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21 pages, 3069 KB  
Article
Chitosan-graft-poly(N-vinylcaprolactam) Nanoparticles Containing Crotalus atrox Snake Venom: Biological and Physicochemical Characterization
by Serena Sophia Rudy, Jorge Jimenez-Canale, Jose A. Sarabia-Sainz, Ana María Guzmán Partida, Alexel J. Burgara-Estrella, Erika Silva-Campa, Aracely Angulo Molina, Marcelino Montiel-Herrera, Nelly Flores-Ramírez, Paul Zavala-Rivera and Daniel Fernández-Quiroz
Nanomaterials 2025, 15(19), 1538; https://doi.org/10.3390/nano15191538 - 9 Oct 2025
Abstract
The development of snake venom-loaded nanobiosystems based on smart biopolymers represents a promising therapeutic approach in several biomedical research fields. Specifically, the western diamondback rattlesnake (Crotalus atrox) contains various bioactive peptides and proteins with reported antitumor activity. This research aimed to [...] Read more.
The development of snake venom-loaded nanobiosystems based on smart biopolymers represents a promising therapeutic approach in several biomedical research fields. Specifically, the western diamondback rattlesnake (Crotalus atrox) contains various bioactive peptides and proteins with reported antitumor activity. This research aimed to establish a simplistic, facile and straightforward protocol for preparing chitosan-g-poly(N-vinylcaprolactam) nanoparticles containing C. atrox venom for potential use as a therapeutic nanocarrier against breast carcinoma cell lines. Herein, the physicochemical properties of venom-loaded nanoparticles were evaluated by FTIR, DLS, and SDS-PAGE. Also, the biological properties of both C. atrox venom and Cs-Venom NPs such as hemagglutination and hemolysis activity were evaluated in vitro. Finally, we evaluated their cytotoxic activity against two breast carcinoma cell lines (T-47D and MDA-MB-231). The most suitable formulation exhibited a hydrodynamic size of 222 nm, a ζ-potential of 42.0 mV and an encapsulation efficiency of 88.6%. C. atrox venom exhibited hemagglutination at concentrations >15 µg/mL but, no hemagglutination or hemolysis was observed for the CS-Venom NPs. Lastly, the IC50 of Cs-Venom NPs was determined for the T-47D and MDA-MB-231 cell lines, at 61.7 and 59.0 µg/mL, respectively. Thus, Cs-Venom NPs exhibit promising properties that can be considered a feasible alternative for developing controlled-release therapeutic systems. Full article
(This article belongs to the Special Issue Fabrication and Application of Polymer-Based Nanomaterials)
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24 pages, 3398 KB  
Article
Histological and Proteomic Approaches to Assessing the Adrenal Stress Response in Common Dolphins (Delphinus delphis)
by Claudia Medina Santana, Orla Slattery, Jim O’Donovan and Sinéad Murphy
Animals 2025, 15(19), 2924; https://doi.org/10.3390/ani15192924 - 9 Oct 2025
Abstract
The adrenal glands are central to the stress response in cetaceans, yet their morphological and molecular changes under chronic stress remain poorly described. We investigated adrenal histology and protein composition in stranded common dolphins (Delphinus delphis) to assess whether post-mortem material [...] Read more.
The adrenal glands are central to the stress response in cetaceans, yet their morphological and molecular changes under chronic stress remain poorly described. We investigated adrenal histology and protein composition in stranded common dolphins (Delphinus delphis) to assess whether post-mortem material can provide insights into stress physiology. Adrenal glands from 58 dolphins recovered along the Irish coast during a period of reported nutritional stress in the species were analyzed for adrenal mass, cortex-to-medulla (C:M) ratios, and cortical cell density. Additionally, two archival formalin-fixed, paraffin-embedded (FFPE) tissues were included in a pilot trial to assess the feasibility of protein extraction and mass spectrometry analysis. While adrenal mass did not differ significantly between stress types, chronically stressed dolphins exhibited significantly higher C:M ratios and cortical mass, consistent with cortical hypertrophy. Protein extraction from FFPE tissues was feasible, with the in-gel digestion method yielding more proteins (136) than the filter-aided sample preparation method (22). These findings demonstrate that histological and proteomic approaches can detect stress-related signatures in dolphins and highlight the potential of archival tissues for retrospective biomarker discovery. Full article
(This article belongs to the Section Aquatic Animals)
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14 pages, 3003 KB  
Article
Eco-Friendly Biopolymer Composite Sheet Derived from Water Hyacinth Reinforced with Cassava Chip: Optimal Conditions for Mixing, Blending, and Forming
by Praepilas Dujjanutat, Woravut Suwanrueng and Pakawadee Kaewkannetra
Polymers 2025, 17(19), 2709; https://doi.org/10.3390/polym17192709 - 9 Oct 2025
Abstract
The persistence of the synthetic plastic waste problem makes it one of the most pressing environmental challenges. Sustainable material is an alternative approach to reduce petroleum plastics. In this research, our work aims to convert two biomaterials, water hyacinth (WH) and cassava chip [...] Read more.
The persistence of the synthetic plastic waste problem makes it one of the most pressing environmental challenges. Sustainable material is an alternative approach to reduce petroleum plastics. In this research, our work aims to convert two biomaterials, water hyacinth (WH) and cassava chip (CC), into value-added biopolymer composite sheets (BCS). The raw materials of both WH and CC were prepared and characterized using physical and chemical treatments. Alkali treatments and chemical modifications were applied to remove lignin, protein, lipid, and other inhibiting components. After that, the two main raw materials of the WH and CC components were varied (100:0, 90:10, 80:20, 70:30, and 60:40, respectively) to investigate the optimal conditions for mixing, blending, and forming processes. Finally, mechanical properties (tensile strength), physical properties (surface morphology using a scanning electron microscope (SEM), crystalline structure by X-ray diffraction (XRD), and water solubility were also evaluated. The results obtained obviously revealed that the BCS reached an optimal ratio of 80:20 and exhibited outstanding properties. We were successful in exploring the potential use of a combination of two kinds of biopolymers under optimal conditions to produce an effective and environmentally friendly BCS in a manner that promotes a sustainable bio-circular economy and zero-waste concepts. Full article
(This article belongs to the Section Circular and Green Sustainable Polymer Science)
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33 pages, 2592 KB  
Article
Synthesis of New Phenothiazine/3-cyanoquinoline and Phenothiazine/3-aminothieno[2,3-b]pyridine(-quinoline) Heterodimers
by Victor V. Dotsenko, Vladislav K. Kindop, Vyacheslav K. Kindop, Eva S. Daus, Igor V. Yudaev, Yuliia V. Daus, Alexander V. Bespalov, Dmitrii S. Buryi, Darya Yu. Lukina, Nicolai A. Aksenov and Inna V. Aksenova
Int. J. Mol. Sci. 2025, 26(19), 9798; https://doi.org/10.3390/ijms26199798 - 8 Oct 2025
Abstract
The aim of this work was to prepare new heterodimeric molecules containing pharmacophoric fragments of 3-cyanoquinoline/3-aminothieno[2,3-b]pyridine/3-aminothieno[2,3-b]quinoline on one side and phenothiazine on the other. The products were synthesized via selective S-alkylation of readily available 2-thioxo-3-cyanopyridines or -quinolines with N-(chloroacetyl)phenothiazines, followed by base-promoted Thorpe–Ziegler [...] Read more.
The aim of this work was to prepare new heterodimeric molecules containing pharmacophoric fragments of 3-cyanoquinoline/3-aminothieno[2,3-b]pyridine/3-aminothieno[2,3-b]quinoline on one side and phenothiazine on the other. The products were synthesized via selective S-alkylation of readily available 2-thioxo-3-cyanopyridines or -quinolines with N-(chloroacetyl)phenothiazines, followed by base-promoted Thorpe–Ziegler isomerization of the resulting N-[(3-cyanopyridin-2-ylthio)acetyl]phenothiazines. We found that both the S-alkylation and the Thorpe–Ziegler cyclization reactions, when conducted with KOH under heating, were accompanied to a significant extent by a side reaction involving the elimination of phenothiazine. Optimization of the conditions (0–5 °C, anhydrous N,N-dimethylacetamide and NaH or t-BuONa as non-nucleophilic bases) minimized the side reaction and increased the yields of the target heterodimers. The structures of the products were confirmed by IR spectroscopy, 1H, and 13C DEPTQ NMR studies. It was demonstrated that the synthesized 3-aminothieno[2,3-b]pyridines can be acylated with chloroacetyl chloride in hot chloroform. The resulting chloroacetamide derivative reacts with potassium thiocyanate in DMF to form the corresponding 2-iminothiazolidin-4-one; in this process, phenothiazine elimination does not occur, and the Gruner–Gewald rearrangement product was not observed. The structural features and spectral characteristics of the synthesized 2-iminothiazolidin-4-one derivative were investigated by quantum chemical methods at the B3LYP-D4/def2-TZVP level. A range of drug-relevant properties was also evaluated using in silico methods, and ADMET parameters were calculated. A molecular docking study identified a number of potential protein targets for the new heterodimers, indicating the promise of these compounds for the development of novel antitumor agents. Full article
(This article belongs to the Section Molecular Pharmacology)
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13 pages, 1760 KB  
Article
Association Between Body Mass Index and the Composition of Leucocyte-Poor Platelet-Rich Plasma: Implications for Personalized Approaches in Musculoskeletal Medicine
by Hadrian Platzer, Alena Bork, Malte Wellbrock, Ghazal Pourbozorg, Simone Gantz, Reza Sorbi, Ravikumar Mayakrishnan, Sébastien Hagmann, Yannic Bangert and Babak Moradi
Curr. Issues Mol. Biol. 2025, 47(10), 824; https://doi.org/10.3390/cimb47100824 - 8 Oct 2025
Abstract
Platelet-rich plasma (PRP) has gained attention in regenerative medicine due to its bio-active proteins with tissue-healing potential. However, heterogeneity in PRP composition remains a major challenge for reproducibility and standardization. Given that body mass index (BMI) affects systemic blood parameters, we investigated whether BMI [...] Read more.
Platelet-rich plasma (PRP) has gained attention in regenerative medicine due to its bio-active proteins with tissue-healing potential. However, heterogeneity in PRP composition remains a major challenge for reproducibility and standardization. Given that body mass index (BMI) affects systemic blood parameters, we investigated whether BMI affects the cellular and molecular composition of PRP. Seventy-three participants were stratified into normal weight, overweight, and obese groups. PRP was prepared using a double-syringe system, and platelet activation was induced by freeze–thaw cycles. Whole blood and PRP cell counts were analyzed, and IL6, IGF1, HGF, and PDGF-BB levels in PRP were quantified by ELISA. Platelet enrichment and levels of IGF1, HGF, and PDGF-BB in PRP did not significantly differ between BMI groups. In contrast, IL6 concentrations were higher in normal-weight compared to overweight and obese individuals. Moreover, BMI-related associations emerged between platelet counts and PDGF-BB, and between PRP proteins and sex or caffeine intake, suggesting a more complex BMI-specific modulation of PRP composition. In conclusion, our findings support considering BMI as a relevant factor in PRP therapy. Incorporating BMI into PRP standardization strategies could improve reproducibility and support personalized regenerative approaches. Full article
(This article belongs to the Special Issue Feature Papers in Molecular Medicine 2025)
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22 pages, 1931 KB  
Article
The Effect of a Multi-Component Plant Supplement on the Nutritional Value of Meat Patties
by Gulnur Nurymkhan, Zhanar Kalibekkyzy, Duman Orynbekov, Bakhytkul Assenova, Aray Kambarova, Assel Dautova, Aigul Maizhanova, Gulnara Zhumanova, Zhibek Atambayeva and Eleonora Okuskhanova
Processes 2025, 13(10), 3171; https://doi.org/10.3390/pr13103171 - 6 Oct 2025
Viewed by 179
Abstract
Growing consumer demand for healthier meat products with clean-label ingredients has increased interest in plant-based fortification strategies. The present study evaluated the effects of a multicomponent cereal supplement comprising rice (35%), buckwheat (20%), oats (20%), and corn (25%) on the physicochemical, functional, oxidative, [...] Read more.
Growing consumer demand for healthier meat products with clean-label ingredients has increased interest in plant-based fortification strategies. The present study evaluated the effects of a multicomponent cereal supplement comprising rice (35%), buckwheat (20%), oats (20%), and corn (25%) on the physicochemical, functional, oxidative, hydrolytic, and sensory properties of meat patties. Four formulations were prepared with 0% (control), 5%, 10%, and 15% supplement inclusion. At higher inclusion levels of the cereal supplement, the patties showed reduced moisture, protein, and fat contents, while ash and carbohydrate levels increased. Conversely, ash content increased from 1.38% to 2.82%, and carbohydrates rose to 8.99%. pH remained stable (5.92–6.04), whereas aw decreased significantly at 10% (0.921) and 15% (0.889) inclusion (p < 0.05). Functional tests showed dose-dependent improvements in water-binding capacity, which increased from 65.98% in the control to 71.58% at 10% supplement, and in fat retention, which rose from 38.3% to 54.14% under the same conditions, with optimal performance observed at 10% inclusion. TBARS values in 10% and 15% formulations were 13–20% lower than control throughout storage (p < 0.05). The increase in acid number was significantly slower in supplemented patties, indicating that the cereal blend effectively inhibited lipid hydrolysis during storage. Sensory evaluation revealed maximal acceptability at 10% inclusion, with declines at 15% due to grainy texture and flavor dilution. These findings establish 10% multicomponent cereal supplementation as a promising strategy to enhance yield, shelf-life stability, and consumer appeal of meat patties without compromising processing parameters. Full article
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19 pages, 11841 KB  
Article
Fabrication and Mechanism of Pickering Emulsions Stability over a Broad pH Range Using Tartary Buckwheat Protein–Sodium Alginate Composite Particles
by Yu Song, Xueli Shen, Gangyue Zhou, Xia Xu, Yanan Cao, Wei Li, Yichen Hu, Jianglin Zhao, Dingtao Wu, Zunxi Huang and Liang Zou
Foods 2025, 14(19), 3429; https://doi.org/10.3390/foods14193429 - 5 Oct 2025
Viewed by 357
Abstract
In this study, the insufficient ability of tartary buckwheat protein (TBP) to stabilize Pickering emulsions was addressed by preparing TBP–sodium alginate (SA) composite particles via cross-linking and systematic optimization of the preparation parameters. The results showed that at a pH of 9.0 with [...] Read more.
In this study, the insufficient ability of tartary buckwheat protein (TBP) to stabilize Pickering emulsions was addressed by preparing TBP–sodium alginate (SA) composite particles via cross-linking and systematic optimization of the preparation parameters. The results showed that at a pH of 9.0 with 1.0% (w/v) TBP and 0.2% (w/v) SA, the zeta potential of the prepared TBP–SA composite particles was significantly more negative, and the particle size was significantly larger, than those of TBP, while emulsifying activity index and emulsifying stability index increased to 53.76 m2/g and 78.78%, respectively. Scanning electron microscopy confirmed the formation of a dense network structure; differential scanning calorimetry revealed a thermal denaturation temperature of 83 °C. Fourier transform infrared spectroscopy and surface hydrophobicity results indicated that the complex was formed primarily through hydrogen bonding and hydrophobic interactions between TBP and SA, which induced conformational changes in the protein. The Pickering emulsion prepared with 5% (w/v) TBP–SA composite particles and 60% (φ) oil phase was stable during 4-month storage, at a high temperature of 75 °C, high salt conditions of 600 mM, and pH of 3.0–9.0. The stabilization mechanisms may involve: (1) strong electrostatic repulsion provided by the highly negative zeta potential; (2) steric hindrance and mechanical strength imparted by the dense interfacial network; and (3) restriction of droplet mobility due to SA-induced gelation. Full article
(This article belongs to the Special Issue Advanced Technology to Improve Plant Protein Functionality)
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23 pages, 4451 KB  
Article
Investigation of the Effect of Enamel Matrix Protein, Platelet-Rich Fibrin, and Bone Graft on New Bone Formation in Guided Tissue Regeneration in Rat Calvarium
by Tuğçe Dönmezer, Tuba Talo Yildirim, Serkan Dündar, Alihan Bozoğlan and İbrahim Hanifi Özercan
Medicina 2025, 61(10), 1795; https://doi.org/10.3390/medicina61101795 - 4 Oct 2025
Viewed by 189
Abstract
Background and Objective: The aim of this study was to evaluate the effects of enamel matrix protein, platelet-rich fibrin (PRF), and bone graft on new bone formation beyond the skeletal system by creating calvarial bone defects in rats. The effects were assessed [...] Read more.
Background and Objective: The aim of this study was to evaluate the effects of enamel matrix protein, platelet-rich fibrin (PRF), and bone graft on new bone formation beyond the skeletal system by creating calvarial bone defects in rats. The effects were assessed using histopathological and immunohistochemical analyses. Materials and Methods: In this study, calvarial bone defects were created in male Sprague Dawley rats weighing 500–550 g. The animals were randomly divided into seven groups: Control (n = 13), Emdogain (EMD, n = 13), Emdogain + Bone Graft (EMD + BG, n = 13), Platelet-Rich Fibrin (PRF, n = 13), PRF + Bone Graft (PRF + BG, n = 13), Bone Graft (BG, n = 13), and PRF + Emdogain + Bone Graft (PRF + EMD + BG, n = 13). An additional group of 36 rats was used for PRF preparation. Titanium domes were placed on the calvarial bone defects, and the animals were sacrificed after three months. Bone samples were evaluated histopathologically for new bone formation, numbers of osteoblasts and osteoclasts, angiogenesis, and fibrosis. Immunohistochemical analysis of bone formation was performed using OPG and RANKL staining kits. Data were analyzed statistically. Results: The PRF group showed a significantly higher level of moderate new bone formation compared with the PRF + BG, EMD + BG, and PRF + EMD + BG groups (p ≤ 0.05). No significant differences were observed among the groups in terms of fibrosis or angiogenesis (p > 0.05). Similarly, OPG and RANKL levels, as well as the OPG/RANKL ratio, did not differ significantly between groups (p > 0.05). Conclusions: Based on the findings of this study, the combined use of Emdogain, PRF, and bone graft appears to have beneficial effects on enhancing bone formation in calvarial defects. Full article
(This article belongs to the Section Dentistry and Oral Health)
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20 pages, 3589 KB  
Article
Comparison of Different Aliphatic Polyester-Based Microparticles as Protein Delivery Systems
by Viktor Korzhikov-Vlakh, Ekaterina Sinitsyna, Mariia Stepanova, Evgenia Korzhikova-Vlakh and Tatiana Tennikova
Polymers 2025, 17(19), 2676; https://doi.org/10.3390/polym17192676 - 3 Oct 2025
Viewed by 261
Abstract
The utilization of encapsulated biopharmaceuticals, including peptides and proteins, has grown substantially in recent years. In this study, the influence of aliphatic polyester physicochemical properties, specifically crystallinity and hydrophobicity, on the development of protein-loaded microparticles was investigated. A series of polyesters, namely amorphous [...] Read more.
The utilization of encapsulated biopharmaceuticals, including peptides and proteins, has grown substantially in recent years. In this study, the influence of aliphatic polyester physicochemical properties, specifically crystallinity and hydrophobicity, on the development of protein-loaded microparticles was investigated. A series of polyesters, namely amorphous PDLLA and semicrystalline PLLA, PCL, and PPDL, were synthesized via chemical and enzymatic ring-opening polymerization. Bovine serum albumin (BSA)-loaded microparticles were fabricated using a water-in-oil-in-water (w/o/w) double emulsion solvent evaporation method. The size of microparticles obtained was determined by scanning electron microscopy and dynamic light scattering methods. The enzymatic degradation of the polymer microparticles was assessed through incubation in a lipase-containing buffer solution. BSA and α-chymotrypsin (ACHT) were used as model proteins for the preparation of encapsulated polymer microspheres and comparison of their characteristics and properties. Protein encapsulation efficacy, release rate, and enzyme activity retained after encapsulation were evaluated and compared for selected aliphatic polyesters. The release profiles were processed with the use of various mathematical models to reveal the possible mechanism(s) of protein release. Full article
(This article belongs to the Special Issue Polyester-Based Materials: 3rd Edition)
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13 pages, 1484 KB  
Article
Development of an Empirical Model as a Prediction Tool for the Sound Absorption Performance of Wool/Soy Protein Biocomposites
by Jesús Alba, Marta Urdanpilleta, Romina del Rey, Itsaso Leceta, Pedro Guerrero and Koro de la Caba
Polymers 2025, 17(19), 2666; https://doi.org/10.3390/polym17192666 - 2 Oct 2025
Viewed by 714
Abstract
Finding eco-friendly alternatives to the synthetic materials used for acoustic application in building industry is necessary to address environmental sustainability. Biocomposites of natural fibers combined with a biopolymer matrix emerge as a promising approach. In this study, soy protein biocomposites were prepared with [...] Read more.
Finding eco-friendly alternatives to the synthetic materials used for acoustic application in building industry is necessary to address environmental sustainability. Biocomposites of natural fibers combined with a biopolymer matrix emerge as a promising approach. In this study, soy protein biocomposites were prepared with 10, 15, and 20 wt% sheep wool and were added spent coffee grounds by freeze-drying to create fibro-porous biocomposites for acoustic applications. Transmission loss (TL) measurements underlined good behavior as sound insulators, with maximum values around 22 dB at 2500 Hz and even better performance than those of commercial synthetic solutions. The obtained sound absorption coefficients were competitive, as they almost reached unity at medium and high frequencies. Airflow resistivity was determined, and values were higher for the biocomposites with coffee grounds, specifically 14–18 kPa·s·m−2 vs. 5.62–11.6 kPa·s·m−2. Using the input of the measured airflow resistivity, an empirical model using a genetic algorithm was developed as a prediction tool for the sound absorption performance of the samples. All in all, results showcase the feasibility of employing the studied biocomposites as competitive sound insulators and absorbers in building construction industry. Full article
(This article belongs to the Special Issue Modeling of Polymer Composites and Nanocomposites (2nd Edition))
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38 pages, 2377 KB  
Review
CRISPR-Cas-Based Diagnostics in Biomedicine: Principles, Applications, and Future Trajectories
by Zhongwu Zhou, Il-Hoon Cho and Ulhas S. Kadam
Biosensors 2025, 15(10), 660; https://doi.org/10.3390/bios15100660 - 2 Oct 2025
Viewed by 743
Abstract
CRISPR (Clustered Regularly Interspaced Short Palindromic Repeats)-Cas (CRISPR-associated) systems, originally identified as prokaryotic adaptive immune mechanisms, have rapidly evolved into powerful tools for molecular diagnostics. Leveraging their precise nucleic acid targeting capabilities, CRISPR diagnostics offer rapid, sensitive, and specific detection solutions for a [...] Read more.
CRISPR (Clustered Regularly Interspaced Short Palindromic Repeats)-Cas (CRISPR-associated) systems, originally identified as prokaryotic adaptive immune mechanisms, have rapidly evolved into powerful tools for molecular diagnostics. Leveraging their precise nucleic acid targeting capabilities, CRISPR diagnostics offer rapid, sensitive, and specific detection solutions for a wide array of targets. This review delves into the fundamental principles of various Cas proteins (e.g., Cas9, Cas12a, Cas13a) and their distinct mechanisms of action (cis- and trans-cleavage). It highlights the diverse applications spanning infectious disease surveillance, cancer biomarker detection, and genetic disorder screening, emphasizing key advantages such as speed, high sensitivity, specificity, portability, and cost-effectiveness, particularly for point-of-care (POC) testing in resource-limited settings. The report also addresses current challenges, including sensitivity limitations without pre-amplification, specificity issues, and complex sample preparation, while exploring promising future trajectories like the integration of artificial intelligence (AI) and the development of universal diagnostic platforms to enhance clinical translation. Full article
(This article belongs to the Special Issue Aptamer-Based Biosensors for Point-of-Care Diagnostics)
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12 pages, 1810 KB  
Article
Polyethyleneimine-Assisted Fabrication of Poly(Lactic-Co-Glycolic Acid) Nanoparticles Loaded with Tamibarotene (Am80) for Meflin Expression Upregulation
by Tomoya Inose, Tadashi Iida, Hiroki Kawashima, Atsushi Enomoto, Maki Nakamura and Ayako Oyane
J. Funct. Biomater. 2025, 16(10), 368; https://doi.org/10.3390/jfb16100368 - 1 Oct 2025
Viewed by 511
Abstract
Tamibarotene (Am80) is a promising anti-tumor drug that induces the expression of Meflin (a glycosylphosphatidyl inositol-anchored protein) in cancer-associated fibroblasts, thereby improving the tumor microenvironment. However, Am80, which is approved only for oral administration owing to its poor water solubility, has the challenge [...] Read more.
Tamibarotene (Am80) is a promising anti-tumor drug that induces the expression of Meflin (a glycosylphosphatidyl inositol-anchored protein) in cancer-associated fibroblasts, thereby improving the tumor microenvironment. However, Am80, which is approved only for oral administration owing to its poor water solubility, has the challenge of poor tumor penetration. In this study, we developed poly(lactic-co-glycolic acid) nanoparticles loaded with Am80 (Am80–PLGA nanoparticles) as a potential intravenous drug for targeted Am80 delivery to the tumor site. The Am80–PLGA nanoparticles were fabricated using the single-emulsion method in the presence of cationic polyethyleneimine (PEI). The loading efficiency of Am80 in the nanoparticles was controlled by tuning the PEI concentration in the preparation mixture. Nanoparticles with the highest Am80-loading efficiency were dispersible and showed a hydrodynamic diameter of approximately 190 nm in phosphate-buffered saline for up to 2 weeks. The Am80 release from the nanoparticles started in a day and lasted for weeks. The nanoparticles upregulated Meflin expression in human fibroblasts (fHDF/TERT166 cells). These results suggest the potential of Am80–PLGA nanoparticles as a new intravenous anti-tumor drug that can improve the tumor microenvironment, thereby enhancing the efficacy of chemotherapy and immunotherapy. Full article
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69 pages, 1993 KB  
Review
Glycyrrhizin (Glycyrrhizic Acid)—Pharmacological Applications and Associated Molecular Mechanisms
by Deepak Kumar Semwal, Ankit Kumar, Ruchi Badoni Semwal, Nand Kishor Dadhich, Ashutosh Chauhan and Vineet Kumar
Drugs Drug Candidates 2025, 4(4), 44; https://doi.org/10.3390/ddc4040044 - 30 Sep 2025
Viewed by 889
Abstract
Background/Objectives: Natural products, especially plant metabolites, play a crucial role in drug development and are widely used in medicine, cosmetics, and nutrition. The present review aims to provide a comprehensive overview of the pharmacological profile of Glycyrrhizin (GL), with a specific focus on [...] Read more.
Background/Objectives: Natural products, especially plant metabolites, play a crucial role in drug development and are widely used in medicine, cosmetics, and nutrition. The present review aims to provide a comprehensive overview of the pharmacological profile of Glycyrrhizin (GL), with a specific focus on its molecular targets. Methods: Scientific literature was thoroughly retrieved from reputable databases, including Scopus, Web of Science, and PubMed, up to 30 July 2025. The keywords “glycyrrhizin” and “glycyrrhizic acid” were used to identify relevant references, with a focus on pharmacological applications. Studies on synthetic analogs, non-English publications, non-pharmacological applications, and GL containing crude extracts were largely excluded. Results: Glycyrrhizin, the major bioactive constituent of Glycyrrhiza glabra, exhibits diverse pharmacological activities, including anti-inflammatory, antiviral, hepatoprotective, antitumor, neuroprotective, and immunomodulatory effects. These actions are primarily mediated through the inhibition of high-mobility group box 1 (HMGB1) and the modulation of key signaling pathways, including nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (MAPK), phosphoinositide 3-kinase/protein kinase B (PI3K/Akt), and various cytokine networks. As a result of its therapeutic potential, GL-based formulations, including Stronger Neo-Minophagen C, and GL-rich extracts of G. glabra are commercially available as pharmaceutical preparations and food additives. Conclusions: Despite its therapeutic potential, the clinical application of GL is limited by poor oral bioavailability, metabolic variability, and adverse effects such as pseudoaldosteronism. Hence, careful consideration of pharmacokinetics and safety is essential for translating its therapeutic potential into clinical practice. Full article
(This article belongs to the Section Drug Candidates from Natural Sources)
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13 pages, 579 KB  
Article
Is There Need for Pancreatic Enzyme Replacement Therapy in Patients with Exocrine Pancreatic Insufficiency When Using High-Caloric Liquid Diets? Orientating Studies on Praecaecal Digestibility in Pigs with Experimentally Induced Pancreatic Exocrine Insufficiency and Ileocaecal Fistula
by Anne Katrin Mößeler, Annette Liesegang, Paul Torgerson and Josef Kamphues
Biomolecules 2025, 15(10), 1392; https://doi.org/10.3390/biom15101392 - 30 Sep 2025
Viewed by 141
Abstract
In patients with pancreatic exocrine insufficiency (PEI), focus is primarily placed on fat digestion. Using high-caloric drinks (HCD) is often recommended to avoid malnutrition, but knowledge is limited whether pancreatic enzyme replacement therapy (PERT) is needed. In this study the animal model of [...] Read more.
In patients with pancreatic exocrine insufficiency (PEI), focus is primarily placed on fat digestion. Using high-caloric drinks (HCD) is often recommended to avoid malnutrition, but knowledge is limited whether pancreatic enzyme replacement therapy (PERT) is needed. In this study the animal model of pancreatic duct-ligated (PL) and ileocaecal-fistulated minipig was used to determine the praecaecal disappearance rates (pcDR) of the fat and protein of four HCD in controls and PL-pigs with or without PERT. In controls pcDR were high (95.5–96.6% for fat; 70.2–78.6% for protein) while in PL-pigs receiving no PERT the pcDR were significantly lower (fat DR: 47.4–54.3%; protein 22.4–33.5%) despite a high fat pcDR value (84.0%) of one diet. PERT resulted in a normalisation of pcDR of fat and protein with values not differing from controls. This study demonstrates the massive impact of PEI on pcDR, even in HCD typically considered highly digestible. Using PERT is highly recommended in PEI patients using HCD to avoid maldigestion and associated digestive tract symptoms. Optimisation of formulations and galenic preparations of the HCD seems to be necessary as well, as the high fat pcDR of one drink showed that even without PERT high values can be reached. Full article
(This article belongs to the Special Issue Digestive Enzymes in Health and Disease)
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16 pages, 2117 KB  
Article
Potential Therapeutic Effects of Oolong Tea Phytochemicals on NLRP3 Inflammasome Assembly and Oxidative Stress
by Ming-Shyan Wang, Szu-Nian Yang, Yi-Ping Chang, Chi-Sheng Wu, Hung-Chi Yang and Jia-Feng Chang
Nutrients 2025, 17(19), 3106; https://doi.org/10.3390/nu17193106 - 30 Sep 2025
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Abstract
Background/Objectives: Tea, the world’s second most consumed beverage after water, contains diverse phytochemicals that have garnered growing interest for their potential ability to modulate inflammasome activation. This study examined the antioxidant and anti-inflammatory properties of oolong tea (OLT) extracts, with a specific focus [...] Read more.
Background/Objectives: Tea, the world’s second most consumed beverage after water, contains diverse phytochemicals that have garnered growing interest for their potential ability to modulate inflammasome activation. This study examined the antioxidant and anti-inflammatory properties of oolong tea (OLT) extracts, with a specific focus on their regulatory effects on NLRP3 inflammasome assembly—a critical mediator in chronic inflammatory diseases. Methods: OLT extracts were prepared from the Jin-Xuan cultivar with quantification for bioactive components (total phenolics, flavonoids, condensed tannins, and proanthocyanidins). J774A.1 murine macrophages were primed with LPS and stimulated with ATP to induce inflammasome activation. Therapeutic potentials of OLT extracts were assessed by measuring cytokine secretion, expression of NLRP3 inflammasome-related proteins (NLRP3, ASC, Caspase-1, and IL-1β), inflammasome complex formation, and ROS generation via biochemical assays, immunoblotting, and fluorescence microscopy. Results: OLT extracts, particularly at 100 µg/mL, markedly suppressed both the priming and activation phases of NLRP3 inflammasome formation. OLT treatment reduced IL-1β secretion by more than 50%, attenuated ASC oligomerization and speck formation, inhibited caspase-1 cleavage, and lowered intracellular ROS levels by approximately 50%. Conclusions: These findings suggest that OLT extracts exert potent anti-NLRP3 inflammasome activity and offer immunomodulation potential in preventing inflammation-related diseases such as infections, cancer, and neurodegenerative disorders. Further in vivo investigations, followed by clinical applications and epidemiological studies, are warranted to validate these preventive effects in human populations. Full article
(This article belongs to the Section Nutrition and Metabolism)
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