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小肽修饰的PAMAM树枝状化合物的生物活性

THE BIOACTIVITY OF PAMAM DENDRIMERS MODIFIED WITH PEPTIDES

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【作者】 钟弘贾欣茹罗宇飞陈丽蓉危岩

【Author】 ZHONG Hong, JIA Xinru, LUO Yufei, CHEN Lirong (College of Chemistry and Molecular Engineering, Peking University, Beijing 100871) WEI Yen (Department of Chemistry, Drexel University, Philadelphia PA 19104)

【机构】 北京大学化学与分子工程学院美国Drexel大学化学系 北京100871北京100871费城PA19104

【摘要】 合成了甘氨酸 (Gly) 天冬氨酸 (Asp)组成的肽链Gly Asp、Gly Asp Gly Asp、Gly Asp (Gly Asp) 2 .分别将天冬氨酸及上述合成的肽链引入到聚酰胺 胺型树枝状化合物 (PAMAM)的表面 .对所得化合物进行了分子模拟 ,结果表明Gly Asp (Gly Asp) 2 肽链在PAMAM表面可形成接近于 β sheet的构象 .由实验得知 ,经Asp、Gly Asp、Gly Asp Gly Asp、Gly Asp (Gly Asp) 2 修饰的PAMAM树枝状化合物对抗坏血酸还原FeⅢ 细胞色素C(cytc)的反应有干扰作用 ,导致该反应速率下降 .这说明所合成的化合物与cytc有较好的结合能力 .特别是Gly Asp (Gly Asp) 2 修饰的PAMAM ,其与cytc的结合常数为 1 6ⅹ 1 0 5.

【Abstract】 The peptides of Gly-Asp,Gly-Asp-Gly-Asp and Gly-Asp-(Gly-Asp) 2 were synthesized.These peptides and Asp were introduced at the periphery of G3.5 PAMAM dendrimers,respectively.It was found by calculating from 1H integrations of each modified compound that 77%,60%,24% and 18% of ester groups on the surface of these dendrimers reacted with the Asp、Gly-Asp,Gly-Asp-Gly-Asp and Gly-Asp-(Gly-Asp) 2 peptides,respectively.The molecular simulating showed that the conformation of Gly-Asp-(Gly-Asp) 2 is quite similar to β-sheets.Compared with PAMAMC,these modified PAMAM dendrimers could obviously decrease the reduction rate of Fe Ⅲ-cyt c by ascorbic acid,especially,the dendrimer with Gly-Asp-(Gly-Asp) 2 on its exterrior. The experimental results demonstrated the better recognition and affinity between the peptides modified PAMAM dendrimers and Cytochrome C.The association constant of G3.5-Gly-Asp-(Gly-Asp) 2 with cytochrome C is 1.6×10 5.

【基金】 国家自然科学基金资助项目 (基金号 5 99730 0 1)
  • 【文献出处】 高分子学报 ,Acta Polymerica Sinica , 编辑部邮箱 ,2002年06期
  • 【分类号】TQ323
  • 【被引频次】4
  • 【下载频次】227
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