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Pharmaceuticals
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Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology
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Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology

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

Deadline for manuscript submissions: 28 November 2025 | Viewed by 8466

Special Issue Editors

Dr. Marvin Antonio Soriano-Ursúa

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Guest Editor
Laboratorio de Neurofisiología, Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luis y Díaz Mirón s/n, Mexico City 11340, Mexico
Interests: boron; medicinal chemistry; drug design; GPCR; human physiology
Special Issues, Collections and Topics in MDPI journals
Dr. Andrei Biță

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Guest Editor
Department of Pharmacognosy, Faculty of Pharmacy, University of Medicine and Pharmacy of Craiova, 2 Petru Rareş Street, 200349 Craiova, Romania
Interests: natural products chemistry; boron containing compounds; chromatography; bioactivity analysis

Special Issue Information

Dear Colleagues,

Boron-containing compounds (BCCs) are gaining increasing attention in drug development due to their promising therapeutic potential. Currently, five BCCs—bortezomib, tavaborole, ixazomib, crisaborole, and vaborbactam—have been successfully developed into marketed drugs. Additionally, naturally occurring BCCs, such as boric acid, sodium tetraborate, and fructoborate, have shown bioactivity and have been proposed as pharmacophores for various medical applications. While many BCCs have been predominantly explored for their antimicrobial and anticancer properties, emerging research suggests they may hold therapeutic potential across a wider range of biomedical fields.

This Special Issue aims to highlight and compile new research on BCCs, whether discovered in nature or synthesized in the laboratory. We welcome studies focusing on the chemistry and bioactivity of these compounds, as well as investigations into their pharmacological (pharmacodynamics/pharmacokinetics) profiles, including those already in clinical use. We are also interested in medicinal chemistry studies involving BCCs, including but not limited to the design of novel formulations, biomaterials, and compounds with potential applications in the prevention, diagnosis, or treatment of diseases.

This Special Issue will serve as a platform to highlight recent advancements in the medicinal chemistry of boron-containing compounds and their evolving role in addressing unmet medical needs.

We look forward to your valuable contributions to this exciting and rapidly growing field.

Dr. Marvin Antonio Soriano-Ursúa
Dr. Andrei Biță
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

  • boron
  • drug development
  • drug discovery
  • bioactive boron compounds
  • bioinorganic chemistry
  • inorganic biological chemistry
  • synthesis
  • natural boron compounds
  • chemical characterization

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Published Papers (5 papers)

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Research

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19 pages, 2397 KB  
Article
Effects of Two Boron-Containing Compounds Structurally Related to Topiramate on Three Models of Drug-Induced Seizures in Mice
by Yaqui Valenzuela-Schejtman, Marvin A. Soriano-Ursúa, Elizabeth Estevez-Fregoso, Daniel García-López, R. Ivan Cordova-Chavez, Maricarmen Hernández-Rodríguez, Andrei Biță, Alejandra Contreras-Ramos, Miriam Hernández-Zamora and Eunice D. Farfán-García
Pharmaceuticals 2025, 18(10), 1470; https://doi.org/10.3390/ph18101470 - 30 Sep 2025
Viewed by 783
Abstract
Background: Epilepsy is a high-burden neurological disorder worldwide, and several sedative drugs are used as therapy. Topiramate is among the more recent drugs shown to be effective in some patients, although its benefits are limited. Two carbohydrate derivatives, FB1 (from D-fructose) and AB1 [...] Read more.
Background: Epilepsy is a high-burden neurological disorder worldwide, and several sedative drugs are used as therapy. Topiramate is among the more recent drugs shown to be effective in some patients, although its benefits are limited. Two carbohydrate derivatives, FB1 (from D-fructose) and AB1 (from D-arabinose), as well as phenylboronic acid, were recently reported as sedative and safe agents in mice. Their sedative properties and structural similarity to topiramate suggest potential antiseizure activity. Objective: The objective of this study was to evaluate the antiseizure potential of FB1 and AB1. Methods: Boron-containing compounds were administered to mice with seizures induced by pentylenetetrazol (a GABA-A receptor antagonist), 4-aminopyridine (a non-selective K+ channel blocker), or pilocarpine (a muscarinic agonist) to assess efficacy across models and explore potential mechanisms of action. Neuronal and glial toxicity was evaluated both in vitro and in vivo. Results: AB1 reduced seizure activity after intraperitoneal administration, whereas FB1 did not exhibit anticonvulsant effects, although it modified motor performance and limited neuronal loss. The effect of AB1 was comparable to that of topiramate across all three seizure models. Docking studies suggested that these compounds can interact with GABA-A (chloride), NMDA (glutamate), calcium, and potassium channels. Toxicity assays indicated that the concentrations required to affect neurons or glial cells were ≥300 µM, supporting the safety of these compounds. Conclusions: This preliminary evaluation demonstrates the antiseizure potential of AB1. Further experimental studies are needed to clearly establish its mechanism(s) of action. Full article
(This article belongs to the Special Issue Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology)
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18 pages, 5890 KB  
Article
Targeting Hippo Signaling Pathway with a Boron Derivative, Sodium Pentaborate Pentahydrate (NaB): Therapeutic Strategies in Colorectal Cancer
by Büşra Yüksel, Fikrettin Şahin and Nezaket Türkel
Pharmaceuticals 2025, 18(8), 1171; https://doi.org/10.3390/ph18081171 - 8 Aug 2025
Viewed by 635
Abstract
Background/Objectives: Colorectal cancer (CRC) remains a leading cause of cancer-related mortality globally, highlighting the urgent need for novel therapeutic strategies. This study aimed to investigate the anticancer potential of sodium pentaborate pentahydrate (NaB) in CRC by evaluating its effects on human colorectal [...] Read more.
Background/Objectives: Colorectal cancer (CRC) remains a leading cause of cancer-related mortality globally, highlighting the urgent need for novel therapeutic strategies. This study aimed to investigate the anticancer potential of sodium pentaborate pentahydrate (NaB) in CRC by evaluating its effects on human colorectal cancer cell lines and elucidating underlying molecular mechanisms. Methods: The cytotoxic and molecular effects of NaB were assessed in three human CRC cell lines (HCT-116, HT-29, and COLO-205) and one normal colon epithelial cell line (CCD-18CO). Cell viability assays were conducted to determine time- and dose-dependent responses. Apoptosis, cell cycle progression, colony formation, and migration capacity were evaluated. Gene and protein expression analyses were performed to examine apoptosis-related, DNA damage response, cell cycle, and Hippo signaling pathway components. Results: NaB significantly reduced cancer cell viability in a time- and dose-dependent manner, with minimal cytotoxicity to normal colon cells. It induced marked apoptosis, especially in HCT-116 and COLO-205 cells, and caused G2/M cell cycle arrest. In HCT-116 cells, NaB suppressed proliferation by downregulating PCNA and MKI-67 and reduced colony formation and migration. Molecular analyses revealed upregulation of pro-apoptotic BAX and downregulation of BCL-2, ATM, ATR, and cell cycle–related genes. NaB also inhibited oncogenic Hippo signaling by enhancing YAP1 phosphorylation and decreasing CTGF and CYR61 expression. Conclusions: These findings demonstrate that sodium pentaborate pentahydrate exerts selective anticancer effects on colorectal cancer cells through the induction of apoptosis, cell cycle arrest, and suppression of key oncogenic pathways. NaB represents a promising candidate for further development as a therapeutic agent in CRC treatment. Full article
(This article belongs to the Special Issue Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology)
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14 pages, 7660 KB  
Article
Boric Acid Protects the Uterus and Fallopian Tubes from Cyclophosphamide-Induced Toxicity in a Rat Model
by Enes Karaman and Adem Yavuz
Pharmaceuticals 2024, 17(12), 1716; https://doi.org/10.3390/ph17121716 - 19 Dec 2024
Viewed by 1882
Abstract
Background/Objectives: Cyclophosphamide (CP) is widely used for treating various cancers and autoimmune diseases, but it causes damage to reproductive organs due to oxidative stress (OS) and inflammation. Boric acid (BA) has antioxidant properties that may help reduce OS, which is critical for [...] Read more.
Background/Objectives: Cyclophosphamide (CP) is widely used for treating various cancers and autoimmune diseases, but it causes damage to reproductive organs due to oxidative stress (OS) and inflammation. Boric acid (BA) has antioxidant properties that may help reduce OS, which is critical for preserving uterine functionality, particularly for cancer patients considering pregnancy after cryopreservation. This study aimed to determine whether BA could diminish CP-induced toxicity in the uterus and fallopian tubes (FT) using CP-induced toxicity in a rat model. Methods: Forty female Wistar rats, aged 18–20 weeks, were divided into four groups as follows: control, oral BA (OBR), CP, and CP plus OBR (CP + OBR). The toxicity was induced in the CP and CP + OBR groups with an initial dose of 200 mg/kg CP, followed by 8 mg/kg daily for 14 days. Rats in the OBR and CP + OBR groups received 20 mg/kg/day of BA. After the 16-day experiment, tissues were collected for analysis. Results: Histopathological and immunohistochemical assessments of IL-6 and HIF-1α expressions were used to evaluate inflammation and OS. The control, OBR, and CP + OBR groups maintained normal tissue features, while the CP group showed epithelial cell shedding, vacuolization, degenerative endometrial glands, lymphocyte infiltration, and reduced collagen fiber density. Elevated HIF-1α and IL-6 expressions in the uterus and FT indicated significant OS and inflammation. Conclusions: The study concluded that BA supplementation in CP-treated rats effectively reduced CP-induced uterine and FT damage, suggesting the potential protective role of BA in managing CP-associated toxicity. Full article
(This article belongs to the Special Issue Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology)
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Review

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28 pages, 1526 KB  
Review
Microbiota-Accessible Borates as Novel and Emerging Prebiotics for Healthy Longevity: Current Research Trends and Perspectives
by Andrei Biţă, Ion Romulus Scorei, Marvin A. Soriano-Ursúa, George Dan Mogoşanu, Ionela Belu, Maria Viorica Ciocîlteu, Cristina Elena Biţă, Gabriela Rău, Cătălina Gabriela Pisoschi, Maria-Victoria Racu, Iurie Pinzaru, Alejandra Contreras-Ramos, Roxana Kostici, Johny Neamţu, Viorel Biciuşcă and Dan Ionuţ Gheonea
Pharmaceuticals 2025, 18(6), 766; https://doi.org/10.3390/ph18060766 - 22 May 2025
Viewed by 2874
Abstract
Precision nutrition-targeted gut microbiota (GM) may have therapeutic potential not only for age-related diseases but also for slowing the aging process and promoting longer healthspan. Recent studies have shown that restoring a healthy symbiosis of GM by counteracting dysbiosis (DYS) through precise nutritional [...] Read more.
Precision nutrition-targeted gut microbiota (GM) may have therapeutic potential not only for age-related diseases but also for slowing the aging process and promoting longer healthspan. Recent studies have shown that restoring a healthy symbiosis of GM by counteracting dysbiosis (DYS) through precise nutritional intervention is becoming a major target for extending healthspan. Microbiota-accessible borate (MAB) complexes, such as boron (B)–pectins (rhamnogalacturonan–borate) and borate–phenolic esters (diester chlorogenoborate), have a significant impact on healthy host–microbiota symbiosis (HMS). The mechanism of action of MABs involves the biosynthesis of the autoinducer-2–borate (AI-2B) signaling molecule, B fortification of the mucus gel layer by the MABs diet, inhibition of pathogenic microbes, and reversal of GM DYS, strengthening the gut barrier structure, enhancing immunity, and promoting overall host health. In fact, the lack of MAB complexes in the human diet causes reduced levels of AI-2B in GM, inhibiting the Firmicutes phylum (the main butyrate-producing bacteria), with important effects on healthy HMS. It can now be argued that there is a relationship between MAB-rich intake, healthy HMS, host metabolic health, and longevity. This could influence the deployment of natural prebiotic B-based nutraceuticals targeting the colon in the future. Our review is based on the discovery that MAB diet is absolutely necessary for healthy HMS in humans, by reversing DYS and restoring eubiosis for longer healthspan. Full article
(This article belongs to the Special Issue Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology)
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Other

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19 pages, 3424 KB  
Perspective
Boronate-Based Inhibitors of Penicillin-Binding Proteins: An Underestimated Avenue for Antibiotic Discovery?
by Valentina Villamil, Luca Svolacchia Brusoni, Fabio Prati, Emilia Caselli and Nicolò Santi
Pharmaceuticals 2025, 18(9), 1325; https://doi.org/10.3390/ph18091325 - 4 Sep 2025
Viewed by 852
Abstract
Penicillin-binding proteins (PBPs) are essential enzymes involved in bacterial cell wall biosynthesis and represent the primary targets of β-lactam antibiotics. However, the efficacy of these agents is threatened by β-lactamase production and PBP alterations, prompting the search for alternative strategies. In this context, [...] Read more.
Penicillin-binding proteins (PBPs) are essential enzymes involved in bacterial cell wall biosynthesis and represent the primary targets of β-lactam antibiotics. However, the efficacy of these agents is threatened by β-lactamase production and PBP alterations, prompting the search for alternative strategies. In this context, boronic acids, long established as potent inhibitors of serine β-lactamases (SBLs), have been proposed as scaffolds for PBP inhibition based on the shared structural and mechanistic features of these enzyme families. This perspective provides a literature-based survey with structural analysis to evaluate emerging evidence on the potential role of boronic acids as PBP-targeting agents, with a particular focus on peptidomimetic boronic acids, repurposed β-lactamase inhibitors, and novel scaffold architectures. While early work showed limited activity against low-molecular-mass PBPs, more recent compounds, particularly certain bicyclic boronates, have demonstrated potent binding and, in some cases, antibacterial activity. Structural analyses reveal diverse binding modes and underscore the role of conformational dynamics in modulating affinity. Despite these advances, significant challenges remain, including target selectivity, membrane permeability, and species-specific differences. Nevertheless, the direct inhibition of PBPs by boronic acids, while still in early development, may offer a viable complement or alternative to β-lactam therapy, warranting further exploration through structure-guided design and comprehensive biological evaluation. Here, we analyze the potential of boronic acid inhibitors (BAIs) to target PBP enzymes, considering their promise as non-β-lactam antimicrobial agents with possible clinical relevance. Full article
(This article belongs to the Special Issue Boron-Containing Compounds: Identification, Synthesis, Biological Actions and Pharmacology)
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