| 三元FA-HSA-MTO靶向给药体系的研究 |
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| 引用本文： | 周秋菊,毕雅静,向俊锋,唐亚林,杨千帆,徐广智. 三元FA-HSA-MTO靶向给药体系的研究[J]. 中国化学, 2008, 26(8): 1385-1389. DOI: 10.1002/cjoc.200890252 |
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| 作者姓名： | 周秋菊 毕雅静 向俊锋 唐亚林 杨千帆 徐广智 |
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| 作者单位： | 1.中国科学院化学研究所分子动态与稳态结构国家重点实验室，中国北京，100190 ;2.中国科学院研究生院，中国北京，100049 ; |
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| 摘 要： | 本论文设计了一种叶酸－人血清白蛋白－米托蒽醌（即FA-HSA-MTO)三元靶向给药体系，其中，由于叶酸和米托蒽醌能同时结合于人血清白蛋白的不同位点而被人血清白蛋白运输到体内，再利用叶酸与其受体的特异性结合而使肿瘤细胞更有效地摄取米托蒽醌。紫外吸收光谱、荧光光谱和核磁共振实验数据都证实了FA-HSA-MTO三元体系的形成。而且，细胞毒试验显示，FA-HSA-MTO三元体系的细胞毒性达79.95％，比HSA-MTO二元体系高出30％。本论文证明：叶酸－人血清白蛋白－米托蒽醌三元靶向给药体系是可行的也是有效的。
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| 关 键 词： | 靶向给药体系 米托蒽醌 人血清白蛋白 叶酸 细胞毒试验 |
| 收稿时间： | 2007-10-22 |
| 修稿时间： | 2008-02-28 |
Investigation on a Potential Targeting Drug Delivery System Consisting of Folate,Mitoxantrone and Human Serum Albumin |
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| Qiu‐Ju ZHOU,Ya‐Jing BI,Jun‐Feng XIANG,Ya‐Lin TANG,Qian‐Fan YANG,Guang‐Zhi XU. Investigation on a Potential Targeting Drug Delivery System Consisting of Folate,Mitoxantrone and Human Serum Albumin[J]. Chinese Journal of Chemistry, 2008, 26(8): 1385-1389. DOI: 10.1002/cjoc.200890252 |
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| Authors: | Qiu‐Ju ZHOU Ya‐Jing BI Jun‐Feng XIANG Ya‐Lin TANG Qian‐Fan YANG Guang‐Zhi XU |
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| Affiliation: | 1. Beijing National Laboratory for Molecular Sciences (BNLMS), Center for Molecular Sciences, State Key Laboratory for Structural Chemistry of Unstable and Stable Species, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China;2. Graduate University of Chinese Academy of Sciences, Beijing 100049, China |
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| Abstract: | A potential targeting drug delivery system consisting of folate (FA), the targeting molecule, human serum albumin (HSA), the carrier, and mitoxantrone (MTO), the medicine, has been designed. Data obtained by UV absorption, fluorescence, and NMR techniques indicated the formation of ternary complexes and possible application to building a targeting drug delivery system by using FA, MTO and HSA. Furthermore, cytotoxicity assay indicated that the toxicity of the FA‐HSA‐MTO against PC‐3 cell line was 79.95%, which was much higher than that of free MTO tested in totally the same conditions. About 30% increase of the toxicity should be owed to the targeting effect of FA. Thus, the feasibility and validity of a novel targeting drug delivery system, FA‐HSA‐MTO, was confirmed. |
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| Keywords: | targeting drug delivery system mitoxantrone human serum albumin folate cytotoxicity assay |
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