ABSTRACT
Background OC26 and its pro-drug BOC26P, both ortho-aryl chalcone compounds, showed a well-definedantitumor activity in various cancer cells especially in drug-resistant tumor cell lines.Aim The purpose of this study was to investigate the bile excretion characteristics of OC26 after OC26 and BOC26Padministered in rats respectively.Method An ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) method wasdeveloped and validated for OC26 in rat bile. Liquid-liquid extraction with ethyl acetate method was use to pretreatthe bile samples. After that, a gradient mobile phase at a flow rate 0.5mL/min of acetonitrile and 2mM CH3COONH4with 0.1% aqueous ammonia solution (v/v) and the positive ion alternate mode separated and quantified OC26.Bile samples were collected from rats after intravenous injection (i.v) 12.5mg/kg of OC26 and BOC26P, respectively.Results For method validation, the method showed high extraction recovery. The assay showed a good linearitywith correlation coefficient >0.99 at the concentration ranges of 20-2000ng/mL. All data were within the requiredlimits. The bile excretion results showed that the excretion amount of OC26 was gradually stabilized after 2h. Theaccumulative excretion percentage of OC26 after i.v 12.5mg/kg BOC26P was significantly higher than that of OC26after i.v 12.5mg/kg OC26. Significant gender differences were also observed in bile excretion of OC26.Conclusion This method was selective, sensitive and reliable and successfully applied to the bile excretion of OC26.This study provided theoretical basis for OC26 further research.