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

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.

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

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.