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41.
Mehdi Asadi Mostafa Ebrahimi Maryam Mohammadi‐Khanaposhtani Homa Azizian Saghi Sepehri Hamid Nadri Mahmood Biglar Massoud Amanlou Bagher Larijani Roghieh Mirzazadeh Najmeh Edraki Mohammad Mahdavi 《化学与生物多样性》2019,16(11)
A novel series of phthalimide‐dithiocarbamate hybrids was synthesized and evaluated for in vitro inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The anti‐cholinesterase results indicated that among the synthesized compounds, the compounds 7g and 7h showed the most potent anti‐AChE and anti‐BuChE activities, respectively. Molecular docking and dynamic studies of the compounds 7g and 7h , respectively, in the active site of AChE and BuChE revealed that these compounds as well interacted with studied cholinesterases. These compounds also possessed drug‐like properties and were able to cross the BBB. 相似文献
42.
Mohankrishna Dalvoy Vasudevarao Pushpak Mizar Sujata Kumari Somnath Mandal Soumik Siddhanta Mahadeva MM Swamy Stephanie Kaypee Ravindra C Kodihalli Amrita Banerjee Chandrabhas Naryana Dipak Dasgupta Tapas K. Kundu 《The Journal of biological chemistry》2014,289(11):7702-7717
Hydroxynaphthoquinone-based inhibitors of the lysine acetyltransferase KAT3B (p300), such as plumbagin, are relatively toxic. Here, we report that free thiol reactivity and redox cycling properties greatly contribute to the toxicity of plumbagin. A reactive 3rd position in the naphthoquinone derivatives is essential for thiol reactivity and enhances redox cycling. Using this clue, we synthesized PTK1, harboring a methyl substitution at the 3rd position of plumbagin. This molecule loses its thiol reactivity completely and its redox cycling ability to a lesser extent. Mechanistically, non-competitive, reversible binding of the inhibitor to the lysine acetyltransferase (KAT) domain of p300 is largely responsible for the acetyltransferase inhibition. Remarkably, the modified inhibitor PTK1 was a nearly non-toxic inhibitor of p300. The present report elucidates the mechanism of acetyltransferase activity inhibition by 1,4-naphthoquinones, which involves redox cycling and nucleophilic adduct formation, and it suggests possible routes of synthesis of the non-toxic inhibitor. 相似文献
43.
44.
A one-pot and efficient method for the synthesis of pyrazolo[4',3':5,6]pyrido[2,3-d]pyrimidine-dione derivatives by condensation reaction of barbituric acids, 1H-pyrazol-5-amines and aldehydes under solvent-free conditions is reported. These products were evaluated in vitro for their antibacterial activities. 相似文献
45.
Afforestation is a recommended practice to mitigate global warming. However, their implementation may generate undesirable impacts, mostly if exotic species are used. Plantations of Pinus radiata D Don in Ventania (Bs. As., Argentina) soils showed notorious increments of extractable P (Pe), which could affect the dynamic of this element as well as the degree of phosphorus saturation (GSPBray). The objectives of this study were: i) to quantify the GSPBray in Mollisols afforested with P. radiata comparing the results with those coming from adjacent, natural grassland areas (base line); ii) to evaluate the potential environmental risk induced by afforestation through the identification of a change point (PC) in the GSPBray indicative of a phosphate leaching increment. Treatments included mature stands of P. radiata (TB) and adjacent areas with natural grassland vegetation (TP). Samples were taken at 0-15; 15-30 and 30-45 cm soil depth, and texture, pH, total organic carbon (COT), Pe, soluble reactive phosphorus (PSR), phosphorus sorption index (ISP) and GSPBray were determined. The results showed a significant acidification in TB and an increase in the COT stock, indicating an additional atmospheric CO2 sequestration by the trees. The Pe and PSR values were notoriously higher in TB, and they were reflected in a significant increment in the GSPBray with respect to TP. The detection of a significant PC in the GSPBray-PSR regression indicates higher chances of phosphate leaching in the forest stands, which could reach water courses, lakes and artificial reservoirs promoting their eutrophication. Because of the potential environmental pollution risk of biologic origin derived from the afforestation with P. radiata in Mollisols areas, their inclusion in clean development practices must be reconsidered. 相似文献
46.
47.
Resumé Les auteurs ont étudié la composition chimique (N, substances humiques, lignine) de copeaux de bois blanc exposés à l'air libre depuis 2 à 10 ans, ainsi que leur type de peuplement fongique. En l'absence de lignivore, le pH, les taux de lignine et d'N s'élèvent et il se forme des quantités modérées d'humus à forte capacité d'échange. Dans le cas contraire, on voit apparaître, en abondance, des substances humiques peu condensées et la matière organique subit une évolution rappelant celle du mor.Avec la collaboration technique de Melle. M. Clet.Kononova, dans sa monographie5, signale de Troussov (1916) une étude que nous n'avons pas eu en mains. 相似文献
48.
Studies of esterase 6 in Drosophila melanogaster. XVIII. Biochemical differences between the slow and fast allozymes 总被引:1,自引:0,他引:1
Most natural populations of Drosophila melanogaster are polymorphic for two
major electrophoretic variants at the esterase-6 locus. The frequency of
the EST 6F allozyme is greatest in populations in warmer latitudes, whereas
the EST 6S allozyme is predominant in colder latitudes. Latitudinal clines
in electromorph frequencies are found on three continents. Purified
preparations of the allozymes have been characterized for their pH optimum,
substrate specificity, organophosphate inhibition, alcohol activation,
thermal stability, and kinetic parameters. These and previous analyses of
the EST 6 allozymes reveal that the two variants have differences in their
physical and kinetic properties that may provide a basis for the selective
maintenance of the polymorphisms and an explanation of the clinal variation
observed in natural populations.
相似文献
49.
C André Lévesque Henk Brouwer Liliana Cano John P Hamilton Carson Holt Edgar Huitema Sylvain Raffaele Gregg P Robideau Marco Thines Joe Win Marcelo M Zerillo Gordon W Beakes Jeffrey L Boore Dana Busam Bernard Dumas Steve Ferriera Susan I Fuerstenberg Claire MM Gachon Elodie Gaulin Francine Govers Laura Grenville-Briggs Neil Horner Jessica Hostetler Rays HY Jiang Justin Johnson Theerapong Krajaejun Haining Lin Harold JG Meijer Barry Moore Paul Morris Vipaporn Phuntmart Daniela Puiu Jyoti Shetty Jason E Stajich Sucheta Tripathy Stephan Wawra Pieter van West Brett R Whitty Pedro M Coutinho Bernard Henrissat Frank Martin Paul D Thomas Brett M Tyler Ronald P De Vries Sophien Kamoun Mark Yandell Ned Tisserat C Robin Buell 《Genome biology》2010,11(7):1-22
50.
The XI International Rotifer Symposium was held during 11–18 March, 2006 at the National Autonomous University of Mexico Campus Iztacala located at the North Mexico City (Mexico). These triennial international meetings, first organized in Austria by Late Ruttner-Kolisko in September 1976, are gradually becoming the focal point of discussion and collaboration from rotifer workers across the world. The present XI symposium was attended by 125 participants from 20 nations. During this meeting, different themes of rotifer research from morphology to molecular biology were considered. In addition, there were four invited lectures and four workshops covering different themes of the symposium. During the last 30 years, rotifer research has witnessed gradual shift from the conventional morphological taxonomy to molecular and evolutionary systematics. While the basic rotifer ecological studies continue today, applied areas such as ecotoxicology and aquaculture have taken key roles in the recent meetings. The international rotifer meetings provide ample opportunities not only for exchange of ideas and recent research, but also for material and in establishing inter-personal relationships. Over the last 30 years, the number of participants attending the rotifer meetings has increased. 相似文献