Antimalarials Active against  the Five Gametocyte Stages
Plouffe DM, Wree M, Du AY, Meister S, Li F, Patra K, Lubar A, Okitsu SL,Flannery EL, Kato N, Tanaseichuk O, Comer E, Zhou B, Kuhen K, Zhou Y, Leroy D,Discovery of Small Molecules that Interrupt Malaria Transmission. Cell Host Microbe. 2016 Jan 13;19(1):114-26. doi: 10.1016/j.chom.2015.12.001. Epub 2015 Dec 31. PMID: 26749441
Antimalarials Active against Asexual Blood Stages Tested against the Five Gametocyte Stages
Compound Chemical Class EC50 (μM) ± STD Oocyst Reduction
Stage I Stage II Stage III Stage IV Stage V
Artemisinin Endoperoxide 0.024 ± 0.001 0.020 ± 0.010 0.012 ± 0.002 0.037 ± 0.003 >12.500 ± 0.000
Artemisone Endoperoxide 0.003 ± 0.000 0.002 ± 0.000 0.003 ± 0.000 0.004 ± 0.001 >12.500 ± 0.000
Artemether Endoperoxide 0.016 ± 0.006 0.005 ± 0.001 0.006 ± 0.002 0.019 ± 0.004 >12.500 ± 0.000 10 μM: 75%–99%3
Artenimol (Dihydroartemisinin) Endoperoxide 0.006 ± 0.001 0.003 ± 0.001 0.007 ± 0.000 0.021 ± 0.008 >12.500 ± 0.000 1 μM: ∼90%1
Artesunate Endoperoxide 0.008 ± 0.002 0.004 ± 0.000 0.013 ± 0.003 0.049 ± 0.013 >10.601 ± 2.686 1 μM: ∼55%1
OZ439 mesylate Endoperoxide 0.011 ± 0.001 0.005 ± 0.000 0.003 ± 0.000 0.002 ± 0.000 >12.500 ± 0.000 1 μM: 100%1
OZ277(RBX-11160) Endoperoxide 0.008 ± 0.001 0.004 ± 0.000 0.002 ± 0.000 0.008 ± 0.003 >12.500 ± 0.000 10 μM: 75%–99%3
Amodiaquine 4-aminoquinoline 0.012 ± 0.001 0.006 ± 0.001 0.096 ± 0.013 2.456 ± 0.757 1.783 ± 0.119 10 μM: 50%–74%3
AQ-13 4-aminoquinoline 0.043 ± 0.002 0.033 ± 0.000 0.484 ± 0.159 6.471 ± 0.888 6.051 ± 1.091 10 μM: 25%–49%3
Chloroquine 4-aminoquinoline 0.096 ± 0.007 0.098 ± 0.005 >6.250 ± 0.000 >6.250 ± 0.000 >6.25 ± 0.000 10 μM: 25%–49%3
Hydroxychloroquine 4-aminoquinoline 0.107 ± 0.011 0.131 ± 0.005 >4.489 ± 2.490 >6.250 ± 0.000 >6.25 ± 0.000 10 μM: 25%–49%3
Naphthoquine 4-aminoquinoline 0.025 ± 0.003 0.014 ± 0.000 0.296 ± 0.078 >4.167 ± 0.000
Activity of 18 MMV Control Compounds against Sexual and Asexual Stages
Compound Viability INDEX EC50 (μM)
Stage I Stage II Stage III Stage IV Stage V Stage Asex Stage I Stage III Stage V
MMV000442 0.12 0.192 0.385 0.633 0.442 0.362a 0.553 ± 0.041
>10.000 ±0.000
>10.000 ±0.000
MMV665971 0.056 0.097 0.137 0.171 0.416 0.489a 0.746 ± 0.116
>10.000 ±0.000
>10.000 ±0.000
MMV011438 0.005 0.005 0.015 0 0 0.327a, 0.332b 1.120 ± 0.116
2.428 ±0.620
4.225 ±0.609
MMV000248 0.006 0.057 0.061 0.085 0.121 0.719a 1.058 ± 0.026
3.074 ±0.533
3.700 ±0.173
MMV666125 0.006 0.002 0.071 0.196 0.234 0.381a, 2.844b 0.094 ± 0.068
1.342 ±0.259
6.154 ±0.569
MMV019918 0.017 0.014 0.01 0.015 0.033 0.800a 1.264 ± 0.145
0.576 ±0.069
1.463 ±0.296
MMV019266 0.028 0.014 0.035 0.082 0.066 0.615a 0.935 ± 0.214
1.372 ±0.210
1.743 ±0.206
MMV396797 0.034 0.007 0.033 0.094 0.077 0.477a 5.435 ± 0.470
2.094 ±0.424
3.477 ±0.175
MMV667491 0.037 0.048 0.034 0.032 0 1.230a 0.980 ± 0.069
0.667 ±0.101
0.596 ±0.085
MMV019881 0.063 0.065 0.039 0.047 0.013 0.646a 3.048 ± 3.278
8.408 ±1.577
0.721 ±0.141
MMV000448 0.066 0.016 0.083 0.201 0.231 0.235a, 0.033b 1.195 ± 0.113
5.356 ±0.612
4.652 ±0.394
MMV665882 0.116 0.092 0.122 0.168 0.13 0.466a 0.180 ± 0.036
1.477 ±0.136
0.984 ±0.022
MMV665941 0.157 0.02 0.095 0.061 0.11 0.255a 0.388 ± 0.035
2.271 ±0.751
1.044 ±0.040
MMV665980 0.24 0.184 0.087 0.108 0.247 0.211b >10.000 ± 0.000
9.350 ±3.237
6.612 ±1.100
MMV007116 0.377 0.505 0.734 0.733 0.846 0.351a, 0.716b >10.000 ± 0.000
>10.000 ±0.000
>10.000 ±0.000
MMV665827 0.592 0.9 0.81 0.769 0.791 0.119a, 0.166b >10.000 ± 0.000
>10.000 ±0.000
>10.000 ±0.000
MMV666021 0.61 0.871 0.74 0.897 1.055 0.094a, 1.998b >10.000 ± 0.000
>10.000 ±0.000
>10.000 ±0.000
MMV020492 0.768 0.756 0.97 0.912 0.989 0.026a >10.000 ± 0.000
>10.000 ±0.000
>10.000 ±0.000
The viability index shows the ratio for each gametocyte stage (I–V) compared to DMSO-treated control wells screened at 12.5 μM (384-well TSSA). EC50 values for stage I, III, and V, gametocytes are displayed as mean ± SD (1,536-well SaLSSA, in duplicate). Asexual stage data for 3D7 parasites as provided by MMV and the ChEMBL-NTD repository (https://www.ebi.ac.uk/chemblntd).
a72 hr DAPI assay (Duffy and Avery, 2012).
b72 hr SYBR green assay
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