Objective To investigate the mechanism of gossypol taurine induced apoptosis of liver cancerous HepG2 cells based on phosphatidylinositol⁃3 kinase (PI3K)/serine/threonine protein kinase (AKT) signaling pathway. Methods (1) After 24⁃hour intervention on liver cancerous HepG2 cells by gossypol taurine with different concentrations of 0 μg/mL, 25 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL, 125 μg/mL, and 150 μg/mL, the CCK⁃8 method was employed to detect survival rate of cells, to calculate median inhibition concentration of gossypol taurine on liver cancerous HepG2 cells, and to screen intervention concentration of gossypol taurine. (2) After 24⁃hour intervention on liver cancerous HepG2 cells by 0 μg/mL, 25 μg/mL, 50 μg/mL, and 100 μg/mL gossypol taurine (setting as 0 μg/mL gossypol taurine group, 25 μg/mL gossypol taurine group, 50 μg/mL gossypol taurine group, or 100 μg/mL gossypol taurine group, respectively), cell apoptosis and cell cycle were detected by employing the flow cytometry, the real⁃time fluorescent quantitative PCR was used to detect mRNA expressions of B⁃cell lymphoma 2⁃associated X protein (Bax), B⁃cell lymphoma 2 (Bcl⁃2), Caspase⁃3, PI3K, and AKT, and the Western blot was employed to detect protein expressions of apoptosis⁃associated protein Bax, Bcl⁃2, Caspase⁃3, and PI3K/AKT signaling pathway⁃associated protein PI3K, phosphorylated PI3K (p⁃PI3K), AKT, and phosphorylated AKT (p⁃AKT). Results (1) Compared with 0 μg/mL gossypol taurine, the survival rate of liver cancerous HepG2 cells after intervention by 25 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL, 125 μg/mL, and 150 μg/mL gossypol taurine was declined (P<0.05). The median inhibition concentration of liver cancerous HepG2 cells after 24⁃hour intervention by gossypol taurine was 108 μg/mL. Therefore, 25 μg/mL, 50 μg/mL, and 100 μg/mL were selected as the intervention concentrations of gossypol taurine in subsequent experiments. (2) Compared with the 0 μg/mL gossypol taurine group, the 25 μg/mL, 50 μg/mL, and 100 μg/mL gossypol taurine groups exhibited elevated early apoptosis rate and total apoptosis rate of liver cancerous HepG2 cells, and up⁃regulated cell proportion in G0/G1 phase (P<0.05); furthermore, compared with the 0 μg/mL gossypol taurine group, the 50 μg/mL and 100 μg/mL gossypol taurine groups yielded elevated advanced apoptosis rate of liver cancerous HepG2 cells, and the cell proportion in G2/M phase was declined (P<0.05). Compared with the 0 μg/mL gossypol taurine group, the 50 μg/mL and 100 μg/mL gossypol taurine groups demonstrated up⁃regulated mRNA and protein expressions of Bax and Caspase⁃3 in liver cancerous HepG2 cells, while down⁃regulated mRNA and protein expressions of Bcl⁃2; in addition, compared with the 0 μg/mL gossypol taurine group, the 25 μg/mL, 50 μg/mL, and 100 μg/mL gossypol taurine groups depicted down⁃regulated mRNA expressions of PI3K and AKT in liver cancerous HepG2 cells, and the 50 μg/mL and 100 μg/mL gossypol taurine groups expressed down⁃regulated protein expressions of p⁃PI3K, AKT, p⁃AKT in liver cancerous HepG2 cells (P<0.05). Conclusion Gossypol taurine can up regulate expressions of Bax, Caspase⁃3, and down regulate Bcl⁃2 expression, so as to inhibit proliferation of liver cancerous HepG2 cells, induce their apoptosis through inhibiting the activation of PI3K/AKT signaling pathway.

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