Release of 5‐aminosalicylic acid from bioadhesive N‐(2‐hydroxypropyl)methacrylamide copolymers by azoreductases in vitro

摘要: N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers (11a, b) containing side chains terminating in 5-aminosalicylic acid (5-ASA) and fucosylamine (10) were synthesized. A reactive polymeric precursor (9), a copolymer of HPMA (7) N-methacryloylglycylglycine p-nitrophenyl ester (8), was consecutively aminolyzed with 5-[4-(2-aminoethylcarbamoyl)phenylazo]-salicylic (6) (10). The latter renders the bioadhesive gastrointestinal tract. release 5-ASA from 11a, b studied vitro by incubation cell-free extracts isolated rat cecum, factors influencing degradation determined. rate azo bond cleavage similar to low-molecular-weight substrates, methyl orange compound 6. Addition benzyl viologen, low potential electron carrier, increased cleavage. At optimal viologen substrate concentration ratios, zero order observed. higher concentration, decreased.