高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (5): 817.

• 论文 • 上一篇    下一篇

聚(L-天冬氨酸)衍生物-顺铂结合物的制备及体外细胞毒性研究

吕正荣, 余家会, 卓仁禧, 王旭立, 杨复华   

  1. 武汉大学化学系, 国家教育委员会生物医用高分子材料开放研究实验室, 武汉, 430072
  • 收稿日期:1996-11-28 出版日期:1998-05-24 发布日期:1998-05-24
  • 通讯作者: 卓仁禧
  • 作者简介:吕正荣,男,33岁,教授.
  • 基金资助:

    国家自然科学基金

Studies on the Preparation and in vitro Cytotoxicity of Poly(L-aspartic acid) Derivatives-cis-platin Conjugates

LÜ Zheng-Rong, YU Jia-Hui, ZHUO Ren-Xi, WANG Xu-Li, YANG Fu-Hua   

  1. Laboratory of Biomedical Polymer of SECC, Department of Chemistry, Wuhan University, Wuhan, 430072
  • Received:1996-11-28 Online:1998-05-24 Published:1998-05-24

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被引次数

74

摘要： 通过α,β-聚(L-天冬氨酸)及其衍生物α,β,L-天冬氨酸和[α,β,L-(N-羟乙基)天冬酰胺]共聚物,[α,β,L-(N-羟乙基)天冬酰胺]和[α,β,L-(N-丁二酸基)天冬酰胺]共聚物为载体,与顺式二氯二氨合铂(Ⅱ)结合,合成了相应高分子-顺铂结合物.研究结果表明,在中性pH值络合最有效,聚合物-顺铂结合物的体外细胞毒性随结合物浓度增大而增大,但均小于同浓度顺铂毒性.

关键词: 高分子载体抗肿瘤药物, 高分子-顺铂结合物, 细胞毒性

Abstract: Three α, β-poly(L-aspartic acid) derivatives cis platin conjugates were synthesized by conjugation of α,β-poly(Laspartic acid), (α,β,L-aspartic acid) [ α,β,L-(Nhydroxyethyl) aspartamide] copolymer and [ α,β,L-(N-hydroxyethyl) aspartamide]-[ α,β,L-(N-succinyl) aspartamide] copolymer with cis-dichlorodiammine platinum(Ⅱ) respectively. The polymer carriers were characterized by IR, GPC and intrinsic viscosity. The influence of pHon the conjugation reaction was studied. Cytotoxicity of polymer-cis-platin conjugates was tested against cervix uteri Hela cells in vitro . The cytotoxicity of polymer-cis-platin conjugates increases with the increase of concentration of the congugates, but lower than cis-platin of the corresponding concentration.

Key words: Polymer antitumor drug, Polymer-cis-platin conjugates, Cytotoxicity

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