Nelumal A, the Active Principle of Ligularia nelumbifolia, is a Novel Aromatase Inhibitor

被引:0
|
作者
Epifano, Francesco [1 ]
Genovese, Salvatore [1 ]
Fiorito, Serena [1 ]
Nde, Chantal Magne [2 ]
Clyne, Colin [2 ,3 ]
机构
[1] Univ G dAnnunzio, Dept Pharm, I-66100 Chieti, CH, Italy
[2] Prince Henrys Inst Med Res, Canc Drug Discovery Lab, Clayton, Vic 3168, Australia
[3] Monash Univ, Dept Biochem & Mol Biol, Clayton, Vic 3168, Australia
关键词
Aromatase inhibitors; Ligularia nelumbifolia; Nelumal A; Oxyprenylated secondary metabolites;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Nelumal A, the active principle of Ligularia nelumbifolia was preliminarily tested as an aromatase inhibitors in HEK293 cells trartsfected with aromatase cDNA and using anastrazole as the reference drug. This screening revealed that it showed an appreciable level of inhibition. Subsequent experiments aimed to evaluate the aromatase activity and expression in KGN cells confirmed that the title natural product, after an incubation of 48 h, compared favourably with artastrazole (1 mu M) in the concentration range 10 - 30 mu M. Moreover, nelumal A (30 mu M) abolished the aromatase mRNA expression in the same cell line.
引用
收藏
页码:823 / 824
页数:2
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