@article{fdi:010060554,
  title = {{P}ro-oxidant properties of indolone-{N}-oxides in relation to their antimalarial properties},
  author = {{Y}en, {N}. {T}. {H}. and {I}brahim, {H}. and {R}eybier, {K}. and {P}erio, {P}ierre and {S}ouard, {F}. and {N}ajahi, {E}. and {F}abre, {P}. {L}. and {N}epveu, {F}.},
  editor = {},
  language = {{ENG}},
  abstract = {{I}ndolone-{N}-oxides ({INOD}s) are bioreducible and possess remarkable anti-malarial activities in the low nanomolar range in vitro against different {P}lasmodium falciparum ({P}. falciparum) strains and in vivo. {INOD}s have an original mechanism of action: they damage the host cell membrane without affecting non-parasitized erythrocytes. {T}hese molecules produce a redox signal which activates {SYK} tyrosine kinases and induces a hyperphosphorylation of {AE}1 (band 3, erythrocyte membrane protein). {T}he present work aimed to understand the early stages of the biochemical interactions of these compounds with some erythrocyte components from which the redox signal could originate. {T}he interactions were studied in a biomimetic model and compared with those of chloroquine and artemisinin. {T}he results showed that {INOD}s i) do not enter the coordination sphere of the metal in the heme iron complex as does chloroquine; ii) do not generate iron-dependent radicals as does artemisinin; iii) generate stable free radical adducts after reduction at one electron; iv) cannot trap free radicals after reduction. {T}hese results confirm that the bioactivity of {INOD}s does not lie in their spin-trapping properties but rather in their pro-oxidant character. {T}his property may be the initiator of the redox signal which activates {SYK} tyrosine kinases.},
  keywords = {{P}ro-oxidant drugs ; {I}ndolone-{N}-oxides ; {A}ntimalarial drugs ; {C}yclic voltammetry ; {E}lectron paramagnetic resonance ({EPR})},
  booktitle = {},
  journal = {{J}ournal of {I}norganic {B}iochemistry},
  volume = {126},
  numero = {},
  pages = {7--16},
  ISSN = {0162-0134},
  year = {2013},
  DOI = {10.1016/j.jinorgbio.2013.04.012},
  URL = {https://www.documentation.ird.fr/hor/fdi:010060554},
}