Interactions of chloroquine with different glycerophospholipids.

Amphiphilic drugs are able to accumulate acidic phospholipids in different animal tissues, such as the pineal gland, iris muscle, retina and also in lymphocytes. Chloroquine, an amphiphilic cation, causes a phospholipidosis in liver. Not only is the phospholipid content markedly increased but an unusual acidic glycerophospholipid bis(monoacylglycero)phosphate is enriched many-fold in rat liver lysosomes if the animals have been treated with this drug. Since we found bis(monoacylglycero)-phosphate to be present in these cell organelles of untreated animals in only small amounts, we wanted to prove that chloroquine is able to react with lipids. If this were the case, we were interested in the kind of interactions taking place between the drug and the lipids.