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Scientists develop more powerful form of vancomycin

Researchers at The Scripps Research Institute structurally modified vancomycin to create an even more potent and durable version of the antibiotic — a discovery that could eliminate the threat of antibiotic-resistant infections for years into the future, according to findings published in Proceedings of the National Academy of Sciences.

Studying the original drug is an ideal starting point for improving antibiotics, according to a related press release. After 60 years of clinicians prescribing the original form of vancomycin, bacteria are just now developing resistance to it, suggesting that the drug’s original mechanism of action — disturbing how bacteria form cell walls — creates a difficult barrier for bacteria to overcome, according to the release.

Previous studies by researchers at The Scripps Research Institute (TSRI) revealed that adding two modifications to vancomycin make it more powerful.

“With these modifications, you need less of the drug to have the same effect,” Dale Boger, PhD, lead researcher and co-chair of TSRI’s department of chemistry, said in the release.

The current study found that making a third modification in combination with the previous alterations increases vancomycin’s activity 1,000-fold. This modification allows clinicians to prescribe less of the antibiotic to fight infection. The new form of vancomycin has three independent mechanisms of action, making it the first antibiotic of its kind, according to the release.

“This increases the durability of this antibiotic,” Boger said. “Organisms just can't simultaneously work to find a way around three independent mechanisms of action. Even if they found a solution to one of those, the organisms would still be killed by the other two.”

The researchers found that the new version of vancomycin is able to kill both vancomycin-resistant enterococci bacteria and the original forms of enterococci.

“Doctors could use this modified form of vancomycin without fear of resistance emerging,” Boger said.

The current method of synthesizing the modified vancomycin in the lab takes 30 steps, thus the next phase of research will be to design a method with fewer stages; however, when compared with creating a new molecule, this phase will be “easy,” according to Boger.

The new version of vancomycin and its lifesaving powers make its production valuable even if the process is not streamlined, Boger said.

“Antibiotics are total cures for bacterial infections,” he added. “Making this molecule is important, even by the current approach, if the failure of antibiotics continues.” – by Alaina Tedesco

Disclosure: The researchers report funding from NIH.