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2',4'-二羟基-6'-甲氧基-3',5'-二甲氧基查尔酮对人胰腺癌细胞系的影响。

The Effects of 2',4'-Dihydroxy-6'-methoxy-3',5'- dimethylchalcone from Buds on Human Pancreatic Cancer Cell Lines.

机构信息

Hanoi University of Pharmacy, 13 Le Thanh Tong Street, Hoan Kiem District, Hanoi 100100, Vietnam.

Faculty of Pharmacy, Nguyen Tat Thanh University, 300C Nguyen Tat Thanh Street, District 4, Hochiminh City 72820, Vietnam.

出版信息

Molecules. 2019 Jul 11;24(14):2538. doi: 10.3390/molecules24142538.

Abstract

2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), a principal natural chalcone of buds, suppresses the growth of many types of cancer cells. However, the effects of this compound on pancreatic cancer cells have not been evaluated. In our experiments, we explored the effects of this chalcone on two human pancreatic cancer cell lines. A cell proliferation assay revealed that DMC exhibited concentration-dependent cytotoxicity against PANC-1 and MIA PACA2 cells, with IC values of 10.5 ± 0.8 and 12.2 ± 0.9 µM, respectively. Treatment of DMC led to the apoptosis of PANC-1 by caspase-3 activation as revealed by annexin-V/propidium iodide double-staining. Western blotting indicated that DMC induced proteolytic activation of caspase-3 and -9, degradation of caspase-3 substrate proteins (including poly[ADP-ribose] polymerase [PARP]), augmented bak protein level, while attenuating the expression of bcl-2 in PANC-1 cells. Taken together, our results provide experimental evidence to support that DMC may serve as a useful chemotherapeutic agent for control of human pancreatic cancer cells.

摘要

2',4'-二羟基-6'-甲氧基-3',5'-二甲基查尔酮(DMC)是芽中主要的天然查尔酮,它能抑制多种类型的癌细胞生长。然而,这种化合物对胰腺癌细胞的影响尚未得到评估。在我们的实验中,我们研究了这种查尔酮对两种人胰腺癌细胞系的影响。细胞增殖测定显示,DMC 对 PANC-1 和 MIA PACA2 细胞表现出浓度依赖性细胞毒性,IC 值分别为 10.5±0.8 和 12.2±0.9 μM。用 DMC 处理可通过半胱天冬酶-3 的激活诱导 PANC-1 细胞凋亡,如用 Annexin-V/碘化丙啶双染色所显示的。Western blot 分析表明,DMC 诱导了 caspase-3 和 -9 的蛋白水解激活、caspase-3 底物蛋白(包括多聚(ADP-核糖)聚合酶[PARP])的降解、bak 蛋白水平的增加,同时减弱了 PANC-1 细胞中 bcl-2 的表达。总之,我们的结果提供了实验证据支持 DMC 可能作为一种用于控制人胰腺癌细胞的有用化疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b443/6680674/0401dc4570ef/molecules-24-02538-g001.jpg

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