Table 2.
Trypanocidal activity of the NO-donors on BT forms at different concentrations and time of incubation
|
Trypanocidal activity (% TA) |
||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| T=1 h |
T=4 h |
T=24 h |
||||||||
| NO donors |
Concentrations (mM) |
|||||||||
| 0.1 | 0.5 | 1 | 0.1 | 0.5 | 1 | 0.1 | 0.5 | 1 | IC50try (μM) | |
| t-[Ru(NO)(NH3)4pz]3+ | 30±4 | 66±5 | 100 | 85±4 | 100 | 100 | 100 | 100 | 100 | 50 |
| t-[Ru(NO)(NH3)4L-hist]3+ | 36±4 | 86±4 | 88±4 | 58±4 | 79±4 | 83±5 | 98±4 | 100 | 100 | 51 |
| t-[Ru(NO)(NH3)4imN]3+ | 87±6 | 91±5 | 92±4 | 68±4 | 97±3 | 100 | 97±4 | 100 | 100 | 52 |
| SNP | 56±7 | 78±3 | 90±4 | 75±4 | 89±7 | 92±4 | 97±4 | 98±5 | 100 | 52 |
| Benznidazole | 0 | 7±6 | 12±4 | 15±5 | 21±5 | 37±7 | 89±8 | 92±5 | 100 | 53 |
| t-[Ru(NO)(NH3)4SO3]+ | 40±5 | 80±2 | 88±4 | 47±7 | 74±6 | 86±4 | 85±4 | 88±4 | 100 | 59 |
| t-[Ru(NO)(NH3)4P(OEt)3]3+ | 57±3 | 68±2 | 86±4 | 62±4 | 90±4 | 92±4 | 84±4 | 92±8 | 100 | 60 |
| t-[Ru(NO)(NH3)4ina]3+ | 55±4 | 83±4 | 87±5 | 56±4 | 64±2 | 77±5 | 79±4 | 100 | 100 | 63 |
| t-[Ru(NO)(NH3)4py]3+ | 60±2 | 79±4 | 83±3 | 49±6 | 76±4 | 80±4 | 67±4 | 91±6 | 92±5 | 75 |
| t-[Ru(NO)(NH3)4isn]3+ | 90±4 | 81±5 | 81±7 | 59±4 | 55±5 | 52±7 | 65±7 | 83±4 | 97±4 | 77 |
| t-[Ru(NO)(NH3)4nic]3+ | 36±6 | 60±4 | 67±5 | 38±2 | 63±4 | 93±4 | 44±5 | 86±4 | 100 | 158 |
| t-[Ru(NO)(NH3)44-pic]3+ | 48±4 | 77±3 | 90±5 | 35±3 | 50±4 | 78±4 | 44±5 | 76±4 | 95±3 | 177 |
| [Ru(NO)(Hedta)] | 12±7 | 15±6 | 82±4 | 20±3 | 50±4 | 56±3 | 33±3 | 72±2 | 89±2 | 275 |
| t-[Ru(NO)(NH3)4imC]3+ | 5±4 | 8±3 | 14±8 | 11±7 | 12±7 | 18±4 | 15±5 | 21±5 | 26±4 | ≈3400 |
Abbreviations: BT, bloodstream trypomastigote; NO, nitric oxide.
Results are mean±s.e.m., n=4–8, P<0.05. Trypanocidal activity expressed as the percentage of the number of lysed trypomastigotes compared to the negative control. IC50try corresponds to the concentration with 50% trypanocidal activity after 24 h of incubation.