Chia Nan University of Pharmacy & Science Institutional Repository:Item 310902800/21555
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    標題: Role of Ginsenoside Rd in Inhibiting 26S Proteasome Activity
    作者: Tsui-Ling Chang
    Hsiou-Yu Ding
    Yi-Wen Kao
    丁秀玉
    貢獻者: 化粧品科技研究所
    關鍵字: Ginsenoside Rd
    MG 132
    Panax ginseng C.A. Meyer
    26S proteasome
    proteasome inhibitor
    日期: 2008-12
    上傳時間: 2009-07-20 09:53:24 (UTC+8)
    摘要: Drugs targeting 26S proteasome as antitumor agents are considered to be important for cancer therapy. Although the active components are yet to be identified, for more than 1000 years, the low-toxicity Panax ginseng has been used in traditional herbal medicine for either treating or preventing cancer. Ginsenosides Rb1, Rb2, Rc, Rd, Re, Rf, and Rg1 are distinct components that can be isolated from P. ginseng C.A. Meyer. In this study 26S proteasome was purified from pig red blood cells, and the activity of the seven isolated ginsenosides was analyzed by proteolysis assay. It was found that ginsenoside Rd inhibited 52.9% the chymotrypsin-like activity of 26S proteasome with an IC50 value of 107.5 μM when Suc-LLVY-AMC was used as a substrate. Ginsenoside Rd displayed a mixed type inhibition of 26S proteasome when analyzed by Lineweaver−Burk plots of the inhibition kinetics. Unlike ginsenoside Rd, the other ginsenosides showed low inhibitory effect of the chymotrypsin-like activity of 26S proteasome. Seven ginsenosides did not inhibit the trypsin-like and caspase-like activities of 26S when Ac-RLR-AMC or Z-LLE-AMC was used as substrate. These results suggest that ginsenoside Rd is a potential drug for cancer prevention due to its specific 26S proteasome inhibitory effect and known low toxicity. Furthermore, both 3-O-Glc2-Glc and 20-O-β-Glc positions of the ginsenoside may play a role in the inhibitory property of the chymotrypsin-like activity in 26S proteasome.
    關聯: Journal of agricultural and food chemistry56(24)：p.12011-12015
    显示于类别:[化妝品應用與管理系(所)] 期刊論文

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