Institute of Biology and Ecology, Department of Cellular Biology, Pavol Jozef Šafárik University in Kosice, Košice, Slovakia.
Toxicol In Vitro. 2011 Feb;25(1):37-44. doi: 10.1016/j.tiv.2010.09.004. Epub 2010 Sep 17.
One of the ways for searching for potentially new anti-cancer drugs is the testing of various naturally synthesized compounds. Lichens are a source of unique chemical agents of which some have already been proved to be effective against various cancer in vitro models. Our study reports on the sensitivity of up to nine human cancer cell lines (A2780, HeLa, MCF-7, SK-BR-3, HT-29, HCT-116 p53(+/+), HCT-116 p53(-/-), HL-60 and Jurkat) to the anti-proliferative/cytotoxic effects of four typical secondary metabolites of lichens (parietin, atranorin, usnic acid and gyrophoric acid). Variations in the dynamics of tumour cell line populations were evaluated by the MTT, clonogenic and viability assays, cell proliferation and detachment, cell cycle transition and apoptotic nuclear morphology, thereby confirming their concentration- and time-dependent cytotoxicity. However, in comparison with parietin and gyrophoric acid, the suppression of viability and cell proliferation by usnic acid or atranorin was found to be more efficient at equitoxic doses and correlated more strongly with an increased number of floating cells or a higher apoptotic index. Moreover, the analysis of cell cycle distribution also revealed an accumulation of cells in S-phase. This study has confirmed a differential sensitivity of cancer cell lines to lichen secondary metabolites.
寻找潜在抗癌药物的方法之一是测试各种天然合成化合物。地衣是独特化学物质的来源,其中一些已经被证明对各种体外癌症模型有效。我们的研究报告了多达九种人类癌细胞系(A2780、HeLa、MCF-7、SK-BR-3、HT-29、HCT-116 p53(+/+)、HCT-116 p53(-/-)、HL-60 和 Jurkat)对四种典型地衣次生代谢物(parietin、atranorin、usnic acid 和 gyrophoric acid)的抗增殖/细胞毒性作用的敏感性。通过 MTT、集落形成和活力测定、细胞增殖和脱落、细胞周期转变和凋亡核形态学评估肿瘤细胞系群体动态,从而证实了它们的浓度和时间依赖性细胞毒性。然而,与 parietin 和 gyrophoric acid 相比,usnic acid 或 atranorin 对活力和细胞增殖的抑制作用在等效毒性剂量下更为有效,并且与更多的漂浮细胞或更高的凋亡指数更相关。此外,细胞周期分布分析还显示 S 期细胞的积累。这项研究证实了癌症细胞系对地衣次生代谢物的敏感性存在差异。