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Abstract Title:

Multitarget Action of Xanthones fromagainstα-Amylase, α-Glucosidase and Pancreatic Lipase.

Abstract Source:

Molecules. 2022 May 20 ;27(10). Epub 2022 May 20. PMID: 35630761

Abstract Author(s):

Juan Cardozo-Muñoz, Luis E Cuca-Suárez, Juliet A Prieto-Rodríguez, Fabian Lopez-Vallejo, Oscar J Patiño-Ladino

Article Affiliation:

Juan Cardozo-Muñoz

Abstract:

Digestive enzymes suchα-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.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 fromagainst 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 (-). Six derivatives (-) 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,,,and, highlightingwith ICvalues of 33.3µM 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.

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