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BioAssay: AID 699018

Transactivation of PPARalpha expressed in human HepG2 cells assessed as Sult2a1 expression at 100 nM by luciferase reporter gene assay relative to vehicle-treated control

Tithonia diversifolia is a well-known traditional Chinese medicine treating diabetes, hepatitis, and hepatocarcinoma but its molecular mechanism is not fully understood. Peroxisome proliferator-activated receptors (PPARs) alpha and gamma are members of nuclear receptor superfamily. Their agonists are prescribed as antihyperlipidemic and antihyperglycemic drugs now. In this study, sesquiterpene more ..
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Unspecified(2)
 
 
 Related BioAssays
 Related BioAssays
AID: 699018
Data Source: ChEMBL (859762)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-05-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor alpha; Short=PPAR-alpha; AltName: Full=Nuclear receptor subfamily 1 group C member 1
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARA     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.

Abstract: Tithonia diversifolia is a well-known traditional Chinese medicine treating diabetes, hepatitis, and hepatocarcinoma but its molecular mechanism is not fully understood. Peroxisome proliferator-activated receptors (PPARs) alpha and gamma are members of nuclear receptor superfamily. Their agonists are prescribed as antihyperlipidemic and antihyperglycemic drugs now. In this study, sesquiterpene lactones, tirotundin and tagitinin A, were isolated from T. diversifolia and evaluated for their activity against PPARs by the transient transfection reporter assay. Tirotundin and tagitinin A transactivated PPARgamma dependent promoters including PPRE (PPARgamma response element), SHP, and ABCA1 gene promoters in dose-dependent manner. Furthermore, the fluorescence polarization competitive binding assay showed that tirotundin (IC(50)=27 muM) and tagitinin A (IC(50)=55 muM) enhanced PPARgamma transactivation activity by directly binding to PPARgamma ligand binding domain. Additionally, they stimulated the transactivation of PPARalpha dependent SULT2A1 gene promoter by 2.3-fold of vehicle effect at 10 muM. These results highly indicated that tirotundin and tagitinin A are the active components of T. diversifolia to exert anti-diabetic effect through PPARgamma pathway. Moreover, these sesquiterpene lactones behaved as PPARalpha/gamma dual agonists so they might be useful as the potential herbal treatment for diabetes.
(PMID: 22424975)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: HepG2

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1RLU activity commentRLU activity commentString
2RLU standard flagRLU standard flagInteger
3RLU qualifierRLU qualifierString
4RLU published valueRLU published valueFloat
5RLU standard valueRLU standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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