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Entecavir as a P2X7R antagonist ameliorates platelet activation and thrombus formation.

Abstract：

:Platelet activation is the primary cause of thrombosis. The P2X7 receptor (P2X7R) is a therapeutic target of thrombosis. However, it is still unknown whether P2X7R activation affects platelet thrombus. Our molecular docking results showed that entecavir as a P2X7R antagonist interacted perfectly with the human P2X7R (hP2X7R) in silico simulation studies. Furthermore, our experimental data revealed that entecavir could act as a P2X7R antagonist to exert cytoprotective effects against platelet activation via protecting mitochondrial function, improving lipid peroxidation and increasing antioxidant activity. Correlated with this, entecavir inhibited platelet aggregation, dense-granule secretion, P-selectin expression, integrin activation and Ca2+ increase. In experimental mouse model, entecavir could significantly inhibit arteriovenous thrombosis and prolong the bleeding time. Furthermore, we found that entecavir had no significant effect on prothrombin time (PT), activated partial thrombin time (APTT), thrombin time (TT), fibrinogen (FIB), mean platelet volume (MPV) and platelet counts (PLT). This study demonstrates that entecavir markedly prevents platelet activation and thrombosis through inhibiting P2X7R without affecting coagulation system. Therefore, entecavir may be a potential candidate for treating thrombosis disease.

journal_name

J Pharmacol Sci

journal_title

Journal of pharmacological sciences

authors

Ming Y,Xin G,Ji B,Ji C,Wei Z,Zhang B,Zhang J,Yu K,Zhang X,Li S,Li Y,Xing Z,Niu H,Huang W

doi

10.1016/j.jphs.2020.07.002

subject

Has Abstract

pub_date

2020-09-01 00:00:00

pages

43-51

issue

1

eissn

1347-8613

issn

1347-8648

pii

S1347-8613(20)30066-9

journal_volume

144

pub_type

杂志文章

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