Search Results (7,131)

Chronic neuropathic pain severely impairs quality of life, with current therapies often causing adverse effects. Our research group identified αO-conotoxin GeXIVA[1,2] as a potent analgesic candidate derived from marine cone snails. However, its clinical application is limited by rapid clearance and complex administration. This study developed a sustained-release hydrogel microneedle patch encapsulating GeXIVA[1,2] to address these challenges. Optimized 4:3 (w/w) polyvinyl alcohol (PVA)–sucrose hydrogel formulation achieved 98.6% structural integrity and controlled swelling (ratio = 1.9 at 48 h). The microneedles demonstrated uniform conical morphology (height: 889 ± 49 µm, base: 381 ± 26 µm) enabling epidermal penetration. In spared nerve injury (SNI) models, a single microneedle patch application increased mechanical paw withdrawal thresholds from 0.056 g to 0.7269 g, maintaining efficacy for 3 days. Chronic constriction injury (CCI) models showed comparable pain relief. Notably, microneedle patch treatment improved locomotor function in SNI mice (total movement: 1518 cm vs. 1126 cm untreated). This hydrogel microneedle patch platform extends GeXIVA[1,2]’s analgesic duration from hours to days through sustained release, while resolving administration challenges through transdermal delivery, expanding the potential applications of GeXIVA[1,2], and demonstrating a promising strategy for the chronic neuropathic pain management. Full article

This study employs layer-by-layer self-assembly technology to develop novel antibacterial hemostatic microspheres to tackle significant blood loss and related complications resulting from accidents, surgeries, and natural disasters. By measuring the zeta potential and particle size of protamine, carboxymethyl starch (CMS), and hydroxypropyl trimethyl ammonium chloride chitosan (HACC), the optimal assembly conditions were determined. The optimal pH for the monolayer assembly is 3.0, with a CMS concentration of 3 mg/mL and a mass ratio of 1:4 between protamine and CMS, and the assembly process lasts for 2 h. The optimal assembly conditions for the bilayer assembly are a pH of 4.0, an HACC concentration of 1 mg/mL, and a mass ratio of the one-layer assembly to HACC of 1:2. The performance of the assembled microspheres was analyzed via antibacterial and coagulation experiments, revealing excellent antibacterial and coagulation effects, with inhibition rates against Escherichia coli and Bacillus subtilis both exceeding 99%, and a coagulation index of 0%. Additionally, the bilayer assembled microspheres also exhibited strong adsorption capacity and good biocompatibility. In summary, this study provides important scientific evidence for the development of new hemostatic materials, demonstrating significant clinical application potential. Full article

α-Amylases, catalyzing starch degradation, serve as vital biocatalysts in industrial and pharmaceutical applications. This study identified a new α-amylase, Alphaz, from Nocardiopsis aegyptia HDN19-252 of Antarctic animal origin, achieving heterologous expression in Escherichia coli. Phylogenetic analysis confirmed its classification into the GH13_5 subfamily of glycoside hydrolases. Recombinant Alphaz exhibited optimal activity at 40 °C/pH 8.0 while maintaining stability across 0–30 °C and pH 6.6–9.6. Its distinctive halotolerant properties included full activity retention in 0.6 M NaCl and >60% efficiency in salt-free conditions. The enzyme exhibits tolerance to K⁺, Ca²⁺, and Fe³⁺ while demonstrating specific inhibition by Cu²⁺/Zn²⁺. With its heterologously validated functional properties, Alphaz emerges as a programmable enzymatic tool offering advantages in sustained-release formulation quality control, targeted prodrug modification, and precision medicine applications, thereby enabling sustainable biomanufacturing solutions that harmonize process reliability with environmental compatibility. Full article

Chronic obstructive pulmonary disease (COPD) is frequently accompanied by skeletal muscle dysfunction, a critical and severe extrapulmonary complication. This dysfunction contributes to reduced exercise capacity, increased frequency of acute exacerbations, and elevated mortality, serving as an independent risk factor for poor prognosis in COPD patients. Owing to the unique physicochemical conditions of the marine environment, marine-derived bioactive compounds exhibit potent anti-inflammatory and antioxidant properties, demonstrating therapeutic potential for ameliorating COPD skeletal muscle dysfunction. This review summarizes marine-derived bioactive compounds with promising efficacy against skeletal muscle dysfunction in COPD, including polysaccharides, lipids, polyphenols, peptides, and carotenoids. The discussed compounds have shown bioactivities in promoting skeletal muscle health and suppressing muscle atrophy, thereby providing potential strategies for the prevention and treatment of COPD skeletal muscle dysfunction. These findings may expand the therapeutic strategies for managing COPD skeletal muscle dysfunction. Full article

The marine environment, covering over 70% of the Earth’s surface, serves as a reservoir of bioactive molecules, including peptides and proteins. Due to the unique and often extreme marine conditions, these molecules exhibit distinctive structural features and diverse functional properties, making them promising candidates for therapeutic applications. Marine-derived bioactive peptides, typically consisting of 3 to 40 amino acid residues—though most commonly, 2 to 20—are obtained from parent proteins through chemical or enzymatic hydrolysis, microbial fermentation, or gastrointestinal digestion. Like peptides, protein hydrolysates from collagen, a dominant protein of such materials, play an important role. Peptide bioactivities include antioxidant, antihypertensive, antidiabetic, antimicrobial, anti-inflammatory, anticoagulant, and anti-cancer effects as well as immunoregulatory and wound-healing activities. These peptides exert their effects through mechanisms such as enzyme inhibition, receptor modulation, and free radical scavenging, among others. Fish, algae, mollusks, crustaceans, microbes, invertebrates, and marine by-products such as skin, bones, and viscera are some of the key marine sources of bioactive proteins and peptides. The advancements in the extraction and purification processes, e.g., enzymatic hydrolysis, ultrafiltration, ion-exchange chromatography, high-performance liquid chromatography (HPLC), and molecular docking, facilitate easy identification and purification of such bioactive peptides in greater purity and activity. Despite their colossal potential, their production, scale-up, stability, and bioavailability are yet to be enhanced for industrial applications. Additional work needs to be carried out for optimal extraction processes, to unravel the mechanisms of action, and to discover novel marine sources. This review emphasizes the enormous scope of marine-derived peptides and proteins in the pharmaceutical, nutraceutical, cosmeceutical, and functional food industries, emphasizing their role in health promotion and risk reduction of chronic diseases. Full article

BG136, a β-1,3/1,6-glucan derived from Durvillaea antarctica, is an injectable anticancer drug and has entered Phase II clinical trials. Rational oral formulation design is a pivotal focus for our future drug development research; therefore, elucidating the gastrointestinal fate of BG136 becomes imperative. This study investigated the stability and biotransformation of BG136 via in vitro digestion and gut microbiota fermentation. The results confirmed BG136’s structural integrity, resistance to degradation in a highly acid environment and by gastrointestinal tract enzymes. In contrast, BG136 was degraded by intestinal bacteria into mid-size fragments along with smaller oligosaccharides. Additionally, the biotransformation process notably elevated total short-chain fatty acids (SCFAs) to 38.37 ± 3.29 mM, representing a 59.4% increase versus controls (24.08 ± 2.29 mM), with propionic acid exhibiting the most substantial increase. Meanwhile, the process was accompanied by significant microbial regulation, including an increase in beneficial genera (Lactobacillus, Enterococcus) and a reduction in Lachnoclostridium populations. Overall, these findings systematically map the oral bioavailability challenges and prebiotic potential of BG136, highlighting its microbiota-modulating capacity through species-specific ecological regulation, providing insights into oral drug development for BG136. Full article

The liver is an active metabolic site that generates high levels of reactive oxygen species (ROS). Oxidative stress has been implicated in the chronicity of hepatitis and hepatitis B virus (HBV) infection. This study aimed to determine the involvement of oxidative stress in HBV-infected cells and the efficacy of natural Nrf2 activators. The intracellular HBV pregenomic RNA copy number relative to total RNA was measured by RT-PCR, and various protein expressions associated with oxidative stress were analyzed by a Western blot analysis. The results showed that the Nrf2, HO-1, Akt, and Bcl-xL proteins were decreased by the continuous infection, indicating that HBV-positive cells were exposed to oxidative stress. The present study evaluated the anti-HBV infection effects of the Nrf2 activator fucoxanthin (Fx), a marine carotenoid from edible biological resources, including the comparative natural Nrf2 activator pteryxin (Ptx). These Nrf2 activators suppressed the HBV pregenomic RNA production in the HBV-infected cells, thus increasing the expression of the proteins of Nrf2 and HO-1. In the persistently infected cells transfected with the HBV genome, the Bcl-xL and Keap1 proteins, which contribute to suppressing the HBx protein involved in the HBV replication, were overexpressed. In particular, the activity of these protein expressions was marked at low concentrations of Fx. This suggests that natural Nrf2 activators may play a significant role in the HBV infection and could be a valuable source for further development through the functional utilization of food resources. Full article

Background: Oxidative stress, inflammation, and endothelial dysfunction are important processes in the progression of atherosclerosis and the occurrence of acute coronary syndromes (ACSs). Omega-3 polyunsaturated fatty acids (Omega-3 PUFAs) are present in marine organisms and have the capacity to reduce all these processes and, at the same time, the progression of atherosclerosis and the emergence of ACSs. Aim: To evaluate the role of Omega-3 PUFAs therapy on parameters of oxidative stress, inflammatory syndrome, endothelial dysfunction, and long-term prognosis in acute coronary syndromes. Methods: One thousand one hundred forty patients were admitted to Clinic County Emergency Hospital Brasov with ACS and were enrolled in a prospective study. The study was divided into four groups related to the type of ACS and treatment with Omega-3 PUFAs added to the optimal medical therapy (OMT). The effect of Omega-3 PUFAs therapy associated with the OMT was determined by measuring the dynamics of the following parameters: (a) oxidative stress—total antioxidant status (TAS), oxidated low density lipoprotein cholesterol antibodies (Ab anti-ox-LDL), IgG anti-Myeloperoxidase antibodies (IgG type Ab anti-MPO); (b) inflammatory syndrome—C-reactive protein and fibrinogen; (c) endothelial dysfunction—flow mediated dilation (FMD) and von Willebrand factor (vWf) activity, from baseline to 6 months of follow-up. Clinical events followed at 5 years were cardiovascular and sudden death, Non-ST and ST segment elevation ACS, in stent thrombosis and restenosis, stroke, readmission in hospital for ACS and for heart failure. Results: In ACS groups, treatment with Omega-3 PUFAs added to the OMT significantly decreased the parameters of oxidative stress, inflammatory syndrome, and endothelial dysfunction at 6 months of follow-up. Regarding the clinical events, a significant reduction in the risk of cardiovascular and sudden death and a decreased incidence of Non-ST and ST segment elevation ACS, in-stent restenosis, readmission for ACS and heart failure, was observed in Omega-3 PUFA-treated groups in comparison to control groups. Conclusions: In acute coronary syndromes, therapy with Omega-3 PUFAs added to the OMT resulted in a significant decrease of parameters of oxidative stress, inflammation, and endothelial dysfunction at 6 months and also a significant improvement in the long-term prognosis. Full article

Currently, marine algae are still an under-exploited natural bioresource of bioactive compounds. Seaweeds represent a sustainable source for obtaining bioactive compounds that can be useful for the fabrication of new active products with biomedical benefits and applications as biomedicinals and nutraceuticals. The objective of this review is to highlight scientific papers that identify biocompounds from marine macroalgae and emphasize their benefits. The method used was data analysis to systematize information to identify biocompounds and their various benefits in pharmaceuticals, cosmetics, and nutraceuticals. The research results demonstrate the multiple uses of seaweeds. As pharmaceuticals, seaweeds are rich sources of bioactive compounds like polysaccharides, protein compounds, pigments, and polyphenols, which have demonstrated various pharmacological activities such as antioxidant, antibacterial, anti-inflammatory, antiviral, anticoagulant, and potentially anticarcinogenic effects. Seaweed has gained recognition as a functional food and offers a unique set of compounds that promote body health, including vitamins, minerals, and antioxidants. In conclusion, the importance of this review is to expand the possibilities for utilizing natural resources by broadening the areas of research for human health and marine nutraceuticals. Full article

The mixotrophic dinoflagellate Akashiwo sanguinea is known to have acute toxic effects on multiple marine organisms, while the composition and chemical properties of its toxins remain unclear. In this study, we established a method for separation and purification of A. sanguinea toxins using chromatographic techniques. The acetone extract of A. sanguinea exhibited higher hemolytic activity and shorter incubation time compared to methanol and ethyl acetate extracts. Five fractions were obtained by solid-phase extraction (SPE), of which SPE3 (acetone/water ratio 3:2) and SPE4 (acetone/water ratio 4:1) exhibited the highest hemolytic activities and allelopathic effects. Further purification on SPE3 and SPE4 using reverse-phase high-performance liquid chromatography (RP-HPLC) coupled with a diode array detector (DAD) resulted in 11 subfractions, among which Fr4-5 displayed the strongest hemolytic activity. Nearly all active subfractions exhibited higher hemolytic activities incubated under light than those in the dark (p < 0.05), suggesting that A. sanguinea can produce both photosensitive and non-photosensitive toxins, with the former being the primary contributors to its hemolytic activity. Molecular characterization by UV-Vis, FTIR, and HRMS/MS analysis revealed that the structural features of Fr4-5 were highly consistent with porphyrin analogs and could be derived from chlorophyll c-related precursors. These findings highlight that the photosensitive toxins in A. sanguinea may serve dual roles in stress adaptation and ecological competition, potentially contributing to the formation of the blooms. Full article

Bone tissue injuries are a significant health risk, and their repair is challenging. While various materials have potential for bone repair, issues like sourcing and immune rejection limit their use. Marine-derived collagen, abundant and free from religious and disease transmission concerns, is a promising biomaterial in bone tissue engineering. Cross-linking modification can enhance its mechanical properties and degradation rate, making it more suitable for bone repair. However, detailed analysis of cross-linking methods, property changes post-cross-linking, and their impact on bone repair is needed. This review examines marine collagen’s modification methods, improved characteristics, and potential in bone tissue repair, providing a foundation for its effective use in bone tissue engineering. Full article

As a kind of eco-friendly material with wide application prospects, chitooligosaccharide (COS) has attracted increasing attention because of its unique bioactivities. In this study, novel polyphenol-functionalized COS pyridinium salts were designed and synthesized. The structural characteristics of the desired derivatives were confirmed by FT-IR and ¹H NMR spectroscopy. Their antioxidant activities were evaluated in vitro by DPPH radical scavenging assay, superoxide anion radical scavenging assay, and reducing power assay. The solubility assay in common solvents and cytotoxicity assay against L929 cells using the MTT method in vitro were also performed. The antioxidant assay results showed that the compounds functionalized by polyphenol displayed improved antioxidant activities, which were enhanced with the increase of sample concentration and the number of phenolic hydroxyl groups. The solubility assay indicated that the prepared derivatives had good water solubility. Besides, the modified products were non-toxic to the cells tested. In short, the polyphenol-functionalized COS pyridinium salts with enhanced antioxidant activity and good biocompatibility could be employed as newly safe antioxidant in the fields of biomedicine and food. Full article

This study explores the potential anti-H1N1 Influenza A activity of bioactive compounds extracted from Streptomyces ardesiacus, a marine-derived microorganism known for producing diverse secondary metabolites. Four major compounds—1-acetyl-β-carboline, 1H-indole-3-carbaldehyde, anthranilic acid, and indole-3-carboxylic acid—were isolated and characterized through NMR. Among these, the identified structure of 1-acetyl-β-carboline showed the highest IC₅₀ effect, with a dose of 9.71 μg/mL in anti-influenza assays. Using network pharmacology and molecular docking analyses, the interactions of these compounds with key proteins involved in H1N1 pathogenesis were examined. Protein–protein interaction (PPI) networks and Gene Ontology enrichment analysis revealed CDC25B, PARP1, and PTGS2 as key targets, associating these compounds with pathways related to catalytic activity, inflammation, and cell cycle regulation. The molecular docking results demonstrated that 1-acetyl-β-carboline exhibited binding affinities comparable to Tamiflu, the positive control drug, with LibDock scores of 81.89, 77.49, and 89.21 for CDC25B, PARP1, and PTGS2, respectively, compared to Tamiflu’s scores of 84.34, 86.13, and 91.29. These findings highlight the potential of the active compound 1-acetyl-β-carboline from S. ardesiacus as a novel anti-influenza agent, offering insights into their molecular mechanisms of action. The results support further in vitro and in vivo studies to validate the observed inhibitory mechanisms and therapeutic applications against H1N1 Influenza A. Full article

Sixteen polyketides, including six new compounds (1–2, and 5–8), were isolated from the culture of the marine sponge-associated fungus Neopestalotiopsis sp. SCSIO 41422. Their structures were elucidated through NMR, MS spectroscopic analyses, calculated electronic circular dichroism, quantum chemical NMR calculations, and X-ray single-crystal diffraction. To screen and evaluate the inhibitory activity of these polyketides in renal fibrosis, a TGF-β1-stimulated HK-2 cell model was used. All tested compounds (1, 5–8, and 11–12) at 10 µM showed obvious anti-fibrotic activity by inhibiting TGF-β1-induced α-SMA expression and extracellular matrix production (collagen I and fibronectin). Among them, gamahorin A (1) was shown to be the most potent and the most promising inhibitor against renal fibrosis. Full article

Marine macroalgae are excellent sources of bioactive compounds recognized by their pharmaceutical and biomedical potential. A subcritical water extraction (SWE) was applied to the macroalga Codium tomentosum, and the extract was used to prepare phytosomes. A Box–Behnken design was applied to optimize the entrapment efficiency. These phytosomes were further modified with DSPE-PEG (2000)-maleimide and apolipoprotein E and characterized by dynamic light scattering, UV spectrophotometry, octanol/water partition coefficient, differential scanning calorimetry, and Fourier transform infrared spectroscopy. As proof of concept, prototypes of functional food tailored to the elderly were produced. Yogurts were fortified with seaweed extract or phytosomes, and physicochemical properties and proximal composition (pH, acidity, syneresis, moisture, peroxides, proteins, total lipids, sugar content, ash, and mineral composition) were analyzed. The antioxidant and the inhibition capacity of two brain enzymes, cholinesterases (AChE and BuChE), involved in the pathogenesis of Alzheimer’s disease, were also evaluated in the final prototypes. Despite their unappealing sensory characteristics, the results are promising for integrating marine extracts with potential neuroprotective effects into functional foods. Full article