Jurášek Michal, Rimpelová Silvie, Pavlíčková Vladimíra, Ruml Tomáš, Lapčík Oldřich, Drašar Pavel B
Department of Chemistry of Natural Compounds, Institute of Chemical Technology in Prague, 166 28 Prague, Czech Republic.
Department of Biochemistry and Microbiology, Institute of Chemical Technology in Prague, 166 28 Prague, Czech Republic.
Steroids. 2015 May;97:62-6. doi: 10.1016/j.steroids.2014.10.002. Epub 2014 Nov 1.
Here, we report synthesis and biological evaluation of fluorescent nandrolone-3-carboxymethyloxime derivatives conjugated with green-emitting bodipy dye via PEG linkers. All the newly-synthesized compounds were evaluated for their effect on cell proliferation in vitro in MCF-7, LNCaP, PC-3 and HEK 293T model cell lines using WST-1 assay. By means of live-cell fluorescence microscopy, the intracellular localization of nandrolone-bodipy conjugates was revealed in endoplasmic reticulum. Moreover, we performed competitive localization study with nonfluorescent nandrolone, metandrolone, boldenone, trenbolone, and testosterone.
在此，我们报告了通过聚乙二醇（PEG）接头与发出绿色荧光的硼二吡咯（BODIPY）染料共轭的荧光诺龙-3-羧甲基肟衍生物的合成及生物学评价。使用WST-1检测法，对所有新合成的化合物在MCF-7、LNCaP、PC-3和HEK 293T模型细胞系中的体外细胞增殖作用进行了评价。通过活细胞荧光显微镜观察，发现诺龙-硼二吡咯共轭物在内质网中的细胞内定位。此外，我们用非荧光的诺龙、美雄酮、勃地酮、群勃龙和睾酮进行了竞争性定位研究。
