Abstract:Ligustrazine is a bioactive component contained in Chuanxiong （Ligusticum chuanxiong Hort），Curcuma aromatica salisb （Zingiberaceae），Jatropha podagrica （Euphorbiaceae） as well as vinegar，liquor and nat to fermented by Bacillus subtilis. A comprehensive review on the bioactivity of ligustrazine is presented，such as anti-tumor，anti-inflammation，anti-apoptosis，vasodilation and so on. In addition，ligustrazine had been widely used to treat cardiovascular and cerebrovascular diseases. This paper summarizes the research progress of structural characteristics，toxicology characteristics and bioactivities of ligustrazine for the last five years.