, Arkadiusz; Bronowicka-Szydełko, Agnieszka; Dzierzba, Katarzyna; Seweryn, Ewa; Dobrzyński, Maciej; Gamian, Andrzej

    2009-11-12

    So far, the main sources of biologically active substances used in medicine have been plants, molds, and propolis. The obtained compounds have either therapeutic features or require additional modification. They are sometimes combined with other pharmacological substances to intensify their therapeutic effect. However, the effectiveness of many drugs has been rapidly decreasing.The overuse of antibiotics in the treatment and prophylaxis of human infections (especially in hospitals) as well as their widespread and often unjustified use in the treatment and prophylaxis of farm animal illnesses contribute to the development of a variety of resistance mechanisms by microorganisms. Because of the increasing ineffectiveness of antibiotics used so far and difficulties in obtaining new drugs, it is necessary to find new sources of these compounds, for example in animal organisms. Research has demonstrated that amphibian skin secretions are rich in a variety of active substances which have strong pharmacological properties. In these compounds we can distinguish, for example, toxins, antimicrobial peptides, opioid peptides, steroids, and alkaloids.These compounds show cytotoxic, antimicrobial, analgesic, anti-inflammatory, and even antiviral activities (including anti-HIV). These substances can be used in cell receptor studies and in transmembrane ion transport analysis. Because these compounds are secreted by skin glands,they can be easy obtained without injuring these animals. It is probable that amphibian skin constitutes a potential source of modern drugs.

  5. Hop pellets as an interesting source of antioxidant active compounds

    Directory of Open Access Journals (Sweden)

    Andrea Holubková

    2013-02-01

    Full Text Available Hop is a plant used by humankind for thousands of years. This plant is one of the main and indispensable raw materials for the beer production. It is used for various dishes preparation in the cuisine. Hop is also used to inhibit bacterial contamination. The hop extracts are used for its sedative, antiseptic and antioxidant properties in medicine, as a part of many phytopharmaceuticals. The present paper have focused on the extraction of polyphenolic compounds from 4 samples of hop pellets varieties of Aurora, Saaz, Lublin and Saphir, on the analyzing of bioactive substances (polyphenolics and flavonoids in prepared extracts and on the determination of antioxidant activity.  The highest content of polyphenolic substances was determined in the sample Lublin (153.06 mg gallic acid (GAE/g and Saaz (151.87 mg GAE/g. The amount of flavonoids in the samples  was descending order Saaz > Saphir > Aurora > Lublin. Hops, as plant, is known by high content of antioxidant active substances. Antioxidant activity was determined using three independent spectrofotometric methods, radical scavenging assays using 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS and 1,1-diphenyl-2-picrylhydrazyl (DPPH radical and ferric reducing antioxidant power (FRAP. The sample Aurora showed the highest ability to scavenge of ABTS radical cation. Antioxidant activity continued to decline in a row Saphir> Lublin> Saaz. The same trend was also observed by using the FRAP assay. The most effective DPPH radical scavengering activity had the sample Saaz a Saphir (p>0.05.doi:10.5219/270 Normal 0 21 false false false SK X-NONE X-NONE

  6. Activity-Guided Isolation of Antioxidant Compounds from Rhizophora apiculata

    Directory of Open Access Journals (Sweden)

    Hongbin Xiao

    2012-09-01

    Full Text Available Rhizophora apiculata (R. apiculata contains an abundance of biologically active compounds due its special salt-tolerant living surroundings. In this study, the total phenolic content and antioxidant activities of various extract and fractions of stem of R. apiculata were investigated. Results indicated that butanol fraction possesses the highest total phenolic content (181.84 mg/g GAE/g dry extract with strongest antioxidant abilities. Following in vitro antioxidant activity-guided phytochemical separation procedures, lyoniresinol-3α-O-β-arabinopyranoside (1, lyoniresinol-3α-O-β-rhamnoside (2, and afzelechin-3-O-L-rhamno-pyranoside (3 were separated from the butanol fraction. These compounds showed more noticeable antioxidant activity than a BHT standard in the DPPH, ABTS and hydroxyl radical scavenging assays. HPLC analysis results showed that among different plant parts, the highest content of 13 was located in the bark (0.068%, 0.066% and 0.011%, respectively. The results imply that the R. apiculata might be a potential source of natural antioxidants and 13 are antioxidant ingredients in R. apiculata.

  7. Biological activity of diterpenoids isolated from Anatolian Lamiaceae Plants

    Directory of Open Access Journals (Sweden)

    Gülaçtı Topçu

    2007-05-01

    Full Text Available In this study, antibacterial, antifungal, antimycobacterial, cytotoxic, antitumor, cardiovascular, antifeedant, insecticidal, antileishmanial and some other single activities of diterpenoids and norditerpenoids isolated from Turkish Lamiaceae plants, are reviewed. The diterpenoids were isolated from species of Salvia, Sideritis, and Ballota species growing in Anatolia. Fifty abietanes, ten kaurenes, seven pimaranes, six labdanes with their biological activities were reported. While twenty five diterpenoids showed antibacterial activity, eight of which showed activity against fungi. The most cytotoxic one was found to be taxodione (44 isolated from species of Salvia. Antifeedant, insecticidal and insect repellent activity of kaurenes, antimycobacterial activity and cardioactivity of abietanes and norabietanes together with labdanes were also reported.

  8. Synthesis and biological evaluation of 4-(hydroxyalkyl)estradiols and related compounds.

    Science.gov (United States)

    Lovely, C J; Bhat, A S; Coughenour, H D; Gilbert, N E; Brueggemeier, R W

    1997-11-07

    A series of synthetic estrogens containing hydroxyalkyl side chains at the C-4 position of the A ring were designed as metabolically stable analogs of 4-hydroxyestradiol, a catechol estrogen. These synthetic steroids would facilitate investigations on the potential biological role of catechol estrogens and also enable further examination of the structural and electronic constraints on the A ring in the interaction of estrogens with the estrogen receptor. Catechol estrogens are implicated as possible causative agents in estrogen-induced tumorigenesis. 4-Hydroxyestradiol has weaker affinity for the estrogen receptor and exhibits lower estrogenic activity in vivo; on the other hand, the catechol estrogens are prone to further oxidative metabolism and can form reactive intermediates. This report describes the synthesis and initial biochemical evaluation of 4-(hydroxyalkyl)estrogens and 4-(aminoalkyl)estradiols. The 4-(hydroxyalkyl)estrogens were prepared by oxidative hydroboration of 4-alkenylestradiols. The alkenylestradiols were obtained via a Stille cross-coupling between a MOM-protected 4-bromoestradiol and an alkenylstannane. The (4-aminoalkyl)estrogens were prepared from the hydroxyalkyl derivatives with phthalimide under Mitsunobu conditions. The substituted estradiols were evaluated for estrogen receptor binding activity in MCF-7 human mammary carcinoma cells, and 4-(hydroxymethyl)estradiol 1 exhibited the highest affinity with an apparent EC50 value of 364 nM. The relative activities for mRNA induction of the pS2 gene in MCF-7 cell cultures by the 4-(hydroxyalkyl)estrogens closely parallel the relative binding affinities. 4-(Hydroxymethyl)estradiol 1 did not stimulate the growth of MCF-7 cells at concentrations up to 1 microM. Thus, 4-(hydroxymethyl)estradiol 1 exhibited similar estrogen receptor affinity as the catechol estrogen, 4-hydroxyestradiol, and may prove useful in the examination of the biological effects of 4-hydroxyestrogens.

  9. Biologically active substances of hydrophytes Potamogeton perfoliatus L. and Zostera noltii: composition, properties, applications

    Directory of Open Access Journals (Sweden)

    O. V. Novichenko

    2016-01-01

    Full Text Available Primary, the author places special emphasis on the study of traditional technologies for processing of geophytes. Modern development trends in biotechnology demand of expansion of the raw material base. The increase in needs medicine, food and feed industries in biologically active substances pay attention to new unconventional sources of renewable raw materials. From this perspective, higher aquatic plants Zostera noltii and Potamogeton perfoliatus L. can be considered as a perspective object due to its high content of unique biologically active substances with different properties. Rationale of choosing of plant material and identifications of optimum performance and operational conditions for the production of biologically active substances: alcohol extraction in the mixer at room temperature limited to 7-10 days. Studied the organoleptic, physicochemical and microbial properties of end products – aqueous-alcoholic extracts of hydrophytes. Experimentations (UV spectrophotometric analysis, thin layer chromatography, mass spectrometry indicate that the composition of plants and extracts contains different biologically active substances. The high content of quercetin and pigments in the extracts of Z. noltii and Potamogeton perfoliatus L. shows the future use of hydrophytes in the Volga river and the Northern Caspian sea as an additional natural source of flavonoids and antioxidants. Therefore, plant preparations (aqueousalcoholic extracts of zostera and pondweed are combinations of various compounds, which have a high biological activity with different properties: adsorptive capacity, antioxidant and antimicrobial activity. Products of studied plants after extraction with water-alcohol can be used in the food industry as a source-native with minerals, carbohydrates, protein, vitamins, flavonoids, terpenoids, alcohols, aliphatic acids and etc. Find an opportunity of use of biologically active substances from eelgrass and pondweed

  10. Analogs of sex pheromone of processionary moth,Thaumetopoea pityocampa: Synthesis and biological activity.

    Science.gov (United States)

    Camps, F; Fabriàs, G; Gasol, V; Guerrero, A; Hernández, R; Montoya, R

    1988-05-01

    The synthesis and biological activity of some analogs of (Z)-13-hexadecen-11-ynyl acetate1, the major component of the sex pheromone of the processionary mothThaumetopoea pityocampa is described. The analogs have been formally derived by structural modification of the enyne and acetate functions of the parent compound1. In field tests, trifluoroacetate ester16 and the analog,11, with fluorine substitution at the olefin site, decreased the pheromone action, whereas epoxy derivative,10, from epoxidation of the olefin moiety in1, and propionate ester15 gave synergistic activity. The formate14 had a variable effect according to the composition of the lure. Formal reduction of the enyne to give the acetylene2 was found to retain activity. Alcohols12 and13, resulting from hydrolysis of the enyne1 and acetylene2, respectively, inhibited the action of their parent compounds.

  11. Polyphenolic Profile and Biological Activity of Chinese Hawthorn (Crataegus pinnatifida BUNGE Fruits

    Directory of Open Access Journals (Sweden)

    Tunde Jurikova

    2012-12-01

    Full Text Available Chinese hawthorn (Crataegus pinnatifida Bge. fruits are rich in polyphenols (e.g., epicatechin, procyanidin B2, procyanidin B5, procyanidin C1, hyperoside, isoquercitrin and chlorogenic acid—active compounds that exert beneficial effects. This review summarizes all information available on polyphenolic content and methods for their quantification in Chinese hawthorn berries and the relationships between individual polyphenolic compounds as well. The influence of species or cultivars, the locality of cultivation, the stage of maturity, and extract preparation conditions on the polyphenolic content were discussed as well. Currently, only fruits of C. pinnatifida and C. pinnatifida var. major are included in the Chinese Pharmacopoeia. Recent trials have demonstrated the efficacy of Chinese hawthorn fruit in lowering blood cholesterol and the risk of cardiovascular diseases. The fruit has also demonstrated anti-inflammatory and anti-tumour activities. This review deals mainly with the biological activity of the fruit related to its antioxidant properties.

  12. Polyphenolic profile and biological activity of Chinese hawthorn (Crataegus pinnatifida BUNGE) fruits.

    Science.gov (United States)

    Jurikova, Tunde; Sochor, Jiri; Rop, Otakar; Mlcek, Jiri; Balla, Stefan; Szekeres, Ladislav; Adam, Vojtech; Kizek, Rene

    2012-12-06

    Chinese hawthorn (Crataegus pinnatifida Bge.) fruits are rich in polyphenols (e.g., epicatechin, procyanidin B2, procyanidin B5, procyanidin C1, hyperoside, isoquercitrin and chlorogenic acid)--active compounds that exert beneficial effects. This review summarizes all information available on polyphenolic content and methods for their quantification in Chinese hawthorn berries and the relationships between individual polyphenolic compounds as well. The influence of species or cultivars, the locality of cultivation, the stage of maturity, and extract preparation conditions on the polyphenolic content were discussed as well. Currently, only fruits of C. pinnatifida and C. pinnatifida var. major are included in the Chinese Pharmacopoeia. Recent trials have demonstrated the efficacy of Chinese hawthorn fruit in lowering blood cholesterol and the risk of cardiovascular diseases. The fruit has also demonstrated anti-inflammatory and anti-tumour activities. This review deals mainly with the biological activity of the fruit related to its antioxidant properties.

  13. Antioxidative activities and active compounds of extracts from Catalpa plant leaves.

    Science.gov (United States)

    Xu, Hongyu; Hu, Gege; Dong, Juane; Wei, Qin; Shao, Hongbo; Lei, Ming

    2014-01-01

    In order to screen the Catalpa plant with high antioxidant activity and confirm the corresponding active fractions from Catalpa ovata G. Don, C. fargesii Bur., and C. bungei C. A. Mey., total flavonoid contents and antioxidant activities of the extracts/fractions of Catalpa plant leaves were determined. The determined total flavonoid content and antioxidant activity were used as assessment criteria. Those compounds with antioxidant activity were isolated with silica gel column chromatography and ODS column chromatography. Our results showed that the total flavonoid content in C. bungei C. A. Mey. (30.07 mg/g · DW) was the highest, followed by those in C. fargesii Bur. (25.55 mg/g · DW) and C. ovata G. Don (24.96 mg/g · DW). According to the determination results of total flavonoid content and antioxidant activity in 3 clones of leaves of C. bungei C. A. Mey., the total flavonoid content and antioxidant activity in crude extracts from C. bungei C. A. Mey. 6 (CA6) leaves were the highest. Moreover, the results showed that the total flavonoid content and antioxidant activities of ethyl acetate (EA) fraction in ethanol crude extracts in CA6 leaves were the highest, followed by n-butanol, petroleum ether (PE), and water fractions. Two flavonoid compounds with antioxidant activity were firstly isolated based on EA fraction. The two compounds were luteolin (1) and apigenin (2), respectively.

  14. Antioxidative Activities and Active Compounds of Extracts from Catalpa Plant Leaves

    Directory of Open Access Journals (Sweden)

    Hongyu Xu

    2014-01-01

    Full Text Available In order to screen the Catalpa plant with high antioxidant activity and confirm the corresponding active fractions from Catalpa ovata G. Don, C. fargesii Bur., and C. bungei C. A. Mey., total flavonoid contents and antioxidant activities of the extracts/fractions of Catalpa plant leaves were determined. The determined total flavonoid content and antioxidant activity were used as assessment criteria. Those compounds with antioxidant activity were isolated with silica gel column chromatography and ODS column chromatography. Our results showed that the total flavonoid content in C. bungei C. A. Mey. (30.07 mg/g·DW was the highest, followed by those in C. fargesii Bur. (25.55 mg/g·DW and C. ovata G. Don (24.96 mg/g·DW. According to the determination results of total flavonoid content and antioxidant activity in 3 clones of leaves of C. bungei C. A. Mey., the total flavonoid content and antioxidant activity in crude extracts from C. bungei C. A. Mey. 6 (CA6 leaves were the highest. Moreover, the results showed that the total flavonoid content and antioxidant activities of ethyl acetate (EA fraction in ethanol crude extracts in CA6 leaves were the highest, followed by n-butanol, petroleum ether (PE, and water fractions. Two flavonoid compounds with antioxidant activity were firstly isolated based on EA fraction. The two compounds were luteolin (1 and apigenin (2, respectively.

  15. Synthesis and biological activity studies of some thiazolidinones and azetidinones

    Directory of Open Access Journals (Sweden)

    Mehta P

    2006-01-01

    Full Text Available A series of 4-thiazolidinones and 2-azetidinones have been synthesized by condensation of 4,4′-diaminodiphenylsulphone with various aromatic or heterocyclic aldehydes to yield the Schiff′s bases. Cyclocondensation of Schiff′s bases with 2-mercaptopropionic acid afforded 4-thiazolidinone derivatives, and cyclocondensation of Schiff′s bases with chloroacetylchloride in presence of triethylamine afforded 2-azetidinone derivatives. The structures of the newly synthesized compounds were confirmed by analytical and spectral (IR, NMR, and Mass data. All these compounds were evaluated for their in vitro growth-inhibitory activity against several microbes. Compound 4b and 4c exhibited equipotent antibacterial activity with the reference standard ampicillin against Bacillus subtilis.

  16. Chemical Constituents of Descurainia sophia L. and its Biological Activity

    Directory of Open Access Journals (Sweden)

    Nawal H. Mohamed

    2009-01-01

    Full Text Available Seven coumarin compounds were isolated for the first time from the aerial parts of DescurainiaSophia L. identified as scopoletine, scopoline, isoscopoline, xanthtoxol, xanthtoxin, psoralene and bergaptane.Three flavonoids namely kaempferol, quercetine and isorhamnetine and three terpenoid compounds -sitosterol-amyrine and cholesterol were also isolated and identified by physical and chemical methods; melting point, Rfvalues, UV and 1H NMR spectroscopy. Qualitative and quantitative analyses of free and protein amino acidsusing amino acid analyzer were performed. The plant contains 15 amino acids as free and protein amino acidswith different range of concentrations. Fatty acid analysis using GLC, revealed the presence of 10 fatty acids,the highest percentage was palmitic acid (27.45 % and the lowest was lauric acid (0.13%. Biological screeningof alcoholic extract showed that the plant is highly safe and has analgesic, antipyretic and anti-inflammatoryeffects.

  17. In vitro and in vivo biological activities of anthocyanins from Nitraria tangutorun Bobr. fruits.

    Science.gov (United States)

    Ma, Tao; Hu, Na; Ding, Chenxi; Zhang, Qiulong; Li, Wencong; Suo, Yourui; Wang, Honglun; Bai, Bo; Ding, Chenxu

    2016-03-01

    Anthocyanins are the main compounds in Nitraria tangutorun Bobr. The enrichment and purification of anthocyanins on macroporous resins were investigated. Regarding anthocyanin purification, static adsorption and desorption were studied. The optimal experimental conditions were the following: resin type: X-5; static adsorption time: 6h; desorption solution: ethanol-water-HCl (80:19:1, V/V/V; pH 1); desorption time: 40min. Furthermore, the in vitro and in vivo biological activities of the anthocyanins were evaluated. The anthocyanins showed ideal scavenging effects on free radicals in vitro, especially on 1,1-diphenyl-2-picrylhydrazyl (DPPH) and hydroxyl free radical (OH). In the animal experiment, blood lipid metabolism of hyperlipidemia rats was regulated by anthocyanin contents. The superoxide dismutase (SOD) activity and the total antioxidant capacity (TAC) of hyperlipidemia rats were also improved by anthocyanins. These results showed that anthocyanins from N. tangutorun Bobr. fruits had potential biological activities in vivo as well as in vitro.

  18. Phenolic Compounds and Antioxidant Activity of Phalaenopsis Orchid Hybrids

    Directory of Open Access Journals (Sweden)

    Truong Ngoc Minh

    2016-09-01

    Full Text Available Phalaenopsis spp. is the most commercially and economically important orchid, but their plant parts are often left unused, which has caused environmental problems. To date, reports on phytochemical analyses were most available on endangered and medicinal orchids. The present study was conducted to determine the total phenolics, total flavonoids, and antioxidant activity of ethanol extracts prepared from leaves and roots of six commercial hybrid Phalaenopsis spp. Leaf extracts of “Chian Xen Queen” contained the highest total phenolics with a value of 11.52 ± 0.43 mg gallic acid equivalent per g dry weight and the highest total flavonoids (4.98 ± 0.27 mg rutin equivalent per g dry weight. The antioxidant activity of root extracts evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay and β-carotene bleaching method was higher than those of the leaf extracts. Eleven phenolic compounds were identified, namely, protocatechuic acid, p-hydroxybenzoic acid, vanillic acid, caffeic acid, syringic acid, vanillin, ferulic acid, sinapic acid, p-coumaric acid, benzoic acid, and ellagic acid. Ferulic, p-coumaric and sinapic acids were concentrated largely in the roots. The results suggested that the root extracts from hybrid Phalaenopsis spp. could be a potential source of natural antioxidants. This study also helps to reduce the amount of this orchid waste in industrial production, as its roots can be exploited for pharmaceutical purposes.

  19. Phenolic Compounds and Antioxidant Activity of Phalaenopsis Orchid Hybrids

    Science.gov (United States)

    Minh, Truong Ngoc; Khang, Do Tan; Tuyen, Phung Thi; Minh, Luong The; Anh, La Hoang; Quan, Nguyen Van; Ha, Pham Thi Thu; Quan, Nguyen Thanh; Toan, Nguyen Phu; Elzaawely, Abdelnaser Abdelghany; Xuan, Tran Dang

    2016-01-01

    Phalaenopsis spp. is the most commercially and economically important orchid, but their plant parts are often left unused, which has caused environmental problems. To date, reports on phytochemical analyses were most available on endangered and medicinal orchids. The present study was conducted to determine the total phenolics, total flavonoids, and antioxidant activity of ethanol extracts prepared from leaves and roots of six commercial hybrid Phalaenopsis spp. Leaf extracts of “Chian Xen Queen” contained the highest total phenolics with a value of 11.52 ± 0.43 mg gallic acid equivalent per g dry weight and the highest total flavonoids (4.98 ± 0.27 mg rutin equivalent per g dry weight). The antioxidant activity of root extracts evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay and β-carotene bleaching method was higher than those of the leaf extracts. Eleven phenolic compounds were identified, namely, protocatechuic acid, p-hydroxybenzoic acid, vanillic acid, caffeic acid, syringic acid, vanillin, ferulic acid, sinapic acid, p-coumaric acid, benzoic acid, and ellagic acid. Ferulic, p-coumaric and sinapic acids were concentrated largely in the roots. The results suggested that the root extracts from hybrid Phalaenopsis spp. could be a potential source of natural antioxidants. This study also helps to reduce the amount of this orchid waste in industrial production, as its roots can be exploited for pharmaceutical purposes. PMID:27649250

  20. Bioassay-Directed Isolation of Active Compounds with Antiyeast Activity from a Cassia fistula Seed Extract

    Directory of Open Access Journals (Sweden)

    Subramanion L. Jothy

    2011-09-01

    Full Text Available Background and objective: Cassia fistula L belongs to the family Leguminosae, and it is one of the most popular herbal products in tropical countries. C. fistula seeds have been used as a herbal medicine and have pharmacological activity which includes anti-bacterial, anti-fungal, and antioxidant properties. The goal of this study was to identify compounds from C. fistula seeds which are responsible for anti-Candida albicans activity using bioassay-directed isolation. Results: The preliminary phytochemical screening of the plant seed revealed the presence of anthraquinones, flavonoids, saponins, tannins and terpenoids. The isolation of active compounds was carried out in four steps: multiple extractions, fractionation using column chromatography and purification using preparative thin-layer chromatography (TLC and liquid chromatography/mass spectrometry (LC/MS. The structure of separated compounds was determined on the basis of mass spectrometry data. One compound was identified is roseanone. Conclusions: The MS analysis on the active fraction from seed extract of C. fistula confirmed the presence of roseanone with antiyeast activity.

  1. Biological Activity of Curcuminoids Isolated from Curcuma longa

    Directory of Open Access Journals (Sweden)

    Simay Çıkrıkçı

    2008-04-01

    Full Text Available Curcumin is the most important fraction of turmeric which is responsible for its biological activity. In this study, isolation and biological assessment of turmeric and curcumin have been discussed against standard bacterial and mycobacterial strains such as E.coli , S.aureus, E.feacalis, P.aeuroginosa, M.smegmatis, M.simiae, M.kansasii, M. terrae, M.szulgai and the fungi Candida albicans. The antioxidant activity of curcumin and turmeric were also determined by the CUPRAC method.

  2. Transformation of Contaminant Candidate List (CCL3) compounds during ozonation and advanced oxidation processes in drinking water: Assessment of biological effects.

    Science.gov (United States)

    Mestankova, Hana; Parker, Austa M; Bramaz, Nadine; Canonica, Silvio; Schirmer, Kristin; von Gunten, Urs; Linden, Karl G

    2016-04-15

    The removal of emerging contaminants during water treatment is a current issue and various technologies are being explored. These include UV- and ozone-based advanced oxidation processes (AOPs). In this study, AOPs were explored for their degradation capabilities of 25 chemical contaminants on the US Environmental Protection Agency's Contaminant Candidate List 3 (CCL3) in drinking water. Twenty-three of these were found to be amenable to hydroxyl radical-based treatment, with second-order rate constants for their reactions with hydroxyl radicals (OH) in the range of 3-8 × 10(9) M(-1) s(-1). The development of biological activity of the contaminants, focusing on mutagenicity and estrogenicity, was followed in parallel with their degradation using the Ames and YES bioassays to detect potential changes in biological effects during oxidative treatment. The majority of treatment cases resulted in a loss of biological activity upon oxidation of the parent compounds without generation of any form of estrogenicity or mutagenicity. However, an increase in mutagenic activity was detected by oxidative transformation of the following CCL3 parent compounds: nitrobenzene (OH, UV photolysis), quinoline (OH, ozone), methamidophos (OH), N-nitrosopyrolidine (OH), N-nitrosodi-n-propylamine (OH), aniline (UV photolysis), and N-nitrosodiphenylamine (UV photolysis). Only one case of formation of estrogenic activity was observed, namely, for the oxidation of quinoline by OH. Overall, this study provides fundamental and practical information on AOP-based treatment of specific compounds of concern and represents a framework for evaluating the performance of transformation-based treatment processes.

  3. TERPENOIDS FROM THE STEM BARK OF JATROPHA PLANTS AND THEIR BIOLOGICAL ACTIVITIES

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    Manggau Marianti

    2011-11-01

    Full Text Available Three terpenoids, including two diterpenes (curcusone B and jatrophone and a triterpene (stigmasterol have beenisolated from the stem bark of Jatropha plants. Curcusone B and stigmasterol were isolated from J. curcas, meanwhilejatrophone and stigmasterol were from J. gossypifolia. The biological activities of these compounds have beenevaluated toward bacteria, fungi and tumour cells. Isolation was carried out in vacuum liqiud cromatography (VLCtechnique with silica gel as an adsorben and some solvents as eluents. The compound structures were determined byspectroscopic methodes i.e. UV-vis, FTIR, NMR (1-D, 2-D and were then compared based on their spectroscopic datawith similiar data from literatures. The biological properties of these compounds were evaluated against four strains ofbacteria (Acetobacter sp., Eschericia coli, Staphylococcus aureus, and Streptococcus sp., 4 strains of fungi (Aspergilusniger, Penicillium sp. (grey, Penicillium sp. (white and Rhizopus sp. and murine leukemia P-388 cells. The resultsshowed that cytotoxic property of curcusone B towards murine leukemia P-388 cells is better than jatrophone andstigmasterol which are IC50 = 0.57 μg/mL (1.93 μM for curcusone B and IC50 > 100 μg/mL for jatrophone andstigmasterol. Meanwhile, activities against bacteria, jatrophone is better than curcusone B and stigmasterol. Jatrophoneis the most active against S. aureus (bacteria with growth inhibition zone 36 mm and A.niger (fungi is 44 mm. Furtherstudy indicated that jatrophone was bacteriostatic against S. aureus.

  4. Potential Amoebicidal Activity of Hydrazone Derivatives: Synthesis, Characterization, Electrochemical Behavior, Theoretical Study and Evaluation of the Biological Activity

    Directory of Open Access Journals (Sweden)

    Yanis Toledano-Magaña

    2015-05-01

    Full Text Available Four new hydrazones were synthesized by the condensation of the selected hydrazine and the appropriate nitrobenzaldehyde. A complete characterization was done employing 1H- and 13C-NMR, electrochemical techniques and theoretical studies. After the characterization and electrochemical analysis of each compound, amoebicidal activity was tested in vitro against the HM1:IMSS strain of Entamoeba histolytica. The results showed the influence of the nitrobenzene group and the hydrazone linkage on the amoebicidal activity. meta-Nitro substituted compound 2 presents a promising amoebicidal activity with an IC50 = 0.84 μM, which represents a 7-fold increase in cell growth inhibition potency with respect to metronidazole (IC50 = 6.3 μM. Compounds 1, 3, and 4 show decreased amoebicidal activity, with IC50 values of 7, 75 and 23 µM, respectively, as a function of the nitro group position on the aromatic ring. The observed differences in the biological activity could be explained not only by the redox potential of the molecules, but also by their capacity to participate in the formation of intra- and intermolecular hydrogen bonds. Redox potentials as well as the amoebicidal activity can be described with parameters obtained from the DFT analysis.

  5. Influence of hydrothermal treatment on dietary fiber and phenolic compounds content as well as antioxidative activity of legumes seeds

    OpenAIRE

    Agnieszka Filipiak-Florkiewicz; Adam Florkiewicz; Ewa Cieślik; Maria Walczycka; Joanna Kapusta-Duch; Teresa Leszczyńska

    2012-01-01

    Background. Dry legumes seeds are food of high nutrient density. Besides the biologically precious protein they contain essential unsaturated fatty acids, vitamins of group B, dietary fiber and antioxidants. The aim of the research was to assess the influence of different soaking and cooking methods on dietary fiber and phe- nolic compounds content, as well as antioxidative activity of selected legumes’seeds. Material and methods. The experimental material was dry kidney bean origin...

  6. Theoretical and experimental study on lipophilicity and wound healing activity of ginger compounds

    Institute of Scientific and Technical Information of China (English)

    Mohammed Afroz Bakht; Mohammed F Alajmi; Perwez Alam; Aftab Alam; Prawez Alam; Tariq Mohammed Aljarba

    2014-01-01

    Objective: To correlate the chromatographic and computational method to calculate lipophilicity of selected ginger compounds and to observe the effects of log P on wound healing. Methods:Mixtures of acetonitrile and water with acetonitrile content between 95% and 50% v/v in 5% increments were kept separately in 10 different chromatographic chambers, saturated with solvent for 2 h. Spots were observed under UV light at λ=254 nm p-anisaldehyde used as a spraying reagent. Theoretical calculation was done using the Alogps 2.1 online program at www. vcclab.org/lab/alogps. For percentage wound contraction, five groups of animal (mice) (25-30 g) of either sex were selected. Wound were created on dorsal surface of animals using toothed forceps, scalpel and pointed scissors. The wound areas were calculated using vernier caliper. After making wound mice were orally administered 35 mg/kg 6-shogoal, 6-gingerol, 8-gingerol and 10-gingerol respectively. Group E as the control group received tap water. Results:The lipophilicity values determined in thin layer chromatography were correlated with the theoretically calculated various log P by linear regression analysis. Significant correlations were found between log P values calculated by software program and the experimental reversed-phase thin-layer chromatography data. Order of wound healing property of ginger compounds is directly dependent on lipophilicity i.e. more lipophilic compound has highest activity. Conclusions:Experimentally determined lipophilicity (RMO) values were correlated with log Pdetermined by software's and found satisfactory. Lipophilicity (RMO) is a useful parameter for the determination and prediction of biological activity of ginger compounds.

  7. A comparative DFT study on the antioxidant activity of apigenin and scutellarein flavonoid compounds

    Science.gov (United States)

    Sadasivam, K.; Kumaresan, R.

    2011-03-01

    The potent antioxidant activity of flavonoids relevant to their ability to scavenge reactive oxygen species is the most important function of flavonoids. Density functional theory calculations were explored to investigate the antioxidant activity of flavonoid compounds such as apigenin and scutellarein. The biological characteristics are dependent on electronic parameters, describing the charge distribution on the rings of the flavonoid molecules. The computation of structural and various molecular descriptors such as polarizability, dipole moment, energy gap, homolytic O-H bond dissociation enthalpies (BDEs), ionization potential (IP), electron affinity, hardness, softness, electronegativity, electrophilic index and density plot of molecular orbital for neutral as well as radical species were carried out and studied. The B3LYP/6-311G(d,p) basis set was adopted for all the computations. This computation reveals that scutellarein exhibits higher degree of antioxidant activity than apigenin. Their dipole moment and polarizability analysis show that both the compounds are polar in nature and have the capacity to polarize other atoms.

  8. Caatinga plants: Natural and semi-synthetic compounds potentially active against Trichomonas vaginalis.

    Science.gov (United States)

    Vieira, Patrícia de Brum; Silva, Nícolas Luiz Feijó; da Silva, Gloria Narjara Santos; Silva, Denise Brentan; Lopes, Norberto Peporine; Gnoatto, Simone Cristina Baggio; da Silva, Márcia Vanusa; Macedo, Alexandre José; Bastida, Jaume; Tasca, Tiana

    2016-05-01

    Trichomonas vaginalis causes trichomoniasis; the most common but overlooked non-viral sexually transmitted disease worldwide. The treatment is based at 5'-nitroimidazoles, however, failure are related to resistance of T. vaginalis to chemotherapy. Caatinga is a uniquely Brazilian region representing a biome with type desert vegetation and plants present diverse biological activity, however, with few studies. The aim of this study was to investigate the activity against T. vaginalis of different plants from Caatinga and identify the compounds responsible by the activity. A bioguided fractionation of Manilkara rufula was performed and four major compounds were identified: caproate of α-amyrin (1b), acetate of β-amyrin (2a), caproate of β-amyrin (2b), and acetate of lupeol (3a). In addition, six derivatives of α-amyrin (1), β-amyrin (2) and lupeol (3) were synthesized and tested against the parasite. Ursolic acid (5) reduced about 98% of parasite viability after 2h of incubation and drastic ultrastructural alterations were observed by scanning electron microscopy. Moreover, 5 presented high cytotoxicity to HMVII and HeLa cell line and low cytotoxicity against Vero line at 50 μM (MIC against the parasite). Metronidazole effect against T. vaginalis resistant isolate was improved when in association with 5.

  9. The Study of Interactions between Active Compounds of Coffee and Willow (Salix sp. Bark Water Extract

    Directory of Open Access Journals (Sweden)

    Agata Durak

    2014-01-01

    Full Text Available Coffee and willow are known as valuable sources of biologically active phytochemicals such as chlorogenic acid, caffeine, and salicin. The aim of the study was to determine the interactions between the active compounds contained in water extracts from coffee and bark of willow (Salix purpurea and Salix myrsinifolia. Raw materials and their mixtures were characterized by multidirectional antioxidant activities; however, bioactive constituents interacted with each other. Synergism was observed for ability of inhibition of lipid peroxidation and reducing power, whereas compounds able to scavenge ABTS radical cation acted antagonistically. Additionally, phytochemicals from willow bark possessed hydrophilic character and thermostability which justifies their potential use as an ingredient in coffee beverages. Proposed mixtures may be used in the prophylaxis or treatment of some civilization diseases linked with oxidative stress. Most importantly, strong synergism observed for phytochemicals able to prevent lipids against oxidation may suggest protective effect for cell membrane phospholipids. Obtained results indicate that extracts from bark tested Salix genotypes as an ingredient in coffee beverages can provide health promoting benefits to the consumers; however, this issue requires further study.

  10. The study of interactions between active compounds of coffee and willow (Salix sp.) bark water extract.

    Science.gov (United States)

    Durak, Agata; Gawlik-Dziki, Urszula

    2014-01-01

    Coffee and willow are known as valuable sources of biologically active phytochemicals such as chlorogenic acid, caffeine, and salicin. The aim of the study was to determine the interactions between the active compounds contained in water extracts from coffee and bark of willow (Salix purpurea and Salix myrsinifolia). Raw materials and their mixtures were characterized by multidirectional antioxidant activities; however, bioactive constituents interacted with each other. Synergism was observed for ability of inhibition of lipid peroxidation and reducing power, whereas compounds able to scavenge ABTS radical cation acted antagonistically. Additionally, phytochemicals from willow bark possessed hydrophilic character and thermostability which justifies their potential use as an ingredient in coffee beverages. Proposed mixtures may be used in the prophylaxis or treatment of some civilization diseases linked with oxidative stress. Most importantly, strong synergism observed for phytochemicals able to prevent lipids against oxidation may suggest protective effect for cell membrane phospholipids. Obtained results indicate that extracts from bark tested Salix genotypes as an ingredient in coffee beverages can provide health promoting benefits to the consumers; however, this issue requires further study.

  11. Phenolic Compounds from Olea europaea L. Possess Antioxidant Activity and Inhibit Carbohydrate Metabolizing Enzymes In Vitro

    Directory of Open Access Journals (Sweden)

    Nadia Dekdouk

    2015-01-01

    Full Text Available Phenolic composition and biological activities of fruit extracts from Italian and Algerian Olea europaea L. cultivars were studied. Total phenolic and tannin contents were quantified in the extracts. Moreover 14 different phenolic compounds were identified, and their profiles showed remarkable quantitative differences among analysed extracts. Moreover antioxidant and enzymatic inhibition activities were studied. Three complementary assays were used to measure their antioxidant activities and consequently Relative Antioxidant Capacity Index (RACI was used to compare and easily describe obtained results. Results showed that Chemlal, between Algerian cultivars, and Coratina, among Italian ones, had the highest RACI values. On the other hand all extracts and the most abundant phenolics were tested for their efficiency to inhibit α-amylase and α-glucosidase enzymes. Leccino, among all analysed cultivars, and luteolin, among identified phenolic compounds, were found to be the best inhibitors of α-amylase and α-glucosidase enzymes. Results demonstrated that Olea europaea fruit extracts can represent an important natural source with high antioxidant potential and significant α-amylase and α-glucosidase inhibitory effects.

  12. Phenolic Compounds from Olea europaea L. Possess Antioxidant Activity and Inhibit Carbohydrate Metabolizing Enzymes In Vitro

    Science.gov (United States)

    Dekdouk, Nadia; Malafronte, Nicola; Russo, Daniela; Faraone, Immacolata; De Tommasi, Nunziatina; Ameddah, Souad; Severino, Lorella; Milella, Luigi

    2015-01-01

    Phenolic composition and biological activities of fruit extracts from Italian and Algerian Olea europaea L. cultivars were studied. Total phenolic and tannin contents were quantified in the extracts. Moreover 14 different phenolic compounds were identified, and their profiles showed remarkable quantitative differences among analysed extracts. Moreover antioxidant and enzymatic inhibition activities were studied. Three complementary assays were used to measure their antioxidant activities and consequently Relative Antioxidant Capacity Index (RACI) was used to compare and easily describe obtained results. Results showed that Chemlal, between Algerian cultivars, and Coratina, among Italian ones, had the highest RACI values. On the other hand all extracts and the most abundant phenolics were tested for their efficiency to inhibit α-amylase and α-glucosidase enzymes. Leccino, among all analysed cultivars, and luteolin, among identified phenolic compounds, were found to be the best inhibitors of α-amylase and α-glucosidase enzymes. Results demonstrated that Olea europaea fruit extracts can represent an important natural source with high antioxidant potential and significant α-amylase and α-glucosidase inhibitory effects. PMID:26557862

  13. Volatile compounds of raspberry fruit: from analytical methods to biological role and sensory impact.

    Science.gov (United States)

    Aprea, Eugenio; Biasioli, Franco; Gasperi, Flavia

    2015-01-30

    Volatile compounds play a key role in the formation of the well-recognized and widely appreciated raspberry aroma. Studies on the isolation and identification of volatile compounds in raspberry fruit (Rubus idaeus L.) are reviewed with a focus on aroma-related compounds. A table is drawn up containing a comprehensive list of the volatile compounds identified so far in raspberry along with main references and quantitative data where available. Two additional tables report the glycosidic bond and enantiomeric distributions of the volatile compounds investigated up to now in raspberry fruit. Studies on the development and evolution of volatile compounds during fruit formation, ripening and senescence, and genetic and environmental influences are also reviewed. Recent investigations showing the potential role of raspberry volatile compounds in cultivar differentiation and fruit resistance to mold disease are reported as well. Finally a summary of research done so far and our vision for future research lines are reported.

  14. Volatile Compounds of Raspberry Fruit: From Analytical Methods to Biological Role and Sensory Impact

    Directory of Open Access Journals (Sweden)

    Eugenio Aprea

    2015-01-01

    Full Text Available Volatile compounds play a key role in the formation of the well-recognized and widely appreciated raspberry aroma. Studies on the isolation and identification of volatile compounds in raspberry fruit (Rubus idaeus L. are reviewed with a focus on aroma-related compounds. A table is drawn up containing a comprehensive list of the volatile compounds identified so far in raspberry along with main references and quantitative data where available. Two additional tables report the glycosidic bond and enantiomeric distributions of the volatile compounds investigated up to now in raspberry fruit. Studies on the development and evolution of volatile compounds during fruit formation, ripening and senescence, and genetic and environmental influences are also reviewed. Recent investigations showing the potential role of raspberry volatile compounds in cultivar differentiation and fruit resistance to mold disease are reported as well. Finally a summary of research done so far and our vision for future research lines are reported.

  15. Identification of new compounds with high activity against stationary phase Borrelia burgdorferi from the NCI compound collection.

    Science.gov (United States)

    Feng, Jie; Shi, Wanliang; Zhang, Shuo; Zhang, Ying

    2015-06-03

    Lyme disease is the leading tick-borne disease in the USA. Whereas the majority of Lyme disease patients with early disease can be cured with standard treatment, some patients suffer from chronic fatigue and joint and muscular pain despite treatment, a syndrome called posttreatment Lyme disease syndrome. Although the cause is unclear, ineffective killing of Borrelia burgdorferi persisters by current Lyme disease antibiotics is one possible explanation. We took advantage of our recently developed high-throughput viability assay and screened the National Cancer Institute compound library collection consisting of 2526 compounds against stationary phase B. burgdorferi. We identified the top 30 new active hits, including the top six anthracycline antibiotics daunomycin 3-oxime, dimethyldaunomycin, daunomycin, NSC299187, NSC363998 and nogalamycin, along with other compounds, including prodigiosin, mitomycin, nanaomycin and dactinomycin, as having excellent activity against B. burgdorferi stationary phase culture. The anthracycline or anthraquinone compounds, which are known to have both anti-cancer and antibacterial activities, also had high activity against growing B. burgdorferi with low minimum inhibitory concentration. Future studies on the structure-activity relationship and mechanisms of action of anthracyclines/anthraquinones are warranted. In addition, drug combination studies with the anthracycline class of compounds and the current Lyme antibiotics to eradicate B. burgdorferi persisters in vitro and in animal models are needed to determine if they improve the treatment of Lyme disease.

  16. Synthesis and Biological Activity of Some 3,5-Diaryl-1-Benzothiazolopyrazoline Derivatives: Reaction of Chalcones with 2-Hyrazinobenzothiazoles

    Directory of Open Access Journals (Sweden)

    Vandana Sharma

    2009-01-01

    Full Text Available A series of 3,5-diaryl-1-benzothiazolopyrazoline derivatives were synthesized by the reaction of appropriately substituted chalcones and 2-hydrazinobenzothiazole in ethanol. The synthesized heterocycles have been characterized on the basis of their chemical properties and spectroscopic data. These compounds were tested for biological activity against a variety of test organisms.

  17. Synthesis and Biological Activity of Some 3, 5-Diarylisoxazoline Derivatives: Reaction of Substituted Chalcones with Hydroxylamine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Vandana Sharma

    2010-01-01

    Full Text Available A series of 3-aryl-5-styrylisoxazoline/ 3,5-diarylisoxazoline derivatives were synthesized by the reaction of appropriately substituted chalcones and hydroxylamine hydrochloride in presence of alkali in ethanol. The synthesized heterocycles have been characterized on the basis of their chemical properties and spectroscopic data. These compounds were tested for biological activity against a variety of test organisms

  18. Synthesis and biological activity of nifuroxazide and analogs. II.

    Science.gov (United States)

    Tavares, L C; Chisté, J J; Santos, M G; Penna, T C

    1999-09-01

    Nifuroxazyde and six analogs were synthesized by varying the substitute from the para-position of the benzenic ring and the heteroatom of the heterocyclic ring. The MIC of seven resultant compounds was determined by serial dilutions, testing the ATCC 25923 strain of Staphylococcus aureus. A significant increase in the anti-microbial activity of thyophenic analogs, as compared with furanic and pyrrholic analogs, was observed. In addition, unlike the cyano and hydroxyl groups, the acetyl group promoted anti-microbial activity.

  19. Synthesis of Novel Biologically Active s-Triazolo[3,4-b]-1,3,4-thiadiazole Derivatives

    Institute of Scientific and Technical Information of China (English)

    SUN,Yi-Feng

    2004-01-01

    @@ Heterocycles bearing a symmetrical triazole or 1,3,4-thiadiazole ring system are reported to show a broad spectrum of biological activities.[1,2] The 1,2,4-triazole nucleus has been recently incorporated into a wide variety of therapeutically interesting drugs including H1/H2 histamine receptor blockers, cholinesterase active agents, CNS stimulants, antianxiety and sedatives[3] Coumarins are nowadays an important group of organic compounds that used as bactericides, fungicides,anti-inflammatory, anticoagulant, anti-HIV and antitumour agents.[4,5] Keeping in view the biological importance of the above mentioned heterocyclic compounds and in continuation of our search for biologically active nitrogen and sulphur heterocycles, a series of s-triazolo[3,4-b]-1,3,4-thiadiazole derivatives was synthesized.

  20. Antioxidative activity and emulsifying properties of cuttlefish skin gelatin modified by oxidised phenolic compounds

    NARCIS (Netherlands)

    Aewsiri, T.; Benjakul, S.; Visessanguan, W.; Eun, J.B.; Wierenga, P.A.; Gruppen, H.

    2009-01-01

    Antioxidative activity and emulsifying properties of cuttlefish skin gelatin modified by different oxidised phenolic compounds including caffeic acid, ferulic acid and tannic acid at different concentrations were investigated. Oxidised phenolic compounds were covalently attached to gelatin as indica

  1. Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK.

    Science.gov (United States)

    Shen, Sida; Zhuang, Jingjing; Chen, Yijia; Lei, Min; Chen, Jing; Shen, Xu; Hu, Lihong

    2013-07-01

    A series of new arctigenin and 9-deoxy-arctigenin derivatives bearing different ester and ether side chains at the phenolic hydroxyl positions are designed, synthesized, and evaluated for activating AMPK potency in L6 myoblasts. Initial biological evaluation indicates that some alkyl ester and phenethyl ether arctigenin derivatives display potential activities in AMPK phosphorylation improvement. Further structure-activity relationship analysis shows that arctigenin ester derivatives 3a, 3h and 9-deoxy-arctigenin phenethyl ether derivatives 6a, 6c, 6d activate AMPK more potently than arctigenin. Moreover, the 2-(3,4-dimethoxyphenyl)ethyl ether moiety of 6c has been demonstrated as a potential functional group to improve the effect of AMPK phosphorylation. The structural optimization of arctigenin leads to the identification of 6c as a promising lead compound that exhibits excellent activity in AMPK activation.

  2. Synthesis and biological activity of fluorescent neonicotinoid insecticide thiamethoxam.

    Science.gov (United States)

    Taillebois, Emiliane; Langlois, Paul; Cunha, Thomas; Seraphin, Denis; Thany, Steeve H

    2014-08-01

    Here, we describe the synthesis of two new fluorescent derivatives of thiamethoxam and compared their toxicity on aphid Acyrthosiphon pisum and their mode of action on insect nicotinic acetylcholine receptors expressed on the sixth abdominal ganglion. The compound 3 with two 2-chlorothiazole moieties was found to be more toxic using toxicological bioassays 24 h and 48 h after exposure while compound 4 appeared more active using cockroach ganglionic depolarization. Interestingly, thiamethoxam appeared more effective than component 3 and 4, respectively. Our results demonstrated that component 3 and 4 act as agonists of insect nicotinic acetylcholine receptors.

  3. Activated by Combined Magnrtic Field Gravitropic Reaction Reply on Nanodose of Biologicaly Active Compounds

    Science.gov (United States)

    Sheykina, Nadezhda; Bogatina, Nina

    The new science direction nanotechnologies initiated a big jump in the pharmacology and medicine. This leads to the big development of homeopathy. The most interest appeared while investigating of the reaction of biological object on the nano dose of iologically substances. The changing of concentration (in nmol/l) of biologically active material is also possible during weak energy action. For instance, weak combined magnetic field may change a little the concentration of ions that are oriented parallel to the external magnetic field and, by the analogy with said above, lead to the similar effects. Simple estimations give the value for the threshold to the magnetic field by two orders smaller than the geomagnetic field. By this investigation we wanted to understand whether the analogy in the action of nano dose of biologically active substances and weak combined magnetic field presents and whether the action of one of these factors may be replaced by other one. The effect of one of biologically active substances NPA (Naphtyl-Phtalame Acid) solution with the concentration 0.01 mol/l on the gravitropic reaction of cress roots was investigated. It was shown that its effect was the inhibition of cress roots gravitropic reaction. The same inhibition was achieved by the combined magnetic field action on the cress roots, germinated in water. The alternative component of the combined magnetic field coincided formally with the cyclotron frequency of NPA ions. So the analogy in the action of nano dose of biologically active substances and weak combined magnetic field was shown. The combined magnetic field using allows to decrease sufficiently the dose of biologically active substances. This fact can be of great importance in pharmacy and medicine.

  4. Development of Analyses of Biological Steroids Using Chromatography--Special Reference to Vitamin D Compounds and Neurosteroids--

    Institute of Scientific and Technical Information of China (English)

    Kazutake Shimada; Tatsuya Higashi; Kuniko Mitamura

    2003-01-01

    Steroids comprise a large group of natural substances that must frequently be monitored in various biological materials. Due to the metabolic versatility of steroid molecules, extremely complex mixtures are often encountered, necessitating the use of a chromatographic procedure prior to measurement. In this article we present our work, that is, the development of analyses of biological steroids (especially vitamin D compounds and neurosteroids) using gas chromatography/mass spectrometry, high-performance liquid chromatography (including inclusion chromatography using cyclodextrin) and liquid chromatography/mass spectrometry.

  5. Biologically active substances produced by antarctic cryptoendolithic fungi.

    Science.gov (United States)

    Ocampo-Friedmann, R; Friedmann, E I

    1993-01-01

    Researchers report results of laboratory studies of over 200 microbial strains of fungi, algae, cyanobacteria, and heterotrophic bacteria collected in the Ross Desert region of Antarctica. All of the 35 fungal strains produced substances that inhibited the growth of cyanobacteria and algae. The inhibitory effect of the biologically active substance was evident in crushed cell extract but less in spent broth.

  6. Polysaccharies of higher fungi: Biological role, structure and antioxidative activity

    NARCIS (Netherlands)

    Kozarski, M.S.; Klaus, A.; Niksic, M.; Griensven, van L.J.L.D.; Vrvic, M.M.; Jakovljevic, D.M.

    2014-01-01

    The fungal polysaccharides attract a lot of attention due to their multiple challenging bio-logical properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypo-lipidemic, immunomodulatory and immune-stimulatory activities, which all together make them suitable for application

  7. Solar Energy Education. Renewable energy activities for biology

    Energy Technology Data Exchange (ETDEWEB)

    1982-01-01

    An instructional aid for teachers is presented that will allow biology students the opportunity to learn about renewable energy sources. Some of the school activities include using leaves as collectors of solar energy, solar energy stored in wood, and a fuel value test for green and dry woods. A study of organic wastes as a source of fuel is included. (BCS)

  8. Occurrence, biological activity and synthesis of drimane sesquiterpenoids

    NARCIS (Netherlands)

    Jansen, B.J.M.; Groot, de Æ.

    2004-01-01

    In this review the names, structures and occurrence of all new drimanes and rearranged drimanes, which have been published between January 1990 and January 2003 have been collected. Subjects that have been treated are biosynthesis, analysis, biological activities, with special attention to cytotoxic

  9. Biological activities and phytochemical profiles of extracts from different parts of bamboo (Phyllostachys pubescens).

    Science.gov (United States)

    Tanaka, Akinobu; Zhu, Qinchang; Tan, Hui; Horiba, Hiroki; Ohnuki, Koichiro; Mori, Yasuhiro; Yamauchi, Ryoko; Ishikawa, Hiroya; Iwamoto, Akira; Kawahara, Hiroharu; Shimizu, Kuniyoshi

    2014-06-18

    Besides being a useful building material, bamboo also is a potential source of bioactive substances. Although some studies have been performed to examine its use in terms of the biological activity, only certain parts of bamboo, especially the leaves or shoots, have been studied. Comprehensive and comparative studies among different parts of bamboo would contribute to a better understanding and application of this knowledge. In this study, the biological activities of ethanol and water extracts from the leaves, branches, outer culm, inner culm, knots, rhizomes and roots of Phyllostachys pubescens, the major species of bamboo in Japan, were comparatively evaluated. The phytochemical profiles of these extracts were tentatively determined by liquid chromatography-mass spectrometry (LC-MS) analysis. The results showed that extracts from different parts of bamboo had different chemical compositions and different antioxidative, antibacterial and antiallergic activities, as well as on on melanin biosynthesis. Outer culm and inner culm were found to be the most important sources of active compounds. 8-C-Glucosylapigenin, luteolin derivatives and chlorogenic acid were the most probable compounds responsible for the anti-allergy activity of these bamboo extracts. Our study suggests the potential use of bamboo as a functional ingredient in cosmetics or other health-related products.

  10. Biological Activities and Phytochemical Profiles of Extracts from Different Parts of Bamboo (Phyllostachys pubescens

    Directory of Open Access Journals (Sweden)

    Akinobu Tanaka

    2014-06-01

    Full Text Available Besides being a useful building material, bamboo also is a potential source of bioactive substances. Although some studies have been performed to examine its use in terms of the biological activity, only certain parts of bamboo, especially the leaves or shoots, have been studied. Comprehensive and comparative studies among different parts of bamboo would contribute to a better understanding and application of this knowledge. In this study, the biological activities of ethanol and water extracts from the leaves, branches, outer culm, inner culm, knots, rhizomes and roots of Phyllostachys pubescens, the major species of bamboo in Japan, were comparatively evaluated. The phytochemical profiles of these extracts were tentatively determined by liquid chromatography-mass spectrometry (LC-MS analysis. The results showed that extracts from different parts of bamboo had different chemical compositions and different antioxidative, antibacterial and antiallergic activities, as well as on on melanin biosynthesis. Outer culm and inner culm were found to be the most important sources of active compounds. 8-C-Glucosylapigenin, luteolin derivatives and chlorogenic acid were the most probable compounds responsible for the anti-allergy activity of these bamboo extracts. Our study suggests the potential use of bamboo as a functional ingredient in cosmetics or other health-related products.

  11. Enzymes useful for chiral compound synthesis: structural biology, directed evolution, and protein engineering for industrial use.

    Science.gov (United States)

    Kataoka, Michihiko; Miyakawa, Takuya; Shimizu, Sakayu; Tanokura, Masaru

    2016-07-01

    Biocatalysts (enzymes) have many advantages as catalysts for the production of useful compounds as compared to chemical catalysts. The stereoselectivity of the enzymes is one advantage, and thus the stereoselective production of chiral compounds using enzymes is a promising approach. Importantly, industrial application of the enzymes for chiral compound production requires the discovery of a novel useful enzyme or enzyme function; furthermore, improving the enzyme properties through protein engineering and directed evolution approaches is significant. In this review, the significance of several enzymes showing stereoselectivity (quinuclidinone reductase, aminoalcohol dehydrogenase, old yellow enzyme, and threonine aldolase) in chiral compound production is described, and the improvement of these enzymes using protein engineering and directed evolution approaches for further usability is discussed. Currently, enzymes are widely used as catalysts for the production of chiral compounds; however, for further use of enzymes in chiral compound production, improvement of enzymes should be more essential, as well as discovery of novel enzymes and enzyme functions.

  12. [Comparative study of the estrogenic activity of modified estrogens based on data of competitive binding analysis and biological assay].

    Science.gov (United States)

    Pokrovskaia, E V; Ivanenko, T I

    1981-01-01

    A series of bromo- and silyl-derivatives was studied in experiments on immature female rats in vivo and in vitro. All the estrogens studied were conventionally divided into 4 groups according to their ability for concurrent binding with the rat uterus cytosol receptors and their specific bioeffect: equally concurrent and bioeffective compounds (estrone, ethynyl estradiol); slightly concurrent substances with a pronounced uterotropic action (4-silyl estrogens, mestranol); little effective compounds with 4 to 8% of estradiol concurrent activity (2- and 4-bromo-and silyl estradiols, estriol); compounds, not having concurrent and biological effects (2-silyl estrones, 4-bromoestradiol diacetate).

  13. Antioxidant, α-glucosidase and xanthine oxidase inhibitory activity of bioactive compounds from maize (Zea mays L.).

    Science.gov (United States)

    Nile, Shivraj H; Park, Se W

    2014-01-01

    Chemical investigations into maize (Zea mays L.) kernels yielded phenolic compounds, which were structurally established using chromatographic and spectroscopic methods. The isolated phenolic compounds from maize kernel were examined in vitro for their antioxidant abilities by DPPH (2,2-diphenyl-1-picryl hydrazine) radical, OH radical scavenging activity, and reducing ability, along with α-glucosidase and xanthine oxidase (XO) inhibition. The isolated maize phenolics revealed significant xanthine oxidase and α-glucosidase inhibitory activity to that of allopurinol and acarbose in vitro and in vivo, respectively. The kinetics study with xanthine oxidase revealed competitive type of inhibition by isolated maize vanillic acid (M2), ferulic acid (M5), 3'-methoxyhirsutrin (M7), and peonidin-3-glucoside (M10) as compared to control allopurinol. Overall, with few exceptions, all the phenolic compounds from maize kernel revealed significant biological activities with all parameters examined. Also, the phenolic compounds from maize were found to be more reactive toward DPPH radical and had considerable reducing ability and OH radical scavenging activity. These findings suggest that maize kernel phenolic compounds can be considered as potential antioxidant, α-glucosidase, and XO inhibitory agents those might be further explored for the design of lead antioxidant, antidiabetic and antigout drug candidates using in vivo trials.

  14. Biologically Active Substances of Plants from Sali x L. Genus

    OpenAIRE

    O. O. Frolova; E. V. Kompantseva; T. M. Dementieva

    2016-01-01

    The review systematizes data about chemical composition of bark, leaves, inflorescences, and sprouts of different species of Salix L. The closest attention is payed to investigations of Salix, which has been recently carried out in our country and abroad. For every group of biologically active substances described in Salix there are data about suppressed types of pharmacological activity.

  15. Biologically Active Substances of Plants from Sali x L. Genus

    Directory of Open Access Journals (Sweden)

    O. O. Frolova

    2016-01-01

    Full Text Available The review systematizes data about chemical composition of bark, leaves, inflorescences, and sprouts of different species of Salix L. The closest attention is payed to investigations of Salix, which has been recently carried out in our country and abroad. For every group of biologically active substances described in Salix there are data about suppressed types of pharmacological activity.

  16. Chemical composition and biological activity of the plum seed extract

    OpenAIRE

    Savić, Ivan M.; Nikolić, Vesna D.; Savić-Gajić, Ivana M.; Kundaković, Tatjana D.; Stanojković, Tatjana P.; Najman, Stevo J.; id_orcid 0000-0002-2411-9802

    2016-01-01

    The aim of this paper was to estimate the biological activity of the plum seed extract and to define the chemical composition by using the ESI-MS method. During the investigation of the antioxidant activity, the extract showed a better ability to inhibit DPPH radicals compared with amygdalin standard. The results of the antimicrobial study indicate that the extract has a greater effect on Gram-negative bacteria compared with amygdalin. Gram-positive bacteria and fungi remained resistant in bo...

  17. Reactions of 3-Formylchromone with Active Methylene and Methyl Compounds and Some Subsequent Reactions of the Resulting Condensation Products

    Directory of Open Access Journals (Sweden)

    M. Lácova

    2005-08-01

    Full Text Available This review presents a survey of the condensations of 3-formylchromone with various active methylene and methyl compounds, e.g. malonic or barbituric acid derivatives, five-membered heterocycles, etc. The utilisation of the condensation products for the synthesis of different heterocyclic systems, which is based on the ability of the γ-pyrone ring to be opened by the nucleophilic attack is also reviewed. Finally, the applications of microwave irradiation as an unconventional method of reaction activation in the synthesis of condensation products is described and the biological activity of some chromone derivatives is noted.

  18. Comparison of various assays to quantitate macrophage activation by biological response modifiers

    Energy Technology Data Exchange (ETDEWEB)

    Schultz, R.M.; Nanda, S.; Altom, M.G.

    1984-01-01

    Macrophages treated with various compounds that enhance host antitumor resistance exhibit measurable changes in metabolism, function, and surface antigens. In this study, murine peptone-induced peritoneal macrophages were stimulated in vitro by bacterial lipopolysaccharide (LPS), muramyl dipeptide (MDP), and poly I.poly C. They were subsequently compared in their ability to release superoxide and act as tumoristatic and tumoricidal effector cells. Superoxide generation was assayed by the reduction of ferricytochrome C. All three compounds failed to induce significant O/sub 2/- release, unless the cells were also treated with phorbol myristate acetate (PMA). MDP was most active in potentiating the PMA response. In the tumor growth inhibition assay, cytostatic activity was comparable for all three compounds and did not exceed 32 percent. The combination of subthreshold levels of these compounds and hybridoma-derived MAF acted synergistically to induce potent cytostatic activity. In the chromium release assay, LPS and poly I.poly C rendered macrophages cytolytic for P815 target cells at concentrations greater than or equal to 1 microgram/ml. In contrast, significant cytolysis was observed with MDP only at 100 micrograms/ml. Defining precisely the effect of various biological response modifiers on several parameters of macrophage function may facilitate use of these agents in cancer therapy.

  19. How do 2D fingerprints detect structurally diverse active compounds? Revealing compound subset-specific fingerprint features through systematic selection.

    Science.gov (United States)

    Heikamp, Kathrin; Bajorath, Jürgen

    2011-09-26

    In independent studies it has previously been demonstrated that two-dimensional (2D) fingerprints have scaffold hopping ability in virtual screening, although these descriptors primarily emphasize structural and/or topological resemblance of reference and database compounds. However, the mechanism by which such fingerprints enrich structurally diverse molecules in database selection sets is currently little understood. In order to address this question, similarity search calculations on 120 compound activity classes of varying structural diversity were carried out using atom environment fingerprints. Two feature selection methods, Kullback-Leibler divergence and gain ratio analysis, were applied to systematically reduce these fingerprints and generate alternative versions for searching. Gain ratio is a feature selection method from information theory that has thus far not been considered in fingerprint analysis. However, it is shown here to be an effective fingerprint feature selection approach. Following comparative feature selection and similarity searching, the compound recall characteristics of original and reduced fingerprint versions were analyzed in detail. Small sets of fingerprint features were found to distinguish subsets of active compounds from other database molecules. The compound recall of fingerprint similarity searching often resulted from a cumulative detection of distinct compound subsets by different fingerprint features, which provided a rationale for the scaffold hopping potential of these 2D fingerprints.

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

    Science.gov (United States)

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

    2015-10-16

    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.

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

    Directory of Open Access Journals (Sweden)

    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.

  2. Mutagenic and genotoxic activity of chosen dyes and surface active compounds used in the textile industry.

    Science.gov (United States)

    Przybojewska, B; Barański, B; Spiechowicz, E; Szymczak, W

    1989-01-01

    This study was designed to investigate the mutagenic and genotoxic properties of ten dyes and four surface active compounds using Salmonella/microsome assay and the micronucleus test. Five of the investigated dyes (Acid Blue 7, Acid Green 16, Direct Black 19:1, Basic Red 22, Basic Orange 28) possessed mutagenic activity with regard to test strains of Salmonella. In addition, all of them increased the frequency of micronucleated polychromatic erythrocytes in the bone marrow of mice. Three other compounds (Acid Blue 62, Direct Yellow 12, Direct Red 81), which were not mutagenic in the Salmonella/microsome assay, were genotoxic in the micronucleus test. The other two dyes (Reactive Blue 13, Acid Red 213), as well as tested surface active compounds, did not exert mutagenic and genotoxic effects, and therefore, it is most probable that they do not have carcinogenic properties. Besides, it was noted that Acid Blue 62, Direct Black 19:1, Direct Red 81 and Basic Orange 28 cause a significant decrease in the ratio polychromatic to normochromatic erythrocytes in the bone marrow of mice, which means that, at the doses used in the experiment, they are toxic to the erythrocyte series cells of bone marrow. The other compounds under consideration have no such effect.

  3. HPLC Fingerprint of Bioactive Compounds and Antioxidant Activities of Viscum album from Different Host Trees

    Directory of Open Access Journals (Sweden)

    Simona Ioana VICAŞ

    2011-05-01

    Full Text Available Viscum album L. is a medicinal plants used for many years as a remedy in the traditional medicine and in complementary cancer therapies. We investigated the influence of some host trees: Acer campestre (VAA, Fraxinus excelsior (VAF, Populus nigra (VAP, Malus domestica (VAM, and Robinia pseudoacacia (VAR, on the chemical composition and antioxidant activity of leaves and stems from V. album, as well the influence of the solvent (water and ethanol used for extraction on biological activity. HPLC with photodiode array detector analysis of bioactive compounds from leaves and stems of mistletoes (V. album hosted by five differents trees was performed. Antioxidant activities, determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH, Oxygen Radical Absorbance Capacity (ORAC, (Trolox-equivalent antioxidant capacity (TEAC methods were compared with the quantification of total phenolics using the Folin -Ciocalteu reagent. V. album hosted by Fraxinus excelsior (VAF, recorded the highest level of total phenolic acids (108.64 μg/g dry matter while the mistletoe hosted by Malus domestica (VAM had the lowest level of total polyphenols (39.37 μg/g dry matter. In general, higher antioxidant activity was detected in the alcoholic than in the aqueous extracts. The values obtained for total phenolics in both, aqueous and ethanol extracts, decreased in the order: VAR > VAF > VAP > VAA > VAM. The mistletoe stem extracts contained lower levels of phenolics, as compared to leaves, in both solvents. Our results suggest that mistletoe extracts possess significant antioxidant activities that may be due to their bioactive compounds content, suggesting that this plant may be an important source of natural products with chemopreventive and chemotherapeutic activities.

  4. Evaluation of Antimicrobial Activity of Some Compounds Isolated from Rhamnus cathartica L.

    Directory of Open Access Journals (Sweden)

    Manal M. Hamed

    2015-06-01

    Full Text Available A new anthraquinone derivative, 1,8-dihydroxy-2-[(z-4-methylpenta-1,3-dien-1-yl] anthraquinone (1, together with known anthraquinone compounds were defined to be, 2-acetyl-3,8-dihydroxy-6-methoxy-anthraquinone (2 , emodin (3, glucofrangulin A (4 and phenanthrene derivative named dendrochrysanene (5, lactone compounds named [β-sorigenin (6 and geshoidin (7], xanthone compound termed pruniflorone H (8, oxanthrone compound named rumejaposide I (9, flavonol compounds called [kaempferol (10 and quercetin (11] have been isolated from the methanolic extract of Rhamnus cathartica L. All isolated compounds were obtained for the first time from the genus Rhamnus cathartica L. except emodin; they were subjected to antimicrobial activity test; compounds (1, (3, (9 exhibited antibacterial activity [G+ve, G-ve] and anti-yeast activity, whereas, compounds (5, (11 exhibited antibacterial activity [G+ve and G-ve]. But, compounds (2, (4, (7, (10 exhibited antibacterial activity G-ve while compounds (6, (8 exhibited antibacterial activity G-ve and anti-yeast activity. The isolated compounds were confirmed by detailed analysis of their 1H, 13CNMR, mass spectral data and by the results of hydrolytic cleavage.

  5. Quinoxaline 1,4-di-N-Oxides: Biological Activities and Mechanisms of Actions.

    Science.gov (United States)

    Cheng, Guyue; Sa, Wei; Cao, Chen; Guo, Liangliang; Hao, Haihong; Liu, Zhenli; Wang, Xu; Yuan, Zonghui

    2016-01-01

    Quinoxaline 1,4-di-N-oxides (QdNOs) have manifold biological properties, including antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities. These diverse activities endow them broad applications and prospects in human and veterinary medicines. As QdNOs arouse widespread interest, the evaluation of their medicinal chemistry is still in progress. In the meantime, adverse effects have been reported in some of the QdNO derivatives. For example, genotoxicity and bacterial resistance have been found in QdNO antibacterial growth promoters, conferring urgent need for discovery of new QdNO drugs. However, the modes of actions of QdNOs are not fully understood, hindering the development and innovation of these promising compounds. Here, QdNOs are categorized based on the activities and usages, among which the antimicrobial activities are consist of antibacterial, antimycobacterial and anticandida activities, and the antiprotozoal activities include antitrypanosomal, antimalarial, antitrichomonas, and antiamoebic activities. The structure-activity relationship and the mode of actions of each type of activity of QdNOs are summarized, and the toxicity and the underlying mechanisms are also discussed, providing insight for the future research and development of these fascinating compounds.

  6. Quinoxaline 1, 4-di-N-oxides: Biological activities and mechanisms of actions

    Directory of Open Access Journals (Sweden)

    Guyue eCheng

    2016-03-01

    Full Text Available Quinoxaline 1, 4-di-N-oxides (QdNOs have manifold biological properties, including antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities. These diverse activities endow them broad applications and prospects in human and veterinary medicines. As QdNOs arouse widespread interest, the evaluation of their medicinal chemistry is still in progress. In the meantime, adverse effects have been reported in some of the QdNO derivatives. For example, genotoxicity and bacterial resistance have been found in QdNO antibacterial growth promoters, conferring urgent need for discovery of new QdNO drugs. However, the modes of actions of QdNOs are not fully understood, hindering the development and innovation of these promising compounds. Here, QdNOs are categorized based on the activities and usages, among which the antimicrobial activities are consist of antibacterial, antimycobacterial and anticandida activities, and the antiprotozoal activities include antitrypanosomal, antimalarial, antitrichomonas and antiamoebic activities. The structure-activity relationship and the mode of actions of each type of activity of QdNOs are summarized, and the toxicity and the underlying mechanisms are also discussed, providing insight for the future research and development of these fascinating compounds.

  7. 3D-quantitative structure-activity relationship study of organophosphate compounds

    Institute of Scientific and Technical Information of China (English)

    ZHAO Jinsong; WANG Bin; DAI Zhaoxia; WANG Xiaodong; KONG Lingren; WANG Liansheng

    2004-01-01

    The biological effects of most organophosphate compounds (OP) are arising by inhibition of the enzyme acetylcholinesterase (AChE). The 3D-quantitative structure-activity relationship (3D-QSAR) on the acute toxicity to housefly (Musca nobulo L.) of 35 dialkyl phenyl phosphate compounds are studied by using comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) methods, and the reaction mechanism between the OP and the AChE are discussed. In contrast to classical QSAR methods, CoMFA and CoMSIA, especially the combination of both approaches, can give more comprehensive and accurate perspectives on the mechanism of the reaction between OP and AChE. The results show that the length of alkyl, and the electronegative of substituent on phenyl of OP have significant effects on the AChE activity, whereas, the hydrophobicity of OP has little influence. The steric and electronic properties of OP have a dominant influence on the reaction between OP and AChE.

  8. Rapid Preparation Methods of Biological Samples for Ionic Compounds Using Ion Exchange Type Monolithic Silica Spin Column

    OpenAIRE

    宮崎, 将太; 山田, 智子; 太田, 茂徳; 斉藤, 剛; 奈女良, 昭; 大平, 真義

    2010-01-01

    We developed a device comprising a spin column packed with ion exchange type (SCX and SAX) monolithic silica for extracting ionic compounds from biological samples. The methods involving the use of these spin column are not useful for the extraction of ionic analytes, but are highly reproducible for the analysis in serum and urine. This spin column enabled sample preparation in less than 10 min. Handling such as sample loading, washing, and elution of analytes, was exhibited by the centrifuga...

  9. Paradoxical cellular effects and biological role of the multifaceted compound nordihydroguaiaretic acid.

    Science.gov (United States)

    Hernández-Damián, Jacqueline; Andérica-Romero, Ana Cristina; Pedraza-Chaverri, José

    2014-10-01

    Nordihydroguaiaretic acid (NDGA) is a phenolic compound obtained from the leaves of the evergreen desert shrub Larrea tridentata (Creosote bush), which has been used anciently in folk medicine for the treatment of multiple diseases. At the molecular level, NDGA is a potent scavenger of reactive oxygen species. Lipoxygenase inhibition by NDGA has been broadly studied over several cell models; however, NDGA exerts other antioxidant properties and cytoprotective effects in non-tumor cells, which are related with its role as modulator of the nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant response element (ARE) antioxidant pathway. In contrast, in tumor cells NDGA exerts pro-apoptotic activity and anti-tumor effects. Different effects of NDGA have been observed in mitochondria, where NDGA prevents mitochondrial damage in non-tumor cells and induces loss of mitochondrial function in tumor cells. Moreover, NDGA exerts beneficial effects in diverse diseases like cancer, renal damage, Huntington's disease, Alzheimer's disease, and other neurodegenerative pathologies. This work represents a critical review about relevant NDGA mechanisms, cellular effects, and signal pathways involved with possible useful effects.

  10. Oscillatory Activities in Regulatory Biological Networks and Hopf Bifurcation

    Institute of Scientific and Technical Information of China (English)

    YAN Shi-Wei; WANG Qi; XIE Bai-Song; ZHANG Feng-Shou

    2007-01-01

    Exploiting the nonlinear dynamics in the negative feedback loop, we propose a statistical signal-response model to describe the different oscillatory behaviour in a biological network motif. By choosing the delay as a bifurcation parameter, we discuss the existence of Hopf bifurcation and the stability of the periodic solutions of model equations with the centre manifold theorem and the normal form theory. It is shown that a periodic solution is born in a Hopf bifurcation beyond a critical time delay, and thus the bifurcation phenomenon may be important to elucidate the mechanism of oscillatory activities in regulatory biological networks.

  11. Synthesis and biological activity of salinomycin conjugates with floxuridine.

    Science.gov (United States)

    Huczyński, Adam; Antoszczak, Michał; Kleczewska, Natalia; Lewandowska, Marta; Maj, Ewa; Stefańska, Joanna; Wietrzyk, Joanna; Janczak, Jan; Celewicz, Lech

    2015-03-26

    As part of our program to develop anticancer agents, we have synthesized new compounds, which are conjugates between well-known anticancer drug, floxuridine and salinomycin which is able to selectivity kill cancer stem cells. The conjugates were obtained in two ways i.e. by copper(I) catalysed click Huisgen cycloaddition reaction performed between 3'-azido-2',3'-dideoxy-5-fluorouridine and salinomycin propargyl amide, and by the ester synthesis starting from salinomycin and floxuridine under mild condition. The compounds obtained were characterized by spectroscopic methods and evaluated for their in vitro cytotoxicity against seven human cancer cell lines as well as antibacterial activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). The conjugate obtained by esterification reaction showed a significantly higher antiproliferative activity against the drug-resistant cancer cells and lower toxicity than those of salinomycin and floxuridine towards normal cells, as well as standard anticancer drugs, such as cisplatin and doxorubicin. The conjugate compound revealed also moderate activity against MRSA and MRSE bacterial strains. Very high activity of floxuridine and 5-fluorouracil against MRSA and MRSE has been also observed.

  12. Compounds and methods for the production of long chain hydrocarbons from biological sources

    Science.gov (United States)

    Gordon, John Cameron; Silks, Louis A; Sutton, Andrew D; Wu, Ruilian; Schlaf, Marcel; Waldie, Fraser; West, Ryan; Collias, Dimitris Ioannis

    2016-08-23

    The present invention is directed to the preparation of oxygenated, unsaturated hydrocarbon compounds, such as derivatives of furfural or hydroxymethyl furfural produced by aldol condensation with a ketone or a ketoester, as well as methods of deoxidatively reducing those compounds with hydrogen under acidic conditions to provide saturated hydrocarbons useful as fuels.

  13. WENDI: A tool for finding non-obvious relationships between compounds and biological properties, genes, diseases and scholarly publications

    Directory of Open Access Journals (Sweden)

    Zhu Qian

    2010-08-01

    Full Text Available Abstract Background In recent years, there has been a huge increase in the amount of publicly-available and proprietary information pertinent to drug discovery. However, there is a distinct lack of data mining tools available to harness this information, and in particular for knowledge discovery across multiple information sources. At Indiana University we have an ongoing project with Eli Lilly to develop web-service based tools for integrative mining of chemical and biological information. In this paper, we report on the first of these tools, called WENDI (Web Engine for Non-obvious Drug Information that attempts to find non-obvious relationships between a query compound and scholarly publications, biological properties, genes and diseases using multiple information sources. Results We have created an aggregate web service that takes a query compound as input, calls multiple web services for computation and database search, and returns an XML file that aggregates this information. We have also developed a client application that provides an easy-to-use interface to this web service. Both the service and client are publicly available. Conclusions Initial testing indicates this tool is useful in identifying potential biological applications of compounds that are not obvious, and in identifying corroborating and conflicting information from multiple sources. We encourage feedback on the tool to help us refine it further. We are now developing further tools based on this model.

  14. Structure-property relationship of quinuclidinium surfactants--Towards multifunctional biologically active molecules.

    Science.gov (United States)

    Skočibušić, Mirjana; Odžak, Renata; Štefanić, Zoran; Križić, Ivana; Krišto, Lucija; Jović, Ozren; Hrenar, Tomica; Primožič, Ines; Jurašin, Darija

    2016-04-01

    Motivated by diverse biological and pharmacological activity of quinuclidine and oxime compounds we have synthesized and characterized novel class of surfactants, 3-hydroxyimino quinuclidinium bromides with different alkyl chains lengths (CnQNOH; n=12, 14 and 16). The incorporation of non conventional hydroxyimino quinuclidinium headgroup and variation in alkyl chain length affects hydrophilic-hydrophobic balance of surfactant molecule and thereby physicochemical properties important for its application. Therefore, newly synthesized surfactants were characterized by the combination of different experimental techniques: X-ray analysis, potentiometry, electrical conductivity, surface tension and dynamic light scattering measurements, as well as antimicrobial susceptibility tests. Comprehensive investigation of CnQNOH surfactants enabled insight into structure-property relationship i.e., way in which the arrangement of surfactant molecules in the crystal phase correlates with their solution behavior and biologically activity. The synthesized CnQNOH surfactants exhibited high adsorption efficiency and relatively low critical micelle concentrations. In addition, all investigated compounds showed very potent and promising activity against Gram-positive and clinically relevant Gram-negative bacterial strains compared to conventional antimicrobial agents: tetracycline and gentamicin. The overall results indicate that bicyclic headgroup with oxime moiety, which affects both hydrophilicity and hydrophobicity of CnQNOH molecule in addition to enabling hydrogen bonding, has dominant effect on crystal packing and physicochemical properties. The unique structural features of cationic surfactants with hydroxyimino quinuclidine headgroup along with diverse biological activity have made them promising structures in novel drug discovery. Obtained fundamental understanding how combination of different functionalities in a single surfactant molecule affects its physicochemical

  15. Evaluation of in vivo biological activity profile of isoorientin.

    Science.gov (United States)

    Küpeli, Esra; Aslan, Mustafa; Gürbüz, Ilhan; Yesilada, Erdem

    2004-01-01

    Anti-nociceptive, anti-inflammatory and gastroprotective activities of the known C-glycosyl flavonoid, isoorientin, were studied in rats and mice. For the anti-nociceptive activity assessment the p-benzoquinone-induced writing test, for the anti-inflammatory activity the carrageenan-induced hind paw edema model in mice, and for the gastroprotective activity the EtOH-induced ulcerogenesis model in rats were used. Isoorientin was shown to possess significant anti-nociceptive and anti-inflammatory activities at 15 mg/kg and 30 mg/kg doses, without inducing any apparent acute toxicity as well as gastric damage. However, the compound did not possess any significant gastroprotective activity against EtOH-induced ulcerogenesis.

  16. Extraction of high added value biological compounds from sardine, sardine-type fish and mackerel canning residues--a review.

    Science.gov (United States)

    Ferraro, Vincenza; Carvalho, Ana P; Piccirillo, Clara; Santos, Manuela M; Castro, Paula M L; Pintado, Manuela E

    2013-08-01

    Different valuable compounds, which can be employed in medicine or in other industries (i.e. food, agrochemical, pharmaceutical) can be recovered from by-products and waste from the fish canning industries. They include lipids, proteins, bio-polymers, minerals, amino acids and enzymes; they can be extracted from wastewaters and/or from solid residues (head, viscera, skin, tails and flesh) generated along the canning process, through the filleting, cooking, salting or smoking stages. In this review, the opportunities for the extraction and the valorisation of bioactive compounds from sardine, sardine-type fish and mackerel canning residues are examined and discussed. These are amongst the most consumed fishes in the Mediterranean area; moreover, canning is one of the most important and common methods of preservation. The large quantities of by-products generated have great potentials for the extraction of biologically desirable high added value compounds.

  17. Studies on chemical modification and biology of a natural product, gambogic acid (III): determination of the essential pharmacophore for biological activity.

    Science.gov (United States)

    Wang, Xiaojian; Lu, Na; Yang, Qian; Gong, Dandan; Lin, Changjun; Zhang, Shenglie; Xi, Meiyang; Gao, Yuan; Wei, Libing; Guo, Qinglong; You, Qidong

    2011-04-01

    Caged 4-oxa-tricyclo[4.3.1.0(3,7)]dec-2-one structural motifs are found in Garcinia natural products that demonstrate anti-tumor activity. Gambogic acid (GA, 1), the most abundant caged Garcinia xanthones, has been reported to be a promising anti-cancer agent. To identify the essential pharmacophore for its anti-tumor activity, a series of GA analogues that address potential key structural features for biological activity were synthesized, among which compound 11a displayed comparable in vitro anti-tumor activity as GA. Mechanistic studies on 11a determined that the compound induces apoptosis as well as arrests the G2/M phase of the cell cycle in HepG2 cells. The determination of the essential part of the scaffold found in GA to maintain anti-tumor effects, and the SAR based on the caged pharmacophore are reported and will provide key information for future anti-cancer drug development studies.

  18. Synthesis of Lactosylated Piperazinyl Porphyrins and Their Biological Activity

    Institute of Scientific and Technical Information of China (English)

    LI,He-Ping; CAO,Zhong; XIAO,Hua-Wu

    2008-01-01

    The aim of this work is to synthesize of a new family of lactosylated piperazinly porphyrins, in which the galactoside piperazine moieties are linked to the tetra- and mono-phenyl rings of tetraphenylporphyrin (TPP).5,10,15,20-Tetrakis[4-(4-lactobionylpiperazin-1-yl)phenyl]porphyrin (TLPP) and 5-mono[4-(4-lactobionylpiperazin-1-yl)phenyl]-10,15,20-triphenylporphyrin (MLPP) have been synthesized. A detailed 1H NMR study gave their complete structural elucidation. The UV-Visible, mass spectra and elemental analysis are also presented. The biological activity on cancer cells and the pharmacokinetics have also been evaluated, showing a better biological activity, a very high liver to skin ratio and short retention time in tissues. It was suggested that such novel lactosylated piperazinly porphyrins, as potential hepatocyte-selective targeting drugs, exhibit a promising activity in photodynamic therapy (PDT).

  19. Protein stability and enzyme activity at extreme biological temperatures

    Energy Technology Data Exchange (ETDEWEB)

    Feller, Georges, E-mail: gfeller@ulg.ac.b [Laboratory of Biochemistry, Centre for Protein Engineering, Institute of Chemistry B6a, University of Liege, B-4000 Liege (Belgium)

    2010-08-18

    Psychrophilic microorganisms thrive in permanently cold environments, even at subzero temperatures. To maintain metabolic rates compatible with sustained life, they have improved the dynamics of their protein structures, thereby enabling appropriate molecular motions required for biological activity at low temperatures. As a consequence of this structural flexibility, psychrophilic proteins are unstable and heat-labile. In the upper range of biological temperatures, thermophiles and hyperthermophiles grow at temperatures > 100 {sup 0}C and synthesize ultra-stable proteins. However, thermophilic enzymes are nearly inactive at room temperature as a result of their compactness and rigidity. At the molecular level, both types of extremophilic proteins have adapted the same structural factors, but in opposite directions, to address either activity at low temperatures or stability in hot environments. A model based on folding funnels is proposed accounting for the stability-activity relationships in extremophilic proteins. (topical review)

  20. Polysaccharides of higher fungi: Biological role, structure, and antioxidative activity

    Directory of Open Access Journals (Sweden)

    Kozarski Maja S.

    2014-01-01

    Full Text Available Fungal polysaccharides attract a lot of attention due to their multiple challenging biological properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypolipidemic and immunomodulatory and immune-stimulatory activities, which all together make them suitable for application in many quite distinctive areas, such as food industry, biomedicine, cosmetology, agriculture, environmental protection and waste water management. This article presents results with respect to biological properties, structure and procedures related to the isolation and activation of polysaccharides of higher fungi. It is considered and presented along with a review of the critical antioxidative activity and possible influence of the structural composition of polysaccharide extracts (isolated from these higher fungi upon their antioxidative properties.

  1. Synthesis, Characterization, and Biological Activity of 4-(2-Hydroxy-5-(aryl-diazenylphenyl-6-(arylpyrimidin-2-ols Derivatives

    Directory of Open Access Journals (Sweden)

    Chandrashekhar P. Pandhurnekar

    2013-01-01

    Full Text Available With the aim of synthesizing new heterocyclic compounds and exploring biological potency, new series of chalcones, that is, 3-(2-hydroxy-5-(aryl-diazenylphenyl-1-(arylprop-2-en-1-one and their pyrimidine derivatives, that is, 4-(2-hydroxy-5-(aryl-diazenylphenyl-6-(arylpyrimidin-2-ols were synthesized using different aromatic amines and salicylaldehyde as starting moieties. The structures of newly synthesized compounds were confirmed using different spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, and mass spectral analysis, and elemental analysis. The newly synthesized pyrimidines derivatives were screened for their in vitro antibacterial and antifungal activities. It was observed that some of the newly synthesized compounds had shown promising activity against several bacterial and fungal stains. Anti-bacterial activity and anti-fungal activity studies revealed that pyrimidine derivatives consisting of nitro group in their molecular structure possess better activity than their corresponding chalcones.

  2. Isolation of biologically active constituents from Moringa peregrina (Forssk. Fiori. (family: Moringaceae growing in Egypt

    Directory of Open Access Journals (Sweden)

    Taha S El-Alfy

    2011-01-01

    Full Text Available Background: Moringa peregrina is a wild plant that grown in the eastern desert mountains in Egypt. Although, this plant is native to Egypt, no details studies were traced on its chemical composition and biological activity. Materials and Methods: The different fractions of the ethanolic extract of the dried aerial parts of the plants were subjected to fractionation and purification on various silica and sephadex columns for the isolation of the major compounds which were tested for there anticancer activity. The aqueous and ethanolic extract as well as its different fractions were tested for antihyperglycemic effect on Streptozitocin-induced diabetes in rats. Results: Investigation of the different fractions of the ethanolic extract of the aerial parts of M. peregrina yielded lupeol acetate (1, β-amyrin (2, α-amyrin (3, β-sitosterol (4, β-sitosterol-3-O-glucoside (5, apigenin (6, rhamnetin (7, neochlorogenic acid (10, rhamnetin-3-O-rutinoside (12, and 6-methoxy-acacetin-8-C-β-glucoside (13 which were isolated for the first time from the plant. Compound (13 was isolated for the first time from genus Moringa. In addition, quercetin (8, chryseriol-7-O-rhamnoside (9 and quercetin-3-O-rutinoside (11 were also isolated. Identification has been established by spectral data (UV, MS, IR, 1H, 1H -1H COSY, and 13C-NMR. The major isolated compounds were found to have valuable cytotoxic activities against breast (MCF 7 and colon (HCT 116 cancer cell lines and their activities were comparable to the reference drug doxorubicin. On the other hand, the aqueous and ethanolic extracts as well as the n-hexane fraction were found to have potent antihyperglycemic effect on Streptozitocin-induced diabetes in rats. Conclusion: The Egyptian plant M. peregrina is rich in biologically active ingredients which showed potent cytotoxic activity and also its ethanolic extraxt exert a significant antihyperglycemic effect.

  3. The structure, occurrence and biological activity of ellagitannins: a general review

    Directory of Open Access Journals (Sweden)

    Lidia Lipińska

    2014-09-01

    Full Text Available The present paper deals with the structure, occurrence and biological activity of ellagitannins. Ellagitannins belong to the class of hydrolysable tannins, they are esters of hexahydroxydiphenoic acid and monosaccharide (most commonly glucose. Ellagitannins are slowly hydrolysed in the digestive tract, releasing the ellagic acid molecule. Their chemical structure determines physical and chemical properties and biological activity. Ellagitannins occur naturally in some fruits (pomegranate, strawberry, blackberry, raspberry, nuts (walnuts, almonds, and seeds. They form a diverse group of bioactive polyphenols with anti-infl ammatory, anticancer, antioxidant and antimicrobial (antibacterial, antifungal and antiviral activity. Furthermore, they improve the health of blood vessels. The paper discusses the metabolism and bioavailability of ellagitannins and ellagic acid. Ellagitannins are metabolized in the gastrointestinal tract by intestinal microbiota. They are stable in the stomach and undergo neither hydrolysis to free ellagic acid nor degradation. In turn, ellagic acid can be absorbed in the stomach. This paper shows the role of cancer cell lines in the studies of ellagitannins and ellagic acid metabolism. The biological activity of these compounds is broad and thus the focus is on their antimicrobial, anti-inflammatory and antitumor properties. Ellagitannins exhibit antimicrobial activity against fungi, viruses, and importantly, bacteria, including antibiotic-resistant strains such as methicillinresistant Staphylococcus aureus.

  4. Hydrodynamic collective effects of active proteins in biological membranes

    CERN Document Server

    Koyano, Yuki; Mikhailov, Alexander S

    2016-01-01

    Lipid bilayers forming biological membranes are known to behave as viscous 2D fluids on submicrometer scales; usually they contain a large number of active protein inclusions. Recently, it has been shown [Proc. Nat. Acad. Sci. USA 112, E3639 (2015)] that such active proteins should in- duce non-thermal fluctuating lipid flows leading to diffusion enhancement and chemotaxis-like drift for passive inclusions in biomembranes. Here, a detailed analytical and numerical investigation of such effects is performed. The attention is focused on the situations when proteins are concentrated within lipid rafts. We demonstrate that passive particles tend to become attracted by active rafts and are accumulated inside them.

  5. Design, Synthesis and Biological Evaluation of 1,4-Disubstituted-3,4-dihydroisoquinoline Compounds as New Tubulin Polymerization Inhibitors

    Directory of Open Access Journals (Sweden)

    Ling Zhang

    2015-05-01

    Full Text Available A series of 1,4-disubstituted-3,4-dihydroisoquinoline derivatives designed as tubulin polymerization inhibitors were synthesized. Their cytotoxic activities against the CEM leukemia cell line were evaluated. Most of them displayed moderate cytotoxic activities, and compounds 21 and 32 showed good activities with IC50 of 4.10 and 0.64 μM, respectively. The most potent compound 32 was further confirmed to be able to inhibit tubulin polymerization, and its hypothetical binding mode with tubulin was obtained by molecular docking.

  6. Glutarimides: Biological activity, general synthetic methods and physicochemical properties

    Directory of Open Access Journals (Sweden)

    Popović-Đorđević Jelena B.

    2015-01-01

    Full Text Available Glutarimides, 2,6-dioxopiperidines are compounds that rarely occur in natural sources, but so far isolated ones exert widespread pharmacological activities, which makes them valuable as potential pharmacotherapeutics. Glutarimides act as androgen receptor antagonists, anti-inflammatory, anxiolytics, antibacterials, and tumor suppressing agents. Some synthetic glutarimide derivatives are already in use as immunosuppressive and sedative (e.g., thalidomide or anxiolytics (buspirone drugs. The wide applicability of this class of compounds, justify the interest of scientists to explore new pathways for its syntheses. General methods for synthesis of six-membered imide ring, are presented in this paper. These methods include: a reaction of dicarboxylic acids with ammonia or primary amine, b reactions of cyclization: amido-acids, diamides, dinitriles, nitrilo-acids, amido-nitriles, amido-esters, amidoacyl-chlorides or diacyl-chlorides, c adition of carbon-monoxide on a,b-unsaturated amides, d oxidation reactions, e Michael adition of active methylen compounds on methacrylamide or conjugated amides. Some of the described methods are used for closing glutarimide ring in syntheses of farmacological active compounds sesbanimide and aldose reductase inhibitors (ARI. Analyses of the geometry, as well as, the spectroscopic analyses (NMR and FT-IR of some glutarimides are presented because of their broad spectrum of pharmacological activity. To elucidate structures of glutarimides, geometrical parameters of newly synthesized tert-pentyl-1-benzyl-4-methyl-glutarimide-3-carboxylate (PBMG are analyzed and compared with the experimental data from X-ray analysis for glutarimide. Moreover, molecular electrostatic potential (MEP surface which is plotted over the optimized geometry to elucidate the reactivity of PBMG molecule is analyzed. The electronic properties of glutarimide derivatives are explained on the example of thalidomide. The Frontier Molecular Orbital

  7. Compositions comprising a polypeptide having cellulolytic enhancing activity and a heterocyclic compound and uses thereof

    Energy Technology Data Exchange (ETDEWEB)

    Xu, Feng; Sweeney, Matthew; Quinlan, Jason

    2016-08-02

    The present invention relates to compositions comprising: a polypeptide having cellulolytic enhancing activity and a heterocyclic compound. The present invention also relates to methods of using the compositions.

  8. Compositions comprising a polypeptide having cellulolytic enhancing activity and a bicycle compound and uses thereof

    Energy Technology Data Exchange (ETDEWEB)

    Xu, Feng; Sweeney, Matthew; Quinlan, Jason

    2015-06-16

    The present invention relates to compositions comprising: a polypeptide having cellulolytic enhancing activity and a bicyclic compound. The present invention also relates to methods of using the compositions.

  9. Compositions comprising a polypeptide having cellulolytic enhancing activity and a bicyclic compound and uses thereof

    Energy Technology Data Exchange (ETDEWEB)

    Quinlan, Jason; Xu, Feng; Sweeney, Matthew

    2016-10-04

    The present invention relates to compositions comprising: a polypeptide having cellulolytic enhancing activity and a bicyclic compound. The present invention also relates to methods of using the compositions.

  10. The relationship between molecular structure and biological activity of alkali metal salts of vanillic acid: Spectroscopic, theoretical and microbiological studies

    Science.gov (United States)

    Świsłocka, Renata; Piekut, Jolanta; Lewandowski, Włodzimierz

    In this paper we investigate the relationship between molecular structure of alkali metal vanillate molecules and their antimicrobial activity. To this end FT-IR, FT-Raman, UV absorption and 1H, 13C NMR spectra for lithium, sodium, potassium, rubidium and caesium vanillates in solid state were registered, assigned and analyzed. Microbial activity of studied compounds was tested against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Proteus vulgaris, Bacillus subtilis and Candida albicans. In order to evaluate the dependence between chemical structure and biological activity of alkali metal vanillates the statistical analysis was performed for selected wavenumbers from FT-IR spectra and parameters describing microbial activity of vanillates. The geometrical structures of the compounds studied were optimized and the structural characteristics were determined by density functional theory (DFT) using at B3LYP method with 6-311++G** as basis set. The obtained statistical equations show the existence of correlation between molecular structure of vanillates and their biological properties.

  11. Biologically active acylglycerides from the berries of saw-palmetto (Serenoa repens).

    Science.gov (United States)

    Shimada, H; Tyler, V E; McLaughlin, J L

    1997-04-01

    Brine shrimp lethality-directed fractionation of the 95% EtOH extract of the powdered, dried berries of Serenoa repens (Bart.) Small (saw-palmetto) (Palmae) led to the isolation of two monoacylglycerides, 1-monolaurin (1) and 1-monomyristin (2). Compounds 1 and 2 showed moderate biological activities in the brine shrimp lethality test and against renal (A-498) and pancreatic (PACA-2) human tumor cells; borderline cytotoxicity was exhibited against human prostatic (PC-3) cells. The fruits and extracts of saw-palmetto are taken orally as an herbal medicine to prevent prostatic hyperplasias.

  12. Antioxidant and other biological activities of phenols from olives and olive oil.

    Science.gov (United States)

    Visioli, Francesco; Poli, Andrea; Gall, Claudio

    2002-01-01

    Olive oil is the principal source of fats in the Mediterranean diet, which has been associated with a lower incidence of coronary heart disease and certain cancers. Phenolic compounds, e.g., hydroxytyrosol and oleuropein, in extra-virgin olive oil are responsible for its peculiar pungent taste and for its high stability. Recent findings demonstrate that olive oil phenolics are powerful antioxidants, both in vitro and in vivo, and possess other potent biological activities that could partially account for the observed healthful effects of the Mediterranean diet.

  13. BIOLOGICAL VALUE OF PUNY FRUITS RELATED TO THEIR ANTIRADICAL ACTIVITY

    Directory of Open Access Journals (Sweden)

    M. BALOGHOVÁ

    2013-12-01

    Full Text Available All analysed species of puny fruits (red currant (Ribes rubrum L variant Jonkheervan Tets, white currant (Ribes vulgare L. variant Blanka, black currant (Ribesnigrum L. variant Eva, blueberry (Vaccinium myrtilis variant Berkeley, elderberry(Sambucus nigra L. variant Sambo, hawthorn (Crataegus oxyacantha, mulberry(Morus nigra L. genotypes M152 and M047 are natural sources of anthocyanpigments and vitamin C with a high antiradical activity. Due to the fact that thehighest antiradical activity is not accompanied by the highest content of anthocyansand vitamin C in puny fruits, we suppose that the antiradical activity of plantmaterials is also connected with the presence of other compounds with antioxidantand antiradical activity. From our results follows that all studied puny fruits with ahigh antiradical activity increase the antioxidant value of human nutrition and alsoits prophylactic and medicinal effect.

  14. Search for biological activities from an invasive shrub species rose myrtle (Rhodomyrtus tomentosa

    Directory of Open Access Journals (Sweden)

    IRAWAN WIJAYA KUSUMA

    2016-01-01

    Full Text Available Abstract. Kusuma IW, Ainiyati N, Suwinarti W. 2016. Search for biological activities from an invasive shrub species rose myrtle (Rhodomyrtus tomentosa. Nusantara Bioscience 8: 55-59. Research into the potential of diversity, ethnobotany and ethnopharmacology and bioactivity of Indonesia plants is essential. In continuation of our search into biologically-active substances from plant sources, the ethanol extract of fruit, leaves, twig and stem of masisin or rose myrtle (Rhodomyrtus tomentosa were evaluated for their antioxidant and antimicrobial properties and toxicity. Antioxidant property was evaluated by DPPH free radical scavenging activity. Antimicrobial activity was examined by agar well diffusion against Salmonella typhi, Bacillus cereus, Propionibacterium acnes and Candida albicans. Toxicity of the plant was determined by brine shrimp lethality test. The plant ethanolic extracts showed the occurrences of flavonoid, triterpenoid and carbohydrate in the phytochemical analysis. In the antioxidant assay, the plant extracts exhibited 90-93% of DPPH radical scavenging activity at 50 ppm. Ascorbic acid, a standard compound showed 96-98% activity at the same concentration tested. In the antimicrobial assay, the activities against B. cereus and C. albicans were displayed by the fruit and leaves of R. tomentosa with activity index (AI of 0.42 and 0.35, respectively. Leaves, stem, twig and fruit of the plant showed activity against S. typhi and P. acnes with AI of 0.19-0.50 in comparison to that of reference compound, chloramphenicol. In the brine shrimp lethality test, leaves and fruit showed cytotoxicity with LD50 of 43.4 and 8.5 μg/mL. The stem and twig ethanolic extracts were shown to be cytotoxic inactive. The present results showed potential of R. tomentosa extracts as natural antioxidant, antimicrobial and cytotoxic agents.

  15. Antimicrobial activity, synergism and inhibition of germ tube formation by Crocus sativus-derived compounds against Candida spp.

    Science.gov (United States)

    Carradori, Simone; Chimenti, Paola; Fazzari, Marina; Granese, Arianna; Angiolella, Letizia

    2016-01-01

    The limited arsenal of synthetic antifungal agents and the emergence of resistant Candida strains have prompted the researchers towards the investigation of naturally occurring compounds or their semisynthetic derivatives in order to propose new innovative hit compounds or new antifungal combinations endowed with reduced toxicity. We explored the anti-Candida effects, for the first time, of two bioactive compounds from Crocus sativus stigmas, namely crocin 1 and safranal, and some semisynthetic derivatives of safranal obtaining promising biological results in terms of minimum inhibitory concentration/minimum fungicidal concentration (MIC/MFC) values, synergism and reduction in the germ tube formation. Safranal and its thiosemicarbazone derivative 5 were shown to display good activity against Candida spp.

  16. Synthesis, Dimeric Crystal Structure, and Biological Activities of N-(4-Methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-N-(2-trifluoromethyl-phenyl)-guanidine

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The title compound, N-(4-methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl)-N′-(2-trifluoromethyl-phenyl)-guanidine, was synthesized and its structure was confirmed by using IR, MS, 1H NMR, and elemental analysis. The single crystal structure of the title compound was determined by X-ray diffraction. The preliminary biological test showed that the synthesized compound has a weak herbicidal activity.

  17. Phenolic Compounds from the Flowers of Bombax malabaricum and Their Antioxidant and Antiviral Activities

    Directory of Open Access Journals (Sweden)

    Yu-Bo Zhang

    2015-11-01

    Full Text Available Three new phenolic compounds 1–3 and twenty known ones 4–23 were isolated from the flowers of Bombax malabaricum. Their chemical structures were elucidated by spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, 1D- and 2D-NMR and chemical reactions. The antioxidant capacities of the isolated compounds were tested using FRAP and DPPH radical-scavenging assays, and compounds 4, 6, 8, 12, as well as the new compound 2, exhibited stronger antioxidant activities than ascorbic acid. Furthermore, all of compounds were tested for their antiviral activities against RSV by the CPE reduction assay and plaque reduction assay. Compounds 4, 10, 12 possess in vitro antiviral activities, and compound 10 exhibits potent anti-RSV effects, comparable to the positive control ribavirin.

  18. Antiproliferative Pt(IV) complexes: synthesis, biological activity, and quantitative structure-activity relationship modeling.

    Science.gov (United States)

    Gramatica, Paola; Papa, Ester; Luini, Mara; Monti, Elena; Gariboldi, Marzia B; Ravera, Mauro; Gabano, Elisabetta; Gaviglio, Luca; Osella, Domenico

    2010-09-01

    Several Pt(IV) complexes of the general formula [Pt(L)2(L')2(L'')2] [axial ligands L are Cl-, RCOO-, or OH-; equatorial ligands L' are two am(m)ine or one diamine; and equatorial ligands L'' are Cl- or glycolato] were rationally designed and synthesized in the attempt to develop a predictive quantitative structure-activity relationship (QSAR) model. Numerous theoretical molecular descriptors were used alongside physicochemical data (i.e., reduction peak potential, Ep, and partition coefficient, log Po/w) to obtain a validated QSAR between in vitro cytotoxicity (half maximal inhibitory concentrations, IC50, on A2780 ovarian and HCT116 colon carcinoma cell lines) and some features of Pt(IV) complexes. In the resulting best models, a lipophilic descriptor (log Po/w or the number of secondary sp3 carbon atoms) plus an electronic descriptor (Ep, the number of oxygen atoms, or the topological polar surface area expressed as the N,O polar contribution) is necessary for modeling, supporting the general finding that the biological behavior of Pt(IV) complexes can be rationalized on the basis of their cellular uptake, the Pt(IV)-->Pt(II) reduction, and the structure of the corresponding Pt(II) metabolites. Novel compounds were synthesized on the basis of their predicted cytotoxicity in the preliminary QSAR model, and were experimentally tested. A final QSAR model, based solely on theoretical molecular descriptors to ensure its general applicability, is proposed.

  19. Synthesis and Biological Activity of 4,5-Dihydro-1,2,4-triazole-5-thione Schiff Base

    Institute of Scientific and Technical Information of China (English)

    SUN, Xiaohong; BAI, Yan; LIU, Yuanfa; CHEN, Bang; JIA, Yingqi; ZENG, Zhenfang

    2009-01-01

    The 4,5-dihydro-1,2,4-triazole Schiff base derivatives were synthesized with 4-amino-4,5-dihydro-3-(phenoxy- methyl)-1H-1,2,4-triazole-5-thione and substituted benzaidehydes. The chemical structures of the compounds have been confirmed by 1H NMR, IR spectra and elemental analysis. Their biological activities were investigated, and the results showed that they exhibited good fungicidal activities.

  20. Rare Gases Inserted into Biological Building Blocks: A Theoretical Study of Glycine - Rg Compounds (Rg-Xe, Kr, Ar)

    Science.gov (United States)

    Chaban, Galina M.

    2005-01-01

    Compounds formed by insertion of rare-gas atoms (Xe, Kr, and Ar) into glycine molecule are investigated using accurate ab initio computational methods. Identification of such insertion compounds may open new frontiers in the field of rare-gas chemistry, such as possible existence of biological molecules that include chemically bound rare gas atoms. The most stable glycine-Rg configuration is found to correspond to insertion of Rg atoms into the 0-H bond of glycine. These NH2CH2COORgH compounds are metastable , but separated by sizable potential barriers from the Rg + glycine dissociation products. Preliminary calculations show that NH2CH2COOXeH compound is energetically stable with respect to another (3-body) dissociation channel (NH2CH2COO + Rg + H), while the corresponding Ar species is not stable in this respect. The compound with the inserted Kr is a borderline case, with the 3-body dissociation products being close in energy to the NH2CH2COOKrH minimum.

  1. Biological activity of two red algae, Gracilaria salicornia and Hypnea flagelliformis from Persian Gulf.

    Directory of Open Access Journals (Sweden)

    S Saeidnia

    2009-01-01

    Full Text Available Among marine organisms, algae are a large and diverse group of organisms from which a wide range of secondary metabolites have been isolated. A number of these compounds possess biological activity. In this study, we aim to evaluate the cytotoxic, antibacterial and antifungal activity of two red algae, Gracilaria salicornia and Hypnea flagelliformis, collected from Persian Gulf. Ethyl acetate extracts of both algae showed a potent cytotoxic effect against Artemia salina nauplii (LC50 = 3 and 4 μg.ml−1, respectively. Aqueous methanol (50% extracts were also effective. None of the methanol and aqueous methanol extracts of the algae showed antifungal and antibacterial activity against Staphylococcus aureus, Escherichia coli, Candida albicans and Aspergillus niger by the Broth-dilution method. Only the ethyl acetate extracts exhibited antibacterial activity (MIC = 2 μg.ml−1 on S. aureus. In conclusion, G. salicornia and H. flagelliformis could be a promising source of cytotoxic components.

  2. Biological activity of selected plants with adaptogenic effect

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2016-05-01

    Full Text Available The aim of this study was to determine biological activity of plants with adaptogenic effect: Panax ginseng Mayer., Withania somnifera L., Eleuterococcus senticosus Rupr. et Maxim., Astragallus membranaceus Fisch. and Codonopsis pilosulae Franch. The antioxidant activity was detected by DPPH and phosphomolybdenum method, total polyphenol content with Folin – Ciocalteu reagent, flavonoids content by aluminium chloride method. The detection of antimicrobial activity was carried out by disc diffusion method against three species of Gram-negative bacteria: Escherichia coli CCM 3988, Salmonella enterica subsp. enterica CCM 3807, Yersinia enterocolitica CCM 5671 and two Gram-positive bacteria: Bacillus thuringiensis CCM 19, Stapylococcus aureus subsp. aureus CCM 2461. Results showed that plants with adaptogenic effect are rich for biologically active substances. The highest antioxidant activity by DPPH method was determined in the sample of Eleuterococcus senticosus (3.15 mg TEAC – Trolox equivalent antioxidant capacity per g of sample and by phosphomolybdenum method in the sample of Codonopsis pilosulae (188.79 mg TEAC per g of sample. In the sample of Panax ginseng was measured the highest content of total polyphenols (8.10 mg GAE – galic acid equivalent per g of sample and flavonoids (3.41 μg QE – quercetin equivalent per g of sample. All samples also showed strong antimicrobial activity with the best results in Panax ginseng and Withania somnifera in particular for species Yersinia enterocolitica CCM 5671 and Salmonella enterica subsp. enterica CCM 3807. The analyzed species of plant with high value of biological activity can be used more in the future, not only in food, but also in cosmetics and pharmaceutical industries.

  3. Marine Sponge Lectins: Actual Status on Properties and Biological Activities

    Directory of Open Access Journals (Sweden)

    Sandro Mascena Gomes Filho

    2014-12-01

    Full Text Available Marine sponges are primitive metazoans that produce a wide variety of molecules that protect them against predators. In studies that search for bioactive molecules, these marine invertebrates stand out as promising sources of new biologically-active molecules, many of which are still unknown or little studied; thus being an unexplored biotechnological resource of high added value. Among these molecules, lectins are proteins that reversibly bind to carbohydrates without modifying them. In this review, various structural features and biological activities of lectins derived from marine sponges so far described in the scientific literature are discussed. From the results found in the literature, it could be concluded that lectins derived from marine sponges are structurally diverse proteins with great potential for application in the production of biopharmaceuticals, especially as antibacterial and antitumor agents.

  4. MILK KEFIR: COMPOSITION, MICROBIAL CULTURES, BIOLOGICAL ACTIVITIES AND RELATED PRODUCTS

    Directory of Open Access Journals (Sweden)

    Maria Rosa Prado

    2015-10-01

    Full Text Available In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir’s exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir’s microflora and the importance of kefiran as a beneficial health substance.

  5. Marine Omega-3 Phospholipids: Metabolism and Biological Activities

    Directory of Open Access Journals (Sweden)

    Nils Hoem

    2012-11-01

    Full Text Available The biological activities of omega-3 fatty acids (n-3 FAs have been under extensive study for several decades. However, not much attention has been paid to differences of dietary forms, such as triglycerides (TGs versus ethyl esters or phospholipids (PLs. New innovative marine raw materials, like krill and fish by-products, present n-3 FAs mainly in the PL form. With their increasing availability, new evidence has emerged on n-3 PL biological activities and differences to n-3 TGs. In this review, we describe the recently discovered nutritional properties of n-3 PLs on different parameters of metabolic syndrome and highlight their different metabolic bioavailability in comparison to other dietary forms of n-3 FAs.

  6. Fucoidans from brown alga Fucus evanescens: structure and biological activity

    Directory of Open Access Journals (Sweden)

    Roza Menshova

    2016-08-01

    Full Text Available Brown alga Fucus evanescens, widespread in the Far Eastern seas of Russia, is valuable source of sulfated polysaccharides – fucoidans with beneficial biological activities. The most homogenous fraction of fucoidan from F. evanescens was shown to be molecule containing linear main chain of alternating 2-sulfated 1,3- and 1,4-linked α-L-fucose residues. Few sulfate groups were found in position 4 of some 1,3-linked fucose residues. Acetyl groups occupied free C-3 of 1,4-linked residues and/or the C-4 of 1,3-linked fucose residues. Enzymatic hydrolysis, mild acid hydrolysis and autohydrolysis of native fucoidan were used for elucidation of the fine structural characteristics of fucoidan from F. evanescens. The aim of this review to summarize published data on biological activities of fucoidan from F. evanescens: antiviral, anticoagulant, thrombolytic, hepatoprotective, immunomodulatory, anticancer, and their practical application.

  7. A facile synthesis of arylazonicotinates for dyeing polyester fabrics under microwave irradiation and their biological activity profiles.

    Science.gov (United States)

    Al-Mousawi, Saleh M; El-Apasery, Morsy A; Mahmoud, Huda M

    2012-09-27

    A as textile dyes and the fastness properties of the dyed samples were measured. Most of the dyed fabrics tested displayed very good washing and perspiration fastness and series of 2-hydroxy- and 2-amino-6-substituted-5-arylazonicotinate monoazo compounds 7a-e and 9a-c were prepared via condensation of 3-oxo-3-substituted-2-arylhydrazonals 2a-e with active methylene nitriles 3a-d using microwave irradiation as an energy source. These substances were then tested moderate light fastness. Finally, the biological activity of the synthesized compounds against gram positive bacteria, gram negative bacteria and yeast were evaluated.

  8. A Facile Synthesis of Arylazonicotinates for Dyeing Polyester Fabrics under Microwave Irradiation and Their Biological Activity Profiles

    Directory of Open Access Journals (Sweden)

    Saleh M. Al-Mousawi

    2012-09-01

    Full Text Available A as textile dyes and the fastness properties of the dyed samples were measured. Most of the dyed fabrics tested displayed very good washing and perspiration fastness and series of 2-hydroxy- and 2-amino-6-substituted-5-arylazonicotinate monoazo compounds 7a–e and 9a–c were prepared via condensation of 3-oxo-3-substituted-2-arylhydrazonals 2a–e with active methylene nitriles 3a–d using microwave irradiation as an energy source. These substances were then tested moderate light fastness. Finally, the biological activity of the synthesized compounds against Gram positive bacteria, Gram negative bacteria and yeast were evaluated.

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

    Science.gov (United States)

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

    2017-02-01

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

  10. Protein folding activity and the central dogma of molecular biology

    OpenAIRE

    Pallavi, Ghosh; Dipankar, Chatterji

    2003-01-01

    Biological systems, in general, can function effectively when the products of the system are in proper configuration and harmful effects due to misaggregation are avoided. Folding of proteins and their functional consequences have been a subject of active research since several years now. However it is not clear whether during protein synthesis from genetic message, the same set of rules are employed or participation of new efforts take place. In this review we show that at least in the case ...

  11. Chemistry and Biological Activities of Flavonoids: An Overview

    OpenAIRE

    Shashank Kumar; Pandey, Abhay K

    2013-01-01

    There has been increasing interest in the research on flavonoids from plant sources because of their versatile health benefits reported in various epidemiological studies. Since flavonoids are directly associated with human dietary ingredients and health, there is need to evaluate structure and function relationship. The bioavailability, metabolism, and biological activity of flavonoids depend upon the configuration, total number of hydroxyl groups, and substitution of functional groups about...

  12. Current status of pyrazole and its biological activities.

    Science.gov (United States)

    Naim, Mohd Javed; Alam, Ozair; Nawaz, Farah; Alam, Md Jahangir; Alam, Perwaiz

    2016-01-01

    Pyrazole are potent medicinal scaffolds and exhibit a full spectrum of biological activities. This review throws light on the detailed synthetic approaches which have been applied for the synthesis of pyrazole. This has been followed by an in depth analysis of the pyrazole with respect to their medical significance. This follow-up may help the medicinal chemists to generate new leads possessing pyrazole nucleus with high efficacy.

  13. Biological Activities and Phytochemicals of Swietenia macrophylla King

    Directory of Open Access Journals (Sweden)

    Habsah Abdul Kadir

    2013-08-01

    Full Text Available Swietenia macrophylla King (Meliaceae is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.

  14. Synthesis, characterisation, stereochemistry and biological activity of N-formylpiperidin-4-ones

    Science.gov (United States)

    Sakthivel, P.; Ponnuswamy, S.

    2014-09-01

    A new series of N-formyl-2,6-bis(4-methoxyphenyl)piperidin-4-ones 5-8 has been synthesized and characterised using IR, mass and 1H, 13C, DEPT and 2D (COSY and HSQC) NMR spectral techniques. The NMR spectral data indicated that the N-formylpiperidin-4-ones 5-8 prefer to exist in a conformational equilibrium between a syn rotamer with a twist boat conformation (TB1) and an anti rotamer with a twist boat conformation (TB2) in solution. The stereodynamics of these systems have been studied by recording the dynamic 1H NMR spectra of compound 5, and the energy barrier for the N-CO rotation was determined to be 64.3 kJ/mol. All of the synthesized compounds (5-8) were screened for their biological activity.

  15. Study on Synthesis and Biological Activities of Novel Water-Soluble Metalloporphyrins

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    The synthesis and characterization of a series of metal porphyrins, M11(Por), {Por = dianionic of 5, 10, 15, 20-tetrakis [4- (4'-bromobutyloxy) phenyl ] porphyrinato and 5, 10, 15, 20-tetrakis [ 4- (4'-butyIoxypyridine bromide)phenyl] porphyrinato, M = Zn, Cu, Mn, Co, Ni, Ru-CO} were described. The complexes 3a-3e were prepared from the reactions of compound 2 with metal acetates in chloroform, and the treatment of 3a-3f with excess of pyridine gave corresponding complexes 4a-4f. These new compounds were identified by absorption spectroscopies, 1H-NMR and elemental analyses. The results of biological activity testing for 4a-4f revealed that 4a and 4c had stronger inhibiting action on the growth metabolism of Esche richia coli.

  16. Expression of biologically active murine interleukin-18 in Lactococcus lactis.

    Science.gov (United States)

    Feizollahzadeh, Sadegh; Khanahmad, Hossein; Rahimmanesh, Ilnaz; Ganjalikhani-Hakemi, Mazdak; Andalib, Alireza; Sanei, Mohammad Hossein; Rezaei, Abbas

    2016-11-01

    The food-grade bacterium Lactococcus lactis is increasingly used for heterologous protein expression in therapeutic and industrial applications. The ability of L. lactis to secrete biologically active cytokines may be used for the generation of therapeutic cytokines. Interleukin (IL)-18 enhances the immune response, especially on mucosal surfaces, emphasizing its therapeutic potential. However, it is produced as an inactive precursor and has to be enzymatically cleaved for maturation. We genetically manipulated L. lactis to secrete murine IL-18. The mature murine IL-18 gene was inserted downstream of a nisin promoter in pNZ8149 plasmid and the construct was used to transform L. lactis NZ3900. The transformants were selected on Elliker agar and confirmed by restriction enzyme digestion and sequencing. The expression and secretion of IL-18 protein was verified by SDS-PAGE, western blotting and ELISA. The biological activity of recombinant IL-18 was determined by its ability to induce interferon (IFN)-γ production in L. lactis co-cultured with murine splenic T cells. The amounts of IL-18 in bacterial lysates and supernatants were 3-4 μg mL(-1) and 0.6-0.7 ng mL(-1), respectively. The successfully generated L. lactis strain that expressed biologically active murine IL-18 can be used to evaluate the possible therapeutic effects of IL-18 on mucosal surfaces.

  17. Isolation of biologically active nanomaterial (inclusion bodies from bacterial cells

    Directory of Open Access Journals (Sweden)

    Peternel Špela

    2010-09-01

    Full Text Available Abstract Background In recent years bacterial inclusion bodies (IBs were recognised as highly pure deposits of active proteins inside bacterial cells. Such active nanoparticles are very interesting for further downstream protein isolation, as well as for many other applications in nanomedicine, cosmetic, chemical and pharmaceutical industry. To prepare large quantities of a high quality product, the whole bioprocess has to be optimised. This includes not only the cultivation of the bacterial culture, but also the isolation step itself, which can be of critical importance for the production process. To determine the most appropriate method for the isolation of biologically active nanoparticles, three methods for bacterial cell disruption were analyzed. Results In this study, enzymatic lysis and two mechanical methods, high-pressure homogenization and sonication, were compared. During enzymatic lysis the enzyme lysozyme was found to attach to the surface of IBs, and it could not be removed by simple washing. As this represents an additional impurity in the engineered nanoparticles, we concluded that enzymatic lysis is not the most suitable method for IBs isolation. During sonication proteins are released (lost from the surface of IBs and thus the surface of IBs appears more porous when compared to the other two methods. We also found that the acoustic output power needed to isolate the IBs from bacterial cells actually damages proteins structures, thereby causing a reduction in biological activity. High-pressure homogenization also caused some damage to IBs, however the protein loss from the IBs was negligible. Furthermore, homogenization had no side-effects on protein biological activity. Conclusions The study shows that among the three methods tested, homogenization is the most appropriate method for the isolation of active nanoparticles from bacterial cells.

  18. In vitro activity of dicationic compounds against a North American foxhound isolate of Leishmania infantum.

    Science.gov (United States)

    Rosypal, Alexa C; Hall, James E; Bakunova, Svetlana; Patrick, Donald A; Bakunov, Stanislav; Stephens, Chad E; Kumar, Arvind; Boykin, David W; Tidwell, Richard R

    2007-04-30

    Canine leishmaniasis caused by Leishmania infantum is enzootic in the North American foxhound population. Currently available chemotherapy for canine leishmaniasis is not completely effective and relapses are common in treated dogs. Pentamidine and related aromatic diamidines possess broad spectrum antiprotozoal activity. The in vitro antileishmanial activities of 35 aromatic cationic molecules were determined, using pentamidine as the reference drug. The compounds were examined for activity against promastigotes of L. infantum isolated from a foxhound from Virginia. The compounds most active against Leishmania parasites were reversed amidines. Compound 9, a reversed amidine, exhibited the highest activity against L. infantum, with a 50% inhibitory concentration (IC(50)) of 0.0042 microM compared with 14.2 microM for pentamidine. Antileishmanial activities of nine compounds were at least 1000-fold higher relative to the reference drug. Results from this study indicate that several pentamidine-related compounds warrant further investigation as possible new agents for the treatment of canine leishmaniasis.

  19. Established and emerging biological activity markers of inflammatory bowel disease

    DEFF Research Database (Denmark)

    Nielsen, O H; Vainer, B; Madsen, S M;

    2000-01-01

    Assessment of disease activity in inflammatory bowel disease (IBD), i.e., ulcerative colitis (UC) and Crohn's disease (CD), is done using clinical parameters and various biological disease markers. Ideally, a disease marker must: be able to identify individuals at risk of a given disorder......, be disease specific, mirror the disease activity and, finally, be easily applicable for routine clinical purposes. However, no such disease markers have yet been identified for IBD. In this article, classical disease markers including erythrocyte sedimentation rate, acute phase proteins (especially...

  20. Review-An overview of Pistacia integerrima a medicinal plant species: Ethnobotany, biological activities and phytochemistry.

    Science.gov (United States)

    Bibi, Yamin; Zia, Muhammad; Qayyum, Abdul

    2015-05-01

    Pistacia integerrima with a common name crab's claw is an ethnobotanically important tree native to Asia. Traditionally plant parts particularly its galls have been utilized for treatment of cough, asthma, dysentery, liver disorders and for snake bite. Plant mainly contains alkaloids, flavonoids, tannins, saponins and sterols in different parts including leaf, stem, bark, galls and fruit. A number of terpenoids, sterols and phenolic compounds have been isolated from Pistacia integerrima extracts. Plant has many biological activities including anti-microbial, antioxidant, analgesic, cytotoxicity and phytotoxicity due to its chemical constituents. This review covers its traditional ethnomedicinal uses along with progresses in biological and phytochemical evaluation of this medicinally important plant species and aims to serve as foundation for further exploration and utilization.

  1. Biologically active cis-cinnamic acid occurs naturally in Brassica parachinensis

    Institute of Scientific and Technical Information of China (English)

    2003-01-01

    The biologically active cis-cinnamic acid (cis-CA) has been perceived as a synthetic plant growth regulator for decades. However, in the present study, we found that cis-CA actually exists as a naturally occurring compound in a Brassica plant. This natural growth- regulating substance presents in both the sunlight-irradiated leaf tissue and the non-irradiated root tissue. The concentrations of cis-CA in both tissues are comparable to the biologically effective levels of those major plant hormones. The presence of cis-CA in root tissue suggests that it may be produced through both light-dependent and -independent path- ways or it can be transported from a plant organ to another.

  2. The Biological Diversity and Production of Volatile Organic Compounds by Stem-Inhabiting Endophytic Fungi of Ecuador

    Directory of Open Access Journals (Sweden)

    Susan M. Rundell

    2015-12-01

    Full Text Available Fungal endophytes colonize every major lineage of land plants without causing apparent harm to their hosts. Despite their production of interesting and potentially novel compounds, endophytes—particularly those inhabiting stem tissues—are still a vastly underexplored component of microbial diversity. In this study, we explored the diversity of over 1500 fungal endophyte isolates collected from three Ecuadorian ecosystems: lowland tropical forest, cloud forest, and coastal dry forest. We sought to determine whether Ecuador’s fungal endophytes are hyperdiverse, and whether that biological diversity is reflected in the endophytes’ chemical diversity. To assess this chemical diversity, we analyzed a subset of isolates for their production of volatile organic compounds (VOCs, a representative class of natural products. This study yielded a total of 1526 fungal ITS sequences comprising some 315 operational taxonomic units (OTUs, resulting in a non-asymptotic OTU accumulation curve and characterized by a Fisher’s α of 120 and a Shannon Diversity score of 7.56. These figures suggest that the Ecuadorian endophytes are hyperdiverse. Furthermore, the 113 isolates screened for VOCs produced more than 140 unique compounds. These results present a mere snapshot of the remarkable biological and chemical diversity of stem-inhabiting endophytic fungi from a single neotropical country.

  3. Biological and therapeutic effects of ortho-silicic acid and some ortho-silicic acid-releasing compounds: New perspectives for therapy

    Directory of Open Access Journals (Sweden)

    Jurkić Lela Munjas

    2013-01-01

    Full Text Available Abstract Silicon (Si is the most abundant element present in the Earth's crust besides oxygen. However, the exact biological roles of silicon remain unknown. Moreover, the ortho-silicic acid (H4SiO4, as a major form of bioavailable silicon for both humans and animals, has not been given adequate attention so far. Silicon has already been associated with bone mineralization, collagen synthesis, skin, hair and nails health atherosclerosis, Alzheimer disease, immune system enhancement, and with some other disorders or pharmacological effects. Beside the ortho-silicic acid and its stabilized formulations such as choline chloride-stabilized ortho-silicic acid and sodium or potassium silicates (e.g. M2SiO3; M= Na,K, the most important sources that release ortho-silicic acid as a bioavailable form of silicon are: colloidal silicic acid (hydrated silica gel, silica gel (amorphous silicon dioxide, and zeolites. Although all these compounds are characterized by substantial water insolubility, they release small, but significant, equilibrium concentration of ortho-silicic acid (H4SiO4 in contact with water and physiological fluids. Even though certain pharmacological effects of these compounds might be attributed to specific structural characteristics that result in profound adsorption and absorption properties, they all exhibit similar pharmacological profiles readily comparable to ortho-silicic acid effects. The most unusual ortho-silicic acid-releasing agents are certain types of zeolites, a class of aluminosilicates with well described ion(cation-exchange properties. Numerous biological activities of some types of zeolites documented so far might probably be attributable to the ortho-silicic acid-releasing property. In this review, we therefore discuss biological and potential therapeutic effects of ortho-silicic acid and ortho-silicic acid -releasing silicon compounds as its major natural sources.

  4. Molecular Descriptors Family on Structure Activity Relationships 2. Insecticidal Activity of Neonicotinoid Compounds

    Directory of Open Access Journals (Sweden)

    Sorana BOLBOACĂ

    2005-01-01

    Full Text Available The neonicotinoids are the newest major class of insecticides modeled after the basic nicotine molecule having improved insecticide activity and generally low toxicity. The insecticidal activities of neonicotinoids were previous studied using 3D and standard partial least squares regression models. The paper describes the ability of the MDF SAR methodology in prediction of insecticidal activities of neonicotinoid compounds. The best MDF SAR bi-varied model was validated on training and test sets and its ability on prediction of insecticidal activity was compared with previous reported models. Even if the MDF SAR methodology is complex and time consuming the results worth the effort because they are statistical significant better then previous reported results.

  5. Biological Degradation of Some Organic Compounds Enrolled in Paper Industry—A Pollution Prevention Approach 

    Institute of Scientific and Technical Information of China (English)

    RIFAATABDELWAHAAB

    2000-01-01

    Evaluation of the elimination and the "ultimate" biodegradation by aerobic microorganisms of some organic compounds commonly used in paper manufacturing technology was investigated.Biodegradation lines of nine orgainc compounds were determined as percentage removal of chemical oxygen demand(COD) over 7 days incubation.The results of the biodegradable,while others rank from fairly to even non-biodegradable.Significant biodegradation results were recorder for anticoating ester(95.0%),basoplast 200D(85.3%) and basoplast PR 8050(87.6%),A bleaching agent(formamidin-sulfinic acid),ukanol BAS and solidurit KM demonstrate moderate biodegradation results of 62.1%,76.2% and 69.8%,respectively,Poor biodegradation results for Hedifix M/35(12.7%),basazol orange(34.9%)and basazol brown(29.0%) were recorded,Accordingly,appropriate precaution should be taken into consideration when using these compounds for industrial applications.

  6. A new method for calculating the activity of stable compound from binary phase diagram

    Institute of Scientific and Technical Information of China (English)

    CHEN Dengfu; DONG Lingyan; BAI Chenguang; LIU Qingcai; WANG Chuanjun

    2006-01-01

    A new method to calculate the activity of a stable compound in a binary phase diagram was presented and dis cussed. According to the formula for calculating activity from the binary phase diagram, the equilibrium constant can be calculated through the mass action principle after the activities of two pure components were computed respectively. Based on that, the activity of a stable compound can be easily obtained at last. The activity of the stable compound InSb is calculated in the In-Sb binary system by using this method. The result is well consistent with another calculation value.

  7. Methanobactin: a copper binding compound having antibiotic and antioxidant activity isolated from methanotrophic bacteria

    Science.gov (United States)

    DiSpirito, Alan A.; Zahn, James A.; Graham, David W.; Kim, Hyung J.; Alterman, Michail; Larive, Cynthia

    2007-04-03

    A means and method for treating bacterial infection, providing antioxidant activity, and chelating copper using a copper binding compound produced by methanotrophic bacteria is described. The compound, known as methanobactin, is the first of a new class of antibiotics having gram-positive activity. Methanobactin has been sequenced, and its structural formula determined.

  8. Application of Genetic Programming in Predicting Infinite Dilution Activity Coefficients of Organic Compounds in Water

    Institute of Scientific and Technical Information of China (English)

    Yi Lin CAO; Huan Ying LI

    2003-01-01

    In this paper, we calculated 37 structural descriptors of 174 organic compounds. The154 molecules were used to derive quantitative structure-infinite dilution activity coefficientrelationship by genetic programming, the other 20 compounds were used to test the model. Theresult showed that molecular partition property and three-dimensional structural descriptors havesignificant influence on the infinite dilution activity coefficients.

  9. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...... includes multipoint intermolecular interactions that probably involve aggregation of both polymorphic and monomorphic T cell surface molecules. Such aggregations have been shown in vitro to markedly enhance and, in some cases, induce T cell activation. The production of T-derived lymphokines that have been...... implicated in B cell activation is dependent on the T cell receptor for antigen and its associated CD3 signalling complex. T-dependent help for B cell activation is therefore similarly MHC-restricted and involves T-B intercellular interaction. Recent reports that describe antigen-independent B cell...

  10. Biologically active traditional medicinal herbs from Balochistan, Pakistan.

    Science.gov (United States)

    Zaidi, Mudassir A; Crow, Sidney A

    2005-01-01

    The biological activities of the following four important medicinal plants of Balochistan, Pakistan were checked; Grewia erythraea Schwein f. (Tiliaceae), Hymenocrater sessilifolius Fisch. and C.A. Mey (Lamiaceae), Vincetoxicum stocksii Ali and Khatoon (Asclepiadaceae) and Zygophyllum fabago L. (Zygophyllaceae). The methanolic extracts were fractionated into hexane, ethyl acetate, chloroform, butanol and water. The antifungal and antibacterial activities of these plants were determined against 12 fungal and 12 bacterial strains by agar well diffusion and disk diffusion assays. The extract of Zygophyllum fabago was found to be highly effective against Candida albicans and Escherichia coli. The extract of Vincetoxicum stocksii was also found to be significantly active against Candida albicans, Bacillus subtilis and Bacillus cereus. Extracts of Hymenocrater sessilifolius and Grewia erythraea showed good activity only against Pseudomonas aeruginosa.

  11. [Influence of biological activated carbon dosage on landfill leachate treatment].

    Science.gov (United States)

    Cui, Yan-Rui; Guo, Yan; Wu, Qing

    2014-08-01

    Effects of biological activated carbon (BAC) dosage on COD removal in landfill leachate treatment were compared. The COD removal efficiency of reactors with 0, 100 and 300 g activated carbon dosage per litre activated sludge was 12.9%, 19.6% and 27.7%, respectively. The results indicated that BAC improved the refractory organic matter removal efficiency and there was a positive correlation between COD removal efficiency and BAC dosage. The output of carbon dioxide after 8h of aeration in reactors was 109, 193 and 306 mg corresponding to the activated carbon dosages mentioned above, which indicated the amount of biodegradation and BAC dosage also had a positive correlation. The combination of adsorption and bioregeneration of BAC resulted in the positive correlation betweem organic matter removal efficiency and BAC dosage, and bioregeneration was the root cause for the microbial decomposition of refractory organics.

  12. Biological activities of triazine derivatives. Combining DFT and QSAR results

    Directory of Open Access Journals (Sweden)

    Majdouline Larif

    2017-02-01

    Full Text Available In order to investigate the relationship between activities and structures, a 3D-QSAR study is applied to a set of 43 molecules based on triazines. This study was conducted using the principal component analysis (PCA method, the multiple linear regression method (MLR and the artificial neural network (ANN. The predicted values of activities are in good agreement with the experimental results. The artificial neural network (ANN techniques, considering the relevant descriptors obtained from the MLR, showed a correlation coefficient of 0.9 with an 8-3-1 ANN model which is a good result. As a result of quantitative structure–activity relationships, we found that the model proposed in this study is constituted of major descriptors used to describe these molecules. The obtained results suggested that the proposed combination of several calculated parameters could be useful to predict the biological activity of triazine derivatives.

  13. Isolation and Characterization of Phenolic Compounds and Anthocyanins from Murta (Ugni molinae Turcz. Fruits. Assessment of Antioxidant and Antibacterial Activity

    Directory of Open Access Journals (Sweden)

    Maria Paula Junqueira-Gonçalves

    2015-03-01

    Full Text Available Berry fruit consumption has become important in the promotion of human health, mainly due to their phenolic compounds, which have been associated with protection against different pathologies, as well as antimicrobial and other biological activities. Consequently, there has been a growing interest in identifying natural antioxidants and antimicrobials from these plants. This study aimed to characterize the phenolic chemical composition and anthocyanin profile of murta (Ugni molinae Turcz. fruit, and to evaluate the antioxidant and antimicrobial activity of its extracts (ethanolic and methanolic. LC/MS of the ethanolic extracts showed the presence of three major compounds: caffeic acid 3-glu, quercetin-3-glu and quercetin, while in the methanolic acid extract they were cyanidin-3-glucoside, pelargonidin-3-arabinose and delphinidin-3-glucoside. The antioxidant activity of ethanolic extracts (DPPH· and ORAC assays was higher than that of methanol acid extracts or purified anthocynins. Furthermore, the methanol acid extract showed an inhibitory activity against the bacteria E. coli and S. typhi similar to that of standard antibiotics. The results suggest that the antioxidant activity of the ethanolic extract is regulated by the high content of phenolic compounds and the fruit’s characteristic color is due to the content of pelargonidin-3-arabinose and delphinidin-3-glucoside. The obtained results demonstrated the appreciable antioxidant and antibacterial activities, providing opportunities to explore murta extracts as biopreservatives.

  14. Combining activated carbon adsorption with heterogeneous photocatalytic oxidation: lack of synergy for biologically treated greywater and tetraethylene glycol dimethyl ether.

    Science.gov (United States)

    Gulyas, Holger; Argáez, Angel Santiago Oria; Kong, Fanzhuo; Jorge, Carlos Liriano; Eggers, Susanne; Otterpohl, Ralf

    2013-01-01

    The aim of the study was to evaluate whether the addition of activated carbon in the photocatalytic oxidation of biologically pretreated greywater and of a polar aliphatic compound gives synergy, as previously demonstrated with phenol. Photocatalytic oxidation kinetics were recorded with fivefold concentrated biologically pretreated greywater and with aqueous tetraethylene glycol dimethyl ether solutions using a UV lamp and the photocatalyst TiO2 P25 in the presence and the absence of powdered activated carbon. The synergy factor, SF, was quantified as the ratio of photocatalytic oxidation rate constant in the presence of powdered activated carbon to the rate constant without activated carbon. No synergy was observed for the greywater concentrate (SF approximately 1). For the aliphatic compound, tetraethylene glycol dimethyl ether, addition of activated carbon actually had an inhibiting effect on photocatalysis (SF photocatalytic oxidation of tetraethylene glycol dimethyl ether by addition of powdered activated carbon was attributed to shading of the photocatalyst by the activated carbon particles. It was assumed that synergy in the hybrid process was limited to aromatic organics. Regardless of the lack of synergy in the case of biologically pretreated greywater, the addition of powdered activated carbon is advantageous since, due to additional adsorptive removal of organics, photocatalytic oxidation resulted in a 60% lower organic concentration when activated carbon was present after the same UV irradiation time.

  15. Ovicidal and adulticidal activities of Cinnamomum zeylanicum bark essential oil compounds and related compounds against Pediculus humanus capitis (Anoplura: Pediculicidae).

    Science.gov (United States)

    Yang, Young-Cheol; Lee, Hoi-Seon; Lee, Si Hyeock; Clark, J Marshall; Ahn, Young-Joon

    2005-12-01

    The toxicity of cinnamon, Cinnamomum zeylanicum, bark essential oil compounds against eggs and adult females of human head louse, Pediculus humanus capitis, was examined using direct contact and vapour phase toxicity bioassays and compared with the lethal activity of their related compounds, benzyl alcohol, cinnamic acid, cinnamyl acetate, 4-hydroxybenzaldehyde and salicylaldehyde, as well as two widely used pediculicides, d-phenothrin and pyrethrum. In a filter-paper contact toxicity bioassay with female lice at 0.25 mg/cm(2), benzaldehyde was 29- and 27-fold more toxic than pyrethrum and d-phenothrin, respectively, as judged by median lethal time (LT(50)) values. Salicylaldehyde was nine and eight times more active than pyrethrum and d-phenothrin, respectively. Pediculicidal activity of linalool was comparable with that of d-phenothrin and pyrethrum. Cinnamomum bark essential oil was slightly less effective than either d-phenothrin or pyrethrum. Benzyl alcohol and (E)-cinnamaldehyde exhibited moderate pediculicidal activity. After 24h of exposure, no hatching was observed with 0.063 mg/cm(2) salicylaldehyde, 0.125 mg/cm(2) benzaldehyde, 0.5mg/cm(2)Cinnamomum bark essential oil, 1.0 mg/cm(2) (E)-cinnamaldehyde, and 1.0 mg/cm(2) benzyl cinnamate. Little or no ovicidal activity was observed with d-phenothrin or pyrethrum. In vapour phase toxicity tests with female lice, benzaldehyde and salicylaldehyde were much more effective in closed containers than in open ones, indicating that the mode of delivery of these compounds was largely due to action in the vapour phase. Neither d-phenothrin nor pyrethrum exhibited fumigant toxicity. Cinnamomum bark essential oil and test compounds described merit further study as potential pediculicides or ovicides for the control of P. h. capitis.

  16. Phenolic compounds and antioxidant activity of hydroalcoholic extracts of wild and cultivated murtilla (Ugni molinae Turcz.

    Directory of Open Access Journals (Sweden)

    Thalita Riquelme Augusto

    2014-12-01

    Full Text Available Over the last decade a considerable increase in the number of studies addressing the use of antioxidants from natural sources has led to the identification and understanding of the potential mechanisms of biologically active components. This results from the fact that they can be used to replace synthetic antioxidants commonly used in food. Murtilla (Ugni molinae Turcz is a native berry grown in Chile, and in the present study, the phenolic composition and antioxidant activity of its fruits were studied. Hydroalcoholic extracts of dehydrated fruits from two genotypes of murtilla (Ugni molinae Turcz. were produced. Extracts of wild murtilla and 14-4 genotype fruits had 19.35 and 40.28mg GAE/g for Total Phenolic Compounds, 76.48, and 134.35μmol TEAC/g for DPPH, and 157.04 and 293.99 μmol TEAC/g for ABTS, respectively. Components such as quercetin, epicatechin, and gallic, benzoic and hydrocaffeic acids were identified by CG/MS analysis. All of them showed antioxidant activity. Therefore, it is possible to say that the hydroalcoholic extracts of murtilla have antioxidant potential to be used in lipidic food.

  17. Anti-inflammatory and anticancer activities of extracts and compounds from the mushroom Inonotus obliquus.

    Science.gov (United States)

    Ma, Lishuai; Chen, Haixia; Dong, Peng; Lu, Xueming

    2013-08-15

    Mushroom Inonotus obliquus (I. obliquus) has been used as functional food and traditional Chinese herbs for long time. An efficient method for bioassay-guided preparative isolation was used for identifying the anti-inflammatory and anticancer constituents in I. obliquus. The petroleum ether and ethyl acetate fractions were found to have significant inhibition effects on NO production and NF-κB luciferase activity in macrophage RAW 264.7 cells and cytotoxicity against human prostatic carcinoma cell PC3 and breast carcinoma cell MDA-MB-231. Six main constituents were isolated from these two fractions and they were identified as lanosterol (1), 3β-hydroxy-8,24-dien-21-al (2), ergosterol (3), inotodiol (4), ergosterol peroxide (5) and trametenolic acid (6). Compound ergosterol, ergosterol peroxide and trametenolic acid showed anti-inflammatory activities and ergosterol peroxide and trametenolic acid showed obviously cytotoxicity on human prostatic carcinoma cell PC3 and breast carcinoma MDA-MB-231 cell. The results obtained in this work might contribute to understanding the biological activity of mushroom I. obliquus for food and drug application.

  18. Nematicidal activity of natural ester compounds and their analogues against pine wood nematode, Bursaphelenchus xylophilus.

    Science.gov (United States)

    Seo, Seon-Mi; Kim, Junheon; Koh, Sang-Hyun; Ahn, Young-Joon; Park, Il-Kwon

    2014-09-17

    In this study, we evaluated the nematicidal activity of natural ester compounds against the pine wood nematode, Bursaphelenchus xylophilus, to identify candidates for the development of novel, safe nematicides. We also tested the nematicidal activity of synthesized analogues of these ester compounds to determine the structure-activity relationship. Among 28 ester compounds tested, isobutyl 2-methylbutanoate, 3-methylbutyl 2-methylbutanoate, 3-methylbutyl tiglate, 3-methyl-2-butenyl 2-methylbutanoate, and pentyl 2-methylbutanoate showed strong nematicidal activity against the pine wood nematode at a 1 mg/mL concentration. The other ester compounds showed weak nematicidal activity. The LC50 values of 3-methylbutyl tiglate, isobutyl 2-methylbutanoate, 3-methylbutyl 2-methylbutanoate, 3-methyl-2-butenyl 2-methylbutanoate, and pentyl 2-methylbutanoate were 0.0218, 0.0284, 0.0326, 0.0402, and 0.0480 mg/mL, respectively. The ester compounds described herein merit further study as potential nematicides for pine wood nematode control.

  19. The removal of endocrine disrupting compounds, pharmaceutically activated compounds and cyanobacterial toxins during drinking water preparation using activated carbon--a review.

    Science.gov (United States)

    Delgado, Luis F; Charles, Philippe; Glucina, Karl; Morlay, Catherine

    2012-10-01

    This paper provides a review of recent scientific research on the removal by activated carbon (AC) in drinking water (DW) treatment of 1) two classes of currently unregulated trace level contaminants with potential chronic toxicity-pharmaceutically activate compounds (PhACs) and endocrine disrupting compounds (EDCs); 2) cyanobacterial toxins (CyBTs), which are a group of highly toxic and regulated compounds (as microcystin-LR); and 3) the above mentioned compounds by the hybrid system powdered AC/membrane filtration. The influence of solute and AC properties, as well as the competitive effect from background natural organic matter on the adsorption of such trace contaminants, are also considered. In addition, a number of adsorption isotherm parameters reported for PhACs, EDCs and CyBTs are presented herein. AC adsorption has proven to be an effective removal process for such trace contaminants without generating transformation products. This process appears to be a crucial step in order to minimize PhACs, EDCs and CyBTs in finished DW, hence calling for further studies on AC adsorption removal of these compounds. Finally, a priority chart of PhACs and EDCs warranting further study for the removal by AC adsorption is proposed based on the compounds' structural characteristics and their low removal by AC compared to the other compounds.

  20. Chemical composition and biological activity of ripe pumpkin fruits (Cucurbita pepo L.) cultivated in Egyptian habitats.

    Science.gov (United States)

    Badr, Sherif E A; Shaaban, Mohamed; Elkholy, Yehya M; Helal, Maher H; Hamza, Akila S; Masoud, Mohamed S; El Safty, Mounir M

    2011-09-01

    The chemical composition and biological activity of three parts (rind, flesh and seeds) of pumpkin fruits (Cucurbita pepo L.) cultivated in Egypt were studied. Chemical analysis of fibre, protein, β-carotene, carbohydrates, minerals and fatty acids present in the rind, flesh, seeds and defatted seeds meal was conducted. Chemical, GC-MS and biological assays of organic extracts of the main fruit parts, rind and flesh established their unique constituents. Chromatographic purification of the extracts afforded triglyceride fatty acid mixture (1), tetrahydro-thiophene (2), linoleic acid (3), calotropoleanly ester (4), cholesterol (5) and 13(18)-oleanen-3-ol (6). GC-MS analysis of the extract's unpolar fraction revealed the existence of dodecane and tetradecane. Structures of the isolated compounds (1-6) were confirmed by NMR and EI-MS spectrometry. Antimicrobial, antiviral and antitumour activities of the fruit parts were discussed. The promising combined extract of rind and flesh was biologically studied for microbial and cytotoxic activities in comparison with the whole isolated components.