Abstract Propolis is a resinous product collected by honeybees with a complex chemical composition. Sodium carboxymethylcellulose is a polymer commonly used in wound care. The goal of the present work was to produce and characterize NaCMC membranes loaded with extract of Brazilian brown propolis (CMC-P). Flavonoids and phenolic acids were identified in the propolis extracts, where the main identified substance was kaempferide. The brown propolis extracted was active against S. aureus. The low swelling capacity and high gel fraction of CMC-P would be the consequence of propolis (responsible for a hydrophobic barrier) filling the pores of the membrane. Propolis could be anchoring the NaCMC chains (as observed by FTIR) due to interaction between components, which is corroborated by the CMC-P sample degrading less than the CMC sample (>400ºC). There was non-linear diffusion release kinetics for most phenolic substances of the propolis extract. The CMC-P sample presents potential as a dressing material.

Resumo Este trabalho teve como objetivo caracterizar a lignina na parede celular de Euterpe oleracea Mart. Foram adquiridas amostras de duas regiões da base da palmeira: região externa e região interna (OR e IR, respectivamente). A extração com solventes orgânicos e o tratamento com NaOH 1% foram realizados. O conteúdo de holocelulose, α-celulose e lignina foi quantificado, esta última também isolada pelo método de Björkman para a caracterização estrutural utilizando RMN de 1H e 13C no estado líquido, assim como análises espectroscópicas (FTIR) e cromatográficas. O caule extraído apresentou 10,33% (OR) e 15,66% (IR) de lignina. Após tratamento com NaOH 1%, observou-se uma redução desses valores, e foi possível confirmar esse resultado também através da diminuição nas intensidades dos sinais referentes aos grupos funcionais ligados à lignina e hemicelulose. As análises espectroscópicas e cromatográficas revelaram lignina do tipo GS incorporada com ácido p-hidroxibenzoico e protocatecuico em ambas as amostras. Também foram observadas as principais unidades estruturais presentes na lignina como ligação β-O-4, β-O-4’ ϒ-acetiladas, spiro-dienona, unidade guaiacila, unidade siringila e p-hidroxibenzoato.

Abstract This paper aimed to characterize the lignin in the cell wall of Euterpe oleracea Mart. Samples from two regions of the base of the palm were acquired: outer and inner regions (OR and IR, respectively). The extraction with organic solvents and the treatment with 1% NaOH were carried out. Holocellulose, α-cellulose and lignin content were quantified, the latter also isolated by the Björkman method for the structural characterization using 1H and 13C NMR in the liquid state, as well as spectroscopic (FTIR) and chromatographic analysis. The extracted stem had 10.33% (OR) and 15.66% (IR) of the lignin. After the treatment with 1% NaOH, a reduction in these values was observed, and it was also possible to confirm this result through the decrease in the intensities of the signals referring to the functional groups linked to lignin and hemicellulose. The spectroscopic and chromatographic analyzes revealed GS-type lignin incorporated with p-hydroxybenzoic and protocatechuic acid in both samples. The main structural units present in the lignin were also observed, such as β-O-4 bond, β-O-4’ ϒ-acetyl bond, guaiacyl unit, syringyl unit and p-hydroxybenzoate.

NaCMC is a biocompatible polymer that can be crosslinked with citric acid to form a gel matrix. Melaleuca oils have antimicrobial and anti-inflammatory properties with potential for wound healing. The goal of this work was to investigate the characteristics of NaCMC-Melaleuca oils gels. The gels were characterized by FTIR, TGA, mechanical analysis, and in vitro swelling and S. aureus inhibition tests. The oils were characterized using chromatography, presenting high values of (1,8-cineol/terpinen-4-ol), and evaluated for confirmation of their effect against S. aureus. The samples showed physical interactions between NaCMC, citric acid and the Melaleuca oils. Erosion in saline solution was higher in the gels with oils, attributable to interference with crosslinking. The membranes presented high contribution of relaxation mechanism and low contribution of Fickian diffusion regarding the swelling ability. The presence of the oils increased thermal stability and diminished gel fraction and mechanical properties, indicating that the oils interact with the matrix anchoring the chains. Although melaleuca oils themselves were active against S. aureus and CA was responsible for the NaCMC hydrogels activity, the incorporation of melaleuca oils in NaCMC gels was not reported previously. This report indicates that NaCMC hydrogel may be a proper matrix for essential oils incorporation.

Abstract Persea americana Mill., belonging to the family Lauraceae, is noteworthy for the large amount of ethnopharmacological information in its regard, attributing to it many and varied medicinal properties. The tea and alcoholic extracts made from its leaves are used in folk medicine to treat various ailments. This study was designed to analyze the cytogenotoxicity and underlying chemistry of aqueous and hydroalcoholic extracts of avocado leaves, using the Allium cepa and micronucleus tests. The results obtained by applying the experimental models demonstrate that the extracts did not have a genotoxic effect at any of the concentrations analyzed, and even demonstrated a certain protective effect, possibly due to the presence of flavonoids and phenols, both of which are antioxidant substances. However, the extracts did present a cytotoxic effect. There were numerous karyorrhectic cells and those with nuclear alterations related to cell death. At the highest concentrations, it was possible to observe cytoplasmic alterations and binucleated cells. The extracts also caused a significant reduction in the number of cells undergoing division. These effects can be a response to the phytochemical agents present in the extracts. The results suggest that the extracts contain bioactive components that deserve further studies related to cancer therapies.

BACKGROUND Malaria is responsible for 429,000 deaths per year worldwide, and more than 200 million cases were reported in 2015. Increasing parasite resistance has imposed restrictions to the currently available antimalarial drugs. Thus, the search for new, effective and safe antimalarial drugs is crucial. Heterocyclic compounds, such as dihydropyrimidinones (DHPM), synthesised via the Biginelli multicomponent reaction, as well as bicyclic compounds synthesised from DHPMs, have emerged as potential antimalarial candidates in the last few years. METHODS Thirty compounds were synthesised employing the Biginelli multicomponent reaction and subsequent one-pot substitution/cyclisation protocol; the compounds were then evaluated in vitro against chloroquine-resistant Plasmodium falciparum parasites (W2 strain). Drug cytotoxicity in baseline kidney African Green Monkey cells (BGM) was also evaluated. The most active in vitro compounds were evaluated against P. berghei parasites in mice. Additionally, we performed an in silico target fishing approach with the most active compounds, aiming to shed some light into the mechanism at a molecular level. RESULTS The synthetic route chosen was effective, leading to products with high purity and yields ranging from 10-84%. Three out of the 30 compounds tested were identified as active against the parasite and presented low toxicity. The in silico study suggested that among all the molecular targets identified by our target fishing approach, Protein Kinase 3 (PK5) and Glycogen Synthase Kinase 3β (GSK-3β) are the most likely molecular targets for the synthesised compounds. CONCLUSIONS We were able to easily obtain a collection of heterocyclic compounds with in vitro anti-P. falciparum activity that can be used as scaffolds for the design and development of new antiplasmodial drugs.

Resumo Com o objetivo de caracterizar os efeitos não-alvo da ação do fluazuron, foram realizados testes bioquímicos para analisar possíveis alterações no metabolismo de carboidratos em carrapatos Rhipicephalus (Boophilus) microplus após sua exposição ao composto. Foram coletados hemolinfa e corpo gorduroso de fêmeas ingurgitadas antes e após (4, 8 e 15 dias) a exposição ao fluazuron. Análises espectrofotométricas foram usadas para quantificar a concentração de glicose e a atividade da lactato desidrogenase (LDH) na hemolinfa e concentração de glicogênio no corpo gorduroso. Cromatografia Líquida de Alta Eficiência (CLAE) foi usada para determinação das concentrações de ácidos carboxílicos na hemolinfa e avaliar possíveis alterações em metabolismo intermediário em relação ao consumo de oxigênio. Aumento na atividade de LDH e concentração de ácido lático indicaram que o fluazuron pode regular o metabolismo fermentativo em carrapatos. A exposição ao fluazuron também aumentou a concentração de glicose na hemolinfa, apesar de não ter havido diferença significativa na comparação entre as médias no mesmo dia de avaliação. Além de aumentar o conhecimento sobre o modo de ação do fluazuron, investigações sobre tais mecanismos também são úteis no descobrimento de novos efeitos secundários ainda não explorados.

Abstract Aiming to characterize the potential off-target effects of fluazuron on ticks, biochemical analyses were conducted to evaluate changes in the carbohydrate metabolism of Rhipicephalus (Boophilus) microplus ticks after exposure to fluazuron. Hemolymph and fat body were collected from female ticks before and after (4, 8 and 15 days) exposure to fluazuron. Spectrophotometric analyses were done to quantify glucose concentration and lactate dehydrogenase (LDH) activity in the hemolymph and the concentration of glycogen in the tick’s fat body. High Performance Liquid Chromatography (HPLC) was employed to determine the concentration of carboxylic acids in the hemolymph and to evaluate changes in intermediary metabolic processes requiring oxygen consumption. Increases in the levels of LDH activity and lactic acid concentration indicated that fluazuron enhanced fermentative metabolism in ticks. Exposure to fluazuron was also found to increase glucose concentrations in the hemolymph over time, although no significant differences were noted daily. In addition to expanding the body of knowledge about the mode of action of fluazuron, investigations into these mechanisms may also be useful in discovering new and as yet unexplored secondary effects.

The flavonoid fraction was purified by a combination of chromatography on Amberlite XAD-2 and preparative silica gel TLC. Morin (3, 5, 7, 2', 4'- pentahydroxyflavone) was the only flavonol found in honey from Brazilian Citrus sp.. The structure of morin was determined on the basis of UV and ¹H and 13C NMR spectral data together with literature references. This is the first report on the isolation of morin from Brazilian Citrus honey.