Background: Salvia is the largest genus of family Lamiaceae and has nearly 1000 species. This genus
produces several representative phytometabolites, e.g., diterpenoids and phenolic acids. The traditional uses in ethnomedicine
and contemporary experimental studies have corroborated extensive therapeutic efficacy of Salvia
plants. Drug metabolism and pharmacokinetic (DMPK) studies of Salvia natural products and their derivatives are
indispensable in the optimization of lead compounds. New chemical entity with improved DMPK profiles is preferred.
So far, there are few summaries concerning about the DMPK features of Salvia derived medicinal compounds.
Tanshinones and Salvianolic acids raise concerns of herb-drug interaction. DMPK studies of various Salvia
species, especially Salvia miltiorrhiza, are swiftly increasing.
Objective: Here, the latest awareness, as well as the gaps of the DMPK issues in drug development and clinical usage
of Salvia compounds, was highlighted.
Conclusion: Herb-herb interactions of Salvia-containing traditional Chinese medicine (TCM) medicine pair/formula
significantly impact the PK/pharmacodynamic performance of compounds thereof, which may inspire researchers to
develop novel herbal formula. While the absorption, distribution, metabolism, elimination and toxicity (ADME/T) of
some tanshinones and Salvianolic acids have been outlined, DMPK studies should be extended to more compounds,
Salvia species, and Salvia-containing formulations. In the context of systems pharmacology, the DMPK knowledgebase
is expected to streamline the Salvia-based drug discovery and development.