Abstract: Tanshinone is a class of lipophilic bioactive compounds extracted from the traditional Chinese herb Salvia miltiorrhiza, primarily consists of monosubstituted compounds such as tanshinone I, tanshinone IIA, dihydrotanshinone, 3-hydroxytanshinone, and cryptotanshinone, et al. These monosubstituted compounds exhibit diverse pharmacological effects including antibacterial and anti-inflammatory activities, anti-tumor effects, and cardiovascular protection. Multiple studies have suggested that tanshinone may exert its pharmacological activity by modulating various cell signaling pathways or targeting key drivers of disease progression. This review aims to comprehensively summarize the pharmacological mechanisms of action of various monosubstituted compounds of tanshinone in recent years, thereby providing theoretical support for subsequent research and clinical application of tanshinone-based drugs.