13 May 2019

Against infections and cancer

Russian scientists have identified a new antibiotic

Department of Strategic Communications of TSU

Employees of the Institute of X-BIO of TSU Alexey and Anastasia Vasilchenko, together with colleagues from the Institute of Bioorganic Chemistry of the Russian Academy of Sciences and the Research Institute for the Research of New Antibiotics named after G. Gause, isolated emericellipsin A – a compound with antibacterial, antifungal and antitumor effects.

An article about this was published in the journal Molecules (Rogzhin et al., A Novel Lipopeptaibol Emericellipsin A with Antimicrobial and Antitumor Activity Produced by the Extremophilic Fungus Emericellopsis alkaline).

According to WHO, the problem of antibiotic resistance is one of the main problems in the field of healthcare. Statistics also indicate this: the number of deaths from bacterial infections, according to a study published in The Lancet Infectious Diseases, has been growing since 2007. According to scientists, mycelial fungi growing in extreme habitats are promising candidates for the role of suppliers of new-generation antibiotics. In the process of adapting to extreme conditions, they synthesize a number of substances, among which there are peptaibols – antibiotics of a peptide nature. The latter, due to their chemical structure, suppress pathogenic strains of microorganisms resistant to other antibiotics.

Of particular interest are representatives of the genus Emericellopsis, which produce a wide range of peptide antibiotics. And, importantly, some of them are already used in clinical practice. In the current work, the researchers drew attention to Emericellopsis alkaline, which synthesizes a new peptaibol, named by the authors of the article emericellipsin A. Scientists managed to decipher the chemical structure of the new antibiotic, as well as to find out the features of its biological properties. It is reported that emericellipsin A is a small polypeptide with a molecular weight of 1 kDa, consisting of seven amino acids. It is worth noting that only two of them, alanine and isoleucine, are ribosomally encoded: the remaining seven are non-standard, that is, structural information about them is not embedded in the DNA of the organism. Fatty acids can also be found in the structure of the substance, which also determines its unique physico-chemical properties.

As for biological properties, emericellipsin A proved to be effective against gram-positive and, to a lesser extent, gram-negative bacteria. Similar results were shown by vancomycin, which today is commonly called the "antibiotic of last hope".  The mechanism of action of emericellipsin A, as reported by scientists, is associated with damage to the cell wall, which leads to death. However, emericellipsin A has shown antimicrobial properties not only against bacteria, but also pathogens of fungal infections. The antibiotic suppresses the growth of fungi of the genus Candida and Aspergillus, pathogens of candidiasis (causes thrush) and aspergillosis, respectively.  In addition, emericellipsin A, like other representatives of the peptaibol class, exhibits toxicity against tumor cells. The corresponding results were obtained on Hep G2 and HeLa cell lines. As the authors note, it is 40 times less toxic to healthy cells than doxorubicin, an antibiotic widely used in chemotherapy.

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