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Marine Drugs
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Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0
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Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0

A special issue of Marine Drugs (ISSN 1660-3397).

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 47246

Special Issue Editor

Dr. Diana Cláudia Pinto

E-Mail Website
Guest Editor
LAQV-REQUIMTE, Department of Chemistry, Universidade de Aveiro, 3810-193 Aveiro, Portugal
Interests: organic chemistry; medicinal chemistry; biotransformations; natural products; plant chemical profile; sustainable chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Although the use of seaweeds in gastronomy is increasing, in many countries, they are still considered unconventional food plants. Scientific evidence of their nutritional value and their health benefits is still needed and numerous researchers are dedicated to establishing the health and nutritional potential of seaweeds. Moreover, scientific research has gone further and, recently, efforts to establish the relationship between the secondary metabolites of seaweeds and health and nutritional effects have been explored.

The Special Issue "Seaweeds Secondary Metabolites: Successes in and/or Probable Therapeutic Applications” has been a success and we think that more interesting results are being achieved; therefore, a second Special Issue of Marine Drugs dedicated to this subject, seems to be essential. The Special Issue "Seaweeds Secondary Metabolites: Successes in and/or Probable Therapeutic Applications 2.0” welcomes high-quality manuscripts exploring bioactive compounds from seaweeds and their therapeutic applications.

As Guest Editor, I invite scientists to submit their latest research findings and review articles in this area and contribute interesting papers with significant advances in this field to this Special Issue of Marine Drugs.

Prof. Dr. Diana Cláudia Pinto
Guest Editor

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

  • Seaweeds
  • Secondary Metabolites
  • Biological Activities
  • Algae
  • Nutritional Supplements
  • Polysaccharides
  • Antioxidants
  • Fucoidan
  • Drug delivery

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Published Papers (10 papers)

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Research

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25 pages, 2401 KiB  
Article
The Remarkable Antioxidant and Anti-Inflammatory Potential of the Extracts of the Brown Alga Cystoseira amentacea var. stricta
by Gina De La Fuente, Marco Fontana, Valentina Asnaghi, Mariachiara Chiantore, Serena Mirata, Annalisa Salis, Gianluca Damonte and Sonia Scarfì
Mar. Drugs 2021, 19(1), 2; https://doi.org/10.3390/md19010002 - 23 Dec 2020
Cited by 30 | Viewed by 3995
Abstract
Inflammation and oxidative stress are part of the complex biological responses of body tissues to harmful stimuli. In recent years, due to the increased understanding that oxidative stress is implicated in several diseases, pharmaceutical industries have invested in the research and development of [...] Read more.
Inflammation and oxidative stress are part of the complex biological responses of body tissues to harmful stimuli. In recent years, due to the increased understanding that oxidative stress is implicated in several diseases, pharmaceutical industries have invested in the research and development of new antioxidant compounds, especially from marine environment sources. Marine seaweeds have shown the presence of many bioactive secondary metabolites, with great potentialities from both the nutraceutical and the biomedical point of view. In this study, 50%-ethanolic and DMSO extracts from the species C. amentacea var. stricta were obtained for the first time from seaweeds collected in the Ligurian Sea (north-western Mediterranean). The bioactive properties of these extracts were then investigated, in terms of quantification of specific antioxidant activities by relevant ROS scavenging spectrophotometric tests, and of anti-inflammatory properties in LPS-stimulated macrophages by evaluation of inhibition of inflammatory cytokines and mediators. The data obtained in this study demonstrate a strong anti-inflammatory effect of both C. amentacea extracts (DMSO and ethanolic). The extracts showed a very low grade of toxicity on RAW 264.7 macrophages and L929 fibroblasts and a plethora of antioxidant and anti-inflammatory effects that were for the first time thoroughly investigated. The two extracts were able to scavenge OH and NO radicals (OH EC50 between 392 and 454 μg/mL; NO EC50 between 546 and 1293 μg/mL), to partially rescue H2O2-induced RAW 264.7 macrophages cell death, to abate intracellular ROS production in H2O2-stimulated macrophages and fibroblasts and to strongly inhibit LPS-induced inflammatory mediators, such as NO production and IL-1α, IL-6, cyclooxygenase-2 and inducible NO synthase gene expression in RAW 264.7 macrophages. These results pave the way, for the future use of C. amentacea metabolites, as an example, as antioxidant food additives in antiaging formulations as well as in cosmetic lenitive lotions for inflamed and/or damaged skin. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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12 pages, 2870 KiB  
Article
Polysaccharide from Codium fragile Induces Anti-Cancer Immunity by Activating Natural Killer Cells
by Hae-Bin Park, Juyoung Hwang, Wei Zhang, Seulgi Go, Jihoe Kim, Inho Choi, SangGuan You and Jun-O Jin
Mar. Drugs 2020, 18(12), 626; https://doi.org/10.3390/md18120626 - 8 Dec 2020
Cited by 27 | Viewed by 3550
Abstract
Natural polysaccharides exhibit beneficial immune modulatory effects, including immune stimulatory and anti-cancer activities. In this study, we examined the effect of Codium fragile polysaccharide (CFP) on natural killer (NK) cell activation, and its effect on tumor-bearing mice. Intravenous CFP treatment of C57BL/6 mice [...] Read more.
Natural polysaccharides exhibit beneficial immune modulatory effects, including immune stimulatory and anti-cancer activities. In this study, we examined the effect of Codium fragile polysaccharide (CFP) on natural killer (NK) cell activation, and its effect on tumor-bearing mice. Intravenous CFP treatment of C57BL/6 mice resulted in the upregulation of CD69, which is a marker associated with NK cell activation. In addition, intracellular levels of interferon (IFN)-γ and the cytotoxic mediators perforin and granzyme B were markedly increased in response to the CFP treatment of splenic NK cells. IFN-γ production by NK cells was directly induced by CFP, whereas the upregulation of CD69 and cytotoxic mediators required IL-12. Finally, intraperitoneal treatment with CFP prevented CT-26 (murine carcinoma) tumor cell infiltration in the lungs, without significantly reducing the body weight. In addition, treatment with CFP prevented B16 melanoma cell infiltration in the lung of C57BL/6 mice. Moreover, the anti-tumor effect was diminished by the depletion of NK cells. Therefore, these data suggest that CFP may be used as an NK cell stimulator to produce a phenomenon that contributes to anti-cancer immunity. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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17 pages, 7573 KiB  
Article
Fucoidan Isolated from Saccharina japonica Inhibits LPS-Induced Inflammation in Macrophages via Blocking NF-κB, MAPK and JAK-STAT Pathways
by Jing Ye, Donghui Chen, Zhicheng Ye, Yayan Huang, Na Zhang, Edmund M. K. Lui, Changhu Xue and Meitian Xiao
Mar. Drugs 2020, 18(6), 328; https://doi.org/10.3390/md18060328 - 24 Jun 2020
Cited by 40 | Viewed by 4112
Abstract
Fucoidan has been reported to have a variety of biological activities. However, different algae species, extraction methods, harvesting seasons, and growth regions lead to the structural variation of fucoidan, which would affect the bioactivities of fucoidan. To date, the anti-inflammatory properties and the [...] Read more.
Fucoidan has been reported to have a variety of biological activities. However, different algae species, extraction methods, harvesting seasons, and growth regions lead to the structural variation of fucoidan, which would affect the bioactivities of fucoidan. To date, the anti-inflammatory properties and the underlying mechanism of fucoidan from brown alga Saccharina japonica (S. japonica) remain limited. The aims of the present study were to investigate the structure, the anti-inflammatory properties, and the potential molecular mechanisms of fucoidan isolated from S. japonica (SF6) against lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. SF6 was characterized using high performance liquid gel permeation chromatography (HPGPC), Fourier transform infrared spectroscopy (FTIR), and nuclear magnetic resonance spectroscopy (NMR), and observed to be rich in fucose, galactose, and sulfate. Additionally, results showed that SF6 remarkably inhibited LPS-induced production of various inflammatory mediators and pro-inflammation cytokines, including nitric oxide (NO), NO synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis factor-α (TNF-α), interleukin-β (IL-β), and interleukin-6 (IL-6). A mechanism study showed that SF6 could effectively inhibit inflammatory responses through blocking LPS-induced inflammation pathways, including nuclear factor-κB (NF-κB), mitogen-activated protein kinase (MAPK), and Janus kinase (JAK)-2 and signal transducer and activator of transcription (STAT)-1/3 pathways. These results suggested that SF6 has the potential to be developed as an anti-inflammatory agent applied in functional food. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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16 pages, 1177 KiB  
Article
In Vitro Enzyme Inhibitory Properties, Secondary Metabolite Profiles and Multivariate Analysis of Five Seaweeds
by Mohamad Fawzi Mahomoodally, Nabeelah Bibi Sadeer, Gokhan Zengin, Zoltán Cziáky, József Jekő, Alina Diuzheva, Kouadio Ibrahime Sinan, Kishneth Palaniveloo, Doo Hwan Kim and Kannan R. R. Rengasamy
Mar. Drugs 2020, 18(4), 198; https://doi.org/10.3390/md18040198 - 8 Apr 2020
Cited by 11 | Viewed by 3372
Abstract
Seaweeds have been exploited as both food products and therapeutics to manage human ailments for centuries. This study investigated the metabolite profile of five seaweeds (Halimeda spp., Spyridia hypnoides (Bory de Saint-Vincent) Papenfuss, Valoniopsis pachynema (G. Martens) Børgesen, Gracilaria fergusonii J. Agardh [...] Read more.
Seaweeds have been exploited as both food products and therapeutics to manage human ailments for centuries. This study investigated the metabolite profile of five seaweeds (Halimeda spp., Spyridia hypnoides (Bory de Saint-Vincent) Papenfuss, Valoniopsis pachynema (G. Martens) Børgesen, Gracilaria fergusonii J. Agardh and Amphiroa anceps (Lamarck) Decaisne using ultra-high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (UHPLC-ESI-MS/MS). Furthermore, these seaweeds were assessed for antioxidant and inhibitory effects against α-amylase, α-glucosidase, acetyl-cholinesterase (AChE), butyryl-cholinesterase (BChE) and tyrosinase. Valoniopsis pachynema and A. anceps yielded the highest flavonoid (4.30 ± 0.29 mg RE/g) and phenolic content (7.83 ± 0.08 mg RE/g), respectively. Additionally, A. anceps exhibited significant antioxidant properties with all assays and significantly depressed BChE (IC50 = 6.68 ± 0.83 mg/mL) and α-amylase activities (IC50 = 5.34 ± 0.14 mg/mL). Interestingly, the five seaweeds revealed potent inhibitory effects against tyrosinase activity. In conclusion, A. anceps might be considered as a key source of phytoantioxidants and a potential candidate to develop nutritional supplements. Besides, the five tested seaweeds warrant further study and may be exploited as promising natural sources for managing hyperpigmentation. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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18 pages, 8299 KiB  
Article
Laminarin-Derived from Brown Algae Suppresses the Growth of Ovarian Cancer Cells via Mitochondrial Dysfunction and ER Stress
by Hyocheol Bae, Gwonhwa Song, Jin-Young Lee, Taeyeon Hong, Moon-Jeong Chang and Whasun Lim
Mar. Drugs 2020, 18(3), 152; https://doi.org/10.3390/md18030152 - 9 Mar 2020
Cited by 29 | Viewed by 4194
Abstract
Ovarian cancer (OC) is difficult to diagnose at an early stage and leads to the high mortality rate reported in the United States. Standard treatment for OC includes maximal cytoreductive surgery followed by platinum-based chemotherapy. However, relapse due to chemoresistance is common in [...] Read more.
Ovarian cancer (OC) is difficult to diagnose at an early stage and leads to the high mortality rate reported in the United States. Standard treatment for OC includes maximal cytoreductive surgery followed by platinum-based chemotherapy. However, relapse due to chemoresistance is common in advanced OC patients. Therefore, it is necessary to develop new anticancer drugs to suppress OC progression. Recently, the anticancer effects of laminarin, a beta-1,3-glucan derived from brown algae, have been reported in hepatocellular carcinoma, colon cancer, leukemia, and melanoma. However, its effects in OC are not reported. We confirmed that laminarin decreases cell growth and cell cycle progression of OC cells through the regulation of intracellular signaling. Moreover, laminarin induced cell death through DNA fragmentation, reactive oxygen species generation, induction of apoptotic signals and endoplasmic reticulum (ER) stress, regulation of calcium levels, and alteration of the ER-mitochondria axis. Laminarin was not cytotoxic in a zebrafish model, while in a zebrafish xenograft model, it inhibited OC cell growth. These results suggest that laminarin may be successfully used as a novel OC suppressor. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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17 pages, 2628 KiB  
Article
Purification and Evaluation of N-benzyl Cinnamamide from Red Seaweed Gracilaria fisheri as an Inhibitor of Vibrio harveyi AI-2 Quorum Sensing
by Kulwadee Karnjana, Saksit Nobsathian, Chumporn Soowannayan, Wei Zhao, Ya-Jie Tang and Kanokpan Wongprasert
Mar. Drugs 2020, 18(2), 80; https://doi.org/10.3390/md18020080 - 27 Jan 2020
Cited by 19 | Viewed by 4131
Abstract
Previously, we reported that the ethanol extract from red seaweed Gracilaria fisheri effectively decreased biofilm formation of Vibrio harveyi. In this study, the anti-biofilm active compounds in the ethanol extract were isolated and their structures identified. The anti-biofilm fractionation assay for minimum [...] Read more.
Previously, we reported that the ethanol extract from red seaweed Gracilaria fisheri effectively decreased biofilm formation of Vibrio harveyi. In this study, the anti-biofilm active compounds in the ethanol extract were isolated and their structures identified. The anti-biofilm fractionation assay for minimum inhibitory concentration (MIC) produced two fractions which possessed maximal inhibitory activities toward the biofilm formation of V. harveyi strains 1114 and BAA 1116. Following chromatographic separation of the bioactive fractions, two pure compounds were isolated, and their structures were elucidated using FTIR, NMR, and HR-TOF-MS. The compounds were N-benzyl cinnamamide and α-resorcylic acid. The in vitro activity assay demonstrated that both compounds inhibited the biofilm formation of V. harveyi and possessed the anti-quorum sensing activity by interfering with the bioluminescence of the bacteria. However, the N-benzyl cinnamamide was more potent than α-resorcylic acid with a 10-fold lesser MIC. The present study reveals the beneficial property of the N-benzyl cinnamamide from the ethanol extract as a lead anti-microbial drug against V. harveyi. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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16 pages, 3199 KiB  
Article
Inhibitory Effect of Depolymerized Sulfated Galactans from Marine Red Algae on the Growth and Adhesion of Diarrheagenic Escherichia coli
by Yixiang Liu, Wenqiang Liu, Yanbo Wang, Yu Ma, Ling Huang, Chao Zou, Donghui Li, Min-Jie Cao and Guang-Ming Liu
Mar. Drugs 2019, 17(12), 694; https://doi.org/10.3390/md17120694 - 10 Dec 2019
Cited by 22 | Viewed by 3403
Abstract
Active polysaccharides as safe and natural polymers against bacterial diarrhea have been reconsidered as an alternative to antibiotics. This work investigated the inhibiting effect of depolymerized sulfated galactans from Eucheuma serra and Gracilaria verrucosa on the growth and adhesion of diarrheagenic enterotoxigenic Escherichia [...] Read more.
Active polysaccharides as safe and natural polymers against bacterial diarrhea have been reconsidered as an alternative to antibiotics. This work investigated the inhibiting effect of depolymerized sulfated galactans from Eucheuma serra and Gracilaria verrucosa on the growth and adhesion of diarrheagenic enterotoxigenic Escherichia coli (ETEC) K88. Results showed that the sulfated polysaccharides with molecular weight distribution ≤20.0 kDa exhibited antibacterial activity against ETEC K88. A structure–activity study revealed that the anti-ETEC K88 activity of sulfated polysaccharides is strictly determined by their molecular weight distribution, sulfate group content, and monosaccharide composition. In addition, the promoted nucleic acid release and the fluorescence quenching of membrane proteins were observed after the treatment with selected polysaccharides. Scanning electron microscopy further confirmed that the depolymerized sulfated galactans can effectively inhibit ETEC K88 adhesion. In conclusion, depolymerized sulfated galactans exhibited an inhibitory effect on the growth and adhesion of ETEC K88. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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Review

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11 pages, 1439 KiB  
Review
The Application of Seaweed Polysaccharides and Their Derived Products with Potential for the Treatment of Alzheimer’s Disease
by Sarah Bauer, Weihua Jin, Fuming Zhang and Robert J. Linhardt
Mar. Drugs 2021, 19(2), 89; https://doi.org/10.3390/md19020089 - 4 Feb 2021
Cited by 45 | Viewed by 6419
Abstract
Neurodegenerative diseases are among the most widespread diseases affecting humans, and the number of patients is only rising. Seaweed polysaccharide extracts show significant neuroprotective and reparative activities. Seaweed polysaccharides might provide the next big breakthrough in neurodegenerative disease treatment. This paper reviews the [...] Read more.
Neurodegenerative diseases are among the most widespread diseases affecting humans, and the number of patients is only rising. Seaweed polysaccharide extracts show significant neuroprotective and reparative activities. Seaweed polysaccharides might provide the next big breakthrough in neurodegenerative disease treatment. This paper reviews the applications of seaweed polysaccharides as potential treatments of neurodegenerative diseases. The particular focus is on fucoidan, ulvan, and their derivatives as potential agents to treat Alzheimer’s disease. This review provides a critical update on the progress in this important research area. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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20 pages, 1423 KiB  
Review
Polyphenols from Brown Seaweeds (Ochrophyta, Phaeophyceae): Phlorotannins in the Pursuit of Natural Alternatives to Tackle Neurodegeneration
by Mariana Barbosa, Patrícia Valentão and Paula B. Andrade
Mar. Drugs 2020, 18(12), 654; https://doi.org/10.3390/md18120654 - 18 Dec 2020
Cited by 21 | Viewed by 4503
Abstract
Globally, the burden of neurodegenerative disorders continues to rise, and their multifactorial etiology has been regarded as among the most challenging medical issues. Bioprospecting for seaweed-derived multimodal acting products has earned increasing attention in the fight against neurodegenerative conditions. Phlorotannins (phloroglucinol-based polyphenols exclusively [...] Read more.
Globally, the burden of neurodegenerative disorders continues to rise, and their multifactorial etiology has been regarded as among the most challenging medical issues. Bioprospecting for seaweed-derived multimodal acting products has earned increasing attention in the fight against neurodegenerative conditions. Phlorotannins (phloroglucinol-based polyphenols exclusively produced by brown seaweeds) are amongst the most promising nature-sourced compounds in terms of functionality, and though research on their neuroprotective properties is still in its infancy, phlorotannins have been found to modulate intricate events within the neuronal network. This review comprehensively covers the available literature on the neuroprotective potential of both isolated phlorotannins and phlorotannin-rich extracts/fractions, highlighting the main key findings and pointing to some potential directions for neuro research ramp-up processes on these marine-derived products. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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21 pages, 3495 KiB  
Review
Marine Seaweed Polysaccharides-Based Engineered Cues for the Modern Biomedical Sector
by Muhammad Bilal and Hafiz M. N. Iqbal
Mar. Drugs 2020, 18(1), 7; https://doi.org/10.3390/md18010007 - 19 Dec 2019
Cited by 77 | Viewed by 8599
Abstract
Seaweed-derived polysaccharides with unique structural and functional entities have gained special research attention in the current medical sector. Seaweed polysaccharides have been or being used to engineer novel cues with biomedical values to tackle in practice the limitations of counterparts which have become [...] Read more.
Seaweed-derived polysaccharides with unique structural and functional entities have gained special research attention in the current medical sector. Seaweed polysaccharides have been or being used to engineer novel cues with biomedical values to tackle in practice the limitations of counterparts which have become ineffective for 21st-century settings. The inherited features of seaweed polysaccharides, such as those of a biologically tunable, biocompatible, biodegradable, renewable, and non-toxic nature, urge researchers to use them to design therapeutically effective, efficient, controlled delivery, patient-compliant, and age-compliant drug delivery platforms. Based on their significant retention capabilities, tunable active units, swelling, and colloidal features, seaweed polysaccharides have appeared as highly useful materials for modulating drug-delivery and tissue-engineering systems. This paper presents a standard methodological approach to review the literature using inclusion-exclusion criteria, which is mostly ignored in the reported literature. Following that, numerous marine-based seaweed polysaccharides are discussed with suitable examples. For the applied perspectives, part of the review is focused on the biomedical values, i.e., targeted drug delivery, wound-curative potential, anticancer potentialities, tissue-engineering aspects, and ultraviolet (UV) protectant potential of seaweed polysaccharides based engineered cues. Finally, current challenges, gaps, and future perspectives have been included in this review. Full article
(This article belongs to the Special Issue Seaweeds Secondary Metabolites: Successes In and/or Probable Therapeutic Applications 2.0)
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