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41.
Ali Alipour Najmi Elchin Jafariyeh-Yazdi Mojgan Hadian Jos Hermans Prof. Rainer Bischoff Prof. Jun Yue Prof. Alexander Dömling Prof. Arne Wittstock Dr. Hjalmar P. Permentier 《ChemMedChem》2022,17(11):e202200040
A novel method for the selective catalytic N-dealkylation of drug molecules on a nanoporous gold (NPG) catalyst producing valuable N-dealkylated metabolites and intermediates is described. Drug metabolites are important chemical entities at every stage of drug discovery and development, from exploratory discovery to clinical development, providing the safety profiles and the ADME (adsorption, distribution, metabolism, and elimination) of new drug candidates. Synthesis was carried out in aqueous solution at 80 °C using air (oxygen source) as oxidant, in single step with good isolated yields. Different examples examined in this study showed that aerobic catalytic N-dealkylation of drug molecules on NPG has a broad scope supporting N-deethylation, N-deisopropylation and N-demethylation, converting either 3° amines to 2° amines, or 2° amines to 1° amines. 相似文献
42.
近年来,非传染性慢性疾病的发病率迅速上升,已成为一个全球性的问题。过度食用简单的加工碳水化合物食品被认为是导致年轻人和老年人罹患非传染性慢性疾病的主要原因之一。全谷物米是碳水化合物、膳食纤维的重要来源,富含维生素、矿物质和抗氧化剂。然而,糙米的适口性是其在长期以白米消费为主的人群中被接受的关键因素。在初始阶段,我们成功培育出了水稻品种,其全谷物米芳香、柔软且白米具有较高的铁锌密度和中血糖指数(GI)。最成功的品种是独特的具有较软质构的黑紫色稻米,名为紫莓香米(Riceberry),富含蓝莓花青素等营养物质的稻米。针对富含膳食纤维、高抗氧化活性的稻米产品研发一直是学术界、实体部门和中小企业极为活跃的领域,目前共有关于紫莓香米相关的39项专利申请(18项已授权专利)、12项国际出版物、以及18 700个与紫莓香米有关的YouTube视频。从2017年开始,紫莓香米已超越泰国Hom茉莉香米(Thai Hommali Rice)成为最受欢迎的产品开发选择原料,已有超过200种作为乳制品替代品、配菜、主餐食品、热饮料、烘焙食品和早餐麦片等的商业化食品和非食品产品。在第二阶段,我们成功地培育出了名为Pink+4的低血糖指数水稻品种,该品种具有对骤发洪水、水稻白叶枯病、稻瘟病和破坏性褐飞虱的首选抗性,适用于有机水稻生产。以紫色紫莓香米为原料的低GI米粉创新产品已成为功能性配料和功能性食品的下一个发展趋势。这些健康的稻米产品在全球具有较好的发展潜力,可以作为健康食品、无麸质、富含纤维、复杂碳水化合物和可持续有机农业的营养密集型产品。 相似文献
43.
Alexandra Gros Landre Lavenu Jean-Luc Morel Philippe De Deurwaerdre 《International journal of molecular sciences》2021,22(21)
Microgravity, one of the conditions faced by astronauts during spaceflights, triggers brain adaptive responses that could have noxious consequences on behaviors. Although monoaminergic systems, which include noradrenaline (NA), dopamine (DA), and serotonin (5-HT), are widespread neuromodulatory systems involved in adaptive behaviors, the influence of microgravity on these systems is poorly documented. Using a model of simulated microgravity (SMG) during a short period in Long Evans male rats, we studied the distribution of monoamines in thirty brain regions belonging to vegetative, mood, motor, and cognitive networks. SMG modified NA and/or DA tissue contents along some brain regions belonging to the vestibular/motor systems (inferior olive, red nucleus, cerebellum, somatosensorily cortex, substantia nigra, and shell of the nucleus accumbens). DA and 5-HT contents were reduced in the prelimbic cortex, the only brain area exhibiting changes for 5-HT content. However, the number of correlations of one index of the 5-HT metabolism (ratio of metabolite and 5-HT) alone or in interaction with the DA metabolism was dramatically increased between brain regions. It is suggested that SMG, by mobilizing vestibular/motor systems, promotes in these systems early, restricted changes of NA and DA functions that are associated with a high reorganization of monoaminergic systems, notably 5-HT. 相似文献
44.
45.
Prof. Tsung-Shing Andrew Wang Ruo-Yu Wu Yu Hong Dr. Zhe-Chong Wang Dr. Tsung-Lin Li Dr. Jiun-Jie Shie Prof. Cheng-Chih Hsu 《Chembiochem : a European journal of chemical biology》2021,22(14):2415-2419
Secondary metabolites are structurally diverse natural products (NPs) and have been widely used for medical applications. Developing new tools to enrich NPs can be a promising solution to isolate novel NPs from the native and complex samples. Here, we developed native and deuterated chemoselective labeling probes to target phenol-containing glycopeptides by the ene-type labeling used in proteomic research. The clickable azido-linker was included for further biotin functionalization to facilitate the enrichment of labeled substrates. Afterward, our chemoselective method, in conjunction with LC-MS and MSn analysis, was demonstrated in bacterial cultures. A vancomycin-related phenol-containing glycopeptide was labeled and characterized by our labeling strategy, showing its potential in glycopeptide discovery in complex environments. 相似文献
46.
Hong-Jie Wang Biao Huang Xue-Zheng Shi Jeremy Landon Darilek Dong-Sheng Yu Wei-Xia Sun Yong-Cun Zhao Qing Chang Ingrid Öborn 《Nutrient Cycling in Agroecosystems》2008,81(3):203-218
Balances of major nutrients such as nitrogen (N), phosphorus (P), and potassium (K) in small-scale farming systems are of
critical importance to nutrient management and sustainable agricultural development. Mass balances of N, P, and K and some
of their influencing factors were studied for two years from July 2003 to July 2005 on small-scale vegetable-farming systems
in two contrasting peri-urban areas (Nanjing and Wuxi) of the Yangtze river delta region of China. This balance approach considered
organic fertilizer inputs (cow manure, pig manure, and human biosolids), inorganic fertilizer inputs (urea, composite fertilizer,
and phosphates), irrigation water, and atmospheric deposition; and considered outputs by vegetables. Input via organic fertilizers
was significant for all element balances in the Nanjing area. Inorganic and organic fertilizer, particularly inorganic fertilizer,
contributed major nutrient inputs to the system in the Wuxi area. Compared with nutrient output by vegetables, there were
significant surpluses of N and P on two vegetable farm systems. Furthermore, N surplus in the Nanjing area was higher than
that in the Wuxi area with an inverse relationship to P surplus. In contrast, the general trend of K balances was negative
on both sites; hence, the nutrient use efficiency was significantly lower for N and P than K. The nutrient imbalance may be
attributed to the differences between fertilizer types and management modes driven by social economic status differences among
farmer households. The large N and P net excess creates an environmental threat because of potential losses to ground or surface
waters, whereas negative K balance creates soil fertility risks. The results highlight researchers’ and farmers’ need to develop
rational fertilization technology to optimize nutrient management on vegetable farmlands to promote sustainable agricultural
development in peri-urban areas. 相似文献
47.
[目的]研究旨在优化苦瓜中氰霜唑(Cyazofamid)及其代谢物CCIM的QuEChERS-液相色谱-串联质谱残留分析方法;同时结合苦瓜的田间残留消解动态试验,对膳食摄入风险进行评价。[方法]苦瓜样品采用含1%乙酸的乙腈溶液提取,LC-MS/MS进行检测,通过基质匹配标准溶液外标法定量。通过在黑龙江、河北、河南、重庆、浙江和广东6地进行了100 g/L氰霜唑悬浮剂在苦瓜上残留的田间试验,研究了氰霜唑在苦瓜中的消解动态,对苦瓜中氰霜唑可能产生的膳食摄入风险安全进行评价。[结果]试验结果表明:1)氰霜唑在0.005-1.0 mg/L、CCIM在0.001-1.0 mg/L质量浓度范围内线性关系良好,相关系数均大于0.9987;在0.010、0.10、0.50 mg/kg 3个浓度下,苦瓜中氰霜唑及CCIM的回收率为80.0%~100.0%,相对标准偏差(RSD)为0.05%~12.1%。检出限(LOD)为0.364-0.654 μg/kg,方法定量限(LOQ)为添加的最低浓度0.010 mg/kg。2)田间试验结果表明:氰霜唑在苦瓜中消解符合一级反应动力学方程,半衰期为3.0~4.9 d,属易降解农药;使用100 g/L氰霜唑悬浮剂,施药剂量105-157.5 g a.i./hm2,分别施药2、3次,苦瓜中氰霜唑总的最终残留量最大值为6.54 mg/kg。3)膳食摄入风险评估结果表明:氰霜唑的风险概率为每人每日摄入总量的1.0%。[结论]在苦瓜生长期间按照推荐剂量合理使用氰霜唑对消费者的膳食健康风险极低,对消费者健康是安全的。 相似文献
48.
为从用户角度合理的对烟草田间作业机械进行适应性评价,利用可拓学原理和方法,建立了烟草田间作业机械的可拓评价模型,而后针对烟草田间起垄机械,在提出相应的评价指标体系的同时,将该模型运用到对7个起垄机组的实际评价当中。经试验数据采集与处理分析,结果表明:第Ⅰ、Ⅱ、Ⅲ、Ⅴ、Ⅵ机组均属于第v类(优),第Ⅳ机组与第Ⅶ机组分别属于第ii类(可)和第i类(差),机组的变量特征值排序为Ⅱ (4.67) > Ⅰ (4.07) > Ⅴ (3.82) > Ⅲ (3.78) > Ⅵ (3.33) > Ⅶ (2.53) > Ⅳ (2.33),其评价结果与实际情况相符合,说明该模型具有较好的适用性和可行性,可为评判烟草起垄机械适应性满意度提供量化的比较依据,同时该模型也对其他种植领域内的农业机械选型具有较好的借鉴参考价值。 相似文献
49.
This study was performed to investigate blood metabolite, tumor necrosis factor-alpha, and hormone responses to intravenous administration of lipopolysaccharides (2 microg of endotoxin of Escherichia coli 026:B6/kg body weight at times of feeding) in veal calves orally supplemented with arginine (0.25 g/kg of body weight twice daily for 4 d; group GrA) compared with calves not supplemented with arginine (group GrC). Arginine supplementation alone caused a significant rise of plasma arginine, urea, and insulin concentrations, whereas glucagon concentrations tended to increase, but there were no significant group differences. Concentrations of triglycerides, NEFA, glucose, protein, albumin, growth hormone, insulin-like growth factor-I, 3.5.3'-triiodothyronine, and thyroxine were not affected by arginine supplementation. Lipopolysaccharide administration alone caused a rise of tumor necrosis-factor-a, lactate, and cortisol concentrations and concentrations of tumor necrosis-factor-a after 1 h, and of triglycerides and urea after 6 h were higher, whereas of glucose after 3 h were lower in GrA than in GrC. Concentrations of NEFA, glucose, protein, albumin, insulin, growth hormone, insulin-like growth factor-I, 3.5.3'-triiodothyronine, and thyroxine were not affected by lipopolysaccharide administration. In conclusion, arginine supplementation had selective effects on plasma metabolites and hormones, but barely modified lipopolysaccharide effects. Effects of lipopolysaccharides in the postprandial state were different from what is usually seen in the fasted state. 相似文献
50.
Use of coupled canopy structure dynamic and radiative transfer models to estimate biophysical canopy characteristics 总被引:3,自引:0,他引:3
Leaf area index (LAI) is a key variable for the understanding of several eco-physiological processes within a vegetation canopy. The LAI could thus provide vital information for the management of the environment and agricultural practices when estimated continuously over time and space thanks to remote sensing sensors.This study proposed a method to estimate LAI spatial and temporal variation based on multi-temporal remote sensing observations processed using a simple semi-mechanistic canopy structure dynamic model (CSDM) coupled with a radiative transfer model (RTM). The CSDM described the temporal evolution of the LAI as function of the accumulated daily air temperature as measured from classical ground meteorological stations.The retrieval performances were evaluated for two different data sets: first, a data set simulated by the RTM but taking into account realistic measurement conditions and uncertainties resulting from different error sources; second, an experimental data set acquired over maize crops the Blue Earth City area (USA) in 1998. Results showed that the proposed approach improved significantly the retrieval performances for LAI mainly by smoothing the residual errors associated to each individual observation. In addition it provides a way to describe in a continuous manner the LAI time course from a limited number of observations during the growth cycle. 相似文献