Norcantharidin, a clinical used chemotherapeutic agent, acts as a powerful inhibitor by interfering with fibrinogen-integrin αIIbβ3 binding in human platelets

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題名:	Norcantharidin, a clinical used chemotherapeutic agent, acts as a powerful inhibitor by interfering with fibrinogen-integrin αIIbβ3 binding in human platelets
作者:	Hsia, Chih-Hsuan;Lu, Wan-Jung;Lin, Kuan-Hung;Chou, Duen-Suey;Geraldine, Pitchairaj;Jayakuma, Thanasekaran;Chang, Nen-Chung;Sheu, Joen-Rong
貢獻者:	視光學系
關鍵詞:	antithrombosis;fibrinogen;integrin αIIbβ3;norcantharidin;platelet aggregation
日期:	2018-01-01
上傳時間:	2025-08-11 14:44:18 (UTC+8)
摘要:	During platelet activation, fibrinogen binds to its specific platelet receptor, integrin αIIb β3 , thus completing the final common pathway for platelet aggregation. Norcantharidin (NCTD) is a promising anticancer agent in China from medicinal insect blister beetle. In this study, we provided the evidence to demonstrate NCTD (0.1-1.0 μM) possesses very powerful antiplatelet activity in human platelets; nevertheless, it had no effects on surface P-selectin expression and only slight inhibition on ATP-release reaction in activated platelets. Moreover, NCTD markedly hindered integrin αIIb β3 activation by interfering with the binding of FITC-labelled PAC-1. It also markedly reduced the number of adherent platelets and the single platelet spreading area on immobilized fibrinogen as well as clot retraction. Additionally, NCTD attenuated phosphorylation of proteins such as integrin β3 , Src and FAK in platelets spreading on immobilized fibrinogen. These results indicate that NCTD restricts integrin αIIb β3 -mediated outside-in signalling in human platelets. Besides, NCTD substantially prolonged the closure time in human whole blood and increased the occlusion time of thrombotic platelet plug formation and prolonged the bleeding time in mice. In conclusion, NCTD has dual activities, it can be a chemotherapeutic agent for cancer treatment, and the other side it possesses powerful antiplatelet activity for treating thromboembolic disorders.
關聯:	Journal of Cellular And Molecular Medicine, 22, 2142-2152. https://doi.org/10.1111/jcmm.13488
顯示於類別:	[視光學系] 期刊論文

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