赵晓瑜, 刘泽民, 静天玉, 武金霞, 赵专友. 一种体内溶栓活性优于总蚯蚓纤溶酶的组分J. 药学学报, 2006, 41(11): 1068-1073.
引用本文: 赵晓瑜, 刘泽民, 静天玉, 武金霞, 赵专友. 一种体内溶栓活性优于总蚯蚓纤溶酶的组分J. 药学学报, 2006, 41(11): 1068-1073.
ZHAO Xiao-yu, LIU Ze-ming, JING Tian-yu, WU Jin-xia, ZHAO Zhuan-you. A component of earthworm fibrinolytic enzyme having higher thrombolytic activity than total components in vivoJ. Acta Pharmaceutica Sinica, 2006, 41(11): 1068-1073.
Citation: ZHAO Xiao-yu, LIU Ze-ming, JING Tian-yu, WU Jin-xia, ZHAO Zhuan-you. A component of earthworm fibrinolytic enzyme having higher thrombolytic activity than total components in vivoJ. Acta Pharmaceutica Sinica, 2006, 41(11): 1068-1073.

一种体内溶栓活性优于总蚯蚓纤溶酶的组分

A component of earthworm fibrinolytic enzyme having higher thrombolytic activity than total components in vivo

  • 摘要: 目的筛选高效低毒的蚯蚓纤溶酶单一组分。方法通过亲和色谱从赤子爱胜蚓获得含多组分的总蚯蚓纤溶酶(EFE),经离子交换分离得到3个主要溶栓组分EfP-0-2,EfP-I-1和EfP-I-2,与EFE比较体内外溶栓效果和毒副作用。结果与其他组分比较,EfP-I-1的体外溶栓作用较强;当静脉注射4.5 mg·kg-1时,各组分对纤维蛋白原的影响均不明显,只有EfP-I-1能显著溶解动静脉旁路血栓;当静脉注射达6 mg·kg-1时,只有该组分对延长出血时间的影响不明显;急性毒性实验表明,该组分的LD50是EFE的2.17倍。结论EfP-I-1有较高的体内外溶栓活性和较低的毒副作用。由于该组分在总EFE中所占比例较高,并易于分离纯化,故适于作为单一组分的溶栓药物进行开发。

     

    Abstract: AimTo select higher thrombolytic and lower toxic single component of earthworm fibrinolytic enzymes (EFE). MethodsEFE containing total components were obtained by affinity chromatography from Eisenia fetida. Using ion-exchange chromatography to separate three main components EfP-0-2, EfP-I-1 and EfP-I-2 from EFE, their thrombolytic activity and toxicity were compared with EFE. ResultsAmong these components, EfP-I-1 had higher thrombolytic activity in vitro. When 4.5 mg·kg-1 of these components were injected, the contents of fibrinogen in rat serum were not affected , but only EfP-I-1 exhibited distinct thrombolytic activity. When 6.0 mg·kg-1 of them were injected intravenously, the bleeding time was not evidently delayed only by EfP-I-1. The acute toxicity test showed that the LD50 of EfP-I-1 was higher than EFE by 2.17 times. ConclusionBecause of distinct thrombolytic activity, lower toxicity in vivo, higher content in EFE and easy to purify, EfP-I-1 was adapted to be developed as a single component medicine for treating thrombus.

     

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