Division of Cancer Pathophysiology, National Cancer Center Research Institute, 1-1, Tsukiji 5-chome, Chuo-ku, Tokyo 104-0045, Japan.
Curr Pharm Des. 2012;18(31):4839-53. doi: 10.2174/138161212803216924.
Traditional Japanese herbal, or Kampo medicine was developed and modified from Chinese herbal medicine. After the Japanese government approved Kampo for clinical use, much attention has been paid to establishing scientific evidence for the effectiveness of these medicines. Recent progress has been made in elucidating the mechanisms of action of some types of Kampo medicine, including rikkunshito (RKT), daikenchuto, and yokukansan. In this review, we focused on identifying the target molecules and the active ingredients of RKT. Thus far, many target molecules have been implicated in the mechanism of action of Kampo medicines, such as ion channels, enzymes, and receptors. In particular, G protein-coupled receptors are attractive candidates for explaining herbal medicine activity. This is particularly true of RKT, which is composed of 8 independent, crude drug extracts. Recent reports have shown that RKT elicits its effects through dual action to the G protein-coupled receptors: inhibition of serotonergic 5-HT2C and 5-HT2B receptors and activation of ghrelin receptors via specific ingredients of RKT. In addition, we suggest that the identification of the effective ingredients from Kampo medicines could contribute to the discovery and development of new drugs by means of modern high-throughput drug screening technology.
传统的日本草药，或汉方药，是从中国草药发展和修改而来的。日本政府批准汉方用于临床后，人们非常关注为这些药物的有效性建立科学证据。最近在阐明某些类型的汉方药的作用机制方面取得了进展，包括六君子汤、大建中汤和优克方。在这篇综述中，我们重点关注确定六君子汤的靶分子和有效成分。到目前为止，许多靶分子已被牵涉到汉方药的作用机制中，如离子通道、酶和受体。特别是，G 蛋白偶联受体是解释草药活性的有吸引力的候选者。这对于由 8 种独立的粗药提取物组成的六君子汤尤其如此。最近的报告表明，六君子汤通过对 G 蛋白偶联受体的双重作用发挥作用：抑制血清素 5-HT2C 和 5-HT2B 受体，以及通过六君子汤的特定成分激活胃饥饿素受体。此外，我们建议从汉方药中鉴定有效成分可能有助于通过现代高通量药物筛选技术发现和开发新药。
