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BioAssay: AID 620705

Induction of BODIPY-labeled 4,4-difluoro-5-methyl-4-bora-3a,4a-diaza-s-indacene-3-dodecanoic acid uptake in human HepG2 cells after 1 min by FACS analysis

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: 620705
Data Source: ChEMBL (770716)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-05-26

Data Table ( Complete ):           All
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
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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