ABSTRACT In this study, chemical changes during the development of acerola, cultivar Okinawa, were evaluated. The biochemical alterations during the development of the acerola cultivar Okinawa were ...evaluated, to determine the peroxidase activity (POD) and its thermal stability. Peroxidase (POD) has been considered the main enzyme responsible for the quality deterioration of fruits. Additionally, characteristics evaluated in this study can be important postharvest quality criteria for fruit processing, screening and breeding. Changes in physiological development were evaluated by the determination of moisture content, ascorbic acid, ashes, total and reducing sugars, pectin, chlorophyll a and b, amounts of anthocyanins, flavonols and total carotenoids. These biochemical determinations may serve as a basis for further improvement of techniques for predicting and modeling the optimal harvesting time. The values of chlorophylls, anthocyanins, flavonols, and carotenoids were higher in the peel rather than in the pulp (p < 0.05). Acerola presents high levels of ascorbic acid. The development of acerola (from opening of flowers to maturation of fruits) was of 25 days. The increase of the values for total and reducing sugars, anthocyanins, carotenoids, the solubilization of pectic acid and degradation of chlorophyll suggested that physiological maturation and harvest day occurred on days 19 and 23 after anthesis, respectively. The specific activity of POD was higher in the green stage. Maximum POD activity was observed at pH 6.5 and 45 ºC. Total inactivation was not achieved, suggesting the presence of isoenzymes with high thermal resistance. A loss of 50% of activity occurred after 4 minutes of treatment at 80 °C.
Angiotensin‐converting enzyme inhibitors are widely used in treating arterial hypertension, acting on the renin‐angiotensin‐aldosterone system and controlling blood pressure. We present a novel, ...greener, and faster methodology to assess the 1,2,4‐oxadiazol‐5‐one ring and perform molecular modifications to obtain angiotensin‐converting enzyme (ACE) inhibitors using this heterocyclic core. Molecular docking simulations indicate that the tested compounds exhibited an affinity for the ACE binding site, with scores comparable to the commercial inhibitor lisinopril. However, in vitro assays revealed that the compounds were ineffective in inhibiting ACE activity. The lack of inhibition may be related to the compounds' more apolar nature. These results emphasize the importance of integrating computational and experimental approaches in developing new drugs, providing valuable insights for planning future studies to optimize the activity of synthesized compounds.
This work presents a novel methodology for designing new activity of synthesized compounds (ACE) inhibitors using the 1,2,4‐oxadiazol‐5‐one ring as a heterocyclic core. Our findings highlight the importance of integrating computational and experimental approaches in drug development.
Type 2 diabetes is a chronic disease characterized by insulin resistance and alterations in incretin secretion, such as the glucagon‐like peptide‐1 (GLP‐1) hormone. GLP‐1 plays a crucial role in ...signaling insulin production in the pancreas, with its activity regulated by the dipeptidyl peptidase 4 (DPP‐4) enzyme. DPP‐4 presents an intriguing strategy for controlling type 2 diabetes. This study focuses on synthesizing 22 novel oxadiazolone and pyrimidinone derivatives, in vitro DPP‐4 inhibition, and elucidating binding modes through molecular docking simulations. Nine compounds showed promising inhibitory activity, with IC50 values ranging from 0.3 to 1.86 mM. Molecular docking simulations revealed interactions between these compounds and critical residues in the enzyme's active site, such as Arg125, Glu206, Ser630, and His740. This investigation introduces a new class of DPP‐4 inhibitors, providing insights into the design of more potent molecules as potential candidates for combating type 2 diabetes. The findings contribute to developing innovative therapeutics for managing this prevalent metabolic disorder.
Our investigation introduces a novel class of DPP‐4 inhibitors and contributes to the ongoing efforts to develop new type 2 diabetes drugs.
The synthesis of 2‐thiopyrimidinones through thiol‐ene coupling is reported here, resulting in 35 unpublished molecules. Thiopyrimidinones may exhibit one up to three tautomeric forms, and favoring ...the thiol tautomer is favored is the key to success of this reaction. Five compounds from all obtained products, those substituted with a carbonyl ester portion in the side chain, were chosen to be tested in a preliminary evaluation for human aldose reductase inhibition. All tested compounds showed an inhibition percentage equal to or >60%.
Michael type thiol‐ene coupling was employed to functionalize thiopyrimidinones resulting in 35 new molecules.
Display omitted
The present study evaluated the role of heme oxygenase 1 (HO-1)/carbon monoxide (CO) pathway in the cholera toxin-induced diarrhea and its possible action mechanism. The ...pharmacological modulation with CORM-2 (a CO donor) or Hemin (a HO-1 inducer) decreased the intestinal fluid secretion and Cl− efflux, altered by cholera toxin. In contrast, ZnPP (a HO-1 inhibitor) reversed the antisecretory effect of Hemin and potentiated cholera toxin-induced intestinal secretion. Moreover, CORM-2 also prevented the alteration of intestinal epithelial architecture and local vascular permeability promoted by cholera toxin. The intestinal absorption was not altered by any of the pharmacological modulators. Cholera toxin inoculation also increased HO-1 immunoreactivity and bilirubin levels, a possible protective physiological response. Finally, using fluorometric technique, ELISA assay and molecular docking simulations, we show evidence that CO directly interacts with cholera toxin, forming a complex that affects its binding to GM1 receptor, which help explain the antisecretory effect. Thus, CO is an essential molecule for protection against choleric diarrhea and suggests its use as a possible therapeutic tool.
Introduction: Orthognathic surgery associated with temporomandibular disc reposition is a modality of surgical treatment for dentofacial deformities associated with temporomandibular disorders that ...has been shown to be a stable and predictable alternative for such situations. However, there is still no consensus in the literature regarding the treatment modality in these cases. Several studies have been developed looking for more stable and predictable results in favor of the best patient treatment.
Case Report: Patient with a class II facial pattern and temporomandibular dysfunction, submitted to bilateral repositioning of the articular disc and orthognathic surgery with counterclockwise rotation of the maxillomandibular complex, with improvement of the symptoms and of the functionality of the stomatognathic system, and satisfaction with facial aesthetics.
Conclusion: Although there are controversies about the surgical repositioning of chronic articular disc displacements in retrognathism, this treatment modality has demonstrated long-term stability and reduction or resolution of joint symptoms.
Nesse estudo o objetivo foi adicionar couve (Brassica oleraceae var. acephala) desidratada à formulação de pão de forma, nas concentrações de 2,5% e 5%, e submeter os produtos obtidos as análises ...físico-químicas, sensoriais e de composição química. Ainda, foi elaborado um pão controle, para fins de comparação. A adição de couve desidratada promoveu elevação no pH e acidez dos pães, entretanto, não interferiu no volume específico, que variou de 4,57 a 4,08 cm3/g, e na atividade de água, que foi de 0,95, sendo possível obter produtos com características tecnológicas satisfatórias. No teste sensorial, os pães adicionados de couve apresentaram boa aceitação, com escores médios variando de 6,5 a 8,4, destacando-se quanto à maciez. A cor do pão com 5% de couve foi o único atributo que obteve escore médio abaixo do obtido para o pão controle. A adição de couve desidratada promoveu maior elevação no teor de fibras (133-281%), cálcio (176-297%), fósforo (201-232%), potássio (208-318%) e magnésio (181-300%) dos pães, entretanto, somente para cobre (140-160%) e manganês (76-118%) os incrementos foram suficientes para tornar os produtos fontes desses minerais. Quanto aos teores de ácido oxálico, as concentrações obtidas foram bem abaixo do considerado de risco a saúde. Portanto, a adição de couve desidratada à formulação de pão de forma resultou em produtos com boa aceitação sensorial, com incrementos no valor nutricional, além de oferecer ao consumidor uma nova opção de consumo desse tipo de pão.
The aim of this study was to add dehydrated kale (Brassica oleracea var. acephala) to the formulation of a loaf of bread at concentrations of 2.5% and 5%, and submit the products obtained to ...physico-chemical, sensory and chemical composition analysis. We also designed a control loaf of bread for comparison purposes. The addition of dehydrated kale increased the pH and acidity of the bread; however, it did not affect the specific volume, which ranged from 4.57 to 4.08 cm3/ g, and the water activity, which was 0.95, making it possible to obtain products with satisfactory technological characteristics. In the sensory test, the kale bread showed good acceptance, with mean scores ranging from 6.5 to 8.4, and outstanding softness. The color of the bread with 5% kale was the only attribute that obtained a mean score below the one obtained for the control bread. The addition of dehydrated kale promoted greater increase in the fiber (133-281%), calcium (176-297%), phosphorus (201-232%), potassium (208-318%) and magnesium (181-300%) content of the bread; however, only for copper (140-160%) and manganese (76-118%), were increments sufficient to make the products good sources of these minerals. As regards the level of oxalic acid, the concentrations obtained were far below the level considered as risky to health. Therefore, the addition of dehydrated kale to the formulation of bread resulted in products with good sensory acceptance, increased their nutritional value, and offered consumers a new choice of bread.
The objective of the study was to evaluate the quality of French type bread from bakeries of João Pessoa – PB – Brazil using sensory and instrumental methods. Initially, samples from twelve bakeries ...selected in this study were submitted for determination of specific volume, moisture, pH, acidity, crust color, crumb color and texture profile, all of these analyses have been performed in triplicate, with 10 repetitions. A sensory acceptance test was applied using a 9-point hedonic scale, with 65 tasters. The samples were evaluated considering attributes of appearance, crust color, crumb color, crust crispness, aroma, taste, texture and the overall acceptability. In instrumental tests, it was observed that most of samples showed moisture below 26% and acidity above 4.5 mL of N/10 NaOH 0.1N/10 g of bread. With respect to the specific volume, satisfactory values were observed in 86,2% of samples (between 5.0 and 8.0 cm³/g), while for skin brightness (60-78) and firmness (2.87 to 6.32 N), this percentage was around 80%. In other textural characteristics was observed that the elasticity varied from 0.91 – 1.93, cohesiveness 0.72 – 0.86 and chewiness of 1.91 – 5.71 N. In relation to sensory acceptance, only 50% of the bakeries have had their bread accepted in all evaluated attributes, with average scores similar or superior to 6. The other samples were rejected due to the lack of crispness, and one of those also had its bread rejected in the attributes of aroma, taste and appearance, therefore showing increased need for adequacy.Na presente pesquisa, o objetivo foi avaliar a qualidade do pão tipo francês, comercializado em panificadoras de João Pessoa-PB, por meio de métodos instrumentais e sensoriais. Inicialmente, amostras de pães das doze panificadoras selecionadas nesse estudo foram submetidas às determinações de volume específico, umidade, pH, acidez, cor da casca, cor do miolo e perfil de textura, tendo todas essas análises sido realizadas em triplicata, com 10 repetições. Em seguida, foi aplicado um teste de aceitação sensorial, utilizando-se uma escala hedônica de nove pontos, com 65 provadores, que avaliaram as amostras quanto aos atributos aparência, cor da casca, cor do miolo, crocância da casca, aroma, sabor, textura e aceitação global. Nos testes instrumentais, foi observado que a maioria dos pães apresentou umidade abaixo de 26% e acidez acima de 4,5 mL de NaOH 0,1N/10 g de pão. Com relação ao volume específico, valores satisfatórios foram observados em 86,2% das amostras (entre 5,0 e 8,0 cm³/g), enquanto para a luminosidade da casca (60-78), e firmeza (2,87 a 6,32 N), esse percentual foi em torno de 80%. Para as demais características de textura foi observado que a média da elasticidade variou de 0,91 – 1,93, da coesividade de 0,72 – 0,86 e da mastigabilidade de 1,91 –5,71 N. Em relação à aceitação sensorial, somente 50% das panificadoras tiveram seus pães aceitos em todos os atributos avaliados, com escores médios iguais ou superiores a 6. As demais amostras foram rejeitadas por falta de crocância, e uma destas teve seus pães rejeitados também nos atributos aroma, sabor e aparência, apresentando, portanto, maior necessidade de adequação.
PDF
