Evaluation of Thr 6 -bradykinin purified from Polybia occidentalis wasp venom in the choline uptake of mammal cortices.

Autor: Mortari MR; a Neuropharmacology Laboratory, Department of Physiological Sciences , Institute of Biological Sciences, University of Brasília , Brasília , Brazil., Cunha AO; d Neurobiology and Venoms Laboratory, Department of Biology, College of Philosophy, Sciences and Literature of Ribeirão Preto , University of São Paulo , São Paulo , Brazil., Carolino RO; b Department of Biochemistry and Immunology, School of Medicine of Ribeirão Preto , University of São Paulo , São Paulo , Brazil., Silva JC; a Neuropharmacology Laboratory, Department of Physiological Sciences , Institute of Biological Sciences, University of Brasília , Brasília , Brazil., Lopes NP; c Organic Chemistry Laboratory, Department of Physics and Chemistry, Faculty of Pharmaceutical Sciences of Ribeirão Preto , University of São Paulo , São Paulo , Brazil., Santos WF; d Neurobiology and Venoms Laboratory, Department of Biology, College of Philosophy, Sciences and Literature of Ribeirão Preto , University of São Paulo , São Paulo , Brazil.
Jazyk: angličtina
Zdroj: Pharmaceutical biology [Pharm Biol] 2016 Dec; Vol. 54 (12), pp. 3169-3171. Date of Electronic Publication: 2016 Aug 26.
DOI: 10.1080/13880209.2016.1211715
Abstrakt: Context: Thr 6 -bradykinin is a peptide found in the venom of social and solitary wasps. This kinin, along with other bradykinin-like peptides, is known to cause irreversible paralysis in insects by presynaptic blockade of cholinergic transmission. However, this activity has never been tested in mammals.
Objective: As such, the objective of this study was to evaluate the effect of Thr 6 -bradykinin on the cholinergic system of rats.
Materials and Methods: The peptide was isolated from the venom of the Neotropical social wasp Polybia occidentalis Olivier (Vespidae). After correct identification and quantification by ESI-MS and MS/MS, the peptide was tested in [ 14 C]-choline uptake using rat cortical synaptosomes. Each uptake assay was accompanied by lactic acid dehydrogenase (LDH) activity measurement to evaluate synaptosome integrity in the presence of six increasing concentrations of BK or Thr 6 -BK (0.039, 0.156, 0.625, 2.500, 10.000 and 40.000 μM).
Results: Data revealed that neither BK nor Thr 6 -BK at any of the six concentrations tested (from 0.039 to 40.000 μM) affected [ 14 C]-choline uptake in synaptosomes. Moreover, there was no increase in LDH in the supernatants, indicating that BK and Thr 6 -BK did not disrupt the synaptosomes.
Discussion and Conclusion: In contrast to previous reports for the insect central nervous system (CNS), Thr 6 -BK had no effect on mammalian cholinergic transmission. Nevertheless, this selectivity for the insect CNS, combined with its irreversible mode of action may be relevant to the discovery of new sources of insecticides and could contribute to understanding the role of kinins in the mammalian CNS.
Databáze: MEDLINE
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