In vivo schistosomicidal activity of 7-epiclusianone and its quantification in the plasma of healthy and Schistosoma mansoni infected mice using UPLC-MS/MS.
Phytomedicine
; 38: 66-73, 2018 Jan 01.
Article
em En
| MEDLINE
| ID: mdl-29425656
ABSTRACT
BACKGROUND:
The tetraprenylated benzophenone 7-epiclusianone (7-epi) is a substance isolated from the fruits of Garcinia brasiliensis and in vitro studies have demonstrated that 7-epi is effective against Schistosoma mansoni adult worms. HYPOTHESIS/PURPOSE:
Here we report the in vivo evaluation of 7-epi and its pharmacokinetic in healthy and Schistosoma mansoni infected mice. STUDY DESIGN ANDMETHODS:
In this work, we assayed the schistosomicidal activity of 7-epi at the dose of 100â¯mg/kg and 300â¯mg/kg body weight/day in S. mansoni experimentally infected mice. Besides, two groups of animals were treated and a detailed analysis of plasma samples was performed by liquid chromatography coupled to mass spectrometry (LC-MS/MS).RESULTS:
The worm burden showed a reduction in the infected mice after treatment with 300â¯mg/kg for five days (p < .05). And we found an increase of AUC0-∞ (20846 vs. 32438â¯ng.h/ml) and a decrease of total apparent clearance (0.006 vs. 0.004â¯l/h/kg) of 7- epi in the infected group compared to the healthy group. Consequently, the half-life increased (1.73 vs. 6.11â¯h) and Cmax was reduced (5427.5 vs. 3321.0â¯ng/ml) in the infected group compared to the healthy group. In addition, histopathological investigations were performed analysing liver samples from healthy and infected mice.CONCLUSION:
The results showed significant schistosomicidal in vivo activity at 300â¯mg/kg. In addition, livers from S. mansoni infected mice showed a greater number of egg granulomas and the changes in the pharmacokinetic parameters in this group could be associated with the pathology of the murine experimental schistosomiasis.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Esquistossomicidas
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Benzofenonas
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Esquistossomose mansoni
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Benzoquinonas
Limite:
Animals
Idioma:
En
Revista:
Phytomedicine
Assunto da revista:
TERAPIAS COMPLEMENTARES
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Brasil