Ren Hongyu, Gao Qi, Wang Mengmeng, Zhang Luyao, Wang Sen, Zhang Xingyu, Li Hanxue, Ye Xiaoqing, Zhou Lili, Zhou Chongyun, Li Xiuming, Zeng Kaile, Ji Jing
Key Laboratory of Marine Pharmaceutical Compound Screening, College of Pharmacy, Jiangsu Ocean University, Lianyungang, China.
College of Pharmacy and Chemistry & Chemical Engineering, Taizhou University, Taizhou, China.
Naunyn Schmiedebergs Arch Pharmacol. 2025 Jan 31. doi: 10.1007/s00210-025-03805-9.
Triple-negative breast cancer (TNBC) is characterized by high aggressiveness and recurrence rates due to the lack of effective treatment options. Piperine, a natural alkaloid extracted from black pepper, has demonstrated significant anticancer potential in recent years. Therefore, developing piperine derivatives to enhance its anticancer effects holds critical clinical significance. In this study, a novel piperine derivative, MHJ-LN, was designed and synthesized. Its anticancer effects against TNBC were systematically evaluated through in vitro and in vivo experiments. The MTT assay, EdU incorporation assay, and colony formation assay were employed to assess the impact of MHJ-LN on TNBC cell proliferation. Tumor cell adhesion, scratch wound healing, and Transwell invasion assays were performed to analyze the antitumor activity of MHJ-LN. Additionally, apoptosis was detected using YO-PRO-1/PI staining, and immunofluorescence combined with Western blotting was used to assess the expression of p53 pathway-related proteins. MHJ-LN exhibited significant antitumor activity in the TNBC xenograft model. Its mechanism of antitumor action was found to depend on the activation of the MDM2-p53 pathway, effectively blocking G1/S cell cycle progression and inducing apoptosis and cell cycle arrest. This research suggests that the piperine derivative MHJ-LN shows significant potential as an effective therapy targeting breast cancer.
三阴性乳腺癌(TNBC)因缺乏有效的治疗方案而具有高侵袭性和复发率的特点。胡椒碱是从黑胡椒中提取的一种天然生物碱,近年来已显示出显著的抗癌潜力。因此,开发胡椒碱衍生物以增强其抗癌效果具有至关重要的临床意义。在本研究中,设计并合成了一种新型胡椒碱衍生物MHJ-LN。通过体外和体内实验系统地评估了其对TNBC的抗癌作用。采用MTT法、EdU掺入法和集落形成法评估MHJ-LN对TNBC细胞增殖的影响。进行肿瘤细胞黏附、划痕伤口愈合和Transwell侵袭实验以分析MHJ-LN的抗肿瘤活性。此外,使用YO-PRO-1/PI染色检测细胞凋亡,并采用免疫荧光结合蛋白质免疫印迹法评估p53通路相关蛋白的表达。MHJ-LN在TNBC异种移植模型中表现出显著的抗肿瘤活性。发现其抗肿瘤作用机制依赖于MDM2-p53通路的激活,有效阻断G1/S细胞周期进程并诱导细胞凋亡和细胞周期停滞。本研究表明,胡椒碱衍生物MHJ-LN作为一种针对乳腺癌的有效治疗方法具有显著潜力。