Identification of ruthenium (II) complexes with furan‐substituted ligands as possible antibacterial agents against Staphylococcus aureus
| Autor: | Mao Lingyu, Guangbin Jiang, Jintao Wang, Guijuan Jiang, Xiangwen Liao, Jing Wang, Bin Huang |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Staphylococcus aureus
Pyridines medicine.drug_class Stereochemistry Phenanthroline Antibiotics chemistry.chemical_element Microbial Sensitivity Tests Ligands medicine.disease_cause Biochemistry Ruthenium Mice Structure-Activity Relationship chemistry.chemical_compound Bipyridine Coordination Complexes Drug Discovery medicine Animals Humans Furans Pharmacology Mice Inbred BALB C Organic Chemistry Staphylococcal Infections Antimicrobial Anti-Bacterial Agents chemistry Biofilms Molecular Medicine Female Growth inhibition Antibacterial activity Phenanthrolines |
| Zdroj: | Chemical Biology & Drug Design. 98:885-893 |
| ISSN: | 1747-0285 1747-0277 |
| DOI: | 10.1111/cbdd.13943 |
| Popis: | The growing burden of antibiotic resistance worldwide calls for developing new classes of antimicrobial strategy. Recently years, the use of adjuvants that rescue antibiotics identified as a promising strategy for overcoming bacterial resistance. In this study, three ruthenium complexes functionalized with furan-substituted ligands([Ru(phen)2 (CAPIP)](ClO4 )2 (Ru(Ⅱ)-1), [Ru(dmp)2 (CAPIP)](ClO4 )2 (Ru(Ⅱ)-2) and [Ru(dmb)2 (CAPIP)](ClO4 )2 (Ru(Ⅱ)-3) (dmb=4,4'-dimethyl-2,2'-bipyridine, phen=1,10-phenanthroline, dmp=2,9-dimethyl-1,10-phenanthroline, CAPIP=(E)-2- (2-(furan-2-yl)vinyl)-1H-imidazo[4,5-f][1,10]phenanthroline)) were designed and synthesized. The antimicrobial activities of all compounds against S. aureus were assessed by growth inhibition assays. The MIC values of three complexes range from 0.015 to 0.050 mg/ml. Subsequently, the Ru(II)-2 complexes which exhibited strongest antibacterial activity were further tested against bacteria biofilms formation and toxin secretion. In addition, aimed to test whether ruthenium complexes have potential value as antimicrobial adjuvants, the synergism between Ru(Ⅱ)-2 and some antibiotics against S. aureus were examined through checkerboard method. Interestingly, Ru(Ⅱ)-2 could not only effectively inhibit biofilms formation of S. aureus and inhibit the hemolysin toxin secretion, but also selectivity show synergism with two common antibiotics. More importantly, mouse infection study also verified Ru(Ⅱ)-2 were highly effective against S. aureus in vivo. |
| Databáze: | OpenAIRE |
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