Scientists tweak 80-year-old antibiotic for new medical uses

"Gramicidin A" was originally discovered in soil bacteria and was the first commercially produced

antibiotic in the early 1940s.Today, doctors continue to prescribe it as a cream or topical drops for certain skin, eye, and throat infections. However, it cannot be used in tablet or injection form. 

Recently, a team from the Department of Pharmaceutical Sciences of the University of Tokyo developed and analyzed over 4,000 artificial analogues of Gramicidin A.

"Gramicidin A" is a spiral of15 amino acids. The researchers strategically selected six of those amino acids that could be changed without losing essential aspects of the normal structure of gramicidin A. Each of these six amino acids could be replaced with four different amino acids to change the way the peptides bind, resulting in a total of 4,096 variations.

Researchers started testing their newversion of "Gramicidin A" for activity against streptococcus, a common bacterial infection. The strongest participants were then evaluated for their potential ability not to indiscriminately kill human cells by testing their reactions with rabbit blood cells and mouse leukemia cells.

These tests revealed about 10 varieties"Gramicidin A" as promising antibacterial drugs of the future. The results also allowed the researchers to determine how specific structural changes in amino acids affect the overall function of the molecule. This basic information about structure and function is critical to understanding why and how pharmaceuticals work.

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