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Sample records for biologically active derivative

  1. Biological Activities of Hydrazone Derivatives

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    S. Güniz Küçükgüzel

    2007-08-01

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

  2. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    New substituted trichostatic acid derivatives have been synthesized and evaluated for their biological activities towards the H661 non-small lung cancer cell line. These syntheses were achieved by alkylation of propiophenones to introduce the side chain with a terminal precursor of hydroxamic acid and aminobenzamide ...

  3. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Administrator

    , although weaker zinc ligands than the hydroxamic acids, generally lead to bioactive molecules and pos- sess higher stability in biological environments. In this respect we prepared both hydroxamic acids and benzamide versions of the target ...

  4. Synthetic Approaches and Biological Activities of 4-Hydroxycoumarin Derivatives

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    Oee-Sook Park

    2009-11-01

    Full Text Available The main purpose of this review is to summarize recent chemical syntheses and structural modifications of 4-hydroxycoumarin and its derivatives, of interest due to their characteristic conjugated molecular architecture and biological activities.

  5. Biological activities of substituted trichostatic acid derivatives

    Indian Academy of Sciences (India)

    Administrator

    as 6-fluoro trichostatin A, with antiproliferative activities in the micromolar range and with histone deacetylase inhibitory activity. Keywords. Trichostatic acid; HDAC; inhibitor. 1. Introduction. Reversible chemical modifications of DNA and his- tones are important cellular events that promote activation or repression of DNA ...

  6. SYNTHESIS, REACTIVITY AND BIOLOGICAL ACTIVITY OF QUINOXALIN-2-ONE DERIVATIVES

    OpenAIRE

    El Mokhtar Essassi; R. Bouhfid; Y. Kandri Rodi; S. Ferfra; H. Benzeid; Y. Ramli

    2010-01-01

    Quinoxalines have a great interest in various fields and particularly in chemistry, biology and pharmacology. It enabled the researchers to develop many methods for their preparations and to seek new fields of application. In this review, we’ll expose different methods of synthesis of the quinoxalin-2-one, its reactivity and finally we’ll discuss the various biological activities of its derivatives.

  7. Biological activities of water-soluble fullerene derivatives

    Energy Technology Data Exchange (ETDEWEB)

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

    2009-04-01

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

  8. SYNTHESIS, REACTIVITY AND BIOLOGICAL ACTIVITY OF QUINOXALIN-2-ONE DERIVATIVES

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    El Mokhtar Essassi

    2010-04-01

    Full Text Available Quinoxalines have a great interest in various fields and particularly in chemistry, biology and pharmacology. It enabled the researchers to develop many methods for their preparations and to seek new fields of application. In this review, we’ll expose different methods of synthesis of the quinoxalin-2-one, its reactivity and finally we’ll discuss the various biological activities of its derivatives.

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

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    Lazić Anita M.

    2016-01-01

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

  10. Photoelectron spectra and biological activity of cinnamic acid derivatives revisited

    Science.gov (United States)

    Novak, Igor; Klasinc, Leo; McGlynn, Sean P.

    2018-01-01

    The electronic structures of several derivatives of cinnamic acid have been studied by UV photoelectron spectroscopy (UPS) and Green's function quantum chemical calculations. The spectra reveal the presence of dimers in the gas phase for p-coumaric and ferulic acids. The electronic structure analysis has been related to the biological properties of these compounds through the analysis of some structure-activity relationships (SAR).

  11. Facile Chemical Access to Biologically Active Norcantharidin Derivatives from Biomass

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    Konstantin I. Galkin

    2017-12-01

    Full Text Available Reductive amination of 2,5-diformylfuran (DFF was used to implement the transition from bio-derived 5-hydroxymethylfurfural (HMF to pharmaceuticals. The synthesized bis(aminomethylfurans were utilized as building blocks for the construction of new derivatives with structural cores of naturally occurring biologically active compounds. Using the one-pot procedure, which included the Diels–Alder reaction followed by hydrogenation of the double bond, bio-derived analogues of the anticancer drug norcantharidin were obtained. The cyclization process was diastereoselective, and resulted in the formation of tricyclic products with the endo configuration. Analysis of cytotoxycity for the resulting tricyclic amine-containing compounds showed an increase of anticancer activity as compared with the unsubstituted norcantharimide.

  12. Summary of diamino pyrazoles derived and study their biological activities

    International Nuclear Information System (INIS)

    Hagui, Marwa

    2016-01-01

    The work involves the synthesis of new heterocyclic structures diamino pyrazoles derivatives that are present in many natural products and products of pharmacological and therapeutic interests and study their biological activities. In order to develop a radiotracer interest and use in diagnostic nuclear medicine, we are interested to synthesis a pyrazole derivative with the precursor [Re(CO)5Br] and studying the antibacterial and antifungal activity of 3.5-diamino pyrazole and even thioamide complex rhenium. The objectives of our workout: 1/ Synthesis of molecules 3,5-diamino pyrazole and thioamide. 2/ Synthesis of 3,5-diamino pyrazole-rhenium complex. 3/ The in vitro study: Bacteriological Tests (Study of antibacterial and antifungal activity of 3,5-diamino pyrazole and thioamide). The first part of this work concerns the chemical synthesis of molecules such as: thioamide, Amp z1 Ampz2 and then we had synthesized the complex 3,5-diamino pyrazole-rhenium. Similarly we determined the physicochemical characteristics of the compounds synthesized by CLHP, CCM and RMN ( 1 H, 13 C). The second part is devoted to the study in vitro of biological activities of the synthesized molecules and complex 3,5 diaminopyrazole-rhenium with concentration 1 mg/mL and 2 mg/mL. The results allow us to say that the thioamide and Ampz2 have antibacterial activity against S. enterica and Ampz2 has low activity against S. aureus and P. aeruginossa. Other pyrazole derivatives have no significant antibacterial and antifungal activity. The results also show that the synthesized compounds of concentration 2 mg/mL in relation to the inhibition zones of amoxicillin and DMSO: 1/ Escherichia coli, there is antibacterial activity for thioamide, and the Amp z1-Re Ampz2 compound. 2/ Staphylococcus aureus, the complex Ampz 1-Re and the thioamide have significant antibacterial activity. 3/ Salmonella, we observe that the thioamide molecules, Ampz2 and Amp z1-Re have significant antibacterial activity

  13. New enamine derivatives of lapachol and biological activity.

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    Oliveira, Mailcar F; Lemos, Telma G; de Mattos, Marcos C; Segundo, Taciana A; Santiago, Gilvandete M P; Braz-Filho, Raimundo

    2002-06-01

    A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione, 2-(1-piperidinyl)-3-(3-methyl-2-butenyl)-1,4-naphtalenedione and 2-(1-pyrrolidinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (lapachol) and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

  14. New enamine derivatives of lapachol and biological activity

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    OLIVEIRA MAILCAR F.

    2002-01-01

    Full Text Available A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl-3-(3-methyl-2-butenyl-1,4-naphthalenedione, 2-(1-piperidinyl-3-(3-methyl-2-butenyl-1,4-naphtalenedione and 2-(1-pyrrolidinyl-3-(3-methyl-2-butenyl-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl-1,4-naphthalenedione (lapachol and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

  15. Biological activities of triazine derivatives. Combining DFT and QSAR results

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    Majdouline Larif

    2017-02-01

    Full Text Available In order to investigate the relationship between activities and structures, a 3D-QSAR study is applied to a set of 43 molecules based on triazines. This study was conducted using the principal component analysis (PCA method, the multiple linear regression method (MLR and the artificial neural network (ANN. The predicted values of activities are in good agreement with the experimental results. The artificial neural network (ANN techniques, considering the relevant descriptors obtained from the MLR, showed a correlation coefficient of 0.9 with an 8-3-1 ANN model which is a good result. As a result of quantitative structure–activity relationships, we found that the model proposed in this study is constituted of major descriptors used to describe these molecules. The obtained results suggested that the proposed combination of several calculated parameters could be useful to predict the biological activity of triazine derivatives.

  16. Synthesis and biological activities of turkesterone 11?-acyl derivatives

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    Laurence Dinan

    2003-02-01

    Full Text Available Turkesterone is a phytoecdysteroid possessing an 11alpha-hydroxyl group. It is an analogue of the insect steroid hormone 20-hydroxyecdysone. Previous ecdysteroid QSAR and molecular modelling studies predicted that the cavity of the ligand-binding domain of the ecdysteroid receptor would possess space in the vicinity of C-11/C-12 of the ecdysteroid. We report the regioselective synthesis of a series of turkesterone 11alpha-acyl derivatives in order to explore this possibility. The structures of the analogues have been unambiguously determined by spectroscopic means (NMR and low-resolution mass spectrometry. Purity was verified by HPLC. Biological activities have been determined in Drosophila melanogaster BII cell-based bioassay for ecdysteroid agonists and in an in vitro radioligand-displacement assay using bacterially expressed D. melanogaster EcR/USP receptor proteins. The 11alpha-acyl derivatives do retain a significant amount of biological activity relative to the parent ecdysteroid. Further, although activity initially drops with the extension of the acyl chain length (C2 to C4, it then increases (C6 to C10, before decreasing again (C14 and C20. The implications of these findings for the interaction of ecdysteroids with the ecdysteroid receptor and potential applications in the generation of affinity-labelled and fluorescently-tagged ecdysteroids are discussed.

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

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    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.

  18. Anthraquinones and Derivatives from Marine-Derived Fungi: Structural Diversity and Selected Biological Activities.

    Science.gov (United States)

    Fouillaud, Mireille; Venkatachalam, Mekala; Girard-Valenciennes, Emmanuelle; Caro, Yanis; Dufossé, Laurent

    2016-03-25

    Anthraquinones and their derivatives constitute a large group of quinoid compounds with about 700 molecules described. They are widespread in fungi and their chemical diversity and biological activities recently attracted attention of industries in such fields as pharmaceuticals, clothes dyeing, and food colorants. Their positive and/or negative effect(s) due to the 9,10-anthracenedione structure and its substituents are still not clearly understood and their potential roles or effects on human health are today strongly discussed among scientists. As marine microorganisms recently appeared as producers of an astonishing variety of structurally unique secondary metabolites, they may represent a promising resource for identifying new candidates for therapeutic drugs or daily additives. Within this review, we investigate the present knowledge about the anthraquinones and derivatives listed to date from marine-derived filamentous fungi's productions. This overview highlights the molecules which have been identified in microorganisms for the first time. The structures and colors of the anthraquinoid compounds come along with the known roles of some molecules in the life of the organisms. Some specific biological activities are also described. This may help to open doors towards innovative natural substances.

  19. Anthraquinones and Derivatives from Marine-Derived Fungi: Structural Diversity and Selected Biological Activities

    Directory of Open Access Journals (Sweden)

    Mireille Fouillaud

    2016-03-01

    Full Text Available Anthraquinones and their derivatives constitute a large group of quinoid compounds with about 700 molecules described. They are widespread in fungi and their chemical diversity and biological activities recently attracted attention of industries in such fields as pharmaceuticals, clothes dyeing, and food colorants. Their positive and/or negative effect(s due to the 9,10-anthracenedione structure and its substituents are still not clearly understood and their potential roles or effects on human health are today strongly discussed among scientists. As marine microorganisms recently appeared as producers of an astonishing variety of structurally unique secondary metabolites, they may represent a promising resource for identifying new candidates for therapeutic drugs or daily additives. Within this review, we investigate the present knowledge about the anthraquinones and derivatives listed to date from marine-derived filamentous fungi′s productions. This overview highlights the molecules which have been identified in microorganisms for the first time. The structures and colors of the anthraquinoid compounds come along with the known roles of some molecules in the life of the organisms. Some specific biological activities are also described. This may help to open doors towards innovative natural substances.

  20. Synthesis of some new hydrazone derivatives as biologically active agents.

    Science.gov (United States)

    Sen Gupta, A K; Rastogi, A

    1986-05-01

    A series of [4-(6H/bromo-4-oxo-2-phenyl-3(4H)-quinazolinyl)phenoxy]acetic acid (1,2-dihydro-1-H/methyl-2-oxo-3H-indol-3-ylidene)hydrazides (VII1-16) were synthesised by condensing 1-H/methyl-5-substituted indoline-2,3-diones with [4-(6H/bromo-4-oxo-2-phenyl-3(4H)-quinazolinyl) phenoxy]acetic acid hydrazides (IV1-2) which in turn were obtained by reacting ethyl [4-(6H/bromo-4-oxo-2-phenyl-3(4H)-quinazolinyl)phenoxy]acetates (III1-2) with hydrazine hydrate. All the synthesised compounds (VIII1-16) were screened for their antibacterial, acetylcholinesterase enzyme inhibitory and antiviral activities.

  1. Synthesis and biological evaluation of arctigenin ester and ether derivatives as activators of AMPK.

    Science.gov (United States)

    Shen, Sida; Zhuang, Jingjing; Chen, Yijia; Lei, Min; Chen, Jing; Shen, Xu; Hu, Lihong

    2013-07-01

    A series of new arctigenin and 9-deoxy-arctigenin derivatives bearing different ester and ether side chains at the phenolic hydroxyl positions are designed, synthesized, and evaluated for activating AMPK potency in L6 myoblasts. Initial biological evaluation indicates that some alkyl ester and phenethyl ether arctigenin derivatives display potential activities in AMPK phosphorylation improvement. Further structure-activity relationship analysis shows that arctigenin ester derivatives 3a, 3h and 9-deoxy-arctigenin phenethyl ether derivatives 6a, 6c, 6d activate AMPK more potently than arctigenin. Moreover, the 2-(3,4-dimethoxyphenyl)ethyl ether moiety of 6c has been demonstrated as a potential functional group to improve the effect of AMPK phosphorylation. The structural optimization of arctigenin leads to the identification of 6c as a promising lead compound that exhibits excellent activity in AMPK activation. Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

  2. synthesis and characterization of some poly functionalized heterocyclic derivatives of expected biological activity

    International Nuclear Information System (INIS)

    El-sayed, M.S.

    2001-01-01

    The present work was aimed and designed to fulfil The following objectives : 1- Continuation of the effort done by our research group in the field of chemistry of pyridinethione derivatives and their biological activities. 2- Synthesis of several new heterocyclic derivatives containing N and/or S using the laboratory available reagents. 3- Establishment of the structures of the newly synthesized heterocyclic compounds by the data of IR, 1 H-NMR, mass spectra in addition to the elemental analysis. 4- Synthesis of some of these heterocyclic derivatives via alternative routs and this used as a tool to confirm the structures of the newly synthesized heterocyclic derivatives. 5- study of the most probable mechanisms leading to the formation of the new heterocyclic derivatives. 6- The antimicrobial activity of some of the newly synthesized heterocyclic derivatives was tested against several types of organisms

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

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    Martin J. G. Hébert

    2015-01-01

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

  4. Design and synthesis of a new steroid-macrocyclic derivative with biological activity.

    Science.gov (United States)

    López-Ramos, Maria; Figueroa-Valverde, Lauro; Herrera-Meza, Socorro; Rosas-Nexticapa, Marcela; Díaz-Cedillo, Francisco; García-Cervera, Elodia; Pool-Gómez, Eduardo; Cahuich-Carrillo, Regina

    2017-04-01

    The aims of this study were to evaluate the positive inotropic effect of a new macrocyclic derivative (compound 11 ) and characterize the molecular mechanism involved in its biological activity. The first step was achieved by synthesis of a macrocyclic derivative involving a series of reactions for the preparation of several steroid derivatives such as (a) steroid-pyrimidinone ( 3 and 4 ), (b) steroid-amino ( 5 ), (c) steroid-imino ( 6 ), (d) ester-steroid ( 7 and 8 ), and (e) amido-steroid ( 9 and 10 ). Finally, 11 was prepared by removing the tert -butyldimethylsilane fragment of 10 . The biological activity of compounds on perfusion pressure and vascular resistance was evaluated on isolated rat heart using the Langendorff model. The inotropic activity of 11 was evaluated in presence of prazosin, metoprolol, indomethacin, nifedipine, and flutamide to characterize its molecular mechanism. Theoretical experiments were carried out with a Docking model, to assess potential interactions of androgen receptor with 11 . The results showed that only this macrocyclic derivative exerts changes on perfusion pressure and vascular resistance translated as the positive inotropic effect, and this effect was blocked with flutamide; these data indicate that the positive inotropic activity induced by this macrocyclic derivative was via androgen receptor activation. The theoretical results indicated that the interaction of the macrocyclic derivative with the androgen receptor involves several amino acid residues such as Leu 704 , Asn 705 , Met 780 , Cys 784 , Met 749 , Leu 762 , Phe 764 , Ser 778 , and Met 787 . In conclusion, all these data suggest that the positive inotropic activity of the macrocyclic derivative may depend on its chemical structure.

  5. Physiochemical, optical and biological activity of chitosan-chromone derivative for biomedical applications.

    Science.gov (United States)

    Kumar, Santosh; Koh, Joonseok

    2012-01-01

    This paper describes the physiochemical, optical and biological activity of chitosan-chromone derivative. The chitosan-chromone derivative gels were prepared by reacting chitosan with chromone-3-carbaldehyde, followed by solvent exchange, filtration and drying by evaporation. The identity of Schiff base was confirmed by UV-Vis absorption spectroscopy and Fourier-transform infrared (FTIR) spectroscopy. The chitosan-chromone derivative was evaluated by X-ray diffraction (XRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photoluminescence (PL) and circular dichroism (CD). The CD spectrum showed the chitosan-chromone derivative had a secondary helical structure. Microbiological screening results demonstrated the chitosan-chromone derivative had antimicrobial activity against Escherichia coli bacteria. The chitosan-chromone derivative did not have any adverse effect on the cellular proliferation of mouse embryonic fibroblasts (MEF) and did not lead to cellular toxicity in MEFs. These results suggest that the chitosan-chromone derivative gels may open a new perspective in biomedical applications.

  6. Synthesis and reactions of some biologically active 2-(2'-thienyl)benzoxazinone and quinazolinone derivatives.

    Science.gov (United States)

    el-Khamry, A M; el-Nagdy, S; Habashy, M M; el-Bassiouny, F A

    1989-05-01

    Different amines were found to attack the hitherto unknown 6,8-dibromo-2-(2'-thienyl)-3,1-benzoxazin-4(H)-one (2) entirely at position-4, producing the corresponding benzamide derivatives 3a-i. Compound 2 reacted with hydrazoic acid affording the tetrazole 5, beside the benzimidazole derivative 6. Similarly carbon nucleophiles, such as ethyl acetoacetate attack 2 to give 7. 6,8-Dibromo-2(2'-thienyl)-4(3H)-quinazoline and its 3-substituted derivatives 8 a-g were also synthesized. Theoretical calculations for the benzoxazinone 2 and others, based on the simple HMO-method were performed. Close accordance between the theoretically predicted reactivities and the experimental findings was obtained. Biological activities of some of the compounds obtained were also tested.

  7. Synthesis of the ensembles from succinylated interleukin-2 derivatives and their biological activity in vitro

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    Artur Martynov

    2015-11-01

    Full Text Available Purpose: The biological activity (direct anticancer action in vitro of combinatorial IL-2 succinylated derivatives was examined. Acylation of IL-2 was performed using succinic anhydride with various levels of acylation, with the formation of a complex assembly of many derivatives (self-assembled quasi-living structure.Methods: In the study, we used recombinant interleukin-2 (IL-2 (Ronkoleukin, Russia in oxidizing form and other reagents from Sigma-Aldrich and Fluka (USA. For acylation, recombinant IL-2 in the form of a matrix fluid with a protein concentration of 0.6 mg/ml was used. The IL-2 matrix solution was brought to a pH of 8.0 through the addition of a 0.01% solution of sodium hydroxide. The synthesized ensemble of succinyl-IL-2 was analyzed using the capillary gel electrophoresis method in an Agilent-2100 bioanalyzer. The molecular masses of the synthesized ensemble were established in comparison to standard samples of low-molecular proteins with known molecular masses that were part of the bioanalyzer’s collection. The additional negative charge of the modified IL-2 was determined by a FPLC (Fast Protein Liquid Chromatography system from Pharmacia (Woerden, Netherlands. CTLL-2, a murine IL-2-dependent cell line, was obtained fromBiokontrol (Kiev, Ukraine. These respondingcells were used in proliferative assays comparing the activityof the IL-2 and succinylated IL-2 derivatives to the WHO InternationalStandard. For statistical data analysis, the one-way ANOVA was used.Results: After treatment with Suc-IL-2, BTL were studied in vitro on the CTLL-2 cell line, dose-dependently, in a BTL induction reaction. The highest level of biological activity in acylated IL-2 was observed in Suc-IL-2 with four modified lysine residues. In conclusion, succinylated IL-2 with four substituted lysines may be useful as a prospective anticancer agent.Conclusions: Ten-fold increase in the biological activity of IL-2 was observed after partial succinylation

  8. Coordination chemistry and biological activity of 5'-OH modified quinoline-B12 derivatives.

    Science.gov (United States)

    Zelenka, Karel; Brandl, Helmut; Spingler, Bernhard; Zelder, Felix

    2011-10-14

    The consequences of structural modifications at the 5'-OH ribofuranotide moiety of quinoline modified B12 derivatives are discussed in regard of the coordination chemistry, the electrochemical properties and the biological behaviour of the compound.

  9. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties

    Science.gov (United States)

    2013-03-19

    Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4- Triazole Moieties Bedia Kocyigit-Kaymakcioglu 1,*, Ahmet Ozgur Celen...of novel thiourea and urea derivatives containing 1,2,4- triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity... Triazole derivatives 3a–e and 4a–e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a–e and 2a–e, respectively

  10. Use of Brevibacillus choshinensis for the production of biologically active brain-derived neurotrophic factor (BDNF).

    Science.gov (United States)

    Angart, Phillip A; Carlson, Rebecca J; Thorwall, Sarah; Patrick Walton, S

    2017-07-01

    Brain-derived neurotrophic factor (BDNF) is a member of the neurotrophin family critical for neuronal cell survival and differentiation, with therapeutic potential for the treatment of neurological disorders and spinal cord injuries. The production of recombinant, bioactive BDNF is not practical in most traditional microbial expression systems because of the inability of the host to correctly form the characteristic cystine-knot fold of BDNF. Here, we investigated Brevibacillus choshinensis as a suitable expression host for bioactive BDNF expression, evaluating the effects of medium type (2SY and TM), temperature (25 and 30 °C), and culture time (48-120 h). Maximal BDNF bioactivity (per unit mass) was observed in cultures grown in 2SY medium at extended times (96 h at 30 °C or >72 h at 25 °C), with resulting bioactivity comparable to that of a commercially available BDNF. For cultures grown in 2SY medium at 25 °C for 72 h, the condition that led to the greatest quantity of biologically active protein in the shortest culture time, we recovered 264 μg/L of BDNF. As with other microbial expression systems, BDNF aggregates did form in all culture conditions, indicating that while we were able to recover biologically active BDNF, further optimization of the expression system could yield still greater quantities of bioactive protein. This study provides confirmation that B. choshinensis is capable of producing biologically active BDNF and that further optimization of culture conditions could prove valuable in increasing BDNF yields.

  11. Synthesis, biological evaluation, QSAR analysis, and molecular docking of chalcone derivatives for antimalarial activity

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    Jufrizal Syahri

    2017-01-01

    Full Text Available Objective: To synthesize chalcone derivatives and investigate their antimalarial activity toward chloroquine-sensitive Plasmodium falciparum 3D7 (Pf3D7 strain; to develop quantitative structureactivity relationships (QSAR model to estimate IC50 values for biological activity of antimalarial and compared to experimental measurement; and to determine the binding interactions of the most active compounds with targeting P. falciparum dihydrofolate reductase-thymidylate synthase using molecular docking simulation. Methods: Seven chalcone derivatives have been synthesized from substituted acetophenone and substituted benzaldehyde in ethanol with the presence of bases catalysis at reflux condition. The QSAR analysis was conducted by using Gaussian 09 software to predict IC50 value for antimalarial activity. The in vitro test was evaluated against the chloroquine-sensitive Pf3D7 strain. Finally, the docking studies were performed with the CDOCKER protocol under the receptor-ligand interaction section in Discovery Studio® 3.1 (Accelrys, Inc., San Diego, USA. Results: Among the synthesized chalcone, a prenylated chalcone 5c and an allylated chalcones 10a showed the best IC 50 values of 1.08 and 1.73 μg/mL respectively against Pf3D7 strain (1.37 and 2.33 μg/mL based on QSAR analysis. Comparison between the prediction of IC50 value generated from the QSAR and the outcome from an in vitro assay showed a similar result as seen from the r2 value (r2 = 0.99. The most active compound 5c was employed in the docking simulation to determine the potential binding interactions with active sites of P. falciparum dihydrofolate reductase-thymidylate synthase (protein data bank ID: 1J3I. The docking simulation study showed 5c bind well with Ala16, Ser108, Ile164, Trp48, and Phe58 which are the crucial interactions that could possibly interrupt the sequential catalysis reactions in the thymidylate cycle and subsequently prevent deoxythymidine monophosphate production

  12. Synthesis, Spectroscopic Characterization and Biological Activities of Transition Metal Complexes Derived from a Tridentate Schiff Base

    Directory of Open Access Journals (Sweden)

    J. Senthil Kumaran

    2013-01-01

    Full Text Available A new series of Cu (II, Ni (II, Co (II and Zn (II complexes have been synthesized from the Schiff base derived from 4-hydroxy-3-methoxybenzylidine-4-aminoantipyrine and 2-aminophenol. The structural features have been determined from their elemental analysis, magnetic susceptibility, molar conductance, Mass, IR, UV-Vis, 1H-NMR, 13C-NMR and ESR spectral studies. The redox behavior of the copper complex has been studied by cyclic voltammetry. The data confirm that the complexes have composition of ML2 type. The electronic absorption spectral data of the complexes propose an octahedral geometry around the central metal ion. All the metal complexes with DNA structure were guided by the presence of inter-molecular C–H⋯O and C–H⋯N hydrogen bonds. The biological activity of the synthesized compounds were tested against the bacterial species such as Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris and fungal species such as Candida albicans by the well-diffusion method.

  13. Synthesis, structure combined with conformational analysis, biological activities and docking studies of bis benzylidene cyclohexanone derivatives

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    Gehad Lotfy

    2017-07-01

    Full Text Available We report the synthesis and biological evaluation of bis benzylidne cyclohexanone derivatives 2,6-di(4-fluorobenzylidenecyclohexanone 3a and (2E,6E‐2,6‐bis({[4‐(trifluoromethylphenyl]methylidene}cyclohexanone 3b. Compound 3b crystallized in the monoclinic space group P21/n with unit cell parameters a = 29.3527(12 Å, b = 8.3147(3 Å, c = 32.7452(14 Å, β = 112.437(2°, and V = 7386.8(5 Å3, Z = 16, and Rint = 0.072 at T = 100 K. The asymmetric unit contains four independent molecules, each of which has slight differences in the bond lengths and angles. One non-classical C11D–H11F⋯F3A hydrogen bond connects the molecules. Density functional theory was used to optimize the structures and calculate the natural charges, dipole moments, frontier molecular orbitals, and NMR and UV–Vis spectroscopic properties, which are discussed and compared with the experimental data. The synthetic derivatives were evaluated for α-glucosidase inhibitory activity, and we found that compound 3a (IC50 = 96.3 ± 0.51 μM is a potent α-glucosidase inhibitor, showing superior activity to the standard drug acarbose (IC50 = 841 ± 1.73 μM. Compound 3b (IC50 = 7.92 ± 1.3 μg/mL was found to be a potent antileishmanial compound, especially compared to the antileishmanial drugs pentamidine (IC50 = 5.09 ± 0.04 μM and amphotericine B (IC50 = 0.29 ± 0.05 μg/mL. In addition, 3a and 3b have cytotoxic effects against PC3 (prostate cancer, HeLa (cervical cancer, and MCF-3 (breast cancer cell lines. Docking study for compounds activity was performed with Openeye software in order to understanding their pose of interaction in the target receptors.

  14. Biological activity, quantitative structure–activity relationship analysis, and molecular docking of xanthone derivatives as anticancer drugs

    Science.gov (United States)

    Miladiyah, Isnatin; Jumina, Jumina; Haryana, Sofia Mubarika; Mustofa, Mustofa

    2018-01-01

    Background Xanthone derivatives have a wide range of pharmacological activities, such as those involving antibacterial, antiviral, antimalarial, anthelmintic, anti-inflammatory, antiprotozoal, and anticancer properties. Among these, we investigated the anticancer properties of xanthone. This research aimed to analyze the biological activity of ten novel xanthone derivatives, to investigate the most contributing-descriptors for their cytotoxic activities, and to examine the possible mechanism of actions of xanthone compound through molecular docking. Materials and methods The cytotoxic tests were carried out on WiDR and Vero cell lines, by a 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay method. The structural features required for xanthone’s anticancer activity were conducted by using the semi-empirical Austin Model-1 method, and continued with quantitative structure-activity relationship (QSAR) analysis using BuildQSAR program. The study of the possible mechanism of actions of the selected xanthone compound was done through molecular docking with PLANTS. Results The three novel xanthone derivatives (compounds 5, 7, and 8) exhibited cytotoxic activity with compound 5 showed the highest degree of cytotoxicity at concentration 9.23 µg/mL (37.8 µM). The following best equation model was obtained from the BuildQSAR calculation: log 1/IC50 = −8.124 qC1 −35.088 qC2 −6.008 qC3 + 1.831 u + 0.540 logP −9.115 (n = 10, r = 0.976, s = 0.144, F = 15.920, Q2 = 0.651, SPRESS = 0.390). This equation model generated 15 proposed new xanthone compounds with better-predicted anticancer activities. A molecular docking study of compound 5 showed that xanthone formed binding interactions with some receptors involved in cancer pathology, including telomerase, tumor-promoting inflammation (COX-2), and cyclin-dependent kinase-2 (CDK2) inhibitor. Conclusion The results suggested that compound 5 showed the best cytotoxic activity among the xanthone

  15. Synthesis and Biological Activity of Some 3,5-Diaryl-1-Benzothiazolopyrazoline Derivatives: Reaction of Chalcones with 2-Hyrazinobenzothiazoles

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    Vandana Sharma

    2009-01-01

    Full Text Available A series of 3,5-diaryl-1-benzothiazolopyrazoline derivatives were synthesized by the reaction of appropriately substituted chalcones and 2-hydrazinobenzothiazole in ethanol. The synthesized heterocycles have been characterized on the basis of their chemical properties and spectroscopic data. These compounds were tested for biological activity against a variety of test organisms.

  16. Synthesis and Biological Activity of Some 3, 5-Diarylisoxazoline Derivatives: Reaction of Substituted Chalcones with Hydroxylamine Hydrochloride

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    Vandana Sharma

    2010-01-01

    Full Text Available A series of 3-aryl-5-styrylisoxazoline/ 3,5-diarylisoxazoline derivatives were synthesized by the reaction of appropriately substituted chalcones and hydroxylamine hydrochloride in presence of alkali in ethanol. The synthesized heterocycles have been characterized on the basis of their chemical properties and spectroscopic data. These compounds were tested for biological activity against a variety of test organisms

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

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    Yasmeen Gull

    2016-02-01

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

  18. Biological activities of novel derivatives of DIF-1 isolated from Dictyostelium.

    Science.gov (United States)

    Kikuchi, Haruhisa; Ishiko, Shinya; Oshima, Yoshiteru; Gokan, Naomi; Hosaka, Kohei; Kubohara, Yuzuru

    2008-12-19

    The differentiation-inducing factor-1 (DIF-1) is a lipophilic signal molecule (chlorinated alkylphenone) that induces stalk cell differentiation in the cellular slime mold Dictyostelium discoideum. In addition, DIF-1 and its derivatives have been shown to possess anti-leukemic activity and glucose consumption-promoting activity in vitro in mammalian cells. In this study, to assess the chemical structure-effect relationship of DIF-1, we synthesized eight derivatives of DIF-1 and investigated their stalk cell-inducing activity in Dictyostelium cells and pharmacological activities in mammalian cells. Of the derivatives, two amide derivatives of DIF-1, whose hydrophobic indexes are close to that of DIF-1, induced stalk cell differentiation as strongly as DIF-1 in Dictyostelium cells. It was also found that some derivatives suppressed cell growth in human K562 leukemia cells and promoted glucose consumption in mouse 3T3-L1 cells. These results give us valuable information as to the chemical structure-effect relationship of DIF-1.

  19. Oleanolic Acid and Its Derivatives: Biological Activities and Therapeutic Potential in Chronic Diseases

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    Taiwo Betty Ayeleso

    2017-11-01

    Full Text Available The increasing demand for natural products as an alternative therapy for chronic diseases has encouraged research into the pharmacological importance of bioactive compounds from plants. Recently, there has been a surge of interest in the therapeutic potential of oleanolic acid (OA in the prevention and management of chronic diseases. Oleanolic acid is a pentacyclic triterpenoid widely found in plants, including fruits and vegetables with different techniques and chromatography platforms being employed in its extraction and isolation. Several studies have demonstrated the potential therapeutic effects of OA on different diseases and their symptoms. Furthermore, oleanolic acid also serves as a framework for the development of novel semi-synthetic triterpenoids that could prove vital in finding therapeutic modalities for various ailments. There are recent advances in the design and synthesis of chemical derivatives of OA to enhance its solubility, bioavailability and potency. Some of these derivatives have also been therapeutic candidates in a number of clinical trials. This review consolidates and expands on recent reports on the biological effects of oleanolic acid from different plant sources and its synthetic derivatives as well as their mechanisms of action in in vitro and in vivo study models. This review suggests that oleanolic acid and its derivatives are important candidates in the search for alternative therapy in the treatment and management of chronic diseases.

  20. The presence of food-derived collagen peptides in human body-structure and biological activity.

    Science.gov (United States)

    Sato, Kenji

    2017-12-13

    It has been demonstrated that the ingestion of some protein hydrolysates exerts health-promoting effects. For understanding the underlying mechanisms responsible for these effects, the identification of bioactive peptides in the target organ is crucial. For this purpose, in vitro activity-guided fractionation for peptides in the protein hydrolysate has been performed. However, the peptides in the hydrolysate may be further degraded during digestion. The concentration of the active peptides, which were identified by in vitro activity-guided fractionation, in human blood is frequently very low (nanomolar levels). In contrast, micromolar levels of food-derived collagen peptides are present in human blood. Pro-Hyp, one of the major food-derived collagen peptides, enhances the growth of fibroblasts and synthesis of hyaluronic acid. These observations partially explain the beneficial effects of collagen hydrolysate ingestion on the enhancement of wound healing and improvement in the skin condition. The recent advancement involving liquid chromatography and mass spectrometry coupled with a pre-column derivatization technique has enabled the identification of food-derived peptides at nanomolar levels in the body post-ingestion of protein hydrolysates. Thus, this technique can be used for the identification of bioactive food-derived peptides in the body.

  1. Opuntia ficus indica peel derived pectin mediated hydroxyapatite nanoparticles: Synthesis, spectral characterization, biological and antimicrobial activities

    Science.gov (United States)

    Gopi, D.; Kanimozhi, K.; Kavitha, L.

    2015-04-01

    In the present study, we have adapted a facile and efficient green route for the synthesis of HAP nanoparticles using pectin as a template which was extracted from the peel of prickly pear (Opuntia ficus indica) fruits. The concentration of pectin plays a major role in the behavior of crystallinity, purity, morphology as well as biological property of the as-synthesized HAP nanoparticles. The extracted pectin and the as-synthesized nanoparticles were characterized by various analytical techniques. The in vitro apatite formation on the surface of the as-synthesized nanoparticles in simulated body fluid (SBF) for various days showed an enhanced bioactivity. Also, the antimicrobial activity was investigated using various microorganisms. All the results revealed the formation of pure, low crystalline and discrete granular like HAP nanoparticles of size around 25 nm with enhanced biological and antimicrobial activities. Hence the as-synthesized nanoparticles can act as a better bone regenerating material in the field of biomedicine.

  2. Synthesis, Reactivity and Biological Activity of Novel Bisbenzofuran-2-yl-Methanone Derivatives

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    Cavit Kazaz

    2005-11-01

    Full Text Available Preparation of bisbenzofuran-2-yl-methanone (1, the corresponding ketoxime 4, semicarbazone and thiosemicarbazone 3a and 3b, ether derivatives of the ketoximes 5a-j and the alcohol 2 are described. These substances have been prepared in excellent yields. All the synthesized compounds except 5i have been tested against five different microorganisms and some of them were found to be active against some of the species studied.

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

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    Atalla, M. M.

    2008-01-01

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

  4. Synthesis and biological activity of some new pyrazoline and pyrimidine derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Hassan, Seham Y. [University of Alexandria (Egypt). Faculty of Science. Dept. of Chemistry

    2011-07-01

    New series of pyrazoline 3-aryl-4,5-dihydro-1H-pyrazole-1-carbaldehydes (4-6), (aryl-4,5- dihydro-1H-pyrazol-1-yl)ethanones (9-11) and 3-aryl-4,5-dihydro-1H-pyrazoles (24 and 25) were synthesized by reacting chalcones (1-3) with hydrazine hydrate in either formic acid, acetic acid or ethanol, respectively. Also, new 6-arylpyrimidin-2-amine derivatives (32-34) were synthesized from the same chalcones. The structures of the newly synthesized compounds were established on the basis of IR, {sup 1}H NMR, {sup 13}C NMR, mass spectral data and elemental analyses. The compounds were evaluated for their antibacterial and antifungal activities. Three heterocycles showed relevant activity against C. albicans and some compounds also showed activity against E. coli. (author)

  5. Synthesis and Spectroscopic Characterization of Some New Biological Active Azo–Pyrazoline Derivatives

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    Farouq E. Hawaiz

    2012-01-01

    Full Text Available A number of 3-[4-(benzyloxy-3-(2-Chlorophenylazo-phenyl]-5-(substituted-phenyl-1-substituted-2-pyrazolines( 4a-j and (5a-j have been synthesized by diazotization of 2-chloroaniline and its coupling reaction with 4-hydroxy acetophenone, followed by benzyloxation of the hydroxyl group to give the substrate [4-benzyloxy-3-(2-chlorophenylazo-acetophenone (1].The prepared starting material (1 has been reacted with different substituted benzaldehydes to give a new series of chalcone derivatives 1-[(4-benzyloxy-3-(2-chloro-phenylazo-phenyl]-3-(substituted phenyl-2-propen-1-one (3a-j, in high yields and in a few minutes, and the later compounds were treated with hydrazine hydrate according to Michael addition reaction to afford a new biolological active target compounds (4a-j and (5a-j. Furthermore, The structures of the newly synthesized compounds were confirmed by FT-IR, 13C-NMR,13C-DEPT & 1H-NMR spectral data. The chalcone and pyrazoline derivatives were evaluated for their anti bacterial activity against Escherichia coli as gram negative and Staphylococcus aureus as gram positive, the results showed significant activity against both types of bacteria.

  6. Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity.

    Science.gov (United States)

    Martins, Filomena; Santos, Susana; Ventura, Cristina; Elvas-Leitão, Ruben; Santos, Lídia; Vitorino, Susana; Reis, Marina; Miranda, Vanessa; Correia, Henrique F; Aires-de-Sousa, João; Kovalishyn, Vasyl; Latino, Diogo A R S; Ramos, Jorge; Viveiros, Miguel

    2014-06-23

    The disturbing emergence of multidrug-resistant strains of Mycobacterium tuberculosis (Mtb) has been driving the scientific community to urgently search for new and efficient antitubercular drugs. Despite the various drugs currently under evaluation, isoniazid is still the key and most effective component in all multi-therapeutic regimens recommended by the WHO. This paper describes the QSAR-oriented design, synthesis and in vitro antitubercular activity of several potent isoniazid derivatives (isonicotinoyl hydrazones and isonicotinoyl hydrazides) against H37Rv and two resistant Mtb strains. QSAR studies entailed RFs and ASNNs classification models, as well as MLR models. Strict validation procedures were used to guarantee the models' robustness and predictive ability. Lipophilicity was shown not to be relevant to explain the activity of these derivatives, whereas shorter N-N distances and lengthy substituents lead to more active compounds. Compounds 1, 2, 4, 5 and 6, showed measured activities against H37Rv higher than INH (i.e., MIC ≤ 0.28 μM), while compound 9 exhibited a six fold decrease in MIC against the katG (S315T) mutated strain, by comparison with INH (i.e., 6.9 vs. 43.8 μM). All compounds were ineffective against H37RvINH (ΔkatG), a strain with a full deletion of the katG gene, thus corroborating the importance of KatG in the activation of INH-based compounds. The most potent compounds were also shown not to be cytotoxic up to a concentration 500 times higher than MIC. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  7. Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity.

    Science.gov (United States)

    Liu, Wenfeng; Li, Yonlian; Yue, Yuan; Zhang, Kun; Chen, Qian; Wang, Huaqian; Lu, Yujing; Huang, Mou-Tuan; Zheng, Xi; Du, Zhiyun

    2015-08-01

    Oral administration of nonsteroidal anti-inflammatory drugs (NSAIDs) was frequently associated with serious adverse effects. Inspired by curcumin-a naturally traditional Chinese medicine, a series of curcumin derivatives containing NSAIDs, used for transdermal application, were synthesized and screened for their anti-inflammatory activities in vitro and in vivo. Compared with curcumin and parent NSAID (salicylic acid and salsalate), topical application of A11 and B13 onto mouse ear edema, prior to TPA treatment markedly suppressed the expression of IL-1β, IL-6 and TNF-α, respectively. Mechanistically, A11 and B13 blocked the phosphorylation of IκBα and suppressed the activation of p65 and IκBα. It was found that A11 and B13 may be potent anti-inflammatory agents for the treatment of inflammatory diseases. Copyright © 2015 Elsevier Ltd. All rights reserved.

  8. [Synthesis of phosphonic acid and phosphinic acid derivatives for development of biologically active compounds].

    Science.gov (United States)

    Shibuya, Shiroshi

    2004-11-01

    This paper covers recent publications from our laboratory on the synthesis of a variety of phosphonate and phosphinate derivatives. New methods for the enantioselective synthesis of alpha-hydroxyphosphonates were established by Lewis acid-mediated cleavage of homochiral 1,3-dioxaneacetals with P(OEt)(3) and chiral metal ligand-mediated hydrophosphonylation of aldehydes. Two diastereomers of HPmp derivatives were prepared by an application of these methods. The HPmp derivatives were convered to FPmp derivatives but with low diastereoselectivity. Hydrophosphonylation of alpha-aminoaldehydes afforded threo- and erythro-beta-amino-alpha-hydroxyphosphonates under chelation and nonchelation controlled conditions, respectively. The asymmetric dihydroxylation of alpha, beta-, and beta, gamma-unsaturated phosphonates with AD-mix-alpha and AD-mix-beta reagents gave alpha, beta- and beta, gamma-dihydroxyphosphonates with high enantioselectivity. The method was applied to the kinetic resolution of racemic alpha-oxygetated beta, gamma-unsaturated phosphonates. Treatment of allyloxymethylphosphonates with the base afforded alpha-hydroxyphosphonates via the [2,3]-Wittig reaction. Threo- and erythro-beta-amino-alpha-hydroxyphosphinates were obtained with high diastereoselectivity by phosphinylation of alpha-aminoaldehydes in the presence of (R)- and (S)-ALB, respectively. The phosphinylation of alpha-oxygenated aldehydes afforded the corresponding alpha, beta-dioxygenated phosphinates, but with low diastereoselectivity. Sphingomyelin analogues containing CF(2)PO(OH)(2) were synthesized starting from (S)- and (R)-Garner aldehyde for the purpose of obtaining potent sphyngomyelinase inhibitors. A useful method for the synthesis of alpha, alpha-difluorobenzylphosphonates was established based on the cross coupling reaction of an iodobenzene derivative with ZnCuBr(2)CF(2)PO(OEt)(2). The synthetic utility of ZnCuBr(2)CF(2)PO(OEt)(2) was examined to obtain alpha, alpha

  9. Novel topoisomerase I inhibitors. Syntheses and biological evaluation of phosphorus substituted quinoline derivates with antiproliferative activity.

    Science.gov (United States)

    Alonso, Concepción; Fuertes, María; Martín-Encinas, Endika; Selas, Asier; Rubiales, Gloria; Tesauro, Cinzia; Knudssen, Birgitta K; Palacios, Francisco

    2018-02-22

    This work describes the synthesis of 1,2,3,4-tetrahydroquinolinylphosphine oxides, phosphanes and phosphine sulfides as well as that of quinolinylphosphine oxides and phosphine sulfides, which were synthesized in good to high overall yield. The synthetic route involves a multicomponent reaction of (2-phosphine-oxide)-, 2-phosphine- or (2-phosphine-sulfide)-aniline, aldehydes and olefins and allows the selective generation of two stereogenic centres in a short, efficient and reliable synthesis. The selective dehydrogenation of 1,2,3,4-tetrahydroquinolinylphosphine oxides and phosphine sulfides leads to the formation of corresponding phosphorus substituted quinolines. Some of the products which were prepared showed excellent activity as topoisomerase I (Top1) inhibitors. In addition, prolonged effect of the most potent compounds is maintained with the same intensity even after 3 min of the beginning of the enzymatic reaction. The cytotoxic effect on cell lines derived from human lung adenocarcinoma (A549), human ovarian carcinoma (SKOV03) and human embryonic kidney (HEK293) was also screened. 1,2,3,4-Tetrahydroquinolinylphosphine oxide 6g with an IC 50 value of 0.25 ± 0.03 μM showed excellent activity against the A549 cell line in vitro, while 1,2,3,4-tetrahydroquinolinylphosphane 9c with an IC 50 value of 0.08 ± 0.01 μM and 1,2,3,4-tetrahydroquinolinylphosphine sulfide derivative 10f with an IC 50 value of 0.03 ± 0.04 μM are more active against the A549 cell line. Moreover, selectivity towards cancer cell (A549) over non-malignant cells (MRC5) has been observed. According to their structure, they may be excellent antiproliferative candidates. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  10. Synthesis, crystal structure, biological activity and theoretical calculations of novel isoxazole derivatives

    Science.gov (United States)

    Jin, R. Y.; Sun, X. H.; Liu, Y. F.; Long, W.; Chen, B.; Shen, S. Q.; Ma, H. X.

    2016-01-01

    Series of isoxazole derivatives were synthesized by substituted chalcones and 2-chloro-6-fluorobenzene formaldehyde oxime with 1,3-dipolar cycloaddition. The target compounds were determined by melting point, IR, 1H NMR, elemental analyses and HRMS. The crystal structure of compound 3a was detected by X-ray diffraction and it crystallizes in the triclinic space group p2(1)/c with z = 4. The molecular geometry of compound 3a was optimized using density functional theory (DFT/B3LYP) method with the 6-31G+(d,p) basis set in the ground state. From the optimized geometry of the molecule, FT-IR, FT-Raman, HOMO-LUMO and natural bond orbital (NBO) were calculated at B3LYP/6-31G+(d,p) level. Finally, the antifungal activity of the synthetic compounds were evaluated against Pythium solani, Gibberella nicotiancola, Fusarium oxysporium f.sp. niveum and Gibberella saubinetii.

  11. Biological activity of the azlactone derivative EPA-35 against Trypanosoma cruzi.

    Science.gov (United States)

    de Azeredo, Camila Maria Oliveira; Ávila, Eloah Pereira; Pinheiro, Danielle Lobo Justo; Amarante, Giovanni Wilson; Soares, Maurilio José

    2017-02-01

    Chagas disease, caused by Trypanosoma cruzi, affects six to seven million people worldwide. Treatment is based on benznidazole, producing several side effects and debatable efficacy, highlighting the need for new alternative drugs. We investigated the activity of four C-4 functionalized azlactone derivatives (EPA-27, EPA-35, EPA-63 and EPA-91) as potential T. cruzi inhibitors. Screening with epimastigotes indicated EPA-35 as the best compound (IC50/24 h: 33 μM). This compound was 14.1 times more potent against intracellular amastigotes (IC50/24 h: 2.34 μM). Treatment of infected Vero cells for 72 h (up to 30 μM EPA-35) resulted in a dose-dependent decrease in number of trypomastigotes and amastigotes released in the supernatant, but the amastigote/trypomastigote ratio remained constant, indicating that amastigote growth was disturbed, but cell differentiation was unaffected. Analysis of treated epimastigotes by flow cytometry indicated that the plasma membrane remained intact, but there was a significant decrease in mitochondrial membrane potential. The pattern of cell distribution in the cell cycle stages (G1, G2, M) was unaltered in treated epimastigotes, indicating a trypanocidal rather than a trypanostatic activity. Scanning electron microscopy and flow cytometry showed epimastigotes with a round shape and decrease in cell size. Taken together, our data indicate that the EPA-35 is effective against T. cruzi. Synthetic transformation of EPA-35 into other derivatives may provide promising compounds for further evaluation against this parasite. © FEMS 2017. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  12. A recyclable protein resource derived from cauliflower by-products: Potential biological activities of protein hydrolysates.

    Science.gov (United States)

    Xu, Yang; Li, Yuting; Bao, Tao; Zheng, Xiaodong; Chen, Wei; Wang, Jianxu

    2017-04-15

    Cauliflower by-products (CBP) are rich in leaf protein. Every year tons of CBP will lead to environmental pollution. Therefore, this study was conducted to extract leaf protein from CBP and investigate its biological activities. Our results showed that the optimal extraction parameters were: a liquid to solid ratio of 4mL/g, a pH of 11, an ultrasonic extraction lasting 15min, and at an applied power of 175W. Under these optimized conditions, 12.066g of soluble leaf protein (SLP) was obtained from 1000g of CBP and its extraction yield was 53.07%. The obtained SLP was further hydrolysed by Alcalase and the SLP hydrolysate (SLPH) showed a potent angiotensin I-converting enzyme (ACE) inhibitory activity with an IC 50 value of 138.545μg/mL in vitro. In addition, SLPH promoted the glucose consumption and enhanced the glycogen content in HepG2 cells. Overall, our results suggested that CBP may be recycled for designing future functional foods. Copyright © 2016 Elsevier Ltd. All rights reserved.

  13. Spectroscopic analysis on the binding interaction of biologically active pyrimidine derivative with bovine serum albumin

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    Vishwas D. Suryawanshi

    2016-02-01

    Full Text Available A biologically active antibacterial reagent, 2–amino-6-hydroxy–4–(4-N, N-dimethylaminophenyl-pyrimidine-5-carbonitrile (AHDMAPPC, was synthesized. It was employed to investigate the binding interaction with the bovine serum albumin (BSA in detail using different spectroscopic methods. It exhibited antibacterial activity against Escherichia coli and Staphylococcus aureus which are common food poisoning bacteria. The experimental results showed that the fluorescence quenching of model carrier protein BSA by AHDMAPPC was due to static quenching. The site binding constants and number of binding sites (n≈1 were determined at three different temperatures based on fluorescence quenching results. The thermodynamic parameters, enthalpy change (ΔH, free energy (ΔG and entropy change (ΔS for the reaction were calculated to be 15.15 kJ/mol, –36.11 kJ/mol and 51.26 J/mol K according to van't Hoff equation, respectively. The results indicated that the reaction was an endothermic and spontaneous process, and hydrophobic interactions played a major role in the binding between drug and BSA. The distance between donor and acceptor is 2.79 nm according to Förster's theory. The alterations of the BSA secondary structure in the presence of AHDMAPPC were confirmed by UV–visible, synchronous fluorescence, circular dichroism (CD and three-dimensional fluorescence spectra. All these results indicated that AHDMAPPC can bind to BSA and be effectively transported and eliminated in the body. It can be a useful guideline for further drug design.

  14. Comparative study on the antioxidant and biological activities of carvacrol, thymol, and eugenol derivatives.

    Science.gov (United States)

    Mastelić, Josip; Jerković, Igor; Blazević, Ivica; Poljak-Blazi, Marija; Borović, Suzana; Ivancić-Baće, Ivana; Smrecki, Vilko; Zarković, Neven; Brcić-Kostic, Krunoslav; Vikić-Topić, Drazen; Müller, Norbert

    2008-06-11

    Four derivatives of thymol, carvacrol, and eugenol were synthesized: 4-(hydroxymethyl)-5-isopropyl-2-methylphenol, 4,4'-methylenebis(5-isopropyl-2-methyl)phenol, 4-allyl-6-(hydroxymethyl)-2-methoxyphenol, and 4-(hydroxymethyl)-2-isopropyl-5-methylphenol. The obtained derivatives showed remarkably better antioxidative properties according to 1,1-diphenyl-2-picrylhydrazyl assay (50% inhibitory concentrations = 4-156 microg/mL) and Rancimat assay (protection factors = 1.55-5.84) when compared with parent compounds and values similar to or better than those of butylated hydroxytoluene and vitamin C. At concentrations of 10 mM carvacrol derivatives had no toxic effect on viability of Escherichia coli K-12 (determined by minimum inhibitory concentrations). Other phenol derivatives showed reduced cytotoxic effect on E. coli K-12 at concentrations of 2-5 mM on the basis of 50% lethal dose measurements. In comparison with the parent compounds, phenol derivatives showed reduced cytotoxic effect for Saccharomyces cerevisiae cells (determined by yeast colony reduction). On the other hand, the majority of synthesized compounds had dose-dependent antiproliferative effects on human uterine carcinoma cells (HeLa), which makes them potentially interesting for the adjuvant experimental cancer treatments. The 4,4'-methylenebis(5-isopropyl-2-methyl)phenol derivative of carvacrol showed lower inhibiting capacity also for the HeLa cells, which makes this particular derivative attractive as an efficient antioxidant with negligible cytotoxic effects.

  15. Synthesis of umbelliferone derivatives in Escherichia coli and their biological activities

    OpenAIRE

    Chu, Luan Luong; Pandey, Ramesh Prasad; Lim, Haet Nim; Jung, Hye Jin; Thuan, Nguyen Huy; Kim, Tae-Su; Sohng, Jae Kyung

    2017-01-01

    Background Umbelliferone, also known as 7-hydroxycoumarin, is a phenolic metabolite found in many familiar plants. Its derivatives have been shown to have various pharmacological and chemo-preventive effects on human health. A uridine diphosphate glycosyltransferase YjiC from Bacillus licheniformis DSM 13, a cytochrome P450BM3 (CYP450 BM3) variant namely mutant 13 (M13) from Bacillus megaterium, and an O-methyltransferase from Streptomyces avermitilis (SaOMT2) were used for modifications of u...

  16. Synthesis and Biological Activity of 2,5-Bisubstituted Derivatives of 1,3,4-Thiadiazol-2,5-dithiol

    Directory of Open Access Journals (Sweden)

    T. S. Zhivotova

    2013-01-01

    Full Text Available By reaction of 1,3,4-thiadiazol-2,5-dithiol with different organohalogens, chlorides of carboxylic acids, acrylic acid derivatives, alkaloids, and secondary amines, various derivatives of 2,5-bi-substituted 1,3,4-thiadiazole were synthesized, and biological properties of some of them were studied.

  17. Biological and structure-activity evaluation of chalcone derivatives against bacteria and fungi

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Wender A.; Andrade, Carlos Kleber Z.; Napolitano, Hamilton B., E-mail: wender@unb.br, E-mail: ckleber@unb.br [Universidade de Brasilia (LaQMOS/UnB), DF (Brazil). Inst. de Quimica; Vencato, Ivo; Castro, Miriam R.C. de; Camargo, Ademir J. [Universidade Estadual de Goias (UEG), Anapolis, GO (Brazil). Ciencias Exatas e Tecnologicas; Lariucci, Carlito [Universidade Estadual de Goias (UEG), Goiania, GO (Brazil). Inst. de Fisica

    2013-01-15

    The present work describes the antibacterial and antifungal activities of several chalcones obtained by a straight Claisen-Schmidt aldol condensation determined by the minimal inhibitory concentration against different microorganisms (Gram-positive and Gram-negative bacteria and fungi). Solid state crystal structures of seven chalcones were determined by X-ray diffraction (XRD) analysis. Chemometric studies were carried out in order to identify a potential structure activity relationship. (author)

  18. Biological and structure-activity evaluation of chalcone derivatives against bacteria and fungi

    OpenAIRE

    Silva, Wender A.; Andrade, Carlos Kleber Z.; Napolitano, Hamilton B.; Vencato, Ivo; Lariucci, Carlito; Castro, Miriam. R. C. de; Camargo, Ademir J.

    2013-01-01

    The present work describes the antibacterial and antifungal activities of several chalcones obtained by a straight Claisen-Schmidt aldol condensation determined by the minimal inhibitory concentration against different microorganisms (Gram-positive and Gram-negative bacteria and fungi). Solid state crystal structures of seven chalcones were determined by X-ray diffraction (XRD) analysis. Chemometric studies were carried out in order to identify a potential structure-activity relationship. ...

  19. Synthesis, characterization and biological activity of transition metal complexes with Schiff bases derived from 2-nitrobenzaldehyde with glycine and methionine

    Science.gov (United States)

    Singh, Bibhesh K.; Rajour, Hemant K.; Prakash, Anant

    Schiff bases derived from 2-nitrobenzaldehyde with amino acids (glycine, methionine) and their Co(II), Ni(II) and Cu(II) complexes have been synthesized and characterized by various physico-chemical techniques. From spectral studies, it has been concluded that the ligands acts as bidentate molecule, coordinates metal through azomethine nitrogen and carboxylate oxygen. Mass spectrum explains the successive degradation of the molecular species in solution and justifies ML2 complexes. X-ray powder diffraction helps to determine the cell parameters of the complexes. Molecular structure of the complexes has been optimized by MM2 calculations and suggests a square planar geometry. The ligands and their metal complexes have been tested in vitro against Streptococcus, Staph, Staphylococcus aureus and Escherchia coli bacteria in order to assess their antibacterial potential. The results indicate that the biological activity increases on complexation.

  20. Synthesis and studies of the biological activity of novel pyrimido fused acridine derivatives

    Directory of Open Access Journals (Sweden)

    MANISH P. PATEL

    2006-10-01

    Full Text Available Anthranilic acid was reacted with various substituted 6-bromoquinazolinones in the presence of Cu-powder and anhydrous potassium carbonate in DMF to give acid intermediates (Ullmann Type-II condensation. All these acids were then cyclized in phosphorus oxychloride to give 11-chloropyrimido[4,5-b]acridin-4(3H-ones. All the synthesized compounds were identified by conventional methods (1H-NMR, IR, elemental analysis and were screened for their antimicrobial activity on some bacterial and fungal cultures. The results were compared with standard bactericides and fungicides. All the synthesized compounds exhibited moderate antibacterial and antifungal activity.

  1. Neuronal targeting, internalization, and biological activity of a recombinant atoxic derivative of botulinum neurotoxin A

    Science.gov (United States)

    Botulinum neurotoxins (BoNT) have the unique capacity to cross epithelial barriers, target neuromuscular junctions, and translocate active metalloprotease component to the cytosol of motor neurons. We have taken advantage of the molecular carriers responsible for this trafficking to create a family ...

  2. Chicken cathelicidin-2-derived peptides with enhanced immunomodulatory and antibacterial activities against biological warfare agents

    NARCIS (Netherlands)

    Molhoek, E.M.; Dijk, A. van; Veldhuizen, E.J.A.; Dijk-Knijnenburg, H.; Mars-Groenendijk, R.H.; Boele, L.C.L.; Kaman-van Zanten, W.E.; Haagsman, H.P.; Bikker, F.J.

    2010-01-01

    Host defence peptides (HDPs) are considered to be excellent candidates for the development of novel therapeutic agents. Recently, it was demonstrated that the peptide C1-15, an N-terminal segment of chicken HDP cathelicidin-2, exhibits potent antibacterial activity while lacking cytotoxicity towards

  3. Synthesis and characterization of transition metal complexes derived from some biologically active furoic acid hydrazones

    Directory of Open Access Journals (Sweden)

    P. Venkateswar Rao

    2007-04-01

    Full Text Available Two new physiologically active ligands, N’-2-[(E-1-hydroxy-4-methyl-2-oxo-2H-8-chromenyl ethylidene-2-furan carbohydrazide (HMCFCH and N’-2-[(Z-1-(4-hydroxy-6-methyl-2-oxo-2H-pyranyl ethylidene]-furan carbohydrazide (HMPFCH and their VO(II, Mn(II, Fe(II, Co(II, Ni(II and Cu(II complexes have been prepared. The ligands and the metal complexes have been characterized by elemental analyses, electrical conductance, magnetic susceptibility measurements, UV-Vis, IR, and ESR spectroscopic data. Basing on the above data, Fe(II and Co(II complexes of HMCFCH and HMPFCH have been assigned a dimeric octahedral geometry. VO(II complexes of HMCFCH and HMPFCH have been assigned sulfate bridged dimeric square pyramidal geometry. Mn(II complex of HMCFCH has been assigned a dimeric octahedral geometry, where as Mn(II complex of HMPFCH has been ascribed to monomeric octahedral geometry. Cu(II and Ni(II complexes of HMCFCH have been ascribed to a polymeric structure. Ni(II complex of HMPFCH has been assigned a dimeric square planar geometry. Cu(II complex of HMPFCH has been proposed an octahedral geometry. The ligands and their metal chelates were screened against S. aureus and P. aeruginosa. The ligands and the metal complexes have been found to be active against these microorganisms. The ligands show more activity than the metal complexes.

  4. Synthesis, characterization and biological activity of symmetric dinuclear complexes derived from a novel macrocyclic compartmental ligand

    International Nuclear Information System (INIS)

    Mruthyunjayaswamy, B.H.M.; Ijare, Omkar B.; Jadegoud, Y.

    2005-01-01

    A phenol based novel macrocyclic binucleating compartmental ligand N,N-bis(2,6-diiminomethyl-4-methyl-1-hydroxyphenyl)malonoyldicarboxamide was prepared. The complexes were prepared by template method by reacting 2,6-diformyl-4-methylphenol, malonoyl dihydrazide and the metal chlorides of Cu(II), Ni(II), Co(II), Cd(II), Zn(II) and Hg(II) in methanol to get a series of dinuclear complexes. The complexes were characterized by elemental analyses, conductivity measurements, magnetic susceptibility data, IR, UV-Vis, ESR, NMR and FAB mass spectral data. The dinuclear nature of the complexes was confirmed on the basis of elemental analyses, magnetic susceptibility, ESR and FAB mass spectral data. The ligand as well as Cu(II), Ni(II), Co(II) and Zn(II) complexes were tested for their antibacterial and antifungal properties against Escherichia coli, Staphyloccocus aureus, Aspergillus niger and Fusarium oxysporum. Magnetic susceptibility measurements of Cu(II), Ni(II) and Co(II) complexes reveal that these complexes exhibit antiferromagnetic coupling behavior due to the presence of two metal ions in close proximity. FAB mass spectrum of the Cu(II) complex gave a clear evidence for the dinuclear nature. The ligand and the complexes were found to be less active against the tested bacteria, but the ligand alone was found active against the fungus Fusarium oxysporum. (author)

  5. Design, synthesis and biological activity evaluation of novel 4-subtituted 2-naphthamide derivatives as AcrB inhibitors.

    Science.gov (United States)

    Wang, Yinhu; Mowla, Rumana; Ji, Shengli; Guo, Liwei; De Barros Lopes, Miguel A; Jin, Chaobin; Song, Di; Ma, Shutao; Venter, Henrietta

    2018-01-01

    A novel series of 4-substituted 2-naphthamide derivatives were designed, synthesized and evaluated for their biological activity. In particular, the ability of the compounds to potentiate the action of antibiotics, to inhibit Nile Red efflux and to target AcrB specifically was investigated. The results indicated that most of the 4-substituted 2-naphthamide derivatives were able to synergize with the antibiotics tested, and inhibit Nile Red efflux by AcrB in the resistant phenotype. Subsequent exclusion of compounds with off target effects such as outer- or inner membrane permeabilization identified compounds 7c, 7g, 12c, 12i and 13g as efflux pump inhibitors (EPIs). Particularly, compounds 7c, 7g and 12i were found to be the most potent EPIs, which synergized with the two substrates tested at lower concentrations than that of parent A3, demonstrating an improvement in potency as compared to A3. Additionally, when the outer membrane of E. coli was permeabilized, compound 12c displayed a huge increase in efficacy and was able to synergize with erythromycin at a concentration that was 16 times lower than that of the parent A3. Hence we were able to design and synthesize compounds that displayed significant increase in efficacy as EPIs against AcrB. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  6. Electrochemical Behavior of Biologically Important Indole Derivatives

    Directory of Open Access Journals (Sweden)

    Cigdem Karaaslan

    2011-01-01

    Full Text Available Voltammetric techniques are most suitable to investigate the redox properties of a new drug. Use of electrochemistry is an important approach in drug discovery and research as well as quality control, drug stability, and determination of physiological activity. The indole nucleus is an essential element of a number of natural and synthetic products with significant biological activity. Indole derivatives are the well-known electroactive compounds that are readily oxidized at carbon-based electrodes, and thus analytical procedures, such as electrochemical detection and voltammetry, have been developed for the determination of biologically important indoles. This paper explains some of the relevant and recent achievements in the electrochemistry processes and parameters mainly related to biologically important indole derivatives in view of drug discovery and analysis.

  7. Synthesis, crystal structure and theoretical analysis of intermolecular interactions in two biologically active derivatives of 1,2,4-triazoles

    Science.gov (United States)

    Shukla, Rahul; Mohan, T. P.; Vishalakshi, B.; Chopra, Deepak

    2017-04-01

    In the present study, we have synthesized and structurally characterized two biologically active derivatives of 1,2,4 triazoles, namely 3-(4-fluoro-3-phenoxyphenyl)-1-(piperidin-1-ylmethyl)-1H-1,2,4-triazole-5(4H)-thione (TR) and 1-((3-(4-fluoro-3-phenoxyphenyl)-5-(methylthio)-1H-1,2,4-triazol-1-yl)methyl)piperidine (TR1) via single crystal X-ray diffraction. Both the structures show the presence of various intermolecular interactions in the crystalline solid such as Csbnd H…F, Csbnd H…S, Csbnd H…N, Csbnd H…O, Csbnd H … π, and π … π intermolecular interactions. The role of these interactions in molecular packing was analyzed, and the nature of these interactions was evaluated through computational procedures using PIXEL. Hirshfeld analysis further reveals that the contribution of H…F interactions was more prominent towards packing as compared to H…N/O intermolecular interactions.

  8. The Redox Chemistry and Chemical Biology of H2S, Hydropersulfides and Derived Species: Implications to Their Possible Biological Activity and Utility

    Science.gov (United States)

    Ono, Katsuhiko; Akaike, Takaake; Sawa, Tomohiro; Kumagai, Yoshito; Wink, David A.; Tantillo, Dean J.; Hobbs, Adrian J.; Nagy, Peter; Xian, Ming; Lin, Joseph; Fukuto, Jon M.

    2014-01-01

    Hydrogen sulfide (H2S) is an endogenously generated and putative signaling/effector molecule. In spite of its numerous reported functions, the chemistry by which it elicits its functions is not understood. Moreover, recent studies allude to the existence of other sulfur species besides H2S that may play critical physiological roles. Herein, the basic chemical biology of H2S as well as other related or derived species is discussed and reviewed. A particular focus of this review are the per- and poly-sulfides which are likely in equilibrium with free H2S and which may be important biological effectors themselves. PMID:25229186

  9. Redox chemistry and chemical biology of H2S, hydropersulfides, and derived species: implications of their possible biological activity and utility.

    Science.gov (United States)

    Ono, Katsuhiko; Akaike, Takaaki; Sawa, Tomohiro; Kumagai, Yoshito; Wink, David A; Tantillo, Dean J; Hobbs, Adrian J; Nagy, Peter; Xian, Ming; Lin, Joseph; Fukuto, Jon M

    2014-12-01

    Hydrogen sulfide (H2S) is an endogenously generated and putative signaling/effector molecule. Despite its numerous reported functions, the chemistry by which it elicits its functions is not understood. Moreover, recent studies allude to the existence of other sulfur species besides H2S that may play critical physiological roles. Herein, the basic chemical biology of H2S as well as other related or derived species is discussed and reviewed. This review particularly focuses on the per- and polysulfides which are likely in equilibrium with free H2S and which may be important biological effectors themselves. Copyright © 2014 Elsevier Inc. All rights reserved.

  10. A mini review on biological activities of pyridazinone derivatives as antiulcer, antisecretory, antihistamine and particularly against histamine H3R.

    Science.gov (United States)

    Asif, Mohammad

    2015-01-01

    Pyridazinone derivatives and their related analoges were introduced for gastric antiulcer and antisecretory activities. Selected compounds were applied to ulcer models and showed their antiulcer and anti secretary activities. Some pyridazinone compounds are recently reported as H3R antagonists. Some amine analogs of pyridazinones, pyridazinone- phenethylamines and 4,5-fused pyridazinones showed histamine H3R antagonist activity with significant affinity for rat and human H3R. These pyridazinone analogs also showed excellent selectivity and metabolic stability, with adequate pharmacokinetics.

  11. SYNTHESIS OF IMIDAZO[2,1-b][1,3,4]THIADIAZOLE DERIVATIVES AS POSSIBLE BIOLOGICALLY ACTIVE AGENTS.

    Science.gov (United States)

    Kumar, Sujeet; Metikurki, Basavaraj; Bhadauria, Vivek Singh; Clercq, Erik De; Schols, Dominique; Tokuda, Harukuni; Karki, Subhas S

    2016-07-01

    A series of 2-(4-methylbenzyl)-5,6-substituted-imidazo[2,1-b][1,3,4]thiadiazole derivatives were synthesized, characterized and evaluated for antiproliferative activity and cancer chemopreventive activity. Results showed that molecules with formyl and thiocyanate substiments at the 5 position exhibited an increase in activity against the full panel of 60 human tumor cell lines at a minimum of five concentrations at 10-fold dilutions. Derivative 22 displayed significant in vino anticancer activity against colon cancer (MID GI₅₀ = 0.75 μM). The cancer chemopreventive effect of 19 (IC₅₀ = 489 nM) was almost equipotent to standard oleanolic acid (IC₅₀ = 449 nM).

  12. Synthesis and Biological Activity of 3-[Phenyl(1,3-thiazol-2-yl-amino]propanoic Acids and Their Derivatives

    Directory of Open Access Journals (Sweden)

    Vytautas Mickevičius

    2013-12-01

    Full Text Available New N,N-disubstituted β-amino acids and their derivatives with thiazole, aromatic, and heterocyclic substituents were synthesized from N-phenyl-N-thiocarbamoyl-β-alanine by the Hantzsch method; derivatives with hydrazone fragments were also obtained. Some of the synthesized compounds exhibited discrete antimicrobial activity, and 3-[(4-oxo-4,5-dihydro-1,3-thiazol-2-yl(phenylamino]propanoic acid was found to promote rapeseed growth and to increase seed yield and oil content.

  13. Synthesis and biological activities of some new spiro 1,2,4-triazole derivatives having sulfonamide moiety

    Directory of Open Access Journals (Sweden)

    Hany M. Dalloul

    2017-10-01

    Full Text Available A new series of spiro 1,2,4-triazoles 5-9a-j were prepared by the reaction of appropriate amidrazones 4 with cyclic ketones in catalytic amount of p-toluene sulfonic acid. The structures of the titled compounds have been elucidated by the elemental analysis and spectroscopic data (IR, 1H NMR, 13C NMR and MS. The biological activities of the prepared compounds were investigated using well-established methods from the literature.

  14. Synthesis, characterization and biological activities of novel chalcone derivatives, containing 4, 7-ethanoisoindole-1,3-dione units

    Directory of Open Access Journals (Sweden)

    Mustafa Ceylan

    2013-09-01

    Full Text Available Novel chalcone derivatives, containing 4, 7-ethanoisoindole-1,3-dione units were synthesized starting from 1,3-cyclohexadine (4 and maleic anhydride (5. Addition of maleic anhydride (5 to 1,3-cyclehexadine (4 gave an endo-adduct, 3a,4,7,7a-tetrahydro-4,7-ethano-2-benzofuran-1,3-dione (6, in 90% yield. Heating the solution of the adduct dione (6 and 1-(4-aminophenylethanone (7 in the presence of Et 3N in toluene at 110 oC for 24 hours afforded 2-(4-acetylphenyl-3a,4,7,7a-tetrahydro-1H-4,7-ethanoisoindole-1,3-dione (8 in high yield. Piperidine-catalyzed addition of benzaldehyde derivatives (9a-i to the compound 8 in CH 2Cl 2 at 55 oC gave the expected chalcone derivatives (10-i in the range of 42% - 96% yields. The antibacterial activities of the chalcone derivatives (10a-i were evaluated against human pathogenic microorganism and the compounds showed low activity compared to the standard, name of the standard.

  15. Biological activity of N(4)-boronated derivatives of 2'-deoxycytidine, potential agents for boron-neutron capture therapy.

    Science.gov (United States)

    Nizioł, Joanna; Uram, Łukasz; Szuster, Magdalena; Sekuła, Justyna; Ruman, Tomasz

    2015-10-01

    Boron-neutron capture therapy (BNCT) is a binary anticancer therapy that requires boron compound for nuclear reaction during which high energy alpha particles and lithium nuclei are formed. Unnatural, boron-containing nucleoside with hydrophobic pinacol moiety was investigated as a potential BNCT boron delivery agent. Biological properties of this compound are presented for the first time and prove that boron nucleoside has low cytotoxicity and that observed apoptotic effects suggest alteration of important functions of cancer cells. Mass spectrometry analysis of DNA from cancer cells proved that boron nucleoside is inserted into nucleic acids as a functional nucleotide derivative. NMR studies present very high degree of similarity of natural dG-dC base pair with dG-boron nucleoside system. Copyright © 2015 Elsevier Ltd. All rights reserved.

  16. Synthesis and Biological Activity of Substituted Urea and Thiourea Derivatives Containing 1,2,4-Triazole Moieties

    Directory of Open Access Journals (Sweden)

    David E. Wedge

    2013-03-01

    Full Text Available A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives 3a–e and 4a–e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds 1a–e and 2a–e, respectively, in a 130–140 °C oil bath. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV, IR, 1H-NMR and mass spectroscopy. All compounds were evaluated for antifungal activity against plant pathogens, larvicidal and biting deterrent activity against the mosquito Aedes aegypti L. and in vitro cytotoxicity and anti-inflammatory activity against some human cell lines. Phomopis species were the most sensitive fungi to these compounds. Compounds 1b, 1c, 3a and 4e demonstrated selectively good activity against Phomopis obscurans and only 1b and 4e showed a similar level of activity against P. viticola. Compound 3d, with a LD50 value of 67.9 ppm, followed by 1c (LD50 = 118.8 ppm and 3e (LD50 = 165.6 ppm, showed the highest toxicity against Aedes aegypti larvae. Four of these compounds showed biting deterrent activity greater than solvent control, with the highest activity being seen for 1c, with a proportion not biting (PNB value of 0.75, followed by 1e, 2b and 1a. No cytotoxicity was observed against the tested human cancer cell lines. No anti-inflammatory activity was observed against NF-kB dependent transcription induced by phorbol myristate acetate (PMA in human chondrosarcoma cells.

  17. Synthesis and Biological Activities of Some Novel (E-Alpha-(methoxyiminobenzeneacetate Derivatives with Modified 1,2,4-Triazole Moiety

    Directory of Open Access Journals (Sweden)

    Xianyou Wang

    2014-01-01

    Full Text Available To find new strobilurin analogues with high activity against resistant pathogens, a series of (E-α-(methoxyiminobenzeneacetate derivatives containing 1,2,4-triazole Schiff base side chain were designed and synthesized. Their structures were confirmed by IR, 1H NMR, and 13C NMR, ESI-HRMS, or elemental analyses. Bioassays indicated that most of the target compounds showed moderate to good fungicidal activities against Rhizoctonia solani, Botrytis cinerea Pers., Fusarium graminearum, Cotton rhizoctoniosis, and Blumeria graminis. For example, compounds 6g and 6j exhibited promising antifungal activity against Rhizoctonia solani, Botrytis cinerea Pers., and Fusarium graminearum. Compounds 6c, 6l, and 6m had higher fungicidal activities against Blumeria graminis at the concentration of 50 µg/mL; inhibitory rate is 91.41%, 92.13%, and 91.77%, respectively.

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

    Directory of Open Access Journals (Sweden)

    Ticuţa Negreanu-Pîrjol

    2011-05-01

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

  19. Synthesis, Characterization, and Biological Activity of 5-Phenyl-1,3,4-thiadiazole-2-amine Incorporated Azo Dye Derivatives

    Directory of Open Access Journals (Sweden)

    Chinnagiri T. Keerthi Kumar

    2013-01-01

    Full Text Available 5-Phenyl-1,3,4-thiadiazole-2-amine has been synthesized by single step reaction. A series of heterocyclic azodyes were synthesized by diazotisation of 5-phenyl-1,3,4-thiadiazole-2-amine by nitrosyl sulphuric acid followed by coupling with different coupling compounds such as 8-hydroxyquinoline, 2,6-diaminopyridine, 2-naphthol, N,N-dimethyl aniline, resorcinol, and 4,6-dihydroxypyrimidine. The dyes were characterized by UV-Vis, IR, 1H-NMR, 13C NMR, and elemental analysis. The synthesized compounds were also screened for biological activity.

  20. BIOPEP-PBIL Tool for the Analysis of the Structure of Biologically Active Motifs Derived from Food Proteins

    Directory of Open Access Journals (Sweden)

    Jerzy Dziuba

    2011-01-01

    Full Text Available This work describes a flexible technique for the analysis of protein sequences as a source of motifs affecting bodily functions. The BIOPEP database, along with the Pôle Bioinformatique Lyonnais (PBIL server, were applied to define which activities of peptides dominated in their protein precursors and which structure of the protein contained the most of the revealed activities. Such an approach could be helpful in finding some structural requirements for peptide(s to be regarded as biologically active (bioactive. It was found that apart from the activities of peptides that commonly occur in the majority of proteins (e.g. ACE inhibitors, all analyzed proteins can be a source of motifs involved in e.g. activation of ubiquitin-mediated proteolysis. This could be important in designing diets for patients who suffer from neural diseases. The structure and bioactivity analyses revealed that if peptides were to be 'bioactive', it is essential that they assume the position of a coil (or combination of coil and a-helix in the sequence of their protein precursors. However, it is recommended to consider the factors such as the length of peptide chains, the number of peptides in the database as well as the repeatability of the occurrence of characteristic amino acids, both in the peptide and in the protein when studying the bioactivity and structure of biomolecules.

  1. Novel Bifunctional Quinolonyl Diketo Acid Derivatives as HIV-1 Integrase Inhibitors: Design, Synthesis, Biological Activities and Mechanism of Action

    Science.gov (United States)

    Di Santo, Roberto; Costi, Roberta; Roux, Alessandra; Artico, Marino; Lavecchia, Antonio; Marinelli, Luciana; Novellino, Ettore; Palmisano, Lucia; Andreotti, Mauro; Amici, Roberta; Galluzzo, Clementina Maria; Nencioni, Lucia; Palamara, Anna Teresa; Pommier, Yves; Marchand, Christophe

    2008-01-01

    The virally encoded integrase protein is an essential enzyme in the life cycle of the HIV-1 virus and represents an attractive and validated target in the development of therapeutics against HIV infection. Drugs that selectively inhibit this enzyme, when used in combination with inhibitors of reverse transcriptase and protease, are believed to be highly effective in suppressing the viral replication. Among the HIV-1 integrase inhibitors, the β-diketo acids (DKAs) represent a major lead for anti-HIV-1drug development. In this study, novel bifunctional quinolonyl diketo acid derivatives were designed, synthesized and tested for their inhibitory ability against HIV-1 integrase. The compounds are potent inhibitors of integrase activity. Particularly, derivative 8 is a potent IN inhibitor for both steps of the reaction (3′-processing and strand transfer) and exhibits both high antiviral activity against HIV-1 infected cells and low cytotoxicity. Molecular modeling studies provide a plausible mechanism of action, which is consistent with ligand SARs and enzyme photo-crosslinking experiments. PMID:16539381

  2. Biological role of Trichoderma harzianum-derived platelet-activating factor acetylhydrolase (PAF-AH) on stress response and antagonism.

    Science.gov (United States)

    Yu, Chuanjin; Fan, Lili; Wu, Qiong; Fu, Kehe; Gao, Shigang; Wang, Meng; Gao, Jinxin; Li, Yaqian; Chen, Jie

    2014-01-01

    We investigated the properties of platelet-activating factor acetylhydrolase (PAF-AH) derived from Trichoderma harzianum. The enzyme, comprised of 572 amino acids, shares high homology with PAF-AH proteins from T. koningii and other microbial species. The optimum enzymatic activity of PAF-AH occurred at pH 6 in the absence of Ca2+ and it localized in the cytoplasm, and we observed the upregulation of PAF-AH expression in response to carbon starvation and strong heat shock. Furthermore, PAF-AH knockout transformant growth occurred more slowly than wild type cells and over-expression strains grown in SM medium at 37°C and 42°C. In addition, PAF-AH expression significantly increased under a series of maize root induction assay. Eicosanoic acid and ergosterol levels decreased in the PAF-AH knockouts compared to wild type cells, as revealed by GC/MS analysis. We also determined stress responses mediated by PAF-AH were related to proteins HEX1, Cu/Zn superoxide dismutase, and cytochrome c. Finally, PAF-AH exhibited antagonistic activity against Rhizoctonia solani in plate confrontation assays. Our results indicate PAF-AH may play an important role in T. harzianum stress response and antagonism under diverse environmental conditions.

  3. Synthesis, Characterization, and Biological Activity of Some Transition Metal Complexes Derived from Novel Hydrazone Azo Schiff Base Ligand

    Directory of Open Access Journals (Sweden)

    C. Anitha

    2011-01-01

    Full Text Available A series of metal(II complexes ML where M = VO(II, Co(II, Ni(II, Cu(II, and Zn(II have been synthesized from azo Schiff base ligand (N′E-N′-(5-((4-chlorophenyldiazenyl-2-hydroxybenzylidene-2-hydroxybenzohydrazide and characterized on the basis of elemental analyses, electronic, IR, and 1H NMR spectra, magnetic susceptibility and also by aid of scanning electron microscopy (SEM, X-ray powder diffraction, fluorescence spectral studies, and molar conductivity measurements. Conductivity measurements reveal that the complexes are nonelectrolytes. Spectroscopy and other analytical studies reveal distorted square planar geometry for copper, square-pyramidal geometry for oxovanadium, and tetrahedral geometry for other complexes. Redox behavior of the copper(II complex has been studied with cyclic voltammetry, and the biological activities of the ligand and metal complexes have been studied against several microorganisms by the well diffusion method. All synthesized compounds can serve as potential photoactive materials as indicated from their characteristic fluorescence properties. The second harmonic generation (SHG efficiency of the ligand was measured and found to be higher than that of urea and KDP. The SEM image of the copper(II complex implies that the size of the particles is 50 nm.

  4. Novel 2-arylazoimidazole derivatives as inhibitors of Trypanosoma cruzi proliferation: Synthesis and evaluation of their biological activity.

    Science.gov (United States)

    Salerno, Alejandra; Celentano, Ana M; López, Julieta; Lara, Virginia; Gaozza, Carlos; Balcazar, Darío E; Carrillo, Carolina; Frank, Fernanda M; Blanco, María M

    2017-01-05

    In this work, the synthesis of a series of 2-arylazoimidazole derivatives 6-20 has been achieved through the reaction of imidazole with aryldiazonium salts, followed by ultrasound-assisted alkylation. This approach has important advantages including higher yield, shorter reaction times and milder reaction conditions. The structures of the compounds obtained were determined by MS, IR; and 1 H and 13 C NMR. The anti-Trypanosoma cruzi activity of the 15 compounds obtained was evaluated. Two compounds with piperidino substituents in the carboxamide moiety proved to be effective inhibitors of epimastigote proliferation, obtaining inhibition values comparable to those achieved with the reference drug Benznidazole. Besides, these compounds displayed low cytotoxicity on mammalian cells. In vivo, both compounds protected mice against a challenge with a lethal Trypanosoma cruzi strain. These results allow us to propose 2-arylazoimidazoles as lead compounds for the design of novel drugs to treat Chagas' disease. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  5. Metal complexes of Schiff base derived from sulphametrole and o-vanilin . Synthesis, spectral, thermal characterization and biological activity

    Science.gov (United States)

    Mohamed, Gehad G.; Sharaby, Carmen M.

    2007-04-01

    Metal complexes of Schiff base derived from condensation of o-vanilin (3-methoxysalicylaldehyde) and sulfametrole [ N1-(4-methoxy-1,2,5-thiadiazole-3-yl)sulfanilamide] (H 2L) are reported and characterized based on elemental analyses, IR, 1H NMR, solid reflectance, magnetic moment, molar conductance, mass spectra, UV-vis and thermal analysis (TGA). From the elemental analyses data, the complexes were proposed to have the general formulae [M 2X 3(HL)(H 2O) 5]· yH 2O (where M = Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), X = Cl, y = 0-3); [Fe 2Cl 5(HL)(H 2O) 3]·2H 2O; [(FeSO 4) 2(H 2L)(H 2O) 4] and [(UO 2) 2(NO 3) 3(HL)(H 2O)]·2H 2O. The molar conductance data reveal that all the metal chelates were non-electrolytes. The IR spectra show that, H 2L is coordinated to the metal ions in a tetradentate manner with ON and NO donor sites of the azomethine-N, phenolic-OH, enolic sulphonamide-OH and thiadiazole-N. From the magnetic and solid reflectance spectra, it is found that the geometrical structures of these complexes are octahedral. The thermal behaviour of these chelates shows that the hydrated complexes losses water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters, such as, E*, Δ H*, Δ S* and Δ G* are calculated from the DrTG curves using Coats-Redfern method. The synthesized ligand, in comparison to their metal complexes also were screened for their antibacterial activity against bacterial species, Escherichia coli, Salmonella typhi, Bacillus subtillus, Staphylococcus aureus and Fungi ( Aspergillus terreus and Aspergillus flavus). The activity data show that the metal complexes to be more potent/antimicrobial than the parent Shciff base ligand against one or more microbial species.

  6. Synthesis and Biological Evaluation of Some Pyridine Derivatives as ...

    African Journals Online (AJOL)

    Synthesis and Biological Evaluation of Some Pyridine Derivatives as Antimicrobial Agents. ... Ethiopian Pharmaceutical Journal ... In this study, several pyridine derivatives were synthesized and evaluated for their in vitro antimicrobial activity against Gram-positive bacteria (Bacillus cereus and Staphylococcus aureus), ...

  7. Synthesis and preliminary biologic activity evaluation of nitric oxide-releasing andrographolide derivatives in RIN-m cells.

    Science.gov (United States)

    Liang, Zhibin; Du, Enming; Xu, Lipeng; Sun, Yewei; Zhang, Gaoxiao; Yu, Pei; Wang, Yuqiang

    2014-01-01

    Pancreatic β-cell dysfunction and death are important feature of diabetes mellitus. Beta-cell protection has demonstrated clinical benefits in the treatment of this disease. In the present study, andrographolide derivatives with nitric oxide (NO)-releasing capability were synthesized and their protective effects against tert-butyl hydroperoxide (t-BHP) induced cell damage were investigated in RIN-m cells. Compound 6b was found to release a moderate amount of NO and was more potent than its natural parent andrographolide in inhibiting cell apoptosis. These findings suggested that andrographolide derivatives with NO-releasing capacity may be a potential therapy for diabetes.

  8. Synthesis and Biological Activity of Some Novel Derivatives of 4-Amino-3-(D-galactopentitol-1-yl-5-mercapto-1,2,4-triazole

    Directory of Open Access Journals (Sweden)

    Jiang-Hai Zhu

    2007-07-01

    Full Text Available To discover new 1,2,4-triazole derivatives which may possess significant biological activities, we synthesized a series of novel 6-aryl-3-(D-galactopentitol-1-yl- 7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines and 4-(arylmethylideneamino-5-(D-galactopentitol- 1-yl-3-mercapto-4H-1,2,4-triazoles from 4-amino-3-(D-galactopentitol-1-yl-5- mercapto-1,2,4-triazole. All the title compounds were characterized by elemental analysis, IR, 1H- and 13C-NMR. Plant growth-regulating activity tests showed that these compounds have remarkable effects on the growth of radish and wheat.

  9. Synthesis and biological activity evaluation of hydrazone derivatives based on a Tröger's base skeleton

    Czech Academy of Sciences Publication Activity Database

    Kaplánek, R.; Havlík, M.; Dolenský, B.; Rak, J.; Džubák, P.; Konečný, P.; Hajdúch, M.; Králová, Jarmila; Král, V.

    2015-01-01

    Roč. 23, č. 7 (2015), s. 1651-1659 ISSN 0968-0896 R&D Projects: GA ČR(CZ) GAP303/11/1291 Grant - others:GA MŠk(CZ) EE2.3.30.0060; GA MŠk(CZ) LO1304 Program:EE; LD Institutional support: RVO:68378050 Keywords : Anticancer agents * Cancer treatment * Complexation studies * Hydrazone * Troger's base Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.923, year: 2015

  10. Biological activity of two new pyrrole derivatives against stored-product species: influence of temperature and relative humidity.

    Science.gov (United States)

    Boukouvala, M C; Kavallieratos, N G; Athanassiou, C G; Hadjiarapoglou, L P

    2016-08-01

    Members of the pyrrole group are likely to have interesting properties that merit additional investigation as insecticides at the post-harvest stages of agricultural commodities. In the present work, the insecticidal effect of two new pyrrole derivatives, ethyl 3-(benzylthio)-4,6-dioxo-5-phenyl-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrrole-carboxylate (3i) and isopropyl 3-(benzylthio)-4,6-dioxo-5-phenyl-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrrole-carboxylate (3k) were studied as stored-wheat protectants against two major stored-product insect species, the confused flour beetle, Tribolium confusum Jaquelin du Val adults and larvae and the Mediterranean flour moth, Ephestia kuehniella Zeller larvae at different doses (0.1, 1 and 10 ppm), exposure intervals (7, 14 and 21 days), temperatures (20, 25 and 30°C) and relative humidity (55 and 75%) levels. For T. confusum adults, in the case of the pyrrole derivative 3i, mortality was low and it did not exceed 32.2% in wheat treated with 10 ppm 3i at 30°C and 55% relative humidity. Progeny production was very low (relative humidity, including control. In the case of the pyrrole derivative 3k, mortality reached 67.8% at 30°C and 55% relative humidity in wheat treated with 10 ppm after 21 days of exposure. Progeny production was low in all tested combinations (≤0.7 individuals/vial) of 55% relative humidity, including control. For T. confusum larvae, in the case of the pyrrole derivative 3i, at the highest dose, mortality was 82.2% at 25°C and 55% relative humidity whereas in the case of 3k it reached 77.8% at the same combination. In contrast, mortality at 75% relative humidity remained very low and did not exceed 13.3%. For E. kuehniella larvae, the highest mortalities, 44.4 and 63.3%, were observed in 10 ppm at 25°C and 55% relative humidity for both pyrrole derivatives. The compounds tested here have a certain insecticidal effect, but this effect is moderated by the exposure, the target species, the temperature and the

  11. Activity on Trypanosoma cruzi, erythrocytes lysis and biologically relevant physicochemical properties of Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones.

    Science.gov (United States)

    Santos, Diego; Parajón-Costa, Beatriz; Rossi, Miriam; Caruso, Francesco; Benítez, Diego; Varela, Javier; Cerecetto, Hugo; González, Mercedes; Gómez, Natalia; Caputto, María E; Moglioni, Albertina G; Moltrasio, Graciela Y; Finkielsztein, Liliana M; Gambino, Dinorah

    2012-12-01

    American trypanosomiasis or Chagas disease, caused by the protist parasite Trypanosoma cruzi (T. cruzi), is a major health concern in Latin America. In the search for new bioactive compounds, eight Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones (HL) were evaluated as potential anti-T. cruzi compounds. Their unspecific cytotoxicity was determined on human erythrocytes. Two physicochemical features, lipophilicity and redox behavior, that could be potentially relevant for the biological activity of these complexes, were determined. Crystal structure of [Pd(HL1)(L1)]Cl·CH(3)OH, where HL1=1-indanone thiosemicarbazone, was solved by X-ray diffraction methods. Five of the eight metal complexes showed activity against T. cruzi with IC(50) values in the low micromolar range and showed significantly higher activity than the corresponding free ligands. Four of them resulted more active against the parasite than the reference antitrypanosomal drug Nifurtimox. Anti-T. cruzi activity and selectivity towards the parasite were both higher for the Pd(II) compounds than for the Pt(II) analogues, showing the effect of the metal center selection on the biological behavior. Among both physicochemical features tested for this series of compounds, lipophilicity and redox behavior, only the former seemed to show correlation with the antiproliferative effects observed. Metal coordination improved bioactivity but lead to an increase of mammalian cytotoxicity. Nevertheless, some of the metal complexes tested in this work still show suitable selectivity indexes and deserve further developments. Copyright © 2012 Elsevier Inc. All rights reserved.

  12. Imidazole: Having Versatile Biological Activities

    Directory of Open Access Journals (Sweden)

    Amita Verma

    2013-01-01

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

  13. Design and synthesis of some substituted thiazolo[3,2-a]pyrimidine derivatives of potential biological activities

    Directory of Open Access Journals (Sweden)

    Samia G. Abdel Moty

    2016-03-01

    Full Text Available In continuation to our previous work, thiazolopyrimidines 2a–x were synthesized through intramolecular cyclization of 2-phenacylthio-dihydropyrimidine hydrobromides 1a–x using polyphosphoric acid. On the other hand, thiazolo[3,2-a]pyrimidine-3-one 3 was coupled with aryldiazonium salts or condensed with isatin to afford compounds 4a–c or 5, respectively. Chemical structure of the target compounds was substantiated by IR, FT-IR, 1H-, 13C and DEPT-13C NMR, MS as well as microanalyses. Moreover, the lipophilicity of the target compounds is expressed as ClogP. The antimicrobial screening of the test compounds 2a–x, 4a–c and 5 revealed moderate activity in comparison to reference drugs. Compounds 2a–c, 2e, 2o and 2v showed a gradual increase in their anti-inflammatory activity reaching its maximum at 5 h compared to indomethacin. Furthermore, the analgesic activity of compounds 2a–c, 2e, 2o and 2v revealed a maximum activity after 5 h of injection compared to aspirin and the LD50 of compounds 2e and 2v was determined.

  14. Synthesis of a labelled derivative of methomyl with potential affinity for the biological active site of mitochondrias Texas

    International Nuclear Information System (INIS)

    Aranda, G.; Herbert, M.; Pichat, L.

    1986-01-01

    The Grignard reagent from 1-chloro-4-methoxy butane was carbonated with 14 CO 2 giving [carboxyl 14 C]-5-methoxy pentanoic acid. Yield: 80%. Specific activity: 24,3 mCi/mmole. Treated with dry hydrogen bromide in acetic acid, the latter gave [carboxyl 14 C]-5-bromopentanoic acid which was condensed with diphenylphosphoryl azide leading to 5-bromobutyl [carbonyl 14 C] isocyanate. Without isolation, the latter was reacted with methylthioacetoxy hydroxamate giving [carbonyl 14 C] S-methyl-N [(4-azidobutyl carbamoyl) oxy] thioacetimidate with an overall yield of 15,7 %/ 14 CO 2 and a radiochemical purity of 99.8%. Specific activity: 23,7 mCi/mmole. (author)

  15. Synthesis and Biological Activity of Novel Amino Acid-(N'-Benzoyl Hydrazide and Amino Acid-(N'-Nicotinoyl Hydrazide Derivatives

    Directory of Open Access Journals (Sweden)

    Sherine N. Khattab

    2005-09-01

    Full Text Available The coupling reaction of benzoic acid and nicotinic acid hydrazides with N- protected L-amino acids including valine, leucine, phenylalanine, glutamic acid and tyrosine is reported. The target compounds, N-Boc-amino acid-(N`-benzoyl- and N- Boc-amino acid-(N`-nicotinoyl hydrazides 5a-5e and 6a-6e were prepared in very high yields and purity using N-[(dimethylamino-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl- methylene]-N-methyl-methanaminium hexafluorophosphate N-oxide (HATU as coupling reagent. The antimicrobial activity of the Cu and Cd complexes of the designed compounds was tested. The products were deprotected affording the corresponding amino acid-(N`-benzoyl hydrazide hydrochloride salts (7a-7e and amino acid-(N`- nicotinoyl hydrazide hydrochloride salts (8a-8e. These compounds and their Cu and Cd complexes were also tested for their antimicrobial activity. Several compounds showed comparable activity to that of ampicillin against S. aureus and E. coli.

  16. Síntese e atividade biológica do derivado 6-formil-oxamniquina Synthesis and biological activity of 6-formyl-oxamniquine derivative

    Directory of Open Access Journals (Sweden)

    Adélia Emília de Almeida

    2008-12-01

    Full Text Available A esquistossomose, uma importante doença no Brasil, é causada por trematódeo pertencente ao gênero Schistosoma, atingindo milhões de pessoas, numa das maiores regiões endêmicas dessa doença em todo globo. O principal objetivo desse trabalho foi sintetizar o derivado 6-formil-oxamniquina e avaliar sua atividade biológica. O derivado 6-formil- oxamniquina foi obtido por oxidação da oxamniquina com dióxido de manganês empregando diclorometano como solvente, à temperatura ambiente, por 24 horas. Sua obtenção foi confirmada por espectrometria na região de infravermelho e espectroscopia de RMN 13C e ¹H, apresentando atividade similar quando comparada à oxamniquina comercial (Mansil®.Schistosomiasis, an important disease in Brazil, is caused by a trematode of the genus Schistosoma, reaching millions of person in one of the most endemic region of this disease in the whole globe. The main goal of this work was to syntetize the 6-formyl-oxamniquine derivative and evaluate its biological activity. The 6-formyl-oxamniquine derivative was obtained by the oxidation of oxamniquine with MnO2, applying CH2Cl2 as solvent at room temperature for 24 hours. The obtaintion of 6-formyl-oxamniquine derivative compound was confirmed by IR spectroscopy and 13C NMR and ¹H NMR, presenting similar activity when compared to the commercial oxamniquine (Mansil®.

  17. Synthesis, reactions, and biological activities of some new thieno[3,2-c]quinoline and pyrrolo[3,2-c]quinoline derivatives.

    Science.gov (United States)

    Abdel-Wadood, Fatma K; Abdel-Monem, Maisa I; Fahmy, Atiat M; Geies, Ahmed A

    2014-02-01

    2-Bromo-4-fluoroaniline (1) was condensed with ethyl 2-cyano-3-ethoxyacrylate (2) in ethanol to afford 3, which upon refluxing in paraffin oil at 250°C gave 8-bromo-3-cyano-6-fluoroquinoline-4(1H)-one (4). Then, compound 4 was taken as a versatile building block that allows the synthesis of thieno[3,2-c]quinoline, pyrrolo[3,2-c]quinoline, and N-methylpyrrolo[3,2-c]quinoline systems. The newly synthesized compounds and their derivatives were characterized by elemental analysis and spectroscopy (IR, (1)H NMR, (13)C NMR, and mass). Furthermore, some of these synthesized compounds were screened for their biological activities against various pathogenic bacterial and fungal strains. Our results demonstrate that most of the synthesized compounds possess a significant broad antibacterial activity against all strains of both gram-positive and gram-negative bacteria. In addition, compound 5 showed remarkable antifungal activity. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  18. Study of an octadecaneuropeptide derived from diazepam binding inhibitor (DBI): biological activity and presence in rat brain

    Energy Technology Data Exchange (ETDEWEB)

    Ferrero, P.; Santi, M.R.; Conti-Tronconi, B.; Costa, E.; Guidotti, A.

    1986-02-01

    An endogenous brain neuropeptide with 104 amino acid residues that modulates ..gamma..-aminobutyric acid receptor function was termed DBI because it displaces diazepam from its specific brain binding sites. Tryptic digestion of DBI generates an octadecaneuropeptide (ODN) that is more potent than the parent compound in the displacement of specifically bound ..beta..-(/sup 3/H)carboline-3-carboxylate methyl ester ((/sup 3/H)BCCM) and in proconflict action. The proconflict action of ODN is antagonized by the imidobenzodiazepinone Ro 15-1788, which is a specific antagonist of ..beta..-carboline and benzodiazepine recognition sites. The ODN amino acid sequence is Gln-Ala-Thr-Val-Gly-Asp-Val-Asn-Thr-Asp-Arg-Pro-Gly-Leu-Leu-Asp-Leu-Lys. The pharmacological properties associated with this sequence were confirmed by comparing the activity of ODN generated from tryptic digestion of DBI with that of ODN obtained by synthesis. In primary cultures of cerebellar granule cells of rat, DBI, ODN, octapeptide, heptapeptide, and hexapeptide preferentially displace (/sup 3/H)BCCM over (/sup 3/H)flunitrazepam; moreover, they displace bound (/sup 3/H)BCCM completely but (/sup 3/H)flunitrazepam only by 50%. These data suggest that ODN includes a specific ligand for the ..gamma..-aminobutyric acid receptor regulatory site occupied by ..beta..-carbolines. Using rabbit antibodies directed against the NH/sub 2/-terminal portion of ODN, the authors detected ODN-like material in rat brain homogenates. However, whether this material is identical to the ODN generated by tryptic digestion of DBI remains to be established.

  19. NEW DERIVATIVES OF 2-R1-N-(5-R-1,3,4-THIADIAZOL-2-YL-BENZOLSULFONAMIDES: SYNTHESIS, PHYSICOCHEMICAL PROPERTIES AND BIOLOGICAL ACTIVITY PREDICTION

    Directory of Open Access Journals (Sweden)

    Sych I.V.

    2015-12-01

    Full Text Available Introduction: The analysis of modern literature, including overseas one, showed that a lot of the scientific researches is devoted to finding and creating biologically active compounds on base 1,3,4-thiadiazole. Derivatives of 1,3,4-thiadiazole are the large group of heterocyclic compounds with high rates of antimicrobial, antituberculosis, antidiabetic, antineoplastic and anticonvulsant activity. Material and methods: The purpose of this study was the expansion of sulfone derivatives substituted nitrogen-containing heterocyclic systems through the synthesis of 2-R1-N (5-R-1,3,4-thiadiazol-2-ilbenzolsulfonamides and prediction their pharmacological activity for future planning pharmacological screening. Synthesis of semi-products 2-amino-5-R-1,3,4-thiadiazoles was carried out by cyclization thiosemicarbazide and substituted derivatives of carboxylic acids in the presence of concentrated sulfuric acid. The synthesis of target compounds 2-R1-N(5-R-1,3,4-thiadiazol-2-ylbenzolsulfon-amides was carried out by N-acylation of 2-amino-5R-1,3,4-thiadiazole substituted benzolsul-fochlorides in the presence of anhydrous pyridine. The reaction proceeds by the classic SN2-mechanism. The resulting compounds are white crystalline substances, soluble in alcohol, chloroform and acetone, difficult to dissolve in water. Yields of obtained compounds was satisfactory (76-84%. The purity of the obtained compounds was determined by TLC. The structure of the obtained compounds was proved by elemental analysis, IR methods and 1H NMR spectroscopy. NMR 1H spectra were recorded at Bruker WM spectrometer (200 MHz; solvent DMSO-d6; chemical shifts were in ppm, internal standard (TMS (tetramethylsilane was used. The prognosis of biological activity for obtained compounds were carried out using the program PASS (Prediction of Activity Spectra for Substances in order to plan the further pharmacological screening. The program PASS predicts more than 500 kinds of biological

  20. Biologic rhythms derived from Siberian mammoths' hairs.

    Science.gov (United States)

    Spilde, Mike; Lanzirotti, Antonio; Qualls, Clifford; Phillips, Genevieve; Ali, Abdul-Mehdi; Agenbroad, Larry; Appenzeller, Otto

    2011-01-01

    Hair is preserved for millennia in permafrost; it enshrines a record of biologic rhythms and offers a glimpse at chronobiology as it was in extinct animals. Here we compare biologic rhythms gleaned from mammoth's hairs with those of modern human hair. Four mammoths' hairs came from varying locations in Siberia 4600 km, four time zones, apart ranging in age between 18,000 and 20,000 years before present. We used two contemporaneous human hairs for comparison. Power spectra derived from hydrogen isotope ratios along the length of the hairs gave insight into biologic rhythms, which were different in the mammoths depending on location and differed from humans. Hair growth for mammoths was ∼31 cms/year and ∼16 cms/year for humans. Recurrent annual rhythms of slow and fast growth varying from 3.4 weeks/cycles to 8.7 weeks/cycles for slow periods and 1.2 weeks/cycles to 2.2 weeks/cycles for fast periods were identified in mammoth's hairs. The mineral content of mammoth's hairs was measured by electron microprobe analysis (k-ratios), which showed no differences in sulfur amongst the mammoth hairs but significantly more iron then in human hair. The fractal nature of the data derived from the hairs became evident in Mandelbrot sets derived from hydrogen isotope ratios, mineral content and geographic location. Confocal microscopy and scanning electron microscopy showed varied degrees of preservation of the cuticle largely independent of age but not location of the specimens. X-ray fluorescence microprobe and fluorescence computed micro-tomography analyses allowed evaluation of metal distribution and visualization of hollow tubes in the mammoth's hairs. Seasonal variations in iron and copper content combined with spectral analyses gave insights into variation in food intake of the animals. Biologic rhythms gleaned from power spectral plots obtained by modern methods revealed life style and behavior of extinct mega-fauna.

  1. Biologic rhythms derived from Siberian mammoths' hairs.

    Directory of Open Access Journals (Sweden)

    Mike Spilde

    Full Text Available Hair is preserved for millennia in permafrost; it enshrines a record of biologic rhythms and offers a glimpse at chronobiology as it was in extinct animals. Here we compare biologic rhythms gleaned from mammoth's hairs with those of modern human hair. Four mammoths' hairs came from varying locations in Siberia 4600 km, four time zones, apart ranging in age between 18,000 and 20,000 years before present. We used two contemporaneous human hairs for comparison. Power spectra derived from hydrogen isotope ratios along the length of the hairs gave insight into biologic rhythms, which were different in the mammoths depending on location and differed from humans. Hair growth for mammoths was ∼31 cms/year and ∼16 cms/year for humans. Recurrent annual rhythms of slow and fast growth varying from 3.4 weeks/cycles to 8.7 weeks/cycles for slow periods and 1.2 weeks/cycles to 2.2 weeks/cycles for fast periods were identified in mammoth's hairs. The mineral content of mammoth's hairs was measured by electron microprobe analysis (k-ratios, which showed no differences in sulfur amongst the mammoth hairs but significantly more iron then in human hair. The fractal nature of the data derived from the hairs became evident in Mandelbrot sets derived from hydrogen isotope ratios, mineral content and geographic location. Confocal microscopy and scanning electron microscopy showed varied degrees of preservation of the cuticle largely independent of age but not location of the specimens. X-ray fluorescence microprobe and fluorescence computed micro-tomography analyses allowed evaluation of metal distribution and visualization of hollow tubes in the mammoth's hairs. Seasonal variations in iron and copper content combined with spectral analyses gave insights into variation in food intake of the animals. Biologic rhythms gleaned from power spectral plots obtained by modern methods revealed life style and behavior of extinct mega-fauna.

  2. Metal based biologically active compounds: Design, synthesis, DNA binding and antidiabetic activity of 6-methyl-3-formyl chromone derived hydrazones and their metal (II) complexes.

    Science.gov (United States)

    Philip, Jessica Elizabeth; Shahid, Muhammad; Prathapachandra Kurup, M R; Velayudhan, Mohanan Puzhavoorparambil

    2017-10-01

    Two chromone hydrazone ligands HL 1 and HL 2 were synthesized and characterized by elemental analyses, IR, 1 H NMR & 13 C NMR, electronic absorption and mass spectra. The reactions of the chromone hydrazones with transition metals such as Ni, Cu, and Zn (II) salts of acetate afforded mononuclear metal complexes. Characterization and structure elucidation of the prepared chromone hydrazone metal (II) complexes were done by elemental, IR, electronic, EPR spectra and thermo gravimetric analyses as well as conductivity and magnetic susceptibility measurements. The spectroscopic data showed that the ligand acts as a mono basic bidentate with coordination sites are azomethine nitrogen and hydrazonic oxygen, and they exhibited distorted geometry. The biological studies involved antidiabetic activity i.e. enzyme inhibition of α-amylase and α-glucosidase, Calf Thymus - DNA (CT-DNA) interaction and molecular docking. Potential capacity of synthesized compounds to inhibit the α-amylase and α-glucosidase activity was assayed whereas DNA interaction studies were carried out with the help UV-Vis absorption titration and viscosity method. The docking studies of chromone hydrazones show that they are minor groove binders. Complexes were found to be good DNA - intercalates. Chromone hydrazones and its transition metal complexes have shown comparable antidiabetic activity with a standard drug acarbose. Copyright © 2017 Elsevier B.V. All rights reserved.

  3. Synthesis, characterization and biological evaluation of tryptamine based benzamide derivatives.

    Science.gov (United States)

    Aftab, Kiran; Aslam, Kinza; Kousar, Shazia; Nadeem, Muhammad Jawad Ul Hasan

    2016-03-01

    Benzamides and tryptamine are biologically significant compounds, therefore, various benzamide analogous of tryptamine have been efficiently synthesized using tryptamine and different benzoyl chlorides, in order to find new biologically active compounds. The resulting products were then characterized by melting point determination, calculation of Rf values and LC-MS techniques. At last, structure activity relationship (SAR) of the synthesized compounds was evaluated against two microbial strains; Bacillus subtilis and Aspergillus niger. All the five prepared products have shown high yield, sharp characterization and significant resistance against the growth of tested microorganism, providing a new range of tryptamine based benzamide derivatives having significant antimicrobial activities.

  4. Spectral studies, thermal investigation and biological activity of some metal complexes derived from (E)-N‧-(1-(4-aminophenyl)ethylidene)morpholine-4-carbothiohydrazide

    Science.gov (United States)

    El-Samanody, El-Sayed A.; Polis, Magdy W.; Emara, Esam M.

    2017-09-01

    A new series of biologically active Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) complexes derived from the novel thiosemicarbazone ligand; (E)-N‧-(1-(4-aminophenyl)ethylidene)morpholine-4-carbothiohydrazide (HL) were synthesized. The mode of bonding of the ligand and the geometrical structures of its metal complexes were achieved by different analytical and spectral methods. The ligand coordinated with metal ions in a neutral bidentate fashion through the thione sulfur and azomethine nitrogen atoms. All metal complexes adopted octahedral geometry, except Cu(II) complexes (3, 6, 7) which have a square planar structure. The general thermal decomposition pathways of the ligand along with its metal complexes were explained. The thermal stability of the complexes is controlled by the number of outer and inner sphere water molecules, ionic radii and the steric hindrance. The activation thermodynamic parameters; (activation energy (E*), enthalpy of activation (ΔH*), entropy of activation (ΔS*) and Gibbs free energy (ΔG*)) along with order of reaction (n) were estimated from DTG curves. The ESR spectra of Cu(II) complexes indicated that (dx2-y2)1 is the ground state with covalence character of metal-ligand bonds. The molluscicidal and biochemical effects of the ligand and its Ni(II); Cu(II) complexes (2; 3, 5, 7) along with their combinations with metaldehyde were screened in vitro on the mucous gland of Eobania vermiculata. The tested compounds exhibited a significant toxicity against the tested animals and have almost the same toxic effect of metaldehyde which increases the mucous secretion of the snails and leads to death.

  5. Biologic Rhythms Derived from Siberian Mammoths Hairs

    Energy Technology Data Exchange (ETDEWEB)

    M Spilde; A Lanzirotti; C Qualls; G Phillips; A Ali; L Agenbroad; O Appenzeller

    2011-12-31

    Hair is preserved for millennia in permafrost; it enshrines a record of biologic rhythms and offers a glimpse at chronobiology as it was in extinct animals. Here we compare biologic rhythms gleaned from mammoth's hairs with those of modern human hair. Four mammoths' hairs came from varying locations in Siberia 4600 km, four time zones, apart ranging in age between 18,000 and 20,000 years before present. We used two contemporaneous human hairs for comparison. Power spectra derived from hydrogen isotope ratios along the length of the hairs gave insight into biologic rhythms, which were different in the mammoths depending on location and differed from humans. Hair growth for mammoths was {approx}31 cms/year and {approx}16 cms/year for humans. Recurrent annual rhythms of slow and fast growth varying from 3.4 weeks/cycles to 8.7 weeks/cycles for slow periods and 1.2 weeks/cycles to 2.2 weeks/cycles for fast periods were identified in mammoth's hairs. The mineral content of mammoth's hairs was measured by electron microprobe analysis (k-ratios), which showed no differences in sulfur amongst the mammoth hairs but significantly more iron then in human hair. The fractal nature of the data derived from the hairs became evident in Mandelbrot sets derived from hydrogen isotope ratios, mineral content and geographic location. Confocal microscopy and scanning electron microscopy showed varied degrees of preservation of the cuticle largely independent of age but not location of the specimens. X-ray fluorescence microprobe and fluorescence computed micro-tomography analyses allowed evaluation of metal distribution and visualization of hollow tubes in the mammoth's hairs. Seasonal variations in iron and copper content combined with spectral analyses gave insights into variation in food intake of the animals. Biologic rhythms gleaned from power spectral plots obtained by modern methods revealed life style and behavior of extinct mega-fauna.

  6. Comparative analysis of biological activities of Der p I-derived peptides on Fc epsilon receptor-bearing cells from Dermatophagoides pteronyssinus-sensitive patients.

    Science.gov (United States)

    Jeannin, P; Pestel, J; Bossus, M; Lassalle, P; Tartar, A; Tonnel, A B

    1993-04-01

    The ability of four uncoupled synthetic peptides (p52-71, p117-133, p176-187, p188-199) derived from Der p I, a major allergen from the house dust mite Dermatophagoides pteronyssinus (Dpt) to stimulate Fc epsilon R+ cells from Dpt-sensitive patients was comparatively analysed. Each free peptide may specifically stimulate basophils (Fc epsilon RI+ cells) and platelets (Fc epsilon RII+ cells) from patients with significant levels of anti-Der p I IgE antibodies; p52-71 and p117-133 appear the best cell stimulation inducers. Both concentration-dependent biological activities of Der p I-peptide on Fc epsilon R+ cells are enhanced by coupling peptide to a carrier (as human serum albumin). Interestingly each Der p I-sensitive patient tested presents an individual pattern of response to peptide. Thus, from our results it appears that different Der p I sequences could be involved in the immune response to Der p I.

  7. Chitooligosaccharide and Its Derivatives: Preparation and Biological Applications

    Directory of Open Access Journals (Sweden)

    Gaurav Lodhi

    2014-01-01

    Full Text Available Chitin is a natural polysaccharide of major importance. This biopolymer is synthesized by an enormous number of living organisms; considering the amount of chitin produced annually in the world, it is the most abundant polymer after cellulose. The most important derivative of chitin is chitosan, obtained by partial deacetylation of chitin under alkaline conditions or by enzymatic hydrolysis. Chitin and chitosan are known to have important functional activities but poor solubility makes them difficult to use in food and biomedicinal applications. Chitooligosaccharides (COS are the degraded products of chitosan or chitin prepared by enzymatic or chemical hydrolysis of chitosan. The greater solubility and low viscosity of COS have attracted the interest of many researchers to utilize COS and their derivatives for various biomedical applications. In light of the recent interest in the biomedical applications of chitin, chitosan, and their derivatives, this review focuses on the preparation and biological activities of chitin, chitosan, COS, and their derivatives.

  8. SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 3,6 ...

    African Journals Online (AJOL)

    SYNTHESIS AND BIOLOGICAL ACTIVITIES OF 3,6-DISUBSTITUTED-1,2,4-. TRIAZOLO-1,3 ... Thus, many chemists reported synthesis and antimicrobial activity of some 1,2,4-triazolothiadiazole derivatives in ..... N.H. Synthesis and biological activity of oxadiazole and triazolothiadiazole derivatives as tyrosinase inhibitors.

  9. Biological Derived Nanomotors in a ``Domino Fashion''

    Science.gov (United States)

    Maksoed, W. H.

    2015-11-01

    For disproportionation of H2 O2 , we also considers an electrokinetic mechanism they appear.So far, the more efficient micro/nanoscale motors are derived from biological systems [2003]. Besides, a control experimenting using 3 stripped Au/Pt/Au rods with catalyzed the composition of H2 O2 , at a similar rate-Walter F Paxton: ``Catalytic Nanomotors,'' JACS, 2004. We also intended to accomaplishes the HCCI quotes from Marcin Frackowiak, dissertation, 2009, just in several characters seems as twin of IGNITION through IceCube document project held since Oct 11, 2001 ever concludes as ``saw none'' so they can be follows the ITER/IFMIF. Refers to S29286 file in UI retrieved: ``magnetic quantum-dot cellular automata which is nonvolatile & lower power consist of nanomagnets. Since they are magnetically coupled, logic can be performed by switching, on the other hand in a DOMINO fashion..'' [A. Klenm: ``Fabrication of Magnetic Tunnel Junction-based Spintronic Devices..,'' convocation, Aug 11-14, 2010]. Acknowledgments devotes to BB Mandelbrot: ``Fractal Geometry: What is it & What Does it do?''.

  10. Chemical Composition and Biological Activity of Extracts Obtained by Supercritical Extraction and Ethanolic Extraction of Brown, Green and Red Propolis Derived from Different Geographic Regions in Brazil.

    Science.gov (United States)

    Machado, Bruna Aparecida Souza; Silva, Rejane Pina Dantas; Barreto, Gabriele de Abreu; Costa, Samantha Serra; Silva, Danielle Figuerêdo da; Brandão, Hugo Neves; Rocha, José Luiz Carneiro da; Dellagostin, Odir Antônio; Henriques, João Antônio Pegas; Umsza-Guez, Marcelo Andres; Padilha, Francine Ferreira

    2016-01-01

    The variations in the chemical composition, and consequently, on the biological activity of the propolis, are associated with its type and geographic origin. Considering this fact, this study evaluated propolis extracts obtained by supercritical extraction (SCO2) and ethanolic extraction (EtOH), in eight samples of different types of propolis (red, green and brown), collected from different regions in Brazil. The content of phenolic compounds, flavonoids, in vitro antioxidant activity (DPPH and ABTS), Artepillin C, p-coumaric acid and antimicrobial activity against two bacteria were determined for all extracts. For the EtOH extracts, the anti-proliferative activity regarding the cell lines of B16F10, were also evaluated. Amongst the samples evaluated, the red propolis from the Brazilian Northeast (states of Sergipe and Alagoas) showed the higher biological potential, as well as the larger content of antioxidant compounds. The best results were shown for the extracts obtained through the conventional extraction method (EtOH). However, the highest concentrations of Artepillin C and p-coumaric acid were identified in the extracts from SCO2, indicating a higher selectivity for the extraction of these compounds. It was verified that the composition and biological activity of the Brazilian propolis vary significantly, depending on the type of sample and geographical area of collection.

  11. Chemical Composition and Biological Activity of Extracts Obtained by Supercritical Extraction and Ethanolic Extraction of Brown, Green and Red Propolis Derived from Different Geographic Regions in Brazil

    Science.gov (United States)

    Machado, Bruna Aparecida Souza; Silva, Rejane Pina Dantas; Barreto, Gabriele de Abreu; Costa, Samantha Serra; da Silva, Danielle Figuerêdo; Brandão, Hugo Neves; da Rocha, José Luiz Carneiro; Dellagostin, Odir Antônio; Henriques, João Antônio Pegas; Umsza-Guez, Marcelo Andres; Padilha, Francine Ferreira

    2016-01-01

    The variations in the chemical composition, and consequently, on the biological activity of the propolis, are associated with its type and geographic origin. Considering this fact, this study evaluated propolis extracts obtained by supercritical extraction (SCO2) and ethanolic extraction (EtOH), in eight samples of different types of propolis (red, green and brown), collected from different regions in Brazil. The content of phenolic compounds, flavonoids, in vitro antioxidant activity (DPPH and ABTS), Artepillin C, p-coumaric acid and antimicrobial activity against two bacteria were determined for all extracts. For the EtOH extracts, the anti-proliferative activity regarding the cell lines of B16F10, were also evaluated. Amongst the samples evaluated, the red propolis from the Brazilian Northeast (states of Sergipe and Alagoas) showed the higher biological potential, as well as the larger content of antioxidant compounds. The best results were shown for the extracts obtained through the conventional extraction method (EtOH). However, the highest concentrations of Artepillin C and p-coumaric acid were identified in the extracts from SCO2, indicating a higher selectivity for the extraction of these compounds. It was verified that the composition and biological activity of the Brazilian propolis vary significantly, depending on the type of sample and geographical area of collection. PMID:26745799

  12. Chemical Composition and Biological Activity of Extracts Obtained by Supercritical Extraction and Ethanolic Extraction of Brown, Green and Red Propolis Derived from Different Geographic Regions in Brazil.

    Directory of Open Access Journals (Sweden)

    Bruna Aparecida Souza Machado

    Full Text Available The variations in the chemical composition, and consequently, on the biological activity of the propolis, are associated with its type and geographic origin. Considering this fact, this study evaluated propolis extracts obtained by supercritical extraction (SCO2 and ethanolic extraction (EtOH, in eight samples of different types of propolis (red, green and brown, collected from different regions in Brazil. The content of phenolic compounds, flavonoids, in vitro antioxidant activity (DPPH and ABTS, Artepillin C, p-coumaric acid and antimicrobial activity against two bacteria were determined for all extracts. For the EtOH extracts, the anti-proliferative activity regarding the cell lines of B16F10, were also evaluated. Amongst the samples evaluated, the red propolis from the Brazilian Northeast (states of Sergipe and Alagoas showed the higher biological potential, as well as the larger content of antioxidant compounds. The best results were shown for the extracts obtained through the conventional extraction method (EtOH. However, the highest concentrations of Artepillin C and p-coumaric acid were identified in the extracts from SCO2, indicating a higher selectivity for the extraction of these compounds. It was verified that the composition and biological activity of the Brazilian propolis vary significantly, depending on the type of sample and geographical area of collection.

  13. Synthetic Methods and Exploring Biological Potential of Various Substituted Quinoxalin-2-one Derivatives

    OpenAIRE

    Mohammad Asif

    2016-01-01

    Substituted quinoxaline have considerable interest in chemistry, biology and pharmacology. Quinoxaline derivatives are capable with variety of biological activities and possess different biological activities, of which the most potent are anti-microbial, analgesic and anti-inflammatory activities. It facilitated the researchers to develop various methods for their synthesis and their applications. In this review represented different methods of synthesis, reactivity and various biological act...

  14. Advantages and limitations of classic and 3D QSAR approaches in nano-QSAR studies based on biological activity of fullerene derivatives

    Science.gov (United States)

    Jagiello, Karolina; Grzonkowska, Monika; Swirog, Marta; Ahmed, Lucky; Rasulev, Bakhtiyor; Avramopoulos, Aggelos; Papadopoulos, Manthos G.; Leszczynski, Jerzy; Puzyn, Tomasz

    2016-09-01

    In this contribution, the advantages and limitations of two computational techniques that can be used for the investigation of nanoparticles activity and toxicity: classic nano-QSAR (Quantitative Structure-Activity Relationships employed for nanomaterials) and 3D nano-QSAR (three-dimensional Quantitative Structure-Activity Relationships, such us Comparative Molecular Field Analysis, CoMFA/Comparative Molecular Similarity Indices Analysis, CoMSIA analysis employed for nanomaterials) have been briefly summarized. Both approaches were compared according to the selected criteria, including: efficiency, type of experimental data, class of nanomaterials, time required for calculations and computational cost, difficulties in the interpretation. Taking into account the advantages and limitations of each method, we provide the recommendations for nano-QSAR modellers and QSAR model users to be able to determine a proper and efficient methodology to investigate biological activity of nanoparticles in order to describe the underlying interactions in the most reliable and useful manner.

  15. Advantages and limitations of classic and 3D QSAR approaches in nano-QSAR studies based on biological activity of fullerene derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Jagiello, Karolina; Grzonkowska, Monika; Swirog, Marta [University of Gdansk, Laboratory of Environmental Chemometrics, Faculty of Chemistry, Institute for Environmental and Human Health Protection (Poland); Ahmed, Lucky; Rasulev, Bakhtiyor [Jackson State University, Interdisciplinary Nanotoxicity Center, Department of Chemistry and Biochemistry (United States); Avramopoulos, Aggelos; Papadopoulos, Manthos G. [National Hellenic Research Foundation, Institute of Biology, Pharmaceutical Chemistry and Biotechnology (Greece); Leszczynski, Jerzy [Jackson State University, Interdisciplinary Nanotoxicity Center, Department of Chemistry and Biochemistry (United States); Puzyn, Tomasz, E-mail: t.puzyn@qsar.eu.org [University of Gdansk, Laboratory of Environmental Chemometrics, Faculty of Chemistry, Institute for Environmental and Human Health Protection (Poland)

    2016-09-15

    In this contribution, the advantages and limitations of two computational techniques that can be used for the investigation of nanoparticles activity and toxicity: classic nano-QSAR (Quantitative Structure–Activity Relationships employed for nanomaterials) and 3D nano-QSAR (three-dimensional Quantitative Structure–Activity Relationships, such us Comparative Molecular Field Analysis, CoMFA/Comparative Molecular Similarity Indices Analysis, CoMSIA analysis employed for nanomaterials) have been briefly summarized. Both approaches were compared according to the selected criteria, including: efficiency, type of experimental data, class of nanomaterials, time required for calculations and computational cost, difficulties in the interpretation. Taking into account the advantages and limitations of each method, we provide the recommendations for nano-QSAR modellers and QSAR model users to be able to determine a proper and efficient methodology to investigate biological activity of nanoparticles in order to describe the underlying interactions in the most reliable and useful manner.

  16. Advantages and limitations of classic and 3D QSAR approaches in nano-QSAR studies based on biological activity of fullerene derivatives

    International Nuclear Information System (INIS)

    Jagiello, Karolina; Grzonkowska, Monika; Swirog, Marta; Ahmed, Lucky; Rasulev, Bakhtiyor; Avramopoulos, Aggelos; Papadopoulos, Manthos G.; Leszczynski, Jerzy; Puzyn, Tomasz

    2016-01-01

    In this contribution, the advantages and limitations of two computational techniques that can be used for the investigation of nanoparticles activity and toxicity: classic nano-QSAR (Quantitative Structure–Activity Relationships employed for nanomaterials) and 3D nano-QSAR (three-dimensional Quantitative Structure–Activity Relationships, such us Comparative Molecular Field Analysis, CoMFA/Comparative Molecular Similarity Indices Analysis, CoMSIA analysis employed for nanomaterials) have been briefly summarized. Both approaches were compared according to the selected criteria, including: efficiency, type of experimental data, class of nanomaterials, time required for calculations and computational cost, difficulties in the interpretation. Taking into account the advantages and limitations of each method, we provide the recommendations for nano-QSAR modellers and QSAR model users to be able to determine a proper and efficient methodology to investigate biological activity of nanoparticles in order to describe the underlying interactions in the most reliable and useful manner.

  17. Brassinosteroids: synthesis and biological activities

    Czech Academy of Sciences Publication Activity Database

    Oklešťková, Jana; Rárová, Lucie; Kvasnica, Miroslav; Strnad, Miroslav

    2015-01-01

    Roč. 14, č. 6 (2015), s. 1053-1072 ISSN 1568-7767 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Brassinosteroids * Chemical synthesis * Plant biological activity Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.686, year: 2015

  18. Phytochemical Profile and Evaluation of the Biological Activities of Essential Oils Derived from the Greek Aromatic Plant Species Ocimum basilicum, Mentha spicata, Pimpinella anisum and Fortunella margarita.

    Science.gov (United States)

    Fitsiou, Eleni; Mitropoulou, Gregoria; Spyridopoulou, Katerina; Tiptiri-Kourpeti, Angeliki; Vamvakias, Manolis; Bardouki, Haido; Panayiotidis, Mihalis Ι; Galanis, Alex; Kourkoutas, Yiannis; Chlichlia, Katerina; Pappa, Aglaia

    2016-08-16

    Natural products, known for their medicinal properties since antiquity, are continuously being studied for their biological properties. In the present study, we analyzed the composition of the volatile preparations of essential oils of the Greek plants Ocimum basilicum (sweet basil), Mentha spicata (spearmint), Pimpinella anisum (anise) and Fortunella margarita (kumquat). GC/MS analyses revealed that the major components in the essential oil fractions, were carvone (85.4%) in spearmint, methyl chavicol (74.9%) in sweet basil, trans-anethole (88.1%) in anise, and limonene (93.8%) in kumquat. We further explored their biological potential by studying their antimicrobial, antioxidant and antiproliferative activities. Only the essential oils from spearmint and sweet basil demonstrated cytotoxicity against common foodborne bacteria, while all preparations were active against the fungi Saccharomyces cerevisiae and Aspergillus niger. Antioxidant evaluation by DPPH and ABTS radical scavenging activity assays revealed a variable degree of antioxidant potency. Finally, their antiproliferative potential was tested against a panel of human cancer cell lines and evaluated by using the sulforhodamine B (SRB) assay. All essential oil preparations exhibited a variable degree of antiproliferative activity, depending on the cancer model used, with the most potent one being sweet basil against an in vitro model of human colon carcinoma.

  19. Phytochemical Profile and Evaluation of the Biological Activities of Essential Oils Derived from the Greek Aromatic Plant Species Ocimum basilicum, Mentha spicata, Pimpinella anisum and Fortunella margarita

    Directory of Open Access Journals (Sweden)

    Eleni Fitsiou

    2016-08-01

    Full Text Available Natural products, known for their medicinal properties since antiquity, are continuously being studied for their biological properties. In the present study, we analyzed the composition of the volatile preparations of essential oils of the Greek plants Ocimum basilicum (sweet basil, Mentha spicata (spearmint, Pimpinella anisum (anise and Fortunella margarita (kumquat. GC/MS analyses revealed that the major components in the essential oil fractions, were carvone (85.4% in spearmint, methyl chavicol (74.9% in sweet basil, trans-anethole (88.1% in anise, and limonene (93.8% in kumquat. We further explored their biological potential by studying their antimicrobial, antioxidant and antiproliferative activities. Only the essential oils from spearmint and sweet basil demonstrated cytotoxicity against common foodborne bacteria, while all preparations were active against the fungi Saccharomyces cerevisiae and Aspergillus niger. Antioxidant evaluation by DPPH and ABTS radical scavenging activity assays revealed a variable degree of antioxidant potency. Finally, their antiproliferative potential was tested against a panel of human cancer cell lines and evaluated by using the sulforhodamine B (SRB assay. All essential oil preparations exhibited a variable degree of antiproliferative activity, depending on the cancer model used, with the most potent one being sweet basil against an in vitro model of human colon carcinoma.

  20. Copper(II Complexes with Ligands Derived from 4-Amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one: Synthesis and Biological Activity

    Directory of Open Access Journals (Sweden)

    Raluca Cernat

    2006-11-01

    Full Text Available The synthesis of Cu(II complexes derived from Schiff base ligands obtainedby the condensation of 2-hydroxybenzaldehyde or terephtalic aldehyde with 4-amino-antipyrine (4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one is presented. The newlyprepared compounds were characterized by 1H-NMR, UV-VIS, IR and ESRspectroscopy. The determination of the antimicrobial activity of the ligands and of thecomplexes was carried out on samples of Escherichia coli, Klebsiella pneumoniae,Acinetobacter boumanii, Pseudomonas aeruginosa, Staphylococcus aureus and Candidasp. The qualitative and quantitative antimicrobial activity test results proved that all theprepared complexes are very active, especially against samples of Ps. aeruginosa, A.Boumanii, E. coli and S. aureus.

  1. Synthesis, antibacterial activity, and biological evaluation of formyl hydroxyamino derivatives as novel potent peptide deformylase inhibitors against drug-resistant bacteria.

    Science.gov (United States)

    Yang, Shouning; Shi, Wei; Xing, Dong; Zhao, Zheng; Lv, Fengping; Yang, Liping; Yang, Yushe; Hu, Wenhao

    2014-10-30

    Peptide deformylase (PDF) has been identified as a promising target for novel antibacterial agents. In this study, a series of novel formyl hydroxyamino derivatives were designed and synthesized as PDF inhibitors and their antibacterial activities were evaluated. Among the potent PDF inhibitors (1o, 1q, 1o', 1q', and 1x), in vivo studies showed that compound 1q possesses mild toxicity, a good pharmacokinetic profile and protective effects. The good in vivo efficacy and low toxicity suggest that this class of compounds has potential for development and use in future antibacterial drugs. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  2. Design, synthesis and biological evaluation of hybrid bioisoster derivatives of N-acylhydrazone and furoxan groups with potential and selective anti-Trypanosoma cruzi activity.

    Science.gov (United States)

    Massarico Serafim, Ricardo Augusto; Gonçalves, José Eduardo; de Souza, Felipe Pereira; de Melo Loureiro, Ana Paula; Storpirtis, Silvia; Krogh, Renata; Andricopulo, Adriano Defini; Dias, Luiz Carlos; Ferreira, Elizabeth Igne

    2014-07-23

    Hybrid bioisoster derivatives from N-acylhydrazones and furoxan groups were designed with the objective of obtaining at least a dual mechanism of action: cruzain inhibition and nitric oxide (NO) releasing activity. Fifteen designed compounds were synthesized varying the substitution in N-acylhydrazone and in furoxan group as well. They had its anti-Trypanosoma cruzi activity in amastigotes forms, NO releasing potential and inhibitory cruzain activity evaluated. The two most active compounds (6, 14) both in the parasite amastigotes and in the enzyme contain the nitro group in para position of the aromatic ring. The permeability screening in Caco-2 cell and cytotoxicity assay in human cells were performed for those most active compounds and both showed to be less cytotoxic than the reference drug, benznidazole. Compound 6 was the most promising, since besides activity it showed good permeability and selectivity index, higher than the reference drug. Thereby the compound 6 was considered as a possible candidate for additional studies. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  3. Antileishmanial activity of polycyclic derivatives

    Directory of Open Access Journals (Sweden)

    Sarciron M.E.

    2005-09-01

    Full Text Available 33 polycyclic derivatives have been studied and tested on Leishmania donovani and L. major promastigotes. Their antileishmanial activity was assessed in vitro and an assay of their cytotoxicity was realized on human myelomonocytic cell line. The reference molecules used in the assays were amphotericin B and pentamidine. Among the compounds tested, 29 possess an antileishmanial activity; 25 of those were more active against L. donovani than amphotericin B, and nine were as effective as amphotericin B against L. major. Many synthesized derivatives were more active against L.donovani than against L. major. The cytotoxicity studies have shown that among the thirty-three derivatives tested, 12 molecules have an IC50 towards THP-1 cells about equal than that reference drugs, the 21 other derivatives are much less toxic. A 3D QSAR study was undertaken and has permitted to predict activity against L. donovani and L. major and to highlight critical area to optimize activity against the two species.

  4. 9,10-Dihydrophenanthrene derivatives and one 1,4-anthraquinone firstly isolated from Dioscorea zingiberensis C. H. Wright and their biological activities.

    Science.gov (United States)

    Du, Dan; Zhang, Rui; Xing, Zhihua; Liang, Yuyan; Li, Shengfu; Jin, Tao; Xia, Qing; Long, Dan; Xin, Guang; Wang, Guangzhi; Huang, Wen

    2016-03-01

    Two new phenanthrene derivatives, 2,5,7-trimethoxy-9,10-dihydrophenanthrene-1,4-dione (1) and 2,5,6-trihydroxy-3,4-dimethoxy-9,10-dihydrophenanthrene (3), one new anthracenedione, 2,5,7-trimethoxyanthracene-1,4-dione (2), together with two known 9,10-dihydrophenanthrenes (4-5) were isolated from the rhizomes of Dioscorea zingiberensis C. H. Wright. The structures of these new compounds were established based on extensive NMR spectroscopy. Several isolated compounds were evaluated for the inhibition against nitric oxide (NO) production in the lipopolysaccharide (LPS)-activated RAW 264.7 macrophage cell line, DPPH radical scavenging, and inhibitory activity on Free Fatty Acids (FFAs) induced triglyceride accumulation in HepG2 cells. Compound 2 exhibited moderate anti-inflammatory activity, compound 3 possessed comparable DPPH radical scavenging activity as Vitamin C, compounds 2 and 4 showed potent inhibitory activities on triglyceride accumulation. Copyright © 2015 Elsevier B.V. All rights reserved.

  5. Synthesis Characterization and Biological Activity Study of New Schiff and Mannich Bases and Some Metal Complexes Derived from Isatin and Dithiooxamide

    Science.gov (United States)

    Abdulghani, Ahlam J.; Abbas, Nada M.

    2011-01-01

    Two new Schiff and Mannich bases, namely, 1-Morpholinomethyl-3(1′ -N-dithiooxamide)iminoisatin (LIH) and 1-diphenylaminomethyl-3-1′-N-dithiooxamide)iminoisatin (LIIH), were prepared from condensation reaction of new Schiff base 3-(1′-N-dithiooxamide)iminoisatin (SBH) with morpholine or diphenylamine respectively in presence of formaldehyde . The structures were characterized by IR, 1HNMR, mass spectrometry, and CHN analyses. Metal complexes of the two ligands were synthesized, and their structures were characterized by elemental analyses, atomic absorption, IR and UV-visible spectra, molar conductivity, and magnetic moment determination. All complexes showed octahedral geometries except palladium complexes which were square planar. The biological activity of the prepared compounds and some selected metal complexes was tested against three types of bacteria and against cell line of human epidermoid larynx carcinoma (Hep-2). PMID:21949661

  6. Recent advances in gossypol derivatives and analogs: a chemistry and biology view.

    Science.gov (United States)

    Lu, Yuzhi; Li, Jun; Dong, Chun-E; Huang, Jian; Zhou, Hai-Bing; Wang, Wei

    2017-07-01

    Gossypol as a natural occurring polyphenol has been studied in a wide range of therapeutic contexts for a long time. The chemical modifications on gossypol were limited due to the unique chemical properties of polyphenols. The design and synthesis of gossypol derivatives and the exploration of their biological activities are the interest of the synthetic chemists, medicinal chemists and pharmacologists. Thus, the progress of diverse gossypol derivatives and analogs' synthesis, biological activities, mechanism elucidation and drug discovery based on gossypol scaffold is summarized.

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

    Directory of Open Access Journals (Sweden)

    Yamaji N

    2014-11-01

    line. Mebiol Gel based hepatocytes had better differentiation and the cells were susceptible to hepatitis C virus replication. The Mebiol Gel based 3D culture system can be used as a better cell culture system for viral studies. Potential Solutions: The works presented in the IIDIAS session have portrayed that original invention in any field when subjected to multi-disciplinary interaction after carefully evaluating the potentials can lead to novel solutions. Though the experts in various disciplines in the reported work have got to interact by chance or due to geographical proximity to each other, when a networking platform to throw such ideas to a forum with mutually rewarding opportunities given for discussion and planning of interactive researches is made possible, novel solutions may not be impossible, if the target platform is well understood within the limitations of each stake holder. Creation of a niche or a suitable environment for such multi disciplinary interaction may prevail and work to its best in a physical state of interaction but advances in information technology has broken the need for such physical interaction among peers to bring out novel solutions. Interactions across specialties in the IIDIAS session help in identifying roles for the invention in other fields which may not be directly related to healthcare. The probable solutions and advantages by combining the electro-physical activity-derived biosimilar and the chemically synthesized polymer described in the study include: A novel platform for in vitro culture of HCV having been described, similar platforms for not so easily cultivable viruses can also be developed. The 3D viral culture technology can be exploited to study the replication process and other intricacies of the virus in in vitro culture. When in vitro expansion of viruses in an appropriate manner becomes feasible, anti-viral agents, either virostatic or virucidal, herbal or synthetic biosimilars can be analysed to come out with

  8. Phosphorus Determination by Derivative Activation Analysis: A Multifaceted Radiochemical Application.

    Science.gov (United States)

    Kleppinger, E. W.; And Others

    1984-01-01

    Although determination of phosphorus is important in biology, physiology, and environmental science, traditional gravimetric and colorimetric methods are cumbersome and lack the requisite sensitivity. Therefore, a derivative activation analysis method is suggested. Background information, procedures, and results are provided. (JN)

  9. Synthesis, characterization and biological activity of some platinum(II) complexes with Schiff bases derived from salicylaldehyde, 2-furaldehyde and phenylenediamine

    Science.gov (United States)

    Gaballa, Akmal S.; Asker, Mohsen S.; Barakat, Atiat S.; Teleb, Said M.

    2007-05-01

    Four platinum(II) complexes of Schiff bases derived from salicylaldehyde and 2-furaldehyde with o- and p-phenylenediamine were reported and characterized based on their elemental analyses, IR and UV-vis spectroscopy and thermal analyses (TGA). The complexes were found to have the general formula [Pt(L)(H 2O) 2]Cl 2· nH 2O (where n = 0 for complexes 1, 3, 4; n = 1 for complex 2. The data obtained show that Schiff bases were interacted with Pt(II) ions in the neutral form as a bidentate ligand and the oxygens rather than the nitrogens are the most probable coordination sites. Square planar geometrical structure with two coordinated water molecules were proposed for all complexes The free ligands, and their metal complexes were screened for their antimicrobial activities against the following bacterial species: E. coli, B. subtilis, P. aereuguinosa, S. aureus; fungus A. niger, A. fluves; and the yeasts C. albican, S. cervisiea. The activity data show that the platinum(II) complexes are more potent antimicrobials than the parent Schiff base ligands against one or more microorganisms.

  10. Benzimidazoles: A biologically active compounds

    Directory of Open Access Journals (Sweden)

    Salahuddin

    2017-02-01

    Full Text Available Synthesis of commercially available benzimidazole involves condensation of o-phenylenediamine with formic acid. The most prominent benzimidazole compound in nature is N-riosyldimethylbenzimidazole, which serves as a axial ligand for cobalt in vitamin B12. The benzimidazole and its derivatives play a very important role as a therapeutic agent e.g. antiulcer and anthelmintic drugs. Apart from this the benzimidazole derivatives exhibit pharmacological activities such as antimicrobial, antiviral, anticancer, anti-inflammatory, analgesic, etc. The substituted benzimidazoles are summarized in this review to know about the chemistry as well as pharmacological activities.

  11. Sonochemical-assisted fabrication of biologically active chiral poly(ester-imide/TiO2 bionanocomposites derived from L-methionine and L-tyrosine amino acids

    Directory of Open Access Journals (Sweden)

    2011-09-01

    Full Text Available A new chiral poly(ester-imide (PEI was prepared via direct polyesterification of N,N'-(pyromellitoyl-bis-(Ltyrosine dimethyl ester and N-trimellitylimido-L-methionine using tosyl chloride/pyridine/N,N'-dimethylformamide system as a condensing agent. The resulting new chiral polymer was obtained in good yield and had good thermal stability as well as good solubility in common organic solvents. After that, PEI/titanium bionanocomposites (PEI/TiO2 BNCs were prepared using the modified nanosized TiO2 via sonochemical reaction that can accelerate hydrolysis, increase collision chance for the reactive system and improve the dispersion of the nanoparticles in polymer matrix. The scanning electron microscopy (SEM, field emission scanning electron microscopy (FE-SEM and transmission electron microscopy (TEM results indicated that there is no aggregation of a large quantity of particles. Thermogravimetric analysis (TGA confirmed that the heat stability of the BNC polymers in the temperature range of 400–800ºC was enhanced by addition of TiO2 nanoparticles. Furthermore, in vitro toxicity test was employed for assessing the sensitivity of these compounds to microbial degradation. To this purpose, polymer and PEI/TiO2 BNCs were investigated under soil burial conditions. The results of this study revealed that polymer and its BNCs are biologically active and non-toxic in the natural environment although some antimicrobial properties were found for BNCs.

  12. Microwave Mediated Organic Reaction: A Convenient Approach for Rapid and Efficient Synthesis of Biologically Active Substituted 1,3-Dihydro-2H-indol-2-one Derivatives

    Directory of Open Access Journals (Sweden)

    Jnyanaranjan Panda

    2013-01-01

    Full Text Available A simple and efficient method has been developed for the synthesis of 1,3-dihydro-2H-indol-2-one derivatives using microwave irradiation technique. By taking advantage of the efficient source of energy of microwave, compound libraries for lead generation and optimization can be assembled in a fraction of time. In the present work, first the Schiff’s bases are synthesized by reaction of isatin with substituted anilines in the presence of acetic acid under microwave heating. Then the condensation of Schiff bases with different secondary amines in the presence of formaldehyde produces Mannich bases. The newly synthesized Mannich bases were characterized by means of spectral data and then evaluated for anthelmintic activity against Pheretima posthuma (Indian earthworm and compared with standard albendazole. The compounds were evaluated at the concentrations of 10, 20, and 50 mg/mL. The effect of the standard drug albendazole at 10 mg/mL was also evaluated. The results of the present study indicate that some of the test compounds significantly demonstrated paralysis and also caused death of worms in a dose-dependent manner.

  13. Correlation between the predicted and the observed biological activity of the symmetric and nonsymmetric cyclic urea derivatives used as HIV-1 protease inhibitors. A 3D-QSAR-CoMFA method for new antiviral drug design.

    Science.gov (United States)

    Avram, Speranta; Svab, I; Bologa, C; Flonta, Maria-Luiza

    2003-01-01

    The predicted inhibition constant (Ki) and the predicted inhibitor concentration (IC90) of the HIV-1 protease (HIV- 1 PR) inhibitors: symmetric and nonsymmetric - benzyl, ketone, oxime, pyrazole, imidazole, and triazole cyclic urea derivatives, were obtained by the 3D-CoMFA (Comparative Molecular Field Analysis) method. The CoMFA statistical parameters: cross-validate correlation coefficient (q2), higher than 0.5, and the fitted correlation coefficient (r2), higher than 0.90 validated the predicted biological activities. The best predictions were found for the trifluoromethyl ketoxime derivative (log 1/Ki predict = 8.42), the m-pyridineCH2 pyrazole derivative (log 1/Ki predict = 9.77) and the 1,2,3 triazole derivative (log 1/Ki predict = 7.03). We attempted to design a new potent HIV-1 protease inhibitor by addition of o-benzyl to the (p-HOPhCH2) pyrazole 12f derivative inhibitor. A favorable steric area surrounded the o-benzyl, suggesting a possible new potent HIV-1 protease inhibitor.

  14. Synthesis, characterization, molecular modeling and biological activity of metal complexes derived from (E)-N'-(furan-2-ylmethylene)morpholine-4-carbothiohydrazide

    Science.gov (United States)

    El-Samanody, El-Sayed A.; Emam, Sanaa M.; Emara, Esam M.

    2017-10-01

    A new series of some biologically active Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) complexes was synthesized from the novel thiosemicarbazone ligand; (E)-N'-(furan-2-ylmethylene)morpholine-4-carbothiohydrazide (HL). Elemental, spectral, thermal analyses, magnetic susceptibility and molar conductivity measurements were used to elucidate the structure of separated compounds. The data prove that the ligand reacts with all metal ions in a neutral thione form. The electrolytic tetra-coordinate Cu(II); Zn(II) complexes (5, 6; 10) bind through the thione sulfur, furfural oxygen and azomethine nitrogen atoms of the ligand (NSO type) to construct fused five membered rings. However, the rest non-electrolyte octahedral complexes chelate via the furfural oxygen and azomethine nitrogen atoms of the ligand (NO type). Molecular modeling was conducted for the ligand and two representative complexes (1, 5) in order to substantiate their chemical structures. Thermal analyses are compatible with molecular modeling studies to support the proposed thermal decomposition pathways of metal complexes which start with the rupture of the long and weak N-NH bond. The thermal stability of metal complexes varies according to the number of solvents of crystallization, ionic radii and steric effect of anions. The ESR spectra of Cu(II) complexes are compatible with a primarily (dx2-y2)1 ground state with axial symmetry. The ligand and its Co(II); Cu(II); Cd(II) complexes (1; 5, 8; 11) along with their mixtures with metaldehyde were screened in vitro for their molluscicidal activity against Eobania vermiculata. Combination with metaldehyde enhances the toxicity effect of the tested compounds through reducing the period required for mortality and increasing the percentage of mortality after 24 h of treatments. The tested compounds gathered with metaldehyde are strongly affecting on the activity of ACP and ALP enzymes and TP content which are very important factors in the mucous secretion of Eobania

  15. 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

    Science.gov (United States)

    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.

  16. N9-Substituted N(6)-[(3-methylbut-2-en-1-yl)amino]purine derivatives and their biological activity in selected cytokinin bioassays

    Czech Academy of Sciences Publication Activity Database

    Mik, V.; Szüčová, Lucie; Spíchal, Lukáš; Plíhal, O.; Nisler, Jaroslav; Zahajská, L.; Doležal, Karel; Strnad, Miroslav

    2011-01-01

    Roč. 19, č. 23 (2011), s. 7244-7251 ISSN 0968-0896 R&D Projects: GA MŠk ED0007/01/01; GA ČR GA522/09/1576 Keywords : N6-[(3-Methylbut-2-en-1-yl)amino]purine * Isopentenyladenine derivatives * N9-Substituted derivatives * Cytokinins * Cytokinin receptors Subject RIV: EF - Botanics Impact factor: 2.921, year: 2011

  17. Microwave-assisted synthesis and biological evaluation of novel uracil derivatives inhibiting human thymidine phosphorylase.

    Science.gov (United States)

    Corelli, Federico; Botta, Maurizio; Lossani, Andrea; Pasquini, Serena; Spadari, Silvio; Focher, Federico

    2004-12-01

    New 5-chloro-6-substituted-uracil derivatives have been prepared by microwave assisted-synthesis and tested in vitro as thymidine phosphorylase inhibitors. One of these compounds showed potent inhibitory activity, with an IC50 value in the submicromolar range. The biological activity of the new compounds is discussed in terms of structure-activity relationship.

  18. The Teratogenic Potencies of Valproic Acid Derivatives and Their Effects on Biological End-points are Related to Changes in Histone Deacetylase and Erk1/2 Activities

    DEFF Research Database (Denmark)

    Gotfryd, Kamil; Hansen, Maria; Kawa, Anna

    2011-01-01

    Valproic acid (VPA) is a known teratogen. In the present study, the effects of VPA and seven VPA derivatives with different teratogenic potencies (isobutyl-, 5-methyl-, ethyl-, propyl-, butyl-, pentyl- and hexyl-4-yn-VPA) were investigated in L929 cells in vitro. Evaluated end-points included cha...

  19. Zinc(II) complexes with potent cyclin-dependent kinase inhibitors derived from 6-benzylaminopurine: synthesis, characterization, X-ray structures and biological activity

    Czech Academy of Sciences Publication Activity Database

    Trávníček, Zdeněk; Kryštof, Vladimír; Šipl, M.

    2006-01-01

    Roč. 100, č. 2 (2006), s. 214-225 ISSN 0162-0134 R&D Projects: GA ČR GA203/04/1168 Institutional research plan: CEZ:AV0Z50380511 Keywords : Zinc(II) complexes * 6-Benzylaminopurine derivatives * Bohemine * Olomoucine * X-ray structures Subject RIV: CA - Inorganic Chemistry Impact factor: 2.654, year: 2006

  20. Towards the rational design of novel drugs based on solubility, partitioning/distribution, biomimetic permeability and biological activity exemplified by 1,2,4-thiadiazole derivatives

    DEFF Research Database (Denmark)

    Volkova, T. V.; Terekhova, I. V.; Silyukov, O. I.

    2017-01-01

    Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-oct...

  1. Synthesis, characterization and biological activity of ring-substituted 6-benzylamino-9-tetrahydropyran-2-yl and 9-tetrahydrofuran-2-ylpurine derivatives

    Czech Academy of Sciences Publication Activity Database

    Szüčová, Lucie; Spíchal, Lukáš; Doležal, Karel; Zatloukal, Marek; Greplová, Jarmila; Galuszka, P.; Kryštof, Vladimír; Voller, Jiří; Popa, Igor; Massino, F.J.; Jorgensen, J.E.; Strnad, Miroslav

    2009-01-01

    Roč. 17, č. 5 (2009), s. 1938-1947 ISSN 0968-0896 R&D Projects: GA MŠk 1M06030; GA ČR GA522/09/1576; GA ČR(CZ) GA522/08/0920 Institutional research plan: CEZ:AV0Z50380511 Keywords : Cytokinins * Antisenescence * Receptor Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.822, year: 2009

  2. In vivo biology and toxicology of fullerenes and their derivatives

    DEFF Research Database (Denmark)

    Nielsen, Gunnar Damgård; Roursgaard, Martin; Jensen, Keld Alstrup

    2008-01-01

    half-life, whereas the most water-soluble derivatives are eliminated from the exposed animals within weeks. A long biological half-life raises concern about bioaccumulation and long-term effects. In general, the acute oral, dermal and airway toxicity is low. However, few relevant experimental studies...

  3. Synthesizing a Berberine Derivative and Evaluating Antimicrobial Activity to Reinforce with Students the Potential Significance of Small Chemical Structure Changes for Biological Systems

    Science.gov (United States)

    Rodrigues, Catarina A. B.; Neto, Iris; Rijo, Patricia; Afonso, Carlos A. M.

    2018-01-01

    The convenient synthesis of dihydroberberine by the reduction of berberine is described as an experiment for an upper-division undergraduate organic chemistry laboratory course. Students obtained up to 74% yield of the desired pure product without the use of chromatographic techniques. The antimicrobial activities of both compounds against…

  4. Chalcone derivatives as potential antifungal agents: Synthesis, and antifungal activity

    Directory of Open Access Journals (Sweden)

    Deepa Gupta

    2015-01-01

    Full Text Available Much research has been carried out with the aim to discover the therapeutic values of chalcone derivatives. Chalcones possess wide range of pharmacological activity such as antibacterial, antimalarial, antiprotozoal, antitubercular, anticancer, and antifungal agents etc. The presence of reactive α,β-unsaturated keto group in chalcones is found to be responsible for their biological activity. The rapid developments of resistance to antifungal agents, led to design, and synthesize the new antifungal agents. The derivatives of chalcones were prepared using Claisen-Schmidt condensation scheme with appropriate tetralone and aldehyde derivatives. Ten derivatives were synthesized and were biologically screened for antifungal activity. The newly synthesized derivatives of chalcone showed antifungal activity against fungal species, Microsporum gypseum. The results so obtained were superior or comparable to ketoconazole. It was observed that none of the compounds tested showed positive results for fungi Candida albicans nor against fungi Aspergillus niger. Chalcone derivatives showed inhibitory effect against M. gypseum species of fungus. It was found that among the chalcone derivatives so synthesized, two of them, that is, 4-chloro derivative, and unsubstituted derivative of chalcone showed antifungal activity superior to ketoconazole. Thus, these can be the potential new molecule as antifungal agent.

  5. Design and optimization of N-acylhydrazone pyrimidine derivatives as E. coli PDHc E1 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study.

    Science.gov (United States)

    He, Haifeng; Xia, Hongying; Xia, Qin; Ren, Yanliang; He, Hongwu

    2017-10-15

    By targeting the thiamin diphosphate (ThDP) binding site of Escherichia coli (E. coli) pyruvate dehydrogenase multienzyme complex E1 (PDHc E1), a series of novel 'open-chain' classes of ThDP analogs A, B, and C with N-acylhydrazone moieties was designed and synthesized to explore their activities against E. coli PHDc E1 in vitro and their inhibitory activity against microbial diseases were further evaluated in vivo. As a result, A1-23 exhibited moderate to potent inhibitory activities against E. coli PDHc E1 (IC 50 =0.15-23.55μM). The potent inhibitors A13, A14, A15, C2, had strong inhibitory activities with IC 50 values of 0.60, 0.15, 0.39 and 0.34μM against E. coli PDHc E1 and with good enzyme-selective inhibition between microorganisms and mammals. Especially, the most powerful inhibitor A14 could 99.37% control Xanthimonas oryzae pv. Oryzae. Furthermore, the binding features of compound A14 within E. coli PDHc E1 were investigated to provide useful insights for the further construction of new inhibitor by molecular docking, site-directed mutagenesis, and enzymatic assays. The results indicated that A14 had most powerful inhibition against E. coli PDHc E1 due to the establishment of stronger interaction with Glu571, Met194, Glu522, Leu264 and Phe602 at active site of E.coli PDHc E1. It could be used as a lead compound for further optimization, and may have potential as a new microbicide. Copyright © 2017 Elsevier Ltd. All rights reserved.

  6. Synthesis and biological evaluation of chalcone derivatives (mini review).

    Science.gov (United States)

    Bukhari, Syed Nasir Abbas; Jasamai, Malina; Jantan, Ibrahim

    2012-11-01

    Chalcones are the principal precursors for the biosynthesis of flavonoids and isoflavonoids. A three carbon α, β-unsaturated carbonyl system constitutes chalcones. Chalcones are the condensation products of aromatic aldehyde with acetophenones in attendance of catalyst. They go through an assortment of chemical reactions and are found advantageous in synthesis of pyrazoline, isoxazole and a variety of heterocyclic compounds. In synthesizing a range of therapeutic compounds, chalcones impart key role. They have showed worth mentioning therapeutic efficacy for the treatment of various diseases. Chalcone based derivatives have gained heed since they own simple structures, and diverse pharmacological actions. A lot of methods and schemes have been reported for the synthesis of these compounds. Amongst all, Aldol condensation and Claisen-Schmidt condensation still grasp high up position. Other distinguished techniques include Suzuki reaction, Witting reaction, Friedel-Crafts acylation with cinnamoyl chloride, Photo-Fries rearrangement of phenyl cinnamates etc. These inventive techniques utilize various catalysts and reagents including SOCl(2) natural phosphate, lithium nitrate, amino grafted zeolites, zinc oxide, water, Na(2)CO(3), PEG400, silicasulfuric acid, ZrCl(4) and ionic liquid etc. The development of better techniques for the synthesis of α, β- unsaturated carbonyl compounds is still in high demand. In brief, we have explained the methods and catalysts used in the synthesis of chalcones along with their biological activities in a review form to provide information for the development of new-fangled processes targeting better yield, less reaction time and least side effects with utmost pharmacological properties.

  7. Synthesis and antibacterial activity of sulfonamide derivatives at C-8 ...

    Indian Academy of Sciences (India)

    Synthesis and antibacterial activity of some novel biologically active sulfonamide derivatives at C-8 alkyl chain of anacardic acid (7a-7l), prepared from commercially available anacardic acid mixture (1a-d). These compounds were tested for Gram positive and Gram negative bacterial cultures; most of the compounds ...

  8. Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

    Directory of Open Access Journals (Sweden)

    Khalid Karrouchi

    2018-01-01

    Full Text Available Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

  9. Synthesis, Characterization, and Antimicrobial and Antispermatogenic Activity of Bismuth(III and Arsenic(III Derivatives of Biologically Potent Nitrogen and Sulfur Donor Ligands

    Directory of Open Access Journals (Sweden)

    Latika Dawara

    2012-01-01

    Full Text Available A series of Bi(III and As(III complexes with two N∩S donor ligands, 1-(4-chloro-2-oxo-2H-chromen-3-yl-methylene-thiosemicarbazide (L1H and N′-[1-(2-oxo-2H-chrome-3yl-ethylidene]-hydrazinecarbodithionic acid benzyl ester (L2H have been synthesized by the reaction of BiCl3 and Ph3As with ligands in 1 : 1 and 1 : 2 molar ratios. All the synthesized compounds were characterized by elemental analyses, melting point determinations, and a combination of electronic, IR, 1H NMR, 13C NMR spectroscopic techniques, and X-ray diffraction for structure elucidation. In order to evaluate the effect of metal ions upon chelation, both the ligands and their complexes have been screened for their antimicrobial activity against the various pathogenic bacterial and fungal strains. The metal complexes have shown to be more antimicrobial against the microbial species as compared to free ligands. Both the ligands and their corresponding metal complexes have been tested for their antifertility activity in male albino rats. The marked reduction in sperm motility and density resulted in infertility. Significant alterations were found in biochemical parameters of reproductive organs in treated animals as compared to control group. It is concluded that all these effects may finally impair the fertility of male rats.

  10. Specific binding of an immunoreactive and biologically active 125I-labeled substance P derivative to mouse mesencephalic cells in primary culture

    International Nuclear Information System (INIS)

    Beaujouan, J.C.; Torrens, Y.; Herbet, A.; Daguet, M.C.; Glowinski, J.; Prochiantz, A.

    1982-01-01

    Binding characteristics of 125 I-labeled Bolton-Hunter substance P ([ 125 I]BHSP), a radioactive analogue of substance P, were studied with mesencephalic primary cultures prepared from embryonic mouse brain. Nonspecific binding represented no more than 20% of the total binding observed on the cells. In contrast, significant specific binding--saturable, reversible, and temperature-dependent--was demonstrated. Scatchard analysis of concentration-dependent binding saturation indicates a single population of noninteracting sites with a high affinity (Kd . 169 pM). Substance P and different substance P analogues were tested for their competitive potencies with regard to [ 125 I]BHSP binding. BHSP itself, substance P, (Tyr8)-substance P, and (nor-Leu11)-substance P strongly inhibited the binding. Good inhibition was also obtained with physalaemin and eledoisin, two peptides structurally related to substance P. When substance P C-terminal fragments were tested for their ability to compete with [ 125 I]BHSP binding, a good relationship was found between competitive activity and peptide length. Regional distribution of [ 125 I]BHSP binding sites was found using primary cultures obtained from different regions of embryonic mouse brain. Mesencephalic, hypothalamic, and striatal cultures had the highest [ 125 I]BHSP binding capacities, whereas cortical, hippocampal, and cerebellar cells shared only little binding activity. Finally, when mesencephalic cells were grown under conditions impairing glial development, [ 125 I]BHSP binding was not affected, demonstrating that binding sites are located on neuronal cells

  11. Biologically Active Metabolites Synthesized by Microalgae

    Directory of Open Access Journals (Sweden)

    Michele Greque de Morais

    2015-01-01

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

  12. Biologically Active Metabolites Synthesized by Microalgae.

    Science.gov (United States)

    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.

  13. Biologically Active Metabolites Synthesized by Microalgae

    Science.gov (United States)

    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

  14. The biological activities of (1,3)-(1,6)-{beta}-d-glucan and porous electrospun PLGA membranes containing {beta}-glucan in human dermal fibroblasts and adipose tissue-derived stem cells

    Energy Technology Data Exchange (ETDEWEB)

    Woo, Yeon I; Park, Bong Joo; Kim, Hye-Lee; Lee, Mi Hee; Kim, Jungsung; Park, Jong-Chul [Department of Medical Engineering, Yonsei University College of Medicine, 134 Shinchon-dong, Seodaemun-gu, Seoul 120-752 (Korea, Republic of); Yang, Young-Il [Department of Pathology, School of Medicine, Paik Institute for Clinical Research, Inje University, 633-165 Gae-dong, Busan-jin-gu, Busan 614-735 (Korea, Republic of); Kim, Jung Koo [Department of Biomedical Engineering, College of Biomedical Science and Engineering, Inje University, Kimhae 621-749 (Korea, Republic of); Tsubaki, Kazufumi [R and D division, Asahi Denka Co. Ltd, 7-2-35 Higashi-ogu, Arakawa-ku, Tokyo 116-8554 (Japan); Han, Dong-Wook, E-mail: parkjc@yuhs.a [Department of Nanomedical Engineering, College of Nanoscience and Nanotechnology, Pusan National University, geumjeong-gu, Busan 609-735 (Korea, Republic of)

    2010-08-01

    In this study, we investigated the possible roles of (1,3)-(1,6)-{beta}-d-glucan ({beta}-glucan) and porous electrospun poly-lactide-co-glycolide (PLGA) membranes containing {beta}-glucan for skin wound healing, especially their effect on adult human dermal fibroblast (aHDF) and adipose tissue-derived stem cell (ADSC) activation, proliferation, migration, collagen gel contraction and biological safety tests of the prepared membrane. This study demonstrated that {beta}-glucan and porous PLGA membranes containing {beta}-glucan have enhanced the cellular responses, proliferation and migration, of aHDFs and ADSCs and the result of a collagen gel contraction assay also revealed that collagen gels contract strongly after 4 h post-gelation incubation with {beta}-glucan. Furthermore, we confirmed that porous PLGA membranes containing {beta}-glucan are biologically safe for wound healing study. These results indicate that the porous PLGA membranes containing {beta}-glucan interacted favorably with the membrane and the topical administration of {beta}-glucan was useful in promoting wound healing. Therefore, our study suggests that {beta}-glucan and porous PLGA membranes containing {beta}-glucan may be useful as a material for enhancing wound healing.

  15. Design, synthesis, spectral characterization, DNA interaction and biological activity studies of copper(II), cobalt(II) and nickel(II) complexes of 6-amino benzothiazole derivatives

    Science.gov (United States)

    Daravath, Sreenu; Kumar, Marri Pradeep; Rambabu, Aveli; Vamsikrishna, Narendrula; Ganji, Nirmala; Shivaraj

    2017-09-01

    Two novel Schiff bases, L1 = (2-benzo[d]thiazol-6-ylimino)methyl)-4,6-dichlorophenol), L2 = (1-benzo[d]thiazol-6-ylimino)methyl)-6-bromo-4-chlorophenol) and their bivalent transition metal complexes [M(L1)2] and [M(L2)2], where M = Cu(II), Co(II) and Ni(II) were synthesized and characterized by elemental analysis, NMR, IR, UV-visible, mass, magnetic moments, ESR, TGA, SEM, EDX and powder XRD. Based on the experimental data a square planar geometry around the metal ion is assigned to all the complexes (1a-2c). The interaction of synthesized metal complexes with calf thymus DNA was explored using UV-visible absorption spectra, fluorescence and viscosity measurements. The experimental evidence indicated that all the metal complexes strongly bound to CT-DNA through an intercalation mode. DNA cleavage experiments of metal(II) complexes with supercoiled pBR322 DNA have also been explored by gel electrophoresis in the presence of H2O2 as well as UV light, and it is found that the Cu(II) complexes cleaved DNA more effectively compared to Co(II), Ni(II) complexes. In addition, the ligands and their metal complexes were screened for antimicrobial activity and it is found that all the metal complexes were more potent than free ligands.

  16. Synthesis and antimicrobial activity of amphiphilic carbohydrate derivatives

    International Nuclear Information System (INIS)

    Reis, Roberta C.N.; Oda, Simone C.; Almeida, Mauro V. de; Le Hyaric, Mireille; Barbosa, Nadia R.; Trevizani, Rafael; Santos, Priscila L.C.

    2008-01-01

    N-monoalkylated diamines were synthesised and treated with D-ribonolactone or D-gluconolactone. The resulting aldonamides were evaluated for their antimicrobial activity against S. aureus, E. coli, M. tuberculosis and C. albicans. Two hydrazides were also prepared from ribonohydrazide and their biological activity was compared to their amide analogues. All the ribono-derivatives displayed moderated antitubercular activity, and some of them were also active against S. aureus. (author)

  17. Synthesis and Biological Evaluation of Resveratrol Derivatives as Melanogenesis Inhibitors

    Directory of Open Access Journals (Sweden)

    Qing Liu

    2015-09-01

    Full Text Available Resveratrol (1, a naturally occurring stilbene compound, has been suggested as a potential whitening agent with strong inhibitory activity on melanin synthesis. However, the use of resveratrol in cosmetics has been limited due to its chemical instability and poor bioavailability. Therefore, resveratrol derivatives were prepared to improve bioavailability and anti-melanogenesis activity. Nine resveratrol derivatives including five alkyl ether derivatives with C2H5, C4H9, C5H11, C6H13, and C8H17 (2a–2e and four ester derivatives with CH3, CH=C(CH32, CH(C2H5C4H9, C7H15 (3a–3d were newly synthesized and their effect on melanin synthesis were assessed. All the synthetic derivatives efficiently reduced the melanin content in α-MSH stimulated B16F10 melanoma cells. Further investigation showed that the inhibitory effect of 2a on melanin synthesis was achieved not by the inhibition of tyrosinase activity but by the inhibition of melanogenic enzyme expressions such as tyrosinase and tyrosinase-related protein (TRP-1. Our synthetic resveratrol derivatives have more lipophilic properties than resveratrol by the addition of alkyl or acyl chains to free hydroxyl moiety of resveratrol; thus, they are expected to show better bioavailability in skin application. Therefore, we suggest that our synthetic resveratrol derivatives might be promising candidates for better practical application to skin-whitening cosmetics.

  18. Ethnobotanical and biological activities of Leptadenia pyrotechnica ...

    African Journals Online (AJOL)

    Conclusion: This review includes the substance of different ethnobotanical uses, phytochemistry and exclusive capability of this plant in the field of anti-microbial and human disease activities. Key words: Leptadenia pyrotechnica, Biological activities, Desert plant, Ethnobotanical, Phytochemical activity, phytochemistry.

  19. Biologically Active and Antimicrobial Peptides from Plants

    Directory of Open Access Journals (Sweden)

    Carlos E. Salas

    2015-01-01

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

  20. Natural Cinnamic Acids, Synthetic Derivatives and Hybrids with Antimicrobial Activity

    Directory of Open Access Journals (Sweden)

    Juan David Guzman

    2014-11-01

    Full Text Available Antimicrobial natural preparations involving cinnamon, storax and propolis have been long used topically for treating infections. Cinnamic acids and related molecules are partly responsible for the therapeutic effects observed in these preparations. Most of the cinnamic acids, their esters, amides, aldehydes and alcohols, show significant growth inhibition against one or several bacterial and fungal species. Of particular interest is the potent antitubercular activity observed for some of these cinnamic derivatives, which may be amenable as future drugs for treating tuberculosis. This review intends to summarize the literature data on the antimicrobial activity of the natural cinnamic acids and related derivatives. In addition, selected hybrids between cinnamic acids and biologically active scaffolds with antimicrobial activity were also included. A comprehensive literature search was performed collating the minimum inhibitory concentration (MIC of each cinnamic acid or derivative against the reported microorganisms. The MIC data allows the relative comparison between series of molecules and the derivation of structure-activity relationships.

  1. Biologically Active Secondary Metabolites from the Fungi.

    Science.gov (United States)

    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

  2. Synthesis and Biological Activities of Some Benzimidazoles ...

    African Journals Online (AJOL)

    The chemical structures of these compounds were elucidated using NMR and elemental analysis. The biological activity of these compounds as fungicides was tested against three commercially known fungicides (C. albicans, patient isolate C. glabrata and C. krusei).The biological activity of two compounds was found to be ...

  3. Triazoles: a valuable insight into recent developments and biological activities.

    Science.gov (United States)

    Sahu, Jagdish K; Ganguly, Swastika; Kaushik, Atul

    2013-09-01

    In recent years, heterocyclic compounds, analogs, and derivatives have attracted strong interest due to their useful biological and pharmacological properties. The small and simple triazole nucleus is present in compounds aimed at evaluating new entities that possess anti-microbial, anti-tumor, antitubercular, anti-convulsant, anti-depressant, antimalarial, and anti-inflammatory activities. Triazoles display a broad range of biological activities and are found in many potent, biologically active compounds, such as trazodone (antidepressant drug), rizatriptan (antimigrane drug), hexaconazole (antifungal drug) and alprazolam (hyptonic, sedative and tranquilizer drug). So far, modifications of the triazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized triazoles possessing important biological activities. Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

  4. Molluscicidal and trypanocidal activities of lapachol derivatives.

    Science.gov (United States)

    Santos, A F; Ferraz, P A; de Abreu, F C; Chiari, E; Goulart, M O; Sant'Ana, A E

    2001-02-01

    The activity of the potassium salt of lapachol against the snail Biomphalaria glabrata and its egg masses was tested. The obtained IC50 values (2.70 ppm and 1.43 ppm, respectively) are indicative of a strong activity. Lapachol derivatives were also assayed against infective trypomastigote blood forms of T. cruzi and the triacetoxy derivative of reduced lapachol showed relevant trypanocidal activity, killing 95.7% of the parasites at the concentration of 42 microg/mL.

  5. Synthesis and Biological Activity of Some 3,4-Dihydro-4-(4-substituted aryl-6-(naptho[2,1-b]furan-2-yl pyrimidine-2(1H-one Derivatives

    Directory of Open Access Journals (Sweden)

    Sanjeevan S. Gaikwad

    2012-01-01

    Full Text Available A series of new oxopyrimidine were prepared by cyclocondensation route with various substituted chalcones in presence of alcoholic solution of potassium hydroxide at reflux temperature. The synthesized oxopyrimidine derivatives were characterized by means of their IR, 1H NMR, mass spectral data and elemental analysis. The synthesized oxopyrimidines derivatives were evaluated for antibacterial and antifungal activities, some of them were found to possess significant activity.

  6. Synthesis and biological evaluation of 2-substituted benzimidazole derivatives

    Directory of Open Access Journals (Sweden)

    Gurusamy Mariappan

    2015-09-01

    Full Text Available A novel series of 2-substituted benzimidazole derivatives (3a–3j were synthesized by the reaction of 2-chloro methyl benzimidazole with substituted primary aromatic amines. All the compounds were characterized by UV, IR, 1H NMR, mass spectral data and CHN elemental analysis. The synthesized derivatives were screened for analgesic and anti-inflammatory activities. All the compounds showed significant effect at 100 mg/kg p.o. and the experimental data are statistically significant at p < 0.01 level.

  7. SYNTHESIS OF BIOLOGICALLY-ACTIVE 2-BENZOYL PACLITAXEL ANALOGS

    DEFF Research Database (Denmark)

    GEORG, GI; ALI, SM; BOGE, TC

    1995-01-01

    The influence of aromatic substitution at the 2-benzoyl moiety of paclitaxel on biological activity was investigated, following the Topliss Operational Scheme. Twelve paclitaxel derivatives were synthesized and evaluated in a microtubule assembly assay and for cytotoxicity against B16 melanoma ce...

  8. Synthesis and Biological Evaluation of Some Novel Dithiocarbamate Derivatives

    Directory of Open Access Journals (Sweden)

    Begüm Nurpelin Sağlık

    2014-01-01

    Full Text Available 18 novel dithiocarbamate derivatives were synthesized in order to investigate their inhibitory potency on acetylcholinesterase enzyme and antimicrobial activity. Structures of the synthesized compounds were elucidated by spectral data and elemental analyses. The synthesized compounds showed low enzyme inhibitory activity. However, they displayed good antimicrobial activity profile. Antibacterial activity of compounds 4a, 4e, and 4p (MIC = 25 μg/mL was equal to that of chloramphenicol against Klebsiella pneumoniae (ATCC 700603 and Escherichia coli (ATCC 35218. Most of the compounds exhibited notable antifungal activity against Candida albicans (ATCC 10231, Candida glabrata (ATCC 90030, Candida krusei (ATCC 6258, and Candida parapsilosis (ATCC 7330. Moreover, compound 4a, which carries piperidin-1-yl substituent and dimethylthiocarbamoyl side chain as variable group, showed twofold better anticandidal effect against all Candida species than reference drug ketoconazole.

  9. Potent 5-nitrofuran derivatives inhibitors of Trypanosoma cruzi growth: Electrochemical, spectroscopic and biological studies

    Science.gov (United States)

    Maria Aravena, C.; Claudio Olea, A.; Cerecetto, Hugo; González, Mercedes; Maya, Juan Diego; Rodríguez-Becerra, Jorge

    2011-07-01

    Cyclic voltammetry and electron spin resonance techniques were used in the investigation of several potential antiprotozoal containing thiosemicarbazone and carbamate nitrofurans. In the electrochemical behaviour, a self-protonation process involving the nitro group was observed. The reactivity of the nitro anion radical for these derivatives with glutathione, a biological relevant thiol, was also studied in means of cyclic voltammetry. These studies demonstrated that glutathione could react with radical species from 5-nitrofuryl system. Furthermore, from the voltammetric results, some parameters of biological significance as E71 (indicative of the biological nitro anion radical formation), and K (thermodynamic indicator the of oxygen redox cycling) have been calculated. We also evaluated the stability of the nitro anion radical in terms of the dimerization constant ( kd). The nitrofuran-free radicals from cyclic voltammetry were characterized by electron spin resonance. A clear dependence between both the thiosemicarbazone or carbamate substructure and the length of the linker, furyl- or furylpropenyl-spacer, and the delocalization of the unpaired electron was observed. Through of biological assays we obtained important parameters that account for the selective anti-trypanosomal activity of these derivatives. The trypomastigote viability study showed that all derivatives are as active as in the epimastigote form of the parasite in a doses dependent manner.

  10. The double radio-isotope derivative techniques for the assay of drugs in biological material

    International Nuclear Information System (INIS)

    Riess, W.

    1977-01-01

    The neuroleptic drug opipramol and its deshydroxyethyl metabolite can be determined simultaneously in the same biological sample. Known amounts of 14 C-labelled opipramol and 14 C-labelled metabolite are added to the sample to serve as internal standards. After suitable extraction, both compounds are acetylated by 3 H-labelled acetic anhydride. Together with μg-amounts of carrier compounds, the O-acetyl derivative of opipramol and the N-acetyl derivative of the metabolite are purified and separated by two-dimensional thin-layer chromatography. Each of the derivatives is isolated and counted for 14 C- and 3 H-activity. The 14 C-activities recovered serve to determine the overall yield of the opipramol and metabolite, and to convert the measured 3 H-activity to 100% theoretical yield. From analyses of standard samples, the specific 3 H-activities of the acetyl derivatives were calculated and these values were used to convert the measured 3 H-activites from biological samples to concentrations of original opipramol and metabolite. For both compounds the standard deviations of blank samples were +- 1 ng/ml. For concentrations up to 100 ng/ml the standard deviation was +- 3 ng/ml

  11. Biological activity of liposomal vanillin.

    Science.gov (United States)

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

    2013-06-01

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

  12. INVESTIGATION OF ANTIFUNGAL ACTIVITY OF QUINOLINIUM DERIVATIVES

    Directory of Open Access Journals (Sweden)

    G. A. Alexandrova

    2013-01-01

    Full Text Available Abstract. Antifungal activity (Candida albicans, Candida krusei of some substituted quinolinium derivatives has been investigated. It was established that the most perspective compound for detail investigation of antifungal activity by labeled biomarkers method was N-phenylbenzoquinaldinium tetrafluoroborate.

  13. Synthesis, characterization and biological behavior of some Schiff's and Mannich base derivatives of Lamotrigine

    Directory of Open Access Journals (Sweden)

    A.A. Kulkarni

    2017-02-01

    Full Text Available A series of various Schiff's and Mannich base derivatives (N1–2 & ND1–6 of Lamotrigine with isatin and substituted isatin were synthesized to get more potent anticonvulsant agents. The starting material for the synthesis of various new Schiff's and Mannich base derivatives was isatin (1H-indole- 2, 3-dione which in turn was prepared from substituted isonitrosoacetanilide using aniline. Lamotrigine reacts with isatin & substituted isatin gave Schiff's bases (N1–2 which on reaction with various secondary amines (dimethylamine, diethylamine, morpholine produced Mannich bases (ND1–6. The structures of newly synthesized compounds were characterized by using TLC, UV, FT-IR, 1HNMR and studied for their anticonvulsant activity. Anticonvulsant activity of all the derivatives was evaluated by MES method using phenobarbitone sodium & Lamotrigine as standard drugs and % reduction of time spent by animals in extension, flexion, clonus, and stupor phase were noted. Compounds ND-4 and ND-6 showed significant anticonvulsant activity when compared with that of standard drugs. The remaining all compounds show moderate activity. Biological activity data of the synthesized derivatives revealed that, the synthesized derivatives are good anticonvulsant agents as compared to Lamotrigine.

  14. Synthesis, characterization and biological evaluation of some newer carbazole derivatives

    Directory of Open Access Journals (Sweden)

    Sharma Divyanshu

    2014-01-01

    Full Text Available A series of novel 5-((9H-carbazol-9-ylmethyl-N-((substituted phenyl(piperazin-1-ylmethyl-1,3,4-oxadiazol-2-amine (4a-4o derivatives was synthesized by starting with carbazole which on reaction with ethyl choloroacetate yielded ethyl 2-(9H-carbazole-9-ylacetate (1, compound (1 on reaction with semicarbazide followed by cyclisation with sulphuric acid gave 5-((9H-carbazole-9-yl-1,3,4-oxadiazol-2-amine (3 which through Mannich reaction with piperazine and a variety of aromatic aldehydes in the presence of acetic acid yielded the titled compounds (4a-4o. The structures of compounds were characterized by UV, FT-IR, 1H-NMR, MS spectral studies and elemental analysis. All the derivatives were evaluated for their antibacterial, antifungal and anticancer activities. Among the tested compounds 4a, 4d, 4e and 4n exhibited significant antibacterial and antifungal activity while the compounds 4a, 4d, 4k and 4n were found to be active on Human Breast Cancer Cell Line i.e. MCF7.

  15. Elsholtzia: phytochemistry and biological activities

    Directory of Open Access Journals (Sweden)

    Guo Zhiqin

    2012-12-01

    Full Text Available Abstract 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.

  16. Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives

    Directory of Open Access Journals (Sweden)

    Anwei Ding

    2013-08-01

    Full Text Available A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC50 values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC50 values being 96.4, 71.0 and 75.4 μM, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin.

  17. Synthesis and biological activities of substituted N ...

    African Journals Online (AJOL)

    use

    2011-12-07

    Dec 7, 2011 ... The present study describes the synthesis, antioxidant and antibacterial activities of substituted N'- benzoylhydrazone derivatives, to ... addition, the dramatically rising prevalence of multidrug- resistant microbial infections has ...... extract of Chinese green tea (Camellia sinensis) on Listeria monocytogenes.

  18. Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

    Directory of Open Access Journals (Sweden)

    David Collu

    2009-12-01

    Full Text Available A series of twenty arylpiperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione have been prepared. These derivatives were tested in vitro with the aim of identifying novel lead compounds active against emergent and re-emergent human and cattle infectious diseases (AIDS, hepatitis B and C, tuberculosis, bovine viral diarrhea. In particular, these compounds were evaluated in vitro against representatives of different virus classes, such as a HIV-1 (Retrovirus, a HBV (Hepadnavirus and the single-stranded RNA+ viruses Yellow fever virus (YFV and Bovine viral diarrhea virus (BVDV, both belonging to the Flaviridae. Compounds 2c, 2g and 3d showed a modest activity against CVB-2. The molecular structures of the starting imide 1 and one of propyl-piperazine derivatives, 3b, have been determined by an X-ray crystallography study.

  19. Atividade biológica do lapachol e de alguns derivados sobre o desenvolvimento fúngico e em germinação de sementes Biological activity of lapachol and some derivatives as antifungal and in seed germination

    Directory of Open Access Journals (Sweden)

    Marco Andre Alves de Souza

    2008-01-01

    Full Text Available The natural quinones lapachol, α-lapachone and β-lapachone, and the synthetic derivative β-lapachone-3-sulfonic-acid were assayed for inhibition of fungal growth (Fusarium oxysporum and germination of lettuce seeds (Lactuca sativa L.. β-Lapachone has the strongest activity as a germination inhibitor and lapachol shows no effect. β-Lapachone, followed by lapachol, are the most active in reducing fungal growth.

  20. Atividade biológica do lapachol e de alguns derivados sobre o desenvolvimento fúngico e em germinação de sementes Biological activity of lapachol and some derivatives as antifungal and in seed germination

    OpenAIRE

    Marco Andre Alves de Souza; Andrea Rosane da Silva; Marcio Alcântara Ferreira; Marcela Jacques de Lemos; Rafael Gonçalves Ramos; Aurélio Baird Buarque Ferreira; Sonia Regina de Souza

    2008-01-01

    The natural quinones lapachol, α-lapachone and β-lapachone, and the synthetic derivative β-lapachone-3-sulfonic-acid were assayed for inhibition of fungal growth (Fusarium oxysporum) and germination of lettuce seeds (Lactuca sativa L.). β-Lapachone has the strongest activity as a germination inhibitor and lapachol shows no effect. β-Lapachone, followed by lapachol, are the most active in reducing fungal growth.

  1. 5-Nitroimidazole Derivatives and their Antimicrobial Activity

    International Nuclear Information System (INIS)

    Khan, K.M.; Salar, U.; Yousuf, S.; Naz, F.

    2016-01-01

    5-Nitroimidazole derivatives 2-8 were synthesized from secnidazole. The syntheses were accomplished in two steps which start from the oxidation of secnidazole to the secnidazolone 1. Secnidazolone 1 was converted into its hydrazone derivative 2-8 by treating with different substituted acid hydrazide. Compounds 2-8 were evaluated for their antimicrobial activity against Gram-positive and Gram-negative bacteria, compounds 3 and 4 showed the significant activity against Staphylococcus epidermidis, however, compound 2 showed good inhibitions against Corynebacterium diphtheria when compared with the standard. Compound 3 showed good inhibitory potential against tested Gram-negative bacterial strains i.e. Enterobacter aerogene, Escherichia coli, Salmonella typhi, Salmonella paratyphi A, Shigella flexeneri and Vibrio choleriae. All synthetic derivatives were also tested against eight fungal stains, however, they were weekly active against Aspergillus flavus and Candida albican. The synthesized compounds were characterized by different spectroscopy techniques. (author)

  2. Marine Biology Activities. Ocean Related Curriculum Activities.

    Science.gov (United States)

    Pauls, John

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

  3. Genus Pouteria: chemistry and biological activity

    Directory of Open Access Journals (Sweden)

    Cíntia A. M. Silva

    Full Text Available The genus Pouteria belongs to the family Sapotaceae and can be widely found around the World. These plants have been used as building material, as food, because the eatable fruits, as well as remedies in folk medicine. Some biological activities have been reported to species of this genus such as antioxidant, anti-inflammatory, antibacterial and antifungal. However, the real potential of this genus as source of new drugs or phytomedicines remains unknown. Therefore, a review of the so far known chemical composition and biological activities of this genus is presented to stimulate new studies about the species already reported moreover that species have no reference about chemistry or biological activities could be found until now.

  4. Marine Sponge Lectins: Actual Status on Properties and Biological Activities

    Directory of Open Access Journals (Sweden)

    Sandro Mascena Gomes Filho

    2014-12-01

    Full Text Available Marine sponges are primitive metazoans that produce a wide variety of molecules that protect them against predators. In studies that search for bioactive molecules, these marine invertebrates stand out as promising sources of new biologically-active molecules, many of which are still unknown or little studied; thus being an unexplored biotechnological resource of high added value. Among these molecules, lectins are proteins that reversibly bind to carbohydrates without modifying them. In this review, various structural features and biological activities of lectins derived from marine sponges so far described in the scientific literature are discussed. From the results found in the literature, it could be concluded that lectins derived from marine sponges are structurally diverse proteins with great potential for application in the production of biopharmaceuticals, especially as antibacterial and antitumor agents.

  5. Biological roles and potential applications of immune cell-derived extracellular vesicles.

    Science.gov (United States)

    Wen, Chuan; Seeger, Robert C; Fabbri, Muller; Wang, Larry; Wayne, Alan S; Jong, Ambrose Y

    2017-01-01

    Extracellular vesicles (EVs) deliver bioactive macromolecules (i.e. proteins, lipids and nucleic acids) for intercellular communication in multicellular organisms. EVs are secreted by all cell types including immune cells. Immune cell-derived EVs modulate diverse aspects of the immune system to either enhance or suppress immune activities. The extensive effects of immune cell-derived EVs have become the focus of great interest for various nano-biomedical applications, ranging from the medical use of nanoplatform-based diagnostic agents to the development of therapeutic interventions as well as vaccine applications, and thus may be ideal for 'immune-theranostic'. Here, we review the latest advances concerning the biological roles of immune cell-derived EVs in innate and acquired immunity. The intercellular communication amongst immune cells through their EVs is highlighted, showing that all immune cell-derived EVs have their unique function(s) in immunity through intricate interaction(s). Natural-killer (NK) cell-derived EVs, for example, contain potent cytotoxic proteins and induce apoptosis to targeted cancer cells. On the other hand, cancer cell-derived EVs bearing NK ligands may evade immune surveillance and responses. Finally, we discuss possible medical uses for the immune cell-derived EVs as a tool for immune-theranostic: as diagnostic biomarkers, for use in therapeutic interventions and for vaccination.

  6. Biochemical activity of fullerenes and related derivatives

    International Nuclear Information System (INIS)

    Huczko, A.; Lange, H.; Calko, E.

    1999-01-01

    An astonishing scientific interest, embodied in over 15000 research articles so far, has been encountered since 1985 when fullerenes were discovered. From new superconductors to a rich electrochemistry and reaction chemistry, fullerene nanostructures continue to excite the scientific world, and new findings continue at record pace. This review presents many examples of the biochemical activities of fullerenes and derivatives, e. g. cytotoxic activity, selective DNA cleavage and antiviral activity against HIV. We also present some results of our testing which show that, despite its chemical and biochemical activity, fullerene matter does not present any health hazard directly related to skin irritation and allergic risks. (author)

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

    OpenAIRE

    Bankova, Vassya; Popova, Milena; Trusheva, Boryana

    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...

  8. Biologically stable [18F]-labeled benzylfluoride derivatives

    International Nuclear Information System (INIS)

    Magata, Yasuhiro; Lang, Lixin; Kiesewetter, Dale O.; Jagoda, Elaine M.; Channing, Michael A.; Eckelman, William C.

    2000-01-01

    Use of the [ 18 F]-fluoromethyl phenyl group is an attractive alternative to direct fluorination of phenyl groups because the fluorination of the methyl group takes place under milder reaction conditions. However, we have found that 4-FMeBWAY showed femur uptake equal to that of fluoride up to 30 min in rat whereas 4-FMeQNB had a significantly lower percent injected dose per gram in femur up to 120 min. For these and other benzylfluoride derivatives, there was no clear in vivo structure-defluorination relationship. Because benzylchlorides (BzCls) are known alkylating agents, benzylfluorides may be alkylating agents as well, which may be the mechanism of defluorination. On this basis, the effects of substitution on chemical stability were evaluated by the 4-(4-nitro-benzyl)-pyridine (NBP) test, which is used to estimate alkylating activity with NBP. The effect of substitution on the alkylating activity was evaluated for nine BzCl derivatives: BzCl; 3- or 4-methoxy (electron donation) substituted BzCl; 2-, 3-, or 4-nitro (electron withdrawing) substituted BzCl; and 2-, 3-, or 4-chloro (electron withdrawing) substituted BzCl. Taken together, the alkylating reactivity of 3-chloro-BzCl was the weakest. This result was then applied to [ 18 F]-benzylfluoride derivatives and in vivo and in vitro stability were evaluated. Consequently, 3-chloro-[ 18 F]-benzylfluoride showed a 70-80% decrease of defluorination in both experiments in comparison with [ 18 F]-benzylfluoride, as expected. Moreover, a good linear relationship between in vivo femur uptake and in vitro hepatocyte metabolism was observed with seven 18 F-labeled radiopharmaceuticals, which were benzylfluorides, alkylfluorides, and arylfluorides. Apparently, the [ 18 F]-fluoride ion is released by metabolism in the liver in vivo. In conclusion, 3-chloro substituted BzCls are the most stable, which suggests that 3-chloro benzylfluorides will be the most chemically stable compound. This result should be important in

  9. Structure-activity relationships of bumetanide derivatives

    DEFF Research Database (Denmark)

    Pedersen, Kasper Lykke; Töllner, Kathrin; Römermann, Kerstin

    2015-01-01

    , the effect of a series of diuretically active bumetanide derivatives was investigated on human NKCC2 variant A (hNKCC2A) expressed in Xenopus laevis oocytes. KEY RESULTS: Bumetanide blocked hNKCC2A transport with an IC50 of 4 μM. There was good correlation between the diuretic potency of bumetanide and its...... derivatives in dogs and their inhibition of hNKCC2A (r(2) = 0.817; P ... of the structural requirements that determine relative potency of loop diuretics on human NKCC2 splice variants, and may lead to the discovery of novel high-ceiling diuretics....

  10. An Efficient Synthesis of 3,4-Dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine Derivatives Catalyzed by Zirconyl(IV) Chloride and Evaluation of its Biological Activities

    Energy Technology Data Exchange (ETDEWEB)

    Kategaonkar, Amol H.; Sonar, Swapnil S.; Pokalwar, Rajkumar U.; Shingate, Bapurao B.; Shingare, Murlidhar S. [Babasaheb Ambedkar Marathwada University, Maharashtra (India); Kategaonkar, Atul H. [Maharashtra Institute of Pharmacy, Maharashtra (India)

    2010-06-15

    An efficient and novel one-pot synthesis of new 3,4-dihydro-3-substituted-2H-naphtho[2,1-e][1,3]oxazine derivatives from 1-naphthol, various anilines and formalin at room temperature grinding is presented. The six-membered N,O-heterocyclic skeleton was constructed via zirconyl(IV) chloride promoted Mannich type reaction. In vitro antimicrobial activities of synthesized compounds have been investigated against Gram-positive Bacillus subtilis, Gram negative Escherichia coli and two fungi Candida albicans and Aspergillus niger in comparison with standard drugs. The results of preliminary bioassay indicate that some of title compounds possess significant antibacterial and antifungal activity.

  11. Simple glycolipids of microbes: Chemistry, biological activity and metabolic engineering

    Directory of Open Access Journals (Sweden)

    Ahmad Mohammad Abdel-Mawgoud

    2018-03-01

    Full Text Available Glycosylated lipids (GLs are added-value lipid derivatives of great potential. Besides their interesting surface activities that qualify many of them to act as excellent ecological detergents, they have diverse biological activities with promising biomedical and cosmeceutical applications. Glycolipids, especially those of microbial origin, have interesting antimicrobial, anticancer, antiparasitic as well as immunomodulatory activities. Nonetheless, GLs are hardly accessing the market because of their high cost of production. We believe that experience of metabolic engineering (ME of microbial lipids for biofuel production can now be harnessed towards a successful synthesis of microbial GLs for biomedical and other applications. This review presents chemical groups of bacterial and fungal GLs, their biological activities, their general biosynthetic pathways and an insight on ME strategies for their production.

  12. Synthesis and biological evaluation of coumarin derivatives containing imidazole skeleton as potential antibacterial agents.

    Science.gov (United States)

    Hu, Yang; Shen, Yufeng; Wu, Xiaohu; Tu, Xiao; Wang, Gao-Xue

    2018-01-01

    Emergence of multidrug-resistant bacteria causes an urgent need for new generation of antibiotics, which may have a different mechanism of inhibition or killing action from the existing. Here, we report on the design, synthesis, and biological evaluation of thirty-nine coumarin derivatives in order to solve the antibacterial resistance by targeting at the inhibition of biosynthesis pathway of fatty acids. Their antibacterial activities against Escherichia coli, Staphylococcus aureus, Streptococcus agalactiae, and Flavobacterium cloumnare are tested and action mechanism against the key enzyme in bacterial fatty acid synthesis pathway are studied. The results show that compounds 13 and 18 have potent and broad spectrum antimicrobial activity. In addition, 9, 14 and 19 show eminent antimicrobial efficacy toward S. aureus, S. agalactiae, and F. cloumnare. Mechanistically, coumarin derivatives display the antibacterial activity via the control of FabI and FabK function. The structure-activity relationship analysis indicate that the length of linker and imidazole substitute group could significantly influence the antimicrobial activity, as well as the inhibitory activity against FabI and FabK. The structural optimization analysis of coumarin suggest that derivatives 9, 13, 14, 18 and 19 could be a viable way of preventing and controlling bacteria and considered as promising lead compounds for the development of commercial drugs. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  13. Expression and Purification of Soluble, Biologically Active ...

    African Journals Online (AJOL)

    Expression and Purification of Soluble, Biologically Active Recombinant Dipeptidyl Peptidase 4 (DPP4/CD26/ADAbp) Comprising the Extracellular Domain in the Yeast, Pichia ... Purpose: To investigate Pichia pastoris expression system for producing clinically usable, high-quality dipeptidyl peptidase 4 recombinant protein.

  14. Parameters of biological activity in colorectal cancer

    Czech Academy of Sciences Publication Activity Database

    Svobodová, Š.; Topolčan, O.; Holubec jr., L.; Levý, M.; Pecen, Ladislav; Svačina, Š.

    2011-01-01

    Roč. 31, č. 1 (2011), s. 373-378 ISSN 0250-7005 Institutional research plan: CEZ:AV0Z10300504 Keywords : colorectal cancer * biological activity * prognosis * tumor markers * angiogenetic factors * metalloproteinases * adhesion molecules Subject RIV: FD - Oncology ; Hematology Impact factor: 1.725, year: 2011

  15. Sulfonic acid functionalized boron nitride nanomaterials as a microwave-assisted efficient and highly biologically active one-pot synthesis of piperazinyl-quinolinyl fused Benzo[c]acridine derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Murugesan, Arul; Gengan, R.M., E-mail: genganrm@dut.ac.za; Krishnan, Anand

    2017-02-15

    Boron nitride nano material based solid acid catalyst was found to be an efficient and reusable sulfonic acid catalyst for the synthesis of one-pot Knoevenagel and Michael type reactions in 3, 3-dimethyl-9-(2-(4-methylpiperazin-1-yl) quinolin-3-yl)-3, 4, 9, 10-tetrahydroacridin-1(2H)-one derivatives under microwave irradiation conditions. The catalyst was prepared by mixing boron nitrile and (3-mercaptopropyl) trimethoxysilane. This is simple and safe method for the preparation of solid acid catalysts. The morphological properties of catalyst determined by using FT-IR, XRD, TEM, SEM and Raman spectroscopy. The synthesised catalyst was employed in Knoevenagel and Michael type reactions to synthesise novel piperazinyl-quinolinyl based acridine derivatives. Furthermore the newly-synthesised compounds have been used for molecular docking in DNA binding studies. The method developed in this study has the advantages of good yield, simplicity coupled with safety and short reaction time. Most importantly it was found that the solid acid catalyst can be recycled with only 5% loss of activity. - Highlights: • One-pot Synthesis of Knoevenagel and Michel type reactions. • Synthesis of Sulfonic acid Functionalized Boron nitride nano materials. • Synthesis of piperazinyl-quinolinyl fused Benzo[c]acridine derivatives under Microwave irradiation. • Molecular docking studies were performed on piperazinyl-quinolinyl acridine derivatives using DNA.

  16. New derivatives of aryl-propionic acid. Synthesis and biological evaluation.

    Science.gov (United States)

    Vasincu, Ioana; Apotrosoaei, Maria; Tuchiluş, Cristina; Pânzariu, Andreea Teodora; Dragostin, Oana; Lupaşcu, D; Profire, Lenuta

    2013-01-01

    To design new derivatives of aryl-propionic acid with potential antibacterial and antioxidant activity. New hydrazone of ibuprofen (2-(4-isobutylphenyl)propionic acid) have been synthesized by reaction of ethyl ester of ibuprofen with hydrazine hydrate and then condensation of corresponding hydrazide with various aromatic aldehydes. The synthesized compounds were screened for their antibacterial activity against Gram positive (Staphylococcus aureus ATCC 25923, Sarcinalutea ATCC 9341, Bacillus cereus ATCC 14579, Bacillus subtilis) and Gram negative bacterial strains (Escherichia coli ATCC 25922). Some of them were found to have good antibacterial activity. The antioxidant activity of these compounds was also tested using the total antiox idant capacity test. The chemical modulations performed on ibuprofen structure have a good influence on the biological activity of the synthesized compounds.

  17. Design, synthesis and biological evaluation of lapachol derivatives possessing indole scaffolds as topoisomerase I inhibitors.

    Science.gov (United States)

    Zhang, Chong; Qu, Yan; Niu, Bingxuan

    2016-11-15

    A series of novel lapachol derivatives possessing indole scaffolds was designed and synthesized. The in vitro anti-proliferative activity of these novel compounds was evaluated in Eca109 and Hela cell lines. Almost all the tested compounds showed manifested potent inhibitory activity against the two tested cancer cell lines. Topo I-mediated DNA relaxation activity indicated that these novel compounds have potent Topoisomerase I inhibition activity. The most potent compounds 4n and 4k demonstrated more cytotoxicity than camptothecin and was comparable to camptothecin in inhibitory activities on Topoisomerase I in our biological assay. In addition, the Hoechst 33342 staining method also showed that the complex can induce Hela cell apoptosis. Copyright © 2016 Elsevier Ltd. All rights reserved.

  18. Biological activity screening of seven Plectranthus species

    OpenAIRE

    Epole Ntungwe N; Joana Marçalo; Catarina Garcia; Catarina Reis; Catarina Teodósio; Carolina Oliveira; Cláudia Oliveira; Amílcar Roberto; Patrícia Rijo

    2017-01-01

    Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE) inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus,...

  19. Biological activity of SV40 DNA

    International Nuclear Information System (INIS)

    Abrahams, P.J.

    1978-01-01

    This thesis deals with a study on the biological activity of SV40 DNA. The transforming activity of SV40 DNA and DNA fragments is investigated in order to define as precisely as possible the area of the viral genome that is involved in the transformation. The infectivity of SV40 DNA is used to study the defective repair mechanisms of radiation damages of human xeroderma pigmentosum cells. (C.F.)

  20. Biology-oriented drug synthesis (BIODS) of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives, in vitro α-amylase inhibitory activity and in silico studies.

    Science.gov (United States)

    Taha, Muhammad; Imran, Syahrul; Ismail, Nor Hadiani; Selvaraj, Manikandan; Rahim, Fazal; Chigurupati, Sridevi; Ullah, Hayat; Khan, Fahad; Salar, Uzma; Javid, Muhammad Tariq; Vijayabalan, Shantini; Zaman, Khalid; Khan, Khalid Mohammed

    2017-10-01

    A new library of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives (1-23) were synthesized and characterized by EI-MS and 1 H NMR, and screened for their α-amylase inhibitory activity. Out of twenty-three derivatives, two molecules 19 (IC 50 =0.38±0.82µM) and 23 (IC 50 =1.66±0.14µM), showed excellent activity whereas the remaining compounds, except 10 and 17, showed good to moderate inhibition in the range of IC 50 =1.77-2.98µM when compared with the standard acarbose (IC 50 =1.66±0.1µM). A plausible structure-activity relationship has also been presented. In addition, in silico studies was carried out in order to rationalize the binding interaction of compounds with the active site of enzyme. Copyright © 2017 Elsevier Inc. All rights reserved.

  1. [Fe2L3]4+ Cylinders Derived from Bis(bidentate 2-Pyridyl-1,2,3-triazole “Click” Ligands: Synthesis, Structures and Exploration of Biological Activity

    Directory of Open Access Journals (Sweden)

    James D. Crowley

    2013-05-01

    Full Text Available A series of metallosupramolecular [Fe2L3](BF44 “click” cylinders have been synthesized in excellent yields (90%–95% from [Fe(H2O6](BF42 and bis(bidentate pyridyl-1,2,3-triazole ligands. All complexes were characterized by elemental analysis, IR, UV-vis, 1H-, 13C- and DOSY-NMR spectroscopies and, in four cases, the structures confirmed by X-ray crystallography. Molecular modeling indicated that some of these “click” complexes were of similar size and shape to related biologically active pyridylimine-based iron(II helicates and suggested that the “click” complexes may bind both duplex and triplex DNA. Cell-based agarose diffusion assays showed that the metallosupramolecular [Fe2L3](BF44 “click” cylinders display no antifungal activity against S. cerevisiae. This observed lack of antifungal activity appears to be due to the poor stability of the “click” complexes in DMSO and biological media.

  2. Synthesis and pharmacological activity of diterpenylnaphthoquinone derivatives.

    Science.gov (United States)

    Pertino, Mariano Walter; Theoduloz, Cristina; Palenzuela, Jose Antonio; Afonso, Maria del Mar; Yesilada, Erdem; Monsalve, Francisco; González, Paulo; Droguett, Daniel; Schmeda-Hirschmann, Guillermo

    2011-10-13

    New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.

  3. Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

    Directory of Open Access Journals (Sweden)

    Samar I. Faggal

    2012-04-01

    Full Text Available New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl piperazin-1-ylacetylindoline-2,3-dione (IIId was found to be the most potent.

  4. Determination of phosphorus using derivative neutron activation

    International Nuclear Information System (INIS)

    Scindia, Y.M.; Nair, A.G.C.; Reddy, A.V.R.; Manohar, S.B.

    2002-01-01

    For the determination of phosphorus in different matrices, the derivative neutron activation analysis is especially applicable to aqueous samples, since the conventional neutron activation analysis is not useful for the determination of phosphorus. Phosphorus when reacted with ammonium molybdate 4 hydrate and ammonium metavanadate forms molybdo vanado phosphoric acid. This complex is preconcentrated by extracting into methyl isobutyl ketone. The organic phase containing the molybdo vanado phosphoric acid is neutron activated and the phosphorus is determined through the activation product of 52 V. Preparation of this complex, its stoichiometry, application to trace level determination of phosphorus and improved detection limit are discussed. This method was applied for the analysis of industrial effluent samples. (author)

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

    Science.gov (United States)

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

    2012-01-01

    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

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

    Science.gov (United States)

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

    2013-03-01

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

  7. Antitumor and biological investigation of doubly cyclometalated ruthenium(II) organometallics derived from benzimidazolyl derivatives.

    Science.gov (United States)

    Elumalai, Palani; Jeong, Yong Joon; Park, Dae Won; Kim, Dong Hwan; Kim, Hyunuk; Kang, Se Chan; Chi, Ki-Whan

    2016-04-21

    In this study, we report the synthesis, anticancer and biological properties of three doubly cyclometalated phenylbenzimidazole derived ruthenium(ii) organometallics () and their corresponding three organic ligands. The structures of were fully characterized by various analytical techniques, and the meso stereoisomer of the doubly cyclometalated ruthenacycle was unambiguously confirmed by single crystal X-ray diffraction. The anticancer effects of the newly synthesized compounds were tested against selected human cancer cell lines AGS (gastric carcinoma), SK-hep-1 (hepatocellular carcinoma), and HCT-15 (colorectal carcinoma). The growth inhibitory effects of ruthenacycles on cancer cells were found to be considerably more effective against the abovementioned cancer cells than the reference drug oxaliplatin. Compound exhibited a more specific effect on the AGS cells. Gene-fishing and ELISA array were performed to analyze the target genes and cytokine secretion by . As a result, a significant reduction was observed in RPS21 by . Moreover, increased the secretion of cytokines such as IFNγ in macrophages and reduced the release of cytokines such as rantes and IGF-1. These results show that could be a very good anticancer drug through the regulation of the RPS21 gene and cytokines.

  8. Direct FGF receptor 1 activation through an anti-idiotypic strategy mimicks the biological activity of FGF-2 and inhibits the progression of the bladder carcinoma derived from NBT-II cells.

    Science.gov (United States)

    Malavaud, Bernard; Pedron, Sandrine; Sordello, Sylvie; Mazerolles, Catherine; Billottet, Clotilde; Thiery, Jean-Paul; Jouanneau, Jacqueline; Plouët, Jean

    2004-09-02

    The hypothesis that tumor growth is angiogenesis-dependent has been documented by a considerable body of direct and indirect experimental data. Since the discovery of the vascular endothelial growth factor (VEGF), most attention has been focused on the VEGF system. Although fibroblast growth factors 1 and 2 (FGF-1 and FGF-2) can exert a strong angiogenic activity when they are supplied as a single pharmacological agent, their role in pathological angiogenesis in preclinical models remains controversial. To decipher the contribution of FGF receptors in various models of angiogenesis, we took advantage of the anti-idiotypic strategy to obtain circulating agonists specific for FGFR-1 and FGFR-2 (AIdF-1 and AIdF-2). They mimicked FGF-1 and FGF-2 for receptor binding, signal transduction, proliferation of endothelial cells and differentiation of the bladder carcinoma cell NBT-II which expresses FGFR-2b but not FGFR-1. The constitutive expression of FGFR-1 allowed binding of FGF-2 and AIdF-2 and inhibition of the proliferation of NBT-II cells. AIdF-1 and AIdF-2 induced angiogenesis in the corneal pocket assay. Although FGFR-1 dimerization achieved by AIdF-2 injection led to highly differentiated and smaller NBT-II tumors, no sign of reduction of tumor angiogenesis was observed, thus suggesting that endothelial cells are resistant to FGF.

  9. Synthesis and biological evaluation of novel imidazolidine derivatives as candidates to schistosomicidal agents

    Directory of Open Access Journals (Sweden)

    Thiago José Matos-Rocha

    Full Text Available ABSTRACT Introduction: Schistosomiasis is an infectious parasitic disease caused by trematodes of the genus Schistosoma, which threatens at least 258 million people worldwide and its control is dependent on a single drug, praziquantel. The aim of this study was to evaluate the anti-Schistosoma mansoni activity in vitro of novel imidazolidine derivatives. Material and methods: We synthesized two novel imidazolidine derivatives: (LPSF/PTS10 (Z-1-(2-chloro-6-fluorobenzyl-4-(4-dimethylaminobenzylidene-5-thioxoimidazolidin-2-one and (LPSF/PTS23 (Z-1-(2-chloro-6-fluoro-benzyl-5-thioxo-4-(2,4,6-trimethoxy-benzylidene-imidazolidin-2-one. The structures of two compounds were determined by spectroscopic methods. During the biological assays, parameters such as motility, oviposition, mortality and analysis by Scanning Electron Microscopy were performed. Results: LPSF/PTS10 and LPSF/PTS23 were considered to be active in the separation of coupled pairs, mortality and to decrease the motor activity. In addition, LPSF/PTS23 induced ultrastructural alterations in worms, after 24 h of contact, causing extensive erosion over the entire body of the worms. Conclusion: The imidazolidine derivatives containing the trimetoxy and benzylidene halogens showed promising in vitro schistosomicidal activity.

  10. Monitoring Biological Activity at Geothermal Power Plants

    Energy Technology Data Exchange (ETDEWEB)

    Peter Pryfogle

    2005-09-01

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

  11. Role of arginine and its methylated derivatives in cancer biology and treatment

    Directory of Open Access Journals (Sweden)

    Tyihák Erno

    2001-12-01

    Full Text Available Abstract Both L-arginine supplementation and deprivation influence cell proliferation. The effect of high doses on tumours is determined by the optical configuration: L-arginine is stimulatory, D-arginine inhibitory. Arginine-rich hexapeptides inhibited tumour growth. Deprivation of L-arginine from cell cultures enhanced apoptosis. The pro-apoptotic action of NO synthase inhibitors, like NG-monomethyl-L-arginine, is manifested through inhibition of the arginase pathway. NG-hydroxymethyl-L-arginines caused apoptosis in cell cultures and inhibited the growth of various transplantable mouse tumours. These diverse biological activities become manifest through formaldehyde (HCHO because guanidine group of L-arginine in free and bound form can react rapidly with endogenous HCHO, forming NG-hydroxymethylated derivatives. L-arginine is a HCHO capturer, carrier and donor molecule in biological systems. The role of formaldehyde generated during metabolism of NG-methylated and hydroxymethylated arginines in cell proliferation and death can be shown. The supposedly anti-apoptotic homozygous Arg 72-p53 genotype may increase susceptibility of some cancers. The diverse biological effects of L-arginine and its methylated derivatives call for further careful studies on their possible application in chemoprevention and cancer therapy.

  12. Silychristin: Skeletal Alterations and Biological Activities

    Czech Academy of Sciences Publication Activity Database

    Biedermann, David; Buchta, M.; Holečková, Veronika; Sedlák, David; Valentová, Kateřina; Cvačka, Josef; Bednárová, Lucie; Křenková, Alena; Kuzma, Marek; Škuta, Ctibor; Peikerová, Žaneta; Bartůněk, Petr; Křen, Vladimír

    2016-01-01

    Roč. 79, č. 12 (2016), s. 3086-3092 ISSN 0163-3864 R&D Projects: GA ČR(CZ) GA15-03037S; GA MZd(CZ) NV16-27317A; GA MŠk LO1220; GA MŠk LM2015063; GA MŠk(CZ) LD15081 Institutional support: RVO:61388971 ; RVO:68378050 ; RVO:61388963 Keywords : Silychristin * skeletal alterations * biological activities Subject RIV: CC - Organic Chemistry Impact factor: 3.281, year: 2016

  13. Synthesis and Biological Evaluation of Novel Jatrorrhizine Derivatives with Amino Groups Linked at the 3-Position as Inhibitors of Acetylcholinesterase

    Directory of Open Access Journals (Sweden)

    Xiaofei Jiang

    2017-01-01

    Full Text Available Jatrorrhizine was considered as one of the active constituents of Coptis chinensis Franch. Herein, jatrorrhizine derivatives with substituted amino groups linked at the 3-position were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Jatrorrhizine derivatives inhibited the activity of acetylcholinesterase (AChE to a greater extent than the lead compound jatrorrhizine. All these jatrorrhizine derivatives were proved to be potent inhibitors of acetylcholinesterase (AChE with submicromolar IC50 values, but less sensitive to butyrylcholinesterase (BuChE, which suggests that these jatrorrhizine derivatives are selective for AChE/BuChE. Compound 3g gave the most potent inhibitor activity for AChE (IC50 = 0.301 μM, which is greater than the lead compound jatrorrhizine. All these results demonstrated that these jatrorrhizine derivatives are potential inhibitors for AChE.

  14. Radiation degradation of carbohydrates and their biological activities for plants

    International Nuclear Information System (INIS)

    Kume, T.; Nagasawa, N.; Matsuhashi, S.

    2000-01-01

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using 48 V and 62 Zn. (author)

  15. Radiation degradation of carbohydrates and their biological activities for plants

    Energy Technology Data Exchange (ETDEWEB)

    Kume, T.; Nagasawa, N.; Matsuhashi, S. [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment] [and others

    2000-03-01

    Radiation effects on carbohydrates such as chitosan, sodium alginate, carrageenan, cellulose, pectin have been investigated to improve the biological activities. These carbohydrates were easily degraded by irradiation and induced various kinds of biological activities such as anti-bacterial activity, promotion of plant growth, suppression of heavy metal stress, phytoalexins induction. Pectic fragments obtained from degraded pectin induced the phytoalexins such as glyceollins in soybean and pisatin in pea. The irradiated chitosan shows the higher elicitor activity for pisatin than that of pectin. For the plant growth promotion, alginate derived from brown marine algae, chitosan and ligno-cellulosic extracts show a strong activity. Kappa and iota carrageenan derived from red marine algae can promote growth of rice and the highest effect was obtained with kappa irradiated at 100 kGy. Some radiation degraded carbohydrates suppressed the damage of heavy metals on plants. The effects of irradiated carbohydrates on transportation of heavy metals have been investigated by PETIS (Positron Emitting Tracer Imaging System) and autoradiography using {sup 48}V and {sup 62}Zn. (author)

  16. Biological Validation of Plant-derived Anti-human Colorectal Cancer Monoclonal Antibody CO17-1A

    NARCIS (Netherlands)

    Jamal, Arshad; Ahn, Mi-Hyun; Song, Mira; Oh, Eun-Yi; Hong, Juyeon; Choo, Young-Kug; Ko, Kinarm; Han, Yeon Soo; Oh, Seung Han; Van Der Linden, Joke; Leusen, Jeanette H. W.; Ko, Kisung

    We validated expression and biological activities of plant-derived monoclonal antibody (MAb(P)) CO17-1A for its efficacy in cancer immunotherapy. PCR and immunoblot analyses demonstrated insertion and expression of heavy and light chains of MAb CO17-1A in transgenic plants, respectively. Confocal

  17. Biological activities of secondary metabolites of the order Zoanthids

    Directory of Open Access Journals (Sweden)

    Zahra Aminikhoei

    2015-11-01

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

  18. Controlled release of biologically active silver from nanosilver surfaces.

    Science.gov (United States)

    Liu, Jingyu; Sonshine, David A; Shervani, Saira; Hurt, Robert H

    2010-11-23

    Major pathways in the antibacterial activity and eukaryotic toxicity of nanosilver involve the silver cation and its soluble complexes, which are well established thiol toxicants. Through these pathways, nanosilver behaves in analogy to a drug delivery system, in which the particle contains a concentrated inventory of an active species, the ion, which is transported to and released near biological target sites. Although the importance of silver ion in the biological response to nanosilver is widely recognized, the drug delivery paradigm has not been well developed for this system, and there is significant potential to improve nanosilver technologies through controlled release formulations. This article applies elements of the drug delivery paradigm to nanosilver dissolution and presents a systematic study of chemical concepts for controlled release. After presenting thermodynamic calculations of silver species partitioning in biological media, the rates of oxidative silver dissolution are measured for nanoparticles and macroscopic foils and used to derive unified area-based release kinetics. A variety of competing chemical approaches are demonstrated for controlling the ion release rate over 4 orders of magnitude. Release can be systematically slowed by thiol and citrate ligand binding, formation of sulfidic coatings, or the scavenging of peroxy-intermediates. Release can be accelerated by preoxidation or particle size reduction, while polymer coatings with complexation sites alter the release profile by storing and releasing inventories of surface-bound silver. Finally, the ability to tune biological activity is demonstrated through a bacterial inhibition zone assay carried out on selected formulations of controlled release nanosilver.

  19. Synthesis and biological assessment of novel acylhydrazone derivatives of 2-methyl-1,4-naphthoquinone

    Directory of Open Access Journals (Sweden)

    Kamal Bouhadir

    2017-10-01

    Full Text Available Naphthoquinones are medicinally important molecules with a diverse array of biological properties such as antimicrobial, antifungal, antiviral, anti-inflammatory, anti-artherosclerotic and anticarcinogenic activities. In this study, we report the simple and direct preparation of a new group of novel menadione-hydrazone conjugates by reaction of 2-methyl-1,4-naphthoquinones with several aliphatic, aromatic and nucleobase hydrazides. The menadione-hydrazone conjugates were produced in excellent yields and characterized by IR, NMR and HRMS. The menadione derivatives were tested for their anticancer effects against human colon cancer HCT116 and human breast cancer MCF-7 cell lines. Interestingly, the molecules displayed disparate activities against both cell lines; the menadione hydrazones derived from the lipophilic myristic hydrazide and stearic hydrazide exhibited the most potent activity against HCT116 cell lines with IC50 of 89 and 64 μM. The most effective compounds against MCF-7 cells were the lauric hydrazide and benzoic hydrazide-derived menadione hydrazones with IC50 of 56 µM.

  20. Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: synthesis and in vitro biological evaluation. Part 1.

    Science.gov (United States)

    Bozorov, Khurshed; Ma, Hai-Rong; Zhao, Jiang-Yu; Zhao, Hai-Qing; Chen, Hua; Bobakulov, Khayrulla; Xin, Xue-Lei; Elmuradov, Burkhon; Shakhidoyatov, Khusnutdin; Aisa, Haji A

    2014-09-12

    Series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate (DDTD) derivatives: azomethines of DDTD (2a-l) have been synthesized and screened for their anticancer, antimicrobial and anti-diabetic activities. The novel synthesized compounds were characterized by (1)H, (13)C NMR, MS and FT-IR analyses. All compounds were evaluated for their antiproliferative activity against three types of cancer cell line such as T47D and MCF-7 (human breast cancer), Hela (human cervical cancer) and Ishikawa (human endometrial cancer) lines. The results showed that most compounds exhibited significant antiproliferative activity against breast cancer cells. The majority of azomethines DDTD influenced strongly against breast cancer cells T47D and MCF-7, among them compounds 2b (2.3 μM), 2c (12.1 μM), 2e (13.2 μM), 2i (14.9 μM), 2j (16.0 μM), 2k (7.1 μM), 2l (8.6 μM) manifest potent anticancer activity against cancer cell T47D than Doxorubicin (DOX, 15.5 μM). Compound 2j has shown potent activity on all three types of cancer cells concurrently and IC50 values were considerably low in comparison with positive control DOX. In addition, all compounds were tested for antimicrobial activity against Staphylococcus aureus ATCC 6538 (Gram positive bacteria), Escherichia coli ATCC 11229 (Gram negative bacteria) and Candida albicans ATCC 10231 (Fungi) strains and 2j which contains in the ring nitrofurfural fragment, showed the highest effect on the three species of microbial pathogens simultaneously. Some compounds induced enzymatic inhibition in a concentration-dependent manner on PTP-1B inhibitor. Copyright © 2014. Published by Elsevier Masson SAS.

  1. Synthesis and Pharmacological Activity of Diterpenylnaphthoquinone Derivatives

    Directory of Open Access Journals (Sweden)

    Guillermo Schmeda-Hirschmann

    2011-10-01

    Full Text Available New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, and hepatocellular carcinoma (Hep G2. Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.

  2. Biological Activities and Phytochemicals of Swietenia macrophylla King

    Directory of Open Access Journals (Sweden)

    Habsah Abdul Kadir

    2013-08-01

    Full Text Available Swietenia macrophylla King (Meliaceae is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.

  3. Exploring the biological activities of Echeveria leucotricha.

    Science.gov (United States)

    Martínez Ruiz, María G; Gómez-Velasco, Anaximandro; Juárez, Zaida N; Hernández, Luis R; Bach, Horacio

    2013-01-01

    Echeveria leucotricha J. A. Purpus (Crassulaceae) was evaluated for its potential antibacterial, antifungal, antiparasitic, cytotoxic and anti-inflammatory bioactivities. Aerial parts were extracted with hexane, methanol and chloroform, and fractionated accordingly. Biological activity was assessed in vitro against five Gram-positive and four Gram-negative bacteria, four human pathogenic fungi and the protozoan Leishmania donovani. Extracts and fractions showing bioactivities were further investigated for their cytotoxic activities on macrophages. Results show that several extracts and fractions exhibited significant antibacterial, antifungal, and antiparasitic activities, but no anti-inflammatory activity was recorded. Here, we report for the first time, and to the best of our knowledge, these bioactivities, which suggest that this plant can be used in the traditional Mexican medicine.

  4. Discrepancy of biologic behavior influenced by bone marrow derived cells in lung cancer.

    Science.gov (United States)

    Zhang, Jie; Niu, Xiao-Min; Liao, Mei-Lin; Liu, Yun; Sha, Hui-Fang; Zhao, Yi; Yu, Yong-Feng; Tan, Qiang; Xiang, Jia-Qing; Fang, Jing; Lv, Dan-Dan; Li, Xue-Bing; Lu, Shun; Chen, Hai-Quan

    2010-11-01

    Disseminated cancer cells may initially require local nutrients and growth factors to thrive and survive in bone marrow. However, data on the influence of bone marrow derived cells (BMDC, also called bone stromal cells in some publications) on lung cancer cells is largely unexplored. This study explored the mechanism of how bone stromal factors contribute to the bone tropism in lung cancer. The difference among lung cancer cell lines in their abilities to metastasize to bone was found using the SCID animal model. Supernatant of bone marrow aspiration (BM) and condition medium from human bone stromal cells (BSC) were used to study the activity of bone stromal factors. We found bone stromal factors significantly increased the proliferation, invasion, adhesion and expression of angiogenosis-related factors, and inhibited the apoptosis for high bone metastasis H460 lung cancer cells. These biologic effects were not seen in SPC-A1 or A549 cells, which are low bone metastasis lung cancer cells. Adhesion of H460 cells to surface coated with bone stromal cells can activate some signal transduction pathways, and alter the expression of adhesion associated factors, including integrin β 3 and ADAMTS-1, two potential targets related with bone metastasis. We concluded that bone marrow derived cells had a profound effect on biological behavior of lung cancers, therefore favoring the growth of lung cancer cells in bone.

  5. Synthesis and Biological Activity of Reversed Pyrimidine Nucleosides

    Directory of Open Access Journals (Sweden)

    Nataša Župančić

    2015-03-01

    Full Text Available An efficient approach to reversed nucleosides which enables their synthesis in gram quantities is described. N-1′-Pyrimidine reversed nucleosides were prepared by treating of the sodium salt of pyrimidine bases with protected 5-tosyl ribose. Additionally, N-1′,N-3′-disubstituted reversed nucleosides were isolated in the condensation reactions with the 5-halogen pyrimidines. Using the Sonogashira coupling of 5′-iodouracil reversed nucleoside with ethynyltrimethyl silane gave 5′-ethynyl derivative which was further transformed into 5′-acetyl reversed nucleoside. Biological activity of deprotected reversed nucleosides was validated on the panel of six human carcinoma cell lines (HeLa, MIAPaCa2, Hep2, NCI-H358, CaCo-2, and HT-29. 5′-Iodouracil derivative displayed moderate growth inhibition activity against human colon carcinoma (CaCo-2 cells.

  6. Isoprenoid-derived plant signaling molecules: biosynthesis and biological importance

    Czech Academy of Sciences Publication Activity Database

    Tarkowská, Danuše; Strnad, Miroslav

    2018-01-01

    Roč. 247, č. 5 (2018), s. 1051-1066 ISSN 0032-0935 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Dimethylallyl diphosphate * Isopentenyl diphosphate * Isoprenoids * Phytoecdysteroids * Plant hormones * Terpenoids Subject RIV: EB - Genetics ; Molecular Biology OBOR OECD: Biochemical research methods Impact factor: 3.361, year: 2016

  7. Recyclable Keggin Heteropolyacids as an Environmentally Benign Catalyst for the Synthesis of New 2-Benzoylamino-N-phenyl-benzamide Derivatives under Microwave Irradiations at Solvent-Free Conditions and the Evaluation of Biological Activity.

    Science.gov (United States)

    Ighilahriz-Boubchir, Karima; Boutemeur-Kheddis, Baya; Rabia, Cherifa; Makhloufi-Chebli, Malika; Hamdi, Maamar; Silva, Artur M S

    2017-12-21

    2-Benzoylamino- N -phenyl-benzamide derivatives ( 5a - h ) were prepared from 2-phenyl-3,1-(4 H )-benzoxazin-4-one 3 and substituted anilines 4a - h in the presence of a Keggin-type heteropolyacids series (H₃PW 12 O 40 ·13H₂O; H₄SiW 12 O 40 ·13H₂O; H₄SiMo 12 O 40 ·13H₂O; and H₃PMo 12 O 40 ·13H₂O) as catalysts without solvent and under microwave irradiation. We found that the use of H₃PW 12 O 40 ·13H₂O acid coupled to microwave irradiation allowed obtaining a high-yielding reaction with a short time. The compound structures were established by ¹H-NMR and 13 C-NMR. The antibacterial and antifungal activities of the synthesized compounds exhibited an inhibition of the growth of bacteria and fungi.

  8. Biological Activities of Royal Jelly - Review

    Directory of Open Access Journals (Sweden)

    Crenguţa I. Pavel

    2011-10-01

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

  9. Anticonvulsant activity of novel 1-(morpholinomethyl-3-substituted isatin derivatives

    Directory of Open Access Journals (Sweden)

    Govindaraj Saravanan

    2014-06-01

    Full Text Available A variety of novel isatin derivatives 5a–5j and 6a–6j were synthesized and characterized by spectroscopic means and elemental analysis. The title compounds were investigated for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by the rotorod test. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Among the synthesized analogs, the most active one was 6f that revealed protection in MES at a dose of 30 mg/kg (i.p. after 0.5 h and 4 h. This molecule also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h and 300 mg/kg (4 h.

  10. Synthesis, physical-chemical and biological properties of 7-benzyl-3-methyl-8-thioxanthine derivatives

    Directory of Open Access Journals (Sweden)

    D. H. Ivanchenko

    2017-12-01

    Full Text Available Introduction . Interest to the problem of creating new effective antimicrobial agents among xanthine derivatives does not decrease. Primarily, this is due to the increasing of microbial resistance to conventional antimicrobial agents and the emergence of their new strains. In recent years interest to the therapeutic use of antioxidants in the treatment of diseases associated with oxidative stress has increased. The aim of this work is to elaborate simple laboratory methods of 7-benzyl-3-methyl-8-thioxanthine derivatives synthesis, unspecified in scientific papers earlier, and to study their physical, chemical and biological properties. Materials and methods. The melting point has been determined with the help of an open capillary method with PTP-M device. Elemental analysis has been performed with the help of the instrument Elementar Vario L cube, NMR-spectra have been taken on a spectrometer Bruker SF-400 (operating frequency of 400 MHz, solvent DMSO, internal standard – TMS. Study of antimicrobial and antifungal activity of synthesized compounds has been performed by two-fold serial dilution method. Standard test strains have been used for the study: Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 885-653. Dimethylsulfoxide was used as the solvent of the compounds. Results. Under short-time heating up of the initial 7-benzyl-3-methyl-8-thioxanthine with alkyl, alkenyl, benzyl halides or heteroalkylchlorides in a water-propanol-2 mixture in the presence of an equimolar amount of sodium hydroxide leads to the formation of 8-S-substituted of 7-benzyl-3-methylxanthines. Structure of synthesized compounds was definitely proved by NMR-spectroscopy. We conducted primary screening research of antimicrobial activity of 7-benzyl-3-methyl-8-thioxanthine derivatives, which revealed moderate and weak activity in concentrations 50-100 mcg/ml. Most of the obtained compounds showed a

  11. Fluid dynamics in biological active nematics

    Science.gov (United States)

    Tan, Amanda; Hirst, Linda

    We use biological materials to form a self-mixing active system that consists of microtubules driven by kinesin clusters. Microtubules are rigid biopolymers that are a part of the cytoskeleton. Kinesin motors are molecular motors that walk along microtubules to transport cellular cargo. In this system, microtubules are bundled together, and as the kinesin clusters walk along the filaments, the microtubule bundles move relative to each other. As microtubules shear against each other, they extend, bend, buckle and fracture. When confined in a 2D water-oil interface, the system becomes an active nematic that self-mixes due to the buckling and fracturing. To quantify this self-mixing, we attached beads to the microtubules, and tracked their motion. We quantify the quality of mixing using the bead trajectories. This new active material has potential applications as a self-mixing solvent. CCBM NSF-CREST, UC Merced Health Science Research Institute.

  12. Biological activities of Curcuma longa L.

    Directory of Open Access Journals (Sweden)

    Araújo CAC

    2001-01-01

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

  13. Biological upgrading of coal-derived synthesis gas: Final report

    Energy Technology Data Exchange (ETDEWEB)

    Barik, S.; Johnson, E.R.; Ko, C.W.; Clausen, E.C.; Gaddy, J.L.

    1986-10-01

    The technical feasibility of the biological conversion of coal synthesis gas to methane has been demonstrated in the University of Arkansas laboratories. Cultures of microorganisms have been developed which achieve total conversion in the water gas shift and methanation reactions in either mixed or pure cultures. These cultures carry out these conversions at ordinary temperatures and pressures, without sulfur toxicity. Several microorganisms have been identified as having commercial potential for producing methane. These include a mixed culture of unidentified bacteria; P. productus which produces acetate, a methane precursor; and Methanothrix sp., which produces methane from acetate. These cultures have been used in mixed reactors and immobilized cell reactors to achieve total CO and H/sub 2/ conversion in a retention time of less than two hours, quite good for a biological reactor. Preliminary economic projections indicate that a biological methanation plant with a size of 5 x 10/sup 10/ Btu/day can be economically attractive. 42 refs., 26 figs., 86 tabs.

  14. Polysulfides as biologically active ingredients of garlic.

    Science.gov (United States)

    Münchberg, Ute; Anwar, Awais; Mecklenburg, Susanne; Jacob, Claus

    2007-05-21

    Garlic has long been considered as a natural remedy against a range of human illnesses, including various bacterial, viral and fungal infections. This kind of antibiotic activity of garlic has mostly been associated with the thiosulfinate allicin. Even so, recent studies have pointed towards a significant biological activity of trisulfides and tetrasulfides found in various Allium species, including a wide range of antibiotic properties and the ability of polysulfides to cause the death of certain cancer cells. The chemistry underlying the biological activity of these polysulfides is currently emerging. It seems to include a combination of several distinct transformations, such as oxidation reactions, superoxide radical and peroxide generation, decomposition with release of highly electrophilic S(x) species, inhibition of metalloenzymes, disturbance of metal homeostasis and membrane integrity and interference with different cellular signalling pathways. Further research in this area is required to provide a better understanding of polysulfide reactions within a biochemical context. This knowledge may ultimately form the basis for the development of 'green' antibiotics, fungicides and possibly anticancer agents with dramatically reduced side effects in humans.

  15. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...... includes multipoint intermolecular interactions that probably involve aggregation of both polymorphic and monomorphic T cell surface molecules. Such aggregations have been shown in vitro to markedly enhance and, in some cases, induce T cell activation. The production of T-derived lymphokines that have been...... implicated in B cell activation is dependent on the T cell receptor for antigen and its associated CD3 signalling complex. T-dependent help for B cell activation is therefore similarly MHC-restricted and involves T-B intercellular interaction. Recent reports that describe antigen-independent B cell...

  16. Biological Activities of Polyphenols from Grapes

    Directory of Open Access Journals (Sweden)

    Hua-Bin Li

    2010-02-01

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

  17. Biological Activities of Polyphenols from Grapes

    Science.gov (United States)

    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

  18. Urine: Waste product or biologically active tissue?

    Science.gov (United States)

    2018-03-01

    Historically, urine has been viewed primarily as a waste product with little biological role in the overall health of an individual. Increasingly, data suggest that urine plays a role in human health beyond waste excretion. For example, urine might act as an irritant and contribute to symptoms through interaction with-and potential compromise of-the urothelium. To explore the concept that urine may be a vehicle for agents with potential or occult bioactivity and to discuss existing evidence and novel research questions that may yield insight into such a role, the National Institute of Diabetes and Digestive and Kidney Disease invited experts in the fields of comparative evolutionary physiology, basic science, nephrology, urology, pediatrics, metabolomics, and proteomics (among others) to a Urinology Think Tank meeting on February 9, 2015. This report reflects ideas that evolved from this meeting and current literature, including the concept of urine quality, the biological, chemical, and physical characteristics of urine, including the microbiota, cells, exosomes, pH, metabolites, proteins, and specific gravity (among others). Additionally, the manuscript presents speculative, and hopefully testable, ideas about the functional roles of urine constituents in health and disease. Moving forward, there are several questions that need further understanding and pursuit. There were suggestions to consider actively using various animal models and their biological specimens to elaborate on basic mechanistic information regarding human bladder dysfunction. Published 2018. This article is a U.S. Government work and is in the public domain in the USA.

  19. Reconstructing Causal Biological Networks through Active Learning.

    Directory of Open Access Journals (Sweden)

    Hyunghoon Cho

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

  20. Study of Biological Pigments by Single Specimen Derivative Spectrophotometry

    Science.gov (United States)

    Goldstein, Jack M.

    1970-01-01

    The single specimen derivative (SSD) method provides an absolute absorption spectrum of a substance in the absence of a suitable reference. Both a reference and a measuring monochromatic beam pass through a single sample, and the specimen itself acts as its own reference. The two monochromatic beams maintain a fixed wavelength difference upon scanning, and the difference in absorbance of the two beams is determined. Thus, the resulting spectrum represents the first derivative of the conventional type absorption spectrum. Tissues and cell fractions have been examined at room and liquid N2 temperature and chromophoric molecules such as the mitochondrial cytochromes and blood pigments have been detectable in low concentrations. In the case of isolated cellular components, the observed effects of substrates and inhibitors confirm similar studies by conventional spectrophotometry. The extension of the SSD concept to the microscopic level has permitted the study of the tissue compartmentalization and function of cytochromes and other pigments within layered tissue. PMID:4392452

  1. Antispasmodic activity of xanthoxyline derivatives: structure-activity relationships.

    Science.gov (United States)

    Cechinel Filho, V; Miguel, O G; Nunes, R J; Calixto, J B; Yunes, R A

    1995-04-01

    The antispasmodic activity of several xanthoxyline derivatives against acetylcholine-induced contraction of the guinea pig ileum was evaluated in vitro. The acetophenones with two methoxyl groups, mainly in the 3,4 positions, exhibited potent antispasmodic activity. Modification of the hydroxyl group in xanthoxyline by the introduction of benzoyl, acetyl, or tosyl groups produced inactive compounds, whereas the introduction of benzyl or p-methoxybenzyl groups furnished compounds that were four- to eight-fold more potent than xanthoxyline. In marked contrast, the introduction of a methyl group gave a compound that caused contractant activity. Modification of the carbonyl group of xanthoxyline lead to inactive compounds, whereas the condensation of xanthoxyline with benzaldehydes gave chalkones that were about fivefold more potent than xanthoxyline. The introduction of benzyl and styrene groups, on the basis of the similarity with papaverine, improves the antispasmodic action of the xanthoxyline derivates. Our results suggest that the methoxyl and carbonyl groups are critical structural points for the antispasmodic activity of xanthoxyline derivatives. The hydroxyl group improves antispasmodic activity, but is not fundamental to its manifestation.

  2. Synthesis and biological evaluation of some New pyrimidine derivatives

    Directory of Open Access Journals (Sweden)

    Firyal Weli Askar

    2017-06-01

    Full Text Available New pyrimidine derivatives comprising azo, schiff's bases, chalcones, and chromene ring moieties were prepared.The newly synthesized compounds have been established on the basis of their m.p., TLC, FT-IR, UV-Vis ,¹H-NMR data and element analysis. These compounds were screened for their antimicrobial and in vitro antioxidant properties. The results of this investigation revealed that these compounds are potent antimicrobial and antioxidant agent.

  3. Studies on digoxin derivatives in different biological media by radioimmunoassay

    International Nuclear Information System (INIS)

    Barmasch, Martha; Perez, L.N.; Altschuler, Noe.

    1978-05-01

    The fundamental aim of this study was to develop a methodology to be applied to pharmacological studies, directed to demonstrate the passage of digitalic compounds through the blood-brain barrier. This study was a comparative one between β methyl digoxin (βMD) and digitoxin (Dt). A methodology of radioimmunoassay was developed for different biological media: serum (S), plasma (P) and cerebro spinal fluid (CSF). In addition, the immunochemical behaviour (affinity, displacement, etc.) of βMD was studied when reacted with digoxin (D) and digoxin-antisera, supplied by the commercial kits utilized in these studies. (author) [es

  4. Quinones from plants of northeastern Brazil: structural diversity, chemical transformations, NMR data and biological activities.

    Science.gov (United States)

    Lemos, Telma L G; Monte, Francisco J Q; Santos, Allana Kellen L; Fonseca, Aluisio M; Santos, Hélcio S; Oliveira, Mailcar F; Costa, Sonia M O; Pessoa, Otilia D L; Braz-Filho, Raimundo

    2007-05-20

    The present review focus in quinones found in species of Brazilian northeastern Capraria biflora, Lippia sidoides, Lippia microphylla and Tabebuia serratifolia. The review cover ethnopharmacological aspects including photography of species, chemical structure feature, NMR datea and biological properties. Chemical transformations of lapachol to form enamine derivatives and biological activities are discussed.

  5. Chemical constituents and biological activities of the genus Linaria (Scrophulariaceae).

    Science.gov (United States)

    Cheriet, Thamere; Mancini, Ines; Seghiri, Ramdane; Benayache, Fadila; Benayache, Samir

    2015-01-01

    This is a review on 95 references dealing with the genus Linaria (Scrophularioideae-Antirrhineae tribe), a known genus of the Scrophulariaceae family, which comprises about 200 species mainly distributed in Europe, Asia and North Africa. The use of some Linaria species in folk medicine has attracted the attention for chemical and biological studies. This report is aimed to be a comprehensive overview on the isolated or identified known and often new metabolites from the 41 Linaria species so far cited. It is organised presenting first the phytochemical classes of alkaloids, polyphenols including flavonoids, the latter being quite diffused and mostly present as flavones, flavonols and their glycosides, and terpenoids including iridoids and steroids. Second, the results from biological investigation on plant extracts, pure natural products isolated from Linaria species and some synthetic derivatives are reported, with antitumour, anti-acetylcholinesterase, anti-inflammatory and analgesic, antioxidant and antibacterial activities.

  6. Chemistry and biology of natural product derived protease inhibitors

    OpenAIRE

    Stolze, Sara Christina

    2012-01-01

    Im Rahmen dieser Dissertation sollten Naturstoffe und davon abgeleitete Derivate synthetisiert und im Hinblick auf ihre biologische Aktivität als Protease-Inhibitoren untersucht werden. Für die Naturstoffklasse der 3-Amino-6-Hydroxy-2-piperidon(Ahp)-Cyclodepsipeptide, die als nicht-kovalente Serin-Protease-Inhibitoren bekannt sind, konnte eine Festphasensynthese basierend auf einem allgemeinen Ahp-Vorläufermolekül entwickelt werden. Für den Ahp-Vorläufer wurde eine Lösungssynthese entwicke...

  7. Biological activity screening of seven Plectranthus species

    Directory of Open Access Journals (Sweden)

    Epole Ntungwe N

    2017-07-01

    Full Text Available Natural products from Plectranthus spp. plants have an ethnopharmacological use, inspiring several scientific investigations. As such, this work aims to perform a biological activity screening in order to scientifically validate the use of these plants. Assays on in vitro acetylcholinesterase (AChE inhibition, antioxidant effects, antimicrobial activity and Artemia salina lethality were performed on seven Plectranthus spp. extracts (P. swynnertonii, P. welwischii, P. woodii, P. cylindraceus, P. spicatus, P. ramosior and P. petiolaris. Acetonic extracts were obtained by sonication (10% w/v, where P. ramosior had the highest yield of dry extract (13.49% w/w. In the AChE inhibition assay, only P. cylindraceus extract decreased enzymatic activity (30.2 ± 3.78%. The antimicrobial activity was screened using the well diffusion method, against Gram positive and negative bacteria and yeast. P. ramosior extract showed not only an inhibition zone against S. aureus and C. albicans (15 and 11 mm, respectively, but also the highest scavenging activity (DPPH method, 36.4 ± 0.04%. On the lethality test in A. salina, P. swynnertonnii extract was the most toxic (LC50 = 0.036 mg/L. These preliminary results showed that P. cylindraceus, P. ramosior and P. swynnertonnii are potential bioactive extracts for further isolation and antimicrobial and cytotoxic studies.

  8. Novel Triazole Hybrids of Betulin: Synthesis and Biological Activity Profile.

    Science.gov (United States)

    Bębenek, Ewa; Jastrzębska, Maria; Kadela-Tomanek, Monika; Chrobak, Elwira; Orzechowska, Beata; Zwolińska, Katarzyna; Latocha, Małgorzata; Mertas, Anna; Czuba, Zenon; Boryczka, Stanisław

    2017-11-01

    Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by ¹H and 13 C NMR, IR, and high-resolution mass spectrometry (HR-MS) analysis. The target triazoles were screened for their antiviral activity against DNA and RNA viruses. The cytotoxic activity of the obtained compounds 5a - k and 6a - h was determined using five human cancer cell lines (T47D, MCF-7, SNB-19, Colo-829, and C-32) by a WST-1 assay. The bistriazole 6b displayed a promising IC 50 value (0.05 μM) against the human ductal carcinoma T47D (500-fold higher potency than cisplatin). The microdilution method was applied for an evaluation of the antimicrobial activity of all of the compounds. The triazole 5e containing a 3'-deoxythymidine-5'-yl moiety exhibited antibacterial activity against two gram-negative bacteria vz. Klebsiella pneumoniae and Escherichia coli (minimal inhibitory concentration (MIC) range of 0.95-1.95 μM).

  9. Novel Triazole Hybrids of Betulin: Synthesis and Biological Activity Profile

    Directory of Open Access Journals (Sweden)

    Ewa Bębenek

    2017-11-01

    Full Text Available Betulin derivatives containing a 1,2,3-triazole ring possess a wide spectrum of biological activities, including antiviral, anticancer, and antibacterial activity. A series of novel triazoles were prepared by the 1,3-dipolar cycloaddition reaction between the alkyne derivatives of betulin and organic azides. The chemical structures of the obtained compounds were defined by 1H and 13C NMR, IR, and high-resolution mass spectrometry (HR-MS analysis. The target triazoles were screened for their antiviral activity against DNA and RNA viruses. The cytotoxic activity of the obtained compounds 5a–k and 6a–h was determined using five human cancer cell lines (T47D, MCF-7, SNB-19, Colo-829, and C-32 by a WST-1 assay. The bistriazole 6b displayed a promising IC50 value (0.05 μM against the human ductal carcinoma T47D (500-fold higher potency than cisplatin. The microdilution method was applied for an evaluation of the antimicrobial activity of all of the compounds. The triazole 5e containing a 3′-deoxythymidine-5′-yl moiety exhibited antibacterial activity against two gram-negative bacteria vz. Klebsiella pneumoniae and Escherichia coli (minimal inhibitory concentration (MIC range of 0.95–1.95 μM.

  10. Recyclable Keggin Heteropolyacids as an Environmentally Benign Catalyst for the Synthesis of New 2-Benzoylamino-N-phenyl-benzamide Derivatives under Microwave Irradiations at Solvent-Free Conditions and the Evaluation of Biological Activity

    Directory of Open Access Journals (Sweden)

    Karima Ighilahriz-Boubchir

    2017-12-01

    Full Text Available 2-Benzoylamino-N-phenyl-benzamide derivatives (5a–h were prepared from 2-phenyl-3,1-(4H-benzoxazin-4-one 3 and substituted anilines 4a–h in the presence of a Keggin-type heteropolyacids series (H3PW12O40·13H2O; H4SiW12O40·13H2O; H4SiMo12O40·13H2O; and H3PMo12O40·13H2O as catalysts without solvent and under microwave irradiation. We found that the use of H3PW12O40·13H2O acid coupled to microwave irradiation allowed obtaining a high-yielding reaction with a short time. The compound structures were established by 1H-NMR and 13C-NMR. The antibacterial and antifungal activities of the synthesized compounds exhibited an inhibition of the growth of bacteria and fungi.

  11. Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues

    Directory of Open Access Journals (Sweden)

    Jaroslaw Polanski

    2009-10-01

    Full Text Available 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.

  12. Antimicrobial activity of resin acid derivatives.

    Science.gov (United States)

    Savluchinske-Feio, Sonia; Curto, Maria João Marcelo; Gigante, Bárbara; Roseiro, J Carlos

    2006-09-01

    The wide potential of resin acids as bioactive agents gave rise to a growing effort in the search for new applications of the natural forms and their derivatives. In some of these compounds, the antimicrobial activity is associated to the presence in the molecules of functional groups such as the hydroxyl, aldehyde, and ketone or to their cis or trans configurations. The resin acid family covers a spectrum of antimicrobial activities against several microorganisms, from bacteria to fungi, in which the mode of action was studied by electron microscopy. The morphological alterations are consistent with an unspecific mode of action causing inhibition of the fungal growth or damaging the fungal cells in parallel with a mechanism of resistance based on the retention of the compound by the lipid accumulation. The sterol composition of phytopathogenic fungi Botrytis cinerea and Lophodermium seditiosum treated with methyl cis-7-oxo-deisopropyldehydroabietate revealed the presence of ergosterol (M+ 396) and dihydroergosterol (M+ 398) in both cultures showing that this compound did not interfere with the ergosterol metabolic pathway of both fungi.

  13. Distribution and biological activities of the flavonoid luteolin.

    Science.gov (United States)

    López-Lázaro, Miguel

    2009-01-01

    Epidemiological evidence suggests that flavonoids may play an important role in the decreased risk of chronic diseases associated with a diet rich in plant-derived foods. Flavonoids are also common constituents of plants used in traditional medicine to treat a wide range of diseases. The purpose of this article is to summarize the distribution and biological activities of one of the most common flavonoids: luteolin. This flavonoid and its glycosides are widely distributed in the plant kingdom; they are present in many plant families and have been identified in Bryophyta, Pteridophyta, Pinophyta and Magnoliophyta. Dietary sources of luteolin include, for instance, carrots, peppers, celery, olive oil, peppermint, thyme, rosemary and oregano. Preclinical studies have shown that this flavone possesses a variety of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial and anticancer activities. The ability of luteolin to inhibit angiogenesis, to induce apoptosis, to prevent carcinogenesis in animal models, to reduce tumor growth in vivo and to sensitize tumor cells to the cytotoxic effects of some anticancer drugs suggests that this flavonoid has cancer chemopreventive and chemotherapeutic potential. Modulation of ROS levels, inhibition of topoisomerases I and II, reduction of NF-kappaB and AP-1 activity, stabilization of p53, and inhibition of PI3K, STAT3, IGF1R and HER2 are possible mechanisms involved in the biological activities of luteolin.

  14. Synthesis and biological activity of radiolabeled phytosterols

    Energy Technology Data Exchange (ETDEWEB)

    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.

  15. Synthesis and biological activity of radiolabeled phytosterols

    International Nuclear Information System (INIS)

    De Palma, A.

    1984-01-01

    3 H and 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 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- 3 H]-[24- 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 3 H/ 14 C ratio decreases in the organic layer as a function of time, due to loss of 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- 3 H] phytosterols alone are reliable substrates for the first rapid in vivo bioassay of phytosterol dealkylation

  16. Biologic effects of platelet-derived growth factor receptor α blockade in uterine cancer.

    Science.gov (United States)

    Roh, Ju-Won; Huang, Jie; Hu, Wei; Yang, XiaoYun; Jennings, Nicholas B; Sehgal, Vasudha; Sohn, Bo Hwa; Han, Hee Dong; Lee, Sun Joo; Thanapprapasr, Duangmani; Bottsford-Miller, Justin; Zand, Behrouz; Dalton, Heather J; Previs, Rebecca A; Davis, Ashley N; Matsuo, Koji; Lee, Ju-Seog; Ram, Prahlad; Coleman, Robert L; Sood, Anil K

    2014-05-15

    Platelet-derived growth factor receptor α (PDGFRα) expression is frequently observed in many kinds of cancer and is a candidate for therapeutic targeting. This preclinical study evaluated the biologic significance of PDGFRα and PDGFRα blockade (using a fully humanized monoclonal antibody, 3G3) in uterine cancer. Expression of PDGFRα was examined in uterine cancer clinical samples and cell lines, and biologic effects of PDGFRα inhibition were evaluated using in vitro (cell viability, apoptosis, and invasion) and in vivo (orthotopic) models of uterine cancer. PDGFRα was highly expressed and activated in uterine cancer samples and cell lines. Treatment with 3G3 resulted in substantial inhibition of PDGFRα phosphorylation and of downstream signaling molecules AKT and mitogen-activated protein kinase (MAPK). Cell viability and invasive potential of uterine cancer cells were also inhibited by 3G3 treatment. In orthotopic mouse models of uterine cancer, 3G3 monotherapy had significant antitumor effects in the PDGFRα-positive models (Hec-1A, Ishikawa, Spec-2) but not in the PDGFRα-negative model (OVCA432). Greater therapeutic effects were observed for 3G3 in combination with chemotherapy than for either drug alone in the PDGFRα-positive models. The antitumor effects of therapy were related to increased apoptosis and decreased proliferation and angiogenesis. These findings identify PDGFRα as an attractive target for therapeutic development in uterine cancer. ©2014 American Association for Cancer Research.

  17. Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives.

    Science.gov (United States)

    Kos, Ivan; Jadrijević-Mladar, Milena; Butula, Ivan; Biruš, Mladen; Maravić-Vlahoviček, Gordana; Dabelić, Sanja

    2013-06-01

    5 Synthesis and biological evaluation of a series (N = 16) of cyclic and acyclic hydroxyurea derivatives, including benzotriazole-, isocyanuric acid- and biuret-containing compounds, are disclosed. 1-N-(benzyloxycarbamoyl)benzotriazole was used as a benzyloxyisocyanate donor, a useful intermediate in the preparation of substituted hydroxyurea. Antibacterial activities of synthesized hydroxyurea derivatives were tested on three E. coli strains, i.e., a strain susceptible to antibiotics, a strain resistant to macrolide antibiotics and a strain resistant to aminoglycoside antibiotics. Six compounds (three acyclic and three cyclic hydroxyureas) showed growth inhibition of the tested E. coli strains, with different specificity toward each strain. Results of the cytotoxic activity evaluation revealed that twelve out of sixteen test compounds were cytotoxic to human acute monocytic leukemia THP-1 and/or human acute T cell leukemia Jurkat cell line. 1-(N-hydroxycarbamoyl) benzotriazole () increased the metabolic activity of both cell lines. Two compounds, 1-(N-hydroxycarbamoyl) benzotriazole (5) and N,N',N''-trihydroxybiuret (15), were identified as potential NO donors.

  18. NBS activities in biological reference materials

    Energy Technology Data Exchange (ETDEWEB)

    Rasberry, S.D.

    1988-12-01

    NBS activities in biological reference materials during 1986-1988 are described with a preview of plans for future certifications of reference materials. During the period, work has been completed or partially completed on about 40 reference materials of importance to health, nutrition, and environmental quality. Some of the reference materials that have been completed during the period and are described include: creatinine (SRM 914a), bovine serum albumin (SRM 927a), cholesterol in human serum (SRM's 1951-1952), aspartate aminotransferase (RM 8430), cholesterol and fat-soluble vitamins in coconut oil (SRM 1563), wheat flour (SRM 1567a), rice flour (SRM 1568a), mixed diet (RM 8431a), dinitropyrene isomers and 1-nitropyrene (SRM 1596), and complex PAH's from coal tar (SRM 1597). Oyster tissue (SRM 1566a) is being analyzed and should be available in 1988.

  19. ACTIVE AND PARTICIPATORY METHODS IN BIOLOGY: MODELING

    Directory of Open Access Journals (Sweden)

    Brînduşa-Antonela SBÎRCEA

    2011-01-01

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

  20. QSAR analysis of antitumor activities of 3,4-ethylenedioxythiphene derivatives

    Science.gov (United States)

    Rastija, Vesna; Bajić, Miroslav; Stolić, Ivana; Krstulović, Luka; Jukić, Marijana; Glavaš-Obrovac, Ljubica

    2015-12-01

    QSAR analysis was performed for the antitumor activity of 27 derivatives of 3,4-ethylenedioxythiophene against six carcinoma cell lines. The best models were obtained with surface area (SAG) in combination with lipohilicity (log P) as descriptors. Results have shown that molecules with smaller solvent accessible surface area and higher lipophilicy should have higher biological activity against carcinoma cell.

  1. Structural Diversity and Biological Activities of the Cyclodipeptides from Fungi

    Directory of Open Access Journals (Sweden)

    Xiaohan Wang

    2017-11-01

    Full Text Available Cyclodipeptides, called 2,5-diketopiperazines (2,5-DKPs, are obtained by the condensation of two amino acids. Fungi have been considered to be a rich source of novel and bioactive cyclodipeptides. This review highlights the occurrence, structures and biological activities of the fungal cyclodipeptides with the literature covered up to July 2017. A total of 635 fungal cyclodipeptides belonging to the groups of tryptophan-proline, tryptophan-tryptophan, tryptophan–Xaa, proline–Xaa, non-tryptophan–non-proline, and thio-analogs have been discussed and reviewed. They were mainly isolated from the genera of Aspergillus and Penicillium. More and more cyclodipeptides have been isolated from marine-derived and plant endophytic fungi. Some of them were screened to have cytotoxic, phytotoxic, antimicrobial, insecticidal, vasodilator, radical scavenging, antioxidant, brine shrimp lethal, antiviral, nematicidal, antituberculosis, and enzyme-inhibitory activities to show their potential applications in agriculture, medicinal, and food industry.

  2. Tomato Derived Polysaccharides for Biotechnological Applications: Chemical and Biological Approaches

    Directory of Open Access Journals (Sweden)

    Barbara Nicolaus

    2008-06-01

    Full Text Available Recent studies concerning the isolation and purification of exopolysaccharides from suspension-cultured tomato (Lycopersicon esculentum L. var. San Marzano cells and the description of a simple, rapid and low environmental impact method with for obtaining polysaccharides from solid tomato-processing industry wastes are reported. Their chemical composition, rheological properties and partial primary structure were determined on the basis of spectroscopic analyses (UV, IR, GC-MS, 1H-, 13C-NMR. Moreover, the anticytotoxic activities of exopolysaccharides obtained from cultured tomato cells were tested in a brine shrimp bioassay and the preparation of biodegradable film by chemical processing of polysaccharides from solid tomato industry waste was also reported.

  3. Synthesis, biological activities, and quantitative structure-activity relationship (QSAR) study of novel camptothecin analogues.

    Science.gov (United States)

    Wu, Dan; Zhang, Shao-Yong; Liu, Ying-Qian; Wu, Xiao-Bing; Zhu, Gao-Xiang; Zhang, Yan; Wei, Wei; Liu, Huan-Xiang; Chen, An-Liang

    2015-05-13

    In continuation of our program aimed at the development of natural product-based pesticidal agents, three series of novel camptothecin derivatives were designed, synthesized, and evaluated for their biological activities against T. Cinnabarinus, B. brassicae, and B. xylophilus. All of the derivatives showed good-to-excellent activity against three insect species tested, with LC50 values ranging from 0.00761 to 0.35496 mmol/L. Remarkably, all of the compounds were more potent than CPT against T. Cinnabarinus, and compounds 4d and 4c displayed superior activity (LC50 0.00761 mmol/L and 0.00942 mmol/L, respectively) compared with CPT (LC50 0.19719 mmol/L) against T. Cinnabarinus. Based on the observed bioactivities, preliminary structure-activity relationship (SAR) correlations were also discussed. Furthermore, a three-dimensional quantitative structure-activity relationship (3D-QSAR) model using comparative molecular field analysis (CoMFA) was built. The model gave statistically significant results with the cross-validated q2 values of 0.580 and correlation coefficient r2 of 0.991 and  of 0.993. The QSAR analysis indicated that the size of the substituents play an important in the activity of 7-modified camptothecin derivatives. These findings will pave the way for further design, structural optimization, and development of camptothecin-derived compounds as pesticidal agents.

  4. BIOLOGICALLY ACTIVE SUBSTANCES OF SPIRIT PRODUCTION WASTE

    Directory of Open Access Journals (Sweden)

    A. S. Kayshev

    2014-01-01

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

  5. New Potentially Active Pyrazinamide Derivatives Synthesized Under Microwave Conditions

    Directory of Open Access Journals (Sweden)

    Ondrej Jandourek

    2014-07-01

    Full Text Available A series of 18 N-alkyl substituted 3-aminopyrazine-2-carboxamides was prepared in this work according to previously experimentally set and proven conditions using microwave assisted synthesis methodology. This approach for the aminodehalogenation reaction was chosen due to higher yields and shorter reaction times compared to organic reactions with conventional heating. Antimycobacterial, antibacterial, antifungal and photosynthetic electron transport (PET inhibiting in vitro activities of these compounds were investigated. Experiments for the determination of lipophilicity were also performed. Only a small number of substances with alicyclic side chain showed activity against fungi which was the same or higher than standards and the biological efficacy of the compounds increased with rising lipophilicity. Nine pyrazinamide derivatives also inhibited PET in spinach chloroplasts and the IC50 values of these compounds varied in the range from 14.3 to 1590.0 μmol/L. The inhibitory activity was connected not only with the lipophilicity, but also with the presence of secondary amine fragment bounded to the pyrazine ring. Structure-activity relationships are discussed as well.

  6. Article Synthesis and Trypanocidal Activity of Novel 2,4,5-Triaryl-N-Hydroxylimidazole Derivatives

    Directory of Open Access Journals (Sweden)

    Edson Ferreira da Silva

    2013-03-01

    Full Text Available Herein, we report the design, synthesis and trypanocidal activity of some novel trisubstituted imidazole derivatives. These heterocyclic derivatives were structurally planned by exploring the concept of molecular hybridisation between two arylhydrazones derived from megazol, which has potent trypanocidal activity. The trypanocidal activity of these triarylimidazole derivatives was evaluated against infective trypomastigote forms of T. cruzi and the derivative 2'-(4-bromophenyl-1-methyl-5'-phenyl-1H,3'H-2,4'-biimidazol-3'-ol showed moderate biological activity (IC50 = 23.9 µM when compared to benznidazole, a standard trypanocidal drug. These compounds did not present cytotoxic effects at concentrations near the trypanocidal IC50, being considered a good starting point for the development of new anti-Chagas drug candidates.

  7. Biological activity of Serratia marcescens cytotoxin

    Directory of Open Access Journals (Sweden)

    G.V. Carbonell

    2003-03-01

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

  8. Activation analysis of biological materials at the Activation Analysis Centre

    International Nuclear Information System (INIS)

    Kukula, F.; Obrusnik, I.; Simkova, M.; Kucera, J.; Krivanek, M.

    1976-01-01

    A review is presented of the work of the Activation Analysis Centre of the Nuclear Research Institute for different fields of the Czechoslovak economy, aimed primarily at analyzing biological materials with the purpose of determining the contents of the so-called vital trace elements and of elements which already have a toxic effect on the organism in trace concentrations. Another important field of research is the path of trace elements from the environment to the human organism. A destructive method for the simultaneous determination of 12 trace elements in 11 kinds of human tissue has been studied. (Z.M.)

  9. Accelerating patient access to novel biologics using stable pool-derived product for non-clinical studies and single clone-derived product for clinical studies.

    Science.gov (United States)

    Munro, Trent P; Le, Kim; Le, Huong; Zhang, Li; Stevens, Jennitte; Soice, Neil; Benchaar, Sabrina A; Hong, Robert W; Goudar, Chetan T

    2017-11-01

    Cell cloning and subsequent process development activities are on the critical path directly impacting the timeline for advancement of next generation therapies to patients with unmet medical needs. The use of stable cell pools for early stage material generation and process development activities is an enabling technology to reduce timelines. To successfully use stable pools during development, it is important that bioprocess performance and requisite product quality attributes be comparable to those observed from clonally derived cell lines. To better understand the relationship between pool and clone derived cell lines, we compared data across recent first in human (FIH) programs at Amgen including both mAb and Fc-fusion modalities. We compared expression and phenotypic stability, bioprocess performance, and product quality attributes between material derived from stable pools and clonally derived cells. Overall, our results indicated the feasibility of matching bioprocess performance and product quality attributes between stable pools and subsequently derived clones. These findings support the use of stable pools to accelerate the advancement of novel biologics to the clinic. © 2017 The Authors Biotechnology Progress published by Wiley Periodicals, Inc. on behalf of American Institute of Chemical Engineers Biotechnol. Prog., 33:1476-1482, 2017. © 2017 The Authors Biotechnology Progress published by Wiley Periodicals, Inc. on behalf of American Institute of Chemical Engineers.

  10. Synthesis and Biological Evaluation of 2H-Indazole Derivatives: Towards Antimicrobial and Anti-Inflammatory Dual Agents

    Directory of Open Access Journals (Sweden)

    Jaime Pérez-Villanueva

    2017-10-01

    Full Text Available Indazole is considered a very important scaffold in medicinal chemistry. It is commonly found in compounds with diverse biological activities, e.g., antimicrobial and anti-inflammatory agents. Considering that infectious diseases are associated to an inflammatory response, we designed a set of 2H-indazole derivatives by hybridization of cyclic systems commonly found in antimicrobial and anti-inflammatory compounds. The derivatives were synthesized and tested against selected intestinal and vaginal pathogens, including the protozoa Giardia intestinalis, Entamoeba histolytica, and Trichomonas vaginalis; the bacteria Escherichia coli and Salmonella enterica serovar Typhi; and the yeasts Candida albicans and Candida glabrata. Biological evaluations revealed that synthesized compounds have antiprotozoal activity and, in most cases, are more potent than the reference drug metronidazole, e.g., compound 18 is 12.8 times more active than metronidazole against G. intestinalis. Furthermore, two 2,3-diphenyl-2H-indazole derivatives (18 and 23 showed in vitro growth inhibition against Candida albicans and Candida glabrata. In addition to their antimicrobial activity, the anti-inflammatory potential for selected compounds was evaluated in silico and in vitro against human cyclooxygenase-2 (COX-2. The results showed that compounds 18, 21, 23, and 26 display in vitro inhibitory activity against COX-2, whereas docking calculations suggest a similar binding mode as compared to rofecoxib, the crystallographic reference.

  11. New improved method for evaluation of growth by food related fungi on biologically derived materials

    DEFF Research Database (Denmark)

    Bergenholtz, Karina P.; Nielsen, Per Væggemose

    2002-01-01

    Biologically derived materials, obtained as commercial and raw materials (Polylactate (PLA), Polyhydroxybutyrate (PHB), potato, wheat and corn starch) were tested for their ability to support fungal growth using a modified ASTM G21-96 (American Society for Testing and Materials) standard as well...... as a new method where 10 mul of a spore suspension is placed in a spot on the test sample. The new method gave additional information about fungal growth on biologically derived materials, revealing a clear difference between survival and growth. PHB and PIA turned out to be most suitable for food...

  12. Protease activated receptors (PARS) mediation in gyroxin biological activity

    International Nuclear Information System (INIS)

    Silva, Jose Alberto Alves da

    2009-01-01

    Gyroxin is a serine protease enzyme from the South American rattlesnake (Crotalus durissus terrificus) venom; it is only partially characterized and has multiple activities. Gyroxin induces blood coagulation, blood pressure decrease and a neurotoxic behavior named barrel rotation. The mechanisms involved in this neurotoxic activity are not known. Whereas gyroxin is a member of enzymes with high potential to become a new drug with clinical applications such as thrombin, batroxobin, ancrod, tripsyn and kalicrein, it is important to find out how gyroxin works. The analysis on agarose gel electrophoresis and circular dichroism confirmed the molecules' integrity and purity. The gyroxin intravenous administration in mice proved its neurotoxicity (barrel rotation). In vivo studies employing intravital microscopy proved that gyroxin induces vasodilation with the participation of protease activated receptors (PARs), nitric oxide and Na+K+ATPase. The leukocytes' adherence and rolling counting indicated that gyroxin has no pro inflammatory activity. Gyroxin induced platelet aggregation, which was blocked by inhibitors of PAR1 and PAR4 receptors (SCH 79797 and tcY-NH 2 , respectively). Finally, it was proved that the gyroxin temporarily alter the permeability of the blood brain barrier (BBB). Our study has shown that both the protease-activated receptors and nitric oxide are mediators involved in the biological activities of gyroxin. (author)

  13. Biologically active extracts with kidney affections applications

    International Nuclear Information System (INIS)

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

    2015-01-01

    Highlights: • The paper highlighted the compositional similarities and differences between the three extracts of bilberry and cranberry fruit derived from the same Ericaceae family. • A method of antioxidant activity, different cellulose membranes, a Whatman filter and Langmuir – kinetic model were used. • Arbutoside presence in all three extracts of bilberry and cranberry fruit explains their use in urinary infections – cystitis and colibacillosis. • Following these research studies, it was established that the fruits of bilberry and cranberry (fruit and leaves) significantly reduce the risk of urinary infections, and work effectively to protect against free radicals and inflammation. - Abstract: 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.

  14. Biologically active extracts with kidney affections applications

    Energy Technology Data Exchange (ETDEWEB)

    Pascu, Mihaela, E-mail: mihhaela_neagu@yahoo.com [SC HOFIGAL S.A., Analytical Research Department, 2 Intr. Serelor, Bucharest-4 042124 (Romania); Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania); Pascu, Daniela-Elena [Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania); Cozea, Andreea [SC HOFIGAL S.A., Analytical Research Department, 2 Intr. Serelor, Bucharest-4 042124 (Romania); Transilvania University of Brasov, Faculty of Food and Tourism, 148 Castle Street, 500036 Brasov (Romania); Bunaciu, Andrei A. [SCIENT – Research Center for Instrumental Analysis, S.C. CROMATEC-PLUS S.R.L., 18 Sos. Cotroceni, Bucharest 060114 (Romania); Miron, Alexandra Raluca; Nechifor, Cristina Aurelia [Politehnica University of Bucharest, Faculty of Applied Chemistry and Material Science, 1-5 Polizu Street, 11061 Bucharest (Romania)

    2015-12-15

    Highlights: • The paper highlighted the compositional similarities and differences between the three extracts of bilberry and cranberry fruit derived from the same Ericaceae family. • A method of antioxidant activity, different cellulose membranes, a Whatman filter and Langmuir – kinetic model were used. • Arbutoside presence in all three extracts of bilberry and cranberry fruit explains their use in urinary infections – cystitis and colibacillosis. • Following these research studies, it was established that the fruits of bilberry and cranberry (fruit and leaves) significantly reduce the risk of urinary infections, and work effectively to protect against free radicals and inflammation. - Abstract: 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.

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

    Science.gov (United States)

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

    2012-06-01

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

  16. Radiation degradation of polysaccharides and induced biological activity

    Energy Technology Data Exchange (ETDEWEB)

    Nagasawa, Naotsugu; Yoshii, Fumio; Makuuchi Keizo; Kume Tamikazu [Japan Atomic Energy Research Inst., Takasaki, Gunma (Japan). Takasaki Radiation Chemistry Research Establishment; Mitomo, Hiroshi [Gunma Univ., Kiryu (Japan). Faculty of Engineering

    1999-09-01

    Relationship between irradiation effect of polysaccharides and induced biological activity for plants has been investigated. Sodium alginate was irradiated by gamma-rays from a Co-60 source in liquid state (aqueous solution) and in solid state (powder form). Measurement of molecular weight and analysis of UV spectra of irradiated sodium alginate have been carried out. The molecular weight was decreased by irradiation in both conditions. New absorbance peak derived from double bond or/and carbonyl group was appeared at close to 267 nm by irradiation in UV spectra. It was found that alginate having molecular weight about 10,000 is most suitable to used as growth promoter in plants. To obtain the molecular weight of 10,000 by irradiation, the necessary doses are 100 kGy in liquid state and 500 kGy in solid state, respectively. (author)

  17. Changes in soluble factor-mediated CD8+ cell-derived antiviral activity in cynomolgus macaques infected with simian immunodeficiency virus SIVmac251: relationship to biological markers of progression.

    Science.gov (United States)

    Dioszeghy, Vincent; Benlhassan-Chahour, Kadija; Delache, Benoit; Dereuddre-Bosquet, Nathalie; Aubenque, Celine; Gras, Gabriel; Le Grand, Roger; Vaslin, Bruno

    2006-01-01

    Cross-sectional studies have shown that the capacity of CD8+ cells from human immunodeficiency virus (HIV)-infected patients and simian immunodeficiency virus (SIV) SIVmac-infected macaques to suppress the replication of human and simian immunodeficiency viruses in vitro depends on the clinical stage of disease, but little is known about changes in this antiviral activity over time in individual HIV-infected patients or SIV-infected macaques. We assessed changes in the soluble factor-mediated noncytolytic antiviral activity of CD8+ cells over time in eight cynomolgus macaques infected with SIVmac251 to determine the pathophysiological role of this activity. CD8+ cell-associated antiviral activity increased rapidly in the first week after viral inoculation and remained detectable during the early phase of infection. The net increase in antiviral activity of CD8+ cells was correlated with plasma viral load throughout the 15 months of follow-up. CD8+ cells gradually lost their antiviral activity over time and acquired virus replication-enhancing capacity. Levels of antiviral activity correlated with CD4+ T-cell counts after viral set point. Concentrations of beta-chemokines and interleukin-16 in CD8+ cell supernatants were not correlated with this antiviral activity, and alpha-defensins were not detected. The soluble factor-mediated antiviral activity of CD8+ cells was neither cytolytic nor restricted to major histocompatibility complex. This longitudinal study strongly suggests that the increase in noncytolytic antiviral activity from baseline and the maintenance of this increase over time in cynomolgus macaques depend on both viral replication and CD4+ T cells.

  18. Changes in Soluble Factor-Mediated CD8+ Cell-Derived Antiviral Activity in Cynomolgus Macaques Infected with Simian Immunodeficiency Virus SIVmac251: Relationship to Biological Markers of Progression†

    Science.gov (United States)

    Dioszeghy, Vincent; Benlhassan-Chahour, Kadija; Delache, Benoit; Dereuddre-Bosquet, Nathalie; Aubenque, Celine; Gras, Gabriel; Le Grand, Roger; Vaslin, Bruno

    2006-01-01

    Cross-sectional studies have shown that the capacity of CD8+ cells from human immunodeficiency virus (HIV)-infected patients and simian immunodeficiency virus (SIV) SIVmac-infected macaques to suppress the replication of human and simian immunodeficiency viruses in vitro depends on the clinical stage of disease, but little is known about changes in this antiviral activity over time in individual HIV-infected patients or SIV-infected macaques. We assessed changes in the soluble factor-mediated noncytolytic antiviral activity of CD8+ cells over time in eight cynomolgus macaques infected with SIVmac251 to determine the pathophysiological role of this activity. CD8+ cell-associated antiviral activity increased rapidly in the first week after viral inoculation and remained detectable during the early phase of infection. The net increase in antiviral activity of CD8+ cells was correlated with plasma viral load throughout the 15 months of follow-up. CD8+ cells gradually lost their antiviral activity over time and acquired virus replication-enhancing capacity. Levels of antiviral activity correlated with CD4+ T-cell counts after viral set point. Concentrations of β-chemokines and interleukin-16 in CD8+ cell supernatants were not correlated with this antiviral activity, and α-defensins were not detected. The soluble factor-mediated antiviral activity of CD8+ cells was neither cytolytic nor restricted to major histocompatibility complex. This longitudinal study strongly suggests that the increase in noncytolytic antiviral activity from baseline and the maintenance of this increase over time in cynomolgus macaques depend on both viral replication and CD4+ T cells. PMID:16352548

  19. Antifungal activity of naphthothiazoles derived from Lawsone ...

    African Journals Online (AJOL)

    A series of Naphtho [2,3-d] thiazole-4, 9-diones was prepared by the condensation of bromolawsone with thiosemicarbazones derived from the aldehydes and ketones in dry dimethyl formamide (DMF). The products are also obtained by the cyclization of the intermediate 2-chlorobenzaldehyde thiosemicarbazone of 1 ...

  20. Office of Biological Informatics and Outreach geospatial technology activities

    Science.gov (United States)

    ,

    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.

  1. Design, Synthesis, and Biological Evaluation of Vanillin Hydroxamic Acid Derivatives as Novel Peptide Deformylase Inhibitors.

    Science.gov (United States)

    Gao, Jian; Qiu, Shengzhi; Liang, Li; Hao, Zhixiang; Zhou, Qianqian; Wang, Fanfan; Mou, Jie; Lin, Qisi

    2018-01-01

    Infectious disease is increasingly hampering human health, which challenge the discovery of new antibacterial target. Peptide deformylase (PDF), a metalloenzyme responsible for catalyzing the removal of the N-formyl group from nascent proteins, was considered as an important target in antibacterial drug discovery. Reported here are the design, synthesis and biological evaluation of vanillin hydroxamic acid derivatives. Analysis of the structure-activity relationships lead to the discovery of compound 8, which exhibits promising antibacterial activity against Escherichia coli, Staphylococcus aureus, Aspergillus oryzae, and Aspergillus foetidus with the MIC value of 0.32 µg/ml, 0.32 µg/ml, 0.16 µg/ml and 0.16 µg/ml, respectively. Furthermore, molecular docking study was applied to elucidate binding interaction between compound 8 and PDF, which indicate that compound 8 not only shares the same binding pocket with actinonin, but also has a similar binding pattern. In silico pharmacokinetic and toxicity prediction studies also suggested that compound 8 has a relatively high drug score of 0.80, and has no risk of toxicity. Compound 8 might represent a promising scaffold for the further development of novel antibacterial drugs. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  2. Derivation and computation of discrete-delay and continuous-delay SDEs in mathematical biology.

    Science.gov (United States)

    Allen, Edward J

    2014-06-01

    Stochastic versions of several discrete-delay and continuous-delay differential equations, useful in mathematical biology, are derived from basic principles carefully taking into account the demographic, environmental, or physiological randomness in the dynamic processes. In particular, stochastic delay differential equation (SDDE) models are derived and studied for Nicholson's blowflies equation, Hutchinson's equation, an SIS epidemic model with delay, bacteria/phage dynamics, and glucose/insulin levels. Computational methods for approximating the SDDE models are described. Comparisons between computational solutions of the SDDEs and independently formulated Monte Carlo calculations support the accuracy of the derivations and of the computational methods.

  3. Molluscicidal activity of synthetic lapachol amino and hydrogenated derivatives.

    Science.gov (United States)

    Silva, Tania M S; Camara, Celso A; Barbosa, Ticiano P; Soares, André Z; da Cunha, Luciana C; Pinto, Angelo C; Vargas, Maria D

    2005-01-03

    A series of new amino derivatives and a new partially hydrogenated derivative of the natural naphthoquinone lapachol were assayed for molluscicidal activity against Biomphalaria glabrata. These derivatives showed low to medium LC(50) values, and a 3.1 microg/mL value for the most potent derivative of the series. The toxicity is in agreement with the decrease of polar character of the tested compounds.

  4. Synthesis, biological investigation, calf thymus DNA binding and docking studies of the sulfonyl hydrazides and their derivatives

    Science.gov (United States)

    Murtaza, Shahzad; Shamim, Saima; Kousar, Naghmana; Tahir, Muhammad Nawaz; Sirajuddin, Muhammad; Rana, Usman Ali

    2016-03-01

    The present study describes the syntheses and biological investigations of sulfonyl hydrazides and their novel derivatives. The detailed investigations involved the characterization of the newly synthesized compounds using FTIR, NMR, mass spectrometry and by single crystal X-Ray diffraction (XRD) analysis techniques. The binding tendencies of these compounds with CT-DNA (calf thymus DNA) have been explored by electronic absorption (UV) spectroscopy and viscosity measurement. The binding constant (K) and Gibb's free energy (ΔG) values were also calculated accordingly. In addition, we also investigated the biological activities such as antioxidant, antibacterial, enzyme inhibition and DNA interactions. The antioxidant activity was assayed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity, while antibacterial activity was investigated against four bacterial strains (viz. Escherichia coli, Crynibacteria bovius, Staphylococcus auras and Bacillus antherasis) by employing the common disc diffusion method. Enzyme inhibition activity of the synthesized compounds was examined against butyrylcholinestrase. The results of enzyme inhibition activity and the DNA binding interaction studies were also collected through molecular docking program using computational analysis. Our study reveals that the newly synthesized compounds possess moderate to good biological activities.

  5. New improved method for evaluation of growth by food related fungi on biologically derived materials

    DEFF Research Database (Denmark)

    Bergenholtz, Karina P.; Nielsen, Per Væggemose

    2002-01-01

    Biologically derived materials, obtained as commercial and raw materials (Polylactate (PLA), Polyhydroxybutyrate (PHB), potato, wheat and corn starch) were tested for their ability to support fungal growth using a modified ASTM G21-96 (American Society for Testing and Materials) standard as well...

  6. OTC Derivatives and Global Economic Activity: An Empirical Analysis

    Directory of Open Access Journals (Sweden)

    Gordon Bodnar

    2017-06-01

    Full Text Available That the global market for derivatives has expanded beyond recognition is well known. What is not know is how this market interacts with economic activity. We provide the first empirical characterization of interdependencies between OECD economic activity and the global OTC derivatives market. To this end, we apply a vector-error correction model to OTC derivatives disaggregated across instruments and counterparties. The results indicate that with one exception, the heterogeneity of OTC contracts is too pronounced to be reliably summarized by our measures of economic activity. The one exception is interest-rate derivatives held by Other Financial Institutions.

  7. Unambiguous Synthesis and Prophylactic Antimalarial Activities of Imidazolidinedione Derivatives

    National Research Council Canada - National Science Library

    Zhang, Quan; Guan, Jian; Sacci, John; Ager, Arba; Ellis, William; Mihlhous, Wilbur; Kyle, Dennis; Lin, Ai J

    2005-01-01

    .... To search for compounds with good oral efficacy, a series of carbamate derivatives of the active components were prepared by the new procedure, many of which showed profound causal prophylactic antimalarial activity against Plasmodium yoelil in mouse by oral administration.

  8. Synthesis, chemical and biological properties of the new mono- and bis-derivatives of imidazoles

    Directory of Open Access Journals (Sweden)

    E. V. Welchinska

    2014-12-01

    Full Text Available The aim of research. The problem of finding effective antitumour medical preparation with low toxicity is an important issue of medical and pharmaceutical chemistry. Knowledge of cancer cell features and its metabolism enables to predict the direction of chemical and biological research, to conduct a targeted synthesis of potential drugs, and to assess their applicability in oncological practice as antitumor agents. The purpose of work is to explain preformed heterocycles as purines, its synthesis and investigation of chemical and biological properties. After construction of the potential active structures we proposed the new method of original derivatives synthesis which are received on the base of imidazole, from one side, and fluorocontaining common anesthetic halothane (2-bromo-1,1,1-trifluoro-2-chloroethane from other side. Molecular complex of more perspective biologically active bis-imidazole with antitumour bacterial lectine has been received. With the purpose to synthesize potential antitumour compounds on the base of halothane and imidazole, new convenient methods for the preparation of original heterocyclic derivatives of imidazole have been described. The structure and composition of synthesized compound has been confirmed by the methods of elemental analysis, IR- and NMRІН-spectra. Materials and methods. The majority of the absolute organic solvents (benzene, dimethylformamide, ethyl ester employed in the present studies were distilled before their use. Organic solvents were dried over anhydrous magnesium sulfate or metallic sodium. Gas-liquid chromatography was carried out by Perkin Elmer chromatograph with UV-detector ("Perkin", Germany. IR spectra were recorded in a UR-20 spectrometer ("Charles Ceise Hena", Germany. The 1HNMR spectra were recorded in DMSO-d6 on a 200 MHz BrakerWP-200 ("Braker", Switzerland or Varian T-60 spectrometer ("Varian", USA. Investigation of critical toxicity of new compounds was carried out at

  9. Antitumor activity of 3,4-ethylenedioxythiophene derivatives and quantitative structure-activity relationship analysis

    Science.gov (United States)

    Jukić, Marijana; Rastija, Vesna; Opačak-Bernardi, Teuta; Stolić, Ivana; Krstulović, Luka; Bajić, Miroslav; Glavaš-Obrovac, Ljubica

    2017-04-01

    The aim of this study was to evaluate nine newly synthesized amidine derivatives of 3,4- ethylenedioxythiophene (3,4-EDOT) for their cytotoxic activity against a panel of human cancer cell lines and to perform a quantitative structure-activity relationship (QSAR) analysis for the antitumor activity of a total of 27 3,4-ethylenedioxythiophene derivatives. Induction of apoptosis was investigated on the selected compounds, along with delivery options for the optimization of activity. The best obtained QSAR models include the following group of descriptors: BCUT, WHIM, 2D autocorrelations, 3D-MoRSE, GETAWAY descriptors, 2D frequency fingerprint and information indices. Obtained QSAR models should be relieved in elucidation of important physicochemical and structural requirements for this biological activity. Highly potent molecules have a symmetrical arrangement of substituents along the x axis, high frequency of distance between N and O atoms at topological distance 9, as well as between C and N atoms at topological distance 10, and more C atoms located at topological distances 6 and 3. Based on the conclusion given in the QSAR analysis, a new compound with possible great activity was proposed.

  10. Incorporation of poly-saccharidic derivatives in model biological systems: monolayers, lamellar phases and vesicles

    International Nuclear Information System (INIS)

    Deme, Bruno

    1995-01-01

    Our aim is to introduce a soluble polymer in a lyotropic lamellar phase, and to modify the force balance in the case of a collapsed system where no repulsive contribution overcomes the van der Waals attraction, except at very short distances where hydration forces dominate (i.e. a collapsed stack of membranes). Mixed layers of a synthetic lecithin (DMPC) and a hydrophobically modified polysaccharide (cholesteryl-pullulan, CHP) have been investigated at the air-water interface by surface tension experiments and by specular reflection of neutrons. The DMPC/CHP/water ternary phase diagram has been determined by small angle X-ray scattering (SAXS) and small angle neutron scattering (SANS). CHP derivatives are associative polymers bearing lateral cholesterol groups that interact with a polar phases such as phospholipid monolayers and biological membranes. These derivatives are surface active and self-aggregate in solution leading to the formation of soluble micellar type aggregates. The interaction of CHP derivatives with lipidic structures involves the anchoring of the cholesterol groups that yields to the tethering of the poly-saccharidic backbones at lipid/water interfaces. These poly-saccharidic backbones are flexible chains in good solvent in water. Using these derivatives and a new preparation procedure, we show that it is possible to avoid the depletion of the polysaccharide due to its steric exclusion by the collapsed DMPC lamellar phase. We are able to prepare samples at thermodynamic equilibrium with the polysaccharide solubilized in the lamellar phase, a situation opposed to the well known behavior of mixed polysaccharide/lecithin Systems commonly used in osmotic stress experiments. Here, the osmotic pressure of the chains confined in the lamellar lattice acts as a new long range repulsive contribution in the DMPC lyotropic L α phase and results in the swelling of the lamellar phase at large membrane separations (570 A). Such bilayer separations allow out of

  11. [Antidiuretic activity of dithiocarbamic acid derivatives].

    Science.gov (United States)

    Korablec, M V; Evets, M A

    1977-01-01

    Chemically pure dithiocarbamates, thiuramsulphides and ethylene-bis-dithiocarbamates display a well-marked antidiuretic action. They materially reduce diuresis, natri- and kaliuresis in rats (1/5 LD(50) per 1 kg into the stomach) and in dogs (sodium N, N-diethyl-dithiocarbamate-into renal artery). Without changing the tubular reabsorption DEDTC inhibits the glomerular filtration of the dogs' kidneys. Furosemide (lasix) prevents the development of the an antidiuletic anidiuretic effect and reduction of the sodium and potassium excretion provoked in rats with DEDTC, zinc N, N', N"-tetraethylthiuram-disulphide and ethylene-bis-dithiocarbamate. Furosemide is recommended for the treatment of acute poisonings with dithiocarbaminic acid derivatives.

  12. Instrumental neutron activation analysis of biological samples

    International Nuclear Information System (INIS)

    Guinn, V.P.; Gavrilas, M.

    1990-01-01

    The elemental compositions of 18 biological reference materials have been processed, for 14 stepped combinations of irradiation/decay/counting times, by the INAA Advance Prediction Computer Program. The 18 materials studied include 11 plant materials, 5 animal materials, and 2 other biological materials. Of these 18 materials, 14 are NBS Standard Reference Materials and four are IAEA reference materials. Overall, the results show that a mean of 52% of the input elements can be determined to a relative standard deviation of ±10% or better by reactor flux (thermal plus epithermal) INAA

  13. Dew formation and activity of biological crusts

    NARCIS (Netherlands)

    Veste, M.; Heusinkveld, B.G.; Berkowicz, S.M.; Breckle, S.W.; Littmann, T.; Jacobs, A.F.G.

    2008-01-01

    Biological soil crusts are prominent in many drylands and can be found in diverse parts of the globe including the Atacama desert, Chile, the Namib desert, Namibia, the Succulent-Karoo desert, South Africa, and the Negev desert, Israel. Because precipitation can be negligible in deserts ¿ the

  14. Biological activities of synthesized silver nanoparticles from ...

    Indian Academy of Sciences (India)

    Nanotechnology is interdisciplinary which includes physics, chemistry, biology, material science and medicine. Nanotechnology is a universal term for the creation, manip ... range of medical devices including bone cement, surgical instruments, surgical masks, etc. Synthesis of noble metal na- noparticles, in particular, silver ...

  15. Synthesis, radiosynthesis and biological evaluation of 1, 4-dihydroquinoline derivatives as new carriers for specific brain delivery

    Energy Technology Data Exchange (ETDEWEB)

    Foucout, L.; Bohn, P.; Dupas, G.; Marsais, F.; Levacher, V. [Laboratoire de Chimie Organique Fine et Heterocyclique, UMR 6014, IRCOF, CNRS, Universite et INSA de Rouen, B.P. 08 F-76131, Mont- Saint-Aignan Cedex (France); Gourand, F.; Dhilly, M.; Barre, L. [Groupe de Developpements Methodologiques en Tomographie par Emission de Positons, CEA/DSV/I2BM/CI-NAPS UMR6232, Universite de Caen Basse Normandie, Caen (France); Bohn, P.; Costentin, J. [Laboratoire de Neuropharmacologie Experimentale associe au CNRS, FRE-2735, Faculte de Medecine et de pharmacie, Universite de Rouen, F-76000 (France); Abbas, A. [Inserm-EPHE-Universite de Caen Basse-Normandie, Unite U923, GIP Cyceron, CHU Cote de Nacre, Caen (France)

    2009-07-01

    In spite of numerous reports dealing with the use of 1, 4-dihydro-pyridines as carriers to deliver biological active compounds to the brain, this chemical delivery system (CDS) suffers from poor stability of the 1, 4-dihydropyridine derivatives towards oxidation and hydration reactions seriously limiting further investigations in vivo. In an attempt to overcome these limitations, we report herein the first biological evaluation of more stable annellated NADH models in the quinoline series as relevant neuro-active drug-carrier candidates. The radiolabeled 1, 4-dihydroquinoline [{sup 11}C]1a was prepared to be subsequently peripherally injected in rats. The injected animals were sacrificed and brains were collected. The radioactivity measured in rat brain indicated a rapid penetration of the carrier [{sup 11}C]1a into the CNS. HPLC analysis of brain homogenates showed that oxidation of [{sup 11}C]1a into the corresponding quinolinium salt [{sup 11}C]4a was completed in less than 5 min. An in vivo evaluation in mice is also reported to illustrate the potential of such 1, 4-dihydroquinoline derivatives to transport a neuro-active drug in the CNS. For this purpose, g-aminobutyric acid (GABA), well known to poorly cross the brain blood barrier (BBB) was connected to this 1, 4-dihydroquinoline-type carrier. After i.p. injection of 1, 4-dihydroquinoline-GABA derivative 1b in mice, a significant alteration of locomotor activity (LMA) was observed presumably resulting from an enhancement of central GABAergic activity. These encouraging results give strong evidence for the capacity of carrier-GABA derivative 1b to cross the BBB and exert a pharmacological effect on the CNS. This study paves the way for further progress in designing new redox chemical delivery systems. (authors)

  16. Engineering catalyst microenvironments for metal-catalyzed hydrogenation of biologically derived platform chemicals.

    Science.gov (United States)

    Schwartz, Thomas J; Johnson, Robert L; Cardenas, Javier; Okerlund, Adam; Da Silva, Nancy A; Schmidt-Rohr, Klaus; Dumesic, James A

    2014-11-17

    It is shown that microenvironments formed around catalytically active sites mitigate catalyst deactivation by biogenic impurities that are present during the production of biorenewable chemicals from biologically derived species. Palladium and ruthenium catalysts are inhibited by the presence of sulfur-containing amino acids; however, these supported metal catalysts are stabilized by overcoating with poly(vinyl alcohol) (PVA), which creates a microenvironment unfavorable for biogenic impurities. Moreover, deactivation of Pd catalysts by carbon deposition from the decomposition of highly reactive species is suppressed by the formation of bimetallic PdAu nanoparticles. Thus, a PVA-overcoated PdAu catalyst was an order of magnitude more stable than a simple Pd catalyst in the hydrogenation of triacetic acid lactone, which is the first step in the production of biobased sorbic acid. A PVA-overcoated Ru catalyst showed a similar improvement in stability during lactic acid hydrogenation to propylene glycol in the presence of methionine. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  17. SYNTHESIS, CHARACTERIZATION OF BIOLOGICALLY ACTIVE N ...

    African Journals Online (AJOL)

    DR. AMINU

    2013-12-02

    Dec 2, 2013 ... assigned to v(Co-N) and v(Co-O) stretching vibrations confirming the coordination of the Schiff ... and histidine and its complex compounds with divalent ... derived from acetylacetone and amino acids and their cobalt(II), copper(II), nickel(II), and zinc(II) complexes. The schiff bases and their complexes are.

  18. Egg yolk proteins and peptides with biological activity

    Directory of Open Access Journals (Sweden)

    Aleksandra Zambrowicz

    2014-12-01

    Full Text Available Many proteins of food reveal biological activity. In the sequence of these proteins also numerous biologically active peptides are encrypted. These peptides are released during proteolysis naturally occurring in the gastrointestinal tract, food fermentation or during designed enzymatic hydrolysis in vitro. Biopeptides may exert multiple activities, affecting the cardiovascular, endocrine, nervous and immune systems. An especially rich source of bioactive proteins and biopeptides is egg. Bioactive peptides released from egg white proteins have been well described, whereas egg yolk proteins as precursors of biopeptides are less well characterized. This manuscript describes biologically active proteins and peptides originating from egg yolk and presents their potential therapeutic role.

  19. Galloylation of polyphenols alters their biological activity

    Czech Academy of Sciences Publication Activity Database

    Karas, D.; Ulrichová, J.; Valentová, Kateřina

    2017-01-01

    Roč. 105, JUL 2017 (2017), s. 223-240 ISSN 0278-6915 R&D Projects: GA MŠk(CZ) LD15082; GA MŠk(CZ) LD15084; GA MŠk(CZ) LO1304 Grant - others:GA ČR(CZ) GAP303/12/G163 Program:GA Institutional support: RVO:61388971 Keywords : Polyphenols * Gallic acid * Galloylation Subject RIV: CE - Biochemistry OBOR OECD: Biochemistry and molecular biology Impact factor: 3.778, year: 2016

  20. Synthesis, antiproliferative activity and molecular docking of Colchicine derivatives.

    Science.gov (United States)

    Huczyński, Adam; Majcher, Urszula; Maj, Ewa; Wietrzyk, Joanna; Janczak, Jan; Moshari, Mahshad; Tuszynski, Jack A; Bartl, Franz

    2016-02-01

    In order to create more potent anticancer agents, a series of five structurally different derivatives of Colchicine have been synthesised. These compounds were characterised spectroscopically and structurally and their antiproliferative activity against four human tumour cell lines (HL-60, HL-60/vinc, LoVo, LoVo/DX) was evaluated. Additionally the activity of the studied compounds was calculated using computational methods involving molecular docking of the Colchicine derivatives to β-tubulin. The experimental and computational results are in very good agreement indicating that the antimitotic activity of Colchicine derivatives can be readily predicted using computational modeling methods. Crown Copyright © 2016. Published by Elsevier Inc. All rights reserved.

  1. Quantitative structure activity relationship of benzoxazinone derivatives as neuropeptide Y Y5 receptor antagonists.

    Science.gov (United States)

    Deswal, S; Roy, N

    2006-04-01

    Quantitative structure activity relationship (QSAR) has been established for 30 benzoxazinone derivatives acting as neuropeptide Y Y5 receptor antagonists. The genetic algorithm and multiple linear regression were used to generate the relationship between biological activity and calculated descriptors. Model with good statistical qualities was developed using four descriptors from topological, thermodynamic, spatial and electrotopological class. The validation of the model was done by cross validation, randomization and external test set prediction.

  2. Chemically and biologically-mediated fertilizing value of manure-derived biochar.

    Science.gov (United States)

    Subedi, R; Taupe, N; Ikoyi, I; Bertora, C; Zavattaro, L; Schmalenberger, A; Leahy, J J; Grignani, C

    2016-04-15

    This study evaluates the potential of manure-derived biochars in promoting plant growth and enhancing soil chemical and biological properties during a 150day pot experiment. Biochars from pyrolysis of poultry litter (PL) and swine manure (SM) at 400 and 600°C, and a commonly available wood chip (WC) biochar produced at high temperature (1000°C) were incorporated to silt-loam (SL) and sandy (SY) soils on a 2% dry soil weight basis. Ryegrass was sown and moisture was adjusted to 60% water filled pore space (WFPS). The PL400 and SM400 biochars significantly increased (psoil) and enhanced nitrogen (N), phosphorus (P) and potassium (K) uptake by the plants in both soils, compared to the Control. All biochars significantly increased the soil carbon (C) contents compared to the Control. Total N contents were significantly greater for PL400 and PL600 treatments in both soils. The dehydrogenase activity (DA) significantly increased for PL400 and SM400 treatments and was positively correlated with the volatile matter (VM) contents of the biochars, while β-glucosidase activity (GA) decreased for the same treatments in both soils. All biochars significantly shifted (p≤0.05) the bacterial community structure compared to the Control. This study suggests that pyrolysis of animal manures can produce a biochar that acts as both soil amendment and an organic fertilizer as proven by increased NPK uptake, positive liming effect and high soil nutrient availability, while WC biochar could work only in combination with fertilizers (organic as well as mineral). Copyright © 2016 Elsevier B.V. All rights reserved.

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

    Science.gov (United States)

    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

  4. Adsorption of heavy metals by agroforestry waste derived activated ...

    African Journals Online (AJOL)

    Adsorption of heavy metals by agroforestry waste derived activated carbons applied to aqueous solutions. Jane M Misihairabgwi, Abisha Kasiyamhuru, Peter Anderson, Colin J Cunningham, Tanya A Peshkur, Ignatious Ncube ...

  5. Synthesis, characterization and antibacterial activity of new fluorescent chitosan derivatives

    Czech Academy of Sciences Publication Activity Database

    Přichystalová, H.; Almonasy, N.; Abdel-Mohsen, A. M.; Abdel-Rahman, R. M.; Fouda, M. M. G.; Vojtova, L.; Kobera, Libor; Spotz, Z.; Burgert, L.; Jancar, J.

    2014-01-01

    Roč. 65, April (2014), s. 234-240 ISSN 0141-8130 Institutional support: RVO:61389013 Keywords : chitosan derivatives * fluorescence * antibacterial activity Subject RIV: CD - Macromolecular Chemistry Impact factor: 2.858, year: 2014

  6. Biological activities of Croton palanostigma Klotzsch.

    Science.gov (United States)

    Mota, Eduardo Ferreira; Rosario, Diele Magno; Silva Veiga, Andreza Socorro; Barros Brasil, Davi Do Socorro; Silveira, Fernando Tobias; Dolabela, Maria Fâni

    2016-01-01

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

  7. Synthesis and Antimicrobial Activity of Amino Acids Conjugated Diphenylmethylpiperazine Derivatives

    Directory of Open Access Journals (Sweden)

    K. N. Shivakumara

    2009-01-01

    Full Text Available A series of amino acid conjugated diphenylmethylpiperazine derivatives were synthesized by coupling diphenylmethylpiperazine with different Boc-amino acids using EDCI/HOBt as coupling agent and NMM as base. The synthesized compounds were characterized by 1H-NMR and elemental analysis. The Boc-deblocked derivatives were tested for their antimicrobial activity. We are here reporting that Phe and Trp conjugated diphenylmethylpiperazine showed equally good antibacterial activities as that of conventional antimicrobial drugs.

  8. Trypanosoma cruzi: activities of lapachol and alpha- and beta-lapachone derivatives against epimastigote and trypomastigote forms.

    Science.gov (United States)

    Salas, Cristian; Tapia, Ricardo A; Ciudad, Karina; Armstrong, Verónica; Orellana, Myriam; Kemmerling, Ulrike; Ferreira, Jorge; Maya, Juan Diego; Morello, Antonio

    2008-01-15

    Derivatives of natural quinones with biological activities, such as lapachol, alpha- and beta-lapachones, have been synthesized and their trypanocidal activity evaluated in vitro in Trypanosoma cruzi cells. All tested compounds inhibited epimastigote growth and trypomastigote viability. Several compounds showed similar or higher activity as compared with current trypanocidal drugs, nifurtimox and benznidazole. The results presented here show that the anti-T. cruzi activity of the alpha-lapachone derivatives can be increased by the replacement of the benzene ring by a pyridine moiety. Free radical production and consequently oxidative stress through redox cycling or production of electrophilic metabolites are the potential biological mechanism of action for these synthetic quinones.

  9. Synthesis, spectroscopic and biological studies of transition metal complexes of novel schiff bases derived from amoxicillin and sugars

    International Nuclear Information System (INIS)

    Naz, N.

    2009-01-01

    Fe (II), Co (II) and Ni (II) metal complexes of new Schiff bases derived from amoxicillin with sugars (D-Glucose, D-Galactose and D-Mannose) have been synthesized and characterized by elemental analysis, FTIR, electronic absorption, and atomic absorption spectroscopy, magnetic moment measurements and thermal analysis. It has been found that Schiff bases behave as bi-dentate ligands forming complexes with 1:2 (metal:ligand) stoichiometry. The complexes were neutral as confirmed by their low conductance values. The biological applications of complexes have been studied on two gram negative (Escherichia coli and Pseudomonas aeruginosa) and two gram positive (Bacillus subtilis and Staphylococcus aureus) microorganisms by Agar diffusion disc method. It has been found that all the complexes have higher biological activities than the pure amoxicillin. (author)

  10. Biological activities of Castela coccinea Griseb. extracts

    OpenAIRE

    Campagna, María Noel; Ratti, María Soledad; Sciara, Mariela; García Vescovi, Eleonora; Gattuso, Martha; Martínez, María Laura

    2011-01-01

    Infusions of leaf and bark of Castela coccinea Griseb. (Simaroubaceae) were traditionally used against dysentery. In this work, anti-bacterial and antioxidant activity were studied in C. coccinea extracts. The higest DPPH scavenging activity was detected in ethanolic leaf extracts with an IC50= 0.015 mg/ml. Bark ethanolic extracts showed inhibition of lipoperoxidation and free radical scavenging. However, a previous work evidenced that this extract is toxic at a concentration needed ...

  11. Baltic cyanobacteria- A source of biologically active compounds

    Digital Repository Service at National Institute of Oceanography (India)

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

    Cyanobacteria are effective producers of bioactive metabolites, including both acute toxins and potential pharmaceuticals. In the current work, the biological activity of 27 strains of Baltic cyanobacteria representing different taxonomic groups...

  12. Biologically active substances from Zanthoxylum capense(thumb.) Harv.

    CSIR Research Space (South Africa)

    Steyn, PS

    1998-08-01

    Full Text Available A chemical investigation into the composition of Zanthoxylum capense yielded several biologically active compounds, including pellitorine. A convenient HPLC method was developed to determine the presence of pellitorine in crude extracts from plants...

  13. Synthesis and Anti-Tumor Activity of Novel Aminomethylated Derivatives of Isoliquiritigenin

    Directory of Open Access Journals (Sweden)

    Haoran Fu

    2014-10-01

    Full Text Available A series of new aminomethylated derivatives of isoliquiritigenin was synthesized. The structures of the compounds were confirmed by IR, MS, NMR, 13C-NMR and elemental analyses. Cytotoxic activities of these derivatives towards the human prostatic cell line PC-3, human mammary cancer cell line MCF-7 and human oophoroma cell line HO-8910 in vitro were tested. The IC50 values showed cytotoxic activities of some of these new derivatives were relatively strong. Furthermore, tumor growth inhibition in vivo of aminomethylated derivatives of isoliquiritigenin 15 was superior to that of isoliquritigenin and reached inhibition rates of 71.68%. The detailed synthesis, spectroscopic data, biological and pharmacologicalactivities of the synthesized compounds were provided.

  14. Physical activity and biological maturation: a systematic review

    Directory of Open Access Journals (Sweden)

    Eliane Denise Araújo Bacil

    2015-03-01

    Full Text Available OBJECTIVE: To analyze the association between physical activity (PA and biological maturation in children and adolescents. DATA SOURCE: We performed a systematic review in April 2013 in the electronic databases of PubMed/MEDLINE, SportDiscus, Web of Science and LILACS without time restrictions. A total of 628 potentially relevant articles were identified and 10 met the inclusion criteria for this review: cross-sectional or longitudinal studies, published in Portuguese, English or Spanish, with schoolchildren aged 9-15 years old of both genders. DATA SYNTHESIS: Despite the heterogeneity of the studies, there was an inverse association between PA and biological maturation. PA decreases with increased biological and chronological age in both genders. Boys tend to be more physically active than girls; however, when controlling for biological age, the gender differences disappear. The association between PA and timing of maturation varies between the genders. Variation in the timing of biological maturation affects the tracking of PA in early adolescent girls. This review suggests that mediators (BMI, depression, low self-esteem, and concerns about body weight can explain the association between PA and biological maturation. CONCLUSIONS: There is an association between PA and biological maturation. PA decreases with increasing biological age with no differences between genders. As for the timing of biological maturation, this association varies between genders.

  15. Biological activity of Herissantia crispa (L. Brizicky

    Directory of Open Access Journals (Sweden)

    Igara Oliveira Lima

    Full Text Available The crude methanol extract (EMeOH of the aerial parts of Herissantia crispa (L. Brizicky, plant riches in flavonoids and without pharmacological studies, was tested to value its activity under the behaviour parameters and to determine the lethal dose (LD50 in mice; antimicrobial and antiulcerogenic activities. The EMeOH (5,000 mg/kg, v.o. or 2,000 mg/kg i.p. did not alter the behaviour parameters and there were not mice deaths. The extract inhibited the bacterial growth. The EMeOH (750 mg/kg showed anti-diarroeal activity. The EMeOH (250, 500 and 750 mg/kg decreased the gastric lesions induced by 0.3 M HCl/ethanol 60% in mice. In conclusion, the EMeOH presents anti-ulcerogenic activity;, however it is necessary to value the antiulcerogenic activity in more specific models and to study the action mechanism by which the vegetable sample protects the gastric mucosa.

  16. Controlled Release of Biologically Active Silver from Nanosilver Surfaces

    OpenAIRE

    Liu, Jingyu; Sonshine, David A.; Shervani, Saira; Hurt, Robert H.

    2010-01-01

    Major pathways in the antibacterial activity and eukaryotic toxicity of nano-silver involve the silver cation and its soluble complexes, which are well established thiol toxicants. Through these pathways, nano-silver behaves in analogy to a drug delivery system, in which the particle contains a concentrated inventory of an active species, the ion, which is transported to and released near biological target sites. Although the importance of silver ion in the biological response to nano-silver ...

  17. Activated Sludge. Student Manual. Biological Treatment Process Control.

    Science.gov (United States)

    Boe, Owen K.; Klopping, Paul H.

    This student manual contains the textual material for a seven-lesson unit on activated sludge. Topic areas addressed in the lessons include: (1) activated sludge concepts and components (including aeration tanks, aeration systems, clarifiers, and sludge pumping systems); (2) activated sludge variations and modes; (3) biological nature of activated…

  18. Synthesis and enhanced neuroprotective activity of C60-based ebselen derivatives

    International Nuclear Information System (INIS)

    Liu, X.-F.; Guan, W.-C.; Ke, W.-S.

    2007-01-01

    A C 60 -based ebselen derivative 4 was synthesized through the cycloaddition of C 60 with the azide (3) containing the ebselen component. It was obtained in a four-step synthesis starting from 2-(chloroseleno)benzoyl chloride and 2-(2-aminoethoxy)ethanol in 53% yield (based on consumed C 60 ). Its structure was characterized by 1 H NMR, 13 C NMR, IR, UV, and FAB-MS. To verify that the C 60 -based ebselen derivative 4 had enhanced antioxidative and neuroprotective activity, the C 60 derivative 5 and the ebselen derivative 6 were selected to treat cortical neuronal cells using the same procedures as with the C 60 -based ebselen derivative 4. The cellular viability of different derivative treatment groups was estimated by LDH leakage assay and MTT assay. At the same final concentration (30 μmol/L), the results showed that the antioxidative and protective potencies of the C 60 -based ebselen derivative 4 (MTT (OD) 0.340 ± 0.035, LDH release (UL -1 ) 4.80 ± 0.16) against H 2 O 2 -mediated neuronal injury have an advantage over those of C 60 derivative 5 (MTT (OD) 0.297 ± 0.036, LDH release (UL -1 ) 5.37 ± 0.31) and ebselen derivative 6 (MTT (OD) 0.267 ± 0.027, LDH release (UL -1 ) 5.85 ± 0.26). Correspondingly, the GPX activity of 4 (1.62 U/μmol) was higher than that of 5 (0.77 U/μmol) and 6 (1.24 U/μmol). These findings demonstrate that the incorporation of two components with similar biological activity (C 60 component and ebselen component) may be a desirable way of obtaining a new and more biologically effective C 60 -based compound. (author)

  19. The study of biological value of peptone derived from secondary raw fish

    Directory of Open Access Journals (Sweden)

    Kuranova L. K.

    2016-09-01

    Full Text Available The possibility of using secondary fish raw materials in particular musculoskeletal waste from filleting the cod species of fish as raw material base for production of food peptones has been studied. The content of water, fat, protein substances, chloride sodium in the raw material and the product have been determined by standard methods. Amino-acid composition has been determined by high effective liquid chromatography. The biological value of peptone and the balance of essential amino acids have been calculated. It has been established that waste from the cod filleting (the humerus with excess flesh contains 18.95 % protein and a slight (0.15 % amount of fat. The models of peptone – fermentative fish hydrolyzate obtained from cod withdrawals – have been researched. Proteolytic activity used in the hydrolysis of enzyme (protosubtilin G3X has been defined as 560.77 mmol TYR/g. Peptone is an amorphous, fine powder of a light beige color. The product is hygroscopic, readily soluble in water. The chemical and biochemical quality characteristics of enzymatic peptone have been defined. Mass fraction of protein in the derived product is 92.27 %, mass fraction of water – 4.7 %, sodium chloride and 2.6 %, fat – 0.3 %. The total number of amino acids in the product is 94.7 %. Peptone in protein contains all the essential amino acids, the total content of which is 40.8 %. The biological value of the product has been estimated by calculation methods. It has been established that tryptophan is the only limiting amino acid in the protein of peptone, amino-acid score is 66.8 %, the rationality coefficient of the product is 0.42, which characterizes it as a fairly balanced protein product. Peptone obtained from secondary fish raw materials by protein content and its properties corresponds to the category of protein isolates and can be recommended for use in food as complete protein food additives and as protein content in sports nutrition products.

  20. Raman Optical Activity of Biological Molecules

    Science.gov (United States)

    Blanch, Ewan W.; Barron, Laurence D.

    Now an incisive probe of biomolecular structure, Raman optical activity (ROA) measures a small difference in Raman scattering from chiral molecules in right- and left-circularly polarized light. As ROA spectra measure vibrational optical activity, they contain highly informative band structures sensitive to the secondary and tertiary structures of proteins, nucleic acids, viruses and carbohydrates as well as the absolute configurations of small molecules. In this review we present a survey of recent studies on biomolecular structure and dynamics using ROA and also a discussion of future applications of this powerful new technique in biomedical research.

  1. Biologically active compounds of semi-metals.

    Science.gov (United States)

    Rezanka, Tomás; Sigler, Karel

    2008-02-01

    Semi-metals (boron, silicon, arsenic and selenium) form organo-metal compounds, some of which are found in nature and affect the physiology of living organisms. They include, e.g., the boron-containing antibiotics aplasmomycin, borophycin, boromycin, and tartrolon or the silicon compounds present in "silicate" bacteria, relatives of the genus Bacillus, which release silicon from aluminosilicates through the secretion of organic acids. Arsenic is incorporated into arsenosugars and arsenobetaines by marine algae and invertebrates, and fungi and bacteria can produce volatile methylated arsenic compounds. Some prokaryotes can use arsenate as a terminal electron acceptor while others can utilize arsenite as an electron donor to generate energy. Selenium is incorporated into selenocysteine that is found in some proteins. Biomethylation of selenide produces methylselenide and dimethylselenide. Selenium analogues of amino acids, antitumor, antibacterial, antifungal, antiviral, anti-infective drugs are often used as analogues of important pharmacological sulfur compounds. Other metalloids, i.e. the rare and toxic tellurium and the radioactive short-lived astatine, have no biological significance.

  2. Production of biologically active recombinant human factor H in Physcomitrella.

    Science.gov (United States)

    Büttner-Mainik, Annette; Parsons, Juliana; Jérôme, Hanna; Hartmann, Andrea; Lamer, Stephanie; Schaaf, Andreas; Schlosser, Andreas; Zipfel, Peter F; Reski, Ralf; Decker, Eva L

    2011-04-01

    The human complement regulatory serum protein factor H (FH) is a promising future biopharmaceutical. Defects in the gene encoding FH are associated with human diseases like severe kidney and retinal disorders in the form of atypical haemolytic uremic syndrome (aHUS), membranoproliferative glomerulonephritis II (MPGN II) or age-related macular degeneration (AMD). There is a current need to apply intact full-length FH for the therapy of patients with congenital or acquired defects of this protein. Application of purified or recombinant FH (rFH) to these patients is an important and promising approach for the treatment of these diseases. However, neither protein purified from plasma of healthy individuals nor recombinant protein is currently available on the market. Here, we report the first stable expression of the full-length human FH cDNA and the subsequent production of this glycoprotein in a plant system. The moss Physcomitrella patens perfectly suits the requirements for the production of complex biopharmaceuticals as this eukaryotic system not only offers an outstanding genetical accessibility, but moreover, proteins can be produced safely in scalable photobioreactors without the need for animal-derived medium compounds. Transgenic moss lines were created, which express the human FH cDNA and target the recombinant protein to the culture supernatant via a moss-derived secretion signal. Correct processing of the signal peptide and integrity of the moss-produced rFH were verified via peptide mapping by mass spectrometry. Ultimately, we show that the rFH displays complement regulatory activity comparable to FH purified from plasma. © 2010 The Authors. Plant Biotechnology Journal © 2010 Society for Experimental Biology, Association of Applied Biologists and Blackwell Publishing Ltd.

  3. Design, Synthesis and Insecticidal Activity of Novel Phenylurea Derivatives

    Directory of Open Access Journals (Sweden)

    Jialong Sun

    2015-03-01

    Full Text Available A series of novel phenylurea derivatives were designed and synthesized according to the method of active groups linkage and the principle of aromatic groups bioisosterism in this study. The structures of the novel phenylurea derivatives were confirmed based on ESI-MS, IR and 1H-NMR spectral data. All of the compounds were evaluated for the insecticidal activity against the third instars larvae of Spodoptera exigua Hiibner, Plutella xyllostella Linnaeus, Helicoverpa armigera Hubner and Pieris rapae Linne respectively, at the concentration of 10 mg/L. The results showed that all of the derivatives displayed strong insecticidal activity. Most of the compounds presented higher insecticidal activity against S. exigua than the reference compounds tebufenozide, chlorbenzuron and metaflumizone. Among the synthesized compounds, 3b, 3d, 3f, 4b and 4g displayed broad spectrum insecticidal activity.

  4. Co-evaluation of plant extracts as petrochemical substitutes and for biologically active compounds

    Energy Technology Data Exchange (ETDEWEB)

    McChesney, J.D.; Adams, R.P.

    Recent efforts to discover phytochemicals that could substitute for petroleum-derived fuels and industrial feedstocks have not given much attention to the potential of these same phytochemicals to provide sources of biologically active compounds. The suitability of extraction products made to assess specific plants as potential botanochemical sources has been evaluated for use in screening procedures for evidence of biologically active compounds. Screening procedures for antibacterial, antifungal and toxic properties are discussed. Screening results are presented for extracts of nearly 80 species of plants from the southeastern United States and southern Great Plains that had previously been evaluated as sources of botanochemicals.

  5. New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies.

    Science.gov (United States)

    Carradori, Simone; Mollica, Adriano; Ceruso, Mariangela; D'Ascenzio, Melissa; De Monte, Celeste; Chimenti, Paola; Sabia, Rocchina; Akdemir, Atilla; Supuran, Claudiu T

    2015-07-01

    Novel amide derivatives of Probenecid were synthesized and discovered to act as potent and selective inhibitors of the human carbonic anhydrase (hCA, EC 4.2.1.1) transmembrane isoforms hCA IX and XII. The proposed chemical transformation of the carboxylic acid into an amide group led to a complete loss of hCA I and II inhibition (Kis >10,000nM) and enhanced the inhibitory activity against hCA IX and XII, with respect to the parent compound (incorporating a COOH function). These promising biological results have been corroborated by molecular modelling studies within the active sites of the four studied human carbonic anhydrases, which enabled us to rationalize both the isoform selectivity and high activity against the tumor-associated isoforms hCA IX/XII. Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

    Energy Technology Data Exchange (ETDEWEB)

    Wubulikasimu, Reyila; Yang, Yanbing; Xue, Fei; Luo, Xianjin; Shao, Dongping [Shanghai Jiaotong Univ., Shanghai (China); Li, Yuhuan; Gao, Rongmei [Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing (China); Ye, Weidong [Zhejiang Medicine Co. Ltd., Zhejiang (China)

    2013-08-15

    A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4- or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 (IC{sub 50} = 1.08 μg/mL, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.

  7. Biological roles and potential applications of immune cell-derived extracellular vesicles

    OpenAIRE

    Wen, Chuan; Seeger, Robert C.; Fabbri, Muller; Wang, Larry; Wayne, Alan S.; Jong, Ambrose Y.

    2017-01-01

    ABSTRACT Extracellular vesicles (EVs) deliver bioactive macromolecules (i.e. proteins, lipids and nucleic acids) for intercellular communication in multicellular organisms. EVs are secreted by all cell types including immune cells. Immune cell-derived EVs modulate diverse aspects of the immune system to either enhance or suppress immune activities. The extensive effects of immune cell-derived EVs have become the focus of great interest for various nano-biomedical applications, ranging from th...

  8. Synthesis and Biological Evaluation of New 5-Fluorouracil-Substituted Ampelopsin Derivatives

    Directory of Open Access Journals (Sweden)

    Na Zhang

    2010-03-01

    Full Text Available This study reports two novel 5-fluorouracil-substituted ampelopsin derivatives. The structures of two new derivatives were characterized by elemental analysis, 1H-NMR, 13C-NMR, IR and MS. Their anticancer activities in vitro against two cancer cell lines, K562 and K562/ADR, were investigated using the MTT assay, and the results showed that the two new compounds were more effective than reference drugs such as ampelopsin and verapamil.

  9. Copper Nanoparticles: Synthesis and Biological Activity

    Science.gov (United States)

    Satyvaldiev, A. S.; Zhasnakunov, Z. K.; Omurzak, E.; Doolotkeldieva, T. D.; Bobusheva, S. T.; Orozmatova, G. T.; Kelgenbaeva, Z.

    2018-01-01

    By means of XRD and FESEM analysis, it is established that copper nanoparticles with sizes less than 10 nm are formed during the chemical reduction, which form aggregates mainly with spherical shape. Presence of gelatin during the chemical reduction of copper induced formation of smaller size distribution nanoparticles than that of nanoparticles synthesized without gelatin and it can be related to formation of protective layer. Synthesized Cu nano-powders have sufficiently high activity against the Erwinia amylovora bacterium, and the bacterial growth inhibition depends on the Cu nanoparticles concentration. At a concentration of 5 mg / ml of Cu nanoparticles, the exciter growth inhibition zone reaches a maximum value within 72 hours and the lysis zone is 20 mm, and at a concentration of 1 mg / ml this value is 16 mm, which also indicates the significant antibacterial activity of this sample.

  10. Biological activities of synthesized silver nanoparticles from ...

    Indian Academy of Sciences (India)

    ical scavenging activity was measured by the salicylic acid method [16]. The synthesized AgNPs solution at different concentrations (10 to 80 μg ml. −1. ) was dissolved in 1 ml of distilled water. One millilitre of AgNPs mixed with 1 ml of. 9 mM salicylic acid, 1 ml of 9 mM ferrous sulphate and 1ml of 9 mM hydrogen peroxide.

  11. Heterologous expression of biologically active chicken granulocyte ...

    African Journals Online (AJOL)

    user

    2012-02-07

    Feb 7, 2012 ... CD4+ T cells to enhance the ability of secreting antibody and also enhance the function of CD8+ T cells. (Papatriantafyllou, 2011; Tovey and Lallemand, 2010). GM-CSF also is a key regulator of IL-1beta production. Furthermore, It was reported that GM-CSF play a key role in the activation of Th1 and Th17 ...

  12. The antibacterial activity of honey derived from Australian flora.

    Directory of Open Access Journals (Sweden)

    Julie Irish

    Full Text Available Chronic wound infections and antibiotic resistance are driving interest in antimicrobial treatments that have generally been considered complementary, including antimicrobially active honey. Australia has unique native flora and produces honey with a wide range of different physicochemical properties. In this study we surveyed 477 honey samples, derived from native and exotic plants from various regions of Australia, for their antibacterial activity using an established screening protocol. A level of activity considered potentially therapeutically useful was found in 274 (57% of the honey samples, with exceptional activity seen in samples derived from marri (Corymbia calophylla, jarrah (Eucalyptus marginata and jellybush (Leptospermum polygalifolium. In most cases the antibacterial activity was attributable to hydrogen peroxide produced by the bee-derived enzyme glucose oxidase. Non-hydrogen peroxide activity was detected in 80 (16.8% samples, and was most consistently seen in honey produced from Leptospermum spp. Testing over time found the hydrogen peroxide-dependent activity in honey decreased, in some cases by 100%, and this activity was more stable at 4 °C than at 25 °C. In contrast, the non-hydrogen peroxide activity of Leptospermum honey samples increased, and this was greatest in samples stored at 25 °C. The stability of non-peroxide activity from other honeys was more variable, suggesting this activity may have a different cause. We conclude that many Australian honeys have clinical potential, and that further studies into the composition and stability of their active constituents are warranted.

  13. The antibacterial activity of honey derived from Australian flora.

    Science.gov (United States)

    Irish, Julie; Blair, Shona; Carter, Dee A

    2011-03-28

    Chronic wound infections and antibiotic resistance are driving interest in antimicrobial treatments that have generally been considered complementary, including antimicrobially active honey. Australia has unique native flora and produces honey with a wide range of different physicochemical properties. In this study we surveyed 477 honey samples, derived from native and exotic plants from various regions of Australia, for their antibacterial activity using an established screening protocol. A level of activity considered potentially therapeutically useful was found in 274 (57%) of the honey samples, with exceptional activity seen in samples derived from marri (Corymbia calophylla), jarrah (Eucalyptus marginata) and jellybush (Leptospermum polygalifolium). In most cases the antibacterial activity was attributable to hydrogen peroxide produced by the bee-derived enzyme glucose oxidase. Non-hydrogen peroxide activity was detected in 80 (16.8%) samples, and was most consistently seen in honey produced from Leptospermum spp. Testing over time found the hydrogen peroxide-dependent activity in honey decreased, in some cases by 100%, and this activity was more stable at 4 °C than at 25 °C. In contrast, the non-hydrogen peroxide activity of Leptospermum honey samples increased, and this was greatest in samples stored at 25 °C. The stability of non-peroxide activity from other honeys was more variable, suggesting this activity may have a different cause. We conclude that many Australian honeys have clinical potential, and that further studies into the composition and stability of their active constituents are warranted.

  14. Physical aspects of biological activity and cancer

    Science.gov (United States)

    Pokorný, Jiří

    2012-03-01

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

  15. Use of Activated Carbon Derived from Maize Cob and Mahogany ...

    African Journals Online (AJOL)

    MBI

    2015-12-28

    Dec 28, 2015 ... Khan et al., 2004; Gregorio, 2006). The aim of the present work is to investigate the adsorption capacity of activated carbon derived from Maize cob and Mahogany seed shells for the removal of Colour from textile effluent. This will be achieved through the production activated carbon from Maize cob and.

  16. Synthesis and Antifungal Activities of Some Novel Pyrimidine Derivatives

    Directory of Open Access Journals (Sweden)

    Dequn Sun

    2011-06-01

    Full Text Available Three series of new pyrimidine derivatives were synthesized and their antifungal activities were evaluated in vitro against fourteen phytopathogenic fungi. The results indicated that most of the synthesized compounds possessed fungicidal activities and some of them are more potent than the control fungicides. Preliminary SAR was also discussed.

  17. Saponins from Swartzia langsdorffii: biological activities

    Directory of Open Access Journals (Sweden)

    Magalhães Aderbal Farias

    2003-01-01

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

  18. Polycyclic Aromatic Compounds as Anticancer Agents: Synthesis and Biological Evaluation of Methoxy Dibenzofluorene Derivatives

    Directory of Open Access Journals (Sweden)

    Bimal Krishna Banik

    2014-08-01

    Full Text Available Synthesis of a new methoxy dibenzofluorene through alkylation, cyclodehydration and aromatization in a one-pot operation is achieved for the first time. Using this hydrocarbon, a few derivatives are prepared through aromatic nitration, catalytic hydrogenation, coupling reaction with a side chain and reduction. The benzylic position of this hydrocarbon with the side chain is oxidized and reduced. Some of these derivatives have demonstrated excellent antitumor activities in vitro. This study confirms antitumor activity depends on the structures of the molecules.

  19. Synthesis and Biological Evaluation of 7-O-Modified Formononetin Derivatives

    Directory of Open Access Journals (Sweden)

    Ying Yang

    2008-01-01

    Full Text Available Three series of novel formononetin derivatives were synthesized, in which formononetin and heterocyclic moieties were separated by 2-carbon, 3-carbon, and 4-carbon spacers. The chemical structures of these compounds were confirmed. All the derivatives were screened for antiproliferative activities against Jurkat cell line and HepG-2 cell line. In this paper, compounds prepared were also screened for their antibacterial activity of six bacterial strains. Compound 3b exihibited promising antibacterial activity against B. subtilis with minimal inhibitory concentration (MIC value of 0.78 μg/mL, and compound 5e showed significant antiproliferative activities against Jurkat cell growth with IC50 of 1.35×10−4 μg/mL. The preliminary investigation of structure-activity relationships (SARs was also discussed based on the obtained experimental data.

  20. Biologically active extracts with kidney affections applications

    Science.gov (United States)

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

    2015-12-01

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

  1. Biological activities of radiation-degraded carrageenan

    Energy Technology Data Exchange (ETDEWEB)

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

    2001-03-01

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

  2. Biological activities of radiation-degraded carrageenan

    International Nuclear Information System (INIS)

    Relleve, Lorna; Dela Rosa, Alumanda; ABAD, Lucille; Aranilla, Charito; Aliganga, Anne Kathrina; Yoshii, Fumio; Kume, Tamikazu; Nagasawa, Naotsugu

    2001-01-01

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

  3. [Oregano: properties, composition and biological activity].

    Science.gov (United States)

    Arcila-Lozano, Cynthia Cristina; Loarca-Piña, Guadalupe; Lecona-Uribe, Salvador; González de Mejía, Elvira

    2004-03-01

    The oregano spice includes various plant species. The most common are the genus Origanum, native of Europe, and the Lippia, native of Mexico. Among the species of Origanum. their most important components are the limonene, gamma-cariofilene, rho-cymenene, canfor, linalol, alpha-pinene, carvacrol and thymol. In the genus Lippia, the same compounds can be found. The oregano composition depends on the specie, climate, altitude, time of recollection and the stage of growth. Some of the properties of this plant's extracts are being currently studied due to the growing interest for substituting synthetic additives commonly found in foods. Oregano has a good antioxidant capacity and also presents antimicrobial activity against pathogenic microorganisms like Salmonella typhimurium, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis, among others. These are all characteristics of interest for the food industry because they may enhance the safety and stability of foods. There are also some reports regarding the antimutagenic and anticarcinogenic effect of oregano; representing an alternative for the potential treatment and/or prevention of certain chronic ailments, like cancer.

  4. Azaglycomimetics: Natural Occurrence, Biological Activity, and Application

    Science.gov (United States)

    Asano, Naoki

    A large number of alkaloids mimicking the structures of monosaccharides or oligosaccharides have been isolated from plants and microorganisms. The sugar mimicking alkaloids with a nitrogen in the ring are called azasugars or iminosugars. Naturally occurring azasugars are classified into five structural classes: polyhydroxylated piperidines, pyrrolidines, indolizidines, pyrrolizidines, and nortropanes. They are easily soluble in water because of their polyhydroxylated structures and inhibit glycosidases because of a structural resemblance to the sugar moiety of the natural substrate. Glycosidases are involved in a wide range of anabolic and catabolic processes, such as digestion, lysosomal catabolism of glycoconjugates, biosynthesis of glycoproteins, and the endoplasmic reticulum (ER) quality control and ER-associated degradation of glycoproteins. Hence, modifying or blocking these processes in vivo by inhibitors is of great interest from a therapeutic point of view. Azasugars are an important class of glycosidase inhibitors and are arousing great interest for instance as antidiabetics, antiobesity drugs, antivirals, and therapeutic agents for some genetic disorders. This review describes the recent studies on isolation, characterization, glycosidase inhibitory activity, and therapeutic application of azaglycomimetics.

  5. Design, Synthesis, DFT Study and Antifungal Activity of Pyrazolecarboxamide Derivatives

    Directory of Open Access Journals (Sweden)

    Jin-Xia Mu

    2016-01-01

    Full Text Available A series of novel pyrazole amide derivatives were designed and synthesized by multi-step reactions from phenylhydrazine and ethyl 3-oxobutanoate as starting materials, and their structures were characterized by NMR, MS and elemental analysis. The antifungal activity of the title compounds was determined. The results indicated that some of title compounds exhibited moderate antifungal activity. Furthermore, DFT calculations were used to study the structure-activity relationships (SAR.

  6. A biological evaluation on in vitro radiosensitization of nitro-triazole derivatives

    International Nuclear Information System (INIS)

    Li Wuling; Zhang Wensheng; Yang Xinhai

    1997-01-01

    Objective: To assess the radiosensitization of nitro-triazole derivatives and elucidate the structure-activity relationships within this group of compounds. Method: The partition coefficient (p), reduction potential (E 1/2 ), cytotoxicity and sensitization activity were determined by HPLC, polarography and colony formation, respectively. Results: It was found that among these 22 derivatives, two compounds were more efficient than MISO, and other three were of the same efficiency as MISO was in radiosensitizing hypoxic cells, the rest showed poor radiosensitizing properties. As 2-nitroimidazoles, the radiosensitizing activity of a 3-nitro-triazole derivative correlates with its electron affinity, determined as E 1/2 , half-wave reduction potential. The greater is the electron affinity i.e. the more positive the E 1/2 , the greater is the radiosensitizing efficiency. The value of E 1/2 , partition coefficient p value and cytotoxicity of a nitro-triazole derivative are influenced by the structure and chemical properties of the substituent at N 1 or 5 position of triazole ring. The nitro-triazoles examined show only limited differential hypoxic: aerobic toxicity. Conclusion: Although the nitro-triazole derivation are not viable hypoxia-mediated cytotoxins, the radiosensitization of some of them should be studied thoroughly

  7. Comparative study of biological activity of glutathione, sodium ...

    African Journals Online (AJOL)

    Glutathione (GSH) and sodium tungstate (Na2WO4) are important pharmacological agents. They provide protection to cells against cytotoxic agents and thus reduce their cytotoxicity. It was of interest to study the biological activity of these two pharmacological active agents. Different strains of bacteria were used and the ...

  8. Assessing Student Behaviors and Motivation for Actively Learning Biology

    Science.gov (United States)

    Moore, Michael Edward

    2017-01-01

    Vision and Change states that one of the major changes in the way we design biology courses should be a switch in approach from teacher-centered learning to student-centered learning and identifies active learning as a recommended methods. Studies show performance benefits for students taking courses that use active learning. What is unknown is…

  9. Synthesis, spectroscopic and biological studies of transition metal complexes of novel schiff bases derived from cephradine and sugars

    International Nuclear Information System (INIS)

    Naz, N.; Iqbal, M.Z.

    2011-01-01

    Fe(II), Co(II) and Ni(II) metal complexes of novel schiff bases derived from Cephradine and sugars (D-Glucose, L. Arabinose and D-Galactose) were synthesized and characterized by elemental analysis, magnetic susceptibility, thermal analysis, electronic absorption and FT-IR spectral studies. It has been found that schiff bases behave as bi-dentate-ligands forming complexes with 1:2 (metal:ligand) stoichiometry. the neutral nature of the complexes was confirmed by their low conductance values. The biological activities of complexes have been evaluated against two gram negative (Escherichia coli and Pseudomonas aeruginosa) and two gram positive (Bacillus subtilis and staphylococcus aureus) bacteria by Agar diffusion disc method. It has been found that the complexes have higher activity as compared to the pure Cephradine against the same bacteria. (author)

  10. Multifunctional biomaterial coatings: synthetic challenges and biological activity.

    Science.gov (United States)

    Pagel, Mareen; Beck-Sickinger, Annette G

    2017-01-01

    A controlled interaction of materials with their surrounding biological environment is of great interest in many fields. Multifunctional coatings aim to provide simultaneous modulation of several biological signals. They can consist of various combinations of bioactive, and bioinert components as well as of reporter molecules to improve cell-material contacts, prevent infections or to analyze biochemical events on the surface. However, specific immobilization and particular assembly of various active molecules are challenging. Herein, an overview of multifunctional coatings for biomaterials is given, focusing on synthetic strategies and the biological benefits by displaying several motifs.

  11. Synthesis and biological evaluation of novel urea and thiourea derivatives of valacyclovir

    Directory of Open Access Journals (Sweden)

    Katla Ramana Venkata

    2014-01-01

    Full Text Available A series of novel urea and thiourea derivatives of valacyclovir were efficiently synthesized in high yields and evaluated their antiviral activity. 2-((6-Amino-4-oxo-4,5-dihydro-1H-imidazo[4,5-c]pyridin-1-ylmethoxyethyl-2-amino-3-ethylbutanoate (valacyclovir 1 is reacted with various aromatic isocyanates/thiocyanates 2 in the presence of N, N- dimethyl piperazine as a base in THF: pyridine (4:1 to obtain valacyclovir urea/thiourea derivatives 3(a-j. The structures of the title compounds 3(a-j were confirmed by IR, NMR (1H, 13C, mass spectral and elemental analysis. The newly synthesized compounds were screened for their antiviral activity against Tobacco mosaic virus (TMV and antioxidant activity was evaluated by DPPH, SOD and GST methods. The title compounds exhibited potent antiviral and good antioxidant activities.

  12. Synthesis of Different Substituted Pyridazinone Derivatives and Their Anticonvulsant Activity

    Directory of Open Access Journals (Sweden)

    Kartick Chandra Samanta

    2011-01-01

    Full Text Available 6-Phenyl(3᾽-imino-benzylidene-2,3,4,5-tetrahydro pyridazin-3-one derivatives were synthesized from 6-(3᾽-aminophenyl-2,3,4,5-tetrahydro pyridazin-3-one by reaction with different aldehydes. The respective pyridazinone was prepared by cyclization of appropriate β-(aminophenyl propionic acid with hydrazine hydrate. The pyridazinone derivatives were tested for anticonvulsant activity by MES (maximal electro shock method and found that few of them have shown significant anticonvulsant activity.

  13. Regulation of mast cell activation by complement-derived peptides.

    Science.gov (United States)

    Erdei, Anna; Andrásfalvy, Márton; Péterfy, Hajna; Tóth, Gábor; Pecht, Israel

    2004-03-29

    It is known for more than 25 years that the complement-derived anaphylatoxic peptides, C3a, C4a and C5a are potent activators of basophils and certain types of mast cells. Although tissue distribution of receptors for C3a and C5a well exceeds myeloid cells, apparently they are not expressed on mucosal type mast cells, consequently these cells are not activated by C3a and C5a. Our results do however demonstrate that C3a and peptides related to this complement activation product are able to inhibit FcRI-clustering induced activation of mucosal type mast cells-such as RBL-2H3 cells and bone-marrow derived mast cells. Based on the current results we propose the presence of separate "activator" and "inhibitor" sequence motifs in C3a which are in balance under physiologic conditions.

  14. Synthesis and antimalarial activity of new haemanthamine-type derivatives.

    Science.gov (United States)

    Cedrón, Juan C; Gutiérrez, David; Flores, Ninoska; Ravelo, Ángel G; Estévez-Braun, Ana

    2012-09-15

    Thirty one derivatives were prepared from the natural alkaloids haemanthamine (1), haemanthidine (2) and 11-hydroxyvittatine (3). They were evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum and some structure-activity relationships were outlined. For haemanthamine derivatives having a methoxy group at C-3, the presence of a free hydroxyl group at C-11 is important for the activity. The double bond at C-1-C-2 plays also an important role to achieve good inhibitory activity. Compound 35 with two nicotinate groups at C-3 and at C-11 was the most active compound with a IC(50) = 0.8 ± 0.06 μM. Copyright © 2012 Elsevier Ltd. All rights reserved.

  15. Marine-Derived Bioactive Peptides with Pharmacological Activities- A Review

    Directory of Open Access Journals (Sweden)

    Sana Rabiei

    2017-10-01

    Full Text Available Some nutritional factors are related to chronic disease. In response to increased concern regarding nutrition and health, the functional and nutraceuticals food markets have been developed. During food digestion, proteins are hydrolyzed and a wide range of peptides are formed. Some of these peptides have special structures which permit them to confer particular biological functions. Marine animals which involve more than half of the world biological varieties are a wide source of bioactive proteins and peptides. Marine derived peptides show various physiologic functions such as anti-oxidant, antimicrobial, anti-cancer, Angiotensin1-Converting Enzyme (ACE glucosidase and a-amylase inhibitory effects in vitro. Before application of marine bioactive peptides as nutraceuticals or functional food ingredients, their efficacy should be approved through pre-clinical animal and then clinical studies. The aim of this study was to review the studies conducted on the pharmacological effect of marine bioactive peptides in animal models and humans.

  16. Synthesis and Antimicrobial Activities of Some Novel Quinoxalinone Derivatives

    Directory of Open Access Journals (Sweden)

    Y. A. Ammar

    2000-06-01

    Full Text Available Condensation of 4-benzoyl-1,2-phenylenediamine with sodium pyruvate in acetic acid furnished two products which were identified as 6-benzoyl and 7-benzoyl-3-methyl-2(1Hquinoxalinones (1a,b. Fusion of 1a with aromatic aldehydes furnished the styryl derivatives 2a-c. Alkylation of 1a,b with dimethyl sulphate or ethyl chloroacetate produced the N-alkyl derivatives 3a,b and 4a,b. Hydrazinolysis of the ester derivative 4a with hydrazine hydrate afforded the hydrazide derivative 5 which underwent condensation with aldehydes to give the corresponding hydrazone derivatives 6a,b. In addition, chlorination of 1a with thionyl chloride afforded the 2-chloro derivative 7 which was subjected to reaction with sodium azide and n-butylamine to yield the corresponding tetrazolo (8 and n-butylamino (9 derivatives, respectively. The structures of the compounds prepared were confirmed by analytical and spectral data. Also, some of the synthesized compounds were screened for antimicrobial activity.

  17. Biological activity of antitumoural MGBG: the structural variable.

    Science.gov (United States)

    Marques, M P M; Gil, F P S C; Calheiros, R; Battaglia, V; Brunati, A M; Agostinelli, E; Toninello, A

    2008-05-01

    The present study aims at determining the structure-activity relationships (SAR's) ruling the biological function of MGBG (methylglyoxal bis(guanylhydrazone)), a competitive inhibitor of S-adenosyl-L-methionine decarboxylase displaying anticancer activity, involved in the biosynthesis of the naturally occurring polyamines spermidine and spermine. In order to properly understand its biochemical activity, MGBG's structural preferences at physiological conditions were ascertained, by quantum mechanical (DFT) calculations.

  18. Synthesis and biological activity of some heterocyclic compounds ...

    Indian Academy of Sciences (India)

    A number of 1-substituted-2-methyl benzimidazole derivatives have been synthesized and tested for their antibacterial activities. The chemical structures of the newly synthesized compounds were verified on the basis of spectral and elemental methods of analyses. Investigation of antimicrobial activity of the compounds ...

  19. Quinoline derivatives bearing pyrazole moiety: Synthesis and biological evaluation as possible antibacterial and antifungal agents.

    Science.gov (United States)

    El Shehry, Mohamed F; Ghorab, Mostafa M; Abbas, Samir Y; Fayed, Eman A; Shedid, Said A; Ammar, Yousry A

    2018-01-01

    In an attempt for development of new antimicrobial agents, three series of quinoline derivatives bearing pyrazole moiety have been synthesized. The first series was synthesized through the synthesis of 4-(quinolin-2-yloxy)benzaldehyde and 4-(quinolin-2-yloxy)acetophenone and then treatment with ketone or aldehyde derivatives to afford the corresponding chalcones. Cyclization of the latter chalcones with hydrazine derivatives led to the formation of new pyrazoline derivatives. The second series was synthesized via the synthesis of 2-hydrazinylquinoline and then treatment with formylpyrazoles to afford the corresponding hydrazonyl pyrazole derivatives. The third series was synthesized through the treatment of 2-hydrazinylquinoline with ethoxyethylidene, dithioacetal and arylidene derivatives to afford the corresponding pyrazole derivatives. The synthesized compounds were evaluated for their expected antibacterial and antifungal activities; where, the majority of these compounds showed potent antibacterial and antifungal activities against the tested strains of bacteria and fungi. Pyrazole derivative 13b showed better results when compared with the reference drugs as revealed from their MIC values (0.12-0.98 μg/mL). The pyrazole derivative 13b showed fourfold potency of gentamycin in inhibiting the growth of S. flexneri (MIC 0.12 μg/mL). Also, compound 13b showed fourfold potency of amphotericin B in inhibiting the growth of A. clavatus (MIC 0.49 μg/mL) and C. albicans (MIC 0.12 μg/mL), respectively. The same compound showed twofold potency of gentamycin in inhibiting the growth of P. vulgaris (MIC 0.98 μg/mL), equipotent to the ampicillin and amphotericin B in inhibiting the growth of S. epidermidis (MIC 0.49 μg/mL), A. fumigatus (MIC 0.98 μg/mL), respectively. Thus, these studies suggest that quinoline derivatives bearing pyrazole moiety are interesting scaffolds for the development of novel antibacterial and antifungal agents. Copyright © 2017

  20. New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi.

    Science.gov (United States)

    de Moraes Gomes, Paulo André Teixeira; de Oliveira Barbosa, Miria; Farias Santiago, Edna; de Oliveira Cardoso, Marcos Veríssimo; Capistrano Costa, Natáli Tereza; Hernandes, Marcelo Zaldini; Moreira, Diogo Rodrigo Magalhães; da Silva, Aline Caroline; Dos Santos, Thiago André Ramos; Pereira, Valéria Rêgo Alves; Brayner Dos Santosd, Fábio André; do Nascimento Pereira, Glaécia Aparecida; Ferreira, Rafaela Salgado; Leite, Ana Cristina Lima

    2016-10-04

    In previous studies, the compound 3-(bromopropiophenone) thiosemicarbazone was described as a potent anti-Trypanosoma cruzi and cruzain inhibitor. In view to optimize this activity, 1,3-thiazole core was used as building-block strategy to access new lead generation of anti T. cruzi agents. In this way a series of thiazole derivatives were synthesized and most of these derivatives exhibited antiparasitic activity similar to benznidazole (Bzd). Among them, compounds (1c) and (1g) presented better selective index (SI) than Bzd. In addition, compounds showed inhibitory activity against the cruzain protease. As observed by electron microscopy, compound (1c) treatment caused irreversible and specific morphological changes on ultrastructure organization of T. cruzi, demonstrating that this class of compounds is killing parasites. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  1. Insights into female germ cell biology: from in vivo development to in vitro derivations.

    Science.gov (United States)

    Jung, Dajung; Kee, Kehkooi

    2015-01-01

    Understanding the mechanisms of human germ cell biology is important for developing infertility treatments. However, little is known about the mechanisms that regulate human gametogenesis due to the difficulties in collecting samples, especially germ cells during fetal development. In contrast to the mitotic arrest of spermatogonia stem cells in the fetal testis, female germ cells proceed into meiosis and began folliculogenesis in fetal ovaries. Regulations of these developmental events, including the initiation of meiosis and the endowment of primordial follicles, remain an enigma. Studying the molecular mechanisms of female germ cell biology in the human ovary has been mostly limited to spatiotemporal characterizations of genes or proteins. Recent efforts in utilizing in vitro differentiation system of stem cells to derive germ cells have allowed researchers to begin studying molecular mechanisms during human germ cell development. Meanwhile, the possibility of isolating female germline stem cells in adult ovaries also excites researchers and generates many debates. This review will mainly focus on presenting and discussing recent in vivo and in vitro studies on female germ cell biology in human. The topics will highlight the progress made in understanding the three main stages of germ cell developments: namely, primordial germ cell formation, meiotic initiation, and folliculogenesis.

  2. New α-Methylene-γ-Butyrolactone Derivatives as Potential Fungicidal Agents: Design, Synthesis and Antifungal Activities

    Directory of Open Access Journals (Sweden)

    Yongling Wu

    2016-01-01

    Full Text Available In consideration of the fact that the α-methylene-γ-butyrolactone moiety is a major bio-functional group in the structure of carabrone and possesses some agricultural biological activity, forty-six new ester and six new ether derivatives containing α-methylene-γ-butyrolactone moieties were synthesized, and their fungicidal activities against Colletotrichum lagenarium and Botrytis cinerea were investigated. Most of the synthesized compounds showed moderate to significant fungicidal activity. Among them, halogen atom-containing derivatives showed better activity than others, especially compounds 6a,d which exhibited excellent fungicidal activity against C. lagenarium, with IC50 values of 7.68 and 8.17 μM. The structure-activity relationship (SAR analysis indicated that ester derivatives with electron-withdrawing groups on the benzene ring showed better fungicidal activity than those with electron-donating groups. A quantitative structure-activity relationship (QSAR model (R2 = 0.9824, F = 203.01, S2 = 0.0083 was obtained through the heuristic method. The built model revealed a strong correlation of fungicidal activity against C. lagenarium with the molecular structures of these compounds. These results are expected to prove helpful in the design and exploration of low toxicity and high efficiency α-methylene-γ-butyrolactone-based fungicides.

  3. Chemical Composition and Biological Activities of Fragrant Mexican Copal (Bursera spp.)

    OpenAIRE

    Giulia Gigliarelli; Judith X. Becerra; Massimo Curini; Maria Carla Marcotullio

    2015-01-01

    Copal is the Spanish word used to describe aromatic resins from several genera of plants. Mexican copal derives from several Bursera spp., Protium copal, some Pinus spp. (e.g., P. pseudostrobus) and a few Fabaceae spp. It has been used for centuries as incense for religious ceremonies, as a food preservative, and as a treatment for several illnesses. The aim of this review is to analyze the chemical composition and biological activity of commercial Mexican Bursera copal.

  4. Chemical Composition and Biological Activities of Fragrant Mexican Copal (Bursera spp.).

    Science.gov (United States)

    Gigliarelli, Giulia; Becerra, Judith X; Curini, Massimo; Marcotullio, Maria Carla

    2015-12-12

    Copal is the Spanish word used to describe aromatic resins from several genera of plants. Mexican copal derives from several Bursera spp., Protium copal, some Pinus spp. (e.g., P. pseudostrobus) and a few Fabaceae spp. It has been used for centuries as incense for religious ceremonies, as a food preservative, and as a treatment for several illnesses. The aim of this review is to analyze the chemical composition and biological activity of commercial Mexican Bursera copal.

  5. Chemical Composition and Biological Activities of Fragrant Mexican Copal (Bursera spp.

    Directory of Open Access Journals (Sweden)

    Giulia Gigliarelli

    2015-12-01

    Full Text Available Copal is the Spanish word used to describe aromatic resins from several genera of plants. Mexican copal derives from several Bursera spp., Protium copal, some Pinus spp. (e.g., P. pseudostrobus and a few Fabaceae spp. It has been used for centuries as incense for religious ceremonies, as a food preservative, and as a treatment for several illnesses. The aim of this review is to analyze the chemical composition and biological activity of commercial Mexican Bursera copal.

  6. Secondary metabolites in grasses: characterization and biological activity

    Directory of Open Access Journals (Sweden)

    Aldo Tava

    2007-12-01

    Full Text Available In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers, but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to their possible pharmacological use. In the present paper studies on secondary metabolites from herbaceous plants are reviewed. Indications of the chemical methods used for their analyses, their presence in the green material and their biological activity are also reported.

  7. Secondary metabolites in grasses: characterization and biological activity

    Directory of Open Access Journals (Sweden)

    Aldo Tava

    2011-02-01

    Full Text Available In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers, but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to their possible pharmacological use. In the present paper studies on secondary metabolites from herbaceous plants are reviewed. Indications of the chemical methods used for their analyses, their presence in the green material and their biological activity are also reported.

  8. Biological Activity of Curcuminoids Isolated from Curcuma longa

    Directory of Open Access Journals (Sweden)

    Simay Çıkrıkçı

    2008-04-01

    Full Text Available Curcumin is the most important fraction of turmeric which is responsible for its biological activity. In this study, isolation and biological assessment of turmeric and curcumin have been discussed against standard bacterial and mycobacterial strains such as E.coli , S.aureus, E.feacalis, P.aeuroginosa, M.smegmatis, M.simiae, M.kansasii, M. terrae, M.szulgai and the fungi Candida albicans. The antioxidant activity of curcumin and turmeric were also determined by the CUPRAC method.

  9. Synthesis, antimicrobial and antioxidative activity of some new isatin derivatives

    Directory of Open Access Journals (Sweden)

    Šekularac Gavrilo M.

    2014-01-01

    Full Text Available The isatin derivatives, Schiff bases, were synthesized by the reaction of isatin and various substituted primary amines and characterized by several spectroscopic methods. Investigation of the antimicrobial activity of the synthesized compounds was performed by the agar dilution method, against different strains of bacteria and one fungi. The antioxidative activity of the synthesized compounds was also determined. Some of the compounds have shown the significant activity against the selected strains of microorganisms and the antioxidative activity. [Projekat Ministarstva nauke Republike Srbije, br. 172013 i III 46010

  10. Insecticidal and fumigant activities of Cinnamomum cassia bark-derived materials against Mechoris ursulus (Coleoptera: attelabidae).

    Science.gov (United States)

    Park, I K; Lee, H S; Lee, S G; Park, J D; Ahn, Y J

    2000-06-01

    The insecticidal and fumigant activities of Cinnamomum cassia (Blume) bark-derived materials against the oak nut weevil (Mechoris ursulus Roelofs) were examined using filter paper diffusion and fumigation methods and compared to those of the commercially available Cinnamomum bark-derived compounds (eugenol, salicylaldehyde, trans-cinnamic acid, and cinnamyl alcohol). The biologically active constituent of the Cinnamomum bark was characterized as trans-cinnamaldehyde by spectroscopic analysis. In a test with the filter paper diffusion method, trans-cinnamaldehyde showed 100 and 83.3% mortality at rates of 2.5 and 1.0 mg/filter paper, respectively. At 2.5 mg/paper, strong insecticidal activity was produced from eugenol (90.0% mortality) and salicylaldehyde (88. 9%), whereas trans-cinnamic acid revealed moderate activity (73.3%). At 5 mg/paper, weak insecticidal activity (50.0%) was produced from cinnamyl alcohol. In a fumigation test, the Cinnamomum bark-derived compounds were much more effective against M. ursulus larvae in closed cups than in open ones. These results indicate that the insecticidal activity of test compounds was attributable to fumigant action, although there is also significant contact toxicity. As a naturally occurring insect-control agent, the Cinnamomum bark-derived materials described could be useful as a new preventive agent against damage caused by M. ursulus.

  11. Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies.

    Science.gov (United States)

    Gerpe, Alejandra; Aguirre, Gabriela; Boiani, Lucía; Cerecetto, Hugo; González, Mercedes; Olea-Azar, Claudio; Rigol, Carolina; Maya, Juan D; Morello, Antonio; Piro, Oscar E; Arán, Vicente J; Azqueta, Amaia; de Ceráin, Adela López; Monge, Antonio; Rojas, María Antonieta; Yaluff, Gloria

    2006-05-15

    A series of indazole N-oxide derivatives have been synthesized and their antichagasic and leishmanocidal properties studied. 3-Cyano-2-(4-iodophenyl)-2H-indazole N1-oxide exhibited interesting antichagasic activity on the two parasitic strains and the two parasitic stages evaluated. Furthermore, besides its trypanocidal activity, 3-cyano-2-(4-nitrophenyl)-2H-indazole N1-oxide showed leishmanocidal activity in the three parasitic strains evaluated. To gain insight into the mechanism of action, electrochemical behaviour, ESR experiment, inhibition of parasitic respiration and QSAR were performed.

  12. Larvicidal Activity of Essential Oil Derived from Illicium henryi Diels ...

    African Journals Online (AJOL)

    Purpose: To determine larvicidal activity of the essential oil derived from Illicium henryi Diels (Illiciaceae) leaf and stem against the larvae of Aedes albopictus Skuse. Methods: The essential oil of I. henryi leaves was obtained by hydrodistillation and analyzed by gas chromatography (GC) and gas chromaotography-mass ...

  13. Polyphenol derivatives inhibit human neutrophil activity by suppressing oxidative burst

    Czech Academy of Sciences Publication Activity Database

    Drábiková, K.; Perečko, T.; Nosáľ, R.; Harmatha, Juraj; Šmidrkal, J.; Jančinová, V.

    2012-01-01

    Roč. 5, Suppl.1 (2012), s. 31-31 ISSN 1337-6853. [Interdisciplinary Toxicological Conference & Advanced Toxicological Course /17./. 27.08.2012-31.08.2012, Stará Lesná] Institutional research plan: CEZ:AV0Z40550506 Keywords : polyphenol derivatives * neutrophil activity * pinosylvin Subject RIV: CC - Organic Chemistry

  14. Insecticidal activity of extracts derived from different parts of the ...

    African Journals Online (AJOL)

    The insecticidal and antifeedant activity of extracts derived from different parts of the mangrove tree Rhizophora mucronata (Rhizophoraceae) Lam. is reported. The 70% ethanol extracts of leaves, bark, stem wood and pith were tested for toxicity against adults of the desert locust Schistocerca gregaria (Forskal), the 2nd ...

  15. Synthesis and antibacterial activity of novel enolphosphate derivatives.

    Science.gov (United States)

    Grison, Claude; Barthes, Nicolas; Finance, Chantal; Duval, Raphael E

    2010-10-01

    A new class of enolphosphates derivatives, the 1-alkenyldiphosphates, was designed and a rapid and efficient synthesis for these compounds was developed. These new molecules showed interesting in vitro antibacterial activities (MIC) against Gram-positive bacteria (Staphylococcus aureus) and Gram-negative pathogens including Pseudomonas aeruginosa and Escherichia coli. 2010 Elsevier Inc. All rights reserved.

  16. Improved Antitumoral Activity of Extracts Derived from Cultured ...

    African Journals Online (AJOL)

    Erah

    with the total polyphenol content suggesting a causal link related to extract content of polyphenols and phenolic acids [8], while other authors have reported a variety of fatty acids and derivatives with ..... the effectiveness of anticancer therapy; some anticancer drugs show their anticancer activity by inducing apoptosis of ...

  17. Synthesis and biological assessment of novel acylhydrazone derivatives of 2-methyl-1,4-naphthoquinone

    OpenAIRE

    Kamal Bouhadir; Hala Atallah; Rana Mezher; Maamoun Fatfat; Hala Gali-Muhtasib; Jomana Elaridi

    2017-01-01

    Naphthoquinones are medicinally important molecules with a diverse array of biological properties such as antimicrobial, antifungal, antiviral, anti-inflammatory, anti-artherosclerotic and anticarcinogenic activities. In this study, we report the simple and direct preparation of a new group of novel menadione-hydrazone conjugates by reaction of 2-methyl-1,4-naphthoquinones with several aliphatic, aromatic and nucleobase hydrazides. The menadione-hydrazone conjugates were produced in excellent...

  18. Octulosonic acid derivatives from Roman chamomile (Chamaemelum nobile) with activities against inflammation and metabolic disorder.

    Science.gov (United States)

    Zhao, Jianping; Khan, Shabana I; Wang, Mei; Vasquez, Yelkaira; Yang, Min Hye; Avula, Bharathi; Wang, Yan-Hong; Avonto, Cristina; Smillie, Troy J; Khan, Ikhlas A

    2014-03-28

    Six new octulosonic acid derivatives (1-6) were isolated from the flower heads of Roman chamomile (Chamaemelum nobile). Their structures were elucidated by means of spectroscopic interpretation. The biological activity of the isolated compounds was evaluated toward multiple targets related to inflammation and metabolic disorder such as NAG-1, NF-κB, iNOS, ROS, PPARα, PPARγ, and LXR. Similar to the action of NSAIDs, all the six compounds (1-6) increased NAG-1 activity 2-3-fold. They also decreased cellular oxidative stress by inhibiting ROS generation. Compounds 3, 5, and 6 activated PPARγ 1.6-2.1-fold, while PPARα was activated 1.4-fold by compounds 5 and 6 only. None of the compounds showed significant activity against iNOS or NF-κB. This is the first report of biological activity of octulosonic acid derivatives toward multiple pathways related to inflammation and metabolic disorder. The reported anti-inflammatory, hypoglycemic, antiedemic, and antioxidant activities of Roman chamomile could be partly explained as due to the presence of these constituents.

  19. Gemini ester quat surfactants and their biological activity.

    Science.gov (United States)

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

    2013-03-01

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

  20. C60-based ebselen derivative: synthesis by bingel cyclopropanation and enhanced antioxidative and neuroprotective activity

    International Nuclear Information System (INIS)

    Xufeng Liu; Wenchao Guan; Wengshan Ke

    2007-01-01

    C 60 -based ebselen derivative 3 was synthesized through Bingel cyclopropanation of C 60 with the ebselen malonate 2. Compound 3 was obtained in 42% yield (based on consumed C 60 ) in a three-step synthesis starting from 2-(chloroseleno)benzoyl chloride and 2-(2aminoethoxy)ethanol. Its structure was confirmed by 1H NMR, 13 C NMR, IR, UV and FAB-MS spectroscopy analyses. In order to verify the enhanced antioxidative and neuroprotective activity of 3, a C 60 derivative (4), an ebselen derivative (2), and their mixture (4 plus 2 in equimolar ratio) were employed to treat cortical neuronal cells, following the same procedure used with 3 and at the same final concentration (30 μmol L -1 ). Cell viabilities of the four treated groups were estimated by LDH (lactic dehydrogenase) leakage and MTT (3-(4, 5-dimethylthiazole-2yl)-2,5-diphenyl-tetrazolium bromide) assays. Results showed that the antioxidative and protective activities of C 60 -based ebselen derivative 3 against H 2 O 2 -mediated neuronal injury (MTT(OD) 0.364 ± 0.028; LDH release (UL -1 ) 4.66 ± 0.28) were significantly higher than those of C 6 )0 derivative 4 (MTT(OD) 0.324 ± 0.025; LDH release (UL -1 ) 5.39 ± 0.17), ebselen derivative 2 (MTT(OD) 0.294 ± 0.021; LDH release (UL -1 ) 5.71 ± 0.27), and the mixture of 4 and 2 (MTT(OD) 0.310 ± 0.018; LDH release (UL -1 ) 5.54 ±0.39). These findings demonstrated that the combination of two molecular units with similar biological activities (C 60 and ebselen) may be a desirable way of obtaining new and more biologically effective C 60 -based compounds. (author)

  1. Synthesis and Biological Evaluation of Apigenin Derivatives as Antibacterial and Antiproliferative Agents

    Directory of Open Access Journals (Sweden)

    Jinyi Wang

    2013-09-01

    Full Text Available Two series of apigenin [5,7-dihydroxy-2-(4-hydroxyphenyl-4H-chromen-4-one] derivatives, 3a–3j and 4a–4j, were synthesized. The apigenin and alkyl amines moieties of these compounds were separated by C2 or C3 spacers, respectively. The chemical structures of the apigenin derivatives were confirmed using 1H-NMR, 13C-NMR, and electrospray ionization mass spectroscopy. The in vitro antibacterial and antiproliferative activities of all synthesized compounds were determined. Among the tested compounds, 4a–4j displayed significant antibacterial activity against the tested strains (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. Additionally, 4i showed the best inhibitory activity with minimum inhibitory concentrations of 1.95, 3.91, 3.91, and 3.91 μg/mL against S. aureus, B. subtilis, E. coli, and P. aeruginosa, respectively. The antiproliferative activity of the apigenin derivatives was evaluated by an MTT [3-(4,5-dimethylthiazol-2-yl-2,5-diphenyl tetrazolium bromide] assay. We determined that 4a–4j displayed better growth inhibition activity against four human cancer cell lines, namely, human lung (A549, human cervical (HeLa, human hepatocellular liver (HepG2, and human breast (MCF-7 cancer cells, than the parent apigenin. Compound 4j was found to be the most active antiproliferative compound against the selected cancer cells. Structure-activity relationships were also discussed based on the obtained experimental data.

  2. Bactericidal and endotoxin neutralizing activity of a peptide derived from Limulus antilipopolysaccharide factor.

    Science.gov (United States)

    Weiss, C A; Wasiluk, K R; Kellogg, T A; Dunn, D L

    2000-08-01

    Release of lipopolysaccharide (endotoxin, LPS) is a critical inciting event in the development of sepsis syndrome due to gram-negative bacteria, and mortality associated with this entity remains approximately 40%. Limulus anti-LPS factor (LALF) is a naturally occurring horseshoe crab derived protein that, unlike antibiotics, is both bactericidal for gram-negative bacteria and capable of neutralizing LPS. We hypothesized that a peptide derived from the active domain of LALF (LALF #28-54) would exhibit potent biologic activity similar to that of LALF itself and could potentially be useful as a therapeutic agent. The effects of LALF, synthetic peptide LALF #28-54, polymyxin B (PmB), and a biologically inactive synthetic peptide were examined in several models. In vitro bactericidal activity was determined against Pseudomonas aeruginosa, and LPS-neutralizing capacity was determined via inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) secretion by RAW 264.7 cells. In vivo biologic activity was determined via pretreatment following which P aeruginosa endotoxemia or bacteremia was induced; serum TNF-alpha levels, bacterial clearance, and survival were assessed. LALF and LALF #28-54 exhibited potent in vitro bactericidal and LPS-neutralizing activity comparable to PmB (P bacterial clearance similar to that observed for LALF (P .1). These data demonstrate that peptide LALF #28-54 retained the LPS-neutralizing and bactericidal biologic activity of LALF but failed to protect during overwhelming P aeruginosa bacteremia, perhaps due to short serum half-life.

  3. Antibacterial and Antioxidant Activities of Ursolic Acid and Derivatives

    Directory of Open Access Journals (Sweden)

    Patrícia G.G. do Nascimento

    2014-01-01

    Full Text Available Ursolic acid, an important bioactive compound, was isolated from ethanol extract of aerial parts of Sambucus australis. In order to develop bioactive ursolic acid derivatives, two semi-synthetic compounds were obtained through modification at C-3. The antibacterial activity of the ursolic acid and its derivatives was investigated. The microdilution method was used for determination of the minimal inhibitory concentration (MIC, against twelve bacterial strains. The influence of ursolic acid and its derivatives on the susceptibility of some bacterial pathogens to the aminoglycosides antibiotics neomycin, amikacin, kanamycin and gentamicin was evaluated. The most representative synergistic effect was observed by 3β-formyloxy-urs-12-en-28-oic acid at the concentration of 64 μg/mL in combination with kanamycin against Escherichia coli (27, a multidrug-resistant clinical isolate from sputum, with reduction of MIC value from 128 μg/mL to 8 μg/mL. Ursolic acid and its derivatives were examined for their radical scavenger activity using the DPPH assay, and showed significant activity.

  4. QSAR models for antioxidant activity of new coumarin derivatives.

    Science.gov (United States)

    Erzincan, P; Saçan, M T; Yüce-Dursun, B; Danış, Ö; Demir, S; Erdem, S S; Ogan, A

    2015-01-01

    This study presents 37 new antioxidant coumarin derivatives and strategies for structural modification to improve their antioxidant activities, the main ferric-reducing antioxidant power (FRAP) assay used to evaluate their antioxidant properties and the generation of validated quantitative structure-activity (antioxidant activity) relationship (QSAR) models. In an attempt to generate QSAR models, structures of all coumarin derivatives in the data set were fully optimized by semi-empirical PM6 method using SPARTAN 10 software. Descriptors were calculated by DRAGON 6.0 software. Multiple linear regression (MLR) models were developed with different training/test set combinations using QSARINS 2.2.1 software. Robustness, reliability and predictive power of the models were tested by internal and external validations. Applicability domain of the best two-descriptor model (nTR = 30; r(2) = 0.924; RMSETR = 0.213; nTEST = 7; r(2)ext = 0.887; RMSEext = 0.255; CCCext = 0.939) was determined. Descriptors appeared in the model revealed that complexity, H-bond donor and lipophilic character are important parameters in describing the antioxidant activity. Apart from the compounds in the data set, we also designed 31 new antioxidant coumarin derivatives and predicted their antioxidant activity using the best two-descriptor model. Most of these compounds are promising antioxidants.

  5. Antiproliferative and quinone reductase-inducing activities of withanolides derivatives.

    Science.gov (United States)

    García, Manuela E; Nicotra, Viviana E; Oberti, Juan C; Ríos-Luci, Carla; León, Leticia G; Marler, Laura; Li, Guannan; Pezzuto, John M; van Breemen, Richard B; Padrón, José M; Hueso-Falcón, Idaira; Estévez-Braun, Ana

    2014-07-23

    Two new and five known withanolides (jaborosalactones 2, 3, 4, 5, and 24) were isolated from the leaves of Jaborosa runcinata Lam. We also obtained some derivatives from jaborosalactone 5, which resulted to be the major isolated metabolite. The natural compounds as well as derivatives were evaluated for their antiproliferative activity and the induction of quinone reductase 1 (QR1; NQ01) activity. Structure-activity relationships revealed valuable information on the pharmacophore of withanolide-type compounds. Three compounds of this series showed significantly higher antiproliferative activity than jaborosalactone 5. The effect of these compounds on the cell cycle was determined. Furthermore, the ability of major compounds to induce QR1 was evaluated. It was found that all the active test compounds are monofunctional inducers that interact with Keap1. The most promising derivatives prepared from jaborosalactone 5 include (23R)-4β,12β,21-trihydroxy-1,22-dioxo-12,23-cycloergostan-2,5,17,24-tetraen-26,23-olide (18) and (23R)-21-acetoxy-12β-hydroxy-1,22-dioxo-12,23-cycloergostan-2,5,17,24-tetraen-26,23-lactame (20). Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  6. Antibacterial and Antitumor Activities of Biscoumarin and Dihydropyran Derivatives

    Directory of Open Access Journals (Sweden)

    Yun-Peng Sui

    2015-09-01

    Full Text Available A novel series of biscoumarin (1–4 and dihydropyran (5–13 derivatives were synthesized via a one-pot multicomponent condensation reaction and evaluated for antibacterial and antitumor activity in vitro. The X-ray crystal structure analysis of four representative compounds, 3, 7, 9 and 11, confirmed the structures of these compounds. Compounds 1–4 showed the most potent antitumor activity among the total 13 derivatives; especially for compounds 1 and 2, they also emerged as promising antibacterial members with better antibacterial activity. In addition, the results of density functional theory (DFT showed that compared with compounds 3 and 4, biscoumarins 1 and 2 had lower intramolecular hydrogen bonds (HB energy in their structures.

  7. Recent Advances in Momordica charantia: Functional Components and Biological Activities.

    Science.gov (United States)

    Jia, Shuo; Shen, Mingyue; Zhang, Fan; Xie, Jianhua

    2017-11-28

    Momordica charantia L. ( M. charantia ), a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been reported, such as antihyperglycemic, antibacterial, antiviral, antitumor, immunomodulation, antioxidant, antidiabetic, anthelmintic, antimutagenic, antiulcer, antilipolytic, antifertility, hepatoprotective, anticancer and anti-inflammatory activities. However, both in vitro and in vivo studies have also demonstrated that M. charantia may also exert toxic or adverse effects under different conditions. This review addresses the chemical constituents of M. charantia and discusses their pharmacological activities as well as their adverse effects, aimed at providing a comprehensive overview of the phytochemistry and biological activities of M. charantia .

  8. Recent Advances in Momordica charantia: Functional Components and Biological Activities

    Directory of Open Access Journals (Sweden)

    Shuo Jia

    2017-11-01

    Full Text Available Momordica charantia L. (M. charantia, a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been reported, such as antihyperglycemic, antibacterial, antiviral, antitumor, immunomodulation, antioxidant, antidiabetic, anthelmintic, antimutagenic, antiulcer, antilipolytic, antifertility, hepatoprotective, anticancer and anti-inflammatory activities. However, both in vitro and in vivo studies have also demonstrated that M. charantia may also exert toxic or adverse effects under different conditions. This review addresses the chemical constituents of M. charantia and discusses their pharmacological activities as well as their adverse effects, aimed at providing a comprehensive overview of the phytochemistry and biological activities of M. charantia.

  9. Simple Synthesis of Modafinil Derivatives and Their Anti-inflammatory Activity

    Directory of Open Access Journals (Sweden)

    Mankil Jung

    2012-09-01

    Full Text Available Simple synthesis of modafinil derivatives and their biological activity are described. The key synthetic strategies involve substitution and coupling reactions. We determined the anti-inflammatory effects of modafinil derivatives in cultured BV2 cells by measuring the inhibition of nitrite production and expression of iNOS and COX-2 after LPS stimulation. It was found that for sulfide analogues introduction of aliphatic groups on the amide part (compounds 11ad resulted in lower anti-inflammatory activity compared with cyclic or aromatic moieties (compounds 11ek. However, for the sulfoxide analogues, introduction of aliphatic moieties (compounds 12ad showed higher anti-inflammatory activity than cyclic or aromatic fragments (compounds 12ek in BV-2 microglia cells.

  10. Traditional uses, phytochemistry and biological activities of Cotula ...

    African Journals Online (AJOL)

    Cotula cinerea contains a wide range of phytochemical compounds such as saponins, essential oils, tannins, flavonoids, steroids, and terpenoids. This paper reviews information pertaining its traditional uses, phytochemistry and biological activities such as antibacterial, antifungal, antioxidant, herbicidal, anti-diarrheal and ...

  11. Polysaccharies of higher fungi: Biological role, structure and antioxidative activity

    NARCIS (Netherlands)

    Kozarski, M.S.; Klaus, A.; Niksic, M.; Griensven, van L.J.L.D.; Vrvic, M.M.; Jakovljevic, D.M.

    2014-01-01

    The fungal polysaccharides attract a lot of attention due to their multiple challenging bio-logical properties, such as: anti-tumor, anti-viral, anticomplementary, anticoagulant, hypo-lipidemic, immunomodulatory and immune-stimulatory activities, which all together make them suitable for application

  12. Occurrence, biological activity and synthesis of drimane sesquiterpenoids

    NARCIS (Netherlands)

    Jansen, B.J.M.; Groot, de Æ.

    2004-01-01

    In this review the names, structures and occurrence of all new drimanes and rearranged drimanes, which have been published between January 1990 and January 2003 have been collected. Subjects that have been treated are biosynthesis, analysis, biological activities, with special attention to cytotoxic

  13. The cell biology of T-dependent B cell activation

    DEFF Research Database (Denmark)

    Owens, T; Zeine, R

    1989-01-01

    The requirement that CD4+ helper T cells recognize antigen in association with class II Major Histocompatibility Complex (MHC) encoded molecules constrains T cells to activation through intercellular interaction. The cell biology of the interactions between CD4+ T cells and antigen-presenting cells...

  14. A Review on Chemical Constituents and Biological Activities of the ...

    African Journals Online (AJOL)

    The current review is aimed to deliver some updates on the ethnobotany, phytochemistry and biological activities of Beilschmiedia species in order to throw more light on their therapeutic potentials and future research priorities. Phytochemical studies on Beilschmiedia genus yielded essential oils, endiandric acid ...

  15. Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity

    Czech Academy of Sciences Publication Activity Database

    Novotná, E.; Waisser, K.; Kuneš, J.; Palát, K.; Skálová, L.; Szotáková, B.; Buchta, V.; Stolaříková, J.; Ulmann, V.; Pávová, Marcela; Weber, Jan; Komrsková, J.; Hašková, P.; Vokřál, I.; Wsól, V.

    2017-01-01

    Roč. 350, č. 8 (2017), č. článku e1700020. ISSN 0365-6233 Institutional support: RVO:61388963 Keywords : biological activity * cytotoxicity * isocitrate lyase * isothiosemicarbazone * tuberculosis Subject RIV: EE - Microbiology, Virology OBOR OECD: Microbiology Impact factor: 1.994, year: 2016

  16. Solar Energy Education. Renewable energy activities for biology

    Energy Technology Data Exchange (ETDEWEB)

    1982-01-01

    An instructional aid for teachers is presented that will allow biology students the opportunity to learn about renewable energy sources. Some of the school activities include using leaves as collectors of solar energy, solar energy stored in wood, and a fuel value test for green and dry woods. A study of organic wastes as a source of fuel is included. (BCS)

  17. Biological activities of species in the genus Tulbaghia : A review ...

    African Journals Online (AJOL)

    Species of the genus Tulbaghia has been widely used in traditional medicine to treat various ailments such rheumatism, fits, fever, earache, tuberculosis etc. It is believed that the species possess several therapeutic properties. This paper evaluates some of the biological activities of the genus Tulbaghia. It is evident from ...

  18. Physio-chemical evaluation and biological activity of Ajuga ...

    African Journals Online (AJOL)

    Physio-chemical evaluation and biological activity of Ajuga bracteosa wall and Viola odoroto Linn. Anwar Ali Shad, M. Zeeshan, Hina Fazal, Hamid Ullah Shah, Shabir Ahmed, Hasem Abeer, E. F. Abd_Allah, Riaz Ullah, Hamid Afridi, Akash tariq, Muhammad Adnan Asma ...

  19. Traditional uses, phytochemistry and biological activities of Cotula ...

    African Journals Online (AJOL)

    Keywords: Asteraceae, Cotula cinerea, Traditional uses, Phytochemistry, Biological activities. This is an Open .... desert conditions with an average annual rainfall .... Desert area between. Cairo and. Ismailia. (Egypt). Not stated. [33]. The essential oil of C. cinerea has also been subjected to many studies. The essential oil.

  20. Volatile compounds and biological activities of aerial parts of ...

    African Journals Online (AJOL)

    Volatile compounds and biological activities of aerial parts of Pituranthos scoparius (Coss and ... mg/mL. Conclusion: These findings indicate that the essential oil of P.scoparius has a potential for use as a preservative and flavorant in ..... Values are expressed as mean ± standard deviation (n=3). Key: control (♢), BHT (□) ...

  1. Students' Learning Activities While Studying Biological Process Diagrams

    Science.gov (United States)

    Kragten, Marco; Admiraal, Wilfried; Rijlaarsdam, Gert

    2015-01-01

    Process diagrams describe how a system functions (e.g. photosynthesis) and are an important type of representation in Biology education. In the present study, we examined students' learning activities while studying process diagrams, related to their resulting comprehension of these diagrams. Each student completed three learning tasks. Verbal…

  2. Biological activity of phenolic compounds present in buckwheat plants

    Czech Academy of Sciences Publication Activity Database

    Kalinová, J.; Tříska, Jan; Vrchotová, Naděžda

    2005-01-01

    Roč. 16, č. 1 (2005), s. 123-129 ISSN 0971-4693 Institutional research plan: CEZ:AV0Z60870520 Keywords : biological activity, extract, Fagopyrum esculenthum Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 0.686, year: 2005

  3. The Biological Activities of Moltkia aurea; an Endemic Species to ...

    African Journals Online (AJOL)

    Neslihan BALPINAR

    inclination that studies on medicinal plants, which are basis for the development of new biologically active molecules for pharmaceuticals, have rapidly increased. Recent studies associated with medicinal plants make possible to better understand their properties, safety and efficiency. In this study, Moltkia aurea Boiss.

  4. Synthesis, characterization and evaluation of biological activities of ...

    African Journals Online (AJOL)

    Original Research Article. Synthesis, characterization and evaluation of biological activities of manganese-doped zinc oxide nanoparticles. Shakeel Ahmad Khan1*, Sammia Shahid1, Waqas Bashir1, Sadia Kanwal2 and. Ahsan Iqbal3. 1Department of Chemistry, University of Management and Technology, Lahore-54000, ...

  5. BIOLOGICALLY ENHANCED OXYGEN TRANSFER IN THE ACTIVATED SLUDGE PROCESS (JOURNAL)

    Science.gov (United States)

    Biologically enhanced oxgyen transfer has been a hypothesis to explain observed oxygen transfer rates in activated sludge systems that were well above that predicted from aerator clean-water testing. The enhanced oxygen transfer rates were based on tests using BOD bottle oxygen ...

  6. Biological activities of some Fluoroquinolones-metal complexes ...

    African Journals Online (AJOL)

    Background: Metal ions play a vital role in the design of more biologically active drugs. Aim: The paper reviewed the antimicrobial, toxicological and DNA cleavage studies of some synthesized metal complexes of fluoroquinolone antibiotics. Materials and Methods: Literature searches were done using scientific databases.

  7. Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents.

    Science.gov (United States)

    Bekhit, Adnan A; Farghaly, Ahmed M; Shafik, Ragab M; Elsemary, Mona M A; Bekhit, Alaa El-Din A; Guemei, Aida A; El-Shoukrofy, Mai S; Ibrahim, Tamer M

    2018-04-01

    New thienopyrimidinone and triazolothienopyrimidinone derivatives have been synthesized. These compounds were subjected to anti-inflammatory and antimicrobial activity screening aiming to identify new candidates that have dual anti-inflammatory and antimicrobial activities. Compounds 5, 7 and 10a showed minimal ulcerogenic effect and high selectivity towards human recombinant COX-2 over COX-1 enzyme. Their docking outcome correlated with their biological activity and assured the high selectivity binding towards COX-2. In addition, they could act safely up to 80 mg/kg orally or 40 mg/kg parentrally. The antimicrobial screening showed that compound 10a displayed distinctive inhibitory effect on the growth of Escherichia coli comparable to that of ampicillin. Moreover, compounds 5, 7, 9 and 12a possessed 50% of the inhibitory activity of ampicillin against E. coli. Thus, compounds 5, 7 and 10a represent promising dual acting anti-inflammatory and antimicrobial agents. This work provides rewarding template enriching the chemical space for dual anti-inflammatory anti-microbial activities. Copyright © 2018 Elsevier Inc. All rights reserved.

  8. Silica-titania xerogel for solid phase spectrophotometric determination of salicylate and its derivatives in biological liquids and pharmaceuticals.

    Science.gov (United States)

    Morosanova, Maria A; Morosanova, Elena I

    2015-01-01

    Salicylic acid and its derivatives are widely used drugs with potential toxicity. The main areas of salicylate derivatives determination are biological liquids and pharmaceuticals analysis. Silica-titania xerogel has been used for solid phase spectrophotometric determination of various salicylate derivatives (salicylate, salicylamide, methylsalicylate). The reaction conditions influence on the interaction of salicylate derivatives with silica-titania xerogels has been investigated; the characteristics of titanium(IV)-salicylate derivatives complexes in solid phase have been described. The simple solid phase spectrophotometric procedures are based on the formation of xerogel incorporated titanium(IV) colored complexes with salicylate derivatives. A linear response has been observed in the following concentration ranges 0.1-5, 0.5-10 and 0.05-4.7 mM for salicylate, salicylamide, and methylsalicylate, respectively. The proposed procedures have been applied to the analysis of human urine, synthetic serum, and pharmaceuticals. The simple solid phase spectrophotometric procedures of salicylate derivatives determination based on the new sensor materials have been proposed for biological liquids and pharmaceuticals analysis. Graphical abstractComplexation of titanium (IV), incorporated in silica-titania xerogels (Si-Ti), with salicylate derivatives (L) resulting in yellow-colored xerogels (Si-Ti/Ln) has been proposed for salicylate derivatives determination in biological liquids and pharmaceuticals.

  9. Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine.

    Science.gov (United States)

    Papadopoulou, Christina; Geronikaki, Athina; Hadjipavlou-Litina, Dimitra

    2005-01-01

    A series of thiazolyl-N-phenyl piperazines has been synthesised and tested for anti-inflammatory activity. Their R(M) values were determined as an expression of their lipophilicity. Theoretical calculation of their lipophilicity, as clog P and logPsk also performed. The effect of the synthesised compounds on inflammation, using the carrageenin induced mouse paw oedema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents (44-74.1%). Anti-inflammatory activity was influenced by some structural characteristics of the synthesised compounds. An attempt was made to correlate their biological activity with some physicochemical parameters using a quantitative structure-activity relationship approach (QSAR).

  10. Biological Activities of the Essential Oil from Erigeron floribundus

    OpenAIRE

    Riccardo Petrelli; Giuseppe Orsomando; Leonardo Sorci; Filippo Maggi; Farahnaz Ranjbarian; Prosper C. Biapa Nya; Dezemona Petrelli; Luca A. Vitali; Giulio Lupidi; Luana Quassinti; Massimo Bramucci; Anders Hofer; Loredana Cappellacci

    2016-01-01

    Erigeron floribundus (Asteraceae) is an herbaceous plant widely used in Cameroonian traditional medicine to treat various diseases of microbial and non-microbial origin. In the present study, we evaluated the in vitro biological activities displayed by the essential oil obtained from the aerial parts of E. floribundus, namely the antioxidant, antimicrobial and antiproliferative activities. Moreover, we investigated the inhibitory effects of E. floribundus essential oil on nicotinate mononucle...

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

    Directory of Open Access Journals (Sweden)

    Yoon-Ha Kim

    2010-03-01

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

  12. Secondary metabolites from Inula britannica L. and their biological activities.

    Science.gov (United States)

    Khan, Abdul Latif; Hussain, Javid; Hamayun, Muhammad; Gilani, Syed Abdullah; Ahmad, Shabir; Rehman, Gauhar; Kim, Yoon-Ha; Kang, Sang-Mo; Lee, In-Jung

    2010-03-10

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

  13. Syntehsis and antiproliferative activities of chloropyridazine derivatives retain alkylsulfonyl moiety

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Chae Won; Park, Myung Sook [College of Pharmacy, Duksung Women' s University, Seoul (Korea, Republic of)

    2016-11-15

    Some chloropyridazine derivatives have shown interesting pharmacodynamics properties in terms of antioxidant and anti-human rotavirus (HRV) activities (Figure 1). To date, however, no study has evaluated the antiproliferative effects of chloropyridazines in other types of human cancer cells. In conclusion, we designed and synthesized a total of five groups of alkoxy-(or alkylthio-, alkylselenyl-, alkylsufinyl alkylsulfonyl-)chloropyridazines, and their antiproliferative activity was evaluated in the human cancer cell lines. IC{sub 50} values showed that the alkylsulfonylchloropyridazine compounds exhibited more active than the other four groups having alkoxy, alkylthio, alkylselenyl, alkylsulfinyl moieties against MCF-7 and Hep2B Cells.

  14. Hydrogen bonds and antiviral activity of benzaldehyde derivatives

    Science.gov (United States)

    Tolstorozhev, G. B.; Skornyakov, I. V.; Belkov, M. V.; Shadyro, O. I.; Brinkevich, S. D.; Samovich, S. N.

    2012-09-01

    We have obtained the Fourier transform IR spectra of solutions of benzaldehyde derivatives having different antiviral activities against a herpes virus. We observe a correlation between the presence of hydrogen bonds in the benzaldehyde molecules and the appearance of antiviral properties in the compounds. For compounds having antiviral activity, we have obtained spectral data suggesting the existence of hydrogen bonds of the type C=OṡṡṡH-O and O-HṡṡṡO in the molecules. When the hydrogen atom in the hydroxyl groups are replaced by a methyl group, no intramolecular hydrogen bonds are formed and the compounds lose their antiviral activity.

  15. Synthesis of Diethylpropione Derivatives and Their Leukocyte-Increasing Activities

    Energy Technology Data Exchange (ETDEWEB)

    Li, Chung Gang; Sun, Yi Ping; Wang, Guo Ping; Tan, Xiang Duan [Guilin Medical University, Guilin (China)

    2014-09-15

    In search of new antileukopenia agents, twenty dithiolopyrrolone derivatives were synthesized and evaluated for their leukocyte-increasing activities in normal mice. Among the synthesized compounds 4-23, compounds 5 and 6 showed significant leukocyte-increasing activity ( p < 0.01), and compounds 4, 9 and 16 had a moderate effect ( p < 0.05). Compound 5 also displayed stronger leukocyte-increasing activity than that of the positive recombinant human granulocyte colony stimulating factor (rhG-CSF). Above all, compound 5 would be a potential antileukopenia agent which deserved further research.

  16. Assessing Student Behaviors and Motivation for Actively Learning Biology

    Science.gov (United States)

    Moore, Michael Edward

    Vision and Change states that one of the major changes in the way we design biology courses should be a switch in approach from teacher-centered learning to student-centered learning and identifies active learning as a recommended methods. Studies show performance benefits for students taking courses that use active learning. What is unknown is why active learning is such an effective instructional tool and the limits of this instructional method’s ability to influence performance. This dissertation builds a case in three steps for why active learning is an effective instructional tool. In step one, I assessed the influence of different types of active learning (clickers, group activities, and whole class discussions) on student engagement behavior in one semester of two different introductory biology courses and found that active learning positively influenced student engagement behavior significantly more than lecture. For step two, I examined over four semesters whether student engagement behavior was a predictor of performance and found participation (engagement behavior) in the online (video watching) and in-class course activities (clicker participation) that I measure were significant predictors of performance. In the third, I assessed whether certain active learning satisfied the psychological needs that lead to students’ intrinsic motivation to participate in those activities when compared over two semesters and across two different institutions of higher learning. Findings from this last step show us that student’s perceptions of autonomy, competency, and relatedness in doing various types of active learning are significantly higher than lecture and consistent across two institutions of higher learning. Lastly, I tie everything together, discuss implications of the research, and address future directions for research on biology student motivation and behavior.

  17. Synthesis and biological evaluation of new pyrazolo[3,4-d]pyrimidine derivatives

    Directory of Open Access Journals (Sweden)

    Asma Agrebi

    2014-05-01

    Full Text Available Several new pyrazolopyrimidine compounds were achieved from aminocyanopyarazole 1. The starting material 1 was initially coupled with orthoester at refluxed with various primary amines, ammonia, hydrazines and hydroxylamine to furnish a series of pyrazolo[3,4-d]pyrimidines. The reaction of imidate 2a-b with hydrazide derivatives led to the formation of pyrazolo[3,4-d][1,2,4]triazolo[4,3-c]pyrimidines. Some of the synthesized compounds 3a and 4c were evaluated for their anti-inflammatory, antipyretic and nociceptive activities. We start by studing the toxicity of these two molecules by measuring the corresponding DL50. The DL50 of 3a and 4c are estimated to 1333.2mg / kg and 1593.5mg / kg respectively. Pharmacological evaluation showed that compounds 3a and 4c at doses (5.5-22.2 mg / Kg, i.p exhibited anti-inflammatory activities compared to Ibuprofen (150 mg / Kg, i.p, used as a refer ence drug. Further, our study showed that the injection of derived pyrazolopyrimidines on hyperthermic animal leads to a decrease in temperature after 1 hours of treatment compared to paracetamol used as reference. In addition, the injection of derived pyrazolopyrimidines at different doses contains a potent nociceptive activity. This effect is dose-dependent compared to aspirin.

  18. [Exosomes Derived from Mesenchymal Stem Cells--the Future Ideal Vector of Biological Therapy].

    Science.gov (United States)

    Zhang, Juan; Shi, Jing-Shu; Li, Jian

    2015-08-01

    MSC-exosomes are homogeneous menbrane vesicles with diameter 40-100 nm, derived from mesenchymal stem cells at physiological or pathology conditions. MSC-exosomes contain a great quantity and a wide variety of bioactive substances, such as proteins and miRNA. MSC-exosomes transfer bioactive substances to recipient cells to affect their functions through membrane fusion or endocytosis, which like the storage pools of signal vehicles for cell-to-cell comunication in vivo. MSC-exosomes can mimic the beneficial effect of MSC treatment, such as the promotion of tissue repair or the immune regulation. The biological property and functions of MSC-exosomes are reviwed in this article.

  19. Synthesis and Biological Evaluation of Novel Acenaphthene Derivatives as Potential Antitumor Agents

    Directory of Open Access Journals (Sweden)

    Ying-Lan Zhao

    2011-03-01

    Full Text Available Twelve novel acenaphthene derivatives have been synthesized. The structures of all compounds were confirmed by 1H-NMR, MS and elemental analysis. Their antitumor activities were evaluated in six human solid tumor cell lines, namely non-small cell lung cancer (H460, human colon adenocarcinoma (SW480, human breast cancer cell (MDA-MB-468 and SKRB-3, human melanoma cell (A375 and human pancreatic cancer (BxPC-3 . Among them, compound 3c shows the best antitumor activity against SKRB-3 cell line, as high as the positive control adriamycin.

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

    Directory of Open Access Journals (Sweden)

    André Luiz Lourenço

    2015-04-01

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

  1. Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.

    Science.gov (United States)

    Vale-Costa, Sílvia; Vale, Nuno; Matos, Joana; Tomás, Ana; Moreira, Rui; Gomes, Paula; Gomes, Maria Salomé

    2012-11-01

    The current treatment of visceral leishmaniasis is made difficult by the low efficacy, elevated costs, low bioavailability, and high toxicity of many of the available drugs. Primaquine, an antimalarial 8-aminoquinoline, displays activity against Leishmania spp., and several of its derivatives have been developed as potential antileishmanial drugs. However, primaquine exhibits low oral bioavailability due to oxidative deamination of its aliphatic chain. We previously developed peptidomimetic and organometallic derivatives of primaquine, with higher resistance to proteolytic degradation and oxidative deamination, which presented significant activity against primaquine-sensitive pathogens such as Plasmodium or Pneumocystis. In light of these relevant findings, we decided to evaluate these compounds against both the promastigote and intramacrophagic amastigote forms of Leishmania infantum, the agent of Mediterranean visceral leishmaniasis. We found that several of these compounds had significant activity against L. infantum. One of the peptidomimetic (3c) and one of the organometallic (7a) derivatives of primaquine were active against the clinically relevant intramacrophagic amastigote form of the parasite, causing >96% reductions in the number of amastigotes per 100 macrophages at 60 and 40 μM, respectively, while being less cytotoxic for host cells than the reference drugs sitamaquine and miltefosine. Hence, compounds 3c and 7a represent new entries toward the development of new antileishmanial leads.

  2. Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9-Epipolygodial Against Drug Resistant Cancer Cells

    Science.gov (United States)

    Dasari, Ramesh; De Carvalho, Annelise; Medellin, Derek C.; Middleton, Kelsey N.; Hague, Frédéric; Volmar, Marie N. M.; Frolova, Liliya V.; Rossato, Mateus F.; De La Chapa, Jorge J.; Dybdal-Hargreaves, Nicholas F.; Pillai, Akshita; Mathieu, Véronique; Rogelj, Snezna; Gonzales, Cara B.; Calixto, João B.; Evidente, Antonio; Gautier, Mathieu; Munirathinam, Gnanasekar; Glass, Rainer; Burth, Patricia; Pelly, Stephen C.; van Otterlo, Willem A. L.; Kiss, Robert; Kornienko, Alexander

    2015-01-01

    Polygodial, a terpenenoid dialdehyde isolated from Polygonum hydropiper L., is a known TRPV1 agonist. In this investigation a series of polygodial analogues were prepared and investigated for TRPV1 agonistic and anticancer activities. These experiments led to the identification of 9-epipolygodial, possessing antiproliferative potency significantly exceeding that of polygodial. Epipolygodial maintained potency against apoptosis-resistant cancer cells as well as those displaying the MDR phenotype. In addition, a chemical feasibility for the previously proposed mechanism of action of polygodial, involving the Paal-Knorr pyrrole formation with a lysine residue on the target protein, was demonstrated through the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. They should inspire further work in this area aimed at the development of new pharmacological agents or exploration of novel mechanisms of covalent modification of biological molecules with natural products. PMID:26434977

  3. Characterization and biological function of milk-derived miRNAs.

    Science.gov (United States)

    Golan-Gerstl, Regina; Elbaum Shiff, Yaffa; Moshayoff, Vardit; Schecter, Daniel; Leshkowitz, Dena; Reif, Shimon

    2017-10-01

    Breastfeeding is associated with reduced risk of infection, immune-mediated disorders, obesity, and even cancer. Recently it was found that breast milk contains a variety of microRNAs (miRNAs) in the skim and fat layer that can be transferred to infants, and appear to play important roles in those biological functions. This study applied next generation sequencing and quantitative real-time PCR analysis to determine the miRNA expression profile of the skim and fat fraction of human, goat, and bovine milk as well as infant formulas. Human and mammalian milk were found to contain known advantageous miRNAs in exosomes and also in the fat layer. These miRNAs are highly conserved in human, bovine and goat milk. However, they were not detected in several infant formulas. Further, miRNAs present in milk were able to enter normal and tumor cells and affect their biological functions. Following incubation of milk derived human miRNA with normal and cancer cells, the expression of miRNA-148a was upregulated and the expression of the DNA methyltransferase1 target gene of miRNA-148a was down regulated. These results reinforce previous findings on the importance of miRNA in breast milk. Future studies should concentrate on the addition of miRNA to infant formulas. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  4. Synthesis and biological evaluation of carbamates derived from aminocombretastatin A-4 as vascular disrupting agents.

    Science.gov (United States)

    Conesa-Milián, Laura; Falomir, Eva; Murga, Juan; Carda, Miguel; Meyen, Eef; Liekens, Sandra; Alberto Marco, J

    2018-03-10

    A series of twenty-six carbamates derived from aminocombretastatin A-4 (AmCA-4) were synthesized and evaluated for their capacity to affect cell proliferation, tubulin polymerization, mitotic cell arrest, microtubule network organization, apoptosis and endothelial tubular structures in vitro. The anti-proliferative activity of the synthetic carbamates was measured on several human tumor cell lines (i.e. HT-29, MCF-7, HeLa, A-549, MDA-MB-231, HL-60) as well as on the endothelial cell line HMEC-1 and the non-tumor cell line HEK-293. The compounds showed anti-proliferative activity in the nanomolar range thereby exceeding by far the activity of combretastatin A-4 (CA-4) and, in some cases, the activity of AmCA-4. The most active compounds proved to be the carbamates bearing chloro, bromo or methoxy groups in the meta position of the phenyl ring. Moreover, all carbamates inhibited in vitro tubulin polymerization, in a similar manner to that of CA-4 and AmCA-4 by interacting with the colchicine binding site in tubulin. The synthetic carbamates proved as active as AmCA-4 in causing mitotic arrest, as assessed in A549 human lung cancer cells, and disruption of the microtubule cellular network. Some selected carbamates induced apoptosis at concentrations as low as 10 nM, being more active than AmCA-4. Finally, these selected carbamates displayed a vascular disrupting activity on endothelial cells in a dose-dependent manner. In conclusion, our data indicate that carbamates derived from aminocombretastatin A-4 represent interesting lead compounds for the design of vascular disrupting agents. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

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

    Science.gov (United States)

    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. Biological Activities of Phenolic Compounds Present in Virgin Olive Oil

    Directory of Open Access Journals (Sweden)

    Russell Keast

    2010-02-01

    Full Text Available 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.

  7. Should Soil Testing Services Measure Soil Biological Activity?

    Directory of Open Access Journals (Sweden)

    Alan J. Franzluebbers

    2016-02-01

    Full Text Available Health of agricultural soils depends largely on conservation management to promote soil organic matter accumulation. Total soil organic matter changes slowly, but active fractions are more dynamic. A key indicator of healthy soil is potential biological activity, which could be measured rapidly with soil testing services via the flush of CO during 1 to 3 d following rewetting of dried soil. The flush of CO is related to soil microbial biomass C and has repeatedly been shown strongly related to net N mineralization during standard aerobic incubations. New research is documenting the close association with plant N uptake in semicontrolled greenhouse conditions ( = 0.77, = 36. Field calibrations are underway to relate the flush of CO to the need for in-season N requirement in a variety of crops. An index of soil biological activity can and should be determined to help predict soil health and soil N availability.

  8. Structural Diversity and Biological Activities of Cyclic Depsipeptides from Fungi

    Directory of Open Access Journals (Sweden)

    Xiaohan Wang

    2018-01-01

    Full Text Available Cyclic depsipeptides (CDPs are cyclopeptides in which amide groups are replaced by corresponding lactone bonds due to the presence of a hydroxylated carboxylic acid in the peptide structure. These peptides sometimes display additional chemical modifications, including unusual amino acid residues in their structures. This review highlights the occurrence, structures and biological activities of the fungal CDPs reported until October 2017. About 352 fungal CDPs belonging to the groups of cyclic tri-, tetra-, penta-, hexa-, hepta-, octa-, nona-, deca-, and tridecadepsipeptides have been isolated from fungi. These metabolites are mainly reported from the genera Acremonium, Alternaria, Aspergillus, Beauveria, Fusarium, Isaria, Metarhizium, Penicillium, and Rosellina. They are known to exhibit various biological activities such as cytotoxic, phytotoxic, antimicrobial, antiviral, anthelmintic, insecticidal, antimalarial, antitumoral and enzyme-inhibitory activities. Some CDPs (i.e., PF1022A, enniatins and destruxins have been applied as pharmaceuticals and agrochemicals.

  9. Dystrophin-deficient cardiomyocytes derived from human urine: New biologic reagents for drug discovery

    Directory of Open Access Journals (Sweden)

    Xuan Guan

    2014-03-01

    Full Text Available The ability to extract somatic cells from a patient and reprogram them to pluripotency opens up new possibilities for personalized medicine. Induced pluripotent stem cells (iPSCs have been employed to generate beating cardiomyocytes from a patient's skin or blood cells. Here, iPSC methods were used to generate cardiomyocytes starting from the urine of a patient with Duchenne muscular dystrophy (DMD. Urine was chosen as a starting material because it contains adult stem cells called urine-derived stem cells (USCs. USCs express the canonical reprogramming factors c-myc and klf4, and possess high telomerase activity. Pluripotency of urine-derived iPSC clones was confirmed by immunocytochemistry, RT-PCR and teratoma formation. Urine-derived iPSC clones generated from healthy volunteers and a DMD patient were differentiated into beating cardiomyocytes using a series of small molecules in monolayer culture. Results indicate that cardiomyocytes retain the DMD patient's dystrophin mutation. Physiological assays suggest that dystrophin-deficient cardiomyocytes possess phenotypic differences from normal cardiomyocytes. These results demonstrate the feasibility of generating cardiomyocytes from a urine sample and that urine-derived cardiomyocytes retain characteristic features that might be further exploited for mechanistic studies and drug discovery.

  10. Synthesis and antibacterial activity against ralstonia solanacearum for novel hydrazone derivatives containing a pyridine moiety

    Directory of Open Access Journals (Sweden)

    Wu Jian

    2012-04-01

    Full Text Available Abstract Background Ralstonia solanacearum, one of the most important bacterial diseases on plants, is a devastating, soil-borne plant pathogen with a global distribution and an unusually wide host range. In order to discover new bioactive molecules and pesticides acting on tobacco bacterial wilt, we sought to combine the active structure of hydrazone and pyridine together to design and synthesize a series of novel hydrazone derivatives containing a pyridine moiety. Results A series of hydrazone derivatives containing a pyridine moiety were synthesized. Their structures were characterized by 1 H-NMR, 13 C-NMR, IR, and elemental analysis. The preliminary biological activity tests showed that compound 3e and 3g exhibited more than 80% activity against Ralstonia solanacearum at 500 mg/L, especially compound 3g displayed relatively good activity to reach 57.0% at 200 mg/L. Conclusion A practical synthetic route to hydrazone derivatives containing a pyridine moiety by the reaction of intermediates 2 with different aldehydes in ethanol at room temperature using 2-chloronicotinic acid and 2-amino-5-chloro-3-methylbenzoic acid as start materials is presented. This study suggests that the hydrazone derivatives containing a substituted pyridine ring could inhibit the growth of Ralstonia solanacearum.

  11. Synthesis of [13C6]-labelled phenethylamine derivatives for drug quantification in biological samples.

    Science.gov (United States)

    Karlsen, Morten; Liu, HuiLing; Berg, Thomas; Johansen, Jon Eigill; Hoff, Bård Helge

    2014-05-15

    The availability of high-quality (13)C-labelled internal standards will improve accurate quantification of narcotics and drugs in biological samples. Thus, the synthesis of 10 [(13)C6]-labelled phenethylamine derivatives, namely amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine, 3,4-methylenedioxymethamphetamine, 3,4-methylenedioxy-N-ethylamphetamine, 4-methoxyamphetamine, 4-methoxymethamphetamine, 3,5-dimethoxyphenethylamine 4-bromo-2,5-dimethoxyphenethylamine and 2,5-dimethoxy-4-iodophenethylamine, have been undertaken. [(13)C6]-Phenol proved to be an excellent starting material for making (13)C-labelled narcotic substances in the phenethylamine class, and a developed Stille-type coupling enabled an efficient synthesis of the 3,4-methylenedioxy and 4-methoxy derivatives. The pros and cons of alternative routes and transformations are also discussed. The [(13)C6]-labelled compounds are intended for use as internal standards in forensic analysis, health sciences and metabolomics studies by gas chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry. Copyright © 2014 John Wiley & Sons, Ltd.

  12. Biological Characterization and Pluripotent Identification of Sheep Dermis-Derived Mesenchymal Stem/Progenitor Cells

    Directory of Open Access Journals (Sweden)

    Peng Cui

    2014-01-01

    Full Text Available Dermis-derived mesenchymal stem/progenitor cells (DMS/PCs were a multipotential stem cell population, which has potential applications in the tissue damage repair and skin transplant. Although a large number of studies deal with the human DMS/PCs self-renewal and regulation, however, the study of livestock-derived DMS/PCs has rarely been reported. Here, sheep DMS/PCs were isolated from one-month-old sheep embryos and studied at the cellular and molecular level. And then the DMS/PCs biological characteristics were analysed by RT-PCR and immunofluorescence. Experimental results showed that DMS/PCs could be expanded for 48 passages and the cells viability and hereditary character were steady. In addition, the DMS/PCs maker β-integrin, CD71, CD44, and CD73 were expressed positively through RT-PCR and immunofluorescence. Passage 3 DMS/PCs were successfully induced to differentiate into adipocytes, osteoblasts, chondrocytes, and neurocytes, respectively. The above results suggest that DMS/PCs not only have strong self-renewal capacity but also have the potential to differentiate into adipocytes, osteoblasts, chondrocytes, and neurocytes. The study provides theoretical basis and experimental evidence for potential clinical application.

  13. Adsorption Properties of Lignin-derived Activated Carbon Fibers (LACF)

    Energy Technology Data Exchange (ETDEWEB)

    Contescu, Cristian I. [Oak Ridge National Lab. (ORNL), Oak Ridge, TN (United States); Gallego, Nidia C. [Oak Ridge National Lab. (ORNL), Oak Ridge, TN (United States); Thibaud-Erkey, Catherine [United Technologies Research Center (UTRC), East Hartford, CT (United States); Karra, Reddy [United Technologies Research Center (UTRC), East Hartford, CT (United States)

    2016-04-01

    The object of this CRADA project between Oak Ridge National Laboratory (ORNL) and United Technologies Research Center (UTRC) is the characterization of lignin-derived activated carbon fibers (LACF) and determination of their adsorption properties for volatile organic compounds (VOC). Carbon fibers from lignin raw materials were manufactured at Oak Ridge National Laboratory (ORNL) using the technology previously developed at ORNL. These fibers were physically activated at ORNL using various activation conditions, and their surface area and pore-size distribution were characterized by gas adsorption. Based on these properties, ORNL did down-select five differently activated LACF materials that were delivered to UTRC for measurement of VOC adsorption properties. UTRC used standard techniques based on breakthrough curves to measure and determine the adsorption properties of indoor air pollutants (IAP) - namely formaldehyde and carbon dioxide - and to verify the extent of saturated fiber regenerability by thermal treatments. The results are summarized as follows: (1) ORNL demonstrated that physical activation of lignin-derived carbon fibers can be tailored to obtain LACF with surface areas and pore size distributions matching the properties of activated carbon fibers obtained from more expensive, fossil-fuel precursors; (2) UTRC investigated the LACF potential for use in air cleaning applications currently pursued by UTRC, such as building ventilation, and demonstrated their regenerability for CO2 and formaldehyde, (3) Both partners agree that LACF have potential for possible use in air cleaning applications.

  14. Synthesis, characterization, in vitro antimicrobial, and U2OS tumoricidal activities of different coumarin derivatives

    Science.gov (United States)

    2013-01-01

    Background Coumarin and its derivatives are biologically very active. It was found that the enhanced activities are dependent on the coumarin nucleus. Biological significance of these compounds include anti-bacterial, anti-thrombotic and vasodilatory, anti-mutagenic, lipoxygenase and cyclooxygenase inhibition, scavenging of reactive oxygen species, and anti-tumourigenic. Our interest in medicinal chemistry of dicoumarol compounds have been developed by keeping in view the importance of coumarins along with its derivatives in medicinal chemistry. All the synthesized compounds were fully characterized by spectroscopic and analytical techniques and were screened for antimicrobial and U2OS bone cancer activities. Results 4-hydroxycoumarin was derivatized by condensing with different aldehydes yielding the dicoumarol and translactonized products. Elemental analyses, ESI(+,−) MS, 1H and 13C{1H}-NMR, infrared spectroscopy and conductance studies were used to characterize the synthesized compounds which revealed the dicoumarol and dichromone structures for the compounds. The compounds were screened against U2OS cancerous cells and pathogenic micro organisms. The compounds with intermolecular H-bonding were found more active revealing a possible relationship among hydrogen bonding, cytotoxicity and antimicrobial activities. Conclusion Coumarin based drugs can be designed for the possible treatment of U2OS leukemia. PMID:23587363

  15. Anacardic acid derivatives from Brazilian propolis and their antibacterial activity

    Energy Technology Data Exchange (ETDEWEB)

    Silva, M.S.S.; Lima, S.G. de; Lopes, J.A.D.; Chaves, M.H.; Cito, A.M.G.L. [Universidade Federal do Piaui (UFPI), Teresina, PI (Brazil). Dept. de Quimica]. E-mail: gracito@ufpi.br; Oliveira, E.H. [Universidade Federal do Piaui (UFPI), Teresina, PI (Brazil). Dept. de Microbiologia e Parasitologia; Reis, F.A.M. [Universidade Estadual de Campinas (UNICAMP), Campinas, SP (Brazil). Inst. de Quimica

    2008-07-01

    Propolis is a sticky, gummy, resinous substance collected by honeybees (Apis mellifera L.) from various plant sources, which has excellent medicinal properties. This paper describes the isolation and identification of triterpenoids and anacardic acid derivatives from Brazilian propolis and their antibacterial activity. Their structures were elucidated by {sup 1}H and {sup 13}C NMR, including uni- and bidimensional techniques; in addition, comparisons were made with data from academic literature. These compounds were identified as: cardanols (1a + 1b), cardols (2a + 2b), mono ene anacardic acid (3), alpha-amirine (4), beta-amirine (5), cycloartenol (6), 24-methylene-cycloartenol (7) and lupeol (8). The determination of the position of the double bond after a reaction with Dimethyl disulfide (DMDS) is described for the phenol derivatives. The ethanolic extract was tested in vitro for antimicrobial activity by using the disc diffusion method and it showed significant results against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Shigella spp. (author)

  16. Anacardic acid derivatives from Brazilian propolis and their antibacterial activity

    International Nuclear Information System (INIS)

    Silva, M.S.S.; Lima, S.G. de; Lopes, J.A.D.; Chaves, M.H.; Cito, A.M.G.L.; Oliveira, E.H.; Reis, F.A.M.

    2008-01-01

    Propolis is a sticky, gummy, resinous substance collected by honeybees (Apis mellifera L.) from various plant sources, which has excellent medicinal properties. This paper describes the isolation and identification of triterpenoids and anacardic acid derivatives from Brazilian propolis and their antibacterial activity. Their structures were elucidated by 1 H and 13 C NMR, including uni- and bidimensional techniques; in addition, comparisons were made with data from academic literature. These compounds were identified as: cardanols (1a + 1b), cardols (2a + 2b), mono ene anacardic acid (3), alpha-amirine (4), beta-amirine (5), cycloartenol (6), 24-methylene-cycloartenol (7) and lupeol (8). The determination of the position of the double bond after a reaction with Dimethyl disulfide (DMDS) is described for the phenol derivatives. The ethanolic extract was tested in vitro for antimicrobial activity by using the disc diffusion method and it showed significant results against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Shigella spp. (author)

  17. Anti-cancer activities of diospyrin, its derivatives and analogues

    KAUST Repository

    Sagar, Sunil

    2010-09-01

    Natural products have played a vital role in drug discovery and development process for cancer. Diospyrin, a plant based bisnaphthoquinonoid, has been used as a lead molecule in an effort to develop anti-cancer drugs. Several derivatives/analogues have been synthesized and screened for their pro-apoptotic/anti-cancer activities so far. Our review is focused on the pro-apoptotic/anti-cancer activities of diospyrin, its derivatives/analogues and the different mechanisms potentially involved in the bioactivity of these compounds. Particular focus has been placed on the different mechanisms (both chemical and molecular) thought to underlie the bioactivity of these compounds. A brief bioinformatics analysis at the end of the article provides novel insights into the new potential mechanisms and pathways by which these compounds might exert their effects and lead to a better realization of the full therapeutic potential of these compounds as anti-cancer drugs. © 2010 Elsevier Masson SAS. All rights reserved.

  18. Derivation of criteria for primary circuit activity in an HTGR

    International Nuclear Information System (INIS)

    Su, S.D.; Barsell, A.W.

    1980-11-01

    This paper derives specific criteria for the circulating and plateout activity in the primary circuit for a 2170-MW(t) high temperature gas-cooled reactor-gas turbine (HTGR-GT) plant. Results show that for a design basis, (1) the circulating activity should be limited to 14,000 Ci Kr-88 (a principal nuclide) to meet both offsite dose and containment access constraint during normal operation and depressurization accidents, and (2) the plateout inventories for those important nuclides affecting shutdown maintenance should not exceed 10,000 Ci Ag-110m, 45,000 Ci Cs-134 and 130,000 Ci Cs-137. This paper presents bases and methodology for deriving such criteria and compares them with light water reactors. 5 tables

  19. Inhibitory activity of the peptides derived from buffalo prolactin on ...

    Indian Academy of Sciences (India)

    http://www.ias.ac.in/jbiosci. Inhibitory activity of the peptides derived from buffalo prolactin on angiogenesis. JAEOK LEE, SYAMANTAK MAJUMDER, SUVRO CHATTERJEE and KAMBADUR MURALIDHAR. M L1 L2 L3 L4 L5. (A). (B). Densitometry of 15% SDS-PAGE on 20th Oct. 07. 0. 0.5. 1. 1.5. Rf. O.D.. Protein Marker.

  20. Anacardic acid derivatives from Brazilian propolis and their antibacterial activity

    OpenAIRE

    Silva, M. S. S.; De Lima, S. G.; Oliveira, E. H.; Lopes, J. A. D.; Chaves, M. H.; Reis, F. A. M.; Citó, A. M. G. L.

    2008-01-01

    Propolis is a sticky, gummy, resinous substance collected by honeybees (Apis mellifera L.) from various plant sources, which has excellent medicinal properties. This paper describes the isolation and identification of triterpenoids and anacardic acid derivatives from Brazilian propolis and their antibacterial activity. Their structures were elucidated by ¹H and 13C NMR, including uni- and bidimensional techniques; in addition, comparisons were made with data from academic literature. These co...

  1. Facile synthesis, biological evaluation and molecular docking studies of novel substituted azole derivatives

    Science.gov (United States)

    Rafiq, Muhammad; Saleem, Muhammad; Jabeen, Farukh; Hanif, Muhammad; Seo, Sung-Yum; Kang, Sung Kwon; Lee, Ki Hwan

    2017-06-01

    In this study, we synthesized the series of novel azole derivatives and evaluated for enzyme inhibition assays, corresponding kinetic analysis and molecular modeling. Among the investigated bioassays, the oxadiazole derivatives 4a-k were found potent α-glucosidase inhibitors while the Schiff base derivatives 7a-k exhibited considerable potential toward urease inhibition. The inhibition kinetics for the most active compounds were analyzed by the Lineweaver-Burk plots to investigate the possible binding modes of the synthesized compounds toward the tested proteins. Moreover, the detailed docking studies were performed on the synthesized library of 4a-k and 7a-k to study the molecular interaction and binding mode in the active site of the modeled yeast α-glucosidase and Jack Bean Urease, respectively. It could be inferred from docking results that theoretical studies are in close agreement to that of the experimental results. The structure of one of the compound 7k was characterized by the single crystal X-ray diffraction analysis in order to find out the predominant conformation of the molecules.

  2. Indonesian propolis: chemical composition, biological activity and botanical origin.

    Science.gov (United States)

    Trusheva, Boryana; Popova, Milena; Koendhori, Eko Budi; Tsvetkova, Iva; Naydenski, Christo; Bankova, Vassya

    2011-03-01

    From a biologically active extract of Indonesian propolis from East Java, 11 compounds were isolated and identified: four alk(en)ylresorcinols (obtained as an inseparable mixture) (1-4) were isolated for the first time from propolis, along with four prenylflavanones (6-9) and three cycloartane-type triterpenes (5, 10 and 11). The structures of the components were elucidated based on their spectral properties. All prenylflavanones demonstrated significant radical scavenging activity against diphenylpicrylhydrazyl radicals, and compound 6 showed significant antibacterial activity against Staphylococcus aureus. For the first time Macaranga tanarius L. and Mangifera indica L. are shown as plant sources of Indonesian propolis.

  3. Synthesis, biological evaluation and molecular docking studies of chromone hydrazone derivatives as α-glucosidase inhibitors.

    Science.gov (United States)

    Wang, Guangcheng; Chen, Ming; Wang, Jing; Peng, Yaping; Li, Luyao; Xie, ZhenZhen; Deng, Bing; Chen, Shan; Li, Wenbiao

    2017-07-01

    A series of chromone hydrazone derivatives 4a-4p have been synthesized, characterized by 1 H NMR and 13 C NMR and evaluated for theirinvitro α-glucosidase inhibitory activity. Out of these tested compounds, six (4a, 4b, 4d, 4j, 4o and 4p) displayed potent α-glucosidase inhibitory activity with IC 50 values in the range of 20.1±0.19μM to 45.7±0.23μM, as compared to the standard drug acarbose (IC 50 =817.38±6.27μM). Among this series, compound 4d (IC 50 =20.1±0.19μM) with 4-sulfonamide substitution at phenyl part of hydrazide was found to be the most active compound. Lineweaver-Burk plot analysis indicated that compound 4d is a non-competitive inhibitor of α-glucosidase. The binding interactions of the most active analogs were confirmed through molecular docking studies. Docking studies showed 4d are interacting with the residues Glu-276, Asp-214, Asp-349 and Arg-439 through hydrogen bonds, arene-anion and arene-cation interactions. In summary, our studies shown that these chromone hydrazone derivatives are a new class of α-glucosidase inhibitors. Copyright © 2017 Elsevier Ltd. All rights reserved.

  4. Synthesis and Antiproliferative Activity of Thioxoflavones Mannich Base Derivatives.

    Science.gov (United States)

    Li, Wei; Li, Xueli; Liu, Manhui; Wang, Qiuan

    2017-07-01

    Two series of 12 novel thioxoflavones Mannich base derivatives 5a-f and 6a-f were synthesized via Mannich reaction of 4',7-dimethoxy-5-hydroxyflavothione (3) or 3',4',7-trimethoxy-5-hydroxyflavothione (4) with appropriate aliphatic amines or alicyclic amines and formaldehyde. Thioxoflavones 3 and 4 were prepared from 4',7-dimethoxy-5-hydroxyflavone (1) and 3',4',7-trimethoxy-5-hydroxyflavone (2) with Lawesson's reagent, respectively. Their antiproliferative activities in vitro were evaluated on a panel of three human cell lines (HeLa, HCC1954, and SK-OV-3) by CCK-8 assay. The results showed that most of the thioxoflavones and their Mannich base derivatives exhibited potential antiproliferative activities on the tested cancer cell lines, with IC 50 values ranging from 9.16 to 55.50 μM. In particular, thioxoflavone 4 and the thioxoflavone Mannich base derivatives 5a and 5d showed the best antiproliferative activity on all three human cancer cell lines; they are promising candidates worthy of further development. The structures of all synthesized compounds were confirmed by 1 H NMR, 13 C NMR, IR, and MS techniques. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  5. Preparation and biological evaluation of novel acylhydrazide derivatives of 2,3-dichloronaphthoquinone

    Directory of Open Access Journals (Sweden)

    Jomana Elaridi

    2017-04-01

    Full Text Available Naphthoquinones have been reported to possess a variety of pharmacological properties including antibacterial, antifungal, antiviral, anti-inflammatory, anti-artherosclerotic and anticancer effects. We have successfully synthesized a series of novel naphthoquinone acylhydrazides. The straightforward synthesis of these molecules involves a coupling reaction between 2,3-dichloro-1,4-naphthoquinone and several alkyl and aromatic hydrazides and the hydrazides of the pyrimidine nucleobases, uracil and thymine. The product hydrazides were isolated in good yields and completely characterized by spectroscopic analysis. Biological evaluation against human colon cancer HCT116 cells and human breast cancer MCF-7 cells indicated that the novel hydrazides possessed significant anticancer activity.

  6. Correlation between the lipophilicity and antifungal activity of some benzoxazole derivatives

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2010-01-01

    Full Text Available In the present work, a quantitative relationship between the lipophilicity and antifungal activity of some benzoxazole derivatives against Candida albicans was investigated by using QSAR (quantitative structure-activity relationship analyses. The descriptors which describe numerically the lipophilicity, logP, were calculated using Chem-Office Software version 7.0. The linear correlation between the minimal inhibitory concentration (log1/cMIC and lipophilicity descriptors was investigated. The best QSAR model predicting the antifungal activity of the investigated series of benzoxazole was developed. The results are discussed on the basis of statistical data. High agreement between theoretical and experimental inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on antifungal activity of this class of compounds, which can be very useful in the design of new biologically active molecules.

  7. Design, Synthesis and Biological Evaluation of C(6-Modified Celastrol Derivatives as Potential Antitumor Agents

    Directory of Open Access Journals (Sweden)

    Kaiyong Tang

    2014-07-01

    Full Text Available New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468. The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84–0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.

  8. Pyrazolodiazepine derivatives with agonist activity toward Drosophila RYamide receptor.

    Science.gov (United States)

    Yoon, Yeu Kyung; Kim, Jung Ha; Kim, Jeong-Hyun; Kwon, Jae-Young; Kim, Yong-Chul; Kim, Young-Joon; Park, Zee-Yong

    2016-10-15

    The neuropeptide Y (NPY)-like signaling is conserved broadly in many animal species, and implicated in diverse biological functions, particularly those associated with feeding and metabolism. In Drosophila, three G protein coupled receptors (GPCRs) are closely related to the vertebrate NPY receptors: RYamide receptor (RYa-R) CG5811, neuropeptide F receptor (NPFR) CG1147 and short neuropeptide F receptor (sNPF-R) CG7395. Here, we screened 442 compounds of the pyrazolodiazepine analogs library, and identified four synthetic small compounds that activate the RYa-R, but not other two receptors. Their maximum activity is about 40% of the endogenous ligand, Drosophila RYamide-1, indicating they are partial agonists. Structural comparisons of these agonists identified an active core structure, characterized by phenylalanine and lysine fused pyrazolodiazepine skeletons, which can be utilized as a lead structure for further development of more potent drugs active on mammalian NPYRs. Identification of small compound agonists selective on RYa-R of the genetically amenable insect model will facilitate future efforts to understand biological functions of RYa-R, a GPCR conserved in many species. Copyright © 2016 Elsevier Ltd. All rights reserved.

  9. QSAR Study of the Biologically Active Organosulfurs in Natural Products

    Directory of Open Access Journals (Sweden)

    Fakhr M. Abu-Awwad

    2010-01-01

    Full Text Available The biological activities of two sets of a total of 30 different polysulfides were investigated using QSAR. The semiempirical AM1 in Gaussian 2003 for windows was used to optimize the structures whereas a subsequent calculation of hundreds of various types of descriptors at the density functional (B3LYP/6-31G* using CODESSA package was employed. The known 15-lipoxygenase inhibitory activity data (IC50 of 19 polysulfides out of the whole data set were correlated in a multiple linear regression procedures with the computed descriptors. Statistically, the most significant overall correlations were five- and four- parameter equations with good statistical parameters; R2= 0.9981, R2CV = 0.9970 and R2=9967, R2CV = 0.9933 respectively. The models concluded that biological activity of polysulfides is mainly attributed to quantum-chemical, geometrical and topological descriptors with neither electrostatic contribution nor chief role of sulfur atoms. Also sulfur related descriptors were not the most significant contributors in the concluded models. The obtained models were efficiently employed to estimate the biological activities of the other 11 polysulfides available in natural products such as garlic and mushroom.

  10. Biological activity and photostability of biflorin micellar nanostructures.

    Science.gov (United States)

    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.

  11. Biological Activity and Photostability of Biflorin Micellar Nanostructures

    Directory of Open Access Journals (Sweden)

    Edson R. B. Santana

    2015-05-01

    Full Text Available 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.

  12. Essential Oils’ Chemical Characterization and Investigation of Some Biological Activities: A Critical Review

    Science.gov (United States)

    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

  13. Synthesis and evaluation of antioxidant activity of new quinoline-2-carbaldehyde hydrazone derivatives: bioisosteric melatonin analogues.

    Science.gov (United States)

    Puskullu, M Orhan; Shirinzadeh, Hanif; Nenni, Merve; Gurer-Orhan, Hande; Suzen, Sibel

    2016-01-01

    Overproduction of reactive oxygen species results in oxidative stress that can cause fatal damage to vital cell structures. It is known that the use of antioxidants could be beneficial in the prevention or delay of numerous diseases associated with oxidative stress. Melatonin (MLT) is known as a powerful free-radical scavenger and antioxidant. It was found that indole ring of MLT can be employed by bioisosteric replacement by other aromatic rings. Quinoline derivatives constitute an important class of compounds for new drug development. Owing to quinoline and hydrazones appealing physiological properties and are mostly found in numerous biologically active compounds a series of quinoline-2-carbaldehyde hydrazone derivatives were synthesized as bioisosteric analogues of MLT, characterized and in vitro antioxidant activity was investigated by evaluating their reducing effect against oxidation of a redox-sensitive fluorescent probe. Cytotoxicity potential of all compounds was investigated both by lactate dehydrogenase leakage assay and by MTT assay.

  14. Pharmacological Activities and Synthesis of Esculetin and Its Derivatives: A Mini-Review

    Directory of Open Access Journals (Sweden)

    Chengyuan Liang

    2017-03-01

    Full Text Available Esculetin, synonymous with 6,7-dihydroxycoumarin, is the main active ingredient of the traditional Chinese medicine Cortex Fraxini. The twig skin or trunk bark of Cortex Fraxini are used by herb doctors as a mild, bitter liver and gallbladder meridians’ nontoxic drug as well as dietary supplement. Recently, with a variety of novel esculetin derivatives being reported, the molecular mechanism research as well as clinical application of Cortex Fraxini and esculetin are becoming more attractive. This mini-review will consolidate what is known about the biological activities, the mechanism of esculetin and its synthetic derivatives over the past decade in addition to providing a brief synopsis of the properties of esculetin.

  15. Synthesis and pharmacological activity evaluation of arctigenin monoester derivatives.

    Science.gov (United States)

    Chen, Qiulian; Yang, Limin; Han, Mei; Cai, Enbo; Zhao, Yan

    2016-12-01

    Arctigenin (ARG), a nature medicine with many pharmacological activities, was poorly soluble in water and placed restriction on practical usage. Six novel arctigenin monoester derivatives were obtained from the reflux reaction with arctigenin, carboxylic acids (crotonic acid, furoic acid, 2-naphthalene acid and indol-3-acetic acid), EDCI and DMAP in dichloromethane at 60°C for 4-6h and their properties on nitrite scavenging assay were investigated in vitro. Based on the results, the one of the most effective derivatives, arctigenin β-indolylacetate (ARG6), was selected to study anti-tumor activity in vivo at doses of 20 and 40mg/kg. The results showed that comparison with ARG group, ARG6 exhibited more anti-tumor activity in H22 tumor-bearing mice. Furthermore, ARG6 exhibited less damage to the liver, kidney, spleen and thymus when compared with those in positive group. Biochemical parameters of ALT, AST, BUN and Cre showed ARG6 had little toxicity to mice as well. ARG6 significantly improved serum cytokine levels of IL-2, IL-6, IFN-γ and TNF-α, and decreased VEGF compared with ARG. Moreover, H & E staining, TUNEL assay and immunohistochemical of tumor issues also indicated that ARG6 exhibited anti-tumor activity in vivo. In brief, the present study provide a method to improve ARG anti-tumor activity and provide a reference for new anti-tumor agent. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  16. Antimicrobial activity of rhodanine-3-acetic acid derivatives.

    Science.gov (United States)

    Krátký, Martin; Vinšová, Jarmila; Stolaříková, Jiřina

    2017-03-15

    Twenty-four 2-(4-oxo-2-thioxothiazolidin-3-yl)acetic acid (rhodanine-3-acetic acid)-based amides, esters and 5-arylalkylidene derivatives were synthesized, characterized and evaluated as potential antimicrobial agents against a panel of bacteria, mycobacteria and fungi. All of the derivatives were active against mycobacteria. N-(4-Chlorophenyl)-2-[5-(2-hydroxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl]acetamide demonstrated the highest activity against Mycobacterium tuberculosis with minimum inhibitory concentrations (MIC) of 8-16μM. Non-tuberculous mycobacteria were the most susceptible to 2-[5-(2-hydroxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl]acetic acids (MIC values ⩾32μM). The highest antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus exhibited 4-(trifluoromethyl)phenyl 2-(4-oxo-2-thioxothiazolidin-3-yl)acetate (MIC⩾15.62μM). Several structure-activity relationships were identified. The activity against Gram-negative and fungal pathogens was marginal. Copyright © 2017 Elsevier Ltd. All rights reserved.

  17. Design, Synthesis and Fungicidal Activities of Some Novel Pyrazole Derivatives

    Directory of Open Access Journals (Sweden)

    Xue-Ru Liu

    2014-09-01

    Full Text Available In order to discover new compounds with good fungicidal activities, 32 pyrazole derivatives were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR, and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS, and their fungicidal activities against Botrytis cinerea, Rhizoctonia solani Kuhn, Valsa mali Miyabe et Yamada, Thanatephorus cucumeris (Frank Donk, Fusarium oxysporum (S-chl f.sp. cucumerinum Owen, and Fusarium graminearum Schw were tested. The bioassay results indicated that most of the derivatives exhibited considerable antifungal activities, especially compound 26 containing a p-trifluoromethyl- phenyl moiety showed the highest activity, with EC50 values of 2.432, 2.182, 1.787, 1.638, 6.986, and 6.043 μg/mL against B. cinerea, R. solani, V. mali, T. cucumeris, F. oxysporum, and F. graminearum, respectively. Moreover, the activities of compounds such as compounds 27–32 were enhanced by introducing isothiocyanate and carboxamide moieties to the 5-position of the pyrazole ring.

  18. Thrombin-specific inactivation of endothelial cell derived plasminogen activator

    International Nuclear Information System (INIS)

    Highsmith, R.F.; Gallaher, M.J.

    1986-01-01

    Although thrombin (T) has diverse functions in the overall hemostatic mechanism, relatively little is known about its direct effect on components of the fibrinolytic enzyme system. The authors have investigated the interaction of T with plasminogen activators (PA) derived from bovine aortic endothelial cells (EC) in culture (2-5th passage, preconfluent monolayers). Varying concentrations of purified bovine or human thrombin were added to EC-conditioned media (CM). CM + T mixtures were assayed at various times for PA activity using purified plasminogen and a sensitive 125 I-fibrinogenolytic or caseinolytic assay. T (5 nM), but not plasmin or trypsin at equivalent concentrations, resulted in a time-dependent inhibition of the PA activity in CM. T had no effect on the PA activity of urokinase, streptokinase or preformed plasmin. The ability of T to inactivate the EC-derived PA was abolished by prior treatment of T with active site-directed reagents. SDS-PAGE and zymography with copolymerized fibrinogen and plasminogen revealed further specificity in that only one of the multiple-molecular weight forms of PA present in EC-CM was inactivated by T. The authors conclude that in a highly specific fashion, T inactivates the predominant PA present in EC-CM by limited proteolysis. Thus, another potentially important function of T is suggested which may have particular significance in the temporal regulation of coagulation and fibrinolysis at the blood-endothelium interface

  19. Thrombin-specific inactivation of endothelial cell derived plasminogen activator

    Energy Technology Data Exchange (ETDEWEB)

    Highsmith, R.F.; Gallaher, M.J.

    1986-03-05

    Although thrombin (T) has diverse functions in the overall hemostatic mechanism, relatively little is known about its direct effect on components of the fibrinolytic enzyme system. The authors have investigated the interaction of T with plasminogen activators (PA) derived from bovine aortic endothelial cells (EC) in culture (2-5th passage, preconfluent monolayers). Varying concentrations of purified bovine or human thrombin were added to EC-conditioned media (CM). CM + T mixtures were assayed at various times for PA activity using purified plasminogen and a sensitive /sup 125/I-fibrinogenolytic or caseinolytic assay. T (5 nM), but not plasmin or trypsin at equivalent concentrations, resulted in a time-dependent inhibition of the PA activity in CM. T had no effect on the PA activity of urokinase, streptokinase or preformed plasmin. The ability of T to inactivate the EC-derived PA was abolished by prior treatment of T with active site-directed reagents. SDS-PAGE and zymography with copolymerized fibrinogen and plasminogen revealed further specificity in that only one of the multiple-molecular weight forms of PA present in EC-CM was inactivated by T. The authors conclude that in a highly specific fashion, T inactivates the predominant PA present in EC-CM by limited proteolysis. Thus, another potentially important function of T is suggested which may have particular significance in the temporal regulation of coagulation and fibrinolysis at the blood-endothelium interface.

  20. Synthesis and antimicrobial activity of 2-chloroquinoline incorporated pyrazoline derivatives

    Directory of Open Access Journals (Sweden)

    Sandhya Bawa

    2009-01-01

    Full Text Available Purpose : A series of 2-chloroquinoline containing pyrazoline derivatives having 3,4-dichloro/ 3,4-dimethoxy in the phenyl ring were synthesized and screened for their antimicrobial activity against a panel of bacterial and fungal strains. Materials and Methods : The structures of the newly synthesized compounds were established on the basis of spectral data obtained from the FTIR, 1H and 13C-NMR, and mass spectrometry. All the compounds were evaluated for their antibacterial activity against Escherichia coli (NCTC, 10418, Staphylococcus aureus (NCTC, 65710, and Pseudomonas aeruginosa (NCTC, 10662. The compounds were also tested for antifungal activity aganist Aspergillus niger (MTCC, 281, Aspergillus flavus (MTCC, 277, Monascus purpureus (MTCC, 369 and Penicillium citrinum (NCIM, 768 by the cup-plate method. Results : Among the compounds tested, 3,4-dichloro derivatives were comparatively more active in antimicrobial screening with respect to their 3,4-dimethoxy analog. Conclusion : A careful analysis of the antimicrobial activity data of the compounds revealed that compounds 3a, 3b, 3c, and 3e exhibited potent antibacterial

  1. Synthesis and Biological Evaluation of Novel 5,7-Dichloro-1,3-benzoxazole Derivatives

    Directory of Open Access Journals (Sweden)

    N. D. Jayanna

    2013-01-01

    Full Text Available A new class of 5,7-dichloro-1,3-benzoxazole derivatives 4–11 were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole 3 nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound 3 on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by 1H NMR, IR, Mass, and 13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds 4, 5, and 8 have shown significant antimicrobial activities, whereas compounds 6 and 8 have been emerged as leading cytotoxic agents. The compounds 9, 10, and 11 were found to be strong enzyme inhibitors.

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

    Directory of Open Access Journals (Sweden)

    Ranga Rao Ambati

    2014-01-01

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

  3. QSAR analysis on Spodoptera litura antifeedant activities for flavone derivatives

    International Nuclear Information System (INIS)

    Duchowicz, Pablo R.; Goodarzi, Mohammad; Ocsachoque, Marco A.; Romanelli, Gustavo P.; Ortiz, Erlinda del V.; Autino, Juan C.; Bennardi, Daniel O.; Ruiz, Diego M.; Castro, Eduardo A.

    2009-01-01

    We establish useful models that relate experimentally measured biological activities of compounds to their molecular structure. The pED 50 feeding inhibition on Spodoptera litura species exhibited by aurones, chromones, 3-coumarones and flavones is analyzed in this work through the hypothesis encompassed in the Quantitative Structure-Activity Relationships (QSAR) Theory. This constitutes a first necessary computationally based step during the design of more bio-friendly repellents that could lead to insights for improving the insecticidal activities of the investigated compounds. After optimizing the molecular structure of each furane and pyrane benzoderivative with the semiempirical molecular orbitals method PM3, more than a thousand of constitutional, topological, geometrical and electronic descriptors are calculated and multiparametric linear regression models are established on the antifeedant potencies. The feature selection method employed in this study is the Replacement Method, which has proven to be successful in previous analyzes. We establish the QSAR both for the complete molecular set of compounds and also for each chemical class, so that acceptably describing the variation of the inhibitory activities from the knowledge of their structure and thus achieving useful predictive results. The main interest of developing trustful QSAR models is that these enable the prediction of compounds having no experimentally measured activities for any reason. Therefore, the structure-activity relationships are further employed for investigating the antifeedant activity on previously synthesized 2-,7-substituted benzopyranes, which do not pose any measured values on the biological expression. One of them, 2-(α-naphtyl)-4H-1-benzopyran-4-one, results in a promising structure to be experimentally analyzed as it has predicted pED 50 = 1.162.

  4. QSAR analysis on Spodoptera litura antifeedant activities for flavone derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Duchowicz, Pablo R., E-mail: pabloducho@gmail.com [Instituto de Investigaciones Fisicoquimicas Teoricas y Aplicadas INIFTA (UNLP, CCT La Plata-CONICET), Diag. 113 y 64, Sucursal 4, C.C. 16, 1900 La Plata (Argentina); Goodarzi, Mohammad [Instituto de Investigaciones Fisicoquimicas Teoricas y Aplicadas INIFTA (UNLP, CCT La Plata-CONICET), Diag. 113 y 64, Sucursal 4, C.C. 16, 1900 La Plata (Argentina); Ocsachoque, Marco A. [Centro de Investigacion y Desarrollo en Ciencias Aplicadas ' Dr. J. J. Ronco' (CINDECA), Departamento de Quimica, Facultad de Ciencias Exactas, UNLP-CONICET. Calle 47 No 257, B1900AJK La Plata (Argentina); Romanelli, Gustavo P. [Centro de Investigacion y Desarrollo en Ciencias Aplicadas ' Dr. J. J. Ronco' (CINDECA), Departamento de Quimica, Facultad de Ciencias Exactas, UNLP-CONICET. Calle 47 No 257, B1900AJK La Plata (Argentina); Catedra de Quimica Organica, Facultad de Ciencias Agrarias y Forestales, UNLP. Calles 60 y 119, B1904AAN La Plata (Argentina); Ortiz, Erlinda del V. [Facultad de Tecnologia y Ciencias Aplicadas, Universidad Nacional de Catamarca, Av. Maximio Victoria 55, (4700), Catamarca (Argentina); Autino, Juan C.; Bennardi, Daniel O.; Ruiz, Diego M. [Catedra de Quimica Organica, Facultad de Ciencias Agrarias y Forestales, UNLP. Calles 60 y 119, B1904AAN La Plata (Argentina); Castro, Eduardo A. [Instituto de Investigaciones Fisicoquimicas Teoricas y Aplicadas INIFTA (UNLP, CCT La Plata-CONICET), Diag. 113 y 64, Sucursal 4, C.C. 16, 1900 La Plata (Argentina)

    2009-12-20

    We establish useful models that relate experimentally measured biological activities of compounds to their molecular structure. The pED{sub 50} feeding inhibition on Spodoptera litura species exhibited by aurones, chromones, 3-coumarones and flavones is analyzed in this work through the hypothesis encompassed in the Quantitative Structure-Activity Relationships (QSAR) Theory. This constitutes a first necessary computationally based step during the design of more bio-friendly repellents that could lead to insights for improving the insecticidal activities of the investigated compounds. After optimizing the molecular structure of each furane and pyrane benzoderivative with the semiempirical molecular orbitals method PM3, more than a thousand of constitutional, topological, geometrical and electronic descriptors are calculated and multiparametric linear regression models are established on the antifeedant potencies. The feature selection method employed in this study is the Replacement Method, which has proven to be successful in previous analyzes. We establish the QSAR both for the complete molecular set of compounds and also for each chemical class, so that acceptably describing the variation of the inhibitory activities from the knowledge of their structure and thus achieving useful predictive results. The main interest of developing trustful QSAR models is that these enable the prediction of compounds having no experimentally measured activities for any reason. Therefore, the structure-activity relationships are further employed for investigating the antifeedant activity on previously synthesized 2-,7-substituted benzopyranes, which do not pose any measured values on the biological expression. One of them, 2-({alpha}-naphtyl)-4H-1-benzopyran-4-one, results in a promising structure to be experimentally analyzed as it has predicted pED{sub 50} = 1.162.

  5. Composting of the solid fraction of digestate derived from pig slurry: Biological processes and compost properties

    International Nuclear Information System (INIS)

    Tambone, Fulvia; Terruzzi, Laura; Scaglia, Barbara; Adani, Fabrizio

    2015-01-01

    Highlights: • Anaerobic digestion leads to the production of a biologically stable digestate. • Solid–liquid separation produces a solid fraction having high fertilizer value. • Composting process shows low biological activity due to high biological stability of digestate. • Solid digestate fraction can be composted in a short time or used directly as organic fertilizer. - Abstract: The aim of this paper was to assess the characteristics of the solid fractions (SF) obtained by mechanical separation of digestate, their compostability and compost quality. To do so, the SF of digestates obtained from anaerobic digestion of pig slurry, energy crops and agro-industrial residues were sampled in five plants located in Northern Italy. Results obtained indicated that anaerobic digestion by itself promoted the high biological stability of biomasses with a Potential Dynamic Respiration Index (PDRI) close to 1000 mgO 2 kg V S −1 h −1 . Subsequent composting of digestates, with an added bulking agent, did not give remarkably different results, and led only to a slight modification of the characteristics of the initial non-composted mixtures; the composts obtained fully respected the legal limits for high quality compost. Chemical studies of organic matter composition of the biomasses by using CP MAS 13 C NMR, indicated that the compost was composed of a high relative content of O-alkyl-C (71.47% of total C) (cellulose and hemicelluloses) and a low alkyl-C (12.42%) (i.e. volatile fatty acids, steroid-like molecules, aliphatic biopolymers and proteins)

  6. Synthesis and antitubercular activity of quaternized promazine and promethazine derivatives.

    Science.gov (United States)

    Bate, Aaron B; Kalin, Jay H; Fooksman, Eric M; Amorose, Erica L; Price, Cristofer M; Williams, Heather M; Rodig, Michael J; Mitchell, Miguel O; Cho, Sang Hyun; Wang, Yuehong; Franzblau, Scott G

    2007-03-01

    Quaternized chlorpromazine, triflupromazine, and promethazine derivatives were synthesized and examined as antitubercular agents against both actively growing and non-replicating Mycobacterium tuberculosis H37Rv. Impressively, several compounds inhibited non-replicating M. tuberculosis at concentrations equal to or double their MICs against the actively growing strain. All active compounds were non-toxic toward Vero cells (IC50 > 128 microM). N-Allylchlorpromazinium bromide was only weakly antitubercular, but replacing allyl with benzyl or substituted benzyl improved potency. An electron-withdrawing substituent on the phenothiazine ring was also essential. Branching at the carbon chain decreased antitubercular activity. The optimum antitubercular structures possessed N-(4- or 3-chlorobenzyl) substitution on triflupromazine.

  7. Design, Synthesis, and Antibacterial Activities of Novel Heterocyclic Arylsulphonamide Derivatives.

    Science.gov (United States)

    Singh, Anuradha; Srivastava, Ritika; Singh, Ramendra K

    2017-02-13

    Design, synthesis, and antibacterial activities of a series of arylsulphonamide derivatives as probable peptide deformylase (PDF) inhibitors have been discussed. Compounds have been designed following Lipinski's rule and after docking into the active site of PDF protein (PDB code: 1G2A) synthesized later on. Furthermore, to assess their antibacterial activity, screening of the compound was done in vitro conditions against Gram-positive and Gram-negative bacterial strains. In silico, studies revealed these compounds as potential antibacterial agents and this fact was also supported by their prominent scoring functions. Antibacterial results indicated that these molecules possessed a significant activity against Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Escherichia coli with MIC values ranging from 0.06 to 0.29 μM. TOPKAT results showed that high LD 50 values and the compounds were assumed non-carcinogenic when various animal models were studied computationally.

  8. Evaluation of antituberculosis activity and DFT study on dipyrromethane-derived hydrazone derivatives

    Science.gov (United States)

    Rawat, Poonam; Singh, R. N.; Niranjan, Priydarshni; Ranjan, Alok; Holguín, Norma Rosario Flores

    2017-12-01

    This paper evaluates the anti-tubercular activity of dipyrromethane-derived hydrazones derivatives (3a-d) against strain of Mycobacterium tuberculosis H37Rv. The newly synthesized compounds have been obtained in good yield based on the condensation of aromatic aldehyde derivatives with pyrrole hydrazone in presence of catalyst and well characterized with spectroscopic methods (1H, 13C NMR, Mass spectrometry) and elemental analysis. The singlet observed in the experimental 1H and 13C NMR spectra in the range of 5.3-5.7 ppm and 30-33.86 ppm, respectively, indicating that two pyrrole units are joined at meso position. The electronic transitions observed in the experimental spectra are n→π* and π →π* in nature. Experimental and theoretical findings corroborate well with each other. The substitution of acceptor group (-NO2) at ortho- and meta-positions of benzene ring, present at meso-position of dipyrromethane is responsible for variation in β0 values. The calculated NLO of (3a-d) are much greater than those of p-nitroaniline (PNA). The solvent induced effects on the non-linear optical properties were studied and found to enhance NLO properties of the molecules as dielectric constants of the solvents increases. On the basis of results it is anticipated that these dipyrromethanes will be useful for both antimicrobial and non-linear optical (NLO) applications. With the help of Microplate Alamar Blue assay (MABA) method all (3a-d) compounds were screened for their anti-tubercular activity and found that 3b and 3d have higher inhibitory activity against strain of M. tuberculosis H37Rv.

  9. Characterization of biologically active substances from Calendula officinalis.

    Science.gov (United States)

    Lovecka, Petra; Lipov, Jan; Thumova, Kamila; Macurkova, Anna

    2018-02-26

    The aim of this work was to compare water and organic extracts, infusions and tinctures from flowers and leaves of Calendula officinalis in terms of their biological activity and composition. The purpose of work was investigation whether the leaves and stems are really the waste or they contain interesting substances which could be utilized. Antimicrobial, antifungal, antioxidant and anti-inflammatory activities were studied. Then the ability to inhibit collagenase was studied as well. Cytotoxicity was tested for all the samples on mammalian cell lines. To determine the composition of extracts, infusions and tinctures phytochemical analysis (the set of colour reactions for detection of groups of biologically active compounds) was carried out and shown that samples from flowers and leaves contain the same groups of biologically active substances (proteins and amino acids, reducing sugars, flavonoids, saponins, phenolics, terpenoids, steroids, glycosides). The antimicrobial activity of tested samples was proved, where the most sensitive bacterium was Micrococcus luteus and the most sensitive yeast was Geotrichum candidum. The study of anti - collagenase activity has shown that the enzymatic reaction of collagenase was affected by all tested samples and their effect was concentration dependent. Cytotoxicity of water and methanol extracts at cell lines HEK 293T and HepG2 was observed. Cells HepG2 were more sensitive than cells HEK 293T. Using cell line RAW 264.7 anti-inflammatory activity of all samples was observed. Tincture of leaves was the most effective. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  10. Biological activity of selected plants with adaptogenic effect

    Directory of Open Access Journals (Sweden)

    Eva Ivanišová

    2016-05-01

    Full Text Available The aim of this study was to determine biological activity of plants with adaptogenic effect: Panax ginseng Mayer., Withania somnifera L., Eleuterococcus senticosus Rupr. et Maxim., Astragallus membranaceus Fisch. and Codonopsis pilosulae Franch. The antioxidant activity was detected by DPPH and phosphomolybdenum method, total polyphenol content with Folin – Ciocalteu reagent, flavonoids content by aluminium chloride method. The detection of antimicrobial activity was carried out by disc diffusion method against three species of Gram-negative bacteria: Escherichia coli CCM 3988, Salmonella enterica subsp. enterica CCM 3807, Yersinia enterocolitica CCM 5671 and two Gram-positive bacteria: Bacillus thuringiensis CCM 19, Stapylococcus aureus subsp. aureus CCM 2461. Results showed that plants with adaptogenic effect are rich for biologically active substances. The highest antioxidant activity by DPPH method was determined in the sample of Eleuterococcus senticosus (3.15 mg TEAC – Trolox equivalent antioxidant capacity per g of sample and by phosphomolybdenum method in the sample of Codonopsis pilosulae (188.79 mg TEAC per g of sample. In the sample of Panax ginseng was measured the highest content of total polyphenols (8.10 mg GAE – galic acid equivalent per g of sample and flavonoids (3.41 μg QE – quercetin equivalent per g of sample. All samples also showed strong antimicrobial activity with the best results in Panax ginseng and Withania somnifera in particular for species Yersinia enterocolitica CCM 5671 and Salmonella enterica subsp. enterica CCM 3807. The analyzed species of plant with high value of biological activity can be used more in the future, not only in food, but also in cosmetics and pharmaceutical industries.

  11. Semisynthetic macrolide antibacterials derived from tylosin. Synthesis and structure-activity relationships of novel desmycosin analogues.

    Science.gov (United States)

    Mutak, Stjepan; Marsić, Natasa; Kramarić, Miroslava Dominis; Pavlović, Drazen

    2004-01-15

    A series of 20-O-substituted and 3,20-di-O-substituted derivatives of desmycosin were synthesized and their biological properties were evaluated. In particular, we have synthesized numerous side chain modified analogues of desmycosin as well as some analogues possessing a combination of modified side chain and alternative C-3 substituents. Thus, alpha,beta-unsaturated analogues of desmycosin (2), tylosin (1), 10,11,12,13-tetrahydrotylosin (11), and 2,3-didehydrodesmycosin (13) were prepared from the corresponding aldehydes by a Wittig reaction with the stabilized ylides (a-d), generating a trans-double bond, followed by modified Pfitzner-Moffat oxidation of the C-3 hydroxyl group. To evaluate the importance of the C-3 position of desmycosin for biological activity, the C-3 substituted derivatives were synthesized by a standard sequence of protective group chemistry followed by Wittig reaction and esterification as the key steps. For the attachment of the C-3 ester functionality, a mixed anhydride protocol was adopted. Reaction proceeded smoothly to give corresponding esters in yields ranging from 70 to 80%. Base- and acid-catalyzed rearrangement products including desmycosin 8,20-aldols (24a and 24b) and desmycosin 3,19-aldol (25) are also described. Parallel array synthesis and purification techniques allowed for the rapid exploration of structure-activity relationships within this class and for the improvement in potency. In vitro evaluation of these derivatives demonstrated good antimicrobial activity against Gram-positive bacteria for most of the compounds. The present derivatives of 16-membered macrolides were active against MLS(B)-resistant strains that were inducibly resistant, but not those constitutively resistant to erythromycin.

  12. MILK KEFIR: COMPOSITION, MICROBIAL CULTURES, BIOLOGICAL ACTIVITIES AND RELATED PRODUCTS

    Directory of Open Access Journals (Sweden)

    Maria Rosa Prado

    2015-10-01

    Full Text Available In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir’s exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir’s microflora and the importance of kefiran as a beneficial health substance.

  13. Milk kefir: composition, microbial cultures, biological activities, and related products.

    Science.gov (United States)

    Prado, Maria R; Blandón, Lina Marcela; Vandenberghe, Luciana P S; Rodrigues, Cristine; Castro, Guillermo R; Thomaz-Soccol, Vanete; Soccol, Carlos R

    2015-01-01

    In recent years, there has been a strong focus on beneficial foods with probiotic microorganisms and functional organic substances. In this context, there is an increasing interest in the commercial use of kefir, since it can be marketed as a natural beverage that has health promoting bacteria. There are numerous commercially available kefir based-products. Kefir may act as a matrix in the effective delivery of probiotic microorganisms in different types of products. Also, the presence of kefir's exopolysaccharides, known as kefiran, which has biological activity, certainly adds value to products. Kefiran can also be used separately in other food products and as a coating film for various food and pharmaceutical products. This article aims to update the information about kefir and its microbiological composition, biological activity of the kefir's microflora and the importance of kefiran as a beneficial health substance.

  14. Charged particle activation analysis of phosphorus in biological materials

    International Nuclear Information System (INIS)

    Masumoto, K.; Yagi, M.

    1983-01-01

    Charged particle activation analysis of phosphorus in biological materials using the 31 P(α,n) sup(34m)Cl reaction has been studied. Since sup(34m)Cl is also produced by the 32 S(α,pn) and the 35 Cl(α,α'n) reactions, the thick-target yield curves on phosphorus, sulfur and chlorine were determined in order to choose the optimum irradiation conditions. As a result, it was found that the activation analysis for phosphorus without interferences from sulfur and chlorine is possible by bombarding with less than 17 MeV alphas. The applicability of this method to biological samples was then examined by irradiating several standard reference materials. It was confirmed that phosphorus can readily be determined at the detection limit of 1μg free from interferences due to the matrix elements. (author)

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

    Science.gov (United States)

    Pal, Dilipkumar; Mishra, Pragya; Sachan, Neetu; Ghosh, Ashoke K

    2011-10-01

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

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

    Directory of Open Access Journals (Sweden)

    Dilipkumar Pal

    2011-01-01

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

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

    Science.gov (United States)

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

    2012-07-01

    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.

  18. Secondary metabolites in grasses: characterization and biological activity

    OpenAIRE

    Aldo Tava

    2007-01-01

    In a series of studies dealing on the nutritional value of forage species, more attention was focussed on several compounds, named secondary metabolites, that are important in determining nutritional characteristics. Secondary metabolites are compounds detected in the green materials in low concentration compared to primary metabolites (proteins, sugars, lipids, fibers), but of fundamental importance for the plant physiology. The possess several biological activities and this contribute to th...

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

    Science.gov (United States)

    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.

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

    OpenAIRE

    Cicerale, Sara; Lucas, Lisa; Keast, Russell

    2010-01-01

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

  1. Recent Advances in Momordica charantia: Functional Components and Biological Activities

    OpenAIRE

    Jia, Shuo; Shen, Mingyue; Zhang, Fan; Xie, Jianhua

    2017-01-01

    Momordica charantia L. (M. charantia), a member of the Cucurbitaceae family, is widely distributed in tropical and subtropical regions of the world. It has been used in folk medicine for the treatment of diabetes mellitus, and its fruit has been used as a vegetable for thousands of years. Phytochemicals including proteins, polysaccharides, flavonoids, triterpenes, saponins, ascorbic acid and steroids have been found in this plant. Various biological activities of M. charantia have been report...

  2. Structural Diversity and Biological Activities of Cyclic Depsipeptides from Fungi

    OpenAIRE

    Xiaohan Wang; Xiao Gong; Peng Li; Daowan Lai; Ligang Zhou

    2018-01-01

    Cyclic depsipeptides (CDPs) are cyclopeptides in which amide groups are replaced by corresponding lactone bonds due to the presence of a hydroxylated carboxylic acid in the peptide structure. These peptides sometimes display additional chemical modifications, including unusual amino acid residues in their structures. This review highlights the occurrence, structures and biological activities of the fungal CDPs reported until October 2017. About 352 fungal CDPs belonging to the groups of cycli...

  3. Chemical composition and biological activities of the Agaricus mushrooms

    Directory of Open Access Journals (Sweden)

    L Munkhgerel

    2014-10-01

    Full Text Available Two species of Agaricus mushroom grown in Mongolia were analyzed for their element content. Biological activity and chemical components study of Agaricus, grown in the Mongolian flora has been investigated for the first time. The ethanol extracts of dried Agaricus sp. mushrooms were analyzed for antioxidant activity on 1,1-diphenyl-2- picrylhydrazyl (DPPH radicals and interferon-like activity. The ethanol extracts from Agaricus arvensis showed the most potent radical scavenging activity. The IC50 of A. silvaticus and A. arvensis were 216 and 17.75 g/ml respectively. Among the twenty three mushroom extracts, the extracts from A. silvatisus and A. arvensis have shown the interferon-like activity. DOI: http://dx.doi.org/10.5564/mjc.v14i0.197Mongolian Journal of Chemistry 14 (40, 2013, p41-45

  4. Milk proteins-derived bioactive peptides in dairy products: molecular, biological and methodological aspects.

    Science.gov (United States)

    Dziuba, Bartłomiej; Dziuba, Marta

    2014-01-01

    Proteins are one of the primary components of the food, both in terms of nutrition and function. They are main source of amino acids, essential for synthesis of proteins, and also source of energy. Additionally, many proteins exhibit specific biological activities, which may have effect on functional or pro-health properties of food products. These proteins and their hydrolysis products, peptides, may influence the properties of food and human organism. The number of commercially available food products containing bioactive peptides is very low, apart from that milk proteins are their rich source. It could be supposed that number of available products with declared activity will rise in near future because of observed strong uptrend on interest in such products. Molecular and biological properties of milk proteins, as precursors of bioactive peptides was characterised in the work. Therefore, the strategy of research and obtaining of such peptides both in laboratory and industrial scale, as well as the range of their commercial application, was presented. Several examples of research efforts presenting high potential to develop new products containing bioactive peptides from milk proteins and predetermined as nutraceuticals was described.

  5. Current Advances in L-DOPA and DOPA-Peptidomimetics: Chemistry, Applications and Biological Activity.

    Science.gov (United States)

    Bizzarri, Bruno Mattia; Tortolini, Silvia; Rotelli, Luca; Botta, Giorgia; Saladino, Raffaele

    2015-01-01

    L-3,4-Dihydroxyphenylalanine [2-amino-3-(3,4-dihydroxyphenyl) propanoic acid (L-DOPA) is a natural constituent of animal and plant tissue derived from post-translational modification of the amino acid tyrosine. L-DOPA is modified during metabolism to catecholamine neurotransmitters, noradrenaline and adrenaline, which are characterized by different biological activities. L-DOPA has been the first drug of choice in the therapy of Parkinson's disease that is a progressive neurodegenerative disorder involving the loss of dopaminergic neurons of substantia nigra pars compacta. The social and economic impact of these diseases is very high due to the progressive aging of the population. This review focuses on the biological effect of LDOPA, as well as on the synthesis of L-DOPA derivatives and their application in central nervous system diseases. Among them, L-DOPA-containing peptides (L-DOPA-Pep) show important biological and pharmacological activities. For example, L-DOPA analogues of the alpha-factor interact with models of the G protein-coupled receptor, inhibit the oxidation of low-density lipoproteins, and are used for improving L-DOPA absorption in long-term treatment of Parkinson's disease and as skin moisturizer in cosmetic compositions. Moreover, L-DOPA residues in proteins provide reactive tools for the preparation of adhesives and coatings materials. Usually, L-DOPA-Pep is prepared by traditional liquid or solid state procedures starting from simple amino acids. Recently, selective side-chain modifications of pre-formed peptides have also been reported both for linear and branched peptides. Here, we describe the recent advances in the synthesis of L-DOPA and dopa-peptidomimetics and their biological and pharmacological activities, focusing the attention on new synthetic procedures and biological mechanism of actions.

  6. Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors.

    Science.gov (United States)

    Cui, Peng; Tomsig, Jose L; McCalmont, William F; Lee, Sangderk; Becker, Christopher J; Lynch, Kevin R; Macdonald, Timothy L

    2007-03-15

    Autotaxin (ATX) is an autocrine motility factor that promotes cancer cell invasion, cell migration, and angiogenesis. ATX, originally discovered as a nucleotide phosphodiesterase, is known now to be responsible for the lysophospholipid-preferring phospholipase D activity in plasma. As such, it catalyzes the production of lysophosphatidic acid (LPA) from lysophophatidylcholine (LPC). ATX is thus an attractive drug target; small molecular inhibitors might be efficacious in slowing the spread of cancers. With this study we have generated a series of beta-keto and beta-hydroxy phosphonate derivatives of LPA, some of which are potent ATX inhibitors.

  7. Biological evaluation and simple method for the synthesis of tetrahydrobenzo[a]xanthenes-11-one derivatives

    Directory of Open Access Journals (Sweden)

    Ali Akbari

    2017-01-01

    Full Text Available A simple method for the synthesis of Tetrahydrobenzo[a]xanthenes-11-one derivatives in the presence of BF3.SiO2, and its antibacterial activity was assessed against Pseudomonas syringae, Xanthomonas citi and Pectobacterium carotovorum. The structure of the isolated compounds has been determined by means of 1H/13C NMR and FT-IR spectroscopy. The reactions were carried out in water at room temperature for 5 h. This method has some advantages such as good to excellent yield, mild reaction condition, ease of operation and workup, high product purity and green process.

  8. Marine-derived fungi: Source of biologically potent and novel compounds

    Digital Repository Service at National Institute of Oceanography (India)

    Majik, M.S.; Parvatkar, R.R.; Tilvi, S.; Gawas, S.G.

    )-3β-hydroxy-5α,6α,8α,14α-diepoxyergosta- 22-en-7-one (4), both of which displayed weak cytotoxic activity towards the lung cancer cell line A549 [33]. Conformational analysis on the basis of the observed NOEs in the ROESY spectrum indicated... against several cancer cell lines [35]. Moreover, fellutamide C (9) isaderivative of the previously described fellutamides A and B, metabolites of a marine fish-derived Penicillium fellutanum [36], which were not detected in the extract of A. versicolor...

  9. Expression of biologically active murine interleukin-18 in Lactococcus lactis.

    Science.gov (United States)

    Feizollahzadeh, Sadegh; Khanahmad, Hossein; Rahimmanesh, Ilnaz; Ganjalikhani-Hakemi, Mazdak; Andalib, Alireza; Sanei, Mohammad Hossein; Rezaei, Abbas

    2016-11-01

    The food-grade bacterium Lactococcus lactis is increasingly used for heterologous protein expression in therapeutic and industrial applications. The ability of L. lactis to secrete biologically active cytokines may be used for the generation of therapeutic cytokines. Interleukin (IL)-18 enhances the immune response, especially on mucosal surfaces, emphasizing its therapeutic potential. However, it is produced as an inactive precursor and has to be enzymatically cleaved for maturation. We genetically manipulated L. lactis to secrete murine IL-18. The mature murine IL-18 gene was inserted downstream of a nisin promoter in pNZ8149 plasmid and the construct was used to transform L. lactis NZ3900. The transformants were selected on Elliker agar and confirmed by restriction enzyme digestion and sequencing. The expression and secretion of IL-18 protein was verified by SDS-PAGE, western blotting and ELISA. The biological activity of recombinant IL-18 was determined by its ability to induce interferon (IFN)-γ production in L. lactis co-cultured with murine splenic T cells. The amounts of IL-18 in bacterial lysates and supernatants were 3-4 μg mL -1 and 0.6-0.7 ng mL -1 , respectively. The successfully generated L. lactis strain that expressed biologically active murine IL-18 can be used to evaluate the possible therapeutic effects of IL-18 on mucosal surfaces. © FEMS 2016. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

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

    Science.gov (United States)

    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.

  11. Biologically active and biomimetic dual gelatin scaffolds for tissue engineering.

    Science.gov (United States)

    Sánchez, P; Pedraz, J L; Orive, G

    2017-05-01

    We have designed, developed and optimized Genipin cross-linked 3D gelatin scaffolds that were biologically active and biomimetic, show a dual activity both for growth factor and cell delivery. Type B gelatin powder was dissolved in DI water. 100mg of genipin was dissolved in 10ml of DI water. Three genipin concentrations were prepared: 0.1%, 0.2% and 0.3% (w/v). Solutions were mixed at 40°C and under stirring and then left crosslinking for 72h. Scaffolds were obtained by punching 8 mm-cylinders into ethanol 70% solution for 10min and then freeze-drying. Scaffolds were biologically, biomechanically and morphologically evaluated. Cell adhesion and morphology of D1-Mesenchymal stem cells (MSCs) and L-929 fibroblast was studied. Vascular endothelial grwoth factor (VEGF) and Sonic hedgehog (SHH) were used as model proteins. Swelling ratio increased and younǵs module decreased along with the concentration of genipin. All scaffolds were biocompatible according to the toxicity test. MSC and L-929 cell adhesion improved in 0.2% of genipin, obtaining better results with MSCs. VEGF and SHH were released from the gels. This preliminary study suggest that the biologically active and dual gelatin scaffolds may be used for tissue engineering approaches like bone regeneration. Copyright © 2017 Elsevier B.V. All rights reserved.

  12. Synthesis, antimicrobial and antitubercular activities of some novel pyrazoline derivatives

    Directory of Open Access Journals (Sweden)

    Aftab Ahmad

    2016-09-01

    Full Text Available In the present study, two new series of pyrazolines (3a–h & 4a–h were synthesized starting from p-acetamidophenol (paracetamol and evaluated for their antibacterial, antifungal and antitubercular activities. Chalcones (2a–h prepared by condensing 3-acetyl-4-hydroxyphenyl acetamide (1 with different aromatic aldehydes were reacted with phenyl hydrazine and isonicotinic acid hydrazide to obtain phenyl-pyrazolines (3a–h and isoniazid-pyrazolines (4a–h, respectively. The structures of the synthesized compounds were confirmed by spectral and microanalysis studies. Newly prepared pyrazoline compounds exhibited significant antibacterial activity against the organisms Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa when compared with the standard antibiotic Ciprofloxacin. Compound 4g showed potent antibacterial activity against P. aeruginosa and S. aureus (MIC-3.12 μg/mL, however, against E. coli compound 3d, 4c, 4d, 4f & 4g were found to have an MIC of 6.25 μg/mL. Antifungal activity of compound 4d against Candida albicans and Aspergillus niger (MIC-3.12 μg/mL was found to be better than the standard drug Ketoconazole. The results of antitubercular activity of the synthesized compounds against Mycobacterium tuberculosis H37Rv by the agar microdilution method are quite promising. The antitubercular activity of compounds 4c, 4d & 4g (MIC-3.12 μg/mL was found to be superior than that of the reference drug Streptomycin which showed MIC equal to 6.25 μg/mL. It was observed that pyrazolines with chloro, nitro or methoxy substituent showed better activity. Also, the pyrazolines derived from isoniazid (4a–h were found to be better in their antibacterial, antifungal and antitubercular action than those derived from phenyl-hydrazine (3a–h.

  13. Radiopharmacology of iminodiacetic acid N-derivatives analysis in biological models and comparison to human beings

    International Nuclear Information System (INIS)

    Canellas, C.O.; Arguelles, M.G.; Mitta, A.E.A.

    1987-01-01

    It was studied the influence of chemical structures and molecular weight in the distribution of several iminodiacetic acid N-derivatives and to determine the potential use of these radiopharmaceuticals in humans. The study was performed with the following derivatives: N-(2,6 dimetyphenylcarbamoylmethy) iminodiacetic acid, N(2.6 dietylphenyl-carbamoylmethy) iminodiacetic acid, N-(2,6 diisopropylphenylcarbamoylmethy) iminodiacetic acid and the previously unknown N-derivative N-(2,6 diisopropyl, phenylcarbamoylethyl) iminodiacetic aced. These were sinthesized by a modified procedure by MITTA et al. and controlled by NMR, mass spectrometry, elemental composition and also toxicity pirogens, lethal dose and the chelate's radiochemical dose were determined. Liver gallbladder, intestinal and renal kinetics were studied in mice. In order to evaluate the metabolic pathways of the radiopharmaceuticals, the content of gallbladder and the urine were reinjected. Plasma kinetics and the plasmatic half life was determined by extracorporeal circulation in Wistar rats. For the use in human beings, test were carried out in different branches of nuclear medicine, in normal volunteers and carriers of different pathologic disorders. The patients were divided into four groups: acute and chronic cholecystitis, cirrhosis and jaundice. It was obtained the liver/heart activity ratio and estimated the appearance times of the intrahepatic ducts, gallbladder, duodenum and renal persistence. (M.E.L.) [es

  14. Synthesis and Biological Evaluation of Norcantharidin Derivatives Possessing an Aromatic Amine Moiety as Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Yang Wang

    2015-12-01

    Full Text Available Based on the structure of naturally produced cantharidin, different arylamine groups were linked to the norcantharidin scaffold to provide thirty six compounds. Their structures were confirmed by melting point, 1H-NMR, 13C-NMR and HRMS-ESI studies. These synthetic compounds were tested as fungistatic agents against eight phytopathogenic fungi using the mycelium growth rate method. Of these thirty six derivatives, seven displayed stronger antifungal activity than did norcantharidin, seven showed higher activity than did cantharidin and three exhibited more significant activity than that of thiabendazole. In particular, 3-(3′-chloro-phenylcarbamoyl norcantharidate II-8 showed the most significant fungicidal activity against Sclerotinia fructigena and S. sclerotiorum, with IC50 values of 0.88 and 0.97 μg/mL, respectively. The preliminary structure-activity relationship data of these compounds revealed that: (1 the benzene ring is critical for the improvement of the spectrum of antifungal activity (3-phenylcarbamoyl norcantharidate II-1 vs norcantharidin and cantharidin; (2 among the three sites, including the C-2′, C-3′ and C-4′ positions of the phenyl ring, the presence of a halogen atom at the C-3′position of the benzene ring caused the most significant increase in antifungal activity; (3 compounds with strongly electron-drawing or electron-donating groups substitutions were found to have a poor antifungal activity; and (4 compared with fluorine, bromine and iodine, chlorine substituted at the C-3′ position of the benzene ring most greatly promoted fungistatic activity. Thus, compound II-8 has emerged as new lead structure for the development of new fungicides.

  15. Biological variation of homeostasis model assessment-derived insulin resistance in type 2 diabetes.

    Science.gov (United States)

    Jayagopal, Vijay; Kilpatrick, Eric S; Jennings, Paul E; Hepburn, David A; Atkin, Stephen L

    2002-11-01

    Individuals with type 2 diabetes are particularly vulnerable to cardiovascular disease. Insulin resistance is a major determinant of this increased risk and is a potential therapeutic target. This study was undertaken to establish the natural biological variation of insulin resistance in individuals with type 2 diabetes. The biological variation of insulin resistance was assessed by measuring insulin resistance at 4-day intervals on 10 consecutive occasions in 12 postmenopausal women with diet-controlled type 2 diabetes and in 11 weight- and age-matched postmenopausal women without type 2 diabetes. Insulin resistance was derived using the homeostasis model assessment for insulin resistance (HOMA-IR) method. The distribution of HOMA-IR was log Gaussian in the type 2 diabetic study group and Gaussian in the control group. The HOMA-IR in the type 2 diabetic group was significantly greater than that of the control group (mean +/- SD: 4.33 +/- 2.3 vs. 2.11 +/- 0.79 units, P = 0.001). After accounting for analytical variation, the mean intraindividual variation was also substantially greater in the type 2 diabetic group than in the control group (mean 1.05 vs. 0.15, P = 0.001). Consequently, at any level of HOMA-IR, a subsequent sample must increase by >90% or decrease by >47% to be considered significantly different from the first. HOMA-IR is significantly greater and more variable for individuals with type 2 diabetes. Therefore, this inherent variability needs to be accounted for in studies evaluating therapeutic reduction of HOMA-IR in this group.

  16. Antitumor Activity of Fascaplysin Derivatives on Glioblastoma Model In Vitro.

    Science.gov (United States)

    Lyakhova, I A; Bryukhovetsky, I S; Kudryavtsev, I V; Khotimchenko, Yu S; Zhidkov, M E; Kantemirov, A V

    2018-03-01

    Antitumor efficiency of fascaplysin synthetic derivatives (7-phenylfascaplysin, 3-chlorofascaplysin, 3-bromofascaplysin, and 10-bromofascaplysin) was compared out in vitro on C6 glioma cells. The cytotoxic efficiency of all tested compounds was higher than that of unsubstituted fascaplysin; 3-bromofascaplysin and 7-phenylfascaplysin exhibited the best capacity to kill glioma C6 cells. Apoptosis was the main mechanism of glioma cell death. The cytotoxic activity of these compounds increased with prolongation of exposure to the substance and increase of its concentration. Fascaplysin derivatives modified all phases of glioma cell vital cycle. The count of viable tumor cell in G0 phase remained minimum by the end of experiment under the effects of 3-bromofascaplysin and 7-phenylfascaplysin.

  17. Adsorption of Heavy Metals on Biologically Activated Brown Coal Sludge

    Directory of Open Access Journals (Sweden)

    Mária Praščáková

    2005-11-01

    Full Text Available Adsorption of cooper (II and zinc (II ions from aqueous solutions on a biologically activated brown coal sludge was investigated. Four families of adsorbents were prepared from the brown coal sludge bya microorganism’s activity. There were used microscopic fungi such as Aspergillus niger, Aspergillus clavatus, Penicillium glabrum and Trichoderma viride. Prepared sorbents were capable of removing Cu (II and Zn (II. The sorption isotherm has been constructed and the specific metal uptake and the maximum capacity of the adsorbent have been determined.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    2012-10-15

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

  19. Molluscicidal hydroxynaphthoquinones and derivatives: correlation between their redox potentials and activity against Biomphalaria glabrata

    Directory of Open Access Journals (Sweden)

    Lima Nadja M. F.

    2002-01-01

    Full Text Available Several 2-hydroxy-3-alkyl-1,4-naphthoquinones have been submitted to molluscicidal bioassays against the snail Biomphalaria glabrata, intermediate host of Schistosoma mansoni. Cyclic voltammetric studies in aprotic medium (N,N-dimethylformamide plus tetrabutylammonium perchlorate on Hg and glassy carbon electrodes have been performed on these compounds in order to obtain information about their biological mechanism of action. Several of the quinones assayed showed significant molluscicidal activities, and correlation of their activities and electrochemical parameters showed that the first wave reduction potential is an important parameter. The easily reduced quinones (>Ep1c were more active against adult snails and against their egg masses, whilst the 3-methylamino-2-hydroxy derivatives presented higher negative reduction potentials and were not active as molluscicides.

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

    Science.gov (United States)

    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.