AsianScientist (Oct. 22, 2019) – An antibiotic derived from a fungus shows promise against multidrug-resistant bacteria, according to research by scientists in Japan. They published their findings in the journal Molecules.
In 2006, researchers discovered a compound called eushearilide in fungi which possessed antifungal and anti-yeast properties. A team of scientists at the Tokyo University of Science, Japan, had previously explored the unique chemical structure and the method of synthesis of eushearilide.
Now, this same research group, led by Professor Isamu Shiina, has built on their earlier findings to derive compounds from eushearilide that may have antimicrobial properties. The researchers first converted eushearilide into a compound colloquially called usharelide using a set of reactions that altered the chemical subgroups attached at the 23rd carbon atom of eushearilide.
Thereafter, usharelide was subjected to further chemical modification to obtain many structural variations of the compound, which were subsequently tested for their antibiotic properties, specifically against fungi and bacteria. The researchers found that two variants of usharelide showed antimicrobial properties against Candida albicans, a fungus responsible for yeast infections.
Meanwhile, most of the usharelide variants showed antimicrobial properties against Cryptococcus neoformans, which causes lung infections, meningitis and encephalitis, particularly in AIDS patients. This finding echoed the previous findings on the antifungal properties of eushearilide.
However, what caught the researchers’ attention was the fact that these usharelide variants also showed good antibacterial properties against several disease-causing bacterial species, including methicillin-resistant Staphylococcus aureus (MRSA), which is known to be a particularly difficult bacterium to tackle due to its resistance to several antibiotics.
“The antibiotic properties of eushearilide derivatives are not only against various fungi but also against bacteria, especially important drug-resistant bacteria such as MRSA. This is a novel finding that definitely warrants deeper research, given the urgent need for MRSA treatment options,” said Shiina.
The article can be found at: Tonoi et al. (2019) Total Synthesis and Antimicrobial Evaluation of 23-Demethyleushearilide and Extensive Antimicrobial Evaluation of All Synthetic Stereoisomers of (16Z,20E)-Eushearilide and (16E,20E)-Eushearilide.
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Source: Tokyo University of Science.
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