Figure 3
From: Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites
Gametocytocidal activity of the selected epi-drugs against early and late stage gametocytes of P. falciparum. (A) Compounds were screened using the pLDH assay to determine dose-response against early (>85% stage II and III, EG) and late (>95% stage IV/V, LG) gametocytes after drug pressure for 72 h. Positive assay controls included MMV390048 and Methylene Blue while the negative controls included culture media supplemented with erythrocytes and untreated gametocytes to monitor background and viability, respectively. Data are represented as a percentage of untreated control. Sigmoidal dose-response curves were plotted using GraphPad 6.0 (www.graphpad.com), from which the IC50 values could be determined (data also provided in Supplementary Data File). Results for all compounds are representative of three independent biological replicates (n = 3 ± SEM), except for HC Toxin, LG Scriptaid, EG Sirtinol (n = 2). Where not show, error bars fall within the symbol. (B) The ability of selected compounds to inhibit male gamete formation at 2 µM drug pressure. Activity on male gametes on the exflagellation inhibition assay for two independent biological repeats from at least 15 videos per repeat, ± SEM. The positive control, MB (Methylene Blue) is shown with 100% inhibition of male exflagellation.
