Topic
Xanthone
About: Xanthone is a research topic. Over the lifetime, 1639 publications have been published within this topic receiving 25870 citations. The topic is also known as: 9-oxo-xanthene & Diphenyline ketone oxide.
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TL;DR: The first phytochemical investigation of the twig extracts of Maclura fruticosa led to the isolation and identification of a new xanthone, maclurafruticosone (1), together with 14 known compounds.
Abstract: The first phytochemical investigation of the twig extracts of Maclura fruticosa led to the isolation and identification of a new xanthone, maclurafruticosone (1), together with 14 known compounds (...
3 citations
Journal Article•
TL;DR: A series of xanthone 1,4-dihydropyridine derivatives bearing a 2,3-lactone ring and a 2-acetoxymethyl group were prepared as discussed by the authors.
Abstract: A series of xanthone 1,4-dihydropyridine derivatives bearing a 2,3-lactone ring and a 2-acetoxymethyl group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. The introduction of a 2,3-lactone ring improved the negative inotropic activity and selectivity.
3 citations
TL;DR: In this article, a non-linear QSAR model was constructed on a series of 57 xanthone and curcuminoide derivatives as α-glucosidase inhibitors by back-propagation neural network method.
Abstract: Department of Chemistry, Faculty of Sciences, University of Djelfa, 17000, AlgeriaReceived November 26, 2012, Accepted March 6, 2013A non linear QSAR model was constructed on a series of 57 xanthone and curcuminoide derivatives as α-glucosidase inhibitors by back-propagation neural network method. The neural network architecture wasoptimized to obtain a three-layer neural network, composed of five descriptors, nine hidden neurons and oneoutput neuron. A good predictive determination coefficient was obtained (R
3 citations
TL;DR: Enzymatic kinetics and molecular docking studies showed that the bioactive xanthones are mainly competitive inhibitors on AA, mixed inhibitors on AG and non-competitive inhibitors on PL, and the presence of methoxy, hydroxyl and carbonyl groups are important in the activity and interaction of polyfunctional xanthone.
Abstract: Digestive enzymes such α-amylase (AA), α-glucosidase (AG) and pancreatic lipase (PL), play an important role in the metabolism of carbohydrates and lipids, being attractive therapeutic targets for the treatment of type 2 diabetes and obesity. Garcinia mangostana is an interesting species because there have been identified xanthones with the potential to inhibit these enzymes. In this study, the multitarget inhibitory potential of xanthones from G. mangostana against AA, AG and PL was assessed. The methodology included the isolation and identification of bioactive xanthones, the synthesis of some derivatives and a molecular docking study. The chemical study allowed the isolation of five xanthones (1–5). Six derivatives (6–11) were synthesized from the major compound, highlighting the proposal of a new solvent-free methodology with microwave irradiation for obtaining aromatic compounds with tetrahydropyran cycle. Compounds with multitarget activity correspond to 2, 4, 5, 6 and 9, highlighting 6 with IC50 values of 33.3 µM on AA, 69.2 µM on AG and 164.4 µM on PL. Enzymatic kinetics and molecular docking studies showed that the bioactive xanthones are mainly competitive inhibitors on AA, mixed inhibitors on AG and non-competitive inhibitors on PL. The molecular coupling study established that the presence of methoxy, hydroxyl and carbonyl groups are important in the activity and interaction of polyfunctional xanthones, highlighting their importance depending on the mode of inhibition.
3 citations
TL;DR: Polygalaxanthone A has been shown by synthesis to have the structure 1,2,3-trimethoxy-6,7-methylenedioxyxanthone (2a ) and not that originally proposed as discussed by the authors.
3 citations