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1.
FEMS Yeast Res ; 242024 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-38444195

RESUMO

In this study, we explored the sphingolipid (SL) landscape in Candida auris, which plays pivotal roles in fungal biology and drug susceptibility. The composition of SLs exhibited substantial variations at both the SL class and molecular species levels among clade isolates. Utilizing principal component analysis, we successfully differentiated the five clades based on their SL class composition. While phytoceramide (PCer) was uniformly the most abundant SL class in all the isolates, other classes showed significant variations. These variations were not limited to SL class level only as the proportion of different molecular species containing variable number of carbons in fatty acid chains also differed between the isolates. Also a comparative analysis revealed abundance of ceramides and glucosylceramides in fluconazole susceptible isolates. Furthermore, by comparing drug-resistant and susceptible isolates within clade IV, we uncovered significant intraclade differences in key SL classes such as high PCer and low long chain base (LCB) content in resistant strains, underscoring the impact of SL heterogeneity on drug resistance development in C. auris. These findings shed light on the multifaceted interplay between genomic diversity, SLs, and drug resistance in this emerging fungal pathogen.


Assuntos
Antifúngicos , Candida , Antifúngicos/farmacologia , Candida auris , Esfingolipídeos , Farmacorresistência Fúngica , Testes de Sensibilidade Microbiana
2.
Physiol Plant ; 176(3): e14324, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38705866

RESUMO

Broomrape (Orobanche cumana) negatively affects sunflower, causing severe yield losses, and thus, there is a need to control O. cumana infestation. Brassinosteroids (BRs) play key roles in plant growth and provide resilience to weed infection. This study aims to evaluate the mechanisms by which BRs ameliorate O. cumana infection in sunflower (Helianthus annuus). Seeds were pretreated with BRs (1, 10, and 100 nM) and O. cumana inoculation for 4 weeks under soil conditions. O. cumana infection significantly reduced plant growth traits, photosynthesis, endogenous BRs and regulated the plant defence (POX, GST), BRs signalling (BAK1, BSK1 to BSK4) and synthesis (BRI1, BR6OX2) genes. O. cumana also elevated the levels of malondialdehyde (MDA), hydroxyl radical (OH-), hydrogen peroxide (H2O2) and superoxide (O2 •-) in leaves/roots by 77/112, 63/103, 56/97 and 54/89%, as well as caused ultrastructural cellular damages in both leaves and roots. In response, plants activated a few enzymes, superoxide dismutase (SOD), peroxidase (POD) and reduced glutathione but were unable to stimulate the activity of ascorbate peroxidase (APX) and catalase (CAT) enzymes. The addition of BRs (especially at 10 nM) notably recovered the ultrastructural cellular damages, lowered the production of oxidative stress, activated the key enzymatic antioxidants and induced the phenolic and lignin contents. The downregulation in the particular genes by BRs is attributed to the increased resilience of sunflower via a susceptible reaction. In a nutshell, BRs notably enhanced the sunflower resistance to O. cumana infection by escalating the plant immunity responses, inducing systemic acquired resistance, reducing oxidative or cellular damages, and modulating the expression of BR synthesis or signalling genes.


Assuntos
Brassinosteroides , Helianthus , Orobanche , Sementes , Helianthus/efeitos dos fármacos , Helianthus/imunologia , Helianthus/fisiologia , Brassinosteroides/farmacologia , Brassinosteroides/metabolismo , Orobanche/fisiologia , Orobanche/efeitos dos fármacos , Sementes/efeitos dos fármacos , Sementes/imunologia , Plantas Daninhas/efeitos dos fármacos , Plantas Daninhas/fisiologia , Doenças das Plantas/parasitologia , Doenças das Plantas/imunologia , Imunidade Vegetal/efeitos dos fármacos , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Fotossíntese/efeitos dos fármacos , Raízes de Plantas/imunologia , Raízes de Plantas/efeitos dos fármacos , Peróxido de Hidrogênio/metabolismo , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/imunologia , Proteínas de Plantas/metabolismo , Proteínas de Plantas/genética , Malondialdeído/metabolismo
3.
Cell Mol Biol (Noisy-le-grand) ; 69(4): 7-15, 2023 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-37329554

RESUMO

This study investigates the hazardous effects of lead on the histological and genotoxic parameters of the fish, Oreochromis niloticus. Present work was conducted in a series of three steps. In first step, acute toxicity, LC50 and lethal lead concentration were measured using Probit analysis method. LC50 value and lethal concentration for O. niloticus was measured as 77.673 mgL-1 and 150.924 mgL-1, respectively. In second step, histological changes were assessed by preparing slides of tissues of the gills, liver and kidney of both control and Pb-stressed O. niloticus and examining the respective tissues under the light microscope. The inferences showed significant histological alterations (p<0.05) in the gills of Pb-exposed fish including necrosis, edema, vascular congestion, shortening and curling and lifting of the epithelium of secondary lamella in gills. The cellular degeneration and dilation of sinusoids in liver and loss of hemopoietic tissue, necrosis and edema in kidney was observed. Histomorphometry of the liver showed a decrease in diameter of the central vein and hepatocyte along with an increase in width of sinusoids. The histomorphometry of kidney showed an increase in the diameter of renal corpuscle, glomerulus, proximal and distal convoluted tubules. The nuclear anomalies were studied in the RBCs of fish. Non-parametric Mann-Whitney U-test was conducted to compare nuclear abnormalities and the frequency of micronuclei among the control and lead-treated fish groups. Results declared an increased micronucleus, notched and de-shaped nuclei frequency, in RBCs of fish exposed to lead as compared to control group.


Assuntos
Ciclídeos , Poluentes Químicos da Água , Animais , Chumbo/toxicidade , Fígado , Necrose/patologia , Dano ao DNA , Brânquias/patologia , Poluentes Químicos da Água/toxicidade
4.
Ecotoxicol Environ Saf ; 252: 114624, 2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36758507

RESUMO

The excessive accumulation of cobalt (Co) in plant tissues severely impairs plant growth that ultimately reduces the yield. However, melatonin (MT) has been known to mediate the abiotic stress tolerance in plants. The present study aimed at investigating the protective mechanisms of exogenously applied MT (0, 50 and 100 µM) under Co (0, 100, 200 and 300 µM) stress by focusing on morpho-physiological, biochemical and cellular characterizations of Brassica napus plants. Cobalt (300 µM) alone treatment drastically inhibited the stomatal conductance, plant height (45%), leaf area (30%), free amino acid (139%), relative electrolyte leakage (109%), and total soluble sugars (71%), compared with the control. However, the exogenous supply of MT notably minimized the oxidative damage, lipid peroxidation and maintained the membrane integrity under Co-toxicity by restricting the overproduction of ROS (H2O2 and O2•), and MDA in leaves and roots. Melatonin significantly enhanced the activities of ROS-scavenging antioxidant enzymes, secondary metabolism-related phenylalanine ammonia lyase (PAL), polyphenol oxidase (PPO), stress-responsive genes (heat shock protein as HSP-90, methyl transferase as MT) and regulated the Co-transporters, especially in roots. These findings indicated that an exogenous supply of MT improve the plant morphology, photosynthetic apparatus, osmotic adjustments, and antioxidant defense systems by enhancing the Co-detoxification in B. napus plants.


Assuntos
Brassica napus , Melatonina , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Melatonina/farmacologia , Melatonina/metabolismo , Brassica napus/genética , Brassica napus/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio/metabolismo
5.
Int J Mol Sci ; 22(23)2021 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-34884597

RESUMO

The proteins of membrane transporters (MTs) are embedded within membrane-bounded organelles and are the prime targets for improvements in the efficiency of water and nutrient transportation. Their function is to maintain cellular homeostasis by controlling ionic movements across cellular channels from roots to upper plant parts, xylem loading and remobilization of sugar molecules from photosynthesis tissues in the leaf (source) to roots, stem and seeds (sink) via phloem loading. The plant's entire source-to-sink relationship is regulated by multiple transporting proteins in a highly sophisticated manner and driven based on different stages of plant growth and development (PG&D) and environmental changes. The MTs play a pivotal role in PG&D in terms of increased plant height, branches/tiller numbers, enhanced numbers, length and filled panicles per plant, seed yield and grain quality. Dynamic climatic changes disturbed ionic balance (salt, drought and heavy metals) and sugar supply (cold and heat stress) in plants. Due to poor selectivity, some of the MTs also uptake toxic elements in roots negatively impact PG&D and are later on also exported to upper parts where they deteriorate grain quality. As an adaptive strategy, in response to salt and heavy metals, plants activate plasma membranes and vacuolar membrane-localized MTs that export toxic elements into vacuole and also translocate in the root's tips and shoot. However, in case of drought, cold and heat stresses, MTs increased water and sugar supplies to all organs. In this review, we mainly review recent literature from Arabidopsis, halophytes and major field crops such as rice, wheat, maize and oilseed rape in order to argue the global role of MTs in PG&D, and abiotic stress tolerance. We also discussed gene expression level changes and genomic variations within a species as well as within a family in response to developmental and environmental cues.


Assuntos
Adaptação Fisiológica , Regulação da Expressão Gênica de Plantas , Proteínas de Membrana Transportadoras/metabolismo , Desenvolvimento Vegetal , Proteínas de Plantas/metabolismo , Plantas/metabolismo , Estresse Fisiológico , Transporte Biológico , Secas , Proteínas de Membrana Transportadoras/genética , Proteínas de Plantas/genética
6.
J Org Chem ; 85(13): 8352-8359, 2020 07 02.
Artigo em Inglês | MEDLINE | ID: mdl-32496068

RESUMO

The hydrolysis of carbonyl sulfide (COS) to form H2S by carbonic anhydrase has been demonstrated to be a viable strategy to deliver H2S in a biological system. Herein, we describe N-dithiasuccinoyl amines as thiol-triggered COS/H2S donors. Notably, thiol species especially GSH and homocysteine can trigger the release of both COS and H2S directly from several specific analogues via an unexpected mechanism. Importantly, two representative analogues Dts-1 and Dts-5 show intracellular H2S release, and Dts-1 imparts potent anti-inflammatory effects in LPS-challenged microglia cells. In conclusion, N-dithiasuccinoyl amine could serve as promising COS/H2S donors for either H2S biological studies or H2S-based therapeutics development.


Assuntos
Sulfeto de Hidrogênio , Compostos de Sulfidrila , Aminas , Óxidos de Enxofre
7.
Bioorg Chem ; 105: 104365, 2020 12.
Artigo em Inglês | MEDLINE | ID: mdl-33091669

RESUMO

Urease enzyme is responsible to catalyze the hydrolysis of urea into carbamate and ammonia. Then carbamate hydrolyzed to ammonia and carbon dioxide. Excess release of ammonia leads to increase pH in stomach that actually encourages the survival of Helicobacter pylori. H. pylori involves in various disorders most commonly peptic ulcer, pyelonephritis, hepatic coma, kidney stone formation, urolithiasis, and encephalopathy. Apart from many pharmacological properties, coumarin and Schiff bases are known to possess urease inhibitory activity. Therefore, these two pharmacologically important scaffolds are combined into single hybrid molecules to assess their potential as urease inhibitors. For this aim, N'-benzylidene-2-((2-oxo-2H-chromen-4-yl)oxy)acetohydrazide Schiff base derivatives 3-27 were synthesized by following a three step reaction strategy. Structures of all synthetic molecules were characterized by EI-MS, 1H-, and 13C NMR spectroscopic techniques. All molecules were assessed for urease inhibitory activity and found to possess a varying degree of inhibitory potential in the range of IC50 = 12.3 ± 0.69 to 88.8 ± 0.04 µM. Amongst the active analogs, compounds 7 (IC50 = 16.2 ± 0.11 µM), 9 (IC50 = 15.2 ± 0.14 µM), 10 (IC50 = 12.3 ± 0.69 µM), 12 (IC50 = 16.3 ± 0.45 µM), and 15 (IC50 = 17.6 ± 0.28 µM) were identified as potent inhibitors compared to standard urea (IC50 = 21.5 ± 0.47 µM). It is conferred from structure-activity relationship (SAR) that variation in inhibitory activity is due to different substitutions pattern on aryl ring. Moreover, molecular docking studies were carried out to understand the interactions of ligand with the active pocket of urease enzyme.


Assuntos
Cumarínicos/farmacologia , Inibidores Enzimáticos/farmacologia , Hidrazinas/farmacologia , Urease/antagonistas & inibidores , Cumarínicos/química , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Hidrazinas/síntese química , Hidrazinas/química , Simulação de Acoplamento Molecular , Estrutura Molecular , Bases de Schiff/síntese química , Bases de Schiff/química , Bases de Schiff/farmacologia , Relação Estrutura-Atividade , Urease/metabolismo
8.
Bioorg Chem ; 104: 104238, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-32911195

RESUMO

Thirty benzofuran-2-yl(phenyl)methanones 1-30 were synthesized and characterized their structures by spectroscopic techniques. Substituted phenacyl bromide and different derivatives of 2-hydroxy-benzaldehyde treated in the presence of anhydrous K2CO3 in acetonitrile at room temperature to afford the desired benzofurans 1-30. All compounds were screened for their in vitro α-amylase inhibitory and radical scavenging (DPPH and ABTS) activities. Results revealed that para substituted compounds were found to be more active than the others with IC50 values ranges for α-amylase inhibition (IC50 = 18.04-48.33 µM), DPPH (IC50 = 16.04-32.33 µM) and ABTS (IC50 = 16.99-33.01 µM) radical scavenging activities. Activities results were compared with the standards acarbose (IC50 = 16.08 ± 0.07 µM) for α-amylase, ascorbic acid (IC50 = 15.08 ± 0.03 and 15.09 ± 0.17 µM) for DPPH and ABTS radical scavenging activities, respectively. Kinetic studies predicted that all compounds followed non-competitive mechanism of inhibition. Molecular docking results showed good protein-ligand interactions profile against the corresponding target. To the best of our knowledge, out of thirty molecules, ten compounds 18-20, 22, and 25-30 were structurally new.


Assuntos
Benzofuranos/farmacologia , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/farmacologia , Simulação de Acoplamento Molecular , alfa-Amilases/antagonistas & inibidores , Benzofuranos/síntese química , Benzofuranos/química , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/química , Cinética , Estrutura Molecular , Picratos/antagonistas & inibidores , Relação Estrutura-Atividade , Ácidos Sulfônicos/antagonistas & inibidores , alfa-Amilases/metabolismo
9.
BMC Plant Biol ; 19(1): 507, 2019 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-31752690

RESUMO

BACKGROUND: The ubiquitous signaling molecule melatonin (N-acetyl-5-methoxytryptamine) (MT) plays vital roles in plant development and stress tolerance. Selenium (Se) may be phytotoxic at high concentrations. Interactions between MT and Se (IV) stress in higher plants are poorly understood. The aim of this study was to evaluate the defensive roles of exogenous MT (0 µM, 50 µM, and 100 µM) against Se (IV) (0 µM, 50 µM, 100 µM, and 200 µM) stress based on the physiological and biochemical properties, thiol biosynthesis, and antioxidant system of Brassica napus plants subjected to these treatments. RESULTS: Se (IV) stress inhibited B. napus growth and biomass accumulation, reduced pigment content, and lowered net photosynthetic rate (Pn) and PSII photochemical efficiency (Fv/Fm) in a dose-dependent manner. All of the aforementioned responses were effectively alleviated by exogenous MT treatment. Exogenous MT mitigated oxidative damage and lipid peroxidation and protected the plasma membranes from Se toxicity by reducing Se-induced reactive oxygen species (ROS) accumulation. MT also alleviated osmotic stress by restoring foliar water and sugar levels. Relative to standalone Se treatment, the combination of MT and Se upregulated the ROS-detoxifying enzymes SOD, APX, GR, and CAT, increased proline, free amino acids, and the thiol components GSH, GSSG, GSH/GSSG, NPTs, PCs, and cys and upregulated the metabolic enzymes γ-ECS, GST, and PCS. Therefore, MT application attenuates Se-induce oxidative damage in plants. MT promotes the accumulation of chelating agents in the roots, detoxifies Se there, and impedes its further translocation to the leaves. CONCLUSIONS: Exogenous MT improves the physiological traits, antioxidant system, and thiol ligand biosynthesis in B. napus subjected to Se stress primarily by enhancing Se detoxification and sequestration especially at the root level. Our results reveal better understanding of Se-phytotoxicity and Se-stress alleviation by the adequate supply of MT. The mechanisms of MT-induced plant tolerance to Se stress have potential implications in developing novel strategies for safe crop production in Se-rich soils.


Assuntos
Antioxidantes/metabolismo , Brassica napus/fisiologia , Melatonina/metabolismo , Reguladores de Crescimento de Plantas/metabolismo , Selênio/toxicidade , Compostos de Sulfidrila/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Oxirredução , Estresse Oxidativo , Folhas de Planta/fisiologia , Espécies Reativas de Oxigênio/metabolismo
10.
Inorg Chem ; 58(5): 3167-3174, 2019 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-30776223

RESUMO

The construction of metallosupramolecular complexes toward interesting topological structures is a critical challenge for chemists. The fluctuation in the synthetic strategy, by keeping the same metal-ligand combination, has proved a very significant approach to construct metallosupramolecular architectures. Herein, by varying the reaction conditions four new DyIII-supramolecular complexes based on a flexible dihydrazone ligand H2L (H2L = bis(2-hydroxy-3-methoxybenzylidene)adipohydrazide) in cooperation with different anions and solvents having formulas [Dy4L4(µ2-N3)2](NO3)2·6CH3OH·2H2O (1), [Dy8L8(µ2-CH3OH)4]Cl8·6CH3OH·14H2O (2), [Dy12L12(µ2-OH)2(OH)6(CH3O)2](NO3)2·2CH3OH·14H2O (3), and [Dy12L12(µ2-OH)2(NO3)2(OH)3(CH3O)](NO3)4·22H2O (4), have been successfully synthesized and their crystal structures confirmed by single crystal X-ray diffraction studies. The structural study reveals that 1 and 2 have quadruple-stranded helicate and dual triple-stranded helicate supramolecular structures, respectively, while 3 and 4 display "octahedron" cagelike supramolecular structures. The magnetic studies reveal that complexes 1-3 exhibit slow magnetic relaxation behavior, while complex 4 displays a series of typical frequency-dependent relaxation signals at 0 Oe applied dc field which is a rare case in polynuclear 4f single-molecule magnet (SMM) family to date. Interestingly, the distinct magnetic dynamic behavior was noticed for nearly isoskeletal complexes 3 and 4, which can be attributed to the modification of the coordination environment around DyIII ions.

11.
Bioorg Chem ; 82: 163-177, 2019 02.
Artigo em Inglês | MEDLINE | ID: mdl-30321779

RESUMO

Benzohydrazide derivatives 1-43 were synthesized via "one-pot" reaction and structural characterization of these synthetic derivatives was carried out by different spectroscopic techniques such as 1H NMR and EI-MS. The synthetic molecules were evaluated for their in vitro urease inhibitory activity. All synthetic derivatives showed good inhibitory activities in the range of (IC50 = 0.87 ±â€¯0.31-19.0 ±â€¯0.25 µM) as compared to the standard thiourea (IC50 = 21.25 ±â€¯0.15 µM), except seven compounds 17, 18, 23, 24, 29, 30, and 41 which were found to be inactive. The most active compound of the series was compound 36 (IC50 = 0.87 ±â€¯0.31 µM) having two chloro groups at meta positions of ring A and methoxy group at para position of ring B. The structure-activity relationship (SAR) of the active compounds was established on the basis of different substituents and their positions in the molecules. Kinetic studies of the active compounds revealed that compounds can inhibit enzyme via competitive and noncompetitive modes. In silico study was also performed to understand the binding interactions of the molecules (ligand) with the active site of enzyme.


Assuntos
Inibidores Enzimáticos/química , Hidrazinas/química , Urease/antagonistas & inibidores , Domínio Catalítico , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/farmacocinética , Hidrazinas/síntese química , Hidrazinas/farmacocinética , Ligação de Hidrogênio , Cinética , Simulação de Acoplamento Molecular , Estrutura Molecular , Eletricidade Estática , Relação Estrutura-Atividade , Urease/química
12.
Int J Phytoremediation ; 21(8): 760-767, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30656967

RESUMO

Phytoremediation is an important technique to remove heavy metals from contaminated soils due to its efficiency and cost-effectiveness. The present study was conducted to assess the synergistic role of 5-aminolevulinic acid (ALA) and citric acid (CA) in improving the phyto-extraction of chromium (Cr) by sunflower. Sunflower plants were grown in soil, spiked with different concentrations of Cr (0, 5, 10, 20 mg kg-1). Various concentrations of 5-ALA (0, 10, 20 mg L-1) and CA (0, 2.5, 5 mM) were applied exogenously at juvenile stage. A significant decrease was observed in biomass and agronomic traits of sunflower under Cr stress alone. Further, Cr toxicity significantly decreased the plant growth, soluble proteins and photosynthetic pigments. However, exogenously applied ALA and CA significantly improved the plants' physiological as well as agronomic attributes by lowering the production of reactive oxygen species and reducing electrolyte leakage. Moreover, Cr uptake was increased with increasing concentration of Cr in spiked soil, which was further enhanced by combined application of ALA and CA.


Assuntos
Helianthus , Poluentes do Solo , Ácido Aminolevulínico , Antioxidantes , Biodegradação Ambiental , Biomassa , Cromo , Ácido Cítrico , Fotossíntese , Solo
13.
Pak J Pharm Sci ; 32(1): 15-19, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30772785

RESUMO

This research based on the anti-inflammatory and antiplatelet aggregation properties of some new thiazolyl hydrazone derivatives of 1-indanone. In this regard a thiosemicabazone and twelve thiazolyl derivatives of 1-indanone have been synthesized. Out of these synthetic compounds seven derivatives 1-3, 6, 11-13 exhibited varying degree of anti-inflammatory action with IC50 esteems going from 5.1±1.3 - 78.8±4.6µM/mL. Compound 1 (IC50 =5.1±1.9µM) displayed potent result than standard ibuprofen (IC50 = 11.2±1.9 µM). In antiplatelet aggregation assay, five compounds 1, 5, 6, 8 and 11 were observed to be dynamic with IC50 esteems observed in the range of 38.34-255.7±4.1µM, wher eas, aspirin (IC50 = 30.3±2.6 µM) was used as standard. However, compound 11 was found to be good active for both anti-inflammatory and antiplatelet aggregation activities (IC50 = 13.9±4.9µg/mL) (IC50 = 38.60±3.1µM), respectively.


Assuntos
Anti-Inflamatórios/farmacologia , Hidrazonas/farmacologia , Indanos/farmacologia , Inibidores da Agregação Plaquetária/farmacologia , Agregação Plaquetária/efeitos dos fármacos , Explosão Respiratória/efeitos dos fármacos , Anti-Inflamatórios/síntese química , Relação Dose-Resposta a Droga , Humanos , Hidrazonas/síntese química , Ibuprofeno/farmacologia , Indanos/síntese química , Estrutura Molecular , Inibidores da Agregação Plaquetária/síntese química , Relação Estrutura-Atividade , Tiossemicarbazonas/síntese química
14.
Plant Cell Environ ; 41(12): 2882-2898, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30107647

RESUMO

Monitoring of ozone damage to crops plays an increasingly important role for the food security of many developing countries. Ethylenediurea (EDU) could be a tool to assess ozone damage to vegetation on field scale, but its physiological mode of action remains unclear. This study investigated mechanisms underlying the ozone-protection effect of EDU in controlled chamber experiments. Ozone sensitive and tolerant rice genotypes were exposed to ozone (108 ppb, 7 hr day-1 ) and control conditions. EDU alleviated ozone effects on plant morphology, foliar symptoms, lipid peroxidation, and photosynthetic parameters in sensitive genotypes. Transcriptome profiling by RNA sequencing revealed that thousands of genes responded to ozone in a sensitive variety, but almost none responded to EDU. Significant interactions between ozone and EDU application occurred mostly in ozone responsive genes, in which up-regulation was mitigated by EDU application. Further experiments documented ozone degrading properties of EDU, as well as EDU deposits on leaf surfaces possibly related to surface protection. EDU application did not mitigate the reaction of plants to other abiotic stresses, including iron toxicity, zinc deficiency, and salinity. This study provided evidence that EDU is a surface protectant that specifically mitigates ozone stress without interfering directly with the plants' stress response systems.


Assuntos
Oryza/metabolismo , Ozônio/antagonistas & inibidores , Compostos de Fenilureia/farmacologia , Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas , Ferro/metabolismo , Microscopia Eletrônica de Varredura , Oryza/efeitos dos fármacos , Ozônio/metabolismo , Fotossíntese , Estresse Salino , Estresse Fisiológico/efeitos dos fármacos , Zinco/deficiência
15.
Bioorg Chem ; 79: 363-371, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29859384

RESUMO

A series of 1-[(4'-chlorophenyl)carbonyl-4-(aryl)thiosemicarbazide derivatives 1-25 was synthesized and characterized by spectroscopic techniques such as EI-MS and 1H NMR. All compounds were screened for urease inhibitory activity in vitro and demonstrated excellent inhibitory activity in the range of IC50 = 0.32 ±â€¯0.01-25.13 ±â€¯0.13 µM as compared to the standard thiourea (IC50 = 21.25 ±â€¯0.13 µM). Amongst the potent analogs, compounds 3 (IC50 = 2.31 ±â€¯0.01 µM), 6 (IC50 = 2.14 ±â€¯0.04 µM), 10 (IC50 = 1.14 ±â€¯0.06 µM), 20 (IC50 = 2.15 ±â€¯0.05 µM), and 25 (IC50 = 0.32 ±â€¯0.01 µM) are many folds more active than the standard. Structure-activity relationship (SAR) was rationalized by looking at the effect of diversely substituted aryl ring on inhibitory potential which predicted that regardless of the nature of substituents, their positions on aryl ring is worth important for the potent activity. Furthermore, to verify these interpretations, in silico study was performed on all compounds and a good correlation was perceived between the biological evaluation and docking study of compounds.


Assuntos
Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Semicarbazidas/farmacologia , Urease/antagonistas & inibidores , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Humanos , Estrutura Molecular , Semicarbazidas/síntese química , Semicarbazidas/química , Relação Estrutura-Atividade , Urease/metabolismo
16.
Bioorg Chem ; 79: 34-45, 2018 09.
Artigo em Inglês | MEDLINE | ID: mdl-29723741

RESUMO

Nicotinic and isonicotinic thiosemicarbazide or hydrazine carbothioamides 3-27 were synthesized and the structures of synthetic compounds were elucidated by various spectroscopic techniques such as EI-MS, 1H-, and 13C NMR. Synthetic derivatives were evaluated for their urease inhibitory activity which revealed that except few all derivatives demonstrated excellent inhibition in the range of IC50 values of 1.21-51.42 µM as compared to the standard thiourea (IC50 = 21.25 ±â€¯0.13 µM). Among the twenty-five synthetic derivatives nineteen 1-5, 7, 8, 10, 12, 14-18, 20-22, 24-27 were found to be more active showing IC50 values between 1.13 and 19.74 µM showing superior activity than the standard. Limited structure-activity relationship demonstrated that the positions of substituent as well as position of nitrogen in pyridine ring are very important for inhibitory activity of this class of compound. To verify these interpretations, in silico study was also performed. A good correlation was obtained between the biological evaluation of active compounds and docking study.


Assuntos
Inibidores Enzimáticos/química , Ácidos Isonicotínicos/química , Ácidos Nicotínicos/química , Tiossemicarbazonas/química , Canavalia/enzimologia , Domínio Catalítico , Inibidores Enzimáticos/síntese química , Ácidos Isonicotínicos/síntese química , Simulação de Acoplamento Molecular , Estrutura Molecular , Ácidos Nicotínicos/síntese química , Relação Estrutura-Atividade , Tiossemicarbazonas/síntese química , Urease/química
17.
Mol Divers ; 22(4): 841-861, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29948581

RESUMO

This study is focused on the identification of thiazole-based inhibitors for the [Formula: see text]-glucosidase enzyme. For that purpose, (E)-2-(2-(arylmethylene)hydrazinyl)-4-arylthiazole derivatives were synthesized in two steps and characterized by various spectroscopic techniques. All derivatives and intermediates were evaluated for their in vitro [Formula: see text]-glucosidase inhibitory activity. Thiosemicarbazones 20 and 35, and cyclized thiazole derivatives 2, 5-11, 13, 15, 21-24, 27-31, and 36-37 showed significant inhibitory potential in the range of [Formula: see text]-[Formula: see text] as compared to standard acarbose ([Formula: see text]). A molecular modeling study was carried out to understand the binding interactions of compounds with the active site of enzyme.


Assuntos
Simulação por Computador , Glucosidases/antagonistas & inibidores , Tiazóis/síntese química , Tiazóis/farmacologia , Tiossemicarbazonas/síntese química , Tiossemicarbazonas/farmacologia , Técnicas de Química Sintética , Desenho de Fármacos , Glucosidases/química , Glucosidases/metabolismo , Simulação de Acoplamento Molecular , Conformação Proteica , Relação Estrutura-Atividade , Tiazóis/química , Tiazóis/metabolismo , Tiossemicarbazonas/química , Tiossemicarbazonas/metabolismo
18.
Int J Mol Sci ; 18(9)2017 Sep 14.
Artigo em Inglês | MEDLINE | ID: mdl-28906478

RESUMO

To uncover the alleviation mechanism of quinclorac stress by salicylic acid (SA), leaf samples of Oryza sativa ssp. Japonica under quinclorac stress with and without SA pre-treatment were analyzed for transcriptional and proteomic profiling to determine the differentially expressed genes (DEGs) and proteins (DEPs), respectively. Results showed that quinclorac stress altered the expression of 2207 DEGs (1427 up-regulated, 780 down-regulated) and 147 DEPs (98 down-regulated, 49 up-regulated). These genes and proteins were enriched in glutathione (GSH) metabolism, porphyrin and chlorophyll metabolism, the biosynthesis of secondary metabolites, glyoxylate and dicarboxylate metabolism, and so on. It also influenced apetala2- ethylene-responsive element binding protein (AP2-EREBP) family, myeloblastosis (MYB) family and WRKY family transcription factors. After SA pre-treatment, 697 genes and 124 proteins were differentially expressed. Pathway analysis showed similar enrichments in GSH, glyoxylate and dicarboxylate metabolism. Transcription factors were distributed in basic helix-loop-helix (bHLH), MYB, Tify and WRKY families. Quantitative real-time PCR results revealed that quinclorac stress induced the expression of glutathion reductase (GR) genes (OsGR2, OsGR3), which was further pronounced by SA pre-treatment. Quinclorac stress further mediated the accumulation of acetaldehyde in rice, while SA enhanced the expression of OsALDH2B5 and OsALDH7 to accelerate the metabolism of herbicide quinclorac for the protection of rice. Correlation analysis between transcriptome and proteomics demonstrated that, under quinclorac stress, correlated proteins/genes were mainly involved in the inhibition of intermediate steps in the biosynthesis of chlorophyll. Other interesting proteins/genes and pathways regulated by herbicide quinclorac and modulated by SA pre-treatment were also discussed, based on the transcriptome and proteomics results.


Assuntos
Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Oryza/genética , RNA Complementar , Análise de Sequência de RNA , Estresse Fisiológico/genética , Transcriptoma , Biologia Computacional/métodos , Perfilação da Expressão Gênica/métodos , Ontologia Genética , Herbicidas/farmacologia , Metabolômica/métodos , Oryza/metabolismo , Proteômica/métodos , Quinolinas/farmacologia , Ácido Salicílico/farmacologia , Estresse Fisiológico/efeitos dos fármacos
19.
J Integr Plant Biol ; 59(7): 496-505, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-28267270

RESUMO

The plant hormone auxin plays a crucial role in lateral root development. To better understand the molecular mechanisms underlying lateral root formation, an auxin-responsive gene OsCYP2 (Os02g0121300) was characterized from rice. Compared to the wild type, OsCYP2-RNAi (RNA interference) lines exhibited distinctive defects in lateral root development. Yeast two-hybrid and glutathione S-transferase pull-down results confirmed that OsCYP2 interacted with a C2HC-type zinc finger protein (OsZFP, Os01g0252900) which is located in the rice nucleus. T2 OsZFP-RNAi lines had significantly fewer lateral roots than did wild-type plants, which suggests a role for OsCYP2 and OsZFP in regulating lateral root development. Quantitative real-time polymerase chain reaction showed that the expression of certain Aux/IAA (auxin/indole-3-acetic acid) genes was altered in OsCYP2- and OsZFP-RNAi lines in response to IAA. These findings imply that OsCYP2 and OsZFP participate in IAA signal pathways controlling lateral root development. More importantly, OsIAA11 showed functional redundancy not only in OsCYP2-RNAi lines but also in OsZFP-RNAi lines, which provides important clues for the elucidation of mechanisms controlling lateral root development in response to auxin.


Assuntos
Ácidos Indolacéticos/metabolismo , Oryza/crescimento & desenvolvimento , Oryza/metabolismo , Proteínas de Plantas/metabolismo , Raízes de Plantas/crescimento & desenvolvimento , Raízes de Plantas/metabolismo , Ciclofilinas/metabolismo , Regulação da Expressão Gênica de Plantas , Oryza/genética , Proteínas de Plantas/genética , Raízes de Plantas/genética , Ligação Proteica , Dedos de Zinco
20.
BMC Genomics ; 17(1): 885, 2016 11 07.
Artigo em Inglês | MEDLINE | ID: mdl-27821044

RESUMO

BACKGROUND: Chromium (Cr) being multifarious industrial used element, is considered a potential environmental threat. Cr found to be a prospective water and soil pollutant, and thus it is a current area of concern. Oilseed rape (Brassica napus L.) is well known as a major source of edible oil around the globe. Due to its higher growth, larger biomass and capability to uptake toxic materials B. napus is considered a potential candidate plant against unfavorable conditions. To date, no study has been done that described the Cr and GSH mechanism at RNA-Seq level. RESULTS: Both digital gene expression (DGE) and transcriptome profile analysis (TPA) approaches had opened new insights to uncover the several number of genes related to Cr stress and GSH alleviating mechanism in two leading cultivars (ZS 758 and Zheda 622) of B. napus plants. Data showed that Cr inhibited KEGG pathways i.e. stilbenoid, diarlyheptanoid and gingerol biosynthesis; limonene and pentose degradation and glutathione metabolism in ZS 758; and ribosome and glucosinolate biosynthesis in Zheda-622. On the other hand, vitamin B6, tryptophan, sulfur, nitrogen and fructose and manose metabolisms were induced in ZS 758, and zeatin biosynthesis, linoleic acid metabolism, arginine and proline metabolism, and alanine, asparate and glutamate metabolism pathways in Zheda 622. Cr increased the TFs that were related to hydralase activity, antioxidant activity, catalytic activity phosphatase and pyrophosphatase activity in ZS 758, and vitamin binding and oxidoreductase activity in Zheda 622. Cr also up-regulated the promising proteins related to intracellular membrane bounded organelles, nitrile hyrdatase activity, cytoskeleton protein binding and stress response. It also uncovered, a novel Cr-responsive protein (CL2535.Contig1_All) that was statistically increased as compared to control and GSH treated plants. Exogenously applied GSH successfully not only recovered the changes in metabolic pathways but also induced cysteine and methionine metabolism in ZS 758 and ubiquinone and other terpenoid-quinone biosynthesis pathways in Zheda 622. Furthermore, GSH increased the level of TFs i.e. the gene expression of antioxidant and catalytic activities, iron ion binding and hydrolase activity as compared with Cr. Moreover, results pointed out a novel GSH responsive protein (CL827.Contig3_All) whose expression was found to be significantly increased when compared than Cr stress. Results further delineated that GSH induced TFs such as glutathione disulphide oxidoreducatse and aminoacyl-tRNA ligase activity, and beta glucosidase activity in ZS 758. Similarly in Zheda 622, GSH induced the TFs for instance DNA binding and protein dimerization activity. GSH also highlighted the proteins that were involved in transportation, photosynthesis process, RNA polymerase activity, and against the metal toxicity. These results indicated that cultivar ZS 758 had better metabolism and showed higher tolerance against Cr toxicity. CONCLUSION: The responses of ZS 758 and Zheda 622 differed considerably at both physiological and transcriptional level. Moreover, RNA-Seq method explored the hazardous behavior of Cr as well as GSH up-regulating mechanism by activating plant metabolism, stress responsive genes, TFs and protein encyclopedia.


Assuntos
Brassica napus/efeitos dos fármacos , Brassica napus/fisiologia , Cromo/toxicidade , Glutationa/metabolismo , Intoxicação por Metais Pesados , Intoxicação/genética , Intoxicação/metabolismo , Transcriptoma , Biomassa , Análise por Conglomerados , Biologia Computacional/métodos , Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas , Ontologia Genética , Redes e Vias Metabólicas , Metais Pesados/metabolismo , Mapeamento de Interação de Proteínas , Estresse Fisiológico/genética
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