Methicillin-resistant (MRSA), a WHO high-priority pathogen that can cause great harm to living beings, is a primary cause of death from antibiotic-resistant infections. In the present study, six new compounds, including fumindoline A-C (-), 12, 13-hydroxy-asperfumigatin (), 2--tryptoquivaline F () and penibenzophenone E (), and thirty-nine known ones were isolated from the marine-derived fungus H22. The structures and the absolute configurations of the new compounds were unambiguously assigned by spectroscopic data, mass spectrometry (MS), electronic circular dichroism (ECD) spectroscopic analyses, quantum NMR and ECD calculations, and chemical derivatizations. Bioactivity screening indicated that nearly half of the compounds exhibit antibacterial activity, especially compounds and , and - showed excellent antimicrobial activities against MRSA, with minimum inhibitory concentration (MIC) values ranging from 1.25 to 2.5 μM. In addition, compound showed moderate inhibitory activity against (MIC: 25 μM), compound showed moderate inhibitory activity against (MIC: 50 μM), and compound showed strong inhibitory activity against the hatching of a egg (IC: 2.5 μM).
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http://dx.doi.org/10.3390/md20050302 | DOI Listing |
FEBS J
January 2025
Institute of Bioorganic Chemistry, Polish Academy of Sciences, Poznan, Poland.
Rhizobium etli is a nitrogen-fixing bacterium that encodes two l-asparaginases. The structure of the inducible R. etli asparaginase ReAV has been recently determined to reveal a protein with no similarity to known enzymes with l-asparaginase activity, but showing a curious resemblance to glutaminases and β-lactamases.
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January 2025
Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.
In this study, new cinnamic acid linked to triazole acetamide derivatives was synthesized and evaluated for anti-Alzheimer and anti-melanogenesis activities. The structural elucidation of all analogs was performed using different analytical techniques, including H-NMR, C-NMR, mass spectrometry, and IR spectroscopy. The synthesized compounds were assessed in vitro for their inhibitory activities against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase enzymes.
View Article and Find Full Text PDFMycoses
January 2025
Department of Dermatology and Venereology, Peking University First Hospital, Beijing, China.
Background: Microsporum canis, a dermatophyte commonly associated with pets, is a leading cause of severe tinea capitis. The increasing prevalence of antifungal resistance among dermatophytes poses a significant global health challenge.
Objectives: This study aims to define the updated antifungal susceptibility profile of M.
Acta Pharmacol Sin
January 2025
State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin, 300350, China.
Histone lysine-specific demethylase 1 (LSD1) is overexpressed in various solid and hematological tumors, suggesting its potential as a therapeutic target, but there are currently no LSD1 inhibitors available on the market. In this study we employed a computer-guided approach to identify novel LSD1/EGFR dual inhibitors as a potential therapeutic agent for non-small cell lung cancer. Through a multi-stage virtual screening approach, we found L-1 and L-6, two compounds with unique scaffolds that effectively inhibit LSD1 with IC values of 6.
View Article and Find Full Text PDFActa Pharmacol Sin
January 2025
Laboratory for Neurophysiology, Department of Cell and Chemical Biology, Leiden University, Medical Centre, Leiden, 2333, ZC, The Netherlands.
Daylength (i.e., photoperiod) provides essential information for seasonal adaptations of organisms.
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