RESUMO
1,4-Dihydropyridine derivatives possess various physiological activities but their mechanism of membranotropic action is not completely investigated yet. We have examined the membranotropic effects of 4-beta-pyridyl-1,4-Dihydropyridine derivatives containing different length alkyl chain substituent at N-quaternised 4-beta-pyridyl moiety. The results show the relation between incorporation of 1,4-dihydropyridine derivatives in the liposomal membranes and influence on bilayer fluidity. The compound with hexadecyl (C16H33) substituent in the 4-beta-pyridyl moiety possess the most pronounced incorporation ability and fluidizing effect. This compound causes the remarkable release of fluorescent probe calcein from liposomes and induces the hemolysis of human erythrocytes as well. The obtained results suggest that the length of alkyl chain at quaternized 4-beta-pyridyl moiety is significant for the expression of membranotropic effects of tested compounds.
Assuntos
Di-Hidropiridinas/farmacologia , Membrana Eritrocítica/efeitos dos fármacos , Lipossomos , Fluidez de Membrana/efeitos dos fármacos , 1,2-Dipalmitoilfosfatidilcolina , Di-Hidropiridinas/química , Membrana Eritrocítica/fisiologia , Fluoresceínas/metabolismo , Corantes Fluorescentes/metabolismo , Hemólise , Humanos , Bicamadas Lipídicas , Espectrometria de Fluorescência , Relação Estrutura-AtividadeRESUMO
The 1,4-dihydropyridine (1,4-DHP) and 1,4-dihydroindeno[1,2-b]pyridine (1,4-DHIP) derivatives were investigated as glutathione S-transferase (GT) inhibitors. The obtained results indicate that some of the 1,4-DHP's containing lipophylic and bulky substituents have inhibitory effects on GT in vitro. The derivatives of 1,4-DHIP are more pronounced inhibitors.
Assuntos
Di-Hidropiridinas/farmacologia , Glutationa Transferase/antagonistas & inibidores , Piridinas/farmacologia , Animais , Bovinos , Fígado/enzimologiaRESUMO
Cardiovascular drugs nifedipine and riodipine (1,4-dihydropyridine derivatives) were studied as to their effect on some biochemical characteristics of erythrocytes. Both compounds failed to effect 2,3-diphosphoglycerate concentration in intact erythrocytes, but slightly decreased the level of adenosinetriphosphate. The drugs inhibited the process of acid hemolysis, this inhibition being particularly manifest in the case of nifedipine.
