26 March 2018

Changing the rules of the game

Synthesized antibiotic coped with a dangerous infection

Evgenia Efimova, Vesti

An international team of researchers has successfully synthesized and used for the first time for the treatment of infection a new antibiotic capable of killing dangerous superbugs.

According to scientists, this antibiotic "changes the rules of the game."

We are talking about a natural antibiotic called teixobactin, discovered back in 2015 in soil samples. Now, for the first time, experts have used its synthetic form to treat bacterial infection in laboratory mice, and the results have been positive.

According to scientists, such an achievement is a major step forward towards the development of a drug based on teixobactin. According to experts, it will help in the fight against antibiotic-resistant superbugs, such as methicillin-resistant Staphylococcus aureus and enterococcus resistant to vancomycin.

It's no secret that today scientists around the world are concerned about the problem of antibiotic-resistant bacteria. Last year, a UK government report concluded that by 2050, superbugs could potentially cause up to ten million deaths per year, and earlier this year, WHO published a list of antibiotic–resistant priority pathogens - the first such document in the entire 69-year history of the organization.

For this reason, many specialists are looking for and developing antibiotics that will cope with dangerous enemies.

According to one of the scientists involved in a recent study, Ishwar Singh, when researchers first discovered theixobactin, it already surprised many, because it was able to destroy bacteria without resistance, including superbugs such as methicillin-resistant Staphylococcus aureus.

"Meanwhile, natural theixobactin was not suitable for human use," he notes.

After a while, scientists from the University of Lincoln (Great Britain) created a simplified synthesized version of theixobactin. Experts have developed a whole "library" of synthetic versions of theixobactin, replacing key amino acids in certain places of the structure of the antibiotic to make it easier to re-create.

But at that time, the effectiveness of the new simplified synthesized drug was demonstrated only outside of a living organism – in experiments in a Petri dish (in vitro).

And recently, researchers from the Singapore Ophthalmology Research Institute have shown that one synthetic version of the drug can successfully cope with bacterial infection in mice. It was about keratitis caused by Staphylococcus aureus.

As part of the study, scientists have shown that such a simplified version of an antibiotic can be used to treat real bacterial infections and be the basis for a new drug.

Synthesized theixobactin also reduced the severity of infection in animals, which did not occur in the case of clinically used moxifloxacin. The latter was used as a control.

"The fact that we started using such simplified synthetic versions in real cases after testing with test tubes is a quantum leap in the development of new antibiotics. All this brings us closer to realizing the therapeutic potential of simplified theixobactin," says Singh.

According to him, there is still a significant amount of work to be done to develop teixobactin as a therapeutic antibiotic for human use. Probably, it will take another 6-10 years before doctors will be able to prescribe the drug to patients, the specialist believes.

"But this is a real step in the right direction, and now it opens the door to improving our analogues in experiments in the body of living models," concludes Singh.

The authors presented the results of the study in the Journal of Medicinal Chemistry.

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