DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Activity of alkaloids from Aspidosperma nitidum against Leishmania (Leishmania) amazonensis.(2022) Veiga, Andreza do Socorro Silva da; Silveira, Fernando Tobias; Silva, Edilene Oliveira da; Diniz Júnior, José Antônio Picanço; Araújo, Sanderson Corrêa; Campos, Marliane Batista; Marinho, Andrey Moacir do Rosário; Brandão, Geraldo Célio; Vale, Valdicley Vieira; Percário, Sandro; Dolabela, Maria FâniThis study evaluated the morphological changes caused by fractions and subfractions, obtained from barks of Aspidosperna nitidum, against L. (L.) amazonensis promastigotes. The ethanolic extract (EE) obtained through the maceration of trunk barks was subjected to an acid–base partition, resulting the neutral (FN) and the alkaloid (FA) fractions, and fractionation under refux, yielded hexane (FrHEX), dichloromethane (FrDCL), ethyl acetate (FrACoET), and methanol (FrMEOH) fractions. The FA was fractionated and three subfractions (SF5-6, SF8, and SF9) were obtained and analyzed by HPLC–DAD and 1 H NMR. The antipromastigote activity of all samples was evaluated by MTT, after that, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for the active fractions were performed. Chromatographic analyzes suggest the presence of alkaloids in EE, FN, FA, and FrDCL. The fractionation of FA led to the isolation of the indole alkaloid dihydrocorynantheol (SF8 fractions). The SF5-6, dihydrocorynantheol and SF-9 samples were active against promastigotes, while FrDCL was moderately active. The SEM analysis revealed cell rounding and changes in the fagellum of the parasites. In the TEM analysis, the treated promastigotes showed changes in fagellar pocket and kinetoplast, and presence of lipid inclusions. These results suggest that alkaloids isolated from A. nitidum are promising as leishmanicidal.Item Antileishmanial activity of Handroanthus serratifolius (Vahl) S. Grose (Bignoniaceae).(2017) Costa, Erica Vanessa Souza; Brígido, Heliton Patrick Cordovil; Silva, João Victor da Silva e; Ferreira, Marlia Regina Coelho; Brandão, Geraldo Célio; Dolabela, Maria FâniThis study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from Handroanthus serratifolius against Leishmania amazonensis. Furthermore, this activity was related to cytotoxicity, and the selectivity index was determined.The ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. The lapachol was obtained by acid base extraction followed by purification in chromatographic column. The antipromastigote activity and cytotoxicity tests were carried out by the cell viabilitymethod (MTT).Modified THP-1 cells were infected with L. amazonensis promastigotes and treated for 24 h with different concentrations of the extract, fractions, and lapachol. Theethanol extract, dichloromethane, and ethyl acetate fractions were not active against promastigotes (IC50 > 200 𝜇g/mL) or cytotoxic (CC50 > 500 𝜇g/mL), and the selectivity index (SI)was greater than 2.5.The ethyl acetate fractionwas active only in promastigotes; it is not cytotoxic (CC50 > 500 𝜇g/mL, SI > 5).The lapachol was selectively active only against amastigote (IS > 2.5, CC50 > 500 𝜇g/mL). In summary, lapachol and ethyl acetate fraction are promising against amastigote and promastigote forms, respectively.Item Anti-malarial activity and toxicity assessment of Himatanthus articulatus, a plant used to treat malaria in the Brazilian Amazon.(2015) Vale, Valdicley Vieira; Vilhena, Thyago da Costa; Trindade, Rafaela Cabral dos Santos; Ferreira, Marlia Regina Coelho; Percário, Sandro; Soares, Luciana Ferreira; Pereira, Washington Luiz Assunção; Brandão, Geraldo Célio; Oliveira, Alaíde Braga de; Dolabela, Maria Fâni; Vasconcelos, Flávio deBackground: Plasmodium falciparum has become resistant to some of the available drugs. Several plant species are used for the treatment of malaria, such as Himatanthus articulatus in parts of Brazil. The present paper reports the phyto-chemistry, the anti-plasmodial and anti-malarial activity, as well as the toxicity of H. articulatus. Methods: Ethanol and dichloromethane extracts were obtained from the powder of stem barks of H. articulates and later fractionated and analysed. The anti-plasmodial activity was assessed against a chloroquine resistant strain P. falciparum (W2) in vitro, whilst in vivo anti-malarial activity against Plasmodium berghei (ANKA strain) was tested in mice, evaluating the role of oxidative stress (total antioxidant capacity - TEAC; lipid peroxidation – TBARS, and nitrites and nitrates - NN). In addition, cytotoxicity was evaluated using the HepG2 A16 cell-line. The acute oral and sub-chronic toxicity of the ethanol extract were evaluated in both male and female mice. Results: Plumieride was isolated from the ethyl acetate fraction of ethanol extract, Only the dichloromethane extract was active against clone W2. Nevertheless, both extracts reduced parasitaemia in P. berghei-infected mice. Besides, a significant reduction in pulmonary and cerebral levels of NN (nitrites and nitrates) was found, as well as in pulmonary TBARS, indicating a reduced oxidative damage to these organs. The ethanol extract showed low cytotoxicity to HepG2 A16 cells in the concentrations used. No significant changes were observed in the in vivo toxicity studies. Conclusions: The ethanol extract of H. articulatus proved to be promising as anti-malarial medicine and showed low toxicity.