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

1
Hanoi University of Pharmacy, 13 Le Thanh Tong Street, Hoan Kiem District, Hanoi 100100, Vietnam
2
Faculty of Pharmacy, Nguyen Tat Thanh University, 300C Nguyen Tat Thanh Street, District 4, Hochiminh City 72820, Vietnam
3
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
5
Faculty of Biology and Biotechnology, University of Science, Vietnam National University Hochiminh City, 227 Nguyen Van Cu, District 5, Hochiminh City 748000, Vietnam
6
Biomedical Sciences Department, Institute for Research & Executive Education (VNUK), The University of Danang, 158A Le Loi, Hai Chau District, Danang City 551000, Vietnam
*
Author to whom correspondence should be addressed.
These authors contributed equally to this research.
Academic Editor: Pinarosa Avato
Molecules 2019, 24(14), 2538; https://doi.org/10.3390/molecules24142538
Received: 3 May 2019 / Revised: 29 June 2019 / Accepted: 8 July 2019 / Published: 11 July 2019
(This article belongs to the Special Issue Natural Products and Drug Discovery)
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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. View Full-Text
Keywords: Cleistocalyx operculatus; 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC); pPancreatic cancer; PANC-1 Cleistocalyx operculatus; 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone (DMC); pPancreatic cancer; PANC-1
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Tuan, H.N.; Minh, B.H.; Tran, P.T.; Lee, J.H.; Oanh, H.V.; Ngo, Q.M.T.; Nguyen, Y.N.; Lien, P.T.K.; Tran, M.H. The Effects of 2′,4′-Dihydroxy-6′-methoxy-3′,5′- dimethylchalcone from Cleistocalyx operculatus Buds on Human Pancreatic Cancer Cell Lines. Molecules 2019, 24, 2538.

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