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Marine Drugs
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Marine Natural Products as Anticancer Agents
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Marine Natural Products as Anticancer Agents

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

Deadline for manuscript submissions: closed (15 June 2021) | Viewed by 40119

Printed Edition Available!
A printed edition of this Special Issue is available here.

Special Issue Editors

Dr. Celso Alves

E-Mail Website
Guest Editor
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
Prof. Dr. Marc Diederich

E-Mail Website
Guest Editor
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 concerning cancer biology and its therapeutic strategies achieved in the last decades, cancer remains a huge threat for human health, and one of the deadliest diseases worldwide. One of the main factors contributing to the high cancer mortality is related to therapy failure and consequent cancer relapse; thus it is of the utmost importance to develop innovative therapeutics strategies, including new drugs. In this field, marine natural products have revealed uncommon and rare chemical features, not found in the terrestrial environment, on which the molecular modelling and chemical synthesis of novel anticancer drugs can be inspired. As these compounds were produced in co-evolution with biological systems, they present greater an efficiency and specificity for interacting with biological target sites, exhibiting novel mechanisms of action and the ability to modulate distinct intracellular signaling pathways.

The focus of this Special Issue will be to 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 and 3D culture models, to avoid the gap between in vitro and in vivo experiments is encouraged. 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, publications describing the cancer activity of such marine compounds alone or in combination with checkpoint inhibitors are encouraged to be submitted.

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 or novel marine compounds with a 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

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Published Papers (10 papers)

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Editorial

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3 pages, 200 KiB  
Editorial
Marine Natural Products as Anticancer Agents
by Celso Alves and Marc Diederich
Mar. Drugs 2021, 19(8), 447; https://doi.org/10.3390/md19080447 - 4 Aug 2021
Cited by 12 | Viewed by 3451
Abstract
Cancer remains one of the major threats to human health and one of the deadliest diseases worldwide [...] Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)

Research

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29 pages, 9849 KiB  
Article
Anti-Leukemic Properties of Aplysinopsin Derivative EE-84 Alone and Combined to BH3 Mimetic A-1210477
by Sungmi Song, Sua Kim, Eslam R. El-Sawy, Claudia Cerella, Barbora Orlikova-Boyer, Gilbert Kirsch, Christo Christov, Mario Dicato and Marc Diederich
Mar. Drugs 2021, 19(6), 285; https://doi.org/10.3390/md19060285 - 21 May 2021
Cited by 11 | Viewed by 3586
Abstract
Aplysinopsins are a class of marine indole alkaloids that exhibit a wide range of biological activities. Although both the indole and N-benzyl moieties of aplysinopsins are known to possess antiproliferative activity against cancer cells, their mechanism of action remains unclear. Through in vitro [...] Read more.
Aplysinopsins are a class of marine indole alkaloids that exhibit a wide range of biological activities. Although both the indole and N-benzyl moieties of aplysinopsins are known to possess antiproliferative activity against cancer cells, their mechanism of action remains unclear. Through in vitro and in vivo proliferation and viability screening of newly synthesized aplysinopsin analogs on myelogenous leukemia cell lines and zebrafish toxicity tests, as well as analysis of differential toxicity in noncancerous RPMI 1788 cells and PBMCs, we identified EE-84 as a promising novel drug candidate against chronic myeloid leukemia. This indole derivative demonstrated drug-likeness in agreement with Lipinski’s rule of five. Furthermore, EE-84 induced a senescent-like phenotype in K562 cells in line with its cytostatic effect. EE-84-treated K562 cells underwent morphological changes in line with mitochondrial dysfunction concomitant with autophagy and ER stress induction. Finally, we demonstrated the synergistic cytotoxic effect of EE-84 with a BH3 mimetic, the Mcl-1 inhibitor A-1210477, against imatinib-sensitive and resistant K562 cells, highlighting the inhibition of antiapoptotic Bcl-2 proteins as a promising novel senolytic approach against chronic myeloid leukemia. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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Graphical abstract

9 pages, 5202 KiB  
Communication
Optimization of Two Steps in Scale-Up Synthesis of Nannocystin A
by Tingrong Zhang, Shaojie Miao, Mingxiao Zhang, Wenjie Liu, Liang Wang and Yue Chen
Mar. Drugs 2021, 19(4), 198; https://doi.org/10.3390/md19040198 - 31 Mar 2021
Cited by 4 | Viewed by 2238
Abstract
We have accomplished a 10-step (longest linear) total synthesis of nannocystin A on a four hundred milligram scale. The previously reported Kobayashi vinylogous Mukaiyama aldol reaction to connect C4 and C5 was unreproducible during the scaling up process. A more convenient and cost-efficient [...] Read more.
We have accomplished a 10-step (longest linear) total synthesis of nannocystin A on a four hundred milligram scale. The previously reported Kobayashi vinylogous Mukaiyama aldol reaction to connect C4 and C5 was unreproducible during the scaling up process. A more convenient and cost-efficient Keck asymmetric vinylogous aldol reaction was employed to improve this transformation. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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14 pages, 3745 KiB  
Article
Astaxanthin Reduces Stemness Markers in BT20 and T47D Breast Cancer Stem Cells by Inhibiting Expression of Pontin and Mutant p53
by Yong Tae Ahn, Min Sung Kim, Youn Sook Kim and Won Gun An
Mar. Drugs 2020, 18(11), 577; https://doi.org/10.3390/md18110577 - 20 Nov 2020
Cited by 16 | Viewed by 4238
Abstract
Astaxanthin (AST) is a product made from marine organisms that has been used as an anti-cancer supplement. It reduces pontin expression and induces apoptosis in SKBR3, a breast cancer cell line. Using Western blotting and qRT-PCR analyses, this study revealed that in the [...] Read more.
Astaxanthin (AST) is a product made from marine organisms that has been used as an anti-cancer supplement. It reduces pontin expression and induces apoptosis in SKBR3, a breast cancer cell line. Using Western blotting and qRT-PCR analyses, this study revealed that in the T47D and BT20 breast cancer cell lines, AST inhibits expression of pontin and mutp53, as well as the Oct4 and Nanog cancer stem cell (CSC) stemness genes. In addition, we explored the mechanism by which AST eradicates breast cancer cells using pontin siRNAs. Pontin knockdown by pontin siRNA reduced proliferation, Oct4 and Nanog expression, colony and spheroid formation, and migration and invasion abilities in breast cancer cells. In addition, reductions in Oct4, Nanog, and mutp53 expression following rottlerin treatment confirmed the role of pontin in these cells. Therefore, pontin may play a central role in the regulation of CSC properties and in cell proliferation following AST treatment. Taken together, these findings demonstrate that AST can repress CSC stemness genes in breast cancer cells, which implies that AST therapy could be used to improve the efficacy of other anti-cancer therapies against breast cancer cells. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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19 pages, 3732 KiB  
Article
Marine-Derived Penicillium purpurogenum Reduces Tumor Size and Ameliorates Inflammation in an Erlich Mice Model
by Amanda Mara Teles, Leticia Prince Pereira Pontes, Sulayne Janayna Araújo Guimarães, Ana Luiza Butarelli, Gabriel Xavier Silva, Flavia Raquel Fernandes do Nascimento, Geusa Felipa de Barros Bezerra, Carla Junqueira Moragas-Tellis, Rui Miguel Gil da Costa, Marcos Antonio Custódio Neto da Silva, Fernando Almeida-Souza, Kátia da Silva Calabrese, Ana Paula Silva Azevedo-Santos and Maria do Desterro Soares Brandão Nascimento
Mar. Drugs 2020, 18(11), 541; https://doi.org/10.3390/md18110541 - 29 Oct 2020
Cited by 6 | Viewed by 3069
Abstract
Background: This study addresses the antitumoral properties of Penicillium purpurogenum isolated from a polluted lagoon in Northeastern Brazil. Methods: Ethyl Acetate Extracellular Extract (EAE) was used. The metabolites were studied using direct infusion mass spectrometry. The solid Ehrlich tumor model was used for [...] Read more.
Background: This study addresses the antitumoral properties of Penicillium purpurogenum isolated from a polluted lagoon in Northeastern Brazil. Methods: Ethyl Acetate Extracellular Extract (EAE) was used. The metabolites were studied using direct infusion mass spectrometry. The solid Ehrlich tumor model was used for antitumor activity. Female Swiss mice were divided into groups (n = 10/group) as follows: The negative control (CTL−), treated with a phosphate buffered solution; the positive control (CTL+), treated with cyclophosphamide (25 mg/kg); extract treatments at doses of 4, 20, and 100 mg/kg; animals without tumors or treatments (Sham); and animals without tumors treated with an intermediate dose (EAE20). All treatments were performed intraperitoneally, daily, for 15 days. Subsequently, the animals were euthanized, and the tumor, lymphoid organs, and serum were used for immunological, histological, and biochemical parameter evaluations. Results: The extract was rich in meroterpenoids. All doses significantly reduced tumor size, and the 20 and 100 mg/kg doses reduced tumor-associated inflammation and tumor necrosis. The extract also reduced the cellular infiltration of lymphoid organs and circulating TNF-α levels. The extract did not induce weight loss or renal and hepatic toxic changes. Conclusions: These results indicate that P. purpurogenum exhibits immunomodulatory and antitumor properties in vivo. Thus, fungal fermentation is a valid biotechnological approach to the production of antitumor agents. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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13 pages, 1136 KiB  
Article
New Biscembranoids Sardigitolides A–D and Known Cembranoid-Related Compounds from Sarcophyton digitatum: Isolation, Structure Elucidation, and Bioactivities
by Tzu-Yin Huang, Chiung-Yao Huang, Chih-Hua Chao, Chi-Chien Lin, Chang-Feng Dai, Jui-Hsin Su, Ping-Jyun Sung, Shih-Hsiung Wu and Jyh-Horng Sheu
Mar. Drugs 2020, 18(9), 452; https://doi.org/10.3390/md18090452 - 29 Aug 2020
Cited by 16 | Viewed by 3261
Abstract
Chemical examination from the cultured soft coral Sarcophyton digitatum resulted in the isolation and structural identification of four new biscembranoidal metabolites, sardigitolides A–D (1–4), along with three previously isolated biscembranoids, sarcophytolide L (5), glaucumolide A (6 [...] Read more.
Chemical examination from the cultured soft coral Sarcophyton digitatum resulted in the isolation and structural identification of four new biscembranoidal metabolites, sardigitolides A–D (1–4), along with three previously isolated biscembranoids, sarcophytolide L (5), glaucumolide A (6), glaucumolide B (7), and two known cembranoids (8 and 9). The chemical structures of all isolates were elucidated on the basis of 1D and 2D NMR spectroscopic analyses. Additionally, in order to discover bioactivity of marine natural products, 1–8 were examined in terms of their inhibitory potential against the upregulation of inflammatory factor production in lipopolysaccharide (LPS)-stimulated murine macrophage J774A.1 cells and their cytotoxicities against a limited panel of cancer cells. The anti-inflammatory results showed that at a concentration of 10 µg/mL, 6 and 8 inhibited the production of IL-1β to 68 ± 1 and 56 ± 1%, respectively, in LPS-stimulated murine macrophages J774A.1. Furthermore, sardigitolide B (2) displayed cytotoxicities toward MCF-7 and MDA-MB-231 cancer cell lines with the IC50 values of 9.6 ± 3.0 and 14.8 ± 4.0 µg/mL, respectively. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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13 pages, 3519 KiB  
Article
Anti-Tumor Effects of Astaxanthin by Inhibition of the Expression of STAT3 in Prostate Cancer
by Shao-Qian Sun, You-Xi Zhao, Si-Yu Li, Jing-Wen Qiang and Yi-Zhi Ji
Mar. Drugs 2020, 18(8), 415; https://doi.org/10.3390/md18080415 - 7 Aug 2020
Cited by 36 | Viewed by 5966
Abstract
Astaxanthin is a natural product gaining increasing attention due to its safety and anti-cancer properties. In this study, we investigated the mechanisms of the anti-cancer effects of astaxanthin on prostate cancer (PCa) cell lines using aggressive PCa DU145 cells. Also an instantaneous silenced [...] Read more.
Astaxanthin is a natural product gaining increasing attention due to its safety and anti-cancer properties. In this study, we investigated the mechanisms of the anti-cancer effects of astaxanthin on prostate cancer (PCa) cell lines using aggressive PCa DU145 cells. Also an instantaneous silenced cell line (si-STAT3) derived from DU145 and a control cell line (si-NK) were used for the MTT and colony formation assays to determine the role of astaxanthin in proliferation and colony formation abilities. Flow cytometry assays were used to detect the apoptosis of tumor cells. Migration and invasion assays detected the weakening of the respective abilities. Western blot and RT-PCR tests detected the levels of STAT3 protein and mRNA. Astaxanthin resulted in suppression of the proliferation of DU145 cells and the level of STAT3. The treatment of DU145 cells with astaxanthin decreased the cloning ability, increased the apoptosis percentage and weakened the abilities of migration and invasion of the cells. Furthermore, astaxanthin reduced the expression of STAT3 at protein and mRNA levels. The effects were enhanced when astaxanthin and si-STAT3 were combined. The results of animal experiments were consistent with the results in cells. Thus, astaxanthin inhibits the proliferation of DU145 cells by reducing the expression of STAT3. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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12 pages, 4482 KiB  
Article
Exploring the Mechanism of Flaccidoxide-13-Acetate in Suppressing Cell Metastasis of Hepatocellular Carcinoma
by Yu-Jen Wu, Wen-Chi Wei, Guo-Fong Dai, Jui-Hsin Su, Yu-Hwei Tseng and Tsung-Chang Tsai
Mar. Drugs 2020, 18(6), 314; https://doi.org/10.3390/md18060314 - 15 Jun 2020
Cited by 14 | Viewed by 3028
Abstract
Hepatocellular carcinoma (HCC) is the most common liver or hepatic cancer, accounting for 80% of all cases. The majority of this cancer mortality is due to metastases, rather than orthotopic tumors. Therefore, the inhibition of tumor metastasis is widely recognized as the key [...] Read more.
Hepatocellular carcinoma (HCC) is the most common liver or hepatic cancer, accounting for 80% of all cases. The majority of this cancer mortality is due to metastases, rather than orthotopic tumors. Therefore, the inhibition of tumor metastasis is widely recognized as the key strategy for successful intervention. A cembrane-type diterpene, flaccidoxide-13-acetate, isolated from marine soft coral Sinularia gibberosa, has been reported to have inhibitory effects against RT4 and T24 human bladder cancer invasion and cell migration. In this study, we investigated its suppression effects on tumor growth and metastasis of human HCC, conducting Boyden chamber and Transwell assays using HA22T and HepG2 human HCC cell lines to evaluate invasion and cell migration. We utilized gelatin zymography to determine the enzyme activities of matrix metalloproteinases MMP-2 and MMP-9. We also analyzed the expression levels of MMP-2 and MMP-9. Additionally, assays of tissue inhibitors of metalloproteinase-1/2 (TIMP-1/2), the focal adhesion kinase (FAK)/phosphatidylinositide-3 kinases (PI3K)/Akt/mammalian target of the rapamycin (mTOR) signaling pathway, and the epithelial-mesenchymal transition (EMT) process were performed. We observed that flaccidoxide-13-acetate could potentially inhibit HCC cell migration and invasion. We postulated that, by inhibiting the FAK/PI3K/Akt/mTOR signaling pathway, MMP-2 and MMP-9 expressions were suppressed, resulting in HCC cell metastasis. Flaccidoxide-13-acetate was found to inhibit EMT in HA22T and HepG2 HCC cells. Our study results suggested the potential of flaccidoxide-13-acetate as a chemotherapeutic candidate; however, its clinical application for the management of HCC in humans requires further research. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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10 pages, 2363 KiB  
Article
Cytotoxic Secondary Metabolites Isolated from the Marine Alga-Associated Fungus Penicillium chrysogenum LD-201810
by Lin-Lin Jiang, Jin-Xiu Tang, Yong-Heng Bo, You-Zhi Li, Tao Feng, Hong-Wei Zhu, Xin Yu, Xing-Xiao Zhang, Jian-Long Zhang and Weiyi Wang
Mar. Drugs 2020, 18(5), 276; https://doi.org/10.3390/md18050276 - 22 May 2020
Cited by 17 | Viewed by 3927
Abstract
A new pentaketide derivative, penilactonol A (1), and two new hydroxyphenylacetic acid derivatives, (2’R)-stachyline B (2) and (2’R)-westerdijkin A (3), together with five known metabolites, bisabolane-type sesquiterpenoids 4–6 and meroterpenoids 7 [...] Read more.
A new pentaketide derivative, penilactonol A (1), and two new hydroxyphenylacetic acid derivatives, (2’R)-stachyline B (2) and (2’R)-westerdijkin A (3), together with five known metabolites, bisabolane-type sesquiterpenoids 4–6 and meroterpenoids 7 and 8, were isolated from the solid culture of a marine alga-associated fungus Penicillium chrysogenum LD-201810. Their structures were elucidated based on extensive spectroscopic analyses, including 1D/2D NMR and high resolution electrospray ionization mass spectra (HRESIMS). The absolute configurations of the stereogenic carbons in 1 were determined by the (Mo2(OAc)4)-induced circular dichroism (CD) and comparison of the calculated and experimental electronic circular dichroism (ECD) spectra, while the absolute configuration of the stereogenic carbon in 2 was established using single-crystal X-ray diffraction analysis. Compounds 2 and 3 adapt the 2’R-configuration as compared to known hydroxyphenylacetic acid-derived and O-prenylated natural products. The cytotoxicity of 1–8 against human carcinoma cell lines (A549, BT-549, HeLa, HepG2, MCF-7, and THP-1) was evaluated. Compound 3 exhibited cytotoxicity to the HepG2 cell line with an IC50 value of 22.0 μM. Furthermore, 5 showed considerable activities against A549 and THP-1 cell lines with IC50 values of 21.2 and 18.2 μM, respectively. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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Review

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28 pages, 5153 KiB  
Review
Marine-Derived Secondary Metabolites as Promising Epigenetic Bio-Compounds for Anticancer Therapy
by Mariarosaria Conte, Elisabetta Fontana, Angela Nebbioso and Lucia Altucci
Mar. Drugs 2021, 19(1), 15; https://doi.org/10.3390/md19010015 - 31 Dec 2020
Cited by 18 | Viewed by 4607
Abstract
Sessile organisms such as seaweeds, corals, and sponges continuously adapt to both abiotic and biotic components of the ecosystem. This extremely complex and dynamic process often results in different forms of competition to ensure the maintenance of an ecological niche suitable for survival. [...] Read more.
Sessile organisms such as seaweeds, corals, and sponges continuously adapt to both abiotic and biotic components of the ecosystem. This extremely complex and dynamic process often results in different forms of competition to ensure the maintenance of an ecological niche suitable for survival. A high percentage of marine species have evolved to synthesize biologically active molecules, termed secondary metabolites, as a defense mechanism against the external environment. These natural products and their derivatives may play modulatory roles in the epigenome and in disease-associated epigenetic machinery. Epigenetic modifications also represent a form of adaptation to the environment and confer a competitive advantage to marine species by mediating the production of complex chemical molecules with potential clinical implications. Bioactive compounds are able to interfere with epigenetic targets by regulating key transcriptional factors involved in the hallmarks of cancer through orchestrated molecular mechanisms, which also establish signaling interactions of the tumor microenvironment crucial to cancer phenotypes. In this review, we discuss the current understanding of secondary metabolites derived from marine organisms and their synthetic derivatives as epigenetic modulators, highlighting advantages and limitations, as well as potential strategies to improve cancer treatment. Full article
(This article belongs to the Special Issue Marine Natural Products as Anticancer Agents)
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