%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture non répertoriées par l'AERES
%A Fournet, Alain
%A Inchausti, A.
%A Yaluff, G.
%A Rojas de Arias, A.
%A Guinaudeau,H.
%A Bruneton, J.
%A Breidenbach, M.A.
%A Karplus, P.A.
%A Faerman, C.H.
%T Trypanocidal bisbenzylisoquinoline alkaloids are inhibitors of trypanothione reductase
%D 1998
%L fdi:010013809
%G ENG
%J Journal of Enzyme Inhibition
%K MALADIE DE CHAGAS ; TRAITEMENT MEDICAL ; ALCALOIDE
%K INHIBITEUR DE LA TRYPANOTHIONE REDUCTASE ; ALCALOIDE TRYPANOCIDE ; BISBENZYLISOQUINOLEINE
%P 1-9
%U https://www.documentation.ird.fr/hor/fdi:010013809
%> https://horizon.documentation.ird.fr/exl-doc/pleins_textes/pleins_textes_6/b_fdi_49-50/010013809.pdf
%V 13
%W Horizon (IRD)
%X Eleven bisbenzylisoquinoline (BBIQ) alkaloids were studied for in vitro trypanocidal activity against trypomastigote forms of the Y strain of #Trypanosoma cruzi$. The inhibitory activity of these compounds against trypanothione reductase (TR), a target enzyme for chemotherapy against Chagas disease, was also studied. Six BBIQ alkaloids (antioquine, cepharanthine, daphnoline, limacine, cycleanine and (-) curine) displayed a 50% lethal concentration (LC50) against #T. cruzi$ of less than 100 microM. Daphnoline and curine, with LC50 values of 10 microM, are attractive for further investigation as potential anti-Chagasic drugs. Kinetic analyses suggested the BBIQ alkaloids are mixed inhibitors of TR. These compounds are reasonably potent inhibitors of TR ; the best TR inhibitor, cepharanthine, had an IC50 of 15 microM, which is the same order of magnitude as its LC50 against #T. cruzi$. The similar magnitudes of the IC50 and LC50 values suggest that inhibition of TR could contribute to the trypanocidal activity exhibited by the BBIQ alkaloids. (Résumé d'auteur)
%$ 052GLOTRY03