title: In vitro antileishmanial activity of resveratrol and its hydroxylated analogues against Leishmania major promastigotes and amastigotes.
abstract: Resveratrol, a natural phytoalexin found mainly in grapes, possesses a variety of beneficial activities including anticancer, antimicrobial and antiviral. However, there is no information about its effects on kinetoplastid parasites such as Leishmania. Leishmania is a human pathogen responsible for a spectrum of diseases known as leishmaniases and a significant health problem in many parts of the world. In this study, we investigated effects of resveratrol and its hydroxylated analogues on Leishmania major, a causative agent of zoonotic cutaneous leishmaniasis in the Old World. Resveratrol showed antileishmanial activity against promastigotes in vitro and, more importantly, was effective against intracellular amastigotes, a parasite life stage infectious in humans, as detected in in vitro macrophage assay. The hydroxylated stilbenes tested in this study also showed antileishmanial activity against promastigotes, the most promising being 3,4,4',5'-tetrahydroxy-trans-stilbene. This compound showed excellent antileishmanial activity against extracellular promastigotes in vitro but not intracellular amastigotes. Our results suggest that resveratrol may be useful as a therapeutic agent to treat leishmaniasis and warrant its further assessment in animal models of disease.
authors.affiliation: Infection and Immunity Division, Walter and Eliza Hall Institute of Medical Research, Parkville, 3050, Victoria, Australia. kedzierski@wehi.edu.au
authors.forename: Lukasz
authors.initials: L
authors.lastname: Kedzierski
authors.forename: Joan M
authors.initials: JM
authors.lastname: Curtis
authors.forename: Milena
authors.initials: M
authors.lastname: Kaminska
authors.forename: Jadwiga
authors.initials: J
authors.lastname: Jodynis-Liebert
authors.forename: Marek
authors.initials: M
authors.lastname: Murias
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D006801:Humans; D018320:Leishmania major / Q000187:drug effects*; D008264:Macrophages; D051379:Mice; D000077185:Resveratrol; D013267:Stilbenes / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D013267:Stilbenes; D000077185:Resveratrol