Luk G D, Goodwin G, Marton L J, Baylin S B
Proc Natl Acad Sci U S A. 1981 Apr;78(4):2355-8. doi: 10.1073/pnas.78.4.2355.
Many human small-cell lung carcinoma culture lines grow as multicellular aggregate spheroids, for which high L-dopa decarboxylase activity is a marker. During the initial cell aggregation and the exponential growth phase, there is a marked increase in ornithine decarboxylase activity and an accumulation of polyamines. alpha-Difluoromethylornithine, a specific enzyme-activated, irreversible ornithine decarboxylase inhibitor, blocks the increase in ornithine decarboxylase activity and in polyamines and inhibits human small-cell lung carcinoma cell growth. After the onset of a decreased proliferation rate, the multicellular spheroid aggregates become poorly formed, cell loss ensues, and there is a decrease in L-dopa decarboxylase activity. These findings support the hypothesis that ornithine decarboxylase and the polyamines play an essential role not only in the proliferative phase but also in the viability of human small-cell lung carcinoma cells in culture. The results suggest that alpha-difluoromethylornithine, a virtually nontoxic compound, may be potentially useful in the therapy of this human tumor.
许多人类小细胞肺癌细胞系会以多细胞聚集体球体的形式生长,其中高L-多巴脱羧酶活性是一个标志物。在初始细胞聚集和指数生长期,鸟氨酸脱羧酶活性显著增加,多胺积累。α-二氟甲基鸟氨酸是一种特异性酶激活的不可逆鸟氨酸脱羧酶抑制剂,它能阻断鸟氨酸脱羧酶活性和多胺的增加,并抑制人类小细胞肺癌细胞的生长。在增殖速率开始下降后,多细胞球体聚集体形成不良,细胞随后丢失,L-多巴脱羧酶活性降低。这些发现支持了这样一种假说,即鸟氨酸脱羧酶和多胺不仅在增殖期而且在培养的人类小细胞肺癌细胞的生存能力中都起着至关重要的作用。结果表明,α-二氟甲基鸟氨酸这种几乎无毒的化合物可能在这种人类肿瘤的治疗中具有潜在用途。