RESUMO
In this study, we aimed to investigate for the first time antimicrobial and antimutagenic activities new two Schiff bases, obtained from a primary amine (p-toluidine, o-toluidine) and an aldehyde (Helicin). Synthesized compounds characterized with elemental analysis, fourier transform infrared spectroscopy, ultraviolet-visible spectrophotometry. 1H-13C nuclear magnetic resonance spectroscopy. Antimutagenic activity was evaluated by micronuclei assay. Antimicrobial activity of Schiff bases have been demonstrated against pathogenic four Gram-positive bacteria (Staphylococcus aureus, Staphylococcus epidermis, Micrococcus luteus, Bacillus cereus) and four Gram-negative bacteria (Pseudumonas aeroginosa, Salmonella typhi H, Brucella abortus, Escherichia coli) and two yeasts (Candida albicans and Saccharomyces cerevisiae). The results showed that both Schiff bases have antimutagenic activity. Especially, high concentration (20 µM) of (E)-2-(hydroxymethyl)-6-(2-((p-tolylimino)methyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triol (Compound I) and (E)-2-(hydroxymethyl)-6-(2-((o-tolylimino)methyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triol (Compound II) have strong antimutagenic activity against aflatoxin B1. On the other hand, both of studied compounds were found effective against pathogenic bacteria and yeasts. Compound I exhibited more activity against P. aeroginosa, S aureus, S.typhi H and C. albicans comparable to Compound II and standard antibiotics. Additionally, Compound II showed better inhibitory activity than Compound I against Candida albicans and Br. Abortus. Therefore, these compounds can be used in phytotherapeutic due to theirs antimutagenic and antimicrobial activities.
Assuntos
Anti-Infecciosos , Bases de Schiff , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Candida albicans , Fungos , Testes de Sensibilidade Microbiana , Bases de Schiff/farmacologiaRESUMO
New polymeric microspheres containing azomethine (1a-1c and 2a-2c) were synthesized by condensation to compare the enzymatic properties of the enzyme glucose oxidase (GOx) and to investigate antimutagenic and antimicrobial activities. The polymeric microspheres were characterized by elemental analysis, infrared spectra (FT-IR), proton nuclear magnetic resonance spectra, thermal gravimetric analysis, and scanning electron microscopy analysis. The catalytic activity of the glucose oxidase enzyme follows Michaelis-Menten kinetics. Influence of temperature, reusability, and storage capacity of the free and immobilized glucose oxidase enzyme were investigated. It is determined that immobilized enzymes exhibit good storage stability and reusability. After immobilization of GOx in polymeric supports, the thermal stability of the enzyme increased and the maximum reaction rate (Vmax ) decreased. The activity of the immobilized enzymes was preserved even after 5 months. The antibacterial and antifungal activity of the polymeric microspheres were evaluated by well-diffusion method against some selected pathogenic microorganisms. The antimutagenic properties of all compounds were also examined against sodium azide in human lymphocyte cells by micronuclei and sister chromatid exchange tests.
Assuntos
Anti-Infecciosos/farmacologia , Antimutagênicos/farmacologia , Candida albicans/efeitos dos fármacos , Enzimas Imobilizadas/farmacocinética , Glucose Oxidase/farmacocinética , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Microesferas , Compostos Azo/química , Células Cultivadas , Enzimas Imobilizadas/química , Feminino , Glucose Oxidase/química , Voluntários Saudáveis , Humanos , Concentração de Íons de Hidrogênio , Linfócitos/efeitos dos fármacos , Linfócitos/metabolismo , Masculino , Testes para Micronúcleos , Microscopia Eletrônica de Varredura , Troca de Cromátide Irmã/efeitos dos fármacos , Azida Sódica/efeitos adversos , Azida Sódica/farmacologia , Temperatura , Tiossemicarbazonas/químicaRESUMO
An efficient and versatile synthesis method has been postulated for hydroxymethylated rac- and meso-cyclohexanoid derivatives. The synthesis of these stereoisomers was achieved easily with traditional methods using hexahydroisobenzofuran 6, prepared from commercially available cis-hydrophthalic anhydride. The study, involving diastereoselective epoxidation and cis-hydroxylation, was conducted to obtain epoxy-, cis-, and trans-diol-furans 7, 8, and 9. After sulfamic acid-catalyzed ring-opening reaction of the epoxide and furan rings, rac- and meso-tetraacetates 14, 15, and 16 were afforded. Hydrolysis of acetate groups with ammonia in absolute methanol yielded the desired tetrols rac-17, meso-18, and meso-19. All structures, after purification by chromatographic methods and elucidation by spectral techniques, were screened against α- and ß-glucosidases. Compounds 7, 8, 10, 17, 18, and 19 were also evaluated for their antibacterial and antifungal activity against some selected synthesized compounds with varying degrees of inhibitory effects on the growth of different pathogenic microorganisms by the well-diffusion method. In addition, Saccharomyces cerevisiae α-glucosidase molecular modeling studies were performed for all rac- and meso-compounds 7, 8, 10, 17, 18, and 19.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Cicloexanos/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Simulação de Acoplamento Molecular , alfa-Glucosidases/metabolismo , Antibacterianos/síntese química , Antibacterianos/química , Antifúngicos/síntese química , Antifúngicos/química , Candida albicans/efeitos dos fármacos , Cicloexanos/síntese química , Cicloexanos/química , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Saccharomyces cerevisiae/enzimologia , Estereoisomerismo , Relação Estrutura-AtividadeRESUMO
The aim of this study is to investigate for the first time in vitro antimicrobial and antimutagenic activities of Schiff bases included the azomethine group. Antimutagenic activity was evaluated by micronucleus (MN) assay. These group have been examined for antibacterial activity against pathogenic strains, Staphylococcus aureus, Escherichia coli, Salmonella typhi H, Brucella abortus, Micrococcus luteus, Bacillus cereus, Pseudomonas aeroginosa and antifungal activity against Candida albicans and Saccharomyces cerevisiae. The results of MN showed that Schiff bases ((E)-N-(4-chlorophenyl)-1-(5-nitrothiophen-2-yl)methanimine ; (E)-N-(2,4-dichlorophenyl)-1-(5-nitrothiophen-2-yl) methanimine) different concentrations decreased the toxic effects of Aflatoxin B1. Especially, high concentration (20µM) of (E)-N-(4-chlorophenyl)-1-(5-nitrothiophen-2-yl)methanimine (compound 1) has strong antimutagenic activity. In our in vitro test systems, it was observed that Schiff bases had antimutagenic effects on human lymphocytes. On the other hand these compounds were also found to possess antimicrobial activity against some test bacteria and yeast. The antimicrobial test results of these Schiff bases included the azomethine group exhibited better activity than some known antibiotics. In particular, Compound 1 were more potent bactericides than all of the substances synthesized. In conclusion, this Schiff bases included the azomethine group can be use pharmacy industries as recognized with their noncytotoxic, antimicrobial and antimutagenic features.
Assuntos
Anti-Infecciosos/síntese química , Antimutagênicos/síntese química , Bases de Schiff/síntese química , Tiofenos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Bacillus cereus/efeitos dos fármacos , Brucella abortus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Escherichia coli/efeitos dos fármacos , Humanos , Linfócitos/efeitos dos fármacos , Micrococcus luteus/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Saccharomyces cerevisiae/efeitos dos fármacos , Salmonella typhi/efeitos dos fármacos , Bases de Schiff/química , Bases de Schiff/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Tiofenos/química , Tiofenos/farmacologiaRESUMO
In this paper, eight novel α-N-heterocyclic thiosemicarbazone complexes were synthesized in search of new biologically active compounds, and characterized via organic elemental analysis, nuclear magnetic resonance spectroscopy, infrared spectra, thermogravimetric analysis, ultraviolet-visible spectroscopy, molar conductance and magnetic susceptibility measurements. The in vitro antimicrobial activity of these complexes was examined against ten disease-causing pathogens: Gram-positive bacteria (Micrococcus luteus ATCC9341, Staphylococcus epidermidis ATCC12228, Bacillus cereus RSKK863) and Gram-negative bacteria (Pseudomonas aeroginosa ATCC27853, Klebsiella pneumonia ATCC27853, Enterobacter aerogenes ATCC51342, Salmonella typhi H NCTC9018394, Shigella dysenteria NCTC2966, Proteus vulgaris RSKK96026) and yeast (Candida albicans Y-1200-NIH). The results revealed that the α-N-heterocyclic thiosemicarbazone compounds showed potent activity. It was observed that all thiosemicarbazone complexes were more susceptible to Gram-negative strains based on the presence of an electron-withdrawing substituent (-Br/-Cl/-F). It was determined that thiosemicarbazone Cu2+complexes showed stronger antifungal effects.
RESUMO
Co3O4 nanoparticles (NPs) were formed using hydrothermal synthesis method and various surfactants to study the effect of changing surface morphology on catalytic and antibacterial activities. FT-IR, TEM, SEM, BET, XRD, and XPS analyses were performed to characterize the NPs. It was observed that as the morphology of Co3O4 changes, it creates differences in the reduction efficiency of organic dyes and p-nitrophenol (p-NP), which are toxic to living organisms and widely used in industry. The reaction rate constants (Kapp) for Co3O4-urea, Co3O4-ed, and Co3O4-NaOH in the reduction of p-NP were found to be 1.86 × 10-2 s-1, 1.83 × 10-2 s-1, and 2.4 × 10-3 s-1, respectively. In the presence of Co3O4-urea catalyst from the prepared nanoparticles, 99.29% conversion to p-aminophenol (p-AP) was observed, while in the presence of the same catalyst, 98.06% of methylene blue (MB) was removed within 1 h. The antibacterial activity of Co3O4 particles was compared with five standard antibiotics for both gram-positive and gram-negative bacteria. The results obtained indicate that the antimicrobial activity of the synthesized Co3O4 particles has a remarkable inhibitory effect on the growth of various pathogenic microorganisms. The current work could be an innovative and beneficial search for both biomedical and wastewater treatment applications.
Assuntos
Antibacterianos , Nanopartículas , Antibacterianos/farmacologia , Espectroscopia de Infravermelho com Transformada de Fourier , Bactérias Gram-Negativas , Bactérias Gram-Positivas , UreiaRESUMO
Heads of sunflower (Helianthus annuus L.) were first biodegraded at 55 degrees C by their microflora. Biodegradation products of sunflower heads (BPSH) were analyzed. They were found to contain 9.77% dry matter, 3.98% total ash, 3.18% crude protein and 5.75% total organic matter. BOD load was determined as 4.80 g/100 g. Subsequently, the effects of BPSH at various concentrations (1.0%, 2.5%, 10% and 100%) on the seed germination and some growth parameters of Phaseolus vulgaris L., Cicer arietinum L. and Triticum vulgare L. were investigated. The percentages of seed germination and germination index of seeds were similar between the control and 1.0% and 2.5% BPSH groups, but these values decreased at higher concentrations. On the other hand, growth of the seedlings gradually increased up to a concentration of 10% BPSH and decreased at 100% concentration. As a result, at concentrations up to 10% the product was found to be beneficial for growth of plants.
Assuntos
Agricultura/métodos , Produtos Agrícolas/crescimento & desenvolvimento , Flores/metabolismo , Helianthus/metabolismo , Biodegradação Ambiental , Flores/química , Germinação/fisiologia , Helianthus/químicaRESUMO
The present study is focused on evaluating the antimutagenic properties of Schiff bases and Mn(III) complexes with L-Threonine, L-Serine and L-Tyrosine, which have antimicrobial activity. These six compounds were investigated for antimutagenic properties against Aflatoxin Bi (AFBi) by the micronucleus (MN) assay in a human lymphocyte cell culture in vitro. The protective role of these compounds against AFBi-induced MN is probably related to its doses. A mechanism has been proposed to reduce the effect of AFBi.
Assuntos
Aflatoxina B1 , Antibacterianos , Antídotos , Compostos Azo , Manganês , Serina , Tiossemicarbazonas , Treonina , Tirosina , Aflatoxina B1/antagonistas & inibidores , Aflatoxina B1/toxicidade , Antibacterianos/química , Antibacterianos/farmacologia , Antídotos/química , Antídotos/farmacologia , Compostos Azo/química , Compostos Azo/farmacologia , Bactérias/crescimento & desenvolvimento , Feminino , Humanos , Masculino , Manganês/química , Manganês/farmacologia , Serina/química , Serina/farmacologia , Tiossemicarbazonas/química , Tiossemicarbazonas/farmacologia , Treonina/química , Treonina/farmacologia , Tirosina/química , Tirosina/farmacologiaRESUMO
This study was conducted to evaluate the antimutagenic and antimicrobial activities of Schiff bases attached L-glutamine and L-asparagine. Antibacterial activities of the compounds against S. aureus, Sh. dys. typ 7, L. monocytogenes 4b, E. coli, S. typhi H, S. epidermis, Br. abortus, M. luteus, B. cereus, P. putida, and antifungal activity against Candida albicans were studied. These compounds were investigated for antimutagenic properties against Aflatoxin Bi (AFBi) using micronuclei (MN) assay in human lymphocyte cell culture in vitro. The protective role of these compounds against AFBi-induced MN is probably related to its doses.
Assuntos
Asparagina/química , Asparagina/farmacologia , Glutamina/química , Glutamina/farmacologia , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Antimutagênicos/química , Antimutagênicos/farmacologia , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Feminino , Humanos , Linfócitos/efeitos dos fármacos , Linfócitos/metabolismo , Masculino , Manganês/química , Testes para Micronúcleos , Bases de Schiff/químicaRESUMO
A new amine containing selenium and their five imine, (SeSchX)(X: -H, F, Cl, Br, CH3), and Ni (II) complexes, [Ni(SeSchX)(H2O)2]Cl/[Ni(SeSchCl)(H2O)Cl], were synthesized. The compounds were characterized by means of elemental analyses, (13)C and (1)H NMR (for imine), FT-IR, UV-Visible spectroscopy, TGA/DTA and elemental analyses. [Ni(SeSchCl)(H2O)Cl] complex from Ni(II) complexes changes color from yellow to orange in the range pH 5-7. [Ni(SeSchCl)(H2O)Cl] complex has ligand-to-metal charge-transfer (LMCT) transitions in the basic medium. Excitation characteristics and energetic of [Ni(SeSchCl)(H2O)Cl] complex, examined via TD-DFT calculations, reveals transitions of LMCT and πâπ(*) character that matches the experimental values. [Ni(SeSchCl)(H2O)Cl] complex showed the highest antibacterial activity when compared to other complexes reported in this work.