Abstract
This study was designed to evaluate the anti-cancer effects of bufalin against the human gastric cancer cells and unveil the underlying mechanism. The results showed that bufalin inhibited the proliferation and colony formation of the MGC-803 gastric cancer cells and exhibited an IC50 of 10 μM. These antiproliferative effects were found to be due to the induction of G2/M cell cycle arrest. The G2/M cell cycle arrest was also concomitant with inhibition of cdc2, cdc25 and cyclin B1. Furthermore, bufalin suppressed the epithelial-to-mesenchymal transition, migration, and invasion of the MGC-803 gastric cancer cells. The Western blot analysis revealed that bufalin exerted its effects via deactivation of EK/ERK signaling pathway. Taken together, these results suggest the potential of bufalin as the lead molecule for the development of chemotherapy for gastric cancer.
Highlights
Gastric cancer is a serious global disease and has been reported to be the 5th most diagnosed human cancer in 2018 (Thrift and El-Serag, 2020)
The percentage of the G2/M phase cells increased from 17.2% in control to 61.0% at 20 μM bufalin
The Western blotting of cell cycle regulatory proteins indicated that the expression of cdc2, Cyclin B1 and cdc25c proteins was highly repressed by bufalin in a dose-dependence manner (Figure 2B)
Summary
Gastric cancer is a serious global disease and has been reported to be the 5th most diagnosed human cancer in 2018 (Thrift and El-Serag, 2020). Despite the application of advanced diagnostic regimes and effective therapeutic modalities, gastric cancer remains generally undetected till advanced stages and the overall 5-year survival rates are still not so encouraging. During the past two decades, rigorous research explorations have led to the identification of many natural compounds with substantial biological effects and anticancer potential against several types of human cancer (Prakash et al, 2013). Bufalin has attained tremendous scientific attention during recent past years because of its anti-cancer effects against a wide range of cancer cell types like lung cancer, liver cancer, gastric cancer (Jiang et al, 2010; Qiu et al, 2013; Wamg et al, 2018). Bufalin was shown to modulate mTOR and ERK-driven signaling cascades in gastric cancer cells (Qi et al, 2019)
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