Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 μM concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC(50) value of 121 ± 3 μM was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013380 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2010.10.139 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Deciphering the impact of NOS-derived NO on nitrogen metabolism and carbon flux in the heterocytous cyanobacterium Aphanizomenon flos-aquae 2012/KM1/D3.
Plant Physiol Biochem
January 2025
Laboratory of Microbial Genetics, Department of Botany, Institute of Science, Banaras Hindu University, Varanasi, 221005, India. Electronic address:
Nitric oxide synthases (NOSs) are heme-based monooxygenases that catalyze the NADPH-dependent oxidation of L-arginine to produce NO and L-citrulline. Over the past five years, the identification and characterization of NOS homologs in cyanobacteria have significantly advanced our understanding of these enzymes. However, the precise mechanisms through which NOS-derived NO influences nitrogen metabolism remain incompletely elucidated.
View Article and Find Full Text PDFImpact of disease duration and surgical intervention on arousal networks in temporal lobe epilepsy.
J Neurosurg
January 2025
Departments of1Biomedical Engineering.
Objective: Epilepsy is a common neurological disease affecting nearly 1% of the global population, and temporal lobe epilepsy (TLE) is the most common type. Patients experience recurrent seizures and chronic cognitive deficits that can impact their quality of life, ability to work, and independence. These cognitive deficits often extend beyond the temporal lobe and are not well understood.
View Article and Find Full Text PDFAmphibian-Derived Peptides as Natural Inhibitors of SARS-CoV-2 Main Protease (Mpro): A Combined In Vitro and In Silico Approach.
Chem Biodivers
January 2025
Universidad Nacional del Litoral Facultad de Bioquimica y Ciencias Biologicas, Química Orgánica, Ciudad Universitaria. Paraje el Pozo S/N, Argentina, 3000, Santa Fe, ARGENTINA.
The COVID-19 pandemic, caused by the SARS-CoV-2 virus, has highlighted the urgent need for novel therapeutic agents targeting viral enzymes such as the main protease (Mpro), which plays a crucial role in viral replication. In this study, we investigate the inhibitory potential of 23 peptides isolated from the skin of amphibians belonging to the Hylidae and Leptodactylidae families against SARS-CoV-2 Mpro. Five peptides demonstrated significant inhibition using a colorimetric Mpro inhibition assay, with IC50 values ranging from 41 to 203 µM.
View Article and Find Full Text PDFPhosphorylation-dependent VaMYB4a regulates cold stress in grapevine by inhibiting VaPIF3 and activating VaCBF4.
Plant Physiol
January 2025
School of Life Science, Ningxia University, Yinchuan 750021, Ningxia, China.
Cold stress severely impacts the quality and yield of grapevine (Vitis L.). In this study, we extend our previous work to elucidate the role and regulatory mechanisms of Vitis amurensis MYB transcription factor 4a (VaMYB4a) in grapevine's response to cold stress.
View Article and Find Full Text PDFThe P2X7-Mediated Mitochondrial ROS as an Emerging Core Target of Tuftsin Nanoparticles in Severe Acute Pancreatitis Therapy via Regulating Mitophagy.
ACS Appl Mater Interfaces
January 2025
Department of Gerontology, The Second Affiliated Hospital of Chongqing Medical University, Chongqing 400010, People's Republic of China.
20% acute pancreatitis (AP) develops into severe AP (SAP), a global health crisis, with an increased mortality rate to 30%-50%. Mitochondrial damage and immune disorders are direct factors, which exacerbate the occurrence and progression of AP. So far, mitochondrial and immunity injury in SAP remains largely elusive, with no established treatment options available.
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!