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

Autor: Jeong Hyung Lee, Pham Thi Kim Lien, Bui Hoang Minh, Phuong Thao Tran, Yen Nhi Nguyen, Manh Hung Tran, Huynh Nhu Tuan, Ha Van Oanh, Quynh Mai Thi Ngo
Rok vydání: 2019
Předmět:
PANC-1
Chalcone
Syzygium
Pharmaceutical Science
pPancreatic cancer
Antineoplastic Agents
Apoptosis
Article
Cleistocalyx operculatus
Analytical Chemistry
lcsh:QD241-441
2′
4′-dihydroxy-6′-methoxy-3′
5′-dimethylchalcone (DMC)

03 medical and health sciences
chemistry.chemical_compound
Chalcones
0302 clinical medicine
lcsh:Organic chemistry
Cell Line
Tumor

Pancreatic cancer
Drug Discovery
medicine
Humans
Propidium iodide
Physical and Theoretical Chemistry
Cytotoxicity
Cell Proliferation
030304 developmental biology
0303 health sciences
Molecular Structure
biology
Caspase 3
Plant Extracts
Cell growth
Organic Chemistry
biology.organism_classification
medicine.disease
Molecular biology
Pancreatic Neoplasms
Gene Expression Regulation
chemistry
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Cancer cell
Molecular Medicine
Biomarkers
Zdroj: Molecules
Volume 24
Issue 14
Molecules, Vol 24, Iss 14, p 2538 (2019)
ISSN: 1420-3049
DOI: 10.3390/molecules24142538
Popis: 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.
Databáze: OpenAIRE
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