Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity
Autor(a) principal: | |
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Data de Publicação: | 2009 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Journal of the Brazilian Chemical Society (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000600009 |
Resumo: | Endopleura uchi (Huber) Cuatrec. is an Amazon species traditionally used for the treatment of inflammations and female disorders. Pure bergenin was isolated from the methanolic extract of bark of E. uchi, firstly by using liquid-liquid partition chromatography followed by column chromatography over Sephadex LH-20 and then silica gel 60 flash chromatography. The structure of bergenin was identified on the basis of its NMR spectra. The in vitro anti-inflammatory activity was determined by the measurement of the inhibitory concentration (IC) of bergenin against three key enzymes: COX-1, COX-2 (cyclooxygenases) and phospholipase A2 (PLA2). These enzymes were selected because they are important targets for the discovery of new anti-inflammatory drugs associated with the biosynthesis of prostaglandins. The IC50 of bergenin for phopholipase A2 was determined as 156.6 µmol L-1 and bergenin was not considered active as compared to the positive control, tioetheramide PC. Bergenin did not inhibit COX-1 as well (IC50 = 107.2 µmol L-1). However, bergenin selectively inhibited COX-2 (IC50 = 1.2 µmol L-1). Because of the use of E. uchi in traditional medicine, bergenin was quantified in teas prepared as prescribed in traditional medicine by RP-HPLC as being 3% in the bark of E. uchi. The inhibitory activity towards COX-2 is important, since selective inhibitors of COX-2 have been clinically validated as anti-inflammatory therapeutics due to their enhanced gastrointestinal safety. |
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Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activityCOX-1COX-2PLA2quantificationHumiriaceaeEndopleura uchiEndopleura uchi (Huber) Cuatrec. is an Amazon species traditionally used for the treatment of inflammations and female disorders. Pure bergenin was isolated from the methanolic extract of bark of E. uchi, firstly by using liquid-liquid partition chromatography followed by column chromatography over Sephadex LH-20 and then silica gel 60 flash chromatography. The structure of bergenin was identified on the basis of its NMR spectra. The in vitro anti-inflammatory activity was determined by the measurement of the inhibitory concentration (IC) of bergenin against three key enzymes: COX-1, COX-2 (cyclooxygenases) and phospholipase A2 (PLA2). These enzymes were selected because they are important targets for the discovery of new anti-inflammatory drugs associated with the biosynthesis of prostaglandins. The IC50 of bergenin for phopholipase A2 was determined as 156.6 µmol L-1 and bergenin was not considered active as compared to the positive control, tioetheramide PC. Bergenin did not inhibit COX-1 as well (IC50 = 107.2 µmol L-1). However, bergenin selectively inhibited COX-2 (IC50 = 1.2 µmol L-1). Because of the use of E. uchi in traditional medicine, bergenin was quantified in teas prepared as prescribed in traditional medicine by RP-HPLC as being 3% in the bark of E. uchi. The inhibitory activity towards COX-2 is important, since selective inhibitors of COX-2 have been clinically validated as anti-inflammatory therapeutics due to their enhanced gastrointestinal safety.Sociedade Brasileira de Química2009-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000600009Journal of the Brazilian Chemical Society v.20 n.6 2009reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532009000600009info:eu-repo/semantics/openAccessNunomura,Rita C. S.Oliveira,Viviane G.Da Silva,Saulo L.Nunomura,Sergio M.eng2009-08-04T00:00:00Zoai:scielo:S0103-50532009000600009Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2009-08-04T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false |
dc.title.none.fl_str_mv |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
title |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
spellingShingle |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity Nunomura,Rita C. S. COX-1 COX-2 PLA2 quantification Humiriaceae Endopleura uchi |
title_short |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
title_full |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
title_fullStr |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
title_full_unstemmed |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
title_sort |
Characterization of bergenin in Endopleura uchi bark and its anti-inflammatory activity |
author |
Nunomura,Rita C. S. |
author_facet |
Nunomura,Rita C. S. Oliveira,Viviane G. Da Silva,Saulo L. Nunomura,Sergio M. |
author_role |
author |
author2 |
Oliveira,Viviane G. Da Silva,Saulo L. Nunomura,Sergio M. |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Nunomura,Rita C. S. Oliveira,Viviane G. Da Silva,Saulo L. Nunomura,Sergio M. |
dc.subject.por.fl_str_mv |
COX-1 COX-2 PLA2 quantification Humiriaceae Endopleura uchi |
topic |
COX-1 COX-2 PLA2 quantification Humiriaceae Endopleura uchi |
description |
Endopleura uchi (Huber) Cuatrec. is an Amazon species traditionally used for the treatment of inflammations and female disorders. Pure bergenin was isolated from the methanolic extract of bark of E. uchi, firstly by using liquid-liquid partition chromatography followed by column chromatography over Sephadex LH-20 and then silica gel 60 flash chromatography. The structure of bergenin was identified on the basis of its NMR spectra. The in vitro anti-inflammatory activity was determined by the measurement of the inhibitory concentration (IC) of bergenin against three key enzymes: COX-1, COX-2 (cyclooxygenases) and phospholipase A2 (PLA2). These enzymes were selected because they are important targets for the discovery of new anti-inflammatory drugs associated with the biosynthesis of prostaglandins. The IC50 of bergenin for phopholipase A2 was determined as 156.6 µmol L-1 and bergenin was not considered active as compared to the positive control, tioetheramide PC. Bergenin did not inhibit COX-1 as well (IC50 = 107.2 µmol L-1). However, bergenin selectively inhibited COX-2 (IC50 = 1.2 µmol L-1). Because of the use of E. uchi in traditional medicine, bergenin was quantified in teas prepared as prescribed in traditional medicine by RP-HPLC as being 3% in the bark of E. uchi. The inhibitory activity towards COX-2 is important, since selective inhibitors of COX-2 have been clinically validated as anti-inflammatory therapeutics due to their enhanced gastrointestinal safety. |
publishDate |
2009 |
dc.date.none.fl_str_mv |
2009-01-01 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000600009 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000600009 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1590/S0103-50532009000600009 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
text/html |
dc.publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
dc.source.none.fl_str_mv |
Journal of the Brazilian Chemical Society v.20 n.6 2009 reponame:Journal of the Brazilian Chemical Society (Online) instname:Sociedade Brasileira de Química (SBQ) instacron:SBQ |
instname_str |
Sociedade Brasileira de Química (SBQ) |
instacron_str |
SBQ |
institution |
SBQ |
reponame_str |
Journal of the Brazilian Chemical Society (Online) |
collection |
Journal of the Brazilian Chemical Society (Online) |
repository.name.fl_str_mv |
Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ) |
repository.mail.fl_str_mv |
||office@jbcs.sbq.org.br |
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1750318169892847616 |