α-生育酚琥珀酸酯的合成及抑制肿瘤作用  

Synthesis of α-tocopherol succinate and study on its function form in inhibiting SGC-7901 cell growth

作　　者：李红卫[1] 赵岚[1] 吴坤[1] 

机构地区：[1]哈尔滨医科大学公共卫生学院营养与食品卫生教研室,哈尔滨150001

出　　处：《中国公共卫生》2005年第2期173-175,共3页Chinese Journal of Public Health

基　　金：黑龙江科技厅科技攻关项目 (GB0 1C1 0 5)

摘　　要：目的　合成α-生育酚琥珀酸酯 (α -Tocopherolsuccinate,α -TOS) ,验证其对人胃癌细胞SGC - 790 1的生长抑制作用 ,并研究其发挥作用的分子形式。方法　利用α -生育酚 (α -Tocopherol,α -TOH)和琥珀酸酐在催化剂的作用下合成α-TOS ,用噻唑蓝〔3- (4,5 -dimethyl-thiazol- 2 - y1 ) - 2 ,5 -diphenyltetrazoliumbromideMTT〕法观察其对SGC - 790 1细胞增殖的影响 ,应用琼脂糖凝胶电泳检测α -TOS对SGC - 790 1细胞凋亡的诱导作用 ,并利用高效液相色谱 (HighPerformanceLiquidChromatography ,HPLC)法检测α -TOS抑制癌细胞生长的作用形式。 结果　经红外光谱和质谱分析鉴定 ,本研究合成的α-TOS与标准品一致 ;与对照组相比 ,1 0和 2 0 μg/ml剂量组的α -TOS对SGC - 790 1细胞增殖的抑制作用明显 ,处理第 6d时 ,癌细胞的生存率分别降至 2 1 .7%和 7.7%;1 0和 2 0 μg/ml的α -TOS处理SGC - 790 1细胞 4 8h后 ,琼脂糖凝胶电泳检测到细胞发生凋亡时DNA降解形成梯形分子条带 ;在生长受到抑制的SGC - 790 1细胞及其培养体系中 ,利用HPLC法仅检测到α -TOS ,均未检测到其水解产物α -TOH。结论　α-TOS合成品对SGC - 790 1细胞具有明显剂量依赖的抑制增殖和诱导凋亡作用 ,且αObjective To synthesize α-tocopherol succinate(α-TOS);to examine its effect on the growth of human gastric carcinoma cell(SGC-7901) and to explore its molecular function form. Methods α-TOS was synthesized by reacting α-tocopherol(α-TOH) with succinic anhydrite in the presence of catalyst.Human gastric cancer SGC-7901 cell in vitro was used as the experimental cell,the inhibitory effect of α-TOS on the cell proliferation was investigated with 3-(4,5-dimethyl-thizazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method and its inducibility of cell apoptosis by DNA ladder.Identification of the molecular function form of α-TOS was accomplished by High Performance Liquid Chromatography (HPLC).Results The analytic result of the infrared spectrometry and mass spectrometry indicated the synthesis of α-TOS.Compared with the control group,α-TOS at 10 and 20?μg/ml had significatly inhibitory effect on the proliferation of SGC-7901 cells,whose survival rates were 21.7% and 7.7%,respectively,after 6-day treatment.The typical DNA ladders were observed in SGC-7901 cells after 48 administration of α-TOS at concentrations 10 and 20?μg/ml.α-TOS was detected in the cells and culture medium by HPLC,but its hydrolyzed object α-TOH was not found. Conclusion The synthesized α-TOS can inhibit the proliferation of SGC-7901 cells and induce the apoptosis of the cells in dose-dependent manner;α-TOS inhibit SGC-7901 cell growth by its intact form.

关 键 词：生育酚琥珀酸酯 合成 人胃癌细胞SGC-7901 

分 类 号：R730.5[医药卫生—肿瘤]