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31.
Inhibitors of acetylcholine breakdown by acetylcholinesterase (AChE) constitute the main therapeutic modality for Alzheimer's disease. In the search for natural products with inhibitory action on AChE, this study investigated the activity of saffron extract and its constituents by in vitro enzymatic and molecular docking studies. Saffron has been used in traditional medicine against Alzheimer's disease. Saffron extract showed moderate AChE inhibitory activity (up to 30%), but IC(50) values of crocetin, dimethylcrocetin, and safranal were 96.33, 107.1, and 21.09 μM, respectively. Kinetic analysis showed mixed-type inhibition, which was verified by in silico docking studies. Safranal interacts only with the binding site of the AChE, but crocetin and dimethylcrocetin bind simultaneously to the catalytic and peripheral anionic sites. These results reinforce previous findings about the beneficial action of saffron against Alzheimer's disease and may be of value for the development of novel therapeutic agents based on carotenoid-based dual binding inhibitors.  相似文献   
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目的由于烟草烟雾中游离脂肪酸可与二价铁形成亲脂性复合物并输送铁到哺乳动物细胞,故其可能是重要的有毒成分。尽管早已发现这种铁负载增加了细胞膜不饱和脂肪酸氧化易感性,但脂肪酸:铁络合物的其他毒性所知甚少。方法利用酿酒酵母研究脂肪酸和铁的协同毒性和突变作用,同时观察了线粒体中脂肪酸介导铁沉积、脂质过氧化和活性氧产生。结果单纯铁和游离脂肪酸对酵母的活性及突变无明显影响,但二者联用有明显毒性。把酵母悬浮液在氮气中孵育可防止这种毒性,表明线粒体代谢生成的活性氧可能参与其中。呼吸缺陷酵母可对抗铁:脂肪酸诱导的毒性,具有增强铁储存能力的CCC1过表达酵母也有类似的保护作用。因维生素E或拉扎洛依(多不饱和脂肪酸过氧化反应抑制剂)可防止其杀伤作用,铁+脂肪酸的细胞毒性作用很可能是由膜多不饱和脂肪酸氧化损伤介导。结论铁:脂肪酸络合物所致铁超负荷的毒性作用可能涉及线粒体代谢。如果酵母中这些结果与吸烟相关的渐进性肺损伤有关,意味着烟草中看似无害的脂肪酸可能在微量"松散"铁存在情况下成为重要的有毒成分。  相似文献   
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The aim of this study was to examine species‐specific differences in pre‐ and post‐stress concentrations of haematological, metabolic and hormonal parameters in two Mediterranean fish species, one with relatively high (European sea bass, Dicentrarchus labrax) and the other with low (meagre, Argyrosomus regius) basal and post‐stress blood cortisol concentrations, in relation to different water temperatures. Fish were reared in net‐pen sea cages and exposed to an identical acute stressor (crowding and chasing with a net for 5 min) in three different periods of the year. Results indicated that inter‐specific differences occurred in most of the examined parameters. In addition, within each species, differences between sampling periods existed in plasma cortisol, glucose, osmolarity, blood pH and muscle glycogen concentration. Glucose, lactate and osmotic pressure showed a constant pattern of change, with maxima at half an hour post stress in both species, while cortisol, and blood and muscle pH, were significantly altered only in E. sea bass. No alterations were observed in liver and muscle glycogen concentrations in E. sea bass, while a significant reduction was evident only in the coldest temperature in meagre. It is concluded that there are important species‐specific differences in the magnitude of hormonal and metabolic response to acute stress and that both basal and post‐stress blood cortisol concentrations are affected by the sampling period.  相似文献   
35.
Cotton although is an autogamous species could be cross pollinated under favorable climate conditions and/or in the presence of pollinators. The coexistence of cotton with Malvaceae species raises questions on the possibility pollen to be exchanged among Malvaceae species and on the resulted consequences. The present work was undertaken to evaluate the in situ response of cotton flowers (G.hirsutum L, G. barbadense L.) and their F1 interspecific hybrids when are artificially pollinated with Malva sylvestris L., Hibiscus syriacus L. and Abelmoschus esculentus Moench. Furthermore, an in vitro protocol was attempted to support embryos’ growth in order to produce viable progenies originating from crosses between cotton and the aforementioned Malvaceae species. The obtained results gave evidence that pollen from the above Malvaceae species stimulated cotton ovaries without successful hybridization. The interaction between pollen and cotton’s stigmas was higher at early stages when M. sylvestris was used as pollinator but in crosses with H. syriacus and A. esculentus more ovules were activated as revealed by the percentage of carpodesis and life-time of bolls onto maternal plants. Only crosses between cotton with okra produced cotton seeds under in situ conditions. The in vitro embryo-ovule culture protocol, used, increased the number of regenerated cotton plants, especially in crosses among F1 interspecific cotton hybrids and A. esculentus. In this case, regenerated plants were recombinant aneuploids, combining traits from both cotton species. This novel cotton germplasm possessing unique chromosome rearrangements, at aneuploid level could be proved useful after cytogenetic, molecular or QTL genetic analysis referring to important agronomic traits.  相似文献   
36.
This study aims to investigate the response of 10 Greek Oregano (Origanum vulgare subsp. hirtum) populations, collected across Greece, under 3 levels of N-fertilization during 2012 and 2013. The populations were differentiated for dry matter (from 32.7 to 63.3?g·pot?1), for essential oil content (from 2.31 to 5.86?ml·100?1?g dry weight) and for amount of essential oil (from 1.37 to 2.46?ml·pot?1), for both years. Those with the highest dry matter (1-“Palaiochori” and 5-“Gliki”) and the highest essential oil content (10-“Gytheio” and 9-“Achladocastro”) were superior by 30%, as compared to the general mean of the experiment. The populations 3-“Litochoro” and 5-“Gliki” had an increased amount of essential oil (24%) as compared to the general mean of the experiment. An additional nitrogen supply (N0 to N1 level) increased dry matter production and amount of essential oil per pot, while decreased essential oil content for all populations. Further increase of nitrogen supply, favored six populations for dry matter production and two populations for amount of essential oil per pot while had almost no effect on five populations for essential oil content. The superior populations could be used in a breeding program as starting material for the development of new cultivars.  相似文献   
37.
We present a Bayesian nonparametric modeling approach to inference and risk assessment for developmental toxicity studies. The primary objective of these studies is to determine the relationship between the level of exposure to a toxic chemical and the probability of a physiological or biochemical response. We consider a general data setting involving clustered categorical responses on the number of prenatal deaths, the number of live pups, and the number of live malformed pups from each laboratory animal, as well as continuous outcomes (e.g., body weight) on each of the live pups. We utilize mixture modeling to provide flexibility in the functional form of both the multivariate response distribution and the various dose–response curves of interest. The nonparametric model is built from a structured mixture kernel and a dose-dependent Dirichlet process prior for the mixing distribution. The modeling framework enables general inference for the implied dose–response relationships and for dose-dependent correlations between the different endpoints, features which provide practical advances relative to traditional parametric models for developmental toxicology. We use data from a toxicity experiment that investigated the toxic effects of an organic solvent (diethylene glycol dimethyl ether) to demonstrate the range of inferences obtained from the nonparametric mixture model, including comparison with a parametric hierarchical model.Supplementary materials accompanying this paper appear on-line.  相似文献   
38.
BACKGROUND: The activity of several garlic oil ingredients against Culex pipiens L. larvae was studied. In addition to diallyl sulfide (DS) and diallyl disulfide (DDS), the garlic oils used included one essential oil (EO) and two semi‐synthetic garlic essential oils (SSGEO1 and SSGEO2), which resulted from the enrichment of EO with DS and DDS standards respectively. The oils were compared with respect to their toxicity. RESULTS: The chemical composition of the tested oils was evaluated by means of gas chromatography–mass spectrometry. Experimental data from the tested samples revealed high toxicity. In detail, DDS (6.09 mg L?1) was the most active, followed by SSGEO2 (7.05 mg L?1) and EO (8.01 mg L?1), while SSGEO1 and DS were relatively inactive. CONCLUSION: The addition of DDS to EO did not change the toxic effect of the essential oil, whereas the presence of DS in excess produced an enriched essential oil with low toxicity. Furthermore, the antagonistic effect of DS and DDS against the other components of EO was shown by the application of two equations obtained from the literature. Their larvicidal performances were correlated, for the first time, with their detailed chemical composition. Data analysis strongly indicated the toxicity of the other EO sulfur ingredients. Copyright © 2008 Society of Chemical Industry  相似文献   
39.
Four α‐amylases and two glucoamylases from various sources, in eight combinations, were used to study the synergistic hydrolysis of crude corn starch at various temperatures. At 40 and 50°C, the combinations containing Rhizopus mold glucoamylase enhanced hydrolysis of corn starch compared wth that obtained with the combinations from Aspergillus niger. At 60°C, Rhizopus mold combinations gave low reaction yields as the enzyme was inactivated. The differences observed between α‐amylases are smaller, with the exception of Bacillus licheniformis α‐amylase, which presented more than twice the productivity of the other α‐amylases, at all temperatures. In terms of substrate conversion at 5 hr of hydrolysis, the combination of B. licheniformis α‐amylase with Rhizopus mold glucoamylase at 50°C presents 76% substrate conversion, whereas, with all the other combinations, starch conversion was 13–73%. HPLC analysis of the reaction products obtained at 50°C showed that the main product of corn starch hydrolysis was glucose at 85–100%. Further experiments showed that A. niger glucoamylase and B. licheniformis α‐amylase were the only enzymes that retained their initial activity after incubation at the temperatures studied.  相似文献   
40.
The effects of rearing volume on on‐growing European sea bass performance and stress parameters were investigated for the first time in a pilot aquaculture farm. Fish were held under the same initial stocking densities in triplicate net‐pen cages of different sizes (1.4, 45 and 252 m3) for a period of 8 months. Results showed significant differences among the experimental groups in most parameters tested, with better performance in the two larger rearing volumes. In particular, growth rate showed a linear association with rearing volume, being 0.68 g day?1 for the large cage group, 0.56 g day?1 and 0.32 g day?1 for the medium and the small groups respectively. The feed conversion ratio and per cent survival (%) were also better in the large cage group. Fish reared in the small and medium‐sized cages showed higher plasma cortisol concentrations than those reared in large cages, which showed low basal cortisol concentrations. Additionally, after an acute chasing stress challenge, fish in the large and small groups, but not the medium group, showed increased cortisol concentrations. Differences also occurred in the ratio of the expression of cortisol receptors, namely the mineralocorticoid (mr) and glucocorticoid receptors (gr). In specific, the ratio of mr to grmRNA expression in the liver was higher in fish reared in the small cages. These findings verify that experimental scale significantly affects experimental results and is a critical factor for the interpretation of results.  相似文献   
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