El-Kadi A O, Tanira M O M, Ali B H, Bashir A K, Souich P Du
Department of Pharmacology and Toxicology, University of Western Ontario, Canada.
Phytother Res. 2003 Jun;17(6):688-90. doi: 10.1002/ptr.1224.
The strongly basic alkaloidal fraction of the traditional medicinal plant Rhazya stricta (RS) was given orally to mice, in a single dose of 10 mg/kg (group 1) or, twice daily for 3 days at the same dose (group 2). A third group (control) received normal saline. Liver homogenates from all animals were used to assess the microsomal activity of cytochrome P450 and its isoforms as well as its catalytic activity (using theophylline as a substrate). RS alkaloidal fraction had no significant effect on the total amount of microsomal cytochrome P450, but it caused a significant increase in the cytochrome P450 isoforms CYPs 1A1 and 1A2. It also significantly increased the concentrations of some metabolites of theophylline. These results suggest that RS has the potential to interact with other drugs that are biotransformed by cytochrome P450, when given concomitantly with it.
将传统药用植物刺山柑(RS)的强碱性生物碱部分以10毫克/千克的单剂量口服给予小鼠(第1组),或以相同剂量每日两次连续3天给药(第2组)。第三组(对照组)给予生理盐水。使用所有动物的肝脏匀浆来评估细胞色素P450及其同工酶的微粒体活性以及其催化活性(以茶碱为底物)。RS生物碱部分对微粒体细胞色素P450的总量没有显著影响,但它导致细胞色素P450同工酶CYP 1A1和1A2显著增加。它还显著增加了茶碱的一些代谢物的浓度。这些结果表明,当与细胞色素P450同时给药时,RS有可能与其他经细胞色素P450进行生物转化的药物发生相互作用。