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
{"title":"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。","authors":"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","doi":"10.1007/s00210-024-03707-2","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":18876,"journal":{"name":"Naunyn-Schmiedeberg's archives of pharmacology","volume":" ","pages":"7121-7131"},"PeriodicalIF":3.1000,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"A novel piperine derivative HJ-23 exhibits anti-colorectal cancer effects by activating the p53 pathway.\",\"authors\":\"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\",\"doi\":\"10.1007/s00210-024-03707-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":18876,\"journal\":{\"name\":\"Naunyn-Schmiedeberg's archives of pharmacology\",\"volume\":\" \",\"pages\":\"7121-7131\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2025-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Naunyn-Schmiedeberg's archives of pharmacology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1007/s00210-024-03707-2\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/24 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Naunyn-Schmiedeberg's archives of pharmacology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1007/s00210-024-03707-2","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/24 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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.
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.