Ento-Ⅰ涂膜剂的镇痛及其抗凝抗血栓形成作用  

Effects of Ento-Ⅰplastic on analgesia,anticoagulation and anti-thrombosis

作　　者：冯锐 王音 朱凤 赵海荣 李慧敏 张枝雪 巫秀美 

机构地区：[1]大理大学,云南省昆虫生物医药研发重点实验室,大理671000 [2]大理大学,中国西南药用昆虫及蛛形类资源开发利用协同创新中心,大理671000 [3]药用特种昆虫开发国家地方联合工程研究中心,大理671000

出　　处：《国际药学研究杂志》2016年第3期509-513,共5页Journal of International Pharmaceutical Research

基　　金：云南省高新技术产业发展项目(云发改高技[2012]1956号);云南省战略性新兴产业发展专项资金项目(云发改高技[2013]1527号);2011省级协同创新中心"中国西南药用昆虫记蛛形类资源开发利用协同创新中心"建设项目(云教科[2012]25号)

摘　　要：目的研究Ento-Ⅰ涂膜剂对小鼠的镇痛作用和家兔的体外抗凝活性,并观察其对胶原-肾上腺素合剂诱导小鼠体内血栓形成的保护作用。方法采取热板法测定Ento-Ⅰ涂膜剂的镇痛作用;通过胶原-肾上腺素合剂诱导小鼠体内血栓形成模型,观察Ento-Ⅰ涂膜剂对小鼠死亡数、小鼠偏瘫恢复数、小鼠偏瘫开始形成时间、小鼠生存时间及小鼠偏瘫恢复时间的影响;通过家兔预防给药,测定家兔血浆凝血酶时间(TT)、凝血酶原时间(PT)、活化部分凝血活酶时间(APTT),以研究Ento-Ⅰ涂膜剂的抗凝活性。结果热板镇痛法实验结果显示,与生理盐水组比较,Ento-Ⅰ涂膜剂组能显著延长小鼠给药后30、60和90min的痛阈值(P<0.01);且涂膜剂能有效降低胶原蛋白-肾上腺素诱导小鼠血栓性偏瘫引起的死亡率,提高小鼠偏瘫恢复率(P<0.05)。与波立维组比较,Ento-Ⅰ涂膜剂2 mg/kg组能明显缩短小鼠偏瘫恢复时间(P<0.05)。与生理盐水组比较,Ento-Ⅰ涂膜剂4.65 mg/kg组能显著延长家兔血浆TT、PT和APTT(P<0.05、P<0.05和P<0.01)。结论 Ento-Ⅰ涂膜剂具有镇痛、抗凝、抗血栓形成作用,是一种有临床应用前景的治疗血栓性疾病的药物。Objective To investigate the analgesic effect and the in vitro anticoagulation activity of Ento-Ⅰ,along with its protective effect against the formation of collagen-adrenaline induced thrombus. Methods The threshold of pain in mice was deter mined with the method of hot plate. Mice thrombogenesis induced by collagen-epinephrine mixture injected through tail-vein was adopted for observing the mortality,hemiplegia recovery rates,hemiplegia formation time,survival time and time for hemiplegia recovery in mice to evaluate the protective effects of test drugs against thrombus in vivo. Anticoagulation effects of test drugs were detected by measuring the thrombin time（TT）,prothrombin time（PT）,and activated partial thromboplastin time（APTT）of rabbits with in vitro clotting model. Results The experiment of hot plate for analgesia showed that compared with those of normal control group Ento-Ⅰplastic could significantly prolong pain thresholds in mice at 30,60 and 90 min after final administration（P0.01）. The mortality of collagen-epinephrine induced thrombotic hemiplegia was reduced while its recovery rates were significantly increased for mice administered Ento-Ⅰplastic（P0.05）. Compared with clopidogrel group,Ento-Ⅰplastic 2 mg/kg could effectively reduce the time for hemiplegia recovery（P0.05）. In addition,compared with substrate matrix group,Ento-Ⅰplastic（4.65 mg/kg）could significantly prolong TT,PT,and APTT in rabbit plasma（P0.05,P0.05 and P0.01）. Conclusion The Ento-Ⅰplastic possesses analgesic effect,anti coagulability and antithrombotic activity,and it may be a promising medicine for the treatment of thrombotic diseases.

关 键 词：镇痛 抗凝 抗血栓形成 

分 类 号：R285.5[医药卫生—中药学]