Suppr超能文献

对胰腺导管腺癌细胞具有抗癌活性的新型铂(II)配合物。

Novel Pt (II) Complexes With Anticancer Activity Against Pancreatic Ductal Adenocarcinoma Cells.

作者信息

Stefàno Erika, Rovito Gianluca, Cossa Luca G, Castro Federica De, Vergaro Viviana, Ali Asjad, My Giulia, Migoni Danilo, Muscella Antonella, Marsigliante Santo, Benedetti Michele, Fanizzi Francesco Paolo

机构信息

Department of Biological and Environmental Sciences and Technologies (DiSTeBA), University of Salento, Lecce, Via Monteroni I-73100, Italy.

Department of Experimental Medicine, University of Salento, Lecce, Via Monteroni I-73100, Italy.

出版信息

Bioinorg Chem Appl. 2024 Dec 31;2024:5588491. doi: 10.1155/bca/5588491. eCollection 2024.

Abstract

Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive type of solid tumor that is becoming more common. -[PtCl (NH)] (in short cisplatin or CDDP) has been shown to be effective in treating various cancers, including PDAC. However, the development of resistance to chemotherapy drugs has created a need for the synthesis of new anticancer agents. Platinum-based drugs containing the bidentate ligand phenanthroline have been found to have strong antitumor activity due to their ability to cause DNA damage. In this study, we examined the ability of two Pt (II) cationic complexes, [Pt( -CHOR) (DMSO) (phen)] (in short Pt-EtORSOphen;  = Me, ; Et, ), to inhibit the growth and spread of BxPC-3 PDAC cells, in comparison to CDDP. The length of the alkyl chain and its associated lipophilic properties did not affect the anticancer effects of complexes and in BxPC-3 cells. However, it did appear to influence the rapid loss of mitochondrial membrane potential (ΔΨ), suggesting that these complexes could potentially be used as mitochondria-targeted lipophilic cations in anticancer therapy.

摘要

胰腺导管腺癌(PDAC)是一种侵袭性很强的实体瘤,且越来越常见。顺铂([PtCl₂(NH₃)₂],简称顺铂或CDDP)已被证明对包括PDAC在内的多种癌症有效。然而,化疗药物耐药性的出现使得有必要合成新的抗癌药物。含有双齿配体菲咯啉的铂类药物因其能够引起DNA损伤而具有很强的抗肿瘤活性。在本研究中,我们研究了两种Pt(II)阳离子配合物[Pt(η²-CH₂CH₂OR)(DMSO)(phen)](简称Pt-EtORSOphen;R = Me,R' = Et)与顺铂相比,抑制BxPC-3 PDAC细胞生长和扩散的能力。烷基链的长度及其相关的亲脂性特性并不影响配合物1和2对BxPC-3细胞的抗癌作用。然而,它似乎确实影响线粒体膜电位(ΔΨ)的快速丧失,这表明这些配合物有可能在抗癌治疗中用作线粒体靶向亲脂性阳离子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/77e3/11779987/64a2d834c01c/BCA2024-5588491.001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验