Fan Lu, Xiao Qingling, Chen Yanyan, Chen Gang, Duan Jinao, Tao Weiwei
School of Medicine and Life Sciences, Nanjing University of Chinese MedicineNanjing, China.
School of Basic Biomedical Science, Nanjing University of Chinese MedicineNanjing, China.
Front Pharmacol. 2017 Jun 29;8:424. doi: 10.3389/fphar.2017.00424. eCollection 2017.
Hepatocellular carcinoma (HCC) is a malignant primary liver cancer with poor prognosis. In the present study, we report that pekinenin E (PE), a casbane diterpenoid derived from the roots of , has a strong antitumor activity against human HCC cells both and . PE suppressed the growth of human HCC cells Hep G2 and SMMC-7721. In addition, PE-mediated endoplasmic reticulum (ER) stress caused increasing expressions of C/EBP homologous protein (CHOP), leading to apoptosis in HCC cells both and . Inhibition of ER stress with CHOP small interfering RNA or 4-phenyl-butyric acid partially reversed PE-induced cell death. Furthermore, PE induced S cell cycle arrest, which could also be partially reversed by CHOP knockdown. In all, these findings suggest that PE causes ER stress-associated cell death and cell cycle arrest, and it may serve as a potent agent for curing human HCC.
肝细胞癌（HCC）是一种预后较差的原发性肝癌。在本研究中，我们报告了从[植物名称]根中提取的卡斯巴烷二萜类化合物佩金宁E（PE），在体外和体内均对人肝癌细胞具有强大的抗肿瘤活性。PE抑制人肝癌细胞Hep G2和SMMC - 7721的生长。此外，PE介导的内质网（ER）应激导致C/EBP同源蛋白（CHOP）表达增加，从而导致体外和体内肝癌细胞凋亡。用CHOP小干扰RNA或4-苯基丁酸抑制ER应激可部分逆转PE诱导的细胞死亡。此外，PE诱导S期细胞周期停滞，CHOP基因敲低也可部分逆转这一现象。总之，这些发现表明PE导致与ER应激相关的细胞死亡和细胞周期停滞，它可能是治疗人类HCC的有效药物。
