Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation
Induction of cytochrome P450 2B6 activity by the herbal medicine baicalin as measured by bupropion hydroxylation
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DOI：
10.1007/s00228-008-0594-3
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发表时间：
2009-04-01
影响因子：
2.9
通讯作者：
Zhou, Hong-Hao
中科院分区：
文献类型：
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作者：
Fan, Lan;Wang, Jin-Chao;Zhou, Hong-Hao
17名健康男性志愿者(6名CYP2B6*1/*1、6名CYP2B6*1/*6和5名CYP2B6*6/*6)在口服安非他酮的同时，每日服用黄芩苷，观察黄芩苷对安非他酮羟化作用的影响。给药后72h采血测定安非他酮和羟基安非他酮的药代动力学曲线。黄芩苷使羟基安非他酮的最大血药浓度(C(Max))增加73%[90%可信区间(CI)，44-108%；P<；0.01]，药时曲线下面积外推至无穷大(AUC(0-az))87%(90%可信区间，48-137%；P<；0.01)，消除半衰期无变化。黄芩苷可使羟基安非他酮与安非他酮的AUC(0-az)比值增加63%(90%CI，38-92%；P<；0.01)。黄芩苷可显著诱导CYP2B6催化的安非他酮羟化，其对其他药物的作用值得进一步研究。
This study investigated the effect of the herbal medicine baicalin on bupropion hydroxylation, a probe reaction for CYP2B6 activity related to different CYP2B6 genotype groups.Seventeen healthy male volunteers (6 CYP2B6*1/*1, 6 CYP2B6*1/*6, and 5 CYP2B6*6/*6) received orally administered bupropion alone and during daily treatment with baicalin. Blood samples were taken up to 72 h after each bupropion dose, and pharmacokinetics profiles were determined on days 1 and 25 for bupropion and hydroxybupropion.Baicalin administration increased hydroxybupropion maximum plasma concentration (C (max)) by 73% [90% confidence interval (CI), 44-108%; P < 0.01] and the area under the concentration time curve extrapolated to infinity (AUC(0-az)) of hydroxybupropion by 87% (90% CI, 48-137%; P < 0.01), with no change in the elimination half-life of hydroxybupropion. Baicalin increased the AUC(0-az) ratio of hydroxybupropion to bupropion by 63% (90% CI, 38-92%; P < 0.01).Baicalin significantly induced CYP2B6-catalyzed bupropion hydroxylation, and the effects of baicalin on other CYP2B6 substrate drugs deserve further investigation.