Since antiquity, Piper betel. Linn, commonly known as betel vine, has been used as a religious, recreational and medicinal plant in Southeast Asia. The leaves, which are the most commonly used plant part, are pungent with aromatic flavor and are widely consumed as a mouth freshener. It is carminative, stimulant, astringent and is effective against parasitic worms. Experimental studies have shown that it possess diverse biological and pharmacological effects, which includes antibacterial, antifungal, larvicidal, antiprotozal, anticaries, gastroprotective effects, free radical scavenging, antioxidant, anti-inflammatory hepatoprotective, immunomodulatory, antiulcer and chemopreventive activities. The active principles hydroxychavicol, allylpyrocatechol and eugenol with their plethora of pharmacological properties may also have the potential to develop as bioactive lead molecule. In this review, an attempt is made to summarize the religious, traditional uses, phytochemical composition and experimentally validated pharmacological properties of Piper betel. Emphasis is also placed on aspects warranting detail studies for it to be of pharmaceutical/clinical use to humans.