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Natural Products and Synthetic Derivatives in Cancer and Inflammatory Diseases

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: 20 November 2025 | Viewed by 3446

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Guest Editor
REQUIMTE/LAQV, Laboratório de Farmacognosia, Departamento de Química, Faculdade de Farmácia, Universidade do Porto, 4050-313 Porto, Portugal
Interests: natural products chemistry; marine natural products; ethnopharmacology; nuclear magnetic resonance; structure elucidation
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Special Issue Information

Dear Colleagues,

The role of natural products, particularly those derived from plants and microorganisms, in the development of new drugs is not limited to mere historical context. In fact, the increasing number of clinical candidates of natural origin spans virtually all pharmacotherapeutic classes. This trend is supported by the exploration of new natural product sources, the enhanced sensitivity of analytical techniques, the greater robustness of preclinical development methodologies, as well as the improved accuracy of virtual screening methodologies. This Special Issue aims to showcase cutting-edge research on natural products for anti-inflammatory and anticancer therapies, namely contributions ranging from initial studies on the chemical composition and pharmacological potential of uninvestigated natural sources to advanced preclinical research on new clinical candidates, whether naturally occurring or synthetic analogues. Reviews and original research articles focused on the following topics are particularly welcome:

  • Chemical characterization and evaluation of anti-inflammatory properties of medicinal plants based on ethnopharmacological approaches.
  • Chemical characterization and exploration of the anti-inflammatory and anticancer effects of less-studied microorganisms and marine organisms.
  • Discovery and structure elucidation of new chemical entities and the investigation of their in vitro and in vivo effects on targets and pathways related to inflammation and cancer.
  • Identification and analysis of molecular mechanisms in preclinical candidates and synthetic derivatives, including structure–activity relationship (SAR) studies.

Dr. Nelson G.M. Gomes
Guest Editor

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Keywords

  • angiogenesis inhibition
  • caspase activation
  • cytokine modulation
  • drug discovery
  • ethnopharmacology
  • plant metabolites
  • marine natural products
  • molecular docking
  • oxidative stress
  • tumor microenvironment

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Published Papers (2 papers)

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Research

21 pages, 4364 KiB  
Article
Fermented Kamut Wheat Diet Prevents DSS-Induced Colitis via Modulating Gut Microbiota in Mice
by Juni Lee, Bum Ju Kil, Yeojin Choi, Hyungyung Chai, Donghoon Lee, Hee-Geun Jo and Donghun Lee
Int. J. Mol. Sci. 2025, 26(7), 3017; https://doi.org/10.3390/ijms26073017 - 26 Mar 2025
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Abstract
Inflammatory bowel disease (IBD) is a chronic and relapsing inflammatory disorder of the gastrointestinal tract with limited treatment options. This study investigates the preventive effects of fermented Kamut wheat enzyme (FKW) diet on the progression of dextran sulfate sodium (DSS)-induced colitis in mice, [...] Read more.
Inflammatory bowel disease (IBD) is a chronic and relapsing inflammatory disorder of the gastrointestinal tract with limited treatment options. This study investigates the preventive effects of fermented Kamut wheat enzyme (FKW) diet on the progression of dextran sulfate sodium (DSS)-induced colitis in mice, with a focus on gut microbiota modulation and inflammatory cytokine regulation. Female C57BL/6J mice were divided into groups and fed a diet consisting of either a FKW diet (containing 39.80% FKW) or a control diet under 1.25% and 2.50% DSS conditions. The FKW diet was formulated based on the AIN-93G standard rodent formula, with the FKW diet providing comparable amounts of total proteins, crude lipids, and dietary fibers as the control diet. The FKW diet effectively mitigated the progression of colitis, as evidenced by improvements in key indicators such as dietary intake, body weight, colon length, stool consistency, and bleeding, particularly in the 1.25% DSS group. Histopathological analysis revealed preservation of colonic architecture and reduced mucosal damage in the FKW group. The diet also resulted in a significant reduction in pro-inflammatory cytokines (TNF-α, IL-6, IL-1β, and IFN-γ) and myeloperoxidase (MPO) levels, coupled with an increase in anti-inflammatory IL-10. Gut microbiota analysis showed increased abundance of beneficial bacteria such as Muribaculaceae, Lachnospiraceae NK4A136 and Bacteroides acidifaciens and decreased pathogenic bacteria like Escherichia/Shigella and Bilophila. These findings underscore the potential of FKW as a preventive dietary intervention for mitigating the progression of colitis, emphasizing the role of gut microbiota in supporting intestinal health. These results highlight FKW’s potential to reduce the risk of colitis development, providing a foundation for future research into its preventive applications. Full article
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23 pages, 8668 KiB  
Article
Methanolic Leaves Extract of Ziziphus spina-christi Inhibits Cell Proliferation and Migration of HER2-Positive Breast Cancer via p38 MAPK Signaling Pathway
by Sumayyah Saeed, Arij Fouzat Hassan, Azza Suliman, Ala-Eddin Al Moustafa and Feras Alali
Int. J. Mol. Sci. 2025, 26(2), 654; https://doi.org/10.3390/ijms26020654 - 14 Jan 2025
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Abstract
Human epidermal growth factor receptor 2 (HER2) is a subtype of breast cancer that is associated with poor prognosis and low survival rates. The discovery of novel anti-cancer agents to manage this subtype of cancer is still needed. Ziziphus spina-christi (ZSC) is [...] Read more.
Human epidermal growth factor receptor 2 (HER2) is a subtype of breast cancer that is associated with poor prognosis and low survival rates. The discovery of novel anti-cancer agents to manage this subtype of cancer is still needed. Ziziphus spina-christi (ZSC) is a plant species that is native to Qatar. It exerts various biological activities, including cytotoxicity as it contains different essential bioactive constituents, mainly rutin and quercetin. To examine the outcome of ZSC on HER2-positive breast cancer, we standardized the ZSC methanolic leaves extracted by Reverse Phase High-Performance Liquid Chromatography (RP-HPLC) analysis using the flavonoids rutin and quercetin as marker compounds. Here we used two HER2-positive breast cancer cell lines, ZR-75-1 and SK-BR-3, and the chorioallantoic membrane as an angiogenesis model. We found that ZSC extract significantly reduces viability, alters the normal morphological phenotype of HER2-positive breast cancer cells, and inhibits cell migration as well as colony formation; this is accompanied by deregulating different apoptotic markers such as Bax/Bcl-2 and NF-κB in both cell lines. Additionally, ZSC methanolic extract significantly represses the angiogenesis of the chorioallantoic membrane model. Moreover, the molecular pathway investigations pointed out that ZSC extract represses the activity of HER2 and p38 MAPK which could be the main pathways behind the effect of ZSC in HER2-positive cells. Collectively, our results support the potential role of ZSC in the management of HER2-positive breast cancer and form the basis for future investigations. Full article
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