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通过端氨基聚乙二醇PEG(Ⅰ)与二亚乙基三胺五乙酸二酐(DTPAA)开环合成新型端氨基聚(醚-酰胺)(PEG/DTPA)共聚物造影剂配体(Ⅱ)(Step1);Ⅱ的端氨基与偶联剂3-马来酰亚胺苯甲酸-N-琥珀酰亚胺酯(MBS)的活化端COOH反应,生成偶联剂/聚(醚-酰胺)MB/PEG/DTPA(Ⅲ′)(Step2);再通过Ⅲ′中MBS的CC双键与肝癌细胞靶向黏附肽FAM-AGKGTPSLETTPC-(SH)-COOH(FAM-13)上的巯基SH发生Michael加成反应(Step3),合成含有荧光探针FAM(5-carboxyfluorescein)的肝癌靶向肽/聚(醚-酰胺)(FAM-13/PEG/DTPA,Ⅲ).用1H-NMR和13C-NMR等方法对共聚物进行表征.Ⅲ对正常肝细胞L-02几乎观察不到荧光现象,而对肝癌细胞BEL-7404则有很强的黄绿色荧光,Ⅲ对肝癌细胞有很强的靶向性.大分子配体Ⅲ可望用于制备大分子造影剂及靶向载体负载药物.
A novel poly (ether-amide) (PEG / DTPA) copolymer contrast agent (Ⅱ) was synthesized by ring opening polymerization of terminal amino polyethylene glycol PEG (Ⅰ) and diethylene triamine pentaacetic acid dianhydride (DTPAA) ) (Step1); The terminal amino group of Ⅱ was reacted with the activated terminal COOH of coupling agent 3-maleimidobenzoic acid N-succinimidyl ester (MBS) to form coupling agent / poly (ether-amide) (SH) -COOH (FAM-13) on the surface of human hepatocellular carcinoma cell line M-MB / PEG / DTPA (Ⅲ ’) (Step2) (FAM-13 / PEG / DTPA, Ⅲ) with the fluorescent probe FAM (5-carboxyfluorescein) was synthesized by 1H-NMR and 13C-NMR And so on.Ⅲ showed almost no fluorescence on normal liver cells L-02, but yellow-green fluorescence on hepatoma BEL-7404, and highly targeted on liver cancer cells Ⅲ Macromolecule ligand Ⅲ is expected to be used in the preparation of macromolecular contrast agent and targeted carrier drug loading.