Cell lines

Jurkat CD4+ T cell leukemia cell line

Preparation method

The solubility of this compound in DMSO is >17.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

2.5, 5, 10, 20 or 40 μM; 1 ~ 3 days

Applications

In Jurkat CD4+ T cell leukemia cell line, Orlistat, at the concentration of 40 μM, reduced O6-methylguanine-DNA methyltransferase (MGMT) expression by >50% on day 2, whereas little or no effect was observed when lower concentrations were applied. The effect of Orlistat persisted on day 3. However, on day 1, Orlistat did not remarkably change the MGMT level.

Animal models

Nude mice bearing PC-3 tumors

Dosage form

155 mg/kg or 240 mg/kg/day; i.p.

Applications

In nude mice bearing PC-3 tumors, Orlistat at the dose of 240 mg/kg/day inhibited tumor growth and induced tumor cell apoptosis. A pharmacokinetic study of Orlistat (155 mg/kg) administered by i.p. injection showed the peak blood level of Orlistat (~10 μM) achieved 2 hrs after dosing. After 2hrs, the blood level of Orlistat decreased rapidly.

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.

Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats.

References:
[1]. Zhi J, et al. Review of limited systemic absorption of orlistat, a lipase inhibitor, in healthy human volunteers. J Clin Pharmacol. 1995 Nov;35(11):1103-8.
[2]. Zhang E, et al. Glycycoumarin Sensitizes Liver Cancer Cells to ABT-737 by Targeting De Novo Lipogenesis and TOPK-Survivin Axis. Nutrients. 2018 Mar 15;10(3). pii: E353.
[3]. Padwal R, et al. Long-term pharmacotherapy for obesity and overweight. Cochrane Database Syst Rev. 2004;(3):CD004094.