Three distinctive end group-containing organotin (IV) carboxylates complexes (YDCOOSn, CLCOOSn and BZCOOSn) were designed and synthesized. Together with theoretical calculations, a thorough examination was carried out to investigate the photophysical properties of these compounds. The cytotoxicity of the synthesized compounds was tested using normal cell line GES-1 and was assessed against four cancer cell lines (A549, Hela, H1299 and HepG2). The outcomes of the experiments demonstrated that these complexes had superior selectivity than cisplatin towards cancerous cells, particularly in the A549 cell line. BZCOOSn was selected as a candidate compound for additional research because it exhibited the lowest IC value and the most impressive inducing effect on cell death and G2/M phase arrest. Increased caspase-3 and -9 enzyme activity, a decline in mitochondrial membrane potential (MMP), characteristic nuclear apoptotic morphology, and an accumulation of intracellular reactive oxygen species (ROS) were seen in A549 exposed to BZCOOSn. These findings demonstrated that BZCOOSn exhibited strong cytotoxicity by triggering cell death in A549 via the mitochondrial route. Furthermore, using the scratch wound healing assay, it was discovered that BZCOOSn reduced the migration of A549 cancerous cells. These data all pointed to BZCOOSn as a possible candidate for more research and development as a chemotherapeutic drug.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.jinorgbio.2024.112609 | DOI Listing |
J Biol Chem
January 2025
Department of Pharmaceutical Chemistry, University of California, San Francisco, San Francisco, CA 94158, USA; Department of Cellular and Molecular Pharmacology, University of California, San Francisco, San Francisco, CA 94158, USA. Electronic address:
Carboxyl-terminus of Hsp70-Interacting Protein (CHIP) is an E3 ubiquitin ligase that marks misfolded substrates for degradation. Hyper-activation of CHIP has been implicated in multiple diseases, including cystic fibrosis and cancer, suggesting that it may be a potential drug target. However, there are few tools available for exploring this possibility.
View Article and Find Full Text PDFSci Total Environ
January 2025
US Geological Survey, New England Water Science Center, Northborough, MA, USA.
Groundwater-dependent ecosystems in areas with industrial land use are at risk of exposure to a PFAS chemicals. We investigated one such system with several known PFAS source areas, where high and low permeability sediments (glacial) coupled with groundwater-lake and groundwater/surface-water interactions created complex 'source to seep' dynamics. Using heat-tracing and chemical methods, numerous preferential groundwater discharge zones were identified and sampled across the upper Quashnet River stream-wetland system in Mashpee, MA, USA, downgradient of Joint Base Cape Cod (JBCC).
View Article and Find Full Text PDFMolecules
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 PDFMolecules
January 2025
Academy of Interdisciplinary Studies on Intelligent Molecules, College of Chemistry, Tianjin Normal University, Tianjin 300387, China.
Peptide-based therapy is appealing in modern medicine owing to its high activity and excellent biocompatibility. Poor stability, leading to unacceptable bioavailability, severely constrains its clinical application. Here, we proposed a general supramolecular approach for improving the plasma resistance of a commercially available peptide agent, thymopentin.
View Article and Find Full Text PDFMolecules
January 2025
A.V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Sciences, Leninsky Prospect 29, Moscow 119991, Russia.
In this study, the homogeneous carboxylation of potassium, sodium, and lithium phenolates in DMSO solution at 100 °C by the Kolbe-Schmitt reaction was investigated. The impact of water, phenolate concentration, and cation nature on the yield of products and reaction selectivity was demonstrated. Based on the patterns observed, it was concluded that a complex cluster mechanism governs the carboxylation reaction in the solution.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!