Evidence map›Paper›PMID 24329519›Full record

ArticleBritish journal of pharmacology2014

Identification of plumericin as a potent new inhibitor of the NF-κB pathway with anti-inflammatory activity in vitro and in vivo.

N Fakhrudin, B Waltenberger, M Cabaravdic, A G Atanasov, C Malainer, D Schachner, E H Heiss, R Liu, S M Noha, A M Grzywacz and 8 more

Open access · hybridAbstract read
In one paragraph

Article in British journal of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.

0numbers the graph read from it
0cells of the map it votes in
36citing papers in PubMed
2.2field-weighted citation impact, top 13% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

36 citing papers in PubMed, 67 citations in OpenAlex.

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  17. UNaProd: A Universal Natural Product Database forEvidence-based complementary and alternative medicine : eCAM · 2020
    Article
  18. Article
  19. C13 Megastigmane Derivatives FromFrontiers in pharmacology · 2019
    Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

18 authors at 4 institutions in 2 countries.

N FakhrudinDepartment of Pharmacognosy, University of Vienna, Vienna, Austria; Department of Pharmaceutical Biology, Faculty of Pharmacy, Universitas Gadjah Mada, Yogyakarta, Indonesia.
B Waltenberger
M Cabaravdic
A G Atanasov
C Malainer
D Schachner
E H Heiss
R Liu
S M Noha
A M Grzywacz
J Mihaly-Bison
E M Awad
D Schuster
J M Breuss
J M Rollinger
V Bochkov
H Stuppner
V M Dirsch
University of Vienna · ATMedical University of Vienna · ATUniversität Innsbruck · ATUniversitas Gadjah Mada · ID

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

background and purposeThe transcription factor NF-κB orchestrates many pro-inflammatory signals and its inhibition is considered a promising strategy to combat inflammation. Here we report the characterization of the natural product plumericin as a highly potent inhibitor of the NF-κB pathway with a novel chemical scaffold, which was isolated via a bioactivity-guided approach, from extracts of Himatanthus sucuuba, an Amazonian plant traditionally used to treat inflammation-related disorders. EXPERIMENTAL APPROACH: A NF-κB luciferase reporter gene assay was used to identify NF-κB pathway inhibitors from H. sucuuba extracts. Monitoring of TNF-α-induced expression of the adhesion molecules VCAM-1, ICAM-1 and E-selectin by flow cytometry was used to confirm NF-κB inhibition in endothelial cells, and thioglycollate-induced peritonitis in mice to confirm effects in vivo. Western blotting and transfection experiments were used to investigate the mechanism of action of plumericin. KEY

resultsPlumericin inhibited NF-κB-mediated transactivation of a luciferase reporter gene (IC50 1 μM), abolished TNF-α-induced expression of the adhesion molecules VCAM-1, ICAM-1 and E-selectin in endothelial cells and suppressed thioglycollate-induced peritonitis in mice. Plumericin exerted its NF-κB pathway inhibitory effect by blocking IκB phosphorylation and degradation. Plumericin also inhibited NF-κB activation induced by transfection with the constitutively active catalytic subunit of the IκB kinase (IKK-β), suggesting IKK involvement in the inhibitory action of this natural product. CONCLUSION AND IMPLICATIONS: Plumericin is a potent inhibitor of NF-κB pathways with a new chemical scaffold. It could be further explored as a novel anti-inflammatory lead compound.

Indexed as

AnimalsAnti-Inflammatory AgentsApocynaceaeCell Adhesion MoleculesDisease Models, AnimalDose-Response Relationship, DrugHEK293 CellsHumansHuman Umbilical Vein Endothelial CellsI-kappa B KinaseI-kappa B ProteinsIndenesInflammationInflammation MediatorsIridoidsMaleAnti-Inflammatory AgentsCell Adhesion MoleculesI-kappa B KinaseI-kappa B ProteinsIndenesInflammation MediatorsIridoidsNF-kappa BPlant ExtractsplumericinThioglycolatesadhesion moleculesIKK-βinflammationIκBnatural productsNF-κBperitonitisplumericin

Identifiers

PMID24329519
PMCPMC3966748
OpenAlexW1593082823

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.