Table 5.
Toxicokinetic parameters of 11 Gelsemium alkaloids after intravenous administration in rats (0.1 mg/kg for each alkaloid).
| Compound | AUC(0-t) | AUC(0-∞) | MRT(0-t) | MRT(0-∞) | t 1/2z | Vz | CLz/F | C max |
|---|---|---|---|---|---|---|---|---|
| ng/mL∗h | ng/mL∗h | h | h | h | L/kg | L/h/kg | ng/mL | |
| Humantenirine | 73.1 ± 19.5 | 73.2 ± 19.5 | 1.4 ± 0.1 | 1.4 ± 0.1 | 0.9 ± 0.3 | 2.0 ± 0.8 | 1.4 ± 0.4 | 43.7 ± 6.9 |
| Humantenine | 14.7 ± 3.7 | 14.0 ± 3.7 | 1.2 ± 0.1 | 1.2 ± 0.1 | 1.5 ± 0.3 | 15.9 ± 4.9 | 7.6 ± 2.3 | 11.5 ± 3.6 |
| Akuammidine | 4.7 ± 1.31.3 | 4.7 ± 1.2 | 1.0 ± 0.4 | 1.2 ± 0.5 | 2.3 ± 1.2 | 84.0 ± 63.3 | 22.5 ± 6.5 | 7.8 ± 2.1 |
| Gelsevirine | 73.8 ± 12.9 | 122.7 ± 107.2 | 7.2 ± 1.6 | 22.0 ± 31.1 | 15.8 ± 8.1 | 14.2 ± 6.3 | 1.2 ± 0.5 | 13.2 ± 3.9 |
| Rankinidine | 2.2 ± 0.8 | 2.2 ± 0.8 | 1.0 ± 0.2 | 1.1 ± 0.2 | 0.9 ± 0.1 | 67.5 ± 22.7 | 52.7 ± 22.4 | 2.3 ± 1.2 |
| n-Methoxyanhydrovobasinediol | 3.1 ± 0.7 | 3.6 ± 0.7 | 1.8 ± 0.5 | 3.3 ± 2.0 | 2.7 ± 1.9 | 106.9 ± 72.2 | 28.3 ± 5.7 | 2.4 ± 1.4 |
| Gelsenicine | 7.5 ± 4.9 | 7.6 ± 4.9 | 0.8 ± 0.2 | 0.8 ± 0.2 | 1.4 ± 1.0 | 3.2 ± 2.2 | 1.7 ± 0.8 | 9.4 ± 4.9 |
| Gelsemine | 1.7 ± 0.5 | 2.0 ± 0.6 | 2.1 ± 0.4 | 3.7 ± 2.1 | 3.0 ± 1.7 | 216.2 ± 104.3 | 53.0 ± 16.3 | 1.1 ± 0.5 |
| Koumine | 7.9 ± 2.3 | 8.5 ± 2.7 | 0.8 ± 0.2 | 1.2 ± 0.5 | 1.1 ± 0.6 | 21.5 ± 12.6 | 13.6 ± 7.3 | 10.3 ± 3.6 |
| Koumidine | 6.7 ± 2.9 | 6.9 ± 2.9 | 1.8 ± 0.3 | 2.1 ± 0.5 | 2.2 ± 1.0 | 54.4 ± 34.7 | 17.1 ± 7.5 | 5.4 ± 2.1 |
| Sempervirine | 25.7 ± 6.8 | 29.4 ± 9.7 | 6.5 ± 2.1 | 9.7 ± 4.9 | 7.7 ± 3.8 | 37.2 ± 12.1 | 3.7 ± 1.2 | 9.3 ± 4.4 |