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Isolation and In Silico SARS-CoV-2 Main Protease Inhibition Potential of Jusan Coumarin, a New Dicoumarin from .
Molecules
March 2022
Pharmacognosy and Medicinal Plants Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo 11884, Egypt.
A new dicoumarin, jusan coumarin, (), has been isolated from aerial parts. The chemical structure of jusan coumarin was estimated, by 1D, 2D NMR as well as HR-Ms spectroscopic methods, to be 7-hydroxy-6-methoxy-3-[(2-oxo-2H-chromen-6-yl)oxy]-2H-chromen-2-one. As the first time to be introduced in nature, its potential against SARS-CoV-2 has been estimated using various in silico methods.
View Article and Find Full Text PDFUnravelling the collateral damage of antibiotics on gut bacteria.
Nature
November 2021
Genome Biology Unit, European Molecular Biology Laboratory, Heidelberg, Germany.
Antibiotics are used to fight pathogens but also target commensal bacteria, disturbing the composition of gut microbiota and causing dysbiosis and disease. Despite this well-known collateral damage, the activity spectrum of different antibiotic classes on gut bacteria remains poorly characterized. Here we characterize further 144 antibiotics from a previous screen of more than 1,000 drugs on 38 representative human gut microbiome species.
View Article and Find Full Text PDFA pharmacological review of dicoumarol: An old natural anticoagulant agent.
Pharmacol Res
October 2020
School of Basic Medicine, Qingdao University, Qingdao, 266071, China; State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau. Electronic address:
Dicoumarol is an oral anticoagulant agent prescribed in clinical for decades. It is a natural hydroxycoumarin discovered from the spoilage of Melilotus officinalis (L.) Pall and is originally discovered as a rodenticide.
View Article and Find Full Text PDFβ-Lapachone Induces Acute Oxidative Stress in Rat Primary Astrocyte Cultures that is Terminated by the NQO1-Inhibitor Dicoumarol.
Neurochem Res
October 2020
Centre for Biomolecular Interactions Bremen, Faculty 2 (Biology/Chemistry), University of Bremen, P.O. Box 330440, 28334, Bremen, Germany.
β-lapachone (β-lap) is reduced in tumor cells by the enzyme NAD(P)H: quinone acceptor oxidoreductase 1 (NQO1) to a labile hydroquinone which spontaneously reoxidises to β-lap, thereby generating reactive oxygen species (ROS) and oxidative stress. To test for the consequences of an acute exposure of brain cells to β-lap, cultured primary rat astrocytes were incubated with β-lap for up to 4 h. The presence of β-lap in concentrations of up to 10 µM had no detectable adverse consequences, while higher concentrations of β-lap compromised the cell viability and the metabolism of astrocytes in a concentration- and time-dependent manner with half-maximal effects observed for around 15 µM β-lap after a 4 h incubation.
View Article and Find Full Text PDFAn insight into the therapeutic applications of coumarin compounds and their mechanisms of action.
Eur J Pharm Sci
September 2020
Amity Institute of Biotechnology (AIB), Amity University, Noida, Uttar Pradesh, India. Electronic address:
The coumarins are heterocyclic compounds belonging to the class of benzopyrone enriched in various plants like tonka beans. Coumarins and their derivatives exert a vast array of bioactive properties such as anticoagulant, antibacterial, anti-inflammatory, antioxidant, antitumor, antiviral, and enzyme inhibition. Higher doses of coumarin are found to be hepatotoxic however they exhibit beneficial effects by reducing the risk of cancer and other neuronal and cardiovascular ailments.
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