Metal complexes of Tridentate Schiff base: Synthesis, Characterization, Biological Activity and Molecular Docking Studies with COVID-19 Protein Receptor.

Mononuclear chelates of Cr(III), Mn(II), Fe(III), Ni(II), Cu(II), Zn(II) and Cd(II) resulted from new tridentate Schiff base ligand, 4-((1-(5-acetyl-2,4-dihydroxyphenyl)ethylidene)amino)-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one, were synthesized. Metal to ligand ratio was found to be1 : 1, which was revealed via elemental analysis and characterized via various spectroscopic tools. IR has point out that the coordination of the ligand towards the metal ions was carried out via NOO donor atoms. UV-Vis, 1H NMR spectral data, molar conductivity measurements, BET surface area, melting points and theoretically through density function theory were used such as characterizing techniques in supporting further interpretation of the complexes structures. The complexes were octahedral except Cu(II) and Ni(II) complexes were tetrahedral as suggested from the magnetic moment measurement. The complexes were found to have surface area, pore volume and particle radius of 23-176 m2 g-1, 0.02-0.33 cc/g and 8.71-4.32 nm, respectively, as pointed out from BET measurement. Schiff base ligand and metal complexes were tested in vitro to estimate their antimicrobial activity opposed to Gram-negative and Gram-positive bacterial and fungal organisms. MOE 2008 was used headed for screen potential drugs with molecular docking by the protein sites of new coronavirus and the study was constructed to molecular docking without validation through MD simulations.

A Study for Improving Compressive Strength of Cementitious Mortar Utilizing Magnetic Water.

This research investigates the means to improve the compressive strength of mortar mixtures through using novel mixtures. These mixtures include magnetic water (MW) and fly ash (FA). MW was obtained by circulating tap water (TW) through a magnetic field. The magnetization duration was represented by the number of cycles, the content of FA was replaced with cement, and the super plasticizer percentage (SP) and the curing age were used and evaluated experimentally for producing the mortar mixtures. Mortar flow, crushing compressive strength, and ultrasonic pulse velocity (UPV) tests were applied to evaluate the performances of mixing characteristics. The results demonstrate that the MW-treated mortar mixtures show higher compression strength results than those prepared by TW. The compressive strength was increased up to 60% with 150 cycles, a dose of 0.5% of SP and no FA content at the age of 56 days. The dose of SP can be cut down by a maximum of 40% to 50% in cementitious mortar. the workability was enhanced by a percentage of 70%.

Virtual Screening-Based Discovery of Potent Hypoglycemic Agents: In Silico, Chemical Synthesis and Biological Study.

BACKGROUND: Dipeptidyl peptidase IV has been reported to be an important target for the development and discovery of new therapies for diabetes mellitus type II. OBJECTIVE: The main aim of this study was to discover chemical entities that target the inhibition of DPP IV and feature potent hypoglycemic action. METHODS: A structure-based virtual screening was applied to discover new hypoglycemic agents. Molecular docking was performed to compute the binding free energies. Molecular dynamics simulations were done to evaluate the binding stability of resulted hits. RESULTS: Seven small non-peptide potential inhibitors of Dipeptidyl peptidase IV with 3-imino-4-(4- substituted phenyl)-1, 2, 5-thiadiazolidine-1,1-dioxide scaffold were discovered. The binding free energies ranged from -24.50 to -36.06 kJ/mol. Molecular dynamics simulations revealed high stability of all protein-ligand complexes with low root mean square deviation over 10 ns simulation time. The tested compounds expressed a significant reduction in blood glucose level up to 90% with excellent oral glucose tolerance test after 120 minutes of injection in a diabetes mellitus type II animal model. A promising release of insulin was observed with a potential hypoglycemic activity for all compounds. CONCLUSION: The virtual screening was successful to discover potent hypoglycemic agents with drug-like properties that may need more consideration for future studies and development.

The implementation of the Japanese Dental English core curriculum: active learning based on peer-teaching and learning activities.

BACKGROUND: Education in Japan and other Asian countries advocates the stereotypical passive learning style where students are limited in their breadth of knowledge dismissing anything not imparted by their teachers. With globalized education, professions are becoming very competitive, embracing student-centeredness compelling them to introduce active learning activities. A study funded by Japan's Ministry of Education conducted a needs analysis, proposed a solution, and implemented an active learning approach. Since the latter is still new in the Japanese teaching-learning environment, this current study aimed at assessing the willingness of undergraduate students of dental medicine to participate in active learning activities rather than the typical passive-style teaching-learning educational process. METHODS: Three active implementation-learning activities, namely International Group Discussions (IGD), Student-Teacher Experience (STE) and Role Play Activities (RPA) were included in the Dental English course in a classroom setting at a dental school in Japan. Students had to choose between participating in the activity or taking the final examination. Two hundred and three third-year undergraduate dental students participated over a 5-year period from October 2013 to March 2017. For IGD, the researchers assigned students to a topic and grouped them with visiting international exchange students. For STE, researchers gave students teacher-prepared presentation slides on basic dental topics, which they presented in front of their classmates. For RPA, students had to do prepared role-play and impromptu role play. Peer and teacher feedbacks of the activities were given to all students. At the end of the course, the students evaluated the active learning activities and wrote their comments in a free entry survey. RESULTS: All 203 students participated in the active learning activities confirming the changing learning needs of Japanese students in this dental school. The most common comment was that the class was interesting, fun, an easy-to-understand way to learn dental terms, and a safe way to express themselves in the English language. CONCLUSION: The majority of Japanese students preferred the active learning style. The study revealed that students reported greater engagement and better learning with proper guidance and time to prepare for the activities.

Bioactive new metabolites from the green alga Udotea orientalis growing on the Gorgonian coral Pseudopterogorgia rigida.

As part of our continued search for bioactive secondary metabolites from marine sources using a bioassay-guided fractionation technique (Cytotoxic and anti-trypanosome activities), we have examined the organic extract of Papua New Guinean collection of the green alga Udotea orientalis growing on the Gorgonian coral Pseudopterogorgia rigida. Successive HPLC investigations resulted in isolation of three new compounds, (+) curcuepoxide A, (+) curcuepoxide B and (+)-10α-hydroxycurcudiol. Analysis of different spectroscopic data e.g. UV, IR, LRMS, HRMS, 1D NMR and 2D NMR on the isolated compounds allowed for construction of the planar structures. Stereochemistry assignment at C-7 and C-10 in the new compounds was discussed. Isolated compounds were found to be active in an in vitro assay of antitrypanosome activity. The isolated compounds were found to have variable cytotoxic activity in human lung cancer cell lines.

Cytotoxic halogenated monoterpenes from Plocamium cartilagineum.

As a result of our efforts to identify bioactive agents from marine algae, we have isolated and identified one new halogenated monoterpene 1 [(-)-(5E,7Z)-348-trichloro-7-dichloromethyl-3-methyl-157-octatriene] in addition to three known compounds (2, 3 and 4) from the red alga Plocamium cartilagineum collected by hand from the eastern coast of South Africa. Compound 1 was found to be active as a cytotoxic agent in human lung cancer (NCI-H460) and mouse neuro-2a cell lines (IC50 4 µg/mL). Two of these compounds (3 and 4) were found to have cytotoxic activity in other cell line assays, especially against human leukaemia and human colon cancers (IC50 1.3 µg/mL). None of these metabolites were active as sodium channel blockers or activators. All structures were determined by spectroscopic methods (UV, IR, LRMS, HRMS, 1D NMR and 2D NMR). 1D and 2D NOE experiments were carried out on these compounds to confirm the geometry of the double bonds.

Prevalence of prematurely lost primary teeth in 5-10-year-old children in Thamar city, Yemen: A cross-sectional study.

OBJECTIVES: The premature loss of primary teeth is a potential risk factor for poor arch length development. Adequate arch length is important to the progression of the permanent teeth. Poor arch length can lead to crowding, ectopic eruption, or impaction of these teeth. This study is designed to assess the prevalence of premature loss of primary teeth in the 5-10-year-old age group. MATERIALS AND METHODS: The study group included 185 children, that is, 91 boys and 94 girls. The dental examination was conducted by an experienced examiner under sufficient artificial light. Data including patient age and missing teeth were collected. Descriptive statistics were applied for data analysis, and from the results, Chi-square tests were used at a level of significance of 5% (P < 0.05). RESULTS: We observed a 40.54% prevalence of premature loss of primary teeth with no statistically significant difference between genders. The lower left primary second molar was the most commonly absent tooth in the dental arch (13.5%). CONCLUSION: The status of premature loss of primary teeth was high in the study group. Implementation of efficient educational and preventive programs to promote oral health would help children maintain a healthy primary dentition and eventually prevent the disturbances in the future development of normal occlusion. Early detection and management of the space problems associated with the early loss of primary teeth would help in reducing malocclusion problems.

A proposed core curriculum for dental English education in Japan.

BACKGROUND: Globalization of the professions has become a necessity among schools and universities across the world. It has affected the medical and dental professions in terms of curriculum design and student and patient needs. In Japan, where medicine and dentistry are taught mainly in the Japanese language, profession-based courses in English, known as Medical English and Dental English, have been integrated into the existing curriculum among its 83 medical and 29 dental schools. Unfortunately, there is neither a core curriculum nor a model syllabus for these courses. METHODS: This report is based on a survey, two discussion forums, a workshop, and finally, the drafting of a proposed core curriculum for dental English approved by consensus of the participants from each university. RESULTS: The core curriculum covers the theoretical aspects, including dental English terms and oral pathologies; and practical aspects, including blended learning and dentist-patient communication. It is divided into modules and is recommended to be offered for at least two semesters. CONCLUSIONS: The core curriculum is expected to guide curriculum developers in schools where dental English courses are yet to be offered or are still in their early development. It may also serve as a model curriculum to medical and dental schools in countries in Asia, Europe, Africa, and Central and South America, where English is not the medium of instruction.

Tempol ameliorates cardiac fibrosis in streptozotocin-induced diabetic rats: role of oxidative stress in diabetic cardiomyopathy.

Long-standing diabetes is associated with increased oxidative stress and cardiac fibrosis. This, in turn, contributes to the progression of cardiomyopathy. The present study was sought to investigate whether the free radical scavenger, 4-hydroxy-2,2,6,6-tetramethyl piperidinoxyl (tempol) can protect against diabetic cardiomyopathy and to explore the specific underlying mechanism(s) in this setting. Diabetes was induced in rats by a single intraperitoneal injection dose of streptozotocin (50 mg/kg). These animals were treated with tempol (18 mg kg(-1) day(-1), orally) for 8 weeks. Our results showed significant increases in collagen IV and fibronectin protein levels and a marked decrease in matrix metalloproteinase-2 (MMP-2) activity measured by gelatin-gel zymography alongside elevated cardiac transforming growth factor (TGF)-ß level determined using ELISA or immunohistochemistry in cardiac tissues of diabetic rats compared with control. This was accompanied by an increased in the oxidative stress as evidenced by increased reactive oxygen species (ROS) production and decreased antioxidant enzyme capacity along with elevated lactate dehydrogenase (LDH) and creatine kinase (CK-MB) serum levels as compared with the control. Tempol treatment significantly corrected the changes in the cardiac extracellular matrix, TGF-ß, ROS or serum LDH, CK-MB levels, and normalized MMP-2 activity along with preservation of cardiac tissues integrity of diabetic rats against damaging responses. Moreover, tempol normalized the elevated systolic blood pressure and improved some cardiac functions in diabetic rats. Collectively, our data suggest a potential protective role of tempol against diabetes-associated cardiac fibrosis in rats via reducing oxidative stress and extracellular matrix remodeling.

Undergraduate dental English education in Japanese dental schools.

Dental schools in Japan are among many worldwide whose medium of instruction is not in English. With advances in science, technology, and communication, the demand for the globalization of professions increases. At present, dental schools in Asia, the Middle East, and Europe have started revising their dental curricula to either include English courses for dentistry or offer a full English dental curriculum. In Japan, dental English courses started to be introduced into curricula in the early 1990s. However, a survey conducted in 1999 found that English courses were not offered in Japan's twenty-nine dental schools and there was no consensus as to what such courses should include or when and how they should be taught. Ten years after that survey, the survey results reported in this article found that the problems reported in the 1999 survey still exist. Additionally, there are still differences among schools offering English courses in terms of the timing and contents of the courses. Since teachers and school officials will have an important role in curriculum development, this article recommends that a fact-finding meeting with educators, school, and education officials be initiated to discuss, develop, and implement a core curriculum for these dental English courses.

Postural stability and occlusal status among Japanese elderly.

BACKGROUND: There are still no data available on the relationship between postural stability and occlusal status among the elderly. OBJECTIVES: To examine relationships between postural stability and occlusal status through a cohort study among elderly Japanese. METHOD: Oral examination, occlusal status, postural stability and a questionnaire were conducted and given to 87 community-dwelling Japanese at enrolment. RESULTS: The average occlusal pressure of the female group was statistically higher than the male group while average occlusal pressure and postural stability length were lesser in the group with more remaining teeth. Postural stability area and number of remaining teeth showed statistically significant correlations. Postural stability length was lesser in the group with strong occlusal force. Furthermore, the number of decayed teeth was fewer in the good hygiene group. CONCLUSIONS: This study identified a close relationship between occlusal status and postural stability of Japanese older individuals. Occlusal hypofunction was observed more in those with occlusal problems, and a decrease in their occlusal functions resulted in postural instability.

Synthesis, structural, thermal studies and biological activity of a tridentate Schiff base ligand and their transition metal complexes.

Schiff base (L) ligand is prepared via condensation of pyridine-2,6-dicarboxaldehyde with -2-aminopyridine. The ligand and its metal complexes are characterized based on elemental analysis, mass, IR, solid reflectance, magnetic moment, molar conductance, and thermal analyses (TG, DTG and DTA). The molar conductance reveals that all the metal chelates are non-electrolytes. IR spectra shows that L ligand behaves as neutral tridentate ligand and bind to the metal ions via the two azomethine N and pyridine N. From the magnetic and solid reflectance spectra, it is found that the geometrical structures of these complexes are octahedral (Cr(III), Fe(III), Co(II), Ni(II), Cu(II), and Th(IV)) and tetrahedral (Mn(II), Cd(II), Zn(II), and UO2(II)). The thermal behaviour of these chelates shows that the hydrated complexes losses water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters, such as, E*, ΔH*, ΔS* and ΔG* are calculated from the DTG curves using Coats-Redfern method. The synthesized ligand, in comparison to their metal complexes also was screened for its antibacterial activity against bacterial species, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus pyogones and Fungi (Candida). The activity data shows that the metal complexes to be more potent/antibacterial than the parent Schiff base ligand against one or more bacterial species.

Synthesis, spectroscopic, thermal and biological activity studies on triazine metal complexes.

The coordination behaviour of the triazine ligand with NNO donation sites, derived from 3-benzyl-7-hydrazinyl-4H-[1,3,4]thiadiazolo[2,3c][1,2,4]triazin-4-one (HL), towards some metal ions namely Mn(II), Fe(III), Co(II), Ni(II), Cu(II) and Zn(II) are reported. The metal complexes are characterized based on elemental analyses, IR, (1)H NMR, solid reflectance, magnetic moment, molar conductance and thermal analyses (TG, DTG and DTA). The ionization constants of the organic ligand under investigation as well as the stability constants of its metal chelates are calculated spectrophotometrically at 25°C. The chelates are found to have octahedral geometrical structures. The ligand (HL) and its binary chelates are subjected to thermal analyses (TG, DTG and DTA) and the different activation thermodynamic parameters are calculated from their corresponding DTG curves to throw more light on the nature of changes accompanying the thermal decomposition process of these compounds. The synthesized ligand and its metal complexes were found to have biological activity against the desert locust Schistocerca gregaria (Forsk.) (Orthoptera - Acrididae) and its adult longevities.

Preparation, characterization and biological activity of novel metal-NNNN donor Schiff base complexes.

Novel Schiff base (H(2)L) ligand is prepared via condensation of benzil and triethylenetetraamine. The ligand is characterized based on elemental analysis, mass, IR and (1)H NMR spectra. Metal complexes are reported and characterized based on elemental analyses, IR, (1)H NMR, solid reflectance, magnetic moment, molar conductance, and thermal analyses (TG, DTG and DTA). 1:1 [M]:[H(2)L] complexes are found from the elemental analyses data having the formulae [M(H(2)L)Cl(2)]xyH(2)O (M=Mn(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II)), [Fe(H(2)L)Cl(2)]ClxH(2)O, [Th(H(2)L)Cl(2)]Cl(2)x3H(2)O and [UO(2)(H(2)L)](CH(3)COO)(2)x2H(2)O. The metal chelates are found to be non-electrolytes except Fe(III), Th(IV) and UO(2)(II) complexes are electrolytes. IR spectra show that H(2)L is coordinated to the metal ions in a neutral tetradentate manner with 4Ns donor sites of the two azomethine N and two NH groups. The geometrical structures of these complexes are found to be octahedral. The thermal behaviour of these chelates is studied where the hydrated complexes lose water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters are calculated using Coats-Redfern method. The ligand (H(2)L), in comparison to its metal complexes, is screened for its antibacterial activity. The activity data show that the metal complexes have antibacterial activity more than the parent Schiff base ligand and cefepime standard against one or more bacterial species.

Biological activity studies on metal complexes of novel tridentate Schiff base ligand. Spectroscopic and thermal characterization.

Metal complexes of novel Schiff base (HL) ligand, prepared via condensation of 4-aminoantipyrine and 2-aminophenol, are prepared. The ligand is characterized based on elemental analysis, mass, IR and (1)H NMR spectra. Metal complexes are reported and characterized based on elemental analyses, IR, (1)H NMR, solid reflectance, magnetic moment, molar conductance, ESR spectra and thermal analyses (TG, DTG and DTA). From the elemental analyses, 1:1 [M]:[ligand] complexes are prepared with the general formulae [M(L)Cl(H(2)O)(2)] x yH(2)O (M = Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II), y = 3-4), [Fe(L)Cl(2)(H(2)O)] x 3 H(2)O and [Th(L)Cl(H(2)O)(2)]Cl(2) x 3 H(2)O. The molar conductance data reveal that all the metal chelates are non-electrolytes (except Th(IV) complex, it is 2:1 electrolyte). IR spectra show that HL is coordinated to the metal ions in a uninegatively tridentate manner with NNO donor sites of the azomethine-N, amino N and deprotonated phenolic-O. From the magnetic and solid reflectance spectra, it is found that the geometrical structures of these complexes are octahedral. The thermal behaviour of these chelates shows that the hydrated complexes losses water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters are calculated from the DTG curves using Coats-Redfern method. The synthesized ligand, in comparison to its metal complexes is screened for its antibacterial activity against bacterial species, Escherichia coli, Pseudomonas putida, Exiguobacterium acetylicum and Bacillus simplex. The activity data show that the metal complexes to be more potent/antibacterial than the parent Schiff base ligand against one or more bacterial species.

Cytoglobin is upregulated by tumour hypoxia and silenced by promoter hypermethylation in head and neck cancer.

BACKGROUND: Cytoglobin (Cygb) was first described in 2002 as an intracellular globin of unknown function. We have previously shown the downregulation of cytoglobin as a key event in a familial cancer syndrome of the upper aerodigestive tract. METHODS: Cytoglobin expression and promoter methylation were investigated in sporadic head and neck squamous cell carcinoma (HNSCC) using a cross-section of clinical samples. Additionally, the putative mechanisms of Cygb expression in cancer were explored by subjecting HNSCC cell lines to hypoxic culture conditions and 5-aza-2-deoxycitidine treatment. RESULTS: In clinically derived HNSCC samples, CYGB mRNA expression showed a striking correlation with tumour hypoxia (measured by HIF1A mRNA expression P=0.013) and consistent associations with histopathological measures of tumour aggression. CYGB expression also showed a marked negative correlation with promoter methylation (P=0.018). In the HNSCC cell lines cultured under hypoxic conditions, a trend of increasing expression of both CYGB and HIF1A with progressive hypoxia was observed. Treatment with 5-aza-2-deoxycitidine dramatically increased CYGB expression in those cell lines with greater baseline promoter methylation. CONCLUSION: We conclude that the CYGB gene is regulated by both promoter methylation and tumour hypoxia in HNSCC and that increased expression of this gene correlates with clincopathological measures of a tumour's biological aggression.

Culture-based PCR analysis of plaque samples of Japanese school children to assess the presence of six common cariogenic bacteria and its association with caries risk.

The aim of the study was to assess the presence of six common cariogenic bacteria from Cariostat-inoculated plaque samples of Japanese elementary school children through PCR analysis and check its associations with caries risk testing the validity of Cariostat as a caries risk assessment tool. This epidemiological school-based study investigated plaque samples of 399 Japanese elementary school children. Assessed using the Cariostat, 48.2% of the children had high caries risk. DNA detection of Streptococcus mutans, Streptococcus sobrinus, Streptococcus salivarius, Lactobacillus casei, Lactobacillus plantarum, Lactobacillus fermentum and both S. mutans and S. sobrinus was seen in 65.2%, 24.1%, 69.7%, 17.5%, 7.8%, 19.3%, and 17.3% of the participants, respectively. Except for S. salivarius, the presence of all other investigated bacteria resulted in a statistically significant increase among the proportion of subjects with high caries risk. Caries risk assessed using Cariostat was significantly influenced by the presence of cariogenic bacteria. Being a selective medium for cariogenic bacteria, the Cariostat can be a useful and direct source of cariogenic bacterial DNA for PCR analysis while effectively assessing caries risk.

Spectroscopic characterization of metal complexes of novel Schiff base. Synthesis, thermal and biological activity studies.

Novel Schiff base (HL) ligand is prepared via condensation of 4-aminoantipyrine and 2-aminobenzoic acid. The ligand is characterized based on elemental analysis, mass, IR and (1)H NMR spectra. Metal complexes are reported and characterized based on elemental analyses, IR, (1)H NMR, solid reflectance, magnetic moment, molar conductance and thermal analyses (TGA, DrTGA and DTA). The molar conductance data reveal that all the metal chelates are non-electrolytes. IR spectra show that HL is coordinated to the metal ions in a uninegatively tridentate manner with NNO donor sites of the azomethine N, amino N and deprotonated caroxylic-O. From the magnetic and solid reflectance spectra, it is found that the geometrical structures of these complexes are octahedral. The thermal behaviour of these chelates shows that the hydrated complexes losses water molecules of hydration in the first step followed immediately by decomposition of the anions and ligand molecules in the subsequent steps. The activation thermodynamic parameters, such as, E*, DeltaH*, DeltaS* and DeltaG* are calculated from the DrTG curves using Coats-Redfern method. The synthesized ligands, in comparison to their metal complexes also were screened for their antibacterial activity against bacterial species, Escherichia Coli, Pseudomonas aeruginosa, Staphylococcus Pyogones and Fungi (Candida). The activity data show that the metal complexes to be more potent/antibacterial than the parent Shciff base ligand against one or more bacterial species.

Effect of host medium on the fluorescence emission intensity of rhodamine B in liquid and solid phase.

In this work, we study the effect of concentration, host medium, PH and phase states on the fluorescence emission from the laser dye Rhodamine B pumped by UV laser as exited source. The polymethylmethacrylate PMMA is used as a host medium in case of solid phase samples while, ethanol and Tetrahydrofuran (THF) are used in case of a liquid one. Laser Induced Fluorescence (LIF) technique was used to study the fluorescence properties of both cases of liquid and thin film solid-state samples. In addition, the Dual Thermal Lens (DTL) technique was used to study the quantum yield of these samples. The concentrations of Rhodamine B in ethanol as solvent between 2 x 10(-2) M and 5 x 10(-6) M were studied. The maximum fluorescence emission is observed at concentration of Rhodamine B C = 3 x 10(-4) M. Comparison studies were investigated for different host medium such as ethanol, THF, PMMA in liquid phase state and PMMA in solid phase state. The measurements revealed that, the behavior of both phases state was analogous. Rhodamine B/PMMA thin film sample by ratio of 4:1 and thickness 0.12 mm was found to have the best photostability sample with a quantum yield about approximately 0.82.

Mutation-, aging-, and gene dosage-dependent accumulation of neuroserpin (G392E) in endoplasmic reticula and lysosomes of neurons in transgenic mice.

Mutations in human neuroserpin gene cause an autosomal dementia, familial encephalopathy with neuroserpin inclusion bodies (FENIB). We generated and analyzed transgenic mice expressing high levels of either FENIB-type (G392E) or wild-type human neuroserpin in neurons of the central nervous system. G392E neuroserpin accumulated age-dependently in neurons of the neocortex, thalamus, amygdala, pons, and spinal cord of homozygous transgenic mice. Such accumulations were not observed in hemizygous transgenic mice nor in transgenic mice for wild-type neuroserpin. In differential centrifugation of brain homogenates, G392E neuroserpin recovered in the nucleus-rich fraction dramatically increased along with aging, suggesting that the aggregations gradually increase their densities presumably by their conversion into heavier and more compact configurations. In immunoelectron microscopical analyses, immunopositivities for G392E neuroserpin were found not only in endoplasmic reticulum but also in lysosomes. G392E neuroserpin transgenic mice were much more susceptible to seizures induced by kainate administration than nontransgenic mice. Overall, G392E neuroserpin accumulated in the central nervous system neurons of transgenic mice in mutation-, aging-, and gene dosage-dependent manners. The established transgenic mice will be valuable to elucidate not only mechanisms for the formation of G392E neuroserpin aggregations but also pathways for the degradation and/or clearance of the already formed aggregations in neurons.