Plasma pharmacokinetics and metabolism of the antitumour drug candidate 2'-benzoyloxycinnamaldehyde in rats

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dc.contributor.authorKiho Lee-
dc.contributor.authorByoung-Mog Kwon-
dc.contributor.authorKang Jeon Kim-
dc.contributor.authorJ Ryu-
dc.contributor.authorSoo Jin Oh-
dc.contributor.authorKye Sook Lee-
dc.contributor.authorM G Kwon-
dc.contributor.authorSong Kyu Park-
dc.contributor.authorJong Soon Kang-
dc.contributor.authorChang Woo Lee-
dc.contributor.authorHwan Mook Kim-
dc.date.accessioned2017-04-19T09:13:21Z-
dc.date.available2017-04-19T09:13:21Z-
dc.date.issued2009-
dc.identifier.issn0049-8254-
dc.identifier.uri10.1080/00498250802650069ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/8870-
dc.description.abstractThe pharmacokinetics and metabolism of 2'-benzoyloxycinnamaldehyde (BCA) was characterized in male Sprague-Dawley rats as part of the preclinical evaluations for developing this compound as an antitumour agent. BCA was not detected in the plasma following either intravenous or oral dose, whereas its putative metabolites 2'-hydroxycinnamaldehyde (HCA) and o-coumaric acid were present at considerable levels. In separate pharmacokinetics studies, HCA exhibited a high systemic clearance and a large volume of distribution, whereas both pharmacokinetic parameters were much lower for o-coumaric acid. The terminal half-life of both metabolites was approximately 2 h. BCA was converted rapidly to HCA in rat serum, liver microsomes and cytosol in vitro; HCA was subsequently converted to o-coumaric acid in a quantitative manner only in the liver cytosol. In addition, the formation of o-coumaric acid was inhibited significantly by menadione, a specific inhibitor for aldehyde oxidase. Taken collectively, the results suggest that the rapid systemic clearance of HCA is likely due mainly to hepatic clearance occurring from aldehyde oxidase-catalysed biotransformation to o- coumaric acid. In conclusion, the present work demonstrates that the anticancer drug candidate BCA is highly likely to work as its active metabolite HCA in the body.-
dc.publisherT&F (Taylor & Francis)-
dc.titlePlasma pharmacokinetics and metabolism of the antitumour drug candidate 2'-benzoyloxycinnamaldehyde in rats-
dc.title.alternativePlasma pharmacokinetics and metabolism of the antitumour drug candidate 2'-benzoyloxycinnamaldehyde in rats-
dc.typeArticle-
dc.citation.titleXenobiotica-
dc.citation.number3-
dc.citation.endPage265-
dc.citation.startPage255-
dc.citation.volume39-
dc.contributor.affiliatedAuthorKiho Lee-
dc.contributor.affiliatedAuthorByoung-Mog Kwon-
dc.contributor.affiliatedAuthorKang Jeon Kim-
dc.contributor.affiliatedAuthorSoo Jin Oh-
dc.contributor.affiliatedAuthorKye Sook Lee-
dc.contributor.affiliatedAuthorSong Kyu Park-
dc.contributor.affiliatedAuthorJong Soon Kang-
dc.contributor.affiliatedAuthorChang Woo Lee-
dc.contributor.affiliatedAuthorHwan Mook Kim-
dc.contributor.alternativeName이기호-
dc.contributor.alternativeName권병목-
dc.contributor.alternativeName김강전-
dc.contributor.alternativeName유제경-
dc.contributor.alternativeName오수진-
dc.contributor.alternativeName이계숙-
dc.contributor.alternativeName권무길-
dc.contributor.alternativeName박성규-
dc.contributor.alternativeName강종순-
dc.contributor.alternativeName이창우-
dc.contributor.alternativeName김환묵-
dc.identifier.bibliographicCitationXenobiotica, vol. 39, no. 3, pp. 255-265-
dc.identifier.doi10.1080/00498250802650069-
dc.subject.keyword2'-Benzoyloxycinnamaldehyde-
dc.subject.keyword2'-hydroxycinnamaldehyde-
dc.subject.keywordActive metabolite-
dc.subject.keywordAnticancer-
dc.subject.keywordAntitumour-
dc.subject.keywordDrug metabolism-
dc.subject.keywordO-coumaric acid-
dc.subject.keywordPharmacokinetics-
dc.subject.local2'-Benzoyloxycinnamaldehyde (BCA)-
dc.subject.local2'-Benzoyloxycinnamaldehyde-
dc.subject.local2′-benzoyloxycinnamaldehyde-
dc.subject.local2′-hydroxycinnamaldehyde-
dc.subject.local2'-hydroxycinnamaldehyde-
dc.subject.local2-Hydroxycinnamaldehyde-
dc.subject.local2'-Hydroxycinnamaldehyde-
dc.subject.local2′-Hydroxycinnamaldehyde-
dc.subject.localActive metabolite-
dc.subject.localAnti-cancer-
dc.subject.localAnticancer-
dc.subject.localanti-cancer-
dc.subject.localanticancer-
dc.subject.localAnti-Cancer-
dc.subject.localAntitumour-
dc.subject.localdrug metabolism-
dc.subject.localDrug metabolism-
dc.subject.localO-coumaric acid-
dc.subject.localpharmacokinetics-
dc.subject.localPharmacokinetics-
dc.description.journalClassY-
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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