Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)

Detalhes bibliográficos
Autor(a) principal: Jorge, Roberta Jeane Bezerra
Data de Publicação: 2011
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional da Universidade Federal do Ceará (UFC)
Texto Completo: http://www.repositorio.ufc.br/handle/riufc/2625
Resumo: Snake envenoming is an important health problem widespread in tropical countries. Among the most dangerous species in South America is the Bothrops genus. Snakebites accidents caused by Bothrops species quickly develop severe local tissue damage, including swelling, hemorrhage, myonecrosis, skin ulceration and pain. The traditional serum therapy has limited effectiveness against these effects. Natural compounds isolated from plants, mainly from species used in folk medicine to treat snakebite, are a good choice to find new lead compounds to improve the snakebite treatment and minimize the sequelae of the victims. Antiophidic activity of the new steroidal alkaloids: 22-epoxy-solanide-1,4,9-trien-3-one (1), 22-epoxy-solanide-1,4-dien-3-one (2) and 3,9-dihydroxy-22,23-epoxy-9,10-secosolanida-1,3,5(10)-triene (3) isolated from leaves of Solanum campaniforme was tested through inhibition of phospholipasic activity, proteolytic activity, myotoxicity, hemorrhage and necrosis induced by Bothrops pauloensis venom. The three compounds were able to complete inhibit the creatine kinase release from skeletal muscles and minimize the histological changes, without inhibiting the phospholipasic A2 activity of whole venom. The inhibition of myotoxicity appears to be independent of catalytic activity of phospholipase A2 (PLA2) and may be related to inhibition of PLA2 Lys 49, enzymatically inactive, and / or an indirect action on metalloproteinases. There was also, the inhibition of proteolytic activity of the venom on different substrates with three alkaloids. Hemorrhage as well as skin necrosis, both induced by metalloproteases present in the venom, were reduced in the presence of alkaloids 1 and 2 , but not with the alkaloid 3. Inhibition of proteolytic activities and the reduction of hemorrhagic and necrotizing effects induced by vBp, mainly attributed to the alkaloids 1 and 2, may be associated with the interaction of these compounds with the metalloproteases present in the venom and / or divalent metal ions required for their action.
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spelling Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)Inhibition of the local effects of Bothrops pauloensis by steroidal alkaloids from Solanum campaniforme Roem. & Schult. (Solanaceae)Alcaloides de SolanáceasNecroseSnake envenoming is an important health problem widespread in tropical countries. Among the most dangerous species in South America is the Bothrops genus. Snakebites accidents caused by Bothrops species quickly develop severe local tissue damage, including swelling, hemorrhage, myonecrosis, skin ulceration and pain. The traditional serum therapy has limited effectiveness against these effects. Natural compounds isolated from plants, mainly from species used in folk medicine to treat snakebite, are a good choice to find new lead compounds to improve the snakebite treatment and minimize the sequelae of the victims. Antiophidic activity of the new steroidal alkaloids: 22-epoxy-solanide-1,4,9-trien-3-one (1), 22-epoxy-solanide-1,4-dien-3-one (2) and 3,9-dihydroxy-22,23-epoxy-9,10-secosolanida-1,3,5(10)-triene (3) isolated from leaves of Solanum campaniforme was tested through inhibition of phospholipasic activity, proteolytic activity, myotoxicity, hemorrhage and necrosis induced by Bothrops pauloensis venom. The three compounds were able to complete inhibit the creatine kinase release from skeletal muscles and minimize the histological changes, without inhibiting the phospholipasic A2 activity of whole venom. The inhibition of myotoxicity appears to be independent of catalytic activity of phospholipase A2 (PLA2) and may be related to inhibition of PLA2 Lys 49, enzymatically inactive, and / or an indirect action on metalloproteinases. There was also, the inhibition of proteolytic activity of the venom on different substrates with three alkaloids. Hemorrhage as well as skin necrosis, both induced by metalloproteases present in the venom, were reduced in the presence of alkaloids 1 and 2 , but not with the alkaloid 3. Inhibition of proteolytic activities and the reduction of hemorrhagic and necrotizing effects induced by vBp, mainly attributed to the alkaloids 1 and 2, may be associated with the interaction of these compounds with the metalloproteases present in the venom and / or divalent metal ions required for their action.Envenenamentos por serpentes são um importante problema de saúde muito difundido em países tropicais. Entre as espécies mais perigosas da América do Sul encontra-se o gênero Bothrops. Acidentes ofídicos causados por espécies Bothrops podem desenvolver rapidamente dano tecidual local grave, incluindo edema, hemorragia, mionecrose, ulceração de pele e dor. A soroterapia tradicional tem eficácia limitada contra esses efeitos. Compostos naturais isolados de plantas, principalmente a partir de espécies usadas na medicina popular para tratar envenenamentos de serpente, podem ser uma boa alternativa para encontrar novos compostos para melhorar o tratamento do envenenamento e minimizar as sequelas das vítimas. Atividade antiofídica dos novos alcalóides esteroidais: 1 -22,23-epoxi-solanida-1,4,9-trien-3-ona (1), 2-22,23-epoxi-solanida-1,4-dien-3-ona (2) 3-3,9-dihidroxi-22,23-epoxi-9-10-secosolanida-1,3,5(10)-trieno (3) isolados das folhas de Solanum campaniforme foram testados através da inibição da atividade fosfolipásica, atividade proteolítica, miotoxicidade, hemorragia e necrose induzidas pelo veneno de Bothrops pauloensis. Os três compostos foram capazes de inibir completamente a liberação de creatina quinase de músculos estriados esqueléticos e minimizar as alterações histológicas sem inibir a atividade fosfolipásica A2 do veneno total de B. pauloensis. A inibição da miotoxicidade parece ser independente da atividade catalítica de fosfolipase (PLA2) e pode estar relacionada à inibição da PLA2 Lys 49, enzimaticamente inativas, e / ou uma ação indireta sobre metaloproteinases. Houve também, a inibição da atividade proteolitica do veneno em diferentes substratos com os três alcaloides A hemorragia, bem como a necrose de pele, ambas induzidas por metaloproteases presentes no veneno, foram reduzidas na presença dos alcalóides 1 e 2, mas não com o alcalóide 3. A inibição das atividades proteolíticas e a redução dos efeitos hemorrágicos e necrosantes induzidas pelo vBp, principalmente atribuídos aos alcalóides 1 e 2, podem estar associadas com a interação destes compostos com as metaloproteases presentes no veneno e/ou com íons metálicos bivalentes necessários para sua ação.Monteiro, Helena Serra AzulJorge, Roberta Jeane Bezerra2012-05-14T16:02:25Z2012-05-14T16:02:25Z2011info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfJORGE, R. J. B. Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult (SOLANACEAE). 2011. 86 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, 2011.http://www.repositorio.ufc.br/handle/riufc/2625porreponame:Repositório Institucional da Universidade Federal do Ceará (UFC)instname:Universidade Federal do Ceará (UFC)instacron:UFCinfo:eu-repo/semantics/openAccess2019-10-25T12:55:58Zoai:repositorio.ufc.br:riufc/2625Repositório InstitucionalPUBhttp://www.repositorio.ufc.br/ri-oai/requestbu@ufc.br || repositorio@ufc.bropendoar:2024-09-11T18:37:50.686789Repositório Institucional da Universidade Federal do Ceará (UFC) - Universidade Federal do Ceará (UFC)false
dc.title.none.fl_str_mv Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
Inhibition of the local effects of Bothrops pauloensis by steroidal alkaloids from Solanum campaniforme Roem. & Schult. (Solanaceae)
title Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
spellingShingle Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
Jorge, Roberta Jeane Bezerra
Alcaloides de Solanáceas
Necrose
title_short Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
title_full Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
title_fullStr Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
title_full_unstemmed Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
title_sort Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult. (Solanaceae)
author Jorge, Roberta Jeane Bezerra
author_facet Jorge, Roberta Jeane Bezerra
author_role author
dc.contributor.none.fl_str_mv Monteiro, Helena Serra Azul
dc.contributor.author.fl_str_mv Jorge, Roberta Jeane Bezerra
dc.subject.por.fl_str_mv Alcaloides de Solanáceas
Necrose
topic Alcaloides de Solanáceas
Necrose
description Snake envenoming is an important health problem widespread in tropical countries. Among the most dangerous species in South America is the Bothrops genus. Snakebites accidents caused by Bothrops species quickly develop severe local tissue damage, including swelling, hemorrhage, myonecrosis, skin ulceration and pain. The traditional serum therapy has limited effectiveness against these effects. Natural compounds isolated from plants, mainly from species used in folk medicine to treat snakebite, are a good choice to find new lead compounds to improve the snakebite treatment and minimize the sequelae of the victims. Antiophidic activity of the new steroidal alkaloids: 22-epoxy-solanide-1,4,9-trien-3-one (1), 22-epoxy-solanide-1,4-dien-3-one (2) and 3,9-dihydroxy-22,23-epoxy-9,10-secosolanida-1,3,5(10)-triene (3) isolated from leaves of Solanum campaniforme was tested through inhibition of phospholipasic activity, proteolytic activity, myotoxicity, hemorrhage and necrosis induced by Bothrops pauloensis venom. The three compounds were able to complete inhibit the creatine kinase release from skeletal muscles and minimize the histological changes, without inhibiting the phospholipasic A2 activity of whole venom. The inhibition of myotoxicity appears to be independent of catalytic activity of phospholipase A2 (PLA2) and may be related to inhibition of PLA2 Lys 49, enzymatically inactive, and / or an indirect action on metalloproteinases. There was also, the inhibition of proteolytic activity of the venom on different substrates with three alkaloids. Hemorrhage as well as skin necrosis, both induced by metalloproteases present in the venom, were reduced in the presence of alkaloids 1 and 2 , but not with the alkaloid 3. Inhibition of proteolytic activities and the reduction of hemorrhagic and necrotizing effects induced by vBp, mainly attributed to the alkaloids 1 and 2, may be associated with the interaction of these compounds with the metalloproteases present in the venom and / or divalent metal ions required for their action.
publishDate 2011
dc.date.none.fl_str_mv 2011
2012-05-14T16:02:25Z
2012-05-14T16:02:25Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv JORGE, R. J. B. Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult (SOLANACEAE). 2011. 86 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, 2011.
http://www.repositorio.ufc.br/handle/riufc/2625
identifier_str_mv JORGE, R. J. B. Inibição dos efeitos locais do veneno de Bothrops pauloensis por alcalóides esteroidais de Solanum campaniforme Roem. & Schult (SOLANACEAE). 2011. 86 f. Dissertação (Mestrado em Farmacologia) - Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, 2011.
url http://www.repositorio.ufc.br/handle/riufc/2625
dc.language.iso.fl_str_mv por
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dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Institucional da Universidade Federal do Ceará (UFC)
instname:Universidade Federal do Ceará (UFC)
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instname_str Universidade Federal do Ceará (UFC)
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reponame_str Repositório Institucional da Universidade Federal do Ceará (UFC)
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