Human dependence on plants as a source of medicine dates back to prehistoric times. Even now, more than three-fourths of the world’s population relies mainly on plants and plant extracts for healthcare. Several prescription drugs in the developed countries contain plant components and more than 120 important prescription drugs are derived from plants. Recent years have witnessed a resurgence of interest in plants as a source of medicine, especially those of antiquity and ethno-medicine. Betel vine (Piper betle L.; PB), a shadeloving, perennial evergreen climber of tropical origin, generally known as ‘paan’ in the Indian subcontinent and by different names in the Asiatic region is a plant of antiquity. According to estimates, it is consumed daily by nearly 600 million people and the custom of betel chewing encompasses a vast area of the world, extending 11,000 km west to east and 6000 km north to south, an area stretching from east Africa to Polynesia. Piper betle is a plant with known ethnomedicinal properties and its use in India, Indonesia and other countries of the Indo-China region – Malaysia, Vietnam, Laos, Kampuchea, Thailand, Myanmar, Singapore and the Far East is well known. Use of PB leaf (PBL) was known for centuries for its curative properties such as: to reduce/prevent body odour and bad breath, throat and lung problems, cough prevention and healing, to reduce unwanted vaginal secretion and bad odour and to prevent itching caused by fungus and internal/external bacteria. In Chinese folk medicine betel leaves are used for the treatment of various disorders and claimed to have detoxication, antioxidation and antimutation properties. It may be mentioned that the traditional health systems recognized the value of PB and discovered many uses. Several tribes in India still use it as cure and protection from different ailments and several of the claimed PB uses have been validated over a period of time. Some of the work done earlier did show the useful effects of PB, including a sense of well-being. PB use involves chewing, ingestion and topical applications.