Marine Natural Products as Anticancer Agents 2.0

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

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 29299

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Special Issue Editors

MARE - Marine and Environmental Sciences Centre, Polytechnic of Leiria, 2520-630 Peniche, Portugal
Interests: marine natural products; biotechnological applications; pharmaceutical applications; signal transduction; anticancer activities; compounds isolation
Special Issues, Collections and Topics in MDPI journals
Department of Pharmacy, College of Pharmacy, Seoul National University, Building 29 Room 223, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Republic of Korea
Interests: oncology; signal transduction; cell death; inflammation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Despite the advances achieved in cancer biology and therapeutic strategies in recent decades, cancer remains a considerable threat to human health and one of the deadliest diseases worldwide. Therapy failure and consequent cancer relapse are the main factors contributing to the high cancer mortality, making it crucial to find and develop new therapeutic options, including new drugs. Marine natural products have revealed uncommon and rare chemical features not found in the terrestrial environment. The molecular modeling and chemical synthesis of novel anticancer drugs can find inspiration in these compounds. As marine natural products were produced in co-evolution with biological systems, they present greater efficiency and specificity when it comes to interacting with biological target sites (e.g., receptors, DNA, proteins), exhibiting novel mechanisms of action, and modulating distinct intracellular signaling pathways, with fewer side effects.

Based on the success of the Special Issue “Marine Natural Products as Anticancer Agents” (https://www.mdpi.com/journal/marinedrugs/special_issues/AnticancerAgents) as well as the critical relevance of this topic, we are pleased to announce the second edition of this Special Issue.

This Special Issue will highlight the potential of marine natural products as anticancer agents, empathizing the diversity of the molecular targets and the mechanistic effects. The application of innovative scientific approaches, including co-cultures, 3D cultures, organoids, and in vivo applications to avoid the gap between in vitro and in vivo experiments is encouraged. In addition, approaches describing synergistic combination treatments of marine compounds with clinically used or experimental anticancer agents are welcome.

As compounds with anticancer immune-modulatory functions are well known, papers describing the cancer activity of such marine compounds alone or in combination with checkpoint inhibitors or others are encouraged.

For this Special Issue, we invite academic and industry scientists to submit reviews and original and conceptual research articles highlighting the biological activities of known, novel, or derived natural marine compounds with potential anticancer activity.

Dr. Celso Alves
Prof. Dr. Marc Diederich
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

  • anticancer
  • anti-tumor
  • immune
  • molecular targets
  • co-cultures
  • 3D culture models
  • marine natural products
  • receptors
  • proteins
  • molecular modeling
  • chemical synthesis
  • immune-modulatory

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Published Papers (12 papers)

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Editorial

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4 pages, 201 KiB  
Editorial
Marine Natural Products as Anticancer Agents 2.0
by Celso Alves and Marc Diederich
Mar. Drugs 2023, 21(4), 247; https://doi.org/10.3390/md21040247 - 17 Apr 2023
Viewed by 1249
Abstract
Global cancer incidence and death are expected to increase to 28 [...] Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)

Research

Jump to: Editorial, Review

13 pages, 2818 KiB  
Article
7S,15R-Dihydroxy-16S,17S-epoxy-docosapentaenoic Acid Overcomes Chemoresistance of 5-Fluorouracil by Suppressing the Infiltration of Tumor-Associated Macrophages and Inhibiting the Activation of Cancer Stem Cells in a Colorectal Cancer Xenograft Model
by Yan Su, Hack Sun Choi, Jong Hyun Choi, Hee-Sik Kim, Yong-Suk Jang and Jeong-Woo Seo
Mar. Drugs 2023, 21(2), 80; https://doi.org/10.3390/md21020080 - 24 Jan 2023
Cited by 3 | Viewed by 1849
Abstract
Although the tumor bulk is initially reduced by 5-fluorouracil (5-FU), chemoresistance developed due to prolonged chemotherapy in colorectal cancer (CRC). The enrichment of cancer stem cells (CSCs) and the infiltration of tumor-associated macrophages (TAMs) contribute to chemoresistance and poor outcomes. A docosahexaenoic acid [...] Read more.
Although the tumor bulk is initially reduced by 5-fluorouracil (5-FU), chemoresistance developed due to prolonged chemotherapy in colorectal cancer (CRC). The enrichment of cancer stem cells (CSCs) and the infiltration of tumor-associated macrophages (TAMs) contribute to chemoresistance and poor outcomes. A docosahexaenoic acid derivative developed by our group, 7S,15R-dihydroxy-16S,17S-epoxy-docosapentaenoic acid (diHEP-DPA), exerts antitumor effects against TAMs infiltration and CSCs enrichment in our previous study. The current study aimed to investigate whether diHEP-DPA was able to overcome chemoresistance to 5-FU in CRCs, together with the potential synergistic mechanisms in a CT26-BALB/c mouse model. Our results suggested that although 5-FU inhibited tumor growth, 5-FU enriched CSCs via the WNT/β-catenin signaling pathway, resulting in chemoresistance in CRCs. However, we revealed that 5-FU promoted the infiltration of TAMs via the NF-kB signaling pathway and improved epithelial–mesenchymal transition (EMT) via the signal transducer and activator of the transcription 3 (STAT3) signaling pathway; these traits were believed to contribute to CSC activation. Furthermore, supplementation with diHEP-DPA could overcome drug resistance by decreasing the CSCs, suppressing the infiltration of TAMs, and inhibiting EMT progression. Additionally, the combinatorial treatment of diHEP-DPA and 5-FU effectively enhanced phagocytosis by blocking the CD47/signal regulatory protein alpha (SIRPα) axis. These findings present that diHEP-DPA is a potential therapeutic supplement to improve drug outcomes and suppress chemoresistance associated with the current 5-FU-based therapies for colorectal cancer. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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11 pages, 1080 KiB  
Article
Type-I Hemins and Free Porphyrins from a Western Australian Sponge Isabela sp.
by Samuele Sala, Stephen A. Moggach, Gareth L. Nealon, Jane Fromont, Oliver Gomez, Daniel Vuong, Ernest Lacey and Gavin R. Flematti
Mar. Drugs 2023, 21(1), 41; https://doi.org/10.3390/md21010041 - 03 Jan 2023
Cited by 3 | Viewed by 2011
Abstract
Two novel free porphyrins, isabellins A and B, as well as the known compounds corallistin D and deuteroporphyrin IX were isolated from a marine sponge Isabela sp. LC-MS analysis of the crude extract revealed that the natural products were present both as free [...] Read more.
Two novel free porphyrins, isabellins A and B, as well as the known compounds corallistin D and deuteroporphyrin IX were isolated from a marine sponge Isabela sp. LC-MS analysis of the crude extract revealed that the natural products were present both as free porphyrins and iron(III) coordinated hemins, designated isabellihemin A, isabellihemin B, corallistihemin D and deuterohemin IX, respectively. Structures were determined via high-resolution mass spectrometry, UV-Vis spectroscopy and extensive NOESY NMR spectroscopic experiments. The type-I alkyl substitution pattern of isabellin A and isabellihemin A was assigned unambiguously by single crystal X-ray diffraction. Biological evaluation of the metabolites revealed potent cytotoxicity for isabellin A against the NS-1 murine myeloma cell line. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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15 pages, 2358 KiB  
Article
Laminaria japonica Peptides Suppress Liver Cancer by Inducing Apoptosis: Possible Signaling Pathways and Mechanism
by Yingzi Wu, Yuanhui Li, Wenhai Guo, Jie Liu, Weiguo Lao, Penghui Hu, Yiguang Lin and Hongjie Chen
Mar. Drugs 2022, 20(11), 704; https://doi.org/10.3390/md20110704 - 10 Nov 2022
Cited by 2 | Viewed by 1852
Abstract
The anticancer properties of Laminaria japonica peptides (LJPs) have never been studied. Here, we extracted LJPs from fresh seaweed and explored their anti-liver cancer activity (in vivo and in vitro). LJPs were isolated/purified by HPLC-ESI-MS. HepG2 cell apoptosis and cell cycle were evaluated. [...] Read more.
The anticancer properties of Laminaria japonica peptides (LJPs) have never been studied. Here, we extracted LJPs from fresh seaweed and explored their anti-liver cancer activity (in vivo and in vitro). LJPs were isolated/purified by HPLC-ESI-MS. HepG2 cell apoptosis and cell cycle were evaluated. MTT assays were used to examine the cytotoxicity of LJPs. Caspase activation of caspases 3 and 9, cleaved caspases 3 and 9, and cleaved PARP was examined by Western blotting. The PI3K/AKT pathway and the phosphorylation states of MAPKs (p38 and JNK) were examined. We found that the LJP-1 peptide had the most antiproliferative activity in H22 cells in vitro. LJP-1 blocked H22 cells in the G0/G1 phase, accompanied by inhibition of cyclin expression. LJP-1 induced apoptosis through caspase activation and regulation of the ASK1/MAPK pathway. Concurrent in vivo studies demonstrated that LJP-1 significantly inhibited tumor growth and induced tumor cell apoptosis/necrosis. In conclusion, LJPs, particularly LJP-1, exert strong inhibitory effects on liver cancer growth in vivo and in vitro. LJP-1 induces HCC cell apoptosis through the caspase-dependent pathway and G0/G1 arrest. LJP-1 induces caspase-dependent apoptosis, in part by inhibiting PI3K, MAPK signaling pathways, and cell cycle proteins. LJP-1 has the potential to be a novel candidate for human liver cancer therapeutics. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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17 pages, 6255 KiB  
Article
Bromoditerpenes from the Red Seaweed Sphaerococcus coronopifolius as Potential Cytotoxic Agents and Proteasome Inhibitors and Related Mechanisms of Action
by Celso Alves, Joana Silva, Susete Pintéus, Romina A. Guedes, Rita C. Guedes, Rebeca Alvariño, Rafaela Freitas, Márcia I. Goettert, Helena Gaspar, Amparo Alfonso, Maria C. Alpoím, Luis M. Botana and Rui Pedrosa
Mar. Drugs 2022, 20(10), 652; https://doi.org/10.3390/md20100652 - 20 Oct 2022
Cited by 2 | Viewed by 1980
Abstract
Seaweeds are a great source of compounds with cytotoxic properties with the potential to be used as anticancer agents. This study evaluated the cytotoxic and proteasome inhibitory activities of 12R-hydroxy-bromosphaerol, 12S-hydroxy-bromosphaerol, and bromosphaerol isolated from Sphaerococcus coronopifolius. The [...] Read more.
Seaweeds are a great source of compounds with cytotoxic properties with the potential to be used as anticancer agents. This study evaluated the cytotoxic and proteasome inhibitory activities of 12R-hydroxy-bromosphaerol, 12S-hydroxy-bromosphaerol, and bromosphaerol isolated from Sphaerococcus coronopifolius. The cytotoxicity was evaluated on malignant cell lines (A549, CACO-2, HCT-15, MCF-7, NCI-H226, PC-3, SH-SY5Y, and SK-MEL-28) using the MTT and LDH assays. The ability of compounds to stimulate the production of hydrogen peroxide (H2O2) and to induce mitochondrial dysfunction, the externalization of phosphatidylserine, Caspase-9 activity, and changes in nuclear morphology was also studied on MCF-7 cells. The ability to induce DNA damage was also studied on L929 fibroblasts. The proteasome inhibitory activity was estimated through molecular docking studies. The compounds exhibited IC50 values between 15.35 and 53.34 µM. 12R-hydroxy-bromosphaerol and 12S-hydroxy-bromosphaerol increased the H2O2 levels on MCF-7 cells, and bromosphaerol induced DNA damage on fibroblasts. All compounds promoted a depolarization of mitochondrial membrane potential, Caspase-9 activity, and nuclear condensation and fragmentation. The compounds have been shown to interact with the chymotrypsin-like catalytic site through molecular docking studies; however, only 12S-hydroxy-bromosphaerol evidenced interaction with ALA20 and SER169, key residues of the proteasome catalytic mechanism. Further studies should be outlined to deeply characterize and understand the potential of those bromoditerpenes for anticancer therapeutics. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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18 pages, 2814 KiB  
Article
5-O-(N-Boc-l-Alanine)-Renieramycin T Induces Cancer Stem Cell Apoptosis via Targeting Akt Signaling
by Darinthip Suksamai, Satapat Racha, Nicharat Sriratanasak, Chatchai Chaotham, Kanokpol Aphicho, Aye Chan Khine Lin, Chaisak Chansriniyom, Khanit Suwanborirux, Supakarn Chamni and Pithi Chanvorachote
Mar. Drugs 2022, 20(4), 235; https://doi.org/10.3390/md20040235 - 29 Mar 2022
Cited by 11 | Viewed by 3187
Abstract
Cancer stem cells (CSCs) drive aggressiveness and metastasis by utilizing stem cell-related signals. In this study, 5-O-(N-Boc-l-alanine)-renieramycin T (OBA-RT) was demonstrated to suppress CSC signals and induce apoptosis. OBA-RT exerted cytotoxic effects with a half-maximal inhibitory concentration [...] Read more.
Cancer stem cells (CSCs) drive aggressiveness and metastasis by utilizing stem cell-related signals. In this study, 5-O-(N-Boc-l-alanine)-renieramycin T (OBA-RT) was demonstrated to suppress CSC signals and induce apoptosis. OBA-RT exerted cytotoxic effects with a half-maximal inhibitory concentration of approximately 7 µM and mediated apoptosis as detected by annexin V/propidium iodide using flow cytometry and nuclear staining assays. Mechanistically, OBA-RT exerted dual roles, activating p53-dependent apoptosis and concomitantly suppressing CSC signals. A p53-dependent pathway was indicated by the induction of p53 and the depletion of anti-apoptotic Myeloid leukemia 1 (Mcl-1) and B-cell lymphoma 2 (Bcl-2) proteins. Cleaved poly (ADP-ribose) polymerase (Cleaved-PARP) was detected in OBA-RT-treated cells. Interestingly, OBA-RT exerted strong CSC-suppressing activity, reducing the ability to form tumor spheroids. In addition, OBA-RT could induce apoptosis in CSC-rich populations and tumor spheroid collapse. CSC markers, including prominin-1 (CD133), Octamer-binding transcription factor 4 (Oct4), and Nanog Homeobox (Nanog), were notably decreased after OBA-RT treatment. Upstream CSCs regulating active Akt and c-Myc were significantly decreased; indicating that Akt may be a potential target of action. Computational molecular modeling revealed a high-affinity interaction between OBA-RT and an Akt molecule. This study has revealed a novel CSC inhibitory effect of OBA-RT via Akt inhibition, which may improve cancer therapy. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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16 pages, 3479 KiB  
Article
Semi-Synthesis, Cytotoxic Evaluation, and Structure—Activity Relationships of Brefeldin A Derivatives with Antileukemia Activity
by Xu-Xiu Lu, Yao-Yao Jiang, Yan-Wei Wu, Guang-Ying Chen, Chang-Lun Shao, Yu-Cheng Gu, Ming Liu and Mei-Yan Wei
Mar. Drugs 2022, 20(1), 26; https://doi.org/10.3390/md20010026 - 24 Dec 2021
Cited by 7 | Viewed by 2687
Abstract
Brefeldin A (1), a potent cytotoxic natural macrolactone, was produced by the marine fungus Penicillium sp. (HS-N-29) from the medicinal mangrove Acanthus ilicifolius. Series of its ester derivatives 216 were designed and semi-synthesized, and their structures were characterized [...] Read more.
Brefeldin A (1), a potent cytotoxic natural macrolactone, was produced by the marine fungus Penicillium sp. (HS-N-29) from the medicinal mangrove Acanthus ilicifolius. Series of its ester derivatives 216 were designed and semi-synthesized, and their structures were characterized by spectroscopic methods. Their cytotoxic activities were evaluated against human chronic myelogenous leukemia K562 cell line in vitro, and the preliminary structure–activity relationships revealed that the hydroxy group played an important role. Moreover, the monoester derivatives exhibited stronger cytotoxic activity than the diester derivatives. Among them, brefeldin A 7-O-2-chloro-4,5-difluorobenzoate (7) exhibited the strongest inhibitory effect on the proliferation of K562 cells with an IC50 value of 0.84 µM. Further evaluations indicated that 7 induced cell cycle arrest, stimulated cell apoptosis, inhibited phosphorylation of BCR-ABL, and thereby inactivated its downstream AKT signaling pathway. The expression of downstream signaling molecules in the AKT pathway, including mTOR and p70S6K, was also attenuated after 7-treatment in a dose-dependent manner. Furthermore, molecular modeling of 7 docked into 1 binding site of an ARF1–GDP-GEF complex represented well-tolerance. Taken together, 7 had the potential to be served as an effective antileukemia agent or lead compound for further exploration. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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14 pages, 1341 KiB  
Article
Marine Bromophenol Bis(2,3,6-Tribromo-4,5-Dihydroxybenzyl)ether Inhibits Angiogenesis in Human Umbilical Vein Endothelial Cells and Reduces Vasculogenic Mimicry in Human Lung Cancer A549 Cells
by Songtao Dong, Zhongyuan Chen, Li Wang, Yankai Liu, Dimitrios Stagos, Xiukun Lin and Ming Liu
Mar. Drugs 2021, 19(11), 641; https://doi.org/10.3390/md19110641 - 16 Nov 2021
Cited by 6 | Viewed by 2363
Abstract
Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the significant therapies in tumor treatment, while the clinical angiogenesis inhibitors usually [...] Read more.
Angiogenesis, including the growth of new capillary blood vessels from existing ones and the malignant tumors cells formed vasculogenic mimicry, is quite important for the tumor metastasis. Anti-angiogenesis is one of the significant therapies in tumor treatment, while the clinical angiogenesis inhibitors usually exhibit endothelial cells dysfunction and drug resistance. Bis(2,3,6-tribromo-4,5-dihydroxybenzyl)ether (BTDE), a marine algae-derived bromophenol compound, has shown various biological activities, however, its anti-angiogenesis function remains unknown. The present study illustrated that BTDE had anti-angiogenesis effect in vitro through inhibiting human umbilical vein endothelial cells migration, invasion, tube formation, and the activity of matrix metalloproteinases 9 (MMP9), and in vivo BTDE also blocked intersegmental vessel formation in zebrafish embryos. Moreover, BTDE inhibited the migration, invasion, and vasculogenic mimicry formation of lung cancer cell A549. All these results indicated that BTDE could be used as a potential candidate in anti-angiogenesis for the treatment of cancer. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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10 pages, 1380 KiB  
Article
Oxygenated Cembrene Diterpenes from Sarcophyton convolutum: Cytotoxic Sarcoconvolutum A–E
by Tarik A. Mohamed, Abdelsamed I. Elshamy, Asmaa M. Abdel-Tawab, Mona M. AbdelMohsen, Shinji Ohta, Paul W. Pare and Mohamed-Elamir F. Hegazy
Mar. Drugs 2021, 19(9), 519; https://doi.org/10.3390/md19090519 - 13 Sep 2021
Cited by 10 | Viewed by 2519
Abstract
The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (15) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton [...] Read more.
The soft coral genus Sarcophyton contains the enzymatic machinery to synthesize a multitude of cembrene-type diterpenes. Herein, highly oxygenated cembrenoids, sarcoconvolutum A–E (15) were purified and characterized from an ethyl acetate extract of the red sea soft coral, Sarcophyton convolutum. Compounds were assemblies according to spectroscopic methods including FTIR, 1D- and 2D-NMR as well as HRMS. Metabolite cytotoxicity was tested against lung adenocarcinoma, cervical cancer, and oral-cavity carcinoma (A549, HeLa and HSC-2, respectively). The most cytotoxic compound, (4) was observed to be active against cell lines A549 and HSC-2 with IC50 values of 49.70 and 53.17 μM, respectively. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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24 pages, 11895 KiB  
Article
Synthesis and Cytotoxicity Evaluation of Spirocyclic Bromotyrosine Clavatadine C Analogs
by Piyush A. Patel, Tanja Bruun, Polina Ilina, Heidi Mäkkylä, Antti Lempinen, Jari Yli-Kauhaluoma, Päivi Tammela and Paula S. Kiuru
Mar. Drugs 2021, 19(7), 400; https://doi.org/10.3390/md19070400 - 20 Jul 2021
Cited by 4 | Viewed by 2235
Abstract
Marine-originated spirocyclic bromotyrosines are considered as promising scaffolds for new anticancer drugs. In a continuation of our research to develop potent and more selective anticancer compounds, we synthesized a library of 32 spirocyclic clavatadine analogs by replacing the agmatine, i.e., 4-(aminobutyl)guanidine, side chain [...] Read more.
Marine-originated spirocyclic bromotyrosines are considered as promising scaffolds for new anticancer drugs. In a continuation of our research to develop potent and more selective anticancer compounds, we synthesized a library of 32 spirocyclic clavatadine analogs by replacing the agmatine, i.e., 4-(aminobutyl)guanidine, side chain with different substituents. These compounds were tested for cytotoxicity against skin cancer using the human melanoma cell line (A-375) and normal human skin fibroblast cell line (Hs27). The highest cytotoxicity against the A-375 cell line was observed for dichloro compound 18 (CC50 0.4 ± 0.3 µM, selectivity index (SI) 2). The variation of selectivity ranged from SI 0.4 to reach 2.4 for the pyridin-2-yl derivative 29 and hydrazide analog of 2-picoline 37. The structure–activity relationships of the compounds in respect to cytotoxicity and selectivity toward cancer cell lines are discussed. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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Review

Jump to: Editorial, Research

35 pages, 1495 KiB  
Review
Immunopotentiating Activity of Fucoidans and Relevance to Cancer Immunotherapy
by Yani Li, Eileen McGowan, Size Chen, Jerran Santos, Haibin Yin and Yiguang Lin
Mar. Drugs 2023, 21(2), 128; https://doi.org/10.3390/md21020128 - 15 Feb 2023
Cited by 6 | Viewed by 3023
Abstract
Fucoidans, discovered in 1913, are fucose-rich sulfated polysaccharides extracted mainly from brown seaweed. These versatile and nontoxic marine-origin heteropolysaccharides have a wide range of favorable biological activities, including antitumor, immunomodulatory, antiviral, antithrombotic, anticoagulant, antithrombotic, antioxidant, and lipid-lowering activities. In the early 1980s, fucoidans [...] Read more.
Fucoidans, discovered in 1913, are fucose-rich sulfated polysaccharides extracted mainly from brown seaweed. These versatile and nontoxic marine-origin heteropolysaccharides have a wide range of favorable biological activities, including antitumor, immunomodulatory, antiviral, antithrombotic, anticoagulant, antithrombotic, antioxidant, and lipid-lowering activities. In the early 1980s, fucoidans were first recognized for their role in supporting the immune response and later, in the 1990s, their effects on immune potentiation began to emerge. In recent years, the understanding of the immunomodulatory effects of fucoidan has expanded significantly. The ability of fucoidan(s) to activate CTL-mediated cytotoxicity against cancer cells, strong antitumor property, and robust safety profile make fucoidans desirable for effective cancer immunotherapy. This review focusses on current progress and understanding of the immunopotentiation activity of various fucoidans, emphasizing their relevance to cancer immunotherapy. Here, we will discuss the action of fucoidans in different immune cells and review how fucoidans can be used as adjuvants in conjunction with immunotherapeutic products to improve cancer treatment and clinical outcome. Some key rationales for the possible combination of fucoidans with immunotherapy will be discussed. An update is provided on human clinical studies and available registered cancer clinical trials using fucoidans while highlighting future prospects and challenges. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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20 pages, 4299 KiB  
Review
Marine Migrastatics: A Comprehensive 2022 Update
by Marzia Vasarri, Emanuela Barletta and Donatella Degl’Innocenti
Mar. Drugs 2022, 20(5), 273; https://doi.org/10.3390/md20050273 - 19 Apr 2022
Cited by 2 | Viewed by 2450
Abstract
Metastasis is responsible for the bad prognosis in cancer patients. Advances in research on metastasis prevention focus attention on the molecular mechanisms underlying cancer cell motility and invasion to improve therapies for long-term survival in cancer patients. The so-called “migrastatics” could help block [...] Read more.
Metastasis is responsible for the bad prognosis in cancer patients. Advances in research on metastasis prevention focus attention on the molecular mechanisms underlying cancer cell motility and invasion to improve therapies for long-term survival in cancer patients. The so-called “migrastatics” could help block cancer cell invasion and lead to the rapid development of antimetastatic therapies, improving conventional cancer therapies. In the relentless search for migrastatics, the marine environment represents an important source of natural compounds due to its enormous biodiversity. Thus, this review is a selection of scientific research that has pointed out in a broad spectrum of in vitro and in vivo models the anti-cancer power of marine-derived products against cancer cell migration and invasion over the past five years. Overall, this review might provide a useful up-to-date guide about marine-derived compounds with potential interest for pharmaceutical and scientific research on antimetastatic drug endpoints. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents 2.0)
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