Table 2.
Cytotoxic activities (IC50) of 1β-hydroxy alantolactone (1) and ivangustin (2) and their C1-OH modified derivatives.
| No. | IC50a (μM) | |||||
|---|---|---|---|---|---|---|
| HeLa | PC-3 | HEp-2 | HepG2 | CHO | HUVEC | |
| 1 | 3.2 ± 0.8 | 4.5 ± 0.7 | 3.3 ± 0.2b | 5.2 ± 0.1 | 6.4 ± 0.1b | 9.2 ± 0.1 |
| 1a | 8.2 ± 1.0 | 8.1 ± 0.3 | 10.3 ± 1.8 | 6.3 ± 1.3 | 10.3 ± 1.8 | 12.3 ± 1.6 |
| 1b | 25.5 ± 3.2 | >40 | >40 | >40 | NDd | ND |
| 1c | >40 | >40 | >40 | >40 | ND | ND |
| 1d | >40 | >40 | >40 | 23.5 ± 3.6 | ND | ND |
| 1e | >40 | >40 | >40 | 34.1 ± 4.8 | ND | ND |
| 1f | >40 | 18.7 ± 5.2 | >40 | 12.5 ± 2.2 | ND | ND |
| 1g | 10.0 ± 2.1 | 11.8 ± 2.8 | >40 | 15.2 ± 3.8 | ND | ND |
| 1h | >40 | >40 | >40 | >40 | ND | 39.5 ± 2.5 |
| 1i | 2.7 ± 0.1 | 2.5 ± 0.8 | 3.5 ± 0.9 | 5.1 ± 0.2 | 2.5 ± 0.2 | 8.8 ± 0.7 |
| 2 | 7.7 ± 1.3 | 10.8 ± 2.9 | 4.8 ± 0.4b | 8.9 ± 2.2 | 8.5 ± 0.1b | 16.6 ± 1.8 |
| 2a | 32.3 ± 2.0 | 28.9 ± 4.5 | >40 | >40 | ND | ND |
| 2b | 27.9 ± 2.5 | >40 | >40 | >40 | ND | ND |
| 2c | >40 | >40 | >40 | >40 | ND | ND |
| 2d | 8.6 ± 1.4 | 7.0 ± 2.1 | 14.1 ± 2.9 | 7.7 ± 1.5 | 12.1 ± 5.2 | 10.5 ± 0.5 |
| VP-16 | 3.0 ± 0.3c | 0.6 ± 0.1 | 4.8 ± 0.5c | 7.6 ± 0.8 | 2.6 ± 0.2c | 1.9 ± 0.2 |
| P | 7.6 ± 0.6 | 3.4 ± 0.6 | 6.8 ± 0.3 | — | 5.3 ± 0.7 | — |
aThe IC50 values represent the concentration that causes 50% inhibition of cell viability. Cells were treated with compounds for 72 h. All data (mean ± SD) are the average of three or four independent experiments in triplicate. Cancer cell lines: HeLa (human cervix cancer), PC-3 (human prostate cancer), HEp-2 (human larynx epidermal cancer), HepG2 (human liver cancer); Normal cell lines: CHO (Chinese hamster ovary), HUVEC (human umbilical vein endothelial cell). VP-16 represents etoposide, and P represents parthenolide. bThese values derive from Xiang et al.22. cDerive from Dong et al.19. dND: not detected.