Avaliação da atividade antimicrobiana de extratos de Plinia cauliflora (Mart.) Kausel (Myrtaceae) em sistema nanoestruturado e de forma livre.
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Data
2021-01-27
Autores
Sorrechia, Rodrigo
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Universidade Estadual Paulista (Unesp)
Resumo
Mesmo com o avanço da tecnologia farmacêutica na descoberta de novos compostos ativos e formas de administração, a geração cada vez mais recorrente de linhagens de microrganismos patogênicos resistentes a diversas classes de antibióticos constitui uma preocupação atual para a área de saúde. A pesquisa de novas substâncias constitui um nicho de pesquisa de grande importância para o setor químico-farmacêutico. Nesse sentido, a busca destes compostos na rica flora brasileira tem sido explorada por pesquisadores do mundo todo, baseando-se, sobretudo nos conhecimentos tradicionais regionais para fazer uma triagem das espécies mais promissoras. Plinia cauliflora (Myrtaceae), uma árvore nativa do Brasil e conhecida como jabuticabeira, têm diversas atividades biológicas relatadas no uso doméstico para afecções do trato digestivo e irritações cutâneas. Além disso, a atividade antifúngica de seus extratos já foi comprovada cientificamente contra espécies de Candida. No entanto, os compostos presentes nos extratos de P. cauliflora podem ter sua atividade prejudicada por diversos fatores como variação de pH, temperatura e, principalmente, sua solubilidade. Uma alternativa para contornar esses fatores é a incorporação em sistemas lipídicos nanoestruturados, como as microemulsões. A microemulsão é uma dispersão coloidal entre água e óleo, estruturada por tensoativos, apresentam vantagens na incorporação de agentes terapêuticos, como a proteção contra dissolução, alteração de pH, degradação enzimática e solubilidade podendo ser também utilizadas no desenvolvimento de produtos farmacêuticos. Através de um screening preliminar de atividade antimicrobiana, constatou-se que o extrato hidroalcóolico 70 foi o que apresentou melhores resultados frente às leveduras e fungos dermatófitos, sendo o escolhido para a continuidade dos experimentos. O extrato etanólico foi submetido à partição líquido-líquido dando origem às frações acetato de etila, n-butanol e aquosa. O estudo demonstrou alta atividade antimicrobiana contra Candida glabrata e Candida parapsilosis nas concentrações de 4,88 e 78,12 µg/mL para o extrato etanólico 70 e também atividade antidermatofítica considerável. Tais atividades ainda tiveram incrementos significativos com a incorporação na microemulsão desenvolvida. Além disso, apresentaram boa capacidade antioxidante e não foram tóxicas para o modelo alternativo in vivo de Galleria mellonella.
Even with the advance of pharmaceutical technology in discovery of new active compounds and forms of administration, the increase recurrent generation of strains of pathogenic microorganisms resistant to different classes of antibiotics is a current concern for the health area. The search for new substances is a research fild of great importance for the chemical-pharmaceutical. In this way, the search for these compounds in the rich Brazilian flora has been explored by researchers from all over the world, based mainly on traditional regional knowledge to screening the most promising species. Plinia cauliflora (Myrtaceae), a tree native to Brazil and known as jabuticabeira, has several biological activities reported in domestic use for digestive tract disorders and skin irritations. In addition, the antifungal activity of its extracts has already been scientifically proven against species of Candida. However, the compounds present in the extracts of P. cauliflora can have their activity impaired by several factors such as variation in pH, temperature and, mainly, its solubility. An alternative to these factors is the incorporation in nanostructured lipid systems, such microemulsions. Microemulsion is a colloidal dispersion between water and oil, structured by surfactants, show advantages in the incorporation of therapeutic agents, such as protection against dissolution, pH changes, enzymatic degradation and solubility and can also be used in the development of pharmaceutical products. Through a preliminary screening for antimicrobial activity, it was found that the hydroalcoholic extract 70 presented the best results against the yeast and dermatophyte fungi, being the chosen one for the continuity of the experiments. The ethanolic extract was submitted to liquid-liquid partition giving rise to the ethyl acetate, n-butanol and aqueous fractions. The study demonstrated high antimicrobial activity against Candida glabrata and Candida parapsilosis at concentrations of 4.88 and 78.12 µg / mL for ethanol extract 70 and also considerable antidermatophytic activity. Such activities still had significant increases with the incorporation in the developed microemulsion. In addition, they showed good antioxidant capacity and were not toxic to the alternative in vivo model of Galleria mellonella.
Even with the advance of pharmaceutical technology in discovery of new active compounds and forms of administration, the increase recurrent generation of strains of pathogenic microorganisms resistant to different classes of antibiotics is a current concern for the health area. The search for new substances is a research fild of great importance for the chemical-pharmaceutical. In this way, the search for these compounds in the rich Brazilian flora has been explored by researchers from all over the world, based mainly on traditional regional knowledge to screening the most promising species. Plinia cauliflora (Myrtaceae), a tree native to Brazil and known as jabuticabeira, has several biological activities reported in domestic use for digestive tract disorders and skin irritations. In addition, the antifungal activity of its extracts has already been scientifically proven against species of Candida. However, the compounds present in the extracts of P. cauliflora can have their activity impaired by several factors such as variation in pH, temperature and, mainly, its solubility. An alternative to these factors is the incorporation in nanostructured lipid systems, such microemulsions. Microemulsion is a colloidal dispersion between water and oil, structured by surfactants, show advantages in the incorporation of therapeutic agents, such as protection against dissolution, pH changes, enzymatic degradation and solubility and can also be used in the development of pharmaceutical products. Through a preliminary screening for antimicrobial activity, it was found that the hydroalcoholic extract 70 presented the best results against the yeast and dermatophyte fungi, being the chosen one for the continuity of the experiments. The ethanolic extract was submitted to liquid-liquid partition giving rise to the ethyl acetate, n-butanol and aqueous fractions. The study demonstrated high antimicrobial activity against Candida glabrata and Candida parapsilosis at concentrations of 4.88 and 78.12 µg / mL for ethanol extract 70 and also considerable antidermatophytic activity. Such activities still had significant increases with the incorporation in the developed microemulsion. In addition, they showed good antioxidant capacity and were not toxic to the alternative in vivo model of Galleria mellonella.
Descrição
Palavras-chave
Plinia cauliflora, jabuticabeira, Myrtaceae, atividade antimicrobiana, dermatófitos, Candida spp., sistemas nanoestruturados, microemulsão, antimicrobial activity, dermatophytes, nanostructured system, microemulsion