Background: Euterpe oleracea Martius, popularly known as açaí, is a fruit rich in α-tocopherols, fibers, lipids, mineral ions and polyphenols. It is believed that the high content of polyphenols, specially flavonoids, provides several health-promoting effects to the açaí fruit, including anti-inflammatory, immunomodulatory, antinociceptive and antioxidant properties. Most of flavonoids are antioxidant molecules from vegetable origin that act as a trap for free radicals, reacting and neutralizing them, thus offering perspectives in preventing oxidative damage. Objective: In this study we aim to perform an in silico evaluation of flavonoids present in the pulp and in the oil of Euterpe oleracea Martius, and their potential to represent antioxidant agents. Methods: First, we selected 16 flavonoid molecules present in Euterpe oleracea Martius pulp and oil, and then their physicochemical properties were analysed with respect to the Lipinski’s rule of five. Moreover, we evaluated their pharmacokinetic properties using the QikProp module of the Schrödinger software and their toxicity profile using the DEREK software. Docking simulations in the GOLD 4.1 software and calculation of the pharmacophore hypothesis of molecules were also performed. Results: Flavonoids present in the açaí pulp, catechin, epicatechin, luteolin, chrisoeriol, taxifolin, apigenin, dihydrokaempferol, isovitexin and vitexin presented good oral bioavailability. Regarding pharmacokinetic properties, the compounds catechin, epicatechin, isovitexin, luteolin, chrisoeriol, taxifolin and isorhamnetina rutinoside presented the best results and high human oral absorption. In the prediction of toxicological properties, compounds isorhamnetin rutinoside and rutin presented alert concerning mutagenicity for hydroxynaphthalene or derivate, and in docking simulations all the compounds presented key interactions with the corresponding targets tested. Conclusion: The flavonoids catechin, chrysoeriol and taxifolin presented overall best results, allowing such computational results to serve as a theoretical basis for future studies of developing drug candidates for biological tests in vitro and in vivo, which can contribute to the treatment of neurodegenerative diseases.
Introdução: A saúde da população LGBT+ apresenta particularidades e vulnerabilidades que requerem atenção diferenciada. Sensibilizar e qualificar profissionais de saúde para as necessidades dessa população é fundamental para garanti-la o direito à saúde. Os currículos das graduações em saúde, que em geral não incorporam tais questões, têm sido interrogados pelo alunado com denúncias de LGBTfobia no curso médico e reivindicação de capacitação prática. Nesse contexto, o Internato Integrado de Medicina de Família e Comunidade e Saúde Mental da Faculdade de Medicina da Universidade Federal do Rio de Janeiro organizou oficina sobre Saúde da População LGBT, apresentada neste artigo. Métodos: Realizada em maio de 2018, teve como público alvo internos em estágio curricular na Atenção Primária em Saúde (APS), no município do Rio de Janeiro. Sensibilizar para o tema e apresentar ferramentas úteis para o cuidado na APS, e em outros cenários, foram os objetivos. Graduandos de medicina autodeclarados LGBT+ foram convidados a assumir a condução da atividade, preparada sob orientação de professoras do internato. O protagonismo dado a esses alunos permitiu articular à expertise científica, promovida nos estudos regulares sobre o tema, a expertise experiencial. A oficina ocorreu em 4 tempos: i) sensibilização; ii) discussão de casos; iii) informação e exposição de orientações para boas práticas em saúde; iv) dúvidas e avaliação. A duração total foi de 4 horas, com metodologias ativas e participativas. Resultados: Os objetivos foram alcançados e a atividade bem avaliada em sua organização e execução. Avaliação narrativa foi realizada com alunos e professores organizadores. Os internos participantes responderam questionário online com perguntas abertas e fechadas e também avaliaram positivamente a atividade nos quesitos metodologia e conteúdo. Conclusão/Desdobramentos: A oficina foi incluída nas atividades regulares do internato. Estão em construção, com vistas a difundir esses conhecimentos a outros estudantes do curso médico e a profissionais da rede de saúde municipal, disciplina eletiva e projeto de extensão. A inclusão longitudinal do tema no currículo permanece como desafio.
Among neurodegenerative disorders, Alzheimer's disease (AD) is the most common type of dementia, and there is an urgent need to discover new and efficacious forms of treatment for it. Pathological patterns of AD include cholinergic dysfunction, increased β‐amyloid (Aβ) peptide concentration, the appearance of neurofibrillary tangles, among others, all of which are strongly associated with specific biological targets. Interactions observed between these targets and potential drug candidates in AD most often occur by competitive mechanisms driven by orthosteric ligands that sometimes result in the production of side effects. In this context, the allosteric mechanism represents a key strategy; this can be regarded as the selective modulation of such targets by allosteric modulators in an advantageous manner, as this may decrease the likelihood of side effects. The purpose of this review is to present an overview of compounds that act as allosteric modulators of the main biological targets related to AD.
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