# name
Sequence-activity relationship, and mechanism of action of mastoparan analogues against extended-drug resistant Acinetobacter baumannii

# metadata.dc.description.abstract[].value
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.

# metadata.dc.relation.ispartof[].value
European Journal of Medicinal Chemistry, 2015, vol. 101, p. 34-40

# metadata.dc.source[].value
Articles publicats en revistes (Química Inorgànica i Orgànica)

# metadata.dc.title[].value
Sequence-activity relationship, and mechanism of action of mastoparan analogues against extended-drug resistant Acinetobacter baumannii