Abstract

Silver(I) complexes with aromatic nitrogen-containing heterocycles have shown an effective and wide-spectrum of antimicrobial activity. The possible mechanism of their antimicrobial activity can be attributed to interactions of these complexes with biomolecules, including DNA and proteins. Herein, we investigated the interactions of two antimicrobial active dinuclear phthalazine-silver(I) complexes, [{Ag(NO3)(phtz)}2(μ-phtz)2] (Ag1) and [{Ag(CF3SO3)(phtz)}2(μ-phtz)2] (Ag2) (phtz is phthalazine), with calf thymus DNA (ctDNA) and bovine serum albumin (BSA) to evaluate their binding affinities towards these biomolecules for possible insights on their mode of antimicrobial activity. The value of binding constants (KA) of Ag1 and Ag2 to BSA is higher than that for DNA, indicating greater affinity of the complexes toward this model protein. The partition coefficient (logP) values for Ag1 and Ag2 are 0.0035 and -0.0063, respectively, what is in accordance with higher cellular uptake efficiency and better antibacterial activity of Ag1 in respect to Ag2. In order to determine the therapeutic potential of Ag1 and Ag2 complexes, their toxicity in vivo against nematode, Caenorhabditis elegans, was investigated.

Highlights

  • ✓ Silver(I) complexes showed significant antimicrobial activity against the strains which are resistant to the currently used antimicrobial drugs, while their toxicity to the normal human cells was not pronounced

  • We investigated the interactions of two antimicrobial active dinuclear phthalazine-silver(I) complexes, [{Ag(NO3)(phtz)}2(μ-phtz)2] (Ag1) and [{Ag(CF3SO3)(phtz)}2(μ-phtz)2] (Ag2), with calf thymus DNA and bovine serum albumin (BSA) to evaluate their binding affinities towards these biomolecules for possible insights on their mode of antimicrobial activity

  • The partition coefficient values for Ag1 and Ag2 are 0.0035 and -0.0063, respectively, what is in accordance with higher cellular uptake efficiency and better antibacterial activity of Ag1 in respect to Ag2

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Summary

Introduction

✓ Silver(I) complexes showed significant antimicrobial activity against the strains which are resistant to the currently used antimicrobial drugs, while their toxicity to the normal human cells was not pronounced. Kragujevac, Serbia 2Institute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11042 Belgrade, Serbia 3University of Kragujevac, Institute for Information Technologies Kragujevac, Department of Science, Jovana Cvijića bb, 34000 Kragujevac, Serbia 4Serbian Academy of Sciences and Arts, Knez Mihailova 35, 11000 The possible mechanism of their antimicrobial activity can be attributed to interactions of these complexes with biomolecules, including DNA and proteins.

Results
Conclusion

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