Effect of natural and structurally modified bile acids on cholesterol metabolizing enzymes in rat liver microsomes. II.
Articolo
Data di Pubblicazione:
1991
Citazione:
Effect of natural and structurally modified bile acids on cholesterol metabolizing enzymes in rat liver microsomes. II. / E. De Fabiani, M. Crestani, L. Fasoli, E. Bosisio. - In: CHEMISTRY AND PHYSICS OF LIPIDS. - ISSN 0009-3084. - 57:1(1991), pp. 97-101.
Abstract:
The effect of ursodeoxycholic acid analogues bearing modifications at the side-chain moiety of the molecule was tested on cholesterol 7 alpha-hydroxylase and HMG-CoA reductase in rat liver microsomes. The compounds included 23 R,S mixture and the single isomers 23R and 23S of 23 methylursodeoxycholic acid (23-methyl UDCA), the isomeric mixture (cis + trans) of 3 alpha,7 beta-dihydroxy-20,22-methylen-5 beta-cholan-23-oic acid (norcypro-UDCA) and the corresponding single isomers. Each steroid was added to liver microsomes as the sodium salt, at concentrations ranging from 25 to 200 microM. Isomers 23R and 23S of 23-methyl-UDCA inhibited cholesterol 7 alpha-hydroxylase in a concentration-dependent manner. The inhibitory capacity was similar for the two isomers. The extent of inhibition of the analogues was greater than that of the parent compound UDCA. Shortening of the side-chain in norcypro-UDCA resulted in a partial loss of the inhibitory effect, as compared to cypro-UDCA (3 alpha,7 beta-dihydroxy-22,23-methylen-5 beta-cholan-24-oic acid). None of these bile acid derivatives affected the activity of the enzyme HMG-CoA reductase
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
bile acid analogues; cholesterol 7α-hydroxylase; HMGCoA reductase; liver microsomes
Elenco autori:
E. De Fabiani, M. Crestani, L. Fasoli, E. Bosisio
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