Effect of mono-guanidine-like derivatives on platelet aggregation and tumour cell induced platelet aggregation
Nadhim Kamil Hante, Aaron P. Keogh, Yanni Huang, Tanya Kapoor, Harriet Bennett-Lenane, Eleanor Walsh, Isabel Rozas, Carlos Medina, Maria Jose Santos-Martinez
TL;DR
This study explores new guanidine-based compounds that may inhibit platelet aggregation and reduce tumor cell interactions with platelets.
Contribution
The study identifies novel aryl guanidine-like derivatives with antiplatelet and anti-tumor cell aggregation properties.
Findings
Three compounds significantly inhibited platelet aggregation induced by ADP and collagen.
These compounds modulated tumor cell-induced platelet aggregation across three cancer cell lines.
The compounds showed high affinity for H2 histamine receptors and α2C-adrenoceptors.
Abstract
Antiplatelet agents are the cornerstone for the treatment and prevention of cardiovascular diseases. However, they can induce severe side effects such as gastrointestinal bleeding. The main aim of this study is to determine the effect that novel guanidine-based derivatives exert on platelet aggregation. From a screening, in collaboration with the Psychoactive Drug Screening Project service of several compounds from our in-house library of α2-adrenoceptors' ligands, four compounds showed high to medium affinity towards α2C-adrenoceptors and H2 histamine receptors. Based on the structure of these compounds, another two in-house α2-adrenoceptors' ligands were also selected. The effect of the six compounds on platelet aggregation was investigated by light transmission aggregometry and optical microscopy. Flow cytometry was used to analyse their effect on platelet activation by measuring the…
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Taxonomy
TopicsAdenosine and Purinergic Signaling · Antiplatelet Therapy and Cardiovascular Diseases · Inflammatory Biomarkers in Disease Prognosis