Photosensitized lysis of red blood cells by phototoxic antimalarial compounds.
A family of 12 phototoxic quinolinemethanol antimalarials and three other non-phototoxic clinically used compounds were irradiated in the presence of red blood cells to determine if the resulting hemolysis would be a reliable predictor of phototoxicity. The most phototoxic compounds from in vivo tests were also the most phototoxic in this study. Quinine caused little RBC lysis, paralleling its non-phototoxicity in humans. The quinolinemethanol-induced photohemolysis occurs both in the presence and absence of oxygen. Enriching the RBC with BHA and cholesterol was particularly effective at protecting the cells from photohemolysis. Other compounds offered some measure of protection, while superoxide dismutase and sodium azide, among others, afforded no protection.
D000962:Antimalarials / Q000494:pharmacology*; D004912:Erythrocytes / Q000187:drug effects / Q000528:radiation effects*; D006461:Hemolysis / Q000187:drug effects / Q000528:radiation effects*; D006801:Humans; D014466:Ultraviolet Rays
D000962:Antimalarials