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Kłodawska Kinga Kovács László Vladkova Radka Rzaska Agnieszka Gombos Zoltán Laczkó-Dobos Hajnalka Malec Przemysław 《Photosynthesis research》2020,143(3):251-262
Photosynthesis Research - In Synechocystis sp. PCC 6803 and some other cyanobacteria photosystem I reaction centres exist predominantly as trimers, with minor contribution of monomeric form, when... 相似文献
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Kinga Chojnacka Roger L. Papke Nicole A. Horenstein 《Bioorganic & medicinal chemistry letters》2013,23(14):4145-4149
We introduce the term ‘silent agonists’ to describe ligands that can place the α7 nicotinic acetylcholine receptor (nAChR) into a desensitized state with little or no apparent activation of the ion channel, forming a complex that can subsequently generate currents when treated with an allosteric modulator. KC-1 (5′-phenylanabaseine) was synthesized and identified as a new silent agonist for the α7 nAChR; it binds to the receptor but does not activate α7 nAChR channel opening when applied alone, and its agonism is revealed by co-application with the type II positive allosteric modulator PNU-120596 in the Xenopus oocyte system. The concise synthesis was accomplished in three steps with the C–C bonds formed via Pd-catalyzed mono-arylation and organolithium coupling with N-Boc piperidinone. Comparative structural analyses indicate that a positive charge, an H-bond acceptor, and an aryl ring in a proper arrangement are needed to constitute one class of silent agonist for the α7 nAChR. Because silent agonists may act on signaling pathways not involving ion channel opening, this class of α7 nAChR ligands may constitute a new alternative for the development of α7 nAChR therapeutics. 相似文献
305.
An attempt was made to extract the substance present in the nerve fibres of the cerebral cortex and basal ganglia which reduced Nitro-BT in alkaline medium pH 9-5 [4,5]. The investigations were performed on 40 white Wistar rats of both sexes and ca. 200 g of body weight. The brains taken for studies were fixed in Baker's formalin for 1,5 hr, thereafter grinded and homogenized in chloroform-methanol solution supplemented up to 100 ml of final volume after homogenisation. Thus prepared solution was left for 24 hr at 4 degrees C temperature and than centrifuged 2000 g/min. The extract was evaporated and the sediment further investigated. The following fraction were received: 1. fraction soluble in aceton, 2. fraction soluble in ethylalcohol, 3. fraction soluble in ether, 4. fraction soluble in water and 5. the sediment. Each fraction was incubated with a standard medium containing Nitro-BT. After incubation the amount of reduced Nitro-BT in each of the incubation medium was spectrophotometrically measured. The most intense reduction was found in the incubation medium with the water fraction. The spectrophotometrically determined reduction of Nitro-BT of the water fraction compared with that of the gangliosides solution were similar. The addition into the incubation media biogenic amines and N,N-diethyl-p-phenylenediamine enhances the reduction of Nitro-BT significantly. According to the results obtained an interference of gangliosides and of the investigated amines in the reduction of Nitro-BT is suggested. 相似文献
306.
In this study we determined the levels of trace elements (zinc, copper, lead, cadmium and mercury) in three layers of bones
of the hip joint (cartilage, compact bone and spongy bone) of 30 red foxes (Vulpes vulpes) from north-western Poland. Concentrations of Cu, Zn, Pb and Cd were determined by atomic absorption spectrophotometry (ICP-AES)
in inductively coupled argon plasma using a Perkin-Elmer Optima 2000 DV. Determination of Hg concentration was performed by
atomic absorption spectroscopy. In cartilage, compact bone and spongy bone samples from the red fox, median concentrations
of the metals studied could be arranged in the following descending series: Zn > Cu > Pb > Cd > Hg, the values ranging from
142 to 0.002 mg/kg dw. There was a significant difference in Cu concentrations, among all the materials analyzed, with much
more Cu found in spongy bone than in compact bone. Significant differences were also noted in the case of Hg concentrations
in cartilage with compact bone and the spongy bone, and between concentrations of this metal in compact bone and spongy bone.
In males, the concentration of Hg in spongy bone was greater than in females. Younger foxes had a higher concentration of
this metal in cartilage than adults. The strongest synergistic relationships were observed in spongy bone between the Zn and
Cu, Zn and Cd, as well as between Cu and Cd. Statistically significant antagonistic relationships were detected between zinc
and lead in compact bone. In addition to monitoring studies conducted on the abiotic environment, an urgent need exists for
long-term monitoring of concentrations of heavy metals with long-term effects on living organisms. An important addition is
provided by biomonitoring studies on domesticated and free-living mammals, including Canidae. 相似文献
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Juan F. Marquez Ruiz Kinga Kedziora Mary O’Reilly Jacqueline Maguire Brian Keogh Henry Windle Dermot P. Kelleher John F. Gilmer 《Bioorganic & medicinal chemistry letters》2012,22(24):7573-7577
Budesodine is a synthetic glurocorticoid that undergoes substantial first pass metabolism, limiting systemic exposure. Its use in treatment of inflammatory bowel disease would benefit from a targeting strategy that could lead to a local topical effect, improving safety and increasing anti-inflammatory efficacy. A two-step prodrug strategy involving azoreduction/cyclization that we developed previously for prednisolone is here applied with some variations to budesonide. The budesodine prodrugs were tested using an in vitro azoreductase assay simulating human colonic microflora. The kinetics of amino steroid ester cyclization and its pH dependence was also evaluated. The stability of the prodrugs systems in simulated human duodenal and gastric fluid was evaluated to determine the likelihood of intact intestinal transit. The propionic acid derived prodrug 3 undergoes rapid activation by Clostridium perfingens and its putative reduction product cyclizes with acceptable rapidity when synthesized independently. These properties of 3 suggest that it has potential in management of ulcerative colitis. 相似文献