title: Identification of UDP-glucuronosyltransferase isoforms involved in hepatic and intestinal glucuronidation of phytochemical carvacrol.
abstract: 1. Carvacrol (2-methyl-5-(1-methylethyl)-phenol), one of the main components occurring in many essential oils of the family Labiatae, has been widely used in food, spice and pharmaceutical industries. 2. The carvacrol glucuronidation was characterized by human liver microsomes (HLMs), human intestinal microsomes (HIMs) and 12 recombinant UGT (rUGT) isoforms. 3. One metabolite was identified as a mono-glucuronide by liquid chromatography/mass spectrometry with HLMs, HIMs, rUGT1A3, rUGT1A6, rUGT1A7, rUGT1A9 and rUGT2B7. 4. The study with a chemical inhibition, rUGT, and kinetics study demonstrated that rUGT1A9 was the major isozyme responsible for glucuronidation in HLMs, and rUGT1A7 played a major role for glucuronidation in HIMs.
authors.affiliation: Department of Clinical Pharmacology, Affiliated Hospital, Academy of Military Medical Sciences, Beijing, China.
authors.forename: Rui-Hua
authors.initials: RH
authors.lastname: Dong
authors.forename: Zhong-Ze
authors.initials: ZZ
authors.lastname: Fang
authors.forename: Liang-Liang
authors.initials: LL
authors.lastname: Zhu
authors.forename: Guang-Bo
authors.initials: GB
authors.lastname: Ge
authors.forename: Ling
authors.initials: L
authors.lastname: Yang
authors.forename: Ze-Yuan
authors.initials: ZY
authors.lastname: Liu
mesh_terms: D000293:Adolescent; D000328:Adult; D002648:Child; D002851:Chromatography, High Pressure Liquid; D000081007:Cymenes; D057075:Enzyme Assays; D005260:Female; D020719:Glucuronides / Q000378:metabolism*; D014453:Glucuronosyltransferase / Q000378:metabolism*; D006801:Humans; D007422:Intestines / Q000187:drug effects / Q000201:enzymology*; D007527:Isoenzymes / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000187:drug effects / Q000201:enzymology*; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D008875:Middle Aged; D039821:Monoterpenes / Q000737:chemistry; D015742:Propofol / Q000494:pharmacology; D011994:Recombinant Proteins / Q000378:metabolism; D055815:Young Adult
chemical_list: D000081007:Cymenes; D020719:Glucuronides; D007527:Isoenzymes; D039821:Monoterpenes; D011994:Recombinant Proteins; C073316:carvacrol; D014453:Glucuronosyltransferase; D015742:Propofol