Amentoflavone is a biflavonoid that is obtained by oxidative coupling of two molecules of apigenin resulting in a bond between positions C-3 of the hydroxyphenyl ring and C-8 of the chromene ring. A natural product found particularly in Ginkgo biloba and Hypericum perforatum. It has a role as an antiviral agent, an angiogenesis inhibitor, a P450 inhibitor, a cathepsin B inhibitor and a plant metabolite. It is a hydroxyflavone, a ring assembly and a biflavonoid. Amentoflavone is a novel natural inhibitor of human Cathepsin B(CatB), which has antifungal , antioxidant, antiviral, antidiabetic, and neuroprotective activities, it stimulates apoptosis in HSFBs and inhibits angiogenesis of endothelial cells, it is a promising molecule that can be used in hypertrophic scar treatment. Amentoflavone regulated β-catenin and caspase-3 expressions, and inhibited NF-κB signal transduction pathways. Amentoflavone (Didemeethyl ginkgetin) is an effective and orally active GABA (A) negative regulator. Amentoflavone also exhibits anti-inflammatory, antioxidant, antiviral, anti-tumor, anti radiation, and antibacterial activities. Amentoflavone induces cell apoptosis and cell cycle arrest in the sub-G1 phase.