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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/69208
Sequence-activity relationship, and mechanism of action of mastoparan analogues against extended-drug resistant Acinetobacter baumannii
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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.
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VILA FARRÉS, Xavier, et al. Sequence-activity relationship, and mechanism of action of mastoparan analogues against extended-drug resistant Acinetobacter baumannii. European Journal of Medicinal Chemistry. 2015. Vol. 101, num. 34-40. ISSN 0223-5234. [consulted: 11 of October of 2026]. Available at: https://hdl.handle.net/2445/69208