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  • Open Access

11 July 2019

11 Pages

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

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1
Hanoi University of Pharmacy, 13 Le Thanh Tong Street, Hoan Kiem District, Hanoi 100100, Vietnam
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Faculty of Pharmacy, Nguyen Tat Thanh University, 300C Nguyen Tat Thanh Street, District 4, Hochiminh City 72820, Vietnam
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Department of Biochemistry, College of Natural Sciences, Kangwon National University, Chuncheon, Gangwon-Do 24414, Korea
4
College of Pharmacy, Hai Phong University of Medicine and Pharmacy, 72A Nguyen Binh Khiem, Hai Phong 180000, Vietnam
This article belongs to the Special Issue Natural Products and Drug Discovery

Abstract

2′,4′-Dihydroxy-6’-methoxy-3′,5′-dimethylchalcone (DMC), a principal natural chalcone of Cleistocalyx operculatus 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 IC50 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.

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