Plant extracts, composed of bioactive non-nutrient phytochemicals, have historically stood out as a primary reservoir for the development of new leads in anticancer drug research. Piper betel (L.), a widely cultivated plant in Asia, particularly renowned for its medicinal properties, has been traditionally employed in treating various health ailments. Piper betel L., commonly known as Pan and belonging to the Piperaceae family, flourishes in regions like Sri Lanka, India, Thailand, Taiwan, and other Southeast Asian countries. Remarkably, P. betel leaves have shown significant effectiveness against various bacteria, including Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Candida albicans. The oil extracted from betel leaves holds potential as a raw material in the production of medicines, perfumes, mouth fresheners, tonics, and food additives. Rich in nutrients and possessing anti-carcinogenic properties, betel leaves present a promising avenue for the development of drugs targeting blood cancer. This comprehensive review serves as a scientific compendium for researchers and manufacturers engaged in the development of products derived from betel leaves. Widely dubbed as “Green Gold,” betel leaves serve various purposes including stimulation, antiseptic action, and breath freshening. Their diverse properties encompass anti-fungal, anti-bacterial, anti-inflammatory, antimicrobial, antioxidant, antimutagenic, anti-haemolytic, anti-diabetic, and anti-ulcer effects. This review not only furnishes fundamental insights into the manifold effects of betel leaves but also delineates the phytochemical compounds found in their extracts and essential oils, safety profiles, and value-added products.