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-l7,12-olide (2), as the anti-Trypanosoma cruzi active principles. T...

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Bibliographic Details
Published in:Natural product communications 2012-09, Vol.7 (9), p.1139-1142
Main Authors: Varela, Javier, Lavaggi, María L., Cabrera, Mauricio, Rodríguez, Alejandra, Miño, Patricio, Chiriboga, Ximena, Cerecetto, Hugo, González, Mercedes
Format: Article
Language:English
Subjects:
Animals
Asteraceae - chemistry
Cell Line
Diterpenes - pharmacology
Humans
Mice
Trypanocidal Agents - pharmacology
Trypanosoma cruzi - drug effects
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Summary: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-l7,12-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 μg/mL) whereas the isolated compounds 1 and 2 were near to seven- and one and a half-fold (IC50= 3.0 and 15.6 μg/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.
ISSN:1934-578X
1555-9475
DOI:10.1177/1934578X1200700907