In vitro antileishmanial activity of resveratrol and its hydroxylated analogues against Leishmania major promastigotes and amastigotes

Infection and Immunity Division, Walter and Eliza Hall Institute of Medical Research, Parkville, 3050, Victoria, Australia.
Parasitology Research (Impact Factor: 2.1). 01/2008; 102(1):91-7. DOI: 10.1007/s00436-007-0729-y
Source: PubMed


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.

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Available from: Marek Murias, Feb 18, 2014
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    • "Plant derived compounds like genistein, virosecurine, ursolic acid, RESV etc. have shown as promising anthelmintic agents when exposed to different helminthes like cestode (R. echinobothrida), trematode (Fasciolopsis buski) and nematodes (Ascaridia galli, Setaria cervi and Trichinella spiralis) (Ozkoc et al., 2009; Kar and Tandon, 2004; Roy et al., 2012; Dasgupta et al., 2013; Giri and Roy, 2014; Saini et al., 2014). RESV also reported to have antiprotozoan properties as it inhibit the growth of different protozoa like Leishmania major and Plasmodium falciparum (Kedzierski et al., 2007; Son et al., 2007). "
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    ABSTRACT: Northeast India is geographically nestled as one of the biodiversity hotspots, rich in traditionally used medicinal plants. Resveratrol, a naturally occurring phytoalexin found in berries, peanuts, grapes, red wine and also in numerous anthelmintic plants, has attracted wide interest because of its diverse pharmacological characteristics. Recently, anthelmintic potential of the compound is established. The present study was carried out to understand the possible mechanism of action of resveratrol on poultry tapeworm Raillietina echinobothrida. Resveratrol showed excellent cestocidal activity in a dose dependent manner as revealed through 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay. The progressive ultrastructural alterations followed by complete disruption of nuclear membrane, chromosomal condensation and in situ DNA fragmentation confirm the occurrence of apoptosis like cell death. Increased pro-apoptotic caspase activity and significant decreases in mitochondrial membrane potential in R. echinobothrida exposed to resveratrol confirm the involvement of mitochondria in the process of apoptosis. Copyright © 2015 Elsevier Ltd. All rights reserved.
    Full-text · Article · Jun 2015 · Research in Veterinary Science
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    • "Benzimidazole is a privileged structure in antiparasitic molecules [17]; particularly, in a compound prepared in our group, 5,6-dicloro-2-(trifluoromethyl)- 1H-benzimidazole, denoted in this work as G2 [18]. Nitrobenzene, anisole and phenol groups are present in several anti-parasitic drugs [19] [20]. With the aim of exploring PTR1 binding site surfaces of the protein, we employed docking studies using TAQ as ligand and attempted to reproduce this ligand is in the previously reported crystal structure [12]. "
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    ABSTRACT: A series of quinazoline-2,4,6-triamine were synthesized and evaluated in vitro against Leishmania mexicana. Among them, N6-(ferrocenmethyl)quinazolin-2,4,6-triamine (H2) showed activity on promastigotes and intracellular amastigotes, as well as low cytotoxicity in mammalian cells. Docking and electrochemical studies showed the importance of both the ferrocene and the heterocyclic nucleus to the observed activity. H2 is readily oxidized electrochemically, indicating that the mechanism of action probably involves redox reactions.
    Full-text · Article · Mar 2015 · European Journal of Medicinal Chemistry
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    • "Stilbene-based compounds are widely represented in nature (Shen et al., 2009), and have become of particular interest to chemists and biologists because of their wide range of biological effects including chemopreventive, antitumor, antioxidant, antimicrobial, anti-inflammatory and antihistaminic activities (Hart, 1981; Fremont, 2000; Young and Chaplin, 2004). Recently, several natural and synthetic stilbenoids have been studied for their leishmanicidal properties (del Rey et al., 1999; del Olmo et al., 2001; Getti et al., 2006), and some of them, including resveratrol (trans-3,4 0 ,5-tri- hydroxystilbene) (Kedzierski et al., 2007) and piceatannol (trans- 3,3 0 ,4 0 ,5-tetrahydroxystilbene) (Duarte et al., 2008), have shown anti-leishmanial activity in vitro. "
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