Marine Drugs

13 pages, 8761 KiB

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessReview

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessCommunication

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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

Open AccessArticle

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

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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