PHARMACOLOGY AND PHARMACY / BASIC RESEARCH
Therapeutic properties of isoliquiritigenin with molecular modeling studies: investigation of anti-pancreatic acinar cell tumor and HMG-CoA reductase inhibitor activity for treatment of hypercholesterolemia
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1 |
Interventional Radiology Department of Zhuhai Hospital affiliated with Jinan University (Zhuhai People’s Hospital), Zhuhai, Guangdong, China |
2 |
Department of Hepatobiliary Surgery, the First Affiliated Hospital of University of South China, Hengyang, Hunan, China |
3 |
Department of General Surgery, Chongqing Hechuan District Maternal and Child Health Care Hospital, Chongqing, China |
CORRESPONDING AUTHOR
Ping Che
Chongqing Hechuan District Maternal and Child Health Care Hospital, China
Submission date: 2021-12-22
Final revision date: 2021-12-30
Acceptance date: 2021-12-31
Online publication date: 2022-01-15
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ABSTRACT
Introduction:
Isoliquiritigenin, one of the components in the root of Glycyrrhiza glabra L., is a member of the flavonoids, which are known to have anti-tumor activity in vitro and in vivo. HMG-CoA reductase inhibitors, called statins, are used to reduce the risk of heart disease by lowering blood cholesterol levels.
Material and methods:
HMG-CoA Reductase activity according to the method described by Takahashi S. et al. The structure of human HMG-COA reductase in the resolution of 2.22 Å with X-RAY diffraction method (PDB ID: 1HWK) was obtained from the PDB database.
Results:
In our study, inhibition result of Isoliquiritigenin on HMG-CoA reductase showed lower value IC50 = 193.77±14.85 µg / mL. For a better understanding of biological activities and interactions, the molecular docking study was accomplished. The results of molecular docking revealed that isoliquiritigenin with a docking score of -6.740 has a strong binding affinity to the HMG-COA reductase. Therefore, this compound could be considered as a potential inhibitor for the enzyme. Also, the properties of Isoliquiritigenin against common human pancreatic acinar cell tumor cell lines i.e. 266-6, TGP49, and TGP47 were evaluated.
Conclusions:
The cells treated with isoliquiritigenin were assessed by MTT assay for 48 h as regards the cytotoxicity and anti-human pancreatic acinar cell tumor properties in normal (HUVEC) and human pancreatic acinar cell tumor cell lines, i.e. 266-6, TGP49, and TGP47. The IC50 values of isoliquiritigenin were 262, 389, and 211 µg/ml against 266-6, TGP49, and TGP47 cell lines, respectively. The viability of the human pancreatic acinar cell tumor cell line decreased dose-dependently in the presence of isoliquiritigenin. After clinical study, isoliquiritigenin can be utilized as an efficient drug in the treatment of human pancreatic acinar cell tumor in humans.