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Penicillin redux: Rearming proven warriors for the 21st century
Date:4/14/2014

but differ in the surrounding molecular "shrubbery." Physicians heavily use the many versions of beta-lactam antibiotics to fight bacterial infections, and many have been retired because they're no longer effective against the defenses bacteria have evolved in response.

One of the most effective bacterial defenses is an enzyme called beta-lactamase, which chews up the beta-lactam structure. Some bacteria, such as MRSA, have developed the ability to biosynthesize and release beta-lactamase when needed. It's a devastating defense because it's so general, targeting the common structural motif in all of the many beta-lactam antibiotics.

But that also creates the opportunity for a general approach to solving the problem, which is what Carolina's Chuanbing Tang and colleagues just reported in the Journal of the American Chemical Society.

"Instead of developing new antibiotics, here we ask the question, 'can we recycle the old antibiotics?' " he said. "With traditional antibiotics like penicillin G, amoxicillin, ampicillin and so on, can we give them new life?"

The approach pairs the drug with a protective polymer developed in Tang's chemistry laboratory. In lab tests, graduate student Jiuyang Zhang prepared a cobaltocenium metallopolymer that greatly slowed the destructiveness of beta-lactamase on a model beta-lactam molecule (nitrocefin).

The interdisciplinary team, which included Mitzi Nagarkatti and Alan Decho, from the university's School of Medicine and Arnold School of Public Health, respectively, also showed that the antimicrobial effectiveness of the four beta-lactams studied in detail was enhanced by the polymer. The enhancement was modest against two strains, but very pronounced with the hospital-associated strain of MRSA (HA-MRSA).

The metallopolymer by itself even demonstrated antimicrobial properties, lysing bacterial cells while leaving human red blood cells unaffected. By a variety of measures, t
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Contact: Steven Powell
803-777-1923
University of South Carolina
Source:Eurekalert  

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