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A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3
Joint Authors
Ding, Xue
Liu, Tong-dan
Xie, Zhou-ling
Zhao, Qi
Cao, Yuan
Liu, Xiao-dong
Wang, Cai-hui
Gamariel, Rwibasira Rudinga
Li, Zhi-yu
Ming, Xin
Kong, Yi
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-12-20
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
Integrin αIIbβ3 plays a crucial role in the process of platelet aggregation.
Three integrin αIIbβ3 antagonists (abciximab, eptifibatide, and tirofiban) have been approved by FDA for clinical use.
Unfortunately, they all showed severe side effects such as thrombocytopenia and bleeding risk.
Thus, researches on the development of more effective and safer antiplatelet agents are needed.
In this manuscript we reported a novel naphthalenic derivative compound ND-1 with potent antithrombotic effect and lower bleeding risk.
ND-1 inhibited ADP-, collagen-, thrombin-, and U46619-induced platelet aggregation with IC50 values of 1.29, 14.46, 12.84, and 40.24 μM, respectively.
Mechanism studies indicated that ND-1 inhibited the binding of fibrinogen to integrin αIIbβ3 in a dose-dependent manner with an IC50 value of 3.12 μM.
ND-1 inhibited P-selectin expression induced by ADP, collagen, thrombin, and U46619 on the surface of platelets.
Additionally, this compound reduced platelets spreading to the immobilized fibrinogen.
In vivo, ND-1 potently decreased thrombus formation in an arteriovenous shunt thrombosis model in rats and slightly prolonged bleeding time in a tail cutting model in mice.
Taken together, our results reveal that ND-1 is a novel antagonist of αIIbβ3 with strong antithrombotic effect and lower bleeding risk.
American Psychological Association (APA)
Ding, Xue& Liu, Tong-dan& Xie, Zhou-ling& Zhao, Qi& Cao, Yuan& Liu, Xiao-dong…[et al.]. 2016. A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3. BioMed Research International،Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1099093
Modern Language Association (MLA)
Ding, Xue…[et al.]. A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3. BioMed Research International No. 2016 (2016), pp.1-8.
https://search.emarefa.net/detail/BIM-1099093
American Medical Association (AMA)
Ding, Xue& Liu, Tong-dan& Xie, Zhou-ling& Zhao, Qi& Cao, Yuan& Liu, Xiao-dong…[et al.]. A Naphthalenic Derivative ND-1 Inhibits Thrombus Formation by Interfering the Binding of Fibrinogen to Integrin αIIbβ3. BioMed Research International. 2016. Vol. 2016, no. 2016, pp.1-8.
https://search.emarefa.net/detail/BIM-1099093
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1099093