Drug intelligence / Profile preview

acacetin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

Acacetin is a naturally occurring O-methylated flavone (flavonoid) found in several vascular plants, including *Robinia pseudoacacia* and *Agastache rugosa*. It exhibits diverse pharmacological activities, such as spasmolytic, anti-nociceptive, antioxidant, anti-inflammatory, anti-cancer, anti-plasmodial, antiarrhythmic, and neuroprotective effects. - **Mechanism of Action:** - Acacetin acts as an inhibitor of several enzymes and signaling pathways, including PI3K (phosphoinositide 3-kinase), RARγ (retinoic acid receptor-γ), BACE-1 (β-amyloid cleaving enzyme), and both monoamine oxidase isoforms (MAO-A and MAO-B), with a preference for MAO-B. - It modulates apoptotic pathways via caspase activation, influences cell cycle progression, inhibits ROS production, and affects MAPK, AKT, and Nrf2 signaling. - In the context of antibacterial activity, acacetin inhibits virulence factors such as listeriolysin O, suilysin, and pneumolysin, and also sortase A in bacteria. - Additional effects involve the suppression of inflammatory cytokines TNF-α, IL-6, and IL-1β via the Nrf2, AMPK, PI3K/AKT/IKK, and MAPK pathways. - In cardiovascular research, acacetin has demonstrated antiarrhythmic properties, particularly against atrial fibrillation. - **Indications:** Historically studied for chronic lymphocytic leukemia, hepatocellular carcinoma, oral squamous cell carcinoma, Alzheimer’s disease, neurodegenerative and inflammatory conditions, and arrhythmias[1][2][3][5][6].

Other names
5,7-dihydroxy-4'-methoxyflavone4'-methoxy-5,7-dihydroxyflavone5,7-dihydroxy-2-(4-methoxyphenyl)-4H-chromen-4-oneabieticacacetinelinarigeninlinariseninapigenin 4'-methyl etherapisenin 4'-methyl etherbuddleoflavonol
02

Targets

NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)PIK3CA (Phosphoinositide 3-kinase alpha)RARG (Retinoic acid receptor gamma)STAT3 (Signal Transducer and Activator of Transcription 3)BACE1 (Beta-site APP-cleaving enzyme 1)LLO (Listeriolysin O)MAOA (Monoamine oxidase A)MAOB (Monoamine oxidase B)Ply (Pneumolysin)SrtA (Sortase A)SLY (Suilysin)

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