Author | Castro, Aline Pereira | |
Author | Kawano, Taila | |
Author | Spelta, Lidia Emmanuela Wiazowski | |
Author | Castro, Andreísa Teixeira de | |
Author | Pereira, Neusa Araújo | |
Author | Couto, Flavia Fernanda Bubula | |
Author | Santos, Marcelo Henrique dos | |
Author | Boralli, Vanessa Bergamin | |
Author | Marques, Marcos José | |
Access date | 2018-09-06T16:33:30Z | |
Available date | 2018-09-06T16:33:30Z | |
Document date | 2018 | |
Citation | CASTRO, Aline Pereira et al. 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, v. 38, p. 66-73, 2018. | pt_BR |
ISSN | 0944-7113 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/28591 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | restricted access | pt_BR |
Subject in Portuguese | 7-epiclusianona | pt_BR |
Subject in Portuguese | rato | pt_BR |
Subject in Portuguese | Farmacocinética | pt_BR |
Subject in Portuguese | schistosoma | pt_BR |
Subject in Portuguese | UPLC-MS/MS | pt_BR |
Title | In vivo schistosomicidal activity of 7-epiclusianone and its quantification in the plasma of healthy and Schistosoma mansoni infected mice using UPLC-MS/MS | pt_BR |
Type | Article | pt_BR |
DOI | 10.1016/j.phymed.2017.11.001 | |
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 and methods: In this work, we assayed the schistosomicidal activity of 7-epi at the dose of 100 mg/kg and 300 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 300 mg/kg for five days (p < .05). And we found an increase of AUC0–∞ (20846 vs. 32438 ng.h/ml) and a decrease of total apparent clearance (0.006 vs. 0.004 l/h/kg) of 7- epi in the infected group compared to the healthy group. Consequently, the half-life increased (1.73 vs. 6.11 h) and Cmax was reduced (5427.5 vs. 3321.0 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 300 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. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Instituto de Ciências Biomédicas. Laboratório de Parasitologia. Alfenas, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Departamento de Análises Clínicas e Toxicológicas. Alfenas, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Departamento de Análises Clínicas e Toxicológicas. Alfenas, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Instituto de Ciências Biomédicas. Laboratório de Parasitologia. Alfenas, MG, Brazil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Rene Rachou. Belo Horizonte, MG, Brazil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Rene Rachou. Belo Horizonte, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Viçosa. Departamento de Química. Viçosa, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Departamento de Análises Clínicas e Toxicológicas. Alfenas, MG, Brazil. | pt_BR |
Affilliation | Universidade Federal de Alfenas. Instituto de Ciências Biomédicas. Laboratório de Parasitologia. Alfenas, MG, Brazil. | pt_BR |
Subject | 7-epiclusianone | pt_BR |
Subject | Mice | pt_BR |
Subject | Pharmacokinetics | pt_BR |
Subject | Schistosomiasis | pt_BR |
Subject | UPLC-MS/MS | pt_BR |
Embargo date | 2025-01-01 | |