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

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.

• Authors: Huynh Nhu Tuan, Bui Hoang Minh, Phuong Thao Tran, Jeong Hyung Lee, Ha Van Oanh, Quynh Mai Thi Ngo, Yen Nhi Nguyen, Pham Thi Kim Lien, Manh Hung Tran
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 24 Issue 14 (Jul 11 2019) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 31336786 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Biomarkers
• Chalcones
• Plant Extracts
• CASP3 protein, human
• Caspase 3

Topics

• Antineoplastic Agents (chemistry, pharmacology)
• Apoptosis (drug effects, genetics)
• Biomarkers
• Caspase 3 (metabolism)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Chalcones (chemistry, pharmacology)
• Gene Expression Regulation
• Humans
• Molecular Structure
• Pancreatic Neoplasms
• Plant Extracts (chemistry, pharmacology)
• Syzygium (chemistry)