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排序方式: 共有251条查询结果,搜索用时 62 毫秒
91.
Shen W Fakhoury S Donner G Henry K Lee J Zhang H Cohen J Warner R Saeed B Cherian S Tahir S Kovar P Bauch J Ng SC Marsh K Sham H Rosenberg S 《Bioorganic & medicinal chemistry letters》1999,9(5):703-708
Synthesis and biological evaluation of heteroarenes as reduced cysteine replacements are described. Of the heteroaryl groups examined with respect to FT inhibitor FTI-276 (1), pyridyl was the replacement found to be most effective. Substitutions at C4 of the pyridyl moiety did not affect the in vitro activity. Compound 9a was found to have moderate in vivo bioavailability. 相似文献
92.
Claire SM Kwan Rafael P Vázquez-Manrique Sung Ly Kshamata Goyal Howard A Baylis 《BMC physiology》2008,8(1):11
Background
Ultradian rhythms, rhythms with a period of less than 24 hours, are a widespread and fundamental aspect of life. The mechanisms underlying the control of such rhythms remain only partially understood. Defecation in C. elegans is a very tightly controlled rhythmic process. Underlying the defecation motor programme is an oscillator which functions in the intestinal cells of the animal. This mechanism includes periodic calcium release and subsequent intercellular calcium waves which in turn regulate the muscle contractions that make up the defecation motor programme. Here we investigate the role of TRPM cation channels in this process. 相似文献93.
Intermittent administration stimulates bone formation, whereas sustained elevation of parathyroid hormone (PTH) as in hyperparathyroidism stimulates bone resorption. Even though PTH(1-34) is the only anabolic agent clinically approved for the treatment of osteoporosis, the molecular mechanism whereby PTH mediates these opposing effects depending on timing of administration is not well understood. In this study, we sought to determine the involvement of gap junctions and hemichannels, and the protein that forms them, connexin 43 (Cx43), in the effect of PTH(1-34) on osteoblast mineralization. The osteoblast-like cell line MLO-A5 that rapidly mineralizes in culture was used. Intermittent PTH enhances mineralization, whereas continuous PTH inhibits this process. The mineralization was significantly inhibited by 18 beta-glycyrrhetinic acid, an inhibitor known to block gap junctions and hemichannels. When the cells were treated with PTH(1-34), gap junctional coupling was increased; however, the degree of stimulation was similar between intermittent and continuous treatment. The permeabilization to dye was not detected under various intermittent or continuous PTH treatments. On the other hand, the overall level of Cx43 protein increased in response to continuous PTH treatment. In contrast, when the cells were subjected to intermittent treatment overall level of Cx43 was unchanged, but there was an increase of connexons associated with an increase in Cx43 expression on the cell surface. Our results suggest that Cx43 overall expression, connexon formation and cell surface expression are differentially regulated by intermittent and continuous PTH(1-34), implying the involvement of Cx43 and Cx43-forming channels in mediating the effects of PTH on bone formation. 相似文献
94.
Control of nematode parasites with reduced reliance on the use of anthelmintics was studied in 16 ewes with suckling twin
lambs on contaminated pasture in Denmark. Ewes and lambs were treated with albendazole at turn-out 3 May. Ewes were removed
from the groups on 26 July, and lambs were slaughtered on 11 October. The animals were allocated to 4 groups of 8 lambs and
their 4 ewes. Group TS was treated with albendazole at weeks 3, 6 and 8 after turnout and set-stocked; group TM was similarly
treated but moved to clean pasture in conjunction with the last drenching; group US was untreated and set-stocked, and group
UM was left untreated but moved to clean pasture week 8 after turn-out. Supplementary feed was offered in June and August
due to scarcity of pasture. Strategic treatments of ewes and lambs weeks 3, 6 and 8 after turn-out, with or without a move
to clean pasture, were highly effective in controlling nematode infections for most of the season. This was reflected in better
weight gains and carcass characteristics in the treated compared to untreated lambs, resulting in an average increase in the
value of the product by 36%. The effect of moving without treatment (UM) on faecal egg counts was limited but peak pasture
infectivity was reduced to less than 10% compared to the set-stocked group and weight gains of lambs were significantly better
despite poor feed availability in late season. The study showed that under set-stocked conditions repeated anthelmintic treatments
of both ewes and lambs in early season may ensure sufficient nematode control whereas moving animals to clean pasture without
dosing was less efficient. The latter may, however, still be a viable option in organic and other production systems where
routine use of anthelmintics is banned, particularly if weaning and moving are combined or a second move is performed. 相似文献
95.
The agricultural sector, and particularly the horticultural production, has a singular importance in agriculture, considering that it ranks second on agricultural products, nationally and worldwide. Fungal diseases are one of the major causes of vegetable loss during storage, reducing their nutritional value, quality and sale price. Vegetables are usually exposed to diverse treatments with chemical products before storage; as a result, fungal populations develop an increased resistance over time becoming more difficult to control. Because of this, research efforts toward finding more suitable chemicals to control fungal diseases are needed. Natural extracts may be an alternative solve this problem. In the present investigation the fungicidal activity of aqueous and ethanol extracts of Agave scabra was evaluated on the growth of Botrytis cinerea, Mucor sp., Aspergillus niger, Fusarium sp. and Penicillium sp., whose strains were isolated from potato and tomato. To assess their effects, the agar-dilution and agar-well techniques were performed. The ethanol extract was more effective against Botrytis cinerea and Mucor sp. when the agar-well method was used. However, when using the agar-dilution method the ethanol extract of Agave scabra inhibited the growth of Botrytis cinerea, Mucor sp. and Penicillium sp. 相似文献
96.
C Magnoli SM Chiacchiera R Miazzo G Palacio A Angeletti C Hallak A Dalcero 《Mycotoxin Research》2002,18(1):7-22
Feedstuffs used for poultry nutrition in Argentina were analyzed for fungal flora and natural incidence of mycotoxins. Survey
of 120 samples of poultry feeds, taken from May 1998 to April 1999, showed the presence of 15 genera of filamentous fungi.
The predominant genera wereFusarium spp. andPenicillium ssp., isolated in 67.5 % of the samples, followed byAspergillus spp. (57.5 %). Yeast, were significantly isolated from most of the samples. Species identification was carried down for the
toxigenic genera. Fungal total counts of poultry feeds ranged from 2.0 × 103 to 3.0 × 105 CFU g-1 The fungal total counts during two months of sampling, were slightly over the limit value of 1 × 105 CFU g-1, which ensure the hygienic quality of the feed. Potentially toxicogenic species presented moderate mean colony counts. Many
of the fungi isolated from poultry feeds are mycotoxin producers. Fumonisins had the highest incidence, and were found in
97 % of the analyzed samples followed by aflatoxin B1 (46 %), zearalenone (18 %) and deoxynivalenol (6 %). On the co-occurrence of both carcinogenic mycotoxins, all of the FBs
contaminated feed samples were co-contaminated with AFB1. The results show the relevance of the samples screening for viable fungi propagules and the surveillance of their associated
mycotoxins in poultry feeds. 相似文献
97.
98.
Contusion injury is produced experimentally in anaesthetised monkeys by weight drop method. A group of animals having laminectomy alone served as sham controls. Drugs were administered 30 min after injury initially. Naloxone and nifedipine were administered as single dose administration immediately after injury. Dipyridamole and DMSO were administered daily for a period of 1 week. Acetylcholinesterase (AchE) was estimated in 2 spinal tissue segments, S1-at the site of injury and S2-the segment above the site of injury, at the end of 1 week after sacrificing the animals. Contusion injury produced significant decrease in specific activity of AchE in the traumatised segment of the experimental animals. The non-traumatised adjacent segment did not show any significant change. Nifedipine, naloxone and DMSO produced a decrease in AchE activity in S1 and S2 segments. Monkeys developed paraplegia after contusion injury. A score 2+ was observed after 1 week as compared to the score of 4+ of sham controls. Single dose administration of naloxone seemed to reverse the motor deficit by getting a score of 3+; other drugs did not produce any beneficial effect on motor deficit. 相似文献
99.
Joyce Nikolakopoulos Cherian Zachariah Duarte Mota de Freitas †Evan B. Stubbs Jr. ‡Ravichandran Ramasamy §M. Margarida C. A. Castro §Carlos F. G. C. Geraldes 《Journal of neurochemistry》1998,71(4):1676-1684
Abstract: Lithium has been used clinically in the treatment of manic depression. However, its pharmacologic mode of action remains unclear. Characteristics of Li+ interactions in red blood cells (RBCs) have been identified. We investigated Li+ interactions on human neuroblastoma SH-SY5Y cells by developing a novel 7 Li NMR method that provided a clear estimation of the intra- and extracellular amounts of Li+ in the presence of the shift reagent thulium-1,4,7,10-tetrazacyclododecane- N,N ', N ", N ‴-tetramethylene phosphonate (HTmDOTP4− ). The first-order rate constants of Li+ influx and efflux for perfused, agarose-embedded SH-SY5Y cells in the presence of 3 m M HTmDOTP4− were 0.055 ± 0.006 (n = 4) and −0.025 ± 0.006 min−1 (n = 3), respectively. Significant increases in the rate constants of Li+ influx and efflux in the presence of 0.05 m M veratridine indicated the presence of Na+ channel-mediated Li+ transport in SH-SY5Y cells. 7 Li NMR relaxation measurements showed that Li+ is immobilized more in human neuroblastoma SH-SY5Y cells than in human RBCs. 相似文献
100.
A. S. Balasubramanian T. Alam R. Mathur S. Lakshmi R. Cherian K. Alvares 《Journal of biosciences》1983,5(1):61-64
Concanavalin A bound to Sepharose has been used for the purification of brain β-galactosidase, α-L-fucosidase, α-D-mannosidase, arylsulphatase and β-glucuronidase.0 Several factorsviz pH, temperature and concentration of α-methyl glucoside influenced the binding and elution of these enzymes. A lysosomal acid α-mannosidase and a cytosolic neutral mannosidase were separable by concanavalin A-Sepharose chromatography. Similarly lysosomal and microsomal β-glucuronidases were separable using gradient elution with α-methyl glucoside. The results indicate the usefulness of this lectin for the isolation of wide variety of enzymes under specified experimental conditions. 相似文献