毛冬青总提取物的抗血栓作用及基于ADP的机制研究  

Antithrombotic Activity of Ilex Pubescens Total Extract and the Action of Mechanism Based on ADP

作　　者：陈元元[1] 熊天琴[1] 赵玉民[1] 廖嘉仪[1] 林曦[1] 谭庆龙[1] 赵钟祥[1] 

机构地区：[1]广州中医药大学,广东广州510006

出　　处：《中华中医药学刊》2015年第5期1092-1096,I0006,共6页Chinese Archives of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(81270054;30901954);广东省优秀青年教师培养计划项目(Yq2013045);广州市珠江科技新星专项(2011J2200047)

摘　　要：目的:研究毛冬青总提取物的抗血栓作用。方法:采用家兔体外血凝块溶解实验,胶原-肾上腺素小鼠血栓实验,角叉菜胶小鼠血栓实验,Fe Cl3大鼠血栓形成实验,观察毛冬青提取物溶解血栓和抗血栓形成的作用。结果:毛冬青总提取物的0.2 mg/m L浓度对体外形成的家兔血凝块有明显的溶解作用;毛冬青总提取物(1、0.5、0.25 g/kg)剂量组均能减少胶原蛋白-肾上腺素诱发血栓形成小鼠的死亡数,增加保护率;能减少角叉菜胶诱导血栓形成小鼠的相对黑尾长度;毛冬青总提取物(195、97.5、48.75 mg/kg)各剂量组均减轻Fe Cl3颈动脉血栓模型大鼠的血栓的重量和内皮受损程度;降低ADP诱导的血小板聚集率;降低FIB的含量及抑制P2Y12受体的表达,对APTT、TT、PT的表达几乎无影响;提高c AMP的表达水平;减少TXB2和P-选择素的含量、不影响6-Keto-PGF1α的表达;并降低血小板胞浆Ca2+平均荧光强度及抑制GPⅡb/Ⅲa的表达。结论:毛冬青总提取物具有一定的抗血栓的作用,能改善血管内皮的受损程度,具有保护血管内皮的作用,并通过影响P2Y12受体αGi亚单位和βγ亚单位功能的表达,降低P2Y12受体的含量,抑制血小板的聚集,最终抑制血栓的形成。AIM： To study the antithrombotic activity of Ilex Pubescens total extract. Methods： Thrombolytic and an- tithrombotic activity of Ilex Pubescens total extract were observed by in vitro solubility test of blood clot in rabbits, Colla- gen - epinephrine - induced thrombosis in mice, carrageenan - induced thrombosis in mice and FeC13 - induced thrombo- sis in rat. Results ： The concentration of Ilex Pubescens total extract（0.2 mg/mL） had significant dissolved effect on solu- bility experiment of blood clot in rabbits. Both the dose groups of Ilex Pubescens total extract （ 1, 0.5, 0.25 g/kg） all decreased the number of death and increased protection rate induced thrombosis by collagen - epinephrine in mice also re- duced the relative to black tail length induced thrombosis by carrageenan in mice. The dose groups of Ilex Pubescens total extract （ 195,97.5,48.75 mg/kg） all reduced the wet weight of thrombus and the degree of endothelial injury induced carotid artery thrombosis by FeC13 in rat, both reduced ADP - induced platelet aggregation also FIB and the P2Y12 recep- tor expression, but it has no difference of the AprI＇T, TT, PT. It not only increased expression levels of cAMP, but also reduced the content of TXB2and P -selectin, however it didn＇t affect the 6 -Keto -PGF In addition, it reduced the GP II b/m a expression and Ca2 ＋ mean fluorescence of platelet cytosolic. Conclusion ： The llex Pubescens total extract has the significant antithrombotic activity and can improve the degree of endothelial injury, so it has the role of protectiving vascular endothelial. Additionally it inhibits platelet aggregation and thrombus formation by affecting the expression otGi subunit and βy subunit of P2Y12 receptor and reducing the content of P2Y12 receptor.

关 键 词：毛冬青总提取物 抗血栓 血小板 P2Y12受体 

分 类 号：R285.5[医药卫生—中药学]