一种新的胡椒碱衍生物HJ-23通过激活p53通路显示出抗结直肠癌的作用。

IF 3.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Meiqi Zhang, Ruotong Liu, Wentao Jiang, Hanxue Li, Siyi Zhang, Wenhao Cheng, Xiaoqing Ye, Jingliang He, Yuanyuan Liu, Aixin Jing, Yizhuo Song, Dan Wang, Xing Liu, Boyu Zhang, Xiujun Wang, Jing Ji
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引用次数: 0

摘要

近年来,结直肠癌的发病率有所上升,预后较差。在一些研究中,胡椒碱已被证明可以抑制结肠癌细胞的生长并诱导细胞凋亡。本研究旨在探讨一种新型胡椒衍生化合物HJ-23(2,2-二氟苯并[d][1,3]二恶醇-5-基)(4-(2,4-二氟苯基)哌嗪-1-基)甲烷酮)是否能通过特定的分子机制有效抑制结直肠癌的发生发展。采用MTT法评价HJ-23对结直肠癌细胞活力的影响。通过细胞和鸡胚模型的抗增殖实验进一步证实了该化合物的有效性。此外,采用RNA测序(RNA- seq)技术分析基因表达变化,采用基因集富集分析(GSEA)技术鉴定HJ-23调控的通路。MTT实验、克隆形成实验和鸡胚实验均证实HJ-23能显著抑制结直肠癌细胞的增殖。RNA-Seq分析显示,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)通路调控细胞增殖和细胞周期过程。HJ-23通过激活p53通路,抑制肿瘤细胞增殖,具有明显的抗肿瘤作用。这些发现表明HJ-23是一种很有前景的治疗结直肠癌的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
A novel piperine derivative HJ-23 exhibits anti-colorectal cancer effects by activating the p53 pathway.

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.

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来源期刊
CiteScore
6.20
自引率
5.60%
发文量
142
审稿时长
4-8 weeks
期刊介绍: Naunyn-Schmiedeberg''s Archives of Pharmacology was founded in 1873 by B. Naunyn, O. Schmiedeberg and E. Klebs as Archiv für experimentelle Pathologie und Pharmakologie, is the offical journal of the German Society of Experimental and Clinical Pharmacology and Toxicology (Deutsche Gesellschaft für experimentelle und klinische Pharmakologie und Toxikologie, DGPT) and the Sphingolipid Club. The journal publishes invited reviews, original articles, short communications and meeting reports and appears monthly. Naunyn-Schmiedeberg''s Archives of Pharmacology welcomes manuscripts for consideration of publication that report new and significant information on drug action and toxicity of chemical compounds. Thus, its scope covers all fields of experimental and clinical pharmacology as well as toxicology and includes studies in the fields of neuropharmacology and cardiovascular pharmacology as well as those describing drug actions at the cellular, biochemical and molecular levels. Moreover, submission of clinical trials with healthy volunteers or patients is encouraged. Short communications provide a means for rapid publication of significant findings of current interest that represent a conceptual advance in the field.
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