title: Metabolism of chamaechromone in vitro with human liver microsomes and recombinant human drug-metabolizing enzymes.
abstract: Chamaechromone is a major component in the dried roots of Stellera chamaejasme with antihepatitis B virus and insecticidal activity. In this study, metabolic profiles of chamaechromone were investigated in human liver microsomes. One monohydroxide and two monoglucuronides of chamaechromone were identified. The enzyme kinetics for both hydroxylation and glucuronidation were fitted to the Michaelis-Menten equation. The hydroxylation of chamaechromone was inhibited by α-naphthoflavone, and predominantly catalyzed by recombinant human cytochrome P450 1A2, whereas the glucuronidation was inhibited by quercetin, 1-naphthol, and fluconazole, and mainly catalyzed by recombinant human UDP-glucuronosyltransferase 1A3, 1A7, 1A9, and 2B7.
authors.affiliation: The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Lou
authors.affiliation: Laboratory of Pharmaceutical Analysis and Drug Metabolism, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Haihong
authors.initials: H
authors.lastname: Hu
authors.affiliation: The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Yunqing
authors.initials: Y
authors.lastname: Qiu
authors.affiliation: Zhejiang Institute for Food and Drug Control, Hangzhou, People's Republic of China.
authors.forename: Jinqi
authors.initials: J
authors.lastname: Zheng
authors.affiliation: The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Linrun
authors.initials: L
authors.lastname: Wang
authors.affiliation: The First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Xingguo
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Laboratory of Pharmaceutical Analysis and Drug Metabolism, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
authors.forename: Su
authors.initials: S
authors.lastname: Zeng
mesh_terms: D000998:Antiviral Agents / Q000378:metabolism; D001571:Benzoflavones / Q000494:pharmacology; D019388:Cytochrome P-450 CYP1A2 / Q000378:metabolism; D004347:Drug Interactions; D004365:Drugs, Chinese Herbal / Q000378:metabolism*; D047309:Flavones / Q000378:metabolism*; D015725:Fluconazole / Q000494:pharmacology; D014453:Glucuronosyltransferase / Q000378:metabolism*; D006801:Humans; D006900:Hydroxylation; D066298:In Vitro Techniques; D008099:Liver / Q000201:enzymology / Q000378:metabolism*; D008862:Microsomes, Liver / Q000378:metabolism*; D009284:Naphthols / Q000494:pharmacology; D018517:Plant Roots; D011794:Quercetin / Q000494:pharmacology; D011994:Recombinant Proteins / Q000378:metabolism; D029645:Thymelaeaceae / Q000737:chemistry*
chemical_list: D000998:Antiviral Agents; D001571:Benzoflavones; D004365:Drugs, Chinese Herbal; D047309:Flavones; D009284:Naphthols; D011994:Recombinant Proteins; C561087:chamaechromone; C029350:1-naphthol; C011512:alpha-naphthoflavone; D015725:Fluconazole; D011794:Quercetin; D019388:Cytochrome P-450 CYP1A2; C122075:UDP-glucuronosyltransferase, UGT1A3; D014453:Glucuronosyltransferase