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水蛭素的回归——一种老牌抗凝剂。

The comeback of hirudin--an old-established anticoagulant agent.

作者信息

Markwardt F

机构信息

Institute of Pharmacology and Toxicology, Medical Academy Erfurt, GDR.

出版信息

Folia Haematol Int Mag Klin Morphol Blutforsch. 1988;115(1-2):10-23.

PMID:2459000
Abstract

Early studies dating back to 1884 revealed that extracts from medicinal leeches contain a substance which is able to prevent blood from clotting. Since our successful isolation of hirudin, the pure anticoagulant substance, in the late 1950s and its characterization as a selective thrombin inhibitor with polypeptide structure, hirudin preparations have been employed for diagnostic and scientific uses in haemostaseology. As early as 25 years ago we have shown in experimental pharmacotoxicological studies that hirudin is an anticoagulant of high quality. The antithrombotic effect of hirudin was demonstrated in several thrombosis models. But the clinical use of hirudin remained limited since it was not available in adequate amounts for therapeutic purposes. One hundred years after its discovery there is a renewed interest in this naturally occurring thrombin inhibitor. Advanced methods of peptide isolation and genetic engineering are about to provide sufficient quantities of hirudin in purified form. This prompted us to resume our investigations in hirudin and to represent new experimental and clinical pharmacological studies with natural hirudin prepared from medicinal leeches and genetically engineered recombinant hirudin, thus appreciating the comeback of hirudin into the focus of interest.

摘要

可追溯到1884年的早期研究表明,药用水蛭的提取物含有一种能够防止血液凝固的物质。自20世纪50年代末我们成功分离出纯抗凝物质水蛭素,并将其鉴定为具有多肽结构的选择性凝血酶抑制剂以来,水蛭素制剂已被用于血液学的诊断和科学研究。早在25年前,我们就在实验性药物毒理学研究中表明,水蛭素是一种优质的抗凝剂。水蛭素的抗血栓形成作用在多个血栓形成模型中得到了证实。但由于水蛭素的量不足以用于治疗目的,其临床应用仍然有限。在其被发现一百年后,人们对这种天然存在的凝血酶抑制剂重新产生了兴趣。先进的肽分离方法和基因工程即将提供足够数量的纯化水蛭素。这促使我们重新开展对水蛭素的研究,并展示用从药用水蛭中制备的天然水蛭素和基因工程重组水蛭素进行的新的实验和临床药理学研究,从而认识到水蛭素重新成为人们关注的焦点。

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