一种含膦酸酯的荧光团，能够选择性诱导癌细胞凋亡。
A Phosphinate-Containing Fluorophore Capable of Selectively Inducing Apoptosis in Cancer Cells.
机构信息
Department of Chemistry, University of Nebraska, Lincoln, NE, 68588, USA.
Nebraska Center for Integrated Biomolecular Communication, University of Nebraska, Lincoln, NE, 68588, USA.
出版信息
Chembiochem. 2019 Jul 1;20(13):1712-1716. doi: 10.1002/cbic.201800811. Epub 2019 May 3.
Chemotherapeutic agents generally suffer from off-target cytotoxicity in noncancerous cell types, leading to undesired side effects. As a result, significant effort has been put into identifying compounds that are selective for cancerous over noncancerous cell types. Our laboratory has recently developed a series of near-infrared (NIR) fluorophores containing a phosphinate functionality at the bridging position of a xanthene scaffold, termed Nebraska Red (NR) fluorophores. Herein, we report the selective cytotoxicity of one NR derivative, NR , against HeLa (cervical cancer) cells versus NIH-3T3 (noncancerous fibroblast) cells. Mechanistic studies based on the NIR fluorescence signal of NR showed distinct subcellular localization in HeLa (mitochondrial) versus NIH-3T3 (lysosomal) that resulted from the elevated mitochondrial potential in HeLa cells. This study provides a new, NIR scaffold for the further development of reagents for targeted cancer therapy.
化疗药物通常会对非癌细胞类型产生非靶向细胞毒性，导致不良的副作用。因此，人们已经投入大量精力来寻找对癌细胞具有选择性的化合物，而不是非癌细胞。我们实验室最近开发了一系列近红外（NIR）荧光染料，它们在香豆素支架的桥接位置含有膦酸酯官能团，称为内布拉斯加红（NR）荧光染料。在此，我们报告了 NR 的一种衍生物 NR 对 HeLa（宫颈癌）细胞与 NIH-3T3（非癌细胞成纤维细胞）的选择性细胞毒性。基于 NR 的近红外荧光信号的机制研究表明，它在 HeLa（线粒体）与 NIH-3T3（溶酶体）中的亚细胞定位不同，这是由于 HeLa 细胞中线粒体的电势升高所致。这项研究为进一步开发用于靶向癌症治疗的试剂提供了一个新的近红外支架。
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