Mechanism-Based Inhibition of CYP3A4 by Constituents of Zingiber aromaticum(Pharmacognosy)
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概要
- 論文の詳細を見る
Sixteen compounds isolated from Zingiber aromaticum and showing concentration-dependent inhibition with IC_<50> values less than 100 μM, were analyzed for their possibility of time-, concentration-, and NADPH-de-pendent inhibition of CYP3A4 and four were analyzed for CYP2D6. All seven kaempferol glycosides and two kaempferol derivatives (4, 5, 8-14) appear to be the mechanism-based inhibitors of CYP3A4 enzyme in which the inhibition is irreversible and driven by the catalytic process. The other compounds showed no NADPH-dependent inhibition or reversible inhibition, and thus do not appear to be mechanism-based inhibitors. K_I values for compounds 4, 5, 8-14 were in the range of 2.21-27.01μM, whereas the k_<inact> values were 0.23-0.65 min^<-1>. Kaempferol-3-O-(2, 3, 4-tri-O-acetyl-α-L-rhamnopyranoside) (5) was found to be the most potent CYP3A4 inactivator with K_I and k_<inact> values of 2.21 μM and 0.45 min^<-1>, respectively.
- 公益社団法人日本薬学会の論文
- 2005-03-01
著者
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門田 重利
富山大学和漢医薬学総合研究所 化学応用部門
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Kadota S
富山大学和漢医薬学総合研究所
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門田 重利
冨山大学和漢医薬学総合研究所
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門田 重利
富山大学和漢医薬学総合研究所資源開発部門化学応用分野
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手塚 康弘
富山大学和漢医薬学総合研究所化学応用分野
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WATABE Tadashi
Department of Molecular Toxicology, Nihon Pharmaceutical University
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TEZUKA Yasuhiro
Department of Natural Products Chemistry, Institute of Natural Medicine,Toyama Medical and Pharmaceu
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KALAUNI Surya
Institute of Natural Medicine, University of Toyama
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Kadota Shigetoshi
Department of Natural Products Chemistry, Institute of Natural Medicine, Toyama Medical and Pharmace
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Kadota Shigetoshi
Institute Of Natural Medicine University Of Toyama
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Kadota Shigetoshi
富山大学和漢医薬学総合研究所 化学応用分野
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Kadota S
Institute Of Natural Medicine University Of Toyama
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Kadota Shigetoshi
Univ. Toyama Toyama Jpn
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Kadota Shigetoshi
インドネシア
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Watabe Tadashi
Department Of Drug Metabolism And Molecular Toxicology Tokyo University Of Pharmacy And Life Science
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Watabe T
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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Usia T
Toyama Medical And Pharmaceutical Univ. Toyama Jpn
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門田 重利
Institute Of Natural Medicine University Of Toyama
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Tezuka Yasuhiro
Univ. Toyama Toyama Jpn
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Tezuka Yasuhiro
Department Of Natural Products Chemistry Institute Of Natural Medicine Toyama Medical And Pharmaceut
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Tezuka Y
Department Of Natural Products Chemistry Institute Of Natural Medicine Toyama Medical And Pharmaceut
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USIA Tepy
Department of Natural Products Chemistry, Institute of Natural Medicine, Toyama Medical and Pharmace
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Kadota S
Research Institute For Wakan-yaku(traditional Sino-japanese Medicines) Toyama Medical And Pharmaceut
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Kalauni S
Institute Of Natural Medicine University Of Toyama
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Kadota S
Toyama Medical And Pharamaceutical Univ. Toyama Jpn
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門田 重利
Research Institute For Wakan-yaku (oriental Medicines) Toyama Medical And Pharmaceutical University
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Usia Tepy
Department Of Natural Products Chemistry Institute Of Natural Medicine Toyama Medical And Pharmaceut
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Tezuka Yasuhiro
Department Of Natural Products Chemistry Institute Of Natural Medicine Toyama Medical And Pharmaceut
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Tezuka Yasuhiro
Department Of General Thoracic Surgery Jichi Medical University And Saitama Medical Center
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Watabe Tadashi
Department Of Drug Metabolism And Molecular Toxicology School Of Pharmacy Tokyo University Of Pharma
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手塚 康弘
Institute Of Natural Medicine University Of Toyama
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Watabe Tadashi
Department of Natural Products Chemistry, Institute of Natural Medicine, Toyama Medical and Pharmaceutical University
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門田 重利
Institute of Natural Medicine, University of Toyama
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