@article{fdi:010013809, title = {{T}rypanocidal bisbenzylisoquinoline alkaloids are inhibitors of trypanothione reductase}, author = {{F}ournet, {A}lain and {I}nchausti, {A}. and {Y}aluff, {G}. and {R}ojas de {A}rias, {A}. and {G}uinaudeau,{H}. and {B}runeton, {J}. and {B}reidenbach, {M}.{A}. and {K}arplus, {P}.{A}. and {F}aerman, {C}.{H}.}, editor = {}, language = {{ENG}}, abstract = {{E}leven bisbenzylisoquinoline ({BBIQ}) alkaloids were studied for in vitro trypanocidal activity against trypomastigote forms of the {Y} strain of #{T}rypanosoma cruzi$. {T}he inhibitory activity of these compounds against trypanothione reductase ({TR}), a target enzyme for chemotherapy against {C}hagas disease, was also studied. {S}ix {BBIQ} alkaloids (antioquine, cepharanthine, daphnoline, limacine, cycleanine and (-) curine) displayed a 50% lethal concentration ({LC}50) against #{T}. cruzi$ of less than 100 micro{M}. {D}aphnoline and curine, with {LC}50 values of 10 micro{M}, are attractive for further investigation as potential anti-{C}hagasic drugs. {K}inetic analyses suggested the {BBIQ} alkaloids are mixed inhibitors of {TR}. {T}hese compounds are reasonably potent inhibitors of {TR} ; the best {TR} inhibitor, cepharanthine, had an {IC}50 of 15 micro{M}, which is the same order of magnitude as its {LC}50 against #{T}. cruzi$. {T}he similar magnitudes of the {IC}50 and {LC}50 values suggest that inhibition of {TR} could contribute to the trypanocidal activity exhibited by the {BBIQ} alkaloids. ({R}{\'e}sum{\'e} d'auteur)}, keywords = {{MALADIE} {DE} {CHAGAS} ; {TRAITEMENT} {MEDICAL} ; {ALCALOIDE} ; {INHIBITEUR} {DE} {LA} {TRYPANOTHIONE} {REDUCTASE} ; {ALCALOIDE} {TRYPANOCIDE} ; {BISBENZYLISOQUINOLEINE}}, booktitle = {}, journal = {{J}ournal of {E}nzyme {I}nhibition}, volume = {13}, numero = {}, pages = {1--9}, year = {1998}, URL = {https://www.documentation.ird.fr/hor/fdi:010013809}, }