血管内皮细胞分泌众多的生物活性因子,调节血液凝血系统、纤溶系统和血小板聚集功能,影响血栓的发生和发展。我国中医药研究表明,大量植物来源的单体化合物具有确切的抗血栓作用,这些化合物的安全性好。因此,发展纯天然的抗血栓药物是目前研制新型抗血栓药物的有效途径。本研究室系列研究发现,中药单体化合物虽然安全性好,但疗效往往不强。进一步研究发现,多种单体化合物在联合使用时,疗效大大增强,用药量大大降低。例如,我们研究了两个活血化瘀类中药和一个理气化瘀类中药中的3个单体化合物A、B和C。此3个化合物均可调节内皮细胞功能,但药理作用环节不同,分别为促进NO的释放、促进PGI2的释放和抑制血小板聚集。在联合使用时,剂量分别为0.05、1.0和1.0mg/kg即可产生显著的抗血栓作用,比任一单体化合物的有效剂量低20～100倍或以上。为发展有效、安全、适于长期使用的纯天然口服抗血栓新药打下坚实的基础。

Vascular endo thelium is able to prod uce a variety of bioactive factors,w hich can modulate the functions of bl ood coag-ulation,fibrinolytic system and pl atelet aggrega tion,resulting in re tarding the pathogenesis of thrombosis.At the same time ,the functional disorders occu r in endothelium in the pathogenesis of thrombos is.Therefore,it is a pro mising re-search direction to develop new drugs agai nst thrombosis through modula ting the functions of endothelium.At present quit e a lot of compounds derived from traditional Chinese medi cines have proved to be against throm bosis and in satisfactory safety,but are oar s till weak in th e experiment of their t herapeutic effects.The potent effe cts against thrombos is could be achieved by the combined administration of these natural products . A new anti -thrombosis drug has been discovered in our laboratory,w hich conta ins three compounds deriv ed from three kinds of traditional Chinese medicines. Its molecular mechanism s underlying anti -thrombosis have p roved to be able t o stimulate the rele ase of nitric oxide and prostacyclin from v ascular endothe lium and inhibit pla telet aggregation.Buttery tests are being used in our labo ratory in order to develop th is natural product of anti -at thromb osis accord ing to technical require ments for the approval of new drugs in China.

国家重点基础研究规划项目No.199805112血管内皮细胞保护作用新靶点及创新药物先导结构的发现与优化;;北京赛德维康医药研究院科技风险基金:心脑血管疾病治疗药物的研究。