Fucosylated heparin pentasaccharide as well as preparation method and application thereof

By modularly synthesizing fucoidan-heparin pentasaccharide, the problems of high bleeding risk and difficulty in synthesizing nonasaccharide in existing anticoagulant drugs have been solved, realizing the development of a potent and safe anticoagulant drug suitable for the treatment of thrombotic diseases.

CN122080097APending Publication Date: 2026-05-26GUANGXI UNIV OF CHINESE MEDICINE
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Patent Information

Application Number
CN202610132774.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-01-30
Publication Date
2026-05-26

AI Technical Summary

Technical Problem

Existing anticoagulants such as enoxaparin sodium have significant adverse bleeding reactions, which limit the therapeutic window and patient compliance. Furthermore, the chemical synthesis of the nonaglycone structure is difficult and cannot be scaled up, thus hindering the development of new anticoagulants.

Method used

By using fucoidan to pentose heparin, a nonaglycone analog was constructed by combining the sulfated fucoidan side chain with the heparin pentose backbone through modular synthesis, which retained FXase inhibitory activity and reduced preparation cost.

Benefits of technology

Fucosylated heparin pentasaccharide exhibits potent anticoagulant activity, selectively inhibits FXase, and significantly reduces bleeding tendency. It is characterized by high efficacy and low toxicity, making it suitable for preparing drugs or functional foods for the treatment of thrombotic cardiovascular diseases.

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Abstract

The invention belongs to the fields of medicinal chemistry, carbohydrate chemistry and biological medicine, and provides fucosylated heparin pentasaccharide as well as a preparation method and application of the fucosylated heparin pentasaccharide. According to the preparation method, a target product is obtained through chemical connection and purification of sulfated azidoethyl-alpha-L-fucopyranoside and alkynylated heparin pentasaccharide. The compound plays an anticoagulant and antithrombotic role by strongly inhibiting an endogenous blood coagulation factor X enzyme complex (FXase), APTT extension and FXase inhibitory activity of the compound are remarkably superior to those of heparin pentasaccharide, the bleeding risk is remarkably reduced under the equivalent anti-suppository dose, and the compound can be used for developing drugs or functional foods for treating thrombotic cardiovascular and cerebrovascular diseases.
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