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[阿霉素与甲胎蛋白抗体结合物的制备及其性质]

[Preparation of conjugates of adriamycin with antibodies to alpha-fetoprotein and their properties].

作者信息

Nishiwaki S, Takei N, Higashi T, Hibi N, Tsukada Y, Hirai H

出版信息

Gan To Kagaku Ryoho. 1984 Aug;11(8):1591-7.

PMID:6206799
Abstract

For its selective accumulation into tumor cells, the antitumor drug adriamycin (ADM) was attached to specific antibodies reactive against alpha-fetoprotein, a carcinoembryonic protein, and the antibody and antitumor activities of the resulting conjugate were investigated. Using the glutaraldehyde or carbodiimide binding methods, preparations containing 4-5 moles of ADM per mole of antibody were obtained. They retained 60-75% of the original antibody activity. Upon incubation of AH-66 ascites hepatoma cells with the conjugates, an increased number of dead cells and inhibited uptake of 3H-thymidine by the cells were observed. The conjugates were more effective against tumor cells than the free drug, and it was further presumed that the cytotoxic action of ADM on normal cells could be reduced by binding it to a macromolecular protein.

摘要

为了使其能选择性地积聚到肿瘤细胞中,将抗肿瘤药物阿霉素(ADM)与针对甲胎蛋白(一种癌胚蛋白)的特异性抗体相连,并对所得偶联物的抗体和抗肿瘤活性进行了研究。采用戊二醛或碳二亚胺结合法,得到了每摩尔抗体含4 - 5摩尔ADM的制剂。它们保留了60 - 75%的原始抗体活性。用这些偶联物孵育AH - 66腹水肝癌细胞后,观察到死亡细胞数量增加,且细胞对³H - 胸腺嘧啶核苷的摄取受到抑制。这些偶联物对肿瘤细胞的作用比游离药物更有效,并且进一步推测,将ADM与大分子蛋白结合可降低其对正常细胞的细胞毒性作用。

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