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Pharmaceuticals
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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 2180

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 (3 papers)

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25 pages, 3468 KB  
Article
Baicalin–Myricetin-Coated Selenium Nanoparticles Mitigate Pathology in an Aβ1-42 Mice Model of Alzheimer’s Disease
by Rosa Martha Pérez Gutiérrez, Julio Téllez Gómez, José María Mota Flores, Mónica Corea Téllez and Alethia Muñiz Ramírez
Pharmaceuticals 2025, 18(9), 1391; https://doi.org/10.3390/ph18091391 - 17 Sep 2025
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Abstract
Background: Current Alzheimer’s disease (AD) treatments primarily focus on symptom management and offer limited potential to arrest disease progression. To address this limitation, we developed baicalin–myricetin (BM) functionalized selenium nanoparticles (SeNPs), termed BMSe@BSA, aimed at multi-targeted neuroprotection. Materials and Methods: BMSe@BSA [...] Read more.
Background: Current Alzheimer’s disease (AD) treatments primarily focus on symptom management and offer limited potential to arrest disease progression. To address this limitation, we developed baicalin–myricetin (BM) functionalized selenium nanoparticles (SeNPs), termed BMSe@BSA, aimed at multi-targeted neuroprotection. Materials and Methods: BMSe@BSA nanoparticles were synthesized via a gel–sol technique using bovine serum albumin (BSA), ascorbic acid, selenous acid, and BM. Interactions among BSA, BM, and SeNPs were characterized by microscopy and spectrometry. Cytotoxicity was assessed on RAW 264.7 and PC12 cells to determine biocompatibility. Neuroinflammation and cognitive function were evaluated in C57BL6/J mice challenged with Aβ1-42. Recognition memory was tested through open-field exploration, novel object recognition (NOR), and T-maze assays. Inflammatory markers (IL-1β and TNF-α) and microglial changes in the cerebral cortex were quantified, while amyloid fibril morphology was assessed using atomic force microscopy (AFM). Results: Spectroscopic analysis verified successful BM functionalization. Transmission electron microscopy revealed a spherical morphology with an average particle size of 90.57 nm, zeta potential of 27.2 mV, and a polydispersity index (PDI) of 0.270. BM entrapment efficiency reached approximately 90%. Cytotoxicity assays confirmed the nanoparticles’ safety, with no toxicity observed at concentrations up to 400 µg/mL after 4 h of incubation. BMSe@BSA effectively inhibited amyloid fibril formation, downregulated pro-inflammatory cytokine expression, preserved neuronal integrity, and significantly enhanced cognitive performance in AD mouse models. Conclusion: BMSe@BSA appear as a potential nanotherapeutic approach for targeted brain delivery and multi-pathway intervention in Alzheimer’s disease. Full article
(This article belongs to the Special Issue Pharmacological Activities of Flavonoids and Their Analogues, Third Edition)
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36 pages, 11682 KB  
Article
Isoliquiritigenin as a Neuronal Radiation Mitigant: Mitigating Radiation-Induced Anhedonia Tendency Targeting Grik3/Grm8/Grin3a via Integrated Proteomics and AI-Driven Discovery
by Boyang Li, Suqian Cheng, Han Zhang and Bo Li
Pharmaceuticals 2025, 18(9), 1307; https://doi.org/10.3390/ph18091307 - 30 Aug 2025
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Abstract
Background/Objectives: Radiotherapy can cause severe and irreversible brain damage, including cognitive impairment, increased dementia risk, debilitating depression, and other neuropsychiatric disorders. Current radioprotective drugs face limitations, such as single-target inefficacy or manufacturing hurdles. Isoliquiritigenin (ISL), a natural flavonoid derived from licorice root, [...] Read more.
Background/Objectives: Radiotherapy can cause severe and irreversible brain damage, including cognitive impairment, increased dementia risk, debilitating depression, and other neuropsychiatric disorders. Current radioprotective drugs face limitations, such as single-target inefficacy or manufacturing hurdles. Isoliquiritigenin (ISL), a natural flavonoid derived from licorice root, exhibits broad bioactivities. It exhibits anti-inflammatory, anti-cancer, immunoregulatory, hepatoprotective, and cardioprotective activities. This study aimed to elucidate ISL’s neuronal radiation mitigation effects and key targets. Methods: In vitro and in vivo models of radiation-induced neuronal injury were established. ISL’s bioactivities were evaluated through cellular cytotoxicity assays, LDH release, ROS, ATP, glutamate, and GSH levels. In vivo, ISL’s radiation mitigation effect was evaluated with sucrose preference test, IL-β level, histopathological analysis, and Golgi-Cox staining analysis. Proteomics, pathway enrichment, and ensemble models (four machine learning models, weighted gene co-expression network, protein–protein interaction) identified core targets. Molecular docking and dynamic simulations validated ISL’s binding stability with key targets. Results: ISL attenuated radiation-induced cellular cytotoxicity, reduced LDH/ROS, restored ATP, elevated GSH, and mitigated glutamate accumulation. In rats, ISL alleviated anhedonia-like phenotypes and hippocampal synaptic loss. ISL also significantly suppressed radiation-induced neuroinflammation, as evidenced by reduced levels of the pro-inflammatory cytokine IL-1β. Proteomic analysis revealed that ISL’s main protective pathways included the synaptic vesicle cycle, glutamatergic synapse, MAPK signaling pathway, SNARE interactions in vesicular transport, insulin signaling pathway, and insulin secretion. Grm8, Grik3, and Grin3a were identified as key targets using the integrated models. The expression of these targets was upregulated post-radiation and restored by ISL. Molecular docking and dynamic simulations indicated that ISL showed stable binding to these receptors compared to native ligands. Conclusions: ISL demonstrates multi-scale radiation mitigation activities in vitro and in vivo by modulating synaptic and inflammatory pathways, with glutamate receptors as core targets. This work nominates ISL as an important natural product for mitigating radiotherapy-induced neural damage. Full article
(This article belongs to the Special Issue Pharmacological Activities of Flavonoids and Their Analogues, Third Edition)
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Other

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38 pages, 2064 KB  
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
Cited by 1 | Viewed by 813
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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