PMID: 6972939Nov 1, 1980Paper

Izumenolide-a novel beta-lactamase inhibitor produced by Micromonospora. II. Biological properties

The Journal of Antibiotics
K BushR B Sykes

Abstract

Izumenolide is a potent inhibitor of beta-lactamases, especially from Gram-negative bacteria. The I50 value of 0.01 microgram/ml for TEM-2 beta-lactamase, after 10 min preincubation, corresponds to a ratio of 7.6 moles inhibitor per mole of enzyme. The initial inhibitory reaction with TEM-2 beta-lactamase exhibits mixed reaction kinetics, suggesting a possible overlapping binding site with the active center. Tem-2 beta-lactamase is irreversible inactivated by izumenolide in a biphasic reaction. Carbenicillin offers partial protection against inactivation. Izumenolide exhibits limited antibiotic activity against some Gram-negative bacteria. Against beta-lactamase producing bacteria izumenolide provides protection to ampicillin and cephaloridine but the protection is limited due to permeability problems associated with izumenolide entry into the cells.

Citations

Jan 1, 1986·Journal of Enzyme Inhibition·C Reading, M Cole
Oct 1, 1983·Medicinal Research Reviews·S J Cartwright, S G Waley

❮ Previous
Next ❯

Related Concepts

Related Feeds

Allergy & Infectious Diseases

Allergies result from the hyperreactivity of the immune system to some environmental substance and can be life-threatening. Infectious diseases are caused by organisms including bacteria, viruses, fungi and parasites. They can be transmitted different ways, such as person-to-person. Here is the latest research on allergy and infectious diseases.

Antimicrobial Resistance (ASM)

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.

Allergy & Infectious Diseases (ASM)

Allergies result from the hyperreactivity of the immune system to some environmental substance and can be life-threatening. Infectious diseases are caused by organisms including bacteria, viruses, fungi and parasites. They can be transmitted different ways, such as person-to-person. Here is the latest research on allergy and infectious diseases.

Antimicrobial Resistance

Antimicrobial resistance poses a significant threat to the continued successful use of antimicrobial agents for the treatment of bacterial infections.

Beta-lactamase Inhibitors

Beta-lactamase inhibitors are a class of antibiotics that inhibit beta-lactamases, a family of enzymes involved in bacterial resistance to beta-lactam antibiotics. Here is the latest research.

Beta-lactamase Inhibitors (ASM)

Beta-lactamase inhibitors are a class of antibiotics that inhibit beta-lactamases, a family of enzymes involved in bacterial resistance to beta-lactam antibiotics. Here is the latest research.