Skip to main content
. 2011 Jul 19;5(7):e1253. doi: 10.1371/journal.pntd.0001253

Table 1. Host cell toxicity and efficacy of compounds against L. donovani intracellular amastigotes, promastigotes and axenic amastigotes.

Compounds GI50 THP-1 (µM) GI50 Intracellular amastigote (µM) GI50 Promastigote (µM) GI50 Axenic amastigote (µM) Selectivitya Specificityb
Naloxonazine 33.8 3.49 >50 >50 9.68 14.32
Metergoline 37.14 0.78 15.08 >50 47.22 19.17
R(-)-Apomorphine >16.5 2.7 38.15 5.20 6.1 14.12
Clotrimazole >16.5 1.08 12.92 4.56 15.32 11.92
Cetylpyridinium chloride 9.16 0.41 3.30 0.92 22.34 8.05
Aminacrine 12.97 1.9 8.96 >16.5 6.82 4.71
4,4′-Diethylaminoethoxyhexestrol 6.11 1.4 5 10.93 4.36 3.57
Hexachlorophene 16.5 4.54 15.88 14.76 3.62 3.49
Loperamide Hydrochloride >16.5 5.4 17.3 >50 3.02 3.15
Tamsulosin 27.97 6.3 20 >50 4.43 3.17
Salinomycin 16.09 0.92 2.71 0.06 17.30 2.92
Cycloheximide 21 1.15 2.95 0.39 18.13 2.55
Prazocin Hydrochloride 23.32 6.73 16.74 >50 3.46 2.48
Carvedilol 37.5 6.16 12.41 >16.5 6.07 2.01
Brilliant green 1.64 6 0.10 0.03 15.88 0.02
Antimycin A >50 2.15 0.1 0.01 500 0.05
BAY 11–7085 >50 >16,5 1.54 0.42 32.46 0.06
Haloprogin 20 6 1.05 0.56 19.04 0.17
Pentamidine Isethionate >50 9.55 1.69 1.64 29.49 0.17
Zinc Dibutyldithiocarbamate >50 >50 8.48 >50 5.89 0.17
Amlodipine >16.5 9.78 3.11 27 5.34 0.31
Nisoldipine >16,5 32.17 9.85 13.86 1.67 0.30
Parthenolide >16.5 >50 15.54 4.35 1.06 0.31
Pyrithione zinc 1.043 ND 0.07 0.01 14.9 ND
Thimerosal 12.81 ND 0.49 1.50 26.18 ND
Gramicidin 8.38 ND 0.68 5.76 12.19 ND
Digitonin 13.46 ND 4.376 13.81 3.075 ND
Emetine 1.28 0.082 0.03 1.62 15.58 0.42
Amphotericin B >50 1.12 1.61 5.42 44.52 1.43
Chlorhexidine >16,5 1.79 2.81 4.78 9.27 1.56
Oxiconazole >16,5 6.6 2.65 0.53 2.51 0.40
Bazedoxifene >16,5 4.8 6.52 >16.5 3.45 1.35
chlorquinaldol 39.3 5.5 6.3 1.72 7.14 1.14
Doxazocin >16,5 5 8.45 >16.5 3.32 1.69
Aclacynomycine a1 29.1 5.81 9.15 >16.5 5 1.57
Mebeverine >50 8.5 6.91 2.36 5.88 0.81
Miconazole >16,5 15.44 7.48 4.73 1.07 0.48
Terfenadine 39.03 14.4 11.92 0.61 2.71 0.82
Tamoxifen Citrate >16.5 20.79 10.22 >50 1.61 0.49
Auranofin 20.89 21.76 11.11 >50 1.88 0.51
Benzetonium chloride 40.18 10 11.34 10.7 3.54 1.13
Ciclopirox 42 22 15.25 >50 1.90 0.69
Sporidesmin A 0.02 ND 1.18 1.66 0.02 ND
Harringtonin 0.10 4.89 16.61 10.6 0.02 3.39
3,3′,4′,5-tetrachlorosalicylanilide 0.32 ND 1.45 1.38 0.22 ND
Thiram 1.58 10.4 4.62 5.42 0.34 0.44
Idarubicin 1.89 ND 4.65 1.78 0.40 ND
Cerivastatin 7.15 >50 10.8 0.02 0.66 0.22

aSelectivity is the ratio between parasite GI50 and THP-1 GI50.

bSpecificity is the ratio between promastigote GI50 and intracellular amastigote GI50. Specificity value >2 was the cut-off chosen to define a compound as more active against the intracellular amastigote stage; while a specificity value <0.4 indicated a compound more active against promastigotes; compounds with specificity values between 0.4 and 2 were considered active against both stages.