DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Chemical characterization and anti-inflammatory assessment of the hydroethanolic extract of Fridericia chica.(2020) Takenaka, Isabella Kuniko Tavares Magalhães; Amorim, Juliana Mendes; Barros, Patrícia Aparecida Vieira de; Brandão, Geraldo Célio; Contarini, Sara Moreira Lopes; Melo, Éricka Lorenna de Sales Souza e; Leite, Camila Megale Almeida; Martins, Flaviano dos Santos; Cardoso, Valbert Nascimento; Castilho, Rachel Oliveira; Diniz, Simone Odília Antunes FernandesFridericia chica (Bonpl.) L.G. Lohmann, Bignoniaceae, is an Amazonian species known as “pariri” or “crajiru” that is included in the Brazilian National List of Medicinal Plants of Interest to the Unified Health System (Renisus). This herbal remedy is traditionally used as an infusion to treat diarrhea, anemia, inflammation, symptoms of mucositis, and frequent complications of chemotherapy. This study aimed to characterize the chemical profile of the hydroethanolic extract of F. chica and to assess its intestinal anti-inflammatory activity. The chemical profile of the leaves was determined by ultra-performance liquid chromatog raphy coupled to mass spectrometry, and its potential anti-inflammatory activity in the gut was evaluated in mucositis induced by 5-fluorouracil. Three novel compounds from this the species were identified 6,7,3′,4′-tetrahydroxy-5-methoxyflavilium-O-glu curonide, scutellarein-O-glucuronide, and 5-methyl-scutellarein-O-glucuronide, as well as flavones and anthocyanidins that have been previously described. Mice received the hydroethanolic extract (300 mg/kg) for 9 days, and no signs of toxicity were observed. After 72 h of 5-fluorouracil administration, intestinal permeability, bacterial translocation, myeloperoxidase activity, eosinophil peroxidase activity, and histological analyses were performed. Treatment with the analyzed extract was beneficial, as it normalized intestinal permeability, bacterial translocation, myeloperoxidase activity/eosinophil peroxidase and preserved intestinal epithelium architecture. This study provides new insights into the chemical composition and biological activity of the polar extracts from “pariri”, an important Amazonian crude medicinal drug.Item Variation in susceptibility to benznidazole in isolates derived from Trypanosoma cruzi parental strains.(2001) Veloso, Vanja Maria; Toledo, Max Jean de Ornelas; Lana, Marta de; Chiari, Egler; Tafuri, Washington Luiz; Bahia, Maria TerezinhaIn this work, the susceptibility to benznidazole of two parental Trypanosoma cruzi strains, Colombian and Berenice-78, was compared to isolates obtained from dogs infected with these strains for several years. In order to evaluate the susceptibility to benznidazole two groups of mice were infected with one of five distinct populations isolated from dogs as well as the two parental strains of T. cruzi. The first group was treated with benznidazole during the acute phase and the second remained untreated controls. The animals were considered cured when parasitological and serological tests remained persistently negative. Mice infected with the Colombian strain and its isolates Colombian (A and B) did not cure after treatment. On the other hand, all animals infected with Berenice-78 were cured by benznidazole treatment. However, 100%, 50% and 70% of cure rates were observed in animals infected with the isolates Berenice-78 B, C and D, respectively. No significant differences were observed in serological profile of infected control groups, with all animals presenting high antibody levels. However, the ELISA test showed differences in serological patterns between mice inoculated with the different T. cruzi isolates and treated with benznidazole. This variability was dependent on the T. cruzi population used and seemed to be associated with the level of resistance to benznidazole.Item An alternative in vitro drug screening test using Leishmania amazonensis transfected with red fluorescent protein.(2013) Rocha, Marcele Neves; Corrêa, Célia Maria; Melo, Maria Norma; Beverley, Stephen M.; Martins Filho, Olindo Assis; Madureira, Ana Paula; Soares, Rodrigo Pedro PintoFluorescent and colorimetric reporter genes are valuable tools for drug screening models, since microscopy islabor intensive and subject to observer variation. In this work, we propose afluorimetric method for drugscreening using redfluorescent parasites. FluorescentLeishmania amazonensiswere developed aftertransfection with integration plasmids containing either red (RFP) or greenfluorescent protein (GFP)genes. After transfection, wild-type (LaWT) and transfected (LaGFP and LaRFP) parasites were subjected toflow cytometry, macrophage infection, and tests of susceptibility to current antileishmanial agents andpropranolol derivatives previously shown to be active againstTrypanosoma cruzi. Flow cytometry analysisdiscriminated LaWT from LaRFP and LaGFP parasites, without affecting cell size or granulosity. Withmicroscopy, transfection with antibiotic resistant genes was not shown to affect macrophage infectivity andsusceptibility to amphotericin B and propranolol derivatives. Retention offluorescence remained in theintracellular amastigotes in both LaGFP and LaRFP transfectants. However, detection of intracellular RFPparasites was only achieved in thefluorimeter. Murine BALB/c macrophages were infected with LaRFPparasites, exposed to standard (meglumine antimoniate, amphotericin B, Miltefosine, and allopurinol) andtested molecules. Although it was possible to determine IC50values for 4 propranolol derivatives (1, 2b, 3, and4b), all compounds were considered inactive. This study is thefirst to develop afluorimetric drug screeningtest forL. amazonensisRFP. Thefluorimetric test was comparable to microscopy with the advantage of beingfaster and not requiring manual counting.Item Trypanosoma cruzi : induction of benznidazole resistance in vivo and its modulation by in vitro culturing and mice infection.(2008) Santos, Fabiane Matos dos; Caldas, Sérgio; Cáu, Stêfany Bruno de Assis; Crepalde, Geovam Pereira; Lana, Marta de; Coelho, George Luiz Lins Machado; Veloso, Vanja Maria; Bahia, Maria TerezinhaThrough a continuous in vivo drug pressure protocol, using mice as experimental model, we induced benznidazole resistance in Trypanosoma cruzi stocks. Full resistance was obtained for four out of five T. cruzi stocks analyzed. However, the number of benznidazole doses (40–180), as well as the time (4–18 months) necessary to induce resistance varied among the different T. cruzi stocks. The resistance phenotype remained stable after T. cruzi stocks has been maintained by 12 passages in mice (six months) and in acellular culture for the same time. However, the maintenance of resistant parasite for 12 months in acellular culture induces a reduction in its level of benznidazole resistance, while no alteration was detected in parasite maintained for the same time in mice. The data showed the stability of the resistance acquired by drug pressure, but suggest the possibility of reversible changes in the resistance levels after maintenance for long time in acellular culture.Item Trypanosoma cruzi : acute and long-term infection in the vertebrate host can modify the response to benznidazole.(2008) Caldas, Sérgio; Santos, Fabiane Matos dos; Lana, Marta de; Diniz, Lívia de Figueiredo; Coelho, George Luiz Lins Machado; Veloso, Vanja Maria; Bahia, Maria TerezinhaWe analyzed the influence of Trypanosoma cruzi maintenance in different hosts (dog and mouse) on its susceptibility to benznidazole treatment. Five T. cruzi stocks were isolated from dogs inoculated with Be-62 or Be-78 strain (both sensitive to benznidazole) 2–10 years ago, and the benznidazole sensitivity was then determined using the mouse as experimental model. The different T. cruzi stocks obtained from long-term infected dogs showed 50–90% drug resistance right after isolation. However, maintenance of these T. cruzi stocks in mice, by successive blood passages (2.5 years), led to either a decrease or stability of the drug resistance pattern and an increase in parasite virulence. We also demonstrated the effectiveness of the induction of parasitemia reactivation by cyclophosphamide immunosuppression in the evaluation of the response to the specific drug treatment.