Information
Demethylzeylasteral (T-96) Demethylzeylasteral (T-96), the active component isolated from Tripterygium wilfordii Hook F., inhibits UDP-glucuronosyltransferase (UGT) isoforms UGT1A6 and UGT2B7 with immunosuppressive effects.
Targets
UGT1A6 (Cell-free assay); UGT2B7 (Cell-free assay) 0.6 μM(Ki); 17.3 μM(Ki)
In vitro
Demethylzeylasteral shows strong inhibition towards UGT1A6 and UGT2B7, with negligible influence towards UGT1A9. Demethylzeylasteral has an anti-tumor property in melanoma cells. Demethylzeylasteral not only inhibits cell proliferation through cell cycle arrest at S phase, but also induces cell apoptosis in melanoma cells. CDK2 and Cycin E1 decrease in a dose-dependent manner after Demethylzeylasteral treatment. Demethylzeylasteral inhibits MCL1, whose overexpression recovers the proliferation ability inhibited by demethylzeylasteral. Demethylzeylasteral inhibits clonogenicity and tumorigenesis in melanoma cells through downregulating the expression of MCL1. Demethylzeylasteral is found to inhibit Ca2+ currents in mouse spermatogonia and has an antifertility ability.
In vivo
T-96 demonstrates a significant proteinuria reduction both in a time and concentration-dependent manner. T-96 significantly inhibits the activation of NF-kB in the kidneys of MRL/lpr mice. In addition, T-96 reduces the secretion of pro-inflammatory mediators such as TNF-α, COX-2 and ICAM-1.
Cell Research(from reference)
Cell lines：melanoma cell lines, MV3 and A375
Concentrations：1, 5, 10 and 20\u2009μM
Incubation Time：48 h
K2415629