Biotransformation of 9- (p-methylanilino) acridine in rabbit

The metabolic pathway of PMAA was studied with TLC and spectro-fluorophotometric method in rabbits. After ig 100 mg/kg the urine and feces were collected and extracted with CHC13 and BuOH successively. Besides PMAA, 8 metabolites were identified. It is supposed there are 2 metabolic pathways of PMAA in rabbits. The first, PMAA is converted to acridone through an unstable metabolite. The greater part of acridone is conjugated with sulfuric acid, glucuronic acid and cysteine; the smaller part of acridone is oxidized t0 2-hydroxy-acridone. In the second process, a part of PMAA is converted t0 9-aminoacridine which is, in turn, conjugated with glucu-ronic acid. The antitumor activity of PMAA was compared with that of the main metab-olites by cultured BEL-7402 cells. The metabolic biotransformation of acridone decreased the activity,but 9-aminoacridine was more active than PMAA.