Bio-Organic and Photochemistry Laboratory, Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143 005, Punjab, India.
Eur J Med Chem. 2013 Nov;69:310-5. doi: 10.1016/j.ejmech.2013.08.017. Epub 2013 Aug 19.
A series of β-ionone derived chalcones were evaluated for cytotoxic activity against various human cancer cell lines using SRB dye assay. All the compounds displayed moderate to high cytotoxic effect against almost all the cancer cell lines. The results also revealed the effect of substituents of the aromatic ring on their inhibitory potential. In general, compounds bearing electron withdrawing groups such as nitro, fluoro, chloro and bromo showed more inhibitory potential than those bearing electron donating groups. The nitro substituted compound (7h) showed comparatively more inhibitory potential than other derivatives, therefore, it was further investigated for observing its effect on cell morphology in Chinese hamster ovary (CHO) cells by using phase contrast imaging, cell cycle analysis and annexin-FITC apoptosis assay. The treated cells exhibited the characteristics of apoptosis i.e. cell shrinkage, chromatin condensation and nuclear fragmentation, and induced the inhibition of cell proliferation by arresting the cells at G0 phase.
用 SRB 染料法评估了一系列β-紫罗兰酮衍生的查耳酮对各种人癌细胞系的细胞毒性。所有化合物对几乎所有癌细胞系均显示出中等至高的细胞毒性作用。结果还揭示了芳香环取代基对其抑制潜力的影响。一般来说,带有吸电子基团(如硝基、氟、氯和溴)的化合物比带有供电子基团的化合物具有更高的抑制潜力。带有硝基的化合物(7h)显示出比其他衍生物更高的抑制潜力,因此,进一步研究了它对中国仓鼠卵巢(CHO)细胞形态的影响,使用相差成像、细胞周期分析和 Annexin-FITC 凋亡检测。处理过的细胞表现出凋亡的特征,即细胞收缩、染色质浓缩和核片段化,并通过将细胞阻滞在 G0 期来诱导细胞增殖的抑制。