Antiproliferative Activity of Diarylheptanoids from the Seeds of Alpinia blepharocalyx
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概要
- 論文の詳細を見る
The 95% EtOH extract of the seeds of Alpinia blepharocalyx (Zingiberaceae) showed significant antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells. Chemical investigation of the extract led to the isolation of forty-four new (1-44) and one known (45) diarylheptanoids, eleven phenolic compounds (46-56) together with β-sitosterol glucoside (57). Almost all the isolated compounds showed significant antiproliferative activity in a concentration-dependent manner. Among the compounds, epicalyxin F(17) exhibited the most potent activity against the proliferation of colon 26-L5 carcinoma cells with an ED_50 value of 0.89 μM, while calyxin B(2) exhibited the most potent activity against human HT-1080 fibrosarcoma cells with an ED_50 value of 0.69 μM. Moreover, calyxins B(2) and K(11), epicalyxins F(17), I(20) and K(22), 6-hydroxycalyxin F(25), blepharocalyxin B(27) and mixtures of 7 and epicalysin G(18) and of calyxin J(10) and epicalyxin J(21) possessed more potent activity than a clinically used anticancer drug, 5-fluorouracil, towards HT-1080 fibrosarcoma cells. Analysis of the structure activity relationship suggested that the position of the attachment of a chalcone or a flavanone moiety does not affect the activity, although their presence in association causes a substantial enhancement of the antiproliferative activity. Moreover, the conjugated double bond of the chalcone moiety and the phenolic hydroxyl group potentiate the antiproliferative activity of the compounds.
- 社団法人日本薬学会の論文
- 2001-05-01
著者
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KADOTA Shigetoshi
Institute of Natural Medicine, University of Toyama
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TEZUKA Yasuhiro
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University
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SAIKI Ikuo
Institute of Natural Medicine, University of Toyama
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BANSKOTA Arjun
Institute of Natural Medicine, University of Toyama
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Banskota A
Institute Of Natural Medicine University Of Toyama
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Banskota Arjun
富山医科薬科大学和漢薬研究所
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Banskota Arjun
Institute Of National Medicine Toyama Medical And Pharmaceutical University
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Saiki Ikuo
富山大学 薬学研究科応用薬理学
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Saiki I
Division Of Pathogenic Biochemistry Institute Of Natural Medicine University Of Toyama
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ALI Mohammad
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University
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SAIKI Ikuo
Division of Pathogenic Biochemistry, 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
インドネシア
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Saiki Ikuo
Division Of Pathogenic Biochemistry Institute Of Natural Medicine University Of Toyama
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Saiki I
Institute Of Natural Medicine University Of Toyama
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Saiki Ikuo
Department Of Pathological Biochemistry Institute Of Natural Medicine Toyama Medical And Pharmaceuti
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門田 重利
Institute Of Natural Medicine University Of Toyama
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Tezuka Yasuhiro
Institute Of Natural Medicine Univeristy Of Toyama
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Saiki Ikuo
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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Kadota Shigetoshi
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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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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Saiki Ikuo
Institute Of Immunological Science Hokkaido University
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Ali Mohammad
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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手塚 康弘
Institute Of Natural Medicine University Of Toyama
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Banskota Arjun
Institute For Marine Biosciences National Research Council
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門田 重利
Institute of Natural Medicine, University of Toyama
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