Table 1.
In vitro antiparasitic and cytotoxic activities of sponge-isolated compounds 1–9.
Compound | % of inhibition of the growth a | ||||
---|---|---|---|---|---|
U-937 cells (20 μM) | L. panamensis | P. falciparum Total forms (5 μM) | T. cruzi Intracellular amastigotes (10 μM) | ||
Axenic amastigotes (20 μM) | Intracellular amastigotes (10 μM) | ||||
1 | 94.8 ± 3.6 | 0 | NE | 35.3 ± 3.5 | 29.1 ± 0.4 |
2 | 8.2 ± 1.7 | 0.3 ± 0.06 | 2.1 ± 0.4 | 7.9 ± 1.2 | 0 |
3 | 0 | 0 | NE | 0 | 0 |
4 | 5.3 ± 1.1 | 0 | NE | 0 | 0 |
5 | 45.3 ± 13.5 | 0 | NE | 7.1 ± 1.2 | 1.6 ± 0.3 |
6 | 0 | 0 | NE | 0 | 0.2 ± 0.03 |
7 | 0 | 1.6 ± 0.4 | 0 | 23.2 ± 1.0 | 0 |
8 | 0 | 0.0 | 12.6 ± 0.9 | 8.0 ± 0.5 | 0 |
9 | 58.2 ± 12.0 | 7.7 ± 1.6 | NE | 10.8 ± 1.5 | 6.3 ± 1.3 |
Amphotericin B b | 53.2 | 60.4 ± 5.7 | 44.9 ± 7.1 | NA | NA |
Chloroquine c | NA | NA | NA | 66.8 ± 1.3 | NA |
Benznidazole d | NA | NA | NA | NA | 44.5 ± 2.7 |
Percentage of inhibition corresponds to the inhibition of the U-937 cells or parasites growth determined by colorimetric MTT method (for U-937 cells and axenic amastigotes of L. panamensis), flow cytometry (for intracellular amastigotes of L. panamensis), fluorometry (for P. falciparum total forms) and colorimetric β-galactosidase method (for T. cruzi intracellular amastigotes). Data are expressed as the average from at least two independent experiments, each done in triplicate;
Lethal Concentration 50 (LC50) for U-937 cells (previously determined in our lab) = 33.2 μM; Effective Concentration 50 (EC50) for axenic and intracellular amastigotes of L. panamensis (previously determined in our lab) = 0.05 μM and 0.04 μM, respectively;
EC50 for total forms of P. falciparum (previously determined in our lab) = 42.6 μM;
EC50 for intracellular amastigotes of T. cruzi (previously determined in our lab) = 9.3 μM. NE: Not evaluated due to the high toxicity level; NA: Not applicable because these drugs are not used for these parasites.