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EFFECTS OF INDIVIDUAL GINSENOSIDES, GINKGOLIDES AND FLAVONOIDS ON CYP2C19 AND CYP2D6 ACTIVITY IN HUMAN LIVER MICROSOMES
Author(s) -
He Nu,
Xie HongGuang,
Collins Xavier,
Edeki Timi,
Yan Zhengyin
Publication year - 2006
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1111/j.1440-1681.2006.04445.x
Subject(s) - mephenytoin , microsome , chemistry , quercetin , hydroxylation , cyp2c19 , pharmacology , flavonoid , cyp2d6 , ginkgolides , cyp3a4 , biochemistry , cyp1a2 , enzyme , stereochemistry , cytochrome p450 , biology , ginkgo biloba , antioxidant
SUMMARY1 The 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. 2 Increasing 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 IC 50 values (compound concentration yielding 50% inhibition of a marker enzyme activity), which were estimated by graphical inspection. 3 For CYP2C19, the IC 50 values were 46, 46 and 62 mmol/L for ginsenoside Rd, quercetin and ginsenoside Rb2, respectively, whereas only ginsenoside Rd had an IC 50 value of 57 mmol/L for CYP2D6. 4 The 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.