3,4′,5-三羟基芪-3-β-单-D-葡萄糖甙抑制凝血酶非依赖花生四烯酸途径诱导兔血小板聚集作用及机理  

Inhibitory effect of 3,4',5-trihydroxystibene-3-β-mono-D-glucoside on rabbit platelet aggregation induced by thrombin-independent AA and its mechanism

作　　者：骆苏芳[1] 余传林[1] 孙莉莎[1] 张佩文[1] 

机构地区：[1]第一军医大学药理教研室,广州510515

出　　处：《中国药理学与毒理学杂志》1993年第2期130-133,共4页Chinese Journal of Pharmacology and Toxicology

基　　金：国家自然科学基金 № 3880738

摘　　要：3,4’,5-三羟基芪-3-β-单-D-葡萄糖甙(PD)0.33,0.56,0.95,1.63,2.79mmol·L^1能显著抑制2.3mmol·L^1·s^1凝血酶诱导的家兔洗涤血小板聚集,呈良好的量效关系,PD对1 min和最大血小板聚集抑制率IC_(50)分别为0.57和1.16 mmol·L^1,并能使血小板聚集延迟相延长,血小板聚集速度减慢,PD0.33～1.63mmol·L^1对血小板聚集时TXA_2释放无明显影响,仅在浓度为2.79mmol·L^1时,才明显减少TXA_2释放,PD的作用与阿司匹林不完全相同.这可能与它们的作用机理不同有关,本文还观察了PD0.33 mmol·L^1有抑制凝血酶诱导兔血小板胞浆游离钙离子浓度升高的作用。3.4'.5 Trihydroxystibene 3β monoD glucoside(PD)0.33.0.56.0.95,1.63 and 2.79mmol·L-1 could inhibit the rabbit's plateletsaggregation induced by 2.3 mmol·L-1·s-1thrombin significantly,which showed a good dose ef-fect relationship.The IC50 at 1 min and its maximum inhibition rate of platelet aggregation were 0.57 mmol·L-1 and 1.16 mmol·L-1 respectively.Meanwhile PD could prolong the lag phase of aggregation and slow down the maximum aggregation velocity,hut at a concentration of 0.33 1.63 mmol·L-1 PD didn't exhibit the influence on TXA2 release by thrombin-in-duced platelet aggregation significantly.It diminished the TXA,2release significantly only at a concentration of 2.79 mmol·L-1 However,the inhibitory effect of 11 mmol·L-1 aspirin(ASA)on platelet aggregation was significantly weaker than that of 1.63 mmol·L-1 PD and the inhibitory effect of 11 mmol ·L-1 ASA on the platelet TXA2 release was significantly stronger than that of 1.63 mmol·L-1 PD.PD 0.33 mmol·L-1 also inhibited the increase of the cytosolic free Ca2+ concentration inducedby thrombin.These results show that the inhibition of PD on platelet aggregation induced by thrombin was not only due to the inhibition of TXA2 release,but also due to the influence on other factors,such as increasing PGI2,inhibiting the activation of platelets aroused by Ca2+ and decreasing PAF and histamine secretion.

关 键 词：凝血酶 阿司匹林 血小板聚集 

分 类 号：R965.1[医药卫生—药理学]