Colchicine
作者：齐岳
发布时间：2023-08-30
09:00:47
点击数：
产品名称：Colchicine
产品描述：
| 植物来源 | 天然产物 > 秋水仙科 > 秋水仙属 |
| 结构类型 | 天然产物 > 生物碱 |
| 产品描述 | Colchicine is a tubulin inhibitor (IC50: 3 nM) and blocks polymerization of microtubules by binding to tubulin. |
| 靶点活性 | microtubule:3 nM |
| 体外活性 | 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]. |
| 体内活性 | 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]. |
| 动物实验 | 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. |
| 别名 | 秋水仙碱, Colchisol, Colchineos, 秋水仙素, Colcin |
| 分子量 | 399.44 |
| 分子式 | C22H25NO6 |
| CAS No. | 64-86-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 39.9 mg/mL(100 mM)
H2O: 1.33 mg/mL(3.34 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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