Ethnopharmacological relevance

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.

Materials and methods

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.

Results

All calibration curves for PM-SG in rat plasma and tissues were linear (all r² > 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.

Conclusions

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.

中文翻译：

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中药何首乌2,3,5,4'-四羟基sti-2- O - β -d-葡萄糖苷在大鼠口服后的药代动力学和组织分布

民族药理学意义

何首乌是促进健康和治疗疾病的重要中药。何首乌中的一种主要生物活性化合物是二糖苷（2,3,5,4'-四羟基sti-2- O - β - d-葡萄糖苷，PM -SG），具有抗氧化，抗炎和保护内皮的作用活动。

材料和方法

本研究的目的是通过反相高效液相色谱结合液相-液相萃取法研究何首乌提取物口服给药后对大鼠PM- SG的体内药代动力学和组织分布。使用隔室和非隔室分析来确定药代动力学参数。

结果

大鼠血浆和组织中PM -SG的所有校准曲线在 0.27–185.00μg/ ml范围内均为线性（所有r ² > 0.99）。在8.7–131.2μg/ ml的浓度范围内，日内和日间变化小于3％，并且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）和达到该浓度的时间（T _max）分别为31.9μg/ ml和40.0 min。通过拟合两室和非室模型估计的药代动力学特征表明，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。在肝和肺中检测到最高的PM -SG水平（分别为90.3±20.8μg/ g和86.8±9.0μg/ g），而在脑和睾丸中则很少，这表明PM -SG几乎不能穿透血脑和血液。睾丸屏障。

结论

这是关于口服后大鼠血浆和组织中PM -SG有利药代动力学特征的首次报道。它可以为这种草药生物活性化合物的临床应用提供有意义的基础。