生物活性
Colchicine是一种微管蛋白抑制剂和微管干扰剂，其IC50值为3 nM。Colchicine 还是 α3 甘氨酸受体 (GlyRs) 的竞争性拮抗剂。Colchicine is a toxic natural product and secondary metabolite, originally extracted from plants of the genus Colchicum. Colchicine inhibited stimulated endothelial adhesiveness via its effects on microtubules since vinblastine, an agent which perturbs microtubule function by other mechanisms, diminished adhesiveness whereas the photoinactivated colchicine derivative gamma-lumicolchicine was inactive. Colchicine (Colchineos, Colchisol, Colcin) had no effect on cell viability. At higher, therapeutic, concentrations colchicine (IC50 = 300 nM, P < 0.001) also diminished the expression of L-selectin on the surface of neutrophils (but not lymphocytes) without affecting expression of the beta 2-integrin CD11b/CD18. Since one of the defining characteristics of cancer cells is a significantly increased rate of mitosis, this means that cancer cells are significantly more vulnerable to colchicine poisoning than are normal cells. However, the therapeutic value of colchicine against cancer is (as is typical with chemotherapy agents) limited by its toxicity against normal cells.
化学数据
| 分子量 | 399.44 |
| 分子式 | C22H25NO6 |
| CAS号 | 64-86-8 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 45 mg/mL
Water 30 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | COS-7 cells |
| 方法 | After 20 min, the samples were mixed with 5 nM CT20126, colchicine or Taxol and incubated at 37 °C for 5 min. The samples were cooled in an ice bath for depolymerization (still within the light path cell). Successive reactions were performed for another 25 min at 37 °C. |
| 浓度 | 5 nM |
| 处理时间 | 5 min |
| 动物实验 |
|---|
| 动物模型 | Male Sprague–Dawley rats |
| 配制 | water |
| 剂量 | 5 mg/kg |
| 给药处理 | gavage |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5035 mL | 12.5175 mL | 25.035 mL |
| 5 mM | 0.5007 mL | 2.5035 mL | 5.007 mL |
| 10 mM | 0.2504 mL | 1.2518 mL | 2.5035 mL |
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