Colchicine 是微管蛋白抑制剂和微管干扰剂，通过与微管蛋白结合来阻断微管的聚合，IC50值为 3 nM。它还是α3甘氨酸受体的竞争性拮抗剂。

Colchicine is a tubulin inhibitor (IC50: 3 nM) and blocks polymerization of microtubules by binding to tubulin.

Colchicine (1 μM) 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[1]. Colchicine treatment inhibits 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 inhibits the protein expression of cleaved caspase-1 and mature IL-1β, without affecting the mRNA expression of NLRP3 and IL-1β [2].

Vehicle or Colchicine (1 mg/kg) is administered orally 30 min prior to indomethacin administration. The lesions stained with Evans blue in the small intestine are smaller in Colchicine-treated mice than those in vehicle-treated mice 24 h after indomethacin administration. Colchicine treatment significantly reduces the lesion index at doses of 1 mg/kg and 3 mg/kg (by 86% and 94%, respectively) compared with vehicle treatment. Colchicine treatment significantly inhibits the protein levels of mature IL-1β at doses of 1 mg/kg and 3 mg/kg (by 56% and 69%, respectively) without affecting those of pro-IL-1β. Colchicine treatment also significantly inhibits the protein levels of cleaved caspase-1 at doses of 1 mg/kg and 3 mg/kg (by 26% and 39%, respectively) without affecting those of procaspase-1 [2].

a C57BL/6 background are used. To examine the effects of Colchicine on NSAID-induced small intestinal injury, vehicle or Colchicine (1 or 3 mg/kg) is administered orally 30 min prior to indomethacin administration. Mice received intraperitoneal injections of sterilized phosphate buffered saline or mouse recombinant IL-1β (0.1 μg/kg) 3 h after indomethacin treatment. Vehicle or Colchicine (1 or 3 mg/kg) is also administered to NLRP3?/? mice before indomethacin administration. The lesion index is evaluated 24 h after indomethacin administration and examined mRNA and protein expression of inflammasome components 6 h after indomethacin administration.

64-86-8

C22H25NO6

399.443

Colchineos;Colcin;Colchisol;秋水仙碱;秋水仙素

DMSO:39.9 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years