Uses
δ-Tocotrienol prodrug-1 (compound 5b) is a prodrug of δ-tocotrienol (HY-122778). δ-Tocotrienol prodrug-1 shows radioprotective efficacy. δ-Tocotrienol prodrug-1 promotes the hematopoietic progenitor and stem cell regeneration in murine bone marrow and spleen[1].
in vivo
δ-Tocotrienol prodrug-1 (compound 5b) (100 mg/kg; s.c.; once) shows radioprotective efficacy[1].
Pharmacokinetic Parameters[1].
| Parameters | 100 mg/kg (i.v./DT3) | 100 mg/kg (s.c./DT3) |
| tmax (h) | 0.083 | 0.67 |
| Cmax (ng/ml) | 5.15 × 105 | 2.02 × 103 |
| t1/2 (h) | 10.40 | 26.76 |
| AUC(0-t) (h ng/mL) | 1.96×105 | 0.27×105 |
| AUC(0-∞) (h ng/ mL) | 2.06×105 | 0.54×105 |
| CL (mL/h/kg) | 225.32 | - |
| MRT(0-t) (h) | 1.36 | 11.89 |
| MRT(0-∞) (h) | 3.47 | 38.38 |
| V(dss) (mL/kg) | 336.58 | - |
| F % | - | 13.86 |
| Animal Model: | 21-24 g C57BL/6J male mice[1] |
| Dosage: | 100 mg/kg |
| Administration: | S.c.;once; 24 h prior to 8.5 Gy or 9.5 Gy total-body irradiation (TBI) |
| Result: | showed 90 % survival rate at 30 days in mice. |
References
[1] Zuo Z, et al. Radioprotective effectiveness of a novel delta-tocotrienol prodrug on mouse hematopoietic system against 60Co gamma-ray irradiation through inducing granulocyte-colony stimulating factor production. Eur J Med Chem. 2024 Apr 5;269:116346. DOI:
10.1016/j.ejmech.2024.116346
