title: Transformation of trollioside and isoquercetin by human intestinal flora in vitro.
abstract: 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.
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Ming
authors.initials: M
authors.lastname: Yuan
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Duo-Zhi
authors.initials: DZ
authors.lastname: Shi
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Teng-Yu
authors.initials: TY
authors.lastname: Wang
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Shi-Qi
authors.initials: SQ
authors.lastname: Zheng
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Li-Jia
authors.initials: LJ
authors.lastname: Liu
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.
authors.forename: Zhen-Xiao
authors.initials: ZX
authors.lastname: Sun
authors.affiliation: School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China. Electronic address: wangrufeng@tsinghua.org.cn.
authors.forename: Ru-Feng
authors.initials: RF
authors.lastname: Wang
authors.affiliation: Drug Discovery Facility, Tsinghua University, Beijing 100084, China. Electronic address: yiding@mail.tsinghua.edu.cn.
authors.forename: Yi
authors.initials: Y
authors.lastname: Ding
mesh_terms: D065767:Activation, Metabolic; D000900:Anti-Bacterial Agents / Q000378:metabolism*; D001419:Bacteria / Q000378:metabolism*; D001565:Benzoates / Q000378:metabolism*; D001711:Biotransformation; D000069196:Gastrointestinal Microbiome; D005960:Glucosides / Q000378:metabolism*; D006801:Humans; D007422:Intestines / Q000382:microbiology; D008826:Microbial Sensitivity Tests; D008954:Models, Biological; D011794:Quercetin / Q000031:analogs & derivatives* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D001565:Benzoates; D005960:Glucosides; C484703:trollioside; C016527:isoquercitrin; D011794:Quercetin
keywords: Antibacterial activity; Biotransformation; Human intestinal flora; Isoquercetin; Trollioside