Identification of active compound combination contributing to anti-inflammatory activity of Xiao-Cheng-Qi Decoction via human intestinal bacterial metabolism

作     者：LIU Xing-Yan LI Li LI Xue-Qing YU Bo-Yang LIU Ji-Hua 

作者机构：Jiangsu Key Laboratory of TCM Evaluation and Translational Research China Pharmaceutical University State Key Laboratory of Natural Medicines China Pharmaceutical University 

出 版 物：《Chinese Journal of Natural Medicines》 (中国天然药物（英文版）)

年 卷 期：2018年第16卷第7期

页      面：513-524页

核心收录：

学科分类：0710[理学-生物学] 1007[医学-药学(可授医学、理学学位)] 100704[医学-药物分析学] 1005[医学-中医学] 1002[医学-临床医学] 0703[理学-化学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(No.81173471) 

主　　题：Xiao-Cheng-Qi decoction Human intestinal bacteria Metabolism Anti-inflammatory LC-Q-TOF/MS 

摘      要：Human intestinal bacteria play an important role in the metabolism of herbal medicines, leading to the variations in their pharmacological profile. The present study aimed to investigate the metabolism of Xiao-Cheng-Qi decoction(XCQD) by human intestinal bacteria and to discover active component combination(ACC) contributing to the anti-inflammatory activity of XCQD. The water extract of XCQD was anaerobically incubated with human intestinal bacteria suspensions for 48 h at 37 °C. A liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry(LC-Q-TOF/MS) method was performed for identification of the metabolites. In addition, the anti-inflammatory effects of XCQD and biotransformed XCQD(XCQD-BT) were evaluated in vitro with cytokines in RAW264.7 cells induced by lipopolysaccharide(LPS). A total of 51 compounds were identified in XCQD and XCQD-BT. Among them, 20 metabolites were proven to be transformed by human intestinal bacteria. Significantly, a combination of 14 compounds was identified as ACC from XCQD-BT, which was as effective as XCQD in cell models of inflammation. In conclusion, this study provided an applicable method, based on intestinal bacterial metabolism, for identifying combinatory compounds responsible for a certain pharmacological activity of herbal medicines.