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Betel leaf (Piper betle Linn.) is a plant that holds cultural significance and is noted for its medicinal uses across Asia, where it serves various religious, social, and therapeutic functions. The plant contains a range of phytochemicals such as chavibetol, safrole, allylpyrocatechol, and eugenol, which contribute to its diverse pharmacological effects, including antimicrobial, antioxidant, antidiabetic, anticancer, antifungal, and gastroprotective properties. In traditional Ayurveda, betel leaf has been used to manage ailments such as headaches, constipation, respiratory problems, inflammation, and wound healing. The economic significance of the plant is evident in its roles within pharmaceuticals, cosmetics, nutraceuticals, and cultural practices. However, prolonged use, particularly in combinations like betel quid with tobacco and areca nut, can result in toxicity and negative health outcomes. This review covers the botanical characteristics, phytochemistry, cultivation, pharmacological effects, traditional applications, and economic importance of betel leaf, offering a thorough overview of its potential therapeutic benefits and limitations.