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Pharmaceuticals
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Therapeutic Potential of Chalcone Derivatives
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Therapeutic Potential of Chalcone Derivatives

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

Deadline for manuscript submissions: 10 November 2025 | Viewed by 2394

Special Issue Editor

Dr. Hélcio Silva Dos Santos

E-Mail Website
Guest Editor
Center for Exact Sciences and Technology—Chemistry Course, Vale do Acaraú University, Sobral, CE, Brazil
Interests: chalcones; natural products; antimicrobial activity; zebrafish; anxiolytic activity; spectroscopy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Chalcones are group of naturally occurring compounds, and they are precursors of flavonoids and important constituents of natural product such as fruits, vegetables, spices, and tea. Chemically chalcones have two aromatic rings linked by a highly electrophilic three-carbon α,β-unsaturated carbonyl system. The conjugated double bonds and completely delocated π-electron system present in chalcones showed relatively low redox potentials and greater probabilities of undergoing electron transfer reactions. Recently, studies have shown different pharmacological activities for chalcones, such as antimicrobial, antioxidant, antinociceptive, antiparasitic, antitumor, analgesic, antidepression, antiviral, anticonvulsant, antidiabetic, anti-inflammatory, neuroprotective, and anxiolytic activities.  We look forward to receiving your contributions.

Dr. Hélcio Silva Dos Santos
Guest Editor

Manuscript Submission Information

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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

  • chalcones
  • pharmacological potential
  • structural characterization
  • bioactivity
  • in silico study
  • cytotoxicity
  • quantum chemical calculations
  • ecapsulation

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Published Papers (2 papers)

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Research

19 pages, 2438 KiB  
Article
Microwave-Assisted Synthesis of Morpholine-Based Chalcones as Reversible MAO-A Inhibitors in the Management of Mental Depression
by Diksha Choudhary, Bhupinder Kumar, Balakumar Chandrasekaran, Thakur Gurjeet Singh, Rajwinder Kaur, Afaf Aldahish, Rajalakshimi Vasudevan and Prasanalakshmi Balaji
Pharmaceuticals 2025, 18(3), 309; https://doi.org/10.3390/ph18030309 - 23 Feb 2025
Viewed by 736
Abstract
Background: Depression is one of the most serious and common health problems among the youth population and is responsible for the initiation of many diseases. As per the World Health Organization, 3.8% of the population suffers from mental depression, globally. The monoamine oxidase-A [...] Read more.
Background: Depression is one of the most serious and common health problems among the youth population and is responsible for the initiation of many diseases. As per the World Health Organization, 3.8% of the population suffers from mental depression, globally. The monoamine oxidase-A (MAO-A) enzyme is responsible for the degradation of neurotransmitters leading to lower levels of neurotransmitters. Methods: Chalcones (C1-C15) were synthesized by reacting substituted acetophenone with various benzaldehydes in a basic ethanolic solvent at 80 °C under microwave irradiation conditions. To compare the reaction time and product yield, a conventional method of synthesis of chalcones was also performed. The synthesized chalcones (C1-C15) were spectroscopically characterized and screened initially for inhibitory activities against MAO-A and MAO-B. The best active compounds were undertaken for IC50 determination against MAO-A enzyme followed by the reversibility of inhibition analysis and the antioxidant assay. Moreover, in silico molecular docking and ADME pharmacokinetic investigations were accomplished. Results: Most of the compounds inhibited MAO-A, specifically, compounds C14 and C6 exhibited the highest inhibition at IC50 values of 7.91 ± 0.08 μM and 8.45 ± 0.19 μM, respectively. Both these compounds exhibited a reversible MAO-A inhibition displaying up to 60% recovery of enzymatic activity when diluted with substrate (Tyramine). The results of the in silico study indicated docking scores of −9.56 Kcal/mol (C14) and −9.45 Kcal/mol (C6) and exhibited a π-π stacking interaction with the crucial amino acid Trp-397. The compounds were determined to cross the blood–brain barrier (BBB) and displayed favorable gastrointestinal (GI) absorption. Further, the antioxidant assay results demonstrated that the synthesized compounds possess modest free radical scavenging potential. Conclusions: This study displayed the MAO-A inhibitory potential of morpholine-substituted chalcones as a promising pharmacophore for the development of novel antidepressant lead compounds. Full article
(This article belongs to the Special Issue Therapeutic Potential of Chalcone Derivatives)
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23 pages, 10010 KiB  
Article
Evaluation of Emulsification Techniques to Optimize the Properties of Chalcone Nanoemulsions for Antifungal Applications
by Joice Farias do Nascimento, Flavia Oliveira Monteiro da Silva Abreu, Taysse Holanda, Raquel Oliveira dos Santos Fontenelle, Júlio César Sousa Prado, Emmanuel Silva Marinho, Matheus Nunes da Rocha, Jesyka Macêdo Guedes, Bruno Coelho Cavalcanti, Wesley Lyeverton Correia Ribeiro, Márcia Machado Marinho and Helcio Silva dos Santos
Pharmaceuticals 2024, 17(11), 1442; https://doi.org/10.3390/ph17111442 - 28 Oct 2024
Viewed by 1153
Abstract
Background/Objectives: Nanoemulsions (NEs) possess properties that enhance the solubility, bioavailability and therapeutic efficacy of drugs. Chalcones are compounds known for their antifungal properties. In this study, we evaluated different emulsification techniques to create alginate nanoemulsions containing chalcone (1E,4E)-1,5-bis (4-methoxyphenyl) penta-1,4-dien-3-one (DB4OCH3). [...] Read more.
Background/Objectives: Nanoemulsions (NEs) possess properties that enhance the solubility, bioavailability and therapeutic efficacy of drugs. Chalcones are compounds known for their antifungal properties. In this study, we evaluated different emulsification techniques to create alginate nanoemulsions containing chalcone (1E,4E)-1,5-bis (4-methoxyphenyl) penta-1,4-dien-3-one (DB4OCH3). Our goal was to develop an antifungal formulation targeting Candida albicans strains. Methods: Ultrasound and ultrasound combined with high-speed homogenization techniques were used to prepare alginate-stabilized nanoemulsions. Particle size, zeta potential and encapsulation efficiency were evaluated. Additionally, in vitro release studies were conducted. Results: The combined emulsification technique produced stable nanoparticles with high encapsulation efficiency and antifungal activity, with a minimum inhibitory concentration of 8.75 μg/mL for the nanoemulsions compared to 312 µg/mL for free DB4OCH3. NEs’ effectiveness can be attributed to their ability to form nanodroplets efficiently, facilitating the solubilization of the chalcone in the oily phase. The particle size varied between 195.70 ± 2.69 and 243.40 ± 4.49 nm, with an increase in chalcone concentration leading to larger particle sizes. The zeta potential showed values from −91.77 ± 5.58 to −76.90 ± 4.44 mV. The UHS-7 sample exhibited an encapsulation efficiency of 92.10% ± 0.77, with a controlled in vitro release of 83% after 34 h. Molecular docking simulations showed that the aromatic nature of DB4OCH3 resulted in the formation of apolar interactions with aromatic residues located in the active site of the TMK, as observed in their respective co-crystallized inhibitors, within an affinity energy range that enables optimum specificity of the ligand for these two pathways. Pharmacokinetic analyses indicated high passive cell permeability and low hepatic clearance, and phase I metabolism reduces its oral bioavailability and metabolic stability, suggesting a promising active ingredient as an oral drug with control of the daily oral dose administered. Conclusions: The combined nanoemulsification technique led to the formation of finely dispersed nanodroplets that favored the solubilization of the chalcone in the oil phase, which led to a better performance in the antifungal properties. DB4OCH3 shows promise as an oral drug with controlled dosing. Full article
(This article belongs to the Special Issue Therapeutic Potential of Chalcone Derivatives)
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