The inhibitory potential of Broussochalcone A for the human cytochrome P450 2J2 isoform and its anti-cancer effects via FOXO3 activation
DC Field | Value | Language |
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dc.contributor.author | Park, See-Hyoung | - |
dc.contributor.author | Lee, Jongsung | - |
dc.contributor.author | Shon, Jong Cheol | - |
dc.contributor.author | Nguyen Minh Phuc | - |
dc.contributor.author | Jee, Jun Goo | - |
dc.contributor.author | Liu, Kwang-Hyeon | - |
dc.date.available | 2020-07-10T04:29:09Z | - |
dc.date.created | 2020-07-06 | - |
dc.date.issued | 2018-03-15 | - |
dc.identifier.issn | 0944-7113 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/hongik/handle/2020.sw.hongik/3903 | - |
dc.description.abstract | Background: Broussonetia papyrifera (L.) Ventenat, a traditional medicinal herb, has been applied as a folk medicine to treat various diseases. Broussochalcone A (BCA), a chalcone compound isolated from the cortex of Broussonetia papyrifera (L.) Ventenat, exhibits several biological activities including potent anti-oxidant, antiplatelet, and cytotoxic effects. Purpose: The purpose of this study is to elucidate the inhibitory effect of BCA against CYP2J2 enzyme which is predominantly expressed in human tumor tissues and carcinoma cell lines. Study design: The inhibitory effect of BCA on the activities of CYP2J2-mediated metabolism were investigated using human liver microsomes (HLMs), and its anti-cancer effect against human hepatoma HepG2 cells was also evaluated. Methods: Two representative CYP2J2-specific probe substrates, astemizole and ebastine, were incubated in HLMs with BCA. After incubation, the samples were analyzed using liquid chromatography-tandem mass spectrometry. To investigate the binding model between BCA and CYP2J2, we carried out structure-based docking simulations by using software and scripts written in-house. Results: BCA inhibited CYP2J2-mediated astemizole O-demethylation and ebastine hydroxylase activities in a concentration dependent manner with K-i values of 2.3 and 3.7 mu M, respectively. It also showed cytotoxic effects against human hepatoma HepG2 cells in a dose-dependent manner with activation of apoptosis related proteins. Conclusion: Overall, this was the first report of the inhibitory effects of BCA on CYP2J2 in HLMs. The present data suggest that BCA is a potential candidate for further evaluation for its CYP2J2 targeting anti-cancer activities. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | ELSEVIER GMBH, URBAN & FISCHER VERLAG | - |
dc.subject | FUNCTIONAL-SIGNIFICANCE | - |
dc.subject | ACCURATE DOCKING | - |
dc.subject | FORCE-FIELD | - |
dc.subject | HEPG2 CELLS | - |
dc.subject | CYP2J2 | - |
dc.subject | PROMOTES | - |
dc.subject | EXPRESSION | - |
dc.subject | GLIDE | - |
dc.subject | P450S | - |
dc.subject | HYDROXYEBASTINE | - |
dc.title | The inhibitory potential of Broussochalcone A for the human cytochrome P450 2J2 isoform and its anti-cancer effects via FOXO3 activation | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Park, See-Hyoung | - |
dc.identifier.doi | 10.1016/j.phymed.2018.03.032 | - |
dc.identifier.scopusid | 2-s2.0-85044600283 | - |
dc.identifier.wosid | 000429905400023 | - |
dc.identifier.bibliographicCitation | PHYTOMEDICINE, v.42, pp.199 - 206 | - |
dc.relation.isPartOf | PHYTOMEDICINE | - |
dc.citation.title | PHYTOMEDICINE | - |
dc.citation.volume | 42 | - |
dc.citation.startPage | 199 | - |
dc.citation.endPage | 206 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Plant Sciences | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Integrative & Complementary Medicine | - |
dc.relation.journalWebOfScienceCategory | Plant Sciences | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Integrative & Complementary Medicine | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | FUNCTIONAL-SIGNIFICANCE | - |
dc.subject.keywordPlus | ACCURATE DOCKING | - |
dc.subject.keywordPlus | FORCE-FIELD | - |
dc.subject.keywordPlus | HEPG2 CELLS | - |
dc.subject.keywordPlus | CYP2J2 | - |
dc.subject.keywordPlus | PROMOTES | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | GLIDE | - |
dc.subject.keywordPlus | P450S | - |
dc.subject.keywordPlus | HYDROXYEBASTINE | - |
dc.subject.keywordAuthor | Anti-cancer activity | - |
dc.subject.keywordAuthor | Apoptosis | - |
dc.subject.keywordAuthor | Broussochalcone A | - |
dc.subject.keywordAuthor | CYP2J2 | - |
dc.subject.keywordAuthor | Cytotoxicity | - |
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