Demethylzeylasteral (T-96)

Demethylzeylasteral 是从雷公藤中分离出的一种三萜烯化合物，具有抗炎、免疫抑制和抗肿瘤活性。Demethylzeylasteral 能显著减轻动脉粥样硬化 (AS)。Demethylzeylasteral 通过阻断 TGF-β 信号通路，抑制三阴性乳腺癌的侵袭。 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

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