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1.
J Oleo Sci ; 69(10): 1273-1280, 2020 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-32908102

RESUMO

The study involved the isolation and identification of a member of Streptomyces griseorubens and the identification of its secondary metabolite content. Two extract samples were prepared by using butanol and chloroform. In the analyses of the extracts TLC, FT-IR, and GC-MS were employed. Butanol extract appeared to be dominated by three different pyrrole compounds (43.59%), while two fatty acids, linoleic- and erucic acids, were the most abundant secondary metabolites in the chloroform extract, 27.57% and 12.34%, respectively. Pyrrolo[1,2-a]pyrazine-1,4-dione, hexahydro-compound was represented by a single and distinct band on the thin layer chromatography plate. In GC-MS spectra, it also constituted 13.50% of the butanol extract.


Assuntos
Produtos Biológicos/química , Produtos Biológicos/isolamento & purificação , Ácido Linoleico/análise , Pirróis/análise , Streptomyces/química , Streptomyces/metabolismo , Butanóis , Cromatografia em Camada Fina , Ácidos Erúcicos/análise , Cromatografia Gasosa-Espectrometria de Massas , Streptomyces/isolamento & purificação
2.
J Biochem Mol Toxicol ; : e22239, 2018 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-30368973

RESUMO

The 1,2,4-triazole and its derivatives were reported to exhibit various pharmacological activities such as antimicrobial, analgesic, anti-inflammatory, antitumoural, cytotoxic, and antioxidant properties. In this study, a series of triazole compounds (M1-M10) were evaluated for some biological activities. In vitro qualifications of these compounds on acetylcholinesterase (AChE) and human carbonic anhydrase enzyme activities were performed. Also, their antitumoral activities in human colon cancer (HT29) cell line cultures were examined. In addition, colon cancer experimentation was induced in rats by an in vivo method, and the in vivo anticancer effects of triazole derivatives were investigated. Also, the effects of these derivatives in levels of antioxidant vitamin A, vitamin E, and MDA were studied in rat liver and blood samples. Most of the compounds were found to exhibit significant antioxidant and antitumoral activities. All the compounds had cytotoxic activities on HT29 cell lines with their IC50 values lower than 10 µM concentrations. The low IC 50 values of the compounds are M1 (3.88 µM), M2 (2.18 µM), M3 (4.2 µM), M4 (2.58 µM), M5 (2.88 µM), M6 (2.37 µM), M7 (3.49 µM), M8 (4.01 µM), M9 (8.90 µM), and M10 (3.12 µM).

3.
J Biochem Mol Toxicol ; 32(1)2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28960668

RESUMO

In this study, carbonic anhydrase (CA) enzyme was purified and characterized from blood samples of Kangal Akkaraman sheep and inhibitory properties on certain antibiotics were examined. CA purification was composed of preparation of the hemolysate and conducting the Sepharose-4B-tyrosine-sulfanilamide affinity gel chromatography in having specific activity of 11626 EU mg-1 , yield of 14.40%, and 242.76-fold purification. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis was performed to assess the enzyme purity and a single band was observed. Some antibiotics were exhibited in vitro inhibition on the CA activity. IC50 values of these inhibitors were calculated by plotting activity percentage. IC50 values of certain drugs (dexamethasone; caffeine; metamizole sodium; tetramisol; ceftiofur HCl; ivermectin; tavilin 50; penokain G; neosym; and sulfamezathine) were found as 0.38, 8.24, 285.53, 114.77, 5.33, 2.76, 27.58, 213.50, 208.28, and 36.60 µM, respectively. Ki values of different drugs on Kangal Akkaraman sheep blood CA activity were found in the range of 0.21 ± 0.038-266.64 ± 37.11 µM.


Assuntos
Antibacterianos/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Anidrases Carbônicas/metabolismo , Animais , Animais Endogâmicos , Antibacterianos/química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Ligação Competitiva , Cafeína/química , Cafeína/farmacologia , Inibidores da Anidrase Carbônica/química , Anidrases Carbônicas/química , Anidrases Carbônicas/isolamento & purificação , Estimulantes do Sistema Nervoso Central/química , Estimulantes do Sistema Nervoso Central/farmacologia , Dexametasona/química , Dexametasona/farmacologia , Eritrócitos/enzimologia , Cinética , Estrutura Molecular , Peso Molecular , Carneiro Doméstico , Turquia
4.
J Biochem Mol Toxicol ; 32(1)2018 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29131470

RESUMO

Some novel derivatives of thiosemicarbazide and 1,2,4-triazole-3-thiol were synthesized and evaluated for their biological activities. The title compounds were prepared starting from readily available pyridine-2,5-dicarboxylic acid. The reaction carboxylic acid with absolute ethanol afforded the corresponding dimethyl pyridine-2,5-dicarboxylate (1). The reaction of dimethyl-2,5-pyridinedicarboxylate (1) with hydrazine hydrate good yielded pyridine-2,5-dicarbohydrazide (2). Refluxing compound 2 with alkyl/aryl isothiocyanate derivatives for 3-8 h afforded 1,4-disubstituted thiosemicarbazides (3a-e). Base-catalyzed intra-molecular dehydrative cyclization of these intermediates furnished the 4,5-disubstituted bis-mercaptotriazoles (4a-e) in good yield (85%-95%). Among the target compounds, 2,2'-(pyridine-2,5-diyldicarbonyl)bis[N-(p-methoxyphenyl)hydrazinecarbothioamide] (3c) showed very high activity with value of 72.93% against 1,1-diphenyl-2-picrylhydrazyl free radical at the concentration of 25 µg/mL. The inhibitory effects of the target compounds against acetylcholinesterase (AChE), hCA I, and II were studied. AChE, cytosolic hCA I and II isoforms were potently inhibited by synthesized these derivatives with Ki s in the range of 3.07 ± 0.76-87.26 ± 29.25 nM against AChE, in the range of 1.47 ± 0.37-10.06 ± 2.96 nM against hCA I, and in the range of 3.55 ± 0.57-7.66 ± 2.06 nM against hCA II, respectively.


Assuntos
Antioxidantes/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Colinesterase/farmacologia , Nootrópicos/farmacologia , Piridinas/farmacologia , Tiossemicarbazonas/farmacologia , Triazóis/farmacologia , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Antioxidantes/síntese química , Antioxidantes/química , Anidrase Carbônica I , Inibidores da Anidrase Carbônica/síntese química , Inibidores da Anidrase Carbônica/química , Anidrases Carbônicas/química , Anidrases Carbônicas/isolamento & purificação , Anidrases Carbônicas/metabolismo , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Desenho de Fármacos , Humanos , Quelantes de Ferro/síntese química , Quelantes de Ferro/química , Quelantes de Ferro/farmacologia , Isoenzimas/antagonistas & inibidores , Isoenzimas/isolamento & purificação , Isoenzimas/metabolismo , Cinética , Estrutura Molecular , Nootrópicos/síntese química , Nootrópicos/química , Piridinas/síntese química , Piridinas/química , Relação Estrutura-Atividade , Tiossemicarbazonas/síntese química , Tiossemicarbazonas/química , Temperatura de Transição , Triazóis/síntese química , Triazóis/química
5.
J Biochem Mol Toxicol ; 31(11)2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28833991

RESUMO

The aim of this study was to evaluate biologically active novel molecules having potentials to be drugs by their antitumor properties and by activities of apoptotic caspase and topoisomerase. Following syntheses of novel eight bis(α-aminoalkyl)phosphinic acid derivatives (4a-h) as a result of array of reactions, compounds were evaluated by cytotoxic effects in vitro on human breast cancer (MCF-7) and normal endothelial (HUVEC) cell lines. All phosphinic acid derivatives were effective for cytotoxicity on both MCF-7 and HUVEC lines, while 4c, 4e, and 4f compounds were found significantly more effective. For the evaluation of antitumor properties of compounds in a highly sensitive method, their effects on inhibiting topoisomerases I and II were investigated. Also, some of the bis(α-aminoalkyl)phosphinic acid derivatives (4a, 4e-h) showed nice inhibitory action against acetylcholinesterase and human carbonic anhydrase isoforms I and II.


Assuntos
Antineoplásicos/farmacologia , Inibidores da Anidrase Carbônica/farmacologia , Inibidores da Colinesterase/farmacologia , Inibidores da Topoisomerase I/farmacologia , Inibidores da Topoisomerase II/farmacologia , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Neoplasias da Mama/tratamento farmacológico , Inibidores da Colinesterase/química , DNA Topoisomerases Tipo I/metabolismo , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Células Endoteliais da Veia Umbilical Humana , Humanos , Células MCF-7 , Ácidos Fosfínicos/química , Inibidores da Topoisomerase I/química , Inibidores da Topoisomerase II/química
6.
Pak J Pharm Sci ; 29(5 Suppl): 1853-1862, 2016 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28476714

RESUMO

Aminophosphinic acids which are organophosphorus compounds widely investigated for potential production of antibacterial, antitumor and antiviral materials. In vitro antioxidant, cytotoxic and antimicrobial activities of synthesized novel compounds of 8 different bis(ß-amino alkyl)phosphinic acids (4a-h) were investigated on MCF-7 breast adenocarcinoma cell and human umbilical vein endothelial cell (HUVEC) cultures. Malondialdehyde (MDA) levels were evaluated as an indication of lipid peroxidation in cell cultures for antioxidant capacities. In vitro antioxidant activities in cell cultures were determined by evaluating totals of antioxidant, oxidant, thiol levels and activities of paraoxanase, aryl esterase. It was found that 4c compound reduced MDA level significantly while 4a and 4g compounds increased MDA levels significantly compared to control. 4c compound was found most effective in reducing MDA levels by neutralizing reactive oxygen species to prevent cell damage while compounds 4c, 4f and 4h were found presenting adequate activity with other antioxidants. In vitro anti-proliferation was evaluated on MCF-7 and HUVEC cells using XTT to investigate anti-cancer potentials as therapeutics. Compounds 4c, 4e and 4f were exhibited better compared to others. Most compounds were found cytotoxic to both MCF-7 and HUVECs. Antimicrobial and antifungal activities were investigated by disc diffusion and compared to MICs of Gentamycin and Nystatin.


Assuntos
Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Ácidos Fosfínicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Células Endoteliais da Veia Umbilical Humana , Humanos , Células MCF-7 , Malondialdeído/metabolismo , Ácidos Fosfínicos/química
7.
Pak J Pharm Sci ; 28(3 Suppl): 1141-50, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26051736

RESUMO

Ability to taste Phenylthiocarbamide (PTC) a bitter molecule, is usually used to know the heritable characteristic in both genetic and physiological studies. So far, no research has yet attested whether PTC blindness relation with obesity and some nutrition behaviors of human. This study is the first attempt on a large scale to examine PTC sensitivity in healthy and overweight people in Turkish population to define in the perception of bitter senses which is associated with nutrition habits, body mass index, age, gender, and to be in stable weight. PTC taste perception was measured by tasting PTC solution filtered in a paper. The results showed that tasters were significantly more frequent (81,8%) than nontasters (18,2%) in all population. A higher proportion of nontasters were observed in the quite fat individual group (BMI >40kg/m(2)). Alterations explained these differences in basic taste sensitivity, age, gender, BMI, individuals' family obesity situations, vegetarian nourishment. Increased frequency of nontasters allele is evident with obesity condition. This could be due to lack of preference for nutrition among nontasters. So the phenotypic variation in PTC sensitivity is genetic in origin; it may represent an association with obesity, dietary habits, regular weight, gender, and age.


Assuntos
Comportamento Alimentar , Obesidade/genética , Feniltioureia/administração & dosagem , Percepção Gustatória/genética , Adolescente , Adulto , Fatores Etários , Idoso , Índice de Massa Corporal , Feminino , Estudos de Associação Genética , Marcadores Genéticos , Predisposição Genética para Doença , Humanos , Masculino , Pessoa de Meia-Idade , Estado Nutricional/genética , Obesidade/fisiopatologia , Obesidade/psicologia , Fenótipo , Fatores de Risco , Fatores Sexuais , Turquia , Aumento de Peso/genética , Adulto Jovem
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