Delays in detection, increased mortality rate and 5-year survival rate, chemo- resistance to conventional therapies, chances of secondary tumor formation leading to field cancerization after cure are the major concerns faced today in oral cancer diagnosis and treatment. Physical and physiological side effects produced by the conventional treatment option in oral cancer are also remarkable problem forcing people to opt for the unconventional alternative and complementary medicines and chemopreventive strategies of herbal medications. This overview highlights on the natural chemopre-ventive components reported in the recent literatures which have shown to exert anticancer potential against oral precancerous and cancerous lesions, as well as possess chemopreventive and modulating efficacy emphasizing the major molecular mechanisms beneath the process. Implementation of these dietary chemopreventive approaches in daily routine, discussed in this chapter, may further aid in reduction of global oral cancer burden. © 2017 by Apple Academic Press, Inc.