In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-## 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-##; however, ursolic acid enhances the binding of PPAR-## to the peroxisome more ..
Tested Compound:
Description:
Title: Ursolic acid is a PPAR-## agonist that regulates hepatic lipid metabolism.
Abstract: In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-## 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-##; however, ursolic acid enhances the binding of PPAR-## to the peroxisome proliferator response element in PPAR-##-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-## agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-##.
(PMID: 21855333)
Abstract: In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-## 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-##; however, ursolic acid enhances the binding of PPAR-## to the peroxisome proliferator response element in PPAR-##-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-## agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-##.
(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
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
ChEMBL Assay Type: Functional
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Activity activity comment | Activity activity comment | String | |||
| 2 | Activity standard flag | Activity standard flag |  | Integer | ||
| 3 | Activity qualifier | Activity qualifier | String | |||
| 4 | Activity published value | Activity published value | | Float | ||
| 5 | Activity standard value | Activity standard value | | Float |
Data Table (Concise)
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