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Chuanxiong (Ligusticum wallichi Franchat) was first described in a traditional Chinese medicine book, Shennong Bencaojing, written in 200 BC. It has been used in clinical treatment for more than 2000 years . The bioactive component, 2, 3, 5, 6-tetramethylpyrazine (TMP) was extracted from Chuanxiong in 1973 . Currently, there are 36 pharmaceutical factories that produce injections or tablets in China . These medicines were firstly used in treatment of patients with neural disease with mild side effects, such as, ischemic, cerebral infarction, Alzheimer’s disease (AD), Parkinson’s disease (PD) and multiple sclerosis (MS) . However, accumulating evidence has confirmed that combining TMP with other treatments could significantly attenuate multidrug resistance of chemotherapy and inhibit proliferation and metastasis of cancer cells . This mini-review is focused on the application and mechanism of TMP to proliferation and metastasis of cancer cells.