Drug intelligence / Profile preview

butein

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal (preclinical), Oral (supplement)
01

Overview

**Butein** is a natural plant polyphenol classified as a chalcone (a type of flavonoid) found in several plant sources including Toxicodendron vernicifluum, Dalbergia odorifera, Cyclopia subternata, and Butea monosperma[1][4][5][7][8]. It exhibits diverse pharmacological properties including **anti-inflammatory**, **anti-cancer**, **anti-oxidant**, **anti-angiogenic**, and **aldose reductase inhibition** effects[1][2][5][6][7][9]. Butein acts primarily as a **protein tyrosine kinase inhibitor**, particularly inhibiting kinases such as EGF receptor and c-Src, modulating signal transduction and cell proliferation[1][4][7]. It also inhibits NF-κB transcription factor activity, resulting in downstream suppression of inflammatory cytokines (e.g., TNF-α, IL-6, IL-8)[1][6]. Mechanistically, butein suppresses cancer cell proliferation, induces cell cycle arrest (in part via the FOXO3a/p27kip1 pathway)[3], inhibits aromatase activity (making it of interest for breast cancer)[5], modulates RANKL pathway (relevant to bone loss)[9], and activates sirtuins[5]. Butein is used experimentally in preclinical models for cancer, inflammation, neurological disorders, atherosclerosis, and infectious diseases but is not approved as a pharmaceutical for human use[1][7].

Other names
2',3,4,4'-tetrahydroxychalcone(E)-1-(2,4-dihydroxyphenyl)-3-(3,4-dihydroxyphenyl)prop-2-en-1-one2’,3,4,4’-tetrahydroxy Chalcone3,4,2',4'-Tetrahydroxychalcone(2E)-1-(2,4-dihydroxyphenyl)-3-(3,4-dihydroxyphenyl)prop-2-en-1-onebutrinisobutrinbutein(P)CCG208298CCG-208298CCG 208298NMPC-696NMPC696NMPC 696
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)STAT3 (Signal Transducer and Activator of Transcription 3)TWEAK–FN14 (Tumor necrosis factor-like weak inducer of apoptosis–Fibroblast growth factor-inducible 14 complex)SRC (Proto-oncogene tyrosine-protein kinase Src)AR (Adrenergic receptors)CYP19A1 (Aromatase)FOXO3 (Forkhead box protein O3)RELA (Nuclear Factor Kappa B Subunit p65)PTK (Protein-Tyrosine Kinase)SIRT (Sirtuin family)

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