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熊果酸的结构修饰物及其抗肿瘤活性
引用本文:白育军,杨小生,康文艺,郝小江,徐筱杰,宋宝安. 熊果酸的结构修饰物及其抗肿瘤活性[J]. 华西药学杂志, 2003, 18(2): 87-90
作者姓名:白育军  杨小生  康文艺  郝小江  徐筱杰  宋宝安
作者单位:1. 贵州省、中国科学院天然产物化学重点实验室,贵州,贵阳,550002
2. 北京大学化学与分子工程学院,北京,100871
3. 贵州大学精细化工中心,贵州,贵阳,550025
基金项目:贵州省科技厅科学技术基金资助项目[黔基合计字 (2 0 0 0 ) 3 1 0 5号 ],贵州省省长科研教育基金项目[黔科教办 (2 0 0 1 ) 3号 ]
摘    要:目的 结构修饰熊果酸,制备其衍生物以观察抗肿瘤活性。方法 对熊果酸的1、2位和3位进行氧化,制备其衍生物,并以Hela和HL-60为模型进行了生物活性测试。结果 制备了6个衍生物,其中4个化合物为新化合物;熊果酸结构修饰物的活性均较熊果酸弱。结论 熊果酸经过结构修饰、改造后,生物活性受到影响。

关 键 词:熊果酸 衍生物 抗肿瘤活性 A环碳原子 结构修饰物
文章编号:1006-0103(2003)02-0087-04
修稿时间:2002-11-01

The modificated compounds from ursolic acid and their antitumor activities
BAI Yu-jun ,YANG Xiao-sheng ,KANG Wen-yi ,HAO Xiao-jiang ,XU Xiao-jie ,SONG Bao-an. The modificated compounds from ursolic acid and their antitumor activities[J]. West China Journal of Pharmaceutical Sciences, 2003, 18(2): 87-90
Authors:BAI Yu-jun   YANG Xiao-sheng   KANG Wen-yi   HAO Xiao-jiang   XU Xiao-jie   SONG Bao-an
Affiliation:BAI Yu-jun 1,YANG Xiao-sheng 1*,KANG Wen-yi 1,HAO Xiao-jiang 1,XU Xiao-jie 2,SONG Bao-an 31.The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550002,China, 2. College of Chemistry and Molecular Engineering,Peking University,Beijing 100871,China, 3. Research and Development Center of Fine Chemicals,Guizhou University,Guiyang 550025,China
Abstract:OBJECTIVE To develop the modification of ursolic acid for preparing its derivatives and observing their antitumour activities. METHODS Oxidation of ursolic acid on its 1,2 and 3-position was carried out and the models of Hela and HL-60 cells were used for bioactive screenings. RESULTS Six derivatives were obtained and four of them were new compounds. Their antitumor values on the model of Hela and HL-60 were less than that of ursolic acid. CONCLUSION The antitumour activity of ursolic acid may decrease after its structure modification.
Keywords:Ursolic acid  Derivatives  Antitumour  
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