ReferenceID 6073
The Antithrombotic Agent Pterostilbene Interferes with Integrin αIIbβ3-Mediated Inside-Out and Outside-In Signals in Human Platelets
Int J Mol Sci
Platelets play a crucial role in the physiology of primary hemostasis and pathological processes such as arterial thrombosis; thus, developing a therapeutic target that prevents platelet activation can reduce arterial th
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- Reference Id
- 6073
- Evidence Id
- 22663
- Core Evidence Id
- 22663
- Source Reference Id
- 5409
- Herb2 Reference Id
- HBREF006206
- Subject Paper Key
- HBIN041217_33807403
- Pubmed Id
- 33807403
- Doi
- 10.3390/ijms22073643
- Paper Title
- The Antithrombotic Agent Pterostilbene Interferes with Integrin αIIbβ3-Mediated Inside-Out and Outside-In Signals in Human Platelets
- Paper Abstract
- Platelets play a crucial role in the physiology of primary hemostasis and pathological processes such as arterial thrombosis; thus, developing a therapeutic target that prevents platelet activation can reduce arterial thrombosis. Pterostilbene (PTE) has remarkable pharmacological activities, including anticancer and neuroprotection. Few studies have reported the effects of pterostilbene on platelet activation. Thus, we examined the inhibitory mechanisms of pterostilbene in human platelets and its role in vascular thrombosis prevention in mice. At low concentrations (2-8 muM), pterostilbene strongly inhibited collagen-induced platelet aggregation. Furthermore, pterostilbene markedly diminished Lyn, Fyn, and Syk phosphorylation and hydroxyl radical formation stimulated by collagen. Moreover, PTE directly hindered integrin alphaIIbbeta3 activation through interfering with PAC-1 binding stimulated by collagen. In addition, pterostilbene affected integrin alphaIIbbeta3-mediated outside-in signaling, such as integrin beta3, Src, and FAK phosphorylation, and reduced the number of adherent platelets and the single platelet spreading area on immobilized fibrinogen as well as thrombin-stimulated fibrin clot retraction. Furthermore, pterostilbene substantially prolonged the occlusion time of thrombotic platelet plug formation in mice. This study demonstrated that pterostilbene exhibits a strong activity against platelet activation through the inhibition of integrin alphaIIbbeta3-mediated inside-out and outside-in signaling, suggesting that pterostilbene can serve as a therapeutic agent for thromboembolic disorders.
- Journal
- Int J Mol Sci
- Publish Year
- 2021
- Experiment Subject
- mouse; human
- Experiment Type
- Animal & Cell Experiment
- Phenotype Related
- Arterial Thrombosis; Thromboembolic Disorders; Vascular Thrombosis
- Paper Title Cn
- Paper Title En
- The Antithrombotic Agent Pterostilbene Interferes with Integrin αIIbβ3-Mediated Inside-Out and Outside-In Signals in Human Platelets
- Bilingual Status
- semi_complete