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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
1   Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
3   Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Ana Carolina Alves de Mattos
2   Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil
,
Neusa Araújo Pereira
2   Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil
,
Naira Ferreira Anchieta
3   Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Matheus Siqueira Silva
1   Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Danielle Ferreira Dias
1   Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Claudinei Alves Silva
1   Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Giulliano Vilela Barros
3   Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Raquel Lopes Martins Souza
3   Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
,
Marcelo Henrique Dos Santos
4   Departament of Chemistry, Federal University of Viçosa, Viçosa-MG, Brazil
,
Marcos José Marques
3   Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil
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Publikationsverlauf

received 16. Februar 2015
revised 16. Februar 2015

accepted 14. März 2015

Publikationsdatum:
23. April 2015 (online)

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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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