Aschele C, Romanini A, Nicolin A, Rosso R, Sobrero A
Department of Medical Oncology, Istituto Nazionale per la Ricerca sul Cancro, Genova, Italy.
Anticancer Res. 1990 May-Jun;10(3):759-64.
In a search for a rapid and simple method to determine drug-induced cell lethality, the inhibition of tritium release from [5-3H]-2'-deoxyuridine (ITR) was compared with a standard clonogenic assay. Seven drugs were studied. After a 4 hr incubation period, [5-3H]-2'-deoxyuridine was added to cultures of human colon carcinoma cells (HCT-8) in vitro and four dose-response curves were generated for each drug by sampling the culture medium for tritiated H2O formation 4, 24, 48 and 72 hr later. These curves were compared to those obtained by a standard clonogenic assay. The ED50 values for 5 of the 7 drugs tested, methotrexate, 5-fluorouracil, doxorubicin, vincristine and cisplatin, as measured by inhibition of HCT-8 colony growth, were within 3 times the values observed with the metabolic assay. The ITR highly overestimated the cytotoxicity of 5-fluoro-2'-deoxyuridine: the irreversible inhibition of thymidylate synthase by this nucleoside resulted in an ED50 value 100-fold lower than that observed with the clonogenic assay. Opposite results were obtained with 5-fluorouridine. These data indicate that the ITR can be used to determine drug sensitivity of these cells to a host of compounds although it cannot be used indiscriminately for every antineoplastic agent as a cytotoxicity assay.
为寻找一种快速简便的方法来测定药物诱导的细胞致死率,将[5-³H]-2'-脱氧尿苷的氚释放抑制率(ITR)与标准克隆形成试验进行了比较。研究了七种药物。在4小时的孵育期后,将[5-³H]-2'-脱氧尿苷添加到体外培养的人结肠癌细胞(HCT-8)中,并在4、24、48和72小时后通过采集培养基以检测氚化水的形成,为每种药物生成四条剂量反应曲线。将这些曲线与通过标准克隆形成试验获得的曲线进行比较。通过抑制HCT-8集落生长测定的7种受试药物中的5种,即甲氨蝶呤、5-氟尿嘧啶、阿霉素、长春新碱和顺铂的ED50值,在代谢试验观察值的3倍以内。ITR高估了5-氟-2'-脱氧尿苷的细胞毒性:该核苷对胸苷酸合成酶的不可逆抑制导致ED50值比克隆形成试验观察到的值低100倍。5-氟尿苷则得到相反的结果。这些数据表明,ITR可用于测定这些细胞对多种化合物的药物敏感性,尽管它不能作为细胞毒性试验不加区分地用于每种抗肿瘤药物。