Inhibition Mechanism of Novel Pyrazolo1,5-apyrazin-4(5H)-one Derivatives Against Proliferation of A549 and H322 Cancer Cells

Jin-hui Shao; Gui-hua Feng

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Inhibition Mechanism of Novel Pyrazolo1,5-apyrazin-4(5H)-one Derivatives Against Proliferation of A549 and H322 Cancer Cells

机译：新型吡唑并1,5-a吡嗪-4（5H）-one衍生物对A549和H322癌细胞增殖的抑制机制

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Objective To explore the inhibition mechanism and safety of pyrazolo[1,5-a]pyrazin-4(5H)-one derivatives against proliferation of human lung cancer A549 cells, H322 cells, and human umbilical vein endothelial cell (HUVEC). Methods Cells were treated with 40μmol/L of the ppo3a, ppo3b, ppo3i, and 0.1% DMSO (control) for 48 hours, respectively. Apoptosis was determined by Hoechst 33258 staining assay in H322 and A549 cells. Cell cycle distribution was determined by flow cytometry analysis in A549 cell. LC3-II, p53, and heat shock protein (HSP) 70 protein levels were detected by Western blotting in A549 cells treated with ppo3b for 48 hours. The morphology and viability of HUVEC were observed by inverted microscope and sulforhodamine B (SRB) assay. Results Ppo3a, ppo3b, and ppo3i significantly induced apoptosis in H322 and A549 cells. A strong G1-phase arrest was concomitant with the growth inhibitory effect on A549 cells. Ppo3b effectively elevated the p53 protein level, but significantly reduced the HSP70 protein level. There were no significantly inhibitory effect on the morphology and viability of HUVEC when treated with ppo3a, ppo3b, and ppo3i. Conclusions ppo3a, ppo3b, and ppo3i could inhibit H322 proliferation through apoptosis and inhibit A549 through apoptosis and G1-phase arrest. The protein p53 and HSP70 might involve in the inhibition effects. These derivatives might be a clue to find effective and safe drug for lung cancers.

机译：目的探讨吡唑并[1,5-a]吡嗪-4（5H）-一衍生物对人肺癌A549细胞，H322细胞和人脐静脉内皮细胞（HUVEC）增殖的抑制作用和安全性。方法分别用40μmol/ L的ppo3a，ppo3b，ppo3i和0.1％DMSO（对照）处理细胞48小时。通过Hoechst 33258染色法测定H322和A549细胞中的凋亡。通过流式细胞术分析确定A549细胞中的细胞周期分布。通过蛋白质印迹法在经ppo3b处理48小时的A549细胞中检测到LC3-II，p53和热休克蛋白（HSP）70蛋白水平。倒置显微镜和磺基若丹明B（SRB）检测观察到HUVEC的形态和活力。结果Ppo3a，ppo3b和ppo3i显着诱导H322和A549细胞凋亡。强烈的G1期阻滞伴随着对A549细胞的生长抑制作用。 Ppo3b有效提高了p53蛋白水平，但显着降低了HSP70蛋白水平。用ppo3a，ppo3b和ppo3i处理时，对HUVEC的形态和生存力没有明显的抑制作用。结论ppo3a，ppo3b和ppo3i可通过凋亡抑制H322增殖，并通过凋亡和G1期阻滞抑制A549。蛋白p53和HSP70可能参与了抑制作用。这些衍生物可能是寻找有效且安全的肺癌药物的线索。

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《中国医学科学杂志（英文版）》 |2015年第4期|260-265|共6页
作者
Jin-hui Shao; Gui-hua Feng;
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Department of Medical Morphology, School of Medicine, Hubei University of Art and Science, Xiangyang 441053, Hubei, China;

Department of Medical Morphology, School of Medicine, Hubei University of Art and Science, Xiangyang 441053, Hubei, China;

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Inhibition Mechanism of Novel Pyrazolo1,5-apyrazin-4(5H)-one Derivatives Against Proliferation of A549 and H322 Cancer Cells

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