• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

具有辅助β-咔啉眼镜潜力的基于色氨酸的生物活性铜配合物对人乳腺癌细胞的作用：体外和体内研究。

Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies.

机构信息

Department of Chemistry, Faculty of Science, King Khalid University, P.O. Box 9004, Abha 62529, Saudi Arabia.

Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2021 Mar 14;26(6):1606. doi: 10.3390/molecules26061606.

DOI:10.3390/molecules26061606
PMID:33799355
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8001361/
Abstract

Biocompatible tryptophan-derived copper () and zinc () complexes with norharmane (β-carboline) were designed, synthesized, characterized, and evaluated for the potential anticancer activity in vitro and in vivo. The in vitro cytotoxicity of both complexes and were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of against MCF7 cells with an IC value of 7.8 ± 0.4 μM compared to (less active, IC ~ 20 μM). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of .

摘要

设计、合成、表征了具有 norharmane（β-咔啉）的生物相容色氨酸衍生的铜（）和锌（）配合物，并评估了它们在体外和体内的潜在抗癌活性。两种配合物[Cu(trp)(nor)]（）和[Zn(trp)(nor)]（）的体外细胞毒性均针对两种癌细胞（人乳腺癌）MCF7 和（肝肝癌）HepG2 细胞与非致瘤细胞（人胚肾）HEK293 细胞进行了评估。结果显示，[Cu(trp)(nor)]（）对 MCF7 细胞具有潜在的良好选择性，IC 值为 7.8 ± 0.4 μM，而[Zn(trp)(nor)]（活性较低，IC~20 μM）。此外，我们分析了谷胱甘肽水平、脂质过氧化和可视化 ROS 生成，以深入了解其机制途径并见证氧化应激。这些体外结果通过体内实验得到了证实，这也支持了自由基介导的氧化应激。彗星试验证实了导致 DNA 损伤的氧化应激。肝组织病理学也证实了 的低毒性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/e0543a248bf7/molecules-26-01606-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/77e326c997cd/molecules-26-01606-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/49138ab66688/molecules-26-01606-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/cf877ce1a8a6/molecules-26-01606-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/5f7a402efd28/molecules-26-01606-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/4d544ecad5b5/molecules-26-01606-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/5d490f2a868a/molecules-26-01606-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/439ec23d74c9/molecules-26-01606-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/df5e9acf79fe/molecules-26-01606-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/e0543a248bf7/molecules-26-01606-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/77e326c997cd/molecules-26-01606-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/49138ab66688/molecules-26-01606-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/cf877ce1a8a6/molecules-26-01606-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/5f7a402efd28/molecules-26-01606-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/4d544ecad5b5/molecules-26-01606-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/5d490f2a868a/molecules-26-01606-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/439ec23d74c9/molecules-26-01606-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/df5e9acf79fe/molecules-26-01606-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3a47/8001361/e0543a248bf7/molecules-26-01606-g009.jpg

相似文献

1
Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies.具有辅助β-咔啉眼镜潜力的基于色氨酸的生物活性铜配合物对人乳腺癌细胞的作用：体外和体内研究。
Molecules. 2021 Mar 14;26(6):1606. doi: 10.3390/molecules26061606.
2
Enhanced reactive oxygen species overexpression by CuO nanoparticles in poorly differentiated hepatocellular carcinoma cells.氧化铜纳米颗粒增强低分化肝癌细胞内活性氧的过度表达。
Nanoscale. 2015 Feb 7;7(5):1820-9. doi: 10.1039/c4nr05843g.
3
Evaluation of the in vivo acute toxicity and in vitro genotoxicity and mutagenicity of synthetic β-carboline alkaloids with selective cytotoxic activity against ovarian and breast cancer cell lines.评价具有选择性细胞毒活性的合成β-咔啉生物碱的体内急性毒性和体外遗传毒性及致突变性。
Mutat Res Genet Toxicol Environ Mutagen. 2024 Oct;899:503808. doi: 10.1016/j.mrgentox.2024.503808. Epub 2024 Aug 10.
4
Mechanistic insights into a novel chromone-appended Cu(II) anticancer drug entity: in vitro binding profile with DNA/RNA substrates and cytotoxic activity against MCF-7 and HepG2 cancer cells.新型色酮修饰的铜（II）抗癌药物实体的作用机制研究：与DNA/RNA底物的体外结合情况及对MCF-7和HepG2癌细胞的细胞毒性活性
Dalton Trans. 2015 Jun 14;44(22):10330-42. doi: 10.1039/c5dt00770d.
5
Discovery of β-carboline-(phenylsulfonyl)furoxan hybrids as potential anti-breast cancer agents.β-咔啉-(苯磺酰基)呋咱杂合体的发现作为潜在的抗乳腺癌药物。
Bioorg Med Chem Lett. 2021 May 15;40:127952. doi: 10.1016/j.bmcl.2021.127952. Epub 2021 Mar 17.
6
Verbesina encelioides: cytotoxicity, cell cycle arrest, and oxidative DNA damage in human liver cancer (HepG2) cell line.假泽兰：对人肝癌（HepG2）细胞系的细胞毒性、细胞周期阻滞及氧化性DNA损伤
BMC Complement Altern Med. 2016 May 10;16:126. doi: 10.1186/s12906-016-1106-0.
7
Anticancer activity of a new copper(II) complex with a hydrazone ligand. Structural and spectroscopic characterization, computational simulations and cell mechanistic studies on 2D and 3D breast cancer cell models.新型含腙配体的铜（II）配合物的抗癌活性。二维和三维乳腺癌细胞模型的结构和光谱表征、计算模拟和细胞机制研究。
Dalton Trans. 2021 Jul 21;50(28):9812-9826. doi: 10.1039/d1dt00869b.
8
Redox cycling of copper by coumarin-di(2-picolyl)amine hybrid molecule leads to ROS-mediated modulation of redox scavengers, DNA damage and cell death in diethylnitrosamine induced hepatocellular carcinoma.香豆素二（2-吡啶基）胺杂化分子介导的铜的氧化还原循环导致活性氧介导的氧化还原清除剂、二乙基亚硝胺诱导的肝癌中的 DNA 损伤和细胞死亡的调节。
Bioorg Chem. 2020 Jun;99:103818. doi: 10.1016/j.bioorg.2020.103818. Epub 2020 Apr 3.
9
Copper-redox cycling by coumarin-di(2-picolyl)amine hybrid molecule leads to ROS-mediated DNA damage and apoptosis: A mechanism for cancer chemoprevention.香豆素-二（2-吡啶基）胺杂化分子的铜氧化还原循环导致 ROS 介导的 DNA 损伤和细胞凋亡：癌症化学预防的一种机制。
Chem Biol Interact. 2018 Jun 25;290:64-76. doi: 10.1016/j.cbi.2018.05.010. Epub 2018 May 24.
10
Antioxidant and apoptotic effects of Callistemon lanceolatus leaves and their compounds against human cancer cells.金蒲桃叶及其化合物的抗氧化和促凋亡作用及其对人癌细胞的影响。
Biomed Pharmacother. 2018 Oct;106:1195-1209. doi: 10.1016/j.biopha.2018.07.016. Epub 2018 Jul 19.

引用本文的文献

1
Exploring the antitumor effects of Pd(II) complexes with nitrogen donor ligands towards breast carcinoma.探索含氮供体配体的钯（II）配合物对乳腺癌的抗肿瘤作用。
Biometals. 2025 Jun 5. doi: 10.1007/s10534-025-00702-9.
2
Study of novel bidentate heterocyclic amine-based metal complexes and their biological activities: cytotoxicity and antimicrobial activity evaluation.新型双齿杂环胺基金属配合物及其生物活性研究：细胞毒性和抗菌活性评估
BMC Chem. 2023 Jul 15;17(1):78. doi: 10.1186/s13065-023-00996-1.

本文引用的文献

1
Clinical developments of antitumor polymer therapeutics.抗肿瘤聚合物疗法的临床进展
RSC Adv. 2019 Aug 8;9(43):24699-24721. doi: 10.1039/c9ra04358f.
2
Curcumin-containing Silver Nanoparticles Prevent Carbon Tetrachloride- induced Hepatotoxicity in Mice.含姜黄素的银纳米粒子可预防四氯化碳诱导的小鼠肝毒性。
Comb Chem High Throughput Screen. 2021;24(10):1609-1617. doi: 10.2174/1386207323666201211100830.
3
β-Carboline copper complex as a potential mitochondrial-targeted anticancer chemotherapeutic agent: Favorable attenuation of human breast cancer MCF7 cells via apoptosis.
β-咔啉铜配合物作为一种潜在的线粒体靶向抗癌化疗药物：通过凋亡对人乳腺癌MCF7细胞产生良好的抑制作用。
Saudi J Biol Sci. 2020 Aug;27(8):2164-2173. doi: 10.1016/j.sjbs.2020.05.001. Epub 2020 May 8.
4
Chemopreventive effect of riboflavin on the potassium bromate-induced renal toxicity in vivo.核黄素对体内溴酸钾诱导的肾毒性的化学预防作用。
Naunyn Schmiedebergs Arch Pharmacol. 2020 Dec;393(12):2355-2364. doi: 10.1007/s00210-020-01938-7. Epub 2020 Jul 14.
5
Copper Mediates Anti-Inflammatory and Antifibrotic Activity of Gleevec in Hepatocellular Carcinoma-Induced Male Rats.铜介导格列卫在肝癌诱导的雄性大鼠中的抗炎和抗纤维化作用。
Can J Gastroenterol Hepatol. 2019 Mar 3;2019:9897315. doi: 10.1155/2019/9897315. eCollection 2019.
6
Ameliorative effect of zinc oxide nanoparticles against potassium bromate-mediated toxicity in Swiss albino rats.氧化锌纳米粒子对溴酸钾介导的瑞士白化大鼠毒性的改善作用。
Environ Sci Pollut Res Int. 2019 Apr;26(10):9966-9980. doi: 10.1007/s11356-019-04443-4. Epub 2019 Feb 9.
7
Photocytotoxic copper(II) complexes of N-salicylyl-l-tryptophan and phenanthroline bases.N-水杨酰基-L-色氨酸和菲咯啉碱基的光细胞毒性铜（II）配合物。
J Inorg Biochem. 2019 Feb;191:60-68. doi: 10.1016/j.jinorgbio.2018.11.005. Epub 2018 Nov 9.
8
Therapeutic effect of chitosan on CCl4‑induced hepatic fibrosis in rats.壳聚糖对四氯化碳致大鼠肝纤维化的治疗作用。
Mol Med Rep. 2018 Sep;18(3):3211-3218. doi: 10.3892/mmr.2018.9343. Epub 2018 Aug 1.
9
Competitive reactions among glutathione, cisplatin and copper-phenanthroline complexes.谷胱甘肽、顺铂和铜-菲咯啉配合物之间的竞争反应。
J Inorg Biochem. 2017 Aug;173:126-133. doi: 10.1016/j.jinorgbio.2017.05.004. Epub 2017 May 8.
10
Transition-metal norharmane compounds as possible cytotoxic agents: New insights based on a coordination chemistry perspective.过渡金属去甲哈尔满化合物作为潜在的细胞毒性剂：基于配位化学视角的新见解。
J Inorg Biochem. 2016 Dec;165:128-135. doi: 10.1016/j.jinorgbio.2016.07.001. Epub 2016 Jul 7.