Academic Journal
Novel (+)-usnic acid derivatives, computational studies and biological evaluation as neuroprotective agents.
| Τίτλος: | Novel (+)-usnic acid derivatives, computational studies and biological evaluation as neuroprotective agents. |
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| Συγγραφείς: | Kumar G; Department of Pharmacy, Vidya Vihar, Birla Institute of Technology and Science Pilani, Pilani, India., Kumar R; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research-Hyderabad, Hyderabad, India., Tanish; Department of Pharmacy, Vidya Vihar, Birla Institute of Technology and Science Pilani, Pilani, India., Singh SB; Department of Biological Sciences, National Institute of Pharmaceutical Education and Research-Hyderabad, Hyderabad, India.; Dr. B.R. Ambedkar Centre for Biomedical Research (ACBR), University of Delhi, Delhi, India. |
| Πηγή: | Future medicinal chemistry [Future Med Chem] 2026 Jun; Vol. 18 (12), pp. 1495-1515. Date of Electronic Publication: 2026 May 26. |
| Τύπος έκδοσης: | Journal Article; Research Support, Non-U.S. Gov't |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Taylor & Francis Country of Publication: England NLM ID: 101511162 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1756-8927 (Electronic) Linking ISSN: 17568919 NLM ISO Abbreviation: Future Med Chem Subsets: MEDLINE |
| Imprint Name(s): | Publication: 2024- : [Milton Park, Oxfordshire] : Taylor & Francis Original Publication: London : Future Science, 2009- |
| Ιατρικοί όροι (MeSH): | Neuroprotective Agents*/pharmacology , Neuroprotective Agents*/chemistry , Neuroprotective Agents*/chemical synthesis , Benzofurans*/pharmacology , Benzofurans*/chemistry , Benzofurans*/chemical synthesis, Reactive Oxygen Species/metabolism ; Nitric Oxide/metabolism ; Neuroglia/drug effects ; Neuroglia/metabolism ; Neuroglia/cytology ; Scopolamine/pharmacology ; Membrane Potential, Mitochondrial/drug effects ; Lipid Peroxidation/drug effects ; Antioxidants/pharmacology ; Antioxidants/chemistry ; Antioxidants/chemical synthesis ; Cell Survival/drug effects ; Animals ; Rats ; Structure-Activity Relationship ; Molecular Docking Simulation ; Cell Line |
| Περίληψη: | Aims: This study involves the semi-synthetic modification of (+)-usnic acid and the evaluation of the synthesized compounds for neuroprotective effects in scopolamine-injured C6 glial cells. Materials and Methods: Usnic acid derivatives were synthesized and characterized using 1H and 13C nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). Furthermore, compounds were evaluated for their neuroprotective effects using several biochemical assays, including acetylcholinesterase, lipid peroxidation, nitric oxide (NO), reduced glutathione (GSH), oxidized glutathione (GSSG), and GSH/GSSG, reactive oxygen species (ROS), NFkB-p65, proinflammatory cytokines, and mitochondrial membrane potential (MMP). In silico studies were conducted to predict drug-likeness and binding sites for these molecules. Results: (+)-Usnic acid, compounds 6, 13, and 16 showed antioxidative effects by decreasing ROS, malondialdehyde, and NO production in scopolamine-injured C6 glial cells. Additionally, these compounds enhanced the antioxidant effects by restoring the GSH/GSSG ratio and improving mitochondrial function by restoring the MMP in scopolamine-injured C6 glial cells. Moreover, these compounds exhibited anti-inflammatory effects by reducing IL-6 and tumor necrosis factor alpha (TNF-α) secretion and NFkB activity in C6 glial cells. In silico studies confirmed that these compounds decreased NO production by binding to neuronal nitric oxide synthase. Conclusion: Usnic acid and its derivatives, 6, 13, and 16, increased the survival of scopolamine-injured C6 glial cells. |
| Contributed Indexing: | Keywords: C6 glial cells; Usnic acid; neuroprotective; oxidative stress; pyrazole; scopolamine |
| Substance Nomenclature: | 0 (Neuroprotective Agents) 0W584PFJ77 (usnic acid) 0 (Benzofurans) 0 (Reactive Oxygen Species) 31C4KY9ESH (Nitric Oxide) DL48G20X8X (Scopolamine) 0 (Antioxidants) |
| Entry Date(s): | Date Created: 20260526 Date Completed: 20260610 Latest Revision: 20260726 |
| Update Code: | 20260726 |
| PubMed Central ID: | PMC13245065 |
| DOI: | 10.1080/17568919.2026.2675872 |
| PMID: | 42186692 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1756-8927 |
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| DOI: | 10.1080/17568919.2026.2675872 |