A Superior Corrosion Protection of Mg Alloy via Smart Nontoxic Hybrid Inhibitor-Containing Coatings

Molecules, Journal Year: 2023, Volume and Issue: 28(6), P. 2538 - 2538

Published: March 10, 2023

The increase of corrosion resistance magnesium and its alloys by forming the smart self-healing hybrid coatings was achieved in this work two steps. In first step, using plasma electrolytic oxidation (PEO) treatment, a ceramic-like bioactive coating synthesized on surface biodegradable MA8 alloy. During second formed porous PEO layer impregnated with inhibitor 8-hydroxyquinoline (8-HQ) bioresorbable polymer polycaprolactone (PCL) different variations to enhance protective properties coating. composition, anticorrosion, antifriction were studied. 8-HQ allows controlling rate material degradation due effect PCL treatment inhibitor-containing significantly improves wear retains an pores layer. It revealed that incorporation method (including number steps, impregnation, type solvent) matters mechanism. obtained 1-step dichloromethane solution containing 6 wt.% 15 g/L are characterized best resistance. This demonstrates lowest value current density (3.02 × 10-7 A cm-2). formation results decrease 18 times (0.007 mm year-1) as compared blank (0.128 year-1). An efficiency established be 83.9%. mechanism protection Mg alloy via revealed.

Language: Английский

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8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases

Acta Pharmaceutica Sinica B, Journal Year: 2023, Volume and Issue: 13(5), P. 2152 - 2175

Published: Jan. 19, 2023

We describe the development of quinolylnitrones (QNs) as multifunctional ligands inhibiting cholinesterases (ChEs: acetylcholinesterase and butyrylcholinesterase-hBChE) monoamine oxidases (hMAO-A/B) for therapy neurodegenerative diseases. identified QN 19, a simple, low molecular weight nitrone, that is readily synthesized from commercially available 8-hydroxyquinoline-2-carbaldehyde. Quinolylnitrone 19 has no typical pharmacophoric element to suggest ChE or MAO inhibition, yet unexpectedly showed potent inhibition hBChE (IC50 = 1.06 ± 0.31 nmol/L) hMAO-B 4.46 0.18 μmol/L). The crystal structures with provided structural basis binding, which was further studied by enzyme kinetics. Compound acted free radical scavenger biometal chelator, crossed blood-brain barrier, not cytotoxic, neuroprotective properties in 6-hydroxydopamine cell model Parkinson's disease. In addition, vivo studies anti-amnesic effect scopolamine-induced mouse AD without adverse effects on motoric function coordination. Importantly, chronic treatment double transgenic APPswe-PS1δE9 mice reduced amyloid plaque load hippocampus cortex female mice, underscoring disease-modifying 19.

Language: Английский

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Chelation in Antibacterial Drugs: From Nitroxoline to Cefiderocol and Beyond

Antibiotics, Journal Year: 2022, Volume and Issue: 11(8), P. 1105 - 1105

Published: Aug. 15, 2022

In the era of escalating antimicrobial resistance, need for antibacterial drugs with novel or improved modes action (MOAs) is a health concern utmost importance. Adding improving chelating abilities existing finding new, nature-inspired agents seems to be one major ways ensure progress. This review article provides insight into agents, class by class, through perspective chelation. We covered wide scope antibacterials, from century-old quintessential agent nitroxoline, currently unearthed due its newly discovered anticancer and antibiofilm activities, over commonly used classes, new cephalosporin cefiderocol potential future tetramates. show impressive spectrum roles that chelation plays in MOAs. This, itself, demonstrates importance understanding fundamental chemistry behind such complex processes.

Language: Английский

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Cu(II) and Zn(II) Complexes of New 8-Hydroxyquinoline Schiff Bases: Investigating Their Structure, Solution Speciation, and Anticancer Potential

Inorganic Chemistry, Journal Year: 2023, Volume and Issue: 62(29), P. 11466 - 11486

Published: July 13, 2023

We report the synthesis and characterization of three novel Schiff bases (L1-L3) derived from condensation 2-carbaldehyde-8-hydroxyquinoline with amines containing morpholine or piperidine moieties. These were reacted CuCl2 ZnCl2 yielding six new coordination compounds, general formula ML2, where M = Cu(II) Zn(II) L L1-L3, which all characterized by analytical, spectroscopic (Fourier transform infrared (FTIR), UV-visible absorption, nuclear magnetic resonance (NMR), electron paramagnetic (EPR)), mass spectrometric techniques, as well single-crystal X-ray diffraction. In solid state, two complexes, L1 L2, are obtained dinuclear relatively short Cu-Cu distances (3.146 3.171 Å for Cu2(L1)4 Cu2(L2)4, respectively). The free ligands show moderate lipophilicity, while their complexes more lipophilic. pKa values L1-L3 formation constants complex (for ML ML2) species determined spectrophotometric titrations, showing higher stability than complexes. EPR indicated presence several in solution pH varied binding modes proposed. to bovine serum albumin (BSA) was evaluated fluorescence circular dichroism (CD) spectroscopies. All bind BSA, demonstrated CD, process takes hours reach equilibrium. antiproliferative activity malignant melanoma cells (A375) noncancerous keratinocytes (HaCaT). display significant cytotoxicity (IC50 < 10 μM) but modest selectivity. ligands, being active approximately twice cytotoxic cisplatin. A Guava ViaCount assay corroborated activity.

Language: Английский

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Facing diseases caused by trypanosomatid parasites: rational design of multifunctional oxidovanadium(IV) complexes with bioactive ligands

Frontiers in Chemical Biology, Journal Year: 2024, Volume and Issue: 2

Published: Jan. 16, 2024

Searching for new prospective drugs against Chagas disease (American trypanosomiasis) and Leishmaniasis, a series of five heteroleptic vanadium compounds, [V IV O(L-H)(mpo)], where L are 8-hydroxyquinoline derivatives mpo is 2-mercaptopyridine N -oxide, synthesized characterized. Comprehensive characterizations conducted in solid state solution. The compounds evaluated on epimastigotes trypomastigotes Trypanosoma cruzi promastigotes Leishmania infantum , alongside VERO cells, as mammalian cell model. exhibit activity both forms T. L. with the trypomastigote infective stage displaying highest sensitivity. most selective compound O(L2-H)(mpo)], L2 = 5-chloro-7-iodo-8-hydroxyquinoline, globally shows adequate selectivity towards parasite was selected to carry out further in-depth biological studies. O(L2-H)(mpo)] significantly impacted infection potential cell-derived hindered replication amastigote form. Low total uptake by parasites preferential accumulation soluble proteins fraction, negligible localization DNA determined. A trypanocide effect observed across various concentrations compound. generation oxidative stress induction mitochondria-dependent apoptosis proposed main mechanisms parasite’s death V O compounds. Both theoretical predictions experimental data support hypothesis that inhibiting parasite-specific enzyme NADH-fumarate reductase plays crucial role trypanocidal action these complexes. Globally, O(L-H)(mpo)] complexes could be considered interesting anti- agents deserve research.

Language: Английский

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Solution chemical properties and anticancer potential of 8-hydroxyquinoline hydrazones and their oxidovanadium(IV) complexes

Journal of Inorganic Biochemistry, Journal Year: 2022, Volume and Issue: 235, P. 111932 - 111932

Published: July 15, 2022

We report the synthesis and characterization of a family benzohydrazones (Ln, n = 1-6) derived from 2-carbaldehyde-8-hydroxyquinoline benzylhydrazides containing different substituents in para position. Their oxidovanadium(IV) complexes were prepared compounds with 1:1 1:2 metal-to-ligand stoichiometry obtained. All characterized by elemental analyses mass spectrometry as well FTIR, UV-visible absorption, NMR (ligand precursors) EPR (complexes) spectroscopies, DFT computational methods. Proton dissociation constants, lipophilicity solubility aqueous media determined for all ligand precursors. Complex formation V(IV)O was evaluated spectrophotometry L4 (Me-substituted) L6 (OH-substituted) constants mono [VO(HL)]+, [VO(L)] bis [VO(HL)2], [VO(HL)(L)]-, [VO(L)2]2- determined. spectroscopy indicates [VO(HL)]+ this latter being major species at physiological pH. Noteworthy, data suggest behaviour L6, which confirm results obtained solid state. The antiproliferative activity malignant melanoma (A-375) lung (A-549) cancer cells. show much higher on A-375 (IC50 < 6.3 μM) than A-549 cells > 20 μM). 3 (F-substituted) shows lowest IC50 both cell lines lower cisplatin (in A-375). Studies identified compound one showing highest increase Annexin-V staining, caspase induction double stranded breaks, corroborating cytotoxicity results. mechanism action involves reactive oxygen (ROS) induced DNA damage, death apoptosis.

Language: Английский

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Cobalt-electrocatalytic C–H hydroxyalkylation ofN-heteroarenes with trifluoromethyl ketones

Chemical Science, Journal Year: 2022, Volume and Issue: 14(1), P. 143 - 148

Published: Nov. 21, 2022

By merging paired electrolysis and cobalt catalysis, we have developed an electrochemical redox-neutral coupling for the synthesis of N -heteroaryl trifluoromethyl carbinols from readily available -heteroarenes ketones.

Language: Английский

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Solution chemistry and anti-proliferative activity against glioblastoma cells of a vanadium(V) complex with two bioactive ligands

Frontiers in Chemical Biology, Journal Year: 2024, Volume and Issue: 3

Published: July 5, 2024

Introduction: Glioblastoma is a brain cancer difficult to treat but recently mixed-ligand vanadium(V) Schiff base/catecholato complexes have exhibited high in vitro anti-proliferative activity. Hence, we explored the activity of [V V OL 1 L 2 ], which contains two iron chelating ligands, 2-hydroxy-1-naphthylaldehyde iso -nicotinoyhydrazone (L H ) and clioquinol H). This complex was previously reported be very effective against Trypanosoma cruzi , causative agent Chagas disease. These studies possibility that compound with efficacy also has human glioblastoma cells. Since ] poorly soluble water ligand dissociated from upon addition an aqueous environment, understanding speciation important interpret its biological Methods: Stability cell media were followed by UV/Vis spectroscopy determine relevance T98G cells, measured absence presence Fe(III). Results Discussion: The current work demonstrated vanadium coordination had (T98G) line. enhanced effects cells could due either hydrolysis release toxic clioquinol, or rapid uptake lipophilic prior hydrolysis. showed at least part potent toxicity stemmed bioactive complex, depended on whether Fe(III) present. (O) H)] most remained intact and, hence, active. Thus, future development should focus one-ligand making any more soluble, stable solution, designed rapidly taken up diseased

Language: Английский

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Nitroxoline evidence Amoebicidal Activity against Acanthamoeba castellanii through DNA damage and the stress response pathways

International Journal for Parasitology Drugs and Drug Resistance, Journal Year: 2025, Volume and Issue: 27, P. 100578 - 100578

Published: Jan. 5, 2025

Acanthamoeba castellanii is a widespread unicellular eukaryote found in diverse environments, including tap water, soil, and swimming pools. It responsible for severe infections, such as keratitis granulomatous amebic encephalitis, particularly individuals with immunocompromisation. The ability of protozoans to form dormant persistent cysts complicates treatment, current therapies are ineffective against cyst stages suffer from poor specificity side effects. Nitroxoline, quinoline derivative well-established antibacterial, antifungal, antiviral properties, promising therapeutic candidate. This study aimed elucidate cellular signalling events that counteract the effects nitroxoline. In this study, nitroxoline significantly reduced viability A. trophozoites dose- time-dependent manner, inducing morphological changes apoptosis. Transcriptomic analysis revealed substantial alterations gene expression, enrichment metabolic pathways, DNA damage responses, iron ion binding. Nitroxoline treatment upregulated genes involved repair oxidative stress response while regulating methionine cysteine cycles. also decreased mitochondrial membrane potential, H₂S production, total amount castellanii. Bioinformatic analyses molecular docking studies suggest direct interactions between several proteins. Our research provides comprehensive map nitroxoline, revealing significant expression related pathways. These findings underscore potential potent anti-Acanthamoeba agent, offering new insights into its mechanism action paving way effective combinational strategies.

Language: Английский

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Marine actinobacteria metabolites: unlocking new treatments for acne vulgaris

Frontiers in Microbiology, Journal Year: 2025, Volume and Issue: 15

Published: Jan. 6, 2025

Marine-derived actinobacteria isolated from sponge Cliona varians and soft coral Eunicea fusca were screened for antibacterial activity against acne-related bacteria, specifically Staphylococcus epidermidis ATCC 14990, methicillin-resistant aureus BAA44, Cutibacterium acnes 6919. Cytotoxicity assays performed on human dermal fibroblast (HDFa) keratinocyte (HaCaT) cell lines to assess the safety profile of extracts. Chemical characterization was conducted using high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Among extracts, six derived Kocuria sp., Rhodococcus Nocardia Micrococcus Streptomyces sp. demonstrated significant activity. Notably, extract Z9.216 exhibited highest efficacy, inhibiting S. by 68%, 93%, C. 98.7% at a concentration 0.003 mg/mL, which comparable standard antibiotics erythromycin vancomycin, while maintaining over 90% viability in both HDFa HaCaT lines. Untargeted metabolomic analysis suggested that might be associated compounds chemical families alkaloids, terpenoids, fatty acids, among others. These findings highlight therapeutic potential marine underexplored environments as promising strategy treating acne vulgaris, chronic inflammatory skin condition.

Language: Английский

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