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The present study investigates the utilization of nanoparticles based on poly-l-lactide (PLLA) and polyglycerol adipate (PGA), alone and blended, for the encapsulation of usnic acid (UA), a potent natural compound with various therapeutic properties including antimicrobial and anticancer activities. The development of these carriers offers an innovative approach to overcome the challenges associated with usnic acid's limited aqueous solubility, bioavailability, and hepatotoxicity. The nanosystems were characterized according to their physicochemical properties (among others, size, zeta potential, thermal properties), apparent aqueous solubility, and in vitro cytotoxicity. Interestingly, the nanocarrier obtained with the PLLA-PGA 50/50 weight ratio blend showed both the lowest size and the highest UA apparent solubility as well as the ability to decrease UA cytotoxicity towards human hepatocytes (HepG2 cells). This research opens new avenues for the effective utilization of these highly degradable and biocompatible PLLA-PGA blends as nanocarriers for reducing the cytotoxicity of usnic acid.
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http://dx.doi.org/10.3390/polym16030427 | DOI Listing |
Schiff bases have various pharmacological activities due to the azomethine (-C=N-) group. Usnic acid is the most famous lichen metabolite and it contains two carbonyl groups to synthesize the Schiff base derivatives with primary amines. Therefore, in the current study, the known Schiff base derivatives (2-5) of usnic acid (1) were synthesized to explore their antidiabetic, neuroprotective, antioxidant, antidepressant and anti-Parkinson's properties.
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July 2025
Department of Food Engineering, Faculty of Chemical and Metallurgical Engineering, Yildiz Technical University, 34220 Istanbul, Türkiye.
This study employed response surface methodology for the first-time optimization of the ultrasound-assisted extraction (UAE) of the total phenolic content (TPC) and ABTS from edible lichens, including , , , , and . Fourteen experimental points were generated using Design Expert Software, with the extraction temperature (25-40 °C), extraction time (5-20 min), and ethanol concentration (0-80%) as independent variables, and TPC and ABTS as dependent variables. The phenolic profile and mineral and antibacterial properties of the optimized lichen extracts were determined.
View Article and Find Full Text PDFMolecules
July 2025
Department of Pharmacognosy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Chirality plays a key role in the effectiveness and toxicity of bioactive compounds. Usnic acid (UA), a lichen metabolite, exists as two enantiomers. Despite numerous studies on its biological properties, enantioselective aspects remain poorly recognized.
View Article and Find Full Text PDFRSC Med Chem
July 2025
Department of Drug Sciences, University of Pavia viale Taramelli 12 27100 Pavia Italy
The prevalence of human fungal infections (FIs) is rapidly increasing worldwide, posing substantial challenges to public health. The underestimation of FIs risk led to a limited knowledge of the fungal pathogenicity and a concomitant paucity of antimycotic drugs that are increasingly unable to effectively address resistance liabilities. The identification of innovative antifungal drugs is therefore an urgent need.
View Article and Find Full Text PDFJ Pharm Biomed Anal
November 2025
Novosibirsk State University, Pirogov St., 2, Novosibirsk 630090, Russia; Institute of Chemical Biology and Fundamental Medicine of SB RAS, Lavrent'ev ave., 8, Novosibirsk 630090, Russia.
In the present study, we developed and validated three liquid chromatography-tandem mass spectrometry (LC-MS/MS) methods for quantification of the agent OL9-116, a Tdp1 inhibitor based on usnic acid, in murine lungs, liver and kidney, respectively. Additionally, a semi-quantitative method was developed for quantification of the agent in the primary tumor node of Lewis lung carcinoma. Tissue samples were prepared using ultrasonic homogenization and QuEChERS methodology.
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