Alterations in liver microsomal drug-metabolizing enzymes and phosphol
ipids following oral administration of chloroquine to rats for 14 days
were investigated. An increase in cytochrome P450 and cytochrome b(5)
contents and an increase in the activities of NADPH cytochrome c redu
ctase and NADH microsomal cytochrome reductase were observed. A decrea
se in cholesterol and an increase in phospholipids were noted in the m
icrosomal membranes, which altered the membrane fluidity, which may be
of importance in controlling different membrane functions. The increa
se in different fractions of microsomal phospholipid is probably due t
o an increased incorporation of acetate into phospholipids.