Butein, a plant polyphenol, has been reported to exhibit several important pharmacological effects, such as anti-inflammatory, anti-cancer, anti-oxidant and anti-angiogenic. It was first found in Toxicodendronvernicifluum, a tree widely used as a local food additive and therapeutic supplement in South East Asia. It can also be isolated from the heartwood of Dalbergiaodorifera, the seed of Cyclopiasubternata and the stems of Semecarpusanacardium, as well as many other plants. Butein was shown to be a specific protein tyrosine kinase inhibitor. This compound inhibited tyrosine-specific protein kinase activities of EGF receptor and p60(c-Src). In preclinical settings, it was shown to improve the treatment outcome of several chronic diseases including inflammation, neurological disorders, neoplasms, atherosclerosis, as well as infectious diseases, and most of these actions were accomplished by the inhibition of the transcription factor NF-κB and its downstream targets.