Abstract Tanshinones, a class of lipophilic abietane-type diterpenoid, represents the major bioactive constituents of Salvia miltiorrhiza Bunge (Danshen), a key herb in traditional Chinese medicine with growing therapeutic importance. This review offers an in-depth overview of tanshinones from phytochemical and pharmacological perspectives. The review outlines the biosynthetic pathway, highlights the key synthetic approaches, and provides a detailed chemical and stereochemical characterization of the major tanshinones isomers. Pharmacologically, tanshinones exhibit broad, multi-system activities including antioxidant and anti-inflammatory effects, cardiovascular and hepatorenal protection, antitumor activity, immunomodulatory effects, and therapeutic benefits across neurological, metabolic, skeletal, respiratory, and infectious diseases. Despite their broad therapeutic potential, progression of tanshinones toward clinical application is restricted by low oral bioavailability, poor aqueous solubility, and rapid metabolism. To overcome these barriers, novel drug-delivery strategies including lipid nanocapsules, liposomes, polymeric nanoparticles, solid liquid nanoparticles, microemulsions, and nanoemulsions significantly improve solubility, stability, and pharmacokinetics. This review integrates the current evidence to guide future optimization and mechanistic exploration and support the development of innovative nanoformulations for next-generation tanshinone-based therapies.
Abdel-dayem et al. (2026) studied this question.