A Critical Review of Tetramethylpyrazine: Diseases and Derivatives.
As the primary active constituent of the traditional Chinese medicinal herb Ligusticum chuanxiong, Tetramethylpyrazine (TMP) has demonstrated broad therapeutic potential across multiple disease areas. Its clinical applications span cardiovascular and cerebrovascular disorders, oncology, hepatorenal protection, and respiratory diseases. The mechanisms of action involve antiplatelet aggregation, anti-inflammatory, antioxidant, and anti-apoptotic effects, as well as modulation of autophagy and multiple signaling pathways. Despite its pleiotropic efficacy, the clinical utility of TMP is constrained by unfavorable pharmacokinetic properties, including rapid metabolism and limited oral bioavailability. To overcome these limitations, researchers have developed various TMP derivatives, which exhibit significantly improved metabolic stability and enhanced pharmacological activity. This review summarizes recent advances in TMP and its derivatives over the past five years, aiming to provide insights for the future development of novel TMP-based therapeutics.