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Teglicar Induces Apoptosis in HeLa Cervical Cancer Cells via Endoplasmic Reticulum Stress-Mediated Pathway
Iranian Journal of Science and Technology, Transactions A: Science ( IF 1.7 ) Pub Date : 2020-07-23 , DOI: 10.1007/s40995-020-00940-1
Rui Zhang , Dunli Nie , Yan Chen , Yunlan Zeng , Yu Huang , Ning Xiao

Carnitine palmitoyltransferase 1A (CPT1A) is a potential therapeutic target for several cancers. The inhibition of CPT1A has anticancer effects. Teglicar is a new reversible CPT1A inhibitor. The aim of this research was to expound the effect of teglicar in cervical cancer cells. Cell proliferation was conducted using the CCK8 assay. The apoptotic rate was examined by Annexin V-APC/PI staining and flow cytometry. The expression levels of apoptosis-related proteins and endoplasmic reticulum (ER) stress-related proteins were determined by western blot assay. Teglicar was found to inhibit the proliferation of HeLa cells in a dose-dependent manner, with an IC50 value of 18.38 µM at 24 h. The apoptotic rate of HeLa cells was significantly increased following treatment with teglicar. Western blot analysis indicated that the treatment of teglicar enhanced ER stress and apoptosis in HeLa cells. However, inhibition of proliferation and enhancement of apoptosis in teglicar-treated HeLa cells was reversed by 4-PBA. These results revealed that teglicar promoted apoptosis of HeLa cells via ER stress.

中文翻译:

Teglicar通过内质网应激介导的途径诱导HeLa宫颈癌细胞凋亡。

肉碱棕榈酰转移酶1A(CPT1A)是几种癌症的潜在治疗靶标。CPT1A的抑制作用具有抗癌作用。Teglicar是一种新型的可逆CPT1A抑制剂。这项研究的目的是阐明teglicar在宫颈癌细胞中的作用。使用CCK8测定法进行细胞增殖。通过膜联蛋白V-APC / PI染色和流式细胞术检查细胞凋亡率。Western blot法检测凋亡相关蛋白和内质网应激相关蛋白的表达水平。发现Teglicar具有IC 50呈剂量依赖性抑制HeLa细胞增殖24小时后的值为18.38 µM。teglicar治疗后,HeLa细胞的凋亡率显着增加。蛋白质印迹分析表明,teglicar处理可增强HeLa细胞的内质网应激和细胞凋亡。但是,4-PBA可逆转teglicar处理的HeLa细胞的增殖抑制作用和凋亡的增强作用。这些结果表明,teglicar通过内质网应激促进HeLa细胞凋亡。
更新日期:2020-07-23
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