人参皂苷Rg3的脂肪酸衍生物的合成及其体外抗肿瘤活性

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

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。

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 time- dependent manner in the concentration range of 10-- 100 μg/mL. After incubation for 24, 48 h and 72 h, the ICs0 was 146.68, 122.39 μtg/mL and 101.95μg/mL, respectively. These results suggest that this derivatized gensinoside Rg3 is a potential raw material for pharmaceuticals.