Drug intelligence / Profile preview

baicalein

Development stage
Phase 2
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Baicalein is a flavone, a type of flavonoid (5,6,7-trihydroxyflavone), originally isolated from the roots of *Scutellaria baicalensis* and *Scutellaria lateriflora*. It is also found in *Oroxylum indicum* and thyme. Baicalein acts as a neuroprotective agent and has demonstrated anticancer, antidiabetic, antimicrobial, antiaging, neuroprotective, cardioprotective, respiratory protective, gastroprotective, hepatic protective, and renal protective effects. Mechanistically: - Baicalein is a positive allosteric modulator at the benzodiazepine site of Gamma-aminobutyric acid receptor A (GABA A receptor) (with selectivity for α2/α3 subunits) but with much lower affinity than diazepam. - It inhibits certain lipoxygenases (notably 12-lipoxygenase), which are involved in inflammation and cancer progression. - It inhibits Cytochrome P450 2C9 enzyme activity. - Baicalein suppresses Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) signaling pathways leading to reduced expression of pro-inflammatory cytokines such as TNF-α and IL-6. Baicalein has been studied in clinical trials for influenza fever (Phase IIa) and Parkinson’s disease (Phase I). Preclinical studies suggest potential benefits in Alzheimer’s disease models by promoting nonamyloidogenic processing of amyloid precursor protein. Additional animal studies indicate efficacy against liver injury/fibrosis and food allergies[1][2][4][5][7].

Brand names
Baccoli
Other names
biacaleinnoroxylin
02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)CYP2C9 (Cytochrome P450 family 2 subfamily C member 9)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)

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