Chemical Modification of Oleanene Type Triterpenes and Their Inhibitory Activity against HIV-1 Protease Dimerization
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概要
- 論文の詳細を見る
Oleanolic acid derivatives with different lengths of 3-O-acidic acyl chains were synthesized and evaluated for their inhibitory activity against HIV-1 protease. The lengths of the acidic chains were optimized to 6 and 8 carbons. Changing a 3-ester bond to an amide bond or dimerization of the triterpenes retained their inhibitory activity against HIV-1 protease. Introduction of an additional acidic chain to C-28 of oleanolic acid increased the inhibitory activity appreciably, though a derivative with only one acidic chain linked at C-28 also showed potent activity against HIV-1 protase.The inhibitory mechanism was proved directly by size exclusion chromatography to be inhibition of dimerization of the enzyme polypeptides. The ester bonds of the triterpene derivatives were found to be stable to lipase under mild alkaline conditons.
- 公益社団法人日本薬学会の論文
- 2000-11-01
著者
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Nakamura Norio
Institute Of Natural Medicine University Of Toyama
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MA Chao-Mei
Institute of Natural Medicine, University of Toyama
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HATTORI Masao
Institute of Natural Medicine, University of Toyama
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Ma Chao-mei
富山大学和漢医薬学総合研究所
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Hattori M
Research Institute For Wakan-yaku Toyama Medical And Pharmaceutical University
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Ma Chao-mei
Institute Of Natural Medicine University Of Toyama
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Nakamura N
Institute Of Natural Medicine Toyama Medical And Pharmaceutical University
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Hattori Masao
Institute Of Natural Medicine Faculty Of Pharmaceutical Sciences
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Nakamura Norio
Institute Of Natural Medicine
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