An antimitotic inhibitor of tubulin polymerization
Vincristine is a naturally occurring alkaloid that potently inhibits the tubulin addition with the inhibition constant Ki value of 0.085 μM and exhibits an anti-proliferative activity against B16 melanoma cells with the half maximal inhibition concentration IC50 value of 0.45 M [1].
Vincristine is extracted from leaves of the periwinkle plant Catharanthus roseus (L.) G. Don of the family Apocynaceae and has an asymmetric structure consisting of two dimers, a dihydroindole nucleus (vindoline) and an indole nucleus (catharanthine), that are linked by a carbon-carbon bond [2].
Vincristine has been found to be active against a wild range of malignancies, including acute lymphoblastic leukemia (ALL), acute non-lymphoblastic leukemia (ANLL), non-Hodgkin lymphoma (NHL), Hodgkin’s disease and brain tumors [2].
参考文献:
[1] Jordan MA, Himes RH, Wilson L. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res. 1985 Jun;45(6):2741-7.
[2] Gidding CE1, Kellie SJ, Kamps WA, de Graaf SS. Vincristine revisited. Crit Rev Oncol Hematol. 1999 Feb;29(3):267-87.
| Cell experiment [1]: | |
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Cell lines |
B16 melanoma cell |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
10 ~ 100 nM; 3 days |
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Applications |
In B16 melanoma cells, Vincristine inhibited the tubulin addition at assembly ends of steady-state microtubules with the Ki value of 85 nM. |
| Animal experiment [2]: | |
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Animal models |
Mice bearing human rhabdomyosarcoma xenografts Rh12 or Rh18 |
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Dosage form |
3 mg/kg; i.p.; a single dose |
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Applications |
In mice bearing human rhabdomyosarcoma xenografts Rh12 or Rh18, Vincristine (3 mg/kg, i.p., a single dose) induced mean growth delay of > 120 and > 52 days, as well as repopulating fractions of 0.06% and 5%, respectively. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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参考文献: [1]. Jordan MA, Himes RH, Wilson L. Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro. Cancer Res. 1985 Jun;45(6):2741-7. [2]. Baguley BC, Holdaway KM, Thomsen LL, Zhuang L, Zwi LJ. Inhibition of growth of colon 38 adenocarcinoma by vinblastine and colchicine: evidence for a vascular mechanism. Eur J Cancer. 1991;27(4):482-7. |
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