β-Galactosidase fluorescence probe with improved cellular accumulation based on a spirocyclized rhodol scaffold

J Am Chem Soc. 2011 Aug 24;133(33):12960-3. doi: 10.1021/ja204781t. Epub 2011 Aug 3.

Abstract

We identified a rhodol bearing a hydroxymethyl group (HMDER) as a suitable scaffold for designing fluorescence probes for various hydrolases. HMDER shows strong fluorescence at physiological pH, but phenolic O-alkylation of HMDER results in a strong preference for the spirocyclic form, which has weak fluorescence. As a proof of concept, we utilized this finding to develop a new fluorescence probe for β-galactosidase. This probe has favorable characteristics for imaging in biological samples: it has good cellular permeability, and its hydrolysis product is well-retained intracellularly. It could rapidly and clearly visualize β-galactosidase activity in cultured cells and in Drosophila melanogaster tissue, which has rarely been achieved with previously reported fluorescence probes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Membrane Permeability
  • Cells, Cultured
  • Cyclization
  • Drosophila melanogaster
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • Fluorescent Dyes / pharmacokinetics
  • Spiro Compounds / chemistry
  • beta-Galactosidase / analysis*

Substances

  • Fluorescent Dyes
  • Spiro Compounds
  • beta-Galactosidase