Piper betle L., belonging to Piperaceae family, referred to as a standard herbal medicinal plant and used for several health benefits in Asian countries. Currently, demand for its products like herbal drugs, medicines, and natural herbal formulations have increased. The beneficial effects of betel leaves and its products have traditionally exploited for the treatment of several diseases like bad breath, cuts, injuries, inflammations, cold cough, indigestion, etc. Till now, a broad range of bioactive compounds including polyphenols, terpenes, etc., has been identified from the extracts and volatile oil (EO) of betel leaves. Most of the health-related benefits of betel leaves are related to their bioactive phenolic compounds. The extract of this highly perishable product are often utilized in organic synthesis, food, and beverage industry, pharmaceuticals, etc., to the environmental issues. The present review provides information on pharmacognostic aspects, bioactive compounds, and their biological activities of Piper betle L.