Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor. Ellipticine is also a natural product, isolated in 1959 from the Australian evergreen tree of the Apocynaceae family. Ellipticine can act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of cells with ellipticine results in inhibition of cell growth and proliferation.
In vivo, Ellipticine treatment results in ellipticine-derived DNA adduct generation in several healthy organs and in DNA of mammary adenocarcinoma. The induced expression of cytochrome b5 protein in liver of rats treated with ellipticine suggests that cytochrome b5 may modulate the CYP-mediated bioactivation and detoxification of ellipticine.
|Cell lines||MCF-7, U87MG, CCRF-CEM, UKF-NB-3 and UKF-NB-4 neuroblastoma cell lines|
|Preparation method||Cells in exponential growth were seeded at 1×104 per well in a 96-well microplate. After incubation (48 hours) at 37 °C in 5% CO2 saturated atmosphere the MTT solution (2 mg/ml PBS) was added, the microplates were incubated for 4 hours and cells lysed in 50% N,N-dimethylformamide containing 20% of sodium dodecyl sulfate (SDS), pH 4.5. The absorbance at 570 nm was measured for each well by multiwell ELISA reader Versamax (Molecular devices, CA, USA). The mean absorbance of medium controls was subtracted as a background. The viability of control cells was taken as 100% and the values of treated cells were calculated as a percentage of control. The IC50 values were calculated from at least 3 independent experiments using linear regression of the dose-log response curves by SOFTmaxPro.|
|Concentrations||0, 0.1, 1, 5 or 10 μM|
|Incubation time||48 hours|
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO 10 mM|
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