State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang 550004, PR China; School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550004, PR China.
School of Pharmaceutical Sciences, Guizhou Medical University, Guiyang 550004, PR China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Nov 1;1248:124356. doi: 10.1016/j.jchromb.2024.124356. Epub 2024 Oct 30.
Biancaea decapetala (Roth) O.Deg. (Fabaceae), traditionally utilized by the Hmong for treating rheumatoid arthritis (RA), has its pharmacokinetic behavior under disease conditions largely unexplored. In view of this, a UPLC-MS/MS method was established for the determination of protosappanin B (PTB), protosappanin B-3-O-β-D-glucoside (PTD), and 3-deoxysappanchalcone (3-DSC), key bioactive components of the herb, in rat plasma and RAW264.7 cells to explore the effect of disease state on the pharmacokinetic profiles changes of these three components in vitro and in vivo. These components were detected using multiple reaction monitoring (MRM) process in positive and negative mode. Each calibration curve had a high R value of > 0.99. The intra- and inter-day precisions of PTD, PTB, 3-DSC were all < 15 %, and accuracy ranged from 85 % to 115 %. The RSD values pertaining to stability, recovery, matrix effect, and stability remained below 15.0 %. It was successfully applied for the investigation of the pharmacokinetics of these three components in rat plasma and RAW264.7 cells after administration of Biancaea decapetala extracts (BDE). In rat pharmacokinetic experiments, significant differences were observed in the AUC, MRT, and Cl/F values of PTD, PTB, 3-DSC between adjuvant-induced arthritis (AA) and normal rats. In cellular pharmacokinetic experiments, comparison with the normal group revealed increased AUC and MRT for these three components in the LPS-induced inflammatory cell model, along with decreased Cl/F, which was consistent with in vivo experimental outcomes. These findings suggest an increased absorption rate and a decreased elimination rate of the three components of BDE in AA rats and inflammatory cells, indicating a potential alteration in the rate and extent of drug metabolism. This study provided a theoretical reference for further clarification of its pharmacodynamic basis.
山蚂蝗（Biancaea decapetala）（豆科），被苗族传统用于治疗类风湿关节炎（RA），但其在疾病状态下的药代动力学行为尚未得到充分研究。有鉴于此，本研究建立了 UPLC-MS/MS 法，用于测定该草药中关键生物活性成分原山芝麻素 B（PTB）、原山芝麻素 B-3-O-β-D-葡萄糖苷（PTD）和 3-去氧山芝麻素（3-DSC）在大鼠血浆和 RAW264.7 细胞中的含量，以探讨疾病状态对这三种成分在体外和体内药代动力学特征变化的影响。采用正、负离子多反应监测（MRM）模式检测这三种成分。每个校准曲线的 R 值均>0.99。PTD、PTB 和 3-DSC 的日内和日间精密度均<15%，准确度在 85%-115%之间。稳定性、回收率、基质效应和稳定性的 RSD 值均<15.0%。该方法成功应用于测定山蚂蝗提取物（BDE）给药后大鼠血浆和 RAW264.7 细胞中这三种成分的药代动力学。在大鼠药代动力学实验中，与正常大鼠相比，关节炎大鼠中 PTD、PTB 和 3-DSC 的 AUC、MRT 和 Cl/F 值均有显著差异。在细胞药代动力学实验中，与正常组相比，LPS 诱导的炎症细胞模型中这三种成分的 AUC 和 MRT 增加，Cl/F 降低，与体内实验结果一致。这些发现表明，AA 大鼠和炎症细胞中 BDE 的三种成分吸收速率增加，消除速率降低，提示药物代谢的速率和程度可能发生变化。本研究为进一步阐明其药效学基础提供了理论参考。
