天津医药

天津医药 ›› 2017, Vol. 45 ›› Issue (6): 566-570.doi: 10.11958/20170369

• 细胞与分子生物学 • 上一篇    下一篇

蛋白激酶 C ζ 抑制剂对皮肤鳞癌细胞 A-431 增殖和 侵袭的影响

邢艳玲 1，吴静 2?   

  1. 1 天津市津南区咸水沽医院皮肤科（邮编 300350）；2 天津市第三中心医院检验科，天津市肝胆疾病研究所，天津市人工细胞重 点实验室，卫生部人工细胞工程技术研究中心
  • 收稿日期:2017-03-24 修回日期:2017-05-16 出版日期:2017-06-15 发布日期:2017-07-05
  • 通讯作者: △通讯作者 E-mail: wujing_821013@sina.com E-mail:wujing_821013@sina.com
  • 作者简介:邢艳玲（1982），女，硕士，主治医师，主要从事皮肤病、性病的研究
  • 基金资助:
    国家自然科学基金青年项目（81301985）；天津市应用基础与前沿技术研究计划青年项目（14JCQNJC14000）；天津市第三中心 医院、卫生部人工细胞工程技术研究中心、天津市人工细胞重点实验室国家自然科学基金孵育项目（2017YNR3）

The effect of PKC ζ inhibitor on the proliferation and invasion of skin squamous carcinoma cell line A-431

XING Yan-ling1, WU Jing2?   

  1. 1 Department of Dermatology, Xianshuigu Hospital Jinnan District, Tianjin 300350, China; 2 Department of Clinical Laboratory, the Third Central Hospital of Tianjin, Tianjin Institute of Hepatobiliary Disease, Tianjin Key Laboratory of Artificial Cell, Artificial Cell Engineering Technology Research Center of Public Health Ministry
  • Received:2017-03-24 Revised:2017-05-16 Published:2017-06-15 Online:2017-07-05
  • Contact: △Corresponding Author E-mail: wujing_821013@sina.com E-mail:wujing_821013@sina.com

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摘要： 目的 探讨蛋白激酶 C（PKC）ζ 抑制剂 T5450996 对皮肤鳞癌细胞 A-431 增殖和侵袭能力的影响。方 法 应用 Z′-LYTE™试剂盒筛选 PKCζ 抑制剂 T5450996；利用细胞增殖实验和细胞周期分析观察 T5450996 对皮肤 鳞癌细胞 A-431 增殖的影响；运用划痕实验和侵袭实验分析 T5450996 对 A-431 迁移和侵袭能力的影响。结果 T5450996 可以抑制 PKCζ 激酶的活性，半数抑制浓度（IC50）约为 35 μmol/L；与对照组相比，35 μmol/L 和 70 μmol/L 的 T5450996 可以显著抑制 A-431 细胞的增殖，阻滞 A-431 细胞周期；划痕实验和侵袭实验结果显示 35 μmol/L 和 70 μmol/L 的 T5450996 处理 A-431 细胞后，A-431 细胞的迁移及侵袭能力明显下降（均 P＜0.05），20 μmol/L 的 T5450996 没有明显作用（均 P＞0.05）。结论 PKCζ 抑制剂 T5450996 可显著抑制皮肤鳞癌细胞 A-431 的增殖和侵 袭能力，是一个有潜在应用前景的小分子抑制剂。

关键词: 蛋白激酶 C, 蛋白激酶抑制剂, 皮肤肿瘤, 细胞增殖, 肿瘤侵润, 肿瘤转移, A-431

Abstract: Objective To investigate the effect of protein kinase C (PKC)ζ inhibitor T5450996 on the proliferation and invasion of skin squamous carcinoma cell line A-431. Methods PKCζ inhibitor T5450996 was screened through Z′-LYTE™ kit. Cell proliferation assay and cell cycle analysis were used to observe the effects of T5450996 on the proliferation of skin squamous carcinoma A-431 cells. Scratch assay and invasion assay were used to explore the effects of T5450996 on the migration and invasion of skin squamous carcinoma A-431 cells. Results The PKCζ inhibitor T5450996 can inhibit the activity of PKCζ kinase, and the IC50 value of T5450996 was about 35 μmol/L. Compared to the control group, 35 μmol/L and 70 μmol/L concentrations of T5450996 significantly suppressed the proliferation of A-431 cells and blocked the cell cycle of A-431 cells. The results of scratch assay and invasion assay indicated that the migration and invasion capacities of A-431 cells were markedly impaired after the treatments with 35 μmol/L and 70 μmol/L concentrations of T5450996 (P＜ 0.05). However, 20 μmol/L concentration of T5450996 showed no significant effect (P＞0.05). Conclusion PKCζ inhibitor T5450996 significantly inhibits the proliferation and invasion capacities of skin squamous carcinoma cell line A- 431, and which may be a small molecular inhibitor with potential applications in the future.

Key words: protein kinase C, protein kinase inhibitors, skin neoplasms, cell proliferation, neoplasm invasiveness, neoplasm metastasis, A-431