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BioAssay: AID 517389

Inhibition of AMPK-mediated adipocyte differentiation in mouse 3T3L1 cells

Among nine flavonols (1-9) obtained from Sophorae Flos, we first isolated compounds 4, 5, 8, and 9. These isolates (1-9) were evaluated for the phosphorylation of AMPK and ACC. Administered at 10 muM, 9 possessed high potent activity. Compound 9 displayed a dose-dependent stimulation of glucose uptake in 3T3-L1 cells, and this increase was obviously attenuated by compound C, an AMPK inhibitor. In more ..
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 Tested Compounds
 Tested Compounds
All(9)
 
 
Active(9)
 
 
 Tested Substances
 Tested Substances
All(9)
 
 
Active(9)
 
 
 Related BioAssays
 Related BioAssays
AID: 517389
Data Source: ChEMBL (665257)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2013-11-17

Data Table ( Complete ):           Active    All
BioActive Compounds: 9
Description:
Title: The selected flavonol glycoside derived from Sophorae Flos improves glucose uptake and inhibits adipocyte differentiation via activation AMPK in 3T3-L1 cells.

Abstract: Among nine flavonols (1-9) obtained from Sophorae Flos, we first isolated compounds 4, 5, 8, and 9. These isolates (1-9) were evaluated for the phosphorylation of AMPK and ACC. Administered at 10 muM, 9 possessed high potent activity. Compound 9 displayed a dose-dependent stimulation of glucose uptake in 3T3-L1 cells, and this increase was obviously attenuated by compound C, an AMPK inhibitor. In addition, 9 also phosphorylated AMPK and its downstream substrate ACC in 3T3-L1 cells in a time- and dose-dependent manner. Moreover, we discovered that compound C inhibits 9-stimulated ACC phosphorylation and motivated the 9-inhibited C/EBPalpha and PPARgamma, and FAS gene expression, significantly. These results revealed the role of the AMPK downstream signaling pathway in 9-improved glucose metabolism in 3T3-L1 cells and 9-inhibited adipocyte differentiation. Differentiation was investigated by Oil Red O staining activity after 9 administration (0-20 muM) in 6 days. Compound 9 decreased mean droplet size in a dose-dependent manner. The results revealed that 9 blocked adipogenic conversion in 3T3-L1 cells together with several significant downregulating adipocyte-specific transcription factors, including PPARgamma, C/EBPalpha, and SREBP1. It also reduced FAS gene expression in a dose-dependent manner, which is crucial for adipogenesis in vitro.
(PMID: 20822902)
Comment
Putative Target:

ChEMBL Target ID: 103565
Target Type: SINGLE PROTEIN
Pref Name: 5'-AMP-activated protein kinase catalytic subunit alpha-2
Synonyms: 5'-AMP-activated protein kinase catalytic subunit alpha-2;ACACA kinase;Acetyl-CoA carboxylase kinase;AMPK subunit alpha-2;HMGCR kinase;Hydroxymethylglutaryl-CoA reductase kinase;
Gene Name: Prkaa2;
Protein Accession: Q8BRK8;
Protein GI: 341940616;
Organism: Mus musculus
Tax ID: 10090
Target Classification: enzyme
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

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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