Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Biblioteca Digital de Teses e Dissertações da UFPB |
Texto Completo: | https://repositorio.ufpb.br/jspui/handle/tede/6775 |
Resumo: | Heterocyclic compounds are the biggest sources of synthetic drugs and have grown exponentially with important applications in the pharmaceutical industry. Amongst the heterocyclic compounds, it has been highlighted the thiophenes category and its derivatives, which call attention for presenting important pharmacological actions, especially analgesic and the anti-inflammatory ones. The present study aims to investigate the Antinociceptive, anti-inflammatory activity and acute pre-clinical from tiophenic derivative 6CN10. The behavioral pharmacological screening of treated animals (250, 500 and 1000 mg/kg) showed changes, such as analgesia and ambulation reduction. There was no death of animals or the presence of toxic signs. From the pharmacological screening was determined the use of three doses (25, 50 and 100 mg/kg) for other studies. In the Rota rod and open field tests, there were no changes in the motor coordination of animals, discarding the possibility of a myorelaxant effect. Through models of nociception inducers, such as the abdominal constriction induced by acetic acid, formalin and hot plate, it was noticed a dose-dependent Antinociceptive activity of 6CN10. Such effect did not show itself to be associated to the opioid via of central analgesia, once this derivative did not produce any significant effect in the hot plate test, and because it has not been blocked by naloxone, an pattern antagonist opioid. The 6CN10 inhibited significantly the time of paw licking in both phases of the formalin test, especially at the inflammatory phase, being needed an analysis of the anti-inflammatory activity of the derivative. For this purpose, it was used the model of induced peritonitis by carrageenan, where there was inhibition of neutrophil migration to the intra-peritoneal cavity of treated animals, demonstrating the anti-inflammatory activity of 6CN10. In the acute toxicological study after treatment with the dosage of 1000 mg/kg 6CN10, it was observed a reduction in the food intake and in the body weight in females. The examined hematological parameters remained unaffected. The treatment was able to raise levels of ALT and AST, in both sexes, corroborating with histopathological findings that showed evidence of Hepatotoxicity. The kidneys, heart and lungs showed no histological particularities. Therefore, the results presented in this study showed a promising effect of 6CN10 as an analgesic and anti-inflammatory substance, however its security should be better investigated. |
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Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongosAntinociceptive and Anti-inflammatory Effect of the 2-[4-nitro-benzylidene)-amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3carbonitrile(6CN10) in miceDerivado do tiofenoAtividade AntinociceptivaAtividade AntiinflamatóriaAvaliação ToxicológicaThiophene derivativeAntinociceptive activityAnti-inflammatory activityToxicological evaluationCNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIAHeterocyclic compounds are the biggest sources of synthetic drugs and have grown exponentially with important applications in the pharmaceutical industry. Amongst the heterocyclic compounds, it has been highlighted the thiophenes category and its derivatives, which call attention for presenting important pharmacological actions, especially analgesic and the anti-inflammatory ones. The present study aims to investigate the Antinociceptive, anti-inflammatory activity and acute pre-clinical from tiophenic derivative 6CN10. The behavioral pharmacological screening of treated animals (250, 500 and 1000 mg/kg) showed changes, such as analgesia and ambulation reduction. There was no death of animals or the presence of toxic signs. From the pharmacological screening was determined the use of three doses (25, 50 and 100 mg/kg) for other studies. In the Rota rod and open field tests, there were no changes in the motor coordination of animals, discarding the possibility of a myorelaxant effect. Through models of nociception inducers, such as the abdominal constriction induced by acetic acid, formalin and hot plate, it was noticed a dose-dependent Antinociceptive activity of 6CN10. Such effect did not show itself to be associated to the opioid via of central analgesia, once this derivative did not produce any significant effect in the hot plate test, and because it has not been blocked by naloxone, an pattern antagonist opioid. The 6CN10 inhibited significantly the time of paw licking in both phases of the formalin test, especially at the inflammatory phase, being needed an analysis of the anti-inflammatory activity of the derivative. For this purpose, it was used the model of induced peritonitis by carrageenan, where there was inhibition of neutrophil migration to the intra-peritoneal cavity of treated animals, demonstrating the anti-inflammatory activity of 6CN10. In the acute toxicological study after treatment with the dosage of 1000 mg/kg 6CN10, it was observed a reduction in the food intake and in the body weight in females. The examined hematological parameters remained unaffected. The treatment was able to raise levels of ALT and AST, in both sexes, corroborating with histopathological findings that showed evidence of Hepatotoxicity. The kidneys, heart and lungs showed no histological particularities. Therefore, the results presented in this study showed a promising effect of 6CN10 as an analgesic and anti-inflammatory substance, however its security should be better investigated.Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorOs compostos heterocíclicos são as maiores fontes de fármacos sintéticos e têm crescido exponencialmente apresentando importantes aplicações na indústria farmacêutica. Entre os compostos heterocíclicos destacamos a classes dos tiofenos e seus derivados, que despertam grande interesse por apresentarem ações farmacológicas importantes, sobretudo, analgésica e antiinflamatória. O presente estudo se propôs a investigar a atividade antinociceptiva, antiinflamatória e a toxicidade pré-clínica aguda do derivado tiofênico 6CN10. A triagem farmacológica comportamental dos animais tratados (250, 500 e 1000 mg/kg) demonstrou alterações, tais como, analgesia e redução da ambulação. Não houve morte dos animais, nem presença de sinais tóxicos. A partir da triagem farmacológica determinou-se a utilização de três doses (25, 50 e 100 mg/kg) para os demais estudos. Nos testes de rota rod e campo aberto, não foram observadas alterações na coordenação motora dos animais, descartando a possibilidade de um efeito miorelaxante. Por meio de modelos indutores de nocicepção, como os testes das contorções abdominais induzidas por ácido acético, da formalina e da placa quente, foi observado uma atividade antinociceptiva dose-dependente de 6CN10. Tal efeito não demonstrou associar-se à via opióide de analgesia central, uma vez que este derivado não produziu efeito significativo no teste da placa quente, e por não ter sido bloqueado pela naloxona, um antagonista opióide padrão. 6CN10 inibiu significativamente o tempo de lambedura da pata em ambas as fases do teste formalina, sobretudo na fase inflamatória, se fazendo necessário uma análise da atividade antiinflamatória do derivado. Para este fim, utilizou-se o modelo de peritonite induzida pela carragenina, onde houve inibição da migração de neutrófilos para a cavidade intraperitoneal dos animais tratados, demonstrando a atividade antiinflamatória do 6CN10. No estudo toxicológico agudo após tratamento com a dose de 1000 mg/kg de 6CN10, foi observado redução da ingestão de alimentos e peso corpóreo nas fêmeas tratadas. Os parâmetros hematológicos analisados permaneceram inalterados. O tratamento foi capaz de elevar os níveis de ALT e AST, em ambos os sexos, corroborando com os achados histopatológicos que mostraram indícios de hepatotoxicidade. Os rins, coração e pulmões não apresentaram particularidades histológicas. Portanto, os resultados apresentados neste estudo evidenciaram um efeito promissor de 6CN10 como substância analgésica e antiinflamatória, contudo a sua segurança deve ser melhor investigada.Universidade Federal da ParaíbaBRFarmacologiaPrograma de Pós Graduação em Produtos Naturais e Sintéticos BioativosUFPBDiniz, Margareth de Fátima Formiga Melohttp://lattes.cnpq.br/4173269414899195Mota, Clélia de Alencar Xavier2015-05-14T12:59:49Z2018-07-21T00:24:55Z2014-07-032018-07-21T00:24:55Z2012-08-27info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfMOTA, Clélia de Alencar Xavier. Antinociceptive and Anti-inflammatory Effect of the 2-[4-nitro-benzylidene)-amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3carbonitrile(6CN10) in mice. 2012. 150 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal da Paraíba, João Pessoa, 2012.https://repositorio.ufpb.br/jspui/handle/tede/6775porinfo:eu-repo/semantics/openAccessreponame:Biblioteca Digital de Teses e Dissertações da UFPBinstname:Universidade Federal da Paraíba (UFPB)instacron:UFPB2018-09-06T01:45:48Zoai:repositorio.ufpb.br:tede/6775Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufpb.br/PUBhttp://tede.biblioteca.ufpb.br:8080/oai/requestdiretoria@ufpb.br|| diretoria@ufpb.bropendoar:2018-09-06T01:45:48Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB)false |
dc.title.none.fl_str_mv |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos Antinociceptive and Anti-inflammatory Effect of the 2-[4-nitro-benzylidene)-amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3carbonitrile(6CN10) in mice |
title |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
spellingShingle |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos Mota, Clélia de Alencar Xavier Derivado do tiofeno Atividade Antinociceptiva Atividade Antiinflamatória Avaliação Toxicológica Thiophene derivative Antinociceptive activity Anti-inflammatory activity Toxicological evaluation CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
title_short |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
title_full |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
title_fullStr |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
title_full_unstemmed |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
title_sort |
Efeito antinociceptivo e antiinflamatório do 2-[(4-nitro-benzilideno)-amino]-4,5,6,7-tetraidro-benzo[b]tiofeno-3-carbonitrila (6CN10) em camundongos |
author |
Mota, Clélia de Alencar Xavier |
author_facet |
Mota, Clélia de Alencar Xavier |
author_role |
author |
dc.contributor.none.fl_str_mv |
Diniz, Margareth de Fátima Formiga Melo http://lattes.cnpq.br/4173269414899195 |
dc.contributor.author.fl_str_mv |
Mota, Clélia de Alencar Xavier |
dc.subject.por.fl_str_mv |
Derivado do tiofeno Atividade Antinociceptiva Atividade Antiinflamatória Avaliação Toxicológica Thiophene derivative Antinociceptive activity Anti-inflammatory activity Toxicological evaluation CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
topic |
Derivado do tiofeno Atividade Antinociceptiva Atividade Antiinflamatória Avaliação Toxicológica Thiophene derivative Antinociceptive activity Anti-inflammatory activity Toxicological evaluation CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA |
description |
Heterocyclic compounds are the biggest sources of synthetic drugs and have grown exponentially with important applications in the pharmaceutical industry. Amongst the heterocyclic compounds, it has been highlighted the thiophenes category and its derivatives, which call attention for presenting important pharmacological actions, especially analgesic and the anti-inflammatory ones. The present study aims to investigate the Antinociceptive, anti-inflammatory activity and acute pre-clinical from tiophenic derivative 6CN10. The behavioral pharmacological screening of treated animals (250, 500 and 1000 mg/kg) showed changes, such as analgesia and ambulation reduction. There was no death of animals or the presence of toxic signs. From the pharmacological screening was determined the use of three doses (25, 50 and 100 mg/kg) for other studies. In the Rota rod and open field tests, there were no changes in the motor coordination of animals, discarding the possibility of a myorelaxant effect. Through models of nociception inducers, such as the abdominal constriction induced by acetic acid, formalin and hot plate, it was noticed a dose-dependent Antinociceptive activity of 6CN10. Such effect did not show itself to be associated to the opioid via of central analgesia, once this derivative did not produce any significant effect in the hot plate test, and because it has not been blocked by naloxone, an pattern antagonist opioid. The 6CN10 inhibited significantly the time of paw licking in both phases of the formalin test, especially at the inflammatory phase, being needed an analysis of the anti-inflammatory activity of the derivative. For this purpose, it was used the model of induced peritonitis by carrageenan, where there was inhibition of neutrophil migration to the intra-peritoneal cavity of treated animals, demonstrating the anti-inflammatory activity of 6CN10. In the acute toxicological study after treatment with the dosage of 1000 mg/kg 6CN10, it was observed a reduction in the food intake and in the body weight in females. The examined hematological parameters remained unaffected. The treatment was able to raise levels of ALT and AST, in both sexes, corroborating with histopathological findings that showed evidence of Hepatotoxicity. The kidneys, heart and lungs showed no histological particularities. Therefore, the results presented in this study showed a promising effect of 6CN10 as an analgesic and anti-inflammatory substance, however its security should be better investigated. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-08-27 2014-07-03 2015-05-14T12:59:49Z 2018-07-21T00:24:55Z 2018-07-21T00:24:55Z |
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 |
MOTA, Clélia de Alencar Xavier. Antinociceptive and Anti-inflammatory Effect of the 2-[4-nitro-benzylidene)-amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3carbonitrile(6CN10) in mice. 2012. 150 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal da Paraíba, João Pessoa, 2012. https://repositorio.ufpb.br/jspui/handle/tede/6775 |
identifier_str_mv |
MOTA, Clélia de Alencar Xavier. Antinociceptive and Anti-inflammatory Effect of the 2-[4-nitro-benzylidene)-amino]-4,5,6,7-tetrahydro-benzo[b]thiophene-3carbonitrile(6CN10) in mice. 2012. 150 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal da Paraíba, João Pessoa, 2012. |
url |
https://repositorio.ufpb.br/jspui/handle/tede/6775 |
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por |
language |
por |
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info:eu-repo/semantics/openAccess |
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openAccess |
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application/pdf |
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Universidade Federal da Paraíba BR Farmacologia Programa de Pós Graduação em Produtos Naturais e Sintéticos Bioativos UFPB |
publisher.none.fl_str_mv |
Universidade Federal da Paraíba BR Farmacologia Programa de Pós Graduação em Produtos Naturais e Sintéticos Bioativos UFPB |
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reponame:Biblioteca Digital de Teses e Dissertações da UFPB instname:Universidade Federal da Paraíba (UFPB) instacron:UFPB |
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Universidade Federal da Paraíba (UFPB) |
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UFPB |
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UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB |
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Biblioteca Digital de Teses e Dissertações da UFPB - Universidade Federal da Paraíba (UFPB) |
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diretoria@ufpb.br|| diretoria@ufpb.br |
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