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1.
Bioorg Chem ; 116: 105406, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34628227

RESUMO

INTRODUCTION: Investigating the binding site of six novel curcumin-based diazepine compounds as a non-competitive antagonist on ionotropic, AMPA-type glutamate receptors, including homomeric and heteromeric subunits. These receptors play a pivotal role in neurodegenerative diseases such as Alzheimer's and epilepsy due to excitotoxicity. Furthermore, it appears that AMPAR signaling plays a significant role in disease development outside the nervous system, as a potential relationship between AMPAR activation and cancer development may exist. OBJECTIVES: Study the biophysical gating effects of the curcumin-based diazepine on AMPAR variants and identify CBD binding sites on AMPARs with the hopes of discovering more potent drug candidates with less undesirable side effects. METHODS: Our current study uses patch-clamp electrophysiology technology to estimate whole-cell amplitudes changes when exposing HEK293T cells expressing AMPAR subunits to different curcumin-based diazepines. RESULTS: The non-competitive antagonist curcumin-based compounds successfully reduced AMPAR activation currents and increased the rate of desensitization and deactivation. CBD-4 and CBD-5 show the most significant impact on AMPARs, reducing the current by 7-fold. The results contrast with those obtained by the halogenated benzodiazepine-fused curcumins reported previously and lake pyrimidine and pyrazine moieties. This indicates that the N's presence in the effused rings plays a significant role in binding to receptors. CBD-4 showed the highest effect on GluA2 subunits in receptors, while CBD-5 most dramatically impacting GluA1 homomeric receptors, demonstrating that the compounds are more selective towards AMPA-type glutamate receptors. The compounds also showed significant cytotoxic activities against breast cancer cell line (MCF-7), with CBD-4 having the most significant impact. CONCLUSION: Curcumin-based compounds (i.e., CBD-4 and CBD-5) yield significant neurodegenerative drug potential, and it creates a novel structure with significant activities in reducing AMPAR excitation compared to traditional benzodiazepine analogs, yet their binding mechanisms are still not fully understood. Moreover, AMPARs appear to have a potential influence on cancer development, and the curcumin-based compounds might provide insight into the nature of this relationship.


Assuntos
Azepinas/farmacologia , Curcumina/farmacologia , Receptores de AMPA/antagonistas & inibidores , Azepinas/síntese química , Azepinas/química , Curcumina/síntese química , Curcumina/química , Relação Dose-Resposta a Droga , Células HEK293 , Humanos , Estrutura Molecular , Receptores de AMPA/metabolismo , Transdução de Sinais/efeitos dos fármacos , Relação Estrutura-Atividade
2.
Int J Mol Sci ; 22(11)2021 Jun 04.
Artigo em Inglês | MEDLINE | ID: mdl-34200114

RESUMO

The goal of this work was to develop polymer-based heterocycle for water purification from toxic pesticides such as difenoconazole. The polymer chosen for this purpose was cellulose nanocrystalline (CNC); two cellulose based heterocycles were prepared by crosslinking with 2,6-pyridine dicarbonyl dichloride (Cell-X), and derivatizing with 2-furan carbonyl chloride (Cell-D). The synthesized cellulose-based heterocycles were characterized by SEM, proton NMR, TGA and FT-IR spectroscopy. To optimize adsorption conditions, the effect of various variable such as time, adsorbent dose, pH, temperature, and difenoconazole initial concentration were evaluated. Results showed that, the maximum difenoconazole removal percentage was about 94.7%, and 96.6% for Cell-X and Cell-D, respectively. Kinetic and thermodynamic studies on the adsorption process showed that the adsorption of difenoconazole by the two polymers is a pseudo-second order and follows the Langmuir isotherm model. The obtained values of ∆G ° and ∆H suggest that the adsorption process is spontaneous at room temperature. The results showed that Cell-X could be a promising adsorbent on a commercial scale for difenoconazole. The several adsorption sites present in Cell-X in addition to the semi crown ether structure explains the high efficiency it has for difenoconazole, and could be used for other toxic pesticides. Monte Carlo (MC) and Molecular Dynamic (MD) simulation were performed on a model of Cell-X and difenoconazole, and the results showed strong interaction.


Assuntos
Celulose/química , Dioxolanos/isolamento & purificação , Nanopartículas/química , Polímeros/química , Polímeros/metabolismo , Triazóis/isolamento & purificação , Poluentes Químicos da Água/isolamento & purificação , Purificação da Água/métodos , Adsorção , Dioxolanos/metabolismo , Concentração de Íons de Hidrogênio , Simulação de Acoplamento Molecular , Termodinâmica , Triazóis/metabolismo , Poluentes Químicos da Água/metabolismo
3.
Heliyon ; 10(13): e33808, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-39040342

RESUMO

Curcumin is classified as a chemotherapeutic medication because of its potential against numerous cancer cell lines and ability to inhibit cancer cell proliferation. Despite these findings, curcumin has yet to be commercialized as a drug due to its low water solubility, low absorption, and restricted bioavailability. As a result, there is a demand for water-soluble curcumin with improved solubility, bioavailability, and thus bioactivity. In this study we report the synthesis and the anticancer activities of water-soluble curcumins derivatives with alkyl sulfonate moiety. The target water-soluble curcumin with alkyl sulfonate moieties was created utilizing a straightforward technique that involved reacting curcumin with various sultones. The cytotoxic (24 h) and cytostatic (72 h) anticancer effect on breast carcinoma (MCF-7), liver carcinoma (HepG2), skin melanoma (B16-F110), colon human cancer and HeLa cervical carcinoma cell lines viability % via MTT assay were determined for the prepared derivatives. Results showed that curcumin-derived compounds have a pronounced cytostatic anticancer effect rather than cytotoxic one in relation to the compound type, cancer cell line type, and examined concentration compared to curcumin. The curcumin sulfonates outperformed curcumin activity against the tested cancer cells and showed to be powerful anticancer candidate drugs as supported by the theoretical calculations. This is evident by their high capacity to form H-bonding during docking with the amino acid side chains and the Vina docking score.

4.
BMC Chem ; 18(1): 4, 2024 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-38172974

RESUMO

The development of biobased polymeric materials for wastewater purification has become a demand due to the growing need for water free of hazardous metal ions for safe purposes. The organic components of the OLLW including carbohydrates, phenolics, aromatic acids and others are cost-effective and sustainable choices for this application. This work focuses on a method for turning the organic components of liquid waste from the olive industry (OILW) into a foam-based value-added polymer that has several metal ion binding sites. The process of making the target polymers involved reacting the components of the OILW with hexamethylene diisocyante and 1,4-phnyelene diisocynate to create the polymeric materials LHMIDIC and LPDIC that are in foam forms with urethane linkages, respectively. The adsorption competence of the polymeric foams toward Pb(II) was evaluated as a function of various parameters including adsorbent dose, pH, temperature, initial ion concentration and time. The optimum parameters values that led to a quantitative removal of Pb(II) were identified. The obtained thermodynamic parameters showed that the adsorption by the two foams was spontaneous at room temperature. The isothermal and kinetic values showed that the adsorption by synthesized foams follows a second order kinetic and obeys the Langmuir isothermal model. The foams showed a high tendency for removing multi metal ions present in a real sample of wastewater. The original nature of the starting material used in making the foam, cost and the obtained results showed the potential of using the foam in a large-scale plants of wastewater purification.

5.
Polymers (Basel) ; 15(4)2023 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-36850079

RESUMO

In this work, we present a process for converting olive industry solid waste (OISW) into a value-added material with ionic receptors for use in the removal of toxic metal ions from wastewater. This 3D polymer is a promising adsorbent for large-scale application, since it is a low-cost material made from agricultural waste and showed exceptional performance. The synthesis of the network polymer involved the carboxymethylation of OISW and curing of the carboxymethylated OISW at an elevated temperature to promote the formation of ester linkages between OISW's components. FT-IR, atomic force microscopy, and thermal analysis were performed on the crosslinked product. The adsorption efficiency of the crosslinked carboxymethylated OISW toward Pb(II), Cu(II), and other toxic metal ions present in sewage was evaluated as a function of adsorbent dose, temperature, pH, time, and initial metal ion. The percentage removal of about 20 metal ions present in a sewage sample collected from a sewer plant located in the Palestinian Territories was determined. The adsorption efficiency did not drop even after six cycles of use. The kinetic study showed that the adsorption process follows the Langmuir isotherm model and the second-order adsorption rate. The experimental Qe values of 13.91 and 13.71 mg/g were obtained for Pb(II) and Cu(II) removal, respectively. The thermodynamic results confirm the spontaneous metal bonding to the receptor sites of the crosslinked carboxymethylated OISW.

6.
Int J Biol Macromol ; 239: 124328, 2023 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-37019199

RESUMO

Contamination in water is due to various environmental pollutants from natural and anthropogen activities. To remove toxic metals from contaminated water, we developed a novel adsorbent in foam form based on an olive industry waste material. The foam synthesis involved oxidation of cellulose extracted from the waste to dialdehyde, functionalization of the cellulose dialdehyde with an amino acid group, reacting the functionalized cellulose with hexamethylene diisocyanate and p-phenylene diisocyanate to produce the target polyurethanes Cell-F-HMDIC and Cell-F-PDIC, respectively. The optimum condition for lead(II) adsorption by Cell-F-HMDIC and Cell-F-PDIC were determined. The foams show the ability to quantitatively remove most of metal ions present in a real sample of sewage. The kinetic and thermodynamic studies confirmed a spontaneous metal ion binding to the foams with a second pseudo-order adsorption rate. The adsorption study revealed it obeys the Langmuir isotherm model. The experimental Qe values of both foams Cell-F-PDIC and Cell-F-HMDIC were 2.1929 and 2.0345 mg/g, respectively. Monte Carlo (MC) and Dynamic (MD) and simulations showed excellent affinity of both foams for lead ions with high adsorption negative energy value indicating vigorous interactions of Pb(II) with the adsorbent surface. The results indicate the usefulness of the developed foam in commercial applications. ENVIRONMENTAL IMPLICATION: Elimination of metal ions from contaminated environments is important for a number of reasons. They are toxic to humans via interaction with biomolecules, resulting in disruption of the metabolism and biological activities of many proteins. They are toxic to plants. Industrial effluents and/or wastewater discharged from production processes, contain a considerable amount of metal ions. In this work, the use of naturally produced materials, such as olive waste biomass, as adsorbents for environmental remediation has received great attention. This biomass represents unused resources and presents serious disposal problems. We demonstrated that such materials are capable of selectively adsorbing metal ions.


Assuntos
Metais Pesados , Poluentes Químicos da Água , Purificação da Água , Humanos , Celulose/química , Poliuretanos , Aminoácidos , Metais , Purificação da Água/métodos , Íons , Água , Adsorção , Poluentes Químicos da Água/química , Cinética , Concentração de Íons de Hidrogênio
7.
BMC Chem ; 16(1): 43, 2022 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-35689266

RESUMO

BACKGROUND: Cellulose polymers with multidentate chelating functionalities that have high efficiency for toxic metal ions present in water were designed, synthesized, and analyzed. The synthesis was carried out by reacting microcrystalline cellulose extracted from the solid waste of the olive industry with tert-Butyl acetoacetate (Cell-AA), produced cellulose with ß-ketoester functionality was then reacted with aniline and the amino acid glycine to produce Cell-ß-AN and Cell-ß-GL, respectively. RESULTS: The adsorption efficiency of the three polymers toward Pb(II) and various toxic metal ions present in sewage was evaluated as a function of adsorbent dose, time, temperature, pH value, and initial ion concentration to determine optimum adsorption conditions. The three polymers showed excellent efficiency toward about 20 metal ions present in a sewage sample collected from the sewer. The adsorption process follows the Langmuir adsorption isotherm model with a second-order of adsorption rate, the calculated qe values (2.675, 15.252, 20.856 mg/g) were close to the experimental qe values (2.133, 13.91, 18.786 mg/g) for the three polymers Cell-AA, Cell-ß-AG and Cell-ß-AN, respectively. Molecular Dynamic (MD) and Monte Carlo (MC) simulations were performed on the three polymers complexed with Pb(II). CONCLUSION: The waste material of the olive industry was used as a precursor for making the target cellulose polymers with ß-Amino Ester Pendant Group. The polymer was characterized by SEM, proton NMR, TGA, and FT-IR spectroscopy. The efficacy of adsorption was quantitative for metal ions present in a real sample of wastewater and the efficiency didn't drop even after 7 cycles of use. The results indicate the existence of strong complexation. The thermodynamic study results showed a spontaneous bonding between of Pb(II) and the polymers pendant groups expressed by the negative value of the Gibbs free energy.

8.
Polymers (Basel) ; 13(3)2021 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-33573294

RESUMO

In this study, cellulose-based derivatives with heterocyclic moieties were synthesized by reacting cellulose with furan-2-carbonyl chloride (Cell-F) and pyridine-2,6-dicarbonyl dichloride (Cell-P). The derivatives were evaluated as adsorbents for the pesticide tetraconazole from aqueous solution. The prepared adsorbents were characterized by SEM, TGA, IR, and H1 NMR instruments. To maximize the adsorption efficiency of tetraconazole, the optimum conditions of contact time, pH, temperature, adsorbent dose, and initial concentration of adsorbate were determined. The highest removal percentage of tetraconazole from water was 98.51% and 95% using Cell-F and Cell-P, respectively. Underivatized nanocellulose was also evaluated as an adsorbent for tetraconazole for comparison purpose, and it showed a removal efficiency of about 91.73%. The best equilibrium adsorption isotherm model of each process was investigated based on the experimental and calculated R2 values of Freundlich and Langmuir models. The adsorption kinetics were also investigated using pseudo-first-order, pseudo-second-order, and intra-particle-diffusion adsorption kinetic models. The Van't Hoff plot was also studied for each adsorption to determine the changes in adsorption enthalpy (∆H), Gibbs free energy (∆G), and entropy (∆S). The obtained results showed that adsorption by Cell-F and Cell-P follow the Langmuir adsorption isotherm and the mechanism follows the pseudo-second-order kinetic adsorption model. The obtained negative values of the thermodynamic parameter ∆G (-4.693, -4.792, -5.549 kJ) for nanocellulose, Cell-F, and Cell-P, respectively, indicate a spontaneous adsorption process. Cell-F and Cell-P could be promising absorbents on a commercial scale for tetraconazole and other pesticides.

9.
Front Chem ; 9: 709600, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34336793

RESUMO

The expanding amount of remaining drug substances in wastewater adversely affects both the climate and human well-being. In the current investigation, we developed new cellulose acetic acid derivation/zeolite fiber as an effective technique to eliminate erythromycin (ERY) from wastewater. The number of interchangeable sites in the adsorbent structures and the ratio of ERY to the three adsorbents were identified as the main reasons for the reduction in adsorption as the initial ERY concentrations increased. Additionally, for all adsorbents, the pseudo-second-order modeling showed better fitting for the adsorption than the pseudo-first-order modeling. However, the findings obtained in the pseudo-first-order model were still enough for explaining the sorption kinetics of ERY, showing that the surface displayed all chemisorption and physi-sorption adsorption processes by both adsorbents. The R 2 for the second order was very close to 1 for the three adsorbents in the case of pseudo-second-order. The adsorption capacity reached 17.76 mg/g. The three adsorbents showed negative values of ΔH, and these values were -6,200, -8,500, and -9600 kJ/mol for zeolite, CA, and ZCA, respectively, and this shows that the adsorption is exothermic. The desorption analysis shows no substantial loss of adsorption site after three trials, indicating higher stability and resilience of the three adsorbents, indicating a strong repeatability of their possible use in adsorption without contaminating the environment. In addition, the chemical attitude and possible donor-acceptor interactions of ERY were assessed by the quantum chemical parameters (QCPs) and NBO analysis performed, at the HF/6-311G** calculations.

10.
Materials (Basel) ; 13(15)2020 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-32726973

RESUMO

In recent years, concerns have been raised about the occurrence of active raw materials and pharmaceutical ingredients that may be present in water, including wastewater, in the pharmaceutical industry. Wastewater treatment methods are not enough to completely remove active pharmaceuticals and other waste; thus, this study aims to assess the use of a multiwall carbon nanotube after derivatization and magnetization as a new and renewable absorbent for removing ibuprofen from an aqueous medium. The adsorbents were prepared by first oxidizing a multiwall carbon nanotube and then deriving the oxidized product with hydroxyl amine (m-MWCNT-HA), hydrazine (m-MWCNT-HYD), and amino acid (m-MWCNT-CYS). Adsorbents were characterized by Raman spectroscopy, Fourier Transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM and TEM), Brunauer-Emmett-Teller surface area analysis (BET), thermogravimetric analysis (TGA), and vibrating sample magnetometer (VSM). Batch adsorption studies were conducted to study the effects of pH, temperature, time, and initial concentration of the adsorbate. Adsorption isotherm, kinetics, and thermodynamics studies were also conducted. The results show that the optimal pH for nearly complete removal of Ibu in a short time at room temperature was 4 for three adsorbents. The adsorption followed the Langmuir isotherm model with pseudo-second-order kinetics. The percentage of removal of ibuprofen reached up to 98.4%, 93%, and 61.5% for m-MWCNT-CYS, m-MWCNT-HYD, and m-MWCNT-HA respectively. To the best of our knowledge, the grafted MWCNTs presented in this work comprise the first example in the literature of oxidized MWCNT modified with such functionalities and applied for ibuprofen removal.

11.
Med Chem ; 16(8): 1112-1123, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31448712

RESUMO

BACKGROUND: Curcumin is a safe, versatile natural product with unlimited number of biological activities and a precursor for various heterocyclic compounds. OBJECTIVE: The present study was aimed to the development of a curcumin based antimicrobial reagent with high potency against gram-positive and gram-negative bacteria. METHODS: Herein we report a simple and convenient one step method for synthesizing a series of 1,4-benzodiazepines via condensation cyclization reaction between curcumin and various 1,2- phenylenediamine in refluxed ethanol. RESULTS: A series of new 1,4-benzodiazepins were synthesized and their structures were supported by FT-IR, 1H NMR, 13C NMR, and mass spectral analysis. Synthesized 1,4-benzodiazepins were evaluated for their in vitro antimicrobial activity against gram positive (S. aureus and S. epidermidis) and gram negative (E. coli and P. aeruginosa) bacteria. They exhibited low to high potency against the tested organisms. In particular, dichlorinated 1,4-benzodiazepine 9 exhibited a remarkable potency against the gram-positive bacteria S. aureus (MIC: 3.125 µg mL-1, MBC: 12 µg mL-1). It showed a higher potency than most of the tested reference drugs. Compound 9 showed the medium activity against E. coli. Genotoxic study revealed that, benzodiazepines 9 attacked the DNA of E. coli strains and damaged it. The potency of compound 9, could be attributed to the multiple chlorine atoms present on the aromatic ring. CONCLUSION: Some of the synthesized curcumin based benzodiazepines showed excellent potency against gram positive bacteria. These benzodiazepines could be a great candidate as a future antimicrobial agent.


Assuntos
Antibacterianos/farmacologia , Benzodiazepinas/farmacologia , Curcumina/química , Desenho de Fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Benzodiazepinas/síntese química , Benzodiazepinas/química , Testes de Sensibilidade Microbiana , Estrutura Molecular
12.
BMC Chem ; 13(1): 86, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31384833

RESUMO

Pesticides and herbicides have been used extensively in agricultural practices to control pests and increase crop yields. Paraquat (PQT2+, 1,1-dimethyl-4,4-dipyridinium chloride) is one of the herbicide that belois classified as bipyridines and is used over the world. The objective of this study is to use ketoenol-pyrazole receptor functionalized silica hybrid as adsorbent for removal PQT2+ from aqueous solution. The adsorbent was synthesized, and characterized using scanning electron microscopy (SEM), nuclear magnetic resonance (NMR), Thermal analysis and other techniques. Different experimental parameters such as the effect of the amount of adsorbent, solution pH and temperatures and contact times were studied. Pseudo-order kinetics models were studied, and our data followed a pseudo second order. Experimental data were analyzed for both Langmuir and Freundlich models and the data fitted well with the Langmuir isotherm model. To understand the mechanism of adsorption, thermodynamic parameters like standard enthalpy, standard Gibbs free energy, and standard entropy were studied. The study indicated that the process is spontaneous, exothermic in nature and follow physisorption mechanisms. The novelty of this study showed surface of pyrazol-enol-imine-substituted silica (SiNPz) has the ability to highlight the surface designed for efficient removal of PQT2+, from aqueous solutions more than other studies. The study also showed that ketoenol-pyrazole receptor can be regenerated in five cycles using HNO3 without affecting its adsorption capacity.

13.
Environ Sci Pollut Res Int ; 26(27): 28080-28091, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31363973

RESUMO

A cross-linked cellulose-amine polymer composed of nanocrystalline cellulose and 1,4-pheneylnediamine was synthesized, and its application as an adsorbent of metal ions from wastewater was dementated. The nanocrystalline cellulose was generated from an olive industry solid waste. The cross-linked polymer analysis results of FTIR, NMR, TEM, SEM, and XRD were generated. The adsorption efficiency of the cellulose-amine polymer toward Cu(II) and Pb(II) was investigated as a function of adsorbent dose, temperature, pH, and time. The adsorption parameters that lead to an excellent adsorption efficiency were determined. The polymer also showed an excellent extraction efficiency toward 20 metal ions present in a sewage sample. The various functional groups present on polymer surface such as amino, hydroxyl, and aryl played a crucial role on metal adsorption. Thermodynamic analysis results support the high efficiency of the polymer toward the metal ions. Kinetic study results reveal that the adsorption process fits well with the pseudo-second-order model and the adsorption isotherm follows a Langmuir isotherm model.


Assuntos
Eliminação de Resíduos Líquidos/métodos , Adsorção , Aminas , Celulose/química , Íons/análise , Cinética , Metais Pesados/análise , Polímeros , Temperatura , Termodinâmica , Águas Residuárias/química , Poluentes Químicos da Água/análise , Purificação da Água/métodos
14.
PLoS One ; 14(8): e0221132, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31454362

RESUMO

The development of efficacious and safe drugs for the treatment of neurological diseases related to glutamate toxicity has been a focus in neuropharmacological research. Specifically, discovering antagonists to modulate the activity and kinetics of AMPA receptors, which are the fastest ligand-gated ion channels involved in excitatory neurotransmission in response to glutamate. Thus, the current study investigated novel curcumin derivatives on the biophysical properties of AMPA receptors, specifically on the homomeric GluA2 and the heteromeric GluA2/A3 subunits and assessed for inhibitory actions. The biophysical parameter (i.e., desensitization, deactivation, and peak currents) were measured by using whole-cell patch clamp electrophysiology with and without the administration of the derivatives onto HEK293 cells. CR-NN, CR-NNPh, CR-MeNH, and CR-NO of the tested derivatives showed inhibition on all AMPA receptors up to 6 folds. Moreover, the inhibitory derivatives also increased desensitization and deactivation, which further intensifies the compounds' neuroprotective effects. However, CR-PhCl, CR-PhF, and CR-PhBr did not show any significant changes on the peak current, deactivation or desensitization rates. By comparison to other discovered and widely used antagonist, the prepared curcumin derivatives are not selective to a specific AMPA subunit, instead implement its effect in the same way between all types of AMPA receptors. Additionally, the obtained results provide derivatives that not only noncompetitively inhibit AMPARs but also decrease its biophysical kinetics, specifically desensitization and deactivation rates. Hence, to potentially serve as a new AMPAR inhibitor with therapeutic potential, the current study provides compounds that are non-selective and non-competitive antagonist, which also effect the desensitization and deactivation rates of the receptor.


Assuntos
Curcumina/farmacologia , Doenças do Sistema Nervoso/tratamento farmacológico , Receptores de AMPA/química , Fenômenos Biofísicos/efeitos dos fármacos , Curcumina/análogos & derivados , Curcumina/química , Eletrofisiologia , Ácido Glutâmico/química , Ácido Glutâmico/metabolismo , Células HEK293 , Humanos , Doenças do Sistema Nervoso/metabolismo , Doenças do Sistema Nervoso/patologia , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Técnicas de Patch-Clamp , Receptores de AMPA/antagonistas & inibidores
15.
Eur J Pharm Sci ; 136: 104951, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31173869

RESUMO

Curcumin is a natural polyphenol that has a broad spectrum of therapeutic characters, including neuroprotective actions against various neurological diseases. However, the molecular mechanism behind its neuroprotective properties remains obscure. The current study investigated the neuroprotective properties of 7 different curcumin derivatives on the gating biophysical properties of AMPA receptors, specifically on the calcium-permeable homomeric GluA1 and calcium impermeable heteromeric GluA1/A2 subunits. Due to the association between excessive activation of AMPARs and neurotoxicity linked to numerous pathologies, we aim to target and manipulate the kinetics of AMPARs through these derivatives. The current study used patch-clamp electrophysiology to measure the whole-cell currents in the presence and absence of the curcumin derivatives onto HEK293 cells expressing AMPA subunits. Our results showed that some of the curcumin derivatives showed an inhibitory effect and altered the gating biophysical properties, namely, deactivation and desensitization. In the presence of those derivatives, the peak current measured was significantly reduced, and the desensitization and deactivation rates decreased as well, achieving slower kinetics of the receptor and depressing its activity. These results suggest that the two most promising derivatives have inhibitory actions and act as allosteric modulators. Many neurological diseases like epilepsy, ALS, and strokes are associated with overactivation of AMPA receptors. We can potentially synthesize a more potent neuroprotective drug to treat those neurological diseases, by understanding the most stable chemical interaction between the derivative and the receptor underlying the reported neuronal depressive properties.


Assuntos
Curcumina/farmacologia , Subunidades Proteicas/antagonistas & inibidores , Receptores de AMPA/antagonistas & inibidores , Cálcio/metabolismo , Linhagem Celular , Células HEK293 , Humanos , Cinética , Doenças do Sistema Nervoso/tratamento farmacológico , Doenças do Sistema Nervoso/metabolismo , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Fármacos Neuroprotetores/farmacologia
16.
Environ Sci Pollut Res Int ; 25(22): 22060-22074, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29802610

RESUMO

The work shown in this article demonstrate a novel example of converting olive industry solid waste (OISW) into a magnetic cellulose nanocrystalline (MNCs) to serve as selective magnetic sorbents for methylene blue. Olive industry solid waste contains about 40% cellulose. The cellulose was extracted in a powder form from olive industry solid waste by subjecting it to a multistep pulping and bleaching process. The extracted powder cellulose was then converted to nanocrystalline cellulose (NCs) by acid hydrolysis. The NCs were then treated with a solution of FeCl3.6H2O, FeSO4, and H2O by a colloidal suspension method which produced free-flowing porous MNCs. The produced MNCs are characterized by several spectroscopic and analytical techniques such as SEM, TEM, XRD, FTIR VSM, and TGA. The efficiency of the three polymers cellulose powder, NCs, and MNCs toward extracting methylene blue (MB) from water was evaluated. Cellulose powder and NCs showed acceptable tendency for methylene blue. However, MNCs showed excellent extraction efficiency toward MB. The thermodynamic studies revealed a spontaneous adsorption of MB by MNCs at various temperatures. The spontaneous adsorption could be attributed to the electrostatic interaction and H-bonding between MNCs and MB. However, the interaction between cellulose, NCs, and MB is limited to the H-bonding.


Assuntos
Celulose/química , Azul de Metileno/isolamento & purificação , Resíduos Sólidos , Eliminação de Resíduos Líquidos/métodos , Poluentes Químicos da Água/isolamento & purificação , Adsorção , Indústria de Processamento de Alimentos , Magnetismo , Azul de Metileno/química , Microscopia Eletrônica de Varredura , Microscopia Eletrônica de Transmissão , Nanoestruturas/química , Olea , Espectroscopia de Infravermelho com Transformada de Fourier , Termodinâmica , Águas Residuárias/química , Poluentes Químicos da Água/química , Difração de Raios X
17.
Chem Cent J ; 9: 59, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26491467

RESUMO

BACKGROUND: Electrochemical oxidation considered to be among the best methods in waste water desalination and removing toxic metals and organic pesticides from wastewater like Methidathion. The objective of this work is to study the electrochemical oxidation of aqueous wastes containing Methidathion using boron doped diamond thin-film electrodes and SnO2, and to determine the calculated partial charge and frontier electron density parameters. RESULTS: Electrolysis parameters such as current density, temperature, supporting electrolyte (NaCl) have been optimized. The influences of the electrode materials on methidathion degradation show that BDD is the best electrode material to oxidize this pesticide organophosphorous. Energetic cost has been determinate for all experiments. The results provide that 2 % of NaCl, 60 mA cm(-2) and 25 ºC like the optimized values to carry out the treatment. For BDD the achieved Chemical Oxidation Demand reduction was about 85 %, while for SnO2 it was about 73 %. The BDD anode appears to be the more promising one for the effective electrochemical treatment of methidathion. Finally the theoretical calculation was done by using the calculation program Gaussian 03W, they are a permit to identify the phenomena engaged near the electrode and to completely determine the structures of the products of electrochemical oxidation formed during the degradation and which they are not quantifiable in experiments because of their high reactivity. CONCLUSIONS: The comparison of the results relating to the two electrodes indicates that these materials have a power to reduce the quantity of the organic matter in the electrolyzed solution. But the speed of oxidation of these compounds is different according to the materials of the electrodes used. Graphical abstract:Structural of methidathion [O,O-dimethyl-S-(5-methoxy-1,3,4-thiadiazolinyl-3-methyl) dithiophosphate] used for study the electrochemical oxidation.

18.
Iran J Pharm Res ; 12(1): 47-56, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-24250571

RESUMO

A series of curcumin derivatives containing heterocyclic moiety have been synthesized and evaluated for their antibacterial activities. The chemical structures of the synthesized compounds were verified on the basis of spectral data and elemental analyses. Investigation of antimicrobial activity of the derivatives demonstrated the ability to inhibit Gram-positive microorganisms with zone of inhibition ranging from 14-18 mm, MIC ranging between 0.0625 and 0.25 mg/mL. Among all tested derivatives, diazepine 4 exhibited remarkable potency against Gram-positive bacteria S. aureus. An extensive study is underway to optimize the effectiveness of diazepine type of compounds and to determine their mode of action.

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