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目的:研究新型姜黄素衍生物的合成及其体外抗癌活性。方法:以“十全大补丸”方中抗癌活性成分为原料,利用拼合原理,设计、合成姜黄素衍生物,并采用四甲基偶氮唑蓝(MTT)法体外检测姜黄素衍生物在HT-29(人结肠癌细胞)、Bel7402(人肝癌细胞)、HepG2(人肝癌细胞)、Hela(人宫颈癌细胞)4种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:发现化合物4和CU-T能明显抑制4种人源性癌细胞的增殖,二者体外抗癌活性(IC50)与顺铂相似,显著高于姜黄素;且对MDCK细胞的毒性明显小于顺铂。结论:以拼合原理为指导,进一步验证了从经典方药中发现高效、低毒的抗癌先导化合物的研究思路是可行的。
Objective: To study the synthesis of novel curcumin derivatives and their anticancer activity in vitro. Methods: The antitumor active ingredients of “Shiquan Dabu Pills” were used as raw materials. The curcumin derivatives were designed and synthesized by using the principle of splitting. Curcumin was detected by MTT method in vitro. The antitumor activity of the derivatives in four cancer cell models of HT-29 (human colon cancer cells), Bel 7402 (human hepatoma cells), HepG2 (human hepatoma cells) and Hela (human cervical cancer cells) Renal epithelial cells) toxicity. Results: It was found that compound 4 and CU-T could significantly inhibit the proliferation of 4 kinds of human cancer cells. The in vitro anticancer activity (IC50) was similar to that of cisplatin and was significantly higher than that of curcumin. The cytotoxicity to MDCK cells was significantly lower than that of curcumin Cisplatin. Conclusion: Based on the principle of “combination”, the research idea of the anti-cancer lead compound with high efficiency and low toxicity found in classical prescription drugs is further verified.