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Pharmaceuticals
Special Issues
Pharmacological Activities of Flavonoids and Their Analogues, Third Edition
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Pharmacological Activities of Flavonoids and Their Analogues, Third Edition

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: 25 November 2025 | Viewed by 426

Special Issue Editors

Dr. Fernando Calzada

E-Mail Website
Guest Editor
Medical Research Unit in Pharmacology, Speciality Hospital, National Medical Center Siglo XXI, Av. Cuauhtémoc 330 Col Doctores, México City CP 06725, Mexico
Interests: pharmacognosy of Mexican medicinal plants; diabetes mellitus; cancer; diarrhea; molecular docking; secondary metabolites
Special Issues, Collections and Topics in MDPI journals
Dr. Miguel Valdes

E-Mail Website
Guest Editor
Medical Research Unit in Pharmacology, Speciality Hospital, National Medical Center Siglo XXI, Av. Cuauhtémoc 330 Col Doctores, Mexico City CP 06725, Mexico
Interests: pharmacology; pharmacognosy; phytochemistry; medicinal plants; diabetes mellitus; cancer; diarrhea; drug development; isolation of natural compounds; terpenoids; flavonoids; molecular docking; molecular mechanism elucidation; pharmacological evaluation of natural compounds isolated from plants used in traditional Mexican medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The development of new drugs continues to be important for the health of global society. In recent years, there has been increased interest in the study of polyphenols due to the multiple pharmacological activities that they demonstrate. Flavonoids are a class of polyphenols that have been widely studied; they are characterized as having a 15-C skeleton with a 2-phenylbenzopyranone core structure. They are classified as flavones, isoflavones, flavonols, anthocyanidins, flavanones, flavanols, chalcones, and aurones. Within the various classes, further differentiation is possible based on the number and nature of substituent groups attached to the rings. Moreover, flavonoids can exist as free aglycones or conjugated glycosidic bonds. Flavonoids are present in almost all types of nourishment, and recent studies have focused on their biological, nutritional, pharmacological, and medicinal relevance. These kind of molecules and their analogues are of the utmost relevance due to their multiple applications. Considering the above, we invite researchers to publish their findings regarding the pharmacological applications of flavonoids and their analogs, while also highlighting the importance of using these molecules as a basis for the development of new drugs.

We look forward to your contributions.

Dr. Fernando Calzada
Dr. Miguel Valdes
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. Pharmaceuticals 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

  • natural products
  • polyphenols
  • flavonoids
  • medicinal chemistry
  • traditional medicine
  • flavonoids isolation
  • flavonoids identification
  • flavonoids pharmacology
  • flavonoids as prodrugs
  • in vivo, in vitro, and in silico studies
  • molecular modeling studies

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Published Papers (1 paper)

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38 pages, 2064 KiB  
Systematic Review
Humulus lupulus (Hop)-Derived Chemical Compounds Present Antiproliferative Activity on Various Cancer Cell Types: A Meta-Regression Based Panoramic Meta-Analysis
by Georgios Tsionkis, Elisavet M. Andronidou, Panagiota I. Kontou, Ioannis A. Tamposis, Konstantinos Tegopoulos, Panagiotis Pergantas, Maria E. Grigoriou, George Skavdis, Pantelis G. Bagos and Georgia G. Braliou
Pharmaceuticals 2025, 18(8), 1139; https://doi.org/10.3390/ph18081139 - 31 Jul 2025
Viewed by 239
Abstract
Background/Objectives: Humulus lupulus (hops) are a perennial, dioecious plant widely cultivated for beer production, used for their distinguishing aroma and bitterness—traits that confer high added value status. Various hop-derived compounds have been reported to exhibit antioxidant, antimicrobial, antiproliferative and other bioactive effects. [...] Read more.
Background/Objectives: Humulus lupulus (hops) are a perennial, dioecious plant widely cultivated for beer production, used for their distinguishing aroma and bitterness—traits that confer high added value status. Various hop-derived compounds have been reported to exhibit antioxidant, antimicrobial, antiproliferative and other bioactive effects. This systematic review and meta-analysis assesses the impact of hop compounds on the viability of diverse cancer cell lines. Methods: A comprehensive literature search was performed following PRISMA guidelines. Data were synthesized via multivariate meta-analysis and meta-regression, using IC50 values as the effect size. Key variables included assay type (SRB, tetrazolium salt-based, crystal violet), exposure duration (24, 48, 72 h), specific hop compound and cancer cell line. Results: Of 622 articles identified, 61 met eligibility criteria, yielding 354 individual experiments. Meta-regression of xanthohumol (XN) IC50 values across SRB, tetrazolium and crystal violet assays revealed no statistically significant differences at 24 h (p = 0.77), 48 h (p = 0.35) and 72 h (p = 0.70), supporting the interchangeability of the methods. Meta-analysis confirmed that hop constituents inhibit cancer cell proliferation; XN emerged as the most potent flavonoid (IC50 = 16.89 μM at 72 h), while lupulone was the strongest compound overall (IC50 = 5.00 μM at 72 h). Crude hop extracts demonstrated greater antiproliferative selectivity for cancer versus non-cancer cells (IC50 = 35.23 vs. 43.80 μg/mL at 72 h). Conclusions: Hop compounds, and particularly bitter acids, demonstrate promising antiproliferative activity against cancer cells with comparatively low toxicity to healthy cells. Furthermore, our analysis confirms the comparability of SRB, tetrazolium-based and crystal violet assays, supporting the robust integration of antiproliferative data. Full article
(This article belongs to the Special Issue Pharmacological Activities of Flavonoids and Their Analogues, Third Edition)
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