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Occurrence, removal and environmental risk assessment of pharmaceutical active compounds (PhACs) and metabolites in hospital wastewater.
J Hazard Mater
December 2024
State Key laboratory of Environmental Criteria and Risk Assessment, Chinese Research Academy of Environmental Sciences, Beijing 100012, China; Institute of Water Environment Research, Chinese Research Academy of Environmental Sciences, Beijing 100012, China. Electronic address:
Article Synopsis
- The study examines the presence and removal of 74 pharmaceutical active compounds (PhACs) in wastewater from 11 hospitals, with a focus on their potential environmental impact.
- A total of 51 PhACs were found in wastewater, with notable differences based on hospital type and size, indicating that these factors influence PhAC levels.
- The study highlights varying removal efficiencies of treatment methods, with membrane bioreactors performing better than biological contact oxidation, and calls for improved management of wastewater discharge in smaller and specialized hospitals.
Bitopic Ligands Support the Presence of a Metastable Binding Site at the β Adrenergic Receptor.
J Med Chem
July 2024
Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, 2100 Copenhagen, Denmark.
Metastable binding sites (MBS) have been observed in a multitude of molecular dynamics simulations and can be considered low affinity allosteric binding sites (ABS) that function as stepping stones as the ligand moves toward the orthosteric binding site (OBS). Herein, we show that MBS can be utilized as ABS in ligand design, resulting in ligands with improved binding kinetics. Four homobivalent bitopic ligands (-) were designed by molecular docking of ()-alprenolol (()-ALP) in the cocrystal structure of the β adrenergic receptor (βAR) bound to the antagonist ALP.
View Article and Find Full Text PDFWidely distributable and retainable in-situ gelling material for treating myocardial infarction.
Acta Biomater
March 2024
Department of Biomedical Engineering, National Cerebral and Cardiovascular Center Research Institute, 6-1 Kishibe Shimmachi, Suita, Osaka 564-8565, Japan; Department of Clinical Engineering, Faculty of Health Sciences, Komatsu University, He 14-1, Mukai-motoori-machi, Komatsu, Ishikawa 923-0961, Japan. Electronic address:
Intramyocardial hydrogel injection is a promising therapy to prevent negative remodeling following myocardial infarction (MI). In this study, we report a mechanism for in-situ gel formation without external stimulation, resulting in an injectable and tissue-retainable hydrogel for MI treatment, and investigate its therapeutic outcomes. A liquid-like polymeric solution comprising poly(3-acrylamidophenylboronic acid-co-acrylamide) (BAAm), polyvinyl alcohol (PVA), and sorbitol (S) increases the viscous modulus by reducing the pre-added sorbitol concentration is developed.
View Article and Find Full Text PDFThe β-Blocker Carvedilol and Related Aryloxypropanolamines Promote ERK1/2 Phosphorylation in HEK293 Cells with Values Distinct From Their Equilibrium Dissociation Constants as -Adrenoceptor Antagonists: Evidence for Functional Affinity.
J Pharmacol Exp Ther
January 2024
Lung Health Research Group, Department of Physiology and Pharmacology, Snyder Institute for Chronic Diseases, Cumming School of Medicine, University of Calgary, Calgary, Alberta, Canada
The determination of affinity by using functional assays is important in drug discovery because it provides a more relevant estimate of the strength of interaction of a ligand to its cognate receptor than radioligand binding. However, empirical evidence for so-called, "functional affinity" is limited. Herein, we determined whether the affinity of carvedilol, a -adrenoceptor antagonist used to treat heart failure that also promotes extracellular signal-regulated kinases 1 and 2 (ERK1/2) phosphorylation, differed between these two pharmacological activities.
View Article and Find Full Text PDFEffect of liposome composition on β-blocker interactions studied by capillary electrokinetic chromatography.
J Sep Sci
September 2023
Department of Chemistry, University of Helsinki, Helsinki, Finland.
Article Synopsis
- The study used liposome capillary electrokinetic chromatography to analyze how three different β-blockers (alprenolol, propranolol, and carvedilol) interact with various liposome solutions.
- The liposome compositions were tailored using a specific design approach to find the ideal formulations for the experiments.
- Results revealed that cholesterol and a particular phospholipid significantly affected how these β-blockers distributed within the liposome systems.
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