Garcinol (Gar), a polyisoprenylated benzophenone derivative, is purified from the rind of the Garcinia indica fruit, and its antioxidative, antiglycation and free radical-scavenging activities have been studied previously. Although the fruit has been consumed traditionally for centuries, its biological activities, specifically its anticancer potential, were only determined in recent scientific investigations. Gar is also effective in blocking azoxymethane-induced colonic aberrant crypt focus formation and induces apoptosis in human HL60 cancer cells. Another study demonstrated that cigarette smoke extract-induced COX-2 expression is blocked by Gar pretreatment. In a previous study, we demonstrated that the α9-nicotinic receptor (α9-nAChR) was significantly induced by nicotine (Nic) in human breast cancer cells. We also found that Nic-induced α9-nAChR protein expression was blocked by Gar. Both in vitro and in vivo studies have demonstrated the potential of this compound against several cancer types, including breast cancer, colon cancer, pancreatic cancer, and leukemia. These findings suggest a possible chemopreventive and/or therapeutic potential of Gar through the inhibition of different types of hazard factor-induced protein expression, which is known to play a role in environmental factor-mediated tumorigenesis.