Institute of Materia Medica, Zhejiang Chinese Medical University, Hangzhou 310053, China.
J Ethnopharmacol. 2011 Sep 1;137(1):449-56. doi: 10.1016/j.jep.2011.05.049. Epub 2011 Jun 6.
Polygonum multiflorum is an important traditional Chinese medicine used for health promotion and disease treatment. One major bioactive compound in P. multiflorum is a stilbene glycoside (2,3,5,4'-tetrahydroxystilbene-2-O-β-d-glucoside, PM-SG), which possesses antioxidative, anti-inflammatory and endothelial-protective activities.
The purpose of the present study was to investigate in vivo pharmacokinetics and tissue distribution of PM-SG after oral administration of Polygonum multiflorum extract to rats by using a reversed-phase high-performance liquid chromatography coupled with liquid-liquid phase extraction. The pharmacokinetic parameters were determined using both compartmental and non-compartmental analyses.
All calibration curves for PM-SG in rat plasma and tissues were linear (all r(2)>0.99) over the range of 0.27-185.00 μg/ml. The intra- and inter-day variations were less than 3% at concentration range of 8.7-131.2 μg/ml and good overall recoveries (97.7-101.5%) were obtained at the same range. The maximum concentration (C(max)) and the time to reach this concentration (T(max)) of PM-SG were 31.9 μg/ml and 40.0 min, respectively. The pharmacokinetic profiles estimated by fitting two-compartment and non-compartment models revealed that PM-SG was rapidly absorbed into the body fluids and widely distributed throughout the body, with great efficiency of utility, followed by quick elimination. The highest PM-SG levels were detected in liver and lungs (90.3 ± 20.8 μg/g and 86.8 ± 9.0 μg/g, respectively) whereas little in brain and testes, indicating PM-SG can hardly penetrate the blood-brain and blood-testicle barriers.
This was the first report on the favorable pharmacokinetic profiles of PM-SG in rat plasma and tissues after oral administration. It may provide a meaningful basis for clinical application of such a bioactive compound of herbal medicines.
何首乌是一种重要的传统中药，用于促进健康和治疗疾病。何首乌中的一种主要生物活性化合物是一种二苯乙烯苷（2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷，PM-SG），具有抗氧化、抗炎和内皮保护作用。
本研究旨在通过反相高效液相色谱法结合液-液萃取法，研究口服何首乌提取物后 PM-SG 在大鼠体内的药代动力学和组织分布。采用房室模型和非房室模型分析方法确定药代动力学参数。
PM-SG 在大鼠血浆和组织中的所有校准曲线均呈线性（r²均>0.99），范围为 0.27-185.00 μg/ml。在 8.7-131.2 μg/ml 的浓度范围内，日内和日间变化均小于 3%，在相同范围内获得了良好的总回收率（97.7-101.5%）。PM-SG 的最大浓度（C(max)）和达到此浓度的时间（T(max)）分别为 31.9 μg/ml 和 40.0 min。通过拟合两室和非房室模型估计的药代动力学曲线表明，PM-SG 被迅速吸收到体液中并广泛分布于全身，具有很高的利用效率，随后迅速消除。PM-SG 水平最高的器官是肝脏和肺部（分别为 90.3±20.8 μg/g 和 86.8±9.0 μg/g），而在脑和睾丸中含量较低，表明 PM-SG 很难穿透血脑和血睾屏障。
这是口服 PM-SG 在大鼠血浆和组织中良好药代动力学特征的首次报道。这可能为草药中此类生物活性化合物的临床应用提供有意义的基础。
