姜黄素硒化衍生物的合成和抗肿瘤活性研究

Studies on Synthesis and Antitumor Activity of a Curcumin-Selenium Compound

目的合成姜黄素的硒化衍生物并研究其体外抗肿瘤活性。方法用姜黄素和氯氧化硒反应合成目标化合物,通过氢化物发生-石墨炉原子吸收光谱测定了合成物中的硒含量,用UV、IR、MS、1H-NMR和13C-NMR表征其结构;用姜黄素和顺铂做对照,采用四氮唑盐(MTT)法考察目标化合物对胃癌(human gastric cancer BGC823cells,BGC823)细胞、鼻咽癌(human nasopharyngeal carcinoma CNE cells,CNE)、白血病(human leukemic HL-60cells,HL-60)、口腔上皮癌(human oral epithelial carcinoma KB cells,KB)、结肠癌(human colon carcinoma LS174T cells,LS174T)、前列腺癌(human prostate cancer PC3cells,PC3)及宫颈癌(human cervical cancer cell line HELA cells,HELA)的细胞毒活性。结果确认目标化合物为一种新化合物二姜黄素硒氧配合物;对上述细胞株的IC50分别为45.71,>100,30.09,3.18,>100,21.76,2.54mg·L-1,对KB和HELA均表现出比姜黄素强的抑制活性,对HELA的抑制活性比顺铂要高。结论合成出一个新化合物二姜黄素硒氧配合物;该化合物对部分肿瘤细胞有很强的抑制活性;有关其硒化衍生物对肿瘤细胞生长的抑制机制有待进一步研究。

OBJECTIVE To synthesize curcumin-selenium compound and investigate its antitumor activities in vitro. METHODS A novel organoselenium was synthesized from curcumin and SeOCl2. The content of selenium was determined by hydride generator atomic absorb spectrometry. The structure of new compound was confirmed by UV,IR,MS,1H-NMR and 13C-NMR spectral data. The cytotoxicity activities in vitro were evaluated against seven human cancer cell lines including BGC823,CNE,HL-60,KB,LS174T,PC-3 and HELA by MTT assay. Curcumin and cisplatin were used for comparative purpose. RESULTS The structure of the compound was confirmed as a new curcumin-selenium complex. The IC50 of the new compound on BGC823,CNE,HL-60,KB,LS174T,PC3 and HELA were 45.71,〉100,30.09,3.18,〉100,21.76 and 2.54 mg·L^-1 respectively. The new compound showed inhibition function on KB and HELA cells. CONCLUSION A new curcumin-selenium compound was synthesized for the first time and showed effective potential antitumor activities. It is worthy of further investigation.