In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Outros Autores: | , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da UNESP |
Texto Completo: | http://dx.doi.org/10.1016/j.jep.2018.12.032 http://hdl.handle.net/11449/188561 |
Resumo: | Ethnopharmacological relevance: The number of bacterial strains that are resistant to multiple conventional antimicrobial agents is increasing. In this context, natural products have been widely used as a strategy to treat diseases caused by bacteria. Infections by Helicobacter pylori have attracted attention because they are directly related to severe gastric medical conditions. Casearia sylvestris Swartz, popularly known as guaçatonga, is largely employed to treat gastric disorders in Brazilian folk medicine. This plant species has aroused much interest mainly because it displays anti-inflammatory activity and can act as an antiulcer agent. Aim of the study: To evaluate the in vitro and in vivo anti-H. pylori action of C. sylvestris leaf derivatives incorporated or not in a nanostructured drug delivery system. Materials and methods: The essential oil (obtained by hydrodistillation) and ethanolic extract (obtained by maceration) were obtained from C. sylvestris leaves. The ethanolic extract was submitted to fractionation through solid phase extraction and column chromatography, to yield the ethanolic fractions. Hydrolyzed casearin J was achieved by submitting isolated casearin J to acid hydrolysis. The derivatives were chemically characterized by nuclear magnetic resonance (NMR), gas chromatography (GC), and gas chromatography-mass spectrometry (GC–MS) analyses. A nanostructured lipid system was used as drug delivery system. To assess the in vitro antibacterial activity of C. sylvestris leaf essential oil, ethanolic extract, and derivatives, microdilution, biofilm, and time-kill assays were performed against H. pylori ATCC 43504. Finally, the in vivo action was investigated by employing male Wistar rats experimentally infected with H. pylori. Results: Many C. sylvestris leaf derivatives presented significant in vitro activity against H. pylori. Among the derivatives, fraction 2 (F2) was the most effective. In vivo tests showed that both the ethanolic extract and F2 decreased the ulcerative lesion size, but only the ethanolic extract eradicated H. pylori from the gastric lesions. Incorporation of plant derivatives in nanostructured lipid system blunted the in vitro action, as demonstrated by the microdilution assay. However, this incorporation improved the ethanolic extract activity against biofilms. Conclusion: C. sylvestris leaf derivatives are effective against H. pylori both in vitro and in vivo. According to phytochemical analyses, these derivatives are rich in terpenoids, which could be related to the anti-H. pylori action. Synergism could also underlie C. sylvestris efficacy judging from the fact that the sub-fractions and isolated compounds had lower activity than the extract. Incorporation in a nanostructured lipid system did not improve the activity of the compounds in our in vivo protocol. |
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In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivativesAntibacterial activityCasearia sylvestrisDiterpenesHelicobacter pyloriMicrodilutionEthnopharmacological relevance: The number of bacterial strains that are resistant to multiple conventional antimicrobial agents is increasing. In this context, natural products have been widely used as a strategy to treat diseases caused by bacteria. Infections by Helicobacter pylori have attracted attention because they are directly related to severe gastric medical conditions. Casearia sylvestris Swartz, popularly known as guaçatonga, is largely employed to treat gastric disorders in Brazilian folk medicine. This plant species has aroused much interest mainly because it displays anti-inflammatory activity and can act as an antiulcer agent. Aim of the study: To evaluate the in vitro and in vivo anti-H. pylori action of C. sylvestris leaf derivatives incorporated or not in a nanostructured drug delivery system. Materials and methods: The essential oil (obtained by hydrodistillation) and ethanolic extract (obtained by maceration) were obtained from C. sylvestris leaves. The ethanolic extract was submitted to fractionation through solid phase extraction and column chromatography, to yield the ethanolic fractions. Hydrolyzed casearin J was achieved by submitting isolated casearin J to acid hydrolysis. The derivatives were chemically characterized by nuclear magnetic resonance (NMR), gas chromatography (GC), and gas chromatography-mass spectrometry (GC–MS) analyses. A nanostructured lipid system was used as drug delivery system. To assess the in vitro antibacterial activity of C. sylvestris leaf essential oil, ethanolic extract, and derivatives, microdilution, biofilm, and time-kill assays were performed against H. pylori ATCC 43504. Finally, the in vivo action was investigated by employing male Wistar rats experimentally infected with H. pylori. Results: Many C. sylvestris leaf derivatives presented significant in vitro activity against H. pylori. Among the derivatives, fraction 2 (F2) was the most effective. In vivo tests showed that both the ethanolic extract and F2 decreased the ulcerative lesion size, but only the ethanolic extract eradicated H. pylori from the gastric lesions. Incorporation of plant derivatives in nanostructured lipid system blunted the in vitro action, as demonstrated by the microdilution assay. However, this incorporation improved the ethanolic extract activity against biofilms. Conclusion: C. sylvestris leaf derivatives are effective against H. pylori both in vitro and in vivo. According to phytochemical analyses, these derivatives are rich in terpenoids, which could be related to the anti-H. pylori action. Synergism could also underlie C. sylvestris efficacy judging from the fact that the sub-fractions and isolated compounds had lower activity than the extract. Incorporation in a nanostructured lipid system did not improve the activity of the compounds in our in vivo protocol.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Department of Biological Sciences School of Pharmaceutical Sciences São Paulo State University (UNESP)Department of Natural Active Principles and Toxicology School of Pharmaceutical Sciences São Paulo State University (UNESP)Department of Chemistry Faculty of Philosophy Sciences and Letters USPDepartment of Drugs and Medicines School of Pharmaceutical Sciences São Paulo State University (UNESP)Department of Biological Sciences School of Pharmaceutical Sciences São Paulo State University (UNESP)Department of Natural Active Principles and Toxicology School of Pharmaceutical Sciences São Paulo State University (UNESP)Department of Drugs and Medicines School of Pharmaceutical Sciences São Paulo State University (UNESP)FAPESP: #2016/08559-5Universidade Estadual Paulista (Unesp)Universidade de São Paulo (USP)Spósito, Larissa [UNESP]Oda, Fernando Bombarda [UNESP]Vieira, Júlia Hunger [UNESP]Carvalho, Flávio Alexandre [UNESP]dos Santos Ramos, Matheus Aparecido [UNESP]de Castro, Rogério Cardoso [UNESP]Crevelin, Eduardo JoséCrotti, Antônio Eduardo MillerSantos, André Gonzaga [UNESP]da Silva, Patrícia Bento [UNESP]Chorilli, Marlus [UNESP]Bauab, Taís Maria [UNESP]2019-10-06T16:12:04Z2019-10-06T16:12:04Z2019-04-06info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article1-12http://dx.doi.org/10.1016/j.jep.2018.12.032Journal of Ethnopharmacology, v. 233, p. 1-12.1872-75730378-8741http://hdl.handle.net/11449/18856110.1016/j.jep.2018.12.0322-s2.0-85059364059Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengJournal of Ethnopharmacologyinfo:eu-repo/semantics/openAccess2024-06-24T14:51:40Zoai:repositorio.unesp.br:11449/188561Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T16:30:07.712694Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
title |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
spellingShingle |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives Spósito, Larissa [UNESP] Antibacterial activity Casearia sylvestris Diterpenes Helicobacter pylori Microdilution |
title_short |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
title_full |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
title_fullStr |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
title_full_unstemmed |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
title_sort |
In vitro and in vivo anti-Helicobacter pylori activity of Casearia sylvestris leaf derivatives |
author |
Spósito, Larissa [UNESP] |
author_facet |
Spósito, Larissa [UNESP] Oda, Fernando Bombarda [UNESP] Vieira, Júlia Hunger [UNESP] Carvalho, Flávio Alexandre [UNESP] dos Santos Ramos, Matheus Aparecido [UNESP] de Castro, Rogério Cardoso [UNESP] Crevelin, Eduardo José Crotti, Antônio Eduardo Miller Santos, André Gonzaga [UNESP] da Silva, Patrícia Bento [UNESP] Chorilli, Marlus [UNESP] Bauab, Taís Maria [UNESP] |
author_role |
author |
author2 |
Oda, Fernando Bombarda [UNESP] Vieira, Júlia Hunger [UNESP] Carvalho, Flávio Alexandre [UNESP] dos Santos Ramos, Matheus Aparecido [UNESP] de Castro, Rogério Cardoso [UNESP] Crevelin, Eduardo José Crotti, Antônio Eduardo Miller Santos, André Gonzaga [UNESP] da Silva, Patrícia Bento [UNESP] Chorilli, Marlus [UNESP] Bauab, Taís Maria [UNESP] |
author2_role |
author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Universidade Estadual Paulista (Unesp) Universidade de São Paulo (USP) |
dc.contributor.author.fl_str_mv |
Spósito, Larissa [UNESP] Oda, Fernando Bombarda [UNESP] Vieira, Júlia Hunger [UNESP] Carvalho, Flávio Alexandre [UNESP] dos Santos Ramos, Matheus Aparecido [UNESP] de Castro, Rogério Cardoso [UNESP] Crevelin, Eduardo José Crotti, Antônio Eduardo Miller Santos, André Gonzaga [UNESP] da Silva, Patrícia Bento [UNESP] Chorilli, Marlus [UNESP] Bauab, Taís Maria [UNESP] |
dc.subject.por.fl_str_mv |
Antibacterial activity Casearia sylvestris Diterpenes Helicobacter pylori Microdilution |
topic |
Antibacterial activity Casearia sylvestris Diterpenes Helicobacter pylori Microdilution |
description |
Ethnopharmacological relevance: The number of bacterial strains that are resistant to multiple conventional antimicrobial agents is increasing. In this context, natural products have been widely used as a strategy to treat diseases caused by bacteria. Infections by Helicobacter pylori have attracted attention because they are directly related to severe gastric medical conditions. Casearia sylvestris Swartz, popularly known as guaçatonga, is largely employed to treat gastric disorders in Brazilian folk medicine. This plant species has aroused much interest mainly because it displays anti-inflammatory activity and can act as an antiulcer agent. Aim of the study: To evaluate the in vitro and in vivo anti-H. pylori action of C. sylvestris leaf derivatives incorporated or not in a nanostructured drug delivery system. Materials and methods: The essential oil (obtained by hydrodistillation) and ethanolic extract (obtained by maceration) were obtained from C. sylvestris leaves. The ethanolic extract was submitted to fractionation through solid phase extraction and column chromatography, to yield the ethanolic fractions. Hydrolyzed casearin J was achieved by submitting isolated casearin J to acid hydrolysis. The derivatives were chemically characterized by nuclear magnetic resonance (NMR), gas chromatography (GC), and gas chromatography-mass spectrometry (GC–MS) analyses. A nanostructured lipid system was used as drug delivery system. To assess the in vitro antibacterial activity of C. sylvestris leaf essential oil, ethanolic extract, and derivatives, microdilution, biofilm, and time-kill assays were performed against H. pylori ATCC 43504. Finally, the in vivo action was investigated by employing male Wistar rats experimentally infected with H. pylori. Results: Many C. sylvestris leaf derivatives presented significant in vitro activity against H. pylori. Among the derivatives, fraction 2 (F2) was the most effective. In vivo tests showed that both the ethanolic extract and F2 decreased the ulcerative lesion size, but only the ethanolic extract eradicated H. pylori from the gastric lesions. Incorporation of plant derivatives in nanostructured lipid system blunted the in vitro action, as demonstrated by the microdilution assay. However, this incorporation improved the ethanolic extract activity against biofilms. Conclusion: C. sylvestris leaf derivatives are effective against H. pylori both in vitro and in vivo. According to phytochemical analyses, these derivatives are rich in terpenoids, which could be related to the anti-H. pylori action. Synergism could also underlie C. sylvestris efficacy judging from the fact that the sub-fractions and isolated compounds had lower activity than the extract. Incorporation in a nanostructured lipid system did not improve the activity of the compounds in our in vivo protocol. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-10-06T16:12:04Z 2019-10-06T16:12:04Z 2019-04-06 |
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/10.1016/j.jep.2018.12.032 Journal of Ethnopharmacology, v. 233, p. 1-12. 1872-7573 0378-8741 http://hdl.handle.net/11449/188561 10.1016/j.jep.2018.12.032 2-s2.0-85059364059 |
url |
http://dx.doi.org/10.1016/j.jep.2018.12.032 http://hdl.handle.net/11449/188561 |
identifier_str_mv |
Journal of Ethnopharmacology, v. 233, p. 1-12. 1872-7573 0378-8741 10.1016/j.jep.2018.12.032 2-s2.0-85059364059 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Journal of Ethnopharmacology |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
1-12 |
dc.source.none.fl_str_mv |
Scopus 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_ |
1808128661650407424 |