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Appl Biochem Biotechnol. 2010 Mar;160(6):1752-9. doi: 10.1007/s12010-009-8656-2. Epub 2009 May 9.

Inhibition of beta-lactamase by 1,4-naphthalenedione from the plant Holoptelea integrifolia.

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  • 1Department of Biotechnology and Microbiology, Kannur University, Thalassery Campus, Palayad P. O., Kannur, Kerala, 670661, India.


The most important mechanism of the beta-lactam antibiotic resistance is the destruction of the antibiotics by the enzyme beta-lactamase. Use of beta-lactamase inhibitors in combination with antibiotics is one of the successful antibacterial strategies. The inhibitory effect of a phytochemical, 1,4-naphthalenedione, isolated from the plant Holoptelea integrifolia on beta-lactamase is reported here. This compound was found to have a synergistic effect with the antibiotic amoxicillin against a resistant strain of Staphylococcus aureus. The enzyme was purified from the organism and incubated with the compound. An assay showed that the compound can inhibit the enzymatic activity of beta-lactamase. Modeling and molecular docking studies indicated that the compound can fit into the active site of beta-lactamase. Hence, the compound can serve as a potential lead compound for the development of effective beta-lactamase inhibitor that can be used against beta-lactam-resistant microbial strains.

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