Mangostin是有多种生物活性的膳食呫吨酮。它是一种IDH1突变体的抑制剂，Ki值为 2.85 μM。

Mangostin is a natural xanthonoid, a type of organic compound isolated from various parts of the mangosteen tree.

Alpha-mangostin exhibits a selective inhibitory effect on IDH1-R132H, but not on IDH1. Alpha-mangostin competitively inhibits the binding of alpha-mangostin (α-KG) to IDH1-R132H. The structure–relationship study reveals that alpha-mangostin exhibits the strongest core inhibitor structure. Alpha-mangostin selectively promotes demethylation of 5-methylcytosine (5mC) and histone H3 trimethylated lysine residues in IDH1 (+/R132H) MCF10A cells[1]. Cell proliferation significantly decreases in a dose-dependent manner in the cells treated with alpha-mangostin. Alpha-mangostin also increases the levels of Bax (pro-apoptotic), cleaved caspase-3, cleaved caspase-9 and cleaved-poly(ADP-ribose) polymerase (PARP)[2]. Alpha-mangostin significantly inhibits light-induced degeneration of photoreceptors and 200 μM Water2-induced apoptosis of RPE cells. 200 μM Water2-induced generation of reactive oxygen species (ROS) and light-induced generation of malondialdehyde (MDA) are suppressed by alpha-mangostin[3].

Alpha-mangostin reduces risk of liver fibrosis through the decrease in p53 expression as compared to the TAA_DMSO treatment. The serum levels of the liver enzymes AST and ALT after treatment with α-mangostin decrease as compared to DMSO alone[4].

IDH1+/+ and IDH1

Cas No.

6147-11-1

分子式

C24H26O6

分子量

410.466

别名

α-Mangostin;α-倒捻子素;Mangostin

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years