Antiprotozoal and cytotoxic studies on some isocordoin derivatives.
Isocordoin (1) and 2',4'-dihydroxy-3'-(gamma,gamma-dimethylallyl)-dihydrochalcone (7), chalcones isolated from the root of Lonchocarpus xuul, together with six analogues of 1 were tested in vitro against promastigotes of Leishmania mexicana and epimastigotes of Trypanosoma cruzi. Additionally, cytotoxic studies with MDCK cells were carried out using the MTT method. Among these derivatives, 2',4'-diacetoxy-3'-(3-methylbut-2-enyl)-chalcone (2) and 2',4'-dimethoxy-3'-(3-methylbut-2-enyl)-chalcone (3) showed the strongest antiprotozoal activity and lower cytotoxicity in comparison with isocordoin at a concentration in the microM range. Derivative 3 had the strongest trypanocidal activity with IC(50) values lower than those of nifurtimox and benznidazole, the common drugs used against these parasites. The selectivity index calculated for 3 (SI 109.3) confirms the selective trypanocidal activity of this metabolite.
Centro de Investigación Científica de Yucatán, Mérida, Yucatán, Mexico. rborges@cicy.mx
Rocio
R
Borges-Argáez
Teresita
T
Vela-Catzín
Alejandro
A
Yam-Puc
Manuel Jesús
MJ
Chan-Bacab
Rosa Esther
RE
Moo-Puc
Mirbella
M
Cáceres-Farfán
D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001203:Ascomycota; D002396:Catechols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D002460:Cell Line; D004285:Dogs; D007887:Fabaceae / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D007894:Leishmania mexicana / Q000187:drug effects*; D010936:Plant Extracts / Q000737:chemistry; D014349:Trypanosoma cruzi / Q000187:drug effects*
D000981:Antiprotozoal Agents; D002396:Catechols; D010936:Plant Extracts; C438026:isocordoin