Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells

[Display omitted] •Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compou...

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Veröffentlicht in:Toxicology in vitro 2015-06, Vol.29 (4), p.681-687
Hauptverfasser: Silva, Ana P., Silva, Marcos P., Oliveira, Cristiano G., Monteiro, Daniela C., Pinto, Pedro L., Mendonça, Ronaldo Z., Costa Júnior, Joaquim S., Freitas, Rivelilson M., de Moraes, Josué
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container_end_page 687
container_issue 4
container_start_page 681
container_title Toxicology in vitro
container_volume 29
creator Silva, Ana P.
Silva, Marcos P.
Oliveira, Cristiano G.
Monteiro, Daniela C.
Pinto, Pedro L.
Mendonça, Ronaldo Z.
Costa Júnior, Joaquim S.
Freitas, Rivelilson M.
de Moraes, Josué
description [Display omitted] •Garcinielliptone FC is able to kill Schistosoma mansoni adult worms.•Garcinielliptone FC induced morphological changes on the tegument of the worms.•Garcinielliptone FC exhibited no in vitro activity toward Vero cells.•Garcinielliptone FC may be a promising antischistosomal compound. Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent.
doi_str_mv 10.1016/j.tiv.2014.12.014
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Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. 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Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. 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Garcinielliptone FC (GFC) is a natural prenylated benzophenone found in the seeds of Platonia insignis Mart. (Clusiaceae), a native Brazilian plant. It has been chemically characterized and it is known that GFC has several biological activities such as antioxidant and vasorelaxant properties. In this study, we report the in vitro effect of GFC against the blood fluke Schistosoma mansoni, the parasite responsible for schistosomiasis mansoni. The anti-S. mansoni activity and cytotoxicity toward mammalian cells were determined for the compound. GFC⩾6.25μM showed antischistosomal activity and confocal laser scanning microscopy analysis demonstrated several morphological alterations on the tegument of worms, and a correlation between viability and tegumental damage was observed. In addition, at sub-lethal concentrations of GFC (⩽3.125μM), the number of S. mansoni eggs was reduced. More importantly, GFC exhibited no activity toward mammalian cells and, therefore, there is an appreciable selectivity of this compound against the helminths. In conclusion, these findings indicate the potential of GFC as an antiparasitic agent.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>25553916</pmid><doi>10.1016/j.tiv.2014.12.014</doi><tpages>7</tpages></addata></record>
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subjects Animals
Antiparasitic activity
Antiparasitic Agents - pharmacology
Antiparasitic Agents - toxicity
Antischistosomal drug
Cell Survival - drug effects
Cells, Cultured
Cercopithecus aethiops
Clusiaceae
Clusiaceae - chemistry
Confocal laser scanning microscopy
Cytotoxicity
Female
Garcinielliptone FC
Male
Models, Molecular
Motor Activity - drug effects
Reproduction - drug effects
Schistosoma
Schistosoma mansoni
Schistosoma mansoni - drug effects
Schistosomicides - toxicity
Seeds - chemistry
Trematoda
Triterpenes - isolation & purification
Triterpenes - pharmacology
Triterpenes - toxicity
Vero Cells
title Garcinielliptone FC: Antiparasitic activity without cytotoxicity to mammalian cells
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