Vitexin is an apigenin flavone glycoside and it is extensively present in numerous edible and medicinal plants. It is considered as important as other flavonoids. It possessed a variety of biological properties, including anti-oxidation, anti-inflammation, anticancer, neuron-protective, cardio-protective, hepatopancreatic protective effects. Other reported health relevant effects, includes fat reduction and glucose metabolism. The possible mechanism of protective effect through activation or inhibition of the different signaling pathways like AMPKa, Nrf-2, mTOR, PUMA, MMP, PARP, JNK, p38, Bcl-2/Bax ratio etc. The molecular targets of vitexin are very critical to utilize its potential effect as emerging chemopreventive and chemotherapeutic agent.