Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity
Autor(a) principal: | |
---|---|
Data de Publicação: | 2016 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Revista Brasileira de Farmacognosia (Online) |
Texto Completo: | http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2016000100050 |
Resumo: | Abstract The ferulic and gallic acid related compounds from natural origin were studied against xanthine oxidase and cyclooxygenase-2 along with their anti-inflammatory activity. The compounds gallic acid, ferulic acid, caffeic acid and p-coumaric acid revealed promising anti-inflammatory activity (30–40% TNF-α and 60–75% IL-6 inhibitory activity at 10 µM). Bioavailability of compounds were checked by in vitro cytotoxicity using CCK-8 cell lines and confirmed to be nontoxic, but found toxic at higher concentration (50 µM). Gallic, ferulic, caffeic acid was demonstrated potential dual inhibition toward xanthine oxidase and cyclooxygenase-2 as calculated by IC50: 68, 70.2, and 65 µg/ml (xanthine oxidase) and 68.5, 65.2, and 62.5 µg/ml (cyclooxygenase-2), respectively. The structure activity relationship and in silico drug relevant properties (HBD, HBA, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study, which was expected for further rational drug design against xanthine oxidase and cyclooxygenase. |
id |
SBFGNOSIA-1_ba9678e83c4f7e8e679bca400ce005b5 |
---|---|
oai_identifier_str |
oai:scielo:S0102-695X2016000100050 |
network_acronym_str |
SBFGNOSIA-1 |
network_name_str |
Revista Brasileira de Farmacognosia (Online) |
repository_id_str |
|
spelling |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activityFerulic acidGallic acidXanthine oxidaseCyclooxygenaseSARGoutAbstract The ferulic and gallic acid related compounds from natural origin were studied against xanthine oxidase and cyclooxygenase-2 along with their anti-inflammatory activity. The compounds gallic acid, ferulic acid, caffeic acid and p-coumaric acid revealed promising anti-inflammatory activity (30–40% TNF-α and 60–75% IL-6 inhibitory activity at 10 µM). Bioavailability of compounds were checked by in vitro cytotoxicity using CCK-8 cell lines and confirmed to be nontoxic, but found toxic at higher concentration (50 µM). Gallic, ferulic, caffeic acid was demonstrated potential dual inhibition toward xanthine oxidase and cyclooxygenase-2 as calculated by IC50: 68, 70.2, and 65 µg/ml (xanthine oxidase) and 68.5, 65.2, and 62.5 µg/ml (cyclooxygenase-2), respectively. The structure activity relationship and in silico drug relevant properties (HBD, HBA, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study, which was expected for further rational drug design against xanthine oxidase and cyclooxygenase.Sociedade Brasileira de Farmacognosia2016-02-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2016000100050Revista Brasileira de Farmacognosia v.26 n.1 2016reponame:Revista Brasileira de Farmacognosia (Online)instname:Sociedade Brasileira de Farmacognosia (SBFgnosia)instacron:SBFGNOSIA10.1016/j.bjp.2015.08.013info:eu-repo/semantics/openAccessNile,Shivraj HariramKo,Eun YoungKim,Doo HwanKeum,Young-Sooeng2016-02-03T00:00:00Zoai:scielo:S0102-695X2016000100050Revistahttp://www.sbfgnosia.org.br/revista/https://old.scielo.br/oai/scielo-oai.phprbgnosia@ltf.ufpb.br1981-528X0102-695Xopendoar:2016-02-03T00:00Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia)false |
dc.title.none.fl_str_mv |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
title |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
spellingShingle |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity Nile,Shivraj Hariram Ferulic acid Gallic acid Xanthine oxidase Cyclooxygenase SAR Gout |
title_short |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
title_full |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
title_fullStr |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
title_full_unstemmed |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
title_sort |
Screening of ferulic acid related compounds as inhibitors of xanthine oxidase and cyclooxygenase-2 with anti-inflammatory activity |
author |
Nile,Shivraj Hariram |
author_facet |
Nile,Shivraj Hariram Ko,Eun Young Kim,Doo Hwan Keum,Young-Soo |
author_role |
author |
author2 |
Ko,Eun Young Kim,Doo Hwan Keum,Young-Soo |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Nile,Shivraj Hariram Ko,Eun Young Kim,Doo Hwan Keum,Young-Soo |
dc.subject.por.fl_str_mv |
Ferulic acid Gallic acid Xanthine oxidase Cyclooxygenase SAR Gout |
topic |
Ferulic acid Gallic acid Xanthine oxidase Cyclooxygenase SAR Gout |
description |
Abstract The ferulic and gallic acid related compounds from natural origin were studied against xanthine oxidase and cyclooxygenase-2 along with their anti-inflammatory activity. The compounds gallic acid, ferulic acid, caffeic acid and p-coumaric acid revealed promising anti-inflammatory activity (30–40% TNF-α and 60–75% IL-6 inhibitory activity at 10 µM). Bioavailability of compounds were checked by in vitro cytotoxicity using CCK-8 cell lines and confirmed to be nontoxic, but found toxic at higher concentration (50 µM). Gallic, ferulic, caffeic acid was demonstrated potential dual inhibition toward xanthine oxidase and cyclooxygenase-2 as calculated by IC50: 68, 70.2, and 65 µg/ml (xanthine oxidase) and 68.5, 65.2, and 62.5 µg/ml (cyclooxygenase-2), respectively. The structure activity relationship and in silico drug relevant properties (HBD, HBA, PSA, c Log P, ionization potential, molecular weight, EHOMO and ELUMO) further confirmed that the compounds were potential candidates for future drug discovery study, which was expected for further rational drug design against xanthine oxidase and cyclooxygenase. |
publishDate |
2016 |
dc.date.none.fl_str_mv |
2016-02-01 |
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=S0102-695X2016000100050 |
url |
http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0102-695X2016000100050 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
10.1016/j.bjp.2015.08.013 |
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 Farmacognosia |
publisher.none.fl_str_mv |
Sociedade Brasileira de Farmacognosia |
dc.source.none.fl_str_mv |
Revista Brasileira de Farmacognosia v.26 n.1 2016 reponame:Revista Brasileira de Farmacognosia (Online) instname:Sociedade Brasileira de Farmacognosia (SBFgnosia) instacron:SBFGNOSIA |
instname_str |
Sociedade Brasileira de Farmacognosia (SBFgnosia) |
instacron_str |
SBFGNOSIA |
institution |
SBFGNOSIA |
reponame_str |
Revista Brasileira de Farmacognosia (Online) |
collection |
Revista Brasileira de Farmacognosia (Online) |
repository.name.fl_str_mv |
Revista Brasileira de Farmacognosia (Online) - Sociedade Brasileira de Farmacognosia (SBFgnosia) |
repository.mail.fl_str_mv |
rbgnosia@ltf.ufpb.br |
_version_ |
1752122469677793280 |