Vegetable oils as green solvents for carotenoid extraction from pumpkin (Cucurbita argyrosperma Huber) byproducts: Optimization of extraction parameters.

Pumpkin pulp is the main waste generated by pumpkin seed growers. This agro-industrial waste is a valuable source of bioactive compounds, especially carotenoids (ß-carotene, α-carotene, and lutein), which exhibit a broad spectrum of health-promoting effects. In this study, vegetable oils (canola, corn, and soybean oil) were used as green solvent alternatives to conventional organic solvents for carotenoid extraction from dried pumpkin pulp (DPP) waste. The highest carotenoid extraction yield (CEY) was obtained with canola oil, at a 1:10 DPP/oil ratio. Response surface methodology (RSM) was used to optimize the extraction process parameters (temperature, time, and stirring rate) through a Box-Behnken design (BBD) maximizing CEY in canola oil. The extraction temperature and stirring rate were found to have a significant linear and quadratic effect, respectively, on CEY. Optimum conditions were achieved at 21.8 min, 250 rpm, and 60°C. Under these optimized conditions, the estimated value for CEY was 378.1 µg ß-carotene equivalents/g of DPP, corresponding to 61.6% of the total carotenoid content present in the DPP. In contrast, the observed experimental value was 373.2 µg ß-carotene equivalents/g of DPP (61.2%). The experimental value was very close to the estimated value, which verifies the model's adequacy and fit. This study shows an alternative method to extract carotenoids from DPP with canola oil, obtaining an oil naturally enriched with carotenoids that could be used as a potential functional ingredient in the development of food, cosmetics, and medicinal products. PRACTICAL APPLICATION: Pumpkin by-products are a potential carotenoid source. Vegetable oil can be used as an alternative solvent for carotenoid extraction from pumpkin residues to obtain an enriched carotenoid oil that can be used to formulate food products.

Actividad antimicrobiana de propóleos de abejas sin aguijón en combinación con ajo, Allium sativum (Amaryllidaceae) / Stingless bees propolis antimicrobial activity in combination with garlic, Allium sativum (Amaryllidaceae)

The excessive use of antibiotics has increased pathogenic microorganisms resistance, which derives in patient mortality. Therefore, the strategies for searching new natural and unconventional strategies has become constant and important. Objective: To determine the antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) against stingless bees propolis. Methods: We evaluated nine (20 %) propolis from stingless bees ethanolic extracts from different regions: Melipona beecheii, Melipona solani, Tetragonisca angustula and Scaptotrigona mexicana. The chemical characterization was performed by liquid chromatography (HPLC) and microbial resistance tests by the macrodilution method, to determine the effect of the combinations. Results: The compounds that were of interests and the most abundant were the following; hydroxycinnamic acids, flavanones, flavonoids and the glycosylated derivatives. Four of the nine propolis were effective against MRSA, which came from the following species; one from M. solani and three from S. mexicana. The minimum inhibitory concentration for S. mexicana was in the range of 3-8 mg mL-1 and for M. solani it was 4 mg mL-1. Isobolographic studies resulted in an additive effect (ɤ = 1) for the combination of Allium sativum with the S. mexicana propolis sambles and an antagonistic effect (ɤ > 1) for the combination of A. sativum with the propolis of M. solani. Conclusions: the combination of extracts with lower concentrations of A. sativum, may be the most effective, than those that were individually tested. More detailed studies are required to define the mechanisms of stingless bees propolis as well as their combination with other organic substances.

Introducción: El uso excesivo de antibióticos ha traído el aumento de resistencia en los microorganismos patógenos que provocan mortalidad de los pacientes. Por consiguiente, la búsqueda de nuevas estrategias naturales y no convencionales se ha vuelto constante e importante. Objetivo: Determinar la actividad antimicrobiana contra Staphylococcus aureus resistente a meticilina (SARM) de los propóleos por abejas sin aguijón. Métodos: Nueve fueron los extractos etanolicos de propóleos al 20 % de las abejas sin aguijón de distintas regiones: de Melipona beecheii, de Melipona solani, de Tetragonisca angustula y de Scaptotrigona mexicana. Se realizó la caracterización química de los compuestos por cromatografía liquida y las pruebas de resistencia microbiana por el método de macrodilución para determinar el efecto de las combinaciones. Resultados: Los compuestos de interés fueron detectados, y destacan como los más abundantes los ácidos hidroxicinámicos, flavanonas, flavonoides y sus derivados glicosilados. Cuatro de los nueve propóleos resultaron efectivos contra SARM, los cuales provinieron, uno de Melipona solani y tres de Scaptotrigona mexicana. La CMI para S. mexicana está en el rango de 3-8 mg mL-1 y para M. solani fue de 4 mg mL-1. Los estudios isobolográficos dieron como resultado un efecto aditivo (ɤ = 1) para la combinación de Allium sativum con los 3 propóleos de S. mexicana y un efecto antagónico (ɤ > 1) para la combinación de A. sativum con el propóleos de M. solani. Conclusiones: la combinación de extractos menores puede ser más efectiva que usando la CE50 de los extractos de forma individual. Se requieren estudios más detallados para definir los mecanismos de los propóleos de las abejas sin aguijón, así como su combinación con otras sustancias orgánicas.

In Silico Analysis of FDA Drugs as P2X4 Modulators for the Treatment of Alcohol Use Disorder.

Recent studies have shown the potential application of ivermectins in the treatment of alcohol use disorder (AUD). Ivermectin is a positive allosteric modulator (PAM) of P2X4R and this molecule exerts its action in the transmembrane region (known as the TM region) of trimeric channel structure (the pocket formed by Asp331, Met336, Trp46, Trp50, and Tyr42). The aim of this study is to identify FDA drugs with potential PAM properties, by exploring the P2X4Rs from four organisms (Danio rerio, Mus musculus, Rattus norvegicus, and Homo sapiens). The in silico study consists of carrying out the molecular docking of 1656 FDA-approved drugs on the structure of P2X4R, using the commercially available compounds from the ZINC15 database for virtual screening. To strengthen the reliability of the results, two docking protocols were used involving the use of two programs, Autodock 4.2 and Autodock Vina. Nine FDA drugs with potential PAM properties were identified. In addition, eight molecules with potential negative allosteric modulator (NAM) action, and 13 molecules with potential allosteric modulator (AM) action were identified. The FDA drugs identified in this study with PAM, NAM, and AM action, shared in the P2X4Rs of the four organisms, can provide a guideline to proceed with research concerning new drugs for the study and treatment of AUD.

Apoptosis in pancreatic ß-cells is induced by arsenic and atorvastatin in Wistar rats with diabetes mellitus type 2.

INTRODUCTION: Diabetes Mellitus type 2 (T2D) is a multifactorial disease. However, it is known that there is an important effect in pancreatic ß-cells caused by apoptosis of pro-apoptotic proteins, possibly related to arsenic exposure and atorvastatin treatment. OBJECTIVE: The goal of this study was to evaluate the effects of atorvastatin treatment on apoptosis of pancreatic ß-cells in Wistar rats with induced diabetes type 2 exposed to arsenic. MATERIAL & METHODS: T2D in Wistar rats was induced by administration of Streptozotocin. The plasmatic glucose concentrations were measured using the glucose oxidase method, and the concentration of glycated hemoglobin (HbA1c) in whole blood was determined. Exposure to arsenic was measured from urine using atomic absorption with hydride generation, and pro-apoptotic proteins in pancreatic ß-cells were observed using the Western blotting technique. RESULTS: Caspase-3 was present in rats that were treated with 10 mg/kg of oral atorvastatin and exposed to 0.01 and 0.025 mg/L of arsenic, but no others proteins were present, such as pro Caspase-8, bcl-2, and Fas. The glycemic levels were 129.2 ±â€¯7.0 mg/dL in the control group and 161.8 ±â€¯14.6 mg/dL and 198.3 ±â€¯18.2 mg/dL (p < .05) in the study groups. HbA1c increased from 2.53% to 3.64% (p < .05) in the control and study groups. CONCLUSIONS: Atorvastatin treatment and arsenic exposure alone are capable of generating apoptosis in pancreatic ß-cells of Wistar rats with T2D. Together, all of these factors induce apoptosis in pancreatic cells.