Institute of Wudang Traditional Chinese Medicine, Taihe Hospital, Hubei University of Medicine, 32 South Renmin Road, Shiyan, Hubei 442000, China.
College of Pharmacy, Hubei University of Medicine, 30 South Renmin Road, Shiyan, Hubei 442000, China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2018 Jun 1;1086:105-109. doi: 10.1016/j.jchromb.2018.04.012. Epub 2018 Apr 10.
Maoecrystal A (MC-A) is an ent-kaurane-type diterpene isolated from Rabdosia eriocalyx (Dunn) Hara. MC-A has been reported to show different types of pharmacological activities, including anticancer, anti-inflammatory and bacteriostatic functions. However, bioanalysis of MC-A has not been reported. The purpose of this study is to develop an UPLC-MS/MS method to quantify MC-A in plasma and determine its pharmacokinetic properties using an animal model. The separation was performed using a Waters HSS T3 column (50 mm × 2.1 mm, 1.8 μm, Waters Corp., Milford, MA, USA) with methanol and water containing 0.1% of formic acid as the mobile phases. The mass analysis was performed in a Waters Xevo TQ mass spectrometer using multiple reaction monitoring (MRM) in positive scan mode. Protein precipitation was used to extract the drug from rat plasma samples. The calibration curve is linear in the concentration range 0.49-2000.0 ng/mL. The extraction recovery and the matrix effect were 78.11 to 91.72% and 90.38 to 98.02%, respectively. The RSD of inter/intra-day precisions were <13.72% and the accuracy was >86.41%. Stability studies showed that MC-A was stable (RSD < 14.98%) at different conditions (i.e., short-term, long-term, bench, and three freeze-thaw cycles) in rat plasma. The method was successfully applied to a pharmacokinetic study using rats through oral and intravenous administration routes. The oral bioavailability of MC-A was only 2.9%. Further studies are needed to determine the absorption and metabolism in order to improve the oral bioavailability of MC-A.
毛萼晶 A（MC-A）是从 Rabdosia eriocalyx（Dunn）Hara 中分离得到的一种贝壳杉烷型二萜。MC-A 已被报道具有多种药理活性，包括抗癌、抗炎和抑菌作用。然而，尚未有关于 MC-A 的生物分析报道。本研究旨在建立一种 UPLC-MS/MS 方法，用于定量检测血浆中的 MC-A，并使用动物模型确定其药代动力学特性。分离采用 Waters HSS T3 柱（50mm×2.1mm，1.8μm，Waters Corp.，Milford，MA，USA），以甲醇和含 0.1%甲酸的水为流动相。质谱分析采用 Waters Xevo TQ 质谱仪，以正扫描模式进行多重反应监测（MRM）。采用蛋白沉淀法从大鼠血浆样品中提取药物。校准曲线在 0.49-2000.0ng/mL 浓度范围内呈线性。提取回收率和基质效应分别为 78.11%至 91.72%和 90.38%至 98.02%。日内和日间精密度的 RSD 均<13.72%，准确度均>86.41%。稳定性研究表明，MC-A 在大鼠血浆中的不同条件下（即短期、长期、台架和三个冻融循环）均稳定（RSD<14.98%）。该方法成功应用于大鼠通过口服和静脉给药途径的药代动力学研究。MC-A 的口服生物利用度仅为 2.9%。需要进一步研究以确定吸收和代谢情况，以提高 MC-A 的口服生物利用度。
