Bergapten

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Chemical Structure| 484-20-8 同义名 : 佛手苷内酯 ;5-Methoxypsoralen; 5-MOP; NSC 95437; Heraclin
CAS号 : 484-20-8
货号 : A141454
分子式 : C12H8O4
纯度 : 98%
分子量 : 216.19
MDL号 : MFCD00010272
存储条件:

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 5-Methoxypsoralen (Bergapten) is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. 5-methoxypsoralen led to time-dependent as well as dose-dependent inhibitory effects on U-87MG human glioma cells. 5-Methoxypsoralen led to a substantial decrease of cell count along with distorted cell morphology. 5-methoxypsoralen also led to dose-dependent G2/M phase cell cycle arrest. 5-Methoxypsoralen-treated cells also exhibited altered cell ultrastructure with the appearance of autophagic vacuoles and the number of these vacuoles increased with increasing drug dose[3]. 5-MOP (5-Methoxypsoralen) increased the activity of NAT (N-acetyltransferase) and also increased the further metabolism of AAF ( 2-acetylaminofluorene) at 24 h in the rat stomach. 5-MOP decreased the activity of NAT only at 72-h incubation in SC-M1 cells. The optimal concentrations of 5-MOP to induce decreased NAT activity in SC-M1 (human stomach) cells were 0.05 mM to 25 mM. In COLO 205 cells, there is decreased NAT activity at low doses of Bergapten (0.05 mM and 0.5 mM) and increased NAT activity at a high dose (50 mM)[4]. In addition, DSG (diosgenin) and 5-MOP may improve insulin resistance through an ER-mediated PI3K/Akt activation pathway[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00533195 Atopic Dermatitis Phase 3 Completed - Austria ... 展开 >> Medical University of Vienna; University Clinic of Dermatology; Division of Special and Environmental Dermatology Vienna, Austria, 1090 收起 <<
NCT00811005 Pustular Palmoplantar Psoriasi... 展开 >>s 收起 << Phase 3 Unknown October 2010 Austria ... 展开 >> Medical University of Vienna; University Clinic of Dermatology; Division of Special and Environmental Dermatology Vienna, Austria, 1180 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.63mL

0.93mL

0.46mL

23.13mL

4.63mL

2.31mL

46.26mL

9.25mL

4.63mL

参考文献

[1]Panno ML, Giordano F, et al.Bergapten induces ER depletion in breast cancer cells through SMAD4-mediated ubiquitination. Breast Cancer Res Treat. 2012 Nov;136(2):443-55.

[2]Liu WX, Jia FL, et al. Protective effects of 5-methoxypsoralen against acetaminophen-induced hepatotoxicity in mice. World J Gastroenterol. 2012 May 14;18(18):2197-202.

[3]Guo H, He Y, Bu C, Peng Z. Antitumor and apoptotic effects of 5-methoxypsoralen in U87MG human glioma cells and its effect on cell cycle, autophagy and PI3K/Akt signaling pathway. Arch Med Sci. 2019;15(6):1530-1538

[4]Lee YM, Wu TH. Effects of 5-methoxypsoralen (5-MOP) on arylamine N-acetyltransferase activity in the stomach and colon of rats and human stomach and colon tumor cell lines. In Vivo. 2005;19(6):1061-1069

[5]Fang K, Dong H, Jiang S, et al. Diosgenin and 5-Methoxypsoralen Ameliorate Insulin Resistance through ER-α/PI3K/Akt-Signaling Pathways in HepG2 Cells. Evid Based Complement Alternat Med. 2016;2016:7493694