New, more powerful antibiotic discovered that could fight drug resistance

Chemists in Australia and the UK have discovered a new class of antibiotics that can kill drug-resistant bacterial pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterobacteriaceae (VRE). The research was published in a recent issue of the Journal of the American Chemical Society.

According to Australia's Monash University, the new antibiotic, called pre-methylenomycin C lactone, was found as a chemical intermediate in the natural process that produces the long-known antibiotic methylenomycin A.

Study co-author Professor Greg Challis of Monash University and Warwick University in the UK said methylenomycin A was discovered 50 years ago and although it has been synthesized many times, it seems that no scientists have tested the antibacterial activity of the intermediates in this synthesis. According to Professor Challis, by deleting the biosynthetic genes, chemists discovered two previously unknown synthetic intermediates. Both of these substances are much more powerful antibiotics than methylenomycin A.

When tested for antibacterial activity, one of the intermediates, called pre-methylenomycin C lactone, was shown to be 100 times more active than the antibiotic methylenomycin A against a variety of Gram-positive bacteria. Specifically, pre-methylenomycin C lactone was effective against S. aureus and E. faecium, the bacteria that cause MRSA and VRE. This finding is considered to have great potential in treating VRE, a pathogen that the World Health Organization (WHO) has placed particular emphasis on.

With its simple structure, potent activity, resistance-resistant properties, and scalable synthesis, pre-methylenomycin C lactone is a promising new candidate for saving the lives of approximately 1.1 million people worldwide who fall victim to drug resistance each year, according to the researchers.

Professor Challis said the discovery could lead to a new paradigm for antibiotic discovery. By identifying and testing intermediates in the production of diverse natural compounds, researchers could find new antibiotics that are more potent and more resistant to resistance.

Earlier this month, the WHO released a report showing that very few antibacterial drugs are currently being researched. The reason, it said, is that easy-to-discover antibiotics have already been found, and that limited funding and commercial incentives are hindering investment in antibiotic research.

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