Abstract
BackgroundStilbene-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 FindingsOur 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 μM, 65 μM, 95 μM and 65 μM for promastigotes, respectively. For intracellular amastigotes, the IC50 values of the analogs were 33.2 μM, 45 μM, 29 μM and 30.5 μM, 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 (ΔΨm) and increased the number of annexin-V positive promastigotes, which suggests incidental death.Conclusion/SignificanceAmong the analogs tested, piceatannol, which is a metabolite of resveratrol, was the more promising candidate for future studies regarding treatment of leishmaniasis.
Highlights
Leishmaniasis is a public health problem that affects 98 countries on 5 continents, and approximately 1.1 to 1.7 million cases of leishmaniasis occurs each year [1]
Our results demonstrated an anti-leishmanial activity of these analogs with IC50 values of 18, 65, 95.5 and 65 μM for pterostilbene, piceatannol, polydatin and oxyresveratrol, respectively, after 48 h of treatment
The anti-amastigote activity was tested after 24 h of treatment, and our results showed that the IC50 value of pterostilbene, piceatannol, polydatin and oxyresveratrol was calculated as 33.2 μM, 45 μM, 29 μM and 30.5 μM, respectively (Table 1)
Summary
Leishmaniasis is a public health problem that affects 98 countries on 5 continents, and approximately 1.1 to 1.7 million cases of leishmaniasis occurs each year [1]. Pentavalent antimonials are the first-line drugs for treating leishmaniasis; amphotericin B, pentamidine, and paramomycin, are secondary options for the treatment of resistant cases [2, 3]. All of these drugs have problems that limit their use, such as side effects, the induction of parasite resistance, in-patient. Leishmanicidal Effect of Synthetic trans-Resveratrol Analogs administration and high costs [4]. We evaluated the effect of the trans-resveratrol analogs, pterostilbene, piceatannol, polydatin and oxyresveratrol, against Leishmania amazonensis
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