Scientists have identified a new group of antibacterial molecules

Scientists from Karolinska Institutet, Umeå University, and the University of Bonn have identified a new group of antibacterial molecules that are effective even against antibiotic-resistant bacteria.

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Since their properties can be easily changed by chemical manipulation, could become the basis for the development of a new, effective class of antibiotics with low side effects.

The growing worldwide resistance to antibiotics is a very serious, even alarming problem. Meanwhile, very few new treatments for fighting bacteria are available – only a few new types of antibiotics have been developed in the last 50 years. Thus, there is a great need to find new antimicrobial substances.

Most antibiotics used in clinical practice work by inhibiting the ability of bacteria to form a protective cell wall and are therefore easily lysed (destroyed). This is how, for example, the well-known penicillin works.

There are also newer antibiotics, such as daptomycin and the recently discovered teixobactin, that bind to a special molecule called lipid II. Lipid II is needed by all bacteria to build a cell wall.

Antibiotics, which work by inhibiting the components of the bacterial cell wall (including lipid II), preventing their proper synthesis, are usually very large and complex molecules. It is quite difficult to improve them by chemical methods.

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Additionally, in most cases they are ineffective against a group of bacteria surrounded by an additional layer (outer membrane) that prevents the penetration of drugs into the cell.

“Lipid II, however, is still a very attractive target for new antibiotics,” says Prof. Birgitta Henriques, one of the authors of the publication.

“We were able to identify the first small antimicrobial substances that work by binding to this molecule, and importantly, we did not find any resistant bacterial mutants eluding it. It is very promising, ”she noted.

Together with colleagues from several other research facilities, Henriques tested a large number of chemicals for their ability to lyse pneumococci, the bacteria that is the most common cause of community acquired pneumonia. She discovered that a certain group of molecules – the so-called THCz – inhibits the formation of the bacterial cell wall by binding to lipid II.

THCz can also prevent the formation of the polysaccharide shell that pneumococci need to elude our immune system and cause disease.

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“The advantage of such small molecules is that they are easier to chemically modify,” explains another co-author of the study, Prof. Fredrik Almqvist. “We hope to be able to alter the properties of THCz so as to increase their anti-microbial properties and reduce any negative effects on human cells,” he said.

Laboratory experiments revealed that THCz has antibacterial activity against many pathogens resistant to antibiotics currently in use: methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant pneumococci. They have also been shown to be effective against gonorrhea-causing gonococci and mycobacterium tuberculosis.

However, scientists did not identify the bacteria that developed resistance to THCz in the laboratory environment.

“In the next stage, we want to start chemical modifications of the THCz molecule, which will allow it to penetrate the outer cell membrane found in some multiresistant bacteria” – the researchers announce.

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About Banner Leon

Videogames entered his life in the late '80s, at the time of the first meeting with Super Mario Bros, and even today they make it a permanent part, after almost 30 years. Pros and defects: he manages to finish Super Mario Bros in less than 5 minutes but he has never finished Final Fight with a credit ... he's still trying.

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