Native to Southeast Asia, the betel, also known as Piper betle, is a species of flowering plant in the Piperaceae family of pepper plants. This article provides a thorough exploration of the traditional and ethnomedical uses of the betel leaf (Piper betle) across various cultures, with a focus on its extensive therapeutic properties. The review encompasses the historical significance of betel leaf in Ayurvedic and Unani systems, detailing its diverse applications, ranging from anthelmintic to neuropharmacological effects. Furthermore, the article delves into the rich phytochemical composition of betel leaves, highlighting the presence of various compounds, such as phenols, alkaloids, flavonoids, and essential oils. The article dedicates a significant portion to elucidating the emerging research on betel leaf's potential in the realm of cancer treatment, showcasing its antitumour and anticancer properties. Additionally, the review explores betel leaf's efficacy in addressing various health issues, including its analgesic, anti-inflammatory, Antinociceptive, and neuropharmacological activities. The article also discusses the antioxidant, hepatoprotective, anti-ulcerogenic, Antihyperglycemic, antihyperlipidemic, anti-atherogenic, cardio protective, antifertility, and antimicrobial activities of betel leaves. Through a comprehensive examination of preclinical studies and scientific findings, this article aims to present a holistic understanding of the therapeutic potential of betel leaves, emphasizing its multifaceted contributions to traditional medicine and its promising role in contemporary healthcare.