A novel validated assay to support the discovery of new anti-malarial gametocytocidal agents

Malaria Journal

Table 1 Characteristics of the anti-malarial compounds tested in the assay

Compound^e	Structure	P.f. gametocytes IC₅₀ (µM)	TOX50 (µM)^b	Assay concentration (µM)^c
Chloroquine^d	–	23.47	51.84	5.00
Methylene blue	–	0.49	6.52	5.00
Dihydroartemisinin	–	3.56	>50	71.20
Epoxomicin	–	0.0005	0.003	0.001
Thiostrepton	–	0.90	–	18.00
TCMDC-134278		>5	19.95	NT
TCMDC-136869		1.66	12.59	NT
TCMDC-125520		0.0098	12.80	0.20
TCMDC-123475		0.0098	>25	0.20
TCMDC-125133		0.54	>50	10.76
TCMDC-125769		0.04	>25	0.86
TCMDC-125114		0.13	>50	2.60

^aIC₅₀ values measured in the laboratory for 3D7A P. falciparum mature gametocytes with the ATP bioluminescence assay [24]
^bCytotoxicity data using the short-term resazurin-based reductase assay [24]
^cWorking concentrations were 20 × IC₅₀ if that was below the TOX₅₀
^dWorking concentration of chloroquine was 5 µM corresponding to ×125 the asexual IC₅₀
^eGSK compounds were published in Ref. [23]

ISSN: 1475-2875