title: Potent Schistosomicidal Constituents from Garcinia brasiliensis.
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.
authors.affiliation: Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Aline Pereira
authors.initials: AP
authors.lastname: Castro
authors.affiliation: Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil.
authors.forename: Ana Carolina Alves
authors.initials: AC
authors.lastname: de Mattos
authors.affiliation: Laboratory of Schistosomiasis, Institute René Rachou-Fiocruz, Belo Horizonte, Brazil.
authors.forename: Neusa Araújo
authors.initials: NA
authors.lastname: Pereira
authors.affiliation: Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Naira Ferreira
authors.initials: NF
authors.lastname: Anchieta
authors.affiliation: Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Matheus Siqueira
authors.initials: MS
authors.lastname: Silva
authors.affiliation: Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Danielle Ferreira
authors.initials: DF
authors.lastname: Dias
authors.affiliation: Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Claudinei Alves
authors.initials: CA
authors.lastname: Silva
authors.affiliation: Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Giulliano Vilela
authors.initials: GV
authors.lastname: Barros
authors.affiliation: Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Raquel Lopes Martins
authors.initials: RL
authors.lastname: Souza
authors.affiliation: Departament of Chemistry, Federal University of Viçosa, Viçosa-MG, Brazil.
authors.forename: Marcelo Henrique
authors.initials: MH
authors.lastname: Dos Santos
authors.affiliation: Department of Pathology and Parasitology, Laboratory of Parasitology, Institute of Biomedical Sciences, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil.
authors.forename: Marcos José
authors.initials: MJ
authors.lastname: Marques
mesh_terms: D000818:Animals; D001577:Benzophenones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016227:Benzoquinones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D044946:Biflavonoids / Q000494:pharmacology; D005260:Female; D029760:Garcinia / Q000737:chemistry*; D008297:Male; D015394:Molecular Structure; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D012550:Schistosoma mansoni / Q000187:drug effects*; D012552:Schistosomiasis / Q000188:drug therapy*; D012556:Schistosomicides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: C118110:7-epiclusianone; D001577:Benzophenones; D016227:Benzoquinones; D044946:Biflavonoids; D010936:Plant Extracts; D012556:Schistosomicides; C105620:morelloflavone