Table 3.
In vitro antiparasitic activity of controls and Ru-KTZ complexes against promastigotes of L. major and epimastigotes of T. cruzi, and cytotoxic activity on mammalian cells (p-value <0.0001). Hs27: human fibroblast; U205: human osteoblasts; RAW 264.7: mice macrophages;IPΦ: intraperitoneal macrophages
| Compound |
L. major (μM)1 [Rel. Act.]2 / (S.I.)3 |
T. cruzi (μM)1 [Rel. Act.]2 / (S.I.)3 |
Mammalian Cells μM)4 | |||
|---|---|---|---|---|---|---|
| Hs27 | U2O5 | RAW 264.7 |
IPΦ | |||
| C1 | 15.36 ± 3.68 [0.12] (> 0.5) |
> 30 | >7.5 | >7.5 | >7.5 | |
| C2 | 13.23 ± 4.48 [0.14] (> 0.6) |
> 30 | >7.5 | >7.5 | >7.5 | |
| C3 | 12.52 ± 3.34 [0.15] (> 0.6) |
> 30 | >7.5 | >7.5 | >7.5 | |
| KTZ | 1.9 ± 0.5 [1.0](> 63) |
1.5 ± 2.9 [10] (> 82) |
>120 | 120 | >7.5 | >3.5 |
| 1 | 9.30 ± 3.66 [0.2] |
24.8 ± 2.9 [0.9] |
ND | ND | ND | |
| 2 | 2.34 ± 1.25 [0.8] |
28.36 [0.9] |
ND | ND | ND | |
| 3 | 0.8 ± 1.32 [>2.4] (> 150) |
1.39 ± 2.32 [1.04] (> 86) |
>120 | 120 | >7.5 | >3.5 |
| 4 | 1.16 ± 0.52 [1.6](> 103) |
2.28 ± 0.26 [0.64] (> 53) |
>120 | >120 | >7.5 | >3.5 |
| 5 | 1.53 ± 0.84 [1.2] (>78) |
8.00 ± 2.96 [0.18](> 15) |
>120 | 120 | >15 | >3.5 |
| 6 | 9.53 ± 6.3 [0.2] |
> 30 | ND | ND | ND | |
1
LD50: Median lethal dose calculated with 95% confidence interval; ± values are the estimated LD50 interval.
2
[Rel. Act.]: Relative Activity (LD50 of KTZ)/(LD50 of Ru-KTZ complex)
3
S.I.: Selectivity index (IC50 in Hs27 human cells)/(LD50 in parasites)
4
IC50: Median inhibitory concentration