[1]龙莎,吕卓伦,李小红,等.单环刺螠纤溶酶的季节积累及初步药效学[J].华侨大学学报(自然科学版),2018,39(4):583-588.[doi:10.11830/ISSN.1000-5013.201711035]
 LONG Sha,Lü Zhuolun,LI Xiaohong,et al.Seasonal Accumulation of Monocyclic Thrips Fibrinolytic Enzyme UFE and Preliminary Pharmacodynamic Study of UFE[J].Journal of Huaqiao University(Natural Science),2018,39(4):583-588.[doi:10.11830/ISSN.1000-5013.201711035]
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单环刺螠纤溶酶的季节积累及初步药效学()
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《华侨大学学报(自然科学版)》[ISSN:1000-5013/CN:35-1079/N]

卷:
第39卷
期数:
2018年第4期
页码:
583-588
栏目:
出版日期:
2018-07-18

文章信息/Info

Title:
Seasonal Accumulation of Monocyclic Thrips Fibrinolytic Enzyme UFE and Preliminary Pharmacodynamic Study of UFE
文章编号:
1000-5013(2018)04-0583-06
作者:
龙莎1 吕卓伦1 李小红2 宋伟杰3 王立强1
1. 华侨大学 生物医学学院, 福建 泉州 362021;2. 广州优米健医药科技有限公司, 广东 广州 510000; 3. 中国人民解放军第211医院, 黑龙江 哈尔滨 150080
Author(s):
LONG Sha1 Lü Zhuolun1 LI Xiaohong2 SONG Weijie3 WANG Liqiang1
1. School of Biomedical Sciences, Huaqiao University, Quanzhou 362021, China; 2. Guangzhou Youmijian Pharmaceutical Technology Company Limited, Guangzhou 510000, China; 3. No. 211 Hospital of PLA, Harbin 150080, China
关键词:
单环刺螠 单环刺螠纤溶酶 抗凝血 溶栓 季节累积性 药效学
Keywords:
Urechis unicinctus Urechis unicinctus fibrinolysin enzymes anticlotting thrombolytic seasonal accumulation pharmacodynamics
分类号:
R944
DOI:
10.11830/ISSN.1000-5013.201711035
文献标志码:
A
摘要:
研究单环刺螠纤溶酶(UFE)的季节累积规律,并验证UFE的药效学.首先,将不同季节采收的单环刺螠体腔液通过离心、葡聚糖凝胶过滤、阴离子交换层析等工艺进行分离、提纯,获得单一组分.然后,使用聚丙烯酰胺凝胶电泳(SDS-PAGE)测定UFE的相对分子质量,用Folin-酚试剂法测定其活力.最后,通过体内、外溶栓实验和大鼠脑中动脉栓塞模型来考察UFE的抗凝血和溶血栓作用.结果表明:从秋季批单环刺螠中分离纯化的UFE比活力达到194.57 nkat·mg-1,纯化倍数为17.9倍,回收率为16.9%,与春季批、夏季批结果相比有统计学意义.药效学实验证实:UFE与尿激酶类似,能明显延长体外凝血时间,有效抑制体内血栓形成;UFE的活性与季节变化相关,具有季节累积性;UFE具有显著的抗凝血和溶栓作用,且无溶血毒性.
Abstract:
The season cumulative rules of the monocyclic sting fibula plasmin was studied, and the pharmacodynamics of Urechis unicinctus fibrinolysin enzymes(UFE)was verified. The mononuclear stinger fluid collected in different seasons was separated and purified by centrifugation, dextrane gel filtration and anion exchange chromatography to obtain single component. And then, the relative molecular weight of UFE was determined by polyacrylamide gel electrophoresis(SDS-PAGE), the activity of UFE was measured by Folin-phenol reagent method, and the anticoagulant effect and thrombolytic effect of UFE was evaluated by in vivo and in vitro thrombolysis tests and arterial embolism model in rat brain. The results showed that the specific activity of UFE isolated and purified from Monochamus alternatus in autumn was 11.672 μkat·mg-1, the purification fold was 17.9 folds, and the recovery rate was 16.9%, which was significantly different from the spring batch and summer batch results. Pharmacodynamics experiments confirmed that UFE was similar to urokinase, which could prolong the clotting time in vitro significantly, and inhibit thrombosis in vivo effectively. In addition, the content of UFE was related to the seasonal change and had season accumulation. Besides, UFE had a significant anticoagulant and thrombolytic effect with no hemolysis toxicity.

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备注/Memo

备注/Memo:
收稿日期: 2017-12-11
通信作者: 王立强(1970-),男,教授,博士,主要从事药剂学和创新药物研发的研究.E-mail:wlq1599@163.com.
基金项目: 国家重点研发计划资助项目(2016YFE0101700); 福建省自然科学基金资助项目(2015J01342); 华侨大学研究生科研创新基金资助项目(1611316003)
更新日期/Last Update: 2018-07-20