Division of Breast and Thyroid Surgical Oncology, Department of Surgery, St. Vincent's Hospital, College of Medicine, The Catholic University of Korea, Suwon, Gyeonggi 16247, Republic of Korea.
Mol Med Rep. 2018 Apr;17(4):5581-5588. doi: 10.3892/mmr.2018.8580. Epub 2018 Feb 8.
The Janus kinase (JAK)1 and JAK2 inhibitor, ruxolitinib, and the active form of vitamin D (calcitriol) were previously reported to possess anticancer effects in breast cancer. The present study investigated the combined effects of ruxolitinib and calcitriol on an estrogen receptor (ER)‑positive, human epidermal growth factor receptor 2 (HER2)‑positive, breast cancer cell line. The ER and HER2‑positive MCF7‑HER18 breast cancer cell line was used to investigate the combination effect of ruxolitinib and calcitriol. A bromodeoxyuridine (BrdU) assay was used to investigate cell growth inhibition. The synergism of this combination therapy was examined using the Chou‑Talalay method. Cell cycle analysis was performed by flow cytometry, and apoptosis was evaluated by flow cytometry following Annexin V‑fluorescein isothiocyanate (FITC) and propidium iodide (PI) staining. Alterations in protein expression levels were analyzed by western blotting. The BrdU assay indicated that combination treatment using ruxolitinib and calcitriol produced a synergistic anti‑proliferative effect in MCF7‑HER18 breast cancer cells. Annexin V‑FITC/PI staining and cell cycle analysis identified a synergistic increase in apoptosis and sub‑G1 arrest in the presence of ruxolitinib and calcitriol. Western blot analysis revealed that these synergistic effects of ruxolitinib and calcitriol were associated with reduced protein levels of JAK2, phosphorylated JAK2, c‑Myc proto oncogene protein, cyclin‑D1, apoptosis regulator Bcl‑2 and Bcl‑2‑like protein 1, and with increased levels of caspase‑3 and Bcl‑2‑associated agonist of cell death proteins. The results of the present study demonstrated the synergistic anticancer effects of ruxolitinib and calcitriol in ER and HER2‑positive MCF7‑HER18 breast cancer cells. Based on these findings, ruxolitinib and calcitriol may have potential as a combination therapy for patients with ER and HER2‑positive breast cancer.
Janus 激酶 (JAK)1 和 JAK2 抑制剂芦可替尼和活性维生素 D(骨化三醇)先前已被报道在乳腺癌中具有抗癌作用。本研究探讨了芦可替尼和骨化三醇联合应用对雌激素受体 (ER) 阳性、人表皮生长因子受体 2 (HER2) 阳性的乳腺癌细胞系的影响。使用 ER 和 HER2 阳性 MCF7-HER18 乳腺癌细胞系来研究芦可替尼和骨化三醇联合用药的效果。溴脱氧尿苷 (BrdU) 检测法用于检测细胞生长抑制情况。采用 Chou-Talalay 法检测这种联合治疗的协同作用。通过流式细胞术进行细胞周期分析,并用 Annexin V-荧光素异硫氰酸酯 (FITC) 和碘化丙啶 (PI) 染色后通过流式细胞术评估细胞凋亡。通过 Western blot 分析检测蛋白表达水平的变化。BrdU 检测法表明,芦可替尼和骨化三醇联合治疗在 MCF7-HER18 乳腺癌细胞中产生了协同的抗增殖作用。Annexin V-FITC/PI 染色和细胞周期分析表明,在存在芦可替尼和骨化三醇的情况下,凋亡和亚 G1 期阻滞协同增加。Western blot 分析显示,芦可替尼和骨化三醇的这些协同作用与 JAK2、磷酸化 JAK2、c-Myc 原癌蛋白、细胞周期蛋白 D1、凋亡调节蛋白 Bcl-2 和 Bcl-2 样蛋白 1 的蛋白水平降低以及 caspase-3 和细胞死亡相关蛋白 Bcl-2 激动剂蛋白水平升高有关。本研究结果表明,芦可替尼和骨化三醇在 ER 和 HER2 阳性 MCF7-HER18 乳腺癌细胞中具有协同的抗癌作用。基于这些发现,芦可替尼和骨化三醇可能有潜力作为 ER 和 HER2 阳性乳腺癌患者的联合治疗药物。