RRC ID 32576
Author Yamada H, Kikuchi S, Inui T, Takahashi H, Kimura K.
Title Gentiolactone, a secoiridoid dilactone from Gentiana triflora, inhibits TNF-α, iNOS and Cox-2 mRNA expression and blocks NF-κB promoter activity in murine macrophages.
Journal PLoS One
Abstract BACKGROUND:Gentian roots have been used as a herbal medicine because of their anti-inflammatory activities. However, the molecular mechanisms of these anti-inflammatory effects remain to be completely explained.
METHODS AND FINDINGS:Here, we investigated anti-inflammatory effects of gentian roots and showed that root extracts from Gentiana triflora inhibited lipopolysaccharide (LPS)-induced expression of TNF-α in RAW264.7 cells. The extracts also contained swertiamarin and gentiopicroside, which are the major active compounds of gentian roots; however, neither compound had any effect on LPS-induced TNF-α production in our test system. We isolated gentiolactone as an inhibitor of TNF-α production from the extracts. Gentiolactone also inhibited LPS-induced inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (Cox-2) expression at the mRNA level. Moreover, gentiolactone suppressed NF-κB transcriptional activity without inhibition of IκB degradation or NF-κB nuclear transport.
CONCLUSIONS:Our results indicate that inhibition of TNF-α, iNOS and Cox-2 expression by gentiolactone is one of the mechanisms of the anti-inflammatory properties of gentian roots.
Volume 9(11)
Pages e113834
Published 2014-1-1
DOI 10.1371/journal.pone.0113834
PII PONE-D-14-21637
PMID 25423092
PMC PMC4244148
MeSH Animals Cyclooxygenase 2 / genetics* Gentiana / chemistry* Iridoids / pharmacology* Macrophages / drug effects* Macrophages / metabolism Mice NF-kappa B / genetics* Nitric Oxide Synthase Type II / genetics* Promoter Regions, Genetic* RNA, Messenger / genetics* Tumor Necrosis Factor-alpha / genetics*
IF 2.74
Times Cited 11
DNA material pNF-kappaB RE-TK hRluc(F) (RDB05576)