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.
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