Alpinetin: anti-human gastric cancer potential and urease inhibition activity in vitro

Abstract

Introduction Alpinetin is the bioactive component of a traditional Chinese medicine. This compound, one of the main constituents of the seeds of Alpinia katsumadai Hayata, is a member of the flavonoids, with anti-inflammatory, antibacterial, and other significant therapeutic activities of important potency and low systemic toxicity. Material and methods In our study, the inhibitory effect of isoliquiritigenin on HMG-CoA reductase showed a lower value of IC50 = 21.86 ±1.44 µg/ml. A molecular docking study was performed as a complementary study to provide additional data about the biological activities of alpinetin in the presence of urease. The docking calculations revealed that alpinetin with a docking score of –5.097 (kcal/mol) has an acceptable binding affinity to the enzyme, and because of various hydrophobic contacts and hydrogen bonds created by this chemical compound, alpinetin could be considered as an adequate inhibitor of urease. Results In the cellular and molecular part of the study, the cells treated with alpinetin were assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay for 48 h as regards the cytotoxicity and anti-human gastric carcinoma properties towards normal (human umbilical vein endothelial cells (HUVECs)) and gastric carcinoma cell lines, i.e. SNU-1, Hs 746T, and KATO III. The IC50 values of alpinetin were 426, 586, and 424 µg/ml against SNU-1, Hs 746T, and KATO III cell lines, respectively. The viability of the malignant gastric cell line decreased dose-dependently in the presence of alpinetin. Conclusions It seems that the anti-human gastric carcinoma effect of the investigated molecule is due to its antioxidant effects.

Keywords

• alpinetin
• anti-human gastric cancer
• urease
• molecular docking
• enzyme inhibition