Artocarpesin acts on human platelet aggregation through inhibition of cyclic nucleotides and MAPKs

The cardiovascular diseases (CVDs) are becoming a critical threat to our lives in these years. It is now widely accepted that platelets play an important role in cardiovascular disease as they have a fundamental role in thrombosis. Therefore, many drugs or natural substances have been developed to treat CVDs. Cudrania tricuspidata is a regional plant containing various constituents, such as xanthones, flavonoids, organic acids, and polysaccharides. It has been widely used in East Asia as an important ethnomedicine for the treatment of many diseases such as eczema, mumps, tuberculosis and acute arthritis. Therefore, we evaluated antiplatelet effects using artocarpesin isolated from C. tricuspidata. Confirmation of the antiplatelet function of artocarpesin was made according to the following analyzes. Artocarpesin inhibited collagen-induced human platelet aggregation, calcium mobilization, glycoprotein Ilb/IIIa activation and thrombin-induced clot retraction through the regulation of associated signaling molecules. Artocarpesin increased the phosphorylation of vasodilator-stimulated phosphoprotein (VASP) and inositol 1, 4, 5-triphosphate receptor I (IP3RI). On the other hand, the phosphorylation of cytosolic phospholipase A(2) (cPLA(2)), mitogen-activated protein kinases p38, JNK and phosphoinositide 3-kinase (PI3K)/Akt decreased. Thus, the study highlights that artocarpesin has an inhibitory effect on platelet activity and thrombus formation, showing its potential value in preventing platelet-induced cardiovascular disease.

Automated summary

Cardiovascular diseases are a critical threat to our lives, and platelets play an important role in these diseases. This study evaluated the antiplatelet effects of artocarpesin, a compound isolated from Cudrania tricuspidata, and found that artocarpesin inhibits platelet activity and thrombus formation through the regulation of associated signaling molecules, highlighting its potential value in preventing platelet-induced cardiovascular diseases.