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https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#1
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28332138/benzo-a-pyrene-exposure-causes-genotoxic-and-biochemical-changes-in-the-midge-larvae-of-chironomus-sancticaroli-strixino-strixino-diptera-chironomidae
#2
M Vicentini, G S Morais, D Rebechi-Baggio, V S Richardi, G S Santos, M M Cestari, M A Navarro-Silva
Benzo(a)pyrene (BaP) is a carcinogenic polycyclic aromatic hydrocarbon, also found in nature due to human activities. BaP adheres to sediments showing toxic effects on benthic organisms, including midge larvae of the family Chironomidae. We tested for toxic effects of benzo(a)pyrene on Chironomus sancticaroli Strixino & Strixino 1981 using biochemical and genotoxic biomarkers, to identify changes in metabolic and antioxidant pathways, besides neurotoxic and DNA damage. Enzyme activity was compared by exposing larvae to four nominal concentrations (0...
March 22, 2017: Neotropical Entomology
https://www.readbyqxmd.com/read/28332030/molecular-cloning-expression-and-characterization-of-pectin-methylesterase-ctpme-from-clostridium-thermocellum
#3
Vikky Rajulapati, Arun Goyal
Many phytopathogenic micro-organisms such as bacteria and fungi produce pectin methylesterases (PME) during plant invasion. Plants and insects also produce PME to degrade plant cell wall. In the present study, a thermostable pectin methylesterase (CtPME) from Clostridium thermocellum belonging to family 8 carbohydrate esterase (CE8) was cloned, expressed and purified. The amino acid sequence of CtPME exhibited similarity with pectin methylesterase from Erwinia chrysanthemi with 38% identity. The gene encoding CtPME was cloned into pET28a(+) vector and expressed using Escherichia coli BL21(DE3) cells...
March 22, 2017: Molecular Biotechnology
https://www.readbyqxmd.com/read/28331945/from-a-metagenomic-source-to-a-high-resolution-structure-of-a-novel-alkaline-esterase
#4
Mariana Rangel Pereira, Thaís Carvalho Maester, Gustavo Fernando Mercaldi, Eliana Gertrudes de Macedo Lemos, Marko Hyvönen, Andrea Balan
Esterases catalyze the cleavage and formation of ester bonds and are members of the diverse family of α/β hydrolase fold. They are useful in industries from different sectors, such as food, detergent, fine chemicals, and biofuel production. In a previous work, 30 positive clones for lipolytic activity were identified from a metagenomic library of a microbial consortium specialized in diesel oil degradation. In this study, a putative gene encoding an esterase/lipase, denominated est8, has been cloned and the corresponding protein expressed recombinantly, purified to homogeneity and characterized functional and structurally...
March 22, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28330103/profiling-and-production-of-hemicellulases-by-thermophilic-fungus-malbranchea-flava-and-the-role-of-xylanases-in-improved-bioconversion-of-pretreated-lignocellulosics-to-ethanol
#5
Manju Sharma, Chhavi Mahajan, Manpreet S Bhatti, Bhupinder Singh Chadha
This study reports thermophilic fungus Malbranchea flava as a potent source of xylanase and xylan-debranching accessory enzymes. M. flava produced high levels of xylanase on sorghum straw containing solidified culture medium. The optimization of culture conditions for production of hemicellulases was carried out using one factor at a time approach and Box-Behnken design of experiments with casein (%), inoculum age (h) and inoculum level (ml) as process variables and xylanase, β-xylosidase, acetyl esterases and arabinofuranosidase as response variables...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28327423/characterization-of-an-extracellular-protein-rv1076-from-m-tuberculosis-with-a-potential-role-in-humoral-response
#6
Gurkamaljit Kaur, Bandana Kumari, Jagdeep Kaur
Many mycobacterial proteins involved in lipid metabolism are reported to be essential for survival and pathogenesis of M. tuberculosis. Rv1076 of M. tuberculosis has been annotated as a putative esterase/lipase based on the consensus sequence 'GXSXG'. It is conserved in all the mycobacterial species. Therefore, in the present study we have characterized Rv1076 gene product in detail. The gene rv1076 was expressed in E. coli and purified from inclusion bodies with approx. 40% yield. The protein showed high specific activity with pNP- butyrate as preferred substrate...
March 19, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28327083/the-effect-of-an-interactive-cycling-training-on-cognitive-functioning-in-older-adults-with-mild-dementia-study-protocol-for-a-randomized-controlled-trial
#7
E G A Karssemeijer, W J R Bossers, J A Aaronson, R P C Kessels, M G M Olde Rikkert
BACKGROUND: To date there is no cure or an effective disease-modifying drug to treat dementia. Available acetylcholine-esterase inhibiting drugs or memantine only produce small benefits on cognitive and behavioural functioning and their clinical relevance remains controversial. Combined cognitive-aerobic interventions are an appealing alternative or add-on to current pharmacological treatments. The primary aim of this study is to investigate the efficacy of a combined cognitive-aerobic training and a single aerobic training compared to an active control group in older adults with mild dementia...
March 21, 2017: BMC Geriatrics
https://www.readbyqxmd.com/read/28326461/toxicity-and-detoxification-mechanism-of-black-pepper-and-its-major-constituent-in-controlling-rhynchophorus-ferrugineus-olivier-curculionidae-coleoptera
#8
A Hussain, M Rizwan-Ul-Haq, H Al-Ayedh, A M Aljabr
The survival, feeding response, and detoxification mechanism of Rhynchophorus ferrugineus Olivier, a key pest responsible for destruction of date palm, was examined with different extracts of Piper nigrum and its major constituent (piperine) identified by GC-MS. In the present study, toxicity of different extracts of black pepper was evaluated by incorporating diffferent doses of extracts into the artificial diet of red palm weevil larvae. All extracts showed dose-dependent insecticidal activity to the tested eighth-instar red palm weevil larvae...
March 21, 2017: Neotropical Entomology
https://www.readbyqxmd.com/read/28320973/structure-of-the-infectious-salmon-anemia-virus-receptor-complex-illustrates-a-unique-binding-strategy-for-attachment
#9
Jonathan D Cook, Azmiri Sultana, Jeffrey E Lee
Orthomyxoviruses are an important family of RNA viruses, which include the various influenza viruses. Despite global efforts to eradicate orthomyxoviral pathogens, these infections remain pervasive. One such orthomyxovirus, infectious salmon anemia virus (ISAV), spreads easily throughout farmed and wild salmonids, constituting a significant economic burden. ISAV entry requires the interplay of the virion-attached hemagglutinin-esterase and fusion glycoproteins. Preventing infections will rely on improved understanding of ISAV entry...
March 20, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28319769/effects-of-different-cellulases-on-the-release-of-phenolic-acids-from-rice-straw-during-saccharification
#10
Yiyun Xue, Xiahui Wang, Xingxuan Chen, Jiajun Hu, Min-Tian Gao, Jixiang Li
Effects of different cellulases on the release of phenolic acids from rice straw during saccharification were investigated in this study. All cellulases tested increased the contents of phenolic acids during saccharification. However, few free phenolic acids were detected, as they were present in conjugated form after saccharification when the cellulases from Trichoderma reesei, Trichoderma viride and Aspergillus niger were used. On the other hand, phenolic acids were present in free form when the Acremonium cellulolyticus cellulase was used...
March 4, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28317491/predictive-value-of-the-leukocyte-esterase-test-for-the-detection-of-pleocytosis-in-cerebrospinal-fluid
#11
Shervin Shokouhi, Ilad Alavi Darazam, Mehdi Karamipour, HasanAli Ahmadi, Mohammad M Sajadi
BACKGROUND: Rapid and accurate diagnostic tests for patients with suspected bacterial meningitis is crucial to prevent subsequent mortality and morbidity. We carried out this study to determine diagnostic value of the rapid leukocyte esterase (LE) strip test to identify PMN pleocytosis in cerebral spinal fluid. METHODS: A total of 126 patients with suspected meningitis were enrolled in this prospective study. Microscopic examination (cell count and differential) and leukocyte esterase (LE) rapid strip test was performed on cerebrospinal fluid (CSF) samples...
March 17, 2017: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/28316396/sexual-alteration-in-antioxidant-response-and-esterase-profile-in-hyalomma-anatolicum-anatolicum-acari-ixodidae-ticks
#12
Mayukh Ghosh, Nirmal Sangwan, Arun K Sangwan, Rajesh Kumar, Ruchi Singh Gaur
The objective of the study was to reveal physiological link between sex specific engorgement pattern and evading mechanism of ticks against oxidative stress as well as acaricides. Quantitative determination of nitric oxide radical scavenging, superoxide dismutase activity and reduced glutathione (GSH) concentrations in salivary gland and gut extracts of male and female Hyalomma anatolicum anatolicum (Acari: Ixodidae) ticks established significant variation in antioxidant responses between two sexes of the ticks...
March 2017: Journal of Parasitic Diseases: Official Organ of the Indian Society for Parasitology
https://www.readbyqxmd.com/read/28316339/uv-mediated-thiol-ene-click-reactions-for-the-synthesis-of-drug-loadable-and-degradable-gels-based-on-copoly-2-oxazoline-s
#13
Klaus P Luef, Charlotte Petit, Bettina Ottersböck, Gernot Oreski, Francis Ehrenfeld, Bruno Grassl, Stéphanie Reynaud, Frank Wiesbrock
An 80-membered library of gels composed of monofunctional 2-ethyl-2-oxazoline and 2-nonyl-2-oxazoline and one of four selected difunctional 2-oxazolines (containing either ether or ester bonds) were synthesized by microwave-assisted ring-opening polymerizations. The difunctional 2-oxazolines were prepared from the thiol-ene reaction of glycol dimercaptoacetate or 2,2'-(ethylenedioxy)diethanethiol and 2-but-3'-enyl-2-oxazoline or 2-dec-9'-enyl-2-oxazoline. 53 of the gels exhibited glass-transition temperatures, which ranged from -5...
April 2017: European Polymer Journal
https://www.readbyqxmd.com/read/28314873/exploring-the-bioprospecting-and-biotechnological-potential-of-white-rot-and-anaerobic-neocallimastigomycota-fungi-peptidases-esterases-and-lignocellulolytic-enzymes
#14
REVIEW
Ronivaldo Rodrigues da Silva, Rafael Pedezzi, Tatiane Beltramini Souto
Fungi constitute an invaluable natural resource for scientific research, owing to their diversity; they offer a promising alternative for bioprospecting, thus contributing to biotechnological advances. For a long time, extensive information has been exploited and fungal products have been tested as a source of natural compounds. In this context, enzyme production remains a field of interest, since it offers an efficient alternative to the hazardous processes of chemical transformations. Owing to their vast biodiversity and peculiar biochemical characteristics, two fungal categories, white-rot and anaerobic Neocallimastigomycota, have gathered considerable attention for biotechnological applications...
March 17, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28303585/the-effect-of-depth-of-centrifuged-synovial-fluid-on-leukocyte-esterase-test-for-periprosthetic-joint-infection
#15
Pakpoom Ruangsomboon, Sriprapa Chinprasertsuk, Varanya Khejonnit, Keerati Chareancholvanich
Centrifugation of aspirated synovial fluid before leukocytes esterase (LE) testing for diagnosing periprosthetic joint infection (PJI) may make blood tinged specimens interpretable. We aimed to establish the proper sampling depth of centrifuged specimens for LE testing as one diagnostic criterion and also AS-D chloroacetate esterase (CAE) staining testing as an adjunctive tool. A definite PJI knee joint group and an aseptic primary total knee arthroplasty control group were studied quasi-experimentally (N = 46)...
March 17, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28300775/protective-effects-of-fucoidan-on-a%C3%AE-25-35-and-d-gal-induced-neurotoxicity-in-pc12-cells-and-d-gal-induced-cognitive-dysfunction-in-mice
#16
Hengyun Wei, Zixiang Gao, Luping Zheng, Cuili Zhang, Zundong Liu, Yazong Yang, Hongming Teng, Lin Hou, Yuling Yin, Xiangyang Zou
Alzheimer's disease (AD) is a chronic neurodegenerative disease which contributes to memory loss and cognitive decline in the elderly. Fucoidan, extracted from brown algae, is a complex sulfated polysaccharide and potential bioactive compound. In this study, we investigated whether fucoidan protects PC12 cells from apoptosis induced by a combination of beta-amyloid 25-35 (Aβ25-35) and d-galactose (d-Gal), and improves learning and memory impairment in AD model mice. The results indicated that fucoidan could inhibit the release of cytochrome c from the mitochondria to cytosol and activation of caspases, and increase the expression of apoptosis inhibitor proteins (IAPs), including livin and X-linked IAP (XIAP) in PC12 cells damaged by Aβ25-35 and d-Gal-induction...
March 16, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28299395/phenyl-valerate-esterase-activity-of-human-butyrylcholinesterase
#17
Iris Mangas, Eugenio Vilanova, Jorge Estévez
Phenyl valerate is used for detecting and measuring neuropathy target esterase (NTE) and has been used for discriminating esterases as potential target in hen model of organophosphorus delayed neuropathy. In previous studies we observed that phenyl valerate esterase (PVase) activity of an enzymatic fraction in chicken brain might be due to a butyrylcholinesterase protein (BuChE), and it was suggested that this enzymatic fraction could be related to the potentiation/promotion phenomenon of the organophosphate-induced delayed neuropathy (OPIDN)...
March 15, 2017: Archives of Toxicology
https://www.readbyqxmd.com/read/28298692/enrichment-of-maize-and-triticale-bran-with-recombinant-aspergillus-tubingensis-ferulic-acid-esterase
#18
Eunice N Zwane, Petrus J van Zyl, Kwaku G Duodu, Shaunita H Rose, Karl Rumbold, Willem H van Zyl, Marinda Viljoen-Bloom
Ferulic acid is a natural antioxidant found in various plants and serves as a precursor for various fine chemicals, including the flavouring agent vanillin. However, expensive extraction methods have limited the commercial application of ferulic acid, in particular for the enrichment of food substrates. A recombinant Aspergillus tubingensis ferulic acid esterase Type A (FAEA) was expressed in Aspergillus niger D15#26 and purified with anion-exchange chromatography (3487 U/mg, Km  = 0.43 mM, Kcat = 0.48/min on methyl ferulate)...
March 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28295488/identification-of-contaminant-interferences-which-cause-positive-urine-reagent-test-strip-reactions-in-a-cage-setting-for-the-laboratory-housed-nonhuman-primate-beagle-dog-and-sprague-dawley-rat
#19
William D Siska, Dennis J Meyer, Albert E Schultze, Catherine Brandoff
BACKGROUND: A high incidence of unexplained positive urine reagent test strip reactions was observed in healthy, untreated laboratory-housed nonhuman primates, Beagle dogs, and Sprague-Dawley rats. Exposure of urine to cage pan contaminants was the suspected cause of the positive reactions. OBJECTIVES: The objective of this study was to identify cage pan contaminants which could cause positive reagent test strip reactions. METHODS: Contaminated urine was simulated by exposing water samples to cage pan contaminants, including cleaning solutions, feces from nonhuman primates, Beagle dogs, and Sprague-Dawley rats, certified laboratory animal diets, and dietary enrichments (vegetables, fruits, and food treats)...
March 2017: Veterinary Clinical Pathology
https://www.readbyqxmd.com/read/28294564/cultivation-based-strategies-to-find-efficient-marine-biocatalysts
#20
Carlos J C Rodrigues, Ricardo F S Pereira, Pedro Fernandes, Joaquim M S Cabral, Carla C C R de Carvalho
Marine bacteria have evolved to survive in the marine environment by using unique physiological, biochemical and metabolic features and the ability to produce enzymes and compounds which may have commercial value. The Azores archipelago presents several ecosystems with strong volcanic activity where bacteria thrive under e.g. high temperatures. In this study, samples collected in the island of São Miguel were screened for biocatalysts possessing e.g. lipase, esterase, amylase, and inulinase activities. After isolation of several hundred bacterial strains, high throughput screening methods allowed the fast identification of biocatalysts...
March 10, 2017: Biotechnology Journal
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