Scoulerine:一种靶向 SLC6A3 的天然异喹啉生物碱,用于治疗 RCC

IF 6.9 2区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL
Tianrui Qu , Yu Sun , Jingying Zhao , Nanqi Liu , Jianli Yang , Dantong Lyu , Wenjie Huang , Weizhen Zhan , Tao Li , Zichuan Yao , Rongbo Yan , Haiyan Zhang , Hong Hong , Liye Shi , Xin Meng , Bo Yin
{"title":"Scoulerine:一种靶向 SLC6A3 的天然异喹啉生物碱,用于治疗 RCC","authors":"Tianrui Qu ,&nbsp;Yu Sun ,&nbsp;Jingying Zhao ,&nbsp;Nanqi Liu ,&nbsp;Jianli Yang ,&nbsp;Dantong Lyu ,&nbsp;Wenjie Huang ,&nbsp;Weizhen Zhan ,&nbsp;Tao Li ,&nbsp;Zichuan Yao ,&nbsp;Rongbo Yan ,&nbsp;Haiyan Zhang ,&nbsp;Hong Hong ,&nbsp;Liye Shi ,&nbsp;Xin Meng ,&nbsp;Bo Yin","doi":"10.1016/j.biopha.2024.117524","DOIUrl":null,"url":null,"abstract":"<div><div>Scoulerine, an isoquinoline alkaloid derived from the corydalis plant, exhibits diverse therapeutic properties against tumors, Alzheimer's disease, and inflammation. This research delves into the pharmacological impact and underlying mechanism of scoulerine on renal cell carcinoma (RCC). Our findings suggest that Scoulerine displays promise as a potential therapeutic agent for RCC, demonstrating notable inhibitory effects in both in vivo and in vitro models. In addition, scoulerine inhibited the viability of 769-P and 786-O cell lines in a time-dependent and dose-dependent manner, and promoted the level of apoptosis associated with B-cell lymphoma-2 associated X protein (Bax). Moreover, the administration of scoulerine resulted in a significant suppression of the mitogen activated protein kinase (MAPK) signaling pathway. Subsequently, utilizing bioinformatics and spatial transcriptomic databases, we identified solute carrier family 6 Member 3 (SLC6A3) as the most promising target of scoulerine. Through experimental validation, we confirmed the functional and therapeutic relevance of SLC6A3 in scoulerine-mediated treatment of RCC. The results of our study indicate a significant affinity between scoulerine and SLC6A3, with competitive inhibition of this interaction leading to a reduction in the inhibitory impact of scoulerine on RCC cell viability. In conclusion, our findings suggest that scoulerine may induce apoptosis in RCC by targeting SLC6A3 and inhibiting the activation of the MAPK signaling pathway, thereby positioning it as a promising natural compound for potential future RCC treatment.</div></div>","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"180 ","pages":"Article 117524"},"PeriodicalIF":6.9000,"publicationDate":"2024-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Scoulerine: A natural isoquinoline alkaloid targeting SLC6A3 to treat RCC\",\"authors\":\"Tianrui Qu ,&nbsp;Yu Sun ,&nbsp;Jingying Zhao ,&nbsp;Nanqi Liu ,&nbsp;Jianli Yang ,&nbsp;Dantong Lyu ,&nbsp;Wenjie Huang ,&nbsp;Weizhen Zhan ,&nbsp;Tao Li ,&nbsp;Zichuan Yao ,&nbsp;Rongbo Yan ,&nbsp;Haiyan Zhang ,&nbsp;Hong Hong ,&nbsp;Liye Shi ,&nbsp;Xin Meng ,&nbsp;Bo Yin\",\"doi\":\"10.1016/j.biopha.2024.117524\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Scoulerine, an isoquinoline alkaloid derived from the corydalis plant, exhibits diverse therapeutic properties against tumors, Alzheimer's disease, and inflammation. This research delves into the pharmacological impact and underlying mechanism of scoulerine on renal cell carcinoma (RCC). Our findings suggest that Scoulerine displays promise as a potential therapeutic agent for RCC, demonstrating notable inhibitory effects in both in vivo and in vitro models. In addition, scoulerine inhibited the viability of 769-P and 786-O cell lines in a time-dependent and dose-dependent manner, and promoted the level of apoptosis associated with B-cell lymphoma-2 associated X protein (Bax). Moreover, the administration of scoulerine resulted in a significant suppression of the mitogen activated protein kinase (MAPK) signaling pathway. Subsequently, utilizing bioinformatics and spatial transcriptomic databases, we identified solute carrier family 6 Member 3 (SLC6A3) as the most promising target of scoulerine. Through experimental validation, we confirmed the functional and therapeutic relevance of SLC6A3 in scoulerine-mediated treatment of RCC. The results of our study indicate a significant affinity between scoulerine and SLC6A3, with competitive inhibition of this interaction leading to a reduction in the inhibitory impact of scoulerine on RCC cell viability. In conclusion, our findings suggest that scoulerine may induce apoptosis in RCC by targeting SLC6A3 and inhibiting the activation of the MAPK signaling pathway, thereby positioning it as a promising natural compound for potential future RCC treatment.</div></div>\",\"PeriodicalId\":8966,\"journal\":{\"name\":\"Biomedicine & Pharmacotherapy\",\"volume\":\"180 \",\"pages\":\"Article 117524\"},\"PeriodicalIF\":6.9000,\"publicationDate\":\"2024-10-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Biomedicine & Pharmacotherapy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0753332224014100\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"MEDICINE, RESEARCH & EXPERIMENTAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Biomedicine & Pharmacotherapy","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0753332224014100","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"MEDICINE, RESEARCH & EXPERIMENTAL","Score":null,"Total":0}
引用次数: 0

摘要

胭脂虫碱是从堇菜植物中提取的一种异喹啉生物碱,对肿瘤、老年痴呆症和炎症具有多种治疗特性。这项研究深入探讨了胭脂虫碱对肾细胞癌(RCC)的药理影响和内在机制。我们的研究结果表明,胭脂虫碱有望成为一种潜在的治疗 RCC 的药物,在体内和体外模型中均显示出显著的抑制作用。此外,黄芩碱以时间依赖性和剂量依赖性的方式抑制了 769-P 和 786-O 细胞系的活力,并促进了与 B 细胞淋巴瘤-2 相关的 X 蛋白(Bax)的凋亡水平。此外,给予 scoulerine 还能显著抑制丝裂原活化蛋白激酶(MAPK)信号通路。随后,我们利用生物信息学和空间转录组数据库,确定了溶质运载家族 6 成员 3(SLC6A3)是最有希望成为 scoulerine 靶点的细胞。通过实验验证,我们证实了 SLC6A3 在 scoulerine 介导的 RCC 治疗中的功能和治疗相关性。我们的研究结果表明,scoulerine 与 SLC6A3 之间具有显著的亲和力,竞争性抑制这种相互作用会降低 scoulerine 对 RCC 细胞活力的抑制作用。总之,我们的研究结果表明,scoulerine 可通过靶向 SLC6A3 和抑制 MAPK 信号通路的活化来诱导 RCC 细胞凋亡,从而使其成为未来治疗 RCC 的一种有潜力的天然化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Scoulerine: A natural isoquinoline alkaloid targeting SLC6A3 to treat RCC
Scoulerine, an isoquinoline alkaloid derived from the corydalis plant, exhibits diverse therapeutic properties against tumors, Alzheimer's disease, and inflammation. This research delves into the pharmacological impact and underlying mechanism of scoulerine on renal cell carcinoma (RCC). Our findings suggest that Scoulerine displays promise as a potential therapeutic agent for RCC, demonstrating notable inhibitory effects in both in vivo and in vitro models. In addition, scoulerine inhibited the viability of 769-P and 786-O cell lines in a time-dependent and dose-dependent manner, and promoted the level of apoptosis associated with B-cell lymphoma-2 associated X protein (Bax). Moreover, the administration of scoulerine resulted in a significant suppression of the mitogen activated protein kinase (MAPK) signaling pathway. Subsequently, utilizing bioinformatics and spatial transcriptomic databases, we identified solute carrier family 6 Member 3 (SLC6A3) as the most promising target of scoulerine. Through experimental validation, we confirmed the functional and therapeutic relevance of SLC6A3 in scoulerine-mediated treatment of RCC. The results of our study indicate a significant affinity between scoulerine and SLC6A3, with competitive inhibition of this interaction leading to a reduction in the inhibitory impact of scoulerine on RCC cell viability. In conclusion, our findings suggest that scoulerine may induce apoptosis in RCC by targeting SLC6A3 and inhibiting the activation of the MAPK signaling pathway, thereby positioning it as a promising natural compound for potential future RCC treatment.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
CiteScore
11.90
自引率
2.70%
发文量
1621
审稿时长
48 days
期刊介绍: Biomedicine & Pharmacotherapy stands as a multidisciplinary journal, presenting a spectrum of original research reports, reviews, and communications in the realms of clinical and basic medicine, as well as pharmacology. The journal spans various fields, including Cancer, Nutriceutics, Neurodegenerative, Cardiac, and Infectious Diseases.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信