Effect of a new 8-aminoquinoline antimalarial compound on hepatic microsomal mixed function oxidase system of mice.

ABSTRACT

A new 8-aminoquinoline derivative (compound 80/53) synthesized at the Central Drug Research Institute, Lucknow (India), has been found to be an active anti-relapse (tissue schizontocidal) compound. Compound 80/53 at 8.75 mg/kg x 4 days and primaquine at 7.00 mg/kg (base) x 4 days given orally to Swiss mice led to inhibition of the different components of the hepatic microsomal mixed function oxidase system to varying degrees. Compound 80/53 inhibited cytochrome P-450, aminopyrine-N-demethylase, aniline and benzo (a) pyrene hydroxylase, cytochrome b5 and heme content of the normal mice by 12, 14, 0, 57, 20 and 6 per cent respectively, whereas the inhibition caused by primaquine in these components was 25, 21, 17, 48, 26 and 6 per cent respectively. Thus, there was less inhibition of hepatic microsomal MFO system of mice by compound 80/53 as compared to that by primaquine.