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PLoS One. 2014 Nov 25;9(11):e113834. doi: 10.1371/journal.pone.0113834. eCollection 2014.

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.

Author information

1
Department of Bioresource Sciences, Iwate Biotechnology Research Center, Kitakami, Iwate, Japan.
2
Graduate School of Agriculture, Iwate University, Morioka, Iwate, Japan.

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.

PMID:
25423092
PMCID:
PMC4244148
DOI:
10.1371/journal.pone.0113834
[Indexed for MEDLINE]
Free PMC Article

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