刺五加提取物的化学成分及其对斑蝥素增效减毒作用的研究

Study of Chemical Constituents from Radix Acanthopanacis Senticosi Extraction for Injection and Their Synergism and Attenuation on Cantharidin

目的研究注射用刺五加提取物的化学成分及其对斑蝥素的增效减毒作用。方法制备注射用刺五加提取物，并利用反相半制备液相色谱、凝胶柱色谱对其化学成分进行分离纯化，利用其理化性质和波谱学分析鉴定它们的结构；采用MTT法考察刺五加提取物的化学成分与斑蝥素抑制肿瘤细胞的协同作用，并探讨此类化合物成分对斑蝥素抑制正常细胞的保护作用。结果鉴定出4个化合物，分别为刺五加皂苷B（1）、刺五加皂苷E（2）、4-（1，2，3-三羟基丙基）-2，6-二甲氧基苯-1-O—B—D-葡萄糖苷（3）、松柏苷（4）。MTT法检测显示，化合物1-3在-定浓度下与斑蝥素合用对肿瘤细胞的抑制率高于单药组，有明显的增效作用；同时化合物1～3在-定浓度下与斑蝥素合用能明显降低斑蝥素对正常细胞的细胞毒作用。结论4-（1，2，3-三羟基丙基）-2，6-二甲氧基苯-1-O—B—D-葡萄糖苷为首次发现，注射用刺五加提取物的化合物成分与斑蝥素联合使用能明显提高斑蝥素抗瘤作用及降低其毒副作用。

Objective To investigate the chemical constituents of Radix Acanthopanacis Senticosi extraction for injection and their efficacy-enhancing and toxicity-reducing effects on cantharidin. Methods The chemical constituents were isolated by chromatography on Sephadex LH-20 gel and Semi-preparation HPLC repeatedly, and their structures were elucidated by spectroscopic analysis （NMR and MS）. The efficacy-enhancing and toxicity-reducing effects of the compounds with cantharidin on tumor cells and normal cells were tested by MTT method. Results Four compounds were isolated, and their structure was identified as syringin（ 1 ）, elentheroside E（2）, 4-（1, 2, 3-trihydroxypropyl） -2, 6-dimethoxyphenyl-l-O- β -D-glucopyranoside （3）, and coniferin （4）. The MIT results showed that compounds 1-3 at some concentrations combined with cantharidin markedly inhibited the proliferation of tumor cells, and decreased the toxicity of cantharidin to normal cells. Conclusion Compound 3 has been obtained from Radix Acanthopanacis Senticosi for the first time. Some constituents of Radix Acanthopanacis Senticosi extraction for injection combined with cantharidin show an obvious effect on inhibiting tumor cell growth and decreasing toxicity of cantharidin to normal cells.