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1.
Bo Ram Kim Ji-Young Park Hyung Jae Jeong Hyung-Jun Kwon Su-Jin Park In-Chul Lee 《Journal of enzyme inhibition and medicinal chemistry》2018,33(1):1256-1265
Sialidases are key virulence factors that remove sialic acid from the host cell surface glycan, unmasking receptors that facilitate bacterial adherence and colonisation. In this study, we developed potential agents for treating bacterial infections caused by Streptococcus pneumoniae Nan A that inhibit bacterial sialidase using Turmeric and curcumin analogues. Design, synthesis, and structure analysis relationship (SAR) studies have been also described. Evaluation of the synthesised derivatives demonstrated that compound 5e was the most potent inhibitor of S. pneumoniae sialidase (IC50?=?0.2?±?0.1?µM). This compound exhibited a 3.0-fold improvement in inhibitory activity over that of curcumin and displayed competitive inhibition. These results warrant further studies confirming the antipneumococcal activity 5e and indicated that curcumin derivatives could be potentially used to treat sepsis by bacterial infections. 相似文献
2.
Latika P. Chanderkar Gouri Shanker Robert L. Knobler Fred D. Lublin Woon Ki Paik Sangduk Kim 《Neurochemical research》1987,12(5):445-449
Mice with the dysmyelinating mutation shiverer were studied by measuring the activity of two protein methylases and myelin marker enzymes in the brain. It was observed thatS-adenosylmethionine: protein-lysineN-methyltransferase (protein methylase III, EC. 2.1.1.43) activity is significantly reduced in phenotypically affected homozygous shiverer (shi/shi) mutant mouse brain compared to the unaffected heterozygous littermate brain. This reduction in enzyme activity is manifested mainly by reduced formation of trimethyllysine during the in vitro methylation of histone. In contrast, myelin marker enzymes such as 2,3-cyclic nucleotide 3-phosphohydrolase and 5-nucleotidase as well asS-adenosyl-methionine: protein-carboxylO-methyltransferase (protein methylase II, EC. 2.1.1.24) activities were not significantly affected in these strains of mice. 相似文献
3.
The experiment was conducted to investigate the human thermoregulatory responses during rest, exercise and recovery atT
a 20°C and 60% R.H. under the conditions of wearing two different types of clothing. Six healthy men wore two types of clothing: one covering the whole body area except the head (Type A, weight 1656 g), and the other covering only the trunk, upper arms and thighs (Type B, weight 996 g). The level of rectal temperature was kept significantly higher in Type B than in Type A during rest and recovery. The increased and decreased rates of rectal temperature during exercise and recovery were significantly greater in Type A than in Type B, respectively. These findings are discussed from the viewpoint of the differences of skin temperatures of the extremities between Type A and Type B. 相似文献
4.
Receptor activation of G proteins 总被引:6,自引:0,他引:6
E R Weiss D J Kelleher C W Woon S Soparkar S Osawa L E Heasley G L Johnson 《FASEB journal》1988,2(13):2841-2848
G proteins are a highly conserved family of membrane-associated proteins composed of alpha, beta, and gamma subunits. The alpha subunit, which is unique for each G protein, binds GDP or GTP. Receptors such as those for beta- and alpha-adrenergic catecholamines, muscarinic agonists, and the retinal photoreceptor rhodopsin, catalyze the exchange of GDP for GTP binding to the alpha subunit of a specific G protein. G alpha.GTP regulates appropriate effector enzymes such as adenylyl cyclase or the cyclic GMP phosphodiesterase. The beta gamma-subunit complex of G proteins is required for efficient receptor-catalyzed alpha subunit guanine nucleotide exchange and also functions as an attenuator of alpha subunit activation of effector enzymes. Recent elucidation of both receptor and G protein primary sequence has allowed structural predictions and new experimental approaches to study the mechanism of receptor-catalyzed G protein regulation of specific effector systems and the control of cell function including metabolism, secretion, and growth. 相似文献
5.
M P Czech B M Clancy A Pessino C W Woon S A Harrison 《Trends in biochemical sciences》1992,17(5):197-201
Facilitated sugar entry into mammalian cells is catalysed by multiple isoforms of the glucose transporter and regulated by hormonal stimuli, nutritional status and oncogenesis. A large reserve of latent glucose transport capacity must be maintained by muscle and adipose cells that are sensitive to insulin, the primary activator of sugar uptake after feeding. Intracellular sequestration of sugar transporters accounts for a large part of this latent capacity, but new findings suggest that there is also reversible suppression of intrinsic catalytic activity of those glucose transporters residing at the cell surface. The mechanism of this suppression appears to be occlusion or disruption of the exofacial sugar-binding sites on the glucose-transporter proteins. 相似文献
6.
The foodborne pathogenStaphylococcus aureus is distinguished by its ability to grow within environments of extremely high osmolarity (e.g., foods with low water activity values). In the present study, we examined the accumulation of intracellular organic solutes withinS. aureus strain ATCC 12600 when cells were grown in a complex medium containing high concentrations of NaCl. Consistent with previous reports [Measures JC (1975) Nature 257:398–400; Koujima I, et al. (1978) Appl Environ Microbiol 35:467–470; and Anderson CB, Witter LD (1982) Appl Environ Microbiol 43:1501–1503], intracellular proline was found to accumulate to high concentrations. However, NMR spectroscopy of cell extracts revealed glycine betaine to be the predominant intracellular organic solute accumulated within cells grown at high osmolarity. In additional experiments, we examined the growth rate ofS. aureus in a defined medium of high osmolarity and found it to be stimulated significantly by the presence of either exogenous proline or glycine betaine. Highest growth rates were obtained when the defined medium was supplemented with glycine betaine. 相似文献
7.
S. O. Hwang G. H. Gil Y. J. Cho K. R. Kang J. H. Lee J. C. Bae 《Applied microbiology and biotechnology》1985,22(2):108-113
Summary A process for l-phenylalanine production was studied using a tyrosine auxotrophic regulatory mutant of Escherichia coli, resistant to both -2-thienyl-dl-alanine and p-fluoro-dl-phenylalanine. Fermentations were carried out in a 30-1 fermentor with intermittent feeding of glucose plus phosphate. The mutant accumulated l-phenylalanine in the fermentation broth up to 15 g/l at pH 7.0 and 33°C. Column chromatography on a strong cation exchanger was employed as the most effective step in the purification of l-phenyl-alanine from the broth. This step brought about 4-fold concentration of the product with 96% recovery. 相似文献
8.
Gwang Hoon Gil Seung Rim Kim Jong Chan Bae Jae Heung Lee 《Enzyme and microbial technology》1985,7(8):370-372
Effects of inoculum size and total sugar content on both l-phenylalanine productivity and titre have been investigated using a tyrosine auxotrophic regulatory mutant of Escherichia coli. Fermentations were carried out in a 500 litre pilot fermenter with intermittent feeding of d-glucose plus phosphate. It was found that the productivity was not greatly affected by inoculum size. However, the l-phenylalanine titre was significantly affected by total sugar content. Relatively high productivities of up to 0.35–0.40 g l-phenylalanine l?1 h?1 have been achieved at l-phenylalanine titres of 14–15 g l?1. 相似文献
9.
Biochemical Studies on Amphibian Metamorphosis : I. The effect of thyroxine on protein synthesis in the tadpole 总被引:6,自引:0,他引:6
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Thyroxine has been shown to accelerate the synthesis of carbamyl phosphate synthetase in the liver of Rana catesbeiana. Stimulation of carbamyl phosphate synthetase synthesis by thyroxine appears to be relatively specific because of the following observations: (1) succinoxidase activity decreased during the time that carbamyl phosphate synthetase increased; (2) liver catalase responded more slowly than carbamyl phosphate synthetase to thyroxine; (3) the ratio of biochemical changes/morphological changes was greatly altered during thyroxine-induced metamorphosis. The relationships between the concentration of thyroxine and (1) temperature; (2) duration of exposure of the tadpole to thyroxine; and (3) the activity of carbamyl phosphate synthetase during the induced synthesis of carbamyl phosphate synthetase by thyroxine are discussed. Chloramphenicol and thiouracil partly counteracted the effect of thyroxine on the synthesis of carbamyl phosphate synthetase. 相似文献
10.
Comparison of lodging safety factor of untreated and succinic Acid 2,2-dimethylhydrazide-treated shoots of mulberry tree 总被引:1,自引:0,他引:1
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![点击此处可从《Plant physiology》网站下载免费的PDF全文](/ch/ext_images/free.gif)
This study examined the lodging resistance of mulberry tree (Morus bombycis Koidz. cv Kenmochi) shoots treated or not treated with succinic acid 2,2-dimethylhydrazide (SADH). The lodging safety factor, an indicator of lodging resistance, was defined as the ratio of critical lodging load to the leaf fresh weight observed, provided that the distribution of the critical lodging load along the stem was similar to that of the leaf fresh weight observed. The critical lodging load was experimentally estimated by loading weights onto the stems. In the untreated trees, the lodging safety factor was maintained at about 3.2. In the SADH-treated trees, the stem elongation was inhibited to about 80% of that in the untreated trees, and the percentage of shoot dry matter partitioned into the leaves was always larger than that of the untreated trees. This dwarfing of the stem caused by SADH increased the critical lodging load supported by the unit stem dry weight, while this large investment of materials in leaves increased the leaf fresh weight supported by the unit stem dry weight. Since the increments canceled each other, the lodging safety factor of the SADH-treated shoots was similar to that of the untreated ones. These results suggest that the shoot formation of the mulberry tree is controlled to maintain the lodging safety factor at a constant level. 相似文献