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BioAssay: AID 499575

Agonist activity at RXRalpha in HEK293 cells assessed as transcriptional activation after 48 hrs by luciferase reporter gene assay

Screening of a total of 86 crude drugs for retinoid X receptor (RXR) ligands demonstrated that the methanol extract of the bark of Magnolia obovata markedly activated the transcriptional activity of RXRalpha in luciferase reporter assays. Thereafter, honokiol (1) was isolated as a constituent able to activate RXR selectively as a natural rexinoid, but not RARalpha. The activity of 1 was more more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 499575
Data Source: ChEMBL (649615)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-02-25
Modify Date: 2014-05-26

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Retinoic acid receptor RXR-alpha; AltName: Full=Nuclear receptor subfamily 2 group B member 1; AltName: Full=Retinoid X receptor alpha
Description ..   
Protein Family: The ligand binding domain of the retinoid X receptor and Ultraspiracle, members of nuclear receptor superfamily
Comment ..   

Gene:RXRA     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Identification of a naturally occurring rexinoid, honokiol, that activates the retinoid X receptor.

Abstract: Screening of a total of 86 crude drugs for retinoid X receptor (RXR) ligands demonstrated that the methanol extract of the bark of Magnolia obovata markedly activated the transcriptional activity of RXRalpha in luciferase reporter assays. Thereafter, honokiol (1) was isolated as a constituent able to activate RXR selectively as a natural rexinoid, but not RARalpha. The activity of 1 was more potent than those of phytanic acid and docosahexaenoic acid, both of which are known to be natural RXR agonists. Honokiol (1) is capable of activating a RXR/LXR heterodimer, resulting in the induction of ATP-binding cassette transporter A1 mRNA and protein expression in RAW264.7 cells, as well as an increase in [(3)H]cholesterol efflux from peritoneal macrophages. These effects of 1 were enhanced synergistically in the presence of an LXR agonist, 22(R)-hydroxycholesterol. The results obtained demonstrate that 1, a newly identified natural rexinoid, regulates the functions of RXR/LXR heterodimer and abrogates foam cell formation by the induction of ABCA1 via activation of the RXR/LXR heterodimer.
(PMID: 20695472)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Functional

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: HEK293

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloatμM
6EC50 standard valueEC50 standard valueFloatnM
7EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

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