Activity of 8.O.4'-neolignans against Trypanosoma cruzi.
The in vitro evaluation of a series of 8.O.4'-neolignans (in their ketone, alcohol, and acetylated forms) on the proliferation of Trypanosoma cruzi led to the detection of three compounds with interesting activities against T. cruzi epimastigotes. These compounds also inhibited the in vitro differentiation of epimastigotes to trypomastigotes. When tested against HeLa cells, the same compounds did not affect the cell vitality and showed a low influence on cell viability as measured by dimethylthiazol diphenyltetrazolium bromide reduction. The three phenylpropanoid moieties tested did not show any activity against T. cruzi. One of the tested compounds, compound 4 (3,4-methylenedioxi7-oxo-1'-allyl-3',5'-dimethoxy-8.O.4'-neolignan) showed the best performance in both trypanocide and cytotoxic assays, suggesting that it should be considered as a leading structure for further research.
Nocito
Isabel
I
Area Parasitología, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Suipacha 531, 2000, Rosario, Argentina.
Castelli
María Victoria
MV
Zacchino
Susana A
SA
Serra
Esteban
E
D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002470:Cell Survival; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D017705:Lignans / Q000494:pharmacology* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development
D000981:Antiprotozoal Agents; D017705:Lignans
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