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Molecules 2017, 22(5), 786; doi:10.3390/molecules22050786

Anti-Helicobacter pylori Activity of Isocoumarin Paepalantine: Morphological and Molecular Docking Analysis

1
Graduate Program in Pharmaceutical Sciences, Federal University of Espirito Santo–UFES, Marechal Campos Av., 1468, Vitoria 29043-900, ES, Brazil
2
Department of Pharmaceutical Sciences, Federal University of Espirito Santo–UFES, Marechal Campos Av., 1468, Vitoria 29043-900, ES, Brazil
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 14 March 2017 / Revised: 29 April 2017 / Accepted: 3 May 2017 / Published: 12 May 2017
(This article belongs to the Section Natural Products)
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Abstract

The Helicobacter pylori bacterium is one of the main causes of chronic gastritis, peptic ulcers, and even gastric cancer. It affects an average of half of the world population. Its difficult eradication depends upon multi-drug therapy. Since its classification as a group 1 carcinogenic by International Agency for Research on Cancer (IARC), the importance of H. pylori eradication has obtained a novel meaning. There is considerable interest in alternative therapies for the eradication of H. pylori using compounds from a wide range of natural products. In the present study, we investigated the antibacterial property of the isocoumarin paepalantine against H. pylori and it exhibited significant anti-H. pylori activity at a minimum inhibitory concentration (MIC) of 128 μg/mL and at a minimum bactericidal concentration (MBC) of 256 μg/mL. The scanning electron microscopy (SEM) revealed significant morphological changes of the bacterial cell as a response to a sub-MIC of paepalantine, suggesting a penicillin-binding protein (PBP) inhibition. Computational studies were carried out in order to study binding modes for paepalantine in PBP binding sites, exploring the active and allosteric sites. The data from the present study indicates that paepalantine exhibits significant anti-H. pylori activity, most likely by inhibiting membrane protein synthesis. View Full-Text
Keywords: paepalantine; isocoumarin; antibacterial; Helicobacter pylori; penicillin-binding protein; docking paepalantine; isocoumarin; antibacterial; Helicobacter pylori; penicillin-binding protein; docking
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Damasceno, J.P.L.; Rodrigues, R.P.; Gonçalves, R.C.R.; Kitagawa, R.R. Anti-Helicobacter pylori Activity of Isocoumarin Paepalantine: Morphological and Molecular Docking Analysis. Molecules 2017, 22, 786.

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