Colchicine, an orally active alkaloid, disrupts cytoskeletal function by inhibiting the polymerization of β-tubulin into microtubules, with an IC50 of 3 nM. Additionally, colchicine acts as a competitive antagonist of the α3 glycine receptor (GlyR) [1]. Colchicine exhibits a broad spectrum of anti-inflammatory, immunosuppressive, and potent anti-fibrotic effects, making it effective in controlling gout and reducing the risk of cardiovascular events [2-3].
Colchicine(10 nM; 1h) prevented foam cell formation induced by ox-LDL in macrophages differentiated from human THP-1 cells[4]. Colchicine (1 nM; 24h) treatment diminished GSK-3β phosphorylation and β-catenin translocation to the nucleus in cultured human aortic SMCs exposed to PDGF-BB stimulation[5].
Colchicine (0.102 mg/kg; 12 weeks; i.g) demonstrates anti-atherosclerotic and plaque-stabilizing effects at low doses by inhibiting foam cell formation and reducing cholesterol crystal-induced inflammation[4]. Colchicine (0.1 mg/kg/d; i.p.; 2 weeks) can restrict abdominal aortic aneurysm (AAA) formation by preventing the infiltration of immune cells into the aortic wall[6]. Colchicine inhibits the activation of the NLRP3 inflammasome, thereby preventing small intestine damage induced by non-steroidal anti-inflammatory drugs (NSAIDs)[7].
References:
[1]. Muñoz-Montesino C, Burgos CF, et,al. Inhibition of the Glycine Receptor alpha 3 Function by Colchicine. Front Pharmacol. 2020 Jul 30;11:1143. doi: 10.3389/fphar.2020.01143. PMID: 32903667; PMCID: PMC7438739.
[2]. McKenzie BJ, Wechalekar MD, et,al. Colchicine for acute gout. Cochrane Database Syst Rev. 2021 Aug 26;8(8):CD006190. doi: 10.1002/14651858.CD006190.pub3. PMID: 34438469; PMCID: PMC8407279.
[3]. Zhang FS, He QZ, et,al.Therapeutic potential of colchicine in cardiovascular medicine: a pharmacological review. Acta Pharmacol Sin. 2022 Sep;43(9):2173-2190. doi: 10.1038/s41401-021-00835-w. Epub 2022 Jan 19. PMID: 35046517; PMCID: PMC8767044.
[4]. Schwarz N, Fernando S, et,al. Colchicine exerts anti-atherosclerotic and -plaque-stabilizing effects targeting foam cell formation. FASEB J. 2023 Apr;37(4):e22846. doi: 10.1096/fj.202201469R. PMID: 36856983.
[5]. Chen M, Yang D, et,al. Colchicine Blocks Abdominal Aortic Aneurysm Development by Maintaining Vascular Smooth Muscle Cell Homeostasis. Int J Biol Sci. 2024 Mar 17;20(6):2092-2110. doi: 10.7150/ijbs.93544. PMID: 38617538; PMCID: PMC11008260.
[6]. Zhao Y, Shen QR, et,al. Colchicine protects against the development of experimental abdominal aortic aneurysm. Clin Sci (Lond). 2023 Oct 11;137(19):1533-1545. doi: 10.1042/CS20230499. PMID: 37748024; PMCID: PMC10550771.
[7]. Otani K, Watanabe T, et,al. Colchicine prevents NSAID-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Sci Rep. 2016 Sep 2;6:32587. doi: 10.1038/srep32587. PMID: 27585971; PMCID: PMC5009328.
Colchicine（秋水仙碱）是一种可口服的生物碱，通过抑制β-微管蛋白聚合成微管来破坏细胞骨架功能，Colchicine抑制微管的IC50为3 nM。Colchicine也是α3甘氨酸受体(GlyR)的竞争性拮抗剂[1]。Colchicine具有广泛的抗炎、免疫抑制和强抗纤维化作用，可用于控制痛风，降低心血管疾病风险[2-3]。
Colchicine (10 nM; 1h)抑制ox-LDL诱导（从人THP-1细胞分化的）巨噬细胞分化形成泡沫细胞 [4]。Colchicine (1 nM; 24h)减少了在PDGF-BB刺激下的人主动脉SMCs中GSK-3β磷酸化和β-catenin核易位[5]。
Colchicine (0.102 mg/kg; 12weeks; i.g)通过抑制泡沫细胞形成和胆固醇晶体诱导的炎症，在低剂量下发挥抗动脉粥样硬化和稳定斑块的作用[4]。Colchicine (0.1 mg/kg/d; i.p.; 2 weeks) 可以通过阻止免疫细胞浸润到主动脉壁来限制腹主动脉瘤(AAA)的形成[6]。Colchicine可抑制NLRP3炎性体的激活来预防非甾体抗炎药(NSAID)诱导的小肠损伤[7]。