Journal
XENOBIOTICA
Volume 42, Issue 10, Pages 1009-1016Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/00498254.2012.682614
Keywords
UDP-glucuronosyltransferase; carvacrol; human liver microsomes; human intestinal microsomes
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Funding
- National Key Technology R D Program [2009BADB9B02]
- National Novel Drug Innovation Program of China [2012ZX09501001-002, 2012ZX09506001-006]
- National Natural Science Foundation of China [81001473, 81102507, 81173124]
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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.
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