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1.
Pak J Pharm Sci ; 32(1): 61-68, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-30772791

RESUMO

In the current research work, a series of new N-(alkyl/aralkyl)-N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamides has been synthesized by reacting 1,4-benzozzdioxan-6-amine (1) with 4-chlorobenzenesulfonyl chloride (2) to yield N-(2,3-dihydro-1,4-benzodioxan-6-yl)-4-chlorobenzenesulfonamide (3) which was further reacted with different alkyl/aralkyl halides (4a-n) to afford the target compounds (5a-n). Structures of the synthesized compounds were confirmed by IR, 1H-NMR, EI-MS spectral techniques and CHN analysis data. The results of enzyme inhibition showed that the molecules, N-2-phenethyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5j) and N-(1-butyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5d), exhibited moderate inhibitory potential against acetylcholinesterase with IC50 values 26.25±0.11 µM and 58.13±0.15 µM respectively, whereas, compounds N-benzyl-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5i) and N-(pentane-2-yl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-chlorobenzenesulfonamide (5f) showed moderate inhibition against α-glucosidase enzyme as evident from IC50 values 74.52±0.07 and 83.52±0.08 µM respectively, relative to standards Eserine having IC50 value of 0.04±0.0001 µM for cholinesterases and Acarbose having IC50 value 38.25±0.12 µM for α-glucosidase, respectively.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/farmacologia , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/farmacologia , Sulfonamidas/síntese química , Sulfonamidas/farmacologia , Acetilcolinesterase/metabolismo , Doença de Alzheimer/enzimologia , Butirilcolinesterase/metabolismo , Diabetes Mellitus Tipo 2/enzimologia , Espectrometria de Massas , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Relação Estrutura-Atividade , alfa-Glucosidases/metabolismo
2.
Ecotoxicol Environ Saf ; 151: 255-265, 2018 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-29353175

RESUMO

Soil contamination with heavy metals is threatening the food security around the globe. Chromium (Cr) contamination results in poor quality and reduction in yield of crops. The present research was performed to figure out the Cr toxicity in sunflower and the ameliorative role of 5-aminolevulinic acid (ALA) as a plant growth regulator. The sunflower (FH-614) was grown under increasing concentration of Cr (0, 5, 10 and 20mgkg-1) alone and/or in combination with 5-ALA (0, 10 and 20mgL-1). Results showed that Cr suppressed the overall growth, biomass, gas exchange attributes and chlorophyll content of sunflower plants. Moreover, lower levels of Cr (5 and 10mgkg-1) increased the production of reactive oxygen species (ROS) and electrolyte leakage (EL) along with the activities of antioxidant enzymes i.e., superoxide dismutase (SOD), guaiacole peroxidase (POD), ascorbate (APX), catalase (CAT). But at higher concentration of Cr (20mgkg-1), the activities of these enzymes presented a declining trend. However, the addition of 5-ALA significantly alleviated the Cr-induced toxicity in sunflower plant and enhanced the plant growth and biomass parameters along with increased chlorophyll content, gas exchange attributes, soluble proteins and soil plant analysis development (SPAD) values by scavenging the ROS and lowering down the EL. The 5-ALA also enhanced the activities of antioxidant enzymes at all levels of Cr. The increase in Cr concentration in all plant parts such as leaf, root and stem was directly proportional to the Cr concentration in soil. The application of 5-ALA further enhanced the uptake of Cr and its concentration in the plants. To understand this variation in response of plants to 5-ALA, detailed studies are required on plant biochemistry and genetic modifications.


Assuntos
Ácido Aminolevulínico/farmacologia , Cromo/toxicidade , Helianthus/metabolismo , Reguladores de Crescimento de Plantas/farmacologia , Poluentes do Solo/toxicidade , Catalase/metabolismo , Clorofila/análise , Cromo/análise , Relação Dose-Resposta a Droga , Helianthus/efeitos dos fármacos , Peroxidase/metabolismo , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/metabolismo , Raízes de Plantas/efeitos dos fármacos , Raízes de Plantas/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Poluentes do Solo/análise , Estresse Fisiológico , Superóxido Dismutase/metabolismo
3.
Pak J Pharm Sci ; 30(1): 105-112, 2017 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-28603120

RESUMO

The purpose of the present investigation was to assess the enzyme inhibition, antifungal, antibacterial and hemolytic activities of various fractions of Colebrookia oppositifolia Smith. The MeOH extract of plant was dissolved in dist. water and partitioned with n-hexane, CHCl3, EtOAc and n-BuOH sequentially. Enzyme inhibition studies were done against four enzymes i.e. α-glucosidase, butyrylcholinesterase, acetyl cholinesterase and lipoxygenase. Ethyl acetate fraction possessed very good activity against α-glucosidase (IC50 57.38±1.23µg/mL). CHCl3 fraction displayed good activity against α-glucosidase and lipoxygenase while moderate activity against butyryl cholinesterase. EtOAc fraction displayed good activity against lipoxygenase. Antifungal activity was studied against four fungi i.e. Aspergillus niger, Aspergillus flavus, Ganoderma lucidum and Alternaria alternata by the disc diffusion method using fluconazole, a standard antifungal drug, as positive control. Aqueous fraction displayed good activity against G. lucidum and A. flavus. Antibacterial activity was checked against Staphylococcus aureus, Bacillus subtilis, Pasturella multocida and Escherichia coli by the disc diffusion method using streptomycin sulphate, a standard antibiotic, as positive control. Chloroform, ethyl acetate and aqueous fraction showed good activity against E. coli. Chloroform fraction showed good activity against B. subtilis. Ethyl acetate fraction showed good activity against the P. multocida. All the studied fractions showed very less toxicity i.e. < 7%.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Inibidores Enzimáticos/farmacologia , Hemólise/efeitos dos fármacos , Lamiaceae/química , Solventes/química , Acetilcolinesterase/metabolismo , Antibacterianos/isolamento & purificação , Antibacterianos/toxicidade , Antifúngicos/isolamento & purificação , Antifúngicos/toxicidade , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Testes de Sensibilidade a Antimicrobianos por Disco-Difusão , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/toxicidade , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Humanos , Lamiaceae/toxicidade , Inibidores de Lipoxigenase/isolamento & purificação , Inibidores de Lipoxigenase/farmacologia , Fitoterapia , Plantas Medicinais
4.
Environ Sci Pollut Res Int ; 22(15): 11679-89, 2015 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25850739

RESUMO

Chromium (Cr) toxicity is widespread in crops grown on Cr-contaminated soils and has become a serious environmental issue which requires affordable strategies for the remediation of such soils. This study was performed to assess the performance of citric acid (CA) through growing Brassica napus in the phytoextraction of Cr from contaminated soil. Different Cr (0, 100, and 500 µM) and citric acid (0, 2.5, and 5.0 mM) treatments were applied alone and in combinations to 4-week-old seedlings of B. napus plants in soil under wire house condition. Plants were harvested after 12 weeks of sowing, and the data was recorded regarding growth characteristics, biomass, photosynthetic pigments, malondialdehyde (MDA), electrolytic leakage (EL), antioxidant enzymes, and Cr uptake and accumulation. The results showed that the plant growth, biomass, chlorophyll contents, and carotenoid as well as soluble protein concentrations significantly decreased under Cr stress alone while these adverse effects were alleviated by application of CA. Cr concentration in roots, stem, and leaves of CA-supplied plant was significantly reduced while total uptake of Cr increased in all plant parts with CA application. Furthermore, in comparison with Cr treatments alone, CA supply reduced the MDA and EL values in both shoots and roots. Moreover, the activity of superoxide dismutase (SOD), guaiacol peroxidase (POD), catalase (CAT), and ascorbate peroxidase (APX) in shoots and roots markedly increased by 100 µM Cr exposure, while decreased at 500 µM Cr stress. CA application enhanced the activities of antioxidant enzymes compared to the same Cr treatment alone. Thus, the data indicate that exogenous CA application can increase Cr uptake and can minimize Cr stress in plants and may be beneficial in accelerating the phytoextraction of Cr through hyper-accumulating plants such as B. napus.


Assuntos
Brassica napus/crescimento & desenvolvimento , Brassica napus/metabolismo , Cromo/isolamento & purificação , Ácido Cítrico/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Fotossíntese/efeitos dos fármacos , Poluentes do Solo/isolamento & purificação , Antioxidantes/metabolismo , Biodegradação Ambiental/efeitos dos fármacos , Brassica napus/efeitos dos fármacos , Brassica napus/enzimologia , Clorofila/metabolismo , Cromo/metabolismo , Relação Dose-Resposta a Droga , Malondialdeído/metabolismo , Poluentes do Solo/metabolismo
5.
Environ Sci Pollut Res Int ; 22(2): 1534-44, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25163559

RESUMO

Copper (Cu) is an essential micronutrient for normal plant growth and development, but in excess, it is also toxic to plants. The present study investigated the influence of ethylenediaminetetraacetic acid (EDTA) in enhancing Cu uptake and tolerance as well as the morphological and physiological responses of Brassica napus L. seedlings under Cu stress. Four-week-old seedlings were transferred to hydroponics containing Hoagland's nutrient solution. After 2 weeks of transplanting, three levels (0, 50, and 100 µM) of Cu were applied with or without application of 2.5 mM EDTA and plants were further grown for 8 weeks in culture media. Results showed that Cu alone significantly decreased plant growth, biomass, photosynthetic pigments, and gas exchange characteristics. Cu stress also reduced the activities of antioxidants, such as superoxide dismutase (SOD), peroxidase (POD), ascorbate peroxidase (APX), and catalase (CAT) along with protein contents. Cu toxicity increased the concentration of reactive oxygen species (ROS) as indicated by the increased production of malondialdehyde (MDA) and hydrogen peroxide (H2O2) in both leaves and roots. The application of EDTA significantly alleviated Cu-induced toxic effects in B. napus, showing remarkable improvement in all these parameters. EDTA amendment increased the activity of antioxidant enzymes by decreasing the concentrations of MDA and H2O2 both in leaves and roots of B. napus. Although, EDTA amendment with Cu significantly increased Cu uptake in roots, stems, and leaves in decreasing order of concentration but increased the growth, photosynthetic parameters, and antioxidant enzymes. These results showed that the application of EDTA can be a useful strategy for phytoextraction of Cu by B. napus from contaminated soils.


Assuntos
Brassica napus/efeitos dos fármacos , Cobre/farmacocinética , Ácido Edético/farmacologia , Poluentes do Solo/farmacocinética , Análise de Variância , Ascorbato Peroxidases/metabolismo , Biodegradação Ambiental , Brassica napus/crescimento & desenvolvimento , Brassica napus/metabolismo , Catalase/metabolismo , Clorofila/metabolismo , Cobre/administração & dosagem , Cobre/toxicidade , Peróxido de Hidrogênio/metabolismo , Hidroponia , Malondialdeído/metabolismo , Folhas de Planta/metabolismo , Raízes de Plantas/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Plântula/efeitos dos fármacos , Plântula/crescimento & desenvolvimento , Poluentes do Solo/toxicidade , Superóxido Dismutase/metabolismo
6.
ScientificWorldJournal ; 2014: 607091, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25401149

RESUMO

Narrow genetic base and complex allotetraploid genome of cotton (Gossypium hirsutum L.) is stimulating efforts to avail required polymorphism for marker based breeding. The availability of draft genome sequence of G. raimondii and G. arboreum and next generation sequencing (NGS) technologies facilitated the development of high-throughput marker technologies in cotton. The concepts of genetic diversity, QTL mapping, and marker assisted selection (MAS) are evolving into more efficient concepts of linkage disequilibrium, association mapping, and genomic selection, respectively. The objective of the current review is to analyze the pace of evolution in the molecular marker technologies in cotton during the last ten years into the following four areas: (i) comparative analysis of low- and high-throughput marker technologies available in cotton, (ii) genetic diversity in the available wild and improved gene pools of cotton, (iii) identification of the genomic regions within cotton genome underlying economic traits, and (iv) marker based selection methodologies. Moreover, the applications of marker technologies to enhance the breeding efficiency in cotton are also summarized. Aforementioned genomic technologies and the integration of several other omics resources are expected to enhance the cotton productivity and meet the global fiber quantity and quality demands.


Assuntos
Cruzamento/métodos , Marcadores Genéticos/genética , Variação Genética/genética , Gossypium/genética , Previsões , Genômica , Polimorfismo de Nucleotídeo Único/genética
7.
Ecotoxicol Environ Saf ; 109: 38-47, 2014 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-25164201

RESUMO

Phytoextraction is an environmentally friendly and a cost-effective strategy for remediation of heavy metal contaminated soils. However, lower bioavailability of some of the metals in polluted environments e.g. lead (Pb) is a major constraint of phytoextraction process that could be overcome by applying organic chelators. We conducted a glasshouse experiment to evaluate the role of citric acid (CA) in enhancing Pb phytoextraction. Brassica napus L. seedlings were grown in hydroponic media and exposed to various treatments of Pb (50 and 100 µM) as alone or in combination with CA (2.5mM) for six weeks. Pb-induced damage in B. napus toxicity was evident from elevated levels of malondialdehyde (MDA) and H2O2 that significantly inhibited plant growth, biomass accumulation, leaf chlorophyll contents and gas exchange parameters. Alternatively, CA application to Pb-stressed B. napus plants arrested lipid membrane damage by limiting MDA and H2O2 production and by improving antioxidant enzyme activities. In addition, CA significantly increased the Pb accumulation in B. napus plants. The study concludes that CA has a potential to improve Pb phytoextraction without damaging plant growth.


Assuntos
Brassica napus/efeitos dos fármacos , Ácido Cítrico/farmacologia , Chumbo/metabolismo , Poluentes do Solo/análise , Biodegradação Ambiental , Biomassa , Brassica napus/química , Brassica napus/enzimologia , Brassica napus/metabolismo , Clorofila/metabolismo , Peróxido de Hidrogênio/metabolismo , Chumbo/análise , Malondialdeído/metabolismo , Oxirredutases/metabolismo , Folhas de Planta/química , Folhas de Planta/efeitos dos fármacos , Folhas de Planta/metabolismo , Raízes de Plantas/química , Raízes de Plantas/efeitos dos fármacos , Raízes de Plantas/metabolismo , Caules de Planta/química , Caules de Planta/efeitos dos fármacos , Caules de Planta/metabolismo , Plântula/efeitos dos fármacos , Plântula/metabolismo , Poluentes do Solo/isolamento & purificação , Espectrofotometria Atômica
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