Journal Description
Marine Drugs
Marine Drugs
is the leading, peer-reviewed, open access journal on the research, development, and production of biologically and therapeutically active compounds from the sea. Marine Drugs is published monthly online by MDPI. Australia New Zealand Marine Biotechnology Society (ANZMBS) is affiliated with Marine Drugs and its members receive a discount on article processing charges.
- Open Access— free for readers, with article processing charges (APC) paid by authors or their institutions.
- High Visibility: indexed within Scopus, SCIE (Web of Science), PubMed, MEDLINE, PMC, Embase, PubAg, MarinLit, AGRIS, and other databases.
- Journal Rank: JCR - Q1 (Pharmacology & Pharmacy) / CiteScore - Q1 (Pharmacology, Toxicology and Pharmaceutics (miscellaneous))
- Rapid Publication: manuscripts are peer-reviewed and a first decision is provided to authors approximately 14 days after submission; acceptance to publication is undertaken in 1.9 days (median values for papers published in this journal in the second half of 2023).
- Recognition of Reviewers: reviewers who provide timely, thorough peer-review reports receive vouchers entitling them to a discount on the APC of their next publication in any MDPI journal, in appreciation of the work done.
Impact Factor:
5.4 (2022);
5-Year Impact Factor:
5.5 (2022)
Latest Articles
Purification and Characterization of a Novel Fibrinolytic Enzyme from Marine Bacterium Bacillus sp. S-3685 Isolated from the South China Sea
Mar. Drugs 2024, 22(6), 267; https://doi.org/10.3390/md22060267 (registering DOI) - 10 Jun 2024
Abstract
A novel fibrinolytic enzyme, BSFE1, was isolated from the marine bacterium Bacillus sp. S-3685 (GenBank No.: KJ023685) found in the South China Sea. This enzyme, with a molecular weight of approximately 42 kDa and a specific activity of 736.4 U/mg, exhibited its highest
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A novel fibrinolytic enzyme, BSFE1, was isolated from the marine bacterium Bacillus sp. S-3685 (GenBank No.: KJ023685) found in the South China Sea. This enzyme, with a molecular weight of approximately 42 kDa and a specific activity of 736.4 U/mg, exhibited its highest activity at 37 °C in a phosphate buffer at pH 8.0. The fibrinolytic enzyme remained stable over a pH range of 7.5 to 10.0 and retained about 76% of its activity after being incubated at 37 °C for 2 h. The Km and Vmax values of the enzyme at 37 °C were determined to be 2.1 μM and 49.0 umol min−1 mg−1, respectively. The fibrinolytic activity of BSFE1 was enhanced by Na+, Ba2+, K+, Co2+, Mn2+, Al3+, and Cu2+, while it was inhibited by Fe3+, Ca2+, Mg2+, Zn2+, and Fe2+. These findings indicate that the fibrinolytic enzyme isolated in this study exhibits a strong affinity for fibrin. Moreover, the enzyme we have purified demonstrates thrombolytic enzymatic activity. These characteristics make BSFE1 a promising candidate for thrombolytic therapy. In conclusion, the results obtained from this study suggest that our work holds potential in the development of agents for thrombolytic treatment.
Full article
(This article belongs to the Special Issue Advances of Marine-Derived Enzymes)
Open AccessArticle
Halenaquinol Blocks Staphylococcal Protein A Anchoring on Cell Wall Surface by Inhibiting Sortase A in Staphylococcus aureus
by
Jaepil Lee, Jae-Hyeong Choi, Jayho Lee, Eunji Cho, Yeon-Ju Lee, Hyi-Seung Lee and Ki-Bong Oh
Mar. Drugs 2024, 22(6), 266; https://doi.org/10.3390/md22060266 (registering DOI) - 10 Jun 2024
Abstract
Sortase A (SrtA) is a cysteine transpeptidase that binds to the periplasmic membrane and plays a crucial role in attaching surface proteins, including staphylococcal protein A (SpA), to the peptidoglycan cell wall. Six pentacyclic polyketides (1‒6) were isolated from
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Sortase A (SrtA) is a cysteine transpeptidase that binds to the periplasmic membrane and plays a crucial role in attaching surface proteins, including staphylococcal protein A (SpA), to the peptidoglycan cell wall. Six pentacyclic polyketides (1‒6) were isolated from the marine sponge Xestospongia sp., and their structures were elucidated using spectroscopic techniques and by comparing them to previously reported data. Among them, halenaquinol (2) was found to be the most potent SrtA inhibitor, with an IC50 of 13.94 μM (4.66 μg/mL). Semi-quantitative reverse transcription PCR data suggest that halenaquinol does not inhibit the transcription of srtA and spA, while Western blot analysis and immunofluorescence microscopy images suggest that it blocks the cell wall surface anchoring of SpA by inhibiting the activity of SrtA. The onset and magnitude of the inhibition of SpA anchoring on the cell wall surface in S. aureus that has been treated with halenaquinol at a value 8× that of the IC50 of SrtA are comparable to those for an srtA-deletion mutant. These findings contribute to the understanding of the mechanism by which marine-derived pentacyclic polyketides inhibit SrtA, highlighting their potential as anti-infective agents targeting S. aureus virulence.
Full article
(This article belongs to the Section Marine Pharmacology)
Open AccessArticle
Purification and Structural Analyses of Sulfated Polysaccharides from Low-Value Sea Cucumber Stichopus naso and Anticoagulant Activities of Its Oligosaccharides
by
Lige Cui, Huifang Sun, Xiaolei Shang, Jing Wen, Pengfei Li, Shengtao Yang, Linxia Chen, Xiangyang Huang, Haoyang Li, Ronghua Yin and Jinhua Zhao
Mar. Drugs 2024, 22(6), 265; https://doi.org/10.3390/md22060265 (registering DOI) - 8 Jun 2024
Abstract
Three polysaccharides (SnNG, SnFS and SnFG) were purified from the body wall of Stichopus naso. The physicochemical properties, including monosaccharide composition, molecular weight, sulfate content, and optical rotation, were analyzed, confirming that SnFS and SnFG are sulfated polysaccharides commonly found in sea
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Three polysaccharides (SnNG, SnFS and SnFG) were purified from the body wall of Stichopus naso. The physicochemical properties, including monosaccharide composition, molecular weight, sulfate content, and optical rotation, were analyzed, confirming that SnFS and SnFG are sulfated polysaccharides commonly found in sea cucumbers. The highly regular structure {3)-L-Fuc2S-(α1,}n of SnFS was determined via a detailed NMR analysis of its oxidative degradation product. By employing β-elimination depolymerization of SnFG, tri-, penta-, octa-, hendeca-, tetradeca-, and heptadeca-saccharides were obtained from the low-molecular-weight product. Their well-defined structures confirmed that SnFG possessed the backbone of {D-GalNAc4S6S-β(1,4)-D-GlcA}, and each GlcA residue was branched with Fuc2S4S. SnFS and SnFG are both structurally the simplest version of natural fucan sulfate and fucosylated glycosaminoglycan, facilitating the application of low-value sea cucumbers S. naso. Bioactivity assays showed that SnFG and its derived oligosaccharides exhibited potent anticoagulation and intrinsic factor Xase (iXase) inhibition. Moreover, a comparative analysis with the series of oligosaccharides solely branched with Fuc3S4S showed that in oligosaccharides with lower degrees of polymerization, such as octasaccharides, Fuc2S4S led to a greater increase in APTT prolongation and iXase inhibition. As the degree of polymerization increases, the influence from the sulfation pattern diminishes, until it is overshadowed by the effects of molecular weight.
Full article
(This article belongs to the Special Issue Polysaccharides from Marine Environment)
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Open AccessArticle
Status of Fishery Discards and By-Products in Greece and Potential Valorization Scenarios towards a National Exploitation Master Plan
by
Efstratios Roussos, George Triantaphyllidis, Vassiliki Ilia, Konstantinos Tsagarakis, Athanasios Machias, Leto-Aikaterini Tziveleka, Vassilios Roussis, Efstathia Ioannou and Yannis Kotzamanis
Mar. Drugs 2024, 22(6), 264; https://doi.org/10.3390/md22060264 - 7 Jun 2024
Abstract
The valorization of aquaculture/fishery processing by-products, as well as unavoidable/unwanted catches and discards in Greece, is currently an underutilized activity despite the fact that there are several best practices in Northern Europe and overseas. One of the main challenges is to determine whether
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The valorization of aquaculture/fishery processing by-products, as well as unavoidable/unwanted catches and discards in Greece, is currently an underutilized activity despite the fact that there are several best practices in Northern Europe and overseas. One of the main challenges is to determine whether the available quantities for processing are sufficient to warrant the valorization of discards and fish side streams. This is the first attempt to systematically record and analyze the available quantities of fish by-products and discards in Greece spatially and temporally in an effort to create a national exploitation Master Plan for the valorization of this unavoidable and unwanted biomass. A thorough survey conducted within the VIOAXIOPIO project unveiled a substantial biomass of around 19,000 tonnes annually that could be harnessed for valorization. Furthermore, the production of various High-Added-Value Biomolecules (HAVBs) was investigated and experimental trials were conducted to assess the potential yields, with the collected data used to formulate four valorization scenarios.
Full article
(This article belongs to the Special Issue Fishery Discards, Processing Waste and Marine By-Products)
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Open AccessArticle
Elements in Serum, Muscle, Liver, and Kidney of Rabbits Fed Macroalgae-Supplemented Diets
by
Sabela Al-Soufi, Marta Miranda, Javier García, Antonio Muíños, Eugenio Cegarra, Nuria Nicodemus, Carlos Herrero-Latorre and Marta López-Alonso
Mar. Drugs 2024, 22(6), 263; https://doi.org/10.3390/md22060263 - 7 Jun 2024
Abstract
The addition of marine macroalgae to animal feed has garnered interest due to the demonstrated benefits of gut health in many livestock species. Most macroalgae have a higher mineral content than terrestrial vegetables, making them an attractive, sustainable source of minerals. However, some
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The addition of marine macroalgae to animal feed has garnered interest due to the demonstrated benefits of gut health in many livestock species. Most macroalgae have a higher mineral content than terrestrial vegetables, making them an attractive, sustainable source of minerals. However, some macroalgae contain elevated concentrations of iodine and arsenic, which may be transferred to the meat of livestock fed with macroalgae. This study evaluated the mineral profile of rabbit serum, muscle, liver, and kidney of rabbits fed diets supplemented with different marine macroalgae, with the goal of improving post-weaning gut health and reducing reliance on antibiotics. We found increased deposition of iodine in muscle, liver, and kidney due to macroalgae supplementation, which is particularly promising for regions with low iodine endemicity. Higher, though relatively low arsenic concentrations, compared to those in other animal meats and food sources, were also detected in the muscle, liver, and kidney of macroalgae-fed rabbits. The absence of apparent interactions with other micronutrients, particularly selenium, suggests that the inclusion of macroalgae in rabbit diets will not affect the overall mineral content. Enhanced bioavailability of elements such as phosphorus and iron may provide additional benefits, potentially reducing the need for mineral supplementation.
Full article
(This article belongs to the Special Issue Marine Natural Products in Anti-obesity and Metabolic Syndrome)
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Open AccessCommunication
The Discovery of Cyclic Lipopeptide Olenamidonins in a Deepsea-Derived Streptomyces Strain by Knocking Out a DtxR Family Regulator
by
Qiannan Sun, Dongqi Yu, Xueqing Zhang, Fei Xiao and Wenli Li
Mar. Drugs 2024, 22(6), 262; https://doi.org/10.3390/md22060262 - 6 Jun 2024
Abstract
Three new cyclic lipopeptides, olenamidonins A-C (1–3), in addition to two previously reported metabolites (4 and 5), were accumulated in the ΔdtxRso deletion mutant of deepsea-derived Streptomyces olivaceus SCSIO 1071. The structures of these cyclic
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Three new cyclic lipopeptides, olenamidonins A-C (1–3), in addition to two previously reported metabolites (4 and 5), were accumulated in the ΔdtxRso deletion mutant of deepsea-derived Streptomyces olivaceus SCSIO 1071. The structures of these cyclic lipopeptides were determined by a combination of spectroscopic methods and circular dichroism (CD) measurement. The antibacterial assay results showed that compounds 1–5 displayed different degrees of growth inhibition against multidrug-resistant (MDR) bacterial strains Enterococcus faecalis CCARM 5172 and Enterococcus faecium CCARM 5203 with minimum inhibitory concentrations (MICs) of 1.56−6.25 μg/mL.
Full article
(This article belongs to the Special Issue Bioactive Natural Products From the Deep-Sea-Sourced Microbes)
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Open AccessArticle
Quality Assessment of Fish Oil Obtained after Enzymatic Hydrolysis of a Mixture of Rainbow Trout (Oncorhynchus mykiss) and Atlantic Salmon (Salmo salar) Rest Raw Material Pretreated by High Pressure
by
Elissavet Kotsoni, Egidijus Daukšas, Grete Hansen Aas, Turid Rustad, Brijesh K. Tiwari and Janna Cropotova
Mar. Drugs 2024, 22(6), 261; https://doi.org/10.3390/md22060261 - 5 Jun 2024
Abstract
Utilization of fish rest raw material for fish oil extraction has received interest with the increasing demand for sustainable food sources. Enzymatic hydrolysis is an efficient method for the extraction of value-added compounds, but its effectiveness may be enhanced by high-pressure processing (HPP).
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Utilization of fish rest raw material for fish oil extraction has received interest with the increasing demand for sustainable food sources. Enzymatic hydrolysis is an efficient method for the extraction of value-added compounds, but its effectiveness may be enhanced by high-pressure processing (HPP). However, HPP can induce lipid oxidation, affecting the quality of the oil. This study aimed to evaluate the quality of fish oil obtained after enzymatic hydrolysis of a mixture of rainbow trout (Oncorhynchus mykiss) and Atlantic salmon (Salmo salar) rest raw material pretreated by HPP. Six pretreatments were tested prior to enzymatic hydrolysis; 200 MPa × 4 min, 200 MPa × 8 min, 400 MPa × 4 min, 400 MPa × 8 min, 600 MPa × 4 min, and 600 MPa × 8 min. The oil samples were analyzed for lipid oxidation parameters, free fatty acid content, fatty acid composition, and color changes over 8 weeks. The results confirmed that HPP may induce lipid oxidation and revealed significant influence of HPP parameters on lipid oxidation, with higher pressures leading to increased oxidation. Fatty acid composition varied among samples, but it was not substantially affected by HPP.
Full article
(This article belongs to the Special Issue Fishery Discards, Processing Waste and Marine By-Products)
Open AccessArticle
TRAF6 Inhibitors from Marine Compound Library: Pharmacophore, Virtual Screening, Fragment Replacement, ADMET, and Molecular Dynamics
by
Xuexuan Wu, Saiyi Zhong, Nan Zhou and Lianxiang Luo
Mar. Drugs 2024, 22(6), 260; https://doi.org/10.3390/md22060260 - 5 Jun 2024
Abstract
TRAF6 is an E3 ubiquitin ligase that plays a crucial role in cell signaling. It is known that MMP is involved in tumor metastasis, and TRAF6 induces MMP-9 expression by binding to BSG. However, inhibiting TRAF6’s ubiquitinase activity without disrupting the RING domain
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TRAF6 is an E3 ubiquitin ligase that plays a crucial role in cell signaling. It is known that MMP is involved in tumor metastasis, and TRAF6 induces MMP-9 expression by binding to BSG. However, inhibiting TRAF6’s ubiquitinase activity without disrupting the RING domain is a challenge that requires further research. To address this, we conducted computer-based drug screening to identify potential TRAF6 inhibitors. Using a ligand–receptor complex pharmacophore based on the inhibitor EGCG, known for its anti-tumor properties, we screened 52,765 marine compounds. After the molecular docking of 405 molecules with TRAF6, six compounds were selected for further analysis. By replacing fragments of non-binding compounds and conducting second docking, we identified two promising molecules, CMNPD9212-16 and CMNPD12791-8, with strong binding activity and favorable pharmacological properties. ADME and toxicity predictions confirmed their potential as TRAF6 inhibitors. Molecular dynamics simulations showed that CMNPD12791-8 maintained a stable structure with the target protein, comparable to EGCG. Therefore, CMNPD12791-8 holds promise as a potential inhibitor of TRAF6 for inhibiting tumor growth and metastasis.
Full article
(This article belongs to the Special Issue Bioinformatics of Marine Natural Products 3.0)
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Open AccessArticle
Chrysomycins, Anti-Tuberculosis C-Glycoside Polyketides from Streptomyces sp. MS751
by
Jiaming Yu, Hui Guo, Jing Zhang, Jiansen Hu, Hongtao He, Caixia Chen, Na Yang, Fan Yang, Zexu Lin, Huanqin Dai, Liming Ouyang, Cuihua Liu, Xiaoguang Lei, Lixin Zhang, Guoliang Zhu and Fuhang Song
Mar. Drugs 2024, 22(6), 259; https://doi.org/10.3390/md22060259 - 3 Jun 2024
Abstract
A new dimeric C-glycoside polyketide chrysomycin F (1), along with four new monomeric compounds, chrysomycins G (2), H (3), I (4), J (5), as well as three known analogues, chrysomycins A (6
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A new dimeric C-glycoside polyketide chrysomycin F (1), along with four new monomeric compounds, chrysomycins G (2), H (3), I (4), J (5), as well as three known analogues, chrysomycins A (6), B (7), and C (8), were isolated and characterised from a strain of Streptomyces sp. obtained from a sediment sample collected from the South China Sea. Their structures were determined by detailed spectroscopic analysis. Chrysomycin F contains two diastereomers, whose structures were further elucidated by a biomimetic [2 + 2] photodimerisation of chrysomycin A. Chrysomycins B and C showed potent anti-tuberculosis activity against both wild-type Mycobacterium tuberculosis and a number of clinically isolated MDR M. tuberculosis strains.
Full article
(This article belongs to the Special Issue Marine Streptomyces-Derived Natural Products 2024)
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Open AccessArticle
Distribution and Level of Bioactive Monoacylglycerols in 12 Marine Microalgal Species
by
Giovanna Santaniello, Gianna Falascina, Marcello Ziaco, Laura Fioretto, Angela Sardo, Martina Carelli, Mariarosaria Conte, Giovanna Romano and Adele Cutignano
Mar. Drugs 2024, 22(6), 258; https://doi.org/10.3390/md22060258 - 31 May 2024
Abstract
Microalgae are currently considered an attractive source of highly valuable metabolites potentially exploitable as anticancer agents, nutraceuticals and cosmeceuticals and for bioenergy purposes. Their ease of culturing and their high growth rates further promote their use as raw material for the production of
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Microalgae are currently considered an attractive source of highly valuable metabolites potentially exploitable as anticancer agents, nutraceuticals and cosmeceuticals and for bioenergy purposes. Their ease of culturing and their high growth rates further promote their use as raw material for the production of specialty products. In the present paper, we focused our attention on specific glycerol-based lipid compounds, monoacylglycerols (MAGs), which displayed in our previous studies a selective cytotoxic activity against the haematological U-937 and the colon HCT-116 cancer cell lines. Here, we performed a quali/quantitative analysis of MAGs and total fatty acids (FAs) along with a profiling of the main lipid classes in a panel of 12 microalgal species, including diatoms and dinoflagellates. Our results highlight an inter- and intraspecific variability of MAG profile in the selected strains. Among them, Skeletonema marinoi (strain FE7) has emerged as the most promising source for possible biotechnological production of MAGs.
Full article
(This article belongs to the Special Issue Biotechnological Applications of Marine Microalgae)
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Open AccessArticle
Functional Characterization of the First Bona Fide Phytoene Synthase in Red Algae from Pyropia yezoensis
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Cheng-Ling Li, Jia-Qiu Pu, Wei Zhou, Chuan-Ming Hu, Yin-Yin Deng, Ying-Ying Sun and Li-En Yang
Mar. Drugs 2024, 22(6), 257; https://doi.org/10.3390/md22060257 - 31 May 2024
Abstract
The formation of phytoene by condensing two geranylgeranyl diphosphate molecules catalyzed by phytoene synthase (PSY) is the first committed and rate-limiting step in carotenoid biosynthesis, which has been extensively investigated in bacteria, land plants and microalgae. However, this step in macroalgae remains unknown.
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The formation of phytoene by condensing two geranylgeranyl diphosphate molecules catalyzed by phytoene synthase (PSY) is the first committed and rate-limiting step in carotenoid biosynthesis, which has been extensively investigated in bacteria, land plants and microalgae. However, this step in macroalgae remains unknown. In the present study, a gene encoding putative phytoene synthase was cloned from the economic red alga Pyropia yezoensis—a species that has long been used in food and pharmaceuticals. The conservative motifs/domains and the tertiary structure predicted using bioinformatic tools suggested that the cloned PyPSY should encode a phytoene synthase; this was empirically confirmed by pigment complementation in E. coli. This phytoene synthase was encoded by a single copy gene, whose expression was presumably regulated by many factors. The phylogenetic relationship of PSYs from different organisms suggested that red algae are probably the progeny of primary endosymbiosis and plastid donors of secondary endosymbiosis.
Full article
(This article belongs to the Special Issue Enzymes from Marine By-Products and Wastes)
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Open AccessReview
Revolutionizing Cardiovascular Health with Nano Encapsulated Omega-3 Fatty Acids: A Nano-Solution Approach
by
Richa Gill, Mashael Al-Badr, Mohammad Alghouti, Nura Adam Mohamed, Haissam Abou-Saleh and Md Mizanur Rahman
Mar. Drugs 2024, 22(6), 256; https://doi.org/10.3390/md22060256 - 30 May 2024
Abstract
Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) offer diverse health benefits, such as supporting cardiovascular health, improving cognitive function, promoting joint and musculoskeletal health, and contributing to healthy aging. Despite their advantages, challenges like oxidation susceptibility, low bioavailability, and potential adverse effects at high
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Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) offer diverse health benefits, such as supporting cardiovascular health, improving cognitive function, promoting joint and musculoskeletal health, and contributing to healthy aging. Despite their advantages, challenges like oxidation susceptibility, low bioavailability, and potential adverse effects at high doses persist. Nanoparticle encapsulation emerges as a promising avenue to address these limitations while preserving stability, enhanced bioavailability, and controlled release. This comprehensive review explores the therapeutic roles of omega-3 fatty acids, critically appraising their shortcomings and delving into modern encapsulation strategies. Furthermore, it explores the potential advantages of metal–organic framework nanoparticles (MOF NPs) compared to other commonly utilized nanoparticles in improving the therapeutic effectiveness of omega-3 fatty acids within drug delivery systems (DDSs). Additionally, it outlines future research directions to fully exploit the therapeutic benefits of these encapsulated omega-3 formulations for cardiovascular disease treatment.
Full article
(This article belongs to the Special Issue Value-Added Products from Marine Fishes)
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Open AccessArticle
Stem-Cell-Regenerative and Protective Effects of Squid (Symplectoteuthis oualaniensis) Skin Collagen Peptides against H2O2-Induced Fibroblast Injury
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Mingjun Wei, Lakshmi Jeevithan, Na Li, Lixin Liu, Jiren Xu, Wenhui Wu and Jeevithan Elango
Mar. Drugs 2024, 22(6), 255; https://doi.org/10.3390/md22060255 - 30 May 2024
Abstract
Recently, there has been a growing interest in collagen peptides derived from marine sources for their notable ability to protect skin cells against apoptosis induced by oxidants. Therefore, the current study aimed to investigate the fundamental properties of collagen peptides, including their physicochemical,
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Recently, there has been a growing interest in collagen peptides derived from marine sources for their notable ability to protect skin cells against apoptosis induced by oxidants. Therefore, the current study aimed to investigate the fundamental properties of collagen peptides, including their physicochemical, thermal, structural, stem-cell-regenerative, and skin-cell-protective effects, in comparison to commercial collagen peptides. The acid-soluble (ASC) and pepsin-soluble (PSC) collagens exhibited three distinct bands on SDS-PAGE, namely α (α1 and α2), β, and γ chains, confirming a type I pattern. The thermal profiles obtained from TG and DSC analyses confirmed the denaturation of PSC and ASC at temperatures ranging from 51.94 to 56.4 °C and from 52.07 to 56.53 °C, respectively. The purified collagen peptides were analyzed using SDS-PAGE and MALDI-TOF mass spectrometry, revealing a mass range of 900–15,000 Da. Furthermore, the de novo peptide sequence analysis confirmed the presence of the Gly-X-Y repeating sequence in collagen peptides. Collagen peptide treatments significantly enhanced HFF-1 cell proliferation and migration compared to the control group. ELISA results confirmed the potential interactions between collagen peptides and HFF-1 cells through α2β1, α10β1, and α11β1 integrin receptors. Notably, collagen peptide treatment effectively restored the proliferation of HFF-1 cells damaged by H2O2. Consequently, the advantageous characteristics of squid skin collagen peptides highlight their promising role in regenerative medicine.
Full article
(This article belongs to the Special Issue Fundamentals and Biomedical Applications of Marine Collagen)
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Open AccessArticle
Tracing the Impact of Domestic Storage Conditions on Antioxidant Activity and Lipid Profiles in the Edible Microalgae Chlorella vulgaris and Tetraselmis chui
by
Diana Lopes, Felisa Rey, Alexandrina Gomes, Luís Duarte, João Pereira, Marisa Pinho, Tânia Melo and Rosário Domingues
Mar. Drugs 2024, 22(6), 254; https://doi.org/10.3390/md22060254 - 30 May 2024
Abstract
The microalgae Chlorella vulgaris and Tetraselmis chui are valued for their nutrient-rich content, including lipids and polyunsaturated fatty acids (PUFA). However, little is known about how storage and processing affect their lipid quality. This study aimed to assess the impact of domestic storage
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The microalgae Chlorella vulgaris and Tetraselmis chui are valued for their nutrient-rich content, including lipids and polyunsaturated fatty acids (PUFA). However, little is known about how storage and processing affect their lipid quality. This study aimed to assess the impact of domestic storage and cooking practices in dried biomass of C. vulgaris and T. chui. Four conditions were tested: control (newly opened package), light (storage at room temperature and daily light regimen for three weeks), frozen (storage in the freezer at −20 °C for three weeks), and heated (three cycles of 90 min at 100 °C). Lipid extracts were analyzed by GC-MS and LC-MS, and antioxidant activity through DPPH and ABTS radical scavenging assays. Tested storage conditions promoted a decrease in fatty acid content and in diacyl/lyso lipid species ratios of phospholipid (PC/LPC, PE/LPE) and betaine lipids (DGTS/MGTS). Lipid extracts from light treatment showed the lowest antioxidant activity in C. vulgaris (ABTS, IC40: 104.9; DPPH, IC20: 187.9 ± 15.0), while heat affected the antioxidant activity of T. chui (ABTS, IC40: 88.5 ± 2.8; DPPH, IC20 209.4 ± 10.9). These findings underscore the impact of managing storage and processing conditions to optimize the nutritional and functional benefits of C. vulgaris and T. chui in food and feed applications.
Full article
(This article belongs to the Special Issue Lipidomics in Marine Microalgae and Seaweeds: Applications and Perspectives)
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Open AccessReview
Transition-Metal-Catalyzed Transformations for the Synthesis of Marine Drugs
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Lucía G. Parte, Sergio Fernández, Eva Sandonís, Javier Guerra and Enol López
Mar. Drugs 2024, 22(6), 253; https://doi.org/10.3390/md22060253 - 29 May 2024
Abstract
Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to
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Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to achieve selective, sustainable and efficient transformations, which cannot be obtained otherwise. In this perspective, we aim to showcase how a variety of transition metals have provided fruitful couplings in a wide variety of marine drug-like scaffolds over the past few years, by accelerating the production of these valuable molecules.
Full article
(This article belongs to the Special Issue Scaffold Diversity of Marine Natural Products)
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Open AccessArticle
αO-Conotoxin GeXIVA[1,2] Suppresses In Vivo Tumor Growth of Triple-Negative Breast Cancer by Inhibiting AKT-mTOR, STAT3 and NF-κB Signaling Mediated Proliferation and Inducing Apoptosis
by
Xijun Guo, Leping He, Weifeng Xu, Wanrong Wang, Xiaoli Feng, Yuanfeng Fu, Xiaofan Zhang, Ren-Bo Ding, Xingzhu Qi, Jiaolin Bao and Sulan Luo
Mar. Drugs 2024, 22(6), 252; https://doi.org/10.3390/md22060252 - 29 May 2024
Abstract
Breast cancer is one of the leading causes of cancer mortality worldwide, and triple-negative breast cancer (TNBC) is the most problematic subtype. There is an urgent need to develop novel drug candidates for TNBC. Marine toxins are a valuable source for drug discovery.
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Breast cancer is one of the leading causes of cancer mortality worldwide, and triple-negative breast cancer (TNBC) is the most problematic subtype. There is an urgent need to develop novel drug candidates for TNBC. Marine toxins are a valuable source for drug discovery. We previously identified αO-conotoxin GeXIVA[1,2] from Conus generalis, which is a selective antagonist of α9 nicotinic acetylcholine receptors (nAChRs). Recent studies indicated that α9 nAChR expression is positively correlated with breast cancer development; thus, α9 nAChR could serve as a therapeutic target for breast cancer. In this study, we aimed to investigate the in vivo antitumor effects of GeXIVA[1,2] on TNBC and to elucidate its underlying anticancer mechanism. Our data showed that GeXIVA[1,2] effectively suppressed 4T1 tumor growth in vivo at a very low dose of 0.1 nmol per mouse. Our results uncovered that the antitumor mechanism of GeXIVA[1,2] simultaneously induced apoptosis and blocked proliferation. Further investigations revealed that GeXIVA[1,2]-induced Caspase-3-dependent apoptosis was achieved through regulating Bax/Bcl-2 balance, and GeXIVA[1,2]-inhibited proliferation was mediated by the downregulation of the AKT-mTOR, STAT3 and NF-κB signaling pathways. Our study provides valuable arguments to demonstrate the potential of GeXIVA[1,2] as a novel marine-derived anticancer drug candidate for the treatment of TNBC.
Full article
(This article belongs to the Section Marine Toxins)
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Open AccessArticle
Fucoidan from Lessonia trabeculata Induces Apoptosis through Caspase Dependent and Caspase-Independent Activation in 4T1 Breast Adenocarcinoma In Vitro
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Raisa Teresa Cruz Riquelme, Erasmo Honorio Colona-Vallejos, Libertad Alzamora-Gonzales and Rosa María Condori Macuri
Mar. Drugs 2024, 22(6), 251; https://doi.org/10.3390/md22060251 - 29 May 2024
Abstract
Experiments conducted on triple-negative breast cancer have shown that fucoidan from Lessonia trabeculata (FLt) exhibits cytotoxic and antitumor properties. However, further research is necessary to gain a complete understanding of its bioactivity and level of cytotoxicity. The cytotoxic effect of FLt was determined
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Experiments conducted on triple-negative breast cancer have shown that fucoidan from Lessonia trabeculata (FLt) exhibits cytotoxic and antitumor properties. However, further research is necessary to gain a complete understanding of its bioactivity and level of cytotoxicity. The cytotoxic effect of FLt was determined by the 2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Apoptosis was analyzed using annexin V and caspase 3/7 staining kit and DNA fragmentation. In addition, transcriptional expression of antiapoptotic (Bcl-2 and XIAP) and proapoptotic (caspase 8, caspase 9, and AIF) genes were analyzed in TNBC 4T1 cells. After 72 h of culture, the IC50 for FLt was 561 μg/mL, while doxorubicin (Dox) had an IC50 of 0.04 μg/mL. In addition, assays for FLt + Dox were performed. Annexin V and caspase 3/7 revealed that FLt induces early and late-stage apoptosis. DNA fragmentation results support necrotic death of 4T1 cells. Similarly, transcripts that prevent cell death were decreased, while transcripts that promote cell death were increased. This study showed that FLt induces apoptosis by both caspase-dependent and caspase-independent mechanisms. These findings suggest that FLt may have potential applications in breast cancer treatment. Further research will provide more information to elucidate the mechanism of action of FLt.
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(This article belongs to the Special Issue Antioxidant and Anticancer Activities of Compounds Isolated from Seagrasses and Seaweeds)
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Marine Cytotoxin Santacruzamate A Derivatives as Potent HDAC1-3 Inhibitors and Their Synergistic Anti-Leukemia Effects with Venetoclax
by
Wanting Hao, Leyan Wang, Tongqiang Xu, Geng Jia, Yuqi Jiang, Chong Qin and Xiaoyang Li
Mar. Drugs 2024, 22(6), 250; https://doi.org/10.3390/md22060250 - 28 May 2024
Abstract
Acute myeloid leukemia (AML) is a hematologic malignancy characterized by infiltration of the blood and bone marrow, exhibiting a low remission rate and high recurrence rate. Current research has demonstrated that class I HDAC inhibitors can downregulate anti-apoptotic proteins, leading to apoptosis of
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Acute myeloid leukemia (AML) is a hematologic malignancy characterized by infiltration of the blood and bone marrow, exhibiting a low remission rate and high recurrence rate. Current research has demonstrated that class I HDAC inhibitors can downregulate anti-apoptotic proteins, leading to apoptosis of AML cells. In the present investigation, we conducted structural modifications of marine cytotoxin Santacruzamate A (SCA), a compound known for its inhibitory activity towards HDACs, resulting in the development of a novel series of potent class I HDACs hydrazide inhibitors. Representative hydrazide-based compound 25c exhibited concentration-dependent induction of apoptosis in AML cells as a single agent. Moreover, 25c exhibited a synergistic anti-AML effect when combined with Venetoclax, a clinical Bcl-2 inhibitor employed in AML therapy. This combination resulted in a more pronounced downregulation of anti-apoptotic proteins Mcl-1 and Bcl-xL, along with a significant upregulation of the pro-apoptotic protein cleaved-caspase3 and the DNA double-strand break biomarker γ-H2AX compared to monotherapy. These results highlighted the potential of 25c as a promising lead compound for AML treatment, particularly when used in combination with Venetoclax.
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(This article belongs to the Special Issue Synthesis and Discovery of Marine Antitumor Molecules)
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Pinctada martensii Hydrolysate Modulates the Brain Neuropeptidome and Proteome in Diabetic (db/db) Mice via the Gut–Brain Axis
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Jiayun Li, Yijun Lv, Yuanqing Wei, Xinzhi Wang, Shenghan Yan, Binyuan Zhao, Jipeng Sun, Rui Liu and Yueyang Lai
Mar. Drugs 2024, 22(6), 249; https://doi.org/10.3390/md22060249 - 28 May 2024
Abstract
Pinctada martensii hydrolysate (PMH) has been proved to have the effect of ameliorating disorders of glucose and lipid metabolism in db/db mice, but the mechanism of its hyperglycemia effect is still unclear. Bacterial communities in fecal samples from a normal control group, a
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Pinctada martensii hydrolysate (PMH) has been proved to have the effect of ameliorating disorders of glucose and lipid metabolism in db/db mice, but the mechanism of its hyperglycemia effect is still unclear. Bacterial communities in fecal samples from a normal control group, a diabetic control group, and a PMH-treated diabetes mellitus type 2 (T2DM) group were analyzed by 16S gene sequencing. Nano LC-MS/MS was used to analyze mice neuropeptides and proteomes. The 16S rDNA sequencing results showed that PMH modulated the structure and composition of the gut microbiota and improved the structure and composition of Firmicutes and Bacteroidetes at the phylum level and Desulfovibrionaceae and Erysipelatoclostridiaceae at the family level. Furthermore, the expressions of functional proteins of the central nervous system, immune response-related protein, and proteins related to fatty acid oxidation in the brain disrupted by an abnormal diet were recovered by PMH. PMH regulates the brain neuropeptidome and proteome and further regulates blood glucose in diabetic mice through the gut–brain axis. PMH may be used as a prebiotic agent to attenuate T2DM, and target-specific microbial species may have unique therapeutic promise for metabolic diseases.
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(This article belongs to the Special Issue Marine Natural Products in Anti-obesity and Metabolic Syndrome)
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Evaluation of the Biological Activities of Peptides from Epidermal Mucus of Marine Fish Species from Chilean Aquaculture
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Claudio A. Álvarez, Teresa Toro-Araneda, Juan Pablo Cumillaf, Belinda Vega, María José Tapia, Tanya Roman, Constanza Cárdenas, Valentina Córdova-Alarcón, Carlos Jara-Gutiérrez, Paula A. Santana and Fanny Guzmán
Mar. Drugs 2024, 22(6), 248; https://doi.org/10.3390/md22060248 - 28 May 2024
Abstract
The skin of fish is a physicochemical barrier that is characterized by being formed by cells that secrete molecules responsible for the first defense against pathogenic organisms. In this study, the biological activity of peptides from mucus of Seriola lalandi and Seriolella violacea
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The skin of fish is a physicochemical barrier that is characterized by being formed by cells that secrete molecules responsible for the first defense against pathogenic organisms. In this study, the biological activity of peptides from mucus of Seriola lalandi and Seriolella violacea were identified and characterized. To this purpose, peptide extraction was carried out from epidermal mucus samples of juveniles of both species, using chromatographic strategies for purification. Then, the peptide extracts were characterized to obtain the amino acid sequence by mass spectrometry. Using bioinformatics tools for predicting antimicrobial and antioxidant activity, 12 peptides were selected that were chemically produced by simultaneous synthesis using the Fmoc-Tbu strategy. The results revealed that the synthetic peptides presented a random coil or extended secondary structure. The analysis of antimicrobial activity allowed it to be discriminated that four peptides, named by their synthesis code 5065, 5069, 5070, and 5076, had the ability to inhibit the growth of Vibrio anguillarum and affected the copepodite stage of C. rogercresseyi. On the other hand, peptides 5066, 5067, 5070, and 5077 had the highest antioxidant capacity. Finally, peptides 5067, 5069, 5070, and 5076 were the most effective for inducing respiratory burst in fish leukocytes. The analysis of association between composition and biological function revealed that the antimicrobial activity depended on the presence of basic and aromatic amino acids, while the presence of cysteine residues increased the antioxidant activity of the peptides. Additionally, it was observed that those peptides that presented the highest antimicrobial capacity were those that also stimulated respiratory burst in leukocytes. This is the first work that demonstrates the presence of functional peptides in the epidermal mucus of Chilean marine fish, which provide different biological properties when the fish face opportunistic pathogens.
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(This article belongs to the Special Issue Marine Bioactive Peptides—Structure, Function, and Application 2.0)
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