Table 2.
Lycorine, lycorine analogues, and their in vitro growth inhibitory activity in cancer versus normal cell lines.
| Lycorine Analogue | # | Therapeutic ratio | IC50In Vitro Growth Inhibitory Values (μM)a | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cancer Cell Lines | Normal Cell Lines | ||||||||||||
| A549 | OE21 | Hs683 | U373 | SKMEL | B16F10 | Mean ± SEM | Wi38 | WS1 | NHDF | Mean ± SEM | |||
| Lycorine | 1 | > 15 | 4.3 ± 0.3 | 5.1 ± 0.4 | 6.7 ± 0.3 | 7.6 ± 0.2 | 8.5 ± 0.3 | 6.3 ± 0.4 | 6.4 ± 0.6 | > 100 | > 100 | > 100 | > 100 |
| 2-O-Acetyllycorine | 5 | > 2 | 47.6 ± 2.3 | 77.4 ± 3.1 | 43.0 ± 2.0 | 63.1 ± 4.1 | 87.8 ± 3.9 | 37.1 ± 2.8 | 59.3 ± 8.2 | 88.5 | > 100 | > 100 | > 96.2 ± 2.7 |
| Lycorine chlorohydrin | 6 | > 11 | 3.8 ± 0.2 | 9.6 ± 0.7 | 3.1 ± 0.3 | 2.3 ± 0.1 | 14.8 ± 1.1 | 6.9 ± 0.5 | 6.8 ± 2.0 | 46.0 | > 100 | 72.1 | > 72.7 ± 11.0 |
| 1,2-epoxy-lycorine | 14 | 5 | 3.4 ± 0.1 | 8.5 ± 0.5 | 3.3 ± 0.2 | 2.4 ± 0.1 | 9.5 ± 0.4 | 4.6 ± 0.2 | 5.3 ± 1.2 | 28.6 | 36.8 | 9.3 | 24.9 ± 8.2 |
| Lycorine hydrochloride | 15 | > 15 | 4.3 ± 0.2 | 4.6 ± 0.1 | 6.5 ± 0.2 | 8.6 ± 0.3 | 8.3 ± 0.3 | 5.5 ± 0.2 | 6.3 ± 0.8 | > 100 | > 100 | > 100 | > 100 |
| Pseudolycorine | 18 | 7 | 7.5 ± 0.4 | 7.7 ± 0.3 | 7.9 ± 0.2 | 7.8 ± 0.3 | 15.5 ± 1.1 | 7.5 ± 0.3 | 9.0 ± 1.3 | 44.0 | 79.1 | 66.9 | 63.3 ± 7.3 |
| Anhydrolycorine | 20 | 2 | 4.5 ± 0.1 | 8.8 ± 0.2 | 7.1 ± 0.3 | 5.1 ± 0.1 | 20.9 ± 1.2 | 23.3 ± 1.2 | 11.6 ± 3.4 | 30.1 | 23.7 | 26.6 | 26.8 ± 1.3 |
| Amarbellisine | 22 | > 13 | 7.2 ± 0.3 | 6.7 ± 0.2 | 8.3 ± 0.3 | 7.3 ± 0.2 | 8.3 ± 0.2 | 6.7 ± 0.3 | 7.4 ± 0.3 | > 100 | 97.6 | > 100 | > 99.2 ± 0.6 |
a
Cancer cell lines were cultured as specified in Table 1. WI-38 fibroblasts (ATCC code CCL-75; see Fig. 2) were cultured in MEM medium supplemented with 10% heat inactivated fetal bovine serum and 100μM non-essential amino acids; WS-1 (ECACC code 88021104) fibroblasts were cultured in MEM medium supplemented with 10% heat inactivated fetal bovine serum; NADH (PromoCell code c-12300) were cultured in MEM medium supplemented with 10% heat inactivated fetal bovine serum and 100 μM non-essential amino acids.