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1.
Artículo en Inglés | MEDLINE | ID: mdl-38416335

RESUMEN

Pancreatic lipase (PLP) is an enzyme responsible for the catalytic hydrolysis of fats and its inhibition is relevant for obesity management. Side effects linked with orthodox inhibitors have, however, paved the way for an increased search for safe natural sources. The present study investigated the anti-glycation, anti-inflammatory, and anti-lipase properties of Rauvolfia vomitoria aqueous (ARV), ethanolic (ERV), and methanolic (MRV) leaf extracts coupled with the molecular interactions of selected bioactive compounds with PLP using in vitro and in silico techniques. Phytochemical constituents were characterized using spectroscopic techniques. Drug-likeness and chemical reactivity profile of selected bioactive compounds were analyzed using SwissADME and quantum chemical calculations. FT-IR and GC-MS affirmed the presence of phenolic compounds including 3-phenyl-2-ethoxypropylphthalimide and 5-methyl-2-phenyl-1H-indole. All extracts showed moderate anti-glycation, anti-inflammatory, and lipase inhibitory capacities relative to standard controls. However, MRV exhibited the highest lipase inhibition (IC50, 0.17 ± 0.01 mg/mL), using a mixed-inhibition pattern. MRV interaction with PLP resulted in decreased secondary structure components of PLP (α-sheet, ß-turn). MRV compounds (MCP20, MCP28, etc.) exhibited low chemical hardness, EHOMO-ELUMO energy gap, and high chemical reactivity. Foremost MRV compounds obeyed Lipinski's rule of five for drug-likeness and interacted with PHE-78 amongst others at PLP catalytic domain with high binding affinity (≥ - 9.3 kcal/mol). Pi-alkyl hydrophobic interaction and hydrogen bonding were predominantly involved. Our findings provide scientific insights into the ethnotherapeutic uses of R. vomitoria extracts for the management of obesity and related complications, plus useful information for optimizable drug-like candidates against obesity.

2.
Biol Trace Elem Res ; 202(4): 1628-1643, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37468716

RESUMEN

Drinking water polluted by heavy metals has the potential to expose delicate biological systems to a range of health issues. This study embraced the health risks that may arise from subchronic exposure of thirty-four male Wistar rats to nickel (Ni)-cadmium (Cd)-contaminated water. It was done by using the Box-Behnken design (BBD) with three treatment factors (Ni and Cd doses at 50-150 mg/L and exposure at 14-21-28 days) at a single alpha level, resulting in seventeen experimental combinations. Responses such as serum creatinine (CREA) level, blood urea nitrogen (BUN) level, BUN/CREA ratio (BCR), aspartate and alanine aminotransferases (AST and ALT) activities, and the De Ritis ratio (DRR), as well as malondialdehyde (MDA) level, catalase (CAT), and superoxide dismutase (SOD) activities, were evaluated. The results revealed that these pollutants jointly caused hepatocellular damage by raising AST and ALT activities and renal dysfunction by increasing CREA and BUN levels in Wistar rats' sera (p < 0.05). These outcomes were further supported by BCR and DRR values beyond 1. In rats' hepatocytes and renal tissues, synergistic interactions of these metals resulted in higher MDA levels and significant impairments of CAT and SOD activities (p < 0.05). In order to accurately forecast the effects on the responses, the study generated seven acceptable regression models (p < 0.05) with r-squared values of > 80% at no discernible lack of fit (p > 0.05). The findings hereby demonstrated that Wistar rats exposed to these pollutants at varied doses had increased risks of developing liver cirrhosis and azotemia marked by metabolic stress.


Asunto(s)
Azotemia , Agua Potable , Contaminantes Ambientales , Metales Pesados , Ratas , Masculino , Animales , Cadmio/farmacología , Ratas Wistar , Níquel/toxicidad , Níquel/metabolismo , Azotemia/metabolismo , Azotemia/patología , Metales Pesados/metabolismo , Antioxidantes/metabolismo , Cirrosis Hepática/metabolismo , Estrés Fisiológico , Superóxido Dismutasa/metabolismo , Contaminantes Ambientales/metabolismo , Estrés Oxidativo , Hígado/metabolismo , Riñón/metabolismo
3.
Sci Rep ; 12(1): 20705, 2022 12 01.
Artículo en Inglés | MEDLINE | ID: mdl-36456798

RESUMEN

Spices are prolific sources of phytochemicals of pharmaceutical and nutritional importance. They have been employed for centuries in the treatment of various maladies, in cuisines, and as inhibitors of oxidative degradation in foods. On this premise, a comparative assessment of the quantitative mineral composition, phytochemical and proximate constituents of Xylopia aethiopica (fruits), Piper guineense (seeds), and Rhaphiostylis beninensis (roots) was done using standard protocols. Subsequently, methanol extracts of the spices were subjected to Gas Chromatography-Mass Spectrometry (GC-MS) analysis. Mineral analysis of the culinary spices revealed significant differences (p < 0.05) in the spices' magnesium, zinc, iron, selenium, copper, calcium, manganese, molybdenum, potassium, and sodium contents. In the phytochemical analysis, flavonoids, phenols, and alkaloids (4.04%, 2.92%, 2.23%) predominate in X. aethiopica. Similarly, proximate analysis shows a preponderance of carbohydrates (81.24%) and proteins (4.83%) in R. beninensis and P. guineense respectively. However, values for the selenium (0.25 mg/L), saponin (0.23%), and moisture (0.71%) contents for R. beninensis were the lowest among the three spices. Results from the GC-MS analysis revealed the presence of thirteen, twelve, and thirteen phytoconstituents of X. aethiopica, P. guineense, and R. beninensis respectively. Prominent among them are hydrocarbons, acids, and esters with renowned biological attributes such as antioxidant, antimicrobial and anti-inflammatory. These findings indicate that the spices are notable wellsprings of bioactive components and justify their plethoric applications in Nigeria. Therefore, they could serve as lead compounds in the search for natural ingredients for drugs and nutraceuticals formulation.


Asunto(s)
Selenio , Nigeria , Fitoquímicos , Especias , Zinc
4.
Appl Biochem Biotechnol ; 194(6): 2620-2631, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35230606

RESUMEN

The utilization of solid-state fermentation (SSF) of cassava stem, "Manihot esculenta Crantz-MEC", is central in this study for its biochemical characterization and formulation of a new poultry feed using a starter culture of Rhizopus oligosporus strain at specified experimental conditions (26 ± 1 °C, 72 h and pH 6). The coupling of R. oligosporus strain to SSF of cassava stem caused significant increase (p < 0.05) in glucose, total reducing sugar (TRS) and total soluble protein (TSP) concentrations at variable but marked effect at 10% inoculum size of the fermented cassava stem, as compared with the unfermented type. Further evaluations of DPPH-radical scavenging activity, total phenolic and flavonoid contents (TPC and TFC), as indices of correlation to antioxidant activity in both fermented and unfermented cassava stems showed marked significant difference with prominence at 10% inoculum size (p < 0.05). Results of high α-amylase activities were observed in fermented cassava stem when compared with the unfermented type (p < 0.05) at increasing inoculum sizes (5-15%) but with marked dominance at 10%. Broiler chicks fed with formulated feed showed marked increase in weight gain at 10% inoculum size of the fermented cassava stem relative to a typical poultry feed. Also, examination of alkaline phosphatase (ALP) and alanine and aspartate aminotransferases (ALT and AST) showed no marked difference in their activities for fermented feed at increasing inoculum sizes when compared with typical poultry feed, respectively (p > 0.05). The study hereby suggests the use of fermented cassava stem as an alternative raw material during formulation of livestock feeds.


Asunto(s)
Manihot , Animales , Pollos , Fermentación , Manihot/química , Aves de Corral , Verduras
5.
Biol Trace Elem Res ; 200(9): 4160-4170, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34791624

RESUMEN

The contamination of the aquatic ecosystem beyond tolerable limits may pose serious health challenges to its components. This study evaluated the toxic effects of a binary mixture of lead (Pb) and zinc (Zn) compounds on the activity of Na+/K+-ATPase in tissues of Clarias gariepinus in a controlled aquatic system. The study employed Box-Behnken Design (BBD) with 17 runs in which Pb and Zn concentrations were considered process variables in a time-dependent fashion. Metal exposure levels consisted of 0, 10 and 20% of 96 h-LC50 of Pb (55.12 mg/L) and Zn (32.15 mg/L) for three weeks. Thereafter, membrane-bound Na+/K+-ATPase activity was assessed in gill, hepatic and renal tissues, and data generated from the BBD were used for the development of models. Three regression models were obtained, for gill, hepatic and renal Na+/K+-ATPase activities with exposure to metals differ significantly (p < 0.05) at R2 > 90%, and no significant lack of fit (p > 0.05) was observed in each case. Congruent to the synergistic interactions observed between Pb and Zn in the study, the gill and hepatic Na+/K+-ATPase activities were significantly inhibited, whereas renal Na+/K+-ATPase activity was significantly stimulated (p < 0.05). The optimized models were considered reliable, as they were confirmed in the laboratory through accurate prediction of hepatic, renal and gill Na+/K+-ATPase activities with equivalences of 1.22 ± 0.17, 1.66 ± 0.07 and 3.50 ± 0.33 µmol pi/min/mg protein (p < 0.05) respectively. It is hereby concluded that the synergistic interaction between Pb and Zn truncated the physiological function of Na+/K+-ATPase activity in the respective tissues except for renal tissue of exposed C. gariepinus.


Asunto(s)
Bagres , Animales , Bagres/metabolismo , Ecosistema , Branquias , Iones/farmacología , Plomo/toxicidad , Proteínas de Transporte de Membrana , Sodio , ATPasa Intercambiadora de Sodio-Potasio/metabolismo , Zinc/toxicidad
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