Delineation of platelet activation pathway of Scutellarein revealed its intracellular target as Protein Kinase C

摘要: Erigeron breviscapus has been widely used in traditional Chinese medicine (TCM) and its total flavonoid component is commonly to treat ischemic stroke, coronary heart disease, diabetes hypertension. Scutellarin the major ingredient of E. scutellarein one main bioactive metabolites scutellarin vivo, but latter's pharmacological activities have not fully characterized. Provided evidence that could inhibit platelet aggregation, effect on rat washed platelets underlying mechanisms were evaluated our research. Scutellarein inhibited adhesion aggregation induced by multiple G protein coupled receptor agonists such as thrombin, U46619 ADP, a concentration-dependent manner. Furthermore, mild intracellular Ca(2+) mobilization cyclic AMP (cAMP) level was observed. On other hand, role potential kinase C (PKC) inhibitor confirmed PKC activity analysis molecular docking. The phorbol myristate acetate-induced assay with or without ADP implied takes PKC(s) primary target(s), acts it reversible way. Finally, promising agent exhibited high inhibition ADP-induced among analogues. This study clarifies PKC-related signaling pathway involved antiplatelet action scutellarein, may be beneficial for treatment cardiovascular diseases.