Abstract

We previously reported that Dai-saiko-to (Da-Chai-Hu-Tang), a traditional Japanese kampo medicine, increased LDL receptor mRNA expression in the liver of the hypercholesterolemic rabbits. In this study, we focused on LDL receptor gene expression in a human hepatoma cell line (HepG2) treated with Dai-saiko-to extract and the extracts of eight herbs presented in Dai-saiko-to. Dai-saiko-to extract significantly increased LDL receptor gene and SREBP2 gene expression compared with the control. The extracts of four herbs, Bupleurum root, Pinellia tuber, Scutellaria root and Peony root significantly increased the LDL receptor gene expression. Whereas, Jujube, Immature orange, Ginger and Rhubarb extracts did not change the gene expression. These results suggest that Dai-saiko-to increased the expression of the cholesterol transport gene (LDL receptor) regulated by SREBP2 gene in the human hepatoma cell line. The pharmacological activity of Dai-saiko-to against hypercholesterolemia and atheromatous lesions related for these four herbal components.

Highlights

  • It is well known that hypercholesterolemia is a major risk factor for coronary heart disease [1,2]

  • We previously reported that Dai-saiko-to (Da-Chai-Hu-Tang), a traditional Japanese kampo medicine, increased low density lipoprotein (LDL) receptor mRNA expression in the liver of the hypercholesterolemic rabbits

  • We focused on LDL receptor gene expression in a human hepatoma cell line (HepG2) treated with Dai-saiko-to extract and the extracts of eight herbs presented in Dai-saiko-to

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Summary

Introduction

It is well known that hypercholesterolemia is a major risk factor for coronary heart disease [1,2]. Several kinds of drugs are used to improve the plasma lipid levels of patients with hypercholesterolemia [3,4,5,6]. Dai-saiko-to (Da-Chai-Hu-Tang) is used clinically to alleviate hypertension, cholestasis, and various causes of liver dysfunction. We previously reported that Dai-saikoto inhibited the progression of atherosclerotic lesions in heritable hyperlipidemic model rabbits (KHC rabbits) [8,9,10]. Plasma lipid levels were decreased and low density lipoprotein (LDL) receptor mRNA expression in the liver was increased in the Dai-saiko-to treated KHC rabbits. We demonstrated that the antiatherosclerotic effects of Dai-saiko-to arise from many factors, including antioxidation and relation to gene expression. Our results demonstrate that Dai-saiko-to provides a combination of beneficial thera-

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