Jo Jun Hyeon, Kim Ju-Hyun, Lee Hye Suk, Jeong Gil-Saeng, Lee Jae-Mok, Lee Sangkyu
BK21 Plus KNU Multi-Omics based Creative Drug Research Team, College of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Republic of Korea.
College of Pharmacy, The Catholic University of Korea, 43 Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do 14662, Republic of Korea.
Fitoterapia. 2017 Jul;120:194-198. doi: 10.1016/j.fitote.2017.06.007. Epub 2017 Jun 8.
Bakuchicin is a furanocoumarin isolated from the seeds of Psoralea corylifolia, which is used in oriental medicine. However, limited information on the pharmacokinetics of bakuchicin is available and in addition, no determined method has been devised to quantify bakuchicin levels in the plasma. In the present study, we developed and validated a quantification method using liquid chromatography (LC) coupled with tandem mass spectrometry (LC-MS/MS), which was applied to a pharmacokinetic investigation in mouse plasma. LC was performed using an ACE 5 C18 column, and a mixture of acetonitrile and water containing 0.1% formic acid was used as the mobile phase at a flow rate of 220μL/min. Bakuchicin transition ions in multiple reaction-monitoring modes using positive ionization were observed at m/z 187.0 to m/z 131.0. Bakuchicin and the internal standard (reserpine) had retention times of 4.5 and 4.3min, respectively. Acceptable linearity (r=0.996) was observed over the concentration range of 20-1000ng/mL, with a lower quantification limit of 20ng/mL in mouse plasma. This method was successfully applied to determine the pharmacokinetic parameters of bakuchicin in mouse plasma and showed that the bioavailability of bakuchicin was 58.3% at 5mg/kg oral administration.
补骨脂素是一种从补骨脂种子中分离出的呋喃香豆素，用于传统东方医学。然而，关于补骨脂素的药代动力学信息有限，此外，尚未设计出测定血浆中补骨脂素水平的方法。在本研究中，我们开发并验证了一种使用液相色谱（LC）与串联质谱（LC-MS/MS）联用的定量方法，并将其应用于小鼠血浆的药代动力学研究。使用ACE 5 C18柱进行液相色谱分析，以含0.1%甲酸的乙腈和水的混合物作为流动相，流速为220μL/min。在正离子模式下的多反应监测模式中观察到补骨脂素的跃迁离子，质荷比为m/z 187.0至m/z 131.0。补骨脂素和内标（利血平）的保留时间分别为4.5和4.3分钟。在20 - 1000ng/mL的浓度范围内观察到良好的线性关系（r = 0.996），小鼠血浆中的定量下限为20ng/mL。该方法成功应用于测定小鼠血浆中补骨脂素的药代动力学参数，结果表明，口服给药5mg/kg时补骨脂素的生物利用度为58.3%。
