Trypanocidal activity and acute toxicity assessment of triterpene acids.
The present study evaluates the in vitro and in vivo trypanocidal activity of ursolic acid and oleanolic acid against the Bolivia strain of Trypanosoma cruzi. Their acute toxicity is also assessed on the basis of median lethal dose (DL50) determination and quantification of biochemical parameters. Ursolic acid is the most active compound in vitro, furnishing IC50 of 25.5 microM and displaying 77% of trypomastigote lysis at a concentration of 128 microM. In agreement with in vitro assays, the results obtained for the in vivo assay reveals that ursolic acid (at a dose of 20 mg/Kg/day) provides the most significant reduction in the number of parasites at the parasitemic peak. Results concerning the LD50 assay and the biochemical parameters evaluated in the present study demonstrate that these substances can be safely used on an experimental basis.
Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil. danisf@fcfrp.usp.br
Daniele da Silva
Dda S
Ferreira
Viviane Rodrigues
VR
Esperandim
Miriam Paula Alonso
MP
Toldo
Juliana
J
Saraiva
Wilson Roberto
WR
Cunha
Sérgio
S
de Albuquerque
D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D014355:Chagas Disease / Q000188:drug therapy* / Q000469:parasitology; D006801:Humans; D020128:Inhibitory Concentration 50; D007928:Lethal Dose 50; D008297:Male; D018512:Parasitemia; D051381:Rats; D017208:Rats, Wistar; D014315:Triterpenes / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000494:pharmacology* / Q000627:therapeutic use* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects*; D000097245:Ursolic Acid
D014315:Triterpenes; D014344:Trypanocidal Agents; D000097245:Ursolic Acid