Salvianolic acids from antithrombotic Traditional Chinese Medicine Danshen are antagonists of human P2Y₁ and P2Y₁₂ receptors.

ABSTRACT: Many hemorheologic Traditional Chinese Medicines (TCMs) that are widely-used clinically lack molecular mechanisms of action. We hypothesized that some of the active components of hemorheologic TCMs may function through targeting prothrombotic P2Y₁ and/or P2Y₁₂ receptors. The interactions between 253 antithrombotic compounds from TCM and these two G protein-coupled P2Y receptors were evaluated using virtual screening. Eleven highly ranked hits were further tested in radioligand binding and functional assays. Among these compounds, salvianolic acid A and C antagonized the activity of both P2Y₁ and P2Y₁₂ receptors in the low µM range, while salvianolic acid B antagonized the P2Y₁₂ receptor. These three salvianolic acids are the major acti

SUBMITTER: Liu X 

PROVIDER: S-EPMC5967328 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature