The first examples of ilexgenin A hybrids as a new class of multi-potent,anti-platelet agents

作     者：Li-Ping Lin Fei-Hua Wu Jing-Yu Liang 

作者机构：School of Traditional Chinese PharmacyChina Pharmaceutical University Jiangsu Center for Research & Development of Medicinal PlantsInstitute of BotanyJiangsu Province and Chinese Academy of Sciences 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2013年第24卷第8期

页      面：723-726页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by a grant from the Postgraduate Innovation Project of Jiangsu Province,China(No. CX09B_284Z) the Natural Science Foundation of Jiangsu Province,China(No.BK2012378) 

主　　题：Ilexgenin A Hybrids Multi potent anti platelet activity ADP agonists 

摘      要：Seventeen novel ilexgenin A hybrids（lA-aspirin） and（IA-NO）,as donor hybrids（IA-NO will release NO in vivo and function as NO donor）,were designed and synthesized in order to develop new multi-targeting agents for the treatment of platelet *** in vitro activities against ADP,AA and thrombin were *** a result,IA hybrids achieved substantial increases in the three tested pathways compared with ***,the most potent hybrid compounds 6d and 14d displayed about 8-fold higher potency than aspirin,and 3-fold higher potency than the simultaneous administration of aspirin and IA in inhibiting ADP-induced aggregation with IC_（50） values of 0.15 mmol/L and 0.14 mmol/L,respectively. The results suggest these IA hybrids are good candidates for multi-target therapies,and especially,may be considered as promising ADP agonists.