SYNTHESIS OF TRITERPENE POLYMER CONSTRUCTIONS

Abstract

The pentacyclic triterpenoids betulin and betulonic acid are promising sources of new biologically active compounds. Grafting them onto polymer matrices leads to the formation of effective dosage forms compared to the original drug. On the basis of betulin and betulonic acid, the synthesis of polymer structures with a fragment of triterpene in the side chain was carried out. New triterpene-containing polymer ensembles were obtained by the method of polymer-analogous transformations of copolymers of N-vinylpyrrolidone with N-(n-carboxy) phenylmaleimide and p-aminostyrene. By crosslinking the carboxyl groups of the copolymer of N-vinylpyrrolidone with N-(n-carboxy) phenylmaleimide with betulin hydroxyl groups and the reaction of the amino groups of the copolymer of N-vinyl pyrrolidone with p-aminopyrol with carboxyl groups of betulonic acid, polymer structures with polycyclic triterpene fragments are obtained. The resulting polymer ensembles have higher activity against melanoma compared to the original copolymers. A polymer based on a copolymer of N-vinylpyrrolidone with N-(n-carboxy) phenylmaleimide and betulin at a concentration of 40.48 μM inhibits 50% of MS cells, while 50% of MS cells die under the influence of 68.29 μM betulin. New triterpene-containing polymer ensembles are promising for the development of new biologically active polymer bioconjugates.