Effects of Panax notoginseng Saponins on the Activities of CYP1A2, CYP2C9, CYP2D6 and CYP3A4 in Rats In Vivo
Effects of Panax notoginseng Saponins on the Activities of CYP1A2, CYP2C9, CYP2D6 and CYP3A4 in Rats In Vivo
复制标题
三七总皂苷对大鼠体内CYP1A2、CYP2C9、CYP2D6、CYP3A4活性的影响
DOI：
10.1002/ptr.3688
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发表时间：
2012-08-01
影响因子：
7.2
通讯作者：
Liu, Gaofeng
中科院分区：
文献类型：
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作者：
Liu, Rui;Qin, Mengnan;Liu, Gaofeng
本研究旨在探讨三七皂苷（PNS）对药物代谢酶细胞色素P450 (CYP450) 1A2, 2？C9, 2D6和3A4。CYP1A2, 2？用特异性探针药物测定C9、2D6和3A4。预处理1？大鼠腹腔注射探针药物咖啡因（10mg /kg， CYP1A2活性）、甲苯丁胺（15mg /kg， CYP2C9活性）、美托洛尔（20mg /kg， CYP2D6活性）、氨苯砜（10mg /kg， CYP3A4活性），经PNS或生理盐水（对照组）治疗。然后在不同时间采集血液进行超高效液相色谱/串联质谱（UPLC-MS/MS）分析。数据显示，PNS通过降低咖啡因Cmax (36.3%, p？
The aim of this study was to assess the influence of the Panax notoginseng saponins (PNS) on the activities of the drug-metabolizing enzymes cytochrome P450 (CYP450) 1A2, 2?C9, 2D6 and 3A4 in rats. The activities of CYP1A2, 2?C9, 2D6 and 3A4 were measured using specific probe drugs. After pretreatment for 1?week with PNS or physiological saline (control group), probe drugs caffeine (10?mg/kg; CYP1A2 activity), tolbutamide (15?mg/kg; CYP2C9 activity), metoprolol (20?mg/kg; CYP2D6 activity) and dapsone (10?mg/kg; CYP3A4 activity) were administered to rats by intraperitoneal injection. The blood was then collected at different times for ultra performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) analysis. The data showed that PNS exhibited an induction effect on CYP1A2 by decreasing caffeine Cmax (36.3%, p?