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  1. 055 医学部附属病院
  2. 0551 学術論文

Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol

http://hdl.handle.net/10091/00020869
http://hdl.handle.net/10091/00020869
c66b9e8a-f5f4-4ff3-a753-ddb8ef23dcf9
名前 / ファイル ライセンス アクション
Manuscript Manuscript (CBI 2014 Yamaori).pdf (1.5 MB)
Item type 学術雑誌論文 / Journal Article(1)
公開日 2018-09-18
タイトル
タイトル Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol
言語
言語 eng
DOI
関連識別子 https://doi.org/10.1016/j.cbi.2014.03.007
関連名称 10.1016/j.cbi.2014.03.007
キーワード
主題 Cannabidiol, CYP1A1, Inactivation, Mechanism-based inhibition, Structural requirement
資源タイプ
資源 http://purl.org/coar/resource_type/c_6501
タイプ journal article
著者 Yamaori, Satoshi

× Yamaori, Satoshi

en Yamaori, Satoshi

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Okushima, Yoshimi

× Okushima, Yoshimi

en Okushima, Yoshimi

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Yamamoto, Ikuo

× Yamamoto, Ikuo

en Yamamoto, Ikuo

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Watanabe, Kazuhito

× Watanabe, Kazuhito

en Watanabe, Kazuhito

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信州大学研究者総覧へのリンク
氏名 Yamaori, Satoshi
URL https://soar-rd.shinshu-u.ac.jp/profile/ja.jefNgUkh.html
出版者
出版者 ELSEVIER IRELAND LTD
引用
内容記述 CHEMICO-BIOLOGICAL INTERACTIONS.215:62-68(2014)
書誌情報 CHEMICO-BIOLOGICAL INTERACTIONS

巻 215, p. 62-68, 発行日 2014-05-25
抄録
内容記述 We previously demonstrated that cannabidiol (CBD) was a potent mechanism-based inhibitor of human cytochrome P450 1A1 (CYP1A1). However, the moiety of CBD that contributes to the potent mechanism-based inhibition of human CYP1A1 remains unknown. Thus, the effects of compounds structurally related to CBD on CYP1A1 activity were examined with recombinant human CYP1A1 in order to characterize the structural requirements for potent inactivation by CBD. When preincubated in the presence of NADPH for 20 min, olivetol, which corresponds to the pentylresorcinol moiety of CBD, enhanced the inhibition of the 7-ethoxyresorufin O-deethylase activity of CYP1A1. In contrast, d-limonene, which corresponds to the terpene moiety of CBD, failed to inhibit CYP1A1 activity in a metabolism-dependent manner. Pentylbenzene, which lacks two free phenolic hydroxyl groups, also did not enhance CYP1A1 inhibition. On the other hand, preincubation of the CBD-2′-monomethyl ether (CBDM) and CBD-2′,6′-dimethyl ether (CBDD) enhanced the inhibition of CYP1A1 activity. Inhibition by cannabidivarin (CBDV), which possessed a propyl side chain, was strongly potentiated by its preincubation. Orcinol, which has a methyl group, augmented CYP1A1 inhibition, whereas its derivative without an alkyl side chain, resorcinol, did not exhibit any metabolism-dependent inhibition. The preincubation of CBD-hydroxyquinone did not markedly enhance CYP1A1 inhibition. We further confirmed that olivetol, CBDM, CBDD, CBDV, and orcinol, as well as CBD (kinact = 0.215 min−1), inactivated CYP1A1 activity; their kinact values were 0.154, 0.0638, 0.0643, 0.226, and 0.0353 min−1, respectively. These results suggest that the methylresorcinol structure in CBD may have structurally important roles in the inactivation of CYP1A1.
資源タイプ(コンテンツの種類)
ISSN
収録物識別子タイプ PISSN
収録物識別子 0009-2797
書誌レコードID
収録物識別子タイプ NCID
収録物識別子 AA0060252X
PubMed
識別子タイプ PMID
関連識別子 https://www.ncbi.nlm.nih.gov/pubmed/24667653
関連名称 24667653
出版タイプ
出版タイプ AM
出版タイプResource http://purl.org/coar/version/c_ab4af688f83e57aa
WoS
URL http://gateway.isiknowledge.com/gateway/Gateway.cgi?&GWVersion=2&SrcAuth=ShinshuUniv&SrcApp=ShinshuUniv&DestLinkType=FullRecord&DestApp=WOS&KeyUT=000336357600009
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Cite as

Yamaori, Satoshi, Okushima, Yoshimi, Yamamoto, Ikuo, Watanabe, Kazuhito, 2014, Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol: ELSEVIER IRELAND LTD, 62–68 p.

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