RESUMO
We have recently discovered that ester-stabilized phosphorus ylides, resulting from deprotonation of a phosphonium salt such as [Ph3PCH2COOR], can transfer protons across artificial and biological membranes. To create more effective cationic protonophores, we synthesized similar phosphonium salts with one ((heptyloxycarbonylmethyl)(p-tolyl)bromide) or two ((butyloxycarbonylmethyl)(3,5-xylyl)osphonium bromide) methyl substituents in the phenyl groups. The methylation enormously augmented both protonophoric activity of the ylides on planar bilayer lipid membrane (BLM) and uncoupling of mammalian mitochondria, which correlated with strongly accelerated flip-flop of their cationic precursors across the BLM.
Assuntos
Mitocôndrias Hepáticas , Fósforo , Animais , Mitocôndrias Hepáticas/metabolismo , Fósforo/metabolismo , Ésteres/metabolismo , Brometos/metabolismo , Metilação , Bicamadas Lipídicas/metabolismo , MamíferosRESUMO
The chemical derivatization to enhance the signal intensity and signal-to-noise (S/N) of several organophosphorus (OP) acids in liquid chromatography tandem mass spectrometry (LC-ESI-MS/MS) is illustrated. The OP class of compounds represents the environmental degradants of OP nerve agents and pesticides. N-(2-(bromomethyl)benzyl)-N,N-diethylethanaminium bromide (CAX-B) was utilized to derivatize a panel of eight acids consisting of five alkyl methylphosphonic acids (ethyl-, isopropyl-, isobutyl-, cyclohexyl-, and pinacolyl-methylphosphonic acid) along with three dialkylphosphate analogs (diethyl-, dibutyl-, and diethyl thio-phosphate). The derivatization reaction with CAX-B was conducted in acetonitrile in the presence of potassium carbonate at 70 °C for 1 h. The resulting acid derivatives were analyzed with an LC-Orbitrap-ESI-MS/MS, and their dissociation processes were investigated. It was found that the derivatization procedure increased the limits of identification (LOIs) by one to over two orders of magnitude from the range of 1 to 10 ng/mL for the intact OP-acids to the range of 0.02-0.2 ng/mL for the derivatized acids utilizing an LC-MS(QqQ) in MRM mode, regardless of the sample matrix (hair, concrete, or plant extracts). The interpretation of the corresponding ESI-MS/MS spectra for each type of derivatized sub-OP family revealed the formation of characteristic neutral losses and a characteristic ion for the organophosphorus core. This derivatization is beneficial and useful for screening and identifying target and "unknown" OP acids.
Assuntos
Brometos , Espectrometria de Massas em Tandem , Cátions , Cromatografia LíquidaRESUMO
A deaminative reductive coupling of amino acid pyridinium salts with aryl bromides has been developed to enable efficient synthesis of noncanonical amino acids and diversification of peptides. This method transforms natural, commercially available lysine, ornithine, diaminobutanoic acid, and diaminopropanoic acid to aryl alanines and homologated derivatives with varying chain lengths. Attractive features include ability to transverse scales, tolerance of pharma-relevant (hetero)aryls and biorthogonal functional groups, and the applicability beyond monomeric amino acids to short and macrocyclic peptide substrates. The success of this work relied on high-throughput experimentation to identify complementary reaction conditions that proved critical for achieving the coupling of a broad scope of aryl bromides with a range of amino acid and peptide substrates including macrocyclic peptides.
Assuntos
Aminoácidos , Brometos , Aminoácidos/química , Aminas/química , Peptídeos/química , OrnitinaRESUMO
Tertiary phosphine oxides, phosphine sulfides, and phosphine selenides containing pyridine, imidazole, and pyrazole groups have been synthesized via the reaction of elemental phosphorus or secondary phosphine oxides with functional pyridines, imidazoles, and pyrazoles. Alkyl tris(2-pyridylethyl)phosphonium iodide and bromide are also obtained by quaternization of the corresponding phosphine. Antimicrobial activity of the synthesized compounds, including nitrogen-containing heterocycles, phosphorus, selenium, and sulfur, with respect to Enterococcus durans, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa microorganisms is evaluated. It is found that phosphine chalcogenides bearing imidazole (14, 19), pyrazole (13), and pyridine fragments (5, 9) and phosphonium salts (11, 12) can be considered as new promising antibacterial agents. For some synthesized compounds, LC50 is determined. Phosphine oxide with methylpyrazole fragments (13) and phosphonium salts (11, 12) show strong profile of antimicrobial activity, and cytotoxic effect of phosphonium bromide having a long chain radical (12) is by order of magnitude higher than that of cisplatin. We believe that the results obtained may contribute to the development of highly effective agents for the treatment and prevention of bacterial infections and cancers.
Assuntos
Anti-Infecciosos , Citostáticos , Fósforo , Brometos , Sais , Anti-Infecciosos/farmacologia , Antibacterianos/farmacologia , Pirazóis/farmacologia , Piridinas , Imidazóis/farmacologia , Óxidos , Testes de Sensibilidade MicrobianaRESUMO
Ficus rubiginosa plant extract showed antimicrobial activity, but no evidence concerning its antiviral properties was reported. The antiviral activity of the methanolic extract (MeOH) and its n-hexane (H) and ethyl acetate (EA) fractions against Herpes simplex virus-1 (HSV-1), Human coronavirus (HCoV) -229E, and Poliovirus-1 (PV-1) was investigated in the different phases of viral infection in the VERO CCL-81 cell line. To confirm the antiviral efficacy, a qPCR was conducted. The recorded cytotoxic concentration 50% was 513.1, 298.6, and 56.45 µg/mL for MeOH, H, and EA, respectively, assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay after 72 h of treatment. The Ficus rubiginosa leaf extract inhibited the replication of HSV-1 in the early stages of infection, showing a complete inhibition up to 0.62, 0.31, and 1.25 µg/mL. Against HCoV-229E, a total inhibition up to 1.25 µg/mL for MeOH and H as well as 5 µg/mL for EA was observed. Otherwise, no activity was recorded against PV-1. The leaf extract could act directly on the viral envelope, destructuring the lipid membrane and/or directly blocking the enriched proteins on the viral surface. The verified gene inhibition suggested that the treatments with M, H, and EA impaired HSV-1 and HCoV-229E replication, with a greater antiviral efficiency against HSV-1 compared to HCoV-229E, possibly due to a greater affinity of Ficus rubiginosa towards membrane glycoproteins and/or the different lipid envelopes.
Assuntos
Coronavirus Humano 229E , Ficus , Herpesvirus Humano 1 , Poliovirus , Humanos , Antivirais/farmacologia , Brometos , Extratos Vegetais/farmacologia , Glicoproteínas de Membrana , LipídeosRESUMO
Data regarding the therapeutic potential of Caladium lindenii (C. lindenii) are insufficient. It becomes more important to explore plants as an alternative or palliative therapeutics in deadly diseases around the globe. The current study was planned to explore C. lindenii for its anticancer activity of ethanolic and hexane extracts of C. lindenii leaves against hepatic carcinoma (HepG2) and human embryonic kidney (HEK293T) cell lines. HepG2 and HEK293T cells were treated with 10, 50, 100, 200, and 400 µg/mL of ethanolic and hexane extracts of C. lindenii and were incubated for 72 h. Antiproliferative activity was measured by 3-(4,5-dimethylthiazol-2yl)-2,5-biphenyl tetrazolium bromide (MTT) assay, and percentage viability were calculated through crystal violet staining and cellular morphology by Floid Cell Imaging Station. The study showed ethanolic extract exhibiting a significantly higher antiproliferative effect on HepG2 (IC50 = 31µg/mL) in a concentration-dependent manner, while HEK293T (IC50 = 241µg/mL) cells showed no toxicity. Hexane extract exhibited lower cytotoxicity (IC50 = 150µg/mL) on HepG2 cells with no effect on HEK293T (IC50 = 550µg/mL). On the other hand, the percentage viability of HepG2 cells was recorded as 78%, 67%, 50%, 37%, and 28% by ethanolic extracts, and 88%, 80%, 69%, 59%, and 50% by hexane extracts at tested concentrations of both extracts. Toxicity assay showed significantly safer ranges of percentage viabilities in normal cells (HEK293T), i.e., 95%, 90%, 88%, 76%, and 61% with ethanolic extract and 97%, 95%, 88%, 75%, and 62% with hexane extract. The assay validity revealed 100% viability in the control negative (dimethyl sulfoxide treated) and less than 45% in the control positive (cisplatin) on both HepG2 and HEK293T cells. Morphological studies showed alterations in HepG2 cells upon exposure to >50 µg/mL of ethanolic extracts and ≥400 µg/mL of hexane extracts. HEK293T on the other hand did not change its morphology against any of the extracts compared to the aggressive changes on the HepG2 cell line by both extracts and positive control (cisplatin). In conclusion, extracts of C. lindenii are proved to have significant potential for cytotoxicity-induced apoptosis in human cancer HepG2 cells and are less toxic to normal HEK293T cells. Hence C. lindenii extracts are proposed to be used against hepatocellular carcinoma (HCC) after further validations.
Assuntos
Carcinoma Hepatocelular , Neoplasias Hepáticas , Brometos/uso terapêutico , Carcinoma Hepatocelular/tratamento farmacológico , Carcinoma Hepatocelular/patologia , Cisplatino/uso terapêutico , Dimetil Sulfóxido , Violeta Genciana/uso terapêutico , Células HEK293 , Hexanos , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/patologia , Extratos Vegetais/químicaRESUMO
OBJECTIVE: Plants are valuable sources of new pharmaceuticals. Secondary metabolites of the genus Erythrophleum exhibit cytotoxicity and may have therapeutic value. The cytotoxic activity of ethanolic leaf extract of Erythrophleum succirubrum Gagnep. against a human cholangiocarcinoma cell line was assessed. METHODS: Crude extract of E. succirubrum was prepared by ethanol extraction. The ethanolic leaf extract of E. succirubrum was evaluated for cytotoxicity against the human cholangiocarcinoma cell line KKU-M213 using 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assays. The chemical composition of E. succirubrum leaf extract was analyzed using GC/MS. RESULT: The ethanolic leaf extract of E. succirubrum reduced the viability of KKU-M213 cells in a dose- and time-dependent manner. It showed high cytotoxicity, with IC50 values of 65.22 ± 1.18 µg/mL and 1.19 ± 1.38 µg/mL at exposure times of 24 and 96 h, respectively. GC/MS analysis of the ethanolic leaf extract of E. succirubrum identified 22 components. The main constituents identified were Cyclohexanone, 2-[2-nitro-1-(2-naphthyl)ethyl]-(14.79%) followed by allomycin (14.65%), mome inositol (14.30%), campesterol (11.80%) and ethyl linolenate (10.83%), respectively. CONCLUSION: Five major groups of compounds were found, with lipids dominating, followed by carbohydrates, benzenoids, phenylpropanoids, polyketides and organoheterocyclic compounds. Many of the bioactive components discovered in the ethanolic leaf extract of E. succirubrum might be responsible for its cytotoxic properties.
Assuntos
Neoplasias dos Ductos Biliares , Colangiocarcinoma , Fabaceae , Policetídeos , Neoplasias dos Ductos Biliares/tratamento farmacológico , Ductos Biliares Intra-Hepáticos , Brometos/uso terapêutico , Carboidratos/uso terapêutico , Linhagem Celular Tumoral , Colangiocarcinoma/tratamento farmacológico , Cicloexanonas , Etanol , Humanos , Inositol/uso terapêutico , Lipídeos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Policetídeos/uso terapêuticoRESUMO
A simple and sensitive colorimetric assay for detecting organophosphorus pesticides (OPs) was developed based on 3,3',5,5'-tetramethylbenzidine (TMB)/hydrogen peroxide (H2O2)/dodecyl trimethylammonium bromide (DTAB)-tetramethyl zinc (4-pyridinyl) porphyrin (ZnTPyP). In this system, based on the peroxidase-like activity of DTAB-ZnTPyP, H2O2 decomposes to produce hydroxyl radicals, which oxidize TMB, resulting in blue oxidation products. The OPs (trichlorfon, dichlorvos, and thimet) were first combined with DTAB-ZnTPyP through electrostatic interactions. The OPs caused a decrease in the peroxidase-like activity of DTAB-ZnTPyP due to spatial site blocking. At the same time, π-interactions occurred between them, and these interactions also inhibited the oxidation of TMB (652 nm), thus making the detection of OPs possible. The limits of detection for trichlorfon, dichlorvos, and thimet were 0.25, 1.02, and 0.66 µg/L, respectively, and the corresponding linear ranges were 1-35, 5-45, and 1-40 µg/L, respectively. Moreover, the assay was successfully used to determine OPs in cabbage, apple, soil, and traditional Chinese medicine samples (the recovery ratios were 91.8-109.8%), showing a great promising potential for detecting OPs also in other complex samples.
Assuntos
Praguicidas , Porfirinas , Brometos , Colorimetria/métodos , Diclorvós , Peróxido de Hidrogênio , Metaloporfirinas , Compostos Organofosforados , Peroxidases , Praguicidas/análise , Triclorfon , Zinco , Compostos de ZincoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Mayaro fever is a neglected tropical disease. The region of the most significant circulation of the Mayaro virus (MAYV) is the Amazon rainforest, situated in remote areas that are difficult to access and where medicine is scarce. Thus, the regional population uses plants as an alternative for the treatment of various diseases. Fridericia chica is an endemic plant of tropical regions used in traditional medicine to treat fever, malaise, inflammation, and infectious diseases such as hepatitis B. However, its antiviral activity is poorly understood. AIM OF THE STUDY: This study aimed to investigate the anti-MAYV activity of the hydroethanolic extract of the leaves of Fridericia chica (HEFc) in mammalian cells and its possible mechanism of action. MATERIALS AND METHODS: The antiviral activity of HEFc was studied using Vero cell lines against MAYV. The cytotoxicity and antiviral activity of the extract were evaluated by the 3-(4, 5- dimethyl-2-thiazolyl)-2, 5-diphenyl-2H-tetrazolium bromide (MTT) assay. The overall antiviral activity was confirmed by the plaque forming units (PFU) method. Then, the effects of HEFc on MAYV multiplication kinetics, virus adsorption, penetration, and post-penetration, and its virucidal activity were determined in Vero cells using standard experimental procedures. RESULTS: HEFc exerted a effect against viral infection in Vero cells at a non-cytotoxic concentration, and no virion was detected in the supernatant in a dose-dependent and selective manner. HEFc inhibited MAYV in the early and late stages of the viral multiplication cycle. The extract showed significant virucidal activity at low concentrations and did not affect adsorption or viral internalization stages. In addition, HEFc reduced virions at all post-infection times investigated. CONCLUSIONS: HEFc has good antiviral activity against MAYV, acting directly on the viral particles. This plant extract possesses an excellent and promising potential for developing effective herbal antiviral drugs.
Assuntos
Alphavirus , Bignoniaceae , Animais , Antivirais/farmacologia , Brometos/farmacologia , Chlorocebus aethiops , Mamíferos , Extratos Vegetais/farmacologia , Células VeroRESUMO
In this study, silver nanoparticles were synthesized using Alpinia officinarum rhizome extract via an eco-friendly green synthesis method. The silver nanoparticles (AO-AgNPs) were characterized by UV-Vis spectrometry, scanning electron microscopy, energy-dispersive X-ray spectroscopy, and dynamic light scattering. Further, the cytotoxic and apoptotic effects of AO-AgNPs were investigated in human cancer cells with different tissue origins via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay and flow cytometric analyses, respectively. The expression levels of anti-apoptotic Bcl-2 protein were evaluated via a real-time polymerase chain reaction. The synthesized AO-AgNPs induced a significant cytotoxic effect in all tested cancer cells but not in normal cells. AO-AgNPs induced the percentage of apoptotic cells and reduced the levels of anti-apoptotic Bcl-2 mRNA levels in cancer cells. These results demonstrate the potential application of AO-AgNPs in cancer treatment.
Assuntos
Alpinia , Antineoplásicos , Nanopartículas Metálicas , Neoplasias , Alpinia/metabolismo , Antineoplásicos/farmacologia , Apoptose , Brometos/farmacologia , Humanos , Nanopartículas Metálicas/uso terapêutico , Extratos Vegetais/farmacologia , RNA Mensageiro/farmacologia , Rizoma/metabolismo , Prata/farmacologiaRESUMO
Bromism is an unusual syndrome characterized by a variety of nervous system impairments such as ataxia, confusion, and delusions. Contemporaneous cases are rare as therapeutic use of bromide-containing medications has declined, but bromides can still be obtained as unregulated dietary supplements. Bromism from dietary supplements is not well-described. We present a case of a 23-year-old male who was taking numerous supplements and developed bromism, characterized by ataxia, confusion, and persistent agitation. His laboratory evaluation revealed a large negative anion gap and a serum bromide level of 1200 mg/L (ref: 0-12 mg/L). He was treated with maintenance intravenous normal saline to promote excretion of the bromide ion and slowly returned to baseline over ten days. Bromism is an unusual but well-described constellation of neurologic impairments that presents insidiously and may be easily missed. The emergency physician should be aware of the dangers of bromide-containing dietary supplements and should educate patients taking these supplements of their risks.
Assuntos
Brometos , Solução Salina , Adulto , Ataxia , Confusão , Suplementos Nutricionais/efeitos adversos , Humanos , Internet , Masculino , Adulto JovemRESUMO
Six new (1-6) and seven known depsidones (7-13) were isolated from the culture of an ant (Monomorium chinensis)-derived fungus Spiromastix sp. MY-1. Their structures were elucidated by extensive spectroscopic analysis including high resolution MS, 1D and 2D NMR data. The new bromide depsidones were obtained through supplementing potassium bromide in the fermentation medium of Spiromastix sp. MY-1. All isolated compounds showed various bioactivities against the tested phytopathogenic bacteria. Particularly, new bromide compound 4, named spiromastixone S, exhibited the strongest activity against Xanthomonas oryzae pv. oryzae with a MIC value of 5.2 µmol·-1.
Assuntos
Formigas , Brometos , Animais , Antibacterianos , Depsídeos , Fungos , Lactonas , Testes de Sensibilidade Microbiana , Estrutura MolecularRESUMO
Neuroblastoma is the most common solid tumor in children. New treatment approaches are needed because of the harmful side effects and costs of the methods used in the treatment of neuroblastoma. Medicinal and aromatic plants are important for new treatment approaches due to their minimal side effects and economic advantages. Therefore, the present study was carried out to examine the cytotoxic effect of Chaerophyllum macropodum extract on human neuroblastoma (SH-SY5Y) and fibroblast (HDFa) cell lines. 3-[4,5-dimethylthiazole-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and lactate dehydrogenase release (LDH) assays were used to determine the cytotoxic effect of C. macropodum. The extracts were analyzed for their phenolic content by HPLC-PDA. Major components were determined as 63.600% o-coumaric acid, 15.606% catechine hydrate, 8.713% rosmarinic acid, 4.376% clorogenic acid, and 3.972% salicylic acid. The obtained results from cytotoxicity testing revealed that C. macropodum exerted a significant cytotoxic effect on human neuroblastoma cells at all tested concentrations (p < 0.05). But it did not lead to any cytotoxic potential on human fibroblasts. As a result, the obtained data clearly revealed C. macropodum exerted a selective cytotoxic action on neuroblastoma cells for the first time.
Assuntos
Antineoplásicos , Neuroblastoma , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Brometos/farmacologia , Brometos/uso terapêutico , Linhagem Celular Tumoral , Sobrevivência Celular , Criança , Ácidos Cumáricos/uso terapêutico , Humanos , Lactato Desidrogenases , Neuroblastoma/patologia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ácido Salicílico/farmacologia , Ácido Salicílico/uso terapêuticoRESUMO
For the past few years, the environmental safety problems of radioactive nuclides caused wide public concern. In this work, the dodecyl trimethyl ammonium bromide-modified silicon dioxide composite (DTAB/SiO2) was synthesized for the elimination of uranium. The dodecyl trimethyl ammonium bromide can decorate the surface of the silicon dioxide and change its surface topography, which can offer more active sites and functional groups for the combination of U(VI). The removal capacity of U(VI) on DTAB/SiO2 reached 78.1 mg/g, which was greater than that of the silicon dioxide nanopowder. In the adsorption process, the surface oxygen-containing functional groups formed surface complexation with uranium. The results may provide helpful content to eliminate U(VI) and expand the application of surfactant in radioactive nuclide cleanup.
Assuntos
Urânio , Adsorção , Brometos , Oxigênio , Compostos de Amônio Quaternário , Dióxido de Silício/química , Tensoativos , Urânio/químicaRESUMO
We have studied the impact of the lipid ratio on the membrane permeability of mixed phosphatidylcholine (POPC)/phosphatidylglycerol (POPG) membranes induced by 1-dodecyl-3-methylimidazolium bromide ([C12MIM]+Br-) ionic liquid by evaluating the role of affinity and architecture of the phospholipid bilayer. Nine different model membranes composed of negatively charged POPG and zwitterionic POPC lipids mixed in molar ratios of 9:1, 8:2, 7:3, 6:4, 5:5, 4:6, 3:7, 2:8, and 1:9 have been studied. The membrane permeability of each composition has been evaluated using fluorescence-based dye leakage assays. Despite having the highest membrane affinity, POPG-rich membranes doped with 10 and 20 mol % POPC are found to be the least permeable. 31P- and 2H-based solid-state NMR investigations reveal that the minor POPC component is homogeneously dispersed in the PG/PC (8:2) membrane. In contrast, the lipids seem to be segregated into POPG- and POPC-rich domains in the complementary PG/PC (2:8) composition. Although [C12MIM]+ cations have a stronger interaction with the POPG component in the mixed membranes, their insertion has a limited impact on the overall structure and dynamics of the PG/PC (8:2) composition.
Assuntos
Líquidos Iônicos , Fosfatidilgliceróis , Brometos , Imidazóis , Bicamadas Lipídicas , Permeabilidade , FosfatidilcolinasRESUMO
In recent times, silver (Ag) based semiconductors have been gained a lot of attention as photocatalysts for industrial waste-water treatment owing to their strong visible-light absorbing capability and small bandgap energy. Therefore, herein, we have designed and utilized a one-pot hydrothermal approach to the synthesis of nano-sized AgBr covered potato-like Ag2MoO4 composite photocatalysts for the elimination of organic wastes from the aquatic environment. To achieve a high-performance photocatalyst, a sequence of AgBr/Ag2MoO4 composites were acquired with varying CTAB from 1 to 4 mmol. Furthermore, the photocatalytic activity of these photocatalysts was confirmed from decomposing of Rhodamine B (RhB) dye via visible-light elucidation. It can be noticed that AgBr/Ag2MoO4 composites exhibited significantly increased photocatalytic behaviour as compared with pure AgBr and Ag2MoO4. Surprisingly, the AgBr/Ag2MoO4 composite obtained from 2 mmol CTAB was eliminated the entire RhB dye with 25 min. Also, the recycling experiment indicates the AgBr/Ag2MoO4 composite has an excellent photo-stability. Accordingly, the as-acquired AgBr/Ag2MoO4 composite would be a suitable photocatalytic material for industrial waste-water purification.
Assuntos
Prata , Solanum tuberosum , Brometos , Catálise , Resíduos Industriais , Compostos de Prata , Águas Residuárias , ÁguaRESUMO
A novel biobased monomer for the preparation of thermally reversible networks based on the Diels-Alder reaction was synthesized from jatropha oil. The oil was epoxidized and subsequently reacted with furfurylamine to attach furan groups via an epoxide ring opening reaction. However, furfurylamine also reacted with the ester groups of the triglycerides via aminolysis, thus resulting in short-chain molecules that ultimately yielded brittle thermally reversible polymers upon cross-linking via a Diels-Alder reaction. A full-factorial experimental design was used in finding the optimum conditions to minimize ester aminolysis and to maximize the epoxide ring opening reaction as well as the number of furans attached to the modified oil. The optimum conditions were determined experimentally and were found to be 80 °C, 24 h, 1:1 molar ratio, with 50 mol % of LiBr with respect to the modified oil, resulting in 35% of ester conversion, 99% of epoxide conversion, and an average of 1.32 furans/triglyceride. Ultimately, further optimization by a statistical approach led to an average of 2.19 furans per triglyceride, which eventually yielded a flexible network upon cross-linking via a Diels-Alder reaction instead of the brittle one obtained when the furan-functionalization reaction was not optimized.
Assuntos
Furanos/química , Jatropha/química , Óleos de Plantas/química , Brometos/química , Catálise , Reação de Cicloadição , Compostos de Epóxi/química , Jatropha/metabolismo , Compostos de Lítio/química , Temperatura , Triglicerídeos/químicaRESUMO
In this study, the protective effects and potential mechanisms of (2-Carboxyethyl) dimethylsulfonium Bromide (Br-DMPT) were evaluated in relation to the gill health status of on-growing young grass carp (Ctenopharyngodon idella). A total of 450 grass carp (216.49 ± 0.29 g) were randomly distributed into five treatments of three replicates each (30 fish per replicate) and were fed diets supplemented with gradational Br-DMPT (0-520.0 mg/kg levels) for 60 days. Subsequently, the fish were challenged with Flavobacterium columnare for 3 days, and the gills were sampled to evaluate antioxidant status and immune responses evaluation. Our results showed that, when compared to the control group, dietary supplementation with appropriate Br-DMPT levels resulted in the following: (1) decreased gill rot morbidity and improved gill histological symptoms after exposure to F. columnare (P < 0.05); (2) improved activities and gene expression levels (except GSTP2 gene) of antioxidant enzymes and decreased oxidative damage parameter values (reactive oxygen species, malondialdehyde and protein carbonyl) (P < 0.05), which may be partially associated with the nuclear factor-erythroid 2-related factor 2 (Nrf2) signalling pathway (P < 0.05); (3) increased lysozyme (LZ) and acid phosphatase (ACP) activities and complement 3 (C3), C4 and immunoglobulin M (IgM) contents, and upregulated genes expressions of antibacterial peptides (liver-expressed antimicrobial peptide-2A, -2B, hepcidin, ß-defensin and mucin2) (P < 0.05); (4) upregulated gene expressions of anti-inflammatory cytokines (except IL--4/13B) that may be partially to the TOR/(S6K1, 4E-BP1) signalling pathway, and downregulated gene expressions of pro-inflammatory cytokines (except IL-12P35) may be partially to the IKK ß, γ/IκBα/NF-kB) signalling pathway (P < 0.05). Taken together, our results indicate that dietary supplementation with appropriate amounts of Br-DMPT may effectively protect on-growing grass carp from F. columnare by strengthening gill antioxidant capacity and immunity. Furthermore, based on measures of combatting gill rot, antioxidant indices (MDA) and immune indices (LZ), the dietary Br-DMPT supplementation levels for on-growing grass carp are recommended to be 291.14, 303.38 and 312.01 mg/kg diet, respectively.
Assuntos
Brometos/metabolismo , Carpas/imunologia , Substâncias Protetoras/metabolismo , Compostos de Sulfônio/metabolismo , Ração Animal/análise , Animais , Brometos/administração & dosagem , Dieta/veterinária , Suplementos Nutricionais/análise , Relação Dose-Resposta a Droga , Substâncias Protetoras/administração & dosagem , Distribuição Aleatória , Compostos de Sulfônio/administração & dosagemRESUMO
BACKGROUND: Trace elements function as essential cofactors that are involved in various biochemical processes in mammals. Autophagy is vital for nutrient supplement, which is an important Zeitegber for the circadian homeostasis in heart. Here, we considered the possibility that autophagy, as well as the cardiomyocyte clock and glycolysis are interlinked. Detrimental effects were observed when cardiac system is exposed to bromine containing drugs. This study investigated the effects and mechanisms of bromide on the circadian clock and glycolytic metabolism of H9C2 cardiomyocytes. RESULTS: In the present study, bromide does not affect cell viability and apoptosis of H9C2 cardiomyocytes. Bromide dampens the clock and glycolytic (Hk2 and Pkm2) gene expression rhythmicity in a dose-dependent manner. Additionally, bromide inhibits autophagic process in H9C2 cardiomyocytes. In contrast, rapamycin (an autophagy inducer) dramatically restores the inhibitory effect of NaBr on the mRNA expression levels of clock genes (Bmal1, Cry1 and Rorα) and glycolytic genes (Hk2 and Pkm2). CONCLUSIONS: Our results reveal that bromide represses the clock and glycolytic gene expression patterns, partially through inhibition of autophagy.
Assuntos
Autofagia/efeitos dos fármacos , Brometos/farmacologia , Relógios Circadianos/efeitos dos fármacos , Glicólise/efeitos dos fármacos , Miócitos Cardíacos , Fatores de Transcrição ARNTL/genética , Fatores de Transcrição ARNTL/metabolismo , Animais , Brometos/metabolismo , Linhagem Celular , Relógios Circadianos/genética , Criptocromos/genética , Criptocromos/metabolismo , Expressão Gênica , Glicólise/genética , Hexoquinase/genética , Hexoquinase/metabolismo , Homeostase , Miócitos Cardíacos/efeitos dos fármacos , Miócitos Cardíacos/metabolismo , Membro 1 do Grupo F da Subfamília 1 de Receptores Nucleares/genética , Membro 1 do Grupo F da Subfamília 1 de Receptores Nucleares/metabolismo , Piruvato Quinase/genética , Piruvato Quinase/metabolismo , RatosRESUMO
Inspired by chasing-escaping behaviors of predator and swarming prey in nature, here we demonstrate a concept to create active micromotor systems from two species of passive microparticles with biomimetic predator-prey interactions. In this concept, the biomimetic predator-prey interactions are established in a binary particle system comprising the diffusiophoretic attractive microparticles (prey particles) and the diffusiophoretic repulsive ones (predator particles). In the absence of additional chemical fuels and external fields, the predator particles are attracted by and constantly chase the swarming prey particles, which, in response, escape from the former and show dynamic group reconfigurations because of the local repulsion. Based on this concept, various synthetic active micromotor systems have been demonstrated, including active ZnO-TiO2, Ag3PO4-TiO2, and ZnO-AgBr micromotor systems. As the predator and prey particles are powered by each other through the biomimetic predator-prey interactions, the concept proposed here provides an advanced method to develop not only a class of single micromotors powered by passive particles or "solid fuels" but also micromotor swarms capable of manipulating "moving cargo". In addition, it also illustrates a proof-of-concept implementation of intelligent micro/nanomotor systems composed of heterogeneous individuals with complementary or cooperative functions.