槲皮素-3-O-乙酸苯佐卡因的合成及抗肿瘤活性研究

发布时间：2018-10-24 18:20

【摘要】：目的:合成槲皮素-3-O-乙酸苯佐卡因,并测定其抗肿瘤活性。方法:以芦丁为原料,利用苄基选择性保护羟基,脱去芦丁糖,再经Williamson反应及脱苄基,合成了槲皮素-3-O-乙酸苯佐卡因。结果:收率72.5%。经1H NMR、13C NMR及MS显示,与目标化合物相吻合。用MTT法检测目标化合物对肿瘤细胞增殖的抑制作用,结果显示:目标化合物对EC109的抑制作用(IC50=10.25μmol/L)明显优于母药槲皮素(IC50=31.884μmol/L),和5-FU(IC50=41.738μmol/L);其对EC9706及B16-F10两种肿瘤细胞的抑制作用也均强于母药槲皮素。结论:槲皮素-3-O-乙酸苯佐卡因较槲皮素和5-FU具有更强的细胞增殖抑制活性。
[Abstract]:Aim: to synthesize quercetin-3-o-acetic acid benzocaine and to determine its anti-tumor activity. Methods: using rutin as raw material, benzyl selective protection of hydroxyl group, removal of rutin sugar, Williamson reaction and debenzyl group were used to synthesize quercetin 3-Oacetate benzocaine. Results: the yield was 72.5%. The results of 1H NMR,13C NMR and MS show that it is consistent with the target compound. The inhibitory effects of the target compounds on the proliferation of tumor cells were detected by MTT assay. The results showed that the inhibitory effect of the target compound on EC109 (IC50=10.25 渭 mol/L) was significantly superior to that of IC50=31.884 渭 mol/L and 5-FU (IC50=41.738 渭 mol/L), and the inhibitory effect of the target compound on EC9706 and B16-F10 tumor cells was also stronger than that of quercetin. Conclusion: quercetin-3-o-acetic acid benzocaine has stronger cell proliferation inhibitory activity than quercetin and 5-FU.
【作者单位】：郑州工业应用技术学院医学院;郑州工业应用技术学院药学院;郑州大学药学院;
【基金】：基金资助:郑州地方高校技术技能名师工作室(No.郑教高[2015]70号])~~
【分类号】：R914;R96

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