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<p>The emergence of multidrug-resistant bacterial strains such as <i>Klebsiella pneumoniae, Acinetobacter baumannii</i>, and methicillin-resistant <i>Staphylococcus aureus</i>, known for their recalcitrant biofilm-forming abilities, poses significant challenges to current antimicrobial therapies. This study evaluates the efficacy of 1-acetyl-4-(4-hydroxyphenyl) piperazine in inhibiting the growth and biofilm formation of these high-priority pathogens, as well as assessing its potential cytotoxicity in mammalian cell lines. The compound demonstrated minimum inhibitory concentration at 1&#xa0;mg/ml against <i>Klebsiella pneumoniae subsp. rhinoscleromatis</i> (MTCC-661) strain, <i>Klebsiella pneumoniae</i>, <i>Acinetobacter baumannii</i> clinical isolates and 0.5&#xa0;mg/ml against methicillin-resistant Staphylococcus aureus (ATCC-MRSA-NR-46071). Molecular docking revealed strong interactions with key biofilm-associated proteins, including YcgR and&#xa0;BlrP1 in <i>Klebsiella pneumoniae</i>, and CarO, Omp38, CsuA/B, and BfmR in <i>Acinetobacter baumannii</i>, with binding energies ranging from −6.0 to −7.2&#xa0;kcal/mol, indicating mechanisms that potentially disrupt biofilm formation. Up to 34% of biofilm reduction was observed at twice the minimum inhibitory concentration among the pathogens, demonstrating dose-dependent inhibition. Additionally, the compound was tested for cytotoxicity in the NIH 3T3 Mouse Fibroblast cell lines, with 93% cell survival at 10&#xa0;mg/ml concentration. These findings suggest that AHPP is a promising candidate for further development into therapeutic agents or coatings designed to combat biofilm-associated infections, offering potent antimicrobial and biofilm inhibitory activities with minimal cytotoxicity.</p> Graphical Abstract <p></p>

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1-acetyl-4-(hydroxylphenyl) piperazine inhibits biofilm formation in ESKAPE pathogens Klebsiella pneumoniae and Acinetobacter baumannii

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年9月26日

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  • Pooja Rao,
  • Jamuna Bai Aswathanarayan,
  • M. V. S. S. T. Subba Rao,
  • V. Ravishankar Rai,
  • G. S. Sowmya

摘要

The emergence of multidrug-resistant bacterial strains such as Klebsiella pneumoniae, Acinetobacter baumannii, and methicillin-resistant Staphylococcus aureus, known for their recalcitrant biofilm-forming abilities, poses significant challenges to current antimicrobial therapies. This study evaluates the efficacy of 1-acetyl-4-(4-hydroxyphenyl) piperazine in inhibiting the growth and biofilm formation of these high-priority pathogens, as well as assessing its potential cytotoxicity in mammalian cell lines. The compound demonstrated minimum inhibitory concentration at 1 mg/ml against Klebsiella pneumoniae subsp. rhinoscleromatis (MTCC-661) strain, Klebsiella pneumoniae, Acinetobacter baumannii clinical isolates and 0.5 mg/ml against methicillin-resistant Staphylococcus aureus (ATCC-MRSA-NR-46071). Molecular docking revealed strong interactions with key biofilm-associated proteins, including YcgR and BlrP1 in Klebsiella pneumoniae, and CarO, Omp38, CsuA/B, and BfmR in Acinetobacter baumannii, with binding energies ranging from −6.0 to −7.2 kcal/mol, indicating mechanisms that potentially disrupt biofilm formation. Up to 34% of biofilm reduction was observed at twice the minimum inhibitory concentration among the pathogens, demonstrating dose-dependent inhibition. Additionally, the compound was tested for cytotoxicity in the NIH 3T3 Mouse Fibroblast cell lines, with 93% cell survival at 10 mg/ml concentration. These findings suggest that AHPP is a promising candidate for further development into therapeutic agents or coatings designed to combat biofilm-associated infections, offering potent antimicrobial and biofilm inhibitory activities with minimal cytotoxicity.

Graphical Abstract