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若干重要生理活性天然产物的化学与生物学研究:A Structure-Activity Guided Strategy for Fluorescent Labeling ...

  • 关键字: A Structure-Activity Guided Strategy 发布者:Hai-Xia Liu, Zhu-Jun Yao 发布时间:2009-03-02 18:03:28 点击数: 4158次

ChemBioChem. 2007, 8, 172-177.
 
A Structure-Activity Guided Strategy for Fluorescent Labeling of Annonaceous Acetogenin Mimetics and Its Application in Cell Biology
 
Hai-Xia Liu, Guo-Rui Huang, Huan-Ming Zhang, Sheng Jiang, Jia-Rui Wu2, Zhu-Jun Yao1
 
1. State Key Laboratory of Bioorganic and Natural Product Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China; 2. Shanghai Institute of Biochemistry and Cell Biology, SIBS, Chinese Academy of Sciences, Shanghai 200031 China.
 
Abstract: The potent anticancer agent AA005 has been successfully biolabeled with fluorescein. Of the two compounds synthesized, only AA005-flu retained the selectivity of AA005 for cancerous (e.g., BEL-7404) over normal (e.g., LO2) cells. Fluorescent-imaging studies revealed that AA005-flu's distribution in human normal cells was significantly difference from that in cancer cells, where AA005-flu accumulates in the mitochondria. This direct and visible evidence suggests that membrane recognition of AA005 is involved in its selective action.