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5-Methylindole kills various bacterial pathogens and potentiates aminoglycoside against methicillin-resistant

Zhongyan Li1, Fengqi Sun1, Xinmiao Fu1

  • 1Fujian Normal University, Fuzhou, Fujian, China.

Peerj
|September 20, 2022
PubMed

Insights

5-methylindole demonstrates potent antibacterial activity against diverse pathogens, including resistant strains. This indole derivative also enhances aminoglycoside antibiotic efficacy, offering new therapeutic strategies.

Area of Science:

  • Microbiology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Antibiotic resistance poses a significant global health threat, necessitating novel therapeutic approaches.
  • Developing new antibiotics and improving existing ones are crucial for combating resistant bacterial infections.

Purpose of the Study:

  • To investigate the antibacterial potential of 5-methylindole, an indole derivative.
  • To evaluate 5-methylindole's efficacy against various Gram-positive and Gram-negative pathogens, including antibiotic-resistant strains.
  • To determine if 5-methylindole can potentiate the activity of existing antibiotics.

Main Methods:

  • Testing the direct antibacterial activity of 5-methylindole against a panel of bacterial pathogens.
  • Assessing the synergistic effects of 5-methylindole in combination with aminoglycoside and fluoroquinolone antibiotics.
  • Evaluating the efficacy of 5-methylindole against specific resistant strains like methicillin-resistant Staphylococcus aureus and multidrug-resistant Klebsiella pneumoniae.

Main Results:

  • 5-methylindole exhibited direct bactericidal activity against both Gram-positive and Gram-negative bacteria.
  • The compound was effective against challenging pathogens, including methicillin-resistant Staphylococcus aureus, multidrug-resistant Klebsiella pneumoniae, Mycobacterium tuberculosis, and antibiotic-tolerant persisters.
  • 5-methylindole significantly enhanced the killing efficacy of aminoglycoside antibiotics against Staphylococcus aureus, while 5-iodoindole also showed similar potentiation.

Conclusions:

  • 5-methylindole represents a promising new class of antibacterial agents.
  • Indole derivatives, such as 5-methylindole, offer a novel strategy for developing new treatments against antibiotic-resistant bacteria.
  • 5-methylindole can serve as an effective adjuvant to aminoglycoside antibiotics, potentially revitalizing their use against resistant infections.
Keywords:
5-MethylindoleAminoglycosideAntibiotic resistanceAntibiotic toleranceGram-positive bacteriaIndoleMRSAPersisterStaphylococcus aureus

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