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Biomolecules
Special Issues
Antitumor Agents from Natural Sources 2026
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Antitumor Agents from Natural Sources 2026

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Natural and Bio-derived Molecules".

Deadline for manuscript submissions: 31 December 2026 | Viewed by 15309

Special Issue Editor

Prof. Dr. Hang Fai (Henry) Kwok

E-Mail Website
Guest Editor
1. Institute of Translational Medicine, Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR 999078, China
2. Department of Biomedical Sciences, Faculty of Health Sciences, University of Macau, Avenida de Universidade, Taipa, Macau SAR 999078, China
Interests: novel therapeutic antibody development; venom-based peptide and natural biomolecule prototype drug development; cancer biomarker and immunotherapy marker discovery for prognostic and therapeutic validation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleague,

This Special Issue aims to highlight the pleiotropic mechanism(s) underlying the processes of cancer initiation as well as progression and focus on the antitumor properties of agents derived from natural sources. Several small molecules isolated from plants, fruits, vegetables, spices, animal venoms/secretions, etc., have demonstrated significant efficacy against various malignancies. These agents can suppress different characteristic hallmarks of cancer cells and have been investigated in various preclinical as well as clinical studies. This Special Issue will highlight the potential role of such important natural agents in both cancer prevention and therapy.

Dr. Hang Fai (Henry) Kwok
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 250 words) can be sent to the Editorial Office for assessment.

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. Biomolecules 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 2700 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

  • antitumor agents
  • natural sources
  • cancer prevention and therapy

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Published Papers (4 papers)

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Research

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20 pages, 4815 KB  
Article
Theaflavin-3,3′-Digallate Targets Pin1 to Suppress Hepatocellular Carcinoma Malignant Proliferation Through Modulation of MAPK and PI3K/AKT Signaling Pathways In Vitro
by Shaoli Lv, Wenli Jiang, Jingyi Liu, Jiaxin Tao, Hui Zhong, Huaqing He, Xinling Liao, Jiayang Xie, Xiyuan Ouyang and Wang Wang
Biomolecules 2026, 16(4), 583; https://doi.org/10.3390/biom16040583 - 14 Apr 2026
Viewed by 431
Abstract
Theaflavin-3,3′-digallate (TF3), a flavan-3-ol derivative found in black tea, exhibits anti-tumor activity, but its mechanism of action in hepatocellular carcinoma (HCC) remains to be elucidated. Here we systematically delineate how TF3 targets Pin1 to suppress HCC through an integrated approach combining computational simulations, [...] Read more.
Theaflavin-3,3′-digallate (TF3), a flavan-3-ol derivative found in black tea, exhibits anti-tumor activity, but its mechanism of action in hepatocellular carcinoma (HCC) remains to be elucidated. Here we systematically delineate how TF3 targets Pin1 to suppress HCC through an integrated approach combining computational simulations, enzyme assay and cell-based assays. TF3 spontaneously occupies the active site of Pin1 with a docking score of −8.9 kcal/mol, inhibiting its PPIase activity (IC50 = 60.33 μmol/L) and yielding a binding constant (Ka) of 3.1 × 105 mol/L. Drug affinity responsive target stability (DARTS) assays further corroborated that TF3 directly engages Pin1 within HCC cells. Functionally, TF3 potently suppressed the viability of HepG2, SK-Hep-1 and Huh-7 cells in both dose- and time-dependent manners (IC50 = 61.22, 14.09 and 69.85 μmol/L at 24 h, respectively), and exhibited a modest selectivity window against the viability of L02 and THLE-2 cells (IC50 = 133.43 and 90.29 μmol/L at 24 h, respectively). In addition, TF3 triggers mitochondrial-mediated apoptosis, evidenced by ROS accumulation, loss of mitochondrial membrane potential, an elevated Bax/Bcl-2 ratio, cytochrome c release and enhanced PARP cleavage, and induces G2/M phase arrest. It also robustly inhibits HCC cell proliferation, invasion and migration, coinciding with downregulation of proteins governing cell cycle progression and invasive behavior. Transcriptome profiling coupled with enrichment analysis discovered that TF3 treatment differentially regulated 5009 genes, which were prominently enriched in pathways linked to apoptosis, cell cycle control, MAPK and PI3K/AKT signaling pathways. Western blotting analysis revealed that TF3 selectively suppresses phosphorylation of p38 and the PI3K/AKT cascade, activating JNK phosphorylation. In summary, our findings indicate that TF3 suppresses HCC proliferation by targeting Pin1, with attendant modulation of the MAPK and PI3K/AKT pathways, thereby presenting a potential candidate for targeted HCC therapy. Full article
(This article belongs to the Special Issue Antitumor Agents from Natural Sources 2026)
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14 pages, 4544 KB  
Article
Iberverin Downregulates GPX4 and SLC7A11 to Induce Ferroptotic Cell Death in Hepatocellular Carcinoma Cells
by Haoying Yang, Bolei Dai, Liangjie Chen, Yingping Li, Xiaorui Jin, Chengchang Gao, Linfen Han and Xueli Bian
Biomolecules 2024, 14(11), 1407; https://doi.org/10.3390/biom14111407 - 5 Nov 2024
Cited by 11 | Viewed by 5795
Abstract
Ferroptosis, a recently elucidated style of regulated cell death, has emerged as a significant area of investigation in cancer biology. Natural active compounds that have anti-cancer effects are promising candidates for cancer prevention. Iberverin, a natural compound derived from Brassica oleracea var. capitata [...] Read more.
Ferroptosis, a recently elucidated style of regulated cell death, has emerged as a significant area of investigation in cancer biology. Natural active compounds that have anti-cancer effects are promising candidates for cancer prevention. Iberverin, a natural compound derived from Brassica oleracea var. capitata, has been shown to exert anti-tumor activities in some cancers. However, its role in hepatocellular carcinoma (HCC) cells and the molecular mechanisms are still poorly understood. In this study, we proved that iberverin can induce intracellular reactive oxygen species (ROS) generation to inhibit cell proliferation and initiate ferroptotic cell death in HCC cells, which can be eradicated by the ferroptosis inhibitor ferrostatin-1 (Fer-1) or deferoxamine mesylate (DFO) and ROS scavenger (GSH or NAC). Mechanistically, iberverin treatment can simultaneously downregulate SLC7A11 mRNA level and degrade GPX4 through the ubiquitination pathway, leading to lipid peroxidation and ferroptotic cell death in HCC cells. Significantly, a low dose of iberverin can remarkably increase the sensitivity of HCC cells to ferroptosis induced by canonical ferroptosis inducers RSL3 and imidazole ketone erastin (IKE). This study uncovers a critical function of iberverin in preventing HCC through ferroptosis and provides a promising strategy for HCC treatment either via iberverin alone or in combination with canonical ferroptosis inducers in the future. Full article
(This article belongs to the Special Issue Antitumor Agents from Natural Sources 2026)
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Review

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35 pages, 6962 KB  
Review
The Antitumor Potential of Celastrol: Research Progress on Antitumor Mechanisms and Strategies for Toxicity Reduction with Efficacy Enhancement
by Qian Jiang, Zhaojing Liu, Jie Cheng, Zhiyuan Geng, Yu Gu, Yan Wei, Mengjia Yu and Yi Bi
Biomolecules 2026, 16(5), 620; https://doi.org/10.3390/biom16050620 - 22 Apr 2026
Viewed by 588
Abstract
Celastrol, a natural compound with potent antitumor activity, has gained considerable attention in drug research and development. Although its use is limited by high toxicity, a narrow therapeutic window, and severe side effects, studies show that celastrol can inhibit tumors through multiple targets [...] Read more.
Celastrol, a natural compound with potent antitumor activity, has gained considerable attention in drug research and development. Although its use is limited by high toxicity, a narrow therapeutic window, and severe side effects, studies show that celastrol can inhibit tumors through multiple targets and pathways, including by inducing apoptosis, autophagy, as well as suppressing invasion and adhesion. It also enhances antitumor effects by reshaping the immunosuppressive tumor microenvironment, regulating stromal components, and suppressing angiogenesis. This review systematically summarizes recent advances in related research and elaborates on the molecular mechanisms underlying the antitumor activity of celastrol and the key factors contributing to its toxicity. In addition, we further discuss current progress in research focused on reducing celastrol’s toxicity and enhancing its efficacy, aiming to promote its safety and druggability through rational structural modification, target optimization, and advanced formulation development. Full article
(This article belongs to the Special Issue Antitumor Agents from Natural Sources 2026)
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23 pages, 1998 KB  
Review
Astragalus membranaceus: A Traditional Chinese Medicine with Multifaceted Impacts on Breast Cancer Treatment
by Zhong Tang and Xuefei Tian
Biomolecules 2024, 14(10), 1339; https://doi.org/10.3390/biom14101339 - 21 Oct 2024
Cited by 18 | Viewed by 7051
Abstract
Breast cancer, the most prevalent malignant tumor among women globally, remains a critical area of focus for researchers striving to refine therapeutic approaches. As an important component of traditional Chinese medicine, Astragalus membranaceus (AM) has demonstrated potential for multifaceted impacts on breast cancer treatment [...] Read more.
Breast cancer, the most prevalent malignant tumor among women globally, remains a critical area of focus for researchers striving to refine therapeutic approaches. As an important component of traditional Chinese medicine, Astragalus membranaceus (AM) has demonstrated potential for multifaceted impacts on breast cancer treatment through various mechanisms. To guide clinical practice and further explore the under-researched field of AM in breast cancer treatment, this paper mainly reviews the regulatory roles of AM-derived compounds and extracts on breast cancer cell proliferation, migration, invasion, and chemoresistance. Furthermore, this study delves into the synergistic effects observed when AM is co-administered with chemotherapeutic agents, including the enhancement of chemosensitivity, mitigation of toxic side effects, and reversal of drug resistance. This review indicates that AM holds promise not only as a therapy in breast cancer treatment but also paves the way for innovative integrated treatment approaches that combine the benefits of traditional medicine with modern pharmaceuticals. Nevertheless, future research endeavors are also urged to elucidate the in vivo pharmacological effects and underlying mechanisms of AM to inform more effective clinical treatment strategies. Full article
(This article belongs to the Special Issue Antitumor Agents from Natural Sources 2026)
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