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1.
Curr Top Med Chem ; 2024 Aug 12.
Artigo em Inglês | MEDLINE | ID: mdl-39136505

RESUMO

OBJECTIVE: In this study, we have synthesized 19 Thiazolidine (TZD) derivatives to investigate their potential anti-ZIKV effects. METHODS: Nineteen thiazolidine derivatives were synthesized and evaluated for their cytotoxicity and antiviral activity against the ZIKA virus. RESULTS: Among them, six demonstrated remarkable selectivity against the ZIKV virus, exhibiting IC50 values of <5µM, and the other compounds did not demonstrate selectivity for the virus. Interestingly, several derivatives effectively suppressed the replication of ZIKV RNA copies, with derivatives significantly reducing ZIKV mRNA levels at 24 hours post-infection (hpi). Notably, two derivatives (ZKC-4 and -9) stood out by demonstrating a protective effect against ZIKV cell entry. Informed by computational analysis of binding affinity and intermolecular interactions within the NS5 domain's N-7 and O'2 positions, ZKC-4 and FT-39 displayed the highest predicted affinities. Intriguingly, ZKC-4 and ZKC-9 derivatives exhibited the most favorable predicted binding affinities for the ZIKV-E binding site. CONCLUSION: The significance of TZDs as potent antiviral agents is underscored by these findings, suggesting that exploring TZD derivatives holds promise for advancing antiviral therapeutic strategies.

2.
Materials (Basel) ; 16(24)2023 Dec 08.
Artigo em Inglês | MEDLINE | ID: mdl-38138706

RESUMO

This work presents the structural and electrical characterization of K2NiF4-type layered perovskites of LaSrAl1-xMgxO4-δ composition to be used as oxide-ion electrolytes for a solid-oxide fuel cell (SOFC). These perovskites were prepared by mechano-chemical synthesis (ball milling), an alternative to traditional synthesis methods such as citrate-nitrates and solid-state reaction. With these methods, two things are avoided: first, the use of nitrate salts, which are more environmentally harmful than oxide precursors, and second, it saves the series of long thermal treatments associated with solid-state reactions. After grinding the precursors, nanometric particles were obtained with a combination of crystalline regions and amorphous regions; this effect was determined by XRD and TEM, showing that Mg has a positive effect on the phase formation by only mechanical synthesis. R2C4: After sintering, it was found by XRD that the sample x = 0.1 only presents the diffraction peaks corresponding to the desired phase, which shows a phase purity greater than 97%, even higher than that of the standard undoped sample. For x = 0.2 and 0.3, there was a segregation of impurities, possibly by the local migration of La and Sr heavy cations; this was determined by SEM and EDS. The electrical characterization of the sintered pellets was carried out by electrochemical impedance spectroscopy, which determined that the incorporation of Mg in the structure improves the ionic conductivity by three orders of magnitude, obtaining conductivities of 1.6 mS/cm at 900 °C for x = 0.2. Although the improvement in conductivity is considerable, many challenges such as densification, the segregation of impurities, and the study of mechanical and thermal properties must be carried out on these materials to endorse them as solid electrolytes in SOFC.

3.
Sheng Wu Gong Cheng Xue Bao ; 39(9): 3605-3614, 2023 Sep 25.
Artigo em Chinês | MEDLINE | ID: mdl-37805841

RESUMO

Brasilicardin A (BraA) is a natural diterpene glycoside isolated from the pathogenic actinomycete Nocardia brasiliensis IFM 0406 with highly potent immunosuppressive activity (IC50=0.057 µg/mL). BraA potently inhibits the uptake of amino acids that are substrates for amino acid transport system L of T cells, which is different from the existing clinical immunosuppressants. BraA is more potent in a mouse mixed lymphocyte reaction and less toxic against various human cell lines compared with the known clinical immunosuppressants, such as cyclosporin A, ascomycin and tacrolimus. Therefore, BraA attracted more attention as a new promising immunosuppressant. However, the development of this promising immunosuppressant as drug for medical use is so far hindered because BraA has the unusual and synthetically challenging skeleton and shows the low-yield production in the natural pathogenic producer. This review introduces the molecular structure of BraA, its activity, mechanism of action, chemical synthesis of BraA analogs, heterologous expression of gene cluster, and an application of combining microbial and chemical synthesis for production of BraA, with the aim to facilitate the efficient production of BraA and its analogs.


Assuntos
Diterpenos , Imunossupressores , Animais , Camundongos , Humanos , Imunossupressores/farmacologia , Imunossupressores/química , Aminoglicosídeos/farmacologia , Ciclosporina/farmacologia
4.
Antibiotics (Basel) ; 12(7)2023 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-37508180

RESUMO

Bacterial biofilms are a significant problem in the food industry, as they are difficult to eradicate and represent a threat to consumer health. Currently, nanoparticles as an alternative to traditional chemical disinfectants have garnered much attention due to their broad-spectrum antibacterial activity and low toxicity. In this study, silver nanoparticles (AgNPs) were synthesized by a biological method using a Jacaranda mimosifolia flower aqueous extract and by a chemical method, and the factors affecting both syntheses were optimized. The nanoparticles were characterized by Ultraviolet-visible (UV-Vis) spectrophotometry, Fourier-transform infrared spectroscopy (FTIR), Dynamic light scattering (DLS), X-ray diffraction (XRD), and Transmission electron microscopy (TEM) with a spherical and uniform shape. The antibacterial and antibiofilm formation activity was carried out on bacterial species of Pseudomonas aeruginosa and Staphylococcus aureus with the capacity to form biofilm. The minimum inhibitory concentration was 117.5 µg/mL for the chemical and 5.3 µg/mL for the biological nanoparticles. Both types of nanoparticles showed antibiofilm activity in the qualitative Congo red test and in the quantitative microplate test. Antibiofilm activity tests on fresh lettuce showed that biological nanoparticles decreased the population of S. aureus and P. aeruginosa by 0.63 and 2.38 logarithms, respectively, while chemical nanoparticles had little microbial reduction. In conclusion, the biologically synthesized nanoparticles showed greater antibiofilm activity. Therefore, these results suggest their potential application in the formulation of sanitizing products for the food and healthcare industries.

5.
Pharmaceuticals (Basel) ; 16(6)2023 May 24.
Artigo em Inglês | MEDLINE | ID: mdl-37375730

RESUMO

BACKGROUND: Statins present a plethora of pleiotropic effects including anti-inflammatory and antimicrobial responses. A,α-difluorophenylacetamides, analogs of diclofenac, are potent pre-clinical anti-inflammatory non-steroidal drugs. Molecular hybridization based on the combination of pharmacophoric moieties has emerged as a strategy for the development of new candidates aiming to obtain multitarget ligands. METHODS: Considering the anti-inflammatory activity of phenylacetamides and the potential microbicidal action of statins against obligate intracellular parasites, the objective of this work was to synthesize eight new hybrid compounds of α,α-difluorophenylacetamides with the moiety of statins and assess their phenotypic activity against in vitro models of Plasmodium falciparum and Trypanosoma cruzi infection besides exploring their genotoxicity safety profile. RESULTS: None of the sodium salt compounds presented antiparasitic activity and two acetated compounds displayed mild anti-P. falciparum effect. Against T. cruzi, the acetate halogenated hybrids showed moderate effect against both parasite forms relevant for human infection. Despite the considerable trypanosomicidal activity, the brominated compound revealed a genotoxic profile impairing future in vivo testing. CONCLUSIONS: However, the chlorinated derivative was the most promising compound with chemical and biological profitable characteristics, without presenting genotoxicity in vitro, being eligible for further in vivo experiments.

6.
J Biol Chem ; 299(4): 103056, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36822328

RESUMO

Cationic and amphiphilic peptides can be used as homing devices to accumulate conjugated antibiotics to bacteria-enriched sites and promote efficient microbial killing. However, just as important as tackling bacterial infections, is the modulation of the immune response in this complex microenvironment. In the present report, we designed a peptide chimaera called Chim2, formed by a membrane-active module, an enzyme hydrolysis site and a formyl peptide receptor 2 (FPR2) agonist. This molecule was designed to adsorb onto bacterial membranes, promote their lysis, and upon hydrolysis by local enzymes, release the FPR2 agonist sequence for activation and recruitment of immune cells. We synthesized the isolated peptide modules of Chim2 and characterized their biological activities independently and as a single polypeptide chain. We conducted antimicrobial assays, along with other tests aiming at the analyses of the cellular and immunological responses. In addition, assays using vesicles as models of eukaryotic and prokaryotic membranes were conducted and solution structures of Chim2 were generated by 1H NMR. Chim2 is antimicrobial, adsorbs preferentially to negatively charged vesicles while adopting an α-helix structure and exposes its disorganized tail to the solvent, which facilitates hydrolysis by tryptase-like enzymes, allowing the release of the FPR2 agonist fragment. This fragment was shown to induce accumulation of the cellular activation marker, lipid bodies, in mouse macrophages and the release of immunomodulatory interleukins. In conclusion, these data demonstrate that peptides with antimicrobial and immunomodulatory activities can be considered for further development as drugs.


Assuntos
Anti-Infecciosos , Receptores de Formil Peptídeo , Animais , Camundongos , Antibacterianos/farmacologia , Anti-Infecciosos/química , Bactérias , Membranas , Receptores de Formil Peptídeo/antagonistas & inibidores
7.
Int J Mol Sci ; 23(21)2022 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-36362102

RESUMO

American trypanosomiasis is a worldwide health problem that requires attention due to ineffective treatment options. We evaluated n-butyl and isobutyl quinoxaline-7-carboxylate 1,4-di-N-oxide derivatives against trypomastigotes of the Trypanosoma cruzi strains NINOA and INC-5. An in silico analysis of the interactions of 1,4-di-N-oxide on the active site of trypanothione reductase (TR) and an enzyme inhibition study was carried out. The n-butyl series compound identified as T-150 had the best trypanocidal activity against T. cruzi trypomastigotes, with a 13% TR inhibition at 44 µM. The derivative T-147 behaved as a mixed inhibitor with Ki and Ki' inhibition constants of 11.4 and 60.8 µM, respectively. This finding is comparable to the TR inhibitor mepacrine (Ki = 19 µM).


Assuntos
Doença de Chagas , Tripanossomicidas , Trypanosoma cruzi , Humanos , Tripanossomicidas/farmacologia , Tripanossomicidas/química , Quinoxalinas/química , Óxidos/farmacologia , NADH NADPH Oxirredutases , Doença de Chagas/tratamento farmacológico , Inibidores Enzimáticos/química
8.
Braz. dent. j ; Braz. dent. j;33(3): 99-108, July-Sept. 2022. tab, graf
Artigo em Inglês | LILACS-Express | LILACS, BBO - Odontologia | ID: biblio-1384038

RESUMO

Abstract This study showed the synthesis of Glass ionomer cements (GIC) modified with calcium phosphate nanoparticles (nCaP). The nCaP/GIC were submitted to mechanical compression and diametral tensile tests. The biocomposite were characterized by scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). Cytotoxicity and cell viability tests were performed on the human bone marrow mesenchymal stem cells using a 3-(4,5-dimethylthiazol-2yl)2,5-diphenyl- tetrazolium-bromide assay and LIVE/DEAD assays. Statistically significant differences were observed for mechanical properties (Kruskal-Wallis, p<0.001), nCaP/GIC showed higher resistance to compression and diametral traction. The SEM analyses revealed a uniform distribution nCaP in the ionomer matrix. The EDX and XRD results indicated that hydroxyapatite and calcium β-triphosphate phases. The FTIR spectra revealed the asymmetric band of ν3PO43- between 1100-1030cm-1 and the vibration band associated with ν1PO43- in 963cm-1 associated with nCaP. The nCaP/GIC presented response to adequate cell viability and non-cytotoxic behavior. Therefore, the new nCaP/GIC composite showed great mechanical properties, non-cytotoxic behavior, and adequate response to cell viability with promising dental applications.


Resumo Este estudo apresenta a síntese de cimentos de ionômero de vidro (GIC) modificados com nanopartículas de fosfato de cálcio (nCaP). Os nCaP / GIC foram submetidos a ensaios mecânicos de compressão e tração diametral. Os biocompósitos foram caracterizados por microscopia eletrônica de varredura (MEV), espectroscopia de energia dispersiva de raios-X (EDX), difração de raios-X (XRD) e espectroscopia de infravermelho com transformada de Fourier (FTIR). Os testes de citotoxicidade e viabilidade celular foram realizados em células-tronco mesenquimais da medula óssea humana usando um ensaio de 3- (4,5-dimetiltiazol-2-il) 2,5-difeniltetrazólio-brometo e ensaios LIVE / DEAD. Diferenças estatisticamente significativas foram observadas para as propriedades mecânicas (Kruskal-Wallis, p <0,001), nCaP / GIC apresentou maior resistência à compressão e tração diametral. As análises de SEM revelaram uma distribuição uniforme de nCaP na matriz do ionômero. Os resultados de EDX e DRX indicaram fases de hidroxiapatita e β-trifosfato de cálcio. Os espectros de FTIR revelaram a banda assimétrica de ν3PO4 3- entre 1100-1030cm-1 e a banda de vibração associada a ν1PO4 3- em 963cm-1 associada a nCaP. O nCaP / GIC apresentou resposta adequada à viabilidade celular e comportamento não citotóxico. Portanto, o novo compósito nCaP / GIC apresentou ótimas propriedades mecânicas, comportamento não citotóxico e resposta adequada à viabilidade celular com promissoras aplicações odontológicas.

9.
Artigo em Espanhol | LILACS-Express | LILACS | ID: biblio-1392032

RESUMO

Objetivo: Analizar los indicadores hematológicos en pacientes con infección por SARS COV-2. Método: Observacional de tipo descriptiva. Resultados: Se ha encontrado la existencia de un patrón común de exámenes anormales del recuento leucocitario con Neutrófilos elevados en 43.69 % (neutrofilia) y los linfocitos, pero por debajo de los valores normales (linfopenia) en un 20.16 %. Además de monocitopenia en un 13.44%. Conclusión: La detección de Proteína C reactiva elevada y neutrofilia se relaciona con casos severos de COVID-19 en pacientes adultos. Ambas pruebas combinadas tienen una alta especificidad y sensibilidad para predicción temprana de casos se veros de COVID -19.


Objective: To analyze hematological indicators in patients with SARS COV-2 infection. Methods: Descriptive observational study. Results: A common pattern of abnormal leukocyte count tests was found with elevated neutrophils in 43.69% (neutrophilia) and lymphocytes, but below normal values (lymphopenia) in 20.16%. In addition to monocytopenia in 13.44%. Conclusion: The detection of elevated C-reactive protein and neutrophilia is associated with severe cases of COVID-19 in adult patients. Both tests combined have high specificity and sensitivity for early prediction of severe cases of COVID -19.

10.
Life Sci ; 278: 119647, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34043990

RESUMO

Recently, the dramatic emergence of antimicrobial resistance has received attention from World Health Organization. Synthetic antimicrobial peptides (SAMPs) are considered new weapons to fight against infections caused by multi-drug resistant pathogens. Here, the authors provide an overview of the current research on SAMPs. The focus is SAMPs, how to design them, which features must be considered during design, and comparison with natural peptides. This review also includes a discussion about the natural AMPs, mechanisms of action and applications as new drugs or even as adjuvants molecules to enhance commercial drugs activity. The advances in chemical synthesis have reduced the cost to produce synthetic peptides open ways to achieve new antimicrobial agents. Therefore, synthetic peptides are new promising molecules to safeguard human and animal health.


Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Desenho de Fármacos , Resistência Microbiana a Medicamentos , Proteínas Citotóxicas Formadoras de Poros/química , Proteínas Citotóxicas Formadoras de Poros/farmacologia , Animais , Anti-Infecciosos/síntese química , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Técnicas de Química Sintética , Resistência Microbiana a Medicamentos/efeitos dos fármacos , Resistência a Múltiplos Medicamentos/efeitos dos fármacos , Fungos/efeitos dos fármacos , Humanos , Micoses/tratamento farmacológico , Proteínas Citotóxicas Formadoras de Poros/síntese química
11.
Molecules ; 25(23)2020 Nov 25.
Artigo em Inglês | MEDLINE | ID: mdl-33255643

RESUMO

This paper reports an Alkali-Activated Materials (AAM) using two different precursors, metakaolin and a metallurgical slag with photocatalytic zinc oxide nanoparticles, as novel photocatalytic composites. The photodegradation performance of the composites using methylene blue (MB) dye as a wastewater model was investigated by ultraviolet radiations (UV-vis) spectroscopy. Adsorption in dark conditions and photodegradation under UV irradiation are the mechanisms for removing MB dye. The pseudo-first-order kinetic and pseudo-second-order kinetic models were employed, and the experimental data agreed with the pseudo-second-order model in both cases with UV and without UV irradiations. As new photocatalytic materials, these composites offer an alternative for environmental applications.


Assuntos
Álcalis/química , Nanopartículas/química , Processos Fotoquímicos , Óxido de Zinco/química , Adsorção , Algoritmos , Catálise , Cinética , Modelos Químicos , Nanopartículas/ultraestrutura , Difração de Raios X
12.
Mater Sci Eng C Mater Biol Appl ; 111: 110739, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32279792

RESUMO

Octa-(3-chloropropryl)silsesquioxane was chemically modified with histidine (SSQ-H) and characterized by spectroscopy in the infrared region (FT-IR), X-ray diffraction (XRD), X-ray Dispersive Energy Spectroscopy (EDX), Scanning Electron Microscopy (SEM). The analytical properties of SSQ-H were tested regarding of Cu2+ and Zn2+ adsorption and as an electrochemical sensor for the detection of ascorbic acid. The metal sorption results indicate that maximum amount of Cu2+ and Zn2+ adsorbed (Nfmax) were 1.58 × 10-3 and 5.67 × 10-4 mol g-1, respectively. After Cu2+ and Zn2+ ion adsorption and interaction with potassium hexacyanoferrate (III), the investigated materials displayed electroactivity for ascorbic acid detection. The anodic peak currents responses of a graphite paste electrode containing CuHCFSSQ-H presented a linear response in the concentration range of 4.0 × 10-4 to 4.0 × 10-3 mol L-1 for ascorbic acid detection. The limit of detection was of 2.99 × 10-4 mol L-1, with an amperometric sensitivity of 1.69 µA/mol L-1. The intensity of the anodic peak currents of the graphite paste electrode containing ZnHCFSSQ-H in the concentration range of 9.0 × 10-5 to 9.0 × 10-4 mol L-1 also displayed a linear response. The limit of detection was of 6.76 × 10-5 mol L-1, with an amperometric sensitivity of 0.0206 A/mol L-1.


Assuntos
Ácido Ascórbico/análise , Cobre/química , Técnicas Eletroquímicas/métodos , Histidina/química , Compostos de Organossilício/química , Zinco/química , Adsorção , Ácido Ascórbico/química , Eletrodos , Grafite/química , Limite de Detecção , Oxirredução , Reprodutibilidade dos Testes , Propriedades de Superfície
13.
Pest Manag Sci ; 76(4): 1435-1442, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31639267

RESUMO

BACKGROUND: The cashew stem borer Anthistarcha binocularis (Meyrick) is a major pest in cashew orchards in Brazil. The damage caused by the larvae results in economic losses, and the available chemical control is not suitable because of the endophytic nature of A. binocularis. The identification of the A. binocularis sex pheromone could provide novel applications for the detection and monitoring of this species. RESULTS: Two compounds from female sex gland extracts elicited electrophysiological responses on male antennae. They were identified as dodec-6-en-1-ol and dodec-6-en-1-yl acetate by gas chromatography-mass spectrometry. E/Z stereoisomers of both compounds were synthesized, and the electroantennograms for the synthetic compounds showed the strongest responses for the (E)-stereoisomers of the alcohol and acetate. In a field trial, the E6-12:OH/E6-12:OAc mixture attracted male A. binocularis, whereas the Z6-12:OH/Z6-12:OAc mixture attracted no specimens. CONCLUSIONS: The bioactive compounds from the sex pheromone of A. binocularis have been identified as a mixture of two previously unidentified pheromone compounds: E6-12:OH and E6-12:OAc. The mixture of both compounds was attractive to males in preliminary field experiments, and this study is the first report of Δ6-unsaturated monoenyl pheromone compounds in Lepidoptera. © 2019 Society of Chemical Industry.


Assuntos
Anacardium , Lepidópteros , Animais , Brasil , Feminino , Masculino , Feromônios , Atrativos Sexuais
14.
Mater Sci Eng C Mater Biol Appl ; 98: 789-799, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30813085

RESUMO

Zeolite/nanoparticle composites are synthesized and used as additive for waterborne formulations in replacement of traditional isothiazolinone-based biocides. Silver nanoparticles dispersed onto micrometer-sized crystals of A-type zeolite were prepared by thermal treatment or chemical reduction methods applied to the Ag-exchanged zeolite. The antifungal efficiency against Trichoderma sp. of waterborne outdoor coatings containing the supported silver nanoparticles, measured in terms of inhibition halo development, shows similar results to those obtained by using traditional organic biocides, the type, size and size distribution of the nanoparticles being the main factors affecting the biocidal action of the prepared coatings.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Nanopartículas Metálicas/química , Prata/química , Zeolitas/química , Escherichia coli/efeitos dos fármacos
15.
Sci Total Environ ; 651(Pt 2): 2845-2856, 2019 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-30463137

RESUMO

CuO nanostructured thin films supported on silicon with 6.5 cm2 area (geometric area greater than the studies reported in the literature) were synthesized by a chemical bath deposition technique. The electrodes were characterized by MEV, XRD, XPS, contact angle, cyclic voltammetry and electrochemical impedance spectroscopy analyses. To evaluate the photoelectrochemical properties of the CuO films, photocurrent-voltage measurements were performed using linear voltammetry. The catalytic activities of CuO nanostructures were evaluated by monitoring photodegradation of Mitoxantrone (MTX) under UV-A light irradiation. The method of photoelectrocatalysis (PEC), applying a voltage of 1.5 V and assisted by adding H2O2, was undertaken. To the best of our knowledge, no studies on the degradation of anticancer agents using PEC process have been found in the literature. For comparison purposes, experiments were performed under the same conditions by assisted photocatalysis (PC) with H2O2 and direct photolysis. CuO deposits consist of a needle-like morphology. The presence of CuO in the tenorite phase was evidenced by XRD and the XPS spectra showed the presence of copper(II) oxide. The increase in current under illumination shows that CuO exhibits photoactivity. The PEC system showed a 75% level of MTX degradation, while the level achieved using PC was 50%. Under UV-A light alone only 3% removal was obtained after 180 min. Up to 10 by-products were identified by chromatography-mass spectrometry (LC-MS) with m/z values ranging between 521 and 285 and a plausible degradation route has been proposed. It is worth mentioning that 9 by-products identified in this work, were not found in the literature in other studies of degradation or products generated as metabolites. The toxicity tests of MTX before and after PEC treatment with Artemia Salina and Allium cepa showed a decrease in the acute toxicity of the medium as the antineoplastic was degraded.


Assuntos
Antineoplásicos/química , Cobre/química , Mitoxantrona/química , Nanoestruturas/química , Processos Fotoquímicos , Antineoplásicos/análise , Antineoplásicos/toxicidade , Peróxido de Hidrogênio/química , Mitoxantrona/análise , Mitoxantrona/toxicidade , Modelos Químicos
16.
Biotechnol Prog ; 34(5): 1093-1101, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29882241

RESUMO

In this study we report the enzymatic synthesis of N-α-[Carbobenzyloxy]-Tyr-Gln-Gln (Z-YQQ), a new anticoagulant tripeptide. It was obtained using phytoproteases from the stems and petioles of Asclepias curassavica L. as catalyst in an aqueous-organic biphasic system formed by 50% (v/v) ethyl acetate and 0.1 M Tris-HCl buffer pH 8. The resulting peptide was compared with the analogous peptide Tyr-Gln-Gln (YQQ) produced by solid-phase chemical synthesis. The in vitro anticoagulant activity of the aforementioned peptides was determined using Wiener Lab Test (Wiener, Argentina). The toxicological activity of the peptides was also determined. The enzymatically synthesized Z-YQQ peptide acted on the extrinsic pathway of the coagulation cascade, delaying the conversion time of prothrombin to thrombin and fibrinogen to fibrin by 136 and 50%, respectively, with respect to the controls. The chemically synthesized YQQ peptide acted specifically on the intrinsic pathway of the coagulation cascade, affecting factors VIII, IX, XI, and XII from such cascade, and increasing the coagulation time by 105% with respect to the control. The results suggest that two new anticoagulant peptides (Z-YQQ and YQQ) can be useful for safe pharmaceutical applications. Nevertheless, some aspects related to peptide production should be optimized. © 2018 American Institute of Chemical Engineers Biotechnol. Prog., 2018 © 2018 American Institute of Chemical Engineers Biotechnol. Prog., 34:1093-1101, 2018.


Assuntos
Anticoagulantes/síntese química , Peptídeos/síntese química , Anticoagulantes/química , Anticoagulantes/farmacologia , Coagulação Sanguínea/efeitos dos fármacos , Catálise , Humanos , Peptídeos/química , Peptídeos/farmacologia , Preparações Farmacêuticas
17.
Chemosphere ; 182: 339-347, 2017 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28505575

RESUMO

In this study, cobalt (Co) was recycled from spent lithium ion batteries (LIBs) and used to synthesize cobalt ferrite (CoFe2O4-LIBs), which was applied as a catalyst for heterogeneous photo Fenton reactions that discolored methylene blue (MB) dye. The co-precipitation method was used to synthesize CoFe2O4-LIBs and CoFe2O4-R nanoparticles with spinel structures using as raw materials of the LIB cathodes and commercial reagents. X-ray diffraction (XRD) identified the formation of spinel-type CoFe2O4, which formed clusters that could be seen under scanning electron microscopy (SEM) analysis and nanometric particles seen under transmission electron microscopy (TEM). Inductively Coupled Plasma Optical Emission Spectrometer (ICP OES) analysis was used to determine the concentrations of metals present in the ferrite, which reached 6.5% (w/w) of Co. The optimal conditions for discoloring the dye were evaluated using a factorial design. Using CoFe2O4 as a catalyst, the best conditions for catalytic reaction were pH 3, 30.0 mg of catalyst, and 8.0 mL of H2O2 73% (v/v). Discoloration efficiencies of 87.3% and 87.7% were obtained from CoFe2O4-R and CoFe2O4-LIBs, respectively. Therefore, CoFe2O4-LIBs proved to be an efficient catalyst for discoloring MB dye using heterogeneous photo-Fenton reactions. This work is of scientific, social, economic, and environmental interest. It investigates the process of synthesizing,characterizing CoFe2O4LIBs and the efficiency of degrading MB dye, subjects that have economic and environmental, and therefore, social interest. The work has scientific interest particularly because of the correlation between the structure of the recycled material and its catalytic properties.


Assuntos
Catálise , Fontes de Energia Elétrica , Compostos Férricos/síntese química , Lítio , Nanoestruturas/química , Cobalto/química , Compostos Férricos/química , Peróxido de Hidrogênio/química , Microscopia Eletrônica de Varredura , Microscopia Eletrônica de Transmissão , Reciclagem/métodos , Difração de Raios X
18.
Regul Toxicol Pharmacol ; 86: 25-32, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28202347

RESUMO

Peroxisome proliferator-activated receptors (PPARs) are nuclear receptors involved in the metabolism of lipids and carbohydrates. The exogenous ligands of these receptors are thiazolidinediones (TZDs), which are used to treat type 2 diabetes mellitus (DM2). However, drugs from this group produce adverse effects such as hepatic steatosis. Hence, the aim of this work was to design a set of small molecules that can activate the γ isoform of PPARs while minimizing the adverse effects. The derivatives were designed containing the polar head of TZD and an aromatic body, serving simultaneously as the body and tail. Two ligands were selected out of 130 tested. These compounds were synthesized in a solvent-free reaction and their physicochemical properties and toxicity were examined. Acute oral toxicity was determined by administering these compounds to female Wistar rats in increasing doses (as per the OECD protocol 425). The median lethal dose (LD50) of the compound substituted with a hydroxyl heteroatom was above 2000 mg/kg, and that of the compound substituted with halogens was 700-1400 mg/kg. The results suggest that the compounds can interact with PPARγ and elicit biological responses similar to other TZDs, but without showing adverse effects. The compounds will be subsequently evaluated in a DM2 animal model.


Assuntos
Hipoglicemiantes/toxicidade , PPAR gama/agonistas , Tiazolidinedionas/síntese química , Tiazolidinedionas/toxicidade , Animais , Simulação por Computador , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes/síntese química , Ratos , Ratos Wistar
19.
Appl Microbiol Biotechnol ; 100(13): 5703-18, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27154347

RESUMO

Apocarotenoids are natural compounds derived from the oxidative cleavage of carotenoids. Particularly, C13-apocarotenoids are volatile compounds that contribute to the aromas of different flowers and fruits and are highly valued by the Flavor and Fragrance industry. So far, the chemical synthesis of these terpenoids has dominated the industry. Nonetheless, the increasing consumer demand for more natural and sustainable processes raises an interesting opportunity for bio-production alternatives. In this regard, enzymatic biocatalysis and metabolically engineered microorganisms emerge as attractive biotechnological options. The present review summarizes promising bioengineering approaches with regard to chemical production methods for the synthesis of two families of C13-apocarotenoids: ionones/dihydroionones and damascones/damascenone. We discuss each method and its applicability, with a thorough comparative analysis for ionones, focusing on the production process, regulatory aspects, and sustainability.


Assuntos
Biotecnologia/métodos , Carotenoides/biossíntese , Carotenoides/síntese química , Técnicas de Química Sintética/métodos , Aromatizantes/síntese química , Aromatizantes/metabolismo , Biotecnologia/tendências , Carotenoides/química , Técnicas de Química Sintética/tendências , Aromatizantes/química
20.
Materials (Basel) ; 9(1)2016 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-28787830

RESUMO

Pyrrole monomer was chemically polymerized onto SrCO3-Sr(OH)2 powders to obtain SrCO3-Sr(OH)2/polypyrrole nanocomposite to be used as a candidate for photocatalytic degradation of methylene blue dye (MB). The material was characterized by Fourier transform infrared (FTIR) spectroscopy, UV/Vis spectroscopy, and X-ray diffraction (XRD). It was observed from transmission electronic microscopy (TEM) analysis that the reported synthesis route allows the production of SrCO3-Sr(OH)2 nanoparticles with particle size below 100 nm which were embedded within a semiconducting polypyrrole matrix (PPy). The SrCO3-Sr(OH)2 and SrCO3-Sr(OH)2/PPy nanocomposites were tested in the photodegradation of MB dye under visible light irradiation. Also, the effects of MB dye initial concentration and the catalyst load on photodegradation efficiency were studied and discussed. Under the same conditions, the efficiency of photodegradation of MB employing the SrCO3-Sr(OH)2/PPy nanocomposite increases as compared with that obtained employing the SrCO3-Sr(OH)2 nanocomposite.

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