A Phosphinate-Containing Fluorophore Capable of Selectively Inducing Apoptosis in Cancer Cells

Xinqi Zhou, Yuan Fang, Lauren Lesiak, Cliff I. Stains

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

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, NR744, against HeLa (cervical cancer) cells versus NIH-3T3 (noncancerous fibroblast) cells. Mechanistic studies based on the NIR fluorescence signal of NR744 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.

Original languageEnglish (US)
Pages (from-to)1712-1716
Number of pages5
JournalChemBioChem
Volume20
Issue number13
DOIs
StatePublished - Jul 1 2019

Keywords

  • apoptosis
  • cancer
  • cytotoxicity
  • fluorescence probes
  • phosphinate

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry

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