EFFECTS OF INDIVIDUAL GINSENOSIDES, GINKGOLIDES AND FLAVONOIDS ON CYP2C19 AND CYP2D6 ACTIVITY IN HUMAN LIVER MICROSOMES
Version of Record online: 10 AUG 2006
Clinical and Experimental Pharmacology and Physiology
Volume 33, Issue 9, pages 813–815, September 2006
How to Cite
He, N., Xie, H.-G., Collins, X., Edeki, T. and Yan, Z. (2006), EFFECTS OF INDIVIDUAL GINSENOSIDES, GINKGOLIDES AND FLAVONOIDS ON CYP2C19 AND CYP2D6 ACTIVITY IN HUMAN LIVER MICROSOMES. Clinical and Experimental Pharmacology and Physiology, 33: 813–815. doi: 10.1111/j.1440-1681.2006.04445.x
- Issue online: 10 AUG 2006
- Version of Record online: 10 AUG 2006
- Received 31 October 2005; revision 15 February 2006; accepted 6 March 2006.
- herb–drug interactions;
- human liver microsome;
- 1The effects of four individual ginsenosides (Rb1, Rb2, Rc and Rd), two ginkgolides (A and B) and one flavonoid (quercetin) on CYP2C19-dependent S-mephenytoin 4¢-hydroxylation and CYP2D6-mediated bufuralol 1¢-hydroxylation were evaluated in human liver microsomes.
- 2Increasing concentrations of each test compound were added to microsomal incubation mixtures containing a well-characterized marker substrate (S-mephenytoin for CYP2C19 or bufuralol for CYP2D6) to determine their IC50 values (compound concentration yielding 50% inhibition of a marker enzyme activity), which were estimated by graphical inspection.
- 3For CYP2C19, the IC50 values were 46, 46 and 62 mmol/L for ginsenoside Rd, quercetin and ginsenoside Rb2, respectively, whereas only ginsenoside Rd had an IC50 value of 57 mmol/L for CYP2D6.
- 4The data suggest that the tested compounds are not likely to inhibit the metabolism of the concurrent use of a given drug whose primary route of elimination is through CYP2C19 or CYP2D6.