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Amentoflavone is a biflavonoid compound with several notable characteristics and roles. Here's an overview of its properties and functions:

Chemical Structure: Amentoflavone is classified as a biflavonoid, which means it is formed by the oxidative coupling of two molecules of apigenin. This coupling results in a specific bond formation between positions C-3 of the hydroxyphenyl ring and C-8 of the chromene ring. This unique structure sets it apart from other flavonoid compounds.

Natural Occurrence: Amentoflavone is found in several plant species, including Ginkgo biloba, Chamaecyparis obtusa (hinoki), Biophytum sensitivum, Selaginella tamariscina, Hypericum perforatum (St. John's Wort), and Xerophyta plicata. It is considered a natural product and is extracted from these plants for various purposes.

Biological Activities:

Cathepsin B Inhibitor: Amentoflavone has been identified as an inhibitor of human cathepsin B, an enzyme involved in cellular processes and protein degradation.

Antiviral Agent: It possesses antiviral properties and may have potential applications in inhibiting viral infections.

Angiogenesis Inhibitor: Amentoflavone is known for its ability to inhibit angiogenesis, the formation of new blood vessels from existing ones. This property may be relevant in cancer research and treatment.

P450 Inhibitor: It acts as an inhibitor of cytochrome P450 enzymes, specifically CYP3A4 and CYP2C9. These enzymes are responsible for metabolizing various drugs in the body. Inhibition of these enzymes can affect the metabolism of drugs and their efficacy.

Pharmacological Activities:

Antimalarial Activity: Amentoflavone exhibits antimalarial activity, indicating its potential use in combating malaria.

Anticancer Activity: It has shown anticancer properties, which may be attributed, at least in part, to its inhibition of fatty acid synthase. This activity suggests its potential as a cancer treatment or adjunct therapy.

Opioid Receptor Activity: Amentoflavone acts as an antagonist at the κ-opioid receptor.

GABAA Receptor Activity: It interacts with the allosteric benzodiazepine site of the GABAA receptor as a negative allosteric modulator.

Due to its diverse pharmacological activities, amentoflavone is a subject of interest in various fields of research, including pharmacology, oncology, and virology. Its interactions with drug-metabolizing enzymes make it important in drug development and pharmacokinetics.

Chemical and Physical Properties

Source: PubChem