Butyrylcholinesterase (BChE) is a crucial hydrolytic enzyme predominantly synthesized in the liver, playing a significant role in conditions like liver disorders, diabetes, Alzheimer's disease, and fat metabolism regulation. This study aims to address the current limitations in visualizing BChE activity in diseases at various states by introducing an ultra-sensitive near-infrared fluorescent probe, FDCM-BChE. The probe was engineered to have several properties, such as a large Stokes shift, rapid response time, high stability, excellent selectivity, and low detection limits. We validated the efficacy of FDCM-BChE in quantifying BChE activity in human serum and leveraged its low cytotoxicity for cellular imaging. The study revealed the downregulation of BChE activity in liver cancer and hepatic injury and the upregulation in diabetes. Thus, FDCM-BChE shows promise as a tool for specific applications, providing insights into diseases associated with BChE activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.saa.2023.123801 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Mechanism of dsDNA binding, enzyme inhibition, antioxidant activities, and molecular docking studies of taxifolin, daidzein, and S-equol.
Int J Biol Macromol
January 2025
Afsin Vocational School, Department of Chemistry and Chemical Processing Technologies, Kahramanmaras Sutcu Imam University, Kahramanmaras, Turkey. Electronic address:
This study investigated the binding mechanism of taxifolin (TA), daidzein (DA), and S-equol (SQ) flavonoids with fish sperm double helix DNA (dsDNA) under the simulated physiological pH condition using UV-Vis and photoluminescence spectroscopy, as well as viscometric methods. Binding constants (K) for the flavonoids to dsDNA were determined as 1.8 × 10 M for SQ, 1.
View Article and Find Full Text PDFSpecific Rosetta-based protein-peptide prediction protocol allows the design of novel cholinesterase inhibitor peptides.
Bioorg Chem
January 2025
Laboratorio de Peptidos Bioactivos, Department of Organic Chemistry, Faculty of Biochemistry and Biological Sciences, National University of the Littoral, Ciudad Universitaria UNL, 3000 Santa Fe, Argentina; National Scientific and Technical Research Council (CONICET), Ministry of Science, Technology and Innovation, Godoy Cruz 2290, Ciudad de Buenos Aires, Argentina. Electronic address:
The search for novel cholinesterase inhibitors is essential for advancing treatments for neurodegenerative disorders such as Alzheimer's disease (AD). In this study, we employed the Rosetta pepspec module, originally developed for designing peptides targeting protein-protein interactions, to design de novo peptides targeting the peripheral aromatic site (PAS) of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). A total of nine peptides were designed for human AChE (hAChE), T.
View Article and Find Full Text PDFResveratrol-Based Carbamates as Selective Butyrylcholinesterase Inhibitors: Design, Synthesis, Computational Study and Biometal Complexation Capability.
Molecules
January 2025
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.
Considering our previous experience in the design of new cholinesterase inhibitors, especially resveratrol analogs, in this research, the basic stilbene skeleton was used as a structural unit for new carbamates designed as potentially highly selective butyrylcholinesterase (BChE) inhibitors with excellent absorption, distribution, metabolism, excretion and toxicity ADMET properties. The inhibitory activity of newly prepared carbamates - was tested toward the enzymes acetylcholinesterase (AChE) and BChE. In the tested group of compounds, the leading inhibitors were and , which achieved excellent selective inhibitory activity for BChE with IC values of 0.
View Article and Find Full Text PDFCardiac acetylcholinesterase and butyrylcholinesterase have distinct localization and function.
Am J Physiol Heart Circ Physiol
January 2025
Comenius University Bratislava, Faculty of Pharmacy, Department of Pharmacology and Toxicology, Bratislava, Slovakia.
Cholinesterase (ChE) inhibitors are under consideration to be used in the treatment of cardiovascular pathologies. A prerequisite to advancing ChE inhibitors into the clinic is their thorough characterization in the heart. The aim here was to provide a detailed analysis of cardiac ChE to understand their molecular composition, localization, and physiological functions.
View Article and Find Full Text PDFComprehensive Analysis of the Antioxidant and Enzyme Inhibitory Properties and Phenolic Compounds of Phlomis armeniaca: Potential Applicant in Neurodegenerative Diseases.
Chem Biodivers
January 2025
Gümüşhane Üniversitesi: Gumushane Universitesi, GUMUSHANE HEALTH SERVICES VOCATIONAL SCHOOL, Gumushane University, Vocational School of Health Services, 29100, Gumushane, Tü, Gümüşhane, TURKEY.
This study investigates the antioxidant and enzyme inhibitory properties of Phlomis armeniaca, a perennial plant native to the eastern and southeastern regions of Türkiye. Ethanol extracts of the plant were analyzed using various bioanalytical methods, including Fe³⁺-Fe²⁺ reducing power, CUPRAC, DPPH, and ABTS radical scavenging activities, as well as total phenolic and flavonoid content assessments. The results showed that Phlomis armeniaca is rich in phenolic (38.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!