| DBAH-Tf靶向药物及其对乳腺癌细胞的杀伤作用分析 |
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| 引用本文： | 谢伟玲,杨培慧,曾鑫,蔡继业.DBAH-Tf靶向药物及其对乳腺癌细胞的杀伤作用分析[J].分析化学,2009,37(5). |
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| 作者姓名： | 谢伟玲 杨培慧 曾鑫 蔡继业 |
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| 作者单位： | 暨南大学化学系,广州,510632 |
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| 基金项目： | 国家自然科学基金，广州市科技计划 |
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| 摘 要： | 以转铁蛋白(Tf)为靶向载体,与双氢青蒿素(DHA)化学偶联制备一种新的双氢青蒿素衍生物-转铁蛋白靶向药物.以DHA为原料先合成了12β-对甲酰肼苯基双氢青蒿素(DBAH),并采用紫外、红外、核磁共振及电化学等手段对目标产物的结构进行了表征.利用高碘酸钠氧化Tf的C端的N-糖链上的邻位羟基,其氧化产物和DBAH通过希夫碱偶联合成了DBAH-Tf靶向药物,采用紫外吸收光谱法和电化学方法进行表征.四甲基氮唑蓝法(MTT)分析了DBAH-Tf及DHA对人乳腺癌细胞(MCF-7)和正常乳腺细胞的体外杀伤作用, 结果表明,DBAH-Tf对MCF-7的杀伤作用是正常乳腺癌细胞的286倍,体现出良好的靶向性.
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| 关 键 词： | 双氢青蒿素衍生物 转铁蛋白 乳腺癌细胞 |
Effects of 4-(12-Dihydroartemisininoxy) Benzoic Acid Hydrozidetransferrin Targeted Drug on Human Breast Cancer Cells |
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| XIE Wei-Ling,YANG Pei-Hui,ZENG Xin,CAI Ji-Ye.Effects of 4-(12-Dihydroartemisininoxy) Benzoic Acid Hydrozidetransferrin Targeted Drug on Human Breast Cancer Cells[J].Chinese Journal of Analytical Chemistry,2009,37(5). |
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| Authors: | XIE Wei-Ling YANG Pei-Hui ZENG Xin CAI Ji-Ye |
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| Institution: | Department of Chemistry of Jinan University;Guangzhou 510632 |
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| Abstract: | As target-carrier,transferrin(Tf) was conjugated with dihydroartemisinin(DHA) to form a new targeted drug.An analog of artemisinin,4-(12-dihydroartemisininoxy) benzoic acid hydrazide(DBAH) have been synthesized and characterized by UV/vis absorption spectroscopy,IR spectroscopy,NMR,electroanalytic chemistry.Periodate was used to oxidize hydroxide group on the N-glycoside chains of C-domain,and then DBAH was reacted with the oxidized transferrin to form a covalent conjugate.In addition,this targeted drug was... |
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| Keywords: | Dihydroartemisinin derivatives transferrin breast cancer cell |
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