Immobilization of alpha-[di-(beta-chloroethyl)-amide]-N-(m-nitrobenzoyl)-D,L-asparagic acid on xanthan.
The paper studies the coupling reaction, through ester-type covalent bonds, of an oxazolone derived from the N-(m-nitrobenzoyl)-L-asparagic acid, the cycle of which is opened with an N-mustard derivative, on xanthan (a polysaccharide of microbian synthesis), in conditions of activation with dicyclohexyl carbodiimide. The coupling product has been characterized through elemental analysis and IR spectroscopy. For the establishment of the capacity of the active principle's controlled release by the polymer-active principle system thus obtained, active principle's release kinetics from the polysaccharide support, in conditions of basic hydrolysis, is studied. In vivo tests realized on mice proved the antitumoral activity of the compounds resulted by chemical bonding of the N-mustard derivative on xanthan.
Marcel
Popa
P
Department of Macromolecules, Gh.Asachi Technical University of Iaşi Bd. D. Mangeron, No. 71 A 6600 Iaşi, Romania. marpopa@ch.tuiasi.ro
Lăcrămioara
Bălăită Rusu
BR
Valeriu
Sunel
S
D000284:Administration, Oral; D000327:Adsorption; D000818:Animals; D001224:Aspartic Acid / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000633:toxicity; D002277:Carcinoma / Q000188:drug therapy*; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000633:toxicity; D005260:Female; D008297:Male; D051379:Mice; D009588:Nitrogen Mustard Compounds / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000633:toxicity; D011135:Polysaccharides, Bacterial / Q000737:chemistry*; D016019:Survival Analysis; D016896:Treatment Outcome
D003692:Delayed-Action Preparations; D009588:Nitrogen Mustard Compounds; D011135:Polysaccharides, Bacterial; D001224:Aspartic Acid; C002563:xanthan gum