Marine Drugs

28 pages, 6511 KiB

Open AccessArticle

Identification and Characterization of Two Aryl Sulfotransferases from Deep-Sea Marine Fungi and Their Implications in the Sulfation of Secondary Metabolites

by Nicolas Graziano, Beatriz Arce-López, Tristan Barbeyron, Ludovic Delage, Elise Gerometta, Catherine Roullier, Gaëtan Burgaud, Elisabeth Poirier, Laure Martinelli, Jean-Luc Jany, Nolwenn Hymery and Laurence Meslet-Cladiere

Mar. Drugs 2024, 22(12), 572; https://doi.org/10.3390/md22120572 (registering DOI) - 20 Dec 2024

Abstract

Sulfation plays a critical role in the biosynthesis of small molecules, regulatory mechanisms such as hormone signaling, and detoxification processes (phase II enzymes). The sulfation reaction is catalyzed by a broad family of enzymes known as sulfotransferases (SULTs), which have been extensively studied [...] Read more.

Sulfation plays a critical role in the biosynthesis of small molecules, regulatory mechanisms such as hormone signaling, and detoxification processes (phase II enzymes). The sulfation reaction is catalyzed by a broad family of enzymes known as sulfotransferases (SULTs), which have been extensively studied in animals due to their medical importance, but also in plant key processes. Despite the identification of some sulfated metabolites in fungi, the mechanisms underlying fungal sulfation remain largely unknown. To address this knowledge gap, we conducted a comprehensive search of available genomes, resulting in the identification of 174 putative SULT genes in the Ascomycota phylum. Phylogenetic analysis and structural modeling revealed that these SULTs belong to the aryl sulfotransferase family, and they are divided into two potential distinct clusters of PAPS-dependent SULTs within the fungal kingdom. SULT genes from two marine fungi isolated from deep-sea hydrothermal vents, Hortaea werneckii UBOCC-A-208029 (HwSULT) and Aspergillus sydowii UBOCC-A-108050 SULT (AsSULT), were selected as representatives of each cluster. Recombinant proteins were expressed in Escherichia coli and biochemically characterized. HwSULT demonstrated high and versatile activity, while AsSULT appeared more substrate-specific. Here, HwSULT was used to sulfate the mycotoxin zearalenone, enhancing its cytotoxicity toward healthy feline intestinal cells. Full article

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

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22 pages, 3596 KiB

Open AccessArticle

Chondroitin Sulfate Nanovectorized by LC-PUFAs Nanocarriers Extracted from Salmon (Salmo salar) by Green Process with Decreased Inflammatory Marker Expression in Interleukin-1β-Stimulated Primary Human Chondrocytes In Vitro Culture

by Louis Pruvost, Maureen Gerlei, Cédric Paris, Émilie Velot, Cyril J.-F. Kahn, Arnaud Bianchi and Michel Linder

Mar. Drugs 2024, 22(12), 571; https://doi.org/10.3390/md22120571 - 20 Dec 2024

Abstract

Chondroitin sulfate (CS), a glycosaminoglycan, supports health through various physiological functions, including tissue protection, bone growth, and skin aging prevention. It also contributes to anticoagulant or anti-inflammatory processes, with its primary clinical use being osteoarthritis treatment. This study presents the results of the [...] Read more.

Chondroitin sulfate (CS), a glycosaminoglycan, supports health through various physiological functions, including tissue protection, bone growth, and skin aging prevention. It also contributes to anticoagulant or anti-inflammatory processes, with its primary clinical use being osteoarthritis treatment. This study presents the results of the valorization of lipids and CS, both extracted from salmon co-products through enzymatic processes. The polar lipids, naturally rich in long-chain fatty acids (docosahexaenoic acid DHA C22:6 n-3 and eicosapentaenoic acid EPA C20:5 n-3), and the CS, primarily located in the nasal cartilage, were separated and concentrated before being characterized using various techniques to determine functional and lipid composition. These compounds were then used to formulate liposomes of 63 to 95 nm in size composed of 19.38% of DHA and 7.44% of EPA and encapsulating CS extract with a Δdi-4S/Δdi-6S ratio of 0.53 at 2 weight masses (10–30 kDa and >30 kDa) or CS standard all at two different concentrations. Liposomes were tested on human chondrocytes in inflamed conditions. Thus, compatibility tests, the expression of various inflammation markers at transcriptional and molecular levels, nitrites, and the amount of collagenase produced were analyzed. The results showed that CS, in synergy with the liposomes, played a positive role in combating chondrocyte inflammation even at a low concentration. Full article

(This article belongs to the Special Issue Marine Anti-Inflammatory and Antioxidant Agents, 4th Edition)

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15 pages, 5680 KiB

Open AccessArticle

Enhanced Eicosapentaenoic Acid Production via Synthetic Biological Strategy in Nannochloropsis oceanica

by Congcong Miao, Mingting Du, Hongchao Du, Tao Xu, Shan Wu, Xingwei Huang, Xitao Chen, Suxiang Lei and Yi Xin

Mar. Drugs 2024, 22(12), 570; https://doi.org/10.3390/md22120570 - 19 Dec 2024

Abstract

The rational dietary ratio of docosahexaenoic acid (DHA) to eicosapentaenoic acid (EPA) can exert neurotrophic and cardiotrophic effects on the human body. The marine microalga Nannochloropsis oceanica produces EPA yet no DHA, and thus, it is considered an ideal EPA-only model to pursue [...] Read more.

The rational dietary ratio of docosahexaenoic acid (DHA) to eicosapentaenoic acid (EPA) can exert neurotrophic and cardiotrophic effects on the human body. The marine microalga Nannochloropsis oceanica produces EPA yet no DHA, and thus, it is considered an ideal EPA-only model to pursue a rational DHA/EPA ratio. In this study, synthetic biological strategy was applied to improve EPA production in N. oceanica. Firstly, to identify promoters and terminators, fifteen genes from N. oceanica were isolated using a transcriptomic approach. Compared to α-tubulin, NO08G03500, NO03G03480 and NO22G01450 exhibited 1.2~1.3-fold increases in transcription levels. Secondly, to identify EPA-synthesizing modules, putative desaturases (NoFADs) and elongases (NoFAEs) were overexpressed by the NO08G03500 and NO03G03480 promoters/terminators in N. oceanica. Compared to the wild type (WT), NoFAD1770 and NoFAE0510 overexpression resulted in 47.7% and 40.6% increases in EPA yields, respectively. Thirdly, to store EPA in triacylglycerol (TAG), NoDGAT2K was overexpressed using the NO22G01450 promoter/terminator, along with NoFAD1770–NoFAE0510 stacking, forming transgenic line XS521. Compared to WT, TAG-EPA content increased by 154.8% in XS521. Finally, to inhibit TAG-EPA degradation, a TAG lipase-encoding gene NoTGL1990 was knocked out in XS521, leading to a 49.2–65.3% increase in TAG-EPA content. Our work expands upon EPA-enhancing approaches through synthetic biology in microalgae and potentially crops. Full article

(This article belongs to the Special Issue Synthetic Biology in Marine Microalgae)

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23 pages, 10192 KiB

Open AccessArticle

Genome Analysis of a Polysaccharide-Degrading Bacterium Microbulbifer sp. HZ11 and Degradation of Alginate

by Xiao Liu, Wentao Zhao, Yan Li, Zhongliang Sun, Chang Lu and Liqin Sun

Mar. Drugs 2024, 22(12), 569; https://doi.org/10.3390/md22120569 - 18 Dec 2024

Abstract

Marine bacteria are crucial sources of alginate lyases, which play an essential role in alginate oligosaccharide (AOS) production. This study reports the biochemical characteristics of a new species of the Microbulbifer genus, Microbulbifer sp. HZ11. The strain HZ11 is Gram-negative, aerobic, flagellate-free, and [...] Read more.

Marine bacteria are crucial sources of alginate lyases, which play an essential role in alginate oligosaccharide (AOS) production. This study reports the biochemical characteristics of a new species of the Microbulbifer genus, Microbulbifer sp. HZ11. The strain HZ11 is Gram-negative, aerobic, flagellate-free, and rod-shaped. The genome of strain HZ11 is a 4,248,867 bp circular chromosome with an average GC content of 56.68%. HZ11 can degrade alginate and other polysaccharides. The carbohydrate-active enzyme (CAZyme) genes account for 4.57% of the total protein-coding genes of HZ11. Its alginate metabolism process is consistent with the characteristics of the polysaccharide utilization locus (PUL) system. The alginate lyase produced by strain HZ11 showed the highest activity at 50 °C, pH 8.5, and 0.1 M NaCl. The substrate preference was as follows: sodium alginate > poly mannuronic acid > poly guluronic acid. The thin layer chromatography (TLC) results revealed that the main enzymatic degradation products were monosaccharides or AOSs with a degree of polymerization (DP) of 2–3. These results help clarify the metabolism and utilization mechanism of alginate by marine bacteria and provide a theoretical reference for its application in the degradation of alginate and other polysaccharides. Full article

(This article belongs to the Special Issue Marine Functional Carbohydrates: Enzymatic Manufacturing and Activity Evaluation)

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15 pages, 1810 KiB

Open AccessArticle

Antioxidant Activity and DPP-IV Inhibitory Effect of Fish Protein Hydrolysates Obtained from High-Pressure Pretreated Mixture of Rainbow Trout (Oncorhynchus mykiss) and Atlantic Salmon (Salmo salar) Rest Raw Material

by Elissavet Kotsoni, Egidijus Daukšas, Grete Hansen Aas, Turid Rustad, Brijesh K. Tiwari, Carmen Lammi, Carlotta Bollati, Melissa Fanzaga, Lorenza d’Adduzio, Janne Kristin Stangeland and Janna Cropotova

Mar. Drugs 2024, 22(12), 568; https://doi.org/10.3390/md22120568 - 18 Dec 2024

Abstract

The use of fish rest raw material for the production of fish protein hydrolysates (FPH) through enzymatic hydrolysis has received significant interest in recent decades. Peptides derived from fish proteins are known for their enhanced bioactivity which is mainly influenced by their molecular [...] Read more.

The use of fish rest raw material for the production of fish protein hydrolysates (FPH) through enzymatic hydrolysis has received significant interest in recent decades. Peptides derived from fish proteins are known for their enhanced bioactivity which is mainly influenced by their molecular weight. Studies have shown that novel technologies, such as high-pressure processing (HPP), can effectively modify protein structures leading to increased biological activity. This study investigated the effect of various HPP conditions on the molecular weight distribution, antioxidant activity, and dipeptidyl-peptidase IV (DPP-IV) inhibitory effect of FPH derived from a mixture of rainbow trout (Oncorhynchus mykiss) and Atlantic salmon (Salmo salar) rest raw material. Six different treatments were applied to the samples before enzymatic hydrolysis; 200 MPa × 4 min, 200 MPa × 8 min, 400 MPa × 4 min, 400 MPa × 8 min, 600 MPa × 4 min, and 600 MPa × 8 min. The antioxidant and DPP-IV inhibitory effects of the extracted FPH were measured both in vitro and at cellular level utilizing human intestinal Caco-2 cells. The results indicated that low and moderate pressures (200 and 400 MPa) increased the proportion of larger peptides (2–5 kDa) in the obtained FPH, while treatment at 600 MPa × 4 min resulted in a higher proportion of smaller peptides (1–2 kDa). Furthermore, HPP led to the formation of peptides that demonstrated increased antioxidant activity in Caco-2 cells compared to the control, whereas their potential antidiabetic activity remained unaffected. Full article

(This article belongs to the Special Issue Marine-Derived Ingredients for Functional Foods)

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15 pages, 2194 KiB

Open AccessArticle

Comparative Analysis of the Biochemical and Molecular Responses of Nannochloropsis gaditana to Nitrogen and Phosphorus Limitation: Phosphorus Limitation Enhances Carotenogenesis

by Sun Young Kim, Hanbi Moon, Yong Min Kwon, Kyung Woo Kim and Jaoon Young Hwan Kim

Mar. Drugs 2024, 22(12), 567; https://doi.org/10.3390/md22120567 - 18 Dec 2024

Abstract

Nannochloropsis gaditana is well known for its potential for biofuel production due to its high lipid content. Numerous omics and biochemical studies have explored the overall molecular mechanisms underlying the responses of Nannochloropsis sp. to nutrient availability, primarily focusing on lipid metabolism. However, [...] Read more.

Nannochloropsis gaditana is well known for its potential for biofuel production due to its high lipid content. Numerous omics and biochemical studies have explored the overall molecular mechanisms underlying the responses of Nannochloropsis sp. to nutrient availability, primarily focusing on lipid metabolism. However, N. gaditana is able to synthesize other valuable products such as carotenoids, including violaxanthin, which has various biological functions and applications. In this study, we comparatively investigated the physiological, biochemical, and molecular responses of N. gaditana to nitrogen and phosphorus limitation, examining biomass production, photosynthetic activity, lipid, chlorophyll, and carotenoids content, and RNA-seq data. Nitrogen limitation decreased photosynthetic activity, chlorophyll content, and biomass production but increased lipid content. Phosphorus limitation substantially increased carotenoids content, with violaxanthin productivity of 10.24 mg/L, 3.38-fold greater than under the control condition, with little effect on biomass production or photosynthetic function. These results were generally consistent with the gene expression pattern observed in transcriptomic analysis. This integrated analysis shows that phosphorus limitation can be an economically competitive solution by enhancing valuable carotenoids while maintaining lipid and biomass production in N. gaditana. Full article

(This article belongs to the Special Issue High-Value Algae Products)

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29 pages, 385 KiB

Open AccessReview

The Beneficial Roles of Seaweed in Atopic Dermatitis

by Ah-Reum Kim, Myeong-Jin Kim, Jaeseong Seo, Kyoung Mi Moon and Bonggi Lee

Mar. Drugs 2024, 22(12), 566; https://doi.org/10.3390/md22120566 - 17 Dec 2024

Abstract

Atopic dermatitis (AD) is a chronic, inflammatory skin condition characterized by severe pruritus and recurrent flare-ups, significantly impacting patients’ quality of life. Current treatments, such as corticosteroids and immunomodulators, often provide symptomatic relief but can lead to adverse effects with prolonged use. Seaweed, [...] Read more.

Atopic dermatitis (AD) is a chronic, inflammatory skin condition characterized by severe pruritus and recurrent flare-ups, significantly impacting patients’ quality of life. Current treatments, such as corticosteroids and immunomodulators, often provide symptomatic relief but can lead to adverse effects with prolonged use. Seaweed, a sustainable and nutrient-dense resource, has emerged as a promising alternative due to its rich bioactive compounds—polysaccharides, phlorotannins, polyphenols, and chlorophyll—that offer anti-inflammatory, antioxidant, and immunomodulatory properties. This review explores the therapeutic potential of brown, red, and green algae in alleviating AD symptoms, highlighting the effects of specific species, including Undaria pinnatifida, Laminaria japonica, Chlorella vulgaris, and Sargassum horneri. These seaweeds modulate immune responses, reduce epidermal thickness, and restore skin barrier function, presenting a novel, safe, and effective approach to AD management. Further clinical studies are needed to confirm their efficacy and establish dosing strategies, paving the way for seaweed-derived therapies as natural alternatives in AD treatment. Full article

(This article belongs to the Special Issue Immunomodulatory Activities of Marine Products)

18 pages, 4279 KiB

Open AccessArticle

Chemical Composition, Free Radicals and Pathogenic Microbes in the Extract Derived from Dictyota dichotoma: In Silico and In Vitro Approaches

by Fouad Oumassi, Khalid Chebbac, Naouar Ben Ali, Soundouss Kaabi, Zineb Nejjar El Ansari, Amira Metouekel, Azeddin El Barnossi, Abdelfattah El Moussaoui, Mohamed Chebaibi, Loubna Bounab, Ibrahim Mssillou, Abdelaaty Abdelaziz Shahat, Brahim El Bouzdoudi and Mohammed L’bachir El Kbiach

Mar. Drugs 2024, 22(12), 565; https://doi.org/10.3390/md22120565 - 17 Dec 2024

Abstract

Marine algae are renowned for their health benefits due to the presence of functional bioactive compounds. In this context, this study aims to valorize the extract of a seaweed, Dictyota dichotoma (D. dichotoma), through phytochemical characterization using liquid chromatography–mass spectrometry (HPLC-MS), [...] Read more.

Marine algae are renowned for their health benefits due to the presence of functional bioactive compounds. In this context, this study aims to valorize the extract of a seaweed, Dictyota dichotoma (D. dichotoma), through phytochemical characterization using liquid chromatography–mass spectrometry (HPLC-MS), as well as in vitro and in silico evaluation of its biological activities (antioxidant and antimicrobial). Phytochemical characterization revealed that the ethanolic extract of Dictyota dichotoma (DdEx) is rich in phenolic compounds, with a total of 22 phycocompounds identified. Antioxidant activity, measured by various methods, showed an IC₅₀ of 120 µg/mL for the DPPH assay, an EC₅₀ of 120.53 µg/mL for the FRAP assay, and a total antioxidant power of 685.26 µg AAE/mg according to the phosphomolybdate (TAC) method. Evaluation of antibacterial activity showed a zone of inhibition diameter ranging from 11.93 to 22.58 mm, with the largest zone observed for the Escherichia coli (E. coli) strain. For antifungal activity, inhibition zone diameters ranged from 22.38 to 23.52 mm, with the largest recorded for the Saccharomyces cerevisiae (S. cerevisiae) strain. The in silico study identified tetragalloyl-glucose, apigenin-7-O-glucoside, and pentagalloyl-glucose as the most active compounds against NADPH oxidase, with docking scores of −7.723, −7.424, and −6.402 kcal/mol, respectively. Regarding antibacterial activity, apigenin-7-O-glucoside, pelargonidin-3-O-glucoside, and secoisolariciresinol demonstrated high affinity for E. coli beta-ketoacyl-[acyl carrier protein] synthase, with docking scores of −7.276, −6.811, and −6.594 kcal/mol, respectively. These in vitro and in silico evaluations showed that D. dichotoma extract possesses antioxidant and antimicrobial properties, due to its richness in bioactive compounds identified by HPLC. Full article

(This article belongs to the Special Issue Therapeutic Potential of Marine Algae)

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20 pages, 8399 KiB

Open AccessArticle

Butyrolactone-I from Marine Fungal Metabolites Mitigates Heat-Stress-Induced Apoptosis in IPEC-J2 Cells and Mice Through the ROS/PERK/CHOP Signaling Pathway

by Xueting Niu, Shengwei Chen, Xinchen Wang, Jiaying Wen, Xiaoxi Liu, Yanhong Yong, Zhichao Yu, Xingbing Ma, A. M. Abd El-Aty and Xianghong Ju

Mar. Drugs 2024, 22(12), 564; https://doi.org/10.3390/md22120564 - 17 Dec 2024

Abstract

Heat stress poses a significant challenge to animal husbandry, contributing to oxidative stress, intestinal mucosal injury, and apoptosis, which severely impact animal health, growth, and production efficiency. The development of safe, sustainable, and naturally derived solutions to mitigate these effects is critical for [...] Read more.

Heat stress poses a significant challenge to animal husbandry, contributing to oxidative stress, intestinal mucosal injury, and apoptosis, which severely impact animal health, growth, and production efficiency. The development of safe, sustainable, and naturally derived solutions to mitigate these effects is critical for advancing sustainable agricultural practices. Butyrolactone-I (BTL-I), a bioactive compound derived from deep-sea fungi (Aspergillus), shows promise as a functional feed additive to combat heat stress in animals. This study explored the protective effects of BTL-I against heat-stress-induced oxidative stress and apoptosis in IPEC-J2 cells and mice. Our findings demonstrated that BTL-I effectively inhibited the heat-stress-induced upregulation of HSP70 and HSP90, alleviating intestinal heat stress. Both in vitro and in vivo experiments revealed that heat stress increased intestinal cell apoptosis, with a significant upregulation of Bax/Bcl-2 expression, while BTL-I pretreatment significantly reduced apoptosis-related protein levels, showcasing its protective effects. Furthermore, BTL-I suppressed oxidative stress markers (ROS and MDA) while enhancing antioxidant activity (SOD levels). BTL-I also reduced the expression of p-PERK, p-eIF2α, ATF4, and CHOP, mitigating oxidative and endoplasmic reticulum stress in intestinal cells. In conclusion, BTL-I demonstrates the potential to improve animal resilience to heat stress, supporting sustainable livestock production systems. Its application as a natural, eco-friendly feed additive will contribute to the development of sustainable agricultural practices. Full article

(This article belongs to the Special Issue Marine Anti-Inflammatory and Antioxidant Agents, 4th Edition)

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2 pages, 1809 KiB

Open AccessCorrection

Correction: Zhang et al. Astaxanthin Alleviates Early Brain Injury Following Subarachnoid Hemorrhage in Rats: Possible Involvement of Akt/Bad Signaling. Mar. Drugs 2014, 8, 4291

by Xiang-Sheng Zhang, Xin Zhang, Qi Wu, Wei Li, Qing-Rong Zhang, Chun-Xi Wang, Xiao-Ming Zhou, Hua Li, Ji-Xin Shi and Meng-Liang Zhou

Mar. Drugs 2024, 22(12), 563; https://doi.org/10.3390/md22120563 - 17 Dec 2024

Abstract

Errors in Figures [...] Full article

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13 pages, 1865 KiB

Open AccessArticle

Optimization of Collagen Extraction from Fish Scales Using Tris-Glycine Buffer: A Taguchi Methodological Approach

by Mokgadi Ursula Makgobole, Stanley Chibuzor Onwubu, Abayomi Baruwa, Nomakhosi Mpofana, Zodidi Obiechefu, Deneshree Naidoo, Andile Khathi and Blessing Mkhwanazi

Mar. Drugs 2024, 22(12), 562; https://doi.org/10.3390/md22120562 - 17 Dec 2024

Abstract

Collagen, a critical biomaterial with wide applications in pharmaceuticals, cosmetics, and medical industries, can be sourced sustainably from fish scales. This study optimizes the extraction of collagen using Tris-Glycine buffer from fish scales via the Taguchi method. Various extraction parameters—buffer concentration, temperature, pH, [...] Read more.

Collagen, a critical biomaterial with wide applications in pharmaceuticals, cosmetics, and medical industries, can be sourced sustainably from fish scales. This study optimizes the extraction of collagen using Tris-Glycine buffer from fish scales via the Taguchi method. Various extraction parameters—buffer concentration, temperature, pH, and time—were evaluated to identify optimal conditions. Under optimal conditions (0.5 M of acetic acids, volume of acids of 100 mL, soaking time of 120 min, and Tris-Glycine buffer of 10 mL), the results demonstrate that temperature and buffer concentration significantly influence collagen yield, with a collagen purity of 17.14 ± 0.05 mg/g. R² value of 73.84% was obtained for the mathematical model). FTIR analysis confirmed the presence of characteristic collagen peaks at 1611 cm⁻¹ (amide I), 1523 cm⁻¹ (amide II), and 1300 cm⁻¹ (amide III), indicating the successful extraction of type I collagen. SDS-PAGE analysis revealed a protein banding pattern consistent with the molecular weight of collagen, and amino acid analysis shows high percentages of glycine (20.98%), proline (15.43%), and hydroxyproline (11.51%), implying fibrous collagen structures. The finding suggests that the Taguchi method offers an efficient and sustainable approach for collagen extraction, reducing waste from fish processing industries. Nevertheless, there is a need for further experimental validation to align with mathematical modeling on the optimized conditions. Full article

(This article belongs to the Special Issue Fishery Discards, Processing Waste and Marine By-Products)

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19 pages, 6914 KiB

Open AccessArticle

Interaction of Liposomes Containing the Carrageenan/Echinochrome Complex with Human HaCaT Keratinocytes In Vitro

by Ekaterina S. Menchinskaya, Vladimir I. Gorbach, Evgeny A. Pislyagin, Tatiana Y. Gorpenchenko, Evgeniya A. Pimenova, Irina V. Guzhova, Dmitry L. Aminin and Irina M. Yermak

Mar. Drugs 2024, 22(12), 561; https://doi.org/10.3390/md22120561 - 16 Dec 2024

Abstract

Liposomal drug delivery systems are successfully used in various fields of medicine for external and systemic applications. Marine organisms contain biologically active substances that have a unique structure and exhibit a wide range of biological activities. Polysaccharide of red seaweed (carrageenan (CRG)), and [...] Read more.

Liposomal drug delivery systems are successfully used in various fields of medicine for external and systemic applications. Marine organisms contain biologically active substances that have a unique structure and exhibit a wide range of biological activities. Polysaccharide of red seaweed (carrageenan (CRG)), and water-insoluble sea urchin pigment (echinochrome (Ech)) interact with each other and form a stable complex. We included the CRG/Ech complex in liposomes for better permeability into cells. In our research, tetramethylrhodamine isothiocyanate TRITC-labeled CRG was synthesized to study the interaction of the complex encapsulated in liposomes with human epidermal keratinocytes (HaCaTs) widely used to expose the skin to a variety of substances. Using confocal microscopy, we found that liposomes were able to penetrate HaCaT cells with maximum efficiency within 24 h, and pre-incubation of keratinocytes with liposomes resulted in the delivery of the CRG/Ech complex into the cytoplasm. We investigated the anti-inflammatory effects of liposomes, including the lysosomal regulation, increased intracellular ROS levels, and increased NO synthesis in lipopolysaccharide (LPS)- or Escherichia coli (E. coli)-induced inflamed skin cells. Liposomes containing the CRG/Ech complex significantly reduced lysosomal activity by 26% in LPS-treated keratinocytes and decreased ROS levels in cells by 23% after LPS exposure. It was found that liposomes with the complex improved the migration of HaCaT keratinocytes incubated with high-dose LPS by 47%. The results of the work, taking into account the good permeability of liposomes into keratinocytes, as well as the anti-inflammatory effect on cells treated with LPS or E. coli, show the prospects of using liposomes containing the CRG/Ech complex as an anti-inflammatory agent in the fight against skin infections. Full article

(This article belongs to the Special Issue Marine Polysaccharide-Based Biomaterials)

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28 pages, 2112 KiB

Open AccessArticle

Composition of Triterpene Glycosides of the Far Eastern Sea Cucumber Cucumaria conicospermium Levin et Stepanov; Structure Elucidation of Five Minor Conicospermiumosides A₃-1, A₃-2, A₃-3, A₇-1, and A₇-2; Cytotoxicity of the Glycosides Against Human Breast Cancer Cell Lines; Structure–Activity Relationships

by Alexandra S. Silchenko, Ekaterina A. Chingizova, Ekaterina S. Menchinskaya, Elena A. Zelepuga, Anatoly I. Kalinovsky, Sergey A. Avilov, Kseniya M. Tabakmakher, Roman S. Popov, Pavel. S. Dmitrenok, Salim Sh. Dautov and Vladimir I. Kalinin

Mar. Drugs 2024, 22(12), 560; https://doi.org/10.3390/md22120560 - 16 Dec 2024

Abstract

Five new non-holostane di- and trisulfated triterpene pentaosides, conicospermiumosides A₃-1 (1), A₃-2 (2), A₃-3 (3), A₇-1 (4), and A₇-2 (5) were isolated from [...] Read more.

Five new non-holostane di- and trisulfated triterpene pentaosides, conicospermiumosides A₃-1 (1), A₃-2 (2), A₃-3 (3), A₇-1 (4), and A₇-2 (5) were isolated from the Far Eastern sea cucumber Cucumaria conicospermium Levin et Stepanov (Cucumariidae, Dendrochirotida). Twelve known glycosides found earlier in other Cucumaria species were also obtained and identified. The structures of new compounds were established on the basis of extensive analysis of the 1D and 2D NMR spectra, as well as by the HR-ESI-MS data. The aglycones of 1–5 differed by side chains structures. Additionally, conicospermiumoside A₇-1 (4) had a 9(11)-double bond in the aglycone, while the remaining glycosides contained a 7(8)-intranuclear double bond. Eight types of carbohydrate chains known earlier from the glycosides of the sea cucumbers of the Cucumaria genus were found as part of the glycosides of C. conicospermium. The set of sugar chains of the glycosides from C. conicospermium was similar to that from C. okhotensis. The raw biogenetic series of aglycones, leading to the formation of hexa-nor-lanostane derivatives in the process of biosynthesis and a sort of functionally-structural division that was realized due to separation of biosynthetic pathways of holostane and lanostane derivatives, can be traced when the structures of the glycosides isolated from C. conicospermium are compared. The cytotoxic action against three human breast cancer cell lines (MCF-7, T-47D, MDA-MB-231), and non-tumor MCF-10A and hemolytic activity of compounds 1–5, as well as seven known glycosides were tested. Conicospermiumosides A₃-3 (3) and A₇-1 (4), having a 22-oxo-23(24)-en fragment, were strongly hemolytic despite lacking a lactone in their aglycones. Moreover, both compounds demonstrated a promising suppressing action against triple negative breast cancer cells. The cells of the MDA-MB-231 line were most sensitive to the cytotoxic action of the glycosides, while the MCF-7 cell line was most sustainable. Six glycosides were selected for further study of some aspects of anticancer action against MDA-MB-231. The selective action of the compounds 4 and 8 on the MDA-MB-231 cells without significant toxicity against the MCF-10A cells was noticeable. More importantly, the selectivity of the compounds was changed over time and maximal selectivity to cancer cells was demonstrated by glycoside 1 at 48 h of exposition. The glycosides 1, 3 and the desulfated derivative 7a strongly inhibited colony formation and growth of the TNBC cells until the process stops completely. Okhotoside B₁ (8), DS-okhotoside A₁-1 (7a), and conicospermiumoside A₃-3 (3) showed a potent cell migration-inhibiting capacity. Quantitative structure–activity relationships (QSARs) calculated on the basis of a correlational analysis of the physicochemical properties and structural features of the glycosides and their cytotoxic activity against different cell lines showed some structural features influenced differently, sometimes even in opposite ways, on the activity of glycosides toward diverse cells (erythrocytes, MCF-10A, and TNBC MDA-MB-231 cells). This observation indicated that glycosides obviously target different membrane components, such as lipids of erythrocytes and some receptors on the surface of mammary normal or tumor cells. Full article

(This article belongs to the Special Issue Novel Biomaterials and Active Compounds from Sea Cucumbers)

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10 pages, 1989 KiB

Open AccessArticle

Three New Dipeptide and Two New Polyketide Derivatives from the Mangrove-Derived Fungus Talaromyces sp.: Antioxidant Activity of Two Isolated Substances

by Zhihao Zeng, Jian Cai, Yi Chen, Xinlong Li, Chunmei Chen, Yonghong Liu, Lalith Jayasinghe and Xuefeng Zhou

Mar. Drugs 2024, 22(12), 559; https://doi.org/10.3390/md22120559 - 14 Dec 2024

Abstract

Five new metabolites, including three cyclic dipeptide derivatives (1–3) and two new polyketides (10–11), together with nine known ones (4–9 and 12–15), were isolated from the mangrove-sediments-derived fungus Talaromyces [...] Read more.

Five new metabolites, including three cyclic dipeptide derivatives (1–3) and two new polyketides (10–11), together with nine known ones (4–9 and 12–15), were isolated from the mangrove-sediments-derived fungus Talaromyces sp. SCSIO 41431. Their structures were determined using detailed NMR, MS spectroscopic analyses, and quantum chemical calculations. X-ray single-crystal diffraction analysis of 1 was described. Compounds 13–15 demonstrated activity against Staphylococcus aureus, with MIC values ranging from 25 to 50 µg/mL. Compound 9 showed activity against Escherichia coli, Streptococcus suis, and Erysipelothrix rhusiopathiae, with an MIC value of 100 µg/mL. In addition, compounds 1 and 12 showed DPPH radical scavenging activity, with the EC₅₀ of 27.62 and 29.34 µg/mL, compared to the positive control (ascorbic acid, EC₅₀, 12.74 µg/mL). Full article

(This article belongs to the Special Issue Novel Marine Antimicrobial Agents: Isolation, Synthesis, and Biological Evaluation)

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11 pages, 2492 KiB

Open AccessArticle

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

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

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

Abstract

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

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

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

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13 pages, 2327 KiB

Open AccessArticle

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

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

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

Abstract

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

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

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

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24 pages, 1964 KiB

Open AccessArticle

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

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

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

Abstract

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

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

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

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18 pages, 4799 KiB

Open AccessArticle

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

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

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

Abstract

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

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

(This article belongs to the Section Marine Pharmacology)

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44 pages, 2640 KiB

Open AccessReview

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

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

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

Abstract

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

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

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

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