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Trypanocidal structure-activity relationship for cis- and trans-methylpluviatolide.
- Source :
-
Phytochemistry [Phytochemistry] 2008 Jun; Vol. 69 (9), pp. 1890-4. Date of Electronic Publication: 2008 May 12. - Publication Year :
- 2008
-
Abstract
- The trypanocidal activity of racemic mixtures of cis- and trans-methylpluviatolides was evaluated in vitro against trypomastigote forms of two strains of Trypanosoma cruzi, and in the enzymatic assay of T. cruzi gGAPDH. The cytotoxicity of the compounds was assessed by the MTT method using LLC-MK2 cells. The effect of the compounds on peroxide and NO production were also investigated. The mixture of the trans stereoisomers displayed trypanocidal activity (IC50 approximately 89.3 microM). Therefore, it was separated by chiral HPLC, furnishing the (+) and (-)-enantiomers. Only the (-)-enantiomer was active against the parasite (IC50 approximately 18.7 microM). Despite being inactive, the (+)-enantiomer acted as an antagonistic competitor. Trans-methylpluviatolide displayed low toxicity for LLC-MK2 cells, with an IC50 of 6.53 mM. Furthermore, methylpluviatolide neither inhibited gGAPDH activity nor hindered peroxide and NO production at the evaluated concentrations.
- Subjects :
- Animals
Cell Line
Macrophages drug effects
Macrophages metabolism
Mice
Molecular Structure
Nitric Oxide biosynthesis
Structure-Activity Relationship
Lactones chemistry
Lactones pharmacology
Lignans chemistry
Lignans pharmacology
Trypanocidal Agents chemistry
Trypanocidal Agents pharmacology
Trypanosoma cruzi drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0031-9422
- Volume :
- 69
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Phytochemistry
- Publication Type :
- Academic Journal
- Accession number :
- 18479721
- Full Text :
- https://doi.org/10.1016/j.phytochem.2008.04.002