The Effect of Antiplatelet P2Y₁₂ Receptor Blockers on Anti-Inflammatory Properties of Vascular Endothelial Cells in Vitro

Introduction: Cardiovascular pharmacotherapy aims to reduce cardiovascular outcomes and to restore the endothelium. It is emphasised that P2Y₁₂ receptor blockers, apart from its antiplatelet effect, have beneficial effect on endothelial cells. Most of the findings documenting its favourable effects come from the clinical trials. Less is known about its direct impact on endothelium cultured in vitro.
Purpose: We assess the impact of P2Y₁₂ receptor blockers on anti-inflammatory properties of cultured endothelial cells.
Methods: HUVEC line EA.hy926 were exposed 24 h to the culture medium supplemented with Il -1 (1 ng/ml) and anti-platelet drugs, in concentrations detected in the blood during standard therapy, with loading doses (LD) and clinically doses (CD) (ticagrelor - LD: 2 µM, CD: 1 µM, prasugrel - LD: 2 µM, CD: 0.3 µM, clopidogrel LD: 0.4 µM, CD: 0.04 µM). After the treatment the following parameters were measured in cultured medium using ELISA tests: sICAM-1, Il-6, Il-8, and MCP-1. Cell viability was measure using Trypane blue exclusion test.
Results (mean ± SD) are presented in the Table
Conclusions: P2Y₁₂ receptor blockers in clinically doses do not alter cell viability. Of the three tested drugs, Ticagrelor in LD and CD has the potent anti-inflammatory effect on the endothelium in vitro.