食品科学 ›› 2013, Vol. 34 ›› Issue (11): 45-48.doi: 10.7506/spkx1002-6630-201311011

• 基础研究 • 上一篇    下一篇

人参皂苷Rg3的脂肪酸衍生物的合成及其体外抗肿瘤活性

叶 慧1,2,张 兵1,2,蒋海伟1,2,程文娟1,2,邓泽元1,2,胡蒋宁1,2,*   

  1. 1.南昌大学 食品科学与技术国家重点实验室,江西 南昌 330047;
    2.南昌大学生命科学与食品工程学院,江西 南昌 330031
  • 收稿日期:2013-01-07 修回日期:2013-05-09 出版日期:2013-06-15 发布日期:2013-06-03
  • 通讯作者: 胡蒋宁 E-mail:yh881018106@yahoo.com.cn
  • 基金资助:

    中国博士后第四批特别资助项目(201104590);中国博士后基金第47批面上资助项目(20100471424);
    全国高校博士点基金项目(20103601120004)

Synthesis and in vitro Anti-tumor Activity of Fatty Acid Derivatives of Ginsenoside Rg3

YE Hui1,2,ZHANG Bing1,2,JIANG Hai-wei1,2,CHENG Wen-juan1,2,DENG Ze-yuan1,2,HU Jiang-ning1,2,*   

  1. 1. State Key Laboratory of Food Science and Engineering, Nanchang University, Nanchang 330047, China;
    2. College of Life Science and Food Engineering, Nanchang University, Nanchang 330031, China
  • Received:2013-01-07 Revised:2013-05-09 Online:2013-06-15 Published:2013-06-03
  • Contact: HU Jiang-ning E-mail:yh881018106@yahoo.com.cn

摘要:

以人参皂苷Rg3和棕榈酸酰氯为反应原料,二氯甲烷为溶剂,K2CO3为缚酸剂,在40℃条件下加热搅拌6h合成人参皂苷Rg3衍生物,经硅胶柱柱层析纯化后得到一种新的人参皂苷衍生物,并利用紫外、红外色谱、高效液质联用、核磁共振等方法鉴定其结构。用MTT法检测该衍生物对人乳腺癌细胞株MCF-7的生长抑制作用。结果表明:从10~100μg/mL质量浓度范围内,药物作用时间越长,质量浓度越大抑制率越高。药物作用24、48、72h的IC50 值分别为146.68、122.39、101.95μg/mL。提示人参皂苷Rg3衍生物是一种较有潜力的药物原料。

关键词: 人参皂苷Rg3, 棕榈酸酰氯, 人乳腺癌细胞株

Abstract:

The aim of this study was to synthesize fatty acid derivatives from ginsenoside Rg3. Esterified compounds were
prepared from the reaction of ginsenoside Rg3 and palmitoyl chloride with methylene dichloride as solvent and potassium
carbonate as acid-binding agent by stiring the mixture at 40 ℃ for 6 h. In addition, one major product was obtained by silica
gel column chromatography and its structure was characterized by UV, IR, HPLC/QTOF-MS and NMR. MTT method was
used to evaluate the mortality rate of MCF-7 cells after incubation with the product at different concentrations. The results
indicated that the proliferation of MCF-7 cells was inhibited by the derivative of gensinoside Rg3 in a dose- and timedependent
manner in the concentration range of 10-100 μg/mL. After incubation for 24, 48 h and 72 h, the IC50 was 146.68,
122.39 μg/mL and 101.95 μg/mL, respectively. These results suggest that this derivatized gensinoside Rg3 is a potential raw
material for pharmaceuticals.

Key words: ginsenoside Rg3, palmitoyl chloride, human breast cell lines

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