Determinação da atividade leishmanicida, antiproteolítica e antioxidante de Arrabidaea brachypoda
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Data
2012-12-20
Autores
Pereira, Ivan de Oliveira [UNESP]
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
Infecções causadas por tripanosomatídeos do gênero Leishmania representam um dos maiores problemas de saúde pública mundial, com alta endemicidade, sobretudo em países em desenvolvimento. As substâncias de escolha para o tratamento destas parasitoses, de modo geral, causam notória toxicidade renal e cardíaca, além de induzirem resistência no parasito e muitas vezes apresentarem eficácia insuficiente. As plantas são utilizadas no tratamento e cura de enfermidades desde a antiguidade, quando o homem começou a utilizar a natureza em seu favor. Estas plantas, pela sua riqueza química e farmacológica, têm sido estudadas no intuito de comprovar atividades atribuídas pela crença popular e obtenção de novos compostos ativos. Neste contexto, destaca-se a família Bignoniaceae, típica do Cerrado brasileiro, que compreende mais de cem gêneros, entre eles o gênero Arrabidaea, que é rico em uma considerável diversidade de compostos, porém muito pouco estudado até o momento, especialmente quando se fala da espécie A. brachypoda. Este trabalho visou estudar o extrato das folhas de A. brachypoda e determinar suas atividades leishmanicida, antiproteolítica e antioxidante. Após obtido, por percolação, o extrato hidro-etanólico das folhas de A. brachypoda, este foi fracionado por partição líquido-líquido em hexânico, acetato-etílico, butanólico e aquoso, e analisados por UFLC-MS para determinação das massas moleculares dos principais constituintes de cada fração, em seguida, o extrato bruto e frações foram avaliados quanto a sua atividade leishmanicida in vitro, sua citotoxicidade, e também quanto ao seu potencial inibitório perante proteases obtidas de promastigotas e amastigotas (pool), assim como proteases purificadas (oligopeptidases B e C, Catepsina-L e Cruzaína) e recombinantes...
Infections caused by trypanosomatids of the genus Leishmania represent one of the largest global public health problems, with high endemicity, especially in developing countries. The drugs of choice for the treatment of these parasitic infections generally cause notorious heart and kidney toxicity, and induce resistance in parasite and often have insufficient effectiveness. The plants are used in the treatment and cure of illnesses since antiquity, when the man has begum to use nature in his favor. These plants by their chemical and pharmacological wealth, have been studied in order to prove the activities assigned by the popular belief and obtaining new active compounds. In this context, highlight the family Bignoniaceae, typical of the Brazilian Cerrado, which comprises more than a hundred genera, among them the Arrabidaea genus, which is rich in a considerable diversity of compounds, however very little studied so far, especially when talking of the specie A. brachypoda. This work aimed to study the extract from leaves of A. brachypoda and evaluate its leishmanicidal, antiproteolitic and antioxidant activities. After obtained by maceration, the hidro-etanolic extract from leaves of A. brachypoda, this was fractioned by liquid-liquid partition in hexanic, ethyl-acetate, butanolic and watery, and analyzed by HPLC-MS for molecular weights determination of the main constituents from each fraction, then the crude extract and fractions were evaluated on their leishmanicidal activity in vitro, their cytotoxicity, and also regarding its potential as protease inhibitor obtained from amastigotes and promastigotes (pool), as well as purified proteases (oligopeptidases B and C, Cathepsin-L and Cruzain) and recombinants proteases (rCPB2.8, rCPB3.0 and rH84Y), additionally evaluated the antioxidant activity of... (Complete abstract click electronic access below)
Infections caused by trypanosomatids of the genus Leishmania represent one of the largest global public health problems, with high endemicity, especially in developing countries. The drugs of choice for the treatment of these parasitic infections generally cause notorious heart and kidney toxicity, and induce resistance in parasite and often have insufficient effectiveness. The plants are used in the treatment and cure of illnesses since antiquity, when the man has begum to use nature in his favor. These plants by their chemical and pharmacological wealth, have been studied in order to prove the activities assigned by the popular belief and obtaining new active compounds. In this context, highlight the family Bignoniaceae, typical of the Brazilian Cerrado, which comprises more than a hundred genera, among them the Arrabidaea genus, which is rich in a considerable diversity of compounds, however very little studied so far, especially when talking of the specie A. brachypoda. This work aimed to study the extract from leaves of A. brachypoda and evaluate its leishmanicidal, antiproteolitic and antioxidant activities. After obtained by maceration, the hidro-etanolic extract from leaves of A. brachypoda, this was fractioned by liquid-liquid partition in hexanic, ethyl-acetate, butanolic and watery, and analyzed by HPLC-MS for molecular weights determination of the main constituents from each fraction, then the crude extract and fractions were evaluated on their leishmanicidal activity in vitro, their cytotoxicity, and also regarding its potential as protease inhibitor obtained from amastigotes and promastigotes (pool), as well as purified proteases (oligopeptidases B and C, Cathepsin-L and Cruzain) and recombinants proteases (rCPB2.8, rCPB3.0 and rH84Y), additionally evaluated the antioxidant activity of... (Complete abstract click electronic access below)
Descrição
Palavras-chave
Enzimas proteoliticas, Leishmania, Leishmaniose, Tripanosomatideos, Antioxidantes, Plantas medicinais, Plantas dos cerrados, Espectrometria de massa, Analise cromatografica
Como citar
PEREIRA, Ivan de Oliveira. Determinação da atividade leishmanicida, antiproteolítica e antioxidante de Arrabidaea brachypoda. 2012. 99 f. Tese (doutorado) - Universidade Estadual Paulista, Faculdade de Ciências Farmacêuticas, 2012.