Table 2.
P-gp inhibitory activity of the natural compounds 3, 10, 15, 17, 40–42, and the acyl derivatives 7, 18–20, and 22 in human ABCB1-gene-transfected mouse lymphoma cells (Ramalhete et al. 2009b, 2016) (Mónico et al. 2019)
| Compounds | Conc. μM | FARa |
|---|---|---|
| Verapamil | 22 | 7.4 |
| Balsaminol C (3) | 2 | 2.9 |
| 20 | 198.9 | |
| Balsaminagenin B (15) |
2 20 |
5.98 104.2 |
| Balsaminoside A (10) |
2 20 |
1.45 89.4 |
| Karavilagenin C (17) |
0.5 1 2 20 |
1.5 15.0 42.1 46.0 |
| Cucurbalsaminone A (40) |
0.2 2 20 |
1.4 14.2 87.5 |
| Cucurbalsaminone B (41) |
0.2 2 20 |
5.9 76.9 105.5 |
| Cucurbalsaminone C (42) |
0.2 2 20 |
3.1 62.2 117.7 |
| Triacetylbalsaminol F (7) |
2 20 |
3.0 15.0 |
| Karavoate A (18) |
2 20 |
35.2 34.2 |
| Karavoate B (19) |
2 20 |
5.7 37.5 |
| Karavoate C (20) |
2 20 |
1.7 40.6 |
| Karavoate E (22) |
2 20 |
1.0 21.7 |
aFAR—Fluorescence activity ratio: accumulation ratio of rhodamine 123 between resistant (MDR) and sensitive (PAR) cells. FAR > 1 means the compound is active; FAR > 10 means strong P-gp modulation