Marine Drugs

11 pages, 2492 KiB

Open AccessArticle

Lichenase and Cellobiohydrolase Activities of a Novel Bi-Functional β-Glucanase from the Marine Bacterium Streptomyces sp. J103

by Youngdeuk Lee, Eunyoung Jo, Yeon-Ju Lee, Min Jin Kim, Navindu Dinara Gajanayaka, Mahanama De Zoysa, Gun-Hoo Park and Chulhong Oh

Mar. Drugs 2024, 22(12), 558; https://doi.org/10.3390/md22120558 - 13 Dec 2024

Abstract

In this study, we report the molecular and enzymatic characterisation of Spg103, a novel bifunctional β-glucanase from the marine bacterium Streptomyces sp. J103. Recombinant Spg103 (rSpg103) functioned optimally at 60 °C and pH 6. Notably, Spg103 exhibited distinct stability properties, with increased activity [...] Read more.

In this study, we report the molecular and enzymatic characterisation of Spg103, a novel bifunctional β-glucanase from the marine bacterium Streptomyces sp. J103. Recombinant Spg103 (rSpg103) functioned optimally at 60 °C and pH 6. Notably, Spg103 exhibited distinct stability properties, with increased activity in the presence of Na+ and EDTA. Spg103 displays both lichenase and cellobiohydrolase activity. Despite possessing a GH5 cellulase domain, FN3 and CBM3 domains characteristic of cellulases and CBHs, biochemical assays showed that rSpg103 exhibited higher activity towards mixed β-1,3-1,4-glucan such as barley β-glucan and lichenan than towards beta-1,4-linkages. The endolytic activity of the enzyme was confirmed by TLC and UPLC-MS analyses, which identified cellotriose as the main hydrolysis product. In addition, Spg103 exhibited an exo-type activity, selectively releasing cellobiose units from cellooligosaccharides, which is characteristic of cellobiohydrolases. These results demonstrate the potential of Spg103 for a variety of biotechnological applications, particularly those requiring tailor-made enzymatic degradation of mixed-linked β-glucans. This study provides a basis for further structural and functional investigations of the bifunctional enzyme and highlights Spg103 as a promising candidate for industrial applications. Full article

(This article belongs to the Special Issue Advances of Marine-Derived Enzymes)

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13 pages, 2327 KiB

Open AccessArticle

Fucosterol, a Phytosterol of Marine Algae, Attenuates Immobilization-Induced Skeletal Muscle Atrophy in C57BL/6J Mice

by Jieun Hwang, Mi-Bo Kim, Sanggil Lee and Jae-Kwan Hwang

Mar. Drugs 2024, 22(12), 557; https://doi.org/10.3390/md22120557 - 12 Dec 2024

Abstract

The objective of this study was to examine whether fucosterol, a phytosterol of marine algae, could ameliorate skeletal muscle atrophy in tumor necrosis factor-alpha (TNF-α)-treated C2C12 myotubes and in immobilization-induced C57BL/6J mice. Male C57BL6J mice were immobilized for 1 week to induce skeletal [...] Read more.

The objective of this study was to examine whether fucosterol, a phytosterol of marine algae, could ameliorate skeletal muscle atrophy in tumor necrosis factor-alpha (TNF-α)-treated C2C12 myotubes and in immobilization-induced C57BL/6J mice. Male C57BL6J mice were immobilized for 1 week to induce skeletal muscle atrophy. Following immobilization, the mice were administrated orally with saline or fucosterol (10 or 30 mg/kg/day) for 1 week. Fucosterol significantly attenuated immobilization-induced muscle atrophy by enhancing muscle strength, with a concomitant increase in muscle volume, mass, and myofiber cross-sectional area in the tibialis anterior (TA) muscle in mice. In both the TNF-α-treated C2C12 myotubes and the TA muscle of immobilized mice, fucosterol significantly prevented muscle protein degradation, which was attributed to a reduction in atrogin-1 and muscle ring finger 1 gene expression through an increase in forkhead box O3α (FoxO3α) phosphorylation. Continuously, fucosterol stimulated muscle protein synthesis by increasing the phosphorylation of the mammalian target of the rapamycin (mTOR), 70 kDa ribosomal protein S6 kinase, and 4E binding protein 1, which was mediated through the stimulation of the phosphatidylinositol 3-kinase (PI3K)/Akt signaling pathway. Thus, fucosterol alleviated skeletal muscle atrophy in TNF-α-treated C2C12 myotubes and immobilized C57BL/6J mice through the regulation of the Akt/mTOR/FoxO3α signaling pathway. Full article

(This article belongs to the Special Issue High-Value Compounds from Marine Algae)

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24 pages, 1964 KiB

Open AccessArticle

Detection of the Cyclic Imines Pinnatoxin G, 13-Desmethyl Spirolide C and 20-Methyl Spirolide G in Bivalve Molluscs from Great Britian

by Ryan P. Alexander, Alison O’Neill, Karl J. Dean, Andrew D. Turner and Benjamin H. Maskrey

Mar. Drugs 2024, 22(12), 556; https://doi.org/10.3390/md22120556 - 12 Dec 2024

Abstract

Harmful algal biotoxins in the marine environment are a threat to human food safety due to their bioaccumulation in bivalve shellfish. Whilst official control monitoring provides ongoing risk management for regulated toxins in live bivalve molluscs, no routine monitoring system is currently in [...] Read more.

Harmful algal biotoxins in the marine environment are a threat to human food safety due to their bioaccumulation in bivalve shellfish. Whilst official control monitoring provides ongoing risk management for regulated toxins in live bivalve molluscs, no routine monitoring system is currently in operation in the UK for other non-regulated toxins. To assess the potential presence of such compounds, a systematic screen of bivalve shellfish was conducted throughout Great Britain. A rapid dispersive methanolic extraction was used with UHPLC-MS/MS analysis to test for fifteen cyclic imines and seven brevetoxins in 2671 shellfish samples taken from designated shellfish harvesting areas around Great Britian during 2018. Out of the 22 toxins incorporated into the method, only pinnatoxin G, 13-desmethyl spirolide C and 20-methyl spirolide G were detected, with maximum concentrations of 85.4 µg/kg, 13.4 µg/kg and 51.4 µg/kg, respectively. A follow up study of pinnatoxin G-positive samples examined its potential esterification to fatty acids and concluded that following hydrolysis, pinnatoxin G concentration increased by an average of 8.6%, with the tentative identification of these esters determined by LC-HRMS. This study highlights the requirement for ongoing monitoring of emerging threats and the requirement for toxicological and risk assessment studies. Full article

(This article belongs to the Special Issue Marine Biotoxins 3.0)

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18 pages, 4799 KiB

Open AccessArticle

Transgenic Schizochytrium as a Promising Oral Vaccine Carrier: Potential Application in the Aquaculture Industry

by Ke Ma, Lei Deng, Yuanjie Wu, Yuan Gao, Jianhua Fan and Haizhen Wu

Mar. Drugs 2024, 22(12), 555; https://doi.org/10.3390/md22120555 - 12 Dec 2024

Abstract

Schizochytrium limacinum SR21, a kind of eukaryotic heterotrophic organism rich in unsaturated fatty acids, is an emerging microbial alternative to fish oil. The dietary inclusion of 15% SR21 was optimal for the growth performance of zebrafish. Previous studies demonstrated that fructose-1,6-bisphosphate aldolase (FBA) [...] Read more.

Schizochytrium limacinum SR21, a kind of eukaryotic heterotrophic organism rich in unsaturated fatty acids, is an emerging microbial alternative to fish oil. The dietary inclusion of 15% SR21 was optimal for the growth performance of zebrafish. Previous studies demonstrated that fructose-1,6-bisphosphate aldolase (FBA) of Edwardsiella tarda is a valuable broad-spectrum antigen against various pathogens in aquaculture (e.g., Aeromonas hydrophila, Vibro anguillarum, Vibro harveyi, Vibro alginolyticus). We pioneered the development of stable S. limacinum SR21 transformants expressing the antigen protein FBA, exploring their potential as a novel oral vaccine for the aquaculture industry. The model animal zebrafish (Danio rerio) and ornamental fish koi carp (Cyprinus carpio koi) were harnessed to assess the immunoprotective effect, respectively. According to the quantitative expression analysis, zebrafish fed with recombinant Schizochytrium expressing FBA exhibited specific immune responses in the intestine. The expression levels of MHC-I and MHC-II, involved in cell-mediated adaptive immune responses, were significantly upregulated on the 14th and 28th days post-immunization. Additionally, the expression of highly specialized antibody genes IgZ1 and IgZ2 in mucosal immunity were significantly triggered on the 14th day post-immunization. Feeding koi carp with recombinant S. limacinum SR21-FBA increased the production of myeloperoxidase and FBA-specific antibodies in the sera. Furthermore, the sera of koi fed with recombinant S. limacinum SR21-FBA exhibited significant bactericidal activities against pathogen E. tarda. Thus, S. limacinum SR21 is a natural and highly promising oral vaccine carrier that not only provides essential nutrients as a functional feed ingredient but also offers specific immune protection to aquatic animals. This dual application is vital for promoting the sustainable development of the aquaculture industry. Full article

(This article belongs to the Section Marine Pharmacology)

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44 pages, 2640 KiB

Open AccessReview

Shrimp Lipid Bioactives with Anti-Inflammatory, Antithrombotic, and Antioxidant Health-Promoting Properties for Cardio-Protection

by Paschalis Cholidis, Dimitrios Kranas, Aggeliki Chira, Evangelia Aikaterini Galouni, Theodora Adamantidi, Chryssa Anastasiadou and Alexandros Tsoupras

Mar. Drugs 2024, 22(12), 554; https://doi.org/10.3390/md22120554 - 11 Dec 2024

Abstract

Marine animals, especially shrimp species, have gained interest in research, due to the fact that they contain a plethora of biomolecules, specifically lipids, which have been proven to possess many health benefits in various diseases linked to chronic inflammation or other exogenous factors. [...] Read more.

Marine animals, especially shrimp species, have gained interest in research, due to the fact that they contain a plethora of biomolecules, specifically lipids, which have been proven to possess many health benefits in various diseases linked to chronic inflammation or other exogenous factors. This review refers to the lipid composition of a large number of shrimp species, as well as the effects that can alternate the lipid content of these crustaceans. Emphasis is given to the potent anti-inflammatory, antioxidant, and antithrombotic properties of shrimp bioactives, as well as the effects that these bioactives hold in other diseases, such as cancer, diabetes, neurodegenerative disorders, and more. The various health-promoting effects deriving from the consumption of shrimp lipid bioactives and the usage of products containing shrimp lipid extracts are also addressed in this study, through the exploration of several mechanisms of action and the interference of shrimp lipids in these biochemical pathways. Nevertheless, further research on this cultivatable edible species is needed, due to their existing limitations and future prospects which are discussed in this paper. Full article

(This article belongs to the Special Issue Marine-Derived Compounds Applied in Cardiovascular Disease)

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13 pages, 3180 KiB

Open AccessArticle

Two New Diterpenoids Formed by Transannular Diels–Alder Cycloaddition from the Soft Coral Sarcophyton tortuosum, and Their Antibacterial and PPAR-β Agonist Activities

by Min Sun, Songwei Li, Jianang Zeng, Yuewei Guo, Changyun Wang and Mingzhi Su

Mar. Drugs 2024, 22(12), 553; https://doi.org/10.3390/md22120553 - 10 Dec 2024

Abstract

Two new cembrane-derived tricyclic diterpenes belonging to the sarcophytin family, namely 4a-hydroxy-chatancin (1) and sarcotoroid (2), together with two known related ones (3 and 4), were isolated from the soft coral Sarcophyton tortuosum collected off [...] Read more.

Two new cembrane-derived tricyclic diterpenes belonging to the sarcophytin family, namely 4a-hydroxy-chatancin (1) and sarcotoroid (2), together with two known related ones (3 and 4), were isolated from the soft coral Sarcophyton tortuosum collected off Ximao Island in the South China Sea. The structures of the new compounds were elucidated by extensive spectroscopic analysis, a quantum mechanical nuclear magnetic resonance (QM-NMR) method, a time-dependent density functional theory electronic circular dichroism (TDDFT-ECD) calculation, X-ray diffraction analysis, and comparison with the reported data in the literature. A plausible biosynthetic pathway of compounds 1–4 was proposed, involving undergoing a transannular Diels–Alder cycloaddition. In the bioassay, the new compound 1 displayed significant inhibitory activities against the fish pathogens Streptococcus parauberis KSP28, oxytetracycline-resistant Streptococcus parauberis SPOF3K, and Photobacterium damselae FP2244, with MIC values of 9.1, 9.1, and 18.2 μg/mL, respectively. Furthermore, by conducting a luciferase reporter assay on rat liver Ac2F cells, compounds 1, 3, and 4 were evaluated for peroxisome proliferator-activated receptor (PPAR) transcriptional activity, and compound 3 showed selective PPAR-β agonist activity at a concentration of 10 μΜ. Full article

(This article belongs to the Special Issue Bioactive Compounds from Soft Corals and Their Derived Microorganisms)

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19 pages, 4015 KiB

Open AccessReview

Asteroid Saponins: A Review of Their Bioactivity and Selective Cytotoxicity

by Stuart J. Smith, Tianfang Wang and Scott F. Cummins

Mar. Drugs 2024, 22(12), 552; https://doi.org/10.3390/md22120552 - 7 Dec 2024

Abstract

Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e., sea cucumbers) is extensive, the class Asteroidea-derived saponins (i.e., seastars) [...] Read more.

Saponins are a diverse class of secondary metabolites that are often reported to exhibit a variety of pharmacological applications. While research into the elucidation and application of plant and class Holothuroidea-derived saponins (i.e., sea cucumbers) is extensive, the class Asteroidea-derived saponins (i.e., seastars) have been largely overlooked and primarily limited to elucidation. This review provides a comprehensive overview of the cytotoxic activities of asteroid-derived saponins against various cell cultures, for instance, mammalian erythrocytes, multiple microbial strains and cancer cell lines, including melanoma, breast, colon, and lung cancers. Highlighting the distinct structural variations in these saponins, this review examines their selective cytotoxicity and potency, with many demonstrating IC₅₀ values in the low micromolar range. Specific compounds, such as asterosaponins and polyhydroxylated saponins, exhibit noteworthy effects, particularly against melanoma and lung carcinoma cells, while triterpenoid saponins were found to be highly cytotoxic to both erythrocytes and fungal cells. This review also addresses gaps in the research area, including the need for additional in vitro antimicrobial studies, in vivo studies, and further exploration of their mechanisms of action. By consolidating recent findings, we have shed light on the therapeutic potential of asteroid-derived steroidal saponins in developing novel antimicrobial and anticancer agents. Full article

(This article belongs to the Special Issue Biologically Active Compounds from Marine Invertebrates 2025)

11 pages, 1779 KiB

Open AccessArticle

New Sesterterpenes from the Antarctic Sponge Suberites sp.

by Stine S. H. Olsen, Sydney K. Morrow, Julia L. Szabo, Michael N. Teng, Kim C. Tran, Charles D. Amsler, James B. McClintock and Bill. J. Baker

Mar. Drugs 2024, 22(12), 551; https://doi.org/10.3390/md22120551 - 6 Dec 2024

Abstract

Chemical investigation of the Antarctic sponge Suberites sp. has previously led to the identification of new suberitane derivatives, some of which show bioactivity toward respiratory syncytial virus (RSV). Our ongoing NMR-guided investigation of new specimens of the sponge resulted in the isolation of [...] Read more.

Chemical investigation of the Antarctic sponge Suberites sp. has previously led to the identification of new suberitane derivatives, some of which show bioactivity toward respiratory syncytial virus (RSV). Our ongoing NMR-guided investigation of new specimens of the sponge resulted in the isolation of five new analogs (1–5), previously reported suberitenones A–D (6–9), and oxaspirosuberitenone (10). Suberitenone K (1) was characterized as the 8-keto derivative of 6, while three new phenols, suberitandiol (2), abeosuberitandiol (3), and furanosuberitandiol (4), and the degraded sesterterpene norsuberitenone B (5) were also found. Compound 3 displays a ring contraction while 4 has a new dihydrofuran ring. Structural characterization was achieved by a combination of NMR, HR-MS, and X-ray diffraction (XRD). Moderate activity towards RSV was reported for 9 and the new metabolite 1, with IC₅₀ values of 15.0 μM and 39.8 μM, respectively. Full article

(This article belongs to the Section Synthesis and Medicinal Chemistry of Marine Natural Products)

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28 pages, 3065 KiB

Open AccessReview

Biomarkers and Seaweed-Based Nutritional Interventions in Metabolic Syndrome: A Comprehensive Review

by Ana Valado, Margarida Cunha and Leonel Pereira

Mar. Drugs 2024, 22(12), 550; https://doi.org/10.3390/md22120550 - 4 Dec 2024

Abstract

Metabolic Syndrome (MetS) is a complex, multifactorial condition characterized by risk factors such as abdominal obesity, insulin resistance, dyslipidemia and hypertension, which significantly contribute to the development of cardiovascular disease (CVD), the leading cause of death worldwide. Early identification and effective monitoring of [...] Read more.

Metabolic Syndrome (MetS) is a complex, multifactorial condition characterized by risk factors such as abdominal obesity, insulin resistance, dyslipidemia and hypertension, which significantly contribute to the development of cardiovascular disease (CVD), the leading cause of death worldwide. Early identification and effective monitoring of MetS is crucial for preventing serious cardiovascular complications. This article provides a comprehensive overview of various biomarkers associated with MetS, including lipid profile markers (triglyceride/high-density lipoprotein cholesterol (TG/HDL-C) ratio and apolipoprotein B/apolipoprotein A1 (ApoB/ApoA1) ratio), inflammatory markers (interleukin 6 (IL-6), tumor necrosis factor alpha (TNF-α), plasminogen activator inhibitor type 1 (PAI-1), C-reactive protein (CRP), leptin/adiponectin ratio, omentin and fetuin-A/adiponectin ratio), oxidative stress markers (lipid peroxides, protein and nucleic acid oxidation, gamma-glutamyl transferase (GGT), uric acid) and microRNAs (miRNAs) such as miR-15a-5p, miR5-17-5p and miR-24-3p. Additionally, this review highlights the importance of biomarkers in MetS and the need for advancements in their identification and use for improving prevention and treatment. Seaweed therapy is also discussed as a significant intervention for MetS due to its rich content of fiber, antioxidants, minerals and bioactive compounds, which help improve cardiovascular health, reduce inflammation, increase insulin sensitivity and promote weight loss, making it a promising nutritional strategy for managing metabolic and cardiovascular health. Full article

(This article belongs to the Collection Marine Drugs in the Management of Metabolic Diseases)

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24 pages, 3164 KiB

Open AccessArticle

Cytotoxic Effects of ZnO and Ag Nanoparticles Synthesized in Microalgae Extracts on PC12 Cells

by Giacomo Fais, Agnieszka Sidorowicz, Giovanni Perra, Debora Dessì, Francesco Loy, Nicola Lai, Paolo Follesa, Roberto Orrù, Giacomo Cao and Alessandro Concas

Mar. Drugs 2024, 22(12), 549; https://doi.org/10.3390/md22120549 - 4 Dec 2024

Abstract

The green synthesis of silver (Ag) and zinc oxide (ZnO) nanoparticles (NPs), as well as Ag/Ag₂O/ZnO nanocomposites (NCs), using polar and apolar extracts of Chlorella vulgaris, offers a sustainable method for producing nanomaterials with tunable properties. The impact of the [...] Read more.

The green synthesis of silver (Ag) and zinc oxide (ZnO) nanoparticles (NPs), as well as Ag/Ag₂O/ZnO nanocomposites (NCs), using polar and apolar extracts of Chlorella vulgaris, offers a sustainable method for producing nanomaterials with tunable properties. The impact of the synthesis environment and the nanomaterials’ characteristics on cytotoxicity was evaluated by examining reactive species production and their effects on mitochondrial bioenergetic functions. Cytotoxicity assays on PC12 cells, a cell line originated from a rat pheochromocytoma, an adrenal medulla tumor, demonstrated that Ag/Ag₂O NPs synthesized with apolar (Ag/Ag₂O NPs A) and polar (Ag/Ag₂O NPs P) extracts exhibited significant cytotoxic effects, primarily driven by Ag⁺ ion release and the disruption of mitochondrial function. However, it is more likely the organic content, rather than size, influenced anticancer activity, as commercial Ag NPs, despite smaller crystallite sizes, exhibit less effective activity. ZnO NPs P showed increased reactive oxygen species (ROS) generation, correlated with higher cytotoxicity, while ZnO NPs A produced lower ROS levels, resulting in diminished cytotoxic effects. A comparative analysis revealed significant differences in LD₅₀ values and toxicity profiles. Differentiated PC12 cells showed higher resistance to ZnO, while AgNPs and Ag/Ag₂O-based materials had similar effects on both cell types. This study emphasizes the crucial role of the synthesis environment and bioactive compounds from C. vulgaris in modulating nanoparticle surface chemistry, ROS generation, and cytotoxicity. The results provide valuable insights for designing safer and more effective nanomaterials for biomedical applications, especially for targeting tumor-like cells, by exploring the relationships between nanoparticle size, polarity, capping agents, and nanocomposite structures. Full article

(This article belongs to the Special Issue Discovery of Marine-Derived Anticancer Agents, 2nd Edition)

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22 pages, 1965 KiB

Open AccessArticle

Revealing the Potential of Fucus vesiculosus Linnaeus for Cosmetic Purposes: Chemical Profile and Biological Activities of Commercial and Wild Samples

by Marina Muñoz-Quintana, Carolina Padrón-Sanz, Marina Dolbeth, Francisco Arenas, Vitor Vasconcelos and Graciliana Lopes

Mar. Drugs 2024, 22(12), 548; https://doi.org/10.3390/md22120548 - 4 Dec 2024

Abstract

The natural products industry is gaining increasing interest, not only due to modern lifestyles becoming more aware of environmental and sustainability issues but also because of the loss of efficacy and undesirable side effects of synthetic ingredients. This pioneering study provides a comprehensive [...] Read more.

The natural products industry is gaining increasing interest, not only due to modern lifestyles becoming more aware of environmental and sustainability issues but also because of the loss of efficacy and undesirable side effects of synthetic ingredients. This pioneering study provides a comprehensive comparison between extracts obtained from wild and commercial samples of Fucus vesiculosus Linnaeus, highlighting their multifaceted benefits in cosmetic applications. The antiaging potential of acetone (70 and 90%) and ethanol 60% extracts from wild and commercial samples of F. vesiculosus, focusing on their application in cosmetics, was explored. The extracts were chemically characterized, their carotenoid profiles being established by HPLC, and the total phenolic content and phlorotannins by spectrophotometry. The extracts were evaluated for their antioxidant potential against the physiologic free radicals superoxide anion radical (O₂^•−) and nitric oxide (^•NO), for their ability to inhibit the enzymes hyaluronidase and tyrosinase, and for their anti-inflammatory potential in the macrophage cell model RAW 264.7. The acetone 70% extract of wild F. vesiculosus was the richest in fucoxanthin, which accounted for more than 67% of the total pigments identified, followed by the acetone 90% extract of the same sample, where both fucoxanthin and pheophytin-a represented 40% of the total pigments. The same behavior was observed for phenolic compounds, with the ethanol 60% presenting the lowest values. A chemical correlation could be established between the chemical composition and the biological activities, with acetone extracts from the wild F. vesiculosus, richer in fucoxanthin and phlorotannins, standing out as natural ingredients with anti-aging potential. Acetone 90% can be highlighted as the most effective extraction solvent, their extracts presenting the highest radicals scavenging capacity, ability to inhibit tyrosinase to a greater extent than the commercial ingredient kojic acid, and potential to slow down the inflammatory process. Full article

(This article belongs to the Special Issue Marine Natural Products with Anti-aging Activity)

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30 pages, 2314 KiB

Open AccessArticle

Enzymatic Interesterification of Cold-Pressed Maqui (Aristotelia chilensis (Mol.) Stuntz) Seed Oil and Belly Oil from Rainbow Trout (Oncorhynchus mykiss) Through Supercritical CO₂

by Francisca Reinoso, Alicia Rodríguez, Camila Sánchez, Benjamín Claria, Nalda Romero, Alejandra Espinosa, María Elsa Pando, Rodrigo Valenzuela, Dayana Apaza, Gretel Dovale-Rosabal and Santiago P. Aubourg

Mar. Drugs 2024, 22(12), 547; https://doi.org/10.3390/md22120547 - 4 Dec 2024

Abstract

A new antioxidant lipid (AL) was synthesized from rainbow trout (Oncorhynchus mykiss) belly oil and cold-pressed maqui (CPM) (Aristotelia chilensis (Mol.) Stuntz) seed oil via enzymatic interesterification using Thermomyces lanuginosus in supercritical CO₂ medium. A Box–Behnken design with 15 [...] Read more.

A new antioxidant lipid (AL) was synthesized from rainbow trout (Oncorhynchus mykiss) belly oil and cold-pressed maqui (CPM) (Aristotelia chilensis (Mol.) Stuntz) seed oil via enzymatic interesterification using Thermomyces lanuginosus in supercritical CO₂ medium. A Box–Behnken design with 15 experiments was employed, with the independent variables being the following: belly oil/CPM oil ratio (10/90, 50/50, and 90/10, w/w), supercritical CO₂ temperature (40.0, 50.0, and 60.0 °C), and supercritical CO₂ pressure (100.0, 200.0, and 300.0 bar) for enzymatic interesterification. A multiple optimization was conducted based on the response variables yield and eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA), and tocopherol contents. The optimized conditions for the AL synthesis were: 81.4/18.6 (w/w), 40.0 °C and 299.99 bar, respectively. The corresponding responses variables were: 77.10% for yield, 5.12 and 4.95 g·100 g⁻¹ total fatty acids for EPA and DHA, respectively, and 217.96, 4.28, 3.48, 64.48, and 6.39 mg·kg⁻¹ oil for α-tocopherol, α-tocotrienol, β-tocopherol, γ-tocopherol, and δ-tocopherol, respectively. A novel AL was successfully synthesized starting from two abundant natural resources commonly considered as by-products during industrial processing. In agreement with the high EPA, DHA, and tocopherol presence, this AL can be recommended to be employed in nutritional and therapeutic supplements, according to its health benefits, particularly concerning antioxidant and anti-inflammatory properties. Full article

(This article belongs to the Section Marine-Derived Ingredients for Drugs, Cosmeceuticals and Nutraceuticals)

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30 pages, 8265 KiB

Open AccessReview

Research Progress on Using Modified Hydrogel Coatings as Marine Antifouling Materials

by Ying Wang, Xiaohong Zhou, Lingyan He, Xiangkai Zhou, Yantian Wang and Peijian Zhou

Mar. Drugs 2024, 22(12), 546; https://doi.org/10.3390/md22120546 - 3 Dec 2024

Abstract

The adhesion of marine organisms to marine facilities negatively impacts human productivity. This phenomenon, known as marine fouling, constitutes a serious issue in the marine equipment industry. It increases resistance for ships and their structures, which, in turn, raises fuel consumption and reduces [...] Read more.

The adhesion of marine organisms to marine facilities negatively impacts human productivity. This phenomenon, known as marine fouling, constitutes a serious issue in the marine equipment industry. It increases resistance for ships and their structures, which, in turn, raises fuel consumption and reduces ship speed. To date, numerous antifouling strategies have been researched to combat marine biofouling. However, a multitude of these resources face long-term usability issues due to various limitations, such as low adhesion quality, elevated costs, and inefficacy. Hydrogels, exhibiting properties akin to the slime layer on the skin of many aquatic creatures, possess a low frictional coefficient and a high rate of water absorbency and are extensively utilized in the marine antifouling field. This review discusses the recent progress regarding the application of hydrogels as an important marine antifouling material in recent years. It introduces the structure, properties, and classification of hydrogels; summarizes the current research status of improved hydrogels in detail; and analyzes the improvement in their antifouling properties and the prospects for their application in marine antifouling. Full article

(This article belongs to the Special Issue Marine Natural Products with Antifouling Activity, 3rd Edition)

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19 pages, 1654 KiB

Open AccessArticle

Pectiniferosides A–J: Diversified Glycosides of Polyhydroxy Steroids Isolated from the Sea Star Patiria (=Asterina) pectinifera

by Ranran Zhang, Zhen Lu, Derui Wang, Zhi Yan, Xueting Sun, Xiaodong Li, Xiuli Yin, Song Wang and Ke Li

Mar. Drugs 2024, 22(12), 545; https://doi.org/10.3390/md22120545 - 3 Dec 2024

Abstract

To optimize the utilization of the sea star Patiria (=Asterina) pectinifera, which has demonstrated potential pharmaceutical properties in Chinese folk medicine, ten glycosides of polyhydroxy steroids, pectiniferosides A–J (1–10), were isolated and characterized. These compounds possess 3β, 6α, [...] Read more.

To optimize the utilization of the sea star Patiria (=Asterina) pectinifera, which has demonstrated potential pharmaceutical properties in Chinese folk medicine, ten glycosides of polyhydroxy steroids, pectiniferosides A–J (1–10), were isolated and characterized. These compounds possess 3β, 6α, 8, 15α (or β), 16β-pentahydroxycholestane aglycones with sulfated and (or) methylated monosaccharides. The chemical structures of 1–10 were determined using NMR spectroscopy and HR-ESI-MS. The discovery of saponins with multiple substitution patterns in sea stars exemplified the molecular diversity of secondary metabolites in marine echinoderms. These compounds exhibited no embryotoxicity or teratogenicity at a concentration of 100 μM in a bioassay with marine medaka (Oryzias melastigma) embryos, implying that these compounds may not be ecologically toxic to marine fish embryos. In addition, none of the compounds exhibited significant cytotoxicity against five human cancer cell lines at 40 μM or anti-inflammatory activities at 50 μM, suggesting their potential for further structural optimization to enhance bioactivity. The research on the constituents of P. pectinifera provides a potential foundation for drug development and marine ecotoxicology. Full article

(This article belongs to the Section Structural Studies on Marine Natural Products)

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30 pages, 2544 KiB

Open AccessReview

Abiotic Factors Modulating Metabolite Composition in Brown Algae (Phaeophyceae): Ecological Impacts and Opportunities for Bioprospecting of Bioactive Compounds

by Clara Lopes, Johana Marcela Concha Obando, Thalisia Cunha dos Santos, Diana Negrão Cavalcanti and Valéria Laneuville Teixeira

Mar. Drugs 2024, 22(12), 544; https://doi.org/10.3390/md22120544 - 2 Dec 2024

Abstract

Brown algae are vital structural elements and contributors to biodiversity in marine ecosystems. These organisms adapt to various environmental challenges by producing primary and secondary metabolites crucial for their survival, defense, and resilience. Besides their ecological role, these diverse metabolites have potential for [...] Read more.

Brown algae are vital structural elements and contributors to biodiversity in marine ecosystems. These organisms adapt to various environmental challenges by producing primary and secondary metabolites crucial for their survival, defense, and resilience. Besides their ecological role, these diverse metabolites have potential for biotechnological applications in industries including pharmaceuticals, cosmetics, and food. A literature review was conducted encompassing studies from 2014–2024, evaluating the effects of hydrodynamics, temperature, light, nutrients, seasonality, and salinity on the chemical profiles of various Phaeophyceae algae species. Thirty original articles spanning 69 species from the Sargassaceae, Dictyotaceae, Fucaceae, and Scytosiphonaceae families were analyzed and systematically arranged, with a focus on methodologies and key findings. This review furthers ecological discussions on each environmental factor and explores the biotechnological potential of metabolites such as polysaccharides, fatty acids, phenolics, diterpenes, and pigments. The information in this work is beneficial for metabolite bioprospecting and in vitro cultivation models as well as indoor and outdoor cultivation studies. Full article

(This article belongs to the Special Issue Marine Algal Chemical Ecology 2024)

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12 pages, 1339 KiB

Open AccessArticle

Optimized Extraction of Sargahydroquinoic Acid, Major Bioactive Substance, from Sargassum yezoense Using Response Surface Methodology

by Suhyeon Baek, Ji-Eun Bae, Yu Miao, Gahyeon Kim, Bomi Ryu, Byung-Hoo Lee and Sanggil Lee

Mar. Drugs 2024, 22(12), 543; https://doi.org/10.3390/md22120543 - 2 Dec 2024

Abstract

Sargahydroquinoic acid (SHQA), a bioactive compound found in certain Sargassum species, exhibits significant health benefits. This study optimized the extraction of SHQA from Sargassum yezoense using response surface methodology (RSM) and evaluated its antioxidant effects through in vitro and in vivo assays. A [...] Read more.

Sargahydroquinoic acid (SHQA), a bioactive compound found in certain Sargassum species, exhibits significant health benefits. This study optimized the extraction of SHQA from Sargassum yezoense using response surface methodology (RSM) and evaluated its antioxidant effects through in vitro and in vivo assays. A Box–Behnken design (BBD) was effectively employed to investigate the effects of incubation temperature, time, and ethanol concentration on SHQA yield, achieving a high coefficient of determination (R² = 0.961). Analysis of variance (ANOVA) validated the model’s reliability (F = 13.86, p = 0.005) and highlighted ethanol concentration as a highly significant factor (p < 0.001). Optimal extraction conditions were identified as 52.8 °C, 8.3 h, and 74.1% ethanol. The SHQA-maximized extract (SME) contained 67.8 ± 0.6 mg SHQA/g and 25.00 ± 1.01 mg phloroglucinol equivalent/g. SME exhibited antioxidant capacity of 26.45 ± 0.66 mg and 28.74 ± 2.30 mg vitamin C equivalent/g in ABTS and DPPH assays, respectively, and 0.29 ± 0.02 mM FeSO₄ equivalent/g in the FRAP assay. Additionally, SME at 50 µg/mL and SHQA at 1 µg/mL inhibited reactive oxygen species (ROS) generation in an H₂O₂-induced zebrafish model. This study presents the first optimization of SHQA extraction using RSM and demonstrates SHQA’s ROS inhibition in a zebrafish model. Full article

(This article belongs to the Special Issue Green Extraction of High-Value Compounds in Marine Algae)

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30 pages, 5277 KiB

Open AccessArticle

Sea Anemone Kunitz Peptide HCIQ2c1: Structure, Modulation of TRPA1 Channel, and Suppression of Nociceptive Reaction In Vivo

by Aleksandra N. Kvetkina, Sergey D. Oreshkov, Pavel A. Mironov, Maxim M. Zaigraev, Anna A. Klimovich, Yulia V. Deriavko, Aleksandr S. Menshov, Dmitrii S. Kulbatskii, Yulia A. Logashina, Yaroslav A. Andreev, Anton O. Chugunov, Mikhail P. Kirpichnikov, Ekaterina N. Lyukmanova, Elena V. Leychenko and Zakhar O. Shenkarev

Mar. Drugs 2024, 22(12), 542; https://doi.org/10.3390/md22120542 - 2 Dec 2024

Abstract

TRPA1 is a homotetrameric non-selective calcium-permeable channel. It contributes to chemical and temperature sensitivity, acute pain sensation, and development of inflammation. HCIQ2c1 is a peptide from the sea anemone Heteractis magnifica that inhibits serine proteases. Here, we showed that HCIQ2c1 significantly reduces AITC- [...] Read more.

TRPA1 is a homotetrameric non-selective calcium-permeable channel. It contributes to chemical and temperature sensitivity, acute pain sensation, and development of inflammation. HCIQ2c1 is a peptide from the sea anemone Heteractis magnifica that inhibits serine proteases. Here, we showed that HCIQ2c1 significantly reduces AITC- and capsaicin-induced pain and inflammation in mice. Electrophysiology recordings in Xenopus oocytes expressing rat TRPA1 channel revealed that HCIQ2c1 binds to open TRPA1 and prevents its transition to closed and inhibitor-insensitive ‘hyperactivated’ states. NMR study of the ¹⁵N-labeled recombinant HCIQ2c1 analog described a classical Kunitz-type structure and revealed two dynamic hot-spots (loops responsible for protease binding and regions near the N- and C-termini) that exhibit simultaneous mobility on two timescales (ps–ns and μs–ms). In modelled HCIQ2c1/TRPA1 complex, the peptide interacts simultaneously with one voltage-sensing-like domain and two pore domain fragments from different channel’s subunits, and with lipid molecules. The model explains stabilization of the channel in the open conformation and the restriction of ‘hyperactivation’, which are probably responsible for the observed analgetic activity. HCIQ2c1 is the third peptide ligand of TRPA1 from sea anemones and the first Kunitz-type ligand of this channel. HCIQ2c1 is a prototype of efficient analgesic and anti-inflammatory drugs. Full article

(This article belongs to the Special Issue Toxins as Marine-Based Drug Discovery, 2nd Edition)

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14 pages, 1355 KiB

Open AccessArticle

The Effect of Phosphorus Concentration on the Co-Production of Fucoxanthin and Fatty Acids in Conticribra weissflogii

by Ning Zhang, Di Peng, Xiangyu Rui, Wenquan Zheng, Zhenglin Zeng, Xianghu Huang, Changling Li and Feng Li

Mar. Drugs 2024, 22(12), 541; https://doi.org/10.3390/md22120541 - 30 Nov 2024

Abstract

The production of fucoxanthin and fatty acids in Conticribra weissflogii has been examined, but the role of elements like phosphorus in their mutualistic interactions is not well understood. To fill this gap, our study utilized potassium dihydrogen phosphate (KH₂PO₄) [...] Read more.

The production of fucoxanthin and fatty acids in Conticribra weissflogii has been examined, but the role of elements like phosphorus in their mutualistic interactions is not well understood. To fill this gap, our study utilized potassium dihydrogen phosphate (KH₂PO₄) as a source of phosphorus to examine its impact on the synthesis of fucoxanthin and fatty acids in C. weissflogii. Our findings revealed that at a phosphorus concentration of 10 mg L⁻¹, the cell density (9.5 × 10⁵ cells mL⁻¹), carotenoid concentration (1.67 mg g⁻¹), fucoxanthin concentration (0.91 mg L⁻¹), and fucoxanthin content (1.33 mg g⁻¹) were maximized. Additionally, at a phosphorus concentration of 20 mg L⁻¹, cell dry weight (0.76 ± 0.08 g L⁻¹), total fatty acid content, saturated fatty acids, and unsaturated fatty acids were all at their highest levels, making this concentration optimal for EPA accumulation. In conclusion, manipulating the phosphorus concentration can enhance the levels of fucoxanthin and unsaturated fatty acids in C. weissflogii, offering valuable insights into the co-production of these two high-value compounds within this species. Full article

(This article belongs to the Special Issue Advances in Marine-Derived Fucoxanthin Studies)

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25 pages, 817 KiB

Open AccessReview

Recent Advances of the Zebrafish Model in the Discovery of Marine Bioactive Molecules

by Changyu Liu, Jiaxun Li, Dexu Wang, Jibin Liu, Kechun Liu, Peihai Li and Yun Zhang

Mar. Drugs 2024, 22(12), 540; https://doi.org/10.3390/md22120540 - 30 Nov 2024

Abstract

Marine natural products are increasingly utilized in nutrition, cosmetics, and medicine, garnering significant attention from researchers globally. With the expansion of marine resource exploration in recent years, the demand for marine natural products has risen, necessitating rapid and cost-effective activity evaluations using model [...] Read more.

Marine natural products are increasingly utilized in nutrition, cosmetics, and medicine, garnering significant attention from researchers globally. With the expansion of marine resource exploration in recent years, the demand for marine natural products has risen, necessitating rapid and cost-effective activity evaluations using model organisms. Zebrafish, a valuable vertebrate model, has become an efficient tool for screening and identifying safe, active molecules from marine natural products. This review, based on nearly 10 years of literature, summarizes the current status and progress of zebrafish models in evaluating marine natural product bioactivity. It also highlights their potential in exploring marine resources with health benefits, offering a reference for the future development and utilization of marine biological resources. Full article

(This article belongs to the Special Issue Zebrafish Models in Marine Drug Discovery)

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