Sulfated derivatives of fucosylated chondroitin sulfate oligosaccharides and uses thereof

By preparing sulfated fucosylated chondroitin sulfate oligosaccharide derivatives (S-dFCS), the problem of insufficient antitumor activity of fucosylated chondroitin sulfate in the prior art has been solved, achieving efficient and safe inhibition of tumor metastasis and expanding its application in the prevention and treatment of tumor metastasis after surgery.

CN117510679BActive Publication Date: 2026-01-09OCEAN UNIV OF CHINA
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Patent Information

Application Number
CN202311469593.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-11-07
Publication Date
2026-01-09
Estimated Expiration
2043-11-07

AI Technical Summary

Technical Problem

In the existing technology, there is insufficient research on the anti-tumor activity of fucosylated chondroitin sulfate (FCS), and chemotherapy drugs are not effective against circulating cells with low tumor cell proliferation rates, making it difficult to control tumor metastasis and recurrence. Postoperative metastasis leads to serious consequences, and there is a lack of safe and effective drug prevention and treatment methods.

Method used

We developed a sulfated derivative of chondroitin sulfate oligosaccharide (S-dFCS). By sulfating specific sites on the main chain and side chain, we prepared S-dFCS with a sulfation degree of 40% to 60% and a molecular weight between 500 Da and 20,000 Da. This S-dFCS was used to interact with adhesion molecules P,L-selectin and vascular endothelial growth factor (VEGF) to inhibit tumor cell adhesion and angiogenesis.

Benefits of technology

S-dFCS significantly inhibits tumor cell migration and angiogenesis, effectively preventing and treating tumor metastasis. In vitro and in vivo experiments show that it is superior to unmodified oligosaccharides and has no toxic side effects. It is suitable for use in combination with chemotherapy and targeted drugs to improve treatment efficacy.

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Abstract

The application provides sulfated derivatives of fucosylated chondroitin sulfate oligosaccharides and application thereof, and belongs to the technical field of marine drugs. The structure of the sulfated derivatives of fucosylated chondroitin sulfate oligosaccharides is mainly a disaccharide repeating unit with GlcA and GalNAc connected through a beta-1,3 / beta-1,4 glycosidic bond as a main chain, and a fucose connected to the O-3 position of GlcA as a side chain; sulfation occurs at any 1-3 positions of C4 and / or C6 of the acetylglucosamine in the main chain, and C2,3,4 of the fucose in the side chain. Through in-vivo and in-vitro level verification, the application plays an anti-tumor metastasis role by significantly inhibiting the adhesion of tumors to endothelium, platelets and the like and tumor angiogenesis, so as to use S-dFCS as an active substance, prepare a medicine or a health product with the aid of a pharmaceutically acceptable carrier, and be capable of being used for preventing and treating tumors and diseases related to postoperative metastasis.
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