Luo Hui, Yang Shengjie, Hong Da, Xue Wei, Xie Pu
Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang, 550006 P. R. China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025 P. R. China.
Chem Cent J. 2017 Mar 15;11:23. doi: 10.1186/s13065-017-0253-9. eCollection 2017.
Cancer is one of the leading causes of death and only second to heart diseases. Recently, preclinical studies have demonstrated that curcumin had a number of anticancer properties. Thus, we planned to synthesize a series of curcumin analogs to assess their antiproliferation efficacy.
A series of (1,4)-1-aryl-5-(2-((quinazolin-4-yl)oxy)phenyl)-1,4-pentadien-3-one derivatives (curcumin analogs) were synthesized and characterized by IR, NMR, and elemental analysis techniques. All of the prepared compounds were screened for antitumor activities against MGC-803, PC3, and Bcap-37 cancer cell lines. A significant inhibition for cancer cells were observed with compound and also less toxic on NIH3T3 normal cells. The mechanism of cell death induced by compound was further investigated by acridine orange/ethidium bromide staining, Hoechst 33,258 staining, TUNEL assay, and flow cytometry cytometry, which revealed that the compound can induce cell apoptosis in MGC-803 cells.
This study suggests that most of the derivatives could inhibit the growth of human cancer cell lines. In addition, compound could induce apoptosis of cancer cells, and it should be subjected to further investigation as a potential anticancer drug candidate.
癌症是主要的死亡原因之一，仅次于心脏病。最近，临床前研究表明姜黄素具有多种抗癌特性。因此，我们计划合成一系列姜黄素类似物以评估其抗增殖功效。
合成了一系列(1,4)-1-芳基-5-(2-((喹唑啉-4-基)氧基)苯基)-1,4-戊二烯-3-酮衍生物（姜黄素类似物），并通过红外光谱、核磁共振和元素分析技术进行了表征。所有制备的化合物均针对MGC-803、PC3和Bcap-37癌细胞系进行了抗肿瘤活性筛选。化合物对癌细胞有显著抑制作用，且对NIH3T3正常细胞毒性较小。通过吖啶橙/溴化乙锭染色、Hoechst 33258染色、TUNEL检测和流式细胞术进一步研究了化合物诱导细胞死亡的机制，结果表明该化合物可诱导MGC-803细胞凋亡。
本研究表明大多数衍生物可抑制人癌细胞系的生长。此外，化合物可诱导癌细胞凋亡，作为一种潜在的抗癌药物候选物应进一步研究。
