地奥司明通过激活 P53 下调 AKT 磷酸化诱导人肾癌细胞 ACHN 凋亡。
Diosmetin Induces Apoptosis by Downregulating AKT Phosphorylation via P53 Activation in Human Renal Carcinoma ACHN Cells.
机构信息
Laboratory of Urology, Guangdong Medical University, Zhanjiang, China
College of Veterinary Medicine, Northwest A&F University, Yangling, China
出版信息
Protein Pept Lett. 2020;27(10):1022-1028. doi: 10.2174/0929866527666200330172646.
BACKGROUND
Diosmetin (DIOS) is the aglycone of the flavonoid glycoside, diosmin, derived naturally from the leaves of the legume, Olea europaea, and Acacia farnesiana. It has potent anticancer activity against multiple forms of cancers. However, the role of DIOS in renal carcinoma and its mechanism of action remain unclear.
OBJECTIVE
The purpose of this study is to investigate the effect of DIOS on cell viability and apoptosis in renal carcinoma cells and explore the possible mechanism of action.
METHODS
Cell viability, cytotoxicity, caspase activity, apoptosis, and expression of apoptotic related proteins were analyzed in renal carcinoma ACHN cells.
RESULTS
The results showed that DIOS inhibited the cell viability, and induced cytotoxicity and apoptosis in ACHN cells. Furthermore, DIOS increased expression of p53 mRNA and proteins, and downregulated phosphorylation of the phosphoinositide 3-kinase and protein B kinase (PI3K/AKT). In addition, it was observed that the anticancer effect of DIOS was significantly enhanced by the p53 activator, but inhibited by the p53 inhibitor.
CONCLUSION
Our data suggested that DIOS induced apoptosis in renal carcinoma ACHN cells by reducing AKT phosphorylation through p53 upregulation.
背景
地奥司明（DIOS）是黄酮糖苷地奥司明的苷元，天然存在于豆科植物油橄榄和金合欢的叶子中。它对多种癌症具有强大的抗癌活性。然而，DIOS 在肾细胞癌中的作用及其作用机制尚不清楚。
目的
本研究旨在探讨 DIOS 对肾癌细胞活力和细胞凋亡的影响，并探讨其可能的作用机制。
方法
分析肾癌细胞 ACHN 中的细胞活力、细胞毒性、半胱天冬酶活性、细胞凋亡和凋亡相关蛋白的表达。
结果
结果表明，DIOS 抑制 ACHN 细胞的细胞活力，并诱导其细胞毒性和细胞凋亡。此外，DIOS 增加了 p53 mRNA 和蛋白的表达，并下调了磷酸肌醇 3-激酶和蛋白 B 激酶（PI3K/AKT）的磷酸化。此外，观察到 p53 激活剂显著增强了 DIOS 的抗癌作用，而 p53 抑制剂则抑制了其作用。
结论
我们的数据表明，DIOS 通过上调 p53 减少 AKT 磷酸化诱导肾癌细胞 ACHN 凋亡。
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