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Etude pharmacologique expérimentale de l'activité antipaludique d'un composé de synthèse: le chlorure de methylthioninium

Abstract : We studied the antimalarial activity of methylene blue (BM), which was the first synthetic molecule used in the treatment of malaria. We showed that BM is active on Plasmodium falciparum strains from different geographical origins and chloroquino-sensitivities (IC50<10nM). It is also active on the blood cycle of rodent malaria (ED50<15mg/Kg), but not on the hepatic phase. The most sensitive erythrocytic stages are young stages. Associations with traditional treatments are: antagonist with amodiaquine; antagonism-additive with atovaquone, doxycycline, pyrimethamine; additive-pas d'interaction with artemether, chloroquine, mefloquine, primaquine and synergistic with quinine. We showed by spectrometry UV, TLC and mass spectrometry, that there is no association between BM and hem. We also developed a new technique to measure the transformation of hem by the glutathione and to measure the activity of drugs on this transformation.
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Submitted on : Tuesday, November 8, 2011 - 2:09:26 PM
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Giovanny Garavito. Etude pharmacologique expérimentale de l'activité antipaludique d'un composé de synthèse: le chlorure de methylthioninium. Pharmacologie. Université Paul Sabatier - Toulouse III, 2007. Français. ⟨tel-00639025⟩

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