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Evaluation of the inhibitory effects of compounds on UGTs is clinically important because inhibition of UGT isoforms could not only result in serious drug\u2013drug interactions (DDIs), but also induce metabolic disorders of endogenous substances. The aim of the present study was to investigate the inhibitory effects of carvacrol on major UGT isoforms. The results showed that carvacrol could inhibit the activity of UGT1A9 with negligible effects on other UGT isoforms. When 4\u2010methylumbelliferone (4\u2010MU) was used as a nonspecific probe substrate and recombinant UGT enzymes were utilized as an enzyme resource, the inhibition of UGT1A9 was best fit to the competitive type and the inhibition kinetic parameter (<jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub>) was calculated to be 5.7\u2009\u00b5<jats:sc>m<\/jats:sc>. Furthermore, another specific probe substrate, propofol, was employed to determine the inhibitory kinetics of UGT1A9, and the results demonstrated that the inhibitory type was noncompetitive. The inhibition kinetic parameter (<jats:italic>K<\/jats:italic><jats:sub>i<\/jats:sub>) was determined to be 25.0\u2009\u00b5<jats:sc>m<\/jats:sc>. Because this substrate\u2010dependent inhibition of UGT1A9 might confuse the<jats:italic>in vitro\u2013in vivo<\/jats:italic>extrapolation, these<jats:italic>in vitro<\/jats:italic>inhibition kinetic parameters should be interpreted with special caution. Copyright \u00a9 2011 John Wiley &amp; Sons, Ltd.<\/jats:p>","DOI":"10.1002\/ptr.3525","type":"journal-article","created":{"date-parts":[[2011,5,5]],"date-time":"2011-05-05T07:10:32Z","timestamp":1304579432000},"page":"86-90","source":"Crossref","is-referenced-by-count":41,"title":["Investigation of UDP\u2010glucuronosyltransferases (<scp>UGTs<\/scp>) Inhibitory Properties of Carvacrol"],"prefix":"10.1002","volume":"26","author":[{"given":"Rui\u2010Hua","family":"Dong","sequence":"first","affiliation":[{"name":"Department of Clinical Pharmacology, Affiliated Hospital Academy of Military Medical Sciences Beijing 100071 China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhong\u2010Ze","family":"Fang","sequence":"additional","affiliation":[{"name":"Laboratory of Pharmaceutical Resource Discovery Dalian Institute of Chemical Physics Chinese Academy of Sciences Dalian 116023 China"},{"name":"Graduate School of Chinese Academy of Sciences Beijing 100049 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