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Marine Drugs
Special Issues
Synthesis and Discovery of Marine Antitumor Molecules
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Synthesis and Discovery of Marine Antitumor Molecules

A special issue of Marine Drugs (ISSN 1660-3397). This special issue belongs to the section "Synthesis and Medicinal Chemistry of Marine Natural Products".

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 3831

Special Issue Editors

Dr. Xiaoyang Li

E-Mail Website
Guest Editor
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao 266003, China
Interests: medicinal chemistry; drug design; epigenetic targets; histone deacetylases inhibitors; anti-tumor; inflammation
Dr. Chong Qin

E-Mail Website
Guest Editor
Center for Targeted Protein Degradation and Drug Discovery, Ocean University of China, Qingdao 266003, China
Interests: drug discovery; PROTACs; prostate cancer; marine natural active substances
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is a prominent cause of death and a significant obstacle to increasing life expectancy in all countries around the world. The World Health Organization's (WHO) estimates from 2019 suggest that cancer is the leading or second-leading cause of death before the age of 70. The discovery of novel anticancer agents continues to represent a popular field of research. The ecological environment of marine organisms differs significantly from that of terrestrial organisms. The ocean harbors a wealth of structurally novel, biologically active, and highly potent natural products that have the potential to serve as drug leads, including those for anti-cancer drugs. These marine products are also paving the way for the identification of novel biological targets and biochemical pathways in cancer research.

In this Special Issue, we present cutting-edge research in medicinal chemistry, pharmacology, and chemical biology related to marine antitumor molecules. This includes studies on the synthesis and structural modification of marine molecules, the total synthesis of marine antitumor drugs, and investigations into the pharmacological and biological antitumor mechanisms. Our aim is to provide valuable insights into the discovery of novel antitumor agents from marine sources as well as into the elucidation of their mechanisms of action. Furthermore, we aim to offer new perspectives for the design and optimization of marine drug candidates, for the benefit of both academic and industry researchers. We welcome both research articles and reviews.

Dr. Xiaoyang Li
Dr. Chong Qin
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

  • marine
  • natural products
  • antitumor agents
  • drug design
  • drug discovery
  • biological mechanism
  • chemical synthesis
  • medicinal chemistry

Published Papers (2 papers)

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Research

32 pages, 49487 KiB  
Article
Simplified Synthesis of Renieramycin T Derivatives to Target Cancer Stem Cells via β-Catenin Proteasomal Degradation in Human Lung Cancer
by Zin Zin Ei, Satapat Racha, Masashi Yokoya, Daiki Hotta, Hongbin Zou and Pithi Chanvorachote
Mar. Drugs 2023, 21(12), 627; https://doi.org/10.3390/md21120627 - 30 Nov 2023
Viewed by 1684
Abstract
Cancer stem cells (CSCs) found within cancer tissue play a pivotal role in its resistance to therapy and its potential to metastasize, contributing to elevated mortality rates among patients. Significant strides in understanding the molecular foundations of CSCs have led to preclinical investigations [...] Read more.
Cancer stem cells (CSCs) found within cancer tissue play a pivotal role in its resistance to therapy and its potential to metastasize, contributing to elevated mortality rates among patients. Significant strides in understanding the molecular foundations of CSCs have led to preclinical investigations and clinical trials focused on CSC regulator β-catenin signaling targeted interventions in malignancies. As part of the ongoing advancements in marine-organism-derived compound development, it was observed that among the six analogs of Renieramycin T (RT), a potential lead alkaloid from the blue sponge Xestospongia sp., the compound DH_32, displayed the most robust anti-cancer activity in lung cancer A549, H23, and H292 cells. In various lung cancer cell lines, DH_32 exhibited the highest efficacy, with IC50 values of 4.06 ± 0.24 μM, 2.07 ± 0.11 μM, and 1.46 ± 0.06 μM in A549, H23, and H292 cells, respectively. In contrast, parental RT compounds had IC50 values of 5.76 ± 0.23 μM, 2.93 ± 0.07 μM, and 1.52 ± 0.05 μM in the same order. Furthermore, at a dosage of 25 nM, DH_32 showed a stronger ability to inhibit colony formation compared to the lead compound, RT. DH_32 was capable of inducing apoptosis in lung cancer cells, as demonstrated by increased PARP cleavage and reduced levels of the proapoptotic protein Bcl2. Our discovery confirms that DH_32 treatment of lung cancer cells led to a reduced level of CD133, which is associated with the suppression of stem-cell-related transcription factors like OCT4. Moreover, DH_32 significantly suppressed the ability of tumor spheroids to form compared to the original RT compound. Additionally, DH_32 inhibited CSCs by promoting the degradation of β-catenin through ubiquitin–proteasomal pathways. In computational molecular docking, a high-affinity interaction was observed between DH_32 (grid score = −35.559 kcal/mol) and β-catenin, indicating a stronger binding interaction compared to the reference compound R9Q (grid score = −29.044 kcal/mol). In summary, DH_32, a newly developed derivative of the right-half analog of RT, effectively inhibited the initiation of lung cancer spheroids and the self-renewal of lung cancer cells through the upstream process of β-catenin ubiquitin–proteasomal degradation. Full article
(This article belongs to the Special Issue Synthesis and Discovery of Marine Antitumor Molecules)
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21 pages, 9064 KiB  
Article
Ascomylactam C Induces an Immunogenic Cell Death Signature via Mitochondria-Associated ER Stress in Lung Cancer and Melanoma
by Yun Huang, Hongmei Yan, Bingzhi Zhang, Ge Zhu, Jianchen Yu, Xuhan Xiao, Wenxuan He, Yan Chen, Xiaoxia Gao, Zhigang She, Mengfeng Li and Jie Yuan
Mar. Drugs 2023, 21(12), 600; https://doi.org/10.3390/md21120600 - 21 Nov 2023
Cited by 1 | Viewed by 1943
Abstract
Ascomylactam C (AsC) is a new 13-membered-ring macrocyclic alkaloid, which was first isolated and identified in 2019 from the secondary metabolites of the mangrove endophytic fungus Didymella sp. CYSK-4 in the South China Sea. AsC has been found to have a broad-spectrum cytotoxic [...] Read more.
Ascomylactam C (AsC) is a new 13-membered-ring macrocyclic alkaloid, which was first isolated and identified in 2019 from the secondary metabolites of the mangrove endophytic fungus Didymella sp. CYSK-4 in the South China Sea. AsC has been found to have a broad-spectrum cytotoxic activity. However, the antitumor effects in vivo and mechanisms of AsC remain unclear. The aim of this study was to describe the effects of AsC on lung cancer and melanoma cells and to explore the antitumor molecular mechanism of AsC. In vitro, we used plate colony formation experiments and demonstrated the ability of AsC to inhibit low-density tumor growth. An Annexin V/PI cell apoptosis detection experiment revealed that AsC induced tumor cell apoptosis. In vivo, AsC suppressed the tumor growth of LLC and B16F10 allograft significantly in mice, and promoted the infiltration of CD4+ T and CD8+ T cells in tumor tissues. Mechanistically, by analyses of Western blotting, immunofluorescence and ELISA analysis, we found that AsC increased ROS formation, induced endoplasmic reticulum (ER) stress, activated the protein kinase RNA-like ER kinase (PERK)/eukaryotic translation initiation factor (eIF2α)/activating transcription factor 4 (ATF4)/C/EBP homologous protein (CHOP) signaling pathway, and induced immunogenic cell death (ICD) of tumor cells. Our results suggest that AsC may be a potentially promising antitumor drug candidate. Full article
(This article belongs to the Special Issue Synthesis and Discovery of Marine Antitumor Molecules)
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