Brown D H, Braakhuis B J, Van Dongen G A, Snow G B
Department of Otolaryngology-Head and Neck Surgery, Free University Hospital, Amsterdam, The Netherlands.
Otolaryngol Head Neck Surg. 1990 Jan;102(1):20-5. doi: 10.1177/019459989010200104.
Squamous cell lines cultured in vitro provide a potential test system for the selection of analogs that have an improved therapeutic index. The growth inhibitory effects of methotrexate and the new folate analog 10-ethyl, 10-deazaaminopterin were compared in three in vitro-cultured human head and neck squamous cell carcinoma cell lines. The inhibitory concentrations of the new analog were 10- to 100-fold lower than the inhibitory concentrations of methotrexate. The sensitivity of these three head and neck squamous cell carcinoma cell lines to both drugs was essentially the same as the sensitivity of a rhabdomyosarcoma cell line known to be very sensitive to methotrexate when the cell line is grown as a xenograft in athymic nude mice. These data indicate that 10-ethyl, 10-deazaaminopterin may be a new and effective agent against head and neck squamous cell carcinoma.
体外培养的鳞状细胞系为筛选具有更高治疗指数的类似物提供了一个潜在的测试系统。在三种体外培养的人头颈部鳞状细胞癌细胞系中比较了甲氨蝶呤和新型叶酸类似物10-乙基-10-脱氮氨基蝶呤的生长抑制作用。新类似物的抑制浓度比甲氨蝶呤的抑制浓度低10至100倍。当这三种头颈部鳞状细胞癌细胞系作为异种移植物在无胸腺裸鼠中生长时，它们对这两种药物的敏感性与已知对甲氨蝶呤非常敏感的横纹肌肉瘤细胞系的敏感性基本相同。这些数据表明，10-乙基-10-脱氮氨基蝶呤可能是一种治疗头颈部鳞状细胞癌的新型有效药物。
