Fournet Alain auteur aut IRD Inchausti A. auteur aut IRD Yaluff G. auteur aut IRD Rojas de Arias A. auteur aut IRD Guinaudeau H. auteur aut IRD Bruneton J. auteur aut IRD Breidenbach M.A. auteur aut IRD Karplus P.A. auteur aut IRD Faerman C.H. auteur aut IRD text journalArticle eng text/pdf reformatted digital access 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) specialized MALADIE DE CHAGAS TRAITEMENT MEDICAL ALCALOIDE INHIBITEUR DE LA TRYPANOTHIONE REDUCTASE ALCALOIDE TRYPANOCIDE BISBENZYLISOQUINOLEINE 052GLOTRY03 13 1-9 1998 https://www.documentation.ird.fr/hor/fdi:010013809 [F B010013809] 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 IRD - Base Horizon / Pleins textes 1998-06-10 2020-08-03 fdi:010013809 fre