Department of Biomedical Engineering and Environmental Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan.
J Ethnopharmacol. 2010 Feb 3;127(2):292-8. doi: 10.1016/j.jep.2009.11.006. Epub 2009 Nov 10.
San-Huang-Xie-Xin-Tang (SHXXT), an important Chinese medicine formula, contains Rhei Rhizoma (RR), Scutellariae Radix (SR) and Coptidis Rhizoma (CR). RR and SR are abundant in anthraquinone and flavonoid polyphenols. Pharmacokinetic study of SHXXT indicated that glucuronides were the predominant forms of polyphenols in rats.
As an extension of pharmacokinetic study, the serum metabolites of SHXXT, RR, SR and CR were prepared from rats and quantitated, then the immunomodulation effects were examined by culturing these serum metabolites with murine and human immune cells.
The results indicated that the inhibitions on nitric oxide (NO) and cytokine production from mitogen-activated peritoneal macrophages by the serum metabolites of SHXXT, RR, SR and CR were through reducing the protein expression of inducible NO synthase (iNOS) and the IC(50) were 0.8%, 1.5%, 3.0% and 0.8% of their blood concentrations, respectively. In addition, the serum metabolites of SHXXT, RR, SR and CR significantly decreased the ratios of interferon-gamma (IFN-gamma) to interleukin (IL)-4 in mitogen-stimulated mice spleen cells and human peripheral blood mononuclear cells (PBMCs). Moreover, the serum metabolites of SHXXT and SR significantly arrested the mitogen-stimulated mice spleen cells at G2/M stage.
In conclusion, the serum metabolites of SHXXT and the component herbs exerted promising modulation activities on the immune functions and the cell cycle distribution of mice and human immune cells. We suggest that SHXXT is a promising remedy for immunomodulation through Th1/Th2 regulation.
三黄泻心汤（SHXXT）是一种重要的中药方剂，由大黄、黄芩和黄连三味中药组成。大黄和黄芩富含蒽醌和类黄酮多酚。SHXXT 的药代动力学研究表明，葡萄糖醛酸苷是多酚在大鼠体内的主要形式。
作为药代动力学研究的延伸，从大鼠中制备 SHXXT、大黄、黄芩和黄连的血清代谢物，并进行定量分析，然后通过培养这些血清代谢物与鼠和人免疫细胞来检测其免疫调节作用。
结果表明，SHXXT、大黄、黄芩和黄连的血清代谢物通过降低诱导型一氧化氮合酶（iNOS）的蛋白表达来抑制有丝分裂原激活的腹腔巨噬细胞产生一氧化氮（NO）和细胞因子，其 IC50 分别为其血液浓度的 0.8%、1.5%、3.0%和 0.8%。此外，SHXXT、大黄、黄芩和黄连的血清代谢物显著降低了有丝分裂原刺激的小鼠脾细胞和人外周血单个核细胞（PBMCs）中干扰素-γ（IFN-γ）与白细胞介素（IL）-4 的比值。此外，SHXXT 和黄芩的血清代谢物显著阻止了有丝分裂原刺激的小鼠脾细胞进入 G2/M 期。
综上所述，SHXXT 的血清代谢物和成分草药对小鼠和人免疫细胞的免疫功能和细胞周期分布具有显著的调节作用。我们认为，SHXXT 通过 Th1/Th2 调节具有免疫调节的潜力。
