Potent Schistosomicidal Constituents from Garcinia brasiliensis

Aline Pereira Castro; Ana Carolina Alves de Mattos; Neusa Araújo Pereira; Naira Ferreira Anchieta; Matheus Siqueira Silva; Danielle Ferreira Dias; Claudinei Alves Silva; Giulliano Vilela Barros; Raquel Lopes Martins Souza; Marcelo Henrique Dos Santos; Marcos José Marques

doi:10.1055/s-0035-1545927

Planta Medica, Inhaltsverzeichnis

Planta Med 2015; 81(09): 733-741
DOI: 10.1055/s-0035-1545927

Biological and Pharmacological Activity

Original Papers

Georg Thieme Verlag KG Stuttgart · New York

Potent Schistosomicidal Constituents from Garcinia brasiliensis

Aline Pereira Castro

¹Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

³Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Ana Carolina Alves de Mattos

²Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil

,

Neusa Araújo Pereira

²Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil

,

Naira Ferreira Anchieta

³Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Matheus Siqueira Silva

¹Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Danielle Ferreira Dias

¹Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Claudinei Alves Silva

¹Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Giulliano Vilela Barros

³Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Raquel Lopes Martins Souza

³Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

,

Marcelo Henrique Dos Santos

⁴Departament of Chemistry, Federal University of Viçosa, Viçosa-MG, Brazil

,

Marcos José Marques

³Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil

› Institutsangaben

Abstract

Praziquantel is the drug of choice for the treatment of schistosomiasis. However, several strains of Schistosoma mansoni are resistant to praziquantel, making it necessary to discover new drugs that might be used for its treatment. With this in mind, the properties of a schistosomicidal ethanolic extract of Garcinia brasiliensis Mart. epicarp, the fractions obtained by partitioning this extract, including the hexane fractions, ethyl acetate fraction, and the aqueous fraction, and the isolated compounds 7-epiclusianone, a major component from these fractions, and fukugetin were tested in vitro on adult worms of S. mansoni. Mortality, damage to membranes, and excretory system activity were observed at 100.0, 50.0, 75.0, and 14.0 µg/mL for the ethanolic extract of G. brasiliensis Mart. epicarp, its hexane fractions, the ethyl acetate fraction, and 7-epiclusianone, respectively. For 7-epiclusianone, these data were confirmed by fluorescent probe Hoechst 33 258 and resorufin. Additionally, the biocidal effect of 7-epiclusianone was even higher than the hexane fractions. Moreover, an inhibitory effect of 7-epiclusianone on the egg laying of female adult S. mansoni worms was observed in cercariae and schistossomula. Thus, 7-epiclusianone is a promising schistosomicidal compound; however, more studies are needed to elucidate its mechanism of toxicity and to evaluate the in vivo activity of this compound.

Key words

Clusiaceae - Garcinia brasiliensis - 7-epiclusianone - fukugetin - Schistosoma mansoni - Schistosomiasis

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Referenzen

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