CAS NO: | 6147-11-1 |
生物活性 | alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutantIDH1(IDH1-R132H) with aKiof 2.85 μM. | ||||||||||||||||
IC50& Target | IC50: 2.85 μM (IDH1-R132H)[1] | ||||||||||||||||
体外研究 (In Vitro) | alpha-Mangostin (α-Mangostin) exhibits a selective inhibitory effect on IDH1-R132H, but not on IDH1. alpha-Mangostin (α-Mangostin) competitively inhibits the binding of alpha-mangostin (α-KG) to IDH1-R132H. The structure–relationship study reveals that alpha-Mangostin (α-Mangostin) exhibits the strongest core inhibitor structure. alpha-Mangostin (α-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 (α-Mangostin) significantly inhibits light-induced degeneration of photoreceptors and 200 μM H2O2-induced apoptosis of RPE cells. 200 μM H2O2-induced generation of reactive oxygen species (ROS) and light-induced generation of malondialdehyde (MDA) are suppressed by alpha-Mangostin (α-Mangostin)[3]. | ||||||||||||||||
体内研究 (In Vivo) | alpha-Mangostin (α-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]. | ||||||||||||||||
分子量 | 410.46 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C24H26O6 | ||||||||||||||||
CAS 号 | 6147-11-1 | ||||||||||||||||
中文名称 | α-倒捻子素 | ||||||||||||||||
结构分类 |
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来源 |
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 110 mg/mL(267.99 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液
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