amentoflavone

**Amentoflavone** is a naturally occurring biflavonoid formed by the oxidative coupling of two apigenin molecules at positions C-3 (hydroxyphenyl ring) and C-8 (chromene ring)[2][5][8][7]. It is found in a variety of plants such as *Selaginella tamariscina*, *Ginkgo biloba*, *Hypericum perforatum* (St. John’s Wort), and others[4][7]. Amentoflavone exhibits **multifunctional biological activity**: it acts as an anti-inflammatory, antioxidant, antiviral, antidiabetic, neuroprotective, anticancer, anti-microbial, anti-senescence, and anti-fungal agent[1][7][13]. Mechanistically, it inhibits signaling pathways like ERK, NF-κB, PI3K/Akt, GLI-1/IL-6/STAT3, and enzymes such as cathepsin B, CYP3A4, CYP2C9, group II phospholipase A2, and cyclooxygenase[1][4][10][14][16]. It also antagonizes the κ-opioid receptor and is a negative allosteric modulator at the allosteric benzodiazepine site of the GABA_A receptor[4][16]. Recent research highlights its inhibition of SARS-CoV-2 via strong binding to 3CLpro (main protease), spike protein RBD, and RNA-dependent RNA polymerase, as well as its suppression of fatty acid synthase[1][6][13]. Pharmacokinetic studies suggest low oral bioavailability due to rapid metabolism[7]. While clinical development is ongoing for antiviral indications (notably COVID-19), most evidence is preclinical and pharmacological[6]. No brand products or commercial formulations with amentoflavone as a single agent are currently approved.

Other names

amenthoflavonetridemethylsciadopitysindidemethyl-ginkgetin3',8''-biapigenin1617-53-4