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BioAssay: AID 620704

Hypolipidemic activity in human HepG2 cells assessed as decrease in cholesterol level at 80 uM by fluorescence-based method relative to control

In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-alpha in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-alpha; however, ursolic acid enhances the binding of PPAR-alpha to the peroxisome more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 620704
Data Source: ChEMBL (770715)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-26

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Tested Compound:
Description:
Title: Ursolic acid is a PPAR-alpha agonist that regulates hepatic lipid metabolism.

Abstract: In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-alpha in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-alpha; however, ursolic acid enhances the binding of PPAR-alpha to the peroxisome proliferator response element in PPAR-alpha-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-alpha agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-alpha.
(PMID: 21855333)
Comment
Putative Target:
ChEMBL Target ID: 81020
Target Type: CELL-LINE
Cell Line: HepG2
Tissue: Hepatoblastoma cells
Pref Name: HepG2
Organism: Homo sapiens
Tax ID: 9606
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: HepG2
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
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