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S-己基-L-半胱氨酸衍生物在肝素存在下对凝血酶原激活和凝血时间的影响。

Effects of S-hexyl-L-cysteine derivatives on prothrombin activation and clotting time determined in the presence of heparin.

机构信息

Department of Organic Chemistry, Medical University of Bialystok, Bialystok, Poland.

出版信息

Adv Med Sci. 2009;54(1):47-50. doi: 10.2478/v10039-009-0013-8.

DOI:10.2478/v10039-009-0013-8
PMID:19648086
Abstract

PURPOSE

The aim of the study is the examination of effects of dipeptides containing S-hexyl-L-cysteine and glycine, on the prothrombin activation and the thrombin clotting time determined in the presence of heparin.

MATERIAL AND METHODS

The activation of prothrombin was determined with the use of the thromboplastin test, the recalcification and partial thromboplastin with kaolin tests. The thrombin clotting time determined in the presence of heparin was evaluated with the use of the heparin-thrombin test.

RESULTS

The investigated derivatives slightly inhibited the prothrombin activation. The unsubstituted derivatives and dipeptides with a free amino or carboxyl group significantly enhanced the clotting time determined in the presence of heparin at concentration 20 mM. S-Hexyl-L-cysteinylglycine (H-(S-hexyl)-L-Cys-Gly-OH) was the most active compound.

CONCLUSIONS

The obtained results indicate that some dipeptide derivatives of S-hexyl-L-cysteine apart from the earlier observed possibility to prolong the thrombin clotting time, can also prolong the clotting time determined in the presence of heparin.

摘要

目的

本研究旨在考察含 S-己基-L-半胱氨酸和甘氨酸的二肽对凝血酶原激活和肝素存在下凝血酶凝固时间的影响。

材料与方法

采用凝血酶原测试、复钙和高岭土部分凝血酶原测试来测定凝血酶原的激活。肝素-凝血酶测试用于评估肝素存在下凝血酶凝固时间。

结果

研究的衍生物对凝血酶原的激活略有抑制。未取代的衍生物和具有游离氨基或羧基的二肽在 20mM 浓度下显著延长了肝素存在下的凝血时间。S-己基-L-半胱氨酰甘氨酸(H-(S-己基)-L-Cys-Gly-OH)是最具活性的化合物。

结论

研究结果表明,S-己基-L-半胱氨酸的某些二肽衍生物除了先前观察到的延长凝血酶凝固时间的可能性外,还可以延长肝素存在下的凝血时间。

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