Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni
2015
Authors
Guimaraes, Maria A.de Oliveira, Rosimeire N.
Veras, Leiz M. C.
Lima, David F.
Campelo, Yuri D. M.
Campos, Stefano Augusto
Kuckelhaus, Selma A. S.
Pinto, Pedro L. S.
Eaton, Peter
Mafud, Ana C.
Mascarenhas, Yvonne P.
Allegretti, Silmara M.
de Moraes, Josue
Lolić, Aleksandar
Verbić, Tatjana
Leite, Jose Roberto S. A.
Article (Published version)
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Schistosomiasis is a serious disease currently estimated to affect more that 207 million people worldwide. Due to the intensive use of praziquantel, there is increasing concern about the development of drug-resistant strains. Therefore, it is necessary to search for and investigate new potential schistosomicidal compounds. This work reports the in vivo effect of the alkaloid epiisopiloturine (EPI) against adults and juvenile worms of Schistosoma mansoni. EPI was first purified its thermal behavior and theoretical solubility parameters charaterised. In the experiment, mice were treated with EPI over the 21 days post-infection with the doses of 40 and 200 mg/kg, and 45 days post-infection with single doses of 40, 100 and 300 mg/kg. The treatment with EPI at 40 mg/kg was more effective in adult worms when compared with doses of 100 and 300 mg/kg. The treatment with 40 mg/kg in adult worms reduced parasite burden significantly, lead to reduction in hepatosplenomegaly, reduced the egg burde...n in faeces, and decreased granuloma diameter. Scanning electron microscopy revealed morphological changes to the parasite tegument after treatment, including the loss of important features. Additionally, the in vivo treatment against juvenile with 40 mg/kg showed a reduction of the total worm burden of 50.2%. Histopathological studies were performed on liver, spleen, lung, kidney and brain and EPI was shown to have a DL50 of 8000 mg/kg. Therefore EPI shows potential to be used in schistosomiasis treatment. This is the first time that schistosomicidal in vivo activity of EPI has been reported.
Source:
PLoS Neglected Tropical Diseases, 2015, 9, 3Publisher:
- Public Library Science, San Francisco
Funding / projects:
- The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-MESTD-Basic Research (BR or ON)-172008)
- Faculdade de Ciencias de Guarulhos FACIG/UNIESP
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico, Brazilian Ministry of Science and Technology (MCTI/CNPq/MS-SCTIE) [40/2012, 404134/2012-2]
- Fundacao para a Ciencia e a Tecnologia (FCT) [PEst-C/EQB/LA0006/2011, PTDC/CTM-NAN/109877/2009]
- Fundacao e Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [2014/02282-6]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico, Brazilian Ministry of Science and Technology (CNPq/FCT) [490585/2010-8]
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Supeior, Brazilian Ministry of Education (CAPES) [705/2009]
DOI: 10.1371/journal.pntd.0003656
ISSN: 1935-2735
PubMed: 25816129
WoS: 000352199400102
Scopus: 2-s2.0-84928820292
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Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Guimaraes, Maria A. AU - de Oliveira, Rosimeire N. AU - Veras, Leiz M. C. AU - Lima, David F. AU - Campelo, Yuri D. M. AU - Campos, Stefano Augusto AU - Kuckelhaus, Selma A. S. AU - Pinto, Pedro L. S. AU - Eaton, Peter AU - Mafud, Ana C. AU - Mascarenhas, Yvonne P. AU - Allegretti, Silmara M. AU - de Moraes, Josue AU - Lolić, Aleksandar AU - Verbić, Tatjana AU - Leite, Jose Roberto S. A. PY - 2015 UR - https://cherry.chem.bg.ac.rs/handle/123456789/1688 AB - Schistosomiasis is a serious disease currently estimated to affect more that 207 million people worldwide. Due to the intensive use of praziquantel, there is increasing concern about the development of drug-resistant strains. Therefore, it is necessary to search for and investigate new potential schistosomicidal compounds. This work reports the in vivo effect of the alkaloid epiisopiloturine (EPI) against adults and juvenile worms of Schistosoma mansoni. EPI was first purified its thermal behavior and theoretical solubility parameters charaterised. In the experiment, mice were treated with EPI over the 21 days post-infection with the doses of 40 and 200 mg/kg, and 45 days post-infection with single doses of 40, 100 and 300 mg/kg. The treatment with EPI at 40 mg/kg was more effective in adult worms when compared with doses of 100 and 300 mg/kg. The treatment with 40 mg/kg in adult worms reduced parasite burden significantly, lead to reduction in hepatosplenomegaly, reduced the egg burden in faeces, and decreased granuloma diameter. Scanning electron microscopy revealed morphological changes to the parasite tegument after treatment, including the loss of important features. Additionally, the in vivo treatment against juvenile with 40 mg/kg showed a reduction of the total worm burden of 50.2%. Histopathological studies were performed on liver, spleen, lung, kidney and brain and EPI was shown to have a DL50 of 8000 mg/kg. Therefore EPI shows potential to be used in schistosomiasis treatment. This is the first time that schistosomicidal in vivo activity of EPI has been reported. PB - Public Library Science, San Francisco T2 - PLoS Neglected Tropical Diseases T1 - Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni VL - 9 IS - 3 DO - 10.1371/journal.pntd.0003656 ER -
@article{ author = "Guimaraes, Maria A. and de Oliveira, Rosimeire N. and Veras, Leiz M. C. and Lima, David F. and Campelo, Yuri D. M. and Campos, Stefano Augusto and Kuckelhaus, Selma A. S. and Pinto, Pedro L. S. and Eaton, Peter and Mafud, Ana C. and Mascarenhas, Yvonne P. and Allegretti, Silmara M. and de Moraes, Josue and Lolić, Aleksandar and Verbić, Tatjana and Leite, Jose Roberto S. A.", year = "2015", abstract = "Schistosomiasis is a serious disease currently estimated to affect more that 207 million people worldwide. Due to the intensive use of praziquantel, there is increasing concern about the development of drug-resistant strains. Therefore, it is necessary to search for and investigate new potential schistosomicidal compounds. This work reports the in vivo effect of the alkaloid epiisopiloturine (EPI) against adults and juvenile worms of Schistosoma mansoni. EPI was first purified its thermal behavior and theoretical solubility parameters charaterised. In the experiment, mice were treated with EPI over the 21 days post-infection with the doses of 40 and 200 mg/kg, and 45 days post-infection with single doses of 40, 100 and 300 mg/kg. The treatment with EPI at 40 mg/kg was more effective in adult worms when compared with doses of 100 and 300 mg/kg. The treatment with 40 mg/kg in adult worms reduced parasite burden significantly, lead to reduction in hepatosplenomegaly, reduced the egg burden in faeces, and decreased granuloma diameter. Scanning electron microscopy revealed morphological changes to the parasite tegument after treatment, including the loss of important features. Additionally, the in vivo treatment against juvenile with 40 mg/kg showed a reduction of the total worm burden of 50.2%. Histopathological studies were performed on liver, spleen, lung, kidney and brain and EPI was shown to have a DL50 of 8000 mg/kg. Therefore EPI shows potential to be used in schistosomiasis treatment. This is the first time that schistosomicidal in vivo activity of EPI has been reported.", publisher = "Public Library Science, San Francisco", journal = "PLoS Neglected Tropical Diseases", title = "Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni", volume = "9", number = "3", doi = "10.1371/journal.pntd.0003656" }
Guimaraes, M. A., de Oliveira, R. N., Veras, L. M. C., Lima, D. F., Campelo, Y. D. M., Campos, S. A., Kuckelhaus, S. A. S., Pinto, P. L. S., Eaton, P., Mafud, A. C., Mascarenhas, Y. P., Allegretti, S. M., de Moraes, J., Lolić, A., Verbić, T.,& Leite, J. R. S. A.. (2015). Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni. in PLoS Neglected Tropical Diseases Public Library Science, San Francisco., 9(3). https://doi.org/10.1371/journal.pntd.0003656
Guimaraes MA, de Oliveira RN, Veras LMC, Lima DF, Campelo YDM, Campos SA, Kuckelhaus SAS, Pinto PLS, Eaton P, Mafud AC, Mascarenhas YP, Allegretti SM, de Moraes J, Lolić A, Verbić T, Leite JRSA. Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni. in PLoS Neglected Tropical Diseases. 2015;9(3). doi:10.1371/journal.pntd.0003656 .
Guimaraes, Maria A., de Oliveira, Rosimeire N., Veras, Leiz M. C., Lima, David F., Campelo, Yuri D. M., Campos, Stefano Augusto, Kuckelhaus, Selma A. S., Pinto, Pedro L. S., Eaton, Peter, Mafud, Ana C., Mascarenhas, Yvonne P., Allegretti, Silmara M., de Moraes, Josue, Lolić, Aleksandar, Verbić, Tatjana, Leite, Jose Roberto S. A., "Anthelmintic Activity In Vivo of Epiisopiloturine against Juvenile and Adult Worms of Schistosoma mansoni" in PLoS Neglected Tropical Diseases, 9, no. 3 (2015), https://doi.org/10.1371/journal.pntd.0003656 . .