Discovery of Marine-Derived Anticancer Agents, 2nd Edition

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

Deadline for manuscript submissions: 30 September 2025 | Viewed by 2601

Special Issue Editor


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Guest Editor
Department of Anatomy & Physiology, Kansas State University College of Veterinary Medicine, Manhattan, KS 66506, USA
Interests: anticancer agents in green algae; immune checkpoin inhibitor-based cancer therapy; nanoparticle-based cancer gene therapy; mesanchymal stem cell-based gene therapy
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Special Issue Information

Dear Colleagues,

Following on from the success of the Special Issue titled “Discovery of Marine-Derived Anticancer Agents” , we are delighted to edit the second edition of this Special Issue.

Cancer is one of the deadliest diseases worldwide. Despite the therapeutic strategies achieved in recent decades, cancer remains a huge threat to human health, and therefore it is important to develop innovative therapeutic strategies, including new drugs.

In recent years, many studies have indicated that marine-derived compounds exhibit anticancer properties, such as inhibiting cell growth and migration in vitro and in vivo. As many of these compounds are involved in several biological processes and interactions, they may have a more effective role in interacting with biological target sites and mediating distinct intracellular signaling pathways.

Our objective is to present these new marine sources as active molecules for cancer prevention and therapy and demonstrate their efficiency. As the Guest Editor of this Special Issue, I invite scientists from all over the world to submit reviews and original and conceptual research articles highlighting the use of marine resources as drugs for the treatment of cancer and their mechanisms of action.

Prof. Dr. Masaaki Tamura
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

  • anticancer
  • anti-tumor
  • anti-proliferation
  • molecular targets
  • marine biotechnology
  • marine natural products
  • isolation and structure elucidation
  • drug discovery

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Related Special Issue

Published Papers (3 papers)

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Research

14 pages, 3081 KiB  
Article
Marine Sponge-Derived Gukulenin A Sensitizes Ovarian Cancer Cells to PARP Inhibition via Ferroptosis Induction
by Jin-Hyung Kim, Jung-Rae Rho and Jung-Hye Choi
Mar. Drugs 2025, 23(4), 138; https://doi.org/10.3390/md23040138 - 22 Mar 2025
Viewed by 362
Abstract
Resistance to PARP inhibitors (PARPi), such as olaparib (OLA), is a major challenge in ovarian cancer treatment. In this study, we investigated the combination effect of PARPi and gukulenin A (GUA), a bis-tropolone tetraterpenoid isolated from the marine sponge Phorbas gukhulensis. We [...] Read more.
Resistance to PARP inhibitors (PARPi), such as olaparib (OLA), is a major challenge in ovarian cancer treatment. In this study, we investigated the combination effect of PARPi and gukulenin A (GUA), a bis-tropolone tetraterpenoid isolated from the marine sponge Phorbas gukhulensis. We found that GUA at a mildly cytotoxic dose synergistically enhanced OLA-induced cytotoxicity in human ovarian cancer cells. The combination treatment significantly increased reactive oxygen species (ROS) levels and lipid peroxidation, leading to ferroptotic rather than apoptotic cell death. Network pharmacology and gene ontology (GO) enrichment analyses revealed oxidative stress-related pathways as key mediators of this effect. Inhibition of NADPH oxidase (NOX) reversed combination-induced cell death, while ferrostatin-1 (FER-1), a ferroptosis inhibitor, significantly reduced lipid peroxidation and cytotoxicity. Additionally, GUA and OLA treatment suppressed ERK1/2 activation, and ERK overexpression attenuated the combination-induced cell death. Collectively, these findings suggest that marine-derived GUA enhances PARPi efficacy in ovarian cancer cells by inducing ferroptosis through oxidative stress and ERK pathway modulation. Full article
(This article belongs to the Special Issue Discovery of Marine-Derived Anticancer Agents, 2nd Edition)
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18 pages, 3187 KiB  
Article
Discovery of PD-L1 Peptide Inhibitors from Ascidian Enzymatic Hydrolysates by Affinity Ultrafiltration Coupled to NanoLC-MS/MS
by Qiuyang Huang, Xiaoling Zang, Xinyu Jin, Qian Liu, Xin Zhang, Xinyu Li, Lizhen Zhao and Zhihua Lv
Mar. Drugs 2025, 23(4), 137; https://doi.org/10.3390/md23040137 - 21 Mar 2025
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Abstract
Anti-PD-1 and anti-PD-L1 antibodies have achieved great clinical success in cancer immunotherapy, and peptide and small molecule inhibitors of PD-1/PD-L1 binding also attract much attention. Ascidians are not only seafood, but are also an important source of bioactive substances, including anti-tumor components. In [...] Read more.
Anti-PD-1 and anti-PD-L1 antibodies have achieved great clinical success in cancer immunotherapy, and peptide and small molecule inhibitors of PD-1/PD-L1 binding also attract much attention. Ascidians are not only seafood, but are also an important source of bioactive substances, including anti-tumor components. In this study, ascidian enzymatic hydrolysates were found to contain PD-1/PD-L1 inhibitory components. Affinity ultrafiltration (AUF) coupled with the nanoLC-MS/MS method was first applied in screening for PD-L1 peptide inhibitors from ascidian enzymatic hydrolysates. Two anti-PD-L1 ascidian peptides, C5 (LDVVIHTVTYGDR) and S2 (VLRDNIQGITKPAIR), were filtered out from the ascidians Ciona intestinalis and Styela clava, respectively. C5 and S2 showed moderate anti-PD-1/PD-L1 effects with the IC50 values of 33.9 µM (C5) and 112.8 μM (S2), respectively, by homogenous time-resolved fluorescence (HTRF) binding assay, and the KD values of 22.9 µM (C5) and 29.1 µM (S2), respectively, by surface plasmon resonance (SPR) assay. The results of this study suggest that ascidian enzymatic hydrolysates may be a potential source of bioactive peptides with anti-PD-1/PD-L1 activity. Full article
(This article belongs to the Special Issue Discovery of Marine-Derived Anticancer Agents, 2nd Edition)
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24 pages, 3164 KiB  
Article
Cytotoxic Effects of ZnO and Ag Nanoparticles Synthesized in Microalgae Extracts on PC12 Cells
by Giacomo Fais, Agnieszka Sidorowicz, Giovanni Perra, Debora Dessì, Francesco Loy, Nicola Lai, Paolo Follesa, Roberto Orrù, Giacomo Cao and Alessandro Concas
Mar. Drugs 2024, 22(12), 549; https://doi.org/10.3390/md22120549 - 4 Dec 2024
Cited by 6 | Viewed by 1531
Abstract
The green synthesis of silver (Ag) and zinc oxide (ZnO) nanoparticles (NPs), as well as Ag/Ag2O/ZnO nanocomposites (NCs), using polar and apolar extracts of Chlorella vulgaris, offers a sustainable method for producing nanomaterials with tunable properties. The impact of the [...] Read more.
The green synthesis of silver (Ag) and zinc oxide (ZnO) nanoparticles (NPs), as well as Ag/Ag2O/ZnO nanocomposites (NCs), using polar and apolar extracts of Chlorella vulgaris, offers a sustainable method for producing nanomaterials with tunable properties. The impact of the synthesis environment and the nanomaterials’ characteristics on cytotoxicity was evaluated by examining reactive species production and their effects on mitochondrial bioenergetic functions. Cytotoxicity assays on PC12 cells, a cell line originated from a rat pheochromocytoma, an adrenal medulla tumor, demonstrated that Ag/Ag2O NPs synthesized with apolar (Ag/Ag2O NPs A) and polar (Ag/Ag2O NPs P) extracts exhibited significant cytotoxic effects, primarily driven by Ag+ ion release and the disruption of mitochondrial function. However, it is more likely the organic content, rather than size, influenced anticancer activity, as commercial Ag NPs, despite smaller crystallite sizes, exhibit less effective activity. ZnO NPs P showed increased reactive oxygen species (ROS) generation, correlated with higher cytotoxicity, while ZnO NPs A produced lower ROS levels, resulting in diminished cytotoxic effects. A comparative analysis revealed significant differences in LD50 values and toxicity profiles. Differentiated PC12 cells showed higher resistance to ZnO, while AgNPs and Ag/Ag2O-based materials had similar effects on both cell types. This study emphasizes the crucial role of the synthesis environment and bioactive compounds from C. vulgaris in modulating nanoparticle surface chemistry, ROS generation, and cytotoxicity. The results provide valuable insights for designing safer and more effective nanomaterials for biomedical applications, especially for targeting tumor-like cells, by exploring the relationships between nanoparticle size, polarity, capping agents, and nanocomposite structures. Full article
(This article belongs to the Special Issue Discovery of Marine-Derived Anticancer Agents, 2nd Edition)
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