天麻和钩藤对大鼠细胞色素 P450 酶活性的影响。

Effects of Tianma (Rhizoma Gastrodiae) and Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis) on cytochrome P450 enzyme activities in rats.

机构信息

College of Medicine, Southwest Jiaotong University, Chengdu 610031, China.

出版信息

J Tradit Chin Med. 2021 Apr;41(2):284-292.

Abstract

OBJECTIVE

To investigate the efficacy of Tianma (Rhizoma Gastrodiae) and Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis) on cytochrome P450 (CYP450) enzyme activities in rats.

METHODS

A cocktail strategy was followed to evaluate the influence of Tianma (Rhizoma Gastrodiae) and Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis) on the activities of CYP450 isoforms (CYP1A2, CYP3A4, CYP2E1, CYP2C19, CYP2C9, CYP2D6), which were determined by changes in the pharmacokinetic parameters of six probe drugs, theophylline, dapsone, chlorzoxazone, omeprazole, tolbutamide and dextromethorphan. Study groups included, Control group (CG), Tianma (Rhizoma Gastrodiae) group (TM), Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis) group (GT) and Tianma Gouteng (Gastrodia Uncaria) group (TMGT).

RESULTS

No significant differences between Tianma (Rhizoma Gastrodiae) and control groups were found. Compared with the control group, in the Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis) group both the AUC and t1/2 of dapsone and tolbutamide were reduced, whereas the CL (clearance rate) of dapsone and tolbutamide were increased. Compared with the control group, in the Tianma Gouteng group, the AUC and t1/2 of dapsone and tolbutamide were reduced, the CL of dapsone and tolbutamide were increased, and the AUC and t1/2 of chlorzoxazone were increased and the CL of chlorzoxazone was reduced.

CONCLUSION

Tianma (Rhizoma Gastrodiae) has no significant effect on the six CYP450 subtypes. The activities of CYP3A4 and CYP2C9 were increased by Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis). The activities of CYP3A4 and CYP2C9 were increased, whereas the activity of CYP32E1 was reduced by combined Tianma (Rhizoma Gastrodiae) and Gouteng (Ramulus Uncariae Rhynchophyllae cum Uncis).

摘要

目的

研究天麻（Rhizoma Gastrodiae）和钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）对大鼠细胞色素 P450（CYP450）酶活性的影响。

方法

采用鸡尾酒策略评估天麻（Rhizoma Gastrodiae）和钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）对 CYP450 同工酶（CYP1A2、CYP3A4、CYP2E1、CYP2C19、CYP2C9、CYP2D6）活性的影响，这是通过六种探针药物的药代动力学参数变化来确定的，这些探针药物分别为茶碱、氨苯砜、氯唑沙宗、奥美拉唑、甲苯磺丁脲和右美沙芬。研究组包括对照组（CG）、天麻（Rhizoma Gastrodiae）组（TM）、钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）组（GT）和天麻钩藤（Gastrodia Uncaria）组（TMGT）。

结果

天麻（Rhizoma Gastrodiae）与对照组相比无显著差异。与对照组相比，钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）组中氨苯砜和甲苯磺丁脲的 AUC 和 t1/2 降低，而氨苯砜和甲苯磺丁脲的 CL（清除率）增加。与对照组相比，天麻钩藤组中氨苯砜和甲苯磺丁脲的 AUC 和 t1/2 降低，氨苯砜和甲苯磺丁脲的 CL 增加，氯唑沙宗的 AUC 和 t1/2 增加，氯唑沙宗的 CL 降低。

结论

天麻（Rhizoma Gastrodiae）对 6 种 CYP450 亚型无显著影响。钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）增加 CYP3A4 和 CYP2C9 的活性。天麻（Rhizoma Gastrodiae）和钩藤（Ramulus Uncariae Rhynchophyllae cum Uncis）合用可增加 CYP3A4 和 CYP2C9 的活性，同时降低 CYP32E1 的活性。