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Leishmanicidal Effect of Synthetic trans-Resveratrol Analogs.


ABSTRACT:

Background

Stilbene-based compounds show antitumoral, antioxidant, antihistaminic, anti-inflammatory and antimicrobial activities. Here, we evaluated the effect of the trans-resveratrol analogs, pterostilbene, piceatannol, polydatin and oxyresveratrol, against Leishmania amazonensis.

Methodology/principal findings

Our results demonstrated a low murine macrophage cytotoxicity of all four analogs. Moreover, pterostilbene, piceatannol, polydatin and oxyresveratrol showed an anti-L. amazonensis activity with IC50 values of 18 ?M, 65 ?M, 95 ?M and 65 ?M for promastigotes, respectively. For intracellular amastigotes, the IC50 values of the analogs were 33.2 ?M, 45 ?M, 29 ?M and 30.5 ?M, respectively. Among the analogs assayed only piceatannol altered the cell cycle of the parasite, increasing 5-fold the cells in the Sub-G0 phase and decreasing 1.7-fold the cells in the G0-G1 phase. Piceatannol also changed the parasite mitochondrial membrane potential (??m) and increased the number of annexin-V positive promastigotes, which suggests incidental death.

Conclusion/significance

Among the analogs tested, piceatannol, which is a metabolite of resveratrol, was the more promising candidate for future studies regarding treatment of leishmaniasis.

SUBMITTER: Passos CL 

PROVIDER: S-EPMC4627731 | BioStudies | 2015-01-01

REPOSITORIES: biostudies

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