Effects of Traditional Herbal Formulae on Human CYP450 Isozymes

• Published in: Chinese journal of integrative medicine 2017, Vol.23 (1), p.62-69
• Main Authors: Jin, Seong Eun, Ha, Hyekyung, Shin, Hyeun-Kyoo
• Format: Article
• Language: English
• Subjects: CYP2D6; CYP2E1; CYP450; Cytochrome P-450 Enzyme System - metabolism; Drugs, Chinese Herbal - pharmacology; Herb-Drug Interaction; Hot Temperature; Humans; Inhibitory Concentration 50; Isoenzymes - metabolism; Medicine; Medicine & Public Health; Plant Extracts - pharmacology; Water - chemistry; 中草药配方; 中药配方; 同工酶; 细胞色素P450; 药物代谢酶
• ISSN: 1672-0415; 1993-0402
• DOI: 10.1007/s11655-016-2476-3

Objective：To assess the effects of traditional herbal formulae Sijunzi Decoction（四君子汤,Sagunja-tang,SJZD）,Siwu Decoction（四物汤,Samul-tang,SWD）,Bawu Decoction（八物汤,Palmul-tang,BWD）and Shiquan Dabu Decoction（十全大补汤,Sipjeondaebo-tang,SDD）on the activities of human cytochrome P450（CYP450）,a drug-metabolizing enzyme.Methods：Herbal formula water extracts were filtered and lyophilized after the powder extracts were dissolved in distilled water.The activities of major human CYP450isozymes（CYP3A4,CYP2C19,CYP2D6 and CYP2E1）were measured using in vitro fluorescence-based enzyme assays.The inhibitory effects of the herbal formulas on the activities of CYP450 were characterized as half maximal inhibition concentration（IC50）values.Results：All the tested herbal formulae inhibited CYP2C19activity（IC50：SJZD,83.28μg/m L;SWD,235.54μg/m L;BWD,166.82μg/m L;SDD,178.19μg/m L）;SJZD（IC50=196.46μg/m L）,SWD（IC50=333.42μg/m L）and SDD（IC50=163.42μg/m L）inhibited CYP2E1-mediated metabolism;whereas BWD exhibited comparatively weak inhibition of CYP2E1（IC50=501.78μg/m L）.None of the four herbal formulas significantly affected CYP3A4 or CYP2D6.Conclusions：These results suggest that SJZD,SWD,BWD and SDD could potentially inhibit the metabolism of co-administered synthetic drugs whose primary route of elimination is via CYP2C19.In addition,clinically relevant pharmacokinetic interactions could occur when SJZD,SWD or SDD is co-administered with drugs metabolized by CYP2E1.Our findings provide information for the safety and effective clinical use of these four classic herbal formulas.