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Environmental sustainability is an increasing challenge in the pharmaceutical field, leading to the search for eco-friendly active ingredients. Among natural ingredients, propolis arises as an excellent alternative, being a complex substance with pharmacological properties. This work aims to explore the potential of propolis as a new pharmaceutical ingredient for the replacement of conventional vulvovaginal antifungals. Propolis extracts were obtained by Ultrasound-Assisted Extraction using different solvents (water, water/ethanol (50:50, v/v), and ethanol). Afterwards, the extracts were characterized regarding total phenolic content (TPC), antioxidant/antiradical activities, radical scavenging capacity, antifungal activity against strains of Candida species, and viability effect on two female genital cell lines. The aqueous extract achieved the best TPC result as well as the highest antioxidant/antiradical activities and ability to capture reactive oxygen species. A total of 38 phenolic compounds were identified and quantified by HPLC, among which ferulic acid, phloridzin and myricetin predominated. Regarding the anti-Candida spp. activity, the aqueous and the hydroalcoholic extracts achieved the best outcomes (with MIC values ranging between 128 and 512 μg/mL). The cell viability assays confirmed that the aqueous extract presented mild selectivity, while the hydroalcoholic and alcoholic extracts showed higher toxicities. These results attest that propolis has a deep potential for vulvovaginal candidiasis management, supporting its economic valorization. [ABSTRACT FROM AUTHOR]

Glioblastoma (GBM) is the most common and deadly primary malignant brain tumor. Current therapies are insufficient, and survival for individuals diagnosed with GBM is limited to a few months. New GBM treatments are urgent. Polymeric nanoparticles (PNs) can increase the circulation time of a drug in the brain capillaries. Polymersomes (PMs) are PNs that have been described as having attractive characteristics, mainly due to their stability, prolonged circulation period, biodegradability, their ability to sustain the release of drugs, and the possibility of surface functionalization. In this work, a poly(ethylene glycol)-ε-caprolactone (PEG-PCL) copolymer was synthesized and PMs were prepared and loaded with an hydrolytic instable compound, previously synthesized by our research team, the 3,6-bis(2,3,4,6-tetra-O-acetyl-β-glucopyranosyl)xanthone (XGAc), with promising cytotoxicity on glioblastoma cells (U-373 MG) but also on healthy cerebral endothelial cells (hCMEC/D3). The prepared PMs were spherical particles with uniform morphology and similar sizes (mean diameter of 200 nm) and were stable in aqueous suspension. The encapsulation of XGAc in PMs (80% encapsulation efficacy) protected the healthy endothelial cells from the cytotoxic effects of this compound, while maintaining cytotoxicity for the glioblastoma cell line U-373 MG. Our studies also showed that the prepared PMs can efficiently release XGAc at intratumoral pHs. [ABSTRACT FROM AUTHOR]

Chestnut shells (CS) are fruit by-products with a high content of (poly)phenols that may play a key role in the oral mucositis (OM) pathogenesis. OM is an inflammatory condition and a common side effect of oncological treatments, being characterized by painful ulceration, difficulty in swallowing and speaking, and an increased risk of infection that can compromise the primary treatment outcome. Natural antioxidants have emerged as an interesting approach to the prevention and treatment of OM by inhibiting the redox imbalance responsible for its development. To overcome the instability and poor water solubility of (poly)phenols, CS extract was encapsulated by spray-drying. The results attested the successful microencapsulation with a product yield of 44%, a total phenolic content of 9.73 mg GAE/g, an antioxidant activity of 91.76 μmol FSE/g and an antiradical ability of 7.83 mg TE/g. FTIR results showed successful encapsulation. The CS-loaded microparticles revealed a median size of 1.95 μm (Dv 50), a moisture content of 4.33% and a swelling capacity of 98.16%. The thermal properties of the extract were preserved, while rheological studies evidenced the microparticles pseudoplastic behavior. The microparticles safety was demonstrated through experiments on oral epithelial cell lines, where no adverse effects were observed at concentrations up to 1 mg/mL. Additionally, the (poly)phenols permeation, such as vanillin, succinic acid, protocatechuic acid, pyrocatechol, and 4-hydroxybenzoic acid, was confirmed by LC-HRMS using an in vitro buccal model. This study demonstrated the potential application of CS-loaded microparticles for the prevention/treatment of OM. [Display omitted] • Chestnut shells (CS) extract was successfully encapsulated. • Microparticles presented high phenolic content and antioxidant activity. • LC-HRMS analysis validated the encapsulation of most of the CS extract. • Vanillin, pyrocatechol, 4-hydroxybenzoic acid and pyroglutamic acid permeated. [ABSTRACT FROM AUTHOR]

[Display omitted] • Lycium barbarum L. berries as a source of valuable bioactive compounds. • Response Surface Methodology enabled the optimization of the extraction process. • Phenolic acids, flavanols, and phenylamides were detected. • The extract proved to be safe for intestinal application at doses up to 500 ug/mL. • Different extract's compounds permeated the cell monolayer. Lycium barbarum L. berries have a remarkable chemical composition and extensive biological activities, being a valuable component of health and nutraceutical practices. Nevertheless, a deep insight on the intestinal permeation of the pro-healthy bioactive compounds is urgently needed to predict the real effects on human body. This study attempted, for the first time, to optimize the Ultrasound-Assisted Extraction (UAE) of goji berries using a Response Surface Methodology approach and establish the intestinal permeation of the principal pro-healthy compounds. The optimal extraction conditions were a solid:liquid ratio of 8.75 % for 56.21 min, using an intensity of 59.05 W/m2. The optimal extract displayed a remarkable antioxidant capacity, with LC/DAD-ESI-MS analysis unveiled a diverse phytochemical profile, encompassing different compounds (e.g. glu-lycibarbarspermidine F, 2-glu-kukoamine, rutin, 3,5-dicaffeoylquinic acid). The intestinal co-culture model demonstrated that glu-lycibarbarspermidine F (isomer 2) (73.70 %), 3,5-dicaffeoylquinic acid (52.66 %), and isorhamnetin-3- O -rutinoside (49.31 %) traversed the intestinal cell layer, exerting beneficial health-promoting effects. [ABSTRACT FROM AUTHOR]

BACKGROUND RESULTS CONCLUSION In recent years, the demand for high‐quality natural extracts to be included in nutraceutical formulations has increased sharply. Hazelnut (Corylus avellana L.) shells (HZS) are underrated agricultural by‐products that could be exploited as a source of active ingredients with pro‐healthy properties. In the present study, a fully green microwave‐assisted extraction (MAE) method was established for the first time aiming to recover bioactive constituents from HZS with significant nutraceutical value. Key MAE parameters, including ethanol in water concentration, microwave power, irradiation time and solvent‐to‐powder ratio, were optimized through response surface methodology utilizing a Box–Behnken design to achieve the highest total phenolic content and antioxidant/antiradical activities in the final extract.The optimal MAE conditions (28% v/v ethanol/water, 270 s, 670 W, and 37 mL g−1) yielded an extract with significant scavenging capacity against reactive oxygen species and remarkable inhibitory activity towards both α‐amylase (IC50 = 7.73 μg mL−1) and α‐glucosidase (IC50 = 49.44 μg mL−1), demonstrating stronger hypoglycaemic properties than the anti‐diabetic drug acarbose. Additionally, fluorescence spectroscopy results highlighted the ability of the optimized extract from HZS (OHS‐E) to counteract advanced glycation end‐product formation throughout the glycation cascade in a dose‐dependent manner. Liquid chromatography/electrospray ionization‐tandem mass spectrometry profiling unveiled the presence of fatty acids and phenolic compounds, including lignans, flavonoids, gallic acid derivatives and diarylheptanoids. Lastly, the biocompatibility of OHS‐E was attested on HT29‐MTX and Caco‐2 intestinal cells.Altogether, these findings encourage the potential application of OHS‐E as an effective nutraceutical component against type 2 diabetes mellitus and oxidative stress. © 2024 The Author(s). Journal of the Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry. [ABSTRACT FROM AUTHOR]