In today’s post-antibiotic era, the search for new antimicrobial compounds is of major importance and nature represents one of the primary sources of bioactive molecules. In this work, through a cheminformatics approach, we clustered an in-house library of natural products and their derivatives based on a combination of fingerprints and substructure search. We identified the preny-lated emodine-type anthranoid ferruginin A as a novel antimicrobial compound. We tested its ability to inhibit and kill a panel of Gram-positive and Gram-negative bacteria, and compared its activity with that of two analogues, vismione B and ferruanthrone. Furthermore, the capability of these three anthranoids to disrupt staphylococcal biofilm was investigated, as well as their effect on the viability of human keratinocytes. Ferruginin A showed a potent activity against both the planktonic and biofilm forms of Gram-positive bacteria (i.e., Staphylococcus aureus and S. epidermidis) and had the best therapeutic index compared to vismione B and ferruanthrone. In conclusion, ferruginin A represents a promising scaffold for the further development of valuable antimicrobial agents.

The triprenylated anthranoid Ferruginin A, a promising scaffold for the development of novel antibiotics against Gram-positive bacteria / Casciaro, B.; Ghirga, F.; Cappiello, F.; Vergine, V.; Loffredo, M. R.; Cammarone, S.; Puglisi, E.; Tortora, C.; Quaglio, D.; Mori, M.; Botta, B.; Mangoni, M. L.. - In: ANTIBIOTICS. - ISSN 2079-6382. - 11:1(2022), p. 84. [10.3390/antibiotics11010084]

The triprenylated anthranoid Ferruginin A, a promising scaffold for the development of novel antibiotics against Gram-positive bacteria

Casciaro B.
Primo
;
Ghirga F.;Cappiello F.;Vergine V.;Loffredo M. R.;Cammarone S.;Puglisi E.;Tortora C.;Quaglio D.
;
Botta B.;Mangoni M. L.
Ultimo
2022

Abstract

In today’s post-antibiotic era, the search for new antimicrobial compounds is of major importance and nature represents one of the primary sources of bioactive molecules. In this work, through a cheminformatics approach, we clustered an in-house library of natural products and their derivatives based on a combination of fingerprints and substructure search. We identified the preny-lated emodine-type anthranoid ferruginin A as a novel antimicrobial compound. We tested its ability to inhibit and kill a panel of Gram-positive and Gram-negative bacteria, and compared its activity with that of two analogues, vismione B and ferruanthrone. Furthermore, the capability of these three anthranoids to disrupt staphylococcal biofilm was investigated, as well as their effect on the viability of human keratinocytes. Ferruginin A showed a potent activity against both the planktonic and biofilm forms of Gram-positive bacteria (i.e., Staphylococcus aureus and S. epidermidis) and had the best therapeutic index compared to vismione B and ferruanthrone. In conclusion, ferruginin A represents a promising scaffold for the further development of valuable antimicrobial agents.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11573/1610047
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