Bioactive-guided identification of labdane diterpenoids from aerial parts of Aristeguietia glutinosa as anti-Trypanosoma cruzi agents.
A bioactive-guided investigation of the hydro-ethanolic extract of aerial parts of Aristeguietia glutinosa Lam. resulted in the isolation of two diterpenoids, (+)-15-hydroxy-labd-7-en-17-al (1) and (+)-13,14,15,16-tetranor-labd-7-en-17,12-olide (2), as the anti-Trypanosoma cruzi active principles. The structures of 1 and 2 were determined by spectroscopic analysis. The hydro-ethanolic extract showed anti-T. cruzi activity (IC50 = 19.6 microg/mL) whereas the isolated compounds 1 and 2 were near to seven- and one and a half-fold (IC50 = 3.0 and 15.6 microg/mL), respectively more active than the original extract. Labdene 1, equipotent as the reference compound (Nifurtimox), displayed low hemolytic activity, low toxicity against murine macrophages, and absence of mutagenicity. These results support the vernacular medicinal use of this plant as an anti-T. cruzi agent.
Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, Uruguay.
Javier
J
Varela
María L
ML
Lavaggi
Mauricio
M
Cabrera
Alejandra
A
Rodríguez
Patricio
P
Miño
Ximena
X
Chiriboga
Hugo
H
Cerecetto
Mercedes
M
González
D000818:Animals; D019659:Asteraceae / Q000737:chemistry*; D002460:Cell Line; D004224:Diterpenes / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D014344:Trypanocidal Agents / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D004224:Diterpenes; D014344:Trypanocidal Agents; C433017:labdane