磺化聚环氧乙烷及磺化聚环氧乙烷接枝聚氨酯的类肝素抗凝活性

Heparin-like anticoagulant activity of sulphonated poly(ethylene oxide) and sulphonated poly(ethylene oxide)-grafted polyurethane.

作者信息

Han D K, Lee N Y, Park K D, Kim Y H, Cho H I, Min B G

机构信息

Polymer Chemistry Laboratory, Korea Institute of Science and Technology, Cheongryang, Seoul.

出版信息

Biomaterials. 1995 Apr;16(6):467-71. doi: 10.1016/0142-9612(95)98819-z.

DOI:10.1016/0142-9612(95)98819-z

PMID:7654873

Abstract

Sulphonated poly(ethylene oxide) (PEO-SO3) and PEO-SO3-grafted polyurethane (PU-PEO-SO3) were prepared by bulk modification and their anticoagulant and heparin-like activities were investigated. Anticoagulant activity measured by activated partial thromboplastin time of PU-PEO-SO3 displayed 2%, whereas that of PEO-SO3 itself reached 14% as compared to free heparin. In addition, the anticoagulant effects of these sulphonated polymers were not due to factor Xa inhibition but mainly thrombin inhibition. From the clotting time measurements using reptilase instead of thrombin and antithrombin III (AT III), PEO-SO3 and PU-PEO-SO3 indicated heparin-like activity which represents both prolonged thrombin time (TT) and normal reptilase time and increased TT in the presence of AT III. Thrombin was also neutralized by sulphonated polymers to a great extent. Therefore, the anticoagulant and heparin-like activities of PEO-SO3 and PU-PEO-SO3 seem to contribute to their improved blood compatibility.

摘要

通过本体改性制备了磺化聚环氧乙烷（PEO-SO3）和接枝有PEO-SO3的聚氨酯（PU-PEO-SO3），并研究了它们的抗凝血和类肝素活性。与游离肝素相比，通过活化部分凝血活酶时间测定的PU-PEO-SO3的抗凝血活性为2%，而PEO-SO3本身的抗凝血活性达到14%。此外，这些磺化聚合物的抗凝血作用并非由于对因子Xa的抑制，而是主要由于对凝血酶的抑制。通过使用蛇毒凝血酶而非凝血酶和抗凝血酶III（AT III）进行凝血时间测量，PEO-SO3和PU-PEO-SO3显示出类肝素活性，表现为凝血酶时间（TT）延长、蛇毒凝血酶时间正常以及在存在AT III时TT增加。凝血酶也在很大程度上被磺化聚合物中和。因此，PEO-SO3和PU-PEO-SO3的抗凝血和类肝素活性似乎有助于改善它们的血液相容性。