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学科主题: 物理化学
题名: Hepatobiliary disposition of deoxyschizandrin in perfused rat livers in situ
作者: Wu JJ(吴敬敬) ;  Zhang YY(张延延) ;  Ge GB(葛广波) ;  Yang L(杨凌)
会议名称: 16th North American Regional ISSX Meeting
会议日期: 2009-10-18
出版日期: 2009-10-18
会议地点: 美国
通讯作者: 杨凌
部门归属: 十八室
主办者: The International Society for the Study of Xenobiotics
摘要: Deoxyschizandrin (Schizandrin A, Sin A), is one of the major active lignans isolated from Schisandra fruits. In vitro studies have indicated that Sin A was selectively metabolized by CYP3A4 in human liver microsome. However, except for metabolism, blood flow, protein binding and transporter activity have also been identified as the determinants of organ clearance. Aim to determine the respective contributions of enzyme and transporter to hepatic clearance, and further develop Sin A as a new in vivo CYP3A probe, we investigated the disposition of deoxyschizandrin in recirculated perfused rat livers, descibed as a simple physiologically based pharmacokinetic (PBPK) liver model. Sin A was introduced as a bolus into the perfusate reservoir at a concentration of 25 μM. The perfusate and bile samples were collected over 60 min, and the concentrations of Sin A and it’s metabolite in perfusate and bile were measured using ultra fast liquid chromatograph assay-diode array detection (UFLC-DAD). Both Sin A and its C-7 hydroxylation metabolite, schizandrol A (Sol A), were identified in perfusate and bile. The levels of formation of other metabolites except for Sol A were negligible during our experimental procedure. Sin A was eliminated from the perfusate in a biexponential manner. The hepatic clearance was characterized with a high hepatic extraction ratio of approximately 63% for the parent drug. However, Sin A exhibited minimal biliary excretion, representing around 0.003% of the dose administered. Over 32% of the starting Sin A could be converted to Sol A at steady state. In conclusion, Sin A is unitarily metabolized in rat liver and hepatic metabolism is the major elimination pathway for Sin A, which improve the probability that Sin A might be served as a in vivo probe to evalute the elimination capability of liver via CYP3A.
语种: 中文
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内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113510
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Wu JJ,Zhang YY,Ge GB,et al. Hepatobiliary disposition of deoxyschizandrin in perfused rat livers in situ[C]. 见:16th North American Regional ISSX Meeting. 美国. 2009-10-18.
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