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| Ferreira,Daiane Dias; Mesquita,Juliana Tonini; Silva,Thais Alves da Costa; Romanelli,Maiara Maria; Batista,Denise da Gama Jaen; Silva,Cristiane França da; Gama,Aline Nefertiti Silva da; Neves,Bruno Junior; Melo-Filho,Cleber Camilo; Soeiro,Maria de Nazare Correia; Andrade,Carolina Horta; Tempone,Andre Gustavo. |
| Abstract Background: Drug repurposing has been an interesting and cost-effective approach, especially for neglected diseases, such as Chagas disease. Methods: In this work, we studied the activity of the antidepressant drug sertraline against Trypanosoma cruzi trypomastigotes and intracellular amastigotes of the Y and Tulahuen strains, and investigated its action mode using cell biology and in silico approaches. Results: Sertraline demonstrated in vitro efficacy against intracellular amastigotes of both T. cruzi strains inside different host cells, including cardiomyocytes, with IC50 values between 1 to 10 μM, and activity against bloodstream trypomastigotes, with IC50 of 14 μM. Considering the mammalian cytotoxicity, the drug resulted in a selectivity... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Trypanosoma cruzi; Drug; Treatment; Sertraline; Drug repurposing; Drug repositioning. |
| Ano: 2018 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992018000100321 |
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| Alexandre,Tatiana Rodrigues; Lima,Marta Lopes; Galuppo,Mariana Kolos; Mesquita,Juliana Tonini; Nascimento,Matilia Ana do; Santos,Augusto Leonardo dos; Sartorelli,Patricia; Pimenta,Daniel Carvalho; Tempone,Andre Gustavo. |
| Abstract Background Major drawbacks of the available treatment against Chagas disease (American trypanosomiasis) include its toxicity and therapeutic inefficiency in the chronic phase of the infection, which makes it a concern among neglected diseases. Therefore, the discovery of alternative drugs for treating chronic Chagas disease requires immediate action. In this work, we evaluated the mushroom Pleurotus salmoneostramineus in the search for potential antiparasitic compounds. Methods Fruit bodies of the basidiomycete Pleurotus salmoneostramineus were triturated and submitted to organic solvent extraction. After liquid-liquid partition of the crude extract, three fractions were obtained and the bioguided fractionation study was conducted to isolate... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Pleurotus salmoneostramineus; Ergosterol; Trypanosoma cruzi; Mechanism of action. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992017000100313 |
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| Pereira,Andreia Vieira; Barros,Gustavo de; Pinto,Erika Gracielle; Tempone,Andre Gustavo; Orsi,Ricardo de Oliveira; Santos,Lucilene Delazari dos; Calvi,Sueli; Ferreira Jr,Rui Seabra; Pimenta,Daniel Carvalho; Barraviera,Benedito. |
| Abstract Background Apis mellifera venom, which has already been recommended as an alternative anti-inflammatory treatment, may be also considered an important source of candidate molecules for biotechnological and biomedical uses, such as the treatment of parasitic diseases. Methods Africanized honeybee venom from Apis mellifera was fractionated by RP-C18-HPLC and the obtained melittin was incubated with promastigotes and intracellular amastigotes of Leishmania (L.) infantum. Cytotoxicity to mice peritoneal macrophages was evaluated through mitochondrial oxidative activity. The production of anti- and pro-inflammatory cytokines, NO and H2O2 by macrophages was determined. Results Promastigotes and intracellular amastigotes were susceptible to melittin... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Melittin; Apis mellifera; Leishmania; Leishmaniasis; Peptides; Toxins; Antiparasitic; Cytokines. |
| Ano: 2016 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1678-91992016000100301 |
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