生物活性 | |||
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描述 | Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[3]. Exposure to 1 mM colchicine, a microtubule disrupting agent, triggered apoptosis in rat cerebellar granule cells (CGC). Colchicine treatment also causes alterations in Ca2+ responses to chemical depolarization and a moderate, but progressive, increase in the resting intracellular Ca2+ concentration[4]. Colchicine appears to be efficacious and well tolerated for recurrent pericarditis/postpericardiotomy syndrome and recurrence of postprocedural atrial fibrillation[5]. Colchicine treatment inhibited indomethacin-induced small intestinal injury by 86% (1 mg/kg) and 94% (3 mg/kg) as indicated by the lesion index 24 h after indomethacin administration. Colchicine inhibited the protein expression of cleaved caspase-1 and mature IL-1β, without affecting the mRNA expression of NLRP3 and IL-1β[6]. Short-term treatment with colchicine (0.1 mg/kg/day, p.o.) successfully attenuated pro-inflammatory cytokines and NLRP3 inflammasome, and improved cardiac function, heart failure, and survival after MI (myocardial infarction)[7]. Colchicine reduces ALI (acute lung injury) and respiratory failure in experimental ARDS (acute respiratory distress syndrome) in relation with reduced lung neutrophil recruitment and reduced circulating leukocyte activation[8]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.50mL 0.50mL 0.25mL |
12.52mL 2.50mL 1.25mL |
25.04mL 5.01mL 2.50mL |
参考文献 |
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[2]Hastie SB. Interactions of colchicine with tubulin. Pharmacol Ther. 1991;51(3):377-401. [3]Hastie SB. Interactions of colchicine with tubulin. Pharmacol Ther. 1991;51(3):377-401 |