Identification of active compound combination contributing to anti-inflammatory activity of Xiao-Che

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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 ℃.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.
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