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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 (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 were 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.