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

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.

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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.
    Research in Veterinary Science 06/2015; 101(2015):220-225. DOI:10.1016/j.rvsc.2015.06.010 · 1.41 Impact Factor
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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.
    European Journal of Medicinal Chemistry 03/2015; 92. DOI:10.1016/j.ejmech.2014.12.051 · 3.45 Impact Factor
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    • "There is therefore increasing interest in the use of natural products in aquaculture to treat or prevent infections. Resveratrol (trans-3,4′,5- trihydroxystilbene; RESV) is a naturally occurring phytoalexin, produced by some plants in response to a parasitic attack or under conditions of stress (Pirola and Fröjdö 2008), that has anti-parasitic properties (Leiro et al. 2004a, b; Kedzierski et al. 2007; Son et al. 2007). The aims of the present study were to compare the anti-ciliate in vitro activity of RESV with that of formalin and hydrogen peroxide and to evaluate the susceptibility of different P. dicentrarchi isolates to these compounds. "
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    ABSTRACT: Philasterides dicentrarchi is a histophagous scuticociliate that causes important losses in aquaculture. Several strains that differ in morphological, genetic and serological characteristics and virulence have been isolated from outbreaks of turbot scuticociliatosis. In the present study, seven isolates of the ciliate were exposed in vitro to formalin, hydrogen peroxide and resveratrol (a phytoalexin produced by plants) in order to evaluate the susceptibility of the isolates to the different compounds. The LD50 values for the three compounds tested varied widely among the isolates. The LD100 values were similar among isolates for formalin (25-30 ppm) and resveratrol (60-70 ppm) but were very different for hydrogen peroxide (25->80 ppm). The results indicate that there are many physiological differences among isolates and even among specimens of the same isolates, which must be taken into account in designing control programmes. The naturally occurring resveratrol may be a good alternative to other compounds for reducing the amounts of viable ciliates in water.
    Parasitology Research 10/2011; 110(4):1573-8. DOI:10.1007/s00436-011-2664-1 · 2.10 Impact Factor
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