Marine Drugs

11 pages, 1552 KiB

Open AccessArticle

Chrysomycins, Anti-Tuberculosis C-Glycoside Polyketides from Streptomyces sp. MS751

by Jiaming Yu, Hui Guo, Jing Zhang, Jiansen Hu, Hongtao He, Caixia Chen, Na Yang, Fan Yang, Zexu Lin, Huanqin Dai, Liming Ouyang, Cuihua Liu, Xiaoguang Lei, Lixin Zhang, Guoliang Zhu and Fuhang Song

Mar. Drugs 2024, 22(6), 259; https://doi.org/10.3390/md22060259 (registering DOI) - 3 Jun 2024

Abstract

A new dimeric C-glycoside polyketide chrysomycin F (1), along with four new monomeric compounds, chrysomycins G (2), H (3), I (4), J (5), as well as three known analogues, chrysomycins A (6 [...] Read more.

A new dimeric C-glycoside polyketide chrysomycin F (1), along with four new monomeric compounds, chrysomycins G (2), H (3), I (4), J (5), as well as three known analogues, chrysomycins A (6), B (7), and C (8), were isolated and characterised from a strain of Streptomyces sp. obtained from a sediment sample collected from the South China Sea. Their structures were determined by detailed spectroscopic analysis. Chrysomycin F contains two diastereomers, whose structures were further elucidated by a biomimetic [2 + 2] photodimerisation of chrysomycin A. Chrysomycins B and C showed potent anti-tuberculosis activity against both wild-type Mycobacterium tuberculosis and a number of clinically isolated MDR M. tuberculosis strains. Full article

(This article belongs to the Special Issue Marine Streptomyces-Derived Natural Products 2024)

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15 pages, 2188 KiB

Open AccessArticle

Distribution and Level of Bioactive Monoacylglycerols in 12 Marine Microalgal Species

by Giovanna Santaniello, Gianna Falascina, Marcello Ziaco, Laura Fioretto, Angela Sardo, Martina Carelli, Mariarosaria Conte, Giovanna Romano and Adele Cutignano

Mar. Drugs 2024, 22(6), 258; https://doi.org/10.3390/md22060258 - 31 May 2024

Abstract

Microalgae are currently considered an attractive source of highly valuable metabolites potentially exploitable as anticancer agents, nutraceuticals and cosmeceuticals and for bioenergy purposes. Their ease of culturing and their high growth rates further promote their use as raw material for the production of [...] Read more.

Microalgae are currently considered an attractive source of highly valuable metabolites potentially exploitable as anticancer agents, nutraceuticals and cosmeceuticals and for bioenergy purposes. Their ease of culturing and their high growth rates further promote their use as raw material for the production of specialty products. In the present paper, we focused our attention on specific glycerol-based lipid compounds, monoacylglycerols (MAGs), which displayed in our previous studies a selective cytotoxic activity against the haematological U-937 and the colon HCT-116 cancer cell lines. Here, we performed a quali/quantitative analysis of MAGs and total fatty acids (FAs) along with a profiling of the main lipid classes in a panel of 12 microalgal species, including diatoms and dinoflagellates. Our results highlight an inter- and intraspecific variability of MAG profile in the selected strains. Among them, Skeletonema marinoi (strain FE7) has emerged as the most promising source for possible biotechnological production of MAGs. Full article

(This article belongs to the Special Issue Biotechnological Applications of Marine Microalgae)

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13 pages, 7709 KiB

Open AccessArticle

Functional Characterization of the First Bona Fide Phytoene Synthase in Red Algae from Pyropia yezoensis

by Cheng-Ling Li, Jia-Qiu Pu, Wei Zhou, Chuan-Ming Hu, Yin-Yin Deng, Ying-Ying Sun and Li-En Yang

Mar. Drugs 2024, 22(6), 257; https://doi.org/10.3390/md22060257 - 31 May 2024

Abstract

The formation of phytoene by condensing two geranylgeranyl diphosphate molecules catalyzed by phytoene synthase (PSY) is the first committed and rate-limiting step in carotenoid biosynthesis, which has been extensively investigated in bacteria, land plants and microalgae. However, this step in macroalgae remains unknown. [...] Read more.

The formation of phytoene by condensing two geranylgeranyl diphosphate molecules catalyzed by phytoene synthase (PSY) is the first committed and rate-limiting step in carotenoid biosynthesis, which has been extensively investigated in bacteria, land plants and microalgae. However, this step in macroalgae remains unknown. In the present study, a gene encoding putative phytoene synthase was cloned from the economic red alga Pyropia yezoensis—a species that has long been used in food and pharmaceuticals. The conservative motifs/domains and the tertiary structure predicted using bioinformatic tools suggested that the cloned PyPSY should encode a phytoene synthase; this was empirically confirmed by pigment complementation in E. coli. This phytoene synthase was encoded by a single copy gene, whose expression was presumably regulated by many factors. The phylogenetic relationship of PSYs from different organisms suggested that red algae are probably the progeny of primary endosymbiosis and plastid donors of secondary endosymbiosis. Full article

(This article belongs to the Special Issue Enzymes from Marine By-Products and Wastes)

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24 pages, 5396 KiB

Open AccessReview

Revolutionizing Cardiovascular Health with Nano Encapsulated Omega-3 Fatty Acids: A Nano-Solution Approach

by Richa Gill, Mashael Al-Badr, Mohammad Alghouti, Nura Adam Mohamed, Haissam Abou-Saleh and Md Mizanur Rahman

Mar. Drugs 2024, 22(6), 256; https://doi.org/10.3390/md22060256 - 30 May 2024

Viewed by 16

Abstract

Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) offer diverse health benefits, such as supporting cardiovascular health, improving cognitive function, promoting joint and musculoskeletal health, and contributing to healthy aging. Despite their advantages, challenges like oxidation susceptibility, low bioavailability, and potential adverse effects at high [...] Read more.

Omega-3 polyunsaturated fatty acids (ω-3 PUFAs) offer diverse health benefits, such as supporting cardiovascular health, improving cognitive function, promoting joint and musculoskeletal health, and contributing to healthy aging. Despite their advantages, challenges like oxidation susceptibility, low bioavailability, and potential adverse effects at high doses persist. Nanoparticle encapsulation emerges as a promising avenue to address these limitations while preserving stability, enhanced bioavailability, and controlled release. This comprehensive review explores the therapeutic roles of omega-3 fatty acids, critically appraising their shortcomings and delving into modern encapsulation strategies. Furthermore, it explores the potential advantages of metal–organic framework nanoparticles (MOF NPs) compared to other commonly utilized nanoparticles in improving the therapeutic effectiveness of omega-3 fatty acids within drug delivery systems (DDSs). Additionally, it outlines future research directions to fully exploit the therapeutic benefits of these encapsulated omega-3 formulations for cardiovascular disease treatment. Full article

(This article belongs to the Special Issue Value-Added Products from Marine Fishes)

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21 pages, 5548 KiB

Open AccessArticle

Stem-Cell-Regenerative and Protective Effects of Squid (Symplectoteuthis oualaniensis) Skin Collagen Peptides against H₂O₂-Induced Fibroblast Injury

by Mingjun Wei, Lakshmi Jeevithan, Na Li, Lixin Liu, Jiren Xu, Wenhui Wu and Jeevithan Elango

Mar. Drugs 2024, 22(6), 255; https://doi.org/10.3390/md22060255 - 30 May 2024

Viewed by 77

Abstract

Recently, there has been a growing interest in collagen peptides derived from marine sources for their notable ability to protect skin cells against apoptosis induced by oxidants. Therefore, the current study aimed to investigate the fundamental properties of collagen peptides, including their physicochemical, [...] Read more.

Recently, there has been a growing interest in collagen peptides derived from marine sources for their notable ability to protect skin cells against apoptosis induced by oxidants. Therefore, the current study aimed to investigate the fundamental properties of collagen peptides, including their physicochemical, thermal, structural, stem-cell-regenerative, and skin-cell-protective effects, in comparison to commercial collagen peptides. The acid-soluble (ASC) and pepsin-soluble (PSC) collagens exhibited three distinct bands on SDS-PAGE, namely α (α₁ and α₂), β, and γ chains, confirming a type I pattern. The thermal profiles obtained from TG and DSC analyses confirmed the denaturation of PSC and ASC at temperatures ranging from 51.94 to 56.4 °C and from 52.07 to 56.53 °C, respectively. The purified collagen peptides were analyzed using SDS-PAGE and MALDI-TOF mass spectrometry, revealing a mass range of 900–15,000 Da. Furthermore, the de novo peptide sequence analysis confirmed the presence of the Gly-X-Y repeating sequence in collagen peptides. Collagen peptide treatments significantly enhanced HFF-1 cell proliferation and migration compared to the control group. ELISA results confirmed the potential interactions between collagen peptides and HFF-1 cells through α₂β₁, α₁₀β₁, and α₁₁β₁ integrin receptors. Notably, collagen peptide treatment effectively restored the proliferation of HFF-1 cells damaged by H₂O₂. Consequently, the advantageous characteristics of squid skin collagen peptides highlight their promising role in regenerative medicine. Full article

(This article belongs to the Special Issue Fundamentals and Biomedical Applications of Marine Collagen)

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16 pages, 951 KiB

Open AccessArticle

Tracing the Impact of Domestic Storage Conditions on Antioxidant Activity and Lipid Profiles in the Edible Microalgae Chlorella vulgaris and Tetraselmis chui

by Diana Lopes, Felisa Rey, Alexandrina Gomes, Luís Duarte, João Pereira, Marisa Pinho, Tânia Melo and Rosário Domingues

Mar. Drugs 2024, 22(6), 254; https://doi.org/10.3390/md22060254 - 30 May 2024

Viewed by 102

Abstract

The microalgae Chlorella vulgaris and Tetraselmis chui are valued for their nutrient-rich content, including lipids and polyunsaturated fatty acids (PUFA). However, little is known about how storage and processing affect their lipid quality. This study aimed to assess the impact of domestic storage [...] Read more.

The microalgae Chlorella vulgaris and Tetraselmis chui are valued for their nutrient-rich content, including lipids and polyunsaturated fatty acids (PUFA). However, little is known about how storage and processing affect their lipid quality. This study aimed to assess the impact of domestic storage and cooking practices in dried biomass of C. vulgaris and T. chui. Four conditions were tested: control (newly opened package), light (storage at room temperature and daily light regimen for three weeks), frozen (storage in the freezer at −20 °C for three weeks), and heated (three cycles of 90 min at 100 °C). Lipid extracts were analyzed by GC-MS and LC-MS, and antioxidant activity through DPPH and ABTS radical scavenging assays. Tested storage conditions promoted a decrease in fatty acid content and in diacyl/lyso lipid species ratios of phospholipid (PC/LPC, PE/LPE) and betaine lipids (DGTS/MGTS). Lipid extracts from light treatment showed the lowest antioxidant activity in C. vulgaris (ABTS, IC40: 104.9; DPPH, IC20: 187.9 ± 15.0), while heat affected the antioxidant activity of T. chui (ABTS, IC40: 88.5 ± 2.8; DPPH, IC20 209.4 ± 10.9). These findings underscore the impact of managing storage and processing conditions to optimize the nutritional and functional benefits of C. vulgaris and T. chui in food and feed applications. Full article

(This article belongs to the Special Issue Lipidomics in Marine Microalgae and Seaweeds: Applications and Perspectives)

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47 pages, 12167 KiB

Open AccessReview

Transition-Metal-Catalyzed Transformations for the Synthesis of Marine Drugs

by Lucía G. Parte, Sergio Fernández, Eva Sandonís, Javier Guerra and Enol López

Mar. Drugs 2024, 22(6), 253; https://doi.org/10.3390/md22060253 - 29 May 2024

Viewed by 341

Abstract

Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to [...] Read more.

Transition metal catalysis has contributed to the discovery of novel methodologies and the preparation of natural products, as well as new chances to increase the chemical space in drug discovery programs. In the case of marine drugs, this strategy has been used to achieve selective, sustainable and efficient transformations, which cannot be obtained otherwise. In this perspective, we aim to showcase how a variety of transition metals have provided fruitful couplings in a wide variety of marine drug-like scaffolds over the past few years, by accelerating the production of these valuable molecules. Full article

(This article belongs to the Special Issue Scaffold Diversity of Marine Natural Products)

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13 pages, 2805 KiB

Open AccessArticle

αO-Conotoxin GeXIVA[1,2] Suppresses In Vivo Tumor Growth of Triple-Negative Breast Cancer by Inhibiting AKT-mTOR, STAT3 and NF-κB Signaling Mediated Proliferation and Inducing Apoptosis

by Xijun Guo, Leping He, Weifeng Xu, Wanrong Wang, Xiaoli Feng, Yuanfeng Fu, Xiaofan Zhang, Ren-Bo Ding, Xingzhu Qi, Jiaolin Bao and Sulan Luo

Mar. Drugs 2024, 22(6), 252; https://doi.org/10.3390/md22060252 - 29 May 2024

Viewed by 213

Abstract

Breast cancer is one of the leading causes of cancer mortality worldwide, and triple-negative breast cancer (TNBC) is the most problematic subtype. There is an urgent need to develop novel drug candidates for TNBC. Marine toxins are a valuable source for drug discovery. [...] Read more.

Breast cancer is one of the leading causes of cancer mortality worldwide, and triple-negative breast cancer (TNBC) is the most problematic subtype. There is an urgent need to develop novel drug candidates for TNBC. Marine toxins are a valuable source for drug discovery. We previously identified αO-conotoxin GeXIVA[1,2] from Conus generalis, which is a selective antagonist of α9 nicotinic acetylcholine receptors (nAChRs). Recent studies indicated that α9 nAChR expression is positively correlated with breast cancer development; thus, α9 nAChR could serve as a therapeutic target for breast cancer. In this study, we aimed to investigate the in vivo antitumor effects of GeXIVA[1,2] on TNBC and to elucidate its underlying anticancer mechanism. Our data showed that GeXIVA[1,2] effectively suppressed 4T1 tumor growth in vivo at a very low dose of 0.1 nmol per mouse. Our results uncovered that the antitumor mechanism of GeXIVA[1,2] simultaneously induced apoptosis and blocked proliferation. Further investigations revealed that GeXIVA[1,2]-induced Caspase-3-dependent apoptosis was achieved through regulating Bax/Bcl-2 balance, and GeXIVA[1,2]-inhibited proliferation was mediated by the downregulation of the AKT-mTOR, STAT3 and NF-κB signaling pathways. Our study provides valuable arguments to demonstrate the potential of GeXIVA[1,2] as a novel marine-derived anticancer drug candidate for the treatment of TNBC. Full article

(This article belongs to the Section Marine Toxins)

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11 pages, 2106 KiB

Open AccessArticle

Fucoidan from Lessonia trabeculata Induces Apoptosis through Caspase Dependent and Caspase-Independent Activation in 4T1 Breast Adenocarcinoma In Vitro

by Raisa Teresa Cruz Riquelme, Erasmo Honorio Colona-Vallejos, Libertad Alzamora-Gonzales and Rosa María Condori Macuri

Mar. Drugs 2024, 22(6), 251; https://doi.org/10.3390/md22060251 - 29 May 2024

Viewed by 242

Abstract

Experiments conducted on triple-negative breast cancer have shown that fucoidan from Lessonia trabeculata (FLt) exhibits cytotoxic and antitumor properties. However, further research is necessary to gain a complete understanding of its bioactivity and level of cytotoxicity. The cytotoxic effect of FLt was determined [...] Read more.

Experiments conducted on triple-negative breast cancer have shown that fucoidan from Lessonia trabeculata (FLt) exhibits cytotoxic and antitumor properties. However, further research is necessary to gain a complete understanding of its bioactivity and level of cytotoxicity. The cytotoxic effect of FLt was determined by the 2,5-diphenyl-2H-tetrazolium bromide (MTT) assay. Apoptosis was analyzed using annexin V and caspase 3/7 staining kit and DNA fragmentation. In addition, transcriptional expression of antiapoptotic (Bcl-2 and XIAP) and proapoptotic (caspase 8, caspase 9, and AIF) genes were analyzed in TNBC 4T1 cells. After 72 h of culture, the IC₅₀ for FLt was 561 μg/mL, while doxorubicin (Dox) had an IC₅₀ of 0.04 μg/mL. In addition, assays for FLt + Dox were performed. Annexin V and caspase 3/7 revealed that FLt induces early and late-stage apoptosis. DNA fragmentation results support necrotic death of 4T1 cells. Similarly, transcripts that prevent cell death were decreased, while transcripts that promote cell death were increased. This study showed that FLt induces apoptosis by both caspase-dependent and caspase-independent mechanisms. These findings suggest that FLt may have potential applications in breast cancer treatment. Further research will provide more information to elucidate the mechanism of action of FLt. Full article

(This article belongs to the Special Issue Antioxidant and Anticancer Activities of Compounds Isolated from Seagrasses and Seaweeds)

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36 pages, 3836 KiB

Open AccessArticle

Marine Cytotoxin Santacruzamate A Derivatives as Potent HDAC1-3 Inhibitors and Their Synergistic Anti-Leukemia Effects with Venetoclax

by Wanting Hao, Leyan Wang, Tongqiang Xu, Geng Jia, Yuqi Jiang, Chong Qin and Xiaoyang Li

Mar. Drugs 2024, 22(6), 250; https://doi.org/10.3390/md22060250 - 28 May 2024

Viewed by 240

Abstract

Acute myeloid leukemia (AML) is a hematologic malignancy characterized by infiltration of the blood and bone marrow, exhibiting a low remission rate and high recurrence rate. Current research has demonstrated that class I HDAC inhibitors can downregulate anti-apoptotic proteins, leading to apoptosis of [...] Read more.

Acute myeloid leukemia (AML) is a hematologic malignancy characterized by infiltration of the blood and bone marrow, exhibiting a low remission rate and high recurrence rate. Current research has demonstrated that class I HDAC inhibitors can downregulate anti-apoptotic proteins, leading to apoptosis of AML cells. In the present investigation, we conducted structural modifications of marine cytotoxin Santacruzamate A (SCA), a compound known for its inhibitory activity towards HDACs, resulting in the development of a novel series of potent class I HDACs hydrazide inhibitors. Representative hydrazide-based compound 25c exhibited concentration-dependent induction of apoptosis in AML cells as a single agent. Moreover, 25c exhibited a synergistic anti-AML effect when combined with Venetoclax, a clinical Bcl-2 inhibitor employed in AML therapy. This combination resulted in a more pronounced downregulation of anti-apoptotic proteins Mcl-1 and Bcl-xL, along with a significant upregulation of the pro-apoptotic protein cleaved-caspase3 and the DNA double-strand break biomarker γ-H2AX compared to monotherapy. These results highlighted the potential of 25c as a promising lead compound for AML treatment, particularly when used in combination with Venetoclax. Full article

(This article belongs to the Special Issue Synthesis and Discovery of Marine Antitumor Molecules)

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14 pages, 2861 KiB

Open AccessArticle

Pinctada martensii Hydrolysate Modulates the Brain Neuropeptidome and Proteome in Diabetic (db/db) Mice via the Gut–Brain Axis

by Jiayun Li, Yijun Lv, Yuanqing Wei, Xinzhi Wang, Shenghan Yan, Binyuan Zhao, Jipeng Sun, Rui Liu and Yueyang Lai

Mar. Drugs 2024, 22(6), 249; https://doi.org/10.3390/md22060249 - 28 May 2024

Viewed by 151

Abstract

Pinctada martensii hydrolysate (PMH) has been proved to have the effect of ameliorating disorders of glucose and lipid metabolism in db/db mice, but the mechanism of its hyperglycemia effect is still unclear. Bacterial communities in fecal samples from a normal control group, a [...] Read more.

Pinctada martensii hydrolysate (PMH) has been proved to have the effect of ameliorating disorders of glucose and lipid metabolism in db/db mice, but the mechanism of its hyperglycemia effect is still unclear. Bacterial communities in fecal samples from a normal control group, a diabetic control group, and a PMH-treated diabetes mellitus type 2 (T2DM) group were analyzed by 16S gene sequencing. Nano LC-MS/MS was used to analyze mice neuropeptides and proteomes. The 16S rDNA sequencing results showed that PMH modulated the structure and composition of the gut microbiota and improved the structure and composition of Firmicutes and Bacteroidetes at the phylum level and Desulfovibrionaceae and Erysipelatoclostridiaceae at the family level. Furthermore, the expressions of functional proteins of the central nervous system, immune response-related protein, and proteins related to fatty acid oxidation in the brain disrupted by an abnormal diet were recovered by PMH. PMH regulates the brain neuropeptidome and proteome and further regulates blood glucose in diabetic mice through the gut–brain axis. PMH may be used as a prebiotic agent to attenuate T2DM, and target-specific microbial species may have unique therapeutic promise for metabolic diseases. Full article

(This article belongs to the Special Issue Marine Natural Products in Anti-obesity and Metabolic Syndrome)

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17 pages, 2097 KiB

Open AccessArticle

Evaluation of the Biological Activities of Peptides from Epidermal Mucus of Marine Fish Species from Chilean Aquaculture

by Claudio A. Álvarez, Teresa Toro-Araneda, Juan Pablo Cumillaf, Belinda Vega, María José Tapia, Tanya Roman, Constanza Cárdenas, Valentina Córdova-Alarcón, Carlos Jara-Gutiérrez, Paula A. Santana and Fanny Guzmán

Mar. Drugs 2024, 22(6), 248; https://doi.org/10.3390/md22060248 - 28 May 2024

Viewed by 253

Abstract

The skin of fish is a physicochemical barrier that is characterized by being formed by cells that secrete molecules responsible for the first defense against pathogenic organisms. In this study, the biological activity of peptides from mucus of Seriola lalandi and Seriolella violacea [...] Read more.

The skin of fish is a physicochemical barrier that is characterized by being formed by cells that secrete molecules responsible for the first defense against pathogenic organisms. In this study, the biological activity of peptides from mucus of Seriola lalandi and Seriolella violacea were identified and characterized. To this purpose, peptide extraction was carried out from epidermal mucus samples of juveniles of both species, using chromatographic strategies for purification. Then, the peptide extracts were characterized to obtain the amino acid sequence by mass spectrometry. Using bioinformatics tools for predicting antimicrobial and antioxidant activity, 12 peptides were selected that were chemically produced by simultaneous synthesis using the Fmoc-Tbu strategy. The results revealed that the synthetic peptides presented a random coil or extended secondary structure. The analysis of antimicrobial activity allowed it to be discriminated that four peptides, named by their synthesis code 5065, 5069, 5070, and 5076, had the ability to inhibit the growth of Vibrio anguillarum and affected the copepodite stage of C. rogercresseyi. On the other hand, peptides 5066, 5067, 5070, and 5077 had the highest antioxidant capacity. Finally, peptides 5067, 5069, 5070, and 5076 were the most effective for inducing respiratory burst in fish leukocytes. The analysis of association between composition and biological function revealed that the antimicrobial activity depended on the presence of basic and aromatic amino acids, while the presence of cysteine residues increased the antioxidant activity of the peptides. Additionally, it was observed that those peptides that presented the highest antimicrobial capacity were those that also stimulated respiratory burst in leukocytes. This is the first work that demonstrates the presence of functional peptides in the epidermal mucus of Chilean marine fish, which provide different biological properties when the fish face opportunistic pathogens. Full article

(This article belongs to the Special Issue Marine Bioactive Peptides—Structure, Function, and Application 2.0)

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14 pages, 3545 KiB

Open AccessArticle

Antiviral Potential of Fucoxanthin, an Edible Carotenoid Purified from Sargassum siliquastrum, against Zika Virus

by Nalae Kang, Eun-A Kim, Areumi Park, Seong-Yeong Heo, Jun-Ho Heo and Soo-Jin Heo

Mar. Drugs 2024, 22(6), 247; https://doi.org/10.3390/md22060247 - 28 May 2024

Viewed by 208

Abstract

Considering the lack of antiviral drugs worldwide, we investigated the antiviral potential of fucoxanthin, an edible carotenoid purified from Sargassum siliquastrum, against zika virus (ZIKV) infection. The antiviral activity of fucoxanthin was assessed in ZIKV-infected Vero E6 cells, and the relevant structural [...] Read more.

Considering the lack of antiviral drugs worldwide, we investigated the antiviral potential of fucoxanthin, an edible carotenoid purified from Sargassum siliquastrum, against zika virus (ZIKV) infection. The antiviral activity of fucoxanthin was assessed in ZIKV-infected Vero E6 cells, and the relevant structural characteristics were confirmed using molecular docking and molecular dynamics (MD) simulation. Fucoxanthin decreased the infectious viral particles and nonstructural protein (NS)1 mRNA expression levels at concentrations of 12.5, 25, and 50 µM in ZIKV-infected cells. Fucoxanthin also decreased the increased mRNA levels of interferon-induced proteins with tetratricopeptide repeat 1 and 2 in ZIKV-infected cells. Molecular docking simulations revealed that fucoxanthin binds to three main ZIKV proteins, including the envelope protein, NS3, and RNA-dependent RNA polymerase (RdRp), with binding energies of −151.449, −303.478, and −290.919 kcal/mol, respectively. The complex of fucoxanthin with RdRp was more stable than RdRp protein alone based on MD simulation. Further, fucoxanthin bonded to the three proteins via repeated formation and disappearance of hydrogen bonds. Overall, fucoxanthin exerts antiviral potential against ZIKV by affecting its three main proteins in a concentration-dependent manner. Thus, fucoxanthin isolated from S. siliquastrum is a potential candidate for treating zika virus infections. Full article

(This article belongs to the Special Issue Antiviral Effects and Molecular Mechanisms of Marine Compounds)

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13 pages, 1787 KiB

Open AccessArticle

Optimizing Phycocyanin Extraction from Cyanobacterial Biomass: A Comparative Study of Freeze–Thaw Cycling with Various Solvents

by Konstantinos Pispas, Georgios Manthos, Eirini Sventzouri, Maria Geroulia, Savvas Giannis Mastropetros, Sameh Samir Ali and Michael Kornaros

Mar. Drugs 2024, 22(6), 246; https://doi.org/10.3390/md22060246 - 28 May 2024

Viewed by 331

Abstract

Cyanobacterial phycocyanin pigment is widely utilized for its properties in various industries, including food, cosmetics, and pharmaceuticals. Despite its potential, challenges exist, such as extraction methods impacting yield, stability, and purity. This study investigates the impact of the number of freeze–thaw (FT) cycles [...] Read more.

Cyanobacterial phycocyanin pigment is widely utilized for its properties in various industries, including food, cosmetics, and pharmaceuticals. Despite its potential, challenges exist, such as extraction methods impacting yield, stability, and purity. This study investigates the impact of the number of freeze–thaw (FT) cycles on the extraction of phycocyanin from the wet biomass of four cyanobacteria species (Arthrospira platensis, Chlorogloeopsis fritschii, Phormidium sp., and Synechocystis sp.), along with the impact of five extraction solutions (Tris-HCl buffer, phosphate buffer, CaCl₂, deionized water, and tap water) at various pH values. Synechocystis sp. exhibited the highest phycocyanin content among the studied species. For A. platensis, Tris-HCl buffer yielded maximum phycocyanin concentration from the first FT cycle, while phosphate buffer provided satisfactory results from the second cycle. Similarly, Tris-HCl buffer showed promising results for C. fritschii (68.5% of the maximum from the first cycle), with the highest concentration (~12% w/w) achieved during the seventh cycle, using phosphate buffer. Phormidium sp. yielded the maximum pigment concentration from the first cycle using tap water. Among species-specific optimal extraction solutions, Tris-HCl buffer demonstrated sufficient extraction efficacy for all species, from the first cycle. This study represents an initial step toward establishing a universal extraction method for phycocyanin from diverse cyanobacteria species. Full article

(This article belongs to the Special Issue Recent Advances in Marine-Derived Pigments)

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23 pages, 10914 KiB

Open AccessArticle

Development and Validation of a Liquid Chromatography–Tandem Mass Spectrometry Method for Screening Potential Citrate Lyase Inhibitors from a Library of Marine Compounds

by Jiahong Wang, Huashi Guan and Zhe Xu

Mar. Drugs 2024, 22(6), 245; https://doi.org/10.3390/md22060245 - 27 May 2024

Viewed by 328

Abstract

Tuberculosis, a persistent illness caused by Mycobacterium tuberculosis, remains a significant global public health challenge. The widespread use of anti-tuberculosis drugs has resulted in the emergence of drug-resistant strains, which complicates treatment efforts. Addressing this issue is crucial and hinges on the [...] Read more.

Tuberculosis, a persistent illness caused by Mycobacterium tuberculosis, remains a significant global public health challenge. The widespread use of anti-tuberculosis drugs has resulted in the emergence of drug-resistant strains, which complicates treatment efforts. Addressing this issue is crucial and hinges on the development of new drugs that can effectively target the disease. This involves identifying novel therapeutic targets that can disrupt the bacterium’s survival mechanisms in various environments such as granulomas and lesions. Citrate lyase, essential for the survival of Mycobacterium species at lesion sites and in granulomatous conditions, is a potential target for the treatment of tuberculosis. This manuscript aimed to construct an efficient enzyme inhibitor screening platform using ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UHPLC-QTOF MS). This system can accurately identify compounds with enzyme inhibitory activity from a library of marine terpenoids and phenolic compounds. Utilizing the screened herbal enzyme inhibitors as a starting point, we analyzed their chemical structures and skillfully built a library of marine compounds based on these structures. The results showed that all of the tested compounds from the phenolics library inhibited citrate lyase by more than 50%, and a significant portion of terpenoids also demonstrated inhibition, with these active terpenoids comprising over half of the terpenoids tested. The study underscores the potential of marine-derived phenolic and terpenoid compounds as potent inhibitors of citrate lyase, indicating a promising direction for future investigations in treating tuberculosis and associated disorders. Full article

(This article belongs to the Special Issue Marine-Derived Terpenes: Chemistry, Synthesis and Their Therapeutic Potential)

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15 pages, 2904 KiB

Open AccessArticle

The Identification of Peptide Inhibitors of the Coronavirus 3CL Protease from a Fucus ceranoides L. Hydroalcoholic Extract Using a Ligand-Fishing Strategy

by Luiz Antonio Miranda de Souza Duarte Filho, Cintia Emi Yanaguibashi Leal, Pierre-Edouard Bodet, Edilson Beserra de Alencar Filho, Jackson Roberto Guedes da Silva Almeida, Manon Porta Zapata, Oussama Achour, Hugo Groult, Carlos Arthur Gouveia Veloso, Claudio Viegas Júnior, Nathalie Bourgougnon and Laurent Picot

Mar. Drugs 2024, 22(6), 244; https://doi.org/10.3390/md22060244 - 27 May 2024

Viewed by 413

Abstract

Brown seaweeds of the Fucus genus represent a rich source of natural antiviral products. In this study, a Fucus ceranoides hydroalcoholic extract (FCHE) was found to inhibit 74.2 ± 1.3% of the proteolytic activity of the free SARS-CoV-2 3CL protease (3CLpro), an enzyme [...] Read more.

Brown seaweeds of the Fucus genus represent a rich source of natural antiviral products. In this study, a Fucus ceranoides hydroalcoholic extract (FCHE) was found to inhibit 74.2 ± 1.3% of the proteolytic activity of the free SARS-CoV-2 3CL protease (3CLpro), an enzyme that plays a pivotal role in polyprotein processing during coronavirus replication and has been identified as a relevant drug discovery target for SARS- and MERS-CoVs infections. To purify and identify 3CLpro ligands with potential inhibitory activity using a one-step approach, we immobilized the enzyme onto magnetic microbeads (3CLpro-MPs), checked that the enzymatic activity was maintained after grafting, and used this bait for a ligand-fishing strategy followed by a high-resolution mass spectrometry analysis of the fished-out molecules. Proof of concept for the ligand-fishing capacity of the 3CLpro-MPs was demonstrated by doping the FCHE extract with the substrate peptide TSAVLQ-pNA, resulting in the preferential capture of this high-affinity peptide within the macroalgal complex matrix. Ligand fishing in the FCHE alone led to the purification and identification via high-resolution mass spectrometry (HRMS) of seven hepta-, octa-, and decapeptides in an eluate mix that significantly inhibited the free 3CLpro more than the starting FCHE (82.7 ± 2.2% inhibition). Molecular docking simulations of the interaction between each of the seven peptides and the 3CLpro demonstrated a high affinity for the enzyme’s proteolytic active site surpassing that of the most affine peptide ligand identified so far (a co-crystallographic peptide). Testing of the corresponding synthetic peptides demonstrated that four out of seven significantly inhibited the free 3CLpro (from 46.9 ± 6.4 to 76.8 ± 3.6% inhibition at 10 µM). This study is the first report identifying peptides from Fucus ceranoides with high inhibitory activity against the SARS-CoV-2 3CLprotease which bind with high affinity to the protease’s active site. It also confirms the effectiveness of the ligand-fishing strategy for the single-step purification of enzyme inhibitors from complex seaweed matrices. Full article

(This article belongs to the Section Marine Pharmacology)

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14 pages, 1733 KiB

Open AccessArticle

Miniaturized Cultivation Profiling (MATRIX)-Facilitated Discovery of Noonazines A–C and Noonaphilone A from an Australian Marine-Derived Fungus, Aspergillus noonimiae CMB-M0339

by Sarani Kankanamge, Paul V. Bernhardt, Zeinab G. Khalil and Robert J. Capon

Mar. Drugs 2024, 22(6), 243; https://doi.org/10.3390/md22060243 - 27 May 2024

Viewed by 451

Abstract

Subjecting the Australian marine-derived fungus Aspergillus noonimiae CMB-M0339 to cultivation profiling using an innovative miniaturized 24-well plate format (MATRIX) enabled access to new examples of the rare class of 2,6-diketopiperazines, noonazines A–C (1–3), along with the known analogue coelomycin [...] Read more.

Subjecting the Australian marine-derived fungus Aspergillus noonimiae CMB-M0339 to cultivation profiling using an innovative miniaturized 24-well plate format (MATRIX) enabled access to new examples of the rare class of 2,6-diketopiperazines, noonazines A–C (1–3), along with the known analogue coelomycin (4), as well as a new azaphilone, noonaphilone A (5). Structures were assigned to 1–5 on the basis of a detailed spectroscopic analysis, and in the case of 1–2, an X-ray crystallographic analysis. Plausible biosynthetic pathways are proposed for 1–4, involving oxidative Schiff base coupling/dimerization of a putative Phe precursor. Of note, 2 incorporates a rare meta-Tyr motif, typically only reported in a limited array of Streptomyces metabolites. Similarly, a plausible biosynthetic pathway is proposed for 5, highlighting a single point for stereo-divergence that allows for the biosynthesis of alternate antipodes, for example, the 7R noonaphilone A (5) versus the 7S deflectin 1a (6). Full article

(This article belongs to the Special Issue MS- or NMR-Guided Discovery of Marine Specialized Metabolites)

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13 pages, 1563 KiB

Open AccessArticle

New Naphthalene Derivatives from the Mangrove Endophytic Fungus Daldinia eschscholzii MCZ-18

by Zhiyong Xu, Ting Feng, Zhenchang Wen, Qing Li, Biting Chen, Pinghuai Liu and Jing Xu

Mar. Drugs 2024, 22(6), 242; https://doi.org/10.3390/md22060242 - 27 May 2024

Viewed by 318

Abstract

Five new naphthalene derivatives dalesconosides A–D, F (1–4, 6), a known synthetic analogue named dalesconoside E (5), and eighteen known compounds (7–24) were isolated from Daldinia eschscholzii MCZ-18, which is an endophytic [...] Read more.

Five new naphthalene derivatives dalesconosides A–D, F (1–4, 6), a known synthetic analogue named dalesconoside E (5), and eighteen known compounds (7–24) were isolated from Daldinia eschscholzii MCZ-18, which is an endophytic fungus obtained from the Chinese mangrove plant Ceriops tagal. Differing from previously reported naphthalenes, compounds 1 and 2 were bearing a rare ribofuranoside substituted at C-1 and the 5-methyltetrahydrofuran-2,3-diol moiety, respectively. Their structures were determined by detailed nuclear magnetic resonance (NMR) and mass spectroscopic (MS) analyses, while the absolute configurations were established by theoretical electronic circular dichroism (ECD) calculation. Compounds 1, 3, 13–17 and 19 showed broad ranges of antimicrobial spectrum against five indicator test microorganisms (Enterococcus faecalis, Methicillin-resistant Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans); especially, 1, 16 and 17 were most potent. The variations in structure and attendant biological activities provided fresh insights concerning structure−activity relationships for the naphthalene derivatives. Full article

(This article belongs to the Special Issue Bio-Active Products from Mangrove Ecosystems 2.0)

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11 pages, 2658 KiB

Open AccessArticle

Proangiogenic Azaphilones from the Marine-Derived Fungus Neopestalotiopsis sp. HN-1-6

by Ting Feng, Rongxiang Wu, Yufei Wang, Pei Wang, Liman Zhou, Cong Wang and Fandong Kong

Mar. Drugs 2024, 22(6), 241; https://doi.org/10.3390/md22060241 - 26 May 2024

Viewed by 323

Abstract

Developing novel, safe, and efficient proangiogenic drugs is an important approach for the prevention and treatment of cardiovascular diseases. In this study, 4 new compounds, including 3 azaphilones (1–3) and 1 dihydroisocoumarin (4), as well as 13 [...] Read more.

Developing novel, safe, and efficient proangiogenic drugs is an important approach for the prevention and treatment of cardiovascular diseases. In this study, 4 new compounds, including 3 azaphilones (1–3) and 1 dihydroisocoumarin (4), as well as 13 known compounds (5–17), were isolated from the sea-mud-derived fungus Neopestalotiopsis sp. HN-1-6 from the Beibu Gulf of China. The structures of the new compounds were determined by NMR, MS, ECD, and NMR calculations. Compounds 3, 5, and 7 exhibited noteworthy proangiogenic activities in a zebrafish model at a concentration of 40 μM, without displaying cytotoxicity toward five human cell lines. In addition, some compounds demonstrated antibacterial effects against Staphylococcus aureus, Escherichia coli, and Candida albicans, with MIC values ranging from 64 μg/mL to 256 μg/mL. Full article

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

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22 pages, 4634 KiB

Open AccessArticle

Investigation into the Phytochemical Composition, Antioxidant Properties, and In-Vitro Anti-Diabetic Efficacy of Ulva lactuca Extracts

by Safae Ouahabi, Nour Elhouda Daoudi, El Hassania Loukili, Hbika Asmae, Mohammed Merzouki, Mohamed Bnouham, Allal Challioui, Belkheir Hammouti, Marie-Laure Fauconnier, Larbi Rhazi, Alicia Ayerdi Gotor, Flore Depeint and Mohammed Ramdani

Mar. Drugs 2024, 22(6), 240; https://doi.org/10.3390/md22060240 - 25 May 2024

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Abstract

In this research, the chemical compositions of various extracts obtained from Ulva lactuca, a type of green seaweed collected from the Nador lagoon in the northern region of Morocco, were compared. Their antioxidant and anti-diabetic properties were also studied. Using GC–MS technology, [...] Read more.

In this research, the chemical compositions of various extracts obtained from Ulva lactuca, a type of green seaweed collected from the Nador lagoon in the northern region of Morocco, were compared. Their antioxidant and anti-diabetic properties were also studied. Using GC–MS technology, the fatty acid content of the samples was analyzed, revealing that palmitic acid, eicosenoic acid, and linoleic acid were the most abundant unsaturated fatty acids present in all samples. The HPLC analysis indicated that sinapic acid, naringin, rutin, quercetin, cinnamic acid, salicylic acid, apigenin, flavone, and flavanone were the most prevalent phenolic compounds. The aqueous extract obtained by maceration showed high levels of polyphenols and flavonoids, with values of 379.67 ± 0.09 mg GAE/g and 212.11 ± 0.11 mg QE/g, respectively. This extract also exhibited an impressive ability to scavenge DPPH radicals, as indicated by its IC₅₀ value of 0.095 ± 0.12 mg/mL. Additionally, the methanolic extract obtained using the Soxhlet method demonstrated antioxidant properties by preventing β-carotene discoloration, with an IC₅₀ of 0.087 ± 0.14 mg/mL. Results from in-vitro studies showed that extracts from U. lactuca were able to significantly inhibit the enzymatic activity of α-amylase and α-glucosidase. Among the various extracts, methanolic extract (S) has been identified as the most potent inhibitor, exhibiting a statistically similar effect to that of acarbose. Furthermore, molecular docking models were used to evaluate the interaction between the primary phytochemicals found in these extracts and the human pancreatic α-amylase and α-glucosidase enzymes. These findings suggest that U. lactuca extracts contain bioactive substances that are capable of reducing enzyme activity more effectively than the commercially available drug, acarbose. Full article

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

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16 pages, 655 KiB

Open AccessArticle

Occurrence and Exposure Assessment of Lipophilic Shellfish Toxins in the Zhejiang Province, China

by Qin Weng, Ronghua Zhang, Pinggu Wu, Jiang Chen, Xiaodong Pan, Chenyang Zheng, Dong Zhao, Jikai Wang, Hexiang Zhang, Xiaojuan Qi, Junde Han, Zijie Lu and Biao Zhou

Mar. Drugs 2024, 22(6), 239; https://doi.org/10.3390/md22060239 - 24 May 2024

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Abstract

Although lipophilic shellfish toxins (LSTs) pose a significant threat to the health of seafood consumers, their systematic investigation and risk assessment remain scarce. The goals of this study were as follows: (1) analyze LST levels in commercially available shellfish in Zhejiang province, China, [...] Read more.

Although lipophilic shellfish toxins (LSTs) pose a significant threat to the health of seafood consumers, their systematic investigation and risk assessment remain scarce. The goals of this study were as follows: (1) analyze LST levels in commercially available shellfish in Zhejiang province, China, and determine factors influencing LST distribution; (2) assess the acute dietary risk of exposure to LSTs for local consumers during the red tide period; (3) explore potential health risks of LSTs in humans; and (4) study the acute risks of simultaneous dietary exposure to LSTs and paralytic shellfish toxins (PSTs). A total of 546 shellfish samples were collected. LSTs were detected in 89 samples (16.3%) at concentrations below the regulatory limits. Mussels were the main shellfish species contaminated with LSTs. Spatial variations were observed in the yessotoxin group. Acute exposure to LSTs based on multiple scenarios was low. The minimum tolerable exposure durations for LSTs calculated using the mean and the 95th percentile of consumption data were 19.7 and 4.9 years, respectively. Our findings showed that Zhejiang province residents are at a low risk of combined exposure to LSTs and PSTs; however, the risk may be higher for children under 6 years of age in the extreme scenario. Full article

(This article belongs to the Special Issue Emerging Toxins Accumulation in Shellfish)

20 pages, 4397 KiB

Open AccessArticle

Functional Genomics of a Collection of Gammaproteobacteria Isolated from Antarctica

by Michele Giovannini, Walter Vieri, Emanuele Bosi, Christopher Riccardi, Angelina Lo Giudice, Renato Fani, Marco Fondi and Elena Perrin

Mar. Drugs 2024, 22(6), 238; https://doi.org/10.3390/md22060238 - 23 May 2024

Viewed by 374

Abstract

Antarctica, one of the most extreme environments on Earth, hosts diverse microbial communities. These microbes have evolved and adapted to survive in these hostile conditions, but knowledge on the molecular mechanisms underlying this process remains limited. The Italian Collection of Antarctic Bacteria ( [...] Read more.

Antarctica, one of the most extreme environments on Earth, hosts diverse microbial communities. These microbes have evolved and adapted to survive in these hostile conditions, but knowledge on the molecular mechanisms underlying this process remains limited. The Italian Collection of Antarctic Bacteria (Collezione Italiana Batteri Antartici (CIBAN)), managed by the University of Messina, represents a valuable repository of cold-adapted bacterial strains isolated from various Antarctic environments. In this study, we sequenced and analyzed the genomes of 58 marine Gammaproteobacteria strains from the CIBAN collection, which were isolated during Italian expeditions from 1990 to 2005. By employing genome-scale metrics, we taxonomically characterized these strains and assigned them to four distinct genera: Pseudomonas, Pseudoalteromonas, Shewanella, and Psychrobacter. Genome annotation revealed a previously untapped functional potential, including secondary metabolite biosynthetic gene clusters and antibiotic resistance genes. Phylogenomic analyses provided evolutionary insights, while assessment of cold-shock protein presence shed light on adaptation mechanisms. Our study emphasizes the significance of CIBAN as a resource for understanding Antarctic microbial life and its biotechnological potential. The genomic data unveil new horizons for insight into bacterial existence in Antarctica. Full article

(This article belongs to the Special Issue Polar Marine Bacteria: From Physiology to Biotechnological Applications)

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10 pages, 602 KiB

Open AccessArticle

New Secondary Metabolites from Marine-Derived Fungus Talaromyces minnesotensis BTBU20220184

by Weiliang Wang, Jingjing Wang, Fuhang Song, Renming Jia, Long Wang, Xiuli Xu and Na Yang

Mar. Drugs 2024, 22(6), 237; https://doi.org/10.3390/md22060237 - 23 May 2024

Viewed by 446

Abstract

Six new compounds, talamitones A and B (1 and 2), demethyltalamitone B (3), talamiisocoumaringlycosides A and B (4 and 5), and talaminaphtholglycoside (6), together with six known compounds (7–12), were isolated [...] Read more.

Six new compounds, talamitones A and B (1 and 2), demethyltalamitone B (3), talamiisocoumaringlycosides A and B (4 and 5), and talaminaphtholglycoside (6), together with six known compounds (7–12), were isolated from the marine-derived fungus Talaromyces minnesotensis BTBU20220184. The new structures were characterized by using HRESIMS and NMR. This is the first report of isocoumaringlycoside derivatives from a fungus of the Talaromyces genus. Compounds 5, 6, and 9 showed synergistic antibacterial activity against Staphylococcus aureus. Full article

(This article belongs to the Special Issue Bioactive Secondary Metabolites of Marine Fungi 2.0)

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11 pages, 1768 KiB

Open AccessArticle

Genomics- and Transcriptomics-Guided Discovery of Clavatols from Arctic Fungi Penicillium sp. MYA5

by Yuan-Yuan Sun, Bo Hu, Hao-Bing Yu, Jing Zhou, Xian-Chao Meng, Zhe Ning, Jin-Feng Ding, Ming-Hui Cui and Xiao-Yu Liu

Mar. Drugs 2024, 22(6), 236; https://doi.org/10.3390/md22060236 - 22 May 2024

Viewed by 411

Abstract

Clavatols exhibit a wide range of biological activities due to their diverse structures. A genome mining strategy identified an A5cla cluster from Penicillium sp. MYA5, derived from the Arctic plant Dryas octopetala, is responsible for clavatol biosynthesis. Seven clavatols, including one new [...] Read more.

Clavatols exhibit a wide range of biological activities due to their diverse structures. A genome mining strategy identified an A5cla cluster from Penicillium sp. MYA5, derived from the Arctic plant Dryas octopetala, is responsible for clavatol biosynthesis. Seven clavatols, including one new clavatol derivate named penicophenone F (1) and six known clavatols (2–7), were isolated from Penicillium sp. MYA5 using a transcriptome mining strategy. These structures were elucidated by comprehensive spectroscopic analysis. Antibacterial, aldose reductase inhibition, and siderophore-producing ability assays were conducted on compounds 1–7. Compounds 1 and 2 demonstrated inhibitory effects on the ALR2 enzyme with inhibition rates of 75.3% and 71.6% at a concentration of 10 μM, respectively. Compound 6 exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC values of 4.0 μg/mL and 4.0 μg/mL, respectively. Additionally, compounds 1, 5, and 6 also showed potential iron-binding ability. Full article

(This article belongs to the Special Issue Bioinformatics of Marine Natural Products 3.0)

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15 pages, 4979 KiB

Open AccessArticle

Methanolic Extract and Brominated Compound from the Brazilian Marine Sponge Aplysina fulva Are Neuroprotective and Modulate Inflammatory Profile of Microglia

by Catarina de Jesus Nunes, Cinthia Cristina Santos, Erica Novaes Soares, Irlã Santos Lima, Uesley Vieira Alves, Emílio Lanna, Ronan Batista, Ravena Pereira do Nascimento and Silvia Lima Costa

Mar. Drugs 2024, 22(6), 235; https://doi.org/10.3390/md22060235 - 22 May 2024

Viewed by 440

Abstract

Neurodegenerative diseases involve neuroinflammation and a loss of neurons, leading to disability and death. Hence, the research into new therapies has been focused on the modulation of the inflammatory response mainly by microglia/macrophages. The extracts and metabolites of marine sponges have been presented [...] Read more.

Neurodegenerative diseases involve neuroinflammation and a loss of neurons, leading to disability and death. Hence, the research into new therapies has been focused on the modulation of the inflammatory response mainly by microglia/macrophages. The extracts and metabolites of marine sponges have been presented as anti-inflammatory. This study evaluated the toxicity of an extract and purified compound from the Brazilian marine sponge Aplysina fulva as well as its neuroprotection against inflammatory damage associated with the modulation of microglia response. PC12 neuronal cells and neonatal rat microglia were treated with the methanolic extract of A. fulva (AF-MeOH, 0.1–200 μg/mL) or with its purified dimethyl ketal of 3,5-dibromoverongiaquinol (AF-H1, 0.1–100 μM). Cytotoxicity was determined by MTT tetrazolium, Trypan blue, and propidium iodide; microglia were also treated with the conditioned medium (CM) from PC12 cells in different conditions. The microglia phenotype was determined by the expression of Iba-1 and CD68. AF-MeOH and AF-H1 were not toxic to PC12 or the microglia. Inflammatory damage with Escherichia coli lipopolysaccharide (LPS, 5 μg/mL) was not observed in the PC12 cells treated with AF-MeOH (1–10 μg/mL) or AF-H1 (1–10 μM). Microglia subjected to the CM from PC12 cells treated with LPS and AF-MeOH or AF-H1 showed the control phenotype-like (multipolar, low-CD68), highlighting the anti-neuroinflammatory and neuroprotective effect of components of this marine sponge. Full article

(This article belongs to the Special Issue Bio-Active Components from Marine Sponges)

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15 pages, 3940 KiB

Open AccessArticle

Immunostimulatory Effects of Korean Mineral-Rich Seawaters on Cyclophosphamide-Induced Immunosuppression in Mice

by Choong-Gon Kim, Jae Ho Choi, Sae-Kwang Ku and Chang-Hyun Song

Mar. Drugs 2024, 22(6), 234; https://doi.org/10.3390/md22060234 - 21 May 2024

Viewed by 382

Abstract

Deep seawater (DS), obtained from a depth over 200 m, has health benefits due to its rich nutrients and minerals, and intake of DS has shown diverse immunomodulatory effects in allergies and cancer. Therefore, the immunostimulatory effects of Korean mineral-rich seawaters were examined [...] Read more.

Deep seawater (DS), obtained from a depth over 200 m, has health benefits due to its rich nutrients and minerals, and intake of DS has shown diverse immunomodulatory effects in allergies and cancer. Therefore, the immunostimulatory effects of Korean mineral-rich seawaters were examined in a cyclophosphamide (CPA)-induced immunosuppression model. Three samples of Korean seawater, namely DS from the East Sea off the coasts of Pohang (PDS) and Uljin (UDS), and seawater from the West Sea off the coast of Boryeong (BS), were collected. The seawaters were abundant in several minerals (calcium, iron, zinc, selenium, etc.). Mice were orally administered the seawaters for 42 days, followed by CPA-induced immunosuppression. The CPA induction reduced the weight of the spleen and lymph nodes; however, the administration of seawaters increased the weight of the lymphoid organs, accompanied by stimulation of natural killer cells’ activity and NF-kB-mediated cytokine production (IFNγ, TNFα, IL1β, IL6, and IL12). The mouse-derived splenocytes showed lymphoproliferation without cytotoxicity in the seawater groups. Histopathological analysis revealed that the seawaters improved the CPA-induced atrophic changes by promoting lymphoproliferation in the spleen and lymph nodes. These results provide useful information for the use of Korean mineral-rich seawaters, particularly PDS and UDS, as alternative immunostimulants under immunosuppressive conditions. Full article

(This article belongs to the Special Issue Marine Drug Research in Korea II)

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Mar. Drugs, Volume 22, Issue 6 (June 2024) – 26 articles

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