Interaction of beta-lactamase of Streptomyces cacaoi. I. Clavulanic acid and PS-5. 1981

H Ogawara, and A Mantoku

Inactivation of a beta-lactamase of Streptomyces cacaoi by clavulanic acid and PS-5 was investigated and compared with that of a beta-lactamase of Bacillus cereus. Inhibition of the enzymes induced by clavulanic acid and the beta-lactam antibiotic PS-5 was found to be progressive with time. However, the degree of inhibition of the beta-lactamase from S. cacaoi increased more progressively with time than that of the enzyme from B. cereus. Conformative response constants were determined. As compared with clavulanic acid, over ten times higher concentrations of PS-5 were necessary to give a similar degree of inhibition. At lower concentrations, both clavulanic acid and PS-5 behaved as competitive inhibitors. Ki values calculated from the integrated form of the LINEWEAVER-BURK type were 1.1 X 10(-7) M and 7.6 X 10(-6) M for clavulanic acid and PS-5, respectively.

UI MeSH Term Description Entries
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D013302 Streptomyces A genus of bacteria that form a nonfragmented aerial mycelium. Many species have been identified with some being pathogenic. This genus is responsible for producing a majority of the ANTI-BACTERIAL AGENTS of practical value.
D013845 Thienamycins Beta-lactam antibiotics that differ from PENICILLINS in having the thiazolidine sulfur atom replaced by carbon, the sulfur then becoming the first atom in the side chain. They are unstable chemically, but have a very broad antibacterial spectrum. Thienamycin and its more stable derivatives are proposed for use in combinations with enzyme inhibitors. Antibiotics, Thienamycin,Thienamycin Antibiotics
D047090 beta-Lactams Four-membered cyclic AMIDES, best known for the PENICILLINS based on a bicyclo-thiazolidine, as well as the CEPHALOSPORINS based on a bicyclo-thiazine, and including monocyclic MONOBACTAMS. The BETA-LACTAMASES hydrolyze the beta lactam ring, accounting for BETA-LACTAM RESISTANCE of infective bacteria. beta-Lactam,4-Thia-1-Azabicyclo(3.2.0)Heptanes,4-Thia-1-Azabicyclo(4.2.0)Octanes,beta Lactam,beta Lactams
D019818 Clavulanic Acid A beta-lactam antibiotic produced by the actinobacterium Streptomyces clavuligerus. It is a suicide inhibitor of bacterial beta-lactamase enzymes. Administered alone, it has only weak antibacterial activity against most organisms, but given in combination with other beta-lactam antibiotics it prevents antibiotic inactivation by microbial lactamase. Clavulanate,BRL-14151,Clavulanate Potassium,Clavulanic Acid, Monopotassium Salt,Clavulanic Acid, Monosodium Salt,MM-14151,Potassium Clavulanate,Sodium Clavulanate,BRL 14151,BRL14151,Clavulanate, Potassium,Clavulanate, Sodium,MM 14151,MM14151,Potassium, Clavulanate
D065093 beta-Lactamase Inhibitors Endogenous substances and drugs that inhibit or block the activity of BETA-LACTAMASES. beta Lactamase Inhibitor,beta Lactamase Inhibitors,beta-Lactamase Inhibitor,beta Lactamase Antagonists,Antagonists, beta Lactamase,Inhibitor, beta Lactamase,Inhibitor, beta-Lactamase,Inhibitors, beta Lactamase,Inhibitors, beta-Lactamase,Lactamase Antagonists, beta,Lactamase Inhibitor, beta,Lactamase Inhibitors, beta

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