Ethnopharmacological relevance

In traditional Chinese Medicine, Rehmannia glutinosa (Gaertn.) DC., as the principle herb of ShengDiHuang Decotion (SDHD), has the effect of cooling blood and hemostasis, and tonifying the yin and kidney. Rheum L., as adjuvant herbs, assist Rehmannia glutinosa (Gaertn.) DC. to promote blood circulation to remove blood stasis.

Aim of study

To study the mechanism of Rhein (RH) involved in the promotion of Rehmannioside D (RD) absorption by pharmacokinetic studies, single-pass intestinal perfusion, Caco-2 cell models, molecular docking technique and western blotting.

Materials and methods

Initially, the intestinal absorption of RD in the presence or absence of RH was conducted through pharmacokinetic studies. Thereafter, the intestinal absorption of RD and RH was studied using the single-pass intestinal perfusion and Caco-2 cell models. Finally, using molecular docking technique and western blotting.

Results

We found that the promotion of RD absorption by RH was mediated by breast cancer resistance and multidrug resistance-associated protein 2, thereby affecting the permeability of the intestinal epithelium. Additionally, RH and RD can competitively bind to breast cancer resistance and multidrug resistance-associated protein 2, and that RH inhibits the expression of breast cancer resistance and multidrug resistance-associated protein 2 in the ileum to promote the intestinal absorption of RD.

Conclusion

This study reveals the mechanisms associated with the RH-mediated promotion of RD absorption and provides a basis for further exploring the synergistic effect of Rehmannia glutinosa (Gaertn.) DC and rhubarb.

中文翻译：

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大黄酸对 rehmaionoside D 吸收的影响：体内、原位、体外和计算机模拟研究

民族药理学相关性

在中医中，地黄为生地黄汤的主药，具有凉血止血、补阴补肾的功效。Rheum L.，作为佐药草药，辅助 Rehmannia glutinosa (Gaertn.) DC。活血化瘀。

学习目的

通过药代动力学研究、单次肠道灌注、Caco-2 细胞模型、分子对接技术和蛋白质印迹研究大黄酸 (RH) 参与促进地黄苷 D (RD) 吸收的机制。

材料和方法

最初，通过药代动力学研究进行了在存在或不存在 RH 的情况下 RD 的肠道吸收。此后，使用单次肠道灌注和 Caco-2 细胞模型研究了 RD 和 RH 的肠道吸收。最后，使用分子对接技术和western blotting。

结果

我们发现 RH 促进 RD 吸收是由乳腺癌耐药和多药耐药相关蛋白 2 介导的，从而影响肠上皮细胞的通透性。此外，RH与RD可竞争性结合乳腺癌耐药及多药耐药相关蛋白2，RH通过抑制回肠中乳腺癌耐药及多药耐药相关蛋白2的表达，促进RD的肠道吸收。

结论

该研究揭示了与 RH 介导的促进 RD 吸收相关的机制，并为进一步探索地黄 (Gaertn.) DC 和大黄的协同作用提供了基础。