| Identification | Back Directory | [Name]
8α-Tigloyloxyhirsutinolide 13-O-acetate | [CAS]
83182-58-5 | [Synonyms]
8α-Tigloyloxyhirsutinolide13-O-acetate
8α-Tigloyloxyhirsutinolide 13-O-acetate
8alpha-Tigloyloxyhirsutinolide 13-O-acetate
2-Butenoic acid, 2-methyl-, (4S,6R,7S,10R,11E)-3-[(acetyloxy)methyl]-2,4,5,6,7,8,9,10-octahydro-7-hydroxy-6,10-dimethyl-2-oxo-7,10-epoxycyclodeca[b]furan-4-yl ester, (2E)- | [Molecular Formula]
C22H28O8 | [MOL File]
83182-58-5.mol | [Molecular Weight]
420.45 |
| Hazard Information | Back Directory | [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 (5?mg/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 100?μL PBS) | | Dosage: | 5?mg/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. |
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