Tanshen, the rhizome of Salvia miltiorrhiza Bunge, has been used in Chinese traditional medicine (TCM) for multiple therapeutic remedies. The major constituents of Tanshen include water‐soluble phenolic acids and lipophilic tanshinones. Phenolic acids possess antioxidant and anticoagulant activities, whereas tanshinones show antibacterial, antioxidant, and antineoplastic activities. This review will focus on recent developments concerning the chemical constituents of Tanshen and their biological activities. These chemical and biological studies continue to increase our understanding about a scientific basis for the traditional clinical use of Tanshen and can also contribute to the development of new drug candidates. Recently, in the author's laboratory, a new compound, neo‐tanshinlactone, was discovered to have potent selective antibreast cancer activity. This compound might serve as a lead for developing promising antibreast cancer clinical trials candidates. © 2006 Wiley Periodicals, Inc. Med Res Rev, 27, No. 1, 133–148, 2007