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	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)
	2001-05-24
会议名称	the 1st asia pacific issx meeting
会议日期	2001-5-24
会议地点	韩国
页码	229/1
通讯作者	杨凌
中文摘要	objective: 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)
学科主题	物理化学
语种	中文
WOS记录号	WOS:000242406900181
内容类型	会议论文
源URL	[http://159.226.238.44/handle/321008/112180]
专题	大连化学物理研究所_中国科学院大连化学物理研究所
推荐引用方式 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]. 见:the 1st asia pacific issx meeting. 韩国. 2001-5-24.

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