A novel physiological property of snake bradykinin-potentiating peptides-Reversion of MK-801 inhibition of nicotinic acetylcholine receptors

A novel physiological property of snake bradykinin-potentiating peptides-Reversion of MK-801 inhibition of nicotinic acetylcholine receptors

Autor Nery, Arthur A. Google Scholar
Trujillo, Cleber A. Google Scholar
Lameu, Claudiana Autor UNIFESP Google Scholar
Konno, Katsuhiro Autor UNIFESP Google Scholar
Oliveira, Vitor Autor UNIFESP Google Scholar
Camargo, Antonio C. M. Autor UNIFESP Google Scholar
Ulrich, Henning Google Scholar
Hayashi, Mirian A. F. Autor UNIFESP Google Scholar
Instituição Universidade de São Paulo (USP)
Universidade Federal de São Paulo (UNIFESP)
Resumo The first naturally occurring angiotensin-converting enzyme (ACE) inhibitors described are pyroglutamyl proline-rich oligopeptides, found in the venom of the viper Bothrops jararaca, and named as bradykinin-potentiating peptides (BPPs). Biochemical and pharmacological properties of these peptides were essential for the development of Captopril, the first active site-directed inhibitor of ACE, currently used for the treatment of human hypertension. However, a number of data have suggested that the pharmacological activity of BPPs could not only be explained by their inhibitory action on enzymatic activity of somatic ACE. in fact, we showed recently that the strong and long-lasting anti-hypertensive effect of BPP-10c [<ENWPHPQIPP] is independent of somatic ACE inhibition. On the other hand, nicotinic acetylcholine receptors expressed in blood vessels have been related to blood pressure regulation. Therefore, we have studied the effects of BPP-10c on acetylcholine receptor function in the PC12 pheochromocytoma cell line, which following induction to neuronal differentiation expresses most of the nicotinic receptor subtypes. BPP-10c did not induce receptor-mediated ion flux, nor potentiated carbamoylcholine-provoked receptor activity as determined by whole-cell recording. This peptide, however, alleviated MK-801-induced inhibition of nicotinic acetylcholine receptor activity. Although more data are needed for understanding the mechanism of the BPP-10c effect on nicotinic receptor activity and its relationship with the anti-hypertensive activity, this work reveals possible therapeutic applications for BPP-10c in establishing normal acetylcholine receptor activity. (C) 2008 Elsevier Inc. All rights reserved.
Palavra-chave Bradykinin-potentiating peptides
Nicotinic acetylcholine receptor
MK-801 inhibition
PC12 pheochromocytoma cells
Idioma Inglês
Financiador Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
Data de publicação 2008-10-01
Publicado em Peptides. New York: Elsevier B.V., v. 29, n. 10, p. 1708-1715, 2008.
ISSN 0196-9781 (Sherpa/Romeo, fator de impacto)
Publicador Elsevier B.V.
Extensão 1708-1715
Fonte http://dx.doi.org/10.1016/j.peptides.2008.06.002
Direito de acesso Acesso restrito
Tipo Artigo
Web of Science WOS:000260284100010
Endereço permanente http://repositorio.unifesp.br/handle/11600/30947

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