Mechanism of Inhibition of Human Cytochrome P450 1A1 and 1B1 by Piceatannol
DC Field | Value | Language |
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dc.contributor.author | Chae, Ah-Reum | - |
dc.contributor.author | Shim, Jae-Ho | - |
dc.contributor.author | Chun, Young-Jin | - |
dc.date.available | 2019-05-30T04:35:57Z | - |
dc.date.issued | 2008-12 | - |
dc.identifier.issn | 1976-9148 | - |
dc.identifier.issn | 2005-4483 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/23544 | - |
dc.description.abstract | The resveratrol analogue piceatannol (3,5,3',4'-tetrahydroxy-trans-stilbene) is a polyphenol present in grapes and wine and reported to have anti-carcinogenic activities. To investigate the mechanism of anticarcinogenic activities of piceatannol, the effects on CYP 1 enzymes were determined in Escherichia coli membranes co-expressing recombinant human CYP1A1, CYP1A2 or CYP1B1 with human NADPH-P450 reductase. Piceatannol showed a strong inhibition of CYP1A1 and CYP1B1 in a concentration-dependent manner, and IC50 of human CYP1A1 and CYP1B1 was 5.8 mu M and 16.6 mu M, respectively. However, piceatannol did not inhibit CYP1A2 activity in the concentration of up to 100 mu M. Piceatannol exhibited 3-fold selectivity for CYP1B1 over CYP1A1. The mode of inhibition of piceatannol was non-competitive for CYP1A1 and CYP1B1. The result that piceatannol did not inhibit CYP1B1-mediated alpha-naphthoflavone (alpha-NF) metabolism suggests piceatannol may act as a non-competitive inhibitor as well. In human prostate carcinoma PC-3 cells, piceatannol induces apoptosis and prevents Akt-mediated signal pathway. Taken together, abilities of piceatannol to induce apoptotic cell death as well as CYP1 enzyme inhibition make this compound a useful tool for cancer chemoprevention. | - |
dc.format.extent | 7 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | KOREAN SOC APPLIED PHARMACOLOGY | - |
dc.title | Mechanism of Inhibition of Human Cytochrome P450 1A1 and 1B1 by Piceatannol | - |
dc.type | Article | - |
dc.identifier.doi | 10.4062/biomolther.2008.16.4.336 | - |
dc.identifier.bibliographicCitation | BIOMOLECULES & THERAPEUTICS, v.16, no.4, pp 336 - 342 | - |
dc.identifier.kciid | ART001300435 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000262747300006 | - |
dc.identifier.scopusid | 2-s2.0-69549095795 | - |
dc.citation.endPage | 342 | - |
dc.citation.number | 4 | - |
dc.citation.startPage | 336 | - |
dc.citation.title | BIOMOLECULES & THERAPEUTICS | - |
dc.citation.volume | 16 | - |
dc.type.docType | Article | - |
dc.publisher.location | 대한민국 | - |
dc.subject.keywordAuthor | Cytochrome P450 | - |
dc.subject.keywordAuthor | Enzyme inhibition | - |
dc.subject.keywordAuthor | Resveratrol | - |
dc.subject.keywordAuthor | Piceatannol | - |
dc.subject.keywordPlus | SIGNALING PATHWAY | - |
dc.subject.keywordPlus | BAX TRANSLOCATION | - |
dc.subject.keywordPlus | DRUG-METABOLISM | - |
dc.subject.keywordPlus | CELL-SURVIVAL | - |
dc.subject.keywordPlus | HL-60 CELLS | - |
dc.subject.keywordPlus | APOPTOSIS | - |
dc.subject.keywordPlus | RESVERATROL | - |
dc.subject.keywordPlus | AKT | - |
dc.subject.keywordPlus | PHOSPHORYLATION | - |
dc.subject.keywordPlus | MODULATION | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
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