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Ticagrelor and clopidogrel suppress NF-κB signaling pathway to alleviate LPS-induced dysfunction in vein endothelial

Zhuyin Jia1,2,3, Yiwei Huang2, Xiaojun Ji2

  • 1Department of Cardiology, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.

BMC Cardiovascular Disorders
|January 1, 2020
PubMed

Insights

Ticagrelor and clopidogrel inhibit inflammation by suppressing the NF-κB pathway. These P2Y12 receptor antagonists reduce inflammatory factors and improve cellular function in cardiovascular disease models.

Area of Science:

  • Cardiovascular Research
  • Inflammation Biology
  • Molecular Pharmacology

Background:

  • Ticagrelor and clopidogrel are P2Y12 receptor antagonists used for thrombotic events in cardiovascular diseases.
  • Inflammation, regulated by NF-κB, is implicated in cardiovascular conditions.
  • This study investigated the role of ticagrelor and clopidogrel in regulating the NF-κB signaling pathway.

Purpose of the Study:

  • To determine if ticagrelor and clopidogrel modulate the NF-κB signaling pathway.
  • To assess the effects of these drugs on inflammatory responses and cellular functions in endothelial cells.

Main Methods:

  • Human umbilical vein endothelial cells (HUVECs) were treated with ticagrelor or clopidogrel, followed by lipopolysaccharide (LPS) stimulation.
  • Quantitative polymerase chain reaction (qPCR), western blotting, and immunofluorescence assays were used to analyze NF-κB pathway molecules and inflammatory factors.
  • Cell viability, apoptosis, cell cycle, migration, and vascular formation were assessed using various assays.

Main Results:

  • Ticagrelor and clopidogrel inhibited IκBα degradation and p65 phosphorylation.
  • These drugs prevented p65 nuclear translocation and reduced the production of inflammatory cytokines (TNFα, IL-1, IL-8, IL-6, IL-2).
  • The drugs alleviated LPS-induced decreases in cell viability, migration, and angiogenesis, and normalized cell cycle and apoptosis.

Conclusions:

  • Ticagrelor and clopidogrel suppress the NF-κB signaling pathway.
  • These P2Y12 receptor antagonists mitigate cellular dysfunction by inhibiting inflammation.
  • The findings suggest a broader therapeutic role for ticagrelor and clopidogrel in inflammatory cardiovascular conditions.
Abstract

Keywords:
ClopidogrelHUVECsLPS-induced dysfunctionNF-ΚB signaling pathwayTicagrelor

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