2025/05/30 by Eva Stodůlková, Dominik Lovás, Miroslav Flieger +19 · 1 voice
Biochemistry, Genetics and Molecular Biology · Medicine · #Microbial Natural Products and Biosynthesis #Phytochemical compounds biological activities #Research on Leishmaniasis Studies
paper · pdf · doi:10.1021/acsomega.5c01325
openalex publication_date 2025/05/30 · openalex created_date 2025/05/31 · openalex updated_date 2026/08/01
High Resolution Image Download MS PowerPoint Slide Six new pyranonaphthoquinone derivatives, gunacin A–E ( 2–7 ), along with the known compounds gunacin ( 1 ) and the isocoumarin derivative (+) orthosporin ( 8 ), were isolated from the fungus Exobasidium sp. Their chemical structures were elucidated by X-ray crystallography, extensive spectroscopic analysis supported by ROESY experiments, and mass spectrometry. Two tested compounds ( 1, 5 ) demonstrated high activity against Leishmania mexicana and four salivarian Trypanosoma species, with the lowest detected EC 50 value of 0.02–0.24 μM, a value that is comparable to those of currently used drugs. In addition, compounds 1, 3, 5, 6, and 7 demonstrated antibacterial properties at micromolar concentrations, while 1, 5, 6, and 7 exhibited moderate antifungal activity (MIC 33.3–66.7 μM). In cytotoxicity assays, the compounds exhibited a range of toxicity against mammalian Jurkat, RAT2, MDCK cell lines, HeLa cells, and fibroblasts, with inhibition levels varying from strong to minimal inhibition (EC 50 = 0.03–125 μM). This study is among the first to explore Exobasidium, a genus of phytopathogenic fungi and highlights the untapped potential of smut fungi (Basidiomycota: Ustilaginomycetes). The discovery of gunacins, which exhibit potent antiprotozoal activity at submicromolar concentrations, suggests a promising avenue for the development of antiprotozoal agents.