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(20S)-Protopanaxatriol

CAS No. : 34080-08-5

MCE 站：(20S)-Protopanaxatriol

产品活性：(20S)-Protopanaxatriol 是人参皂苷的代谢物，通过 glucocorticoid receptor 和 oestrogen receptor 起作用，同时为 LXRα 的抑制剂。(20S)-Protopanaxatriol 具有广泛的抗癌活性。

研究领域：GPCR/G Protein  |  Others  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Glucocorticoid Receptor  |  Estrogen Receptor/ERR  |  LXR  |  Apoptosis

In Vitro: (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER) in human umbilical vein endothelial cells (HUVECs). (20S)-Protopanaxatriol (g-PPT) increases [Ca²⁺]_i with an EC₅₀ of 482 nM in HUVECs. (20S)-Protopanaxatriol (1 ?M) elevates NO production via ERβ. (20S)-Protopanaxatriol (PPT) inhibits the autonomous transactivation of Gal4-LXRα LBD, the T0901317-dependent transcription of SREBP-1c and its promoter. (20S)-Protopanaxatriol (10 μg/mL) blocks the recruitment of RNA polymerase II to the LXRE region of SREBP-1c. (20S)-Protopanaxatriol also inhibits T0901317-dependent transcription of LXRα target genes related to lipogenesis, and reduces T0901317-induced cellular triglyceride (TG) accumulation in primary hepatocytes, but does not alter transcription of ABCA1, also an LXRα target gene.
Both In HCC827GR and H1975 cell lines, g-PPT (100?nM, 1?μM, 10?μM, 20?μM; 48 hours) results in SCD1 expression decreased.

In Vivo: (20S)-Protopanaxatriol (10?mg/kg; i.p.; daily for four weeks) synergizes with Gefitinib to inhibit xenograft growth.
20(S)-PPD (50-100 mg/kg; p.o.; 25 days; female BALB/c nude mice bearing breast cancer MCF-7 cell) inhibits the growth of MCF-7 breast cancer cells in a nude mice xenograft assay.

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