甘草次酸与大鼠肝膜血管紧张素Ⅱ受体相结合

目的从中药成份中筛选血管紧张素Ⅱ（ＡⅡ）受体的拮抗剂。方法采用大鼠肝细胞膜为材料的受体放射配基结合分析。结果大鼠肝细胞膜ＡⅡ受体的ＫＤ值为０５１８ｎｍｏｌ·Ｌ－１，Ｂｍａｘ为０１１９ｐｍｏｌ·Ｌ－１，是属于高和性的单位点结合。膜制剂在－７０℃保存３０～６０ｄ，结合率基本不受影响。从２１种中药有效成分选出甘草次酸对血管紧张素Ⅱ受体有较好结合作用，其ＩＣ５０为７５０μｍｏｌ·Ｌ－１。结论甘草次酸有望成为ＡⅡ受体非肽拮抗剂的先导化合物

Binding of glycyrrhetinic acid to the angiotensinⅡ receptor in rat liver membrane

Abstract AIM To investigate the angiotensin Ⅱ receptors nonpeptide antagonists from traditional medical herbs component. METHODS AngiotensinⅡ receptor radioligand binding assay was established with rat liver membrane receptor. RESULTS The rat liver membrane angiotensin Ⅱ receptors are stable at -70℃ kept for thirty sixty days and its maximal binding ( B max ) is 0 119 pmol·L -1 while K D value is 0 518 nmol·L -1 . The application of the reaction systems to screen have obtained glycyrrhetinic acid, IC 50 value is 75 μmol·L -1 . CONCLUSIONS The glycyrrhetinic acid will be able to be a lead compound of AⅡ nonpeptide antagonist.