Table 1.
In vitro antiprotozoal and cytotoxic activity (IC50 values in μg/mL; values in μM of pure compounds are reported in brackets) of the dichloromethane (DCM) extract from Anacyclus pyrethrum roots and of the isolated alkamides (3–5). Selectivity indices (SIs) represent the ratio of cytotoxic over antiprotozoal IC50 values. Data are means of two independent determinations ± deviation from mean value. The in vitro activity data of 1 (anacycline) and 2 (pellitorine) was previously reported by us [2].
| Sample | Tbr 1 | Tc 2 | Ld 3 | Pf 4 | Cytotox 5 | SI Tbr |
SI Ld |
SI Pf |
|---|---|---|---|---|---|---|---|---|
| Pos. contr. | 0.003 ± 0.001 | 0.439 ± 0.094 | 0.127 ± 0.052 | 0.080 ± 0.003 | 0.008 ± 0.001 | |||
| (0.008) | (1.688) | (0.312) | (0.250) | (0.019) | ||||
| DCM extr. 6 | >10 | 8.83 ± 0.75 | 4.22 ± 1.57 | 3.04 ± 0.07 | 13.4 ± 3.2 | >1.3 | 3.2 | 4.4 |
| 3 | 2.91 ± 0.21 | 39.9 | 4.77 ± 1.02 | 7.13 ± 0.63 | 16.7 ± 0.1 | 5.7 | 3.5 | 2.3 |
| (13.2) | (181) | (21.6) | (32.2) | (75.3) | ||||
| 4 | 4.03 | 5.02 ± 0.05 | 2.97 ± 0.54 | >5 | 7.88 | 2.0 | 2.7 | >1.6 |
| (14.9) | (18.5) | (11.0) | (>18) | (29.1) | ||||
| 5 | 4.59 ± 0.39 | 16.3 ± 0.3 | 4.04 ± 0.71 | 10.3 ± 1.4 | 28.2 ± 6.9 | 6.2 | 7.0 | 2.7 |
| (18.9) | (66.9) | (16.6) | (42.5) | (116) | ||||
| 6 | 6.37 ± 0.94 | 38.8 ± 2.1 | 5.04 ± 1.17 | 7.19 ± 0.49 | 19.4 ± 1.7 | 3.1 | 3.9 | 2.7 |
| (23.7) | (144) | (18.7) | (26.7) | (72.2) | ||||
| 7 | 2.26 ± 0.18 | 1.88 | 4.19 ± 1.64 | 3.18 ± 0.20 | 0.19 ± 0.05 | 0.1 | <0.1 | <0.1 |
| (7.17) | (5.97) | (13.3) | (10.1) | (0.69) | ||||
| 8 + 9 (1:4) | 1.66 ± 0.12 | 3.90 | 5.31 ± 0.53 | 7.64 ± 2.57 | 2.47 ± 0.36 | 1.5 | 0.5 | 0.3 |
1 T. b. rhodesiense (STIB 900 strain, bloodstream trypomastigotes, positive control: melarsoprol); 2 T. cruzi (Tulahuen C4 strain; intracellular amastigotes, pos. contr.: benznidazole); 3 L. donovani (MHOM-ET-67/L82 strain, axenic amastigotes, pos. contr.: miltefosine); 4 P. falciparum (NF54 IEF, pos.: chloroquine); 5 Cytotoxicity (L6 rat skeletal myoblast cell line, pos.contr.: podophyllotoxin); 6 Data for the crude extract were previously reported and are repeated here for comparison [2].