Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Outros Autores: | , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1155/2012/987517 http://hdl.handle.net/11449/381 |
Resumo: | Secretory phospholipases A(2) (sPLA(2)) exert proinflammatory actions through lipid mediators. These enzymes have been found to be elevated in many inflammatory disorders such as rheumatoid arthritis, sepsis, and atherosclerosis. The aim of this study was to evaluate the effect of harpalycin 2 (Har2), an isoflavone isolated from Harpalyce brasiliana Benth., in the enzymatic, edematogenic, and myotoxic activities of sPLA2 from Bothrops pirajai, Crotalus durissus terrificus, Apis mellifera, and Naja naja venoms. Har2 inhibits all sPLA(2) tested. PrTX-III (B. pirajai venom) was inhibited at about 58.7%, Cdt F15 (C. d. terrificus venom) at 78.8%, Apis (from bee venom) at 87.7%, and Naja (N. naja venom) at 88.1%. Edema induced by exogenous sPLA(2) administration performed in mice paws showed significant inhibition by Har2 at the initial step. In addition, Har2 also inhibited the myotoxic activity of these sPLA(2)s. In order to understand how Har2 interacts with these enzymes, docking calculations were made, indicating that the residues His48 and Asp49 in the active site of these enzymes interacted powerfully with Har2 through hydrogen bonds. These data pointed to a possible anti-inflammatory activity of Har2 through sPLA(2) inhibition. |
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Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana BenthSecretory phospholipases A(2) (sPLA(2)) exert proinflammatory actions through lipid mediators. These enzymes have been found to be elevated in many inflammatory disorders such as rheumatoid arthritis, sepsis, and atherosclerosis. The aim of this study was to evaluate the effect of harpalycin 2 (Har2), an isoflavone isolated from Harpalyce brasiliana Benth., in the enzymatic, edematogenic, and myotoxic activities of sPLA2 from Bothrops pirajai, Crotalus durissus terrificus, Apis mellifera, and Naja naja venoms. Har2 inhibits all sPLA(2) tested. PrTX-III (B. pirajai venom) was inhibited at about 58.7%, Cdt F15 (C. d. terrificus venom) at 78.8%, Apis (from bee venom) at 87.7%, and Naja (N. naja venom) at 88.1%. Edema induced by exogenous sPLA(2) administration performed in mice paws showed significant inhibition by Har2 at the initial step. In addition, Har2 also inhibited the myotoxic activity of these sPLA(2)s. In order to understand how Har2 interacts with these enzymes, docking calculations were made, indicating that the residues His48 and Asp49 in the active site of these enzymes interacted powerfully with Har2 through hydrogen bonds. These data pointed to a possible anti-inflammatory activity of Har2 through sPLA(2) inhibition.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Fundação Cearense de Apoio ao Desenvolvimento Científico e Tecnológico (FUNCAP)Univ Fed Ceara, Dept Fisiol & Farmacol, BR-60430270 Fortaleza, CE, BrazilUniversidade Federal de Pernambuco (UFPE), Dept Ciencias Farmaceut, BR-50740520 Recife, PE, BrazilUniv Fed Rio Grande do Norte, Dept Quim, BR-50078970 Natal, RN, BrazilUniv Fed Ceara, Ctr NE Aplicacao & Uso Ressonancia Magnet Nucl CE, BR-60455760 Fortaleza, CE, BrazilUniv Estadual Campinas, Inst Biomed, Dept Bioquim, BR-13082862 Campinas, SP, BrazilUniv Estadual Paulista, Unidade Sao Vicente, BR-11330900 Sao Vicente, SP, BrazilUniv Presbiteriana Mackenzie, Ctr Ciencias Biol & Saude, BR-01302970 São Paulo, BrazilUniv Estadual Paulista, Unidade Sao Vicente, BR-11330900 Sao Vicente, SP, BrazilHindawi Publishing CorporationUniversidade Federal do Ceará (UFC)Universidade Federal de Pernambuco (UFPE)Universidade Federal do Rio Grande do Norte (UFRN)Universidade Estadual de Campinas (UNICAMP)Universidade Estadual Paulista (Unesp)Univ Presbiteriana MackenzieXimenes, Rafael M.Rabello, Marcelo M.Araujo, Renata M.Silveira, Edilberto R.Fagundes, Fabio H. R. [UNESP]Diz-Filho, Eduardo B. S. [UNESP]Buzzo, Simone C. [UNESP]Soares, Veronica C. G. [UNESP]Toyama, Daniela de O.Gaeta, Henrique H. [UNESP]Hernandes, Marcelo Z.Monteiro, Helena S. A.Toyama, Marcos H. [UNESP]2014-05-20T13:12:24Z2014-05-20T13:12:24Z2012-01-01info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article9application/pdfhttp://dx.doi.org/10.1155/2012/987517Evidence-based Complementary and Alternative Medicine. New York: Hindawi Publishing Corporation, p. 9, 2012.1741-427Xhttp://hdl.handle.net/11449/38110.1155/2012/987517WOS:000308300500001WOS000308300500001.pdfWeb of Sciencereponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengEvidence-based Complementary and Alternative Medicine2.064info:eu-repo/semantics/openAccess2023-12-08T06:23:18Zoai:repositorio.unesp.br:11449/381Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T19:48:17.589352Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
title |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
spellingShingle |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth Ximenes, Rafael M. |
title_short |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
title_full |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
title_fullStr |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
title_full_unstemmed |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
title_sort |
Inhibition of Neurotoxic Secretory Phospholipases A(2) Enzymatic, Edematogenic, and Myotoxic Activities by Harpalycin 2, an Isoflavone Isolated from Harpalyce brasiliana Benth |
author |
Ximenes, Rafael M. |
author_facet |
Ximenes, Rafael M. Rabello, Marcelo M. Araujo, Renata M. Silveira, Edilberto R. Fagundes, Fabio H. R. [UNESP] Diz-Filho, Eduardo B. S. [UNESP] Buzzo, Simone C. [UNESP] Soares, Veronica C. G. [UNESP] Toyama, Daniela de O. Gaeta, Henrique H. [UNESP] Hernandes, Marcelo Z. Monteiro, Helena S. A. Toyama, Marcos H. [UNESP] |
author_role |
author |
author2 |
Rabello, Marcelo M. Araujo, Renata M. Silveira, Edilberto R. Fagundes, Fabio H. R. [UNESP] Diz-Filho, Eduardo B. S. [UNESP] Buzzo, Simone C. [UNESP] Soares, Veronica C. G. [UNESP] Toyama, Daniela de O. Gaeta, Henrique H. [UNESP] Hernandes, Marcelo Z. Monteiro, Helena S. A. Toyama, Marcos H. [UNESP] |
author2_role |
author author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Federal do Ceará (UFC) Universidade Federal de Pernambuco (UFPE) Universidade Federal do Rio Grande do Norte (UFRN) Universidade Estadual de Campinas (UNICAMP) Universidade Estadual Paulista (Unesp) Univ Presbiteriana Mackenzie |
dc.contributor.author.fl_str_mv |
Ximenes, Rafael M. Rabello, Marcelo M. Araujo, Renata M. Silveira, Edilberto R. Fagundes, Fabio H. R. [UNESP] Diz-Filho, Eduardo B. S. [UNESP] Buzzo, Simone C. [UNESP] Soares, Veronica C. G. [UNESP] Toyama, Daniela de O. Gaeta, Henrique H. [UNESP] Hernandes, Marcelo Z. Monteiro, Helena S. A. Toyama, Marcos H. [UNESP] |
description |
Secretory phospholipases A(2) (sPLA(2)) exert proinflammatory actions through lipid mediators. These enzymes have been found to be elevated in many inflammatory disorders such as rheumatoid arthritis, sepsis, and atherosclerosis. The aim of this study was to evaluate the effect of harpalycin 2 (Har2), an isoflavone isolated from Harpalyce brasiliana Benth., in the enzymatic, edematogenic, and myotoxic activities of sPLA2 from Bothrops pirajai, Crotalus durissus terrificus, Apis mellifera, and Naja naja venoms. Har2 inhibits all sPLA(2) tested. PrTX-III (B. pirajai venom) was inhibited at about 58.7%, Cdt F15 (C. d. terrificus venom) at 78.8%, Apis (from bee venom) at 87.7%, and Naja (N. naja venom) at 88.1%. Edema induced by exogenous sPLA(2) administration performed in mice paws showed significant inhibition by Har2 at the initial step. In addition, Har2 also inhibited the myotoxic activity of these sPLA(2)s. In order to understand how Har2 interacts with these enzymes, docking calculations were made, indicating that the residues His48 and Asp49 in the active site of these enzymes interacted powerfully with Har2 through hydrogen bonds. These data pointed to a possible anti-inflammatory activity of Har2 through sPLA(2) inhibition. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-01-01 2014-05-20T13:12:24Z 2014-05-20T13:12:24Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://dx.doi.org/10.1155/2012/987517 Evidence-based Complementary and Alternative Medicine. New York: Hindawi Publishing Corporation, p. 9, 2012. 1741-427X http://hdl.handle.net/11449/381 10.1155/2012/987517 WOS:000308300500001 WOS000308300500001.pdf |
url |
http://dx.doi.org/10.1155/2012/987517 http://hdl.handle.net/11449/381 |
identifier_str_mv |
Evidence-based Complementary and Alternative Medicine. New York: Hindawi Publishing Corporation, p. 9, 2012. 1741-427X 10.1155/2012/987517 WOS:000308300500001 WOS000308300500001.pdf |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Evidence-based Complementary and Alternative Medicine 2.064 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
9 application/pdf |
dc.publisher.none.fl_str_mv |
Hindawi Publishing Corporation |
publisher.none.fl_str_mv |
Hindawi Publishing Corporation |
dc.source.none.fl_str_mv |
Web of Science reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
_version_ |
1808129119953616896 |