Li S, Zhang X Y, Chen X T, Fan D M, Tan L S, Pan H Z, Huang L Q
Laboratory of Gastroenterology, Xijing Hospital, Fourth Military Medical University, Xian.
Chin Med J (Engl). 1990 May;103(5):376-9.
Several chemotherapeutic drugs including methotrexate, daunomycin, mitomycin C and toxin such as ricin, A chain of ricin were chosen to conjugate with murine monoclonal antibodies MGb2 and MG11. The drugs were linked to antibody directly or through human serum albumin as intermediary. The ELISA results showed that the antibody retained well the antigen-binding capacity during conjugation. These conjugates showed highly selective cytotoxic effect on target cells. In chronic cytotoxicity tests, the cytotoxic effect of these conjugates on human gastric cancer cells KATOIII was quite similar to that of free drugs or ricin, but greater than that of irrelevant conjugates, while they had a little effect on non-target cells, suggesting that the selective cytotoxicity on target cells of the conjugates be mediated by antibodies.
选择了几种化疗药物，包括甲氨蝶呤、柔红霉素、丝裂霉素C以及毒素如蓖麻毒素、蓖麻毒素A链，使其与鼠单克隆抗体MGb2和MG11偶联。这些药物直接或通过人血清白蛋白作为中间体与抗体相连。酶联免疫吸附测定（ELISA）结果表明，抗体在偶联过程中很好地保留了抗原结合能力。这些偶联物对靶细胞表现出高度选择性的细胞毒性作用。在慢性细胞毒性试验中，这些偶联物对人胃癌细胞KATOIII的细胞毒性作用与游离药物或蓖麻毒素相当，但大于无关偶联物，而它们对非靶细胞的影响较小，这表明偶联物对靶细胞的选择性细胞毒性是由抗体介导的。
