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(20S)-Protopanaxatriol

CAS No. : 34080-08-5

MCE 国际站：(20S)-Protopanaxatriol

产品活性：(20S)-Protopanaxatriol 是人参皂苷的代谢物，通过结合糖皮质激素受体 (glucocorticoid receptor) 和雌激素受体 (Estrogen Receptor/ERR) 起作用。(20S)-Protopanaxatriol 同时也是 LXRα 的抑制剂。(20S)-Protopanaxatriol 具有广泛的抗癌活性。

研究领域：Immunology/Inflammation  |  Vitamin D Related/Nuclear Receptor  |  Metabolic Enzyme/Protease  |  Apoptosis

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

结构分类：萜类  |  三萜  |  结构分类

来源：植物  |  五加科  |  人参

In Vitro: (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER) in human umbilical vein endothelial cells (HUVECs). (20S)-Protopanaxatriol (PPT) increases [Ca²⁺]_i with an EC₅₀ of 482 nM in HUVECs. ((20S)-Protopanaxatriol (1 µM) elevates NO production via ERβ. (20S)-Protopanaxatriol 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.
(20S)-Protopanaxatriol (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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