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BioAssay: AID 1070428

Activation of Nrf2 in human VSMC assessed as induction of HO-1 expression at 3 uM after 18 hrs by immunoblotting analysis

Activation of nuclear factor-erythroid 2-related factor 2 (Nrf2) contributes to several beneficial bioactivities of natural products, including induction of an increased cellular stress resistance and prevention or resolution of inflammation. In this study, the potential of a crude leaf extract of Chromolaena odorata, traditionally used against inflammation and skin lesions, was examined for Nrf2 more ..
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AID: 1070428
Data Source: ChEMBL (1292044)
Depositor Category: Literature, Extracted
Deposit Date: 2014-08-22
Target
Sequence: RecName: Full=Nuclear factor erythroid 2-related factor 2; Short=NF-E2-related factor 2; Short=NFE2-related factor 2; AltName: Full=HEBP1; AltName: Full=Nuclear factor, erythroid derived 2, like 2
Description ..   
Protein Family: basic leucine zipper DNA-binding and multimerization region of GCN4 and related proteins
Comment ..   

Gene:NFE2L2     Related Protein 3D Structures     More BioActivity Data..
Description:
Title: Identification of chromomoric acid C-I as an Nrf2 activator in Chromolaena odorata.

Abstract: Activation of nuclear factor-erythroid 2-related factor 2 (Nrf2) contributes to several beneficial bioactivities of natural products, including induction of an increased cellular stress resistance and prevention or resolution of inflammation. In this study, the potential of a crude leaf extract of Chromolaena odorata, traditionally used against inflammation and skin lesions, was examined for Nrf2 activation. Guided by an Nrf2-dependent luciferase reporter gene assay, the phytoprostane chromomoric acid C-I (1) was identified as a potent Nrf2 activator from C. odorata with a CD (concentration doubling the response of vehicle-treated cells) of 5.2 muM. When tested at 1-10 muM, 1 was able to induce the endogenous Nrf2 target gene heme oxygenase 1 (HO-1) in fibroblasts. Between 2 and 5 muM, compound 1 induced HO-1 in vascular smooth muscle cells (VSMC) and inhibited their proliferation in a HO-1-dependent manner, without eliciting signs of cytotoxicity.
(PMID: 24476568)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
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

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