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This study assessed the impact of full and late flowering stages on the polyphenols and enzyme inhibitory properties of Hypericum perforatum from Poland. Recognizing the significance of phenolic compounds in disease prevention and melatonin's emerging protective role, we employed an UHPLC-MS/MS system to quantify 38 phenolic compounds, not typical of St. John's wort, and to develop a new method for melatonin quantification. Afterward, the extracts were tested for their antioxidant capabilities (using phosphomolybdenum, DPPH, ABTS, FRAP, CUPRAC and ferrous chelating assays). Moreover, we investigated enzymes (acetylcholinesterase, butyrylcholinesterase and tyrosinase) involved in neurodegenerative disorders and (α-amylase and α-glucosidase) in diabetes. This study recognized the importance of phenolic compounds in disease prevention and explored the emerging protective role of melatonin, taking into account the floral ontogeny of the plant. Indeed, the full-flowering plant contained the greatest concentration of phenolic compounds (a total of 65,276.5 µg/g): hyperoside (18,726.59 µg/g), isoquercitrin (11,895.02 µg/g) and delphindin-3.5-diglucoside (10,619.51 µg/g), and showed the highest inhibitory enzyme activity. Moreover, only full-flowering St. John's wort contained melatonin (40 ng/g). Our results offer additional perspectives on the chemical-biological characteristics of H. perforatum and scientific knowledge that testifies to the importance of considering plant growth conditions for the development of nutraceuticals. [ABSTRACT FROM AUTHOR]

Currently, the number of patients with neurodegenerative pathologies is estimated at over one million, with consequences also on the economic level. Several factors contribute to their development, including overexpression of A2A adenosine receptors (A2AAR) in microglial cells and up-regulation and post-translational alterations of some casein kinases (CK), among them, CK-1δ. The aim of the work was to study the activity of A2AAR and CK1δ in neurodegeneration using in-house synthesized A2A/CK1δ dual anta-inhibitors and to evaluate their intestinal absorption. Experiments were performed on N13 microglial cells, which were treated with a proinflammatory CK cocktail to simulate an inflammatory state typical of neurodegenerative diseases. Results showed that the dual anta-inhibitors have the ability to counteract the inflammatory state, even if compound 2 is more active than compound 1. In addition, compound 2 displayed an important antioxidant effect similar to the reference compound ZM241385. Since many known kinase inhibitors are very often unable to cross lipid bilayer membranes, the ability of A2A/CK1δ double anta-inhibitors to cross the intestinal barrier was investigated by an everted gut sac assay. HPLC analysis revealed that both compounds are able to cross the intestinal barrier, making them promising candidates for oral therapy. [ABSTRACT FROM AUTHOR]

Background: In the scientific literature, there are only a few manuscripts available on small animal faecal proteomics. Methods: In the present pilot study, this evaluation was performed using pooled faecal samples from 10 clinically healthy dogs and, for the first time, in 10 clinically healthy cats by mean of two‐dimensional electrophoresis followed by liquid chromatography‐tandem mass spectrometry. Results: Our results showed the presence of nine (albumin, alkaline phosphatase, chymotrypsin‐C‐like, cytosol aminopeptidase, elastase‐3B/proteinase E, immunoglobulins and nuclear pore membrane glycoprotein 210) and 14 (albumin, caspase recruitment domain‐containing protein, chymotrypsin‐like, deleted in malignant brain tumours 1 protein‐like, hypothetical protein LOC107375, immunoglobulin, kallikrein‐1, superoxide dismutase, transthyretin precursor, interstitial collagenase‐like) different proteins in canine and feline faeces, respectively. Conclusion: These preliminary findings document the presence of a range of proteins in the faeces of apparently healthy dogs and cats and may serve as a basis for larger, prospective studies to establish reference proteomic data against which diseased populations can be compared. [ABSTRACT FROM AUTHOR]

This study quantified, for the first time, 2-isopropylmalic and 3-isopropylmalic acids, in green, roasted and espresso coffee by UHPLC-MS/MS. Moreover, it reports the influence of postharvest processing methods (natural, washed and honey) on their content. New extraction techniques were developed and validated from three coffee matrices (green, roasted and espresso). Honey coffee exhibited levels substantially higher of 2-isopropylmalic acid than those processed by natural and washed methods (p < 0.05). Specifically, 2-isopropylmalic acid levels in honey green, roasted and espresso coffee samples were 48.24 ± 7.31 ng/g, 168.8 ± 10.88 ng/g and 177.5 ± 9.49 ng/g, respectively. This research highlights the significant impact of processing methods on the chemical profile of coffee and introduces 2-isopropylmalic and 3-isopropylmalic acids as potential quality indicators. Moreover, it suggests that the fermentation stage during processing may play a crucial role in their formation, laying the foundation for optimizing coffee processing to enhance quality. [Display omitted] • First quantification of 2-IPMA and 3-IPMA in coffee. • Honey processing boosts 2-IPMA levels. • Novel extraction methods for malic acid derivatives in coffee. • Link between processing methods and chemical profiles. • Potential new indicators of coffee quality. [ABSTRACT FROM AUTHOR]

AbstractObjectivesMethodsResultsConclusionFive solvent extracts (n-hexane, ethyl acetate, ethanol, ethanol/water (70%), and water) of Gladiolus italicus Mill. from Turkey were evaluated for chemical and biological properties.Antioxidant activities, inhibitory properties against key enzymes involved in the etiology of chronic diseases were tested, as well as cytotoxic effects on different cell lines. Chemical characterization was also carried out to determine the most abundant compounds of each extract.The highest total phenolic content (TPC) was observed in the water extract while highest TFC in ethanol/water extract. The most abundant compounds in the extracts were hyperoside (69041.06 mg kg−1), isoquercitrin (46239.49 mg kg−1), delphindin-3,5-diglucoside (42043.81 mg kg−1), myricetin (21486.61 mg kg−1), and kaempferol-3-glucoside (21199.76 mg kg−1). Molecular dynamic (MD) simulations confirmed the structural stability and dynamic conformational integrity of these complexes over a period of 100 ns. In network pharmacology, A total of 657 unique target genes were screened: 52 associated with programmed cell death-1 (PD-1), 85 with vascular endothelial growth factor receptor-2 (VEGFR2), and 130 with fibroblast growth factor receptor-2 (FGFR2), identifying crucial gene interactions for these proteins. Gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were conducted, revealing significant interactions and pathways such as the advanced glycation end products (AGE) and their receptors (RAGE) signaling pathway in diabetic complications and T- helper 17 (Th17) cell differentiation, among others. This elucidation of complex networks involving key genes like AKT Serine/Threonine Kinase 1 (AKT1), MYC proto-oncogene (MYC), tumor protein 53 (TP53), Interleukin 6 (IL6), and tumor necrosis factor (TNF) provides a promising foundation for the development of targeted therapies in the treatment of non-communicable diseases.These results show that G. italicus could be a natural source of potent antioxidants and enzyme inhibitors which need to be further explored for the development of biopharmaceuticals. [ABSTRACT FROM AUTHOR]

Even if the acids composition and their role in coffee still need to be clarified, acidity is one of the main sought-after features in coffee and it is becoming one of the main quality markers. Hence, the aim of this paper was to evaluate the main parameters influencing coffee acidity with a focus on carboxylic acids. To the best of our knowledge, this is the first study regarding filter coffee prepared from specialty and mainstream coffee, differently roasted and through eight diverse extraction methods. Coffee cup chemical composition in terms of organic and chlorogenic acids, caffein and physicochemical parameters were correlated with perceived sourness and mouthfeel to better understand the influence of extracted compounds on the final beverage acidity. Statistical tools revealed that a major impact of chlorogenic acids emerged in pH and titratable acidity, while the sensorial sourness appeared more correlated with organic acids concentration. Thus, these findings suggests that organic acids could be potential predictors of beverage perceived acidity. • The highest organic acids level was found in Ibrik coffee beverage. • Brewing pressure and temperature influence the extraction of organic acids. • In specialty coffee pH and titratable acidity are influenced by CQAs. • In mainstream coffee the CQAs mainly impact the perceived sourness. • Organic acids concentration can predict perceived acidity in specialty coffee. [ABSTRACT FROM AUTHOR]

Boscia coriacea Graells (BC), Grewia erythraea (Schweinf.) Chiov. (GE), Ochradenus baccatus Delile (OB), and Orthosiphon pallidus Royle ex Benth. (OP) are medicinal plants used in Djibouti. They were evaluated to determine their total phenolic content (TPC), flavonoid content (TFC), and phytochemical profile using HPLC-MS/MS. Additionally, their antioxidant capacity was assessed through five various methods. Enzymatic activities were also measured, focusing on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase. OP extract had the highest TPC and exhibited the best antioxidant capacity, whereas OB and BC extracts had the highest TFC. Twenty-seven compounds were identified and quantified by LCMS. GE extract demonstrated the highest AChE activity, whereas OP extract had the highest BChE activity. BC was most active against α-amylase and α-glucosidase, and only GE and OP extracts showed tyrosinase inhibition in vitro. In silico analysis, the compounds were optimized and docked to the human tyrosinase-related protein 1 using AutoDock Vina, with absorption, distribution, metabolism, and elimination to evaluate their suitability based on key therapeutic criteria. Chlorogenic, neochlorogenic, gallic acids, and quercetin emerged as promising tyrosinase inhibitors. These plants can be a viable source in the prevention and treatment related to tyrosinase enzyme inhibition., (© 2024 Wiley‐VHCA AG, Zurich, Switzerland.)