ChloroquineV1, Hal, Checkpoint, bibRecord, 000220

Experimental pharmacological study of the antimalarial activity of a compound of synthesis: the methylthioninium chloride

Identifieur interne : 000220 ( Hal/Checkpoint ); précédent : 000219; suivant : 000221

Experimental pharmacological study of the antimalarial activity of a compound of synthesis: the methylthioninium chloride

Auteurs : Giovanny Garavito [France]

Source :

RBID : Hal:tel-00639025

Descripteurs français

mix :
- Antipaludiques, Bleu de méthylène, Chimiosensibilité, Glutathion, Hème., Interactions de drogues, Paludisme, Pharmacologie, Plasmodium, Stade sensible.
Wicri :
- topic : Pharmacologie.

English descriptors

mix :
- Chemosensitivity, Malaria, antimalarials, drug interactions, glutathione, haem., methylene blue, pharmacology, sensible stage.

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.

Url:

https://tel.archives-ouvertes.fr/tel-00639025

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Hal:tel-00639025

Le document en format XML

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<title xml:lang="fr">Etude pharmacologique expérimentale de l'activité antipaludique d'un composé de synthèse: le chlorure de methylthioninium</title>
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<term>haem.</term>
<term>methylene blue</term>
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<keywords scheme="mix" xml:lang="fr"><term>Antipaludiques</term>
<term>Bleu de méthylène</term>
<term>Chimiosensibilité</term>
<term>Glutathion</term>
<term>Hème.</term>
<term>Interactions de drogues</term>
<term>Paludisme</term>
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<term>Stade sensible</term>
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<front><div type="abstract" xml:lang="en">              <p>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.</p>
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            <title xml:lang="fr">Etude pharmacologique expérimentale de l'activité antipaludique d'un composé de synthèse: le chlorure de methylthioninium</title>
            <author role="aut">              <persName>                <forename type="first">Giovanny</forename>
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                <title xml:lang="fr">Etude pharmacologique expérimentale de l'activité antipaludique d'un composé de synthèse: le chlorure de methylthioninium</title>
                <author role="aut">                  <persName>                    <forename type="first">Giovanny</forename>
                    <surname>Garavito</surname>
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                  <email type="md5">c3a5f36da8ebb36b6ca2db79af664cc4</email>
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                <authority type="jury">J. C. Gantier, (Rapporteur)</authority>
                <authority type="jury">O. Bain (Rapporteur)</authority>
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                <authority type="jury">E. Deharo (Examinateur)</authority>
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                <term xml:lang="en">antimalarials</term>
                <term xml:lang="en">pharmacology</term>
                <term xml:lang="en">methylene blue</term>
                <term xml:lang="en">Chemosensitivity</term>
                <term xml:lang="en">drug interactions</term>
                <term xml:lang="en">sensible stage</term>
                <term xml:lang="en">glutathione</term>
                <term xml:lang="en">haem.</term>
                <term xml:lang="fr">Paludisme</term>
                <term xml:lang="fr">Antipaludiques</term>
                <term xml:lang="fr">Pharmacologie</term>
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            <abstract xml:lang="en">              <p>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.</p>
            </abstract>
            <abstract xml:lang="fr">              <p>Nous nous sommes intéressés à l'activité antipaludique du bleu de méthylène (BM), qui fut la première molécule de synthèse utilisée dans le traitement des accès palustres. Nous avons montré que le BM est actif sur des souches cultivées de Plasmodium falciparum d'origines géographiques et de chloroquino-sensibilités différentes (CI50<10nM). Il est aussi actif sur le cycle sanguin de Plasmodium murin (DE50<15mg/Kg), mais pas sur la phase hépatique. Les stades érythrocytaires les plus sensibles sont les stades jeunes. Les associations avec les traitements classiques sont de type : antagoniste avec amodiaquine ; antagonisme-additif avec atovaquone, doxycycline, pyrimethamine ; additive-pas d'interaction avec artemether, chloroquine, mefloquine, primaquine et synergique avec la quinine. Nous avons montré par spectrométrie UV, CCM et spectrométrie de masse, qu'il n'y a pas de liaison entre le BM et l'hème. Nous avons également mis au point une nouvelle technique pour mesurer la transformation de l'hème par le glutathion et mesurer ainsi l'activité des drogues sur cette transformation.</p>
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Experimental pharmacological study of the antimalarial activity of a compound of synthesis: the methylthioninium chloride

Experimental pharmacological study of the antimalarial activity of a compound of synthesis: the methylthioninium chloride

Source :

Descripteurs français

English descriptors

Abstract

Links toward previous steps (curation, corpus...)

Links to Exploration step

Le document en format XML

Pour manipuler ce document sous Unix (Dilib)

Pour mettre un lien sur cette page dans le réseau Wicri