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 、 1 H-NMR 和 13 C -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 BGC823 cells ， BGC823 ）细胞、鼻咽癌（ human nasopharyngeal carcinoma CNE cells ， CNE ）、白血病（ human leukemic HL-60 cells ， HL-60 ）、口腔上皮癌（ human oral epithelial carcinoma KB cell s ， KB ）、结肠癌（ human colon carcinoma LS174T cells ， LS174T ）、前列腺癌（ human prostate cancer PC3 cells ， 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 ， 2.54 mg·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。
Abstract
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.
关键词
合成 /
姜黄素 /
硒 /
抗肿瘤活性
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Key words
synthesis /
curcumin /
selenium /
antitumor activity
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参考文献
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（ 收稿日期 ： 2009-02-09 ）
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