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.

Fraternine, a Novel Wasp Peptide, Protects against Motor Impairments in 6-OHDA Model of Parkinsonism

“…The chromatogram was similar to that obtained using the venom of the same species [ 25 ] and closely related ones [ 19 , 20 , 26 ], in which the first two fractions were formed by biogenic amines and neurotransmitters, like serotonins. As the objective of the work was to detect new peptides, fractions 1 and 2 were not tested.…”

“…Thirty-four chromatographies were made, total time of the run was 100 min, and the fractions were eluted until 75 min; the more abundant peaks were divided into 7 fractions ( Figure 1). The chromatogram was similar to that obtained using the venom of the same species [25] and closely related ones [19,20,26], in which the first two fractions were formed by biogenic amines and neurotransmitters, like serotonins. As the objective of the work was to detect new peptides, fractions 1 and 2 were not tested.…”

“…Fraction, molecular mass, name, sequence and known effects of the peptides from P. fraternus venom. broad-spectrum action against microorganisms, inhibitory effects against tumor proliferation, antinociceptive and stimulating serotonin release from platelets and mast cell degranulation [25,26,28] After an initial screening in the 6-OHDA model of parkinsonism with the fractions (data not shown) and due to a greater abundance, fraction 6 was selected for sequencing and underwent further tests, and the peptide was named Fraternine. In total, 6 mg of the peptide was purified, and its high degree of purity was confirmed by chromatography and mass spectrometry.…”

Antimicrobial and Anticancer Properties of Synthetic Peptides Derived from the Wasp Parachartergus fraternus

“…[3] Fractionation of wasp venoms has revealed the presence of a wide variety of compounds, including biogenic amines, proteins, and peptides. [4] Wasp peptides can be generally classified into kinins, mastoparans or chemotactic peptides. These three classes represent more than 70 % of the dried venom [5] and are responsible for most of the biological activities described for wasp venom, ranging from mast cell degranulation, hemolysis, and leukocyte chemotaxis, [6] to antitumor, antimicrobial, and neurological activities, [6b,7] which arise from the peptides interacting with cell membranes or with one of several receptors.…”

Centipede venom peptide SsmTX-I with two intramolecular disulfide bonds shows analgesic activities in animal models

“…Ziconotide exhibits stronger analgesic effects than morphine and does not cause tolerance or addiction . Many other peptides have been discovered and identified as potential analgesic drug candidates, including mambalgins, peptides identified from the venom of the black mamba snake ; psalmotoxin 1, a peptide extracted from the South American tarantula ; and mastoparan, from social wasps .…”