Butein

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CAS: 487-52-5

Name:

Butein

Other names:

2',3,4,4'-Tetrahydroxychalcone; 2',4',3,4-Tetrahydroxychalcone; 3,4,2',4'-Tetrahydroxychalcone

Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor. Butein potently inhibits the tyrosine kinase activity of the EGF receptor (IC50 = 65 μM) and p60c-src (IC50 = 65 μM). The inhibition is competitive with respect to ATP and non-competitive with respect to the substrate. Butein is also a potent antioxidant and antiinflammatory agent which has been shown to inhibit glutathione reductase and rat liver GST (glutathione-S-transferase (IC50 = 9 μM)). Butein has been reported to activate sirtuins and promote the survival of eukaryotic cells. The Sirtuins, SIRT1-4 and SIRT7 are deacetylases relevant to histone modification. Butein directly inhibits IKK and suggested to also display inhibition towards PDE (c-AMP dependent PDE-IV). Also a potential CYP19 (Aromatase) inhibitor.

Interactions

Description

UniProt ID

Protein: Alcohol dehydrogenase [NADP(+)], Gene: AKR1A1
Protein: Arachidonate 5-lipoxygenase, Gene: ALOX5
Protein: Proto-oncogene tyrosine-protein kinase Src, Gene: SRC
Protein: C-type lectin domain family 14 member A, Gene: CLEC14A
Protein: Inhibitor of nuclear factor kappa-B kinase subunit beta, Gene: IKBKB

Toxicity

oral LD50 [mouse] mg/kg
Unavailable
oral LD50 [rat] mg/kg
Unavailable
oral LD50 [rabbit] mg/kg
Unavailable

Effects on organism

Anti Inflammation
Anti Cancer
Cardioprotective
Antibacterial

No

Antifungal

No

Antiviral

No

Longevity mechanisms activation

Stress Resistance

Suppression of aging mechanisms

Anti Oxidant

Relation to biomarkers of Aging

Aldose reductase and advanced glycation endproducts inhibitory effects

18670102

Relation to aging associated genes

SHC1IKBKB

Experimental conditions

Not available

Life Extension

Mean LS (%)
Median LS (%)
Mortality rate derease (%)
Max LS (%)
Cell CLS
Cell RLS
31.0

Concentration wth maximum effect

10 mkM

More info about experiment

12939617
Opposite effectNo