Marine Drugs最新文献

Carrageenan oligosaccharides (COSs) possess versatile activities and have drawn increasing attention in recent years. Due to their unique structures, COSs have been considered to be potential antibacterial agents and immune stimulators. Herein, we aimed to efficiently prepare the COSs by using a novel carrageenase CgkA from Zobellia uliginosa with high activity and further investigate the effects of dietary supplementation with COSs on the growth performance, serum biochemical parameters and non-specific immunity in Carassius auratus gibelio. The results indicated that the CgkA could effectively degrade the carrageenan into oligosaccharides with DPs of 2-6 and the oligosaccharides exhibited promoting effects on growth performance, serum biochemical index and non-specific immune parameters. After a 6-month feeding trial, the SR (Survival Ratio) was significantly higher in fish fed 0.1% (Diet 1), 0.2% (Diet 2), 0.5% (Diet 3) and 1% (Diet 4) COSs diets than that in the control group (p < 0.05). In addition, the supplementation of COSs decreased the malondialdehyde (MDA) content in the serum and increased the activity of lysozyme (LZM), superoxide dismutase (SOD) and catalase (CAT). In conclusion, COSs as a dietary supplement enhance the growth performance and non-specific immunity of crucian carp and their resistance to diseases.

Over the last decades, bioprospecting of tropical corals has revealed numerous bioactive compounds with potential for biotechnological applications. However, this search involves sampling in natural reefs, and this is currently hampered by multiple ethical and technological constraints. Living coral displays, research laboratories, and biobanks currently offer an opportunity to continue to unravel coral chemodiversity, acting as "Noah's Arks" that may continue to support the bioprospecting of molecules of interest. This issue is even more relevant if one considers that tropical coral reefs currently face unprecedent threats and irreversible losses that may impair the biodiscovery of molecules with potential for new products, processes, and services. Living coral displays provide controlled environments for studying corals and producing both known and new metabolites under varied conditions, and they are not prone to common bottlenecks associated with bioprospecting in natural coral reefs, such as loss of the source and replicability. Research laboratories may focus on a particular coral species or bioactive compound using corals that were cultured ex situ, although they may differ from wild conspecifics in metabolite production both in quantitative and qualitative terms. Biobanks collect and preserve coral specimens, tissues, cells, and/or information (e.g., genes, associated microorganisms), which offers a plethora of data to support the study of bioactive compounds' mode of action without having to cope with issues related to access, standardization, and regulatory compliance. Bioprospecting in these settings faces several challenges and opportunities. On one hand, it is difficult to ensure the complexity of highly biodiverse ecosystems that shape the production and chemodiversity of corals. On the other hand, it is possible to maximize biomass production and fine tune the synthesis of metabolites of interest under highly controlled environments. Collaborative efforts are needed to overcome barriers and foster opportunities to fully harness the chemodiversity of tropical corals before in-depth knowledge of this pool of metabolites is irreversibly lost due to tropical coral reefs' degradation.

Fusarium wilt of banana (FWB), caused by Fusarium oxysporum f. sp. cubense (Foc) tropical race 4 (TR4), poses a severe threat to the global banana industry. The screening of endophytic fungi from the mangrove plant led to the identification of Medicopsis sp. SCSIO 40440, which exhibited potent antifungal activity against Fusarium. The further fraction of the extract yielded ten compounds, including MK8383 (1) and nine new analogues, MK8383s B-J (2-10). The structures of 1-10 were elucidated using extensive spectroscopic data and single-crystal X-ray diffraction analysis. In vitro antifungal assays revealed that 1 showed strongly antifungal activities against Foc TR4, with an EC₅₀ of 0.28 μg/mL, surpassing nystatin and hygromycin B (32 and 16 μg/mL, respectively). Pot experiments showed that 1 or spores of SCSIO 40440 could significantly reduce the virulence of Foc TR4 on Cavendish banana.

Marine phytoplankton is an emerging source of immunomodulatory bioactive lipids (BLs). Under physiological growth conditions and upon stress challenges, several eukaryotic microalgal species accumulate lipid metabolites that resemble the precursors of animal mediators of inflammation: eicosanoids and prostaglandins. Therefore, marine phytoplankton could serve as a biotechnological platform to produce functional BLs with therapeutic applications in the management of chronic inflammatory diseases and other clinical conditions. However, to be commercially competitive, the lipidic precursor yields should be enhanced. Beside tailoring the cultivation of native producers, genetic engineering is a feasible strategy to accrue the production of lipid metabolites and to introduce heterologous biosynthetic pathways in microalgal hosts. Here, we present the state-of-the-art clinical research on immunomodulatory lipids from eukaryotic marine phytoplankton and discuss synthetic biology approaches to boost their light-driven biosynthesis.

Seven new (1-7) and six known (8-13) statin derivatives were obtained from the deep-sea-derived fungus Penicillium viridicatum MCCC 3A00265. The structures assigned to the new compounds were based on a comprehensive analysis of the spectroscopic data, with absolute configurations established by Mosher analysis and biogenetic consideration. Most of the new compounds (1-5 and 7) share an octohydronaphthalene backbone, except that viridecalin F (6) possesses an uncommon naphthalene core. Viridecalins C (3) and F (6) and the two known compounds 9 and 11 exhibit considerable ability in reactivating mutant p53 protein at 10 μM, while viridecalin C showcases the most potent reactivation activity, indicating the potential of application in cancer therapy.

Sea anemone peptides represent a valuable class of biomolecules in the marine toxin library due to their various structures and functions. Among these, ShK domain peptides are particularly notable for their selective inhibition of the Kv1.3 channel, holding great potential for applications in immune regulation and the treatment of metabolic disorders. However, these peptides' structural complexity and diversity have posed challenges for functional prediction. In this study, we compared 36 ShK domain peptides from four species of sea anemone in the South China Sea and explored their binding ability with Kv1.3 channels by combining molecular docking and dynamics simulation studies. Our findings highlight that variations in loop length, residue composition, and charge distribution among ShK domain peptides affect their binding stability and specificity. This work presents an efficient strategy for large-scale peptide structure prediction and activity screening, providing a valuable foundation for future pharmacological research.

Background: Bipolar disorder is a chronic mental disease that is characterized by depressive and manic episodes. Antipsychotics and mood stabilizers are known therapies that work, but their restrictions and disadvantages resulted in the need for complementary and alternative therapies, such as natural compounds. Omega-3 fatty acids, as basic ingredients of fishes and seafood, play crucial roles in brain development, function of brain membrane enzymes, learning, and many other instances, and their deficiency has been associated with many mental diseases, including bipolar disorder.

Methods: The present narrative review aims to critically summarize and scrutinize the available clinical studies on the use of omega-3 fatty acids in the management and co-treatment of bipolar disorder episodes and symptoms. For this purpose, a thorough and in-depth search was performed in the most accurate scientific databases, e.g., PubMed., Scopus, Web of Science, Cochrane, Embase, and Google Scholar, applying effective and relevant keywords.

Results: There are currently several clinical studies that assessed the effect of omega-3 fatty acids on the severity of BD symptoms. Some of them supported evidence for the potential beneficial impact of omega-3 fatty acids supplementation in the prevention and/or co-treatment of bipolar disorder severity and symptomatology. Nevertheless, a considerable number of clinical studies did not show high efficiency, rendering the existing data rather conflicting. The above may be ascribed to the fact that there is a high heterogeneity amongst the available clinical studies concerning the dosage, the administration duration, the combination of fatty acids administration, the method designs and protocols, and the study populations.

Conclusion: Although the currently available clinical evidence seems promising, it is highly recommended to accomplish larger, long-term, randomized, double-blind, controlled clinical trials with a prospective design in order to derive conclusive results as to whether omega-fatty acids could act as a co-treatment agent or even as protective factors against bipolar disorder symptomatology. Drug design strategies could be developed to derive novel synthetic omega-3 fatty acids analogs, which could be tested for their potential to attenuate the severity of BD episodes and symptoms.

The cosmeceutical industry has increasingly turned its attention to marine macroalgae, recognizing their significant bioactive potential as sources of natural compounds for skincare applications. A growing number of products now incorporate extracts or isolated compounds from various macroalgae species. However, many species remain underexplored, highlighting a valuable opportunity for further research. Among these, Caulerpa prolifera (Forsskål) J.V. Lamouroux has emerged as a promising candidate for cosmeceutical applications. This study provides the most comprehensive phytochemical assessment of C. prolifera to date, revealing its potential as a source of bioactive extracts and compounds. The analysis identified key components of its lipophilic profile, predominantly saturated and unsaturated fatty acids, alongside di-(2-ethylhexyl) phthalate-an endocrine disruptor potentially biosynthesized or bioaccumulated by the algae. While the crude extract exhibited moderate tyrosinase inhibitory activity, its overall antioxidant capacity was limited. Fractionation of the extract, however, yielded subfractions with distinct bioactivities linked to changes in chemical composition. Notably, enhanced inhibitory activities against elastase and collagenase were observed in subfractions enriched with 1-octadecanol and only traces of phthalate. Conversely, antioxidant activity diminished with the loss of specific compounds such as β-sitosterol, erucic acid, nervonic acid, and lignoceric acid. This work advances the understanding of the relationship between the chemical composition of C. prolifera and its bioactivities, emphasizing its potential as a source of cosmeceutical ingredients, leading to a more comprehensive valorization of this macroalga.

Fish body mucus plays a protective role, especially in Halobatrachus didactylus, which inhabits intertidal zones vulnerable to anthropogenic contaminants. In silico predicted bioactive peptides were identified in its body mucus, namely, EDNSELGQETPTLR (HdKTLR), DPPNPKNL (HdKNL), PAPPPPPP (HdPPP), VYPFPGPLPN (HdVLPN), and PFPGPLPN (HdLPN). These peptides were studied in vitro for bioactivities and aggregation behavior under different ionic strengths and pH values. Size exclusion chromatography revealed significant peptide aggregation at 344 mM and 700 mM ionic strengths at pH 7.0, decreasing at pH 3.0 and pH 5.0. Although none exhibited antimicrobial properties, they inhibited Pseudomonas aeruginosa biofilm formation. Notably, HdVLPN demonstrated potential antioxidant activity (ORAC: 1.560 μmol TE/μmol of peptide; ABTS: 1.755 μmol TE/μmol of peptide) as well as HdLPN (ORAC: 0.195 μmol TE/μmol of peptide; ABTS: 0.128 μmol TE/μmol of peptide). Antioxidant activity decreased at pH 5.0 and pH 3.0. Interactions between the peptides and mucus synergistically enhanced antioxidant effects. HdVLPN and HdLPN were non-toxic to Caco-2 and HaCaT cells at 100 μg of peptide/mL. HdPPP showed potential antihypertensive and antidiabetic effects, with IC₅₀ values of 557 μg of peptide/mL for ACE inhibition and 1700 μg of peptide/mL for α-glucosidase inhibition. This study highlights the importance of validating peptide bioactivities in vitro, considering their native environment (mucus), and bioprospecting novel bioactive molecules while promoting species conservation.

Background: Hypertension has been identified as a significant risk factor for cardiovascular disease. Given the prevalence of the adverse effects of angiotensin-converting enzyme-inhibitory (ACEI) drugs, natural and effective alternatives to these medications need to be identified.

Methods: An investigative study was conducted to assess the ACEI capacity and structural characteristics of enzymatic hydrolysates with varying molecular weights derived from squid skin. The amino acid sequences of the enzymatic digests were analyzed via Nano LC-MS/MS and screened for peptides with ACEI activity using an in silico analysis. Furthermore, molecular docking was employed to investigate the interaction between potential ACEI peptides and ACE.

Results: TPSH-V (MW < 1 kDa) exhibited the highest rate of ACEI, a property attributable to its substantial hydrophobic amino acid content. Additionally, TPSH-V exhibited high temperature and pH stability, indicative of regular ordering in its secondary structure. The binding modes of four potential novel ACEI peptides to ACE were predicted via molecular docking with the sequences of FHGLPAK, IIAPPERKY, RGLPAYE, and VPSDVEF, all of which can bind to the ACE active site via hydrogen bonding, with FHGLPAK, RGLPAYE, and VPSDVEF being able to coordinate with Zn²⁺.

Conclusions: Squid skin constitutes a viable resource for the production of ACEI peptides.