The first examples of ilexgenin A hybrids as a new class of multi-potent, anti-platelet agents |
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Authors: | Li-Ping Lin Fei-Hua Wu Jing-Yu Liang |
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Institution: | a School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China;
b Jiangsu Center for Research & Development of Medicinal Plants, Institute of Botany, Jiangsu Province and Chinese Academy of Sciences, Nanjing 210014, China |
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Abstract: | 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. |
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Keywords: | Ilexgenin A Hybrids Multi-potent anti-platelet activity ADP agonists |
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