Alzheimer’s disease (AD) is the most common form of dementia and has no cure. Therapeutic strategies focusing on the reduction of oxidative stress, modulation of amyloid-beta (Aβ) toxicity and inhibition of tau protein hyperphosphorylation are warranted to avoid the development and progression of AD. The aim of this study was to screen the crude extracts (CEs) and ethyl-acetate fractions (EAFs) of Guazuma ulmifolia , Limonium brasiliense , Paullinia cupana , Poincianella pluviosa , Stryphnodendron adstringens and Trichilia catigua using preliminary in vitro bioassays (acetylcholinesterase inhibition, antioxidant activity and total polyphenol content) to select extracts/fractions and assess their protective effects against Aβ 25–35 toxicity in SH-SY5Y cells. The effect of the EAF of S . adstringens on mitochondrial membrane potential, lipid peroxidation, superoxide production and mRNA expression of 10 genes related to AD was also evaluated and the electropherogram fingerprints of EAFs were established by capillary electrophoresis. Chemometric tools were used to correlate the in vitro activities of the samples with their potential to be evaluated against AD and to divide extracts/fractions into four clusters. Pretreatment with the EAFs grouped in cluster 1 ( S . adstringens , P . pluviosa and L . brasiliense ) protected SH-SY5Y cells from Aβ 25-35 -induced toxicity. The EAF of S . adstringens at 15.62 μg/mL was able completely to inhibit the mitochondrial depolarization (69%), superoxide production (49%) and Aβ 25-35 -induced lipid peroxidation (35%). With respect to mRNA expression, the EAF of S . adstringens also prevented the MAPT mRNA overexpression (expression ratio of 2.387x) induced by Aβ 25–35 , which may be related to tau protein hyperphosphorylation. This is the first time that the neuroprotective effects of these fractions have been demonstrated and that the electropherogram fingerprints for the EAFs of G . ulmifolia , L . brasiliense , P . cupana , P . pluviosa and S . adstringens have been established. The study expands knowledge of the in vitro protective effects and quality control of the evaluated fractions.

A metformina é um hipoglicemiante oral da classe das biguanidas muito utilizado no tratamento de diabetes mellitus tipo 2. Os estudos de equivalência farmacêutica destinam-se à avaliação de alguns parâmetros de qualidade dos medicamentos por meio de análise comparativa entre o(s) medicamento(s) teste e o medicamento de referência. Dessa maneira, o presente trabalho teve como objetivo avaliar a equivalência farmacêutica de comprimidos de duas marcas de medicamento genérico e duas marcas de similar frente ao medicamento referência de cloridrato de metformina 850 mg. Os testes realizados nas amostras foram peso médio, teor de substância ativa, friabilidade, desintegração e dissolução. As amostras testadas foram aprovadas em todos os testes, encontrando-se dentro dos limites preconizados pela farmacopeia brasileira 5ª edição. Assim pode-se afi rmar que todos os medicamentos testados são equivalentes farmacêuticos do medicamento referência.

Coronavirus disease 2019 (COVID‐19) is caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS‐CoV‐2), which has a high mortality rate and transmissibility. In this context, medicinal plants have attracted attention due to the wide availability and variety of therapeutic compounds, such as alkaloids, a vast class with several proven pharmacological effects, like the antiviral and anti‐inflammatory activities. Therefore, this scoping review aimed to summarize the current knowledge of the potential applicability of alkaloids for treating COVID‐19. A systematic search was performed on PubMed and Scopus, from database inception to August 2021. Among the 63 eligible studies, 65.07% were in silico model, 20.63% in vitro and 14.28% clinical trials and observational studies. According to the in silico assessments, the alkaloids 10‐hydroxyusambarensine, cryptospirolepine, crambescidin 826, deoxynortryptoquivaline, ergotamine, michellamine B, nigellidine, norboldine and quinadoline B showed higher binding energy with more than two target proteins. The remaining studies showed potential use of berberine, cephaeline, emetine, homoharringtonine, lycorine, narciclasine, quinine, papaverine and colchicine. The possible ability of alkaloids to inhibit protein targets and to reduce inflammatory markers show the potential for development of new treatment strategies against COVID‐19. However, more high quality analyses/reviews in this field are necessary to firmly establish the effectiveness/safety of the alkaloids here described.

The crude acetone extract (CAE) of defatted inflorescences of Tagetes patula was partitioned into five semipurified fractions: n-hexane (HF), dichloromethane (DF), ethyl acetate (EAF), n-butanol (BF), and aqueous (AQF). BF was fractionated by reversed-phase polyamide column chromatography, obtaining 34 subfractions, which were subjected to HSCCC, where patuletin and patulitrin were isolated. CAE and the fractions BF, EAF, DF, and AQF were analyzed by LC-DAD-MS, and patuletin and patulitrin were determined as the major substances in EAF and BF, respectively. BF was also analyzed by HPLC and capillary electrophoresis (CE), and patulitrin was again determined to be the main substance in this fraction. CAE and the semipurified fractions (750, 500, 300, 100, and 50 mg/L) were assayed for larvicidal activity against Aedes aegypti, with mortality rate expressed as percentage. All fractions except AQF showed insecticidal activity after 24 h exposure of larvae to the highest concentration. However, EAF showed the highest activity with more than 50% reduction in larval population at 50 mg/L. The insecticidal activity observed with EAF might have been due to the higher concentration of patuletin present in this fraction.

This study aimed to develop and characterize microparticles containing rutin to improve the analgesic activity of the flavonoid. Rutin-loaded microparticles were produced with casein and pectin using the complex coacervation physicochemical method, resulting in an average particle size of 4.903 μm ± 4.421 (mean ± standard deviation), round shape, and irregular surfaces, and rutin crystals can be observed to be adsorbed on the outer surface of microparticles. The encapsulation efficiency was 76.9% as quantified by the antioxidant activity. In vivo, rutin-loaded microparticles showed greater inhibition of carrageenan-induced mechanical hyperalgesia (64%) than nonmicroencapsulated rutin (28%). The X-ray diffraction showed that rutin was dispersed in an amorphous matrix, and its crystallographic structure and crystal size did not exhibit changes. Differential scanning calorimetric studies confirmed that rutin was dispersed in the amorphous matrix within microparticles. The fact that rutin was dispersed in an amorphous matrix in the microparticles seemed to provide enhanced absorption, resulting in an improved analgesic efficacy compared with non-microencapsulated rutin. In conclusion, rutin-loaded microparticles were successfully produced, and they improved analgesic activity compared to non-microencapsulated rutin.

No abstract

No abstract

Introdução: Os estudos de estabilidade são realizados após o desenvolvimento de uma nova formulação, com intuito de prever, determinar ou acompanhar o seu prazo de validade. Os estudos de estabilidade acelerada são projetados para acelerar a degradação química e/ou mudanças físicas de um produto farmacêutico em condições forçadas de armazenamento. Objetivo: O objetivo deste trabalho foi realizar o estudo de estabilidade acelerada de um xarope fitoterápico que está na etapa de desenvolvimento farmacotécnico por uma empresa localizada no município de Santos (SP). Metodologia: Os testes realizados foram características organolépticas, pH, densidade, viscosidade, volume e contagem de microrganismos mesófilos. Resultados: Os valores obtidos para os xaropes base e xarope contendo substâncias ativas, nas análises de pH, características organolépticas, densidade e ensaio microbiológico, estão de acordo com a literatura consultada. Com relação a análise de volume, os resultados obtidos estavam um pouco abaixo do preconizado pela Farmacopeia Brasileira VI edição. Na avaliação da viscosidade, foram encontrados valores abaixo do esperado para formulações de xarope. Conclusão: Os resultados observados indicam que alguns aspectos do xarope necessitam ser reavaliados para garantir uma melhor eficácia e segurança do medicamento.