(20S)-Protopanaxatriol

(20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects^[1][2][3]. IC50 & Target:Glucocorticoid receptor, Oestrogen receptor^[1];
LXRα^[2] 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^[1]. (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^[2].
Both In HCC827GR and H1975 cell lines, g-PPT (100 nM, 1 μM, 10 μM, 20 μM; 48 hours) results in SCD1 expression decreased^[3]. In Vivo:(20S)-Protopanaxatriol (10 mg/kg; i.p.; daily for four weeks) synergizes with Gefitinib to inhibit xenograft growth^[3].
(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^[4].