半边翼草抗肿瘤化合物对HL-60细胞DNA拓扑异构酶和细胞周期的影响。

J H Li, C W He, N C Liang, L E Mo, X Zhang
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引用次数: 0

摘要

目的:研究半翼草抗肿瘤化合物5F、6F和A对HL-60细胞DNA拓扑异构酶活性和细胞周期的影响,以及化合物6F与染料木素联用的体外增效作用。方法:从HL-60细胞系中分离DNA拓扑异构酶,以超卷曲pBR322 DNA为底物,测定DNA拓扑异构酶I和II的活性。流式细胞术(FCM)分析细胞周期。采用MTT法进行细胞毒性试验。结果:化合物5F、6F和A抑制DNA拓扑异构酶I和II的活性。化合物6F作用后,细胞周期S期和G2/M期细胞数量增加,G0/G1期细胞数量减少。在低浓度(57.8和115.6 nmol.L-1)下,化合物6F与染料木素联用对HL-60细胞株的细胞毒性增强,q值> 1.15。增强倍数分别为57.8和115.6 nmol。染料木素对6F的L-1分别为2.60和4.65。结论:化合物5F、6F、A对HL-60细胞DNA拓扑异构酶活性有抑制作用。化合物6F增加了S期和G2/M期细胞数量,降低了G0/G1期细胞数量,增强了染料木素的细胞毒性,与6F具有协同抗肿瘤作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effects of antitumor compounds isolated from Pteris semipinnata L on DNA topoisomerases and cell cycle of HL-60 cells.

Aim: To study the effect of the antitumor compounds 5F, 6F, and A from Pteris semipinnata L on the activities of DNA topoisomerases and cell cycle of HL-60 cells, and the synergism of compound 6F in combination with genistein in vitro.

Methods: DNA topoisomerases were isolated from HL-60 cell lines, and supercoiled pBR322 DNA was used as substrate to determine the activities of DNA topoisomerase I and II. Cell cycle was analyzed by flow cytometry (FCM). Cytotoxicity assay was tested by MTT method.

Results: Compounds 5F, 6F, and A inhibited the activities of DNA topoisomerase I and II. After exposure of the cells to compound 6F, an increase in cells in the S and G2/M phases and a decrease in cells in the G0/G1 phase of the cell cycle were observed. At low concentrations (57.8 and 115.6 nmol.L-1), compound 6F enhanced the cytotoxicity against HL-60 cell line in combination with genistein, q values were > 1.15. The enhancement times of 57.8 and 115.6 nmol.L-1 of 6F by genistein were 2.60 and 4.65, respectively.

Conclusion: Compounds 5F, 6F, and A inhibited the activities of DNA topoisomerases of HL-60 cells. Compound 6F increased the number of cells in S and G2/M phases, decreased the population of G0/G1 phase cells, and enhanced the cytotoxicity of genistein, which had synergism with 6F in antitumor action.

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