School of Pharmacy, Anhui University of Chinese Medicine, Hefei, China.
Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, China.
Planta Med. 2021 Jul;87(8):620-630. doi: 10.1055/a-1348-1634. Epub 2021 Jan 21.
Peperomin E was first isolated from , an anticarcinogenic herb, and exhibited anticancer activity in many cancer cell lines. To date, it is unknown whether peperomin E has an effect on human prostate cancer DU145 cells and . In this study, we used MTT to assess the proliferation inhibition activity of peperomin E in DU145 cells and observed the cell morphological changes by a phase contrast microscope. A DU145 cell xenograft tumor mouse model was used to evaluate the efficacy of peperomin E . Apoptosis rates were measured by flow cytometry, and protein expression levels were analyzed by western blot. The results showed that peperomin E significantly inhibited the proliferation of DU145 cells and reduced the weight and volume of tumors . Peperomin E also significantly induced the apoptosis and autophagic response of DU145 cells. The autophagic inhibitors LY294002 and chloroquine enhanced peperomin E-mediated inhibition of DU145 cell proliferation and induction of DU145 cell apoptosis. The results also showed that the Akt/mTOR pathway participated in peperomin E-induced autophagy in DU145 cells. In summary, our finding showed that peperomin E had an effect on DU145 cells and in a nude mouse DU145 cell xenograft model , demonstrated that peperomin E could significantly induce apoptosis and the autophagic response in DU145 cells and that autophagy played a cytoprotective role in peperomin E-treated DU145 cells. These results suggest that the combination of peperomin E treatment and autophagic inhibition has potential for the treatment of prostate cancer.
胡椒醇 E 最初从一种抗癌草药中分离出来,并在许多癌细胞系中表现出抗癌活性。迄今为止,尚不清楚胡椒醇 E 是否对人前列腺癌 DU145 细胞有作用。在这项研究中,我们使用 MTT 评估胡椒醇 E 在 DU145 细胞中的增殖抑制活性,并通过相差显微镜观察细胞形态变化。使用 DU145 细胞异种移植肿瘤小鼠模型评估胡椒醇 E 的疗效。通过流式细胞术测量细胞凋亡率,并通过 Western blot 分析蛋白表达水平。结果表明,胡椒醇 E 显著抑制 DU145 细胞的增殖,并减少肿瘤的重量和体积。胡椒醇 E 还显著诱导 DU145 细胞的凋亡和自噬反应。自噬抑制剂 LY294002 和氯喹增强了胡椒醇 E 介导的 DU145 细胞增殖抑制和 DU145 细胞凋亡诱导。结果还表明,Akt/mTOR 通路参与了胡椒醇 E 诱导的 DU145 细胞自噬。总之,我们的发现表明胡椒醇 E 对 DU145 细胞有作用,在裸鼠 DU145 细胞异种移植模型中,表明胡椒醇 E 可显著诱导 DU145 细胞凋亡和自噬反应,自噬在胡椒醇 E 处理的 DU145 细胞中发挥细胞保护作用。这些结果表明,胡椒醇 E 治疗与自噬抑制的联合应用具有治疗前列腺癌的潜力。