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1.
An Acad Bras Cienc ; 93(3): e20191432, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34287457

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/farmacologia
2.
J Biochem Mol Toxicol ; 34(2): e22432, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31851403

RESUMO

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/química
3.
Pak J Pharm Sci ; 32(6): 2679-2686, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31969302

RESUMO

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/farmacologia
4.
Iran J Pharm Res ; 17(1): 326-335, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29755563

RESUMO

In this study, the mutagenic and anti-mutagenic effects of methanol extract of three lichen species (Cetraria aculeata, Cladonia chlorophaea and Cetrelia olivetorum) were investigated by using E. coli-WP2, Ames-Salmonella (TA1535 and TA1537) and sister chromatid exchange (SCE) test systems. The results obtained from bacterial test systems demonstrated that methanol extracts of three lichen species have strong anti-mutagenic potencies on TA1535, TA1537 strains and to a lesser extent on E. coli-WP2 strain. The anti-oxidant level of human lymphocytes cells was determined in order to clarify the mechanism underlying the anti-mutagenic effects of these lichen species. Co-treatments of 5, 10 and 20 µg/mL concentrations of these three lichen species with AFB decreased the frequencies of SCE and the level of MDA and increased the amount of SOD, GSH and GPx which decreased by aflatoxin. The findings of this work have clearly demonstrated that Cetraria aculeata, Cladonia chlorophaea and Cetrelia olivetorum have significant anti-mutagenic effects which are thought to be partly due to the anti-oxidant activities and the interaction capability of lichen extracts with mutagen agents (Sodium azide, acridin, N-methyl-N'-nitro-N-nitrosoguanidine and aflatoxin B1).

5.
Toxicol Ind Health ; 31(11): 990-9, 2015 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23589403

RESUMO

For ages, lichens have long been investigated popularly for biological roles, mainly antitumor, antimicrobial and antioxidant activities. Many positive results were obtained in these previous research. Thus, in this study, we aimed to determine whether extracts of Usnea articulata (UAE) and Usnea filipendula (UFE) possessing a protection against aflatoxin B1 (AFB1)-induced genotoxic and oxidative damage. The results of our studies showed that 5 µM concentrations of AFB1 increased the frequencies of sister chromatid exchange (SCE) and the level of malondialdehyde (MDA) and decreased the activities of superoxide dismutase (SOD), glutathione (GSH) and glutathione peroxidase (GPx). However, when 5, 10 and 20 µg/mL concentrations of UAE and UFE was added to AFB1, the frequencies of SCE and MDA level were decreased and SOD, GSH and GPx level were increased. The Ames (Salmonella typhimurium TA1535, TA1537) and WP2 (Escherichia coli) test systems carried out evinced that UAE and UFE possess any mutagenicity, but have antimutagenic effects. Consequently, the results of this experiment have clearly shown that UAE and UFE have strong antioxidative and antigenotoxic effects that are associated with its antioxidant nature. A detailed study can be performed to determine the antioxidant properties of each compound that will extend the use of lichen extracts in food and pharmacy industries.


Assuntos
Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Dano ao DNA/efeitos dos fármacos , Usnea/química , Aflatoxina B1/toxicidade , Escherichia coli/metabolismo , Glutationa/metabolismo , Glutationa Peroxidase/metabolismo , Malondialdeído/metabolismo , Mutagênicos/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Salmonella typhimurium/efeitos dos fármacos , Troca de Cromátide Irmã/efeitos dos fármacos , Superóxido Dismutase/metabolismo
6.
Toxicol Ind Health ; 28(6): 505-12, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21986884

RESUMO

In this study, the antigenotoxic and antioxidant effects of Umbilicaria vellea (UME) and Xantho somloensis (XME) extracts were determined using sister chromatid exchange (SCE), micronuclei (MN) assays, and superoxide dismutase (SOD) and glutathione peroxidase (GPx) activities and malondialdehyde (MDA) levels against the effects of aflatoxin B(1) (AFB(1))-induced oxidative stress and genotoxicity in human lymphocytes in vitro. The results showed that the frequencies of SCE, MN, and MDA level decreased, but the activities of SOD and GPx increased when 5 µg/mL and 10 µg/mL doses of UME and XME were added to AFB(1)-treated cultures. Also the present results indicate that strong antioxidative and the antigenotoxicity mechanisms of UME and XME are associated with its antioxidant nature.


Assuntos
Aflatoxina B1/toxicidade , Antioxidantes/farmacologia , Líquens/química , Linfócitos/efeitos dos fármacos , Adulto , Glutationa Peroxidase/metabolismo , Humanos , Metanol/química , Testes para Micronúcleos , Testes de Mutagenicidade , Mutagênicos/toxicidade , Extratos Vegetais/farmacologia , Troca de Cromátide Irmã/efeitos dos fármacos , Superóxido Dismutase/metabolismo
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