Service interruption on Monday 11 July from 12:30 to 13:00: all the sites of the CCSD (HAL, EpiSciences, SciencesConf, AureHAL) will be inaccessible (network hardware connection).
Skip to Main content Skip to Navigation
Preprints, Working Papers, ...

Targeting mitochondria with novel, differently vectorized linear phosphorylated nitrones:

Abstract : The free radicals (FR) occurrence in biological signalling or as pathologies triggers is well-documented and the design of specific scavengers to limit oxidative stress is enthralling. Because FR become inactivated upon addition to nitrones, efforts have focused on developing alpha-phenyl-N-tert-butylnitrone derivatives (PBNs) with promising pre-clinical data. To improve efficacy, a new generation of nitrones derived from 2-(diethoxyphosphoryl)-N-(benzylidene)propan-2-amine-N-oxide (PPNs) incorporating an antioxidant framework, gave rise to multipotent drugs exhibiting EPR-spin-trapping properties. As mitochondrial dysfunction is involved in many disorders, efforts have been concentrated on developing tools (pH probes) or pharmacological agents targeting-mitochondria. A series of mitochondria-targeted PPNs was synthesized based on the improved biocompatibility of P-containing nitrones and the expected benefits of introducing a cationic vector. Spin-adducts EPR-parameters toward biologically-relevant FR were established. Cytotoxicity was determined on cells and mitochondria-permeation assessed in isolated rat organs. New mitochondria-targeting nitrones appeared as lower cytotoxic alternative to the commonly used mito-PBN and were safely applied for investigating the anticancer-mechanism of new drugs impacting mitochondria.
Document type :
Preprints, Working Papers, ...
Complete list of metadata
Contributor : Sophie Thétiot-Laurent Connect in order to contact the contributor
Submitted on : Friday, June 18, 2021 - 11:34:45 AM
Last modification on : Sunday, June 26, 2022 - 3:09:53 AM


Files produced by the author(s)


  • HAL Id : hal-03081866, version 3



Caroline Delehedde, Sophie Thétiot-Laurent, Mathieu Esgulian, Mathieu Chocry, Antal Rockenbauer, et al.. Targeting mitochondria with novel, differently vectorized linear phosphorylated nitrones:. 2020. ⟨hal-03081866v3⟩



Record views


Files downloads