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carboxylesterase

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https://www.readbyqxmd.com/read/28805379/cellular-transport-of-esculin-and-its-acylated-derivatives-in-caco-2-cell-monolayers-and-their-antioxidant-properties-in-vitro
#1
Mengmeng Zhang, Xuan Xin, Furao Lai, Xiaoyuan Zhang, Xiao-Feng Li, Hui Wu
Esculin has many pharmacological effects, but these are difficult to observe after oral administration owing to poor lipid solubility. In our previous study, five acylated derivatives with different acyl chain lengths (EA, EP, EO, EL, and EM) were synthesized to improve the lipophilicity of esculin. In this study, the bioavailability and antioxidant activity of the five derivatives were investigated. The logP of esculin, EA, EP, EO, EL, and EM were -1.1±0.1, -0.3±0.14, 0.1±0.17, 1.6±0.09, 2.4±0.11 and 2...
August 14, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28803225/carboxylesterase-1a2-encoding-gene-with-increased-transcription-and-potential-rapid-drug-metabolism-in-asian-populations
#2
Henrik Berg Rasmussen, Majbritt Busk Madsen, Yassine Kamal Lyauk, Peter Riis Hansen, Timothy Hughes
The carboxylesterase 1 gene (CES1) encodes a hydrolase implicated in the metabolism of commonly used drugs. CES1A2, a hybrid of CES1 and a CES1-like pseudogene, has a promoter that is weak in most individuals. However, some individuals harbor a promoter haplotype of this gene with two overlapping Sp1 sites that confer significantly increased transcription potentially leading to rapid drug metabolism. This CES1A2 haplotype has previously been reported to be common among Asians. Using polymerase chain reaction followed by sequencing, the present study examined variation in the promoter and 5' untranslated region of CES1A2 in 120 Han Chinese and 120 Japanese people enrolled in the 1000 Genomes Project...
August 14, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28799241/functional-characterization-of-carboxylesterase-gene-mutations-involved-in-aphis-gossypii-resistance-to-organophosphate-insecticides
#3
Y-H Gong, G-M Ai, M Li, X-Y Shi, Q-Y Diao, X-W Gao
Carboxylesterases (CarEs) play an important role in detoxifying insecticides in insects. Over-expression and structural modification of CarEs have been implicated in the development of organophosphate (OP) insecticide resistance in insects. A previous study identified four nonsynonymous mutations (resulting in four amino acid residue substitutions) in the open reading frame of the carboxylesterase gene of resistant cotton aphids compared to the omethoate susceptible strain, which has possibly influenced the development of resistance to omethoate (a systemic OP insecticide)...
August 11, 2017: Insect Molecular Biology
https://www.readbyqxmd.com/read/28794466/a-family-of-archaea-like-carboxylesterases-preferentially-expressed-in-the-symbiotic-phase-of-the-mychorrizal-fungus-tuber-melanosporum
#4
Davide Cavazzini, Guido Grossi, Elisabetta Levati, Francesca Vallese, Barbara Montanini, Angelo Bolchi, Giuseppe Zanotti, Simone Ottonello
An increasing number of esterases is being revealed by (meta) genomic sequencing projects, but few of them are functionally/structurally characterized, especially enzymes of fungal origin. Starting from a three-member gene family of secreted putative "lipases/esterases" preferentially expressed in the symbiotic phase of the mycorrhizal fungus Tuber melanosporum ("black truffle"), we show here that these enzymes (TmelEST1-3) are dimeric, heat-resistant carboxylesterases capable of hydrolyzing various short/medium chain p-nitrophenyl esters...
August 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28782481/rational-approaches-design-strategies-structure-activity-relationship-and-mechanistic-insights-for-esterase-inhibitors
#5
Harbinder Singh, Jatinder Vir Singh, Navdeep Kaur, Mohit Sanduja, Gurpreet Singh, Preet Mohinder Singh Bedi, Sahil Sharma
BACKGROUND: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of esterases are present in human body to control diverse set of cellular processes and execute their specific functions. It can be seen that any increase in metabolites produced by these enzymes lead to severe pathological conditions like Alzheimer disease, hypercholesterolemia etc. OBJECTIVE: Numerous esterase inhibitors have been developed and reported by the researchers around the globe, but not systematically summarized yet...
August 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28775293/effect-of-carboxylesterase-1-s75n-on-clopidogrel-therapy-among-acute-coronary-syndrome-patients
#6
Fei-Yan Xiao, Jian-Quan Luo, Min Liu, Bi-Lian Chen, Shan Cao, Zhao-Qian Liu, Hong-Hao Zhou, Gan Zhou, Wei Zhang
Carboxylesterase 1 (CES1) hydrolyzes the prodrug clopidogrel to an inactive carboxylic acid metabolite. The effects of CES1 S75N (rs2307240,C>T) on clopidogrel response among 851 acute coronary syndrome patients who came from the north, central and south of China were studied. The occurrence ratios of each endpoint in the CC group were significantly higher than in the CT + TT group for cerebrovascular events (14% vs 4.8%, p < 0.001, OR = 0.31), acute myocardial infarction (15.1% vs 6.1%, p < 0...
August 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28760607/phenolic-glycosides-and-monoterpenoids-from-the-roots-of-euphorbia-ebracteolata-and-their-bioactivities
#7
An-Hua Wang, Xiao-Kui Huo, Lei Feng, Cheng-Peng Sun, Sa Deng, Hou-Li Zhang, Bao-Jing Zhang, Xiao-Chi Ma, Jing-Ming Jia, Chao Wang
The bioactive substance investigation of Euphorbia ebracteolata obtained 17 compounds by various chromatographic techniques. Their structures were elucidated using widely spectroscopic data, including ESI-MS, HRESI-MS, CD, 1D- and 2D-NMR, which gave 5 new phenolic glucosides and 4 new monoterpenoids. The phenolic glucosides and monoterpenoids showed the inhibitory effect against the human carboxylesterase-2 (hCE-2) using a fluorescence bioassay in vitro, with the strongest inhibitor compound 4 (IC50 7.17μM)...
July 28, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28755688/differential-physiological-effects-of-neonicotinoid-insecticides-on-honey-bees-a-comparison-between-apis-mellifera-and-apis-cerana
#8
Zhiguo Li, Meng Li, Jingfang He, Xiaomeng Zhao, Veeranan Chaimanee, Wei-Fone Huang, Hongyi Nie, Yazhou Zhao, Songkun Su
Acute toxicities (LD50s) of imidacloprid and clothianidin to Apis mellifera and A. cerana were investigated. Changing patterns of immune-related gene expressions and the activities of four enzymes between the two bee species were compared and analyzed after exposure to sublethal doses of insecticides. Results indicated that A. cerana was more sensitive to imidacloprid and clothianidin than A. mellifera. The acute oral LD50 values of imidacloprid and clothianidin for A. mellifera were 8.6 and 2.0ng/bee, respectively, whereas the corresponding values for A...
August 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/28737453/the-metabolism-and-drug-drug-interaction-potential-of-the-selective-prostacyclin-receptor-agonist-selexipag
#9
Carmela Gnerre, Jérôme Segrestaa, Swen Seeland, Päivi Äänismaa, Thomas Pfeifer, Stephane Delahaye, Ruben de Kanter, Tomohiko Ichikawa, Tetsuhiro Yamada, Alexander Treiber
- The metabolism of selexipag has been studied in vivo in man and the main excreted metabolites were identified. Also, metabolites circulating in human plasma have been structurally identified and quantified. - The main metabolic pathway of selexipag in man is the formation of the active metabolite ACT-333679. Other metabolic pathways include oxidation and dealkylation reactions. All primary metabolites undergo subsequent hydrolysis of the sulphonamide moiety to their corresponding acids. ACT-333679 undergoes conjugation with glucuronic acid and aromatic hydroxylation to P10, the main metabolite detected in human faeces...
July 24, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28731595/identification-of-carboxylesterase-genes-associated-with-pyrethroid-resistance-in-the-malaria-vector-anopheles-sinensis-diptera-culicidae
#10
Xue-Mei Wu, Bo-Ying Xu, Feng-Ling Si, Jianyong Li, Zhen-Tian Yan, Zheng-Wen Yan, Xiu He, Bin Chen
BACKGROUND: Carboxylesterases (CCEs) are one of three large detoxification enzyme families. Some CCEs are active on synthetic insecticides with ester structures. Anopheles sinensis is an important malaria vector in eastern Asia. This study identified and characterized the CCE genes in the An. sinensis genome and determined CCE genes associated with pyrethroid resistance using RNA-seq and RT-qPCR, in An. sinensis from Anhui, Chongqing, and Yunnan in China. RESULTS: Fifty-seven putative CCEs were identified and placed into 3 classes, 12 subfamilies and 14 clades through phylogenetics and homology analyses...
July 21, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28719874/combined-effects-of-temperature-and-clomazone-gamit-%C3%A2-on-oxidative-stress-responses-and-b-esterase-activity-of-physalaemus-nattereri-leiuperidae-and-rhinella-schneideri-bufonidae-tadpoles
#11
Juliane Silberschmidt Freitas, Andreia Arantes Felício, Fabrício Barreto Teresa, Eduardo Alves de Almeida
Temperature is an important factor influencing the toxicity of chemicals in aquatic environments. Neotropical tadpoles experience large temperature fluctuations in their habitats and many species are distributed in areas impacted by agriculture. This study evaluated the effects caused by the exposure to clomazone (Gamit(®)) at different temperatures (28, 32 and 36 °C) on biochemical stress responses and esterase activities in Physalaemus nattereri and Rhinella schneideri tadpoles. Results evidenced that temperature modulates the effects of clomazone on biochemical response of tadpoles...
October 2017: Chemosphere
https://www.readbyqxmd.com/read/28713276/structure-activity-relationships-of-pentacyclic-triterpenoids-as-potent-and-selective-inhibitors-against-human-carboxylesterase-1
#12
Li-Wei Zou, Tong-Yi Dou, Ping Wang, Wei Lei, Zi-Miao Weng, Jie Hou, Dan-Dan Wang, Yi-Ming Fan, Wei-Dong Zhang, Guang-Bo Ge, Ling Yang
Human carboxylesterase 1 (hCE1), one of the most important serine hydrolases distributed in liver and adipocytes, plays key roles in endobiotic homeostasis and xenobiotic metabolism. This study aimed to find potent and selective inhibitors against hCE1 from phytochemicals and their derivatives. To this end, a series of natural triterpenoids were collected and their inhibitory effects against human carboxylesterases (hCEs) were assayed using D-Luciferin methyl ester (DME) and 6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate (DDAB) as specific optical substrate for hCE1, and hCE2, respectively...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28711984/clarithromycin-co-administration-does-not-increase-irinotecan-cpt-11-toxicity-in-colorectal-cancer-patients
#13
Katsuya Makihara, Sayaka Nakamura, Kazuyo Miyagi, Hiroyuki Ueno, Izumi Nakata
PURPOSE: Irinotecan (CPT-11) is used to treat advanced colorectal cancer. The drug is activated by carboxylesterases and rendered inactive by CYP3A4. Recently, the efficacy of combining CPT-11 and anti-epidermal growth factor receptor (EGFR) agents was confirmed in patients with KRAS wild-type metastatic colorectal cancer. Clarithromycin (CAM) is a strong CYP3A inhibitor often used to prevent rash associated with anti-EGFR therapy. The objective of this study was to evaluate the risk of increased neutropenia and diarrhea in combining CPT-11 and CAM...
July 15, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28697978/functional-characterization-of-bdb1-a-well-conserved-carboxylesterase-among-tephritid-fruit-flies-associated-with-malathion-resistance-in-bactrocera-dorsalis-hendel
#14
Luo-Luo Wang, Xue-Ping Lu, Guy Smagghe, Li-Wei Meng, Jin-Jun Wang
There are many evidences that insect carboxylesterase possess important physiological roles in xenobiotic metabolism and are implicated in the detoxification of organophosphate (OP) insecticides. Despite the ongoing resistance development in the oriental fruit fly, Bactrocera dorsalis (Hendel), the molecular basis of carboxylesterase and its ability to confer OP resistance remain largely obscure. This study was initiated to provide a better understanding of carboxylesterase-mediated resistance mechanism in a tephritid pest fly...
July 8, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28677105/carboxylesterases-in-lipid-metabolism-from-mouse-to-human
#15
REVIEW
Jihong Lian, Randal Nelson, Richard Lehner
Mammalian carboxylesterases hydrolyze a wide range of xenobiotic and endogenous compounds, including lipid esters. Physiological functions of carboxylesterases in lipid metabolism and energy homeostasis in vivo have been demonstrated by genetic manipulations and chemical inhibition in mice, and in vitro through (over)expression, knockdown of expression, and chemical inhibition in a variety of cells. Recent research advances have revealed the relevance of carboxylesterases to metabolic diseases such as obesity and fatty liver disease, suggesting these enzymes might be potential targets for treatment of metabolic disorders...
July 4, 2017: Protein & Cell
https://www.readbyqxmd.com/read/28667306/crystal-structure-of-pelagibacterium-halotolerans-pe8-new-insight-into-its-substrate-binding-pattern
#16
Ying-Yi Huo, Suhua Li, Jing Huang, Zhen Rong, Zhao Wang, Zhengyang Li, Rui Ji, Siyun Kuang, Heng-Lin Cui, Jixi Li, Xue-Wei Xu
Lysophospholipase_carboxylesterase (LPCE) has highly conserved homologs in many diverse species ranging from bacteria to humans, as well as substantial biological significance and potential therapeutic implications. However, its biological function and catalytic mechanism remain minimally investigated because of the lack of structural information. Here, we report the crystal structure of a bacterial esterase PE8 belonging to the LPCE family. The crystal structure of PE8 was solved with a high resolution of 1...
June 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28664339/metabolite-profiling-of-carbamazepine-and-ibuprofen-in-solea-senegalensis-bile-using-high-resolution-mass-spectrometry
#17
Jaume Aceña, Sandra Pérez, Peter Eichhorn, Montserrat Solé, Damià Barceló
The widespread occurrence of pharmaceuticals in the aquatic environment has raised concerns about potential adverse effects on exposed wildlife. Very little is currently known on exposure levels and clearance mechanisms of drugs in marine fish. Within this context, our research was focused on the identification of main metabolic reactions, generated metabolites, and caused effects after exposure of fish to carbamazepine (CBZ) and ibuprofen (IBU). To this end, juveniles of Solea senegalensis acclimated to two temperature regimes of 15 and 20 °C for 60 days received a single intraperitoneal dose of these drugs...
June 29, 2017: Analytical and Bioanalytical Chemistry
https://www.readbyqxmd.com/read/28660514/monitoring-of-organic-pollutants-in-marine-environment-by-semipermeable-membrane-devices-and-mussels-accumulation-and-biochemical-responses
#18
Oya S Okay, Burak Karacık, Abbas Güngördü, Atilla Yılmaz, Nazmi C Koyunbaba, Sevil D Yakan, Bernhard Henkelmann, Karl-Werner Schramm, Murat Ozmen
This study involves the monitoring of organic pollutants using transplanted mussels (Mytilus galloprovincialis) as bioindicator organisms and semipermeable membrane devices (SPMDs) as passive samplers. Mussels and SPMDs were deployed to marinas, shipyards and shipbreaking yards on the coastal area of Turkey and retrieved after 60 days. Polycyclic aromatic hydrocarbons (PAH), polychlorinated biphenyls (PCB) and organochlorine pesticide (OCP) compounds were analysed with high-resolution GC-MS. Total PAH concentrations in SPMDs and mussels ranged from 200 to 4740 ng g sampler(-1) and from 7...
June 28, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28647840/interaction-of-ferulic-acid-with-glutathione-s-transferase-and-carboxylesterase-genes-in-the-brown-planthopper-nilaparvata-lugens
#19
Jun Yang, Xiao-Qin Sun, Shu-Ying Yan, Wen-Jun Pan, Mao-Xin Zhang, Qing-Nian Cai
Plant phenolics are crucial defense phytochemicals against herbivores and glutathione S-transferase (GST) and carboxylesterase (CarE) in herbivorous insects are well-known detoxification enzymes for such xenobiotics. To understand relationship between a plant phenolic and herbivore GST or CarE genes, we evaluated the relationship between a rice phenolic ferulic acid and resistance to brown planthopper (BPH, Nilaparvata lugens), and investigated the interaction of ferulic acid with GST or CarE genes in BPH. The results indicate that ferulic acid content in tested rice varieties was highly associated with resistance to BPH...
June 24, 2017: Journal of Chemical Ecology
https://www.readbyqxmd.com/read/28647665/comparative-metabolism-of-ddao-benzoate-in-liver-microsomes-from-various-species
#20
Hong-Ying Ma, Jia-Da Yang, Jie Hou, Li-Wei Zou, Qiang Jin, Da-Cheng Hao, Jing Ning, Guang-Bo Ge, Ling Yang
DDAB (6,8-dichloro-9,9-dimethyl-7-oxo-7,9-dihydroacridin-2-yl benzoate) is a newly developed near-infrared fluorescent probe for human carboxylesterase 2 (hCE2), exhibiting high specificity and good reactivity for real-time monitoring the enzymatic activities of hCE2 in complex biological systems. In order to explore the applicability of DDAB in commonly used animal species, the interspecies difference in DDAB hydrolysis was carefully investigated by using liver microsomes from human and five experimental animals including mouse, rat, dog, minipig and monkey...
June 21, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
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