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自旋标记鬼臼2位立体异构体酯类分析及生物活性

Spin-labeled 2-stereoisomer esters of podophyllotoxin and its biological activity

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【作者】 张志伟张甲强赵磊田瑄

【Author】 ZHANG Zhi-wei~1,ZHANG Jia-qiang~1,ZHAO Lei~2,TIAN Xuan~1 (1.State Key Laboratory of Applied Organic Chemistry,Lanzhou University,Lanzhou 730000,China; 2.Department of Pharmacy,Gansu College of Traditional Chinese Medicine,Lanzhou 730000,China)

【机构】 兰州大学功能有机分子化学国家重点实验室甘肃中医学院药学系

【摘要】 合成了四对自旋标记的鬼臼2位立体异构体酯类衍生物,通过比较圆二色谱中第一偶合谱(270~290 nm),应用Hulbert规则可区分鬼臼2位酯类立体异构体.薄层色谱研究中,四对化合物的R_f值具有一定的规律性,为区分这些化合物提供了一种简便、快捷的方法.进行了四对自旋标记酯类衍生物对人体三种肿瘤细胞株(肺癌细胞A-549、肝癌细胞Bel-7402和结肠癌细胞HCT-8)的抗肿瘤活性实验,并对Sprague Dawley(SD)大鼠的肝、肾组织做了抗脂质过氧化实验,结果显示该类化合物的抗癌活性与抗氧化活性有一定的相关性.

【Abstract】 Four pairs of spin-labeled 2-stereoisomer esters of podophyllotoxin were studied.The 2-stereoisomers were identified by comparing the first couplet(270~290 nm) and using the Hulbert rules in the circular cichroism spectra.In the thin layer chromatography,the R_f values of the four pairs’ compounds exhibited an orderliness,which provided a simple and convenient method for distinguishing these compounds.The antitumor activities of the four pairs’ compounds against three human tumor cell lines(lung carcinoma cell A-549,hepatoma cells Bel-7402,colorectal carcinoma cell HCT-8) and the antioxidant activities on the liver and kidney tissues of the Sprague Dawley rats were determined.The results indicated the antitumor and antioxidant activities exhibited positive relationship.

【基金】 甘肃省自然科学基金项目(3ZS061-A25-124)
  • 【文献出处】 兰州大学学报(自然科学版) ,Journal of Lanzhou University(Natural Sciences) , 编辑部邮箱 ,2010年02期
  • 【分类号】R285;R284
  • 【被引频次】1
  • 【下载频次】52
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