Department of General Surgery, The First Hospital of China Medical University, Shenyang, Liaoning 110001, P.R. China.
Department of General Surgery, The First Affiliated Hospital of Jinzhou Medical University, Jinzhou, Liaoning 121000, P.R. China.
Int J Mol Med. 2018 Nov;42(5):2700-2708. doi: 10.3892/ijmm.2018.3850. Epub 2018 Aug 31.
The increased expression of sialyl-Lewisx (SLex) epitope on the surface of tumor cells has been known for decades. However, genetic manipulation of the expression of SLex and the role of SLex in cancer cell proliferation remains to be fully elucidated. The present study suggested that the monoclonal antibody of SLex (KM93) significantly inhibited the proliferation of human hepatocarcinoma (HCC) cells. The expression levels of three sialyl‑Lewis oligosaccharide antigens, SLex, SLea and dimeric SLex (SDLex), were determined on the cell surface of the MHCC97 human HCC cell line. The expression of SLex was markedly higher in MHCC97 cells than in normal liver cells. The expression of SDLex was also relatively high, however, no significant difference was observed between normal liver cells and HCC cells. The expression of SLea was only detected in trace quantities. Fucosyltransferase (FUT) is the key enzyme of the fucosylation step in the biosynthesis of sialyl‑Lewis oligosaccharide antigens. Therefore, the present study investigated the expression of FUTs. It was found that the mRNA and protein expression levels of FUT7 were high in the MHCC97 HCC cell line compared with levels in normal liver cells. FUT6 was also expressed at a high level, although the difference was not statistically significant between MHCC97 cells and normal liver cells. No expression of FUT3 was detected. The results were consistent with the change insialyl‑Lewis antigens. The effects of FUT7 small interfering (si)RNA transfection on the expression of FUT7, expression of SLex and MHCC97 cell proliferation were also examined. Following FUT7 siRNA transfection, the expression of FUT7 was markedly downregulated, as determined by western blot and reverse transcription‑quantitative polymerase chain reaction methods. The results from flow cytometry showed that the synthesis of SLex was also inhibited, which was consistent with the downregulated expression of FUT7. MHCC97 cell proliferation was also significantly inhibited following FUT7 siRNA transfection, which was correlated with suppression of the S‑phase in cell cycle progression. By using inhibitors of various signaling pathways, it was found that the knockdown of FUT7 inhibited the activation of phospholipase Cγ (PLCγ) by inhibiting the translocation and phosphorylation of PLCγ. In conclusion, the results suggested that FUT7 has animportant functional role in human HCC cell proliferation by controlling cell cycle progression via the PLCγ/extracellular signal‑regulated kinase signaling pathway. The inhibition of SLex and FUT7 siRNA transfection may provide a novel therapeutic methodology to treat tumors that express SLex glycoconjugates.
肿瘤细胞表面唾液酸化路易斯 X(SLex)表位的过度表达已为人所知数十年。然而,SLex 的表达的遗传调控及其在癌细胞增殖中的作用仍有待充分阐明。本研究表明,SLex 的单克隆抗体(KM93)可显著抑制人肝癌(HCC)细胞的增殖。在 MHCC97 人 HCC 细胞系的细胞表面上测定了三种唾液酸化Lewis 寡糖抗原、SLex、SLea 和二聚体 SLex(SDLex)的表达水平。SLex 的表达在 MHCC97 细胞中明显高于正常肝细胞。SDLex 的表达也相对较高,但正常肝细胞与 HCC 细胞之间无明显差异。仅检测到 SLea 的痕量表达。岩藻糖基转移酶(FUT)是唾液酸化 Lewis 寡糖抗原生物合成中岩藻糖基化步骤的关键酶。因此,本研究调查了 FUTs 的表达。结果发现,与正常肝细胞相比,MHCC97 HCC 细胞系中 FUT7 的 mRNA 和蛋白表达水平较高。FUT6 的表达水平也较高,尽管 MHCC97 细胞与正常肝细胞之间无统计学差异。未检测到 FUT3 的表达。结果与唾液酸化 Lewis 抗原的变化一致。还检查了 FUT7 小干扰(si)RNA 转染对 FUT7 表达、SLex 表达和 MHCC97 细胞增殖的影响。FUT7 siRNA 转染后,通过 Western blot 和逆转录-定量聚合酶链反应方法明显下调 FUT7 的表达。流式细胞术的结果表明,SLex 的合成也受到抑制,这与 FUT7 的下调表达一致。FUT7 siRNA 转染后,MHCC97 细胞增殖也受到显著抑制,这与细胞周期 S 期进展中细胞周期的抑制有关。通过使用各种信号通路的抑制剂,发现通过抑制 PLCγ 的易位和磷酸化,FUT7 的敲低抑制了磷脂酶 Cγ(PLCγ)的激活。总之,研究结果表明,FUT7 通过 PLCγ/细胞外信号调节激酶信号通路控制细胞周期进展,在人 HCC 细胞增殖中具有重要的功能作用。SLex 和 FUT7 siRNA 转染的抑制可能为治疗表达 SLex 糖缀合物的肿瘤提供一种新的治疗方法。