• 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

新型联吡啶和联嘧啶二硫代氨基甲酸金（III）衍生物的强效体外和体内抗癌活性

Potent In Vitro and In Vivo Anticancer Activity of New Bipyridine and Bipyrimidine Gold (III) Dithiocarbamate Derivatives.

作者信息

Altaf Muhammad, Casagrande Naike, Mariotto Elena, Baig Nadeem, Kawde Abdel-Nasser, Corona Giuseppe, Larcher Roberto, Borghese Cinzia, Pavan Claudia, Seliman Adam A, Aldinucci Donatella, Isab Anvarhusein A

机构信息

Department of Chemistry, GC University, Lahore 54000, Pakistan.

Molecular Oncology, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, 33081 Aviano, Italy.

出版信息

Cancers (Basel). 2019 Apr 4;11(4):474. doi: 10.3390/cancers11040474.

DOI:10.3390/cancers11040474
PMID:30987271
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6521029/
Abstract

We synthesized eight new bipyridine and bipyrimidine gold (III) dithiocarbamate-containing complexes (- and tested them in a panel of human cancer cell lines. We used osteosarcoma (MG-63), lung (A549), prostate (PC3 and DU145), breast (MCF-7), ovarian (A2780 and A2780cis, cisplatin- and doxorubicin-resistant), and cervical (ME-180 and R-ME-180, cisplatin resistant) cancer cell lines. We found that , , , and were more cytotoxic than cisplatin in all cell lines tested and overcame cisplatin and doxorubicin resistance in A2780cis and R-ME-180 cells. In the PC3 prostate cancer cell line, the gold (III) complex ([Au₂(BPM)(DMDTC)₂]Cl₄) induced apoptosis and double-stranded DNA breaks, modified cell cycle phases, increased Reactive Oxigen Species (ROS) generation, and reduced thioredoxin reductase and proteasome activities. It inhibited PC3 cell migration and was more cytotoxic against PC3 cells than normal human adipose-derived stromal cells. In mice bearing PC3 tumor xenografts, reduced tumor growth by more than 70% without causing weight loss. Altogether, our results demonstrate the anticancer activity of these new gold (III) complexes and support the potential of as a new agent for prostate cancer treatment.

摘要

我们合成了八种新的含联吡啶和联嘧啶的二硫代氨基甲酸金（III）配合物，并在一组人类癌细胞系中对其进行了测试。我们使用了骨肉瘤（MG-63）、肺癌（A549）、前列腺癌（PC3和DU145）、乳腺癌（MCF-7）、卵巢癌（A2780和A2780cis，顺铂和阿霉素耐药）以及宫颈癌（ME-180和R-ME-180，顺铂耐药）细胞系。我们发现，在所有测试的细胞系中，[Au₂(bpy)(DMDTC)₂]Cl₄、[Au₂(bpy)(BDTC)₂]Cl₄、[Au₂(bpm)(DMDTC)₂]Cl₄和[Au₂(bpm)(BDTC)₂]Cl₄比顺铂具有更强的细胞毒性，并且克服了A2780cis和R-ME-180细胞中的顺铂和阿霉素耐药性。在PC3前列腺癌细胞系中，金（III）配合物[Au₂(BPM)(DMDTC)₂]Cl₄诱导细胞凋亡和双链DNA断裂，改变细胞周期阶段，增加活性氧（ROS）生成，并降低硫氧还蛋白还原酶和蛋白酶体活性。它抑制PC3细胞迁移，并且对PC3细胞的细胞毒性比对正常人脂肪来源的基质细胞更强。在携带PC3肿瘤异种移植的小鼠中，[Au₂(BPM)(DMDTC)₂]Cl₄使肿瘤生长减少超过70%，且未导致体重减轻。总之，我们的结果证明了这些新的金（III）配合物的抗癌活性，并支持[Au₂(BPM)(DMDTC)₂]Cl₄作为一种前列腺癌治疗新药物的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/8466538eda91/cancers-11-00474-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/bd0d83c4aeaa/cancers-11-00474-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/9ada25fe3e47/cancers-11-00474-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/2b1582ce459a/cancers-11-00474-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/8466538eda91/cancers-11-00474-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/bd0d83c4aeaa/cancers-11-00474-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/9ada25fe3e47/cancers-11-00474-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/2b1582ce459a/cancers-11-00474-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb21/6521029/8466538eda91/cancers-11-00474-g004.jpg

相似文献

1
Potent In Vitro and In Vivo Anticancer Activity of New Bipyridine and Bipyrimidine Gold (III) Dithiocarbamate Derivatives.新型联吡啶和联嘧啶二硫代氨基甲酸金（III）衍生物的强效体外和体内抗癌活性
Cancers (Basel). 2019 Apr 4;11(4):474. doi: 10.3390/cancers11040474.
2
New bipyridine gold(III) dithiocarbamate-containing complexes exerted a potent anticancer activity against cisplatin-resistant cancer cells independent of p53 status.新型含二硫代氨基甲酸盐的联吡啶金（III）配合物对顺铂耐药癌细胞具有强大的抗癌活性，且与p53状态无关。
Oncotarget. 2017 Jan 3;8(1):490-505. doi: 10.18632/oncotarget.13448.
3
Antitumor activity of gold(III)-dithiocarbamato derivatives on prostate cancer cells and xenografts.金（III）-二硫代氨基甲酸盐衍生物对前列腺癌细胞和异种移植物的抗肿瘤活性。
Int J Cancer. 2011 Jan 1;128(1):206-15. doi: 10.1002/ijc.25311.
4
Antitumor and Antiangiogenic Properties of Gold(III) Complexes Containing Cycloaurated Triphenylphosphine Sulfide Ligands.含环金化三苯基膦硫醚配体的金（III）配合物的抗肿瘤和抗血管生成特性。
Inorg Chem. 2020 Apr 20;59(8):5662-5673. doi: 10.1021/acs.inorgchem.0c00423. Epub 2020 Apr 7.
5
Anticancer Activity and Apoptosis Induction of Gold(III) Complexes Containing 2,2'-Bipyridine-3,3'-dicarboxylic Acid and Dithiocarbamates.含2,2'-联吡啶-3,3'-二羧酸和二硫代氨基甲酸盐的金(III)配合物的抗癌活性及诱导凋亡作用
Molecules. 2021 Jun 29;26(13):3973. doi: 10.3390/molecules26133973.
6
A novel anticancer gold(III) dithiocarbamate compound inhibits the activity of a purified 20S proteasome and 26S proteasome in human breast cancer cell cultures and xenografts.一种新型抗癌二硫代氨基甲酸金（III）化合物可抑制人乳腺癌细胞培养物和异种移植模型中纯化的20S蛋白酶体和26S蛋白酶体的活性。
Cancer Res. 2006 Nov 1;66(21):10478-86. doi: 10.1158/0008-5472.CAN-06-3017.
7
Preclinical activity of multiple-target gold(III)-dithiocarbamato peptidomimetics in prostate cancer cells and xenografts.多靶点二硫代氨基甲酸盐肽模拟物金（III）在前列腺癌细胞和异种移植瘤中的临床前活性
Future Med Chem. 2014 Jul;6(11):1249-63. doi: 10.4155/fmc.14.81.
8
Overcoming cisplatin resistance using gold(III) mimics: anticancer activity of novel gold(III) polypyridyl complexes.利用金（III）模拟物克服顺铂耐药性：新型金（III）多吡啶配合物的抗癌活性。
J Inorg Biochem. 2012 Jan;106(1):32-42. doi: 10.1016/j.jinorgbio.2011.08.013. Epub 2011 Sep 12.
9
Synthesis, characterization, and antitumor activity of unusual pseudo five coordinate gold(III) complexes: distinct cytotoxic mechanism or expensive ligand delivery systems?异常的伪五配位金（III）配合物的合成、表征及抗肿瘤活性：独特的细胞毒性机制还是昂贵的配体递送系统？
J Inorg Biochem. 2014 Dec;141:121-131. doi: 10.1016/j.jinorgbio.2014.08.014. Epub 2014 Sep 6.
10
Cytotoxic and Apoptotic Effects of Novel Pyrrolo[2,3-d]Pyrimidine Derivatives Containing Urea Moieties on Cancer Cell Lines.含脲基新型吡咯并[2,3-d]嘧啶衍生物对癌细胞系的细胞毒性和凋亡作用
Anticancer Agents Med Chem. 2018;18(9):1303-1312. doi: 10.2174/1871520618666180605082026.

引用本文的文献

1
Anticancer Activity of Metallodrugs and Metallizing Host Defense Peptides-Current Developments in Structure-Activity Relationship.金属药物和金属化宿主防御肽的抗癌活性-结构-活性关系的最新进展。
Int J Mol Sci. 2024 Jul 3;25(13):7314. doi: 10.3390/ijms25137314.
2
G2/M-Phase-Inhibitory Mitochondrial-Depolarizing Re(I)/Ru(II)/Ir(III)-2,2'-Bipyrimidine-Based Heterobimetallic Luminescent Complexes: An Assessment of In Vitro Antiproliferative Activity and Bioimaging for Targeted Therapy toward Human TNBC Cells.基于G2/M期抑制性线粒体去极化的Re(I)/Ru(II)/Ir(III)-2,2'-联嘧啶异双金属发光配合物：对人三阴性乳腺癌细胞靶向治疗的体外抗增殖活性和生物成像评估
ACS Omega. 2023 Mar 21;8(13):12283-12297. doi: 10.1021/acsomega.2c08285. eCollection 2023 Apr 4.
3

本文引用的文献

1
Recent trends in the management of advanced prostate cancer.晚期前列腺癌治疗的最新趋势
F1000Res. 2018 Sep 21;7. doi: 10.12688/f1000research.15382.1. eCollection 2018.
2
Proteasome versus Thioredoxin Reductase Competition as Possible Biological Targets in Antitumor Mixed Thiolate-Dithiocarbamate Gold(III) Complexes.蛋白酶体与硫氧还蛋白还原酶竞争作为抗肿瘤混合硫醇-二硫代氨基甲酸酯金（III）配合物的可能生物学靶点。
Inorg Chem. 2018 Sep 4;57(17):10832-10845. doi: 10.1021/acs.inorgchem.8b01464. Epub 2018 Aug 17.
3
Significance of the mitochondrial thioredoxin reductase in cancer cells: An update on role, targets and inhibitors.
Genome-wide CRISPR Screen Reveal Targets of Chiral Gold(I) Anticancer Compound in Mammalian Cells.全基因组CRISPR筛选揭示手性金（I）抗癌化合物在哺乳动物细胞中的靶点。
ACS Omega. 2022 Oct 20;7(43):39197-39205. doi: 10.1021/acsomega.2c05166. eCollection 2022 Nov 1.
4
In Vitro and In Vivo Relevant Antineoplastic Activity of Platinum(II) Complexes toward Triple-Negative MDA-MB-231 Breast Cancer Cell Line.铂（II）配合物对三阴性MDA-MB-231乳腺癌细胞系的体外和体内相关抗肿瘤活性
Pharmaceutics. 2022 Sep 22;14(10):2013. doi: 10.3390/pharmaceutics14102013.
5
Organometallic gold(I) and gold(III) complexes for lung cancer treatment.用于肺癌治疗的有机金属金（I）和金（III）配合物。
Front Pharmacol. 2022 Sep 13;13:979951. doi: 10.3389/fphar.2022.979951. eCollection 2022.
6
Spheroid Culture Differentially Affects Cancer Cell Sensitivity to Drugs in Melanoma and RCC Models.球体培养在黑色素瘤和 RCC 模型中对癌细胞对药物的敏感性有不同影响。
Int J Mol Sci. 2022 Jan 21;23(3):1166. doi: 10.3390/ijms23031166.
7
Development and Characterization of Calcium-Alginate Beads of Apigenin: In Vitro Antitumor, Antibacterial, and Antioxidant Activities.阿魏酸钙藻酸盐珠的制备及性能表征：体外抗肿瘤、抗菌和抗氧化活性。
Mar Drugs. 2021 Aug 20;19(8):467. doi: 10.3390/md19080467.
8
Anticancer Activity and Apoptosis Induction of Gold(III) Complexes Containing 2,2'-Bipyridine-3,3'-dicarboxylic Acid and Dithiocarbamates.含2,2'-联吡啶-3,3'-二羧酸和二硫代氨基甲酸盐的金(III)配合物的抗癌活性及诱导凋亡作用
Molecules. 2021 Jun 29;26(13):3973. doi: 10.3390/molecules26133973.
9
Colloidal Stability and Cytotoxicity of Polydopamine-Conjugated Gold Nanorods against Prostate Cancer Cell Lines.聚多巴胺修饰的金纳米棒对前列腺癌细胞系的胶体稳定性和细胞毒性。
Molecules. 2021 Feb 28;26(5):1299. doi: 10.3390/molecules26051299.
10
Reactions of Medicinal Gold(III) Compounds With Proteins and Peptides Explored by Electrospray Ionization Mass Spectrometry and Complementary Biophysical Methods.通过电喷雾电离质谱和互补生物物理方法探索药用金（III）化合物与蛋白质和肽的反应
Front Chem. 2020 Oct 21;8:581648. doi: 10.3389/fchem.2020.581648. eCollection 2020.
线粒体硫氧还蛋白还原酶在癌细胞中的意义：作用、靶点和抑制剂的最新研究进展。
Free Radic Biol Med. 2018 Nov 1;127:62-79. doi: 10.1016/j.freeradbiomed.2018.03.043. Epub 2018 Mar 27.
4
Gold(III) Complexes for Antitumor Applications: An Overview.用于抗肿瘤应用的金（III）配合物：概述。
Chemistry. 2018 Aug 14;24(46):11840-11851. doi: 10.1002/chem.201800981. Epub 2018 Jun 8.
5
Editorial: Throwing Light on Recent Advances on Metallodrugs: From Deemed Poisons to a Striking Hope for the Future.社论：揭示金属药物的最新进展：从被视为毒药到未来显著的希望
Curr Med Chem. 2018 Feb 12;25(4):434-436. doi: 10.2174/092986732504180212164536.
6
Medicinal Chemistry of Gold Anticancer Metallodrugs.金抗癌金属药物的药物化学
Met Ions Life Sci. 2018 Feb 5;18. doi: 10.1515/9783110470734-013.
7
New comprehensive studies of a gold(III) Dithiocarbamate complex with proven anticancer properties: Aqueous dissolution with cyclodextrins, pharmacokinetics and upstream inhibition of the ubiquitin-proteasome pathway.新型具有抗癌性能的金（III）二硫代氨基甲酸盐配合物的综合研究：环糊精的水溶作用、药代动力学和泛素-蛋白酶体途径的上游抑制作用。
Eur J Med Chem. 2017 Sep 29;138:115-127. doi: 10.1016/j.ejmech.2017.06.013. Epub 2017 Jun 19.
8
Targeting the Thioredoxin System for Cancer Therapy.靶向硫氧还蛋白系统治疗癌症。
Trends Pharmacol Sci. 2017 Sep;38(9):794-808. doi: 10.1016/j.tips.2017.06.001. Epub 2017 Jun 22.
9
Platinum, palladium, gold and ruthenium complexes as anticancer agents: Current clinical uses, cytotoxicity studies and future perspectives.铂、钯、金和钌配合物作为抗癌剂：当前临床应用、细胞毒性研究及未来展望。
Eur J Med Chem. 2017 Dec 15;142:8-31. doi: 10.1016/j.ejmech.2017.04.007. Epub 2017 Apr 18.
10
Doxorubicin targets multiple players: A new view of an old problem.多柔比星针对多个靶点：一个老问题的新视角。
Pharmacol Res. 2018 Jan;127:4-14. doi: 10.1016/j.phrs.2017.03.016. Epub 2017 Mar 20.