Tanshinone I derived from the traditional herbal medicine, Salvia miltiorrhiza Bunge, is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. It was discovered, that tanshinone I may serve as an effective drug for the treatment of breast cancer. In addition, it induced apoptosis and pro-survival autophagy via inhibiting Bcl-2 expression on gastric cancer, and the combination of chloroquine and Tanshinone I could inhibit tumor growth more efficiently than monotherapy, which might be considered as an effective strategy for the treatment for gastric cancer. Tanshinone I showed in vivo anti-inflammatory activity via inhibition of type IIA human recombinant sPLA2 (phospholipase A (2)).