Citation: Li-Ping Lin, Fei-Hua Wu, Jing-Yu Liang. The first examples of ilexgenin A hybrids as a new class of multi-potent, anti-platelet agents[J]. Chinese Chemical Letters, ;2013, 24(8): 723-726. shu

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

Li-Ping Lin ^a,b ,
Fei-Hua Wu ^a,, ,
Jing-Yu Liang ^a,,

1.
a School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China;
2.
b Jiangsu Center for Research & Development of Medicinal Plants, Institute of Botany, Jiangsu Province and Chinese Academy of Sciences, Nanjing 210014, China

Corresponding author: Fei-Hua Wu, Jing-Yu Liang,
Received Date: 13 April 2013
Available Online: 6 May 2013

Seventeen novel ilexgenin A hybrids (IA-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 IC₅₀ 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.
- Ilexgenin A,
- Hybrids,
- Multi-potent anti-platelet activity,
- ADP agonists
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