Oral squamous cell carcinoma (OSCC) is a global public health problem with high incidence and mortality. The chemotherapeutic agents used in the clinic, alone or in combination, usually lead to ...important side effects. Thus, the discovery and development of new antineoplastic drugs are essential to improve disease prognosis and reduce toxicity. In the present study, acridine-core naphthoquinone compounds were synthesized and evaluated for their antitumor activity in OSCC cells. The mechanism of action, pharmacokinetics, and toxicity parameters of the most promising compound was further analyzed using in silico, in vitro, and in vivo methods. Among the derivatives, compound 4e was highly cytotoxic (29.99 µM) and selective (SI 2.9) at levels comparable and generally superior to chemotherapeutic controls. Besides, compound 4e proved to be non-hemolytic, stable, and well tolerated in animals at all doses tested. Mechanistically, compound 4e promoted cell death by apoptosis in the OSCC cell, and molecular docking studies suggested this compound possibly targets enzymes important for tumor progression, such as RSK2, PKM2, and topoisomerase IIα. Importantly, compound 4e presented a pharmacological profile within desirable parameters for drug development, showing promise for future preclinical trials.
This study evaluated dental students' perceptions and adherence to an interactive web-based response system in the teaching of Oral and Maxillofacial Pathology. Between 2018 and 2019, students from a ...single Brazilian dental school used the Poll Everywhere® app to answer questions on subjects taught during an Oral and Maxillofacial Pathology course. At the end of the academic semester, the students completed a questionnaire containing 10 questions regarding the app's use. The study included 123 students. Regarding the devices used to answer the questions on the app, 117 (95.1%) students used a smartphone and 3 (2.4%) used a laptop. Almost all students (121; 98.4%) agreed that this interactive web-based response system provided the teacher with a better overview of students' understanding and improved their self-assessment of the acquired knowledge of the subjects. Most students (118; 95.9%) preferred classes using this technology and 122 (99.2%) stated that using the app made them feel more engaged in classes. In addition, all students agreed that the app improved student-teacher interactions. Most students (119; 96.7%) considered the digital interactive method more attractive than the conventional teaching approach, and 99 (80.5%) did not have any negative comments regarding the app. In conclusion, the Poll Everywhere® app provides a more dynamic and attractive educational environment for Oral and Maxillofacial Pathology teaching.
Pequi oil is a valuable product for food industries due to its high levels of unsaturated fatty acids and carotenoids. This work used the complex coacervation technique with cashew gum/chitosan and ...cashew gum/gelatin matrices to encapsulate pequi oil in the production of enriched yogurt. Both wall materials achieved good results in encapsulation efficiency (>80%), yield (>50%), and loading capacity (<50%). The FTIR data demonstrated the presence of electrostatic interactions, thereby confirming encapsulation, and TGA, DSC and Rancimat data verified the microcapsule's stability. The acid release and temperature resistance results showed greater stability at pH's close to the optimum condition of the coacervation process and at temperatures below 80 °C. Finally, the potential for its application in yogurts was realized, showing that the preparation procedure of yogurt influenced the oil release rate and fatty acid profile, and that the addition of microcapsules should be optimally done during the cooling step.
•The wall materials achieved good results in EE, yield, and LC.•FTIR proved the electrostatic interaction of the coacervates.•Microcapsules showed greater stability at pH 3–5 and temperature at 80 °C.•Pequi oil microcapsules showed high potential for application in the yogurt food matrix.
In addition to being used in food, fuel and lubricants, vegetable oils are promising in many other applications such as food additives, nutritional supplements, cosmetics and biomedicine; however, ...their low oxidative stability can limit their use. Microencapsulation is a well-established method for the preservation of oil against degradation, controlled release of active ingredients, protection against external factors during storage, and enhanced durability. In this article, microencapsulation methods for vegetable oil are reviewed, including physical methods (spray-drying and freeze-drying), physicochemical methods (complex coacervation, ionic gelation and electrostatic layer-by-layer deposition), and chemical methods (interfacial/in situ polymerization). This article also provides information on the principles, parameters, advantages, disadvantages and applications of these methods.
Binge drinking is common among adolescents, and this type of ethanol exposure may lead to long-term nervous system damage. In the current study, we evaluated motor performance and tissue alterations ...in the cerebral cortex of rats subjected to intermittent intoxication with ethanol from adolescence to adulthood. Adolescent male Wistar rats (35 days old) were treated with distilled water or ethanol (6.5 g/kg/day, 22.5% w/v) during 55 days by gavage to complete 90 days of age. The open field, inclined plane and the rotarod tests were used to assess the spontaneous locomotor activity and motor coordination performance in adult animals. Following completion of behavioral tests, half of animals were submitted to immunohistochemical evaluation of NeuN (marker of neuronal bodies), GFAP (a marker of astrocytes) and Iba1 (microglia marker) in the cerebral cortex while the other half of the animals were subjected to analysis of oxidative stress markers by biochemical assays. Chronic ethanol intoxication in rats from adolescence to adulthood induced significant motor deficits including impaired spontaneous locomotion, coordination and muscle strength. These behavioral impairments were accompanied by marked changes in all cellular populations evaluated as well as increased levels of nitrite and lipid peroxidation in the cerebral cortex. These findings indicate that continuous ethanol intoxication from adolescence to adulthood is able to provide neurobehavioral and neurodegenerative damage to cerebral cortex.
Synthesis and Biological Profiles of 1,2,3-Triazole Scaffold de Carvalho da Silva, Fernando; Ferreira, Vitor Francisco; da Silva Magalhães Forezi, Luana
Current topics in medicinal chemistry,
01/2018, Letnik:
18, Številka:
17
Journal Article
Pequi oil has a high content of bioactive compounds identified in its composition, which gives it excellent potential for use in the food and pharmaceutical industries. Oil microencapsulation offers ...favorable conditions for storage and controlled release in order to maintain its functional characteristics for a longer time. In this study, vibration nozzle microencapsulation technology is applied to the production of pequi oil microparticles using sodium alginate. After encapsulation, the electrolytic complexation of the particles with chitosan is performed. The influence of frequencies (1500, 1800, 2000, 2500 Hz) on particle size and morphology is evaluated using the 120 µm nozzle. The microparticles formed at 1800 and 2000 Hz presented smaller size and greater sphericity, respectively. The formation of the electrolytic complex from alginate and chitosan is confirmed by FTIR analysis. Frequency adjustment is important for obtaining spherical and homogeneous particles. The encapsulation efficiency of pequi oil in alginate‐chitosan matrix is 96.17%. Electrolytic complexation of the alginate particles with chitosan can improve the reinforcement of the matrix and favor future application in the industry.
Optimized conditions of cashew gum (CG)/and chitosan (CT) were evaluated for the encapsulation of pequi oil by complex coacervation. A comparison was established with gum Arabic (GA)/CT. At first, ...the coacervation process without pequi oil was performed for determining the most appropriate proportion and pH for microparticle formation. The best conditions were of 22:1 at pH 4.5 for the CG/CT, and 6:1 at pH 3.5 for the GA/CT. Pequi oil release in a pH range was higher in pH 4.5 and 5 for GA/CT and CG/CT, respectively. Microparticle yield was about 60% for both complexes. The microparticle size was 4.8 and 2.7 µm for CG/CT and GA/CT, respectively. The encapsulation efficiency was 86 and 89% for CG/CT and GA/CT, respectively. CG forms an interesting complex with CT, 22:1 ratio at pH 4.5, for a suitable encapsulation of pequi oil.
Practical applications
Pequi oil has attractive anti‐inflammatory and antioxidant properties that could be used in the formulation of new cosmetics and nutraceuticals. The microencapsulation of pequi oil assists in the conservation of these properties because it avoids the direct exposure of the actives molecules to environmental factors and to the reagents and procedures involved in the preparation of a product. Complex coacervation method is recommended for the encapsulation of lipophilic substances and has the great advantage of not using high temperatures and being carried out in aqueous medium.
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