Transformation of trollioside and isoquercetin by human intestinal flora in vitro  

作　　者：YUAN Ming SHI Duo-Zhi WANG Teng-Yu ZHENG Shi-Qi LIU Li-Jia SUN Zhen-Xiao WANG Ru-Feng DING Yi 

机构地区：[1]School of Chinese Materia Medica, Beijing University of Chinese Medicine [2]Drug Discovery Facility, Tsinghua University

出　　处：《Chinese Journal of Natural Medicines》2016年第3期220-226,共7页中国天然药物（英文版）

基　　金：supported by National Natural Science Foundation of China(NSFC,No.81274044)

摘　　要：The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration(MIC). Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.The present study was designed to determine the intestinal bacterial metabolites of trollioside and isoquercetin and their antibacterial activities. A systematic in vitro biotransformation investigation on trollioside and isoquercetin, including metabolite identification, metabolic pathway deduction, and time course, was accomplished using a human intestinal bacterial model. The metabolites were analyzed and identified by HPLC and HPLC-MS. The antibacterial activities of trollioside, isoquercetin, and their metabolites were evaluated using the broth microdilution method with berberine as a positive control, and their potency was measured as minimal inhibitory concentration （MIC）. Our results indicated that trollioside and isoquercetin were metabolized by human intestinal flora through O-deglycosylation, yielding aglycones proglobeflowery acid and quercetin, respectively The antibacterial activities of both metabolites were more potent than that of their parent compounds. In conclusion, trollioside and isoquercetin are totally and rapidly transformed by human intestinal bacteria in vitro and the transformation favors the improvement of the antibacterial activities of the parent compounds.

关 键 词：Trollioside ISOQUERCETIN BIOTRANSFORMATION Human intestinal flora Antibacterial activity 

分 类 号：R969.1[医药卫生—药理学]