三种滋阴中药配方对人主要细胞色素P450和尿苷二磷酸葡萄糖醛酸转移酶同工酶体外活性的抑制潜力。

Inhibitory potential of three Yin-tonification herbal formulas on the activities of human major cytochrome P450 and UDP- glucuronosyltransferases isozymes in vitro.

作者信息

Seong Eun Jin, Hyeun-Kyoo Shin, Hyekyung Ha

机构信息

K-herb Research Center, Korea Institute of Oriental Medicine, Daejeon 34054, Republic of Korea.

出版信息

J Tradit Chin Med. 2018 Aug;38(4):511-522.

PMID:32186076

Abstract

OBJECTIVE

To investigate the influence of Yin-tonification herbal formulas Jaeumganghwa-tang (Ziyin Jianghuo Tang, JEGHT), Ssanghwa-tang (Shuanghe Tang, SHT) and Yukmijihwang-tang (Liuwei Di huang Tang, YMJHT) on the activities of human major cytochrome P450 (CYP450s) and UDP-glucuronosyltransferases isozymes (UGTs) in vitro.

METHODS

The activities of CYP450s (CYP1A2, CYP3A4, CYP2B6, CYP2C9, CYP2C19, CYP2D6 and CYP2E1) and UGTs (UGT1A1, UGT1A4 and UGT2B7) were assessed using in vitro fluorescence- and luminescence-based enzyme assays, respectively. The effects of herbal formulas on the activities of CYP450s and UGTs were presented as IC50 values.

RESULTS

JEGHT showed the potent inhibition of the CYP2D6 activity, with weak inhibition on the activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2E1, CYP3A4, UGT1A1, UGT1A4 and UGT2B7. SHT inhibited the activities of CYP1A2 and CYP2E1, whereas the negligible inhibition of the activities of CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4, UGT1A1, UGT1A4 and UGT2B7 through SHT was observed. YMJHT inhibited CYP2E1 activity, with a negligible inhibition on the activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4, UGT1A1, UGT1A4 and UGT2B7.

CONCLUSION

These findings provide information about the potential interactions between three Yin-tonifi.

摘要

目的

研究滋阴中药方剂加味升降汤（滋阴降火汤，JEGHT）、双和汤（SHT）和六味地黄丸（六味地黄汤，YMJHT）对人主要细胞色素P450（CYP450s）和尿苷二磷酸葡萄糖醛酸转移酶同工酶（UGTs）体外活性的影响。

方法

分别采用基于荧光和发光的体外酶法评估CYP450s（CYP1A2、CYP3A4、CYP2B6、CYP2C9、CYP2C19、CYP2D6和CYP2E1）和UGTs（UGT1A1、UGT1A4和UGT2B7）的活性。中药方剂对CYP450s和UGTs活性的影响以半数抑制浓度（IC50）值表示。

结果

JEGHT对CYP2D6活性有较强抑制作用，对CYP1A2、CYP2B6、CYP2C9、CYP2C19、CYP2E1、CYP3A4、UGT1A1、UGT1A4和UGT2B7的活性有较弱抑制作用。SHT抑制CYP1A2和CYP2E1的活性，而对CYP2B6、CYP2C9、CYP2C19、CYP2D6、CYP3A4、UGT1A1、UGT1A4和UGT2B7的活性抑制作用可忽略不计。YMJHT抑制CYP2E1活性，对CYP1A2、CYP2B6、CYP2C9、CYP2C19、CYP2D6、CYP3A4、UGT1A1、UGT1A4和UGT2B7的活性抑制作用可忽略不计。