口服吴茱萸次碱对大鼠静脉注射氯唑沙宗药代动力学的影响。
Effects of Oral Rutaecarpine on the Pharmacokinetics of Intravenous Chlorzoxazone in Rats.
作者信息
Bista Sudeep R, Lee Sang Kyu, Thapa Dinesh, Kang Mi Jeong, Seo Young Min, Kim Ju Hyun, Kim Dong Hyeon, Jahng Yurngdong, Kim Jung Ae, Jeong Tae Cheon
机构信息
16College of Pharmacy, Yeungnam University, 214-1, Dae-dong, Gyeongsan, 712-749 Korea.
26Bioanalysis and Biotransformation Research Center, KIST, Seoul, 130-650 Korea.
出版信息
Toxicol Res. 2008 Sep;24(3):195-199. doi: 10.5487/TR.2008.24.3.195. Epub 2008 Sep 1.
It has been reported that hepatic microsomal cytochrome P450 (CYP) 2E1 is responsible for the metabolism of chlorzoxazone (CZX) to 6-hydroxychlorzoxazone. The present study was undertaken to assess the possible interaction of rutaecarpine, an alkaloid originally isolated from the unripe fruit of , with CZX. Male Spraque-Dawley rats were administered with 80 mg/kg/day of oral rutaecarpine for three consecutive days. Twenty four hr after the pre-treatment with rutaecarpine, the rats were treated with 20 mg/kg of intravenous CZX Rat hepatic microsomes isolated from rutaecarpine-treated rats showed greater (50% increase) activity of p-nitrophenol hydroxylase (a marker of CYP2E1) when compared with the control rats. Compared with control rats, the AUC of CZX was significantly smaller (84% decrease) possibly due to significantly faster CL (646% increase) in rats pretreated with rutaecarpine. This could be, at least partially, due to induction of CYP2E1 by rutaecarpine.
据报道，肝脏微粒体细胞色素P450（CYP）2E1负责将氯唑沙宗（CZX）代谢为6 - 羟基氯唑沙宗。本研究旨在评估吴茱萸次碱（一种最初从未成熟果实中分离出的生物碱）与CZX之间可能的相互作用。雄性Spraque - Dawley大鼠连续三天每天口服80 mg/kg的吴茱萸次碱。在用吴茱萸次碱预处理24小时后，给大鼠静脉注射20 mg/kg的CZX。与对照大鼠相比，从用吴茱萸次碱处理的大鼠中分离出的大鼠肝脏微粒体显示对硝基苯酚羟化酶（CYP2E1的标志物）的活性更高（增加50%）。与对照大鼠相比，CZX的AUC显著更小（降低84%），这可能是由于用吴茱萸次碱预处理的大鼠中CL显著更快（增加646%）。这至少部分可能是由于吴茱萸次碱诱导了CYP2E1。
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