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Universidade Do Vale Do Itajaí UNIVERSIDADE DO VALE DO ITAJAÍ TALITA ELISA BERTÉ ESTUDO DA ATIVIDADE ANTICOLINESTERÁSICA DOS COMPOSTOS TARAXEROL E ÁCIDO URSÓLICO: IMPLICAÇÕES SOBRE O PROCESSO DE MEMÓRIA Itajaí - 2009 UNIVERSIDADE DO VALE DO ITAJAÍ PROGRAMA DE MESTRADO ACADÊMICO EM CIÊNCIAS FARMACÊUTICAS ÁREA DE CONCENTRAÇÃO EM PRODUTOS NATURAIS E SUBSTÂNCIAS SINTÉTICAS BIOATIVAS TALITA ELISA BERTÉ ESTUDO DA ATIVIDADE ANTICOLINESTERÁSICA DOS COMPOSTOS TARAXEROL E ÁCIDO URSÓLICO: IMPLICAÇÕES SOBRE O PROCESSO DE MEMÓRIA Dissertação apresentada à Universidade do Vale do Itajaí como parte dos requisitos para a obtenção do Título de Mestre em Ciências Farmacêuticas. Orientadora: Dra. Márcia Maria de Souza Co-orientadora: Dra. Cristiani Bürger Itajaí, Maio de 2009. 2 ESTUDO DA ATIVIDADE ANTICOLINESTERÁSICA DOS COMPOSTOS TARAXEROL E ÁCIDO URSÓLICO: IMPLICAÇÕES SOBRE O PROCESSO DE MEMÓRIA Talita Elisa Berté ‘Esta dissertação foi julgada adequada para obtenção do título de Mestre em Ciências Farmacêuticas, Área de concentração Produtos Naturais e Substâncias Bioativas e aprovada em sua forma final pelo Programa de Mestrado em Ciências Farmacêuticas da Universidade do Vale do Itajaí.’ Márcia Maria de Souza, Doutora Orientador Tania Mari Bellé Bresolin, Doutora Coordenador do Programa Mestrado em Ciências Farmacêuticas Apresentado perante a Banca Examinadora composta pelos Professores: Doutora Márcia Maria de Souza (Univali) Presidente Doutora C ristiani Bürger (Univali) Co-orientador Doutora Nara Lins Meira Quintão (Univali) Membro Doutora Ana Lúcia Severo Rodrigues (UFSC) Membro externo Itajaí (SC), 14 maio 2009 3 Dedico este trabalho aos meus pais os quais são meu alicerce. À Larissa minha irmã querida e também ao meu grande amor Eduardo. 4 AGRADECIMENTOS Agradeço a Deus, por estar sempre presente e nas horas mais difíceis ter me ajudado a escolher o caminho certo. Agradeço aos meus familiares, em especial minha mãe Marizete, meu pai Silvino e minha irmã Larissa por serem a base de meus princípios e de minha formação. Um agradecimento especial para o meu grande amor e companheiro Eduardo pelo apoio, carinho e compreensão. Às orientadoras, Márcia Maria de Souza e Cristiani Bürger, agradeço pelo apoio, incentivo e pela orientação científica. Às professoras colaboradoras Christiane Meyre da Silva Bittencourt e Ângela Malheiros, pela contribuição na orientação dos ensaios fitoquimicos do presente trabalho. Agradeço a professora Nara Lins Meira Quintão pelo apoio e incentivo, e acompanhamento do trabalho desde a fase de projeto. Às amigas Maggie, Carla, Ticiana, Gislaine e Rosana pelo apoio, auxílio e amizade. Agradeço também aos alunos da graduaçãoem Farmácia: Bruna, Fernanda, Patrícia,Taíse, Mauricio e Diogo. Finalmente agradeço em especial a Profa. Dra. Daniela Marti Barros e Dra. Beatriz Moleta e suas equipes os quais foram responsaveis pela analise histológica e por parte da análise estatística dos dados. 5 “A MENTE QUE SE ABRE A UMA NOVA ID ÉIA J AMAIS VOLTARÁ AO TAMANH O NORMAL” (Einstein) 6 TALITA ELISA BERTÉ Maio/2009 Orientador: Márcia Maria de Souza, Doutora Co-orientadora: Cristiani Bürger, Doutora Área de concentração: Produtos naturais e substâncias sintéticas bioativas Número de página: 98 Nos últimos anos os compostos obtidos de plantas medicinais têm constituído alvos terapêuticos importantes para o tratamento de várias patologias neuropsiquiátricas e/ou neurodegenerativas. Os fitoconstituintes com atividade anticolinesterásica que possuem efeitos facilitatórios nos processos de memória atualmente estão sendo muito estudados. Este trabalho teve como objetivo isolar o composto taraxerol (TRX) da planta Eugenia umbelliflora e testá-lo, juntamente com o ácido ursólico (AU), em ensaios bioautográficos, ensaios in vitro e in vivo, verificando seus efeitos sobre atividade da enzima acetilcolinesterase (AChE) e sobre os processos de memória de longa duração (MLD) através do modelo de esquiva inibitória. A atividade anticolinesterásica do TRX e AU foi avaliada em testes bioautográficos e em seguida por teste in vitro com encéfalo e hipocampo de ratos Wistar através do método de Ellman e colaboradores (1961). A partir dos resultados in vitro, estes compostos foram avaliados in vivo infundidos diretamente no hipocampo de ratos, utilizando-se o teste de esquiva inibitória. Neste experimento, os animais sofreram estereotáxia (A= -4,2, L= ± 3,0, V= - 1,3) para implante de cânula-guia. Decorrido o tempo de recuperação dos animais, os mesmos foram treinados e testados avaliando-se os efeitos dos compostos sobre as etapas da memória (aquisição, consolidação e evocação). Para tanto, os animais foram infundidos (região CA1) com os compostos respectivamente 5 minutos antes do treino, imediatamente após o treino e 5 minutos antes do teste. Durante as sessões de treino os animais eram colocados sobre a plataforma do aparato, cronometrando-se a latência de descida. Após a descida, os animais levavam choques de 0,4 mA. Nas sessões de teste (24 horas após o treino) o mesmo procedimento era feito, desta vez com omissão dos choques. Também foi verificado se, os compostos em estudo produziam efeito reversor da amnésia induzida pela escopolamina (5 µg/sítio) no modelo de esquiva inibitória, sendo a escopolamina injetada diretamente no hipocampo 5 minutos antes da infusão dos compostos. Os resultados bioautográficos confirmaram a atividade anticolinesterásica de ambos os compostos, de 180 à 15 µg para TRX e 180 a 6 µg para o AU. Pelo método de Ellman, o TRX apresentou atividade anticolinesterásica somente no hipocampo nas concentrações de 0,89 e 1,77 µM (20,8 ± 1,99 e 23,9% ± 2.42, respectivamente). O AU produziu efeito inibitório no encéfalo de ratos na concentração de 0,27 µM (14,0% ± 1,76) e em hipocampo nas concentrações de 0,01, 0,08, 0,44 e 0,89 µM (14,84% ± 5,49, 18,3% ± 1,82, 29,94% ± 12,6 e 17,83% ± 3,36). No teste de esquiva inibitória o TRX produziu efeito facilitatório significativo no processo de consolidação da memória, revertendo a amnésia induzida pela escopolamina nos processos de aquisição, consolidação e evocação. O AU promoveu um efeito facilitatório da memória na etapa de consolidação e reverteu a amnésia induzida por escopolamina nas etapas de aquisição e consolidação da memória. PALAVRAS-CHAVE: acetilcolinestese. ácido ursólico. memória. taraxerol. 7 TALITA ELISA BERTÉ Maio/2009 Advisor: Márcia Maria de Souza, Doutora Co-Advisor: Cristiani Bürger, Doutora Concentacion Area: Natural Productos and Bioactive Synthetic Substance Numbers pages: 98 In recent years, compounds obtained from medicinal plants have been constituted important therapeutic targets for the treatment of various neuropsychiatric and/or neurodegenerative pathologies. The phytoconstituent with anticholinesterasic activities that currently possess facilitatory effects in the memory processes are being very studied. This study seeks to isolate the taraxerol compound (TRX) from Eugenia umbelliflora plant and test it, together with ursolic acid (UA), in bioauthographic in vitro and in vivo assays, determining their effects on the acetylcholinesterase enzyme activity (AChE) and on of long-term memory (LTM) process, through the inhibitory avoidance model. The anticholinesterasic activity of TRX and UA was assessed in bioauthographic test and later by in vitro test with encephalon and hippocampus of Wistar rats by the method of Ellman et al. (1961). Based the in vitro results, these compounds were assessed in vivo, infusing them directly in the rats’ hippocampus, using the test of inhibitory avoidance. In this experiment, the animals underwent stereotactic surgery (A= - 4.2, L= ± 3.0, V= - 1.3) for the implantation of guide- cannulas. Once the recovery time of the animals had elapsed, they were trained and tested, assessing the effects of the compounds in the study of memory atages (acquisition, consolidation and retrieval). For this purpose, the animals were injected with the compounds respectively 15 minutes before training, immediately after training and 15 minutes before the test. During the training sessions, the animals were placed on the apparatus platform, and the etep-down latency was timed. Each time this occured, the animals received 0,4mA shocks. In the test sessions (24 hours after training), the same procedure was carried out, but this time omitting the shocks. It was also observed whether the compounds studied produced a escpolamine (5 µg/sítio) induced amnesia reserval effect in the inhibitory avoidance model, with the scopolamine being injected directly in the hippocampus 5 minutes before the infusion of compounds. The bioautographic results confirmed the anticholinesterasic activity of both compounds, from 180 to 15 g for TRX and 180 to 6 g for UA. By the method of Ellman, TRX presented anticholinesterasic activity only in the hippocampus in concentrations of 0.89 and 1.77 M (20,8 ± 1,99 and 23,9% ± 2,42 respectively). UA produced inhibitory effect on rats’ encephalon at concentrations of 0,27 M (14,0% ± 1,76) and in the hippocampus at concentrations the 0,017, 0,08, 0,44 e 0,89 µM (14,84% ± 5,49, 18,3% ± 1,82, 29,94% ± 12,6 e 17,83% ± 3,36 respectively). In the test of inhibitory avoidance, TRX produced significant facilitatory effect in the process of consolidation of memory, reverting amnesia induced by scopolamine in this process, as well as in the processes of acquisition and retrieval. UA promoted a facilitatory effect of memory in the consolidation step and reverted the amnesia induced by scopolamine in the steps of acquisition and consolidation of memory. KEYWORDS: acetylcholinesterase.
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