Abstract
Many pathogens involved in human infection have rapidly increased their antibiotic resistance, reducing the effectiveness of therapies in recent decades. Most of them can form biofilms and effective drugs are not available to treat these formations. Natural products could represent an efficient solution in discovering and developing new drugs to overcome antimicrobial resistance and treat biofilm-related infections. In this study, 20 secondary metabolites produced by pathogenic fungi of forest plants and belonging to diverse classes of naturally occurring compounds were evaluated for the first time against clinical isolates of antibiotic-resistant Gram-negative and Gram-positive bacteria. epi-Epoformin, sphaeropsidone, and sphaeropsidin A showed antimicrobial activity on all test strains. In particular, sphaeropsidin A was effective at low concentrations with Minimum Inhibitory Concentration (MIC) values ranging from 6.25 μg/mL to 12.5 μg/mL against all reference and clinical test strains. Furthermore, sphaeropsidin A at sub-inhibitory concentrations decreased methicillin-resistant S. aureus (MRSA) and P. aeruginosa biofilm formation, as quantified by crystal violet staining. Interestingly, mixtures of sphaeropsidin A and epi-epoformin have shown antimicrobial synergistic effects with a concomitant reduction of cytotoxicity against human immortalized keratinocytes. Our data show that sphaeropsidin A and epi-epoformin possess promising antimicrobial properties.
Highlights
IntroductionThe use of antibiotics has played a fundamental role in extending the average human life
In the last century, the use of antibiotics has played a fundamental role in extending the average human life
The were isolated isolated as as phytotoxins phytotoxins produced by different fungal genera responsible for forest plant diseases such as Diplodia, Seiridium, produced by different fungal genera responsible for forest plant diseases such as Diplodia, Seiridium, Biscogniauxia, Sardiniella
Summary
The use of antibiotics has played a fundamental role in extending the average human life. They allow us to treat trivial or serious infections and to carry out complex medical and Toxins 2020, 12, 444; doi:10.3390/toxins12070444 www.mdpi.com/journal/toxins. Toxins 2020, 12, 444 surgical procedures that would otherwise result in very high mortality. The excessive or inappropriate use of antibiotics, in human medicine and zootechnics and agriculture, results in bacterial strains possessing increased antibiotic resistance and isolation frequency. The ability to transfer resistance determinants horizontally makes the bacterium frequently acquire resistance to multiple classes of drugs and infection treatment becomes complicated.
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