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| http://dx.doi.org/10.4088/PCC.15l01874 | DOI Listing |
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Hyperosmotic stress-induced NLRP3 inflammasome activation via the mechanosensitive PIEZO1 channel in dry eye corneal epithelium.
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January 2025
Eye Hospital and School of Ophthalmology and Optometry, Wenzhou Medical University, Zhejiang, 325000, China; State Key Laboratory of Ophthalmology, Optometry and Visual Science, Wenzhou Medical University, Zhejiang, 325000, China. Electronic address:
Unlabelled: The activation of the NLRP3 inflammasome by hyperosmotic stress is a critical pathophysiological response in dry eye disease (DED), driving the chronic cycle of inflammation on the ocular surface. The specific mechanism underlying hyperosmotic mechanical stimulation activates the NLRP3 inflammasome remains unclear. This study provides evidence that PIEZO1, a mechanosensitive ion channel, functions as the primary receptor for corneal epithelial cells in sensing mechanical stimulation induced by tear hyperosmolarity.
View Article and Find Full Text PDFTeMac™ ameliorates memory impairment and cholinergic dysfunction in rats induced by scopolamine.
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January 2025
Department of Biochemistry, Faculty of Science, University of Yaoundé 1, P.O. Box 812, Yaounde, Cameroon.
Alzheimer's disease (AD) is associated with cognitive impairments which are linked to a deficit in cholinergic function. The objective of this study was to evaluate the ability of TeMac™ to prevent memory impairment in scopolamine-rats model of Alzheimer's disease and by in silico approaches to identify molecules in TeMac™ inhibiting acetylcholinesterase. The cholinergic cognitive dysfunction was induced by intraperitoneal injection of scopolamine (1 mg/kg daily) in male Wistar rats for seven consecutive days.
View Article and Find Full Text PDFDevelopment of coumarin-inspired bifunctional hybrids as a new class of anti-Alzheimer's agents with potent efficacy.
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Department of Pharmaceutical Sciences, Guru Nanak Dev University Amritsar Punjab 143005 India
Considering the multifactorial and complex nature of Alzheimer's disease and the requirement of an optimum multifunctional anti-Alzheimer's agent, a series of triazole tethered coumarin-eugenol hybrid molecules was designed as potential multifunctional anti-Alzheimer's agents using donepezil and a template. The designed hybrid molecules were synthesized a click chemistry approach and preliminarily screened for cholinesterase and Aβ aggregation inhibition. Among them, AS15 emerged as a selective inhibitor of AChE (IC = 0.
View Article and Find Full Text PDFPharmacological and non-pharmacological interventions for pain control in outpatient hysteroscopy: A systematic review.
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Discipline of Surgery, University of Galway, Galway, Ireland.
Background: Outpatient hysteroscopy (OPH) is an important diagnostic and therapeutic intervention in gynaecology. However, the most common reason for failure is pain. Currently, there is no consensus regarding analgesia for OPH amongst the literature.
View Article and Find Full Text PDFDesign, synthesis and biological evaluation of galantamine analogues for cognitive improvement in Alzheimer's disease.
Eur J Med Chem
February 2025
Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Liaoning, Shenyang, 110016, China. Electronic address:
Galantamine plays a crucial role in the management of brain disorders. In this study, a series of galantamine analogues were designed, synthesized and evaluated as potential therapeutic agents for Alzheimer's disease (AD). Compound C2, a dual inhibitor of cholinesterase, was obtained by introducing a benzylpyridine ring to the hydroxyl group of galantamine.
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