Cefmenoxime (SCE-1365) の各種β-lactamaseおよびペニシリン結合タンパク質に対する親和性とその抗菌力との関係

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  • CEFMENOXIME (SCE-1365), A NEW PARENTERAL CEPHALOSPORIN, ITS STABILITY AND AFFINITY TO β-LACTAMASES AND PENICILLIN-BINDING PROTEINS AND ANTIBACTERIAL ACTIVITY
  • Cefmenoxime SCE 1365 ノ カクシュ ベータ lactama

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A new parenteral cephalosporin, cefmenoxime (CMX, SCE-1365), was studied for the stability and affinities to β-lactamases and penicillin-binding proteins (PBP: mureintranspeptidases) and for the influence of the drug on bactericidal activity of the serum-complement and phagocytosis by macrophages.<BR>Cefmenoxime was not only stable to all types of β-lactamases, except the type V that hydrolyzed the drug slightly, but also possessed a high Ki values (low binding affinity) to the type III (TEM)β-lactamase controlled by major of trensferable R (bla) plasmids. In fact, substrains of Escherichia coli CSH2 carrying 53 different R (bla) plasmids did not change the susceptibilities to cefmenoxime suggesting that the drug manifests strong antibacterial activity to various gram-negative bacteria regardless of the inheritance of R plasmids.<BR>It was revealed that cefmenoxime possesses a high binding affinity to the PBP I A and III followed by those to PBP IB and II. A strong antibacterial activityof this drug was elucidated to be based upon the good inhibitory effect on the target enzymes and satisfactory penetrability through the outer membrane of gramnegative bacilli addition to the high stability to β-lactamases.<BR>Gram-negative rods grown with subinhibitory concentrations of cefmenoxime were easily killed by the complement in sera and well phagocytized and digested by macrophages derived from mice indicating that the drug can be expected for the excellent in vivo antimicrobial activity.

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