Erika Stefàno, Gianluca Rovito, Luca G Cossa, Federica De Castro, Viviana Vergaro, Asjad Ali, Giulia My, Danilo Migoni, Antonella Muscella, Santo Marsigliante, Michele Benedetti, Francesco Paolo Fanizzi
{"title":"新型Pt （II）复合物对胰腺导管腺癌细胞具有抗癌活性。","authors":"Erika Stefàno, Gianluca Rovito, Luca G Cossa, Federica De Castro, Viviana Vergaro, Asjad Ali, Giulia My, Danilo Migoni, Antonella Muscella, Santo Marsigliante, Michele Benedetti, Francesco Paolo Fanizzi","doi":"10.1155/bca/5588491","DOIUrl":null,"url":null,"abstract":"<p><p>Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive type of solid tumor that is becoming more common. <i>cis</i>-[PtCl<sub>2</sub> (NH<sub>3</sub>)<sub>2</sub>] (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(<i>η</i> <sup>1</sup>-C<sub>2</sub>H<sub>4</sub>OR) (DMSO) (phen)]<sup>+</sup> (in short Pt-EtORSOphen; <i>R</i> = Me, <b>1</b>; Et, <b>2</b>), 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 <b>1</b> and <b>2</b> in BxPC-3 cells. However, it did appear to influence the rapid loss of mitochondrial membrane potential (ΔΨ<sub>M</sub>), suggesting that these complexes could potentially be used as mitochondria-targeted lipophilic cations in anticancer therapy.</p>","PeriodicalId":8914,"journal":{"name":"Bioinorganic Chemistry and Applications","volume":"2024 ","pages":"5588491"},"PeriodicalIF":4.7000,"publicationDate":"2024-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11779987/pdf/","citationCount":"0","resultStr":"{\"title\":\"Novel Pt (II) Complexes With Anticancer Activity Against Pancreatic Ductal Adenocarcinoma Cells.\",\"authors\":\"Erika Stefàno, Gianluca Rovito, Luca G Cossa, Federica De Castro, Viviana Vergaro, Asjad Ali, Giulia My, Danilo Migoni, Antonella Muscella, Santo Marsigliante, Michele Benedetti, Francesco Paolo Fanizzi\",\"doi\":\"10.1155/bca/5588491\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive type of solid tumor that is becoming more common. <i>cis</i>-[PtCl<sub>2</sub> (NH<sub>3</sub>)<sub>2</sub>] (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(<i>η</i> <sup>1</sup>-C<sub>2</sub>H<sub>4</sub>OR) (DMSO) (phen)]<sup>+</sup> (in short Pt-EtORSOphen; <i>R</i> = Me, <b>1</b>; Et, <b>2</b>), 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 <b>1</b> and <b>2</b> in BxPC-3 cells. However, it did appear to influence the rapid loss of mitochondrial membrane potential (ΔΨ<sub>M</sub>), suggesting that these complexes could potentially be used as mitochondria-targeted lipophilic cations in anticancer therapy.</p>\",\"PeriodicalId\":8914,\"journal\":{\"name\":\"Bioinorganic Chemistry and Applications\",\"volume\":\"2024 \",\"pages\":\"5588491\"},\"PeriodicalIF\":4.7000,\"publicationDate\":\"2024-12-31\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11779987/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioinorganic Chemistry and Applications\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1155/bca/5588491\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q1\",\"JCRName\":\"BIOCHEMISTRY & MOLECULAR BIOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioinorganic Chemistry and Applications","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1155/bca/5588491","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/1/1 0:00:00","PubModel":"eCollection","JCR":"Q1","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
Novel Pt (II) Complexes With Anticancer Activity Against Pancreatic Ductal Adenocarcinoma Cells.
Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive type of solid tumor that is becoming more common. cis-[PtCl2 (NH3)2] (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(η1-C2H4OR) (DMSO) (phen)]+ (in short Pt-EtORSOphen; R = Me, 1; Et, 2), 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 1 and 2 in BxPC-3 cells. However, it did appear to influence the rapid loss of mitochondrial membrane potential (ΔΨM), suggesting that these complexes could potentially be used as mitochondria-targeted lipophilic cations in anticancer therapy.
期刊介绍：
Bioinorganic Chemistry and Applications is primarily devoted to original research papers, but also publishes review articles, editorials, and letter to the editor in the general field of bioinorganic chemistry and its applications. Its scope includes all aspects of bioinorganic chemistry, including bioorganometallic chemistry and applied bioinorganic chemistry. The journal welcomes papers relating to metalloenzymes and model compounds, metal-based drugs, biomaterials, biocatalysis and bioelectronics, metals in biology and medicine, metals toxicology and metals in the environment, metal interactions with biomolecules and spectroscopic applications.
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