TABLE 1.
In vitro activity of Clathrotropis brunnea Amshoff on L. braziliensis and T. cruzi amastigotes and its cytotoxicity toward U-937 macrophages.
| Sample | Code | U-937 cells LC50 (μg/ml) a | L. braziliensis | T. cruzi | |||
|---|---|---|---|---|---|---|---|
| EC50 (μg/ml) b | SI c | EC50 (μg/ml) b | SI c | ||||
| Crude extract | SQB-2 | 10.3 ± 0.7 | 15.4 ± 2.7 d | 0.7 | 25.0 ± 5.2 | 0.4 | |
| Fractions | SQB-2-S0 | 232.6 ± 70.3 | 88.4 ± 25.0 | 2.6 | 36.8 ± 0.7 | 6.3 | |
| SQB-2-S1 | 128.2 ± 16.4 | >50 | <2.6 | 22.8 ± 1.0 | 5.6 | ||
| SQB-2-S2 | 37.2 ± 13.8 | 13.3 ± 1.6 | 2.8 | 15.7 ± 0.9 | 2.4 | ||
| SQB-2-S3 | 284.2 ± 137.3 | 145.9 ± 48.2 | 2.0 | 17.0 ± 1.9 | 16.7 | ||
| SQB-2-S4 | 62.2 ± 1.5 | >50 | <0.04 | 35.6 ± 4.3 | 1.8 | ||
| SQB-2-S5 | 153.4 ± 44.7 | >50 | <3.1 | 36.2 ± 1.3 | 4.2 | ||
| SQB-2-S6 | 71.2 ± 5.0 | >50 | <1.4 | 27.6 ± 2.2 | 2.6 | ||
| 3,5-diOMe stilbene | SQB-2-S2-1-3 | 14.8 ± 0.7 (61.6 μM) | 4.2 ± 0.21 (17.0 μM) | 3.6 | 27.7 ± 3.8 (115.4 μM) | 0.6 | |
| Pinostrobin | SQB-2-S2-1-4 | 35.5 ± 9.0 (131.4 μM) | 13.6 ± 0.28 (50.4 μM) | 2.6 | 18.2 ± 0.2 (67.4) | 2.0 | |
| Amb e | 36.6 ± 8.0 | 0.3 ± 0.1 | 122.0 | NA f | NA | ||
| Bnz g | >200.0 | NA | NA | 15.8 ± 2.6 | >12.7 | ||
| Dox h | 1.0 ± 0.2 | NA | NA | NA | NA | ||
Data represent the mean value ± standard deviation. Bold values are active compounds.
a
LC50: Lethal concentration on U-937 cells.
b
EC50: Effective concentration on intracellular amastigotes of L. braziliensis or T. cruzi.
c
SI: Selectivity index (LC50/EC50).
d
High activity: EC50 < 25 μg/ml; moderate activity: EC50 > 25 < 50 μg/ml; low activity: EC50 > 50 μg/ml.
e
Amphotericin B: Leishmanicidal drug control.
f
NA: Not applicable.
g
Benznidazole: Trypanocidal drug control.
h
Doxorubicin: Toxicity drug control.