Betulonic Acid, as One of the Active Components of the Celastrus orbiculatus Extract, Inhibits the Invasion and Metastasis of Gastric Cancer Cells by Mediating Cytoskeleton Rearrangement In Vitro

Abstract

Gastric cancer is a type of malignant tumor that seriously threatens human life and health. Invasion and metastasis present difficulties in the treatment of gastric cancer, and the remodeling of the tumor cytoskeleton plays an important role in mediating the ability of tumor cells to achieve invasion and metastasis. Previous experimental results suggest that Celastrus orbiculatus extract can regulate cytoskeletal remodeling in gastric cancer, but the active component has not been determined. Betulonic acid, as an effective component of COE, inhibits the invasion and metastasis of gastric cancer cells by regulating cytoskeletal remodeling in vitro; its specific mechanisms have been studied here. After betulonic acid was dissolved, it was diluted to various working concentrations in RPMI-1640 medium and added to AGS, HGC-27 and GES-1 cell lines. Cell viability was assessed by CCK-8 and colony formation assays. Cytoskeleton staining was used to detect changes in cytoskeleton morphology. Functional assays including wound healing assays and transwell assays were used to detect the invasion and migration of cells. The effect of betulonic acid on cell invasion and migration was clearly and precisely observed by high-content imaging technology. Western blotting was used to detect the regulation of matrix metalloproteinase-related proteins and epithelial–mesenchymal transformation-related proteins. We found that betulonic acid inhibited the migration and invasion of gastric cancer cells. Therefore, betulonic acid inhibits the invasion and metastasis of gastric cancer cells by mediating cytoskeletal remodeling and regulating epithelial mesenchymal transformation.

Evaluation of the in vitro antioxidant and antitumor activity of extracts from Camellia fascicularis leaves

“…At 250 μg/ml, the viability of HGC27 cells treated with PEE, EAE, and WE was 31.96 ± 3.26%, 39.67 ± 0.78%, and 27.92 ± 2.79%, respectively. The respective EC 50 values of PEE, EAE, and WE were 167.44 ± 8.09, 200.76 ± 11.34, and 147.42 ± 12.42 μg/ml, which were higher than the EC 50 values of betulonic acid (34.13 μg/ml) against HGC27 cell ( Chu et al, 2022 ). Notably, WE showed the smallest EC 50 against HCCLM6 and HGC27 cells, indicating its strongest inhibitory activity.…”

Oxime derivatives of betulonic acid and platanic acid as novel cytotoxic or antiviral agents

“…4.1.18. (3β)-3-(Acetyloxy)-20-oxo-29-norlupan-28-oic acid (18). Acetic anhydride (300 μL; 3.14 mmol) and DMAP (35 mg; 0.28 mmol) were added to a solution of platanic acid (2; 1 g; 2.18 mmol) in THF (10 mL) and triethylamine (1 mL), and the reaction mixture was stirred at 90 °C using a Dimroth condenser under an argon atmosphere for 3 h. The reaction was stopped by the addition of water (10 mL) and left to stir at r.t. for an additional 2 h. Brine was added, and the organic layer was extracted with chloroform.…”

“…16 Betulonic acid, 3-oxo-lup-20(29)-en-28-oic acid (1; Scheme 1), belongs to the lupane family of plant triterpenoids and is found in different plant species. 17,18 Mostly, the content of betulonic acid in the plant sources is low, and, therefore a semisynthetic oxidation procedure from betulin often takes place to obtain betulonic acid in a higher quantity. 19 The solubility of betulonic acid in aqueous media is low, and so is its bioavailability.…”