Fig. 3: Screening of chemical libraries against NF54/iGP1_RE9Hulg8 stage V gametocytes.
Results from the primary screening of small- to medium-sized compound libraries. A–C Effect of compounds of the Epigenetics Screening Library (Cayman Chemical) (A), human kinase inhibitors (SelleckChem, Enzo Life Sciences) (B) or compounds of the Prestwick Chemical Library (C) on NF54/iGP1_RE9Hulg8 stage V (day 12) gametocyte viability (1 µM concentration). Each assay plate included eight treated (50 µM MB; blue dots) and untreated (0.1% DMSO; orange dots) samples each as positive and negative controls, respectively. Values on the y-axis represent RLUs normalized to the mean signal emitted from the negative controls, obtained from n = 1 experiment for each library. Compounds with >50% inhibitory activity (blue shaded areas) are highlighted by numbers (1, SGI-1027; 2, SU4312; 3, monensin; 4, alexidine dihydrocholride; 5, indoprofen; 6, equilin). D Dose-response curves of SGI-1027, monensin and alexidine dihydrochloride tested against NF54/iGP1_RE9Hulg8 stage V gametocytes (day 12). Values on the y-axis represent RLUs normalized to the mean signal emitted from cells exposed to the lowest drug concentration, obtained from n = 3 biological replicates (mean ± s.e.m.) E Dose-response curves of SGI-1027, monensin and alexidine dihydrochloride tested against NF54 wild type asexual blood stage parasite multiplication. Values on the y-axis represent [3H]-hypoxanthine incorporation normalized to the mean signal emitted from eight untreated control samples per plate, obtained from n = 3 biological replicates (mean ± s.e.m.). IC50 values and 95% confidence intervals (CI) are indicated below the graphs.
