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Planta Med ; 78(18): 1939-41, 2012 Dec.
Article de Anglais | MEDLINE | ID: mdl-23150073

RÉSUMÉ

Tetrahydrofuran lignans represent a well-known group of phenolic compounds capable of acting as antiparasitic agents. In the search for new medicines for the treatment of Chagas disease, one promising compound is grandisin which has shown significant activity on trypomastigote forms of Trypanosoma cruzi. In this work, the in vitro metabolism of grandisin was studied in the pig cecum model and by biomimetic phase I reactions, aiming at an ensuing a preclinical pharmacokinetic investigation. Although grandisin exhibited no metabolization by the pig microbiota, one putative metabolite was formed in a biomimetic model using Jacobsen catalyst. The putative metabolite was tested against T. cruzi revealing loss of activity in comparison to grandisin.


Sujet(s)
Antiprotozoaires/pharmacocinétique , Maladie de Chagas/traitement médicamenteux , Furanes/métabolisme , Furanes/pharmacologie , Lignanes/métabolisme , Lignanes/pharmacologie , Piper/composition chimique , Extraits de plantes/pharmacologie , Trypanosoma cruzi/effets des médicaments et des substances chimiques , Animaux , Antiprotozoaires/composition chimique , Caecum/parasitologie , Structure moléculaire , Extraits de plantes/composition chimique , Suidae
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