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Electrophysiological characterization of human KCNT1 channel modulators and the therapeutic potential of hydroquinine and tipepidine in KCNT1 mutation-associated epilepsy mouse model.
Acta Pharmacol Sin
January 2025
Jiangsu Province Key Laboratory of Anesthesiology, Xuzhou Medical University, Xuzhou, 221004, China.
Patients suffering epilepsy caused by the gain-of-function mutants of the hKCNT1 potassium channels are drug refractory. In this study, we cloned a novel human KCNT1B channel isoform using the brain cDNA library and conducted patch-clamp and molecular docking analyses to characterize the pharmacological properties of the hKCNT1B channel using thirteen drugs. Among cinchona alkaloids, we found that hydroquinine exerted the strongest blocking effect on the hKCNT1B channel, especially the F313L mutant.
View Article and Find Full Text PDFPhytochemical Composition, Antibacterial, and Antibiotic-Resistance Modulatory Activity of Extracts of Moldenke M. A. Lawson, and L. Against Multidrug-Resistant .
Scientifica (Cairo)
December 2024
Department of Biochemistry, University of Dschang, Dschang, Cameroon.
Article Synopsis
- A study investigated the antibacterial effects of certain plant extracts, both individually and in combination with antibiotics, against multidrug-resistant (MDR) bacteria, a major health threat due to its resistance to conventional treatments.
- Qualitative and quantitative phytochemical analyses revealed that the extracts contained phenols and flavonoids, with one extract showing the highest concentration of phenolic compounds and the other the highest flavonoid content.
- The research found that the extracts exhibited antibacterial properties, with the best performing extract enhancing the effectiveness of several antibiotics, suggesting potential for developing natural treatments for MDR infections.
Glycyrrhizin alleviates the toxicity of hydroxychloroquine in treating oral lichen planus by occupying heat shock protein 90 alpha.
Phytomedicine
December 2024
State Key Laboratory of Oral Diseases & National Center of Stomatology & National Clinical Research Center for Oral Diseases & Frontier Innovation Center for Dental Medicine Plus, West China Hospital of Stomatology, Sichuan University, Chengdu, 610041 Sichuan, China. Electronic address:
Background: Oral lichen planus (OLP) is a common chronic inflammatory disease with the potential of malignant transformation. Hydroxychloroquine (HCQ), derived from quinine originating from Cinchona spp. bark, is a commonly prescribed off-label for OLP.
View Article and Find Full Text PDFBackground: In the present study, two structurally similar alkaloids from trees of Cinchona genus, chloroquine and cinchonine, were examined for their vasorelaxant effects in a model of phenylephrine-induced smooth muscle contractions.
Methods: Potential mechanisms of action associated with endothelial vasorelaxant compounds, voltage-gated Ca2+ channels (LTCCs), and inositol triphosphate receptors were examined in isolated rat aortic rings. Also, an in silico approach was used to predict the activity of the two test compounds.
Enantiospecific Analysis of Carboxylic Acids Using Alkaloid Dimers as Chiral Solvating Agents.
Anal Chem
May 2024
School of Chemistry, Zhengzhou University, Zhengzhou, 450001, China.
alkaloid derivatives as Brønsted base catalysts have attracted considerable attention in the field of asymmetric catalysis. However, their potential application as chiral solvating agents has not been described. In this research, we investigated the use of the alkaloid dimer, namely, (DHQ)PHAL, as a chiral solvating agent for discerning various mandelic acid derivatives through H NMR spectroscopy.
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