Lupeol, a phytosterol and triterpene, is widely found in edible fruits and vegetables, and has been reported to exhibit a spectrum of pharmacological activities against various disease conditions. In the present study, a derivative generated by the reaction of lupeol with p‐toluenesulfonyl isocyanate was ionizable and fragmentable in the negative mode by electrospray ionization/tandem mass spectrometry. Based on this simple chemical derivatization, a liquid chromatography–electrospray ionization/tandem mass spectrometry method was developed and validated for the quantification of lupeol in rat plasma. The calibration curves were linear (r² > 0.999) over concentrations from 2.5 to 250 ng/ml for lupeol. The method had an accuracy of 96.0–109.4%, and the intra‐ and inter‐day precisions (RSD) were within ± 15%. The stability data showed that no significant degradation occurred under the experimental conditions. The mean recoveries at three quality control levels were within 88.7–95.7%. No significant matrix effects (105.3–109.8%) were observed in rat plasma. This method was successfully applied to the pharmacokinetic study of lupeol in rat plasma after oral administration.

中文翻译：

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LC-ESI / MS / MS方法通过柱前衍生化测定鲁皮酚及其在大鼠血浆药代动力学研究中的应用

羽扇豆酚，一种植物甾醇和三萜烯，广泛存在于可食用的水果和蔬菜中，据报道对各种疾病状况显示出一系列药理活性。在本研究中，通过电喷雾电离/串联质谱，卢贝醇与对甲苯磺酰基异氰酸酯反应生成的衍生物可被电离并在负模态下断裂。在此简单的化学衍生化的基础上，开发了一种液相色谱-电喷雾电离/串联质谱分析方法，并已用于定量大鼠血浆中的羽扇豆酚。校准曲线是线性的（r ²≥0.999）的羽扇豆酚浓度范围从2.5到250 ng / ml。该方法的准确度为96.0–109.4％，日内和日间精度（RSD）在±15％以内。稳定性数据表明在实验条件下没有发生明显的降解。三个质量控制水平的平均回收率在88.7–95.7％之内。在大鼠血浆中未观察到明显的基质效应（105.3–109.8％）。该方法成功地应用于口服后卢佩醇在大鼠血浆中的药代动力学研究。