RESUMO
This study proposes an alternative technique to prevent heat degradation induced by classic procedures of bioactive compound extraction, comparing classical maceration/decoction in hot water of polyphenols from Mango (Mangifera indica L.) (MI) with ultrasound-assisted extraction (UAE) in a water solution of ß-cyclodextrin (ß-CD) at room temperature and testing their biological activity on TNFα-induced endothelial dysfunction. Both extracts counteracted TNFα effects on EAhy926 cells, down-modulating interleukin-6, interleukin-8, cyclooxygenase-2 and intracellular adhesion molecule-1, while increasing endothelial nitric oxide synthase levels. ß-CD extract showed higher efficacy in improving endothelial function. These effects were abolished after pre-treatment with the oestrogen receptor inhibitor ICI1182,780. Moreover, the ß-CD extract induced Akt activation and completely abolished the TNFα-induced p38MAPK phosphorylation. UAE and ß-CD encapsulation provide an efficient extraction protocol that increases polyphenol bioavailability. Polyphenols from MI play a protective role on endothelial cells and may be further considered as oestrogen-like molecules with vascular protective properties.
Assuntos
Células Endoteliais/efeitos dos fármacos , Mangifera/química , Casca de Planta/química , Extratos Vegetais/química , Polifenóis/química , Linhagem Celular , Ciclo-Oxigenase 2/metabolismo , Humanos , Molécula 1 de Adesão Intercelular/metabolismo , Interleucina-6/metabolismo , Interleucina-8/metabolismo , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Fosforilação , Transdução de Sinais , Fator de Necrose Tumoral alfa/farmacologia , Ultrassom , beta-Ciclodextrinas , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismoRESUMO
Recently a new series of nitrooxy-acyl derivatives of salicylic acid (SA) was described presenting similar anti-inflammatory activities but reduced or no gastrotoxicity compared to aspirin. In this work, lipophilicity and permeability profiles of SA derivatives were performed to evaluate their ADME properties related to oral or transdermic delivery. All tested compounds showed potential good passive permeation through gastrointestinal track and also through percutaneous barrier which could be a way to avoid the first hepatic pass.