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In vitro inhibition of Helicobacter pylori and interaction studies of lichen natural products with jack bean urease

Abstract

The interaction of (S)-(-)-usnic acid (2) and fumarprotocetraric acid (3), isolated from Cladonia rappii (lichen), and commercial (R)-(+)-usnic acid (1) with urease was investigated in vitro by molecular spectroscopy at pH 7.4 and kinetics experiments using jack bean type III urease. All lichen compounds tested interact with urease by statistic quenching mechanism forming non-fluorescent complexes that change the native protein structure. Complexes formation were spontaneous and stabilized mainly by electrostatic forces, in which interaction magnitude was determined to be 3 < 2 < 1. Compound 2, whose tridimensional structure is here disclosed, acts as mixed inhibitor while compounds 1 and 3 function as competitive ones. The (R)-(+)-UA (1) were the most efficient lichen metabolite with respect to impairment of the growth of five H. pylori strains. The minimum inhibitory concentrations (MIC) for the lichen metabolites tested were lower (from 2- to 7.8-fold) than those of omeprazole (reference drug) against all H. pylori strains tested. Overall, the lichen metabolites 1-3 are promising lead compounds for the design of more efficient urease inhibitors for the treatment of H. pylori infections.

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Publication details

The article was received on 05 Jan 2018, accepted on 13 Feb 2018 and first published on 13 Feb 2018


Article type: Paper
DOI: 10.1039/C8NJ00072G
Citation: New J. Chem., 2018, Accepted Manuscript
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    In vitro inhibition of Helicobacter pylori and interaction studies of lichen natural products with jack bean urease

    T. C. D. A. Lage, T. M. S. Maciel, Y. C.C. Mota, F. Sisto, J. R. Sabino, J. Carinhanha, I. Figueiredo, C. Masia, A. de Fatima, S. A. Fernandes and L. V. Modolo, New J. Chem., 2018, Accepted Manuscript , DOI: 10.1039/C8NJ00072G

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