Synthesis, Characterization, and Biological Activity of New 4‘-Functionalized Bis-Terpyridine Ruthenium(II) Complexes: Anti-Inflammatory Activity Advances

Theodor Bilharz Research Institute

Bibliographic Information

Authors: Elnagar M.M.; Abou-El-Sherbini K.S.; Samir S.; Sharmoukh W.; Abdel-Aziz M.S.; Shaker Y.M.

Journal: ChemMedChem

Publisher: John Wiley and Sons Ltd

Publication Date: 21 November 2024

Volume / Issue: Volume 20 / Issue 3

Article No.: e202400680

ISSN: 18607179

DOI: 10.1002/cmdc.202400680

Scopus: View on Scopus

PubMed: 39417784

Document Type: Article

Access: All Open Access; Green Open Access; Hybrid Gold Open Access

Authors and Affiliations

Elnagar M.M., Institute of Electrochemistry, Ulm University, Albert-Einstein-Allee 47, Ulm, 89081, Germany, Department of Inorganic Chemistry, National Research Centre, 33 El Bohouth St. (former Tahrir St.), Dokki, Giza, 12622, Egypt; Abou-El-Sherbini K.S., Department of Inorganic Chemistry, National Research Centre, 33 El Bohouth St. (former Tahrir St.), Dokki, Giza, 12622, Egypt; Samir S., Department of Biochemistry and Molecular Biology, Theodor Bilharz Research Institute, P.O. Box 30, Giza, Egypt; Sharmoukh W., Department of Inorganic Chemistry, National Research Centre, 33 El Bohouth St. (former Tahrir St.), Dokki, Giza, 12622, Egypt; Abdel-Aziz M.S., Department of Microbial Chemistry, National Research Centre, 33 El Bohouth St. (former Tahrir St.), Dokki, Giza, 12622, Egypt; Shaker Y.M., Division of Pharmaceutical and Drug Industries, Department of the Chemistry of Natural and Microbial Products, National Research Centre, El Buhouth Street, Dokki, Cairo, 12622, Egypt

Abstract

Ruthenium complexes incorporating 2,2′ : 6′,2′′-terpyridine ligands have emerged as promising candidates due to their versatile biological activities including DNA-binding, anti-inflammatory, antimicrobial, and anticancer properties. In this study, three new 4′-functionalized bis(terpyridine) Ru(II) complexes were synthesized. These complexes feature one ligand as 4-(2,2′ : 6′,2′′-terpyridine-4′-yl) benzoic acid and the second ligand as either 4′-(2-thienyl)-2,2′ : 6′,2′′-terpyridine, 4′-(3,4-dimethoxyphenyl)-2,2′ : 6′,2′′-terpyridine, or 4′-(4-dimethylaminophenyl)-2,2′ : 6′,2′′-terpyridine. Besides the chemical characterization by 1H and 13C NMR, mass spectrometry, and absorption and emission spectroscopy, the complexes were tested for their biological activity as anti-inflammatory, anticancer, and antimicrobial agents. Moreover, the toxicity of the Ru(II) complexes was assessed and benchmarked against diclofenac potassium and ibuprofen using a haemolysis assay. Biological evaluations demonstrate that these ruthenium complexes exhibit promising therapeutic potential with reduced haemolytic activity compared to standard drugs. They demonstrate substantial anti-inflammatory effects through inhibition of albumin denaturation along with moderate cytotoxicity against cancer cell lines and broad-spectrum antimicrobial activity. These findings highlight the multifaceted biomedical applications of 4′-functionalized bis(terpyridine) Ru(II) complexes, suggesting their potential for further development as effective and safe therapeutic agents. © 2024 The Authors. ChemMedChem published by Wiley-VCH GmbH.

Keywords

Anti-cancer; Anti-inflammatory; Antimicrobial agents; Biological activity; Ru(II) complexes; Terpyridine; Animals; Anti-Bacterial Agents; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Antineoplastic Agents; Cell Line, Tumor; Coordination Complexes; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Microbial Sensitivity Tests; Molecular Structure; Pyridines; Ruthenium; Structure-Activity Relationship; albumin; antibiotic agent; antifungal agent; antiinfective agent; antiinflammatory agent; antineoplastic agent; cycloheximide; diclofenac potassium; ibuprofen; pyridine derivative; ruthenium complex; tetracycline; unclassified drug; [4 ([2,2':6',2'' terpyridin] 4' yl) n,n dimethylaniline][4 ([2,2':6',2'' terpyridin] 4' yl)benzoic acid ruthenium di(hexafluoro lambda 6 phosphane); [4' (3,4 dimethoxyphenyl) 2,2':6',2'' terpyridine][4 ([2,2':6',2'' terpyridin] 4' yl)benzoic acid ruthenium di(hexafluoro lambda 6 phosphane); [4' (thiophen 2 yl) 2,2':6',2'' terpyridine][4 ([2,2':6',2'' terpyridin] 4' yl)benzoic acid ruthenium di(hexafluoro lambda 6 phosphane); coordination compound; nonsteroid antiinflammatory agent; animal cell; antifungal activity; antiinflammatory activity; antimicrobial activity; antineoplastic activity; Article; Aspergillus niger; benchmarking; cancer cell line; Candida albicans; carbon nuclear magnetic resonance; controlled study; drug cytotoxicity; drug synthesis; hemolysis; hemolysis assay; human; human cell; ligand binding; mass spectrometry; nonhuman; protein denaturation; proton nuclear magnetic resonance; Pseudomonas aeruginosa; Staphylococcus aureus; animal; chemical structure; chemistry; dose response; drug screening; microbial sensitivity test; structure activity relation; synthesis; tumor cell line

Citation Information

Scopus Citations: 2

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