搜索结果：Marine drugs

Inflammation is pivotal to the pathogenesis of chronic disorders, including diabetes and cardiovascular disorders. Conventional pharmaceuticals used in the treatment of inflammation and related diseases face several challenges. In recent years, polysaccharides isolated from marine organisms have attracted extensive research attention due to their good safety profile, easy availability, and powerful anti-inflammatory properties. However, there is still a lack of systematic elucidation of their anti-inflammatory mechanisms and functional effects. In this review, the sources and structural characteristics of marine polysaccharides were reviewed. Moreover, the anti-inflammatory mechanisms of marine polysaccharides and their advanced applications were discussed. Finally, the current challenges of marine polysaccharides in anti-inflammatory research and food industry applications, as well as future research directions, were proposed. This review deepens the understanding of the anti-inflammatory effects of marine polysaccharides and provides feasible guidance for the development and clinical application of novel anti-inflammatory drugs.

Probiotics are known to improve gut microbiota balance, enhance food digestion, and support overall health. Among these, Bacillus species are particularly promising due to their safety, spore-forming ability, environmental resilience, and diverse enzymatic activities. However, most Bacillus probiotics used in industry are of terrestrial origin, leaving marine-derived strains largely unexplored. Utilising the untapped potential of marine microbial biomass, this study presents a multi-stage methodology for identifying and evaluating marine-derived Bacillus strains with probiotic potential. A structured screening pipeline was applied to 67 microbial isolates from the Great Barrier Reef sponges. Initial selection focused on essential probiotic characteristics, including growth, stability, safety, and survival under gastrointestinal conditions. Strains meeting these criteria were then assessed for desirable properties, including digestive enzyme production and pathogen inhibition. Using this workflow, three marine-derived Bacillus strains were identified as potential probiotics, one of which demonstrated strong antimicrobial activity against Salmonella enterica at 5 and 10 mg/mL (p < 0.01). These findings demonstrate the capability of marine-associated Bacillus as novel bioproducts with functional antimicrobial properties.

The liver is a central regulator of systemic metabolism and exhibits exceptional regenerative capacity, yet aging progressively impairs hepatic resilience through metabolic dysregulation, mitochondrial dysfunction, epigenetic instability, and chronic inflammation. Marine ecosystems constitute a vast and underexplored source of structurally diverse bioactive compounds that have evolved to modulate conserved stress response and homeostatic pathways. This review synthesizes current preclinical evidence demonstrating how marine-derived metabolites target key molecular axes implicated in liver aging, including energy sensing, redox balance, mitochondrial quality control, inflammatory signaling, and chromatin-associated regulation. Rather than focusing solely on isolated hepatoprotective effects, we frame marine bioactives within an aging biology perspective, highlighting their ability to modulate pathways associated with cellular plasticity and resilience. We further propose that this mechanistic convergence provides a theoretical framework for exploring marine compounds as potential adjunctive modulators within emerging, experimental liver rejuvenation strategies, including partial cellular reprogramming approaches that require coordinated metabolic and epigenetic control. While acknowledging that direct reversal of liver aging remains to be clinically established, integrating marine chemodiversity with contemporary aging and regenerative biology outlines a conceptual roadmap for developing liver-directed interventions targeting aging-related vulnerability as a fundamental driver of disease.

The increasing prevalence of pharmaceutical residues in coastal ecosystems represents a critical challenge for the health of marine organisms, which are frequently exposed to complex contaminant mixtures. This study investigated the toxicological effects of single and combined exposure to Acetylsalicylic Acid (ASA, 0.1&#xa0;&#x3bc;g/L) and Dexamethasone (DESA, 4&#xa0;ng/L) in the marine bivalve Mytilus galloprovincialis over a 14-day period. A multi-tier approach was adopted, integrating transcriptional expression, biochemical markers, and histopathological analysis. Due to the functional relevance of the target tissues, molecular and biochemical responses were assessed in pooled gill and digestive gland samples, while structural alterations were evaluated separately via histology. Individual exposures triggered moderate antioxidant responses and localized molecular shifts; however, combined ASA&#xa0;+&#xa0;DESA exposure resulted in pronounced alterations. This group was characterized by a coordinated modulation of detoxification-related genes (abcb, cyp4y1), a reduction in Total Antioxidant Capacity (TAC), and changes in the expression of genes associated with apoptotic processes (casp-2 and casp-8). These biochemical shifts were associated with structural changes, including lamellar hyperplasia in the gills and tubular atrophy in the digestive gland. Principal Component Analysis (PCA) confirmed that the co-exposure group represents a distinct toxicological phenotype, primarily driven by lipid peroxidation and markers of metabolic strain. While further research is needed to formally define the nature of the interaction, these findings indicate that the combined presence of non-steroidal anti-inflammatory drugs and glucocorticoids can significantly alter the physiological homeostasis of marine mussels. The study underscores the importance of considering the cumulative impact of pharmaceutical cocktails in environmental risk assessments for coastal environments.

Antarctica hosts a highly endemic and diverse benthic marine fauna. Despite this biodiversity, the Antarctic marine food web remains structurally simple, rendering the ecosystem particularly vulnerable to environmental stressors. Benthic organisms, due to their sedentary nature, long lifespans, and close interaction with the sediment-water interface, are widely regarded as effective sentinels of ecological change. In this study, we extended a previously validated QuEChERS-based extraction protocol, originally developed for Adamussium colbecki organisms, to assess its applicability across additional Antarctic benthic taxa, including Sphaerotylus antarcticus, Odontaster validus, Trematomus bernacchii, and Laternula elliptica. The extraction method was used in combination with LC-MS/MS analysis for the determination of emerging contaminants in both targeted and suspect screening modes. Method performance was evaluated for 23 targeted emerging contaminants (ECs), yielding recovery rates of 58-116% and matrix effects between 62 and 108% for most compounds, confirming the method's suitability for taxonomically diverse matrices. Samples collected during Antarctic expeditions from 2018 to 2022 revealed the presence of multiple ECs, including perfluorooctanoic acid (PFOA), caffeine, pharmaceuticals and personal care products (PPCPs), and UV filters. Complementarily, a preliminary suspect screening via high-resolution mass spectrometry was attempted, revealing the potential presence of a broader spectrum of drugs, PPCPs, and lifestyle-related compounds in all studied species. This work represents one of the first applications of a QuEChERS-based analytical framework for ECs detection in Antarctic marine fauna, offering a reliable approach for long-term contaminant monitoring in one of the planet's most fragile ecosystems.

Geodia cydonium, a sponge belonging to Demospongiae and endemic species to the Mediterranean Sea, is capturing increasing attention due to its rich and chemically diverse metabolome. Previous studies reported the presence of sterols, alkaloids, polyketides, and glycosaminoglycans within this species, some of which exhibit notable antioxidant, immunomodulatory and antiproliferative effects. In this study, extraction procedure of bioactive metabolites from G. cydonium (Linnaeus, 1767) was optimised. The methanolic extract showed a cytotoxic activity and was purified using chromatographic techniques. Kynurenic acid was isolated for the first time from this sponge and identified by spectroscopic methods (1H-NMR and ESI-MS). Furthermore, a mixture of heteroatom-containing metabolites was also obtained. The cytotoxic activity of the isolated compounds was evaluated using in vitro assays on melanoma cell lines. Our findings contribute to the growing repository of marine natural products with anticancer activity but also underlined the significance of marine biodiversity as a reservoir for drug discovery for melanoma therapy.

The skin serves as the first line barrier of innate immunity, protecting the body from external influences and maintaining its homeostasis. Exogenous and endogenous stress factors alter the structure and functional properties of the skin. The search for compounds capable of counteracting these processes has allowed the identification of peptides as promising ingredients of products for medicinal and cosmetic applications. This review comprehensively examines the mechanisms of action and dermatological applications of two distinct classes of natural products-endogenous human peptides and those derived from marine organisms. Human peptides exhibit numerous biological functions, including antimicrobial and immunomodulatory ones, as well as promoting antioxidant protection and wound healing. Microbiome-associated peptides are an underestimated but powerful regulator of skin aging through immunomodulation, inflammation control, barrier function maintenance, and selection of the proper microbial community. Peptides from marine organisms exhibit significant structural diversity and a broad spectrum of biological activity, including regenerative effects and effects on antibiotic-resistant microorganisms. This review summarizes current data obtained from in vitro, ex vivo, and clinical studies demonstrating a broad potential of peptides for maintaining skin health. Both peptide classes represent powerful, targeted strategies for innovative dermatological interventions aimed at promoting skin rejuvenation, protection, and overall homeostasis.

Fungal infections are a significant contributor to global morbidity and mortality, among which Candida albicans infections, a major cause of systemic candidiasis, have a mortality rate of approximately 40%. Developing effective and safe antifungal drugs with novel chemical scaffolds is urgently needed. In this study, more than 200 fungi from a deep-sea-derived fungal library were screened for anti-C. albicans activity, and a fungus Aspergillus candidus (CHNSCLM-1227) strain with strong activity was discovered. Using anti-C. albicans activity screening combined with LC-MS/MS-based molecular networking, six natural flavones (1-6) were identified, and among them, chlorflavonin (1) showed strong activity with an MIC value of 0.625&#x202f;&#x3bc;g/mL. Guided by its activity and based on a diversified derivatization strategy, a total of 52 derivatives (7-58) were designed. Notably, a chlorinated flavone derivative, CHNQD-02204 (44) showed remarkable and selective in vitro antifungal activity against C. albicans, along with high safety (MIC&#x202f;=&#x202f;0.025&#x202f;&#x3bc;g/mL, SI&#x202f;>&#x202f;1000). Mechanically, CHNQD-02204 (44) inhibited ergosterol production, thereby damaging the integrity of the fungal cell membrane and hindering the normal growth of C. albicans. It also prevented biofilm formation and morphological changes in cells. Moreover, CHNQD-02204 (44) exhibited excellent therapeutic efficacy in a murine model of systemic candidiasis (2.5&#x202f;mg/kg, i.v., bid) and demonstrated high safety. These findings warrant further pharmaceutical exploration of the promising potential of CHNQD-02204 (44), a novel antifungal agent, for combating C. albicans infections.

Seven new sesquiterpenes, named penicipenoids A-G (1-7), were isolated from rice-based fermentation cultures of the marine sponge-derived fungus Penicillium sp. 5975, together with ten known analogues (8-17). Their structures were elucidated using high-resolution mass spectrometry (HR-MS) and nuclear magnetic resonance (NMR) spectroscopy, supported by single-crystal X-ray diffraction analysis and electronic circular dichroism (ECD) calculations. Penicipenoid A (1) features an unprecedented sesquiterpene scaffold characterized by a tricyclo[4.4.11,602,7]hendecane core. Penicipenoid D (4) contains an unusual furan substructure within the cadinane-type sesquiterpenoid class, while penicipenoid F (6) represents a rare norsesquiterpene derivative lacking the carbon atom at the C-7 position. The in vivo anti-oxidant and anti-inflammatory effects of these compounds were evaluated using transgenic fluorescent zebrafish models. Penicipenoids A-C (1-3) exhibited anti-oxidant activity in metronidazole (MTZ)-treated transgenic zebrafish embryos, whereas penicipenoid E (5) demonstrated potent anti-inflammatory activity in CuSO4-induced transgenic fluorescent zebrafish embryos.

Long-chain polyunsaturated fatty acids (LC-PUFAs) of omega-3 family, particularly docosahexaenoic acid and eicosapentaenoic acid, are essential nutrients that play a critical role in children's growth and health. This review examines the evidence on the effects of omega-3 supplements and omega-3-enhanced foods on children's development, as well as on neurological and metabolic disorders. Research consistently highlights the importance of DHA in brain and visual development, especially during early childhood, when rapid neural growth occurs. PubMed, Web of Science, Scopus and the Cochrane Library databases were searched for relevant articles published up to January 2026. Adequate omega-3 intake has been associated with improvements in cognitive performance, attention, and learning outcomes. In children with neurodevelopmental conditions such as attention-deficit/hyperactivity disorder and autism spectrum disorder, omega-3 supplementation shows modest but potential benefits in reducing behavioral symptoms and supporting executive function, although results remain mixed. Additionally, omega-3 fatty acids exhibit anti-inflammatory properties that may positively influence metabolic health, including lipid profiles, insulin sensitivity, and obesity-related risk factors in children. Omega-3-enhanced foods provide an alternative to supplements and may improve adherence and overall dietary quality. However, variability in dosage, study design, and baseline nutritional status limits definitive conclusions. Overall, omega-3 fatty acids appear to support healthy development and may aid in managing certain neurological and metabolic disorders in children.

Modern lifestyles expose humans to a dynamic and complex exposome that significantly influences overall health, including skin physiology [...].

The continuous emergence of SARS-CoV-2 variants highlights the need for novel antiviral agents with favorable safety profiles. Marine microalgae constitute a valuable source of bioactive compounds, including antiviral peptides. Building on previous in silico identification of peptides derived from the marine microalga Phaeodactylum tricornutum with predicted activity against SARS-CoV-2, this study evaluated the antiviral capacity of peptide fractions generated by enzymatic hydrolysis and separated by molecular weight (10-30, 5-10, 3-5, and <3 kDa) in human alveolar epithelial A549 cells infected with the SARS-CoV-2. Cytotoxicity analyses, assessed using MTT and resazurin assays, revealed a moderate, concentration-dependent reduction in metabolic activity while maintaining overall cell viability within an acceptable range for antiviral evaluation, with higher-molecular-weight fractions (10-30 and 5-10 kDa) displaying the most stable profiles. Antiviral activity was assessed by flow cytometry following post-infection treatment. Lower-molecular-weight fractions (3-5 and <3 kDa) showed early reductions in infection at low concentrations but exhibited variable responses. In contrast, the 10-30 and 5-10 kDa fractions showed more robust, dose-dependent inhibition at medium and high concentrations, reducing infection levels to levels close to those observed in uninfected controls. Comparative analysis with the reference antiviral drug lopinavir demonstrated that peptide fractions exhibit lower cytotoxicity while retaining antiviral activity under equivalent experimental conditions. Overall, these results indicate that antiviral efficacy is strongly influenced by peptide molecular weight and consistency of response. This work provides experimental in vitro validation of P. tricornutum-derived peptide fractions as marine antiviral candidates and supports the integration of in silico and functional approaches for marine drug discovery.

Marine pollution in the Mediterranean has far-reaching consequences for the marine environment, wildlife and human health. Emerging contaminants (ECs) and their metabolites are increasingly recognized as critical but underreported contributors to human chemical exposure through seafood. This study aimed to comprehensively identify ECs and their phase I&II metabolites in Mediterranean edible fish. A suspect screening analysis platform was developed based on supramolecular solvent extraction and liquid chromatography-high-resolution mass spectrometry. Identification was guided by a suspect list of 11,000 entries (1702 parent compounds and 9298 metabolites in silico generated for Phase I&II pathways). Method limits of detection ranged from 0.50 to 2.61&#x202f;ng&#xb7;g&#x207b;&#xb9;&#x202f;. The platform was applied to 120 Mediterranean fish specimens, including two demersal (Mullus barbatus and Merluccius merluccius) and two pelagic (Sardina pilchardus and Trachurus trachurus) species. 81 compounds were detected, spanning plasticizers, flame retardants, pesticides, pharmaceuticals & illicit drugs, personal care products, and industrial & others. About half of these compounds (41) were metabolites, with their parent compounds mostly absent. Notably, 20 of them were methylated derivatives, a transformation not typically associated with detoxification in fish metabolism, highlighting the need to elucidate their biotic/abiotic origin. Detection patterns revealed some ecological contrasts: Sardina pilchardus and Trachurus trachurus accumulated the broadest chemical spectrum, while Mullus barbatus reflected sediment-derived contamination and Merluccius merluccius had the lowest chemical burden. This study provides one of the most comprehensive suspect screening of ECs and their metabolites in Mediterranean fish to date, revealing novel contamination pathways and critical implications for human exposure.

The growing demand for clean-label food ingredients drives interest in novel marine flavorings. This study evaluated the physicochemical, antioxidant, volatile (GC-MS), and sensory profiles of freeze-dried powders from blue crab roe (Callinectes sapidus), sea urchin roe (Paracentrotus lividus), and beluga caviar (Huso huso) to assess their culinary potential. Results revealed that sensory quality is governed by the synergy between a matrix's lipid composition and endogenous antioxidant capacity. Sea urchin powder, possessing a low polyunsaturated fatty acid (PUFA) profile and high carotenoid content, exhibited exceptional oxidative stability, yielding a concentrated marine aldehyde signature and top consumer scores. Blue crab roe demonstrated a robust PUFA matrix buffered by high phenolic content, facilitating controlled lipid peroxidation into desirable savory volatiles (ketones and aldehydes). Conversely, the high-fat, monounsaturated-dominant beluga caviar lacked sufficient antioxidants, leading to lipid degradation, oxidized hydrocarbons, earthy off-flavors, and poor texture. Both crab and caviar powders exhibited favorable Atherosclerosis and Thrombogenicity indices. Ultimately, balancing lipid composition and endogenous antioxidants is crucial for flavor stability, highlighting the commercial and environmental potential of transforming underutilized or invasive species like blue crab into stable, nutrient-dense marine flavoring agents.

Attention-Deficit/Hyperactivity Disorder (ADHD), affecting 5-10% of children globally, faces treatment limitations due to adverse effects and uncertain long-term risks of current pharmacotherapies. This study investigated the therapeutic potential of sepia ink (SI), a marine-derived natural complex from cuttlefish, in a scopolamine-induced ADHD-like mouse model. The chemical constituents of SI were characterized via Ultra-Performance Liquid Chromatography-Mass Spectrometry (UPLC-MS). The behavioral assessments, histopathological examinations, flow cytometry, and complete blood counts were utilized to evaluate its effects on ADHD-like phenotypes, neuroinflammation, and immune function. Integrated transcriptomic, plasma metabolomic, and 16S rRNA sequencing were used to explore the underlying mechanisms. SI significantly alleviated hyperactivity and improved spatial learning and memory deficits. It reduced hippocampal neuronal damage, attenuated neuroinflammation, and reversed scopolamine-induced immunosuppression in spleen and thymus. SI also restored the balance of immune cell subsets in both mesenteric lymph nodes and spleen, and the peripheral blood cell counts. Multi-omics analyses suggested that the beneficial effects of SI were associated with reduced neuroinflammation, rebalanced systemic immune responses, partial correction of lipid metabolic disturbances, and restoration of gut microbiota homeostasis. Collectively, our findings indicate that SI effectively mitigates the in vivo ADHD-like impairments by coordinating immune, metabolic, and gut microbiota-related processes, thereby supporting its potential as a marine-derived therapeutic candidate for further ADHD treatment.

Given the established interplay between oxidative stress, cholinergic dysfunction, and metabolic imbalance in cognitive decline, this study investigated the multifunctional potential of three red macroalgae from the Madeira Archipelago (Asparagopsis taxiformis, Grateloupia lanceola, and Nemalion elminthoides) using a sequential biorefinery approach. Marine algae represent a sustainable source of functional food ingredients due to their rich content in bioactive compounds and their compatibility with low-impact production systems. Protein, ethanolic (phenolic-rich), and polysaccharide fractions were obtained through direct extraction and scalable biorefinery processing. Antioxidant activity was evaluated using ORAC, DPPH, FRAP, and FIC assays, while functionality relevant to human health was assessed through acetylcholinesterase, butyrylcholinesterase, and &#x3b1;-glucosidase inhibition. Protein extracts, particularly from N. elminthoides, exhibited strong hydrogen atom transfer-based antioxidant capacity, whereas ethanolic extracts demonstrated multifunctional activity, combining radical scavenging, metal chelation, and enzyme inhibition associated with neuroprotective and glycemic-regulation potential. Polysaccharide fractions contributed mainly to iron chelation and reducing capacity. Correlation analyses highlighted the complementary nature of antioxidant and bioactivity assays. Overall, these findings support the potential of Madeira red macroalgae as functional food ingredients and emphasize the importance of optimized biorefinery strategies to maximize nutritional and health-related benefits.

Human rhinovirus (HRV), first isolated in 1956, belongs to the family Picornaviridae. HRV causes mild cold and severe respiratory disease. To date, no FDA-approved antiviral or anti-inflammatory drugs are available. TA25 is a phenolic amide derivative extracted from Nicotiana tabacum. To investigate the potential candidate for antiviral therapeutics, we evaluated the antiviral potency of TA25 for HRV and multiple zoonotic viruses. The antiviral and anti-inflammatory effects were evaluated using RT-qPCR and RNA-seq. Strand-specific RT-qPCR was performed to measure genomic and anti-genomic RNA expression after TA25 treatment. In addition, an AI-based docking test was conducted to investigate the binding affinity of TA25 with viral proteins. TA25 induced significant reduction in viral replication and suppressed the expression of pro-inflammatory genes. Inhibition of viral replication by TA25 treatment was confirmed by strand-specific RT-qPCR. TA25 showed broad-spectrum antiviral activity against multiple viruses, including HRV-1A, ZIKV, DENV, VACV, and IBV. Using AI-driven structure-based docking analysis, TA25 showed strongest binding affinity with HRV 2B protein. This study demonstrates that TA25 confers the broad antiviral and anti-inflammatory activity against HRV and multiple zoonotic viruses. These findings provide valuable insights into antiviral strategies of TA25 for a promising therapeutic candidate in response to emerging RNA and DNA viruses.

Sulfated polysaccharides (SPs), biologically active macromolecules from marine and terrestrial organisms, hold significant potential in revolutionizing cancer therapy. Characterized by their unique sulfate ester groups and structural diversity, SPs exhibit a broad spectrum of bioactivities, including immunomodulation, apoptosis induction, metastasis suppression, and angiogenesis inhibition. Prominent SPs, such as fucoidan from brown algae and carrageenan from red algae, have shown remarkable anticancer properties, either as standalone agents or in synergy with conventional therapies like chemotherapy and radiotherapy. Their mechanisms of action involve targeting critical pathways such as NF-kB, VEGF, and PI3K/Akt, disrupting cancer cell proliferation, invasion, and tumor microenvironment dynamics. SPs also enhance immune system responses, reduce chemotherapy-induced side effects, and exhibit antioxidant properties, making them versatile candidates in cancer treatment. Innovations like SP-based nanoparticles are addressing bioavailability and drug delivery challenges, providing targeted and sustained therapeutic effects while minimizing off-target toxicity. Despite their promise, challenges such as structural complexity, scalability, and clinical validation hinder their widespread adoption. This review provides a comprehensive analysis of SPs' therapeutic potential, mechanisms, and emerging applications in oncology. It emphasizes the need for advanced extraction, characterization techniques, and clinical research to unlock their full potential, paving the way for novel, efficient, and safer cancer therapies.

Secondary metabolism in Streptomyces is subjected to complex regulation. Compared to regulations on the transcriptional level, our knowledge of those on the post-translational level remains limited. Here, we identify a Gcn5-related N-acetyltransferase, SyPmatA, in the marine-derived Streptomyces youssoufiensis OUC6819, which negatively affects the production of nigericin, a polyether ionophore antibiotic with antifungal and antiparasitic activities. Inactivation of syPmatA enhanced the nigericin yield by 5.2-fold. Using in vitro and in vivo assays, we demonstrate that SyPmatA specifically catalyzes malonylation of P450 NigDSy at K224, negatively modulating its function. Overexpression of nigDSyK224R (mimicking demalonylation) in the &#x394;syPmatA mutant further increased nigericin production. Fermentation optimization and scale-up in a 5L-bioreactor using the engineered strain &#x394;syPmatA/nigDsyK224R achieved a final titer of 444.5 mg/L, representing a 61.9-fold improvement over the wild-type strain. Our findings reveal a novel lysine malonylation-mediated regulatory mechanism in nigericin biosynthesis and highlight the potential of targeting post-translational modification enzymes for metabolic engineering.