Sargent J M, Elgie A W, Williamson C J, Taylor C G
Pembury Hospital, Kent, UK.
Br J Cancer. 1996 Dec;74(11):1730-3. doi: 10.1038/bjc.1996.622.
Enhanced DNA repair has been observed in cisplatin-resistant ovarian cancer cell lines. This resistance can be modulated, on co-incubation with aphidicolin in established cell lines and animal tumour models, by inhibiting DNA polymerases. We describe a study of the in vitro modulation effect of aphidicolin on cisplatin and carboplatin using fresh cells harvested from biopsy samples or ascitic fluids from 25 patients with ovarian adenocarcinoma. The MTT assay was used to measure cell survival after drug exposure. Aphidicolin (up to 30 microM) showed no cytotoxicity when tested alone. Forty-seven comparisons were made between drug with and without aphidicolin, and 37 (79%) cases demonstrated a significant increase in sensitivity to the platinum agents on co-incubation. Overall, there was a median 10-fold (range 1.64- to 58.5-fold) increase in sensitivity. When patients were grouped according to in vitro sensitivity to platinum, aphidicolin had a significantly greater effect in the "resistant' group, causing a median 13.5-fold increase in sensitivity compared with 2.4-fold in the "sensitive' group. Furthermore, a positive correlation between the LC50 for platinum and the corresponding fold increase in sensitivity suggests that aphidicolin overcomes platinum resistance in fresh cells from primary tumours. These results encourage the further development of this interesting compound.
在顺铂耐药的卵巢癌细胞系中观察到DNA修复增强。在已建立的细胞系和动物肿瘤模型中,与阿非迪霉素共同孵育时,这种耐药性可通过抑制DNA聚合酶来调节。我们描述了一项关于阿非迪霉素对顺铂和卡铂体外调节作用的研究,使用从25例卵巢腺癌患者的活检样本或腹水采集的新鲜细胞。采用MTT法测定药物暴露后的细胞存活率。单独测试时,阿非迪霉素(高达30微摩尔)未显示出细胞毒性。对使用和未使用阿非迪霉素的药物进行了47次比较,37例(79%)病例显示共同孵育时对铂类药物的敏感性显著增加。总体而言,敏感性中位数增加了10倍(范围为1.64至58.5倍)。当根据对铂的体外敏感性对患者进行分组时,阿非迪霉素在“耐药”组中的作用明显更大,导致敏感性中位数增加13.5倍,而“敏感”组为2.4倍。此外,铂的半数致死浓度(LC50)与相应的敏感性增加倍数之间呈正相关,这表明阿非迪霉素克服了原发性肿瘤新鲜细胞中的铂耐药性。这些结果鼓励对这种有趣的化合物进行进一步开发。