Carbenoxolone disodium suppresses the migration of gastric cancer by targeting HDAC6.
Carbenoxolone disodium suppresses the migration of gastric cancer by targeting HDAC6.
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DOI：
10.4155/fmc-2022-0246
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发表时间：
2023-03
影响因子：
4.2
通讯作者：
Zhiyu Song;Chenglong Zhao;Jingjing Yan;Dandan Jiang;Gang Jia
中科院分区：
文献类型：
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作者：
Zhiyu Song;Chenglong Zhao;Jingjing Yan;Dandan Jiang;Gang Jia
目的：由于胃癌的严重发病率和死亡率，寻找新的候选药物已成为一个迫切的问题。组蛋白去乙酰化酶6（HDAC 6）与胃癌的密切关系使得开发以HDAC 6为靶点的抗胃癌药物成为一个可行的思路。方法与结果：甘珀酸二钠是一种新的HDAC 6抑制剂。细胞热位移实验、表面等离子体共振实验和分子对接实验证实了其与HDAC 6的结合能力。细胞活力、创伤愈合和transwell实验以及动物实验均表明甘珀酸钠在体内外均能抑制胃癌细胞MGC-803的增殖和迁移。结论：这是第一份报告表明甘珀酸二钠可能是一种HDAC 6抑制剂，具有治疗胃癌的潜力。
Aim: Because of the severe morbidity and mortality of gastric cancer, discovering new candidate drugs has been an urgent issue. The close association between histone deacetylase 6 (HDAC6) and gastric cancer makes the development of HDAC6-targeted anti-gastric cancer drugs a viable idea. Methods & results: Carbenoxolone disodium was identified as a novel HDAC6 inhibitor. Cellular thermal shift assay, surface plasmon resonance assay and molecular docking confirmed its binding ability to HDAC6. Cell viability, wound healing and transwell assays as well as animal studies have demonstrated that carbenoxolone disodium could block the proliferation and migration of gastric cancer cells MGC-803 in vitro and in vivo. Conclusion: This is the first report to indicate that carbenoxolone disodium could be an HDAC6 inhibitor with potential for treatment of gastric cancer.