Influence of simvA glyzin on expression and inhibition of hmg-coa reductase in rats liver

Autor: Yu. I. Ragino, V. A. Vavilin, E. M. Stakhneva, N. F. Salakhutdinov, O. G. Safronova, A. B. Shintyapina, V. V. Lyakhovich, Yu. P. Nikitin
Jazyk: ruština
Rok vydání: 2015
Předmět:
Zdroj: Атеросклероз, Vol 11, Iss 2, Pp 14-19 (2015)
Druh dokumentu: article
ISSN: 2078-256X
Popis: Activity, level of protein and mRNA HMG-CoA reductase were investigated in rats liver treated with simvastatin (SV), its complex compound with glycyrrhizic acid – simvaglyzin (SVG) and glycyrrhizic acid alone. Level of protein HMG-CoA reductase was reduced on 25 % in SVG group (р < 0.05) 24 hours after introduction the last dose. Level of mRNA was significantly increased in experimental group in compared to control. In vitro SVG was uncompetitive inhibitor of HMG-CoA reductase (Ki = 94 nM). SVG gain the inhibitor properties following cytochrome P450-dependent metabolism. The addition of 1mM methyrapone in incubation medium fully prevented the inhibition of 3-HMG-CoA reductase. SV and SVG in concentrations of 300 nM inhibited of mevalonate synthesis rate by 39.15 ± 8.27 % and 38.85 ± 3.04 %, respectively.
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