Arborinine

Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity [1][2].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

LSD1

Arborinine (0, 5, 15, 30 µM; 48 h) 增加 H3K4me1/2、H3K9me1/2、E-cad 蛋白的表达[1]。 Arborinine (20 µM) 降低 786O 细胞中 UBE2O 蛋白水平的表达[1]。 Arborinine (20 µM) 诱导细胞周期停滞在 S 期并抑制细胞凋亡[1]。 Cell Proliferation Assay[1] Cell Line: 786O, A498, 769P, Caki1, OSRC2 cells Concentration: 0-100 µM Incubation Time: 48, 72 h Result: Showed antiproliferative activity with IC50s of 30.62, 39.09, 15.67, 31.42, 30.35 µM at 48 h, 20.92, 27.01, 14.94, 30.26, 17.37 µM at 72 h for 786O, A498, 769P, Caki1, OSRC2 cells, respectively. Western Blot Analysis[1] Cell Line: 786O cells Concentration: 0, 5, 15, 30 µM Incubation Time: 48 h Result: Increased the expression of H3K4me1/2 and H3K9me1/2 protein in a dose-dependent manner. Cell Cycle Analysis[1] Cell Line: 786O and A498 cells Concentration: 20 µM Incubation Time: Result: Induced increased population in S phase and decreased population in G1 phase, significantly inhibited both early and late apoptosis of ccRCC cells

Arborinine (40、80 mg/kg；灌胃； 21 天) 在小鼠体内显示出抗肿瘤活性[2]。 Animal Model: BALB/c nude mice (SGC-7901 cells and SGC-7901/ADR cells)[2] Dosage: 40, 80 mg/kg Administration: P.o.; for 21 days Result: Inhibited the growth of tumors while unchanged the body weights.

[1]. Feng C, et al. Arborinine from Glycosmis parva leaf extract inhibits clear-cell renal cell carcinoma by inhibiting KDM1A/UBE2O signaling. Food Nutr Res. 2022 Sep 16;66.  

[2]. Chu Y, et al. Arborinine, a potential LSD1 inhibitor, inhibits epithelial-mesenchymal transition of SGC-7901 cells and adriamycin-resistant gastric cancer SGC-7901/ADR cells. Invest New Drugs. 2021 Jun;39(3):627-635.