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Role of copper chelating agents: between old applications and new perspectives in neuroscience

Neural Regeneration Research 2025年第3期20卷 751-762页

作者： Rosalba Leuci Leonardo Brunetti Vincenzo Tufarelli Marco Cerini Marco Paparella Nikola Puvača Luca Piemontese Department of pharmacy-Pharmaceutical science University of Bari Aldo MoroBariItaly Department of Precision and Regenerative Medicine and Jonian Area(DiMePRe-J) Section of Veterinary Science and Animal ProductionUniversity of Bari Aldo MoroBariItaly Department of Engineering Management in Biotechnology Faculty of Economics and Engineering Management in Novi SadUniversity Business Academy in Novi SadNovi SadSerbia

The role of copper element has been an increasingly relevant topic in recent years in the fields of human and animal health, for both the study of new drugs and innovative food and feed supplements. This metal plays an important role in the central nervous system, where it is associated with glutamatergic signaling, and it is widely involved in inflammatory processes. Thus, diseases involving copper(Ⅱ) dyshomeostasis often have neurological symptoms, as exemplified by Alzheimer's and other diseases(such as Parkinson's and Wilson's diseases). Moreover, imbalanced copper ion concentrations have also been associated with diabetes and certain types of cancer, including glioma. In this paper, we propose a comprehensive overview of recent results that show the importance of these metal ions in several pathologies, mainly Alzheimer's disease, through the lens of the development and use of copper chelators as research compounds and potential therapeutics if included in multi-target hybrid drugs. Seeing how copper homeostasis is important for the well-being of animals as well as humans, we shortly describe the state of the art regarding the effects of copper and its chelators in agriculture, livestock rearing, and aquaculture, as ingredients for the formulation of feed supplements as well as to prevent the effects of pollution on animal productions.

关键词： agriculture Alzheimer's disease chelators copper feed supplements multi-target

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Utilizing engineered extracellular vesicles as delivery vectors in the management of ischemic stroke:a special outlook on mitochondrial delivery

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Neural Regeneration Research 2025年第8期20卷 2181-2198页

作者： Jiali Chen Yiyang Li Xingping Quan Jinfen Chen Yan Han Li Yang Manfei Zhou Greta Seng Peng Mok Ruibing Wang Yonghua Zhao Institute of Chinese medical sciences State Key Laboratory of Quality Research in Chinese MedicineUniversity of MacaoTaipaMacao Special Administrative RegionChina Department of pharmacy Hunan Provincial People’s Hospitalthe First Affiliated Hospital of Hunan Normal UniversityChangshaHunan ProvinceChina Department of Electrical and Computer Engineering University of MacaoTaipaMacao Special Administrative RegionChina Department of Pharmaceutical sciences Faculty of Health SciencesUniversity of MacaoTaipaMacao Special Administrative RegionChina

Ischemic stroke is a secondary cause of mortality worldwide,imposing considerable medical and economic burdens on *** vesicles,serving as natural nanocarriers for drug delivery,exhibit excellent biocompatibility in vivo and have significant advantages in the management of ischemic ***,the uncertain distribution and rapid clearance of extracellular vesicles impede their delivery *** utilizing membrane decoration or by encapsulating therapeutic cargo within extracellular vesicles,their delivery efficacy may be greatly ***,previous studies have indicated that microvesicles,a subset of large-sized extracellular vesicles,can transport mitochondria to neighboring cells,thereby aiding in the restoration of mitochondrial function post-ischemic *** extracellular vesicles have also demonstrated the capability to transfer mitochondrial components,such as proteins or deoxyribonucleic acid,or their sub-components,for extracellular vesicle-based ischemic stroke *** this review,we undertake a comparative analysis of the isolation techniques employed for extracellular vesicles and present an overview of the current dominant extracellular vesicle modification *** the complex facets of treating ischemic stroke,we also delineate various extracellular vesicle modification approaches which are suited to different facets of the treatment ***,given the burgeoning interest in mitochondrial delivery,we delved into the feasibility and existing research findings on the transportation of mitochondrial fractions or intact mitochondria through small extracellular vesicles and microvesicles to offer a fresh perspective on ischemic stroke therapy.

关键词： delivery engineering extracellular vesicles identification ischemic stroke isolation mitochondria targeting strategy therapeutic effects

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Antioxidant and lipoxygenase inhibitory properties of a novel flavonoid from Pistacia chinensis Bunge and its molecular docking analysis

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Traditional Medicine Research 2025年第2期10卷 30-36页

作者： Abdur Rauf Zuneera Akram Naveed Muhammad Najla AlMasoud Taghrid Saad Alomar Saima Naz Abdul Wadood Chandni Hayat Marcello Iriti Department of Chemistry University of SwabiAmbar 23561Pakistan Department of Pharmacology Faculty of Pharmaceutical SciencesBaqai Medical UniversityKarachi 74600Pakistan Department of pharmacy Abdul Wali Khan University MardanMardan 23200Pakistan Department of Chemistry College of SciencePrincess Nourah bint Abdulrahman UniversityRiyadh 11671Saudi Arabia Department of Biotechnology BKUC-Bacha Khan University CharsaddaCharsadda 24620Pakistan Department of Biochemistry Abdul Wali Khan University MardanMardan 23200Pakistan Department of Biomedical Surgical and Dental SciencesUniversity of MilanMilan 20129Italy National Interuniversity Consortium of Materials science and Technology(INSTM) Firenze 50121Italy

Background:Pistacia chinensis Bunge has been traditionally used to manage various conditions,including asthma,pain,inflammation,hepatoprotection,and *** study was conducted to investigate the antioxidant and anti-lipoxygenase(LOX)properties of the isolated compound 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one from Pistacia ***:LOX assay and antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl(DPPH)assay were *** docking studies were conducted using a molecular operating ***:The LOX assay revealed significant inhibitory effects at 0.2µM concentration,with an IC50 value of 37.80µ*** antioxidant effect demonstrated dose-dependency across 5 to 100µg/mL concentrations,reaching 93.09%at 100µg/mL,comparable to ascorbic acid’s 95.43%*** docking studies highlighted strong interactions with the lipoxygenase enzyme,presenting an excellent docking score of-10.98 kcal/***:These findings provide valuable insights into Pistacia chinensis’chemical components and biological effects,reinforcing its traditional medicinal applications.

关键词： Pistacia chinensis Bunge antioxidant DPPH assay antilipoxygenase docking analysis

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SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL ACTIVITY OF POLYKETONES

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Chinese Journal of Polymer science 2013年第3期31卷 471-480页

作者： Ismail A.Alkskas Altaher M.Alhubge Faizul Azam Polymer Lab Department of ChemistryFaculty of ScienceMisurata University Department of Microbiology Faculty of ScienceMisurata University faculty of pharmacy Misurata University

Polyketone resins have been prepared by the Friedel-Crafts polymerization of dithiophenylidenecyclopentanone （I）, dithiophenylidenecyclohexanone （II） and dithiophenylideneacetone （III） with adipoyl, sebacoyl and terephthaloyl dichlorides using boron trifluoride as catalyst and carbon disulphide as solvent. Polymers were characterized with IR, 1H- NMR, and the results showed the presence of carbonyl of ketonic groups in the main chain. The polyketones have inherent viscosities of 0.40-0.70 dL/g. All the polymers are semicrystalline and most of them are partially soluble in most common organic solvents but freely soluble in aprotic solvents. The temperatures of 50% weight loss are as high as 185℃ to 280℃ in air, indicating that these aromatic polyketones have excellent thermal stability. All the polyketones were tested for their antimicrobial activity against bacteria and fungi.

关键词： Synthesis Characterization Polyketones Biological activity.

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Synthesis and Characterization of Polyesters Based on Diethylketone Moiety

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Chinese Journal of Polymer science 2014年第11期32卷 1450-1459页

作者： Ismail A.Alkskas Bashir A.El-gnidi Khadija M.Ghalieo Faizul Azam Polymer Lab Department of ChemistryFaculty of ScienceMisurata University faculty of pharmacy Misurata University

A new class of unsaturated polyesters based on diethylketone have been prepared by interfacial polymerization of 2,4-bis（4-hydroxybenzylidene）-3-pentanone（I） and 2,4-bis（4-hydroxy-3-methoxybenzylidene）-3-pentanone（II） with 4,4’-azodibenzoyl chloride and 3,3’-azodibenzoyl chloride at ambient temperature. The model compounds were synthesized by reaction of（I） and（II） with benzoyl chloride. The new monomers, model compounds and polyesters have been characterized by different spectral analyses. The polyesters have inherent viscosity of 0.55-0.80 d L/g and moderate number average molecular weight（Mn） in the range of 6150-7400 g/mol. Most of the compounds exhibited their solubility in aprotic solvents while partial solubility in various halogenated organic solvents was observed. The temperatures of 10% weight loss were high（225-330 °C） in nitrogen, indicating that these polyesters have excellent thermal stability. Doping with iodine dramatically raised the conductivity and produced brown colored semiconductive polymers with a maximum conductivity of 2.7 × 10-6 --1cm-1. Moreover, the morphological properties of selected example of polyesters were detected by SEM.

关键词： Diethylketone Azo Polyesters Conductivity.

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Preparation of polypyrrole/nanosilica composite for solid-phase microextraction of bisphenol and phthalates migrated from containers to eye drops and injection solutions

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Journal of Pharmaceutical Analysis 2019年第3期9卷 185-192页

作者： Mehdi Ansari Dogaheh Mansoureh Behzadi Department of Pharmaceutics Faculty of Pharmacy Kerman Medical Science University Kerman Iran Department of Chemistry Faculty of Science Shahid Bahonar University of Kerman Kerman Iran

This paper describes the electrodeposition of polyphosphate-doped polypyrrole/nanosilica nano-composite coating on steel wire for direct solid-phase microextraction of bisphenol A and five phthalates. We optimized influencing parameters on the extraction efficiency and morphology of the nanocomposite such as deposition potential, concentration of pyrrole and polyphosphate, deposition time and the nanosilica amount. Under the optimized conditions, characterization of the nanocomposite was inves-tigated by scanning electron microscopy and Fourier transform infra-red spectroscopy. Also, the factors related to the solid-phase microextraction method including desorption temperature and time, extrac-tion temperature and time, ionic strength and pH were studied in detail. Subsequently, the proposed method was validated by gas chromatography-mass spectrometry by thermal desorption and acceptable figures of merit were obtained. The linearity of the calibration curves was between 0.01 and 50 ng/mL with acceptable correlation coefficients (0.9956-0.9987) and limits of detection were in the range 0.002-0.01 ng/mL. Relative standard deviations in terms of intra-day and inter-day by five replicate analyses from aqueous solutions containing 0.1 ng/mL of target analytes were in the range 3.3%-5.4% and 5%-7.1%, respectively. Fiber-to-fiber reproducibilities were measured for three different fibers prepared in the same conditions and the results were between 7.3% and 9.8%. Also, extraction recoveries at two different concentrations were ≥96%. Finally, the suitability of the proposed method was demonstrated through its application to the analysis of some eye drops and injection solutions.

关键词： Solid-phase microextraction Gas chromatography-mass spectrometry Polyphosphate-doped polypyrrole Nanosilica Phthalates BisphenolA

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Development of pectin nanoparticles through mechanical homogenization for dissolution enhancement of itraconazole

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Asian Journal of Pharmaceutical sciences 2016年第3期11卷 365-375页

作者： Kanokporn Burapapadh Hirofumi Takeuchi Pornsak Sriamornsak Department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University Pharmaceutical Biopolymer Group (PBiG) Faculty of Pharmacy Silpakorn University Laboratory of Pharmaceutical Engineering Gifu Pharmaceutical University

A simple method to fabricate itraconazole(ITZ)-loaded pectin nanoparticles prepared from nanoemulsion templates is described in this study. Nanoemulsions containing ITZ were prepared by a mechanical homogenization using pectin as emulsifier. After freeze-drying, the morphology, crystallinity state, thermal properties, drug dissolution and stability of the obtained pectin nanoparticles were characterized. The results demonstrated that the morphology of freeze-dried products was different, depending on the type of internal phase; the nanoparticles prepared from chloroform-based nanoemulsions were completely dried and provided a fragile characteristic. The pectin nanoparticles also demonstrated good properties in terms of redispersibility, thermal properties, drug crystallinity and dissolution. The ITZ-loaded pectin nanoparticles showed high percentage of drug dissolved(about 60–80%within 2 h), and maintained their good dissolution properties even after 1-year storage. The results suggested that freeze-dried pectin nanoparticles prepared from nanoemulsions could be used as an effective carrier for enhancement of ITZ dissolution.

关键词： Itraconazole Nanoparticles Pectin Poorly water-soluble drug Stability

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Gene therapy for spinal muscular atrophy:perspectives on the possibility of optimizing SMN1 delivery to correct all neurological and systemic perturbations

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Neural Regeneration Research 2025年第7期20卷 2011-2012页

作者： Sharon J.Brown Rafael J.Yáñez-Muñoz Heidi R.Fuller School of pharmacy and Bioengineering Keele UniversityKeeleUK Wolfson Center for Inherited Neuromuscular Disease TORCH BuildingRJAH Orthopaedic HospitalOswestryUK *** Center of Gene and Cell TherapyDepartment of Biological SciencesSchool of Life Sciences and the EnvironmentRoyal Holloway University of LondonEghamUK

Spinal muscular atrophy(SMA)is a genetic condition that results in selective lower motor neuron loss with concomitant muscle weakness and *** genetic cause of SMA was understood in 1995 when loss or impairment of the survival motor neuron 1(SMN1)gene was identified as the main contributing factor(Lefebvre et al.,1995).This,in combination with the discovery that humans have a“back-up”gene,SMN2,which can produce low levels(approximately 10%)of the full-length functional SMN protein,has led to the generation of SMA-specific gene *** was traditionally classified according to age of symptom onset and developmental milestones achieved,with life expectancy and severity varying between ***,SMN2 copy number is used as a proxy for the prediction of disease severity,with higher SMN2 copy number typically being associated with reduced severity of SMA,although this relationship is not absolute:some individuals with low SMN2 copy number have less severe SMA phenotypes and vice ***,the etiology of SMA is further complicated by other factors,such as non-typical nucleotide variants and SMN2-independent modifiers of disease severity.

关键词： atrophy traditionally absolute

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The First Example of a Supramolecular Structure Containing [2-(1H-Pyrazol-3-yl)-pyridine] Complex and both α-and β-Octamolybdates

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Chinese Journal of Structural Chemistry 2009年第8期28卷 1013-1017页

作者：赵文秀董顺福张伟萍彭军庞海军 faculty of pharmacy Jilin Medical College Key Laboratory of Polyoxometalate science of Ministry of Education Faculty of Chemistry Northeast Normal University

The title compound, [Ni（C8N3H7）3]4[Mo8O26]2·6H2O 1, has been synthesized from the reaction of 2-（1H-pyrazol-3-yl）-pyridine （L） with （NH4）2MoO4·2H2O and NiCl2·6H2O. Elemental analysis, IR, UV spectra and X-ray single-crystal diffraction were carried out to determine the composition and crystal structure of the compound. Crystal data： C96H96Mo16N36Ni4O58, Mr = 4451.97, monoclinic system, space group P21/n, a = 20.846（5）, b = 14.825（5）, c = 23.122（5） A ,β= 91.594（5）°, V = 7143（3）A^3, Z = 2, F（000） = 4344, Dc = 2.070 g/cm^3,μ = 1.968 mm^-1, R = 0.0452 and wR = 0.1056 for 17102 independent reflections （Rint = 0.0442） and 11074 observed reflections （I 〉 2σ（I））. Structural analysis indicates that two kinds of octamolybdates （[α-Mo8026]^4- and [β-Mo8026]^4-） co-exist in the compound. This is the first example of a supramolecular structure containing L complex as well as both α- and β-octamolybdate clusters.

关键词： crystal structure octamolybdate 2-(1H-pyrazol-3-yl)-pyridine supramolecularnetwork nickel(II ) complex

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Fabrication and characterization of spearmint oil loaded nanoemulsions as cytotoxic agents against oral cancer cell

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Asian Journal of Pharmaceutical sciences 2018年第5期13卷 425-437页

作者： Sukannika Tubtimsri Chutima Limmatvapirat Siripan Limsirichaikul Prasert Akkaramongkolporn Yutaka Inoue Sontaya Limmatvapirat faculty of Pharmaceutical science Burapha University Department of Pharmaceutical Technology Faculty of Pharmacy Silpakorn University Department of Pharmaceutical Chemistry Faculty of Pharmacy Silpakorn University Department of Biopharmacy Faculty of Pharmacy Silpakorn University Laboratory of Drug Safety Management Faculty of Pharmacy and Pharmaceutical Science Josai University

Spearmint oil(SMO), a commonly used essential oil for oral care products, possesses various interesting functions, especially for anticancer property. However, the application of SMO for cancer treatment is limited due to water insoluble. In the present study, nanoemulsions, which have been widely accepted as dosage forms for poorly water-soluble drugs, were selected as candidate carriers for SMO to inhibit oral cancer cell. The nanoemulsions were fabricated using phase inversion temperature method. The factors affecting formation and properties of nanoemulsions including type and amount of surfactants, oil loading and ratio of SMO to virgin coconut oil(VCO) were investigated. Among the surfactants used, the nanoemulsions containing polyoxyethylene castor oil derivatives(Kolliphor ?EL; PCO35, Cremophor ?RH40; PCO40, Eumulgin ?CO60; PCO60) and polyoxyethylene sorbitan fatty acid esters(PSF80) showed 100% creaming after temperature cycling test indicating excellent physical stability while those containing PCO40 demonstrated more transparency and better physical stability. With an increasing amount of PCO40, the droplet size tended to decrease and was in the nano-size range( < 1000 nm) after increasing to more than 5%(w/w). SMOVCO loading also influenced on the droplet size. At 5%(w/w) PCO40, the maximum SMO-VCO loading of 25%(w/w) to attain nanoemulsions was observed. Moreover, the composition of oils had an impact on size of emulsions. The transparent nanoemulsions were only prepared in the range of SMO-VCO from 40:60 to 80:20, suggesting the optimum ratio of SMO tosurfactant and the composition of oils were the critical factors for formation of nanoemulsions. NMR study disclosed that the interaction between PCO40 with both VCO and SMO should be a possible stabilization mechanism. Furthermore, the SMO-VCO nanoemulsions exhibited significant cytotoxic effect against oral carcinoma(KON) cell line using MTT assay. The finding, therefore, revealed the good feasibility o

关键词： Nanoemulsions Spearmint oil Coconut oil Surfactants Anticancer NMR

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