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Mercaptoacetate thioesters and their hydrolysate mercaptoacetic acids jointly inhibit metallo-β-lactamase L1

Cheng Chen1, Yang Xiang1, Ya Liu1

  • 1Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education , Innovation Laboratory of Chemical Biology , College of Chemistry and Materials Science , Northwest University , Xi'an 710127 , P. R. China .

Medchemcomm
|August 16, 2018
PubMed

Insights

New thioesters targeting metallo-β-lactamases (MβLs) show promise against superbugs. Both the thioester compounds and their breakdown products, mercaptoacetic acid, were found to jointly inhibit the L1 enzyme, restoring antibiotic effectiveness.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Antimicrobial Resistance

Background:

  • Metallo-β-lactamases (MβLs) are a growing threat due to 'superbug' infections.
  • L1 is a specific MβL enzyme implicated in these infections.

Purpose of the Study:

  • To investigate the inhibitory mechanism of mercaptoacetate thioesters against the L1 enzyme.
  • To determine if the thioester itself or its hydrolysate is responsible for L1 inhibition.

Main Methods:

  • Synthesis of ten mercaptoacetate thioesters (compounds 1-10).
  • Enzyme inhibition assays to determine IC50 values.
  • UV-vis and HPLC monitoring to assess thioester hydrolysis.
  • STD-NMR to identify binding interactions.

Main Results:

  • Synthesized thioesters specifically inhibited L1 with IC50 values from 0.17 to 1.2 μM, with compound 8 being the most potent (IC50 = 0.17 μM).
  • Thioesters restored cefazolin activity against L1-expressing E. coli by 2-4 fold.
  • L1 hydrolyzed thioesters 1, 8, and 9, producing mercaptoacetic acid, which was detected by HPLC.
  • STD-NMR indicated that both the thioester and mercaptoacetic acid contribute to L1 inhibition.

Conclusions:

  • Mercaptoacetate thioesters are effective inhibitors of the L1 metallo-β-lactamase.
  • Both the intact thioester and its hydrolysate, mercaptoacetic acid, play a role in inhibiting L1.
  • These findings offer a dual-action strategy for developing new antimicrobial agents against MβL-producing superbugs.

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