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Search Results (4,044)

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Keywords = biologically active agent

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18 pages, 2714 KiB  
Article
Assessing the Efficacy of Chemical and Green-Synthesized CuO Nanoparticles in Combatting Clinical Candida Species: A Comparative Study
by Hiba Younis Khalaf, Ferid Ben Nasr, Bashar Sadeq Noomi, Sami Mnif and Sami Aifa
Microbiol. Res. 2025, 16(8), 178; https://doi.org/10.3390/microbiolres16080178 (registering DOI) - 1 Aug 2025
Abstract
The most prevalent growth of Candida cells is based on biofilm development, which causes the intensification of antifungal resistance against a large range of chemicals. Nanoparticles can be synthesized using green methods via various biological extracts and reducing agents to control Candida biofilms. [...] Read more.
The most prevalent growth of Candida cells is based on biofilm development, which causes the intensification of antifungal resistance against a large range of chemicals. Nanoparticles can be synthesized using green methods via various biological extracts and reducing agents to control Candida biofilms. This study aims to compare copper oxide nanoparticles (CuONPs) synthesized through chemical methods and those synthesized using Cinnamomum verum-based green methods against Candida infections and their biofilms isolated from Iraqi patients, with the potential to improve treatment outcomes. The physical and chemical properties of these nanoparticles were characterized using Fourier-transform infrared spectroscopy (FT-IR,) scanning electron microscopy (SEM), transmission electron microscopy (TEM), atomic force microscopy (AFM) and X-ray diffraction (XRD). Four strains of Candida were isolated and characterized from Iraqi patients in Tikrit Hospital and selected based on their ability to form biofilm on polystyrene microplates. The activity of green-synthesized CuONPs using cinnamon extract was compared with both undoped and doped (Fe, Sn) chemically synthesized CuONPs. Four pathogenic Candida strains (Candida glabrata, Candida lusitaniae, Candida albicans, and Candida tropicalis) were isolated from Iraqi patients, demonstrating high biofilm formation capabilities. Chemically and green-synthesized CuONPs from Cinnamomum verum showed comparable significant antiplanktonic and antibiofilm activities against all strains. Doped CuONPs with iron or tin demonstrated lower minimum inhibitory concentration (MIC) values, indicating stronger antibacterial activity, but exhibited weaker anti-adhesive properties compared to other nanoparticles. The antiadhesive activity revealed that C. albicans strain seems to produce the most resistant biofilms while C. glabrata strain seems to be more resistant towards the doped CuONPs. Moreover, C. tropicalis was the most sensitive to all the CuONPs. Remarkably, at a concentration of 100 µg/mL, all CuONPs were effective in eradicating preformed biofilms by 47–66%. The findings suggest that CuONPs could be effective in controlling biofilm formation by Candida species resistant to treatment in healthcare settings. Full article
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38 pages, 4443 KiB  
Review
The Role of Plant Growth-Promoting Bacteria in Soil Restoration: A Strategy to Promote Agricultural Sustainability
by Mario Maciel-Rodríguez, Francisco David Moreno-Valencia and Miguel Plascencia-Espinosa
Microorganisms 2025, 13(8), 1799; https://doi.org/10.3390/microorganisms13081799 - 1 Aug 2025
Abstract
Soil degradation resulting from intensive agricultural practices, the excessive use of agrochemicals, and climate-induced stresses has significantly impaired soil fertility, disrupted microbial diversity, and reduced crop productivity. Plant growth-promoting bacteria (PGPB) represent a sustainable biological approach to restoring degraded soils by modulating plant [...] Read more.
Soil degradation resulting from intensive agricultural practices, the excessive use of agrochemicals, and climate-induced stresses has significantly impaired soil fertility, disrupted microbial diversity, and reduced crop productivity. Plant growth-promoting bacteria (PGPB) represent a sustainable biological approach to restoring degraded soils by modulating plant physiology and soil function through diverse molecular mechanisms. PGPB synthesizes indole-3-acetic acid (IAA) to stimulate root development and nutrient uptake and produce ACC deaminase, which lowers ethylene accumulation under stress, mitigating growth inhibition. They also enhance nutrient availability by releasing phosphate-solubilizing enzymes and siderophores that improve iron acquisition. In parallel, PGPB activates jasmonate and salicylate pathways, priming a systemic resistance to biotic and abiotic stress. Through quorum sensing, biofilm formation, and biosynthetic gene clusters encoding antibiotics, lipopeptides, and VOCs, PGPB strengthen rhizosphere colonization and suppress pathogens. These interactions contribute to microbial community recovery, an improved soil structure, and enhanced nutrient cycling. This review synthesizes current evidence on the molecular and physiological mechanisms by which PGPB enhance soil restoration in degraded agroecosystems, highlighting their role beyond biofertilization as key agents in ecological rehabilitation. It examines advances in nutrient mobilization, stress mitigation, and signaling pathways, based on the literature retrieved from major scientific databases, focusing on studies published in the last decade. Full article
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19 pages, 4753 KiB  
Article
Biosynthesized Gold Nanoparticles from Eruca sativa Mill. Leaf Extract Exhibit In Vivo Biocompatibility, Antimicrobial, and Antioxidant Activities
by Abdullah Muhsin Hazbar, Abdulkadir Mohammed Noori Jassim, Mustafa Taha Mohammed and Younis Baqi
Antibiotics 2025, 14(8), 776; https://doi.org/10.3390/antibiotics14080776 (registering DOI) - 31 Jul 2025
Abstract
Background/Objectives: Antimicrobial resistance (AMR) is a health related threat world-wide. Biosynthesized gold nanoparticles (AuNPs) using plant extracts have been reported to exhibit certain biological activity. This study aimed to biosynthesize AuNPs using an aqueous extract of Eruca sativa leaves and to evaluate their [...] Read more.
Background/Objectives: Antimicrobial resistance (AMR) is a health related threat world-wide. Biosynthesized gold nanoparticles (AuNPs) using plant extracts have been reported to exhibit certain biological activity. This study aimed to biosynthesize AuNPs using an aqueous extract of Eruca sativa leaves and to evaluate their biocompatibility, antimicrobial activity, and antioxidant properties. Methods: AuNPs were biosynthesized using an aqueous extract of Eruca sativa leaves. Their biocompatibility was evaluated through hemolytic activity and assessments of hepatic and renal functions in rats. AuNPs were biologically evaluated as antimicrobial and antioxidant agents. Results: The AuNPs exhibited particle sizes of 27.78 nm (XRD) and 69.41 nm (AFM). Hemolysis assays on red blood cells revealed negligible hemolytic activity (<1%). Hepatic enzyme levels, including alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and lactate dehydrogenase (LDH) were studied. ALT, AST, and ALP levels showed no significant changes compared to the negative control. However, LDH levels were elevated at higher concentration (52.8 µg/mL), while the lower concentration (26.4 µg/mL) appeared to be safer. Renal biomarkers, urea and creatinine, showed no significant changes at either concentration, indicating minimal nephrotoxicity. The antimicrobial activity of AuNPs, plant extract, and gold salt was tested against five microorganisms: two Gram-positive bacteria (Staphylococcus aureus, Streptococcus pneumoniae), two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and a fungal strain (Candida albicans). The AuNPs exhibited minimum inhibition concentrations (MICs) of 13.2 µg/mL against S. aureus and S. pneumoniae, 26.4 µg/mL against E. coli and C. albicans, and 39.6 µg/mL against P. aeruginosa, suggesting selectivity towards Gram-positive bacteria. Furthermore, the AuNPs demonstrated strong antioxidant activity, surpassing that of vitamin C. Conclusions: The biosynthesized AuNPs exhibited promising biocompatibility, selective antimicrobial properties, and potent antioxidant activity, supporting their potential application in combating the AMR. Full article
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24 pages, 7353 KiB  
Article
Characterization and Application of Synergistically Degraded Chitosan in Aquafeeds to Promote Immunity, Antioxidative Status, and Disease Resistance in Nile Tilapia (Oreochromis niloticus)
by Thitirat Rattanawongwiboon, Natthapong Paankhao, Wararut Buncharoen, Nantipa Pansawat, Benchawan Kumwan, Pakapon Meachasompop, Phunsin Kantha, Tanavan Pansiri, Theeranan Tangthong, Sakchai Laksee, Suwinai Paankhao, Kittipong Promsee, Mongkhon Jaroenkittaweewong, Pattra Lertsarawut, Prapansak Srisapoome, Kasinee Hemvichian and Anurak Uchuwittayakul
Polymers 2025, 17(15), 2101; https://doi.org/10.3390/polym17152101 - 31 Jul 2025
Abstract
This study investigated the immunonutritional potential of high-molecular-weight (Mw~85 kDa), non-degraded chitosan (NCS) and gamma-radiation-degraded, low-molecular-weight chitosan (RCS) incorporated into aquafeeds for Nile tilapia (Oreochromis niloticus). RCS was produced by γ-irradiation (10 kGy) in the presence of 0.25% (w/ [...] Read more.
This study investigated the immunonutritional potential of high-molecular-weight (Mw~85 kDa), non-degraded chitosan (NCS) and gamma-radiation-degraded, low-molecular-weight chitosan (RCS) incorporated into aquafeeds for Nile tilapia (Oreochromis niloticus). RCS was produced by γ-irradiation (10 kGy) in the presence of 0.25% (w/v) H2O2, yielding low-viscosity, colloidally stable nanoparticles with Mw ranging from 10 to 13 kDa. Five diets were formulated: a control, NCS at 0.50%, and RCS at 0.025%, 0.050%, and 0.075%. No adverse effects on growth were observed, confirming safety. Immune gene expression (e.g., ifng1, nfκb, tnf), antioxidant markers (e.g., reduced MDA, increased GSH and GR), and nonspecific humoral responses (lysozyme, IgM, and bactericidal activity) were significantly enhanced in the NCS-0.50, RCS-0.050, and RCS-0.075 groups. Notably, these benefits were achieved with RCS at 10-fold lower concentrations than NCS. Following challenge with Edwardsiella tarda, fish fed RCS-0.050 and RCS-0.075 diets exhibited the highest survival rates and relative percent survival, highlighting robust activation of innate and adaptive immunity alongside redox defense. These results support the use of low-Mw RCS as a biologically potent, cost-effective alternative to traditional high-Mw chitosan in functional aquafeeds. RCS-0.050 and RCS-0.075 show strong potential as immunonutritional agents to enhance fish health and disease resistance in aquaculture. Full article
(This article belongs to the Special Issue Polysaccharides: Synthesis, Properties and Applications)
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28 pages, 9865 KiB  
Article
Enhanced Stability of Multi-Functionalized Gold Nanoparticles and Potential Anticancer Efficacy on Human Cervical Cancer Cells
by Aurora Mocanu, Madalina Anca Ujica, Ossi Horovitz, Gheorghe Tomoaia, Olga Soritau, Cristina Teodora Dobrota, Cristina Roxana Popa, Attila Kun, Horea-Rares-Ciprian Benea, Ionel Marius Mang, Gheorghe Borodi, Viorica Raischi, Marius Roman, Lucian Cristian Pop and Maria Tomoaia-Cotisel
Biomedicines 2025, 13(8), 1861; https://doi.org/10.3390/biomedicines13081861 - 31 Jul 2025
Abstract
Objectives: In this research study, we introduce a novel approach to develop an innovative nanocarrier system comprising gold nanoparticles (GNPs) loaded with doxorubicin (D) in combination with natural molecules, such as trans-resveratrol (R), piperine (P), and icariin (Ic), against human cervical cancer. The [...] Read more.
Objectives: In this research study, we introduce a novel approach to develop an innovative nanocarrier system comprising gold nanoparticles (GNPs) loaded with doxorubicin (D) in combination with natural molecules, such as trans-resveratrol (R), piperine (P), and icariin (Ic), against human cervical cancer. The final objective is to improve the anticancer efficacy of doxorubicin on HeLa and CaSki cell lines. Methods: Resveratrol was also used for the synthesis of GNP_R1 nanoparticles. Multi-functional GNPs loaded with D, R, P, and Ic (e.g., GNP_R1@D/R/P/Ic) were successfully prepared and fully characterized by SPR, TEM, HR-TEM, XRD, AFM, DLS, and zeta potential. They were investigated for in vitro stability in various biological media. The cytotoxicity activity was tested on HeLa and CaSki cell lines, using the MTT assay, for their applications as anticancer agents. Results: Our results demonstrate that the novel multi-functional GNPs (such as GNP_R1@D/R and GNP_R1@D/R/P/Ic) can effectively target the cervical cancer cells, improving the bioavailability of therapeutic agents and enhancing their cytotoxicity against cervical cancer cells. In vitro assessments demonstrated that the multi-functional GNPs exhibited improved stability and potential anticancer efficacy on human cervical cancer cells. Conclusions: The described strategy connects the benefits of biomolecules with functional nanoparticles toward the development of various GNP_R1@D/R/P/Ic nanocarriers for their applications as anticancer agents against human cervical cancer. This study provides compelling evidence that the innovative nanoparticles can enhance the therapeutic efficacy of doxorubicin against cervical cancer and offer a more advantageous alternative compared to doxorubicin monotherapy. Full article
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60 pages, 6122 KiB  
Review
Isorhamnetin: Reviewing Recent Developments in Anticancer Mechanisms and Nanoformulation-Driven Delivery
by Juie Nahushkumar Rana, Kainat Gul and Sohail Mumtaz
Int. J. Mol. Sci. 2025, 26(15), 7381; https://doi.org/10.3390/ijms26157381 - 30 Jul 2025
Abstract
Natural compounds, particularly flavonoids, have emerged as promising anticancer agents due to their various biological activities and no or negligible toxicity towards healthy tissues. Among these, isorhamnetin, a methylated flavonoid, has gained significant attention for its potential to target multiple cancer hallmarks. This [...] Read more.
Natural compounds, particularly flavonoids, have emerged as promising anticancer agents due to their various biological activities and no or negligible toxicity towards healthy tissues. Among these, isorhamnetin, a methylated flavonoid, has gained significant attention for its potential to target multiple cancer hallmarks. This review comprehensively explores the mechanisms by which isorhamnetin exerts its anticancer effects, including cell cycle regulation, apoptosis, suppression of metastasis and angiogenesis, and modulation of oxidative stress and inflammation. Notably, isorhamnetin arrests cancer cell proliferation by regulating cyclins, and CDKs induce apoptosis via caspase activation and mitochondrial dysfunction. It inhibits metastatic progression by downregulating MMPs, VEGF, and epithelial–mesenchymal transition (EMT) markers. Furthermore, its antioxidant and anti-inflammatory properties mitigate reactive oxygen species (ROS) and pro-inflammatory cytokines, restricting cancer progression and modulating tumor microenvironments. Combining isorhamnetin with other treatments was also discussed to overcome multidrug resistance. Importantly, this review integrates the recent literature (2022–2024) and highlights isorhamnetin’s roles in modulating cancer-specific signaling pathways, immune evasion, tumor microenvironment dynamics, and combination therapies. We also discuss nanoformulation-based strategies that significantly enhance isorhamnetin’s delivery and bioavailability. This positions isorhamnetin as a promising adjunct in modern oncology, capable of improving therapeutic outcomes when used alone or in synergy with conventional treatments. The future perspectives and potential research directions were also summarized. By consolidating current knowledge and identifying critical research gaps, this review positions Isorhamnetin as a potent and versatile candidate in modern oncology, offering a pathway toward safer and more effective cancer treatment strategies. Full article
(This article belongs to the Special Issue The Role of Natural Compounds in Cancer and Inflammation, 2nd Edition)
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27 pages, 3430 KiB  
Article
Systematic Characterization of Antioxidant Shielding Capacity Against Oxidative Stress of Aerial Part Extracts of Anacardium occidentale
by Alejandro Ponce-Mora, Lucia Gimeno-Mallench, José Luis Lavandera, Ryland T. Giebelhaus, Alicia Domenech-Bendaña, Antonella Locascio, Irene Gutierrez-Rojas, Salvatore Sauro, Paulina de la Mata, Seo Lin Nam, Vanessa Méril-Mamert, Muriel Sylvestre, James J. Harynuk, Gerardo Cebrián-Torrejón and Eloy Bejarano
Antioxidants 2025, 14(8), 935; https://doi.org/10.3390/antiox14080935 - 30 Jul 2025
Viewed by 18
Abstract
Oxidative stress is a biological imbalance that contributes to cellular damage and is a major driver of aging and age-related disorders, prompting the search for natural antioxidant agents. Our study is a phytochemical, electrochemical, and biological characterization of the antioxidant potential of aqueous [...] Read more.
Oxidative stress is a biological imbalance that contributes to cellular damage and is a major driver of aging and age-related disorders, prompting the search for natural antioxidant agents. Our study is a phytochemical, electrochemical, and biological characterization of the antioxidant potential of aqueous extracts from aerial parts of A. occidentale—leaves, bark, fruit, and cashew nuts—traditionally used in folklore medicine. Extracts were analyzed using FT-IR spectroscopy, GC × GC-TOFMS, polyphenol quantification, and antioxidant capacity assays (ABTS, FRAP, DPPH). Biological activity was tested in different mice and human cell lines (SH-SY5Y, MEF, ARPE-19, and HLECs). Aqueous extracts from the leaves and bark of A. occidentale exhibited significantly higher antioxidant activity compared to those from the fruit and cashew nut. These extracts showed elevated polyphenol content and strong performance in antioxidant capacity assays. In vitro, leaf and bark extracts enhanced cell viability under H2O2-induced oxidative stress, preserved mitochondrial membrane potential, and upregulated cytoprotective genes (HMOX1, NQO1, GCLC, and GCLM) in multiple cell lines. In contrast, fruit and nut extracts showed minimal antioxidant activity and no significant gene modulation. Our findings underscore the therapeutic potential of A. occidentale leaf and bark extracts as effective natural antioxidants and support their further development as candidates for phytotherapeutic interventions. Full article
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20 pages, 4361 KiB  
Article
Pinene-Based Chiral Bipyridine Ligands Drive Potent Antibacterial Activity in Rhenium(I) Complexes
by Justine Horner, Gozde Demirci, Aurelien Crochet, Aleksandar Pavic, Olimpia Mamula Steiner and Fabio Zobi
Molecules 2025, 30(15), 3183; https://doi.org/10.3390/molecules30153183 (registering DOI) - 29 Jul 2025
Viewed by 122
Abstract
Antimicrobial resistance (AMR) poses a critical global health threat by rendering existing antibiotics ineffective against infections, leading to increased mortality, prolonged illnesses, and higher healthcare costs. Developing new antibiotics is essential to combat resistant pathogens, safeguard modern medical procedures, and prevent a return [...] Read more.
Antimicrobial resistance (AMR) poses a critical global health threat by rendering existing antibiotics ineffective against infections, leading to increased mortality, prolonged illnesses, and higher healthcare costs. Developing new antibiotics is essential to combat resistant pathogens, safeguard modern medical procedures, and prevent a return to a pre-antibiotic era where common infections become untreatable. We report a series of chiral tricarbonyl rhenium(I) complexes incorporating enantiopure pinene-substituted bipyridine ligands (L#) of the general formula fac-[Re(CO)3L#X] and fac-[Re(CO)3L#Py]+ (where X = Cl or Br and Py = pyridine). These complexes were isolated as mixtures of two diastereomers, characterized by standard techniques, and evaluated for cytotoxic activity against methicillin-resistant and methicillin-sensitive Staphylococcus aureus (MRSA and MSSA). The results revealed notable antibacterial efficacy (MIC = 1.6 μM), reflected in high therapeutic indices (Ti > 10). In contrast, analogous complexes bearing non-chiral 2,2′-bipyridine ligands exhibited no activity, underscoring the critical role of chirality in modulating biological interactions at the molecular level. These findings highlight the potential of chiral Re(I) complexes as promising scaffolds for the development of more potent and selective antibacterial agents. Full article
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25 pages, 14674 KiB  
Article
Eco-Friendly Silver Nanoparticles Synthesis Method Using Medicinal Plant Fungal Endophytes—Biological Activities and Molecular Docking Analyses
by Harish Chandra, Sagar Vishwakarma, Nilesh Makwana, Arun S. Kharat, Vijeta Chaudhry, Sumit Chand, Rajendra Prasad, Soban Prakash, Annapurna Katara, Archana Yadav, Manisha Nigam and Abhay Prakash Mishra
Biology 2025, 14(8), 950; https://doi.org/10.3390/biology14080950 - 28 Jul 2025
Viewed by 342
Abstract
The integration of nanotechnology and green synthesis strategies provides innovative solutions in biomedicine. This study focuses on the biofabrication of silver nanoparticles (AgNPs) using Corynespora smithii, an endophytic fungus isolated from Bergenia ciliata. The eco-friendly synthesis process employed fungal extracts as [...] Read more.
The integration of nanotechnology and green synthesis strategies provides innovative solutions in biomedicine. This study focuses on the biofabrication of silver nanoparticles (AgNPs) using Corynespora smithii, an endophytic fungus isolated from Bergenia ciliata. The eco-friendly synthesis process employed fungal extracts as reducing and stabilizing agents thereby minimizing the need for hazardous chemicals. The AgNPs demonstrated strong potent biological activities, showcasing significant antioxidant, antibacterial, and anticancer properties. The antibacterial efficacy was demonstrated against various Gram-positive and Gram-negative bacteria, while cytotoxicity on the A549 lung cancer cell line revealed an IC50 value of 10.46 µg/mL. A molecular docking analysis revealed interactions between the major bioactive compound, dimethylsulfoxonium formylmethylide, and the pathogenic proteins, Staphylococcus aureus and Salmonella typhi, displaying moderate binding affinities. Furthermore, the ADME analysis of dimethylsulfoxonium formylmethylide indicated favourable pharmacokinetic properties, including high gastrointestinal absorption, minimal lipophilicity, and low potential for drug–drug interactions, making it a promising candidate for oral drug formulations. These findings further support the compound’s suitability for biomedical applications. This research emphasizes the potential of C. smithii as a sustainable source for synthesizing bioactive nanoparticles, paving the way for their application in developing novel therapeutic agents. This study highlights the significance of harnessing endophytic fungi from medicinal plants for sustainable nanotechnology advancements. Full article
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19 pages, 3605 KiB  
Article
Luminescent Properties and Cytotoxic Activity of 2-phenylbenzoxazole Fluorosulfate Derivatives
by Nadezhda V. Danilenko, Mariia O. Lutsuk, Alexey A. Ryadun, Dmitry I. Pavlov, Evgenii V. Plotnikov, Daria D. Eskova, Yulia D. Klimenko, Andrei S. Potapov and Andrei I. Khlebnikov
Int. J. Mol. Sci. 2025, 26(15), 7261; https://doi.org/10.3390/ijms26157261 - 27 Jul 2025
Viewed by 191
Abstract
The synthesis of 2-phenylbenzoxazole fluorosulfate derivatives was carried out using the SuFEx reaction. To study the anticancer properties of the obtained compounds, the cell lines PC-3 (obtained from prostate adenocarcinoma), BT-474, and MCF-7 (both obtained from breast carcinoma) were used. The cytotoxicity on [...] Read more.
The synthesis of 2-phenylbenzoxazole fluorosulfate derivatives was carried out using the SuFEx reaction. To study the anticancer properties of the obtained compounds, the cell lines PC-3 (obtained from prostate adenocarcinoma), BT-474, and MCF-7 (both obtained from breast carcinoma) were used. The cytotoxicity on murine 3T3L1 embryonic was also investigated. Among the tested compounds, the ortho-substituted fluorosulfate derivative (BOSo) exhibited significant cytotoxicity against MCF-7 cells. The biological findings are consistent with molecular docking results, which revealed a structural similarity between BOSo and known inhibitors of hER and HER2 receptors—tamoxifen and SYR127063. Therefore, BOSo shows promise as a potential therapeutic agent with antiproliferative properties. The photoluminescent characteristics of the fluorosulfate derivatives were examined in the solid state, in acetonitrile solution and in PBS, with the highest quantum yields reaching up to 64% for the para-fluorosulfate derivative in acetonitrile. Overall, these compounds demonstrate considerable potential for the development of new multifunctional molecular tools that combine biological activity with fluorescent properties. Full article
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19 pages, 1941 KiB  
Article
Structural, Quantum Chemical, and Cytotoxicity Analysis of Acetylplatinum(II) Complexes with PASO2 and DAPTA Ligands
by Stefan Richter, Dušan Dimić, Milena R. Kaluđerović, Fabian Mohr and Goran N. Kaluđerović
Inorganics 2025, 13(8), 253; https://doi.org/10.3390/inorganics13080253 - 27 Jul 2025
Viewed by 308
Abstract
The development of novel platinum-based anticancer agents remains a critical objective in medicinal inorganic chemistry, particularly in light of resistance and toxicity limitations associated with cisplatin. In this study, the synthesis, structural characterization, quantum chemical analysis, and cytotoxic evaluation of four new acetylplatinum(II) [...] Read more.
The development of novel platinum-based anticancer agents remains a critical objective in medicinal inorganic chemistry, particularly in light of resistance and toxicity limitations associated with cisplatin. In this study, the synthesis, structural characterization, quantum chemical analysis, and cytotoxic evaluation of four new acetylplatinum(II) complexes (cis-[Pt(COMe)2(PASO2)2], cis-[Pt(COMe)2(DAPTA)2], trans-[Pt(COMe)Cl(DAPTA)2], and trans-[Pt(COMe)Cl(PASO2)]: 14, respectively) bearing cage phosphine ligands PASO2 (2-thia-1,3,5-triaza-phosphaadamantane 2,2-dioxide) and DAPTA (3,7-diacetyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane) are presented. The coordination geometries and NMR spectral features of the cis/trans isomers were elucidated through multinuclear NMR and DFT calculations at the B3LYP/6-311++G(d,p)/LanL2DZ level, with strong agreement between experimental and theoretical data. Quantum Theory of Atoms in Molecules (QTAIM) analysis was applied to investigate bonding interactions and assess the covalent character of Pt–ligand bonds. Cytotoxicity was evaluated against five human cancer cell lines. The PASO2-containing complex in cis-configuration, 1, demonstrated superior activity against thyroid (8505C) and head and neck (A253) cancer cells, with potency surpassing that of cisplatin. The DAPTA complex 2 showed enhanced activity toward ovarian (A2780) cancer cells. These findings highlight the influence of ligand structure and isomerism on biological activity, supporting the rational design of phosphine-based Pt(II) anticancer drugs. Full article
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19 pages, 1230 KiB  
Article
Bioactive Potential of Rheum cordatum Losinsk. Leaf Extracts: Phytochemical Insights from Supercritical CO2, Subcritical Ethanol and Ultrasound-Assisted Extractions
by Madina Amangeldinova, Mehmet Ersatır, Pınar Küce Cevik, Mustafa Abdullah Yilmaz, Oguz Cakır, Nataliya Kudrina, Aizhan Mussayeva, Timur Kulmanov, Nina Terletskaya and Metin Yildirim
Plants 2025, 14(15), 2314; https://doi.org/10.3390/plants14152314 - 26 Jul 2025
Viewed by 247
Abstract
Rheum cordatum Losinsk is a plant species distributed in Kazakhstan but remains relatively understudied despite its promising biological potential. The present study aimed to explore leaf extracts of R. cordatum by utilizing advanced green extraction technologies including supercritical CO2 (ScCO2), [...] Read more.
Rheum cordatum Losinsk is a plant species distributed in Kazakhstan but remains relatively understudied despite its promising biological potential. The present study aimed to explore leaf extracts of R. cordatum by utilizing advanced green extraction technologies including supercritical CO2 (ScCO2), subcritical ethanol (Sc) and ultrasound-assisted extraction (UAE) to characterize their phytochemical composition and evaluate their antioxidant and antimicrobial activities. A total of 53 phytochemical compounds were identified, with gallic acid (30.71 µg/mg UAE-EtOH-4h), rutin (21.93 µg/mg ScCO2-150) and hesperidin (14.98 µg/mg ScCO2-150) being notably abundant. Among the tested extracts, ScCO2 extraction at 150 bar (ScCO2-150) demonstrated the highest antioxidant activity, exhibiting IC50 values of 0.0132 mg/mL (DPPH) and 0.0462 mg/mL (ABTS), coupled with the highest total phenolic content (140 mg GAE/g). Moreover, the ScCO2-150 extract showed pronounced antimicrobial efficacy, particularly against Bacillus subtilis Pseudomonas aeruginosa and Staphylococcus aureus, with minimum inhibitory concentrations (MIC) ranging from 125 to 250 µg/mL. These findings highlight the considerable potential of R. cordatum leaves as a valuable, abundant and sustainable source of natural antioxidants and antimicrobial agents, with supercritical CO2 extraction presenting substantial advantages in selectively obtaining bioactive phytochemicals. Full article
(This article belongs to the Section Phytochemistry)
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16 pages, 2096 KiB  
Article
Acridine Derivatives as Antifungal and Antivirulence Agents Against Candida albicans
by Amra Yunus, Oluwatosin Oluwaseun Faleye, Jin-Hyung Lee and Jintae Lee
Int. J. Mol. Sci. 2025, 26(15), 7228; https://doi.org/10.3390/ijms26157228 - 25 Jul 2025
Viewed by 371
Abstract
Candida albicans is a clinically important fungal pathogen capable of causing both superficial and systemic infections, particularly in immunocompromised individuals. A key factor contributing to its pathogenicity is its ability to form biofilms, structured microbial communities that confer significant resistance to conventional antifungal [...] Read more.
Candida albicans is a clinically important fungal pathogen capable of causing both superficial and systemic infections, particularly in immunocompromised individuals. A key factor contributing to its pathogenicity is its ability to form biofilms, structured microbial communities that confer significant resistance to conventional antifungal therapies. Addressing this challenge, we explored the antivirulence potential of acridine derivatives, a class of heterocyclic aromatic compounds known for their diverse biological activities, including antimicrobial, antitumor, and antiparasitic properties. In this study, a series of acridine derivatives was screened against C. albicans biofilms, revealing notable inhibitory activity and highlighting their potential as scaffolds for the development of novel antifungal agents. Among the tested compounds, acridine-4-carboxylic acid demonstrated the most promising activity, significantly inhibiting the biofilm formation at 10 µg/mL without affecting planktonic cell growth, and with a minimum inhibitory concentration (MIC) of 60 µg/mL. Furthermore, it attenuated filamentation and cell aggregation in a fluconazole-resistant C. albicans strain. Toxicity assessments using Caenorhabditis elegans and plant models supported its low-toxicity profile. These findings highlight the potential of acridine-based scaffolds, particularly acridine-4-carboxylic acid, as lead structures for the development of therapeutics targeting both fungal growth and biofilm formation in Candida albicans infections. Full article
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24 pages, 2749 KiB  
Article
Can In Vitro Cell Cultures of Eryngium planum, Lychnis flos-cuculi, and Kickxia elatine Be an Alternative Source of Plant Biomass with Biological Antimicrobial and Anti-Acanthamoeba Activities?
by Anastasia Aliesa Hermosaningtyas, Anna Budzianowska, Dariusz Kruszka, Monika Derda, Jolanta Długaszewska and Małgorzata Kikowska
Appl. Sci. 2025, 15(15), 8292; https://doi.org/10.3390/app15158292 - 25 Jul 2025
Viewed by 176
Abstract
The sustainable production of plant bioactive compounds is increasingly important as natural habitats decline. This study investigates whether in vitro cell cultures of Eryngium planum, Lychnis flos-cuculi, and Kickxia elatine can serve as alternative sources of biologically active biomass with antimicrobial [...] Read more.
The sustainable production of plant bioactive compounds is increasingly important as natural habitats decline. This study investigates whether in vitro cell cultures of Eryngium planum, Lychnis flos-cuculi, and Kickxia elatine can serve as alternative sources of biologically active biomass with antimicrobial and anti-Acanthamoeba properties. Callus cultures were established under optimized and controlled conditions, and metabolomic profiling was completed using UPLC-HRMS/MS. In silico analysis, using a molecular docking approach, was applied to understand the interaction between target compounds and Acanthamoeba profilin and identify possible targets for antimicrobial properties. Untargeted metabolomic analysis confirmed the presence of valuable compounds in the callus cultures of the studied species. Biological activity was assessed through anti-Acanthamoeba and antimicrobial assays. Lychnis flos-cuculi and Kickxia elatine callus extracts showed significant inhibitory effects on Acanthamoeba trophozoites, with 87.5% and 80.1% inhibition at 10 mg/mL, respectively. In contrast, E. planum extract stimulated amoebic growth. The anti-Acanthamoeba activity correlated with the presence of ferulic acid and p-coumaric acid in L. flos-cuculi extract, and acteoside in K. elatine extract. Antibacterial testing revealed moderate activity of E. planum and K. elatine extracts against Staphylococcus spp., while Gram-negative bacteria and fungi were largely resistant. These findings highlight the potential of in vitro cultures—particularly those from L. flos-cuculi and K. elatine—as promising, sustainable sources of anti-Acanthamoeba and antimicrobial agents, warranting further investigation into their pharmacologically active constituents. Full article
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19 pages, 5345 KiB  
Article
Identification of Novel Biomarkers in Huntington’s Disease Based on Differential Gene Expression Meta-Analysis and Machine Learning Approach
by Nayan Dash, Md Abul Bashar, Jeonghan Lee and Raju Dash
Appl. Sci. 2025, 15(15), 8286; https://doi.org/10.3390/app15158286 - 25 Jul 2025
Viewed by 145
Abstract
Huntington’s disease (HD) is a severe and progressive neurodegenerative disease for which therapeutic options have so far been confined to symptomatic treatment. Currently, the diagnosis relies on the signs and symptoms shown by patients; however, by that stage, the psychomotor issues have progressed [...] Read more.
Huntington’s disease (HD) is a severe and progressive neurodegenerative disease for which therapeutic options have so far been confined to symptomatic treatment. Currently, the diagnosis relies on the signs and symptoms shown by patients; however, by that stage, the psychomotor issues have progressed to a point where reversal of the condition is unattainable. Although numerous clinical trials have been actively investigating therapeutic agents aimed at preventing the onset of disease or slowing down the disease progression, there has been a constant need for reliable biomarkers to assess neurodegeneration, monitor disease progression, and assess the efficacy of treatments accurately. Therefore, to discover the key biomarkers associated with the progression of HD, we employed bioinformatics and machine learning (ML) to create a robust pipeline that integrated differentially expressed gene (DEG) analysis with ML to select potential biomarkers. We performed a meta-analysis to identify DEGs using three Gene Expression Omnibus (GEO) microarray datasets from different platforms related to HD-affected brain tissue, applying both relaxed and strict criteria to identify differentially expressed genes. Subsequently, focusing only on genes identified through the inclusive threshold, we employed 19 diverse ML techniques to explore the common genes that contributed to the top three selected ML algorithms and the shared genes that had an impact on the ML algorithms and were observed in the meta-analysis using the stringent condition were selected. Additionally, a receiver operating characteristic (ROC) analysis was conducted on external datasets to validate the discriminatory power of the identified genes. Based on the results of an inverse variance weighted meta-analysis of the AUCs across both human and mouse cohorts, GABRD and PHACTR1 were identified as the most robust candidates and were selected as key biomarkers for HD. Our comprehensive methodology, which integrates DEG meta-analysis with ML techniques, enabled a systematic prioritization of these biomarkers, providing valuable insights into their biological significance and potential for further validation in clinical research. Full article
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