THE STRUCTURE-HEMOLYSIS RELATIONSHIP OF OLEANOLIC ACID DERIVATIVES AND INHIBITION OF THE SAPONIN-INDUCED HEMOLYSIS WITH SAPOGENINS
スポンサーリンク
概要
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Chikusetsusaponin IV and V, whose genin is oleanolic acid, exhibited weak hemolytic activities. Removal of glucose residue at position 28 of chikusetsusaponin V by partial hydrolysis increased the activity more than 30-fold. Methylation of the carboxyl group at position 28 increased the activity furthermore by about 10-fold, showing HD_<50> value of 3.77 μM. On the other hand, removal of the sugar chain at position 3 of chickusetsusaponin V by partial hydrolysis completely lost the activity. These facts suggest that the sugar chain at position 3 of oleanolic acid is essential but that at position 28 is pernicious for the activity. The cytolytic agents, whose target has been regarded as membrane cholesterol, were inactivated not only by cholesterol but also by sapogenins such as oleanolic acid, gitogenin and hederagenin. Among saponins tested, akebia saponin B and C were inactivated by cholesterol, but not by the genins, probably because their affinities for the genins are too low to form complexes.
- 公益社団法人日本薬学会の論文
著者
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TOMIMORI Tsuyoshi
School of Pharmacy, Hokuriku University
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Yoshizaki Masao
Research Institute For Wakanyaku Toyama Medical And Pharmaceutical University
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MITSUI Kenichiro
Department of Biological Chemistry, Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceu
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Mitsui Kenichiro
Department Of Biochemistry Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical Univ
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Tomimori Tsuyoshi
School Of Pharmacy Hokuriku University
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YOSHIZAKI Masao
Research Institute for Wakan-yaku, Toyaina University
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