Title : In vitro and in vivo inhibitory effects of glycyrrhetinic acid on cytochrome P450 3A activity.

Pub. Date : 2010

PMID : 21042038






5 Functional Relationships(s)
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1 In vitro and in vivo inhibitory effects of glycyrrhetinic acid on cytochrome P450 3A activity. Glycyrrhetinic Acid cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 We have assessed the ability of GA to inhibit the enzyme cytochrome P450 3A (CYP3A). Glycyrrhetinic Acid cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 We have assessed the ability of GA to inhibit the enzyme cytochrome P450 3A (CYP3A). Glycyrrhetinic Acid cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 A Lineweaver-Burk plot showed that GA was a mixed inhibitor of CYP3A, with an IC50 of 7.25 mumol/l, a K(m) of 4.3 mumol/l and a K(i) of 6.4 mumol/l by non-linear regression analysis. Glycyrrhetinic Acid cytochrome P450 family 3 subfamily A member 4 Homo sapiens
5 CYP3A activity was also affected by intragastric administration of GA, which resulted in increases in area under the plasma concentration-time curve (AUC)(0-t) and in apparent elimination half-time (t1/2) and significant decreases in body clearance, as well as in the formation of 1-hydroxy-midazolam after intragastric or intravenous administration of midazolam (p < 0.05). Glycyrrhetinic Acid cytochrome P450 family 3 subfamily A member 4 Homo sapiens