| 摘要: | Treatment and prevention for cardiovascular diseases (CVDs), the most common cause of death globally, are urgent issues. In the human body, platelets play a vital role in hemostasis and thrombosis. Hence, platelet activation and aggregation get involved in various CVDs. Nowadays, several natural compounds proved cardio-protective effects, such as ginkgetin (GK), a non-toxic biflavone. The well-known pharmacological activities of GK are anti-cancer, anti-inflammatory, neuroprotective, hepatoprotective, and antimicrobial. A study has shown the antiplatelet aggregation effect of GK on human platelet-rich plasma. However, no research has revealed the mechanism under antiplatelet effects of this biflavone compound. The results of this investigation show that the low concentration of GK (IC50=0.5 µM) inhibited platelet aggregation stimulated by collagen, whereas a higher concentration of 5 µM GK inhibited arachidonic acid (AA)-induced platelet aggregation. However, no evidence of GK was detected to inhibit platelet aggregation in response to thrombin and U46619. LDH assay showed that GK at concentrations up to 100 µM had no cytotoxic effects on human platelets. Further investigation demonstrates that GK inhibited collagen-induced calcium mobilization, ATP release, and P-selectin expression in human platelets. This compound significantly inhibited PLC gamma 2-PKC, Akt and MAPKs signaling cascades to exert its collagen-induced antiplatelet activation. In conclusion, our study suggests that GK acts as an antiplatelet agent, could be a potential candidate for prevention of CVDs. |
