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1.
Chinese Journal of Biotechnology ; (12): 2126-2140, 2023.
Article in Chinese | WPRIM | ID: wpr-981194

ABSTRACT

ω-transaminase (ω-TA) is a natural biocatalyst that has good application potential in the synthesis of chiral amines. However, the poor stability and low activity of ω-TA in the process of catalyzing unnatural substrates greatly hampers its application. To overcome these shortcomings, the thermostability of (R)-ω-TA (AtTA) from Aspergillus terreus was engineered by combining molecular dynamics simulation assisted computer-aided design with random and combinatorial mutation. An optimal mutant AtTA-E104D/A246V/R266Q (M3) with synchronously enhanced thermostability and activity was obtained. Compared with the wild- type (WT) enzyme, the half-life t1/2 (35 ℃) of M3 was prolonged by 4.8-time (from 17.8 min to 102.7 min), and the half deactivation temperature (T1050) was increased from 38.1 ℃ to 40.3 ℃. The catalytic efficiencies toward pyruvate and 1-(R)-phenylethylamine of M3 were 1.59- and 1.56-fold that of WT. Molecular dynamics simulation and molecular docking showed that the reinforced stability of α-helix caused by the increase of hydrogen bond and hydrophobic interaction in molecules was the main reason for the improvement of enzyme thermostability. The enhanced hydrogen bond of substrate with surrounding amino acid residues and the enlarged substrate binding pocket contributed to the increased catalytic efficiency of M3. Substrate spectrum analysis revealed that the catalytic performance of M3 on 11 aromatic ketones were higher than that of WT, which further showed the application potential of M3 in the synthesis of chiral amines.


Subject(s)
Transaminases/chemistry , Molecular Docking Simulation , Amines/chemistry , Pyruvic Acid/metabolism , Enzyme Stability
2.
Journal of Zhejiang University. Science. B ; (12): 218-233, 2020.
Article in English | WPRIM | ID: wpr-1010529

ABSTRACT

Metastasis is one of the main reasons causing death in cancer patients. It was reported that chemotherapy might induce metastasis. In order to uncover the mechanism of chemotherapy-induced metastasis and find solutions to inhibit treatment-induced metastasis, the relationship between epithelial-mesenchymal transition (EMT) and doxorubicin (DOX) treatment was investigated and a redox-sensitive small interfering RNA (siRNA) delivery system was designed. DOX-related reactive oxygen species (ROS) were found to be responsible for the invasiveness of tumor cells in vitro, causing enhanced EMT and cytoskeleton reconstruction regulated by Ras-related C3 botulinum toxin substrate 1 (RAC1). In order to decrease RAC1, a redox-sensitive glycolipid drug delivery system (chitosan-ss-stearylamine conjugate (CSO-ss-SA)) was designed to carry siRNA, forming a gene delivery system (CSO-ss-SA/siRNA) downregulating RAC1. CSO-ss-SA/siRNA exhibited an enhanced redox sensitivity compared to nonresponsive complexes in 10 mmol/L glutathione (GSH) and showed a significant safety. CSO-ss-SA/siRNA could effectively transmit siRNA into tumor cells, reducing the expression of RAC1 protein by 38.2% and decreasing the number of tumor-induced invasion cells by 42.5%. When combined with DOX, CSO-ss-SA/siRNA remarkably inhibited the chemotherapy-induced EMT in vivo and enhanced therapeutic efficiency. The present study indicates that RAC1 protein is a key regulator of chemotherapy-induced EMT and CSO-ss-SA/siRNA silencing RAC1 could efficiently decrease the tumor metastasis risk after chemotherapy.


Subject(s)
Female , Humans , Amines/chemistry , Antineoplastic Agents/adverse effects , Breast Neoplasms/pathology , Chitosan/chemistry , Doxorubicin/adverse effects , Drug Delivery Systems , Epithelial-Mesenchymal Transition/drug effects , MCF-7 Cells , Neoplasm Metastasis/prevention & control , Oxidation-Reduction , RNA, Small Interfering/administration & dosage , Reactive Oxygen Species/metabolism , rac1 GTP-Binding Protein/physiology
3.
Braz. dent. j ; 28(6): 744-748, Nov.-Dec. 2017. tab
Article in English | LILACS | ID: biblio-888705

ABSTRACT

Abstract To examine the effect of the alternative coinitiator 4,4'bis dimethylamino benzydrol (BZN) in degree of conversion (DC), mechanical and biological properties of experimental composites. The coinitiator BZN was used in three concentrations (0.2, 0.5 and 1.2%), and the coinitiator DMAEMA was used as control at the same concentrations as above. The molar concentration of camphorquinone (CQ) and coinitiators was kept constant (1:1). The composites were manipulated and submitted to microhardness test (VHN), flexural and compressive strength (in MPa), elastic modulus (GPa), DC (FT-IR) and in vitro cytotoxicity (against 3T3 fibroblastic cells) of the experimental resins. Data were subjected to two-way ANOVA and Tukey post-test (α=0.05). The experimental composite resin with BZN showed higher DC values compared to control DMAEMA groups. For the mechanical properties, microhardness values were higher in BZN groups; flexural strength and elastic modulus were similar between all the groups. Compressive strength for groups BZN0.5 and DMAEMA0.5 were not statistically different, being the lowest values attributed to group BZN0.2. The experimental resins with BZN and DMAEMA were considered nontoxic against 3T3 fibroblasts. The inclusion of the coinitiator BZN in experimental composites was considered nontoxic against 3T3 fibroblast cells, without compromising DC and mechanical properties.


Resumo Analisar o efeito do co-iniciador alternativo 4,4'bisdimetilaminobenzidrol (BZN) no grau de conversão (GC) e nas propriedades mecânicas e biológicas de resinas compostas experimentais. O co-iniciador BZN foi utilizado em três concentrações (0,2, 0,5 e 1,2), e o co-iniciador DMAEMA como controle, nas mesmas concentrações acima. A concentração molar entre canforoquinona (CQ) e os co-iniciadores foi mantida constante (1:1). As resinas compostas foram manipuladas e submetidas aos testes de microdureza (VHN), resistência à compressão e flexural (em MPa), módulo de elasticidade (em GPa), GC (em %, por meio de espectroscopia micro-Raman e FTIR com KBr), citotoxicidade in vitro (frente às células fibroblásticas 3T3) das resinas experimentais. Os resultados foram submetidos ao teste ANOVA 1 fator e pós-teste de Tukey (α=0,05). As resinas compostas experimentais com o BZN apresentaram GC e propriedades mecânicas satisfatórias, além de serem consideradas atóxicas a fibroblastos 3T3. A inclusão do co-iniciador BZN à resina composta foi considerada não tóxica frente a células fibroblásticas 3T3 e sem comprometer o grau de conversão e as propriedades mecânicas da mesma.


Subject(s)
Animals , Mice , Amines/chemistry , Composite Resins , Materials Testing , 3T3 Cells
4.
Braz. dent. j ; 28(6): 726-730, Nov.-Dec. 2017. tab
Article in English | LILACS | ID: biblio-888710

ABSTRACT

Abstract The aim in this study was to evaluate the influence of different ratio of camphorquinone/tertiary amine concentration on the flexural strength (FS), elastic modulus (EM), degree of conversion (DC), yellowing (YL), water sorption (WS) and water solubility (WSL) of experimental composites. Thus, acrylate blends were prepared with different camphorquinone (CQ) and amine (DABE) concentrations and ratios by weight: (CQ/DABE%): 0.4/0.4% (C1), 0.4/0.8% (C2), 0.6/0.6% (C3), 0.6/1.2% (C4), 0.8/0.8% (C5), 0.8/1.6% (C6), 1.0/1.0% (C7), 1.0/2.0% (C8), 1.5/1.5% (C9), 1.5/3.0% (C10). For the FS and EM, rectangular specimens (7x2x1 mm, n=10) were photo-activated by single-peak LED for 20 s and tested at Instron (0.5 mm/min). Then, the same specimens were evaluated by FTIR for DC measurement. For YL, disks (5x2 mm, n=10) were prepared, light-cured for 20 s and evaluated in spectrophotometer using the b aspect of the CIEL*a*b* system. For WS and WSL, the volume of the samples was calculated (mm³). For WS and WSL, composites disks (5x0.5 mm, n=5) were prepared. After desiccation, the specimens were stored in distilled water for 7 days and again desiccated, in order to measure the WS and WSL. Data were submitted to one-way ANOVA and Tukey's test (5%). The groups C8, C9 and C10 showed higher DC, EM and YL means, compared to other composites. Therefore, the FS and WS values were similar among all groups. Also, C1, C2 and C3 presented higher WSL in 7 days, compared to other composites. In general, higher concentrations of camphorquinone promoted higher physical-mechanical properties; however, inducing higher yellowing effect for the experimental composites


Resumo O objetivo foi avaliar a influência da concentração e proporção de canforoquinona (CQ)/amina terciária (DABE) na resistência à flexão (RF), módulo flexural (MF), grau de conversão (GC), amarelamento (AM), sorpção (SA) e solubilidade em água (SL) de compósitos experimentais. Blendas acrilatas foram preparadas com diferentes concentrações e proporções de CQ/DABE em peso, como segue: (CQ/DABE%): 0,4/0,4% (C1); 0,4/0,8% (C2); 0,6/0,6% (C3); 0,6/1,2% (C4); 0,8/0,8% (C5); 0,8/1,6% (C6); 1,0/1,0% (C7); 1,0/2,0% (C8); 1,5/1,5% (C9); 1,5/3,0% (C10). Para RF e MF, espécimes retangulares (7x2x1 mm, n=10) foram fotoativados com LED de pico único (Radii Cal) por 20 s e testados em máquina Instron (0,5 mm/min). Após, o GC dos mesmos espécimes (fragmentos) foi mensurado por FTIR. Para AM, discos de compósito (5x2 mm, n=10) foram preparados, fotoativados por 20 s e imediatamente avaliados em espectrofotômetro, considerando o aspecto b do sistema CIEL*a*b*. Para SA e SL, discos de compósito (5x0,5 mm, n=5) foram preparados e seus volumes calculados (mm³). Após desidratação, as amostras foram pesadas e armazenadas em água destilada por 7 dias, pesadas e novamente desidratadas e pesadas, para se calcular o SA e SL. Os dados foram submetidos a one-way ANOVA e teste de Tukey (5%). Os grupos C8, C9 e C10 mostraram maior GC, MF e AM, comparado aos outros grupos. No entanto, RF e SA foram similares entre todos os grupos. Ainda, C1, C2 e C3 apresentaram maior SL em 7 dias comparado aos outros grupos. Em geral, maiores concentrações de CQ promoveram melhores propriedades físico-mecânicas; no entanto, levaram ao maior amarelamento dos compósitos.


Subject(s)
Humans , Composite Resins , Light , Amines/chemistry , Camphor/analogs & derivatives , Camphor/chemistry , Color , Solubility , Water/chemistry
5.
São Paulo; s.n; 2016. 115 p.
Thesis in Portuguese | LILACS | ID: biblio-868246

ABSTRACT

Introdução. O alto consumo de carne, principalmente vermelha e processada, tem sido relacionado com aumento de risco de doenças crônicas, especialmente o câncer. Uma das explicações possíveis são os métodos de preparo culinário a altas temperaturas, que acarretam na formação aminas heterocíclicas. Estes compostos são detoxificados no nosso organismo, passando por um processo, no qual podem ser geradas espécies reativas, relacionadas ao estresse oxidativo e ao dano ao DNA. Entretanto, os indivíduos apresentam respostas diferentes à mesma exposição dietética, podendo ter diferentes níveis de risco ou benefício com a mesma ingestão de alimentos. O código genético individual pode ser uma das causas dessa variação interpessoal. Objetivo. Investigar a relação entre o consumo de carnes e aminas heterocíclicas com estresse oxidativo e dano no DNA, considerando polimorfismos genéticos, fatores demográficos e de estilo de vida em residentes do Município de São Paulo. Métodos. Foram utilizados dados dietéticos, genéticos, bioquímicos e estilo de vida de um estudo transversal com amostra probabilística de múltiplo estágio chamado Inquérito de Saúde de São Paulo (ISACapital). Os dados de carne e aminas heterocíclicas foram obtidos a partir de um recordatório alimentar de 24 horas e questionário sobre métodos de cocção e graus de cozimento das carnes. A extração do DNA ocorreu pelo método por sal e utilizou-se a técnica PCR em tempo real para determinação dos seguintes polimorfismos de nucleotídeo único: CYP1A1 (rs1048943), CYP1A2 (rs762551, rs35694136), CYP1B1 (rs1056836, rs10012), NAT2 (rs1208, rs1041983, rs1799929, rs1801280, rs1799931, rs1799930, rs1801279), NAT1 (rs4986782, rs5030839, rs56379106, rs56318881, rs6586714), SULT1A1 (rs928286), UGT1A9 (rs3832043), SOD2 (rs4880), CAT (rs7943316), GSTA1 (rs3957357), GSTP1 (rs1695), e deleção dos genes GSTM1 e GSTT1. Foram utilizados os biomarcadores malonaldeído (MDA) no plasma para estimar o estresse oxidativo e o 8-OHdG no plasma para estimar dano ao DNA. As associações foram examinadas por meio de modelos de regressão múltipla linear e logística ajustadas por sexo, idade, IMC, consumo de frutas e calorias, atividade física e fumo. Resultados. O consumo médio de aminas heterocíclicas foi de 437ng/dia e a carne de boi foi a que mais contribuiu para o consumo de aminas. Participantes que consumiram carne de boi grelhada muito bem passada apresentaram maiores concentrações de MDA do que os demais. Encontrou-se associação positiva entre consumo de aminas heterocíclicas com estresse oxidativo e dano ao DNA, isto é, indivíduos que consumiram maiores teores de aminas heterocíclicas apresentaram maiores chances de ter elevados concentrações de MDA (OR=1,17; P=0,04) e maiores concentrações de 8-OHdG (=1,62; P=0,04). Observou-se também que esta associação pode ser modificada pelas características genéticas individuais, sendo que polimorfismos nos genes das enzimas de detoxificação NAT2 e CYP1B1 interagiram com o consumo de aminas, diminuindo o estresse oxidativo. Conclusão. Verificou-se que o alto consumo de aminas heterocíclicas contribuiu para maiores níveis de estresse oxidativo e dano ao DNA independente de fatores demográficos e de estilo de vida, aumentando o risco de doenças crônicas. Observou-se também que esta relação pode ser alterada na presença de polimorfismos genéticos individuais


Introduction. The excessive meat intake, especially red and processed meat, has been linked to chronic diseases, especially cancer. One of the reasons for that is the cooking process at high temperatures that can form heterocyclic amines (HCA). During HCA metabolism, reactive species can be formed, which can cause oxidative stress and DNA damage. However, people can show different answers to the same food intake, increasing or decreasing the risk of diseases. The DNA code can be one of the causes of this between-person variations. Objective. To investigate the association between meat/heterocyclic amine intake with oxidative stress and DNA damage, considering polymorphism, demographic and life style factors among population of São Paulo city. Methods. Information on food intake, genetics, biochemical, and lifestyle was obtained from a representative, multistage probability-based cross-sectional study titled Health Survey for Sao Paulo (ISA-Capital). Meat and heterocyclic amine intake was estimated by a 24-hour dietary recall complemented by a detailed questionnaire with preferences of cooking methods and level of doneness for meats. The salt method was used for DNA extraction and real time PCR to identify the following single nucleotide polymorphisms: CYP1A1 (rs1048943), CYP1A2 (rs762551, rs35694136), CYP1B1 (rs1056836, rs10012), NAT2 (rs1208, rs1041983, rs1799929, rs1801280, rs1799931, rs1799930, rs1801279), NAT1 (rs4986782, rs5030839, rs56379106, rs56318881, rs6586714), SULT1A1 (rs928286), UGT1A9 (rs3832043), SOD2 (rs4880), CAT (rs7943316), GSTA1 (rs3957357), GSTP1 (rs1695), GSTM1 and GSTT1 (null or not). We used malondialdehyde (MDA) concentration in plasma to estimated oxidative stress, and 8-OHdG concentration in plasma to estimate DNA damage. Analyses were performed using multivariate logistic and linear regressions adjusted for smoking, sex, age, body mass index, energy intake, fruit intake, smoking and physical activity. Results. Mean HCA intake was 437ng/day and beef was the meat that contributed more to HCA. Participants who consumed grilled beef very well-done presented more MDA concentration than other participants. We found significant association between heterocyclic amine intake with oxidative stress and DNA damage. Participants who consumed high levels of heterocyclic amines showed higher odds to show high MDA concentration (OR=1.17; P=0.04) and high 8-OHdG concentration (=1.62; P=0.04). These associations could be modified by individual genetic characteristics. Polymorphisms in genes that codify NAT2 and CYP1B1 detoxification enzymes interacted with HCA intake, decreasing oxidative stress. Conclusions. The high heterocyclic amine intake contributed to increase oxidative stress independently of lifestyle and demographic factors, increasing risk of chronic diseases. These relationships can be modified by genetic polymorphisms


Subject(s)
Amines/chemistry , DNA Adducts , Eating , Meat/statistics & numerical data , Oxidative Stress/physiology , Cross-Sectional Studies , Statistical Data , Heterocyclic Compounds/chemistry , Life Style , Polymorphism, Genetic , Risk Factors
6.
Rev. chil. pediatr ; 86(4): 251-256, ago. 2015. tab
Article in Spanish | LILACS | ID: lil-764081

ABSTRACT

Introducción: Autoconcepto es el conjunto de ideas y actitudes que se tiene acerca de sí mismo. Nuestro objetivo fue evaluar si existen diferencias en el nivel de autoconcepto de niños de 8-12 años con y sin secuelas de quemaduras, e identificar variables predictoras del autoconcepto en los niños con secuelas. Pacientes y método: Estudio comparativo, transversal de 109 niños con secuelas de quemaduras de 8 a 12 años de edad, con 109 niños sin secuelas de quemaduras, del mismo grupo de edad y nivel socioeconómico. Se utilizó la escala de autoconcepto de Piers-Harris, que entrega medida de autoconcepto general y dimensiones: conductual, estatus intelectual y escolar, apariencia y atributos físicos, ansiedad, popularidad, felicidad y satisfacción. Resultados: No hubo diferencias significativas en el nivel de autoconcepto general ni en sus dimensiones al comparar ambos grupos (p > 0,05). Dentro del grupo con secuelas de quemaduras la variable número de secuelas resultó ser un factor protector para las dimensiones ansiedad, popularidad, felicidad-satisfacción y autoconcepto general. La variable localización surgió como factor de riesgo para la dimensión conductual. Discusión: La ausencia de diferencias en autoconcepto entre niños con secuelas de quemaduras y sin ellas es similar a lo reportado por la literatura. El hallazgo en factores de riesgo y protectores motiva a continuar investigando, incorporando antecedentes premórbidos y familiares.


Introduction: Self-concept is the set of ideas and attitudes that a person has about him/herself. Objective: To evaluate whether there are differences in the level of self-concept in children 8-12 years old with and without burns sequelae. To identify predictive variables of self-concept in children with sequelae. Patients and method: A comparative cross-sectional study of self-concept in 109 children with burns sequelae, from 8 to 12 years old, with 109 children without burns sequelae, and of the same age and socioeconomic status. The Piers-Harris self-concept scale is used, which provides a general measurement of self-concept and behavioural, intellectual and school status, appearance, and physical attributes, anxiety, popularity, happiness and satisfaction dimensions. Results: There were no significant differences in the level of general self-concept or their dimensions (P > .05). In the group with burns sequelae, the protective factor was the variable number of sequels was associated with the dimensions of anxiety, popularity, happiness-satisfaction and general self-concept. The location variable emerged as a risk factor for the behavioural dimension. Discussion: The absence of differences in self-concept between children with burns sequelae and children without them is similar to that reported in the literature. The finding in the risk and protective factors encourages to further research, and perhaps incorporating pre-morbidity and family background.


Subject(s)
Humans , DNA , Quaternary Ammonium Compounds/chemistry , Serine/chemistry , Surface-Active Agents/chemistry , Amides/chemistry , Amines/chemistry , Cell Line, Tumor , Chemistry, Pharmaceutical/methods , Esters/chemistry , Gene Transfer Techniques , Genetic Therapy/methods , HeLa Cells , Lipids/chemistry , Transfection/methods
7.
Electron. j. biotechnol ; 16(3): 4-4, May 2013. ilus, tab
Article in English | LILACS | ID: lil-684002

ABSTRACT

Background: New enzymes for biotransformations can be obtained by different approaches including directed mutagenesis and in vitro evolution. These mutants have to be efficiently produced for laboratory research on bioreactions as well as for process development. In the framework of a European ERA-IB project, two different types of enzymes (ammonia lyases and aminotransferases) have been selected as biocatalysts for the synthesis of industrially relevant amines. New mutant enzymes have been obtained: a) aspartases able to recognize β-amino acids; b) ω-transaminases with improved activity. The objectives are to find out a common operational strategy applicable to different mutants expressed in E. coli with the same initial genetic background, the development of an integrated process for production and the preparation of stable useful biocatalysts. Results: Mutant enzymes were expressed in E. coli BL21 under the control of isopropylthiogalactoside (IPTG) inducible promoter. The microorganisms were grown in a formulated defined medium and a high-cell density culture process was set up. Fed-batch operation at constant specific growth rate, employing an exponential addition profile allowed high biomass concentrations. The same operational strategy was applied for different mutants of both aspartase and transaminase enzymes, and the results have shown a common area of satisfactory operation for maximum production at low inducer concentration, around 2 μmol IPTG/g DCW. The operational strategy was validated with new mutants and high-cell density cultures were performed for efficient production. Suitable biocatalysts were prepared after recovery of the enzymes. The obtained aspartase was immobilized by covalent attachment on MANA-agarose, while ω-transaminase biocatalysts were prepared by entrapping whole cells and partially purified enzyme onto Lentikats (polyvinyl alcohol gel lens-shaped particles). Conclusions: The possibility of expressing different mutant enzymes under similar operation conditions has been demonstrated. The process was standardized for production of new aspartases with β-amino acid selectivity and new ω-transaminases with improved substrate acceptance. A whole process including production, cell disruption and partial purification was set up. The partially purified enzymes were immobilized and employed as stable biocatalysts in the synthesis of chiral amines.


Subject(s)
Amines/metabolism , Transaminases/metabolism , Ammonia-Lyases/metabolism , Bioreactors , Culture Media , Enzymes, Immobilized , Escherichia coli , Biocatalysis , Batch Cell Culture Techniques , Amines/chemistry , Transaminases/genetics , Transaminases/chemistry , Ammonia-Lyases/genetics , Ammonia-Lyases/chemistry , Mutation
8.
Indian J Biochem Biophys ; 2013 Feb; 50(1): 72-79
Article in English | IMSEAR | ID: sea-147289

ABSTRACT

A quantitative structure-activity relationship (QSAR) and molecular modeling study were performed on a series of 3,4-dihyro-1-isoquinolinamines and thienopyridines reported by Beaton et al. [Beaton et al. (2001) Bioorg Med Chem Lett 11, 1023-1026, 1027-1030] as potent, highly selective inhibitors of two isoforms of nitric oxide synthase (NOS) — neuronal NOS (nNOS) and endothelial NOS (eNOS), in order to find the physicochemical properties that governed their activity and the mode of interaction with the receptors, so that still more potent compounds in the series could be suggested. A multiple regression analysis revealed that nNOS and eNOS inhibition potency of these compounds could be controlled by their hydrophobic property and molar refractivity, respectively. Thus, nNOS and eNOS inhibition was indicated to involve the hydrophobic interaction and steric effects, respectively, suggesting some structural differences of the two isoforms of NOS. Based on the correlations obtained, some new, more potent compounds belonging to the series were predicted. These compounds were then docked into the receptors to see their interactions and find out the docking scores. The docked structures of two representative compounds, whose interaction energies with nNOS and eNOS, respectively were found to be the lowest, were given as an example to exhibit the possible orientation of the compounds to interact with the receptors.


Subject(s)
Amines/chemistry , Computer Simulation , Models, Chemical , Models, Molecular , Nitric Oxide Synthase Type I/antagonists & inhibitors , Nitric Oxide Synthase Type I/ultrastructure , Nitric Oxide Synthase Type III/antagonists & inhibitors , Quantitative Structure-Activity Relationship , Thienopyridines/chemistry
9.
Indian J Biochem Biophys ; 1999 Dec; 36(6): 449-52
Article in English | IMSEAR | ID: sea-27598

ABSTRACT

A membrane bound oxalate oxidase from leaves of Amaranthus spionsus has been partially purified and immobilized on alkylamine glass with a yield of 9.2 mg protein/g support. The enzyme retained 99.4% of initial activity of free enzyme after immobilization. There was no change in the optimum pH (3.5) and Vmax but the temperature for maximum activity was slightly decreased (35 degrees C) and energy of activation (Ea) and Km for oxalate were increased after immobilization. The immobilized enzyme preparation was stable for 6 months, when stored in distilled water at 4 degrees C. Presence of Cl- did not affect the activity of immobilized enzyme.


Subject(s)
Adult , Amines/chemistry , Enzymes, Immobilized/chemistry , Humans , Male , Oxidoreductases/chemistry , Plant Leaves/enzymology
10.
Egyptian Journal of Chemistry. 1997; 40 (3): 167-75
in English | IMEMR | ID: emr-107810

ABSTRACT

The Proton-ligand formation constant of 1, 4, 7-triaza cycloronane hydrochloride [[H3[9] ane N3]3+, 3Cl]and the stability constants of its chelates with Mn [II], Fe [II], Fe [III] Co [II], Co [III] and Cu [II] have been determined pH-metrically in aqueous solution in the presence of 0.1 M NaNO3 at 20-32 degree. The mole fraction of different species were calculated and discussed. The thermodynamic parameters for the mono complexes under investigation were also evaluated


Subject(s)
Chelating Agents/chemistry , Amines/chemistry , Spectrophotometry/methods
11.
Egyptian Journal of Pharmaceutical Sciences. 1997; 38 (4-6): 221-231
in English | IMEMR | ID: emr-44543

ABSTRACT

Fusion of 6-bromo, 6,8-dibromo and 6-nitro-3-hydroxycoumarin with primary and secondary amines led to the formation of 3-aminocoumarin derivatives. Reaction of 3-hydroxycoumarin derivatives with hydrazine hydrate yielded 3-hydroazinocoumarin derivatives. Heating alpha- phenylhydrazino-beta-2-hydroxy-5-nitrocinnamic acid phenylhydrazide with acetic anhydride and hydrochloric acid gave 6-nitro-3-phenylhydrazinocoumarin


Subject(s)
Coumarins/chemical synthesis , Coumarins/pharmacology , Amines/chemistry , Hydrazines/chemistry
12.
Egyptian Journal of Chemistry. 1996; 39 (4): 387-93
in English | IMEMR | ID: emr-40848

ABSTRACT

Certain quinazolinones were reported to exert antimicrobial activity[1]. Consequently, in continuation of our previous work on the reaction of 3,1-benzoxazin-4-ones with amines,[2-5], 2-chloromethyl-6- iodobenzoxazin-4-one was synthesized and allowed to react with amines hoping to obtain 4-quinazolinones for evaluation as antimicrobial agents. 5-Iodoanthranilic acid was chloroacetylated to give I which was cyclodehydrated to yield the corresponding 3,1-benzoxazin-4- one II Compound II was allowed to react with different aromatic amines to produce 3-aryl-2-chloromethyl-6-iodoquinazolin-4-ones IIIa-t. Structures of compounds III [Scheme 1] were confirmed by microanalytical and spectroscopic data [Table1 and 2]


Subject(s)
Oxazines/chemistry , Amines/chemistry , Quinazolines/chemical synthesis
13.
Egyptian Journal of Chemistry. 1995; 38 (1): 113-123
in English | IMEMR | ID: emr-37104

ABSTRACT

In continuation of our previous works on the reaction of 3,1 - benzoxazin -4 - ones with amines [1,4], it has been found interesting to synthesize 6 - bromo and 6,8 - dibromo - 2 - chloro - methyl - 3, 1 - benzoxazin - 4 - ones IIa, b and to then study their reactions with a variety of amines. Accordingly, 5-bromo and 3,5-dibromoanthranilic acids were chloroacetylated to give I which were cyclodehydrated to the corresponding benzoxazinones IIa, b. Reaction of IIa, b with aromatic amines, ammonia and/or hydrazine hydrate in ethanol or dioxane produced the 2- chloromethyl -4-quinazolinones IIIa-p, presumably through the attack of the amines on the electrophilic C-2 of the benzoxazinone ring system, regardless the amount of the amine used. Structures of III were confirmed by microanalytical and spectroscopic data [table 1]. Evidence was investigated by conversion of III to the corresponding salicylate esters IV via their reaction with sodium salicylate


Subject(s)
Amines/chemistry , Oxazines/chemistry , Spectrum Analysis
14.
Egyptian Journal of Chemistry. 1995; 38 (4): 427-434
in English | IMEMR | ID: emr-37111

ABSTRACT

In our previous publication[1] the reaction of 2-cyancmethyl-3; 1-benzoxa-zin-4-one with amines was reported to afford 2-cyanomethyl- 4-quinazolines cyano group free 1,2,3,4-tetrahydro-2, 4-quinazolinediones following a decyanomethylation pathway. Consequently, it was found interesting to study the behaviour of 6-bromo-2-cyanomethyl-3, l-benzoxazin-4-one [III] towards a variety of amines


Subject(s)
Amines/chemistry , Spectrum Analysis
15.
Alexandria Journal of Pharmaceutical Sciences. 1994; 8 (3): 173-174
in English | IMEMR | ID: emr-31633

ABSTRACT

The biindone I reacted with morpholine or piperidine and formaldehyde to give the corresponding Mannich bases IIa-b. Treatment of I with formaldehyde, and formaldehyde in AcOH, afforded II and IV, respectively. Compounds V and VI were prepared by treating I with benzaniline and isatinanil, respectively. Coupling of I with benzenediazonium chloride led to the formation of VII


Subject(s)
Chemistry , Amines/chemistry , Diazonium Compounds
16.
Alexandria Journal of Pharmaceutical Sciences. 1993; 7 (2): 142-145
in English | IMEMR | ID: emr-26917
17.
Lima; s.n; 1993. 132 p. tab, graf. (3696).
Monography in Spanish | LILACS | ID: lil-187041

ABSTRACT

Se ha efectuado un estudio cualitativo, usando una serie de reacciones para el reconocimiento y diferenciacion de los distintos tipos de aminas, así como el estudio comparativo entre los métodos volumétricos para la cuantificación de aminas, aprovechando su propiedad básica y el diferente comportamiento del grupo funcional amino frente a algunos reactivos. Se usaron métodos acidimétricos, basados en la titulación de las muestras como base, propiedad que en ciertas condiciones en cuantitativa. Los resultados obtenidos muestran que los métodos basados en reacciones de acilación, son los más convenientes para ser aplicadas a todas las aminas primarias y secundarias ensayadas.


Subject(s)
Amines/analysis , Amines/chemical synthesis , Amines/chemistry , Amines/pharmacokinetics , Amines/pharmacology , Amines/toxicity
18.
Egyptian Journal of Chemistry. 1991; 34 (5): 389-99
in English | IMEMR | ID: emr-107498

ABSTRACT

The reaction kinetics of nucleophilic addition of aromatic amines to trans-3-[P-substituted phenyl]-1-phenyl prop-2-en-1-ones were studied as a function of the structural variation in both reactants. The four-parameter of the equation log kg=log ko + pe sigma + r sigma sigma + were used for dual variation which is characterized by the structural constants sigma and sigma +. This equation indicates that the resonance stabilization of the ground and transition state is the main factor that governs the relative reactivities of the nucleophiles


Subject(s)
Amines/chemistry
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