Uses
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo[1][2].
in vivo
8α-Tigloyloxyhirsutinolide 13-O-acetate (5mg/kg, Oral gavage, 5 times per week for 75 days) suppresses tumor growth in mice[1].
| Animal Model: | Five-week-old female athymic nude mice (injected subcutaneously in the right flank area with MDA-MB-468 cells in 100μL PBS) |
| Dosage: | 5mg/kg |
| Administration: | Oral gavage, every day, 5 times per week for 75 days |
| Result: | Inhibited MDA-MB-468 xenografts growth in mice, with reduced pY705-STAT3, G6PD, TrxR1, and GSH levels. |
IC 50
STAT3; Bcl-2; Bcl-xL; Mcl-1
References
[1] Zhu Y, et al. Natural product preferentially targets redox and metabolic adaptations and aberrantly active STAT3 to inhibit breast tumor growth in vivo. Cell Death Dis. 2022 Dec 6;13(12):1022. DOI:
10.1038/s41419-022-05477-2[2] A Bardón, et al. Glaucolides and related sesquiterpene lactones fromVernonia nudiflora and Chrysolaena propinqua. Phytochemistry, 1992, 31(2):609-613.
