Table 1.
Compounds | TcSir2rp1 | TcSir2rp3 | Trypomastigote | Amastigote | hFIB | SI e |
---|---|---|---|---|---|---|
EC50 ± SEM (µM) a | EC50 ± SEM (µM) a | EC50 ± SEM (µM) b | EC50 ± SEM (µM) c | CC50 ± SEM (µM) d | ||
1 | NA | NA | 23.36 ± 0.12 | 11.75 ± 0.40 | 47.17 ± 0.10 | 4 |
2 | 31.40 ± 2.33 | NA | 12.25 ± 0.25 | 14.70 ± 3.27 | 53.70 ± 7.08 | 4 |
3 | NA | NA | NA | 46.98 ± 1.97 | >100 | >2 |
4 | NA | NA | 43.52 ± 2.32 | 15.28 ± 2.00 | 45.47 ± 0.27 | 3 |
5 | 23.35 ± 2.51 | 6.08 ± 1.16 | NA | 41.67 ± 5.53 | >100 | >2 |
6 | 16.16 ± 4.88 | 7.41 ± 0.65 | NA | 42.39 ± 5.11 | >100 | >2 |
Benznidazole | 11.40 ± 1.09 | 3.13 ± 0.87 | >100 | >32 |
a Sirtuin activity was determined 4 h after incubation. b Determined 24 h after incubation with compounds. c Infected human primary skin fibroblasts (hFIB) were exposed to compounds and activity was determined 72 h after treatment. d hFIB viability was determined 72 h after treatment. e Selectivity index (SI), calculated by the ratio of CC50 (hFIB) to EC50 (amastigote). EC50, effective concentration at 50%; CC50, cytotoxic concentration at 50%. ND, not determined due to lack of activity. Values were calculated using concentrations in triplicate, and three independent experiments were performed.