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Sample records for biologically active compounds

  1. Biologically active compounds from Aphyllophorales (polypore) fungi.

    PubMed

    Zjawiony, Jordan K

    2004-02-01

    This review describes biologically active natural products isolated from Aphyllophorales, many of which are known as polypores. Polypores are a large group of terrestrial fungi of the phylum Basdiomycota (basidiomycetes), and they along with certain Ascomycota are a major source of pharmacologically active substances. There are about 25 000 species of basidiomycetes, of which about 500 are members of the Aphyllophorales, a polyphyletic group that contains the polypores. Many of these fungi have circumboreal distributions in North America, Europe, and Asia and broad distributions on all inhabited continents and Africa; only a small number of the most common species with the most obvious fruiting bodies (basidiocarps) have been evaluated for biological activity. An estimated 75% of polypore fungi that have been tested show strong antimicrobial activity, and these may constitute a good source for developing new antibiotics. Numerous compounds from these fungi also display antiviral, cytotoxic, and/or antineoplastic activities. Additional important components of this vast arsenal of compounds are polysaccharides derived from the fungal cell walls. These compounds have attracted significant attention in recent years because of their immunomodulatory activities, resulting in antitumor effects. These high molecular weight compounds, often called biological response modifiers (BRM), or immunopotentiators, prevent carcinogenesis, show direct anticancer effects, and prevent tumor metastasis. Some of the protein-bound polysaccharides from polypores and other basidiomycetes have found their way to the market in Japan as anticancer drugs. Finally, numerous compounds with cardiovascular, phytotoxic, immunomodulatory, analgesic, antidiabetic, antioxidant, insecticidal, and nematocidal activities, isolated from polypores, are also presented. In fact many of the fungi mentioned in this paper have long been used in herbal medicine, including polypores such as Ganoderma lucidum

  2. Biological activity of acetylated phenolic compounds.

    PubMed

    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.

  3. Recently reported biological activities of pyrazole compounds.

    PubMed

    Faria, Jéssica Venância; Vegi, Percilene Fazolin; Miguita, Ana Gabriella Carvalho; Dos Santos, Maurício Silva; Boechat, Nubia; Bernardino, Alice Maria Rolim

    2017-09-23

    The pyrazole nucleus is an aromatic azole heterocycle with two adjacent nitrogen atoms. Pyrazole derivatives have exhibited a broad spectrum of biological activities, and approved pyrazole-containing drugs include celecoxib, antipyrine, phenylbutazone, rimonabant, and dipyrone. Many research groups have synthesized and evaluated pyrazoles against several biological agents. This review examines recent publications relating the structures of pyrazoles with their corresponding biological activities. Copyright © 2017. Published by Elsevier Ltd.

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

    PubMed

    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.

  5. Biological activities of phenolic compounds present in virgin olive oil.

    PubMed

    Cicerale, Sara; Lucas, Lisa; Keast, Russell

    2010-02-02

    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 traditional Mediterranean diet. Studies (human, animal, in vivo and in vitro) have demonstrated that olive oil phenolic compounds have positive effects on certain physiological parameters, such as plasma lipoproteins, oxidative damage, inflammatory markers, platelet and cellular function, antimicrobial activity and bone health. This paper summarizes current knowledge on the bioavailability and biological activities of olive oil phenolic compounds.

  6. Natural products as a resource for biologically active compounds

    SciTech Connect

    Hanke, F.J.

    1986-01-01

    The goal of this study was to investigate various sources of biologically active natural products in an effort to identify the active pesticidal compounds involved. The study is divided into several parts. Chapter 1 contains a discussion of several new compounds from plant and animal sources. Chapter 2 introduces a new NMR technique. In section 2.1 a new technique for better utilizing the lanthanide relaxation agent Gd(fod)/sub 3/ is presented which allows the predictable removal of resonances without line broadening. Section 2.2 discusses a variation of this technique for use in an aqueous solvent by applying this technique towards identifying the binding sites of metals of biological interest. Section 2.3 presents an unambiguous /sup 13/C NMR assignment of melibiose. Chapter 3 deals with work relating to the molting hormone of most arthropods, 20-hydroxyecdysone. Section 3.1 discusses the use of two-dimensional NMR (2D NMR) to assign the /sup 1/H NMR spectrum of this biologically important compound. Section 3.2 presents a new application for Droplet countercurrent chromatography (DCCC). Chapter 4 presents a basic improvement to the commercial DCCC instrument that is currently being applied to future commercial instruments. Chapter 5 discusses a curious observation of the effects that two previously known compounds, nagilactone C and (-)-epicatechin, have on lettuce and rice and suggest a possible new role for the ubiquitous flavanol (-)-epicatechin in plants.

  7. Polymer application for separation/filtration of biological active compounds

    NASA Astrophysics Data System (ADS)

    Tylkowski, B.; Tsibranska, I.

    2017-06-01

    Membrane technology is an important part of the engineer's toolbox. This is especially true for industries that process food and other products with their primary source from nature. This review is focused on ongoing development work using membrane technologies for concentration and separation of biologically active compounds, such as polyphenols and flavonoids. We provide the readers not only with the last results achieve in this field but also, we deliver detailed information about the membrane types and polymers used for their preparation.

  8. Isolation and biological activity of compounds from Garcinia preussii.

    PubMed

    Biloa Messi, Bernadette; Ho, Raimana; Meli Lannang, Alain; Cressend, Delphine; Perron, Karl; Nkengfack, Augustin Ephrem; Carrupt, Pierre-Alain; Hostettmann, Kurt; Cuendet, Muriel

    2014-06-01

    Plants of the genus Garcinia (Clusiaceae) are traditionally used to relieve stomachaches, toothaches, and as a chew stick. In order to determine which compounds were responsible for these activities, a phytochemical investigation of the fruits and leaves of Garcinia preussii Engl. was pursued. Plants were extracted by solvents of various polarities. Compounds isolation was then carried out using chromatography methods (medium- and high-pressure liquid chromatography, open column and thin-layer chromatography). The isolated compounds were identified and characterized by using 1D and 2D NMR spectroscopies. The antioxidant activity was evaluated using DPPH(•), ABTS(•-), ALP, and ORAC assays. The antimicrobial activity was assayed against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Enterococcus faecalis by determining the minimum inhibitory concentration (MIC) value. The cytotoxic activity of most of the isolated compounds was evaluated on a small panel of human cancer cell lines (DU145, HeLa, HT-29, and A431) using the XTT method. The phytochemical investigation of G. preussii led to the isolation of eight known compounds, six benzophenones and two flavonoids. These compounds were tested for their biological activities. 1, 2, 3, 4, 7 and 8 demonstrated a high free radical scavenging activity with ER50 ranging from 0.1 to 0.7. The antimicrobial activity was shown only against Gram-positive bacteria for 1, 4, and 5. A moderate cytotoxic activity with IC50 ranging from 7 to 50 µM was observed, except for 6 which was not active. These results appear to support some of the properties reported for Garcinia species.

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

    PubMed

    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

    PubMed Central

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

    2013-01-01

    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. PMID:26784660

  11. Propolis volatile compounds: chemical diversity and biological activity: a review

    PubMed Central

    2014-01-01

    Propolis is a sticky material collected by bees from plants, and used in the hive as building material and defensive substance. It has been popular as a remedy in Europe since ancient times. Nowadays, propolis use in over-the-counter preparations, “bio”-cosmetics and functional foods, etc., increases. Volatile compounds are found in low concentrations in propolis, but their aroma and significant biological activity make them important for propolis characterisation. Propolis is a plant-derived product: its chemical composition depends on the local flora at the site of collection, thus it offers a significant chemical diversity. The role of propolis volatiles in identification of its plant origin is discussed. The available data about chemical composition of propolis volatiles from different geographic regions are reviewed, demonstrating significant chemical variability. The contribution of volatiles and their constituents to the biological activities of propolis is considered. Future perspectives in research on propolis volatiles are outlined, especially in studying activities other than antimicrobial. PMID:24812573

  12. [The release of biologically active compounds from peat peloids].

    PubMed

    Babaskin, D V

    2011-01-01

    This work had the objective to study kinetics of the release of flavonoides from peat peloid compositions containing extracts of medicinal herbs in model systems.The key parameters of the process are defined. The rate of liberation of flavonoides is shown to depend on their initial concentration in the compositions being used. The influence of the flavonoide composition of the tested extracts and dimethylsulfoxide on the release of biologically active compounds contained in the starting material in the model environment is estimated. The possibility of the layer-by-layer deposition of the compositions and peat peloids in order to increase the efficacy of flavonoide release from the starting composition and to ensure more rational utilization of the extracts of medicinal plants is demonstrated.

  13. Liposomal forms of rhenium cluster compounds: enhancement of biological activity.

    PubMed

    Shtemenko, Natalia I; Zabitskaya, Elena D; Berzenina, Oksana V; Yegorova, Dina E; Shtemenko, Alexander V

    2008-08-01

    Liposomal formulations of dinuclear cluster rhenium (Re) compounds were used in biochemical trials. Interaction of liposomal forms of some Re compounds with red blood cells in experiments in vitro showed strong cell-stabilizing properties. In the models of tumor growth and hemolytic anemia in vivo, liposomal forms had better therapeutic effects in comparison with their solutions. The process of formation of liposomes of cluster Re compounds with different organic ligands was investigated by the method of electronic absorption spectra and mechanism of their interactions with lipids is proposed. Encapsulation of cluster Re compounds to lipid coating may have activation significance for the quadruple Re-Re bond.

  14. Biological activities of lignin hydrolysate-related compounds.

    PubMed

    Lee, Siseon; Monnappa, Ajay Kalanjana; Mitchell, Robert J

    2012-05-01

    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 downstream loss of product if not removed prior to beginning the fermentative process. In contrast, a search for these compounds within the literature turns up many papers where the same compounds have beneficial properties pertaining to human health, including as antioxidants and in cancer prevention, or are involved in bacterial cell-to-cell signaling. Consequently, this article reviews the dual nature of these and other compounds found in lignin hydrolysates, highlighting both their detrimental and beneficial activities.

  15. Persistence of biologically active compounds in aquatic systems: Final report

    SciTech Connect

    Boelter, A.M.; Fernandez, J.D.; Meyer, J.S.; Sanchez, D.A.; Bergman, H.L.

    1986-11-01

    Waters collected from two study sites were tested for persistence of biologically active compounds as the waters percolated through experimental media. At the first site, the Paraho Lysimeter in Anvil Points, Colorado, two leachate samples (early and late flow in Spring 1983) were collected from each of four piles of processed oil shale overlain by different thicknesses of soil. Although water quality differed among samples, six of eight lysimeter leachates tested were acutely toxic to an aquatic invertebrate, Daphnia magna, and five were acutely toxic to fathead minnows (Pimephales promelas). Water collected from a modified in situ (MIS) retort was percolated through columns containing three different types of soil. Raw leachate from the MIS spent shale was acutely toxic to an aquatic invertebrate, Ceriodaphnia dubia. The toxicity of samples from nine pore volumes of retort water percolating through a column containing a sandy soil increased with successive pore volumes, but leachate toxicity never equaled the toxicity of the retort water. In contrast, the first pore volumes of retort water or reconstituted water leached through a sandy loam soil were more toxic than the retort water; however, the second pore volumes of leachates were not toxic. First pore volume leachates of retort water percolating through a sandy clay loam soil were much less toxic than the retort water; second pore volume leachates were not toxic.

  16. A glimpse on biological activities of tellurium compounds.

    PubMed

    Cunha, Rodrigo L O R; Gouvea, Iuri E; Juliano, Luiz

    2009-09-01

    Tellurium is a rare element which has been regarded as a toxic, non-essential trace element and its biological role is not clearly established to date. Besides of that, the biological effects of elemental tellurium and some of its inorganic and organic derivatives have been studied, leading to a set of interesting and promising applications. As an example, it can be highlighted the uses of alkali-metal tellurites and tellurates in microbiology, the antioxidant effects of organotellurides and diorganoditellurides and the immunomodulatory effects of the non-toxic inorganic tellurane, named AS-101, and the plethora of its uses. Inasmuch, the nascent applications of organic telluranes (organotelluranes) as protease inhibitors and its applications in disease models are the most recent contribution to the scenario of the biological effects and applications of tellurium and its compounds discussed in this manuscript.

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

    PubMed

    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.

  18. Phenolic compounds and biological activity of Kitaibelia vitifolia.

    PubMed

    Mašković, Pavle; Solujić, Slavica; Mihailović, Vladimir; Mladenović, Milan; Cvijović, Milica; Mladenović, Jelena; Aćamović-Đoković, Gordana; Kurćubić, Vladimir

    2011-12-01

    This study was aimed at evaluating the antioxidant activity and efficacy of the ethanolic extract of the endemic plant species Kitaibelia vitifolia in inhibiting the growth of selected fungi and bacteria. Antimicrobial activity was tested using the broth dilution procedure for determination of minimum inhibitory concentration (MIC). MICs were determined for eight selected indicator strains. The highest susceptibility to K. vitifolia ethanolic extract among the bacteria tested was exhibited by Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 25923, and Klebsiella pneumoniae ATCC 13883 (MIC=15.62 μg/mL), followed by Escherichia coli ATCC 25922 and Proteus mirabilis ATCC 14153 (MIC=31.25 μg/mL), and Proteus vulgaris ATCC 13315 (MIC=62.50 μg/mL). Of the fungi, Candida albicans ATCC 10231 (MIC=15.62 μg/mL) showed the highest susceptibility, and Aspergillus niger ATCC 16404 (MIC=31.25 μg/mL) had the lowest. Results showed that K. vitifolia extract possesses antioxidant activity, with total antioxidant capacity of 75.45±0.68 μg of ascorbic acid/g and 50% inhibition concentration values of 47.45±0.55 μg/mL for 2,2-diphenyl-1-picrylhydrazyl free radical scavenging activity, 35.35±0.68 μg/mL for inhibitory activity against lipid peroxidation, 95.25±0.52 μg/mL for hydroxyl radical scavenging activity, and 31.50±0.35 μg/mL for metal chelating activity. Total phenolics, flavonoids, condensed tannins, and gallotannins were 85.25±0.69 mg of gallic acid (GA)/g, 45.32±0.55 mg of rutin/g, 54.25±0.75 mg of GA/g, and 41.74±0.55 mg of GA/g, respectively. The phenolic composition of K. vitifolia extract was determined by high-performance liquid chromatography. Rosmarinic acid was found to be the dominant phenolic compound of the extract.

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

    USDA-ARS?s Scientific Manuscript database

    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. Extraction, chemical characterization and biological activity determination of broccoli health promoting compounds.

    PubMed

    Ares, Ana M; Nozal, María J; Bernal, José

    2013-10-25

    Broccoli (Brassica oleracea L. var. Italica) contains substantial amount of health-promoting compounds such as vitamins, glucosinolates, phenolic compounds, and dietary essential minerals; thus, it benefits health beyond providing just basic nutrition, and consumption of broccoli has been increasing over the years. This review gives an overview on the extraction and separation techniques, as well as the biological activity of some of the above mentioned compounds which have been published in the period January 2008 to January 2013. The work has been distributed according to the different families of health promoting compounds discussing the extraction procedures and the analytical techniques employed for their characterization. Finally, information about the different biological activities of these compounds has been also provided. Copyright © 2013 Elsevier B.V. All rights reserved.

  1. Persistence of biologically active compounds in soil: Final report

    SciTech Connect

    Williams, S.E.

    1987-02-01

    This document describes the long-term effects of soil-applied oil shale process water on the VA fungi and Rhizobium bacteria in a native soil. Techniques include assessing the VA fungal activity at field treatment plots and using treated field soils in a bioassay to determine VA infection and Rhizobium-nodulation potentials four years after process water application. 52 refs., 32 figs., 2 tabs.

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

    PubMed

    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.

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

    PubMed

    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.

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

    EPA Science Inventory

    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...

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

    EPA Science Inventory

    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...

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

    USDA-ARS?s Scientific Manuscript database

    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...

  7. 3-Hydroxy-2-phenyl-4(1H)-quinolinones as promising biologically active compounds.

    PubMed

    Hradil, P; Hlavác, J; Soural, M; Hajdúch, M; Kolár, M; Vecerová, R

    2009-06-01

    2-Phenyl-3-hydroxy-4(1H)-quinolinones can be considered as aza-analogues of flavones, compounds which are known for the wide-range of their biological activity. These quinolinones were studied as inhibitors of topoisomerase, gyrase and IMPDH. They were tested for anticancer activity in-vitro and were also shown to possess immunosuppressive properties. This review is the first summarizing the synthesis and activity of the mentioned quinolinones.

  8. Design, Synthesis, and Biological Activities of Novel Pyrazole Oxime Compounds Containing a Substituted Pyridyl Moiety.

    PubMed

    Chen, Cuili; Chen, Jia; Gu, Haiying; Bao, Ning; Dai, Hong

    2017-05-25

    In this paper, in order to find novel biologically active pyrazole oximes, a series of pyrazole oxime compounds bearing a substituted pyridyl unit were prepared. Bioassays showed that some target compounds were found to have good acaricidal activity against Tetranychus cinnabarinus at a concentration of 500 μg/mL, compound 9q especially displayed potent acaricidal activity against T. cinnabarinus when the concentration was reduced to 100 μg/mL. Interestingly, most target compounds possessed excellent insecticidal activities against Oriental armyworm at 500 μg/mL. Moreover, some compounds were active against Aphis medicaginis and Nilaparvata lugens at 500 μg/mL. Additionally, compounds 9b, 9g, 9l, 9p, 9q, 9r, 9s, 9t, 9u, and 9v displayed significant antiproliferative activities against HepG2 cells with IC50 values of 1.53-17.27 μM, better than that of the control 5-fluorouracil (IC50 = 35.67 μM).

  9. How to acquire new biological activities in old compounds by computer prediction

    NASA Astrophysics Data System (ADS)

    Poroikov, V. V.; Filimonov, D. A.

    2002-11-01

    Due to the directed way of testing chemical compounds' in drug research and development many projects fail because serious adverse effects and toxicity are discovered too late, and many existing prospective activities remain unstudied. Evaluation of the general biological potential of molecules is possible using a computer program PASS that predicts more than 780 pharmacological effects, mechanisms of action, mutagenicity, carcinogenicity, etc. on the basis of structural formulae of compounds, with average accuracy ˜85%. PASS applications to both databases of available samples included hundreds of thousands compounds, and small collections of compounds synthesized by separate medicinal chemists are described. It is shown that 880 compounds from Prestwick chemical library represent a very diverse pharmacological space. New activities can be found in existing compounds by prediction. Therefore, on this basis, the selection of compounds with required and without unwanted properties is possible. Even when PASS cannot predict very new activities, it may recognize some unwanted actions at the early stage of R&D, providing the medicinal chemist with the means to increase the efficiency of projects.

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

    NASA Astrophysics Data System (ADS)

    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.

  11. Terpenoid bioactive compound from Streptomyces rochei (M32): taxonomy, fermentation and biological activities.

    PubMed

    Pazhanimurugan, Raasaiyah; Radhakrishnan, Manikkam; Shanmugasundaram, Thangavel; Gopikrishnan, Venugopal; Balagurunathan, Ramasamy

    2016-10-01

    The present study emphasized the production of biologically active terpenoid compound from Streptomyces rochei M32, which was isolated from Western Ghats ecosystem, South India. The presence of resistant genes like mecA, vanA of Staphylococcus aureus and bla SHV, bla TEM of Pseudomonas aeruginosa was confirmed by molecular studies. The isolated compound from Streptomyces rochei M32 inhibited wide range of standard and clinical drug resistant pathogens and enteric pathogens. The rice bran supplemented basal medium influenced the active compound production on 8th day of fermentation and yielded 1875 mg of crude extract from 10 g of rice bran substrate. Purification and characterization of crude ethyl acetate extract was achieved by preparative thin layer chromatography. The active fraction was identified as terpenoid class compound by chemical screening. Based on the results of spectral studies (NMR, LC-MS, FTIR, etc.), the active compound was tentatively identified as 1, 19-bis (3-hydroxyazetidin-1-yl) nonadeca-5, 14-diene-1, 8, 12, 19-tetraone with molecular weight 462.41 g/mol. Minimum inhibitory concentration value ranges between 7.6 and 31.2 µg/mL against test organisms was observed. The cytotoxicity results on cervical cancer (HeLa) cell line showed IC50 value of 2.034 µg/mL. The corresponding compound is not previously reported from any microbial resources.

  12. Natural hydrazine-containing compounds: Biosynthesis, isolation, biological activities and synthesis.

    PubMed

    Le Goff, Géraldine; Ouazzani, Jamal

    2014-12-01

    Hydrazine, hydrazone and hydrazide derivatives are nitrogen-nitrogen bond containing compounds. Such molecules are relatively scarce in nature and have been isolated from plants, marine organisms and microorganisms. These compounds exhibit remarkable structural diversity and relevant biological activities. The enzymes involved in the formation of the N-N bond are still unknown, but many lines of evidence support the involvement of N-nitrosation and N-hydroxylation activating steps. Beside the challenging N-N bond, N-acylases catalyzing the C-N bond formation contribute to the chemical diversity of N-N-containing natural products (N2NP). This review examines the state of knowledge regarding the biosynthesis of N2NP, for which only two biosynthetic gene clusters have been investigated. Biological properties and chemical synthesis of hydrazines, hydrazones and hydrazides are also reported.

  13. Methods for the synthesis of aza(deaza)xanthines as a basis of biologically active compounds

    NASA Astrophysics Data System (ADS)

    Babkov, D. A.; Geisman, A. N.; Khandazhinskaya, A. L.; Novikov, M. S.

    2016-03-01

    The review covers methods for the synthesis of aza(deaza)xanthines, i.e., fused pyrrolo-, pyrazolo- and triazolopyrimidine heterocyclic systems, which are common core structures of various biologically active compounds. The extensive range of modern synthetic approaches is organized according to target structures and starting building blocks. The presented material is intended to benefit broad audience of specialists in the fields of organic, medicinal and pharmaceutical chemistry. The bibliography includes 195 references.

  14. Cytokinin Nucleosides - Natural Compounds with a Unique Spectrum of Biological Activities.

    PubMed

    Drenichev, Mikhail S; Oslovsky, Vladimir E; Mikhailov, Sergey N

    2016-01-01

    Cytokinin nucleosides exhibit antitumor, antiviral, antiprotozoal, blood pressure reducing, anti-inflammatory, and antipsychotic activity. These compounds also influence platelet aggregation and exhibit some other biological activities. Cytokinins are N6-substituted adenines and represent an important group of phytohormones with diverse biochemical functions in plants, stimulating cell division and plant growth. The main structural feature of cytokinin nucleosides is the presence of a hydrophobic hydrocarbon moiety at the N6-position of adenosine. This moiety is responsible for a difference in physicochemical and biological properties as compared to adenosine. 1-N-Tuberculosinyladenosine and N6-tuberculosinyladenosine are specifically produced by Mycobacterium tuberculosis as components of the plasmatic membrane, thus making them attractive targets for clinical test development. Structurally related compounds were found in marine organisms. It has been shown also that tRNA contains N6-isoprenyladenosine and some other related compounds. This review summarizes the structural features, biological activity, and the synthesis of cytokinin nucleosides and some of their closely related derivatives such as cytokinins and terpene derivatives of adenine.

  15. Evaluation of Biologically Active Compounds from Calendula officinalis Flowers using Spectrophotometry

    PubMed Central

    2012-01-01

    Background This study aimed to quantify the active biological compounds in C. officinalis flowers. Based on the active principles and biological properties of marigolds flowers reported in the literature, we sought to obtain and characterize the molecular composition of extracts prepared using different solvents. The antioxidant capacities of extracts were assessed by using spectrophotometry to measure both absorbance of the colorimetric free radical scavenger 2,2-diphenyl-1-picrylhydrazyl (DPPH) as well as the total antioxidant potential, using the ferric reducing power (FRAP) assay. Results Spectrophotometric assays in the ultraviolet-visible (UV-VIS) region enabled identification and characterization of the full range of phenolic and flavonoids acids, and high-performance liquid chromatography (HPLC) was used to identify and quantify phenolic compounds (depending on the method of extraction). Methanol ensured more efficient extraction of flavonoids than the other solvents tested. Antioxidant activity in methanolic extracts was correlated with the polyphenol content. Conclusions The UV-VIS spectra of assimilator pigments (e.g. chlorophylls), polyphenols and flavonoids extracted from the C. officinalis flowers consisted in quantitative evaluation of compounds which absorb to wavelengths broader than 360 nm. PMID:22540963

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

    PubMed Central

    Mikaili, Peyman; Maadirad, Surush; Moloudizargari, Milad; Aghajanshakeri, Shahin; Sarahroodi, Shadi

    2013-01-01

    Objective(s): Garlic (Allium sativum L. family Liliaceae) is well known in Iran and its leaves, flowers, and cloves have been used in traditional medicine for a long time. Research in recent decades has shown widespread pharmacological effects of A. sativum and its organosulfur compounds especially Allicin. Studies carried out on the chemical composition of the plant show that the most important constituents of this plant are organosulfur compounds such as allicin, diallyl disulphide, S-allylcysteine, and diallyl trisulfide. Allicin represents one of the most studied among these naturally occurring compounds. In addition to A. sativum, these compounds are also present in A. hirtifolium (shallot) and have been used to treat various diseases. This article reviews the pharmacological effects and traditional uses of A. sativum, A. hirtifolium, and their active constituents to show whether or not they can be further used as potential natural sources for the development of novel drugs. Materials and Methods: For this purpose, the authors went through a vast number of sources and articles and all needed data was gathered. The findings were reviewed and classified on the basis of relevance to the topic and a summary of all effects were reported as tables. Conclusion: 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. PMID:24379960

  17. Therapeutic uses and pharmacological properties of garlic, shallot, and their biologically active compounds.

    PubMed

    Mikaili, Peyman; Maadirad, Surush; Moloudizargari, Milad; Aghajanshakeri, Shahin; Sarahroodi, Shadi

    2013-10-01

    Garlic (Allium sativum L. family Liliaceae) is well known in Iran and its leaves, flowers, and cloves have been used in traditional medicine for a long time. Research in recent decades has shown widespread pharmacological effects of A. sativum and its organosulfur compounds especially Allicin. Studies carried out on the chemical composition of the plant show that the most important constituents of this plant are organosulfur compounds such as allicin, diallyl disulphide, S-allylcysteine, and diallyl trisulfide. Allicin represents one of the most studied among these naturally occurring compounds. In addition to A. sativum, these compounds are also present in A. hirtifolium (shallot) and have been used to treat various diseases. This article reviews the pharmacological effects and traditional uses of A. sativum, A. hirtifolium, and their active constituents to show whether or not they can be further used as potential natural sources for the development of novel drugs. For this purpose, the authors went through a vast number of sources and articles and all needed data was gathered. The findings were reviewed and classified on the basis of relevance to the topic and a summary of all effects were reported as tables. 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.

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

    PubMed

    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.

  19. Identification of phenolic compounds and biologically related activities from Ocotea odorifera aqueous extract leaves.

    PubMed

    Gontijo, Douglas Costa; Brandão, Geraldo Célio; Gontijo, Pablo Costa; de Oliveira, Alaíde Braga; Diaz, Marisa Alves Nogueira; Fietto, Luciano Gomes; Leite, João Paulo Viana

    2017-09-01

    Ocotea odorifera (Vell.) Rohwer is popularly used as food and flavoring. The aim of this study was to determine the chemical composition of the aqueous extract from O. odorifera leaves and evaluate the correlation of their phytochemical composition and biological activities. The antioxidant effect was determined by DPPH radical scavenging, β-carotene-linoleic acid and lipid peroxidation assays; the antibacterial activity was evaluated by the hole plate and MIC techniques and the antimutagenic activity was evaluated by the Ames test. Identification of phytochemicals was performed by LC-ESI/MS and the correlation between the phytochemical composition of the extract and the evaluated activities. The results allowed the identification of 13 phenolic compounds in the extract that exhibited high antioxidant activity and moderate antibacterial and antimutagenic action. Statistical analyses showed correlation of the total phenolic content with biologically related activities. The phytochemical analyses, together with the biological results, support the popular use of O. odorifera. Copyright © 2017 Elsevier Ltd. All rights reserved.

  20. Organocatalytic Michael and Friedel-Crafts reactions in enantioselective synthesis of biologically active compounds

    NASA Astrophysics Data System (ADS)

    Maltsev, O. V.; Beletskaya, Irina P.; Zlotin, Sergei G.

    2011-11-01

    Recent applications of organocatalytic Michael and Friedel-Crafts reactions in enantioselective synthesis of biologically active compounds: natural products, pharmaceutical agents and plant protection agents are reviewed. The key mechanisms of stereoinduction, types of organocatalysts and reagents used in these reactions are considered. The material is classified according to the type of newly formed bonds incorporating the asymmetric carbon atom, and the information for the most numerous C-C coupling reactions is systematized according to the natures of the electrophile and the nucleophile. The bibliography includes 433 references. Dedicated to Academician O M Nefedov on the occasion of his 80th birthday.

  1. Advances in structural modifications and biological activities of berberine: an active compound in traditional Chinese medicine.

    PubMed

    Huang, Z-J; Zeng, Y; Lan, P; Sun, P-H; Chen, W-M

    2011-11-01

    Berberine is an isoquinoline alkaloid isolated from Chinese herbs such as Coptidis Rhizome. This paper is a systematic review of the structural modifications of berberine for different biological activities such as antitumor, antimicrobial, anti-Alzheimer's disease, antihyperglycemic, anti-inflammatory and antimalaria. The current review would provide some useful information for further studies on structural modification of berberine for discovering new drug leads.

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

    NASA Astrophysics Data System (ADS)

    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

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

    PubMed

    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.

  4. Synthesis, reactions and biological activity of some new bis-heterocyclic ring compounds containing sulphur atom

    PubMed Central

    2013-01-01

    Background The derivatives of thieno[2,3-b]thiophene belong to a significant category of heterocyclic compounds, which have shown a wide spectrum of medical and industrial application. Results A new building block with two electrophilic center of thieno[2,3-b]thiophene derivatives 2 has been reported by one-pot reaction of diketone derivative 1 with Br2/AcOH in excellent yield. A variety of heteroaromatics having bis(1H-imidazo[1,2a] benzimidazole), bis(1H-imidazo[1,2-b][1,2,4]triazole)-3-methyl-4-phenylthieno[2,3-b]thiophene derivatives, dioxazolo-, dithiazolo-, and 1H-imidazolo-3-methyl-4-phenylthieno[2,3-b]thiophene derivatives as well pyrrolo, thiazolo -3-methyl-4-phenylthieno[2,3-b]thiophene derivatives have been designed, synthesized, characterized, and evaluated for their biological activity. Compounds 3–9 showed good bioassay result. These new derivatives were evaluated for anti-cancer activity against PC-3 cell lines, in vitro antioxidant potential and β-glucuronidase and α-glucosidase inhibitory activities. Compound 3 (IC50 = 56.26 ± 3.18 μM) showed a potent DPPH radical scavenging antioxidant activity and found to be more active than standard N-acetylcystein (IC50 = 105.9 ± 1.1 μM). Compounds 8a (IC50 = 13.2 ± 0.34 μM) and 8b (IC50 = 14.1 ± 0.28 μM) found as potent inhibitor of α-glucusidase several fold more active than the standard acarbose (IC50 = 841 ± 1.73 μM). Most promising results were obtained in β-glucuronidase enzyme inhibition assay. Compounds 5 (IC50 = 0.13 ± 0.019 μM), 6 (IC50 = 19.9 ± 0.285 μM), 8a (IC50 = 1.2 ± 0.0785 μM) and 9 (IC50 = 0.003 ± 0.09 μM) showed a potent inhibition of β-glucuronidase. Compound 9 was found to be several hundred fold more active than standard D-Saccharic acid 1,4-lactone (IC50 = 45.75 ± 2.16 μM). Conclusions Synthesis, characterization, and in vitro biological activity of a series of

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

    PubMed Central

    Friedman, Mendel; Rasooly, Reuven

    2013-01-01

    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. PMID:23612750

  6. Review of the inhibition of biological activities of food-related selected toxins by natural compounds.

    PubMed

    Friedman, Mendel; Rasooly, Reuven

    2013-04-23

    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.

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

    PubMed

    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.

  8. Production of anthraquinones, phenolic compounds and biological activities from hairy root cultures of Polygonum multiflorum Thunb.

    PubMed

    Thiruvengadam, Muthu; Praveen, Nagella; Kim, Eun-Hye; Kim, Seung-Hyun; Chung, Ill-Min

    2014-05-01

    report for the production of anthraquinones (emodin and physcion), phenolic compounds and biological activities from hairy root cultures of P. multiflorum.

  9. Identifying non-point sources of endocrine active compounds and their biological impacts in freshwater lakes

    USGS Publications Warehouse

    Baker, Beth H.; Martinovic-Weigelt, Dalma; Ferrey, Mark L.; Barber, Larry B.; Writer, Jeffrey H.; Rosenberry, Donald O.; Kiesling, Richard L.; Lundy, James R.; Schoenfuss, Heiko L.

    2014-01-01

    Contaminants of emerging concern, particularly endocrine active compounds (EACs), have been identified as a threat to aquatic wildlife. However, little is known about the impact of EACs on lakes through groundwater from onsite wastewater treatment systems (OWTS). This study aims to identify specific contributions of OWTS to Sullivan Lake, Minnesota, USA. Lake hydrology, water chemistry, caged bluegill sunfish (Lepomis macrochirus), and larval fathead minnow (Pimephales promelas) exposures were used to assess whether EACs entered the lake through OWTS inflow and the resultant biological impact on fish. Study areas included two OWTS-influenced near-shore sites with native bluegill spawning habitats and two in-lake control sites without nearby EAC sources. Caged bluegill sunfish were analyzed for plasma vitellogenin concentrations, organosomatic indices, and histological pathologies. Surface and porewater was collected from each site and analyzed for EACs. Porewater was also collected for laboratory exposure of larval fathead minnow, before analysis of predator escape performance and gene expression profiles. Chemical analysis showed EACs present at low concentrations at each study site, whereas discrete variations were reported between sites and between summer and fall samplings. Body condition index and liver vacuolization of sunfish were found to differ among study sites as did gene expression in exposed larval fathead minnows. Interestingly, biological exposure data and water chemistry did not match. Therefore, although results highlight the potential impacts of seepage from OWTS, further investigation of mixture effects and life history factor as well as chemical fate is warranted.

  10. Rethinking molecular similarity: comparing compounds on the basis of biological activity.

    PubMed

    Petrone, Paula M; Simms, Benjamin; Nigsch, Florian; Lounkine, Eugen; Kutchukian, Peter; Cornett, Allen; Deng, Zhan; Davies, John W; Jenkins, Jeremy L; Glick, Meir

    2012-08-17

    Since the advent of high-throughput screening (HTS), there has been an urgent need for methods that facilitate the interrogation of large-scale chemical biology data to build a mode of action (MoA) hypothesis. This can be done either prior to the HTS by subset design of compounds with known MoA or post HTS by data annotation and mining. To enable this process, we developed a tool that compares compounds solely on the basis of their bioactivity: the chemical biological descriptor "high-throughput screening fingerprint" (HTS-FP). In the current embodiment, data are aggregated from 195 biochemical and cell-based assays developed at Novartis and can be used to identify bioactivity relationships among the in-house collection comprising ~1.5 million compounds. We demonstrate the value of the HTS-FP for virtual screening and in particular scaffold hopping. HTS-FP outperforms state of the art methods in several aspects, retrieving bioactive compounds with remarkable chemical dissimilarity to a probe structure. We also apply HTS-FP for the design of screening subsets in HTS. Using retrospective data, we show that a biodiverse selection of plates performs significantly better than a chemically diverse selection of plates, both in terms of number of hits and diversity of chemotypes retrieved. This is also true in the case of hit expansion predictions using HTS-FP similarity. Sets of compounds clustered with HTS-FP are biologically meaningful, in the sense that these clusters enrich for genes and gene ontology (GO) terms, showing that compounds that are bioactively similar also tend to target proteins that operate together in the cell. HTS-FP are valuable not only because of their predictive power but mainly because they relate compounds solely on the basis of bioactivity, harnessing the accumulated knowledge of a high-throughput screening facility toward the understanding of how compounds interact with the proteome.

  11. Strigolactones--intriguing biologically active compounds: perspectives for deciphering their biological role and for proposing practical application.

    PubMed

    Vurro, Maurizio; Yoneyama, Koichi

    2012-05-01

    Strigolactones are a class of bioactive natural metabolites produced by plant roots and released into the rhizosphere. They were discovered as signals indispensable for the induction of germination of seeds of root parasitic weeds, but since then, interestingly, many other biological, physiological and ecological roles have been described. This has suddenly provoked huge scientific interest in these compounds within different research fields. In this short perspective the attention is focused mainly on the ongoing and future research aimed at deciphering the biological roles of strigolactones that could positively affect, more or less directly, the management of parasitic weeds.

  12. SYNTHESIS AND BIOLOGICAL ACTIVITY OF SULFUR COMPOUNDS SHOWING STRUCTURAL ANALOGY WITH COMBRETASTATIN A-4

    PubMed Central

    dos Santos, Edson dos A.; Prado, Paulo C.; de Carvalho, Wanderley R.; de Lima, Ricardo V.; Beatriz e, Adilson; de Lima, Dênis P.; Hamel, Ernest; Dyba, Marzena A.; Albuquerque, Sergio

    2013-01-01

    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). PMID:23766547

  13. SYNTHESIS AND BIOLOGICAL ACTIVITY OF SULFUR COMPOUNDS SHOWING STRUCTURAL ANALOGY WITH COMBRETASTATIN A-4.

    PubMed

    Dos Santos, Edson Dos A; Prado, Paulo C; de Carvalho, Wanderley R; de Lima, Ricardo V; Beatriz E, Adilson; de Lima, Dênis P; Hamel, Ernest; Dyba, Marzena A; Albuquerque, Sergio

    2013-02-01

    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).

  14. Computational Method for the Systematic Identification of Analog Series and Key Compounds Representing Series and Their Biological Activity Profiles.

    PubMed

    Stumpfe, Dagmar; Dimova, Dilyana; Bajorath, Jürgen

    2016-08-25

    A computational methodology is introduced for detecting all unique series of analogs in large compound data sets, regardless of chemical relationships between analogs. No prior knowledge of core structures or R-groups is required, which are automatically determined. The approach is based upon the generation of retrosynthetic matched molecular pairs and analog networks from which distinct series are isolated. The methodology was applied to systematically extract more than 17 000 distinct series from the ChEMBL database. For comparison, analog series were also isolated from screening compounds and drugs. Known biological activities were mapped to series from ChEMBL, and in more than 13 000 of these series, key compounds were identified that represented substitution sites of all analogs within a series and its complete activity profile. The analog series, key compounds, and activity profiles are made freely available as a resource for medicinal chemistry applications.

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

    NASA Astrophysics Data System (ADS)

    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).

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

    NASA Astrophysics Data System (ADS)

    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.

  17. Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1).

    PubMed

    Hsu, Danny C; Roth, Howard S; West, Diana C; Botham, Rachel C; Novotny, Chris J; Schmid, Steven C; Hergenrother, Paul J

    2012-01-09

    Procaspase-Activating Compound 1 (PAC-1) is an ortho-hydroxy N-acyl hydrazone that enhances the enzymatic activity of procaspase-3 in vitro and induces apoptosis in cancer cells. An analogue of PAC-1, called S-PAC-1, was evaluated in a veterinary clinical trial in pet dogs with lymphoma and found to have considerable potential as an anticancer agent. With the goal of identifying more potent compounds in this promising class of experimental therapeutics, a combinatorial library based on PAC-1 was created, and the compounds were evaluated for their ability to induce death of cancer cells in culture. For library construction, 31 hydrazides were condensed in parallel with 27 aldehydes to create 837 PAC-1 analogues, with an average purity of 91%. The compounds were evaluated for their ability to induce apoptosis in cancer cells, and through this work, six compounds were discovered to be substantially more potent than PAC-1 and S-PAC-1. These six hits were further evaluated for their ability to relieve zinc-mediated inhibition of procaspase-3 in vitro. In general, the newly identified hit compounds are two- to four-fold more potent than PAC-1 and S-PAC-1 in cell culture, and thus have promise as experimental therapeutics for treatment of the many cancers that have elevated expression levels of procaspase-3.

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

    PubMed

    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.

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

    PubMed Central

    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

  20. Isolation, identification, synthesis and biological activity of volatile compounds from the heads of Atta ants

    Treesearch

    R. G. Riley; R. M. Silverstein; John C. Moser

    1974-01-01

    S-(+)-4-methyl-3-hetanone has been identified as the principal alarm pheromone of Atta texana and Atta cephalotes. Both enantiomers of 4-methyl-3-heptanone have been synthesized and their biological activities have been compared on both species of ants. Comparison of the geometric averages of responnse rations, at...

  1. [The effectiveness of ultralow doses and concentrations of biologically active compounds].

    PubMed

    Ashmarin, I P; Lelekova, T V; Sanzhieva, L Ts

    1992-01-01

    Numerous data of literature are analysed on the biological activity of ultra-low (10(-12)-10(-19) M) concentrations and corresponding doses of same bioregulators. Our own data are presented on the modulation of lymphatic vessel contractility by peptides (thyroliberin, defensin, and tuftsin) in concentrations ranging from 10(-13) to 10(-16) M. Hypothetic mechanisms of these phenomena are discussed.

  2. Comparison of Nutritional Composition, Aroma Compounds, and Biological Activities of Two Kinds of Tartary Buckwheat Tea.

    PubMed

    Guo, Huimin; Yang, Xiushi; Zhou, Haitao; Luo, Xiuxiu; Qin, Peiyou; Li, Jincai; Ren, Guixing

    2017-07-01

    Tartary buckwheat tea (TBT) is becoming increasingly popular for its unique flavor and health benefits. However, there is little information regarding the differences in nutritional quality among different kinds of TBT. Two kinds of TBT samples, whole grain tea (WGT) and whole plant tea (WPT), were collected from markets in China. The content of their nutritional compositions, including protein, amino acids, starch, fat, fatty acids, and flavonoids, as well as aroma compounds, were determined. Antioxidant and α-glucosidase inhibitory activities were also evaluated. WPT showed higher levels of protein and fat relative to WGT, but the content of essential amino acids and fatty acids was lower. WPT contained more total flavonoids with quercetin as the predominant flavonoid (81%), while rutin was the principal flavonoid compound (86%) in WGT. GC-MS analysis indicated that there were some differences in the aroma compound profile between WGT and WPT, though 14 aroma compounds were identified in both of them with 3-ethyl-2,5-dimethyl-pyrazine as the predominant compound. In addition, WPT showed superior antioxidant and α-glucosidase inhibitory activities than WGT. However, the total flavonoid content determined in tea soup was decreased by 60% and 98% compared with that in the alcohol extracts of WGT and WPT, respectively. The antioxidant and α-glucosidase inhibitory activities of tea soup were also lowered, especially for WPT. The differences between 2 kinds of TBT might be due to the variety of raw materials and processing methods. Diversified plant materials and scientific processing technologies should be taken into account to develop a nutritional and healthy TBT product. © 2017 Institute of Food Technologists®.

  3. Experimental and modeling study on removal of pharmaceutically active compounds in rotating biological contactors.

    PubMed

    Vasiliadou, I A; Molina, R; Martínez, F; Melero, J A

    2014-06-15

    The aim of this work was to study the biological removal of pharmaceutical compounds in rotating biological contactors (RBCs) under continuous operation. A two-stage RBC was used, providing a total surface area of 1.41 m(2). Four pharmaceuticals of different therapeutic classes; caffeine, sulfamethoxazole, ranitidine and carbamazepine, were studied. Six experimental scenarios were applied to the RBC-system by varying substrates' loadings (12-54 gCOD/d), volumetric flow rate (2-5L/d), and pharmaceuticals' concentration (20-50 μg/L). The different conditions resulted to different solid retention times (SRT: 7-21 d) in each scenario. The increase of SRT due to variations of the operating conditions seemed to have a positive effect on pharmaceuticals' removal. Likewise, a negative correlation was observed between substrates' loading and pharmaceuticals' removal. An increase of initial pharmaceuticals' concentration resulted to decrease of SRT and pharmaceuticals' removal, suggesting a toxic effect to the biofilm. The maximum removals achieved were greater than 85% for all pharmaceuticals. Finally, a mathematical model which includes biofilm growth, substrates' utilization and pharmaceuticals' elimination was developed. The model predicts the contribution of sorption and biodegradation on pharmaceuticals' elimination taking into account the diffusion of pharmaceuticals inside biofilm.

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

    PubMed

    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.

  5. Biological and chemical properties of alkanediazotates as active species of N-nitroso compounds.

    PubMed

    Ukawa, S; Mochizuki, M

    1991-01-01

    The mutagenicity and chemical reactivity of (E)- and (Z)-potassium alkanediazotates, as precursors of corresponding alkanediazohydroxides, were investigated. In three microbial strains, Salmonella typhimurium TA1535 and Escherichia coli WP2 and WP2hcr-, the effect of changing the alkyl group on mutagenic potency was similar for (E)- and (Z)-diazotates, N-alkyl-N-nitrosoureas and alpha-hydroxynitrosamines. The capacity to alkylate nicotinamide, measured in an aqueous phosphate buffer, decreased with increasing alkyl chain length. Specific mutagenicity in S. typhimurium TA1535 was linearly related to alkylating activity. These results confirm that alkanediazohydroxides are the active alkylating species of N-nitroso compounds, and that their mutagenicity is determined by their alkylating activity.

  6. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound

    PubMed Central

    Kiyonaka, Shigeki; Kato, Kenta; Nishida, Motohiro; Mio, Kazuhiro; Numaga, Takuro; Sawaguchi, Yuichi; Yoshida, Takashi; Wakamori, Minoru; Mori, Emiko; Numata, Tomohiro; Ishii, Masakazu; Takemoto, Hiroki; Ojida, Akio; Watanabe, Kenta; Uemura, Aya; Kurose, Hitoshi; Morii, Takashi; Kobayashi, Tsutomu; Sato, Yoji; Sato, Chikara; Hamachi, Itaru; Mori, Yasuo

    2009-01-01

    Canonical transient receptor potential (TRPC) channels control influxes of Ca2+ and other cations that induce diverse cellular processes upon stimulation of plasma membrane receptors coupled to phospholipase C (PLC). Invention of subtype-specific inhibitors for TRPCs is crucial for distinction of respective TRPC channels that play particular physiological roles in native systems. Here, we identify a pyrazole compound (Pyr3), which selectively inhibits TRPC3 channels. Structure-function relationship studies of pyrazole compounds showed that the trichloroacrylic amide group is important for the TRPC3 selectivity of Pyr3. Electrophysiological and photoaffinity labeling experiments reveal a direct action of Pyr3 on the TRPC3 protein. In DT40 B lymphocytes, Pyr3 potently eliminated the Ca2+ influx-dependent PLC translocation to the plasma membrane and late oscillatory phase of B cell receptor-induced Ca2+ response. Moreover, Pyr3 attenuated activation of nuclear factor of activated T cells, a Ca2+-dependent transcription factor, and hypertrophic growth in rat neonatal cardiomyocytes, and in vivo pressure overload-induced cardiac hypertrophy in mice. These findings on important roles of native TRPC3 channels are strikingly consistent with previous genetic studies. Thus, the TRPC3-selective inhibitor Pyr3 is a powerful tool to study in vivo function of TRPC3, suggesting a pharmaceutical potential of Pyr3 in treatments of TRPC3-related diseases such as cardiac hypertrophy. PMID:19289841

  7. Enhanced Production of Anthraquinones and Phenolic Compounds and Biological Activities in the Cell Suspension Cultures of Polygonum multiflorum

    PubMed Central

    Thiruvengadam, Muthu; Rekha, Kaliyaperumal; Rajakumar, Govindasamy; Lee, Taek-Jun; Kim, Seung-Hyun; Chung, Ill-Min

    2016-01-01

    Anthraquinones (AQs) and phenolic compounds are important phytochemicals that are biosynthesized in cell suspension cultures of Polygonum multiflorum. We wanted to optimize the effects of plant growth regulators (PGRs), media, sucrose, l-glutamine, jasmonic acid (JA), and salicylic acid (SA) for the production of phytochemicals and biomass accumulation in a cell suspension culture of P. multiflorum. The medium containing Murashige and Skoog (MS) salts and 4% sucrose supplemented with 1 mg/L 2,4-dichlorophenoxyacetic acid, 0.5 mg/L thidiazuron, and 100 µM l-glutamine at 28 days of cell suspension culture was suitable for biomass accumulation and AQ production. Maximum biomass accumulation (12.5 and 12.35 g fresh mass (FM); 3 and 2.93 g dry mass (DM)) and AQ production (emodin 295.20 and 282 mg/g DM; physcion 421.55 and 410.25 mg/g DM) were observed using 100 µM JA and SA, respectively. JA- and SA-elicited cell cultures showed several-fold higher biomass accumulation and AQ production than the control cell cultures. Furthermore, the cell suspension cultures effectively produced 23 phenolic compounds, such as flavonols and hydroxycinnamic and hydroxybenzoic acid derivatives. PGR-, JA-, and SA-elicited cell cultures produced a higher amount of AQs and phenolic compounds. Because of these metabolic changes, the antioxidant, antimicrobial, and anticancer activities were high in the PGR-, JA-, and SA-elicited cell cultures. The results showed that the elicitors (JA and SA) induced the enhancement of biomass accumulation and phytochemical (AQs and phenolic compounds) production as well as biological activities in the cell suspension cultures of P. multiflorum. This optimized protocol can be developed for large-scale biomass accumulation and production of phytochemicals (AQs and phenolic compounds) from cell suspension cultures, and the phytochemicals can be used for various biological activities. PMID:27854330

  8. Enhanced Production of Anthraquinones and Phenolic Compounds and Biological Activities in the Cell Suspension Cultures of Polygonum multiflorum.

    PubMed

    Thiruvengadam, Muthu; Rekha, Kaliyaperumal; Rajakumar, Govindasamy; Lee, Taek-Jun; Kim, Seung-Hyun; Chung, Ill-Min

    2016-11-16

    Anthraquinones (AQs) and phenolic compounds are important phytochemicals that are biosynthesized in cell suspension cultures of Polygonum multiflorum. We wanted to optimize the effects of plant growth regulators (PGRs), media, sucrose, l-glutamine, jasmonic acid (JA), and salicylic acid (SA) for the production of phytochemicals and biomass accumulation in a cell suspension culture of P. multiflorum. The medium containing Murashige and Skoog (MS) salts and 4% sucrose supplemented with 1 mg/L 2,4-dichlorophenoxyacetic acid, 0.5 mg/L thidiazuron, and 100 µM l-glutamine at 28 days of cell suspension culture was suitable for biomass accumulation and AQ production. Maximum biomass accumulation (12.5 and 12.35 g fresh mass (FM); 3 and 2.93 g dry mass (DM)) and AQ production (emodin 295.20 and 282 mg/g DM; physcion 421.55 and 410.25 mg/g DM) were observed using 100 µM JA and SA, respectively. JA- and SA-elicited cell cultures showed several-fold higher biomass accumulation and AQ production than the control cell cultures. Furthermore, the cell suspension cultures effectively produced 23 phenolic compounds, such as flavonols and hydroxycinnamic and hydroxybenzoic acid derivatives. PGR-, JA-, and SA-elicited cell cultures produced a higher amount of AQs and phenolic compounds. Because of these metabolic changes, the antioxidant, antimicrobial, and anticancer activities were high in the PGR-, JA-, and SA-elicited cell cultures. The results showed that the elicitors (JA and SA) induced the enhancement of biomass accumulation and phytochemical (AQs and phenolic compounds) production as well as biological activities in the cell suspension cultures of P. multiflorum. This optimized protocol can be developed for large-scale biomass accumulation and production of phytochemicals (AQs and phenolic compounds) from cell suspension cultures, and the phytochemicals can be used for various biological activities.

  9. Oxidation of antibacterial compounds by ozone and hydroxyl radical: elimination of biological activity during aqueous ozonation processes.

    PubMed

    Dodd, Michael C; Kohler, Hans-Peter E; von Gunten, Urs

    2009-04-01

    A wide variety of antibacterial compounds is rapidly oxidized by 03 and hydroxyl radical (*OH) during aqueous ozonation. Quantitative microbiological assays have been developed here or adapted from existing methods and utilized to measure the resulting changes in antibacterial potencies during O3 and *OH treatment of 13 antibacterial molecules (roxithromycin, azithromycin, tylosin, ciprofloxacin, enrofloxacin, penicillin G, cephalexin, sulfamethoxazole, trimethoprim, lincomycin,tetracycline, vancomycin, and amikacin) from 9 structural classes (macrolides, fluoroquinolones, beta-lactams, sulfonamides, dihydrofolate reductase inhibitors, lincosamides, tetracyclines, glycopeptides, and aminoglycosides), as well as the biocide triclosan. Potency measurements were determined from dose-response relationships obtained by exposing Escherichia coli or Bacillus subtilis reference strains to treated samples of each antibacterial compound via broth micro- or macrodilution assays and related to the measured residual concentrations of parent antibacterial in each sample. Data obtained from these experiments show that O3 and *OH reactions lead in nearly all cases to stoichiometric elimination of antibacterial activity (i.e., loss of 1 mole equivalent of potency per mole of parent compound consumed). The beta-lactams penicillin G (PG) and cephalexin (CP) represent the only clear exceptions, as bioassay measurements indicate that biologically active products may be formed in the reactions of these two compounds with both O3 and *OH. The active product(s) generated in the direct reaction of O3 with PG appear(s) to be recalcitrant to further transformation by O3, though any biologically active products formed in the reactions of CP with O3, or of either PG or CP with *OH, are apparently deactivated by further reactions with O3 or *OH, respectively. Thus, with few exceptions, it can be expected that municipal wastewater ozonation will generally yield sufficient structural modification

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

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed Central

    Jia, Xia; Zhao, YongHua; Wang, WenKe; He, Yunhua

    2015-01-01

    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. PMID:26395070

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

    PubMed

    Jia, Xia; Zhao, YongHua; Wang, WenKe; He, Yunhua

    2015-09-23

    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.

  13. Variability of antioxidant and biological activities of Rhus tripartitum related to phenolic compounds

    PubMed Central

    Ben Miled, Hanène; Saada, Mariem; Jallali, Ines; Ben Barka, Zaineb; Tlili, Mounira; Alimi, Hichem; Sakly, Mohsen; Ben Rhouma, Khémais; Abderrabba, Manef; Abdelmelek, Hafedh; Tebourbi, Olfa; Ksouri, Riadh

    2017-01-01

    Rhus species are known in traditional medicine for their therapeutic virtue and their extracts showed numerous important properties including antimalarial, antimicrobial, antiviral, and hypoglycemic and anticonvulsant activities. Rhus tripartitum (Ucria) is a medicinal plant widely used in Tunisia folk medicine against chronic diarrhea and gastric ulcer. This study was designed to examine in vitro and ex vivo antioxidant, anti-inflammatory and anticancer activities of four extracts of Rhus tripartitum root cortex with increasing solvent polarity (hexane, dichloromethane, methanol and water). HPLC was used to identify and quantify phenolic compounds in Rhus extract. Water extract showed the highest antioxidant activity using oxygen radical absorbance capacity (ORAC method) with 8.95 ± 0.47 µmol Trolox/mg and a cell based-assay with 0.28 ± 0.12 µmol Trolox/mg as compared to the other fractions. Moreover, methanol extract displayed the strongest anti-cancer activity against human lung carcinoma (A-549) and colon adenocarcinoma cell lines (DLD-1) with an IC50 value of 60.69 ± 2.58 and 39.83 ± 4.56 µg/ml (resazurin test) and 44.52 ± 5.96 and 55.65 ± 6.00 µg/ml (hoechst test), respectively. Besides, the highest anti-inflammatory activity, inhibiting nitric oxide (NO) release, was exhibited by dichloromethane extract with 31.5 % at 160 µg/ml in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. The HPLC analysis showed that catechol and kaempferol were the major phenolics. These data suggest the richness of all fractions of Ucria root on interesting bioactive molecules with different polarity and confirm the known traditional therapeutics virtues of this species for the treatment of dysentery, diarrhea and gastric ulcer. PMID:28694749

  14. Supercritical CO2 extraction of functional compounds from Spirulina and their biological activity.

    PubMed

    K G, Mallikarjun Gouda; K, Udaya Sankar; R, Sarada; G A, Ravishankar

    2015-06-01

    Supercritical carbon dioxide (SCCO2) extraction and fractionation of Spirulina platensis was carried out to obtain functional compounds with antioxidant, antimicrobial and enzyme inhibitory activities. Extraction of SCCO2 was carried out using 200 g of Spirulina powder at 40 ºC under 120 bar pressure with CO2 flow rate of 1.2 kg h(-1). SCCO2 fraction obtained was further treated with hexane and ethyl acetate to identify its components. Individual components were identified by comparing mass spectra of samples with standard data and retention indices (RI) of C5-C20 n-alkanes mixture using the kovat index formula. The phenolic and flavonoid content of the SCCO2 extract was found to be 0.34 ± 0.01 g/100 g and 0.12 ± 0.01 g/100 g respectively. The SCCO2 extract had antioxidant activity with IC50 value of 109.6 ± 3.0 μg mL(-1) for DPPH (2,2-Diphenyl-1-picryl hydrazyl radical), IC50 value of 81.66 ± 2.5 μg mL(-1) for reducing power and IC50 value of 112.70 ± 0.8 μg mL(-1) for hydroxyl radical scavenging activity. Further, antioxidant activity study on oxidative induced DNA damage was analysed to elucidate the positive role of SCCO2 extract. SCCO2 extracts showed high antimicrobial activity against Gram-positive bacteria (Staphylococcus aureus FRI 722 and Bacillus cereus F 4810) compared to that of Gram negative bacteria (Escherichia coli MTCC 108 and Yersinia enterocolitica MTCC 859). The SCCO2 extract exhibited inhibitory activity on both Angiotensin-1 converting enzyme and α-glucosidase with IC50 values of 274 ± 1.0 μg mL(-1) and 307 ± 2.0 μg mL(-1) respectively.

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

    USGS Publications Warehouse

    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

  16. Revealing of Biological Activity in Crude Extracts, Seperated Fractions, Groups of Chemical Substance and Individual Compounds

    USDA-ARS?s Scientific Manuscript database

    Crude extracts, separated fractions, groups of chemical substances, and individual compounds from natural sources are all evaluated stepwise while performing purifications in in-house bioassays. In a stepwise fashion proceeding from crude extracts to fractions and on to pure compounds, decisions ar...

  17. Biological activities of nitidine, a potential anti-malarial lead compound

    PubMed Central

    2012-01-01

    Background Nitidine is thought to be the main active ingredient in several traditional anti-malarial remedies used in different parts of the world. The widespread use of these therapies stresses the importance of studying this molecule in the context of malaria control. However, little is known about its potential as an anti-plasmodial drug, as well as its mechanism of action. Methods In this study, the anti-malarial potential of nitidine was evaluated in vitro on CQ-sensitive and -resistant strains. The nitidine's selectivity index compared with cancerous and non-cancerous cell lines was then determined. In vivo assays were then performed, using the four-day Peter's test methodology. To gain information about nitidine's possible mode of action, its moment of action on the parasite cell cycle was studied, and its localization inside the parasite was determined using confocal microscopy. The in vitro abilities of nitidine to bind haem and to inhibit β-haematin formation were also demonstrated. Results Nitidine showed similar in vitro activity in CQ-sensitive and resistant strains, and also a satisfying selectivity index (> 10) when compared with a non-cancerous cells line. Its in vivo activity was moderate; however, no sign of acute toxicity was observed during treatment. Nitidine's moment of action on the parasite cycle showed that it could not interfere with DNA replication; this was consistent with the observation that nitidine did not localize in the nucleus, but rather in the cytoplasm of the parasite. Nitidine was able to form a 1-1 complex with haem in vitro and also inhibited β-haematin formation with the same potency as chloroquine. Conclusion Nitidine can be considered a potential anti-malarial lead compound. Its ability to complex haem and inhibit β-haematin formation suggests a mechanism of action similar to that of chloroquine. The anti-malarial activity of nitidine could therefore be improved by structural modification of this molecule to increase

  18. Volatile compounds secreted by Brindley's glands of adult Triatoma infestans: identification and biological activity of previously unidentified compounds.

    PubMed

    González Audino, P; Alzogaray, R A; Vassena, C; Masuh, H; Fontán, A; Gatti, P; Martínez, A; Camps, E; Cork, A; Zerba, E

    2007-06-01

    Volatile emissions of adult male Triatoma infestans were collected on non-polar SPME fibers and analyzed by gas chromatography linked to a mass spectrometer. A complex mixture of 16 short-chain esters and acids were identified. The composition of short-chain aliphatic acids (ethanoic to nonanoic acids) was similar to previously reported results. The most abundant aliphatic acid was 2-methylpropanoic acid, constituting 18% of the total volatile content. Also abundant were the esters 2- and 3-methylbutyl 2-methylpropanoate, which constituted 30% and 22%, respectively, of the total volatile content. A similar pattern of compounds was observed in the volatiles secreted by dissected male Brindley's glands; however, in this case, 2- and 3-methylbutan-1-ol were detected which were not found in live insect volatile emissions. Large variability in volatile composition was also observed among the glands excised from different insects. Electroantennographic (EAG) evaluation of the components of Brindley's gland showed significant responses for 2- and 3-methylbutyl 2-methylpropanoate compared to controls. The mixture of volatiles secreted by excised Brindley's glands and the isolated 2- and 3-methylbutyl 2-methylpropanoate had repellent effects on both male and female T. infestans, possibly associated with a defensive strategy.

  19. FATE OF PAH COMPOUNDS IN TWO SOIL TYPES: INFLUENCE OF VOLATILIZATION, ABIOTIC LOSS, AND BIOLOGICAL ACTIVITY

    EPA Science Inventory

    The fate of 14 polycyclic aromatic hydrocarbon (PAH) compounds was evaluated with regard to interphase transfer potential and mechanisms of treatment in soil under unsaturated conditions. Volatilization and abiotic and biotic fate of the PAHs were determined using two soils not p...

  20. [Studies by means of 1H NMR spectroscopy of complex formation of aromatic biologically active compounds with antibiotic topotecan].

    PubMed

    Mosunov, A A; Kostiukov, V V; Evstigneev, M P

    2012-01-01

    The analysis of heteroassociation of antibiotic topotecan (TPT) with aromatic biologically active compounds (BAC): caffeine, mutagens ethidium bromide and proflavine, antibiotic daunomycin, vitamins flavin-mononucleotide and nicotinamide, has been carried out in the work using 1H NMR spectroscopy data. The equilibrium constants of heteroassociation and induced chemical shifts of the protons have been obtained in the complexes with BAC. It is found that the complex formation TPT-BAC has the nature of stacking of the chromophores, additionally stabilized in the case of proflavine by intermolecular hydrogen bond. Calculation of the basic components of the Gibbs free energy of the complexation reactions is carried out, and the factors which stabilize and destabilize the heterocomplexes of molecules are revealed.

  1. Fatty acids from lipids of marine organisms: molecular biodiversity, roles as biomarkers, biologically active compounds, and economical aspects.

    PubMed

    Bergé, Jean-Pascal; Barnathan, Gilles

    2005-01-01

    Because of their characteristic living environments, marine organisms produce a variety of lipids. Fatty acids constitute the essential part of triglycerides and wax esters, which are the major components of fats and oils. Nevertheless, phospholipids and glycolipids have considerable importance and will be taken into account, especially the latter compounds that excite increasing interest regarding their promising biological activities. Thus, in addition to the major polyunsaturated fatty acids (PUFA) such as eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids, a great number of various fatty acids occur in marine organisms, e.g. saturated, mono- and diunsaturated, branched, halogenated, hydroxylated, methoxylated, non-methylene-interrupted. Various unprecedented chemical structures of fatty acids, and lipid-containing fatty acids, have recently been discovered, especially from the most primitive animals such as sponges and gorgonians. This review of marine lipidology deals with recent advances in the field of fatty acids since the end of the 1990s. Different approaches will be followed, mainly developing biomarkers of trophic chains in marine ecosystems and of chemotaxonomic interest, reporting new structures, especially those with biological activities or biosynthetic interest. An important part of this review will be devoted to the major PUFA, their relevance to health and nutrition, their biosynthesis, their sources (usual and promising) and market.

  2. Appraisal of biological activities and identification of phenolic compound of African marigold (Tagetes erecta) flower extract.

    PubMed

    Phrutivorapongkul, Ampai; Kiattisin, Kanokwan; Jantrawut, Pensak; Chansakaow, Sunee; Vejabhikul, Suwanna; Leelapornpisid, Pimporn

    2013-11-01

    The flowers of African marigold (Tagetes erecta L), a medicinal plant widely cultivated in Thailand, were subjected to evaluation for total phenolics, DPPH scavenging and thiobarbituric acid-reactive substance (TBARs) assays as well as tyrosinase inhibitory activity. In preliminary studies, the ethyl acetate (EA) extract obtained by continuous extraction showed the highest activities with highest phenolic content among all extracts. Bioassay-guided fractionation of EA extract led to isolation of a flavonoid identified as quercetagetin. Interestingly, it was found that quercetagetin exhibited potent DPPH scavenging activity with IC50 of 3.70 μg/ml which is about 2-3 times higher activity than standard quercetin (IC50 5.07 μg/ml) and trolox (IC50 9.93 μg/ml). Moreover, it exhibited tyrosinase inhibitory activity on L-tyrosine (IC50 89.31 μg/ml), higher than α- and β-arbutins (IC50 157.77 and 222.35 μg/ml) and slightly higher (IC50 128.41 μg/ml) than ellagic acid (IC50 151.1 μg/ml) when using L-DOPA as substrate. Testing with skin fibroblasts, all the extracts and quercetagetin demonstrated no toxic effect. These finding strongly indicate that African marigold flower is a promising source of natural antioxidative and tyrosinase inhibitory substances with safe to skin.

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

    NASA Astrophysics Data System (ADS)

    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.

  4. Euglena gracilis as a supplementary test organism for detecting biologically active compounds.

    PubMed

    Macor, M; Beno, J; Grones, J; Siekel, P; Novotný, J

    1996-01-01

    The mutagenic activity of more than 120 antimicrobial agents and protective components was investigated. Only Kathon showed a consistent increase in revertant counts in the Ames test on Salmonella typhimurium. The hereditary bleaching test on Euglena gracilis used for detecting extranuclear mutations, showed positive results for Kathon, triethanolamine and diamine silver tetraborate.

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

    PubMed

    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 < 0.05). At 6 degrees C storage, there was a significant loss observed from 15 to 30 days. Similar results were obtained at 23 and 35 degrees C (P < 0.05). There was retention of more than 40% of ellagic and quercetin after 60 days at 35 +/- 1 degrees C. Anthocyanins were not detected after 60 days of storage at 35 +/- 1 degrees C. Significant retention (P < 0.05) was obtained for malvidin (42.8 and 25.8%) and peonidin (74.0 and 79.5%) after 60 days of storage at 23

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

    PubMed Central

    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. PMID:23984355

  7. Bioactive compounds and biological activities of Jatropha curcas L. kernel meal extract.

    PubMed

    Oskoueian, Ehsan; Abdullah, Norhani; Ahmad, Syahida; Saad, Wan Zuhainis; Omar, Abdul Rahman; Ho, Yin Wan

    2011-01-01

    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 (Fe(3+)) to ferrous ion (Fe(2+)). Cytotoxicity assay results indicated the potential of methanolic extract as a source of anticancer therapeutic agents toward breast cancer cells.

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

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed

    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.

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

    PubMed

    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, (1)H 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 (K(b)) 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.

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

    PubMed Central

    Oskoueian, Ehsan; Abdullah, Norhani; Ahmad, Syahida; Saad, Wan Zuhainis; Omar, Abdul Rahman; Ho, Yin Wan

    2011-01-01

    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. PMID:22016638

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

    PubMed

    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.

  13. Recent advances in biologically active compounds in herbs and spices: a review of the most effective antioxidant and anti-inflammatory active principles.

    PubMed

    Rubió, Laura; Motilva, Maria-José; Romero, Maria-Paz

    2013-01-01

    Spices, like vegetables, fruit, and medicinal herbs, are known to possess a variety of antioxidant effects and other biological activities. Phenolic compounds in these plant materials are closely associated with their antioxidant activity, which is mainly due to their redox properties and their capacity to block the production of reactive oxygen species. More recently, their ability to interfere with signal transduction pathways involving various transcription factors, protein kinases, phosphatases, and other metabolic enzymes has also been demonstrated. Many of the spice-derived compounds which are potent antioxidants are of great interest to biologists and clinicians because they may help protect the human body against oxidative stress and inflammatory processes. It is important to study the bioactive compounds that can modulate target functions related to defence against oxidative stress, and that might be used to achieve health benefits individually. In the present review, an attempt has been made to summarize the most current scientific evidence about the in vitro and in vivo effects of the bioactive compounds derived from herbs and spices, focused on anti-inflammatory and antioxidant effects, in order to provide science-based evidence for the traditional uses and develop either functional foods or nutraceuticals.

  14. Analysis of biologically active compounds in potatoes (Solanum tuberosum), tomatoes (Lycopersicon esculentum), and jimson weed (Datura stramonium) seeds.

    PubMed

    Friedman, Mendel

    2004-10-29

    Potatoes and tomatoes, members of the Solanaceae plant family, serve as major, inexpensive low-fat food sources providing for energy, high-quality protein, fiber, vitamins, pigments, as well as other nutrients. These crops also produce biologically active secondary metabolites, which may have both adverse and beneficial effects in the diet. This limited overview, based largely on our studies with the aid of HPLC, TLC, ELISA, GC-MS, and UV spectroscopy, covers analytical aspects of two major potato trisaccharide glycoalkaloids, alpha-chaconine and alpha-solanine, and their hydrolysis products (metabolites) with two, one, and zero carbohydrate groups; the potato water-soluble nortropane alkaloids calystegine A3 and B2; the principal potato polyphenolic compound chlorogenic acid; potato inhibitors of digestive enzymes; the tomato tetrasaccharide glycoalkaloids dehydrotomatine and alpha-tomatine and hydrolysis products; the tomato pigments beta-carotene, lycopene, and chlorophyll; and the anticholinergic alkaloids atropine and scopolamine present in Datura stramonium (jimson weed) seeds that contaminate grain and animal feed. Related studies by other investigators are also mentioned. Accurate analytical methods for these food ingredients help assure the consumer of eating a good-quality and safe diet.

  15. Actinobacteria Isolated from an Underground Lake and Moonmilk Speleothem from the Biggest Conglomeratic Karstic Cave in Siberia as Sources of Novel Biologically Active Compounds

    PubMed Central

    Tokovenko, Bogdan T.; Protasov, Eugeniy S.; Gamaiunov, Stanislav V.; Rebets, Yuriy V.; Luzhetskyy, Andriy N.; Timofeyev, Maxim A.

    2016-01-01

    Actinobacteria isolated from unstudied ecosystems are one of the most interesting and promising sources of novel biologically active compounds. Cave ecosystems are unusual and rarely studied. Here, we report the isolation and characterization of ten new actinobacteria strains isolated from an ancient underground lake and moonmilk speleothem from the biggest conglomeratic karstic cave in Siberia with a focus on the biological activity of the obtained strains and the metabolite dereplication of one active strain. Streptomyces genera isolates from moonmilk speleothem demonstrated antibacterial and antifungal activities. Some of the strains were able to inhibit the growth of pathogenic Candida albicans. PMID:26901168

  16. Actinobacteria Isolated from an Underground Lake and Moonmilk Speleothem from the Biggest Conglomeratic Karstic Cave in Siberia as Sources of Novel Biologically Active Compounds.

    PubMed

    Axenov-Gribanov, Denis V; Axenov-Gibanov, Denis V; Voytsekhovskaya, Irina V; Tokovenko, Bogdan T; Protasov, Eugeniy S; Gamaiunov, Stanislav V; Rebets, Yuriy V; Luzhetskyy, Andriy N; Timofeyev, Maxim A

    2016-01-01

    Actinobacteria isolated from unstudied ecosystems are one of the most interesting and promising sources of novel biologically active compounds. Cave ecosystems are unusual and rarely studied. Here, we report the isolation and characterization of ten new actinobacteria strains isolated from an ancient underground lake and moonmilk speleothem from the biggest conglomeratic karstic cave in Siberia with a focus on the biological activity of the obtained strains and the metabolite dereplication of one active strain. Streptomyces genera isolates from moonmilk speleothem demonstrated antibacterial and antifungal activities. Some of the strains were able to inhibit the growth of pathogenic Candida albicans.

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

    PubMed

    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.

  18. 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.

    PubMed

    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.

  19. Topoisomerase inhibition, nucleolytic and electrolytic contribution on DNA binding activity exerted by biological active analogue of coordination compounds.

    PubMed

    Patel, Mohan N; Bhatt, Bhupesh S; Dosi, Promise A

    2012-04-01

    The neutral mononuclear copper complexes with the quinolone antibacterial drug ciprofloxacin and bipyridine derivatives have been synthesized and characterized. Complexes were screened for their antibacterial activity against three Gram((-)) and two Gram((+)) bacteria, and study suggests inhibition of gyrase activity by metal complexes as the possible mechanism. The nucleolytic activity of adducts was carried out on double stranded pUC19 DNA using gel electrophoresis in the presence of radical scavenging agents that suggest hydrolytic cleavage mechanism for plasmid DNA.

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

    PubMed

    Muruzović, Mirjana Ž; Mladenović, Katarina G; Stefanović, Olgica D; Vasić, Sava M; Čomić, Ljiljana R

    2016-07-01

    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. Copyright © 2016. Published by Elsevier B.V.

  1. Phosphorus-nitrogen compounds. Part 23: Syntheses, structural investigations, biological activities, and DNA interactions of new N/O spirocyclotriphosphazenes

    NASA Astrophysics Data System (ADS)

    Asmafiliz, Nuran; Kılıç, Zeynel; Hayvalı, Zeliha; Açık, Leyla; Hökelek, Tuncer; Dal, Hakan; Öner, Yağmur

    2012-02-01

    The Schiff base compounds ( 1 and 2) are synthesized by the condensation reactions of 2-furan-2-yl-methylamine with 2-hydroxy-3-methoxy- and 2-hydroxy-5-methoxy-benzaldehydes and reduced with NaBH 4 to give the new N/O-donor-type ligands ( 3 and 4). The monospirocyclotriphosphazenes containing 1,3,2-oxazaphosphorine rings ( 5 and 6) are prepared from the reactions of N 3P 3Cl 6 with 3 and 4, respectively. The reactions of 5 and 6 with excess pyrrolidine, morpholine, and 1,4-dioxa-8-azaspiro [4,5] decane (DASD) produce tetrapyrrolidino ( 5a and 6a), morpholino ( 5b and 6b), and 1,4-dioxa-8-azaspiro [4,5] deca ( 5c and 6c) spirocyclotriphosphazenes. The structural investigations of the compounds are examined by 1H, 13C, 31P NMR, DEPT, HSQC, and HMBC techniques. The solid-state structures of 5, 5a, and 6 are determined using X-ray crystallography. The compounds 5a, 5b, 5c, 6a, 6b, and 6c are subjected to antimicrobial activity against six patojen bacteria and two yeast strains. In addition, interactions between these compounds and pBR322 plasmid DNA are presented by agarose gel electrophoresis.

  2. Advances in Nutrigenomics research: novel and future analytical approaches to investigate the biological activity of natural compounds and food functions.

    PubMed

    García-Cañas, V; Simó, C; León, C; Cifuentes, A

    2010-01-20

    In recent years, nutrition research has moved from classical epidemiology and physiology to molecular biology and genetics. Following this trend, Nutrigenomics has emerged as a novel and multidisciplinary research field in nutritional science that aims to elucidate how diet can influence human health. It is already well known that bioactive food compounds can interact with genes affecting transcription factors, protein expression and metabolite production. The study of these complex interactions requires the development of advanced analytical approaches combined with bioinformatics. Thus, to carry out these studies Transcriptomics, Proteomics and Metabolomics approaches are employed together with an adequate integration of the information that they provide. In this article, an overview of the current methodologies and a thorough revision of the advances in analytical technologies and their possibilities for future developments and applications in the field of Nutrigenomics is provided.

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

    PubMed

    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.

  4. [Dietary bioactive compounds with potential in preventing pathologies related with overweight and obesity;biologically active peptides].

    PubMed

    Herrera Chalé, Francisco; Betancur Ancona, David; Segura Campos, Maira Rubi

    2014-01-01

    Overweight and obesity are risk factors for noncommunicable diseases such as cardiovascular diseases, diabetes and some types of cancer. The risk for these noncommunicable diseases increase with the increase in body mass index. Dietary proteins are known to carry a wide range of nutritional, functional and biological properties. Nutritionally, the proteins are a source of energy and amino acids, which are essential for growth and maintenance. Functionally, the proteins contribute to the physicochemical and sensory properties of various protein-rich foods. Furthermore, many dietary proteins possess specific biological properties which make these components potential ingredients of functional or health-promoting foods. Many of these properties are attributed to physiologically active peptides encrypted in protein molecules. This paper reviews antihypertensive, antithrombotic, hypocholesterolemic, hypoglycemic and hypolipidemic peptides originating from different sources and hydrolysis of proteins.

  5. Synthesis of novel biologically active heterocyclic compounds from 2-oxo-2H-benzopyran-6-yl-imidazolidine.

    PubMed

    Mulwad, Vinata V; Langi, Bhushan P; Chaskar, Atul C

    2011-01-01

    6-Aminocoumarin on treatment with oxalyl chloride gives coumarinyl-6-isocynate (1a-c) which on treatment with glycine gives 1H-3-[2'-oxo-2'H-benzopyran-6'-yl]-5-imidazolidine-2, 4-dione (2a-c). (2a-c) when refluxed with o-chlorobenzaldehyde, m-hydroxybenzaldehyde, 3,4-dimethoxybenzaldehyde and 3-nitrobenzaldehyde separately gives 1H-5-(2"-chlorobenzylidene)-3-(2'-oxo-2'H-benzopyran-6'-yl) imidazolidine-2,4-dione (3a-c), 1H-5-(3"-hydroxybenzylidene)-3-(2'-oxo-2'H-benzopyran-6'-yl) imidazolidine-2,4-dione (4a-c), 1H-5-(3",4"-dimethoxybenzylidene)-3-(2'-oxo-2'H-benzopyran-6'-yl) imidazolidine-2,4-dione (5a-c) and 1H-5-(3"-nitrobenzylidene)-3-(2'-oxo-2'H-benzopyran-6'-yl) imidazolidine-2,4-dione (6a-c), respectively. 3-(2"-Chlorophenyl)-3a,4-dihydro-6-(2'-oxo-2'H-benzopyran-6'-yl) imidazo[4,5-c]isoxazol-5-one 7a-c is obtained from (3a-c) and hydroxylamine hydrochloride while 2,3a,4-trihydro-3-(3"-hydroxyphenyl)-6-(2'-oxo-2'H-benzopyran-6'-yl) imidazo[4,5-c]pyrazol-5-one (8a-c) obtained by reaction of (4a-c) with hydrazine hydrate. Compound (5a-c) on treatment with urea gives 5,7-dihydro-2-hydroxy-6-(3",4"-dimethoxyphenyl)-9-(2'-oxo-2'H-benzopyran-6'-yl) purin-8-one (9a-c) and compound (6a-c) on treatment with thiourea gives 5,7-dihydro-2-mercapto-6-(3"-nitrophenyl)-9-(2'-oxo-2'H-benzopyran-6'-yl)purin-8-one (10a-c). The structures of the compounds have been established on the basis of spectral analytical data. All the compounds have been screened for their antimicrobial activities against three bacterial strains S. aureus, S. typhi and E. coli. Compounds 2b, 3b, 4b, 5b, 6b, 7b, 8b, 9b and 10b with the presence of methyl groups at C7' and C8' of coumarin moiety were found to be more active than others.

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

    PubMed

    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.

  7. Efficient Electrochemical N-Alkylation of N-Boc-Protected 4-Aminopyridines: Towards New Biologically Active Compounds

    PubMed Central

    Chiarotto, Isabella; Simonetti, Giovanna; Maes, Louis; De Vita, Daniela; Scipione, Luigi; Friggeri, Laura; Di Santo, Roberto; Tortorella, Silvano

    2014-01-01

    The use of electrogenerated acetonitrile anion allows the alkylation of N-Boc-4-aminopyridine in very high yields, under mild conditions and without by-products. The high reactivity of this base is due to its large tetraethylammonium counterion, which leaves the acetonitrile anion “naked.” The deprotection of the obtained compounds led to high yields in N-alkylated 4-aminopyridines. Nonsymmetrically dialkylated 4-aminopyridines were obtained by subsequent reaction of monoalkylated ones with t-BuOK and alkyl halides, while symmetrically dialkylated 4-aminopyridines were obtained by direct reaction of 4-aminopyridine with an excess of t-BuOK and alkyl halides. Some mono- and dialkyl-4-aminopyridines were selected to evaluate antifungal and antiprotozoal activity; the dialkylated 4-aminopyridines 3ac, 3ae and 3ff showed antifungal towards Cryptococcus neoformans; whereas 3cc, 3ee and 3ff showed antiprotozoal activity towards Leishmania infantum and Plasmodium falciparum. PMID:24955255

  8. Variations in the bioactive compounds composition and biological activities of loofah (Luffa cylindrica) fruits in relation to maturation stages.

    PubMed

    Hlel, Takoua Ben; Belhadj, Feten; Gül, Fatih; Altun, Muhammed; ŞahinYağlıoğlu, Ayşe; Demirtaş, Ibrahim; Nejib Marzouki, M

    2017-07-19

    The present work aimed to determine the antioxidant and antiproliferative potential of Luffa cylindrica fruits collected at two different maturation stages and to identify and compare their functional components composition. The methanolic extracts of L. cylindrica fruits harvested at 60 to 65 days after seeding (S1) and 85 to 90 days after seeding (S2) were investigated for their antioxidant activity using various assays. Furthermore, the antiproliferative activity of the extracts against HeLa human cervical cancer cells was explored with xCELLigence real time cell analyzer while the effect of the samples on the membrane integrity of the same cell line was assessed using LDH cytotoxicity leakage assay. Ultimately, the phytochemicals were analyzed using GCMS and HPLC/TOF-MS. The S1 sample had higher contents and more diversity in the phenolic compounds composition than S2. Furthermore, S1 extract showed the highest antioxidant and antiproliferative activity while S2 extract had higher cytotoxicity towards HeLa cells. The findings revealed that the time of harvest has a big impact on the phytochemicals content and activity and that harvesting L. cylindrica at an early stage before the beginning of the development of the cellulose fibrous system is recommended for a rich phytochemical composition and efficient antioxidant and antiproliferative activities. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

  9. Diazo Compounds: Versatile Tools for Chemical Biology.

    PubMed

    Mix, Kalie A; Aronoff, Matthew R; Raines, Ronald T

    2016-12-16

    Diazo groups have broad and tunable reactivity. That and other attributes endow diazo compounds with the potential to be valuable reagents for chemical biologists. The presence of diazo groups in natural products underscores their metabolic stability and anticipates their utility in a biological context. The chemoselectivity of diazo groups, even in the presence of azido groups, presents many opportunities. Already, diazo compounds have served as chemical probes and elicited novel modifications of proteins and nucleic acids. Here, we review advances that have facilitated the chemical synthesis of diazo compounds, and we highlight applications of diazo compounds in the detection and modification of biomolecules.

  10. Organometallic compounds: an opportunity for chemical biology?

    PubMed

    Patra, Malay; Gasser, Gilles

    2012-06-18

    Organometallic compounds are renowned for their remarkable applications in the field of catalysis, but much less is known about their potential in chemical biology. Indeed, such compounds have long been considered to be either unstable under physiological conditions or cytotoxic. As a consequence, little attention has been paid to their possible utilisation for biological purposes. Because of their outstanding physicochemical properties, which include chemical stability, structural diversity and unique photo- and electrochemical properties, however, organometallic compounds have the ability to play a leading role in the field of chemical biology. Indeed, remarkable examples of the use of such compounds-notably as enzyme inhibitors and as luminescent agents-have recently been reported. Here we summarise recent advances in the use of organometallic compounds for chemical biology purposes, an area that we define as "organometallic chemical biology". We also demonstrate that these recent discoveries are only a beginning and that many other organometallic complexes are likely to be found useful in this field of research in the near future.

  11. A Comprehensive Review on the Biological and Pharmacological Activities of Rhodanine Based Compounds for Research and Development of Drugs.

    PubMed

    Liu, Jiachun; Wu, Yan-Ling; Piao, Huri; Zhao, Xiaoyin; Zhang, Wen; Wang, Yanli; Liu, Minrui

    2016-09-28

    At present, diseases resulting from various reasons have been causing deadly fears to humans and previously incogitable losses to health. Meanwhile, the patient compliance has been weakening because of drug resistance and serious drug adverse effects. There is therefore an urgent need for the development of novel structural agents. Rhodanine derivatives have represented wide biological activities, as well as significant industrial applications, which suggests that rhodanine heterocycle represents a key structural motif in heterocyclic chemistry and occupies a prominent position in drug discovery. Here, we review some deadly defects of clinical medicines to the therapy of diseases and important advances on rhodanine derivatives in drug researches (e.g. as anti-diabetic, anti-viral, anti-inflammatory, anti-microbial, anti-tumor agents and inhibitors for Alzheimer Disease), indicating that rhodanine heterocycle could be used as a significant pharmacophore to develop novel pharmacological active molecules. It is believed that the review is helpful for new ideas and rational designs of more promising and less toxic drugs.

  12. Synthesis and biological activities of 2,3-dihydro-1,3,4-oxadiazole compounds and its derivatives as potential activator of ryanodine receptors.

    PubMed

    Zhou, Yunyun; Wang, Baolei; Di, Fengjuan; Xiong, Lixia; Yang, Na; Li, Yongqiang; Li, Yuxin; Li, Zhengming

    2014-05-15

    A series of novel 2,3-dihydro-1,3,4-oxadiazoles containing N-pyridylpyrazole carboxamides moieties were obtained by applying a new synthetic route. Their insecticidal tests against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) indicated that most of the compounds showed moderate to excellent activities at the testing concentrations. In particular, compound 6a showed 40% larvicidal activities against oriental armyworm at 1mg/L, while 7a against diamondback was 100% at 0.01mg/L. Calcium imaging results demonstrated that 6a, 6d and 7a stimulated a transient elevation in [Ca(2+)]i in the absence of external calcium after the central neurons dye loading with fluo-3 AM, implying that these novel compounds were potential activators of the ligand-gated calcium channel on the endoplasmic reticulum.

  13. Synthesis, Characterization, and Biological Activity Studies of Copper(II) Mixed Compound with Histamine and Nalidixic Acid

    PubMed Central

    Bivián-Castro, Egla Yareth; López, Mercedes G.; Pedraza-Reyes, Mario; Bernès, Sylvain; Mendoza-Díaz, Guillermo

    2009-01-01

    A mixed copper complex with deprotonated nalidixic acid (nal) and histamine (hsm) was synthesized and characterized by FTIR, UV-Vis, elemental analysis, and conductivity. The crystal structure of [Cu(hsm)(nal)H2O]Cl·3H2O (chn) showed a pentacoordinated cooper(II) in a square pyramidal geometry surrounded by two N atoms from hsm, two O atoms from the quinolone, and one apical water oxygen. Alteration of bacterial DNA structure and/or associated functions in vivo by [Cu(hsm)(nal)H2O]Cl·3H2O was demonstrated by the induction of a recA-lacZ fusion integrated at the amyE locus of a recombinant Bacillus subtilis strain. Results from circular dichroism and denaturation of calf thymus DNA (CT-DNA) suggested that increased amounts of copper complex were able to stabilize the double helix of DNA in vitro mainly by formation of hydrogen bonds between chn and the sugars of DNA minor groove. In vivo and in vitro biological activities of the chn complex were compared with the chemical nuclease [Cu(phen)(nal)H2O]NO3 · 3H2O (cpn) where phen is phenanthroline. PMID:19557138

  14. Use of the harmonic mean to the determination of dissociation constants of stereoisomeric mixtures of biologically active compounds.

    PubMed

    Guevara-Salazar, J Alberto; Quintana-Zavala, Delia; Jiménez-Vázquez, Hugo A; Trujillo-Ferrara, José

    2014-12-01

    Herein we introduce the derivation of a mathematical expression to evaluate the dissociation constant of a mixture of stereoisomers in equal amounts (KdMIX), when the corresponding dissociation constants (Kd) or medium response (MR50) of the pure stereoisomers are known; the final equation takes the form of the harmonic mean. In order to validate the equation, we carried out a bibliographic search of experimental data of enantiomeric molecules with biological activity, considering the Kd's or MR50's of the isolated enantiomers as well as that of the racemate. The comparisons between the experimental dissociation constants of the mixtures (KdEXP or MR50EXP) and the calculated values (KdMIX or MR50MIX) were consistent; the similarity between these values is supported through statistical analyses of group comparison and simple linear correlation. The equation we obtained, which corresponds to the harmonic mean, was used to predict the values of KdMIX (or MR50MIX) or Kd (or MR50) in systems when only two of the experimental values are known: either the dissociation constants of both enantiomers or the Kd (or MR50) of one of the enantiomers and dissociation constant of the racemate.

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

    PubMed

    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 < 0.01) and CH3SH (P < 0.05) and population yields at the end of the experiments (P < 0.001) compared to placebo and positive control. The in vitro flat-bed perfusion model may be used to replicate many of

  16. Raw and biologically treated paper mill wastewater effluents and the recipient surface waters: Cytotoxic and genotoxic activity and the presence of endocrine disrupting compounds.

    PubMed

    Balabanič, Damjan; Filipič, Metka; Krivograd Klemenčič, Aleksandra; Žegura, Bojana

    2017-01-01

    Paper mill effluents are complex mixtures containing different toxic compounds including endocrine-disrupting (EDCs) and genotoxic compounds. In the present study non-concentrated raw and biologically treated wastewaters from two paper mill plants with different paper production technologies i) Paper mill A uses virgin fibres, and ii) Paper mill B uses recycled fibres for paper production and the corresponding receiving surface waters, were assessed for their cytotoxic/genotoxic activity with SOS/umuC, Ames MPF 98/100 Aqua, and comet assay with human hepatoma HepG2 cells. In addition the levels of seven selected EDCs were quantified in wastewater samples and receiving surface waters. All investigated EDCs were confirmed in raw and biologically treated effluents from both paper mills with concentrations being markedly higher in Paper mill B effluents. In the receiving surface waters three of the studied EDCs were determined downstream of both paper mills effluent discharge. The wastewater samples and the recipient surface water samples from Paper mill A were not mutagenic for bacteria and did not induce DNA damage in HepG2 cells. On the contrary, half of the raw wastewater samples from Paper mill B were mutagenic whereas biologically treated wastewater and the recipient surface water samples were negative. In HepG2 cells most of the raw and biologically treated wastewater samples from Paper mill B as well as surface water samples collected downstream of Paper mill B effluent discharge induced DNA damage. The results confirmed that genotoxic contaminants were present only in wastewaters from Paper mill B that uses recycled fibres for paper production, and that the combined aerobic and anaerobic wastewater treatment procedure efficiently reduced contaminants that are bacterial mutagens, but not those that induce DNA damage in HepG2 cells. This study highlights that in addition to chemical analyses bioassays are needed for a comprehensive toxicological evaluation of

  17. A review exploring biological activities of hydrazones

    PubMed Central

    Verma, Garima; Marella, Akranth; Shaquiquzzaman, Mohammad; Akhtar, Mymoona; Ali, Mohammad Rahmat; Alam, Mohammad Mumtaz

    2014-01-01

    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. PMID:24741273

  18. The influence of the organic matter of sewage sediments on biological activity of microorganisms which carry out the transformations of carbon and nitrogen compounds.

    PubMed

    Pisarek, Izabella; Grata, Katarzyna

    2013-01-01

    Soil microorganisms play an important role in the organic matter transformation process. The soil microorganisms also are in symbiotic relationship with plants. At the same time, soil microorganisms are sensitive to both anthropogenic and natural habitat changes. Particular characteristics of organic matter (the C:N relation, pH, the content the content of assimilated nutrients, the xenobiotics etc.) modify the biotic conditions of the soils. This particularly concerns the microorganisms which carry out the changes in the mineral and organic nitrogen compounds and the transformation of the external organic matter. The first aim of this work was to assess the influence of the sewage sediments and the manure on the phytosanitary potential of the soil environment. The second aim of this article was to estimate the number and activity of microorganisms which carry out the transformation of carbon and nitrogen compounds. This work showed the stimulating effect of the external organic matter both on the number and on the activity of most of the physiological groups. The manure mainly stimulated ammonificators, amylolitic microorganisms and Azotobacter sp. The sewage sediments mainly stimulated ammonificators, nitrifiers of I phase and cellulolytic microorganisms. The statistically significant impact of the physio-chemical soil habitat on the biological activity of the analyzed groups of microbes was also noted.

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

    PubMed

    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.

  20. Validated comprehensive analytical method for quantification of coenzyme A activated compounds in biological tissues by online solid-phase extraction LC/MS/MS.

    PubMed

    Magnes, Christoph; Suppan, Maria; Pieber, Thomas R; Moustafa, Tarek; Trauner, Michael; Haemmerle, Guenter; Sinner, Frank M

    2008-08-01

    We report a robust, reliable, and comprehensive analytical method for the identification and quantification of the entire class of coenzyme A (CoA) activated substances, particularly short-, medium-, and long-chain acyl-CoAs derived from various biological tissues. This online SPE-LC/MS/MS-based method is characterized by a simple three-step sample preparation: (1) addition of buffer, organic solvents, and internal standards; (2) homogenization; and (3) centrifugation. The supernatant is injected directly into the SPE-LC/MS/MS system. Identification of CoA activated compounds is performed by accurate mass determination within the HPLC run. Method validation for short-, medium-, and long-chain acyl-CoA fatty acids revealed excellent quality. Accuracy was found to be between 87 and 107% and precision was between 0.1 and 12.8% in mouse skeletal muscle. The lower limit of quantification for all investigated compounds was well below 3.1% of estimated physiological levels in 200 mg of mouse tissue. Comparable results were obtained for mouse liver, mouse brown white adipose tissue and rat liver. For all investigated tissues, no matrix effect was observed.

  1. Fatty acids, coumarins and polyphenolic compounds of Ficus carica L. cv. Dottato: variation of bioactive compounds and biological activity of aerial parts.

    PubMed

    Marrelli, Mariangela; Statti, Giancarlo A; Tundis, Rosa; Menichini, Francesco; Conforti, Filomena

    2014-01-01

    Leaves, bark and woody part of Ficus carica L. cultivar Dottato collected in different months were examined to assess their chemical composition, antioxidant activity and phototoxicity on C32 human melanoma cells after UVA irradiation. The phytochemical investigation revealed different composition in the coumarin, fatty acid, polyphenol and flavonoid content. The second harvest of leaves and the first harvest of the bark possessed the highest antiradical activity with IC50 values of 64.00 ± 0.59 and 67.00 ± 1.09 μg/mL, respectively. Harvest III of leaves showed the best inhibition of lipid peroxidation (IC50 = 1.48 ± 0.04 μg/mL). Leaf samples of F. carica showed also the best antiproliferative activity in comparison with bark and woody part of F. carica.

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

    PubMed

    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. Copyright © 2014 Elsevier Ltd. All rights reserved.

  3. Skin-mimetic chromatography for prediction of human percutaneous absorption of biologically active compounds occurring in medicinal plant extracts.

    PubMed

    Stepnik, Katarzyna; Malinowska, Irena

    2017-04-01

    The main aim of this study was to predict quantitatively human percutaneous absorption of chosen compounds commonly occurring in plants which can be used as medicinal extracts in the drug and beauty industries. The most important human percutaneous descriptors, i.e. logKp (logarithm of the water/skin partition coefficient) and logJmax (logarithm of the maximum flux of solutes penetrating the skin), of fatty acids and polyphenols were determined using both in vitro and in silico methods. For in vitro determination of human percutaneous absorption, micellar liquid chromatography based on hexadecyltrimethylammonium bromide, sodium dodecyl sulfate and polyoxyethylene (23) lauryl ether (Brij35) was used. Human percutaneous absorption was characterized by entirely new QSAR/QRAR models based on retention, lipophilic, steric and electronic data as well as on the linear free energy relationship parameters. Many different correlations between human skin absorption and different physicochemical parameters were performed, e.g. the in silico estimated logKp value was correlated with the retention parameter logkw (logarithm of the retention factor extrapolated to pure water) from the systems imitating a cutaneous environment (R(2)  = 0.92). Moreover, the influence of lipophilicity on percutaneous absorption was examined. The obtained correlation was excellent (R(2)  = 0.95).

  4. 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.

    PubMed

    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.

  5. In vitro biological activities of seed essential oils from the Cameroonian spices Afrostyrax lepidophyllus MILDBR. and Scorodophloeus zenkeri HARMS rich in sulfur-containing compounds.

    PubMed

    Fogang, Hervet P D; Maggi, Filippo; Tapondjou, Léon A; Womeni, Hilaire M; Papa, Fabrizio; Quassinti, Luana; Bramucci, Massimo; Vitali, Luca A; Petrelli, Dezemona; Lupidi, Giulio; Vittori, Sauro; Barboni, Luciano

    2014-01-01

    The chemical composition of the essential oils obtained from the seeds of bush onion (Afrostyrax lepidophyllus) and tropical garlic tree (Scorodophloeus zenkeri), plants used as spices in the traditional African cuisine, was determined by GC-FID and GC/MS analyses. Moreover, in vitro biological properties of the oils, namely, the cytotoxic, antioxidant, and antimicrobial activities, were investigated by the MTT, the DPPH(.) and ABTS(.+) scavenging, and the agar disc-diffusion methods, respectively. Both oils were composed mainly by S-containing compounds, accounting for 91.0-96.1% of the total oil compositions, which provided them the typical garlic- and onion-like odors of spices. The predominant compound in both oils, 2,4,5,7-tetrathiaoctane (1; 51.5-52.9%), was isolated by preparative TLC and structurally elucidated by (1) H- and (13) C-NMR data. The oils exhibited a strong inhibitory effect on the growth of human cancer cells, namely, T98G (human glioblastoma multiforme cell line), MDA-MB 231 (human breast adenocarcinoma cell line), A375 (human malignant melanoma cell line), and HCT116 (human colon carcinoma cell line) cells, and a good DPPH(.) - and ABTS(.+) -scavenging activity, while the antimicrobial effects were negligible. The volatile compositions of A. lepidophyllus and S. zenkeri oils supported their use as odorous spices. The significant inhibition activities detected make these oils worthy of further investigation as promising chemopreventive agents to be exploited in the African pharmaceutical market. Copyright © 2014 Verlag Helvetica Chimica Acta AG, Zürich.

  6. Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies.

    PubMed

    Simic, Milena; Paunovic, Nikola; Boric, Ivan; Randjelovic, Jelena; Vojnovic, Sandra; Nikodinovic-Runic, Jasmina; Pekmezovic, Marina; Savic, Vladimir

    2016-01-01

    A series of novel 3-substituted isocoumarins was prepared via Pd-catalysed coupling processes and screened in vitro for antifungal activity against Candida species. The study revealed antifungal potential of isocoumarins possessing the azole substituents, which, in some cases, showed biological properties equal to those of clinically used voriconazole. Selected compounds were also screened against voriconazole resistant Candida krusei 6258 and a clinical isolate Candida parapsilosis CA-27. Although the activity against these targets needs to be improved further, the results emphasise additional potential of this new class of antifungal compounds. Copyright © 2015 Elsevier Ltd. All rights reserved.

  7. Metadata Activities in Biology

    SciTech Connect

    Inigo, Gil San; HUTCHISON, VIVIAN; Frame, Mike; Palanisamy, Giri

    2010-01-01

    The National Biological Information Infrastructure program has advanced the biological sciences ability to standardize, share, integrate and synthesize data by making the metadata program a core of its activities. Through strategic partnerships, a series of crosswalks for the main biological metadata specifications have enabled data providers and international clearinghouses to aggregate and disseminate tens of thousands of metadata sets describing petabytes of data records. New efforts at the National Biological Information Infrastructure are focusing on better metadata creation and curation tools, semantic mediation for data discovery and other curious initiatives.

  8. Preparation and characterization of a new harmine-based antiproliferative compound in complex with cyclodextrin: Increasing solubility while maintaining biological activity.

    PubMed

    Meinguet, Céline; Masereel, Bernard; Wouters, Johan

    2015-09-18

    The trisubstituted harmine derivative, 2, present a submicromolar antiproliferative activity on 5 cancer cell lines but a moderate kinetic solubility in pH 7.4 buffer. The aim of this work was to develop a 2-cyclodextrin complex in order to increase the drug solubility while maintaining the biological activity. Firstly, the 2 increasing solubility in presence of several cyclodextrins (CDs) has been shown, with a maximum for 7 glucose subunit CD (βCD and 2 HP-βCD). Phase solubility experiment in presence of 2 HP-βCD has underline an AL-type profile until 80 mM which suggest a 1:1 stoichiometry and a K1:1 of 116 M(-1) and a CE of 0.28 have been calculated. This 1:1 stoichiometry was confirmed by Job Plot experiment, following the CD H-3 proton by (1)H NMR. Secondly, (1)H NMR study of compound 2 in presence of βCD and geometry optimization of the complex has underline an inclusion of 2 into the CD, via the indole part of the drug. Finally, the efficiency of the 2 antiproliferative effect is not affected by the complexation, as shown by viability test.

  9. A convenient synthesis and biological activity of novel thieno[2,3-c]pyrazole compounds as antimicrobial and anti-inflammatory agents.

    PubMed

    El-Dean, Adel M Kamal; Zaki, Remon M; Abdulrazzaq, Abdullah Y

    2015-01-01

    A new method for synthesizing 4-amino-3-methyl-1-phenyl-1H-5-substituted thieno[2,3-c]pyrazole was reported. The substituted groups at position 5 include carbonitrile, carboxamide, N-phenyl carboxamide, and benzoyl groups. The newly synthesized compounds and their derivatives were characterized by elemental analysis and spectroscopy (IR, 1H NMR, and mass spectra). Furthermore, some of these synthesized compounds were screened against various pathogenic bacterial and fungal strains. The results demonstrate that most of the synthesized compounds possess a significant antibacterial activity against gram-positive and gram-negative bacteria. In addition, most of these compounds showed a remarkable anti-fungal activity. On the other hand, some of the synthesized compounds possess high anti-inflammatory activity, which was demonstrated using the carrageenan-induced rat paw edema assay.

  10. Shapeshifting photoswitchable azobenzene compounds and their biological applications

    NASA Astrophysics Data System (ADS)

    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.

  11. 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.

    PubMed

    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.

  12. [Biologically active metabolites of the marine actinobacteria].

    PubMed

    Sobolevskaia, M P; Kuznetsova, T A

    2010-01-01

    This review systematically data on the chemical structure and biological activity of metabolites of obligate and facultative marine actinobacteria, published from 2000 to 2007. We discuss some structural features of the five groups of metabolites related to macrolides and compounds containing lactone, quinone and diketopiperazine residues, cyclic peptides, alkaloids, and compounds of mixed biosynthesis. Survey shows a large chemical diversity of metabolites actinobacteria isolated from marine environment. It is shown that, along with metabolites, identical to previously isolated from terrestrial actinobacteria, marine actinobacteria synthesize unknown compounds not found in other natural sources, including micro organisms. Perhaps the biosynthesis of new chemotypes bioactive compounds in marine actinobacteria is one manifestation of chemical adaptation of microorganisms to environmental conditions at sea. Review stresses the importance of the chemical study of metabolites of marine actinobacteria. These studies are aimed at obtaining new data on marine microorganisms producers of biologically active compounds and chemical structure and biological activity of new low-molecular bioregulators of natural origin.

  13. Biological activity of ionene polymers

    NASA Technical Reports Server (NTRS)

    Rembaum, A.

    1973-01-01

    Ionene polymers are polyammonium salts with positive nitrogens in the backbone, resulting from the polycondensation of diamines with dihalides or from the polycondensation of halo amines. The mechanism of formation of ionene polymers of different structures and their biological activity is reviewed. The antimicrobial and antifungal properties are compared with low molecular weight ammonium salts. Ionenes were found to combine with DNA by means of ionic bonds to yield similar complexes to those obtained with polyamines (spermine and spermidine). They also combine with nerve cell receptors and exercise a more powerful and longer duration ganglionic blocking action than their monomeric analogs. The antiheparin activity of ionenes and the thromboresistance of elastomeric ionene heparin coatings is described. The enhanced biological activity of ionenes as compared with low molecular weight compounds is attributed to a cooperative effect of a large number of positive charges on the polymeric chains.

  14. Biological activity of ionene polymers

    NASA Technical Reports Server (NTRS)

    Rembaum, A.

    1973-01-01

    Ionene polymers are polyammonium salts with positive nitrogens in the backbone, resulting from the polycondensation of diamines with dihalides or from the polycondensation of halo amines. The mechanism of formation of ionene polymers of different structures and their biological activity is reviewed. The antimicrobial and antifungal properties are compared with low molecular weight ammonium salts. Ionenes were found to combine with DNA by means of ionic bonds to yield similar complexes to those obtained with polyamines (spermine and spermidine). They also combine with nerve cell receptors and exercise a more powerful and longer duration ganglionic blocking action than their monomeric analogs. The antiheparin activity of ionenes and the thromboresistance of elastomeric ionene heparin coatings is described. The enhanced biological activity of ionenes as compared with low molecular weight compounds is attributed to a cooperative effect of a large number of positive charges on the polymeric chains.

  15. The computational design of test compounds with potentially specific biological activity: Histamine-H2 agonists derived from 5-HT/H2 antagonists

    NASA Astrophysics Data System (ADS)

    Topiol, Sid; Sabio, Michael

    1991-06-01

    The previously proposed models for the recognition and activation of 5-HT and histamine-H2 receptors, which were employed to explain the antagonist activity of LSD at both of these receptors, as well as the selective antagonism for H2 receptors by SKF-10856 and 9,10-dihydro-LSD, are used herein to design a compound to test the H2-receptor model. The design strategy attempts to construct a compound with potentially selective H2 agonism. The design scheme maintains features which were previously used to explain selective recognition of SKF-10856 and 9,10-dihydro-LSD as well as reintroduces the chemical features proposed to be responsible for H2 activation. The existence of the H2 recognition and activation features in the proposed compound is verified, in a previously proposed model, by computational studies of the molecular electrostatic potentials and shifts in the tautomeric preference.

  16. Molecular characteristics versus biological activity

    USGS Publications Warehouse

    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.

  17. Human biological monitoring of suspected endocrine-disrupting compounds

    PubMed Central

    Faniband, Moosa; Lindh, Christian H; Jönsson, Bo AG

    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. PMID:24369128

  18. Molybdenum: biological activity and metabolism.

    PubMed

    Mendel, Ralf R

    2005-11-07

    Molybdenum and tungsten are available to all organisms, with molybdenum having the far greater abundance and availability. Molybdenum occurs in a wide range of metalloenzymes in bacteria, fungi, algae, plants and animals, while tungsten was found to be essential only for a limited range of bacteria. In order to gain biological activity, molybdenum has to be complexed by a pterin compound, thus forming a molybdenum cofactor. In this article I will review the way that molybdenum takes from uptake into the cell, via formation of the molybdenum cofactor and its storage, to the final modification of molybdenum cofactor and its insertion into apo-metalloenzymes.

  19. Aurones: interesting natural and synthetic compounds with emerging biological potential.

    PubMed

    Zwergel, Clemens; Gaascht, François; Valente, Sergio; Diederich, Marc; Bagrel, Denyse; Kirsch, Gilbert

    2012-03-01

    Aurones [2-benzylidenebenzofuran-3(2H)-ones] are either natural or synthetic compounds, belonging to the flavonoid family. They are isomeric to flavones and provide a bright yellow color to the plants in which they occur. Today, a literature survey indicates that the related flavonoids have been studied not only for their physiological properties and effects on Nature, but also for their therapeutic potential. Aurones are recently attracting the interest of an increasing number of research groups, and, since the last review, some interesting advances have been made in understanding the aurones. In this review, we report the recent advances made on the synthetic routes towards aurones. We also highlight their activity in different biological areas, as well as applied genetic plant modifications to produce these colored compounds. Their synthesis, structure-activity relationships and the importance of the substitution pattern will also be mentioned. Finally, some aspects regarding the possible development of aurones will be discussed briefly.

  20. [Biological activity of Spirulina].

    PubMed

    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.

  1. Biological Mimics: A New Paradigm in the Detection of Toxic Compounds

    ERIC Educational Resources Information Center

    Monty, Chelsea Nicole

    2009-01-01

    The purpose of this thesis is to introduce a new idea: using biological mimics in the detection of toxic compounds. Biological mimics imitate the active site of a given enzyme or have catalytic chemistry similar to enzymes and can be used in place of biological molecules to provide longer stability and simpler operation. In the following text the…

  2. Biological Mimics: A New Paradigm in the Detection of Toxic Compounds

    ERIC Educational Resources Information Center

    Monty, Chelsea Nicole

    2009-01-01

    The purpose of this thesis is to introduce a new idea: using biological mimics in the detection of toxic compounds. Biological mimics imitate the active site of a given enzyme or have catalytic chemistry similar to enzymes and can be used in place of biological molecules to provide longer stability and simpler operation. In the following text the…

  3. Partial characterization of bacteriocin-like compounds from two strains of Bacillus cereus with biological activity against Paenibacillus larvae, the causal agent of American Foulbrood disease.

    PubMed

    Minnaard, J; Alippi, A M

    2016-12-01

    American Foulbrood (AFB), caused by the spore-forming Gram-positive bacterium Paenibacillus larvae, is the most severe bacterial disease affecting honeybees worldwide. Two bacterial isolates showing specific inhibitory activity against P. larvae were identified as Bacillus cereus by 16S rDNA sequencing. Antagonistic compounds were obtained from cell-free supernatants of strains m6c and m387 growing on Trypticase Soy Broth and concentrated by NH4 SO4 precipitation, ultrafiltration and butanol extraction. Both compounds were characterized as bacteriocin-like inhibitory substances (BLIS). BLISm6c and BLISm387 were stable at 70°C for 30 min and active in the pH range from 3 to 7. The antibacterial activity was completely lost at pH values higher than 8 or temperatures >80°C. Both BLIS have a narrow activity range and highly inhibit the growth of P. larvae. BLISm6c and BLISm387 differ from each other and other BLIS reportedly produced by B. cereus with regard to their molecular weights, antibacterial activity, minimal inhibitory concentration values and sensitivity to degradative enzymes. The findings of this study suggest that BLISm6c and BLISm387 can potentially be used to control AFB. An Integrated Pest Management (IPM) approach is needed to ensure the sustainability of the beekeeping industry due to the increasing demand for organic honey and the reduction of dependence on antibiotics. Biocontrol agents produced by bacteria isolated from apiarian sources seem promising and able to combine with an IPM strategy. The most significant findings of this study are the characterization of bacteriocin-like compounds (BLIS) obtained from two strains of Bacillus cereus isolated from honey. Both BLIS have a narrow activity range and highly inhibit the growth of Paenibacillus larvae, the causal agent of American Foulbrood disease of honey bees. © 2016 The Society for Applied Microbiology.

  4. Active Biological Materials

    NASA Astrophysics Data System (ADS)

    Fletcher, Daniel A.; Geissler, Phillip L.

    2009-05-01

    Cells make use of dynamic internal structures to control shape and create movement. By consuming energy to assemble into highly organized systems of interacting parts, these structures can generate force and resist compression, as well as adaptively change in response to their environment. Recent progress in reconstituting cytoskeletal structures in vitro has provided an opportunity to characterize the mechanics and dynamics of filament networks formed from purified proteins. Results indicate that a complex interplay between length scales and timescales underlies the mechanical responses of these systems and that energy consumption, as manifested in molecular motor activity and cytoskeletal filament growth, can drive transitions between distinct material states. This review discusses the basic characteristics of these active biological materials that set them apart from conventional materials and that create a rich array of unique behaviors.

  5. Physicochemical properties and biological activity: thermodynamic properties of compounds related to acetylcholine assessed from depression of freezing-point and enthalpies of dilution.

    PubMed

    Barlow, R B

    1974-07-01

    1 Measurements have been made of the osmotic coefficients and enthalpies of dilution of acetylcholine and of compounds related to it in which the carbonyl and ether groups have been replaced by methylene and the trimethylammonium group by triethylammonium. All were iodides. Measurements were also made with tetraethylammonium iodide and agree with published values.2 Where necessary the affinities of the compounds for acetylcholine receptors in the guinea-pig ileum and frog rectus, or their activities relative to acetylcholine, have been measured.3 The osmotic coefficients were used to calculate activity coefficients and excess free energies, which have been used with the excess enthalpies to calculate the excess entropies of the solutions. These indicate that the ester and carbonyl groups have a marked ordering effect on the ions in water compared with methylene groups; the ether group has an intermediate effect.4 When the results are interpreted in terms of ion-pair formation they can be used to calculate the ion-association constants and enthalpies and entropies of formation of ion-pairs, and lead to similar conclusions: that the order associated with ion-pair formation is greater with the esters and ketones. There appears to be extensive ion-association in the concentrations (0.5 to 1M) usually used in n.m.r. studies.5 There is no obvious correlation between the effects of groups on water and their activity or affinity at muscarine-sensitive acetylcholine receptors but it is possible that ability to activate nicotine-sensitive receptors may be associated with an increase in order, though it would be necessary to study entropy changes in systems actually involving receptors in order to prove this. It is also necessary to suppose that ability to activate these receptors is limited to compounds with small onium groups.

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

    PubMed

    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.

  7. Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.

    PubMed

    Watarai, Yusuke; Ishizawa, Michiyasu; Ikura, Teikichi; Zacconi, Flavia C M; Uno, Shigeyuki; Ito, Nobutoshi; Mouriño, Antonio; Tokiwa, Hiroaki; Makishima, Makoto; Yamada, Sachiko

    2015-12-24

    Novel 19-norvitamin D analogues (ADYW1-4, 5a-d) in which an adamantyl diyne side chain is attached directly to the 17-position of the D ring are designed and stereoselectively synthesized. The adamantane ring of these analogues was expected to interfere with helix 12 (H12, activation function 2) of the vitamin D receptor (VDR) to modulate its activities. The analogue 5b binds to the VDR (7% of the natural hormone) and shows significant partial agonistic activity in transactivation assay. Compound 5b showed considerable selectivity in VDR target genes expressions in vitro, it was taken up by target cells 2-3 times more readily, and its lifetime was three times longer than the natural hormone. The X-ray crystal structure of 5b in complex with VDR reveals that the ligand binds similarly to the natural hormone, but the diyne moiety is slightly bent (angles around the diyne 5° to 8°) with respect to the original diyne vitamin D compound 6 in VDR (<1°) due to steric hindrance with helix 12.

  8. 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.

    PubMed

    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.

  9. Formation and distribution of 2,4-dihydroxy-2,5-dimethyl-3(2H)-thiophenone, a pigment, an aroma and a biologically active compound formed by the Maillard reaction, in foods and beverages.

    PubMed

    Furusawa, Rina; Goto, Chiaki; Satoh, Miki; Nomi, Yuri; Murata, Masatsune

    2013-07-01

    We recently identified 2,4-dihydroxy-2,5-dimethyl-3(2H)-thiophenone (DHDMT) from soy sauce as a low-molecular-weight pigment formed by the Maillard reaction. DHDMT has also been reported as an aroma compound in a model system and a biologically active compound of heated garlic. To utilize these functions efficiently, we here examined how DHDMT was formed during fermentation of soy sauce and in model systems. Although DHDMT was formed from cysteine and glucose, it was formed more from cystine and fructose in the model system. We also showed that this compound exists in various kinds of soy sauce and miso as well as in some brown foods and beverages such as roasted bread and beer.

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

    PubMed

    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.

  11. Biological spectra analysis: Linking biological activity profiles to molecular structure

    PubMed Central

    Fliri, Anton F.; Loging, William T.; Thadeio, Peter F.; Volkmann, Robert A.

    2005-01-01

    Establishing quantitative relationships between molecular structure and broad biological effects has been a longstanding challenge in science. Currently, no method exists for forecasting broad biological activity profiles of medicinal agents even within narrow boundaries of structurally similar molecules. Starting from the premise that biological activity results from the capacity of small organic molecules to modulate the activity of the proteome, we set out to investigate whether descriptor sets could be developed for measuring and quantifying this molecular property. Using a 1,567-compound database, we show that percent inhibition values, determined at single high drug concentration in a battery of in vitro assays representing a cross section of the proteome, provide precise molecular property descriptors that identify the structure of molecules. When broad biological activity of molecules is represented in spectra form, organic molecules can be sorted by quantifying differences between biological spectra. Unlike traditional structure–activity relationship methods, sorting of molecules by using biospectra comparisons does not require knowledge of a molecule's putative drug targets. To illustrate this finding, we selected as starting point the biological activity spectra of clotrimazole and tioconazole because their putative target, lanosterol demethylase (CYP51), was not included in the bioassay array. Spectra similarity obtained through profile similarity measurements and hierarchical clustering provided an unbiased means for establishing quantitative relationships between chemical structures and biological activity spectra. This methodology, which we have termed biological spectra analysis, provides the capability not only of sorting molecules on the basis of biospectra similarity but also of predicting simultaneous interactions of new molecules with multiple proteins. PMID:15625110

  12. Synthesis and spectroscopic studies of biologically active compounds derived from oxalyldihydrazide and benzil, and their Cr(III), Fe(III) and Mn(III) complexes.

    PubMed

    Singh, D P; Kumar, Ramesh; Singh, Jitender

    2009-04-01

    A new series of complexes have been synthesized by template condensation of oxalyldihydrazide and benzil in methanolic medium in the presence of trivalent chromium, manganese and iron salts forming complexes of the type [M(C(32)H(24)N(8)O(4))X]X(2) where M = Cr(III), Mn(III), Fe(III) and X = Cl(-1), NO(3)(-1), CH(3)COO(-1). The complexes have been characterized with the help of elemental analyses, conductance measurements, magnetic susceptibility measurements, electronic, NMR, infrared and far infrared spectral studies. On the basis of these studies, a five coordinate square pyramidal geometry has been proposed for all these complexes. The biological activities of the metal complexes have been tested in vitro against a number of pathogenic bacteria to assess their inhibiting potential. Some of these complexes have been found to exhibit remarkable antibacterial activities.

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

    PubMed

    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.

  14. Discovery and characterization of a novel lachrymatory factor synthase in Petiveria alliacea and its influence on alliinase-mediated formation of biologically active organosulfur compounds.

    PubMed

    Musah, Rabi A; He, Quan; Kubec, Roman

    2009-11-01

    A novel lachrymatory factor synthase (LFS) was isolated and purified from the roots of the Amazonian medicinal plant Petiveria alliacea. The enzyme is a heterotetrameric glycoprotein comprised of two alpha-subunits (68.8 kD each), one gamma-subunit (22.5 kD), and one delta-subunit (11.9 kD). The two alpha-subunits are glycosylated and connected by a disulfide bridge. The LFS has an isoelectric point of 5.2. It catalyzes the formation of a sulfine lachrymator, (Z)-phenylmethanethial S-oxide, only in the presence of P. alliacea alliinase and its natural substrate, S-benzyl-l-cysteine sulfoxide (petiveriin). Depending on its concentration relative to that of P. alliacea alliinase, the LFS sequesters, to varying degrees, the sulfenic acid intermediate formed by alliinase-mediated breakdown of petiveriin. At LFS:alliinase of 5:1, LFS sequesters all of the sulfenic acid formed by alliinase action on petiveriin, and converts it entirely to (Z)-phenylmethanethial S-oxide. However, starting at LFS:alliinase of 5:2, the LFS is unable to sequester all of the sulfenic acid produced by the alliinase, with the result that sulfenic acid that escapes the action of the LFS condenses with loss of water to form S-benzyl phenylmethanethiosulfinate (petivericin). The results show that the LFS and alliinase function in tandem, with the alliinase furnishing the sulfenic acid substrate on which the LFS acts. The results also show that the LFS modulates the formation of biologically active thiosulfinates that are downstream of the alliinase in a manner dependent upon the relative concentrations of the LFS and the alliinase. These observations suggest that manipulation of LFS-to-alliinase ratios in plants displaying this system may provide a means by which to rationally modify organosulfur small molecule profiles to obtain desired flavor and/or odor signatures, or increase the presence of desirable biologically active small molecules.

  15. Identification of UDP-glucuronosyltransferases 1A1, 1A3 and 2B15 as the main contributors to glucuronidation of bakuchiol, a natural biologically active compound.

    PubMed

    Li, Feng; Wang, Shuai; Lu, Danyi; Wang, Yifei; Dong, Dong; Wu, Baojian

    2017-05-01

    1. Bakuchiol, one of the main active compounds of Psoralea corylifolia, possesses a variety of pharmacological activities such as anti-tumor and anti-aging effects. Here, we aimed to characterize the glucuronidation of bakuchiol using human liver microsomes (HLM) and expressed UDP-glucuronosyltransferase (UGT) enzymes. 2. The glucuronide of bakuchiol was confirmed by liquid chromatography-mass spectrometry (LC-MS) and β-glucuronidase hydrolysis assay. Glucuronidation rates and kinetic parameters were derived by enzymatic incubation and model fitting. Activity correlation analyses were performed to identify the main UGT isoforms contributing to hepatic metabolism of bakuchiol. 3. Among the three UGT enzymes (i.e., UGT1A1, UGT1A3 and UGT2B15) capable of catalyzing bakuchiol glucuronidation, UGT2B15 showed the highest activity with a CLint value of 100 μl/min/nmol. Bakuchiol glucuronidation was strongly correlated with glucuronidation of 5-hydroxyrofecoxib (r = 0.933; p < 0.001), 3-O-glucuronidation of β-estradiol (r = 0.719; p < 0.01) and significantly correlated with 24-O-glucuronidation of CDCA (r = 0.594; p < 0.05). In addition, a marked species difference existed in hepatic glucuronidation of bakuchiol. 4. In conclusion, UGT1A1, UGT1A3 and UGT2B15 were identified as the main contributors to glucuronidation of bakuchiol.

  16. [New selen-organic biologically active nutrition supplement as a palliative for protection against chemical exposure].

    PubMed

    Sanotskiĭ, I V

    2009-01-01

    The article covers data on new biologically active nutrition supplement containing 3 generation selenium compound. The data include biologic effects, pharmacokinetics and usage recommendation for the supplement.

  17. Perylenequinones: Isolation, Synthesis, and Biological Activity

    PubMed Central

    Mulrooey, Carol A.; O'Brien, Erin M.; Morgan, Barbara J.

    2013-01-01

    The perylenequinones are a novel class of natural products characterized by pentacyclic conjugated chromophore giving rise to photoactivity. Potentially useful light-activated biological activity, targeting protein kinase C (PKC), has been identified for several of the natural products. Recently discovered new members of this class of compound, as well as several related phenanthroperylenequinones, are reviewed. Natural product modifications that improve biological profiles, and avenues for the total synthesis of analogs, which are not available from the natural product series, are outlined. An overview of structure/function relationships is provided. PMID:24039544

  18. Synthesis and characterization of some metal complexes derived from azo compound of 4,4‧-methylenedianiline and antipyrine: Evaluation of their biological activity on some land snail species

    NASA Astrophysics Data System (ADS)

    AbouEl-Enein, Saeyda A.; Emam, Sanaa M.; Polis, Magdy W.; Emara, Esam M.

    2015-11-01

    A novel series of metal complexes of the azo dye; bis-(1,5-dimethyl-4-[(E)-(3-methylphenyl)diazenyl]-2-phenyl-1,2-dihydro-3H-pyrazol-3-one) derived from 4,4‧-methylenedianiline and antipyrine was synthesized and characterized by different spectral, thermal and analytical methods. The tetradentate ligand reacts with the metal ions as a half unit. All complexes display an octahedral geometry, except Pd(II) complex (7) which has a square planar one. The thermal studies reveal that the complexes have higher thermal stability comparable with that of the free ligand. The activation thermodynamic parameters, such as activation energy (E*), enthalpy of activation (ΔH*), entropy of activation (ΔS*) and Gibbs free energy (ΔG*) have been calculated using DTG curves. The ESR spectra of the solid Cu(II) complexes showed an axial symmetry with 2B1g as a ground state and hyperfine structure. The biological activities of the ligand, as well as its metal complexes have been tested in vitro against two land snail species; Eobania vermiculata and Monacha obstructa. The results show that all the tested compounds have significant biological activities against the two tested land snail species with different sensitivity levels.

  19. 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.

    PubMed

    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

  20. Estrogenic flavonoids: structural requirements for biological activity.

    PubMed

    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.

  1. Chemical transformations that yield compounds with distinct activity profiles.

    PubMed

    Hu, Ye; Bajorath, Jürgen

    2011-07-14

    We have systematically searched for chemical changes that generate compounds with distinct biological activity profiles. For this purpose, activity profiles were generated for ∼42000 compounds active against human targets. Unique activity profiles involving multiple target proteins were determined, and all possible matched molecular pairs (MMPs) were identified for compounds representing these profiles. An MMP is defined as a pair of compounds that are distinguished from each other only at a single site such as an R group or ring system. For example, in an MMP, a hydroxyl group might be replaced by a halogen atom or a benzene ring by an amide group. From ∼37500 MMPs, more than 300 nonredundant chemical transformations were isolated that yielded compounds with distinct activity profiles. None of these transformations was found in pairs of compounds with overlapping activity profiles. These transformations were ranked according to the number of MMPs, the number of activity profiles, and the total number of targets that they covered. In many instances, prioritized transformations involved ring systems of varying complexity. All transformations that were found to switch activity profiles are provided to enable further analysis and aid in compound design efforts.

  2. [Organisms producing hypolipidemic compounds with antioxidant activity].

    PubMed

    Puzhevskaia, T O; Grammatikova, N E; Bibikova, M V; Katlinskiĭ, A V

    2009-01-01

    Complex compounds produced by fungal cultures of Lecanicilium and Beauveria with both high hypolipidemic and antioxydant activities were screened. Two fractions of the hypolipipidemic compounds with antioxidant activity of 95 and 75% in a dose of 25 mcg/ml were isolated.

  3. Study of Compounds for Activity against Leishmania

    DTIC Science & Technology

    1994-03-27

    Comparative Antileishmanial Activity of Selected Compounds Against Leishmania Leishmania donovani and Leishmania Viannia braziliensis 7 IV. Zn vitro...Studies of Oligonucleotides Against Leishmania Leishmania donovani ............................................................ 9 Discussion...for several years in studies to identify new compounds for antileishmanial activity against both visceral (Lelshmania Leishmania donovani ) and

  4. Synthesis of a mixed-model stationary phase derived from glutamine for HPLC separation of structurally different biologically active compounds: HILIC and reversed-phase applications.

    PubMed

    Aral, Tarık; Aral, Hayriye; Ziyadanoğulları, Berrin; Ziyadanoğulları, Recep

    2015-01-01

    A novel mixed-mode stationary phase was synthesised starting from N-Boc-glutamine, aniline and spherical silica gel (4 µm, 60 Å). The prepared stationary phase was characterized by IR and elemental analysis. The new stationary phase bears an embedded amide group into phenyl ring, highly polar a terminal amide group and non-polar groups (phenyl and alkyl groups). At first, this new mixed-mode stationary phase was used for HILIC separation of four nucleotides and five nucleosides. The effects of different separation conditions, such as pH value, mobile phase and temperature, on the separation process were investigated. The optimum separation for nucleotides was achieved using HILIC isocratic elution with aqueous mobile phase and acetonitrile with 20°C column temperature. Under these conditions, the four nucleotides could be separated and detected at 265 nm within 14 min. Five nucleosides were separated under HILIC isocratic elution with aqueous mobile phase containing pH=3.25 phosphate buffer (10mM) and acetonitrile with 20°C column temperature and detected at 265 nm within 14 min. Chromatographic parameters as retention factor, selectivity, theoretical plate number and peak asymmetry factor were calculated for the effect of temperature and water content in mobile phase on the separation process. The new column was also tested for nucleotides and nucleosides mixture and six analytes were separated in 10min. The chromatographic behaviours of these polar analytes on the new mixed-model stationary phase were compared with those of HILIC columns under similar conditions. Further, phytohormones and phenolic compounds were separated in order to see influence of the new stationary phase in reverse phase conditions. Eleven plant phytohormones were separated within 13 min using RP-HPLC gradient elution with aqueous mobile phase containing pH=2.5 phosphate buffer (10mM) and acetonitrile with 20°C column temperature and detected at 230 or 278 nm. The best separation

  5. CHARACTERIZATION OF SULPHIDE SILT PE-LOIDS IN SOME LAKES WITHIN ADJARA REGION AND DETERMINATION OF THE BIOLOGICALLY ACTIVE COMPOUNDS CONTENT.

    PubMed

    Masiukovichi, T; Jokhadze, M; Murtazashvili, T; Bakuridze, A

    2017-09-01

    Medicinal muds, so called Peloids in the last decade attract attention in many countries as effective means for the treatment- preventive, and perfumery-cosmetic purposes. It has been established that the possibilities of this formation of nature are not limited to the many-year experience of the mankind. In terms of further improvement of the human social sphere, nowadays peloids are referred to as XXI century material. The aim of the research was to study the physical-chemical characteristics, such as: humidity, pH, ash content, bulk (volumetric) density and organoleptic properties of sulphide silt peloids of some Adjara region lakes, as well as to determine the content of mineral and organic compounds (humic and organic acids). The objects of the study were the sulphide silt peloids of some Adjara region lakes: Mtsvane, Gasaliani, Shratiani, Nurigeli, Ardagani and Niphi. The main good quality indicators of the sulphide silt peloids have been determined according to the methods described in the State Pharmacopoeia XI. The mineral and organic compounds in the research objects have been determined using the modern instrumental methods of analysis described in the literature. Based on the performed studies, the main physical-chemical characteristics of sulphide silt peloids of some Adjara region lakes (Mtsvane, Gasaliani, Shratiani, Nurigeli, Ardagani and Niphi) have been studied and their mineral contents (Ca-Na Feldspar, K Feldspar, Ca- Montmorillonite, Hematite, Quartz, Magnetite, Chlorite) determined. By the spectrophotometric and gravimetric methods of analysis there is established, that the sulphide silt peloids of the lakes Ardagani (1,22%), Niphi (1,72%) and Gasaliani (1,33%) are distinguished by relatively higher content of humic acids. By the Gas Chromatography-Mass Spectrometry - method of analysis, in the study objects there is established the content of complex ethers of the following organic acids: Stearic, Palmitic, Caprylic, Myristic, Valeric, Lauric

  6. Investigation on the self-association of an inorganic coordination compound with biological activity (Casiopeína III-ia) in aqueous solution.

    PubMed

    Marín-Medina, Alejandro; García-Ramos, Juan Carlos; Ruíz-Azuara, Lena; Carrillo-Nava, Ernesto

    2016-01-01

    From studies using different experimental techniques employed to determine the presence of aggregates e.g. isothermal titration calorimetry, surface tension, electrical conductivity, UV-Vis spectrophotometry, dynamic and static light scattering, it is clearly demonstrated that the compound [Cu(4, 4'-dimethyl-2, 2'-bipyridine)(acetylacetonato)H2O]NO3 (Casiopeína III-ia), promising member of a family of new generation compounds for cancer treatment, is able to auto associate in aqueous media. Physicochemical properties associated with the formation of the aggregates were determined in pure water and in phosphate buffer media in order to simulate physiological conditions. From isothermal titration calorimetry and electrical conductivity measurements we calculated the dissociation constant of the aggregates, KD . For pure water the values obtained in both techniques are 2.73 × 10(-4) and 5.93 × 10(-4) M respectively while for the buffer media we obtained 4.61 × 10(-4) and 1.57 × 10(-3) M. The enthalpy of dissociation, ∆HD , calculated from the calorimetric data shows that the presence of the phosphate ions has an energetic effect on the aggregate stability since in pure water a value of 18.79 kJ mol(-1) was obtained in comparison with the buffer media where a value 4 times bigger was found (70.48 kJ mol(-1)). With the data collected from these techniques the number of monomers calculated which participate in the formation of the aggregates is around two. From our surface tension, electrical conductivity and UV-Vis spectrophotometry measurements the critical aggregate concentration, cac, was determined. For each technique specific concentration ranges were obtained but we can summarize that the cac in pure water is between 3 and 3.5 mM and for the buffer media is between 3.5 and 4 mM. Dynamic light scattering measurements provide us with the hydrodynamic diameter of the aggregates and from static light scattering measurements we determined the

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

    PubMed Central

    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

  8. Characterization of Volatile Compounds of Eleven Achillea Species from Turkey and Biological Activities of Essential Oil and Methanol Extract of A. hamzaoglui Arabacı & Budak.

    PubMed

    Turkmenoglu, Fatma Pinar; Agar, Osman Tuncay; Akaydin, Galip; Hayran, Mutlu; Demirci, Betul

    2015-06-22

    According to distribution of genus Achillea, two main centers of diversity occur in S.E. Europe and S.W. Asia. Diversified essential oil compositions from Balkan Peninsula have been numerously reported. However, report on essential oils of Achillea species growing in Turkey, which is one of the main centers of diversity, is very limited. This paper represents the chemical compositions of the essential oils obtained by hydrodistillation from the aerial parts of eleven Achillea species, identified simultaneously by gas chromatography and gas chromatography-mass spectrometry. The main components were found to be 1,8-cineole, p-cymene, viridiflorol, nonacosane, α-bisabolol, caryophyllene oxide, α-bisabolon oxide A, β-eudesmol, 15-hexadecanolide and camphor. The chemical principal component analysis based on thirty compounds identified three species groups and a subgroup, where each group constituted a chemotype. This is the first report on the chemical composition of A. hamzaoglui essential oil; as well as the antioxidant and antimicrobial evaluation of its essential oil and methanolic extract.

  9. Elsholtzia: phytochemistry and biological activities

    PubMed Central

    2012-01-01

    Plants of the genus Elsholtzia (Lamiaceae) have a long history of medicinal use in folk. The phytochemical investigations revealed the presence of flavonoids, phenylpropanoids, terpenoids, and other compounds. Abundant volatile components are also identified. Pure compounds, volatile constituents and crude extracts from the genus exhibited a wide spectrum of in vitro and in vivo pharmacological activities. The aims of this review hopefully provide comprehensive information on the distribution, phytochemistry, volatile components, and pharmacological research of Elsholtzia for exploring the potential and advance researches. PMID:23216850

  10. Antibacterial activity and biological performance of a novel antibacterial coating containing a halogenated furanone compound loaded poly(L-lactic acid) nanoparticles on microarc-oxidized titanium

    PubMed Central

    Cheng, Yicheng; Zhao, Xianghui; Liu, Xianghui; Sun, Weige; Ren, Huifang; Gao, Bo; Wu, Jiang

    2015-01-01

    Titanium implants have been widely used for many medical applications, but bacterial infection after implant surgery remains one of the most common and intractable complications. To this end, long-term antibacterial ability of the implant surface is highly desirable to prevent implant-associated infection. In this study, a novel antibacterial coating containing a new antibacterial agent, (Z-)-4-bromo-5-(bromomethylene)-2(5H)-furanone loaded poly(L-lactic acid) nanoparticles, was fabricated on microarc-oxidized titanium for this purpose. The antibacterial coating produced a unique inhibition zone against Staphylococcus aureus throughout a 60-day study period, which is normally long enough to prevent the infection around implants in the early and intermediate stages. The antibacterial rate for adherent S. aureus was about 100% in the first 10 days and constantly remained over 90% in the following 20 days. Fluorescence staining of adherent S. aureus also confirmed the excellent antibacterial ability of the antibacterial coating. Moreover, in vitro experiments showed an enhanced osteoblast adhesion and proliferation on the antibacterial coating, and more notable cell spread was observed at the early stage. It is therefore concluded that the fabricated antibacterial coating, which exhibits relatively long-term antibacterial ability and excellent biological performance, is a potential and promising strategy to prevent implant-associated infection. PMID:25632231

  11. Antibacterial activity and biological performance of a novel antibacterial coating containing a halogenated furanone compound loaded poly(L-lactic acid) nanoparticles on microarc-oxidized titanium.

    PubMed

    Cheng, Yicheng; Zhao, Xianghui; Liu, Xianghui; Sun, Weige; Ren, Huifang; Gao, Bo; Wu, Jiang

    2015-01-01

    Titanium implants have been widely used for many medical applications, but bacterial infection after implant surgery remains one of the most common and intractable complications. To this end, long-term antibacterial ability of the implant surface is highly desirable to prevent implant-associated infection. In this study, a novel antibacterial coating containing a new antibacterial agent, (Z-)-4-bromo-5-(bromomethylene)-2(5H)-furanone loaded poly(L-lactic acid) nanoparticles, was fabricated on microarc-oxidized titanium for this purpose. The antibacterial coating produced a unique inhibition zone against Staphylococcus aureus throughout a 60-day study period, which is normally long enough to prevent the infection around implants in the early and intermediate stages. The antibacterial rate for adherent S. aureus was about 100% in the first 10 days and constantly remained over 90% in the following 20 days. Fluorescence staining of adherent S. aureus also confirmed the excellent antibacterial ability of the antibacterial coating. Moreover, in vitro experiments showed an enhanced osteoblast adhesion and proliferation on the antibacterial coating, and more notable cell spread was observed at the early stage. It is therefore concluded that the fabricated antibacterial coating, which exhibits relatively long-term antibacterial ability and excellent biological performance, is a potential and promising strategy to prevent implant-associated infection.

  12. Biological Activity of Dolichandrone serrulata Flowers and Their Active Components.

    PubMed

    Phanthong, Phanida; Phumal, Noppawan; Chancharunee, Sirirat; Mangmool, Supachoke; Anantachoke, Natthinee; Bunyapraphatsara, Nuntavan

    2015-08-01

    Dolichandrone serrulata (DC.) Seem flowers are widely used as vegetables in northern and eastern Thailand. Biological studies of the methanolic extract of these flowers have shown promising antioxidant activity. Biological-guided separation of D. serrulata flowers yielded six compounds, identified as hallerone, protocatechuic acid, rengyolone, cleroindicin B, ixoside, and isomaltose. This is the first report on hallerone, protocatechuic acid, rengyolone, cleroindicin B, and isomaltose in D. serrulata. Protocatechuic acid was the most potent scavenger of 2,2-diphenyl-l-picrylhydrazyl and hydroxyl radicals with IC50 values of 25.6 +/- 0.6 and 29.6 +/- 0.4 microM, respectively. Hallerone and rengyolone showed moderate scavenging action on superoxide radicals and inhibited H202 induced reactive oxygen species production in HEK-293 cell. In addition, the other isolated compounds showed weak activity.

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

    PubMed

    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.

  14. Biologically Active Metabolites Synthesized by Microalgae

    PubMed Central

    de Morais, Michele Greque; Vaz, Bruna da Silva; de Morais, Etiele Greque; Costa, Jorge Alberto Vieira

    2015-01-01

    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. PMID:26339647

  15. Solar Energy Project, Activities: Biology.

    ERIC Educational Resources Information Center

    Tullock, Bruce, Ed.; And Others

    This guide contains lesson plans and outlines of science activities which present concepts of solar energy in the context of biology experiments. Each unit presents an introduction; objectives; skills and knowledge needed; materials; methods; questions; recommendations for further work; and a teacher information sheet. The teacher information…

  16. Antioxidant Activity of Marine Algal Polyphenolic Compounds: A Mechanistic Approach.

    PubMed

    Fernando, I P Shanura; Kim, Misook; Son, Kwang-Tae; Jeong, Yoonhwa; Jeon, You-Jin

    2016-07-01

    Polyphenolic compounds isolated from marine algae exhibit a broad spectrum of beneficial biological properties, including antioxidant, anticancer, antimicrobial, anti-inflammatory, and antidiabetic activities, along with several other bioactivities centered on their antioxidant properties. Consequently, polyphenolic compounds are increasingly being investigated for their potential use in food, cosmetic, and pharmaceutical applications. The antioxidant activities of these compounds have been explored widely through experimental studies. Nonetheless, a theoretical understanding of the structural and electronic properties could broaden research perspectives, leading to the identification and synthesis of efficient structural analogs with prophylactic uses. This review briefly summarizes the current state of knowledge regarding antioxidant polyphenolic compounds in marine algae with an attempt to describe the structure-activity relationship.

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

    PubMed Central

    Singh, Kiran; Kumar, Yogender; Puri, Parvesh; Sharma, Chetan; Aneja, Kamal Rai

    2011-01-01

    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. PMID:22216017

  18. Perspectives on Biologically Active Camptothecin Derivatives

    PubMed Central

    Liu, Ying-Qian; Li, Wen-Qun; Morris-Natschke, Susan L.; Qian, Keduo; Yang, Liu; Zhu, Gao-Xiang; Wu, Xiao-Bing; Chen, An-Liang; Zhang, Shao-Yong; Song, Zi-Long; Lee, Kuo-Hsiung

    2015-01-01

    Camptothecins (CPTs) are cytotoxic natural alkaloids that specifically target DNA topoisomerase I. Research on CPTs has undergone a significant evolution from the initial discovery of CPT in the late 1960s through the study of synthetic small molecule derivatives to investigation of macromolecular constructs and formulations. Over the past years, intensive medicinal chemistry efforts have generated numerous CPT derivatives. Three derivatives, topotecan, irinotecan, and belotecan, are currently prescribed as anticancer drugs, and several related compounds are now in clinical trials. Interest in other biological effects, besides anticancer activity, of CPTs is also growing exponentially, as indicated by the large number of publications on the subject during the last decades. Therefore, the main focus of the present review is to provide an ample but condensed overview on various biological activities of CPT derivatives, in addition to continued up-to-date coverage of anticancer effects. PMID:25808858

  19. Odor-active compounds in cardboard.

    PubMed

    Czerny, Michael; Buettner, Andrea

    2009-11-11

    The odor-active compounds of cardboard were identified by aroma extract dilution analysis and HRGC-MS analysis. In total, 36 compounds were detected with medium to high intensities during HRGC-olfactometry. The highest odor intensities were evaluated for vanillin, (E)-non-2-enal, (R/S)-gamma-nonalactone, 2-methoxyphenol, (R/S)-delta-decalactone, p-anisaldehyde, 3-propylphenol, and a woody-smelling unknown compound. Most of the identified compounds were described as odor-active cardboard constituents for the first time. Sensory experiments demonstrated that extensive release of odor-active compounds occurred upon moistening of the cardboard. Accordingly, data indicated that the odorants are present in cardboard in relatively high amounts. In a further sensory study, a transfer of the released odor to food was demonstrated in a model experiment showing that cardboards with high odor potential can cause unwanted flavor changes in foods.

  20. Chemistry and biology of ω-3 PUFA peroxidation-derived compounds.

    PubMed

    Wang, Weicang; Yang, Haixia; Johnson, David; Gensler, Catherine; Decker, Eric; Zhang, Guodong

    2016-12-31

    The ω-3 polyunsaturated fatty acids (PUFAs) are among the most popular dietary supplements in the US, but they are chemically unstable and highly prone to lipid peroxidation. Many studies performed in different countries demonstrate that the majority of ω-3 PUFA products on the market are oxidized, suggesting that the resulting ω-3 PUFA peroxidation-derived compounds could be widely consumed by the general public. Therefore, it is of practical importance to understand the effects of these oxidized lipid compounds on human health. In this review, we summarize and discuss the chemical structures and biological activities of ω-3 PUFA peroxidation-derived compounds, and emphasize the importance to better understand the role of lipid peroxidation in biological activities of ω-3 PUFAs. Copyright © 2016 Elsevier Inc. All rights reserved.

  1. Diverse biological activities of dandelion.

    PubMed

    González-Castejón, Marta; Visioli, Francesco; Rodriguez-Casado, Arantxa

    2012-09-01

    Dandelion (Taraxacum officinale Weber) is a member of the Asteraceae (Compositae) family, native to Europe but widely distributed in the warmer temperate zones of the Northern Hemisphere. Dandelion and its parts are habitually consumed as plant foods in several areas of the world, where they are also employed in phytotherapy. Indeed, dandelion contains a wide array of phytochemicals whose biological activities are actively being explored in various areas of human health. In particular, emerging evidence suggests that dandelion and its constituents have antioxidant and anti-inflammatory activities that result in diverse biological effects. The present review provides a comprehensive analysis of the constituents of dandelion, an assessment of the pharmacological properties of dandelion, and a description of relevant studies that support the use of dandelion as a medicinal plant.

  2. Bioactive compounds in cranberries and their biological properties.

    PubMed

    Côté, J; Caillet, S; Doyon, G; Sylvain, J-F; Lacroix, M

    2010-08-01

    Cranberries are healthy fruit that contribute color, flavor, nutritional value, and functionality. They are one of only three fruits native to America. Over the past decade, public interest for the North American cranberry (Vaccinium macrocarpon) has been rising with reports of their potential health benefits linked to the numerous phytochemicals present in the fruit--the anthocyanins, the flavonols, the flavan-3-ols, the proanthocyanidins, and the phenolic acid derivatives. The presence of these phytochemicals appears to be responsible for the cranberry property of preventing many diseases and infections, including cardiovascular diseases, various cancers, and infections involving the urinary tract, dental health, and Helicobacter pylori-induced stomach ulcers and cancers. Recent years have seen important breakthroughs in our understanding of the mechanisms through which these compounds exert their beneficial biological effects, yet these remain to be scientifically substantiated. In this paper these characteristics, as well as the antioxidant, radical scavenging, antibacterial, antimutagen, and anticarcinogen properties of cranberry major bioactive compounds are explained.

  3. Biological Activities of Polyphenols from Grapes

    PubMed Central

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

    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 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. PMID:20386657

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

    PubMed

    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.

  5. Synthesis and electrochemical and biological studies of novel coumarin-chalcone hybrid compounds.

    PubMed

    Pérez-Cruz, Fernanda; Vazquez-Rodriguez, Saleta; Matos, Maria João; Herrera-Morales, Alejandra; Villamena, Frederick A; Das, Amlan; Gopalakrishnan, Bhavani; Olea-Azar, Claudio; Santana, Lourdes; Uriarte, Eugenio

    2013-08-08

    A series of novel hydroxy-coumarin-chalcone hybrid compounds 2a-i has been synthesized by employing a simple and efficient methodology. An electrochemical characterization using cyclic voltammetry and ESR spectroscopy were carried out to characterize the oxidation mechanism for the target compounds. The antioxidant capacity and reactivity were determined by ORAC and ESR assays, respectively. Biological assays were assessed to evaluate the cytotoxicity and cytoprotection capacity against ROS/RNS on BAEC. The results revealed that all tested compounds present ORAC values that are much higher than other well-known antioxidant compounds such as quercetin and catechin. Compound 2e showed the highest ORAC value (14.1) and also presented a low oxidation potential, good scavenging capacity against hydroxyl radicals, low cytotoxicity, and high cytoprotective activity.

  6. Study of Compounds for Activity against Leishmania

    DTIC Science & Technology

    1992-10-27

    Mrs. Barbara Harris, Miss Laura A. Lamb, and Miss Shannon Waits. tORZWORD Opinions, interpretations, conclusions and recommendations are those of the...antileishmanial activity against both visceral (Leishmania donovani) and cutaneous (Lebs-Qnia, braziliensis panamensis) leishmaniasis . Among the most promising...active compounds found against visceral leishmaniasis durinq these studies is the 8-aminoquinoline, WR06026. This compound is now undergoing clinical

  7. Biological assay challenges from compound solubility: strategies for bioassay optimization.

    PubMed

    Di, Li; Kerns, Edward H

    2006-05-01

    Compound solubility in buffers and dimethyl sulfoxide (DMSO) has emerged as an important issue. Many discovery compounds have low solubility but are potentially valuable as leads. Unfortunately, low solubility affects bioassays by causing underestimated activity, reduced HTS-hit rates, variable data, inaccurate SAR, discrepancies between enzyme and cell assays and inaccurate in vitro ADME-Tox testing. Strategies for optimizing bioassays include: considering solubility in HTS-library design; early screening for solubility; improving storage and handling of DMSO stocks; optimizing dilution protocols; and ensuring that low-solubility compounds are fully solubilized in bioassays. These approaches allow for adequate assessments of valuable pharmacophores for which solubility can be chemically optimized at a later date.

  8. Aqua mediated synthesis of bio-active compounds.

    PubMed

    Panda, Siva S

    2013-05-01

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

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

    PubMed Central

    Mawa, Shukranul; Husain, Khairana; Jantan, Ibrahim

    2013-01-01

    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. PMID:24159359

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

    PubMed

    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).

  11. Investigating biological activity spectrum for novel quinoline analogues 2: hydroxyquinolinecarboxamides with photosynthesis-inhibiting activity.

    PubMed

    Musiol, Robert; Tabak, Dominik; Niedbala, Halina; Podeszwa, Barbara; Jampilek, Josef; Kralova, Katarina; Dohnal, Jiri; Finster, Jacek; Mencel, Agnieszka; Polanski, Jaroslaw

    2008-04-15

    Two series of amides based on quinoline scaffold were designed and synthesized in search of photosynthesis inhibitors. The compounds were tested for their photosynthesis-inhibiting activity against Spinacia oleracea L. and Chlorella vulgaris Beij. The compounds lipophilicity was determined by the RP-HPLC method. Several compounds showed biological activity similar or even higher than that of the standard (DCMU). The structure-activity relationships are discussed.

  12. Investigating biological activity spectrum for novel styrylquinazoline analogues.

    PubMed

    Jampilek, Josef; Musiol, Robert; Finster, Jacek; Pesko, Matus; Carroll, James; Kralova, Katarina; Vejsova, Marcela; O'Mahony, Jim; Coffey, Aidan; Dohnal, Jiri; Polanski, Jaroslaw

    2009-10-23

    In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.

  13. Gemini ester quat surfactants and their biological activity.

    PubMed

    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.

  14. Potential biological activity of acacia honey.

    PubMed

    Muhammad, Aliyu; Odunola, Oyeronke A; Ibrahim, Mohammed A; Sallau, Abdullahi B; Erukainure, Ochuko L; Aimola, Idown A; Malami, Ibrahim

    2016-01-01

    Recent advances in functional foods-based research have increasingly become an area of major interest because it affects human health and activities. Functional foods are classes of foods with health promoting and disease preventing properties in addition to multiple nutritional values and of such type is honey. Acacia honey is a type of honey produced by bees (Apis mellifera) fed on Acacia flowers, hence the name. This review focuses on the potential biological activities of Acacia honey which includes quality, antioxidant, immuno-modulatory, antiproliferative and neurological properties at in vitro and in vivo levels. Based on our review, Acacia honey used from various researches is of high purity, contains some bioactive compounds ranging from vitamins, phenolics, flavonoids and fatty acids. It's highly nutritional with strong antioxidant and immuno-modulatory potentials which may therefore be considered a potential candidate for both cancer prevention and treatment. Neurologically, it may be considered as a viable therapeutic agent in the management of Alzheimer's disease.

  15. Prediction of biological targets for compounds using multiple-category Bayesian models trained on chemogenomics databases.

    PubMed

    Nidhi; Glick, Meir; Davies, John W; Jenkins, Jeremy L

    2006-01-01

    Target identification is a critical step following the discovery of small molecules that elicit a biological phenotype. The present work seeks to provide an in silico correlate of experimental target fishing technologies in order to rapidly fish out potential targets for compounds on the basis of chemical structure alone. A multiple-category Laplacian-modified naïve Bayesian model was trained on extended-connectivity fingerprints of compounds from 964 target classes in the WOMBAT (World Of Molecular BioAcTivity) chemogenomics database. The model was employed to predict the top three most likely protein targets for all MDDR (MDL Drug Database Report) database compounds. On average, the correct target was found 77% of the time for compounds from 10 MDDR activity classes with known targets. For MDDR compounds annotated with only therapeutic or generic activities such as "antineoplastic", "kinase inhibitor", or "anti-inflammatory", the model was able to systematically deconvolute the generic activities to specific targets associated with the therapeutic effect. Examples of successful deconvolution are given, demonstrating the usefulness of the tool for improving knowledge in chemogenomics databases and for predicting new targets for orphan compounds.

  16. Preparation, characterization and biological activity of C8-substituted cytokinins.

    PubMed

    Zahajská, Lenka; Nisler, Jaroslav; Voller, Jiří; Gucký, Tomáš; Pospíšil, Tomáš; Spíchal, Lukáš; Strnad, Miroslav

    2017-03-01

    Naturally occurring cytokinins are adenine-based plant hormones. Although, the effect of various substituents at positions N1, C2, N3, N(6), N7, or N9 on the biological activity of cytokinins has been studied, the C8-substituted compounds have received little attention. Here, we report the synthesis and in vitro biological testing of thirty-one cytokinin derivatives substituted at the C8 position of the adenine skeleton and twenty-seven compounds which served as their N9-tetrahydropyranyl protected precursors. The cytokinin activity of all the compounds was determined in classical cytokinin biotests (wheat leaf senescence, Amaranthus and tobacco callus assays). With some exceptions, the compounds with a N9-tetrahydropyranyl group were generally less active than their de-protected analogs. The latter were further tested for their ability to activate the Arabidopsis cytokinin receptors AHK3 and CRE1/AHK4 in bacterial receptor activation assays. Using this approach, we identified derivatives bearing short aliphatic chains and retaining high cytokinin activity. Such compounds are suitable candidates for fluorescence labeling or as protein-affinity ligands. We further found that some C8-substituted cytokinins exhibited no or lower cytotoxicity toward tobacco cells when compared to their parent compound. Therefore, we also present and discuss the cytotoxicity of all the compounds against three normal human cell lines.

  17. [Biological activity of Penicillium sp. 10-51 exometabolites].

    PubMed

    Savchuk, Ia I; Zaĭchenko, A M; Tsyganenko, E S

    2012-01-01

    Silica gel column chromatography (silica gel "L" II kind of activity 100/160 mkm) of the chloroform extract from the cultural filtrate of Penicillium sp. 10-51 gave two fractions (chloroform and chloroform-acetone, 5:1) having biological activity. Recrystallization yielded two compounds. On the basis of physico-chemical and spectral data these compounds were identified as curvularin and hydroxycurvularin, which have a large spectrum of biological action as to bacteria, yeast, blue-green algae and phytopathogenic micromycetes.

  18. Biological Activity of Aminophosphonic Acids and Their Short Peptides

    NASA Astrophysics Data System (ADS)

    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).

  19. Monascus secondary metabolites: production and biological activity.

    PubMed

    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.

  20. Biological activation of carbon filters.

    PubMed

    Seredyńska-Sobecka, Bozena; Tomaszewska, Maria; Janus, Magdalena; Morawski, Antoni W

    2006-01-01

    To prepare biological activated carbon (BAC), raw surface water was circulated through granular activated carbon (GAC) beds. Biological activity of carbon filters was initiated after about 6 months of filter operation and was confirmed by two methods: measurement of the amount of biomass attached to the carbon and by the fluorescein diacetate (FDA) test. The effect of carbon pre-washing on WG-12 carbon properties was also studied. For this purpose, the nitrogen adsorption isotherms at 77K and Fourier transform-infrared (FT-IR) spectra analyses were performed. Moreover, iodine number, decolorizing power and adsorption properties of carbon in relation to phenol were studied. Analysis of the results revealed that after WG-12 carbon pre-washing its BET surface increased a little, the pH value of the carbon water extract decreased from 11.0 to 9.4, decolorizing power remained at the same level, and the iodine number and phenol adsorption rate increased. In preliminary studies of the ozonation-biofiltration process, a model phenol solution with concentration of approximately 10mg/l was applied. During the ozonation process a dose of 1.64 mg O(3)/mg TOC (total organic carbon) was employed and the contact time was 5 min. Four empty bed contact times (EBCTs) in the range of 2.4-24.0 min were used in the biofiltration experiment. The effectiveness of purification was measured by the following parameters: chemical oxygen demand (COD(Mn)), TOC, phenol concentration and UV(254)-absorbance. The parameters were found to decrease with EBCT.

  1. Sulfated phenolic compounds from Limonium caspium: Isolation, structural elucidation, and biological evaluation

    PubMed Central

    Gadetskaya, Anastassiya V.; Tarawneh, Amer H.; Zhusupova, Galiya E.; Gemejiyeva, Nadezhda G.; Cantrell, Charles L.; Cutler, Stephen J.; Ross, Samir A.

    2016-01-01

    Three new compounds, (2S,3S)-5-methyldihydromyricetin (1), (2S,3S)-5-methyldihydromyricetin-3′-O-sulfate (2) and β-D-glucopyranoside, 3-methyl, but-3-en-1-yl 4-O-α-L-rhamnopyranosyl (3) have been isolated from the Limonium caspium, together with dihydromyricetin (4), dihydromyricetin-3′-O-sulfate (5), myricetin-3′-O-sulfate (6), 5-methylmyricetin (7), myricetin (8), myricetin-3-O-β-glucoside (9), as well as phloridzin (10), and tyramine (11). Compounds 5 and 6 were isolated for the first time as acids. This is the first report of all these compounds from this plant. Their structures were established by extensive NMR studies (1H NMR, 13C NMR, DEPT, 1H–1H COSY, HSQC, HMBC) as well as HRESIMS. All isolated compounds were evaluated for their antibacterial, antifungal, antimalarial and antileishmanial activities. Compounds 7, 8 and 9 exhibited good antifungal activity against Candida glabrata with IC50 values of 6.79, 15.37 and 8.53 μg/mL, respectively. Compound 8 displayed significant antimalarial activity against resistant and sensitive strains of Plasmodium falciparum with IC50 values of 1.82 and 1.51 μg/mL, respectively. Compounds 1, 4, 6, 8 and 9 showed excellent activity against Trypanosoma brucei with IC50 values of 6.93, 9.65, 8.52, 7.67 and 6.31 μg/mL, respectively. To date, this is the first report on the phytochemical and biological activity of secondary metabolites from L. caspium. PMID:26025854

  2. Virtual screening and biological evaluation of novel antipyretics compounds.

    PubMed

    Froes, Thamires Quadros; Melo, Miriam C C; Souza, Gloria E P; Castilho, Marcelo Santos; Soares, Denis M

    2017-04-08

    Due to the absence ofsafety of the antipyretics to patients withcardiovascular dysfunction,new targets to treatinflammation have been pursued. mPGES-1 is a promising target because its inhibition would not cause the side effectsrelated to COX inhibition. In order to identify novel inhibitorsof mPGES-1, we developed a ligand-basedpharmacophoremodel that differentiates true inhibitors from decoys andenlightens the structure-activity relationships for known mPGES-1 inhibitors.The model (4 hydrophobic centers, 2 hydrogen-bond acceptor and 2 hydrogen-bond donor points) was employed to select lead-like compoundsfrom ZINC database forin vivo evaluation.Among the 18 compoundsselected,fiveinhibited the feverinduced by LPS. The most potent compound (5-(4-fluorophenyl)-3-({6-methylimidazo[1,2-a]pyridin-2-yl}methyl)-2,3dihydro-1,3,4-oxadiazol-2-one) is active peripherally (i.v.) or centrally (i.c.v.) (82.18 and 112% reduction, respectively) and reduces (69,13%) hypothalamic PGE2 production,withoutsignificant COX-1/2 inhibition. In conclusion, our in silico approach lead to the selection of a compound that presents the chemical features to inhibit mPGES-1 and reduces fever induced by LPS. Furthermore, the invivo and in vitro results support the hypothesis that its mechanism of action does not depend on COX inhibition. Hence, it can be considered a promising lead compound for antipyretic development, once it would not have the side effects of COX-1/2 inhibitors. This article is protected by copyright. All rights reserved.

  3. Biotransformations and biological activities of hop flavonoids.

    PubMed

    Karabin, Marcel; Hudcova, Tereza; Jelinek, Lukas; Dostalek, Pavel

    2015-11-01

    Female hop cones are used extensively in the brewing industry, but there is now increasing interest in possible uses of hops for non-brewing purposes, especially in the pharmaceutical industry. Among pharmaceutically important compounds from hops are flavonoids, having proven anticarcinogenic, antioxidant, antimicrobial, anti-inflammatory and estrogenic effects. In this review we aim to present current knowledge on the biotransformation of flavonoids from hop cones with respect to products, catalysis and conversion. A list of microbial enzymatic reactions associated with gastrointestinal microbiota is presented. A comparative analysis of the biological activities of hop flavonoids and their biotransformation products is described, indicating where further research has potential for applications in the pharmaceutical industry.

  4. Strigolactones: structures and biological activities.

    PubMed

    Yoneyama, Koichi; Xie, Xiaonan; Yoneyama, Kaori; Takeuchi, Yasutomo

    2009-05-01

    Strigolactones released from plant roots induce seed germination of root parasitic weeds, witchweeds (Striga spp.) and broomrapes (Orobanche spp.), and hyphal branching of symbiotic arbuscular mycorrhizal (AM) fungi. In addition to these functions in the rhizosphere, strigolactones have recently been shown to be a novel class of plant hormones regulating shoot outgrowth. The natural strigolactones identified so far have the common C-D ring moiety, which is thought to be the essential structure for exhibiting biological activity. The introduction of substitutions on the A-B ring moiety of 5-deoxystrigol, the basic strigolactone, affords various strigolactones, e.g. hydroxylation on C-4, C-5 and C-9 leads to orobanchol, strigol and sorgomol respectively. Then, acetylation and probably other derivatisations of these hydroxy-strigolactones would occur. Although the C-2'-(R) stereochemistry was thought to be an important structural feature for potent germination stimulation activity, 2'-epi-strigolactones were found in root exudates of tobacco, rice, pea and other plant species, indicating that at least some plants produce both epimers.

  5. Biological Activity of Masked Endotoxin

    PubMed Central

    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

  6. Chemical and biological characterisation of nutraceutical compounds of broccoli.

    PubMed

    Moreno, D A; Carvajal, M; López-Berenguer, C; García-Viguera, C

    2006-08-28

    People's diet offers a greater and more diverse group of plant bioactives than do drugs, and they often do not realise that many drugs are derived from the compounds originally discovered in plant foods. Numerous epidemiological studies indicate that Brassica vegetables in general, and broccoli in particular, protect humans against cancer since they are rich sources of glucosinolates as well as possessing a high content of flavonoids, vitamins and mineral nutrients. One unusual phytotherapeutic role of broccoli is for skin diseases--the juice of the leaves is used to treat warts. However, the main use of broccoli stems from its health-promoting properties. Some criteria have been proposed to evaluate the possibilities of developing new "functional foods" to reduce the risk of specific cancers; largely in broccoli, which is associated with cancer protection. Processing conditions, transport, domestic cooking, etc., affect the health-promoting properties of broccoli and these have been widely studied. This review makes an in-depth study of the chemical and biological characterization of the phytochemicals of broccoli and the effects on the bioactive composition of broccoli.

  7. Biologically active phenols from Saussurea medusa.

    PubMed

    Fan, Cheng-Qi; Yue, Jian-Min

    2003-03-06

    Sixteen phenolic compounds were isolated from the polar fraction of Saussurea medusa and were structurally elucidated by chemical evidences and spectral methods. These compounds include two new lignan glucosides, namely medusasides A (1) and B (2), and fourteen known phenolic compounds (3-16). One major compound, apigenin 7-O-[alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside] (6) showed remarkable activity to attenuate the scopolamine induced memory deficit of mice. Compound 6 and another major one, quercetin (8) also exhibited moderate cell protecting activities against hydrogen peroxide (H(2)O(2)) induced PC12 cell damage.

  8. Antiplasmodial activity of some phenolic compounds from Cameroonians Allanblackia.

    PubMed

    Azebaze, Anatole Guy Blaise; Teinkela, Jean Emmanuel Mbosso; Nguemfo, Edwige Laure; Valentin, Alexis; Dongmo, Alain Bertrand; Vardamides, Juliette Catherine

    2015-09-01

    Plasmodium falciparum, one of the causative agents of malaria, has high adaptability through mutation and is resistant to many types of anti-malarial drugs. This study presents an in vitro assessment of the antiplasmodial activity of some phenolic compounds isolated from plants of the genus Allanblackia. Tests were performed on well plates filled with a fixed parasitized erythrocytes volume. Compounds to be tested were then added in wells. After incubation, tritiated hypoxanthine is added and the plates were returned to the incubator. After thawing, the nucleic acids are collected. Inhibitory Concentration 50 (IC50) was determined by linear interpolation. From Allanblackia floribunda, have been isolated and characterized 1,7-dihydroxyxanthone 1, macluraxanthone 4, morelloflavone 9, Volkensiflavone 10 and morelloflavone 7-O-glucoside 11; from Allanblackia monticola, α-mangosine 2, rubraxanthone 3, allaxanthone C 5, norcowanine 6, tovophiline A 7, allaxanthone B 8 and from Allanblackia gabonensis, 1,7-dihydroxyxanthone 1. Six of them were evaluated for their antimalarial properties. The most active compound, macluraxanthone, presented a very interesting activity, with an IC50 of 0.36 and 0.27 µg/mL with the F32 and FcM29 strains respectively. This work confirms that species of Allanblackia genus are medicinally important plants containing many biologically active compounds that can be used effectively as antiplasmodial.

  9. 1,3,4-oxadiazole: a biologically active scaffold.

    PubMed

    Khalilullah, H; Ahsan, M J; Hedaitullah, Md; Khan, S; Ahmed, B

    2012-07-01

    There has been considerable interest in the development of novel compounds with anticonvulsant, antidepressant, analgesic, anti-inflammatory, antiallergic, antipsychotic, antimicrobial, antimycobecterial, antitumour, antiviral and antitubercular activities. 1,3,4-oxadiazoles 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 led to the development of new 1,3,4-oxadiazole derivatives. This review article describes the various biological activities associated with 1,3,4-oxadiazole ring system and is useful in guiding the researchers across the world working on this moiety and consequently have been instrumental in the advancement of 1,3,4-oxadiazole chemistry.

  10. Investigating biological activity spectrum for novel quinoline analogues.

    PubMed

    Musiol, Robert; Jampilek, Josef; Kralova, Katarina; Richardson, Des R; Kalinowski, Danuta; Podeszwa, Barbara; Finster, Jacek; Niedbala, Halina; Palka, Anna; Polanski, Jaroslaw

    2007-02-01

    The lack of the wide spectrum of biological data is an important obstacle preventing the efficient molecular design. Quinoline derivatives are known to exhibit a variety of biological effects. In the current publication, we tested a series of novel quinoline analogues for their photosynthesis-inhibiting activity (the inhibition of photosynthetic electron transport in spinach chloroplasts (Spinacia oleracea L.) and the reduction of chlorophyll content in Chlorella vulgaris Beij.). Moreover, antiproliferative activity was measured using SK-N-MC neuroepithelioma cell line. We described the structure-activity relationships (SAR) between the chemical structure and biological effects of the synthesized compounds. We also measured the lipophilicity of the novel compounds by means of the RP-HPLC and illustrate the relationships between the RP-HPLC retention parameter logK (the logarithm of capacity factor K) and logP data calculated by available programs.

  11. Systemically and Topically Active Antinociceptive Neurotensin Compounds

    PubMed Central

    Rossi, Grace C.; Matulonis, Joshua E.; Richelson, Elliott; Barbut, Denise

    2010-01-01

    Neurotensin is a neurotransmitter/modulator with a wide range of actions. Using a series of 10 stable analogs, we have examined neurotensin antinociception in mice. By incorporating (2S)-2-amino-3-(1H-4-indoyl)propanoic acid (l-neoTrp), a series of neurotensin analogs have been synthesized that are stable in serum and are systemically active in vivo. When administered in mice, they all were antinociceptive in the radiant heat tail-flick assay. Time-action curves revealed a peak effect at 30 min and a duration of action ranging from 2 to 4 h. Dose-response curves revealed that two compounds were partial agonists with maximal responses below 75%, whereas all of the remaining compounds displayed a full response. Overall, the compounds were quite potent, with ED50 values similar to those of opioids. At peak effect, the ED50 values ranged from 0.91 to 9.7 mg/kg s.c. Two of the analogs were active topically. Together, these studies support the potential of neurotensin analogs as analgesics. They are active systemically and by using them topically, it may be possible to avoid problematic side effects, such as hypothermia and hypotension. PMID:20576795

  12. Selenium Compounds Activate Early Barriers of Tumorigenesis*

    PubMed Central

    Wu, Min; Kang, Mandy M.; Schoene, Norberta W.; Cheng, Wen-Hsing

    2010-01-01

    Selenium chemoprevention by apoptosis has been well studied, but it is not clear whether selenium can activate early barriers of tumorigenesis, namely senescence and DNA damage response. To test this hypothesis, we treated normal and cancerous cells with a gradient concentration of sodium selenite, methylseleninic acid and methylselenocysteine for 48 h, followed by a recovery of 1–7 days. Here we show that selenium compounds at doses of ≤LD50 can induce cellular senescence, as evidenced by the expression of senescence-associated β-galactosidase and 5-bromo-2-deoxyuridine incorporation, in normal but not cancerous cells. In response to clastogens, the ataxia telangiectasia mutated (ATM) protein is rapidly activated, which in turn initiates a cascade of DNA damage response. We found that the ATM pathway is activated by the selenium compounds, and the kinase activity is required for the selenium-induced senescence response. Pretreatment of the MRC-5 non-cancerous cells with the antioxidant N-acetylcysteine or 2,2,6,6-tetramethylpiperidine-1-oxyl suppresses the selenium-induced ATM activation and senescence. Taken together, the results suggest a novel role of selenium in the activation of early tumorigenesis barriers specific in non-cancerous cells, whereby selenium induces an ATM-dependent senescence response that depends on reactive oxygen species. PMID:20157118

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

    PubMed

    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.

  14. Biological activity of some conjugated gibberellins.

    PubMed

    Sembdner, G; Borgmann, E; Schneider, G; Liebisch, H W; Miersch, O; Adam, G; Lischewski, M; Schrefber, K

    1976-01-01

    The biological activity of several gibberellin (GA) conjugates was studied and compared with that of the corresponding free GAs. The following conjugates were included: O(3)-β-D-glucopyranosides of GA1, GA3 and GA4; O(13)-β-D-glucopyranosides of GA1, GA3 and GA5; O(13)-β-D-glucopyranosyl-GA5-β-D-glucopyranosyl ester; GA3-β-D-glucopyranosyl ester and GA3-α-D-glucopyranosyl ester; N-GA3-oyl-glycine, its methyl ester, N-GA3-oyl-glycylglycine, and N-GA3-oyl-proline. All compounds were synthesized chemically but some of them are known to occur as endogenous plant products, or to be formed in plants upon application of a free GA. Activity was determined in the dwarf pea, dwarf corn, dwarf rice, and lettuce hypocotyl bioassays. The GA conjugates were found to posses different relative activities depending on the chemical structure, the bioassay system, and the site of application (shoot or roots). It is concluded that the activity of GA conjugates as measured in different bioassays is based upon the ability of plant enzymes and possibly of certain microorganisms to hydrolyze glucosidic, glucosyl ester, and amide-like linkages.

  15. Concepts for Biologically Active Peptides

    PubMed Central

    Kastin, Abba J.; Pan, Weihong

    2012-01-01

    Here we review a unique aspect of CNS research on biologically active peptides that started against a background of prevalent dogmas but ended by exerting considerable influence on the field. During the course of refuting some doctrines, we introduced several concepts that were unconventional and paradigm-shifting at the time. We showed that (1) hypothalamic peptides can act ‘up’ on the brain as well as ‘down’ on the pituitary, (2) peripheral peptides can affect the brain, (3) peptides can cross the blood-brain barrier, (4) the actions of peptides can persist longer than their half-lives in blood, (5) perinatal administration of peptides can exert actions persisting into adulthood, (6) a single peptide can have more than one action, (7) dose-response relationships of peptides need not be linear, (8) the brain produces antiopiate as well as opiate peptides, (9) there is a selective high affinity endogenous peptide ligand for the mu-opiate receptor, (10) a peptide’s name does not restrict its effects, and (11) astrocytes assume an active role in response to metabolic disturbance and hyperleptinemia. The evolving questions in our laboratories reflect the diligent effort of the neuropeptide community to identify the roles of peptides in the CNS. The next decade is expected to see greater progress in the following areas: (a) interactions of peptides with other molecules in the CNS; (b) peptide involvement in cell-cell interactions; and (c) peptides in neuropsychiatric, autoimmune, and neurodegenerative diseases. The development of peptidomics and gene silencing approaches will expedite the formation of many new concepts in a new era. PMID:20726835

  16. Natural compounds with anti-ageing activity.

    PubMed

    Argyropoulou, Aikaterini; Aligiannis, Nektarios; Trougakos, Ioannis P; Skaltsounis, Alexios-Leandros

    2013-10-11

    Ageing is a complex molecular process driven by diverse molecular pathways and biochemical events that are promoted by both environmental and genetic factors. Specifically, ageing is defined as a time-dependent decline of functional capacity and stress resistance, associated with increased chance of morbidity and mortality. These effects relate to age-related gradual accumulation of stressors that result in increasingly damaged biomolecules which eventually compromise cellular homeostasis. Nevertheless, the findings that genetic or diet interventions can increase lifespan in evolutionarily diverse organisms indicate that mortality can be postponed. Natural compounds represent an extraordinary inventory of high diversity structural scaffolds that can offer promising candidate chemical entities in the major healthcare challenge of increasing health span and/or delaying ageing. Herein, those natural compounds (either pure forms or extracts) that have been found to delay cellular senescence or in vivo ageing will be critically reviewed and summarized according to affected cellular signalling pathways. Moreover, the chemical structures of the identified natural compounds along with the profile of extracts related to their bioactive components will be presented and discussed. Finally, novel potential molecular targets for screening natural compounds for anti-ageing activity, as well as the idea that anti-ageing interventions represent a systemic approach that is also effective against age-related diseases will be discussed.

  17. Biologically active proteins from natural product extracts.

    PubMed

    O'Keefe, B R

    2001-10-01

    The term "biologically active proteins" is almost redundant. All proteins produced by living creatures are, by their very nature, biologically active to some extent in their homologous species. In this review, a subset of these proteins will be discussed that are biologically active in heterologous systems. The isolation and characterization of novel proteins from natural product extracts including those derived from microorganisms, plants, insects, terrestrial vertebrates, and marine organisms will be reviewed and grouped into several distinct classes based on their biological activity and their structure.

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

    PubMed

    Tangerman, Albert

    2009-10-15

    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) group and appear in the free gaseous form, in the acid-labile form and in the dithiothreitol-labile form. Dimethyl sulfide is a neutral molecule and exists only in the free form. The foul odor of these sulfur volatiles is a striking characteristic and plays a major role in bad breath, feces and flatus. Because sulfur is a biologically active element, the biological significance of the sulfur volatiles are also highlighted. Despite its highly toxic properties, hydrogen sulfide has been lately recommended to become the third gasotransmitter, next to nitric oxide and carbon monoxide, based on high concentration found in healthy tissues, such as blood and brain. However, there is much doubt about the reliability of the assay methods used. Many artifacts in the sulfide assays exist. The methods to detect the various forms of hydrogen sulfide are critically reviewed and compared with findings of our group. Recent findings that free gaseous hydrogen sulfide is absent in whole blood urged the need to revisit its role as a blood-borne signaling molecule.

  19. Myricetin: A Dietary Molecule with Diverse Biological Activities.

    PubMed

    Semwal, Deepak Kumar; Semwal, Ruchi Badoni; Combrinck, Sandra; Viljoen, Alvaro

    2016-02-16

    Myricetin is a common plant-derived flavonoid and is well recognised for its nutraceuticals value. It is one of the key ingredients of various foods and beverages. The compound exhibits a wide range of activities that include strong anti-oxidant, anticancer, antidiabetic and anti-inflammatory activities. It displays several activities that are related to the central nervous system and numerous studies have suggested that the compound may be beneficial to protect against diseases such as Parkinson's and Alzheimer's. The use of myricetin as a preserving agent to extend the shelf life of foods containing oils and fats is attributed to the compound's ability to protect lipids against oxidation. A detailed search of existing literature revealed that there is currently no comprehensive review available on this important molecule. Hence, the present work includes the history, synthesis, pharmaceutical applications and toxicity studies of myricetin. This report also highlights structure-activity relationships and mechanisms of action for various biological activities.

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

    NASA Astrophysics Data System (ADS)

    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. Biological process for the elimination of sulphur compounds present in gas mixtures

    SciTech Connect

    Torres-Cardona, M.D.; Revah-Moiseev, S.; Hinojosa-Martinez, A.; Paez-Moreno, F.J.; Morales-Baca, V.M.

    1993-08-17

    A continuous process is described for the microbiological conversion and removal of malodorous sulphur-containing organic and inorganic compounds from a gaseous stream, comprising the steps of: (a) providing a column filled with packing material; (b) passing a biologically active liquid stream containing nutrients and bacteria comprising microorganisms of the Thiobacillaceae family through the column whereby the bacteria are immobilized onto all available surface area of the packing material; (c) maintaining the temperature conditions in the column between about 5 C to about 47 C and pH conditions between about 5 to about 9; and (d) concurrently passing a gaseous stream containing the malodorous sulphur-containing organic and inorganic compounds at a liquid/gas mass ratio of about 3:7 for a sufficient period of time so as to allow the bacteria to excrete converted sulphur compounds and recover said converted sulphur compounds as elemental sulphur from the liquid, wherein the excreted and recovered elemental sulphur is in an amount greater than about 97% of said converted sulphur compounds.

  2. 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

    PubMed Central

    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

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

    PubMed

    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

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

    PubMed

    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.

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

    PubMed Central

    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

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

    PubMed

    Adhikari, Bal-Ram; Govindhan, Maduraiveeran; Chen, Aicheng

    2015-09-04

    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.

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

    PubMed Central

    Adhikari, Bal-Ram; Govindhan, Maduraiveeran; Chen, Aicheng

    2015-01-01

    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. PMID:26404304

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

    PubMed

    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.

  9. Synthesis, investigation of the new derivatives of dihydropyrimidines and determination of their biological activity

    NASA Astrophysics Data System (ADS)

    Maharramov, A. M.; Ramazanov, M. A.; Guliyeva, G. A.; Huseynzada, A. E.; Hasanova, U. A.; Shikhaliyev, N. G.; Eyvazova, G. M.; Hajiyeva, S. F.; Mamedov, I. G.; Aghayev, M. M.

    2017-08-01

    We reported of synthesis and investigation of the new biologically active derivatives of dihydropyrimidines 2 and 3. The investigation of structures of compounds by various experiments of NMR spectroscopy revealed the splitting of the signals to doublets and multiplets that confirms the presence of diastereomers in solution of compound 2 and the presence of diastereomers and tautomers in solution of compound 3. The individual diastereomer of compound 3 has been isolated. Biological activity of the synthesized compounds was studied on various species of genus Aspergillus fungi.

  10. Sulfation and biological activities of konjac glucomannan.

    PubMed

    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. Copyright © 2013. Published by Elsevier Ltd.

  11. SYNTHESIS AND BIOLOGICAL EVALUATION OF BIARYL ANALOGS OF ANTITUBULIN COMPOUNDS

    PubMed Central

    Tozatti, Camila Santos Suniga; Khodyuk, Rejane Gonçalves Diniz; da Silva, Adriano Olimpio; dos Santos, Edson dos Anjos; de Lima, Marcos Serrou do Amaral e Dênis Pires; Hamel, Ernest

    2012-01-01

    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 [3H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site. PMID:23087491

  12. SYNTHESIS AND BIOLOGICAL EVALUATION OF BIARYL ANALOGS OF ANTITUBULIN COMPOUNDS.

    PubMed

    Tozatti, Camila Santos Suniga; Khodyuk, Rejane Gonçalves Diniz; da Silva, Adriano Olimpio; Dos Santos, Edson Dos Anjos; de Lima, Marcos Serrou do Amaral E Dênis Pires; Hamel, Ernest

    2012-01-01

    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 [(3)H] colchicine to tubulin, suggesting that, akin to phenstatin and combretastatin A-4, they can bind to tubulin at the colchicine site.

  13. Some recent approaches of biologically active substituted pyridazine and phthalazine drugs.

    PubMed

    Asif, M

    2012-01-01

    Nitrogen atom containing heterocyclic compounds, pyridazines, pyridazinones and phthalazines are important structural feature of many biologically active compounds and show diverse pharmacological properties. Pyridazines and phthalazines hold considerable interest relative to the preparation of organic intermediates and physiologically active compounds. On the basis of literature, pyridazines, pyridazinone and phthalazines further focus our attention because of their easy fictionalization at various ring positions, which makes them attractive synthetic compounds for designing and development of the novel pyridazines and phthalazines drugs in future.

  14. Novel Antiproliferative Chimeric Compounds with Marked Histone Deacetylase Inhibitory Activity

    PubMed Central

    2014-01-01

    Given our interest in finding potential antitumor agents and in view of the multifactorial mechanistic nature of cancer, in the present work, taking advantage of the multifunctional ligands approach, new chimeric molecules were designed and synthesized by combining in single chemical entities structural features of SAHA, targeting histone deacetylases (HDACs), with substituted stilbene or terphenyl derivatives previously obtained by us and endowed with antiproliferative and pro-apoptotic activity. The new chimeric derivatives were characterized with respect to their cytotoxic activity and their effects on cell cycle progression on different tumor cell lines, as well as their HDACs inhibition. Among the other, trans-6 showed the most interesting biological profile, as it exhibited a strong pro-apoptotic activity in tumor cell lines in comparison with both of its parent compounds and a marked HDAC inhibition. PMID:25221651

  15. Biologically active secondary metabolites from Asphodelus microcarpus.

    PubMed

    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.

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

    PubMed

    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. Copyright © 2016 John Wiley & Sons, Ltd.

  17. Potential bioactive Schiff base compounds: Synthesis, characterization, X-ray structures, biological screenings and interaction with Salmon sperm DNA

    NASA Astrophysics Data System (ADS)

    Sirajuddin, Muhammad; Uddin, Noor; Ali, Saqib; Tahir, Muhammad Nawaz

    2013-12-01

    Three Schiff base compounds ofN‧-substituted benzohydrazide and sulfonohydrazide derivatives: N‧-(2-hydroxy-3-methoxybenzylidene)-4-tert-butyl- benzohydrazide (1), N‧-(5-bromo-2-hydroxybenzylidene)-4-tert-butylbenzohydrazide (2) and N‧-(2-hydroxy-3-methoxybenzylidene)-4-methylbenzenesulfonohydrazide (3) were synthesized and characterized by elemental analysis, FT-IR, 1H, 13C NMR spectroscopy and single crystal analysis. The title compounds have been screened for their biological activities including, antibacterial, antifungal, antioxidant, cytotoxic, enzymatic activities as well as interaction with SS-DNA which showed remarkable activities in each area of research. The DNA binding of the compounds 1-3 with SS-DNA has been carried out with absorption spectroscopy, which reveals the binding propensity towards SS-DNA via intercalation mode of interaction. The intercalative mode of interaction is also supported by viscometric results. The synthesized compounds were also found to be effective against alkaline phosphatase enzyme. They also show significant to good antimicrobial activity against six bacterial and five fungal strains. The MIC (minimum inhibitory concentration) for antibacterial activity ranges from 1.95-500 μg/mL. Compounds 1-3 show cytotoxic activity comparable to the control. At higher conc. (100 μg/L) compound 3 shows 100% activity means that it has killed all brine shrimps. They were also found to be effective antioxidant of 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) and show almost comparable antioxidant activity to that of the standard and known antioxidant, ascorbic acid.

  18. Imidazolium compounds are active against all stages of Trypanosoma cruzi.

    PubMed

    Faral-Tello, Paula; Liang, Mary; Mahler, Graciela; Wipf, Peter; Robello, Carlos

    2014-03-01

    Imidazolium salts are best known for their applications in organic synthesis as room-temperature ionic liquids, or as precursors of stable carbenes, but they also show important biological properties such as anti-oxidative effects, induction of mitochondrial membrane permeabilisation and inhibition of the infection cycle of Plasmodium falciparum. For these reasons, and since chemotherapy for Chagas disease is inefficient, the aim of this study was to test the use of imidazolium compounds against the kinetoplastid haemoflagellate aetiological agent for this disease, namely Trypanosoma cruzi. The results show that five of the tested compounds are more effective than the reference drug benznidazole against the epimastigote and trypomastigote forms of T. cruzi. Moreover, intracellular amastigotes were also affected by the compounds, which showed lower toxicity in host cells. Transmission electron microscopy analysis demonstrated that the tested agents induced alterations of the kinetoplast and particularly of the mitochondria, leading to extraordinary swelling of the organelle. These results further demonstrate that the test agents with the best profile are those bearing symmetrical bulky substituents at N(1) and N(3), displaying promising activity against all forms of T. cruzi, interesting selectivity indexes and exceptional activity at low doses. Accordingly, these agents represent promising candidates for the treatment of Chagas disease.

  19. Structure activity relationships: their function in biological prediction

    SciTech Connect

    Schultz, T.W.

    1982-01-01

    Quantitative structure activity relationships provide a means of ranking or predicting biological effects based on chemical structure. For each compound used to formulate a structure activity model two kinds of quantitative information are required: (1) biological activity and (2) molecular properties. Molecular properties are of three types: (1) molecular shape, (2) physiochemical parameters, and (3) abstract quantitations of molecular structure. Currently the two best descriptors are the hydrophobic parameter, log 1-octanol/water partition coefficient (log P), and the /sup 1/X/sup v/(one-chi-v) molecular connectivity index. Biological responses can be divided into three main categories: (1) non-specific effects due to membrane perturbation, (2) non-specific effects due to interaction with functional groups of proteins, and (3) specific effects due to interaction with receptors. Twenty-six synthetic fossil fuel-related nitrogen-containing aromatic compounds were examined to determine the quantitative correlation between log P and /sup 1/X/sup v/ and population growth impairment of Tetrahymena pyriformis. Nitro-containing compounds are the most active, followed by amino-containing compounds and azaarenes. Within each analog series activity increases with alkyl substitution and ring addition. The planar model log BR = 0.5564 log P + 0.3000 /sup 1/X/sup v/ -2.0138 was determined using mono-nitrogen substituted compounds. Attempts to extrapolate this model to dinitrogen-containing molecules were, for the most part, unsuccessful because of a change in mode of action from membrane perturbation to uncoupling of oxidative phosphoralation.

  20. Biological activities of xanthatin from Xanthium strumarium leaves.

    PubMed

    Nibret, Endalkachew; Youns, Mahamoud; Krauth-Siegel, R Luise; Wink, Michael

    2011-12-01

    The objective of the present work was to evaluate the biological activities of the major bioactive compound, xanthatin, and other compounds from Xanthium strumarium (Asteraceae) leaves. Inhibition of bloodstream forms of Trypanosoma brucei brucei and leukaemia HL-60 cell proliferation was assessed using resazurin as a vital stain. Xanthatin was found to be the major and most active compound against T. b. brucei with an IC(50) value of 2.63 µg/mL and a selectivity index of 20. The possible mode of action of xanthatin was further evaluated. Xanthatin showed antiinflammatory activity by inhibiting both PGE(2) synthesis (24% inhibition) and 5-lipoxygenase activity (92% inhibition) at concentrations of 100 µg/mL and 97 µg/mL, respectively. Xanthatin exhibited weak irreversible inhibition of parasite specific trypanothione reductase. Unlike xanthatin, diminazene aceturate and ethidium bromide showed strong DNA intercalation with IC(50) values of 26.04 µg/mL and 44.70 µg/mL, respectively. Substantial induction of caspase 3/7 activity in MIA PaCa-2 cells was observed after 6 h of treatment with 100 µg/mL of xanthatin. All these data taken together suggest that xanthatin exerts its biological activity by inducing apoptosis and inhibiting both PGE(2) synthesis and 5-lipoxygenase activity thereby avoiding unwanted inflammation commonly observed in diseases such as trypanosomiasis.

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

    PubMed Central

    Rajashekar, V; Rao, E Upender; P, Srinivas

    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. PMID:23569975

  2. [Small compounds libraries: a research tool for chemical biology].

    PubMed

    Florent, Jean-Claude

    2013-01-01

    Obtaining and screening collections of small molecules remain a challenge for biologists. Recent advances in analytical techniques and instrumentation now make screening possible in academia. The history of the creation of such public or commercial collections and their accessibility is related. It shows that there is interest for an academic laboratory involved in medicinal chemistry, chemogenomics or "chemical biology" to organize its own collection and make it available through existing networks such as the French National chimiothèque or the European partner network "European Infrastructure of open screening platforms for Chemical Biology" EU-OpenScreen under construction. © Société de Biologie, 2013.

  3. Biological activities of novel gyrase inhibitors of the aminocoumarin class.

    PubMed

    Anderle, Christine; Stieger, Martin; Burrell, Matthew; Reinelt, Stefan; Maxwell, Anthony; Page, Malcolm; Heide, Lutz

    2008-06-01

    Thirty-one aminocoumarin antibiotics derived from mutasynthesis experiments were investigated for their biological activities. Their inhibitory activities toward Escherichia coli DNA gyrase were determined in two different in vitro assays: an ATPase assay and a DNA supercoiling assay. The assays gave a similar rank order of the activities of the compounds tested, although the absolute 50% inhibitory concentrations (IC(50)s) obtained in each assay were different. To confirm that the compounds also acted as gyrase inhibitors in vivo, reporter gene assays were carried out with E. coli by using gyrA and sulA promoter fusions with the luxCDABE operon. A strong induction of both promoters was observed for those compounds that showed gyrase inhibitory activity in the biochemical assays. Compounds carrying analogs of the prenylated benzoyl moiety (ring A) of clorobiocin that were structurally very different showed high levels of activity both in the biochemical assay and in the reporter gene assay, indicating that the structure of this moiety can be varied considerably without a loss of affinity for bacterial gyrase. The experimentally determined IC(50)s were compared to the binding energies calculated in silico, which indicated that a shift of the pyrrole carboxylic acid moiety from the O-3'' to the O-2'' position of the deoxysugar moiety has a significant impact on the binding mode of the compounds. The aminocoumarin compounds were also investigated for their MICs against different bacterial pathogens. Several compounds showed high levels of activity against staphylococci, including a methicillin-resistant Staphylococcus aureus strain. However, they showed only poor activities against gram-negative strains.

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

    PubMed Central

    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

  5. Ethnobotany, chemistry, and biological activities of the genus Tithonia (Asteraceae).

    PubMed

    Chagas-Paula, Daniela A; Oliveira, Rejane B; Rocha, Bruno A; Da Costa, Fernando B

    2012-02-01

    The genus Tithonia is an important source of diverse natural products, particularly sesquiterpene lactones, diterpenes, and flavonoids. The collected information in this review attempts to summarize the recent developments in the ethnobotany, biological activities, and secondary metabolite chemistry of this genus. More than 100 structures of natural products from Tithonia are reported in this review. The species that has been most investigated in this genus is T. diversifolia, from which ca. 150 compounds were isolated. Biological studies are described to evaluate the anti-inflammatory, analgesic, antimalarial, antiviral, antidiabetic, antidiarrhoeal, antimicrobial, antispasmodic, vasorelaxant, cancer-chemopreventive, cytotoxic, toxicological, bioinsecticide, and repellent activities. A few of these studies have been carried out with isolated compounds from Tithonia species, but the majority has been conducted with different extracts. The relationship between the biological activity and the toxicity of compounds isolated from the plants of this genus as well as T. diversifolia extracts still remains unclear, and mechanisms of action remain to be determined. Copyright © 2012 Verlag Helvetica Chimica Acta AG, Zürich.

  6. [Biological activity of probiotic microorganisms].

    PubMed

    Novik, G I; Samartsev, A A; Astapovich, N I; Kavrus, M A; Mikhaliuk, A N

    2006-01-01

    Adaptation of bifidobacteria and lactic acid bacteria to nutrient media with increased concentrations of bile (1%) and protein substrates of animal origin allowed the variants resistant to bile and displaying a high production of proteolytic enzymes (active within the pH range of 2.5-9.0) to be selected. Administration of the preparations involving the selected bifidobacteria and lactic acid bacteria assisted in the normalization of the intestinal microflora and activation of protein metabolism in the organism of animals. Specifically, it increased the total protein level in blood serum and redistributed protein fractions, increasing the content of globulins and decreasing albumin concentration.

  7. Titanates and Titanate-Metal Compounds in Biological Contexts

    PubMed Central

    Chen, Yen-Wei; Drury, Jeanie L.; Chung, Whasun Oh; Hobbs, David T.; Wataha, John C.

    2015-01-01

    Metal ions are notorious environmental contaminants, some causing toxicity at exquisitely low (ppm-level) concentrations. Yet, the redox properties of metal ions make them attractive candidates for bio-therapeutics. Titanates are insoluble particulate compounds of titanium and oxygen with crystalline surfaces that bind metal ions; these compounds offer a means to scavenge metal ions in environmental contexts or deliver them in therapeutic contexts while limiting systemic exposure and toxicity. In either application, the toxicological properties of titanates are crucial. To date, the accurate measurement of the in vitro toxicity of titanates has been complicated by their particulate nature, which interferes with many assays that are optical density (OD)-dependent, and at present, little to no in vivo titanate toxicity data exist. Compatibility data garnered thus far for native titanates in vitro are inconsistent and lacking in mechanistic understanding. These data suggest that native titanates have little toxicity toward several oral and skin bacteria species, but do suppress mammalian cell metabolism in a cells-pecific manner. Titanate compounds bind several types of metal ions, including some common environmental toxins, and enhance delivery to bacteria or cells. Substantial work remains to address the practical applicability of titanates. Nevertheless, titanates have promise to serve as novel vehicles for metal-based therapeutics or as a new class of metal scavengers for environmental applications. PMID:26430701

  8. Biological activity of liposomal vanillin.

    PubMed

    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.

  9. Biological and Clinical Aspects of Lanthanide Coordination Compounds

    PubMed Central

    Misra, Sudhindra N.; M., Indira Devi; Shukla, Ram S.

    2004-01-01

    The coordinating chemistry of lanthanides, relevant to the biological, biochemical and medical aspects, makes a significant contribution to understanding the basis of application of lanthanides, particularly in biological and medical systems. The importance of the applications of lanthanides, as an excellent diagnostic and prognostic probe in clinical diagnostics, and an anticancer material, is remarkably increasing. Lanthanide complexes based X-ray contrast imaging and lanthanide chelates based contrast enhancing agents for magnetic resonance imaging (MRI) are being excessively used in radiological analysis in our body systems. The most important property of the chelating agents, in lanthanide chelate complex, is its ability to alter the behaviour of lanthanide ion with which it binds in biological systems, and the chelation markedly modifies the biodistribution and excretion profile of the lanthanide ions. The chelating agents, especially aminopoly carboxylic acids, being hydrophilic, increase the proportion of their complex excreted from complexed lanthanide ion form biological systems. Lanthanide polyamino carboxylate-chelate complexes are used as contrast enhancing agents for Magnetic Resonance Imaging. Conjugation of antibodies and other tissue specific molecules to lanthanide chelates has led to a new type of specific MRI contrast agents and their conjugated MRI contrast agents with improved relaxivity, functioning in the body similar to drugs. Many specific features of contrast agent assisted MRI make it particularly effective for musculoskeletal and cerebrospinal imaging. Lanthanide-chelate contrast agents are effectively used in clinical diagnostic investigations involving cerebrospinal diseases and in evaluation of central nervous system. Chelated lanthanide complexes shift reagent aided 23Na NMR spectroscopic analysis is used in cellular, tissue and whole organ systems. PMID:18365075

  10. Synthesis and preliminary biological evaluation of a compound library of triazolylcyclitols.

    PubMed

    Carrau, Gonzalo; Drewes, Carine C; Shimada, Ana Lúcia B; Bertucci, Ana; Farsky, Sandra H P; Stefani, Helio A; Gonzalez, David

    2013-07-15

    A small library of compounds was prepared by a combination of toluene dioxygenase (TDO)-catalyzed enzymatic dihydroxylation and copper(I)-catalyzed Hüisgen cycloaddition. Some compounds were obtained by coupling an alkyne and a conduritol derivative, while more complex structures were obtained by a double Hüisgen reaction of a dialkyne and two molecules of the cyclitol. The compounds were fully characterized and subjected to preliminary biological screening.

  11. Biological profile and bioavailability of imidazoline compounds on morphine tolerance modulation.

    PubMed

    Caprioli, Giovanni; Mammoli, Valerio; Ricciutelli, Massimo; Sagratini, Gianni; Ubaldi, Massimo; Domi, Esi; Mennuni, Laura; Sabatini, Chiara; Galimberti, Chiara; Ferrari, Flora; Milia, Chiara; Comi, Eleonora; Lanza, Marco; Giannella, Mario; Pigini, Maria; Del Bello, Fabio

    2015-12-15

    Tolerance to opioid administration represents a serious medical alert in different chronic conditions. This study compares the effects of the imidazoline compounds 1, 2, and 3 on morphine tolerance in an animal model of inflammatory pain in the rat. 1, 2, and 3 have been selected in that, although bearing a common scaffold, preferentially bind to α2-adrenoceptors, imidazoline I2 receptors, or both systems, respectively. Such compounds have been tested in vivo by measuring the paw withdrawal threshold to mechanical pressure after complete Freund's adjuvant injection. To determine the ligand levels in rat plasma, an HPLC-mass spectrometry method has been developed. All the compounds significantly reduced the induction of morphine tolerance, showing different potency and duration of action. Indeed, the selective imidazoline I2 receptor interaction (2) restored the analgesic response by maintaining the same time-dependent profile observed after a single morphine administration. Differently, the selective α2C-adrenoceptor activation (1) or the combination between α2C-adrenoceptor activation and imidazoline I2 receptor engagement (3) promoted a change in the temporal profile of morphine analgesia by maintaining a mild but long lasting analgesic effect. Interestingly, the kinetics of compounds in rat plasma supported the pharmacodynamic data. Therefore, this study highlights that both peculiar biological profile and bioavailability of such ligands complement each other to modulate the reduction of morphine tolerance. Based on these observations, 1-3 can be considered useful leads in the design of new drugs able to turn off the undesired tolerance induced by opioids.

  12. Synthesis and Biological Activities of Oxadiazole Derivatives: A Review.

    PubMed

    Vaidya, Ankur; Jain, Shweta; Jain, Priyanka; Jain, Prachi; Tiwari, Nidhi; Jain, Roshni; Jain, Rashi; Jain, Abhishek K; Agrawal, Ram K

    2016-01-01

    Recently, there has been wide interest in compounds containing the oxadiazole scaffold because of their unique chemical structure and their broad spectrum of biological properties. This review provides readers with an overview of the main synthetic methodologies for oxadiazoles and of their broad spectrum of pharmacological activities such as, anti-microbial, anti-fungal activity, antiviral, anti-tubercular, anti-inflammatory, anti-convulsant, anti-angiogenic, anti-proliferative, analgesic, anti-oedema and in alzheimer activity, which were reported over the past years.

  13. Bioactive components and functional properties of biologically activated cereal grains: A bibliographic review.

    PubMed

    Singh, Arashdeep; Sharma, Savita

    2017-09-22

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

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

    PubMed

    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.

  15. Marine Pyridoacridine Alkaloids: Biosynthesis and Biological Activities.

    PubMed

    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.

  16. Simultaneous gas chromatographic determination of dibutyltin and tributyltin compounds in biological and sediment samples

    SciTech Connect

    Tsuda, T.; Nakanishi, H.; Morita, T.; Takebayashi, J.

    1986-11-01

    A method is described for the simultaneous determination of nanogram amounts of dibutyltin and tributyltin compounds in biological and sediment samples. These compounds are converted to the corresponding chlorides with HCl, extracted with ethyl acetate-hexane (3 + 2) for biological samples and with hexane for sediment samples, and hydrogenated with sodium borohydride. The corresponding hydrides, Bu2SnH2 and Bu3SnH, are detected by electron-capture gas chromatography after cleanup by silica gel column chromatography. Detection limits are 1.0-2.0 and 0.5-1.0 ng/g, respectively, for biological and sediment samples.

  17. Non-biological inhibition-based sensing (NIBS) demonstrated for the detection of toxic arsenic compounds.

    PubMed

    Monty, Chelsea N; Londoño, Nicolas J; Masel, Richard I

    2011-03-01

    This work demonstrates the success of a recently developed technique in chemical amplification, non-biological inhibition-based sensing (NIBS), for the detection of toxic arsenic compounds. Screening for toxic arsenic compounds is especially important due to their prevalence in wastewater and water sources. The detection method presented in this work amplifies the chemical response of toxic arsenic compounds by developing a sensor chemistry where the analyte inhibits, rather than enhances, the rate of a catalytic reaction. This technique mimics the work done with enzyme inhibition; however, using non-biological molecules allows for selective detection without the shelf-life issue associated with biological molecules. Using NIBS we find that we can enhance the sensitivity of the system by two orders of magnitude with no apparent loss in selectivity. This work demonstrates the versatility of NIBS, showing that the technique can be of general use for the detection of toxic compounds. Copyright © 2010 Elsevier Ltd. All rights reserved.

  18. Marine Biology Activities. Ocean Related Curriculum Activities.

    ERIC Educational Resources Information Center

    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…

  19. Ionic surface active compounds in atmospheric aerosols.

    PubMed

    Sukhapan, Jariya; Brimblecombe, Peter

    2002-04-27

    Surfactants in the atmosphere have several potential roles in atmospheric chemistry. They can form films on aqueous surfaces, which lowers the surface tension and possibly delays water evaporation and gaseous transportation across the aqueous interface. They can also increase the solubility of organic compounds in the aqueous phase. Recently, the decrease of surface tension in cloud growing droplets has been suggested as relevant to increases in the number of droplets of smaller size, potentially enhancing cloud albedo. Natural surfactants in the lung aid gas transfer and influence the dissolution rate of aerosol particles, so surfactants in atmospheric aerosols, once inhaled, may interact with pulmonary surfactants. Ambient aerosols were collected from the edge of Norwich, a small city in a largely agricultural region of England, and analysed for surfactants. Methylene blue, a conventional dye for detecting anionic surfactants, has been used as a colorimetric agent. The concentration of surfactants expressed as methylene blue active substances (MBAS) is in the range of 6-170 pmol m(-3)(air). A negative correlation with chloride aerosol indicates that these surfactants are probably not the well-known surfactants derived from marine spray. A more positive correlation with aerosol nitrate and gaseous NOx supports an association with more polluted inland air masses. The surfactants found in aerosols seem to be relatively strong acids, compared with weaker acids such as the long-chain carboxylic acids previously proposed as atmospheric surfactants. Surfactants from the oxidation of organic materials (perhaps vegetation- or soil-derived) seem a likely source of these substances in the atmosphere.

  20. CANTHARELLUS CIBARIUS - CULINARY-MEDICINAL MUSHROOM CONTENT AND BIOLOGICAL ACTIVITY.

    PubMed

    Muszyńska, Bozena; Kała, Katarzyna; Firlej, Anna; Sułkowska-Ziaja, Katarzyna

    2016-01-01

    One of the most frequently harvested mushrooms in Polish forests is Yellow chanterelle (chanterelle) - Cantharellus cibarius Fr. from the Cantharellaceae family. Chanterelle is an ectomycorrhizal mushroom occurring in Poland. Chanterelle lives in symbiosis with pine, spruce, oak and hombeam. In cookery, chanterelle is appreciated because of the aroma, taste, firmness and crunchiness of its fruiting bodies. Wild edible mushrooms are widely consumed in Asia, Western Europe and Central America. Chanterelle contains a great number of carbohydrates and proteins and a low amount of fat. Actual review presents the main groups of physiologically active primary and secondary metabolites in the fruiting bodies of chanterelle such as indole and phenolic compounds, carbohydrates, fatty acids, proteins, free amino acids, sterols, carotenoids, enzymes, vitamins and elements with biological activity. The presence of these compounds and elements conditions the nutrient and therapeutic activity of chanterelle, e.g., immunomodulatory, anti-inflammatory, antioxidant, antiviral, antimicrobial and antigenotoxic properties.

  1. Biological activity of bleached kraft pulp mill effluents before and after activated sludge and ozone treatments.

    PubMed

    Lopes, Alessandra Cunha; Mounteer, Ann H; Stoppa, Teynha Valverde; Aquino, Davi Santiago

    2013-01-01

    Eucalyptus bleached kraft pulp production, an important sector of the Brazilian national economy, is responsible for generating large volume, high pollutant load effluents, containing a considerable fraction of recalcitrant organic matter. The objectives of this study were to quantify the biological activity of the effluent from a eucalyptus bleached kraft pulp mill, characterize the nature of compounds responsible for biological activity and assess the effect of ozone treatment on its removal. Primary and secondary effluents were collected bimonthly over the course of one year at a Brazilian bleached eucalypt kraft pulp mill and their pollutant loads (biochemical oxygen demand (BOD), chemical oxygen demand (COD), total organic carbon (TOC), adsorbable organic halogen (AOX), lignin, extractives) and biological activity (acute and chronic toxicity and estrogenic activity) quantified. The effluent studied did not present acute toxicity to Daphnia, but presented the chronic toxicity effects of algal growth inhibition and reduced survival and reproduction in Ceriodaphnia, as well as estrogenic activity. Chronic toxicity and estrogenic activity were reduced but not eliminated during activated sludge biological treatment. The toxicity identification evaluation revealed that lipophilic organic compounds (such as residual lignin, extractives and their byproducts) were responsible for the toxicity and estrogenic activity. Ozone treatment (50 mg/L O(3)) of the secondary effluent eliminated the chronic toxicity and significantly reduced estrogen activity.

  2. Biologically active steroidal glycosides from Tribulus terrestris.

    PubMed

    Bedir, E; Khan, I A; Walker, L A

    2002-07-01

    The steroidal saponin constituents obtained from Tribulus terrestris were tested for their antimicrobial and cytotoxic effects. The spirostanol-based steroidal saponins 1-3 exhibited remarkable activity against fungal organisms (Candida albicans and Cryptococcus neoformans) and cancer cell lines [human malignant melanoma (SK-MEL), human oral epidermoid carcinoma (KB), human breast ductal carcinoma (BT-549), and human ovary carcinoma (SK-OV-3)], while none of the compounds possessing the furostanol framework 4-7 showed activity. The most active spirostanol glycoside, compound 3 exhibited a broad range of anticancer activity against cell lines, SK-MEL, KB, BT-549 and SK-OV-3 at IC50s of 6.0, 7.0, 6.0 and 8.2 micrograms/ml, respectively, while compounds 1 and 2 showed selective cytotoxicity against SK-MEL at 6.7 and 9.1 micrograms/ml, respectively. The minimum inhibitory concentrations (MIC) in antifungal bioassay for compounds 1-3 varied from 1.5 to 6.2 micrograms/ml, which prompted to conclude certain structural features are required for these bioactivities.

  3. Building biologically active nucleic acid nanocomplexes.

    PubMed

    Smith, C I Edvard; Lundin, Karin E; Simonson, Oscar E; Moreno, Pedro M D; Svahn, Mathias G; Wenska, Malgorzata; Strömberg, Roger

    2008-01-01

    The Bioplex technology allows the hybridization of functional entities to various forms of nucleic acids by the use of synthetic nucleic acid analogs. Such supramolecular assemblies can be made in a predetermined fashion and can confer new properties. The Zorro technology is based on a novel construct generated to simultaneously bind to both DNA strands. Such compounds may have gene silencing activity.

  4. Purification and characterization of biologically active peptides from spider venoms.

    PubMed

    Vassilevski, Alexander A; Kozlov, Sergey A; Egorov, Tsezi A; Grishin, Eugene V

    2010-01-01

    Spider venoms represent invaluable sources of biologically active compounds suitable for use in life science research and also having a significant potential for biotechnology and therapeutic applications. The methods reported herewith are based on our long experience of spider venom fractionation and peptides purification. We routinely screen new peptides for antimicrobial and insecticidal activities and our detailed protocols are also reported here. So far these have been tested on species of Central Asian and European spiders from the families Agelenidae, Eresidae, Gnaphosidae, Lycosidae, Miturgidae, Oxyopidae, Philodromidae, Pisauridae, Segestriidae, Theridiidae, Thomisidae, and Zodariidae. The reported protocols should be easily adaptable for use with other arthropod species.

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

    PubMed Central

    Hébert, Martin J. G.; Flewelling, Andrew J.; Clark, Trevor N.; Jean-François, Jacques; Surette, Marc E.; Gray, Christopher A.; Vogels, Christopher M.; Touaibia, Mohamed; Westcott, Stephen A.

    2015-01-01

    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. PMID:25834744

  6. Synthesis and biological activity of arylspiroborate salts derived from caffeic Acid phenethyl ester.

    PubMed

    Hébert, Martin J G; Flewelling, Andrew J; Clark, Trevor N; Levesque, Natalie A; Jean-François, Jacques; Surette, Marc E; Gray, Christopher A; Vogels, Christopher M; Touaibia, Mohamed; Westcott, Stephen A

    2015-01-01

    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.

  7. The plasminogen activator system: biology and regulation.

    PubMed

    Irigoyen, J P; Muñoz-Cánoves, P; Montero, L; Koziczak, M; Nagamine, Y

    1999-10-01

    The regulation of plasminogen activation involves genes for two plasminogen activators (tissue type and urokinase type), two specific inhibitors (type 1 and type 2), and a membrane-anchored urokinase-type plasminogen-activator-specific receptor. This system plays an important role in various biological processes involving extracellular proteolysis. Recent studies have revealed that the system, through interplay with integrins and the extracellular matrix protein vitronectin, is also involved in the regulation of cell migration and proliferation in a manner independent of proteolytic activity. The genes are expressed in many different cell types and their expression is under the control of diverse extracellular signals. Gene expression reflects the levels of the corresponding mRNA, which should be the net result of synthesis and degradation. Thus, modulation of mRNA stability is an important factor in overall regulation. This review summarizes current understanding of the biology and regulation of genes involved in plasminogen activation at different levels.

  8. Glucosidase inhibitory activity and antioxidant activity of flavonoid compound and triterpenoid compound from Agrimonia Pilosa Ledeb

    PubMed Central

    2014-01-01

    Background In Chinese traditional medicine, Agrimonia pilosa Ledeb (APL) exhibits great effect on treatment of type 2 diabetes mellitus (T2DM), however its mechanism is still unknown. Considering that T2DM are correlated with postprandial hyperglycemia and oxidative stress, we investigated the α-glucosidase inhibitory activity and the antioxidant activity of flavonoid compound (FC) and triterpenoid compound (TC) from APL. Methods Entire plants of APL were extracted using 95% ethanol and 50% ethanol successively. The resulting extracts were partitioned and isolated by applying liquid chromatography using silica gel column and Sephadex LH 20 column to give FC and TC. The content of total flavonoids in FC and the content of total triterpenoids in TC were determined by using UV spectrophotometry. HPLC analysis was used to identify and quantify the monomeric compound in FC and TC. The α-glucosidase inhibitory activities were determined using the chromogenic method with p-nitrophenyl-α-D-glucopyranoside as substrate. Antioxidant activities were assessed through three kinds of radical scavenging assays (DPPH radical, ABTS radical and hydroxyl radical) & β-carotene-linoleic acid assay. Results The results indicate FC is abundant of quercitrin, and hyperoside, and TC is abundant of 1β, 2β, 3β, 19α-tetrahydroxy-12-en-28-oic acid (265.2 mg/g) and corosolic acid (100.9 mg/g). The FC & the TC have strong α-glucosidase inhibitory activities with IC50 of 8.72 μg/mL and 3.67 μg/mL, respectively. We find that FC show competitive inhibition against α-glucosidase, while the TC exhibits noncompetitive inhibition. Furthermore, The FC exhibits significant radical scavenging activity with the EC50 values of 7.73 μg/mL, 3.64 μg/mL and 5.90 μg/mL on DPPH radical, hydroxyl radical and ABTS radical, respectively. The FC also shows moderate anti-lipid peroxidation activity with the IC50 values of 41.77 μg/mL on inhibiting β-carotene bleaching. Conclusion These results

  9. Parsley: a review of ethnopharmacology, phytochemistry and biological activities.

    PubMed

    Farzaei, Mohammad Hosein; Abbasabadi, Zahra; Ardekani, Mohammad Reza Shams; Rahimi, Roja; Farzaei, Fatemeh

    2013-12-01

    To summarize comprehensive information concerning ethnomedicinal uses, phytochemistry, and pharmacological activities of parsley. Databases including PubMed, Scopus, Google Scholar, and Web of Science were searched for studies focusing on the ethnomedicinal use, phytochemical compounds and biological and pharmacological activities of parsley. Data were collected from 1966 to 2013. The search terms were: "Parsley" or "Petroselinum crispum" or "Petroselinum hortence". Parsley has been used as carminative, gastro tonic, diuretic, antiseptic of urinary tract, anti-urolithiasis, anti-dote and anti-inflammatory and for the treatment of amenorrhea, dysmenorrhea, gastrointestinal disorder, hypertension, cardiac disease, urinary disease, otitis, sniffle, diabetes and also various dermal disease in traditional and folklore medicines. Phenolic compounds and flavonoids particularly apigenin, apiin and 6"-Acetylapiin; essential oil mainly myristicin and apiol; and also coumarins are the active compounds identified in Petroselinum crispum. Wide range of pharmacological activity including antioxidant, hepatoprotective, brain protective, anti-diabetic, analgesic, spasmolytic, immunosuppressant, anti-platelet, gastroprotective, cytoprotective, laxative, estrogenic, diuretic, hypotensive, antibacterial and antifungal activities have been exhibited for this plant in modern medicine. It is expectant that this study resulted in improvement the tendencies toward Petroselinum crispum as a useful and important medicinal plant with wide range of proven medicinal activity.

  10. Chemical biology of histone acetyltransferase natural compounds modulators.

    PubMed

    Piaz, Fabrizio Dal; Vassallo, Antonio; Rubio, Osmany Cuesta; Castellano, Sabrina; Sbardella, Gianluca; De Tommasi, Nunziatina

    2011-05-01

    Histone acetyltransferases (HATs) are a class of epigenetic enzymes crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells, thus being a promising target for therapeutic development. Nonetheless, differently from histone deacetylases (HDACs) inhibitors, there is still paucity of small-molecule modulators of HAT activity. After a decline during past decade, natural products and their derivatives could be once again a valuable tool in the lead discovery process and meet such need of Novel Chemical Entities (NCEs). In this review, we will provide a comprehensive summary on the discovery of small-molecule HAT modulators from naturally occurring molecular scaffolds.

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

    PubMed

    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.

  12. The biological activity of silicon carbide whiskers

    SciTech Connect

    Johnson, N.F.

    1989-01-01

    Size characteristics of SiC whiskers are similar to asbestos and contain potentially carcinogenic long thin fibers. Size distribution suggests that it is highly respirable, with majority of particles having diameters <3.0 [mu]m. Cytotoxic activity of SiC whiskers in cultured cells is [ge] than that of crocidolite asbestos. Inhalation exposures are needed to further delineate the biological activity; while SiC whiskers were as or more cytotoxic than crocidolite, JM Code 100 also displays such activity but results in no increased risk of lung cancer, pulmonary fibrosis or mesothelioma. PRD-166, a coarse continuous glass filament, displays little in vitro biological activity. It is recommended that SiC whiskers be treated as asbestos, and to continue investigating the potential health effects of SiC whiskers, in particular conducting animal experiments with acute and chronic inhalation exposures. 17 refs., 11 tabs., 18 figs.

  13. [Biologically Active Peptides of King Crab Hepatopancreas].

    PubMed

    Bogdanov, V V; Berezin, B B; Il'ina, A P; Yamskova, V P; Yamskov, I A

    2015-01-01

    Substances of a peptide nature isolated from the hepatopancreas of the king crab Paralithodes camtschaticus exhibited physicochemical properties and membranotropic and specific activities similar to those of membranotropic homeostatic tissue-specific bioregulators previously found in different mammalian and plant tissues. Their biological effect on vertebrate tissues was demonstrated on a model of roller organotypic cultivation of Pleurodeles waltl newt liver tissue.

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

    PubMed

    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

  15. [Coordination compounds of Pd(II) with potential antitumor activity].

    PubMed

    González Vílchez, F; García Basallote, M; Benítez Ordóñez, J; Vilaplana Serrano, R

    1982-01-01

    The first results about the anti-neoplastic activity of Pd(II) ion coordinative compounds with complexones of the ethylenediamine-tetraacetic acid type are described. The assays employing Ehrlich ascites cancer of the mouse show that the presence of substitutes in the ethylenediamine skeleton originates important changes of the activity of such compounds.

  16. Stereochemical Assignment of Strigolactone Analogues Confirms Their Selective Biological Activity.

    PubMed

    Artuso, Emma; Ghibaudi, Elena; Lace, Beatrice; Marabello, Domenica; Vinciguerra, Daniele; Lombardi, Chiara; Koltai, Hinanit; Kapulnik, Yoram; Novero, Mara; Occhiato, Ernesto G; Scarpi, Dina; Parisotto, Stefano; Deagostino, Annamaria; Venturello, Paolo; Mayzlish-Gati, Einav; Bier, Ariel; Prandi, Cristina

    2015-11-25

    Strigolactones (SLs) are new plant hormones with various developmental functions. They are also soil signaling chemicals that are required for establishing beneficial mycorrhizal plant/fungus symbiosis. In addition, SLs play an essential role in inducing seed germination in root-parasitic weeds, which are one of the seven most serious biological threats to food security. There are around 20 natural SLs that are produced by plants in very low quantities. Therefore, most of the knowledge on SL signal transduction and associated molecular events is based on the application of synthetic analogues. Stereochemistry plays a crucial role in the structure-activity relationship of SLs, as compounds with an unnatural D-ring configuration may induce biological effects that are unrelated to SLs. We have synthesized a series of strigolactone analogues, whose absolute configuration has been elucidated and related with their biological activity, thus confirming the high specificity of the response. Analogues bearing the R-configured butenolide moiety showed enhanced biological activity, which highlights the importance of this stereochemical motif.

  17. Amaryllidaceae alkaloids: Absolute configuration and biological activity.

    PubMed

    Cimmino, Alessio; Masi, Marco; Evidente, Marco; Superchi, Stefano; Evidente, Antonio

    2017-09-01

    Plants belonging to the Amaryllidaceae family are well known for their ornamental and medicinal use. Plant members of this group are distributed through both tropical and subtropical regions of the world and are dominant in Andean South America, the Mediterranean basin, and southern Africa. Amaryllidaceae plants have been demonstrated to be a good source of alkaloids with a large spectrum of biological activities, the latter being strictly related to the absolute stereochemistry of the alkaloid scaffold. Among them, great importance for practical applications in medicine has galanthamine, which has already spawned an Alzheimer's prescription drug as a potent and selective inhibitor of the enzyme acetylcholinesterase. Furthermore, lycorine as well as its related isocarbostyryl analogs narciclasine and pancratistatine have shown a strong anticancer activity in vitro against different solid tumors with malignant prognosis. This review addresses the assignment of the absolute configuration of several Amaryllidaceae alkaloids and its relationship with their biological activities. © 2017 Wiley Periodicals, Inc.

  18. Loranthus micranthus Linn.: Biological Activities and Phytochemistry

    PubMed Central

    Zorofchian Moghadamtousi, Soheil; Hajrezaei, Maryam; Abdul Kadir, Habsah

    2013-01-01

    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. PMID:24109490

  19. Separations of compounds of biological and environmental interest by micellar electrokinetic capillary chromatography

    SciTech Connect

    Balchunas, A.T.; Swaile, D.F.; Powell, A.C.; Sepaniak, M.J.

    1988-10-01

    Important criteria for the effective separation of compounds of biological or environmental interest by micellar electrokinetic capillary chromatography are discussed. Efficiencies of approximately 100,000 plates/meter are achieved in the separations of samples of derivatized amines, aflatoxins, and hydroxy aromatic compounds. Laser fluorometric detection is shown to be capable of detecting subpicogram injected quantities. Organic solvents such as 2-propanol and acetonitrile are added to the aqueous mobile phases normally used to improve the separation of hydrophobic compounds, impart different selectivities, and provide a means for gradient programming. Column diameter is found to influence efficiency, analysis time, and detection.

  20. 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.

    PubMed

    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 < ca. 300), low aromatic ring count (number = 1) and reduced lipophilicity (ClogP < 3.5) were hypothesized to be key factors to avoid the CAD associated 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.

  1. Isoxanthohumol--Biologically active hop flavonoid.

    PubMed

    Żołnierczyk, Anna Katarzyna; Mączka, Wanda Krystyna; Grabarczyk, Małgorzata; Wińska, Katarzyna; Woźniak, Edyta; Anioł, Mirosław

    2015-06-01

    Isoxanthohumol (IXN), apart from xanthohumol (XN) and 8-prenylnaringenin (8PN), is one of the most important prenylflavonoids found in hops. Another natural source of this compound is a shrub Sophora flavescens, used in traditional Chinese medicine. Main dietary source of IXN is beer, and the compound is produced from XN during wort boiling. In the human body, the compound is O-demethylated to 8PN, the strongest known phytoestrogen. This process takes place in the liver and in the intestine, where it is mediated by local microflora. It has been reported in some studies that even though beer contains small amounts of hops and its preparations, these compounds may affect the functioning of the human body. IXN exhibits an antiproliferative activity against human cell lines typical for breast cancer (MCF-7), ovarian cancer (A-2780), prostate cancer (DU145 and PC-3), and colon cancer (HT-29 and SW620) cells. It strongly inhibits the activation of the following carcinogens: 2-amino-3-methylimidazol-[4,5-f]quinoline and aflatoxin B1 (AFB1) via human cytochrome P450 (CYP1A2). It also inhibits the production of prostate specific antigen (PSA). IXN significantly reduces the expression of transforming growth factor-β (TGF-β) in the case of invasive breast cancer MDA-MB-231. It interferes with JAK/STAT signaling pathway and inhibits the expression of pro1inflammatory genes in the monoblastic leukemia cell line (MonoMac6). It activates apoptosis in human umbilical vein endothelial cells (HUVEC) and human aortic smooth muscle cells (HASMCs). In addition, IXN shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV).

  2. The ice nucleation activity of biological aerosols

    NASA Astrophysics Data System (ADS)

    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

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

    PubMed Central

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

    2012-01-01

    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. PMID:23015769

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

    PubMed

    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.

  5. Bioassay Directed Isolation and Biological Evaluation of Compounds Isolated from Rubus fairholmianus Gard.

    PubMed Central

    Plackal George, Blassan; Thangaraj, Parimelazhagan; Sulaiman, Cheruthazhakkatt; Piramanayagam, Shanmughavel; Ramaswamy, Sathish Kumar

    2014-01-01

    The in vitro and in silico analysis of Rubus fairholmianus acetone extract for antioxidant, antiproliferative, and anti-inflammatory activity led to the isolation of six compounds. Amongst all the six isolated compounds tested, 1-(2-hydroxyphenyl)-4-methylpentan-1-one (compound 1) and 2-[(3-methylbutoxy) carbonyl] benzoic acid (compound 2) were found to be more active in inhibiting BRCA and COX target proteins, which also showed the better results for DPPH and ABTS radical scavenging assays. The promising results of this investigation emphasize the importance of using R. fairholmianus in the treatment of radical generated disorders mainly cancer and other inflammatory diseases. PMID:25254204

  6. Synthesis and biological activity of novel deoxycholic acid derivatives.

    PubMed

    Popadyuk, Irina I; Markov, Andrey V; Salomatina, Oksana V; Logashenko, Evgeniya B; Shernyukov, Andrey V; Zenkova, Marina A; Salakhutdinov, Nariman F

    2015-08-01

    We report the synthesis and biological activity of new semi-synthetic derivatives of naturally occurring deoxycholic acid (DCA) bearing 2-cyano-3-oxo-1-ene, 3-oxo-1(2)-ene or 3-oxo-4(5)-ene moieties in ring A and 12-oxo or 12-oxo-9(11)-ene moieties in ring C. Bioassays using murine macrophage-like cells and tumour cells show that the presence of the 9(11)-double bond associated with the increased polarity of ring A or with isoxazole ring joined to ring A, improves the ability of the compounds to inhibit cancer cell growth. Copyright © 2015 Elsevier Ltd. All rights reserved.

  7. Biological activities of selected basidiomycetes from Yemen.

    PubMed

    Al-Fatimi, M; Schröder, G; Kreisel, H; Lindequist, U

    2013-03-01

    In a previous paper we demonstrated the results of biological screening of Yemeni basidiomycetes. The present study was aimed to investigate the antimicrobial and the antioxidant activity of further basidiomycetes collected in Yemen. Dichloromethane, methanol and aqueous extracts of the fruiting bodies of 25 species were screened in vitro for their antibacterial activities against three Gram-positive bacteria (Staphyloccocus aureus, Bacillus subtilis, Micrococcus flavus) and two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), against six human fungal pathogens (Candida albicans, Candida krusei, Aspergillus fumigatus, Mucor sp., Microsporum gypseum, Trichophyton mentagrophytes) and against one non human pathogenic fungus (Candida maltosa). The results indicated that 75 extracts exhibited activity against one or more of the bacteria. The methanol extracts of Agaricus cf. bernardii, Agrocybe pediades, Chlorophyllum molybdites, Coriolopsis polyzona, Ganoderma xylonoides, Pycnoporus sanguineus, Trametes lactinea and Trametes cingulata showed activity against all tested bacteria. The highest antibacterial activity was exhibited by methanol extracts from Chlorophyllum molybdites, Ganoderma xylonoides and Trametes cingulata and Agaricus cf. bernardii, Agrocybe pediades, Coriolopsis polyzona, Pycnoporus sanguineus and Trametes lactinea. The methanol extracts of Chlorophyllum molybdites, Ganoderma xylonoides and Pycnoporus sanguineus showed considerable antifungal activities against the tested fungal strains. Strong antioxidative effects employing the DPPH assay were exhibited by methanol extracts from Chlorophyllum molybdites, Ganoderma xylonoides, Hexagonia velutina, Pycnoporus sanguineus, Trametes lactinea and Trametes cingulata. Our previous and presented studies about 48 basidiomycetes collected in Yemen provide evidence that basidiomycetes from the Arabic region so far should attract more attention as potential source for new biologically active

  8. Platinum (II) Compounds With Antitumor Activity Studied by Molecular Mechanics

    PubMed Central

    Georgieva, Ivelina; Nikolov, George St.

    1998-01-01

    A series of Pt(ll) complexes with antitumor properties: [1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]PtL2 (meso-1-PtL2) and [erythro-1-(2,6-dichloro-4-hydroxyphenyl)-2-(2-halo-4-hydroxyphenyl)ethylenediamine]PtL2, [2L=2Cl−,2I−,SO42−; halo = F (erythro-8-PtL2),halo = Cl (erythro-9-PtL2)] has been modelled by molecular mechanics (MM). The MM calculations were carried out for different isomers and ligand conformations meso-δ, meso-λ, d,l-δ, d,I-λ. The compounds with the lowest MM energies have the same geometries as those obtained by X-ray analysis. The calculated MMX energy orders: meso-1-PtL2 < erythro-9-PtL2 < erythro-8-PtL2 for L=I−, Cl− and SO42− are reverse to the known antitumor activity order - the lowest energy complex (the most stable one)is the one with the highest estrogen activity (meso-1-PtL2). The type of the leaving group (L) does not alter the energy order, which is in agreement with the biological experiments that show a slight dependence of the estrogen properties on the leaving group type. PMID:18475828

  9. Platinum (II) Compounds With Antitumor Activity Studied by Molecular Mechanics.

    PubMed

    Trendafilova, N; Georgieva, I; Nikolov, G S

    1998-01-01

    A SERIES OF PT(LL) COMPLEXES WITH ANTITUMOR PROPERTIES: [1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]PtL(2) (meso-1-PtL(2)) and [erythro-1-(2,6-dichloro-4-hydroxyphenyl)-2-(2-halo-4-hydroxyphenyl)ethylenediamine]PtL(2), [2L=2Cl-,2I-,SO(4) (2)-; halo = F (erythro-8-PtL(2)),halo = Cl (erythro-9-PtL(2))] has been modelled by molecular mechanics (MM). The MM calculations were carried out for different isomers and ligand conformations meso-delta, meso-lambda, d,l-delta, d,I-lambda. The compounds with the lowest MM energies have the same geometries as those obtained by X-ray analysis. The calculated MMX energy orders: meso-1-PtL(2) < erythro-9-PtL(2) < erythro-8-PtL(2) for L=I-, Cl- and SO(4) (2-) are reverse to the known antitumor activity order - the lowest energy complex (the most stable one)is the one with the highest estrogen activity (meso-1-PtL(2)). The type of the leaving group (L) does not alter the energy order, which is in agreement with the biological experiments that show a slight dependence of the estrogen properties on the leaving group type.

  10. Biological activities of water-soluble fullerene derivatives

    NASA Astrophysics Data System (ADS)

    Nakamura, S.; Mashino, T.

    2009-04-01

    Three types of water-soluble fullerene derivatives were synthesized and their biological activities were investigated. C60-dimalonic acid, an anionic fullerene derivative, showed antioxidant activity such as quenching of superoxide and relief from growth inhibition of E. coli by paraquat. C60-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 IC50 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.

  11. Headspace analysis of polar organic compounds in biological matrixes using solid phase microextraction (SPME)

    USDA-ARS?s Scientific Manuscript database

    Analysis of biological fluids and waste material is difficult and tedious given the sample matrix. A rapid automated method for the determination of volatile fatty acids and phenolic and indole compounds was developed using a multipurpose sampler (MPS) with solid phase microextraction (SPME) and GC-...

  12. The relative toxicity of compounds used as preservatives in vaccines and biologics.

    PubMed

    Geier, David A; Jordan, Sarah K; Geier, Mark R

    2010-05-01

    In vaccines/biologics, preservatives are used to prevent microbial growth. The present study examined: (1) the comparative toxicities of commonly used preservatives in US licensed vaccines to human neurons; and (2) the relative toxicity index of these compounds to human neurons in comparison to bacterial cells. Using human neuroblastoma cells, the relative cytotoxicity of the levels of the compounds commonly used as preservative in US licensed vaccines was found to be phenol <2-phenoxyethanol < benzethonium chloride < Thimerosal. The observed relative toxicity indices (human neuroblastoma cells/bacterial cells) were 2-phenoxyethanol (4.6-fold) < phenol (12.2-fold) < Thimerosal (>330-fold). In addition, for the compounds tested, except for 2-phenoxyethanol, the concentrations necessary to induce significant killing of bacterial cells were significantly higher than those routinely present in US licensed vaccine/biological preparations. None of the compounds commonly used as preservatives in US licensed vaccine/biological preparations can be considered an ideal preservative, and their ability to fully comply with the requirements of the US Code of Federal Regulations (CFR) for preservatives is in doubt. Future formulations of US licensed vaccines/biologics should be produced in aseptic manufacturing plants as single dose preparations, eliminating the need for preservatives and an unnecessary risk to patients.

  13. Monitoring Biological Activity at Geothermal Power Plants

    SciTech Connect

    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.

  14. Biological activity and photostability of biflorin micellar nanostructures.

    PubMed

    Santana, Edson R B; Ferreira-Neto, João P; Yara, Ricardo; Sena, Kêsia X F R; Fontes, Adriana; Lima, Cláudia S A

    2015-05-13

    Capraria biflora L. is a shrub from the Scrophulariaceae family which produces in its roots a compound named biflorin, an o-naphthoquinone that shows activity against Gram-positive bacteria and fungi and also presents antitumor and antimetastatic activities. However, biflorin is hydrophobic and photosensitive. These properties make its application difficult. In this work we prepared biflorin micellar nanostructures looking for a more effective vehiculation and better preservation of the biological activity. Biflorin was obtained, purified and characterized by UV-Vis, infrared (IR) and 1H- and 13C-NMR. Micellar nanostructures of biflorin were then assembled with Tween 80®, Tween 20® and saline (0.9%) and characterized by UV-Vis spectroscopy and dynamic light scattering (DLS). The results showed that the micellar nanostructures were stable and presented an average size of 8.3 nm. Biflorin micellar nanostructures' photodegradation was evaluated in comparison with biflorin in ethanol. Results showed that the biflorin in micellar nanostructures was better protected from light than biflorin dissolved in ethanol, and also indicated that biflorin in micelles were efficient against Gram-positive bacteria and yeast species. In conclusion, the results showed that the micellar nanostructures could ensure the maintenance of the biological activity of biflorin, conferring photoprotection. Moreover, biflorin vehiculation in aqueous media was improved, favoring its applicability in biological systems.

  15. Phenolic compounds with IL-6 inhibitory activity from Aster yomena.

    PubMed

    Kim, A Ryun; Jin, Qinglong; Jin, Hong-Guang; Ko, Hae Ju; Woo, Eun-Rhan

    2014-07-01

    A new biflavonoid, named asteryomenin (1), as well as six known phenolic compounds, esculetin (2), 4-O-β-D-glucopyranoside-3-hydroxy methyl benzoate (3), caffeic acid (4), isoquercitrin (5), isorhamnetin-3-O-glucoside (6), and apigenin (7) were isolated from the aerial parts of Aster yomena. The structures of compounds (1-7) were identified based on 1D and 2D NMR, including (1)H-(1)H COSY, HSQC, HMBC and NOESY spectroscopic analyses. Compounds 2-7 were isolated from this plant for the first time. For these isolates, the inhibitory activity of IL-6 production in the TNF-α stimulated MG-63 cell was examined. Among these isolates, compounds 4 and 7 appeared to have potent inhibitory activity of IL-6 production in the TNF-α stimulated MG-63 cell, while compounds 1-3 and 5-6 showed moderate activity.

  16. Application of thermal desorption to the biological monitoring of organic compounds in exhaled breath.

    PubMed

    Periago, J F; Prado, C; Ibarra, I; Tortosa, J

    1993-12-24

    We have developed a thermal desorption-gas chromatographic method for the analysis of organic compounds in exhaled breath air, to be used in the biological monitoring of environmental exposure. The exhaled breath sampler is based on the concentration of compounds present in alveolar air in a solid sorbent material. Isoflurane (1-chloro-2,2,2-trifluoroethyl-difluoromethyl-ether), an inhaled anaesthetic used widely in surgery, and styrene, used in boat construction and the manufacture of fibreglass-reinforced plastics, are partially eliminated from the body in exhaled breath, samples of which can therefore be used to monitor biological exposure to these two organic compounds. Recoveries were tested in controlled atmospheres of isoflurane or styrene, with Chromosorb 106 or Tenax, respectively, as the adsorbent. We also investigated the influence of relative humidity, an important factor in breath sampling, on adsorption.

  17. Nanoparticles made of π-conjugated compounds targeted for chemical and biological applications.

    PubMed

    Xu, Xinjun; Liu, Ronghua; Li, Lidong

    2015-12-07

    Semiconducting organic nanoparticles have recently attracted increasing attention in the chemical and biomedical fields. Such nanoparticles are mainly composed of π-conjugated compounds. They possess the properties of easy synthesis, facile tuning, less toxicity and more biocompatibility relative to the existing inorganic nanoparticles. In addition, they show advantages such as brighter fluorescence, higher photostability and higher biocompatibility, compared with classical fluorescent organic dyes. In this review, we summarize the latest advances in the development of organic nanoparticles made of π-conjugated compounds, including preparation methods, material design, nanoparticle fabrication and surface functionalization for chemical and biological applications. Especially, we focus on the applications of semiconducting organic nanoparticles in chemical and biological sensing by monitoring the fluorescence signal, as nanocarriers for drug/gene delivery, in photothermal and photodynamic therapy, and in photoacoustic imaging. Finally, the challenges and perspectives for the future development of organic nanoparticles based on π-conjugated compounds are also discussed.

  18. Generation and Biological Activities of Oxidized Phospholipids

    PubMed Central

    Oskolkova, Olga V.; Birukov, Konstantin G.; Levonen, Anna-Liisa; Binder, Christoph J.; Stöckl, Johannes

    2010-01-01

    Abstract Glycerophospholipids represent a common class of lipids critically important for integrity of cellular membranes. Oxidation of esterified unsaturated fatty acids dramatically changes biological activities of phospholipids. Apart from impairment of their structural function, oxidation makes oxidized phospholipids (OxPLs) markers of “modified-self” type that are recognized by soluble and cell-associated receptors of innate immunity, including scavenger receptors, natural (germ line-encoded) antibodies, and C-reactive protein, thus directing removal of senescent and apoptotic cells or oxidized lipoproteins. In addition, OxPLs acquire novel biological activities not characteristic of their unoxidized precursors, including the ability to regulate innate and adaptive immune responses. Effects of OxPLs described in vitro and in vivo suggest their potential relevance in different pathologies, including atherosclerosis, acute inflammation, lung injury, and many other conditions. This review summarizes current knowledge on the mechanisms of formation, structures, and biological activities of OxPLs. Furthermore, potential applications of OxPLs as disease biomarkers, as well as experimental therapies targeting OxPLs, are described, providing a broad overview of an emerging class of lipid mediators. Antioxid. Redox Signal. 12, 1009–1059. PMID:19686040

  19. Anti-tumoral activity of native compound morelloflavone in glioma

    PubMed Central

    Li, Xianfeng; Ai, Hongyan; Sun, Deke; Wu, Tao; He, Jian; Xu, Zhai; Ding, Li; Wang, Ling

    2016-01-01

    The aim of the study was to investigate the anti-tumoral activity of morelloflavone substances with different structures. We also studied the possible link between morelloflavone structure and its function. Various types of chromatographic techniques were used to isolate and screen morelloflavone substances from the extracts of gambogic tree trunk and the morelloflavone structures were identified by analytical techniques such as high resolution mass spectrometry and nuclear magnetism. Anti-tumoral activities of different compounds were investigated and the link between the antitumor activity and the structure of compound was exaimed. Our results showed that the isolated morelloflavone substances demonstrated a certain level of antitumor activity. The compound no. 1 had the strongest effect to inhibit glioma U87 and C6 cells followed by compound no. 2 while compound no. 5 was the weakest among them. We conducted a preliminary analysis on the structure-function relationship through the structure comparison and we concluded that the antitumor effects of morelloflavone substances with different structures were significantly different from each other. Thus, the glucose chain in C4 position of biflavone structure can enhance the antitumor activity of the compound in glioma cells. Additionally, the formation of intramolecular hydrogen bonds in biflavone compounds may also play a role in enhancing the antitumor activity and inhibition rate. PMID:27900007

  20. Biologically active extracts with kidney affections applications

    NASA Astrophysics Data System (ADS)

    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.

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

    PubMed

    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.

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

    NASA Astrophysics Data System (ADS)

    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. Biologic Activity of Porphyromonas endodontalis complex lipids

    PubMed Central

    Mirucki, Christopher S.; Abedi, Mehran; Jiang, Jin; Zhu, Qiang; Wang, Yu-Hsiung; Safavi, Kamran E.; Clark, Robert B.; Nichols, Frank C.

    2014-01-01

    Introduction Periapical infections secondary to pulpal necrosis are associated with bacterial contamination of the pulp. Porphyromonas endodontalis, a Gram-negative organism, is considered to be a pulpal pathogen. P. gingivalis is phylogenetically related to P. endodontalis and synthesizes several classes of novel complex lipids that possess biological activity, including the capacity to promote osteoclastogenesis and osteoclast activation. The purpose of this study was to extract and characterize constituent lipids of P. endodontalis, and evaluate their capacity to promote pro-inflammatory secretory responses in the macrophage cell line, RAW 264.7, as well as their capacity to promote osteoclastogenesis and inhibit osteoblast activity. Methods Constituent lipids of both organisms were fractionated by HPLC and were structurally characterized using electrospray-mass spectrometry (ESI-MS) or ESI-MS/MS. The virulence potential of P. endodontalis lipids was then compared with known biologically active lipids isolated from P. gingivalis. Results P. endodontalis total lipids were shown to promote TNF-α secretion from RAW 264.7 cells and the serine lipid fraction appeared to account for the majority of this effect. P. endodontalis lipid preparations also increased osteoclast formation from RAW 264.7 cells but osteoblast differentiation in culture was inhibited and appeared to be dependent on TLR2 expression. Conclusions These effects underscore the importance of P. endodontalis lipids in promoting inflammatory and bone cell activation processes that could lead to periapical pathology. PMID:25146013

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

    PubMed

    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.

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

    PubMed

    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.

  6. Preparation and antibacterial activity of compound chitosan-compound Yizhihao-nanoparticles.

    PubMed

    Ou, Sheng; Zhang, Yang-de

    2008-05-01

    To prepare chitosan (CS)-compound Yizhihao-nanoparticles (NP) and to investigate its antibacterial activity. CS NPs were formed by the incorporation of CS and Na3 PO4. CS-compound Yizhihao NPs were prepared by ion-cross-linking. The particle sizes and surface charges of CS NPs were determined by Malvern Zetasizer 1000-HAS and atomic force microscope (AFM), respectively. The antibacterial activity of CS-compound Yizhihao-NPs was studied in vitro and compared with that of compound Yizhihao powder. Malvern Zetasizer 1000-HAS and AFM demonstrated that the diameter of CS-compound Yizhihao NPs was (137.00+/-14.28)nm and CS NPs had (16.90+/-1.32)mV positive surface charges. The minimal inhibitory concentrations (MIC) of CS-compound Yizhihao NPs on Staphylococcus aureus,Pneumococcus,beta-hemolytic streptococcus, and Escherichia coli were 1:32,1:32,1:16,and 1:2, respectively. The minimal bactericidal concentrations (MBC) of CS-compound Yizhihao-NPs on Staphylococcus aureus, Pneumococcus, beta-hemolytic streptococcus, and Escherichia coli were 1:16,1:16,1:8, and 1:2, respectively. The antibacterial efficacy of CS-compound Yizhihao-NPs to Staphylococcus aureus, Pneumococcus, and beta-hemolytic streptococcus had been improved significantly (P< 0.05). CS-compound Yizhihao-nanoparticles have obvious antibacterial activity to the Staphylococcus aureus,Pneumococcus,and beta-hemolytic streptococcus,which lays the experimental foundation for new preparation of traditional Chinese medicine in future research.

  7. A network-based multi-target computational estimation scheme for anticoagulant activities of compounds.

    PubMed

    Li, Qian; Li, Xudong; Li, Canghai; Chen, Lirong; Song, Jun; Tang, Yalin; Xu, Xiaojie

    2011-03-22

    Traditional virtual screening method pays more attention on predicted binding affinity between drug molecule and target related to a certain disease instead of phenotypic data of drug molecule against disease system, as is often less effective on discovery of the drug which is used to treat many types of complex diseases. Virtual screening against a complex disease by general network estimation has become feasible with the development of network biology and system biology. More effective methods of computational estimation for the whole efficacy of a compound in a complex disease system are needed, given the distinct weightiness of the different target in a biological process and the standpoint that partial inhibition of several targets can be more efficient than the complete inhibition of a single target. We developed a novel approach by integrating the affinity predictions from multi-target docking studies with biological network efficiency analysis to estimate the anticoagulant activities of compounds. From results of network efficiency calculation for human clotting cascade, factor Xa and thrombin were identified as the two most fragile enzymes, while the catalytic reaction mediated by complex IXa:VIIIa and the formation of the complex VIIIa:IXa were recognized as the two most fragile biological matter in the human clotting cascade system. Furthermore, the method which combined network efficiency with molecular docking scores was applied to estimate the anticoagulant activities of a serial of argatroban intermediates and eight natural products respectively. The better correlation (r = 0.671) between the experimental data and the decrease of the network deficiency suggests that the approach could be a promising computational systems biology tool to aid identification of anticoagulant activities of compounds in drug discovery. This article proposes a network-based multi-target computational estimation method for anticoagulant activities of compounds by

  8. Nonclassical biological activities of quinolone derivatives.

    PubMed

    Ahmed, Abeer; Daneshtalab, Mohsen

    2012-01-01

    Quinolones are considered as a big family of multi-faceted drugs; their chemical synthesis is flexible and can be easily adapted to prepare new congeners with rationally devised structures. This is shown by the description of many thousands of derivatives in the literature. Scientists could accurately describe their QSAR, which is essential for effective drug design. This also gave them the chance to discover new and unprecedented activities, which makes quinolones an endless source of hope and enables further development of new clinically useful drugs. Quinolones are among the most common frameworks present in the bioactive molecules that have dominated the market for more than four decades. Since 1962, 4(1H)-quinolone-3-carboxylic acid derivatives are widely used as antibacterial agents. Quinolones have a broad and potent spectrum of activity and are also used as second-line drugs to treat tuberculosis (TB). Recently, quinolones have been reported to display "nonclassical" biological activities, such as antitumor, anti-HIV-1 integrase, anti-HCV-NS3 helicase and -NS5B-polymerase activities. The present review focuses on the structural modifications responsible for the transformation of an antibacterial into an anticancer agent and/or an antiviral agent. Indeed, quinolones' antimicrobial action is distinguishable among antibacterial agents, because they target different type II topoisomerase enzymes. Many derivatives of this family show high activity against bacterial topoisomerases and eukaryotic topoisomerases, and are also toxic to cultured mammalian cells and in vivo tumor models. Moreover, quinolones have shown antiviral activity against HIV and HCV viruses. In this context the quinolones family of drugs seem to link three different biological activities (antibacterial, anticancer, and the antiviral profiles) and the review will also provide an insight into the different mechanisms responsible for these activities among different species.

  9. The biological and toxicological activity of gases and vapors.

    PubMed

    Abraham, Michael H; Sánchez-Moreno, Ricardo; Gil-Lostes, Javier; Acree, William E; Cometto-Muñiz, J Enrique; Cain, William S

    2010-03-01

    A large amount of data on the biological and toxicological activity of gases and vapors has been collected from the literature. Processes include sensory irritation thresholds, the Alarie mouse test, inhalation anesthesia, etc. It is shown that a single equation using only five descriptors (properties of the gases and vapors) plus a set of indicator variables for the given processes can correlate 643 biological and non-lethal toxicological activities of 'non-reactive' compounds with a standard deviation of 0.36 log unit. The equation is scaled to sensory irritation thresholds obtained by the procedure of Cometto-Muñiz, and Cain provides a general equation for the prediction of sensory irritation thresholds in man. It is suggested that differences in biological/toxicological activity arise primarily from transport from the gas phase to a receptor phase or area, except for odor detection thresholds where interaction with a receptor(s) is important. Copyright (c) 2009 Elsevier Ltd. All rights reserved.

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

    PubMed

    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.

  11. Quantum chemical and statistical study of megazol-derived compounds with trypanocidal activity

    NASA Astrophysics Data System (ADS)

    Rosselli, F. P.; Albuquerque, C. N.; da Silva, A. B. F.

    In this work we performed a structure-activity relationship (SAR) study with the aim to correlate molecular properties of the megazol compound and 10 of its analogs with the biological activity against Trypanosoma cruzi (trypanocidal or antichagasic activity) presented by these molecules. The biological activity indication was obtained from in vitro tests and the molecular properties (variables or descriptors) were obtained from the optimized chemical structures by using the PM3 semiempirical method. It was calculated ˜80 molecular properties selected among steric, constitutional, electronic, and lipophilicity properties. In order to reduce dimensionality and investigate which subset of variables (descriptors) would be more effective in classifying the compounds studied, according to their degree of trypanocidal activity, we employed statistical methodologies (pattern recognition and classification techniques) such as principal component analysis (PCA), hierarchical cluster analysis (HCA), K-nearest neighbor (KNN), and discriminant function analysis (DFA). These methods showed that the descriptors molecular mass (MM), energy of the second lowest unoccupied molecular orbital (LUMO+1), charge on the first nitrogen at substituent 2 (qN'), dihedral angles (D1 and D2), bond length between atom C4 and its substituent (L4), Moriguchi octanol-partition coefficient (MLogP), and length-to-breadth ratio (L/Bw) were the variables responsible for the separation between active and inactive compounds against T. cruzi. Afterwards, the PCA, KNN, and DFA models built in this work were used to perform trypanocidal activity predictions for eight new megazol analog compounds.

  12. Rhodiola plants: Chemistry and biological activity.

    PubMed

    Chiang, Hsiu-Mei; Chen, Hsin-Chun; Wu, Chin-Sheng; Wu, Po-Yuan; Wen, Kuo-Ching

    2015-09-01

    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. Copyright © 2015. Published by Elsevier B.V.

  13. Selenium compounds activate early barriers of tumorigenesis

    USDA-ARS?s Scientific Manuscript database

    Selenium chemoprevention by apoptosis has been well studied, but it is not clear whether selenium can activate early barriers of tumorigenesis, namely senescence and DNA damage response. To address this issue, we treated normal and cancerous cells with a gradient concentration of sodium selenite, me...

  14. Myricetin: A Dietary Molecule with Diverse Biological Activities

    PubMed Central

    Semwal, Deepak Kumar; Semwal, Ruchi Badoni; Combrinck, Sandra; Viljoen, Alvaro

    2016-01-01

    Myricetin is a common plant-derived flavonoid and is well recognised for its nutraceuticals value. It is one of the key ingredients of various foods and beverages. The compound exhibits a wide range of activities that include strong anti-oxidant, anticancer, antidiabetic and anti-inflammatory activities. It displays several activities that are related to the central nervous system and numerous studies have suggested that the compound may be beneficial to protect against diseases such as Parkinson’s and Alzheimer’s. The use of myricetin as a preserving agent to extend the shelf life of foods containing oils and fats is attributed to the compound’s ability to protect lipids against oxidation. A detailed search of existing literature revealed that there is currently no comprehensive review available on this important molecule. Hence, the present work includes the history, synthesis, pharmaceutical applications and toxicity studies of myricetin. This report also highlights structure-activity relationships and mechanisms of action for various biological activities. PMID:26891321

  15. Activation of shallow dopants in II-VI compounds

    SciTech Connect

    Walukiewicz, W.

    1995-08-01

    The amphoteric native defect model is applied to the understanding of the variations in the dopant activation efficiency in II-VI compounds. It is shown that the location of the common energy reference, the Fermi level stabilization energy, relative to the band edges can be used to determine the doping induced reduction of the formation energy and the enhancement of the concentration of compensating native defects. The model is applied to the most extensively studied compound semiconductors as well as to ternary and quaternary alloys. The effects of the compound ionicity on the dopant activation are briefly discussed.

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

    NASA Astrophysics Data System (ADS)

    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. The effect of bioactive compounds in tea on lipid metabolism and obesity through regulation of peroxisome proliferator-activated receptors.

    PubMed

    Lee, Sung-Joon; Jia, Yaoyao

    2015-02-01

    The hypolipidemic and antiobesogenic effects of tea intake have been associated with bioactive compounds that regulate peroxisome proliferator-activated receptors (PPARs). This review describes the recent research on two of these compounds, (-)-epigallocatechin gallate (EGCG) and linalool. Catechins (specifically EGCG) are key bioactive compounds found in tea, and a recent study has shown that linalool may also be an active tea compound. These compounds act on lipid metabolism by regulating PPAR subtypes. EGCG inhibits the key adipogenic transcription factor PPARγ while activating PPARα, whereas linalool is a PPARα agonist activating hepatic fatty acid uptake and subsequent oxidation to reduce plasma triglyceride levels. The collective activities of EGCG and linalool in tea may exert hypolipidemic and antiobesogenic effects by regulating PPARs. The research summarized in this review expands our understanding of the biological and physiological mechanisms of the bioactive compounds found in tea.

  18. Hemagglutinating activity in phytopathogenic bacteria surface compounds.

    PubMed

    Serra, M T; Castresana, M C; Tejerina, G

    1987-01-01

    Extracellular components of plant pathogenic bacteria were obtained from their culture medium as well as from the whole cells by using NaCl 1 M, pH 6.0; 20% sucrose dissolved in 0.03 M Tris buffer, pH 8.0; or 0.05 M Na2EDTA. All the extracts from Erwinia carotovora subsp. carotovora, Xanthomonas campestris pv. campestris, Pseudomonas syringae pv. phaseolicola, Xanthomonas campestris pv. phaseoli, Pseudomonas solanacearum, and Erwinia carotovora subsp. atroseptica, were assayed for hemagglutinating activity on sheep, rabbit and chicken red blood cells (RBCs). The only active extracts were those obtained by NaCl treatment. They agglutinated sheep and rabbit erythrocytes. Extracts from E. carotovora subsp. atroseptica gave rise to the high agglutination titer on rabbit RBCs. These extracts had the lowest polysaccharide/protein ratio. E. carotovora subsp. carotovora extracts showed only a low titer (18.5 units). The agglutinating activity present in NaCl extracts of the bacteria tested was inhibited by different carbohydrates to various extent. Extracts from E. carotovora subsp. atroseptica appeared to be the most sensitive ones while those of E. carotovora subsp. carotovora least sensitive to the presence of sugar. It is suggested that hemagglutinins observed in plant pathogenic bacteria and those in plant host are similar and that both may, in some way, be involved in the plant-parasite relationship.

  19. The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds

    PubMed Central

    Hasinoff, Brian B.; Liang, Hong; Wu, Xing; Guziec, Lynn J.; Guziec, Frank S.; Marshall, Kyle; Yalowich, Jack C.

    2008-01-01

    Anticancer drugs that bind to DNA and inhibit DNA-processing enzymes represent an important class of anticancer drugs. In order to find stronger DNA binding and more potent cytotoxic compounds, a series of ester-coupled bisanthrapyrazole derivatives of 7-chloro-2-[2-[(2-hydroxyethyl)methylamino]ethyl]anthra[1,9-cd]pyrazol-6(2H)-one (AP9) were designed and evaluated by molecular docking techniques. Because the anthrapyrazoles are unable to be reductively activated like doxorubicin and other anthracyclines, they should not be cardiotoxic like the anthracyclines. Based on the docking scores of a series of bisanthrapyrazoles with different numbers of methylene linkers (n) that were docked into an X-ray structure of double-stranded DNA, five bisanthrapyrazoles (n = 1 to 5) were selected for synthesis and physical and biological evaluation. The synthesized compounds were evaluated for DNA binding and bisintercalation by measuring the DNA melting temperature increase, for growth inhibitory effects on the human erythroleukemic K562 cell line, and for DNA topoisomerase IIα-mediated cleavage of DNA and inhibition of DNA topoisomerase IIα decatenation activities. The results suggest that the bisanthrapyrazoles with n = 2 to 5 formed bisintercalation complexes with DNA. In conclusion, a novel group of bisintercalating anthrapyrazole compounds have been designed, synthesized and biologically evaluated as possible anticancer agents. PMID:18258442

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

    PubMed

    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.

  1. Chemistry, biological activity, and uses of formamidine pesticides.

    PubMed Central

    Hollingworth, R M

    1976-01-01

    The formamidines, a relatively new group of acaricide-insecticides, are novel both in their range of biological activities and in their mode of action, which is presently unknown. This paper is a review of the historical development, properties, structures, uses, and chemistry of this group of pesticides, with particular emphasis on chlordimeform (Galecron or Fundal), N'-4-chloro-o-tolyl-N,N-dimethylformamidine, and amitraz, 1,3=di-(2,4-dimethylphenylimino)-2-methyl-2-azapropane. Their biological activity and uses are defined by their toxicity to spider mites, ticks, and certain insects, and they are particularly effective against juvenile and resistant forms of these organisms. A significant, but poorly understood feature of their field effectiveness is their breadth of toxic action which includes direct lethality, excitant-repellant behavioral effects, and chemosterilization. They are generally of low hazard for nontarget species with the significant exception of predaceous mites. Several aspects of the chemistry of these compounds are considered, including structure--activity relations, synthetic pathways, isomerism and configuration, and their chemical and environmental stability. A significant feature of the metabolism and toxicity of these agents is the possible activation of chlordimeform by N-demethylation in vivo. Strong evidence for this has been presented with the cattle tick, but recent results discussed here suggest that in other species, i.e., mice, German cockroaches or black cutworm eggs, N-demethylation is neither a strong activation nor a detoxication reaction. PMID:789070

  2. Biological activity, design, synthesis and structure activity relationship of some novel derivatives of curcumin containing sulfonamides.

    PubMed

    Lal, Jaggi; Gupta, Sushil K; Thavaselvam, D; Agarwal, Dau D

    2013-06-01

    Five series of curcumin derivatives with sulfonamides 3a-3e, 4a-4e, 5a-5e, 6a-6e and 7a-7e have been synthesized and evaluated for in vitro antibacterial activity against selected medically important gram-(+) and gram-(-) bacterial species viz. Staphylococcus aureus, Bacillus cereus, Salmonella typhi, Pseudomonas aeruginosa and Escherichia coli, and antifungal activity against few pathogenic fungal species viz. Aspergillus niger, Aspergillus flavus, Trichoderma viride and Curvularia lunata. The cytotoxicity has been determined by measuring IC50 values against human cell lines HeLa, Hep G-2, QG-56 and HCT-116. Among the compounds screened, 3a-3e showed the most potent biological activity against tested bacteria and fungi. Compounds 3a-3e displayed higher cytotoxicity than curcumin. The curcumin derivatives were also evaluated for in vivo anti-inflammatory activity. In contrast, the compounds 6a-6e and 7a-7e showed dramatically decrease in biological activity. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

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

    PubMed

    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.

  4. Identification of Volatile Organic Compounds (VOCs) From Photochemical Activity in Snow Samples

    NASA Astrophysics Data System (ADS)

    Kos, G.; Ariya, P. A.

    2004-05-01

    The occurrence of VOCs in snow has been observed and can be related to anthropogenic emissions and biological activity. Photochemistry and microorganisms play a major role in the transformation of compounds in different compartments of the global ecosystem. Studies so far focused on the determination of single analytes or a class of compounds - mainly of anthropogenic origin (e.g. halogenated aromatic hydrocarbons) - that were considered important with regard to health and environmental concerns. Broader studies that describe a range of different compounds with different functionalities are relatively rare, especially for those of biological origin. The presented study investigated the formation of VOCs in snow samples and their connection with microbiological activity. The main aim was to pre-concentrate, identify and quantify volatile organic compounds. Snow samples were collected in an urban environment (Montreal, Canada) with sterilized containers. Samples were transferred into a heated reaction flask, where the sample was melted. A two-trap system was employed for pre-concentration: The first trap was used for water removal. The second trap was used for the collection of expected analytes by removing volatiles from the circulating air. Circulation was maintained with a pump at atmospheric pressure. Adsorption to glass walls of the reaction flask was prevented with halocarbon wax coating. Different sterilization methods were employed to suppress microbiological activity in order to collect background data and identify compounds of biological origin. VOC concentration and compound identification was performed with gas chromatography and mass spectrometric detection (GC-MS) by taking a sample with a gas-tight syringe through a septum-port. The sample was directly injected into the GC system. Compounds were identified by their respective mass spectra and included aldehydes and alcohols.

  5. Biological activities of yarrow species (Achillea spp.).

    PubMed

    Nemeth, E; Bernath, J

    2008-01-01

    The genus Achillea consists of about 140 perennial herbs native to the Northern hemisphere. Traditional indications of their use include digestive problems, liver and gall-bladder conditions, menstrual irregularities, cramps, fever, wound healing. The Commission E approves its internal use for loss of appetite and dyspeptic ailments (gastric catarrh, spastic discomfort), externally it is used in form of sitz bath or as a compress against skin inflammation, slow healing wounds, bacterial or fungal infections. In the last decades, pharmacological studies became intensive, although human clinical investigations are still rare. Recent findings have confirmed several traditional uses. The largest number of data accumulated for antioxidant and anti-inflammatory effects. There are positive results on the analgesic, anti-ulcer, choleretic, hepatoprotective and wound healing activities. First results on other interesting therapeutical areas - antihypertensive, antidiabetic, antitumor, antispermatogenic activities -need confirmation. Yarrow can be used also as an insect repellent. Contact dermatitis as adverse effect may be connected to sesquiterpenes. The diversity and complexity of the effective compounds of yarrow species explains the broad spectrum of their activity. According to the literature the pharmacological effects are mainly due to the essential oil, proazulenes and other sesquiterpene lactones, dicaffeoylquinic acids and flavonoids. Synergistic actions of these and other compounds are also supposed. Achillea species have different chemical and therapeutical values. Despite of numerous data, correct evaluation of the results is difficult because of missing generally accepted taxonomical nomenclature. The used chemical-analytical methods and bio-assays are utmost diverse, making the comparison complicated. Further research on the activity is needed using exactly defined plant material, standardized methods and chemical analysis.

  6. Synthesis and Assay of SIRT1-Activating Compounds.

    PubMed

    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.

  7. Synthesis and Assay of SIRT1-Activating Compounds

    PubMed Central

    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. Over-expression 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. PMID:27423864

  8. Biological activity of bee propolis in health and disease.

    PubMed

    Khalil, Mahmoud Lotfy

    2006-01-01

    Propolis is a natural product derived from plant resins collected by honeybees. It is used by bees as glue, a general-purpose sealer, and as draught-extruder for beehives. Propolis has been used in folk medicine for centuries. It is known that propolis possesses anti-microbial, antioxidative, anti-ulcer and anti-tumor activities. Therefore, propolis has attracted much attention in recent years as a useful or potential substance used in medicine and cosmetics products. Furthermore, it is now extensively used in foods and beverages with the claim that it can maintain or improve human health. The chemical composition of propolis is quite complicated. More than 300 compounds such as polyphenols, phenolic aldehydes, sequiterpene quinines, coumarins, amino acids, steroids and inorganic compounds have been identified in propolis samples. The contents depend on the collecting location, time and plant source. Consequently, biological activities of propolis gathered from different phytogeographical areas and time periods vary greatly. In this review, the activity of bee propolis will be presented with special emphasis on the antitumor activity.

  9. Milk inhibits the biological activity of ricin.

    PubMed

    Rasooly, Reuven; He, Xiaohua; Friedman, Mendel

    2012-08-10

    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 a component of reconstituted powdered milk has a high binding affinity to ricin. We discovered that milk can competitively bind to and reduce the amount of toxin available to asialofetuin type II, which is used as a model to study the binding of ricin to galactose cell-surface receptors. Milk also removes ricin bound to the microtiter plate. In parallel experiments, we demonstrated by activity assay and by immuno-PCR that milk can bind competitively to 1 ng/ml ricin, reducing the amount of toxin uptake by the cells, and thus inhibit the biological activity of ricin. The inhibitory effect of milk on ricin activity in Vero cells was at the same level as by anti-ricin antibodies. We also found that (a) milk did not inhibit ricin at concentrations of 10 or 100 ng/ml; (b) autoclaving 10 and 100 ng/ml ricin in DMEM at 121 °C for 30 min completely abolished activity; and (c) milk did not affect the activity of another ribosome inactivating protein, Shiga toxin type 2 (Stx2), produced by pathogenic Escherichia coli O157:H7. Unlike ricin, which is internalized into the cells via a galactose-binding site, Stx2 is internalized through the cell surface receptor glycolipid globotriasylceramides Gb3 and Gb4. These observations suggest that ricin toxicity may possibly be reduced at room temperature by a widely consumed natural liquid food.

  10. Synthesis and biological evaluation of novel naphthalene compounds as potential antidepressant agents.

    PubMed

    Ang, Wei; Chen, Gong; Xiong, Li; Chang, Ying; Pi, Weiyi; Liu, Yuanyuan; Li, Chunlong; Zheng, Jiajia; Zhou, Liangxue; Yang, Bo; Deng, Yong; Yang, Shengyong; Luo, Youfu; Wei, Yuquan

    2014-07-23

    In this study, a series of novel naphthalene compounds were synthesized and screened for their antidepressant-like activities in vitro and in vivo. Their values for two descriptors (ClogP, tPSA) of the blood-brain barrier (BBB) were calculated for early assessment of the central nervous system (CNS) drug-likeness. Seven of them (6d, 6i, 6k, 6o, 6p, 6s and 6t) demonstrated potential protective effects on corticosterone-induced lesion of PC12 cells although they cannot repair the irreversible oxidant injury to PC12 cells by hydrogen peroxide. Compounds with promising neurorestorative activities (6k, 6o and 6p) were further evaluated for their in vivo effects by forced swim test (FST) and open field test (OFT) in C57 mice models. The FST results showed that compounds 6k, 6o and 6p remarkably reduced the immobility time of the tested mice. Among them, compound 6k was the most potent one, much more effective than Agomelatine and comparable to Fluoxetine. The OFT results showed that mice treated with compound 6k traveled a longer distance than those treated with Agomelatine or Fluoxetine, indicating a better general locomotor activity. The paper also proposed a possible binding mode of compound 6k with glucocorticoid receptor by docking study. The in vitro cytotoxicity data on HEK293 and L02 cells suggested compound 6k to be a promising antidepressant candidate for subsequent investigation.

  11. SORPTION ON WASTEWATER SOLIDS: ELIMINATION OF BIOLOGICAL ACTIVITY

    EPA Science Inventory

    Sorption was found to be greatly affected by the biological activity in wastewater solids. wo experimental techniques, cyanide treatment and pasteurization, were developed for eliminating the biological activity during isotherm measurements. oth methods are effective; however, pa...

  12. SORPTION ON WASTEWATER SOLIDS: ELIMINATION OF BIOLOGICAL ACTIVITY

    EPA Science Inventory

    Sorption was found to be greatly affected by the biological activity in wastewater solids. wo experimental techniques, cyanide treatment and pasteurization, were developed for eliminating the biological activity during isotherm measurements. oth methods are effective; however, pa...

  13. Synthesis of New Sulfated and Glucuronated Metabolites of Dietary Phenolic Compounds Identified in Human Biological Samples.

    PubMed

    Almeida, A Filipa; Santos, Cláudia N; Ventura, M Rita

    2017-02-23

    (Poly)phenols are a large group of dietary compounds present in fruits and vegetables; their consumption is associated with health beneficial effects. After ingestion, (poly)phenols suffer extensive metabolization, and the identification of their metabolites is an emerging area, because these metabolites are considered the effective bioactive molecules in the human organism. However, a lack of commercially available standards has hampered the study of metabolite bioactivity and the exact structural confirmation in biological samples. New (poly)phenol metabolites previously identified in human samples after the intake of berry juice were chemically synthesized. Efficient chemical reactions were performed with moderate to excellent yields and selectivities. These new compounds could be used as standard chemicals for confirmation of the structure of metabolites in biological samples and will also allow mechanistic studies in cellular models.

  14. Using synthetic biology to increase nitrogenase activity.

    PubMed

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

    2016-02-20

    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. In order to increase nitrogenase activity in heterologous host, a total of 28 selected genes from Paenibacillus sp. WLY78 and Klebsiella oxytoca were placed under the control of Paenibacillus nif promoter in two different vectors and then they are separately or combinationally transferred to the recombinant E. coli 78-7. Our results demonstrate that Paenibacillus suf operon (Fe-S cluster assembly) and the potential electron transport genes pfoAB, fldA and fer can increase nitrogenase activity. Also, K. oxytoca nifSU (Fe-S cluster assembly) and nifFJ (electron transport specific for nitrogenase) can increase nitrogenase activity. Especially, the combined assembly of the potential Paenibacillus electron transporter genes (pfoABfldA) with K. oxytoca nifSU recovers 50.1 % of wild-type (Paenibacillus) activity. However, K. oxytoca nifWZM and nifQ can not increase activity. The combined assembly of the potential Paenibacillus electron transporter genes (pfoABfldA) with K. oxytoca nifSU recovers 50.1 % of wild-type (Paenibacillus) activity in the recombinant E. coli 78-7. Our results will provide valuable insights for the enhancement of nitrogenase activity in heterogeneous host and will provide guidance for engineering cereal plants with minimal nif genes.

  15. Borrelidin B: isolation, biological activity, and implications for nitrile biosynthesis.

    PubMed

    Schulze, Christopher J; Bray, Walter M; Loganzo, Frank; Lam, My-Hanh; Szal, Teresa; Villalobos, Anabella; Koehn, Frank E; Linington, Roger G

    2014-11-26

    Borrelidin (1) is a nitrile-containing bacterially derived polyketide that is a potent inhibitor of bacterial and eukaryotic threonyl-tRNA synthetases. We now report the discovery of borrelidin B (2), a tetrahydro-borrelidin derivative containing an aminomethyl group in place of the nitrile functionality in borrelidin. The discovery of this new metabolite has implications for both the biosynthesis of the nitrile group and the bioactivity of the borrelidin compound class. Screening in the SToPS assay for tRNA synthetase inhibition revealed that the nitrile moiety is essential for activity, while profiling using our in-house image-based cytological profiling assay demonstrated that 2 retains biological activity by causing a mitotic stall, even in the absence of the nitrile motif.

  16. Synthesis and biological activity of radiolabeled phytosterols

    SciTech Connect

    De Palma, A.

    1984-01-01

    /sup 3/H and /sup 14/C-labeled phytosterols were synthesized for the purpose of elucidating insect sterol side-chain dealkylating mechanisms. Sitosterol, stigmasterol, and the 29-fluoro derivatives of these compounds, which are highly toxic, were labeled with /sup 3/H at C-29 in order to study the fate of the two-carbon dealkylation product in vivo and in vitro. The first rapid, reliable in vitro dealkylation bioassay was developed using doubly-labeled (29-/sup 3/H)-(24-/sup 14/C) fucosterol epoxides as the substrates, incubated with midgut preparations from Manduca sexta, the tobacco hornworm. Since C-28 and C-29 are lost in the dealkylation process, the extent of dealkylation is expressed as the change in the isotopic ratio when the system is partitioned between an organic solvent and water after incubation. As predicted, the /sup 3/H//sup 14/C ratio decreases in the organic layer as a function of time, due to loss of /sup 3/H into the aqueous phase as acetate or a biological equivalent. This ratio likewise increases in the aqueous phase for the same reason. The (29-/sup 3/H) phytosterols alone are reliable substrates for the first rapid in vivo bioassay of phytosterol dealkylation.

  17. Transport and biological activities of bile acids.

    PubMed

    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.

  18. Biologically active neutrophil chemokine pattern in tonsillitis

    PubMed Central

    RUDACK, C; JÖRG, S; SACHSE, F

    2004-01-01

    To gain an insight into the mechanisms of chronic and acute inflammation, the production of neutrophil chemokines in different types of tonsillitis – hyperplastic tonsillitis (HT), recurrent tonsillitis (RT) and peritonsillar abscesses (PA) – was investigated. The chemokines interleukin-8 (IL-8), growth-related oncogene-α (GRO-α), epithelial cell-derived neutrophil attractant-78 (ENA-78) and granulocyte chemotactic protein-2 (GCP-2) were detected and shown to have different biological activities. With respect to the biological properties of CXC chemokines, the biological activity of the chemokines was identified using a three-step high-performance liquid chromatography (HPLC) technique, a bioassay involving measurement of neutrophil chemotaxis in a single Boyden chamber in tissue of HT, RT and PA. Using reverse transcription-polymerase chain reaction (RT-PCR), the chemokine concentrations were determined in the different tonsillitis entities. The chemokine pattern was dominated in PA by IL-8 and GRO-α and in RT by GRO-α. Hyperplastic tonsils of patients without a history of infection generated about five times lower IL-8 than PA. A protein concentration of GCP-2 was induced in PA and RT, whereas ENA-78 remained the same in all entities. In conclusion, it would appear that IL-8 was up-regulated in acute inflammation, whereas GRO-α dominated in chronic inflammation. ENA-78 seems not to play a pivotal role in inflammatory processes in tonsils. GCP-2 may serve as a substitute chemokine in certain inflammatory conditions as its quantity of mRNA and protein was higher in RT and PA than in HT. PMID:15008987

  19. Biologically Active Secondary Metabolites from the Fungi.

    PubMed

    Bills, Gerald F; Gloer, James B

    2016-11-01

    Many Fungi have a well-developed secondary metabolism. The diversity of fungal species and the diversification of biosynthetic gene clusters underscores a nearly limitless potential for metabolic variation and an untapped resource for drug discovery and synthetic biology. Much of the ecological success of the filamentous fungi in colonizing the planet is owed to their ability to deploy their secondary metabolites in concert with their penetrative and absorptive mode of life. Fungal secondary metabolites exhibit biological activities that have been developed into life-saving medicines and agrochemicals. Toxic metabolites, known as mycotoxins, contaminate human and livestock food and indoor environments. Secondary metabolites are determinants of fungal diseases of humans, animals, and plants. Secondary metabolites exhibit a staggering variation in chemical structures and biological activities, yet their biosynthetic pathways share a number of key characteristics. The genes encoding cooperative steps of a biosynthetic pathway tend to be located contiguously on the chromosome in coregulated gene clusters. Advances in genome sequencing, computational tools, and analytical chemistry are enabling the rapid connection of gene clusters with their metabolic products. At least three fungal drug precursors, penicillin K and V, mycophenolic acid, and pleuromutilin, have been produced by synthetic reconstruction and expression of respective gene clusters in heterologous hosts. This review summarizes general aspects of fungal secondary metabolism and recent developments in our understanding of how and why fungi make secondary metabolites, how these molecules are produced, and how their biosynthetic genes are distributed across the Fungi. The breadth of fungal secondary metabolite diversity is highlighted by recent information on the biosynthesis of important fungus-derived metabolites that have contributed to human health and agriculture and that have negatively impacted crops

  20. New lignans and their biological activities.

    PubMed

    Zhang, Jia; Chen, Jiejun; Liang, Zizhen; Zhao, Changqi

    2014-01-01

    Lignans, which are widely distributed in higher plants, represent a vast and rather diverse group of phenylpropane derivatives. They have attracted considerable attention due to their pharmacological activities. Some of the lignans have been developed approved therapeutics, and others are considered as lead structures for new drugs. This article is based on our previous review of lignans discovered in the period 2000-2004, and it provides a comprehensive compilation of the 354 new naturally occurring lignans obtained from 61 plant families between 2005 and 2011. We classified five main types according to their structural features, and provided the details of their sources, some typical structures, and diverse biological activities. A tabular compilation of the novel lignans by species is presented at the end. A total of 144 references were considered for this review. Copyright © 2014 Verlag Helvetica Chimica Acta AG, Zürich.

  1. Spectroscopic study of biologically active glasses

    NASA Astrophysics Data System (ADS)

    Szumera, M.; Wacławska, I.; Mozgawa, W.; Sitarz, M.

    2005-06-01

    It is known that the chemical activity phenomenon is characteristic for some inorganic glasses and they are able to participate in biological processes of living organisms (plants, animals and human bodies). An example here is the selective removal of silicate-phosphate glass components under the influence of biological solutions, which has been applied in designing glasses acting as ecological fertilizers of controlled release rate of the nutrients for plants. The structure of model silicate-phosphate glasses containing the different amounts of the glass network formers, i.e. Ca 2+ and Mg 2+, as a binding components were studied. These elements besides other are indispensable of the normal growth of plants. In order to establish the function and position occupied by the particular components in the glass structure, the glasses were examined by FTIR spectroscopy (with spectra decomposition) and XRD methods. It has been found that the increasing amount of MgO in the structure of silicate-phosphate glasses causes the formation of domains the structure of which changes systematically from a structure of the cristobalite type to a structure corresponding to forsterite type. Whilst the increasing content of CaO in the structure of silicate-phosphate glasses causes the formation of domains the structure of which changes from a structure typical for cristobalite through one similar to the structure of calcium orthophosphate, to a structure corresponding to calcium silicates. The changing character of domains structure is the reason of different chemical activity of glasses.

  2. Carbon nanomaterials: Biologically active fullerene derivatives.

    PubMed

    Bogdanović, Gordana; Djordjević, Aleksandar

    2016-01-01

    Since their discovery, fullerenes, carbon nanotubes, and graphene attract significant attention of researches in various scientific fields including biomedicine. Nano-scale size and a possibility for diverse surface modifications allow carbon nanoallotropes to become an indispensable nanostructured material in nanotechnologies, including nanomedicine. Manipulation of surface chemistry has created diverse populations of water-soluble derivatives of fullerenes, which exhibit different behaviors. Both non-derivatized and derivatized fullerenes show various biological activities. Cellular processes that underline their toxicity are oxidative, genotoxic, and cytotoxic responses.The antioxidant/cytoprotective properties of fullerenes and derivatives have been considered in the prevention of organ oxidative damage and treatment. The same unique physiochemical properties of nanomaterials may also be associated with potential health hazards. Non-biodegradability and toxicity of carbon nanoparticles still remain a great concern in the area of biomedical application. In this review, we report on basic physical and chemical properties of carbon nano-clusters--fullerenes, nanotubes, and grapheme--their specificities, activities, and potential application in biological systems. Special emphasis is given to our most important results obtained in vitro and in vivo using polyhydroxylated fullerene derivative C₆₀(OH)₂₄.

  3. Identification of Telomerase-activating Blends From Naturally Occurring Compounds.

    PubMed

    Ait-Ghezala, Ghania; Hassan, Samira; Tweed, Miles; Paris, Daniel; Crynen, Gogce; Zakirova, Zuchra; Crynen, Stefan; Crawford, Fiona

    2016-06-01

    Context • Telomeres are repeated deoxyribonucleic acid (DNA) sequences (TTAGGG) that are located on the 5' ends of chromosomes, and they control the life span of eukaryotic cells. Compelling evidence has shown that the length of a person's life is dictated by the limited number of times that a human cell can divide. The enzyme telomerase has been shown to bind to and extend the length of telomeres. Thus, strategies for activating telomerase may help maintain telomere length and, thus, may lead to improved health during aging. Objective • The current study intended to investigate the effects of several natural compounds on telomerase activity in an established cell model of telomere shortening (ie, IMR90 cells). Design • The research team designed an in vitro study. Setting • The study was conducted at Roskamp Institute in Sarasota, FL, USA. Intervention • The tested single compounds were (1) α-lipoic acid, (1) green tea extract, (2) dimethylaminoethanol L-bitartrate (DMAE L-bitartrate), (3) N-acetyl-L-cysteine hydrochloride (HCL), (4) chlorella powder, (5) L-carnosine, (6) vitamin D3, (7) rhodiola PE 3%/1%, (8) glycine, (9) French red wine extract, (10) chia seed extract, (11) broccoli seed extract, and (12) Astragalus (TA-65). The compounds were tested singly and as blends. Outcome Measures • Telomerase activity for single compounds and blends of compounds was measured by the TeloTAGGG telomerase polymerase chain reaction (PCR) enzyme-linked immunosorbent assay (ELISA). The 4 most potent blends were investigated for their effects on cancer-cell proliferation and for their potential effects on the cytotoxicity and antiproliferative activity of a chemotherapeutic agent, the topoisomerase I inhibitor topotecan. The benefits of 6 population doublings (PDs) were measured for the single compounds, and the 4 blends were compared to 3 concentrations of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). Results • Certain of the compounds increased

  4. Different phenolic compounds activate distinct human bitter taste receptors.

    PubMed

    Soares, Susana; Kohl, Susann; Thalmann, Sophie; Mateus, Nuno; Meyerhof, Wolfgang; De Freitas, Victor

    2013-02-20

    Bitterness is a major sensory attribute of several common foods and beverages rich in polyphenol compounds. These compounds are reported as very important for health as chemopreventive compounds, but they are also known to taste bitter. In this work, the activation of the human bitter taste receptors, TAS2Rs, by six polyphenol compounds was analyzed. The compounds chosen are present in a wide range of plant-derived foods and beverages, namely, red wine, beer, tea, and chocolate. Pentagalloylglucose (PGG) is a hydrolyzable tannin, (-)-epicatechin is a precursor of condensed tannins, procyanidin dimer B3 and trimer C2 belong to the condensed tannins, and malvidin-3-glucoside and cyanidin-3-glucoside are anthocyanins. The results show that the different compounds activate different combinations of the ~25 TAS2Rs. (-)-Epicatechin activated three receptors, TAS2R4, TAS2R5, and TAS2R39, whereas only two receptors, TAS2R5 and TAS2R39, responded to PGG. In contrast, malvidin-3-glucoside and procyanidin trimer stimulated only one receptor, TAS2R7 and TAS2R5, respectively. Notably, tannins are the first natural agonists found for TAS2R5 that display high potency only toward this receptor. The catechol and/or galloyl groups appear to be important structural determinants that mediate the interaction of these polyphenolic compounds with TAS2R5. Overall, the EC(50) values obtained for the different compounds vary 100-fold, with the lowest values for PGG and malvidin-3-glucoside compounds, suggesting that they could be significant polyphenols responsible for the bitterness of fruits, vegetables, and derived products even if they are present in very low concentrations.

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

    PubMed

    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.

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

    PubMed

    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. Copyright © 2013 Elsevier Inc. All rights reserved.

  7. THE BIOLOGICAL ACTIVITIES OF HYPERICUM PERFORATUM L.

    PubMed Central

    Okmen, Gulten; Balpınar, Neslihan

    2017-01-01

    Background: Mastitis reduces milk yield and alters milk composition. Antibiotics are widely used in the treatment of the disease. However, this widespread use of antibiotics causes both antibiotic residues in milks and antibiotic resistance developed in bacteria. Today’s researches are focused on discovering and using new antibiotics against bacteria. Objective: The aim of this work was to discover the antibacterial effects of Hypericum perforatum L. extracts against mastitis pathogens, and its other biological activities. Material and Methods: Kirby-Bauer assay was applied to the extracts. The other antibacterial activity was MIC for plant extracts. The non-enzymatic antioxidant activity was found using 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH). Results: The extract was showed maximum inhibition zone against two bacteria (Coagulase-negative Staphylococci-33 and 37; CNS 33 and 37), and the zone was 17 mm. A bacterium (CNS - 22) showed the lowest sensitivity to 812.5 μg/mL concentration. In addition, the extract was tried against the stable DPPH for antioxidant activity. As a result, the extract showed a strength antioxidant activity. Trolox equivalent is 0.83 mM. Conclusion: The extract of Hypericum perforatum have antibacterial, antioxidant and antimutagenic potentials. PMID:28480399

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

    PubMed

    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.

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

    PubMed

    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.

  10. Phytochemistry and biological activities of Phlomis species.

    PubMed

    Limem-Ben Amor, Ilef; Boubaker, Jihed; Ben Sgaier, Mohamed; Skandrani, Ines; Bhouri, Wissem; Neffati, Aicha; Kilani, Soumaya; Bouhlel, Ines; Ghedira, Kamel; Chekir-Ghedira, Leila

    2009-09-07

    The genus Phlomis L. belongs to the Lamiaceae family and encompasses 100 species native to Turkey, North Africa, Europe and Asia. It is a popular herbal tea enjoyed for its taste and aroma. Phlomis species are used to treat various conditions such as diabetes, gastric ulcer, hemorrhoids, inflammation, and wounds. This review aims to summarize recent research on the phytochemistry and pharmacological properties of the genus Phlomis, with particular emphasis on its ethnobotanical uses. The essential oil of Phomis is composed of four chemotypes dominated by monoterpenes (alpha-pinene, limonene and linalool), sesquiterpenes (germacrene D and beta-caryophyllene), aliphalic compounds (9,12,15-octadecatrienoic acid methyl ester), fatty acids (hexadecanoic acid) and other components (trans-phytol, 9,12,15-octadecatrien-1-ol). Flavonoids, iridoids and phenylethyl alcohol constitute the main compounds isolated from Phlomis extracts. The pharmacological activities of some Phlomis species have been investigated. They are described according to antidiabetic, antinociceptive, antiulcerogenic, protection of the vascular system, anti-inflammatory, antiallergic, anticancer, antimicrobial and antioxidant properties.

  11. Antioxidant Activity of Phenolic Compounds from Fava Bean Sprouts.

    PubMed

    Okumura, Koharu; Hosoya, Takahiro; Kawarazaki, Kai; Izawa, Norihiko; Kumazawa, Shigenori

    2016-06-01

    Fava beans are eaten all over the world and recently, marketing for their sprouts began in Japan. Fava bean sprouts contain more polyphenols and l-3,4-dihydroxyphenylalanine (l-DOPA) than the bean itself. Our antioxidant screening program has shown that fava bean sprouts also possess a higher antioxidant activity than other commercially available sprouts and mature beans. However, the individual constituents of fava bean sprouts are not entirely known. In the present study, we investigated the phenolic compounds of fava bean sprouts and their antioxidant activity. Air-dried fava bean sprouts were treated with 80% methanol and the extract was partitioned in water with chloroform and ethyl acetate. HPLC analysis had shown that the ethyl acetate-soluble parts contained phenolic compounds, separated by preparative HPLC to yield 5 compounds (1-5). Structural analysis using NMR and MS revealed that the compounds isolated were kaempferol glycosides. All isolated compounds had an α-rhamnose at the C-7 position with different sugars attached at the C-3 position. Compounds 1-5 had β-galactose, β-glucose, α-rhamnose, 6-acetyl-β-galactose and 6-acetyl-β-glucose, respectively, at the C-3 position. The amount of l-DOPA in fava bean sprouts was determined by the quantitative (1) H NMR technique. The l-DOPA content was 550.45 mg ± 11.34 /100 g of the raw sprouts. The antioxidant activities of compounds 2-5 and l-DOPA were evaluated using the 2,2-diphenyl-1-picrylhydrazyl scavenging assay. l-DOPA showed high antioxidant activity, but the isolated kaempferol glycosides showed weak activity. Therefore, it can be suggested that l-DOPA contributed to the antioxidant activity of fava bean sprouts. © 2016 Institute of Food Technologists®

  12. Biokinetics of nuclear fuel compounds and biological effects of nonuniform radiation.

    PubMed Central

    Lang, S; Servomaa, K; Kosma, V M; Rytömaa, T

    1995-01-01

    Environmental releases of insoluble nuclear fuel compounds may occur at nuclear power plants during normal operation, after nuclear power plant accidents, and as a consequence of nuclear weapons testing. For example, the Chernobyl fallout contained extensive amounts of pulverized nuclear fuel composed of uranium and its nonvolatile fission products. The effects of these highly radioactive particles, also called hot particles, on humans are not well known due to lack of reliable data on the extent of the exposure. However, the biokinetics and biological effects of nuclear fuel compounds have been investigated in a number of experimental studies using various cellular systems and laboratory animals. In this article, we review the biokinetic properties and effects of insoluble nuclear fuel compounds, with special reference to UO2, PuO2, and nonvolatile, long-lived beta-emitters Zr, Nb, Ru, and Ce. First, the data on hot particles, including sources, dosimetry, and human exposure are discussed. Second, the biokinetics of insoluble nuclear fuel compounds in the gastrointestinal tract and respiratory tract are reviewed. Finally, short- and long-term biological effects of nonuniform alpha- and beta-irradiation on the gastrointestinal tract, lungs, and skin are discussed. Images p920-a Figure 1. PMID:8529589

  13. Synthesis and Radioprotective Activity of New Organosilicon and Germanium Compounds

    PubMed Central

    Rima, Ghassoub; Dagiral, Rodolphe; Lion, Claude; Fatome, Marc; Roman, Vincent; Laval, Jean-Denis

    1998-01-01

    Silathiazolidine and metalladithioacetals (M = Si, Ge) have been prepared by the interaction of dialkyldichloro- or bis(diethylamino)dialkylsilanes and -germanes with 3-[N-(2- thioethyl)]amino-propanamide (WR-2529) and [1-thioethyl-2-(1-naphtylmethyl)]-2- imidazoline. The study of these compounds in the field of chemical radioprotection has shown a notable decrease in the toxicity and a rather large increase in the radioprotective activity of these new derivatives in comparison with the starting organic compounds. PMID:18475835

  14. Nematicidal Activity of Cassia and Cinnamon Oil Compounds and Related Compounds toward Bursaphelenchus xylophilus (Nematoda: Parasitaphelenchidae)

    PubMed Central

    Kong, Jeong-Ok; Lee, Sang-Myung; Moon, Yil-Seong; Lee, Sang-Gil; Ahn, Young-Joon

    2007-01-01

    The nematicidal activity of two cassia, Cinnamomum cassia, oils (Especial and true), four cinnamon, Cinnamomum zey-lanicum, oils (technical, #500, bark and green leaf), and their compounds (e.g., trans-cinnamaldehyde and trans-cinnamic acid) toward adult Bursaphelenchus xylophilus was examined by a direct contact bioassay. Results were compared with those of 34 related compounds. As judged by 24-hour LC50 values, two cassia oils (0.084–0.085 mg/ml) and four cinnamon oils (0.064–0.113 mg/ml) were toxic toward adult B. xylophilus. Of 45 test compounds, trans-cinnamaldehyde (0.061 mg/ml) was the most active nematicide, followed by ethyl cinnamate, α-methyl-trans-cinnamaldehyde, methyl cinnamate and allyl cinnamate (0.114–0.195 mg/ml). Potent nematicidal activity was also observed with 4-methoxycinnamonitrile, trans-4-methoxycinnamaldehyde, trans-2-methoxy-cinnamaldehyde, ethyl α-cyanocinnamate, cinnamonitrile and cinnamyl bromide (0.224–0.502 mg/ml). Structure-activity relationships indicate that structural characteristics, such as types of functional groups, saturation and carbon skeleton, appear to play a role in determining the toxicities to adult B. xylophilus. Cassia and cinnamon oils and test compounds described merit further study as potential nematicides or leads for the control of pine wilt disease caused by B. xylophilus. PMID:19259472

  15. Neuroprotective activity and cytotoxic potential of two Parmeliaceae lichens: Identification of active compounds.

    PubMed

    Fernández-Moriano, Carlos; Divakar, Pradeep Kumar; Crespo, Ana; Gómez-Serranillos, M Pilar

    2015-08-15

    Lichens are symbiotic organisms capable of producing unique secondary metabolites, whose pharmacological activities are attracting much interest. The present study aimed to investigate the in vitro neuroprotective effects and anticancer potential of methanol extracts of two Parmeliaceae lichens: Cetraria islandica and Vulpicida canadensis. The chemical composition of the two lichens was also determined. Neuroprotective activity was studied with respect to the antioxidant properties of the extracts; radical scavenging tests (ORAC and DPPH assays) were performed and oxidative stress markers (intracellular ROS production, caspase-3 activity, MDA and glutathione levels) were assessed in a hydrogen peroxide-induced oxidative stress model in astrocytes. Cytotoxic activity was tested against human HepG2 (hepatocellular carcinoma) and MCF-7 (breast adenocarcinoma) cell lines. Cell viability studies identified a single concentration for each extract that was subsequently used to measure oxidative stress markers. Lichen extracts were able to reverse the oxidative damage caused by hydrogen peroxide, thus promoting astrocyte survival. Both lichen extracts also had anticancer activity in the cell lines, with IC50 values of 19.51-181.05 µg/ml. The extracts had a high total phenolic content, and the main constituents identified by HPLC were fumarprotocetraric acid in Cetraria islandica, and usnic, pinastric and vulpinic acids in Vulpicida canadensis. The biological activities of the lichen extracts can be attributed to these secondary metabolites. The lichen species studied are promising sources of natural compounds with neuroprotective activity and cytotoxic potential, and warrant further research. Copyright © 2015. Published by Elsevier GmbH.

  16. Scalarane and homoscalarane compounds from the nudibranchs Glossodoris sedna and Glossodoris dalli: chemical and biological properties.

    PubMed

    Fontana, A; Mollo, E; Ortea, J; Gavagnin, M; Cimino, G

    2000-04-01

    A series of homoscalarane and scalarane compounds (2-7) have been isolated from two distinct species of Pacific Glossodoris nudibranchs. The structure and elucidation of the relative stereochemistry of the new metabolites 2 and 3 were obtained by spectroscopic methods. Compound 2 was ichthyotoxic at 0.1 ppm against Gambusia affinis and showed moderate activity (IC(50) 18 microM) to inhibit mammalian phospholipase A(2).

  17. Antimicrobial activity of extractable conifer heartwood compounds toward Phytophthora ramorum.

    PubMed

    Manter, Daniel K; Kelsey, Rick G; Karchesy, Joseph J

    2007-11-01

    Ethyl acetate extracts from heartwood of seven western conifer trees and individual volatile compounds in the extracts were tested for antimicrobial activity against Phytophthora ramorum. Extracts from incense and western redcedar exhibited the strongest activity, followed by yellow-cedar, western juniper, and Port-Orford-cedar with moderate activity, and no activity for Douglas-fir and redwood extracts. Chemical composition of the extracts varied both qualitatively and quantitatively among the species with a total of 37 compounds identified by mass spectrometry. Of the 13 individual heartwood compounds bioassayed, three showed strong activity with a Log(10) EC(50) less than or equal to 1.0 ppm (hinokitiol, thymoquinone, and nootkatin), three expressed moderate activity ranging from 1.0-2.0 ppm (nootkatol, carvacrol, and valencene-11,12-diol), four compounds had weak activity at 2.0-3.0 ppm [alpha-terpineol, valencene-13-ol, (+)-beta-cedrene, (-)-thujopsene], and three had no activity [(+)-cedrol, delta-cadinene, and methyl carvacrol]. All of the most active compounds contained a free hydroxyl group, except thymoquinone. The importance of a free hydroxyl was demonstrated by the tremendous difference in activity between carvacrol (Log(10) EC(50) 1.81 +/- 0.08 ppm) and methyl carvacrol (Log(10) EC(50) >3.0 ppm). A field trial in California, showed that heartwood chips from redcedar placed on the forest floor for 4 months under Umbellularia californica (California bay laurel) with symptoms of P. ramorum leaf blight significantly limited the accumulation of P. ramorum DNA in the litter layer, compared with heartwood chips from redwood.

  18. Steroid hormone activity of flavonoids and related compounds.

    PubMed

    Zand, R S; Jenkins, D J; Diamandis, E P

    2000-07-01

    Soy isoflavones have been studied extensively for estrogenic and antiestrogenic properties. Other flavonoids, found in fruits, vegetables, tea and wine, have been much less tested for steroid hormone activity. We therefore assessed the estrogenic, androgenic and progestational activities of 72 flavonoids and structurally-related compounds. These compounds were tested on BT-474 human breast cancer cells at concentrations of 10(8)-10(-5) M, with estradiol (estrogen), norgestrel (progestin) and dihydrotestosterone (androgen) used as positive controls, and ethanol (solvent) as a negative control. pS2, an estrogen-regulated protein, and prostate-specific antigen (PSA), regulated by androgens and progestins, were quantified in tissue culture supernatants using ELISA-type immunofluorometric assays developed in-house. Of the 72 compounds tested, 18 showed estrogenic activity at 10(-5) M. Of this subset, seven also showed progestational activity at this concentration. The soy isoflavones, biochanin A and genistein, showed the most potent estrogenic activity, with a dose-response effect up to 10(-7) M. Of all other flavonoids, luteolin and naringenin displayed the strongest estrogenicity, while apigenin had a relatively strong progestational activity. Based on our data, we have formulated a set of structure/function relationships between the tested compounds. Flavonoids, therefore, exhibit significant steroid hormone activity, and may have an effect in the modification of cancer risk by diet, or in cancer therapeutics and prevention.

  19. Gynura procumbens: An Overview of the Biological Activities

    PubMed Central

    Tan, Hui-Li; Chan, Kok-Gan; Pusparajah, Priyia; Lee, Learn-Han; Goh, Bey-Hing

    2016-01-01

    Gynura procumbens (Lour.) Merr. (Family Asteraceae) is a medicinal plant commonly found in tropical Asia countries such as China, Thailand, Indonesia, Malaysia, and Vietnam. Traditionally, it is widely used in many different countries for the treatment of a wide variety of health ailments such as kidney discomfort, rheumatism, diabetes mellitus, constipation, and hypertension. Based on the traditional uses of G. procumbens, it seems to possess high therapeutic potential for treatment of various diseases making it a target for pharmacological studies aiming to validate and provide scientific evidence for the traditional claims of its efficacy. Although there has been considerable progress in the research on G. procumbens, to date there is no review paper gathering the reported biological activities of G. procumbens. Hence, this review aims to provide an overview of the biological activities of G. procumbens based on reported in vitro and in vivo studies. In brief, G. procumbens has been reported to exhibit antihypertensive, cardioprotective, antihyperglycemic, fertility enhancement, anticancer, antimicrobial, antioxidant, organ protective, and antiinflammatory activity. The commercial applications of G. procumbens have also been summarized in this paper based on existing patents. The data compiled illustrate that G. procumbens is a potential natural source of compounds with various pharmacological actions which can be utilized for the development of novel therapeutic agents. PMID:27014066

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

    PubMed

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

    NASA Astrophysics Data System (ADS)

    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.

  2. [Composition and biological activity of triterpenes and steroids from Inonotus obliquus (chaga)].

    PubMed

    Nikitina, S A; Khabibrakhmanova, V R; Sysoeva, M A

    2016-05-01

    Data on the chemical composition of triterpenic and steroid compounds, isolated from the chaga mushroom grown in natural environment or in a synthetic culture have been summarized. Special attention has been paid to the biological activity of chaga mushroom extracts and these particular compounds against various cancer cell lines in vitro and in vivo. This analysis has demonstrated some common features in inhibition of growth of various cell lines by chaga mushroom components. In this context, the most active are triterpene compounds containing OH group at C-22 and a side chain unsaturated bond.

  3. Organogold(III) compounds as experimental anticancer agents: chemical and biological profiles.

    PubMed

    Massai, Lara; Cirri, Damiano; Michelucci, Elena; Bartoli, Gianluca; Guerri, Annalisa; Cinellu, Maria A; Cocco, Fabio; Gabbiani, Chiara; Messori, Luigi

    2016-10-01

    In the last few years gold(III) complexes have attracted growing attention in the medicinal chemistry community as candidate anticancer agents. In particular some organogold(III) compounds manifested quite attractive pharmacological behaviors in preclinical studies. Here we compare the chemical and biological properties of the novel organogold(III) complex [Au(bipy(dmb)-H)(NH(CO)CH3)][PF6] (Aubipy(aa)) with those of its parent compounds [Au(bipy(dmb)-H)(OH)][PF6] (Aubipy(c)) and [Au2(bipy(dmb)-H)2)(μ-O)][PF6]2 (Au2bipy(c)), previously synthesized and characterized. The three study compounds were comparatively assessed for their antiproliferative actions against HCT-116 cancer cells, revealing moderate cytotoxic effects. Proapoptotic and cell cycle effects were also monitored. Afterward, to gain additional mechanistic insight, the three gold compounds were challenged against the model proteins HEWL, RNase A and cytochrome c and reactions investigated through UV-Vis and ESI-MS analysis. A peculiar and roughly invariant protein metalation profile emerges in the three cases consisting of protein binding of {Au(bipy(dmb)-H)} moieties. The implications of these results are discussed in the frame of current knowledge on anticancer gold compounds.

  4. Biological activity of phenolic compounds. Hepatic cytochrome P-450, cytochrome b/sub 5/ and NADPH cytochrome c reductase in chicks and rats fed phenolic monomers, polymers, and glycosides

    SciTech Connect

    Klasing, S.A.; Mora, M.I.; Wilson, W.C.; Fahey, G.C. Jr.; Garst, J.E.

    1985-09-01

    Experiments were conducted to determine effects of a phenolic polymer (Kraft wood lignin, Indulin), phenolic glycosides (cane molasses and wood molasses), and phenolic monomers (vanillin, vanillic acid, ferulic acid, and p-coumaric acid) on liver cytochromes P-450, cytochrome b/sub 5/, and NADPH cytochrome c reductase in chicks and rats. Chicks fed 6.0% lignin had a higher cytochromes P-450 content than did chicks fed 0% fiber, 6.0% wood cellulose, or 6.0% arenaceous flour. Chicks fed 12.0% wood molasses had a higher cytochromes P-450 level than did chicks fed 0% fiber or 6.0% wood molasses. Cane molasses incorporated at both 6.0 and 12.0% of the diet induced cytochromes P-450 content over those of control-fed birds. Chicks fed 6.0% lignin, with or without antibiotic, had a higher cytochromes P-450 level than did chicks fed control diets, with or without antibiotic. Additionally, chicks fed 6.0% lignin had lower intestinal diaminopimelic acid (DAP) levels than did chicks fed 0% fiber. Rats fed 0% fiber, 6.0% wood cellulose, 6.0% arenaceous flour, or 6.0% lignin exhibited no difference in cytochrome level or activity among treatments. Chicks fed 0.5% vanillin, 0.5% vanillic acid, 0.5% ferulic acid, or 0.5% p-coumaric acid had comparable cytochromes level and activity compared with chicks fed no phenolics. Chicks fed 0.5% p-coumaric acid had lower rates of gain than did chicks fed control or other phenolic-containing diets. Rats fed these phenolics had similar cytochromes P-450 content among treatments.

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

    PubMed

    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.

  6. New Imidazole-Based Compounds Active Against Trypanosoma cruzi.

    PubMed

    Adeyemi, Oluyomi Stephen; Molina, María Teresa; Eseola, Abiodun Omokehinde; Fonseca-Berzal, Cristina; Gómez-Barrio, Alicia

    2017-01-01

    Current drugs available for the treatment of Chagas disease are fraught with several challenges including severe toxicity and limited efficacy. These factors coupled with the absence of effective drugs for treating the chronic stage of the disease have rendered the development of new drugs against Chagas disease a priority. This study screened several imidazole-based compounds for anti-Trypanosoma potential. Using an in vitro experimental infection model, several imidazole-based compounds were screened for anti-proliferative effect on Trypanosoma cruzi epimastigotes. Additionally, all test compounds were evaluated for unspecific cytotoxicity on L929 murine fibroblasts. Benznidazole (BZN) served as reference drug. All test compounds demonstrated interesting trypanocidal potential with IC50 values in the μM range (1< 1C50 <8 μM). The activities of the test compounds compared favorably with BZN, which had an IC50 value ca. 30 μM. Conversely, most of the test compounds were highly cytotoxic, resulting in selectivity lower than that of BZN (SI > 9.42). We provide evidence which implicate the imidazole-based compounds as potential prototypes for the development of anti-parasitic agents. Findings have far-reaching relevance to drug discovery efforts for trypanosomiasis. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

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

    NASA Astrophysics Data System (ADS)

    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.

  8. Multifunctional activity of polyphenolic compounds associated with a potential for Alzheimer's disease therapy from Ecklonia cava.

    PubMed

    Choi, Byoung Wook; Lee, Hye Sook; Shin, Hyeon-Cheol; Lee, Bong Ho

    2015-04-01

    Five polyphenols were isolated and purified from a brown alga Ecklonia cava. These compounds showed diverse biological activities such as antioxidative, antiinflammatory, and enzyme inhibitory activities. This led us to investigate the potential of these compounds as Alzheimer's disease drugs. All of the compounds showed moderate acetylcholinesterase inhibitory activity in a micromolar range (IC50 from 16.0 to 96.3 μM). For butyrylcholinesterase, a new target for the treatment of Alzheimer's disease, phlorofucofuroeckol-A (PFF-A), showed a particularly potent inhibitory activity (IC50 0.95 μM), which is over 100-fold greater than for acetylcholinesterase. These compounds inhibited glycogen synthase kinase 3 beta, which is related to the formation of hyperphosphorylated tau and generation Aβ. Bieckol and PFF-A inhibited amyloid precursor protein biosynthesis. PFF-A also showed very strong β-secretase inhibitory activity with IC50 of submicromole. These results render these compounds as interesting potential drug candidates for Alzheimer's disease.

  9. Biologically active and antimicrobial peptides from plants.

    PubMed

    Salas, Carlos E; Badillo-Corona, Jesus A; Ramírez-Sotelo, Guadalupe; Oliver-Salvador, Carmen

    2015-01-01

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

  10. Biologically Active and Antimicrobial Peptides from Plants

    PubMed Central

    Salas, Carlos E.; Badillo-Corona, Jesus A.; Ramírez-Sotelo, Guadalupe; Oliver-Salvador, Carmen

    2015-01-01

    Bioactive peptides are part of an innate response elicited by most living forms. In plants, they are produced ubiquitously in roots, seeds, flowers, stems, and leaves, highlighting their physiological importance. While most of the bioactive peptides produced in plants possess microbicide properties, there is evidence that they are also involved in cellular signaling. Structurally, there is an overall similarity when comparing them with those derived from animal or insect sources. The biological action of bioactive peptides initiates with the binding to the target membrane followed in most cases by membrane permeabilization and rupture. Here we present an overview of what is currently known about bioactive peptides from plants, focusing on their antimicrobial activity and their role in the plant signaling network and offering perspectives on their potential application. PMID:25815307

  11. Chlorinated and brominated persistent organic compounds in biological samples from the environment

    SciTech Connect

    Jansson, B.; Andersson, R.; Asplund, L.; Litzen, K.; Nylund, K.; Sellstroem, U.; Uvemo, U.; Wahlberg, C.; Wideqvist, U. . Inst. of Applied Environmental Research); Odsjoe, T.; Olsson, M. . Section for Vertebrate Zoology)

    1993-07-01

    Eleven selected biological samples representing different ecosystems, trophic levels, and areas mainly in Sweden have been analyzed for 31 halogenated organic compounds or compound groups. The multiresidue analytical method provides a good opportunity to compare the concentrations of the different compounds in the investigated samples. By the use of ratios of these concentrations, comparisons can be done between species and areas. An attempt to describe an environmental distribution profile is demonstrated for some of the compounds using the concentration ratio between these compounds and 2,2[prime],4,4[prime],5,5[prime]-hexachlorobiphenyl (PCB 153). Chlorinated paraffins (CPs) were found in all samples and in some of them at higher concentrations than the polychlorinated biphenyls (PCBs). The ratio of CP to PCB 153 is higher in the investigated terrestrial species than in the aquatic, which is not the case for the other compounds. Polybrominated diphenyl ethers were also found in all but one sample. The concentrations were highest in industrialized areas but were also present in samples from background areas. Seven major cogeners of PCBs were determined; the sum ranged from 50 to 200,000 ng/g lw in the investigated samples. Three coplanar PCB congeners were also analyzed as well as polychlorinated naphthalenes, which were found at levels between 0.038 and 50 ng/g lw. The latter two groups do not seem to biomagnify in the foot chain of herring to grey seal to the same extent as the major PCB compounds. Pentachlorobenzene was found in only three of the samples, whereas hexachlorobenzene was present in all samples.

  12. [Nonequilibrium state of electrochemically activated water and its biological activity].

    PubMed

    Petrushanko, I Iu; Lobyshev, V I

    2001-01-01

    Changes in the physicochemical parameters (pH, redox potential and electroconductivity) of catholyte and anolyte produced by membrane electrolysis of distilled water and dilute (c < 10(-3) M) sodium chloride solutions were studied. The relaxation of these parameters after electrolysis and the influence of catholyte and anolyte on the growth of roots of Tradescantia viridis grafts, the development of duckweed, and the motive activity of infusoria Spirostomum ambiguum were investigated. It was found that the anolyte of distilled water stimulated development of these biological objects. The direction of shift of physicochemical parameters of catholyte and anolyte from equilibrium values and the type of their biological activity (stimulation or inhibition) depend on salt concentration in initial solution. Barbotage of initial distilled water with argon or nitrogen leads to a greater decrease in the redox potential of catholyte during electrolysis. The physicochemical parameters relax to equilibrium values, and the biological activity of catholite and anolyte decreases with time and practically disappears by the end of the day. It was found that the oxidation of reducing agent by atmospheric oxygen is not the sole cause of the relaxation of catalyte redox potential. The increase in the ionic strength of catholite and anolyte by the addition of concentrated sodium chloride after electrolysis decreases the rate of redox potential relaxation several times. The redox potential can be maintained for long periods by freezing.

  13. Fate of alkylphenolic compounds during activated sludge treatment: impact of loading and organic composition.

    PubMed

    McAdam, Ewan J; Bagnall, John P; Soares, Ana; Koh, Yoong K K; Chiu, Tze Y; Scrimshaw, Mark D; Lester, John N; Cartmell, Elise

    2011-01-01

    The impact of loading and organic composition on the fate of alkylphenolic compounds in the activated sludge plant (ASP) has been studied. Three ASP designs comprising carbonaceous, carbonaceous/nitrification, and carbonaceous/nitrification/denitrification treatment were examined to demonstrate the impact of increasing levels of process complexity and to incorporate a spectrum of loading conditions. Based on mass balance, overall biodegradation efficiencies for nonylphenol ethoxylates (NPEOs), short chain carboxylates (NP(1-3)EC) and nonylphenol (NP) were 37%, 59%, and 27% for the carbonaceous, carbonaceous/nitrification, and carbonaceous/nitrification/denitrification ASP, respectively. The presence of a rich community of ammonia oxidizing bacteria does not necessarily facilitate effective alkylphenolic compound degradation. However, a clear correlation between alkylphenolic compound loading and long chain ethoxylate compound biodegradation was determined at the three ASPs, indicating that at higher initial alkylphenolic compound concentrations (or load), greater ethoxylate biotransformation can occur. In addition, the impact of settled sewage organic composition on alkylphenolic compound removal was evaluated. A correlation between the ratio of chemical oxygen demand (COD) to alkylphenolic compound concentration and biomass activity was determined, demonstrating the inhibiting effect of bulk organic matter on alkylphenol polyethoxylate transformation activity. At all three ASPs the biodegradation pathway proposed involves the preferential biodegradation of the amphiphilic ethoxylated compounds, after which the preferential attack of the lipophilic akylphenol moiety occurs. The extent of ethoxylate biodegradation is driven by the initial alkylphenolic compound concentration and the proportion of COD constituted by the alkylphenol polyethoxylates (APEOs) and their metabolites relative to the bulk organic concentration of the sewage composed of proteins, acids, fats

  14. Chemistry, biogenesis, and biological activities of Cinnamomum zeylanicum.

    PubMed

    Jayaprakasha, G K; Rao, L Jagan Mohan

    2011-07-01

    The genus Cinnamomum comprises of several hundreds of species, which are distributed in Asia and Australia. Cinnamomum zeylanicum, the source of cinnamon bark and leaf oils, is an indigenous tree of Sri Lanka, although most oil now comes from cultivated areas. C. zeylanicum is an important spice and aromatic crop having wide applications in flavoring, perfumery, beverages, and medicines. Volatile oils from different parts of cinnamon such as leaves, bark, fruits, root bark, flowers, and buds have been isolated by hydro distillation/steam distillation and supercritical fluid extraction. The chemical compositions of the volatile oils have been identified by GC and GC-MS. More than 80 compounds were identified from different parts of cinnamon. The leaf oil has a major component called eugenol. Cinnamaldehyde and camphor have been reported to be the major components of volatile oils from stem bark and root bark, respectively. Trans-cinnamyl acetate was found to be the major compound in fruits, flowers, and fruit stalks. These volatile oils were found to exhibit antioxidant, antimicrobial, and antidiabetic activities. C. zeylanicum bark and fruits were found to contain proanthocyandins with doubly linked bis-flavan-3-ol units in the molecule. The present review provides a coherent presentation of scattered literature on the chemistry, biogenesis, and biological activities of cinnamon.

  15. Biology-oriented synthesis of a withanolide-inspired compound collection reveals novel modulators of hedgehog signaling.

    PubMed

    Švenda, Jakub; Sheremet, Michael; Kremer, Lea; Maier, Lukáš; Bauer, Jonathan O; Strohmann, Carsten; Ziegler, Slava; Kumar, Kamal; Waldmann, Herbert

    2015-05-04

    Biology-oriented synthesis employs the structural information encoded in complex natural products to guide the synthesis of compound collections enriched in bioactivity. The trans-hydrindane dehydro-δ-lactone motif defines the characteristic scaffold of the steroid-like withanolides, a plant-derived natural product class with a diverse pattern of bioactivity. A withanolide-inspired compound collection was synthesized by making use of three key intermediates that contain this characteristic framework derivatized with different reactive functional groups. Biological evaluation of the compound collection in cell-based assays that monitored biological signal-transduction processes revealed a novel class of Hedgehog signaling inhibitors that target the protein Smoothened.

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

    PubMed

    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.

  17. Effect of vanadium compounds on acid phosphatase activity.

    PubMed

    Vescina, C M; Sálice, V C; Cortizo, A M; Etcheverry, S B

    1996-01-01

    The direct effect of different vanadium compounds on acid phosphatase (ACP) activity was investigated. Vanadate and vanadyl but not pervanadate inhibited the wheat germ ACP activity. These vanadium derivatives did not alter the fibroblast Swiss 3T3 soluble fraction ACP activity. Using inhibitors of tyrosine phosphatases (PTPases), the wheat germ ACP was partially characterized as a PTPase. This study suggests that the inhibitory ability of different vanadium derivatives to modulate ACP activity seems to depend on the geometry around the vanadium atom more than on the oxidation state. Our results indicate a correlation between the PTPase activity and the sensitivity to vanadate and vanadyl cation.

  18. Nonexercise activity thermogenesis (NEAT): environment and biology.

    PubMed

    Levine, James A

    2004-05-01

    Nonexercise activity thermogenesis (NEAT) is the energy expended for everything that is not sleeping, eating, or sports-like exercise. It includes the energy expended walking to work, typing, performing yard work, undertaking agricultural tasks, and fidgeting. NEAT can be measured by one of two approaches. The first is to measure or estimate total NEAT. Here, total daily energy expenditure is measured, and from it "basal metabolic rate-plus-thermic effect of food" is subtracted. The second is the factoral approach, whereby the components of NEAT are quantified, and total NEAT is calculated by summing these components. The amount of NEAT that humans perform represents the product of the amount and types of physical activities and the thermogenic cost of each activity. The factors that impact a human's NEAT are readily divisible into environmental factors, such as occupation or dwelling within a "concrete jungle," and biological factors such as weight, gender, and body composition. The combined impact of these factors explains the substantial variance in human NEAT. The variability in NEAT might be viewed as random, but human and animal data contradict this. It appears that changes in NEAT subtly accompany experimentally induced changes in energy balance and are important in the physiology of weight change. Inadequate modulation of NEAT plus a sedentary lifestyle may thus be important in obesity. It then becomes intriguing to dissect mechanistic studies that delineate how NEAT is regulated into neural, peripheral, and humoral factors. A scheme is described in this review in which NEAT corresponds to a carefully regulated "tank" of physical activity that is crucial for weight control.

  19. Voltammetric determination of ruthenium in the form of complexes with biologically active ligands

    SciTech Connect

    Medyantseva, E.P.; Budnikov, G.K.; Balakaeva, T.A.

    1992-02-10

    The interest in the analytical chemistry of ruthenium and its compounds has recently been increasing. Ruthenium compounds can be used an antitumor agents and in the treatment of tuberculosis and fungal infections. It has been suggested that there is a specific relationship between the reduction potentials of the compounds and their biological activity. Of greatest interest among the biologically active compounds are the compounds with nitrogen-containing heterocycles. In order to obtain information on the degree of oxidation of the central atom in the complexes and to select the optimum conditions for the determination of the mono- and bi-nuclear complexes of ruthenium compounds with biologically active ligands such as imidazole (Im), histidine (His), benzimidazole (BIm) and its methyl derivative [1,2(CH{sub 3}){sub 2} - BIm], benzohyroxamic acid (Bha), and 1-phenyl-2-methylamino-1-propanol or ephedrine (Eph) in the present work, the authors studied their electrochemical behavior at dropping mercury (dme) and a platinum electrodes. 6 refs., 1 fig., 2 tabs.

  20. HPLC Determination of Bioactive Sulfur Compounds, Amino Acids and Biogenic Amines in Biological Specimens.

    PubMed

    Francioso, Antonio; Fanelli, Sergio; Vigli, Daniele; Ricceri, Laura; Cavallaro, Rosaria A; Conrado, Alessia Baseggio; Fontana, Mario; D'Erme, Maria; Mosca, Luciana

    2017-01-01

    There is an increasing interest for analytical methods aimed to detect biological sulfur-containing amines, because of their involvement in human diseases and metabolic disorders. This work describes an improved HPLC method for the determination of sulfur containing amino acids and amines from different biological matrices. We optimized a pre-column derivatization procedure using dabsyl chloride, in which dabsylated products can be monitored spectrophotometrically at 460 nm. This method allows the simultaneous analysis of biogenic amines, amino acids and sulfo-amino compounds including carnosine, dopamine, epinephrine, glutathione, cysteine, taurine, lanthionine, and cystathionine in brain specimens, urines, plasma, and cell lysates. Moreover, the method is suitable for the study of physiological and non-physiological derivatives of taurine and glutathione such as hypotaurine, homotaurine, homocysteic acid and S-acetylglutathione. The present method displays good efficiency of derivatization, having the advantage to give rise to stable products compared to other derivatizing agents such as o-phthalaldehyde and dansyl chloride.With this method, we provide a tool to study sulfur cycle from a metabolic point of view in relation to the pattern of biological amino-compounds, allowing researchers to get a complete scenario of organic sulfur and amino metabolism in tissues and cells.

  1. Biological Activity and Electronic Structure of the Aflatoxins

    PubMed Central

    Heathcote, J. G.; Hibbert, J. R.

    1974-01-01

    In theoretical studies of aromatic hydrocarbons, Pullman and Pullman (1969) used the molecular orbital method to correlate electronic structure with biological activity. They suggested that the interaction between carcinogens and their molecular receptors must occur through the K region of the carcinogenic molecule and involve a strong chemical binding of the type of an addition reaction. In the present work the electronic structures of aflatoxins B1, G1, 4-20 dehydro B1 and of versicolorin A have been determined by the simple Hückel molecular orbital method using a computer, in order to see whether the correlation between electronic structure and biological activity is applicable to these compounds also. Calculations show that the 2-3 pi-bond, which has the highest bond order of the aflatoxin molecules, should be the most susceptible to electrophilic attack and is the most probable location of the K region. This is in agreement with the experimental observation of Dutton and Heathcote (1968) that aflatoxins B1 and G1 hydrate rapidly in dilute acid to the hydroxyaflatoxins B2a and G2a with an apparent total loss of carcinogenicity. The calculations also show that aflatoxins B1 G1 and M1 have no suitable site for an L region and this probably accounts for their highly carcinogenic nature. PMID:4850776

  2. Chemical Variability and Biological Activities of Eucalyptus spp. Essential Oils.

    PubMed

    Barbosa, Luiz Claudio Almeida; Filomeno, Claudinei Andrade; Teixeira, Robson Ricardo

    2016-12-07

    Many plant species produce mixtures of odorous and volatile compounds known as essential oils (EOs). These mixtures play important roles in Nature and have been utilized by mankind for different purposes, such as pharmaceuticals, agrochemicals, aromatherapy, and food flavorants. There are more than 3000 EOs reported in the literature, with approximately 300 in commercial use, including the EOs from Eucalyptus species. Most EOs from Eucalyptus species are rich in monoterpenes and many have found applications in pharmaceuticals, agrochemicals, food flavorants, and perfumes. Such applications are related to their diverse biological and organoleptic properties. In this study, we review the latest information concerning the chemical composition and biological activities of EOs from different species of Eucalyptus. Among the 900 species and subspecies of the Eucalyptus genus, we examined 68 species. The studies associated with these species were conducted in 27 countries. We have focused on the antimicrobial, acaricidal, insecticidal and herbicidal activities, hoping that such information will contribute to the development of research in this field. It is also intended that the information described in this study can be useful in the rationalization of the use of Eucalyptus EOs as components for pharmaceutical and agrochemical applications as well as food preservatives and flavorants.

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

    PubMed

    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. Synthesis, characterization and biological activities of curcumin nanospheres.

    PubMed

    Arunraj, T R; Sanoj Rejinold, N; Mangalathillam, Sabitha; Saroj, Soumya; Biswas, Raja; Jayakumar, R

    2014-02-01

    Curcumin is one of the most versatile compounds obtained from Curcuma longa. The major obstacle in the therapeutic use of curcumin is its aqueous solubility. To enhance its aqueous solubility and biological activities, we prepared curcumin nanospheres (CNSs) by wet milling-solvent evaporation technique without any surfactants. In this study, we have focused on the synthesis, characterization and biological effects of CNSs. DLS and SEM analyses showed 50-80 nm spherical shaped CNSs with a zeta potential of -31.65 mV. FTIR revealed that there were no structural changes to CNSs. Antibacterial and antifungal studies proved that CNSs were much more effective than curcumin against Escherichia coil, Staphylococcus aureus and Candida albicans. Antioxidant activity of CNSs showed promising result for therapeutic applications. The in vitro anti-inflammatory studies proved that CNSs possessed enhanced anti-inflammatory effect against protein denaturation. Cytotoxicity and uptake of CNSs showed more toxicity on cancer cells (T47D, MG63, A375) sparing normal HDF and IEC cell lines. Skin permeation studies showed CNSs retained at different layers of pig skin. These results give clear evidence for their use against microbial and fungal skin infections as well as cancer treatment.

  5. Some biologically active oxovanadium(IV) complexes of triazole derived Schiff bases: their synthesis, characterization and biological properties.

    PubMed

    Chohan, Zahid H; Sumrra, Sajjad H

    2010-10-01

    A series of biologically active oxovanadium(IV) complexes of triazole derived Schiff bases L(1)-L(5) have been synthesized and characterized by their physical, analytical, and spectral data. The synthesized ligands potentially act as bidentate, in which the oxygen of furfural and nitrogen of azomethine coordinate with the oxovanadium atom to give a stoichiometry of vanadyl complexes 1:2 (M:L) in a square-pyramidal geometry. In vitro antibacterial and antifungal activities on different species of pathogenic bacteria (E. coli, S. flexneri, P. aeruginosa, S. typhi, S. aureus, and B. subtilis) and fungi (T. longifusus, C. albicans, A. flavus, M. canis, F. solani, and C. glabrata) have been studied. All compounds showed moderate to significant antibacterial activity against one or more bacterial strains and good antifungal activity against most of the fungal strains. The brine shrimp bioassay was also carried out to check the cytotoxicity of coordinated and uncoordinated synthesized compounds.

  6. Byrsonima fagifolia Niedenzu Apolar Compounds with Antitubercular Activity

    PubMed Central

    Higuchi, C. T.; Sannomiya, M.; Pavan, F. R.; Leite, S. R. A.; Sato, D. N.; Franzblau, S. G.; Sacramento, L. V. S.; Vilegas, W.; Leite, C. Q. F.

    2011-01-01

    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). PMID:19091782

  7. Compounds active against cell walls of medically important fungi.

    PubMed Central

    Hector, R F

    1993-01-01

    A number of substances that directly or indirectly affect the cell walls of fungi have been identified. Those that actively interfere with the synthesis or degradation of polysaccharide components share the property of being produced by soil microbes as secondary metabolites. Compounds specifically interfering with chitin or beta-glucan synthesis have proven effective in studies of preclinical models of mycoses, though they appear to have a restricted spectrum of coverage. Semisynthetic derivatives of some of the natural products have offered improvements in activity, toxicology, or pharmacokinetic behavior. Compounds which act on the cell wall indirectly or by a secondary mechanism of action, such as the azoles, act against diverse fungi but are usually fungistatic in nature. Overall, these compounds are attractive candidates for further development. PMID:8457977

  8. Dynamic properties of biologically active synthetic heparin-like hexasaccharides.

    PubMed

    Angulo, Jesús; Hricovíni, Milos; Gairi, Margarida; Guerrini, Marco; de Paz, José Luis; Ojeda, Rafael; Martín-Lomas, Manuel; Nieto, Pedro M

    2005-10-01

    A complete study of the dynamics of two synthetic heparin-like hexasaccharides, D-GlcNHSO3-6-SO4-alpha-(1-->4)-L-IdoA-2-SO4-alpha-(1-->4)-D-GlcNHSO3-6-SO4-alpha-(1-->4)-L-IdoA-2-SO4-alpha-(1-->4)-D-GlcNHSO3-6-SO4-alpha-(1-->4)-L-IdoA-2-SO4-alpha-1-->iPr (1) and -->4)-L-IdoA-2-SO4-alpha-(1-->4)-D-GlcNHAc-6-SO4-alpha-(1-->4)-L-IdoA-alpha-(1-->4)-D-GlcNHSO3-alpha-(1-->4)-L-IdoA-2-SO4-alpha-1-->iPr (2), has been performed using 13C-nuclear magnetic resonance (NMR) relaxation parameters, T1, T2, and heteronuclear nuclear Overhauser effect (NOEs). Compound 1 is constituted from sequences corresponding to the major polysaccharide heparin region, while compound 2 contains a sequence never found in natural heparin. They differ from each other only in sulphation patterns, and are capable of stimulating fibroblast growth factors (FGFs)-1 induced mitogenesis. Both oligosaccharides exhibit a remarkable anisotropic overall motion in solution as revealed by their anisotropic ratios (tau /tau||), 4.0 and 3.0 respectively. This is a characteristic behaviour of natural glycosaminoglycans (GAG) which has also been observed for the antithrombin (AT) binding pentasaccharide D-GlcNHSO3-6-SO4-alpha-(1-->4)-D-GlcA-beta-(1-->4)-D-GlcNHSO3-(3,6-SO4)-alpha-(1-->4)-L-IdoA-2-SO4-alpha-(1-->4)-D-GlcNHSO3-6-SO4-alpha-1-->Me (3) (Hricovíni, M., Guerrini, M., Torri, G., Piani, S., and Ungarelli, F. (1995) Conformational analysis of heparin epoxide in aqueous solution. An NMR relaxation study. Carbohydr. Res., 277, 11-23). The motional properties observed for 1 and 2 provide additional support to the suitability of these compounds as heparin models in agreement with previous structural (de Paz, J.L., Angulo, J., Lassaletta, J.M., Nieto, P.M., Redondo-Horcajo, M., Lozano, R.M., Jiménez-Gallego, G., and Martín-Lomas, M. (2001) The activation of fibroblast growth factors by heparin: synthesis, structure and biological activity of heparin-like oligosaccharides. Chembiochem, 2, 673-685; Ojeda, R

  9. Phytochemicals from Mangifera pajang Kosterm and their biological activities.

    PubMed

    Ahmad, Sadikah; Sukari, Mohd Aspollah; Ismail, Nurussaadah; Ismail, Intan Safinar; Abdul, Ahmad Bustamam; Abu Bakar, Mohd Fadzelly; Kifli, Nurolaini; Ee, Gwendoline C L

    2015-03-26

    Mangifera pajang Kosterm is a plant species from the mango family (Anacardiaceae). The fruits are edible and have been reported to have high antioxidant content. However, the detailed phytochemical studies of the plant have not been reported previously. This study investigates the phytochemicals and biological activities of different parts of Mangifera pajang. The plant samples were extracted with solvents of different polarity to obtain the crude extracts. The isolated compounds were characterized using spectroscopic methods. The extracts and isolated compounds were subjected to cytotoxicity tests using human breast cancer (MCF-7), human cervical cancer (HeLa) and human colon cancer (HT-29) cells. The free radical scavenging activity test was conducted using the DPPH assay. Antimicrobial activity tests were carried out by using the disc diffusion method. Phytochemical investigation on the kernel, stem bark and leaves of Mangifera pajang led to the isolation of methyl gallate (1), mixture of benzaldehyde (2) and benzyl alcohol (3), mangiferonic acid (4), 3β-hydroxy-cycloart-24-ene-26-oic acid (5), 3β,23-dihydroxy-cycloart-24-ene-26-oic acid (6), lupeol(7) lupenone(8), β-sitosterol(9), stigmasterol(10), trans-sobrerol(11) and quercitrin (12). Crude ethyl acetate and methanol extracts from the kernel indicated strong cytotoxic activity towards MCF-7 and HeLa cells with IC50 values of less than 10 μg/mL, while petroleum ether, chloroform and ethyl acetate extracts of the stem bark showed strong to moderate activity against MCF-7, HeLa and HT-29 cancer cell lines with IC50 values ranging from 5 to 30 μg/mL. As for the antimicrobial assays, only the ethyl acetate and methanol extracts from the kernel displayed some inhibition against the microbes in the antibacterial assays. The kernel extracts showed highest free radical scavenging activity with IC50 values of less than 10 μg/mL, while the ethyl acetate and methanol extracts of leaves displayed only weak

  10. Potential roles of chemical degradation in the biological activities of curcumin.

    PubMed

    Zhu, Julia; Sanidad, Katherine Z; Sukamtoh, Elvira; Zhang, Guodong

    2017-03-22

    Substantial pre-clinical and human studies have shown that curcumin, a dietary compound from turmeric, has a variety of health-promoting biological activities. A better understanding of the biochemical mechanisms for the health-promoting effects of curcumin could facilitate the development of effective strategies for disease prevention. Recent studies have shown that in aqueous buffer, curcumin rapidly degrades and leads to formation of various degradation products. In this review, we summarized and discussed the biological activities of chemical degradation products of curcumin, including alkaline hydrolysis products (such as ferulic acid, vanillin, ferulaldehyde, and feruloyl methane), and autoxidation products (such as bicyclopentadione). Though many of these degradation products are biologically active, they are substantially less-active compared to curcumin, supporting that chemical degradation has a limited contribution to the biological activities of curcumin.

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

    PubMed

    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. Copyright © 2015 John Wiley & Sons, Ltd.

  12. Design, synthesis, and biological activity of oxime ether strobilurin derivatives containing indole moiety as novel fungicide.

    PubMed

    Xie, Ya-Qiang; Huang, Zi-Long; Yan, Hui-Dong; Li, Jun; Ye, Li-Yi; Che, Li-Ming; Tu, Song

    2015-06-01

    Twenty-one novel oxime ether strobilurins containing indole moiety, which employed an indole group to stabilize the E-styryl group in Enoxastrobin, were designed and synthesized. The biological assay indicated that most compounds exhibited potent fungicidal activities. The structure-activity relationship study demonstrated that the synthesized methyl 3-methoxypropenoate oxime ethers 7b-e exhibited remarkably high activities among all the synthesized oxime ether compounds 7. Moreover, the fungicidal activities of methyl α-(methoxyimino)benzeneacetate oxime ethers compounds 7f-i and N-methoxy-carbamic acid methyl esters compounds 7j-m showed significant differences compared to the corresponding products of ammonolysis. © 2014 John Wiley & Sons A/S.

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

    NASA Technical Reports Server (NTRS)

    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.

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

    PubMed Central

    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

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

    PubMed

    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.

  16. Antibacterial activity of phenolic compounds against the phytopathogen Xylella fastidiosa.

    PubMed

    Maddox, Christina E; Laur, Lisa M; Tian, Li

    2010-01-01

    Xylella fastidiosa is a pathogenic bacterium that causes diseases in many crop species, which leads to considerable economic loss. Phenolic compounds (a group of secondary metabolites) are widely distributed in plants and have shown to possess antimicrobial properties. The anti-Xylella activity of 12 phenolic compounds, representing phenolic acid, coumarin, stilbene and flavonoid, was evaluated using an in vitro agar dilution assay. Overall, these phenolic compounds were effective in inhibiting X. fastidiosa growth, as indicated by low minimum inhibitory concentrations (MICs). In addition, phenolic compounds with different structural features exhibited different anti-Xylella capacities. Particularly, catechol, caffeic acid and resveratrol showed strong anti-Xylella activities. Differential response to phenolic compounds was observed among X. fastidiosa strains isolated from grape and almond. Elucidation of secondary metabolite-based host resistance to X. fastidiosa will have broad implication in combating X. fastidiosa-caused plant diseases. It will facilitate future production of plants with improved disease resistance properties through genetic engineering or traditional breeding approaches and will significantly improve crop yield.

  17. Update on project determining biologically active compounds in milk

    USDA-ARS?s Scientific Manuscript database

    The added health value of raw and pasteurized milk from organic and grass-fed herds is strongly debated because of limited, and often conflicting, scientific data. The Dairy & Functional Foods Research Unit, USDA-ARS-NAA, Wyndmoor, PA has an ongoing project to identify and compare the levels of bio...

  18. Ligand Biological Activity Predictions Using Fingerprint-Based Artificial Neural Networks (FANN-QSAR)

    PubMed Central

    Myint, Kyaw Z.; Xie, Xiang-Qun

    2015-01-01

    This chapter focuses on the fingerprint-based artificial neural networks QSAR (FANN-QSAR) approach to predict biological activities of structurally diverse compounds. Three types of fingerprints, namely ECFP6, FP2, and MACCS, were used as inputs to train the FANN-QSAR models. The results were benchmarked against known 2D and 3D QSAR methods, and the derived models were used to predict cannabinoid (CB) ligand binding activities as a case study. In addition, the FANN-QSAR model was used as a virtual screening tool to search a large NCI compound database for lead cannabinoid compounds. We discovered several compounds with good CB2 binding affinities ranging from 6.70 nM to 3.75 μM. The studies proved that the FANN-QSAR method is a useful approach to predict bioactivities or properties of ligands and to find novel lead compounds for drug discovery research. PMID:25502380

  19. Glycoside vs. Aglycon: The Role of Glycosidic Residue in Biological Activity

    NASA Astrophysics Data System (ADS)

    Křen, Vladimír

    A large number of biologically active compounds are glycosides. Sometimes the glycosidic residue is crucial for their activity, in other cases glycosylation only improves pharmacokinetic parameters. Recent developments in molecular glycobiology brought better understanding of aglycon vs. glycoside activities, and made possible the development of new, more active or more effective glycodrugs based on these findings - a very illustrative recent example is vancomycin. The new enzymatic methodology "glycorandomization" enabled preparation of glycoside libraries and opened up paths to the preparation of optimized or entirely novel glycoside antibiotics. This chapter deals with an array of glycosidic compounds currently used in medicine but also covers the biological activity of some glycosidic metabolites of known drugs. The chapter discusses glycosides of vitamins, polyphenolic glycosides (flavonoids), alkaloid glycosides, glycosides of antibiotics, glycopeptides, cardiac glycosides, steroid and terpenoid glycosides etc. The physiological role of the glycosyl moiety and structure-activity relations (SAR) in the glycosidic moiety (-ies) are also discussed.

  20. [MALDI-TOF mass spectrometry in the investigation of large high-molecular biological compounds].

    PubMed

    Porubl'ova, L V; Rebriiev, A V; Hromovyĭ, T Iu; Minia, I I; Obolens'ka, M Iu

    2009-01-01

    MALDI-TOF (Matrix-Assisted Laser Desorption/Ionization Time-of-Flight) mass spectrometry has become, in the recent years, a tool of choice for analyses of biological polymers. The wide mass range, high accuracy, informativity and sensitivity make it a superior method for analysis of all kinds of high-molecular biological compounds including proteins, nucleic acids and lipids. MALDI-TOF-MS is particularly suitable for the identification of proteins by mass fingerprint or microsequencing. Therefore it has become an important technique of proteomics. Furthermore, the method allows making a detailed analysis of post-translational protein modifications, protein-protein and protein-nucleic acid interactions. Recently, the method was also successfully applied to nucleic acid sequencing as well as screening for mutations.

  1. SAMPLE EXTRACTION AND GC-MS ANALYSIS FOR POLAR VOLATILE ORGANIC COMPOUNDS (PVOCS) IN LIQUID BIOLOGICAL MEDIA

    EPA Science Inventory

    Current approaches for assessing the cumulative exposures and effects from broad classes of environmental stressors incorporate the measurement of specific groups of endogenous compounds in human biological fluids. Recent focus has been on interpreting patterns of differentially...

  2. SAMPLE EXTRACTION AND GC-MS ANALYSIS FOR POLAR VOLATILE ORGANIC COMPOUNDS (PVOCS) IN LIQUID BIOLOGICAL MEDIA

    EPA Science Inventory

    Current approaches for assessing the cumulative exposures and effects from broad classes of environmental stressors incorporate the measurement of specific groups of endogenous compounds in human biological fluids. Recent focus has been on interpreting patterns of differentially...

  3. Formation and emission of volatile polonium compound by microbial activity and polonium methylation with methylcobalamin.

    PubMed

    Momoshima, N; Song, L X; Osaki, S; Maeda, Y

    2001-07-15

    We observed biologically mediated emission of Po from culture solution inoculated sea sediment extract and incubated under natural light/dark cycle condition or dark condition the emitted Po compound would be lipophilic because of effective collection in organic solvent. Sterilization of the culture medium with antibiotics or CuSO4 completely suppressed growth of microorganisms and resulted in no emission of Po, indicating biological activity of microorganisms is responsible for formation and emission of volatile Po compound. Po emission also occurred when seawater was used as a culture medium. Our finding indicates a possibility of biotic source for atmospheric Po in the environment, which has been believed to be originated from abiotic sources. We compared emission behavior of Po and S in the culture experiments, the elements belong to XVI group in the Periodical Table, and consider that their emission mechanisms involved would be different though the emission of both elements is supported by biological activity of microorganisms. One of the chemical forms of S emitted was confirmed to be dimethyl sulfide (DMS) but that of Po is not known. Methylation experiments of Po with methylcobalamin demonstrated a formation and emission of volatile Po compound. The methylation of Po with methylcobalamin might be related to the observed Po emission in the culture experiments.

  4. BIOLOGICAL ACTIVITY OF GREEN TEA EXTRACTS.

    PubMed

    Lursmanashvili, L; Gulua, L; Turmanidze, T; Enukidze, M; Machavariani, M; Sanikidze, T

    2017-02-01

    The purpose of our study was to determine effects of green tea extracts on the Jurkat cells incubated under oxidative stress conditions. The research was conducted on leukemic human mature T cells (Jurkat cells). For the modelling of oxidative stress 30% hydrogen peroxide (H2O2) (Sigma) (10 μl, 25 μl 50 μl and 100 μl) was added to Jurkat cell suspension with subsequent incubation for 4, 6, 8 and 24 h. Control group was represented by intact Jurkat cells. The assessment of cells proliferation activity (viability) was performed by MTT test. The viability of Jurkat cells incubated for 24 hours under acquit oxidative stress conditions dose-depenently, monotonically decreased (irreversibly at 100 μM of H2O2 and reaches the 30% of intact Jurkat cells viability level at 50 μM of H2O2). Low doses of H2O2 (10 μl, 25 μl H2O2) revealed cytotoxicity only within short term (8 hours) of the incubation, afterward the viability of Jurkat cells monotonically increased and after 24 hours it reached 43% and 56% of control level, respectively. Vitamins C and E revealed cytotoxic effect on intact Jurkat cells, while the C+V vitamins complex induced 2-fold stimulation of Jurkat cells viability. Under a moderate oxidative stress condition (25 μl of H2O2) the complex of C + E vitamins revealed cytoprotective effect on Jurkat cells which may be related to ability of vitamin C to induce regeneration and to transform E vitamin tocopheroxyl free radicals into tocopherol. Green tea had no effect, green tea catechins revealed stimulatory effect, while green tea pectin - weak cytotoxic effect on intact Jurkat cells. Green tea and especially extracted catechins (but not pectin) revealed stimulatory effect on the viability of the Jurkat cells incubated under an oxidative stress condition. Our study results confirm the opinion that the natural compounds (green tea extracts) are harmless for normal cellular metabolism. Their differential effects on the "diseased", incubated under an

  5. Natural compounds with aromatase inhibitory activity: an update.

    PubMed

    Balunas, Marcy J; Kinghorn, A Douglas

    2010-08-01

    Several synthetic aromatase inhibitors are currently in clinical use for the treatment of postmenopausal women with hormone-receptor positive breast cancer. However, these treatments may lead to untoward side effects and so the search for new aromatase inhibitors continues, especially those for which the activity is promoter-specific, targeting the breast-specific promoters I.3 and II. Recently, numerous natural compounds have been found to inhibit aromatase in noncellular, cellular, and IN VIVO studies. These investigations, covering the last two years, as well as additional studies that have focused on the evaluation of natural compounds as promoter-specific aromatase inhibitors or as aromatase inducers, are described in this review.

  6. Prioritizing testing of organic compounds detected as gas phase air pollutants: structure-activity study for human contact allergens.

    PubMed Central

    Johnson, R; Macina, O T; Graham, C; Rosenkranz, H S; Cass, G R; Karol, M H

    1997-01-01

    Organic compounds that are used or generated anthropogenically in large quantities in cities can be identified through their presence in the urban atmosphere and in air pollutant source emissions. Compounds identified by this method were screened to evaluate their potential to act as contact allergens. The CASE and MULTICASE computer programs, which are based on the detection of structure-activity relationships (SAR), were used to evaluate this potential. These relationships first are determined by comparing chemical structures to biological activity within a learning set comprised of 458 compounds, each of which had been tested experimentally in human trials for its sensitization potential. Using the information contained in this learning set, CASE and MULTICASE predicted the activity of 238 compounds found in the atmosphere for their ability to act as contact allergens. The analysis finds that 21 of 238 compounds are predicted to be active contact allergens (probability >0.5), with potencies ranging from mild to very strong. The compounds come from chemical classes that include chlorinated aromatics and chlorinated hydrocarbons, N-containing compounds, phenols, alkenes, and an S-containing compound. Using the measured airborne concentrations or emission rates of these compounds as an indication of the extent of their use, together with their predicted potencies, provides an efficient method to prioritize the experimental assessment of contact sensitization of untested organic compounds that can be detected as air pollutants. Images Figure 1. PMID:9300925

  7. Prioritizing testing of organic compounds detected as gas phase air pollutants: structure-activity study for human contact allergens.

    PubMed

    Johnson, R; Macina, O T; Graham, C; Rosenkranz, H S; Cass, G R; Karol, M H

    1997-09-01

    Organic compounds that are used or generated anthropogenically in large quantities in cities can be identified through their presence in the urban atmosphere and in air pollutant source emissions. Compounds identified by this method were screened to evaluate their potential to act as contact allergens. The CASE and MULTICASE computer programs, which are based on the detection of structure-activity relationships (SAR), were used to evaluate this potential. These relationships first are determined by comparing chemical structures to biological activity within a learning set comprised of 458 compounds, each of which had been tested experimentally in human trials for its sensitization potential. Using the information contained in this learning set, CASE and MULTICASE predicted the activity of 238 compounds found in the atmosphere for their ability to act as contact allergens. The analysis finds that 21 of 238 compounds are predicted to be active contact allergens (probability >0.5), with potencies ranging from mild to very strong. The compounds come from chemical classes that include chlorinated aromatics and chlorinated hydrocarbons, N-containing compounds, phenols, alkenes, and an S-containing compound. Using the measured airborne concentrations or emission rates of these compounds as an indication of the extent of their use, together with their predicted potencies, provides an efficient method to prioritize the experimental assessment of contact sensitization of untested organic compounds that can be detected as air pollutants.

  8. Biological Activity and Phytochemical Study of Scutellaria platystegia

    PubMed Central

    Madani mousavi, Seyedeh Neda; Delazar, Abbas; Nazemiyeh, Hossein; Khodaie, Laleh

    2015-01-01

    This study aimed to determine biological activity and phytochemical study of Scutellaria platystegia (family Labiatae). Methanolic (MeOH) extract of aerial parts of S. platystegia and SPE fractions of methanolic extract (specially 20% and 40% methanolic fractions), growing in East-Azarbaijan province of Iran were found to have radical scavenging activity by DPPH (2, 2-diphenyl -1- pycryl hydrazyl) assay. Dichloromethane (DCM) extract of this plant exhibited animalarial activity by cell free method providing IC50 at 1.1876 mg/mL. Crude extracts did not exhibit any toxicity assessed by brine shrimp lethality assay. Phytochemical study of methanolic extract by using reverse phase HPLC method and NMR instrument for isolation and identification of pure compounds respectively, yielded 2-(4- hydroxy phenyl) ethyl-O-β-D- glucopyranoside from 10% and apigenin 7-O-glucoside, verbascoside and martynoside from 40% SPE fraction. Occurance of verbascoside and martynoside as biochemical markers appeared to be widespread in this genus. Antioxidant and antimalarial activity of MeOH and DCM extracts, respectively, as well as no general toxicity of them could provide a basis for further in-vitro and in-vivo studies and clinical trials to develop new therapeutical alternatives. PMID:25561927

  9. Biological and Nonbiological Antioxidant Activity of Some Essential Oils.

    PubMed

    Pérez-Rosés, Renato; Risco, Ester; Vila, Roser; Peñalver, Pedro; Cañigueral, Salvador

    2016-06-15

    Fifteen essential oils, four essential oil fractions, and three pure compounds (thymol, carvacrol, and eugenol), characterized by gas chromatography and gas chromatography-mass spectrometry, were investigated for biological and nonbiological antioxidant activity. Clove oil and eugenol showed strong DPPH (2,2-diphenyl-1-picrylhydrazyl) free-radical scavenging activity (IC50 = 13.2 μg/mL and 11.7 μg/mL, respectively) and powerfully inhibited reactive oxygen species (ROS) production in human neutrophils stimulated by PMA (phorbol 12-myristate 13-acetate) (IC50 = 7.5 μg/mL and 1.6 μg/mL) or H2O2 (IC50 = 22.6 μg/mL and 27.1 μg/mL). Nutmeg, ginger, and palmarosa oils were also highly active on this test. Essential oils from clove and ginger, as well as eugenol, carvacrol, and bornyl acetate inhibited NO (nitric oxide) production (IC50 < 50.0 μg/mL). The oils of clove, red thyme, and Spanish oregano, together with eugenol, thymol, and carvacrol showed the highest myeloperoxidase inhibitory activity. Isomers carvacrol and thymol displayed a disparate behavior in some tests. All in all, clove oil and eugenol offered the best antioxidant profile.

  10. Biologically active peptides: prospects for drug development.

    PubMed

    Hughes, J

    1980-08-11

    Biologically active peptides aree typified by their unbiquity of distribution, their high receptor affinity and an almost infinite diversity of structure. For these reasons, considerable effort is now being expended to elucidate the possible role of peptides in brain function. This effort has been stimulated by the discovery of a number of new endogenous peptides, such as the enkephalins, endorphins, vasoactive intestinal peptide and neurotensin. At present, there is no clearly defined role for these peptides, although they may form an important basis for the chemical coding of various brain functions, including pain, mood and memory. At present, the potential for drug development of peptide agonists remains in fairly circumscribed areas such as analgesia, pituitary hormone control, and gastrointestinal motor and secretory control. Peptide antagonists may provide a vast field for future development, although only one area, that of antifertility drugs based on LHRH antagonists, shows any promise of immediate success. Industrial research approaches to new peptide agonists and antagonists mainly rely at present on rational drug design through structural analogies. Other fruitful approaches to be considered are the screening of natural microbial and plant products and the possible application of genetic engineering techniques.

  11. Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment.

    PubMed

    Andrews, Katherine T; Fisher, Gillian M; Sumanadasa, Subathdrage D M; Skinner-Adams, Tina; Moeker, Janina; Lopez, Marie; Poulsen, Sally-Ann

    2013-11-15

    Despite the urgent need for effective antimalarial drugs with novel modes of action no new chemical class of antimalarial drug has been approved for use since 1996. To address this, we have used a rational approach to investigate compounds comprising the primary benzene sulfonamide fragment as a potential new antimalarial chemotype. We report the in vitro activity against Plasmodium falciparum drug sensitive (3D7) and resistant (Dd2) parasites for a panel of fourteen primary benzene sulfonamide compounds. Our findings provide a platform to support the further evaluation of primary benzene sulfonamides as a new antimalarial chemotype, including the identification of the target of these compounds in the parasite. Copyright © 2013 Elsevier Ltd. All rights reserved.

  12. Synthesis and antitumor activity of natural compound aloe emodin derivatives.

    PubMed

    Thimmegowda, Naraganahalli R; Park, Chanmi; Shwetha, Bettaswamigowda; Sakchaisri, Krisada; Liu, Kangdong; Hwang, Joonsung; Lee, Sangku; Jeong, Sook J; Soung, Nak K; Jang, Jae H; Ryoo, In-Ja; Ahn, Jong S; Erikson, Raymond L; Kim, Bo Y

    2015-05-01

    In this study, we have synthesized novel water soluble derivatives of natural compound aloe emodin 4(a-j) by coupling with various amino acid esters and substituted aromatic amines, in an attempt to improve the anticancer activity and to explore the structure-activity relationships. The structures of the compounds were determined by (1) H NMR and mass spectroscopy. Cell growth inhibition assays revealed that the aloe emodin derivatives 4d, 4f, and 4i effectively decreased the growth of HepG2 (human liver cancer cells) and NCI-H460 (human lung cancer cells) and some of the derivatives exhibited comparable antitumor activity against HeLa (Human epithelial carcinoma cells) and PC3 (prostate cancer cells) cell lines compared to that of the parent aloe emodin at low micromolar concentrations.

  13. Antioxidant activity of compounds from the medicinal herb Aster tataricus.

    PubMed

    Ng, T B; Liu, Fang; Lu, Yanhua; Cheng, C H K; Wang, Zhengtao

    2003-10-01

    A number of compounds were isolated from the medicinal plant Aster tataricus including shionone, epifriedelinol, quercetin, kaempferol, scopoletin, emodin, aurantiamide acetate and 1,7-dihydroxy-6-methyl-anthraquinone. The compounds were compared with regard to their ability in inhibiting hemolysis of rat erythrocytes induced by 2'-2' azobis (2-amidinopropane) dihydrochloride, lipid peroxidation using the FeSO(4)-ascorbic acid system, and generation of superoxide radicals using a phenazine methosulfate-nicotinamide adenine dinucleotide system. The effects on the Fe-bleomycin-induced DNA damage reflected pro-oxidant activity. Quercetin and kaempferol were most potent in inhibiting hemolysis, lipid peroxidation and superoxide radical generation. Scopoletin and emodin were similar to quercetin and kaempferol in inhibiting superoxide radical generation and second to them in inhibiting lipid peroxidation. Aurantiamide acetate exhibited some inhibitory activity toward superoxide radical generation. 1,7-dihydroxy-6-methyl-anthraquinone exerted an inhibitory activity only on superoxide radical generation. Shionone and epifriedelinol did not display any antioxidant activity. Quercetin and kaempferol, but not the remaining compounds, exhibited some pro-oxidant activity.

  14. Anti-cancer activity of compounds from Bauhinia strychnifolia stem.

    PubMed

    Yuenyongsawad, Supreeya; Bunluepuech, Kingkan; Wattanapiromsakul, Chatchai; Tewtrakul, Supinya

    2013-11-25

    The stem and root of Bauhinia strychnifolia Craib (Fabaceae family) have been traditionally used in Thailand to treat fever, alcoholic toxication, allergy and cancer. An EtOH extract of Bauhinia strychnifolia showed good inhibitory activity against several cancer cell lines including HT-29, HeLa, MCF-7 and KB. As there has been no previous reports on chemical constituents of Bauhinia strychnifolia, this study is aimed to isolate the pure compounds with anti-cancer activity. Five pure compounds were isolated from EtOH extract of Bauhinia strychnifolia stem using silica gel, dianion HP-20 and sephadex LH-20 column chromatography and were tested for their cytotoxic effects against HT-29, HeLa, MCF-7 and KB cell lines using the Sulforhodamine B (SRB) assay. Among five compounds, 3,5,7,3',5'-pentahydroxyflavanonol-3-O-α-l-rhamnopyranoside (2) possessed very potent activity against KB (IC₅₀=0.00054μg/mL), HT-29 (IC₅₀=0.00217 μg/mL), MCF-7 (IC₅₀=0.0585 μg/mL) and HeLa cells (IC₅₀=0.0692 μg/mL). 3,5,7-Trihydroxychromone-3-O-α-l-rhamnopyranoside (3) also showed good activity against HT-29 (IC₅₀=0.02366 μg/mL), KB (IC₅₀=0.0412 μg/mL) and MCF-7 (IC₅₀=0.297 μg/mL), respectively. The activity of 2 (IC₅₀=0.00054 μg/mL) against KB cell was ten times higher than that of the positive control, Camptothecin (anti-cancer drug, IC₅₀=0.0057 μg/mL). All compounds did not show any cytotoxicity with normal cells at the concentration of 1 μg/mL. This is the first report of compounds 2 and 3 on anti-cancer activity and based on the anti-cancer activity of extracts and pure compounds isolated from Bauhinia strychnifolia stem, it might be suggested that this plant could be useful for treatment of cancer. © 2013 Elsevier Ireland Ltd. All rights reserved.

  15. [Advances in studies on chemical constituents and biological activities of Lawsonia inermis].

    PubMed

    Li, Qian; Gao, Wen-Qin; Zhao, Yu-Qing

    2013-03-01

    Lawsonia inermis is a single-species genus of the Lythraceae family, its leaves, stem bark, roots, flowers and seeds have been used in traditional medicine. It has been paid more attention by scholars from many countries because of their various types of compounds and significant physiological activities. The plant is reported to contain quinones, phenylpropanoids, flavonoids, terpenoids, phenolic compounds and fatty acids. Modern pharmacological studies have demonstrated that the plant performs antimicrobial, antioxidant, anticancer and antiparasitic activity. This article mainly summarizes the research advances of chemical constituents and biological activities of Lawsonia inermis, for its further development and utilization.

  16. Hybrid energy storage systems utilizing redox active organic compounds

    DOEpatents

    Wang, Wei; Xu, Wu; Li, Liyu; Yang, Zhenguo

    2015-09-08

    Redox flow batteries (RFB) have attracted considerable interest due to their ability to store large amounts of power and energy. Non-aqueous energy storage systems that utilize at least some aspects of RFB systems are attractive because they can offer an expansion of the operating potential window, which can improve on the system energy and power densities. One example of such systems has a separator separating first and second electrodes. The first electrode includes a first current collector and volume containing a first active material. The second electrode includes a second current collector and volume containing a second active material. During operation, the first source provides a flow of first active material to the first volume. The first active material includes a redox active organic compound dissolved in a non-aqueous, liquid electrolyte and the second active material includes a redox active metal.

  17. Two new compounds from Atractylodes macrocephala with neuroprotective activity.

    PubMed

    Zhang, Na; Liu, Chao; Sun, Tie-Min; Ran, Xiao-Ku; Kang, Ting-Guo; Dou, De-Qiang

    2017-01-01

    In the present study, two new compounds, together with six known compounds, were isolated from rhizome of Atractylodes macrocephala Koidz by a series of silica gel, ODS column chromatography, and preparative HPLC. Their structures were characterized as atractylenolide II (1), atractylenolide I (2), biepiasterolid (3), isoatractylenolide I (4), atractylenolide III (5), 3β-acetoxyl atractylenolide I (6), (4E,6E,12E)-tetradeca-4,6,12-triene-8,10-diyne-13,14-triol (7), (3S,4E,6E,12E)-1-acetoxy-tetradeca-4,6,12-triene-8,10-diyne-3,14-diol (8) on the basis of 1D, 2D NMR, and circular dichroism analyses. Among them, compounds 6 and 8 were novel compounds. In addition, their neuroprotective activity against MPP(+)-induced SH-SY5Y cells was evaluated by MTT colorimetry. The results showed that all these compounds have definite protective effect on MPP(+)-induced SH-SY5Y cells.

  18. Diastereoselective Synthesis of Biologically Active Cyclopenta[b]indoles.

    PubMed

    Santos, Marilia S; Fernandes, Daniara C; Rodrigues, Manoel T; Regiani, Thais; Andricopulo, Adriano D; Ruiz, Ana Lúcia T G; Vendramini-Costa, Débora B; de Carvalho, João E; Eberlin, Marcos N; Coelho, Fernando

    2016-08-05

    The cyclopenta[b]indole motif is present in several natural and synthetic biologically active compounds, being directly responsible for the biological effects some of them present. We described herein a three step sequence for the synthesis of cyclopenta[b]indoles with a great structural diversity. The method is based on an oxidative Michael addition of suitable indoles on the double bond of Morita-Baylis-Hillman adducts mediated by a hypervalent iodine reagent (IBX) to form β-ketoesters, which were chemoselectively reduced with NaBH4 in THF to give the corresponding β-hydroxy-esters. The diastereoisomeric mixture was then treated with a catalytic amount of triflic acid (20 mol %) to give cyclopenta[b]indoles with overall yields ranging from 8 to 73% (for 2 steps). The acid-catalyzed cyclization step gave the required heterocycles, via an intramolecular Friedel-Crafts reaction, with high diastereoselectivity, where only the trans product was observed. A mechanistic study monitored by ESI-(+)-MS was also conducted to collect evidence about the mechanism of this reaction. The new molecules herein synthesized were also evaluated against a panel of human cancer cells demonstrating a promising antitumoral profile.

  19. Interesting biological activities from plants traditionally used by Native Australians.

    PubMed

    Pennacchio, Marcello; Kemp, Annabeth S; Taylor, Rory P; Wickens, Kristen M; Kienow, Lucie

    2005-01-15

    Four plants routinely used for medicinal purposes by Native Australians were screened for various biological activities. Methanol extracts of Eremophila maculata, Acacia auriculoformis and Acacia bivenosa exhibited antibiotic effects, while Eremophila alternifolia yielded an extract that induced significant changes to the heart activity of spontaneously hypertensive rats. We report on these biological activities.

  20. KNApSAcK Metabolite Activity Database for retrieving the relationships between metabolites and biological activities.

    PubMed

    Nakamura, Yukiko; Afendi, Farit Mochamad; Parvin, Aziza Kawsar; Ono, Naoaki; Tanaka, Ken; Hirai Morita, Aki; Sato, Tetsuo; Sugiura, Tadao; Altaf-Ul-Amin, Md; Kanaya, Shigehiko

    2014-01-01

    Databases (DBs) are required by various omics fields because the volume of molecular biology data is increasing rapidly. In this study, we provide instructions for users and describe the current status of our metabolite activity DB. To facilitate a comprehensive understanding of the interactions between the metabolites of organisms and the chemical-level contribution of metabolites to human health, we constructed a metabolite activity DB known as the KNApSAcK Metabolite Activity DB. It comprises 9,584 triplet relationships (metabolite-biological activity-target species), including 2,356 metabolites, 140 activity categories, 2,963 specific descriptions of biological activities and 778 target species. Approximately 46% of the activities described in the DB are related to chemical ecology, most of which are attributed to antimicrobial agents and plant growth regulators. The majority of the metabolites with antimicrobial activities are flavonoids and phenylpropanoids. The metabolites with plant growth regulatory effects include plant hormones. Over half of the DB contents are related to human health care and medicine. The five largest groups are toxins, anticancer agents, nervous system agents, cardiovascular agents and non-therapeutic agents, such as flavors and fragrances. The KNApSAcK Metabolite Activity DB is integrated within the KNApSAcK Family DBs to facilitate further systematized research in various omics fields, especially metabolomics, nutrigenomics and foodomics. The KNApSAcK Metabolite Activity DB could also be utilized for developing novel drugs and materials, as well as for identifying viable drug resources and other useful compounds.

  1. Anti-allergic inflammatory activities of compounds of amomi fructus.

    PubMed

    Choi, Hyun Gyu; Je, In-Gyu; Kim, Geum Jin; Choi, Hyukjae; Kim, Sang Hyun; Kim, Jeong Ah; Lee, Kim Seung Ho

    2015-04-01

    Activity-guided isolation of compounds from the fruits of Amomum xanthioides resulted in the purification of fourteen phenolic compounds, 4-hydroxy-benzaldehyde (1), 3,4-dihydroxybenzaldehyde (2), 3,5-dimethoxy-4-methylbenzaldehyde (3), syringic aldehyde (4), benzoic acid (5), 3,4-dihydroxy benzoic acid (6), vanillic acid (7), 3-hydroxy-2-methoxybenzoic acid (8), o-vanillic acid (9), phenylacetic acid (10), tyrosol (11), pyrocatechol (12), 1,2,4,5-tetramethoxybenzene (13), and 3,3',5,5'-tetramethoxybiphenyl-4,4'-diol (14). To evaluate the anti-allergic inflammatory activities of these compounds, we examined the inhibitory effects of the isolates (1-14) on histamine release and on the expressions of tumor necrosis factor (TNF)-ca and interleukin (IL)-6 genes by using human mast cells. Of the tested compounds, 9, 11, and 13 suppressed histamine release from mast cells, and all isolates attenuated the expressions of the pro-inflammatory cytokines, TNF-α and IL-6 genes in human mast cells.

  2. Biological activities and potential health benefits of bioactive peptides derived from marine organisms.

    PubMed

    Ngo, Dai-Hung; Vo, Thanh-Sang; Ngo, Dai-Nghiep; Wijesekara, Isuru; Kim, Se-Kwon

    2012-11-01

    Marine organisms have been recognized as rich sources of bioactive compounds with valuable nutraceutical and pharmaceutical potentials. Recently, marine bioactive peptides have gained much attention because of their numerous health beneficial effects. Notably, these peptides exhibit various biological activities such as antioxidant, anti-hypertensive, anti-human immunodeficiency virus, anti-proliferative, anticoagulant, calcium-binding, anti-obesity and anti-diabetic activities. This review mainly presents biological activities of peptides from marine organisms and emphasizing their potential applications in foods as well as pharmaceutical areas.

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

    PubMed Central

    Mondol, Muhammad Abdul Mojid; Shin, Hee Jae; Islam, Mohammad Tofazzal

    2013-01-01

    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. PMID:23941823

  4. Office of Biological Informatics and Outreach geospatial technology activities

    USGS Publications Warehouse

    ,

    1998-01-01

    The U.S. Geological Survey (USGS) Office of Biological Informatics and Outreach (OBIO) in Reston, Virginia, and its Center for Biological Informatics (CBI) in Denver, Colorado, provide leadership in the development and use of geospatial technologies to advance the Nation's biological science activities.

  5. 40 CFR Table 36 to Subpart G of... - Compound Lists Used for Compliance Demonstrations for Enhanced Biological Treatment Processes...

    Code of Federal Regulations, 2013 CFR

    2013-07-01

    ... Demonstrations for Enhanced Biological Treatment Processes (See § 63.145(h)) 36 Table 36 to Subpart G of Part 63... Vents, Storage Vessels, Transfer Operations, and Wastewater Pt. 63, Subpt. G, Table 36 Table 36 to Subpart G of Part 63—Compound Lists Used for Compliance Demonstrations for Enhanced Biological...

  6. 40 CFR Table 36 to Subpart G of... - Compound Lists Used for Compliance Demonstrations for Enhanced Biological Treatment Processes...

    Code of Federal Regulations, 2012 CFR

    2012-07-01

    ... Demonstrations for Enhanced Biological Treatment Processes (See § 63.145(h)) 36 Table 36 to Subpart G of Part 63... Vents, Storage Vessels, Transfer Operations, and Wastewater Pt. 63, Subpt. G, Table 36 Table 36 to Subpart G of Part 63—Compound Lists Used for Compliance Demonstrations for Enhanced Biological...

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

    PubMed Central

    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. PMID:26150810

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

    PubMed

    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.

  9. Study of the interaction between indole-based compounds and biologically relevant G-quadruplexes.

    PubMed

    Carvalho, Josué; Nottelet, Pierre; Mergny, Jean-Louis; Queiroz, João A; Salgado, Gilmar F; Cruz, Carla

    2017-04-01

    G-quadruplexes (G4s) are high-order secondary structures that modulate several key cell processes such as telomere function, gene expression and DNA replication. In the past years G4s have emerged as promising targets for drug development due to the discovery of small molecules which bind and stabilize these structures. In this work, we report the synthesis of indole-based compounds and the study of their interaction with the biological relevant G4s c-MYC and human telomeric repeat 22AG using several biophysical techniques. The ligands are G4 specific and they can discriminate different G4 structures namely parallel and hybrid-1 topologies. The NMR study of interaction between the most promising indole-derivative (compound 3) and c-MYC quadruplex suggests that the ligand binds on the external tetrads with additional actions in the loops/grooves in a 2:1 ratio. The molecular docking calculations of compound 3 to c-MYC quadruplex corroborates with the (1)H and NOESY NMR studies. Overall, the results suggest that indole-based ligands are promising candidates for future lead optimizations in drug development.

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

    PubMed

    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.

  11. Lung biological activity of American attapulgite

    SciTech Connect

    Begin, R.; Masse, S.; Rola-Pleszczynski, M.; Geoffroy, M.; Martel, M.; Desmarais, Y.; Sebastien, P.

    1987-04-01

    Attapulgite is a fibrous mineral industrially consumed at the rate of over a million tons per year but the biological activity of the material is not fully known. To evaluate the in vivo toxicity of the fibrous materials, they exposed the tracheal lobe of 16 sheep to a single exposure of either 100 ml saline, 100 mg UICC asbestos fibers in 100 ml saline, 100 mg short asbestos fibers in 100 ml saline, or 100 mg attapulgite in 100 ml saline. The animals were studied by bronchoalveolar lavage (BAL) at Days 2, 12, 24, 40, and 60 and by autopsy at Day 60. In the saline-exposed sheep, BAL and lung histology did not change. In the UICC asbestos-exposed animals, they reproduced the BAL changes previously reported. In the short asbestos-exposed sheep, there were no significant BAL changes. In the attapulgite sheep, they found significant and sustained increases in total BAL cells, macrophages, neutrophils, fibronectin, lactate dehydrogenase, ..beta..-glucuronidase, but BAL cellularity returned to control levels by Day 60 whereas in the UICC asbestos-exposed sheep, it remained significantly above control. Lung histology demonstrated the characteristic peribronchiolar fibrosing alveolitis in the UICC asbestos-exposed sheep, whereas macrophagic alveolitis with minimal airway distortion was seen in the short asbestos-exposed sheep, whereas macrophagic alveolitis with minimal airway distortion was seen in the short asbestos-exposed sheep and in all of the attapulgite-exposed sheep but three which had typical peribronchiolar alveolitis quite similar to that observed in UICC-exposed sheep, but of lower intensity.

  12. Two new compounds from Crataegus pinnatifida and their antithrombotic activities.

    PubMed

    Zhou, Chen-Chen; Huang, Xiao-Xiao; Gao, Pin-Yi; Li, Fei-Fei; Li, Dian-Ming; Li, Ling-Zhi; Song, Shao-Jiang

    2014-01-01

    One new sesquiterpene, (1α,4aβ,8aα)-1-isopropanol-4a-methyl-8-methylenedecahydronaphthalene (1), with one new phenylpropanoid, threo-2-(4-hydroxy-3,5-dimethoxyphenyl)-3-(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-ol (2), along with four known phenylpropanoids were isolated from Crataegus pinnatifida. The structures of compounds 1 and 2 were elucidated on the basis of 1D, 2D NMR analyses, and HR-ESI-MS. The antithrombotic activity in vitro of all isolates was assayed, and only compound 1 exhibited potent antithrombotic activity by inhibiting platelet aggregation in rat plasma by 81.4% at 1 mg/ml.

  13. Antileishmanial Activity of Compounds Isolated from Sassafras albidum.

    PubMed

    Pulivarthi, Divya; Steinberg, Kelly Marie; Monzote, Lianet; Piñón, Abel; Setzer, William N

    2015-07-01

    Leishmaniasis is a neglected tropical disease caused by Leishmania parasitic protozoa, which currently lacks efficient treatment. Natural products have shown promise as a potential source for antiprotozoal drugs. This work focuses on the antileishmanial potential of Sassafras albidum (Lauraceae) bark extract. The crude bark extract of S. albidum showed excellent antileishmanial activity with an IC50 value less than 12.5 μg/mL against promastigotes of L. amazonensis. The chloroform stem bark extract of S. albidum was subjected to preparative column chromatography. Five compounds were isolated, purified by recrystallization, and identified as sesamin, spinescin, β-sitosterol, hexatriacontanal, and 1-triacontanol. Antileishmanial and cytotoxic screening were performed on these compounds. Sesamin exhibited the best activity against L. amazonensis with an IC50 of 15.8 μg/mL and was not cytotoxic to mouse macrophage cells (CC50 > 100 μg/mL).

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

    PubMed

    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.

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

    PubMed

    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.

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

    PubMed

    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.

  17. Alternative preparation of propolis extracts: comparison of their composition and biological activities.

    PubMed

    Kubiliene, Loreta; Laugaliene, Virginija; Pavilonis, Alvydas; Maruska, Audrius; Majiene, Daiva; Barcauskaite, Karolina; Kubilius, Raimondas; Kasparaviciene, Giedre; Savickas, Arunas

    2015-05-27

    Propolis is the bee product noted for multiple biological effects, and therefore it is widely used for the prevention and treatment of a variety of diseases. The active substances of propolis are easily soluble in ethanol. However ethanolic extracts cannot be used in treatment of certain diseases encountered in ophthalmology, pediatrics, etc. Unfortunately, the main biologically active substances of propolis are scarcely soluble in water, oil and other solvents usually used in pharmaceutical industry. The aim of this study was to investigate chemical composition, radical scavenging and antimicrobial activity of propolis extracts differently made in nonethanolic solvents. Total content of phenolic compounds in extracts was determined using Folin-Ciocalteu method. Chemical composition and radical scavenging activity of extracts were determined using HPLC system with free radical reaction detector. Antimicrobial activity of examined preparations was evaluated using the agar-well diffusion assay. Total amount of phenolic compounds in extracts made in polyethylene glycol 400 (PEG) and water mixture or in PEG, olive oil and water mixture at 70 °C was comparable to that of ethanolic extract. Predominantly identified compounds were phenolic acids, which contribute ca. 40 % of total radical scavenging activity. Investigated nonethanolic extracts inhibited the growth and reproduction of all tested microrganisms. Antimicrobial activity of some extracts was equal or exceeded the antimicrobial effect of ethanolic extract. Extracts made in pure water or oil only at room temperature, contained more than 5 - 10-fold lower amount of phenolic compounds, and demonstrated no antimicrobial activity. Nonethanolic solvent complex and the effect of higher temperature allows more effective extraction of active compounds from propolis. Concentration of total phenolic compounds in these extracts does not differ significantly from the concentration found in ethanolic extract. Propolis

  18. Resources and Biological Activities of Natural Polyphenols

    PubMed Central

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

    2014-01-01

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

  19. Resources and biological activities of natural polyphenols.

    PubMed

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

    2014-12-22

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

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

    PubMed

    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.

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

    PubMed

    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. © 2014 Society for Laboratory Automation and Screening.

  2. Automated structure–activity relationship mining: connecting chemical structure to biological profiles

    PubMed Central

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

    2017-01-01

    Understanding 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. While 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 dataset, we prioritized groups of compounds for further study, including a novel set of putative histone deacetylase inhibitors. PMID:24710340

  3. Biological activity of peanut (Arachis hypogaea) phytoalexins and selected natural and synthetic Stilbenoids.

    PubMed

    Sobolev, Victor S; Khan, Shabana I; Tabanca, Nurhayat; Wedge, David E; Manly, Susan P; Cutler, Stephen J; Coy, Monique R; Becnel, James J; Neff, Scott A; Gloer, James B

    2011-03-09

    The peanut plant (Arachis hypogaea L.), when infected by a microbial pathogen, is capable of producing stilbene-derived compounds that are considered antifungal phytoalexins. In addition, the potential health benefits of other stilbenoids from peanuts, including resveratrol and pterostilbene, have been acknowledged by several investigators. Despite considerable progress in peanut research, relatively little is known about the biological activity of the stilbenoid phytoalexins. This study investigated the activities of some of these compounds in a broad spectrum of biological assays. Since peanut stilbenoids appear to play roles in plant defense mechanisms, they were evaluated for their effects on economically important plant pathogenic fungi of the genera Colletotrichum, Botrytis, Fusarium, and Phomopsis. We further investigated these peanut phytoalexins, together with some related natural and synthetic stilbenoids (a total of 24 compounds) in a panel of bioassays to determine their anti-inflammatory, cytotoxic, and antioxidant activities in mammalian cells. Several of these compounds were also evaluated as mammalian opioid receptor competitive antagonists. Assays for adult mosquito and larvae toxicity were also performed. The results of these studies reveal that peanut stilbenoids, as well as related natural and synthetic stilbene derivatives, display a diverse range of biological activities.

  4. Biological Activity of Peanut (Arachis hypogaea) Phytoalexins and Selected Natural and Synthetic Stilbenoids

    PubMed Central

    SOBOLEV, VICTOR S.; KHAN, SHABANA I.; TABANCA, NURHAYAT; WEDGE, DAVID E.; MANLY, SUSAN P.; CUTLER, STEPHEN J.; COY, MONIQUE R.; BECNEL, JAMES J.; NEFF, SCOTT A.; GLOER, JAMES B.

    2011-01-01

    The peanut plant (Arachis hypogaea L.), when infected by a microbial pathogen, is capable of producing stilbene-derived compounds that are considered antifungal phytoalexins. In addition, the potential health benefits of other stilbenoids from peanuts, including resveratrol and pterostilbene, have been acknowledged by several investigators. Despite considerable progress in peanut research, relatively little is known about the biological activity of the stilbenoid phytoalexins. This study investigated the activities of some of these compounds in a broad spectrum of biological assays. Since peanut stilbenoids appear to play roles in plant defense mechanisms, they were evaluated for their effects on economically important plant pathogenic fungi of the genera Colletotrichum, Botrytis, Fusarium, and Phomopsis. We further investigated these peanut phytoalexins, together with some related natural and synthetic stilbenoids (a total of 24 compounds) in a panel of bioassays to determine their anti-inflammatory, cytotoxic, and antioxidant activities in mammalian cells. Several of these compounds were also evaluated as mammalian opioid receptor competitive antagonists. Assays for adult mosquito and larvae toxicity were also performed. The results of these studies reveal that peanut stilbenoids, as well as related natural and synthetic stilbene derivatives, display a diverse range of biological activities. PMID:21314127

  5. Separation of phytochemicals from Helichrysum italicum: An analysis of different isolation techniques and biological activity of prepared extracts.

    PubMed

    Maksimovic, Svetolik; Tadic, Vanja; Skala, Dejan; Zizovic, Irena

    2017-06-01

    Helichrysum italicum presents a valuable source of natural bioactive compounds. In this work, a literature review of terpenes, phenolic compounds, and other less common phytochemicals from H. italicum with regard to application of different separation methods is presented. Data including extraction/separation methods and experimental conditions applied, obtained yields, number of identified compounds, content of different compound groups, and analytical techniques applied are shown as corresponding tables. Numerous biological activities of both isolates and individual compounds are emphasized. In addition, the data reported are discussed, and the directions for further investigations are proposed.

  6. Biology-oriented synthesis of stereochemically diverse natural-product-derived compound collections by iterative allylations on a solid support.

    PubMed

    Umarye, Jayant D; Lessmann, Torben; García, Ana B; Mamane, Victor; Sommer, Stefan; Waldmann, Herbert

    2007-01-01

    A strategy aiming at the introduction of stereocenters into polymer-bound natural-product-derived and -inspired compound collections is presented. Treatment of immobilized aldehydes with Brown's pinene-derived allylboranes results in the stereoselective formation of homoallylic alcohols with up to 89 % ee (ee=enantiomeric excess). Subsequent iterative ozonolysis-allylation sequences with up to three allylations on a solid support give access to 1,3-polyols with different relative configurations. Esterification with acryloyl chloride and final ring-closing metathesis yields alpha,beta-unsaturated delta-lactones with multiply oxygenated side chains, a substructure found in a group of natural products with a broad range of biological activity. The flexibility of the approach is exemplified by the parallel synthesis of all eight diastereomers of cryptocarya diacetate on a solid support. The individual isomers are obtained in overall yields of 40-60 % over 10 steps and with 63-85 % diastereoselectivity for the major isomer.

  7. Potentialities of coupling biological processes (biotrickler/biofilter) for the degradation of a mixture of sulphur compounds.

    PubMed

    Malhautier, Luc; Soupramanien, Alexandre; Bayle, Sandrine; Rocher, Janick; Fanlo, Jean-Louis

    2015-01-01

    This study deals with the potential of biological processes combining a biotrickler and a biofilter to treat a mixture of sulphur-reduced compounds including dimethyl sulphide (DMS), dimethyl disulphide (DMDS) and hydrogen sulphide (H2S). As a reference, duplicated biofilters were implemented, and operating conditions were similar for all bioprocesses. The first step of this work was to determine the efficiency removal level achieved for each compound of the mixture and in a second step, to assess the longitudinal distribution of biodegradation activities and evaluate the total bacteria, Hyphomicrobium sp. and Thiobacillus thioparus densities along the bed height. A complete removal of hydrogen sulphide is reached at the start of the experiment within the first stage (biotrickler) of the coupling. This study highlighted that the coupling of a biotrickling filter and a biofilter is an interesting way to improve both removal efficiency levels (15-20% more) and kinetics of recalcitrant sulphur compounds such as DMS and DMDS. The total cell densities remained similar (around 1 × 10(10) 16S recombinant DNA (rDNA) copies g dry packing material) for duplicated biofilters and the biofilter below the biotrickling filter. The relative abundances of Hyphomicrobium sp. and T. thioparus have been estimated to an average of 10 ± 7.0 and 0.23 ± 0.07%, respectively, for all biofilters. Further investigation should allow achieving complete removal of DMS by starting the organic sulphur compound degradation within the first stage and surveying microbial community structure colonizing this complex system.

  8. Quinolone Amides as Antitrypanosomal Lead Compounds with In Vivo Activity

    PubMed Central

    Hiltensperger, Georg; Hecht, Nina; Kaiser, Marcel; Rybak, Jens-Christoph; Hoerst, Alexander; Dannenbauer, Nicole; Müller-Buschbaum, Klaus; Bruhn, Heike; Esch, Harald; Lehmann, Leane; Meinel, Lorenz

    2016-01-01

    Human African trypanosomiasis (HAT) is a major tropical disease for which few drugs for treatment are available, driving the need for novel active compounds. Recently, morpholino-substituted benzyl amides of the fluoroquinolone-type antibiotics were identified to be compounds highly active against Trypanosoma brucei brucei. Since the lead compound GHQ168 was challenged by poor water solubility in previous trials, the aim of this study was to introduce structural variations to GHQ168 as well as to formulate GHQ168 with the ultimate goal to increase its aqueous solubility while maintaining its in vitro antitrypanosomal activity. The pharmacokinetic parameters of spray-dried GHQ168 and the newly synthesized compounds GHQ242 and GHQ243 in mice were characterized by elimination half-lives ranging from 1.5 to 3.5 h after intraperitoneal administration (4 mice/compound), moderate to strong human serum albumin binding for GHQ168 (80%) and GHQ243 (45%), and very high human serum albumin binding (>99%) for GHQ242. For the lead compound, GHQ168, the apparent clearance was 112 ml/h and the apparent volume of distribution was 14 liters/kg of body weight (BW). Mice infected with T. b. rhodesiense (STIB900) were treated in a stringent study scheme (2 daily applications between days 3 and 6 postinfection). Exposure to spray-dried GHQ168 in contrast to the control treatment resulted in mean survival durations of 17 versus 9 days, respectively, a difference that was statistically significant. Results that were statistically insignificantly different were obtained between the control and the GHQ242 and GHQ243 treatments. Therefore, GHQ168 was further profiled in an early-treatment scheme (2 daily applications at days 1 to 4 postinfection), and the results were compared with those obtained with a control treatment. The result was statistically significant mean survival times exceeding 32 days (end of the observation period) versus 7 days for the GHQ168 and control treatments

  9. Biologically active secondary metabolites from Asphodelus microcarpus

    USDA-ARS?s Scientific Manuscript database

    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), em...

  10. Presence of pharmaceutically active compounds in Doñana Park (Spain) main watersheds.

    PubMed

    Camacho-Muñoz, M D; Santos, J L; Aparicio, I; Alonso, E

    2010-05-15

    Among the emerging environmental contaminants, pharmaceutically active compounds have become a growing public concern because of their potential to cause undesirable ecological and human health effects. Doñana Park (South of Spain) includes a mosaic of unique ecosystems known around the world which is particularly affected by the quality of the incoming flowing water. This study reports the presence of a number of priority pharmaceuticals in wastewater and surface water samples from Doñana watersheds. In general, ibuprofen, naproxen, salicylic acid, propranolol, caffeine and gemfibrozil were the compounds most frequently found in all locations, in the range of ng/L to microg/L. Carbamazepine, with high potential risk to the environment, was also detected, although only in a few water samples. The main results are: (i) pharmaceuticals, as water pollutants, are continually discharged into Doñana water bodies and, owing to their biological activity, could lead to adverse effects in this outstanding aquatic ecosystem; (ii) wastewater treatments implemented in the area are insufficient to remove pharmaceuticals; and (iii) therefore, there is a requirement for better wastewater treatments in this natural area to reduce or avoid the presence of organic pollutants in general and pharmaceutical active compounds in particular. To the best of our knowledge, these data constitute the first measurements of pharmaceutical compounds in water not only from the protected area of Doñana Park but also from other Natural or National Parks in the world. Copyright (c) 2010 Elsevier B.V. All rights reserved.

  11. Essential Oils’ Chemical Characterization and Investigation of Some Biological Activities: A Critical Review

    PubMed Central

    Dhifi, Wissal; Bellili, Sana; Jazi, Sabrine; Bahloul, Nada; Mnif, Wissem

    2016-01-01

    This review covers literature data summarizing, on one hand, the chemistry of essential oils and, on the other hand, their most important activities. Essential oils, which are complex mixtures of volatile compounds particularly abundant in aromatic plants, are mainly composed of terpenes biogenerated by the mevalonate pathway. These volatile molecules include monoterpenes (hydrocarbon and oxygenated monoterpens), and also sesquiterpenes (hydrocarbon and oxygenated sesquiterpens). Furthermore, they contain phenolic compounds, which are derived via the shikimate pathway. Thanks to their chemical composition, essential oils possess numerous biological activities (antioxidant, anti-inflammatory, antimicrobial, etc…) of great interest in food and cosmetic industries, as well as in the human health field. PMID:28930135

  12. The Infusion of Environmental Activities into a Secondary Biology Curriculum

    ERIC Educational Resources Information Center

    Foster, Helen M.

    1976-01-01

    Reviewed are "adventure-type" environmental education activities incorporated into a secondary level biology course. Student wilderness experiences included 24 weekend activities of hiking, bird watching, camping, and cross-country skiing. (SL)

  13. Multifunctional and biologically active matrices from multicomponent polymeric solutions

    NASA Technical Reports Server (NTRS)

    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.

  14. Interaction of herbal compounds with biological targets: a case study with berberine.

    PubMed

    Chen, Xiao-Wu; Di, Yuan Ming; Zhang, Jian; Zhou, Zhi-Wei; Li, Chun Guang; Zhou, Shu-Feng

    2012-01-01

    Berberine is one of the main alkaloids found in the Chinese herb Huang lian (Rhizoma Coptidis), which has been reported to have multiple pharmacological activities. This study aimed to analyze the molecular targets of berberine based on literature data followed by a pathway analysis using the PANTHER program. PANTHER analysis of berberine targets showed that the most classes of molecular functions include receptor binding, kinase activity, protein binding, transcription activity, DNA binding, and kinase regulator activity. Based on the biological process classification of in vitro berberine targets, those targets related to signal transduction, intracellular signalling cascade, cell surface receptor-linked signal transduction, cell motion, cell cycle control, immunity system process, and protein metabolic process are most frequently involved. In addition, berberine was found to interact with a mixture of biological pathways, such as Alzheimer's disease-presenilin and -secretase pathways, angiogenesis, apoptosis signalling pathway, FAS signalling pathway, Hungtington disease, inflammation mediated by chemokine and cytokine signalling pathways, interleukin signalling pathway, and p53 pathways. We also explored the possible mechanism of action for the anti-diabetic effect of berberine. Further studies are warranted to elucidate the mechanisms of action of berberine using systems biology approach.

  15. Interaction of Herbal Compounds with Biological Targets: A Case Study with Berberine

    PubMed Central

    Chen, Xiao-Wu; Di, Yuan Ming; Zhang, Jian; Zhou, Zhi-Wei; Li, Chun Guang; Zhou, Shu-Feng

    2012-01-01

    Berberine is one of the main alkaloids found in the Chinese herb Huang lian (Rhizoma Coptidis), which has been reported to have multiple pharmacological activities. This study aimed to analyze the molecular targets of berberine based on literature data followed by a pathway analysis using the PANTHER program. PANTHER analysis of berberine targets showed that the most classes of molecular functions include receptor binding, kinase activity, protein binding, transcription activity, DNA binding, and kinase regulator activity. Based on the biological process classification of in vitro berberine targets, those targets related to signal transduction, intracellular signalling cascade, cell surface receptor-linked signal transduction, cell motion, cell cycle control, immunity system process, and protein metabolic process are most frequently involved. In addition, berberine was found to interact with a mixture of biological pathways, such as Alzheimer's disease-presenilin and -secretase pathways, angiogenesis, apoptosis signalling pathway, FAS signalling pathway, Hungtington disease, inflammation mediated by chemokine and cytokine signalling pathways, interleukin signalling pathway, and p53 pathways. We also explored the possible mechanism of action for the anti-diabetic effect of berberine. Further studies are warranted to elucidate the mechanisms of action of berberine using systems biology approach. PMID:23213296

  16. Compounds from Sedum caeruleum with antioxidant, anticholinesterase, and antibacterial activities.

    PubMed

    Bensouici, Chawki; Kabouche, Ahmed; Karioti, Anastasia; Öztürk, Mehmet; Duru, Mehmet Emin; Bilia, Anna Rita; Kabouche, Zahia

    2016-01-01

    This is the first study on the phytochemistry, antioxidant, anticholinesterase, and antibacterial activities of Sedum caeruleum L. (Crassulaceae). The objective of this study is to isolate the secondary metabolites and determine the antioxidant, anticholinesterase, and antibacterial activities of S. caeruleum. Six compounds (1-6) were isolated from the extracts of S. caeruleum and elucidated using UV, 1D-, 2D-NMR, and MS techniques. Antioxidant activity was investigated using DPPH(•), CUPRAC, and ferrous-ions chelating assays. Anticholinesterase activity was determined against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes using the Ellman method. Antibacterial activity was performed according to disc diffusion and minimum inhibitory concentration (MIC) methods. Isolated compounds were elucidated as ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6). The butanol extract exhibited highest antioxidant activity in all tests (IC50 value: 28.35 ± 1.22 µg/mL in DPPH assay, IC50 value: 40.83 ± 2.24 µg/L in metal chelating activity, and IC50 value: 23.52 ± 0.44 µg/L in CUPRAC), and the highest BChE inhibitory activity (IC50 value: 36.89 ± 0.15 µg/L). Moreover, the chloroform extract mildly inhibited (MIC value: 80 µg/mL) the growth of all the tested bacterial strains. Ursolic acid (1), daucosterol (2), β-sitosterol-3-O-β-D-galactopyranoside (3), apigenin (4), apigetrin (5), and apiin (6) were isolated from Sedum caeruleum for the first time. In addition, a correlation was observed between antioxidant and anticholinesterase activities of bioactive ingredients of this plant.

  17. Isoflavones, their Glycosides and Glycoconjugates. Synthesis and Biological Activity

    PubMed Central

    Szeja, Wiesław; Grynkiewicz, Grzegorz; Rusin, Aleksandra

    2017-01-01

    Glycosylation of small biologically active molecules, either of natural or synthetic origin, has a profound impact on their solubility, stability, and bioactivity, making glycoconjugates attractive compounds as therapeutic agents or nutraceuticals. A large proportion of secondary metabolites, including flavonoids, occur in plants as glycosides, which adds to the molecular diversity that is much valued in medicinal chemistry studies. The subsequent growing market demand for glycosidic natural products has fueled the development of various chemical and biotechnological methods of glycosides preparation. The review gives an extensive overview of the processes of the synthesis of isoflavones and discusses recently developed major routes towards isoflavone-sugar formation processes. Special attention is given to the derivatives of genistein, the main isoflavone recognized as a useful lead in several therapeutic categories, with particular focus on anticancer drug design. The utility of chemical glycosylations as well as glycoconjugates preparation is discussed in some theoretical as well as practical aspects. Since novel approaches to chemical glycosylations and glycoconjugations are abundant and many of them proved suitable for derivatization of polyphenols a new body of evidence has emerged, indicating that sugar moiety can play a much more significant role, when attached to a pharmacophore, then being a mere “solubilizer”. In many cases, it has been demonstrated that semisynthetic glycoconjugates are much more potent cytostatic and cytotoxic agents than reference isoflavones. Moreover, the newly designed glycosides or glycoside mimics can act through different mechanisms than the parent active molecule. PMID:28553156

  18. Biological activities of thionated thyrotropin-releasing hormone analogs.

    PubMed

    Lankiewicz, L; Bowers, C Y; Reynolds, G A; Labroo, V; Cohen, L A; Vonhof, S; Sirén, A L; Spatola, A F

    1992-04-15

    Analogs of thyrotropin-releasing hormone (Glp-His-Pro-NH2, TRH) have been prepared which contain thioamide moieties in the pyroglutamic acid ring, the carboxyamide proline terminus, and in both positions (dithio). These compounds have been tested for TSH-releasing activities (in vitro and in vivo), and for binding to TRH receptors in rat pituitary and cortex. The monothionated analogs showed no significant differences in TSH-releasing potency from TRH either in vitro or in vivo. However, with two thioamide replacements the potency decreases about 50%. Significantly, in terms of receptor selectivity, thionation has resulted in differentiation between brain receptors (pituitary and cortex). The Pro psi[CSNH2] and dithio analogs were more selective (higher affinity to pituitary receptors) than the parent hormone, while the analog containing a thioamide replacement in the pyroglutamyl ring had lower affinity and was not selective. These results suggest that the subtle exchange of sulphur for oxygen can have an important impact on both receptor selectivity and affinity within a biologically active peptide.

  19. A new assay system for guinea pig interferon biological activity.

    PubMed

    Yamamoto, Toshiko; Jeevan, Amminikutty; Ohishi, Kazue; Nojima, Yasuhiro; Umemori, Kiyoko; Yamamoto, Saburo; McMurray, David N

    2002-07-01

    We have developed an assay system for guinea pig interferon (IFN) based on reduction of viral cytopathic effect (CPE) in various cell lines. CPE inhibition was detected optimally in the guinea pig fibroblast cell line 104C1 infected with encephalomyocarditis virus (EMCV). The amount of biologically active guinea pig IFN was quantified by estimating viable cell numbers colorimetrically by means of a tetrazolium compound, 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-1) and 1-methoxy-5-methylphenazinium methylsulfate (PMS). WST-1 color developed until stopped by the addition of sulfuric acid. This had no effect on the colorimetric assay, and the color was stable for at least 24 h. The acid also inactivated the EMCV and, thus, eliminated the viral hazard. Inhibition of CPE activity was highly correlated with the concentration of culture supernatants from BCG-vaccinated guinea pig splenocytes stimulated in vitro with tuberculin or an immunostimulatory oligoDNA. This assay detected guinea pig IFN and human IFN-alpha, but not IFN-gamma from human, mouse, rat, pig, or dog. This assay system has proved useful for the titration of guinea pig IFN, being easy to perform, free from viral hazard, relatively species specific, highly reproducible, and inexpensive.

  20. Organometallic ruthenium(II) arene compounds with antiangiogenic activity.

    PubMed

    Nowak-Sliwinska, Patrycja; van Beijnum, Judy R; Casini, Angela; Nazarov, Alexey A; Wagnieres, Georges; van den Bergh, Hubert; Dyson, Paul J; Griffioen, Arjan W

    2011-06-09

    The antimetastatic ruthenium(II) compounds [Ru(η(6)-p-cymene)Cl(2)(PTA)] (PTA = 1,3,5-triaza-7-phosphaadamantane) (RAPTA-C) and [Ru(η(6)-toluene)Cl(2)(PTA)] (RAPTA-T), as well as their analogues [Ru(η(6)-p-cymene)Cl(2)(DAPTA)] (DAPTA = (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane)) (DAPTA-C) and [Ru(η(6)-toluene)Cl(2)(DAPTA)] (DAPTA-T), respectively, were tested in in vitro bioassays for endothelial cell function. All compounds showed low toxicity profiles and similar dose-dependent antiproliferative effects in endothelial cells at ≥100 μg/mL (∼200 μM). EC migration, measured 6 h after drug exposure, was also efficiently inhibited (ED(50) of ∼300 μg/mL, ∼500 μM, for all compounds). Since no cytostatic effect was noted, the inhibition of proliferation was considered mainly to consist of antiangiogenic activity. RAPTA-T and DAPTA-C were also tested in vivo in the chicken chorioallantoic membrane (CAM) assay and found to inhibit CAM development. Importantly, effective prevention of revascularization of the CAM after vaso-occlusive photodynamic therapy was observed. The reported ruthenium complexes show promising antimetastatic activity involving inhibition of angiogenesis and therefore are attractive agents for development of anticancer therapies based on combination of chemo- and angiostatic treatments.

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

    PubMed

    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.

  2. Vanadium, Ruthenium and Copper Compounds: A New Class of Nonplatinum Metallodrugs with Anticancer Activity.

    PubMed

    Leon, Ignacio Esteban; Cadavid-Vargas, Juan Fernando; Di Virgilio, Ana Laura; Etcheverry, Susana Beatriz

    2017-01-01

    Cancer is a group of diseases involving abnormal cell growth. The cells grow uncontrollably with the potential to invade and spread to other parts of the body. This disease is one of the principal death causes in the world, thus becoming a significant topic of scientific research. On the other hand, transition metals play a fundamental role in different living systems. In particular, Metallodrugs represent new and powerful tools for diverse therapeutic applications. To date, various metallodrugs display interesting biological activities for chemotherapy. In this field, cisplatin was the first inorganic compound with high relevance in cancer treatment. This compound was a leader agent in clinical use. Toxicity and resistance problems trigger the development of other platinum drugs with better clinical perspective and also raise the scientific interest for the putative antitumor properties of V, Ru and Cu compounds. Several scientific articles show that complexes of these metals are the new metal-based drugs used in the treatment of several cancers, such us, lung, colon, breast, bladder, etc. In this review we recapitulate current information and new advances on antitumor in vitro effects of several organic and inorganic compounds derived from copper, ruthenium and vanadium. These metal derived compounds targeting DNA or cell proteins involved in cell signaling pathways related to cancer. The mechanisms of cell death of these metallodrugs have also been comprehensibly reviewed. The knowledge of these mechanisms of death and the relationship between chemical structure and biological activity may be useful for the design of new metal-based drugs with promising pharmacologic applications as anticancer agents. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  3. Factors affecting antibacterial activity of hop compounds and their derivatives.

    PubMed

    Simpson, W J; Smith, A R

    1992-04-01

    The antibacterial effect of weak acids derived from the hop plant (Humulus lupulus L.) increased with decreasing pH. Analysis of the minimum inhibitory concentration of such compounds against Lactobacillus brevis IFO 3960 over pH 4-7 suggests that undissociated molecules were mainly responsible for inhibition of bacterial growth. The antibacterial activity of trans-isohumulone was ca 20 times greater than that of humulone, 11 times greater than that of colupulone and nine times greater than that of trans-humulinic acid when the degree of ionization was taken into account. Monovalent cations (K+, Na+, NH4+, Rb+, Li+) stimulated antibacterial activity of trans-isohumulone but the effect was smaller than that observed with H+. The response to divalent cations varied: Ca2+ had little effect on antibacterial activity, whereas Mg2+ reduced activity. Lipid materials and beta-cyclodextrin also antagonized the antibacterial action of trans-isohumulone.

  4. Phytochemical components and biological activities of Silene arenarioides Desf.

    PubMed

    Golea, Lynda; Benkhaled, Mohammed; Lavaud, Catherine; Long, Christophe; Haba, Hamada

    2017-02-24

    In this study, six known compounds 1-6 were isolated from the aerial parts of Silene arenarioides Desf. using different chromatographic methods. The structures of these compounds were identified as maltol glycoside (1), soyacerebroside I (2), chrysin (3), apigenin (4), quercetin (5) and stigmasterol glucoside (6). The compounds (1) and (2) are reported for the first time from this genus. The isolated compounds were determined using NMR techniques ((1)H NMR, (13)C NMR, COSY, HSQC and HMBC) and mass spectroscopy (ESI-MS). The antibacterial and antioxidant activities of extracts and of compound (1) have been evaluated. The antioxidant activity was performed by DPPH radical scavenging method, which showed that methanol extract possesses a good antioxidant activity with value of IC50 = 8.064 ± 0.005 μg/mL.

  5. Cytotoxic activity of compounds from the lichen: Cladonia convoluta.

    PubMed

    Bézivin, Carine; Tomasi, Sophie; Rouaud, Isabelle; Delcros, Jean-Guy; Boustie, Joël

    2004-09-01

    The depsidone 9'-( O-methyl)protocetraric acid was isolated from the lichen Cladonia convoluta (Lam.) Anders along with the known (-)-usnic acid and fumarprotocetraric acid. The complete structure of 9'-( O-methyl)protocetraric acid was elucidated using HSQC and HMBC spectral data. (-)-Usnic acid was the only compound to display a moderate cytotoxic activity on various cancer cell lines (IC (50) = 6, 12.1, 15.8, 17.8, 8.2 and 6.8 microg/mL on L1210, 3LL, DU145, MCF7, K-562 and U251, respectively). This compound was also shown to induce apoptosis of murine leukaemia L1210 cells in a dose- and time-dependent manner.

  6. Natural Product Compounds with Aromatase Inhibitory Activity: An Update

    PubMed Central

    Balunas, Marcy J.; Kinghorn, A. Douglas

    2010-01-01

    Several synthetic aromatase inhibitors are currently in clinical use for the treatment of postmenopausal women with hormone-receptor positive breast cancer. However, these treatments may lead to untoward side effects and so a search for new aromatase inhibitors continues, especially those for which the activity is promoter-specific, targeting the breast-specific promoters I.3 and II. Recently, numerous natural product compounds have been found to inhibit aromatase in non-cellular, cellular, and in vivo studies. These investigations, covering the last two years, as well as additional studies that have focused on the evaluation of natural product compounds as promoter-specific aromatase inhibitors or as aromatase inducers, are described in this review. PMID:20635310

  7. Milk inhibits the biological activity of ricin

    USDA-ARS?s Scientific Manuscript database

    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...

  8. Relationships Between Bioactive Compound Content and
the Antiplatelet and Antioxidant Activities of Six Allium Vegetable Species.

    PubMed

    Beretta, Hebe Vanesa; Bannoud, Florencia; Insani, Marina; Berli, Federico; Hirschegger, Pablo; Galmarini, Claudio Rómulo; Cavagnaro, Pablo Federico

    2017-06-01

    Allium sp. vegetables are widely consumed for their characteristic flavour. Additionally, their consumption may provide protection against cardiovascular disease due to their antiplatelet and antioxidant activities. Although antiplatelet and antioxidant activities in Allium sp. are generally recognised, comparative studies of antiplatelet and antioxidant potency among the main Allium vegetable species are lacking. Also, the relationship between organosulfur and phenolic compounds and these biological activities has not been well established. In this study, the in vitro antiplatelet and antioxidant activities of the most widely consumed Allium species are characterised and compared. The species total organosulfur and phenolic content, and the HPLC profiles of 11 phenolic compounds were characterised and used to investigate the relationship between these compounds and antiplatelet and antioxidant activities. Furthermore, antiplatelet activities in chives and shallot have been characterised for the first time. Our results revealed that the strongest antiplatelet agents were garlic and shallot, whereas chives had the highest antioxidant activity. Leek and bunching onion had the weakest both biological activities. Significantly positive correlations were found between the in vitro antiplatelet activity and total organosulfur (R=0.74) and phenolic (TP) content (R=0.73), as well as between the antioxidant activity and TP (R=0.91) and total organosulfur content (R=0.67). Six individual phenolic compounds were associated with the antioxidant activity, with catechin, epigallocatechin and epicatechin gallate having the strongest correlation values (R>0.80). Overall, our results suggest that both organosulfur and phenolic compounds contribute similarly to Allium antiplatelet activity, whereas phenolics, as a whole, are largely responsible for antioxidant activity, with broad variation observed among the contributions of individual phenolic compounds.

  9. Relationships Between Bioactive Compound Content and
the Antiplatelet and Antioxidant Activities of Six Allium Vegetable Species

    PubMed Central

    Beretta, Hebe Vanesa; Bannoud, Florencia; Insani, Marina; Berli, Federico; Hirschegger, Pablo; Galmarini, Claudio Rómulo

    2017-01-01

    Summary Allium sp. vegetables are widely consumed for their characteristic flavour. Additionally, their consumption may provide protection against cardiovascular disease due to their antiplatelet and antioxidant activities. Although antiplatelet and antioxidant activities in Allium sp. are generally recognised, comparative studies of antiplatelet and antioxidant potency among the main Allium vegetable species are lacking. Also, the relationship between organosulfur and phenolic compounds and these biological activities has not been well established. In this study, the in vitro antiplatelet and antioxidant activities of the most widely consumed Allium species are characterised and compared. The species total organosulfur and phenolic content, and the HPLC profiles of 11 phenolic compounds were characterised and used to investigate the relationship between these compounds and antiplatelet and antioxidant activities. Furthermore, antiplatelet activities in chives and shallot have been characterised for the first time. Our results revealed that the strongest antiplatelet agents were garlic and shallot, whereas chives had the highest antioxidant activity. Leek and bunching onion had the weakest both biological activities. Significantly positive correlations were found between the in vitro antiplatelet activity and total organosulfur (R=0.74) and phenolic (TP) content (R=0.73), as well as between the antioxidant activity and TP (R=0.91) and total organosulfur content (R=0.67). Six individual phenolic compounds were associated with the antioxidant activity, with catechin, epigallocatechin and epicatechin gallate having the strongest correlation values (R>0.80). Overall, our results suggest that both organosulfur and phenolic compounds contribute similarly to Allium antiplatelet activity, whereas phenolics, as a whole, are largely responsible for antioxidant activity, with broad variation observed among the contributions of individual phenolic compounds. PMID:28867958

  10. A functional [NiFe]-hydrogenase model compound that undergoes biologically relevant reversible thiolate protonation.

    PubMed

    Weber, Katharina; Krämer, Tobias; Shafaat, Hannah S; Weyhermüller, Thomas; Bill, Eckhard; van Gastel, Maurice; Neese, Frank; Lubitz, Wolfgang

    2012-12-26

    Two model compounds of the active site of [NiFe]-hydrogenases with an unusual {S(2)Ni(μ-S)(μ-CO)Fe(CO)(2)S}-coordination environment around the metals are reported. The neutral compound [Ni(xbsms)(μ-CO)(μ-S)Fe(CO)(2)('S')], (1) (H(2)xbsms = 1,2-bis(4-mercapto-3,3-dimethyl-2-thiabutyl)benzene) is converted to [1H][BF(4)] by reversible protonation using HBF(4)·Et(2)O. The protonation takes place at the terminal thiolate sulfur atom that is coordinated to nickel. Catalytic intermediates with a protonated terminal cysteinate were suggested for the native protein but have not yet been confirmed experimentally. [1H][BF(4)] is the first dinuclear [NiFe] model compound for such a species. Both complexes have been synthesized and characterized by X-ray crystallography, NMR-, FTIR-, and (57)Fe-Mössbauer spectroscopy as well as by electronic absorption and resonance Raman spectroscopy. The experimental results clearly show that the protonation has a significant impact on the electronic structure of the iron center, although it takes place at the nickel site. DFT calculations support the interpretation of the spectroscopic data and indicate the presence of a bonding interaction between the metal ions, which is relevant for the enzyme as well. Electrochemical experiments show that both 1 and [1H][BF(4)] are active for electrocatalytic proton reduction in aprotic solvents.

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

    PubMed Central

    Astani, Akram; Reichling, Jürgen; Schnitzler, Paul

    2011-01-01

    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. PMID:20008902

  12. Screening for antiviral activities of isolated compounds from essential oils.

    PubMed

    Astani, Akram; Reichling, Jürgen; Schnitzler, Paul

    2011-01-01

    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.

  13. Studies on the antioxidant activities of some new chromone compounds.

    PubMed

    Kładna, Aleksandra; Berczyński, Paweł; Piechowska, Teresa; Kruk, Irena; Aboul-Enein, Hassan Y; Ceylan-Unlusoy, Meltem; Verspohl, Eugen J; Ertan, Rahmiye

    2014-11-01

    Recent reviews evidence that the naturally occurring compounds containing the chromone skeleton exhibit antiradical activities, providing protection against oxidative stress. The antioxidant activities of 13 new synthesized chromonyl-2,4-thiazolidinediones, chromonyl-2,4-imidazolidinediones and chromonyl-2-thioxoimidzolidine-4-ones were evaluated using in vitro antioxidant assays, including superoxide anion radical (O2(-•)), hydroxyl radical (HO(•)), 2,2-diphenyl-1-picryl-hydrazyl free radical (DPPH(•)) scavenging capacity and total antioxidant capacity ferric ion reducing activity. Superoxide anion radical was produced using potassium superoxide/18-crown-6-ether dissolved in dimethylsulfoxide, and the Fenton-like reaction (Fe(II) + H2O2) was a generator of hydroxyl radicals. Chemiluminescence, spectrophotometry, electron paramagnetic resonance (EPR) and 5,5-dimethyl-1-pyrroline-N-oxide (DMPO) as the spin trap were the measurement techniques. The results showed that the majority of the chromone derivatives tested showed a strong scavenging effect towards free radicals, similar to the chemiluminescence reaction with superoxide anion radical with a high activity, inhibition of the DMPO-OOH radical EPR signal (24-58%), the DMPO-OH radical EPR signal (4-75%) and DPPH radical EPR signal (6-100%) at 1 mmol/L. Several of the examined compounds exhibited the high reduction potentials. The results obtained show that the new synthesized chromone derivatives may directly scavenger reactive oxygen species and thus may play a protective role against oxidative damage. Copyright © 2014 John Wiley & Sons, Ltd.

  14. Anti-allergic activity of compounds from Kaempferia parviflora.

    PubMed

    Tewtrakul, Supinya; Subhadhirasakul, Sanan; Kummee, Sopa

    2008-02-28

    Kaempferia parviflora is one of the plants in the Zingiberaceae family, locally known in Thai as kra-chai-dam. In Thai traditional medicine, the decoction of Kaempferia parviflora powder with alcohol has been reported to cure allergy, asthma, impotence, gout, diarrhea, dysentery, peptic ulcer and diabetes. Therefore, the present study aimed to investigate anti-allergic substances from this plant. Bioassay-guided fractionation led to the isolation of seven methoxyflavone derivatives (1-7) from Kaempferia parviflora extract and they were identified on the basis of spectroscopic methods. Among the compounds tested, 5-hydroxy-3,7,3',4'-tetramethoxyflavone (5) possessed the highest anti-allergic activity against antigen-induced beta-hexosaminidase release as a marker of degranulation in RBL-2H3 cells with an IC(50) value of 8.0 microM, followed by 5-hydroxy-7-methoxyflavone (2, IC(50)=20.6 microM) and 5-hydroxy-7,4'-dimethoxyflavone (4, IC(50)=26.0 microM), whereas others showed moderate activities (IC(50)=37.5-66.5 microM). Structure-activity trends of 7-methoxyflavone derivatives on anti-allergic activity can be summarized as follows: (1) substitution with vicinal methoxyl groups at positions 3' and 4' conferred higher activity than only one methoxylation, (2) methoxylation at position 3 reduced activity and (3) methoxylation at position 5 showed higher activity than hydroxylation. Compounds 2, 4 and 5 were also determined for their mechanisms on ionomycin-induced beta-hexosaminidase release. The results indicated that the mechanism on inhibition of cell degranulation of compounds 2 and 5 mainly involve the inhibition of Ca(2+) influx to the cells, whereas that of 4 may be partly due to this inhibition. In regards to the active constituents for anti-allergic activity of Kaempferia parviflora, 5-hydroxy-3,7,3',4'-tetramethoxyflavone (5), 5-hydroxy-7-methoxyflavone (2) and 5-hydroxy-7,4'-dimethoxyflavone (4) are responsible for anti-allergic effect of this plant. The

  15. Nuclear factor kappa-B- and activator protein-1-mediated immunostimulatory activity of compound K in monocytes and macrophages.

    PubMed

    Yang, Woo Seok; Yi, Young-Su; Kim, Donghyun; Kim, Min Ho; Park, Jae Gwang; Kim, Eunji; Lee, Sang Yeol; Yoon, Keejung; Kim, Jong-Hoon; Park, Junseong; Cho, Jae Youl

    2017-07-01

    Compound K (CK) is a bioactive derivative of ginsenoside Rb1 in Panax ginseng (Korean ginseng). Its biological and pharmacological activities have been studied in various disease conditions, although its immunomodulatory role in innate immunity mediated by monocytes/macrophages has been poorly understood. In this study, we aimed to elucidate the regulatory role of CK on cellular events mediated by monocytes and macrophages in innate immune responses. The immunomodulatory role of CK was explored by various immunoassays including cell-cell adhesion, fibronectin adhesion, cell migration, phagocytic uptake, costimulatory molecules, reactive oxygen species production, luciferase activity, and by the measurement of mRNA levels of proinflammatory genes. Compound K induced cell cluster formation through cell-cell adhesion, cell migration, and phagocytic activity, but it suppressed cell-tissue interactions in U937 and RAW264.7 cells. Compound K also upregulated the surface expression of the cell adhesion molecule cluster of differentiation (CD) 43 (CD43) and costimulatory molecules CD69, CD80, and CD86, but it downregulated the expression of monocyte differentiation marker CD82 in RAW264.7 cells. Moreover, CK induced the release of reactive oxygen species and induced messenger RNA expression of proinflammatory genes, inducible nitric oxide synthase, and tumor necrosis factor-alpha by enhancing the nuclear translocation and transcriptional activities of nuclear factor kappa-B and activator protein-1. Our results suggest that CK has an immunomodulatory role in innate immune responses through regulating various cellular events mediated by monocytes and macrophages.

  16. Identification of Biologically Relevant Compounds in Aboveground and Belowground Induced Volatile Blends

    PubMed Central

    Qiu, Bao-Li; Hordijk, Cornelis A.; Vet, Louise E. M.; Jansen, Jeroen J.

    2010-01-01

    Plants under attack by aboveground herbivores emit complex blends of volatile organic compounds (VOCs). Specific compounds in these blends are used by parasitic wasps to find their hosts. Belowground induction causes shifts in the composition of aboveground induced VOC blends, which affect the preference of parasitic wasps. To identify which of the many volatiles in the complex VOC blends may explain parasitoid preference poses a challenge to ecologists. Here, we present a case study in which we use a novel bioinformatics approach to identify biologically relevant differences between VOC blends of feral cabbage (Brassica oleracea L.). The plants were induced aboveground or belowground with jasmonic acid (JA) and shoot feeding caterpillars (Pieris brassicae or P. rapae). We used Partial Least Squares—Discriminant Analysis (PLSDA) to integrate and visualize the relation between plant-emitted VOCs and the preference of female Cotesia glomerata. Overall, female wasps preferred JA-induced plants over controls, but they strongly preferred aboveground JA-induced plants over belowground JA-induced plants. PLSDA revealed that the emission of several monoterpenes was enhanced similarly in all JA-treated plants, whereas homoterpenes and sesquiterpenes increased exclusively in aboveground JA-induced plants. Wasps may use the ratio between these two classes of terpenes to discriminate between aboveground and belowground induced plants. Additionally, it shows that aboveground applied JA induces different VOC biosynthetic pathways than JA applied to the root. Our bioinformatic approach, thus, successfully identified which VOCs matched the preferences of the wasps in the various choice tests. Additionally, the analysis generated novel hypotheses about the role of JA as a signaling compound in aboveground and belowground induced responses in plants. PMID:20737198

  17. Comparison of the Biological Impacts of the Fluoride Compounds by Graphical Risk Visualization Map Technique.

    PubMed

    Usuda, Kan; Kono, Rei; Ueno, Takaaki; Ito, Yuichi; Dote, Tomotaro; Yokoyama, Hirotaka; Kono, Koichi; Tamaki, Junko

    2015-09-01

    Various fluoride compounds are widely used in industry. The present risk assessment study was conducted using a series of inorganic binary fluorides of the type XFn, where X(n) = Na(+), K(+), Li(+), Mg(2+), Ca(2+), Sr(2+), Ba(2+), Al(3+), Nd(3+), La(3+), Ce(3+), Sm(3+), Gd(3+), Y(3+), Yb(2+), and Zn(2+). The aqueous solutions of these salts were orally administrated to 16 experimental groups (one for each of the salts tested). The levels of fluoride, N-acetyl-β-D-glucosaminidase in cumulative 24-h urine samples and creatinine clearance were measured to assess possible acute renal damages. The levels of fluoride, alanine aminotransferase, and aspartate aminotransferase were also determined in serum samples to assess possible acute hepatic damages. The results reveal that sodium fluoride (NaF), potassium fluoride (KF), and zinc fluoride tetrahydrate (ZnF2 (.)4H2O) can carry the fluoride ion into the bloodstream and that it is excreted via urine more readily than the other compounds tested. These fluorides were assigned the highest risk impact factor. Most of the rare earth fluorides are insoluble in water while those groups 2 and 13 of the periodic table are slightly soluble, so that they do not have a significant negative risk. These findings suggest that the biological impact of fluoride depends on the accompanying counter ion and its solubility. The risk map obtained in the present study shows that the graphical visualization map technique employed is a valuable new tool to assess the toxicological risk of chemical compounds.

  18. Biologically active constituents of a polyphenol extract from Geranium sanguineum L. with anti-influenza activity.

    PubMed

    Pantev, Assen; Ivancheva, Stefka; Staneva, Lidija; Serkedjieva, Julia

    2006-01-01

    From the aerial roots of the medicinal plant Geranium sanguineum L. a polyphenol-rich extract with strong anti-influenza activity has been isolated. To investigate its active fractions, the extract was partitioned by solvents with increasing polarity. The n-BuOH fraction contained the majority of the in vitro antiviral activity; the EtOAc fraction was the most effective one in vivo. A bioassay-directed fractionation of the n-BuOH and EtOAc fractions was performed to obtain information about the nature of the chemical components of the plant extract, responsible for the antiviral effect. The individual constituents were identified by spectroscopic methods and comparison with authentic samples and by HPLC. The cell-toxic and virus-inhibitory effects of the fractions and some individual polyphenol compounds, found in Geranium sanguineum L., were studied using the replication of representative influenza viruses in cell cultures. This study showed that the presence of a variety of biologically active compounds as well as the possible synergistic interactions between them seem to be decisive for the overall antiviral effect.

  19. Structure-activity relationship study of novel anticancer aspirin-based compounds.

    PubMed

    Joseph, Stancy; Nie, Ting; Huang, Liqun; Zhou, Hui; Atmakur, Krishnaiah; Gupta, Ramesh C; Johnson, Francis; Rigas, Basil

    2011-01-01

    We performed a structure-activity relationship (SAR) study of a novel aspirin (ASA) derivative, which shows strong anticancer activity in vitro and in vivo. A series of ASA-based benzyl esters (ABEs) were synthesized and their inhibitory activity against human colon (HT-29 and SW480) and pancreatic (BxPC-3 and MIA PaCa-2) cancer cell lines was evaluated. The ABEs that we studied largely comprise organic benzyl esters bearing an ASA or acyloxy group (X) at the meta or para position of the benzyl ring and one of four different leaving groups. The nature of the salicyloyl/acyloxy function, the leaving group, and the additional substituents affecting the electron density of the benzyl ring, all were influential determinants of the inhibitory activity on cancer cell growth for each ABE. Positional isomerism also played a significant role in this effect. The mechanism of action of these compounds appears consistent with the notion that they generate either a quinone methide or an m-oxybenzyl zwitterion (or an m-hydroxybenzyl cation), which then reacts with a nucleophile, mediating their biological effect. Our SAR study provides an insight into the biological properties of this novel class of compounds and underscores their potential as anticancer agents.

  20. Structure-activity relationship study of novel anticancer aspirin-based compounds

    PubMed Central

    JOSEPH, STANCY; NIE, TING; HUANG, LIQUN; ZHOU, HUI; ATMAKUR, KRISHNAIAH; GUPTA, RAMESH C.; JOHNSON, FRANCIS; RIGAS, BASIL

    2013-01-01

    We performed a structure-activity relationship (SAR) study of a novel aspirin (ASA) derivative, which shows strong anticancer activity in vitro and in vivo. A series of ASA-based benzyl esters (ABEs) were synthesized and their inhibitory activity against human colon (HT-29 and SW480) and pancreatic (BxPC-3 and MIA PaCa-2) cancer cell lines was evaluated. The ABEs that we studied largely comprise organic benzyl esters bearing an ASA or acyloxy group (X) at the meta or para position of the benzyl ring and one of four different leaving groups. The nature of the salicyloyl/acyloxy function, the leaving group, and the additional substituents affecting the electron density of the benzyl ring, all were influential determinants of the inhibitory activity on cancer cell growth for each ABE. Positional isomerism also played a significant role in this effect. The mechanism of action of these compounds appears consistent with the notion that they generate either a quinone methide or an m-oxybenzyl zwitterion (or an m-hydroxybenzyl cation), which then reacts with a nucleophile, mediating their biological effect. Our SAR study provides an insight into the biological properties of this novel class of compounds and underscores their potential as anticancer agents. PMID:21805049

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

    PubMed

    Kim, Se H; Kim, Moon S; Lee, Bun Y; Lee, Pyung C

    2016-02-23

    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-α-tocopherol. 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 4,4'-diapotorulene on rat bone marrow mesenchymal stem cells. Our results demonstrate that a series of structurally novel carotenoids possessing biologically beneficial properties can be synthesized in E. coli.

  2. Biological effects related to geomagnetic activity and possible mechanisms.

    PubMed

    Krylov, Viacheslav V

    2017-06-21

    This review presents contemporary data on the biological effects of geomagnetic activity. Correlations between geomagnetic indices and biological parameters and experimental studies that used simulated geomagnetic storms to detect possible responses of organisms to these events in nature are discussed. Possible mechanisms by which geomagnetic activity influences organisms are also considered. Special attention is paid to the idea that geomagnetic activity is perceived by organisms as a disruption of diurnal geomagnetic variation. This variation, in turn, is viewed by way of a secondary zeitgeber for biological circadian rhythms. Additionally, we discuss the utility of cryptochrome as a biological detector of geomagnetic storms. The possible involvement of melatonin and protein coding by the CG8198 gene in the biological effects of geomagnetic activity are discussed. Perspectives for studying mechanisms by which geomagnetic storms affect organisms are suggested. Bioelectromagnetics. 2017;9999:1-14. © 2017 Wiley Periodicals, Inc. © 2017 Wiley Periodicals, Inc.

  3. Nitrogen-Containing Constituents of Black Cohosh: Chemistry, Structure Elucidation, and Biological Activities

    PubMed Central

    Lankin, David C.; Cisowska, Tamara; Chen, Shao-Nong; Pauli, Guido F.; van Breemen, Richard B.

    2016-01-01

    The roots/rhizomes of black cohosh (Actaea racemosa L. syn. Cimicifuga racemosa [L]. Nutt., Ranunculaceae) have been used traditionally by Native Americans to treat colds, rheumatism, and a variety of conditions related to women’s health. In recent years black cohosh preparations have become popular dietary supplements among women seeking alternative treatments for menopausal complaints. The popularity of the plant has led to extensive phytochemical and biological investigations, including several clinical trials. Most of the phytochemical and biological research has focused on two abundant classes of compounds: the triterpene glycosides and phenolic acids. A third group of phytoconstituents that has received far less attention consists of the alkaloids and related compounds that contain nitrogen. This chapter summarizes the current state of knowledge of the chemistry and biological activities associated with this group of constituents and provides some perspective on their significance for future research on this interesting plant. PMID:27795590

  4. Nitrogen-Containing Constituents of Black Cohosh: Chemistry, Structure Elucidation, and Biological Activities.

    PubMed

    Nikolić, Dejan; Lankin, David C; Cisowska, Tamara; Chen, Shao-Nong; Pauli, Guido F; van Breemen, Richard B

    2015-01-01

    The roots/rhizomes of black cohosh (Actaea racemosa L. syn. Cimicifuga racemosa [L]. Nutt., Ranunculaceae) have been used traditionally by Native Americans to treat colds, rheumatism, and a variety of conditions related to women's health. In recent years black cohosh preparations have become popular dietary supplements among women seeking alternative treatments for menopausal complaints. The popularity of the plant has led to extensive phytochemical and biological investigations, including several clinical trials. Most of the phytochemical and biological research has focused on two abundant classes of compounds: the triterpene glycosides and phenolic acids. A third group of phytoconstituents that has re