Novel antimicrobial peptides with antifungal and cytotoxic activity were derived from the alkalophilic fungus Emericellopsis alkalina VKPM F1428. We previously reported that this strain produced emericellipsin A (EmiA), which has strong antifungal and cytotoxic properties. Further analyses of the metabolites obtained under a special alkaline medium resulted in the isolation of four new homologous (Emi B–E). In this work, we report the complete primary structure and detailed biological activity for the newly synthesized nonribosomal antimicrobial peptides called emericellipsins B–E. The inhibitory activity of themajor compound, EmiA, against drug-resistant pathogenic fungi was similar to that of amphotericin B (AmpB). At the same time, EmiA had no hemolytic activity towards human erythrocytes. In addition, EmiA demonstrated low cytotoxic activity towards the normal HPF line, but possessed cancer selectivity to the K-562 and HCT-116 cell lines. Emericillipsins from the alkalophilic fungus Emericellopsis alkaline are promising treatment alternatives to licensed antifungal drugs for invasive mycosis therapy, especially for multidrug-resistant aspergillosis and cryptococcosis.

Today’s shortage of effective antimicrobial agents can be overcome by using antimicrobial peptides, which are produced naturally by a wide range of organisms, including microorganisms, plants, and mammals. Among these chemical groups, peptaibols are the well-known compounds with various biological activities, including antibacterial, antifungal, anticancer, antimycoplasmic, antitrypanosomal, and others. In this review, we summarize today’s knowledge on the sources, direct surface applications, and the mode of action of the peptaibols with anticancer and antifungal activity produced by filamentous fungi.

Features of the biochemical adaptations of alkaliphilic fungi to exist in extreme environments could promote the production of active antibiotic compounds with the potential to control microorganisms, causing infections associated with health care. Thirty-eight alkaliphilic and alkalitolerant Emericellopsis strains (E. alkalina, E. cf. maritima, E. cf. terricola, Emericellopsis sp.) isolated from different saline soda soils and belonging to marine, terrestrial, and soda soil ecological clades were investigated for emericellipsin A (EmiA) biosynthesis, an antifungal peptaibol previously described for Emericellopsis alkalina. The analysis of the Emericellopsis sp. strains belonging to marine and terrestrial clades from chloride soils revealed another novel form with a mass of 1032.7 Da, defined by MALDI-TOF Ms/Ms spectrometers, as the EmiA lacked a hydroxyl (dEmiA). EmiA displayed strong inhibitory effects on cell proliferation and viability of HCT 116 cells in a dose- and time-dependent manners and induced apoptosis.

The antibiotic activity in 42 strains of 8 species of the Trichoderma genus (T. asperellum, T. viride, T. hamatum,T. koningii, T. atroviride, T. harzianum, T. Citrinoviride, and T. longibrachiatum) isolated from different Siberian ecotops was studied. It was shown that these species differ in the degree of their antibacterial and antifungal activity. The chosen strain, T. citrinoviride TV4-1, exhibited high activity and a wide range of actions against the opportunistic and pathogenic fungi of the Aspergillus and Candida albicans genus; bacteria, including methicillin-resistant Staphylococcus aureus; and cancer cells. According to mass and IR spectrometry data and the spectrum of biological action, peptaibols are probably the most active compounds in the strain culture extracts.

The adaptations that alkaliphilic microorganisms have developed due to their extreme habitats promote the production of active natural compounds with the potential to control microorganisms, causing infections associated with healthcare. The primary purpose of this study was to isolate and identify a hydrophobin, Sa-HFB1, from an alkaliphilic fungus, Sodiomyces alkalinus. A potential antifungal effect against pathogenic and opportunistic fungi strains was determined. The MICs of Sa-HFB1 against opportunistic and clinical fungi ranged from 1 to 8 µg/mL and confirmed its higher activity against both non- and clinical isolates. The highest level of antifungal activity (MIC 1 µg/mL) was demonstrated for the clinical isolate Cryptococcus neoformans 297 m. The hydrophobin Sa-HFB1 may be partly responsible for the reported antifungal activity of S. alkalinus, and may serve as a potential source of lead compounds, meaning that it can be developed as an antifungal drug candidate.

The current information about hydrophobins, low molecular weight proteins synthesized by filamentous fungi, which are one of the strongest cellular biosurfactants, is summarized. The mechanism of biosynthesis of hydrophobins, the chemical structures and spectrum of its natural and synthetic isoforms, biological activity, and role in the regulation of vital processes of producers are presented. The potential for using hydrophobins in biotechnology has been demonstrated.