γ-Tocotrienol

γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment^[1][2][3]. In Vitro:γ-Tocotrienol (25 μM; 24 h) effectively inhibits the expression levels of mdr1 mRNA and P-gp protein, (25 μM and 50 μM; 24 h) suppresses mdr1 promoter activity and the efflux activity of P-gp as well^[2].
γ-Tocotrienol (25 μM and 50 μM; 24 h) reduces the activation of NF-κB signaling pathway and the transcriptional activity of NF-κB^[2].
γ-tocotrienol (50 μM; 48 h) effectively inhibits the process of nuclear translocation of p65 which was induced by TNFα^[2].
In Vivo:γ-Tocotrienol’s liposomal formulation, GT3-Nano (20 mol% γ-Tocotrienol), (10 mg/kg, 6 mol%; i.v.; single dose, observed for 100 d) is highly effective in mitigating the marrow-suppressive effects of sublethal and lethal TBI in mice^[3].
GT3-Nano (50 mg/kg; i.v.; ) can facilitate rapid recovery of hematopoietic components in mice treated with the endoradiotherapeutic agent ¹⁵³Sm-EDTMP^[3].