Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM. 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.
|Source||Cancer Res (2017). Figure 2. Colchicine|
|Method||Scratch migration assay|
|Cell Lines||A375 and RPMI7951 cells|
|Incubation Time||12 and 24 h|
|Results||The effect of DJ101 on A375 cell colony formation was similar to colchicine at the same concentration, which had colonies covering a total area of 34.7% ± 1.5%|
|Cell lines||COS-7 cells|
|Preparation method||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.|
|Incubation time||5 min|
|Animal models||Male Sprague–Dawley rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 45 mg/mL|
Fab fragments of ovine antibody to colchicine enhance its clearance in the rat.
Peake PW, et al. Clin Toxicol (Phila). 2015 Jun;53(5):427-32. PMID: 25858137.
The colchicine derivative CT20126 shows a novel microtubule-modulating activity with apoptosis.
Kim SK, et al. Exp Mol Med. 2013 Apr 19;45:e19. PMID: 23598593.
|Related Microtubule Products|
VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
Crolibulin (also known as EPC2407 and crinobulin) is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
|Ansamitocin P 3
Ansamitocin P-3 is a microtubule inhibitor, it is also a macrocyclic antitumor antibiotic.
Epothilone D is a potent microtubule stabilizer.
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