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目的:合成大黄素10-位希夫氏碱衍生物并研究其抗肿瘤活性。方法:将大黄素与氨衍生物在无水乙醇中以醋酸催化而合成,用核磁共振氢谱、电子轰击质谱法进行结构表征;用四唑盐(MTT)比色法测定其对k562肿瘤细胞增殖抑制率并计算其IC50值。结果:合成了3个大黄素10-位希夫氏碱衍生物,对k562肿瘤细胞的IC50值分别是4.5,3.8,2.0μmol·L-1。结论:大黄素10位希夫氏碱衍生物提高了其母体化合物的抗肿瘤活性并增加了成药性,值得进一步研究。
OBJECTIVE: To synthesize 10-mer derivatives of emodin and study its anti-tumor activity. METHODS: Emodin and ammonia derivatives were synthesized by the catalysis of acetic acid in absolute ethanol. The structures were characterized by 1H-NMR and electron impact mass spectrometry. The effects of emodin and ammonia on k562 tumor cells Proliferation inhibition rate and calculate its IC50 value. Results: Three derivatives of emodin 10-site Schiff base were synthesized, and the IC50 values of k562 tumor cells were 4.5, 3.8 and 2.0 μmol·L-1, respectively. CONCLUSION: Emodin 10-mer Schiff base derivative enhances the antitumor activity of its parent compound and enhances the drug-induced potency, which deserves further study.