Takahashi I, Ohnuma T, Kavy S, Bhardwaj S, Holland J F
Br J Cancer. 1980 Apr;41(4):602-8. doi: 10.1038/bjc.1980.103.
The influence of human serum albumin (HA) on the biological effects of 13 chemotherapeutic agents was studied in vitro in the human leukaemia cell line MOLT-3. On the basis of changes in biological activity influenced by HA, these drugs may be divided into three types. Type I agents include cis-diamminedichloroplatinum (II), 4'-(9-acridinylamino)methanesulphon-m-anisidide, neocarzinostatin, nitrogen mustard, adriamycin, daunorubicin and mitomycin C--drugs whose biological activities are reduced in the presence of HA. The biological activities of Type II drugs (cytosine arabinoside, fluorouracil and actinomycin D) are not influenced by HA. The biological activities of Type III drugs (bleomycin, vincristine and vinblastine) are increased in the presence of HA. These results indicate that serum HA interferes in vitro with certain anticancer agents in terms of biological activity and, probably, clinical effectiveness. HA-drug interaction may be a major factor governing the pharmacology of Type I anticancer agents in man.
在人白血病细胞系MOLT-3中对人血清白蛋白(HA)对13种化疗药物生物学效应的影响进行了体外研究。根据HA影响的生物学活性变化,这些药物可分为三类。I类药物包括顺二氨二氯铂(II)、4'-(9-吖啶基氨基)甲磺基间茴香胺、新制癌菌素、氮芥、阿霉素、柔红霉素和丝裂霉素C,这些药物在有HA存在时生物学活性降低。II类药物(阿糖胞苷、氟尿嘧啶和放线菌素D)的生物学活性不受HA影响。III类药物(博来霉素、长春新碱和长春花碱)在有HA存在时生物学活性增强。这些结果表明,血清HA在体外就生物学活性以及可能的临床疗效方面干扰某些抗癌药物。HA与药物的相互作用可能是决定I类抗癌药物在人体内药理学特性的一个主要因素。