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Coumarins as Effective Therapeutic Agents: Mechanism of Action and Diverse Activity

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pathology, Diagnostics, and Therapeutics".

Deadline for manuscript submissions: 20 July 2025 | Viewed by 2436

Special Issue Editor

Dr. Jarosław Widelski

E-Mail Website
Guest Editor
Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Lublin, 1 Chodźki Street, 20-093 Lublin, Poland
Interests: furanocoumarins; pyranocoumarins; simple coumarins, anti-inflammatory properties; cytotoxic activity; antitumor activity; antimicrobial acitivity; bioactivity of compounds; anxiolytic activity; neuroprotective properties; bioactive metabolites; medicinal plants
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Coumarins are heterocyclic compounds belonging to the class of benzopyrenes, found in various plants, fungi and microorganisms. Coumarins and their derivatives show great chemical diversity and include furanocoumarins, pyranocoumarins, as well as simple coumarins. These natural compounds exhibit bioactive properties such as anticoagulant, antimicrobial, anti-inflammatory, antioxidant, antimalarial, anticancer, antiviral and enzyme inhibitory effects, including acetylcholinesterase, COX or tyrosinase. In recent years, there has been an increasing number of reports on the activity of coumarins in the central nervous system, and they have exhibited neuroprotective, anticonvulsant and anti-anxiety effects.

This Special Issue will include a selection of articles highlighting the current challenges in phytochemical research on coumarins and determining their pharmacological activity and possible applications.

The theme of the issue will be innovative approaches to understanding the molecular mechanisms underlying the pharmacological activity of coumarins, which can be used in the treatment and prevention of many diseases. We invite you to participate in this Special Issue by submitting original research, short communications and review manuscripts. This is a great opportunity to contribute to the search for new natural medicines.

Dr. Jarosław Widelski
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • furanocoumarins
  • pyranocoumarins
  • simple coumarins
  • anti-inflammatory properties
  • cytotoxic activity
  • antitumor activity
  • antimicrobial acitivity
  • bioactivity of compounds
  • anxiolytic activity
  • neuroprotective properties
  • bioactive metabolites
  • medicinal plants

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Published Papers (2 papers)

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Research

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13 pages, 16048 KiB  
Article
Characterization of the Antiproliferative and Antimetastatic Properties of Centrapalus pauciflorus Meroterpenoid Centrapalus Coumarin F
by Hazhmat Ali, Shelan Rasool, Muhammad Bello Saidu, Péter Germán, Gábor J. Szebeni, Enikő Szabó, Dóra Rédei, Judit Hohmann and István Zupkó
Int. J. Mol. Sci. 2025, 26(10), 4489; https://doi.org/10.3390/ijms26104489 - 8 May 2025
Viewed by 608
Abstract
The current study examined the in vitro antineoplastic potentials of centrapalus coumarin F (CCF) obtained from aerial parts of Centrapalus pauciflorus (Willd.) H.Rob. (Asteraceae). Cytotoxic activity was tested against a panel of human adherent cancer cell lines, including breast, cervical, and oropharyngeal cancer [...] Read more.
The current study examined the in vitro antineoplastic potentials of centrapalus coumarin F (CCF) obtained from aerial parts of Centrapalus pauciflorus (Willd.) H.Rob. (Asteraceae). Cytotoxic activity was tested against a panel of human adherent cancer cell lines, including breast, cervical, and oropharyngeal cancer and glioblastoma. Cell cycle analyses using flow cytometry and Hoechst 33258-propidium iodide (HOPI) fluorescent double staining were used to describe the proapoptotic property of CCF. Wound healing assessment and the Boyden chamber assay were performed to characterize the antimetastatic action of the compound. The firefly luciferase assay was applied to clarify the action of CCF on estrogenic receptors. CCF demonstrated remarkable selective growth inhibition against the HPV-18-positive human cervical cancer cell line HeLa (IC50 = 2.28 µM). The compound elicited crucial markers of apoptosis, inhibited the migration and invasion capacity of HeLa cells, and demonstrated an antiestrogenic property. Our current data indicate that the meroterpenoid scaffold presented here displays remarkable antiproliferative and antimetastatic effects on HeLa cells and can be considered a valuable model for designing further analogs targeting cervical carcinoma. Full article
(This article belongs to the Special Issue Coumarins as Effective Therapeutic Agents: Mechanism of Action and Diverse Activity)
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Review

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34 pages, 5416 KiB  
Review
Zebrafish as a Suitable Model for Utilizing the Bioactivity of Coumarins and Coumarin-Based Compounds
by Joanna Lachowicz-Radulska, Jarosław Widelski, Filip Nowaczyński, Anna Serefko, Jan Sobczyński, Agnieszka Ludwiczuk, Natalia Kasica and Aleksandra Szopa
Int. J. Mol. Sci. 2025, 26(4), 1444; https://doi.org/10.3390/ijms26041444 - 8 Feb 2025
Cited by 2 | Viewed by 1247
Abstract
The aim of this review is to summarize the current knowledge on the use of coumarin-derived compounds in the zebrafish (Danio rerio) model. Coumarins, a class of naturally occurring compounds with diverse biological activities, including compounds such as coumarin, angelicin, and [...] Read more.
The aim of this review is to summarize the current knowledge on the use of coumarin-derived compounds in the zebrafish (Danio rerio) model. Coumarins, a class of naturally occurring compounds with diverse biological activities, including compounds such as coumarin, angelicin, and warfarin, have attracted considerable attention in the study of potential therapeutic agents for cancer, central nervous system disorders, and infectious diseases. The capabilities of coumarins as active compounds have led to synthesizing various derivatives with their own properties. While such variety is certainly promising, it is also cumbersome due to the large amount of research needed to find the most optimal compounds. The zebrafish model offers unique advantages for such studies, including high genetic and physiological homology to mammals, optical transparency of the embryos, and rapid developmental processes, facilitating the assessment of compound toxicity and underlying mechanisms of action. This review provides an in-depth analysis of the chemical properties of coumarins, their mechanisms of biological activity, and the results of previous studies evaluating the toxicity and efficacy of these compounds in zebrafish assays. The zebrafish model allows for a holistic assessment of the therapeutic potential of coumarin derivatives, offering valuable insights for advancing drug discovery and development. Full article
(This article belongs to the Special Issue Coumarins as Effective Therapeutic Agents: Mechanism of Action and Diverse Activity)
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