Charles R.M. Soukup , Rebekah N. Duffin , Kirralee J. Burke , Laurence Meagher , Philip C. Andrews
{"title":"The antibacterial activity and selectivity of bismuth(III) tris(8-hydroxyquinolinates)","authors":"Charles R.M. Soukup , Rebekah N. Duffin , Kirralee J. Burke , Laurence Meagher , Philip C. Andrews","doi":"10.1016/j.jinorgbio.2025.112836","DOIUrl":null,"url":null,"abstract":"<div><div>The series of bismuth(III) <em>tris</em>(8-hydroxyquinolinates); [Bi(Q\")<sub>3</sub>] (<strong>1</strong>)<strong>,</strong> [Bi(Q'Cl)<sub>3</sub>] (<strong>2</strong>)<strong>,</strong> [Bi(QCl<sub>2</sub>)<sub>3</sub>] (<strong>3</strong>)<strong>,</strong> [Bi(QBr<sub>2</sub>)<sub>3</sub>] (<strong>4</strong>)<strong>,</strong> and [Bi(QI<sub>2</sub>)<sub>3</sub>] (<strong>5</strong>) (where Q\"-<em>H</em> = C<sub>9</sub>H<sub>7</sub>NO; Q'Cl-<em>H</em> = C<sub>9</sub>H<sub>6</sub>NOCl, QCl<sub>2</sub>-<em>H</em> = C<sub>9</sub>H<sub>5</sub>NOCl<sub>2</sub>; QBr<sub>2</sub>-<em>H</em> = C<sub>9</sub>H<sub>5</sub>NOBr<sub>2</sub>; and QI<sub>2</sub>-<em>H</em> = C<sub>9</sub>H<sub>5</sub>NOI<sub>2</sub>) were synthesised, fully characterised, and evaluated for their antibacterial activity towards three Gram-positive bacteria (vancomycin-resistant <em>E. faecalis</em>, <em>S. aureus</em>, methicillin-resistant <em>S. aureus</em>), and four Gram-negative bacteria (<em>A. baumannii</em>, <em>P. aeruginosa</em>, <em>K. pneumoniae</em>, and <em>E. coli</em>) and also their cytotoxicity towards mammalian cells. New crystallographic data on <strong>4</strong> indicates it is dimeric in the solid state through ‘Bi<sub>2</sub>O<sub>2</sub>’ bridging which is consistent with data previously reported for <strong>5</strong>. The five complexes (<strong>1–5)</strong> all exhibited good but variable antibacterial activity and selectivity. Complexes <strong>2</strong> and <strong>5</strong> showed significant activity towards Gram-positive bacteria with MIC (minimum inhibitory concentration) values ranging from 0.78 μM – 3.13 μM and selectivity indices of 6.2 – ≥16.0. For Gram-negative species, complexes <strong>3</strong> and <strong>4</strong> exhibited highly selective activity towards multi-drug resistant strains of <em>A. baumannii</em> with a range of MIC values 0.39–1.56 μM and selectivity indices of 3.14–7.23 respectively. While some of the 8-hydroxyquinolines themselves show reasonable antibacterial activity this is generally enhanced through complexation to bismuth(III).</div></div>","PeriodicalId":364,"journal":{"name":"Journal of Inorganic Biochemistry","volume":"266 ","pages":"Article 112836"},"PeriodicalIF":3.8000,"publicationDate":"2025-01-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Inorganic Biochemistry","FirstCategoryId":"99","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0162013425000169","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
The series of bismuth(III) tris(8-hydroxyquinolinates); [Bi(Q")3] (1), [Bi(Q'Cl)3] (2), [Bi(QCl2)3] (3), [Bi(QBr2)3] (4), and [Bi(QI2)3] (5) (where Q"-H = C9H7NO; Q'Cl-H = C9H6NOCl, QCl2-H = C9H5NOCl2; QBr2-H = C9H5NOBr2; and QI2-H = C9H5NOI2) were synthesised, fully characterised, and evaluated for their antibacterial activity towards three Gram-positive bacteria (vancomycin-resistant E. faecalis, S. aureus, methicillin-resistant S. aureus), and four Gram-negative bacteria (A. baumannii, P. aeruginosa, K. pneumoniae, and E. coli) and also their cytotoxicity towards mammalian cells. New crystallographic data on 4 indicates it is dimeric in the solid state through ‘Bi2O2’ bridging which is consistent with data previously reported for 5. The five complexes (1–5) all exhibited good but variable antibacterial activity and selectivity. Complexes 2 and 5 showed significant activity towards Gram-positive bacteria with MIC (minimum inhibitory concentration) values ranging from 0.78 μM – 3.13 μM and selectivity indices of 6.2 – ≥16.0. For Gram-negative species, complexes 3 and 4 exhibited highly selective activity towards multi-drug resistant strains of A. baumannii with a range of MIC values 0.39–1.56 μM and selectivity indices of 3.14–7.23 respectively. While some of the 8-hydroxyquinolines themselves show reasonable antibacterial activity this is generally enhanced through complexation to bismuth(III).
期刊介绍:
The Journal of Inorganic Biochemistry is an established international forum for research in all aspects of Biological Inorganic Chemistry. Original papers of a high scientific level are published in the form of Articles (full length papers), Short Communications, Focused Reviews and Bioinorganic Methods. Topics include: the chemistry, structure and function of metalloenzymes; the interaction of inorganic ions and molecules with proteins and nucleic acids; the synthesis and properties of coordination complexes of biological interest including both structural and functional model systems; the function of metal- containing systems in the regulation of gene expression; the role of metals in medicine; the application of spectroscopic methods to determine the structure of metallobiomolecules; the preparation and characterization of metal-based biomaterials; and related systems. The emphasis of the Journal is on the structure and mechanism of action of metallobiomolecules.