Zaffaroni N, Villa R, Silvestro L, Sanfilippo O, Silvestrini R
Istituto Nazionale per lo Studio e la Cura dei Tumori, Milano, Italy.
Anticancer Res. 1990 Nov-Dec;10(6):1599-602.
The in vitro cytotoxic activity of azelaic acid was studied with 25 human melanoma primary cultures and with 5 established cell lines characterized by different contents of melanotic pigment. A dose-dependent antiproliferative effect was observed in both the experimental systems, even though cell lines displayed a slightly greater susceptibility to the compound, with ID50 values generally lower than those for fresh human tumors. Our results do not demonstrate a clear difference between melanotic and non-melanotic melanomas in sensitivity to azelaic acid. The early interference of azelaic acid on nucleic acid metabolism was investigated additionally with 15 human melanoma primary cultures. There were significant inhibitions of RNA and DNA synthesis in a remarkable percentage of tumors, at the highest concentrations of the compound. Moreover, cell proliferation of tumors that showed these antimetabolic effects was always significantly depressed by lower drug concentration as well as by the highest.
用25种人黑色素瘤原代培养物和5种具有不同黑色素含量特征的已建立细胞系研究了壬二酸的体外细胞毒性活性。在两个实验系统中均观察到剂量依赖性抗增殖作用,尽管细胞系对该化合物的敏感性略高,ID50值通常低于新鲜人肿瘤的ID50值。我们的结果未显示黑色素瘤和非黑色素瘤在对壬二酸的敏感性上有明显差异。另外用15种人黑色素瘤原代培养物研究了壬二酸对核酸代谢的早期干扰。在该化合物的最高浓度下,相当比例的肿瘤中RNA和DNA合成受到显著抑制。此外,显示出这些抗代谢作用的肿瘤细胞增殖总是在较低药物浓度以及最高浓度下受到显著抑制。