论文部分内容阅读
目的合成新型川芎嗪衍生物并对其抗癌活性和毒性进行评价。方法以中医经典方药中抗癌活性成分为原料,利用拼合原理,设计、合成川芎嗪衍生物,并采用四甲基偶氮唑蓝(MTT)法体外检测川芎嗪衍生物对Hela(人宫颈癌)细胞模型的抗癌活性和对正常细胞MDCK(犬肾上皮细胞)的毒性。结果获得4个未见报道的川芎嗪类新化合物,均经光谱方法鉴定了结构,其中化合物10和12能明显抑制Hela细胞的增殖,抗癌活性显著高于其合成前体;且对MDCK细胞的毒性明显小于顺铂。结论该结果进一步验证以拼合原理为指导,从经典方药中发现新型低毒抗癌先导化合物的研究思路是可行的。
Objective To synthesize a novel ligustrazine derivative and evaluate its anti-cancer activity and toxicity. Methods The antitumor active ingredients in traditional Chinese medicine prescription were used as raw materials. The tetramethylpyrazine derivatives were designed and synthesized by using the principle of splitting. The effects of ligustrazine derivatives on Hela (human cervical cancer ) Cell model and the toxicity to normal cells MDCK (canine kidney epithelial cells). Results Four novel tetramethylpyrazine compounds were obtained and their structures were identified by spectroscopic methods. Compounds 10 and 12 inhibited the proliferation of Hela cells significantly, and their antitumor activity was significantly higher than that of the synthetic precursors. The toxicity was significantly less than cisplatin. Conclusion This result is further verified by the combination principle as a guideline. It is feasible to find a new research idea of a novel lead compound with low toxicity and anticancer activity from classical prescription drugs.