Table 3.
Macrophage selectivity.
|
Compd |
Cytotoxicity, THP‐1, IC50±SD (μM) |
Selectivity index |
||
|---|---|---|---|---|
|
SI3 [f] |
SI4 [g] |
|||
|
NFT |
>100 |
3 |
10 |
|
|
1 |
99.94±0.09 |
– |
256 |
|
|
2 |
>100 |
25 |
– |
|
|
3 |
– |
– |
– |
|
|
4 |
>100 |
– |
>263 |
|
|
5 |
– |
– |
– |
|
|
6 |
>100 |
– |
27 |
|
|
7 |
>100 |
15 |
16 |
|
|
8 |
>100 |
– |
22 |
|
|
9 |
>100 |
– |
– |
|
|
10 |
>100 |
– |
– |
|
|
11 |
– |
– |
– |
|
|
12 |
– |
– |
– |
|
|
13 |
>100 |
– |
11 |
|
|
14 |
>100 |
– |
86 |
|
|
15 |
>100 |
19 |
– |
|
|
16 |
55.73±1.17 |
9 |
6 |
|
|
17 |
– |
– |
– |
|
|
18 |
– |
– |
– |
|
|
19 |
– |
– |
– |
|
|
20 |
– |
– |
– |
|
|
FZD |
>100 |
36 |
24 |
|
|
NFZ |
>100 |
17 |
20 |
|
|
NFX |
>100 |
7 |
14 |
|
|
AMB |
14.86±0.09 |
495 |
297 |
|
[a] Specificity index (SpI) <0.4 indicates more antipromastigote activity, 0.4<SpI<2.0 indicates activity against both forms, SpI>2.0 indicates more anti‐amastigote activity. [41b] [b] Specificity index of L. major IR‐173: SpI1=IC50 promastigote/IC50 amastigote. [c] Specificity index of L. donovani 9515: SpI2=IC50 promastigote/IC50 amastigote. [d] Selectivity Index of L. major IR‐173: SI1=IC50 HEK‐293/IC50 amastigote. [e] Selectivity Index of L. donovani 9515: SI2=IC50 HEK‐293/IC50 amastigote. [f] Selectivity Index of L. major IR‐173: SI3=IC50 THP‐1/IC50 amastigote. [g] Selectivity Index of L. donovani 9515: SI4=IC50 THP‐1/IC50 amastigote. HEK‐293: human embryonal kidney cells; THP‐1: Human acute monocytic leukemia; NFT: nitrofurantoin; FZD: furazolidone; NFX: nifuroxazide; NFZ: nitrofurazone; AMB: amphotericin B; EM: Emetine. All reported data were significant at p<0.05.