An NBD Derivative of the Selective Rat Toxicant Norbormide as a New Probe for Living Cell Imaging

Frontiers in Pharmacology
Claudio D'AmoreSergio Bova

Abstract

Norbormide (NRB) is a unique compound that acts directly on rat vascular myocytes to trigger a contractile process, through an as yet unknown mechanism, which results in the selective contraction of rat peripheral arteries. To gain insight into the mechanisms involved in NRB rat-selective activity, we investigated the subcellular distribution of NRB-AF12, a nitrobenzoxadiazole (NBD)-derivative of NRB, in living NRB-sensitive and NRB-insensitive cells. In both cell types, NRB-AF12 localized to the endoplasmic reticulum (ER), Golgi apparatus, mitochondria, lysosomes, and endosomes; however, in NRB-sensitive cells, the fluorescence also extended to the plasma membrane. NRB-AF12 was rapidly internalized into the cells, could easily be washed out and then reloaded back into the same cells, all with a high degree of reproducibility. Cells exposed for 24 h to NRB-AF12 did not show apparent signs of toxicity, even at concentrations of the dye (10 μM) much higher than those required for fluorescence labeling (500 ηM). The distribution pattern of NRB-AF12 fluorescence was near identical to that of ER-Tracker® (Er-Tr), a fluorescent derivative of glibenclamide, a known KATP channel blocker. Displacement tests did not demonstrate, but at t...Continue Reading

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Citations

Dec 7, 2018·Molecular Diversity·Xuelian LiuZhaohai Qin
Dec 6, 2019·Frontiers in Neuroscience·Barbara NapoliGenny Orso

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Datasets Mentioned

BETA
GM130

Methods Mentioned

BETA
confocal microscopy
column chromatography
Fluorescence
dissection

Software Mentioned

NIS Elements
Fiji

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