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低分子量肝素的非抗凝血活性——综述

Non-Anticoagulant Activities of Low Molecular Weight Heparins-A Review.

作者信息

Feng Ke, Wang Kaixuan, Zhou Yu, Xue Haoyu, Wang Fang, Jin Hongzhen, Zhao Wei

机构信息

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Nankai University, 38 Tongyan Road, Jinnan District, Tianjin 300350, China.

Department of Stomatology, Tianjin Nankai Hospital, 6 Changjiang Road, Nankai District, Tianjin 300100, China.

出版信息

Pharmaceuticals (Basel). 2023 Sep 5;16(9):1254. doi: 10.3390/ph16091254.

Abstract

Low molecular weight heparins (LMWHs) are derived from heparin through chemical or enzymatic cleavage with an average molecular weight (Mw) of 2000-8000 Da. They exhibit more selective activities and advantages over heparin, causing fewer side effects, such as bleeding and heparin-induced thrombocytopenia. Due to different preparation methods, LMWHs have diverse structures and extensive biological activities. In this review, we describe the basic preparation methods in this field and compare the main principles and advantages of these specific methods in detail. Importantly, we focus on the non-anticoagulant pharmacological effects of LMWHs and their conjugates, such as preventing glycocalyx shedding, anti-inflammatory, antiviral infection, anti-fibrosis, inhibiting angiogenesis, inhibiting cell adhesion and improving endothelial function. LMWHs are effective in various diseases at the animal level, including cancer, some viral diseases, fibrotic diseases, and obstetric diseases. Finally, we briefly summarize their usage and potential applications in the clinic to promote the development and utilization of LMWHs.

摘要

低分子量肝素(LMWHs)是通过化学或酶促裂解从肝素衍生而来,平均分子量(Mw)为2000 - 8000道尔顿。与肝素相比,它们表现出更具选择性的活性和优势,副作用更少,如出血和肝素诱导的血小板减少症。由于制备方法不同,低分子量肝素具有多样的结构和广泛的生物活性。在本综述中,我们描述了该领域的基本制备方法,并详细比较了这些特定方法的主要原理和优势。重要的是,我们关注低分子量肝素及其缀合物的非抗凝药理作用,如防止糖萼脱落、抗炎、抗病毒感染、抗纤维化、抑制血管生成、抑制细胞粘附和改善内皮功能。低分子量肝素在动物水平上对各种疾病有效,包括癌症、一些病毒性疾病、纤维化疾病和产科疾病。最后,我们简要总结它们在临床上的用法和潜在应用,以促进低分子量肝素的开发和利用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3ad8/10537022/25710685b720/pharmaceuticals-16-01254-g001.jpg

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