Review Article

Therapeutic potential of colchicine in cardiovascular medicine: a pharmacological review

Fan-shun Zhang1, Qing-ze He1, Chengxue Helena Qin2, Peter J. Little3,4, Jian-ping Weng1,5, Suo-wen Xu1,5
1 Institute of Endocrine and Metabolic Diseases, The First Affiliated Hospital of USTC, Division of Life Science and Medicine, University of Science and Technology of China, Hefei 230001, China
2 Faculty of Pharmacy and Pharmaceutical Sciences, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), 381 Royal Parade, Parkville 3052 VIC, Australia
3 Sunshine Coast Health Institute, University of the Sunshine Coast, Birtinya 4575 QLD, Australia
4 School of Pharmacy, The University of Queensland, Woolloongabba 4102 QLD, Australia
5 Biomedical Sciences and Health Laboratory of Anhui Province, University of Science & Technology of China, Hefei 230027, China
Correspondence to: Suo-wen Xu: sxu1984@ustc.edu.cn,
DOI: 10.1038/s41401-021-00835-w
Received: 7 September 2021
Accepted: 25 November 2021
Advance online: 19 January 2022

Abstract

Colchicine is an ancient herbal drug derived from Colchicum autumnale. It was first used to treat familial Mediterranean fever and gout. Based on its unique efficacy as an anti-inflammatory agent, colchicine has been used in the therapy of cardiovascular diseases including coronary artery disease, atherosclerosis, recurrent pericarditis, vascular restenosis, heart failure, and myocardial infarction. More recently, colchicine has also shown therapeutic efficacy in alleviating cardiovascular complications of COVID-19. COLCOT and LoDoCo2 are two milestone clinical trials that confirm the curative effect of long-term administration of colchicine in reducing the incidence of cardiovascular events in patients with coronary artery disease. There is growing interest in studying the anti- inflammatory mechanisms of colchicine. The anti-inflammatory action of colchicine is mediated mainly through inhibiting the assembly of microtubules. At the cellular level, colchicine inhibits the following: (1) endothelial cell dysfunction and inflammation; (2) smooth muscle cell proliferation and migration; (3) macrophage chemotaxis, migration, and adhesion; (4) platelet activation. At the molecular level, colchicine reduces proinflammatory cytokine release and inhibits NF-κB signaling and NLRP3 inflammasome activation. In this review, we summarize the current clinical trials with proven curative effect of colchicine in treating cardiovascular diseases. We also systematically discuss the mechanisms of colchicine action in cardiovascular therapeutics. Altogether, colchicine, a bioactive constituent from an ancient medicinal herb, exerts unique anti-inflammatory effects and prominent cardiovascular actions, and will charter a new page in cardiovascular medicine.
Keywords: colchicine; anti-inflammatory drug; cardiovascular diseases; coronary artery disease; atherosclerosis; recurrent pericarditis; restenosis; heart failure; myocardial infarction; cardiovascular complications of COVID-19; microtubules; NF-κB; NLRP3 inflammas

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