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利匹韦林(LEE011)与 5-氟尿嘧啶对人结直肠癌细胞的协同抗增殖作用。

Synergistic Antiproliferative Effect of Ribociclib (LEE011) and 5-Fluorouracil on Human Colorectal Cancer.

机构信息

School of Medicine for International Students, I-Shou University, Kaohsiung, Taiwan, R.O.C.

Department of Nursing, School of Medicine, I-Shou University, Kaohsiung, Taiwan, R.O.C.

出版信息

Anticancer Res. 2020 Nov;40(11):6265-6271. doi: 10.21873/anticanres.14647.

DOI:10.21873/anticanres.14647
PMID:33109564
Abstract

BACKGROUND/AIM: Colorectal cancer (CRC) is one of the most common malignant tumors in the world. This study aimed to investigate the anticancer effect of the combination treatment of Ribociclib (LEE011) and 5-Fluorouracil (5-FU) on CRC cells.

MATERIALS AND METHODS

HT-29 and SW480 cells were treated with LEE011, 5-FU, or the combination of LEE011 and 5-FU. Cell viability and cycle were investigated through 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assay and flow cytometry. The expression of cell cycle-related proteins was determined through western blot.

RESULTS

The combined treatment of LEE011 with 5-FU synergistically reduced cell viability in HT-29 and SW480 cells. Specifically, it induced cell cycle arrest at the G phase, down-regulated the phosphorylation of retinoblastoma protein and the expression of p53.

CONCLUSION

LEE011 exhibited potential as an effective therapeutic inhibitor for the combination treatment of CRC patients.

摘要

背景/目的:结直肠癌(CRC)是世界上最常见的恶性肿瘤之一。本研究旨在探讨利匹韦林(LEE011)联合 5-氟尿嘧啶(5-FU)治疗结直肠癌细胞的抗癌作用。

材料与方法

采用 LEE011、5-FU 或 LEE011 和 5-FU 联合处理 HT-29 和 SW480 细胞。通过 3-(4,5-二甲基噻唑-2-基)-5-(3-羧甲氧基苯基)-2-(4-磺苯基)-2H-四唑比色法和流式细胞术检测细胞活力和细胞周期。通过 Western blot 检测细胞周期相关蛋白的表达。

结果

LEE011 与 5-FU 联合治疗协同降低 HT-29 和 SW480 细胞的活力。具体而言,它诱导细胞周期在 G 期停滞,下调视网膜母细胞瘤蛋白的磷酸化和 p53 的表达。

结论

LEE011 作为 CRC 患者联合治疗的有效治疗抑制剂具有潜力。

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Immunotargets Ther. 2025 Jan 30;14:65-85. doi: 10.2147/ITT.S499680. eCollection 2025.
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Cyclin-Dependent Kinase Inhibitors and Their Therapeutic Potential in Colorectal Cancer Treatment.
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Front Pharmacol. 2021 Dec 21;12:757120. doi: 10.3389/fphar.2021.757120. eCollection 2021.