arborinine

Product Namearborinine
CAS5489-57-6
MFC16H15NO4
MW285.29
EINECS
MOL File5489-57-6.mol

Chemical Properties

Melting point	177-177.5 °C
Boiling point	508.4±50.0 °C(Predicted)
Density	1.296±0.06 g/cm3(Predicted)
solubility	DMSO: 2 mg/mL, clear (warmed)
form	powder
pka	7.29±0.20(Predicted)
color	white to beige
SMILES	O=C1C2=C(C=C(C(OC)=C2O)OC)N(C)C3=C1C=CC=C3

Usage And Synthesis

Uses

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].

Definition

ChEBI: Arborinine is a member of acridines. It is functionally related to an acridone.

in vivo

Arborinine (40, 80 mg/kg; p.o.; for 21 days) shows antitumor activity in mouse^[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.

IC 50

LSD1

References

[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. DOI:10.29219/fnr.v66.8714
[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. DOI:10.1007/s10637-020-01016-y