Second Affiliated Clinical college, Guangzhou University of Traditional Chinese Medicine, No. 111, Dade Road, Guangzhou 510120, China.
J Ethnopharmacol. 2009 Dec 10;126(3):415-20. doi: 10.1016/j.jep.2009.09.023. Epub 2009 Sep 23.
Site-direct delivery is a desirable and elusive goal. In Traditional Chinese Medicine, this goal is usually met by coadministration with a kind of meridian guide drug (MGD). Vinegar-baked Radix Bupleuri (VBRB) is usually used to focus other drugs pharmacological effect on liver in Traditional Chinese Medicine (TCM). However, the scientific data for this effect are not available. In this paper, the liver targeting enhancing effect of VBRB on resveratrol was investigated.
Mice, 144, were divided into four groups by random, resveratrol group as control and resveratrol coadministered with three different doses of VBRB peroral. Concentrations of resveratrol in different tissues were determined by HPLC and the target efficiency was evaluated by relative uptake efficiency (RUE) and relative targeting efficiency (RTE).
Compared to the control group, medium dose VBRB enhanced the targeting efficiency of resveratrol significantly, and the RUE and RTE were 1.79 and 46.9%, respectively. Meanwhile, it considerably reduced the distribution of resveratrol in lung and blood, the RUE and RTE in blood were 1.1, -22.6%, and were 0.88, -55.0% in lung, respectively. VBRB reduced the Cmax of resveratrol in almost all the tissues except for liver, heart and kidney, with the extent in the range of 26-61%. In addition, VBRB prolonged the retention time of resveratrol in liver, and shortened the retention time in other tissues.
VBRB could enhance the distribution of resveratrol in liver, and reduce the distribution in other tissues, implying that VBRB might be a potential drug for achieving target therapy.
靶向递药是一个理想但难以实现的目标。在传统中医中，通常通过联合使用一种经络导向药物（MGD）来实现这一目标。醋制柴胡（VBRB）通常用于将其他药物的药理作用集中在肝脏上。然而，目前尚缺乏关于这种作用的科学数据。本文旨在研究 VBRB 对白藜芦醇的肝靶向增强作用。
将 144 只小鼠随机分为四组，分别为白藜芦醇组（对照组）和白藜芦醇联合三种不同剂量口服 VBRB 组。采用 HPLC 法测定不同组织中白藜芦醇的浓度，通过相对摄取效率（RUE）和相对靶向效率（RTE）评价其靶向效率。
与对照组相比，中剂量 VBRB 能显著增强白藜芦醇的靶向效率，RUE 和 RTE 分别为 1.79 和 46.9%。同时，VBRB 显著减少了白藜芦醇在肺和血液中的分布，RUE 和 RTE 在血液中的值分别为 1.1 和-22.6%，在肺中的值分别为 0.88 和-55.0%。VBRB 降低了除肝脏、心脏和肾脏以外几乎所有组织中白藜芦醇的 Cmax，降低幅度在 26-61%之间。此外，VBRB 延长了白藜芦醇在肝脏中的保留时间，缩短了其在其他组织中的保留时间。
VBRB 可增强白藜芦醇在肝脏中的分布，减少在其他组织中的分布，提示 VBRB 可能是实现靶向治疗的潜在药物。
