Distribution of key ions of chloroquine biotransformation and cholesterol uptake in rat liver

Abstract

Oral administration to rats of chloroquine (5 mg/kg) three times per week for 8 weeks was investigated in two nutritionally compounded diets. It was observed that ferrous ion was preferentially retained in the presence of high (25%) protein diet even though all other ions, Ca²⁺, Mg²⁺ and K⁺ had varying uptake. The study shows no effect on the utilization of glucose and acid phosphatase. The difference in the level of lactate dehydrogenase (LDH) in both diets was not statistically significant. However, the level of cholesterol was significantly lower in both high and low protein diets when compared to control, suggesting that chloroquine biotransformation may interact with cholesterol metabolism in an unknown manner. The decrease in total cholesterol content corresponds to a similar decrease in malondialdehyde formation (lipid peroxidation). This result suggests that the biologic effects of chloroquine including its antimalarial action may be directly related to its lysosomotrophism.