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顺铂的广谱抗癌活性已普遍为人们所接受,它的作用机制一般认为是与DNA作用抑制细胞分裂,最终造成细胞的死亡。但是我们必须看到,顺铂进入人体有可能与多种物质发生化学结合作用。大量事实表明,顺铂可与血浆蛋白质结合,如α_2-巨球蛋白、γ-球蛋白和转铁蛋白以及血清白蛋白。在血清白蛋白肽链34位上有一个可与金属作用的游离巯基,因此,认为是顺铂作用的主要部位。关于血清白蛋白的巯基是否与顺铂结合迄今并没有直接的实验证据。本工作采用凝胶色谱法和光度法测定了顺铂及水解产物与牛血清白蛋白作用后巯基含量的变化,结果表明,牛血清白蛋白巯基含量确实有所改变。
The broad-spectrum anti-cancer activity of cisplatin has been generally accepted by the people, and its mechanism of action is generally believed that the role of DNA and inhibit cell division, and ultimately cause cell death. However, we must see that there is a possibility that cisplatin enters the body and chemically binds to various substances. Numerous facts show that cisplatin binds to plasma proteins such as α 2-macroglobulin, γ-globin and transferrin, and serum albumin. There is a free mercapto group at the 34-position of the serum albumin peptide that interacts with the metal and, therefore, is believed to be a major site of cisplatin action. There is no direct experimental evidence as to whether sulfhydryl of serum albumin binds to cisplatin. This work uses gel permeation chromatography and spectrophotometric determination of cisplatin and hydrolysates and bovine serum albumin after the mercapto content changes, the results show that the bovine serum albumin content has indeed changed.