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Medchem & Toxicology 2018

Page 87

Journal of Organic & Inorganic Chemistry

ISSN: 2472-1123

A n n u a l C o n g r e s s o n

Medicinal Chemistry,

Pharmacology and toxicology

J u l y 3 0 - 3 1 , 2 0 1 8

Am s t e r d a m , N e t h e r l a n d s

H

elicobacter pylori

chronic infection is associated, among other severe gastric disorders, with intestinal-type gastric

carcinogenesis, being this the fifth most common cancer and the third leading cause of cancer-related death worldwide.

Classical

H. pylori

eradication treatment, combining two antibiotics and a proton pump inhibitor, reduces the risk for gastric

carcinoma development, but treatment of

H. pylori

infection is challenged by a dramatic fall in eradication rates all over the world.

Currently, this bacterium is listed among the 16 antibiotic-resistant bacteria that pose greatest threat to human health according

to the World Health Organization. Antimicrobial peptides (AMPs) present an alternative to conventional antibiotic therapies,

being their most striking feature the low tendency to induce bacterial resistance, since AMPs selectively damage the bacterial

membranes through mechanisms that bacteria find difficult to evade. In an

in vivo

scenario, “unbound AMPs” can undergo

proteolysis and peptide aggregation, leading to efficiency decrease. AMP grafting onto nanoparticles has been reported as a

good strategy to protect peptides from aggregation and enzymatic degradation in vivo, therefore increasing long-term stability

and avoiding cytotoxicity is associated with application of high AMP concentrations. In this study, we demonstrated that the

AMP MSI-78A could be surface-grafted without compromising its activity. Moreover, MSI-78A-decorated surfaces were highly

effective against

H. pylori

, killing bacteria by contact in a short time span, since after 2 hrs only, 2% of

H. pylori

remained viable in

suspension. These results encourage the utilization of grafted MSI-78A on biocompatible nanoparticles as an alternative to the

currently available therapy against H. pylori, opening new routes for gastric infection management

.

parreira@i3s.up.pt

Management of H. pylori gastric infection via

surface-grafted antimicrobial peptides

Paula Parreira1,2, Claudia Monteiro1,2, Vanessa Graça2, Joana

Gomes1,3, Sílvia Maia4, Paula Gomes4, Inês C Gonçalves1,2,5

and M Cristina L Martins1,2,6

1

i3S, Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Portugal

2

INEB, Instituto de Engenharia Biomédica, Universidade do Porto, Portugal

3

IPATIMUP, Instituto de Patologia e Imunologia Molecular, Universidade do Porto, Portugal

4

LAQV-REQUIMTE, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade

do Porto, Portugal

5

FEUP, Faculdade de Engenharia, Universidade do Porto, Portugal

6

Instituto de Ciências Biomédicas Abel Salazar, Universidade do Porto, Portugal

J Org Inorg Chem 2018, Volume 4

DOI: 10.21767/2472-1123-C3-009