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Marine Drugs
Special Issues
Therapeutic Potential of Marine Polyphenols
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Therapeutic Potential of Marine Polyphenols

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Marine Pharmacology".

Deadline for manuscript submissions: 30 April 2024 | Viewed by 9563

Special Issue Editors

Dr. Hyeon-Cheol Shin

E-Mail Website
Guest Editor
Center for Molecular Intelligence, The State University of New York, Incheon, Republic of Korea
Interests: phloroglucinol oligomers; phlorotrannins; eckols; pharmcology; anti-neurodegeneration; anti-aging; chemical synthesis
Dr. Bong Ho Lee

E-Mail Website
Guest Editor
Department of Chemical and Biological Engineering, Hanbat National University, Dongseodaero 125, Yuseong‐gu, Daejeon 305‐719, Republic of Korea
Interests: natural product isolation; characterization; bioactivity; Alzheimer drug screening
Dr. Hye Jeong Hwang

E-Mail Website
Guest Editor
Center for Molecular Intelligence, The State University of New York, Korea, 119 Songdomunhwa-ro, Yeonsu-gu, Incheon 21985, Republic of Korea
Interests: anti-cancer; chemo-sensitizer; eckols; chemoprevention; bioactivity; phlorotannins

Special Issue Information

Dear Colleagues,

Polyphenols, which are widely found in plants and well-known for their various physiological effects, exist in a variety of molecular classes. Among them, “marine polyphenols”, which are produced as second metabolites of marine algae, have recently gained attention from the health-care industry. In general, marine polyphenols can be chemically defined as oligomers of phloroglucinol. During the past two decades, scientists have accumulated a large body of in vitro and in vivo evidence that motivates their therapeutic applications in many areas of intractable diseases, including neurodegenerative diseases, cancers, and viral diseases, as well as many other chronic degenerative diseases. Furthermore, the structural nature of marine polyphenols provides unlimited possibility of chemical modifications that may be useful in drug development. In order to exploit such potential and develop them as competitive drugs, research efforts focused on pharmacologically and pharmaceutically relevant information are required.

The aim of this Special Issue is to gather new information regarding the in-depth understanding of pharmacologically and pharmaceutically relevant aspects of marine polyphenols. Scientists who work in the study of marine polyphenols focusing on physicochemical characterizations, synthetic derivatives, bioactivities in general, molecular targets, mechanisms of action, and pharmacology in general are highly welcome to contribute research articles and reviews.

Dr. Hyeon-Cheol Shin
Dr. Bong Ho Lee
Dr. Hye Jeong Hwang
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Marine Drugs is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • phloroglucinol oligomer
  • eckols
  • physicochemical characterization
  • synthetic derivatives
  • bioactivity
  • molecular target
  • mechanism of action
  • pharmacology
  • ADME
  • phlorotannin

Published Papers (5 papers)

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Research

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18 pages, 7241 KiB  
Article
Investigating the Potential Anti-Alzheimer’s Disease Mechanism of Marine Polyphenols: Insights from Network Pharmacology and Molecular Docking
by Kumju Youn, Chi-Tang Ho and Mira Jun
Mar. Drugs 2023, 21(11), 580; https://doi.org/10.3390/md21110580 - 06 Nov 2023
Viewed by 1916
Abstract
Marine polyphenols, including eckol(EK), dieckol(DK), and 8,8’-bieckol(BK), have attracted attention as bioactive ingredients for preventing Alzheimer’s disease (AD). Since AD is a multifactorial disorder, the present study aims to provide an unbiased elucidation of unexplored targets of AD mechanisms and a systematic prediction [...] Read more.
Marine polyphenols, including eckol(EK), dieckol(DK), and 8,8’-bieckol(BK), have attracted attention as bioactive ingredients for preventing Alzheimer’s disease (AD). Since AD is a multifactorial disorder, the present study aims to provide an unbiased elucidation of unexplored targets of AD mechanisms and a systematic prediction of effective preventive combinations of marine polyphenols. Based on the omics data between each compound and AD, a protein–protein interaction (PPI) network was constructed to predict potential hub genes. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analyses were performed to provide further biological insights. In the PPI network of the top 10 hub genes, AKT1, SRC, EGFR, and ESR1 were common targets of EK and BK, whereas PTGS2 was a common target of DK and BK. GO and KEGG pathway analysis revealed that the overlapped genes between each compound and AD were mainly enriched in EGFR tyrosine kinase inhibitor resistance, the MAPK pathway, and the Rap1 and Ras pathways. Finally, docking validation showed stable binding between marine polyphenols and their top hub gene via the lowest binding energy and multiple interactions. The results expanded potential mechanisms and novel targets for AD, and also provided a system-level insight into the molecular targets of marine polyphenols against AD. Full article
(This article belongs to the Special Issue Therapeutic Potential of Marine Polyphenols)
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16 pages, 2888 KiB  
Article
Suppression of Pro-Inflammatory M1 Polarization of LPS-Stimulated RAW 264.7 Macrophage Cells by Fucoxanthin-Rich Sargassum hemiphyllum
by Seungjin Jeong, Mi-Bo Kim, Suhyeon Baek, Joowon Lee, Hyeju Lee, Bei Cao, Yongeun Kim, Lei Cao and Sanggil Lee
Mar. Drugs 2023, 21(10), 533; https://doi.org/10.3390/md21100533 - 12 Oct 2023
Cited by 1 | Viewed by 1538
Abstract
Macrophages play an important role in managing the onset and progression of chronic inflammatory diseases. The primary objective of this study is to explore the antioxidant potential and anti-inflammatory properties of Sargassum hemiphyllum ethanol extract (SHE) and its fraction. SHE and its five [...] Read more.
Macrophages play an important role in managing the onset and progression of chronic inflammatory diseases. The primary objective of this study is to explore the antioxidant potential and anti-inflammatory properties of Sargassum hemiphyllum ethanol extract (SHE) and its fraction. SHE and its five constituent fractions were assessed for overall antioxidant capabilities and inhibitory effects on LPS-induced inflammation by modulating macrophages polarization in both RAW 264.7 macrophages and bone-marrow-derived macrophages (BMDM). Among the organic solvent fractions of SHE, the ethyl acetate fraction displayed the highest total phenolic content and total antioxidant capacity. Notably, the n-hexane (Hex) fraction showed the most substantial suppression of LPS-induced tumor necrosis factor α secretion in BMDM among the five fractions of SHE. The SHE and Hex fraction significantly reduced the heightened expression of pro-inflammatory cytokines and inflammation-inducible enzymes induced by LPS in RAW 264.7 macrophages. In particular, the SHE and Hex fraction inhibited M1 macrophage polarization by reducing the mRNA expression of M1 macrophage markers in macrophages that were polarized toward the M1 phenotype. Furthermore, the SHE and Hex fraction attenuated the induction in nuclear factor E2-related factor 2 and its target genes, which was accompanied by an alteration in antioxidant gene expression in M1-polarized BMDM. The findings suggest that both SHE and its Hex fraction exhibit inhibitory effects on LPS-triggered inflammation and oxidative stress by modulating the polarization of M1 macrophages within macrophage populations. Full article
(This article belongs to the Special Issue Therapeutic Potential of Marine Polyphenols)
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12 pages, 9119 KiB  
Article
Protective Effect and Mechanisms of Eckol on Chronic Ulcerative Colitis Induced by Dextran Sulfate Sodium in Mice
by Mengfan Liao, Songyi Wei, Xianmin Hu, Juan Liu and Jun Wang
Mar. Drugs 2023, 21(7), 376; https://doi.org/10.3390/md21070376 - 25 Jun 2023
Cited by 1 | Viewed by 1541
Abstract
The use of functional foods and their bioactive components is receiving increasing attention as a complementary and alternative therapy for chronic ulcerative colitis (UC). This study explored the protective effect and mechanisms of Eckol, a seaweed-derived bioactive phlorotannin, on the dextran sodium sulfate [...] Read more.
The use of functional foods and their bioactive components is receiving increasing attention as a complementary and alternative therapy for chronic ulcerative colitis (UC). This study explored the protective effect and mechanisms of Eckol, a seaweed-derived bioactive phlorotannin, on the dextran sodium sulfate (DSS)-induced chronic UC in mice. Eckol (0.5–1.0 mg/kg) reduced DSS-enhanced disease activity indexes, and alleviated the shortening of colon length and colonic tissue damage in chronic UC mice. The contents of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 were significantly decreased, and the level of anti-inflammatory IL-10 was enhanced in the serum and colonic tissues collected from Eckol-treated mice compared with the DSS controls. Eckol administration significantly reduced the number of apoptotic cells and the expression of cleaved Caspase-3, and increased the B-cell lymphoma-2 (Bcl-2)/B-cell lymphoma-2- associated X (Bax) ratio in DSS-challenged colons. There were more cluster of differentiation (CD)11c+ dendritic cells and CD8+ T cells, and less CD4+ T cells infiltrated to inflamed colonic tissues in the Eckol-treated groups. Expression of colonic Toll-like receptor 4 (TLR4), nuclear factor kappa-B (NF-κB) p65, phosphorylated-signal transducer and activator of transcription (pSTAT)3 was significantly down-regulated by Eckol compared with the DSS-challenged group. In conclusion, our data suggest that Eckol appeared to be a potential functional food ingredient for protection against chronic UC. The anti-colitis mechanisms of Eckol might be attributed to the down-regulation of the TLR4/NF-κB/STAT3 pathway, inhibition of inflammation and apoptosis, as well as its immunoregulatory activity. Full article
(This article belongs to the Special Issue Therapeutic Potential of Marine Polyphenols)
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Review

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24 pages, 1518 KiB  
Review
Marine Algal Polyphenols as Skin Protective Agents: Current Status and Future Prospectives
by H.H.A.C.K. Jayawardhana, Thilina U. Jayawardena, K.K.A. Sanjeewa, N.M. Liyanage, D.P. Nagahawatta, Hyo-Geun Lee, Jae-Il Kim and You-Jin Jeon
Mar. Drugs 2023, 21(5), 285; https://doi.org/10.3390/md21050285 - 30 Apr 2023
Cited by 2 | Viewed by 2230
Abstract
The skin is the outermost anatomical barrier, which plays a vital role in the maintenance of internal homeostasis and protection against physical, chemical, and biological detractors. Direct contact with various stimuli leads to several physiological changes that are ultimately important for the growth [...] Read more.
The skin is the outermost anatomical barrier, which plays a vital role in the maintenance of internal homeostasis and protection against physical, chemical, and biological detractors. Direct contact with various stimuli leads to several physiological changes that are ultimately important for the growth of the cosmetic industry. Due to the consequences of using synthetic compounds in skincare and cosmeceutical-related industries, the pharmaceutical and scientific communities have recently shifted their focus to natural ingredients. The nutrient-rich value of algae, which are some of the most interesting organisms in marine ecosystems, has attracted attention. Secondary metabolites isolated from seaweeds are potential candidates for a wide range of economic applications, including food, pharmaceuticals, and cosmetics. An increasing number of studies have focused on polyphenol compounds owing to their promising biological activities against oxidation, inflammation, allergies, cancers, melanogenesis, aging, and wrinkles. This review summarizes the potential evidence of the beneficial properties and future perspectives of using marine macroalgae-derived polyphenolic compounds for advancing the cosmetic industry. Full article
(This article belongs to the Special Issue Therapeutic Potential of Marine Polyphenols)
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18 pages, 1370 KiB  
Review
Marine Macroalgae Polyphenols as Potential Neuroprotective Antioxidants in Neurodegenerative Diseases
by Silvia Lomartire and Ana M. M. Gonçalves
Mar. Drugs 2023, 21(5), 261; https://doi.org/10.3390/md21050261 - 23 Apr 2023
Cited by 12 | Viewed by 1812
Abstract
Polyphenols are beneficial natural compounds with antioxidant properties that have recently gain a lot of interest for their potential therapeutic applications. Marine polyphenols derived from marine macroalgae have been discovered to possess interesting antioxidant properties; therefore, these compounds can be included in several [...] Read more.
Polyphenols are beneficial natural compounds with antioxidant properties that have recently gain a lot of interest for their potential therapeutic applications. Marine polyphenols derived from marine macroalgae have been discovered to possess interesting antioxidant properties; therefore, these compounds can be included in several areas of drug development. Authors have considered the use of polyphenol extracts from seaweeds as neuroprotective antioxidants in neurodegenerative diseases. Marine polyphenols may slow the progression and limit neuronal cell loss due to their antioxidant activity; therefore, the use of these natural compounds would improve the quality of life for patients affected with neurodegenerative diseases. Marine polyphenols have distinct characteristics and potential. Among seaweeds, brown algae are the main sources of polyphenols, and present the highest antioxidant activity in comparison to red algae and green algae. The present paper collects the most recent in vitro and in vivo evidence from investigations regarding polyphenols extracted from seaweeds that exhibit neuroprotective antioxidant activity. Throughout the review, oxidative stress in neurodegeneration and the mechanism of action of marine polyphenol antioxidant activity are discussed to evidence the potential of algal polyphenols for future use in drug development to delay cell loss in patients with neurodegenerative disorders. Full article
(This article belongs to the Special Issue Therapeutic Potential of Marine Polyphenols)
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