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一种新型胡椒碱衍生物HJ-23通过激活p53通路发挥抗结直肠癌作用。

A novel piperine derivative HJ-23 exhibits anti-colorectal cancer effects by activating the p53 pathway.

作者信息

Zhang Meiqi, Liu Ruotong, Jiang Wentao, Li Hanxue, Zhang Siyi, Cheng Wenhao, Ye Xiaoqing, He Jingliang, Liu Yuanyuan, Jing Aixin, Song Yizhuo, Wang Dan, Liu Xing, Zhang Boyu, Wang Xiujun, Ji Jing

机构信息

Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, College of Pharmacy, Jiangsu Ocean University, Lianyungang, 222005, China.

College of Pharmacy and Chemistry and Chemical Engineering, Taizhou University, Taizhou, China.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2024 Dec 24. doi: 10.1007/s00210-024-03707-2.

Abstract

There has been an increase in the incidence and poor prognosis of colorectal cancer in recent years. In several studies, piperine has been shown to inhibit colon cancer cell growth and induce apoptosis. This study aimed to investigate whether a novel piperine-derived compound, HJ-23 (2,2-difluorobenzo[d][1,3]dioxol-5-yl)(4-(2,4-difluorophenyl)piperazin-1-yl)methanone), can effectively inhibit the development of colorectal cancer through specific molecular mechanisms. The MTT method was used to evaluate the effect of HJ-23 on the viability of colorectal cancer cells. The effectiveness of the compound was further confirmed by antiproliferation experiments in cell and chicken embryo models. In addition, RNA sequencing (RNA-Seq) was used to analyze changes in gene expression, and gene set enrichment analysis (GSEA) was used to identify pathways regulated by HJ-23. MTT assay, clone formation assay, and chicken embryo assay all confirmed that HJ-23 could significantly inhibit the proliferation of colorectal cancer cells. RNA-Seq analysis showed that HJ-23 significantly downregulated the expression of the tumor proliferation marker Mki67. GSEA showed that HJ-23 mainly regulated cell proliferation and cell cycle processes by activating the p53 pathway and inhibiting the E2F transcription factor (E2F) pathway. HJ-23 exhibits significant anti-tumor effects by activating the p53 pathway and inhibiting tumor cell proliferation. These findings suggest that HJ-23 is a promising drug candidate for treating colorectal cancer.

摘要

近年来,结直肠癌的发病率有所上升且预后较差。在多项研究中,胡椒碱已被证明可抑制结肠癌细胞生长并诱导细胞凋亡。本研究旨在探究一种新型胡椒碱衍生化合物HJ - 23(2,2 - 二氟苯并[d][1,3]二氧杂环戊烯 - 5 - 基)(4 - (2,4 - 二氟苯基)哌嗪 - 1 - 基)甲酮)是否能通过特定分子机制有效抑制结直肠癌的发展。采用MTT法评估HJ - 23对结肠癌细胞活力的影响。通过细胞和鸡胚模型中的抗增殖实验进一步证实了该化合物的有效性。此外,利用RNA测序(RNA - Seq)分析基因表达变化,并采用基因集富集分析(GSEA)鉴定受HJ - 23调控的通路。MTT试验、克隆形成试验和鸡胚试验均证实HJ - 23可显著抑制结肠癌细胞的增殖。RNA - Seq分析表明,HJ - 23显著下调肿瘤增殖标志物Mki67的表达。GSEA显示,HJ - 23主要通过激活p53通路和抑制E2F转录因子(E2F)通路来调控细胞增殖和细胞周期进程。HJ - 23通过激活p53通路和抑制肿瘤细胞增殖展现出显著的抗肿瘤作用。这些发现表明,HJ - 23是一种有前景的治疗结直肠癌的候选药物。

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