Monastrol also inhibits bipolar spindle formation in Xenopus egg extracts. Monastrol arrests cells in mitosis with monoastral spindles comprised of a radial array of microtubules surrounded by a ring of chromosomes while it does not affect microtubules in interphase cells or microtubule polymerization in vitro. In HeLa cells, monastrol activates the spindle checkpoint, leading to mitotic arrest and apoptosis. Monastrol is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cell lines. Monastrol treatment can decrease cell viability in MCF-7 tumor cells.
|Cell lines||BS-C-1 (monkey epithelial kidney) cells|
|Preparation method||For the double thymidine arrest, exponentially growing BS-C-1 cells are cultured for 16 h in normal growth medium containing 2 mM thymidine. After this, the cells are released into normal growth medium supplemented with 24 μM deoxycytidine for 9 h. The second thymidine block is imposed for 16 h during which the cells were maintained in serum-free medium containing 2 mM thymidine. Finally, the cells are released into normal growth medium containing 24 μM deoxycytidine to which is added either 100 μM monastrol or 0.1% DMSO. To assess the reversibility of the effect of monastrol and nocodazole treatment, BS-C-1 cells plated on coverslips are treated for 4 h in normal growth medium containing either 2 μM nocodazole or 100 μM monastrol and then released into normal medium. At the different time points, coverslips are processed for immunofluorescence and the cells in interphase or mitosis are counted and categorized.|
|Incubation time||4 h|
|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.
|CAS Number||329689-23-8; 254753-54-3|
|Solubility||DMSO: 50 mg/mL|
Comparison of the Effects of Monastrol and Oxomonastrol on Human Hepatoma Cell Line HepG2/C3A.
Marques LA, et al. Anticancer Res. 2017 Mar;37(3):1197-1204. PMID: 28314282.
Antiproliferative activity of monastrol in human adenocarcinoma (MCF-7) and non-tumor (HB4a) breast cells.
Marques LA, et al. Naunyn Schmiedebergs Arch Pharmacol. 2016 Dec;389(12):1279-1288. PMID: 27592117.
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