Vinblastine sulfate

Biological Activity

Vinblastine sulfate ia a plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Vinblastine sulfate inhibits normal microtubule assembly and causes aberrant tubulin polymerization. Vinblastine sulfate blocks binding of tubulin to microtubule proteins.Vinblastine sulfate Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression. Cancer chemotherapeutic agent. Vinblastine sulfate is a microtubule disrupter. Vinblastine sulfate induces apoptosis in cultured hepatocytes and human lymphoma cells.Vinblastine sulfate shown to inhibit autophagosome maturation.

Protocol

Cell Experiment
Cell lines	Chinese hamster ovary (CHO) cells
Preparation method	Six-well treatment plates are set up that contained 5 ×104 cells/mL in each well, suspended in 3 mL culture medium, and these are treated with vinblastine for 3 h followed by 21 h growth.
Concentrations	1% (v/v) (dissolved in DMSO)
Incubation time	3h

Animal Experiment
Animal models
Formulation
Dosages
Administration

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information

References

Vinblastine-induced phosphorylation of Bcl-2 and Bcl-XL is mediated by JNK and occurs in parallel with inactivation of the Raf-1/MEK/ERK cascade.
Fan M, et al. J Biol Chem. 2000 Sep 29;275(39):29980-5. PMID: 10913135.

Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells.
Tashiro E, et al. Jpn J Cancer Res. 1998 Sep;89(9):940-6. PMID: 9818030.

Comparison of the effects of vinblastine, vincristine, vindesine, and vinepidine on microtubule dynamics and cell proliferation in vitro.
Jordan MA, et al. Cancer Res. 1985 Jun;45(6):2741-7. PMID: 3986806.