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Title: | Sequence-activity relationship, and mechanism of action of mastoparan analogues against extended-drug resistant Acinetobacter baumannii |
Author: | Vila Farrés, Xavier López Rojas, Rafael Pachón Ibáñez, María Eugenia Teixidó Turà, Meritxell Pachón, Jerónimo Vila Estapé, Jordi Giralt Lledó, Ernest |
Keywords: | Malalties infeccioses Antibiòtics Pèptids Bacteris Communicable diseases Antibiotics Peptides Bacteria |
Issue Date: | 9-Jun-2015 |
Publisher: | Elsevier Masson SAS |
Abstract: | The treatment of some infectious diseases can currently be very challenging since the spread of multi-, extended- or pan-resistant bacteria has considerably increased over time. On the other hand, the number of new antibiotics approved by the FDA has decreased drastically over the last 30 years. The main objective of this study was to investigate the activity of wasp peptides, specifically mastoparan and some of its derivatives against extended-resistant Acinetobacter baumannii. We optimized the stability of mastoparan in human serum since the specie obtained after the action of the enzymes present in human serum is not active. Thus, 10 derivatives of mastoparan were synthetized. Mastoparan analogues (guanidilated at the N-terminal, enantiomeric version and mastoparan with an extra positive charge at the C-terminal) showed the same activity against Acinetobacter baumannii as the original peptide (2.7 muM) and maintained their stability to more than 24 h in the presence of human serum compared to the original compound. The mechanism of action of all the peptides was carried out using a leakage assay. It was shown that mastoparan and the abovementioned analogues were those that released more carboxyfluorescein. In addition, the effect of mastoparan and its enantiomer against A. baumannii was studied using transmission electron microscopy (TEM). These results suggested that several analogues of mastoparan could be good candidates in the battle against highly resistant A. baumannii infections since they showed good activity and high stability. |
Note: | Reproducció del document publicat a: http://dx.doi.org/10.1016/j.ejmech.2015.06.016 |
It is part of: | European Journal of Medicinal Chemistry, 2015, vol. 101, p. 34-40 |
URI: | http://hdl.handle.net/2445/69208 |
Related resource: | http://dx.doi.org/10.1016/j.ejmech.2015.06.016 |
ISSN: | 0223-5234 |
Appears in Collections: | Articles publicats en revistes (ISGlobal) Articles publicats en revistes (Química Inorgànica i Orgànica) Articles publicats en revistes (Fonaments Clínics) Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona)) |
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