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Differential effects of synthesized 2′-oxygenated chalcone derivatives: modulation of human cell cycle phase distribution

机译：合成的2'-氧化查尔酮衍生物的差异作用：调节人类细胞周期的相位分布

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摘要

Ten structurally related 2′-oxygenated chalcone derivatives, bearing either hydroxy and/or methoxy substituents on the A and B rings, were synthesized through Claisen-Schmidt condensation. The synthesis procedure was relatively easy and had an acceptable yield. The in vitro cytotoxicities of these compounds against the human tumor cells such as Jurkat, U937 cells, and normal cells PHA stimulated PBMCs were investigated. Among those, compounds 1 (IC_(50) = 2.5 μM), 2 (1.7 μM), and 8 (3.2 μM) showed potent inhibitory activity toward Jurkat cell line. In parallel, compounds 1 (6.7 μM), 2 (1.5 μM), and 10 (5.3 μM) showed the highest activity against U937 cell line. However, the chalcones also inhibit the PHA stimulated PBMCs cells, but the IC_(50) values were relatively high when compared to the tumor cell line values. Studies were also on the effect of synthesized chalcones on the cell cycle phase distribution. In Jurkat cell line, compounds 7 and 9 showed the highest activity and the most striking effect in reduction of the percentage of cells in the S phase, which was associated with an increase of cells in G2/M phase. In U937 cell line, compound 3 increased the proportion of cells in the G0/G1 phase and reduced the proportion in S phase. In contrast, compounds 1, 9, and 10 showed a decrease effect on the percentage of cells in S phase and an increase effect on the percentage of cells in the G2/M phase of the cell cycle. Whereas in the case of PHA stimulated PBMCs, compounds 1, 4, 8, and 10 increased the percentage of cells in G2/M phase, which was associated with a decrease effect in the S phase of the cell cycle.
机译：通过克莱森-施密特缩合反应，合成了十个在A和B环上带有羟基和/或甲氧基取代基的结构相关的2'-氧化查耳酮衍生物。合成过程相对容易并且具有可接受的产率。研究了这些化合物对人类肿瘤细胞（如Jurkat，U937细胞和正常细胞，经PHA刺激的PBMC）的体外细胞毒性。在这些化合物中，化合物1（IC_（50）= 2.5μM），化合物2（1.7μM）和化合物8（3.2μM）对Jurkat细胞系表现出有效的抑制活性。同时，化合物1（6.7μM），2（1.5μM）和10（5.3μM）对U937细胞系表现出最高活性。但是，查耳酮也抑制PHA刺激的PBMCs细胞，但与肿瘤细胞系值相比，IC_（50）值相对较高。还研究了合成查耳酮对细胞周期相分布的影响。在Jurkat细胞系中，化合物7和9在降低S期细胞百分比方面表现出最高的活性和最显着的作用，这与G2 / M期细胞的增加有关。在U937细胞系中，化合物3增加了G0 / G1期细胞的比例，减少了S期细胞的比例。相反，化合物1、9和10对细胞周期处于S期的细胞百分数显示出降低的作用，并且对细胞周期的G2 / M期对细胞的百分数显示出增加的作用。而在PHA刺激的PBMC中，化合物1、4、8和10增加了G2 / M期细胞的百分比，这与细胞周期S期的作用降低有关。

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