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The ethyl acetate extract of the commercial tannin Tan’Activ QS-SOL (from Schinopsis lorentzii wood), employed for the production of red wine, was subjected to chromatography on Sephadex LH-20, providing nine fractions (A-1–A-9), which were estimated for total phenols content (GAE), antioxidant activity (DPPH, ORAC), and hypoglycemic activity (α-glucosidase and α-amylase inhibition). All the fractions were analyzed by means of HPLC/ESI-MS/MS and 1H-NMR to identify the principal active constituents. Fractions A-1 and A-3 showed the highest antioxidant activity and gallic acid (1), pyrogallol (3), eriodictyol (6), catechin (12), and taxifolin (30) were identified as the major constituents. The highest α-glucosidase and α-amylase inhibitory activity was observed in fractions A-7–A-9 containing condensed (9′, 15, 18, 19, 23, and 27) hydrolysable tannins (13 and 32) as well as esters of quinic acid with different units of gallic acid (5, 11, 11′, 14, and 22). This last class of gallic acid esters are here reported for the first time as α-glucosidase and α-amylase inhibitors.

Honokiol is a natural bisphenol neolignan present in the bark of Magnolia officinalis, whose extracts have been employed in oriental medicine to treat several disorders, showing a variety of biological properties, including antitumor activity, potentially related to radical scavenging. Six bisphenol neolignans with structural motifs related to the natural bioactive honokiol were synthesized. Their chain-breaking antioxidant activity was evaluated in the presence of peroxyl (ROO•) and hydroperoxyl (HOO•) radicals by both experimental and computational methods. Depending on the number and position of the hydroxyl and alkyl groups present on the molecules, these derivatives are more or less effective than the reference natural compound. The rate constant of the reaction with ROO• radicals for compound 7 is two orders of magnitude greater than that of honokiol. Moreover, for compounds displaying quinonic oxidized forms, we demonstrate that the addition of 1,4 cyclohexadiene, able to generate HOO• radicals, restores their antioxidant activity, because of the reducing capability of the HOO• radicals. The antioxidant activity of the oxidized compounds in combination with 1,4-cyclohexadiene is, in some cases, greater than that found for the starting compounds towards the peroxyl radicals. This synergy can be applied to maximize the performances of these new bisphenol neolignans.

The agricultural processing industry usually generates a remarkable amount of by-products rich in bioactive compounds, which can be exploited for agri-food or nutraceutical applications. Pistachio’s hard shell is one of the major by-products from pistachio industrial processing. The aim of this work was the evaluation of pistachio shells as a potential source of natural antioxidants. We evaluated different extraction procedures by measuring total phenolic content, total flavonoid content and antioxidative activity (DPPH•, TEAC and ORAC). The microwave-assisted ethanol extract turned out to be the most promising and was fractionated by XAD-16 column chromatography, affording six fractions analyzed through HPLC/ESI-MS/MS and 1H-NMR to identify the main antioxidative constituents. Fractions Fr4–Fr6 demonstrated the highest antioxidant activity. Gallic acid and a monogalloylglusose isomer are the main phenolic constituents of Fr4. Both simple and complex phenolics, such as flavonoids and hydrolysable tannins, were identified in fractions Fr5 and Fr6; pentagalloylglucose and kaempferol, well-known for their antioxidant activity, are the most abundant constituents. The results highlighted that the proposed methodology can be an effective way to recover bioactive phenolic compounds from pistachio hard shell, making this by-product a promising source of compounds with potential applications in food and healthcare sectors.

Background: Pancreatic lipase (PL), the principal enzyme catalyzing the hydrolysis of dietary triacylglycerols in the intestinal lumen, is pivotal for efficient lipid absorption and plays a central role in metabolic homeostasis. Enhanced PL activity promotes excessive lipid assimilation and contributes to positive energy balance, key pathophysiological mechanisms underlying the escalating global prevalence of obesity—a complex, multifactorial condition strongly associated with metabolic disorders, including type 2 diabetes mellitus and cardiovascular disease. Inhibition of pancreatic lipase (PL) constitutes a well-established therapeutic approach for attenuating dietary lipid absorption and mitigating obesity. Methods: With the aim to identify putative PL inhibitors, a Structure-Based Virtual Screening (SBVS) of PhytoHub database naturally occurring derivatives was performed. A refined library of 10,404 phytochemicals was virtually screened against a crystal structure of pancreatic lipase. Candidates were filtered out based on binding affinity, Lipinski’s Rule of Five, and structural clustering, resulting in six lead compounds. Results: In vitro, enzymatic assays confirmed theoretical suggestions, highlighting Pinoresinol as the best PL inhibitor. Molecular dynamics simulations, performed to investigate the stability of protein–ligand complexes, revealed key interactions, such as persistent hydrogen bonding to catalytic residues. Conclusions: This integrative computational–experimental workflow highlighted new promising natural PL inhibitors, laying the foundation for future development of safe, plant-derived anti-obesity therapeutics.

Inulin is considered a dietary fiber and represents a noteworthy ingredient for food biofortification due to its health effects and its neutral taste. The aim of the work was the evaluation of the quality of pasta produced using whole-meal flours of two ancient Sicilian landraces (Senatore Cappelli-CAP and Timilia—TIM) fortified with two types of inulin (long-chain topinambur inulin IT and low-chain chicory inulin IC), at two different levels of substitution (2 and 4%) to evaluate its possible effect on α-amylase inhibition. The color indices L* and a* were mainly influenced by cultivars, while IT improved the sensory attributes, mainly the elasticity sensation, and influenced less the other sensory attributes: adhesiveness, color, odor, taste, and Over Quality Score for both landraces. The cooking quality was linked mainly to the landrace used, due to the very different gluten matrix of CAP and TIM. IC and IT showed promising α-Amy inhibitory activity with comparable IC50 values of 0.45 ± 0.04 and 0.50 ± 0.06 mg/mL. The enrichment of spaghetti with inulin with an inhibitory effect on α-amylase determined the hypoglycemic properties of pasta, thus lowering the corresponding IC50 value.

The food industry generates the largest number of valuable by-products. The recovery of compounds such as fatty acids and polyphenols with notorious biological properties from biowaste is a new challenge in the circular economy scenario, as they represent value-added starting materials for the preparation of functional foods, food supplements, cosmetics and over-the-counter drugs. Less commonly explored are industrial wastewaters, which return to the nearby water streams without adequate treatment. Distillation wastewater (DWW) from the essential oils or agro-food industries may represent a valuable source of bioactive compounds to be valorized. In this work, DWW from rosemary was treated with different resins through dynamic and static adsorption/desorption approaches, for the recovery of phenolic compounds including rosmarinic acid. The most effective methodology, selected according to total phenolic and rosmarinic acid contents, as well as antioxidant activity evaluation, was applied to sage, thyme and oregano DWWs. The procedure provides several advantages compared with conventional separation processes, as it involves the lower consumption of reagents/solvents, low operational costs, ease of handling, and simplicity of scale-up. The results of this work highlight a fast and sustainable procedure for the recovery of rosmarinic acid and other phenolics (caffeic acid derivatives and flavonoid glycosides) from DWWS, thus affording a fraction with antioxidant and hypoglycemic activities.

Resveratrol is a natural stilbene known for its wide range of biological activities, including antioxidant, anti-inflammatory, and anti-aging effects. However, its application in cosmetics and dermatology is limited by poor stability and bioavailability. Azelaic acid is a natural carboxylic acid employed in cosmetics for its tyrosinase inhibition activity and for cutaneous hyperpigmentation disorders. In this work, we report a concise chemoenzymatic procedure for the synthesis of a novel hybrid molecule combining acetylated resveratrol and azelaic acid. This methodology offers a valuable route for the development of new bioactive compounds for potential cosmetic and dermatological applications.

Among grain pulses, lupins have recently gained considerable interest for a number of attractive nutritional attributes relating to their high protein and dietary fiber and negligible starch contents. The seeds of Lupinus albus (cv. Multitalia and Luxor, and the Modica ecotype); L. luteus (cv. Dukat, Mister, and Taper); and L. angustifolius (cv. Sonet) analyzed in this study were deposited within the germplasm collection of the Research Centre for Cereal and Industrial Crops of Acireale and were sowed in East Sicily in 2013/14. The collected seeds were analyzed for their multielemental micro- and macronutrient profiles, resulting in a wide variability between genotypes. Lupin seed flour samples were subjected to a defatting process using supercritical CO2, with oil yields dependent on the species and genotype. We determined the fatty acid profile and tocopherol content of the lupin oil samples, finding that the total saturated fatty acid quantities of different samples were very close, and the total tocopherol content was about 1500.00 µg/g FW. The proteomic analysis of the defatted lupin seed flours showed substantial equivalence between the cultivars of the same species of Lupinus albus and L. luteus. Moreover, the L. angustifolius proteome map showed the presence of additional spots in comparison to L. albus, corresponding to α-conglutins. Lupin, in addition to being a good source of mineral elements, also contributes vitamin E and, thanks to the very high content of gamma-tocopherols, demonstrates powerful antioxidant activity.

(1) Background: Grape pomace (GP), a major by-product of winemaking, is a sustainable source of bioactive polyphenols with antioxidant, anti-inflammatory, and antimicrobial properties, although their instability limits cosmetic applications. This study aimed to valorize GP through a green extraction process and improve its incorporation and apparent stability in cosmetic formulations through SLN-based systems. (2) Methods: GP extracts were obtained using an eco-friendly extraction method and encapsulated using a W/O/W double emulsion-solvent evaporation technique; nanoparticles were characterized (size, polydispersity, zeta potential) and incorporated into cosmetic formulations compared with a blank and a formulation containing free extract. (3) Results: GP-SLNs exhibited suitable physicochemical properties and preserved antioxidant activity, as confirmed by DPPH and ORAC assays; SLN incorporation appeared to preliminarily improve the photostability profile of the formulation under UVA irradiation conditions; in vivo tests showed enhanced skin hydration and moderate occlusivity, while stability studies confirmed consistent color, odor, pH, and viscosity over 60 days; microbiological analyses demonstrated safety and concentration-dependent antimicrobial activity. (4) Conclusions: SLN encapsulation preserved GP bioactivity and improved formulation stability and performance, supporting its potential use in multifunctional cosmetic products.

Lignans, a class of secondary metabolites found in plants, along with their derivatives, exhibit diverse pharmacological activities, including antioxidant, antimicrobial, anti-inflammatory, and antiangiogenic ones. Angiogenesis, the formation of new blood vessels from pre-existing ones, is a crucial process for cancer growth and development. Several studies have elucidated the synergistic relationship between angiogenesis and inflammation in various inflammatory diseases, highlighting a correlation between inflammation and vascular endothelial growth factor (VEGF)-induced angiogenesis. Thus, the identification of novel molecules capable of modulating VEGF effects presents promising prospects for developing therapies aimed at stabilizing, reversing, or even arresting disease progression. Lignans often suffer from low aqueous solubility and, for their use, encapsulation in a delivery system is needed. In this research, a bioinspired benzoxantene has been encapsulated in solid lipid nanoparticles that have been characterized for their pharmacotechnical properties and their thermotropic behavior. The effects of these encapsulated nanoparticles on angiogenic parameters and inflammation in VEGF-induced angiogenesis were evaluated using human brain microvascular endothelial cells (HBMECs) as a human blood–brain barrier model.