Preparation and antithrombogenic activities of heparinoid from 6-O-(carboxymethyl)chitin |
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| Affiliation: | 1. Laboratory of Pharmaceutical Microbiology, Ghent University, Ghent, Belgium;2. Laboratory of General Biochemistry and Physical Pharmacy, Ghent University, Ghent, Belgium;3. Centre for Nano- and Biophotonics, Ghent University, Ghent, Belgium;4. Laboratory of Pharmaceutical Biotechnology, Ghent University, Ghent, Belgium;5. Research Core Unit Metabolomics, Hannover Medical School, Hannover, Germany;1. Institute of Problems of Chemical Physics, Russian Academy of Sciences, Chernogolovka 142432, Russian Federation;2. P.G. Demidov Yaroslavl State University, Yaroslavl 150000, Russian Federation |
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| Abstract: | The highest antithrombogenic activity was achieved by the sulphation of partially N-deacetylated O-(carboxymethyl)chitin among variously modified chitin derivatives. It was also suggested that the distribution of N-sulphate and N-acetyl groups on the C-2 position might be essential to the selective binding by antithrombin-III to inhibit thrombin activity. Kinetic evaluations demonstrated the non-competitive inhibition on direct interaction with thrombin (Ki = 9.26 × 10−8m) and the competitive inhibition with antithrombin-III (Ki = 3.33 × 10−8) m as well as with heparin. 6-O-Carboxymethyl groups were found, from the data of intravenous injection in mice, to suppress the toxicity of chitin heparinoids. |
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