title: Antinociceptive properties of the mastoparan peptide Agelaia-MPI isolated from social wasps.
abstract: Analgesic therapy is based on the sequential treatment of pain, in which opioids are drugs of last resource and known to be highly effective, but are also responsible for undesirable side effects, tolerance and addiction. There is a need for new drugs with alternative targets in order to minimize side effects and improve treatment efficacy. Mastoparans are an abundant class of peptides in wasp venom and have shown great potential as new drugs, as well as being excellent tools for the study of G-protein-coupled receptors. The objective of this study was to investigate the antinociceptive activity of the mastoparan Agelaia-MP I and the mechanisms involved. Agelaia-MP I (MW 1565 Da) showed dose-dependent antinociceptive activity in mice submitted to i.c.v. injection in two different models. The highest dose produced a maximum effect for up to 4 h, and nociception remained low three days after injection. Further experiments showed that Agelaia-MPI induced partial and reversible blockade of the amplitude of action potential, probably interacting with voltage-gated sodium channels. These results revealed the significant potential impact of compounds isolated from wasp venom on the central nervous system (CNS). In addition, the antinociceptive effect described here is a novel activity for mastoparans.
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil. Electronic address: jacq.coimbra@gmail.com.
authors.forename: Jacqueline
authors.initials: J
authors.lastname: Gonçalves
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil; Immunopathology Laboratory, Butantan Institute, Sao Paulo, Brazil. Electronic address: marisarangel2112@gmail.com.
authors.forename: Marisa
authors.initials: M
authors.lastname: Rangel
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil. Electronic address: andreia.biolchi@gmail.com.
authors.forename: Andréia
authors.initials: A
authors.lastname: Biolchi
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil. Electronic address: eveline_as@hotmail.com.
authors.forename: Eveline
authors.initials: E
authors.lastname: Alves
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil; Department of Physiological Sciences, Biotechnology Institute Federal University of Goias, Catalão, Brazil. Electronic address: karlagmoreira@gmail.com.
authors.forename: Karla
authors.initials: K
authors.lastname: Moreira
authors.affiliation: EMBRAPA-CENARGEN, Brasilia, Brazil. Electronic address: lucianopaulinosilva@gmail.com.
authors.forename: Luciano
authors.initials: L
authors.lastname: Silva
authors.affiliation: Laboratory of Neuropharmacology, Department of Physiological Sciences, Institute of Biological Sciences, University of Brasília, Brasília-DF, 70910-900, Brazil. Electronic address: mmortari@unb.br.
authors.forename: Márcia
authors.initials: M
authors.lastname: Mortari
mesh_terms: D000200:Action Potentials / Q000187:drug effects; D000595:Amino Acid Sequence; D000700:Analgesics / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D001522:Behavior, Animal; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D007276:Injections, Intraventricular; D036341:Intercellular Signaling Peptides and Proteins; D008297:Male; D051379:Mice; D010455:Peptides / Q000008:administration & dosage / Q000494:pharmacology*; D045442:Rotarod Performance Test; D012584:Sciatic Nerve / Q000187:drug effects / Q000502:physiology; D017386:Sequence Homology, Amino Acid; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D014862:Wasp Venoms / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D014863:Wasps
chemical_list: D000700:Analgesics; D036341:Intercellular Signaling Peptides and Proteins; D010455:Peptides; D014862:Wasp Venoms; C037500:mastoparan
keywords: Agelaia-MP I; Antinociception; Mastoparan; Pain; Sodium channels