Table 2 Activity of selected epi-drugs against P. falciparum gametocytes. Compounds were screened for IC50 against the NF54 strain using the parasite lactate dehydrogenase assay. The selectivity index (SI) for each compound is shown. Compounds with SI > 10 are in bold. Results for all compounds are representative of three independent biological replicates with technical triplicates (n = 3, IC50 ± SEM) unless otherwise indicated as represented by a “not determined”.

From: Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites

Compound name

IC50 (μM) against P. falciparum NF54 gametocytes

IC50 human cell line (μM)a

SI (based on NF54 IC50)

EG

LG

Sirtinol

157.15 ± 7.42

0.1303 ± 0.0146

43

383.93

Scriptaid

1.813 ± 0.874

0.8203 ± 0.02757b

2

1.82

CAY10603

1.577 ± 0.767

1.3 ± 0.29

10.8

8.33

Chaetocin

0.92 ± 0.289

1.342 ± 0.175

0.285

0.212

ITF2357

2.978 ± 0.874

2.234 ± 0.095

0.2

0.09

HC Toxin

1.951 ± 0.8655b

1.915 ± 0.3105b

0.03

0.01

Oxamflatin

1.12 ± 0.629

3.001 ± 0.42

0.25

0.08

BIX01294

0.014 ± 0.002

5.862

11

1.88

UNC0638

1.855 ± 0.448

0.442 ± 0.178

23

1.1

C646

>5

>5

10

0.47

  1. aActivity data of the compounds on various mammalian lines were collated from previous reports15,21,41,49,65,66,67,68,69,70,71.
  2. bData are representative two (n = 2) independent biological replicates with technical triplicates.
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