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槲皮素通过抑制特异性蛋白1(Sp1)诱导对人肝癌(HepG2)细胞的抗增殖活性。

Quercetin Induces Antiproliferative Activity Against Human Hepatocellular Carcinoma (HepG2) Cells by Suppressing Specificity Protein 1 (Sp1).

作者信息

Lee Ra Ham, Cho Jin Hyoung, Jeon Young-Joo, Bang Woong, Cho Jung-Jae, Choi Nag-Jin, Seo Kang Seok, Shim Jung-Hyun, Chae Jung-Il

机构信息

Department of Oral Pharmacology, School of Dentistry and Institute of Oral Bioscience, BK21 plus, Chonbuk National University, Jeonju, 651-756.

Department of Pharmacy, Natural Medicine Research Institute, College of Pharmacy, Mokpo National University, Muan-gun, Jeonnam, 534-729.

出版信息

Drug Dev Res. 2015 Feb;76(1):9-16. doi: 10.1002/ddr.21235. Epub 2015 Jan 25.

Abstract

Preclinical Research Quercetin, found in red onions and red apple skin can induce apoptosis insome malignant cells. However, the apoptotic effect of quercetin in hepatocellular carcinoma HepG2 cells via regulation of specificity protein 1 (Sp1) has not been studied. Here, we demonstrated that quercetin decreased cell growth and induce apoptosis in HepG2 cells via suppression of Sp1 using 3-(4,5-dimethyl-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay, 4',6-diamidino-2-phenylindole (DAPI) staining, Annexin V, and Western blot analysis, an effect that was dose- and time-dependent manner. Treatment of HepG2 cells with quercetin reduced cell growth and induced apoptosis, followed by regulation of Sp1 and Sp1 regulatory protein. Taken together, the results suggest that quercetin can induce apoptotic cell death by regulating cell cycle and suppressing antiapoptotic proteins. Therefore, quercetin may be useful for cancer prevention. Drug Dev Res 76 : 9-16, 2015.

摘要

临床前研究

红洋葱和红苹果皮中含有的槲皮素可诱导某些恶性细胞凋亡。然而,槲皮素通过调节特异性蛋白1(Sp1)对肝癌HepG2细胞凋亡的影响尚未得到研究。在此,我们通过使用3-(4,5-二甲基-2-噻唑基)-5-(3-羧甲氧基苯基)-2-(4-磺基苯基)-2H-四唑鎓内盐(MTS)测定法、4',6-二脒基-2-苯基吲哚(DAPI)染色、膜联蛋白V和蛋白质印迹分析,证明槲皮素通过抑制Sp1降低HepG2细胞的生长并诱导其凋亡,且该效应呈剂量和时间依赖性。用槲皮素处理HepG2细胞可降低细胞生长并诱导凋亡,随后调节Sp1及其调节蛋白。综上所述,结果表明槲皮素可通过调节细胞周期和抑制抗凋亡蛋白诱导凋亡性细胞死亡。因此,槲皮素可能对癌症预防有用。《药物研发研究》76: 9 - 16, 2015年。

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