Colchicine inhibits coronary and cerebrovascular events in patients with coronary artery disease (CAD), and although known to have anti-inflammatory properties, its mechanisms of action are incompletely understood. In this study, we investigated the effects of colchicine on platelet activation with a particular focus on its effects on activation via the collagen glycoprotein (GP)VI receptor, P2Y receptor, and procoagulant platelet formation. Therapeutic concentrations of colchicine in vitro (equivalent to plasma levels) significantly decreased platelet aggregation in whole blood and in platelet rich plasma in response to collagen (multiplate aggregometry) and reduced reactive oxygen species (ROS) generation (HDCF-DA, flow cytometry) in response to GPVI stimulation with collagen related peptide-XL (CRP-XL, GPVI specific agonist). Other platelet activation pathways including P-selectin expression, GPIIb/IIIa conformational change and procoagulant platelet formation (GSAO/CD62P) (flow cytometry) were inhibited with higher concentrations of colchicine known to inhibit microtubule depolymerization. Pathway specific mechanisms of action of colchicine on platelets, including modulation of the GPVI receptor pathway at low concentrations, may contribute to its protective role in CAD.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8184800 | PMC |
| http://dx.doi.org/10.1038/s41598-021-91409-7 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Discovery of novel thienopyridine indole derivatives as inhibitors of tubulin polymerization targeting the colchicine-binding site with potent anticancer activities.
Eur J Med Chem
January 2025
School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450001, China. Electronic address:
Based on the molecular hybridization strategy, novel thienopyridine indole derivatives were designed and synthesized as tubulin polymerization inhibitors, and the in vitro antiproliferative potency on MGC-803, KYSE450 and HCT-116 cells was evaluated. Among them, compound 20b showed a broad-spectrum antiproliferative activity against 11 cancer cell lines, with IC values below 4 nmol/L. Notably, it demonstrated exceptional efficacy against MGC-803 (IC = 1.
View Article and Find Full Text PDF()-1-(3-(3-Hydroxy-4-Methoxyphenyl)-1-(3,4,5-Trimethoxyphenyl)allyl)-1-1,2,4-Triazole and Related Compounds: Their Synthesis and Biological Evaluation as Novel Antimitotic Agents Targeting Breast Cancer.
Pharmaceuticals (Basel)
January 2025
School of Pharmacy and Pharmaceutical Sciences, Panoz Institute, Trinity College Dublin, D02 PN40 Dublin, Ireland.
The synthesis of ()-1-(1,3-diphenylallyl)-1-1,2,4-triazoles and related compounds as anti-mitotic agents with activity in breast cancer was investigated. These compounds were designed as hybrids of the microtubule-targeting chalcones, indanones, and the aromatase inhibitor letrozole. : A panel of 29 compounds was synthesized and examined by a preliminary screening in estrogen receptor (ER) and progesterone receptor (PR)-positive MCF-7 breast cancer cells together with cell cycle analysis and tubulin polymerization inhibition.
View Article and Find Full Text PDFThe Anthelmintic Activity of Lam. Against Gastrointestinal Nematodes of Sheep: Rosmarinic Acid Quantification and In Silico Tubulin-Binding Studies.
Pathogens
January 2025
Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Ankara 06330, Turkey.
Gastrointestinal nematodes (GINs) inflict significant economic losses on sheep and goat farming globally due to reduced productivity and the development of anthelmintic resistance. Sustainable control strategies are urgently needed including the exploration of medicinal plants as safer alternatives to chemical anthelmintics. This genus of plants is used for anti-inflammatory, antioxidant, and antimicrobial activities.
View Article and Find Full Text PDFDevelopment of 1,2,3-triazole hybrids as multi-faced anticancer agents co-targeting EGFR/mTOR pathway and tubulin depolymerization.
Bioorg Chem
January 2025
Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia 41522 Egypt. Electronic address:
Novel 1,2,3-triazole hybrids bearing various substituents have been synthesized as potential anticancer agents. Ligand-based approach has been adopted to design these compounds relying on the hybridization of 1,2,3-triazole with α,β-unsaturated carbonyl, 5- and 6-membered heterocyclic scaffolds. All synthesized members were investigated for their cytotoxic potency against nine types comprising 60 panels of human cancerous cells by the US National Cancer Institute: Development Therapeutic Program (US_NCI_DTP).
View Article and Find Full Text PDFEctopic calcifications in the musculoskeletal field: the basis for preventive and curative pharmacological strategies.
Clin Rheumatol
January 2025
Center for Physical Medicine and Rehabilitation, University Clinical Center of Serbia, Belgrade, Serbia.
Ectopic calcifications occur in tendons, ligaments, entheses, muscles, and fasciae, and are often associated with pain and inflammation. In clinical settings, these calcifications are commonly treated by physical therapy and/or surgical interventions. However, there is not enough understanding of pharmacological treatments as primary cures, supportive therapy to physical or surgical treatment, or even preventive measures to avoid or diminish the development of ectopic calcifications.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!