Subject Area物理化学
Screening Study of the Inhibitory Effects 17 Steroids on 6 Major Cytochrome P450 Isoenzymes
Zhang JW(张江伟); Liu Y(刘勇); Li W(李巍); Yang L(杨凌)
Conference NameThe 1st asia Pacific ISSX Meeting
Conference Date2001-5-24
Conference Place韩国
AbstractObjective: To screen the inhibitory effects of 17 steroids on 6 major cytochrome P450 (CYP) isoenzymes. Methods: The inhibitory effects of 17 steroids at 100 μM (25 μM for estrone) were tested towards 6 major CYPs including CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1 and CYP3A4. 17 steroids included aldosterone, androstenedione, corticosterone, cortisol, dehydroepiandrosterone, 11-deoxycortisol, dexamethasone, estrone, 17α-hydroxyprogesterone, medroxyprogesterone, megestrol acetate, methylprednisolone, methyltestosterone, prednisolone, prednisone, pregnenolone and testosterone. Results: Of these isoforms tested, CYP3A4 was most affected; nearly all the 17 steroids inhibited it in certain degree. Dehydroepiandrosterone and methylprednisolone were strongest inhibitors of all steroids tested; CYP3A4 activity was strongly inhibited by 62.9% and 61.9% respectively. Cortisol, estrone and corticosterone also inhibited CYP3A4 activity by more than 50%; the activity was inhibited by 57.4%, 53.0% and 52.4% respectively. CYP2C9 and were moderately inhibited, the strongest inhibition was observed by 100 μM corticosterone, 47.1% of the orginal activity was inhibited. The activity of CYP2C9 was inhibited by dehydroepiandrosterone by 29.9%, methylprednisolone by 26.7%, megestrol acetate by 21.3%. CYP2A6 and CYP2D6 were the least inhibited. Interestingly, several steroids showed certain degree of activation toward CYP2E1, including androstenedione, estrone (25 μM), medroxyprogesterone, 17α-hydroxyprogesterone, testosterone and methyltestosterone, the activity was 150.8%, 147.6%, 145.4%, 133.7%, 127.4% and 126.3% of the control level. Conclusion: Given the limited inhibitory effect and the maximal plasma concentration, these steroids were generally safe; the potential of in vivo metabolim-based drug-drug interactions is quite remote. (Supported by the DUT-DICP scientific cooperation fund and the 973 program 2003CB716006 of the Ministry of Science & Technology of China)
WOS IDWOS:000242406900181
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Document Type会议论文
Corresponding AuthorYang L(杨凌)
Recommended Citation
GB/T 7714
Zhang JW,Liu Y,Li W,et al. Screening Study of the Inhibitory Effects 17 Steroids on 6 Major Cytochrome P450 Isoenzymes[C],2001:229/1.
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