Figure 6. Screening of in vitro hits from TCAMS in thePlasmodium berghei ED₉₀-normalized in vivo assay.

(A) A collection of 590 compounds were screened at 50 mg/kg in 20% Captisol® given orally (open circles, open diamonds, open triangles). The series consisted of a first experiment of 50 compounds followed by 5 experiments of 100 compounds each and three additional experiments with 20, 7, and 13 compounds, respectively. Each experiment included a control group treated with vehicle (closed diamond) as a reference to calculate the percentage of inhibition of parasitemia in peripheral blood (dotted line). The response of standard antimalarials in the same assay is also presented (closed circles). Data shown are the mean log₁₀ [parasitemia at day 4] of two mice per point. Open squares indicate compounds with YOYO-1_530/585 flow cytometry patterns similar to chloroquine (CQ-like, potential fast killing compounds) whereas open triangles mark compounds with patterns similar to pyrimethamine (Pyr-like, potential non-fast killing compounds). (B) Patterns of YOYO-1_530/585 flow cytometry method at day 4 for vehicle-, chloroquine- and, pyrimethamine-treated mice.