论文部分内容阅读
以人血浆组份Ⅳ为原料，经过多步纯化及铁饱和，得到纯度为９９％的铁饱和转铁蛋白（Ｈｏｌｏ－ｔｒａｎｓｆｅｒｒｉｎ，Ｈｏｌｏ－ＴＦ）；以转铁蛋白（Ｔｒａｎｓｆｅｒｒｉｎ，ＴＦ）为载体，采用两种不同的偶联方法制备ＴＦ－氨甲蝶呤（Ｍｅｔｈｏｔｒｅｘａｔｕｍ，ＭＴＸ）偶联物：（１）碳二亚胺（ＣＤＣ）法；（２）活化酯（ａｃｔｉｖｅｅｓｔｅｒ）法。偶联制备得到的偶联物兼具有转铁蛋白和药物的特性。体外杀伤试验表明，ＴＦ－ＭＴＸ对Ｋ（５６２）白血病细胞较游离ＭＴＸ分别强８．０倍（ＣＤＣ）和９．０倍（ａｃｔｉｖｅｅｓｔｅｒ）；对ＢＥＬ－７７２１肝癌细胞较游离ＭＴＸ强１４．７倍（ａｃｔｉｖｅｅｓｔｅｒ）。这说明按本文方法制备的偶联药物对于肝癌细胞，白血病细胞有一定的导向杀伤作用。
Human plasma fraction Ⅳ was used as raw material, and after several steps of purification and iron saturation, Holo-transferrin (Holo-TF) with 99% purity was obtained. Transferrin (TF) TF-Methotrexatum (MTX) conjugates were prepared using two different coupling methods: (1) carbodiimide (CDC) method; and (2) activeester method. Coupling prepared conjugates with both transferrin and drug properties. In vitro cytotoxicity assay showed that TF-MTX was 8.0-fold (CDC) and 9.0-fold (9.0 times) stronger than free MTX on K (562) leukemia cells, respectively. (Activeester). This shows that the coupling method prepared by this method for liver cancer cells, leukemia cells have a certain role in guiding the killing.