The Pharmaceutical Laboratory, Guangdong Provincial Hospital of Traditional Chinese Medicine, No. 111, Dade Road, Guangzhou, China.
J Ethnopharmacol. 2010 Nov 11;132(2):421-8. doi: 10.1016/j.jep.2010.08.021. Epub 2010 Aug 20.
Vinegar-baked Radix Bupleuri (VBRB) is usually used to focus other drugs effect on liver in traditional Chinese medicine (TCM). However, no sufficient scientific data are available to support this concept. In this paper, the liver targeting enhancing effect of VBRB on rhein was investigated. 432 of rats were divided into two large groups according to the dose of rhein, low dose group of rhein (LDGR) and high dose group of rhein (HDGR). In each group, the rats were further divided into four subgroups, rhein control and rhein co-administered with three different doses of VBRB peroral. Concentrations of rhein and its metabolite in different tissues were determined by HPLC. Compared to the control group, VBRB significantly increased the distribution of both rhein and its metabolite in liver and meanwhile decreased their distribution in other tissues, indicating a strong liver targeting enhancing effect. This liver targeting effect of VBRB depended on the dose of VBRB and rhein. Low and high dose of VBRB had a more strong effect than medium dose in HDGR; high dose of rhein was more sensitive than low dose of rhein (P<0.05). Rhein existed in two forms after peroral administration in vivo. It was found that the liver targeting effect of VBRB was more remarkable with the native form of rhein compared to its derivative form. The results of this paper demonstrated that co-administration with VBRB is a simple and efficiencient method for liver targeting therapy, and the meridine guide theory of TCM was credible.
醋炙柴胡通常用于增强中药方剂中其他药物对肝脏的作用。然而，目前没有足够的科学数据支持这一概念。本文研究了醋炙柴胡对大黄酸肝靶向增强作用。将 432 只大鼠按大黄酸剂量分为两组，低剂量大黄酸组（LDGR）和高剂量大黄酸组（HDGR）。每组大鼠进一步分为 4 个亚组，大黄酸对照组和大黄酸分别与 3 种不同剂量的醋炙柴胡口服共给药。采用 HPLC 法测定不同组织中大黄酸及其代谢物的浓度。与对照组相比，醋炙柴胡显著增加了大黄酸及其代谢物在肝脏中的分布，同时减少了其在其他组织中的分布，表明具有很强的肝靶向增强作用。醋炙柴胡的这种肝靶向作用取决于醋炙柴胡和大黄酸的剂量。HDGR 中低剂量和高剂量的醋炙柴胡比中剂量的效果更强；高剂量的大黄酸比低剂量的大黄酸更敏感（P<0.05）。体内口服后，大黄酸存在两种形式。研究发现，与大黄酸的衍生物形式相比，醋炙柴胡对其原型的肝靶向作用更为显著。本文结果表明，醋炙柴胡与药物共给药是一种简单有效的肝靶向治疗方法，中医的“归经”理论是可信的。
