The Screening and Evaluation of Experimental Antiparasitic Drugs

Malaria chemotherapeutic studies included a primary antimalarial blood schizontocidal test system (MM test) where 1502 compounds were evaluated against Plasmodium berghei with 168 exhibiting activity, and a secondary antimalarial program consisting of in depth evaluation of compounds against drug-sensitive and drug-resistant lines. Arteether in sesame oil was more active SC than PO. Chloroquine and primaquine were less toxic when given in fish oil. One sustained release formulation of qinghaosu was more active than another. Two stereoisomers (R and S) of a floxacrine analog interacted synergistically against malaria. Resistance to the R-stereoisomer developed slower than the S- stereoisomer or the racemate. A line resistant to quinghaosu was developed. Suplemental vitamin E did not alter the activity of several standard antimalarials. Changing the fatty acid profile in red blood cells by feeding plant and fish oils containing high levels of omega-3 polyunsaturated fatty rendered vitamin E-deficient mice cured of drug-sensitive, chloroquine or qinghaosu-resistant malaria.