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 

机构地区：[1]School of Traditional Chinese Pharmacy,China Pharmaceutical University [2]Jiangsu Center for Research & Development of Medicinal Plants,Institute of Botany,Jiangsu Province and Chinese Academy of Sciences

出　　处：《Chinese Chemical Letters》2013年第8期723-726,共4页中国化学快报（英文版）

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)

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 disorders.Their in vitro activities against ADP,AA and thrombin were evaluated.As a result,IA hybrids achieved substantial increases in the three tested pathways compared with IA.Encouragingly,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.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 disorders.Their in vitro activities against ADP,AA and thrombin were evaluated.As a result,IA hybrids achieved substantial increases in the three tested pathways compared with IA.Encouragingly,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.

关 键 词：Ilexgenin A Hybrids Multi-potent anti-platelet activity ADP agonists 

分 类 号：R96[医药卫生—药理学]