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Marine Drugs
Volume 22
Issue 11
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Mar. Drugs, Volume 22, Issue 11 (November 2024) – 44 articles

Cover Story (view full-size image): This paper, entitled “Beyond Earth: Harnessing Marine Resources for Sustainable Space Colonization”, explores how marine organisms and their bioactive compounds can address critical challenges of space colonization. By integrating marine and space sciences, this review highlights the potential of algae, invertebrates, and microorganisms in life support systems, food production, pharmaceuticals, energy, and materials in terms of space habitats. With Earth’s oceans offering untapped potential, marine biotechnology emerges as a pivotal tool for humanity's expansion into space. This work envisions a future where humans not only survive but thrive beyond Earth, propelled by the innovative use of marine resources in the final frontier. View this paper
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25 pages, 992 KiB  
Review
Effects of Marine-Derived Components on Cardiovascular Disease Risk Factors and Gut Microbiota Diversity
by Ingrid Lamminpää, Amedeo Amedei and Cinzia Parolini
Mar. Drugs 2024, 22(11), 523; https://doi.org/10.3390/md22110523 - 20 Nov 2024
Viewed by 897
Abstract
Cardiovascular diseases (CVDs), which comprise coronary heart disease, hypertension, and stroke, collectively represent the number one cause of death globally. Atherosclerosis is the dominant cause of CVDs, and its risk factors are elevated levels of low-density lipoprotein cholesterol and triglycerides, hypertension, cigarette smoking, [...] Read more.
Cardiovascular diseases (CVDs), which comprise coronary heart disease, hypertension, and stroke, collectively represent the number one cause of death globally. Atherosclerosis is the dominant cause of CVDs, and its risk factors are elevated levels of low-density lipoprotein cholesterol and triglycerides, hypertension, cigarette smoking, obesity, and diabetes mellitus. In addition, diverse evidence highlights the role played by inflammation and clonal haematopoiesis, eventually leading to immunity involvement. The human microbiota project and subsequent studies using next-generation sequencing technology have indicated that thousands of different microbial species are present in the human gut. Disturbances in the gut microbiota (GM) composition, i.e., gut dysbiosis, have been associated with diseases ranging from localised gastrointestinal disorders to metabolic and cardiovascular illnesses. Of note, experimental studies suggested that GM, host immune cells, and marine-derived ingredients work together to ensure intestinal wall integrity. This review discusses current evidence concerning the links among GM, marine-derived ingredients, and human inflammatory disease. In detail, we summarise the impact of fish-derived proteins/peptides and algae components on CVD risk factors and gut microbiome. Furthermore, we describe the interplay among these dietary components, probiotics/prebiotics, and CVDs. Full article
(This article belongs to the Special Issue Marine Drug Research in Italy)
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19 pages, 6295 KiB  
Article
Chemical Investigation of the Mediterranean Sponge Crambe crambe by UHPLC-HRMS/MS via Manual and Computational Dereplication Approaches
by Pinelopi Vlachou, Nikolaos Tsafantakis, Nikola Milic, Alexandros Polyzois, Eirini Baira, Aikaterini Termentzi, Géraldine Le Goff, Jamal Ouazzani and Nikolas Fokialakis
Mar. Drugs 2024, 22(11), 522; https://doi.org/10.3390/md22110522 - 20 Nov 2024
Viewed by 469
Abstract
The CH2Cl2-MeOH extract of the Mediterranean sponge Crambe crambe was investigated via UHPLC-HRMS/MS employing manual dereplication and in silico mass spectrometry tools. A deconvolution approach was implemented for the extensive metabolic characterization of the sample, resulting in the annotation [...] Read more.
The CH2Cl2-MeOH extract of the Mediterranean sponge Crambe crambe was investigated via UHPLC-HRMS/MS employing manual dereplication and in silico mass spectrometry tools. A deconvolution approach was implemented for the extensive metabolic characterization of the sample, resulting in the annotation of 53 compounds. The analysis of data-dependent HRMS/MS scans was conducted to establish fragmentation patterns characteristic of each crambescin A, B, and C sub-families. Among the 39 compounds identified from these groups, 22 analogues were reported for the first time including 4 new homologous series that differed by the ratio of methylene units in the upper (n + 2) and lower (m + 2) alkyl side chains. More specifically, crambescins presenting m = 5 or 6 and n = 5 (compounds 7, 11, 22 and 24) as well as m = 5 or 6 and n = 4 (compounds 5, 6, 8, 9, 12 and 14) were characterized. Additionally, four new features, potentially corresponding to new crambescidin analogues (compounds 13, 15, 35, and 39), were also reported. The identity of the dereplicated features was further validated by studying crambescins’ spectral similarities through a feature-based molecular networking approach. Overall, this study suggests UHPLC-HRMS/MS—through the integration of manual and computational dereplication approaches—as a valuable tool for the investigation and high-throughput characterization of the C. crambe metabolome. Full article
(This article belongs to the Special Issue Marine Alkaloids: Sources, Discovery, Diversity, and Bioactivities)
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11 pages, 1411 KiB  
Article
Genome-Based Mining of Carpatamides I–M and Their Candidate Biosynthetic Gene Cluster
by Shu-Mei Shen, Yun-Chang Xie, Li-Rong Tu, Miao-Er Wu, Yan-Min Wang, Chun-Hui Song, Yu-Hui Sun and Ming-He Luo
Mar. Drugs 2024, 22(11), 521; https://doi.org/10.3390/md22110521 - 20 Nov 2024
Viewed by 376
Abstract
Chemically investigating the marine-derived Streptomyces parvus 1268 led to the isolation of a new compound of carpatamide I (1). Subsequent genomic analysis identified its candidate biosynthetic gene cluster ctd of approximately 44 kb. In order to obtain more carpatamide derivatives, we [...] Read more.
Chemically investigating the marine-derived Streptomyces parvus 1268 led to the isolation of a new compound of carpatamide I (1). Subsequent genomic analysis identified its candidate biosynthetic gene cluster ctd of approximately 44 kb. In order to obtain more carpatamide derivatives, we conducted the upregulation of Ctd14, which is a positive regulator, and obtained improvement of carpatamide I and four new compounds of carpatamides J–M (2–5). The structures of the aforementioned five new isolates were identified by a combination of ESI-HRMS as well as one-dimensional (1D) and two-dimensional (2D) spectral NMR datasets. Bioassay results showed that compounds 1–5 displayed anti-inflammatory activity and weak cytotoxicity against cell lines of A549, HT-29, and HepG2. Full article
(This article belongs to the Special Issue Marine Streptomyces-Derived Natural Products 2024)
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56 pages, 41424 KiB  
Review
Marine Fungi Bioactives with Anti-Inflammatory, Antithrombotic and Antioxidant Health-Promoting Properties Against Inflammation-Related Chronic Diseases
by Maria-Aliki Papikinou, Konstantinos Pavlidis, Paschalis Cholidis, Dimitrios Kranas, Theodora Adamantidi, Chryssa Anastasiadou and Alexandros Tsoupras
Mar. Drugs 2024, 22(11), 520; https://doi.org/10.3390/md22110520 - 18 Nov 2024
Viewed by 717
Abstract
Fungi play a fundamental role in the marine environment, being promising producers of bioactive molecules in the pharmacological and industrial fields, which have demonstrated potential health benefits against cardiovascular and other chronic diseases. This review pertains to the analysis of the lipid compositions [...] Read more.
Fungi play a fundamental role in the marine environment, being promising producers of bioactive molecules in the pharmacological and industrial fields, which have demonstrated potential health benefits against cardiovascular and other chronic diseases. This review pertains to the analysis of the lipid compositions across various species of marine fungi and their constantly discovered substances, as well as their anti-inflammatory, antioxidant, and antithrombotic effects. The health-promoting aspects of these microorganisms will be explored, through the investigation of several mechanisms of action and interference of their bioactives in biochemical pathways. Despite exceptional results in this field, the potential of marine microorganisms remains largely unexplored due to the limited number of specialists in marine microbiology and mycology, a relatively recent science with significant contributions and potential in biodiversity and biotechnology. Full article
(This article belongs to the Special Issue Diversity of Marine Fungi as a Source of Bioactive Natural Products, 2nd Edition)
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13 pages, 8761 KiB  
Article
Protective Effect of Marine Peptide from Netunea arthritica cumingii Against Gentamicin-Induced Hair Cell Damage in Zebrafish
by Hongbao Zheng, Ranran Zhu, Yun Zhang, Kechun Liu, Qing Xia, Peihai Li, Xiaoyue Sun, Chen Sun and Shanshan Zhang
Mar. Drugs 2024, 22(11), 519; https://doi.org/10.3390/md22110519 - 16 Nov 2024
Viewed by 624
Abstract
Auditory hair cell damage induced by aminoglycoside antibiotics (AmAn) leads to hearing loss, which has a serious effect on people’s mental and physical health. This ototoxicity is thought to be related with the excessive accumulation of reactive oxygen species (ROS) in hair cells. [...] Read more.
Auditory hair cell damage induced by aminoglycoside antibiotics (AmAn) leads to hearing loss, which has a serious effect on people’s mental and physical health. This ototoxicity is thought to be related with the excessive accumulation of reactive oxygen species (ROS) in hair cells. However, therapeutic agents that protect hair cells are limited. Marine peptides have been shown to have excellent potential applications in disease prevention and treatment. Therefore, this study investigated the protective effects of an active peptide from Neptunea arthritica cumingii against AmAn-induced hair cell damage using the model of hair cell damage zebrafish. We identified the number, ultrastructure, and function of hair cells using fluorescence probes and scanning electron microscopy. The uptake of AmAn, ROS level, mitochondrial permeability transition pore, and apoptosis in hair cells were also tested by fluorescence labeling and TUNEL assay. The molecular mechanism for hair cell protection exerted by the peptide was detected by a real-time quantitative PCR assay. The results indicated that the peptide suppressed the uptake of AmAn but did not damage the function of hair cells mediating hearing. It also prevented ROS accumulation, decreased the occurrence of apoptosis, and rescued the abnormal opening and expressions of mitochondrial permeability transition pore and genes related to antioxidants. The peptide may be an effective therapeutic agent for AmAn-induced ototoxicity. In the future, we plan to use mammalian models to further investigate the otoprotective effect of the peptide. Full article
(This article belongs to the Special Issue Zebrafish Models in Marine Drug Discovery)
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22 pages, 1491 KiB  
Article
Unveiling the Lipid Features and Valorization Potential of Atlantic Salmon (Salmo salar) Heads
by João Pedro Monteiro, Tiago Sousa, Tânia Melo, Carla Pires, António Marques, Maria Leonor Nunes, Ricardo Calado and M. Rosário Domingues
Mar. Drugs 2024, 22(11), 518; https://doi.org/10.3390/md22110518 - 15 Nov 2024
Viewed by 992
Abstract
The sustainable utilization of co-products derived from the salmon processing industry is crucial for enhancing the viability and decreasing the environmental footprint of both capture and aquaculture operations. Salmon (Salmo salar) is one of the most consumed fish worldwide and a [...] Read more.
The sustainable utilization of co-products derived from the salmon processing industry is crucial for enhancing the viability and decreasing the environmental footprint of both capture and aquaculture operations. Salmon (Salmo salar) is one of the most consumed fish worldwide and a major species produced in aquaculture. As such, significant quantities of salmon co-products are produced in pre-commercialization processing/steaking procedures. The present study characterized a specific co-product derived from the processing of salmon: minced salmon heads. More specifically, this work aimed to reveal the nutritional profile of this co-product, with a special focus on its lipid content, including thoroughly profiling fatty acids and fully appraising the composition in complex lipids (polar lipids and triglycerides) for the first time. The antioxidant potential of lipid extracts from this salmon co-product was also studied in order to bioprospect lipid functional properties and possibly unveil new pathways for added-value applications. Our analysis indicated that these minced salmon heads are exceptionally rich in lipids. Oleic acid is the most prevalent fatty acid in this co-product, followed by palmitic acid, stearic acid, and linoleic acid. Moreover, relevant lipid indexes inferred from the fatty acid composition of this co-product revealed good nutritional traits. Lipidome analysis revealed that triglycerides were clearly the predominant lipid class present in this co-product while phospholipids, as well as ceramides, were also present, although in minimal quantities. The bioprospecting of antioxidant activity in the lipid extracts of the minced salmon heads revealed limited results. Given the high concentration of triglycerides, minced salmon heads can constitute a valuable resource for industrial applications from the production of fish oil to biodiesel (as triglycerides can be easily converted into fatty acid methyl esters), as well as possible ingredients for cosmetics, capitalizing on their alluring emollient properties. Overall, the valorization of minced salmon heads, major co-products derived from the processing of one of the most intensively farmed fish in the world, not only offers economic benefits but also contributes to the sustainability of the salmon processing industry by reducing waste and promoting a more efficient use of marine bioresources. Full article
(This article belongs to the Special Issue Fatty Acids from Marine Organisms, 2nd Edition)
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13 pages, 2160 KiB  
Article
Heterocycles and a Sorbicillinoid from the Coral-Derived Fungus Penicillium chrysogenum
by Junjie Yang, Yuan Zong, Cili Wang, Kai Li, Yue Zhang and Pinglin Li
Mar. Drugs 2024, 22(11), 517; https://doi.org/10.3390/md22110517 - 15 Nov 2024
Viewed by 553
Abstract
A detailed chemical study of the culture of a coral-derived fungus Penicillium chrysogenum resulted in the isolation and identification of four new aromatic heterocycles chrysoquinazolinones A–B (1–2) and chrysobenzothiazoles A–B (3–4), along with a new [...] Read more.
A detailed chemical study of the culture of a coral-derived fungus Penicillium chrysogenum resulted in the isolation and identification of four new aromatic heterocycles chrysoquinazolinones A–B (1–2) and chrysobenzothiazoles A–B (3–4), along with a new sorbicillinoid 4-carboxylsorbicillin (5). Chrysoquinazolinones A–B (1–2) combine a quinazolinone fragment with a bicyclo[2.2.2]octane or a pyrrolidone moiety, respectively, demonstrating the unexpected structures of marine natural products. Chrysobenzothiazoles A–B (3–4) possess a benzothiazole system and are the second isolation of this class of skeleton compounds from marine organisms. The existence of the pair of enantiomers (±3) was deduced by chiral HPLC analysis. Their structures and absolute configurations were elucidated by detailed spectroscopic analysis, comparison with the literature data, single-crystal X-ray crystallographic analysis and TDDFT-ECD calculations. Compound 5 exhibited moderate cytotoxicity against K562 and NCI-H446 cell lines, with IC50 values of 15.00 μM and 16.87 μM, respectively. Full article
(This article belongs to the Special Issue Pharmacological Potential of Marine Natural Products, 2nd Edition)
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16 pages, 1106 KiB  
Article
Ultrasound-Assisted Extraction of Alginate from Fucus vesiculosus Seaweed By-Product Post-Fucoidan Extraction
by Viruja Ummat, Ming Zhao, Saravana Periaswamy Sivagnanam, Shanmugapriya Karuppusamy, Henry Lyons, Stephen Fitzpatrick, Shaba Noore, Dilip K. Rai, Laura G. Gómez-Mascaraque, Colm O’Donnell, Anet Režek Jambark and Brijesh Kumar Tiwari
Mar. Drugs 2024, 22(11), 516; https://doi.org/10.3390/md22110516 - 14 Nov 2024
Viewed by 632
Abstract
The solid phase byproduct obtained after conventional fucoidan extraction from the brown seaweed Fucus vesiculosus can be used as a source containing alginate. This study involves ultrasound-assisted extraction (UAE) of alginate from the byproduct using sodium bicarbonate. Response surface methodology (RSM) was applied [...] Read more.
The solid phase byproduct obtained after conventional fucoidan extraction from the brown seaweed Fucus vesiculosus can be used as a source containing alginate. This study involves ultrasound-assisted extraction (UAE) of alginate from the byproduct using sodium bicarbonate. Response surface methodology (RSM) was applied to obtain the optimum conditions for alginate extraction. The ultrasound (US) treatments included 20 kHz of frequency, 20–91% of amplitude, and an extraction time of 6–34 min. The studied investigated the crude alginate yield (%), molecular weight, and alginate content (%) of the extracts. The optimum conditions for obtaining alginate with low molecular weight were found to be 69% US amplitude and sonication time of 30 min. The alginate extracts obtained were characterized using Fourier transform infrared (FTIR) spectroscopy, thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC). Ultrasound-assisted extraction involving a short treatment lasting 6–34 min was found to be effective in extracting alginate from the byproduct compared to the conventional extraction of alginate using stirring at 415 rpm and 60 °C for 24 h. The US treatments did not adversely impact the alginate obtained, and the extracted alginates were found to have similar characteristics to the alginate obtained from conventional extraction and commercial sodium alginate. Full article
(This article belongs to the Special Issue Green Extraction for Obtaining Marine Bioactive Products)
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16 pages, 1407 KiB  
Article
The Effects of Agaro-Oligosaccharides Produced by Marine Bacteria (Rheinheimera sp. (HY)) Possessing Agarose-Degrading Enzymes on Myotube Function
by Youshi Huang, Takuya Hirose, Jyh-Ming Tsai and Katsuya Hirasaka
Mar. Drugs 2024, 22(11), 515; https://doi.org/10.3390/md22110515 - 14 Nov 2024
Viewed by 701
Abstract
Agarase and its metabolites are reported to have applications in a variety of fields, but there have been few studies of the effects of agaro-oligosaccharide hydrolysate on muscle function. In this study, we analyzed the functionality of agarase and its metabolites in bacteria [...] Read more.
Agarase and its metabolites are reported to have applications in a variety of fields, but there have been few studies of the effects of agaro-oligosaccharide hydrolysate on muscle function. In this study, we analyzed the functionality of agarase and its metabolites in bacteria isolated from seawater. A bacterium with agar-degrading activity was isolated from Shimabara, Nagasaki, Japan. Through 16S rRNA sequence alignment, it was identified as being closely related to Rheinheimera sp. WMF-1 and was provisionally named Rheinheimera sp. (HY). Crude enzymes derived from this bacterium demonstrated an ability to hydrolyze various polysaccharides, including agar, agarose, and starch, with the highest specificity observed for agarose. The optimum pH and temperature were pH 10 and 50 °C. A glycoside bond specificity analysis of enzymatic activity indicated the cleavage of the α-linkage. Next, we investigated the functional effects of agaro-oligosaccharides on C2C12 myotubes. Treatment with 10–30 kDa oligosaccharides significantly increased the hypertrophy rate, diameter, and expression of myosin heavy-chain genes in C2C12 myotubes. These results indicate that the agaro-oligosaccharides produced by the enzymes identified in this study improve muscle mass, suggesting their potential contribution to muscle function. Full article
(This article belongs to the Special Issue Marine Proteins and Enzymes: Bioactivities and Medicinal Applications)
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15 pages, 22129 KiB  
Article
Biodiversity and Hemolytic Toxicity of the Genus Heterocapsa (Dinophyceae) in the Beibu Gulf, China
by Yixiao Xu, Nina Dzhembekova, Kirsty F. Smith, Haifeng Gu, Uwe John, Huanda Xie, Yujuan Wen and Miao Wu
Mar. Drugs 2024, 22(11), 514; https://doi.org/10.3390/md22110514 - 14 Nov 2024
Viewed by 616
Abstract
The dinoflagellate genus Heterocapsa includes several widely distributed and potentially toxic species associated with Harmful Algal Blooms (HABs), particularly affecting the Western Pacific Ocean. To reveal the biodiversity of Heterocapsa in Beibu Gulf, six strains were morphologically characterized using light and scanning electron [...] Read more.
The dinoflagellate genus Heterocapsa includes several widely distributed and potentially toxic species associated with Harmful Algal Blooms (HABs), particularly affecting the Western Pacific Ocean. To reveal the biodiversity of Heterocapsa in Beibu Gulf, six strains were morphologically characterized using light and scanning electron microscopy, while large subunit rDNA (LSU rDNA) and internal transcribed spacer (ITS) were sequenced for phylogenetic analysis through maximum likelihood and Bayesian inferences. Two strains (BGERL169, BGERL170) were identified as Heterocapsa philippinensis ribotype I, three (BGERL171-BGERL173) as a new Heterocapsa philippinensis ribotype II, and one strain (BGERL174) as Heterocapsa pseudotriquetra. Cells of H. philippinensis were ovoid to spherical, yellowish-brown, with reticulate chloroplasts, and had a sausage-shaped nucleus positioned longitudinally along the dorsal side of the cell, and the theca was arranged in Po, cp, X, 5′, 3a, 7″, 6c, 5s, 5‴, 2⁗. Additionally, BGERL169 and BGERL171 showed no hemolytic toxicity in rabbit erythrocyte lysis assays. To the best of our knowledge, this research provides the first morphological and phylogenetic analysis of H. philippinensis, including the identification of a new ribotype, as well as the discovery of H. pseudotriquetra in Chinese waters. The findings contribute to the understanding of Heterocapsa species biogeography and toxicity in Chinese waters, offering valuable data for future HAB monitoring in Beibu Gulf. Full article
(This article belongs to the Special Issue Marine Biotoxins 3.0)
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19 pages, 99468 KiB  
Article
2-Acetamidophenol (2-AAP) Suppresses the Progression of Atherosclerosis by Alleviating Hyperlipidemia and Attenuating the Ferroptosis Pathway
by Xiaohan Zang, Yongcheng Wang, Cong Han, Lishuang Cui, Haojie Liu, Shuimiao Tian, Kechun Liu, Peihai Li, Chen Sun, Qing Xia and Yun Zhang
Mar. Drugs 2024, 22(11), 513; https://doi.org/10.3390/md22110513 - 13 Nov 2024
Viewed by 476
Abstract
Hyperlipidemia and consequent endothelial inflammation, along with foam cell generation, promote the progression of atherosclerosis (AS). Here, we aimed to investigate the effects of 2-acetamidophenol (2-AAP), which was selected by zebrafish phenotypic screening, in alleviating AS by relieving hyperlipidemia and inhibiting foam cell [...] Read more.
Hyperlipidemia and consequent endothelial inflammation, along with foam cell generation, promote the progression of atherosclerosis (AS). Here, we aimed to investigate the effects of 2-acetamidophenol (2-AAP), which was selected by zebrafish phenotypic screening, in alleviating AS by relieving hyperlipidemia and inhibiting foam cell formation, as well as the underlying mechanisms. In a zebrafish hyperlipidemia model, 2-AAP increased lipid-lowering efficacy; alleviated TC, TG, LDL-C, and MDA levels; elevated HDL-C and T-SOD levels; significantly improved intravascular macrophage aggregation; and improved blood flow. In an ox-LDL-induced RAW264.7 model, 2-AAP inhibited lipid phagocytosis in RAW264.7 cells; reduced the intracellular TC, TG, FC, and CE contents; and decreased the CE/TC ratio, thus slowing foam cell generation. In addition, 2-AAP alleviated intracellular ROS and ferrous ion accumulation in RAW264.7 cells, reduced the MDA content, and increased GPX4 viability. Furthermore, transcriptome analyses and gene expression validation showed 2-AAP treatment upregulates genes related to GSH synthesis and transport, such as gclc, gclm, gss, and gpx4a, and enhanced the expression levels of genes involved in the storage and transportation of iron ions, such as fpn1, fth, and g6pd, indicating that 2-AAP dramatically regulated the ferroptosis and glutathione metabolic pathways. Overall, our study demonstrated that 2-AAP demonstrated potential in AS by alleviating hyperlipidemia and attenuating the ferroptosis pathway and provided evidence supporting the future application of 2-AAP in AS treatment. Full article
(This article belongs to the Special Issue Zebrafish Models in Marine Drug Discovery)
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13 pages, 2988 KiB  
Article
Hot-Melt Extrusion Drug Delivery System-Formulated Haematococcus pluvialis Extracts Regulate Inflammation and Oxidative Stress in Lipopolysaccharide-Stimulated Macrophages
by Tae-Young Gil, Ha-Yeon Sim, Ha-Yeon Lee, Suji Ryu, Jong-Suep Baek, Dae Geun Kim, Jaehoon Sim and Hyo-Jin An
Mar. Drugs 2024, 22(11), 512; https://doi.org/10.3390/md22110512 - 13 Nov 2024
Viewed by 527
Abstract
Haematococcus pluvialis contains valuable bioactive compounds, including astaxanthin, proteins, and fatty acids. Astaxanthin is known for its various health benefits, such as preserving the redox balance and reducing inflammation. However, its low stability and poor water solubility present challenges for various applications. Hot-melt [...] Read more.
Haematococcus pluvialis contains valuable bioactive compounds, including astaxanthin, proteins, and fatty acids. Astaxanthin is known for its various health benefits, such as preserving the redox balance and reducing inflammation. However, its low stability and poor water solubility present challenges for various applications. Hot-melt extrusion (HME) technology enhances the aqueous solubility of H. pluvialis extracts, increasing the usable astaxanthin content through nanoencapsulation (HME-DDS-applied extracts, ASX-60F and ASX-100F). This study compared the effects of HME-DDS-derived extracts (ASX-60F and ASX-100F) and the non-applied extract (ASX-C) under inflammatory and oxidative stress conditions. In animal models of sepsis, 60F and 100F treatment exhibited higher survival rates and a lower expression of pro-inflammatory biomarkers compared to those treated with C. In lipopolysaccharide-stimulated RAW 264.7 macrophages, nitric oxide (NO) production and the expression of pro-inflammatory mediators such as cyclooxygenase-2 and inducible NO synthase were reduced by 60F or 100F treatments via ERK/p-38 mitogen-activated protein kinase (MAPK) signaling. Moreover, 60F or 100F inhibited reactive oxygen species production regulated by nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) signaling. Collectively, these findings suggest that HME-DDS-derived H. pluvialis extracts exert anti-inflammatory and antioxidant effects by inhibiting MAPK phosphorylation and activating Nrf2/HO-1 expression. Full article
(This article belongs to the Section Marine Pharmacology)
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13 pages, 1750 KiB  
Article
Chaetomorpha linum Extract as a Source of Antimicrobial Compounds: A Circular Bioeconomy Approach
by Roberta Barletta, Alfonso Trezza, Michela Geminiani, Luisa Frusciante, Tommaso Olmastroni, Filomena Sannio, Jean-Denis Docquier and Annalisa Santucci
Mar. Drugs 2024, 22(11), 511; https://doi.org/10.3390/md22110511 - 13 Nov 2024
Viewed by 712
Abstract
The circular bioeconomy is currently a promising model for repurposing natural sources; these sources include plants due to their abundance of bioactive compounds. This study evaluated the antimicrobial properties of a Chaetomorpha linum extract. Chaetomorpha linum is an invasive macroalga from the Orbetello [...] Read more.
The circular bioeconomy is currently a promising model for repurposing natural sources; these sources include plants due to their abundance of bioactive compounds. This study evaluated the antimicrobial properties of a Chaetomorpha linum extract. Chaetomorpha linum is an invasive macroalga from the Orbetello Lagoon (Tuscany, Italy), which grows in nutrient-rich environments and has been forming extended mats since 2005. The biomass is mechanically harvested and treated as waste, consuming considerable manpower and financial resources. As a potential way to increase the value of such waste, this study found that C. linum extract (CLE) is a source of antimicrobial compounds. The phytochemical characterization of the extract revealed the predominant presence of palmitic acid, a fatty acid with known antimicrobial activity. Based on such findings, four bacterial species of high clinical relevance (Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli) were tested, revealing a notable antibacterial activity of the extract on Enterococcus faecalis (MIC, 32 μg/mL). Computational analyses identified a potential Enterococcus faecalis molecular target for palmitic acid, offering molecular insights on the interaction. This study presents a comprehensive in vitro and in silico approach for drug and target discovery studies by repurposing C. linum as a source of antimicrobial bioactive compounds. Full article
(This article belongs to the Special Issue Marine Drug Research in Italy)
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26 pages, 2572 KiB  
Review
Marine Algal Toxins and Public Health: Insights from Shellfish and Fish, the Main Biological Vectors
by Kuan-Kuan Yuan, Hong-Ye Li and Wei-Dong Yang
Mar. Drugs 2024, 22(11), 510; https://doi.org/10.3390/md22110510 - 10 Nov 2024
Viewed by 802
Abstract
Exposure to toxigenic harmful algal blooms (HABs) can result in widely recognized acute poisoning in humans. The five most commonly recognized HAB-related illnesses are diarrhetic shellfish poisoning (DSP), paralytic shellfish poisoning (PSP), amnesic shellfish poisoning (ASP), neurotoxic shellfish poisoning (NSP), and ciguatera poisoning [...] Read more.
Exposure to toxigenic harmful algal blooms (HABs) can result in widely recognized acute poisoning in humans. The five most commonly recognized HAB-related illnesses are diarrhetic shellfish poisoning (DSP), paralytic shellfish poisoning (PSP), amnesic shellfish poisoning (ASP), neurotoxic shellfish poisoning (NSP), and ciguatera poisoning (CP). Despite being caused by exposure to various toxins or toxin analogs, these clinical syndromes share numerous similarities. Humans are exposed to these toxins mainly through the consumption of fish and shellfish, which serve as the main biological vectors. However, the risk of human diseases linked to toxigenic HABs is on the rise, corresponding to a dramatic increase in the occurrence, frequency, and intensity of toxigenic HABs in coastal regions worldwide. Although a growing body of studies have focused on the toxicological assessment of HAB-related species and their toxins on aquatic organisms, the organization of this information is lacking. Consequently, a comprehensive review of the adverse effects of HAB-associated species and their toxins on those organisms could deepen our understanding of the mechanisms behind their toxic effects, which is crucial to minimizing the risks of toxigenic HABs to human and public health. To this end, this paper summarizes the effects of the five most common HAB toxins on fish, shellfish, and humans and discusses the possible mechanisms. Full article
(This article belongs to the Special Issue Commemorating the Launch of the Section "Marine Toxins")
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32 pages, 4680 KiB  
Article
Comparison of Microalgae Nannochloropsis oceanica and Chlorococcum amblystomatis Lipid Extracts Effects on UVA-Induced Changes in Human Skin Fibroblasts Proteome
by Sinemyiz Atalay Ekiner, Agnieszka Gęgotek, Pedro Domingues, Maria Rosário Domingues and Elżbieta Skrzydlewska
Mar. Drugs 2024, 22(11), 509; https://doi.org/10.3390/md22110509 - 10 Nov 2024
Viewed by 1591
Abstract
Lipid extracts from the microalgae Nannochloropsis oceanica and Chlorococcum amblystomatis have great potential to prevent ultraviolet A (UVA)-induced metabolic disorders. Therefore, the aim of this study has been to analyze their cytoprotective effect, focused on maintaining intracellular redox balance and inflammation in UVA-irradiated [...] Read more.
Lipid extracts from the microalgae Nannochloropsis oceanica and Chlorococcum amblystomatis have great potential to prevent ultraviolet A (UVA)-induced metabolic disorders. Therefore, the aim of this study has been to analyze their cytoprotective effect, focused on maintaining intracellular redox balance and inflammation in UVA-irradiated skin fibroblasts, at the proteome level. The above lipid extracts reversed the suppression of the antioxidant response caused by UVA radiation, which was more visible in the case of C. amblystomatis. Modulations of interactions between heme oxygenase-1 and matrix metalloproteinase 1/Parkinson’s disease protein 7/transcript1-α/β, as well as thioredoxin and migration inhibitory factor/Parkinson’s disease protein 7/calnexin/ATPase p97, created key molecular signaling underlying their cytoprotective actions. Moreover, they reduced pro-inflammatory processes in the control group but they also showed the potential to regulate the cellular inflammatory response by changing inflammasome signaling associated with the changes in the caspase-1 interaction area, including heat shock proteins HSP90, HSPA8, and vimentin. Therefore, lipid extracts from N. oceanica and C. amblystomatis protect skin fibroblast metabolism from UVA-induced damage by restoring the redox balance and regulating inflammatory signaling pathways. Thus, those extracts have proven to have great potential to be used in cosmetic or cosmeceutical products to protect the skin against the effects of solar radiation. However, the possibility of their use requires the evaluation of their effects at the skin level in in vivo and clinical studies. Full article
(This article belongs to the Special Issue Applications of Lipids from Marine Sources)
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18 pages, 1783 KiB  
Article
New Polyhydroxysteroid Glycosides with Antioxidant Activity from the Far Eastern Sea Star Ceramaster patagonicus
by Timofey V. Malyarenko, Viktor M. Zakharenko, Alla A. Kicha, Arina I. Ponomarenko, Igor V. Manzhulo, Anatoly I. Kalinovsky, Roman S. Popov, Pavel S. Dmitrenok and Natalia V. Ivanchina
Mar. Drugs 2024, 22(11), 508; https://doi.org/10.3390/md22110508 - 10 Nov 2024
Viewed by 740
Abstract
Four new glycosides of polyhydroxysteroids, ceramasterosides A, B, D, and E (1–4), and two previously known compounds, ceramasteroside C1 (5) and attenuatoside B-I (6), were isolated from an extract of a deep-sea sea star [...] Read more.
Four new glycosides of polyhydroxysteroids, ceramasterosides A, B, D, and E (1–4), and two previously known compounds, ceramasteroside C1 (5) and attenuatoside B-I (6), were isolated from an extract of a deep-sea sea star species, the orange cookie star Ceramaster patagonicus. The structures of 1–4 were elucidated by the extensive NMR and ESIMS methods. Steroid monoglycosides 1 and 2 had a common 3β,6α,8,15β,16β-pentahydroxysteroid nucleus and a C–29 oxidized stigmastane side chain and differed from each other only in monosaccharide residues. Ceramasteroside A (1) contained 3-O-methyl-4-O-sulfated β-D-xylopyranose, while ceramasteroside B (2) had 3-O-methyl-4-O-sulfated β-D-glucopyranose, recorded from starfish-derived steroid glycosides for the first time. Their biological activity was studied using a model of lipopolysaccharide-induced (LPS) inflammation in a SIM-A9 murine microglial cell line. During the LPS-induced activation of microglial cells, 1, 3, and 5, at a non-toxic concentration of 1 µM, showed the highest efficiency in reducing the production of intracellular NO, while 4 proved to be most efficient in reducing the extracellular nitrite production. All the test compounds reduced the LPS-induced malondialdehyde (MDA) production. The in vitro experiments have demonstrated, for the first time, the antioxidant activity of the compounds under study. Full article
(This article belongs to the Special Issue Biologically Active Compounds from Marine Invertebrates 2025)
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12 pages, 4238 KiB  
Article
Salmon Nasal Cartilage-Derived Proteoglycans Alleviate Monosodium Iodoacetate-Induced Osteoarthritis in Rats
by Inae Jeong, Jinbum Park, Shinjung Park, Tatuya Wada, Dae Soo Lim and Ok-Kyung Kim
Mar. Drugs 2024, 22(11), 507; https://doi.org/10.3390/md22110507 - 8 Nov 2024
Viewed by 558
Abstract
Osteoarthritis is a chronic inflammatory condition characterized by the degeneration of joint cartilage and underlying bone, resulting in pain, swelling, and reduced mobility. This study evaluates the efficacy of salmon nasal cartilage-derived proteoglycans in mitigating osteoarthritis symptoms and investigates the underlying molecular mechanisms. [...] Read more.
Osteoarthritis is a chronic inflammatory condition characterized by the degeneration of joint cartilage and underlying bone, resulting in pain, swelling, and reduced mobility. This study evaluates the efficacy of salmon nasal cartilage-derived proteoglycans in mitigating osteoarthritis symptoms and investigates the underlying molecular mechanisms. This study employed a rat model of osteoarthritis induced by monosodium iodoacetate (MIA) injection. The rats were orally administered salmon nasal cartilage-derived proteoglycans or ibuprofen. Key aspects of osteoarthritis pathology, including impaired exercise ability, inflammation, extracellular matrix degradation, and chondrocyte apoptosis, were assessed using histological analysis, micro-CT, treadmill testing, serum assays, and mRNA/protein expression studies. The MIA injection caused significant cartilage damage, reduced bone mineral density, and impaired exercise ability. Additionally, it elevated serum levels of prostaglandin E2 and nitric oxide, increased the mRNA and protein levels of inflammation-related factors, and activated apoptosis signaling pathways in cartilage. Treatment with salmon nasal cartilage-derived proteoglycans significantly improved cartilage morphology and mineralization, reduced inflammation, and inhibited apoptosis signaling pathways, with effects comparable to those observed with ibuprofen treatment. These findings highlight the potential of salmon nasal cartilage-derived proteoglycans as a therapeutic agent for managing osteoarthritis by effectively reducing inflammation, preventing cartilage degradation, and inhibiting chondrocyte apoptosis. Full article
(This article belongs to the Special Issue Bioactive Compounds from Marine Fish)
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11 pages, 3130 KiB  
Communication
Aeruginosin 525 (AER525) from Cyanobacterium Aphanizomenon Sp. (KUCC C2): A New Serine Proteases Inhibitor
by Donata Overlingė, Marta Cegłowska, Robert Konkel and Hanna Mazur-Marzec
Mar. Drugs 2024, 22(11), 506; https://doi.org/10.3390/md22110506 - 8 Nov 2024
Viewed by 599
Abstract
Aeruginosins (AERs) are one of the most common classes of cyanobacterial peptides synthesised through a hybrid non-ribosomal peptide synthase/polyketide synthase pathway. They have been found in Microcystis, Nodularia spumigena, Oscillatoria/Plantothrix, and Nostoc. The presence of AER in Aphanizomenon [...] Read more.
Aeruginosins (AERs) are one of the most common classes of cyanobacterial peptides synthesised through a hybrid non-ribosomal peptide synthase/polyketide synthase pathway. They have been found in Microcystis, Nodularia spumigena, Oscillatoria/Plantothrix, and Nostoc. The presence of AER in Aphanizomenon isolated from the Curonian Lagoon was reported for the first time in our previous work. Here, the structure of aeruginosin 525 (AER525), isolated from Aphanizomenon sp. KUCC C2, was characterised based on high-resolution mass spectrometry. This new AER variant shows potent activity against thrombin. It also inhibits trypsin and carboxypeptidase A but has no effect on elastase and chymotrypsin. In terms of the N-terminal residue and biological activity, AER525 displaces some similarity to dysinosins, which belongs to the most potent inhibitors of thrombin among AERs. The findings underline the potential of AER525 as a new anticoagulant agent. Full article
(This article belongs to the Special Issue Bioactive Metabolites Produced by Marine Cyanobacteria and Other Microalgae)
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19 pages, 2361 KiB  
Article
Nannochloropsis oceanica as a Source of Bioactive Compounds: Mapping the Effects of Cultivation Conditions on Biomass Productivity and Composition Using Response Surface Methodology
by Emil Gundersen, Jette Jakobsen, Susan Løvstad Holdt and Charlotte Jacobsen
Mar. Drugs 2024, 22(11), 505; https://doi.org/10.3390/md22110505 - 6 Nov 2024
Viewed by 1404
Abstract
Microalga Nannochloropsis oceanica presents a promising source of high-value food ingredients such as protein, omega-3 fatty acids, and vitamins. To fully unlock its potential, a thorough understanding of how cultivation conditions affect both growth and the nutritional composition is required. Hence, this study [...] Read more.
Microalga Nannochloropsis oceanica presents a promising source of high-value food ingredients such as protein, omega-3 fatty acids, and vitamins. To fully unlock its potential, a thorough understanding of how cultivation conditions affect both growth and the nutritional composition is required. Hence, this study aimed to test and model the effects of temperature, light intensity, and salinity on biomass productivity and the final contents of protein, eicosapentaenoic acid (EPA), and vitamin K2 using response surface methodology (RSM). The RSM experiment revealed that the highest temperature and light intensity tested favored biomass productivity and protein content. According to the generated models, the two responses peaked with 0.135 g DM·L−1·day−1 and 0.559 g·g−1 DM, respectively, at 27 °C and 300–350 µmol·m−2·s−1. In contrast, the contents of both EPA and menaquinone-4 (MK-4), the only detected K vitamer, were stimulated at the lowest tested temperature. Based on the generated models, the two responses peaked with 0.037 g·g−1 DM and 89.3 µg·g−1 DM, respectively, at 19 °C combined with 3.0% salinity (EPA) or 120 µmol·m−2·s−1 (MK-4). Although additional optima may exist beyond the tested conditions, these findings provide valuable information on N. oceanica’s cellular response to changes in key cultivation conditions. Furthermore, it shows that two-stage cultivation may be needed to fully unlock the potential of this microalga as a future source of valuable lipid ingredients. Full article
(This article belongs to the Special Issue High-Value Algae Products)
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10 pages, 1321 KiB  
Article
Influence of Silicate Concentrations on Growth, Carotenoid, and Fatty Acid Profiles of the Marine Diatom Conticribra weissflogii
by David Kwame Amenorfenyo, Feng Li, Xiangyu Rui, Xianghu Huang and Changling Li
Mar. Drugs 2024, 22(11), 504; https://doi.org/10.3390/md22110504 - 6 Nov 2024
Viewed by 626
Abstract
Enhancing microalgal growth and bioactive compound production is becoming a duty for improving photosynthetic microorganisms. In this study, the growth, carotenoid, and fatty acid profiles of Conticribra weissflogii were studied under four different silicate concentrations and silicate-deficient conditions in an f/2 medium with [...] Read more.
Enhancing microalgal growth and bioactive compound production is becoming a duty for improving photosynthetic microorganisms. In this study, the growth, carotenoid, and fatty acid profiles of Conticribra weissflogii were studied under four different silicate concentrations and silicate-deficient conditions in an f/2 medium with continuous aeration, light intensity (30 ± 2 µmol m−2 s−1), salinity (25 ± 2‰), pH (8), and temperature (25 ± 2 °C). At the end of the experiment, we observed that a silicate concentration of 120 mg L−1 produced the maximum biomass dry weight (0.86 g L−1), carotenoid content (1.63 µg mL−1), and fucoxanthin content (1.23 mg g−1) in C. weissflogii. The eicosapentaenoic acid (EPA) (11,354.37 µg g−1), docosahexaenoic acid (DHA) (2516.16 µg g−1), gamma-linolenic acid (C18:3n6) (533.51 µg g−1), and arachidonic acid (C20:4n6) (1261.83 µg g−1) contents were significantly higher at Si 120 mg L−1. The results further showed the maximum fatty acid content in C. weissflogii at Si 120 mg L−1. However, the silicate-deficient conditions (Si 0 mg L−1) resulted in higher levels of saturated fatty acids (38,038.62 µg g−1). This study presents a practical approach for the large-scale optimization of biomass, carotenoid, fucoxanthin, and fatty acid production in C. weissflogii for commercial purposes. Full article
(This article belongs to the Special Issue Marine Biorefinery for Bioactive Compounds Production)
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15 pages, 3337 KiB  
Article
Moisturizing Effects of Alcalase Hydrolysate Fractions from Haliotis discus Viscera, a Marine Organism, on Human Dermal Fibroblasts, HaCaT Keratinocytes, and Reconstructed Human Skin Tissues
by Nalae Kang, Eun-A Kim, Seong-Yeong Heo, Jun-Ho Heo, Ginnae Ahn and Soo-Jin Heo
Mar. Drugs 2024, 22(11), 503; https://doi.org/10.3390/md22110503 - 6 Nov 2024
Viewed by 536
Abstract
Haliotis discus, an abalone, is a marine gastropod mollusk that has been cultivated globally owing to its nutritional value and high market demand. However, the visceral parts of H. discus are typically discarded as by-products, highlighting the need to explore their potential [...] Read more.
Haliotis discus, an abalone, is a marine gastropod mollusk that has been cultivated globally owing to its nutritional value and high market demand. However, the visceral parts of H. discus are typically discarded as by-products, highlighting the need to explore their potential value in developing cosmeceuticals and pharmaceuticals. This study investigated the potential moisturizing effects of H. discus visceral tissues. Various hydrolysates from H. discus viscera tissue were evaluated for proximate composition, radical scavenging, and hyaluronidase inhibition activities. Alcalase hydrolysate was isolated using gel filtration chromatography (GFC), and its moisturizing effects were tested on human dermal fibroblasts (HDF), HaCaT keratinocytes, and reconstructed human skin tissue. The Alcalase hydrolysate showed the highest extraction yield, radical scavenging, and hyaluronidase inhibition activities. The Alcalase hydrolysate GFC fraction 1 increased collagen synthesis-related molecules, including procollagen type 1 in HDF and hyaluronic acid-related molecules in HaCaT cells. These moisturizing effects were confirmed in reconstructed human skin tissues by increased levels of aquaporin 3 and filaggrin. Fraction 1 consisted of two main peptides: DNPLLPGPPF and SADNPLLPGPPF. In conclusion, H. discus Alcalase hydrolysate and its fractions have potential moisturizing properties and can be used as cosmeceuticals. Full article
(This article belongs to the Special Issue Marine Bioactives for Functional Cosmetics with Health-Promoting Properties)
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18 pages, 5059 KiB  
Article
Batzelladine D, a Marine Natural Product, Reverses the Fluconazole Resistance Phenotype Mediated by Transmembrane Transporters in Candida albicans and Interferes with Its Biofilm: An In Vitro and In Silico Study
by Levy T. S. Domingos, Daniel C. de Moraes, Mário F. C. Santos, José A. R. Curvelo, Brayan Bayona-Pacheco, Edgar A. Marquez, Anthony W. B. Martinez, Roberto G. S. Berlinck and Antonio Ferreira-Pereira
Mar. Drugs 2024, 22(11), 502; https://doi.org/10.3390/md22110502 - 5 Nov 2024
Viewed by 671
Abstract
Numerous Candida species are responsible for fungal infections; however, Candida albicans stands out among the others. Treatment with fluconazole is often ineffective due to the resistance phenotype mediated by transmembrane transporters and/or biofilm formation, mechanisms of resistance commonly found in C. albicans strains. [...] Read more.
Numerous Candida species are responsible for fungal infections; however, Candida albicans stands out among the others. Treatment with fluconazole is often ineffective due to the resistance phenotype mediated by transmembrane transporters and/or biofilm formation, mechanisms of resistance commonly found in C. albicans strains. A previous study by our group demonstrated that batzelladine D can inhibit the Pdr5p transporter in Saccharomyces cerevisiae. In the present study, our aim was to investigate the efficacy of batzelladine D in inhibiting the main efflux pumps of Candida albicans, CaCdr1p and CaCdr2p, as well as to evaluate the effect of the compound on C. albicans biofilm. Assays were conducted using a clinical isolate of Candida albicans expressing both transporters. Additionally, to allow the study of each transporter, S. cerevisiae mutant strains overexpressing CaCdr1p or CaCdr2p were used. Batzelladine D was able to reverse the fluconazole resistance phenotype by acting on both transporters. The compound synergistically improved the effect of fluconazole against the clinical isolate when tested in the Caenorhabditis elegans animal model. Moreover, the compound disrupted the preformed biofilm. Based on the obtained data, the continuation of batzelladine D studies as a potential new antifungal agent and/or chemosensitizer in Candida albicans infections can be suggested. Full article
(This article belongs to the Special Issue Marine Anti-Biofilm Compounds from Natural to Synthetic Compounds)
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16 pages, 3715 KiB  
Article
Screening for Potential Antiviral Compounds from Cyanobacterial Secondary Metabolites Using Machine Learning
by Tingrui Zhang, Geyao Sun, Xueyu Cheng, Cheng Cao, Zhonghua Cai and Jin Zhou
Mar. Drugs 2024, 22(11), 501; https://doi.org/10.3390/md22110501 - 5 Nov 2024
Viewed by 790
Abstract
The secondary metabolites of seawater and freshwater blue-green algae are a rich natural product pool containing diverse compounds with various functions, including antiviral compounds; however, high-efficiency methods to screen such compounds are lacking. Advanced virtual screening techniques can significantly reduce the time and [...] Read more.
The secondary metabolites of seawater and freshwater blue-green algae are a rich natural product pool containing diverse compounds with various functions, including antiviral compounds; however, high-efficiency methods to screen such compounds are lacking. Advanced virtual screening techniques can significantly reduce the time and cost of novel antiviral drug identification. In this study, we used a cyanobacterial secondary metabolite library as an example and trained three models to identify compounds with potential antiviral activity using a machine learning method based on message-passing neural networks. Using this method, 364 potential antiviral compounds were screened from >2000 cyanobacterial secondary metabolites, with amides predominating (area under the receiver operating characteristic curve value: 0.98). To verify the actual effectiveness of the candidate antiviral compounds, HIV virus reverse transcriptase (HIV-1 RT) was selected as a target to evaluate their antiviral potential. Molecular docking experiments demonstrated that candidate compounds, including kororamide, mollamide E, nostopeptolide A3, anachelin-H, and kasumigamide, produced relatively robust non-covalent bonding interactions with the RNase H active site on HIV-1 RT, supporting the effectiveness of the proposed screening model. Our data demonstrate that artificial intelligence-based screening methods are effective tools for mining potential antiviral compounds, which can facilitate the exploration of various natural product libraries. Full article
(This article belongs to the Special Issue Marine Drug Discovery through Molecular Docking)
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15 pages, 1988 KiB  
Article
A Pharmacokinetic and Bioavailability Study of Ecklonia cava Phlorotannins Following Intravenous and Oral Administration in Sprague–Dawley Rats
by Hyeon-Cheol Shin, Clint Rosenfeld, Robert J. Guttendorf, Susan B. Wade, Yong Ju Park, Ju Hee Kim, Seong Ho Kim, Bong Ho Lee and Hye Jeong Hwang
Mar. Drugs 2024, 22(11), 500; https://doi.org/10.3390/md22110500 - 4 Nov 2024
Viewed by 701
Abstract
This study examines the pharmacokinetics and bioavailability of phlorotannins from Ecklonia cava in rats following intravenous and oral administration. Known for their potent antioxidant, anti-inflammatory and many other bioactivities, these phlorotannins, particularly dieckol, 8,8′-bieckol, and phlorofucofuroeckol-A (PFF-A), were analyzed using high-performance liquid chromatography [...] Read more.
This study examines the pharmacokinetics and bioavailability of phlorotannins from Ecklonia cava in rats following intravenous and oral administration. Known for their potent antioxidant, anti-inflammatory and many other bioactivities, these phlorotannins, particularly dieckol, 8,8′-bieckol, and phlorofucofuroeckol-A (PFF-A), were analyzed using high-performance liquid chromatography coupled with tandem mass spectrometry. Intravenous administration at 10 mg/kg allowed detectability in plasma for up to 36 h for dieckol and 8,8′-bieckol, but only 2 h for PFF-A. Oral administration at doses of 100 mg/kg and 1000 mg/kg showed limited detectability, indicating low bioavailability and rapid clearance, particularly for PFF-A. The pharmacokinetic data suggest non-linear increases in the maximum plasma concentration (Cmax) and area under the curve (AUC) with increasing doses, pointing to significant challenges in achieving systemic availability of these eckols through oral administration. This study underscores the necessity for advanced formulation strategies and alternative routes of administration to enhance systemic bioavailability. At the same time, this result also suggests their effects may be through non-systemic pathways such as gut microbiome modulation or lipid-rich tissue targeting. The findings lay a crucial foundation for the further development of Ecklonia cava phlorotannins as therapeutic agents, offering insights into their pharmacokinetic behavior and informing enhancements in future clinical utility. Full article
(This article belongs to the Special Issue Therapeutic Potential of Phlorotannins)
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17 pages, 3873 KiB  
Article
Calcium Transport Activity of UV/H2O2-Degraded Fucoidans and Their Structural Characterization
by Biyang Zhu, Jiacheng Wang, Lijun You, Lianzhu Lin, Kuncheng Lin and Kseniya Hileuskaya
Mar. Drugs 2024, 22(11), 499; https://doi.org/10.3390/md22110499 - 4 Nov 2024
Viewed by 588
Abstract
Calcium-chelated polysaccharides have been increasingly considered as promising calcium supplements. In this study, degraded fucoidans (DFs) with different molecular weights (Mws) were prepared after UV/H2O2 treatment; their calcium-chelating capacities and intestinal absorption properties were also investigated. The results showed that [...] Read more.
Calcium-chelated polysaccharides have been increasingly considered as promising calcium supplements. In this study, degraded fucoidans (DFs) with different molecular weights (Mws) were prepared after UV/H2O2 treatment; their calcium-chelating capacities and intestinal absorption properties were also investigated. The results showed that the calcium-chelating capacities of DFs were improved with a decrease in Mw. This was mainly ascribed to the increased carboxyl content, which was caused by free-radical-mediated degradation. Meanwhile, the conformation of DF changed from a rod-like chain to a shorter and softer chain. The thermodynamic analysis demonstrated that DF binding to calcium was spontaneously driven by electrostatic interactions. Additionally, DF-Ca chelates with lower Mw showed favorable transport properties across a Caco-2 cell monolayer and could effectively accelerate the calcium influx through intestinal enterocytes. Furthermore, these chelates also exhibited a protective effect on the epithelial barrier by alleviating damage to tight junction proteins. These findings provide an effective free-radical-related approach for the development of polysaccharide-based calcium supplements with improved intestinal calcium transport ability. Full article
(This article belongs to the Special Issue Isolation, Identification and Applications of Marine Source Polysaccharides and Peptides—2nd Edition)
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13 pages, 1710 KiB  
Article
Extraction Optimization of Polysaccharides from Wet Red Microalga Porphyridium purpureum Using Response Surface Methodology
by Yi Chen, Qianmei Li, Bingqi Xu, Wenzhou Xiang, Aifen Li and Tao Li
Mar. Drugs 2024, 22(11), 498; https://doi.org/10.3390/md22110498 - 4 Nov 2024
Viewed by 1024
Abstract
Porphyridium is a unicellular marine microalga that is rich in polysaccharides and has excellent biological activities. Optimizing the extraction of polysaccharides can significantly improve the value of Porphyridium biomass. In the present study, response surface methodology was employed to optimize the extraction conditions [...] Read more.
Porphyridium is a unicellular marine microalga that is rich in polysaccharides and has excellent biological activities. Optimizing the extraction of polysaccharides can significantly improve the value of Porphyridium biomass. In the present study, response surface methodology was employed to optimize the extraction conditions of polysaccharides, including extraction time, extraction temperature, and biomass-to-water ratio. Furthermore, microwave-assisted extraction was used to improve the yield of polysaccharides further. The results showed that increasing the extraction temperature and extraction time could enhance the yield of polysaccharides. The multiple regression analysis of RSM indicated that the model could be employed to optimize the extraction of polysaccharides. The optimal extraction time, extraction temperature, and biomass-to-water ratio were 45 min, 87 °C, and 1:63 g mL−1, respectively. Under these optimal conditions, the maximum yield of polysaccharides was 23.66% DW, which well matched the predicted yield. The results indicated that the extraction temperature was the most significant condition affecting the yield of polysaccharides. The microwave-assisted extraction could further improve the yield of polysaccharides to 25.48% DW. In conclusion, hot water with microwave-assisted extraction was effective for polysaccharide extraction in P. purpureum. Full article
(This article belongs to the Special Issue Marine Algae: Exploring Their Nutritional, Health, and Nutraceutical Potential)
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16 pages, 4295 KiB  
Review
Molecular Evolution and Adaptation Strategies in Marine Ciliates: An Inspiration for Cold-Adapted Enzyme Engineering and Drug Binding Analysis
by Sandra Pucciarelli, Matteo Mozzicafreddo, Alberto Vassallo, Angela Piersanti and Cristina Miceli
Mar. Drugs 2024, 22(11), 497; https://doi.org/10.3390/md22110497 - 4 Nov 2024
Viewed by 851
Abstract
In the present review, we summarize genome mining of genomic data obtained from the psychrophilic Antarctic marine ciliate Euplotes focardii and its evolutionary-close mesophilic cosmopolitan counterpart E. crassus. This analysis highlights adaptation strategies that are unique to the Antarctic ciliate, including antioxidant [...] Read more.
In the present review, we summarize genome mining of genomic data obtained from the psychrophilic Antarctic marine ciliate Euplotes focardii and its evolutionary-close mesophilic cosmopolitan counterpart E. crassus. This analysis highlights adaptation strategies that are unique to the Antarctic ciliate, including antioxidant gene duplication and distinctive substitutions that may play roles in increased drug binding affinity and enzyme reaction rate in cold environments. Enzymes from psychrophiles are usually characterized by high activities and reaction rates at low temperatures compared with their counterparts from mesophiles and thermophiles. As a rule, catalyst cold activity derives from an increased structural flexibility that may lead to protein denaturation in response to temperature fluctuation. Molecular thermolability has been a major drawback of using macromolecules from psychrophiles in industrial applications. Here, we report a case study in which the role of peculiar amino acid substitution in cold adaptation is demonstrated by site-directed mutagenesis. Combined with a rational design approach, these substitutions can be used for site-directed mutagenesis to obtain cold-active catalysts that are structurally stable. Furthermore, molecular docking analysis of β-tubulin isotypes extrapolated from E. focardii and E. crassus genomes allowed us to obtain additional insight on the taxol binding site and drug affinity. E. focardii genome mining and the comparison with the mesophilic sibling counterpart can be used as an inspiration for molecular engineering for medical and industrial applications. Full article
(This article belongs to the Special Issue Bioactive Molecules from Extreme Environments III)
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19 pages, 4039 KiB  
Review
Marine-Derived Bioactive Ingredients in Functional Foods for Aging: Nutritional and Therapeutic Perspectives
by Youngji Han, Dong Hyun Kim and Seung Pil Pack
Mar. Drugs 2024, 22(11), 496; https://doi.org/10.3390/md22110496 - 4 Nov 2024
Viewed by 1723
Abstract
Aging is closely linked to various health challenges, including cardiovascular disease, metabolic disorders, and neurodegenerative conditions. This study emphasizes the critical role of bioactive compounds derived from marine sources, such as antioxidants, omega-3 fatty acids, vitamins, minerals, and polysaccharides, in addressing oxidative stress, [...] Read more.
Aging is closely linked to various health challenges, including cardiovascular disease, metabolic disorders, and neurodegenerative conditions. This study emphasizes the critical role of bioactive compounds derived from marine sources, such as antioxidants, omega-3 fatty acids, vitamins, minerals, and polysaccharides, in addressing oxidative stress, inflammation, and metabolic disorders closely related to aging. Incorporating these materials into functional foods not only provides essential nutrients but also delivers therapeutic effects, thereby promoting healthy aging and mitigating age-related diseases. The growth of the global anti-aging market, particularly in North America, Europe, and Asia, underscores the significance of this study. This review systematically analyzes the current research, identifying key bioactive compounds, their mechanisms of action, and their potential health benefits, thus highlighting the broad applicability of marine-derived bioactive compounds to enhancing healthy aging and improving the quality of life of aging populations. Full article
(This article belongs to the Special Issue Marine Nutraceuticals and Functional Foods: 2nd Edition)
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13 pages, 4082 KiB  
Article
Odd-Numbered Agaro-Oligosaccharides Produced by α-Neoagaro-Oligosaccharide Hydrolase Exert Antioxidant Activity in Human Dermal Fibroblasts
by Eunyoung Jo, Navindu Dinara Gajanayaka, Minthari Sakethanika Bandara, Svini Dileepa Marasinghe, Gun-Hoo Park, Su-Jin Lee, Chulhong Oh and Youngdeuk Lee
Mar. Drugs 2024, 22(11), 495; https://doi.org/10.3390/md22110495 - 3 Nov 2024
Viewed by 693
Abstract
Agarases produce agar oligosaccharides with various structures exhibiting diverse physiological activities. α-Neoagaro-oligosaccharide hydrolase (α-NAOSH) specifically cleaves even-numbered neoagaro-oligosaccharides, producing 3,6-anhydro-l-galactose (l-AHG) and odd-numbered agaro-oligosaccharides (OAOSs). In this study, α-NAOSH from the agar-degrading marine bacterium Gilvimarinus agarilyticus JEA5 (Gaa117) was [...] Read more.
Agarases produce agar oligosaccharides with various structures exhibiting diverse physiological activities. α-Neoagaro-oligosaccharide hydrolase (α-NAOSH) specifically cleaves even-numbered neoagaro-oligosaccharides, producing 3,6-anhydro-l-galactose (l-AHG) and odd-numbered agaro-oligosaccharides (OAOSs). In this study, α-NAOSH from the agar-degrading marine bacterium Gilvimarinus agarilyticus JEA5 (Gaa117) was purified and characterized using an E. coli expression system to produce OAOSs and determine their bioactivity. Recombinant Gaa117 (rGaa117) showed maximum activity at pH 6.0 and 35 °C. rGaa117 retained >80% of its initial activity after 120 min at 30 °C. The activity was enhanced in the presence of Mn2+. Km, Vmax, and Kcat/Km values of the enzyme were 22.64 mM, 246.3 U/mg, and 15 s−1/mM, respectively. rGaa117 hydrolyzed neoagarobiose, neoagarotetraose, and neoagarohexaose, producing OAOSs that commonly contained l-AHG. Neoagarobiose and neoagarotetraose mixtures, designated NAO24, and mixtures of l-AHG and agarotriose, designated AO13, were obtained using recombinant rGaa16B (β-agarase) and rGaa117, respectively, and their antioxidant activities were compared. AO13 showed higher hydrogen peroxide-scavenging activity than NAO24 in human dermal fibroblasts in vitro because of structural differences: AOSs have d-galactose at the non-reducing end, whereas NAOSs have l-AHG. In conclusion, OAOSs exhibited high ROS-scavenging activity in H2O2-induced human dermal fibroblasts. They may be applicable in cosmetics and pharmaceuticals for prevention of skin aging. Full article
(This article belongs to the Special Issue Advances of Marine-Derived Enzymes)
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13 pages, 4888 KiB  
Article
Design, Synthesis, and Evaluation of Novel Thiazole-Containing Algicides Inspired by Bacillamide A
by Xiaoxue Li, Huili Li, Lei Shi, Zuguang Yin, Yuguo Du, Hongxia Zhang, Xin Wang, Xinxin Wang, Kexin Xu, Weili Wang, Ronglian Xing and Yi Liu
Mar. Drugs 2024, 22(11), 494; https://doi.org/10.3390/md22110494 - 1 Nov 2024
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Abstract
The pursuit of highly effective, low-toxicity, and eco-friendly algicides for controlling and eradicating harmful algal blooms (HABs) is of paramount importance. The natural allelochemical bacillamide A has displayed impressive algicidal activity against harmful algae with favorable safety profiles. However, the poor synthetic efficiency [...] Read more.
The pursuit of highly effective, low-toxicity, and eco-friendly algicides for controlling and eradicating harmful algal blooms (HABs) is of paramount importance. The natural allelochemical bacillamide A has displayed impressive algicidal activity against harmful algae with favorable safety profiles. However, the poor synthetic efficiency and large dose requirements of bacillamide A limit its further application. In this paper, 17 thiazole-containing bacillamide derivatives (BDs) were designed and synthesized in three linear steps as potential algicides. Eight compounds (6a, 6c, 6j, 7b, 7c, 7d, 7e, and 7g) displayed potent inhibitory effects against Prorocentrum minimum, Skeletonema costatum, and Alexandrium pacificum, and they had similar or better activity than the positive control (CuSO4) and bacillamide A. Compound 6a exhibited the most potent algicidal activity against S. costatum (half-maximal effective concentration [EC50] = 0.11 μg/mL), being 23-fold more potent than bacillamide A, 28-fold more potent than CuSO4, and 39-fold more potent than Diuron. Compound 6j exhibited significant algicidal activity against the toxic dinoflagellates P. minimum (EC50 = 1.0 μg/mL) and A. pacificum (EC50 = 0.47 μg/mL), being 3–5-fold more potent than natural bacillamide A, Diuron, and CuSO4. Micrographs and SEM images revealed that 6j induced cell wall rupture and cellular content leakage. Biochemical and physiological studies indicated that 6j might partially disrupt the antioxidant and photosynthetic systems in algal cells, resulting in morphological changes, cell wall rupture, and inclusion leakage. Our work suggests that 6j has a distinct mode of action from CuSO4 and provides a promising candidate for the development of new algicides, worthy of further investigation. Full article
(This article belongs to the Special Issue Synthetic Studies of Marine Bioactive Natural Products and Analogs to Develop Novel Drug Leads)
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